Invention Grant
- Patent Title: Substituted 1,2,3,4-tetrahydroisoquinoline derivatives for the treatment of hormone-dependent diseases
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Application No.: US14912709Application Date: 2014-08-01
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Publication No.: US09708305B2Publication Date: 2017-07-18
- Inventor: Donald Poirier , René Maltais
- Applicant: UNIVERSITÉ LAVAL
- Applicant Address: CA Québec
- Assignee: UNIVERSITÉ LAVAL
- Current Assignee: UNIVERSITÉ LAVAL
- Current Assignee Address: CA Québec
- Agent Beatrice Ngatcha
- International Application: PCT/CA2014/050728 WO 20140801
- International Announcement: WO2015/024111 WO 20150226
- Main IPC: C07D217/04
- IPC: C07D217/04 ; C07D217/06 ; C07D217/08 ; C07D401/10 ; C07D401/12 ; C07D401/14 ; A61K31/472 ; A61K31/4725 ; C07D409/14 ; A61K31/496 ; A61K31/506 ; A61K31/5377 ; A61K31/541 ; C07D405/14 ; C07D405/12 ; A61K45/06

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═O, 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, Cl, 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.
Public/Granted literature
- US20160200685A1 SUBSTITUTED 1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES FOR THE TREATMENT OF HORMONE-DEPENDENT DISEASES Public/Granted day:2016-07-14
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