CA2687321C - Pyridyl piperidine orexin receptor antagonists - Google Patents

Pyridyl piperidine orexin receptor antagonists Download PDF

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Publication number
CA2687321C
CA2687321C CA2687321A CA2687321A CA2687321C CA 2687321 C CA2687321 C CA 2687321C CA 2687321 A CA2687321 A CA 2687321A CA 2687321 A CA2687321 A CA 2687321A CA 2687321 C CA2687321 C CA 2687321C
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Prior art keywords
methyl
methylpiperidin
fluoropyridin
carbonyl
oxy
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Expired - Fee Related
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CA2687321A
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French (fr)
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CA2687321A1 (en
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Michael J. Breslin
Paul J. Coleman
Christopher D. Cox
John D. Schreier
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    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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CA2687321A 2007-05-23 2008-05-22 Pyridyl piperidine orexin receptor antagonists Expired - Fee Related CA2687321C (en)

Applications Claiming Priority (3)

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Families Citing this family (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2662612A1 (en) * 2006-09-29 2008-04-03 Actelion Pharmaceuticals Ltd 3-aza-bicyclo[3.1.0]hexane derivatives
WO2008065626A2 (en) 2006-12-01 2008-06-05 Actelion Pharmaceuticals Ltd 3-heteroaryl (amino or amido)-1- (biphenyl or phenylthiazolyl) carbonylpiperidine derivativesas orexin receptor inhibitors
CL2007003827A1 (es) 2006-12-28 2008-09-26 Actelion Pharmaceuticals Ltd Compuestos derivados de n-(2-aza-biciclo(3.1.0)hex-3-ilmetil)amida; y su uso para prevenir o tratar la depresion, neurosis, esquizofrenia, ansiedad, adicciones, epilepsia, dolor, enfermedades cardiacas, entre otras.
CL2008000836A1 (es) * 2007-03-26 2008-11-07 Actelion Pharmaceuticals Ltd Compuestos derivados de tiazolidina, antagonistas del receptor de orexina; composicion farmaceutica que los comprende; y su uso en el tratamiento de neurosis emocional, depresion grave, trastornos psicoticos, alzheimer, parkinson, dolor, entre otras.
AU2008257411B2 (en) 2007-05-23 2012-04-26 Merck Sharp & Dohme Corp. Pyridyl piperidine orexin receptor antagonists
WO2009016564A2 (en) * 2007-07-27 2009-02-05 Actelion Pharmaceuticals Ltd 2-aza-bicyclo[3.3.0]octane derivatives
WO2009040730A2 (en) * 2007-09-24 2009-04-02 Actelion Pharmaceuticals Ltd Pyrrolidines and piperidines as orexin receptor antagonists
CN101965343A (zh) * 2008-02-21 2011-02-02 埃科特莱茵药品有限公司 2-氮杂-双环[2.2.1]庚烷衍生物
GB0806536D0 (en) * 2008-04-10 2008-05-14 Glaxo Group Ltd Novel compounds
KR20100135962A (ko) * 2008-04-30 2010-12-27 액테리온 파마슈티칼 리미티드 피페리딘 및 피롤리딘 화합물
MX2010012631A (es) * 2008-05-22 2010-12-14 Merck Sharp & Dohme Procedimiento para la preparacion de un antagonista del receptor orexina.
US8546576B2 (en) * 2008-06-06 2013-10-01 Sk Biopharmaceuticals Co., Ltd. 3 or 4-substituted piperidine compounds
AU2009307915A1 (en) * 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,5-disubstituted piperidine orexin receptor antagonists
AU2009307921A1 (en) * 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. Disubstituted azepan orexin receptor antagonists
US8357700B2 (en) 2008-10-21 2013-01-22 Merck Sharp & Dohme Corp. 2,3-disubstituted piperidine orexin receptor antagonists
US8669272B2 (en) * 2008-10-21 2014-03-11 Merck Sharp & Dohme Corp. 2,5-disubstituted piperidine orexin receptor antagonists
EP2349270B1 (en) 2008-10-21 2015-09-09 Merck Sharp & Dohme Corp. 2,5-disubstituted morpholine orexin receptor antagonists
US8357709B2 (en) * 2008-10-21 2013-01-22 Merck Sharp & Dohme Corp. 2,4-disubstituted pyrrolidine orexin receptor antagonists
EP2275421A1 (en) 2009-07-15 2011-01-19 Rottapharm S.p.A. Spiro amino compounds suitable for the treatment of inter alia sleep disorders and drug addiction
JP2013502447A (ja) * 2009-08-24 2013-01-24 グラクソ グループ リミテッド 睡眠障害の治療のためのオレキシン受容体アンタゴニストとしての５−メチル−ピペリジン誘導体
WO2012058129A1 (en) * 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. Process for the preparation of an orexin receptor antagonist
EP2484674A1 (en) 2011-02-02 2012-08-08 Rottapharm S.P.A. Spiro aminic compounds with NK1 antagonist activity
WO2012114252A1 (en) * 2011-02-21 2012-08-30 Actelion Pharmaceuticals Ltd Novel indole and pyrrolopyridine amides
EP2730573A4 (en) 2011-07-05 2014-12-03 Taisho Pharmaceutical Co Ltd METHYLPIPERIDINDERIVAT
SI2736510T1 (sl) 2011-07-28 2017-05-31 Kempharm, Inc. Metilfenidat predzdravila, postopki njih izdelave in uporabe
AR088352A1 (es) * 2011-10-19 2014-05-28 Merck Sharp & Dohme Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
US9029364B2 (en) * 2011-10-21 2015-05-12 Merck Sharp & Dohme Corp. 2,5-disubstituted thiomorpholine orexin receptor antagonists
ITMI20112329A1 (it) 2011-12-21 2013-06-22 Rottapharm Spa Nuovi derivati spiro amminici
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
BR112014019426A8 (pt) * 2012-02-07 2017-07-11 Eolas Therapeutics Inc Prolinas/ piperidinas substituídas como antagonistas do receptor de orexina
US9416109B2 (en) * 2012-02-17 2016-08-16 Eisai R&D Management Co., Ltd. Methods and compounds useful in the synthesis of orexin-2 receptor antagonists
ITMI20120322A1 (it) 2012-03-01 2013-09-02 Rottapharm Spa Composti di 4,4-difluoro piperidina
ITMI20120424A1 (it) 2012-03-19 2013-09-20 Rottapharm Spa Composti chimici
RS55675B1 (sr) * 2012-06-15 2017-06-30 Taisho Pharmaceutical Co Ltd Jedinjenja 1,3-oksazolidina ili 1,3-oksazinana kao antagonisti oreksinskog receptora
EP2922543B1 (en) 2012-11-20 2017-05-24 Merck Sharp & Dohme Corp. Substituted pyridone derivatives as pde10 inhibitors
JP2016028017A (ja) * 2012-12-13 2016-02-25 大正製薬株式会社 フッ素置換ピペリジン化合物
EP2934517A4 (en) * 2012-12-20 2016-05-25 Merck Sharp & Dohme 2-PYRIDYLOXY-3-NITRIL-4-SUBSTITUTED OREXINE RECEPTOR ANTAGONISTS
WO2014099696A1 (en) * 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. 2-pyridyloxy-4-ester orexin receptor antagonists
EP2934516A4 (en) 2012-12-20 2016-07-20 Merck Sharp & Dohme 3 ESTER 4 SUBSTITUTED OREXINE RECEPTOR ANTAGONISTS
EP2945630A4 (en) 2013-01-16 2016-06-22 Merck Sharp & Dohme 4-FLUORPIPERIDINOREXIN receptor antagonists
US9828345B2 (en) 2013-02-28 2017-11-28 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors
TW201444798A (zh) 2013-02-28 2014-12-01 必治妥美雅史谷比公司 作爲強效ｒｏｃｋ１及ｒｏｃｋ２抑制劑之苯基吡唑衍生物
US9745284B2 (en) 2013-03-08 2017-08-29 Merck Sharp & Dohme Corp. 2-pyridyloxy-4-ether orexin receptor antagonists
EP2988746A1 (en) * 2013-04-23 2016-03-02 Merck Sharp & Dohme Corp. Halo and trifluoromethyl substituted orexin receptor antagonists
EP2988748A1 (en) * 2013-04-23 2016-03-02 Merck Sharp & Dohme Corp. Hydroxy-substituted orexin receptor antagonists
WO2015018029A1 (en) 2013-08-08 2015-02-12 Merck Sharp & Dohme Corp. Oxazole orexin receptor antagonists
WO2015018027A1 (en) 2013-08-08 2015-02-12 Merck Sharp & Dohme Corp. Thiazole orexin receptor antagonists
US9676751B2 (en) 2013-12-20 2017-06-13 Merck Sharp & Dohme Corp. 2-amino-3-ester-pyridl orexin receptor antagonists
SG10201900536TA (en) * 2014-03-06 2019-02-27 Shanghai Haiyan Pharmaceutical Tech Co Ltd Piperidine derivatives as orexin receptor antagonist
RU2730674C2 (ru) 2014-03-27 2020-08-24 Берд Рок Байо, Инк., Антитела, связывающиеся с человеческим каннабиноидным рецептором 1 (св1)
AR101558A1 (es) 2014-08-13 2016-12-28 Eolas Therapeutics Inc Difluoropirrolidinas como moduladores del receptor de orexina
WO2016065583A1 (en) 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Oxazole orexin receptor antagonists
WO2016065586A1 (en) 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Pyrazole, triazole and tetrazole orexin receptor antagonists
WO2016065587A1 (en) * 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Pyrazole orexin receptor antagonists
WO2016065585A1 (en) 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Piperidine isoxazole and isothiazole orexin receptor antagonists
WO2016065584A1 (en) 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Piperidine oxadiazole and thiadiazole orexin receptor antagonists
WO2016085784A1 (en) 2014-11-26 2016-06-02 Merck Sharp & Dohme Corp. Methyl diazepane orexin receptor antagonists
WO2016085783A1 (en) 2014-11-26 2016-06-02 Merck Sharp & Dohme Corp. Bridged diazepane orexin receptor antagonists
WO2016086358A1 (en) 2014-12-02 2016-06-09 Merck Sharp & Dohme Corp. Hydroxymethyl piperidine orexin receptor antagonists
WO2016086357A1 (en) 2014-12-02 2016-06-09 Merck Sharp & Dohme Corp. Methyl oxazole orexin receptor antagonists
US9938276B2 (en) 2014-12-19 2018-04-10 Merck Sharp & Dohme Corp. 6,5-bicyclic octahydropyrrolopyridine orexin receptor antagonists
WO2016095204A1 (en) 2014-12-19 2016-06-23 Merck Sharp & Dohme Corp. Pyrrolidine orexin receptor antagonists
WO2016100161A1 (en) * 2014-12-19 2016-06-23 Merck Sharp & Dohme Corp. Ethyldiamine orexin receptor antagonists
WO2016095205A1 (en) 2014-12-19 2016-06-23 Merck Sharp & Dohme Corp. Heteroaryl orexin receptor antagonists
WO2016100162A2 (en) 2014-12-19 2016-06-23 Merck Sharp & Dohme Corp. 5,5-bicyclic oxazole orexin receptor antagonists
WO2016101119A1 (en) 2014-12-23 2016-06-30 Merck Sharp & Dohme Corp. Fused heteroaryl derivatives as orexin receptor antagonists
WO2016101118A1 (en) 2014-12-23 2016-06-30 Merck Sharp & Dohme Corp. Amidoethyl azole orexin receptor antagonists
CN106349228B (zh) 2015-07-17 2019-07-09 广东东阳光药业有限公司 取代的喹唑啉酮类化合物及其制备方法和用途
WO2017028732A1 (zh) * 2015-08-14 2017-02-23 上海海雁医药科技有限公司 食欲素受体拮抗剂化合物的晶型及其制备方法和应用
EP3341012B1 (en) * 2015-08-25 2025-07-30 Armo Biosciences, Inc. Methods of using interleukin-10 for treating diseases and disorders
CA3000167A1 (en) 2015-09-30 2017-04-06 Bird Rock Bio, Inc. Antibodies that bind human cannabinoid 1 (cb1) receptor
SI3411358T1 (sl) * 2016-02-04 2022-04-29 Takeda Pharmaceutical Company Limited Substituirana piperidinska spojina in njena uporaba
US10894789B2 (en) 2016-02-12 2021-01-19 Astrazeneca Ab Halo-substituted piperidines as orexin receptor modulators
US20190151304A1 (en) 2016-05-10 2019-05-23 Inserm (Institut National De La Santé Et De La Rechercjae Médicale Methods and pharmaceutical compositions for the treatment of autoimmune inflammatory
BR112019011640B1 (pt) 2016-12-11 2021-08-17 Kempharm, Inc Compostos conjugados de d-metilfenidato, composições que compreendem os mesmos e kit farmacêutico que compreende as ditas composições
WO2020004537A1 (ja) * 2018-06-29 2020-01-02 武田薬品工業株式会社 複素環化合物およびその用途
EP3924058B1 (en) 2019-02-13 2026-01-07 Merck Sharp & Dohme LLC 5-alkyl pyrrolidine orexin receptor agonists
AU2020286381C1 (en) 2019-06-04 2025-07-10 Hager Biosciences, Llc Imidazolo derivatives, compositions and methods as orexin antagonists
KR20250036472A (ko) 2023-09-07 2025-03-14 경희대학교 산학협력단 Cid16020046의 체중감소 효능과 비만치료제로 적용

Family Cites Families (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA848275B (en) 1983-12-28 1985-08-28 Degussa New piridine-2-ethers or pyridine-2-thioethers having a nitrogen-containing cycloaliphatic ring
AR016817A1 (es) 1997-08-14 2001-08-01 Smithkline Beecham Plc Derivados de fenilurea o feniltiourea, procedimiento para su preparacion, coleccion de compuestos, compuestos intermediarios, composicion farmaceutica,metodo de tratamiento y uso de dichos compuestos para la manufactura de un medicamento
DE69906960T2 (de) 1998-05-08 2004-01-29 Smithkline Beecham Plc Phenylurea und phenylthio urea derivate
ES2231158T3 (es) 1999-02-12 2005-05-16 Smithkline Beecham Plc Derivados y fenil urea y fenil tiourea.
WO2000047576A1 (en) 1999-02-12 2000-08-17 Smithkline Beecham Plc Cinnamide derivatives as orexin-1 receptors antagonists
AU2804400A (en) 1999-02-12 2000-08-29 Smithkline Beecham Plc Phenyl urea and phenyl thiourea derivatives as orexin receptor antagonists
US6784192B2 (en) 2000-01-20 2004-08-31 Eisai Co., Ltd. Piperidine compound and pharmaceutical composition thereof
ES2234840T3 (es) 2000-03-14 2005-07-01 Actelion Pharmaceuticals Ltd. Derivados de 1,2,3,4- tetrahidroisoquinolina.
US6838465B2 (en) 2000-05-11 2005-01-04 Banyu Pharmaceutical Co., Ltd. N-acyltetrahydroisoquinoline derivatives
US6677354B2 (en) 2000-06-16 2004-01-13 Smithkline Beecham P.L.C. Piperdines for use as orexin receptor antagonists
ATE286897T1 (de) 2000-11-28 2005-01-15 Smithkline Beecham Plc Morpholinderivate als antagonisten an orexinrezeptoren
WO2002051232A2 (en) 2000-12-27 2002-07-04 Actelion Pharmaceuticals Ltd. Novel benzazepines and related heterocyclic derivatives
WO2002089800A2 (en) 2001-05-05 2002-11-14 Smithkline Beecham P.L.C. N-aroyl cyclic amine derivatives as orexin receptor antagonists
CN100448874C (zh) 2001-05-05 2009-01-07 史密斯克莱·比奇曼公司 N-芳酰基环胺
GB0115862D0 (en) 2001-06-28 2001-08-22 Smithkline Beecham Plc Compounds
ES2266549T3 (es) 2001-06-28 2007-03-01 Smithkline Beecham Plc Derivados de n-aroil-amina ciclicos como antagonistas del receptor de orexina.
GB0124463D0 (en) 2001-10-11 2001-12-05 Smithkline Beecham Plc Compounds
GB0126292D0 (en) 2001-11-01 2002-01-02 Smithkline Beecham Plc Compounds
GB0127145D0 (en) 2001-11-10 2002-01-02 Smithkline Beecham Compounds
GB0130388D0 (en) 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
GB0130393D0 (en) 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
GB0130335D0 (en) 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
GB0130341D0 (en) 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
TWI283241B (en) 2002-05-29 2007-07-01 Tanabe Seiyaku Co Novel piperidine compound
RU2294927C2 (ru) * 2002-05-29 2007-03-10 Танабе Сейяку Ко., Лтд. Производные пиперидина, способы их получения, фармацевтическая композиция на их основе, их применение и способ лечения
ITMI20021273A1 (it) * 2002-06-11 2003-12-11 Milano Politecnico Sistema e metodo per la rilevazione automatica della limitazione del flusso espiratorio
RU2005103398A (ru) 2002-07-09 2006-06-27 Актелион Фармасьютикалз Лтд. (Ch) Производные 7,8,9,10-тетрагидро-6h-азепино-, 6,7,8,9-тетрагидропиридо-и 2,3-дигидро-2h-пирроло-[2,1-b]-хиназолинона
AU2003262516A1 (en) 2002-09-18 2004-04-08 Glaxo Group Limited N-aroyl cyclic amines as orexin receptor antagonists
CA2500317A1 (en) 2002-10-08 2004-04-22 Merck Frosst Canada & Co. 4-amino-azepan-3-one compounds as cathepsin k inhibitors useful in the treatment of osteoporosis
AU2003294671A1 (en) 2002-10-11 2004-05-04 Actelion Pharmaceuticals Ltd. Sulfonylamino-acetic derivatives and their use as orexin receptor antagonists
GB0225944D0 (en) 2002-11-06 2002-12-11 Glaxo Group Ltd Novel compounds
GB0225884D0 (en) 2002-11-06 2002-12-11 Glaxo Group Ltd Novel compounds
GB0225938D0 (en) 2002-11-06 2002-12-11 Glaxo Group Ltd Novel compounds
US6951882B2 (en) 2002-12-12 2005-10-04 Janssen Pharmaceutica N.V. Substituted 4-phenyl-[1,3]-dioxanes
CL2004000553A1 (es) 2003-03-20 2005-02-04 Actelion Pharmaceuticals Ltd Uso de compuestos derivados de guanidina como antagonistas del receptor de neuropeptido ff; compuestos derivados de guanidina; procedimientos de preparacion; y composicion farmaceutica que los comprende.
EP1611104B1 (en) 2003-03-26 2009-07-01 Actelion Pharmaceuticals Ltd. Tetrahydroisoquinolyl acetamide derivatives for use as orexin receptor antagonists
JO2355B1 (en) 2003-04-15 2006-12-12 ميرك شارب اند دوم كوربوريشن Hereditary calcitonin polypeptide receptor antagonists
CN1780820A (zh) 2003-04-28 2006-05-31 埃科特莱茵药品有限公司 作为阿立新受体拮抗剂的喹喔啉－3－酮衍生物
HUP0304101A3 (en) 2003-12-22 2008-10-28 Sanofi Aventis Pyrazole derivatives, process for producing them, their use, pharmaceutical compositions containing them and their intermediates
HUP0400405A3 (en) 2004-02-10 2009-03-30 Sanofi Synthelabo Pyrimidine derivatives, process for producing them, their use, pharmaceutical compositions containing them and their intermediates
SI1751111T1 (sl) 2004-03-01 2015-04-30 Actelion Pharmaceuticals Ltd. Substituirani 1,2,3,4-tetrahidroizokinolinski derivati
WO2006067224A2 (en) 2004-12-23 2006-06-29 Biovitrum Ab (Publ) Spiro-benzodioxole and spiro-benzodioxane compounds as orexin receptor antagonists
DE102004062544A1 (de) 2004-12-24 2006-07-06 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Pyrrolidinone, deren Herstellung und deren Verewendung als Arzneimittel
WO2006110626A1 (en) 2005-04-12 2006-10-19 Merck & Co., Inc. Amidopropoxyphenyl orexin receptor antagonists
US20090215742A1 (en) 2005-05-03 2009-08-27 Pfizer, Inc. Amide resorcinol compounds
US20090118200A1 (en) 2005-05-23 2009-05-07 Bergman Jeffrey M Proline bis-amide orexin receptor antagonists
CA2617324A1 (en) 2005-08-04 2007-02-15 Merck & Co., Inc. Aminoethane sulfonamide orexin receptor antagonists
CA2620124A1 (en) 2005-08-26 2007-03-01 Merck And Co., Inc. Diazaspirodecane orexin receptor antagonists
AU2006316321A1 (en) 2005-11-22 2007-05-31 Merck & Co., Inc. Indole orexin receptor antagonists
US20090105318A1 (en) 2006-03-29 2009-04-23 Coleman Paul J Amidoethylthioether Orexin Receptor Antagonists
WO2007126935A2 (en) 2006-03-29 2007-11-08 Merck & Co., Inc. Diazepan orexin receptor antagonists
CA2646917A1 (en) 2006-04-11 2007-10-18 Actelion Pharmaceuticals Ltd Novel sulfonamide compounds
WO2007122591A2 (en) 2006-04-26 2007-11-01 Actelion Pharmaceuticals Ltd Pyrazolo-tetrahydro pyridine derivatives as orexin receptor antagonists
US20100029736A1 (en) 2006-07-14 2010-02-04 Merck & Co., Inc. 2-substituted proline bis-amide orexin receptor antagonists
JP2009543785A (ja) 2006-07-14 2009-12-10 メルク エンド カムパニー インコーポレーテッド 架橋ジアゼパンオレキシン受容体アンタゴニスト
EP2049529B1 (en) 2006-07-14 2010-08-11 Merck Sharp & Dohme Corp. Substituted diazepan orexin receptor antagonists
RU2447070C2 (ru) 2006-08-15 2012-04-10 Актелион Фармасьютиклз Лтд Соединения азетидина в качестве антагонистов рецептора орексина
ES2339822T3 (es) 2006-08-28 2010-05-25 Actelion Pharmaceuticals Ltd. Derivados de 1,4,5,6,7,8-hexahidro-1,2,5-triaza-azuleno como antagonistas del receptor de orexina.
CA2662612A1 (en) 2006-09-29 2008-04-03 Actelion Pharmaceuticals Ltd 3-aza-bicyclo[3.1.0]hexane derivatives
PE20081229A1 (es) 2006-12-01 2008-08-28 Merck & Co Inc Antagonistas de receptor de orexina de diazepam sustituido
WO2008065626A2 (en) 2006-12-01 2008-06-05 Actelion Pharmaceuticals Ltd 3-heteroaryl (amino or amido)-1- (biphenyl or phenylthiazolyl) carbonylpiperidine derivativesas orexin receptor inhibitors
AU2008257411B2 (en) 2007-05-23 2012-04-26 Merck Sharp & Dohme Corp. Pyridyl piperidine orexin receptor antagonists
GB0806536D0 (en) 2008-04-10 2008-05-14 Glaxo Group Ltd Novel compounds
MX2010012631A (es) 2008-05-22 2010-12-14 Merck Sharp & Dohme Procedimiento para la preparacion de un antagonista del receptor orexina.
US8669272B2 (en) 2008-10-21 2014-03-11 Merck Sharp & Dohme Corp. 2,5-disubstituted piperidine orexin receptor antagonists
US8357700B2 (en) 2008-10-21 2013-01-22 Merck Sharp & Dohme Corp. 2,3-disubstituted piperidine orexin receptor antagonists
AU2009307915A1 (en) 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,5-disubstituted piperidine orexin receptor antagonists
AU2009307921A1 (en) 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. Disubstituted azepan orexin receptor antagonists
EP2349270B1 (en) 2008-10-21 2015-09-09 Merck Sharp & Dohme Corp. 2,5-disubstituted morpholine orexin receptor antagonists
US8357709B2 (en) 2008-10-21 2013-01-22 Merck Sharp & Dohme Corp. 2,4-disubstituted pyrrolidine orexin receptor antagonists
GB0823467D0 (en) 2008-12-23 2009-01-28 Glaxo Group Ltd Novel Compounds
JP2013502447A (ja) 2009-08-24 2013-01-24 グラクソ グループ リミテッド 睡眠障害の治療のためのオレキシン受容体アンタゴニストとしての５−メチル−ピペリジン誘導体

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