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：US4831039A

公开(公告)日：1989-05-16

申请号：US129064

申请日：1987-12-07

申请人： Stanley F. Dyke ,  Gordon H. Phillipps

发明人： Stanley F. Dyke ,  Gordon H. Phillipps

IPC分类号： A61K31/47 ,  A61P35/00 ,  C07D471/04

CPC分类号： C07D471/04

摘要： 5,14-Dihydrobenz[5,6]isoindolo[2,1-b]isoquinoline-8,13-dione ##STR1## exhibits anticancer activity. The compound can be prepared by reaction of 2-formyl-3-carboxyl-1,2,3,4-tetrahydroisoquinoline with 1,4-naphthoquinone and is particularly suitably administered parenterally in microcrystalline suspension form.

摘要翻译： 5,14-二氢苯并[5,6]异吲哚并[2,1-b]异喹啉-8,13-二酮（I）表现出抗癌活性。 该化合物可以通过2-甲酰基-3-羧基-1,2,3,4-四氢异喹啉与1,4-萘醌的反应制备，特别适合以微晶悬浮液形式肠胃外给药。