公开(公告)号：US5464616A

公开(公告)日：1995-11-07

申请号：US285670

申请日：1994-08-04

申请人： Kazuharu Noguchi ,  Ronald G. Micetich ,  Mohsen Daneshtalab

发明人： Kazuharu Noguchi ,  Ronald G. Micetich ,  Mohsen Daneshtalab

IPC分类号： C07D499/10 ,  A61K31/43 ,  A61P31/04 ,  C07D499/00 ,  C07D499/70 ,  C07D499/72 ,  C07D499/76 ,  A61K31/425

CPC分类号： C07D499/00

摘要： A 6.beta.-substituted penicillanic acid of the formula XII: ##STR1## or a pharmaceutically acceptable salt or ester thereof, whereinA and B are each hydrogen wherein the carbon atoms to which A and B are attached are linked by a single bond, or A and B together form a bond, wherein the carbon atoms to which A and B are attached are linked by a double bond,R1 is selected from the group consisting of a) hydrogen, b) a pharmaceutically acceptable salt and c) a pharmaceutically acceptable group selected from the group consisting of C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkenyl, allyl, aryl, aralkyl, aralkenyl, aralkynyl, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl and alkylheterocyclyl; wherein said group c) is unsubstituted or substituted with a substituent selected from the group consisting of floro, chloro, bromo, iodo, azido, nitro, monoalkyl substituted amino, dialkyl substituted amino, aryl substituted amino, alkanoylamino, arylcarbonylamino, cyano, hydroxy, alkoxy, aryloxy, alkanoyloxy, arylcarbonyloxy, mercapto, alkylthio, arylthio, alkanoylthio, arylcarbonylthio, oxyimino, alkoxyimino and carboxy, andn is an integer between 0 and 2.

摘要翻译： 式XII的6β-取代的青霉烷酸：其中A和B各自为氢，其中A和B所连接的碳原子通过单键连接，或 A和B一起形成键，其中A和B连接的碳原子通过双键连接，R 1选自a）氢，b）药学上可接受的盐，和c）药学上可接受的盐 选自C1-10烷基，C2-10烯基，C2-10炔基，C3-10环烷基，C3-10环烯基，烯丙基，芳基，芳烷基，芳烯基，芳炔基，杂环基，杂环基烷基，杂环基烯基，杂环基炔基和 烷基杂环基 其中所述基团c）未被取代或被选自以下的取代基取代：氟，氯，溴，碘，叠氮基，硝基，单烷基取代的氨基，二烷基取代的氨基，芳基取代的氨基，烷酰基氨基，芳基羰基氨基，氰基，羟基， 烷氧基，芳氧基，烷酰氧基，芳基羰氧基，巯基，烷硫基，芳硫基，烷酰硫基，芳基羰硫基，氧亚氨基，烷氧基亚氨基和羧基，n为0〜2的整数。

公开(公告)号：US06300331B1

公开(公告)日：2001-10-09

申请号：US09508044

申请日：2000-03-03

申请人： Kazuharu Noguchi ,  Motoji Wakida ,  Kenji Suzuki ,  Yuji Yamada ,  Tetsuji Asao

发明人： Kazuharu Noguchi ,  Motoji Wakida ,  Kenji Suzuki ,  Yuji Yamada ,  Tetsuji Asao

IPC分类号： A61K31473

CPC分类号： C07D221/14 ,  C07D401/14 ,  C07D471/04

摘要： The present invention relates to a naphthalimidobenzamide derivative represented by the following formula (1): (wherein, R1 represents a hydrogen atom, etc., Y represents a hydrogen atom or —CON(R4)—A2—X2, R2 and R4 are the same or different and each independently represents a hydrogen atom, etc., A1 and A2 are the same or different and each independently represents an alkylene group which may be interrupted at least once by —N(R3)— (R3 representing a hydrogen atom, etc.) and X1 and X2 are the same or different and each independently represents a (hetero)aryl group which may have a substituent, etc.) or salt thereof; and a pharmaceutical comprising it as an effective ingredient. The compound is useful as an antitumor agent and the like.

摘要翻译： 本发明涉及由下式（1）表示的萘二甲酰亚胺酰胺衍生物:(其中，R1表示氢原子等，Y表示氢原子或-CON（R4）-A2-X2，R2和R4表示 相同或不同，各自独立地表示氢原子等，A1和A2相同或不同，并且各自独立地表示可以被-N（R3） - （R3表示氢原子， 等等），X 1和X 2相同或不同，并且各自独立地表示可以具有取代基的（杂）芳基等）或其盐; 和包含它作为有效成分的药物。 该化合物可用作抗肿瘤剂等。