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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 12459. Отображено 100.
19-01-2012 дата публикации

Taspase1 inhibitors and their uses

Номер: US20120015990A1
Автор: Emily Cheng, James Hsieh
Принадлежит: Washington University in St Louis WUSTL

Provided herein are small molecule inhibitors of Taspase1 and methods of using the small molecule inhibitors of Taspase1 to treat neoplasm in subjects in need thereof.

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Номер записи: 1
31-05-2012 дата публикации

Hydroxy fatty acid compounds and uses thereof for disease treatment and diagnosis

Номер: US20120136057A1
Автор: Dayan Goodenowe, M. Amin Khan, Pearson W.K. Ahiahonu, Shawn Ritchie
Принадлежит: Phenomenome Discoveries Inc

A compound of formula (I): wherein R represents a hydroxy substituted C 24 -C 40 straight chain aliphatic group containing at least one double bond in the carbon chain; and at least one carbon in the chain is substituted with a hydroxy group. Such compounds are useful for detecting inflammation, inflammatory disorders and cancer in a subject, and can also be used in therapeutic applications including treatment and/or prevention of these conditions. Pharmaceutical compositions, combinations and supplements, as well as methods of treatment using the described compounds are therefore also described.

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Номер записи: 2
07-06-2012 дата публикации

Compositions and methods relating to proliferative diseases

Номер: US20120141578A1
Автор: Chandagalu D. Raghavendragowda, Gajanan S. INAMDAR, Gavin P. Robertson, Omer F. Kuzu, Subbarao V. Madhunapantula
Принадлежит: PENN STATE RESEARCH FOUNDATION

Anti-cancer compositions and methods are described herein. In particular, compositions including one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described. Methods for treatment of pathological conditions particularly cancer, in a subject using one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described herein.

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Номер записи: 3
28-06-2012 дата публикации

Amino- and amido-aminotetralin derivatives and related compounds as mu opioid receptor antagonists

Номер: US20120165360A1
Автор: Daniel D. Long, Lan Jiang, Michael R. Leadbetter, Sabine Axt, Sean G. Trapp
Принадлежит: Theravance Inc

The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

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Номер записи: 4
05-07-2012 дата публикации

Negatively birefringent polyesters and optical films

Номер: US20120170118A1
Автор: David S. Hays, David T. Yust, George W. Griesgraber, Lei Wang, Stephen A. Johnson
Принадлежит: 3M Innovative Properties Co

Presently described are multilayer optical films, oriented polyester films, negatively birefringent copolyester polymers, fluorene monomers, and polyester polymers prepared from such fluorene monomers. In one embodiment, the multilayer optical film comprises at least one first birefringent optical layer; and at least one second optical layer having a lower birefringence than the first optical layer; wherein at least one of the optical layers comprises a negatively birefringent polyester polymer comprising a backbone and repeat units comprising at least one pendent aromatic group that is conformationally locked relative to the backbone.

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Номер записи: 5
20-09-2012 дата публикации

Cytotoxic compounds

Номер: US20120238604A1
Автор: Robin Scaife
Принадлежит: Molecular Discovery Systems Ltd

The present invention relates to a compound of general formula (I) or a pharmaceutically acceptable salt or solvate or thereof. In particular, the present invention relates to a method treating diseases involving cell proliferation, migration, apoptosis, or adhesion, comprising administering to a human or non-human mammalian patient an effective amount of a compound of general formula (I) or a pharmaceutically acceptable salt or solvate or thereof.

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Номер записи: 6
27-12-2012 дата публикации

Therapeutic compounds

Номер: US20120329866A1
Автор: Bo Xu, Gerald B. Hammond, Paula J. Bates
Принадлежит: University of Louisville Research Foundation ULRF

The invention provides compounds of Formula (I): R 1 ≡R 2   (I) wherein R 1 and R 2 have any of the values or specific values defined herein, as well as compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.

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Номер записи: 7
21-03-2013 дата публикации

PROPHYLACTIC OR THERAPEUTIC AGENT FOR DIABETES OR OBESITY

Номер: US20130072491A1
Автор: Eto Yuzuru, KITAHARA Yoshiro, Yasuda Reiko
Принадлежит: AJINOMOTO CO., INC.

An object is to provide a CaSR agonist agent that has excellent CaSR agonist effects, and particularly, a pharmaceutical product that can prevent or remedy diabetes or obesity by the effect of CaSR activation. The aforementioned object is achieved by a composition that contains a compound represented by the following General Formula (I) or a salt thereof (refer to the Description for the definitions of the symbols used in the formula). 7. The method according to claim 6 , comprising administering 2-amino-3-{[(5-chloro-2-hydroxy-3-sulfophenyl)carbamoyl]amino}propanoic acid claim 6 , 2-amino-3-{[(3-chloro-4-methyl-5-sulfophenyl)carbamothioyl]amino}propanoic acid claim 6 , or 2-amino-3-{[(3-chloro-2-methyl-5-sulfophenyl)carbamoyl]amino}propanoic acid as an active component. This application is a continuation of International Patent Application No. PCT/JP2011/055124, filed on Mar. 4, 2011, and claims priority to Japanese Patent Application No. 2010-048310, filed on Mar. 4, 2010, and Japanese Patent Application No. 2010-086548, filed on Apr. 2, 2010, all of which are incorporated herein by reference in their entireties.The present invention relates to an alkylamine derivative or a salt thereof, and a pharmaceutical agent comprising the same. More particularly, the present invention relates to a prophylactic or therapeutic agent for diabetes or obesity, which comprises an alkylamine derivative or a pharmaceutically acceptable salt thereof as an active component.Energy metabolism in the body is controlled by insulin produced by pancreatic beta-cells. Insulin plays an important role in controlling the blood sugar level by affecting and promoting the peripheral tissues or cells to take up sugar from the blood. However, insulin sensitivity of the cells is reduced by continuous intake of high caloric diet, an increase in the blood sugar level as well as oversecretion of insulin proceed at the same time. As a result, pancreatic beta-cells are worn out and thus become ...

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Номер записи: 8
28-03-2013 дата публикации

AZO COMPOUNDS REDUCING FORMATION AND TOXICITY OF AMYLOID BETA AGGREGATION INTERMEDIATES

Номер: US20130078186A1
Автор: Babila Julius Tachu, Boeddrich Annett, Schiele Franziska, Schmidt Michael, Wanker Erich, Wiglenda Thomas
Принадлежит: MAX-DELBRUECK-CENTRUM FUER MOLEKULARE MEDIZIN

The present invention relates to compounds suitable as modulators of protein misfolding and/or protein aggregation. The compounds are particularly suitable as inhibitors of amyloid aggregate formation and/or modulators of amyloid surface properties, and/or as activators of degradation or reduction of amyloid aggregates. 2. The compound of claim 1 , which does not comprise a —COOH group.4. The compound of claim 1 , wherein Y is phenyl claim 1 , pyridyl such as pyrid-1-yl claim 1 , pyrid-2-yl claim 1 , pyrid-3-yl or pyrid-4-yl claim 1 , thiazolyl claim 1 , e.g. 1 claim 1 ,3-thiazolyl claim 1 , such as 1 claim 1 ,3-thiazol-2-yl or triazolyl claim 1 , e.g. 1 claim 1 ,2 claim 1 ,4-triazolyl such as 1 claim 1 ,2 claim 1 ,4-triazol-5-yl claim 1 , and particularly Y is phenyl.5. The compound of claim 1 , wherein Y is particularly unsubstituted or comprises at least one substituent which is selected from NH claim 1 , NHR claim 1 , N(R) claim 1 , OH and NO claim 1 , wherein Ris Calkyl or halo.7. The compound according to which comprises at least one detectable group.8. The compound according to claim 1 , which comprises at least one deuterium atom which is particularly a substituent of X or Y or a substituent of a group —NHor —NHR.9. The compound according to which comprises at least one F or F atom which is particularly a substituent selected from an F or F atom or a group comprising an F or F atom.10. The compound according to for use as an inhibitor of amyloid-β aggregate formation and/or as a modulator of amyloid surface properties claim 1 , and/or as an activator of degradation or reduction of amyloid-β aggregates.11. The compound for use according to any of claim 1 , wherein the disease is selected from Alzheimer's disease claim 1 , Parkinson's disease claim 1 , an amyloidosis such as αβ-amyloidosis claim 1 , primary systemic amyloidosis claim 1 , secondary systemic amyloidosis claim 1 , senile systemic amyloidosis claim 1 , familial amyloid polyneuropathy 1 claim 1 , ...

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Номер записи: 9
28-03-2013 дата публикации

NOVEL AMPHIPHILES

Номер: US20130078283A1
Автор: Venkataraman Shrinivas, Yang Yi-Yan
Принадлежит:

Disclosed herein is a compound of structure (A): In this compound, X is either O or S, Ris a rigid group, Ris a hydrophilic group such that (A) is capable of self-assembly in water, and Ris an organic group. 2. The compound of wherein X is S.3. The compound of wherein at least one of Rand Ris oligomeric or polymeric.4. The compound of wherein Rcomprises an oligoether or a polyether chain.5. The compound of wherein the oligoether or polyether chain is an oligo- or poly-oxyethylene chain.6. The compound of wherein Rand Rare the same.7. The compound of wherein Ris a hydrophobic chain.8. The compound of wherein the hydrophobic chain comprises an aliphatic hydrocarbon chain.9. The compound of wherein Rcomprises an aromatic group.10. The compound of wherein the aromatic group is carbocyclic.11. The compound of to wherein R claim 1 , Rand Rare such that the compound has a critical aggregation concentration in water of below about 100 μM.12. The compound of which is non-cytotoxic.14. The process of wherein Rand Rare not the same and the process comprises{'sup': 1', '2', '3', '1, 'sub': 2', '2', '2', '2, 'reacting R(NCX)with one of RNHand RNHin large molar excess of R(NCX);'}{'sup': '1', 'sub': '2', 'separating an intermediate adduct from excess R(NCX); and'}{'sup': 2', '3, 'sub': 2', '2, 'reacting the intermediate adduct with the other of RNHand RNHto produce the compound of structure (A).'}16. The method of wherein Ris a hydrophobic group.18. The method of additionally comprising dialysing the aqueous product so as to remove unencapsulated substance.19. The method of wherein the water soluble substance is a drug.20. The method of wherein the vesicles have a mean diameter of less than about 200 nm.21. The method of wherein Rand Rin the amphiphile are both hydrophilic.22. The method of wherein Rand Rin the amphiphile are the same.24. The method of additionally comprising dialysing the aqueous product so as to remove unencapsulated substance.25. The method of wherein the ...

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Номер записи: 10
11-04-2013 дата публикации

POLYMERIZABLE CARBAMATE AND THIOCARBAMATE COMPOUNDS, POLYMERS DERIVED FROM THEM, AND COMPOSITIONS THEREOF

Номер: US20130090443A1
Автор: Musa Osama M.
Принадлежит: ISP Investments Inc.

Carbamate and thiocarbamate compounds are described that comprise a polymerizable moiety and one or more free hydroxyl and/or thiol groups. Polymers may be obtained by polymerizing these carbamate and/or thiocarbamate compounds. The carbamate and thiocarbamate compounds, as well as the polymers they produce may be formulated into adhesive, agricultural, biocide, cleaning, coating, encapsulation, membrane, oilfield, performance chemical, and personal care compositions. 3. A composition comprising the compound of wherein said composition is an adhesive claim 1 , agricultural claim 1 , biocides claim 1 , cleaning claim 1 , coating claim 1 , encapsulation claim 1 , membrane claim 1 , oilfield claim 1 , performance chemical claim 1 , or personal care composition.5. The polymer according to having a weight-average molecular weight from about 500 Da to about 20 claim 4 ,000 claim 4 ,000 Da.7. The polymer according to wherein said polymer is a non-homopolymer synthesized by the polymerization of the first monomer and at least one second monomer different from said first monomer.8. The polymer according to having a weight-average molecular weight from about 500 Da to about 20 claim 7 ,000 claim 7 ,000 Da.9. The polymer according to wherein the non-homopolymer is an alternating claim 7 , random claim 7 , graft claim 7 , or block non-homopolymer claim 7 , an end-capped derivative thereof claim 7 , or other derivative thereof.10. The polymer according to wherein the molar percentage of said first monomer is from about 0.001 mole percent to about 99.999 mole percent of said non-homopolymer claim 7 , and said second monomer is present from about 0.001 mole percent to about 99.999 mole percent of said non-homopolymer.11. The polymer according to wherein said second monomer is selected from the group consisting of: (meth)acrylamides claim 7 , (meth)acrylates claim 7 , allyls claim 7 , benzoxanes claim 7 , cinnamyls claim 7 , epoxies claim 7 , fumarates claim 7 , maleates claim 7 , ...

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Номер записи: 11
18-04-2013 дата публикации

COATING LIQUID, METHOD FOR MANUFACTURING OPTICAL COMPONENT, AND PHOTOGRAPHIC OPTICAL SYSTEM

Номер: US20130094090A1
Автор: Kobayashi Motokazu, Sakakibara Teigo, Tanaka Hiroyuki
Принадлежит: CANON KABUSHIKI KAISHA

A coating liquid including a fluorine-containing organic magnesium compound represented by the following chemical formula (1), a method for manufacturing an optical component having an optical film obtained from the coating liquid, and a photographic optical system are disclosed: 2. The coating liquid according to claim 1 , wherein Ris (CF)CH.3. The coating liquid according to claim 1 , wherein Ris (CF)C.5. The coating liquid according to claim 4 , wherein Ris (CF)CH.6. The coating liquid according to claim 4 , wherein Ris (CF)C.7. A method for manufacturing an optical component having an optical film claim 4 , the method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'coating the coating liquid according to on a base material to form a film; and'}burning the film.8. The method according to claim 7 , wherein the optical film is made of magnesium fluoride.9. The method according to claim 7 , wherein a temperature for the burning is 150° C. or more and 200° C. or less.10. A photographic optical system claim 7 , wherein light from an object is focused with an optical member manufactured according to the method according to to form an object image. 1. Technical FieldThe present invention relates to a coating liquid, a method for manufacturing an optical component, and a photographic optical system, in particular, an optical component used as a low refractive index material excellent in an antireflection effect.2. Background ArtOn a surface of an optical component constituting an optical instrument, to improve light transmittance, an antireflection film is formed.When, in air, a low refractive index material of which refractive index nc isnc=√ng   (Formula 1)to the refractive index ng of a base material is coated at an optical film thickness of λ/4 to light having a wavelength λ, the refractive index theoretically becomes zero.A general antireflection film is formed by vacuum depositing a material having the refractive index lower than that of a base ...

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Номер записи: 12
18-04-2013 дата публикации

NOVEL THIOUREA OR UREA DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING AIDS, CONTAINING SAME AS ACTIVE INGREDIENT

Номер: US20130096138A1
Автор: Chung Koo Hwan, Han Gyoon Hee, Lee Chul Ho, Song Doo Na, You Ji Chang
Принадлежит: AVIXGEN INC.

Disclosed are novel thiourea or urea derivatives inhibitory of HIV activity. Also provided are a method for preparing the thiourea or urea derivatives, and a pharmaceutical composition for the prophylaxis or therapy of AIDS comprising the derivatives. Having high inhibitory activity against HIV, the thiourea or urea derivatives can be effectively used in the prophylaxis or therapy of AIDS. 3. The thiourea or urea derivative claim 1 , or the pharmaceutically acceptable salt of claim 1 , wherein the thiourea or urea derivative is selected from the group consisting of:1-(4-tert-butyl-benzoyl)-3-(5-hydroxy-naphthalen-1-yl)-thiourea1-(4-tert-butyl-benzoyl)-3-(3-dimethylamino-propyl)-thiourea,1-(4-tert-butyl-benzoyl)-3-(3-dimethylamino-2,2-dimethyl-propyl)-thiourea,4-tert-butyl-N-(4-ethyl-piperazin-1-carbothioyl)-benzoamide,3-(4-tert-butyl-benzoyl)-1-(2-diethylamino-ethyl)-1-methyl-thiourea,3-(4-tert-butyl-benzoyl)-1-(2-dimethylamino-ethyl)-1-methyl-thiourea,1-(4-tert-butyl-benzoyl)-3-(4-diethylamino-1-methyl-butyl)-thiourea,1-(4-tert-butyl-benzoyl)-3-(4-methyl-benzyl)-thiourea,1-(4-tert-butyl-benzoyl)-3-(2-methyl-benzyl)-thiourea,1(4 tert-butyl-benzoyl)-3-(3-propylamino-propyl)-thiourea,1(4 tert-butyl-benzoyl)-3-phenethyl-thiourea,1-(4-tert-butyl-benzoyl)-3-(4-chloro-benzyl)-thiourea,1-(4-tert-butyl-benzoyl)-3-(3-chloro-benzyl)-thiourea,1-(4-tert-butyl-benzoyl)-3-(naphthalen-2-ylmethyl)-thiourea,4-tert-butyl-N-[4-(4-fluoro-phenyl)-piperazin-1-carbothioyl]-benzamide,1-(4-tert-butyl-benzoyl)-3-cyclohexyl-thiourea,1-(4-tert-butyl-benzoyl)-3-(2-fluoro-benzyl)-thiourea,1-benzoyl-3-(naphthalen-2-ylmethyl)-thiourea,1-benzoyl-3-[2-(4-chloro-phenyl)-ethyl]-thiourea,1-benzoyl-3-(4-diethylamino-1-methyl-butyl)-thiourea,3-benzoyl-1-(2-diethylamino-ethyl)-1-methyl-thiourea,N-(4-ethyl-piperazin-1-carbothioyl)-4-methyl-benzamide,1-cyclohexyl-3-(4-methyl-benzoyl)-thiourea,1-(4-chloro-benzyl)-3-(4-methyl-benzoyl)-thiourea,1-(3-dimethylamino-propyl)-3-(4-methyl-benzoyl)-thiourea,1-(4- ...

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Номер записи: 13
30-05-2013 дата публикации

FUSED CYCLOOCTYNE COMPOUNDS AND THEIR USE IN METAL-FREE CLICK REACTIONS

Номер: US20130137763A1
Автор: Dommerholt Frederik Jan, Rutjes Floris Petrus Johannes Theodorus, van Delft Floris Louis
Принадлежит:

The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene. 116.-. (canceled)18. The compound according to claim 17 , wherein the compound is of the Formula (IIa).19. The compound according to claim 17 , wherein p is 1 and L is CH.20. The compound according to claim 17 , wherein Q is selected from the group consisting of —OR claim 17 , —N(R) claim 17 , —N(R) claim 17 , —C(O)N(R) claim 17 , —C(O)OR claim 17 , —OC(O)R—OC(O)OR claim 17 , —OC(O)N(R) claim 17 , —N(R)C(O)R claim 17 , —N(R)C(O)ORand —N(R)C(O)N(R) claim 17 , wherein Ris as defined in .21. The compound according to claim 17 , wherein Q is —OH.22. The compound according to claim 17 , wherein Ris hydrogen.23. The compound according to claim 17 , wherein Ris hydrogen or [(L)-Q].24. The compound according to claim 17 , wherein n is 0.25. The compound according to claim 19 , wherein Q is —OH claim 19 , Ris hydrogen claim 19 , Ris hydrogen or [(L)-Q] and n is 0.26. A conjugate comprising a compound according to conjugated to a label via a functional group Q.27. The conjugate according to claim 26 , wherein the label is selected from the group comprising fluorophores claim 26 , biotin claim 26 , polyethylene glycol chains claim 26 , polypropylene glycol chains claim 26 , mixed polyethylene/polypropylene glycol chains claim 26 , radioactive isotopes claim 26 , steroids claim 26 , pharmaceutical compounds claim 26 , lipids claim 26 , peptides claim 26 , glycans claim 26 , nucleotides and peptide tags ...

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Номер записи: 14
06-06-2013 дата публикации

PROCESS FOR THE SYNTHESIS OF ISOTHIOCYANATES AND DERIVATIVES THEREOF AND USES OF SAME

Номер: US20130142739A1
Автор: Cabou Jérôme, Dubois Jacques, Lacroix Damien, Marchal Alfred
Принадлежит: Auriga International

A method for synthesizing an isothiocyanate of general formula (I) 1. A method for synthesizing an isothiocyanate of general formula (I){'br': None, 'sub': 1', '4', '2, 'SCN—R—R—R\u2003\u2003(I)'}{'sub': 1', '2', '4, 'claim-text': {'br': None, 'sub': 2', '1', '4', '2, 'NH—R—R—R\u2003\u2003(II)'}, 'wherein Rand Rrepresent independently of each other an alkyl, aryl or alkylaryl group, Rrepresents a carbonyl, sulfinyl, sulfonyl, sulfide group and of its derivatives comprising a step for reaction of an amine having the general formula (II)'}{'sub': 1', '2', '4, 'wherein Rand Rrepresent independently of each other an alkyl, aryl or alkylaryl group, Rrepresents a carbonyl, sulfinyl, sulfonyl or sulfide group in the presence of carbon sulfide and of di-tert-butyl dicarbonate with formation of the corresponding aforesaid isothiocyanate.'}2. The method according to claim 1 , wherein said group Rrepresents a sulfinyl group and wherein said amine is an alkylsulfinylalkylamine.3. The method according to claim 2 , wherein said alkylsulfinylalkylamine is obtained by oxidation of alkylthioalkylamine in solution in a solvent based on trifluoroethanol.4. The method according to claim 1 , wherein said amine of general formula (II) is 4-methylsulfinylbutylamine and said corresponding formed isothiocyanate is sulforaphane.5. The method according to claim 1 , wherein Rrepresents a carbonyl group and wherein said amine comprises a keto group.6. The method according to claim 5 , wherein said amine comprising a keto group is 4-methylketobutylamine and the formed corresponding isothiocyanate is 6-isothiocyanatohexan-2-one.7. The method according claim 1 , comprising a reaction of said corresponding isothiocyanate of general formula (I) with a primary or secondary amine for forming a thiourea.8. The method according to claim 7 , wherein the amine is a primary amine having the general formula HNRRwherein Rrepresents a hydrogen atom and Ra methylsulfinylbutyl group.9. The method according to ...

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Номер записи: 15
06-06-2013 дата публикации

ANTI-VIRAL CARBAMIMIDOTHIOIC ACID ESTERS

Номер: US20130143961A1
Автор: An Jianghong, Jones Steven J., Lau Allan Sik-Yin, Law Hing-Yee, Lee Chun-Wai Davy
Принадлежит:

Carbamimidothioic acid esters of formula (I) and 2-nitro-N-[4-(pyridin-4-ylamino)phenyl]-4-(quinolin-4-ylamino)benzamide are used for the treatment of influenza, and for the inhibition of a viral RNA-dependent RNA polymerase. Formulae (I), (II). 3. The compound according to claim 1 , consisting of a compound shown in Table 2.4. A pharmaceutical composition comprising the compound of claim 1 , in admixture with a suitable pharmaceutically acceptable diluent or carrier.5. The pharmaceutical composition of claim 4 , in admixture with a medication for the treatment of influenza.6. The pharmaceutical composition of claim 5 , wherein the medication for the treatment of influenza is oseltamivir claim 5 , zanamivir claim 5 , amantadine claim 5 , or rimantadine.7. A method for the treatment or prophylaxis of influenza claim 1 , comprising administering the compound of to a patient.8. A method for the treatment or prophylaxis of influenza claim 1 , comprising administering carbamimidothioic acid claim 1 , phenyl- claim 1 , 1 claim 1 ,3-propanediyl ester or a pharmaceutically acceptable salt claim 1 , solvent claim 1 , or hydrate thereof to a patient.9. A method for the treatment or prophylaxis of influenza claim 1 , comprising administering carbamimidothioic acid claim 1 , phenyl- claim 1 , 1 claim 1 ,3-propanediyl ester claim 1 , dihydrobromide or 2-nitro-N-[4-(pyridin-4-ylamino)phenyl]-4-(quinolin-4-ylamino)benzamide to a patient.10. The method according to claim 8 , wherein the influenza is influenza A.11. The method according to claim 8 , wherein the influenza is influenza type B or C.12. The method according to claim 10 , wherein the influenza is type A group-1.13. The method according to claim 10 , wherein the influenza is type A group-2.14. The method according to claim 10 , wherein the influenza is H1N1 claim 10 , H1N2 claim 10 , H3N2 claim 10 , H5N1 claim 10 , H9N2 claim 10 , H7N3 claim 10 , or H7N7.15. The method according to claim 8 , for treatment or prophylaxis ...

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Номер записи: 16
06-06-2013 дата публикации

Adamantyl Derivatives as Therapeutic Agents

Номер: US20130143962A1
Автор: Moore Richard G., SINGH Rakesh K.
Принадлежит: Women & Infants' Hospital of Rhode Island

The present invention relates to adamantyl derivatives and their anti-cancer activity. Compounds of formulae I and II are provided as well as related methods of treatment and methods of synthesis. 2. The compound of claim 1 , wherein Ris unsubstituted or substituted C-Calkyl and Rand Rare each hydrogen.3. The compound of claim 2 , wherein Xis S and Xis 0.4. The compound of claim 3 , wherein m and n are each 1 and p is 0.5. The compound of claim 4 , wherein Ris —C(O)OR.6. The compound of claim 1 , wherein R claim 1 , Rand Rare each claim 1 , independently claim 1 , hydrogen claim 1 , nitro claim 1 , unsubstituted or substituted C-Calkyl claim 1 , unsubstituted or substituted C-Caryl claim 1 , unsubstituted or substituted heteroaryl comprising 1-4 heteroatoms selected from N claim 1 , O and S claim 1 , unsubstituted or substituted C-Calkenyl claim 1 , unsubstituted or substituted Calkynyl claim 1 , hydroxyl claim 1 , halogen claim 1 , or —NRR.7. The compound of claim 1 , wherein m claim 1 , n and p are each claim 1 , independently claim 1 , integers from 0 to 10.10. The compound of claim 9 , wherein Rand R are each claim 9 , independently claim 9 , a bond or unsubstituted or substituted C-Calkyl.11. The compound of claim 10 , wherein both (AA)and (AA) claim 10 , comprise one or more α-amino acids.12. The compound of claim 11 , wherein q and r are each claim 11 , independently claim 11 , integers from 1 to 10.13. The compound of claim 12 , wherein q and r are each claim 12 , independently claim 12 , integers from 1 to 5.14. A method for treating cancer in a subject in need of such treatment claim 1 , the method comprising administering to said subject a therapeutically effective amount of a compound of .15. The method of claim 14 , wherein the cancer is selected from the group consisting of: neuroblastoma claim 14 , ovarian cancer claim 14 , breast cancer claim 14 , cervical cancer claim 14 , endometrial cancer claim 14 , prostate cancer claim 14 , pancreatic cancer ...

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Номер записи: 17
20-06-2013 дата публикации

Acrylamide Compounds And Use Thereof For Inhibiting Apoptosis

Номер: US20130158022A1
Автор: He Kunlun, Hu Guoliang, Li Ruijun, Li Song, Li Wei, Li Xin, Liu Chunlei, Liu Juan, Long Long, TANG JIE, WANG JIE, Wang Lili, Xiao Junhai, Zheng Zhibing, Zhong Wu
Принадлежит: CHINESE PLA GENERAL HOSPITAL

The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate of the compound, and to a composition comprising the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents. The present invention also relates to use of the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, and for preventing or treating a disease or disorder associated with cardiomyocyte apoptosis. 4. The compound according to having any one of the following structures claim 1 , or their isomers claim 1 , pharmaceutically acceptable salts and solvates:(1) (2E)-3-(2-thienyl)-N-[1-(8-quinolylamino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(2) (2E)-3-(3-thienyl)-N-[1-(8-quinolylamino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(3) (2E)-3-(2-thienyl)-N-[1-(4-tolylamino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(4) (2E)-3-(2-thienyl)-N-[1-(2-methoxyanilino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(5) (2E)-3-(2-thienyl)-N-(1-benzylaminothioformylamino-2,2,2-trichloroethyl)-2-acrylamide;(6) (2E)-3-(2-thienyl)-N-(1-cyclohexylaminothioformylamino-2,2,2-trichloroethyl)-2-acrylamide;(7) (2E)-3-(2-thienyl)-N-[1-isopropylaminothioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(8) (2E)-3-(2-thienyl)-N-[1-(2-fluoroanilino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(9) (2E)-3-(2-thienyl)-N-[1-(3-isopropoxypropylamino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(10) (2E)-3-(2-thienyl)-N-[1-(2-methoxyformylanilino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(11) (2E)-3-(2-thienyl)-N-(1-cycloheptylaminothioformylamino-2,2,2-trichloroethyl)-2-acrylamide;(12) (2E)-3-(2-thienyl)-N-[1-(1-morpholinyl)thioformylamino-2,2,2- ...

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Номер записи: 18
27-06-2013 дата публикации

PHENYL CARBAMATE COMPOUNDS FOR USE IN PREVENTING OR TREATING STROKE

Номер: US20130165410A1
Автор: Choi Yong Moon
Принадлежит: Bio-Pharm Solutions Co., Ltd.

A phenyl carbamate compound; a composition for treating and/or preventing stroke containing the phenyl carbamate compound or a pharmaceutically acceptable salt thereof as an active ingredient; a method of treating and/or preventing stroke comprising administering the phenyl carbamate compound or a pharmaceutically acceptable salt thereof to a patient in need of stroke treatment; and a use of the phenyl carbamate compound or a pharmaceutically acceptable salt thereof in treating and/or preventing stroke, are provided. 3. The method according to claim 1 , wherein the compound is selected from the group consisting of:1-(2-chlorophenyl)-1-hydroxypropyl-2-carbamate,1-(2-chlorophenyl)-1-hydroxybutyl-2-carbamate,1-(2-chlorophenyl)-1-hydroxy-3-methyl-butyl-2-carbamate,1-(2-chlorophenyl)-1-hydroxyhexyl-2-carbamate,1-(2-chlorophenyl)-1-hydroxypropyl-2-N-methylcarbamate,1-(2-chlorophenyl)-1-hydroxypropyl-2-N-propylcarbamate,1-(2-chlorophenyl)-1-hydroxypropyl-2-N-isopropylcarbamate,1-(2-chlorophenyl)-1-hydroxypropyl-2-N-cyclopropylcarbamate,1-(2-chlorophenyl)-1-hydroxypropyl-2-N-cyclohexylcarbamate,1-(2-chlorophenyl)-1-hydroxypropyl-2-N-benzylcarbamate,1-(2-chlorophenyl)-1-hydroxypropyl-2-N-bicyclo[2,2,1]heptanecarbamate,1-(2,4-dichlorophenyl)-1-hydroxypropyl-2-carbamate,1-(2,6-dichlorophenyl)-1-hydroxypropyl-2-carbamate,1-(2,4-dichlorophenyl)-1-hydroxybutyl-2-carbamate,1-(2,6-dichlorophenyl)-1-hydroxybutyl-2-carbamate,1-(2,4-dichlorophenyl)-1-hydroxy-3-methyl-butyl-2-carbamate,1-(2,6-dichlorophenyl)-1-hydroxy-3-methyl-butyl-2-carbamate,1-(2,4-dichlorophenyl)-1-hydroxyhexyl-2-carbamate,1-(2,6-dichlorophenyl)-1-hydroxyhexyl-2-carbamate,1-(2-chlorophenyl)-2-hydroxypropyl-1-carbamate,1-(2-chlorophenyl)-2-hydroxypropyl-1-N-methylcarbamate,1-(2-chlorophenyl)-2-hydroxypropyl-1-N-propylcarbamate,1-(2-chlorophenyl)-2-hydroxypropyl-1-N-isopropylcarbamate,1-(2-chlorophenyl)-2-hydroxypropyl-1-N-cyclopropylcarbamate,1-(2-chlorophenyl)-2-hydroxypropyl-1-N-cyclohexylcarbamate,1-(2- ...

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Номер записи: 19
18-07-2013 дата публикации

Methods and compositions for treatment of cancer and autoimmune disease

Номер: US20130184342A1
Автор: Caroline Gardner MCPHEE, Kevin David MILLS, Muneer Gulamhusien HASHAM
Принадлежит: Jackson Laboratory

The technology described herein relates to methods of inducing cell death. The technology described herein further relates to treating conditions including cancers and autoimmune diseases comprising administering inhibitors of double strand break repair. Also described herein are inhibitors of double strand break repair and methods of screening for such inhibitors.

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Номер записи: 20
25-07-2013 дата публикации

TERPENOID DERIVATIVES OBTAINED FROM TERPENOIDS STEMING FROM RENEWABLE SOURCES

Номер: US20130190518A1
Автор: Caijo Frédéric, Crevisy Christophe, Mauduit Marc
Принадлежит: Ecole Nationale Superieure de Chimie de Rennes

The present invention relates to a process for preparing a terpenoid derivative, the process comprising a metathesis of an olefin and a terpenoid, and to terpenoid derivatives prepared with said process. 3. The process of claim 1 , wherein the terpenoid has only one double bond.4. The process of claim 1 , wherein the terpenoid has at least two double bonds.5. The process of claim 4 , the process further comprising oxidizing at least one allylic carbon of the terpenoid prior to the olefin metathesis.7. The process of claim 1 , wherein the olefin cross-metathesis is a catalyzed olefin cross-metathesis.8. The process of claim 7 , wherein the catalyst is a ruthenium Hoveyda type catalyst.11. A terpenoid derivative prepared by the process according to .14. The terpenoid derivative of claim 13 , wherein R claim 13 , R claim 13 , R claim 13 , Rare the same or different and are each independently hydrogen claim 13 , a lower alkyl claim 13 , aryl claim 13 , ketone claim 13 , ester claim 13 , ether claim 13 , amide claim 13 , or sulfonamide. Owing to both the decrease of the oil stocks and the rise of their price, and environmental aspects such as green house effect, research attention has recently been focused on the use of renewable resources isolated from agro-resources to produce various types of organic compounds, such as for example raw materials, intermediates, fine chemicals, organic polymers, and solvents (Monomers, polymers and composites from renewable resources, M. N. Belgacem and A. Gandini Eds; Elsevier, Amsterdam, 2008; A. Corma, S. Iborra, A. Velty, Chem. Rev. 2007, 107, 2411-2502.).Among the products that can be isolated from agro-resources, such as vegetable oils and sugars, terpenes and terpenoids appear particularly attractive. Terpenoids are a class of compounds formally assembled from terpene building blocks.The term “terpenes” is generally used to indicate compounds derived from five-carbon isoprene units, while the term “terpenoids” is generally used ...

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Номер записи: 21
01-08-2013 дата публикации

Inhibitors and Methods of Inhibiting Bacterial and Viral Pathogens

Номер: US20130195796A1
Автор: Allen Robert D., Amberg Sean M., Dai Dongcheng, Hruby Dennis E.
Принадлежит: SIGA TECHNOLOGIES INC.

Compounds, pharmaceutical compositions and methods for treating viral and bacterial infections, by administering certain thiourea compounds, specifically acylthiourea, carboximidoylthiourea and S-alkyl isothiourea derivatives and analogs, in therapeutically effective amounts are disclosed. 2. The composition of claim 1 , wherein Ris hydrogen.3. The composition of claim 1 , wherein Ris chloro.4. The composition of claim 1 , wherein Ris hydrogen.5. The composition of claim 1 , wherein Ris trifluoromethyl.6. The composition of claim 1 , wherein Ris amino.7. The composition of claim 1 , wherein Ris methylamino.8. The composition of claim 1 , wherein Ris hydrogen.9. The composition of claim 1 , wherein Ris methoxy.10. The composition of claim 1 , wherein Ris hydrogen.11. The composition of claim 1 , wherein the compound of Formula I is selected from the group consisting of: N-[(4-amino-3-methoxy-phenyl)carbamothioyl]-4-tert-butyl-benzamide; N-[(4-amino-2-chloro-phenyl)carbamothioyl]-4-tert-butyl-benzamide hydrochloride; 4-tert-butyl-N-[[2-chloro-4-(methylamino)phenyl]-carbamothioyl]benzamide hydrochloride; 4-tert-butyl-N-[(2-chloro-5-methyl-phenyl)-carbamothioyl]benzamide; 4-tert-butyl-N-[(2-chloro-6-methyl-phenyl)-carbamothioyl]benzamide; 4-tert-butyl-N-[[2-chloro-3-(trifluoromethyl)phenyl]-carbamothioyl]benzamide; N-[(4-amino-3-methoxy-phenyl)carbamothioyl]-4-tert-butyl-benzamide hydrochloride; 4-tert-butyl-N-[(2-chloro-3-methyl-phenyl)-carbamothioyl]benzamide; 4-tert-butyl-N-[[4-(methylamino)phenyl]-carbamothioyl]benzamide hydrochloride; 4-tert-butyl-N-[[2-chloro-4-(dimethylamino)phenyl]-carbamothioyl]benzamide hydrochloride; 4-tert-butyl-N-[[2-chloro-5-(trifluoromethoxy)phenyl]-carbamothioyl]benzamide; 4-tert-butyl-N-[[4-(3-pyridylamino)phenyl]-carbamothioyl]benzamide hydrochloride; 4-tert-butyl-N-[(2-chlorophenyl)carbamothioyl]-benzamide; 4-tert-butyl-N-(o-tolylcarbamothioyl)-benzamide; 4-tert-butyl-N-[[2-chloro-5-(trifluoromethyl)phenyl]-carbamothioyl]benzamide; N ...

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Номер записи: 22
01-08-2013 дата публикации

TRISUBSTITUTED METHYL ALCOHOLS AND THEIR POLYMERIZABLE DERIVATIVES

Номер: US20130197262A1
Автор: Rao Photon, Sabnis Ram W., Swiss Gerald F.
Принадлежит: Indicator Systems International, Inc.

Provided herein are trisubstituted methyl alcohols, preferably pH indicators that are substituted with optionally substituted aryl and or optionally substituted heteroaryl groups, and optionally include one or more polymerizable substituents. 7. The compound of claim 1 , wherein{'sup': 1', '8, 'Ris hydrogen or —OR;'}{'sup': 2', '8', '9', '2', '8', '8, 'sub': 1', '4, 'each of R-Rindependently is C-Calkyl or is -L-Rprovided that at least one of R-Ris -L-R;'}{'sup': '9', 'Ris a polymerizable group; and'}L is a covalent bond or a linker which joins the one or more polymerizable groups to oxygen atoms.8. The compound of claim 1 , wherein 1-7 of R-Rare -L-R.9. The compound of claim 1 , wherein 2-6 of R-Rare -L-R.10. The compound of claim 1 , wherein 1-6 of R-Ris C-Calkyl.11. The compound of claim 1 , wherein 1-6 of R-Ris methyl.13. The compound of claim 1 , wherein L is C-Calkylene or heteroalkylene optionally substituted with 1-10 substituents selected from the group consisting of oxo (═O) claim 1 , thio (═S) claim 1 , and C-Calkyl.15. The compound of claim 14 , wherein each Rindependently is methyl claim 14 , vinyl claim 14 , allyl claim 14 , —(CH)—OCOCH═CH claim 14 , or —(CH)—OCOC(Me)═CH claim 14 , provided that at least one Ris not methyl.16. The compound of claim 14 , wherein 1 claim 14 , 2 claim 14 , or 3 Rgroups are —(CH)—OCOC(Me)═CH.17. The compound of claim 1 , wherein at least one of R-Ris hydrogen or Ris OH. This application claims priority to U.S. provisional application Ser. No. 61/570,626, filed Dec. 14, 2011, and Ser. No. 61/698,427, filed Sep. 7, 2012. These applications are hereby incorporated by reference in their entireties.This invention relates to trisubstituted methyl alcohols that are substituted with optionally substituted aryl and or optionally substituted heteroaryl groups, which preferably act as pH indicators. This invention also relates to such trisubstituted methyl alcohols that contain one or more polymerizable functional groups so as to ...

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Номер записи: 23
22-08-2013 дата публикации

COMPOUNDS FOR MODULATING RNA BINDING PROTEINS AND USES THEREFOR

Номер: US20130217685A1
Автор: Ryder Sean
Принадлежит: University of Massachusetts

The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders. 1. A method for treating or preventing a parasitic associated state in a subject comprising administering to said subject an effective amount of an RNA binding modulatory compound , such that said parasitic associate state is treated or prevented.3. The method of claim 1 , wherein the RNA binding modulatory compound is a compound of Table 1 or Table 2 claim 1 , and pharmaceutically acceptable salts thereof.4. The method of claim 1 , wherein said subject is a plant claim 1 , an animal or a human.56-. (canceled)7. The method of claim 1 , wherein said parasitic associated state is a parasitic infestation or parasitic re-infestation or a disease caused by a parasitic infestation.8. (canceled)9. The method of claim 1 , wherein said method includes protecting plants from a parasitic infestation claim 1 , inhibiting embryogenesis in a parasite or in a subject suffering from a parasitic infestation claim 1 , or reducing parasitic burden in soil claim 1 , in plants or in an animal suffering from a parasitic infection.10. The method of claim 1 , wherein said parasite is a helminth.11. The method of claim 10 , wherein said helminth is selected from the group consisting of a cestode claim 10 , a trematode and a nematode.12. (canceled)13. A method for inhibiting embryogenesis in a parasite claim 10 , comprising contacting said parasite with an effective amount of an RNA binding modulatory compound claim 10 , such that said embryogenesis is inhibited.15. The method of claim 13 , wherein the RNA binding modulatory compound is a compound of Table 1 or Table 2 claim 13 , and pharmaceutically acceptable salts thereof.16. The method of claim 13 , wherein the parasite is present in a subject.1719-. (canceled)20. The method of claim 13 , wherein said ...

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Номер записи: 24
29-08-2013 дата публикации

Process for the preparation of lubiprostone

Номер: US20130225842A1
Автор: Julian Paul Henschke, Lizhen Xia, Yuanlian Liu, Yung-Fa Chen
Принадлежит: Individual

Processes for preparing and purifying lubiprostone are disclosed. Intermediates and preparation thereof are also disclosed.

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Номер записи: 25
05-09-2013 дата публикации

PREVENTION OF PROTEOMIC AND GENOMIC DAMAGE BY DICARBONYL SUBSTRATES OF GLO 1

Номер: US20130231387A1
Автор: Rabbani Naila, Thornalley Paul, Xue Mingzhan
Принадлежит: THE UNIVERSITY OF WARWICK

The invention concerns the role of Glo 1 in the prevention and reversal of proteomic and genomic damage by carbonyl substrates thereof and, in particular, therapeutics that promote Glo 1 production. 122-. (canceled)23. A screening method for identifying agents that prevent and/or reverse proteomic and/or genomic damage , by dicarbonyl substrates of Glo1 , by inducing the increased expression of the GLO1 gene comprising:a) providing a cell including the GLO1 gene promoter functionally coupled to the coding region of the GLO1 gene and/or the coding region of a selected reporter gene and associated transcription machinery for producing a Glo1 gene product and/or a reporter gene product;b) exposing said cell to at least one test agent;c) investigating said cell for the production of said GLO1 gene product and/or reporter gene product; andd) where said product is produced, or its amount increased, after exposure to the test agent, concluding said test agent has use in inducing the expression of Glo1 and so preventing proteomic and genomic damage by dicarbonyl substrates of Glo1.24. The method according to wherein said cell is a recombinant cell that has been transformed or transfected with a construct encoding said GLO1 gene.25. The method according to wherein said GLO1 gene comprises at least one antioxidant response element (ARE).26. The method according to wherein said GLO1 gene comprises a plurality of AREs.29. The method according to wherein said GLO1 gene comprises the wild-type promoter.30. The method according to wherein said GLO1 gene comprises an artificial promoter.32. A construct encoding the promoter region of the GLO1 gene or a recombinant version thereof claim 23 , including an artificial promoter comprising a plurality of AREs.33. The construct according to further comprising the encoding region of the GLO1 gene and/or the coding region of a gene encoding a reporter molecule functionally linked to said promoter whereby the production of Glo1 protein and/ ...

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Номер записи: 26
12-09-2013 дата публикации

PEPTIDOMIMETIC COMPOUNDS AS IMMUNOMODULATORS

Номер: US20130237580A1
Автор: NAREMADDEPALLI SEETHARAMAIAH SETTY SUDARSHAN, RAMACHANDRA MURALIDHARA, SASIKUMAR POTTAYIL GOVINDAN NAIR
Принадлежит: AURIGENE DISCOVERY TECHNOLOGIES LIMITED

The present invention relates to novel peptidomimetic compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also relates to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them. 2. The compound according to claim 1 , wherein Ris —OH claim 1 , —OCHor —OCOCH.3. The compound according to claim 1 , wherein R′ claim 1 , Rand R′ are hydrogen.4. The compound according to claim 1 , wherein Ris —C(═O)—Am—R; wherein Amis selected from Ser claim 1 , Thr claim 1 , Asp claim 1 , Trp claim 1 , Ile or Phe; and Ris same as defined in .5. The compound according to claim 1 , wherein amino acids of Amis either D or L-amino acids.12. A pharmaceutical composition comprising at least one compound according to and/or a pharmaceutically acceptable salt or a stereoisomer thereof claims 1 , and a pharmaceutically acceptable carrier or excipient.13. The pharmaceutical composition of further comprising at least one additional pharmaceutical agent wherein the said additional pharmaceutical agent is an anticancer agent claim 12 , chemotherapy agent claim 12 , or antiproliferative compound.14. A compound according to claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , for use as a medicament.15. A compound according to or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , for use as a medicament for the treatment of cancer or infectious disease.16. A method of modulating an immune response mediated by PD-1 signaling pathway in a subject claim 1 , comprising administering to the subject therapeutically effective amount of compound according to such that the immune response in the subject is modulated.17. A method of inhibiting growth of tumour cells ...

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Номер записи: 27
12-09-2013 дата публикации

ALKYLAMINE DERIVATIVE

Номер: US20130237702A1
Автор: Okamatsu Toru, Sugiki Masayuki, Taniguchi Shinya, YANO Tetsuo
Принадлежит: AJINOMOTO CO., INC.

A composition containing a compound represented by General Formula (I) below (see the definition in the specification for the symbols in the formula) or a salt thereof has an excellent CaSR agonistic effect and provides a pharmaceutical agent, a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation as well as seasonings and an agent for imparting kokumi. 3. A pharmaceutical agent comprising the compound or a pharmaceutically acceptable salt thereof according to or as an active ingredient.6. The pharmaceutical agent according to claim 3 , which is a prophylactic or therapeutic agent for a disease that is ameliorated through CaSR activation.7. The pharmaceutical agent according to claim 3 , which is a prophylactic or therapeutic agent for hyperparathyroidism.8. The pharmaceutical agent according to claim 3 , which is a prophylactic or therapeutic agent for diarrhea.9. The pharmaceutical agent according to claim 3 , which is a prophylactic or therapeutic agent for peptic ulcer.10. Seasonings comprising the compound according to either one of and or an edible salt thereof as an active ingredient.11. A kokumi-imparting agent comprising the compound according to either one of and or an edible salt thereof as an active ingredient. The present invention relates to an alkylamine derivative or a salt thereof, and a pharmaceutical agent comprising the same. More particularly, the present invention relates to a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation, a prophylactic or therapeutic agent for hyperparathyroidism, diarrhea and peptic ulcer, and seasonings and an agent for imparting kokumi, which have an alkylamine derivative or a pharmaceutically acceptable salt thereof as an active ingredient.The calcium receptor, also called the calcium sensing receptor (also referred to as “CaSR”), was cloned from bovine thyroid in 1993 as G-protein ...

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Номер записи: 28
19-09-2013 дата публикации

Synthetic Ion Channels

Номер: US20130244944A1
Автор: Li Xiang, Yang Dan, Zha Huiyan
Принадлежит:

Provided herein are self-assembling compounds that can form ion channels in lipid bilayers or cell membranes and ion-channel-forming compositions comprising the self-assembling compounds. Also provided are methods of making and using the ion channels formed from a plurality of molecules of the self-assembling compounds. Further, provided are methods of treating or preventing conditions and diseases that are related to the dysfunction of ion channels, including chloride channels. 2. The self-assembling compound of claim 1 , wherein Y is a monovalent claim 1 , divalent claim 1 , trivalent claim 1 , tetravalent claim 1 , pentavalent or hexavalent linking group formed by removing one claim 1 , two claim 1 , three claim 1 , four claim 1 , five and six hydrogen atoms respectively from an unsubstituted or substituted hydrocarbon or carbocycle.3. The self-assembling compound of claim 1 , wherein at least one of Zor Zis S or NR'.4. The self-assembling compound of claim 1 , wherein at least one of A claim 1 , B claim 1 , and D is O or S.5. The self-assembling compound of claim 1 , wherein each of A and D is a bond.6. The self-assembling compound of claim 1 , wherein each of B claim 1 , B claim 1 , and Bis independently NH.7. The self-assembling compound of claim 1 , wherein X is hydrocarbyl or substituted hydrocarbyl.10. The self-assembling compound of claim 9 , wherein at least one of Zor Zis S or NR.11. The self-assembling compound of claim 9 , wherein at least one of A claim 9 , B claim 9 , C claim 9 , and D is O or S.12. The self-assembling compound of claim 9 , wherein each of B claim 9 , B claim 9 , and Bis independently NH.13. A composition claim 9 , comprising a cell membrane and a plurality of molecules of the self-assembling compound of .14. The composition of claim 13 , wherein the cell membrane comprises a lipid bilayer.15. The composition of claim 14 , wherein the plurality of molecules self-assemble to form an anion channel across the thickness of the lipid ...

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Номер записи: 29
19-09-2013 дата публикации

Process for preparing 4-cyclohexyl-2-methyl-2-butanol

Номер: US20130245132A1
Автор: Klaus Ebel, Martin Bock, Ralf Pelzer, Stefan Rüdenauer
Принадлежит: BASF SE

Process for preparing 4-cyclohexyl-2-methyl-2-butanol The present invention relates to a process for preparing 4-cyclohexyl-2-methyl-2-butanol. The process comprises the following steps: a) reaction of styrene with isopropanol at elevated temperature to obtain 4-phenyl-2-methyl-2-butanol, and b) heterogeneously catalyzed hydrogenation of 4-phenyl-2-methyl-2-butanol over a catalyst suitable for ring hydrogenation of aromatics.

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Номер записи: 30
19-09-2013 дата публикации

METHOD FOR PRODUCING ISOTHIOCYANATE COMPOUND

Номер: US20130245305A1
Автор: Iwamoto Shunsuke, Nakano Satoshi, Takada Junko
Принадлежит: NISSAN CHEMICAL INDUSTRIES, LTD.

The object of the present invention is to provide a novel method for producing an isothiocyanate compound having a carboxyl group(s) by a reaction of the corresponding amino compound having a carboxyl group(s), thiocarbonyldiimidazole and a base, in one step with high purity. 2: The method of claim 1 , wherein A is a Caromatic hydrocarbon group that is unsubstituted or substituted with one or more halogen atoms claim 1 , one or more nitro groups claim 1 , one or more cyano groups claim 1 , one or more Calkyl groups claim 1 , one or more protected hydroxy groups claim 1 , one or more Calkoxy groups claim 1 , one or more di Calkylamino groups claim 1 , one or more protected amino groups claim 1 , one or more protected mono Calkylamino groups claim 1 , one or more Calkylcarbonyl groups or one or more Calkoxycarbonyl groups claim 1 , and B is a single bond.3: The method of claim 2 , wherein A is a Caromatic hydrocarbon group that is unsubstituted or substituted with one or more halogen atoms or one or more nitro groups.4: The method of claim 3 , wherein m is 1 and n is 1.5: The method of claim 4 , wherein A is a phenylene group that is unsubstituted or substituted with one or more halogen atoms or one or more nitro groups.6: The method of claim 1 , wherein the base is a tertiary amine.7: The method of claim 6 , wherein the base is a tri Calkylamine.8: The method of claim 7 , wherein the base is triethylamine.9: The method of claim 1 , wherein the solvent is a halogenated hydrocarbon.10: The method of claim 9 , wherein the solvent is methylene chloride.11: The method of claim 1 , wherein the amino compound comprising a carboxyl group is reacted with thiocarbonyldiimidazole in the solvent in the presence of the base claim 1 , followed by a treatment with an acidic aqueous solution.12: The method of claim 11 , wherein the acidic aqueous solution is hydrochloric acid.13: The method of claim 12 , wherein after the treatment with hydrochloric acid claim 12 , without a liquid ...

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Номер записи: 31
19-09-2013 дата публикации

PRODUCTION OF FATTY ACIDS AND DERIVATIVES THEREOF

Номер: US20130245339A1
Автор: Berry David, BRUBAKER Shane, Church George, DEL CARDAYRE Stephen B., Friedman Lisa, HU Zhihao, Keasling Jay D., Schirmer Andreas, Somerville Chris
Принадлежит:

Compositions and methods for production of fatty alcohols using recombinant microorganisms are provided as well as fatty alcohol compositions produced by such methods. 1. A method of producing a fatty alcohol composition in a recombinant microorganism , comprising the steps of:(a) genetically engineering a microorganism to comprise a nucleic acid sequence encoding a polypeptide having acetyl-CoA carboxylase activity (EC 6.4.1.2), and a nucleic acid sequence encoding a polypeptide having fatty alcohol forming activity, resulting in a recombinant microorganism;(b) culturing the recombinant microorganism in a culture medium containing a carbon source under conditions effective to express the acetyl-CoA carboxylase polypeptide and the polypeptide having fatty alcohol forming activity, wherein a fatty alcohol composition is produced by said cultured recombinant microorganism; and(c) optionally recovering the fatty alcohol composition from the culture medium.2. The method of claim 1 , further comprising genetically engineering said microorganism to comprise at least one nucleic acid sequence encoding a polypeptide having thioesterase activity claim 1 , wherein said thioesterase polypeptide is expressed.3. The method of claim 1 , wherein said polypeptide having fatty alcohol forming activity is (i) a fatty alcohol forming acyl-CoA reductase (FAR claim 1 , EC 1.1.1.*) claim 1 , or (ii) an acyl-CoA reductase (EC 1.2.1.50) and an alcohol dehydrogenase (EC 1.1.1.1).4. The method of claim 2 , wherein said polypeptide having fatty alcohol forming activity is (i) a fatty alcohol forming acyl-CoA reductase (FAR claim 2 , EC 1.1.1.*) claim 2 , or (ii) an acyl-CoA reductase (EC 1.2.1.50) and an alcohol dehydrogenase (EC 1.1.1.1).5. The method of claim 4 , wherein said polypeptide having fatty alcohol forming activity is a fatty alcohol forming acyl-CoA reductase.6. The method of claim 1 , wherein said the fatty alcohol composition comprises one or more of saturated or unsaturated ...

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Номер записи: 32
03-10-2013 дата публикации

RADIOFLUORINATED COMPOUNDS AND THEIR PREPARATION

Номер: US20130259802A1
Автор: ARSTAD ERIK, GLASER MATTHIAS EBERHARD
Принадлежит: HAMMERSMITH IMANET LIMITED

The present invention provides a process for [F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [F]-labelled prosthetic groups. [F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided. 126-. (canceled)29. A method of wherein the diagnostic device is a Positron Emission Tomography scanner.37. Radiofluorination kit of further comprising a compound of formula (8):{'br': None, 'sup': '2', 'sub': '2', 'RNH\u2003\u2003(8)'}{'sup': '2', 'wherein Rdenotes a bio-molecule residue having at least one free amino function.'} The present invention relates to processes and reagents for [F]-fluorination, particularly of peptides. The resultant [F]-labelled compounds are useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET).Compounds labelled with short-lived positron emitting radionuclides are used for in vivo studies of human and non-human physiology. In particular, radiolabelled bioactive compounds which selectively interact with specific cell types are useful for the delivery of radioactivity to target tissues. The applications of bioactive compounds such as peptides and proteins, including antibodies and fragments of peptides are useful for receptor imaging. For example, radiolabelled peptides have significant potential for the delivery of radionuclides to the receptors expressed on cells of tissues, e.g. in tumours, infarcts and infected tissues for diagnosis, radiotherapy and monitoring of treatment. PET is a high resolution, non-invasive, imaging technique which has gained increased importance in the recent years for the visualisation of human disease.In PET, F is one of the most widely used ...

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Номер записи: 33
03-10-2013 дата публикации

Therapeutic Compounds for Protozoal and Microbial Infections and Cancer

Номер: US20130261133A1
Автор: Bolstad David Brian, Hoody John Howard
Принадлежит: The University of Montana

The compounds of the invention exhibit antiprotozoal, antimicrobial, and anticancer properties that are useful for the treatment or prevention of infections or cancer in a patient (e.g., a human). For example, the compounds and methods described herein can be used for the treatment or prevention of protozoal infections such as leishmaniasis, malaria, and infections, bacterial infections such as and , and cancers such as breast, colon, lung, or prostate cancer. The invention further provides methods of synthesizing such compounds as well as kits useful for administering the compounds. 2. The compound of claim 1 , wherein said compound is selected from the group consisting of (3S claim 1 ,8R)-8-hydroxyheptadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8R)-8-hydroxyheptadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8S)-8-hydroxyheptadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3S claim 1 ,8R)-8-hydroxyhexadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3S claim 1 ,8S)-8-hydroxyhexadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8R)-8-hydroxyhexadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8S)-8-hydroxyhexadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3S claim 1 ,8R)-8-hydroxypentadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3S claim 1 ,8S)-8-hydroxypentadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8R)-8-hydroxypentadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8S)-8-hydroxypentadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3S claim 1 ,8R)-8-hydroxytetradeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3S claim 1 ,8S)-8-hydroxytetradeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8R)-8-hydroxytetradeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8S)-8-hydroxytetradeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3S claim 1 ,8R)-8-hydroxytrideca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3S claim 1 ,8S)-8-hydroxytrideca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8R)-8-hydroxytrideca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 , ...

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Номер записи: 34
03-10-2013 дата публикации

PHENOXYPROPANOL DERIVATIVES AND THEIR USE IN TREATING CARDIAC AND CARDIOVASCULAR DISEASES

Номер: US20130261178A1
Автор: Baker Jillian Glenda, Daras Etienne, Fischer Peter Martin, Fromont Christophe, Hill Stephen John, Jadhav Gopal, Kellam Barrie, Mistry Shailesh
Принадлежит:

A compound of formula I-0, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: 2. The compound as claimed in wherein Ris selected from unsubstituted and substituted Ccycloalkyl claim 1 , Ccycloalkyl-Calkyl claim 1 , Calkyl claim 1 , Caryl-Calkyl claim 1 , Calkoxy-Caryl-Calkyl.3. The compound as claimed in wherein Xis selected from CO claim 1 , CS claim 1 , SOand a single bond.4. The compound as claimed in wherein Rand Rare selected from ROZO as hereinbefore defined claim 1 , m- claim 1 ,p-(OCH)or o- claim 1 , m- or p-OH claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , NH claim 1 , R claim 1 , OR claim 1 , or CFor a combination thereof.12. A process for the preparation of a compound of formula I-0 or subformulae as defined in .14. A composition comprising a therapeutically effective amount of a compound of formula I-0 or subformulae or its pharmaceutically acceptable salt and physiologically hydrolysable derivative as defined in in association with one or more pharmaceutical carriers or diluents.15. The use of a compound of formula I-0 or subformulae or pharmaceutically acceptable salt or composition as defined in in the prevention or treatment of a condition selected from ischaemic heart disease claim 1 , hypertension and heart failure claim 1 , more preferably with concomitant respiratory disease claim 1 , in particular asthma or COPD.16. A method of treating a condition selected from ischaemic heart disease (also known as myocardial infarction or angina) claim 1 , hypertension and heart failure claim 1 , restenosis and cardiomyopathy claim 1 , more preferably with concomitant respiratory disease claim 1 , in particular asthma or COPD claim 1 , said method comprising administering to a subject in need thereof claim 1 , a compound of formula I-0 or subformulae or pharmaceutically acceptable salt or composition thereof as defined in in an amount sufficient to treat the condition.17. A method of ...

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Номер записи: 35
17-10-2013 дата публикации

PREMATURE-TERMINATION-CODONS READTHROUGH COMPOUNDS

Номер: US20130274283A1
Автор: BERTONI Carmen, DAMOISEAUX Robert, DU Liutao, GATTI Richard A., Jung Michael, KU Jin-Mo, LAI Chih-Hung
Принадлежит: The Regents of the University of California

Premature termination codons readthrough compounds, composition thereof, and methods of making and using the same are provided. 1. A system for high throughput assay for readthrough compound having the ability to read through premature termination codons (PTCs) in RNA , comprising high throughput reading trays and wells containing a plasmid ,wherein the plasmid comprises a fragment of ATM gene that contains a PTC mutation, which fragment being flanked by a sequence that initiates transcription of:a) a myc epitope,b) the ATM fragment, andc) a V5 epitope;wherein the assay is based on a coupled protein transcription/translation (PTT) reaction that is driven by the plasmid;wherein the reading trays are coated with an antibody to the myc epitope; andwherein an antibody to V5 is provided for attaching to readthrough proteins expressing the V5 epitope.2. The system of claim 1 , wherein the V5 epitope is conjugated to horseradish peroxidase.3. The system of claim 1 , further comprising a robot.4. A method of screening for readthrough compounds having the ability to read through premature termination codons (PTCs) in RNA claim 1 , comprising: a) a myc epitope,', 'b) the ATM fragment, and', 'c) a V5 epitope;, 'providing a plasmid template to a reaction well having a test compound to cause a coupled protein transcription/translation (PTT) reaction to occur to generate a PTT reaction product, the plasmid template comprising a fragment of ATM gene that contains a PTC mutation, which fragment being flanked by a sequence that initiates transcription ofadding the PTT reaction product to high throughput reading trays, which are coated with an antibody to the myc epitope to capture a protein fragment of the fragment of ATM gene,adding an antibody to the V5 epitope (V5 antibody) to wells in the reading trays,detecting the attachment of the V5 antibody to proteins in the PTT product, andidentifying the test compound as a readthrough compound if the attachment of the V5 antibody to ...

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Номер записи: 36
31-10-2013 дата публикации

INHIBITORS OF BETA-SECRETASE

Номер: US20130289050A1
Автор: BUKHTIYAROV Yuri, Cacatian Salvacion, Dillard Lawrence Wayne, DORNER-CIOSSEK Cornelia, FUCHS Klaus, Jia Lanqi, Lala Deepak S., Morales-Ramos Angel, RAST Georg, Reeves Jonathan, Singh Suresh B., Venkatraman Shanker, Xu Zhenrong, YUAN Jing, Zhao Yi, ZHENG Yajun
Принадлежит:

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates. 2. A compound according to or a pharmaceutically acceptable salt thereof for use as a medicament.3. A pharmaceutical composition comprising at least one compound according to or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable adjuvant claim 1 , diluent and/or carrier.4. A compound according to or a pharmaceutically acceptable salt thereof for use in the treatment of a BACE1 mediated disorder or disease.5. A compound or a pharmaceutically acceptable salt thereof for use according to claim 4 , wherein the BACE1 mediated disorder or disease is selected from the group consisting of a neurodegenerative disorder claim 4 , cognitive decline claim 4 , cognitive impairment claim 4 , dementia claim 4 , and disease characterized by the production of β-amyloid deposits or neurofibrillary tangles.6. A compound or a pharmaceutically acceptable salt thereof for use according to claim 5 , wherein the disorder or disease is selected from the group consisting of Alzheimer's disease claim 5 , Trisomy 21 (Down Syndrome) claim 5 , Hereditary Cerebral Hemorrhage with Amyloidosis of the Dutch-type (HCHWA-D) claim 5 , senile dementia claim 5 , cerebral amyloid angiopathy claim 5 , degenerative dementia claim 5 , dementias of mixed vascular and degenerative origin claim 5 , dementia associated with Parkinson's disease claim 5 , dementia associated with progressive supranuclear palsy claim 5 , dementia associated with cortical basal degeneration claim 5 , diffuse Lewy body type of Alzheimer's disease claim 5 , dry age related ...

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Номер записи: 37
07-11-2013 дата публикации

GGA AND GGA DERIVATIVES COMPOSITIONS THEREOF AND METHODS FOR TREATING NEURODEGENERATIVE DISEASES INCLUDING PARALYSIS INCLUDING THEM

Номер: US20130296323A1
Автор: Argade Ankush B., Datwani Akash, Ermini Florian, Pan Yonghua, Serizawa Hiroaki, Spencer Natalie
Принадлежит: COYOTE PHARMACEUTICALS, INC.

This invention relates to geranylgeranyl acetone (GGA) derivatives and the use of GGA, its isomers, and GGA derivatives in methods for inhibiting neural death, increasing neural activity, increasing axon growth and cell viability, and increasing the survival rate of subjects administered the GGA or GGA derivatives. 3. A novel compound of Table 1 or a pharmaceutically acceptable salt thereof.4. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient.5. A pharmaceutical composition comprising a sufficient amount of 5E claim 1 , 9E claim 1 , 13E geranylgeranyl acetone or a GGA derivative of claim 1 , and optionally at least one pharmaceutical excipient claim 1 , wherein the sufficient amount is an amount which provides for a dosing of about 1 mg/kg/day to about 12 mg/kg/day to the patient.6. The pharmaceutical composition of claim 5 , wherein the 5E claim 5 , 9E claim 5 , 13E geranylgeranyl acetone is synthetic 5E claim 5 , 9E claim 5 , 13E geranylgeranyl acetone.7. A composition for increasing the expression and/or release of one or more neurotransmitters from a neuron at risk of developing pathogenic protein aggregates associated with AD or ALS claim 5 , said composition comprising a protein aggregate inhibiting amount of GGA or a GGA derivative.8. A composition for increasing the expression and/or release of one or more neurotransmitters from a neuron at risk of developing extracellular pathogenic protein aggregates claim 5 , said composition comprising an extracellular protein aggregate inhibiting amount of GGA or a GGA derivative.10. The method of claim 10 , wherein said pre-contacted neuron exhibits one or more of:(i) a reduction in the axon growth ability,(ii) a reduced expression level of one or more neurotransmitters,(iii) a reduction in the formation of synapses, and(iv) a reduction in electrical excitability.11. The method of claim 9 , wherein the neurostimulation comprises one or more of:(i) enhancing or inducing ...

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Номер записи: 38
07-11-2013 дата публикации

Compositions and Methods for Inhibition of Cathepsins

Номер: US20130296605A1
Автор: Chaplin David J., Gaddale Devanna Kishore Kumar, Parker Erica, Pinney Kevin G., Song Jiangli, Trawick Mary L.
Принадлежит:

This invention is directed to compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin K or cathepsin L, will be therapeutically useful. 2. The compound of claim 1 , wherein X is C(═O) or CH(OR).3. The compound of claim 2 , wherein X is C(═O).4. The compound of claim 1 , wherein m is zero.5. The compound of claim 4 , wherein n is zero and p is zero.6. The compound of claim 1 , wherein n is zero and p is zero.7. The compound of wherein m is 1.8. The compound of claim 7 , wherein Ris halo or acyl.9. The compound of claim 8 , wherein Ris substituted aryl-C(O)— or unsubstituted aryl-C(O)—.10. The compound of claim 8 , wherein Ris benzoyl.11. The compound of claim 1 , whereineach of n and p, independently, is zero or one; and{'sup': 3', '5, 'each of Rand R, independently, is selected from the group consisting of hydroxyl, methyl, methoxy and fluoro.'}13. The compound of claim 12 , wherein X is C(═O).14. The compound of claim 13 , wherein each of n claim 13 , m and p claim 13 , independently claim 13 , is zero or one.15. The compound of claim 13 , wherein n is one and Ris selected from the group consisting of hydroxyl claim 13 , methyl claim 13 , methoxy claim 13 , and fluoro.16. The compound of claim 13 , wherein p is one and Ris selected from the group consisting of hydroxyl claim 13 , methyl claim 13 , methoxy and fluoro18. The compound of claim 12 , wherein X is and m is zero or one.19. The compound of claim 18 , wherein each of n and p claim 18 , independently claim 18 , is zero or one. This application claims the benefit of U.S. provisional patent application No. 61/615,097, filed on 23 Mar. 2012, which application is incorporated herein by reference in its entirety.A. FieldThe present invention relates to compounds and methods of using these compounds in the treatment of conditions in which modulation of the cathepsin, particularly cathepsin K or cathepsin L, is ...

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Номер записи: 39
21-11-2013 дата публикации

P53 ACTIVATING COMPOUNDS

Номер: US20130310382A1
Автор: Hollick Jonathan James, Lain Sonia, Lane David Phillip, McCarthy Anna Rose, Stark Michael John Raymond, Westwood Nicholas James
Принадлежит:

The present invention relates to compounds which activate the p53 response, and find use in, for example, hyperproliferative diseases such as cancer treatment and potentially other diseases/conditions involving sirtuin function. 19-. (canceled)1115-. (canceled)16. The method of claim 10 , wherein Rand Rare hydrogen or a Calkyl.17. The method of claim 10 , wherein Rand Rare hydrogen.18. The method of claim 10 , wherein Y is present.19. The method of claim 10 , wherein Y is —C(O)—.20. The method of claim 10 , wherein Ar′ is a phenyl substituted at one or more available position by a C-Cbranched or unbranched claim 10 , substituted or unsubstituted alkyl.21. The method of claim 10 , wherein Ar′ is a phenyl substituted by a branched alkyl group.22. The method of claim 21 , where the branched alkyl group is isopropyl or tert butyl.23. The method of claim 21 , wherein the branched alkyl group is positioned in the para position of the phenyl ring to which it is bonded.24. The method of claim 10 , wherein the portion R—Y—N(R)— of formula (I) is R—Y—N(H)—.26. The method of claim 25 , wherein R—Y—NH— is RC(O)NH—.27. The method of claim 25 , wherein the groups R—Y—NH— and/or R— are in the para-position on the respective phenyl rings to which they are bonded.28. The method of claim 24 , wherein Rin R—Y—N(H)— is H claim 24 , or a substituted or unsubstituted alkyl or aryl group.29. The method of claim 28 , wherein the alkyl group is a C-Cstraight chain alkyl.30. The method of claim 28 , wherein Ris an alkyl or aryl group substituted one or more times with a group independently selected claim 28 , at each occurrence claim 28 , from the group consisting of alkyl claim 28 , alkenyl claim 28 , alkynyl claim 28 , aryl or heteroaryl claim 28 , carboxy claim 28 , alkyloxycarbonyl hydroxyl claim 28 , amino claim 28 , nitro claim 28 , alkyloxy claim 28 , alkylthio claim 28 , formyl claim 28 , cyano claim 28 , carbamoyl claim 28 , halo claim 28 , a ketone claim 28 , —S(O)NRRor —S(O)R ...

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Номер записи: 40
21-11-2013 дата публикации

Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions

Номер: US20130310555A1
Автор: Hyun-Soon Chong
Принадлежит: Illinois Institute of Technology

Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.

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Номер записи: 41
21-11-2013 дата публикации

INTERMEDIATES FOR THE PREPARATION OF BETA-SANTALOL

Номер: US20130310609A1
Автор: Chapuis Christian
Принадлежит: FIRMENICH SA

The present invention concerns a process for the preparation of a compound of formula (I) in the form of any one of its stereoisomers or mixtures thereof, and wherein the dotted line may represents an additional bond and Rrepresents a hydrogen atom or a Si(R)or (R)COH group, each Rrepresenting Calkyl group or a phenyl group. The invention concerns also the compound (I) as well as its use for the synthesis of β-santalol or of derivatives thereof. 3. A compound according to , wherein X may represent a halogen atom or a sulfonate group as defined in .4. A compound according to claim 1 , wherein Rrepresents a hydrogen atom or a Si(R) claim 1 , each Rrepresenting a Calkyl group or a phenyl group.5. A compound according to claim 1 , wherein said compound is in the form of a mixture of stereoisomers comprising more than 50% (w/w) of:the (1RS,4SR) or the (1RS,2SR,4SR) diastereoisomer, when the dotted line represents a single bond; orthe (1RS,4SR) or the (1RS,2RS,4SR) diastereoisomer, when the dotted line represents a double bond.6. A compound according to claim 1 , wherein said compound is in the form of a mixture of stereoisomers comprising more than 50% (w/w) ofthe (1S,4R) or (1S,2R,4R) enantiomer, when the dotted line represents a single bond; orthe (1R,4S) or (1R,2R,4S) enantiomer, when the dotted line represents a double bond.7. A process for the preparation of a compound of formula (I) claim 1 , as defined in claim 1 , comprising the following steps:{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, 'sub': 'a', 'a) reacting a compound of formula (II), as defined in , with a base having a pKabove 16, preferably comprised between 16 and 30;'}{'sup': a', 'a, 'b) optionally, when Ris not a hydrogen atom, treating the compound obtained in step a) with a suitable base or a fluorine salt to obtain compound (I) wherein Ris hydrogen atom.'} The present invention relates to the field of organic synthesis and more specifically it concerns a process for the preparation of a ...

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Номер записи: 42
12-12-2013 дата публикации

Lipids for therapeutic agent delivery formulations

Номер: US20130330401A1
Автор: John A. Gaudette, Joseph E. Payne, Jun Zhang, Lei Yu, Mohammad Ahmadian, Neda SAFARZADEH, Priya Karmali, Richard P. Witte, Victor Knopov, Violetta Akopian, Wenbin Ying, Zheng Hou
Принадлежит: Nitto Denko Corp

The description is directed to ionizable lipids useful for enhancing the delivery of therapeutic agents in liposomes.

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Номер записи: 43
19-12-2013 дата публикации

Thin film solar cell

Номер: US20130333759A1
Автор: Kyung Ho Kim, Masahiko Maekawa, Naoya Tanaka, Takashi Okubo, Takayoshi Kuroda, Yoshie Inuzuka
Принадлежит: JAPAN SCIENCE AND TECHNOLOGY AGENCY, KINKI UNIVERSITY

[Object] A thin-film solar cell which can be produced using an inexpensive raw material and has improved conversion efficiency has been desired. [Solution] A thin-film solar cell according to the present invention includes at least one organic semiconductor and a coordination polymer. The coordination polymer contains a repeating unit which includes a complex produced by coordinating at least one ligand to at least one metal ion, the metal ion being selected from ions of transition metal elements, and the ligand being capable of coordinating to the metal ion and selected from sulfur-containing compounds, nitrogen-containing compounds, oxygen-containing compounds, and phosphorus-containing compounds.

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Номер записи: 44
09-01-2014 дата публикации

SMALL MOLECULES AS EPIGENETIC MODULATORS OF LYSINE-SPECIFIC DEMETHYLASE 1 AND METHODS OF TREATING DISORDERS

Номер: US20140011857A1
Автор: Bytheway Ian, Casero Robert A., Woster Patrick M.
Принадлежит: THE JOHNS HOPKINS UNIVERSITY

The invention provides for novel compounds which are inhibitors of lysine-specific demethylase 1 (LSD1). Such compounds may be used to treat disorders, including cancer. 3. The compound of claim 2 , wherein J is O.4. The compound of claim 2 , wherein q is 1.5. The compound of claim 2 , wherein Ris nitro claim 2 , hydroxy claim 2 , thio claim 2 , C(O)NRR claim 2 , or C(O)OR.6. The compound of claim 5 , wherein Ris nitro claim 5 , hydroxy claim 5 , thio claim 5 , C(O)NH claim 5 , or C(O)OEt.7. The compound of claim 1 , wherein Y is —NH.8. The compound of claim 7 , wherein J is absent claim 7 , and the carbon to which J is attached is —CH—.9. The compound of claim 7 , wherein q is 3 or 4.10. The compound of claim 7 , wherein Ris nitro claim 7 , hydroxy claim 7 , thio claim 7 , C(O)NRR claim 7 , or C(O)OR.11. The compound of claim 7 , wherein Ris haloalkyl claim 7 , nitro claim 7 , hydroxy claim 7 , thio claim 7 , C(O)NRR claim 7 , or C(O)OR.12. The compound of claim 7 , wherein Ris haloalkyl claim 7 , nitro claim 7 , hydroxy claim 7 , thio claim 7 , C(O)NRR claim 7 , or C(O)OR.14. (canceled)1618-. (canceled)20. A pharmaceutical composition comprising a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt claim 1 , solvate or hydrate thereof thereof claim 1 , in combination with a pharmaceutically acceptable carrier or excipient.21. (canceled)24. The method of claim 22 , wherein the disease or disorder is selected from: tumor claim 22 , cancer claim 22 , blood disorder claim 22 , neoplasia claim 22 , skin disorders claim 22 , neovascularization claim 22 , inflammatory and arthritic diseases claim 22 , retinoblastoma claim 22 , cystoid macular edema (CME) claim 22 , exudative age-related macular degeneration (AMD) claim 22 , diabetic retinopathy claim 22 , diabetic macular edema claim 22 , or ocular inflammatory disorders.2528-. (canceled)3031-. (canceled)33. The method of claim 32 , wherein the compound inhibits LSD1 to thereby treat ...

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Номер записи: 45
09-01-2014 дата публикации

Method for Producing Fluorine-Containing Substituted Compound and Fluorine-Containing Substituted Compound

Номер: US20140012027A1
Автор: NAGAKI Aiichiro, YOSHIDA Junichi
Принадлежит:

A method for producing a fluorine-containing substituted compound, the method including: introducing an organofluorine compound and an organolithium compound into a microreactor provided with a flow path capable of mixing a plurality of liquids, to thereby obtain a reaction product; and introducing, into the microreactor, the reaction product and an electrophile exhibiting electrophilic effect on the reaction product, to thereby obtain a fluorine-containing substituted compound. 1. A method for producing a fluorine-containing substituted compound , the method comprising:introducing an organofluorine compound and an organolithium compound into a microreactor provided with a flow path capable of mixing a plurality of liquids, to thereby obtain a reaction product; andintroducing, into the microreactor, the reaction product and an electrophile exhibiting electrophilic effect on the reaction product, to thereby obtain a fluorine-containing substituted compound.2. The method according to claim 1 ,wherein the organofluorine compound is a fluoroalkyl halide having 6 carbon atoms, and {'br': None, 'i': T≦−', 't−, '3.848.'}, 'wherein a temperature T (° C.) inside the microreactor into which the organofluorine compound and the organolithium compound have been introduced and a residence time t (sec) thereof in the microreactor satisfy the following relation3. The method according to claim 1 ,wherein the organofluorine compound is a fluoroalkyl halide having 2 carbon atoms, andwherein a temperature T (° C.) inside the microreactor into which the organofluorine compound and the organolithium compound have been introduced and a residence time t (sec) thereof in the microreactor satisfy the relations −100≦T≦0 and 0.15≦t≦8.4, respectively.4. The method according to claim 1 ,wherein the organofluorine compound is a fluoroalkyl halide having 3 carbon atoms, and {'br': None, 'i': T≦−', 't−, '3.245.'}, 'wherein a temperature T (° C.) inside the microreactor into which the organofluorine ...

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Номер записи: 46
23-01-2014 дата публикации

Aqueous Solution Containing Partial Ras Polypeptide and Method for Screening Inhibitor of Ras Function

Номер: US20140024123A1
Автор: Araki Mitsugu, Kataoka Tohru, Shima Fumi, Tamuta Atsuo
Принадлежит: NATIONAL UNIVERSITY CORPORATION KOBE UNIVERSITY

Provided is a screening method for a more effective Ras inhibitor. Further provided are amino acid residues at a site important for an interaction with a Ras inhibitor in a Ras polypeptide. By confirming a difference between structural information on the Ras polypeptide by NMR and structural information between a complex of the Ras polypeptide and a seed compound by NMR, a more effective lead compound than the seed compound can be selected. As a result of analysis based on the structural information on the Ras polypeptide by NMR, the amino acid residues capable of interacting with a Ras inhibitor candidate (a) are K5, E37, D38, S39, L56, E63, Y64, A66, M67, Q70, Y71, R73, and T74 with reference to an amino acid sequence set forth in SEQ ID NO: 1. 112-. (canceled)13. A screening method for identifying a Ras inhibitor (A) , comprising the steps of:obtaining an NMR spectrum from a partial Ras polypeptide of an amino acid sequence set forth in SEQ ID NO: 1 or an amino acid sequence having substitutions, deletions, or additions of one to three amino acids in the amino acid sequence set forth in SEQ ID NO: 1;(ii) obtaining an NMR spectrum of a complex produced by contacting a Ras inhibitor candidate with said partial Ras polypeptide; and(iii) identifying whether said Ras inhibitor candidate (a) is a Ras inhibitor (A) by analyzing a difference between the NMR spectrum obtained in said step (i) and the NMR spectrum obtained in said step (ii).14. The screening method for identifying a Ras inhibitor (A) according to claim 13 , wherein said partial Ras polypeptide comprises a polypeptide in which threonine at position 35 is substituted by serine in the amino acid sequence set forth in SEQ ID NO: 1.16. A screening method for identifying a Ras inhibitor candidate (a) claim 13 , comprising:determining whether a substance interacts with at least three or more reference amino acid residues, wherein said reference amino acid residues are selected from the group consisting of, with ...

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Номер записи: 47
23-01-2014 дата публикации

Small molecule inhibitors of necroptosis

Номер: US20140024657A1
Автор: Emily S. Hsu, Junying Yuan
Принадлежит: Harvard College

The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-α induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.

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Номер записи: 48
06-03-2014 дата публикации

S1P Receptors Modulators and Their Use Thereof

Номер: US20140066427A1
Автор: Damian W. Grobelny, Gurmit S. Gill
Принадлежит: Akaal Pharma Pty Ltd

The invention relates to novel compounds that have SIP receptor modulating activity. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate SIP receptor modulating activity or expression, for example, autoimmune response. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate SIP receptor modulating activity or expression such as autoimmune response.

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Номер записи: 49
06-03-2014 дата публикации

REL INHIBITORS AND METHODS OF USE THEREOF

Номер: US20140066486A1
Автор: CHEN Youhai H., Murali Ramachandran, Sun Jing
Принадлежит: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA

This invention provides REL inhibitors which interfere with the DNA binding capacity of a REL protein. Additionally this invention provides methods of treating, abrogating, or preventing diseases which respond with a positive clinical score to a REL inhibitor. Methods of identifying REL inhibitor based on a REL protein three dimensional model are described. 2. The composition of claim 1 , wherein the inhibitor interact with L1 cavity on the surface of the c-Rel.3. The composition of claim 1 , wherein said L1 cavity comprises amino acids Arg 21 claim 1 , Cys 26 claim 1 , Glu 27 claim 1 , Lys 110 claim 1 , and Lys 111.5. The composition of claim 1 , comprising the compound represented by the structure of formula (IV) claim 1 , (V) or their pharmaceutical salt.7. Use of the composition of for preventing claim 1 , inhibiting claim 1 , suppressing or ameliorating symptoms associated with inflammatory conditions that are multiple sclerosis claim 1 , arthritis claim 1 , diabetes claim 1 , colitis claim 1 , lupus claim 1 , autoimmunity claim 1 , graft rejection claim 1 , or a combination thereof.8. A method of inhibiting or suppressing the interaction between c-Rel and a DNA claim 1 , comprising the step of contacting the c-Rel with a compound capable of masking the L1 cavity of the c-Rel claim 1 , thereby inhibiting or suppressing the interaction between c-Rel and a DNA and inflammatory immune response.10. The method of claim 9 , wherein said inhibitor further inhibits the production of interleukin-2 claim 9 , interferon-gamma claim 9 , or the combination thereof.11. The method of claim 9 , wherein said L1 cavity comprises the amino acids Arg 21 claim 9 , Cys 26 claim 9 , Glu 27 claim 9 , Lys 110 claim 9 , and Lys 111.13. The method of claim 9 , whereby the compound capable of masking the L1 cavity of the c-Rel is represented by the structure of formula (IV) claim 9 , (V) or their pharmaceutical salt.15. A method of treating claim 9 , inhibiting or suppressing claim 9 , or ...

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Номер записи: 50
20-03-2014 дата публикации

ISOLATED COMPOUNDS FROM TURMERIC OIL AND METHODS OF USE

Номер: US20140080916A1
Автор: Catalano Susan, Rishton Gilbert M.
Принадлежит: Cognition Therapeutics, Inc.

Compounds that are central nervous system drug candidates for the treatment of cognitive decline and, more particularly, Alzheimer's disease are provided. Methods for treatment, inhibition, and/or abatement of cognitive decline and/or Alzheimer's disease with a compound or pharmaceutically acceptable salt of the invention are also provided. Also provided are methods of preparing the compounds/compositions of the invention. 2. (canceled)3. The compound of selected from:2-methyl-6-p-tolylhept-2-en-4-ol;2-methyl-6-(4-methylcyclohexa-1,3-dienyl)hept-2-en-4-ol;2-methyl-6-p-tolylheptane-2,4-diol;N-isobutyl-2-methyl-6-(p-tolyl)hept-2-en-4-amine;4-(isobutylamino)-2-methyl-6-p-tolylheptan-2-ol;4-(isobutylamino)-2-methyl-6-(4-methylcyclohexa-1,3-dienyl)heptan-2-ol and pharmaceutically acceptable salts thereof.5. (canceled)6. The compound of selected from:(6S)-2-methyl-6-p-tolylhept-2-en-4-ol;(6S)-2-methyl-6-(4-methylcyclohexa-1,3-dienyl)hept-2-en-4-ol;(6S)-2-methyl-6-p-tolylheptane-2,4-diol;(6S)—N-isobutyl-2-methyl-6-(p-tolyl)hept-2-en-4-amine;(6S)-4-(isobutylamino)-2-methyl-6-p-tolylheptan-2-ol;(6S)-4-(isobutylamino)-2-methyl-6-(4-methylcyclohexa-1,3-dienyl)heptan-2-ol and pharmaceutically acceptable salts thereof.8. (canceled)9. The compound of claim 7 , selected from:(4S,6S)—N-isobutyl-2-methyl-6-p-tolylhept-2-en-4-amine;6S)—N-isobutyl-2-methyl-6-p-tolylhept-2-en-4-amine and pharmaceutically acceptable salts thereof.11. (canceled)12. The pharmaceutical composition of claim 10 , wherein the compound is selected from:2-methyl-6-p-tolylhept-2-en-4-ol;2-methyl-6-(4-methylcyclohexa-1,3-dienyl)hept-2-en-4-ol;2-methyl-6-p-tolylheptane-2,4-diol;N-isobutyl-2-methyl-6-(p-tolyl)hept-2-en-4-amine;4-(isobutylamino)-2-methyl-6-p-tolylheptan-2-ol;4-(isobutylamino)-2-methyl-6-(4-methylcyclohexa-1,3-dienyl)heptan-2-ol and pharmaceutically acceptable salts thereof.14. (canceled)15. The pharmaceutical composition of claim 13 , wherein the compound is selected from:(6S)-2-methyl-6-p-tolylhept ...

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Номер записи: 51
10-04-2014 дата публикации

PROCESS FOR PREPARING ALKOXYCARBONYL ISOTHIOCYANATE

Номер: US20140100381A1
Автор: BLAND DOUGLAS C., Fisk Jason S., Frycek George J.
Принадлежит: DOW AGROSCIENCES LLC

Provided herein are processes for the preparation of alkoxycarbonyl isothiocyanates from alkyl chloroformates and thiocyanates in toluene by controlling the amounts of water and catalyst. 2. The process of claim 1 , wherein R is methyl or ethyl.3. The process of claim 2 , wherein R is ethyl.4. The process of claim 1 , wherein the salt of thiocyanate is a sodium claim 1 , potassium or ammonium salt.5. The process of claim 4 , wherein the salt of thiocyanate is a sodium salt.6. The process of claim 1 , wherein the catalyst is pyridine claim 1 , quinoline claim 1 , pyrimidine claim 1 , pyrazine claim 1 , or quinoxaline optionally substituted with one or more alkyl claim 1 , halo claim 1 , or alkoxy groups claim 1 , wherein the pyridine claim 1 , quinoline claim 1 , pyrimidine claim 1 , pyrazine claim 1 , or quinoxaline is unsubstituted at the 2-position.7. The process of claim 6 , wherein the catalyst is pyridine.8. The process of claim 1 , wherein about 0.05 to about 0.1 molar equivalents of water are employed.9. The process of claim 8 , wherein about 0.1 molar equivalents of water are employed.10. The process of claim 1 , wherein about 0.01 to about 0.03 molar equivalents of catalyst are employed.11. The process of claim 10 , wherein about 0.01 equivalents of catalyst are employed.12. The process of claim 1 , wherein the temperature is from about 20° C. to about 40° C.13. The process of claim 12 , wherein the temperature is about 30° C.14. The process of claim 1 , whereina. R is methyl or ethyl;b. the salt of thiocyanate is a sodium, potassium or ammonium salt;c. the catalyst is pyridine, quinoline, pyrimidine, pyrazine, or quinoxaline optionally substituted with one or more alkyl, halo, or alkoxy groups, wherein the pyridine, quinoline, pyrimidine, pyrazine, or quinoxaline is unsubstituted at the 2-position;d. about 0.05 to about 0.1 molar equivalents of water are employed;e. about 0.01 to about 0.03 molar equivalents of catalyst are employed; andf. wherein the ...

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Номер записи: 52
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, ...

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Номер записи: 53
07-01-2016 дата публикации

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

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

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

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Номер записи: 54
04-01-2018 дата публикации

INTERMEDIATE COMPOUNDS FOR PRODUCING PERFUMING INGREDIENTS

Номер: US20180002260A1
Автор: Dupau Philippe, HALDIMANN SANCHEZ Murielle
Принадлежит: FIRMENICH SA

The present invention relates to the field of chemical processes and, more particularly, it concerns valuable new chemical intermediates of formula (IV) for producing perfuming ingredients. 3. The process of claim 1 , wherein at least one of said R claim 1 , R claim 1 , Rand Ris a Calkyl group.4. The process of claim 1 , wherein the R group represents a Calkyl group.5. The process of claim 1 , wherein the reduction of step a) is performed by a catalytic hydrogenation in the presence of a supported Pd.6. A process according to claim 5 , characterised in that said supported Pd is an Pd on charcoal having an egg-shell-type distribution.9. A compound according to claim 8 , characterised in that X is a carbonyl group.10. A compound according to claim 8 , characterised in that X is a CHgroup.11. The compound of claim 8 , wherein:{'sup': 1', '2', '4', '3', '1', '2', '3', '4', '1', '4', '2', '3', '1', '3', '2', '4', '1', '2', '3', '4, 'i) R, Rand Rare each a hydrogen atom and Ris a methyl group, ii) R, Rand Rare each a hydrogen atom and Ris a methyl group, iii) Rand Rare each a hydrogen atom and Rand Rare each a methyl group, iv) Rand Rare each a hydrogen atom and Rand Rare each a methyl group or v) Rand Rare each a hydrogen atom and Rand Rare each a methyl group.'}12. The process of claim 2 , wherein at least one of the R claim 2 , R claim 2 , Rand Ris a Calkyl group.13. The process of claim 2 , wherein the R group represents a Calkyl group.14. The process of claim 2 , wherein the reduction of step a) is performed by a catalytic hydrogenation in the presence of a supported Pd.15. The process of claim 14 , wherein the supported Pd is an Pd on charcoal having an egg-shell-type distribution. The present invention relates to the field of perfumery. More particularly, it concerns valuable new chemical intermediates for producing perfuming ingredients. Moreover, the present invention comprises the also a process for producing said intermediates.EP 1022265 describe a new class of ...

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Номер записи: 55
04-01-2018 дата публикации

(THIO, OXO, AND SELENO) SEMICARBAZONE COMPLEXES WITH ZINC AND THEIR USE FOR TREATING CANCER

Номер: US20180002279A1
Автор: Augeri David J., Bencivenga Anthony F., Blanden Adam, Carpizo Darren R., Gilleran John A., Kimball Spencer David, Loh Stewart N., Yu Xin
Принадлежит:

The invention provides organic complexes of Zn of formula (I) that are useful for treating cancer, as well as compositions and kits comprising such complexes, and intermediate monomer compounds that are useful for the preparation of such complexes. 4. The complex of any one of - wherein the ratio of the number of compounds of formula (I) or ions or poly-ions thereof to zinc Zn ions is about 2:1; or a solvate thereof.8. A pharmaceutical composition , comprising a complex of any one of - or a solvate thereof , and a pharmaceutically acceptable carrier.9. An injectable pharmaceutical formulation comprising , a complex of any one of - or a solvate thereof , and a pharmaceutically acceptable carrier.10. A method of inhibiting cancer cell growth in vivo or in vitro , comprising contacting a cancer cell with a complex of any one of - or a solvate thereof.11. A method of treating cancer in an animal comprising administering a complex of any one of - or a solvate thereof to the animal.12. The method of claim 11 , further comprising administering zinc to the animal.13. The method of any one of - claim 11 , wherein the cancer is caused by mutations affecting zinc binding proteins.14. The method of any one of - claim 11 , wherein the cancer is associated with a zinc binding p53 mutation.15. The method of any one of - claim 11 , wherein the cancer is associated with a zinc binding p53 mutation selected from R175 claim 11 , C176 claim 11 , H179 claim 11 , C238 claim 11 , C242 claim 11 , and G245.16. A complex of any one of - or a solvate thereof for use in medical treatment.17. A complex of any one of - or a solvate thereof for the prophylactic or therapeutic treatment of cancer.18. The complex or solvate of wherein the cancer is caused by mutations affecting zinc binding proteins.19. The complex or solvate of claim 17 , wherein the cancer is associated with a zinc binding p53 mutation.20. The complex or solvate of claim 17 , wherein the cancer is associated with a zinc binding ...

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Номер записи: 56
04-01-2018 дата публикации

(THIO, OXO, AND SELENO) SEMICARBAZONE DERIVATIVES AND THEIR USE FOR TREATING CANCER

Номер: US20180002280A1
Автор: Augeri David J., Bencivenga Anthony F., Blanden Adam, Carpizo Darren R., Gilleran John A., Kimball Spencer David, Loh Stewart N., Yu Xin
Принадлежит:

The invention provides compounds of formula I and II and salts thereof, wherein R, R, Y, R, and Rhave any of the meanings described in the specification, as well as compositions comprising such compounds and salts, and methods for treating cancer using such compounds and salts. 3. A pharmaceutical composition , comprising , a compound of or or a pharmaceutically acceptable salt thereof , and a pharmaceutically acceptable carrier.4. An injectable pharmaceutical formulation comprising , a compound of or or a pharmaceutically acceptable salt thereof , and a pharmaceutically acceptable carrier.5. A method of inhibiting cancer cell growth in vivo or in vitro , comprising contacting a cancer cell with a compound of any one of - or a pharmaceutically acceptable salt thereof.6. A method of treating cancer in an animal comprising administering a compound of any one of - or a pharmaceutically acceptable salt thereof to the animal.7. The method of claim 6 , further comprising administering zinc to the animal.8. The method of any one of - claim 6 , wherein the cancer is caused by mutations affecting zinc binding proteins.9. The method of any one of - claim 6 , wherein the cancer is associated with a zinc binding p53 mutation.10. The method of any one of - claim 6 , wherein the cancer is associated with a zinc binding p53 mutation selected from R175 claim 6 , C176 claim 6 , H179 claim 6 , C238 claim 6 , C242 claim 6 , and G245.11. A compound of any one of - or a pharmaceutically acceptable salt thereof claim 6 , for use in medical treatment.12. A compound of any one of - or a pharmaceutically acceptable salt thereof claim 6 , for the prophylactic or therapeutic treatment of cancer.13. The compound or pharmaceutically acceptable salt of wherein the cancer is caused by mutations affecting zinc binding proteins.14. The compound or pharmaceutically acceptable salt of claim 13 , wherein the cancer is associated with a zinc binding p53 mutation.15. The compound or pharmaceutically ...

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Номер записи: 57
02-01-2020 дата публикации

METHODS FOR CONVERTING GLYCEROL TO ALLYL COMPOUNDS

Номер: US20200002256A1
Автор: RODRIGUEZ HERRERO Yanet, ULLAH Aman
Принадлежит:

The present disclosure is directed towards methods of converting glycerol to an allyl compound, involving deoxydehydrating glycerol with formic acid and heat to form allyl alcohol; and esterifying the allyl alcohol with formic acid and/or phthalic anhydride and heat to form allyl formate and diallyl phthalate. In some instances, the heat is generated by a microwave. In further instances, the methods involve polymerizing the allyl alcohol, allyl formate and/or diallyl phthalate to form poly(allyl alcohol) or poly(allyl formate) or poly (diallyl phthalate). In some instances, the allyl polymers were used for the consolidation of oil sands tailings. 1. A method of converting glycerol to an allyl compound , comprising:a) deoxydehydrating glycerol with formic acid and heat to form allyl alcohol; andb) esterifying the allyl alcohol with formic acid and heat to form allyl formate.2. The method of claim 1 , wherein the heat is generated by a microwave.3. The method of claim 1 , wherein a microwave assists:a. deoxydehydrating glycerol with formic acid and heat by distillation to form allyl alcohol; andb. esterifying the allyl alcohol with formic acid and heat by reflux to form allyl formate.4. The method of claim 1 , wherein deoxydehydrating the glycerol with the formic acid and heat to form the allyl alcohol comprises heating the glycerol and the formic acid to about 195° C. claim 1 , and then heating the glycerol and the formic acid to about 240° C.5. The method of claim 4 , further comprising isolating the allyl alcohol while heating the glycerol and the formic acid to about 240° C.6. The method of claim 5 , further comprising cooling the glycerol and the formic acid to between about 95°-100° C. claim 5 , and then adding more of the formic acid.7. The method of claim 5 , wherein esterifying the allyl alcohol with formic acid and heat to form allyl formate comprises heating the allyl alcohol and formic acid at about 60° C.8. The method of claim 5 , wherein the allyl ...

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Номер записи: 58
03-01-2019 дата публикации

BIAROMATIC VITAMIN D ANALOGS

Номер: US20190002378A1
Автор: BENDIK Igor, Geotti-Bianchini Piero, HEIDL Marc, JACKSON Eileen, Schlifke-Poschalko Alexander
Принадлежит:

Novel biaromatic compounds, which are vitamin D analogs, processes for their preparation and cosmetic, dermatological and pharmaceutical preparations containing one or more of these compounds. 2. Compound according to claim 1 , wherein Ris ethyl.3. Compound according to claim 1 , wherein R claim 1 , Rindependently of each other represent an ethyl group claim 1 , or a CFgroup.4. Compound according to claim 1 , wherein Rand Rare different and represent a hydrogen atom and a methyl group.11. Cosmetic composition comprising a compound according to .12. Cosmetic composition according to claim 11 , wherein the amount of the compound of formula (I) is in the range of 0.00001 to 0.1 wt.-% based on the total weight of the cosmetic composition.13. Method to smoothen wrinkles and/or fine lines and/or to decrease their volume and depth claim 11 , said method comprising the step of applying a cosmetic composition according to to the affected area.14. Dermatological composition comprising one or more compounds according to .15. Pharmaceutical composition comprising one or more compounds according to .16. Process for preparing compounds of formula (I) claim 1 , which comprises the step of hydroboration of a styrene derivative followed by a sp-spSuzuki cross coupling of the resulting organoborane with an aryl halogenide to form the 1 claim 1 ,2 diphenylethane core structure. The present invention relates to novel biaromatic compounds, which are vitamin D analogs. The invention furthermore relates to processes for their preparation and cosmetic, dermatological and pharmaceutical preparations containing one or more of these compounds.Vitamin D comprises a group of fat-soluble compounds, which are e.g. essential for maintaining the calcium and phosphate balance in the body, build and maintain healthy bones, control cell division and specialization and modulate the immune system.The European Food Safety Authority (EFSA) has confirmed that health benefits have been established for the ...

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Номер записи: 59
07-01-2016 дата публикации

DIENE/DIENOPHILE COUPLES AND THERMOSETTING RESIN COMPOSITIONS HAVING REWORKABILITY

Номер: US20160002510A1
Автор: CHAMPAGNE Timothy M., Israel Jonathan B., Jordan Benny E., Klemarczyk Philip T., Sridhar Laxmisha M., Zhang XianMan
Принадлежит:

Thermosetting resin compositions are provided that are useful for mounting onto a circuit board semiconductor devices, such as chip size or chip scale packages (“CSPs”), ball grid arrays (“BGAs”), land grid arrays (“LGAs”) and the like (collectively, “subcomponents”), or semiconductor chips. Reaction products of the compositions are controllably reworkable when subjected to appropriate conditions. 1. A curable composition reaction products of which are controllably degradable upon exposure to a temperature condition greater than a temperature condition used to cure the composition , comprising:(a) a curable resin component;(b) a curative and(c) a diene/dienophile couple functionalized with at least two carboxylic acid groups.2. An electronic device comprising a semiconductor device and a circuit board to which said semiconductor device is electrically connected or a semiconductor chip and a circuit board to which said semiconductor chip is electrically connected claim 1 , assembled using a curable composition according to as an underfill sealant between the semiconductor device and the circuit board or the semiconductor chip and the circuit board claim 1 , respectively claim 1 , wherein reaction products of the composition are capable of softening and losing their adhesiveness under exposure to temperature conditions in excess of those used to cure the composition.3. A method of sealing underfilling between a semiconductor device including a semiconductor chip mounted on a carrier substrate and a circuit board to which said semiconductor device is electrically connected or a semiconductor chip and a circuit board to which said semiconductor chip is electrically connected claim 1 , the steps of which comprise:{'claim-ref': {'@idref': 'CLM-00001', 'claims 1'}, '(a) dispensing into the underfilling between the semiconductor device and the circuit board or the semiconductor chip and the circuit board a composition according to ; and'}(b) exposing the composition as so ...

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Номер записи: 60
07-01-2021 дата публикации

METHOD OF SYNTHESIS OF AN IONIZABLE CATIONIC LIPID

Номер: US20210002217A1
Автор: Chivukula Padmanabh, Payne Joseph E.
Принадлежит:

What is described is a method of synthesis of the compound of formula 1A, 2. The method of claim 1 , wherein the nucleic acid is an RNA.3. The method of claim 2 , wherein the RNA is siRNA claim 2 , mRNA claim 2 , or miRNA.4. The method of claim 1 , wherein the target cell is a lung epithelial cell.5. The method of claim 1 , wherein the target cell is a hepatocyte.6. The method of claim 1 , wherein the lipid formulation is a lipid nanoparticle or a liposome.7. The method of claim 6 , wherein 30-70% of the lipids in the lipid formulation are a compound having Formula IA.8. The method of claim 7 , wherein 5-30% of the lipids in the lipid formulation are a helper lipid.9. The method of claim 7 , wherein 20-40% of the lipids in the lipid formulation are cholesterol.10. The method of claim 1 , wherein the composition is administered in an aqueous solution to a subject via inhalation.11. The method of claim 10 , wherein the composition is administered to the subject via pulmonary inhalation.12. The method of claim 10 , wherein the aqueous solution is aerosolized claim 10 , atomized claim 10 , or nebulized.16. The method of claim 1 , wherein the nucleic acid is a mRNA and delivery of the mRNA into the target cell results in expression of the mRNA into a protein of interest.17. The method of claim 16 , wherein the protein of interest is an enzyme.18. The method of claim 16 , wherein the protein of interest is an antigen.19. The method of claim 1 , wherein the nucleic acid is an siRNA and delivery of the siRNA into the target cell results in reduced expression of a gene of interest.20. The method of claim 1 , wherein the nucleic acid comprises one or more modified nucleotides selected from phosphorothioates claim 1 , phosphoramidates claim 1 , methyl phosphonates claim 1 , 2′-O-methyl ribonucleotides claim 1 , and peptide-nucleic acids. This application is a continuation of U.S. patent application Ser. No. 15/925,670, filed Mar. 19, 2018, which is a continuation of U.S. ...

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Номер записи: 61
07-01-2021 дата публикации

METHOD FOR PREPARING THIONOCARBAMATE AND CO-PRODUCING 2-MERCAPTOETHANOL OR O-ALKYLTHIOETHYL XANTHATE

Номер: US20210002218A1
Автор: CAO Zhanfang, HUANG Xiaoping, WANG Shuai, ZHONG Hong
Принадлежит: CENTRAL SOUTH UNIVERSITY

The invention belongs to the field of mineral flotation collector materials, and particularly discloses a method for preparing thionocarbamate. In the preparation process, xanthate and 2-haloethanol are esterified to obtain O-alkyl-S-hydroxyethyl xanthate, and then O-alkyl-S-hydroxyethyl xanthate and fatty amine are reacted to obtain a mixture of thionocarbamate and 2-mercaptoethanol. The mixture of thionocarbamate and 2-mercaptoethanol is washed with alkali, and the oil phase and water phase are separated. The oil phase and water phase are thionocarbamate and 2-hydroxyethylthiolate, respectively, and 2-mercaptoethanol is obtained by washing with an acid. 2-alkylthioethanol is obtained by reacting 2-hydroxyethanethiolate with alkyl halide, and then with carbon disulfide and alkali to prepare O-alkylthioethyl xanthate. Thionocarbamate, 2-mercaptoethanol and O-alkylthioethyl xanthate prepared by this method possess high yield and high purity. The process is green and environmentally friendly, and is beneficial to the industrialization of co-production. 3. The method according to claim 1 , whereinthe aminolysis reaction in step 2) is conducted at a temperature of 30-100° C. for reaction time of 1-6 h; andthe fatty amine is added at an amount of 0.9-1.2 times a molar weight of the O-alkyl/alkylthioethyl-S-hydroxyethyl xanthate.4. The method according to claim 1 , wherein in step 3) claim 1 , the mixture of the thionocarbamate and the 2-mercaptoethanol is washed 1-5 times with the alkali having a concentration of 0.1-5 mol/L.5. A method for preparing a thionocarbamate and co-producing 2-mercaptoethanol claim 1 , comprising: washing the 2-hydroxyethyl thiolate obtained in step 3) in the method according to claim 1 , with an acid claim 1 , to obtain the 2-mercaptoethanol.7. The method according to claim 6 , wherein the thioalkylation reaction is conducted at a temperature of 5-50° C. for a reaction time of 0.5-3 h claim 6 , andthe alkyl halide is added at an amount of 0.8- ...

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Номер записи: 62
14-01-2016 дата публикации

COMPOSITIONS FOR ANTI-INFLAMMATORY, ANTIOXIDANT EFFECTS AND IMPROVED RESPIRATORY FUNCTION BY SPECIFIC HISTONE DEACETYLASE INHIBITION

Номер: US20160008313A1
Автор: Karagiannis Thomas, McCord Darlene E.
Принадлежит:

Compositions comprising LSF compositions and treatment regiments comprising administration of LSF containing compositions are disclosed. Compositions and/or regiments may optionally include the administration of vitamins, minerals, and anti-oxidants. Methods for using these compositions and treatment regimens for treating subjects for diseases, including diseases associated with inflammation and/or oxidative stress, are provided. Various methods for use of the LSF compositions for inhibition of histone deacetylases (HDACs) in various cells, tissues, and/or conditions are also provided. 1. A pharmaceutical composition for treatment , suppression and/or amelioration of a condition or disease associated with inflammation or oxidative stress , wherein said composition comprises L-sulforaphane (LSF) , an LSF derived and/or substituted compound , and/or an LSF analogue.3. The composition of wherein R is selected from the group consisting of hydrogen claim 1 , substituted or unsubstituted alkyl claim 1 , substituted or unsubstituted alkenyl claim 1 , substituted or unsubstituted alkynyl claim 1 , substituted or unsubstituted aryl claim 1 , substituted or unsubstituted heterocyclyl claim 1 , substituted or unsubstituted acyl claim 1 , ORa claim 1 , SRa claim 1 , SORa claim 1 , SO2Ra claim 1 , OSO2Ra claim 1 , OSO3Ra claim 1 , NO2 claim 1 , NHRa claim 1 , N(Ra)2 claim 1 , ═N—Ra claim 1 , N(Ra)CORa claim 1 , N(CORa)2 claim 1 , N(Ra)SO2R′ claim 1 , N(Ra)C(═NRa)N(Ra)Ra claim 1 , CN claim 1 , halogen claim 1 , CORa claim 1 , COORa claim 1 , OCORa claim 1 , OCOORa claim 1 , OCONHRa claim 1 , OCON(Ra)2 claim 1 , CONHRa claim 1 , CON(Ra)2 claim 1 , CON(Ra)ORa claim 1 , CON(Ra)SO2Ra claim 1 , PO(ORa)2 claim 1 , PO(ORa)Ra claim 1 , PO(ORa)(N(Ra)Ra) and aminoacid ester having inhibitory efficacy against the LSD1 protein; and further wherein each of the Ra groups is independently selected from the group consisting of hydrogen claim 1 , substituted or unsubstituted alkyl claim 1 , ...

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Номер записи: 63
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 ...

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Номер записи: 64
12-01-2017 дата публикации

SYNTHESIS OF THERAPEUTIC AND DIAGNOSTIC DRUGS CENTERED ON REGIOSELECTIVE AND STEREOSELECTIVE RING OPENING OF AZIRIDINIUM IONS

Номер: US20170008863A1
Автор: Chong Hyun-Soon
Принадлежит:

Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds. 2. The method of claim 1 , further comprising:converting a substituted β amino alcohol to a substituted alkylating agent;converting the substituted alkylating agent to the substituted aziridinium ion; andstereoselectively or regioselectively reacting the aziridinium ion with a nucleophile to obtain the compound.4. The method of claim 2 , further comprising:{'sub': 4', '2', '3', '3', '6', '4, 'converting the substituted alkylating agent to the aziridinium ion in the presence of halosequestering agent comprising AgClO, AgOTf, AgCO, AgOTs, AgNO, AgSbF, or AgBF; and'}stereoselectively or regioselectively reacting the aziridinium ion in situ with a nucleophile to obtain the compound.6. The method of claim 5 , further comprising:{'sub': 4', '2', '3', '3', '6', '4, 'converting the substituted alkylating agent to the aziridinium ion in the presence of halosequestering agent comprising AgClO, AgOTf, AgCO, AgOTs, AgNO, AgSbF, or AgBF; and'}stereoselectively or regioselectively reacting the aziridinium ion in situ with the nucleophile in the presence of a base to obtain the compound.7. The method of claim 5 , further comprising:converting a substituted β amino alcohol to a substituted alkylating agent;converting the substituted alkylating agent to the substituted aziridinium ion; andstereoselectively or regioselectively reacting the aziridinium ion with a nucleophile to obtain the compound, wherein the reaction occurs without isolation of any intermediate compound.9. The method of claim 8 , further comprising removing a protecting group comprising an amino claim 8 , a carboxyl claim 8 , or a hydroxyl protecting group from the compound using a deprotection reaction.10. The method of claim 9 , further comprising converting a nitro group in the compound to an amino ...

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Номер записи: 65
14-01-2016 дата публикации

Modified native beta-ketoacyl-acp synthases and engineered microorganisms

Номер: US20160010115A1
Автор: Catherine M. Cho, Fernando Valle, Jonathan VROOM, Louis Clark, Robert Osborne, Smita Shankar
Принадлежит: Codexis Inc

Genetically engineered cells and microorganisms are provided that produce fatty alcohols and fatty acids. In particular, engineered microbial cells comprise a modified native gene having β-ketoacyl-acp synthase activity.

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Номер записи: 66
14-01-2021 дата публикации

METHODS FOR TREATING PROTOZOAN INFECTIONS

Номер: US20210009552A1
Автор: Abraham Rebecca, Keenan Martine, McCluskey Adam, Page Stephen, Stevens Andrew
Принадлежит:

The invention provides compounds of Formula (I), and their use in methods for treating or preventing a protozoan infection in a subject using a compound of Formula (I). The invention also provides the use of a compound of Formula (I) in the manufacture of a medicament for the treatment of a protozoan infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a protozoan infection in a subject and to a medical device comprising the composition of the invention. 141.-. (canceled)43. A composition comprising the compound of .44. A pharmaceutical or veterinarian composition comprising the compound of and a pharmaceutically acceptable excipient.45. The compound of claim 42 , wherein the compound is 4 claim 42 ,6-bis(2-((E)-(6-chloropyridin-3-yl)methylene)hydrazinyl)pyrimidin-2-amine or a stereoisomer claim 42 , tautomer claim 42 , pharmaceutically acceptable salt thereof.46. The compound of claim 42 , wherein the compound is 4 claim 42 ,6-bis(2-((E)-pyridin-3-ylmethylene)hydrazinyl)pyrimidin-2-amine or a stereoisomer claim 42 , tautomer claim 42 , pharmaceutically acceptable salt thereof.47. The compound of claim 42 , wherein the compound is 4 claim 42 ,6-bis(2-((E)-pyridin-2-ylmethylene)hydrazinyl)pyrimidin-2-amine or a stereoisomer claim 42 , tautomer claim 42 , pharmaceutically acceptable salt thereof.48. The compound of claim 42 , wherein the compound is 4 claim 42 ,6-bis(2-((E)-pyridin-4-ylmethylene)hydrazinyl)pyrimidin-2-amine or a stereoisomer claim 42 , tautomer claim 42 , pharmaceutically acceptable salt thereof.49. The compound of claim 42 , wherein the compound is 4 claim 42 ,6-bis(2-((E)-2 claim 42 ,5-dihydroxybenzylidene)hydrazinyl)pyrimidin-2-aminium 2-formyl-4-hydroxyphenolate or a stereoisomer claim 42 , tautomer claim 42 , pharmaceutically acceptable salt thereof.50. The compound of claim 42 , wherein the compound is 4 claim 42 ,6-bis(2-((E)-3 claim 42 ,4-dihydroxybenzylidene)hydrazinyl) ...

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Номер записи: 67
21-01-2016 дата публикации

ISOTHIOCYANATE PRODUCTION METHOD, COMPOSITION FOR TRANSPORTING AND STORING N-SUBSTITUTED O-SUBSTITUTED THIOCARBAMATE, AND ISOTHIOCYANATE COMPOSITION

Номер: US20160016901A1
Автор: Kosugi Yuji, Miyake Nobuhisa, Shinohata Masaaki
Принадлежит: ASAHI KASEI CHEMICALS CORPORATION

The present invention relates to an isothiocyanate production method using an organic primary amine and thiourea as starting materials; to a composition for transporting and storing an N-substituted O-substituted thiocarbamate that includes an N-substituted O-substituted thiocarbamate and a hydroxy compound, the equivalent weight ratio of hydroxy groups of the hydroxy compound with respect to the carbamate groups of the N-substituted O-substituted thiocarbamate being in the range of 1 to 100; to a composition for transporting and storing a compound with a thioureido group that includes a compound with a thioureido group and a hydroxy compound, the equivalent weight ratio of hydroxy groups of the hydroxy compound with respect to the thioureido groups of the compound with a thioureido group being in the range of 1 to 100; and to an isothiocyanate composition containing an isothiocyanate and a compound with a specific functional group.

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Номер записи: 68
21-01-2016 дата публикации

PROTECTIVE MOLECULES AGAINST ANTHRAX TOXIN

Номер: US20160016930A1
Автор: Bradley Kenneth A., Chamberlain Brian T., DAMOISEAUX Robert, Gillespie Eugene, Ho Chi-Lee Charlie, Jung Michael E.
Принадлежит:

Disclosed herein inter alia are compositions and methods useful in the treatment of infectious diseases and exposure to toxins.

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Номер записи: 69
18-01-2018 дата публикации

USE OF ISOTHIOCYANATE FUNCTIONAL SURFACTANTS AS NRF2 INDUCERS TO TREAT EPIDERMOLYSIS BULLOSA SIMPLEX AND RELATED DISEASES

Номер: US20180016229A1
Автор: Silver Michael E.
Принадлежит:

The present invention relates to methods and compositions for the prevention and treatment of keratin-based skin diseases. In particular, the application describes compositions and methods of treating a patient suffering from skin blistering comprising the use of phase II enzyme inducers and/or activity modifiers. 1. A method for treating or preventing skin blistering in a patient in need thereof or at risk of developing skin blistering , comprising the step of administering to the patient a composition comprising a therapeutically effective amount of an Nrf2 inducer , wherein the Nrf2 inducer comprises an isothiocyanate functional surfactant.2. The method according to claim 1 , wherein the patient suffers from skin blistering.3. The method according to claim 1 , wherein the Nrf2 inducer is a phase II enzyme inducer.4. The method according to claim 1 , wherein the Nrf2 inducer causes the selective induction of K6 claim 1 , K16 or K17 in the keratinocytes in the skin of the patient.5. The method according to claim 1 , wherein the composition comprising the Nrf2 inducer is topically administered to the patient.6. The method according to claim 5 , wherein the amount of Nrf2 inducer in the composition topically administered to the patient is from about 0.5 nmol/cm2 to about 10 μmol/cm2.7. The method according to claim 6 , wherein the composition comprising the Nrf2 inducer is a topical preparation selected from the group consisting of ointment claim 6 , cream claim 6 , emulsion claim 6 , lotion and gel.8. The method according to claim 7 , wherein the composition further comprises one or more pharmaceutical claim 7 , biological or molecular biological active agents.9. The method according to claim 1 , wherein the patient is a mammal.10. The method according to claim 9 , wherein the mammal is a human.11. The method according to claim 1 , wherein the patient suffers from epidermolysis bullosa simplex.12. The method according to claim 1 , wherein the patient suffers from ...

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Номер записи: 70
21-01-2016 дата публикации

METHOD FOR PRODUCING POLYTHIOL COMPOUND, POLYMERIZABLE COMPOSITION FOR OPTICAL MATERIAL, AND USES THEREOF

Номер: US20160017085A1
Автор: KAWAGUCHI Masaru, Nishimura Takeshi
Принадлежит: MITSUI CHEMICALS., INC.

Provided is a method for producing a molded product comprising preparing a polymerizable composition for optical materials and curing the polymerizable composition for optical materials to produce the molded product. The preparation of the polymerizable composition comprises preparing a polythiol compound containing, as a main component, one kind or two or more kinds selected from a defined group of compounds, and preparing the polymerizable composition from the polythiol compound. The preparation of the polythiol compound comprises reacting 2-mercaptoethanol with a defined epihalohydrin compound to obtain a defined compound, reacting the defined compound with sodium sulfide to obtain a defined polyalcohol compound, reacting the polyalcohol compound with thiourea in the presence of hydrogen chloride to obtain an isothiuronium salt, adding aqueous ammonia to a reaction solution containing the isothiuronium salt thereby hydrolyzing the isothiuronium salt to obtain the polythiol compound and purifying the polythiol compound with hydrochloric acid.

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Номер записи: 71
15-01-2015 дата публикации

FUNGICIDAL PYRAZOLE MIXTURES

Номер: US20150018374A1
Автор: Bereznak James Francis, Long Jeffrey Keith, Taggi Andrew Edmund
Принадлежит:

Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof, 2. The composition of wherein component (a) comprises a compound of Formula 1 or salt thereof.3. The composition of wherein component (a) comprises a compound selected from the group consisting of4-(2-chloro-4-fluorophenyl)-N-(2-fluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,4-(2-chloro-4-fluorophenyl)-N-(2-chlorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,N-(2-bromophenyl)-4-(2-chloro-4-fluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,4-(2-bromo-4-fluorophenyl)-N-(2-fluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,4-(2-bromo-4-fluorophenyl)-N-(2-chlorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,4-(2-bromo-4-fluorophenyl)-N-(2-bromophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,4-(2-chloro-4-fluorophenyl)-N-(2,6-difluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,4-(2-chloro-4-fluorophenyl)-N-(2-chloro-6-fluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,N-(2-bromo-6-fluorophenyl)-4-(2-chloro-4-fluoromethyl)-1,3-dimethyl-1H-pyrazol-5-amine,4-(2-bromo-4-fluorophenyl)-N-(2,6-difluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,4-(2-bromo-4-fluorophenyl)-N-(2-chloro-6-fluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine, and4-(2-bromo-4-fluorophenyl)-N-(2-bromo-6-fluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine.4. The composition of further comprising (c) at least one additional compound or agent that is biologically active.5. The composition of wherein component (c) comprises at least one fungicidal compound selected from the group consisting of:(c1) methyl benzimidazole carbamate fungicides;(c2) dicarboximide fungicides;(c3) demethylation inhibitor fungicides;(c4) phenylamide fungicides;(c5) amine/morpholine fungicides;(c6) phospholipid biosynthesis inhibitor fungicides;(c7) carboxamide fungicides;(c8) hydroxy(2-amino-)pyrimidine fungicides;(c9) anilinopyrimidine fungicides;(c10) N-phenyl carbamate fungicides;(c11) quinone outside inhibitor fungicides;(c12) ...

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Номер записи: 72
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 ...

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Номер записи: 73
17-01-2019 дата публикации

COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS

Номер: US20190016669A1
Автор: BENENATO Kerry E., CORNEBISE Mark
Принадлежит:

The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression. 2. The compound of claim 1 , wherein Ris selected from the group consisting of NH claim 1 , alkylamino claim 1 , and dialkylamino.3. The compound of claim 1 , wherein Ris selected from the group consisting of methylamino claim 1 , and dimethylamino.4. The compound of claim 1 , wherein Rand Rare the same.5. The compound of claim 4 , wherein Rand Rare Calkyl.6. The compound of claim 1 , wherein n is 3.8. The compound of claim 7 , wherein R′ is C9 alkyl.9. The compound of claim 7 , wherein l is 5.10. The compound of claim 7 , wherein o is 5.11. The compound of claim 7 , wherein Ris selected from the group consisting of NH claim 7 , alkylamino claim 7 , and dialkylamino.12. The compound of claim 7 , wherein Ris selected from the group consisting of methylamino and dimethylamino.14. A nanoparticle composition comprising a lipid component comprising a compound of .15. The nanoparticle composition of claim 14 , wherein the lipid component further comprises a phospholipid selected from the group consisting of 1 claim 14 ,2-dilinoleoyl-sn-glycero-3-phosphocholine (DLPC) claim 14 , 1 claim 14 ,2-dimyristoyl-sn-glycero-phosphocholine (DMPC) claim 14 , 1 claim 14 ,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) claim 14 , 1 claim 14 ,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) claim 14 , 1 claim 14 ,2-distearoyl-sn-glycero-3-phosphocholine (DSPC) claim 14 , 1 claim 14 ,2-diundecanoyl-sn-glycero-phosphocholine (DUPC) claim 14 , 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) claim 14 , 1 claim 14 ,2-di-O-octadecenyl-sn ...

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Номер записи: 74
21-01-2021 дата публикации

USE OF ISOTHIOCYANATE FUNCTIONAL SURFACTANTS AS NRF2 INDUCERS TO TREAT EPIDERMOLYSIS BULLOSA SIMPLEX AND RELATED DISEASES

Номер: US20210017130A1
Автор: Silver Michael E.
Принадлежит:

The present invention relates to methods and compositions for the prevention and treatment of keratin-based skin diseases. In particular, the application describes compositions and methods of treating a patient suffering from skin blistering comprising the use of phase II enzyme inducers and/or activity modifiers. 120-. (canceled)21. A method for treating a patient having a disorder resulting from mutations in the genes encoding keratin 5 and/or keratin 14 , comprising the step of administering to the patient a lysine derivative surfactant , wherein the lysine derivative surfactant comprises an alkanoyl substituent containing at least 8 carbon atoms bound to the α-nitrogen of the lysine , and further wherein the ε-nitrogen of the lysine forms part of an isothiocyanate functional group.22. The method according to claim 21 , wherein the patient is a mammal.23. The method according to claim 22 , wherein the mammal is a human. This application is a continuation of U.S. application Ser. No. 16/506,119, entitled “USE OF ISOTHIOCYANATE FUNCTIONAL SURFACTANTS AS NRF2 INDUCERS TO TREAT EPIDERMOLYSIS BULLOSA SIMPLEX AND RELATED DISEASES,” filed Jul. 9, 2019, now U.S. Pat. No. 10,640,464, which is a continuation of U.S. application Ser. No. 16/218,711, entitled “USE OF ISOTHIOCYANATE FUNCTIONAL SURFACTANTS AS NRF2 INDUCERS TO TREAT EPIDERMOLYSIS BULLOSA SIMPLEX AND RELATED DISEASES,” filed Dec. 13, 2018, now U.S. Pat. No. 10,343,990, which is a continuation-in-part of U.S. application Ser. No. 15/675,915, entitled “USE OF ISOTHIOCYANATE FUNCTIONAL SURFACTANTS AS NRF2 INDUCERS TO TREAT EPIDERMOLYSIS BULLOSA SIMPLEX AND RELATED DISEASES,” filed Aug. 14, 2017, which is a continuation-in-part of U.S. application Ser. No. 15/353,260, entitled “ISOTHIOCYANATE FUNCTIONAL SURFACTANTS, FORMULATIONS INCORPORATING THE SAME, AND ASSOCIATED METHODS OF USE,” filed Nov. 16, 2016, now U.S. Pat. No. 9,962,361, which is a continuation-in-part of U.S. application Ser. No. 15/297,304, entitled “ ...

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Номер записи: 75
28-01-2016 дата публикации

METHOD FOR PRODUCING POLYTHIOL COMPOUND, POLYMERIZABLE COMPOSITION FOR OPTICAL MATERIAL, AND USES THEREOF

Номер: US20160024242A1
Автор: KAWAGUCHI Masaru, Nishimura Takeshi
Принадлежит: MITSUI CHEMICALS., INC.

Provided is a method for producing a molded product comprising a step for preparing a polymerizable composition for optical materials and a step for curing the polymerizable composition for optical materials to produce the molded product. The step for preparing the polymerizable composition for optical materials comprises a step for preparing a defined polythiol compound and a step for preparing the polymerizable composition for optical materials from the polythiol compound. The step for preparing the defined polythiol compound comprises reacting 2-mercaptoethanol with a defined epihalohydrin compound at a temperature of 10° C. to 50° C. to obtain a defined polyalcohol compound, reacting the polyalcohol compound with thiourea in the presence of hydrogen chloride to obtain an isothiuronium salt, hydrolyzing the isothiuronium salt to obtain the polythiol compound, adding hydrochloric acid at a defined concentration to a solution of the polythiol compound, and washing the solution to purify the polythiol compound. 3. The method for producing a molded product according to claim 1 ,wherein the polymerizable composition for optical materials further comprises a polyiso(thio)cyanate compound.4. The method for producing a molded product according to claim 2 ,wherein the polymerizable composition for optical materials further comprises a polyiso(thio)cyanate compound. The present invention relates to a method for producing a polythiol compound, a polymerizable composition for optical materials, and uses thereof.Plastic lenses are lightweight, not easily breakable and tintable as compared with inorganic lenses. Therefore, in recent years, plastic lenses have rapidly been in wide use in optical devices such as spectacle lenses and camera lenses.It has become necessary for resins for plastic lenses to have more enhanced performances, and there have been demands for an increase in the refractive index, an increase in the Abbe number, a decrease in specific gravity, an increase ...

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Номер записи: 76
28-01-2016 дата публикации

Synthesis of a novel odorant

Номер: US20160024424A1
Автор: Kedar Ramesh Vaze
Принадлежит: Individual

A novel odorant of formula (I) wherein each of R 1 , R 2 , R 3 , R 3 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 are independently selected from H, CH 3 , and C 2 H 5 ; X is selected from —CH 2 OH, —CH 2 OCOCH 3 and —CHO, n is selected from 0 and 1. The dotted line represents double bond or single bond.

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Номер записи: 77
17-04-2014 дата публикации

METHOD FOR PRODUCING 2-CHLOROALLYL THIOCYANATE AND 2-CHLOROALLYL ISOTHIOCYANATE

Номер: US20140107367A1
Автор: Decker Matthias, Dunkel Ralf, Gerdes Peter, Himmler Thomas, LITTMANN Martin, LUI Norbert, Schnatterer Albert
Принадлежит: Bayer Intellectual Property GmbH

A process is described for producing 2-chloroallyl isothiocyanate from 2,3-dichloro-1-propene by reacting the 2,3-dichloro-1-propene with a thiocyanate in the presence of a phase transfer catalyst, without diluent or in the presence of up to 15 percent by weight based on 2,3-dichloropropene and simultaneously in the presence of an excess of from 10 to 200 mol percent of 2,3-dichloro-1-propene based on the thiocyanate. A process starting from 1,2,3-trichloropropane is also described. 2. The process according to claim 1 , wherein the amount used of a diluent is up to 10 percent by weight claim 1 , based on the 2 claim 1 ,3-dichloropropene of formula (III).3. The process according to claim 1 , where the amount used of a diluent is up to 5 percent by weight claim 1 , based on the 2 claim 1 ,3-dichloropropene of formula (III).4. The process according to any of claim 1 , where said reacting proceeds at a temperature range from 50 to 100° C. The present invention relates to a process for producing 2-chloroallyl thiocyanate of the formula (I) and 2-chloroallyl isothiocyanate of the formula (II).2-Chloroallyl thiocyanate of the formula (I) is a known compound (see by way of example EP 0761649). It is also known that 2-chloroallyl thiocyanate of the formula (I) can be produced by reacting, in a diluent, a 2,3-dihalo-1-propene, preferably 2,3-dichloro-1-propene of the formula (III)with a thiocyanate of the general formula (IV)M(SCN)  (IV),in whichAn example of a suitable diluent described for the known processes is acetonitrile (EP 446913; CN 1401646) or toluene, optionally with addition of a phase transfer catalyst (Shanghai Huagong 27 (2002) 25-27; J. Agric. Food Chem. 56 (2008) 10805-10810). However, the use of these diluents is disadvantageous for an industrial process. By way of example, the dilution of the starting materials can markedly reduce the reaction rate and thus prolong the reaction time required. The use of a diluent also unavoidably implies additional work-up ...

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Номер записи: 78
25-01-2018 дата публикации

PROCESS AND INTERMEDIATES FOR THE PREPARATION OF NEP INHIBITORS

Номер: US20180022690A1
Автор: MANDRELLI Francesca, MARTIN Benjamin, VENTURONI Francesco
Принадлежит:

The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route. 7. The process according to claim 6 , comprising the step of simultaneously or separately esterifiying the obtained compound of formula (1) claim 6 , or a salt thereof claim 6 , wherein R1 is hydrogen claim 6 , with a C-C-aliphatic alcohol claim 6 , to yield the compound of formula (1) wherein R1 is C-C-alkyl.15. (canceled)19. (canceled)21. (canceled)24. (canceled) The present invention relates to a new chemical synthesis route and intermediates useful for the preparation of neprilysin (NEP) inhibitors and their prodrugs, in particular for the NEP inhibitor prodrug sacubitril.The NEP inhibitor prodrug sacubitril (N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester; IUPAC name 4-{[(1S,3R)-1-([1,1′-biphenyl]-4-ylmethyl)-4-ethoxy-3-methyl-4-oxobutyl]amino}-4-oxobutanoic acid) is represented by the following formula (A)Sacubitril together with valsartan, a known angiotensin receptor blocker (ARB), forms a sodium salt hydrate complex, known as LCZ696, comprising the anionic forms of sacubitril and valsartan, sodium cations and water molecules in the molar ratio of 1:1:3:2.5, respectively (ratio of 6:6:18:15 in the asymmetric unit cell of the solid state crystal), and which is schematically present in formula (B).Said complex is also referred to by the following chemical names: Trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3′-methyl-2′-(pentanoyl{2″-(tetrazol-5-ylate)biphenyl-4′-ylmethyl}amino)butyrate] hemipentahydrate or Octadecasodium hexakis(4-{[(1S,3R)-1-([1,1′-biphenyl]-4-ylmethyl)-4-ethoxy-3-methyl-4-oxobutyl]amino}-4-oxobutanoate) hexakis(N-pentanoyl-N-{[2′-(1H-tetrazol-1-id-5-yl)[1,1′-biphenyl]-4-yl]methyl}-L- ...

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Номер записи: 79
22-01-2015 дата публикации

GGA AND GGA DERIVATIVES COMPOSITIONS THEREOF AND METHODS FOR TREATING NEURODEGENERATIVE DISEASES INCLUDING PARALYSIS INCLUDING THEM

Номер: US20150025077A1
Автор: Argade Ankush B., Datwani Akash, Ermini Florian, Pan Yonghua, Serizawa Hiroaki, Spencer Natalie
Принадлежит: COYOTE PHARMACEUTICALS, INC.

This invention relates to geranylgeranyl acetone (GGA) derivatives and the use of GGA, its isomers, and GGA derivatives in methods for inhibiting neural death, increasing neural activity, increasing axon growth and cell viability, and increasing the survival rate of subjects administered the GGA or GGA derivatives. 3. A novel compound of Table 1 or a pharmaceutically acceptable salt thereof.43. A pharmaceutical composition comprising a compound of any one of - and a pharmaceutically acceptable excipient.53. A pharmaceutical composition comprising a sufficient amount of 5E claims 1 , 9E claims 1 , 13E geranylgeranyl acetone or a GGA derivative of any one of - claims 1 , and optionally at least one pharmaceutical excipient claims 1 , wherein the sufficient amount is an amount which provides for a dosing of about 1 mg/kg/day to about 12 mg/kg/day to the patient.6. The pharmaceutical composition of claim 5 , wherein the 5E claim 5 , 9E claim 5 , 13E geranylgeranyl acetone is synthetic 5E claim 5 , 9E claim 5 , 13E geranylgeranyl acetone.7. A composition for increasing the expression and/or release of one or more neurotransmitters from a neuron at risk of developing pathogenic protein aggregates associated with AD or ALS claim 5 , said composition comprising a protein aggregate inhibiting amount of GGA or a GGA derivative.8. A composition for increasing the expression and/or release of one or more neurotransmitters from a neuron at risk of developing extracellular pathogenic protein aggregates claim 5 , said composition comprising an extracellular protein aggregate inhibiting amount of GGA or a GGA derivative.10. The method of claim 10 , wherein said pre-contacted neuron exhibits one or more of:(i) a reduction in the axon growth ability,(ii) a reduced expression level of one or more neurotransmitters,(iii) a reduction in the formation of synapses, and(iv) a reduction in electrical excitability.11. The method of claim 9 , wherein the neurostimulation comprises one or more ...

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Номер записи: 80
25-01-2018 дата публикации

ELECTROCATALYTIC HYDROGEN EVOLUTION AND BIOMASS UPGRADING

Номер: US20180023199A1
Автор: Sun Yujie
Принадлежит: Utah State University

Disclosed are systems for producing hydrogen gas and upgrading biomass reactants. The systems are able to couple the oxidation of the biomass reactant to hydrogen gas evolution using catalysts that include a metal component and a non-metal component. Also disclosed are methods of using the systems for producing hydrogen gas and upgrading a biomass reactant. 2. The system of claim 1 , wherein the catalyst is selected from the group consisting of cobalt phosphide claim 1 , nickel phosphide claim 1 , cobalt sulfide claim 1 , nickel sulfide claim 1 , nickel nitride claim 1 , cobalt oxide claim 1 , nickel oxide claim 1 , and a combination thereof.3. The system of claim 1 , wherein the conductive substrate is selected from the group consisting of copper claim 1 , nickel claim 1 , stainless steel claim 1 , glassy carbon claim 1 , nickel foam claim 1 , stainless steel foam claim 1 , titanium claim 1 , fluorine-doped tin oxide claim 1 , indium-doped tin oxide claim 1 , and a combination thereof.4. The system of claim 1 , wherein the cathode and the anode each include the same catalyst and conductive substrate.5. The system of claim 1 , wherein the first and second electrolyte each independently comprise potassium hydroxide claim 1 , sodium hydroxide claim 1 , sodium perchlorate claim 1 , borate buffer claim 1 , phosphate buffer claim 1 , or a combination thereof.6. The system of claim 1 , wherein the first and second electrolyte are each independently present at a concentration of from about 0.1 M to about 5 M.7. The system of claim 1 , wherein the alcohol or the aldehyde derived from a lignocellulosic biomass is present at a concentration of from about 1 mM to about 100 mM.8. The system of claim 1 , wherein the alcohol or the aldehyde derived from a lignocellulosic biomass is selected from the group consisting of 5-hydroxymethylfurfural (HMF) claim 1 , 3-hydroxypropionic acid claim 1 , glycerol claim 1 , sorbitol claim 1 , xylitol claim 1 , lactic acid claim 1 , ethanol ...

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Номер записи: 81
24-01-2019 дата публикации

PROCESS FOR PREPARING SUBSTITUTED 2-ARYLETHANOLS

Номер: US20190023633A1
Автор: BRÜCHNER Peter, Himmler Thomas
Принадлежит:

The invention relates to a process for preparing substituted 2-arylethanols of the formula (I) by reacting Grignard compounds of the formula (II) in the presence of a copper compound with ethylene oxide. Moreover, the invention relates to novel substituted 2-arylethanols of the formula (I). 2. Process for preparing a compound of formula (I) according to claim 1 , in which{'sup': 1', '5', '6, 'sub': 1', '6', '1', '2', '1', '4', '1', '4, 'R, Rindependently of one another represent C-C-alkyl, C-C-fluoroalkyl having 1 to 5 fluorine atoms, phenyl optionally substituted by C-C-alkyl, C-C-alkoxy, fluorine or chlorine, fluorine, chlorine or a radical OR, where'}{'sup': '6', 'sub': 1', '6', '1', '2, 'Rrepresents C-C-alkyl, C-C-fluoroalkyl having 1 to 5 fluorine atoms or phenyl,'}{'sup': 2', '3', '4', '6, 'sub': 1', '6', '1', '2', '1', '4', '1', '4, 'R, R, Rindependently of one another represent hydrogen, C-C-alkyl, C-C-fluoroalkyl having 1 to 5 fluorine atoms, phenyl optionally substituted by C-C-alkyl, C-C-alkoxy, fluorine or chlorine, fluorine, chlorine or a radical OR, where'}{'sup': '6', 'sub': 1', '6', '1', '2, 'Rrepresents C-C-alkyl, C-C-fluoroalkyl having 1 to 5 fluorine atoms or phenyl.'}3. Process for preparing a compound of formula (I) according to claim 1 , in which{'sup': 1', '5', '6, 'R, Rindependently of one another represent methyl, ethyl, n-propyl, iso-propyl, trifluoromethyl, phenyl optionally substituted by methyl, ethyl, n-propyl, iso-propyl, methoxy, ethoxy or fluorine, fluorine, chlorine or a radical OR, where'}{'sup': '6', 'sub': 2', '3', '2', '5, 'Rrepresents methyl, ethyl, n-propyl, iso-propyl, n-butyl, tert-butyl, CHF, CFor CFand'}{'sup': 2', '3', '4', '6, 'R, R, Rindependently of one another represent hydrogen, methyl, ethyl, n-propyl, iso-propyl, trifluoromethyl, phenyl optionally substituted by methyl, ethyl, n-propyl, iso-propyl, methoxy, ethoxy or fluorine, fluorine, chlorine or a radical OR, where'}{'sup': '6', 'sub': 2', '3', '2', '5, ' ...

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Номер записи: 82
24-01-2019 дата публикации

Opsin-Binding Ligands, Compositions and Methods of Use

Номер: US20190023649A1
Автор: Berman Judd, Garvey David S., Quach Tan
Принадлежит: BIKAM PHARMACEUTICALS, INC.

Compounds and compositions are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed. 115-. (canceled)17. The method of claim 16 , wherein said visual cycle product is a toxic visual cycle product.18. The method of claim 17 , wherein said toxic visual cycle product is lipofuscin or N-retinylidene-N-retinylethanolamine (A2E).19. The method of claim 16 , wherein said compound reduces mislocalization of said opsin protein.20. The method of claim 16 , wherein said opsin protein is present in a cell.21. The method of claim 20 , wherein said cell is a cone cell or rod cell.22. The method of claim 20 , wherein said cell is present in a mammalian eye.23. A method of inhibiting the formation or accumulation of a visual cycle product claim 20 , comprising contacting an opsin protein with a compound selected from the group consisting of:3-(trifluoromethyl)-N-((2,6,6-trimethylcyclohex-1-enyl)methyl)aniline hydrochloride (Compound 1);3-methyl-N-((2,6,6-trimethylcyclohex-1-enyl)methyl)aniline (Compound 2);3-((2,6,6-trimethylcyclohex-1-enyl)methylamino)benzamide (Compound 3);3-((2,6,6-trimethylcyclohex-1-enyl)methylamino)benzonitrile (Compound 4);3-chloro-N-((2,6,6-trimethylcyclohex-1-enyl)methyl)aniline (Compound 5);1-methyl-3-((2,6,6-trimethylcyclohex-1-enyl)methoxy)benzene (Compound 6);1-fluoro-3-((2,6,6-trimethylcyclohex-1-enyl)methoxy)benzene (Compound 7);1-chloro-3-((2,6,6-trimethylcyclohex-1-enyl)methoxy)benzene (Compound 8);1-(trifluoromethyl)-3-((2,6,6-trimethylcyclohex- ...

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Номер записи: 83
24-01-2019 дата публикации

SHIP1 MODULATORS AND METHODS RELATED THERETO

Номер: US20190023709A1
Автор: Bogucki David, Harwig Curtis, Mackenzie Lloyd F., Pettigrew Jeremy D., Raymond Jeffery R.
Принадлежит:

Compounds of formula (I): 2. The compound of wherein:C1, C4, C11 and C12 are each independently substituted with two hydrogens;C9 is substituted with one hydrogen;C14 is substituted with one hydrogen;C15 is substituted with two hydrogens;{'sup': 1', '8', '9, 'Ris —R—OR;'}{'sup': 2', '8', '9, 'Ris —R—OR;'}{'sup': 4a', '4b', '7', '3, 'sub': 2', '2', '2', '2', '3', '3, 'Ris hydrogen or alkyl, Ris a direct bond to the carbon to which Ris attached, and Ris —CHNHor —CHN(H)C(O)(CH)CH;'}{'sup': '5', 'Ris alkyl;'}{'sup': '6', 'Ris hydrogen;'}{'sup': '7', 'Ris hydrogen;'}{'sup': '8', 'each Ris independently a direct bond or a straight or branched alkylene chain; and'}{'sup': '9', 'each Ris independently hydrogen, alkyl, haloalkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl.'}3. The compound of wherein:C1, C4, C11 and C12 are each independently substituted with two hydrogens;C9 is substituted with one hydrogen;C14 is substituted with one hydrogen;C15 is substituted with two hydrogens;{'sup': '1', 'Ris —OH;'}{'sup': '2', 'sub': '2', 'Ris —CH—OH;'}{'sup': 4a', '4b', '7', '3, 'sub': 2', '2', '2', '2', '3', '3, 'Ris hydrogen or methyl, Ris a direct bond to the carbon to which Ris attached, and Ris —CHNHor —CHN(H)C(O)(CH)CH;'}{'sup': '5', 'Ris methyl;'}{'sup': '6', 'Ris hydrogen; and'}{'sup': '7', 'Ris hydrogen.'}4. The compound of selected from:(1S,3S,4R)-4-((3aS,6S,7R,7aS)-7-(aminomethyl)-3,3a-dimethyl-3a,4,5,6,7,7a-hexahydro-1H-inden-6-yl)-3-(hydroxymethyl)-4-methylcyclohexanol; andN-(((3aR,6S,7R,7aS)-6-((1R,2S,4S)-4-hydroxy-2-(hydroxymethyl)-1-methylcyclohexyl)-3a-methyl-3a,4,5,6,7,7a-hexahydro-1H-inden-7-yl)methyl)pentanamide.6. The compound of wherein:C1, C4, C11 and C12 are each independently substituted with two hydrogens;C9 is ...

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Номер записи: 84
24-01-2019 дата публикации

Sesquiterpene Biosensors and Uses Thereof

Номер: US20190024193A1
Автор: Patrick Nina, Strachan Cameron
Принадлежит: Prospect Bio, Inc.

In an aspect, the invention relates to nucleic acids encoding new bisabolol responsive biosensor polypeptides useful for detecting responses to stimuli, identifying new enzymes, and novel pathways in cells. In other aspects, the invention relates to genes which induce expression in response to bisabolol and the gene products encoded by those genes. In still another aspect, the invention relates to control regions that induce expression in response to bisabolol. In an aspect, the invention also relates to the use of the bisabolol responsive biosensors, bisabolol responsive control regions, and the genes and encoded polypeptides that are expressed in response to bisabolol. 1. A method for monitoring (−)-α-bisabolol , comprising the steps of: providing a host cell , wherein the host cell comprises a polynucleotide , wherein the polynucleotide comprises a nucleic acid encoding a reporter , a nucleic acid encoding a selection marker , a nucleic acid encoding a first ribosome binding site , a nucleic acid encoding a second ribosome binding site , and a control region that increases expression in response to a (−)-α-bisabolol wherein the control region includes at least one of a SEQ ID NOs: 41-60 , 62-136 , wherein the nucleic acid encoding the first ribosome binding site is operably linked to the nucleic acid encoding the reporter , wherein the nucleic acid encoding the second ribosome binding site is operably linked to the nucleic acid encoding the selection marker , and wherein the nucleic acid encoding the reporter and the nucleic acid encoding the selection marker are expressed from the control region that increases expression in response to the (−)-α-bisabolol; expressing the nucleic acid encoding the reporter when a (−)-α-bisabolol is present; and detecting the reporter.2. The method of claim 1 , wherein the host cell is a bacterium.3Escherichia coli.. The method of claim 2 , wherein the bacterium is an428. The method of claim claim 2 , wherein the (−)-α-bisabolol ...

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Номер записи: 85
23-01-2020 дата публикации

CAPSAZEPINE ANALOGS FOR THE TREATMENT OF CANCER AND OTHER PROLIFERATIVE DISEASES

Номер: US20200024276A1
Автор: GONZALES Cara B., McHARDY Stanton
Принадлежит: The Board of Regents of the University of Texas System

The present disclosure relates generally to derivatives of capsazepine and methods of use thereof. In some aspects, the present disclosure relates to using capsazepine derivatives to treat cancer or other hyperproliferative diseases. 2. The method of claim 1 , wherein Xis O.3. The method of claim 1 , wherein Xis S.4. The method according to claim 1 , wherein Ris —NRR claim 1 , wherein: Ris hydrogen claim 1 , alkyl claim 1 , substituted alkyl; and Ris aralkylor substituted aralkyl.512-. (canceled)1443-. (canceled)44. The method according to claim 1 , wherein Ris substituted aralkyl.4546-. (canceled)48. The method according to claim 1 , wherein the cancer is a carcinoma claim 1 , sarcoma claim 1 , lymphoma claim 1 , leukemia claim 1 , melanoma claim 1 , mesothelioma claim 1 , multiple myeloma claim 1 , or seminoma.49. The method according to claim 1 , wherein the cancer is of the bladder claim 1 , blood claim 1 , bone claim 1 , brain claim 1 , breast claim 1 , central nervous system claim 1 , cervix claim 1 , colon claim 1 , endometrium claim 1 , esophagus claim 1 , gall bladder claim 1 , gastrointestinal tract claim 1 , genitalia claim 1 , genitourinary tract claim 1 , head claim 1 , kidney claim 1 , larynx claim 1 , liver claim 1 , lung claim 1 , muscle tissue claim 1 , neck claim 1 , oral or nasal mucosa claim 1 , ovary claim 1 , pancreas claim 1 , prostate claim 1 , skin claim 1 , spleen claim 1 , small intestine claim 1 , large intestine claim 1 , stomach claim 1 , testicle claim 1 , or thyroid.5055-. (canceled)56. The method according to claim 1 , wherein the cancer is a solid tumor.57. The method according to claim 1 , wherein the method comprises injecting the compound directly into the tumor.58. (canceled)59. The method according to claim 1 , wherein the method comprises administering the compound systemically.60. (canceled)61. The method according to claim 1 , wherein the method further comprises alleviating pain.62. The method according to claim 1 , wherein ...

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Номер записи: 86
28-01-2021 дата публикации

Method for Preparing Crosslinker Compound

Номер: US20210024451A1
Автор: Gicheul KIM, Ji Eun Kim, Ki Hyun Kim, Won Taeck Lim, Wonmun Choi, Yongjin Kim
Принадлежит: LG Chem Ltd

The present disclosure relates to a method for preparing a crosslinker compound in which a crosslinker compound capable of using for the production of a super absorbent polymer can be obtained in a higher yield by a simple manner. The crosslinker compound obtained by the above method can be used as a thermally decomposable crosslinker in the process of producing a super absorbent polymer.

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Номер записи: 87
28-01-2021 дата публикации

ISOTHIOCYANATE FUNCTIONAL SURFACTANTS, FORMULATIONS INCORPORATING ISOTHIOCYANATE FUNCTIONAL SURFACTANTS AND ASSOCIATED METHODS FOR TREATING BIOFILMS

Номер: US20210024463A1
Автор: Silver Michael E.
Принадлежит:

The present invention relates to methods, formulations, and compositions for the treatment of biofilms. In particular, the application discloses isothiocyanate functional surfactants either alone or combination with adjunct agents to treat biofilms. One suitable isothiocyanate functional surfactant is represented by the following chemical structure: 120-. (canceled)21. A method , comprising the step of administering to a patient having a biofilm a composition comprising a isothiocyanate functional surfactant comprising an α-nitrogen and a ε-nitrogen , and wherein an alkyl and/or alkanoyl substituent comprising at least approximately 8 carbon atoms is associated with the α-nitrogen , and further wherein at least one isothiocyanate functional group is associated with the ε-nitrogen.22. The method according to claim 21 , wherein the composition comprising the isothiocyanate functional surfactant is administered to the patient at least one of orally claim 21 , intravenously claim 21 , intramuscularly claim 21 , intrathecally claim 21 , cutaneously claim 21 , subcutaneously claim 21 , transdermally claim 21 , sublingually claim 21 , buccally claim 21 , rectally claim 21 , vaginally claim 21 , ocularly claim 21 , otically claim 21 , and nasally.23. The method according to claim 21 , wherein the composition comprising the isothiocyanate functional surfactant is topically administered to the patient.24. The method according to claim 23 , wherein the amount of isothiocyanate functional surfactant in the composition topically administered to the patient ranges from approximately 0.5 nmol/cm2 to approximately 10 μmol/cm2.25. The method according to claim 24 , wherein the composition comprising the isothiocyanate functional surfactant is a topical preparation selected from the group consisting of ointment claim 24 , cream claim 24 , emulsion claim 24 , lotion and gel.26. The method according to claim 25 , wherein the composition further comprises one or more pharmaceutical ...

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Номер записи: 88
28-01-2021 дата публикации

ULTRA LOW RANGE CHLORINE MEASUREMENT

Номер: US20210025862A1
Автор: Das Amit
Принадлежит:

An embodiment provides a method for measuring total chlorine in a solution, including: preparing a thiocarbamate indicator; introducing the thiocarbamate indicator to a solution, wherein the solution contains an amount of monochloramine; adding an additive to the solution, wherein the additive accelerates the reaction rate between the thiocarbamate indicator and monochloramine and causes a change in fluorescence of the solution; and measuring the amount of monochloramine in the solution by measuring an intensity of the fluorescence. Other aspects are described and claimed. 1. A method for measuring total chlorine in a solution , comprising:preparing a thiocarbamate indicator;introducing the thiocarbamate indicator to a solution, wherein the solution contains an amount of monochloramine;adding an additive to the solution, wherein the additive accelerates the reaction rate between the thiocarbamate indicator and monochloramine and causes a change in fluorescence of the solution; andmeasuring the amount of monochloramine in the solution by measuring an intensity of the fluorescence.2. The method of claim 1 , wherein the thiocarbamate indicator comprises a thiocarbamate derivative of hydroxyl coumarin.3. The method of claim 1 , wherein the thiocarbamate derivative comprises 7-hydroxy-coumarin claim 1 , 7-hydroxy-4-methylcoumarin claim 1 , or mixtures thereof.4. The method of claim 1 , wherein the additive comprises phosphate.5. The method of claim 1 , wherein the additive comprises citrate.6. The method of claim 1 , wherein the additive comprises phosphate and citrate.7. The method of claim 5 , further comprising titrating a pH of the solution to a pH between 4 and 7.8. The method of claim 1 , further comprising titrating a pH of the solution to around a pH of between 5 and 6.9. The method of claim 1 , wherein the fluorescence intensity is correlated to a concentration of the monochloramine in the solution.10. The method of claim 1 , further comprising adding a buffer ...

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Номер записи: 89
04-02-2016 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20160029635A1
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”): 2. A molecule according to wherein R1 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.3. A molecule according to wherein R2 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.4. A molecule according to wherein R3 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , ...

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Номер записи: 90
04-02-2016 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20160029636A1
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”): 15-. (canceled)6. 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).7. A composition according to further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 38 , 1 claim 38 ,2-dichloropropane claim 38 , 1 claim 38 ,3-dichloropropene claim 38 , 1-methylcyclopropene claim 38 , 1-naphthol claim 38 , 2-(octylthio)ethanol claim 38 , 2 claim 38 ,3 claim 38 ,5-tri-iodobenzoic acid claim 38 , 2 claim 38 ,3 claim 38 ,6-TBA claim 38 , 2 claim 38 ,3 claim 38 ,6-TBA-dimethylammonium claim 38 , 2 claim 38 ,3 claim 38 ,6-TBA-lithium claim 38 , 2 claim 38 ,3 claim 38 ,6-TBA-potassium claim 38 , 2 claim 38 ,3 claim 38 ,6-TBA-sodium claim 38 , 2 claim 38 ,4 claim 38 ,5-T claim 38 , 2 claim 38 ,4 claim 38 ,5-T-2-butoxypropyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-2-ethylhexyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-3-butoxypropyl claim 38 , 2 claim 38 ,4 claim 38 ,5-TB claim 38 , 2 claim 38 ,4 claim 38 ,5-T-butometyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-butotyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-butyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-isobutyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-isoctyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-isopropyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-methyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-pentyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-sodium claim 38 , 2 claim 38 ,4 claim 38 ,5-T-triethylammonium claim 38 , 2 claim 38 ,4 claim 38 ,5-T-trolamine claim 38 , 2 claim 38 ,4-D claim 38 , 2 claim 38 , ...

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Номер записи: 91
02-02-2017 дата публикации

THIOSEMICARBAZONES INHIBITORS OF LYSOPHOSPHATIDIC ACID ACYLTRANSFERASE AND USES THEREOF

Номер: US20170027893A1
Автор: Lawrence Nicholas J., Sebti Said M., Springett Gregory
Принадлежит: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.

Lysophosphatidic acid acyltransferase-beta (LPAAT-β) catalyzes the production of phosphatidic acid (PA) from lysophosphatidic acid (LPA). The lipid cofactor PA contributes to the activation of c-Raf, BRAF, mTOR and PKC-ζ. LPAAT-β expression is a prognostic factor in gynecologic malignancies and is being investigated as a therapeutic target in a variety of tumor types. A class of thiosemicarbazones was identified as inhibitors of LPAAT-β from a screen of a library of small molecules. A focused library of thiosemicarbazones derivatives was prepared and led to the development of compounds which potently inhibit LPAAT-β and inhibit the growth of MiaPaCa2 human pancreatic cancer cells. 2. The compound of claim 1 , wherein Ris a Calkyl.3. The compound of claim 1 , wherein Ris propenyl.4. The compound of claim 1 , wherein Ris H.5. The compound of claim 1 , wherein Ris methyl.6. The compound of claim 1 , wherein n is 2.7. The compound of claim 1 , wherein n is 3.8. The compound of claim 1 , wherein n is 2 and each Ris chosen from F claim 1 , Cl claim 1 , Br claim 1 , and CN.9. The compound of claim 1 , wherein the compound inhibits LPAAT-β.10. A method of treating cancer in a subject claim 1 , comprising: administering a therapeutically effective amount of a compound of to a subject in need thereof.11. The method of claim 10 , wherein the cancer is pancreatic cancer.12. The method of claim 10 , wherein the compound is administered with an anti-cancer agent.13. The method of claim 10 , wherein the cancer is colon cancer.14. The method of claim 10 , wherein the subject is also administered regorafenib.15. A method of treating obesity in a subject claim 1 , comprising: administering a therapeutically effective amount of a compound of to a subject in need thereof. This invention was made with Government support under Grant No. CA131400 awarded by the National Institutes of Health. The government has certain rights in this invention.Phosphatidic acid (PA) is a cofactor required ...

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Номер записи: 92
29-01-2015 дата публикации

Substituted Phenylcarbamoyl Alkylamino Arene Compounds and N,N'-BIS-Arylurea Compounds

Номер: US20150031726A1
Автор: CHAKRAVARTY Sarvajit, JAIN Rajendra Parasmal
Принадлежит:

Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N′-substituted aryl urea compounds; N-substituted aryl, N′-substituted heteroaryl urea compounds; N-substituted aryl, N′-substituted aryl thiourea compounds and N-substituted aryl, N′-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein;{'sup': 1', 'a', 'b, 'sub': 1', '8, '(a) Ris —C-Calkyl-NRR;'}{'sup': 1', 'a', 'b', '2, 'sub': 1', '8, '(b) Ris —C-Calkyl-NRRand Ris halo; or'}{'sup': 1', 'a', 'b', '2, 'sub': 1', '8, 'claim-text': [{'sup': '1', '(i) Wis CN;'}, {'sup': '2', '(ii) Wis perhaloalkyl;'}, '(iii) Z is S;', {'sup': 1', '2, '(iv) Yand Yare both methyl and'}, '(v) T is C., '(c) Ris —C-Calkyl-NRR, Ris halo, and at least one of (i)-(v) applies3. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein:{'sup': 1', 'c', 'd, 'sub': 1', '8, '(a) Ris —O—C-Calkyl-NRR;'}{'sup': 1', 'c', 'd', '2, 'sub': 1', '8, '(b) Ris —O—C-Calkyl-NRRand Ris hydrogen; or'}{'sup': 1', 'c', 'd', '2, 'sub': 1', '8, 'claim-text': [{'sup': '1', '(i) Wis CN;'}, {'sup': '2', '(ii) Wis perhaloalkyl;'}, '(iii) Z is S;', {'sup': 1', '2, '(iv) Yand Yare both methyl and'}, '(v) T is C., '(c) Ris —O—C-Calkyl-NRR, Ris hydrogen, and at least one of (i)-(v) applies4. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein:{'sup': 1', 'e', 'f, '(a) Ris —C(O)NRR;'}{'sup': 1', 'e', 'f', '2, '(b) Ris —C(O)NRRand Ris halo; or'}{'sup': 1', 'e', 'f', '2, 'claim-text': [{'sup': '1', '(i) Wis CN;'}, {'sup': '2', '(ii) Wis perhaloalkyl or hydrogen ...

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Номер записи: 93
04-02-2016 дата публикации

SHIP1 MODULATORS AND METHODS RELATED THERETO

Номер: US20160031899A1
Автор: Bogucki David, Harwig Curtis, Mackenzie Lloyd F., MacRury Thomas B., Pettigrew Jeremy D., Raymond Jeffery R.
Принадлежит:

Compounds of formula (II): wherein A, R, R, Rand Rare described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds have activity as SHIP1 modulators, and thus may be useful in treating a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of the invention are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof. 3. The compound of wherein:{'sup': 1', '8', '9, 'Ris —R—OR;'}{'sup': 2', '8', '9, 'Ris —R—OR;'}{'sup': 3', '8', '9', '11', '8', '9', '12', '8', '9', '9a', '8', '9', '9a', '8', '9', '9a, 'sub': 2', '2', '2, 'Ris —R—N(R)C(O)R, —R—N(R)—R, —R—N(R)C(═NCN)N(R), —R—N(R)C(O)N(R)or —R—N(R)C(S)N(R);'}{'sup': 4a', '4b, 'Rand Rare each independently hydrogen, alkyl, alkenyl or alkynyl;'}{'sup': 4a', '4b', '7, 'or Ris hydrogen, alkyl, alkenyl or alkynyl and Ris a direct bond to the carbon to which Ris attached;'}{'sup': 4a', '4b, 'or Rand Rtogether form alkylidene or haloalkylidene;'}{'sup': 5', '5, 'Ris alkyl or Ris a direct bond to the carbon at C14;'}{'sup': 6', '8', '9', '8', '9, 'sub': '2', 'Ris hydrogen, —R—ORor —R—N(R);'}{'sup': 7', '8', '9', '8', '9', '7', '4b', '7, 'sub': '2', 'Ris hydrogen, —R—OR, —R—N(R), or a direct bond to C15, provided that when Ris a direct bond to C15, Ris not a direct bond to the carbon to which Ris attached;'}{'sup': '8', 'each Ris independently a direct bond or a straight or branched alkylene chain;'}{'sup': '9', 'each Ris hydrogen, alkyl, optionally substituted aryl and optionally substituted aralkyl;'}{'sup': '9a', 'each Ris hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl;'}optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, ...

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Номер записи: 94
29-01-2015 дата публикации

Compositions and Methods for Inhibition of Cathepsins

Номер: US20150031915A1
Автор: Chaplin David J., Gaddale Devanna Kishore Kumar, Parker Erica, Pinney Kevin G., Song Jiangli, Trawick Mary L.
Принадлежит:

This invention is directed to compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin K or cathepsin L, will be therapeutically useful. 220-. (canceled)21. A compound selected from the group consisting of:1,4-dibenzoylbenzene (1),3-benzoyl benzophenone thiosemicarbazone (3),4-Benzoyl benzophenone thiosemicarbazone (4),3-Benzoyl benzhydrol thiosemicarbazone (6),1-(3-methylbenzoyl),3-(3-methylbenzoyl)benzene thisosemicarbazone (9),1,3-bis(2-fluoro-benzoyl)-5-bromobenzene thiosemicarbazone (11),1,3-bis-(4-fluorobenzoyl)benzene thiosemicarbazone (13),1-(4-hydroxybenzoyl)-3-(4-methoxybenzoyl)benzene thiosemicarbazone (17),1-(4-methoxybenzoyl)-3-(4-hydroxybenzoyl)benzene thiosemicarbazone (18),1-(4-hydroxybenzoyl)-3-(4-methoxybenzoyl)benzene di-thiosemicarbazone (19),1,3-bis-(4-isopropoxybenzoyl)benzene thiosemicarbazone (22),1,3-bis-(4-isopropoxybenzoyl)benzene dithiosemicarbazone (23),1,3-bis-(4-bromobenzoyl)benzene thiosemicarbazone (24),1,3,5-Tribenzoyl benzene thiosemicarbazone (25),2-[(3-benzoylphenyl)(phenyl)methylene]-N-methylhydrazinecarbothioamide (27),2-[(3-benzoylphenyl)(phenyl)methylene]-1-methylhydrazinecarbothioamide (28), and1,3-bis-(4-methoxybenzoyl)benzene dithiosemicarbazone (33). This application claims the benefit of U.S. provisional patent application No. 61/615,097, filed on 23 Mar. 2012, which application is incorporated herein by reference in its entirety.A. FieldThe present invention relates to compounds and methods of using these compounds in the treatment of conditions in which modulation of the cathepsin, particularly cathepsin K or cathepsin L, is therapeutically useful.B. BackgroundThere are five classes of proteases including matrix metalloproteases (MMPs), cysteine proteases, serine proteases, aspartic proteases, and threonine proteases which catalyze the hydrolysis of peptide bonds. Due to their function in many disease states, including cancer ...

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Номер записи: 95
04-02-2016 дата публикации

LIQUID CRYSTAL COMPOUND, LIQUID CRYSTAL COMPOSITION AND LIQUID CRYSTAL DISPLAY DEVICE

Номер: US20160032187A1
Автор: SASADA Yasuyuki, Tanaka Hiroyuki
Принадлежит:

To provide a liquid crystal compound satisfying at least one of physical properties such as high stability to light, a high clearing point, low minimum temperature of a liquid crystal phase, small viscosity, suitable optical anisotropy, large dielectric anisotropy, a suitable elastic constant, excellent compatibility with other liquid crystal compounds and a large dielectric constant in a minor axis direction. 2. The compound according to claim 1 , wherein claim 1 , in formula (1) claim 1 , Ris alkyl having 1 to 15 carbons claim 1 , alkenyl having 2 to 15 carbons claim 1 , alkoxy having 1 to 14 carbons or alkenyloxy having 2 to 14 carbons claim 1 , and in the groups claim 1 , at least one of hydrogen may be replaced by fluorine; and Xis fluorine claim 1 , —C≡N claim 1 , —N═C═S claim 1 , —CHF claim 1 , —CHF claim 1 , —CF claim 1 , —(CH)—F claim 1 , —CHCF claim 1 , —CFCF claim 1 , —(CH)—F claim 1 , —(CH)—CF claim 1 , —(CF)—F claim 1 , —(CH)—F claim 1 , —(CH)—CF claim 1 , —(CF)—F claim 1 , —(CF)—F claim 1 , —(CF)—F claim 1 , —(CF)—F claim 1 , —OCHF claim 1 , —OCHF claim 1 , —OCF claim 1 , —O—(CH)—F claim 1 , —OCHCF claim 1 , —OCFCF claim 1 , —O—(CH)—F claim 1 , —O—(CH)—CF claim 1 , —O—(CF)—F claim 1 , —O(CH)—F claim 1 , —O—(CH)—CF claim 1 , —O—(CF)—F claim 1 , —O—(CF)—F claim 1 , -0—(CF)—F claim 1 , —CH═CHF claim 1 , —CH═CF claim 1 , —CF═CHF claim 1 , —CF═CF claim 1 , —CH═CHCHF claim 1 , —CH═CHCF claim 1 , —CF═CHCF claim 1 , —CF═CFCF claim 1 , —(CH)—CH═CF claim 1 , —(CH)—CF═CF claim 1 , —(CH)—CH═CHCF claim 1 , —(CH)—CF═CHCFor —(CH)—CF═CFCF.3. The compound according to claim 1 , wherein claim 1 , in formula (1) claim 1 , Ris alkyl having 1 to 10 carbons claim 1 , alkenyl having 2 to 10 carbons claim 1 , alkoxy having 1 to 9 carbons or alkenyloxy having 2 to 9 carbons claim 1 , and in the groups claim 1 , at least one of hydrogen may be replaced by fluorine; and Xis fluorine claim 1 , —C≡N claim 1 , —CF claim 1 , —CHF claim 1 , —OCF claim 1 , —OCHF claim 1 , —CH═CHCF ...

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Номер записи: 96
01-02-2018 дата публикации

METHODS FOR PRODUCING 2,6-DIMETHYL-1,5-HEPTADIEN-3-OL AND 2,6-DIMETHYL-1,5-HEPTADIEN-3-YL ACETATE

Номер: US20180029964A1
Автор: Kinsho Takeshi, Yamashita Miyoshi
Принадлежит: SHIN-ETSU CHEMICAL CO., LTD.

Provided are industrial and economical methods for producing 2,6-dimethyl-1,5-heptadien-3-yl acetate (3), which is, for example, a sex pheromone component of Comstock mealybug, and 2,6-dimethyl-1,5-heptadien-3-ol (2), which is an intermediate of the acetate (3). More specifically, provided are a method for producing 2,6-dimethyl-1,5-heptadien-3-ol comprising a step of subjecting 2-methyl-3-buten-2-yl 2-methyl-2-propenyl ether (1) to a rearrangement reaction in the presence of a base to obtain 2,6-dimethyl-1,5-heptadien-3-ol (2), and a method for producing 2,6-dimethyl-1,5-heptadien-3-yl acetate comprising a step of acetylating the produced 2,6-dimethyl-1,5-heptadien-3-ol (2) to obtain 2,6-dimethyl-1,5-heptadien-3-yl acetate (3). 2. The method for producing 2 claim 1 ,6-dimethyl-1 claim 1 ,5-heptadien-3-ol according to claim 1 , wherein the base is selected from the group consisting of metal alkoxides claim 1 , organometallic compounds claim 1 , and metal amides.4. The method for producing 2 claim 3 ,6-dimethyl-1 claim 3 ,5-heptadien-3-yl acetate according to claim 3 , wherein the base is selected from the group consisting of metal alkoxides claim 3 , organometallic compounds claim 3 , and metal amides. The invention relates to 2,6-dimethyl-1,5-heptadien-3-yl acetate, which is a sex pheromone component of Comstock mealybug (scientific name: ), and 2,6-dimethyl-1,5-heptadien-3-ol, which is an intermediate thereof.Since Comstock mealybug (scientific name: ) damages many fruit trees such as apples, pears, peaches and grapes and the excrement of this insect pest causes plant diseases, yield reduction and quality deterioration of these fruits have become a serious problem. At present, insecticides are used for the control of Comstock mealybug. However, they do not have a sufficient effect against the body of mealybugs covered with a waxy substance. Further, in order to prevent the insecticides from remaining on or in crops or prevent them from affecting the environment or ...

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Номер записи: 97
01-02-2018 дата публикации

Isothiocyanate compound and application thereof

Номер: US20180029979A1
Автор: Yongliang Yang
Принадлежит: Drivingforce Therapeutics Co Ltd

The present invention provides an isothiocyanate compound and its application. The compound is an aryl-substituted isothiocyanate compound that has a structure of the general formula I. The isothiocyanate compound of the present invention has very good solubility in water, far better inhibitory activity for XPO1 protein than other non-aryl substituted congeneric compounds, little side effects, and good biological safety and bioavailability, and is quite suitable for clinical application. Therefore, the isothiocyanate compound would have tremendous potential market space and economic benefits.

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Номер записи: 98
17-02-2022 дата публикации

DODECA-4,8,11-TRIEN-1-OL AND ITS USE AS AROMA CHEMICAL

Номер: US20220048842A1
Автор: BRU ROIG Miriam, Garlichs Florian, PELZER Ralf
Принадлежит:

The present invention relates to dodeca-4,8,11-trien-1-ol and a method of preparing same, to the use of dodeca-4,8,11-trien-1-ol as aroma chemical; to the use of dodeca-4,8,11-trien-1-ol for preparing an aroma chemical composition or for modifying the aroma character of an aroma chemical composition; to an aroma chemical composition containing dodeca-4,8,11-trien-1-ol; and to a method of preparing an aromatized composition or for modifying the aroma character of an aromatized composition. 1. A compound which is dodeca-4 ,8 ,11-trien-1-ol.2. The compound of which is selected from the group consisting of (4Z claim 1 ,8E)-dodeca-4 claim 1 ,8 claim 1 ,11-trien-1-ol claim 1 , (4E claim 1 ,8Z)-dodeca-4 claim 1 ,8 claim 1 ,11-trien-1-ol claim 1 , (4E claim 1 ,8E)-dodeca-4 claim 1 ,8 claim 1 ,11-trien-1-ol claim 1 , (4Z claim 1 ,8Z)-dodeca-4 claim 1 ,8 claim 1 ,11-trien-1-ol claim 1 , and mixtures of two or more thereof.3. The compound of which is (4Z claim 2 ,8E)-dodeca-4 claim 2 ,8 claim 2 ,11-trien-1-ol.4. The compound of which is (4E claim 2 ,8Z)-dodeca-4 claim 2 ,8 claim 2 ,11-trien-1-ol.5. The compound of which is a mixture of stereoisomers comprising (4Z claim 2 ,8E)-dodeca-4 claim 2 ,8 claim 2 ,11-trien-1-ol and (4E claim 2 ,8Z)-dodeca-4 claim 2 ,8 claim 2 ,11-trien-1-ol.6. The compound of claim 5 , where (4Z claim 5 ,8E)-dodeca-4 claim 5 ,8 claim 5 ,11-trien-1-ol and (4E claim 5 ,8Z)-dodeca-4 claim 5 ,8 claim 5 ,11-trien-1-ol are present in a molar ratio of from 10:1.7. The compound of claim 5 , wherein the mixture further comprises (4E claim 5 ,8E)-dodeca-4 claim 5 ,8 claim 5 ,11-trien-1-ol claim 5 , or (4Z claim 5 ,8Z)-dodeca-4 claim 5 ,8 claim 5 ,11-trien-1-ol claim 5 , or both (4E claim 5 ,8E)-dodeca-4 claim 5 ,8 claim 5 ,11-trien-1-ol and (4Z claim 5 ,8Z)-dodeca-4 claim 5 ,8 claim 5 ,11-trien-1-ol.8. Aroma chemical composition comprising the compound of :(i) at least one additional aroma chemical different from dodeca-4,8,11-trien-1-ol, or(ii) at least one non ...

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Номер записи: 99
31-01-2019 дата публикации

TETRAHYDRONAPHTHALENE DERIVATIVE

Номер: US20190031605A1
Автор: INAGAKI Yuichi, KUSUMI Kensuke, WATANABE Toshihide
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

A compound represented by general formula (I-1): 3. The compound according to claim 1 , wherein Y is —CH— or —O— claim 1 , or a pharmaceutically acceptable salt thereof.4. The compound according to claim 1 , wherein ring 1 is a C3-10 carbocyclic ring claim 1 , or a pharmaceutically acceptable salt thereof.5. The compound according to claim 1 , wherein ring 3 is a C3-7 saturated carbocyclic ring which may be substituted with a C1-4 alkyl group claim 1 , or a 3- to 7-membered saturated heterocyclic ring which may be substituted with a C1-4 alkyl group claim 1 , or a pharmaceutically acceptable salt thereof.6. The compound according to claim 1 , wherein Z is a carboxyl group which may be substituted with a C1-8 alkyl group claim 1 , or a pharmaceutically acceptable salt thereof.7. A pharmaceutical composition comprising the compound represented by general formula (I-1) according to claim 1 , or a pharmaceutically acceptable salt thereof.8. The pharmaceutical composition according to claim 7 , which is an S1Pbinder and/or modulator.9. The pharmaceutical composition according to claim 7 , which is an agent for preventing and/or treating a S1P-mediated disease.10. The pharmaceutical composition according to claim 9 , wherein the S1P-mediated disease is neurodegenerative disease claim 9 , autoimmune disease claim 9 , infection or cancer.11. The pharmaceutical composition according to claim 10 , wherein the neurodegenerative disease is schizophrenia claim 10 , Binswanger's disease claim 10 , multiple sclerosis claim 10 , neuromyelitis optica claim 10 , Alzheimer's disease claim 10 , cognitive impairment claim 10 , amyotrophic lateral sclerosis or spinocerebellar ataxia.12. A method for preventing and/or treating a S1P-mediated disease claim 1 , comprising administering to a mammal an effective amount of the compound represented by general formula (I-1) according to claim 1 , or a pharmaceutically acceptable salt thereof.1314-. (canceled)15. The compound according to claim 2 ...

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Номер записи: 100