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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    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41921,2,3-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems

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  • 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)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Rheumatology (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 (enExample)
EP (2) EP2687528A1 (enExample)
JP (1) JP6229717B2 (enExample)
CN (1) CN104640859B (enExample)
AU (1) AU2013292782B2 (enExample)
CA (1) CA2879195C (enExample)
ES (1) ES2617241T3 (enExample)
WO (1) WO2014012614A1 (enExample)

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
EP3484884B1 (en) * 2016-07-14 2021-01-27 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

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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.
EP1284729A4 (en) 2000-04-13 2007-12-19 Mayo Foundation A- (BETA) -42 DECREASING MEDICINAL PRODUCTS
CN102584813B (zh) * 2003-05-14 2016-07-06 Ngc药物公司 化合物及其在调节淀粉样蛋白β中的用途
TWI378091B (en) * 2006-03-09 2012-12-01 Eisai R&D Man Co Ltd Multi-cyclic cinnamide derivatives
EA016464B1 (ru) * 2006-03-09 2012-05-30 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Полициклические производные арилимидазола
EP2200990A1 (en) 2007-09-06 2010-06-30 Schering Corporation Gamma secretase modulators
US8450343B2 (en) * 2007-12-06 2013-05-28 Xianhai Huang Gamma secretase modulators
US20110166132A1 (en) * 2007-12-13 2011-07-07 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
SG173710A1 (en) * 2009-02-26 2011-09-29 Eisai R&D Man Co Ltd Nitrogen-containing fused heterocyclic compounds and their use as beta amyloid production inhibitors
CN102482276A (zh) * 2009-07-13 2012-05-30 武田药品工业株式会社 杂环化合物及其用途
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
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
ES2617241T3 (es) 2017-06-15
CN104640859B (zh) 2017-03-01
JP6229717B2 (ja) 2017-11-15
AU2013292782B2 (en) 2017-07-13
AU2013292782A1 (en) 2015-02-26
CN104640859A (zh) 2015-05-20
EP2875025B1 (en) 2016-11-30
JP2015522592A (ja) 2015-08-06
US9527853B2 (en) 2016-12-27
US20150183790A1 (en) 2015-07-02
EP2875025A1 (en) 2015-05-27
WO2014012614A1 (en) 2014-01-23
EP2687528A1 (en) 2014-01-22
CA2879195A1 (en) 2014-01-23

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