OA12929A - Pyrazole derivatives as transforming growth (TGF) inhibitors. - Google Patents

Pyrazole derivatives as transforming growth (TGF) inhibitors. Download PDF

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Publication number
OA12929A
OA12929A OA1200500078A OA1200500078A OA12929A OA 12929 A OA12929 A OA 12929A OA 1200500078 A OA1200500078 A OA 1200500078A OA 1200500078 A OA1200500078 A OA 1200500078A OA 12929 A OA12929 A OA 12929A
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OA
OAPI
Prior art keywords
alkyl
cio
phenyl
cycloalkyl
heteroaryl
Prior art date
Application number
OA1200500078A
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English (en)
Inventor
Laura Cook Blumberg
Michael John Munchhof
Original Assignee
Pfizer Prod Inc
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 Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of OA12929A publication Critical patent/OA12929A/en

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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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
OA1200500078A 2002-09-18 2003-09-08 Pyrazole derivatives as transforming growth (TGF) inhibitors. OA12929A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US41214602P 2002-09-18 2002-09-18
US48454303P 2003-07-02 2003-07-02

Publications (1)

Publication Number Publication Date
OA12929A true OA12929A (en) 2006-10-13

Family

ID=32033585

Family Applications (1)

Application Number Title Priority Date Filing Date
OA1200500078A OA12929A (en) 2002-09-18 2003-09-08 Pyrazole derivatives as transforming growth (TGF) inhibitors.

Country Status (27)

Country Link
US (4) US6958354B2 (es)
EP (2) EP2165708A3 (es)
JP (1) JP4519657B2 (es)
KR (1) KR20050044807A (es)
CN (1) CN1681501A (es)
AP (1) AP2005003263A0 (es)
AR (1) AR041272A1 (es)
AT (1) ATE450258T1 (es)
AU (1) AU2003259475A1 (es)
BR (1) BR0314302A (es)
CA (1) CA2496295C (es)
CO (1) CO5550456A2 (es)
DE (1) DE60330362D1 (es)
EA (1) EA200500377A1 (es)
EC (1) ECSP055679A (es)
ES (1) ES2335099T3 (es)
HR (1) HRP20050247A2 (es)
IS (1) IS7698A (es)
MA (1) MA27440A1 (es)
MX (1) MXPA05002376A (es)
NO (1) NO20050838L (es)
OA (1) OA12929A (es)
PA (1) PA8583201A1 (es)
PE (1) PE20040988A1 (es)
PL (1) PL375979A1 (es)
UY (1) UY27985A1 (es)
WO (1) WO2004026306A2 (es)

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DE60330362D1 (de) * 2002-09-18 2010-01-14 Pfizer Prod Inc Neue pyrazol-verbindungen als hemmer des transformierenden wachstumsfaktors (tgf)
ES2325687T3 (es) * 2002-09-18 2009-09-14 Pfizer Products Inc. Compuestos de imidazol novedosos como inhibidores del factor de crecimiento transformante (tgf).
CL2004000234A1 (es) * 2003-02-12 2005-04-15 Biogen Idec Inc Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid
PA8595001A1 (es) * 2003-03-04 2004-09-28 Pfizer Prod Inc Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf)
GB0313915D0 (en) * 2003-06-16 2003-07-23 Smithkline Beecham Corp Compounds
WO2006026305A1 (en) * 2004-08-31 2006-03-09 Biogen Idec Ma Inc Pyrimidinylpyrazoles as tgf-beta inhibitors
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TW200639163A (en) * 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
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GEP20115239B (en) 2006-10-31 2011-06-10 Pfizer Prod Inc Pyrazoline compounds as mineralocorticoid receptor antagonists
WO2009016460A2 (en) * 2007-08-01 2009-02-05 Pfizer Inc. Pyrazole compounds and their use as raf inhibitors
PL3089971T3 (pl) 2014-01-01 2021-01-25 Medivation Technologies Llc Związki i sposoby ich zastosowania
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US10669528B2 (en) 2015-06-25 2020-06-02 Children's Medical Center Corporation Methods and compositions relating to hematopoietic stem cell expansion, enrichment, and maintenance
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DK3470409T3 (da) * 2016-06-13 2020-05-11 Genfleet Therapeutics Shanghai Inc Benzotriazol-afledt Alfa- og Beta-umættet amidforbindelse anvendt som TGF-BRI-hæmmer
US11266647B2 (en) * 2016-10-26 2022-03-08 Icahn School Of Medicine At Mount Sinai Method for increasing cell proliferation in pancreatic beta cells, treatment method, and composition
WO2018086609A1 (zh) * 2016-11-14 2018-05-17 江苏恒瑞医药股份有限公司 3,4-二吡啶基吡唑类衍生物、其制备方法及其在医药上的应用
WO2019100062A1 (en) 2017-11-20 2019-05-23 Ichan School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
CN111479809B (zh) * 2017-12-13 2021-10-29 劲方医药科技(上海)有限公司 一种TGF-βRI抑制剂的晶型、盐型及其制备方法
US11788064B2 (en) 2018-01-05 2023-10-17 Icahn School Of Medicine At Mount Sinai Method of increasing proliferation of pancreatic beta cells, treatment method, and composition
JP2021518413A (ja) 2018-03-20 2021-08-02 アイカーン スクール オブ メディシン アット マウント サイナイ キナーゼ阻害剤化合物及び組成物ならびに使用方法
TW202012390A (zh) * 2018-06-29 2020-04-01 日商日本歐愛特農業科技股份有限公司 新穎之經取代吡唑衍生物
WO2020113094A1 (en) 2018-11-30 2020-06-04 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
US10952996B2 (en) 2018-12-11 2021-03-23 Theravance Biopharma R&D Ip, Llc ALK5 inhibitors
CN110467601B (zh) * 2019-08-29 2021-07-02 杭州市西溪医院 一种吡唑联吡啶酮类化合物、中间体及其制备方法及应用
TW202132297A (zh) 2019-11-22 2021-09-01 美商施萬生物製藥研發Ｉｐ有限責任公司 經取代吡啶及使用方法

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ES2325687T3 (es) 2002-09-18 2009-09-14 Pfizer Products Inc. Compuestos de imidazol novedosos como inhibidores del factor de crecimiento transformante (tgf).
MXPA05002982A (es) 2002-09-18 2005-06-22 Pfizer Prod Inc Derivados de triazol como inhibidores del factor de crecimiento transformante (tgf).
AP2005003262A0 (en) 2002-09-18 2005-03-31 Pfizer Prod Inc Novel isothiazole and isoxazole compounds as tranforming growth factor (TGF) inhibitors.
EA200500354A1 (ru) 2002-09-18 2005-10-27 Пфайзер Продактс Инк. Новые оксазольные и тиазольные соединения в качестве ингибиторов трансформирующего фактора роста (тфр)
DE60330362D1 (de) 2002-09-18 2010-01-14 Pfizer Prod Inc Neue pyrazol-verbindungen als hemmer des transformierenden wachstumsfaktors (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)

Also Published As

Publication number Publication date
WO2004026306A3 (en) 2004-07-01
ECSP055679A (es) 2005-05-30
AU2003259475A1 (en) 2004-04-08
CO5550456A2 (es) 2005-08-31
EP2165708A2 (en) 2010-03-24
US20070117850A1 (en) 2007-05-24
KR20050044807A (ko) 2005-05-12
AR041272A1 (es) 2005-05-11
BR0314302A (pt) 2005-07-05
US20060025451A1 (en) 2006-02-02
JP4519657B2 (ja) 2010-08-04
DE60330362D1 (de) 2010-01-14
CA2496295C (en) 2010-11-23
US20100056571A1 (en) 2010-03-04
US6958354B2 (en) 2005-10-25
PE20040988A1 (es) 2004-12-25
JP2006507353A (ja) 2006-03-02
WO2004026306A2 (en) 2004-04-01
US7638537B2 (en) 2009-12-29
US20040116474A1 (en) 2004-06-17
CN1681501A (zh) 2005-10-12
EP2165708A3 (en) 2010-07-28
AP2005003263A0 (en) 2005-03-31
HRP20050247A2 (en) 2005-10-31
ES2335099T3 (es) 2010-03-22
PA8583201A1 (es) 2004-04-23
PL375979A1 (en) 2005-12-12
MXPA05002376A (es) 2005-05-23
ATE450258T1 (de) 2009-12-15
EP1542684A2 (en) 2005-06-22
IS7698A (is) 2005-02-17
EP1542684B1 (en) 2009-12-02
NO20050838L (no) 2005-05-18
US7151110B2 (en) 2006-12-19
CA2496295A1 (en) 2004-04-01
EA200500377A1 (ru) 2005-08-25
MA27440A1 (fr) 2005-07-01
UY27985A1 (es) 2004-04-30

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