AU2004276341B2 - Pyrazolopyrrole derivatives as protein kinase inhibitors - Google Patents

Pyrazolopyrrole derivatives as protein kinase inhibitors Download PDF

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Publication number
AU2004276341B2
AU2004276341B2 AU2004276341A AU2004276341A AU2004276341B2 AU 2004276341 B2 AU2004276341 B2 AU 2004276341B2 AU 2004276341 A AU2004276341 A AU 2004276341A AU 2004276341 A AU2004276341 A AU 2004276341A AU 2004276341 B2 AU2004276341 B2 AU 2004276341B2
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AU
Australia
Prior art keywords
independently selected
aliphatic
compound
nitrogen
sulfur
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
AU2004276341A
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English (en)
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AU2004276341A1 (en
Inventor
Hayley Binch
Simon Everitt
Francesca Mazzei
Daniel Robinson
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Publication date
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of AU2004276341A1 publication Critical patent/AU2004276341A1/en
Application granted granted Critical
Publication of AU2004276341B2 publication Critical patent/AU2004276341B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Virology (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2004276341A 2003-09-23 2004-09-23 Pyrazolopyrrole derivatives as protein kinase inhibitors Ceased AU2004276341B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US50523603P 2003-09-23 2003-09-23
US60/505,236 2003-09-23
PCT/US2004/031610 WO2005030776A1 (en) 2003-09-23 2004-09-23 Pyrazolopyrrole derivatives as protein kinase inhibitors

Publications (2)

Publication Number Publication Date
AU2004276341A1 AU2004276341A1 (en) 2005-04-07
AU2004276341B2 true AU2004276341B2 (en) 2011-04-14

Family

ID=34392996

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2004276341A Ceased AU2004276341B2 (en) 2003-09-23 2004-09-23 Pyrazolopyrrole derivatives as protein kinase inhibitors

Country Status (7)

Country Link
US (2) US7652135B2 (https=)
EP (1) EP1668013B1 (https=)
JP (1) JP2007506787A (https=)
AT (1) ATE546452T1 (https=)
AU (1) AU2004276341B2 (https=)
CA (1) CA2539549A1 (https=)
WO (1) WO2005030776A1 (https=)

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ES2319539T3 (es) * 2003-09-17 2009-05-08 Janssen Pharmaceutica Nv Compuestos heterociclicos condensados como moduladores del receptor de serotonina.
NZ568692A (en) 2005-12-21 2011-07-29 Pfizer Prod Inc Carbonylamino pyrrolopyrazoles, potent kinase inhibitors
WO2007099171A2 (en) 2006-03-03 2007-09-07 Nerviano Medical Sciences S.R.L. Bicyclo-pyrazoles active as kinase inhibitors
EP2001455A2 (en) 2006-03-15 2008-12-17 Theralogics, Inc. Methods of treating muscular wasting diseases using nf-kb activation inhibitors
AR060358A1 (es) 2006-04-06 2008-06-11 Novartis Vaccines & Diagnostic Quinazolinas para la inhibicion de pdk 1
US20070286864A1 (en) * 2006-06-09 2007-12-13 Buck Elizabeth A Combined treatment with an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors
WO2008070823A2 (en) 2006-12-07 2008-06-12 University Of South Florida Substrate-mimetic akt inhibitor
AU2008237660B2 (en) * 2007-04-12 2011-12-22 Pfizer Inc. 3-amido-pyrrolo [3, 4-C] pyrazole-5 (1H, 4H, 6H) carbaldehyde derivatives as inhibitors of protein kinase C
AU2008256940A1 (en) * 2007-05-25 2008-12-04 Elan Pharmaceuticals, Inc. Pyrazolopyrrolidines as inhibitors of gamma secretase
KR101438293B1 (ko) 2009-09-21 2014-09-05 에프. 호프만-라 로슈 아게 Jak의 매크로사이클릭 억제자
KR102020485B1 (ko) 2013-01-11 2019-09-11 삼성디스플레이 주식회사 블록 공중합체, 그 형성 방법 및 패턴 형성 방법
CN112472699A (zh) 2013-07-26 2021-03-12 种族肿瘤学公司 改善比生群及衍生物的治疗益处的组合方法
WO2016109684A2 (en) * 2014-12-30 2016-07-07 Novira Therapeutics, Inc. Derivatives and methods of treating hepatitis b infections
AU2016355303B2 (en) * 2015-11-20 2021-10-07 Mingsight Pharmaceuticals, Inc. Treatment of autoimmune disease
EP3397643A1 (en) 2015-12-30 2018-11-07 Yissum Research Development Company of the Hebrew University of Jerusalem Ltd. Pt(IV) PRODRUGS
MY205440A (en) 2018-09-28 2024-10-21 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
JP7539382B2 (ja) * 2019-07-29 2024-08-23 武田薬品工業株式会社 複素環化合物
JP7697934B2 (ja) 2019-09-30 2025-06-24 ヤンセン ファーマシューティカ エヌ.ベー. 放射線標識されたmgl petリガンド
CN115073471B (zh) * 2021-03-11 2023-03-21 沈阳药科大学 吡唑并四氢吡咯类衍生物、其制备方法和在医药上的应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030171357A1 (en) * 2000-08-10 2003-09-11 Deniele Fancelli Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
AU2003244649A1 (en) * 2002-07-25 2004-02-23 Pharmacia Italia Spa Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them

Family Cites Families (22)

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DK27383A (da) 1982-02-17 1983-08-18 Lepetit Spa Fremgangsmaade til fremstilling af pyrazol(4,3-c)pyridiner
US5843912A (en) * 1994-07-06 1998-12-01 Universy Of Maryland Ring-expanded nucleosides and nucleotides
US6677310B1 (en) * 1999-04-21 2004-01-13 Nabi Ring-expanded nucleosides and nucleotides
DE4337611A1 (de) * 1993-11-04 1995-05-11 Boehringer Ingelheim Kg Neue Benzoylguanidine, ihre Herstellung und ihre Verwendung in Arzneimitteln
DE4337609A1 (de) 1993-11-04 1995-05-11 Boehringer Ingelheim Kg Neue Pyrazincarboxamidderivate, ihre Herstellung und ihre Verwendung in Arzneimitteln
US5508300A (en) * 1994-01-14 1996-04-16 Pfizer Inc. Dihydro pyrazolopyrroles, compositions and use
US6187774B1 (en) * 1996-03-04 2001-02-13 Yoshitomi Pharmaceutical Industries, Ltd. Fused heterocyclic compounds and pharmaceutical applications thereof
NZ511674A (en) 1998-12-23 2003-11-28 Du Pont Pharm Co Nitrogen containing heterobicycles as factor Xa inhibitors
CA2374947A1 (en) 1999-05-24 2000-11-30 Robert M. Scarborough Inhibitors of factor xa
JP2003502314A (ja) 1999-06-14 2003-01-21 イーライ・リリー・アンド・カンパニー 化合物
US7217722B2 (en) 2000-02-01 2007-05-15 Kirin Beer Kabushiki Kaisha Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same
DE10023486C1 (de) 2000-05-09 2002-03-14 Schering Ag Ortho substituierte Anthranilsäureamide und deren Verwendung als Arzneimittel
US6897231B2 (en) 2000-07-31 2005-05-24 Signal Pharmaceuticals, Inc. Indazole derivatives as JNK inhibitors and compositions and methods related thereto
WO2002022605A1 (en) * 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
CN1300116C (zh) 2001-04-16 2007-02-14 卫材株式会社 1h-吲唑化合物
WO2002100833A1 (en) 2001-06-12 2002-12-19 Sumitomo Pharmaceuticals Company, Limited Rho KINASE INHIBITORS
TW200306819A (en) * 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
US7429609B2 (en) 2002-05-31 2008-09-30 Eisai R & D Management Co., Ltd. Pyrazole compound and medicinal composition containing the same
EP1526852A1 (en) 2002-07-25 2005-05-04 Pharmacia Italia S.p.A. Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
UA81790C2 (uk) 2002-12-19 2008-02-11 Фармация Италия С.П.А. Заміщені піролопіразольні похідні як інгібітори кінази
US20070037790A1 (en) * 2003-03-11 2007-02-15 Francesca Abrate Bicyclo-pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
US7141568B2 (en) * 2003-07-09 2006-11-28 Pfizer Italia S.R.L. Pyrrolo[3,4-c]pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030171357A1 (en) * 2000-08-10 2003-09-11 Deniele Fancelli Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
AU2003244649A1 (en) * 2002-07-25 2004-02-23 Pharmacia Italia Spa Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them

Also Published As

Publication number Publication date
CA2539549A1 (en) 2005-04-07
ATE546452T1 (de) 2012-03-15
JP2007506787A (ja) 2007-03-22
US7652135B2 (en) 2010-01-26
US8642779B2 (en) 2014-02-04
EP1668013A1 (en) 2006-06-14
AU2004276341A1 (en) 2005-04-07
US20050101594A1 (en) 2005-05-12
US20100087467A1 (en) 2010-04-08
WO2005030776A1 (en) 2005-04-07
EP1668013B1 (en) 2012-02-22

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FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired