CA2539549A1 - Pyrazolopyrrole derivatives as protein kinase inhibitors - Google Patents

Pyrazolopyrrole derivatives as protein kinase inhibitors Download PDF

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Publication number
CA2539549A1
CA2539549A1 CA002539549A CA2539549A CA2539549A1 CA 2539549 A1 CA2539549 A1 CA 2539549A1 CA 002539549 A CA002539549 A CA 002539549A CA 2539549 A CA2539549 A CA 2539549A CA 2539549 A1 CA2539549 A1 CA 2539549A1
Authority
CA
Canada
Prior art keywords
independently selected
nitrogen
sulfur
oxygen
membered saturated
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.)
Abandoned
Application number
CA002539549A
Other languages
English (en)
French (fr)
Inventor
Hayley Binch
Simon Everitt
Francesca Mazzei
Daniel Robinson
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Vertex Pharmaceuticals Inc
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2539549A1 publication Critical patent/CA2539549A1/en
Abandoned legal-status Critical Current

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Classifications

    • 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

Landscapes

  • 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)
CA002539549A 2003-09-23 2004-09-23 Pyrazolopyrrole derivatives as protein kinase inhibitors Abandoned CA2539549A1 (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 (1)

Publication Number Publication Date
CA2539549A1 true CA2539549A1 (en) 2005-04-07

Family

ID=34392996

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002539549A Abandoned CA2539549A1 (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=)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
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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

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
DK1320531T3 (da) * 2000-08-10 2011-01-03 Pfizer Italia Srl Bicyclo-pyrazoler, der er aktive som kinase inhibitorer, fremgangsmåde til fremstilling deraf og farmaceutiske sammensætninger, der indeholder disse
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
CA2493637A1 (en) * 2002-07-25 2004-02-12 Manuela Villa Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
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

Also Published As

Publication number Publication date
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
AU2004276341B2 (en) 2011-04-14

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued

Effective date: 20130307