C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 491/04 (2006.01) A61K 31/136 (2006.01) A61K 31/167 (2006.01) A61K 31/395 (2006.01) A61K 31/404 (2006.01) A61K 31/407 (2006.01) A61K 31/4166 (2006.01) A61K 31/4184 (2006.01) A61K 31/475 (2006.01) A61K 31/565 (2006.01) A61K 31/573 (2006.01) A61K 31/675 (2006.01) A61P 43/00 (2006.01) C07D 209/00 (2006.01) C07D 331/00 (2006.01) C07D 335/00 (2006.01) C07D 495/04 (2006.01) G01N 33/00 (2006.01)
Patent
CA 2419060
The present invention provides novel indole derivatives of formula (I): (I) wherein R1 is lower alkyl, lower alkenyl, (hydroxy)lower alkyl, lower alkynyl, phenyl, benzyl or 2-thienyl, R2, R3, R4 and R5 are the same or different and are each hydrogen or lower alkyl; each R6 is individually hydrogen, lower alkyl, hydroxy, (hydroxy)lower alkyl, lower alkoxy, benzyloxy, lower alkanoyloxy, nitro or halo, n is 1-3, R7 is hydrogen, lower alkyl or lower alkenyl, X is oxy and thio, Y is carbonyl, (CH2)1-3,(CH2)1-3SO2 or (CH2)1- 3C(O), and Z is (.omega.-(4-pyridyl)(C2-C4 alkoxy), (.omega.-((R8)(R9) amino)(C2-C4 alkoxy), wherein R8 and R9 are each H, (C1-C3)alkyl or together with N are a 5- or 6-membered heterocyclic ring comprising 1-3 N(R8), S or nonperoxide O; an amino acid ester of (.omega.-(HO)(C2-C4))alkoxy, N(R8)CH(R8)CO2H, 1'-D-glucuronyloxy; or Y-Z is (CH2)1-3R8; wherein R8 is OH, (C2-C4)acyloxy, SO3H, PO4H2, N(NO)(OH), SO2NH2, PO(OH)(NH2), or a tetrazolyl; or a pharmaceutically acceptable salt thereof, useful to inhibit cancer or sensitize cancer cells to chemotherapeutic agents, radiation or other anti- cancer treatments.
La présente invention concerne de nouveaux dérivés indoliques utilisés pour inhiber le développement du cancer ou sensibiliser les cellules cancéreuses à des agents chimiothérapeutiques, au rayonnement ou à d'autres traitements contre le cancer.
Carson Dennis A.
Cottam Howard B.
Leoni Lorenzo M.
Smart & Biggar
The Regents Of The University Of California
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