ES2054872T3 - Nuevos derivados de acido bencimidazolin-2-oxo-1-carboxilico utiles como antagonistas de los receptores 5-ht. - Google Patents

Nuevos derivados de acido bencimidazolin-2-oxo-1-carboxilico utiles como antagonistas de los receptores 5-ht.

Info

Publication number
ES2054872T3
ES2054872T3 ES88830375T ES88830375T ES2054872T3 ES 2054872 T3 ES2054872 T3 ES 2054872T3 ES 88830375 T ES88830375 T ES 88830375T ES 88830375 T ES88830375 T ES 88830375T ES 2054872 T3 ES2054872 T3 ES 2054872T3
Authority
ES
Spain
Prior art keywords
antagonists
oxo
bencimidazolin
receptors
carboxylic acid
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.)
Expired - Lifetime
Application number
ES88830375T
Other languages
English (en)
Inventor
Marco Turconi
Arturo Donetti
Rosamaria Micheletti
Annamaria Uberti
Massimo Nicola
Antonio Giachetti
Ernesto Montagna
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.)
Boehringer Ingelheim Italia SpA
Original Assignee
Boehringer Ingelheim Italia SpA
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 Boehringer Ingelheim Italia SpA filed Critical Boehringer Ingelheim Italia SpA
Application granted granted Critical
Publication of ES2054872T3 publication Critical patent/ES2054872T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06Oxygen atoms
    • C07D451/12Oxygen atoms acylated by aromatic or heteroaromatic carboxylic acids, e.g. cocaine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/14Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/06Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing isoquinuclidine ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (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)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

NUEVOS DERIVADOS FARMACOLOGICAMENTE ACTIVOS DE BENZIMIDAZOLINE - 2 - OXO - 1 - CARBOXILICO QUE SON ANTAGONISTAS DEL RECEPTOR 5 HT UTILES COMO AGENTES ANTIEMITICOS Y AGENTES PROCINETICOS GASTRICOS, DE LA FORMULA(I), DONDE TODOS LOS SUSTITUYENTES APARECEN EXPLICADOS TAMBIEN EN LA INVENCION. EL PROCESO DE LA PREPARACION DE LOS COMPUESTOS DE LA FORMULA(I) COMO TAMBIEN LAS COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN TAMBIEN ESTAN DESCRITAS.
ES88830375T 1987-09-23 1988-09-19 Nuevos derivados de acido bencimidazolin-2-oxo-1-carboxilico utiles como antagonistas de los receptores 5-ht. Expired - Lifetime ES2054872T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IT8721997A IT1231413B (it) 1987-09-23 1987-09-23 Derivati dell'acido benzimidazolin-2-osso-1-carbossilico utili come antagonisti dei recettori 5-ht

Publications (1)

Publication Number Publication Date
ES2054872T3 true ES2054872T3 (es) 1994-08-16

Family

ID=11189966

Family Applications (1)

Application Number Title Priority Date Filing Date
ES88830375T Expired - Lifetime ES2054872T3 (es) 1987-09-23 1988-09-19 Nuevos derivados de acido bencimidazolin-2-oxo-1-carboxilico utiles como antagonistas de los receptores 5-ht.

Country Status (28)

Country Link
EP (1) EP0309423B1 (es)
JP (1) JPH0631225B2 (es)
KR (1) KR960003604B1 (es)
AT (1) ATE107305T1 (es)
BR (1) BR1100514A (es)
CA (1) CA1337347C (es)
CZ (1) CZ279864B6 (es)
DD (1) DD285354A5 (es)
DE (1) DE3850203T2 (es)
DK (1) DK172226B1 (es)
ES (1) ES2054872T3 (es)
FI (1) FI89920C (es)
HK (1) HK142195A (es)
HU (2) HU200770B (es)
IE (1) IE63234B1 (es)
IL (1) IL87795A (es)
IT (1) IT1231413B (es)
LV (1) LV11035B (es)
MX (1) MX9203249A (es)
NO (1) NO169286C (es)
NZ (1) NZ226291A (es)
PH (1) PH29923A (es)
PL (2) PL152951B1 (es)
SK (1) SK278812B6 (es)
SU (1) SU1676451A3 (es)
UA (1) UA8022A1 (es)
YU (1) YU46925B (es)
ZA (1) ZA887083B (es)

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IT1230881B (it) * 1989-06-20 1991-11-08 Angeli Inst Spa Derivati del r(-) 3-chinuclidinolo
CA2030051C (en) * 1989-11-17 2001-08-07 Haruhiko Kikuchi Indole derivatives
EP0436245A1 (en) * 1989-12-27 1991-07-10 Duphar International Research B.V Substituted 3,4-annelated benzimidazol-2(1H)-ones
JP3122671B2 (ja) * 1990-05-23 2001-01-09 協和醗酵工業株式会社 複素環式化合物
US5192770A (en) * 1990-12-07 1993-03-09 Syntex (U.S.A.) Inc. Serotonergic alpha-oxoacetamides
JP3026845B2 (ja) * 1991-02-20 2000-03-27 日清製粉株式会社 ピペリジン誘導体
IT1250629B (it) * 1991-07-04 1995-04-21 Boehringer Ingelheim Italia Uso dei derivati dell'acido benzimidazolin-2-oxo-1-carbossilico.
GB9204565D0 (en) * 1992-03-03 1992-04-15 Smithkline Beecham Plc Pharmaceuticals
JPH05310732A (ja) * 1992-03-12 1993-11-22 Mitsubishi Kasei Corp シンノリン−3−カルボン酸誘導体
JP2699794B2 (ja) * 1992-03-12 1998-01-19 三菱化学株式会社 チエノ〔3,2−b〕ピリジン誘導体
PH30413A (en) * 1992-03-26 1997-05-09 Boehringer Ingelheim Italia Crystalline forms of endo-2,3-dihydro-n-(8-methyl)-8-azabicyclo-(3,2,1)oct-3-yl)-2-oxo-1h-benzimidazole-1-carboxamides
AU4081393A (en) * 1992-05-23 1993-12-30 Smithkline Beecham Plc Medicaments for the treatment of anxiety
US5300512A (en) * 1992-06-24 1994-04-05 G. D. Searle & Co. Benzimidazole compounds
US5521193A (en) * 1992-06-24 1996-05-28 G. D. Searle & Co. Benzimidazole compounds
US5280028A (en) * 1992-06-24 1994-01-18 G. D. Searle & Co. Benzimidazole compounds
WO1994000113A2 (en) * 1992-06-27 1994-01-06 Smithkline Beecham Plc Medicaments containing 5-ht4 receptor antagonists
FR2694292B1 (fr) * 1992-07-29 1994-10-21 Esteve Labor Dr Dérivés de benzimidazole-2-thione-, leur préparation et leur application en tant que médicament.
US5534521A (en) * 1993-06-23 1996-07-09 G. D. Searle & Co. Benzimidazole compounds
GB9502582D0 (en) * 1995-02-10 1995-03-29 Smithkline Beecham Plc Novel process
AU755117B2 (en) * 1999-05-12 2002-12-05 Sydney Gordon Low A message processing system
TW200533348A (en) 2004-02-18 2005-10-16 Theravance Inc Indazole-carboxamide compounds as 5-ht4 receptor agonists
US8309575B2 (en) 2004-04-07 2012-11-13 Theravance, Inc. Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
TWI351282B (en) 2004-04-07 2011-11-01 Theravance Inc Quinolinone-carboxamide compounds as 5-ht4 recepto
US7728006B2 (en) 2004-04-07 2010-06-01 Theravance, Inc. Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
JP4129445B2 (ja) * 2004-06-15 2008-08-06 ファイザー・インク ベンズイミダゾロンカルボン酸誘導体
ES2332808T3 (es) 2004-11-05 2010-02-12 Theravance, Inc. Compuestos agonistas del receptor 5-ht4.
EP1807423B1 (en) 2004-11-05 2009-05-20 Theravance, Inc. Quinolinone-carboxamide compounds
MX2007007818A (es) 2004-12-22 2007-09-11 Theravance Inc Compuestos de indazol-carboxamida.
ES2523851T3 (es) 2005-03-02 2014-12-02 Theravance Biopharma R&D Ip, Llc Compuestos de quinolinona como agonistas de los receptores 5-HT4
US7317022B2 (en) 2005-06-07 2008-01-08 Theravance, Inc. Benzoimidazolone-carboxamide compounds as 5-HT4 receptors agonists
MY143574A (en) 2005-11-22 2011-05-31 Theravance Inc Carbamate compounds as 5-ht4 receptor agonists
CN101874028B (zh) * 2007-07-27 2012-11-14 埃科特莱茵药品有限公司 2-氮杂-二环[3.3.0]辛烷衍生物
EP2253316B1 (en) 2009-05-20 2013-08-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Serotonin 5-HT3 receptor antagonists for use in the treatment or prevention of an inner ear pathology with vestibular deficits
JP5955767B2 (ja) 2009-05-20 2016-07-20 インセルム(インスティチュート ナショナル デ ラ サンテ エ デ ラ リシェルシェ メディカル) 損傷性前庭障害の処置における使用のためのセロトニン5−ht3受容体拮抗薬
EP2701699B1 (en) 2011-04-28 2019-10-16 The Broad Institute, Inc. Inhibitors of histone deacetylase
JP6337255B2 (ja) 2012-07-27 2018-06-06 ザ ブロード インスティテュート, インコーポレーテッドThe Broad Institute, Inc. ヒストンデアセチラーゼの阻害剤
US9914717B2 (en) 2012-12-20 2018-03-13 The Broad Institute, Inc. Cycloalkenyl hydroxamic acid derivatives and their use as histone deacetylase inhibitors
EP3166940A4 (en) 2014-07-11 2018-04-25 Alpharmagen, LLC Quinuclidine compounds for modulating alpha7 -nicotinic acetylcholine receptor activity
US12128018B2 (en) 2018-01-12 2024-10-29 KDAc Therapeutics, Inc. Combination of a selective histone deacetylase 3 (HDAC3) inhibitor and an immunotherapy agent for the treatment of cancer

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EP0247266B1 (en) * 1986-01-07 1993-03-10 Beecham Group Plc Indole derivatives having an azabicyclic side chain, process for their preparation, intermediates, and pharmaceutical compositions

Also Published As

Publication number Publication date
SK630788A3 (en) 1998-03-04
PL279346A1 (en) 1990-01-08
IT8721997A0 (it) 1987-09-23
AU610040B2 (en) 1991-05-09
HU211566A9 (en) 1995-12-28
IL87795A0 (en) 1989-03-31
DE3850203T2 (de) 1994-09-22
PL152951B1 (en) 1991-02-28
NZ226291A (en) 1991-05-28
NO884202D0 (no) 1988-09-22
HK142195A (en) 1995-09-15
FI89920C (fi) 1993-12-10
LV11035B (en) 1996-08-20
CA1337347C (en) 1995-10-17
FI884350A0 (fi) 1988-09-22
NO169286B (no) 1992-02-24
DK526188D0 (da) 1988-09-22
EP0309423B1 (en) 1994-06-15
HUT48250A (en) 1989-05-29
JPH01106882A (ja) 1989-04-24
PL151434B1 (en) 1990-09-28
EP0309423A2 (en) 1989-03-29
YU177888A (en) 1990-06-30
SK278812B6 (sk) 1998-03-04
CZ279864B6 (cs) 1995-07-12
AU2237888A (en) 1989-03-23
KR890005105A (ko) 1989-05-11
IE63234B1 (en) 1995-04-05
SU1676451A3 (ru) 1991-09-07
JPH0631225B2 (ja) 1994-04-27
KR960003604B1 (en) 1996-03-20
NO884202L (no) 1989-03-28
NO169286C (no) 1992-06-03
PL274751A1 (en) 1989-09-04
IE882869L (en) 1989-03-23
IL87795A (en) 1993-02-21
LV11035A (lv) 1996-02-20
DD285354A5 (de) 1990-12-12
BR1100514A (pt) 2002-04-02
DK172226B1 (da) 1998-01-12
FI89920B (fi) 1993-08-31
ZA887083B (en) 1990-05-30
FI884350A7 (fi) 1989-03-24
MX9203249A (es) 1992-07-01
UA8022A1 (uk) 1995-12-26
PH29923A (en) 1996-09-16
DE3850203D1 (de) 1994-07-21
YU46925B (sh) 1994-06-24
CZ630788A3 (en) 1995-04-12
EP0309423A3 (en) 1989-11-29
DK526188A (da) 1989-03-24
ATE107305T1 (de) 1994-07-15
IT1231413B (it) 1991-12-04
HU200770B (en) 1990-08-28

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