AU2007340944B2 - 2-aza-bicyclo[3.1.0]hexane derivatives as orexin receptor antagonists - Google Patents

2-aza-bicyclo[3.1.0]hexane derivatives as orexin receptor antagonists Download PDF

Info

Publication number
AU2007340944B2
AU2007340944B2 AU2007340944A AU2007340944A AU2007340944B2 AU 2007340944 B2 AU2007340944 B2 AU 2007340944B2 AU 2007340944 A AU2007340944 A AU 2007340944A AU 2007340944 A AU2007340944 A AU 2007340944A AU 2007340944 B2 AU2007340944 B2 AU 2007340944B2
Authority
AU
Australia
Prior art keywords
aza
bicyclo
thiazole
carboxylic acid
hex
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.)
Expired - Fee Related
Application number
AU2007340944A
Other languages
English (en)
Other versions
AU2007340944A1 (en
Inventor
Hamed Aissaoui
Christoph Boss
Markus Gude
Ralf Koberstein
Thierry Sifferlen
Daniel Trachsel
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.)
Actelion Pharmaceuticals Ltd
Original Assignee
Actelion Pharmaceuticals Ltd
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 Actelion Pharmaceuticals Ltd filed Critical Actelion Pharmaceuticals Ltd
Publication of AU2007340944A1 publication Critical patent/AU2007340944A1/en
Application granted granted Critical
Publication of AU2007340944B2 publication Critical patent/AU2007340944B2/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • 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
    • C07D513/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic 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
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/08Antiallergic agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Addiction (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Anesthesiology (AREA)
  • Vascular Medicine (AREA)
  • Reproductive Health (AREA)
AU2007340944A 2006-12-28 2007-12-28 2-aza-bicyclo[3.1.0]hexane derivatives as orexin receptor antagonists Expired - Fee Related AU2007340944B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IBPCT/IB2006/055042 2006-12-28
IB2006055042 2006-12-28
PCT/IB2007/055326 WO2008081399A2 (en) 2006-12-28 2007-12-28 2-aza-bicyclo[3.1.0]hexane derivatives as orexin receptor antagonists

Publications (2)

Publication Number Publication Date
AU2007340944A1 AU2007340944A1 (en) 2008-07-10
AU2007340944B2 true AU2007340944B2 (en) 2013-04-18

Family

ID=39343649

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2007340944A Expired - Fee Related AU2007340944B2 (en) 2006-12-28 2007-12-28 2-aza-bicyclo[3.1.0]hexane derivatives as orexin receptor antagonists

Country Status (28)

Country Link
US (1) US8288435B2 (Direct)
EP (1) EP2094690B1 (Direct)
JP (1) JP2010514751A (Direct)
KR (1) KR20090094168A (Direct)
CN (1) CN101568536B (Direct)
AR (1) AR064561A1 (Direct)
AT (1) ATE505467T1 (Direct)
AU (1) AU2007340944B2 (Direct)
BR (1) BRPI0720876A2 (Direct)
CA (1) CA2669821A1 (Direct)
CL (1) CL2007003827A1 (Direct)
CY (1) CY1111705T1 (Direct)
DE (1) DE602007013937D1 (Direct)
DK (1) DK2094690T3 (Direct)
ES (1) ES2364297T3 (Direct)
HR (1) HRP20110509T1 (Direct)
MA (1) MA31000B1 (Direct)
MX (1) MX2009006860A (Direct)
MY (1) MY157344A (Direct)
NO (1) NO20092762L (Direct)
NZ (1) NZ578642A (Direct)
PL (1) PL2094690T3 (Direct)
PT (1) PT2094690E (Direct)
RU (1) RU2460732C2 (Direct)
SI (1) SI2094690T1 (Direct)
TW (1) TW200833328A (Direct)
WO (1) WO2008081399A2 (Direct)
ZA (1) ZA200905229B (Direct)

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE602007009284D1 (de) * 2006-09-29 2010-10-28 Actelion Pharmaceuticals Ltd 3-aza-bicycloä3.1.0ühexanderivate
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.
AU2008260647A1 (en) 2007-05-23 2008-12-11 Merck Sharp & Dohme Corp. Cyclopropyl pyrrolidine orexin receptor antagonists
CN101874030B (zh) * 2007-09-24 2012-11-14 埃科特莱茵药品有限公司 用作食欲素受体拮抗剂的吡咯烷和哌啶
CA2713184A1 (en) * 2008-02-21 2009-08-27 Actelion Pharmaceuticals Ltd 2-aza-bicyclo[2.2.1]heptane derivatives
CN102015645B (zh) * 2008-04-30 2012-11-14 埃科特莱茵药品有限公司 哌啶和吡咯烷化合物
CA2739344A1 (en) * 2008-10-14 2010-04-22 Actelion Pharmaceuticals Ltd Phenethylamide derivatives and their heterocyclic analogues
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
CA2785957C (en) 2009-12-29 2015-06-16 Suven Life Sciences Limited .alpha.4.beta.2 neuronal nicotinic acetylcholine receptor ligands
PE20131162A1 (es) * 2010-09-22 2013-10-19 Eisai Randd Man Co Ltd Compuestos de ciclopropano como antagonistas del receptor de orexina
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
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
RU2014136339A (ru) 2012-02-07 2016-03-27 Иолас Терапьютикс, Инк. Замещенные пролины/пиперидины как антагонисты орексиновых рецепторов
ITMI20120424A1 (it) 2012-03-19 2013-09-20 Rottapharm Spa Composti chimici
KR101995683B1 (ko) 2012-06-04 2019-07-02 이도르시아 파마슈티컬스 리미티드 벤즈이미다졸-프롤린 유도체
JP6483610B2 (ja) * 2012-07-18 2019-03-13 ユニバーシティ オブ ノートルダム デュ ラック 5,5−ヘテロ芳香族抗感染症化合物
SG11201502493XA (en) 2012-10-10 2015-04-29 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
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
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
US9914720B2 (en) 2013-12-03 2018-03-13 Idorsia Pharmaceuticals Ltd Crystalline form of (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 and its use as orexin receptor antagonists
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
HK1225734B (en) 2013-12-04 2017-09-15 Idorsia Pharmaceuticals Ltd Use of benzimidazole-proline derivatives
TW201613864A (en) 2014-02-20 2016-04-16 Takeda Pharmaceutical Novel compounds
TW201613902A (en) 2014-08-13 2016-04-16 Eolas Therapeutics Inc Difluoropyrrolidines as orexin receptor modulators
BR112017004742B1 (pt) 2014-09-11 2022-11-29 Janssen Pharmaceutica Nv 2-azabiciclos substituídos e seu uso como moduladores de receptor de orexina
RU2703297C2 (ru) 2014-10-23 2019-10-16 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Композиции и способы для лечения бессонницы
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
CN109219606B (zh) 2016-02-12 2021-10-01 阿斯利康(瑞典)有限公司 食欲素受体调节剂的卤素取代的哌啶
BR112018016983A2 (pt) * 2016-02-26 2018-12-26 Jiangsu Hengrui Medicine Co., Ltd. nova toxina e método de preparação de intermediário da mesma
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
KR102582197B1 (ko) 2017-05-03 2023-09-22 이도르시아 파마슈티컬스 리미티드 2-([1,2,3]트리아졸-2-일)-벤조산 유도체의 제조
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
JP2023537963A (ja) 2020-08-13 2023-09-06 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 統合失調症に伴う認知機能障害に対する処置法
JP2023545808A (ja) 2020-10-13 2023-10-31 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 再加工方法
CN116783182B (zh) * 2021-02-02 2025-08-29 南京明德新药研发有限公司 四氢吡咯并环化合物及其应用
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001096302A1 (en) * 2000-06-16 2001-12-20 Smithkline Beecham P.L.C. Piperidines for use as orexin receptor antagonists

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH621126A5 (Direct) 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
CA2429258A1 (en) 2000-11-20 2002-06-13 Scios Inc. Piperidine/piperazine-type inhibitors of p38 kinase
ES2234929T3 (es) 2000-11-28 2005-07-01 Smithkline Beecham Plc Derivados de morfolina como antagonistas de los receptores de orexina.
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
CN100448874C (zh) * 2001-05-05 2009-01-07 史密斯克莱·比奇曼公司 N-芳酰基环胺
GB0111341D0 (en) 2001-05-10 2001-07-04 Bp Chem Int Ltd Novel polymerisation catalysts
CA2451464A1 (en) * 2001-06-28 2003-01-09 Smithkline Beecham P.L.C. 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
GB0130393D0 (en) 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
GB0130335D0 (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
GB0225938D0 (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
GB0225884D0 (en) 2002-11-06 2002-12-11 Glaxo Group Ltd Novel compounds
CN100432056C (zh) * 2003-03-26 2008-11-12 埃科特莱茵药品有限公司 四氢异喹啉基乙酰胺衍生物作为阿立新受体拮抗剂的应用
JP2007523846A (ja) * 2003-04-28 2007-08-23 アクテリオン ファマシューティカルズ リミテッド キノキサリノン誘導体
CA2557163C (en) * 2004-03-01 2011-08-16 Actelion Pharmaceuticals Ltd Substituted 1,2,3,4-tetrahydroisoquinoline derivatives
US20060014733A1 (en) * 2004-07-19 2006-01-19 Pfizer Inc Histamine-3 agonists and antagonists
CA2659299A1 (en) * 2006-08-15 2008-02-21 Actelion Pharmaceuticals Ltd Azetidine compounds
DE602007009284D1 (de) * 2006-09-29 2010-10-28 Actelion Pharmaceuticals Ltd 3-aza-bicycloä3.1.0ühexanderivate
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
UA99620C2 (en) 2007-05-23 2012-09-10 Мерк Шарп Энд Доме Корп. Pyridyl piperidine orexin receptor antagonists
AU2008260647A1 (en) 2007-05-23 2008-12-11 Merck Sharp & Dohme Corp. Cyclopropyl pyrrolidine orexin receptor antagonists
ATE524466T1 (de) 2007-07-03 2011-09-15 Actelion Pharmaceuticals Ltd 3-azabicycloä3.3.0üoktanverbindungen
WO2009016564A2 (en) * 2007-07-27 2009-02-05 Actelion Pharmaceuticals Ltd 2-aza-bicyclo[3.3.0]octane derivatives
AR067665A1 (es) 2007-07-27 2009-10-21 Actelion Pharmaceuticals Ltd Derivados de trans-3- aza-biciclo ( 3.1.0) hexano
CN101874030B (zh) * 2007-09-24 2012-11-14 埃科特莱茵药品有限公司 用作食欲素受体拮抗剂的吡咯烷和哌啶
CA2713184A1 (en) * 2008-02-21 2009-08-27 Actelion Pharmaceuticals Ltd 2-aza-bicyclo[2.2.1]heptane derivatives
CN102015645B (zh) * 2008-04-30 2012-11-14 埃科特莱茵药品有限公司 哌啶和吡咯烷化合物
TW200940822A (en) * 2009-05-07 2009-10-01 Wan Chi Steel Ind Co Ltd Water wheel mechanism with sun-and-planet type blade

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001096302A1 (en) * 2000-06-16 2001-12-20 Smithkline Beecham P.L.C. Piperidines for use as orexin receptor antagonists

Also Published As

Publication number Publication date
PL2094690T3 (pl) 2011-09-30
RU2460732C2 (ru) 2012-09-10
US8288435B2 (en) 2012-10-16
HK1136554A1 (en) 2010-07-02
EP2094690A2 (en) 2009-09-02
HRP20110509T1 (hr) 2011-08-31
ZA200905229B (en) 2010-10-27
AU2007340944A1 (en) 2008-07-10
CN101568536A (zh) 2009-10-28
ATE505467T1 (de) 2011-04-15
NZ578642A (en) 2012-01-12
MY157344A (en) 2016-05-31
BRPI0720876A2 (pt) 2014-03-04
KR20090094168A (ko) 2009-09-03
PT2094690E (pt) 2011-07-08
SI2094690T1 (sl) 2011-07-29
MA31000B1 (fr) 2009-12-01
RU2009128739A (ru) 2011-02-10
WO2008081399A3 (en) 2008-08-28
MX2009006860A (es) 2009-07-07
WO2008081399A2 (en) 2008-07-10
AR064561A1 (es) 2009-04-08
TW200833328A (en) 2008-08-16
JP2010514751A (ja) 2010-05-06
ES2364297T3 (es) 2011-08-30
CA2669821A1 (en) 2008-07-10
DE602007013937D1 (de) 2011-05-26
DK2094690T3 (da) 2011-07-18
US20110124636A1 (en) 2011-05-26
CN101568536B (zh) 2011-12-28
CL2007003827A1 (es) 2008-09-26
CY1111705T1 (el) 2015-10-07
EP2094690B1 (en) 2011-04-13
NO20092762L (no) 2009-07-27

Similar Documents

Publication Publication Date Title
AU2007340944B2 (en) 2-aza-bicyclo[3.1.0]hexane derivatives as orexin receptor antagonists
EP2185512B1 (en) Trans-3-aza-bicyclo[3.1.0]hexane derivatives
US8236801B2 (en) 2-aza-bicyclo[2.2.1]heptane derivatives
EP2079690B1 (en) 3-aza-bicyclo[3.1.0]hexane derivatives
US8063099B2 (en) Trans-3-aza-bicyclo[3.1.0]hexane derivatives
EP2164847B1 (en) 3-aza-bicyclo[3.3.0]octane compounds
AU2008281399A1 (en) 2-aza-bicyclo[3.3.0]octane derivatives
HK1136554B (en) 2-aza-bicyclo[3.1.0]hexane derivatives as orexin receptor antagonists

Legal Events

Date Code Title Description
DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND APPLICANT NAME TO ACTELION PHARMACEUTICALS LTD.

MK25 Application lapsed reg. 22.2i(2) - failure to pay acceptance fee