CN103080089B - 5-ht2b受体拮抗剂 - Google Patents

5-ht2b受体拮抗剂 Download PDF

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Publication number
CN103080089B
CN103080089B CN201180041597.9A CN201180041597A CN103080089B CN 103080089 B CN103080089 B CN 103080089B CN 201180041597 A CN201180041597 A CN 201180041597A CN 103080089 B CN103080089 B CN 103080089B
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CN
China
Prior art keywords
compound
acid
mmol
fluoro
compounds
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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
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CN201180041597.9A
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English (en)
Chinese (zh)
Other versions
CN103080089A (zh
Inventor
J.W.J.F.图林
L.A.L.弗唐克
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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Publication of CN103080089A publication Critical patent/CN103080089A/zh
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Expired - Fee Related legal-status Critical Current
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • 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
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Nutrition Science (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201180041597.9A 2010-09-01 2011-08-30 5-ht2b受体拮抗剂 Expired - Fee Related CN103080089B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10174880 2010-09-01
EP10174880.4 2010-09-01
PCT/EP2011/064906 WO2012028614A1 (en) 2010-09-01 2011-08-30 5-ht2b receptor antagonists

Publications (2)

Publication Number Publication Date
CN103080089A CN103080089A (zh) 2013-05-01
CN103080089B true CN103080089B (zh) 2015-09-23

Family

ID=43127285

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201180041597.9A Expired - Fee Related CN103080089B (zh) 2010-09-01 2011-08-30 5-ht2b受体拮抗剂

Country Status (14)

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US (2) US8703958B2 (enExample)
EP (1) EP2619180B1 (enExample)
JP (1) JP5845263B2 (enExample)
KR (1) KR101815123B1 (enExample)
CN (1) CN103080089B (enExample)
AU (1) AU2011298361B2 (enExample)
BR (1) BR112013004503A2 (enExample)
CA (1) CA2806647C (enExample)
EA (1) EA020967B1 (enExample)
ES (1) ES2525515T3 (enExample)
MX (1) MX2013002409A (enExample)
SG (1) SG188233A1 (enExample)
WO (1) WO2012028614A1 (enExample)
ZA (1) ZA201301561B (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA020967B1 (ru) 2010-09-01 2015-03-31 Янссен Фармацевтика Нв Антагонисты рецептора 5-ht
CN103467596A (zh) * 2012-06-06 2013-12-25 北京大学 一个治疗肺动脉高压的新靶点
WO2015134503A1 (en) * 2014-03-04 2015-09-11 The Children's Hospital Of Philadelphia Methods for managing care of patients predisposed to progressive mitral valve diseases
CN110950843B (zh) * 2019-11-28 2022-12-27 广东东阳光药业有限公司 取代的苯酰胺衍生物及其用途

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN86105972A (zh) * 1985-08-06 1987-04-01 福多纳尔公司 新的苯甲酰胺类
US4962115A (en) * 1981-10-01 1990-10-09 Janssen Pharmaceutica N.V. Novel N-(3-hydroxy-4-piperidinyl)benzamide derivatives
WO2001093849A2 (en) * 2000-06-07 2001-12-13 Aryx Therapeutics Treatment of gastroesophageal reflux disease using piperidine derivatives
CN1918157A (zh) * 2004-01-07 2007-02-21 ARYx医疗有限公司 立体异构化合物及治疗胃肠道和中枢神经系统紊乱的方法
WO2008139152A1 (en) * 2007-05-11 2008-11-20 Sentinel Oncology Limited N-oxide-containing pharmaceutical compounds

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1183847A (en) * 1981-10-01 1985-03-12 Georges Van Daele N-(3-hydroxy-4-piperidinyl)benzamide derivatives
CA1317940C (en) * 1987-09-25 1993-05-18 Georges H. P. Van Daele Substituted n-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides
US6444477B1 (en) * 2000-11-28 2002-09-03 Pharmagene Laboratories Limited Assay method for detecting 5-HT2B antagonists
KR20080080211A (ko) 2005-12-23 2008-09-02 아스트라제네카 아베 항박테리아성 피롤로피리딘, 피롤로피리미딘 및피롤로아제핀
EA020967B1 (ru) 2010-09-01 2015-03-31 Янссен Фармацевтика Нв Антагонисты рецептора 5-ht

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4962115A (en) * 1981-10-01 1990-10-09 Janssen Pharmaceutica N.V. Novel N-(3-hydroxy-4-piperidinyl)benzamide derivatives
CN86105972A (zh) * 1985-08-06 1987-04-01 福多纳尔公司 新的苯甲酰胺类
WO2001093849A2 (en) * 2000-06-07 2001-12-13 Aryx Therapeutics Treatment of gastroesophageal reflux disease using piperidine derivatives
CN1918157A (zh) * 2004-01-07 2007-02-21 ARYx医疗有限公司 立体异构化合物及治疗胃肠道和中枢神经系统紊乱的方法
WO2008139152A1 (en) * 2007-05-11 2008-11-20 Sentinel Oncology Limited N-oxide-containing pharmaceutical compounds

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Molecular structure of two gastrokinetic compounds, cisapride and R53757: comparison with dopaminergic D2 antagonists;S. COLLIN等;《Jouranal of molecular structure》;19891201;第214卷;第159-175页 *

Also Published As

Publication number Publication date
EA020967B1 (ru) 2015-03-31
US8703958B2 (en) 2014-04-22
ZA201301561B (en) 2014-08-27
KR101815123B1 (ko) 2018-01-04
SG188233A1 (en) 2013-04-30
US9139523B2 (en) 2015-09-22
US20130172386A1 (en) 2013-07-04
EA201390312A1 (ru) 2013-07-30
BR112013004503A2 (pt) 2016-06-07
WO2012028614A1 (en) 2012-03-08
EP2619180A1 (en) 2013-07-31
ES2525515T3 (es) 2014-12-23
MX2013002409A (es) 2013-04-03
JP5845263B2 (ja) 2016-01-20
HK1182097A1 (zh) 2013-11-22
KR20130101503A (ko) 2013-09-13
AU2011298361B2 (en) 2014-03-13
CN103080089A (zh) 2013-05-01
CA2806647C (en) 2018-09-18
AU2011298361A1 (en) 2013-02-14
EP2619180B1 (en) 2014-10-08
JP2013536823A (ja) 2013-09-26
CA2806647A1 (en) 2012-03-08
US20140187585A1 (en) 2014-07-03

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