JP5675343B2 - グルタミニルシクラーゼ阻害剤としての尿素誘導体 - Google Patents

グルタミニルシクラーゼ阻害剤としての尿素誘導体 Download PDF

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JP5675343B2
JP5675343B2 JP2010503515A JP2010503515A JP5675343B2 JP 5675343 B2 JP5675343 B2 JP 5675343B2 JP 2010503515 A JP2010503515 A JP 2010503515A JP 2010503515 A JP2010503515 A JP 2010503515A JP 5675343 B2 JP5675343 B2 JP 5675343B2
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alkyl
inhibitor
phenyl
optionally substituted
methyl
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JP2010524898A5 (enExample
JP2010524898A (ja
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ブクフホルズ ミルコ
ブクフホルズ ミルコ
ジェイ.ニエストロジェ アンドレ
ジェイ.ニエストロジェ アンドレ
ヘイセル ウルリクフ
ヘイセル ウルリクフ
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プロビオドルグ エージー
プロビオドルグ エージー
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • 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
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • 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
    • 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
    • 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
    • A61P9/10—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C07D233/61—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Anesthesiology (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2010503515A 2007-04-18 2008-04-18 グルタミニルシクラーゼ阻害剤としての尿素誘導体 Expired - Fee Related JP5675343B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US91252507P 2007-04-18 2007-04-18
US60/912,525 2007-04-18
PCT/EP2008/054716 WO2008128986A1 (en) 2007-04-18 2008-04-18 Urea derivatives as glutaminyl cyclase inhibitors

Publications (3)

Publication Number Publication Date
JP2010524898A JP2010524898A (ja) 2010-07-22
JP2010524898A5 JP2010524898A5 (enExample) 2011-05-26
JP5675343B2 true JP5675343B2 (ja) 2015-02-25

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JP2010503515A Expired - Fee Related JP5675343B2 (ja) 2007-04-18 2008-04-18 グルタミニルシクラーゼ阻害剤としての尿素誘導体

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Country Link
US (1) US9512082B2 (enExample)
EP (1) EP2146968B1 (enExample)
JP (1) JP5675343B2 (enExample)
WO (1) WO2008128986A1 (enExample)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7732162B2 (en) * 2003-05-05 2010-06-08 Probiodrug Ag Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases
JP5676249B2 (ja) * 2007-04-20 2015-02-25 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのアミノピリジン誘導体
AU2008297070A1 (en) * 2007-09-12 2009-03-19 Probiodrug Ag Transgenic mice
WO2009090190A1 (en) * 2008-01-14 2009-07-23 Probiodrug Ag Mouse models carrying a knock-out mutation of the glutaminyl cyclase gene
KR101706789B1 (ko) 2008-07-21 2017-02-14 프로비오드룩 아게 진단용 항체 검사법
PL2475428T3 (pl) 2009-09-11 2015-12-31 Probiodrug Ag Pochodne heterocykliczne jako inhibitory cyklazy glutaminowej
WO2011076854A1 (en) 2009-12-22 2011-06-30 Probiodrug Ag CLEAVAGE OF β-AMYLOID PRECURSOR PROTEIN
EP2537029A1 (en) 2010-02-18 2012-12-26 Probiodrug AG Methods of diagnosing inflammatory diseases by determining pyroglutamate-modified mcp-1 and screening methods for inhibitors of glutaminyl cyclase
CN103459421B (zh) 2011-03-16 2017-07-14 前体生物药物股份公司 诊断性抗体测定
WO2014113495A1 (en) * 2013-01-15 2014-07-24 The Trustees Of Columbia University In The City Of New York Activation or reactivation of ache
US20170363645A1 (en) 2014-12-19 2017-12-21 Probiodrug Ag Novel Method for the Detection of pGlu-Abeta Peptides
EP3135709B1 (en) * 2015-08-31 2018-01-10 ATOTECH Deutschland GmbH Imidazoyl urea polymers and their use in metal or metal alloy plating bath compositions
GB201705263D0 (en) * 2017-03-31 2017-05-17 Probiodrug Ag Novel inhibitors
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
EP3521308B1 (en) 2018-01-31 2024-03-13 Vivoryon Therapeutics N.V. Humanized and de-immunized antibodies
CN109734677A (zh) * 2019-03-07 2019-05-10 四川大学 抑制组蛋白赖氨酸甲基转移酶nsd2的小分子化合物及其应用
KR102230832B1 (ko) * 2019-06-17 2021-03-24 (주) 메디프론디비티 N-치환된 티오우레아 또는 우레아 유도체 및 이를 유효성분으로 함유하는 글루타미닐 사이클레이즈 활성 관련 질환의 예방 또는 치료용 약학적 조성물
TR2023016729A2 (tr) * 2023-12-07 2025-06-23 Bogazici Ueniversitesi Alzhei̇mer hastaliğinin tedavi̇si̇ne yöneli̇k bi̇leşi̇kler ve bu bi̇leşi̇kleri̇n elde edi̇lme yöntemi̇
CN119954726B (zh) * 2025-02-08 2025-12-05 平原实验室 芳基脲-咪唑盐类化合物及其合成方法和抗肿瘤活性

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US4576957A (en) * 1984-07-05 1986-03-18 American Cyanamid Company N-(Substituted phenyl)-N'-[(1H-imidazol-1-yl) and (1H-1,2,4-triazol-1-yl)alkyl]ureas
JPH0275676A (ja) * 1988-09-12 1990-03-15 Mitsubishi Petrochem Co Ltd 熱硬化性エポキシ樹脂ワニス
EP0386931A1 (en) * 1989-03-04 1990-09-12 Konica Corporation A novel cyan coupler
GB9823873D0 (en) 1998-10-30 1998-12-30 Pharmacia & Upjohn Spa 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents
JP2000290260A (ja) 1999-04-01 2000-10-17 Shikoku Chem Corp 新規イミダゾール化合物およびイミダゾール化合物を有効成分とするエポキシ樹脂硬化剤
US6387900B1 (en) * 1999-08-12 2002-05-14 Pharmacia & Upjohn S.P.A. 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents
DE60208630T2 (de) * 2001-05-11 2006-08-17 Pfizer Products Inc., Groton Thiazolderivate und ihre Verwendung als cdk-Inhibitoren
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JP2003192587A (ja) * 2001-12-26 2003-07-09 Bayer Ag 尿素誘導体
US8338120B2 (en) 2003-05-05 2012-12-25 Probiodrug Ag Method of treating inflammation with glutaminyl cyclase inhibitors
EP1620091B1 (en) 2003-05-05 2010-03-31 Probiodrug AG Inhibitors of glutaminyl cyclase
US7732162B2 (en) 2003-05-05 2010-06-08 Probiodrug Ag Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases
KR20060009902A (ko) 2003-05-05 2006-02-01 프로비오드룩 아게 글루타미닐 및 글루타메이트 사이클라제의 이펙터의 용도
AU2004283461B2 (en) 2003-10-15 2010-02-11 Probiodrug Ag Use of effectors of glutaminyl and glutamate cyclases
AU2004290499C1 (en) 2003-11-03 2011-02-24 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
US20050171112A1 (en) 2003-11-03 2005-08-04 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
US7667044B2 (en) 2003-11-03 2010-02-23 Probiodrug Ag Compounds for the treatment of neurological disorders
WO2005075436A2 (en) 2004-02-05 2005-08-18 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
AR059826A1 (es) * 2006-03-13 2008-04-30 Univ California Inhibidores de urea conformacionalmente restringidos de epoxido hidrolasa soluble
WO2008034891A2 (en) 2006-09-21 2008-03-27 Probiodrug Ag Novel genes related to glutaminyl cyclase
JP5599614B2 (ja) 2006-11-09 2014-10-01 プロビオドルグ エージー グルタミニルシクラーゼの新規阻害剤
US8420684B2 (en) 2006-11-09 2013-04-16 Probiodrug Ag Inhibitors of glutaminyl cyclase
ATE554085T1 (de) 2006-11-30 2012-05-15 Probiodrug Ag Neue inhibitoren von glutaminylcyclase
EP2395095A1 (en) 2007-01-19 2011-12-14 Probiodrug AG In vivo screening models for treatment of Alzheimer's disease and other QPCT-related disorders
WO2008110523A1 (en) 2007-03-09 2008-09-18 Probiodrug Ag Imidazo [1,5-a] pyridine derivatives as inhibitors of glutaminyl cyclase

Also Published As

Publication number Publication date
EP2146968B1 (en) 2015-09-23
EP2146968A1 (en) 2010-01-27
US20080262063A1 (en) 2008-10-23
US9512082B2 (en) 2016-12-06
JP2010524898A (ja) 2010-07-22
WO2008128986A1 (en) 2008-10-30

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