JP5676249B2 - 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 - Google Patents

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

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Publication number
JP5676249B2
JP5676249B2 JP2010503513A JP2010503513A JP5676249B2 JP 5676249 B2 JP5676249 B2 JP 5676249B2 JP 2010503513 A JP2010503513 A JP 2010503513A JP 2010503513 A JP2010503513 A JP 2010503513A JP 5676249 B2 JP5676249 B2 JP 5676249B2
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Prior art keywords
imidazol
propyl
alkyl
pyridinyl
phenyl
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Expired - Fee Related
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JP2010524896A (ja
JP2010524896A5 (cg-RX-API-DMAC7.html
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
ソムメル ロベルト
ソムメル ロベルト
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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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P25/14—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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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 three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Dermatology (AREA)
  • Anesthesiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pain & Pain Management (AREA)
JP2010503513A 2007-04-20 2008-04-18 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 Expired - Fee Related JP5676249B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US91294207P 2007-04-20 2007-04-20
US60/912,942 2007-04-20
PCT/EP2008/054714 WO2008128984A1 (en) 2007-04-20 2008-04-18 Aminopyrimidine derivatives as glutaminyl cyclase inhibitors

Publications (3)

Publication Number Publication Date
JP2010524896A JP2010524896A (ja) 2010-07-22
JP2010524896A5 JP2010524896A5 (cg-RX-API-DMAC7.html) 2011-06-02
JP5676249B2 true JP5676249B2 (ja) 2015-02-25

Family

ID=39687042

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2010503513A Expired - Fee Related JP5676249B2 (ja) 2007-04-20 2008-04-18 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

Country Status (4)

Country Link
US (1) US8188094B2 (cg-RX-API-DMAC7.html)
EP (1) EP2142536B1 (cg-RX-API-DMAC7.html)
JP (1) JP5676249B2 (cg-RX-API-DMAC7.html)
WO (1) WO2008128984A1 (cg-RX-API-DMAC7.html)

Families Citing this family (21)

* 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
BRPI0718507A2 (pt) * 2006-09-21 2013-11-12 Probiodrug Ag Genes relacionados à glutaminil ciclase
US9277737B2 (en) 2006-09-21 2016-03-08 Probiodrug Ag Mouse models carrying a knock-out mutation of the QPCTL-gene
US8889709B2 (en) * 2006-09-21 2014-11-18 Probiodrug Ag Use of isoQC inhibitors in the treatment and prevention of inflammatory diseases or conditions
NZ583799A (en) * 2007-09-12 2011-12-22 Probiodrug Ag Transgenic mice comprising a DNA transgene encoding ABeta peptide
WO2009090190A1 (en) * 2008-01-14 2009-07-23 Probiodrug Ag Mouse models carrying a knock-out mutation of the glutaminyl cyclase gene
EA028427B1 (ru) 2008-07-21 2017-11-30 Пробиодруг Аг АНТИТЕЛО, СВЯЗЫВАЮЩЕЕСЯ С Aβ-ПЕПТИДАМИ ИЛИ ИХ ВАРИАНТАМИ, КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ЭТО АНТИТЕЛО, И ЕГО ПРИМЕНЕНИЕ
EP2475428B1 (en) 2009-09-11 2015-07-01 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
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
AU2012228236B2 (en) 2011-03-16 2016-10-27 Vivoryon Therapeutics N.V. Diagnostic antibody assay
EP2702043A1 (en) * 2011-04-29 2014-03-05 Exelixis, Inc. Inhibitors of inducible form of 6-phosphofructose-2-kinase
WO2016097305A1 (en) 2014-12-19 2016-06-23 Probiodrug Ag Novel method for the detection of pglu-abeta peptides
CN105384691B (zh) * 2015-10-26 2018-06-29 深圳大学 一种谷氨酰胺酰基环化酶抑制剂的制备方法及应用
CN105384692B (zh) * 2015-10-26 2018-06-29 深圳大学 一种谷氨酰胺酰基环化酶抑制剂
CN106831712B (zh) * 2017-01-13 2019-04-02 深圳大学 一种多靶点Aβ寡聚化抑制剂
CN106831713B (zh) * 2017-01-13 2019-04-02 深圳大学 一种多靶点Aβ寡聚化抑制剂的合成方法及应用
DK3461819T3 (da) 2017-09-29 2020-08-10 Probiodrug Ag Inhibitorer af glutaminylcyklase
EP3521308B1 (en) 2018-01-31 2024-03-13 Vivoryon Therapeutics N.V. Humanized and de-immunized antibodies
CN109305942B (zh) * 2018-08-23 2022-04-22 深圳大学 一种含有4-咪唑基的谷氨酰胺酰基环化酶抑制剂的制备方法及应用
CN108912051B (zh) * 2018-08-23 2022-04-15 深圳大学 一种含有4-咪唑基的谷氨酰胺酰基环化酶抑制剂

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JPH0710870A (ja) 1993-06-23 1995-01-13 Asahi Glass Co Ltd 新規アミノピリジン誘導体およびその塩
DE19836697A1 (de) 1998-08-13 2000-02-17 Hoechst Marion Roussel De Gmbh Substituierte 4-Amino-2-aryl-pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate
US6948038B2 (en) * 2001-07-24 2005-09-20 Microsoft Corporation System and method for backing up and restoring data
WO2003026661A1 (fr) 2001-09-14 2003-04-03 Yamanouchi Pharmaceutical Co., Ltd. Accelerateur de secretion de l'insuline et nouveau derive de pyrimidine
WO2004041814A1 (en) 2002-11-04 2004-05-21 Vertex Pharmaceuticals Incorporated Heteroaryl-pyramidine derivatives as jak inhibitors
MXPA05005477A (es) * 2002-11-21 2005-07-25 Chiron Corp Pirimidinas 2,4,6-trisustituidas como inhibidores de fosfotidilinositol (pi) 3-cinasa y su uso en el tratamiento del cancer.
ZA200508439B (en) * 2003-05-05 2007-03-28 Probiodrug Ag Medical use of inhibitors of glutaminyl and glutamate cyclases
DK2206496T3 (da) * 2003-05-05 2014-12-15 Probiodrug Ag Screening af inhibitorer af pyroglutaminsyredannelse i amyloid beta-peptid
US7732162B2 (en) * 2003-05-05 2010-06-08 Probiodrug Ag Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases
US8338120B2 (en) * 2003-05-05 2012-12-25 Probiodrug Ag Method of treating inflammation with glutaminyl cyclase inhibitors
DK1675578T3 (da) * 2003-10-15 2013-08-26 Probiodrug Ag Inhibitorer af glutaminyl- og glutamatcyclaser til behandling af de neurodegenerative sygdomme FBD og FDD
US20050171112A1 (en) * 2003-11-03 2005-08-04 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
NZ546887A (en) * 2003-11-03 2009-04-30 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
WO2005058883A1 (en) * 2003-12-15 2005-06-30 Almirall Prodesfarma Ag 2, 6 bisheteroaryl-4-aminopyrimidines as adenosine receptor antagonists
EP1713780B1 (en) * 2004-02-05 2012-01-18 Probiodrug AG Novel inhibitors of glutaminyl cyclase
JO2660B1 (en) * 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
BRPI0718507A2 (pt) * 2006-09-21 2013-11-12 Probiodrug Ag Genes relacionados à glutaminil ciclase
US8420684B2 (en) * 2006-11-09 2013-04-16 Probiodrug Ag Inhibitors of glutaminyl cyclase
WO2008055950A1 (en) * 2006-11-09 2008-05-15 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
WO2008065141A1 (en) * 2006-11-30 2008-06-05 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
US20080200567A1 (en) * 2007-01-19 2008-08-21 Probiodrug Ag In vivo screening models for treatment of alzheimer's disease and other qpct-related disorders
DK2118101T3 (da) * 2007-03-09 2013-01-02 Probiodrug Ag IMIDAZO (1,5-A)-PYRIDinderivater som glutaminylcyclaseinhibitorer
WO2008128981A1 (en) * 2007-04-18 2008-10-30 Probiodrug Ag Nitrovinyl-diamine derivatives as glutaminyl cyclase inhibitors
US9034907B2 (en) * 2007-04-18 2015-05-19 Probiodrug Ag Inhibitors of glutaminyl cyclase
DK2142515T3 (da) * 2007-04-18 2014-06-23 Probiodrug Ag Nitrovinyl-diaminderivater som glutaminyl-cyclase-inhibitorer
US9512082B2 (en) * 2007-04-18 2016-12-06 Probiodrug Ag Inhibitors of glutaminyl cyclase
US9656991B2 (en) * 2007-04-18 2017-05-23 Probiodrug Ag Inhibitors of glutaminyl cyclase
ES2474693T3 (es) * 2007-04-18 2014-07-09 Probiodrug Ag Derivados de ciano-guanidina como inhibidores de glutaminil ciclasa

Also Published As

Publication number Publication date
US8188094B2 (en) 2012-05-29
EP2142536B1 (en) 2015-10-21
US20080260688A1 (en) 2008-10-23
JP2010524896A (ja) 2010-07-22
WO2008128984A1 (en) 2008-10-30
EP2142536A1 (en) 2010-01-13

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