CN102015636B - 作为组胺h3受体拮抗剂的氮杂环丁烷类和环丁烷类化合物 - Google Patents

作为组胺h3受体拮抗剂的氮杂环丁烷类和环丁烷类化合物 Download PDF

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CN102015636B
CN102015636B CN200980117615.XA CN200980117615A CN102015636B CN 102015636 B CN102015636 B CN 102015636B CN 200980117615 A CN200980117615 A CN 200980117615A CN 102015636 B CN102015636 B CN 102015636B
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carbonyl
cyclobutyl
azetidin
nitrae
isosorbide
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Chinese (zh)
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CN102015636A (zh
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A·J·达文波特
D·J·哈莱特
M·科尔西
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Evotec OAI AG
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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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
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    • 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
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • 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
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • 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
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    • 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
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    • 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)
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  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
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  • 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)
CN200980117615.XA 2008-05-08 2009-05-05 作为组胺h3受体拮抗剂的氮杂环丁烷类和环丁烷类化合物 Expired - Fee Related CN102015636B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP08155915.5 2008-05-08
EP08155915 2008-05-08
US13946108P 2008-12-19 2008-12-19
US61/139461 2008-12-19
PCT/EP2009/055418 WO2009135842A1 (en) 2008-05-08 2009-05-05 Azetidines and cyclobutanes as histamine h3 receptor antagonists

Publications (2)

Publication Number Publication Date
CN102015636A CN102015636A (zh) 2011-04-13
CN102015636B true CN102015636B (zh) 2014-08-13

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CN200980117615.XA Expired - Fee Related CN102015636B (zh) 2008-05-08 2009-05-05 作为组胺h3受体拮抗剂的氮杂环丁烷类和环丁烷类化合物

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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
Publication number Priority date Publication date Assignee Title
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4956359A (en) * 1985-02-28 1990-09-11 A. H. Robins Company, Inc. 3-aryloxy and 3-arylthioazetidinecarboxamides as anticonvulsants and antiepileptics
WO2003004480A2 (en) * 2001-07-02 2003-01-16 Novo Nordisk A/S Substituted piperazine and diazepanes as histamine h3 receptor agonists
WO2007049123A1 (en) * 2005-10-27 2007-05-03 Pfizer Products Inc. Histamine-3 receptor antagonists

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA861210B (en) * 1985-02-28 1987-10-28 Robins Co Inc A H 3-aryloxyazetidinecarboxamides 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
US20070142369A1 (en) 2005-12-21 2007-06-21 Margaret Van Heek Combination of an H3 antagonist/inverse agonist and an appetite suppressant
AU2007204426A1 (en) 2006-01-13 2007-07-19 F. Hoffmann-La Roche Ag Cyclohexyl piperazinyl methanone derivatives and their use as histamine H3 receptor modulators
US8106208B2 (en) 2006-05-18 2012-01-31 Albireo Ab Benzamide compounds that act as NK receptor antagonists
EA018582B1 (ru) 2007-11-20 2013-09-30 Янссен Фармацевтика Н.В. Соединения циклоалкилокси- и гетероциклоалкилоксипиридина как модуляторы гистаминового рецептора н

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4956359A (en) * 1985-02-28 1990-09-11 A. H. Robins Company, Inc. 3-aryloxy and 3-arylthioazetidinecarboxamides as anticonvulsants and antiepileptics
WO2003004480A2 (en) * 2001-07-02 2003-01-16 Novo Nordisk A/S Substituted piperazine and diazepanes as histamine h3 receptor agonists
WO2007049123A1 (en) * 2005-10-27 2007-05-03 Pfizer Products Inc. Histamine-3 receptor antagonists

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
XP002498940;略;《CHEMCATS》;20080213 *

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
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
TWI454468B (zh) 2014-10-01
EP2300422B1 (en) 2014-11-05
IL208613A (en) 2015-07-30

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