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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Child & Adolescent Psychology (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
IB2008051167 2008-03-28
IBPCT/IB2008/051167 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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200823227A (en) * 2006-09-29 2008-06-01 Actelion Pharmaceuticals Ltd 3-aza-bicyclo[3.1.0]hexane derivatives
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
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
JP5641664B2 (ja) 2009-10-30 2014-12-17 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ イミダゾ［１，２−ｂ］ピリダジン誘導体およびＰＤＥ１０阻害剤としてのそれらの使用
PH12012501556A1 (en) 2009-12-30 2012-10-22 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
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
BR112013033375B1 (pt) 2011-06-27 2022-05-10 Janssen Pharmaceutica N.V Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxa-lina, seu uso, composição farmacêutica que os compreende, processo de preparação dos mesmos, solução estéril e composto intermediário
JP2014520835A (ja) 2011-07-15 2014-08-25 ビーエーエスエフ ソシエタス・ヨーロピア 動物有害生物を駆除するための置換３−ピリジルチアゾール化合物および誘導体ｉを使用した有害生物防除方法
RU2014136339A (ru) 2012-02-07 2016-03-27 Иолас Терапьютикс, Инк. Замещенные пролины/пиперидины как антагонисты орексиновых рецепторов
US9440982B2 (en) 2012-02-07 2016-09-13 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
PT2855453T (pt) 2012-06-04 2017-03-09 Actelion Pharmaceuticals Ltd Derivados de benzimidazol-prolina
AU2013283426B2 (en) 2012-06-26 2018-02-22 Janssen Pharmaceutica Nv Combinations comprising PDE 2 inhibitors such as 1-aryl-4-methyl- [1,2,4] triazolo [4,3-a] quinoxaline compounds and PDE 10 inhibitors for use in the treatment of neurological or metabolic disorders
WO2014009305A1 (en) 2012-07-09 2014-01-16 Janssen Pharmaceutica Nv Inhibitors of phosphodiesterase 10 enzyme
WO2014015167A2 (en) * 2012-07-18 2014-01-23 University Of Notre Dame Du Lac 5,5-heteroaromatic anti-infective compounds
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
EP3180332B1 (en) 2014-08-13 2021-10-27 Eolas Therapeutics Inc. Difluoropyrrolidines as orexin receptor modulators
KR102738491B1 (ko) 2016-02-12 2024-12-03 아스트라제네카 아베 오렉신 수용체 조정제로서의 할로-치환된 피페리딘
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
CA3195702A1 (en) 2020-10-13 2022-04-21 Boehringer Ingelheim International Gmbh Process of reworking
CA3206870A1 (en) * 2021-02-02 2022-08-11 Wei Wei 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
US20060040937A1 (en) * 2002-09-18 2006-02-23 Glaxo Group Limited N-aroyl cyclic amines as orexin receptor antagonists
TW200823227A (en) * 2006-09-29 2008-06-01 Actelion Pharmaceuticals Ltd 3-aza-bicyclo[3.1.0]hexane derivatives

Also Published As

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

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FZDE Discontinued

Effective date: 20140725