Title:
【発明の名称】胃運動性の3-もしくは4-置換4-(アミノメチル)-ピペリジン誘導体の単環式ベンズアミド
Document Type and Number:
Japanese Patent JP2001509503
Kind Code:
A
Abstract:
Bicyclic benzamide derivatives of 3- or 4-substituted 4-(aminomethyl)piperidine derivatives of formula (I) and their stereoisomers, N-oxides and acidic and basic addition salts are new. R1 + R2 = OCH2O, OCH2CH2O, OCH2CH2, OCH2CH2CH2, OCH2CH2CH2O or OCH2CH2CH2CH2 in which one or two H atoms are optionally substituted by 1-6C alkyl; R3 = H or halo; R4 = H or 1-6C alkyl; R5 = H or 1-6C alkyl; L = 3-6C cycloalkyl, 5-6C cycloalkanone, 2-6C alkenyl or Alk-R6, Alk-X-R7, Alk-Y-COR9 or Alk-Y-CONR11R12; Alk = 1-12C alkanediyl; R6 = H, OH, CN, 1-6C alkylsulphonylamino, 3-6C cycloalkyl, 5-6C cycloalkanone or Het1; R7 = H, 1-6C alkyl, hydroxy(1-6C alkyl), 3-6C cycloalkyl or Het2; X = O, S, SO2 or NR8; R8 = H or 1-6C alkyl; R9 = H, 1-6C alkyl, 3-6C cycloalkyl, 1-6C alkyloxy or OH; Y = NR10 or a bond; R10 = H or 1-6C alkyl; R11, R12 = H, 1-6C alkyl, 3-6C cycloalkyl or NR11R12 = pyrrolidinyl or piperidinyl (both optionally substituted by 1-6C alkyl, amino or mono- or di-(1-6C alkyl)amino) or piperazinyl or 4-morpholinyl (both optionally substituted by 1-6C alkyl); Het1, Het2 = furan (optionally substituted by 1-6C alkyl or halo) or tetrahydrofuran, dioxolane, dioxane or tetrahydropyran (all optionally substituted by 1-6C alkyl), pyrrolidinyl or pyridinyl (both optionally substituted by 1 or 2 halo, OH, CN or 1-6C alkyl); pyrimidinyl (optionally substituted by 1 or 2 halo, OH, CN, 1-6C alkyl, 1-6C alkyloxy, amino or mono- or di-(1-6C alkyl)amino), pyridazinyl (optionally substituted by 1 or 2 OH, 1-6C alkyloxy, 1-6C alkyl or halo) or pyrazinyl (optionally substituted by 1 or 2 halo, OH, CN, 1-6C alkyl, 1-6C alkyloxy, amino, mono- or di-(1-6C alkyl)amino or 1-6C alkyloxycarbonyl); Het1 can also be a group of formulae (a)-(d); Het1, Het2 can also be a group of formulae (e)-(g); R13, R14 = H or 1-4C alkyl. One compound (I) is specifically claimed i.e. trans-(-)-4-amino-5-chloro- 2,3-dihydro-N-[[3-hydroxy-1- (3-methoxypropyl)-4-piperidinyl] -methyl]-2,2-dimethyl-7- benzofurancarboxamide.
Inventors:
Bossman, Jiyang-Paul Rene Marie Andre
De Crane, Michelle Anna Joseph
Sulkin, Michel
De Crane, Michelle Anna Joseph
Sulkin, Michel
Application Number:
JP2000502022A
Publication Date:
July 24, 2001
Filing Date:
July 07, 1998
Export Citation:
Assignee:
JANSSEN PHARMACEUTICA NAAMLOZE VENNOOTSCHAP
International Classes:
A61K31/4427; A61K31/443; A61K31/445; A61K31/4523; A61K31/4525; A61K31/453; A61K31/454; A61K31/4545; A61K31/497; A61K31/501; A61K31/502; A61P1/00; A61P1/10; A61P1/14; A61P43/00; C07C229/60; C07D211/42; C07D211/44; C07D401/06; C07D405/06; C07D405/12; C07D405/14; C07D417/14; C07D513/04; A61P1/00; A61K31/00; (IPC1-7): C07D211/42; A61K31/445; A61K31/4525; A61K31/453; A61K31/454; A61K31/4545; A61K31/501; A61K31/502; A61P1/00; A61P43/00; C07D211/44; C07D401/06; C07D405/06
Domestic Patent References:
| JPS4810471B1 | 1973-04-03 |
Foreign References:
| WO1995026953A1 | 1995-10-12 | |||
| WO1999002156A1 | 1999-01-21 | |||
| WO1997011054A1 | 1997-03-27 | |||
| WO1992014705A1 | 1992-09-03 |
Attorney, Agent or Firm:
Heiyoshi Odashima (1 person outside)