CN105263923B - 嘧啶化合物及它们作为γ分泌酶调节剂的用途 - Google Patents

嘧啶化合物及它们作为γ分泌酶调节剂的用途 Download PDF

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Publication number
CN105263923B
CN105263923B CN201480032083.0A CN201480032083A CN105263923B CN 105263923 B CN105263923 B CN 105263923B CN 201480032083 A CN201480032083 A CN 201480032083A CN 105263923 B CN105263923 B CN 105263923B
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Prior art keywords
methyl
pyrimidine
groups
phenyl
imidazole
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Expired - Fee Related
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CN201480032083.0A
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English (en)
Chinese (zh)
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CN105263923A (zh
Inventor
Y.贝西德斯基
U.英格夫
K.保尔森
C.林德
I.麦克萨里
J.马姆博格
A.帕普奇克海因
P.阿维森
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Acturum Life Science AB
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Acturum Life Science AB
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07D403/14—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 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201480032083.0A 2013-06-04 2014-06-03 嘧啶化合物及它们作为γ分泌酶调节剂的用途 Expired - Fee Related CN105263923B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
SE1350685 2013-06-04
SE1350685-2 2013-06-04
PCT/EP2014/061503 WO2014195323A1 (en) 2013-06-04 2014-06-03 Pyrimidine compounds and their use as gamma secretase modulators

Publications (2)

Publication Number Publication Date
CN105263923A CN105263923A (zh) 2016-01-20
CN105263923B true CN105263923B (zh) 2017-06-23

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CN201480032083.0A Expired - Fee Related CN105263923B (zh) 2013-06-04 2014-06-03 嘧啶化合物及它们作为γ分泌酶调节剂的用途

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Country Link
US (1) US9439904B2 (enExample)
EP (1) EP3004079B1 (enExample)
JP (1) JP6368777B2 (enExample)
CN (1) CN105263923B (enExample)
DK (1) DK3004079T3 (enExample)
ES (1) ES2665421T3 (enExample)
NO (1) NO3004079T3 (enExample)
PL (1) PL3004079T3 (enExample)
WO (1) WO2014195323A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3481829B1 (en) * 2016-07-08 2021-04-07 H. Hoffnabb-La Roche Ag Fused pyrimidine derivatives
CN108191776A (zh) * 2018-01-22 2018-06-22 无锡富泽药业有限公司 一种尿嘧啶的绿色生产工艺
WO2020247707A1 (en) * 2019-06-05 2020-12-10 Chunyu Wang SYSTEMS AND METHOD FOR INHIBITING γ-SECRETASE PRODUCTION OF AMYLOID-β PEPTIDES
US12297244B2 (en) 2019-06-05 2025-05-13 Rensselaer Polytechnic Institute Systems and methods for inhibiting γ-secretase production of amyloid-β peptides
CN110372603A (zh) * 2019-06-24 2019-10-25 南京普锐达医药科技有限公司 一种2-氯-5-氟-6-乙基嘧啶的合成方法
CN113149977A (zh) 2020-01-22 2021-07-23 苏州爱科百发生物医药技术有限公司 一类呼吸道合胞病毒抑制剂的合成与用途
MX2023011027A (es) 2021-03-23 2023-09-27 Halia Therapeutics Inc Derivados de pirimidina utiles como inhibidores de la proteina cinasa de repeticion 2 rica en leucina (lrrk2).

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WO2007053452A1 (en) * 2005-11-01 2007-05-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
WO2009103652A1 (en) * 2008-02-22 2009-08-27 F. Hoffmann-La Roche Ag Modulators for amyloid beta

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ITMI20030312A1 (it) 2003-02-21 2004-08-22 Chiesi Farma Spa Derivati di acidi 2-fenil-2-alchil-acetici per il trattamento della malattia di alzheimer.
ATE464048T1 (de) 2003-08-07 2010-04-15 Merck Sharp & Dohme Behandlung von alzheimer-krankheit und verwandten zuständen
EP1708997B1 (en) 2003-12-03 2009-10-21 Merck and Co., Inc. 1-alkyl-3-thio-substituted indole-2-alkynoic acids useful for the treatment for alzheimer's disease and related conditions
KR100966749B1 (ko) 2004-05-26 2010-06-30 에자이 알앤드디 매니지먼트 가부시키가이샤 신나미드 화합물
CA2649996A1 (en) 2006-04-26 2007-11-08 Merck Sharp & Dohme Limited Piperidines and related compounds for treatment of alzheimer's disease
AU2007252643A1 (en) 2006-05-19 2007-11-29 Eisai R & D Management Co., Ltd. Urea type cinnamide derivative
JP2009184924A (ja) 2006-05-31 2009-08-20 Eisai R & D Management Co Ltd 生物学的試薬用化合物
EP2117311A4 (en) 2007-02-08 2011-05-11 Merck Sharp & Dohme Therapeutic agents
US8252803B2 (en) 2007-02-12 2012-08-28 Merck Sharp & Dohme Corp. Piperidine derivatives
CA2676715A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
US8242150B2 (en) 2007-06-13 2012-08-14 Merck Sharp & Dohme Corp. Triazole derivatives for treating alzheimer'S disease and related conditions
JP2010535762A (ja) 2007-08-06 2010-11-25 シェーリング コーポレイション ガンマセクレターゼモジュレーター
CN101910142B (zh) 2008-01-11 2013-07-10 弗·哈夫曼-拉罗切有限公司 β-淀粉状蛋白的调节剂
JP5502089B2 (ja) * 2008-10-09 2014-05-28 エフ．ホフマン−ラ ロシュ アーゲー アミロイドβのモジュレーター
EP2367826A4 (en) * 2008-11-06 2012-07-04 Astrazeneca Ab MODULATORS OF THE PROTEIN -AMYLOID
JP5378532B2 (ja) 2008-11-10 2013-12-25 エフ．ホフマン−ラ ロシュ アーゲー 複素環γ−セクレターゼモジュレーター
TW201030002A (en) 2009-01-16 2010-08-16 Bristol Myers Squibb Co Bicyclic compounds for the reduction of beta-amyloid production
UY32622A (es) 2009-05-12 2010-12-31 Astrazeneca Ab Nuevos compuestos para el tratamiento de patologías relacionadas con ab(beta)
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TWI468402B (zh) 2009-07-31 2015-01-11 必治妥美雅史谷比公司 降低β－類澱粉生成之化合物
PH12012501381A1 (en) 2010-01-15 2012-10-22 Janssen Pharmaceuticals Inc Novel substituted bicyclic triazole derivatives as gamma secretase modulators
US20110190269A1 (en) 2010-02-01 2011-08-04 Karlheinz Baumann Gamma secretase modulators
TW201206946A (en) 2010-07-15 2012-02-16 Bristol Myers Squibb Co Compounds for the reduction of beta-amyloid production

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000025780A1 (en) * 1998-10-29 2000-05-11 Bristol-Myers Squibb Company Compounds derived from an amine nucleus that are inhibitors of impdh enzyme
WO2007053452A1 (en) * 2005-11-01 2007-05-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
WO2009103652A1 (en) * 2008-02-22 2009-08-27 F. Hoffmann-La Roche Ag Modulators for amyloid beta

Also Published As

Publication number Publication date
EP3004079B1 (en) 2018-01-17
US20160129002A1 (en) 2016-05-12
ES2665421T3 (es) 2018-04-25
DK3004079T3 (en) 2018-04-16
CN105263923A (zh) 2016-01-20
JP6368777B2 (ja) 2018-08-01
WO2014195323A1 (en) 2014-12-11
US9439904B2 (en) 2016-09-13
PL3004079T3 (pl) 2018-07-31
EP3004079A1 (en) 2016-04-13
JP2016520637A (ja) 2016-07-14
NO3004079T3 (enExample) 2018-06-16

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Granted publication date: 20170623

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