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2-[Heteroaryl]alkyl-1,2,3,4-tetrahydro-quinoline derivatives for the treatment of cancer etc.
专利权人:
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人:
DIAMOND, MARC,JONES, JEREMY,RENSLO, ADAM
申请号:
NZ58929909
公开号:
NZ589299A
申请日:
2009.04.24
申请国别(地区):
NZ
年份:
2013
代理人:
摘要:
589299 Disclosed are 2-[heteroaryl]alkyl-1,2,3,4-tetrahydro-quinoline derivatives as represented by the general formula (I), wherein: each R1 is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, alkoxy, -OR4, -SR4, -NR4R5, cycloalkyl, heterocycloalkyl, aryl and heteroaryl; R2 is selected from the group consisting of hydrogen, alkyl, alkyl-OH, alkenyl and alkynyl; R3 is aryl, optionally substituted with from 1 to 3 R6 groups; R4 and R5 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl and alkynyl; or R4 and R5 are combined with the nitrogen to which they are attached to form a heterocyclic ring having from 5 to 7 ring members and from 1 to 3 heteroatoms each independently selected from the group consisting of N, O and S; each R6 is independently selected from the group consisting of H, alkyl, alkenyl, alkynyl and alkoxy; L is a linker selected from the group consisting of alkylene, alkenylene, alynylene and cycloalkylene; X is a heteroaryl ring having from 5 to 6 ring members and from 1 to 3 heteroatoms each independently selected from the group consisting of N, O and S, optionally substituted with from 1 to 3 R8 groups; each R8 is independently selected from the group consisting of H, alkyl, alkenyl, alkynyl and alkoxy; and salts and hydrates thereof. Representative compounds include { 2-[2-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)-vinyl]-1-methyl-1,2,3,4-tetrahydro-quinolin-6-yl} -dimethyl-amine and { 2-[2-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)-ethyl]-1-methyl-1,2,3,4-tetrahydro-quinolin-6-yl} -dimethyl-amine. Further disclosed is a pharmaceutical composition comprising a therapeutically effective amount of a compound as defined above or salts or hydrates thereof, optionally in combination with a therapeutically effective amount of a compound selected from the group consisting of an anti-androgen and a LnRH agonist, for the treatment of prostate cancer, ovarian cancer, hepatocellular carcinoma, a
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