CN102356081B - 减少β-淀粉状蛋白生成的双环化合物 - Google Patents

减少β-淀粉状蛋白生成的双环化合物 Download PDF

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Publication number
CN102356081B
CN102356081B CN201080012637.2A CN201080012637A CN102356081B CN 102356081 B CN102356081 B CN 102356081B CN 201080012637 A CN201080012637 A CN 201080012637A CN 102356081 B CN102356081 B CN 102356081B
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phenyl
azepine
triazolo
amine
tetrahydrochysene
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Expired - Fee Related
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Chinese (zh)
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CN102356081A (zh
Inventor
L·R·马钦
L·A·汤普森三世
K·M·博伊
J·M·盖尔农
M·A·希金斯
施建良
邬永金
张云惠
J·E·马科
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61P25/28Drugs 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/10Spiro-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)
CN201080012637.2A 2009-01-16 2010-01-12 减少β-淀粉状蛋白生成的双环化合物 Expired - Fee Related CN102356081B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US14531909P 2009-01-16 2009-01-16
US61/145319 2009-01-16
PCT/US2010/020710 WO2010083141A1 (en) 2009-01-16 2010-01-12 Bicyclic compounds for the reduction of beta-amyloid production

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CN102356081A CN102356081A (zh) 2012-02-15
CN102356081B true CN102356081B (zh) 2014-08-27

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US (1) US8349880B2 (https=)
EP (1) EP2379553B1 (https=)
JP (1) JP5638007B2 (https=)
CN (1) CN102356081B (https=)
AR (1) AR075139A1 (https=)
ES (1) ES2426023T3 (https=)
TW (1) TW201030002A (https=)
WO (1) WO2010083141A1 (https=)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2742897A1 (en) 2008-11-06 2010-05-14 Astrazeneca Ab Modulators of amyloid beta.
PA8854101A1 (es) 2008-12-18 2010-07-27 Ortho Mcneil Janssen Pharm Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa
WO2010089292A1 (en) 2009-02-06 2010-08-12 Ortho-Mcneil-Janssen Pharmaceuticals, Inc Novel substituted bicyclic heterocyclic compounds as gamma secretase modulators
TWI461425B (zh) 2009-02-19 2014-11-21 Janssen Pharmaceuticals Inc 作為伽瑪分泌酶調節劑之新穎經取代的苯并唑、苯并咪唑、唑并吡啶及咪唑并吡啶衍生物類
AU2010262036B2 (en) 2009-05-07 2014-10-30 Cellzome Limited Novel substituted indazole and aza-indazole derivatives as gamma secretase modulators
JP2012532912A (ja) 2009-07-15 2012-12-20 ジヤンセン・フアーマシユーチカルズ・インコーポレーテツド ガンマセクレターゼモジュレーターとしての置換されたトリアゾールおよびイミダゾール誘導体
BR112012017310A2 (pt) * 2010-01-15 2016-04-19 Janssen Pharmaceuticals Inc derivados de triazol substituídos como moduladores de gama secretase
LT2603513T (lt) 2010-08-10 2020-05-25 Takeda Pharmaceutical Company Limited Heterociklinis junginys ir jo panaudojimas kaip ampa receptoriaus teigiamo alosterinio moduliatoriaus
BR112013004746A2 (pt) 2010-09-02 2016-06-07 Takeda Pharmaceutical "composto, medicamento, inibidor da produção de beta-amilóide, modulador de gama-secretase, métodos para inibir a produção de beta-amilóide, para modular gama-secretase, e para prevenir ou tratar deficiência cognitiva branda ou mal de alzheimer, e, uso do composto."
TW201309655A (zh) * 2011-01-28 2013-03-01 必治妥美雅史谷比公司 降低β-類澱粉生成之化合物
AU2012230348A1 (en) 2011-03-24 2013-08-29 Cellzome Limited Novel substituted triazolyl piperazine and triazolyl piperidine derivatives as gamma secretase modulators
EP2691393B1 (en) 2011-03-31 2016-09-14 Pfizer Inc Novel bicyclic pyridinones
KR101913135B1 (ko) 2011-07-15 2018-10-30 얀센 파마슈티칼즈, 인코포레이티드 감마 세크레타제 조절 인자로서의 신규의 치환 인돌 유도체
US9181245B2 (en) 2012-05-16 2015-11-10 Janssen Pharmaceuticals, Inc. Substituted pyrido[1,2-a]pyrazines and substituted pyrido[1,2-a][1,4]diazepines for the treatment of (inter alia) Alzheimer's disease
EP2687528A1 (en) 2012-07-17 2014-01-22 Ares Trading S.A. Fused triazole derivatives as gamma secretase modulators
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
CA2889249C (en) 2012-12-20 2021-02-16 Francois Paul Bischoff Tricyclic 3,4-dihydro-2h-pyrido[1,2-a]pyrazine-1,6-dione derivatives as gamma secretase modulators
CA2891755C (en) 2013-01-17 2021-10-26 Janssen Pharmaceutica Nv Substituted pyrido-piperazinone derivatives as gamma secretase modulators
EP2958918B1 (en) * 2013-02-21 2016-12-07 Boehringer Ingelheim International GmbH Dihydropteridinones ii
WO2014195323A1 (en) 2013-06-04 2014-12-11 Acturum Life Science AB Pyrimidine compounds and their use as gamma secretase modulators
JP6368776B2 (ja) 2013-06-04 2018-08-01 アクチュラム・ライフ・サイエンス・アクチエボラーグ トリアゾール化合物およびガンマセクレターゼモジュレーターとしてのその使用
JP6396438B2 (ja) 2013-06-04 2018-09-26 アクチュラム・ライフ・サイエンス・アクチエボラーグ トリアゾール化合物およびガンマセクレターゼモジュレーターとしてのその使用
US10562897B2 (en) 2014-01-16 2020-02-18 Janssen Pharmaceutica Nv Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators
MX368391B (es) 2015-02-03 2019-09-30 Pfizer Ciclopropabenzofuranil-piridopirazindionas novedosas.
JP7012715B2 (ja) 2016-06-27 2022-01-28 エフ.ホフマン-ラ ロシュ アーゲー γ-セクレターゼモジュレーターとしてのトリアゾロピリジン
AR109829A1 (es) * 2016-09-29 2019-01-30 Hoffmann La Roche Derivados de piperidina puenteados
WO2018083050A1 (en) * 2016-11-01 2018-05-11 F. Hoffmann-La Roche Ag Bicyclic heteroaryl derivatives
WO2018165520A1 (en) 2017-03-10 2018-09-13 Vps-3, Inc. Metalloenzyme inhibitor compounds
WO2019121434A1 (en) * 2017-12-18 2019-06-27 F. Hoffmann-La Roche Ag Triazolo-azepine derivatives
CN111417636B (zh) * 2018-01-22 2023-09-26 豪夫迈·罗氏有限公司 三唑并-氮杂䓬衍生物
AU2020321955A1 (en) 2019-07-30 2022-03-17 Eikonizo Therapapeutics, Inc. HDAC6 inhibitors and uses thereof
AU2020348675B2 (en) 2019-09-16 2025-11-20 Takeda Pharmaceutical Company Limited Azole-fused pyridazin-3(2H)-one derivatives
EP4065581B1 (en) 2019-11-29 2024-07-24 F. Hoffmann-La Roche AG Process for the preparation (9s)-2-bromo-9-(2,3,4-trifluorophenyl)-6,7,8,9-tetrahydro-5h-[1,2,4]triazolo[1,5-a]azepine
IL316201A (en) 2022-04-08 2024-12-01 Eikonizo Therapeutics Inc Oxadiazole HDAC6 inhibitors and their uses
WO2024032584A1 (zh) * 2022-08-08 2024-02-15 苏州必扬医药科技有限公司 一种蛋白酪氨酸激酶抑制剂及其医疗用途
CN120324393B (zh) * 2025-05-20 2025-11-04 广东海洋大学 (2,4-二氯苯基)甲基硫基甲烷脒及其盐的用途

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR059955A1 (es) * 2006-03-09 2008-05-14 Eisai R&D Man Co Ltd Compuestos policiclicos no peptidicos, medicamentos que los contienen, y usos para prevenir o tratar enfermedades causadas por la produccion de beta amiloide
AU2008248129B8 (en) * 2007-05-07 2013-05-30 Merck Sharp & Dohme Corp. Gamma secretase modulators
EP2155740B1 (en) 2007-05-11 2011-01-26 F. Hoffmann-La Roche AG Hetarylanilines as modulators for amyloid beta
US7935815B2 (en) * 2007-08-31 2011-05-03 Eisai R&D Management Co., Ltd. Imidazoyl pyridine compounds and salts thereof
ES2529648T3 (es) 2007-08-31 2015-02-24 Eisai R&D Management Co., Ltd. Compuesto policíclico
ES2375919T3 (es) 2008-01-11 2012-03-07 F. Hoffmann-La Roche Ag Moduladores de beta-amiloide.
MX2010008700A (es) 2008-02-22 2010-08-30 Hoffmann La Roche Moduladores de beta-amiloide.

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
β-Amyloid Peptide Free Radical Fragments Initiate Synaptosomal Lipoperoxidation in a Sequence-Specific Fashion: Implications to Alzheimer′s Disease;D.A. Butterfield 等;《Biochemical and Biophysical Research Communications》;19940430;第200卷(第2期);第710-715页 *
人参皂苷Rbl抑制p淀粉样蛋白笛塔诱导的皮层神经元tau蛋白过度磷酸化;曾育琦 等;《药学学报》;20050630;第40卷(第3期);第225-230页 *

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Publication number Publication date
EP2379553B1 (en) 2013-06-26
ES2426023T3 (es) 2013-10-18
EP2379553A1 (en) 2011-10-26
TW201030002A (en) 2010-08-16
JP2012515205A (ja) 2012-07-05
JP5638007B2 (ja) 2014-12-10
AR075139A1 (es) 2011-03-09
US8349880B2 (en) 2013-01-08
WO2010083141A1 (en) 2010-07-22
US20110015175A1 (en) 2011-01-20
CN102356081A (zh) 2012-02-15

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