CA2879195C - Fused triazole derivatives as gamma secretase modulators - Google Patents

Fused triazole derivatives as gamma secretase modulators Download PDF

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Publication number
CA2879195C
CA2879195C CA2879195A CA2879195A CA2879195C CA 2879195 C CA2879195 C CA 2879195C CA 2879195 A CA2879195 A CA 2879195A CA 2879195 A CA2879195 A CA 2879195A CA 2879195 C CA2879195 C CA 2879195C
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formula
mixture
compound
pharmaceutically acceptable
salt
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CA2879195A
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English (en)
French (fr)
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CA2879195A1 (en
Inventor
Ben Whittaker
Chris Steele
David Hardick
Dale Mitchell
Vincent Pomel
Anna Quattropani
Dirk Beher
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Ares Trading SA
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Ares Trading SA
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2879195A 2012-07-17 2013-06-14 Fused triazole derivatives as gamma secretase modulators Active CA2879195C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261672436P 2012-07-17 2012-07-17
EP12176726.3 2012-07-17
EP20120176726 EP2687528A1 (en) 2012-07-17 2012-07-17 Fused triazole derivatives as gamma secretase modulators
US61/672,436 2012-07-17
PCT/EP2013/001774 WO2014012614A1 (en) 2012-07-17 2013-06-14 Fused triazole derivatives as gamma secretase modulators

Publications (2)

Publication Number Publication Date
CA2879195A1 CA2879195A1 (en) 2014-01-23
CA2879195C true CA2879195C (en) 2021-02-16

Family

ID=46514224

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2879195A Active CA2879195C (en) 2012-07-17 2013-06-14 Fused triazole derivatives as gamma secretase modulators

Country Status (8)

Country Link
US (1) US9527853B2 (https=)
EP (2) EP2687528A1 (https=)
JP (1) JP6229717B2 (https=)
CN (1) CN104640859B (https=)
AU (1) AU2013292782B2 (https=)
CA (1) CA2879195C (https=)
ES (1) ES2617241T3 (https=)
WO (1) WO2014012614A1 (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6633618B2 (ja) * 2014-08-21 2020-01-22 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 強力なｒｏｃｋ阻害剤としてのタイドバックのベンズアミド誘導体
EP3347363B1 (en) * 2015-09-09 2020-01-01 H. Hoffnabb-La Roche Ag N-(3-azabicyclo[3.2.1]octan-8-yl)-8-(4-phenyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[l,5-a]pyridin-2-amine derivatives as gamma-secretase modulators for treating alzheimer's disease
CN109311878B (zh) * 2016-06-27 2022-05-24 豪夫迈·罗氏有限公司 作为γ-分泌酶调节剂的三唑并吡啶类化合物
WO2018011164A1 (en) * 2016-07-14 2018-01-18 F. Hoffmann-La Roche Ag Fused pyrimidine derivatives
JP6956175B2 (ja) * 2016-10-04 2021-11-02 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 二環式ヘテロアリール誘導体
CN107200737B (zh) * 2017-06-29 2019-03-26 武汉药明康德新药开发有限公司 叔丁氧羰基-3-(羟甲基)-[1,2,3]三氮唑[1,5-a]哌啶-6-酰胺制法
CN116925024B (zh) * 2023-07-24 2025-07-25 阜阳欣奕华制药科技有限公司 一种4,6-二甲基阔马酸甲酯的制备方法

Family Cites Families (15)

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AR035313A1 (es) 1999-01-27 2004-05-12 Wyeth Corp Inhibidores de tace acetilenicos de acido hidroxamico de sulfonamida a base de alfa-aminoacidos, composiciones farmaceuticas y el uso de los mismos para la manufactura de medicamentos.
JP2003530437A (ja) 2000-04-13 2003-10-14 マヨ ファウンデーション フォー メディカル エデュケーション アンド リサーチ Ａβ４２低下物質
WO2004110350A2 (en) * 2003-05-14 2004-12-23 Torreypines Therapeutics, Inc. Compouds and uses thereof in modulating amyloid beta
TWI378091B (en) * 2006-03-09 2012-12-01 Eisai R&D Man Co Ltd Multi-cyclic cinnamide derivatives
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
US8518975B2 (en) 2007-09-06 2013-08-27 Merck Sharp + Dohme Corp. Gamma secretase modulators
US8450343B2 (en) * 2007-12-06 2013-05-28 Xianhai Huang Gamma secretase modulators
AU2008335709A1 (en) * 2007-12-13 2009-06-18 Amgen Inc. Gamma secretase modulators
TW201030002A (en) 2009-01-16 2010-08-16 Bristol Myers Squibb Co Bicyclic compounds for the reduction of beta-amyloid production
JP2012051806A (ja) * 2009-02-26 2012-03-15 Eisai R & D Management Co Ltd イミダゾリルピラジン誘導体
CA2753696A1 (en) * 2009-02-26 2010-09-02 Noritaka Kitazawa Nitrogen-containing fused heterocyclic compounds and their use as beta amyloid production inhibitors
WO2011007756A1 (ja) * 2009-07-13 2011-01-20 武田薬品工業株式会社 複素環化合物及びその用途
EP2523949B1 (en) 2010-01-15 2014-08-20 Janssen Pharmaceuticals Inc. Novel substituted triazole derivatives as gamma secretase modulators
US20110190269A1 (en) * 2010-02-01 2011-08-04 Karlheinz Baumann Gamma secretase modulators
KR20130139895A (ko) * 2010-09-02 2013-12-23 다케다 야쿠힌 고교 가부시키가이샤 경도인지 장애의 치료 또는 예방용 융합 트리아졸

Also Published As

Publication number Publication date
CN104640859B (zh) 2017-03-01
EP2687528A1 (en) 2014-01-22
US9527853B2 (en) 2016-12-27
JP6229717B2 (ja) 2017-11-15
JP2015522592A (ja) 2015-08-06
AU2013292782B2 (en) 2017-07-13
WO2014012614A1 (en) 2014-01-23
CA2879195A1 (en) 2014-01-23
EP2875025A1 (en) 2015-05-27
CN104640859A (zh) 2015-05-20
EP2875025B1 (en) 2016-11-30
US20150183790A1 (en) 2015-07-02
AU2013292782A1 (en) 2015-02-26
ES2617241T3 (es) 2017-06-15

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