ATE552834T1 - Zubereitung von 1,6-disubstituierten azabenzimidazolen als kinasehemmer - Google Patents

Zubereitung von 1,6-disubstituierten azabenzimidazolen als kinasehemmer

Info

Publication number
ATE552834T1
ATE552834T1 AT04794238T AT04794238T ATE552834T1 AT E552834 T1 ATE552834 T1 AT E552834T1 AT 04794238 T AT04794238 T AT 04794238T AT 04794238 T AT04794238 T AT 04794238T AT E552834 T1 ATE552834 T1 AT E552834T1
Authority
AT
Austria
Prior art keywords
azabenzimidazoles
disubstituted
preparation
kinase inhibitor
rho
Prior art date
Application number
AT04794238T
Other languages
English (en)
Inventor
Dennis Lee
Robert Stavenger
Krista Goodman
Mark Hilfiker
Haifeng Cui
Andrew Viet
Original Assignee
Glaxosmithkline Llc
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 Glaxosmithkline Llc filed Critical Glaxosmithkline Llc
Application granted granted Critical
Publication of ATE552834T1 publication Critical patent/ATE552834T1/de

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    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Vascular Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
AT04794238T 2003-10-06 2004-10-06 Zubereitung von 1,6-disubstituierten azabenzimidazolen als kinasehemmer ATE552834T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US50889403P 2003-10-06 2003-10-06
US53194903P 2003-12-23 2003-12-23
PCT/US2004/032824 WO2005037197A2 (en) 2003-10-06 2004-10-06 Preperation of 1,6-disubstituted azabenzimidazoles as kinase inhibitors

Publications (1)

Publication Number Publication Date
ATE552834T1 true ATE552834T1 (de) 2012-04-15

Family

ID=34467951

Family Applications (1)

Application Number Title Priority Date Filing Date
AT04794238T ATE552834T1 (de) 2003-10-06 2004-10-06 Zubereitung von 1,6-disubstituierten azabenzimidazolen als kinasehemmer

Country Status (6)

Country Link
US (1) US7547779B2 (de)
EP (1) EP1675552B1 (de)
JP (1) JP4764823B2 (de)
AT (1) ATE552834T1 (de)
ES (1) ES2387780T3 (de)
WO (1) WO2005037197A2 (de)

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TW200523262A (en) * 2003-07-29 2005-07-16 Smithkline Beecham Corp Inhibitors of AKT activity
WO2005118543A1 (ja) * 2004-06-03 2005-12-15 Ono Pharmaceutical Co., Ltd. キナーゼ阻害薬およびその用途
AR053364A1 (es) * 2005-04-20 2007-05-02 Smithkline Beecham Compuesto de 1h-imidazo 84,5-c) piridin -2- ilo, composicion farmaceutica que lo comprende, proceso para prepararla y su uso para preparar un medicamento para tratamiento de cancer o artritis
TW200726765A (en) 2005-06-17 2007-07-16 Bristol Myers Squibb Co Triazolopyridine cannabinoid receptor 1 antagonists
JP4972551B2 (ja) 2005-06-21 2012-07-11 興和株式会社 緑内障の予防又は治療剤
PT1905452E (pt) 2005-07-12 2013-07-16 Kowa Co Agente para a prevenção ou tratamento do glaucoma
US7625890B2 (en) 2005-11-10 2009-12-01 Smithkline Beecham Corp. Substituted imidazo[4,5-c]pyridine compounds as Akt inhibitors
KR20240045364A (ko) 2007-08-29 2024-04-05 센주 세이야꾸 가부시키가이샤 각막 내피 세포 접착 촉진제
US20090258907A1 (en) * 2008-04-09 2009-10-15 Abbott Laboratories Compounds useful as inhibitors of rock kinases
US8232409B2 (en) 2008-10-15 2012-07-31 Janssen Pharmaceutica N.V. Heterocyclic benzimidazoles as TRPM8 modulators
GB201104267D0 (en) * 2011-03-14 2011-04-27 Cancer Rec Tech Ltd Pyrrolopyridineamino derivatives
TR201903889T4 (tr) 2011-12-06 2019-04-22 Astellas Inst For Regenerative Medicine Korneal endotelyal hücreler üreten yönlendirilmiş diferansiyasyona yönelik yöntem.
US20150044178A1 (en) 2011-12-28 2015-02-12 Kyoto Prefectural Public University Corporation Normalization of culture of corneal endothelial cells
CN102558041A (zh) * 2011-12-28 2012-07-11 合肥科尚医药科技有限公司 一种3，4-二氨基-6-溴吡啶的制备方法
EP3181564B1 (de) * 2012-11-20 2019-09-18 H. Hoffnabb-La Roche Ag Aminopyrimidinverbindungen als inhibitoren von t790m-haltigen egfr-mutanten
US10908161B2 (en) 2013-07-30 2021-02-02 Kyoto Prefectural Public University Corporation Corneal endothelial cell marker
CA2927898C (en) 2013-10-31 2021-11-16 Kyoto Prefectural Public University Corporation Therapeutic drug for diseases related to endoplasmic reticulum cell death in corneal endothelium
BR112016011096A2 (pt) 2013-11-27 2017-09-19 Kyoto Prefectural Public Univ Corp Aplicação de laminina à cultura de célula endotelial da córnea
CN106536718B (zh) 2014-05-21 2021-04-27 国立大学法人京都大学 胰芽细胞的制造方法及含有胰芽细胞的胰疾病治疗剂
EP3416658B1 (de) 2016-02-15 2023-03-22 Kyoto Prefectural Public University Corporation Menschliche funktionelle hornhautendothelzelle und anwendung davon
CN105924390B (zh) * 2016-05-19 2018-07-10 广州南新制药有限公司 一种美他非尼的合成方法
JP7142846B2 (ja) * 2017-01-30 2022-09-28 国立大学法人京都大学 新規化合物及び制御性ｔ細胞の製造方法
JPWO2020045642A1 (ja) 2018-08-31 2021-08-12 学校法人同志社 眼細胞を保存または培養するための組成物および方法
CN113015429A (zh) 2018-10-02 2021-06-22 学校法人同志社 用于保存角膜内皮细胞的方法和容器
EP3747868A1 (de) * 2019-06-04 2020-12-09 Bayer AG Substituierte phenoxypyridine sowie deren salze und ihre verwendung als herbizide wirkstoffe
TWI908740B (zh) * 2019-10-09 2025-12-21 美商百歐克斯製藥公司 口服補體因子d抑制劑
US20230257700A1 (en) 2020-02-27 2023-08-17 Kyoto Prefectural Public University Corporation Functional human corneal endothelial cells and application thereof
EP4234682A4 (de) 2020-10-22 2024-11-27 Kyoto Prefectural Public University Corporation Konservierungsverfahren für menschliche hornhautendothelzellen und/oder menschliche hornhautendothelvorläuferzellen
AU2022270611A1 (en) 2021-05-03 2023-10-12 Astellas Institute For Regenerative Medicine Methods of generating mature corneal endothelial cells
CA3238227A1 (en) 2021-11-11 2023-05-19 The Doshisha Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation
EP4596675A4 (de) 2022-09-26 2026-03-11 Univ Kyoto Verfahren zur herstellung pankreatischer endodermzellen
WO2024242069A1 (ja) 2023-05-19 2024-11-28 国立大学法人京都大学 神経堤細胞の製造方法
AU2024292342A1 (en) 2023-07-17 2026-02-26 Graviton Bioscience Bv Formulations and uses of rock2 inhibitors for als
EP4763975A1 (de) 2023-08-15 2026-06-24 Kyoto University Verfahren zur herstellung von dünndarmgewebe
IL327381A (en) 2023-09-28 2026-05-01 Graviton Pharmaceuticals B V Treatment for type 1 diabetes using ROCK2 and DYRK1 inhibitors
IL327385A (en) 2023-09-29 2026-05-01 Graviton Pharmaceuticals B V ROCK2 inhibitors in the treatment of obesity
WO2026128800A1 (en) 2024-12-13 2026-06-18 Aurion Biotech, Inc. Stable corneal endothelial cell (cec) compositions and methods of use
US20260166089A1 (en) 2024-12-17 2026-06-18 Aurion Biotech, Inc. Treatment of corneal endothelial disease
WO2026156530A1 (en) 2025-01-22 2026-07-30 Bayer Consumer Care Ag New chemical process for the production of 4- (4-fluoro-2-methyl-phenyl) -5-nitro-1h-pyridin-2-one, a key intermediate of elinzanetant

Family Cites Families (5)

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DE3722992A1 (de) * 1987-07-11 1989-01-19 Thomae Gmbh Dr K Neue imidazo-pyridine und purine, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
HN2002000067A (es) * 2001-03-23 2003-10-24 Bayer Healthcare Llc Inhibidores de la rho - quinasa.
FR2831536A1 (fr) * 2001-10-26 2003-05-02 Aventis Pharma Sa Nouveaux derives de benzimidazoles, leur procede de preparation, leur application a titre de medicament, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de kdr
GB0206860D0 (en) * 2002-03-22 2002-05-01 Glaxo Group Ltd Compounds
WO2005037198A2 (en) * 2003-10-06 2005-04-28 Glaxo Group Limited Preparation of 1,7-disubstituted azabenzimidazoles as kinase inhibitors

Also Published As

Publication number Publication date
JP2007507546A (ja) 2007-03-29
EP1675552B1 (de) 2012-04-11
US20080234261A1 (en) 2008-09-25
EP1675552A4 (de) 2009-06-03
EP1675552A2 (de) 2006-07-05
ES2387780T3 (es) 2012-10-01
JP4764823B2 (ja) 2011-09-07
WO2005037197A3 (en) 2005-06-02
WO2005037197A2 (en) 2005-04-28
US7547779B2 (en) 2009-06-16

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