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

Landscapes

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

Families Citing this family (35)

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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
PE20061378A1 (es) * 2005-04-20 2006-12-03 Smithkline Beecham Corp INHIBIDORES DE LA ACTIVIDAD DE Akt
TW200726765A (en) 2005-06-17 2007-07-16 Bristol Myers Squibb Co Triazolopyridine cannabinoid receptor 1 antagonists
EP1902731B1 (de) 2005-06-21 2013-04-10 Kowa Company, Ltd. Mittel zur prävention oder heilmittel für glaukom
EP1905452B1 (de) 2005-07-12 2013-06-19 Kowa Company, Ltd. Wirkstoff zur prävention oder behandlung von glaukomen
US7625890B2 (en) 2005-11-10 2009-12-01 Smithkline Beecham Corp. Substituted imidazo[4,5-c]pyridine compounds as Akt inhibitors
KR20220151013A (ko) 2007-08-29 2022-11-11 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
PL2788472T3 (pl) 2011-12-06 2019-06-28 Astellas Institute For Regenerative Medicine Sposób ukierunkowanego różnicowania z wytwarzaniem komórek śródbłonka rogówki
ES2917222T3 (es) 2011-12-28 2022-07-07 Kyoto Prefectural Public Univ Corp Normalización del cultivo de células endoteliales de la córnea
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
WO2014081718A1 (en) 2012-11-20 2014-05-30 Genentech, Inc. Aminopyrimidine compounds as inhibitors of t790m containing egfr mutants
EP3029140A4 (de) 2013-07-30 2017-06-28 Kyoto Prefectural Public University Corporation Hornhautendothel-zellmarker
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
ES2763433T3 (es) 2013-11-27 2020-05-28 Kyoto Prefectural Public Univ Corp Aplicación de laminina a cultivos de células endoteliales de la córnea
US10472610B2 (en) 2014-05-21 2019-11-12 Kyoto University Method for generating pancreatic bud cells and therapeutic agent for pancreatic disease containing pancreatic bud cells
EP4218773A1 (de) 2016-02-15 2023-08-02 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
EP3575297B1 (de) * 2017-01-30 2024-12-18 Kyoto University Neuartige verbindung und verfahren zur herstellung von regulatorischen t-zellen
CN113056556A (zh) 2018-08-31 2021-06-29 学校法人同志社 用于对眼细胞进行保存或培养的组合物以及方法
WO2020071438A1 (ja) 2018-10-02 2020-04-09 学校法人同志社 角膜内皮細胞を保存するための方法および容器
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
CA3173725A1 (en) 2020-02-27 2021-09-02 Kyoto Prefectural Public University Corporation Functional human corneal endothelial cells and application thereof
WO2022085680A1 (ja) 2020-10-22 2022-04-28 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
MX2023013079A (es) 2021-05-03 2023-11-16 Astellas Inst For Regenerative Medicine Metodos de generacion de celulas maduras del endotelio corneal.
AU2022385051A1 (en) 2021-11-11 2024-06-20 Actualeyes Inc. Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation
CN119948151A (zh) 2022-09-26 2025-05-06 国立大学法人京都大学 胰腺内胚层细胞的制造方法
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
WO2025069008A1 (en) 2023-09-28 2025-04-03 Graviton Bioscience Bv 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

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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
TWI261055B (en) * 2001-03-23 2006-09-01 Bayer Corp Rho-Kinase Inhibitors
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
JP2007507547A (ja) * 2003-10-06 2007-03-29 グラクソ　グループ　リミテッド キナーゼ阻害剤としての１，７−二置換アザベンゾイミダゾールの調製

Also Published As

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

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