Title:
【発明の名称】新規化合物、その製造法及びそれを含む医薬組成物
Document Type and Number:
Japanese Patent JP2799745
Kind Code:
B2
Abstract:
Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein a and b together form an -O- or -CH2- linkage or a bond; either Y is N and R2 is hydrogen; or Y is C-R1 wherein either one of R1 and R2 is hydrogen and the other is nitro, cyano, halo, CF3, formyl, aldoxime, CF3O, NO2-CH=CH-, NC-CH=CH-; a group RxX- wherein Rx is C1-6 alkyl, aryl or heteroaryl either of which may be optionally substituted by one, two or three of C1-4 alkyl, C1-4 alkoxy, nitro, halo, CF3 and cyano; and X is C=O, O.C=O, C=O.O, CHOH, SO, SO2, O.SO, O.SO2, CONH, O.CONH, C=S, O.C=S, C=S.O, CH.SH, SONH, SO2NH, O.SONH, O.SO2NH, CO-CH=CH, C=NHOH, C=NNH2; or a group RyRzNZ- wherein Ry and Rz are independently hydrogen or C1-6 alkyl and Z is C=O, SO or SO2; or R1 is a C3-8 cycloalkyl group or a C1-6 alkyl group optionally substituted by a group which is hydroxy, C1-6 alkoxy, amino optionally substituted by one or two C1-6 alkyl groups, C1-7 alkanoylamino, C3-8 cycloalkyloxy or C3-8 cycloalkylamino; and R2 is hydrogen; or one of R1 and R2 is nitro, cyano or C1-3 alkylcarbonyl and the other is a different group selected from nitro, cyano, halo, C1-3 alkylcarbonyl, methoxy or amino optionally substituted by one or two C1-6 alkyl or by C2-7 alkanoyl; either one of R3 and R4 is hydrogen or C1-4 alkyl and the other is C1-4 alkyl; or R3 and R4 together are C2-5 polymethylene; either R5 is hydrogen, hydroxy, C1-6 alkoxy or C1-7 acyloxy; and R6 is hydrogen; or R5 and R6 together are a bond; either R7 is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C2-6 alkenyl or C2-6 alkynyl; and R8 is hydrogen or C1-6 alkyl; or R7 and R8 together are C2-4 polymethylene; R9 is CN, NO2, COR10 or SO2R10 wherein R10 is C1-3 alkyl, NH2, NH(C1-3 alkyl), CF3 or phenyl optionally substituted as defined for Rx; and the R8N(NR9)NHR7 moiety is trans to the R5 group when R5 is hydroxy, C1-6 alkoxy or C1-7 acyloxy; having antihypertensive and/or bronchodilator activity, processes for their preparation and their use as pharmaceuticals.
Inventors:
Jeffrey Stemp
Gordon Barrel
David Glyn Smith
Gordon Barrel
David Glyn Smith
Application Number:
JP23979189A
Publication Date:
September 21, 1998
Filing Date:
September 14, 1989
Export Citation:
Assignee:
Beechham Group PLC
International Classes:
A61K31/35; A61K31/352; A61K31/435; A61K31/44; A61P1/00; A61P9/00; A61P9/12; A61P11/08; A61K31/155; A61P13/02; A61P15/00; A61P15/04; C07C255/59; C07C255/67; C07C279/16; C07C279/28; C07C335/32; C07D311/58; C07D311/68; C07D405/04; C07D491/04; C07D491/052; A61K; C07C; C07D; (IPC1-7): C07C279/16; A61K31/155; A61K31/35; A61K31/435; C07C335/32; C07D311/58; C07D311/68; C07D405/04; C07D491/052
Domestic Patent References:
| JP1141971A |
Other References:
Ｊ．Ｍｅｄ．Ｃｈｅｍ．２０（６），Ｐ．７７１−７７６（１９７７）
Attorney, Agent or Firm:
Masamitsu Akizawa (1 person outside)