AP1246A - Substituted pyrazoles as p38 Kinase inhibitors. - Google Patents

Substituted pyrazoles as p38 Kinase inhibitors.

Info

Publication number
AP1246A
AP1246A APAP/P/1999/001715A AP9901715A AP1246A AP 1246 A AP1246 A AP 1246A AP 9901715 A AP9901715 A AP 9901715A AP 1246 A AP1246 A AP 1246A
Authority
AP
ARIPO
Prior art keywords
kinase inhibitors
substituted pyrazoles
pyrazoles
substituted
class
Prior art date
Application number
APAP/P/1999/001715A
Other versions
AP9901715A0 (en
Inventor
Ashok Anantanarayan
Michael Clare
Paul W Collins
Joyce Zuowu Crich
Rajesh Devraj
Daniel L Flynn
Lifeng Geng
Gunnar J Hanson
Francis J Koszyk
Shuyuan Liao
Richard A Partis
Shashidhar N Rao
Shaun Raj Selness
Michael J South
Michael A Stealey
Richard M Weier
Xiangdong Xu
Original Assignee
Searle & Co
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 Searle & Co filed Critical Searle & Co
Publication of AP9901715A0 publication Critical patent/AP9901715A0/en
Application granted granted Critical
Publication of AP1246A publication Critical patent/AP1246A/en

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    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • 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

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by formula (i)wherein r1, r2, r3 and r4 are as described in the specification
APAP/P/1999/001715A 1997-05-22 1998-05-22 Substituted pyrazoles as p38 Kinase inhibitors. AP1246A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US4757097P 1997-05-22 1997-05-22
PCT/US1998/010436 WO1998052940A1 (en) 1997-05-22 1998-05-22 SUBSTITUTED PYRAZOLES AS p38 KINASE INHIBITORS

Publications (2)

Publication Number Publication Date
AP9901715A0 AP9901715A0 (en) 1999-12-31
AP1246A true AP1246A (en) 2004-02-07

Family

ID=21949743

Family Applications (1)

Application Number Title Priority Date Filing Date
APAP/P/1999/001715A AP1246A (en) 1997-05-22 1998-05-22 Substituted pyrazoles as p38 Kinase inhibitors.

Country Status (24)

Country Link
EP (1) EP1000055A1 (en)
JP (1) JP2002508754A (en)
KR (1) KR20010012854A (en)
CN (1) CN1264377A (en)
AP (1) AP1246A (en)
AU (1) AU754830C (en)
BG (1) BG64313B1 (en)
BR (1) BR9809147A (en)
CA (1) CA2291115A1 (en)
EA (1) EA003925B1 (en)
EE (1) EE9900527A (en)
GE (1) GEP20033053B (en)
HU (1) HUP0001880A3 (en)
ID (1) ID22982A (en)
IL (1) IL132991A (en)
IS (1) IS5257A (en)
NO (1) NO995695L (en)
NZ (1) NZ501112A (en)
OA (1) OA12981A (en)
PL (1) PL337020A1 (en)
SK (1) SK157899A3 (en)
TR (1) TR200000235T2 (en)
WO (1) WO1998052940A1 (en)
ZA (1) ZA984358B (en)

Families Citing this family (88)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW289752B (en) * 1994-03-11 1996-11-01 Ciba Geigy Ag
US5559137A (en) * 1994-05-16 1996-09-24 Smithkline Beecham Corp. Compounds
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
US6979686B1 (en) 2001-12-07 2005-12-27 Pharmacia Corporation Substituted pyrazoles as p38 kinase inhibitors
EP1023066A4 (en) 1997-06-13 2001-05-23 Smithkline Beecham Corp Novel pyrazole and pyrazoline substituted compounds
US7301021B2 (en) 1997-07-02 2007-11-27 Smithkline Beecham Corporation Substituted imidazole compounds
US6858617B2 (en) 1998-05-26 2005-02-22 Smithkline Beecham Corporation Substituted imidazole compounds
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
US6649617B1 (en) 1998-10-07 2003-11-18 Smithkline Beecham Corporation Treatment for stroke management
ATE258055T1 (en) 1998-11-04 2004-02-15 Smithkline Beecham Corp PYRIDINE-4-YL OR PYRIMIDINE-4-YL SUBSTITUTED PYRAZINE
CA2355075C (en) 1998-12-16 2009-12-08 Aventis Pharma Limited Heteroaryl-cyclic acetals
US6191147B1 (en) * 1998-12-24 2001-02-20 Ppd Discovery, Inc. Pyrazole compounds and uses thereof
WO2000039116A1 (en) * 1998-12-25 2000-07-06 Teikoku Hormone Mfg. Co., Ltd. Aminopyrazole derivatives
UA72244C2 (en) 1999-03-26 2005-02-15 Aryl-substituted pyrazols, imidazols, oxazols, thiazols, pyrrols and their use
CN1281604C (en) * 1999-06-03 2006-10-25 帝国脏器制药株式会社 Substituted pyrazole compounds
US7122666B2 (en) 1999-07-21 2006-10-17 Sankyo Company, Limited Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses
JP2003531103A (en) * 1999-08-12 2003-10-21 バーテックス ファーマシューティカルズ インコーポレイテッド Inhibitors of c-JUNN-terminal kinase (JNK) and other protein kinases
AU7922100A (en) * 1999-10-25 2001-05-08 Basf Aktiengesellschaft Agrochemical compositions containing pyrazoles as the active agents and use of said compositions as plant protection agents with a fungicidal action
DE19952147A1 (en) 1999-10-29 2001-05-03 Boehringer Ingelheim Pharma New cyclopropanes, pharmaceutical compositions containing these compounds and process for their preparation
WO2001038314A1 (en) 1999-11-23 2001-05-31 Smithkline Beecham Corporation 3,4-dihydro-(1h)quinazolin-2-one compounds as csbp/p38 kinase inhibitors
ES2249309T3 (en) 1999-11-23 2006-04-01 Smithkline Beecham Corp COMPOUNDS OF 3,4-DIHIDRO- (1H) QUINAZOLIN-2-ONA AS INHIBITORS OF CSBP / P39 KINASA.
ES2230171T3 (en) 1999-11-23 2005-05-01 Smithkline Beecham Corporation 3,4-DIHIDRO- (1H) QUINAZOLIN-2-ONA COMPOUNDS AS CSBP / P38 QUINASA INHIBITORS.
US7235551B2 (en) 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
NZ524192A (en) 2000-08-14 2005-02-25 Ortho Mcneil Pharm Inc Substituted pyrazoles
GB0102687D0 (en) 2001-02-02 2001-03-21 Pharmacia & Upjohn Spa Oxazolyl-pyrazole derivatives active as kinase inhibitors,process for their preparation and pharmaceutical compositions comprising them
WO2002062792A1 (en) * 2001-02-02 2002-08-15 Takeda Chemical Industries, Ltd. Jnk inhibitor
DE60227794D1 (en) 2001-04-26 2008-09-04 Eisai R&D Man Co Ltd NITROGENIC COMPOUND WITH CONDENSED RING AND PYRAZOLYL GROUP AS A SUBSTITUENT AND MEDICAL COMPOSITION THEREOF
SK287857B6 (en) 2001-05-24 2012-01-04 Eli Lilly And Company Novel pyrrole derivatives as pharmaceutical agents
US7057049B2 (en) 2001-09-25 2006-06-06 Pharmacia Corporation Process for making substituted pyrazoles
RU2277534C2 (en) * 2001-09-25 2006-06-10 Фармация Корпорейшн Method for preparing substituted pyrazoles
IL161009A0 (en) 2001-09-25 2004-08-31 Pharmacia Corp Process for making substituted pyrazoles
US20040082551A1 (en) * 2002-06-05 2004-04-29 Benson Alan G. Novel pyrazoles and their use as p38 kinase inhibitors
GB0215844D0 (en) 2002-07-09 2002-08-14 Novartis Ag Organic compounds
ES2278170T3 (en) 2002-07-09 2007-08-01 BOEHRINGER INGELHEIM PHARMA GMBH & CO.KG PHARMACEUTICAL COMPOSITIONS OF ANTICOLINERGIC AND INHIBITORS OF QUINASE P38 IN THE TREATMENT OF RESPIRATORY DISEASES.
GB0217786D0 (en) * 2002-07-31 2002-09-11 Glaxo Group Ltd Compounds
AU2003265395A1 (en) 2002-08-14 2004-03-03 Ppd Discovery, Inc. Prenylation inhibitors and methods of their synthesis and use
US6649638B1 (en) 2002-08-14 2003-11-18 Ppd Discovery, Inc. Prenylation inhibitors and methods of their synthesis and use
WO2004026302A1 (en) * 2002-09-19 2004-04-01 Eli Lilly And Company Methods of inhibiting tgf beta with substituted pyrazoles
GB0229618D0 (en) * 2002-12-19 2003-01-22 Cancer Rec Tech Ltd Pyrazole compounds
DE602004028800D1 (en) 2003-02-07 2010-10-07 Daiichi Sankyo Co Ltd Pyrazolderivat
US20060035893A1 (en) 2004-08-07 2006-02-16 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
EP1778686B9 (en) 2004-08-12 2009-07-08 Pfizer Limited Triazolopyridinylsulfanyl derivatives as p38 map kinase inhibitors
PE20060777A1 (en) 2004-12-24 2006-10-06 Boehringer Ingelheim Int INDOLINONE DERIVATIVES FOR THE TREATMENT OR PREVENTION OF FIBROTIC DISEASES
WO2006070927A1 (en) 2004-12-28 2006-07-06 Aska Pharmaceutical Co., Ltd. Pyrimidinylisoxazol derivative
EP2024353A2 (en) * 2006-03-16 2009-02-18 Pfizer Products Inc. Pyrazole compounds
JP5244591B2 (en) 2006-06-28 2013-07-24 あすか製薬株式会社 Pyridylisoxazole derivatives
CN101478989A (en) * 2006-06-28 2009-07-08 Aska制药株式会社 Treatment agent for inflammatory bowel disease
AU2008215659B2 (en) 2007-02-16 2012-11-01 Aska Pharmaceutical Co., Ltd. Pharmaceutical composition comprising microparticle oily suspension
EP1992344A1 (en) 2007-05-18 2008-11-19 Institut Curie P38 alpha as a therapeutic target in pathologies linked to FGFR3 mutation
JP2010533147A (en) * 2007-07-13 2010-10-21 アデックス ファルマ エス．エイ． Pyrazole derivatives as modulators of metabotropic glutamate receptors
CL2008003407A1 (en) 2007-11-16 2010-01-11 Boehringer Ingelheim Int Substituted heterobicyclo aryl- and heteroarylcarbonyl derivative compounds; pharmaceutical composition; preparation procedure; and its use in the treatment and / or prevention of metabolic disorders, mediated by the inhibition of the enzyme hsd-1.
CL2009000904A1 (en) * 2008-04-21 2010-04-30 Shionogi & Co Compounds derived from cyclohexyl sulfonamides having antagonist activity at the npy y5 receptor, pharmaceutical composition and pharmaceutical formulation comprising them.
TW200950780A (en) 2008-05-13 2009-12-16 Boehringer Ingelheim Int Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use
AU2009273197B2 (en) 2008-07-24 2014-01-16 Nerviano Medical Sciences S.R.L. 3,4-diarylpyrazoles as protein kinase inhibitors
CA2735204C (en) * 2008-08-25 2017-06-20 Boehringer Ingelheim International Gmbh Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use
KR20110070885A (en) * 2008-10-23 2011-06-24 론자 리미티드 Synthesis method of substituted pyrazole
BRPI0921097B8 (en) * 2008-11-21 2021-05-25 Raqualia Pharma Inc compound or its pharmaceutically acceptable salt, intermediate of the compound, pharmaceutical composition and use of the compound
EP2438049B1 (en) 2009-06-02 2014-05-14 Boehringer Ingelheim International GmbH Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
WO2011011123A1 (en) 2009-06-11 2011-01-27 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure
IN2012DN01693A (en) * 2009-08-26 2015-06-05 Novartis Ag
JO3002B1 (en) 2009-08-28 2016-09-05 Irm Llc Protein kinase inhibitors
EP2308866A1 (en) * 2009-10-09 2011-04-13 Bayer CropScience AG Phenylpyri(mi)dinylpyrazoles and their use as fungicides
CN102762551A (en) 2009-12-21 2012-10-31 拜尔农作物科学股份公司 Thienylpyrimidinylpyrazoles and their use for controlling plant pathogens
WO2011092088A1 (en) 2010-01-27 2011-08-04 Nerviano Medical Sciences S.R.L. Sulfonamido derivatives of 3,4-diarylpyrazoles as protein kinase inhibitors
AR081810A1 (en) 2010-04-07 2012-10-24 Bayer Cropscience Ag BICYCLE PIRIDINYL PIRAZOLS
JP5860042B2 (en) 2010-06-16 2016-02-16 ヴァイティー ファーマシューティカルズ，インコーポレイテッド Substituted 5, 6 and 7 membered heterocycles, medicaments containing such compounds and their use
JP5938038B2 (en) 2010-08-03 2016-06-22 ネルヴィアーノ・メディカル・サイエンシズ・ソチエタ・ア・レスポンサビリタ・リミタータ Derivatives of pyrazolophenyl-benzenesulfonamide compounds and their use as antitumor agents
WO2012085721A1 (en) * 2010-12-20 2012-06-28 Pfizer Inc. Novel fused pyridine compounds as casein kinase inhibitors
WO2012175513A1 (en) 2011-06-20 2012-12-27 Bayer Intellectual Property Gmbh Thienylpyri(mi)dinylpyrazole
JP2014524438A (en) 2011-08-17 2014-09-22 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Indenopyridine derivatives
WO2013050434A1 (en) 2011-10-06 2013-04-11 Bayer Intellectual Property Gmbh Heterocyclylpyri(mi)dinylpyrazole
UA114490C2 (en) 2011-10-06 2017-06-26 Байєр Інтеллектуал Проперті Гмбх Heterocyclylpyri(mi)dinylpyrazole as fungicidals
DE102011115525A1 (en) 2011-10-11 2013-04-11 Boehringer Ingelheim International Gmbh Two-part bottle packaging device for containing pharmaceutical tablets or capsules, has bottle body and bottle base, where bottle is closed with pressure lock or with pressure lock injected at bottle body or with separate rotary lock
CN103917236A (en) 2011-11-11 2014-07-09 诺华股份有限公司 Methods of treating proliferative diseases
DK2782557T3 (en) 2011-11-23 2018-12-10 Array Biopharma Inc PHARMACEUTICAL FORMULATIONS
KR102283996B1 (en) 2013-03-15 2021-07-29 더 스크립스 리서치 인스티튜트 Compounds and methods for inducing chondrogenesis
US9573904B2 (en) * 2013-12-12 2017-02-21 Sumitomo Chemical Company, Limited Aromatic compound and use thereof
CN104829536B (en) * 2015-05-04 2017-12-29 陕西科技大学 A kind of Phenylpyrazole carboxylic acid compound and its synthetic method for having antitumor activity
EP3303284B1 (en) * 2015-05-27 2020-04-08 Kyorin Pharmaceutical Co., Ltd. Urea derivative or pharmacologically acceptable salt thereof
CN112457255B (en) * 2017-11-08 2022-08-19 北京嘉林药业股份有限公司 Compounds and their use for treating cancer
EP3886854A4 (en) 2018-11-30 2022-07-06 Nuvation Bio Inc. PYRROLE AND PYRAZOLE COMPOUNDS AND METHODS OF USE THEREOF
WO2020124397A1 (en) 2018-12-19 2020-06-25 Inventisbio Shanghai Ltd. C-terminal src kinase inhibitors
US12479816B2 (en) 2019-02-08 2025-11-25 University of Pittsburgh—of the Commonwealth System of Higher Education 20-HETE formation inhibitors
US11091447B2 (en) 2020-01-03 2021-08-17 Berg Llc UBE2K modulators and methods for their use
EP3978487A1 (en) * 2020-09-30 2022-04-06 Origo Biopharma, S.L. 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-acetamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5
WO2022146698A1 (en) * 2020-12-29 2022-07-07 Revolution Medicines, Inc. Sos1 inhibitors and uses thereof
WO2025231152A1 (en) * 2024-04-30 2025-11-06 The Cleveland Clinic Foundation Compounds and methods for restoring beta-adrenergic receptor function

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996003385A1 (en) * 1994-07-21 1996-02-08 G.D. Searle & Co. 3,4-substituted pyrazoles for the treatment of inflammation
US5559137A (en) * 1994-05-16 1996-09-24 Smithkline Beecham Corp. Compounds

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2753659B2 (en) * 1990-09-03 1998-05-20 株式会社大塚製薬工場 Pyrazole derivatives
US5593992A (en) * 1993-07-16 1997-01-14 Smithkline Beecham Corporation Compounds
JP3734180B2 (en) * 1994-12-28 2006-01-11 エーザイ株式会社 New pyrazole derivatives

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5559137A (en) * 1994-05-16 1996-09-24 Smithkline Beecham Corp. Compounds
WO1996003385A1 (en) * 1994-07-21 1996-02-08 G.D. Searle & Co. 3,4-substituted pyrazoles for the treatment of inflammation

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