AP401A - Condensed indole derivatives as 5H4-receptor antagonists. - Google Patents

Condensed indole derivatives as 5H4-receptor antagonists. Download PDF

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Publication number
AP401A
AP401A APAP/P/1993/000494A AP9300494A AP401A AP 401 A AP401 A AP 401A AP 9300494 A AP9300494 A AP 9300494A AP 401 A AP401 A AP 401A
Authority
AP
ARIPO
Prior art keywords
indole
alkyl
compound according
hydrogen
treated
Prior art date
Application number
APAP/P/1993/000494A
Other languages
English (en)
Other versions
AP9300494A0 (en
Inventor
Laramie Mary Gaster
Paul Adrian Wyman
Original Assignee
Smithkline Beecham Plc
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
Priority claimed from GB929205428A external-priority patent/GB9205428D0/en
Priority claimed from GB929218846A external-priority patent/GB9218846D0/en
Priority claimed from GB929227045A external-priority patent/GB9227045D0/en
Application filed by Smithkline Beecham Plc filed Critical Smithkline Beecham Plc
Publication of AP9300494A0 publication Critical patent/AP9300494A0/xx
Application granted granted Critical
Publication of AP401A publication Critical patent/AP401A/en

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Classifications

    • 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
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
    • A61K31/245—Amino benzoic acid types, e.g. procaine, novocaine
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
    • 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
    • A61K31/452—Piperidinium derivatives
    • 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
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Indole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
APAP/P/1993/000494A 1992-03-12 1993-03-10 Condensed indole derivatives as 5H4-receptor antagonists. AP401A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB929205428A GB9205428D0 (en) 1992-03-12 1992-03-12 Pharmaceuticals
GB929218846A GB9218846D0 (en) 1992-09-05 1992-09-05 Pharmaceuticals
GB929227045A GB9227045D0 (en) 1992-12-29 1992-12-29 Pharmaceuticals

Publications (2)

Publication Number Publication Date
AP9300494A0 AP9300494A0 (en) 1993-04-30
AP401A true AP401A (en) 1995-08-29

Family

ID=27266092

Family Applications (1)

Application Number Title Priority Date Filing Date
APAP/P/1993/000494A AP401A (en) 1992-03-12 1993-03-10 Condensed indole derivatives as 5H4-receptor antagonists.

Country Status (30)

Country Link
EP (2) EP0884319B1 (de)
JP (1) JP2831467B2 (de)
KR (1) KR100282730B1 (de)
CN (2) CN1043893C (de)
AP (1) AP401A (de)
AT (2) ATE266033T1 (de)
AU (1) AU671102B2 (de)
CA (1) CA2131797C (de)
CY (1) CY2510B1 (de)
CZ (1) CZ286194B6 (de)
DE (2) DE69325167T2 (de)
DK (2) DK0630376T3 (de)
ES (2) ES2219813T3 (de)
FI (1) FI107158B (de)
GR (1) GR3030668T3 (de)
HK (1) HK1012352A1 (de)
HU (1) HU219121B (de)
IL (1) IL105003A (de)
MA (1) MA22819A1 (de)
MX (1) MX9301348A (de)
MY (1) MY110110A (de)
NO (1) NO303638B1 (de)
NZ (1) NZ249565A (de)
PT (1) PT884319E (de)
RU (1) RU2104279C1 (de)
SG (1) SG50693A1 (de)
SI (1) SI9300114B (de)
SK (1) SK281423B6 (de)
UA (1) UA41311C2 (de)
WO (1) WO1993018036A1 (de)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5852014A (en) * 1992-03-12 1998-12-22 Smithkline Beecham P.L.C. Condensed indole derivatives as 5HT4 -receptor antagonists
GB9316195D0 (en) * 1993-08-05 1993-09-22 Smithkline Beecham Plc Pharmaceuticals
US5998409A (en) * 1992-03-12 1999-12-07 Smithkline Beecham Plc Condensed indole derivatives as 5HT4 -receptor antagonists
MX9305947A (es) * 1992-09-29 1994-06-30 Smithkline Beecham Plc Compuestos antagonistas del receptor 5-ht4, procedimiento para su preparacion y composiciones farmaceuticas que las contienen.
WO1994008965A1 (en) * 1992-10-16 1994-04-28 Smithkline Beecham Plc N-alkylpiperidinyl-4-methyl carboxylic esters/amides of condensed ring systems as 5-ht4 receptor antagonists
WO1994010174A1 (en) * 1992-11-05 1994-05-11 Smithkline Beecham Plc Piperidine derivatives as 5-ht4 receptor antagonists
FR2699921B1 (fr) * 1992-12-30 1995-02-10 Synthelabo Dérivés d'acide 2-(thien-2-yl)imidazo[2,1-b]benzothiazole-3-acétique, leur préparation et leur application en thérapeutique.
GB9303340D0 (en) * 1993-02-19 1993-04-07 Smithkline Beecham Plc Pharmaceuticals
GB9310582D0 (en) * 1993-05-22 1993-07-07 Smithkline Beecham Plc Pharmaceuticals
GB9312348D0 (en) * 1993-06-16 1993-07-28 Smithkline Beecham Plc Pharmaceuticals
KR100219922B1 (ko) * 1996-05-16 1999-09-01 이서봉 신규한 항바이러스성 6-아릴옥시 및 6-아릴카르보닐 2,4-피리미딘디온 유도체 및 그의 제조 방법
US6013666A (en) * 1996-07-02 2000-01-11 Sang Sup Jew Oxirane carboxylic acid derivative and its manufacturing method
CZ290517B6 (cs) * 1996-08-16 2002-08-14 Smithkline Beecham Plc Způsob přípravy N-[(1-n-butyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]-oxazino [3,2-a]indol-10-karboxamidu nebo jeho soli a meziprodukt pro tento způsob
US6100397A (en) * 1996-08-16 2000-08-08 Smithkline Beecham Plc Process for the preparation of N-[(1-n butyl-4-piperidyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a] indole-10-carboxamide and salts and intermediates in the process
GB9618967D0 (en) * 1996-09-11 1996-10-23 Smithkline Beecham Plc Pharmaceuticals
GB9725933D0 (en) * 1997-12-05 1998-02-04 Smithkline Beecham Plc Pharmaceuticals
US6251893B1 (en) * 1998-06-15 2001-06-26 Nps Allelix Corp. Bicyclic piperidine and piperazine compounds having 5-HT6 receptor affinity
US20020091271A1 (en) 1998-07-16 2002-07-11 Smithkline Beecham Plc Process for the preparation of an indole derivative
GB9819035D0 (en) * 1998-09-01 1998-10-28 Cerebrus Res Ltd Chemical compounds VII
BRPI9913542B8 (pt) * 1998-09-10 2021-05-25 Hoffmann La Roche derivados de dihidrobenzodioxina carboxamida e dihidrobenzodioxina cetona como antagonistas do receptor 5-ht4 bem como composição farmacêutica, processo para a preparação dos referidos derivados e uso dos mesmos
GB9820294D0 (en) * 1998-09-17 1998-11-11 Smithkline Beecham Plc Pharmaceuticals
US6545004B1 (en) 1999-10-27 2003-04-08 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
AU782870C (en) * 2000-08-07 2007-03-15 Glaxo Group Limited The use of 5HT4 receptor antagonists in the prophylaxis or treatment of certain cardiovascular conditions
AU2005203196B9 (en) * 2000-08-07 2009-04-09 Glaxo Group Limited The use of 5HT4 receptor antagonists in the prophylaxis or treatment of certain cardiovascular conditions
AU782863C (en) * 2000-08-07 2006-08-31 Glaxo Group Limited The use of 5HT4 receptor antagonists in the prophylaxis or treatment of certain cardiovascular conditions
MXPA03001210A (es) * 2000-08-07 2004-08-12 Smithkline Beecham Corp Uso de antagonista del receptor 5-ht4 en la fabricacion de un medicamento para la profilaxis o tratamiento de fibrilacion atrial.
AU2001276558B2 (en) * 2000-08-08 2005-11-24 Smithkline Beecham P.L.C. Pharmaceutical composition comprising condensed indole compound
NZ535261A (en) * 2000-08-08 2004-12-24 Smithkline Beecham P A tablet comprising the hydrochloride salt of N-(1-nbutyl-4-piperidinyl)methyl]-3,4-[1,3]oxazino[3,2-a] indole-10-carboxamide
NZ534333A (en) * 2002-02-14 2006-05-26 Glaxo Group Ltd Pharmaceutical composition comprising N-[(1-n-butyl-4-piperidinyl) methyl]-3,4-dihydro-2H-[1, 3]oxazino[3, 2-a]indole-10-carboxamide or salt, and process for preparing thereof comprising dry granulation
GB0211230D0 (en) 2002-05-16 2002-06-26 Medinnova Sf Treatment of heart failure
ITMI20031467A1 (it) * 2003-07-18 2005-01-19 Acraf Farmaco attivo nel dolore neuropatico
ITMI20031468A1 (it) 2003-07-18 2005-01-19 Acraf Farmaco ativo nel dolore neuropatico
US7834010B2 (en) 2003-12-23 2010-11-16 Serodus As Modulators of peripheral 5-HT receptors
JP4612301B2 (ja) * 2003-12-26 2011-01-12 広栄化学工業株式会社 １−アルキル−４−アミノメチルピペリジンの製造法
EP2173724B1 (de) 2007-06-22 2012-12-05 ArQule, Inc. Chinazolinonverbindungen und verfahren zu ihrer anwendung
GB0905641D0 (en) * 2009-04-01 2009-05-13 Serodus As Compounds
WO2021116487A1 (en) 2019-12-13 2021-06-17 Som Innovation Biotech, S.A. Compounds for use in the treatment of niemann-pick c disease

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1566307A (en) * 1975-12-19 1980-04-30 Hoechst Ag Indole derivatives of amides and amino esters and process for their manufacture
EP0429984A2 (de) * 1989-11-17 1991-06-05 Nisshin Flour Milling Co., Ltd. Indolderivate
EP0485962A2 (de) * 1990-11-16 1992-05-20 Syntex (U.S.A.) Inc. Tricyclische Verbindungen

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU622330B2 (en) * 1989-06-23 1992-04-02 Takeda Chemical Industries Ltd. Condensed heterocyclic compounds having a nitrogen atom in the bridgehead for use as fungicides
GB9103862D0 (en) * 1991-02-25 1991-04-10 Glaxo Group Ltd Chemical compounds
US5206382A (en) * 1991-06-27 1993-04-27 Fidia Georgetown Institute For The Neurosciences Indole derivatives, pharmaceutical compositions and methods of treating neurological and psychiatric disorders

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1566307A (en) * 1975-12-19 1980-04-30 Hoechst Ag Indole derivatives of amides and amino esters and process for their manufacture
EP0429984A2 (de) * 1989-11-17 1991-06-05 Nisshin Flour Milling Co., Ltd. Indolderivate
EP0485962A2 (de) * 1990-11-16 1992-05-20 Syntex (U.S.A.) Inc. Tricyclische Verbindungen

Also Published As

Publication number Publication date
FI944204A0 (fi) 1994-09-12
IL105003A (en) 1996-09-12
ES2219813T3 (es) 2004-12-01
CA2131797C (en) 2010-05-18
CN1043893C (zh) 1999-06-30
NO943348L (no) 1994-11-09
AU3644893A (en) 1993-10-05
FI107158B (fi) 2001-06-15
HUT71121A (en) 1995-11-28
KR100282730B1 (ko) 2001-02-15
HU9402601D0 (en) 1994-12-28
JPH07504433A (ja) 1995-05-18
UA41311C2 (uk) 2001-09-17
DK0884319T3 (da) 2004-08-30
FI944204A (fi) 1994-09-12
HU219121B (hu) 2001-02-28
MX9301348A (es) 1993-09-01
ATE266033T1 (de) 2004-05-15
RU94040864A (ru) 1996-07-20
SK281423B6 (sk) 2001-03-12
JP2831467B2 (ja) 1998-12-02
CZ286194B6 (cs) 2000-02-16
SG50693A1 (en) 1998-07-20
WO1993018036A1 (en) 1993-09-16
CZ221094A3 (en) 1995-09-13
ATE180785T1 (de) 1999-06-15
ES2132223T3 (es) 1999-08-16
DE69325167D1 (de) 1999-07-08
EP0630376A1 (de) 1994-12-28
CN1085083A (zh) 1994-04-13
AU671102B2 (en) 1996-08-15
SI9300114B (sl) 2006-08-31
DE69333504D1 (de) 2004-06-09
DK0630376T3 (da) 1999-06-23
EP0884319B1 (de) 2004-05-06
SI9300114A (sl) 1993-12-31
HK1012352A1 (en) 1999-07-30
EP0630376B1 (de) 1999-06-02
RU2104279C1 (ru) 1998-02-10
SK107894A3 (en) 1995-04-12
AP9300494A0 (en) 1993-04-30
KR950700304A (ko) 1995-01-16
IL105003A0 (en) 1993-07-08
GR3030668T3 (en) 1999-10-29
CA2131797A1 (en) 1993-09-16
NO943348D0 (no) 1994-09-09
EP0884319A2 (de) 1998-12-16
DE69325167T2 (de) 2000-01-20
MY110110A (en) 1998-01-27
DE69333504T2 (de) 2005-05-12
NO303638B1 (no) 1998-08-10
CY2510B1 (en) 2005-12-23
EP0884319A3 (de) 1999-02-10
PT884319E (pt) 2004-09-30
CN1078471A (zh) 1993-11-17
NZ249565A (en) 1997-07-27
MA22819A1 (fr) 1993-10-01

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