JP5675340B2 - 新規阻害剤 - Google Patents

新規阻害剤 Download PDF

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Publication number
JP5675340B2
JP5675340B2 JP2010503510A JP2010503510A JP5675340B2 JP 5675340 B2 JP5675340 B2 JP 5675340B2 JP 2010503510 A JP2010503510 A JP 2010503510A JP 2010503510 A JP2010503510 A JP 2010503510A JP 5675340 B2 JP5675340 B2 JP 5675340B2
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Prior art keywords
methyl
alkyl
inhibitor
imidazol
nitrovinyl
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Expired - Fee Related
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Japanese (ja)
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JP2010524893A5 (enExample
JP2010524893A (ja
Inventor
ブクフホルズ ミルコ
ブクフホルズ ミルコ
ヘイセル ウルリクフ
ヘイセル ウルリクフ
ハマンン アントジェエ
ハマンン アントジェエ
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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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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic 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
    • C07D233/56Heterocyclic 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
    • C07D233/61Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic 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
    • C07D233/64Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Anesthesiology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
JP2010503510A 2007-04-18 2008-04-18 新規阻害剤 Expired - Fee Related JP5675340B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US91253707P 2007-04-18 2007-04-18
US60/912,537 2007-04-18
PCT/EP2008/054710 WO2008128981A1 (en) 2007-04-18 2008-04-18 Nitrovinyl-diamine derivatives as glutaminyl cyclase inhibitors

Publications (3)

Publication Number Publication Date
JP2010524893A JP2010524893A (ja) 2010-07-22
JP2010524893A5 JP2010524893A5 (enExample) 2011-05-19
JP5675340B2 true JP5675340B2 (ja) 2015-02-25

Family

ID=39639570

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2010503510A Expired - Fee Related JP5675340B2 (ja) 2007-04-18 2008-04-18 新規阻害剤

Country Status (6)

Country Link
US (1) US8772508B2 (enExample)
EP (1) EP2142513B1 (enExample)
JP (1) JP5675340B2 (enExample)
DK (1) DK2142513T3 (enExample)
ES (1) ES2468551T3 (enExample)
WO (1) WO2008128981A1 (enExample)

Families Citing this family (23)

* 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
EP2142536B1 (en) * 2007-04-20 2015-10-21 Probiodrug AG Aminopyrimidine derivatives as glutaminyl cyclase inhibitors
EP2195336B1 (en) * 2007-09-12 2015-01-21 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
EP3338796A1 (en) 2008-07-21 2018-06-27 Probiodrug AG Diagnostic antibody assay
US9925282B2 (en) 2009-01-29 2018-03-27 The General Hospital Corporation Cromolyn derivatives and related methods of imaging and treatment
WO2011029920A1 (en) 2009-09-11 2011-03-17 Probiodrug Ag Heterocylcic derivatives as inhibitors of glutaminyl cyclase
US20110152341A1 (en) 2009-12-22 2011-06-23 Probiodrug Ag Cleavage of b-amyloid precursor protein
EP2533651A1 (en) 2010-02-08 2012-12-19 The Coca-Cola Company Solubility enhanced terpene glycoside(s)
JP2013519891A (ja) 2010-02-18 2013-05-30 プロビオドルグ エージー ピログルタミン酸修飾mcp−1を決定することにより炎症性疾患を診断する方法及びグルタミニルシクラーゼの阻害剤のスクリーニング方法
SG192805A1 (en) 2011-03-16 2013-09-30 Probiodrug Ag Diagnostic antibody assay
CA2889446C (en) 2012-10-25 2021-05-11 The General Hospital Corporation Combination therapies for the treatment of alzheimer's disease and related disorders
US10525005B2 (en) 2013-05-23 2020-01-07 The General Hospital Corporation Cromolyn compositions and methods thereof
AU2014340182B2 (en) 2013-10-22 2019-05-23 The General Hospital Corporation Cromolyn derivatives and related methods of imaging and treatment
JP2018501482A (ja) 2014-12-19 2018-01-18 プロビオドルグ エージー pGlu−Abetaペプチドの検出のための新規の方法
WO2017064302A1 (en) * 2015-10-16 2017-04-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of autoimmune inflammatory diseases
JP2019524865A (ja) 2016-08-31 2019-09-05 ザ ジェネラル ホスピタル コーポレイション 神経変性疾患と関連する神経炎症におけるマクロファージ/ミクログリア
KR20210070232A (ko) 2017-07-20 2021-06-14 아즈테라피즈 인코포레이티드 크로몰린 나트륨 및 이부프로펜의 분말화된 제형
EP3461819B1 (en) 2017-09-29 2020-05-27 Probiodrug AG Inhibitors of glutaminyl cyclase
EP3521308B1 (en) 2018-01-31 2024-03-13 Vivoryon Therapeutics N.V. Humanized and de-immunized antibodies
CN113038944A (zh) 2018-07-02 2021-06-25 通用医疗公司 色甘酸钠和α-乳糖的粉末化制剂
AU2019397436A1 (en) 2018-12-10 2021-07-22 The General Hospital Corporation Cromolyn esters and uses thereof
IL297023A (en) 2020-04-06 2022-12-01 Massachusetts Gen Hospital Methods for treating inflammatory conditions caused by the corona virus

Family Cites Families (19)

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Publication number Priority date Publication date Assignee Title
US4277485A (en) * 1973-05-17 1981-07-07 Smith Kline & French Laboratories Limited Oxazole or isoxazole alkylamino ethylene compounds as inhibitors of H-2 histamine receptors
DE3044566A1 (de) * 1980-11-26 1982-07-15 Basf Ag, 6700 Ludwigshafen N-substituierte imidazol-derivate, ihre herstellung, diese enthaltende arzneimittel und ihre verwendung
AU2001241194A1 (en) 2000-03-21 2001-10-03 Ishihara Sangyo Kaisha Ltd. Nitroethenamine derivatives or salts thereof and pharmaceutical compositions containing the derivatives or the salts
US6948038B2 (en) 2001-07-24 2005-09-20 Microsoft Corporation System and method for backing up and restoring data
KR20110059664A (ko) 2003-05-05 2011-06-02 프로비오드룩 아게 글루타미닐 및 글루타메이트 사이클라제의 이펙터의 용도
US8338120B2 (en) 2003-05-05 2012-12-25 Probiodrug Ag Method of treating inflammation with glutaminyl cyclase inhibitors
WO2004098591A2 (en) * 2003-05-05 2004-11-18 Probiodrug Ag Inhibitors of glutaminyl cyclase and their use in the treatment of neurological diseases
US7732162B2 (en) 2003-05-05 2010-06-08 Probiodrug Ag Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases
EP2289498A1 (en) 2003-10-15 2011-03-02 Probiodrug AG Use of inhibitors of glutaminyl clyclase
US7667044B2 (en) 2003-11-03 2010-02-23 Probiodrug Ag Compounds for the treatment of neurological disorders
EP1680120A2 (en) 2003-11-03 2006-07-19 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
EP1713780B1 (en) 2004-02-05 2012-01-18 Probiodrug AG Novel inhibitors of glutaminyl cyclase
EP2581449B1 (en) 2006-09-21 2016-09-14 Probiodrug AG Novel genes related to glutaminyl cyclase
WO2008055950A1 (en) 2006-11-09 2008-05-15 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
US8420684B2 (en) 2006-11-09 2013-04-16 Probiodrug Ag Inhibitors of glutaminyl cyclase
EP2091948B1 (en) 2006-11-30 2012-04-18 Probiodrug AG Novel inhibitors of glutaminyl cyclase
JP2010516235A (ja) 2007-01-19 2010-05-20 プロビオドルグ エージー アルツハイマー病及び他のqpct関連障害の治療のためのインビボスクリーニングモデル
DK2118101T3 (da) 2007-03-09 2013-01-02 Probiodrug Ag IMIDAZO (1,5-A)-PYRIDinderivater som glutaminylcyclaseinhibitorer

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Publication number Publication date
DK2142513T3 (da) 2014-06-10
US8772508B2 (en) 2014-07-08
EP2142513A1 (en) 2010-01-13
EP2142513B1 (en) 2014-03-12
WO2008128981A1 (en) 2008-10-30
JP2010524893A (ja) 2010-07-22
ES2468551T3 (es) 2014-06-16
US20080292582A1 (en) 2008-11-27

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