ES2901418T3 - Difluoropirrolidinas como moduladores del receptor de orexina - Google Patents

Difluoropirrolidinas como moduladores del receptor de orexina Download PDF

Info

Publication number
ES2901418T3
ES2901418T3 ES15832417T ES15832417T ES2901418T3 ES 2901418 T3 ES2901418 T3 ES 2901418T3 ES 15832417 T ES15832417 T ES 15832417T ES 15832417 T ES15832417 T ES 15832417T ES 2901418 T3 ES2901418 T3 ES 2901418T3
Authority
ES
Spain
Prior art keywords
alkyl
compound
group
substituted
methyl
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES15832417T
Other languages
English (en)
Spanish (es)
Inventor
Theodore M Kamenecka
Yuanjun He
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eolas Therapeutics Inc
Original Assignee
Eolas Therapeutics Inc
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 Eolas Therapeutics Inc filed Critical Eolas Therapeutics Inc
Application granted granted Critical
Publication of ES2901418T3 publication Critical patent/ES2901418T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34Tobacco-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Anesthesiology (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
ES15832417T 2014-08-13 2015-08-13 Difluoropirrolidinas como moduladores del receptor de orexina Active ES2901418T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462037024P 2014-08-13 2014-08-13
PCT/US2015/044974 WO2016025669A1 (en) 2014-08-13 2015-08-13 Difluoropyrrolidines as orexin receptor modulators

Publications (1)

Publication Number Publication Date
ES2901418T3 true ES2901418T3 (es) 2022-03-22

Family

ID=55304607

Family Applications (1)

Application Number Title Priority Date Filing Date
ES15832417T Active ES2901418T3 (es) 2014-08-13 2015-08-13 Difluoropirrolidinas como moduladores del receptor de orexina

Country Status (8)

Country Link
US (1) US10221170B2 (cg-RX-API-DMAC7.html)
EP (1) EP3180332B1 (cg-RX-API-DMAC7.html)
JP (1) JP6663909B2 (cg-RX-API-DMAC7.html)
AR (1) AR101558A1 (cg-RX-API-DMAC7.html)
ES (1) ES2901418T3 (cg-RX-API-DMAC7.html)
TW (1) TW201613902A (cg-RX-API-DMAC7.html)
UY (1) UY36272A (cg-RX-API-DMAC7.html)
WO (1) WO2016025669A1 (cg-RX-API-DMAC7.html)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2491038B1 (en) 2009-10-23 2016-04-06 Janssen Pharmaceutica N.V. Disubstituted octahy - dropyrrolo [3,4-c]pyrroles as orexin receptor modulators
DK3414241T3 (da) 2016-02-12 2022-08-01 Astrazeneca Ab Halogensubstituerede piperidiner som orexinreceptormodulatorer
US10828302B2 (en) 2016-03-10 2020-11-10 Janssen Pharmaceutica Nv Methods of treating depression using orexin-2 receptor antagonists
CN106278918B (zh) * 2016-08-12 2018-05-11 合肥久诺医药科技有限公司 一种溴芬酸钠杂质标准品2-氨基-3-(4-溴苯甲酰基)苯甲酸的合成方法
WO2018164192A1 (ja) * 2017-03-08 2018-09-13 武田薬品工業株式会社 置換ピロリジン化合物およびその用途
US11059780B2 (en) 2017-03-08 2021-07-13 Takeda Pharmaceutical Company Limited Substituted pyrrolidine compound and use thereof
IL300063B2 (en) 2017-08-03 2024-02-01 Takeda Pharmaceuticals Co Methanesulfonamide and its use for the prevention or treatment of narcolepsy
US11319286B2 (en) 2017-08-03 2022-05-03 Takeda Pharmaceutical Company Limited Heterocyclic compound and application thereof
CN111132975B (zh) * 2017-09-28 2023-05-23 勃林格殷格翰国际有限公司 N-(2,2-二氟乙基)-n-[(嘧啶基氨基)丙基]芳基甲酰胺
JP7339250B2 (ja) 2018-06-29 2023-09-05 武田薬品工業株式会社 複素環化合物およびその用途
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
JP7379374B2 (ja) 2018-12-12 2023-11-14 武田薬品工業株式会社 複素環化合物
WO2020122093A1 (ja) 2018-12-12 2020-06-18 武田薬品工業株式会社 複素環化合物
TWI841671B (zh) 2019-01-24 2024-05-11 日商第一三共股份有限公司 具有取代基之脲化合物
CN118271298A (zh) 2019-01-31 2024-07-02 武田药品工业株式会社 杂环化合物及其用途
US11434771B2 (en) 2020-01-17 2022-09-06 Raytheon Technologies Corporation Rotor blade pair for rotational equipment
US11208892B2 (en) 2020-01-17 2021-12-28 Raytheon Technologies Corporation Rotor assembly with multiple rotor disks
US11371351B2 (en) 2020-01-17 2022-06-28 Raytheon Technologies Corporation Multi-disk bladed rotor assembly for rotational equipment
US11401814B2 (en) 2020-01-17 2022-08-02 Raytheon Technologies Corporation Rotor assembly with internal vanes
US11339673B2 (en) 2020-01-17 2022-05-24 Raytheon Technologies Corporation Rotor assembly with internal vanes
US11286781B2 (en) 2020-01-17 2022-03-29 Raytheon Technologies Corporation Multi-disk bladed rotor assembly for rotational equipment
US12029718B2 (en) 2021-11-09 2024-07-09 Cct Sciences, Llc Process for production of essentially pure delta-9-tetrahydrocannabinol

Family Cites Families (158)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4172896A (en) 1978-06-05 1979-10-30 Dainippon Pharmaceutical Co., Ltd. Methane-sulfonamide derivatives, the preparation thereof and composition comprising the same
US5049578A (en) 1990-03-09 1991-09-17 E. R. Squibb & Sons, Inc. 1-aroyl or 1-acyl-2-2pyrrolidinyl-3,5-dihydroxy alkanoic and alkenoic acids, salts, esters and lactones
GB9217295D0 (en) 1992-08-14 1992-09-30 Wellcome Found Controlled released tablets
GB9315856D0 (en) 1993-07-30 1993-09-15 Wellcome Found Stabilized pharmaceutical
US5358970A (en) 1993-08-12 1994-10-25 Burroughs Wellcome Co. Pharmaceutical composition containing bupropion hydrochloride and a stabilizer
US5541231A (en) 1993-07-30 1996-07-30 Glaxo Wellcome Inc. Stabilized Pharmaceutical
US6403609B1 (en) 1997-07-29 2002-06-11 Alcon Manufacturing, Ltd. Ophthalmic compositions containing galactomannan polymers and borate
WO1999038504A1 (en) 1998-01-29 1999-08-05 Sepracor Inc. Pharmaceutical uses of optically pure (-)-bupropion
JP4633925B2 (ja) 1998-05-08 2011-02-16 スミスクライン ビーチャム ピー エル シー フェニル尿素およびフェニルチオ尿素誘導体
WO2000047576A1 (en) 1999-02-12 2000-08-17 Smithkline Beecham Plc Cinnamide derivatives as orexin-1 receptors antagonists
JP2002536447A (ja) 1999-02-12 2002-10-29 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 フェニル尿素およびフェニルチオ尿素誘導体
JP2002536445A (ja) 1999-02-12 2002-10-29 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フェニル尿素およびフェニルチオ尿素誘導体
JP2003500386A (ja) 1999-05-24 2003-01-07 シーオーアール セラピューティクス インコーポレイテッド Xa因子阻害剤
US8889112B2 (en) 1999-09-16 2014-11-18 Ocularis Pharma, Llc Ophthalmic formulations including selective alpha 1 antagonists
CA2408343A1 (en) 2000-05-11 2002-11-07 Banyu Pharmaceutical Co., Ltd. N-acyltetrahydroisoquinoline derivatives
AU2001272476A1 (en) 2000-06-16 2001-12-24 Smithkline Beecham Plc Piperidines for use as orexin receptor antagonists
DE60108420T2 (de) 2000-11-28 2005-12-22 Smithkline Beecham P.L.C., Brentford Morpholinderivate als antagonisten an orexinrezeptoren
WO2002051232A2 (en) 2000-12-27 2002-07-04 Actelion Pharmaceuticals Ltd. Novel benzazepines and related heterocyclic derivatives
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
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
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
GB0130341D0 (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
CA2460051A1 (en) 2002-07-09 2004-01-15 Actelion Pharmaceuticals Ltd. 7,8,9,10-tetrahydro-6h-azepino, 6,7,8,9-tetrahydro-pyrido and 2,3-dihydro-2h-pyrrolo[2,1-b]-quinazolinone derivatives
WO2004026866A1 (en) 2002-09-18 2004-04-01 Glaxo Group Limited N-aroyl cyclic amines as orexin receptor antagonists
ATE496884T1 (de) 2002-10-11 2011-02-15 Actelion Pharmaceuticals Ltd Sulphonylaminoessigsaeure derivate und deren verwendung als orexin rezeptor antagoniste
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
GB0225884D0 (en) 2002-11-06 2002-12-11 Glaxo Group Ltd Novel compounds
AU2003299648A1 (en) 2002-12-12 2004-06-30 Janssen Pharmaceutica, N.V. Substituted 4-phenyl-(1,3)-dioxanes
JP4637089B2 (ja) 2003-03-26 2011-02-23 アクテリオン ファーマシューティカルズ リミテッド アセトアミド誘導体
ATE383345T1 (de) 2003-04-28 2008-01-15 Actelion Pharmaceuticals Ltd Quinoxalin-3-on-verdindungen als orexin-rezeptor antagonisten.
US6933289B2 (en) 2003-07-01 2005-08-23 Allergan, Inc. Inhibition of irritating side effects associated with use of a topical ophthalmic medication
ES2593113T3 (es) 2003-08-07 2016-12-05 Allergan, Inc. Composiciones para el suministro de agentes terapéuticos en los ojos y métodos para obtener y usar los mismos
US20050059744A1 (en) 2003-09-12 2005-03-17 Allergan, Inc. Methods and compositions for the treatment of pain and other alpha 2 adrenergic-mediated conditions
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
HRP20150371T1 (hr) 2004-03-01 2015-05-08 Actelion Pharmaceuticals Ltd. Supstituirani derivati 1,2,3,4-tetrahidroizokinolina
WO2006067224A2 (en) 2004-12-23 2006-06-29 Biovitrum Ab (Publ) Spiro-benzodioxole and spiro-benzodioxane compounds as orexin receptor antagonists
JP2008538361A (ja) 2005-04-12 2008-10-23 メルク エンド カムパニー インコーポレーテッド アミドプロポキシフェニルオレキシン受容体アンタゴニスト
JP2008541698A (ja) 2005-05-03 2008-11-27 アンサンブル ディスカバリー コーポレイション 核酸検出のためのターンオーバープローブおよびその使用
CA2609203A1 (en) 2005-05-23 2006-11-30 Merck & Co., Inc Proline bis-amide orexin receptor antagonists
WO2007019234A2 (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
CN101009515A (zh) 2006-01-24 2007-08-01 华为技术有限公司 通信终端设备管理方法及通信终端
TW200800020A (en) 2006-01-26 2008-01-01 Basf Ag Methods to use 3-pyridyl derivatives as pesticides
FR2896798A1 (fr) 2006-01-27 2007-08-03 Sanofi Aventis Sa Derives de sulfonamides, leur preparation et leur application en therapeutique
FR2896799B1 (fr) 2006-02-02 2008-03-28 Sanofi Aventis Sa Derives de sulfonamides, leur preparation et leur application en therapeutique
US20090105318A1 (en) 2006-03-29 2009-04-23 Coleman Paul J Amidoethylthioether Orexin Receptor Antagonists
WO2007116374A1 (en) 2006-04-11 2007-10-18 Actelion Pharmaceuticals Ltd Novel sulfonamide compounds
US7834028B2 (en) 2006-04-26 2010-11-16 Actelion Pharmaceuticals Ltd. Pyrazolo-tetrahydro pyridine derivatives as orexin receptor antagonists
WO2007143813A1 (en) 2006-06-16 2007-12-21 Husky Injection Molding Systems Ltd. Preventative maintenance update system
EP2049110B1 (en) 2006-07-14 2014-08-20 Merck Sharp & Dohme Corp. Bridged diazepan orexin receptor antagonists
DE602007008434D1 (de) 2006-07-14 2010-09-23 Merck Sharp & Dohme Rezeptoren
US20100029736A1 (en) 2006-07-14 2010-02-04 Merck & Co., Inc. 2-substituted proline bis-amide orexin receptor antagonists
DE602007012910D1 (de) 2006-08-15 2011-04-14 Actelion Pharmaceuticals Ltd Azetidinverbindungen als orexin-rezeptor-antagonisten
US20100029617A1 (en) 2006-08-28 2010-02-04 Actelion Pharmaceuticals Ltd. 1,4,5,6,7,8-hexahydro-1,2,5-triaza-azulene derivatives as orexin receptor antagonists
ES2350460T3 (es) 2006-09-29 2011-01-24 Actelion Pharmaceuticals Ltd. Derivados de 3-aza-biciclo[3.1.0]hexano.
PE20081229A1 (es) 2006-12-01 2008-08-28 Merck & Co Inc Antagonistas de receptor de orexina de diazepam sustituido
CA2669060A1 (en) 2006-12-01 2008-06-05 Actelion Pharmaceuticals Ltd Piperidine compounds
AU2007337659A1 (en) 2006-12-22 2008-07-03 Actelion Pharmaceuticals Ltd. 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives
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.
WO2008087611A2 (en) 2007-01-19 2008-07-24 Actelion Pharmaceuticals Ltd Pyrrolidine- and piperidine- bis-amide derivatives
AU2008223546A1 (en) 2007-03-02 2008-09-12 Merck Sharp & Dohme Corp. Bipyridine carboxamide orexin receptor antagonists
JP5138708B2 (ja) 2007-03-05 2013-02-06 エフ.ホフマン−ラ ロシュ アーゲー オレキシンアンタゴニストとしてのアミノアミド
CA2679985A1 (en) 2007-03-15 2008-09-18 F. Hoffmann-La Roche Ag Malonamides as orexin antagonists
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.
KR101158976B1 (ko) 2007-04-04 2012-06-21 에프. 호프만-라 로슈 아게 오렉신 길항제로서의 헤테로사이클
ATE483707T1 (de) 2007-05-14 2010-10-15 Actelion Pharmaceuticals Ltd 2-cyclopropylthiazolderivate
EP2150114A4 (en) 2007-05-18 2012-01-18 Merck Sharp & Dohme OXO-BRIDGED DIAZEPANOREXINE RECEPTOR ANTAGONISTS
CA2687230A1 (en) 2007-05-23 2008-12-11 Merck & Co., Inc. Cyclopropyl pyrrolidine orexin receptor antagonists
PL2152690T3 (pl) 2007-05-23 2012-06-29 Merck Sharp & Dohme Pirydylo piperydynowi antagoniści receptora oreksyny
BRPI0813218A2 (pt) 2007-07-03 2014-12-23 Actelion Pharmaceuticals Ltd Composto, composição farmacêutica que o contém como princípio ativo e uso do composto.
KR20100046047A (ko) 2007-07-27 2010-05-04 액테리온 파마슈티칼 리미티드 2-아자-비시클로[3.3.0]옥탄 유도체
JP2010534646A (ja) 2007-07-27 2010-11-11 アクテリオン ファーマシューティカルズ リミテッド トランス−3−アザ−ビシクロ[3.1.0]ヘキサン誘導体
CN101801918A (zh) 2007-08-02 2010-08-11 弗·哈夫曼-拉罗切有限公司 作为食欲肽受体拮抗剂的单酰胺衍生物
US8003797B2 (en) 2007-08-09 2011-08-23 Merck Sharp & Dohme Corp. Pyridine carboxamide orexin receptor antagonists
BRPI0823262A2 (pt) 2007-08-10 2013-09-24 Cortex Pharma Inc mÉtodo de tratamento de depressço respiratària e uso de um composto na fabricaÇço de um medicamento para o tratamento de depressço respiratària
AU2008288151A1 (en) 2007-08-15 2009-02-19 Actelion Pharmaceuticals Ltd 1,2-diamido-ethylene derivatives as orexin antagonists
WO2009040730A2 (en) 2007-09-24 2009-04-02 Actelion Pharmaceuticals Ltd Pyrrolidines and piperidines as orexin receptor antagonists
JP2011502146A (ja) 2007-10-29 2011-01-20 メルク・シャープ・エンド・ドーム・コーポレイション 置換ジアゼパンオレキシン受容体アンタゴニスト
WO2009079637A1 (en) 2007-12-18 2009-06-25 Concert Pharmaceuticals, Inc. Tetrahydroisoquinoline derivatives
CN101903372B (zh) 2007-12-21 2014-06-18 弗·哈夫曼-拉罗切有限公司 作为食欲肽受体拮抗剂的杂芳基衍生物
ATE511500T1 (de) 2008-01-21 2011-06-15 Hoffmann La Roche Sulfonamide als orexin-antagonisten
MX2010007968A (es) 2008-02-12 2010-08-04 Hoffmann La Roche Derivados de sulfonamida piperidina.
EP2247586B1 (en) 2008-02-21 2012-04-25 Actelion Pharmaceuticals Ltd. 2-aza-bicyclo[2.2.1]heptane derivatives
GB0806536D0 (en) 2008-04-10 2008-05-14 Glaxo Group Ltd Novel compounds
KR20110020906A (ko) 2008-06-11 2011-03-03 액테리온 파마슈티칼 리미티드 오렉신 수용체 안타고니스트로서의 테트라졸 화합물
WO2009153180A1 (en) 2008-06-16 2009-12-23 F. Hoffmann-La Roche Ag Heteroaromatic monoamides as orexinin receptor antagonists
EP2307417A2 (en) 2008-06-25 2011-04-13 Actelion Pharmaceuticals Ltd. 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine 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
MX2011000462A (es) 2008-07-29 2011-04-05 Hoffmann La Roche Pirrolidin-3-ilmetil-amina como antagonista de orexina.
AR072899A1 (es) 2008-08-07 2010-09-29 Merck Sharp & Dohme Derivados de terpiridina-carboxamida antagonistas de receptores de orexina, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del insomnio y la obesidad.
EP2161266A1 (en) 2008-08-22 2010-03-10 EVOTEC Neurosciences GmbH Benzofuran derivatives as orexin receptor antagonists
WO2010038200A1 (en) 2008-10-01 2010-04-08 Actelion Pharmaceuticals Ltd Oxazolidine compounds as orexin receptor antagonists
RU2011119217A (ru) 2008-10-14 2012-11-27 Актелион Фармасьютикалз Лтд Производные фенетиламида и их гетероциклические аналоги
JP2012506374A (ja) 2008-10-21 2012-03-15 メルク・シャープ・エンド・ドーム・コーポレイション 2,5−二置換ピペリジンオレキシン受容体アンタゴニスト
CA2739917A1 (en) 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,5-disubstituted morpholine orexin receptor antagonists
AU2009307920A1 (en) 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,3-disubstituted piperidine orexin receptor antagonists
CA2739927A1 (en) 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. Disubstituted azepan orexin receptor antagonists
EP2349269A4 (en) 2008-10-21 2012-04-25 Merck Sharp & Dohme 2,5-DISUBSTITUTED PIPERIDINOREXINE RECEPTOR ANTAGONISTS
WO2010048014A1 (en) 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,4-disubstituted pyrrolidine orexin receptor antagonists
EP2350010B1 (en) 2008-10-30 2014-03-26 Merck Sharp & Dohme Corp. Isonicotinamide orexin receptor antagonists
US8399494B2 (en) 2008-10-30 2013-03-19 Merck Sharp & Dohme Corp. 2,5-disubstituted phenyl carboxamide orexin receptor antagonists
WO2010051238A1 (en) 2008-10-30 2010-05-06 Merck Sharp & Dohme Corp. Pyridazine carboxamide orexin receptor antagonists
WO2010060470A1 (en) 2008-11-26 2010-06-03 Glaxo Group Limited Piperidine derivatives useful as orexin receptor antagonists
EP2358713A1 (en) 2008-11-26 2011-08-24 Glaxo Group Limited Imidazopyridazine derivatives acting as orexin antagonists
EP2358712A1 (en) 2008-11-26 2011-08-24 Glaxo Group Limited Piperidine derivatives useful as orexin receptor antagonists
KR20110091581A (ko) 2008-12-02 2011-08-11 글락소 그룹 리미티드 N-{[1r,4s,6r-3-(2-피리디닐카르보닐)-3-아자비시클로[4.1.0]헵트-4-일]메틸}-2-헤테로아릴아민 유도체 및 그의 용도
MX2011005800A (es) 2008-12-02 2011-06-20 Glaxo Group Ltd Derivados de n{[(1r,4s,6r)-3-(2-piridinilcarbonil)-3-azabiciclo[4. 1.0]hept-4-il]metil}-2-heteroarilamina y sus usos.
JP2010155827A (ja) 2008-12-04 2010-07-15 Takeda Chem Ind Ltd スピロ環化合物
GB0823467D0 (en) 2008-12-23 2009-01-28 Glaxo Group Ltd Novel Compounds
AR077525A1 (es) 2009-01-30 2011-09-07 Novartis Ag 4-aril-butan-1,3-diamidas y composiciones farmaceuticas
EA201171293A1 (ru) 2009-04-24 2012-05-30 Глэксо Груп Лимитед 3-азабицикло[4.1.0]гептаны, применяемые в качестве антагонистов орексина
WO2011005636A1 (en) 2009-07-09 2011-01-13 Merck Sharp & Dohme Corp. Tetrahydronapthyridine 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
WO2011016234A1 (en) 2009-08-04 2011-02-10 Raqualia Pharma Inc. Picolinamide derivatives as ttx-s blockers
US20120149711A1 (en) 2009-08-24 2012-06-14 Glaxo Group Limited Piperidine derivatives used as orexin antagonists
WO2011023578A1 (en) 2009-08-24 2011-03-03 Glaxo Group Limited 5-methyl-piperidine derivatives as orexin receptor antagonists for the treatment of sleep disorder
EP2491034B1 (en) 2009-10-23 2013-12-18 Janssen Pharmaceutica, N.V. Fused heterocyclic compounds as orexin receptor modulators
US9062044B2 (en) 2009-10-23 2015-06-23 Janssen Pharmaceutica Nv Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators
EP2491038B1 (en) 2009-10-23 2016-04-06 Janssen Pharmaceutica N.V. Disubstituted octahy - dropyrrolo [3,4-c]pyrroles as orexin receptor modulators
US20120196901A1 (en) 2009-10-29 2012-08-02 Merck Sharp & Dohme Corp. Tertiary amide orexin receptor antagonists
EP2504316A1 (en) 2009-11-23 2012-10-03 MSD Oss B.V. Heterocylic compounds as antagonists of the orexin receptors
WO2011073316A1 (en) 2009-12-18 2011-06-23 Novartis Ag 4-aryl-butane-1,3-diamides
ES2459496T3 (es) 2009-12-21 2014-05-09 Novartis Ag Diaza-espiro[5.5]undecanos como antagonistas del receptor de orexina
JP2013515032A (ja) 2009-12-21 2013-05-02 ノバルティス アーゲー 二置換ヘテロアリール縮合ピリジン類
WO2011138265A2 (en) 2010-05-03 2011-11-10 Evotec Ag Indole and indazole derivatives as orexin receptor antagonists
WO2011138266A1 (en) 2010-05-03 2011-11-10 Evotec Ag Indolizine and imidazopyridine derivatives as orexin receptor antagonists
WO2012081692A1 (ja) 2010-12-17 2012-06-21 大正製薬株式会社 ピラゾール誘導体
US20120165339A1 (en) 2010-12-22 2012-06-28 Eisai R&D Management Co., Ltd. Cyclopropane derivatives
US20120165331A1 (en) 2010-12-22 2012-06-28 Sangamesh Badiger Di/tri-aza-spiro-C9-C11alkanes
WO2012085852A1 (en) 2010-12-22 2012-06-28 Actelion Pharmaceuticals Ltd 3,8-diaza-bicyclo[4.2.0]oct-8-yl amides
WO2012089607A1 (en) 2010-12-28 2012-07-05 Glaxo Group Limited Novel compounds with a 3a-azabicyclo [4.1.0] heptane core acting on orexin receptors
WO2012089606A1 (en) 2010-12-28 2012-07-05 Glaxo Group Limited Azabicyclo [4.1.0] hept - 4 - yl derivatives as human orexin receptor antagonists
US9303023B2 (en) 2011-02-18 2016-04-05 Actelion Pharmaceuticals Ltd. Pyrazole and imidazole derivatives useful as orexin antagonists
WO2012114252A1 (en) 2011-02-21 2012-08-30 Actelion Pharmaceuticals Ltd Novel indole and pyrrolopyridine amides
US9586962B2 (en) 2011-04-20 2017-03-07 Janssen Pharmaceutica Nv Disubstituted octahydropyrrolo [3,4-C] pyrroles as orexin receptor modulators
WO2012153729A1 (ja) 2011-05-10 2012-11-15 大正製薬株式会社 ヘテロ芳香環誘導体
US20140228377A1 (en) 2011-07-05 2014-08-14 Taisho Pharmaceutical Co., Ltd. Methylpiperidine derivative
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
AR088352A1 (es) 2011-10-19 2014-05-28 Merck Sharp & Dohme Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
EP2768305A4 (en) 2011-10-21 2015-04-29 Merck Sharp & Dohme 2,5-DISUBSTITUTED THIOMORPHOLIN OREXINE RECEPTOR ANTAGONISTS
US9242995B2 (en) 2011-10-25 2016-01-26 Merck Sharp & Dohme Corp. Isoxazolopyridine orexin receptor antagonists
WO2013062857A1 (en) 2011-10-25 2013-05-02 Merck Sharp & Dohme Corp. Piperidinyl alkyne orexin receptor antagonists
MX343837B (es) 2011-11-08 2016-11-24 Actelion Pharmaceuticals Ltd Derivados de 2 - (1,2,3 -triazol - 2 - il) benzamida y 3 - (1,2,3 - triazol - 2 - il) picolinamida.
ITMI20112329A1 (it) 2011-12-21 2013-06-22 Rottapharm Spa Nuovi derivati spiro amminici
WO2013119639A1 (en) 2012-02-07 2013-08-15 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
EP2814798B1 (en) 2012-02-17 2019-04-03 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
TW201613891A (en) 2014-02-12 2016-04-16 Eolas Therapeutics Inc Substituted prolines / piperidines as orexin receptor antagonists

Also Published As

Publication number Publication date
AR101558A1 (es) 2016-12-28
WO2016025669A1 (en) 2016-02-18
TW201613902A (en) 2016-04-16
UY36272A (es) 2016-02-29
JP6663909B2 (ja) 2020-03-13
US10221170B2 (en) 2019-03-05
US20170226103A1 (en) 2017-08-10
EP3180332A1 (en) 2017-06-21
EP3180332A4 (en) 2018-01-24
JP2017524005A (ja) 2017-08-24
EP3180332B1 (en) 2021-10-27

Similar Documents

Publication Publication Date Title
ES2901418T3 (es) Difluoropirrolidinas como moduladores del receptor de orexina
ES2791315T3 (es) Agonistas triazoles del receptor APJ
RU2610840C2 (ru) Тиазолопиримидины
US12084437B2 (en) Halo-substituted piperidines as orexin receptor modulators
ES2974026T3 (es) Inhibidores de la interacción proteína-proteína entre KEAP1-Nrf2
JP6998204B2 (ja) Rorγtのモジュレーターとしてのトリフルオロメチルアルコール
ES2906258T3 (es) 6-aminopiridin-3-ilo tiazoles como moduladores de ROR gamma t
JP2024516633A (ja) オレキシン-2受容体アゴニスト活性を有する置換されるアミド大環状化合物
ES2834009T3 (es) Moduladores heteroaromáticos del receptor gamma huérfano relacionado con retinoides
US10494363B2 (en) Non-steroidal glucocorticoid receptor modulators for local drug delivery
HK40002227B (en) Halo-substituted piperidines as orexin receptor modulators
HK40002227A (en) Halo-substituted piperidines as orexin receptor modulators
CN119954784A (zh) 化合物、其制备方法及用途
HK40005345A (en) Heteroaromatic modulators of the retinoid-related orphan receptor gamma