CA2693817A1 - Trans-3-aza-bicyclo[3.1.0]hexane derivatives - Google Patents

Trans-3-aza-bicyclo[3.1.0]hexane derivatives Download PDF

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Publication number
CA2693817A1
CA2693817A1 CA2693817A CA2693817A CA2693817A1 CA 2693817 A1 CA2693817 A1 CA 2693817A1 CA 2693817 A CA2693817 A CA 2693817A CA 2693817 A CA2693817 A CA 2693817A CA 2693817 A1 CA2693817 A1 CA 2693817A1
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CA
Canada
Prior art keywords
methyl
aza
bicyclo
thiazole
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.)
Abandoned
Application number
CA2693817A
Other languages
English (en)
French (fr)
Inventor
Hamed Aissaoui
Christoph Boss
Markus Gude
Ralf Koberstein
David Lehmann
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
Individual
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 Individual filed Critical Individual
Publication of CA2693817A1 publication Critical patent/CA2693817A1/en
Abandoned legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • 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
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • 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
    • A61P25/14Drugs 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
    • A61P25/20Hypnotics; 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
    • 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
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • 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
    • 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
    • A61P9/10Drugs 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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Anesthesiology (AREA)
  • Addiction (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
CA2693817A 2007-07-27 2008-07-25 Trans-3-aza-bicyclo[3.1.0]hexane derivatives Abandoned CA2693817A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
IB2007052987 2007-07-27
IBPCT/IB2007/052987 2007-07-27
IBPCT/IB2008/051167 2008-03-28
IB2008051167 2008-03-28
PCT/IB2008/052985 WO2009016560A2 (en) 2007-07-27 2008-07-25 Trans-3-aza-bicyclo[3.1.0]hexane derivatives

Publications (1)

Publication Number Publication Date
CA2693817A1 true CA2693817A1 (en) 2009-02-05

Family

ID=40130778

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2693817A Abandoned CA2693817A1 (en) 2007-07-27 2008-07-25 Trans-3-aza-bicyclo[3.1.0]hexane derivatives

Country Status (8)

Country Link
EP (1) EP2185512B1 (enExample)
JP (1) JP2010534646A (enExample)
CN (1) CN101790515A (enExample)
AT (1) ATE493386T1 (enExample)
CA (1) CA2693817A1 (enExample)
DE (1) DE602008004265D1 (enExample)
TW (1) TW200904799A (enExample)
WO (1) WO2009016560A2 (enExample)

Families Citing this family (30)

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KR20090077051A (ko) * 2006-09-29 2009-07-14 액테리온 파마슈티칼 리미티드 3-아자-비시클로[3.1.0]헥산 유도체
WO2008150364A1 (en) 2007-05-23 2008-12-11 Merck & Co., Inc. Cyclopropyl pyrrolidine orexin receptor antagonists
EP2275421A1 (en) 2009-07-15 2011-01-19 Rottapharm S.p.A. Spiro amino compounds suitable for the treatment of inter alia sleep disorders and drug addiction
EP2493889B1 (en) 2009-10-30 2017-09-06 Janssen Pharmaceutica, N.V. IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS
AU2010339531A1 (en) 2009-12-30 2012-08-23 Arqule, Inc. Substituted naphthalenyl-pyrimidine compounds
AR080754A1 (es) 2010-03-09 2012-05-09 Janssen Pharmaceutica Nv Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10
ES2541531T3 (es) 2011-02-18 2015-07-21 Actelion Pharmaceuticals Ltd. Nuevos derivados de pirazol e imidazol útiles como antagonistas de orexina
MX344600B (es) 2011-06-27 2016-12-20 Janssen Pharmaceutica Nv Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxalina.
EP2731426A2 (en) 2011-07-15 2014-05-21 Basf Se Pesticidal methods using substituted 3-pyridyl thiazole compounds and derivatives for combating animal pests ii
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
NZ628491A (en) 2012-02-07 2016-06-24 Eolas Therapeutics Inc Substituted prolines / piperidines as orexin receptor antagonists
ITMI20120322A1 (it) 2012-03-01 2013-09-02 Rottapharm Spa Composti di 4,4-difluoro piperidina
HRP20170351T1 (hr) 2012-06-04 2017-04-21 Actelion Pharmaceuticals Ltd. Derivati benzimidazol-prolina
HK1206250A1 (en) 2012-06-26 2016-01-08 Janssen Pharmaceutica Nv Combinations comprising pde 2 inhibitors such as 1-aryl-4-methyl-[1,2,4] triazolo [4,3-a] quinoxaline compounds and ped 10 inhibitors for use in the treatment of neurological or metabolic disorders
CN104411314B (zh) 2012-07-09 2017-10-20 詹森药业有限公司 磷酸二酯酶10的抑制剂
WO2014015167A2 (en) * 2012-07-18 2014-01-23 University Of Notre Dame Du Lac 5,5-heteroaromatic anti-infective compounds
EP2906553B1 (en) 2012-10-10 2019-06-26 Idorsia Pharmaceuticals Ltd Orexin receptor antagonists which are [ortho bi (hetero )aryl]-[2-(meta bi (hetero)aryl)-pyrrolidin-1-yl]-methanone derivatives
WO2014141065A1 (en) 2013-03-12 2014-09-18 Actelion Pharmaceuticals Ltd Azetidine amide derivatives as orexin receptor antagonists
NO3077389T3 (enExample) 2013-12-03 2018-02-10
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
HRP20181710T1 (hr) 2013-12-04 2018-12-28 Idorsia Pharmaceuticals Ltd Uporaba derivata benzimidazol-prolina
JP6663909B2 (ja) 2014-08-13 2020-03-13 エオラス セラピューティクス, インコーポレイテッド オレキシンレセプターモジュレーターとしてのジフルオロピロリジン
SI3414241T1 (sl) 2016-02-12 2022-10-28 Astrazeneca Ab Halo-substituitani piperidini kot modulatorji receptorja oreksina
WO2020007964A1 (en) 2018-07-05 2020-01-09 Idorsia Pharmaceuticals Ltd 2-(2-azabicyclo[3.1.0]hexan-1-yl)-1h-benzimidazole derivatives
WO2020099511A1 (en) 2018-11-14 2020-05-22 Idorsia Pharmaceuticals Ltd Benzimidazole-2-methyl-morpholine derivatives
BR112022026698A2 (pt) 2020-08-13 2023-02-23 Boehringer Ingelheim Int Tratamento da deficiência cognitiva associada à esquizofrenia
CN117567449A (zh) 2020-10-13 2024-02-20 勃林格殷格翰国际有限公司 再加工方法
EP4289834B1 (en) * 2021-02-02 2025-11-26 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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0130335D0 (en) * 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
DE60309481T2 (de) * 2002-09-18 2007-06-21 Glaxo Group Ltd., Greenford Cyclische n-aroylamine als orexinrezeptorantagonisten
KR20090077051A (ko) * 2006-09-29 2009-07-14 액테리온 파마슈티칼 리미티드 3-아자-비시클로[3.1.0]헥산 유도체

Also Published As

Publication number Publication date
EP2185512A2 (en) 2010-05-19
CN101790515A (zh) 2010-07-28
TW200904799A (en) 2009-02-01
DE602008004265D1 (de) 2011-02-10
ATE493386T1 (de) 2011-01-15
WO2009016560A3 (en) 2009-03-26
JP2010534646A (ja) 2010-11-11
WO2009016560A2 (en) 2009-02-05
EP2185512B1 (en) 2010-12-29

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Effective date: 20140725