EA201270166A1 - Замещенные производные триазола и имидазола в качестве модуляторов гамма-секретазы - Google Patents

Замещенные производные триазола и имидазола в качестве модуляторов гамма-секретазы

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Publication number
EA201270166A1
EA201270166A1 EA201270166A EA201270166A EA201270166A1 EA 201270166 A1 EA201270166 A1 EA 201270166A1 EA 201270166 A EA201270166 A EA 201270166A EA 201270166 A EA201270166 A EA 201270166A EA 201270166 A1 EA201270166 A1 EA 201270166A1
Authority
EA
Eurasian Patent Office
Prior art keywords
triazole
imidazole
substituted derivatives
gamma
compounds
Prior art date
Application number
EA201270166A
Other languages
English (en)
Other versions
EA021047B1 (ru
Inventor
Тонгфей Ву
Хенрикус Якобус Мария Гейсен
Фредерик Ян Рита Ромбаутс
Франсуа Поль Бишофф
Дидье Жан-Клод Бертело
Дэниел Оельрих
Михел Анна Йозеф Де Клейн
Серж Мария Алоисиус Питерс
Гарретт Берлонд Минн
Адриана Ингрид Велтер
Свен Францискус Анна Ван Брандт
Михел Суркин
Original Assignee
Янссен Фармасьютикалз, Инк.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Янссен Фармасьютикалз, Инк. filed Critical Янссен Фармасьютикалз, Инк.
Publication of EA201270166A1 publication Critical patent/EA201270166A1/ru
Publication of EA021047B1 publication Critical patent/EA021047B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C07D233/60—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
    • 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
    • C07D403/10—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 carbon chain containing aromatic rings
    • 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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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

Abstract

Изобретение относится к новым замещенным производным триазола и имидазола формулы (I) , где R, R, А, А, А, А, Х и Hetимеют значения, определенные в формуле изобретения. Соединения согласно настоящему изобретению пригодны в качестве модуляторов гамма-секретазы. Кроме того, изобретение относится к способам получения таких новых соединений, к фармацевтическим композициям, содержащим указанные соединения в качестве активного ингредиента, а также к применению указанных соединений в качестве лекарственного средства.
EA201270166A 2009-07-15 2010-07-13 Замещенные производные триазола и имидазола в качестве модуляторов гамма-секретазы EA021047B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09165585 2009-07-15
EP10164625 2010-06-01
PCT/EP2010/060083 WO2011006903A1 (en) 2009-07-15 2010-07-13 Substituted triazole and imidazole derivatives as gamma secretase modulators

Publications (2)

Publication Number Publication Date
EA201270166A1 true EA201270166A1 (ru) 2012-06-29
EA021047B1 EA021047B1 (ru) 2015-03-31

Family

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Country Status (18)

Country Link
US (1) US8946266B2 (ru)
EP (1) EP2454239B1 (ru)
JP (2) JP2012532912A (ru)
KR (1) KR20120050450A (ru)
CN (1) CN102482227A (ru)
AP (1) AP2011006034A0 (ru)
AU (1) AU2010272578B2 (ru)
BR (1) BR112012000915A2 (ru)
CA (1) CA2778517A1 (ru)
EA (1) EA021047B1 (ru)
ES (1) ES2519565T3 (ru)
IL (1) IL217491A (ru)
MX (1) MX2012000763A (ru)
NZ (1) NZ597505A (ru)
SG (1) SG177644A1 (ru)
TW (1) TW201109316A (ru)
WO (1) WO2011006903A1 (ru)
ZA (1) ZA201200285B (ru)

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2010002098A (es) * 2007-08-31 2010-03-30 Eisai R&D Man Co Ltd Compuesto policiclico.
US7935815B2 (en) * 2007-08-31 2011-05-03 Eisai R&D Management Co., Ltd. Imidazoyl pyridine compounds and salts thereof
PA8854101A1 (es) 2008-12-18 2010-07-27 Ortho Mcneil Janssen Pharm Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa
AP2011005779A0 (en) 2009-02-06 2011-08-31 Ortho Mcneil Janssen Pharm Novel susbstituted bicyclic heterocyclic compoundsas 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
CN102333777B (zh) 2009-02-26 2014-06-25 卫材R&D管理有限公司 含氮的稠合杂环化合物及其作为β淀粉样蛋白生成抑制剂的用途
US8703954B2 (en) 2009-02-26 2014-04-22 Eisai R&D Management Co., Ltd. Salt of tetrahydrotriazolopyridine derivative and crystal thereof
NZ596843A (en) 2009-05-07 2012-12-21 Janssen Pharmaceuticals Inc Novel substituted indazole and aza-indazole derivatives as gamma secretase modulators
EP2454239B1 (en) 2009-07-15 2014-08-13 Janssen Pharmaceuticals Inc. Substituted triazole and imidazole derivatives as gamma secretase modulators
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
US8637525B2 (en) 2009-07-31 2014-01-28 Bristol-Myers Squibb Company Compounds for the reduction of beta-amyloid production
BR112012017310A2 (pt) 2010-01-15 2016-04-19 Janssen Pharmaceuticals Inc derivados de triazol substituídos como moduladores de gama secretase
EP2611805A1 (en) 2010-09-02 2013-07-10 Takeda Pharmaceutical Company Limited Fused triazoles for the treatment or prophylaxis of mild cognitive impairment
CN102617457A (zh) * 2011-01-28 2012-08-01 天津药物研究院 一种制备罗氟司特的新方法
CN102690194B (zh) * 2011-03-24 2014-06-25 上海通远生物科技有限公司 3-环丙基甲氧基-4-二氟甲氧基苯甲酸的制备方法
KR20140047032A (ko) * 2011-03-24 2014-04-21 얀센 파마슈티칼즈, 인코포레이티드 감마 세크레타제 조정제로서의 신규 치환 트리아졸릴 피페라진 및 트리아졸릴 피페리딘 유도체
WO2013005354A1 (ja) * 2011-07-01 2013-01-10 武田薬品工業株式会社 複素環化合物
WO2013010812A1 (en) 2011-07-15 2013-01-24 Janssen Pharmaceutica Nv Monoclonal antibodies specific for beta-amyloid x-37 and uses thereof
IN2014MN00258A (ru) 2011-07-15 2015-09-25 Janssen Pharmaceuticals Inc
ES2674451T3 (es) * 2012-02-21 2018-06-29 Merck Patent Gmbh 2-amino-[1,2,4]triazolo[1,5-a] pirazinas 8-sustituidos como inhibidores de la SYK tirosina quinasa e inhibidores de la serina quinasa GCN2
AU2013261023B2 (en) 2012-05-16 2016-11-24 Cellzome Limited Substituted 3, 4 - dihydro - 2H - pyrido [1, 2 -a] pyrazine - 1, 6 - dione derivatives useful for the treatment of (inter alia) Alzheimer's disease
NZ704799A (en) * 2012-08-24 2018-06-29 Univ Texas Heterocyclic modulators of hif activity for treatment of disease
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
EP2945944B1 (en) 2013-01-17 2016-11-09 Janssen Pharmaceutica, N.V. Novel substituted pyrido-piperazinone derivatives as gamma secretase modulators
NO3004079T3 (ru) 2013-06-04 2018-06-16
WO2014195321A1 (en) 2013-06-04 2014-12-11 Acturum Life Science AB Triazole compounds and their use as gamma secretase modulators
CN105263922B (zh) 2013-06-04 2018-08-17 阿克图拉姆生命科学股份公司 ***化合物及其作为γ分泌酶调节剂的用途
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
DK3110420T3 (da) 2014-02-25 2019-05-13 Board Of Regents Univ Of Texas System Salte af heterocykliske modulatorer af hif-aktivitet til behandling af sygdomme
MX2017005715A (es) 2014-10-31 2018-02-23 Massachusetts Gen Hospital Potentes moduladores de gamma-secretasa.
EP3053920B1 (en) * 2015-02-05 2020-04-08 AB Science Compounds with anti-tumoral activity
EP3484884B1 (en) * 2016-07-14 2021-01-27 Hoffmann-La Roche AG Fused pyrimidine derivatives
WO2018087018A1 (en) 2016-11-08 2018-05-17 F. Hoffmann-La Roche Ag Phenoxytriazoles
AU2018348930A1 (en) 2017-10-11 2020-03-26 F. Hoffmann-La Roche Ag Bicyclic compounds for use as RIP 1 kinase inhibitors
EP4003966A1 (de) 2019-07-22 2022-06-01 Bayer Aktiengesellschaft 5-amino substituierte pyrazole und triazole als schädlingsbekämpfungsmittel
CN110759902B (zh) * 2019-11-01 2022-04-22 海南一龄医疗产业发展有限公司 Set8赖氨酸甲基转移酶抑制剂及其制备方法和用途
WO2022033991A1 (de) 2020-08-13 2022-02-17 Bayer Aktiengesellschaft 5-amino substituierte triazole als schädlingsbekämpfungsmittel
CN112480073B (zh) * 2020-12-02 2022-03-22 武汉药明康德新药开发有限公司 1-烷基-3,5-芳基取代的1,2,4三氮唑化合物的合成方法
WO2023238065A1 (en) 2022-06-09 2023-12-14 Glaxosmithkline Intellectual Property Development Limited Nitrogen containing condensed 2,3-dihydroquinazolinone compounds as nav1.8 inhibitors

Family Cites Families (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5767144A (en) 1994-08-19 1998-06-16 Abbott Laboratories Endothelin antagonists
DE69615376T2 (de) 1995-07-13 2002-09-05 Knoll Gmbh Piperazin-derivate als heilmittel
KR20010100977A (ko) * 1998-11-03 2001-11-14 스타르크, 카르크 치환된 2-페닐벤즈이미다졸, 그의 제조 및 그의 용도
MXPA01011112A (es) 1999-06-10 2002-06-04 Warner Lambert Co Metodo para la inhibicion de la agregacion de las proteinas amiloides y formacion de imagenes de los depositos amiloides utilizando derivados de la isoindolina.
AU5702201A (en) 2000-04-13 2001-10-30 Mayo Foundation Abeta<sub>42</sub> lowering agents
US20030176454A1 (en) 2000-05-15 2003-09-18 Akira Yamada N-coating heterocyclic compounds
DE10109867A1 (de) 2001-03-01 2002-09-05 Abbott Gmbh & Co Kg Verwendung von Triazolverbindungen zur Prophylaxe und Therapie neurodegenerativer Erkrankungen, Hirntrauma und zerebraler Ischämie
DE10238002A1 (de) 2002-08-20 2004-03-04 Merck Patent Gmbh Benzimidazolderivate
PL378753A1 (pl) 2003-02-27 2006-05-15 F.Hoffmann-La Roche Ag Antagoniści receptora CCR-3
AU2004247013B2 (en) 2003-05-14 2010-07-08 Neurogenetic Pharmaceuticals, Inc. Compounds and uses thereof in modulating amyloid beta
RU2376292C2 (ru) 2003-08-14 2009-12-20 Ф.Хоффманн-Ля Рош Аг Гамк-ергические модуляторы
DE602005023965D1 (de) 2004-03-08 2010-11-18 Prosidion Ltd Pyrrolopyridin-2-carbonsäurehydrazide als inhibitoren von glykogenphosphorylase
KR101128065B1 (ko) 2004-05-26 2012-04-12 에자이 알앤드디 매니지먼트 가부시키가이샤 신나미드 화합물
AU2005297966B2 (en) 2004-10-26 2010-12-23 Eisai R & D Management Co., Ltd. Amorphous object of cinnamide compound
US7572807B2 (en) 2005-06-09 2009-08-11 Bristol-Myers Squibb Company Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
JP2009508929A (ja) 2005-09-22 2009-03-05 サノフイ−アベンテイス Ｃｃｒ３受容体リガンドとしてのアミノ−アルキル−アミド誘導体
US20070078136A1 (en) 2005-09-22 2007-04-05 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
WO2007043786A1 (en) 2005-10-10 2007-04-19 Seiyang Yang Dynamic-based verification apparatus for verification from electronic system level to gate level, and verification method using the same
EP1937767B1 (en) 2005-10-11 2013-05-22 Chemtura Corporation Diaromatic amines
US20090163482A1 (en) 2006-03-13 2009-06-25 Mchardy Stanton Furst Tetralines antagonists of the h-3 receptor
GB0606774D0 (en) 2006-04-03 2006-05-10 Novartis Ag Organic compounds
US7893058B2 (en) 2006-05-15 2011-02-22 Janssen Pharmaceutica Nv Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
US20080090834A1 (en) * 2006-07-06 2008-04-17 Pfizer Inc Selective azole pde10a inhibitor compounds
US7951818B2 (en) 2006-12-01 2011-05-31 Galapagos Nv Imidazolopyridine compounds useful for the treatment of degenerative and inflammatory diseases
WO2008082490A2 (en) 2006-12-20 2008-07-10 Schering Corporation Novel jnk inhibitors
AU2008214372A1 (en) 2007-02-08 2008-08-14 Merck Sharp & Dohme Corp. Therapeutic agents
WO2008100412A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperidine derivatives
EP2121633A2 (en) 2007-02-12 2009-11-25 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
RU2009144998A (ru) 2007-05-07 2011-06-20 Шеринг Корпорейшн (US) Модуляторы гамма-секретазы
BRPI0811993A2 (pt) 2007-05-11 2014-11-18 Hoffmann La Roche " hetarilanilinas como moduladores para beta-amiloide ".
EP2166854A4 (en) 2007-06-13 2012-05-16 Merck Sharp & Dohme TRIAZOLE DERIVATIVES FOR THE TREATMENT OF ALZHEIMER'S DISEASE AND ASSOCIATED STATES
WO2009005729A1 (en) 2007-06-29 2009-01-08 Schering Corporation Gamma secretase modulators
CA2693138A1 (en) * 2007-07-16 2009-01-22 Wyeth Llc Aminoalkylazole derivatives as histamine-3 antagonists
US7935815B2 (en) 2007-08-31 2011-05-03 Eisai R&D Management Co., Ltd. Imidazoyl pyridine compounds and salts thereof
CA2698341A1 (en) 2007-09-06 2009-03-12 Schering Corporation Gamma secretase modulators
GB0720444D0 (en) 2007-10-18 2007-11-28 Glaxo Group Ltd Novel compounds
KR20100094554A (ko) 2007-12-06 2010-08-26 쉐링 코포레이션 감마 세크레타제 조절인자
WO2009076352A1 (en) * 2007-12-11 2009-06-18 Schering Corporation Gamma secretase modulators
CA2713716A1 (en) 2008-02-22 2009-08-27 F. Hoffmann-La Roche Ag Modulators for amyloid beta
US20100137320A1 (en) 2008-02-29 2010-06-03 Schering Corporation Gamma secretase modulators
WO2010010188A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases.
US20120129846A1 (en) 2008-11-06 2012-05-24 Zhaoning Zhu Gamma secretase modulators
KR101293421B1 (ko) 2008-11-10 2013-08-05 에프. 호프만-라 로슈 아게 헤테로사이클릭 감마 분비효소 조절제
CA2744152A1 (en) 2008-12-03 2010-06-10 Via Pharmaceuticals, Inc. Inhibitors of diacylglycerol acyltransferase
PA8854101A1 (es) 2008-12-18 2010-07-27 Ortho Mcneil Janssen Pharm Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa
TW201030002A (en) 2009-01-16 2010-08-16 Bristol Myers Squibb Co Bicyclic compounds for the reduction of beta-amyloid production
AP2011005779A0 (en) 2009-02-06 2011-08-31 Ortho Mcneil Janssen Pharm Novel susbstituted bicyclic heterocyclic compoundsas 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
CN102333777B (zh) 2009-02-26 2014-06-25 卫材R&D管理有限公司 含氮的稠合杂环化合物及其作为β淀粉样蛋白生成抑制剂的用途
JP2012051807A (ja) 2009-02-26 2012-03-15 Eisai R & D Management Co Ltd アリールイミダゾール化合物
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
US20120053165A1 (en) 2009-03-03 2012-03-01 Pfizer Inc. Novel Phenyl Imidazoles and Phenyl Triazoles As Gamma-Secretase Modulators
US20110299830A1 (en) 2009-03-16 2011-12-08 Panasonic Corporation Application running device
EP2424866A1 (en) 2009-04-27 2012-03-07 High Point Pharmaceuticals, LLC Substituted imidazo[1,2-a]pyridine derivatives, pharmaceutical compositions, and methods of use as -secretase inhibitors
NZ596843A (en) 2009-05-07 2012-12-21 Janssen Pharmaceuticals Inc Novel substituted indazole and aza-indazole derivatives as gamma secretase modulators
JP2010274429A (ja) 2009-05-26 2010-12-09 Ihi Corp アライメントステージ
EP2454239B1 (en) 2009-07-15 2014-08-13 Janssen Pharmaceuticals Inc. Substituted triazole and imidazole derivatives as gamma secretase modulators
BR112012017310A2 (pt) 2010-01-15 2016-04-19 Janssen Pharmaceuticals Inc derivados de triazol substituídos como moduladores de gama secretase
KR20140047032A (ko) 2011-03-24 2014-04-21 얀센 파마슈티칼즈, 인코포레이티드 감마 세크레타제 조정제로서의 신규 치환 트리아졸릴 피페라진 및 트리아졸릴 피페리딘 유도체
WO2012131539A1 (en) 2011-03-31 2012-10-04 Pfizer Inc. Novel bicyclic pyridinones
IN2014MN00258A (ru) 2011-07-15 2015-09-25 Janssen Pharmaceuticals Inc

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BR112012000915A2 (pt) 2019-09-24
US20120135981A1 (en) 2012-05-31
AU2010272578B2 (en) 2015-03-05
ZA201200285B (en) 2014-06-25
IL217491A0 (en) 2012-02-29
CN102482227A (zh) 2012-05-30
WO2011006903A1 (en) 2011-01-20
SG177644A1 (en) 2012-03-29
IL217491A (en) 2015-08-31
EP2454239B1 (en) 2014-08-13
MX2012000763A (es) 2012-02-08
EP2454239A1 (en) 2012-05-23
ES2519565T3 (es) 2014-11-07
JP2015129147A (ja) 2015-07-16
AU2010272578A1 (en) 2012-01-19
TW201109316A (en) 2011-03-16
CA2778517A1 (en) 2011-01-20
KR20120050450A (ko) 2012-05-18
JP2012532912A (ja) 2012-12-20
EA021047B1 (ru) 2015-03-31
NZ597505A (en) 2013-05-31
US8946266B2 (en) 2015-02-03

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