AR041276A1 - Compuestos de triazol como inhibidores del factor crecimiento transformador (tgf) - Google Patents

Compuestos de triazol como inhibidores del factor crecimiento transformador (tgf)

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Publication number
AR041276A1
AR041276A1 ARP030103360A ARP030103360A AR041276A1 AR 041276 A1 AR041276 A1 AR 041276A1 AR P030103360 A ARP030103360 A AR P030103360A AR P030103360 A ARP030103360 A AR P030103360A AR 041276 A1 AR041276 A1 AR 041276A1
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Argentina
Prior art keywords
alkyl
phenyl
heteroaryl
heterocycle
cycloalkyl
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ARP030103360A
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English (en)
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Pfizer Prod Inc
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Publication of AR041276A1 publication Critical patent/AR041276A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se describen compuestos de triazol, incluyendo sus derivados, intermedios para su preparación, composiciones farmacéuticas que los contienen y su uso medicinal. Los compuestos son inhibidores potentes de la ruta de senalización del factor delcrecimiento transformador ("TGF")-beta. Son de utilidad en el tratamiento de diversos estados de enfermedad relacionados con TGF incluyendo, por ejemplo cáncer y enfermedades fibróticas. Reivindicación 1: Un compuesto de fórmula (1), (2) o (3) ouna sal, profármaco, tautómero, hidrato y solvato farmacéuticamente aceptable, caracterizado porque R1 es un anillo saturado, insaturado o aromático mono-, bi-, o policíclico C3-20 que contiene opcionalmente al menos un heteroátomo seleccionado delgrupo constituido por N, O, y S, en el que R1 además puede estar opcionalmente sustituido independientemente al menos con un resto seleccionado independientemente del grupo constituido por: carbonilo, halo, haloalquilo C1-6, perhaloalquilo C1-6,perhaloalcoxi C1-6, alquilo C1-6, alquenilo C2-6. alquinilo C2-6, hidroxi, oxo, mercapto, alquiltio C1-6, alcoxi C1-6, arilo C5-10, o heteroarilo C5-10, ariloxi C5-10, o heteroariloxi C5-10, (aril C5-10)alquilo C1-6 o (heteroaril C5-10)alquilo C1-6,(aril C5-10)alcoxi C1-6 o (heteroaril C5-10)alcoxi C1-6, HO-(C=O)-, éster, amido, éter, amino, aminoalquilo C1-6, (alquil C1-6)aminoalquilo C1-6, di(alquil C1-6)aminoalquilo C1-6, (heterociclil C5-10) alquilo C1-6, (alquil C1-6) y di(alquilC1-6)amino, ciano, nitro, carbamoilo, (alquil C1-6) carbonilo, (alcoxi C1-6)carbonilo, (alquil C1-6)aminocarbonilo, di(alquil C1-6)aminocorbonilo, (aril C5-10)carbonilo, (aril C5-10)oxicarbonilo, alquil( C1-6)sulfonilo, y (aril C5-10)sulfonilo; cadaR3 se selecciona independientemente del grupo constituido por H, halo, haloalquilo C1-6, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, perhaloalquilo C1-6, fenilo, heteroarilo C5-10, heterociclo C5-10, cicloalquilo C3-10, hidroxi, alcoxi C1-6,perhaloalcoxi C1-6, fenoxi, (heteroaril C5-10)-O-, (heterociclo C5-10)-O-, (cicloalquil C3-10)-O-, (alquil C1-6)-S-, (alquil C1-6)-SO2-, (alquil C1-6)-NH-SO2-,-O2N, -NC, amino, -Ph(CH2)1-6HN, -(alquil C1-6)-HN, (alquil C1-6)amino, [(alquilC1-6)]2-amino, (alquil C1-6)-SO2-NH-, amino-(C=O), -amino-O2S-, (alquil C1-6)-(C=O)-NH-, (alquil C1-6)-(C=O)-[(alquil C1-6)-N]-, fenil-(C=O)-NH, fenil-(C=O)-[(alquil C1-6)-N]-, (alquil C1-6)-(C=O)-, fenil-(C=O)-, (heteroaril C5-10)-(C=O)-,(heterociclo C5-10)-(C=O)-, (cicloalquil C3-10)-(C=O)-, HO-(C=O)-, (alquil C1-6)-O-(C=O)-, H2N-(C=O)-, (alquil C1-6)-NH-(C=O)-, [(alquil C1-6)]2-N-(C=O)-, fenil-NH-(C=O)-, fenil-[(alquil C1-6)-N]-(C=O)-, (heteroaril C5-10)-NH-(C=O)-, (heterocicloC5-10)-NH-(C=O)-, (cicloalquil C3-10)-NH-(C=O)- y (alquil C1-6)-(C=O)-O-; donde alquilo, alquenilo, alquinilo, fenilo, heteroarilo, heterociclo, cicloalquilo, alcoxi, fenoxi, amino de R3 está opcionalmente sustituido al menos con un sustituyenteseleccionado independientemente de alquilo C1-6, alcoxi C1-6, haloalquilo C1-6, halo, H2N-, Ph(CH2)1-6-HN, y (alquil C1-6)-HN; s es un número entero de 1 a 5; y R6 se selecciona del grupo constituido por H, alquilo C1-6, alquenilo C2-6, alquiniloC2-6, fenilo heteroarilo C5-10, heterociclo C5-10, cicloalquilo C3-10, (alquil C1-6)-(SO2)-, fenil-(SO2)-, H2N(SO2)-, (alquil C1-6)-NH-(SO2)-,(alquil C1-6)2N-(SO2), fenil-NH-(SO2)-, (fenil)2N-(SO2)-, (alquil C1-6)-(C=O)-, fenil-(C=O)-,(heteroarilC5-10)-(C=O)-, (heterociclo C5-10)-(C=O)-, (cicloalquil C3-10-(C=O)-, (alquil C1-6)-O-(C=O)-, (heterociclo C5-10)-O-(C=O)-, (cicloalquil C3-10)-O-(C=O)-,H2N-(C=O)-, (alquil C1-6)-NH-(C=O)-,fenil-NH-(C=O)-, (heteroaril C5-10)-NH-(C=O)-, (heterocicloC5-10)-NH-(C=O)-, (cicloalquil C3-10)-NH-(C=O)-, (alquil C1-6)2N-(C=O)-, (fenil)2N-(C=O)-, fenil-[(alquil C1-6)-N]-(C=O)-, (heteroaril C5-10)-[(alquil C1-6)-N]-(C=O)-, (heterociclo C5-10)-[(alquil C1-6)-N]-(C=O)-, y (cicloalquil C3-10)-[(alquilC1-6)-N]-(C=O); donde alquilo, alquenilo, alquinilo, fenilo, bencilo, heteroarilo, heterociclo, cicloalquilo, alcoxi, fenoxi, amino de R6 está opcionalmente sustituido al menos con un resto seleccionado independientemente del grupo constituido porhalo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, perhaloalquilo C1-6, cicloalquilo C3-10, fenilo, bencilo, heterociclo C5-10, heteroarilo C5-10, (alquil C1-6)-SO2-, formilo, NC-, (alquil C1-6)-(C=O)-, (cicloalquil C3-10)-(C=O)-,fenil-(C=O)-,(heterociclo C5-10)-(C=O)-, (heteroaril C5-10)-(C=O)-, HO-(C=O), (alquil C1-6)-O-(C=O)-, (cicloalquil C3-10)-O-(C=O)-, (heterociclo C5-10)-O-(C=O)-, (alquil C1-6)-NH-(C=O)-, (cicloalquil C3-10)-NH-(C=O)-, fenil-NH-(C=O)-, (heterocicloC5-10)-NH-(C=O)-, (heteroaril C5-10)-NH-(C=O)-, (alquil C1-6)2-N-(C=O)-, fenil-[(alquil C1-6)-N]-(C=O)-, hidroxi, alcoxi C1-6, perhaloalcoxi C1-6, (cicloalquil C3-10)-O-, fenoxi, (heterociclo C5-10)-O-, (heteroaril (C5-10)-O-, (alquilC1-6)-(C=O)-O-, (cicloalquil C3-10)-(C=O)-O-, fenil-(C=O)-O-, (heterociclo C5-10)-(C=O)-O-, (heteroaril C5-10)-(C=O)-O-, O2N-, amino, (alquil C1-6)amino, (alquil C1-6)2-amino, formamidilo, (alquil C1-6)-(C=O)-NH-, (cicloalquil C3-10)-(C=O)-NH,fenil-(C=O)-NH-, (heterociclo C5-10)-(C=O)-NH-, (heteroaril C5-10-(C=O)-NH-, (alquil C1-6)-(C=O)-[(alquil C1-6)-N]-, fenil-(C=O)-[(alquil C1-6)-N]-, (alquil C1-6)-SO2NH-, (cicloalquil C3-10)-SO2NH-,fenil-SO2NH-, (heterociclo C5-10)-SO2NH-, y(heteroaril C5-10)-SO2NH-; en el que el resto fenilo o heteroarilo de un sustituyente R6 está opcionalmente sustituido además al menos con un radical seleccionado independientemente del grupo constituido por halo, alquilo C1-6, alcoxi C1-6,perfluoralquilo C1-6 y perfluoralcoxi C1-6, con la condición de que R1 no es un naftilo o fenilo; y con la condición de que cuando R1 es un fenilo condensado con un anillo cíclico aromático o no aromático de 5-7 miembros que contiene hasta tresátomos de N, dicho N es distinto de -NH o -N(alquilo C1-6) o si dicho N es -NH o -N(alquilo C1-6), entonces R1 debe estar sustituido adicionalmente; y con la condición de que cuando R1 es un fenilo condensado con un anillo cíclico aromático o noaromático de 5-7 miembros que contiene 1-3 heteroátomos seleccionados independientemente de O y S, entonces R1 debe estar sustituido adicionalmente.
ARP030103360A 2002-09-18 2003-09-16 Compuestos de triazol como inhibidores del factor crecimiento transformador (tgf) AR041276A1 (es)

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US48453503P 2003-07-02 2003-07-02

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EP (1) EP1542685A1 (es)
JP (1) JP2006502236A (es)
KR (1) KR20050057393A (es)
CN (1) CN1681502A (es)
AP (1) AP2005003260A0 (es)
AR (1) AR041276A1 (es)
AU (1) AU2003260810A1 (es)
BR (1) BR0314577A (es)
CA (1) CA2497971A1 (es)
CO (1) CO5540390A2 (es)
EA (1) EA200500376A1 (es)
EC (1) ECSP055681A (es)
HR (1) HRP20050251A2 (es)
IS (1) IS7713A (es)
MA (1) MA27442A1 (es)
MX (1) MXPA05002982A (es)
NO (1) NO20051010L (es)
OA (1) OA12927A (es)
PA (1) PA8583401A1 (es)
PE (1) PE20050074A1 (es)
PL (1) PL375974A1 (es)
TW (1) TW200412346A (es)
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WO (1) WO2004026307A1 (es)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY27304A1 (es) 2001-05-24 2002-12-31 Avanir Pharmaceuticals Inhibidores del factor inhibidor de la migración de los macrófagos y métodos para su identificación
CA2499429C (en) 2002-09-18 2010-09-21 Pfizer Products Inc. Novel oxazole and thiazole compounds as transforming growth factor (tgf) inhibitors
CA2498047C (en) * 2002-09-18 2009-05-19 Pfizer Products Inc. Novel imidazole compounds as transforming growth factor (tgf) inhibitors
CA2496295C (en) 2002-09-18 2010-11-23 Michael John Munchhof Novels pyrazole compounds as transforming growth factor (tgf) inhibitors
PA8595001A1 (es) 2003-03-04 2004-09-28 Pfizer Prod Inc Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf)
ES2431843T3 (es) 2005-02-23 2013-11-28 Shionogi & Co., Ltd. Derivado de quinazolina que tiene actividad inhibidora de tirosina quinasa
US7781462B2 (en) 2005-07-25 2010-08-24 Synta Pharmaceuticals Corp. Compounds for the treatment of proliferative disorders
JP2009519977A (ja) * 2005-12-16 2009-05-21 アルコン，インコーポレイテッド Ａｌｋ５調整剤を用いた眼内圧のコントロール
DE102005061840A1 (de) 2005-12-23 2007-06-28 Merck Patent Gmbh Triazolderivate
US8673929B2 (en) 2006-07-20 2014-03-18 Gilead Sciences, Inc. 4,6-di- and 2,4,6-trisubstituted quinazoline derivatives and pharmaceutical compositions useful for treating viral infections
WO2008009078A2 (en) 2006-07-20 2008-01-24 Gilead Sciences, Inc. 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
US8871744B2 (en) 2010-07-21 2014-10-28 B & G Partyers, LLC Compounds and methods for selectively targeting tumor-associated mucins
US9782452B2 (en) 2011-11-22 2017-10-10 Cornell University Methods for stimulating hematopoietic recovery by inhibiting TGFβ signaling
US10023640B2 (en) 2012-10-05 2018-07-17 Kadmon Corporation, Llc Human anti-VEGFR-2/KDR antibodies
HUE049377T2 (hu) 2013-03-14 2020-09-28 Brigham & Womens Hospital Inc Készítmények és eljárások epiteliális õssejtek expanziójára és tenyésztésére
CA2935392C (en) 2014-01-01 2022-07-26 Medivation Technologies, Inc. Amino pyridine derivatives for the treatment of conditions associated with excessive tgf.beta activity
IL299964A (en) 2014-09-03 2023-03-01 Massachusetts Inst Technology Preparations, systems and methods for producing hair cells in the inner ear to treat hearing loss
EA035093B1 (ru) 2015-03-04 2020-04-27 Джилид Сайэнс, Инк. 4,6-диаминопиридо[3,2-d]пиримидиновые соединения, модулирующие toll-подобные рецепторы
JP2019506153A (ja) 2016-01-08 2019-03-07 マサチューセッツ インスティテュート オブ テクノロジー 分化した腸内分泌細胞およびインスリン産生細胞の作製
US11260130B2 (en) 2016-03-02 2022-03-01 Frequency Therapeutics, Inc. Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using a GSK3 inhibitor: IV
US10213511B2 (en) 2016-03-02 2019-02-26 Frequency Therapeutics, Inc. Thermoreversible compositions for administration of therapeutic agents
US10201540B2 (en) 2016-03-02 2019-02-12 Frequency Therapeutics, Inc. Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using GSK3 inhibitors: I
ES2826748T3 (es) 2016-09-02 2021-05-19 Gilead Sciences Inc Derivados de 4,6-diamino-pirido[3,2-d]pirimidina como moduladores de receptores de tipo Toll
ES2906581T3 (es) 2016-09-02 2022-04-19 Gilead Sciences Inc Compuestos moduladores de los receptores tipo Toll
EP3562827A1 (en) 2016-12-30 2019-11-06 Frequency Therapeutics, Inc. 1h-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells
CA3093340A1 (en) 2018-03-20 2019-09-26 Icahn School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
EP3827010A4 (en) 2018-07-23 2022-03-16 Brise Pharmaceuticals Co., Ltd. BISPHOSPHONATE-DRUG CONJUGATES
EP3837351A1 (en) 2018-08-17 2021-06-23 Frequency Therapeutics, Inc. Compositions and methods for generating hair cells by downregulating foxo
CN113195707A (zh) 2018-08-17 2021-07-30 频率治疗公司 用于通过上调jag-1来生成毛细胞的组合物和方法
CA3124700A1 (en) 2018-12-31 2020-07-09 Icahn School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
TW202210480A (zh) 2019-04-17 2022-03-16 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TWI751517B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TW202115056A (zh) 2019-06-28 2021-04-16 美商基利科學股份有限公司 類鐸受體調節劑化合物的製備方法
CN112694477B (zh) * 2019-10-22 2024-02-06 四川科伦博泰生物医药股份有限公司 吡唑并环类化合物，包含其的药物组合物，其制备方法及其用途

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6058981A (ja) * 1983-09-09 1985-04-05 Takeda Chem Ind Ltd ５−ピリジル−１，３−チアゾ−ル誘導体，その製造法およびそれを含んでなる医薬組成物
JPS6025142A (ja) 1983-07-21 1985-02-07 Matsushita Electric Ind Co Ltd 表示装置の電極製造方法
EP0149884B1 (en) * 1983-09-09 1992-12-16 Takeda Chemical Industries, Ltd. 5-pyridyl-1,3-thiazole derivatives, their production and use
GB9201692D0 (en) * 1992-01-27 1992-03-11 Smithkline Beecham Intercredit Compounds
BR9809451A (pt) 1997-05-22 2000-06-20 Searle & Co Pirazóis substituìdos com 3(5)-heteroarila como inibidores de quinase p38.
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
AU7726898A (en) 1997-05-22 1998-12-11 G.D. Searle & Co. Pyrazole derivatives as p38 kinase inhibitors
JPH11193281A (ja) * 1997-10-27 1999-07-21 Takeda Chem Ind Ltd アデノシンａ３受容体拮抗剤およびチアゾール化合物
DE60001229T2 (de) 1999-04-09 2003-10-30 Smithkline Beecham Corp., Philadelphia Triarylimidazole
JP2000302680A (ja) * 1999-04-23 2000-10-31 Takeda Chem Ind Ltd 脳保護剤
CA2381215A1 (en) * 1999-08-06 2001-02-15 Takeda Chemical Industries, Ltd. P38map kinase inhibitors
CO5271680A1 (es) 2000-02-21 2003-04-30 Smithkline Beecham Corp Compuestos
GB0007405D0 (en) 2000-03-27 2000-05-17 Smithkline Beecham Corp Compounds
PE20020506A1 (es) 2000-08-22 2002-07-09 Glaxo Group Ltd Derivados de pirazol fusionados como inhibidores de la proteina cinasa
WO2002040468A1 (en) 2000-11-16 2002-05-23 Smithkline Beecham Corporation Compounds
GB0027987D0 (en) 2000-11-16 2001-01-03 Smithkline Beecham Plc Compounds
EP1354603A1 (en) * 2000-12-26 2003-10-22 Takeda Chemical Industries, Ltd. Concomitant drugs
GB0100762D0 (en) 2001-01-11 2001-02-21 Smithkline Beecham Plc Novel use
GB0102673D0 (en) * 2001-02-02 2001-03-21 Glaxo Group Ltd Compounds
GB0102665D0 (en) * 2001-02-02 2001-03-21 Glaxo Group Ltd Compounds
GB0102668D0 (en) * 2001-02-02 2001-03-21 Glaxo Group Ltd Compounds
US20040087623A1 (en) 2001-02-02 2004-05-06 Gellibert Francoise Jeanne Pyrazole derivatives against tgf overexpression
JPWO2002062775A1 (ja) * 2001-02-02 2004-06-10 山之内製薬株式会社 ２−アシルアミノチアゾール誘導体又はその塩
EP1363904A1 (en) 2001-02-02 2003-11-26 Glaxo Group Limited Pyrazoles as tgf inhibitors
GB0102672D0 (en) 2001-02-02 2001-03-21 Glaxo Group Ltd Compounds
US20050080113A1 (en) * 2001-06-11 2005-04-14 Shigenori Ohkawa Medicinal compositions
AR039241A1 (es) 2002-04-04 2005-02-16 Biogen Inc Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos
GB0217780D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Compounds
TW200417547A (en) 2002-07-31 2004-09-16 Smithkline Beecham Corp Compounds

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EA200500376A1 (ru) 2005-08-25
BR0314577A (pt) 2005-08-09
IS7713A (is) 2005-02-24
WO2004026307A1 (en) 2004-04-01
NO20051010L (no) 2005-05-31
CN1681502A (zh) 2005-10-12
US20060128761A1 (en) 2006-06-15
MXPA05002982A (es) 2005-06-22
UY27981A1 (es) 2004-04-30
TW200412346A (en) 2004-07-16
PL375974A1 (en) 2005-12-12
US20040110798A1 (en) 2004-06-10
ECSP055681A (es) 2005-05-30
CA2497971A1 (en) 2004-04-01
MA27442A1 (fr) 2005-07-01
KR20050057393A (ko) 2005-06-16
US7053095B2 (en) 2006-05-30
PE20050074A1 (es) 2005-03-21
OA12927A (en) 2006-10-13
AP2005003260A0 (en) 2005-03-31
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PA8583401A1 (es) 2004-04-23
HRP20050251A2 (en) 2005-10-31

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