IP Library Granted Patent US 8,487,100
Granted Patent B2
US 8,487,100 · App. 12/967,871 · Granted Jul 16, 2013

Compounds for binding to ER alpha/beta and GPR30, methods of treating disease states and conditions mediated through these receptors and identification thereof

Inventors: Eric R Prossnitz (Albuquerque, NM); Sergey E Tkatchenko (San Diego, CA); Chetana M Revankar (Arlington, VA); Larry A Sklar (Albuquerque, NM); Jeffrey B Arterburn (Las Cruces, NM); Daniel F Cimino (Tijeras, NM); Tudor I Oprea (Albuquerque, NM); Cristian-George Bologa (Albuquerque, NM); Bruce S Edwards (Albuquerque, NM); Alexandor Kiselyov (San Diego, CA); Susan M Young (Albuquerque, NM)
Assignee: STC.UNM
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Quick Facts
Patent No.
US 8,487,100
App. No.
12/967,871
Granted
Jul 16, 2013
Kind
B2
Abstract

The current invention is in the field of molecular biology/pharmacology and provides compounds which modulate the effects of GPR30 as well as the classical estrogen receptors alpha and beta (ERα and ERβ). These compounds may function as agonists and/or antagonists of one or more of the disclosed estrogen receptors. Diseases which are mediated through one or more of these receptors include cancer (particularly breast, reproductive and other hormone-dependent cancers, leukemia, colon cancer, prostate cancer), reproductive (genito-urological) including endometreitis, prostatitis, polycystic ovarian syndrome, bladder control, hormone-related disorders, hearing disorders, cardiovascular conditions including hot flashes and profuse sweating, hypertension, stroke, obesity, osteoporosis, hematologic diseases, vascular diseases or conditions such as venous thrombosis, atherosclerosis, among numerous others and disorders of the central and peripheral nervous system, including depression, insomnia, anxiety, multiple sclerosis, neuropathy, neurodegenerative disoders such as Parkinson's disease and Alzheimer's disease, as well as inflammatory bowel disease, Crohn's disease, coeliac (celiac) disease and related disorders of the intestine. A contraceptive indication to prevent or reduce the likelihood of pregnancy after intercourse is a further aspect of the present invention.

Claims (2)

1. A compound according to the chemical structure:

2. A compound according to any one of the following chemical structures:

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 19, 2018
From: ARTERBURN, JEFFREY B.
To: ARROWHEAD CENTER, INC.
Reel/Frame 044663/0324 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 21, 2012
From: REVANKAR, CHETANA M.; YOUNG, SUSAN M.; CIMINO, DANIEL; PROSSNITZ, ERIC R.; EDWARDS, BRUCE S.; SKLAR, LARRY A.; BOLOGA, CRISTIAN-GEORGE; OPREA, TUDOR I.
To: THE REGENTS OF THE UNIVERSITY OF NEW MEXICO
Reel/Frame 029000/0570 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 21, 2012
From: THE REGENTS OF THE UNIVERSITY OF NEW MEXICO
To: STC.UNM
Reel/Frame 029000/0593 →
Continuity (3)
Division 11497751 · Aug 2, 2006
Provisional Application 60705516 · Aug 4, 2005
Related Publication 20110092533A1 · Apr 21, 2011