EA201401351A1 - Производные бензимидазол-пролина - Google Patents

Производные бензимидазол-пролина

Info

Publication number
EA201401351A1
EA201401351A1 EA201401351A EA201401351A EA201401351A1 EA 201401351 A1 EA201401351 A1 EA 201401351A1 EA 201401351 A EA201401351 A EA 201401351A EA 201401351 A EA201401351 A EA 201401351A EA 201401351 A1 EA201401351 A1 EA 201401351A1
Authority
EA
Eurasian Patent Office
Prior art keywords
benzimidazol
proline
derivatives
compounds
formula
Prior art date
Application number
EA201401351A
Other languages
English (en)
Other versions
EA028046B1 (ru
Inventor
Кристоф Босс
Кристине Брочи
Маркус Гуде
Бибия Хайдманн
Тьерри Зифферлен
Джоди Т. Уилльямс
Original Assignee
Актелион Фармасьютиклз Лтд.
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.)
Filing date
Publication date
Application filed by Актелион Фармасьютиклз Лтд. filed Critical Актелион Фармасьютиклз Лтд.
Publication of EA201401351A1 publication Critical patent/EA201401351A1/ru
Publication of EA028046B1 publication Critical patent/EA028046B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/14—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 three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Anesthesiology (AREA)
  • Nutrition Science (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Изобретение относится к соединениям формулы (I)где Ar, R, R, R, R, Rи (R)имеют значения, как описано в описании, к их получению, к их фармацевтически приемлемым солям, и к их применению в качестве фармацевтических средств, к фармацевтическим композициям, содержащим одно или более соединений формулы (I), и в особенности к их применению в качестве антагонистов рецептора орексина.
EA201401351A 2012-06-04 2013-06-03 Производные бензимидазол-пролина EA028046B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12170748 2012-06-04
EP13158520 2013-03-11
PCT/IB2013/054567 WO2013182972A1 (en) 2012-06-04 2013-06-03 Benzimidazole-proline derivatives

Publications (2)

Publication Number Publication Date
EA201401351A1 true EA201401351A1 (ru) 2015-05-29
EA028046B1 EA028046B1 (ru) 2017-10-31

Family

ID=48914370

Family Applications (2)

Application Number Title Priority Date Filing Date
EA201401351A EA028046B1 (ru) 2012-06-04 2013-06-03 Производные бензимидазол-пролина
EA201600366A EA029899B1 (ru) 2012-06-04 2013-06-03 Производные бензимидазол-пролина

Family Applications After (1)

Application Number Title Priority Date Filing Date
EA201600366A EA029899B1 (ru) 2012-06-04 2013-06-03 Производные бензимидазол-пролина

Country Status (33)

Country Link
US (3) US9732075B2 (ru)
EP (1) EP2855453B1 (ru)
JP (1) JP5814491B2 (ru)
KR (3) KR101689093B1 (ru)
CN (1) CN104334544B (ru)
AR (1) AR091257A1 (ru)
AU (1) AU2013273222B2 (ru)
BR (1) BR112014030173B1 (ru)
CA (1) CA2873341C (ru)
CL (1) CL2014003294A1 (ru)
CY (2) CY1118735T1 (ru)
DK (1) DK2855453T3 (ru)
EA (2) EA028046B1 (ru)
ES (1) ES2617863T3 (ru)
FR (1) FR22C1047I2 (ru)
HR (1) HRP20170351T1 (ru)
HU (2) HUE031753T2 (ru)
IL (1) IL236024A (ru)
LT (2) LT2855453T (ru)
LU (1) LUC00279I2 (ru)
MX (1) MX354102B (ru)
MY (1) MY169986A (ru)
NL (1) NL301197I2 (ru)
NO (1) NO2022044I1 (ru)
NZ (1) NZ703448A (ru)
PH (1) PH12014502540B1 (ru)
PL (1) PL2855453T3 (ru)
PT (1) PT2855453T (ru)
SG (2) SG11201408004SA (ru)
SI (1) SI2855453T1 (ru)
TW (2) TWI570120B (ru)
WO (1) WO2013182972A1 (ru)
ZA (1) ZA201409422B (ru)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101802726B1 (ko) 2010-08-24 2017-11-29 액테리온 파마슈티칼 리미티드 오렉신 수용체 안타고니스트로서의 프롤린 술폰아미드 유도체
PT2855453T (pt) 2012-06-04 2017-03-09 Actelion Pharmaceuticals Ltd Derivados de benzimidazol-prolina
WO2014057435A1 (en) 2012-10-10 2014-04-17 Actelion Pharmaceuticals Ltd Orexin receptor antagonists which are [ortho bi (hetero )aryl]-[2-(meta bi (hetero )aryl)-pyrrolidin-1-yl]-methanone derivatives
EP2970241A1 (en) 2013-03-12 2016-01-20 Actelion Pharmaceuticals Ltd. Azetidine amide derivatives as orexin receptor antagonists
EA030067B1 (ru) 2013-07-22 2018-06-29 Идорсиа Фармасьютиклз Лтд Производные 1-(пиперазин-1-ил)-2-([1,2,4]триазол-1-ил)этанона
PL3077389T3 (pl) * 2013-12-03 2018-03-30 Idorsia Pharmaceuticals Ltd KRYSTALICZNA POSTAĆ (S)-(2-(6-CHLORO-7-METYLO-1H-BENZO[D]lMIDAZOL-2-ILO)- 2-METYLOPIROLIDYN-1-YLO)(5-METOKSY-2-(2H-1,2,3-TRIAZOL-2-ILO)FENYLO)METANONU I JEJ ZASTOSOWANIE JAKO ANTAGONISTY RECEPTORA OREKSYNY
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
UA116053C2 (uk) * 2013-12-04 2018-01-25 Ідорсія Фармасьютікалз Лтд Застосування похідних бензоімідазолу-проліну
US9790220B2 (en) * 2014-02-20 2017-10-17 Takeda Pharmaceutical Company Limited Substituted cyclopentanes, tetrahydrofuranes and pyrrolidines as orexin receptor antagonists
TW201613864A (en) * 2014-02-20 2016-04-16 Takeda Pharmaceutical Novel compounds
AR103399A1 (es) 2015-01-15 2017-05-10 Actelion Pharmaceuticals Ltd Derivados de (r)-2-metil-piperazina como moduladores del receptor cxcr3
RS58349B1 (sr) * 2015-01-15 2019-03-29 Idorsia Pharmaceuticals Ltd Hidroksialkil-piperazinski derivati kao modulatori cxcr3 receptora
US10196383B2 (en) 2015-07-17 2019-02-05 Sunshine Lake Pharma Co., Ltd. Substituted quinazoline compounds and preparation and uses thereof
EP4019022B1 (en) 2015-10-01 2024-01-31 BioCryst Pharmaceuticals, Inc. Human plasma kallikrein inhibitors
WO2017088759A1 (en) 2015-11-23 2017-06-01 Sunshine Lake Pharma Co., Ltd. OCTAHYDROPYRROLO [3, 4-c] PYRROLE DERIVATIVES AND USES THEREOF
CA3059394C (en) 2017-05-03 2023-09-12 Idorsia Pharmaceuticals Ltd Preparation of 2-([1,2,3]triazol-2-yl)-benzoic acid derivatives
WO2019002344A1 (en) 2017-06-29 2019-01-03 Lonza Guangzhou Nansha Ltd. PROCESS FOR THE PREPARATION OF ALPHA-METHYL-L-PROLINE
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
CN108997308A (zh) * 2018-07-09 2018-12-14 西藏大学 一种苯并咪唑类衍生物及其制备方法和应用
WO2020099511A1 (en) 2018-11-14 2020-05-22 Idorsia Pharmaceuticals Ltd Benzimidazole-2-methyl-morpholine derivatives
CN115427037A (zh) 2020-04-19 2022-12-02 爱杜西亚药品有限公司 达立克生(daridorexant)的医药用途
CA3206870A1 (en) * 2021-02-02 2022-08-11 Wei Wei Tetrahydropyrrolocyclic compound and application thereof
WO2023160004A1 (zh) * 2022-02-25 2023-08-31 南京知和医药科技有限公司 具有镇痛活性的稠环化合物及其制备方法与用途
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
CN116239575B (zh) * 2023-03-13 2025-05-23 南开大学 一种联萘咪唑啉三齿手性配体的制法及其应用
CN118724879B (zh) * 2023-12-19 2025-02-11 南京知和医药科技有限公司 一种氘代稠环化合物及其制备方法与用途
ES3038762A1 (es) * 2024-04-12 2025-10-14 Moehs Iberica Sl Procedimiento de síntesis de ácido 5-metoxi-2-(2H-1,2,3-triazol-2yl)benzoico, sal sódica de dicho ácido como intermedio de síntesis y uso del ácido o de su sal en la preparación de daridorexant y ciertos intermedios en la síntesis del mismo
WO2026012316A1 (zh) * 2024-07-08 2026-01-15 石药集团中奇制药技术（石家庄）有限公司 苯并咪唑衍生物及其用途

Family Cites Families (78)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3282927A (en) 1964-05-21 1966-11-01 Bristol Myers Co 5-phenyl-4-thiazolylpenicillins
AUPQ253199A0 (en) 1999-08-30 1999-09-23 Fujisawa Pharmaceutical Co., Ltd. Non-prostanoid prostaglandin I2-agonist
ES2238458T3 (es) 2000-06-16 2005-09-01 Smithkline Beecham Plc Piperidinas para uso como antagonistas de los receptores de orexina.
MXPA03003039A (es) 2000-10-06 2003-10-15 Neurogen Corp Derivados de indola y bencimidazola como moduladores del receptor crf.
AU2002224885A1 (en) 2000-11-28 2002-06-11 Smithkline Beecham Plc Morpholine derivatives as antagonists of orexin receptors
EP1435955A2 (en) 2001-05-05 2004-07-14 SmithKline Beecham P.L.C. N-aroyl cyclic amine derivatives as orexin receptor antagonists
MXPA03010129A (es) 2001-05-05 2004-03-10 Smithkline Beecham Plc N-aroilaminas-ciclicas.
GB0115862D0 (en) 2001-06-28 2001-08-22 Smithkline Beecham Plc Compounds
US7470710B2 (en) 2001-06-28 2008-12-30 Smithkline Beecham P.L.C. N-aroyl cyclic amine derivatives as orexin receptor antagonists
GB0124463D0 (en) 2001-10-11 2001-12-05 Smithkline Beecham Plc Compounds
GB0127145D0 (en) 2001-11-10 2002-01-02 Smithkline Beecham Compounds
GB0130335D0 (en) 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
GB0130393D0 (en) 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
DE10240818A1 (de) 2002-08-30 2004-05-13 Grünenthal GmbH Substituierte 2-Pyrrolidin-2-yl-[1,3,4]-oxadiazol-Derivate
US20060040937A1 (en) 2002-09-18 2006-02-23 Glaxo Group Limited N-aroyl cyclic amines as orexin receptor antagonists
GB0225884D0 (en) 2002-11-06 2002-12-11 Glaxo Group Ltd Novel compounds
GB0225944D0 (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
AR044586A1 (es) 2003-06-04 2005-09-21 Aventis Pharma Sa Productos aril - heteroaromaticos, composiciones que los contienen y su utilizacion
GB0325956D0 (en) 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
US7763638B2 (en) 2004-03-01 2010-07-27 Actelion Pharmaceuticals Ltd. Substituted 1,2,3,4-tetrahydroisoquinoline derivatives
WO2005113522A1 (en) 2004-05-07 2005-12-01 Janssen Pharmaceutica, N.V. Azole carboxamide inhibitors of bacterial type iii protein secretion systems
EP1604989A1 (en) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
US20060019975A1 (en) 2004-07-23 2006-01-26 Pfizer Inc Novel piperidyl derivatives of quinazoline and isoquinoline
GB0510142D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds A1
HUP0500920A2 (en) 2005-10-05 2007-07-30 Richter Gedeon Nyrt Oxadiazole derivatives, process for their preparation and their use
CA2644010A1 (en) 2006-03-15 2007-09-20 Actelion Pharmaceuticals Ltd Tetrahydroisoquinoline derivatives to enhance memory function
EP2049110B1 (en) 2006-07-14 2014-08-20 Merck Sharp & Dohme Corp. Bridged diazepan orexin receptor antagonists
KR101113626B1 (ko) 2006-08-15 2012-02-17 액테리온 파마슈티칼 리미티드 오렉신 수용체 길항제로서 아제티딘 화합물
TW200823227A (en) 2006-09-29 2008-06-01 Actelion Pharmaceuticals Ltd 3-aza-bicyclo[3.1.0]hexane derivatives
US8124623B2 (en) 2006-11-10 2012-02-28 Actelion Pharmaceuticals Ltd. 5-hydroxymethyl-oxazolidin-2-one-derivatives and their uses as antibacterials
PE20081229A1 (es) 2006-12-01 2008-08-28 Merck & Co Inc Antagonistas de receptor de orexina de diazepam sustituido
TW200833328A (en) * 2006-12-28 2008-08-16 Actelion Pharmaceuticals Ltd 2-aza-bicyclo[3.1.0]hexane derivatives
WO2008087611A2 (en) 2007-01-19 2008-07-24 Actelion Pharmaceuticals Ltd Pyrrolidine- and piperidine- bis-amide derivatives
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.
DE602008002934D1 (de) 2007-05-14 2010-11-18 Actelion Pharmaceuticals Ltd 2-cyclopropylthiazolderivate
US7741347B2 (en) 2007-05-17 2010-06-22 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
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
GB0712888D0 (en) 2007-07-03 2007-08-15 Glaxo Group Ltd Novel compounds
ES2371514T3 (es) 2007-07-03 2012-01-04 Actelion Pharmaceuticals Ltd. Compuestos de 3-aza-biciclo[3.3.0]octano.
EA201070091A1 (ru) 2007-07-03 2010-06-30 Глэксо Груп Лимитед Производные пиперидина, пригодные в качестве антагонистов рецептора орексина
US7751938B2 (en) 2007-07-05 2010-07-06 Panasonic Corporation Robot arm control device and control method, robot, and control program
ATE493386T1 (de) 2007-07-27 2011-01-15 Actelion Pharmaceuticals Ltd Trans-3-aza-bicyclo-ä3.1.0ü-hexan-derivate
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
US8288411B2 (en) 2007-09-24 2012-10-16 Actelion Pharmaceuticals Ltd. Pyrrolidines and piperidines as orexin receptor antagonists
PE20091010A1 (es) 2007-10-10 2009-08-08 Actelion Pharmaceuticals Ltd Derivados de tetrahidroquinolina
MX2010006241A (es) 2007-12-18 2010-06-30 Actelion Pharmaceuticals Ltd Derivados de aminotriazol como agonistas de alx.
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
CN102083827A (zh) 2008-07-07 2011-06-01 埃科特莱茵药品有限公司 作为食欲素受体拮抗剂的噻唑烷化合物
WO2010038200A1 (en) 2008-10-01 2010-04-08 Actelion Pharmaceuticals Ltd Oxazolidine compounds as orexin receptor antagonists
BRPI0920183A2 (pt) 2008-10-14 2018-05-22 Actelion Pharmaceuticals Ltd derivados de fenetilamida e seus analogos heterociclicos
CA2739916A1 (en) 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,5-disubstituted piperidine orexin receptor antagonists
JP2012509912A (ja) 2008-11-26 2012-04-26 グラクソ グループ リミテッド 新規の化合物
WO2010060470A1 (en) 2008-11-26 2010-06-03 Glaxo Group Limited Piperidine derivatives useful as orexin receptor antagonists
JP2012509911A (ja) 2008-11-26 2012-04-26 グラクソ グループ リミテッド 新規の化合物
AU2009324239A1 (en) 2008-12-02 2010-06-10 Glaxo Group Limited N-{[(IR,4S,6R-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0]hept-4-yl] methyl}-2-heteroarylamine derivatives and uses thereof
AU2009324238A1 (en) 2008-12-02 2010-06-10 Glaxo Group Limited N-{[(IR,4S,6R-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0] hept-4-yl] methyl}-2-heteroarylamine derivatives and uses thereof
GB0823467D0 (en) 2008-12-23 2009-01-28 Glaxo Group Ltd Novel Compounds
JP2012522794A (ja) 2009-04-03 2012-09-27 メルク・シャープ・エンド・ドーム・コーポレイション レニン阻害薬
EA201171293A1 (ru) 2009-04-24 2012-05-30 Глэксо Груп Лимитед 3-азабицикло[4.1.0]гептаны, применяемые в качестве антагонистов орексина
WO2010143116A1 (en) 2009-06-09 2010-12-16 Actelion Pharmaceuticals Ltd Fluorinated aminotriazole derivatives
WO2011050200A1 (en) 2009-10-23 2011-04-28 Janssen Pharmaceutica Nv Fused heterocyclic compounds as orexin receptor modulators
MX2012004753A (es) 2009-10-23 2012-09-07 Janssen Pharmaceutica Nv Octahidropirrolo[3,4-c]pirrolos disustituidos como moduladores del receptor de orexina.
WO2011050202A1 (en) 2009-10-23 2011-04-28 Janssen Pharmaceutica Nv Fused heterocyclic compounds as orexin receptor modulators
CA2788363A1 (en) 2010-01-19 2011-07-28 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
KR101802726B1 (ko) 2010-08-24 2017-11-29 액테리온 파마슈티칼 리미티드 오렉신 수용체 안타고니스트로서의 프롤린 술폰아미드 유도체
WO2012039717A1 (en) 2010-09-24 2012-03-29 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
CA2815179A1 (en) 2010-11-10 2012-05-18 Actelion Pharmaceuticals Ltd Lactam derivatives useful as orexin receptor antagonists
CN103380130B (zh) 2011-02-18 2015-06-17 埃科特莱茵药品有限公司 用作为食欲素拮抗剂的新颖的吡唑和咪唑衍生物
EA024106B1 (ru) 2011-11-08 2016-08-31 Актелион Фармасьютиклз Лтд. Производные 2-(1,2,3-триазол-2-ил)бензамида и 3-(1,2,3-триазол-2-ил)пиколинамида
PT2855453T (pt) 2012-06-04 2017-03-09 Actelion Pharmaceuticals Ltd Derivados de benzimidazol-prolina
WO2014057435A1 (en) 2012-10-10 2014-04-17 Actelion Pharmaceuticals Ltd Orexin receptor antagonists which are [ortho bi (hetero )aryl]-[2-(meta bi (hetero )aryl)-pyrrolidin-1-yl]-methanone derivatives
EP2970241A1 (en) 2013-03-12 2016-01-20 Actelion Pharmaceuticals Ltd. Azetidine amide derivatives as orexin receptor antagonists
PL3077389T3 (pl) 2013-12-03 2018-03-30 Idorsia Pharmaceuticals Ltd KRYSTALICZNA POSTAĆ (S)-(2-(6-CHLORO-7-METYLO-1H-BENZO[D]lMIDAZOL-2-ILO)- 2-METYLOPIROLIDYN-1-YLO)(5-METOKSY-2-(2H-1,2,3-TRIAZOL-2-ILO)FENYLO)METANONU I JEJ ZASTOSOWANIE JAKO ANTAGONISTY RECEPTORA OREKSYNY
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
UA116053C2 (uk) * 2013-12-04 2018-01-25 Ідорсія Фармасьютікалз Лтд Застосування похідних бензоімідазолу-проліну

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