CA2637335A1 - Thiophene-carboxamides useful as inhibitors of protein kinases - Google Patents

Thiophene-carboxamides useful as inhibitors of protein kinases Download PDF

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Publication number
CA2637335A1
CA2637335A1 CA002637335A CA2637335A CA2637335A1 CA 2637335 A1 CA2637335 A1 CA 2637335A1 CA 002637335 A CA002637335 A CA 002637335A CA 2637335 A CA2637335 A CA 2637335A CA 2637335 A1 CA2637335 A1 CA 2637335A1
Authority
CA
Canada
Prior art keywords
compound
ring
formula
aliphatic
halo
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
CA002637335A
Other languages
English (en)
French (fr)
Inventor
Steven Durrant
Jean-Damien Charrier
Ronald Knegtel
Guy Brenchley
David Kay
Shazia Sadiq
Sharn Ramaya
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 CA2637335A1 publication Critical patent/CA2637335A1/en
Abandoned legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA002637335A 2006-01-23 2007-01-23 Thiophene-carboxamides useful as inhibitors of protein kinases Abandoned CA2637335A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US76109706P 2006-01-23 2006-01-23
US60/761,097 2006-01-23
PCT/US2007/001726 WO2007087283A2 (en) 2006-01-23 2007-01-23 Thiophene-carboxamides useful as inhibitors of protein kinases

Publications (1)

Publication Number Publication Date
CA2637335A1 true CA2637335A1 (en) 2007-08-02

Family

ID=38179584

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002637335A Abandoned CA2637335A1 (en) 2006-01-23 2007-01-23 Thiophene-carboxamides useful as inhibitors of protein kinases

Country Status (7)

Country Link
US (3) US7915305B2 (enExample)
EP (2) EP1989205B1 (enExample)
JP (2) JP5498703B2 (enExample)
CN (1) CN101400678A (enExample)
AU (1) AU2007208358A1 (enExample)
CA (1) CA2637335A1 (enExample)
WO (1) WO2007087283A2 (enExample)

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US7595330B2 (en) 2005-09-06 2009-09-29 Smithkline Beecham Corporation Benzimidazole thiophene compounds
WO2007087283A2 (en) 2006-01-23 2007-08-02 Vertex Pharmaceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
US7829590B2 (en) 2006-04-13 2010-11-09 Guy Brenchley Thiophene-carboxamides useful as inhibitors of protein kinases
US7851495B2 (en) 2006-05-23 2010-12-14 Vertex Pharmaceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
EP2027116A2 (en) * 2006-05-23 2009-02-25 Vertex Pharmaceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
US7615643B2 (en) 2006-06-02 2009-11-10 Smithkline Beecham Corporation Benzimidazole thiophene compounds
ATE469894T1 (de) * 2006-06-02 2010-06-15 Glaxosmithkline Llc Benzimidazol-substituierte thiophenderivate mit wirkung auf plk
AU2008275891B2 (en) 2007-07-19 2013-10-10 H.Lundbeck A/S 5-membered heterocyclic amides and related compounds
WO2010017046A1 (en) * 2008-08-05 2010-02-11 Merck & Co., Inc. Pyrazolo[1,5-a]pyridines as mark inhibitors
EP2493889B1 (en) 2009-10-30 2017-09-06 Janssen Pharmaceutica, N.V. IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS
AR080754A1 (es) 2010-03-09 2012-05-09 Janssen Pharmaceutica Nv Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10
US8933070B2 (en) 2010-07-02 2015-01-13 University Health Network Methods of targeting PTEN mutant diseases and compositions therefor
MX344600B (es) 2011-06-27 2016-12-20 Janssen Pharmaceutica Nv Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxalina.
JO3407B1 (ar) 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
HK1206250A1 (en) 2012-06-26 2016-01-08 Janssen Pharmaceutica Nv Combinations comprising pde 2 inhibitors such as 1-aryl-4-methyl-[1,2,4] triazolo [4,3-a] quinoxaline compounds and ped 10 inhibitors for use in the treatment of neurological or metabolic disorders
CN104411314B (zh) 2012-07-09 2017-10-20 詹森药业有限公司 磷酸二酯酶10的抑制剂
CN108135916B (zh) * 2015-06-19 2022-01-28 北京科辉智药生物科技有限责任公司 手性特异性含硼化合物及其在治疗癌症或淀粉样变性中的应用
WO2018081719A1 (en) * 2016-10-31 2018-05-03 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of nek2 and uses thereof
TW202210472A (zh) 2020-06-05 2022-03-16 美商奇奈特生物製藥公司 纖維母細胞生長因子受體激酶之抑制劑

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IT1255802B (it) 1992-08-07 1995-11-16 Luso Farmaco Inst Derivati imidazolici ad attivita' a ii antagonista
WO1997009325A1 (en) 1995-09-01 1997-03-13 Signal Pharmaceuticals, Inc. Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions
TR199802691T1 (xx) 1997-04-24 1999-07-21 Dow Agrosciences Llc Pestisid etkili 3-(ikameli fenil)-5-(tienil ya da furil)-1,2,4-triazoller
DE19744026A1 (de) 1997-10-06 1999-04-08 Hoechst Marion Roussel De Gmbh Pyrazol-Derivate, ihre Herstellung und ihre Verwendung in Arzneimitteln
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EP1123291B1 (en) 1998-10-23 2007-07-18 Dow Agrosciences LLC Process for preparing 3-(substituted phenyl)-5-thienyl or furyl)-1,2,4-triazoles and novel intermediates utilized therein
WO2001064646A2 (en) 2000-03-01 2001-09-07 Tularik Inc. Hydrazones and analogs as cholesterol lowering agents
US7273868B2 (en) 2000-04-28 2007-09-25 Tanabe Seiyaku Co., Ltd. Pyrazine derivatives
CN1638776A (zh) 2001-06-08 2005-07-13 西托维亚公司 取代的3-芳基-5-芳基-[1,2,4]-噁二唑和类似物
JP2005509645A (ja) 2001-10-30 2005-04-14 ファルマシア・コーポレーション 炎症処置用のヘテロ芳香族カルボキサミド誘導体
BR0304963A (pt) 2002-05-30 2004-09-28 King Pharmaceuticals Res & Dev Compostos, composição farmacêutica, e, métodos para modular a atividade de adenosina em um mamìfero, e para tratar um mamìfero sofrendo de ou suscetìvel às doenças
EP1546137A1 (en) 2002-08-08 2005-06-29 SmithKline Beecham Corporation Benzimidazol-1-yl-thiophene compounds for the treatment of cancer
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WO2007030366A1 (en) * 2005-09-06 2007-03-15 Smithkline Beecham Corporation Regioselective process for preparing benzimidazole thiophenes
WO2007087283A2 (en) 2006-01-23 2007-08-02 Vertex Pharmaceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
US7829590B2 (en) 2006-04-13 2010-11-09 Guy Brenchley Thiophene-carboxamides useful as inhibitors of protein kinases
EP2027116A2 (en) 2006-05-23 2009-02-25 Vertex Pharmaceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
US7851495B2 (en) 2006-05-23 2010-12-14 Vertex Pharmaceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases

Also Published As

Publication number Publication date
CN101400678A (zh) 2009-04-01
US7915305B2 (en) 2011-03-29
US20070219205A1 (en) 2007-09-20
US20110288095A1 (en) 2011-11-24
JP5498703B2 (ja) 2014-05-21
WO2007087283A3 (en) 2007-09-13
JP2013056942A (ja) 2013-03-28
EP2474546A1 (en) 2012-07-11
EP1989205A2 (en) 2008-11-12
AU2007208358A1 (en) 2007-08-02
JP2009523822A (ja) 2009-06-25
WO2007087283A2 (en) 2007-08-02
US8399478B2 (en) 2013-03-19
EP1989205B1 (en) 2012-06-13
US8759389B1 (en) 2014-06-24

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued

Effective date: 20160125