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NEW DIHYDROINDOLONE COMPOUNDS,A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
专利权人:
发明人:
오르투노, 쟝-클라우드,코르디, 알렉시스,라코스테, 진-미하엘,페제스, 임레,부르브리지, 미하엘,힉크맨, 존,피에르, 알랭
申请号:
KR1020100074879
公开号:
KR1013091010000B1
申请日:
2010.08.03
申请国别(地区):
KR
年份:
2013
代理人:
摘要:
Dihydroindolone derivatives (I) and their optical and geometric isomers, or addition salts with an acid or base are new. Dihydroindolone derivatives of formula (I) and their optical and geometric isomers, or addition salts with an acid or base are new. m : 1 or 2; n : 1 or 2; A : a pyrrolyl group optionally substituted by 1-3 groups of 1-6C alkyl; X : C(O), S(O) or SO 2; either R 1>;, R 2>; : 1-6C alkyl; or NR 1>;R 2>; : a heterocyclic group; R 3>;R 4>; : a heterocyclic group; R 5>; : H or 1-6C alkyl; and R 6>; : H or halo, where the heterocyclic group is a mono or bicyclic 5-8 membered group (optionally containing one to three heteroatoms of N, O or S, and one or more unsaturations, and optionally substituted by one or more 1-6C alkyl, 1-6C alkenyl, oxo, hydroxy, 1-6C alkoxy, aryl, arylalkyl or arylalkenyl), the aryl is phenyl group optionally substituted by one or more halo or 1-6C alkyl, and X represents the double bond, which is in configuration is Z or E. Independent claims are included for: (1) the preparations of (I); and (2) combination comprising (I) with an anticancer agent comprising genotoxic agents, mitotic poisons, antimetabolites, proteasome inhibitors or kinase inhibitors. [Image] ACTIVITY : Cytostatic. MECHANISM OF ACTION : None given.본 발명은 하기 화학식(I)의 화합물 및 약제에 관한 것이다:상기 식에서, m 및 n은 1 또는 2이고,A는 피롤릴기를 나타내고,X는 C(O), S(O) 또는 SO2기를 나타내고,R1 및 R2는 알킬기이거나이들을 지니고 있는 질소 원자와 함께 헤테로시클릭기를 형성하고,R3 및 R4는 이들을 지니고 있는 원자와 함꼐 헤테로시클릭기를 형성하고,R5는 수소 원자 또는 알킬기를 나타내고,R6은 수소 원자 또는 할로겐 원자를 나타낸다.
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