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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 6006. Отображено 100.
12-01-2012 дата публикации

Novel liquid-crystalline compound and organic semiconductor device containing the compound

Номер: US20120007062A1
Автор: Tetsuharu Miwa, YASUYUKI Sasada
Принадлежит: JNC Corp

Disclosed is a visible light-transmissive liquid-crystalline compound having good hole and electron-transport characteristics and useful as an organic semiconductor material. The compound is represented by a formula (1): wherein R independently represents hydrogen, or alkyl having from 1 to 24 carbon atoms, and any —CH 2 — in the alkyl may be replaced by —O—, —S—, —CO— or —SiH 2 —, any —(CH 2 ) 2 — may be replaced by —CH≡CH— or —C═C—, and any hydrogen may be replaced by halogen; Ar represents naphthylene, anthrylene, phenanthrylene, or phenylene; and every hydrogen in phenylene is replaced by halogen, and any hydrogen in naphthylene, anthrylene and phenanthrylene may be replaced by halogen.

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Номер записи: 1
21-02-2013 дата публикации

Plant treatment

Номер: US20130045968A1
Автор: Norman Helie
Принадлежит: Individual

An anti-fungal treatment for trees and bushes. Included are all methods of delivery of active ingredients, including foliar and trunk spraying application, granular soil surface, soil drench, soil injection, and trunk injection. The chemical combination includes a group 3 fungicide like propiconazole, that is, a systemic with curative and protective action, that works via the demethylation of C-14 during ergosterol biosynthesis. The combination also includes a group 11 fungicide like Azoxystrobin, or Fluoxastrobin for which their biochemical mode of action is inhibition of electron transport. The combined efficacy of there two classes of chemicals is reduced spreading of the fungus and increased killing of fungus. It has also been found that these chemicals used individually on trees and bushes, have unexpected benefits.

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Номер записи: 2
21-03-2013 дата публикации

Inhibitors of Ion Channels

Номер: US20130072471A1
Автор: Fritch Paul Christopher, Markworth Christopher John, Marron Brian Edward, Maynard Andrew Thomas, Swain Nigel Alan
Принадлежит:

Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel. 2. The compound of claim 1 , with the proviso that the compound of formula (I) is not one of the following compounds:N-(5-methyl-3-isoxazolyl)-3-[[(5-methyl-3-isoxazolyl)amino]sulfonyl]-benzamide;3-[[(5-methyl-3-isoxazolyl)amino]sulfonyl]-N-1,3,4-thiadiazol-2-yl-benzamide;N-(5-ethyl-1,3,4-thiadiazol-2-yl)-3-(4-morpholinylcarbonyl)-benzenesulfonamide;1-[3-[[[5-(1,1-dimethylethyl)-4-methyl-2-thiazolyl]amino]sulfonyl]benzoyl]piperidine;N-(5-methyl-1,3,4-thiadiazol-2-yl)-3-(4-morpholinylcarbonyl)-benzenesulfonamide; andN-methyl-4-[[(1-methyl-1H-pyrazol-3-yl)amino]sulfonyl]-benzamide.3. The compound according to claim 2 , or a pharmaceutically acceptable salt claim 2 , wherein{'sup': '5', 'sub': 1', '10', '3', '8, 'Ris a member selected from (C-C)alkyl and (C-C)cycloalkyl,'}{'sub': 1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4, 'wherein each is optionally substituted with one or more substituents selected from the group consisting of oxo, halogen, cyano, hydroxy, hydroxy(C-C)alkyl, hydroxy(C-C)alkoxy, (C-C)alkyl, halo(C-C)alkyl, (C-C)alkoxy, halo(C-C)alkoxy and phenyl.'}4. The compound according to claim 3 , or a pharmaceutically acceptable salt claim 3 , wherein Ris a member selected from (C-C)alkyl claim 3 , hydroxy(C-C ...

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Номер записи: 3
04-04-2013 дата публикации

Gamma-glutamyl transpeptidase inhibitors and methods of use

Номер: US20130085168A1
Автор: Marie H. Hanigan
Принадлежит: University of Oklahoma

Compositions and methods for inhibiting human gamma-glutamyl transpeptidase (GGT) in vivo or in vitro and for inhibiting and killing neoplastic cancer cells, for example for the treatment, inhibition or prevention of tumors or malignant growths or other neoplasias in mammals, or sensitizing tumor to other therapies including radiation therapy. The GGT inhibitor compounds comprise a class of benzylthiadiazol benzenesulfoniamides. The compounds may also be used to treat a reversible airways obstruction in a mammal or a disease associated with reverse airways obstruction such as asthma, chronic obstructive pulmonary disease (COPD), allergic reaction, respiratory tract infection or upper respiratory tract disease. Other diseases or conditions which may be treated include, for example, degenerative diseases, renal diseases, liver diseases, cardiovascular disease and inner ear conditions or diseases.

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Номер записи: 4
18-04-2013 дата публикации

POLYMERS WITH TUNABLE BAND GAPS FOR PHOTONIC AND ELECTRONIC APPLICATIONS

Номер: US20130092912A1
Автор: You Wei
Принадлежит:

The present invention provides, among other things, a copolymer comprising at least one donor monomer and at least one acceptor monomer. The polymer may optionally further comprise at least one additional comonomer. The polymers are useful as a charge-transport, semiconducting, electrochemical conducting, photoconducting, or light emitting material. Microelectronic devices comprising such polymers (e.g., as a heterojunction therein) are also described. 2. The copolymer of having a number average molecular weight of from 500 to 1 claim 1 ,000 claim 1 ,000 grams per mole.3. The copolymer of claim 1 , further comprising at least one additional comonomer.11. The copolymer of claim 10 , wherein Rand Rare fluoro.12. The copolymer of claim 10 , wherein each R and Ris C1-C20 alkyl.13. The copolymer of claim 10 , wherein R claim 10 , R claim 10 , Rand Rare each H.14. The copolymer of claim 10 , having a number average molecular weight for said polymer of from 500 to 1 claim 10 ,000 claim 10 ,000 grams per mole.16. The polymer of having a number average molecular weight of from 500 to 1 claim 15 ,000 claim 15 ,000 grams per mole.17. The polymer of claim 15 , wherein said polymer is a homopolymer.18. The polymer of claim 15 , wherein said polymer is a copolymer with at least one additional monomer.20. (canceled)21. A microelectronic device comprising a polymer of .22. The device of claim 21 , wherein said device is an optoelectronic device.23. The device of claim 21 , wherein said polymer comprises a heterojunction in said device.24. The device of claim 21 , wherein said device is a photovoltaic cell claim 21 , field effect transistor claim 21 , light emitting diode claim 21 , photodectector claim 21 , photovoltaic detector claim 21 , imaging device claim 21 , lasing device claim 21 , storage element claim 21 , amplifier claim 21 , emitter claim 21 , or electrochromic display.25. The device of claim 21 , wherein said device comprises a first electrode claim 21 , a second ...

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Номер записи: 5
02-05-2013 дата публикации

Chemical Compounds

Номер: US20130109696A1
Автор: Greener Benjamin Scott, Marron Brian Edward, Millan David Simon, Rawson David James, Storer Robert Ian, Swain Nigel Alan
Принадлежит: PFIZER LIMITED

The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y, Y, Z, R, Rand Rare as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain. 2. A compound according to wherein X is S.3. A compound according to wherein X is CH.4. A compound according to wherein Z is either (a) a ‘C-linked’ 5-membered heteroaryl group containing two nitrogen atoms and one sulphur atom claim 1 , or (b) a ‘C-linked’ 6-membered heteroaryl group containing two nitrogen atoms.5. A compound according to wherein Z is ‘C-linked’ thiadiazolyl or ‘C-linked’ a pyrimidinyl.6. A compound according to wherein Yis Cl and Yis F.7. A compound according to wherein Yis CN and Yis H.8. A compound according to wherein Rand Rare independently H claim 1 , F claim 1 , Cl or R.9. A compound according to wherein Rand Rare independently H claim 1 , F claim 1 , CFor OCH.10. A compound according to wherein Ris H claim 1 , F claim 1 , Ror Het.11. A compound according to wherein Ris H; F; (C-C)alkyl claim 1 , optionally substituted by one to three halo atoms; (C-C)alkyloxy claim 1 , such as methoxy; or a ‘C-linked’ 6-membered heteroaryl group comprising one or two nitrogen atoms claim 1 , optionally substituted on a carbon atom by NH.12. A pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof together claim 1 , as defined in claim 1 , with one or more pharmaceutically acceptable excipients.13. A pharmaceutical composition according to including one or more additional therapeutic agents.14. (canceled)15. (canceled)16. (canceled)17. (canceled)18. A method of treating a disorder in a human or animal for which a ...

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Номер записи: 6
16-05-2013 дата публикации

MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF USING THE SAME

Номер: US20130123246A1
Автор: Combs Andrew P., Yue Eddy W.
Принадлежит: INCYTE CORPORATION

The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof. 2. The compound of wherein Ring A is heterocyclyl optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 R.3. The compound of wherein Ring A is 5- or 6-membered heterocyclyl optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 R.4. The compound of wherein Ring A is 5-membered heterocyclyl optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 R.5. The compound of wherein Ring A is 5-membered heterocyclyl containing at least one ring-forming N atom and Ring A is optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 R.6. The compound of wherein Ring A is 5-membered heterocyclyl containing at least one ring-forming O atom and Ring A is optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 R.7. The compound of wherein Ring A is 5-membered heterocyclyl containing at least one ring-forming O atom and containing at least one ring-forming N atom claim 1 , and Ring A is optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 R.10. The compound of wherein Ris H claim 1 , C(O)R claim 1 , C(O)NRR claim 1 , or C(O)OR.11. The compound of wherein Ris H.12. The compound of wherein Ris H.13. The compound of wherein a and b are both 0.14. The compound of wherein Ris aryl claim 1 , cycloalkyl claim 1 , heteroaryl claim 1 , or heterocycloalkyl claim 1 , each optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 substituents independently selected from halo claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , Chaloalkyl claim 1 , Chydroxyalkyl claim 1 , Cy claim 1 , CN claim 1 , NO claim 1 , OR claim 1 , SR claim 1 , C(O)R claim 1 , C(O)NRR claim 1 , C(O)OR claim 1 , OC(O)R claim 1 , OC(O)NRR claim 1 , NRC(O)NRR claim 1 , NRR claim 1 , NRC(O)R claim 1 , NRC(O)OR claim 1 , C(═NR)NRR claim 1 , NRC(═NR)NRR claim 1 , P(R) claim 1 , P( ...

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Номер записи: 7
20-06-2013 дата публикации

COMPOSITION AND METHOD FOR CONTROLLING PESTS

Номер: US20130157849A1
Автор: Kurahashi Makoto, Matsuzaki Yuichi
Принадлежит: Sumitomo Chemical Company, Limited

The present invention provides a composition for controlling pests comprising, as active ingredients, ethaboxam and a neonicotinoid compound represented by formula (1); and so on. 17-. (canceled)9. The composition for controlling pests according to claim 8 , wherein the neonicotinoid compound represented by formula (1) is selected from the group consisting of nitenpyram claim 8 , dinotefuran claim 8 , acetamiprid and thiacloprid.10. The composition for controlling pests according to claim 8 , which has a weight ratio of ethaboxam to the neonicotinoid compound represented by formula (1) of falling within the range of from 1:0.125 to 1:500.11. A seed treatment agent comprising claim 8 , as active ingredients claim 8 , ethaboxam and the neonicotinoid compound represented by formula (1) of ;{'b': '1', 'wherein the neonicotinoid compound represented by formula () is selected from the group consisting of clothianidin, thiamethoxam, imidacloprid, nitenpyram, dinotefuran, acetamiprid and thiacloprid.'}12. A plant seed treated with effective amounts of ethaboxam and the neonicotinoid compound represented by formula (1) of ;wherein the neonicotinoid compound represented by formula (1) is selected from the group consisting of clothianidin, thiamethoxam, imidacloprid, nitenpyram, dinotefuran, acetamiprid and thiacloprid.13. A method for controlling pests which comprises applying claim 8 , to a plant or a locus where a plant is allowed to grow claim 8 , effective amounts of ethaboxam and the neonicotinoid compound represented by formula (1) of ;wherein the neonicotinoid compound represented by formula (1) is selected from the group consisting of clothianidin, thiamethoxam, imidacloprid, nitenpyram, dinotefuran, acetamiprid and thiacloprid. The present invention relates to a composition for controlling pests and a method for controlling pests.A fungicidal compound, ethaboxam (KR-B-0124552) and insecticidal neonicotinoid compounds (“The Pesticide Manual—14th edition” published by ...

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Номер записи: 8
20-06-2013 дата публикации

HETEROCYCLIC INHIBITORS OF GLUTAMINASE

Номер: US20130157998A1
Автор: Chen Lijing, Goyal Bindu, Laidig Guy, Li Jim, Sjogren Eric Brian, Stanton Timothy Friend
Принадлежит: CALITHERA BIOSCIENCES INC.

The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention. 2. The method of claim 1 , wherein L represents CHSCH claim 1 , CHCH claim 1 , CHS or SCH.3. The method of claim 1 , wherein L represents CHCH.4. The method of any preceding claim claim 1 , wherein Y represents H.5. The method of any preceding claim claim 1 , wherein X claim 1 , independently for each occurrence claim 1 , represents S or CH═CH claim 1 , wherein any hydrogen atom of a CH unit may be replaced by alkyl.6. The method of any preceding claim claim 1 , wherein Z represents R(CO).7. The method of claim 6 , wherein each occurrence of Ris not identical.8. The method of any preceding claim claim 6 , wherein Rand Reach represent H.9. The method of any preceding claim claim 6 , wherein R claim 6 , independently for each occurrence claim 6 , represents substituted or unsubstituted arylalkyl claim 6 , heteroarylalkyl claim 6 , cycloalkyl or heterocycloalkyl.10. The method of any preceding claim claim 6 , wherein R claim 6 , independently for each occurrence claim 6 , represents C(R)(R)(R) claim 6 , wherein Rrepresents substituted or unsubstituted aryl claim 6 , arylalkyl claim 6 , heteroaryl or heteroaralkyl claim 6 , Rrepresents H claim 6 , and Rrepresents hydroxy claim 6 , hydroxyalkyl claim 6 , alkoxy or alkoxyalkyl.11. The method of claim 10 , wherein Rrepresents substituted or unsubstituted aryl claim 10 , arylalkyl claim 10 , or heteroaryl.12. The method of or claim 10 , wherein Rrepresents hydroxy claim 10 , hydroxyalkyl claim 10 , or alkoxy.13. The method of claim 1 , wherein L represents CHSCH claim 1 , CHCH claim 1 , CHS or SCH claim 1 , Y represents H claim 1 , X represents S claim 1 , Z represents R(CO) claim 1 , Rand Reach represent H claim 1 , and R claim 1 , independently for each occurrence claim 1 , represents substituted or unsubstituted ...

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Номер записи: 9
27-06-2013 дата публикации

CONJUGATED POLYMERS

Номер: US20130161567A1
Автор: Blouin Nicolas, Carrasco-Orozco Miguel, Meyer Frank Egon, Mitchell William, Tierney Steven
Принадлежит: Merck Patent Gesellschaft Mit Beschrankter Haftung

The invention relates to novel polymers containing repeating units based on benzo[2,1,3]thiadiazole-5,6-dicarboxylic acid bis-ester, monomers and methods for their preparation, their use as semiconductors in organic electronic (OE) devices, especially in organic photovoltaic (OPV) devices, and to OE and OPV devices comprising these polymers. 2. Polymer according to claim 1 , wherein Rand Rin formula I are selected from straight-chain claim 1 , branched or cyclic alkyl with 1 to 35 C atoms claim 1 , in which one or more non-adjacent C atoms are optionally replaced by —O— claim 1 , —S— claim 1 , —C(O)— claim 1 , —C(O)—O— claim 1 , —O—C(O)— claim 1 , —O—C(O)—O— claim 1 , —CR═CR— or —C≡C— and in which one or more H atoms are optionally replaced by F claim 1 , Cl claim 1 , Br claim 1 , I or CN claim 1 , or denote aryl claim 1 , heteroaryl claim 1 , aryloxy claim 1 , heteroaryloxy claim 1 , arylcarbonyl claim 1 , heteroarylcarbonyl claim 1 , arylcarbonyloxy claim 1 , heteroarylcarbonyloxy claim 1 , aryloxycarbonyl or heteroaryloxycarbonyl having 4 to 30 ring atoms that is unsubstituted or substituted by one or more non-aromatic groups R claim 1 , wherein{'sup': 3', '0', '00', '0', '0', '0', '00', '0', '0, 'sub': 2', '3', '2', '2', '3', '5, 'Ris on each occurrence identically or differently F, Br, Cl, —CN, —NC, —NCO, —NCS, —OCN, —SCN, —C(O)NRR, —C(O)X, —C(O)R, —NH, —NRR, —SH, —SR, —SOH, —SOR, —OH, —NO, —CF, —SF, optionally substituted silyl, carbyl or hydrocarbyl with 1 to 40 C atoms that is optionally substituted and optionally comprises one or more hetero atoms, or P-Sp-,'}{'sup': 0', '00, 'sub': '1-40', 'Rand Rare independently of each other H or optionally substituted Ccarbyl or hydrocarbyl,'}P is a polymerisable or crosslinkable group,Sp is a spacer group or a single bond, and{'sup': '0', 'Xis halogen.'}4. Polymer according to claim 3 , which is selected of formula IIa{'br': None, 'sup': 4', '1', '2', '3', '5, 'sub': x', 'y', 'n, 'R—[(Ar—U—Ar)—(Ar)]—R\u2003\u2003IIa ...

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Номер записи: 10
04-07-2013 дата публикации

PREVENTION OF INDWELLING DEVICE RELATED INFECTION: COMPOSITION AND METHODS

Номер: US20130172260A1
Автор: Polaschegg Hans-Dietrich
Принадлежит:

Catheters used for medical treatment, e.g., hemodialysis are filled with a locking solution, usually heparin between treatments. To prevent infections, antimicrobial or antibiotic substances have been used as locking solution alone or in combination with antithrombotic substances. It has been found that these locking solutions are rapidly washed out from the catheter tip. The invention describes a thixotropic gel that can be used as locking solution. Beneficial substances, e.g., antimicrobial or antibiotic substances can be added to the gel. A preferred antimicrobial substance is taurolidine alone or in combination with salicylic acid or one of its salts. 1. A composition comprising a pharmaceutically acceptable gel containing an antimicrobial agent used for catheter protection.2. A composition as claimed in wherein said gel is thixotropic.3. A composition as in wherein said gel is a hydrogel.4. A composition as in wherein said gel is a microgel.5. A composition as in wherein the antimicrobial agent is taurolidine claim 1 , taurultam or a mixture thereof.6. A composition as claimed in wherein said gel also contains an medically acceptable anticoagulant agent.7. A composition as claimed in any of the wherein said composition contains salicylic acid or one of its salts.8. A composition as claimed in wherein said gel can be injected into an indwelling catheter and said gel can be withdrawn from a catheter using conventional medical syringes.9. A locking agent for an indwelling catheter that is composed of a thixotropic gel or a colloidal fluid that is retained in the catheter with minimal loss during instillation and/or the duration between uses of the catheter and can be instilled and withdrawn using a syringe.10. A catheter lock solution according to in which the agent is albumin. This invention relates to methods and compositions, which prevent biofilm formation on or near medical prosthetic devices in order to reduce patient infection related to indwelling devices. ...

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Номер записи: 11
18-07-2013 дата публикации

HERBICIDAL COMPOSITIONS CONTAINING BENTAZON AND ALS INHIBITOR AND ACCASE INHIBITOR

Номер: US20130184156A1
Автор: Huang Yi-hsiou, Mann Richard K., Nguyen Lap
Принадлежит: DOW AGROSCIENCES LLC

Herbicidal compositions comprising (a) bentazon-sodium and (b) an ALS inhibitor and (c) an ACCase inhibitor controls susceptible and resistant weeds in crops, e.g., rice, wheat, barley, oats, rye, sorghum, corn/maize, pastures, grasslands, rangelands, fallowland, turf, tree and vine orchards and IVM, but also additionally in ALS and ACC'ase tolerant crops. 1. A herbicidal composition comprising three herbicidal active ingredients , wherein the first herbicidal active ingredient is bentazon-sodium , the second herbicidal active ingredient is an ALS inhibitor , and the third herbicidal active ingredient is an ACCase inhibitor.2. The composition of claim 1 , wherein the ALS inhibitor is penoxsulam claim 1 , bispyribac-sodium claim 1 , azimsulfuron claim 1 , bensulfuron-methyl claim 1 , chloransulam claim 1 , cinosulfuron claim 1 , diclosulam claim 1 , ethoxysulfuron claim 1 , flazasulfuron claim 1 , florasulam claim 1 , flumetsulam claim 1 , halosulfuron-methyl claim 1 , imazamox claim 1 , imazethapyr claim 1 , imazosulfuron claim 1 , iofensulfuron claim 1 , metazosulfuron claim 1 , metsulfuron-methyl claim 1 , orthosulfamuron claim 1 , propyrisulfuron claim 1 , pyrazosulfuron-ethyl claim 1 , pyribenzoxim claim 1 , pyriftalid claim 1 , pyriminobac-methyl claim 1 , pyrimisulfan claim 1 , pyroxsulam or triafamone.3. The composition of claim 1 , wherein the ACCase inhibitor is cyhalofop-butyl claim 1 , fenoxaprop-P-ethyl claim 1 , clodinafop-propyrgyl claim 1 , diclofop-methyl claim 1 , fluazifop-P-butyl claim 1 , haloxyfop-methyl claim 1 , propaquizafop claim 1 , quizalofop-P-ethyl claim 1 , clethodim claim 1 , cycloxydim claim 1 , profoxydim claim 1 , sethoxydim claim 1 , tepraloxydim claim 1 , tralkoxydim or pinoxaden.4. The composition of claim 1 , wherein ALS inhibitor is penoxsulam and the ACCase inhibitor is cyhalofop butyl.5. The composition of claim 3 , wherein the weight ratio of (a) bentazon-sodium to (b) penoxsulam to (c) cyhalofop-butyl is (a) 50-150 to (b) 0 ...

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Номер записи: 12
18-07-2013 дата публикации

APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES

Номер: US20130184278A1
Автор: Elmore Steven W., Hexamer, Kunzer Aaron R., Park Cheol-Min, Souers Andrew J., SR. Laura, Sullivan Gerard M., Wang Gary T., Wang Xilu, Wendt Michael D.
Принадлежит: ABBOTT LABORATORIES

Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein. 5. The compound of claim 1 , or therapeutically acceptable salt thereof claim 1 , wherein the compound is selected from the group consisting of:4-[4-(cyclohexylmethyl)-4-methoxypiperidin-1-yl]-N-{[5-({(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}benzamide;N-{[5-({(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}-4-[4-methoxy-4-(3-methylbenzyl)piperidin-1-yl]benzamide;N-{[5-({(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}-4-[4-(3,3-diphenylprop-2-enyl)piperazin-1-yl]benzamide;4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl}-N-[(4-{[2-(phenylthio)ethyl]amino}piperidin-1-yl)sulfonyl]benzamide;N-[(4-{acetyl[2-(phenylthio)ethyl]amino}piperidin-1-yl)sulfonyl]-4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl}benzamide;4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl}-N-[(4-{methyl[2-(phenylthio)ethyl]amino}piperidin-1-yl)sulfonyl]benzamide;4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl}-N-{[5-({(1R)-3-[isopropyl(methyl)amino]-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}benzamide;4-(4-{[2-(4-chlorophenyl)cyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-({(1R)-3-[isopropyl(methyl)amino]-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}benzamide;4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-({(1R)-3-[isopropyl(methyl)amino]-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}benzamide;N-{[(5Z)-5-(acetylimino)-4-methyl-4,5-dihydro-1,3,4-thiadiazol-2-yl]sulfonyl}-4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl}benzamide;N-({5-[(benzoylamino)methyl]thien-2-yl}sulfonyl)-4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl ...

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Номер записи: 13
18-07-2013 дата публикации

SMALL MOLECULE INHIBITORS OF THE PLECKSTRIN HOMOLOGY DOMAIN AND METHODS FOR USING SAME

Номер: US20130184317A1
Автор: GOHKALE Vijay M., JR. Eugene A., MAHADEVAN Daruka, MASH, MEUILLET Emmanuelle J., POWIS Garth, ZHANG Shuxing
Принадлежит:

Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein. 181-. (canceled)83. The compound of wherein{'sup': 2', '6', '6a', '6b, 'sub': 6', '20', '2, 'Ris a C-Calkyl, optionally substituted with one or more substituents independently selected from halogen, —OH, —NH, —NHC(O)R, and —NRR;'}{'sup': 6', '7', '7', '7', '7, 'sub': 3', '2', '3', '2', '2', '3', '6', '5', '6', '4', '2', '6', '5', '2', '6', '4', '1', '20', '1', '20', '2', '3', '2', '3', '2', '2', '3', '1', '6', '6', '5', '6', '4', '2', '6', '5', '2', '6', '4, 'Ris —CH, —CHCH, —CHCHCH, —CH, —CHR, —CHCH, —CHCHR, aryl, heteroaryl, or —C-Calkyl, wherein each of the aryl, heteroaryl, or —C-Calkyl may optionally be substituted with one or more substituents independently selected from —NH, —OH, —CH, —CHCH—CHCHCH—C-Calkyl, —CH, —CHR, —CHCH, —CHCHRand halogen;'}{'sup': '6a', 'Rmay be H or methyl;'}{'sup': '6b', 'sub': 6', '5, 'Rmay be methyl 7-nitrobenzene[c][1,2,5]oxadiazole-4-yl, or —C(O)CH; and'}{'sup': '7', 'sub': 3', '3', '3', '2', '3', '2', '2', '2', '2', '3', '2', '3', '2, 'Rmay be —H, —CH, heteroaryl, —C(CH), —OH, —NH, —NHC(O)CH, —S(O)OH, —P(O))H, —As(O)OH, —NO, —OCH, —OCHCH, —C(O)OH, —C(O)NH, or halogen.'}84. The compound of or pharmaceutically acceptable salt thereof claim 82 , wherein Ris a C-Calkyl.85. The compound of or pharmaceutically acceptable salt thereof claim 82 , wherein Ris a straight C-Calkyl.86. The compound of or pharmaceutically acceptable salt thereof claim 82 , wherein Ris a C-Calkyl.87. The compound of or pharmaceutically acceptable salt thereof claim 82 , wherein Ris a C-Calkyl.88. The compound of or pharmaceutically acceptable salt thereof claim 82 , wherein Ris a C-Calkyl.89. The compound of or pharmaceutically acceptable salt thereof claim 82 , wherein Ris —(CH)CH.92. The pharmaceutical composition of claim 91 , wherein:{'sup': 2', '6', '6a', '6b, 'sub': 6', '20', '2, 'Ris a C-Calkyl, optionally ...

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Номер записи: 14
08-08-2013 дата публикации

PESTICIDAL MIXTURES

Номер: US20130203590A1
Автор: Grimm Christoph, Haas Ulrich Johannes, Skillman Stephen Wilson
Принадлежит: SYNGENTA CROP PROTECTION LLC

Mixtures comprising cis-jasmone and an agrochemical active ingredient are useful in agriculture. 1. A mixture comprising cis-jasmone and a component B , wherein component B is an agrochemical active ingredient.2. A mixture according to wherein component B is a compound selected froma) a pyrethroid selected from the group consisting of permethrin, cypermethrin, fenvalerate, esfenvalerate, deltamethrin, cyhalothrin, lambda-cyhalothrin, gamma-cyhalothrin, bifenthrin, fenpropathrin, cyfluthrin, tefluthrin, ethofenprox, natural pyrethrin, tetramethrin, S-bioallethrin, fenfluthrin, prallethrin and5-benzyl-3-furylmethyl-(E)-(1R,3S)-2,2-dimethyl-3-(2-oxothiolan-3-ylidenemethyl)cyclopropane carboxylate;b) an organophosphate selected from the group consisting of sulprofos, acephate, methyl parathion, azinphos-methyl, demeton-s-methyl, heptenophos, thiometon, fenamiphos, monocrotophos, profenofos, triazophos, methamidophos, dimethoate, phosphamidon, malathion, chlorpyrifos, phosalone, terbufos, fensulfothion, fonofos, phorate, phoxim, pirimiphos-methyl, pirimiphos-ethyl, fenitrothion, fosthiazate and diazinon;c) a carbamate selected from the group consisting of pirimicarb, triazamate, cloethocarb, carbofuran, furathiocarb, ethiofencarb, aldicarb, thiofurox, carbosulfan, bendiocarb, fenobucarb, propoxur, methomyl and oxamyl;d) a benzoyl urea selected from the group consisting of diflubenzuron, triflumuron, hexaflumuron, flufenoxuron, lufenuron and chlorfluazuron;e) an organic tin compound selected from the group consisting of cyhexatin, fenbutatin oxide and azocyclotin;f) a pyrazole selected from the group consisting of tebufenpyrad and fenpyroximate;g) a macrolide selected from the group consisting of abamectin, emamectin, ivermectin, milbemycin, spinosad, azadirachtin and spinetoram;h) an organochlorine compound selected from the group consisting of endosulfan, benzene hexachloride, DDT, chlordane and dieldrin;i) an amidine selected from the group consisting of chlordimeform ...

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Номер записи: 15
08-08-2013 дата публикации

CYCLIC AMIDE DERIVATIVE

Номер: US20130203739A1
Автор: Makabe Muneyoshi, Ohkouchi Munetaka, Okano Akihiro
Принадлежит: MOCHIDA PHARMACEUTICAL CO., LTD.

[Problem] 4. The compound according to claim 3 , wherein X is an oxygen atom claim 3 , k is 0 claim 3 , and any one of q and s is 1 or more claim 3 ,a salt of the compound, or a solvate of the compound or the salt.6. The compound according to claim 5 , wherein E is Formula (c2) claim 5 , and any one of q and s is 1 or more claim 5 ,a salt of the compound, or a solvate of the compound or the salt.7. The compound according to any one of to claim 5 , wherein s is 1 claim 5 , a salt of the compound claim 5 , or a solvate of the compound or the salt.10. The compound according to claim 9 , wherein Ea is Formula (c1) claim 9 , and any one of q and s is 1 or more claim 9 ,a salt of the compound, or a solvate of the compound or the salt.11. A pharmaceutical composition characterized by comprising claim 9 , as an active ingredient claim 9 , at least one of the compound as claimed in any one of to claim 9 , a pharmaceutically acceptable salt of the compound claim 9 , and a pharmaceutically acceptable solvate of the compound or the salt.12. A prophylactic agent and/or a therapeutic agent against a GPR40-involving disease characterized by comprising claim 9 , as an active ingredient claim 9 , at least one of the compound as claimed in any one of to claim 9 , a pharmaceutically acceptable salt of the compound claim 9 , and a pharmaceutically acceptable solvate of the compound or the salt.13. An insulin secretagogues characterized by comprising claim 9 , as an active ingredient claim 9 , at least one of the compound as claimed in any one of to claim 9 , a pharmaceutically acceptable salt of the compound claim 9 , and a pharmaceutically acceptable solvate of the compound or the salt.14. A GPR40 activating agent comprising at least one of the compound as claimed in any one of to claim 9 , a pharmaceutically acceptable salt of the compound claim 9 , and a pharmaceutically acceptable solvate of the compound or the salt.15. A pharmaceutical composition characterized by comprising:{' ...

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Номер записи: 16
29-08-2013 дата публикации

PLANT GROWTH REGULATION

Номер: US20130225410A1
Автор: Haas Ulrich Johannes, Harp Tyler L.
Принадлежит: SYNGENTA LIMITED

The present invention relates to a method for improving the plant growth regulation of and/or enhancing crop plants, by applying to the plants a mixture of a plant growth regulator, and acibenzolar-S-methyl, and to a composition comprising the same. 1. A method for regulating the growth of and/or enhancing crop plants , comprising applying to the plants a plant growth regulator and acibenzolar-S-methyl.2. A method according to claim 1 , wherein the plant growth regulator and acibenzolar-S_methyl are applied in a synergistically effective amount.3. A method according to claim 1 , wherein the plant growth regulator is selected from the group consisting of trinexapac-ethyl claim 1 , prohexadione-calcium claim 1 , paclobutrazol claim 1 , uniconazole claim 1 , flurprimidol claim 1 , mefluidide claim 1 , mepiquat-chloride claim 1 , chlormequat-chloride claim 1 , and a mixture thereof.4. A method according to claim 3 , wherein the plant growth regulator is trinexapac-ethyl.5. A method according to claim 3 , wherein the plant growth regulator is paclobutrazol.6. A method according to claim 1 , wherein the crop plants are monocotyledonous plants.7. A method according to claim 6 , wherein the crop plants are selected from the group consisting of cereals claim 6 , rice claim 6 , maize and sugar cane.8. A method according to claim 1 , wherein the plant growth regulator and acibenzolar-S-methyl are applied to the plant in a weight ratio from about 5:1 to about 1:1.9. A method according to claim 1 , wherein the plant growth regulator is applied at a rate from about 50 to about 100 g ai/ha.10. A method according to claim 1 , wherein the acibenzolar-S-methyl is applied at a rate from about 5 to about 25 g ai/ha.11. A method according to claim 1 , wherein the enhancement is improved plant yield.12. A method according to claim 1 , wherein the enhancement is improved plant vigour and/or plant quality claim 1 , and/or plant tolerance to stress factors.13. A method according to claim 12 ...

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Номер записи: 17
29-08-2013 дата публикации

COMPOUND FOR INCREASING KINASE ACTIVE AND APPLICATION THEREOF

Номер: US20130225587A1
Автор: Hu Yunyan, Kang Xinshan, Long Wei, Ma Cunbo, Shen Xiaoyan, Tan Fenlai, Wang Yanping, Wang Yinxiang
Принадлежит:

The compound of Formula (I), pharmaceutically acceptable salts thereof, solvates thereof, chelates thereof, non-covalent complexes thereof or produgs of compounds mentioned above or the mixture of any form above mentioned are provided. The use of the compounds in manufacturing a medicament for the treatment and/or prevention of diabetes, obesity and related disorders. 2. The compound of claim 1 , wherein W is C.34-. (canceled)5. The compound of claim 2 , wherein Y is C claim 2 , X is O claim 2 , and wherein Z is C.6. The compound of claim 2 , wherein Y is N.7. The compound of claim 6 , wherein X is O.8. The compound of claim 7 , wherein Z is C.911-. (canceled)12. The compound of claim 1 , wherein W is N claim 1 , Y is C claim 1 , wherein X is O claim 1 , and wherein Z is C.1319-. (canceled)20. The compound of claim 1 , wherein Ris selected from the group consisting of —H claim 1 , lower alkanyl claim 1 , substituted lower alkanyl claim 1 , lower alkenyl claim 1 , substituted lower alkenyl claim 1 , lower alkynyl claim 1 , substituted lower alkynyl claim 1 , Calkoxy and substituted Calkoxy.21. The compound of claim 20 , wherein Ris —H; Ris selected from the group consisting of cycloalkyl claim 20 , substituted cycloalkyl claim 20 , heterocycloalkyl and substituted heterocycloalkyl; and wherein Ris 5 or 6 membered heteroaryl.2324-. (canceled)25. The compound of claim 1 , wherein Ris selected from the group consisting of C(═O)R claim 1 , SR claim 1 , SORand haloalkyl; and wherein Ris selected the group consisting of Calkanyl claim 1 , substituted Calkanyl claim 1 , NRR claim 1 , Calkoxy claim 1 , and substituted Calkoxy.26. The compound of claim 25 , wherein Ris —H; wherein Ris selected from the group consisting of cycloalkanyl claim 25 , substituted cycloalkanyl claim 25 , heterocycloalkyl and substituted heterocycloalkyl; and wherein Ris substituted 5- or 6-membered heteroaryl.28. The compound of claim 27 , wherein Ris C(═O)R; Ris NRR.29. The compound of claim 27 , ...

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Номер записи: 18
29-08-2013 дата публикации

SALTS OF POTASSIUM ATP CHANNEL OPENERS AND USES THEREOF

Номер: US20130225806A1
Автор: Cowen Neil M., Yamout Khaled A.
Принадлежит: Essentialis, Inc.

Provided are immediate or prolonged administration of certain salts of Kchannel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving Kchannels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals. 2. The method of wherein said cation source is an alkali metal hydroxide.3. The method of wherein said cation source is sodium hydroxide or potassium hydroxide.4. The method of wherein said solvent is selected from the group consisting of acetonitrile claim 3 , low molecular weight ketones claim 3 , and tetrahydrofuran.5. The method of wherein said cation source is an organic cation source comprising an ammonium or at least one tertiary amine group.6. The method of wherein said cation source is choline hydroxide or hexamethyl hexamethylene diammonium dihydroxide.7. The method of wherein said solvent is selected from the group consisting of acetonitrile claim 6 , low molecular weight ketones claim 6 , tetrahydrofuran claim 6 , and 2-methyl tetrahydrofuran.8. The method of wherein said cation source is choline hydroxide claim 6 , and said solvent is selected from the group consisting of acetonitrile claim 6 , low molecular weight ketones claim 6 , tetrahydrofuran claim 6 , and 2-methyl tetrahydrofuran.9. The method of wherein said compound of Formulae I-IV is dissolved in a solvent at a ratio of about 1 g compound of Formulae I-IV to about 1 to 5 mL solvent.10. The method of further comprising adding a co-solvent prior to the step of removing the solvent.11. The method of wherein said co-solvent is selected from the group consisting of methyl tert-butyl ether (MTBE) claim ...

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Номер записи: 19
05-09-2013 дата публикации

METHODS OF CONTROLLING NEONICOTINOID RESISTANT APHIDS

Номер: US20130231334A1
Автор: HOEGGER Patrik, Maienfisch Peter, Rindlisbacher Alfred, Slater Russell
Принадлежит: SYNGENTA CROP PROTECTION LLC

The invention relates to a method of controlling aphids that are resistant to neonicotinoid insecticides, using a trifluoromethylpyri(mi)dine derivative in free form or in agrochemically acceptable salt form as well as the use of compositions comprising said compound to control neonicontinoid resistant insects. In particular the methods relate to controlling neonicotinoid resistant insects in the Aphididae family, that are resistant to one or more neonicotinoid insecticides. Methods of the invention find particular use in controlling neonicotinoid resistant insects in crops of useful plants. Furthermore, the invention extends to methods of controlling plant viruses spread by neonicotinoid resistant insects. 1. A method of controlling insects from the Aphididae family , which insects are resistant to a neonicotinoid insecticide , which method comprises applying a trifluoromethlypyri(mi)dine derivative in free form , or in agrochemically acceptable salt form , to said neonicotinoid resistant insects.3. A method of protecting a crop of useful plants susceptible to and/or under attack by insects from the Aphididae family claim 1 , which insects are resistant to a neonicotinoid insecticide claim 1 , which method comprises applying to said crop claim 1 , treating a plant propagation material of said crop with claim 1 , and/or applying to said neonicotinoid resistant insects claim 1 , a compound claim 1 , as defined in claim 1 , in free form or in agrochemically acceptable salt form.4. A method of controlling resistance to one or more neonicotinoid insecticides in insects from the Aphididae family claim 1 , which comprises (I) alternately applying a compound claim 1 , as defined in claim 1 , and a neonicotinoid insecticide to said insects or to a crop of useful plants susceptible to and/or under attack from said insects; and/or (II) applying a mixture of a compound of formula I or formula II claim 1 , as defined in claim 1 , and a neonicotinoid insecticide to said insects ...

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Номер записи: 20
12-09-2013 дата публикации

COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR

Номер: US20130237531A1
Автор: Ibrahim Prabha N., Shi Songyuan, Spevak Wayne, Tsai James, Wu Guoxian, Zhang Chao, Zhang Jiazhong
Принадлежит:

Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. 2. The compound of claim 1 , wherein Ris hydrogen.3. The compound of claim 2 , wherein Ris halogen.4. The compound of claim 2 , wherein Ris optionally substituted phenyl.5. The compound of claim 2 , wherein Ris phenyl optionally substituted with one or more halogen substituents.6. The compound of claim 1 , wherein Ris phenyl optionally substituted with one or more fluoro substituents.7. The compound of claim 6 , wherein Ris phenyl substituted with two fluoro substituents.8. The compound of claim 1 , wherein each Ris independently optionally substituted lower alkyl or optionally substituted heteroaryl.9. The compound of claim 8 , wherein one Ris lower alkyl and the other Ris heteroaryl substituted with one or more NHgroups.10. The compound of claim 8 , wherein one Ris lower alkyl and the other Ris pyrimidinyl substituted with one or more NHgroups.11. The compound of claim 10 , wherein one Ris t-butyl and the other Ris pyrimidinyl substituted with NH.13. The compound of claim 12 , wherein Ar is thiazolyl.14. The compound of claim 12 , wherein Ar is 4-thiazolyl.16. A pharmaceutical composition comprising: a compound of and a pharmaceutically acceptable carrier or excipient.17. A pharmaceutical composition comprising: a compound of and a pharmaceutically acceptable carrier or excipient.18. A pharmaceutical composition comprising a compound of and another therapeutic agent.19. A method for treating a subject suffering from melanoma claim 15 , thyroid cancer or colorectal cancer claim 15 , said method comprising: administering to the subject an effective amount of a compound of .20. The method of claim 19 , wherein the melanoma is melanoma having a mutation encoding a V600E amino acid substitution. This application is a continuation application of U.S. application Ser. No. 12/669,450, filed Jan ...

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Номер записи: 21
12-09-2013 дата публикации

PROCESS FOR THE PREPARATION OF TAUROLIDINE AND ITS INTERMEDIATES THEREOF

Номер: US20130237700A1
Автор: Dokula Neelam Naidu, Pullagurla Manik Reddy, Rangisetty Jagadeesh Babu
Принадлежит: Biophore India Pharmaceuticals PVT. Ltd.

The present invention relates to a process for the preparation of substantially pure Taurolidine. 1. Process for the preparation of Cbz-taurine sodium salt (II) which comprises:a. Reaction of Taurine and Cbz-cl in the presence of aqueous sodium hydroxide and toluene as solventb. Separation of aqueous and organic layerc. Addition of sodium hydroxide to make the aqueous layer highly basic (pH12-14)d. Separation of Cbz-taurine sodium salt2. Process for the preparation of Taurolidine which comprises:a. Reaction of Taurine and Cbz-cl in the presence of aqueous sodium hydroxide and toluene as solventb. Separation of Cbz-taurine sodium salt precipitated out{'sub': '5', 'c. Conversion of Cbz-taurine sodium to Cbz-Taurinamide in the presence of PClfollowed by treatment with ammonia'}d. Conversion of Cbz-Taurinamide to taurinamide in presence of Pd/C followed by in situ generation of Taurinamide Succinate by reaction of Taurinamide and succinic acide. Treatment of Taurinamide succinate with formaldehyde under basic conditions to generate Taurolidine3. Process for the purification of Taurolidine which involvesa. dissolving Taurolidine in non-aqueous aprotic solvents to obtain clear solutionb. isolation of the pure compound which precipitates from the clear solution4. Process of claim 3 , wherein the non-aqueous aprotic solvents are DMSO claim 3 , DMAc claim 3 , DMF claim 3 , Acetonitrile5. Process of wherein the purification stage has an additional step of adding antisolvent6. Process of claim 5 , wherein the anti solvents are toluene claim 5 , ethyl acetate claim 5 , diethyl ether and dichloromethane. Taurolidine is an antibacterial drug and also has antiendotoxic substance, which is used as an antiseptic solution in surgery for washing out the abdominal cavity and it also prevents septic shock. It is commercially sold as Taurolidine (Formula I). The present invention relates to a process for the preparation of Taurolidine which provides significant advantages over the ...

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Номер записи: 22
19-09-2013 дата публикации

PLANT IRRIGATION METHODS

Номер: US20130247250A1
Автор: Bassi Albert, Haas Ulrich Johannes, Perkins Daniel, Weider Christophe, Zeun Ronald
Принадлежит: SYNGENTA CROP PROTECTION LLC

The present invention is directed to methods of increasing the environmental stress tolerance of a plant, to methods of improving the quality and/or yield of a plant crop, to methods of application of agrochemicals having a physiological effect on a plant in the plant irrigation water, and to crops produced using said methods. 1. A method of increasing the abiotic environmental stress tolerance of a plant comprising the application of one or more agrochemicals independently selected from the group consisting of acibenzolar , acibenzolar-S-methyl (ASM) , trinexapac-ethyl (TXP) , azoxystrobin , propiconazole , thiamethoxam and paclobutrazol (PBZ) in the plant irrigation water wherein said agrochemical has a physiological effect on the plant.2. A method of improving the quality and/or yield and or vigour of a plant crop comprising the application of one or more agrochemicals independently selected from the group consisting of acibenzolar , acibenzolar-S-methyl (ASM) , trinexapac-ethyl (TXP) , azoxystrobin , propiconazole , thiamethoxam and paclobutrazol (PBZ) in the plant irrigation water wherein said agrochemical has a physiological effect on the plant.3. A method of reducing damage to a plant caused by one or more abiotic environmental stress factors , comprising the application of one or more agrochemicals independently selected from the group consisting of acibenzolar , acibenzolar-S-methyl (ASM) , trinexapac-ethyl (TXP) , azoxystrobin , propiconazole , thiamethoxam and paclobutrazol (PBZ) in the plant irrigation water wherein said agrochemical has a physiological effect on the plant.4. A method according to wherein the one or more agrochemicals are each independently selected from azoxystrobin claim 1 , paclobutrazol claim 1 , trinexapac-ethyl claim 1 , propiconazole and acibenzolar-S-methyl.5. A method according to wherein the one or more agrochemicals are each independently selected from the group consisting of azoxystrobin claim 4 , paclobutrazol claim 4 , and ...

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Номер записи: 23
10-10-2013 дата публикации

HETEROCYCLIC SULFONAMIDES

Номер: US20130267537A1
Автор: JR. David J., KRAYNACK Erica Anne, Malik Fady, MORGAN Bradley Paul, Morgans, Muci Alexander Ramon, Qian Xiangping
Принадлежит: CYTOKINETICS, INC.

Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure. 114-. (canceled)16. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ris a phenyl claim 15 , isoxazolyl claim 15 , oxazolyl claim 15 , pyridinyl claim 15 , pyrazinyl claim 15 , pyrimidinyl claim 15 , tetrazol-5-yl claim 15 , thiazolyl claim 15 , thiadiazolyl or imidazolyl group claim 15 , which is optionally substituted with a halogen claim 15 , lower alkoxy claim 15 , aryl or heteroaryl group.17. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ris a [1 claim 15 ,3 claim 15 ,4]thiadiazol-2-yl group which is optionally substituted with a phenyl group.18. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ris 5-phenyl-[1 claim 15 ,3 claim 15 ,4]thiadiazol-2-yl.19. The compound of claim 18 , or a pharmaceutically acceptable salt thereof claim 18 , wherein{'sup': '4', 'Rchloro; and'}{'sup': 5', '6', '7, 'R, Rand Rare hydrogen.'}20. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ris a 1H-imidazol-2-yl group.21. The compound of claim 20 , or a pharmaceutically acceptable salt thereof claim 20 , wherein{'sup': '4', 'Ris chloro; and'}{'sup': 5', '6', '7, 'R, Rand Rare hydrogen.'}22. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ris thiazol-2-yl.23. The compound of claim 22 , or a pharmaceutically acceptable salt thereof claim 22 , wherein{'sup': '4', 'Ris chloro; and'}{'sup': 5', '6', '7, 'R, Rand Rare hydrogen.'}24. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein{'sup': '4', 'Ris chloro; and'}{'sup': 5', '6', '7, 'R, Rand Rare hydrogen.'}25. The compound of claim 15 , or a pharmaceutically ...

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Номер записи: 24
31-10-2013 дата публикации

HETEROCYCLIC FUSED ANTHRAQUINONE DERIVATIVES, MANUFACTURING METHOD AND PHARMACEUTICAL COMPOSITION USING THEREOF

Номер: US20130289028A1
Автор: CHEN Tsung-Chih, HUANG Hsu-Shan, LEE Yu-Ru
Принадлежит: NATIONAL DEFENSE MEDICAL CENTER

A heterocyclic fused anthraquinone derivatives, which is represented by a formula (I): 2. The heterocyclic fused anthraquinone derivatives of claim 1 , wherein Ris aminoalkyl group claim 1 , sulfoalkyl group or haloalkyl group claim 1 , the alkyl group can be selected from the group consisting of Cstraight-chain alkyl group claim 1 , Cbranched alkyl group and Ccyclic alkyl group claim 1 , and the halogens can be selected from the group consisting of F claim 1 , Cl claim 1 , Br and I.3. The heterocyclic fused anthraquinone derivatives of claim 2 , wherein Ris Cl claim 2 , sulfonic acid sodium claim 2 , oxide potassium claim 2 , diethylamino group claim 2 , amino-propyl group claim 2 , amino-cyclobutyl group claim 2 , amino-dimethyl group claim 2 , amino-ethyl group claim 2 , ethyl piperazino group claim 2 , amimo-cyclopentylamino group claim 2 , amino-butylamino group claim 2 , amino-ethylamino claim 2 , amino-2-methylpropylamino group claim 2 , thio-morpholino group claim 2 , thio-ethyl group claim 2 , thio-n-propyl group or thio-isopropyl group.4. The heterocyclic fused anthraquinone derivatives of claim 1 , wherein the Ris amino group and the Ris 3-chlorophenylamino group claim 1 , 2-methylphenylamino group claim 1 , 3-methylphenylamono group claim 1 , 4-methylphenylamino group claim 1 , 4-chlorophenylamino group or 4-chloro-2-fluorophenylamino group.5. The heterocyclic fused anthraquinone derivatives of claim 1 , wherein the Ris oxygen and Ris para-methylphenyl-oxy group.6. The heterocyclic fused anthraquinone derivatives of claim 1 , wherein the Ris sulfur group and Ris phenylthio claim 1 , 2 claim 1 ,5-dimethylphenylthio group claim 1 , benzylthio group claim 1 , 4-chlorophenylthio group claim 1 , 2-methylphenylthio group claim 1 , 4-bromophenylthio group claim 1 , 2 claim 1 ,4-dimethylphenylthio group claim 1 , 4-isopropylphenylthio group claim 1 , 2-bromophenylthio group claim 1 , 4-fluorophenylthio group claim 1 , phenylthioethyl group claim 1 , 2 claim 1 ,3 ...

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Номер записи: 25
07-11-2013 дата публикации

PLANT DISEASE CONTROL AGENT

Номер: US20130296313A1
Автор: HOSOKAWA Hiroyasu, Isshiki Atsunori, SAIGA Tomoyuki, Urihara Ichirou
Принадлежит:

The present invention provides a plant disease control agent containing at least one of tetrazoyloxime dirvatives and salts thereof, and at least one selected from the group consisting of fosetyl, propamocarb, basic copper chloride, chlorothalonil, manzeb, cymoxanil, folpet, iminoctadine, cyazofamid, metalaxyl, fludioxonil, tebuconazole, prothioconazole, thiamethoxam, azoxystrobin and salts thereof. 1. (canceled) The present invention relates to a plant disease control agent containing tetrazoyloxime derivative or the like and an active ingredient for agricultural and horticultural use.Priority is claimed on Japanese Patent Application No. 2008-075748, filed Mar. 24, 2008, the content of which is incorporated herein by reference.Until now, in the cultivation of agricultural and horticultural crops, although a large number of disease control agents are used against crop disease, since the control effects thereof may be inadequate, the use thereof may be restricted due to the appearance of agrichemical-resistance pathogenic organisms, the plants may be damaged or contaminated by the agrichemical or the agrichemical may demonstrate toxicity to humans, livestock or marine life, a considerable number of these disease control agents are not necessarily considered to be satisfactory. Thus, there is a need to develop a plant disease control agent that can be used safely and has few of these shortcomings.The present inventors carried out exhaustive research in view of the above-described circumstances, and discovered that tetrazoyloxime derivative and/or the salt thereof are useful as an active ingredient of plant disease control agent, and previously filed a patent application (Patent Document 1).The present invention was carried out as a part of research on a plant disease control agent containing tetrazoyloxime derivative and/or the salt thereof described in Patent Document 1 as an active ingredient and an objective of present invention is to provide a plant disease ...

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Номер записи: 26
28-11-2013 дата публикации

THIAZOLE AND THIADIAZOLE COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES

Номер: US20130317032A1
Автор: Che Qinglin, Chen Shoujun, Vo Nha Huu, Xie Yu
Принадлежит: Synta Pharmaceuticals Corp.

The invention relates to compounds of structural formula (I): 1137-. (canceled)141. The compound of claim 140 , wherein Y′ is an optionally substituted phenyl or an optionally substituted pyridinyl.142. The compound of claim 141 , wherein Y′ is substituted with one to two substituents.143. The compound of claim 142 , wherein the one to two substituents are each independently a lower alkyl or a halo.144. The compound of claim 143 , wherein Y′ is 2 claim 143 ,6-difluorophenyl.145. The compound of claim 140 , wherein L′ is —NRCH— claim 140 , —CHNR— claim 140 , —C(O)— claim 140 , —NR—C(O)— claim 140 , —C(O)—NR— claim 140 , —OC(O)— claim 140 , —C(O)O— claim 140 , —C(S)— claim 140 , —NR—C(S)— claim 140 , or —C(S)—NR—.146. The compound of claim 145 , wherein L′ is —NH—C(O)—.147. The compound of claim 140 , wherein L′ is —NRS(O)— claim 140 , —S(O)NR— claim 140 , —NRS(O)NR— claim 140 , —NRC(O)CH— claim 140 , —NRC(O)CH═CH— claim 140 , —NRC(O)NR— claim 140 , —NRC(NR)NR— claim 140 , —NRC(S)NR— claim 140 , —NRCHNR— claim 140 , —NRN═CR— claim 140 , —C(NR)— claim 140 , —CR═NNR—; —CH═CH— or148. The compound of claim 140 , wherein Zis lower alkyl.149. The compound of claim 140 , wherein Zis —H.150. The compound of claim 140 , whereinY′ is a phenyl substituted with one to two substituents or a pyridinyl substituted with one to two substituents, wherein the one to two substituents are each independently a lower alkyl or a halo;L′ is —NR—C(O)—;{'sub': '1', 'Zis lower alkyl or —H; and'}{'sub': 5', '6', '3, 'Zand Zare each independently chloro, bromo, fluoro, cyano, trifluoromethyl, —C(O)CH, 2-methyl-2H-tetrazolyl, methoxy, nitro, dimethylamino, thiazol-2-yl, oxazol-2-yl, or methyl.'}153. The compound of claim 138 , wherein the compound is selected from the group consisting of:N-[4-(2,4-Dichloro-phenyl)-thiazol-2-yl]-2,6-difluoro-benzamide;N-[4-(2,5-Dimethoxy-phenyl)-thiazol-2-yl]-2,6-difluoro-benzamide;N-[5-(2,5-Dimethoxy-phenyl)-thiazol-2-yl]-2,6-difluoro-benzamide;N-[5-(2-Chloro-5- ...

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Номер записи: 27
19-12-2013 дата публикации

Chemosensory Receptor Ligand-Based Therapies

Номер: US20130338095A1
Автор: Baron Alain D., Beeley Nigel R.A., Brown Martin R., Jones Christopher R.G.
Принадлежит: Elcelyx Therapeutics, Inc.

Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention. 193-. (canceled)120. A composition according to claim 94 , wherein the composition further releases at least some of the chemosensory receptor ligand in the stomach.121. A composition according to claim 94 , wherein one or more regions of the intestine are the duodenum claim 94 , jejunum claim 94 , ileum claim 94 , caecum claim 94 , colon and/or rectum.122. A composition according to claim 94 , wherein the composition releases at an onset of about 5 to about 45 minutes claim 94 , about 105 to about 135 minutes claim 94 , about 165 to about 195 minutes claim 94 , about 225 to about 255 minutes or a combination of times thereof following administration to a subject.123. A composition according to claim 94 , wherein the composition releases at an onset of about pH 5.0 claim 94 , about pH 5.5 claim 94 , about pH 6.0 claim 94 , about pH 6.5 claim 94 , about pH 7.0 claim 94 , or combination thereof following administration to a subject.124. A composition according to claim 94 , the composition further comprising a second chemosensory receptor ligand selected from the group consisting of a sweet receptor ligand claim 94 , a bitter receptor ligand claim 94 , an umami receptor ligand claim 94 , a fat receptor ligand claim 94 , a sour receptor ligand and a bile acid receptor ligand.125. A composition according to claim 124 , wherein the sweet receptor ligand is selected from the group consisting of sucralose claim 124 , aspartame claim 124 , Stevioside claim 124 , Rebaudioside A claim 124 , Rebaudioside B claim 124 , Rebaudioside C claim 124 , Rebaudioside D claim 124 , ...

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Номер записи: 28
26-12-2013 дата публикации

LOCAL TOPICAL ADMINISTRATION FORMULATIONS CONTAINING INDOXACARB

Номер: US20130345210A1
Автор: "ONeil Peter Andrew", Freehauf Keith Alan, Guerino Frank, Sargent Roger Mervyn, Simmons Robert D., Wang Chen-Chao
Принадлежит:

The present invention provides formulations and methods useful in the control of ectoparasites on a domestic animal, using a formulation comprising Indoxacarb and a veterinarily acceptable carrier that is applied topically to 10% or less of the total surface area of a domestic animal. Other embodiments include these formulations also including one or more additional pesticides such as fipronil. 1. A local , topical , spot-on formulation for control of ectoparasites on a domestic animal comprising an ectoparasitically effective amount of Indoxacarb , a veterinarily acceptable carrier , and a pyrethroid pesticide.2. The formulation of claim 1 , wherein said ectoparasite is an Arthropod.3. The formulation of claim 2 , wherein said Arthropod is an Insecta.4. The formulation of claim 3 , wherein said Insecta is a flea claim 3 , fly claim 3 , or louse.5. The formulation of claim 2 , wherein said Arthropod is an Arachnida.6. The formulation of claim 1 , wherein the concentration of Indoxacarb in said formulation is at least 200 g/L.7. The formulation of claim 1 , wherein the concentration of Indoxacarb in said formulation is at least 150 g/L.8. The formulation of claim 1 , wherein the concentration of Indoxacarb is at least 100 g/L.9. The formulation of claim 1 , wherein said veterinarily acceptable carrier comprises one or more of a solvent claim 1 , crystallization inhibitor claim 1 , adjuvant claim 1 , co-solvent claim 1 , colorant claim 1 , surfactant claim 1 , spreading oil claim 1 , antioxidant claim 1 , light stabilizer or tackifier.10. The formulation of claim 9 , wherein said solvent comprises a glycol ether.11. The formulation of claim 10 , wherein said glycol ether comprises dipropylene glycol monomethyl ether.12. The formulation of claim 9 , wherein said solvent comprises an alkyl acetate.13. The formulation of claim 12 , wherein said alkyl acetate is ethyl acetoacetate.14. The formulation of claim 9 , wherein said crystallization inhibitor is triacetin.15. The ...

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Номер записи: 29
02-01-2014 дата публикации

ACTIVE COMPOUND COMBINATIONS

Номер: US20140005049A1
Автор: Dahmen Peter, HEINEMANN Ulrich, ILG Kerstin, Wachendorff-Neumann Ulrike
Принадлежит:

The invention relates to active compound combinations, in particular within a composition, which comprises (A) an amidine compound of formula (I) and a further fungicidally (B-1), insecticidally (B-2) active or plant growth regulating compound (B-3). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or reducing the mycotoxin contamination of plant or plant parts, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed. 3. The composition according to wherein the at least one further active compound (B-I) is selected from the group consisting of Cyproconazole claim 1 , Epoxiconazole claim 1 , Flusilazole claim 1 , Fluquinconazole Ipconazole claim 1 , Propiconazole claim 1 , Metconazole claim 1 , Tebuconazole claim 1 , Triadimenol claim 1 , Azoxystrobin claim 1 , Fluoxastrobin claim 1 , Kresoxim-methyl claim 1 , Picoxystrobin claim 1 , Pyraclostrobin claim 1 , Boscalid claim 1 , Chlorothalonil claim 1 , Cyprodinil claim 1 , Fludioxonil claim 1 , Fluopyram claim 1 , Thiophanat-methyl claim 1 , Penflufen claim 1 , Isopyrazam claim 1 , Sedaxane claim 1 , Myclobutonil claim 1 , Prochloraz claim 1 , Spiroxamine claim 1 , N-(3′ claim 1 ,4′-dichloro-5-fluoro[1 claim 1 ,1′-biphenyl]-2-yl)-3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxamide claim 1 , Ametoctradin claim 1 , 5-Chlor-6-(2 claim 1 ,4 claim 1 ,6-trifluorphenyl)-7-(4-methylpiperidin-1-yl)[1 claim 1 ,2 claim 1 ,4]triazolo[1 claim 1 ,5-a]pyrimidin claim 1 , 1-methyl-N-{2-[1′-methyl-1 claim 1 ,1′-bi(cyclopropyl)-2-yl]phenyl}-3-(trifluoromethyl)-1H-pyrazole-4-carboxamide claim 1 , N-{2-[1 claim 1 ,1′-bi(cyclopropyl)-2-yl]phenyl}-1-methyl-3-(trifluoromethyl)-1H-pyrazole-4-carboxamide claim 1 , 1-methyl-N-{2-[1′-methyl-1 claim 1 ,1′-bi(cyclopropyl)-2-yl]phenyl}-3-(difluoromethyl)-1H-pyrazole-4-carboxamide claim 1 , and N-{2-[1 claim 1 ,1′-bi(cyclopropyl ...

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Номер записи: 30
09-01-2014 дата публикации

Compounds that Modulate EGFR Activity and Methods for Treating or Preventing Conditions Therewith

Номер: US20140011810A1
Автор: Gray Nathanael S., Zhou Wenjun
Принадлежит: Gatekeeper Pharmaceuticals, Inc.

Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith. 4. The compound of claim 1 , wherein Z is —(CH)NRC(O)R; Ris hydrogen; and Ris C-Calkenyl.6. The compound of claim 1 , wherein:X is oxygen;{'sup': '1', 'sub': 1', '6, 'Ris C-Calkoxy;'}{'sup': '2', 'sub': 1', '6, 'Ris piperazine that is substituted at the N position with C-Calkyl;'}{'sup': 2a', '2b, 'Rand Rare hydrogen;'}{'sup': 3', '4', '5', '3', '4', '5, 'one of R, R, and Ris Z, and the other two of R, R, and Rare hydrogen;'}{'sup': '7', 'sub': 1', '6, 'Ris hydrogen or C-Calkyl;'}{'sup': '8', 'sub': 2', '6, 'Ris C-Calkenyl; and'}{'sub': 2', 'n, 'sup': 7', '8, 'Z is —(CH)NRC(O)R.'}11. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable excipient.12. A kit comprising the compound of and instructions for use of the compound in treating a disease or disorder in a subject in need thereof.13. The kit of claim 12 , wherein the disease or disorder comprises a cancer or a proliferative disorder.14. A method for inhibiting a kinase claim 1 , comprising contacting the kinase with an effective amount of the compound of .15. The method of claim 14 , wherein the kinase comprises EGFR claim 14 , Jak3 claim 14 , Blk claim 14 , Bmx claim 14 , Btk claim 14 , HER2 (ErbB2) claim 14 , HER4 (ErbB4) claim 14 , Itk claim 14 , Tec claim 14 , or Txk.16. The method of claim 15 , wherein the EGFR is a mutant EGFR.17. The method of claim 16 , wherein the EGFR mutation comprises G719S claim 16 , G719C claim 16 , G719A claim 16 , L858R claim 16 , L861Q claim 16 , an exon 19 deletion mutation or an exon 20 insertion mutation.18. The method of claim 17 , wherein the EGFR mutation further comprises an EGFR T790M claim 17 , T854A or D761Y resistance mutation.19. A method for treating or preventing a disease that is mediated by a kinase comprising administering an effective amount of the compound of to a subject in need thereof.20. The method of claim 19 , wherein ...

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Номер записи: 31
16-01-2014 дата публикации

MITOTIC KINESIN INHIBTORS AND METHODS OF USE THEREOF

Номер: US20140018399A1
Автор: Allen Shelley, Corrette Christopher P., DeLisle Robert Kirk, Hans Jeremy, Laird Ellen, Lyssikatos Joseph P., Robinson John E., Voegtli Walter C., Wallace Eli M., Zhao Qian
Принадлежит: ARRAY BIOPHARMA INC.

This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders. 2. The compound of claim 1 , wherein Aris phenyl optionally substituted with one or more groups independently selected from halogen claim 1 , alkyl claim 1 , —ORor —NRR; or Aris a heteroaryl selected from thiophenyl or pyridyl claim 1 , wherein said pyridyl is optionally substituted independently with one or more halogen.3. The compound of claim 1 , wherein Aris phenyl claim 1 , 2 claim 1 ,4-difluorophenyl claim 1 , 2-fluorophenyl claim 1 , 3-fluorophenyl claim 1 , 2-chlorophenyl claim 1 , 3-chlorophenyl claim 1 , 2 claim 1 ,5-dichlorophenyl claim 1 , 2 claim 1 ,3-dichlorophenyl claim 1 , 3 claim 1 ,4-dichlorophenyl claim 1 , 3 claim 1 ,5-dichlorophenyl claim 1 , 2-chloro-5-fluorophenyl claim 1 , 2-fluoro-5-chlorophenyl claim 1 , 2-chloro-5-methylphenyl claim 1 , 2-trifluoromethyl-5-fluorophenyl claim 1 , 2-fluoro-5-methoxyphenyl claim 1 , thiophen-2-yl claim 1 , thiophen-3-yl claim 1 , 5-chlorothiophen-2-yl claim 1 , 2-pyridyl claim 1 , 3-pyridyl claim 1 , 4-chloropyridin-3-yl claim 1 , 3-chloropyridin-2-yl claim 1 , 4-fluoropyridin-3-yl claim 1 , or 3 claim 1 ,6-difluoropyridin-2-yl.4. The compound of claim 1 , wherein Aris phenyl.5. The compound of claim 1 , wherein Aris phenyl optionally substituted with one or more groups independently selected from halogen claim 1 , OR claim 1 , NRR claim 1 , CN claim 1 , NO claim 1 , —OP(═O)(OR) claim 1 , C(═O)OR claim 1 , or Aris a heteroaryl selected from pyridyl claim 1 , thiophenyl optionally substituted with alkyl claim 1 , imidazolyl claim 1 , and pyrazolyl optionally substituted with NRR.6. The compound of claim 1 , wherein Aris phenyl claim 1 , 2-methylphenyl claim 1 , 3- ...

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Номер записи: 32
23-01-2014 дата публикации

SULFAMIDE DERIVATIVE HAVING AN ADAMANTYL GROUP AND ITS PHARMACEUTICALLY ACCEPTABLE SALT

Номер: US20140024636A1
Автор: Ahn Jin Hee, Ahn Sung Hoon, Bae Myung Ae, Jung Won Hoon, KANG Nam Sook, Kang Seung Kyu, Kim Hee Youn, KIM Ki Young, Rhee Sang Dal
Принадлежит: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

Provided is a sulfamide derivative having an adamantyl group represented by the following Formula 1, or a pharmaceutically acceptable salt thereof. The sulfamide derivative suppresses the activity of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), and is useful in the treatment of various diseases that are mediated by 11β-HSD1. 2. The sulfamide derivative or its pharmaceutically acceptable salt according to claim 1 , wherein Rrepresents phenyl or naphthalene group substitutued with halogen claim 1 , C-Calkyl or CF claim 1 , OCF claim 1 , cyano claim 1 , nitro claim 1 , or 5-10 membered aryl or heteroaryl; n represents an integer of 1.3. The sulfamide derivative or its pharmaceutically acceptable salt according to claim 1 , wherein the derivative represented by the Formula 1 is selected from the group consisting of:(1) N-(adamantan-2-yl)-2-(1,1-dioxido-6-(2-oxo-2-phenylethyl)-1,2,6-thiadiazinan-2-yl)acetamide;(2) N-(adamantan-2-yl)-2-(1,1-dioxido-6-phenyl-1,2,6-thiadiazinan-2-yl)acetamide;(3) tert-butyl 6-(2-(adamantan-2-ylamino)-2-oxoethyl)-1,2,6-thiadiazinan-2-carboxylate-1,1-dioxide;(4) N-(adamantan-2-yl)-2-(1,1-dioxido-1,2,6-thiadiazinan-2-yl)acetamide hydro chloride;(5) N-(adamantan-2-yl)-2-(6-benzyl-1,1-dioxido-1,2,6-thiadiazinan-2-yl)acetamide;(6) N-(adamantan-2-yl)-2-(6-(4-fluorobenzyl)-1,1-dioxido-1,2,6-thiadiazinan-2-yl)acetamide;(7) N-(adamantan-2-yl)-2-(1,1-dioxido-6-(4-(trifluoromethoxy)benzyl)-1,2,6-thiadiazinan-2-yl)acetamide;(8) N-(adamantan-2-yl)-2-(6-(4-chlorobenzyl)-1,1-dioxido-1,2,6-thiadiazinan-2-yl)acetamide;(9) N-(adamantan-2-yl)-2-(6-(3-methylbenzyl)-1,1-dioxido-1,2,6-thiadiazinan-2-yl)acetamide;(10) N-(adamantan-2-yl)-2-(6-(3-chlorobenzyl)-1,1-dioxido-1,2,6-thiadiazinan-2-yl)acetamide;(11) N-(adamantan-2-yl)-2-(6-(3-fluorobenzyl)-1,1-dioxido-1,2,6-thiadiazinan-2-yl)acetamide;(12) N-(adamantan-2-yl)-2-(6-(3-methoxybenzyl)-1,1-dioxido-1,2,6-thiadiazinan-2-yl)acetamide;(13) N-(adamantan-2-yl)-2-(6-(2-chlorobenzyl)-1,1-dioxido-1,2,6- ...

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Номер записи: 33
23-01-2014 дата публикации

Gamma-glutamyl transpeptidase inhibitors and methods of use

Номер: US20140024685A1
Автор: Marie H. Hanigan, Pui Kai Li
Принадлежит: Ohio State Innovation Foundation, University of Oklahoma

Compositions that are effective in inhibiting gamma-glutamyl transpeptidase are disclosed. Methods of producing and using these compositions are also disclosed.

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Номер записи: 34
06-02-2014 дата публикации

PLANT TREATMENT

Номер: US20140038950A1
Автор: HELIE NORMAN J.
Принадлежит:

An anti-fungal treatment for trees and bushes. Included are all methods of delivery of active ingredients, including foliar and trunk spraying application, granular soil surface, soil drench, soil injection, and trunk injection. The chemical combination includes a group 3 fungicide like propiconazole, that is, a systemic with curative and protective action, that works via the demethylation of C-14 during ergosterol biosynthesis. The combination also includes a group 11 fungicide like Azoxystrobin, or Fluoxastrobin for which their biochemical mode of action is inhibition of electron transport. The combined efficacy of there two classes of chemicals is reduced spreading of the fungus and increased killing of fungus. It has also been found that these chemicals used individually on trees and bushes, have unexpected benefits. 1. An anti-fungal treatment for trees and bushes , comprising the steps of: i. a group 3 fungicide, that is, a systemic with curative and protective action, and that works via the demethylation of C-14 during ergosterol biosynthesis, and', 'ii. a group 11 fungicide, for which their biochemical mode of action is inhibition of electron transport, and, 'a. forming a treatment product that includesb. applying the treatment product to a tree or bush at a dosage sufficient to reduce spreading of the fungus and increase killing of fungus.2. An anti-fungal treatment as recited in claim 1 , wherein the group 3 fungicide is Propiconazole.3. An anti-fungal treatment as recited in claim 1 , wherein the group 11 fungicide is Azoxystrobin.4. An anti-fungal treatment as recited in claim 1 , wherein the group 11 fungicide is Fluoxastrobin.5. An anti-fungal treatment as recited in claim 1 , wherein the group 11 fungicide is a combination of Azoxystrobin and Fluoxastrobin.6. An anti-fungal treatment as recited in claim 1 , wherein the group 3 fungicide is Propiconazole claim 1 , and wherein the group 11 fungicide is Azoxystrobin.7. An anti-fungal treatment as recited ...

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Номер записи: 35
13-02-2014 дата публикации

Cycloalkane Derivatives

Номер: US20140045862A1
Автор: Domon Yuki, Kimoto Hiroko, Kobayashi Hiroyuki, SHINOZUKA Tsuyoshi, Suzuki Sayaka, Tanaka Kyosuke
Принадлежит: Daiichi Sankyo Company, Limited

Disclosed herein are therapeutic agents and/or preventive agents for pain or therapeutic agents and/or preventive agents for a sodium channel associated disease. The present invention provides compounds represented by the following formula (I) or pharmacologically acceptable salts thereof: 2. The compound or a pharmacologically acceptable salt thereof according to claim 1 , wherein in formula (I) claim 1 ,{'sup': 1', '2, 'Arand Arare each independently a heteroaryl group;'}{'sup': 1', '2', '3, 'R, Rand Rare each independently a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group or a C3-C7 cycloalkyl group;'}{'sup': 4', '5, 'Rand Rare each independently a hydrogen atom, a halogen atom, a C1-C6 alkyl group or a halogenated C1-C6 alkyl group; and'}the heteroaryl group is optionally substituted with one or two groups selected from the group consisting of a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C3-C7 cycloalkyl group, an amino group, a C1-C3 alkylamino group and a di-C1-C3 alkylamino group.3. The compound or a pharmacologically acceptable salt thereof according to claim 1 , wherein the heteroaryl group is a 5- or 6-membered nitrogen-containing aromatic heterocyclic group.4. The compound or a pharmacologically acceptable salt thereof according to claim 1 , wherein Aris a pyridyl group claim 1 , a pyridazinyl group claim 1 , a pyrimidinyl group claim 1 , a pyrazolyl group or an imidazolyl group claim 1 , and wherein Aris optionally substituted.5. The compound or a pharmacologically acceptable salt thereof according to claim 4 , wherein Aris optionally substituted with one or two groups selected from the group consisting of a chlorine atom claim 4 , a fluorine atom claim 4 , a methyl group claim 4 , an ethyl group claim 4 , a trifluoromethyl group claim 4 , an amino group claim 4 , a methylamino group and a dimethylamino group.6. The compound or a ...

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Номер записи: 36
20-02-2014 дата публикации

SYNERGISTIC INSECTICIDAL COMPOSITIONS

Номер: US20140051572A1
Автор: Cometti Maria E., Grigera Maria S., Vassallo Carlos N.
Принадлежит: DOW AGROSCIENCES LLC

A synergistic pesticidal composition including a Spinosyn and thiamethoxam is used to control cutworms. A seed treatment composition including a Spinosyn and thiamethoxam is used to make coated seeds that exhibit synergy in the control of cutworms. In various aspects, the invention relates to pesticidal compositions, seed treatment compositions, methods of controlling cutworms, methods of treating seeds, and coated seeds produced thereby. 1. A method of controlling cutworms , comprising applying to a locus in need of cutworm control a composition comprising a synergistic pesticide mixture , the mixture comprising a pesticidally effective amount of (a) a Spinosyn component comprising a member selected from the group consisting of a Spinosyn and agriculturally acceptable salts thereof , and (b) a thiamethoxam component comprising a member selected from the group consisting of thiamethoxam and agriculturally acceptable salts thereof.2. A method comprising applying a synergistic composition comprising a synergistic pesticide mixture , the mixture comprising a pesticidally effective amount of (a) a Spinosyn component comprising a member selected from the group consisting of a Spinosyn and agriculturally acceptable salts thereof , and (b) a thiamethoxam component comprising a member selected from the group consisting of thiamethoxam and agriculturally acceptable salts thereof to a locus to control cutworms.3. The method in accordance with wherein the weight ratio of the Spinosyn component to the thiamethoxam component is from about 1:150 to about 75:1.4. The method in accordance with wherein the composition further comprises an agriculturally acceptable adjuvant or carrier.5. The method in accordance with wherein the composition further comprises at least one additional pesticide other than a Spinosyn or thiamethoxam.6. The method in accordance with wherein the composition further comprises at least one other compound having insecticidal claim 2 , herbicidal claim 2 , ...

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Номер записи: 37
20-02-2014 дата публикации

SEED TREATMENT METHOD AND COMPOSITION

Номер: US20140051573A1
Автор: Becco Carlos
Принадлежит: SYNGENTA PARTICIPATIONS AG

A method of treating seeds, comprising: providing a batch of seeds; adding a first mixture comprising at least one insecticide, at least one fungicide, and at least one coating agent to the seeds over a period of about 6 to 15 seconds; homogenizing the seeds for 5 to 25 seconds; adding a second mixture comprising at least one inoculant and at least one protectant to seeds over a period of about 6 to 15 seconds; and homogenizing the seeds for about 5 to 25 seconds. 1. A method of treating seeds , comprising:providing a batch of seeds;adding a first mixture comprising at least one insecticide, at least one fungicide, and at least one coating agent to the seeds over a period of about 6 to 15 seconds;homogenizing the seeds for 5 to 25 seconds;adding a second mixture comprising at least one inoculant and at least one protectant to the seeds over a period of about 6 to 15 seconds; andhomogenizing the seeds for about 5 to 25 seconds.2. A method according to claim 1 , further comprising drying the seeds after the second homogenization step.3. A method according to claim 1 , wherein the first homogenization step is 10 to 20 seconds and/or the second homogenization step is 5 to 20 seconds.4. A method according to claim 1 , wherein the insecticide is thiamethoxam.5. A method according to claim 1 , wherein the fungicide is fludioxonil claim 1 , metalaxyl-M claim 1 , or mixtures thereof.6. (canceled)7Bradyrhizobium. A method according to claim 1 , wherein the inoculant is spp.8. A method according to claim 1 , wherein the protectant comprises at least one inorganic nutrient salt and at least one polysaccharide.9Pasteuria. A method according to claim 1 , wherein the first mixture and/or the second mixture further comprises a nematicide claim 1 , preferably abamectin and/or spp.10. A method according to claim 1 , wherein the plant is a legume.11. A method according to claim 10 , wherein the legume is soybean.12. A method of increasing plant yield claim 1 , comprising treating a ...

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Номер записи: 38
27-02-2014 дата публикации

PESTICIDAL COMPOSITIONS

Номер: US20140057785A1
Автор: Adelfinskaya Yelena, Babcock Jonathan M., Buysse Ann M., Eckelbarger Joseph D., Garizi Negar, Hunter Ricky, Parker Marshall H., Samaritoni Jack G., Trullinger Tony K., Yap Maurice C.
Принадлежит: DOW AGROSCIENCES LLC

Molecules according to Formula One: 3. A process comprising applying a molecule according to to an area to control a pest in an amount sufficient to control such pest.4. A molecule that is a pesticidally acceptable acid addition salt claim 1 , a salt derivative claim 1 , a solvate claim 1 , or an ester derivative claim 1 , of a molecule according to .5. A polymorph of a molecule according to .6. A molecule according to wherein at least one H is H or at least one C is C.7. A composition comprising a molecule according to and at least one other compound selected from the Insecticide Group claim 1 , Acaricide Group claim 1 , Nematicide Group claim 1 , Fungicide Group claim 1 , Herbicide Group claim 1 , AI Group claim 1 , or Synergist Group.8. A composition comprising a molecule according to and at least one other compound selected from the Insecticide Group claim 2 , Acaricide Group claim 2 , Nematicide Group claim 2 , Fungicide Group claim 2 , Herbicide Group claim 2 , AI Group claim 2 , or Synergist Group.9. A composition comprising a molecule according to and a seed.10. A composition according to wherein said seed has been genetically modified to express one or more specialized traits.11. A process comprising applying a molecule according to to a genetically modified plant that has been genetically modified to express one or more specialized traits.12. A process comprising: orally administering; or topically applying; a molecule according to claim 1 , to a non-human animal claim 1 , to control endoparasites claim 1 , ectoparasites claim 1 , or both. This application is a continuation of U.S. non-provisional application Ser. No. 13/219,746, filed Aug. 29, 2011, now allowed, which claims the benefit of U.S. provisional application 61/378,528, filed Aug. 31, 2010. The entire contents of these prior applications is hereby incorporated by reference into this application.The invention disclosed in this document is related to the field of processes to produce molecules ...

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Номер записи: 39
27-02-2014 дата публикации

CYCLIC AMIDE DERIVATIVE

Номер: US20140057871A1
Автор: Makabe Muneyoshi, Ohkouchi Munetaka, Okano Akihiro
Принадлежит: MOCHIDA PHARMACEUTICAL CO., LTD.

[Problem] 4. The compound according to claim 3 , wherein T is —CH— or an oxygen atom claim 3 , Ea is Formula (c1) claim 3 , either of q or s is 1 or more claim 3 ,or a pharmaceutically acceptable salt of the compound, or a pharmaceutically acceptable solvate of the compound, or a pharmaceutically acceptable solvate of the salt.6. The compound according to claim 3 , whereinin Formula (III-1)-1 and Formula (III-1-A)-1,{'sup': 8', 'd', 'e1, 'sub': '1-6', 'Rs are independently a group optionally selected from Calkoxy group that is substituted with 1 to 5 substituent(s) M, a —CONRRgroup, and an aralkyloxy group,'}{'sub': 1-6', 'i', '1-6', '1-6', '2, 'sup': a', 'a', 'b1', 'c1', 'd', 'e', 'd', 'e, 'the substituents M are independently a group optionally selected from a halogen atom, —OH, a Calkoxy group, a —S(O)R(i is an integer of 0 to 2; and Ris a Calkyl group or a halogenated Calkyl group) group, a —NRRgroup, a —SONRRgroup, and a —CONRRgroup; and'}{'sup': 9', 'a', 'a', 'b1', 'c1', 'b1', 'c1', 'a', 'a', 'b1', 'c1', 'd', 'e, 'sub': 1-6', '1-6', '1-6', 'i', '1-6', '1-6', '2-6', '1-6', '1-6', '1-6', '2-7', 'i', '1-6', '1-6, 'Rs are independently a group optionally selected from a halogen atom, —OH, a cyano group, a Calkyl group (the Calkyl group is optionally substituted with 1 to 5 halogen atom(s), 1 to 5 —OH, 1 to 5 Calkoxy group(s), 1 to 5 —S(O)R(i is an integer of 0 to 2 and Ris a Calkyl group or a halogenated Calkyl group) group(s), or 1 to 5 —NRRgroup(s)), a Calkenyl group, a Calkoxy group (the Calkoxy group is optionally substituted with 1 to 5 halogen atom(s), 1 to 5 —OH, 1 to 5 Calkoxy group(s), or 1 to 5 —NRRgroup(s)), a Calkanoyl group, a —S(O)R(i is an integer of 0 to 2 and Ris a Calkyl group or a halogenated Calkyl group) group, a —NRRgroup, and a —CONRRgroup,'}or a pharmaceutically acceptable salt of the compound, or a pharmaceutically acceptable solvate of the compound, or a pharmaceutically acceptable solvate of the salt.7. The compound according to claim 6 ...

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Номер записи: 40
06-03-2014 дата публикации

N-(1,2,5-OXADIAZOL-3-YL)PYRIDINECARBOXAMIDES AND USE THEREOF AS HERBICIDES

Номер: US20140066301A1
Автор: Braun Ralf, GATZWEILER ELMAR, Häuser-Hahn Isolde, Heinemann Ines, Köhn Arnim, ROSINGER CHRISTOPHER HUGH, SCHMITT Monika H., Tiebes Joerg, Van Almsick Andreas
Принадлежит: Bayer Intellectual Property GmbH

A description is given of N-(1,2,5-oxadiazol-3-yl)pyridinecarboxamides of the general formula (I) as herbicides. R in this formula (I) stands for radicals such as hydrogen, organic radicals, and other radicals such as halogen. W stands for a substituted pyridyl radical. 3. An N-(1 claim 1 ,2 claim 1 ,5-oxadiazol-3-yl)pyridinecarboxamide and/or salt thereof as claimed in claim 1 , in whichW is a W1, W2 or W3 group,{'sub': 1', '6', '3', '7', '1', '6', '1', '6', '1', '6', '1', '4, 'R is (C-C)-alkyl, (C-C)-cycloalkyl, halo-(C-C)-alkyl, (C-C)-alkoxy, halo-(C-C)-alkoxy, cyano, nitro, methylsulfenyl, methylsulfinyl, methylsulfonyl, (C-C)-alkylcarbonylamino, benzoylamino, methoxycarbonyl, ethoxycarbonyl, benzoyl, phenoxy, methylcarbonyl, piperidinylcarbonyl, trifluoromethylcarbonyl, halogen, amino, aminocarbonyl, methylaminocarbonyl, dimethylaminocarbonyl, methoxymethyl, 1,2,4-triazol-1H,1-pyrazol-1H,2-thiophenyl, 2-pyridinyl, 3-pyridinyl, 4-pyridinyl, 1,2,4-oxadiazol-3-yl, benzoxazol-2-yl, 1-ethylbenzimidazol-2-yl, piperidin-1-yl, or phenyl substituted by at least one s radical selected from the group consisting of methyl, ethyl, methoxy, trifluoromethyl and halogen,'}{'sub': 1', '6', '1', '6', '3', '6', 'n', '1', '6', 'n', '1', '6', '1', '6', '2', '1', '6', '2', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6', '1', '6', '1', '6', '3', '6', 'n', '1', '6', '1', '6', '1', '6', '1', '6', '1', '4, 'sup': 1', '2', '2', '1', '1', '1', '1', '1', '1', '2, 'X and V are each independently hydrogen, nitro, halogen, cyano, (C-C)-alkyl, (C-C)-halo alkyl, (C-C)-cycloalkyl, OR, S(O)R, (C-C)-alkyl-S(O)R, (C-C)-alkyl-OR, (C-C)-alkyl-CON(R), (C-C)-alkyl-SON(R), (C-C)-alkyl-NRCOR, (C-C)-alkyl-NRSORor (C-C)-alkylheteroaryl, (C-C)-alkylheterocyclyl, where the 2 latter radicals are each substituted by at least one s radical selected from the group consisting of halogen, nitro, cyano, (C-C)-alkyl, halo-(C-C)-alkyl, (C-C)-cycloalkyl, S(O)—(C-C)-alkyl, (C-C)-alkoxy, halo-(C-C)-alkoxy, (C-C)- ...

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Номер записи: 41
06-03-2014 дата публикации

USE OF N-(1,2,5-OXADIAZOL-3-YL)BENZAMIDES FOR CONTROLLING UNWANTED PLANTS IN AREAS OF TRANSGENIC CROP PLANTS BEING TOLERANT TO HPPD INHIBITOR HERBICIDES

Номер: US20140066307A1
Автор: Hain Ruediger, Köhn Arnim, Laber Bernd, Poree Fabien, Van Almsick Andreas
Принадлежит: Bayer Intellectual Property GmbH

Use of N-(1,2,5-Oxadiazol-3-yl)benzamides of formula (I) or salts thereof 2. An N-(1 claim 1 ,2 claim 1 ,5-oxadiazol-3-yl)benzamide of formula (I) and/or a salt thereof according to claim 1 , where claim 1 , in formula (I){'sub': 1', '6', '3', '7', '1', '6', '1', '6', '1', '6, 'R is hydrogen, (C-C)-alkyl, (C-C)-cycloalkyl, halo-(C-C)-alkyl, (C-C)-alkoxy, halo-(C-C)-alkoxy, cyano, nitro, methylsulfenyl, methylsulfinyl, methylsulfonyl, acetylamino, benzoylamino, methoxycarbonyl, ethoxycarbonyl, benzoyl, methylcarbonyl, piperidinylcarbonyl, trifluoromethylcarbonyl, halogen, amino, aminocarbonyl, methylaminocarbonyl, dimethylaminocarbonyl, methoxymethyl, a heterocycle selected from the group consisting of pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, benzisoxazol-2-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-triazol-3-yl, 1-ethylbenzimidazol-2-yl, 4-methylthiazol-2-yl, thiophen-2-yl, furan-2-yl, furan-3-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, isoxazol-2-yl, isoxazol-3-yl, oxazol-2-yl, oxazol-3-yl, pyrrol-2-yl, pyrrol-3-yl, imidazol-2-yl, imidazol-5-yl, imidazol-4-yl, pyrazol-3-yl, pyrazol-5-yl, pyrazol-4-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isothiazol-3-yl, isothiazol-4-yl, isothiazol-5-yl, thiazol-2-yl, thiazol-4-yl, thiazol-5-yl, 1,2,3-triazol-4-yl, 1,2,3-triazol-5-yl, 1,2,5-triazol-3-yl, 1,3,4-triazol-2-yl, 1,2,4-triazol-3-yl, 1,2,4-triazol-5-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazol-5-yl, 1,3,4-oxadiazol-2-yl, 1,2,3-oxadiazol-4-yl, 1,2,3-oxadiazol-5-yl, 1,2,5-oxadiazol-3-yl, 1,2,4-thiadiazol-3-yl, 1,2,4-thiadiazol-5-yl, 1,3,4-thiadiazol-2-yl, 1,2,3-thiadiazol-4-yl, 1,2,3-thiadiazol-5-yl, 1,2,5-thiadiazol-3-yl, 2H-1,2,3,4-tetrazol-5-yl, 1H-1,2,3,4-tetrazol-1-yl, 1,2,3,4-oxatriazol-5-yl, 1,2,3,5-ox atriazol-4-yl, 1,2,3,4-thiatriazol-5-yl, 1,2,3,5-thiatriazol-4-yl, pyrazin-2-yl, pyrazin-3-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyridazin-3-yl and pyridazin-4-yl, which ...

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Номер записи: 42
06-03-2014 дата публикации

Fungicide Active Substance Combinations

Номер: US20140066407A1
Автор: Klaus STENZEL, Manfred JAUTELAT, Stefan DUTZMANN
Принадлежит: Bayer Intellectual Property GmbH

The novel active compound combinations comprising 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-2,4-dihydro-[1,2,4]-triazole-3-thione of the formula 2. The composition of claim 1 , wherein the weight ratio of active compound of the formula (I) toactive compound of group (1) is between 1:0.1 and 1:20,active compound of group (2) is between 1:0.2 and 1:150,active compound of group (3) is between 1:0.1 and 1:10,active compound of group (4) is between 1:1 and 1:50,active compound of group (5) is between 1:1 and 1:50,active compound of group (6) is between 1:0.1 and 1:50,active compound of group (7) is between 1:0.2 and 1:50,active compound of group (8) is between 1:0.2 and 1:50,active compound of group (9) is between 1:0.1 and 1.50,active compound of group (10) is between 1:0.1 and 1:50,active compound of group (11) is between 1:0.1 and 1:50,active compound of group (12) is between 1:0.1 and 1:50,active compound of group (13) is between 1:1 and 1:50,active compound of group (14) is between 1:1 and 1:20,active compound of group (15) is between 1:1 and 1:50,active compound of group (16) is between 1:1 and 1:50,active compound of group (17) is between 1:0.1 and 1:10,active compound of group (18) is between 1:0.05 and 1:20,active compound of group (19) is between 1:0.1 and 1:10 andactive compound of group (20) is between 1:0.1 and 1:10.3. A method for controlling fungi comprising applying the composition according to to the fungi and/or their habitat.4. (canceled)5. A process for preparing fungicidal compositions claim 1 , characterized in that active compound combinations according to are mixed with extenders and/or surfactants. The present invention relates to novel active compound combinations which consist of the known 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-2,4-dihydro-[1,2,4]-triazole-3-thione and further known fungicidally active compounds, and which are highly suitable for controlling phytopathogenic fungi.It is already known ...

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Номер записи: 43
13-03-2014 дата публикации

HERBICIDAL COMPOSITIONS COMPRISING AMINOPYRALID AND BENTAZON

Номер: US20140073507A1
Автор: Carranza Garzon Nelson M., Mann Richard K.
Принадлежит: DOW AGROSCIENCES LLC

Provided herein are herbicidal compositions containing (a) aminopyralid or an agriculturally acceptable salt or ester thereof and (b) bentazon or an agriculturally acceptable salt thereof. The compositions provide synergistic weed control of undesirable vegetation, e.g., in rice, wheat, barley, oats, rye, sorghum, corn or maize, oilseed rape/canola, vegetables, pastures, grasslands, rangelands, fallowland, turf, tree and vine orchards, aquatics, industrial vegetation management or rights-of-way. 2. The composition of claim 1 , wherein (a) is the triisopropanolammonium salt or choline salt of compound (I).3. The composition of claim 1 , wherein (a) is the compound of formula (I) claim 1 , which is the carboxylic acid.4. The composition of claim 1 , wherein the (b) is the sodium salt of compound (II).5. The composition of claim 1 , wherein the ratio of the acid equivalent weight of the compound of formula (I) or agriculturally acceptable salt or ester thereof to the weight of the compound of formula II or agriculturally acceptable salt thereof is from about 1:135 to about 1:4.6. The composition of claim 5 , wherein the ratio is from about 1:45 to about 1:12.7. The composition of claim 1 , further comprising an agriculturally acceptable adjuvant or carrier.8. The composition of claim 1 , which is synergistic as determined by the Colby equation.9. A method of controlling undesirable vegetation which comprises contacting the vegetation or the locus thereof with or applying to the soil or water to prevent the emergence or growth of vegetation the composition of .11. The method of claim 10 , wherein the undesirable vegetation is controlled in rice claim 10 , wheat claim 10 , barley claim 10 , oats claim 10 , rye claim 10 , sorghum claim 10 , corn claim 10 , maize claim 10 , pastures claim 10 , grasslands claim 10 , rangelands claim 10 , fallowland claim 10 , turf claim 10 , tree and vine orchards claim 10 , industrial vegetation management or rights-of-way.12. The method ...

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Номер записи: 44
13-03-2014 дата публикации

PLANT PATHOGEN INHIBITOR COMBINATIONS AND METHODS OF USE

Номер: US20140073675A1
Автор: Koivunen Marja, Marrone Pamela, Su Hai
Принадлежит: MARRONE BIO INNOVATIONS, INC.

Combinations, compositions and methods of use for modulating plant pathogen infection using plant extracts containing anthraquinone derivatives which induce resistance to plant phytopathogens and an antimicrobial agent, a biological control agent and/or a surfactant having fungicidal activity 114-. (canceled)16. The synergistic combination of claim 15 , wherein the combination is a composition.17. The synergistic combination of claim 15 , wherein the E/Ee is at least 1.6.18. The synergistic combination of claim 15 , wherein the phytopathogenic infection is a fungal infection.19ReynoutriaReynoutria sachalinensis.. The synergistic combination of claim 15 , wherein the sp. is21. The method of claim 20 , wherein the E/Ee is at least 1.6.22. The method of claim 20 , wherein the phytopathogenic infection is a fungal infection.23ReynoutriaReynoutria sachalinensis. The method of claim 20 , wherein the sp. is This application is a continuation application of U.S. application Ser. No. 12/845,883, filed Jul. 29, 2010, which claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Application No. 61/230,102, filed Jul. 30, 2009, both of which are hereby incorporated by reference into the present disclosure.Disclosed herein are combinations, compositions and methods of use for modulating plant pathogen infection using plant extracts containing anthraquinone derivatives which induce resistance to plant phytopathogens and an antimicrobial agent, a biological control agent and/or a surfactant having fungicidal activity.Plants have evolved highly effective mechanisms for resistance to disease caused by infectious agents, such as bacteria, fungi and viruses. This resistance can be caused by several mechanisms, the best known of which are the systemic acquired resistance (SAR; Ross, 1961; Durrant and Dong, 2004) and induced systemic resistance (ISR; van Loon et al., 1998). In the most simple case, the inducer is the plant pathogen itself, in other cases, the inducer can be ...

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Номер записи: 45
20-03-2014 дата публикации

N-(1,3,4-OXADIAZOL-2-YL)ARYLCARBOXAMIDES AND USE THEREOF AS HERBICIDES

Номер: US20140080705A1
Автор: AHRENS HARTMUT, Braun Ralf, Dörner-Rieping Simon, GATZWEILER ELMAR, Häuser-Hahn Isolde, Heinemann Ines, KOEHN ARNIM, LEHR Stefan, Rosinger Christoper Hugh
Принадлежит: Bayer Intellectual Property GmbH

N-(1,3,4-Oxadiazol-2-yl)arylcarboxamides of the general formula (I) are described as herbicides. 2. An N-(1 claim 1 ,3 claim 1 ,4-oxadiazol-2-yl)arylcarboxamide as claimed in claim 1 , in whichA is N or CY,{'sub': 1', '6', '3', '7', '1', '6', '3', '7, 'R is hydrogen, (C-C)-alkyl, (C-C)-cycloalkyl, halo-(C-C)-alkyl, (C-C)-cycloalkylmethyl, methoxycarbonylmethyl, ethoxycarbonylmethyl, acetylmethyl, methoxymethyl, methoxyethyl, benzyl, pyrazin-2-yl, furan-2-yl, tetrahydrofuran-2-yl, morpholine, dimethylamino, or phenyl substituted by at least one s radical selected from the group consisting of methyl, methoxy, trifluoromethyl and halogen;'}{'sub': 1', '6', '1', '6', '3', '6', 'n', '1', '6', 'n', '1', '6', '1', '6', '2', '1', '6', '2', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6', '1', '6', '1', '6', 'n', '1', '6', '1', '6', '1', '6, 'sup': 1', '2', '2', '1', '1', '1', '1', '1', '1', '2, 'X is nitro, halogen, cyano, (C-C)-alkyl, halo-(C-C)-alkyl, (C-C)-cycloalkyl, OR, S(O)R, (C-C)-alkyl-S(O)R, (C-C)-alkyl-OR, (C-C)-alkyl-CON(R), (C-C)-alkyl-SON(R), (C-C)-alkyl-NRCOR, (C-C)-alkyl-NRSOR, (C-C)-alkylheteroaryl, (C-C)-alkylheterocyclyl, where the two latter radicals are each substituted by s halogen, (C-C)-alkyl, halo-(C-C)-alkyl, S(O)—(C-C)-alkyl, (C-C)-alkoxy, halo-(C-C)-alkoxy radicals, and where heterocyclyl bears n oxo groups,'}{'sub': 1', '6', '1', '6', 'n', '2', '2', '2', '2', '1', '6', 'n', '1', '6', '1', '6', '2', '1', '6', '2', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '3', '6', 'n', '1', '6', '1', '6', '1', '6', '1', '6', '1', '4, 'sup': 1', '2', '1', '1', '1', '2', '1', '1', '2', '1', '1', '1', '1', '1', '1', '2, 'Y hydrogen, nitro, halogen, cyano, (C-C)-alkyl, (C-C)-haloalkyl, OR, S(O)R, SON(R), N(R), NRSOR, NRCOR, (C-C)-alkyl-S(O)R, (C-C)-alkyl-OR, (C-C)-alkyl-CON(R), (C-C)-alkyl-SON(R), (C-C)-alkyl-NRCOR, (C-C)-alkyl-NRSOR, (C-C)-alkylphenyl, (C-C)-alkylheteroaryl, (C-C)-alkylheterocyclyl, phenyl, heteroaryl or ...

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Номер записи: 46
20-03-2014 дата публикации

METHODS FOR INHIBITING FASCIN

Номер: US20140080843A1
Автор: Huang Xin-Yun, SHUE Christy Young
Принадлежит:

Provided are compositions and methods for treating a condition or disorder mediated by fascin activity in a subject in need thereof which method comprises administering to the subject a therapeutically effective amount of at least one compound of any one of Formula I-a to I-n, II, II-a, II-b or III or a pharmaceutically acceptable salt thereof. 6. The method of claim 1 , wherein Ris phenyl optionally substituted with one claim 1 , two claim 1 , or three groups chosen from halo and lower alkyl.7. The method of claim 1 , wherein Ris triazole.8. The method of claim 2 , wherein m is 0.9. The method of claim 1 , wherein Lis —N(R)S(O)—.10. The method of claim 1 , wherein Lis —S—.11. The method of claim 1 , wherein Xis OH and Xis O.12. The method of claim 1 , wherein Ris independently selected from the group consisting of OH claim 1 , halo claim 1 , lower alkyl claim 1 , and —OR.13. The method of claim 1 , wherein the compound is selected from5-(3,4-dichlorobenzyl)-1-(S,S,-dioxo-tetrahydrothiophen-3-yl)-1H-pyrazolo-[3,4-d]pyrimidin-4(5H)-one;N-(1-(4-(trifluoromethyl)benzyl)-1H-indazol-3-yl)furan-2-carboxamide;N-(3-(1H-1,2,4-triazol-3-ylthio)-4-hydroxynaphthalen-1-yl)-2,5-dimethylbenzenesulfonamide;N-(3(1H-1,2,4-triazol-3-ylthio)-4-hydroxynaphthalen-1-yl)-4-ethoxybenzenesulfonamide;N-(3-(1H-1,2,4-triazol-3-ylthio)-4-hydroxynaphthalen-1-yl)-4-methoxybenzenesulfonamide;N-(3-(1H-1,2,4-triazol-3-ylthio)-4-hydroxynaphthalen-1-yl)-4-ethylbenzenesulfonamide;N-(3-(1H-1,2,4-triazol-3-ylthio)-4-hydroxynaphthalen-1-yl)-4-trimethylbenzenesulfonamide;(Z)—N-(3-(1H-1,2,4-triazol-3-ylthio)-4-oxonaphthalen-1(4H)-ylidene)benzenesulfonamide;N-(3-(1H-1,2,4-triazol-3-ylthio)-4-hydroxynaphthalen-1-yl)-4-bromobenzenesulfonamide;N-(3-(1H-1,2,4-triazol-3-ylthio)-4-hydroxynaphthalen-1-yl)-2,4-dimethylbenzenesulfonamide;5-(3-chlorobenzyl)-1-(2-hydroxyethyl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one;2-(4-oxo-1-(S,S,-dioxo-tetrahydrothiophen-3-yl)-1H-pyrazolo[3,4-d]-pyrimidin-5(4H)-yl)-N-(3-( ...

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Номер записи: 47
10-04-2014 дата публикации

HERBICIDALLY AND FUNGICIDALLY ACTIVE 3-PHENYLISOXAZOLINE-5-CARBOXAMIDES AND 3-PHENYLISOXAZOLINE-5-THIOAMIDES

Номер: US20140100108A1
Автор: DITTGEN JAN, Feucht Dieter, FRENZEL Thomas, GATZWEILER ELMAR, HAAF Klaus Bernhard, HÄEUSER-HAHN ISOLDE, Heinemann Ines, HILLS Jeffrey Martin, KEHNE Heinz, Rinolfi Philippe, ROSINGER CHRISTOPHER HUGH, SCHMITT Monika H., Willms Lothar
Принадлежит: Bayer Intellectual Property GmbH

3-Phenylisoxazoline-5-carboxamides and 3-phenylisoxazoline-5-thioamides of the formula (I) and their use as herbicides and fungicides are described. 4. A herbicidal composition which comprises a herbicidally effective amount of at least one compound of formula (I) and/or salt thereof as claimed in .5. The herbicidal composition as claimed in claim 4 , in a mixture with at least one formulation auxiliary.6. The herbicidal composition as claimed in claim 4 , comprising at least one further pesticidally active compound selected from the group consisting of an insecticide claim 4 , an acaricide claim 4 , a herbicide claim 4 , a fungicide claim 4 , a safener and a growth regulator.7. The herbicidal composition as claimed in claim 6 , comprising a safener.8. The herbicidal composition as claimed in claim 7 , where the safener is selected from the group consisting of mefenpyr-diethyl claim 7 , cyprosulfamide claim 7 , isoxadifen-ethyl claim 7 , cloquintocet-mexyl claim 7 , benoxacor and dichlormid.9. The herbicidal composition as claimed in claim 6 , comprising a further herbicide.13. A method for controlling an unwanted plant claim 1 , comprising applying an effective amount of at least one compound of formula (I) and/or salt thereof as claimed in claim 1 , to a plant and/or a site of an unwanted vegetation.14. A compound of formula (I) and/or salt thereof as claimed in claim 1 , capable of being used for controlling an unwanted plant.15. A compound of formula (I) claim 14 , capable of being used as claimed in claim 14 , wherein said compound of formula (I) is used for controlling an unwanted plant in a crop of a useful plant.16. A compound of formula (I) and/or salt thereof capable of being used as claimed in claim 15 , wherein said useful plant is a transgenic useful plant.17. A fungicidal composition which comprises a fungicidally effective amount of at least one compound of formula (I) and/or salt thereof as claimed in .18. The fungicidal composition as claimed in ...

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Номер записи: 48
07-01-2016 дата публикации

Fungicidal Active Compound Combinations

Номер: US20160000076A1
Автор: Dahmen Peter, FISCHER Reiner, Wachendorff-Neumann Ulrike
Принадлежит:

Safeners for herbicides are suitable for increasing the microbicidal activity of fungicides. 1. Use of a safener for increasing the microbicidal activity of a fungicide.4. Use according to one or more of to for dressing seed.5. Use according to one or more of to in transgenic plants.6. Fungicidal composition , comprising one or more compounds of group 1 according to and one or more compounds of groups 2 to 24 according to , except for the following combinations:daimuron and metominostrobin,oxabetrinil and metalaxyl,N-methylsulphonyloxyphenyl-N-methylthiolcarbamate and kasugamycin.7. Fungicidal composition according to claim 6 , where the fungicide is selected from the group consisting of prothioconazole claim 6 , tebuconazole claim 6 , fluoxastrobin claim 6 , trifloxystrobin and spiroxamine.8. Fungicidal composition according to or claim 6 , where the safener is mefenpyr.9. Fungicidal composition according to claim 8 , where the fungicide is selected from the group consisting of prothioconazole claim 8 , tebuconazole claim 8 , fluoxastrobin claim 8 , trifloxystrobin and spiroxamine.10. Method for controlling unwanted phytopathogenic fungi claim 8 , characterized in that a fungicidal composition according to one or more of to is applied to the unwanted phytopathogenic fungi and/or their habitat and/or seed. The invention relates to the use of safeners for increasing the activity of fungicides, to combinations of fungicides and safeners and to their use for controlling unwanted microorganisms.Numerous triazole derivatives, strobilurins, aniline derivatives, dicarboximides, carboxamides and other chemical compounds are already used for controlling unwanted microorganisms (see, for example, The Pesticide Manual, 13th Edition, Farnham, 2003).However, since the environmental and economic requirements imposed on modern-day fungicides are continually increasing, with regard, for example, to the spectrum of action, toxicity, selectivity, application rate, formation of ...

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Номер записи: 49
07-01-2016 дата публикации

MODULATION OF SALTY TASTE PERCEPTION BY ALTERING THE FUNCTION OF BITTER- OR PKD2L1-EXPRESSING TASTE RECEPTOR CELLS

Номер: US20160000126A1
Автор: OKA Yuki, Zuker Charles
Принадлежит: The Trustees of Columbia University in the City of New York

The current invention is in the field of taste and relates to methods and compositions to modulate the perceived taste of saltiness in food or food products where salty taste is desired. The methods and compositions relate to altering the activation and/or activity of the bitter-sensing taste receptor cells and the PKD2L1-expressing taste receptor cells. The invention also relates to food and food products containing agents and composition that alter the activation and/or activity of the bitter-sensing taste receptor cells and the PKD2L1-expressing taste receptor cells. 1. A method for modulating the perceived saltiness of a salty taste stimulant in a food or food product , comprising administering to a subject who is ingesting the food or food product , an agent that alters the activation or activity of bitter-sensing taste receptor cells (TRCs) and/or their concomitant pathway.2. The method of claim 1 , wherein the agent is administered before claim 1 , during or slightly after the subject ingests the food or food product.3. The method of claim 1 , wherein the food or food product contains sodium chloride.4. The method of claim 1 , wherein the food or food product contains a sodium substitute.5. The method of claim 4 , wherein the sodium substitute is chosen from the group consisting of potassium chloride claim 4 , magnesium chloride claim 4 , and calcium chloride.6. The method of claim 1 , wherein the food or food product is chosen from the group consisting of crackers claim 1 , potato chips claim 1 , corn chips claim 1 , tortilla chips claim 1 , sauces claim 1 , canned soups claim 1 , and canned vegetables.7. The method of claim 1 , wherein the agent is chosen from the group consisting of chemicals claim 1 , phytochemicals claim 1 , pharmaceuticals claim 1 , biologics claim 1 , small organic molecules claim 1 , antibodies claim 1 , nucleic acids claim 1 , peptides claim 1 , and proteins.8. The method of claim 1 , wherein the agent is allyl isothiocyanate.9. A ...

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Номер записи: 50
07-01-2016 дата публикации

USE OF QUINOLINE DERIVATIVES FOR IMPROVING PLANT YIELD

Номер: US20160002168A1
Автор: Bickers Udo, BONFIG-PICARD Georg, Hacker Erwin, Hills Martin Jeffrey, LEHR Stefan, RUIZ-SANTAELLA MORENO Juan Pedro, Schmidt Mathias
Принадлежит:

Compounds (A) can be used for increasing the yield of useful plants or crop plants with respect to their harvested plant organs, wherein the Compound (A) is selected from compounds of the formula (I) and hydrates or salts thereof, 2. The compound as claimed in claim 1 , wherein Compound (A) is 1-methylhexyl (5-chloro-8-quinolinoxy)acetate (“cloquintocet-mexyl”).3. The compound as claimed in claim 1 , that is capable of increasing grain yield of crop plants selected from group consisting of cereals claim 1 , canola claim 1 , soybean and cotton crops.4. The compound as claimed in claim 1 , that is capable of increasing grain yield of crop plants selected from group consisting of wheat claim 1 , barley claim 1 , rye or triticale plants.5. The compound as claimed in claim 1 , that is capable of increasing gluten content of seed kernels of crop plants selected from group consisting of cereals claim 1 , canola and soybean crops.6. The compound as claimed in claim 1 , that is capable of increasing gluten content of seed kernels of crop plants selected from group consisting of cereal crops.7. The compound as claimed in claim 1 , that is capable of increasing protein content of seed kernels of crop plants selected from group consisting of cereals claim 1 , canola and soybean crops.8. The compound as claimed in claim 1 , that is capable of increasing yield of the amount by weight of beets of beet plants.9. The compound as claimed in claim 1 , that is capable of increasing sugar content of sugar plants.10. The compound as claimed in claim 1 , that is capable of increasing germination and emergence of cereal crops.11. The compound as claimed in claim 1 , that is capable of increasing biomass yield of maize plants growing in absence of extraordinary environmental conditions.12. The compound as claimed in claim 1 , that is capable of increasing biomass yield of sugar plants.13. A method for increasing yield of useful plants and/or crop plants with respect to their harvested plant ...

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Номер записи: 51
05-01-2017 дата публикации

CYCLOPROPANAMINE COMPOUND AND USE THEREOF

Номер: US20170001994A1
Автор: DAINI Masaki, Hattori Yasushi, Ito Mitsuhiro, KAKU Tomohiro, KOJIMA Takuto, MATSUMOTO Shigemitsu, Morimoto Shinji, TOYOFUKU Masashi
Принадлежит:

The present invention provides a compound having a lysine-specific demethylase-1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, developmental disorders, particularly diseases having intellectual disability (e.g., autistic spectrum disorders, Rett syndrome, Down's syndrome, Kabuki syndrome, fragile X syndrome, Kleefstra syndrome, neurofibromatosis type 1, Noonan syndrome, tuberous sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, spinocerebellar degeneration (e.g., dentatorubural pallidoluysian atrophy) and Huntington's disease), epilepsy (e.g., Dravet syndrome) or drug dependence, and the like. A compound represented by the formula 2. The compound according to claim 1 , wherein A is(1) an optionally substituted heterocyclic group, or{'sub': '3-10', '(2) an optionally substituted Ccycloalkyl group,'}or a salt thereof.3. The compound according to claim 1 , wherein B is a ring selected from(1) a 5- or 6-membered aromatic heterocycle, and(2) a benzene ring fused with an optionally substituted 5- or 6-membered ring,wherein the ring represented by B is optionally substituted, and binds, via two adjacent carbon atoms with one atom in between, to a group represented by the formula (II), and a group represented by the formula (III),or a salt thereof.5. The compound according to claim 1 , wherein R claim 1 , Rand Rare each independently a hydrogen atom or an optionally substituted Calkyl group claim 1 ,or a salt thereof.6. The compound according to claim 1 , wherein Ris(1) a hydrogen atom,{'sub': '1-6', '(2) an optionally substituted Calkyl group,'}{'sub': '3-10', '(3) an optionally substituted Ccycloalkyl group, or'}(4) an optionally substituted heterocyclic group,or a salt thereof.8. The compound according to claim 1 , wherein A is{'sub': '1-6', '(1) a piperidinyl group, an isoxazolyl group, a pyrazolyl group, a thiadiazolyl group, a thiazolyl group, a tetrahydropyranyl group ...

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Номер записи: 52
02-01-2020 дата публикации

CRYSTAL MODIFICATIONS OF ODEVIXIBAT

Номер: US20200002299A1
Автор: Bohlin Martin, Bryland Rikard, Byröd Eva, Dahlquist Ann-Charlotte, Elversson Jessica, Gillberg Per-Göran, Gustafsson Nils Ove, Lundqvist Robert, Tivert Anna-Maria, Ymen Ingvar
Принадлежит:

The present invention relates to crystal modifications of 1,1-dioxo-3,3-dibutyl-5-phenyl-7-methylthio-8-(N—{(R)-α-[N—((S)-1-carboxypropyl)carbamoyl]-4-hydroxybenzyl}carbamoylmethoxy)-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepine (odevixibat), more specifically crystal modifications 1 and 2 of odevixibat. The invention also relates to a process for the preparation of crystal modification 1 of odevixibat, to a pharmaceutical composition comprising crystal modification 1, and to the use of this crystal modification in the treatment of various conditions as described herein. 1. A crystalline hydrate of odevixibat.2. The hydrate according to claim 1 , which is a channel hydrate.3. The hydrate according to claim 1 , which comprises from about 0 to about 2 moles of water associated with the crystal per mole of odevixibat.4. The hydrate according to claim 1 , which is a sesquihydrate.5. The hydrate according to claim 1 , having an XRPD pattern claim 1 , obtained with CuKα1-radiation claim 1 , with peaks at °2θ positions 5.6±0.2 claim 1 , 6.7±0.2 and/or 12.1±0.2.6. The hydrate according to claim 5 , having an XRPD pattern claim 5 , obtained with CuKα1-radiation claim 5 , with specific peaks at °2θ positions 5.6±0.2 claim 5 , 6.7±0.2 and 12.1±0.2 and one or more of the characteristic peaks: 4.1±0.2 claim 5 , 4.6±0.2 claim 5 , 9.3±0.2 claim 5 , 9.4±0.2 and 10.7±0.2.7. (canceled)8. The crystal modification according to claim 5 , having a crystallinity of greater than about 99%.9. A mixed solvate of odevixibat claim 5 , containing about two moles of water per mole of odevixibat.10. The mixed solvate according to claim 9 , wherein the organic solvent is methanol claim 9 , ethanol claim 9 , 2-propanol claim 9 , acetone claim 9 , acetonitrile claim 9 , 1 claim 9 ,4-dioxane claim 9 , DMF or DMSO.11. The mixed solvate according to claim 9 , wherein the organic solvent is ethanol.12. The mixed solvate according to claim 9 , having an XRPD pattern claim 9 , obtained with CuKα1-radiation ...

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Номер записи: 53
05-01-2017 дата публикации

BICYCLOAMINE-SUBSTITUTED-N-BENZENESULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS

Номер: US20170002008A1
Автор: Egbertson Melissa, Jones Kristen L. G., Layton Mark E., Li Dansu, Peng Xuanjia, Roecker Anthony J., Wang Xiu
Принадлежит: Merck Sharp & Dohme Corp.

Disclosed are compounds of Formula A-a, or a salt thereof: Where “B” and “R” through “R” are as defined herein, which compounds have properties for blocking Na1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A-a or their salts, and methods of treating neuropathic pain disorders using the same. 2. A compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein:{'sup': 4', '5, 'Rand Rare independently: —H; or a cyclic-, branched- or linear-alkyl moiety of up to 6 carbon atoms; and'}{'sup': 1', '2, 'sub': '3', 'Rand Rare independently: —H; —F; —Cl; —Br; —CN; a cyclic-, branched, or linear-alkyl moiety comprising up to 6 carbon atoms; or —CF.'}34-. (canceled)5. A compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein:{'sup': '1', 'sub': '3', 'Ris: —H; —F; —Cl; —Br; —CN; or —CH;'}{'sup': '2', 'sub': 3', '2', '3', '3, 'Ris: —H; —F; —Cl; —Br; —CN; CH; —CHCH; or —CF; and'}{'sup': 4', '5, 'sub': '3', 'Rand Rare independently: (i) —H; or (ii) —CH.'}6. (canceled)8. A compound of claim 7 , or a pharmaceutically acceptable salt thereof claim 7 , wherein:{'sup': 3', '4', '5, 'sub': '2', 'A, Aand Aare each [—CH—]; and'} [{'sup': '1', 'sub': '3', 'Ris independently: —H; —F; —Cl; —Br; —CN; or CH;'}, {'sup': '2', 'sub': 3', '3', '2', '3, 'Ris independently: —H; —F; —Cl; —Br; —CN; —CF, —CH; or —CHCH.'}], 'in the structure of Formula A-a9. (canceled)10. A compound of claim 7 , or a pharmaceutically acceptable salt thereof claim 7 , wherein:{'sup': 10a2', '11a2, 'claim-text': [{'sup': 10a2', '11a2, 'claim-text': (a) hydrogen;', '(b) halogen;', {'sub': 1-6', '3-6', '3-6', '1-4', '3-4, '(c) an alkyl moiety which is —C-linear-alkyl, —C-branched-alkyl, or —C-cycloalkyl, which alkyl moiety is optionally substituted with one or more: (i) halogen; (ii) an aryl moiety optionally substituted with C-linear-alkoxy or C-branched-alkoxy; or (iii) —OH; ...

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Номер записи: 54
05-01-2017 дата публикации

Benzothiadiazole-based conjugated molecules capable of forming films on conductive surfaces by electrochemical method

Номер: US20170002024A1
Автор: Anando Devadoss, Cuihua Xue, Han-Kuan Anthony Tsai
Принадлежит: Hitachi Chemical Co America Ltd, Hitachi Chemical Co America Ltd & Hitachi Chemical Company Ltd, Hitachi Chemical Co Ltd

The present disclosure provides new materials that combine the advantages of well-defined polymeric starting materials and the convenience of surface modification by physical methods into one package and, thus, offers a general and powerful platform suitable for use in numerous applications.

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Номер записи: 55
03-01-2019 дата публикации

IDO INHIBITORS

Номер: US20190002402A1
Автор: Balog James Aaron, Cherney Emily Charlotte, Markwalder Jay A., Shan Weifang, Williams David K.
Принадлежит:

There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention. 2. The compound according to wherein Rand Rare independently H claim 1 , Cto Calkyl claim 1 , Cto Calkoxy claim 1 , or join together to form cyclopropyl or cyclobutyl.3. The compound according to wherein Z is —NH— and Ris —SOR claim 1 , halo (C-Calkyl) claim 1 , thiazolyl or oxazolyl claim 1 , wherein Ris Cto Calkyl claim 1 , Cto Ccycloalkyl4. The compound according to wherein Z is O and Ris H.5. The compound according to wherein Ris —COR.6. The compound according to wherein Ris a 5 membered heterocycle containing from 1 to 4 heteroatoms selected from N claim 1 , O claim 1 , and S.7. The compound according to wherein Ris H and Ris —CORor —CONRR; Ris H claim 1 , and Ris phenyl claim 1 , pyridyl claim 1 , isoxazolyl claim 1 , thiadiazolyl claim 1 , indolinyl claim 1 , or benzyl claim 1 , wherein Rmay optionally be substituted with from 1 to 3 substituents selected from the group consisting of halo claim 1 , amino claim 1 , phenoxy claim 1 , benzoxy claim 1 , isoxalyl claim 1 , Cto Calkoxy claim 1 , Cto Calkyl claim 1 , halo-Cto Calkyl claim 1 , and CN.8. The compound according to wherein Ris Cto Ccycloalkyl optionally substituted with halo claim 1 , —OH or Cto Calkoxy; Cto Calkyl optionally substituted with halo claim 1 , —OH or phenyl claim 1 , wherein said phenyl is optionally substituted with Cto Chaloalkyl claim 1 , Cto Calkoxy claim 1 , halo or Cto Calkyl; Cto Calkenyl; Cto Calkoxy; or benzyl optionally substituted with Cto Calkyl claim 1 , halo claim 1 , Cto Calkoxy claim 1 , or haloalkyl.9. The compound according to wherein Ris a Cto Cheterocycloalkyl containing from 1 to 4 heteroatoms selected from O claim 1 , N or S.10. The compound ...

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Номер записи: 56
01-01-2015 дата публикации

TREATMENT OF CANCER WITH HETEROCYCLIC INHIBITORS OF GLUTAMINASE

Номер: US20150004134A1
Автор: BENNETT Mark K., Bromley Susan D., Chen Lijing, Goyal Bindu, Gross Matthew I., Laidig Guy, Li Jim, Sjogren Eric Brian, Stanton Timothy Friend
Принадлежит: CALITHERA BIOSCIENCES, INC.

The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention. 223-. (canceled)2548-. (canceled)49. The method of any preceding claim , wherein the cancer is selected from breast cancer , colorectal cancer , endocrine cancer , lung cancer , melanoma , mesothelioma , renal cancer and a B cell malignancy.50. (canceled)51. The method of claim 49 , wherein the breast cancer comprises basal-type breast cancer cells claim 49 , triple-negative breast cancer cells or claudin-low breast cancer cells.5256-. (canceled)57. The method of claim 49 , wherein the endocrine cancer is selected from adrenal cortex adenoma claim 49 , adrenal cortex carcicnoma claim 49 , adrenal gland pheochromocytoma and parathyroid gland adenoma.5860-. (canceled)61. The method of claim 49 , wherein the B cell malignancy is selected from multiple myeloma claim 49 , leukemia and lymphoma.6263-. (canceled)64. The method of claim 61 , wherein the leukemia is selected from acute lymphoblastic leukemia and chronic lymphoblastic leukemia.65. (canceled)66. The method of claim 61 , wherein the lymphoma is selected from Burkitt's lymphoma claim 61 , Diffuse large B cell lymphoma claim 61 , follicular lymphoma and Hodgkin's lymphoma.67. The method of or claim 61 , further comprising conjointly administering one or more additional chemotherapeutic agents.6872-. (canceled)73. The method of claim 67 , wherein the one or more additional chemotherapeutic agents are selected from aminoglutethimide claim 67 , amsacrine claim 67 , anastrozole claim 67 , asparaginase claim 67 , bcg claim 67 , bicalutamide claim 67 , bleomycin claim 67 , bortezomib claim 67 , buserelin claim 67 , busulfan claim 67 , campothecin claim 67 , capecitabine claim 67 , carboplatin claim 67 , carfilzomib claim 67 , carmustine claim 67 , chlorambucil claim 67 , chloroquine claim 67 , ...

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Номер записи: 57
14-01-2021 дата публикации

FUNGICIDAL COMPOSITIONS

Номер: US20210007358A1
Автор: BEAUDEGNIES Renaud, Haas Ulrich Johannes, HOFFMAN Thomas James, Pouliot Martin, Stierli Daniel
Принадлежит: SYNGENTA PARTICIPATIONS AG

A fungicidal composition comprising a mixture of components (A) and (B), wherein components (A) and (B) are as defined in claim and use of the compositions in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi. 2. A fungicidal composition according claim 1 , wherein component (A) is a compound selected from:N-methoxy-N-[[4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]cyclopropanecarboxamide (compound X.01),N-methoxy-N-[[4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]pent-4-ynamide (compound X.02),N-methoxy-2-methyl-N-[[4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]prop-2-enamide (compound X.03),N,2-dimethoxy-N-[[4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]propanamide (compound X.04),N-cyclopropyl-3,3,3-trifluoro-N-[[4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]propanamide (compound X.05),2,2-difluoro-N-(2-methoxyethyl)-N-[[4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]cyclo propanecarboxamide (compound X.06),N-ethyl-2-methyl-N-[[4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]propanamide (compound X.07),N-[[3-floro-4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]-N-methoxy-propanamide (compound X.08),2-methoxy-N-(2,2,2-trifluoroethyl)-N-[[4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl] acetamide (compound X.09),N-[[2,3-difluoro-4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]-N-methoxy-cyclopropane carboxamide (compound X.10),2-(difluoromethoxy)-N-methyl-N-[[4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]acetamide (compound X.11),N-ethoxy-2-methoxy-N-[[4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]propanamide (compound X.12),N-isopropyl-N-[[4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]tetrahydrofuran-2-carboxamide (compound X.13),1-methoxy-3-methyl-1-[[4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]urea (compound X.14),3- ...

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Номер записи: 58
14-01-2021 дата публикации

PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF

Номер: US20210009542A1
Автор: Chen Shuang, Frost Jennifer M., Kym Philip R., Wang Xueqing, Welch Dennie, Xiong Zhaoming
Принадлежит:

Provided herein are compounds, compositions, and methods useful for inhibiting protein tyrosine phosphatase, e.g., protein tyrosine phosphatase non-receptor type 2 (PTPN2) and/or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and for treating related diseases, disorders and conditions favorably responsive to PTPN1 or PTPN2 inhibitor treatment, e.g., a cancer or a metabolic disease. This application is a continuation of International Patent Application No. PCT/US2019/038459, filed on Jun. 21, 2019, which claims the benefit of, and priority to, U.S. Provisional Application No. 62/688,226, filed on Jun. 21, 2018, the contents of each of which are incorporated herein by reference in their entirety.Cancer immunotherapy regimens targeting immune evasion mechanisms including checkpoint blockade (e.g. PD-1/PD-L1 and CTLA-4 blocking antibodies) have been shown to be effective in treating in a variety of cancers, dramatically improving outcomes in some populations refractory to conventional therapies. However, incomplete clinical responses and the development of intrinsic or acquired resistance will continue to limit the patient populations who could benefit from checkpoint blockade.Protein tyrosine phosphatase non-receptor type 2 (PTPN2), also known as T cell protein tyrosine phosphatase (TC-PTP), is an intracellular member of the class 1 subfamily of phospho-tyrosine specific phosphatases that control multiple cellular regulatory processes by removing phosphate groups from tyrosine substrates. PTPN2 is ubiquitously expressed, but expression is highest in hematopoietic and placental cells (Mosinger, B. Jr. et al., 89:499-503; 1992). In humans, PTPN2 expression is controlled post-transcriptionally by the existence of two splice variants: a 45 kDa form that contains a nuclear localization signal at the C-terminus upstream of the splice junction, and a 48 kDa canonical form which has a C-terminal ER retention motif (Tillmann U. et al., 14:3030-3040; 1994). The 45 kDa ...

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Номер записи: 59
09-01-2020 дата публикации

METHOD FOR PREPARING 3,7-BIS(DIMETHYLAMINO)PHENOTHIAZIN-5-YLIUM IODIDE

Номер: US20200010438A1
Автор: Feraud Michel, LAURENT Marina, QUERU Stéphane, Sayah Babak
Принадлежит: PROVEPHARM LIFE SOLUTIONS

Method for preparing 3,7-bis(dimethylamino)phenothiazin-5-ylium iodide, the method resulting in a high purity while being very simple to implement and producing high yields. The method uses phenothiazine as a starting material and includes the following steps: a) treating phenothiazine with diiodine, b) treating the reaction medium directly obtained from step a) with dimethylamine. 111-. (canceled)12. A process for preparing 3 ,7-bis(dimethylamino)phenothiazin-5-ylium iodide , this process using phenothiazine as starting product and comprising the following steps:a) treating phenothiazine with diiodine,b) treating the reaction medium directly resulting from step a) with dimethylamine.13. The process as claimed in claim 12 , wherein the treatment with diiodine is carried out with an amount of diiodine claim 12 , relative to the phenothiazine claim 12 , ranging from 2.5 molar equivalents to 3.5 molar equivalents.14. The process as claimed in claim 12 , wherein claim 12 , before step b) claim 12 , the reaction medium resulting from step a) is conditioned at a temperature ranging from 5° C. to 50° C.15. The process as claimed in claim 12 , wherein the treatment with dimethylamine is carried out with at least 7 molar equivalents of dimethylamine relative to the phenothiazine.16. The process as claimed in claim 12 , wherein claim 12 , in step a) claim 12 , the solvent is chosen from: an aromatic solvent or acetonitrile claim 12 , or mixtures thereof.17. The process as claimed in claim 16 , wherein in step a) claim 16 , the solvent is chosen from: toluene or acetonitrile claim 16 , or mixtures thereof.18. The process as claimed in claim 12 , wherein claim 12 , in step b) claim 12 , the dimethylamine is introduced into the reaction medium in the form of a solution in water.19. The process as claimed in claim 12 , wherein a precipitate forms at the outcome of the treatment of step b) claim 12 , said precipitate being recovered by filtration.20. The process as claimed in ...

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Номер записи: 60
18-01-2018 дата публикации

FUNGICIDAL ACTIVE COMPOUND COMBINATIONS

Номер: US20180014541A1
Автор: DUTZMANN Stefan, HEINEMANN Ulrich, KERZ-MOHLENDICK Friderich, SUTY-HEINZE Anne
Принадлежит: ARYSTA LIFESCIENCE CORPORATION

The invention relates to active compound combinations comprising firstly the known fluoxastrobin and secondly further known fungicidal active compounds, which combinations are highly suitable for controlling unwanted phytopathogenic fungi. 18-. (canceled)9. A fungicidally active compound combination comprising fluoxastrobin and at least one fungicidally active carbamate compound.101. The combination of claim wherein the carbamate is one or more of propamocarb , propamocarb hydrochloride , and propamocarb-fosetyl.112. The combination of claim wherein the carbamate is propamocarb.121. The combination of claim wherein the ratio of fluoxastrobin to the at least one active carbamate compound is 1:1 to 1:150.134. The combination of claim wherein the ratio of fluoxastrobin to the at least one active carbamate compound is 1:1 to 1:100. This is a continuation application of U.S. patent application Ser. No. 14/178,644, filed Feb. 12, 2014, which is a continuation application of U.S. patent application Ser. No. 11/576,756, filed Jun. 5, 2008, which is a U.S. National Stage of International Patent Application No. PCT/EP05/10919, filed Oct. 11, 2005, which claims priority to German Application No. 10 2004 049 761.3, filed Oct. 12, 2004. The disclosures of these documents, including the specifications, and drawings, and claims are incorporated herein by reference in their entireties.The invention relates to active compound combinations comprising firstly the known fluoxastrobin and secondly further known fungicidal active compounds, which combinations are highly suitable for controlling unwanted phytopathogenic fungi.It is already known, that the compound of the formula (I)(fluoxastrobin)has fungicidal properties (WO 97/271189).Furthermore, it is already known that numerous triazole derivatives, aniline derivatives, dicarboximides and other heterocycles can be employed for controlling fungi (cf. EP-A 0 040 345, DE-A 22 01 063, DE-A 23 24 010, Pesticide Manual, 9th Edition (1991), ...

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Номер записи: 61
16-01-2020 дата публикации

SYNERGISTIC WEED CONTROL FROM APPLICATIONS OF PYRIDINE CARBOXYLIC ACID HERBICIDES AND PHOTOSYSTEM II INHIBITORS

Номер: US20200015481A1
Автор: Bangel Bryston L., Satchivi Norbert M., Schmitzer Paul R.
Принадлежит:

Disclosed herein are herbicidal compositions comprising a herbicidally effective amount of (a) a pyridine carboxylic acid herbicide or an agriculturally acceptable N-oxide, salt, or ester thereof, and (b) a photosystem II inhibitor, or an agriculturally acceptable salt or ester thereof. Also disclosed herein are methods of controlling undesirable vegetation which comprise applying to vegetation or an area adjacent the vegetation or applying to soil or water to prevent the emergence or growth of vegetation (a) a pyridine carboxylic acid herbicide or an agriculturally acceptable N-oxide, salt, or ester thereof, and (b) a photosystem II inhibitor, or an agriculturally acceptable salt or ester thereof, wherein (a) and (b) are each added in an amount sufficient to provide a herbicidal effect. 3. The composition of claim 2 , wherein{'sup': 1', '1′', '1′, 'sub': 1', '8', '7', '10, 'Ris OR, wherein R is hydrogen, C-Calkyl, or C-Carylalkyl;'}{'sup': '2', 'sub': 1', '4', '1', '4', '2', '4', '2', '4', '2', '4', '1', '4', '1', '4', '1', '4', '1', '4, 'Ris halogen, C-Calkyl, C-Chaloalkyl, C-C-alkenyl, C-Chaloalkenyl, C-Calkynyl, C-C-alkoxy, C-Chaloalkoxy, C-Calkylthio, or C-Chaloalkylthio;'}{'sup': 3', '4', '3', '4', '3′', '4′', '3′', '4′, 'sub': 1', '6', '1', '6', '3', '6', '3', '6', '3', '6', '1', '3', '1', '3', '1', '6', '3', '6', '3', '6', '1', '6', '1', '6, 'Rand Rare hydrogen, C-Calkyl, C-Chaloalkyl, C-Calkenyl, C-Chaloalkenyl, C-Calkynyl, formyl, C-Calkylcarbonyl, C-Chaloalkylcarbonyl, or Rand Rtaken together represent ═CR(R), wherein R and R are independently hydrogen, C-Calkyl, C-Calkenyl, C-Calkynyl, C-Calkoxy or C-Calkylamino;'}A is A1, A2, A3, A7, A8, A9, A10, A11, A12, A13, A14, A15, A21, A22, A23, A24, A27, A28, A29, A30, A31, or A32;{'sup': '5', 'sub': 1', '4', '1', '4', '2', '4', '2', '4', '2', '4', '1', '3', '1', '3', '1', '3', '1', '3', '1', '4', '2', '4, 'Ris hydrogen, halogen, C-Calkyl, C-Chaloalkyl, C-Calkenyl, C-Chaloalkenyl, C-Calkynyl, C-Calkoxy, C- ...

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Номер записи: 62
21-01-2016 дата публикации

FLUORINE ATOM-CONTAINING DISULFIDE COMPOUND

Номер: US20160016922A1
Автор: MATSUMURA Tokihiko, MATSUSHITA Yasuaki
Принадлежит: FUJIFILM Corporation

A disulfide compound represented by formula (1):

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Номер записи: 63
21-01-2016 дата публикации

PREPARATION METHOD OF OPTICALLY ACTIVE DIAMINE COMPOUND

Номер: US20160016974A1
Автор: Kaneda Takeshi, Michida Makoto, NAKAMURA Yoshitaka
Принадлежит: Daiichi Sankyo Company, Limited

The problem to be solved is to provide a method for efficiently producing compounds (1) and (1a) that are important intermediate compounds in the production of FXa inhibitors (X) and (X-a). The solutions thereto are a method for producing a compound represented by the formula (8d) using a stereoselective intramolecular cyclization reaction, and a method for producing a compound (1f) or a salt thereof, or a hydrate thereof, which is characterized by desulfonylation of the compound (8d). In each formula, Rrepresents a C1-C6 alkyl group, a benzyl group, etc. 2. The production method according to claim 1 , wherein the desulfonylation is carried out by treating the compound with water and a base.3. The production method according to claim 2 , wherein the base is a pyridine.6. The production method according to claim 1 , wherein Rand Reach represent an ethyl group.8. The production method according to claim 1 , wherein Rrepresents a C1-C6 alkyl group.9. The production method according to claim 1 , wherein Rrepresents a methyl group.12. The production method according to claim 11 , wherein the desulfonylation is carried out by treating the compound with water and a base.13. The production method according to claim 12 , wherein the base is a pyridine.14. The production method according to claim 1 , wherein Ris a di(methyl)amino group.15. The production method according to claim 1 , wherein Ris a tert-butyl group or a benzyl group.16. The production method according to claim 14 , wherein the compound represented by the formula (1d) or a salt thereof claim 14 , or a hydrate thereof is a sulfate of the compound represented by the formula (1d) claim 14 , an oxalate monohydrate of the compound represented by the formula (1d) claim 14 , or an oxalate of the compound represented by the formula (1d).21. The compound according to claim 20 , wherein Rrepresents a C1-C6 alkyl group.22. The compound according to claim 20 , wherein Rrepresents a methyl group.24. The compound according ...

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Номер записи: 64
18-01-2018 дата публикации

Ionic Liquid, Lubricant, and Magnetic Recording Medium

Номер: US20180016510A1
Автор: Hirofumi Kondo, Kouki Hatsuda, KyungSung Yun, Nobuo Tano
Принадлежит: Dexerials Corp

A lubricant, which includes an ionic liquid including a conjugate base and a conjugate acid including 2 or more cations in a molecule of the conjugate acid, wherein the conjugate acid includes a monovalent group including a straight-chain hydrocarbon group having 6 or more carbon atoms, and an acid that is a source of the conjugate base has a pKa in acetonitrile of 10 or less.

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Номер записи: 65
15-01-2015 дата публикации

CYCLOALKANE DERIVATIVES

Номер: US20150018551A1
Автор: Domon Yuki, Kimoto Hiroko, Kobayashi Hiroyuki, SHINOZUKA Tsuyoshi, Suzuki Sayaka, Tanaka Kyosuke
Принадлежит:

Disclosed herein are therapeutic agents and/or preventive agents for pain or therapeutic agents and/or preventive agents for a sodium channel associated disease. The present invention provides compounds represented by the following formula (I) or pharmacologically acceptable salts thereof: 131-. (canceled)33. The method of claim 32 , wherein the removal of the protecting group is conducted by reacting an acid and the compound represented by formula (VI) in a solvent.34. The method of claim 33 , wherein the solvent is selected from the group consisting of an ethers claim 33 , a halogenated hydrocarbon claim 33 , tetrahydrofuran claim 33 , 1 claim 33 ,4-dioxane and dichloromethane.35. The method of claim 33 , further comprising a scavenger.36. The method of claim 35 , wherein the scavenger is selected from the group consisting of trialkylsilane claim 35 , aryl ether claim 35 , triethylsilane and anisole.37. The method of claim 33 , wherein the acid is selected from the group consisting of an organic acid claim 33 , an inorganic acid claim 33 , trichloroacetic acid claim 33 , trifluoroacetic acid claim 33 , acetic acid claim 33 , sulfuric acid and hydrochloric acid.38. The method of claim 32 , wherein the reaction temperature is 0° C. to 200° C.39. The method of claim 32 , wherein the reaction time is from 1 hour to 48 hours.40. The method of claim 32 , wherein the deprotecting of the compound of formula (VI) is in a solvent and in the presence of a palladium catalyst under hydrogen atmosphere.41. The method of claim 40 , wherein the solvent is selected from the group consisting of ethers claim 40 , alcohols claim 40 , tetrahydrofuran claim 40 , methanol and ethanol.42. The method of claim 40 , wherein the catalyst is selected from the group consisting of a zero-valent palladium catalyst claim 40 , a palladium-activated carbon and a palladium hydroxide-activated carbon.43. The method of claim 40 , wherein the reaction temperature is from −20° C. to 120° C.44. The ...

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Номер записи: 66
21-01-2021 дата публикации

BENZOTHIA(DI)AZEPINE COMPOUNDS AND THEIR USE AS BILE ACID MODULATORS

Номер: US20210017141A1
Автор: Gillberg Per-Göran, Kulkarni Santosh S., Mattsson Jan, Starke Ingemar
Принадлежит:

The invention relates to 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases. 1. (canceled)3. The method of claim 2 , wherein Rand Rare each n-butyl.4. The method of claim 2 , wherein Rand Rare each ethyl.5. The method of claim 2 , wherein Ris n-butyl and Ris ethyl.6. The method of claim 2 , wherein Ris selected from the group consisting of hydrogen claim 2 , bromo claim 2 , hydroxy claim 2 , methoxy claim 2 , amino claim 2 , tert-butoxycarbonylamino claim 2 , methylsulfonamido and cyclopropylsulfonamido.7. The method of claim 2 , wherein Ris selected from the group consisting of hydrogen claim 2 , bromo claim 2 , ethyl claim 2 , cyclopropyl claim 2 , methoxy claim 2 , methylthio and dimethylamino.8. The method of claim 2 , wherein Ris selected from the group consisting of hydrogen and fluoro.9. The method of claim 2 , wherein Ris carboxy.11. The method of claim 2 , wherein the a liver disease or disorder is selected from the group consisting of inherited metabolic disorder of the liver; inborn errors of bile acid synthesis; congenital bile duct anomalies; biliary atresia; neonatal hepatitis; neonatal cholestasis; hereditary forms of cholestasis; cerebrotendinous xanthomatosis; a secondary defect of BA synthesis; Zellweger's syndrome; cystic fibrosis-associated liver disease; alpha1-antitrypsin deficiency; Alagilles syndrome (ALGS); Byler syndrome; a primary defect of bile acid (BA) synthesis; progressive familial intrahepatic cholestasis (PFIC); autoimmune hepatitis; primary biliary cirrhosis (PBC); liver fibrosis; non- ...

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Номер записи: 67
24-01-2019 дата публикации

AQUEOUS DISPERSIONS COMPRISING ACLONIFEN AND FLUFENACET

Номер: US20190021311A1
Автор: Deckwer Roland, Krause Jens
Принадлежит:

The present invention relates to formulations in the form of aqueous dispersions comprising aclonifen and flufenacet and a mixture of anionic surfactants from the group of the naphthalenesulphonates or from the group of the condensates of naphthalenesulphonates with formaldehyde, nonionic surfactants from the group of the di- and tri-block-copolymers of alkylene oxides, and a specific mixture of organic and inorganic thickeners, to which further agrochemically active compounds and further customary auxiliaries and additives may optionally be added. 1. Aqueous dispersion , comprisinga) the herbicidally active compounds aclonifen and flufenacet,b) one or more anionic surfactants from the group of the sulphonates, selected from the groups based on naphthalenes, the alkylaryl, the fused naphthalenes and based on lignin,c) one or more nonionic surfactants from the group of the di- and tri-block-copolymers of alkylene oxides,d) an organic thickener based on xanthan gum,e) an inorganic thickener,f) optionally one or more agrochemically active compounds different from component a), g) optionally one or more further customary auxiliaries and additives,andwater;where the components d) and e) are in specific mixing ratios to one another.2. Dispersion according to claim 1 , comprisinga) 20 to 45% aclonifen and 4 to 20% flufenacet, at a total amount of 24 to 65%,b) 0.3 to 3% of one or more anionic surfactants from the group of the sulphonates, selected from the groups based on naphthalenes, the alkylaryl, the fused naphthalenes and based on lignin,c) 2 to 15% of one or more nonionic surfactants from the group of the di- and tri-block-copolymers of alkylene oxides,d) 0.01 to 1% of an organic thickener based on xanthan gum,e) 0.1 to 3% of an inorganic thickener,f) 0 to 50% of one or more agrochemically active compounds different from component a), g) 0 to 20% of one or more further customary auxiliaries and additives,and20 to 70% water;where the components d) and e) are present in ...

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Номер записи: 68
26-01-2017 дата публикации

COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES

Номер: US20170022174A1
Автор: CAM JUDY, CUMMINGS JOEL, ESPOSITO LUKE A., HU QUBAI, HUDSON F. MICHAEL, Lake Thomas, Snow Alan D., YADON MARISA C.
Принадлежит:

Compounds and their pharmaceutically acceptable salts for treatment of tauopathies, such as Alzheimer's disease, Pick's disease, progressive supranuclear palsy, corticobasal degeneration, familial frontotemporal dementia/Parkinsonism linked to chromosome 17, amyotrophic lateral sclerosis/Parkinsonism-dementia complex, argyrophilic grain dementia, dementia pugilistic, diffuse neurofibrillary tangles with calcification, progressive subcortical gliosis and tangle only dementia. 2. A method of disrupting or inhibiting the formation claim 1 , deposition claim 1 , accumulation claim 1 , or persistence of tau fibrils and/or aggregates claim 1 , comprising administering a therapeutically effective amount of the compounds of .3. The method of claim 2 , where the compound administered is in an amount between 0.1 mg/Kg/day and 1000 mg/Kg/day.4. The method of claim 2 , where the compound is administered in an amount between 1 mg/Kg/between 10 mg/Kg/day and 100 mg/Kg/day.5. The method of claim 2 , where amount of compound administered is in an amount between 10 mg/Kg/day and 100 mg/Kg/day.6. A method resulting in neuroprotection from a tauopathy in a mammal comprising the step of administrating a therapeutically effective amount of a compound of .7. The method of where the tauopathy is one selected from; Alzheimer's disease claim 6 , Pick's disease claim 6 , progressive supranuclear palsy claim 6 , corticobasal degeneration claim 6 , familial frontotemporal dementia/Parkinsonism linked to chromosome 17 claim 6 , amyotrophic lateral sclerosis/Parkinsonism-dementia complex claim 6 , argyrophilic grain dementia claim 6 , dementia pugilistic claim 6 , diffuse neurofibrillary tangles with calcification claim 6 , progressive subcortical gliosis and tangle only dementia.8. An article of manufacture claim 1 , comprising packaging material claim 1 , the compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , contained within packaging material claim 1 , which is ...

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Номер записи: 69
17-04-2014 дата публикации

N-(1,2,5-OXADIAZOL-3-YL)-, N-(TETRAZOL-5-YL)- AND N-(TRIAZOL-5-YL)BICYCLOARYLCARBOXAMIDES AND THEIR USE AS HERBICIDES

Номер: US20140106969A1
Автор: AHRENS HARTMUT, Almsick Andreas, Braun Ralf, Dörner-Rieping Simon, GATZWEILER ELMAR, Häuser-Hahn Isolde, Heinemann Ines, Köhn Arnim, ROSINGER CHRISTOPHER HUGH
Принадлежит: Bayer Intellectual Property GmbH

N-(1,2,5-Oxadiazol-3-yl)-, N-(tetrazol-5-yl)- and N-(triazol-5-yl)bicycloarylcarboxamides of the general formula (I) are described as herbicides. 2. An N-(1 claim 1 ,2 claim 1 ,5-oxadiazol-3-yl)- claim 1 , N-(tetrazol-5-yl)- or N-(triazol-5-yl)bicycloarylcarboxamide as claimed in claim 1 , in which{'sup': '1', 'sub': 1', '3', '3', '5', '1', '3', '1', '3', '1', '3, 'Ris (C-C)-alkyl, (C-C)-cycloalkyl, halo-(C-C)-alkyl or (C-C)-alkoxy-(C-C)-alkyl;'}{'sup': '2', 'sub': 1', '3', '3', '5', '1', '3', '1', '3', '1', '3, 'Ris hydrogen, (C-C)-alkyl, (C-C)-cycloalkyl, halo-(C-C)-alkyl, (C-C)-alkoxy, halo-(C-C)-alkoxy, cyano, nitro, methylsulfenyl, methylsulfinyl, methylsulfonyl, acetylamino, methoxycarbonyl, ethoxycarbonyl, halogen, amino, aminocarbonyl, methylaminocarbonyl, dimethylaminocarbonyl or methoxymethyl;'}{'sup': 3', '4, 'sub': 1', '3', '1', '3', '3', '5', '1', '3', '1', '3', '1', '6', '1', '6', '1', '6', '1', '6', '1', '4, 'Rand Rare each independently hydrogen, (C-C)-alkyl, halo-(C-C)-alkyl, (C-C)-cycloalkyl, (C-C)-alkoxy, (C-C)-haloalkoxy, (C-C)-alkylthio, (C-C)-alkylsulfinyl, (C-C)-alkylsulfonyl, (C-C)-alkoxy-(C-C)-alkyl, halogen, nitro or cyano;'}{'sup': '5', 'Ris hydrogen;'}{'sup': 7', '8', '9', '9, 'sub': 1', '3', '1', '3', '3', '5', 'm', '1', '3', '1', '3', '1', '3', '1', '3', '1', '3', '1', '3', '1', '3', '3', '5', '1', '3', '1', '3', '1', '3', '1', '3', '1', '3', '1', '3', '1', '3, 'Rand Rare each independently hydrogen, (C-C)-alkyl, halo-(C-C)-alkyl, (C-C)-cycloalkyl, —OR, —S(O)R, (C-C)-alkylthio, (C-C)-alkylsulfinyl, (C-C)-alkylsulfonyl, (C-C)-alkoxy-(C-C)-alkyl, halogen, nitro, cyano, heteroaryl, heterocyclyl or phenyl, where the three latter radicals are each substituted by at least one u radical selected from the group consisting of halogen, nitro, cyano, (C-C)-alkyl, halo-(C-C)-alkyl, (C-C)-cycloalkyl, (C-C)-alkylthio, (C-C)-alkylsulfinyl, (C-C)-alkylsulfonyl, (C-C)-alkoxy, halo-(C-C)-alkoxy and (C-C)-alkoxy-(C-C)-alkyl,'}or{'sup': 7', '8', '1', '2', ...

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Номер записи: 70
17-04-2014 дата публикации

NOVEL PROSTAMIDES FOR THE TREATMENT OF GLAUCOMA AND RELATED DISEASES

Номер: US20140107124A1
Автор: Burk Robert M., Woodward David F.
Принадлежит: ALLERGAN, INC.

Disclosed herein are compositions comprising an amide related to a prostaglandin and a biogenic amine. Other aspects relate to certain chemical compounds, pharmaceutical compositions, and methods of treating glaucoma. 1. A composition comprising an amide related toa. a prostaglandin; andb. a biogenic amine.2. The composition of wherein the prostaglandin is a natural prostaglandin selected from the group consisting of prostaglandin E claim 1 , prostaglandin E claim 1 , prostaglandin F claim 1 , prostaglandin F claim 1 , and prostaglandin D claim 1 , or is an analog thereof.3. The composition of wherein the biogenic amine is selected from the group consisting of cholinomimetics claim 1 , antimuscarinics claim 1 , adrenergics claim 1 , dopaminergics claim 1 , α-adrenoreceptor antagonists claim 1 , β-adrenergic antagonists claim 1 , monoamine oxidase inhibitors claim 1 , histaminergics claim 1 , serotonergics claim 1 , and thyroid drugs.4. The composition of wherein the biogenic amine is selected from the group consisting of tropicamide claim 1 , epinephrine claim 1 , isoprotenenol claim 1 , dopamine claim 1 , phentolamine claim 1 , timolol claim 1 , trancylpromine claim 1 , histamine claim 1 , dimaprit claim 1 , thyroxine claim 1 , and serotonin claim 1 , or is an analog claim 1 , a pharmaceutically acceptable salt claim 1 , or a prodrug thereof.5. The composition of wherein the prostaglandin is prostaglandin F and the amine is dopamine.6. The composition of wherein the prostaglandin is prostaglandin F and the amine is diacetyl dopamine.7. The composition of wherein the prostaglandin is prostaglandin F and the amine is serotonin.8. A compound comprising an amide related to a prostaglandin and a biogenic amine claim 1 , wherein said compound is not naturally occurring.9. The compound of wherein said biogenic amine is selected from the group consisting of cholinomimetics claim 8 , antimuscarinics claim 8 , adrenergics claim 8 , dopaminergics claim 8 , α-adrenoreceptor ...

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Номер записи: 71
17-04-2014 дата публикации

Processes and intermediates for making sweet taste enhancers

Номер: US20140107370A1
Автор: Catherine Tachdjian, Daniel Levin, Donald S. Karanewsky, Peter Leeming, QING Chen, Tayyab Rashid, Xiao-Qing Tang
Принадлежит: Senomyx Inc

The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): wherein X is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heteroalkyl, substituted heteroalkyl, heteroalkenyl, or substituted heteroalkenyl.

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Номер записи: 72
25-01-2018 дата публикации

METHOD OF PRODUCING BENZO[1,2-B:4,5-B']DITHIOPHENE AND BENZOTHIADIAZOLE-BASED MOLECULAR COMPLEXES

Номер: US20180022717A1
Автор: Earmme Taeshik, Pan Hualong, Woody Kathy, Worfolk Brian
Принадлежит: Phillips 66 Company

A method of forming a molecular complex. The method proceeds by reacting 5-chloro-2,1,3-benzothiadiazole with N-bromosuccinimide to produce 4,7-dibromo-5-chlorobenzo[c][1,2,5]thiadiazole. 4,7-dibromo-5-chlorobenzo[c][1,2,5]thiadiazole is then reacted with trimethyl[4-(2-octyldodecyl)thiophen-2-yl]stannane to produce 5-chloro-4,7-bis(4-(2-octyldodecyl)thiophen-2-yl)benzo[c][1,2,5]thiadiazole. 4, 7-bis(5-bromo-4-(2-octyldodecyl)thiophen-2-yl)-5-chlorobenzo[c][1,2,5]thiadiazole is subsequently synthesized from 5-chloro-4,7-bis(4-(2-octyldodecyl)thiophen-2-yl)benzo[c][1,2,5]thiadiazole. 4,7-bis(5-bromo-4-(2-octyldodecyl)thiophen-2-yl)-5-chlorobenzo[c][1,2,5]thiadiazole with tributyl(thiophen-2-yl)stannane is then reacted to produce 4-bromo-5,6-difluoro-7-(thiophen-2-yl)benzo[c][1,2,5]thiadiazole. This is followed by reacting 4,7-dibromo-5-chloro-2,1,3-benzothiadiazole with tributyl(thiophen-2-yl)stannane to produce 4-bromo-5-chloro-7-(thiophen-2-yl)benzo[c][1,2,5]thiadiazole. trimethyl[4-(2-octyldodecyl)thiophen-2-yl]stannane is then reacted with and 4-bromo-5-chloro-7-(thiophen-2-yl)benzo[c][1,2,5]thiadiazole to produce 5-chloro-4-(4-(2-octyldodecyl)thiophen-2-yl)-7-(thiophen-2-yl)benzo[c][1,2,5]thiadiazole. 5-chloro-4-(4-(2-octyldodecyl)thiophen-2-yl)-7-(thiophen-2-yl)benzo[c][1,2,5]thiadiazole is then reacted with N-bromosuccinimide to produce the co-monomer 4-(5-bromo-4-(2-octyldodecyl)thiophen-2-yl)-7-(5-bromothiophen-2-yl)-5-chlorobenzo[c][1,2,5]thiadiazole. A 2. The method of claim 1 , wherein the molecular complex is used as photovoltaic material in one or more photovoltaic devices.3. The method of claim 2 , wherein the one or more photovoltaic devices are polymer solar cell devices or photodetector devices.4. The method of claim 1 , wherein the molecular complex is used as an active layer material in one or more electronic devices.5. The method of claim 4 , wherein the one or more electronic devices are field effect transistors claim 4 , light emitting devices ...

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Номер записи: 73
25-01-2018 дата публикации

UNSYMMETRICAL BENZOTHIADIAZOLE-BASED MOLECULAR COMPLEXES

Номер: US20180022718A1
Автор: Earmme Taeshik, Pan Hualong, Woody Kathy, Worfolk Brian
Принадлежит: Phillips 66 Company

A molecular complex comprising 2. The molecular complex of claim 1 , wherein the molecular complex is part of an oligomer.3. The molecular complex of claim 1 , wherein the molecular complex is part of a polymer with a molecular weight ranging from about 1 claim 1 ,000 to about 100 claim 1 ,000 kDa.5. The molecular complex of claim 1 , wherein the molecular complex is used as photovoltaic material in one or more photovoltaic devices.6. The molecular complex of claim 5 , wherein the one or more photovoltaic devices are polymer solar cell devices or photodetector devices.7. The molecular complex of claim 1 , wherein the molecular complex is used as an active layer material in one or more electronic devices.8. The molecular complex of claim 4 , wherein the one or more electronic devices are field effect transistors claim 4 , light emitting devices and sensors claim 4 , electrochromic devices and capacitors.9. The molecular complex of claim 1 , wherein when used as a photovoltaic polymer produces a power conversion efficiency greater than 7.0%.10. The molecular complex of claim 1 , wherein when used as a photovoltaic polymer produces a fill factor greater than 69%.11. The molecular complex of claim 1 , wherein R1 and R1′ are not identical.12. The molecular complex of claim 1 , wherein R2 and R2′ are not identical.13. The molecular complex of claim 1 , wherein both R1 and R1′ are not identical and R2 and R2′ are not identical. This application is a non-provisional application which claims the benefit of and priority to U.S. Provisional Application Ser. No. 62/364,088 filed Jul. 19, 2016, entitled “Unsymmetrical Benzothiadiazole-Based Molecular Complexes,” which is hereby incorporated by reference in its entirety.None.This invention relates to unsymmetrically substituted benzothiadiazole-based molecular complexes.Solar energy using photovoltaic effect requires active semiconducting materials to convert light into electricity. Currently, solar cells based on silicon are the ...

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Номер записи: 74
22-01-2015 дата публикации

COMPOUNDS AND COMPOSITIONS FOR USE IN AUGMENTATION OF GLUCOSE

Номер: US20150025094A1
Автор: Cerasi Erol, GRUZMAN Arie Lev, Meltzer-Mats Ella, Sasson Shlomo
Принадлежит:

The present invention is directed to compounds such as: formula wherein linker is independently selected from the group consisting of —S—, —S—S—, —S—(CH2)n—, —NH—, —NH—(CH2)n—, —O—, —S02-, arylene, heteroarylene; R1 is selected from the group consisting of straight or branched C4-C20 alkyl, straight or branched C4-C20 alkenyl, straight or branched C4-C20 alkynyl, each optionally interrupted with at least one NH, C5-C7 saturated cycloalkyl or heteroalkyl ring, C5-C12 aromatic or heteroaromatic ring, each optionally substituted with at least one group selected from —COOH, —NH2, C1-C8 alkoxy, C1-C5 amidyle, C1-C5 carboxyl, halogen; and R2 is independently selected from the group consisting of H, OH, SH, NH2, NO2, halogen, CN, C1-C8 alkoxy, C1-C5 carboxylic acid, straight or branched C1-C8 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2-C12 alkynyl each optionally substituted by at least one substituent selected from the group consisting of C1-C5 alkoxy, C1-C5 carboxylic acid, OH, SH, NH2, halogen; and compositions for use in the treatment of diabetes and related disorders. 132-. (canceled)34. A compound of claim 33 , wherein at least one of Xto Xis O.35. A compound of claim 33 , wherein at least two of Xto Xare O.36. A compound of claim 33 , wherein least one of Xto Xis CHR.37. A compound of claim 33 , wherein Ris aryl or heretroaryl.38. A compound of claim 33 , wherein Y and Z are identical.39. A compound of claim 33 , wherein Y and Z are S.41. A compound of claim 33 , being used as a medicament.42. A composition comprising a compound according to .43. A method of treating or preventing a condition claim 33 , symptom or disease associate with elevated blood glucose levels in a subject in need thereof claim 33 , said method comprising administering to said subject a compound of .44. A method for the treatment or prevention of at least one condition selected from hyperglycemia claim 33 , diabetes claim 33 , altered insulin secretion claim 33 , ...

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Номер записи: 75
10-02-2022 дата публикации

BENZOTHIA(DI)AZEPINE COMPOUNDS AND THEIR USE AS BILE ACID MODULATORS

Номер: US20220041568A1
Автор: Gillberg Per-Göran, Kulkarni Santosh S., Starke Ingemar
Принадлежит:

The invention relates to 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives of formula (1). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases. 2. The method of claim 1 , wherein the disease or disorder is selected from the group consisting of: a cardiovascular disease claim 1 , a disorder of fatty acid metabolism claim 1 , and a glucose utilization disorder.3. The method of claim 2 , wherein the cardiovascular disease claim 2 , disorder of fatty acid metabolism claim 2 , or glucose utilization disorder is selected from the group consisting of: hypercholesterolemia; type 1 or type 2 diabetes mellitus; a complication of diabetes; insulin resistance; hyperglycemia; hyperinsulinemia; elevated blood levels of fatty acids or glycerol; obesity; dyslipidemia; and hyperlipidemia.4. The method of claim 1 , wherein the disease or disorder is a gastrointestinal disease or disorder.5. The method of claim 4 , wherein the gastrointestinal disease or disorder is selected from the group consisting of: constipation; Crohn's disease; primary bile acid malabsorption; irritable bowel syndrome (IBS); inflammatory bowel disease (IBD); ileal inflammation; and reflux disease and complications thereof.6. The method of claim 1 , wherein the disease or disorder is a liver disease or disorder.7. The method of claim 6 , wherein the liver disease or disorder is selected from the group consisting of: inherited metabolic disorder of the liver; an inborn error of bile acid synthesis; a congenital bile duct anomaly; biliary atresia; post-Kasai biliary atresia; post-liver transplantation biliary atresia; neonatal ...

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Номер записи: 76
01-02-2018 дата публикации

METHODS OF MAKING DAZOMET COMPOSITIONS

Номер: US20180027814A1
Автор: Herdman Douglas J., Pope Thomas, Tham Peter
Принадлежит:

Disclosed herein are methods of making solid bodies of dazomet for use in internal remedial treatments of wood and methods of applying such solid bodies to wooden structures and manufacturing such solid bodies. The solid bodies can be easily transported and inserted into treatment holes in utility poles, wooden pilings, and other wooden structures, that can deliver a dose of insecticide and fungicide that combats internal decay in the wood. 1. A method for manufacturing a product essentially free of water for internal remedial treatment of wood , comprising:uniformly blending a composition comprising a mixture of dazomet, a lubricant, and a binder; andcompressing the blended mixture into a solid body without the addition of water or aqueous solutions.2. The method of claim 1 , wherein the solid body has a diameter of about 5 millimeters to about 30 millimeters.3. The method of claim 2 , wherein the solid body has a weight of between 10 grams and 500 grams.4. The method of claim 1 , wherein the mixture is flowable before compressing and comprises between 80% and 96% solid tetrahydro-3 claim 1 ,5-dimethyl-2H-1 claim 1 ,3 claim 1 ,5-thiadiazine-2-thione by weight of the composition; between 0.5% and 5.0% of the lubricant claim 1 , by weight of the composition; and between 1% and 15% of the binder claim 1 , by weight of the composition.5. The method of claim 1 , wherein the solid tetrahydro-3 claim 1 ,5-dimethyl-2H-1 claim 1 ,3 claim 1 ,5-thiadiazine-2-thione is in the form of granules or a powder.6. The method of claim 1 , wherein the lubricant comprises a hydrogenated oil.7. The method of claim 1 , wherein the lubricant comprises a hydrogenated vegetable oil.8. The method of claim 1 , wherein the binder comprises a polysaccharide.9. The method of claim 8 , wherein the polysaccharide comprises a starch.10. The method of claim 9 , wherein the starch comprises a maltodextrin.11. The method of claim 1 , wherein the composition further comprises a first accelerant.12. The ...

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Номер записи: 77
29-01-2015 дата публикации

DAZOMET COMPOSITIONS

Номер: US20150030501A1
Автор: Herdman Douglas J., Pope Thomas, Tham Peter
Принадлежит: Osmose Utilities Services, Inc.

A solid body of dazomet for use in internal remedial treatments of wood and methods of applying such solid bodies to wooden structures and manufacturing such solid bodies. The solid bodies can be easily transported and inserted into treatment holes in utility poles, wooden pilings, and other wooden structures, delivering a precise, accurate dose of insecticide and fungicide that combats internal decay in the wood. 1. A composition comprising a flowable mixture of between 90 and 96% solid tetrahydro-3 ,5-dimethyl-2H-1 ,3 ,5-thiadiazine-2-thione , between 0.5 and 5.0% of a saturated oil and between 1 and 5% of a polysaccharide.2. The composition of claim 1 , wherein the solid tetrahydro-3 claim 1 ,5-dimethyl-2H-1 claim 1 ,3 claim 1 ,5-thiadiazine-2-thione is in the form of granules or a powder.3. The composition of claim 1 , wherein the saturated oil is a hydrogenated oil.4. The composition of claim 3 , wherein the saturated oil is a hydrogenated vegetable oil.5. The composition of claim 1 , wherein the polysaccharide is a starch.6. The composition of claim 5 , wherein the starch is a maltodextrin.7. A product for internal remedial treatment of wood comprising the composition of compressed into a solid body.8. The product of claim 7 , wherein the solid body is compressed into a form selected from the group consisting of a rod claim 7 , tablet claim 7 , pellet and a stick.9. The product of claim 7 , wherein the solid body is a rod.10. The product of claim 8 , wherein the rod has a diameter of about 5 millimeters to about 30 millimeters claim 8 , a length of about 100 millimeters to about 350 millimeters.11. The product of claim 8 , wherein the rod has a weight of between 10 and 500 grams.12. The product of claim 7 , further comprising an accelerant.13. The product of claim 12 , wherein the accelerant is selected from the group consisting of copper naphthenate claim 12 , copper sulfate claim 12 , copper carbonate claim 12 , basic copper carbonate claim 12 , copper ...

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Номер записи: 78
17-02-2022 дата публикации

SYNERGISTIC INSECTICIDAL COMBINATIONS

Номер: US20220046919A1
Автор: Lokhande Sanjay Pradnya, Sawant Gopal Govind, Srivastava Ramprakash Krishna, Uppara Veera Parasu
Принадлежит:

The present invention relates to a synergistic insecticidal combination. In particular, the present invention provides an insecticidal combination comprising aversive agent and at least one insecticide which is useful against harmful pests in plants. The present invention also provides method of controlling harmful pests in plants using said composition. 1. An insecticidal combination comprising aversive agent and at least one insecticide.2. The combination as claimed in claim 1 , wherein said aversive agent is denatonium compound selected from the group consisting of denatonium chloride claim 1 , denatonium citrate claim 1 , denatonium saccharide claim 1 , denatonium carbonate claim 1 , denatonium acetate claim 1 , denatonium benzoate claim 1 , denatonium benzoate monohydrate claim 1 , and mixtures thereof.3. The combination as claimed in claim 1 , wherein said aversive agent is denatonium benzoate.4. The combination as claimed in claim 1 , where said insecticide is selected from the group consisting of chordotonal organ modulators claim 1 , nicotinic acetylcholine receptor (nAChR) competitive modulators claim 1 , acetylcholinesterase (AChE) inhibitors claim 1 , GABA-gated chloride channel blockers claim 1 , sodium channel modulators claim 1 , nicotinic acetylcholine receptor (nAChR) allosteric modulators—Site I claim 1 , glutamate-gated chloride channel (GluCl) allosteric modulators claim 1 , juvenile hormone mimics claim 1 , miscellaneous nonspecific (multi-site) inhibitors claim 1 , chordotonal organ TRPV channel modulators claim 1 , mite growth inhibitors affecting CHS1 claim 1 , microbial disruptors of insect midgut membranes claim 1 , inhibitors of mitochondrial ATP synthase claim 1 , uncouplers of oxidative phosphorylation via disruption of the proton gradient claim 1 , nicotinic acetylcholine receptor (nAChR) channel blockers claim 1 , inhibitors of chitin biosynthesis affecting CHS1 claim 1 , inhibitors of chitin biosynthesis type 1 claim 1 , moulting ...

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Номер записи: 79
02-02-2017 дата публикации

CYCLOPROPANAMINE COMPOUND AND USE THEREOF

Номер: US20170029417A1
Автор: DAINI Masaki, Hattori Yasushi, Ito Mitsuhiro, KAKU Tomohiro, KOJIMA Takuto, MATSUMOTO Shigemitsu, Morimoto Shinji, TOYOFUKU Masashi
Принадлежит:

The present invention provides a compound having a lysine-specific demethylase-1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, developmental disorders, particularly diseases having intellectual disability (e.g., autistic spectrum disorders, Rett syndrome, Down's syndrome, Kabuki syndrome, fragile X syndrome, Kleefstra syndrome, neurofibromatosis type 1, Noonan syndrome, tuberous sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, spinocerebellar degeneration (e.g., dentatorubural pallidoluysian atrophy) and Huntington's disease), epilepsy (e.g., Dravet syndrome) or drug dependence, and the like. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof. 2. The compound according to claim 1 , wherein A is(1) an optionally substituted heterocyclic group, or{'sub': '3-10', '(2) an optionally substituted Ccycloalkyl group, or a salt thereof.'}3. The compound according to claim 1 , wherein B is a ring selected from(1) a 5- or 6-membered aromatic heterocycle, and(2) a benzene ring fused with an optionally substituted 5- or 6-membered ring,wherein the ring represented by B is optionally substituted, and binds, via two adjacent carbon atoms with one atom in between, to a group represented by the formula (II), and a group represented by the formula (III),or a salt thereof.5. The compound according to claim 1 , wherein R claim 1 , Rand Rare each independently a hydrogen atom or an optionally substituted Calkyl group claim 1 ,or a salt thereof.6. The compound according to claim 1 , wherein Ris(1) a hydrogen atom,{'sub': '1-6', '(2) an optionally substituted Calkyl group,'}{'sub': '3-10', '(3) an optionally substituted Ccycloalkyl group, or'}(4) an optionally substituted heterocyclic group,or a salt thereof.8. The compound according to claim 1 , wherein A is{'sub': '1-6', '(1) a piperidinyl group, an isoxazolyl group, a ...

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Номер записи: 80
04-02-2016 дата публикации

COMPOUNDS FOR THE TREATMENT OF TUBERCULOSIS

Номер: US20160031870A1
Автор: Dandapani Sivaraman, Grant Sarah, Hung Deborah, Kawate Tomohiko, Lewis Timothy A., Munoz Benito, Nag Partha
Принадлежит:

Disclosed are compounds that can be used for treating tuberculosis. 4. The pharmaceutical composition of comprising a compound of Formula I or a pharmaceutically acceptable salt claim 1 , ester or prodrug thereof claim 1 , wherein A claim 1 , is O.58-. (canceled)1315-. (canceled)16. The pharmaceutical composition of claim 12 , or a pharmaceutically acceptable salt claim 12 , ester or prodrug thereof wherein Ris halo and Ris H claim 12 , methyl claim 12 , ethyl claim 12 , or propyl claim 12 , CF claim 12 , C-Calkoxy claim 12 , OH claim 12 , —O(CH)C(═O)O(CH)CH claim 12 , —O(CH)C(═O)N(H)(CH)O(CH)N claim 12 , or —O(CH)C≡CH.1719-. (canceled)21. (canceled)24. (canceled)2645-. (canceled)48. (canceled)49. A method of treating tuberculosis comprising administering to a subject a pharmaceutical composition of or a pharmaceutically acceptable salt claim 1 , ester or prodrug thereof.51. A method of treating replicating tuberculosis comprising administering to a subject a pharmaceutical composition of claim 1 , or a pharmaceutically acceptable salt claim 1 , ester or prodrug thereof.5355-. (canceled) This application claims priority to U.S. Provisional Application No. 61/779,051, which is hereby incorporated by reference in its entirety.This invention was made with government support under Grant No. 1R03MH087444, awarded by the National Institutes of Health, and under Grant No. 1K08A1085033, awarded by the National Institutes of Health. The U.S. Government may therefore have certain rights in the invention.The present invention is directed, in part, to compounds or pharmaceutically acceptable salts thereof, for treating tuberculosis.The problem of tuberculosis continues to take a tremendous toll on global health, accounting for almost 2 million deaths per year, despite the discovery of antitubercular chemotherapy more than half a century ago. In fact, the crisis is growing due to the alarming increase in multi-drug resistant, and even totally-drug resistant strains, coupled with ...

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Номер записи: 81
02-02-2017 дата публикации

PLANTS HAVING INCREASED TOLERANCE TO HERBICIDES

Номер: US20170029840A1
Автор: Hutzler Johannes, Kraus Helmut, Lerchl Jens, Mietzner Thomas, PARRA RAPADO Liliana, Pasternak Maciej, Paulik Jill Marie, Tresch Stefan
Принадлежит: BASF SE

The present invention refers to a method for controlling undesired vegetation at a plant cultivation site, the method comprising the steps of: providing, at said site, a plant that comprises at least one nucleic acid comprising a nucleotide sequence encoding a wild-type hydroxyphenyl pyruvate dioxygenase or a mutated hydroxyphenyl pyruvate dioxygenase (mut-HPPD) which is resistant or tolerant to a N-heterocyclyl-arylcarboxamide and/or a nucleotide sequence encoding a wild-type homogentisate solanesyl transferase or a mutated homogentisate solanesyl transferase (mut-HST) which is resistant or tolerant to a N-heterocyclyl-arylcarboxamide, and applying to said site an effective amount of said herbicide. The invention further refers to a method of identifying a nucleotide sequence encoding a mut-HPPD which is resistant or tolerant to a N-heterocyclyl-arylcarboxamide, as well as transgenic plants having increased resistance or tolerance to a N-heterocyclyl-arylcarboxamide as compared to a wild-type variety of the plant cell. 1. A method for controlling undesired vegetation at a plant cultivation site , the method comprising the steps of: (i) a nucleotide sequence encoding a wild-type hydroxyphenyl pyruvate dioxygenase or a mutated hydroxyphenyl pyruvate dioxygenase (mut-HPPD) which is resistant or tolerant to a N-heterocyclyl-arylcarboxamide and/or', '(ii) a nucleotide sequence encoding a wild-type homogentisate solanesyl transferase or a mutated homogentisate solanesyl transferase (mut-HST) which is resistant or tolerant to a N-heterocyclyl-arylcarboxamide, 'a) providing, at said site, a plant that comprises at least one nucleic acid comprising'}b) applying to said site an effective amount of said herbicide. the amino acid corresponding to or at position 236 is other than alanine;', 'the amino acid corresponding to or at position 411 is other than glutamic acid;', 'the amino acid corresponding to or at position 320 is other than leucine;', 'the amino acid corresponding ...

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Номер записи: 82
17-02-2022 дата публикации

SALTS OF POTASSIUM ATP CHANNEL OPENERS AND USES THEREOF

Номер: US20220047605A1
Автор: Cowen Neil M., Yamout Khaled A.
Принадлежит:

Provided are immediate or prolonged administration of certain salts of Kchannel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving Kchannels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals. 1129.-. (canceled)130. A method of treatment of a subject suffering from or at risk for Alzheimer's disease , said method comprising administering to said subject a therapeutically effective amount of a pharmaceutical formulation comprising a Kchannel opener.131. A kit comprising instructions and a crystalline form B of 7-chloro-3-methyl-2H-1 ,2 ,4-benzothiadiazine dioxide:2-hydroxy-N ,N ,N-trimethyl ethanaminium (1:1) salt having characteristic peaks in a XRPD pattern substantially as shown in .132. The kit of claim 131 , wherein the crystalline form B has characteristic infrared absorbances at 3256 claim 131 , 2174 claim 131 , 2890 claim 131 , 1605 claim 131 , 1463 claim 131 , and 1235 cm.133. The kit of claim 131 , wherein the characteristic peaks comprise two-theta peaks (Cu Kα claim 131 , 40 kV claim 131 , 40 mA) at approximately 10.3 claim 131 , 18.3 claim 131 , 20.6 claim 131 , and 26.3 degrees.134. The kit of claim 131 , wherein the characteristic peaks comprise two-theta peaks (Cu Kα claim 131 , 40 kV claim 131 , 40 mA) at approximately 8.9 claim 131 , 12.0 claim 131 , 24.1 claim 131 , 24.5 claim 131 , 27.1 claim 131 , and 28.9 degrees.135. The kit of claim 131 , wherein the crystalline form B has an NMR spectrum substantially as shown in .136. The kit of claim 135 , wherein the crystalline form B has characteristic chemical shifts in an NMR spectrum (DMSO-d6 ...

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Номер записи: 83
30-01-2020 дата публикации

BIODEGRADABLE HYDROGEL TO DELIVER AQUEOUS BAIT TO CONTROL PEST ANTS

Номер: US20200029555A1
Автор: CHOE Dong-Hwan, HODDLE Mark, MULCHANDANI Ashok, Rust Michael, Tay Jia-Wei
Принадлежит:

A biodegradable hydrogel is disclosed for delivering aqueous bait to control pest ants. The biodegradable hydrogel includes a natural polymer of alginate cross-linked with calcium ions. A method of forming a biodegradable hydrogel is disclosed for delivering aqueous bait to control pest ants, the method includes ionotropically cross-linking sodium alginate with calcium ions. 1. A biodegradable hydrogel for delivering aqueous bait to control pest ants , the biodegradable hydrogel comprising:a natural polymer of alginate cross-linked with calcium ions.2. The biodegradable hydrogel of claim 1 , wherein the natural polymer of alginate is a polysaccharide extracted from seaweeds or algae.3. The biodegradable hydrogel of claim 1 , comprising:an active ingredient encapsulated within the biodegradable hydrogel.4. The biodegradable hydrogel of claim 3 , wherein the active ingredient is thiamethoxam.5. The biodegradable hydrogel of claim 1 , wherein biodegradable hydrogel are formed as spherical beads.6. The biodegradable hydrogel of claim 5 , wherein the hydrogel beads are submerged in a sucrose solution with an active ingredient.7. A method of forming a biodegradable hydrogel for delivering aqueous bait to control pest ants claim 5 , the method comprising:ionotropically cross-linking sodium alginate with calcium ions.8. The method of claim 7 , wherein the sodium alginate is a polysaccharide extracted from seaweeds or algae.9. The method of claim 7 , comprising:encapsulating an active ingredient within the biodegradable hydrogel.10. The method of claim 7 , wherein the active ingredient is thiamethoxam.11. The method of claim 7 , comprising:forming the biodegradable hydrogel as spherical beads.12. The method of claim 7 , comprising:the sodium alginate (Na-Alg) having a concentration of 1% to 2%;{'sub': '2', 'the calcium ions are calcium chloride (CaCl) having a concentration of 0.5% to 2%; and'}crosslinking the sodium alginate and the calcium ions for between 5 minutes to 30 ...

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Номер записи: 84
30-01-2020 дата публикации

COMPOSITIONS COMPRISING RECOMBINANT BACILLUS CELLS AND AN INSECTICIDE

Номер: US20200029573A1
Автор: Riggs Jennifer
Принадлежит:

The present invention relates to a composition comprising a) recombinant exosporium-producing cells that express a fusion protein comprising: (i) at least one plant growth stimulating protein or peptide and (ii) a targeting sequence that localizes the fusion protein to the exosporium of the cells; and b) tioxazafen in a synergistically effective amount. Furthermore, the present invention relates to the use of this composition as well as a method for enhancing plant growth, promoting plant health, and/or reducing overall damage of plants and plant parts. 1. A composition comprising:{'i': 'Bacillus', 'claim-text': (i) at least one protein or peptide selected from the group consisting of a plant growth stimulating protein or peptide and a protein or peptide with insecticidal activity; and', '(ii) a targeting sequence, exosporium protein, or exosporium protein fragment; and, 'a) recombinant exosporium-producing cells that express a fusion protein comprisingb) tioxazafen in a synergistically effective amount.2. The composition of claim 1 , wherein the at least one protein or peptide is a plant growth stimulating protein or peptide selected from the group consisting of an enzyme involved in the production or activation of a plant growth stimulating compound and an enzyme that degrades or modifies a bacterial claim 1 , fungal claim 1 , or plant nutrient source.3BacillusBacillus cereus. The composition of claim 1 , wherein the exosporium-producing cells are cells of a family member.4Bacillus cereusBacillus anthracis, Bacillus cereus, Bacillus thuringiensis, Bacillus mycoides, Bacillus pseudomycoides, Bacillus samanii, Bacillus gaemokensis, Bacillus weihenstephensis, Bacillus toyoiensis. The composition according of claim 3 , wherein the family member is selected from the group consisting of and combinations thereof.5. The composition according to claim 1 , wherein the targeting sequence or exosporium protein comprises:an amino acid sequence having at least about 43% ...

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Номер записи: 85
31-01-2019 дата публикации

CFTR REGULATORS AND METHODS OF USE THEREOF

Номер: US20190031630A1
Автор: Cil Onur, Levin Marc H., Verkman Alan S.
Принадлежит:

Provided herein are compounds that activate CFTR and methods for treating constipation, dry eye disorders or other diseases and disorders. 26-. (canceled)814-. (canceled)1619-. (canceled)2123-. (canceled)25. (canceled)27. (canceled)29. (canceled)3144-. (canceled)4648-. (canceled) This application claims the benefit of U.S. Provisional Application No. 62/387,591, filed Dec. 24, 2015, the contents of which is incorporated herein in its entirety and for all purposes.This invention was made with the government support under Grant Nos. TR000004, EY023981, EY013574, EB000415, DK035124, DK072517 and DK101373, awarded by the National Institutes of Health. The government has certain rights in the invention.Constipation is a common clinical complaint in adults and children that negatively impacts quality of life. The prevalence of chronic constipation has been estimated to be 15% in the U.S. population, with health-care costs estimated at approximately 7 billion dollars annually, with in excess of 500 million dollars spent on laxatives. The mainstay of constipation therapy includes laxatives and many of them are available over the counter (soluble fiber, polyethylene glycol, probiotics, etc.). There are two FDA-approved chloride channel activators, lubiprostone and linaclotide, for treatment of constipation, but clinical trials showed variable and unimpressive efficacy of both drugs. Despite the wide range of therapeutic options, there is a continued need for safe and effective drugs to treat constipation.Dry eye is a heterogeneous tear film disorder that results in eye discomfort, visual disturbance, and ocular surface pathology, and remains an unmet need in ocular disease with limited effective therapeutic options available. Dry eye is a major public health concern in an aging population, affecting up to one-third of the global population, including 5 million Americans aged 50 and over. Over-the-counter artificial tears and implantable punctal plugs are frequently used for ...

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Номер записи: 86
01-05-2014 дата публикации

Method for Producing Lanthionine Derivative

Номер: US20140120233A1
Автор: KATO Yumiko, Mizukoshi Toshimi, Sato Seiichi, Suzuki Yumiko
Принадлежит: AJINOMOTO CO., INC.

The present invention relates to a method for producing a novel lanthionine derivative having a CaSR agonist activity, an intermediate compound of the lanthionine derivative, and use of the intermediate compound for production of a CaSR agonist, a kokumi-imparting agent, and a food and/or beverage ingredient. 2. The production method according to claim 1 , wherein{'sub': 4', '7, 'X is SR, and Y is OR.'}3. The production method according to claim 1 , wherein{'sub': 5', '6, 'X is OR, and Y is SR.'}4. The production method according to claim 1 , wherein{'sub': 4', '6, 'X is SR, and Y is SR.'}5. The production method according to claim 1 , wherein X and Y claim 1 , which may be the same or different claim 1 , each represents SH claim 1 , O—POH claim 1 , or O—SOH claim 1 , provided that at least one of X and Y represents SH.6. The production method according to claim 1 , wherein{'sub': 4', '6', '4', '6, 'X is SR, Y is SR, and either Rand Ris a hydrogen atom.'}7. The production method according to claim 1 , wherein{'sub': 4', '6', '4', '6, 'X is SR, Y is SR, and Rand Rare both hydrogen atoms.'}12. The compound according to or a chemically acceptable salt thereof claim 11 , which is γ-Glu-Ser-Cys.14. A method of producing a CaSR agonist comprising mixing the compound according to or a chemically acceptable salt thereof with a pharmaceutically acceptable excipient.15. A method of producing a kokumi-imparting agent comprising mixing the compound according to or a chemically acceptable salt thereof claim 11 , with an edible food additive.16. A method of producing a food and/or beverage ingredient comprising mixing the compound according to or a chemically acceptable salt thereof claim 11 , with an edible food additive. This application is a Continuation of, and claims priority under 35 U.S.C. §120 to, International Application No. PCT/JP2012/066534, filed Jun. 28, 2012, and claims priority therethrough under 35 U.S.C. §119 to Japanese Patent Application No. 2011-142890, filed ...

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Номер записи: 87
05-02-2015 дата публикации

THIADIAZOLIDINEDIONES AS GSK-3 INHIBITORS

Номер: US20150038538A1
Автор: DE CRISTOBAL BLANCO Javier, DOMÍNGUEZ CORREA Juan Manuel, Fuertes Huerta Ana, HERRERO SANTOS Susana, López Ogalla Javier, MARTÍNEZ MONTERO Olga, Medina Padilla Miguel, Palomo Nicolau Francisco, PÉREZ DE LA CRUZ MORENO María Ángeles, RODRÍGUEZ SALGUERO Beatriz, Sánchez-Quesada Jorge
Принадлежит: ASD THERAPEUTICS PARTNERS LLC

The present invention relates to new thiadiazolidinediones of formula (I), or any pharmaceutically acceptable salt, solvate or prodrug thereof, and its use in the treatment of a disease in which glycogen synthase kinase 3 (GSK-3) is involved, particularly neurodegenerative diseases, inflammatory and autoimmune diseases and cardiovascular disorders. Additionally, there is provided a process for preparing such compounds, as well as pharmaceutical compositions comprising them. 2. The compound according to claim 1 , wherein the aryl radical in the substituent Ris phenyl.3. The compound according to claim 1 , wherein m is 1.4. The compound according to claim 1 , wherein Rand Rare hydrogen.5. The compound according to claim 1 , wherein n is 0.6. The compound according to claim 1 , wherein n is 1 and Ris —CO(O)R″ claim 1 , wherein R″ is an alkyl group.7. The compound according to claim 1 , wherein Ris ethyl or methyl claim 1 , optionally substituted with hydroxyl claim 1 , heterocyclyl or —C(O)OR′ claim 1 , wherein R′ is an alkyl group.10. A process according to claim 9 , where the steps 1 and 2 are performed in the absence of any solvent.11. A pharmaceutical composition comprising a compound of Formula (I) as defined in claim 1 , or a salt claim 1 , solvate or prodrug thereof claim 1 , and at least one pharmaceutically acceptable carrier claim 1 , adjuvant claim 1 , and/or vehicle.12. (canceled)13. A method for the therapeutic treatment of a cognitive claim 1 , neurodegenerative or neurological disease or condition claim 1 , said method comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound of Formula (I) as defined in claim 1 , or a salt claim 1 , solvate or prodrug thereof.14. A method for the therapeutic treatment of a disease or condition selected from diabetes claim 1 , inflammatory and autoimmune diseases claim 1 , cardiovascular disorders claim 1 , and pathologies selected from metabolic syndrome X claim 1 , ...

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Номер записи: 88
11-02-2016 дата публикации

TRPV-1 RECEPTOR ANTAGONIST COMPOUND DERIVED FROM 1,3,4-THIADIAZOLE ALKYLAMIDES AND CHALCONES

Номер: US20160039778A1
Автор: BRAUCHI ULLOA Sebastián, LESPAY REBOLLEDO Carolyne, ZÁRRAGA OLAVARRIA Miguel
Принадлежит:

This technology encompasses compounds derived from 1,3,4-thiadiazole alkylamides and chalcone, which inhibit the activation of the TRPV-1 receptor using capsaicin and temperature. Also disclosed is the use of these compounds in the treatment of diseases with TRPV-1 overexpression, such as chronic pain. 1. Compounds derived from 1 ,3 ,4-thiadiazol alkylamides wherein they inhibit TRPV-1 receptor activation.2. Compounds derived from 1 claim 1 ,3 claim 1 ,4-thiadiazol alkylamides claim 1 , according to claim 1 , wherein they inhibit the capsaicin and temperature activation of the TRPV-1 receptor.3. Compounds derived from 1 claim 1 ,3 claim 1 ,4-thiadiazol alkylamides claim 1 , according to claim 1 , wherein their R structure is a saturated alkyl chain defined by saturated linear chains of 6 to 8 carbons where X is defined as a H atom or an iodine atom.4. Compounds derived from 1 claim 1 ,3 claim 1 ,4-thiadiazol alkylamides claim 1 , according to claim 1 , wherein they are obtained through O-acylation reaction claim 1 , amine condensation claim 1 , oxidative cyclization of thiosemicarbazone claim 1 , N-acylation reaction and alkaline hydrolysis.5. Compounds derived from 1 claim 1 ,3 claim 1 ,4-thiadiazol alkylamides claim 1 , according to claim 1 , wherein they correspond specifically to the following compounds:a) N-[5-(4-hydroxy-5-methoxy-3-iodophenyl)-1,3,4-thiadiazole-2-yl]nonamide,b) N-[5-(4-hydroxy-3-methoxyphenyl)-1,3,4-thiadiazole-2-yl]-nonamide,c) N-[5-(4-hydroxy-5-methoxy-3-iodophenyl)-1,3,4-thiadiazole-2-yl]-octanamide,d) N-[5-(4-hydroxy-3-methoxyphenyl)-1,3,4-thiadiazole-2-yl]-octanamide,e) N-[5-(4-hydroxy-5-methoxy-3-iodophenyl)-1,3,4-thiadiazole-2-yl]-heptanamide,f) N-[5-(4-hydroxy-3-methoxyphenyl)-1,3,4-thiadiazole-2-yl]-heptanamide,g) N-[5-(4-hidroxy-5-methoxy-3-iodophenyl)-1,3,4-thiadiazole-2-yl]-hexanamide, andh) N-[5-(4-hydroxy-3-methoxyphenyl)-1,3,4-thiadiazole-2-yl]-hexanamide.6. Compounds derived from chalcones claim 1 , wherein they inhibit the ...

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Номер записи: 89
09-02-2017 дата публикации

Iminothiadiazepane Dioxide Compounds as BACE Inhibitors, Compositions, and Their Use

Номер: US20170037056A1
Автор: Cumming Jared N., Dai Xing, Liu Hong, Palani Anandan, Scott Jack D.
Принадлежит: Merck Sharp & Dohme Corp.

In its many embodiments, the present invention provides certain iminothiadiazepane dioxide compounds, including compounds Formula (I): 2. A compound of claim 1 , or a tautomer thereof claim 1 , or a pharmaceutically acceptable salt of said compound or said tautomer claim 1 , wherein:{'sup': '4', 'sub': '2', 'Ris selected from the group consisting of methyl and —CHF; and'}{'sup': 'N', 'Ris selected from the group consisting of H and methyl.'}3. A compound of claim 2 , or a tautomer thereof claim 2 , or a pharmaceutically acceptable salt of said compound or said tautomer claim 2 , wherein:{'sup': '1A', 'sub': 2', '2', '3, 'Ris selected from the group consisting of H, fluorine, methyl —CHF, —CHF, and —CF; and'}{'sup': '1B', 'sub': 3', '2', '2', '2', '3', '2', '3', '2', '3', '2', '3', '2, 'Ris selected from the group consisting of H, fluoro, methyl, —CF, —CHF, —CHF, —CHCF, —CFCH, —CHOCH, and —CHN(CH).'}4. A compound of claim 3 , or a tautomer thereof claim 3 , or a pharmaceutically acceptable salt of said compound or said tautomer claim 3 , wherein:ring A is selected from the group consisting of phenyl, pyridazinyl, pyridyl, pyrimidinyl, pyrazinyl, triazinyl, and tetrazinyl;m is 0, 1, 2, or 3, with the proviso that the value of m does not exceed the maximum number of substitutable hydrogen atoms on ring A; and{'sup': 'A', 'sub': 5', '3', '3', '2', '3', '2', '3', '2', '2', '3', '3', '2', '3', '2', '2', '3', '2, 'each R(when present) is independently selected from the group consisting of halogen, oxo, —CN, —SF, —NHCH, —N(CH), —OCH, —OCHCH, —O-cyclopropyl, —O—CH-cyclopropyl, —CHOCH, —S(CH), methyl, ethyl, cyclopropyl, —CH-cyclopropyl, —CF, —CHF, —CHF, —OCF, and —OCHF.'}5. A compound of claim 4 , or a tautomer thereof claim 4 , or a pharmaceutically acceptable salt of said compound or said tautomer claim 4 , wherein:{'sup': 'L', 'sub': 3', '2', '2', '2', '3', '2', '3', '2', '3', '2', '2', '3', '2', '2', '3', '3', '3', '2', '3', '2', '2', '3', '2', '2', '3', '2', '3', '2', ' ...

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Номер записи: 90
08-02-2018 дата публикации

PARTICLES FOR ELECTROPHORETIC DISPLAYS

Номер: US20180037744A1
Автор: Farrand Louise Diane, Goulding Mark John, James Mark, Lutz Christopher, Smith Nathan, Wilson Jonathan Henry
Принадлежит:

This invention relates to polymer particles preferably with surface functionality for charge retention, a process for their preparation, the use of these particles for the preparation of an electrophoretic device, electrophoretic displays comprising such particle, and new polymerisable dyes. 118.-. (canceled)19. A coloured polymer particle for use in electrophoretic devices comprising at least one A-B diblock copolymer comprising a hydrophobic polymer block A and a hydrophilic polymer block B containing a charge or being chargeable , and monomer units of at least one monomer , of at least one polymerisable dye , optionally of at least one charged co-monomer , and optionally of at least one crosslinking co-monomer.20. The coloured polymer particle according to claim 19 , wherein block A is a polymethylmethacrylate block.21. The coloured polymer particle according to claim 19 , wherein block B comprises amino groups or carboxylic acid groups.22. The coloured polymer particle according to claim 19 , wherein block B is charged with 0.2% to 100% permanent charge based on partially or completely quaternised nitrogen groups or partially or completely neutralised acid groups.23. The coloured polymer particle according to claim 19 , wherein a polymerisable dye comprises a chromophore claim 19 , at least one polymerisable group claim 19 , optionally at least one linker group claim 19 , and optionally at least one charged group is used.24. The coloured polymer particle according to claim 19 , wherein the polymer particles have a diameter of 50-1000 nm.25. The coloured polymer particle according to claim 19 , wherein a water-soluble polymerisable dye is used.27. A process for the preparation of coloured polymer particles for use in electrophoretic devices claim 19 , comprisinga) the reaction of at least one monomer, at least one A-B diblock copolymer comprising a hydrophobic polymer block A and a hydrophilic polymer block B containing a charge or being chargeable, at least one ...

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Номер записи: 91
24-02-2022 дата публикации

SYNTHESIS OF 3-METHYL-1,2,4-THIADIAZOLE-5-CARBOHYDRAZIDE OR OF THE METHYL-d3 DEUTERATED FORM THEREOF

Номер: US20220056000A1
Автор: Dutheuil Guillaume, Hoveyda Hamid
Принадлежит:

The present invention relates to a method of synthesis of compound (I), wherein Rrepresents methyl or methyl-d3, thus corresponding to 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or to the methyl-d3 deuterated form thereof. These compounds are useful as key intermediates in the synthesis of pharmaceutical compounds, especially fezolinetant and deuterated fezolinetant. 2. The process according to claim 1 , wherein X represents bromo or iodo.3. The process according to or claim 1 , wherein Rrepresents methyl or ethyl.4. The process according to any one of to claim 1 , wherein the alkoxycarbonylation reaction of step a) is performed in presence of carbon monoxide claim 1 , a palladium catalyst claim 1 , a base and an alcohol solvent claim 1 , and optionally in presence of an organophosphorus ligand.5. The process according to claim 4 , wherein the palladium catalyst is Pd(OAc) claim 4 , the organophosphorus ligand is 4 claim 4 ,5-bis(diphenylphosphino)-9 claim 4 ,9-dimethylxanthene (Xantphos) claim 4 , the base is sodium acetate and the solvent is selected from ethanol claim 4 , methanol and mixtures of methyl tert-butyl ether with ethanol or methanol.6. The process according to or claim 4 , wherein step a) is performed in ethanol as solvent or in a mixture of ethanol and methyl tert-butyl ether.7. The process according to any one of to claim 4 , wherein step a) is performed at a temperature ranging from 50° C. to 150° C.8. The process according to any one of to claim 4 , wherein step a) is performed in presence of Fe(CO).9. The process according to claim 4 , wherein the palladium catalyst is bis(triphenylphosphine)palladium chloride (Pd(PPh)Cl) claim 4 , the base is triethylamine and the solvent is ethanol.10. The process according to any one of to claim 4 , wherein the alkoxycarbonylation reaction of step a) is performed by lithium exchange by first contacting the compound of Formula (III) with an organolithium reagent; and then adding a chloroformate or a ...

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Номер записи: 92
16-02-2017 дата публикации

METHOD FOR CONTROLLING ARTHROPOD PESTS

Номер: US20170042158A1
Автор: AKIZUKI Naoya, Iwata Atsushi, SHIMOKAWATOKO Yasutaka
Принадлежит: Sumitomo Chemical Company, Limited

Provided is a method for controlling arthropod pests. The method includes: step A): a step of forming furrows in the soil; step B): a step of placing, in the furrows formed in the previous step, seeds retaining one or more neonicotinoid compounds selected from Group I, on the surface or in the interior, and a step of applying an aqueous dispersion or an aqueous solution containing one or more neonicotinoid compounds selected from Group I to the furrows formed in the previous step; and step C): a step of covering the furrows. In step B above Group I is a group selected from clothianidin, thiamethoxam, imidacloprid, and thiacloprid. 1. A method for controlling arthropod pests , the method comprising:Step A) a step of forming furrows in the soil;Step B) a step of placing, in the furrows formed in the previous step, seeds retaining one or more neonicotinoid compounds selected from Group I, on the surface or in the interior, anda step of applying an aqueous dispersion or an aqueous solution containing one or more neonicotinoid compounds selected from Group I to the furrows formed in the previous step; andStep C): a step of covering the furrows,wherein Group I is a group consisting of clothianidin, thiamethoxam, imidacloprid, and thiacloprid.2. The method for controlling arthropod pests according to claim 1 , wherein the seeds are corn seeds. The present invention relates to a method for controlling arthropod pests.Regarding the method for preventing the damages caused by arthropod pests in crop cultivation, various methods are conventionally known (for example, Patent Citation 1 and Non Patent Citation 1).On the other hand, there is known a method for protecting germinating seeds that have been treated with an agrochemical, by keeping one or more agrochemical-containing particles in the immediate vicinity of agrochemically treated seeds (for example, Patent Citation 2).[Patent Citation 1] JP-A 2014-037401[Patent Citation 2] JP-A 2008-501353[Non Patent Citation 1] ...

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Номер записи: 93
18-02-2016 дата публикации

COMPOUNDS AND METHODS FOR INDUCING CHONDROGENESIS

Номер: US20160045514A1
Автор: CHATTERJEE Arnab K., PAYETTE Joshua, Schultz Peter G., YANG Baiyuan, YOON Hongchul, ZHU Shoutian
Принадлежит: The California Institute for Biomedical Research

Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes. 96. The method of any one of , , , or wherein:{'sup': 2', '4', '7', '8', '4', '7', '8', '9', '10', '4', '7', '8', '9', '10', '4', '7', '8', '4', '7', '8', '4', '11, 'Ris halo, C(O)R, alkyl, optionally substituted alkoxy, haloalkyl, (CRR)OR, (CRR)(CRR)OR, X(CRR)(CRR)OR, X(CRR)C(O)OR, or X(CRR)C(O)NRR; and'}{'sup': 3', '4', '4', '11, 'sub': '2', 'each Ris independently selected from CN, halo, C(O)R, COH, C(O)NRR, alkyl, or optionally substituted alkoxy;'}{'sup': 3', '3', '2, 'or Rtogether with an adjacent Ror with Rform a ring.'}10. The method of wherein:{'sup': 2', '7', '8', '4', '7', '8', '9', '10', '4', '7', '8', '9', '10', '4', '7', '8', '4', '7', '8', '4', '11, 'sub': 3', '3', '3', '3', '3', '2, 'Ris F, Cl, C(O)CH, CH, CF, OCH, OEt, OPr, OCF, OCHF, (CRR)OR, (CRR)(CRR)OR, X(CRR)(CRR)OR, X(CRR)C(O)OR, or X(CRR)C(O)NRR; and'}{'sup': '3', 'sub': 3', '2', '2', '3', '3', '3, 'each Ris independently selected from CN, F, Cl, C(O)CH, COH, C(O)NH, CH, OCF, or OCH;'}{'sup': 3', '3', '2, 'or Rtogether with an adjacent Ror with Rform a ring.'}11. The method of wherein Ris F claim 10 , Cl claim 10 , C(O)CH claim 10 , CH claim 10 , CF claim 10 , OCH claim 10 , OEt claim 10 , OPr claim 10 , OCF claim 10 , OCHF claim 10 , CHOCH claim 10 , CHOH claim 10 , CHCHOH claim 10 , CHOHCHOH claim 10 , CHCHCHOH claim 10 , CHCHOHCHOH claim 10 , OCHC(O)OH claim 10 , or OCHC(O)NH.12. The method of wherein each Ris independently selected from CN claim 11 , F claim 11 , Cl claim 11 , C(O)CH claim 11 , or COH.13. The method of wherein Ris F claim 12 , Cl claim 12 , C(O)CH claim 12 , CH claim 12 , CF claim 12 , OCH claim 12 , OEt claim 12 , OPr claim 12 , OCF claim 12 , or CHCHCHOH.147. The method of any one of claim 12 , claim 12 , claim 12 , or wherein:{'sup': 2', '7', '8', '9', '10', '4', '7', '8', '9', '10', '4', '7', '8', '9', '10', '4', '11 ...

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Номер записи: 94
01-05-2014 дата публикации

HERBICIDE SAFENER COMPOSITIONS

Номер: US20140121104A1
Автор: AHRENS HARTMUT, Dörner-Rieping Simon, Hachker Erwin, Köhn Arnim, ROSINGER CHRISTOPHER HUGH, Van Almsick Andreas, ZIEMER Frank
Принадлежит: Bayer Intellectual Property GmbH

Herbicide-safener compositions are described, comprising active ingredients from the group of the N-(1,2,5-oxadiazol-3-yl)benzamides and safeners. These herbicidal compositions are particularly suitable for use against harmful plants in crops of useful plants. 2. The herbicide-safener composition as claimed in claim 1 , in whichW is CY,{'sub': 1', '6', '3', '7', '1', '6', '1', '6', '1', '6, 'R is hydrogen, (C-C)-alkyl, (C-C)-cycloalkyl, halo-(C-C)-alkyl, (C-C)-alkoxy, halo-(C-C)-alkoxy, cyano, nitro, methylsulfenyl, methylsulfinyl, methylsulfonyl, acetylamino, benzoylamino, methoxycarbonyl, ethoxycarbonyl, benzoyl, methylcarbonyl, piperidinylcarbonyl, trifluoromethylcarbonyl, halogen, amino, aminocarbonyl, methylaminocarbonyl, dimethylaminocarbonyl, methoxymethyl,'}{'sub': 1', '6', '1', '6', '3', '6', 'n', '1', '6', 'n', '1', '6', '1', '6', '2', '1', '6', '2', '2', '1', '6', '1', '6', '2, 'sup': 1', '2', '2', '1', '1', '1', '1', '1', '1', '2, 'X and Z are each independently nitro, halogen, cyano, (C-C)-alkyl, (C-C)-haloalkyl, (C-C)-cycloalkyl, OR, S(O)R, (C-C)-alkyl-S(O)R, (C-C)-alkyl-OR, (C-C)-alkyl-CON(R), (C-C)-alkyl-SON(R), (C-C)-alkyl-NRCOR, (C-C)-alkyl-NRSORor 1,2,4-triazol-1-yl,'}{'sub': 1', '6', '1', '6', '2', '2', '2', '1', '6', 'n', '1', '6', '1', '6', '2', '1', '6', '2', '2', '1', '6', '1', '6', '2', '2', '2', '2', '2', '2, 'sup': 1', '2', '1', '1', '2', '1', '1', '2', '1', '1', '1', '1', '1', '1', '2, 'Y is hydrogen, nitro, halogen, cyano, (C-C)-alkyl, (C-C)-haloalkyl, OR, S(O)—R, SON(R), NRSOR, NRCOR, (C-C)-alkyl-S(O)R, (C-C)-alkyl-OR, (C-C)-alkyl-CON(R), (C-C)-alkyl-SON(R), (C-C)-alkyl-NRCOR, (C-C)-alkyl-NRSOR, tetrahydrofuranyloxymethyl, tetrahydrofuranylmethoxymethyl, O(CH)-3,5-dimethyl-1,2-oxazol-4-yl, O(CH)—O(3,5-dimethoxypyrimidin-2-yl, O(CH)-5-pyrrolidin-2-one or O(CH)-5-2,4-dimethyl-2,4-dihydro-3H-1,2,4-triazol-3-one,'}{'sup': 1', '3, 'sub': 1', '6', '2', '6', '2', '6', '3', '6', '3', '6', '1', '6', '1', '6, 'Ris hydrogen, (C-C)-alkyl, (C-C)- ...

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Номер записи: 95
15-02-2018 дата публикации

1,3,4-THIADIAZOL-2-YL-BENZAMIDE DERIVATIVES AS INHIBITORS OF THE WNT SIGNALLING PATHWAY

Номер: US20180044306A1
Автор: BASTING Daniel, Bender Eckhard, Geisler Jens, GIESE Anja, Golz Stefan, Hägebarth Andrea, Lienau Philip, Liu Ningshu, Mönning Ursula, MÖWES Manfred, Pühler Florian, Schneider Dirk, Scott William J., SIEGEL Franziska, Thede Kai, Zorn Ludwig
Принадлежит: BAYER PHARMA AKTIENGESELLSCHAFT

The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients. 6. (canceled)8. The compound according to claim 1 , which is selected from the group consisting of:3-{[(4-methylpiperazin-1-yl)acetyl]amino}-N-[5-(piperidin-1-yl)-1,3,4-thiadiazol-2-yl]-4-(trifluoromethoxy)benzamide,tert-butyl 4-(5-{[3-{[(4-methylpiperazin-1-yl)acetyl]amino}-4-(trifluoromethoxy)benzoyl]amino}-1,3,4-thiadiazol-2-yl)piperazine-1-carboxylate,{'b': '1', 'tert-butyl 4-[5-({3-[(morpholin-4-ylacetyl)amino]-4-(trifluoromethoxy)benzoyl}amino)-1,3,4-thiadiazol-2-yl]piperazine-1-carboxylate, p 3-{[(4-methylpiperazin-1-yl)acetyl]amino}-N-[5-(pyrrolidin-1-yl)-1,3,4-thiadiazol-2-yl]-4-(trifluoromethoxy)benzamide,'}N-(5-cyclohexyl-1,3,4-thiadiazol-2-yl)-3-{[(4-methylpiperazin-1-yl)acetyl]amino}-4-(trifluoromethoxy)benzamide,methyl 4-(5-{[3-{[(4-methylpiperazin-1-yl)acetyl]amino}-4-(trifluoromethoxy)benzoyl]amino}-1,3,4-thiadiazol-2-yl)piperazine-1-carboxylate,3-{[(4-methylpiperazin-1-yl)acetyl]amino}-N-[5-(4-methylpiperidin-1-yl)-1,3,4-thiadiazol-2-yl]-4-(trifluoromethoxy)benzamide,N-[5-(4-hydroxy-4-methylpiperidin-1-yl)-1,3,4-thiadiazol-2-yl]-3-{[(4-methylpiperazin-1-yl)acetyl]amino}-4-(trifluoromethoxy)benzamide,N-{5-[4-(cyclopropylcarbonyl)piperazin-1-yl]-1,3,4-thiadiazol-2-yl}-3-{[(4-methylpiperazin-1-yl)acetyl]amino}-4-(trifluoromethoxy)benzamide,N-{5-[4-(2-hydroxypropan-2-yl)piperidin-1-yl]-1,3,4-thiadiazol-2-yl}-3-[(morpholin-4-ylacetyl)amino]-4-(trifluoromethoxy)benzamide,N-[5-(4-methoxypiperidin-1-yl)-1,3,4- ...

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Номер записи: 96
15-02-2018 дата публикации

MOLECULES HAVING CERTAIN PESTICIDAL UTILITIES, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES RELATED THERETO

Номер: US20180044332A1
Автор: Baum Erich W., Crouse Gary D., Fischer Lindsey G., Giampitro Natalie C., Petkus Jeff, Sparks Thomas C., Ward Andrew L.
Принадлежит:

This disclosure relates to the field of molecules having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”). 3. A molecule according to and having a structure listed in Table 4.4. A process comprising: applying a molecule according to to a locus to control a pest claim 1 , in an amount sufficient to control such pest. This Application is a continuation-in-part of U.S. patent application Ser. No. 14/959,377 filed on Dec. 4, 2015, which is a divisional of U.S. patent application Ser. No. 14/208,394 filed on Mar. 13, 2014, now U.S. Pat. No. 9,249,133, which claims the benefit and priority from U.S. provisional application Ser. No. 61/784,020 filed on Mar. 14, 2013, where the contents of which are incorporated by reference in their entireties.The U.S. patent application Ser. No. 14/959,377 filed on Dec. 4, 2015 is also a continuation of U.S. patent application Ser. No. 14/661,389 filed on Mar. 18, 2015, now U.S. Pat. No. 9,278,964, which is a continuation of U.S. patent application Ser. No. 14/208,430 filed on Mar. 13, 2014, now U.S. Pat. No. 9,029,560, which claims the benefit and priority from U.S. provisional application Ser. No. 61/784,020, which was filed on Mar. 14, 2013, where the contents of which are incorporated by reference in their entireties.This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Nematoda, Arthropoda, and Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules ...

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Номер записи: 97
13-02-2020 дата публикации

Substituted Oxadiazoles for Combating Phytopathogenic Fungi

Номер: US20200045974A1
Автор: CAMBEIS Erica, Craig Ian Robert, ESCRIBANO CUESTA Ana, Fehr Marcus, Grammenos Wassilios, Grote Thomas, Lohmann Jan Klaas, Mentzel Tobias, Mueller Bernd, QUINTERO PALOMAR Maria Angelica, SEET Michael, TERTERYAN-SEISER Violeta, WIEBE Christine, WINTER Christian Harald
Принадлежит:

The present invention relates to novel trifluoromethyloxadiazoles of the formula I, or the N-oxides, or the agriculturally useful salts thereof; and to their use for controlling phytopathogenic fungi; and to a method for combating phytopathogenic harmful fungi, which process comprises treating the fungi, the plants, the soil or seeds to be protected against fungal attack, with an effective amount of at least one compound of the formula I, or an N-oxide, or an agriculturally acceptable salt thereof; and to agrochemical compositions comprising at least one compound of the formula I; and to agrochemical compositions further comprising seeds. 114-. (canceled)17. The compound of claim 15 , wherein n is 0.18. The compound of claim 15 , wherein W is #1-(C═O)—NR-#2 claim 15 , #1-(C═S)—NR-#2 or #1-S(═O)—NR-#2.19. The compound of claim 15 , wherein Rand Rindependently of each other are selected from the group consisting of hydrogen claim 15 , halogen claim 15 , C-C-alkyl and C-C-haloalkyl; or Rand Rtogether with the carbon atom to which they are bound form a cyclopropyl ring.20. The compound of claim 15 , wherein Ris a bicyclic carbocycle selected from the group consisting of radicals R.10 claim 15 , R.15 claim 15 , R.22 claim 15 , R.23 claim 15 , R.24 claim 15 , R.25 claim 15 , R.26 claim 15 , R.27 and R.31 as defined herein; and wherein each radical may be connected to the group W through one of the ring carbon atoms by substitution of one hydrogen atom; and wherein Ris unsubstituted or substituted with 1 claim 15 , 2 claim 15 , 3 claim 15 , 4 or up to the maximum possible number of radicals selected from the group consisting of oxo claim 15 , hydroxy claim 15 , halogen and C-C-alkyl.21. The compound of claim 15 , wherein Ris a bicyclic carbocycle selected from the group consisting of radicals R.32 claim 15 , R.33 claim 15 , R.34 and R.35 as defined herein; and wherein Ris unsubstituted or substituted with 1 claim 15 , 2 claim 15 , 3 claim 15 , 4 or up to the maximum ...

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Номер записи: 98
23-02-2017 дата публикации

DAZOMET COMPOSITIONS

Номер: US20170049106A1
Автор: Herdman Douglas J., Pope Thomas, Tham Peter
Принадлежит:

A solid body of dazomet for use in internal remedial treatments of wood and methods of applying such solid bodies to wooden structures and manufacturing such solid bodies. The solid bodies can be easily transported and inserted into treatment holes in utility poles, wooden pilings, and other wooden structures, delivering a dose of insecticide and fungicide that combats internal decay in the wood. 1. A method for internal remedial treatment of wood , comprising the step of:inserting a sheathless rod of compressed dazomet composition having a length of about 100 millimeters to about 250 millimeters into a treatment hole in a wooden structure;wherein the dazomet composition is flowable before compression and comprises between 90% to 96% solid tetrahydro-3,5-dimethyl-2H-1,3,5-thiadiazine-2-thione by weight of the composition; between 0.5% and 5.0% of a saturated oil, by weight of the composition; and between 1% and 5% of a polysaccharide, by weight of the composition.2. The method of claim 1 , wherein the sheathless rod of compressed dazomet composition has a diameter of about 5 millimeters to about 30 millimeters.3. The method of claim 2 , wherein the sheathless rod of compressed dazomet composition has a weight of between 10 grams and 500 grams.4. The method of claim 1 , wherein the solid tetrahydro-3 claim 1 ,5-dimethyl-2H-1 claim 1 ,3 claim 1 ,5-thiadiazine-2-thione is in the form of granules or a powder.5. The method of claim 1 , wherein the saturated oil comprises a hydrogenated oil.6. The method of claim 1 , wherein the saturated oil comprises a hydrogenated vegetable oil.7. The method of claim 1 , wherein the polysaccharide comprises a starch.8. The method of claim 7 , wherein the starch comprises a maltodexrin.9. The method of claim 1 , wherein the dazomet composition further comprises a first accelerant.10. The method of claim 9 , wherein the first accelerant is selected from the group consisting of copper naphthenate claim 9 , copper sulfate claim 9 , copper ...

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Номер записи: 99
08-05-2014 дата публикации

1,3,4-OXADIAZOLES-2-THIO DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS

Номер: US20140128348A1
Автор: Chow Ken, IM WHA-BIN, Li Ling, Takeuchi Janet A.
Принадлежит: ALLERGAN, INC.

The present invention relates to substituted 1,3,4-oxadiazoles-2-thio derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 5. A compound according to selected from:3-{[4-(1-{[5-(3,4-Dimethylphenyl)-1,3,4-oxadiazol-2-yl]thio}ethyl)benzyl]amino}propanoic acid;(3-{[4-(1-{[5-(3,4-Dimethylphenyl)-1,3,4-oxadiazol-2-yl]thio}ethyl)benzyl]amino}propyl)phosphonic acid; and(3-{[4-({[5-(3,4-Dimethylphenyl)-1,3,4-oxadiazol-2-yl]thio}methyl)benzyl]amino}propyl)phosphonic acid.6. A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to and a pharmaceutically acceptable adjuvant claim 1 , diluent or carrier.7. A pharmaceutical composition according to wherein the compound is selected from:3-{[4-(1-{[5-(3,4-Dimethylphenyl)-1,3,4-oxadiazol-2-yl]thio}ethyl)benzyl]amino}propanoic acid;(3-{[4-(1-{[5-(3,4-Dimethylphenyl)-1,3,4-oxadiazol-2-yl]thio}ethyl)benzyl]amino}propyl)phosphonic acid; and(3-{[4-({[5-(3,4-Dimethylphenyl)-1,3,4-oxadiazol-2-yl]thio}methyl)benzyl]amino}propyl)phosphonic acid.9. A method of claim 8 , wherein the pharmaceutical composition is administered to the mammal to treat ocular diseases claim 8 , wet and dry age-related macular degeneration claim 8 , diabetic retinopathy claim 8 , retinopathy of prematurity claim 8 , retinal edema claim 8 , geographic atrophy claim 8 , glaucomatous optic neuropathy claim 8 , chorioretinopathy claim 8 , hypertensive retinopathy claim 8 , ocular ischemic syndrome claim 8 , prevention of inflammation-induced fibrosis in the back of the eye claim 8 , various ocular inflammatory diseases including uveitis claim 8 , scleritis claim 8 , keratitis claim 8 , and retinal vasculitis; or systemic vascular barrier related diseases claim 8 , various inflammatory diseases claim 8 , including acute lung injury claim 8 , its prevention claim 8 , sepsis claim 8 , tumor ...

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Номер записи: 100