Benzopyrano[4,3,2-cd]indazole compounds, processes for their production and pharmaceutical compositions comprising the compounds
申请人:WARNER-LAMBERT COMPANY
公开号:EP0172632A1
公开(公告)日:1986-02-26
Benzopyrano[4,3,2-cd]indazole compound having in free base form the following general formula I
and the pharmaceutically acceptable salts thereof, wherein:
R7, R8, R9 and Rio independently represent hydrogen, hydroxy or alkoxy of from one to four carbon atoms;
R2 is ANR'R" in which A is a straight or branched alkylene chain of from 2 to 5 carbon atoms, optionally substituted with hydroxyl; and in which R' and R" are independently hydrogen, a straight or branched alkyl of from one to four carbon atoms, optionally substituted with hydroxyl, or R' and R", when taken together, represent the bifunctional radical
in which n and m are, independently, two or three and B is a direct bond or O, S, or N " wherein R"' is hydrogen or straight or branched alkyl of from one to four carbon atoms, optionally substituted with hydroxyl; and
R5 is nitro, NH2, NHR2 wherein R2 is defined above or NH R"" wherein R"" is a radical having the formula
in which Z is a straight or branched alkylene of from one to four carbon atoms and Rx and Ry are each independently hydrogen or straight or branched alkyl of from one to four carbon atoms optionally substituted with hydroxyl, or R"' is the radical
Also disclosed are processes for producing the compounds and pharmaceutical compositions comprising the compounds. Compounds of the invention have pharmacological properties and are useful antibacterial agents, antifungal agents, and antitumor agents.
具有以下通式 I 的游离碱形式的苯并
吡喃并[4,3,2-cd]
吲唑化合物
及其药学上可接受的盐类,其中
R7、R8、R9 和 Rio 分别代表氢、羟基或一至四个碳原子的烷氧基;
R2 是 ANR'R" 其中 A 是 2 至 5 个碳原子的直链或支链亚烷基,可选择被羟基取代; R' 和 R" 独立地代表氢、1 至 4 个碳原子的直链或支链烷基,可选择被羟基取代,或 R' 和 R" 合在一起代表双官能基
其中 n 和 m 分别为两个或三个,B 为直接键或 O、S 或 N " 其中 R"' 为氢或一至四个碳原子的直链或支链烷基,可选择被羟基取代;以及
R5 是硝基、NH2、NHR2(其中 R2 定义如上)或 NH R""(其中 R""是具有以下式子的基团
其中 Z 为一至四个碳原子的直链或支链亚烷基,Rx 和 Ry 各自独立地为氢或一至四个碳原子的直链或支链烷基,可选择被羟基取代,或 R"' 为以下基团
还公开了生产本发明化合物的工艺和包含本发明化合物的药物组合物。本发明的化合物具有药理特性,是有用的抗菌剂、抗真菌剂和抗肿瘤剂。