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

Zubereitung von 1,6-disubstituierten azabenzimidazolen als kinasehemmer

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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

Landscapes

  • 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)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Vascular Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Psychology (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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AR045134A1 (es) * 2003-07-29 2005-10-19 Smithkline Beecham Plc Compuesto de 1h - imidazo [4,5-c] piridin-ilo, composicion farmaceutica que lo comprende, proceso para prepararla, su uso para preparar dicha composicion farmaceutica, combinacion farmaceutica, uso de la combinacion farmaceutica para la preparacion de un medicamento, procedimientos para preparar dic
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
TW200716110A (en) * 2005-04-20 2007-05-01 Smithkline Beecham Corp Inhibitors of AKT activity
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
PL1905452T3 (pl) 2005-07-12 2013-11-29 Kowa Co Środek do zapobiegania lub leczenia jaskry
US7625890B2 (en) 2005-11-10 2009-12-01 Smithkline Beecham Corp. Substituted imidazo[4,5-c]pyridine compounds as Akt inhibitors
KR20180031066A (ko) 2007-08-29 2018-03-27 센주 세이야꾸 가부시키가이샤 각막 내피 세포 접착 촉진제
WO2009126635A1 (en) * 2008-04-09 2009-10-15 Abbott Laboratories 2-amino-benzothiazole derivates 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
CA3178138A1 (en) 2011-12-06 2013-06-13 Astellas Institute For Regenerative Medicine Method of directed differentiation producing corneal endothelial cells, compositions thereof, and uses thereof
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
EP2799537B1 (de) 2011-12-28 2021-09-22 Kyoto Prefectural Public University Corporation Normalisierung der züchtung von hornhautendothelzellen
EP3181564B1 (de) 2012-11-20 2019-09-18 H. Hoffnabb-La Roche Ag Aminopyrimidinverbindungen als inhibitoren von t790m-haltigen egfr-mutanten
WO2015016371A1 (ja) 2013-07-30 2015-02-05 京都府公立大学法人 角膜内皮細胞マーカー
WO2015064768A1 (ja) 2013-10-31 2015-05-07 京都府公立大学法人 角膜内皮の小胞体細胞死関連疾患治療薬
JP6470286B2 (ja) 2013-11-27 2019-02-13 京都府公立大学法人 ラミニンの角膜内皮細胞培養への応用
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
JP7008337B2 (ja) 2016-02-15 2022-02-10 京都府公立大学法人 ヒト機能性角膜内皮細胞およびその応用
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
CN114921468A (zh) * 2017-01-30 2022-08-19 国立大学法人京都大学 新型化合物以及调节性t细胞的制造方法
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
AU2019352309A1 (en) 2018-10-02 2021-03-11 The Doshisha Method and vessel for preserving corneal endothelial cells
EP3747868A1 (de) * 2019-06-04 2020-12-09 Bayer AG Substituierte phenoxypyridine sowie deren salze und ihre verwendung als herbizide wirkstoffe
UY38912A (es) * 2019-10-09 2021-05-31 Biocryst Pharm Inc Inhibidores del factor d del complemento para administración oral
US20230257700A1 (en) 2020-02-27 2023-08-17 Kyoto Prefectural Public University Corporation Functional human corneal endothelial cells and application thereof
JP7361431B2 (ja) 2020-10-22 2023-10-16 京都府公立大学法人 ヒト角膜内皮細胞及び／又はヒト角膜内皮前駆細胞の保存方法
CA3216719A1 (en) 2021-05-03 2022-11-10 Astellas Institute For Regenerative Medicine Methods of generating mature corneal endothelial cells
US20250000083A1 (en) 2021-11-11 2025-01-02 The Doshisha Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation
US20260097083A1 (en) 2022-09-26 2026-04-09 Kyoto University Method for producing pancreatic endoderm cells
CN121605186A (zh) 2023-05-19 2026-03-03 国立大学法人京都大学 神经嵴细胞的制造方法
WO2025017499A1 (en) 2023-07-17 2025-01-23 Graviton Bioscience Bv Formulations and uses of rock2 inhibitors for als
JPWO2025037497A1 (de) 2023-08-15 2025-02-20
AU2024352423A1 (en) 2023-09-28 2026-05-14 Graviton Pharmaceuticals B.V. Therapy for treating type 1 diabetes using rock2 and dyrk1 inhibitors
WO2025069009A1 (en) 2023-09-29 2025-04-03 Graviton Bioscience Bv Rock2 inhibitors in the treatment of obesity

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
JP4329003B2 (ja) * 2001-03-23 2009-09-09 バイエル コーポレイション Ｒｈｏキナーゼ阻害剤
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
ES2387780T3 (es) 2012-10-01
WO2005037197A2 (en) 2005-04-28
WO2005037197A3 (en) 2005-06-02
JP4764823B2 (ja) 2011-09-07
US20080234261A1 (en) 2008-09-25
EP1675552B1 (de) 2012-04-11
EP1675552A4 (de) 2009-06-03
US7547779B2 (en) 2009-06-16
EP1675552A2 (de) 2006-07-05
JP2007507546A (ja) 2007-03-29

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