Title:
SUBSTITUTED 1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES FOR THE TREATMENT OF HORMONE-DEPENDENT DISEASES
Document Type and Number:
WIPO Patent Application WO/2015/024111
Kind Code:
A8
Abstract:
Provided are compounds of general formula A and A', wherein X1 and X2 are each C, CH or N; R3 and R4 are each H, optionally substituted C1-C30 saturated or unsaturated chemical group, or together form an optionally substituted C5-C8 cycle; Z1; Z2 and Z3 are each N or CH; V is C=0, C=S or CH2; n is from 1 to 12; W1 and W2 are each H, CH2, O or S; and R1 and R2 are each H, Cr1C6 alkyl, C1C6 aryl, C1C12 alkylaryl, optionally substituted phenyl, C1C6 alkoxy, C1C6 thioalkoxy, F, CI, Br or I. These compounds inhibit steroid sulfatase (STS), act as selective estrogen receptor modulators (SERMs), increase alkaline phosphatase (ALP) activity, and are useful in the treatment of medical conditions involving hormones such as breast cancer, prostate cancer, endometriosis, osteoporosis, benign prostatic hyperplasia and endometrial cancer.
Inventors:
POIRIER DONALD (CA)
MALTAIS RENÉ (CA)
MALTAIS RENÉ (CA)
Application Number:
PCT/CA2014/050728
Publication Date:
March 26, 2015
Filing Date:
August 01, 2014
Export Citation:
Assignee:
UNIV LAVAL (CA)
International Classes:
C07D405/14; A61K31/472; A61K31/4725; A61P5/00; A61P5/30; A61P5/32; A61P35/00; C07D401/12; C07D401/14; C07D405/12; C07D409/14
Attorney, Agent or Firm:
GOUDREAU GAGE DUBUC (Montreal, Québec H3A 3H3, CA)
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