Title:
NOVEL COMPOUND, MANUFACTURE AND MEDICINAL COMPOSITION
Document Type and Number:
Japanese Patent JPS62126168
Kind Code:
A
Abstract:
Compounds of formula (I) and pharmaceutically acceptable salts thereof:wherein: Ar is a group of formula (a):wherein either R2 is C1-6 alkoxy and one of R3, R4 and R5 is hydrogen and the other two are selected from hydrogen, halogen, CF3, C1-6 alkylthio, C1-7 acyl, C1-10 carboxylic acylamino, C1-6 alkyl S(0)n wherein n is 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C1-6 alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl C1-4 alkyl or phenyl C1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF3, C1-6 alkyl or C1-6 alkoxy; or R2 is hydrogen and R3, R4 and R6 are independently selected from hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio or halo; or any two on adjacent carbon atoms together are C1-2 alkylenedioxy and the third is hydrogen, C1-6 alkyl, C1-6 alkoxy or halo; or Ar is a group of formula (b):wherein W is CH,, 0, S or NR7 wherein R7 is hydrogen, C1-6 alkyl C3-7 alkenyl-methyl, phenyl or phenyl C1-4 alkyl either of which phenyl moieties may be substituted by one or two of halogen, CF3, C1-6 alkoxy or C1-6 alkyl; and V is CH or N; orW is CH or N and V is NR, where Ra is as defined for R7 above or CHRc where Rc is as defined for Re below;Rb is present when the COX linkage is attached at the phenyl ring, and is selected from hydrogen, halogen CF3, hydroxy, C1-6 alkoxy or C1-6 alkyl;R6 is hydrogen, halogen, CF3, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-7 acyl, C1-7 acylamino, C1-6 alkylsulphonylamino, N-(C1-6 alkylsulphonyl)-N-C1-4 alkylamino, C1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C1-4 alkylamino optionally N-substituted by one or two groups selected from C1-6 alkyl, C3-8 cycloalkyl C3-8 cycloalkyl C1-4alkyl, phenyl or phenyl C1-4 alkyl groups or optionally N-disubstituted by C4-6 polymethylene;X is NH; or 0 when Ar is of formula (a) and R2 is hydrogen, or when Ar is a group of formula (b);Y is a group of formula (c), (d) or (e): wherein p and q are independently 0 or 1;Z is C2 or C3 polymethylene optionally substituted by one or two C1-4 alkyl groups; andR, is hydrogen or C1-6 alkyl or OR, is an in vivo hydrolysable acyloxy group; having gastric motility enhancing activity, anti-emetic activity and/or 5-HT receptor antagonist activity, a process for their preparation and their use as pharmaceuticals.
Inventors:
FURANSHISU DEBITSUDO KINGU
ROJIYAA TOOMASU MAACHIN
ERITSUKU ARUFURETSUDO WATSUTSU
ROJIYAA TOOMASU MAACHIN
ERITSUKU ARUFURETSUDO WATSUTSU
Application Number:
JP26173586A
Publication Date:
June 08, 1987
Filing Date:
November 01, 1986
Export Citation:
Assignee:
BEECHAM GROUP PLC
International Classes:
A61K31/445; A61K31/4468; A61K31/46; A61P1/12; A61P25/00; C07D211/58; C07D451/04; (IPC1-7): A61K31/445; A61K31/46; C07D211/58; C07D451/04
Attorney, Agent or Firm:
Masamitsu Akizawa