TWI454468B - 作為組織胺ｈ３受體拮抗劑之氮雜環丁烷及環丁烷 - Google Patents

作為組織胺ｈ３受體拮抗劑之氮雜環丁烷及環丁烷 Download PDF

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Publication number
TWI454468B
TWI454468B TW098115068A TW98115068A TWI454468B TW I454468 B TWI454468 B TW I454468B TW 098115068 A TW098115068 A TW 098115068A TW 98115068 A TW98115068 A TW 98115068A TW I454468 B TWI454468 B TW I454468B
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TW
Taiwan
Prior art keywords
carbonyl
cyclobutyl
azetidin
oxy
diazepane
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TW098115068A
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English (en)
Chinese (zh)
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TW201006820A (en
Inventor
Adam James Davenport
David James Hallett
Massimo Corsi
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Evotec Ag
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Publication of TWI454468B publication Critical patent/TWI454468B/zh

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW098115068A 2008-05-08 2009-05-07 作為組織胺ｈ３受體拮抗劑之氮雜環丁烷及環丁烷 TWI454468B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08155915 2008-05-08
US13946108P 2008-12-19 2008-12-19

Publications (2)

Publication Number Publication Date
TW201006820A TW201006820A (en) 2010-02-16
TWI454468B true TWI454468B (zh) 2014-10-01

Family

ID=39720542

Family Applications (1)

Application Number Title Priority Date Filing Date
TW098115068A TWI454468B (zh) 2008-05-08 2009-05-07 作為組織胺ｈ３受體拮抗劑之氮雜環丁烷及環丁烷

Country Status (9)

Country Link
US (1) US8691804B2 (https=)
EP (1) EP2300422B1 (https=)
JP (1) JP5780954B2 (https=)
CN (1) CN102015636B (https=)
BR (1) BRPI0913057A2 (https=)
CA (1) CA2721303C (https=)
IL (1) IL208613A (https=)
TW (1) TWI454468B (https=)
WO (1) WO2009135842A1 (https=)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
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SA08290520B1 (ar) 2007-08-22 2012-02-22 استرازينيكا ايه بي مشتقات سيكلو بروبيل أميد وتركيبات صيدلية تحتوي عليها لعلاج حالة مرضية سببها مستقبلات هيستامين h3
WO2010086403A1 (en) 2009-02-02 2010-08-05 Evotec Neurosciences Gmbh Azetidines as histamine h3 receptor antagonists
TW201039825A (en) 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
US20120189546A1 (en) * 2009-07-11 2012-07-26 Bayer Pharma Aktiengesellschaft Radiolabelling Method Using Cycloalkyl Groups
RU2012139082A (ru) * 2010-02-18 2014-03-27 Астразенека Аб Способы получения производных циклопропиламида и связанных с ними промежуточных соединений
SA111320581B1 (ar) * 2010-07-06 2014-06-17 استرازينيكا ايه بي مركبات (3-(4-(أمينو ميثيل ) فينوكسي أو فينيل ثيو) أزيتيدين -1- يل) (5- فينيل -1، 3، 4- أوكسا ديازول -2- يل) ميثانون
EP2694492B1 (en) 2011-02-23 2015-07-29 Suven Life Sciences Limited Novel compounds as histamine h3 receptor ligands
UY34194A (es) 2011-07-15 2013-02-28 Astrazeneca Ab ?(3-(4-(espiroheterocíclico)metil)fenoxi)azetidin-1-il)(5-(fenil)-1,3,4-oxadiazol-2-il)metanona en el tratamiento de la obesidad?
WO2013151982A1 (en) 2012-04-03 2013-10-10 Arena Pharmaceuticals, Inc. Methods and compounds useful in treating pruritus, and methods for identifying such compounds
CA2878217C (en) 2012-08-23 2016-05-17 Suven Life Sciences Limited Acrylamide compounds as histamine h3 receptor ligands
CN104603104B (zh) * 2012-09-05 2016-12-07 浙江海正药业股份有限公司 氮杂环丁烷酮化合物的晶型及其制备方法
US20230130739A1 (en) 2020-03-26 2023-04-27 Cyclerion Therapeutics, Inc. DEUTERATED sGC STIMULATORS
CN112279809A (zh) * 2020-09-23 2021-01-29 山东省海洋化工科学研究院 一种2-氰基-4-氟吡啶的制备方法
CN115073276A (zh) * 2022-07-15 2022-09-20 济南大学 一种泊沙康唑主环杂质的制备及控制方法

Citations (1)

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WO2003004480A2 (en) * 2001-07-02 2003-01-16 Novo Nordisk A/S Substituted piperazine and diazepanes as histamine h3 receptor agonists

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US4956359A (en) 1985-02-28 1990-09-11 A. H. Robins Company, Inc. 3-aryloxy and 3-arylthioazetidinecarboxamides as anticonvulsants and antiepileptics
US6559140B2 (en) 2000-03-09 2003-05-06 Abbott Laboratories Cyclic and bicyclic diamino histamine-3 receptor antagonists
DE10150310A1 (de) * 2001-10-11 2003-04-24 Bayer Ag Substituierte Piperazincyclohexancarbonsäureamide und ihre Verwendung
EP1802307B1 (en) 2004-10-15 2008-02-27 Glaxo Group Limited Pyrrolidine derivatives as histamine receptors ligands
JP2008543923A (ja) 2005-06-22 2008-12-04 ファイザー・プロダクツ・インク ヒスタミン−３受容体アンタゴニスト
US8158673B2 (en) * 2005-10-27 2012-04-17 Pfizer Inc. Histamine-3 receptor antagonists
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Also Published As

Publication number Publication date
CN102015636A (zh) 2011-04-13
US8691804B2 (en) 2014-04-08
BRPI0913057A2 (pt) 2015-10-13
WO2009135842A1 (en) 2009-11-12
US20110105459A1 (en) 2011-05-05
TW201006820A (en) 2010-02-16
CA2721303C (en) 2016-06-28
IL208613A0 (en) 2010-12-30
CN102015636B (zh) 2014-08-13
CA2721303A1 (en) 2009-11-12
JP2011519891A (ja) 2011-07-14
HK1155749A1 (en) 2012-05-25
JP5780954B2 (ja) 2015-09-16
EP2300422A1 (en) 2011-03-30
EP2300422B1 (en) 2014-11-05
IL208613A (en) 2015-07-30

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