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

    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (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 (cg-RX-API-DMAC10.html)
EP (2) EP2474546A1 (cg-RX-API-DMAC10.html)
JP (2) JP5498703B2 (cg-RX-API-DMAC10.html)
CN (1) CN101400678A (cg-RX-API-DMAC10.html)
AU (1) AU2007208358A1 (cg-RX-API-DMAC10.html)
CA (1) CA2637335A1 (cg-RX-API-DMAC10.html)
WO (1) WO2007087283A2 (cg-RX-API-DMAC10.html)

Families Citing this family (19)

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MX2008003173A (es) 2005-09-06 2008-03-18 Smithkline Beecham Corp Compuestos de bencimidazol-tiofeno como inhibidores de plk.
EP2474546A1 (en) 2006-01-23 2012-07-11 Vertex Pharmaceuticals Inc. Thiophene-carboxamides useful as inhibitors of protein kinases
EP2007757B1 (en) * 2006-04-13 2012-10-03 Vertex Pharmceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
CA2652816A1 (en) * 2006-05-23 2007-12-06 Vertex Pharmaceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
JP2009538305A (ja) * 2006-05-23 2009-11-05 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 プロテインキナーゼのインヒビターとして有用なチオフェンカルボキサミド
PE20080710A1 (es) * 2006-06-02 2008-08-07 Smithkline Beecham Corp Compuestos de tiofeno de bencimidazol
US7615643B2 (en) 2006-06-02 2009-11-10 Smithkline Beecham Corporation Benzimidazole thiophene compounds
CN101711245B (zh) 2007-07-19 2015-03-25 H.隆德贝克有限公司 5元杂环酰胺及相关的化合物
WO2010017046A1 (en) 2008-08-05 2010-02-11 Merck & Co., Inc. Pyrazolo[1,5-a]pyridines as mark inhibitors
PH12012500778A1 (en) 2009-10-30 2012-11-26 Janssen Pharmaceutica Nv 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
CA2803446C (en) 2010-07-02 2019-06-04 University Health Network Use of plk4 antagonists for treating pten mutant diseases
JP6115962B2 (ja) 2011-06-27 2017-04-19 ヤンセン ファーマシューティカ エヌ.ベー. 1−アリール−4−メチル−[1,2,4]トリアゾロ[4,3−a]キノキサリン誘導体
JO3407B1 (ar) 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
WO2014001314A1 (en) 2012-06-26 2014-01-03 Janssen Pharmaceutica Nv Combinations comprising pde 2 inhibitors such as 1-aryl-4-methyl- [1,2,4] triazolo [4,3-a] quinoxaline compounds and pde 10 inhibitors for use in the treatment of neurological or metabolic disorders
AU2013289284B2 (en) 2012-07-09 2017-03-30 Janssen Pharmaceutica Nv Inhibitors of phosphodiesterase 10 enzyme
EP3310360B1 (en) * 2015-06-19 2024-03-27 Beijing Artivila BioPharma Co. Ltd. Chiral specific boron-containing compounds and their use in treating cancer or amyloidosis
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
CN116057045B (zh) 2020-06-05 2026-06-09 金耐特生物制药公司 成纤维细胞生长因子受体激酶抑制剂

Family Cites Families (27)

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IT1255802B (it) 1992-08-07 1995-11-16 Luso Farmaco Inst Derivati imidazolici ad attivita' a ii antagonista
AU726058B2 (en) 1995-09-01 2000-10-26 Signal Pharmaceuticals, Inc. Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions
EP0922043B1 (en) 1997-04-24 2002-01-30 Dow AgroSciences LLC Pesticidal 3-(substituted phenyl)-5-(thienyl or furyl)-1,2,4-triazoles
DE19744026A1 (de) 1997-10-06 1999-04-08 Hoechst Marion Roussel De Gmbh Pyrazol-Derivate, ihre Herstellung und ihre Verwendung in Arzneimitteln
PT957099E (pt) 1998-04-15 2003-02-28 Pfizer Prod Inc Carboxamidas heterociclicas
CN1136218C (zh) 1998-10-23 2004-01-28 道农业科学公司 制备3-(取代的苯基)-5-(噻吩基或呋喃基)-1,2,4-三唑的方法以及在其中使用的新中间体
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US7514448B2 (en) * 2004-04-02 2009-04-07 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of rock and other protein kinases
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EP1924572B1 (en) * 2005-09-06 2009-12-30 SmithKline Beecham Corporation Regioselective process for preparing benzimidazole thiophenes
EP2474546A1 (en) 2006-01-23 2012-07-11 Vertex Pharmaceuticals Inc. Thiophene-carboxamides useful as inhibitors of protein kinases
EP2007757B1 (en) 2006-04-13 2012-10-03 Vertex Pharmceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
JP2009538305A (ja) 2006-05-23 2009-11-05 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 プロテインキナーゼのインヒビターとして有用なチオフェンカルボキサミド
CA2652816A1 (en) 2006-05-23 2007-12-06 Vertex Pharmaceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases

Also Published As

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

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Legal Events

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EEER Examination request
FZDE Discontinued

Effective date: 20160125