Inventors:
Dennis Carson - La Jolla CA, US
Lorenzo Leoni - San Diego CA, US
Mary Corr - San Diego CA, US
International Classification:
A61K031/7052, A61K031/4745, A61K031/407, A61K031/675
US Classification:
514/023000, 514/081000, 514/291000, 514/381000, 514/411000
Abstract:
The present invention provides a therapeutic method to treat non-malignant diseases characterized by the excessive tissue growth, e.g., hyperplastic diseases, comprising administering to a mammal (e.g., human) afflicted with excessive tissue growth, an effective amount of a derivative of an indole compound of formula (I):formula (I):
wherein Ris lower alkyl, (hydroxy)lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, phenyl, benzyl or 2-thienyl; R, R, Rand Rare the same or different and are each hydrogen or lower alkyl; each Ris individually hydrogen, lower alkyl, hydroxy, (hydroxy)lower alkyl, lower alkoxy, benzyloxy, lower alkanoyloxy, nitro or halo, Ris hydrogen, lower alkyl or lower alkenyl, X is oxy and thio, Y is carbonyl, —(CH)—, —(C-C)alkyl(CO)—, or —(CH)SO—; Z is hydroxy, lower alkoxy, (C-C)acyloxy, —N(R)(R), phenylamino, (-(4-pyridyl)(C-Calkoxy), (-((R)(R) amino)(C-Calkoxy), an amino acid ester of (-(HO)(C-C))alkoxy, —N(R)CH(R)COH, 1′-D-glucuronyloxy, —SOH, —POH, —N(NO)(OH), —SONH, —PO(OH)(NH), —OCHCHN(CH), or tetrazolyl; wherein Rand Rare each H, (C-C)alkyl or together with N are a 5- or 6-membered heterocyclic ring comprising 1-3 N(R), S or nonperoxide O; n is 0, 1, 2, or 3; wherein Rand Rare each H, (C-C)alkyl or together with N are a 5- or 6-membered heterocyclic ring comprising 1-3 N(R), S or nonperoxide O; each alkyl or phenyl group of R, R, R, R, R, R, Rand Z is optionally substituted with 1, 2, or 3 (C-C)alkyl groups; or a pharmaceutically acceptable salt thereof.