公开(公告)号：US4835158A

公开(公告)日：1989-05-30

申请号：US120654

申请日：1987-11-16

申请人： Gordon H. Phillipps ,  Stanley F. Dyke ,  Esme J. Bailey ,  Peter D. Howes ,  David I. C. Scopes

发明人： Gordon H. Phillipps ,  Stanley F. Dyke ,  Esme J. Bailey ,  Peter D. Howes ,  David I. C. Scopes

IPC分类号： C07D471/04 ,  C07D471/14

CPC分类号： C07D471/04 ,  C07D471/14

摘要： Pharmaceutical compositions for combatting cancer comprising a compound of formula (I) ##STR1## (wherein R.sup.1 represents a hydrogen atom or a C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl group;R.sup.2 represents a hydrogen atom or a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group;R.sup.3 represents a hydrogen atom, or (when R.sup.2 is other than a hydrogen atom) optionally a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group, or R.sup.2 and R.sup.3 together represent a methylenedioxy group;R.sup.4 represents a hydrogen or halogen atom or a C.sub.1-3 alkyl group or a phenyl group optionally substituted by a halogen atom or a hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkanoyloxy group; and the ring A represents a group of formula ##STR2## where R.sup.5 and R.sup.6 each represent a hydrogen atom or a hydroxyl, C.sub.1-4 alkoxy or C.sub.1-4 alkanoyloxy group,R.sup.7 and R.sup.8 each represents a hydrogen atom or a methyl group, and one of X, X.sup.1, X.sup.2 and X.sup.3 represents a nitrogen atom and the others represent --CH-- groups; with the proviso that where Arepresents a group of formula (i) at least one of R.sup.1 to R.sup.6 represents other than a hydrogen atom) together with at least one pharmaceutical carrier or excipient.

摘要翻译： 包括式（I）化合物（I）（其中R1表示氢原子或C1-4烷基，C2-4烯基或C2-4炔基; R2表示氢原子或 羟基，C 1-4烷氧基或C 2-4烷酰氧基; R 3表示氢原子，或（当R 2不是氢原子时）任选的羟基，C 1-4烷氧基或C 2-4烷酰氧基，或R 2和R 3 一起代表亚甲二氧基; R4代表氢或卤原子或C1-3烷基或任选被卤素原子或羟基，C1-4烷基，C1-4烷氧基或C1-4烷酰氧基取代的苯基; 并且环A表示式为“IMAGE”的基团，其中R 5和R 6各自表示氢原子或羟基，C 1-4烷氧基或C 1-4烷酰氧基，R 7和R 8各自表示氢原子或甲基， X，X 1，X 2和X 3中的一个表示氮原子，其余的表示-CH-基团;条件是其中A代表 （i）R 1至R 6中的至少一个表示除氢原子以外的基团）以及至少一种药物载体或赋形剂。

公开(公告)号：US4324792A

公开(公告)日：1982-04-13

申请号：US193846

申请日：1980-10-03

申请人： John Bradshaw ,  Alexander W. Oxford ,  David I. C. Scopes

发明人： John Bradshaw ,  Alexander W. Oxford ,  David I. C. Scopes

IPC分类号： A61K31/415 ,  A61P43/00 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D403/06 ,  A61K31/445

CPC分类号： C07D233/64 ,  C07C255/00

摘要： The present invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts and bioprecursors thereof in which ##STR2## represents either ##STR3## R.sup.1 represents hydrogen, halogen, C.sub.1-4 alkoxy, hydroxy, alkyl, R.sup.4 CH(OH)--, cyano or R.sup.5 CONH--, R.sup.2 and R.sup.3, which may be the same or different, each represents a straight or branched chain alkyl group or alkenyl group or R.sup.2 and R.sup.3 may, together with the nitrogen atom to which they are attached, form a saturated heterocyclic ring containing from 5 to 7 members which may optionally contain an oxygen atom; R.sup.4 represents hydrogen or alkyl; and R.sup.5 represents hydrogen, alkyl or C.sub.1-4 alkoxy. The compounds have been shown to exhibit H.sub.1 -antagonist activity in standard pharmacological tests.

摘要翻译： 本发明提供了通式（I）的化合物及其生理学上可接受的盐和生物前体，其中R 1表示氢，卤素，C 1-4烷氧基，羟基，烷基，R 4 CH （OH） - ，氰基或R 5 CONH - ，R 2和R 3可以相同或不同，表示直链或支链烷基或烯基，或者R 2和R 3可以与它们所连接的氮原子一起 形成含有5至7个可任意含有氧原子的饱和杂环; R4表示氢或烷基; R5代表氢，烷基或C1-4烷氧基。 化合物已被证明在标准药理学试验中显示出H1拮抗剂活性。