EA200500376A1 - Триазольные производные в качестве ингибиторов трансформирующего фактора роста (tgf) - Google Patents

Триазольные производные в качестве ингибиторов трансформирующего фактора роста (tgf)

Info

Publication number
EA200500376A1
EA200500376A1 EA200500376A EA200500376A EA200500376A1 EA 200500376 A1 EA200500376 A1 EA 200500376A1 EA 200500376 A EA200500376 A EA 200500376A EA 200500376 A EA200500376 A EA 200500376A EA 200500376 A1 EA200500376 A1 EA 200500376A1
Authority
EA
Eurasian Patent Office
Prior art keywords
tgf
growth factor
transforming growth
triazole derivatives
inhibitors
Prior art date
Application number
EA200500376A
Other languages
English (en)
Inventor
Лаура Кук Блюмберг
Майкл Джон Манчхоф
Original Assignee
Пфайзер Продактс Инк.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Пфайзер Продактс Инк. filed Critical Пфайзер Продактс Инк.
Publication of EA200500376A1 publication Critical patent/EA200500376A1/ru

Links

Classifications

    • 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

Landscapes

  • 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)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Описаны новые триазольные производные формулы (Ia-c), промежуточные соединения для их получения, содержащие их фармацевтические композиции и их медицинское применение. Соединения настоящего изобретения являются сильными ингибиторами пути проведения сигнала трансформирующего фактора роста β (TGF). Они пригодны для лечения различных заболеваний, связанных с TGF, включая, например, рак и фиброзы.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200500376A 2002-09-18 2003-09-08 Триазольные производные в качестве ингибиторов трансформирующего фактора роста (tgf) EA200500376A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41207902P 2002-09-18 2002-09-18
US48453503P 2003-07-02 2003-07-02
PCT/IB2003/003825 WO2004026307A1 (en) 2002-09-18 2003-09-08 Triazole derivatives as transforming growth factor (tgf) inhibitors

Publications (1)

Publication Number Publication Date
EA200500376A1 true EA200500376A1 (ru) 2005-08-25

Family

ID=32033582

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200500376A EA200500376A1 (ru) 2002-09-18 2003-09-08 Триазольные производные в качестве ингибиторов трансформирующего фактора роста (tgf)

Country Status (25)

Country Link
US (2) US7053095B2 (ru)
EP (1) EP1542685A1 (ru)
JP (1) JP2006502236A (ru)
KR (1) KR20050057393A (ru)
CN (1) CN1681502A (ru)
AP (1) AP2005003260A0 (ru)
AR (1) AR041276A1 (ru)
AU (1) AU2003260810A1 (ru)
BR (1) BR0314577A (ru)
CA (1) CA2497971A1 (ru)
CO (1) CO5540390A2 (ru)
EA (1) EA200500376A1 (ru)
EC (1) ECSP055681A (ru)
HR (1) HRP20050251A2 (ru)
IS (1) IS7713A (ru)
MA (1) MA27442A1 (ru)
MX (1) MXPA05002982A (ru)
NO (1) NO20051010L (ru)
OA (1) OA12927A (ru)
PA (1) PA8583401A1 (ru)
PE (1) PE20050074A1 (ru)
PL (1) PL375974A1 (ru)
TW (1) TW200412346A (ru)
UY (1) UY27981A1 (ru)
WO (1) WO2004026307A1 (ru)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY140679A (en) 2001-05-24 2010-01-15 Avanir Pharmaceuticals Inhibitors of macrohage migration inhibitory factor and methods for identifying the same
WO2004026306A2 (en) * 2002-09-18 2004-04-01 Pfizer Products Inc. Pyrazole derivatives as transforming growth factor (tgf) inhibitors
BR0314383A (pt) 2002-09-18 2005-07-19 Pfizer Prod Inc Compostos de oxazol e tiazol como inibidores do fator de crescimento transformante(tgf)
EA200500378A1 (ru) 2002-09-18 2005-08-25 Пфайзер Продактс Инк. Новые соединения имидазола в качестве ингибиторов трансформирующего фактора роста (tgf)
PA8595001A1 (es) 2003-03-04 2004-09-28 Pfizer Prod Inc Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf)
PT1854789E (pt) * 2005-02-23 2013-10-23 Shionogi & Co Derivado de quinazolina possuindo actividade inibidora de tirosina-cinase
WO2007014198A1 (en) 2005-07-25 2007-02-01 Synta Pharmaceuticals Corp. 1, 2, 3 -triazoles inhibitors of tubulin polymerization for the treatment of poliferative disorders
WO2007070866A2 (en) * 2005-12-16 2007-06-21 Alcon, Inc. Control of intraocular pressure using alk5 modulation agents
DE102005061840A1 (de) 2005-12-23 2007-06-28 Merck Patent Gmbh Triazolderivate
WO2008009077A2 (en) * 2006-07-20 2008-01-24 Gilead Sciences, Inc. 4,6-dl- 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
WO2013078286A1 (en) 2011-11-22 2013-05-30 Cornell University Methods for stimulating hematopoietic recovery by inhibiting tgf beta signaling
CN105007939B (zh) 2012-10-05 2018-10-19 卡德门企业有限公司 人抗vegfr-2/kdr抗体
PT2970890T (pt) 2013-03-14 2020-04-24 Massachusetts Inst Technology Composições e métodos para expansão e cultura de células estaminais epiteliais
SI3089971T1 (sl) 2014-01-01 2020-11-30 Medivation Technologies Llc Spojine in postopki za uporabo
KR20230019500A (ko) 2014-09-03 2023-02-08 더 브리검 앤드 우먼즈 하스피털, 인크. 청력 손실의 치료를 위해 내이 털세포를 생성하기 위한 조성물, 시스템, 및 방법
CA2978188C (en) 2015-03-04 2020-05-12 Gilead Sciences, Inc. Toll-like receptor modulating 4,6-diamino-pyrido[3,2-d]pyrimidine compounds
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
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
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
US10640499B2 (en) 2016-09-02 2020-05-05 Gilead Sciences, Inc. Toll like receptor modulator compounds
WO2018045144A1 (en) 2016-09-02 2018-03-08 Gilead Sciences, Inc. Toll like receptor modulator compounds
CA3048220A1 (en) 2016-12-30 2018-07-05 Frequency Therapeutics, Inc. 1h-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells
EP3768267A4 (en) 2018-03-20 2022-04-20 Icahn School of Medicine at Mount Sinai KINA INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE
EP3827010A4 (en) 2018-07-23 2022-03-16 Brise Pharmaceuticals Co., Ltd. BISPHOSPHONATE-DRUG CONJUGATES
AU2019321641A1 (en) 2018-08-17 2021-04-15 Frequency Therapeutics, Inc. Compositions and methods for generating hair cells by upregulating Jag-1
WO2020037326A1 (en) 2018-08-17 2020-02-20 Frequency Therapeutics, Inc. Compositions and methods for generating hair cells by downregulating foxo
CN113508111A (zh) 2018-12-31 2021-10-15 西奈山伊坎医学院 激酶抑制剂化合物和组合物及使用方法
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
TW202212339A (zh) 2019-04-17 2022-04-01 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
AU7726898A (en) 1997-05-22 1998-12-11 G.D. Searle & Co. Pyrazole derivatives as p38 kinase inhibitors
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
EP0983260A2 (en) 1997-05-22 2000-03-08 G.D. Searle & Co. 3(5)-HETEROARYL SUBSTITUTED PYRAZOLES AS p38 KINASE INHIBITORS
DE69821132T2 (de) * 1997-10-27 2004-10-21 Takeda Chemical Industries Ltd 1,3-thiazole als adenosine a3 rezeptor antagonisten zur behandlung von asthma, allergien und diabetes
WO2000061576A1 (en) 1999-04-09 2000-10-19 Smithkline Beecham Corporation Triarylimidazoles
JP2000302680A (ja) * 1999-04-23 2000-10-31 Takeda Chem Ind Ltd 脳保護剤
AU6471300A (en) * 1999-08-06 2001-03-05 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
AU2002225730A1 (en) 2000-11-16 2002-05-27 Smith Kline Beecham Corporation Compounds
GB0027987D0 (en) 2000-11-16 2001-01-03 Smithkline Beecham Plc Compounds
WO2002051442A1 (fr) * 2000-12-26 2002-07-04 Takeda Chemical Industries, Ltd. Co-prescriptions
GB0100762D0 (en) 2001-01-11 2001-02-21 Smithkline Beecham Plc Novel use
WO2002062787A1 (en) 2001-02-02 2002-08-15 Glaxo Group Limited Pyrazoles as tgf inhibitors
GB0102665D0 (en) * 2001-02-02 2001-03-21 Glaxo Group Ltd Compounds
GB0102668D0 (en) * 2001-02-02 2001-03-21 Glaxo Group Ltd Compounds
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
GB0102673D0 (en) * 2001-02-02 2001-03-21 Glaxo Group Ltd Compounds
GB0102672D0 (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
WO2002100433A1 (en) * 2001-06-11 2002-12-19 Takeda Chemical Industries, Ltd. 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
US20050245520A1 (en) 2002-07-31 2005-11-03 Nerina Dodic 2-Phenylpyridin-4-yl derivatives as alk5 inhibitors

Also Published As

Publication number Publication date
CO5540390A2 (es) 2005-07-29
EP1542685A1 (en) 2005-06-22
BR0314577A (pt) 2005-08-09
US20040110798A1 (en) 2004-06-10
HRP20050251A2 (en) 2005-10-31
IS7713A (is) 2005-02-24
JP2006502236A (ja) 2006-01-19
CN1681502A (zh) 2005-10-12
AP2005003260A0 (en) 2005-03-31
UY27981A1 (es) 2004-04-30
AR041276A1 (es) 2005-05-11
PA8583401A1 (es) 2004-04-23
PE20050074A1 (es) 2005-03-21
PL375974A1 (en) 2005-12-12
KR20050057393A (ko) 2005-06-16
ECSP055681A (es) 2005-05-30
TW200412346A (en) 2004-07-16
WO2004026307A1 (en) 2004-04-01
CA2497971A1 (en) 2004-04-01
OA12927A (en) 2006-10-13
AU2003260810A1 (en) 2004-04-08
US7053095B2 (en) 2006-05-30
MA27442A1 (fr) 2005-07-01
US20060128761A1 (en) 2006-06-15
MXPA05002982A (es) 2005-06-22
NO20051010L (no) 2005-05-31

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