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

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—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
    • A61K31/41—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P3/08—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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Endocrinology (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 (enExample)
EP (1) EP1668013B1 (enExample)
JP (1) JP2007506787A (enExample)
AT (1) ATE546452T1 (enExample)
AU (1) AU2004276341B2 (enExample)
CA (1) CA2539549A1 (enExample)
WO (1) WO2005030776A1 (enExample)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG146683A1 (en) * 2003-09-17 2008-10-30 Janssen Pharmaceutica Nv Fused heterocyclic compounds as serotonin receptor modulators
MY151455A (en) * 2005-12-21 2014-05-30 Pfizer Prod Inc Carbonylamino pyrrolopyrazoles, potent kinase inhibitors
EP1999131B1 (en) 2006-03-03 2013-10-23 Nerviano Medical Sciences S.r.l. Bicyclo-pyrazoles active as kinase inhibitors
CA2646316C (en) * 2006-03-15 2016-05-24 Theralogics, Inc. Methods of treating muscular wasting diseases using nf-kb activation inhibitors
TW200808739A (en) 2006-04-06 2008-02-16 Novartis Vaccines & Diagnostic Quinazolines for PDK1 inhibition
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
CN101675052A (zh) 2007-04-12 2010-03-17 辉瑞大药厂 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物
MX2009012525A (es) * 2007-05-25 2009-12-09 Elan Pharm Inc Pirazol-pirrolidinas como inhibidores de gamma secretasa.
MX2012002385A (es) * 2009-09-21 2012-04-02 Hoffmann La Roche Inhibidores macrociclicos de cinasa janus.
KR102020485B1 (ko) 2013-01-11 2019-09-11 삼성디스플레이 주식회사 블록 공중합체, 그 형성 방법 및 패턴 형성 방법
AU2014293013A1 (en) 2013-07-26 2016-03-17 Race Oncology Ltd. Combinatorial methods to improve the therapeutic benefit of bisantrene
WO2016109689A2 (en) * 2014-12-30 2016-07-07 Novira Therapeutics, Inc. Derivatives and methods of treating hepatitis b infections
CA3005723A1 (en) * 2015-11-20 2017-05-26 Mingsight Pharmaceuticals, Inc. Treatment of autoimmune disease
US20190290656A1 (en) 2015-12-30 2019-09-26 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd Pt(iv) prodrugs
MA53721A (fr) 2018-09-28 2021-09-15 Janssen Pharmaceutica Nv Modulateurs de la monoacylglycérol lipase
WO2021020363A1 (ja) * 2019-07-29 2021-02-04 武田薬品工業株式会社 複素環化合物
CA3156100A1 (en) 2019-09-30 2021-04-08 Janssen Pharmaceutica Nv Radiolabelled mgl pet ligands
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
US6677310B1 (en) 1999-04-21 2004-01-13 Nabi Ring-expanded nucleosides and nucleotides
US5843912A (en) 1994-07-06 1998-12-01 Universy Of Maryland 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
WO2000071511A2 (en) 1999-05-24 2000-11-30 Cor Therapeutics, Inc. INHIBITORS OF FACTOR Xa
CA2375920A1 (en) 1999-06-14 2000-12-21 Eli Lilly And Company Compounds
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
CA2416527C (en) 2000-08-10 2009-12-22 Pharmacia Italia S.P.A. Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
AU2001290912A1 (en) * 2000-09-15 2002-03-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
WO2002083648A1 (fr) 2001-04-16 2002-10-24 Eisai Co., Ltd. Nouveau compose a base de 1h-indazole
EP1403255A4 (en) 2001-06-12 2005-04-06 Sumitomo Pharma RHO KINASE INHIBITORS
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
CN1656079A (zh) 2002-05-31 2005-08-17 卫材株式会社 吡唑化合物和含有该化合物的药物组合物
MXPA05000945A (es) * 2002-07-25 2005-05-16 Pharmacia Italia Spa Biciclo-pirazoles activos como inhibidores de la cinasa, procedimientos para su preparacion y composiciones farmaceuticas que los contienen.
US20060100233A1 (en) 2002-07-25 2006-05-11 Manuela Villa 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
BRPI0408486A (pt) * 2003-03-11 2006-04-04 Pharmacia Italia Spa derivados de biciclopirazol ativos como inibidores da cinase, processo para a sua preparação e composições farmacêuticas compreendendo-os
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
WO2005030776A1 (en) 2005-04-07
US20050101594A1 (en) 2005-05-12
US20100087467A1 (en) 2010-04-08
US7652135B2 (en) 2010-01-26
JP2007506787A (ja) 2007-03-22
EP1668013A1 (en) 2006-06-14
US8642779B2 (en) 2014-02-04
AU2004276341B2 (en) 2011-04-14
AU2004276341A1 (en) 2005-04-07
EP1668013B1 (en) 2012-02-22
ATE546452T1 (de) 2012-03-15

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued

Effective date: 20130307