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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Japanese (ja)
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JP2010524896A5 (enExample
JP2010524896A (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
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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Anesthesiology (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pregnancy & Childbirth (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (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 (enExample) 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 (enExample)
EP (1) EP2142536B1 (enExample)
JP (1) JP5676249B2 (enExample)
WO (1) WO2008128984A1 (enExample)

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* 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
KR101432848B1 (ko) * 2006-09-21 2014-08-27 프로비오드룩 아게 글루타미닐 사이클라제에 관련된 신규한 유전자
US8889709B2 (en) * 2006-09-21 2014-11-18 Probiodrug Ag Use of isoQC inhibitors in the treatment and prevention of inflammatory diseases or conditions
US9277737B2 (en) 2006-09-21 2016-03-08 Probiodrug Ag Mouse models carrying a knock-out mutation of the QPCTL-gene
NZ583799A (en) * 2007-09-12 2011-12-22 Probiodrug Ag Transgenic mice comprising a DNA transgene encoding ABeta peptide
AU2009204864A1 (en) * 2008-01-14 2009-07-23 Probiodrug Ag Mouse models carrying a knock-out mutation of the glutaminyl cyclase gene
US8058405B2 (en) 2008-07-21 2011-11-15 Probiodrug (AG) Antibodies specific for N-terminal truncated and pyroglutamate modified amyloid-beta peptides
NZ598685A (en) 2009-09-11 2013-05-31 Probiodrug Ag Heterocylcic derivatives as inhibitors of glutaminyl cyclase
WO2011076854A1 (en) 2009-12-22 2011-06-30 Probiodrug Ag CLEAVAGE OF β-AMYLOID PRECURSOR PROTEIN
US20110212853A1 (en) 2010-02-18 2011-09-01 Probiodrug Ag Novel diagnostic method
MX343873B (es) 2011-03-16 2016-11-25 Probiodrug Ag Ensayo de diagnostico de anticuerpo.
WO2012149528A1 (en) * 2011-04-29 2012-11-01 Exelixis, Inc. Inhibitors of inducible form of 6-phosphofructose-2-kinase
EP3234611A1 (en) 2014-12-19 2017-10-25 Probiodrug AG Novel method for the detection of pglu-abeta peptides
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
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
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
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
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

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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
ES2289349T3 (es) 2002-11-04 2008-02-01 Vertex Pharmaceuticals Incorporated Derivados de heteroaril-pirimidina como inhibidores de jak.
ES2412273T3 (es) 2002-11-21 2013-07-10 Novartis Ag Inhibidores de 2-morfolín-4-pirimidinas como inhibidores de fosfotidilinositol (PI) 3-quinasa y su uso en el tratamiento del cáncer.
JP4806628B2 (ja) * 2003-05-05 2011-11-02 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
US8338120B2 (en) * 2003-05-05 2012-12-25 Probiodrug Ag Method of treating inflammation with glutaminyl cyclase inhibitors
KR20100106630A (ko) * 2003-05-05 2010-10-01 프로비오드룩 아게 글루타미닐 및 글루타메이트 사이클라제의 이펙터의 용도
US7732162B2 (en) * 2003-05-05 2010-06-08 Probiodrug Ag Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases
AU2004283461B2 (en) 2003-10-15 2010-02-11 Probiodrug Ag Use of effectors of glutaminyl and glutamate cyclases
US7667044B2 (en) * 2003-11-03 2010-02-23 Probiodrug Ag Compounds for the treatment of neurological disorders
US20050171112A1 (en) * 2003-11-03 2005-08-04 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
WO2005049027A2 (en) * 2003-11-03 2005-06-02 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
SMP200600024B (it) * 2003-12-15 2006-07-19 Almirall Prodesfarma Ag 2,6-Biseteroaril-4-amminopirimidine come antagonisti del recettore dell'adenosina
JP4996926B2 (ja) * 2004-02-05 2012-08-08 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の阻害剤
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
KR101432848B1 (ko) * 2006-09-21 2014-08-27 프로비오드룩 아게 글루타미닐 사이클라제에 관련된 신규한 유전자
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
EP2091948B1 (en) * 2006-11-30 2012-04-18 Probiodrug AG Novel inhibitors of glutaminyl cyclase
WO2008087197A1 (en) * 2007-01-19 2008-07-24 Probiodrug Ag In vivo screening models for treatment of alzheimer's disease and other qpct-related disorders
US7803810B2 (en) * 2007-03-09 2010-09-28 Probiodrug Ag Inhibitors
ES2474693T3 (es) * 2007-04-18 2014-07-09 Probiodrug Ag Derivados de ciano-guanidina como inhibidores de glutaminil ciclasa
JP5675343B2 (ja) * 2007-04-18 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尿素誘導体
JP5675344B2 (ja) * 2007-04-18 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ニトロビニルジアミン誘導体
DK2142513T3 (da) * 2007-04-18 2014-06-10 Probiodrug Ag Nitrovinyl-diamin-derivater som glutaminyl-cyclase-inhibitorer
ES2478673T3 (es) * 2007-04-18 2014-07-22 Probiodrug Ag Derivados de tioxoquinazolinona como inhibidores de la glutaminil ciclasa
JP5667440B2 (ja) * 2007-04-18 2015-02-12 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チオ尿素誘導体

Also Published As

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

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