Настройки

Укажите год
-

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

Подробнее
-

Мониторинг СМИ

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

Подробнее

Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Укажите год
Укажите год
Применить Всего найдено 2317. Отображено 100.
10-05-2012 дата публикации

Compound inhibiting in vivo phosphorus transport and medicine containing the same

Номер: US20120115851A1
Автор: Nobuaki Eto, Rika Nagao, Tetsuko Kazama
Принадлежит: Kyowa Hakko Kirin Co Ltd

An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein A represents an optionally substituted five- to nine-membered unsaturated carbocyclic moiety or a five- to nine-membered unsaturated heterocyclic moiety, and represents a single bond or a double bond, R 5 represents optionally substituted aryl or the like, Z represents —N═CHR 6 R 7 or the like, R 6 and R 7 represent H, optionally substituted alkyl, optionally substituted aryl or the like, R 101 and R 102 together form ═O, and R 103 and R 104 represent H, or R 101 and R 104 together from a bond, and R 102 and R 103 together form a bond.

Подробнее
Номер записи: 1
31-05-2012 дата публикации

Substituted Esters as Cannabinoid-1 Receptor Modulators

Номер: US20120135975A1
Автор: Irene E. Whitney, Jeffrey J. Hale, Vincent J. Colandrea, William K. Hagmann
Принадлежит: Merck and Co Inc

Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.

Подробнее
Номер записи: 2
31-05-2012 дата публикации

Substituted acylanilides and methods of use thereof

Номер: US20120136052A1
Автор: Duane D. Miller, James T. Dalton
Принадлежит: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.

Подробнее
Номер записи: 3
16-08-2012 дата публикации

Electroluminescent device using azomethine-lithium-complex as electron injection layer

Номер: US20120205638A1
Автор: Poopathy Kathirgamanathan, Yun Fu Chan
Принадлежит: Merck Patent GmBH

In OLEDs, improved efficiency is obtained by compounds which can form inter alia electron injection layers of the formula (I) wherein R 1 is a 1-5 ring aryl (including polycyclic), aralkyl or heteroaryl group which is optionally substituted with one or more C 1 -C 4 alkyl, alkoxy or cyano; R 2 and R 3 together form a 1-5 ring aryl (including polycyclic), aralkyl or heteroaryl group which is optionally substituted with C 1 -C 4 alkyl, alkoxy or cyano; R 4 is hydrogen, C 1 -C 4 alkyl or aryl; and Ar is monocyclic, bicyclic or tricyclic aryl or heteroaryl which is optionally substituted with one or more C 1 -C 4 -alkyl or alkoxy groups, or an oligomer thereof.

Подробнее
Номер записи: 4
23-08-2012 дата публикации

New compounds, pharmaceutical compositions and uses thereof

Номер: US20120214785A1
Автор: Bernd Nosse, Gerald Juergen Roth, Heike Neubauer, Joerg Kley, Martin Fleck, Niklas Heine, Thorsten Lehmann-Lintz
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Подробнее
Номер записи: 5
25-10-2012 дата публикации

Adamantyl diamide derivatives and uses of same

Номер: US20120270873A1
Автор: Andrew D. White, Dario Doller, Gil Ma, Guiying Li, Hermogenes N. Jimenez, Maojun Guo, Michel Grenon
Принадлежит: H Lundbeck AS

The present invention provides adamantyl-diamide derivatives of formula (I): wherein R 1 and R 2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.

Подробнее
Номер записи: 6
18-07-2013 дата публикации

Adamantyl diamide derivatives and uses of same

Номер: US20130184277A1
Автор: Andrew D. White, Dario Doller, Gil Ma, Guiying Li, Hermogenes N. Jimenez, Maojun Guo, Michel Grenon
Принадлежит: H Lundbeck AS

The present invention provides adamantyl diamide derivatives of formula (I): wherein R 1 and R 2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.

Подробнее
Номер записи: 7
29-08-2013 дата публикации

BENZAMIDE DERIVATIVE WITH ANTICANCER ACTIVITY AND PREPARATION METHOD AND USE THEREOF

Номер: US20130225810A1
Автор: Bai Hua, Gong Yongxiang, Liu Lifei, Liu Xiaoyu, Zhao Xuyang, Zhong Jinqing, Zhou Qixian, Zhu Qifeng
Принадлежит: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.

Provided are a benzamide derivative as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the preparation method and use thereof for preparing a medicine for treating cancer, wherein the group definitions of formula (I) are as set out in the description. 2. The compound according to claim 1 , wherein Rand Rare independently selected from the group consisting of hydrogen claim 1 , substituted or unsubstituted (C-C)alkyl claim 1 , —CORor —COR claim 1 , and Rand Rcan also cyclize to form a substituted or unsubstituted 4- claim 1 , 5- claim 1 , or 6-membered ring claim 1 , wherein Ris a substituted or unsubstituted (C-C)alkyl claim 1 , a substituted or unsubstituted (C-C)alkenyl claim 1 , a substituted or unsubstituted (C-C)alkynyl claim 1 , a substituted or unsubstituted (C-C)cycloalkyl claim 1 , and a substituted or unsubstituted aryl; Ris a substituted or unsubstituted (C-C)alkyl claim 1 , a substituted or unsubstituted (C-C)alkenyl claim 1 , a substituted or unsubstituted (C-C)alkynyl claim 1 , and a substituted or unsubstituted (C-C)cycloalkyl.3. The compound according to claim 2 , wherein Rand Rare independently selected from the group consisting of hydrogen claim 2 , substituted or unsubstituted (C-C)alkyl claim 2 , —CORor —COR claim 2 , and Rand Rcan also cyclize to form a substituted or unsubstituted 4- claim 2 , 5- claim 2 , or 6-membered ring claim 2 , wherein Ris a substituted or unsubstituted (C-C)alkyl claim 2 , a substituted or unsubstituted (C-C)cycloalkyl claim 2 , a substituted or unsubstituted aryl; Ris a substituted or unsubstituted (C-C)alkyl claim 2 , a substituted or unsubstituted (C-C)cycloalkyl.4. The compound according to claim 3 , wherein Rand Rare independently selected from the group consisting of hydrogen claim 3 , methyl claim 3 , ethyl claim 3 , and propyl.5. The compound according to claim 3 , wherein Rand Rcan also cyclize to form a substituted or unsubstituted 5- or 6-membered ring which may contain one or more ...

Подробнее
Номер записи: 8
19-09-2013 дата публикации

CYSTEINE PROTEASE INHIBITORS FOR THE TREATMENT OF PARASITIC DISEASES

Номер: US20130244962A1
Автор: BEAULIEU Christian, ISABEL Elise, MELLON Christopher
Принадлежит: Merck Frosst Canada Ltd.

Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, stronglyoidiasis, trichostrongyliasis, trichomoniasis or cestodiasis. 121.-. (canceled)23. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable carrier.24. A pharmaceutical composition of further comprising another agent selected from the group consisting of: nifurtimox claim 23 , benznidazole claim 23 , allopurinol claim 23 , terbinafine claim 23 , lovastatin claim 23 , ketoconazole claim 23 , itraconazole claim 23 , posaconazole claim 23 , miltefosine claim 23 , ilmofosine claim 23 , pamidronate claim 23 , alendronate claim 23 , risedronate claim 23 , chloroquine claim 23 , proguanil claim 23 , mefloquine claim 23 , quinine claim 23 , pyrimethamine-sulphadoxine claim 23 , doxocycline claim 23 , berberine claim 23 , halofantrine claim 23 , primaquine claim 23 , atovaquone claim 23 , pyrimethamine-dapsone claim 23 , artemisinin claim 23 , quinhaosu claim 23 , meglumine antimonite claim 23 , sodium stibogluconate claim 23 , amphotericin B claim 23 , praziquantel claim 23 , oxamniquine claim 23 , pentamidine claim 23 , melarsoprol claim 23 , suramin and eflornithine and the pharmaceutically acceptable salts and mixtures thereof.25. A method of treating a patient having a parasitic disease comprising administering to the patent in need thereof a composition comprising a compound of claim 22 , wherein the parasitic disease is selected from the group consisting of toxoplasmosis claim 22 , malaria claim 22 , ...

Подробнее
Номер записи: 9
31-10-2013 дата публикации

NOVEL PHARMACEUTICAL FORMS, AND METHODS OF MAKING AND USING THE SAME

Номер: US20130289280A1
Автор: Almarsson Örn, Bis Joanna, Hickey Magali Bourghol, McMahon Jennifer, Peterson Matthew L., Remenar Julius F., Shattock Tanise, Tawa Mark, Zaworotko Michael J.
Принадлежит:

Crystalline salts, polymorphs, solvates, and hydrates of bicalutamide, 5-fluorouracil, donepezil, anastrozole, nelfinavir, mirtazapine, lansoprazole, and tamsulosin, or derivatives thereof are provided by the subject invention. Methods of making and using the same are also provided. 1. A bicalutamide , donepezil , nelfinavir , or tamsulosin salt made by reacting bicalutamide , donepezil , nelfinavir , or tamsulosin with an organic or inorganic acid in a crystallization solvent , wherein the form has an aqueous solubility of approximately 5 micrograms/mL to approximately 100 mg/mL.2. The bicalutamide claim 1 , donepezil claim 1 , nelfinavir claim 1 , or tamsulosin salt of claim 1 , comprising an (R)-tamsulosin HCl salt that is crystallized in a crystallization solvent comprising methanol.3. The bicalutamide claim 1 , donepezil claim 1 , nelfinavir claim 1 , or tamsulosin salt of claim 1 , comprising a nelfinavir HCl salt that is crystallized in a crystallization solvent comprising propylene glycol.4. The bicalutamide claim 1 , donepezil claim 1 , nelfinavir claim 1 , or tamsulosin salt of claim 1 , wherein the mole ratio of bicalutamide claim 1 , donepezil claim 1 , nelfinavir claim 1 , tamsulosin claim 1 , or a derivative thereof to the salt forming component is about M:N claim 1 , wherein M is an integer from 1 to 100 and N is an integer from 1 to 100.5. The bicalutamide claim 4 , donepezil claim 4 , nelfinavir claim 4 , or tamsulosin salt of claim 4 , wherein M is an integer from 1 to 20 and N is an integer from 1 to 20.6. The bicalutamide claim 1 , donepezil claim 1 , nelfinavir claim 1 , or tamsulosin salt of claim 1 , wherein the salt is crystalline.7. The bicalutamide claim 1 , donepezil claim 1 , nelfinavir claim 1 , or tamsulosin salt of claim 1 , wherein said tamsulosin salt is a (R)-tamsulosin salt comprising (R)-tamsulosin HCl.8. The (R)-tamsulosin salt of claim 7 , wherein: {'sup': '3', 'Monoclinic, P2(1), a=7.5499(13) Å, b=9.1496(15) Å, c=31.755(5) Å, ...

Подробнее
Номер записи: 10
07-11-2013 дата публикации

Cyanoenamines and Their use as Fungicides

Номер: US20130298291A1
Автор: Benting Jurgen, Desbordes Philippe, Dubost Christophe, Genix Pierre, Narabu Shinichi, Vors Jean-Pierre, Wachendorff-Neumann Ulrike
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to cyanoenamine derivatives, their process of preparation, intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants and in material protection, using these compounds or compositions. 2. A composition for controlling an unwanted microorganism or insect claim 1 , comprising at least one compound according to claim 1 , and one or more extenders and/or surfactants.3. A compound according to claim 1 , capable of being used for controlling unwanted microorganisms and insects.4. A method for controlling an unwanted microorganism claim 1 , comprising applying a compound according to claim 1 , to the microorganisms and/or a habitat thereof.5. A process for preparing a composition for controlling an unwanted microorganism claim 1 , comprising mixing a compound according to claim 1 , with one or more extenders and/or surfactants.6. A compound according to claim 1 , capable of being used for treating transgenic plants.7. A transgenic plant that has been treated with a compound of .8. A method for treating a transgenic plant complying treating said plant with a compound of . The present invention relates to cyanoenamine derivatives, their process of preparation, intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants and in material protection, using these compounds or compositions.In WO 01/85673 arylcyanoenaminones of general formula:are described, wherein K represents an oxygen or sulphur atom, Ar represents an optionally substituted aryl or heteroaryl, X may represent a cyano group, Z represents an optionally substituted phenyl or naphthyl and Y represents an optionally substituted alkyl chain. However, there is no disclosure or suggestion in this documents of any derivative wherein Ar ...

Подробнее
Номер записи: 11
21-11-2013 дата публикации

Amide derivative, pest control agent containing the amide derivative, and use of the amide derivative

Номер: US20130310459A1
Автор: Atsuko Kawahara, Atsushi Hirabayashi, Hidenori Daido, Hidetaka Tsukada, Hiroyuki Katsuta, Mai Hirose, Michikazu Nomura, Yasuaki FUKAZAWA, Yoji Aoki, Yumi Kobayashi, Yusuke Takahashi
Принадлежит: Mitsui Chemicals Agro Inc

An amide derivative represented by the following Formula (1) is provided as an amide derivative showing a significantly excellent effect for a pest control action. In the following Formula (1), A represents a carbon atom, a nitrogen atom, or the like, and K represents a non-metal atomic group necessary for forming a cyclic linking group derived from benzene or a heterocyclic. X represents a halogen atom or the like; n represents an integer of from 0 to 4. R 1 and R 2 represent hydrogen atoms, alkyl groups, or the like. T represents —C(=G 1 )-Q 1 or —C(=G 1 )-G 2 Q 2 , and G 1 to G 3 each represent oxygen atoms or the like. Q 1 and Q 2 each represent a hydrogen atom, an alkyl group, an aryl group, or the like. Y 1 and Y 5 each represent a halogen atom or the like, Y 2 and Y 4 each represent a hydrogen atom or the like, and Y 3 represents a C2-C5 haloalkyl group.

Подробнее
Номер записи: 12
28-11-2013 дата публикации

PROCESS FOR PRODUCTION OF AROMATIC AMIDE CARBOXYLIC ACID DERIVATIVE

Номер: US20130317247A1
Автор: Katsuta Hiroyuki, Kitajima Kazuki, Kodaka Kenji, Okumura Kunio
Принадлежит: MITSUI CHEMICALS AGRO, INC.

The invention provides a method for producing an aromatic amide carboxylic acid derivative represented by the following Formula (2), including a step of reacting an aromatic amide halide derivative represented by the following Formula (1) with carbon monoxide. In the following Formulae (1) and (2), Rrepresents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; Xrepresents a fluorine atom or a cyano group; Xrepresents a halogen atom; and n represents an integer of from 0 to 3. 5. The aromatic amide halide derivative according to claim 4 , wherein claim 4 , in Formula (1) claim 4 , Rrepresents a methyl group claim 4 , Xrepresents a fluorine atom claim 4 , Xrepresents a chlorine atom claim 4 , and n represents 0 or 1. The invention relates to a method for producing an aromatic amide carboxylic acid derivative.Methods for producing aromatic carboxylic acid derivatives are known in which carbon monoxide is inserted into a certain kind of aromatic halide derivative in the presence of a base and water, using a palladium compound as a catalyst (see, for example, Japanese Patent Application Laid-Open (JP-A) Nos. 8-104661, 2003-48859, and 2005-220107).Furthermore, a method for producing an aromatic amide carboxylic acid derivative having an amide bond and a halogen atom, etc., in the molecule thereof is known (see, for example, International Patent Publication No. WO 2010/18857).The inventors have studied industrial methods for producing aromatic amide carboxylic acid derivatives using the methods described in the above known art. However, the methods require multi-step reactions and are therefore insufficient as industrial production methods.The invention provides a method that allows for the production of an aromatic amide carboxylic acid derivative having a halogen atom, etc., through fewer process steps, and a useful intermediate for use in the production method.As a result of the intensive studies to develop a method that allows for the production of an ...

Подробнее
Номер записи: 13
05-12-2013 дата публикации

Substituted acylanilides and methods of use thereof

Номер: US20130324602A1
Автор: Duane D. Miller, James T. Dalton
Принадлежит: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.

Подробнее
Номер записи: 14
02-01-2014 дата публикации

TREATING ANDROGEN DECLINE IN AGING MALE (ADAM)-ASSOCIATED CONDITIONS WITH SARMS

Номер: US20140005263A1
Автор: Dalton James T., HE Yali, Miller Duane D., Yin Donghua
Принадлежит: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

This invention provides methods for treatment and inhibition of a male subject having an Androgen Decline in Aging Male (ADAM)-associated condition, for example sexual dysfunction, decreased sexual libido, erectile dysfunction, hypogonadism, sarcopenia, osteopenia, osteoporosis, an alteration in cognition and mood, depression, anemia, hair loss, obesity, muscle loss, dry eye, memory loss, benign prostate hyperplasia and/or prostate cancer, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, pro-drug, polymorph, crystal, or any combination thereof. 3. The method of claim 1 , wherein said Z is CN.4. The method of claim 1 , wherein said Q is halogen.6. The method of claim 1 , wherein said SARM does not penetrate the central nervous system (CNS).7. The method of claim 1 , further comprising administering a pharmaceutical preparation comprising said SARM compound and/or its optical isomer or pharmaceutically acceptable salt or any combination thereof; and a pharmaceutically acceptable carrier.8. The method according to claim 7 , comprising intravenously claim 7 , intraarterially claim 7 , or intramuscularly injecting to said subject said pharmaceutical preparation in liquid form; subcutaneously implanting in said subject a pellet containing said pharmaceutical preparation; orally administering to said subject said pharmaceutical preparation in a liquid or solid form; or topically applying to the skin surface of said subject said pharmaceutical preparation.9. The method according to claim 7 , wherein said pharmaceutical preparation is a pellet claim 7 , a tablet claim 7 , a capsule claim 7 , a solution claim 7 , a suspension claim 7 , an emulsion claim 7 , an elixir claim 7 , a gel claim 7 , a cream claim 7 , a suppository or a parenteral formulation.10. The method of claim 1 , wherein said male subject is an ...

Подробнее
Номер записи: 15
02-01-2014 дата публикации

4-(2-(6-SUBSTITUTED-HEXYLIDENE) HYDRAZINYL)BENZONITRILE AND PREPARATION THEREOF

Номер: US20140005395A1
Автор: Ronsheim Matthew
Принадлежит:

The present teachings provide a compound of Formula (I-B): 2. The compound of claim 1 , wherein Ris selected from halo claim 1 , cyano claim 1 , azido claim 1 , —OSOF claim 1 , —OSOCF claim 1 , —OSOCF claim 1 , —OSOPhCH claim 1 , —OSOPh claim 1 , and —OSOCH.3. The compound of claim 2 , wherein Ris selected from I claim 2 , Br claim 2 , and Cl.4. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare each independently selected from H claim 1 , halo claim 1 , —CH claim 1 , —CFand —OCH.5. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare each independently H.6. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare each independently selected from H claim 1 , halo claim 1 , cyano claim 1 , —CH claim 1 , —CFand —OCH.7. The compound of claim 1 , wherein at least one R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris cyano.8. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare each independently H; and Ris cyano.11. The process of claim 10 , wherein Ris selected from halo claim 10 , cyano claim 10 , azido claim 10 , —OSOF claim 10 , —OSOCF claim 10 , —OSOCF claim 10 , —OSOPhCH claim 10 , —OSOPh claim 10 , and —OSOCH.12. The process of claim 11 , wherein Ris selected from I claim 11 , Br claim 11 , and Cl.13. The process of claim 10 , wherein R claim 10 , R claim 10 , R claim 10 , R claim 10 , R claim 10 , R claim 10 , R claim 10 , R claim 10 , R claim 10 , and Rare each independently selected from H claim 10 , halo claim 10 , —CH claim 10 , —CFand —OCH.14. The process of claim 10 , wherein R claim 10 , R claim 10 , R claim 10 , R claim 10 , R claim 10 , R claim 10 , R claim 10 , R claim 10 , R claim 10 , and Rare each independently H.15. The process of claim 10 , wherein at least one of R claim 10 , ...

Подробнее
Номер записи: 16
30-01-2014 дата публикации

Iminopropene compound and use thereof

Номер: US20140031376A1
Автор: Atsushi Iwata, Shigeyuki Itoh
Принадлежит: Sumitomo Chemical Co Ltd

The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.

Подробнее
Номер записи: 17
20-02-2014 дата публикации

SOLID FORMS OF SELECTIVE ANDROGEN RECEPTOR MODULATORS

Номер: US20140051764A1
Автор: AHN Tai, BIRD Thomas G., Dalton James T., DICKASON David A., HONG Seoung-Soo
Принадлежит:

The present invention relates to solid forms of (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide and process for producing the same. 1. A paracrystalline form of (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide compound whereby said paracrystalline form is paracrystalline form B′ characterized by:a. an X-ray powder diffraction pattern displaying a broad halo with two harmonic peaks between 15-25 °2θ andb. a phase transition point of about 55° C. as determined by differenterial scanning calorimetry (DSC).2d.. The paracrystalline form of claim 1 , whereby said form is characterized by an X-ray diffraction pattern as depicted in3. The paracrystalline form of claim 1 , whereby said form is characterized by its solubility in water being between 20-30 mg/L at 22° C.4. A composition comprising a paracrystalline form B′ of (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide of and a suitable carrier or diluent.5. A process for the preparation of a paracrystalline form B′ of compound (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide comprising stiffing a suspension of a crystalline form of (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide in water at ambient temperature of about 20-30° C. for at least 0.5 hours claim 1 , to obtain a paracrystalline compound.6. A process for the preparation of a paracrystalline form B′ of compound (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide comprising stiffing a suspension of solid form A in water at 37° C. overnight claim 1 , wherein said solid form A is characterized by: an X-Ray Powder diffraction pattern comprising peaks at °2θ (d value Å) angles of about 5.6 (15.9) claim 1 , 7.5 (11.8) claim 1 , 8.6 (10.3) claim 1 , 9.9 (8.9) claim 1 , 12.4 (7.1) claim 1 , 15.0 (5.9) claim 1 , 16.7 (5.3) ...

Подробнее
Номер записи: 18
20-03-2014 дата публикации

Method of treating estrogen receptor (er) -positive breast cancers with selective androgen receptor modulator (sarms)

Номер: US20140080905A1
Автор: James T. Dalton, Mitchell S. Steiner, Ramesh Narayanan, Sunjoo Ahn
Принадлежит: GTx Inc

This invention relates to the treatment of androgen receptor-positive breast cancer in a subject, for example a female subject. Accordingly, this invention provides methods of: a) treating a subject suffering from breast cancer; b) treating a subject suffering from metastatic breast cancer; c) treating a subject suffering from refractory breast cancer; d) treating a subject suffering from AR-positive breast cancer; e) treating a subject suffering from AR-positive refractory breast cancer; f) treating a subject suffering from AR-positive metastatic breast cancer; g) treating a subject suffering from AR-positive and ER-positive breast cancer; h) treating a subject suffering from triple negative breast cancer; i) treating a subject suffering from advanced breast cancer; j) treating a subject suffering from breast cancer that has failed SERM (tamoxifen, toremifene), aromatase inhibitor, trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and/or fulvestrant treatments; k) treating, preventing, suppressing or inhibiting metastasis in a subject suffering from breast cancer; l) prolonging survival of a subject with breast cancer, and/or m) prolonging the progression-free survival of a subject with breast cancer; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound, comprising administering to the subject a therapeutically effective amount of a SARM compound of this invention.

Подробнее
Номер записи: 19
04-01-2018 дата публикации

Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto

Номер: US20180000087A1
Автор: Baum Erich W., Benko Zoltan L., CHOY Nakyen, Crouse Gary D., Daeuble, DeKorver Kyle A., Demeter David A., Eckelbarger Joseph D., GRAY KAITLYN, Heemstra Ronald J., Hunter Ricky, JR. Ronald, Knueppel Daniel I., Li Fangzheng, Martin Timothy P., Nissen Jeffrey, Riener Michelle, Ross, Sparks Thomas C., SR. John F., Trullinger Tony K., Vednor Peter, Wessels Frank J., Yap Maurice C.
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 2. A molecule according to claim 1 , wherein Ris selected from the group consisting of H and Cl.3. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , Cl claim 1 , Br claim 1 , CH claim 1 , and CF.4. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , CH claim 1 , CF claim 1 , and OCF.5. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , CH claim 1 , and CF.6. A molecule according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare H.7. A molecule according to claim 1 , wherein Ris Cl.8. A molecule according to claim 1 , wherein Ris Cl.9. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , Cl claim 1 , and CF.10. A molecule according to claim 1 , wherein Ris selected from the group consisting of H and CH.11. A molecule according to claim 1 , wherein Ris selected from the group consisting of cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl claim 1 , cyclohexyl claim 1 , azetidinyl claim 1 , morpholinyl claim 1 , oxetanyl claim 1 , pyranyl claim 1 , tetrahydrothiophenyl claim 1 , thietanyl claim 1 , thietanyl-oxide claim 1 , and thietanyl-dioxide claim 1 ,{'sub': 3', '3', '3, 'wherein each cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, ...

Подробнее
Номер записи: 20
05-01-2017 дата публикации

INSECTICIDAL COMPOUNDS

Номер: US20170000120A1
Автор: Edmunds Andrew, Pitterna Thomas, Stoller Andre
Принадлежит: SYNGENTA PARTICIPATIONS AG

The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests (I) wherein Y, X, X 2 and Q are as defined in claim ; or salts thereof. 3. A compound of formula (I) according to wherein{'sub': '1', 'Xis hydrogen, fluorine or methoxy'}{'sub': 2', '2', '1, 'Xis hydrogen or cyano, with the condition that if Xis cyano, then Xis hydrogen,'}R is hydrogen, methyl or ethyl.4. A compound of formula (I) according to wherein{'sub': 1', '2, 'Xis methoxy and Xis hydrogen.'}5. A compound of formula (I) according to wherein{'sub': 2', '1, 'Xis cyano and Xis hydrogen.'}7. A method of controlling insects claim 1 , acarines claim 1 , nematodes or molluscs which comprises applying to a pest claim 1 , to a locus of a pest claim 1 , or to a plant susceptible to attack by a pest an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in .8. An insecticidal claim 1 , acaricidal claim 1 , nematicidal or molluscicidal composition comprising an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in together with an agrochemically acceptable diluent or carrier.9. A composition according to which further comprises one or more additional insecticidal claim 8 , acaricidal claim 8 , nematicidal or molluscicidal compounds.10. A method of protecting useful plants from insects claim 1 , acarines claim 1 , nematodes or molluscs claim 1 , comprising applying to said plants claim 1 , to the locus thereof claim 1 , or to plant propagation material thereof claim 1 , an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of ...

Подробнее
Номер записи: 21
06-01-2022 дата публикации

SOLID FORMS OF SELECTIVE ANDROGEN RECEPTOR MODULATORS

Номер: US20220000830A1
Автор: AHN Tai, BIRD Thomas G., Dalton James T., DICKASON David A., HONG Seoung-Soo
Принадлежит: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

The present invention relates to solid forms of (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide and process for producing the same. 1. A method of treating a condition caused by androgen decline in aging male (ADAM) or androgen decline in female (ADIF) comprising administering a composition comprising a crystalline form A of (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide compound , characterized by an X-ray powder diffraction pattern displaying peaks at °2θ (d value Å) angles of about 5.6 (15.9) , 7.5 (11.8) , 8.6 (10.3) , 9.9 (8.9) , 12.4 (7.1) , 15.0 (5.9) , 16.7 (5.3) , 17.3 (5.1) , 18.0 (4.9) , 18.5 (4.8) , 19.3 (4.6) , 19.8 (4.5) , 20.6 (4.3) , 21.8 (4.1) , 22.3 (4.0) , 23.4 (3.8) , 23.9 (3.7) , 24.6 (3.6) , 24.9 (3.6) , 25.4 (3.5) , 26.0 (3.4) , 26.5 (3.4) and 27.8 (3.2).2. The method of claim 1 , wherein said condition caused by androgen decline in aging male (ADAM) is selected from fatigue claim 1 , depression claim 1 , decreased libido claim 1 , sexual dysfunction claim 1 , erectile dysfunction claim 1 , hypogonadism claim 1 , osteoporosis claim 1 , hair loss claim 1 , anemia claim 1 , obesity claim 1 , sarcopenia claim 1 , osteopenia claim 1 , benign prostate hyperplasia claim 1 , and prostate cancer or any combination thereof.3. The method of claim 1 , wherein said condition caused by androgen decline in female (ADIF) is selected from sexual dysfunction claim 1 , decreased sexual libido claim 1 , hypogonadism claim 1 , sarcopenia claim 1 , osteopenia claim 1 , osteoporosis claim 1 , depression claim 1 , anemia claim 1 , hair loss claim 1 , obesity claim 1 , endometriosis claim 1 , uterine cancer claim 1 , and ovarian cancer or any combination thereof.4. A method of treating chronic muscular wasting comprising administering a composition comprising a crystalline form A of (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide compound ...

Подробнее
Номер записи: 22
02-01-2020 дата публикации

ISOXAZOLINE-SUBSTITUTED BENZAMIDE COMPOUND AND PESTICIDE

Номер: US20200000777A1
Автор: KIKUCHI Takamasa, KOMODA Mitsuaki, MITA Takeshi, MIZUKOSHI Takashi, Takii Shinji, YAOSAKA Manabu
Принадлежит: NISSAN CHEMICAL CORPORATION

A substituted alkenylbenzene compound of formula (4): 2. The substituted alkenylbenzene compound of formula (4) according to claim 1 , wherein:{'sup': '1', 'sub': 5', '1', '6', '1', '6', '1', '6, 'Xis selected from the group consisting of a halogen atom, —SF, C-Chaloalkyl, C-Chaloalkoxy and C-Chaloalkylthio;'}{'sup': '3', 'sub': 1', '6', '1', '6', '1', '6, 'Xis selected from the group consisting of a hydrogen atom, halogen atom, cyano, nitro, C-Calkyl, C-Chaloalkyl and C-Calkoxy;'}{'sup': '4', 'Xis a hydrogen atom or halogen atom;'}{'sup': 3a', '3b, 'Rand Rare each a fluorine atom;'}{'sup': 3c', '2', '3', '4', '1', '3', '4', '1', '3', '4', '3c, 'Ris selected from the group consisting of a hydrogen atom, fluorine atom, chlorine atom, bromine atom and trifluoromethyl, with a proviso that in case where Xis a fluorine atom, chlorine atom or trifluoromethyl and both Xand Xare a hydrogen atom, in case where both Xand Xare a fluorine atom and Xis a hydrogen atom, and in case where both Xand Xare trifluoromethyl and Xis a hydrogen atom, Ris a hydrogen atom, chlorine atom, bromine atom or trifluoromethyl.'} This application is a continuation of U.S. patent application Ser. No. 15/972,939, filed May 7, 2018, which is a continuation of U.S. patent application Ser. No. 15/097,002, filed Apr. 12, 2016, now U.S. Pat. No. 10,045,969, which is a continuation of U.S. patent application Ser. No. 14/568,964, filed Dec. 12, 2014, which is a continuation of U.S. patent application Ser. No. 13/850,067, filed Mar. 25, 2013, now U.S. Pat. No. 8,946,492, which is a divisional of U.S. patent application Ser. No. 13/350,297, filed Jan. 13, 2012, now U.S. Pat. No. 8,492,311, which is a divisional of U.S. patent application Ser. No. 13/166,294, filed Jun. 22, 2011, now U.S. Pat. No. 8,138,213, which is a divisional of U.S. patent application Ser. No. 12/509,859, filed Jul. 27, 2009, now U.S. Pat. No. 8,022,089, which is a divisional of U.S. patent application Ser. No. 11/514,921, filed Sep. 5, ...

Подробнее
Номер записи: 23
02-01-2020 дата публикации

BIARYL COMPOUND, PREPARATION METHOD AND USE THEREOF

Номер: US20200002280A1
Автор: Huang Yafei, Qiu Ruomeng, Tang Ting, Wang Yonghui
Принадлежит:

The present invention belongs to the technical field of chemical pharmaceuticals, and relates to a compound represented by general formula (I) or formula (II) and a preparation method thereof. The compounds are biaryl derivatives with RORγt activation activity. The biaryl derivatives disclosed in this invention can effectively activate the RORγt protein receptor, and thereby promote the differentiation of Th17 cells and increasing the production of IL-17, which can be used as an immune modulator for the treatment of various cancers or viral infection-related diseases. 2. The compound of Formula (I) or (II) or the pharmaceutically acceptable salt thereof according to claim 1 , wherein:{'sub': 1', '2', '3', '3', '5', '3', '6', '3', '6', '9', '10', '1', '2', '3', '2', '6', '3', '7', '1', '2', '3', '2', '6, 'claim-text': {'sub': 9', '10', '1', '6', '3', '6', '3', '8', '9', '10, 'wherein, R, Rare each independently selected from a group consisting of hydrogen, C-Calkyl, C-Ccycloalkyl and C-Cheterocycloalkyl, or Rand Rform a cyclic group having four to seven ring members together with the nitrogen atom to which they attach; the cyclic group contains or does not contain a second heteroatom selected from oxygen as a ring member.'}, 'R, Rand Rare each independently selected from a group consisting of hydrogen, C-Calkyl, C-Ccycloalkyl, C-Cheterocycloalkyl containing one oxygen atom, and —NRR, or any two of R, Rand Rform C-Calkyl alkenyl or C-Ccycloalkyl alkenyl, or R, Rand Rform C-Calkyl alkynyl;'}3. The compound of Formula (I) or (II) or the pharmaceutically acceptable salt thereof according to claim 2 , wherein Ris selected from a group consisting of C-Calkyl claim 2 , C-Ccycloalkyl claim 2 , C-Coxoheterocycloalkyl claim 2 , phenyl substituted with one or more R; pyridyl substituted with one or more R; pyrimidinyl substituted with one or more R; pyridone substituted with one or more R claim 2 , pyrazolyl substituted with one or more R claim 2 , pyrrolyl substituted with one ...

Подробнее
Номер записи: 24
04-01-2018 дата публикации

TRICYCLIC SPIRO COMPOUND

Номер: US20180002308A1
Автор: ASADA Masaki, FUCHIBE Kazuhiro, HIGUCHI Satonori, HIROBE Masaya, KOTANI Tohru, Oikawa Ryo, TAKANO Hirotsugu, TANI Kousuke
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

A medicinal agent for the prevention and/or treatment of diseases caused by EPreceptor activation. A compound having antagonistic activity against the EPreceptor is contained as an active ingredient in the medicinal agent. The compound represented by the following general formula (I) as defined in the specification, a salt, an N-oxide, or a solvate thereof, or a prodrug of these is useful as a medicinal component having antagonistic activity against the EPreceptor for the prevention and/or treatment of diseases caused by EPreceptor activation. 3. The compound according to claim 1 , wherein at least one Ris —CONHR.4. The compound according to claim 1 , wherein Lis —NHCO— claim 1 , or —CONH—.6. The compound according to claim 1 , which is any one of the following:(1) 4-[4-cyano-2-({[(2′R,4S)-6-(methylcarbamoyl)-2,3-dihydrospiro[chromene-4,1′-cyclopropan]-2′-yl]carbonyl}amino)phenyl]butanoic acid,(2) 4-{4-cyano-2-[({(2′R,4S)-6-[(cyclopropylmethyl)carbamoyl]-2,3-dihydrospiro[chromene-4,1′-cyclopropan]-2′-yl}carbonyl)amino]phenyl}butanoic acid,(3) 4-{4-cyano-2-[({(2′R,4S)-6-[(2-methoxyethyl)carbamoyl]-2,3-dihydrospiro[chromene-4,1′-cyclopropan]-2′-yl}carbonyl)amino]phenyl}butanoic acid,(4) 4-{4-cyano-2-[({(2′R,4S)-6-[(2-methyl-2-propanyl)carbamoyl]-2,3-dihydrospiro[chromene-4,1′-cyclopropan]-2′-yl}carbonyl)amino]phenyl}butanoic acid,(5) 4-[4-cyano-2-({[(2′R,4S)-6-{[(2S)-1-methoxy-2-propanyl]carbamoyl}-2,3-dihydrospiro[chromene-4,1′-cyclopropan]-2′-yl]carbonyl}amino)phenyl]butanoic acid,(6) 4-{4-cyano-2-[({(2′R,4S)-6-[(1-methyl-1H-pyrazol-3-yl)carbamoyl]-2,3-dihydrospiro[chromene-4,1′-cyclopropan]-2′-yl}carbonyl)amino]phenyl}butanoic acid,(7) 4-[4-cyano-2-({[(2′R,4S)-6-(cyclopropylcarbamoyl)-2,3-dihydrospiro[chromene-4, 1′-cyclopropan]-2′-yl]carbonyl}amino)phenyl]butanoic acid,(8) 4-[4-cyano-2-({[(2′R,4S)-6-(isopropylcarbamoyl)-2,3-dihydrospiro[chromene-4,1′-cyclopropan]-2′-yl]carbonyl}amino)phenyl]butanoic acid,(9) 4-[4-cyano-2-({[(2′R,4S)-6-(cyclopentylcarbamoyl)-2,3- ...

Подробнее
Номер записи: 25
04-01-2018 дата публикации

Processes for the preparation of a diarylthiohydantoin compound

Номер: US20180002309A1
Автор: Andras Horvath, Cyril Ben Haim, Jennifer Albaneze-Walker, Johan Erwin Edmond
Принадлежит: Aragon Pharmaceuticals Inc

Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer.

Подробнее
Номер записи: 26
01-01-2015 дата публикации

SUBSTRATE-MIMETIC AKT INHIBITOR

Номер: US20150004698A1
Автор: Cheng Jin Q., Hamilton Andrew D., Kayser-Bricker Katherine, Sebti Said M.
Принадлежит:

Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors. 25.-. (canceled)6. The method of claim 1 , wherein the inhibitor has a p-amino benzoic acid or 4-aminobenzoic acid next to a valanine. This application is a divisional application of Ser. No. 12/480,329, entitled “Substrate-Mimetic AKT Inhibitor”, filed on Jun. 8, 2009, which claims priority to prior-filed International Application, Serial Number PCT/US2007/086751 filed Dec. 7, 2007, which claims priority to U.S. provisional patent application No. 60/868,989 filed Dec. 7, 2006, the contents of which are hereby incorporated by reference into this disclosure.This invention was made with Government support under Grant No. 1R01 CA107078-01, awarded by the National Institutes of Health. The Government may therefore have certain rights in the invention.This invention relates to oncogenic prevention and treatment. Specifically, the invention relates to using substrate inhibitors to block the effects of Akt, also known as protein kinase B (PKB).Akt/protein kinase B (PKB) has been shown to be a widely expressed Ser/Thr protein kinase whose persistent activation leads to human oncogenesis. Its role in cancer and chemoresistance is accomplished by the concomitant promotion of cell growth, migration, and angiogenesis as well as the suppression of the apoptotic pathway. There has been significant interest in Akt for its structural and ...

Подробнее
Номер записи: 27
11-01-2018 дата публикации

Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto

Номер: US20180007911A1
Автор: Baum Erich W., Benko Zoltan L., CHOY Nakyen, Crouse Gary D., Daeuble, DeKorver Kyle A., Demeter David A., Eckelbarger Joseph D., Heemstra Ronald J., Hunter Ricky, JR. Ronald, Knueppel Daniel I., Li Fangzheng, Martin Timothy P., Nissen Jeffrey, Riener Michelle, Ross, Sparks Thomas C., SR. John F., Trullinger Tony K., Vednor Peter, Wessels Frank J., Yap Maurice C.
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 2. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , F claim 1 , and Cl.3. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , F claim 1 , and Cl.4. A molecule according to claim 1 , wherein Ris F or Cl.5. A molecule according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare each independently H.6. A molecule according to claim 1 , wherein Ris selected from the group consisting of Cl and Br.7. A molecule according to claim 1 , wherein Ris selected from the group consisting of Cl and Br.8. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , Cl claim 1 , and CF.9. A molecule according to claim 1 , wherein Ris selected from the group consisting of H and CH.10. A molecule according to claim 1 , wherein Ris selected from the group consisting of CH claim 1 , CHCH claim 1 , CHCHCH claim 1 , CHCHCHCH claim 1 , CHCHCHOCHCH claim 1 , CH claim 1 , CHCH claim 1 , CHCHCH claim 1 , CHCHCHCH claim 1 , CHCHCHCHCH claim 1 , CHCHCHCHCHCH claim 1 , CHCH(CH) claim 1 , CHcyclopropyl claim 1 , CHCHcyclopropyl claim 1 , CHcyclobutyl claim 1 , CHphenyl claim 1 , CHCHphenyl claim 1 , CHC═CH claim 1 , CHC═CH claim 1 , CHCF claim 1 , CHCHF claim 1 , CHCHCF claim 1 , CHCFCF claim 1 , CHCHCHCF claim 1 , CHCHCFCF claim 1 , CHCFCFCF claim 1 , CHCHCHCHF claim 1 , CHCHSCH ...

Подробнее
Номер записи: 28
08-01-2015 дата публикации

METHOD FOR PRODUCING SUBSTITUTED ANTHRANILIC ACID DERIVATIVES

Номер: US20150011772A1
Автор: Himmler Thomas, LUI Norbert, PAZENOK Sergii, Volz Frank
Принадлежит:

The present invention relates to a process for preparing substituted anthranilic acid derivatives of the formula (I) 3. Process according to claim 2 , wherein the compound of formula (IV) is prepared in the presence of a condensing agent and of a base.4. Process according to claim 1 , wherein the palladium catalyst used is a palladium (II) salt and/or Pd(O) species.5. Process according to claim 4 , wherein the palladium catalyst used is bis(dibenzylideneacetone)palladium claim 4 , tris(dibenzylideneacetone)dipalladium claim 4 , palladium chloride claim 4 , palladium bromide and/or palladium acetate.6. Process according to claim 1 , wherein the phosphine ligand used is a compound of formula (X){'br': None, 'sup': 10', '11', '12, 'PRRR\u2003\u2003(X)'}{'sup': 10', '11', '12, 'sub': 1', '8', '1', '8', '6', '10', '1', '8', '1', '10', '1', '8', '6', '10', '6', '10', '1', '8', '1', '8', '1', '8', '1', '8, 'where the R, Rand Rradicals are each independently hydrogen, linear or branched C-C-alkyl, vinyl, aryl or heteroaryl selected from pyridine, pyrimidine, pyrrole, thiophene and furan, which may in turn be substituted by further substituents from the group of linear or branched C-C-alkyl or C-C-aryl, linear or branched C-C-alkyloxy or C-C-aryloxy, halogenated linear or branched C-C-alkyl or halogenated C-C-aryl, C-C-aryloxycarbonyl, linear or branched C-C-alkylamino, linear or branched C-C-dialkylamino, C-C-arylamino, C-C-diarylamino, hydroxyl, carboxyl, cyano and halogen,'}or a chelating biphosphine.7. Process according to claim 6 , wherein the chelating biphosphine is one or more selected from 1 claim 6 ,2-bis(diphenylphosphino)ethane claim 6 , 1 claim 6 ,2-bis(diphenylphosphino)propane claim 6 , 1 claim 6 ,2-bis(diphenylphosphino)butane claim 6 , 2 claim 6 ,2′-bis(diphenylphosphino)-1 claim 6 ,1′-binaphthyl and 1 claim 6 ,1′-bis(diphenylphosphino)ferrocene.8. Process according to claim 6 , wherein the phosphine ligand used is triphenylphosphine.9. Process according to ...

Подробнее
Номер записи: 29
17-01-2019 дата публикации

Selective androgen receptor degrader (sard) ligands and methods of use thereof

Номер: US20190015387A1
Автор: Dong-Jin Hwang, Duane D. Miller, Ramesh Narayanan, Thamarai Ponnusamy, Yali He
Принадлежит: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors, R-isomers, and non-hydroxylated and/or non-chiral propanamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

Подробнее
Номер записи: 30
15-01-2015 дата публикации

ANTI-INFECTIVE COMPOUNDS

Номер: US20150018543A1
Автор: BRODIN Priscille, CHRISTOPHE Thierry, CONTRERAS DOMINGUEZ Monica, EWANN Fanny Anne, FENISTEIN Denis Philippe Cedric, GENOVESIO Auguste, JEON Heekyoung, KANG Sunhee, KIM Eun Hye, KIM Jaeseung, LEE Saeyeon, NAM Ji Youn, NO Zaesung, PARK Eunjung, SEO Min Jung
Принадлежит:

The present invention relates to 4H-pyrido[1,2-a]pyrimidin-4-one compounds and their use in the treatment of bacterial infections, in particular Tuberculosis. 1. A screening method comprising the steps of:{'i': 'M. tuberculosis', '(a) batch infection of host cells with fluorescently labeled mycobacteria;'}(b) removing free unbound mycobacteria;(c) adding compounds that are to be tested to a multi-well plate;{'i': 'M. tuberculosis', '(d) seeding said host cells infected with fluorescently labeled mycobacteria into said multi-well plate containing said compounds;'}{'i': 'M. tuberculosis', '(e) incubating said multi-well plate containing host cells infected with fluorescently labeled mycobacteria and said compounds;'}(f) fluorescently labeling said host cells; and(g) analyzing said multi-well plate using automated confocal microscopy.2M. tuberculosis. The method of claim 1 , wherein the screening method searches for compounds that interfere with the multiplication of within said host cells.3. The method of claim 1 , wherein the host cells are macrophages.4. The method of claim 3 , wherein the macrophages are live macrophages.5. The method of claim 1 , wherein the automated confocal fluorescence microscopy measures intracellular mycobacterial growth.6. The method of claim 1 , wherein step (g) comprises determining for each compounda total host cell number,a percentage of infected host cells; and/ora percent inhibition of infection.7. The method of claim 6 , wherein the host cells are macrophages.8. The method of claim 6 , wherein step (g) further comprises analyzing the total host cell number to determine if it is high or low; and wherein{'i': 'M. tuberculosis', '(i) a low total cell number is indicative for the compound toxicity and/or of the unrestricted growth of inside macrophages;'}and/or(ii) a high (total) cell number is indicative that the compound is not toxic and prevents mycobacterial growth.9. The method of claim 1 , further comprising the step of using ...

Подробнее
Номер записи: 31
17-01-2019 дата публикации

TRIFLUOROMETHOXYLATION OF ARENES VIA INTRAMOLECULAR TRIFLUOROMETHOXY GROUP MIGRATION

Номер: US20190016670A1
Автор: Hojczyk Katarzyna N., Ngai Ming-Yu
Принадлежит: The Research Foundation for The State University of New York

The present invention provides a process of producing a trifluoromethoxylated aryl or trifluoromethoxylated heteroaryl having the structure: 19-. (canceled)11. The process of claim 10 , wherein the second suitable solvent is chloroform claim 10 , dichloromethane claim 10 , nitromethane claim 10 , dimethylforamide claim 10 , diethyl ether claim 10 , tetrahydrofuran claim 10 , dioxane claim 10 , dichloroethane claim 10 , or hexane.12. The process of claim 10 , wherein step (b) is carried out at room temperature.13. The process of claim 10 , wherein step (b) is carried out at a temperature of 50-140° C.14. The process of claim 10 , wherein the compound is maintained in the second suitable solvent for 10-50 hours.15. The process of claim 10 , wherein A is a phenyl or pyridine.16. The process of claim 10 , wherein A is a furan claim 10 , thiophene claim 10 , pyrrole claim 10 , thiazole claim 10 , imidazole claim 10 , pyrazole claim 10 , isooxazole claim 10 , isothiazole claim 10 , naphthalene claim 10 , anthracene claim 10 , pyrimidine claim 10 , pyrazine claim 10 , pyridazine claim 10 , indole claim 10 , indoline claim 10 , benzofuran claim 10 , benzothiophene claim 10 , or quinolone.2037-. (canceled) This application claims priority of U.S. Provisional Application Nos. 62/192,789, filed Jul. 15, 2015; 62/192,462, filed Jul. 14, 2015; 62/063,246, filed Oct. 13, 2014; and 62/062,508, filed Oct. 10, 2014, the contents of each of which are hereby incorporated by reference.Throughout this application various publications are referenced. The disclosures of these documents in their entireties are hereby incorporated by reference into this application in order to more fully describe the state of the art to which this invention pertains.Fluorine atoms are often introduced into organic molecules to enhance their pharmacological properties such as solubility, metabolic and oxidative stability, lipophilicity, and bioavailability. Among the fluorine containing functional groups, ...

Подробнее
Номер записи: 32
26-01-2017 дата публикации

HEPATITIS B ANTIVIRAL AGENTS

Номер: US20170022150A1
Автор: Cao Hui, Gao Xuri, Jin Meizhong, Kass Jorden, Li Wei, Or Yat Sun, Peng Xiaowen, Qiu Yao-Ling
Принадлежит:

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: 4. A compound of claim 1 , wherein R is —C-Calkyl claim 1 , —C-Calkenyl claim 1 , —C-Calkynyl claim 1 , —C-Ccycloalkyl claim 1 , or 3- to 8-membered heterocyclic claim 1 , each optionally substituted with one claim 1 , two or three groups independently selected from hydroxy claim 1 , protected hydroxy claim 1 , halo claim 1 , —CN claim 1 , amino claim 1 , protected amino claim 1 , optionally substituted —C-Calkyl claim 1 , optionally substituted —C-Ccycloalkyl claim 1 , optionally substituted —C-Calkoxy claim 1 , —C(O)OR claim 1 , —OC(O)NH—R claim 1 , —C(O)NH-R claim 1 , and —C(O)—R claim 1 , wherein Ris optionally substituted —C-Calkyl claim 1 , optionally substituted —C-Calkenyl claim 1 , optionally substituted —C-Calkynyl claim 1 , optionally substituted —C-Ccycloalkyl claim 1 , optionally substituted 3- to 8-membered heterocyclic claim 1 , optionally substituted aryl or optionally substituted heteroaryl.8. A pharmaceutical composition claim 1 , comprising a compound or a combination of compounds according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in combination with a pharmaceutically acceptable carrier or excipient.9. A method of treating or preventing an HBV infection in an individual in need thereof claim 1 , comprising administering the subject a therapeutically effective amount of a compound or a combination of compounds of .10. The method of claim 9 , further comprising administering to the individual at least one additional therapeutic agent selected from the group consisting of a HBV polymerase inhibitor claim 9 , interferon claim 9 , viral entry inhibitor claim 9 , viral maturation inhibitor claim 9 , literature-described capsid assembly modulator claim 9 , reverse transcriptase inhibitor claim 9 , TLR-agonist claim 9 , inducer of cellular viral RNA sensor claim 9 , therapeutic vaccine claim 9 , and ...

Подробнее
Номер записи: 33
17-04-2014 дата публикации

COMPOUNDS USEFUL IN THE SYNTHESIS OF BENZAMIDE COMPOUNDS

Номер: US20140107369A1
Автор: Lozanov Mario Emilov, Skufca Anthony Frank, Zeiler Andrew George
Принадлежит: Resverlogix Corp.

Compounds that are useful in the synthesis of 2-amino-4,6-dimethoxybenzamide derivatives and other benzamide compounds. 5. A compound selected from:2-bromo-3,5-dimethoxytrifluoroacetanilide,2,4-dibromo-3,5-dimethoxytrifluoroacetanilide,2-cyano-3,5-dimethoxytrifuoroacetanilide, and2-amino-4,6-dimethoxybenzonitrile.6. A compound according to claim 2 , wherein X is oxygen.7. A compound according to claim 3 , wherein X is oxygen.8. A compound according to claim 4 , wherein X is oxygen.9. A compound according to claim 2 , wherein R is selected from CF claim 2 , CFH claim 2 , CFH claim 2 , CCl claim 2 , CClH claim 2 , and CClH.10. A compound according to claim 3 , wherein R is selected from CF claim 3 , CFH claim 3 , CFH claim 3 , CCl claim 3 , CClH claim 3 , and CClH.11. A compound according to claim 4 , wherein R is selected from CF claim 4 , CFH claim 4 , CFH claim 4 , CCl claim 4 , CClH claim 4 , and CClH.12. The compound according to claim 5 , wherein the compound is 2-bromo-3 claim 5 ,5-dimethoxytrifluoroacetanilide.13. The compound according to claim 5 , wherein the compound is 2 claim 5 ,4-dibromo-3 claim 5 ,5-dimethoxytrifluoroacetanilide.14. The compound according to claim 5 , wherein the compound is 2-cyano-3 claim 5 ,5-dimethoxytrifuoroacetanilide.15. The compound according to claim 5 , wherein the compound is 2-amino-4 claim 5 ,6-dimethoxybenzonitrile. This application claims priority from U.S. Provisional Patent Application No. 61/713,711, filed Oct. 15, 2012, which is pending, and is incorporated herein by reference in its entirety.This invention relates to novel compounds useful in the synthesis of benzamide compounds.Benzamide compounds have been involved as intermediates for the synthesis of many pharmaceutical therapeutic drugs. For example, 2-amino-4,6-dimethoxybenzamide was reported as an intermediate in U.S. Pat. No. 3,966,965 in the synthesis of oxamic acid derivatives for the prevention of hypersensitivity in allergic reactions. More recent patent ...

Подробнее
Номер записи: 34
17-02-2022 дата публикации

TRICYCLIC SPIRO COMPOUND

Номер: US20220048881A1
Автор: ASADA Masaki, FUCHIBE Kazuhiro, HIGUCHI Satonori, HIROBE Masaya, KOTANI Tohru, Oikawa Ryo, TAKANO Hirotsugu, TANI Kousuke
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

A medicinal agent for the prevention and/or treatment of diseases caused by EPreceptor activation is disclosed. A compound having antagonistic activity against the EPreceptor is contained as an active ingredient in the medicinal agent. The compound represented by the following general formula (I) as defined in the specification, a salt, an N-oxide, or a solvate thereof, or a prodrug of these is useful as a medicinal component having antagonistic activity against the EPreceptor for the prevention and/or treatment of diseases caused by EPreceptor activation. 1. A method for preventing and/or treating a disease caused by EPreceptor activation in a subject in need thereof ,the method comprising administering an effective amount of a compound that is 4-[4-cyano-2-({[(2′R,4S)-6-(isopropylcarbamoyl)-2,3-dihydrospiro[chromene-4,1′-cyclopropan]-2′-yl]carbonyl}amino)phenyl]butanoic acid, a salt thereof, or a solvate thereof, or a prodrug of these to the subject.2. The method according to claim 1 , wherein the disease caused by EPreceptor activation is a bone disease claim 1 , a cancer claim 1 , a systemic granulomatous disease claim 1 , an immune disease claim 1 , alveolar pyorrhea claim 1 , gingivitis claim 1 , periodontitis claim 1 , Kawasaki disease claim 1 , multiple organ failure claim 1 , chronic headache claim 1 , pain claim 1 , vasculitis claim 1 , venous incompetence claim 1 , varicose veins claim 1 , aneurysm claim 1 , aortic aneurysm claim 1 , anal fistula claim 1 , diabetes insipidus claim 1 , patent ductus arteriosus in neonates claim 1 , or cholelithiasis.3. The method according to claim 2 , wherein the cancer is breast cancer claim 2 , ovarian cancer claim 2 , colorectal cancer claim 2 , lung cancer claim 2 , prostate cancer claim 2 , head and neck cancer claim 2 , lymphoma claim 2 , uveal melanoma claim 2 , thymoma claim 2 , mesothelioma claim 2 , esophageal cancer claim 2 , stomach cancer claim 2 , duodenal cancer claim 2 , hepatocellular carcinoma claim 2 , ...

Подробнее
Номер записи: 35
11-02-2016 дата публикации

Pesticidal compositions and processes related thereto

Номер: US20160037779A1
Автор: Akshay PATNY, Gerald B. Watson, James E. Hunter, Joshodeep Boruwa, Pravin S. IYER, William C. Lo
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

Подробнее
Номер записи: 36
08-02-2018 дата публикации

BENZAMIDES AND RELATED INHIBITORS OF FACTOR XA

Номер: US20180036296A1
Автор: GOLDMAN Erick A., HUANG Wenrong, Li Wenhao, Scarborough Robert M., Song Yonghong, Wang Lingyan, Zhang Penglie, Zhu Bing-Yan, ZUCKETT Jingmei
Принадлежит:

Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders. 172.-. (canceled)74. The method of claim 73 , wherein the salt is the maleate salt.75. The method of claim 73 , wherein the compound is administered to the mammal in the form of a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier.76. The method of claim 75 , wherein the pharmaceutical composition is in capsule form.78. The method of claim 77 , wherein the salt is the maleate salt.79. The method of claim 77 , wherein the compound is administered to the mammal in the form of a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier.80. The method of claim 79 , wherein the pharmaceutical composition is in capsule form.82. The method of claim 81 , wherein the salt is the maleate salt.83. The method of claim 81 , wherein the compound is administered to the mammal in the form of a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier.84. The method of claim 83 , wherein the pharmaceutical composition is in capsule form. This invention relates to novel compounds which are potent and highly selective inhibitors of isolated factor Xa or when assembled in the prothrombinase complex. These compounds show selectivity for factor Xa versus other proteases of the coagulation (e.g. thrombin, fVIIa, fIXa) or the fibrinolytic cascades (e.g. plasminogen activators, plasmin). In another aspect, the present invention relates to novel monoamidino-containing compounds, their pharmaceutically acceptable salts, and pharmaceutically acceptable compositions thereof which are useful as potent and specific inhibitors of blood ...

Подробнее
Номер записи: 37
09-02-2017 дата публикации

NITRIFICATION INHIBITORS

Номер: US20170036969A1
Автор: Dickhaut Joachim, EBENHOECH Johan, Nave Barbara, SISAY Mihiret Tekeste, WEIGELT Wolfgang, Wissemeier Alexander, ZERULLA Wolfram
Принадлежит:

The present invention relates to novel nitrification inhibitors of formula I. Moreover, the invention relates to the use of these novel nitrification inhibitors for reducing nitrification, as well as agrochemical mixtures and compositions comprising the nitrification inhibitors. Further encompassed by the present invention are methods for reducing nitrification comprising the treatment of plants, soil and/or loci with said nitrification inhibitors, and methods for treating a fertilizer or a composition by applying said nitrification inhibitor. 116-. (canceled)18: The compound of claim 17 , wherein in said compound of formula I claim 17 , A is phenyl or a 6-membered hetaryl claim 17 , preferably phenyl claim 17 , wherein the aromatic ring may in each case be unsubstituted or may be partially or fully substituted by substituents claim 17 , which are independently of each other selected from R.19: The compound of claim 17 , wherein in said compound of formula I claim 17 , Rand Rboth represent hydrogen.20: The compound of claim 17 , wherein in said compound of formula I claim 17 , Ris hydrogen claim 17 , C-C-haloalkyl or ethinylhydroxymethyl claim 17 , and preferably Ris hydrogen.21: The compound of claim 17 , wherein in said compound of formula I claim 17 , R claim 17 , if present claim 17 , is{'sup': a', 'b', 'c', '1', 'c', '1', 'c', '1', 'c', '1', 'a', 'b', '2', '1', '2', '1', 'a', 'b', 'g', 'd', 'e', 'f, 'sub': 2', '2', '1', '6', '2', '6', '1', '4', '1', '4', '2', '4', '1', '2', '2', '4, '(i) halogen, CN, NRR, OR, C(═Y)R, C(═Y)OR, C(═Y)SR, C(═Y)NRR, YC(═Y)R, YC(═Y)NRR, NRN═C(R)(R), S(═O)R, NO, C-C-alkyl, C-C- C-C-haloalkyl, C-C-alkoxy, C-C-alkynyl-C-C-hydroxyalkyl, C-C-alkynyloxy;'}{'sub': 2', '4', '2', '4', '1', '4', '2', '4, 'sup': 1', 'c', '2', '1', 'c, '(ii) C-C-alkenylene-C(═Y)R, C-C-alkenylene-Y—C(═Y)R, wherein the C-C-alkylene or C-C-alkenylene chain may in each case be unsubstituted or may be partially or fully substituted by CN or halogen;'}{'sup': 'h', '( ...

Подробнее
Номер записи: 38
24-02-2022 дата публикации

METHOD OF PREPARING MALONONITRILE OXIME ETHER COMPOUND AND INTERMEDIATE COMPOUND

Номер: US20220055996A1
Автор: CHENG Xueming, GUO CHUNXIAO, SUN Ningning, Wu Hongfei, XU Jingbo, XU Libao, Yu Haibo
Принадлежит:

Provided are a method of preparing a malononitrile oxime ether compound and an intermediate compound. The malononitrile oxime ether compound has a structure as shown in formula (VII), wherein W is selected from aryl or heteroaryl. The preparation method comprises steps: reacting a first raw material with a second raw material in the presence of a first solvent and a catalyst to obtain the intermediate compound, wherein the first raw material has a structure as shown in formula (IV), and the second raw material has a structure as shown in formula (V); and subjecting the intermediate compound as shown in formula (VI), and, a dehyclrant to a dehydrantion reaction in the presence of a second solvent to obtain the malononitrile oxime ether compound. In the preparation process for the intermediate, a cheaper cyanoacetamide is used as a raw material, the reaction conditions are mild. Moreover, the yield of the intermediate compound is high and the cost of the process is low. Furthermore, the required malononitrile oxime ether compound, is obtained only through one-step dehydration reaction. Using the preparation method, is advantageous for improving the yield of malononitrile oxime ethers and reducing the cost of the process. 2. The preparation method according to claim 1 , wherein in the dehydration reaction process claim 1 , a molar ratio of the intermediate compound and the dehydrating agent is 1 to (1-20).3. The preparation method according to claim 1 , wherein the dehydrating agent is one or more selected from a group consisting of acetic anhydride claim 1 , bistrichlomm ethyl carbonate claim 1 , thionyl chloride claim 1 , phosphorus oxychlonde and phosphorus pentoxide claim 1 , and preferably claim 1 , is thionyl claim 1 , chloride and/or phosphorus oxychloride; andthe solvent is one or more selected from a. group consisting of halogenated alkane compounds, aromatic hydrocarbon compounds, nitrite compounds and DMF, and preferably, is trichloromethane, dichloroethane, ...

Подробнее
Номер записи: 39
18-02-2016 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20160044919A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 140-. (canceled)41. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).42. A composition according to further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 73 , 1 claim 73 ,2-dichloropropane claim 73 , 1 claim 73 ,3-dichloropropene claim 73 , 1-methylcyclopropene claim 73 , 1-naphthol claim 73 , 2-(octylthio)ethanol claim 73 , 2 claim 73 ,3 claim 73 ,5-tri-iodobenzoic acid claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-dimethylammonium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-lithium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-potassium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-sodium claim 73 , 2 claim 73 ,4 claim 73 ,5-T claim 73 , 2 claim 73 ,4 claim 73 ,5-T-2-butoxypropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-2-ethylhexyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-3-butoxypropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-TB claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butometyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butotyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isobutyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isoctyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isopropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-methyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-pentyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-sodium claim 73 , 2 claim 73 ,4 claim 73 ,5-T-triethylammonium claim 73 , 2 claim 73 ,4 claim 73 ,5-T-trolamine claim 73 , 2 claim 73 ,4-D claim 73 , 2 claim ...

Подробнее
Номер записи: 40
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 ...

Подробнее
Номер записи: 41
18-02-2021 дата публикации

MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF

Номер: US20210047347A1
Автор: "ONeill David John", Fetalvero Kristina Michelle, Narayan Sridhar, Saiah Eddine, Sengupta Shomit
Принадлежит:

The present invention provides compounds, compositions thereof, and methods of using the same. 131.-. (canceled)34. The method of claim 33 , wherein the pharmaceutically acceptable composition comprises a pharmaceutically acceptable carrier claim 33 , adjuvant claim 33 , or vehicle. The present invention relates to compounds and methods useful for modulating the Sestrin-GATOR2 interaction thereby selectively modulating mTORC1 activity indirectly. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.The mechanistic target of rapamycin complex 1 (mTORC1) protein kinase is a master growth regulator that senses diverse environmental cues, such as growth factors, cellular stresses, and nutrient and energy levels. When activated, mTORC1 phosphorylates substrates that potentiate anabolic processes, such as mRNA translation and lipid synthesis, and limits catabolic ones, such as autophagy. mTORC1 dysregulation occurs in a broad spectrum of diseases, including diabetes, epilepsy, neurodegeneration, immune response, suppressed skeletal muscle growth, and cancer among others (Howell et al., (2013) Biochemical Society transactions 41, 906-912; Kim et al., (2013) Molecules and cells 35, 463-473; Laplante and Sabatini, (2012) Cell 149, 274-293).Many upstream inputs, including growth factors and energy levels, signal to mTORC1 through the TSC complex, which regulates Rheb, a small GTPase that is an essential activator of mTORC1 (Brugarolas et al., (2004) Genes & Development 18, 2893-2904; Garami et al., (2003) Molecular Cell 11, 1457-1466; Inoki et al., (2003) Genes & Development 17, 1829-1834; Long et al., (2005) Current Biology 15, 702-713; Sancak et al., (2008) Science (New York, N.Y.) 320, 1496-1501; Saucedo et al., (2003) Nature cell biology 5, 566-571; Stocker et al., (2003) Nature cell biology 5, 559-565; Tee et al., (2002) Proc ...

Подробнее
Номер записи: 42
18-02-2016 дата публикации

COMPOUNDS USEFUL FOR THE TREATMENT OF METABOLIC DISORDERS AND SYNTHESIS OF THE SAME

Номер: US20160046560A1
Автор: Brenman Jay E., Musso David L., Sexton Jonathan Z.
Принадлежит:

The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds. 23-. (canceled)56-. (canceled)815-. (canceled)19. An amide derivative selected from the group consisting of:3-Chloro-4-{[2-hydroxy-5-(trifluoromethyl)benzene]amido}benzoic acid,Methyl 4-[(5-tert-butyl-2-hydroxybenzene)amido]-3-chlorobenzoate,4-[(5-tert-butyl-2-hydroxybenzene)amido]-3-chlorobenzoic acid, andMethyl 3-chloro-4-[(2-hydroxy-5-methylbenzene)amido]benzoate.21. A pharmaceutical composition comprising one or more pharmaceutically acceptable carriers and a compound of claim 1 , or a pharmaceutically acceptable salt thereof.2223-. (canceled)24. The pharmaceutical composition comprising an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in combination with a pharmaceutically acceptable carrier and one or more hypoglycemic agents.25. The pharmaceutical composition of claim 24 , wherein the hypoglycemic agent is selected from the group consisting of insulin claim 24 , biguanidines claim 24 , sulfonylureas claim 24 , insulin secretagogues claim 24 , a-glycosidase inhibitors claim 24 , and β-adrenoreceptor agonists.26. (canceled)27. A method of treating a disease selected from the group consisting of non-alcoholic fatty liver disease claim 1 , metabolic syndrome claim 1 , diabetes claim 1 , Syndrome X claim 1 , a diabetes-related disorder claim 1 , obesity claim 1 , cardiovascular disease claim 1 , cerebrovascular disease claim 1 , peripheral vessel disease claim 1 , lupus claim 1 , polycystic ovary disease claim 1 , carcinogenesis claim 1 , hyperplasia and combinations thereof comprising the administration to a ...

Подробнее
Номер записи: 43
25-02-2021 дата публикации

Insecticidal compounds

Номер: US20210051955A1
Автор: André Stoller, Andrew Edmunds, Thomas Pitterna
Принадлежит: SYNGENTA PARTICIPATIONS AG

The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests wherein Y, X 1 , X 2 and Q are as defined in claim 1 ; or salts thereof.

Подробнее
Номер записи: 44
25-02-2021 дата публикации

Substituted 1,1'-biphenyl compounds, analogues thereof, and methods using same

Номер: US20210052585A1
Автор: Bruce D. Dorsey, Christopher Brooks Moore, Duyan Nguyen, Yi Fan, Yingzhi Bi
Принадлежит: Arbutus Biopharma Corp, Arbutus Biopharma Inc

The present invention includes substituted 3,3′bis(phenoxymethyl)-1,1′-biphenyl compounds, analogues thereof, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) and/or hepatitis D virus (HDV) infections in a patient.

Подробнее
Номер записи: 45
14-02-2019 дата публикации

MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF

Номер: US20190048029A1
Автор: "ONeill David John", Fetalvero Kristina Michelle, Narayan Sridhar, Saiah Eddine, Sengupta Shomit
Принадлежит:

The present invention provides compounds, compositions thereof, and methods of using the same. 131.-. (canceled)33. A pharmaceutically acceptable composition comprising a compound according to and a pharmaceutically acceptable carrier claim 32 , adjuvant claim 32 , or vehicle.34. The composition according to in combination with an additional therapeutic agent. The present invention relates to compounds and methods useful for modulating the Sestrin-GATOR2 interaction thereby selectively modulating mTORC1 activity indirectly. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.The mechanistic target of rapamycin complex 1 (mTORC1) protein kinase is a master growth regulator that senses diverse environmental cues, such as growth factors, cellular stresses, and nutrient and energy levels. When activated, mTORC1 phosphorylates substrates that potentiate anabolic processes, such as mRNA translation and lipid synthesis, and limits catabolic ones, such as autophagy. mTORC1 dysregulation occurs in a broad spectrum of diseases, including diabetes, epilepsy, neurodegeneration, immune response, suppressed skeletal muscle growth, and cancer among others (Howell et al., (2013) Biochemical Society transactions 41, 906-912; Kim et al., (2013) Molecules and cells 35, 463-473; Laplante and Sabatini, (2012) Cell 149, 274-293).Many upstream inputs, including growth factors and energy levels, signal to mTORC1 through the TSC complex, which regulates Rheb, a small GTPase that is an essential activator of mTORC1 (Brugarolas et al., (2004) Genes & amp; Development 18, 2893-2904; Garami et al., (2003) Molecular Cell 11, 1457-1466; Inoki et al., (2003) Genes & amp; Development 17, 1829-1834; Long et al., (2005) Current Biology 15, 702-713; Sancak et al., (2008) Science (New York, N.Y.) 320, 1496-1501; Saucedo et al., (2003) Nature cell biology 5, 566-571 ...

Подробнее
Номер записи: 46
26-02-2015 дата публикации

Selective androgen receptor modulators

Номер: US20150057452A1
Автор: James David Rozzell, Raymond Mccague
Принадлежит: CATYLIX Inc

Compounds having therapeutic potential as androgen receptor modulators, and methods of making such compounds, are provided. The compounds are structurally related to bicalutamide but bear at least one difluoromethyl or C 2 to C 5 perfluoroalkyl group instead of a trifluoromethyl group.

Подробнее
Номер записи: 47
10-03-2022 дата публикации

PANTOTHENAMIDE ANALOGUES

Номер: US20220073450A1
Автор: Bonnert Roger Victor, DECHERING KOEN JAKOB, Hermkens Pedro Harold Han, SCHALKWIJK JOSEPHUS
Принадлежит:

The present invention provides compounds that have antimalarial activity. More in particular, the present invention provides novel compounds that are analogues of pantothenamides. The pantothenamide analogues of this invention have particularly low ICvalues against the asexual blood stages and gametocytes of malaria parasites. Furthermore, the pantothenamide analogues of this invention are characterized by low hepatic metabolism. Therefore, pantothenamide analogues of the invention are particularly suitable for use in therapeutic and/or prophylactic treatment of protozoan infections in a human or animal subject in need thereof. The invention further provides pharmaceutical formulations comprising the pantothenamide analogues as well as the therapeutic and/or prophylactic uses of the pantothenamide analogues and pharmaceutical formulations comprising them. 119-. (canceled)21. The compound according to claim 20 , wherein ring E represents phenyl claim 20 , which may be substituted with 1-3 substituents independently selected from nitril and halo.22. The compound according to claim 20 , wherein ring E represents phenyl substituted with 1-3 substituents independently selected from chloro and fluoro.23. The compound according to claim 20 , wherein ring E represents phenyl substituted with three fluoro.24. The compound according to claim 20 , wherein ring E represents phenyl substituted with 1 nitril group.26. The compound according to claim 25 , selected from the compounds (A1) claim 25 , (B1) claim 25 , (C1) and (E1).27. The compound according to claim 26 , wherein the compound is (A1).28. A pharmaceutical composition comprising a compound as defined in a pharmaceutically acceptable excipient.29. A pharmaceutical composition according to claim 28 , said composition comprising an additional anti-malarial agent.30. The pharmaceutical composition according to claim 29 , wherein said additional anti-malarial agent is selected from the groups consisting of atovaquone claim ...

Подробнее
Номер записи: 48
20-02-2020 дата публикации

ANTI-FIBROTIC COMPOUNDS

Номер: US20200055814A1
Автор: Miller Thomas, Papaioannou Nikolaos
Принадлежит:

Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound KIN or composition described herein. (Formula (I)) 235-. (canceled)36. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , whereinG is hydrogen;m is H or 2; and{'sup': '6', 'each occurrence of Ris, independently, F or Cl.'}37. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '7', 'G is C(O)R;'}m is 0;{'sup': 7', '9, 'Ris NHR; and'}{'sup': '9', 'Ris tetrazolyl, pyridinyl, pyrazolyl, imidazolyl, or triazolyl, each of which is optionally substituted with up to two alkyl groups.'}40. The compound of claim 39 , or a pharmaceutically acceptable salt thereof claim 39 , whereinX is O;{'sup': '10', 'Y is NR; and'}{'sup': '10', 'sub': '1-4', 'Ris Calkyl.'}41. The compound of claim 39 , or a pharmaceutically acceptable salt thereof claim 39 , wherein{'sup': '10', 'X is NR; and'}Y is O.42. The compound of claim 39 , or a pharmaceutically acceptable salt thereof claim 39 , wherein Rand Rtogether with the carbon atom to which they are attached form a carbonyl.44. A compound selected from the group consisting of:(E)-N-(2-fluorophenyl)-3-(3-methoxy-4-(prop-2-yn-1-yloxy)phenyl)acrylamide (1);(E)-3-(3-methoxy-4-(prop-2-yn-1-yloxy)phenyl)-N-(2-(5-methyl-1H-1,2,4-triazol-3-yl)phenyl)acrylamide (2);(E)-N-(2-chlorophenyl)-3-(3-methoxy-4-(prop-2-yn-1-yloxy)phenyl)acrylamide (3);(E)-N-(2-bromophenyl)-3-(3-methoxy-4-(prop-2-yn-1-yloxy)phenyl)acrylamide (4);(E)-3-(3-methoxy-4-(prop-2-yn-1-yloxy)phenyl)-N-(o-tolyl)acrylamide (5);(E)-N-(2-cyanophenyl)-3-(3-methoxy-4-(prop-2-yn-1-yloxy)phenyl)acrylamide (6);(E)-N-(3,4-dichlorophenyl)-3-(3- ...

Подробнее
Номер записи: 49
09-03-2017 дата публикации

Isoxazoline-substituted benzamide compound and pesticide

Номер: US20170065565A1
Автор: Manabu Yaosaka, Mitsuaki Komoda, Takamasa Kikuchi, Takashi Mizukoshi, Takeshi Mita
Принадлежит: Nissan Chemical Corp

A substituted alkenylbenzene compound of formula (4): wherein X 1 is selected from the group consisting of halogen atom, —SF 5 , C 1 -C 6 halo alkyl, hydroxy C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy C 1 -C 6 haloalkyl, C 3 -C 8 halocycloalkyl, C 1 -C 6 haloalkoxy, C 1 -C 3 haloalkoxy C 1 -C 3 haloalkoxy, C 1 -C 6 haloalkylthio, C 1 -C 6 haloalkylsulfinyl and C 1 -C 6 haloalkylsulfonyl; X 3 is selected from the group consisting of a hydrogen atom, halogen atom, cyano, nitro, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy and C 1 -C 6 alkylthio; X 4 is selected from the group consisting of a hydrogen atom, halogen atom, cyano, C 1 -C 4 alkyl, C 1 -C 4 alkoxy and C 1 -C 4 haloalkoxy; R 3 is —C(R 3a )(R 3b )R 3c , where R 3a and R 3b independently of each other are a halogen atom, or R 3a and R 3b together form 3- to 6-membered ring together with the carbon atom bonding them by forming a C 2 -C 5 haloalkylene chain, and R 3c is selected from the group consisting of a hydrogen atom, halogen atom, C 1 -C 5 alkyl, C 1 -C 5 haloalkyl, C 1 -C 4 haloalkoxy and C 1 -C 4 haloalkylthio, with a proviso that in case where X 1 is a fluorine atom, chlorine atom or trifluoromethyl, and both X 2 and X 3 are a hydrogen atom, in case where both X 1 and X 2 are fluorine atom and X 3 is a hydrogen atom, and in case where both X 1 and X 2 are trifluoromethyl and X 3 is a hydrogen atom, R 3c is a hydrogen atom, chlorine atom, bromine atom, iodine atom, C 1 -C 5 alkyl, C 1 -C 5 haloalkyl, C 1 -C 4 haloalkoxy or C 1 -C 4 haloalkylthio.

Подробнее
Номер записи: 50
11-03-2021 дата публикации

Reagents and Methods for Analysis of Proteins and Metabolites Targeted by Covalent Probes

Номер: US20210072254A1
Автор: Adelmant Guillaume, Ficarro Scott B, Marto Jarrod A
Принадлежит:

The present application relates to mass spectrometry methods for use in identifying proteins or other biomolecules which are bound irreversibly by test compounds. 1. An analytical method , comprising:i) contacting a broad thiol reactive compound with a polypeptide to form a broad thiol reactive compound-polypeptide conjugate;ii) analyzing the broad thiol reactive compound-polypeptide conjugate using a mass spectrometry assay;iii) detecting one or more thiolated ions of the broad thiol reactive compound, or derivative ions thereof, produced in the mass spectrometry assay; andiv) identifying that the broad thiol reactive compound forms an irreversible bond with the polypeptide based on the detection of the one or more thiolated ions, or derivative ions thereof, in the mass spectrometry assay;wherein the thiolated ions or derivatives thereof are fragment ions.2. The method of claim 1 , wherein the compound-polypeptide conjugate comprises one or more thioether bonds between the compound and the polypeptide.3. The method of claim 1 , wherein the irreversible bond is an irreversible covalent bond.4. The method of claim 1 , wherein step i) comprises contacting the compound and the polypeptide in the presence of a first solvent component.5. The method of claim 1 , wherein step i) further comprises contacting the compound and the polypeptide in the presence of a buffer agent.6. The method of claim 1 , wherein step i) is performed using a molar excess of the compound compared to the polypeptide.7. The method of claim 1 , further comprising contacting the broad thiol reactive compound-polypeptide conjugate with an acid in the presence of a second solvent component prior to performing the mass spectrometry assay of step ii).8. The method of claim 1 , wherein the method further comprises digesting the broad thiol reactive compound-polypeptide conjugate prior to the performing the mass spectrometry assay of step ii).9. The method of claim 8 , wherein the digesting comprises ...

Подробнее
Номер записи: 51
15-03-2018 дата публикации

SUBSTITUTED ACYLANILIDES AND METHODS OF USE THEREOF

Номер: US20180071242A1
Автор: Dalton James T., Miller Duane D.
Принадлежит:

This invention provides substituted acylanilide compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, a muscle wasting disease and/or disorder such as muscular dystrophies including Duchenne muscular dystrophy and Becker muscular dystrophy. 2. The method of claim 1 , wherein said administering comprises administering a pharmaceutical composition comprising said compound and/or its isomer claim 1 , pharmaceutically acceptable salt claim 1 , hydrate claim 1 , N-oxide claim 1 , or any combination thereof; and a pharmaceutically acceptable carrier.3. The method of claim 1 , wherein said method further increases the physical function of said subject.4. The method of claim 1 , wherein said method further increases the quality of life of said subject.5. The method of claim 1 , wherein said method increases the survival of said subject.6. The method of claim 1 , wherein said method further delays onset or improves symptoms of cardiomyopathy or respiratory function.8. (canceled)9. (canceled)11. (canceled)13. The method of claim 12 , wherein said administering comprises administering a pharmaceutical composition comprising said compound and/or its isomer claim 12 , pharmaceutically acceptable salt claim 12 , hydrate claim 12 , N-oxide claim 12 , or any combination thereof; and a pharmaceutically acceptable carrier.14. The method of claim 12 , wherein said method further increases the physical function of said subject.15. The method of claim 12 , wherein said method further increases the quality of life of said subject.16. The method of claim 12 , wherein said method further delays onset or improves symptoms of cardiomyopathy or respiratory function.18. The method of claim 17 , wherein said administering comprises administering a pharmaceutical composition comprising said compound and/or its isomer claim 17 , pharmaceutically acceptable salt claim 17 , hydrate claim 17 , N-oxide claim 17 , or any combination thereof; ...

Подробнее
Номер записи: 52
17-03-2016 дата публикации

N-(2-FLUORO-2-PHENETHYL)CARBOXAMIDES AS NEMATICIDES AND ENDOPARASITICIDES

Номер: US20160075637A1
Автор: Coqueron Pierre-Yves, Decor Anne, Goergens Ulrich, Greul Joerg, Heilmann Eike Kevin, ILG Kerstin, LOESEL PETER, Luemmen Peter, MALSAM Olga, Portz Daniela, Schwarz Hans-Georg, WELZ Claudia
Принадлежит:

The present invention relates to N-(2-halogen-2-phenethyl)carboxamides, a process for producing such compounds, their use for the control of nematodes in agricultures and their use as anthelmintics against endoparasites in animals or humans, compositions containing such compounds and methods for the control of nematodes and helminths. 4. Compound of as defined in for use as a medicament with the proviso that the following compounds are disclaimed:3-chloro-N-[2-(4-chlorophenyl)-2,2-difluoroethyl]thiophene-2-carboxamide, 3-bromo-N-[2-(4-chlorophenyl)-2,2-difluoroethyl]thiophene-2-carboxamide, N-[2-(4-chlorophenyl)-2,2-difluoroethyl]-2-(trifluoromethyl)nicotin-amide, N-[2-(2,4-dichlorophenyl)-2,2-difluoroethyl]-2-(trifluoromethyl)nicotin-amide, 2-chloro-N-[2-(4-chlorophenyl)-2,2-difluoroethyl]-4-(trifluoromethyl)nicotinamide, 2-chloro-N-[2-(2,4-dichlorophenyl)-2,2-difluoroethyl]-4-(trifluoromethyl)nicotinamide, 6-chloro-N-[2-(4-chloro-phenyl)-2,2-difluoroethyl]-4-(trifluoromethyl)nicotinamide and 6-chloro-N-[2-(2,4-dichloro phenyl)-2,2-difluoroethyl]-4-(trifluoromethyl)nicotinamide.5. Compound of according to capable for use as a medicament with the proviso that the following compounds are disclaimed:3-chloro-N-[2-(4-chlorophenyl)-2,2-difluoroethyl]thiophene-2-carboxamide, 3-bromo-N-[2-(4-chlorophenyl)-2,2-difluoroethyl]thiophene-2-carboxamide, N-[2-(4-chlorophenyl)-2,2-difluoroethyl]-2-(trifluoromethyl)nicotin-amide, N-[2-(2,4-dichlorophenyl)-2,2-difluoroethyl]-2-(trifluoromethyl)nicotin-amide, 2-chloro-N-[2-(4-chlorophenyl)-2,2-difluoroethyl]-4-(trifluoromethyl)nicotinamide, 2-chloro-N-[2-(2,4-dichlorophenyl)-2,2-difluoroethyl]-4-(trifluoromethyl)nicotinamide, 6-chloro-N-[2-(4-chloro-phenyl)-2,2-difluoroethyl]-4-(trifluoromethyl)nicotinamide and 6-chloro-N-[2-(2,4-dichloro phenyl)-2,2-difluoroethyl]-4-(trifluoromethyl)nicotinamide.6. Compound of as defined in capable for use in treatment of helminths in animals and humans.7. Compound of as defined in capable for use ...

Подробнее
Номер записи: 53
24-03-2022 дата публикации

3-SUBSTITUTED PHENYLAMIDINE COMPOUNDS, PREPARATION AND USE THEREOF

Номер: US20220089523A1
Автор: AUTKAR Santosh Shridhar, Garg Ruchi, GUMME Sachin Nagnath, KLAUSENER Alexander G.M., MAHAJAN Vishal A., NAIK Maruti, Rathod Kishor Singh, SIVAKUMAR S., VENKATESHA Hagalavadi M
Принадлежит: PI INDUSTRIES LTD.

The present invention disclosed 3-substituted phenylamidine compounds of general formula (I), wherein R, R, R, R, R, R, A and E have the same meanings as defined in description. The present invention further discloses methods for their preparation and use of the compounds of general formula (I) as a crop protection agent. 2. The compound of formula (I) as claimed in claim 1 , wherein{'sup': '1', 'sub': 1', '6', '2', '6', '2', '6', '1', '6', '1', '6', '3', '5', '4', '8, 'Ris selected from the group consisting of C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-haloalkyl, C-C-alkoxy, C-C-cycloalkyl and C-C-cycloalkylalkyl;'}{'sup': '2', 'sub': 1', '6', '2', '6', '2', '6', '3', '8', '1', '6, 'Ris selected from the group consisting of C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-cycloalkyl and C-C-haloalkyl;'}{'sup': 3', '4, 'sub': 1', '6', '2', '6', '2', '6', '1', '6', 'n', '3', '8, 'Rand Rare independently selected from the group consisting of X, cyano, C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-haloalkyl, N(R′R′″), OR″, S(O)R′″, (C═O)—R″ and C-C-cycloalkyl;'}{'sup': '5', 'sub': 1', '6', '2', '6', '2', '6', '1', '6', '3', '8, 'Ris selected from the group consisting of hydrogen, C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-haloalkyl, C-C-cycloalkyl and OR′;'}{'sup': 6', '7, 'sub': 1', '4', '2', '4', '2', '4', '1', '4', '3', '4', 'm, 'Rand Rare independently selected from the group consisting of hydrogen, X, cyano, C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-haloalkyl and C-C-cycloalkyl; wherein one or more carbon atoms in cycloalkyl ring may be replaced by heteroatoms selected from the group consisting of N, O, S(O)and optionally including 1 to 3 ring members selected from the group consisting of C(═O) or C(═S);'}{'sub': 3', '10', '5', '10, 'sup': '8', 'ring E is selected from the group consisting of fused or non-fused C-C-carbocyclyl and C-C-heterocyclyl, which may optionally be substituted by one or more groups of R;'}or agriculturally acceptable salts, isomers/structural isomers, stereo ...

Подробнее
Номер записи: 54
24-03-2022 дата публикации

HETEROCYCLIC COMPOUND AND USE THEREOF

Номер: US20220089525A1
Автор: DAINI Masaki, IKEDA Shuhei, Kamata Makoto, KASAHARA Takahito, KIKUCHI Fumiaki, KUBO Osamu, Mikami Satoshi, Morimoto Shinji, MURAKAMI Masataka, Nakamura Minoru, Oguro Yuya, PUENNER Florian, TAKASHIMA Sachie, TOITA Akinori, YAMAGUCHI Fumie, YUKAWA Takafumi
Принадлежит: Takeda Pharmaceutical Company Limited

A heterocyclic compound that can have an antagonistic action on an NMDA receptor containing the NR2B subunit, and is expected to be useful as a prophylactic or therapeutic agent for depression, bipolar disorder, migraine, pain, peripheral symptoms of dementia and the like is provided. A compound represented by the formula (I): 3. N-[(5-cyano-2-methoxypyridin-3-yl)methyl]-6-(difluoromethoxy)-5-fluoropyridine-3-carboxamide or a salt thereof.4. N-[(3-cyano-2-fluoro-6-methoxyphenyl)methyl]-6-(difluoromethoxy)-5-fluoropyridine-3-carboxamide or a salt thereof.5. A medicament comprising the compound according to or a salt thereof.6. The medicament according to claim 5 , wherein the medicament is an antagonist of an NMDA receptor containing an NR2B subunit.7. The medicament according to claim 5 , wherein the medicament is a prophylactic or therapeutic agent for depression claim 5 , bipolar disorder claim 5 , migraine claim 5 , pain claim 5 , or peripheral symptoms of dementia.8. The compound according to or a salt thereof for use in the prophylaxis or treatment of depression claim 1 , bipolar disorder claim 1 , migraine claim 1 , pain claim 1 , or peripheral symptoms of dementia.9. A method for antagonizing an NMDA receptor containing an NR2B subunit in a mammal claim 1 , comprising administering an effective amount of the compound according to or a salt thereof to the mammal.10. A method for preventing or treating depression claim 1 , bipolar disorder claim 1 , migraine claim 1 , pain claim 1 , or peripheral symptoms of dementia in a mammal claim 1 , comprising administering an effective amount of the compound according to or a salt thereof to the mammal.11. Use of the compound according to or a salt thereof for the production of a prophylactic or therapeutic agent for depression claim 1 , bipolar disorder claim 1 , migraine claim 1 , pain claim 1 , or peripheral symptoms of dementia. The present invention relates to a heterocyclic compound that can have an antagonistic ...

Подробнее
Номер записи: 55
18-03-2021 дата публикации

Nitrile oxide compound

Номер: US20210078944A1
Автор: Hiromitsu SOGAWA, Tadashi KANBARA, Toshikazu Takata, Tsuyoshi Noguchi
Принадлежит: Daikin Industries Ltd, Tokyo Institute of Technology NUC

The present invention provides a compound represented by formula (I) wherein symbols in the formula are as defined in the specification.

Подробнее
Номер записи: 56
14-03-2019 дата публикации

INSECTICIDAL COMPOUNDS

Номер: US20190075792A1
Автор: Edmunds Andrew, Pitterna Thomas, Stoller Andre
Принадлежит: SYNGENTA PARTICIPATIONS AG

The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests 3. A compound of formula (I) according to characterized in thatR is hydrogen or ethyl.4. A compound of formula (I) according to characterized in that Y is chlorine claim 1 , bromine or iodine.5. A compound of formula (I) according to characterized in that Q is a group selected from Q2 claim 1 , Q3 claim 1 , Q4 and Q5.6. A method of controlling insects claim 1 , acarines claim 1 , nematodes or molluscs which comprises applying to a pest claim 1 , to a locus of a pest claim 1 , or to a plant susceptible to attack by a pest an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in .7. An insecticidal claim 1 , acaricidal claim 1 , nematicidal or molluscicidal composition comprising an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in together with an agrochemically acceptable diluent or carrier.8. A composition according to which further comprises one or more additional insecticidal claim 7 , acaricidal claim 7 , nematicidal or molluscicidal compounds.9. A method of protecting useful plants from insects claim 1 , acarines claim 1 , nematodes or molluscs claim 1 , comprising applying to said plants claim 1 , to the locus thereof claim 1 , or to plant propagation material thereof claim 1 , an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in . This application is a continuation of U.S. patent application Ser. No. 15/824,099, filed 28 Nov. 2017, which is a divisional of U.S. ...

Подробнее
Номер записи: 57
22-03-2018 дата публикации

INSECTICIDAL COMPOUNDS

Номер: US20180077930A1
Автор: Edmunds Andrew, Pitterna Thomas, Stoller Andre
Принадлежит: SYNGENTA PARTICIPATIONS AG

The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests 3. A compound of formula (I) according to wherein{'sub': '1', 'Xis hydrogen, fluorine or methoxy'}{'sub': 2', '2', '1, 'Xis hydrogen or cyano, with the condition that if Xis cyano, then Xis hydrogen,'}R is hydrogen, methyl or ethyl.4. A compound of formula (I) according to wherein{'sub': 1', '2, 'Xis methoxy and Xis hydrogen.'}5. A compound of formula (I) according to wherein{'sub': 2', '1, 'Xis cyano and Xis hydrogen.'}7. A method of controlling insects claim 4 , acarines claim 4 , nematodes or molluscs which comprises applying to a pest claim 4 , to a locus of a pest claim 4 , or to a plant susceptible to attack by a pest an insecticidally claim 4 , acaricidally claim 4 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in 1.8. An insecticidal claim 4 , acaricidal claim 4 , nematicidal or molluscicidal composition comprising an insecticidally claim 4 , acaricidally claim 4 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in 1 together with an agrochemically acceptable diluent or carrier.9. A composition according to which further comprises one or more additional insecticidal claim 8 , acaricidal claim 8 , nematicidal or molluscicidal compounds.10. A method of protecting useful plants from insects claim 1 , acarines claim 1 , nematodes or molluscs claim 1 , comprising applying to said plants claim 1 , to the locus thereof claim 1 , or to plant propagation material thereof claim 1 , an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula I in . This application is a U.S. divisional ...

Подробнее
Номер записи: 58
12-03-2020 дата публикации

MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF

Номер: US20200079800A1
Автор: "ONeill David John", Fetalvero Kristina Michelle, Narayan Sridhar, Saiah Eddine, Sengupta Shomit
Принадлежит:

The present invention provides compounds, compositions thereof, and methods of using the same. 131.-. (canceled)33. A pharmaceutically acceptable composition comprising a compound according to claim 32 , and a pharmaceutically acceptable carrier claim 32 , adjuvant claim 32 , or vehicle.34. A method for treating depression in a patient in need thereof claim 33 , comprising the step of administering to said patient the composition of . The present invention relates to compounds and methods useful for modulating the Sestrin-GATOR2 interaction thereby selectively modulating mTORC1 activity indirectly. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.The mechanistic target of rapamycin complex 1 (mTORC1) protein kinase is a master growth regulator that senses diverse environmental cues, such as growth factors, cellular stresses, and nutrient and energy levels. When activated, mTORC1 phosphorylates substrates that potentiate anabolic processes, such as mRNA translation and lipid synthesis, and limits catabolic ones, such as autophagy. mTORC1 dysregulation occurs in a broad spectrum of diseases, including diabetes, epilepsy, neurodegeneration, immune response, suppressed skeletal muscle growth, and cancer among others (Howell et al., (2013) Biochemical Society transactions 41, 906-912; Kim et al., (2013) Molecules and cells 35, 463-473; Laplante and Sabatini, (2012) Cell 149, 274-293).Many upstream inputs, including growth factors and energy levels, signal to mTORC1 through the TSC complex, which regulates Rheb, a small GTPase that is an essential activator of mTORC1 (Brugarolas et al., (2004) Genes & Development 18, 2893-2904; Garami et al., (2003) Molecular Cell 11, 1457-1466; Inoki et al., (2003) Genes & Development 17, 1829-1834; Long et al., (2005) Current Biology 15, 702-713; Sancak et al., (2008) Science (New York, N ...

Подробнее
Номер записи: 59
02-04-2015 дата публикации

AGRICULTURAL CHEMICALS

Номер: US20150094474A1
Автор: Jackson Peter, Lindsay Derek, Moulton Benjamin, Screen Thomas, Thompson William, URCH Christopher
Принадлежит:

The present invention relates to derivatives of compounds which are known to be of use in the field of agriculture. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more changes one or more of which may be considered to represent a change of oxidation state relative to the groups in the original compound. We refer to these compounds generally as redox derivatives. The compounds are of use as insecticides, herbicides and insect repellents. 3. A compound according to claim 1 , wherein X is CHor NH.4. A compound according to claim 1 , wherein Yand Ytogether form ═O.612.-. (canceled)19. A compound according to claim 16 , wherein W is COR. The present invention relates to derivatives of compounds which are known to be of use in the field of agriculture. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more changes one or more of which may be considered to represent a change of oxidation state relative to the groups in the original compound. We refer to these compounds generally as redox derivatives.Given the global increase in demand for food, there is an international need for new treatments to reduce food crop losses to disease, insects and weeds. Over 40% of crops are lost before harvest, and 10% post harvest, worldwide. Losses have actually increased since the mid-1990s.A new threat contributing to this is the emergence of chemical-resistant organisms, for example glyphosate-resistant weeds in USA.Many current crop protection products are harmful and may cause acute and chronic health effects in those who are exposed, ranging from irritation of the skin and eyes to ...

Подробнее
Номер записи: 60
28-03-2019 дата публикации

Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto

Номер: US20190090488A1
Автор: Baum Erich W., Benko Zoltan L., CHOY Nakyen, Crouse Gary D., Daeuble, DeKorver Kyle A., Demeter David A., Eckelbarger Joseph D., GRAY KAITLYN, Heemstra Ronald J., Hunter Ricky, JR. Ronald, Knueppel Daniel I., Li Fangzheng, Martin Timothy P., Nissen Jeffrey, Olson Monica B., Riener Michelle, Ross, Sparks Thomas C., SR. John F., Trullinger Tony K., Vednor Peter, Wessels Frank J., Yap Maurice C.
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 2. A process to control a pest claim 1 , said process comprising claim 1 , applying to a locus claim 1 , a pesticidally effective amount of a molecule according to . This Application is a continuation of, and claims the benefit of, U.S. nonprovisional application Ser. No. 15/679,415, which was filed Aug. 17, 2017, and which is now allowed; Ser. No. 15/679,415 is a divisional of, and claims the benefit of, U.S. nonprovisional application Ser. No. 15/092,650, which was filed Apr. 7, 2016, and is now U.S. Pat. No. 9,781,935; Ser. No. 15/092,650 claims the benefit of, and priority from, U.S. provisional application Ser. Nos. 62/148,809; 62/148814; 62/148818; 62/148824; 62/148830; and 62/148,837; all of which were filed on Apr. 17, 2015. The entire contents of all of the above-identified applications are hereby incorporated by reference into this Application.This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides.“Many of the most dangerous human diseases are transmitted by insect vectors” (Rivero et al.). “Historically, malaria, dengue, yellow ...

Подробнее
Номер записи: 61
28-03-2019 дата публикации

Compounds, pharmaceutical composition and their use in treating neurodegenerative diseases

Номер: US20190092721A1
Автор: Bénédicte Oxombre-Vanteghem, Héléne Zephir, Marion Donnier-Marechal, Pascal Carato, Patricia Melnyk, Patrick Vermersch
Принадлежит: Centre Hospitalier Regional Universitaire de Lille CHRU, Universite Lille 2 Droit et Sante

The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts or solvates thereof, and their use.

Подробнее
Номер записи: 62
28-03-2019 дата публикации

IMMUNOREGULATORY AGENTS

Номер: US20190092729A1
Автор: Balog James Aaron, BECK Hilary Plake, Guo Weiwei, JAEN Juan Carlos, OSIPOV Maksim, POWERS Jay Patrick, REILLY Maureen Kay, SHUNATONA Hunter Paul, WALKER James Ross, Williams David K., ZIBINSKY Mikhail
Принадлежит:

Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided. 422-. (canceled)2538-. (canceled)39. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient.40. A method of treating a disease claim 1 , disorder or condition claim 1 , mediated at least in part by IDO claim 1 , comprising administering an effective amount of a compound of to a subject in need thereof.41. The method of claim 40 , wherein said compound is administered concurrently with radiation treatment claim 40 , subsequent to radiation treatment claim 40 , or prior to radiation treatment.42. (canceled)43. (canceled)44. The method of claim 40 , wherein said compound is administered in an amount effective to reverse or stop the progression of IDO-mediated immunosuppression.45. The method of claim 40 , wherein said disease claim 40 , disorder or condition is cancer.46. The method of claim 45 , wherein said cancer is a cancer of the prostate claim 45 , colon claim 45 , rectum claim 45 , pancreas claim 45 , cervix claim 45 , stomach claim 45 , endometrium claim 45 , brain claim 45 , liver claim 45 , bladder claim 45 , ovary claim 45 , testis claim 45 , head claim 45 , neck claim 45 , skin (including melanoma and basal carcinoma) claim 45 , mesothelial lining claim 45 , white blood cell (including lymphoma and leukemia) claim 45 , esophagus claim 45 , breast claim 45 , muscle claim 45 , connective tissue claim 45 , lung (including small-cell lung carcinoma and non-small-cell carcinoma) claim 45 , adrenal gland claim 45 , thyroid claim 45 , kidney claim 45 , or bone; or is glioblastoma claim 45 , mesothelioma claim 45 , renal cell ...

Подробнее
Номер записи: 63
12-04-2018 дата публикации

Molecules haveing pesticidal utiliy and intermediates, compositions and processes related thereto

Номер: US20180098541A1
Автор: Alex Nolan, David A. Demeter, John F. Daeuble, SR., Joseph D. Eckelbarger, Kaitlyn Gray, Nicolaas Vermeulen, Ricky Hunter, Ronald J. Heemstra, Ronald Ross, Jr., Timothy P. Martin, Tony K. Trullinger
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).

Подробнее
Номер записи: 64
20-04-2017 дата публикации

Compounds, pharmaceutical composition and their use in treating neurodegenerative diseases

Номер: US20170107174A1
Автор: Bénédicte Oxombre-Vanteghem, Héléne Zephir, Marion Donnier-Marechal, Pascal Carato, Patricia Melnyk, Patrick Vermersch
Принадлежит: Centre Hospitalier Regional Universitaire de Lille CHRU, Universite Lille 2 Droit et Sante

The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts or solvates thereof, and their use.

Подробнее
Номер записи: 65
02-04-2020 дата публикации

TRICYCLIC SPIRO COMPOUND

Номер: US20200102284A1
Автор: ASADA Masaki, FUCHIBE Kazuhiro, HIGUCHI Satonori, HIROBE Masaya, KOTANI Tohru, Oikawa Ryo, TAKANO Hirotsugu, TANI Kousuke
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

A medicinal agent for the prevention and/or treatment of diseases caused by EPreceptor activation is disclosed. A compound having antagonistic activity against the EPreceptor is contained as an active ingredient in the medicinal agent. The compound represented by the following general formula (I) as defined in the specification, a salt, an N-oxide, or a solvate thereof, or a prodrug of these is useful as a medicinal component having antagonistic activity against the EPreceptor for the prevention and/or treatment of diseases caused by EPreceptor activation. 3. The compound according to claim 1 , or a salt claim 1 , an N-oxide claim 1 , or a solvate thereof claim 1 , or a prodrug thereof claim 1 , wherein at least one Ris —CONHR.4. The compound according to claim 1 , or a salt claim 1 , an N-oxide claim 1 , or a solvate thereof claim 1 , or a prodrug thereof claim 1 , wherein Lis —NHCO— claim 1 , or —CONH—.6. The compound according to claim 1 , which is any one of the following:(1) 4-[4-cyano-2-({[(2′R,4S)-6-(methylcarbamoyl)-2,3-dihydrospiro[chromene-4,1′-cyclopropan]-2′-yl]carbonyl}amino)phenyl]butanoic acid,(2) 4-{4-cyano-2-[({(2′R,4S)-6-[(cyclopropylmethyl)carbamoyl]-2,3-dihydrospiro[chromene-4,1′-cyclopropan]-2′-yl}carbonyl)amino]phenyl}butanoic acid,(3) 4-{4-cyano-2-[({(2′R,4S)-6-[(2-methoxyethyl)carbamoyl]-2,3-dihydrospiro[chromene-4,1′-cyclopropan]-2′-yl}carbonyl)amino]phenyl}butanoic acid,(4) 4-{4-cyano-2-[({(2′R,4S)-6-[(2-methyl-2-propanyl)carbamoyl]-2,3-dihydrospiro[chromene-4,1′-cyclopropan]-2′-yl}carbonyl)amino]phenyl}butanoic acid,(5) 4-[4-cyano-2-({[(2′R,4S)-6-{[(2S)-1-methoxy-2-propanyl]carbamoyl}-2,3-dihydrospiro[chromene-4,1′-cyclopropan]-2′-yl]carbonyl}amino)phenyl]butanoic acid,(6) 4-{4-cyano-2-[({(2′R,4S)-6-[(1-methyl-1H-pyrazol-3-yl)carbamoyl]-2,3-dihydrospiro[chromene-4,1′-cyclopropan]-2′-yl}carbonyl)amino]phenyl}butanoic acid,(7) 4-[4-cyano-2-({[(2′R,4S)-6-(cyclopropylcarbamoyl)-2,3-dihydrospiro[chromene-4,1′-cyclopropan]-2′-yl]carbonyl}amino) ...

Подробнее
Номер записи: 66
27-04-2017 дата публикации

MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF

Номер: US20170114080A1
Автор: "ONeill David John", Fetalvero Kristina Michelle, Narayan Sridhar, Saiah Eddine, Sengupta Shomit
Принадлежит:

The present invention provides compounds, compositions thereof, and methods of using the same. 2. The compound according to claim 1 , wherein Ris H.3. The compound according to claim 1 , wherein Ris Calkyl.4. The compound according to claim 1 , wherein Ris hydrogen.5. The compound according to claim 1 , wherein Ris —C(O)R claim 1 , —SOR claim 1 , or —C(O)N(R).6. The compound according to claim 1 , wherein Ris methyl claim 1 , —(CH)-phenyl claim 1 , or —C(O)CH.7. The compound according to claim 1 , wherein Ris —C(O)R claim 1 , —C(O)OR claim 1 , —C(O)N(R) claim 1 , —SOH claim 1 , —SON(R) claim 1 , —S(O)R claim 1 , —S(O)Ring A claim 1 , —OR or —B(OR).812.-. (canceled)13. The compound according to claim 1 , wherein L is a covalent bond.14. The compound according to claim 1 , wherein L is a straight or branched Calkylene chain optionally substituted with 1-4 fluoro groups.15. The compound according to claim 14 , wherein L is methylene claim 14 , n-butylenyl. ethylenyl claim 14 , or n-propylenyl.16. The compound according to claim 1 , wherein Ris —CF claim 1 , —OR claim 1 , or —SR.17. The compound according to claim 16 , wherein Ris isopropyl claim 16 , tert-butyl claim 16 , cyclopropyl claim 16 , cyclobutyl claim 16 , sec-butyl claim 16 , methoxyl claim 16 , or methylthioyl.18. The compound according to claim 1 , wherein Ris H.19. The compound according to claim 1 , wherein Ris methyl.2025.-. (canceled)26. A pharmaceutically acceptable composition comprising a compound according to and a pharmaceutically acceptable carrier claim 1 , adjuvant claim 1 , or vehicle.27. The composition according to in combination with an additional therapeutic agent.28. The composition according to claim 27 , wherein the additional therapeutic agent is an antiproliferative compound.29. A method for modulating Sestrin-GATOR2 interaction thereby selectively modulating mTORC1 activity indirectly in a biological sample comprising the step of contacting said biological sample with a compound ...

Подробнее
Номер записи: 67
03-05-2018 дата публикации

PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS

Номер: US20180118711A1
Автор: Cutshall Neil S., Gage Jennifer Lynn, Wheeler Thomas Neil
Принадлежит:

Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same. 170-. (canceled)72. The compound of wherein Rand Rare the same or different and independently hydrogen or Calkyl.73. The compound of wherein Rand Rare hydrogen.74. The compound of wherein Ris Calkyl.75. The compound of wherein Ris methyl.76. The compound of wherein Ris ethyl.77. The compound of wherein Ris isopropyl.78. The compound of wherein Ris substituted phenyl.79. The compound of wherein Ris 3 claim 78 ,4 claim 78 ,5-trimethoxyphenyl.80. The compound of wherein Ris 4-bromo-3 claim 78 ,5-dimethoxyphenyl.81. The compound of wherein Ris substituted or unsubstituted phenyl.82. The compound of wherein Ris 4-morpholinophenyl.83. The compound of wherein Ris 4-(1H-pyrazol-1-yl)phenyl.84. The compound of wherein Ris substituted or unsubstituted naphthyl.85. The compound of wherein Ris substituted or unsubstituted heteroaryl.86. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier or diluent.87100-. (canceled) This application is a continuation of U.S. patent application Ser. No. 13/742,199, filed Jan. 15, 2013, now pending, which is a divisional of U.S. patent application Ser. No. 12/535,598, filed Aug. 4, ...

Подробнее
Номер записи: 68
12-05-2016 дата публикации

1,3-DIAMINOCYCLOPENTANE CARBOXAMIDE DERIVATIVES

Номер: US20160130214A1
Автор: CZODROWSKI Paul, Fuchss Thomas, Leuthner Birgitta, Staehle Wolfgang, Tsaklakidis Christos
Принадлежит: Merck Patent GmBH

Compounds of the formula I 2. Compounds according to in which{'sup': '4', 'Rdenotes H, OA′, Hal or A′,'}and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.3. Compounds according to claim 1 , in which{'sub': '2', 'sup': '5', 'A denotes unbranched or branched alkyl with 1-10 C-atoms, wherein one or two non-adjacent CH- and/or CH-groups may be replaced by N- and/or O-atoms and wherein 1-7 H-atoms may be replaced by R,'}and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.4. Compounds according to claim 1 , in which{'sup': 3', '3', '3', '3, 'sub': 2', '2', 'p', '2', 'p', '2, 'Ar denotes phenyl, which is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted by Hal, CN, CON(R), [C(R)]OA, [C(R)]COOR, A, Cyc and/or OCHCyc,'}and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.5. Compounds according to claim 1 , in which{'sup': '1', 'Ardenotes phenyl or naphthyl,'}and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.6. Compounds according to claim 1 , in which{'sup': 3', '3', '3', '3', '1', '3, 'sub': 2', 'p', '2', 'n', '2', '2', '2', 'n, 'Het denotes a mono- or bicyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which is unsubstituted or mono-, di- or trisubstituted by Hal, [C(R)]OA′, [C(R)]N(R), CON(R), Het, A, [C(R)]CN and/or ═O,'}and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.7. Compounds according to claim 1 , in which{'sup': '1', 'Hetdenotes a monocyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which is unsubstituted or mono- or disubstituted by Hal, A and/or ═O,'}and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, including mixtures ...

Подробнее
Номер записи: 69
12-05-2016 дата публикации

GLYCINE TRANSPORTER INHIBITOR

Номер: US20160130278A1
Автор: ABE Kumi, Abe Masahito, Araki Yuko, Matsuda Yohei, OHTA HIROSHI, Shirokawa Shin-ichi, TAMITA Tomoko, Yamada Yousuke, Yamamoto Shuji
Принадлежит: TAISHO PHARMACEUTICAL CO., LTD

The present invention provides novel compounds of formula [IA] or pharmaceutically acceptable salts thereof: 2. The compound according to or a pharmaceutically acceptable salt thereof wherein ring A is a pyridyl group claim 1 ,{'sup': 'a', 'Ris a hydrogen atom, and'}{'sup': 'b', 'Ris a hydrogen atom.'}3. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein Aris a phenyl group optionally substituted with 1 to 3 substituents selected from substituent group 1A claim 1 , or a pyridyl group substituted with 1 to 2 substituents selected from substituent group 1A.4. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein Aris a pyridyl group substituted with 1 to 2 substituents selected from substituent group 1A.5. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein Aris a pyridyl group substituted with 1 to 2 substituents selected from a halogen atom claim 1 , a Chaloalkyl group claim 1 , a Calkylsulfonyl group claim 1 , a pyrazolyl group claim 1 , and a triazolyl group.6. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare the same or different and are each a hydrogen atom claim 1 , a halogen atom claim 1 , or a monocyclic heteroaryl group optionally substituted with a substituent selected from substituent group 4A.7. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare the same or different and are each a hydrogen atom or a halogen atom.8. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein the double line with one line being dotted is a single bond claim 1 ,{'sup': 3', '4, 'Rand Rare the same or different and are each a hydrogen atom or a halogen atom, and'}n is 1 or 2.10. The compound according to or a pharmaceutically acceptable salt thereof claim 9 , wherein Aris a phenyl group optionally substituted with 1 to 3 substituents ...

Подробнее
Номер записи: 70
03-06-2021 дата публикации

MOLECULES HAVING PESTICIDAL UTILITY, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES, RELATED THERETO

Номер: US20210161144A1
Автор: Daeuble, Demeter David A., Eckelbarger Joseph D., GRAY KAITLYN, Heemstra Ronald J., Hunter Ricky, JR. Ronald, Martin Timothy P., NOLAN ALEX, Ross, SR. John F., Trullinger Tony K., VERMEULEN NICOLAAS
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 2. A composition according to wherein said active ingredient is Abamectin.3. A composition according to wherein said active ingredient is Acephate.4. A composition according to wherein said active ingredient is Acetamiprid.5. A composition according to wherein said active ingredient is Afidopyropen.6. A composition according to wherein said active ingredient is Bifenthrin.7. A composition according to wherein said active ingredient is Chlorantraniliprole.8. A composition according to wherein said active ingredient is Chlorfenapyr.9. A composition according to wherein said active ingredient is Cyantraniliprole.10. A composition according to wherein said active ingredient is Dinotefuran.11. A composition according to wherein said active ingredient is Emamectin Benzoate.12. A composition according to wherein said active ingredient is Ethiprole.13. A composition according to wherein said active ingredient is Fluxametamide.14. A composition according to wherein said active ingredient is Imidacloprid.15. A composition according to wherein said active ingredient is Methoxyfenozide.16. A composition according to wherein said active ingredient is Oxamyl.17. A composition according to wherein said active ingredient is Pyriproxyfen.18. A composition according to wherein said active ingredient is Spinetoram.19. A composition according to wherein said active ingredient is Spiromesifen.20. A composition according to wherein said active ingredient is ...

Подробнее
Номер записи: 71
01-09-2022 дата публикации

IMMUNOREGULATORY AGENTS

Номер: US20220274926A1
Автор: Balog James Aaron, BECK Hilary Plake, Guo Weiwei, JAEN Juan Carlos, OSIPOV Maksim, POWERS Jay Patrick, REILLY Maureen Kay, SHUNATONA Hunter Paul, WALKER James Ross, Williams David K., ZIBINSKY Mikhail
Принадлежит:

Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided. 238-. (canceled)39. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient.40. A method of treating cancer claim 1 , said method comprising administering an effective amount of a compound of claim 1 , to a subject in need thereof.41. A method of claim 40 , wherein said compound is administered concurrently with claim 40 , subsequent to claim 40 , or prior to claim 40 , radiation treatment.4245-. (canceled)46. A method of claim 40 , wherein said cancer is a cancer of the prostate claim 40 , colon claim 40 , rectum claim 40 , pancreas claim 40 , cervix claim 40 , stomach claim 40 , endometrium claim 40 , brain claim 40 , liver claim 40 , bladder claim 40 , ovary claim 40 , testis claim 40 , head claim 40 , neck claim 40 , skin (including melanoma and basal carcinoma) claim 40 , mesothelial lining claim 40 , white blood cell (including lymphoma and leukemia) claim 40 , esophagus claim 40 , breast claim 40 , muscle claim 40 , connective tissue claim 40 , lung (including small-cell lung carcinoma and non-small-cell carcinoma) claim 40 , adrenal gland claim 40 , thyroid claim 40 , kidney claim 40 , or bone; or is glioblastoma claim 40 , mesothelioma claim 40 , renal cell carcinoma claim 40 , gastric carcinoma claim 40 , sarcoma (including Kaposi's sarcoma) claim 40 , choriocarcinoma claim 40 , cutaneous basocellular carcinoma claim 40 , or testicular seminoma.47. A method of claim 40 , wherein said cancer is selected from the group consisting of melanoma claim 40 , colon cancer claim 40 , pancreatic cancer claim 40 , breast cancer claim 40 , ...

Подробнее
Номер записи: 72
18-05-2017 дата публикации

SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF

Номер: US20170137374A1
Автор: COSS Christopher C., Dalton James T., DUKE Charles B., Hwang Dong-Jin, JONES Amanda, Miller Duane D., NARAYANAN Ramesh, PONNUSAMY Thamarai
Принадлежит:

This invention provides novel 3-amino propanamide selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject. 5. The SARD compound of claim 1 , wherein Qis CN.6. The SARD compound of wherein Qand Qare joined together to form a substituted or unsubstituted C-Ccarbocyclic or heterocyclic ring.8. A pharmaceutical composition comprising a SARD compound according to claim 1 , or its isomer claim 1 , pharmaceutically acceptable salt claim 1 , pharmaceutical product claim 1 , polymorph claim 1 , hydrate or any combination thereof claim 1 , and a pharmaceutically acceptable carrier.9. The pharmaceutical composition of claim 8 , wherein said composition is formulated for topical use.10. The pharmaceutical composition of claim 9 , wherein said composition is in the form of a solution claim 9 , lotion claim 9 , salve claim 9 , cream claim 9 , ointment claim 9 , lipo some claim 9 , spray claim 9 , gel claim 9 , foam claim 9 , roller stick claim 9 , cleansing soaps or bars claim 9 , emulsion claim 9 , mousse claim 9 , aerosol claim 9 , shampoo claim 9 , or any combination thereof.11. A method of treating claim 1 , suppressing claim 1 , reducing the incidence claim 1 , reducing the severity claim 1 , or inhibiting the progression of prostate cancer (PCa) and its symptoms claim 1 , or increasing the survival of a male subject suffering from prostate cancer comprising administering to said subject a therapeutically effective amount of a compound according to claim 1 , or its isomer claim 1 , ...

Подробнее
Номер записи: 73
07-08-2014 дата публикации

SARMS AND METHOD OF USE THEREOF

Номер: US20140221479A1
Автор: Dalton James T., Kearbey Jeffrey D., Miller Duane D.
Принадлежит: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

This invention is directed to a feed composition and method of affecting the carcass composition by increasing the lean mass, reducing the fat mass, and/or reducing the percent fat mass comprising SARM compounds. 2. The method of claim 1 , wherein said animal is a feedlot animal claim 1 , a beef cattle or a finishing livestock.3. The method of claim 2 , wherein said feedlot animal or finishing livestock is a pig.4. The method of claim 1 , wherein said method comprises feeding said animal a daily feed wherein said feed comprises said compound of formula IIIA.5. The method of claim 1 , wherein said method comprises feeding said animal a daily feed wherein said feed comprises a compound of formula IIIA and a beta-adrenergic agonist.6. The method of claim 5 , wherein said beta-adrenergic agonist is Ractopamine hydrochloride (Paylean®).7. The method of claim 1 , wherein said administering comprises administering said compound via an implant.8. The method of claim 7 , wherein said implant comprises a controlled release implant.9. The method of claim 7 , wherein said animal is a feedlot animal.1071. The method of claim claim 7 , wherein said animal is a pig.11. The method of claim 1 , wherein said administering comprises topical administration.12. The method of claim 11 , wherein said topical administration comprises administering a topical spray claim 11 , a topical cream or a topical ointment claim 11 , or any combination thereof.13. The method of claim 11 , wherein said animal is a feedlot animal.14. The method of claim 11 , wherein said animal is a pig. This application is a Continuation application of U.S. patent application Ser. No. 13/627,900 filed Sep. 26, 2012 which is a Continuation application of U.S. patent application Ser. No. 12/730,094 filed Mar. 23, 2010, now U.S. Pat. No. 8,309,603 which is a Continuation In Part application of U.S. patent application Ser. No. 11/785,250, filed Apr. 16, 2007, now U.S. Pat. No. 7,772,433 which is a Continuation-In-Part ...

Подробнее
Номер записи: 74
09-05-2019 дата публикации

Processes for the preparation of a diarylthiohydantoin compound

Номер: US20190135775A9
Автор: Andras Horvath, Cyril Ben Haim, Jennifer Albaneze-Walker, Johan Erwin Edmond Weerts
Принадлежит: Aragon Pharmaceuticals Inc

Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer.

Подробнее
Номер записи: 75
25-05-2017 дата публикации

MODULATORS OF THE RELAXIN RECEPTOR 1

Номер: US20170144984A1
Автор: Agoulnik Alexander, Agoulnik Irina, Chen Catherine, Ferrer-Alegre Marc, Marugan Juan Jose, Southall Noel, Xiao Jingbo, Zheng Wei
Принадлежит:

Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R, and Rare as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardiovascular disease. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the disclosure, and a method for therapeutic intervention in a facet of mammalian health that is mediated by a human relaxin receptor 1. 120-. (canceled)21. A method for therapeutic intervention in a facet of mammalian health that is mediated by a mammalian relaxin receptor 1 claim 104 , the method comprising administering to a mammal in need thereof an effective amount of a compound or salt of .2239-. (canceled)40. The method of claim 21 , whereinthe facet of mammalian health is cardiovascular disease.41. The method of claim 40 , wherein the cardiovascular disease is selected from myocardial ischemia-reperfusion injury claim 40 , cardiac fibrosis claim 40 , acute congestive heart failure claim 40 , cerebrovascular disease and stroke claim 40 , post-infarction heart claim 40 , cardiac anaphylaxis claim 40 , cerebral ischemia (stroke) claim 40 , intestinal ischemia-reperfusion injury claim 40 , systemic and pulmonary hypertension claim 40 , vascular inflammation claim 40 , hypertension claim 40 , high blood pressure; left ventricular hypertrophy (LVH); vasodilation; renal hypertension; diuresis; nephritis; natriuresis; scleroderma renal crisis; angina pectoris (stable and unstable); myocardial infarction; heart attack; coronary artery disease; coronary heart disease; cardiac arrhythmias; atrial fibrillation; portal hypertension; raised intraocular pressure; vascular restenosis; chronic hypertension; valvular disease; myocardial ischemia; acute pulmonary edema; acute coronary syndrome; hypertensive retinopathy; hypertensive pregnancy sickness; Raynaud's phenomenon; erectile dysfunction claim 40 , glaucoma claim 40 , ...

Подробнее
Номер записи: 76
23-05-2019 дата публикации

MOLECULES HAVEING PESTICIDAL UTILIY AND INTERMEDIATES, COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20190150452A1
Автор: Daeuble, Demeter David A., Eckelbarger Joseph D., GRAY KAITLYN, Heemstra Ronald J., Hunter Ricky, JR. Ronald, Martin Timothy P., NOLAN ALEX, Ross, SR. John F., Trullinger Tony K., VERMEULEN NICOLAAS
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 2. A molecule according to wherein:{'sup': '1', 'sub': 2', '5', '1', '3, '(A) Ris selected from the group consisting of H, F, Cl, Br, I, CN, NO, SF, and (C-C)haloalkyl;'}{'sup': '2', 'sub': 2', '5', '1', '3, '(B) Ris selected from the group consisting of H, F, Cl, Br, I, CN, NO, SF, and (C-C)haloalkyl;'}{'sup': '3', 'sub': 2', '5', '1', '3, '(C) Ris selected from the group consisting of H, F, Cl, Br, I, CN, NO, SF, and (C-C)haloalkyl;'}{'sup': '4', 'sub': 2', '5', '1', '3, '(D) Ris selected from the group consisting of H, F, Cl, Br, I, CN, NO, SF, and (C-C)haloalkyl;'}{'sup': '5', 'sub': 2', '5', '1', '3, '(E) Ris selected from the group consisting of H, F, Cl, Br, I, CN, NO, SF, and (C-C)haloalkyl;'}{'sup': '6', '(F) Ris H;'}{'sup': '7', '(G) Ris selected from the group consisting of F, Cl, and Br;'}{'sup': '8', '(H) Ris selected from the group consisting of F, Cl, and Br;'}{'sup': '9', '(I) Ris H;'}{'sup': '1', '(J) Qis selected from the group consisting of O and S;'}{'sup': '2', '(K) Qis selected from the group consisting of O and S;'}{'sup': '10', 'sub': 1', '3', '2', '3', '2', '3', '1', '3', '1', '3', '1', '3', '1', '3, '(L) Ris selected from the group consisting of H, (C-C) alkyl, (C-C)alkenyl, (C-C)alkynyl, (C-C)alkylO(C-C)alkyl, and (C-C)alkylOC(═O)(C-C)alkyl;'}{'sup': '11', 'sub': 2', '1', '3', '1', '3', '1', '3, '(M) Ris selected from the group consisting of H, F, Cl, Br, I, CN, NO, (C-C)alkyl, (C-C)haloalkyl, and (C-C)alkoxy ...

Подробнее
Номер записи: 77
18-06-2015 дата публикации

COMPOUNDS FOR THE TREATMENT OF MTOR PATHWAY RELATED DISEASES

Номер: US20150166477A1
Автор: ASTON Roger, MORRIS David L., Pourgholami Mohammad Hossein
Принадлежит:

The present invention relates to compounds for the treatment of mTOR (mammalian Target Of Rapamycin) pathway related diseases. Specifically, the present invention relates to the use of aminoactonitrile derivatives (AADs) in the treatment of mTOR pathway related diseases. 2. The compound of claim 1 , wherein claim 1 ,{'sup': '1', 'Ris —CN, H or halogen;'}{'sup': '2', 'Ris H or halogen;'}{'sup': '3', 'sub': '3', 'Ris —CFor halogen;'}{'sup': '4', 'sub': 3', '3', '2', '3', '3', '3, 'Ris —SCF, —SOCF, —SOCF, —OCF, or —CF;'}{'sup': '5', 'Ris H;'}{'sup': '6', 'Ris alkyl;'}X is O; andn is 1 to 5.3. The compound of or claim 1 , wherein Ris para to the amide moiety.4. The compound of any one of to claim 1 , wherein the compound of formula (I) is the (R)- or (S)-enantiomer or the racemate.5. The compound of any one of to claim 1 , wherein the compound of formula (I) is the (S)-enantiomer.10. The compound of any one of to claim 1 , wherein the one or more mTOR pathway related diseases is selected from Alzheimer's disease claim 1 , Huntington's disease claim 1 , age-related diseases claim 1 , diseases related to transplant rejection claim 1 , chronic inflammatory diseases claim 1 , diseases related to glycogen storage claim 1 , cancer claim 1 , metastasis claim 1 , systemic lupus claim 1 , diseases related to inflammation and immune activation claim 1 , anaemia claim 1 , leucopenia claim 1 , thrombocytopenia claim 1 , diseases related to stent coatings claim 1 , renal insufficiency claim 1 , obesity claim 1 , diabetes/insulin resistance claim 1 , diseases related to non-alcoholic fatty liver claim 1 , polycystic kidney claim 1 , Parkinson's disease and fibrosis.11. The compound according to claim 10 , wherein the mTOR pathway related disease is chronic inflammatory disease.12. The compound according to claim 11 , wherein the chronic inflammatory disease is rheumatoid arthritis or organ rejection after transplant.13. The compound according to claim 11 , wherein the fibrosis is ...

Подробнее
Номер записи: 78
16-06-2016 дата публикации

Therapeutic compounds

Номер: US20160168083A1
Автор: Lester R. Drewes, Mohammed Abrar Alam, Shirisha Gurrapu, Sravan K. Jonnalagadda, Venkatram R. Mereddy
Принадлежит: University of Minnesota

The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating cancer or treating autoimmune diseases or preventing transplant rejection using compounds of formula I.

Подробнее
Номер записи: 79
16-06-2016 дата публикации

DI(HETERO)ARYLAMIDES AND SULFONAMIDES, METHODS FOR THEIR PREPARATION AND THERAPEUTIC USES THEREOF

Номер: US20160168132A1
Автор: AYMAMI BOFARULL Juan, BARRIL ALONSO Xavier, GARCÍA COLLAZO Ana Maria, LAVILLA GRIFOLS Rodolfo, MARTINELL PEDEMONTE Marc, Revés Vilaplana Marc
Принадлежит: Minoryx Therapeutics S.L.

The present invention refers to compounds of formula (I): as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or prevention of conditions associated with the alteration of the activity of β-galactosidase, specially galactosidase beta-1 or GLB1, including GM1 gangliosidoses and Morquio syndrome, type B. 2. A compound for use according to wherein G is a group —C(═O)—.3. A compound for use according to anyone of and wherein Ris selected from chloro claim 1 , bromo and —CF.4. A compound for use according to anyone of to wherein Ris selected from hydrogen claim 1 , halogen claim 1 , —ORa and —Calkyl optionally substituted with 1 claim 1 , 2 or 3 groups independently selected from halogen claim 1 , hydroxy claim 1 , —Calkyl claim 1 , —N(Rb) claim 1 , methoxy claim 1 , -haloCalkyl claim 1 , -dihaloCalkyl claim 1 , -trihaloCalkyl claim 1 , halomethoxy claim 1 , dihalomethoxy claim 1 , and trihalomethoxy.5. A compound for use according to anyone of to wherein Ra and Rb are independently selected from —Calkyl claim 1 , —Ccycloalkyl claim 1 , —Caryl claim 1 , —Cheteroaryl claim 1 , and —Cheterocyclyl; said alkyl claim 1 , cycloalkyl claim 1 , aryl claim 1 , heteroaryl claim 1 , or heterocyclyl groups optionally being substituted with 1 claim 1 , 2 or 3 groups independently selected from halogen claim 1 , hydroxy claim 1 , amine claim 1 , —Calkyl claim 1 , —CN claim 1 , methoxy claim 1 , substituted aryl claim 1 , substituted heteroaryl claim 1 , -haloCalkyl claim 1 , -dihaloCalkyl claim 1 , -trihaloCalkyl claim 1 , halomethoxy claim 1 , dihalomethoxy and trihalomethoxy.6. A compound for use according to anyone of to wherein Rc and Rd are independently selected from —Calkyl claim 1 , —Caryl claim 1 , and —Cheterocyclyl; said alkyl claim 1 , cycloalkyl claim 1 , aryl or heterocyclyl groups optionally being substituted with 1 claim 1 , 2 or 3 groups independently selected from halogen claim 1 , ...

Подробнее
Номер записи: 80
21-05-2020 дата публикации

ISOXAZOLINE-SUBSTITUTED BENZAMIDE COMPOUND AND PESTICIDE

Номер: US20200155511A1
Автор: KIKUCHI Takamasa, KOMODA Mitsuaki, MITA Takeshi, MIZUKOSHI Takashi, Takii Shinji, YAOSAKA Manabu
Принадлежит: NISSAN CHEMICAL CORPORATION

A substituted alkenylbenzene compound of formula (4): 1. (canceled)2. (canceled)4. A method according to claim 3 , wherein contacting the fleas with the compound comprises orally administering the compound to a mammal.5. A method according to claim 4 , wherein the mammal is livestock.6. A method according to claim 4 , wherein the mammal is a domestic animal.7. A method according to claim 4 , wherein the mammal is a pet.8. A method according to claim 4 , wherein the mammal is a dog.9. A method according to claim 4 , wherein the mammal is a cat.11. A method according to claim 10 , wherein contacting the fleas with the compound comprises orally administering the compound to a mammal.12. A method according to claim 11 , wherein the mammal is livestock.13. A method according to claim 11 , wherein the mammal is a domestic animal.14. A method according to claim 11 , wherein the mammal is a pet.15. A method according to claim 11 , wherein the mammal is a dog.16. A method according to claim 11 , wherein the mammal is a cat. This application is a continuation of U.S. patent application Ser. No. 15/972,939, filed May 7, 2018, which is a continuation of U.S. patent application Ser. No. 15/097,002, filed Apr. 12, 2016, now U.S. Pat. No. 10,045,969, which is a continuation of U.S. patent application Ser. No. 14/568,964, filed Dec. 12, 2014, which is a continuation of U.S. patent application Ser. No. 13/850,067, filed Mar. 25, 2013, now U.S. Pat. No. 8,946,492, which is a divisional of U.S. patent application Ser. No. 13/350,297, filed Jan. 13, 2012, now U.S. Pat. No. 8,492,311, which is a divisional of U.S. patent application Ser. No. 13/166,294, filed Jun. 22, 2011, now U.S. Pat. No. 8,138,213, which is a divisional of U.S. patent application Ser. No. 12/509,859, filed Jul. 27, 2009, now U.S. Pat. No. 8,022,089, which is a divisional of U.S. patent application Ser. No. 11/514,921, filed Sep. 5, 2006, now U.S. Pat. No. 7,662,972, which is a continuation-in-part of International ...

Подробнее
Номер записи: 81
29-09-2022 дата публикации

AGONISTS OF ROR GAMMAt

Номер: US20220306630A1
Автор: "OMalley Daniel", Fink Brian E., Harikrishnan Lalgudi S., Park Peter Kinam, Purandare Ashok Vinayak, Ruan Zheming, Wan Honghe, Wei Donna D.
Принадлежит:

The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders. 14. A compound which is2,4-dichloro-3-(3-isopropyl-4-methoxyphenoxy)benzonitrile,4,6-dichloro-5-(3-isopropyl-4-methoxyphenoxy)-2-phenyl-1H-benzo[d]imidazole,N-({2,4-dichloro-3-[4-methoxy-3-(propan-2-yl)phenoxy]phenyl}methyl)-2-[(1-methanesulfonylpiperidin-4-yl)oxy]acetamide,N-({2,4-dichloro-3-[4-methoxy-3-(propan-2-yl)phenoxy]phenyl}methyl)-2-{[1-(ethanesulfonyl)piperidin-4-yl]oxy}acetamide,2-benzyl-4,6-dichloro-5-[4-methoxy-3-(propan-2-yl)phenoxy]-1H-1,3-benzodiazole,4,6-dichloro-5-[4-methoxy-3-(propan-2-yl)phenoxy]-2-[(pyridin-3-yl)methyl]-1H-1,3-benzodiazole,3,5-dichloro-4-[4-methoxy-3-(propan-2-yl)phenoxy]aniline, or{3,5-dichloro-4-[4-methoxy-3-(propan-2-yl)phenoxy]phenyl}methanolor a pharmaceutically acceptable salt thereof.15. A pharmaceutical composition comprising one or more compounds according to or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers claim 1 , diluents or excipients. This application claims the benefit of U.S. Provisional Application No. 62/883,171, filed Aug. 6, 2019, the disclosure of which is incorporated herein by reference in its entirety.The invention provides novel compounds, pharmaceutical compositions comprising the compounds, and methods of using them, for example, for the treatment or prophylaxis of certain cancers and to their use in therapy.RORgt is a key lineage-defining transcription factor involved in the differentiation of naïve T cells to Th17 and Tc17 cells. IL-17 is a signature cytokine of RORgt transactivation (Ivanov et al; 2006, 126, 1121).High IL-17 levels have been associated with various autoimmune diseases. Consequently, several groups have identified RORgt inverse agonists to decrease IL-17 ...

Подробнее
Номер записи: 82
06-06-2019 дата публикации

MOLECULES HAVING PESTICIDAL UTILITY, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES RELATED THERETO

Номер: US20190166847A1
Автор: Daeuble, Demeter David A., Eckelbarger Joseph D., GRAY KAITLYN, Heemstra Ronald J., Hunter Ricky, JR. Ronald, Martin Timothy P., NOLAN ALEX, Ross, SR. John F., Trullinger Tony K., VERMEULEN NICOLAAS
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 3. A composition comprising a molecule according to and a carrier.4. A composition comprising a molecule according to and a carrier.5. A composition according to further comprising an active ingredient.6. A composition according to further comprising an active ingredient.7lambda. A composition according to wherein said active ingredient is selected from the group consisting of acrinathrin claim 5 , allethrin claim 5 , d-cis-trans allethrin claim 5 , d-trans allethrin claim 5 , bifenthrin claim 5 , bioallethrin claim 5 , bioallethrin S-cyclopentenyl claim 5 , bioresmethrin claim 5 , cycloprothrin claim 5 , cyfluthrin claim 5 , beta-cyfluthrin claim 5 , cyhalothrin claim 5 , -cyhalothrin claim 5 , gamma-cyhalothrin claim 5 , cypermethrin claim 5 , alpha-cypermethrin claim 5 , beta-cypermethrin claim 5 , theta-cypermethrin claim 5 , zeta-cypermethrin claim 5 , cyphenothrin [(1R)-trans-isomers] claim 5 , deltamethrin claim 5 , empenthrin [(EZ)-(1R)-isomers] claim 5 , esfenvalerate claim 5 , etofenprox claim 5 , fenpropathrin claim 5 , fenvalerate claim 5 , flucythrinate claim 5 , flumethrin claim 5 , tau-fluvalinate claim 5 , halfenprox claim 5 , imiprothrin claim 5 , kadethrin claim 5 , permethrin claim 5 , phenothrin [(1R)-trans-isomer] claim 5 , prallethrin claim 5 , pyrethrins (pyrethrum) claim 5 , resmethrin claim 5 , silafluofen claim 5 , tefluthrin claim 5 , tetramethrin claim 5 , tetramethrin [(1R)-isomers] claim 5 , tralomethrin ...

Подробнее
Номер записи: 83
18-09-2014 дата публикации

COMPOUNDS AND METHODS FOR INDUCING CHONDROGENESIS

Номер: US20140271955A1
Автор: CHATTERJEE Arnab K., PAYETTE Joshua, Schultz Peter G., YANG Baiyuan, YOON Hongchul, ZHU Shoutian
Принадлежит:

Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes. 1115.-. (canceled)119. The method of claim 116 , 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.'}120. The method of claim 119 , 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.'}121. The method of wherein Ris F claim 120 , Cl claim 120 , C(O)CH claim 120 , CH claim 120 , CF claim 120 , OCH claim 120 , OEt claim 120 , OPr claim 120 , OCF claim 120 , OCHF claim 120 , CHOCH claim 120 , CHOH claim 120 , CHCHOH claim 120 , CHOHCHOH claim 120 , CHCHCHOH claim 120 , CHCHOHCHOH claim 120 , OCHC(O)OH claim 120 , or OCHC(O)NH.122. The method of claim 121 , wherein each Ris independently selected from CN claim 121 , F claim 121 , Cl claim 121 , C(O)CH claim 121 , or COH.123. The method of claim 116 , wherein:{'sup': 2', '7', '8', '9', '10', '4', '7', '8', '9', '10', '4', '7', '8', '9', '10', '4', '11', '7', '8', '4', '7', '8', '4', '11', '7', '8', '4', '7', '8', '4', '11', '7', '8', '4', '4', '4', '4, 'sub': '2', 'Ris (CRR)(CRR)OR, X(CRR)(CRR)OR, X ...

Подробнее
Номер записи: 84
13-06-2019 дата публикации

PROCESS FOR THE PREPARATION OF AMINO-PYRAZOLES

Номер: US20190177280A1
Автор: KENNEDY Jason W.J., SAMANN Christoph, VON MORGENSTERN Sascha
Принадлежит:

The present invention discloses an efficient preparation of 3-amino-1-((2,6-di-substituted)phenyl)pyrazoles. 2. Process according to wherein{'sup': '1', 'Rrepresents fluoro'}{'sup': '2', 'Rrepresents fluoro'}n represents 0,{'sup': '4', 'Rrepresents hydrogen and'}{'sup': '5', 'Rrepresents hydrogen.'}4. Process according to claim 1 , comprising (ii) and (iii).5. Process according to claim 4 , comprising (iii). The present invention discloses an efficient preparation of 3-amino-1-((2,6-di-substituted)phenyl)pyrazoles of formula (I)in which R, R, R, R, R, and n have the meanings mentioned below, via a reaction sequence of Michael addition of an acrylonitrile to a phenyl hydrazine, cyclization of the corresponding Michael adduct and subsequent oxidation of the resulting 5-amino-1-phenyl-3,4-dihydropyrazole.Compounds of formula (I) and their derivatives are important building blocks for the synthesis of bio-active compounds that can be used e.g. for the control of unwanted harmful pests.It is known, that various amido-pyrazoles have demonstrated important applications as, for example, pest control agents (e.g. WO 2014/053450 A1, WO 2015/144652 A2, WO 2015/150252 A1).The synthesis of 3-amino-1-phenyl-pyrazoles has been described in literature. The classical synthesis is a two-step process. At first, 5-amino-1-phenyl-3,4-dihydropyrazoles are prepared as intermediates by the reaction of a phenyl hydrazine with an acrylonitrile in ethanol with a large excess of NaOEt (1954, 4081965, 98, 33771998, 39, 5845). The reaction reportedly occurs via a Michael addition to give an α-cyanoethylhydrazine intermediate, which then cyclizes in situ to the 5-amino-3,4-dihydropyrazole. Subsequently, these dihydropyrazole derivatives are oxidized to the corresponding 3-amino-pyrazoles most commonly by using oxidants like DDQ (US 2007/0112034 A12002, 10, 817), p-Chloranil (WO 2013/031922 A1), MnO(2012, 55, 8211; US 2004/0116475 A1) or NBS (WO 2011/132017 A1).Another possibility is the direct ...

Подробнее
Номер записи: 85
09-07-2015 дата публикации

AGONISTS OF SRC HOMOLOGY-2 CONTAINING PROTEIN TYROSINE PHOSPHATASE-1 AND TREATMENT METHODS USING THE SAME

Номер: US20150191467A1
Автор: Chen Kuen-Feng, Shiau Chung-Wai
Принадлежит:

The present invention provides new compounds of formula I, II or III, which have Src homology-2 containing protein tyrosine phosphatase-1 (SHP-1) agonist activity. Also provided are treatment methods using the compounds of formula I, II or III. 4. A pharmaceutical composition comprising a compound as defined in any of to and a pharmacological acceptable carrier.53. A pharmaceutical composition for increasing Src homology-2 containing protein tyrosine phosphatase-1 (SHP-1) expression in a cell claims 1 , comprising a compound as defined in any of to and a pharmacological acceptable carrier.6. A pharmaceutical composition for treating a disease or condition characterized by decreased Src homology-2 containing protein tyrosine phosphatase-1 (SHP-1) claims 1 , comprising a compound as defined in any of to and a pharmacological acceptable carrier claims 1 , wherein the disease or condition is a cancer or osteoporosis.7. The pharmaceutical composition of claim 6 , wherein the cancer is hepatocellular carcinoma claim 6 , leukemia claim 6 , lung cancer claim 6 , breast cancer claim 6 , renal cancer claim 6 , thyroid cancer colon claim 6 , head or neck cancer.8. A method for increasing Src homology-2 containing protein tyrosine phosphatase-1 (SHP-1) expression in a cell claim 6 , comprising contacting the cell with an effective amount of a compound as defined in any of to or a pharmaceutical composition of .9. A method for treating a disease or condition characterized by decreased Src homology-2 containing protein tyrosine phosphatase-1 (SHP-1) expression in a subject in need thereof claim 6 , comprising administering to the subject an effective amount of a compound as defined in any of to or a pharmaceutical composition of claim 6 , wherein the disease or condition is a cancer or osteoporosis.10. The method of claim 9 , wherein the cancer is hepatocellular carcinoma claim 9 , leukemia claim 9 , lung cancer claim 9 , breast cancer claim 9 , renal cancer claim 9 , thyroid ...

Подробнее
Номер записи: 86
04-06-2020 дата публикации

DUAL MODULATORS OF FARNESOID X RECEPTOR AND SOLUBLE EPOXIDE HYDROLASE

Номер: US20200172473A1
Автор: Helmstaedter Moritz, Merk Daniel, Proschak Ewgenij, Schmidt Jurema, SCHUBERT-ZSILAVECZ Manfred
Принадлежит:

The present invention pertains to novel dual modulators of farnesoid X receptor (FXR) and soluble epoxide hydrolase (sEH). The modulators of the invention were designed to provide compounds which harbor a dual activity as agonists of FXR and inhibitors (antagonists) of sEH. The invention also provides methods for treating subjects suffering from diseases associated with FXR and sEH, such as metabolic disorders, in particular non-alcoholic fatty liver or nonalcoholic steatohepatitis (NASH). 2. The compound according to claim 1 , wherein Ris C-Calkyl claim 1 , preferably a branched alky claim 1 , more preferably —C(CH) claim 1 , preferably Ris H claim 1 , —OH or —OMe claim 1 , and preferably Ris H claim 1 , —OH or —OMe.3. The compound according to claim 1 , wherein Ris a mono or polysubstituted aryl.7. The compound according to claim 1 , which is a farnesoid X receptor (FXR) agonist and a soluble epoxide hydrolase (sEH) inhibitor.8. The compound according to claim 1 , for use in the treatment of a disease.9. The compound for use according to claim 8 , wherein the disease is a disorder associated with FXR and sEH.10. The compound for use according to claim 8 , wherein the disease is a metabolic disorder claim 8 , preferably a metabolic disorder caused by or associated with a high-fat diet.11. The compound for use according to claim 8 , wherein the disease is a liver disease claim 8 , such as non-alcoholic fatty liver disease or non-alcoholic steatohepatitis (NASH).12. A method for producing a compound according to any .13. A pharmaceutical composition comprising a compound according to claim 1 , together with a pharmaceutical acceptable carrier and/or excipient.14. A method for concomitant modulation of FXR and sEH claim 1 , the method comprising the step of administering to a subject a compound according to .15. The method according to claim 14 , wherein the subject is suffering from a disease claim 14 , preferably a metabolic disease.16. The method according to claim ...

Подробнее
Номер записи: 87
22-07-2021 дата публикации

ARYL HYDROCARBON RECEPTOR ANTAGONISTS AND METHODS OF USE

Номер: US20210220408A1
Автор: Boitano Anthony, Cooke Michael, GONCALVES Kevin A., HOBAN Megan
Принадлежит:

The disclosure relates to aryl hydrocarbon receptor antagonists as well as methods of modulating aryl hydrocarbon receptor activity and expanding hematopoietic stem cells by culturing hematopoietic stem or progenitor cells in the presence of these agents. Additionally, the disclosure provides methods of treating various pathologies, such as cancer, by administration of these aryl hydrocarbon receptor antagonists. Additionally, the disclosure provides methods of treating various pathologies in a patient by administration of expanded hematopoietic stem cells. The disclosure further provides kits containing aryl hydrocarbon receptor antagonists that can be used for the expansion of hematopoietic stem cells. The disclosure further relates to pharmaceutical compositions comprising the compounds and methods of treating or preventing a disease in which aryl hydrocarbon receptor plays a role. 2. The compound of claim 1 , wherein b is 1 and c is 0.3. The compound of any one of the preceding claims claim 1 , wherein A is an optionally substituted monocyclic ring selected from the group consisting of benzene claim 1 , pyridine claim 1 , thiazole claim 1 , piperazine claim 1 , pyrimidine claim 1 , 1 claim 1 ,2 claim 1 ,3-triazole claim 1 , pyrazole claim 1 , furan claim 1 , isoxazole claim 1 , 4H-pyridazine claim 1 , thiophene claim 1 , oxazole claim 1 , and 2H-pyridine.4. The compound of any one of the preceding claims claim 1 , wherein A is an optionally substituted bicyclic ring selected from the group consisting of benzo[d][1 claim 1 ,2 claim 1 ,3]triazole claim 1 , thieno[2 claim 1 ,3-b]pyridine claim 1 , imidazo[1 claim 1 ,2-a]pyridine claim 1 , quinolone claim 1 , pyrido[1 claim 1 ,2-a]pyrimidine claim 1 , 6 claim 1 ,7-dihydro-5H-thiazolo[4 claim 1 ,5-b]pyridine claim 1 , benzo[d]imidazole claim 1 , isoindoline claim 1 , benzo[d]isothiazole claim 1 , benzo[d]thiazole claim 1 , benzo[b]thiophene claim 1 , indoline claim 1 , and [1 claim 1 ,2 claim 1 ,4]triazolo[1 claim 1 ...

Подробнее
Номер записи: 88
18-06-2020 дата публикации

COMPOUNDS AND METHODS FOR INDUCING CHONDROGENESIS

Номер: US20200188407A1
Автор: CHATTERJEE Arnab K., PAYETTE Joshua, Schultz Peter G., YANG Baiyuan, YOON Hongchul, ZHU Shoutian
Принадлежит:

Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes. 1119.-. (canceled)121. The method of claim 120 , wherein B is NHC(O)R.122. The method of claim 120 , wherein each Rand Ris independently optionally substituted alkyl.123. The method of claim 120 , wherein Rand Rtogether with the N to which they are attached make a ring.124. The method of claim 120 , wherein Ris optionally substituted phenyl.125. The method of claim 120 , wherein the phenyl of Ris monosubstituted or disubstituted.126. The method of claim 125 , wherein substitution on the phenyl of Ris independently selected from F claim 125 , Cl claim 125 , COH claim 125 , CN claim 125 , OCH claim 125 , C(O)CH claim 125 , CF claim 125 , CH claim 125 , CHOH claim 125 , CHCHOH claim 125 , and CHCHCHOH.129. The method of claim 128 , wherein X is O or NH and A is CH—CRR—C(O)R.130. The method of claim 128 , X is NRand A is C(O) or CH.131. The method of claim 128 , wherein Ris phenyl and the phenyl of Ris monosubstituted or disubstituted.132. The method of claim 131 , wherein substitution on the phenyl is independently selected from F claim 131 , Cl claim 131 , COH claim 131 , CN claim 131 , OCH claim 131 , C(O)CH claim 131 , CF claim 131 , CH claim 131 , CHOH claim 131 , CHCHOH claim 131 , and CHCHCHOH.133. The method of claim 128 , wherein n is 0 or 1.134. The method of claim 133 , wherein Ris independently selected from Cl claim 133 , F claim 133 , CHOH claim 133 , CHNH claim 133 , OCH claim 133 , OCF claim 133 , OCHF claim 133 , CN claim 133 , NO claim 133 , COH claim 133 , and COCH.137. A pharmaceutical composition comprising a compound of claim 136 , or a pharmaceutically acceptable salt claim 136 , solvate claim 136 , polymorph claim 136 , prodrug claim 136 , ester claim 136 , metabolite claim 136 , N-oxide claim 136 , stereoisomer claim 136 , or isomer thereof claim 136 , and a pharmaceutically acceptable ...

Подробнее
Номер записи: 89
30-07-2015 дата публикации

OXIME-SUBSTITUTED AMIDE COMPOUND AND PEST CONTROL AGENT

Номер: US20150210630A1
Автор: ASAHI Miho, IMANAKA Hotaka, IWASA Motoyoshi, KUWAHARA Hidehito, MITA Takeshi, TOMIZAWA Mitsutaka, Tsuji Keisuke
Принадлежит: NISSAN CHEMICAL INDUSTRIES, LTD.

To provide a novel pesticide, especially a fungicide and a nematocide. 2. The oxime-substituted amide compound according to claim 1 , wherein:{'sup': 1', '1', '1', '1', '1', '1', '1', '1', '1', '1', '1', '1', '1', '1', '1', '1', '1, 'Gis a structure represented by any one of G-1 to G-5, G-7 to G-13, G-16, G-19, G-20, G-23, G-27, G-30 to G-33, G-41, G-43 to G-46 and G-49 to G-51;'}{'sup': 2', '2', '2', '2', '2', '2', '2', '2, 'Gis a structure represented by any one of G-1 to G-7, G-9 to G-12, G-14, G-16 and G-17;'}{'sup': '1', 'sub': 1', '4', '1', '4', '3', '6', '1', '4', '2, 'Xis a halogen atom, cyano, nitro, C-Calkyl, C-Chaloalkyl, C-Ccycloalkyl, alkoxy, haloalkoxy, alkylthio, C-Chaloalkylthio, —NH, phenyl or D-3;'}{'sup': 2', '1', '1', '1', '2, 'Xis a hydrogen atom or a halogen atom, provided that when Gis a structure represented by G-27 and Xis dihalomethyl, Xis a hydrogen atom;'}{'sup': '3', 'sub': 1', '4', '1', '4', '3', '6', '1', '4', '2, 'Xis a hydrogen atom, a halogen atom, C-Calkyl, C-Chaloalkyl, C-Ccycloalkyl, C-Calkoxy, —NHor phenyl;'}{'sup': '4', 'Xis a hydrogen atom, a halogen atom or trifluoromethyl;'}{'sup': '5', 'Xis a hydrogen atom or a halogen atom;'}{'sup': 1', '10', '11', '2, 'sub': 1', '4', '1', '4', '1', '4', '1', '4', '1', '4, 'Yis a hydrogen atom, a halogen atom, cyano, nitro, C-Calkyl, C-Chaloalkyl, C-Calkoxymethyl, E-9, alkoxy, C-Chaloalkoxy, phenoxy, C-Calkylthio or)-C(R)═NOR, or optionally forms a ring together with Y;'}{'sup': 2', '3, 'sub': 1', '4', '1', '4, 'Yis a hydrogen atom, a halogen atom, cyano, methyl, trifluoromethyl, alkoxy, C-Chaloalkoxy, phenoxy or C-Calkyothio, or may form the after-mentioned ring together with Y,'}{'sup': 2', '1', '1', '2, 'sub': 2', '2', '2', '2', '2', '2', '2, 'or Yoptionally forms, together with Y, —OCHO—, —CHCHCHCH—, —OCHCHO— or —CH═CHCH═CH— to form a 5-membered ring or a 6-membered ring together with the carbon atoms attached to Yand Y, wherein hydrogen atoms on the respective ring-constituting carbon ...

Подробнее
Номер записи: 90
18-06-2020 дата публикации

NOVEL CYSTOBACTAMIDE DERIVATIVES

Номер: US20200190020A1
Автор: Brönstrup Mark, Grandclaudon Charlotte, Herrmann Jennifer, Mollner Tim, Muller Rolf, Prochnow Hans-Peter, Ritter Antje, Testolin Giambattista
Принадлежит:

The present invention relates to novel derivatives of cystobactamides of formula (Ib) and the use thereof for the treatment or prophylaxis of bacterial infections. 2. A compound according to claim 1 , wherein Ris a hydrogen atom and Ris a group of formula —C(═O)—NH.3. A compound according to claim 1 , wherein Ris an —OMe group and Ris a group of formula —C(═O)—NHand G is substituted by a —CN group.4. A compound according to any one of the preceding claims claim 1 , wherein Q is a group of formula —C(═O)—NH— claim 1 , wherein the NH-group is bound to the phenyl group carrying R.5. A compound according to any one of the preceding claims claim 1 , wherein Ar is a phenylene group or a pyridylene group (especially wherein Ar is an unsubstituted phenylene group).7. A compound according to any one of the preceding claims claim 1 , wherein Ris a Calkyl group and wherein Ris an OH group.8. A compound according to any one of the preceding claims claim 1 , wherein A is an optionally substituted phenyl group; an optionally substituted heteroaryl group containing 5 or 6 ring atoms selected from O claim 1 , S claim 1 , N and C; an optionally substituted cycloalkyl group containing from 3 to 7 ring atoms; or an optionally substituted heterocycloalkyl group containing from 3 to 7 ring atoms selected from O claim 1 , S claim 1 , N and C; or an optionally substituted acetylenyl group; or wherein A is a group of formula —CH-A′ or —NH-A′ claim 1 , wherein A′ is an optionally substituted phenyl group; an optionally substituted heteroaryl group containing 5 or 6 ring atoms selected from O claim 1 , S claim 1 , N and C; an optionally substituted cycloalkyl group containing from 3 to 7 ring atoms; or an optionally substituted heterocycloalkyl group containing from 3 to 7 ring atoms selected from O claim 1 , S claim 1 , N and C; or an optionally substituted acetylenyl group.10. A compound according to any one of the preceding claims claim 1 , wherein E is selected from the following groups: ...

Подробнее
Номер записи: 91
06-08-2015 дата публикации

Meta-diarylaniline or meta-diarylpyridinamine compound, preparation method and medical uses thereof

Номер: US20150218088A1
Автор: Chin-Ho Chen, Lan Xie, Lianqi Sun, Na LIU
Принадлежит: Institute of Pharmacology and Toxicology of AMMS

Meta-diarylaniline or meta-diarylpyridinamine compounds, methods for preparing the same and uses thereof in manufacture of a medicament. The compounds according to the present application have strong inhibitory activity (at nM level) against wild-type and various drug-resistant HIV viral strains, exhibit good druggability, and can be easily synthesized.

Подробнее
Номер записи: 92
25-06-2020 дата публикации

MOLECULES HAVING PESTICIDAL UTILITY, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES, RELATED THERETO

Номер: US20200196607A1
Автор: Baum Erich W., Benko Zoltan L., CHOY Nakyen, Crouse Gary D., Daeuble, DeKorver Kyle A., Demeter David A., Eckelbarger Joseph D., GRAY KAITLYN, Heemstra Ronald J., Hunter Ricky, JR. Ronald, Knueppel Daniel I., Li Fangzheng, Martin Timothy P., Nissen Jeffrey, Olson Monica B., Riener Michelle, Ross, Sparks Thomas C., SR. John F., Trullinger Tony K., Vednor Peter, Wessels Frank J., Yap Maurice C.
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 2. A molecule according to wherein the carboxamido claim 1 , and the phenyl claim 1 , which are bonded to the cyclopropane claim 1 , are in the R claim 1 ,R configuration.3. A molecule according to wherein Xis a substituted or unsubstituted heterocyclyl claim 1 , wherein said heterocyclyl is selected from the group consisting of indolyl claim 1 , oxazolyl claim 1 , pyrazinyl claim 1 , pyrazolyl claim 1 , pyridazinyl claim 1 , pyridyl claim 1 , pyrimidinyl claim 1 , tetrazolyl claim 1 , thiadiazolyl claim 1 , thiazolyl claim 1 , thienyl claim 1 , triazinyl claim 1 , [1 claim 1 ,2 claim 1 ,4]triazolo[1 claim 1 ,5-c]pyrimidinyl claim 1 , triazolyl claim 1 , 2 claim 1 ,3-dihydrophthalazine-1 claim 1 ,4-dionyl claim 1 , indolinyl claim 1 , and pyrimidine-2 claim 1 ,4(1H claim 1 ,3H)-dionyl claim 1 ,{'sub': 2', '2', '1', '6', '1', '6', '1', '6', '1', '6', '2', '6', '3', '6', '3', '6, 'wherein substituents are selected from the group consisting of F, Cl, Br, I, H, CN, NH, NO, (C-C)alkoxy, (C-C)alkyl, (C-C)haloalkoxy, (C-C)haloalkyl, (C-C)haloalkenyl, (C-C)halocycloalkenyl, and (C-C)halocycloalkyl.'} This application is a continuation of, and claims the benefit of, U.S. nonprovisional application Ser. No. 16/203,690, which was filed Nov. 29, 2018, now allowed; Ser. No. 16/203,690, is a continuation of nonprovisional application Ser. No. 15/679,415, which was filed Aug. 17, 2017, and is now U.S. Pat. No. 10,219,516; Ser. No. 15/679,415 is a ...

Подробнее
Номер записи: 93
27-07-2017 дата публикации

SYNTHESIS OF AN ANTIVIRAL COMPOUND

Номер: US20170210756A1
Автор: Cagulada Amy, CHAN Johann, Chan Lina, Colby Denise A., Karki Kapil Kumar, Kato Darryl, Keaton Katie Ann, Kondapally Sudha, Levins Christopher, Littke Adam, Martinez Ruben, PCION Dominika, Reynolds Troy, Ross Bruce, Sangi Michael, Schrier Adam J., Seng Pamela, Shapiro Nathan, Siegel Dustin, Tang Donald, Taylor James G., Tripp Jonathan, Waltman Andrew W., Yu Lawrence
Принадлежит:

The present disclosure provides processes for the preparation of a compound of formula I: 115-. (canceled) This application claims priority under 35 U.S.C. §119(e) to U.S. Provisional Application Ser. No. 61/920,446 filed on Dec. 23, 2013, the entirety of which is incorporated herein by reference.The present disclosure relates generally to the field of organic synthetic methodology for the preparation of Flaviviridae virus inhibitor compounds and their synthetic intermediates.The hepatitis C virus (HCV), a member of the hepacivirus genera within the Flaviviridae family, is the leading cause of chronic liver disease worldwide (Boyer, N. et al. J Hepatol. 2000, 32, 98-112). Consequently, a significant focus of current antiviral research is directed toward the development of improved methods for the treatment of chronic HCV infections in humans (Ciesek, S., von Hahn T., and Manns, M P., Clin. Liver Dis., 2011, 15, 597-609; Soriano, V. et al, J. Antimicrob. Chemother., 2011, 66, 1573-1686; Brody, H., Nature Outlook, 2011, 474, S1-S7; Gordon, C. P., et al., J. Med. Chem. 2005, 48, 1-20; Maradpour, D., et al., Nat. Rev. Micro. 2007, 5, 453-463).Virologic cures of patients with chronic HCV infection are difficult to achieve because of the prodigious amount of daily virus production in chronically infected patients and the high spontaneous mutability of HCV (Neumann, et al., Science 1998, 282, 103-7; Fukimoto, et al., Hepatology, 1996, 24, 1351-4; Domingo, et al., Gene 1985, 40, 1-8; Martell, et al., J. Virol. 1992, 66, 3225-9). HCV treatment is further complicated by the fact that HCV is genetically diverse and expressed as several different genotypes and numerous subtypes. For example, HCV is currently classified into six major genotypes (designated 1-6), many subtypes (designated a, b, c, and so on), and about 100 different strains (numbered 1, 2, 3, and so on).HCV is distributed worldwide with genotypes 1, 2, and 3 predominate within the United States, Europe, Australia ...

Подробнее
Номер записи: 94
13-08-2015 дата публикации

COMPOUNDS FOR USE IN THE TREATMENT OF MYCOBACTERIAL INFECTIONS

Номер: US20150225388A1
Автор: Baulard Alain, BRODIN Priscille, Deprez Benoit, Sperando Olivier, Villemagne Baptiste, Villeret Vincent, WILLAND Nicolas
Принадлежит:

The present invention concerns compounds of general formula (I): 2. (canceled)3. A method of treatment of tuberculosis claim 1 , leprosy or atypical mycobacterial infection comprising administering claim 1 , to a patient in need thereof claim 1 , an effective amount of a compound according to .7. The compound according to claim 1 , characterized in that T is CO and R3 is —CHSOR′ wherein the radical R′ is tert-butyl claim 1 , methyl claim 1 , isobutyl claim 1 , isopentyl claim 1 , isohexyl claim 1 , 4-pyridinyl or 4-pyridinyl substituted by a linear C1-C4 alkyl chain.8. The compound according to chosen from the following compounds:Compound 17: 4-(2-(cyanomethyl)thiazol-4-yl)-N-isopentyl benzene sulfonamideCompound 21: 2-(4-(4-(N-isopentylsulfamoyl)phenyl)thiazol-2-yl)acetamideCompound 23: N-(3,3-dimethylbutyl)-4-(2-methylthiazol-4-yl)benzene sulfonamideCompound 24: 4-(2-methylthiazol-4-yl)-N-(2,2,2-trifluoropropyl)benzene sulfonamideCompound 25: 4-(2-methylthiazol-4-yl)-N-(2,2,3,3,3-pentafluoropropyl)benzene sulfonamideCompound 26: 4-(2-methylthiazol-4-yl)-N-(2,2,2-trifluoroethyl)benzene sulfonamideCompound 27: 4-(2-methylthiazol-4-yl)-N-(4,4,4-trifluorobutyl)benzene sulfonamideCompound 28: N-(2,2,3,3,4,4,4-heptafluorobutyl)-4-(2-methylthiazol-4-yl)benzene sulfonamideCompound 32: 4-(2-(cyanomethyl)thiazol-4-yl)-N-(3,3,3-trifluoropropyl)benzene sulfonamideCompound 33: 2-(4-(4-(N-(3,3,3-trifluoropropyl)sulfamoyl)phenyl)thiazol-2-yl)methyl acetateCompound 34: 2-(4-(4-(N-(3,3,3-trifluoropropyl)sulfamoyl)phenyl)thiazol-2-yl)ethyl acetateCompound 35: 2-(4-(4-(N-(3,3,3-trifluoropropyl)sulfamoyl)phenyl)thiazol-2-yl)isopropyl acetateCompound 36: N-isopropyl-2-(4-(4-(N-(3,3,3-trifluoropropyl)sulfamoyl)phenyl)thiazol-2-yl) acetamideCompound 38: 4-(2-(4-methylpentyl)thiazol-4-yl)-N-(3,3,3-trifluoropropyl)benzene sulfonamideCompound 39: 4-(2-(tert-butylsulfonylmethyl)thiazol-4-yl)-N-(3,3,3-trifluoropropyl)benzene sulfonamideCompound 41: 4-(4-methylthiazol-2-yl)-N-(3,3,3- ...

Подробнее
Номер записи: 95
03-08-2017 дата публикации

SPHINOGOSINE-1-PHOSPHATE RECEPTOR MODULATORS FOR TREATMENT OF CARDIOPULMONARY DISORDERS

Номер: US20170217963A1
Автор: Guerrero Miguel A., Roberts Edward, ROSEN Hugh, Urbano Mariangela
Принадлежит:

The invention provides compounds effective as sphingosine-1-phosphate receptor modulators for treatment of cardiopulmonary diseases, such as hypertension (including malignant hypertension), angina, myocardial infarction, cardiac arrhythmias, congestive heart failure, coronary heart disease, atherosclerosis, angina pectoris, dysrhythmias, cardiomyothopy (including hypertropic cardiomyothopy), heart failure, cardiac arrest, bronchitis, asthma, chronic obstructive pulmonary disease, cystic fibrosis, croup, emphysema, pleurisy, pulmonary fibrosis, pneumonia, pulmonary embolus, pulmonary hypertension, mesothelioma, ventricular conduction abnormalities, complete heart block, adult respiratory distress syndrome, sepsis syndrome, idiopathic pulmonary fibrosis, scleroderma, systemic sclerosis, retroperitoneal fibrosis, prevention of keloid formation, or cirrhosis. 3. The compound of claim 2 , wherein X is NR and L is a bond or is C(═O).4. The compound of claim 2 , wherein each of Ar claim 2 , Ar claim 2 , and Aris phenyl.6. The compound of claim 5 , wherein X is NR and L is a bond or is C(═O).7. The compound of claim 5 , wherein Aris pyridyl or quinolyl.8. The compound of claim 5 , wherein Arand Arare phenyl.10. The compound of claim 9 , wherein X is NR and L is a bond or is C(═O).11. The compound of claim 9 , wherein Aris phenyl claim 9 , Aris pyridyl or quinolyl claim 9 , Aris pyridyl or quinolyl claim 9 , or any combination thereof.13. The compound of claim 12 , wherein X is NR and L is a bond or is C(═O).14. The compound of claim 12 , wherein Arand Arare phenyl claim 12 , Aris pyridyl or quinolyl claim 12 , or any combination thereof.16. The compound of claim 15 , wherein X is NR and L is a bond or is C(═O).17. The compound of claim 15 , wherein Aris phenyl claim 15 , Aris pyridyl or quinolyl claim 15 , Aris pyridyl or quinolyl claim 15 , or any combination thereof.18. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient.19. A ...

Подробнее
Номер записи: 96
12-08-2021 дата публикации

ANTI-FIBROTIC COMPOUNDS

Номер: US20210246100A1
Автор: Miller Thomas, Papaioannou Nikolaos
Принадлежит: Certa Therapeutics Pty Ltd

Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound or composition described herein. 5. The compound of or , or a pharmaceutically acceptable salt thereof , whereinX is O or a bond;Y is O or a bond;Z is O or a bond;{'sup': 1', '2', '1', '2', '8, 'Rand Rare independently hydrogen, alkyl, alkynyl, cycloalkylalkyl, heteroarylalkyl, heterocyclyl, or heterocyclylalkyl, wherein Rand Rare each optionally substituted with 1 or 2 independent substituents R;'}{'sup': 1', '2, 'or Rand Rtogether with the atoms to which they are attached form a heterocyclyl ring;'}{'sup': 3', '3', '8, 'Ris hydrogen, alkyl, alkynyl, heteroarylalkyl, heterocyclyl, or heterocyclylalkyl, wherein Ris optionally substituted with 1 or 2 independent substituents R;'}{'sup': 6', 'c, 'sub': '2', 'each occurrence of Ris, independently, halogen, cyano, alkyl, heteroaryl, heterocyclyl, or —S(O)R;'}m is 1 or 2;{'sup': 8', 'a', 'b, 'each occurrence of Ris, independently, alkyl or NRR; and'}{'sup': a', 'b', 'c, 'each occurrence of R, R, and Ris, independently, hydrogen, alkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, and heterocyclyl.'}8. The compound of or , or a pharmaceutically acceptable salt thereof , whereinX is O or a bond;Y is O or a bond; provided that at least one of X and Y is O;{'sup': 1', '2, 'Rand Rare independently, alkyl, alkynyl, heteroarylalkyl, heterocyclyl, or heterocyclylalkyl, wherein said heteroarylalkyl, heterocyclyl, and heterocyclylalkyl are optionally substituted with 1 or 2 independent alkyl groups;'}{'sup': 6', 'c, 'sub': '2', 'each occurrence of Ris, independently, halogen, cyano, alkyl, heteroaryl, heterocyclyl, or —S(O)R;'}m is 1 or 2 ...

Подробнее
Номер записи: 97
27-11-2014 дата публикации

METHOD OF TREATING ANDROGEN RECEPTOR (AR) -POSITIVE BREAST CANCERS WITH SELECTIVE ANDROGEN RECEPTOR MODULATOR (SARMS)

Номер: US20140350102A1
Автор: Ahn Sunjoo, Dalton James T., NARAYANAN Ramesh, Steiner Mitchell S.
Принадлежит: GTx, Inc.

This invention relates to the treatment of breast cancer in a subject, for example a female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer advanced breast cancer; breast cancer that has failed SERM (tamoxifen, toremifene), aromatase inhibitor, trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and/or fulvestrant treatments; metastasis in a subject suffering from breast cancer; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound. 5. The method of claim 1 , wherein said breast cancer is a breast cancer that has failed selective estrogen receptor modulator SERM (tamoxifen claim 1 , toremifene) claim 1 , aromatase inhibitor claim 1 , trastuzumab (Herceptin claim 1 , ado-trastuzumab emtansine) claim 1 , pertuzumab (Perjeta) claim 1 , lapatinib claim 1 , exemestane (Aromasin) claim 1 , bevacizumab (Avastin) claim 1 , and/or fulvestrant treatments.10. The method of claim 6 , wherein said metastatic or advanced breast cancer is AR-positive ER-positive metastatic or advanced breast cancer.15. The method of claim 11 , wherein said refractory AR-positive breast cancer is AR-positive ER-positive refractory breast cancer.16. The method of claim 1 , wherein said AR-positive breast cancer is AR-positive ER-positive breast cancer.17. The method of claim 1 , wherein said AR-positive breast cancer is ER negative PR-negative and HER2 negative.18. The method of claim 1 , wherein said AR-positive breast cancer is ER negative PR-negative and HER2 positive.19. The method of claim 1 , wherein said AR-positive breast cancer is ER negative PR-positive and HER2 negative.20. The method of claim 1 , wherein said AR- ...

Подробнее
Номер записи: 98
14-10-2021 дата публикации

COMPOUNDS WITH ANTIMICROBIAL ACTIVITY

Номер: US20210317076A9
Автор: Ma Cong, Yang Xiao
Принадлежит:

This invention relates to compounds of formula 1, 2 or 3 3. A pharmaceutical composition for treatment or prevention of bacterial or protozoal infections claim 1 , comprising the compound of .4. The pharmaceutical composition of claim 3 , wherein said pharmaceutical composition is in the form of tablets claim 3 , capsules claim 3 , lozenges claim 3 , troches claim 3 , hard candies claim 3 , powders claim 3 , sprays claim 3 , creams claim 3 , salves claim 3 , suppositories claim 3 , jellies claim 3 , gels claim 3 , pastes claim 3 , lotions claim 3 , ointments claim 3 , aqueous suspensions claim 3 , injectable solutions claim 3 , elixirs claim 3 , or syrups.5. The pharmaceutical composition of claim 3 , wherein said pharmaceutical composition comprises 5% to 70% by weight of said compound.6Enterococcus faecalis, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter cloacae, Escherichia coliStreptococcus pneumoniae.. The pharmaceutical composition of claim 3 , wherein said bacterial or protozoal infections are caused by microorganism selected from the group consisting of claim 3 , and7. A method to inhibit NusB-NusE interaction in a microorganism claim 1 , comprising the step of contacting the compound of with said microorganism.8. The method of claim 7 , wherein said NusB is selected from NusB E81 claim 7 , NusB Y18 and NusB E75 claim 7 , and NusE is selected from NusE H15 claim 7 , NusE D19 and NusE R16.9Enterococcus faecalis, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter cloacae, Escherichia coliStreptococcus pneuroniae.. The method of claim 7 , wherein said microorganism is selected from the group consisting of claim 7 , and10. A method of treating or preventing bacterial or protozoal infections in a subject claim 1 , comprising a step of administering a therapeutically effective amount of the compound of to said subject.11. The method of claim 10 , ...

Подробнее
Номер записи: 99
13-08-2020 дата публикации

INSECTICIDAL COMPOUNDS

Номер: US20200253205A1
Автор: Edmunds Andrew, Pitterna Thomas, Stoller Andre
Принадлежит: SYNGENTA PARTICIPATIONS AG

The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests 2. The compound of formula (I) according to claim 1 , wherein in that Q is Q1.3. The compound of formula (I) according to claim 3 , wherein n1 is 2.4. The compound of formula (I) according to claim 1 , wherein in that R is hydrogen claim 1 , methyl or ethyl.6. A method of controlling insects claim 1 , acarines claim 1 , nematodes or molluscs which comprises applying to a pest claim 1 , to a locus of a pest claim 1 , or to a plant susceptible to attack by a pest an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in .7. An insecticidal claim 1 , acaricidal claim 1 , nematicidal or molluscicidal composition comprising an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in together with an agrochemically acceptable diluent or carrier.8. A composition according to which further comprises one or more additional insecticidal claim 7 , acaricidal claim 7 , nematicidal or molluscicidal compounds.9. A method of protecting useful plants from insects claim 1 , acarines claim 1 , nematodes or molluscs claim 1 , comprising applying to said plants claim 1 , to the locus thereof claim 1 , or to plant propagation material thereof claim 1 , an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in . This application is a continuation of U.S. patent application Ser. No. 16/191,145, filed 14 Nov. 2018, which is a continuation of U.S. patent application Ser. No. 15/824,099, filed 28 Nov. 2017, ...

Подробнее
Номер записи: 100