ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ АЗОЛА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ЭТИ ПРОИЗВОДНЫЕ, И СПОСОБЫ ЛЕЧЕНИЯ БОЛЕЗНИ ПАРКИНСОНА С ПРИМЕНЕНИЕМ ЭТИХ ПРОИЗВОДНЫХ

... 1. Замещенное производное азола, представленное следующей формулой (I), или его фармацевтически приемлемая соль:формула (I),где R выбран из группы, состоящей из C-Cарилакила и C-Cгетероарилалкила; и линейного разветвленного или циклического C-Салкилов;Y выбран из группы, состоящей из О и N-R;Rобозначает по меньшей мере один заместитель, выбранный из группы, состоящей из Н и линейного или разветвленного C-Салкила;Rвыбран из группы, состоящей из Н и галогена;А выбран из группы, состоящей из N, О и S;В выбран из группы, состоящей из С и N;Z выбран из группы, состоящей из гетероциклического кольца; карбамата, -OC(=O)NRR; NH; NRR; NC(=NH)NHи -NC(=O)NH;каждый из Rи Rнезависимо выбран из группы, состоящей из Н; C-Cалкила, незамещенного или замещенного по меньшей мере одним заместителем, выбранным из группы, состоящей из NHи NRR; гетероциклического кольца, незамещенного или замещенного C-Салкилом; или Rи Rвместе могут образовать 5- или 7-членное гетероциклическое кольцо, незамещенное или замещенное ...

Method for producing aminothiazole derivative and production intermediate

PHENYL-2-HYDROXY-4,5-DIMETHOXY-BENZOATE AND DERIVATIVES

A compound of formula (3), useful in the production of a compound of formula (5), through the following scheme: (see formula 3) (see formula 4) (see formula 5) ...

METHOD FOR PRODUCING AMINOTHIAZOLE DERIVATIVE AND PRODUCTION INTERMEDIATE

A compound represented by formula (5a): (see formula 5a) and use of the compound as intermediate in a method for producing a compound represented by formula (7) below: (see formula 7) ...

composição antimicrobiana, método de preparação da composição, dispositivo médico e uso da composição

a presente invenção refere-se a formas sólidas com uma atividade antimicrobiana compreendendo um polissacarídeo e tri-iodeto, em que a decomposição do tri-iodeto em iodeto e iodo volátil é significativamente suprimida pela presença de um estabilizador, além disso, refere-se à sua preparação e utilização. comparadas às formas líquidas compreendendo tri-iodeto, as formas sólidas estabilizadas podem ser usadas para uma gama muito maior de aplicações devido à sua estabilidade de forma e a um volume (peso) significativamente menor de material total. polissacarídeo, em que o polissacarídeo compreende ácido hialurônico ou um derivado quimicamente modificado, alginato de sódio, oxicelulose, carboximetil celulose ou hidroxietil celulose, r é uma cadeia alquil c1 ? c30 aromática, heteroaromática, linear ou ramificada, opcionalmente contendo átomos de n ou o, r1 é uma cadeia alquil c1 ? c30 aromática, heteroaromática, linear ou ramificada, contendo opcionalmente átomos de n ou o, ou ?h, em que r1 no estabilizador são independentemente iguais ou diferentes.

Substituted azole derivatives, pharmaceutical composition containing the derivatives, and method for treating Parkinson's disease using the same

Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.

AZA-HETEROCYCLIC COMPOUNDS USED TO TREAT NEUROLOGICAL DISORDERS AND HAIR LOSS

The present invention is directed to novel carboxylic acids and isosteres of heterocyclic ring compounds of formula (I) which have multiple heteroatoms within the heterocyclic ring, novel derivatives containing N-linked diketos, sulfonamides, ureas and carbamates attached thereto, their preparation and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, as well as for treating alopecia and promoting hair growth. A, X, Y, Z, D and n are as defined in the application.

METHOD FOR PRODUCING AMINOTHIAZOLE DERIVATIVE AND PRODUCTION INTERMEDIATE

A compound of formula (3), useful in the production of a compound of formula (5), through the following scheme: (see formula 3) (see formula 4) (see formula 5) ...

METHOD FOR PRODUCING AMINOTHIAZOLE DERIVATIVE AND PRODUCTION INTERMEDIATE

A method for producing a compound represented by the formula (3) below through the following reactions: (see formula 1) (see formula 2) (see formula 3) ...

AZA - HETEROCYCLIC COMPOUNDS, USEFUL FOR TREATING NEUROLOGICAL DISORDERS AND HAIR LOSS

PROCEDURE FOR THE PRODUCTION OF A AMINOTHIAZOLDERIVATS AND INTERMEDIATE PRODUCT

Improved process for the preparation of {1S-(1R*, 2S*, 3R*)}-N-(4-(morpholinylsulfonyl)-L-phenylalanyl-3-(2-amino-4 -thiazolyl)-N-{(1-cyclohexylmethyl)-2,3-dihydroxy-5- methylhexyl}-L-alaninamide

Aza-heterocyclic compounds used to treat neurological disorders and hair loss

METHOD FOR PRODUCING AMINOTHIAZOLE DERIVATIVE AND PRODUCTION INTERMEDIATE

A compound represented by formula (5a): (see formula 5a) and use of the compound as intermediate in a method for producing a compound represented by formula (7) below: (see formula 7)

SUBSTITUTED AZOLE DERIVATIVES, PHARMACEUTICAL COMPOSITION CONTAINING THE DERIVATIVES, AND METHOD FOR TREATING PARKINSON'S DISEASE USING THE SAME

Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.

FUNGICIDAL N-[2-(HALOALKOXY)PHENYL]HETEROARYLCARBOXAMIDES

N-[2-(Haloalkoxy)phenyl]heteroarylcarboxamides of the formula I, where n = 0 or 1, Hal = halogen, X = C2-C4-haloalkyl, Het = a pyrazole, thiazole or pyridine radical (a), (b) or (c), where R1 = C1-C4-alkyl or C1-C4-haloalkyl, R2 = hydrogen or halogen, R3 = C1-C4-alkyl or C1-C4-haloalkyl and R5 = halogen, C1-C4-alkyl or C1-C4-haloalkyl; except for N-[2-(1,1,2,2-tetrafluoroethoxy)phenyl]-1,3-dimethylpyrazol-4-yl-carbox-amide, N-[2-(1,1,2,2-tetrafluoroethoxy)phenyl]-3-trifluoromethyl-1-methylpyrazol-4-yl- carboxamide and N-[2-(2,2,2-trifluorethoxy)phenyl]-3-trifluormethyl-1-methylpyrazol-4-yl-carboxamide. A fungicidal composition comprising at least one compound I, the use of the compounds I for preparing a composition suitable for controlling harmful fungi, a method for controlling harmful fungi using the compounds I and also seed comprising at least one compound I.

Process for the preparation of [1S-(1R*,2S*,3R*)]-N-(4-morpholinylsulfonyl)-L-phenylalanyl-3-(2-amino-4-thiazolyl-N-[(1-cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl]-L-alaninamide

An improved process for the preparation of [1S-(1R*,2S*,3R*)]-N-(4-morpholinylsulfonyl)-L-phenylalanyl-3-(2-amino -4-thiazolyl)-N-[(1-cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl]-L-a laninamide is described where the key intermediate, 3-(2-amino-4-thiazolyl)-L-alanine is converted without protecting the aminothiazole group to the desired compound, as well as valuable intermediates used in the process.

ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ АЗОЛА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ЭТИ ПРОИЗВОДНЫЕ, И СПОСОБЫ ЛЕЧЕНИЯ БОЛЕЗНИ ПАРКИНСОНА С ПРИМЕНЕНИЕМ ЭТИХ ПРОИЗВОДНЫХ

FIELD: medicine, pharmaceutics. SUBSTANCE: invention refers to a substituted azol derivative presented by the following formula (I) 3-(4-benzyloxy-3,5-dimethyl-phenyl)-isoxazol-5-ylmethyl ester of carbamic acid, 3-(4-prop-2-inyl-oxyphenyl)-isoxazol-5-ylmethyl ester of carbamic acid or 2-{[3-(4-benzyloxy-phenyl)-isoxazol-5-ylmethyl]-amino}-propionamide or its pharmaceutically acceptable salt, wherein R is specified in a group consisting of C 4 -C 15 arylalkyl unsubstituted or substituted by at least one substitute specified in a group consisting of halogen, trifluoromethyl, trifluoralkoxy, -NO 2 , C(=O)OCH 3 , linear or branched C 1 -C 6 alkyl, C 1 -C 6 alkoxy, phenyl, phenyloxy, benzyloxy, -C(=O)H, -OH and -C=N-OH; C 4 -C 15 heteroarylalkyl unsubstituted or substituted by at least one substitute specified in a group consisting of halogen, C(=O)OCH 3 , linear or branched C 1 -C 6 alkyl, C 1 -C 6 alkoxy, phenyl, phenyloxy, benzyloxy; linear, branched or cyclic C 1 -C 10 alkyl substituted by at least one substitute specified in a group consisting of C 1 -C 3 -alkyloxy, C 1 -C 3 alkylthio, carbamate, tert-butyl-OC(=O)NH-, -NH 3   + , -NH 2 , -OH, -C(=O)OCH 2 CH 3 , -NHC(=O)NH 2 , trifluoromethylsulphanyl, trifluoromethyl and -CN; wherein when R represents C 4 -C 15 -heteroarylalkyl, a heteroaryl group is specified in a group consisting of imidazol, chlorthiophen, benzothiazol, pyridine, quinoline, benzotriazol, isoxazol, furan, N-oxopyridine, N-methylpyridine and benzo[1,3]dioxol, and when R means C 4 -C 15 arylalkyl, wherein aryl is specified in a group consisting of phenyl, phenyloxy, benzyloxy and naphthalinyl, Y is specified in a group consisting of O and N - R 1 , R 1 means a substitute specified in a group consisting of H and linear or branched C 1 -C 3 alkyl; R 2 is specified in a group consisting of H and halogen; A is specified in a group consisting of O and S; B represents C; Z is specified in a group consisting of imidazol, pyrrolidine and tetrazol ...

СПОСОБ ПОЛУЧЕНИЯ АЛКИЛ- И АЦИЛ-ЗАМЕЩЕННЫХ ТИАЗОЛОВ

Изобретение относится к получению алкил- и ацил-замещенных тиазолов, которое представляет собой кислотно-катализируемую реакцию циклизации, включающему внесение в реактор, снабженный механической мешалкой, капельной воронкой и обогреваемой рубашкой, 2,5-дизамещенного-2,5-дигидрокси-1,4-дитиана, мочевины в воде в присутствии лимонной кислоты и нагрева суспензии до 94°С. В реактор вносят алифатические или ароматические альдегиды, реакционную смесь нагревают и выдерживают в течение 2 часов с поддержанием температуры до 100°С при постоянном перемешивании. Полученную смесь фракционируют при пониженном давлении 100 мм. рт.ст. и по окончании процесса образования алкил- и ацил-замещенных тиазолов собирают кипящую фракцию. Технический результат заключается в упрощении способа, снижении количества стадий, исключении и снижении используемых реагентов, усложняющих способ и высоком выходе целевых веществ. 1 з.п. ф-лы, 3 пр.

Антимикробная композиция, содержащая полисахарид, стабилизирующий агент и трийодид, способ её получения и применение

INHIBITORS OF SHORT-CHAIN DEHYDROGENASE ACTIVITY FOR TREATING FIBROSIS

A method of treating or preventing a fibrotic disease, disorder or condition includes administering to a subject in need of treatment a 15-PGDH inhibitor.

Method for producing aminothiazole derivative and production intermediate

INHIBITORS OF SHORT-CHAIN DEHYDROGENASE ACTIVITY FOR TREATING FIBROSIS

A method of treating or preventing a fibrotic disease, disorder or condition includes administering to a subject in need of treatment a 15-PGDH inhibitor. SW033291 Application Increases Survival and Weight Maintenance in IPF Vehicle (x2 daily) + 2mg/kg Bleomycin Intratracheal Instillation 35 day survival 5.0 mpk 291(+) (x2 daily) Fig. 1 A Vehicle vs.1mgkg SWO Weight Change 95 -.- SWO33291 70- P=0.002 10 20 30 40 Days Post 2mg/kg Bleomyin N= 10 mice/group Fig. 2A Survival of C57 Mice post 2 mg/kg Beomycin 90 e-SWOV33291 > U Vehidle P=0.0617 o 1 20 30: 40 Days post Bloe Fig. 2B N= 25 mice/group ...

Inhibitors of short-chain dehydrogenase activity for treating fibrosis

A method of treating or preventing a fibrotic disease, disorder or condition includes administering to a subject in need of treatment a 15-PGDH inhibitor.

Fungicidal N-[2-(haloalkoxy)phenyl]heteroarylcarboxamides

N-[2-(Haloalkoxy)phenyl]heteroarylcarboxamides of the formula I, where n = 0 or 1, Hal = halogen, X = C2-C4-haloalkyl, Het = a pyrezole, thiazole or pyridine radical (a), (b) or (c), where R1 = C1-C4-alkyl or C1-C4-haloalkyl, R2 = hydrogen or halogen, R3 = C1-C4-alkyl or C1-C4-haloalkyl and R5 = halogen, C1-C4alkyl or C1-C4-haloalkyl; except for N-[2-(1,1,2,2-tetrafluoroethoxy)phenyl]-1,3-dimethylpyrazol-4-yl-carbox-amide, N-[2-(1,1,2,2-tetrafluoroethoxy)phenyl]-3-trifluoromethyl-1-methylpyrazol-4-yl-carboxamide and N-[2-(2,2,2-trifluorethoxy)phenyl]-3-trifluormethyl-1-methylpyrazol-4-yl-carboxamide. A fungicidal composition comprising at least one compound I, the use of the compounds I for preparing a composition suitable for controlling harmful fungi. a method for controlling harmful fungi using the compounds I and also seed comprising at least one compound I.

O-cyclopropylcyclohexyl-carboxanilides and their use as fungicides

The present invention relates to O-CYCLOPROPYLCYCLOHEXYL-CARBOXANILIDES derivatives of formula (I); their process of preparation, their use as fungicide, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.

Method for producing aminothiazole derivative and production intermediate

Disclosed is a selective demethylation process of a 2-methoxy group. Specifically disclosed is a method for producing a compound represented by the formula (7) below through the following reactions.

METHOD FOR PRODUCING 2-HYDROXYBENZOIC ACID DERIVATIVES

The present invention relates to a method for producing 2-hydroxybenzoic acid derivatives represented by the formula (3) below through the following reactions: (see formula 1) .fwdarw. (see formula 2) .fwdarw. (see formula 3), where the compound of formula (I ) reacts with a Lewis acid, wherein said Lewis acid is BF3, TiCI4 or AICl3. The invention further relates to a method for selectively demethylating the 2-methoxy group of an aromatic carboxylic acid, and providing an industrial method for producing an aminothiazole derivative useful as a medicine.

SUBSTITUTED AZOLE DERIVATIVES, PHARMACEUTICAL COMPOSITION CONTAINING THE DERIVATIVES, AND METHOD FOR TREATING PARKINSON'S DISEASE USING THE SAME

Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.

IMPROVED PROCESS FOR THE PREPARATION OF {1S-(1R*, 2S*, 3R*)}-N-(4-(MORPHOLINYLSULFONYL)-L-PHENYLALANYL-3-(2-AMINO-4 -THIAZOLYL)-N-{(1-CYCLOHEXYLMETHYL)-2,3-DIHYDROXY-5- METHYLHEXYL}-L-ALANINAMIDE

IMPROVED PROCESS FOR THE PREPARATION OF [1S-(1R*,2S*,3R*)]-N-(4-MORPHOLINYLSULFONYL)-L-PHENYLALANYL-3-(2-AMINO-4-THIAZOLYL)-N-[(1-CYCLOHEXYLMETHYL)-2,3-DIHYDROXY-5-METHYLHEXYL]-L-ALANINAMIDE

... 2106673 9218486 PCTABS00016 An improved process for the preparation of ¢1S-(1R*, 2S*, 3R*)!-N-(4-morpholinylsulfonyl)-L-phenylalanyl-3-(2-amino-4-thiazolyl)-N-¢(1-_ cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl!-L-alaninamide is described where the key intermediate, 3-(2-amino-4-thiazolyl)-L-alanine is converted without protecting the aminothiazole group to the desired compound, as well as valuable intermediates used in the process.

METHOD FOR PRODUCING AMINOTHIAZOLE DERIVATIVE AND PRODUCTION INTERMEDIATE

Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.

Multiple heteroatom containing heterocyclic ring compounds substituted with carboxylic acids and isosteres thereof

The present invention is directed to novel carboxylic acids and isosteres of heterocyclic ring compounds which have multiple heteroatoms within the heterocyclic ring, novel derivatives containing N-linked diketos, sulfonamides, ureas and carbamates attached thereto, their preparation and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, as well as for treating alopecia and promoting hair growth.

Inhibitors of short-chain dehydrogenase activity for treating fibrosis

A method of treating or preventing a fibrotic disease, disorder or condition includes administering to a subject in need of treatment a 15-PGDH inhibitor.

derivados de azol substituídos, composição farmacêutica contendo os derivados, e método para o tratamento de doença de parkinson usando os mesmos

METHOD OF INHIBITING TAU PHOSPHORYLATION

A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. - 134.-. (canceled)35. A method of inhibiting a TLR4-mediated immune response that comprises administering to TLR4-containing cells in recognized need thereof an effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 , inhibits at least about 60 percent and more preferably about 70 percent of the FITC-labeled naloxone binding when present at a 10 μM concentration and using unlabeled naloxone as the control inhibitor at the same concentration , and contains at least four of the six pharmacophores of , said administration being carried out in the absence of a mu opioid receptor- (MOR-) binding effective amount of a separate MOR agonist or antagonist.36. The method according to claim 35 , wherein said compound contains at least five of the six pharmacophores of .37. The method according to claim 35 , wherein said compound or a pharmaceutically acceptable salt thereof is present dissolved or dispersed in a pharmaceutically acceptable diluent as a pharmaceutical composition when administered.38. The method according to claim 35 , wherein said compound exhibits less than about 80 percent the MOR stimulation provided by DAMGO at the same concentration.47. The method according to claim 46 , wherein said anion claim 46 , X claim 46 , is selected from the group consisting of phosphate claim 46 , hydrogenphosphate claim 46 , dihydrogenphosphate claim 46 , sulfate claim 46 , bisulfate claim 46 , chloride claim 46 , bromide claim 46 , iodide claim 46 , acetate ...

derivado de azol substituído, inibidor de monoamina-oxidase b (maob) e composição farmacêutica contendo os derivadospara o tratamento de doença de parkinson

Substituted azole derivatives, pharmaceutical composition containing the derivatives, and method for treating Parkinson's disease using the same

Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.

Carboxylic acid of aza-heterocyclic compounds contg. multiple hetero-atoms or its electronic isosteric object

Method of inhibiting tau phosphorylation

A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35-40.

Method for producing aminothiazole derivative and production intermediate

Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.

HETEROCYCLIC CARBOXYLIC ACID AMIDE LIGAND AND APPLICATIONS THEREOF IN COPPER CATALYZED COUPLING REACTION OF ARYL HALOGENO SUBSTITUTE

HETEROCYCLIC RING COMPOUNDS CONTAINING MULTIPLE HETEROATOM, SUBSTITUTED BY CARBOXYLIC ACIDS, AND THEIR ISOSTERES

The present invention is directed to novel carboxylic acids and isoteres of heterocyclic ring compounds of formula which have multiple heteroatoms within the heterocyclic ring, novel derivatives containing N-linked diketos, sulfonamides, ureas and carbamates attached thereto, their preparation and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, as well as for treating alopecia and promoting hair growth. A, X, Y, Z, D and n are as defined in the application. 30 claims, 3 figures ...

AZA-HETEROCYCLIC COMPOUNDS USED TO TREAT NEUROLOGICAL DISORDERS AND HAIR LOSS

La présente invention concerne de nouveaux acides carboxyliques et isostères de composés de la formule (I) ayant un noyau hétérocyclique à plusieurs hétéroatomes, A, X, Y,Z, D et n étant, dans ladite formule, tels que définis dans le mémorandum descriptif. L'invention concerne également de nouveaux dérivés contenant des dicétones à liaison N, des sulfonamides, des urées et des carbamates attachés auxdits dérivés. L'invention concerne en outre la préparation desdits composés et leur utilisation pour traiter des troubles neurologiques (y compris des nerfs physiquement altérés) et de maladies neurodégénératives, ainsi que pour traiter l'alopécie et activer la pousse des cheveux.

METHOD FOR PRODUCING AMINOTHIAZOLE DERIVATIVE AND PRODUCTION INTERMEDIATE

A METHOD OF INHIBITING TAU PHOSPHORYLATION

AZA-HETEROCYCLIC COMPOUNDS USED TO TREAT NEUROLOGICAL DISORDERS AND HAIR LOSS

O-cyclopropylcyclohexyl-carboxanilides and their use as fungicides

The present invention relates to O-CYCLOPROPYLCYCLOHEXYL-CARBOXANILIDES derivatives of formula (I); their process of preparation, their use as fungicide, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.

Antimicrobial composition comprising polysaccharide, stabilizer and triiodide, method for producing the same and use thereof

SUBSTITUTED AZOLE DERIVATIVES, PHARMACEUTICAL COMPOSITION CONTAINING THE DERIVATIVES, AND METHOD FOR TREATING PARKINSON'S DISEASE USING THE SAME

derivado de azol substituído, inibidor de monoamina-oxidase b (maob) e composição farmacêutica contendo os derivadospara o tratamento de doença de parkinson

METHOD FOR PRODUCING AMINOTHIAZOLE DERIVATIVE AND PRODUCTION INTERMEDIATE

SUBSTITUTED AZOLE DERIVATIVES, PHARMACEUTICAL COMPOSITION CONTAINING THE DERIVATIVES, AND METHOD FOR TREATING PARKINSON'S DISEASE USING THE SAME

Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.

o-ciclopropilciclohexil-carboxanilidas e sua aplicação como fungicidas

ANTIMICROBIAL COMPOSITION COMPRISING A POLYSACCHARIDE, A STABILIZING AGENT AND TRIIODIDE, METHOD OF PREPARATION THEREOF AND USE THEREOF

A composition having antimicrobial activity is provided. The composition comprises a polysaccharide, a stabilizer, and a triiodide, where the triiodide decomposition to iodide and volatile iodine can be significantly suppressed by the presence of the stabilizer. Methods of preparing and using the composition and devices prepared therewith are also disclosed. As compared to liquid forms comprising triiodide, stabilized solid forms can be used for a much wider range of applications due to their shape stability and a significantly smaller volume and weight of total material.

SUBSITUTED AZOLE DRIVATIVE COMPOUND, A PHARMACEUTICAL COMPOSITION CONTAINING THE SAME, AND A METHOD FOR TREATING PARKINSON'S DISEASE USING THE SAME

PURPOSE: A substituted azole derivative compound and a composition containing the same for treating Parkinson's disease are provided. CONSTITUTION: A substituted azole derivative compound is denoted by chemical formula I. A monoamine-B(MAO-B) inhibitor contains a compound of chemical formula I or a pharmaceutically acceptable amount of salt and pharmaceutically acceptable carrier. A pharmaceutical composition for treating Parkinson's disease contains the compound of chemical formula I or a pharmaceutically acceptable amount of salt and pharmaceutically acceptable carrier. COPYRIGHT KIPO 2011 ...

O-CYCLOPROPYLCYCLOHEXYL-CARBOXANILIDES AND THEIR USE AS FUNGICIDES

The present invention relates to O-cyclopropylcyclohexyl-carboxanilides derivatives of formula (I), their process of preparation, their use as fungicide, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.

AZOLE DERIVATIVES, COMPOSITION COMPRISING THEREOF AND METHOD FOR TREATING PARKINSON'S DISEASE USING THE COMPOUNMD

본 발명은 치환된 아졸 유도체 화합물 및 이들의 약제학적으로 허용 가능한 염, 상기 화합물을 유효량 포함하는 약제학적 조성물, 및 상기 화합물을 포유류에 유효량 투여함을 특징으로 하는 포유류의 파킨슨씨 병 치료방법에 관한 것으로, 하기 화학식 (I)의 아졸 유도체 화합물 및 이들의 약제학적으로 유용한 염은 MAO-B 활성억제 효과로 인한 파킨슨씨 병 치료효능을 가진다. The present invention relates to a substituted azole derivative compound and a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising an effective amount of the compound, and a method for treating Parkinson's disease in a mammal, characterized in that the compound is administered to the mammal in an effective amount. In that, The azole derivative compounds of formula (I) below and their pharmaceutically useful salts have Parkinson's disease therapeutic efficacy due to their MAO-B inhibitory effect.

O-CYCLOPROPYLCYCLOHEXYL-CARBOXANILIDES AND THEIR USE AS FUNGICIDES

METHOD FOR PRODUCING AMINOTHIAZOLE DERIVATIVE AND PRODUCTION INTERMEDIATE

Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.

O-cyclopropylcyclohexyl-carboxanilides and their use as fungicides

The present invention relates to O-cyclopropylcyclohexyl-carboxanilides derivatives of formula (I), their process of preparation, their use as fungicide, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.

COMPOSITIONS FOR IMPROVING THE APPEARANCE OF SKIN

The present invention describes methods for improving the appearance of skin, particularly, treating, ameliorating, preventing, delaying, and/or improving one or more signs of aging, by topically applying compositions comprising aryl-thiazole compounds.

FUNGICIDAL N-[2-(HALOALKOXY)PHENYL]HETEROARYLCARBOXAMIDES

METHOD FOR PRODUCING AMINOTHIAZOLE DERIVATIVE AND PRODUCTION INTERMEDIATE

Method for producing aminothiazole derivative and production intermediate

METHOD OF INHIBITING TAU PHOSPHORYLATION

A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. - 168.-. (canceled)70. The method according to claim 69 , wherein said compound or a pharmaceutically acceptable salt thereof is present dissolved or dispersed in a pharmaceutically acceptable diluent as a pharmaceutical composition when administered.85. The method according to claim 69 , wherein said administration is carried out a plurality of times.86. The method according to claim 85 , wherein said administration is carried out daily.87. The method according to claim 85 , wherein said administration is carried out multiple times daily.88. The method according to claim 70 , wherein said pharmaceutical composition is in liquid form.89. The method according to claim 70 , wherein said pharmaceutical composition is in solid form. This application is a continuation of application Ser. No. 16/030,494 of the same title filed on Jul. 9, 2018 that is now U.S. Pat. No. 10,760,052, that itself was a division of application Ser. No. 13/940,016 of the same title filed on Jul. 11, 2013 and is now U.S. Pat. No. 10,017,736, which claims priority from application Ser. No. 61/789,180 that was filed on Mar. 15, 2013, and application Ser. No. 61/671,235 that was filed on Jul. 13, 2012, whose disclosures are incorporated herein by reference.The present invention contemplates a method of central nervous system (CNS) treatment to inhibit the formation of hyperphosphorylated tau protein and the use of a contemplated compound in the manufacture of a medicament for inhibiting tau protein hyperphosphorylation that can lead to pathological formation of ...

HETEROCYCLIC CARBOXYLIC ACID AMIDE LIGAND AND APPLICATIONS THEREOF IN COPPER CATALYZED COUPLING REACTION OF ARYL HALOGENO SUBSTITUTE

Provided are a heterocyclic carboxylic acid amide ligand and applications thereof in a copper catalyzed coupling reaction. Specifically, provided are uses of a compound represented by formula (I), definitions of radical groups being described in the specifications. The compound represented by formula (I) can be used as the ligand in the copper catalyzed coupling reaction of the aryl halogeno substitute, and is used or catalyzing the coupling reaction for forming the aryl halogeno substitute having C—N, C—O, C—S and other bonds.

Inhibitors of short-chain dehydrogenase activity for treating fibrosis

A method of treating or preventing a fibrotic disease, disorder or condition includes administering to a subject in need of treatment a 15-PGDH inhibitor.

Heterocyclic carboxylic acid amide ligand and applications thereof in copper catalyzed coupling reaction of aryl halogeno substitute

Provided are a heterocyclic carboxylic acid amide ligand and applications thereof in a copper catalyzed coupling reaction. Specifically, provided are uses of a compound represented by formula (I), definitions of radical groups being described in the specifications. The compound represented by formula (I) can be used as the ligand in the copper catalyzed coupling reaction of the aryl halogeno substitute, and is used or catalyzing the coupling reaction for forming the aryl halogeno substitute having C—N, C—O, C—S and other bonds.

FUNGICIDES n (2 (HALOALCOXI) FENIL) HETEROARIL CARBOXAMIDAS

N-[2-(haIoaIcoxi)feniI]heteroariIcarboxamida de la formula 1 donde n es 0 o 1; Hal es halogeno, X es haloalquilo C2-4, Het es un radical pirazol, tiazol o piridina (a), (b) o (c) donde R1 es alquilo C1-4, o haloalquilo C1-4, R2 es hidrogeno o halogeno, R3 es alquilo C1-4 o haloalquilo C1-4 y R4 es halogeno, alquilo C1-4 o haloalquilo C1-4, excepto por N-[2-(1,1,2,2-tetrafluoroetoxi)fenil]-1,3-dimetilpirazol-4-il-carboxamida, N-[2-(1,1,2,2-tetrafluoroetoxi)fenil]-3-trifluorometil-1- metilpirazol-4-il-carboxamida y N[2-(2,2,2-trifluoroetoxi)fenil]-3-trifluorometil-1- metilpirazol-4-il-carboxamida. Una composicion fungicida que comprende al menos un compuesto 1, el uso del compuesto 1 para preparar una composicion adecuada para controlar hongos daninos, un método para controlar hongos daninos usando el compuesto 1 y además semillas que comprenden al menos un compuesto 1.

Method for producing aminothiazole derivative and production intermediate

Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.

Method of inhibiting tau phosphorylation

A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35 - 40.

composto, composição fungicida, uso de compostos, método para controlar fungos nocivos fitopatogênicos, e, semente

USED COMPOSITES AZA HETEROCÍCLICOS TO TREAT NEUROLOGICAL RIOTS AND LOSS OF HAIR

Method for producing aminothiazole derivative and production intermediate

Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.

Method for producing aminothiazole derivative and production intermediate

AZA-HETEROCYCLIC COMPOUNDS USED TO TREAT NEUROLOGICAL DISORDERS AND HAIR LOSS

The present invention is directed to novel carboxylic acids and isosteres of heterocyclic ring compounds of formula (I) which have multiple heteroatoms within the heterocyclic ring, novel derivatives containing N-linked diketos, sulfonamides, ureas and carbamates attached thereto, their preparation and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, as well as for treating alopecia and promoting hair growth. A, X, Y, Z, D and n are as defined in the application.

AROMATIC HETEROCYCLIC SUBSTITUTED OLEFIN COMPOUND, PREPARATION METHOD FOR SAME, PHARMACEUTICAL COMPOSITION OF SAME, AND APPLICATIONS THEREOF

Provided in the present application are an aromatic heterocyclic substituted olefin compound, a preparation method for same, a pharmaceutical composition of same, and applications thereof. The aromatic heterocyclic substituted olefin compound of the present invention is a novel ALK5 inhibitor and is for use in treating and/or preventing various ALK5-mediated diseases.

Substituted azole derivatives, pharmaceutical composition containing the derivatives, and method for treating parkinson's disease using the same

METHOD FOR PRODUCING AMINOTHIAZOLE DERIVATIVE AND PRODUCTION INTERMEDIATE

Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.

Compostos aza heterocìclicos usados para tratar distúrbios neurológicos e perda de cabelo

Multiple heteroatom containing heterocyclic ring compounds substituted with carboxylic acids and isosteres thereof

The present invention is directed to novel carboxylic acids and isosteres of heterocyclic ring compounds which have multiple heteroatoms within the heterocyclic ring, novel derivatives containing N-linked diketos, sulfonamides, ureas and carbamates attached thereto, their preparation and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, as well as for treating alopecia and promoting hair growth.

METHOD FOR PRODUCING AMINOTHIAZOLE DERIVATIVE AND PRODUCTION INTERMEDIATE

METHOD FOR PRODUCING AMINOTHIAZOLE DERIVATIVE AND PRODUCTION INTERMEDIATE

O-CYCLOPROPYLCYCLOHEXYL-CARBOXANILIDES AND THEIR USE AS FUNGICIDES

The present invention relates to O-CYCLOPROPYLCYCLOHEXYL-CARBOXANILIDES derivatives of formula (I); their process of preparation, their use as fungicide, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. 2. A compound of formula (I) as claimed in claim 1 , wherein{'sup': 1', '2, 'Rand Rare, independently, hydrogen or fluoro;'}{'sup': '3', 'sub': 2-6', '3-8, 'Ris Calkyl, optionally substituted Ccycloalkyl, phenyl, thienyl or furyl;'}A represents one of the radicals A1, A2, A3, A4, A5, A6, A9, A10, A11, A12 or A17;{'sup': '18', 'sub': 1', '2', '1', '2, 'Rrepresents hydrogen, cyano, fluorine, chlorine, bromine, iodine, methyl, ethyl, isopropyl, methoxy, ethoxy, methylthio, ethylthio, cyclopropyl, C-Chaloalkyl C-C-haloalkoxy having in each case 1 to 5 fluorine, chlorine and/or bromine atoms, trifluoromethylthio, difluoromethylthio, aminocarbonyl, aminocarbonylmethyl or aminocarbonylethyl;'}{'sup': '19', 'Rrepresents hydrogen, fluorine, chlorine, bromine, iodine, methyl, ethyl, methoxy, ethoxy, methylthio or ethylthio;'}{'sup': '20', 'sub': 1', '2, 'Rrepresents hydrogen, methyl, ethyl, n-propyl, isopropyl, C-C-haloalkyl having 1 to 5 fluorine, chlorine and/or bromine atoms, hydroxymethyl, hydroxyethyl, cyclopropyl, cyclopentyl, cyclohexyl or phenyl.'}{'sup': 21', '22, 'sub': 1', '2, 'Rand Rindependently of one another represent hydrogen, fluorine, chlorine, bromine, methyl, ethyl or C-C-haloalkyl having 1 to 5 fluorine, chlorine and/or bromine atoms;'}{'sup': '23', 'sub': 1', '2', '1', '2, 'Rrepresents fluorine, chlorine, bromine, cyano, methyl, ethyl, C-C-haloalkyl or C-C-haloalkoxy having in each case 1 to 5 fluorine, chlorine and/or bromine atoms;'}{'sup': 24', '25, 'sub': 1', '2, 'Rand Rindependently of one another represent hydrogen, fluorine, chlorine, bromine, methyl, ethyl or C-C-haloalkyl having 1 to 5 fluorine, chlorine and/or bromine atoms;'}{'sup ...

METHOD OF INHIBITING TAU PHOSPHORYLATION

A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35-40.

INHIBITORS OF SHORT-CHAIN DEHYDROGENASE ACTIVITY FOR TREATING FIBROSIS

A method of treating or preventing a fibrotic disease, disorder or condition includes administering to a subject in need of treatment a 15-PGDH inhibitor. 1: A method of treating or preventing a fibrotic disease , disorder or condition in a subject in need thereof , the method comprising administering to the subject a therapeutically effective amount of a 15-PGDH inhibitor.2: The method of claim 1 , wherein the fibrotic disease claim 1 , disorder or condition is characterized claim 1 , in whole or in part claim 1 , by the excess production of fibrous material claim 1 , including excess production of fibrotic material within the extracellular matrix claim 1 , or the replacement of normal tissue elements by abnormal claim 1 , non-functional claim 1 , and/or excessive accumulation of matrix-associated components.3: The method of claim 1 , wherein the fibrotic disease claim 1 , disorder claim 1 , or condition is selected from the group consisting of systemic sclerosis claim 1 , multifocal fibrosclerosis claim 1 , nephrogenic systemic fibrosis claim 1 , scleroderma claim 1 , sclerodermatous graft-vs-host-disease claim 1 , kidney fibrosis claim 1 , glomerular sclerosis claim 1 , renal tubulointerstitial fibrosis claim 1 , progressive renal disease or diabetic nephropathy claim 1 , cardiac fibrosis claim 1 , pulmonary fibrosis claim 1 , glomerulosclerosis pulmonary fibrosis claim 1 , idiopathic pulmonary fibrosis claim 1 , silicosis claim 1 , asbestosis claim 1 , interstitial lung disease claim 1 , interstitial fibrotic lung disease claim 1 , chemotherapy/radiation induced pulmonary fibrosis claim 1 , oral fibrosis claim 1 , endomyocardial fibrosis claim 1 , deltoid fibrosis claim 1 , pancreatitis claim 1 , inflammatory bowel disease claim 1 , Crohn's disease claim 1 , nodular fascilitis claim 1 , eosinophilic fasciitis claim 1 , general fibrosis syndrome characterized by replacement of normal muscle tissue by fibrous tissue in varying degrees claim 1 , retroperitoneal ...

INHIBITORS OF SHORT-CHAIN DEHYDROGENASE ACTIVITY FOR TREATING FIBROSIS

A method of treating or preventing a fibrotic disease, disorder or condition includes administering to a subject in need of treatment a 15-PGDH inhibitor.

Fungicidal N-[2-(Haloalkoxy)Phenyl]Heteroarylcarboxamides

N-[2-(Haloalkoxy)phenyl]heteroarylcarboxamides of the formula I, where n=0 or 1, Hal=halogen, X=C2-C4-haloalkyl, Het=a pyrazole, thiazole or pyridine radical (a), (b) or (c), where R1=C1-C4-alkyl or C1-C4-haloalkyl, R2=hydrogen or halogen, R3=C1-C4-alkyl or C1-C4-haloalkyl and R5=halogen, C1-C4-alkyl or C1-C4-haloalkyl; except for N-[2-(1,1,2,2-tetrafluoroethoxy)phenyl]-1,3-dimethylpyrazol-4-yl-carboxamide, N-[2-(1,1,2,2-tetrafluoroethoxy)phenyl]-3-trifluoromethyl-1-methylpyrazol-4-yl-carboxamide and N-[2-(2,2,2-trifluorethoxy)phenyl]-3-trifluormethyl-1-methylpyrazol-4-yl-carboxamide. A fungicidal composition comprising at least one compound I, the use of the compounds I for preparing a composition suitable for controlling harmful fungi, a method for controlling harmful fungi using the compounds I and also seed comprising at least one compound I.

Substituted azole derivatives, pharmaceutical composition containing the derivatives, and method for treating Parkinson's disease using the same

Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.

O-CYCLOPROPYLCYCLOHEXYL-CARBOXANILIDES AND THEIR USE AS FUNGICIDES

The present invention relates to O-CYCLOPROPYLCYCLOHEXYL-CARBOXANILIDES derivatives of formula (I); their process of preparation, their use as fungicide, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.

Inhibitors of short-chain dehydrogenase activity for treating fibrosis

Substituted pyrrole derivatives, to pharmaceutical compositions containing these derivatives using the same and method for the treatment of Parkinson's disease

置換されたアゾール誘導体、この誘導体を含む医薬組成物、及びこれを利用したパーキンソン病の治療方法

ORAL GSNOR INHIBITOR AND PHARMACEUTICAL USE THEREOF

Disclosed are a thiazolone derivative of N6022 and a pharmaceutical use thereof. The characteristic structure of the thiazolone derivative of N6022 is: 2. A use of the thiazolone derivative of N6022 of or a pharmaceutically acceptable salt thereof in preparing medicines for improvement and treatment on diseases related to asthma claim 1 , cystic fibrosis claim 1 , diabetic vascular complications claim 1 , aortic aneurysm/dissection. The present invention relates to a thiazolone derivative of an s-nitrosoglutathione reductase (GSNOR) N6022 and a pharmaceutical use thereof, and in particular to a use thereof for preparing medicines for improvement and treatment on diseases related to asthma, cystic fibrosis, diabetic vascular complications and aortic aneurysm/dissection.N6022 is a specific and reversible s-nitrosoglutathione reductase (GSNOR) inhibitor;and studies have shown that N6022 can effectively mitigate asthma and allergic airway inflammation. The phase I and phase II clinical trials of N6022 for treating chronic asthma and cystic fibrosis have finished.Diabetes has become a leading health problem causing morbidity and mortality worldwide. 70% of the deaths of the diabetic patients are attributed to cardiovascular complications; and the diabetic vascular complications, including atherosclerosis, peripheral arterial diseases, retinopathy and nephropathy, are also major factors affect the quality of life. Vascular endothelial cells are located on the inner membrane of the vascular wall and serve as a barrier between blood and tissues. Under various physiological and pathological conditions, the endothelial cells can also play a role as “first response” effector cells for adjusting vascular functions. Diabetes induces endothelial cell dysfunction which is mainly manifested by an increase in vascular endothelial permeability, an impairment of angiogenesis ability. This impairment constitutes a main inducement and a pathophysiological basis of various vascular ...

Oral GSNOR inhibitor and pharmaceutical application thereof

一类口服GSNOR抑制剂及其药物用途，本发明具有良好的口服生物利用度和较长的半衰期。体外实验中，本发明化合物能改善高糖导致的人脐静脉内皮细胞迁移能力和成管能力的降低，以及通透性的增加；本发明化合物能明显促进糖尿病小鼠侧肢缺血后的血管新生和血流恢复，提示本发明化合物能用于治疗糖尿病血管并发症相关疾病。本发明化合物能改善血管紧张素II导致的平滑肌细胞表型转化，本发明化合物能明显改善主动脉瘤/夹层的发生率和死亡率，提示本发明化合物能用于治疗主动脉瘤/夹层相关疾病。本发明化合物能有效抑制GSNOR活性，提示本发明化合物能用于治疗哮喘、囊性纤维病相关疾病。

Substituted oxazole derivatives, pharmaceutical composition containing the derivatives, and method of treating Parkinson's disease using them

Un derivado de azol sustituido representado por la siguiente Fórmula (I) o sales farmacéuticamente aceptables del mismo: **Fórmula** en donde, R se selecciona del grupo que consiste de C7-C15 arilalquilo no sustituido o sustituido por al menos uno seleccionado del grupo que consiste de halógeno, trifluorometilo, trifluoroalcoxi, -NO2, C(>=O)OCH3, C1-C6 alquilo lineal o ramificado, C1-C6 alcoxi, fenilo, feniloxi, benciloxi, -C(>=O)H, -OH y -CH>=N-OH; C4-C15 heteroarilalquilo no sustituido o sustituido por al menos uno seleccionado del grupo que consiste de halógeno, C(>=O)OCH3, C1-C6 alquilo lineal o ramificado, C1-C6 alcoxi, fenilo, feniloxi y benciloxi; C1-C10 alquilo lineal, ramificado o cíclico sustituido por al menos uno seleccionado del grupo que consiste de C1-C3alquiloxi, C1-C3alquiltio, carbamato, (-OC(>=O)NH2), tert-butil- OC(>=O)NH-, -NH3+, -NH2, -OH, -C(>=O)OCH2CH3, NHC(>=O)NH2, trifluorometilsufanilo, trifluorometilo, y -CN, Y se selecciona del grupo que consiste de O y -N-R1; R1 se selecciona del grupo que consiste de H y C1-C3 alquilo lineal o ramificado; R2 se selecciona del grupo que consiste de H y halógeno; A se selecciona del grupo que consiste de O y S; B se selecciona del grupo que consiste de C y N; Z se selecciona del grupo que consiste de imidazol, pirrolidina, y tetrazol sustituido o no sustituido por al menos un sustituyente seleccionado del grupo que consiste de OH, carbamato, C1-C4 alquilo lineal o ramificado, halógeno, - NO2, -NH2,-CF3, -CN y fenilo; -OC(>=O)NR3R4; NR5R6; NHC(>=NH)NH2, y -NHC(>=O)NH2; cada uno de R3 y R4 se selecciona independientemente del grupo que consiste de H; C1-C5 alquilo no sustituido o sustituido por al menos uno seleccionado del grupo que consiste de NH2, y NR7R8; piperidina, piperazina, y diazepam no sustituido o sustituido por C1-C3 alquilo; oR3 y R4 juntos pueden formar piperidina, piperazina, imidazol, pirrolidina, triazol, tetrazol, diazepam o morfolina no sustituido o ...

A method of inhibiting tau phosphorylation

compost, fungicidal composition, compound use, method for controlling phytopathogenic harmful fungi, and seed

Mirabegron cocrystal

The subject of the present invention is the cocrystal form of ( R) -2-(2-aminothiazol-4-yl)-4'- {2-[(2-hydroxy-2-phenyl)ethylamino]ethyl}acetamide (mirabegron) of formula (1) and halide salt of an alkaline earth metal or halide salt of a d-yield metal and its solvates, where the alkaline earth metal is preferably calcium or magnesium and the d-yield metal is preferably zinc. The more specific subject of the present invention is the cocrystal form of mirabegron of formula (2) consisting of 2 molecules of mirabegron, 1 molecule of magnesium-chloride (MgC 2 ) and 2 molecules of water (H 2 O), its preparation method, a pharmaceutical composition comprising the cocrystal of formula (2) and the therapeutical use of the latter pharmaceutical composition.

Aza-heterocyclic compounds used to treat neurological disorders and hair loss and process for their preparation and pharmaceutical compositions containing them

A jelen találmány tárgyát az (I) általános képletű heterociklusosgyűrűs vegyületek olyan új karboxilsav és karboxilsav izosztéravegyületei alkotják, amelyek a heterociklusos gyűrűn belül többheteroatommal rendelkeznek, valamint ezeknek a karboxilsavaknak ésizosztéráknak olyan új származékai, amelyek N-atomon keresztülkapcsolódó diketo, szulfonamid, karbamid és karbamát csoportokattartalmaznak. A találmány tárgyát képezik továbbá az azokfelhasználásával készült gyógyszerkészítmények és azok alkalmazásaneurológiai rendellenességek kezelésére, ideértve a fizikaiidegkárosodásokat és a neurodegeneratív betegségeket, valamint azallopecia (kopaszság) kezelésére és a hajnövekedés elősegítésére. (I)általános képletű vegyületben X, Y és Z jelentése egymástólfüggetlenül a C, O, S vagy N által alkotott csoportból kerülkiválasztásra, azzal a kikötéssel, hogy X, Y és Z közül nem mindegyikjelentése C; n értéke 1-3; A jelentése az L1, L2, L3 és L4 képletűcsoportok közül kerül kiválasztásra, ahol a képletekben szereplő R1 ésE jelentése egymástól függetlenül a hidrogénatom, 1-9 szénatomosegyenes vagy elágazó láncú alkilcsoport, 2-9 szénatomos egyenes vagyelágazó láncú alkenilcsoport, arilcsoport, heteroarilcsoport,karbociklusos csoportok és heterociklusos csoportok által alkototthelyettesítő csoportból kerül kiválasztásra; D jelentése a kémiaikötés, az 1-10 szénatomos egyenes vagy elágazó láncú alkiléncsoport azetiléncsoport (-CH=CH-) és a butiléncsoport közül kerül kiválasztásra;R2 jelentése karboxilsav vagy karboxilsav izoszteracsoport. <> Ó The present invention relates to novel carboxylic and carboxylic acid isosteric compounds of the formula (I) which have several heteroatoms within the heterocyclic ring, and novel derivatives of these carboxylic . The present invention also relates to pharmaceutical compositions for use in their use and to the treatment of neurological disorders, including physical nerve damage and neurodegenerative diseases, as well as the treatment of ...

Method for producing aminothiazole derivative and production intermediate

Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions. ( see formula 1) ( see formula 2) ( see formula 3) ( see formula 4) ( see formula 5) ( see formula 6) ( see formula 7).

Method for producing aminothiazole derivative and production intermediate

2-메톡시기의 선택적 탈메틸화법의 제공. 다음의 반응에 의한 화합물 (7) 의 제법. [화학식 1] [색인어] 탈메틸화, 아미노티아졸 유도체 Providing selective demethylation of 2-methoxy groups. The manufacturing method of compound (7) by following reaction. [Formula 1] [Index] Demethylated, aminothiazole derivatives

Method for producing morphologically homogenous mirabegron and mirabegron monohydrochloride

Inhibitors of short-chain dehydrogenase activity for treating fibrosis

A method of treating or preventing a fibrotic disease, disorder or condition includes administering to a subject in need of treatment a 15-PGDH inhibitor. 1/18 SW033291 Application Increases Survival and Weight Maintenance in IPF Vehicle (x2 daily) + 2mg/kg Bleomycin Intratracheal Instillation 35 day survival 5.0 mpk 291(+) (x2 daily) Fig. 1 A Vehicle vs.1mgkg SWO Weight Change 105 100 95 -.- SWO33291 70- P=0.002 10 20 30 40 Days Post 2mg/kg Bleomyin N= 10 mice/group Fig. 2A B Survival of C57 Mice post 2 mg/kg Beomycin 90 e-SWOV33291 > U Vehidle 70 C60 50 P=0.0617 400 o 1 20 30: 40 Days post Bloe Fig. 2B N= 25 mice/group

Aza heterocyclic compounds used to treat neurological diseases and hair loss

Foreliggende oppfinnelse er rettet mot nye karboksylsyrer og iso- sterer av heterosykliske ringforbind- elser av formel (I) C- som har multiple heteroatomer innen den heterosykliske ring, nye derivater inneholdende N-kjedede diketoer, sul- fonamider, ureaer og karbamater bundet dertil, deres fremstilling og anvendelse for behandling av nevrologiske sykdommer, innbefattende fysikalsk skadde nerver og nevrodegenerative sykdommer, så vel som behandling av alopesi og aktivering av hårvekst. A, X, Y, Z, D og n er som definert i beskrivelsen.

Aromatic heterocyclic substituted olefin compound, preparation method for same, pharmaceutical composition of same, and applications thereof

Provided in the present application are an aromatic heterocyclic substituted olefin compound, a preparation method for same, a pharmaceutical composition of same, and applications thereof. The aromatic heterocyclic substituted olefin compound of the present invention is a novel ALK5 inhibitor and is for use in treating and/or preventing various ALK5-mediated diseases.

Method for producing aminothiazole derivative and production intermediate

Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.

Method for producing aminothiazole derivative and production intermediate

Oral gsnor inhibitors and pharmaceutical use thereof

METHOD FOR PRODUCTION OF AMINOTIABLE PRODUCTION AND INTERMEDIATE PRODUCTION

Παρέχεται μέθοδος για εκλεκτική απομεθυλίωση 2-μεθόξυ ομάδας. Πιο συγκεκριμένα παρέχεται μέθοδος παραγωγής ένωσης που αντιπροσωπεύεται από τύπο (7) παρακάτω μέσω των ακόλουθων αντιδράσεων. A method for the selective demethylation of a 2-methoxy group is provided. In particular, a method of producing a compound represented by formula (7) below is provided by the following reactions.

Substituted azole derivatives, pharmaceutical composition containing the derivatives, and method for treating parkinsons disease using the same

Method for producing aminothiazole derivative and production intermediate

2-메톡시기의 선택적 탈메틸화법의 제공. 다음의 반응에 의한 화합물 (7) 의 제법. [화학식 1] [색인어] 탈메틸화, 아미노티아졸 유도체

METHOD FOR PRODUCING AN AMINOTIAZOL DERIVATIVE AND A PRODUCTION INTERMEDIATE.

Un método de producción de un compuesto representado por la fórmula (7): **Fórmula** (en la que el anillo A representa un anillo benceno o un heterociclo aromático de 6 miembros; R 1 representa un átomo de hidrógeno, un grupo alquilo C1-6, un átomo de halógeno, un grupo nitro, un grupo amino, un grupo mono-alquilamino C1-6, o un grupo di-alquilamino C1-6; y al menos uno de R 2 , R 3 y R 4 representa un grupo metoxi, y el resto de cada uno representa un átomo de hidrógeno, un grupo alquilo C1-6, un átomo de halógeno, un grupo nitro, un grupo amino, un grupo mono-alquilamino C1-6, o un grupo di-alquilamino C1-6), que comprende: hacer reaccionar un compuesto representado por la fórmula (3): (en la que el anillo A y R 1 , R 2 , R 3 y R 4 son los mismos que se han definido anteriormente; y R 5 representa un átomo de hidrógeno o un grupo aceptor de electrones seleccionado entre un átomo de halógeno, un grupo nitro, un grupo trifluorometilo, un grupo triclorometilo, un grupo ciano, un grupo acetilo, un grupo ácido sulfónico y un grupo ácido alquilsulfónico) con un compuesto representado por la fórmula (4): (en la que R 6 representa un grupo alquilo) en calentamiento a 150 ºC o superior o en presencia de un éster del ácido bórico para proporcionar un compuesto representado por la fórmula (5): (en la que el anillo A y R 1 , R 2 , R 3 , R 4 y R 6 son los mismos que se han definido anteriormente); y hacer reaccionar el compuesto resultante con N,N-diisopropiletilendiamina en presencia de tolueno.

Method for producing aminothiazole derivative and production intermediate

本发明提供2－甲氧基的选择性脱甲基化方法。利用下述反应的化合物(7)的制备方法。

Production intermediates of aminothiazole derivatives

Inhibitors of short-chain dehydrogenase activity for treating fibrosis

A method of treating or preventing a fibrotic disease, disorder or condition includes administering to a subject in need of treatment a 15-PGDH inhibitor.

PROCEDURE FOR PREPARING AN AMINOTHIAZLE DERIVATIVE AND INTERMEDIATE PRODUCT

Improved process for the preparation of (1s-(1r*, 2s*, 3r*))-n-(4-(morpholinylsulfonyl)-l-phenylalanyl-3-(2-amino-4-thiazolyl)-n-((1-cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl)-l-alaninamide

본 발명은 아미노 티아졸기의 보호없이 주요 중간체인 3-(2-아미노-4-티아졸릴)-L-알라닌을 목적 화합물로 전환시키는 것을 특징으로하는 개선된 [IS-(1R * ,2S * ,3R * )]-N-(4-모르폴리닐술포닐)-L-페닐알라닐-3-(2-아미노-4-티아졸릴)-N-[(1-시클로헥실메틸)-2,3-디히드로-5-메틸헥실]-L-알라닌아미드의 제조 방법 및 이방법에 사용된 유용한 중간체에 관한 것이다. The present invention provides improved [IS- (1R * , 2S * ,) characterized by converting 3- (2-amino-4-thiazolyl) -L-alanine, a major intermediate, without the protection of amino thiazole groups to the desired compound. 3R * )]-N- (4-morpholinylsulfonyl) -L-phenylalanyl-3- (2-amino-4-thiazolyl) -N-[(1-cyclohexylmethyl) -2,3- It relates to a process for preparing dihydro-5-methylhexyl] -L-alanineamide and useful intermediates used in this process.

Method for producing aminothiazole derivative and production intermediate

A compound represented by formula (3): (wherein ring A represents a benzene ring or a 6-membered aromatic heterocycle; R 1 represents a hydrogen atom, a C 1-6 alkyl group, a halogen atom, a nitro group, an amino group, a mono-C 1-6 alkylamino group, or a di-C 1-6 alkylamino group; at least one of R 2 , R 3 , and R 4 represents a methoxy group, and the rest each represents a hydrogen atom, a C 1-6 alkyl group, a halogen atom, a nitro group, an amino group, a mono-C 1-6 alkylamino group, or a di-C 1-6 alkylamino group; and R 5 represents a hydrogen atom or an electron-withdrawing group selected from a halogen atom, a nitro group, a trifluoromethyl group, a trichloromethyl group, a cyano group, an acetyl group, a sulfonic acid group, and an alkylsulfonic acid group).

Aza-heterocyclic compounds used to treat neurological disorders and hair loss and process for their preparation and pharmaceutical compositions containing them

Process for Preparation of Aminothiazole Derivative and Preparation of Intermediate

Resorcinols, methods for their manufacture, and uses thereof

本發明係關於一群作為醫藥學上活性化合物之間苯二酚衍生物及其製備方法。間苯二酚衍生物已用於治療各種疾病及病症。儘管此類治療有前景，但在此項技術中仍需要更有效的治療且此已藉助於本發明之間苯二酚衍生物實現。

Method of inhibiting tau phosphorylation

A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35-40.

레조르시놀, 이의 제조 방법, 및 이의 용도

본 발명은 약학적으로 활성인 화합물로서의 레조르시놀 유도체 군 및 이의 제조 방법에 관한 것이다. 레조르시놀 유도체는 다양한 질병 및 장애를 치료하는 데 사용되어 왔다. 이러한 치료법은 유망하지만, 보다 효과적인 치료법에 대한 당업계의 요구가 남아 있고, 이는 본 발명의 레조르시놀 유도체에 의해 가능하였다.

Orale gsnor-hæmmere og farmaceutisk anvendelse heraf

Oral gsnor inhibitors and pharmaceutical use thereof

Rescorcinols, methods for their manufacture, and uses thereof

The present invention relates to a group of resorcinol derivatives as a pharmaceutically active compounds and methods of preparation thereof. Resorcinol derivatives have been used to treat various diseases and disorders. While such treatments hold promise, there remains a need in the art for more effective treatments and this has been brought about by way of the resorcinol derivative of the invention.

τリン酸化を阻害する方法

Verfahren zur herstellung eines aminothiazolderivats und zwischenprodukt

レゾルシノール類、それら製造のための方法、及びその使用

本発明は、薬学的に活性な化合物としてのレゾルシノール誘導体の群及びその調製の方法に関する。レゾルシノール誘導体は、様々な病気及び障害を処置するために使用されている。そのような処置は有望であるが、より効果的な処置が当技術分野ではなおも必要とされており、これは、本発明のレゾルシノール誘導体によってもたらされた。

间苯二酚、其制造方法及其用途

本发明涉及一组作为药物活性化合物的间苯二酚衍生物及其制备方法。间苯二酚衍生物已经被用于治疗多种疾病和紊乱。虽然这样的治疗保持前景，但在本领域中仍存在对更有效的治疗的需求，并且这已经通过本发明的间苯二酚衍生物实现。

Rescorcinols, methods for their manufacture, and uses thereof

The present invention relates to a group of resorcinol derivatives as a pharmaceutically active compounds and methods of preparation thereof. Resorcinol derivatives have been used to treat various diseases and disorders. While such treatments hold promise, there remains a need in the art for more effective treatments and this has been brought about by way of the resorcinol derivative of the invention.

Rescorcinols, methods for their manufacture, and uses thereof

The present invention relates to a group of resorcinol derivatives as a pharmaceutically active compounds and methods of preparation thereof. Resorcinol derivatives have been used to treat various diseases and disorders. While such treatments hold promise, there remains a need in the art for more effective treatments and this has been brought about by way of the resorcinol derivative of the invention.

다당류, 안정제 및 삼요오드화물을 포함하는 항미생물성 조성물 및 이의 제조 방법과 그 용도

본 발명은 다당류 및 삼요오드화물을 포함하며, 삼요오드화물이 요오드로 분해되고 휘발성 요오드가 안정제의 존재에 의해 현저하게 억제되는, 항미생물 활성을 가진 고체 형태에 관한 것이며, 또한 본 발명은 이의 제조 및 용도에 관한 것이다. 삼요오드화물을 포함하는 액체 형태와 비교해, 안정화된 고체 형태는 이의 형태 안정성과 전체 물질의 현저하게 작은 부피 (중량)으로 인해 훨씬 광범위한 용도로 사용될 수 있다. 식에서, 다당류는 히알루론산 또는 이의 화학적으로 변형된 유도체, 알긴산나트륨, 옥시셀룰로스, 카르복시메틸 셀룰로스 또는 하이드록시에틸 셀룰로스를 포함하며, R 은 선택적으로 N 또는 O 원자를 함유한, C 1 - C 30 의 알킬, 방향족, 헤테로방향족, 직쇄 또는 분지쇄이고, R 1 은 선택적으로 N 또는 O 원자를 함유한, C 1 - C 30 의 알킬, 방향족, 헤테로방향족, 직쇄 또는 분지쇄이거나, 또는 -H이며, 안정제에서 R 1 은 독립적으로 동일하거나 또는 상이하다.

杂环羧酸酰胺配体及其在铜催化芳基卤代物偶联反应中的用途

本发明提供了杂环羧酸酰胺配体及其在铜催化的偶联反应中的应用，具体地，本发明提供了一种如下式I所示的化合物的用途；其中，各基团的定义如说明书中所述。所述的式I化合物可以用作为铜催化芳基卤代物偶联反应中的配体，用于催化形成C‑N、C‑O、C‑S键等芳基卤代物的偶联反应。

Antimicrobial composition comprising a polysaccharide, a stabilizing agent and triiodide, method of preparation thereof and use thereof

The present invention relates to solid forms with an antimicrobial activity comprising a polysaccharide and triiodide, where the triiodide decomposition to iodide and volatile iodine is significantly suppressed by the presence of a stabilizer, further it relates to the preparation and use thereof. Compared to the liquid forms comprising triiodide, the stabilized solid forms can be used for a much wider range of applications due to their shape stability and a significantly smaller volume (weight) of total material. Formula for abstract polysaccharide wherein the polysaccharide comprises hyaluronic acid or a chemically modified derivative thereof, sodium alginate, oxycellulose, carboxymethyl cellulose or hydroxyethyl cellulose, R is an alkyl, aromatic, heteroaromatic, linear or branched chain C1 - C30, optionally containing N or O atoms, R1 is an alkyl, aromatic, heteroaromatic, linear or branched chain C1 - C30, optionally containing N or O atoms, or -H, where R1 in the stabilizer are independently the same or different.

Novos derivados de isobutiramida, preparações cosméticas e/ou dermatológicas contendo tais compostos, assim como seu uso para a profilaxia contra e tratamento de pele sensível, em particular, inflamada ou de condições in-flamatórios da pele

NOVOS DERIVADOS DE ISOBUTIRAMIDA, PREPARAÇÕES COSMÉTICAS E/OU DERMATOLÓGICAS CONTENDO TAIS COMPOSTOS, ASSIM COMO SEU USO PARA A PROFILAXIA CONTRA E TRATAMENTO DE PELE SENSÍVEL, EM PARTICULAR, INFLAMADA OU DE CONDIÇÕES INFLAMATÓRIOS DA PELE. A presente invenção refere-se a novas isobutiramidas.

用于治疗纤维症的短链脱氢酶活性的抑制剂

本发明提供了一种用于治疗或预防纤维化疾病、紊乱或状况的方法，其包括向有需要治疗的受试对象给予15‑PGDH抑制剂。

Rescorcinoles, metodos para su fabricacion, y usos de los mismos.

La presente invención se refiere a un grupo de derivados de resorcinol como compuestos farmacéuticamente activos y a métodos de preparación de los mismos. Los derivados de resorcinol se han utilizado para tratar diversas enfermedades y trastornos. Si bien dichos tratamientos son prometedores, sigue existiendo una necesidad en la técnica de tratamientos más eficaces y esto se ha logrado mediante el derivado de resorcinol de la invención.

Antimicrobial composition comprising a polysaccharide, a stabilizing agent and triiodide, method of preparation thereof and use thereof

The present invention relates to solid forms with an antimicrobial activity comprising a polysaccharide and triiodide, where the triiodide decomposition to iodide and volatile iodine is significantly suppressed by the presence of a stabilizer, further it relates to the preparation and use thereof. Compared to the liquid forms comprising triiodide, the stabilized solid forms can be used for a much wider range of applications due to their shape stability and a significantly smaller volume (weight) of total material. Formula for abstract polysaccharide wherein the polysaccharide comprises hyaluronic acid or a chemically modified derivative thereof, sodium alginate, oxycellulose, carboxymethyl cellulose or hydroxyethyl cellulose, R is an alkyl, aromatic, heteroaromatic, linear or branched chain C 1 - C 30 , optionally containing N or O atoms, R 1 is an alkyl, aromatic, heteroaromatic, linear or branched chain C 1 - C 30 , optionally containing N or O atoms, or -H, where R 1 in the stabilizer are independently the same or different.

Mirabegron cocrystals

Heterocyclic carboxylic acid amide ligand and applications thereof in copper catalyzed coupling reaction of aryl halogeno substitute

New isobutyramide derivatives, cosmetic and/or dermatological preparations containing said compounds, and their use for the prophylaxis and treatment of sensitive, in particular inflamed skin or inflammatory skin conditions

New isobutyramides.

酰胺衍生物及其应用

一种酰胺衍生物及其在医药上的应用，具体而言涉及式(I)的酰胺衍生物或者其药学上可接受的盐或其所有的立体异构体、互变异构体及其氘代物，以及包含上述化合物的药物组合物，上述化合物或组合物可作为NLRP3抑制剂，式(I)中各取代基的定义与说明书的定义相同，

新的异丁酰胺衍生物，含有此类化合物的化妆品和/或皮肤病学制剂，及其用于预防和处理敏感的、特别是发炎的皮肤或炎症性皮肤状况的用途

本发明涉及一种新的异丁酰胺。

Rescorcinols, methods for their manufacture, and uses thereof

The present invention relates to a group of resorcinol derivatives as a pharmaceutically active compounds and methods of preparation thereof. Resorcinol derivatives have been used to treat various diseases and disorders. While such treatments hold promise, there remains a need in the art for more effective treatments and this has been brought about by way of the resorcinol derivative of the invention.

用于治疗纤维症的短链脱氢酶活性的抑制剂

本发明提供了一种用于治疗或预防纤维化疾病、紊乱或状况的方法，其包括向有需要治疗的受试对象给予15‑PGDH抑制剂。

Method for producing morphologically pure mirabegron and mirabegron monohydrochloride

间苯二酚、其制造方法及其用途

本发明涉及一组作为药物活性化合物的间苯二酚衍生物及其制备方法。间苯二酚衍生物已经被用于治疗多种疾病和紊乱。虽然这样的治疗保持前景，但在本领域中仍存在对更有效的治疗的需求，并且这已经通过本发明的间苯二酚衍生物实现。

酰胺衍生物及其应用

一种酰胺衍生物及其在医药上的应用，具体而言涉及式(I)的酰胺衍生物或者其药学上可接受的盐或其所有的立体异构体、互变异构体及其氘代物，以及包含上述化合物的药物组合物，上述化合物或组合物可作为NLRP3抑制剂，式(I)中各取代基的定义与说明书的定义相同，

噻唑类化合物在制备治疗和预防癌症药物中的用途

通式(I)的噻唑类化合物，或其药学上可接受的盐、水合物或溶剂合物，及其作为STAT3通路抑制剂的用途。所述化合物对肿瘤细胞的增殖具有强抑制活性，可用于治疗癌症。

新的异丁酰胺衍生物，含有此类化合物的化妆品和/或皮肤病学制剂，及其用于预防和处理敏感的、特别是发炎的皮肤或炎症性皮肤状况的用途

本发明涉及一种新的异丁酰胺。

一种尿酸促排剂及其合成方法和其在医药上的应用

一类作为尿酸盐转运体(URAT1)抑制剂的尿酸促泄剂的化合物，及其在制备治疗尿酸水平异常病症药物中的应用。具体涉及式(I)所示化合物及其药学上可接受的盐。

N6022的噻唑酮衍生物及其药物用途

N6022的噻唑酮衍生物及其药物用途，本发明具有良好的口服生物利用度和较长的半衰期。体外实验中，本发明化合物能改善高糖导致的人脐静脉内皮细胞迁移能力和成管能力的降低，以及通透性的增加；本发明化合物能明显促进糖尿病小鼠侧肢缺血后的血管新生和血流恢复，提示本发明化合物能用于治疗糖尿病血管并发症相关疾病。本发明化合物能改善血管紧张素II导致的平滑肌细胞表型转化，本发明化合物能明显改善主动脉瘤/夹层的发生率和死亡率，提示本发明化合物能用于治疗主动脉瘤/夹层相关疾病。本发明化合物能有效抑制GSNOR活性，提示本发明化合物能用于治疗哮喘、囊性纤维病相关疾病。

芳香杂环取代烯烃化合物、其制备方法、药物组合物和应用

本发明提供一种芳香杂环取代烯烃化合物、其制备方法、药物组合物和应用。本发明的芳香杂环取代烯烃化合物是一种新型ALK5抑制剂，用于治疗和/或预防各种ALK5介导的疾病。