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AR064561A1 - Derivados de 2-aza-biciclo[3.1.0]hexano y su uso en la preparacion de un medicamento para el tratamiento de enfermedades relacionadas con disfunciones generales del sistema de la orexina. - Google Patents

Derivados de 2-aza-biciclo[3.1.0]hexano y su uso en la preparacion de un medicamento para el tratamiento de enfermedades relacionadas con disfunciones generales del sistema de la orexina.

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Publication number
AR064561A1
AR064561A1 ARP070105930A ARP070105930A AR064561A1 AR 064561 A1 AR064561 A1 AR 064561A1 AR P070105930 A ARP070105930 A AR P070105930A AR P070105930 A ARP070105930 A AR P070105930A AR 064561 A1 AR064561 A1 AR 064561A1
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AR
Argentina
Prior art keywords
alkyl
group
heterocyclyl
aryl
substituents
Prior art date
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ARP070105930A
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English (en)
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Actelion Pharmaceuticals Ltd
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Publication of AR064561A1 publication Critical patent/AR064561A1/es

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    • 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
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    • 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
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Abstract

Derivados 2-aza-biciclo[3.1.0]hexano de formula (1). Uso de dichos compuestos, o de sales farmacéuticamente aceptables de dichos compuestos, como medicamentos, especialmente como antagonistas del receptor orexina. Reivindicacion 1: Un compuesto de formula (1) donde A representa arilo o heterociclilo, donde el arilo o heterociclilo es no sustituido o independientemente mono- o di-sustituido, donde los sustituyentes están independientemente seleccionados del grupo que consiste en alquilo C1-4, cicloalquilo C3-6, alquinilo C2-6, alcoxi C1-4, NR2R3, halogeno y fenilo o piridilo no sustituido o independientemente mono- o di-sustituido, donde los sustituyentes están independientemente seleccionados del grupo que consiste en alquilo C1-4, alcoxi C1-4, trifluormetilo, trifluormetoxi, fluor y cloro; B representa un grupo arilo- o heterociclilo, donde el arilo o heterociclilo es no sustituido o independientemente mono-, di-, o tri-sustituido, donde los sustituyentes están independientemente seleccionados del grupo que consiste en alquilo C1-4, alcoxi C1-4, trifluormetilo, -NR2R3, -NHSO2-alquilo C1-4, -N(R2)C(O)R3 y halogeno; n representa el numero entero 0 o 1; R1 representa arilo o heterociclilo, donde el arilo o heterociclilo es no sustituido o independientemente mono-, di-, o tri-sustituido, donde los sustituyentes están seleccionados independientemente del grupo que consiste en alquilo C1-4, alcoxi C1-4, halogeno, trifluormetilo, ciano, alquiltio C1-4, alquinilo C2-6 y -NR2R3; o R1 representa un grupo 2,3-dihidro-benzofuranilo, benzo[1,3]dioxolilo, 2,3-dihidro-benzo[1,4]dioxinilo, 4H-benzo[1,3]dioxinilo, 2H-cromenilo, cromanilo, 2,3-dihidro-tieno[3,4-b][1,4]dioxinilo, un 34-dihidro-2H- benzo[1,4]oxazinilo, o un grupo 4-morfolino-fenilo, donde dichos grupos están no sustituidos o mono- o di-sustituidos, donde los sustituyentes están seleccionados independientemente del grupo que consiste en alquilo C1-4, alcoxi C1-4 y halogeno; R2 representa hidrogeno o alquilo C1-4 y R3 representa hidrogeno o alquilo C1-4 o una sal de dicho compuesto farmacéuticamente aceptable.
ARP070105930A 2006-12-28 2007-12-27 Derivados de 2-aza-biciclo[3.1.0]hexano y su uso en la preparacion de un medicamento para el tratamiento de enfermedades relacionadas con disfunciones generales del sistema de la orexina. AR064561A1 (es)

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US (1) US8288435B2 (es)
EP (1) EP2094690B1 (es)
JP (1) JP2010514751A (es)
KR (1) KR20090094168A (es)
CN (1) CN101568536B (es)
AR (1) AR064561A1 (es)
AT (1) ATE505467T1 (es)
AU (1) AU2007340944B2 (es)
BR (1) BRPI0720876A2 (es)
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NZ (1) NZ578642A (es)
PL (1) PL2094690T3 (es)
PT (1) PT2094690E (es)
RU (1) RU2460732C2 (es)
SI (1) SI2094690T1 (es)
TW (1) TW200833328A (es)
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Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008038251A2 (en) * 2006-09-29 2008-04-03 Actelion Pharmaceuticals Ltd 3-aza-bicyclo[3.1.0]hexane derivatives
ATE496043T1 (de) 2006-12-01 2011-02-15 Actelion Pharmaceuticals Ltd 3-heteroaryl (amino bzw. amido)-1- (biphenyl bzw. phenylthiazolyl) carbonylpiperdinderivate als orexinrezeptor-inhibitoren
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.
JP2010528007A (ja) 2007-05-23 2010-08-19 メルク・シャープ・エンド・ドーム・コーポレイション シクロプロピルピロリジンオレキシン受容体アンタゴニスト
WO2009040730A2 (en) * 2007-09-24 2009-04-02 Actelion Pharmaceuticals Ltd Pyrrolidines and piperidines as orexin receptor antagonists
JP2011512400A (ja) * 2008-02-21 2011-04-21 アクテリオン ファーマシューティカルズ リミテッド 2−アザ−ビシクロ[2.2.1]ヘプタン誘導体
EP2318367B1 (en) * 2008-04-30 2013-03-20 Actelion Pharmaceuticals Ltd. Piperidine and pyrrolidine compounds
RU2011119217A (ru) * 2008-10-14 2012-11-27 Актелион Фармасьютикалз Лтд Производные фенетиламида и их гетероциклические аналоги
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
MX2012006909A (es) * 2009-12-29 2012-07-10 Suven Life Sciences Ltd LIGANDOS DEL RECEPTOR NICOTINICO NEURONAL A4ß2 DE ACETILCOLINA.
US8268848B2 (en) * 2010-09-22 2012-09-18 Eisai R&D Management Co., Ltd. Cyclopropane compound
US9012489B2 (en) * 2011-08-03 2015-04-21 Boehringer Ingelheim International Gmbh Phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones and the use thereof as medicament
WO2013050938A1 (en) 2011-10-04 2013-04-11 Actelion Pharmaceuticals Ltd 3,7-diazabicyclo[3.3.1]nonane and 9-oxa-3,7-diazabicyclo[3.3.1]nonane derivatives
ITMI20112329A1 (it) * 2011-12-21 2013-06-22 Rottapharm Spa Nuovi derivati spiro amminici
SG11201404738QA (en) 2012-02-07 2014-10-30 Eolas Therapeutics Inc Substituted prolines / piperidines as orexin receptor antagonists
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
ITMI20120424A1 (it) 2012-03-19 2013-09-20 Rottapharm Spa Composti chimici
PT2855453T (pt) * 2012-06-04 2017-03-09 Actelion Pharmaceuticals Ltd Derivados de benzimidazol-prolina
KR102178590B1 (ko) 2012-07-18 2020-11-13 유니버시티 오브 노트르 담 듀락 5,5-헤테로방향족 항-감염 화합물
AU2013328301A1 (en) 2012-10-10 2015-05-28 Actelion Pharmaceuticals Ltd Orexin receptor antagonists which are [ortho bi (hetero-)aryl]-[2-(meta bi (hetero-)aryl)-pyrrolidin-1-yl]-methanone derivatives
CN105051040A (zh) 2013-03-12 2015-11-11 埃科特莱茵药品有限公司 作为食欲素受体拮抗剂的氮杂环丁烷酰胺衍生物
TW201444849A (zh) 2013-03-13 2014-12-01 Janssen Pharmaceutica Nv 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途
TWI621618B (zh) 2013-03-13 2018-04-21 比利時商健生藥品公司 經取代2-氮雜雙環類及其作為食慾素受體調控劑之用途
TW201444821A (zh) 2013-03-13 2014-12-01 Janssen Pharmaceutica Nv 經取代之哌啶化合物及其作為食慾素受體調節劑之用途
MA39163B1 (fr) 2013-12-03 2018-09-28 Idorsia Pharmaceuticals Ltd Forme cristalline de (s)-(2-(6-chloro-7-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1 -yl)(5-methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone et utilisation de celle-ci en tant qu'antagonistes des recepteurs de l'orexine
UA119151C2 (uk) 2013-12-03 2019-05-10 Ідорсія Фармасьютікалз Лтд КРИСТАЛІЧНА СОЛЬОВА ФОРМА (S)-(2-(6-ХЛОР-7-МЕТИЛ-1H-БЕНЗО[d]ІМІДАЗОЛ-2-ІЛ)-2-МЕТИЛПІРОЛІДИН-1-ІЛ)(5-МЕТОКСИ-2-(2H-1,2,3-ТРИАЗОЛ-2-ІЛ)ФЕНІЛ)МЕТАНОНУ ЯК АНТАГОНІСТ ОРЕКСИНОВОГО РЕЦЕПТОРА
MX366642B (es) 2013-12-04 2019-07-17 Idorsia Pharmaceuticals Ltd Uso de derivados de bencimidazol-prolina.
TW201613864A (en) 2014-02-20 2016-04-16 Takeda Pharmaceutical Novel compounds
WO2016025669A1 (en) 2014-08-13 2016-02-18 Eolas Therapeutics, Inc. Difluoropyrrolidines as orexin receptor modulators
MX2017003254A (es) 2014-09-11 2017-10-12 Janssen Pharmaceutica Nv 2-azabiciclos sustituidos y su uso como moduladores de receptores de orexina.
AU2015336463B2 (en) 2014-10-23 2020-06-18 Eisai R&D Management Co., Ltd. Compositions and methods for treating insomnia
CN106588900A (zh) * 2015-10-20 2017-04-26 北京康辰医药科技有限公司 一种苯并双环化合物或其药学上可接受的盐、药物组合物及其应用
WO2017139603A1 (en) 2016-02-12 2017-08-17 Astrazeneca Ab Halo-substituted piperidines as orexin receptor modulators
US10513510B2 (en) 2016-02-26 2019-12-24 Jiangsu Hengrui Medicine Co., Ltd. Toxin and method for preparing intermediate thereof
WO2017194548A1 (en) 2016-05-10 2017-11-16 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of autoimmune inflammatory diseases
JP7182562B2 (ja) 2017-05-03 2022-12-02 イドーシア ファーマシューティカルズ リミテッド 2-([1,2,3]トリアゾール-2-イル)-安息香酸誘導体の製造
WO2019057946A1 (en) 2017-09-25 2019-03-28 F. Hoffmann-La Roche Ag MULTI-CYCLIC AROMATIC COMPOUNDS AS D-FACTOR INHIBITORS
WO2020007964A1 (en) 2018-07-05 2020-01-09 Idorsia Pharmaceuticals Ltd 2-(2-azabicyclo[3.1.0]hexan-1-yl)-1h-benzimidazole derivatives
WO2020007977A1 (en) 2018-07-06 2020-01-09 Idorsia Pharmaceuticals Ltd 7-trifluoromethyl-[1,4]diazepan derivatives
WO2020099511A1 (en) 2018-11-14 2020-05-22 Idorsia Pharmaceuticals Ltd Benzimidazole-2-methyl-morpholine derivatives
US12059408B2 (en) 2020-08-13 2024-08-13 Boehringer Ingelheim International Gmbh Treatment of cognitive impairment associated with schizophrenia
WO2022078927A1 (en) 2020-10-13 2022-04-21 Boehringer Ingelheim International Gmbh Process of reworking
US20240300925A1 (en) * 2021-02-02 2024-09-12 Medshine Discovery Inc. Tetrahydropyrrolocyclic compound and application thereof
TW202400149A (zh) 2022-05-13 2024-01-01 瑞士商愛杜西亞製藥有限公司 經噻唑并芳基-甲基取代之環狀肼-n-甲醯胺衍生物
WO2025224168A1 (en) 2024-04-24 2025-10-30 Idorsia Pharmaceuticals Ltd Aryl sulfone and sulfanone derivatives as orexin receptor modulators

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH621126A5 (es) 1974-02-07 1981-01-15 Plantex Ltd
AU2381995A (en) 1994-04-29 1995-11-29 Pharmacia & Upjohn Company Methanol derivatives for treatment of retroviral infections especially hiv infections
US6677354B2 (en) 2000-06-16 2004-01-13 Smithkline Beecham P.L.C. Piperdines for use as orexin receptor antagonists
WO2002046158A2 (en) 2000-11-20 2002-06-13 Scios Inc. Piperidine/piperazine-type inhibitors of p38 kinase
JP4246490B2 (ja) 2000-11-28 2009-04-02 スミスクライン ビーチャム ピー エル シー オレキシン受容体のアンタゴニストとしてのモルホリン誘導体
HUP0400048A3 (en) 2001-05-05 2008-10-28 Smithkline Beecham Plc N-aroyl cyclic amines and pharmaceutical compositions containing them
JP2004534026A (ja) * 2001-05-05 2004-11-11 スミスクライン ビーチャム パブリック リミテッド カンパニー オレキシン受容体アンタゴニストとしてのn−アロイルサイクリックアミン誘導体
GB0111341D0 (en) 2001-05-10 2001-07-04 Bp Chem Int Ltd Novel polymerisation catalysts
EP1399441B1 (en) * 2001-06-28 2006-07-05 Smithkline Beecham Plc N-aroyl cyclic amine derivatives as orexin receptor antagonists
GB0115862D0 (en) * 2001-06-28 2001-08-22 Smithkline Beecham Plc Compounds
GB0124463D0 (en) 2001-10-11 2001-12-05 Smithkline Beecham Plc Compounds
GB0127145D0 (en) * 2001-11-10 2002-01-02 Smithkline Beecham Compounds
US6727247B2 (en) * 2001-12-10 2004-04-27 Hoffman-La Roche Inc. Substituted benzothiazole amide derivatives
GB0130335D0 (en) * 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
GB0130393D0 (en) 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
US6995144B2 (en) 2002-03-14 2006-02-07 Eisai Co., Ltd. Nitrogen containing heterocyclic compounds and medicines containing the same
JP2006504695A (ja) * 2002-09-18 2006-02-09 グラクソ グループ リミテッド オレキシン受容体アンタゴニストとしてのn−アロイル環状アミン
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
ATE435210T1 (de) * 2003-03-26 2009-07-15 Actelion Pharmaceuticals Ltd Tetrahydroisochinolylacetamidderivate zur verwendung als orexinrezeptorantagonisten
WO2004096780A1 (en) * 2003-04-28 2004-11-11 Actelion Pharmaceuticals Ltd Quinoxalinone-3- one derivatives as orexin receptor antagonists
BRPI0508263B8 (pt) * 2004-03-01 2021-05-25 Idorsia Pharmaceuticals Ltd derivados de 1, 2, 3, 4-tetra-hidro-isoquinolina, composição farmacêutica, e, uso de derivado de 1, 2, 3, 4-tetra-hidro-isoquinolina
US20060014733A1 (en) 2004-07-19 2006-01-19 Pfizer Inc Histamine-3 agonists and antagonists
AU2007285371A1 (en) 2006-08-15 2008-02-21 Actelion Pharmaceuticals Ltd. Azetidine compounds as orexin receptor antagonists
WO2008038251A2 (en) * 2006-09-29 2008-04-03 Actelion Pharmaceuticals Ltd 3-aza-bicyclo[3.1.0]hexane derivatives
ATE496043T1 (de) 2006-12-01 2011-02-15 Actelion Pharmaceuticals Ltd 3-heteroaryl (amino bzw. amido)-1- (biphenyl bzw. phenylthiazolyl) carbonylpiperdinderivate als orexinrezeptor-inhibitoren
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.
ATE483707T1 (de) 2007-05-14 2010-10-15 Actelion Pharmaceuticals Ltd 2-cyclopropylthiazolderivate
JP2010528007A (ja) 2007-05-23 2010-08-19 メルク・シャープ・エンド・ドーム・コーポレイション シクロプロピルピロリジンオレキシン受容体アンタゴニスト
EP2152690B1 (en) 2007-05-23 2012-01-11 Merck Sharp & Dohme Corp. Pyridyl piperidine orexin receptor antagonists
PL2164847T3 (pl) 2007-07-03 2012-02-29 Actelion Pharmaceuticals Ltd Związki 3-azabicyklo[3.3.0]oktanowe
AR067665A1 (es) 2007-07-27 2009-10-21 Actelion Pharmaceuticals Ltd Derivados de trans-3- aza-biciclo ( 3.1.0) hexano
CN101874028B (zh) 2007-07-27 2012-11-14 埃科特莱茵药品有限公司 2-氮杂-二环[3.3.0]辛烷衍生物
WO2009040730A2 (en) 2007-09-24 2009-04-02 Actelion Pharmaceuticals Ltd Pyrrolidines and piperidines as orexin receptor antagonists
JP2011512400A (ja) 2008-02-21 2011-04-21 アクテリオン ファーマシューティカルズ リミテッド 2−アザ−ビシクロ[2.2.1]ヘプタン誘導体
EP2318367B1 (en) 2008-04-30 2013-03-20 Actelion Pharmaceuticals Ltd. Piperidine and pyrrolidine compounds
TW200940822A (en) * 2009-05-07 2009-10-01 Wan Chi Steel Ind Co Ltd Water wheel mechanism with sun-and-planet type blade

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