Elliott S. Klein - Marina del Rey CA Alan T. Johnson - Rancho Santa Margarita CA Andrew M. Standeven - Corona del Mar CA Richard L. Beard - Newport Beach CA Samuel J. Gillett - Albany CA Tien T. Duong - Irvine CA Sunil Nagpal - Lake Forest CA Vidyasagar Vuligonda - Irvine CA Min Teng - Aliso Viejo CA Roshantha A. Chandraratna - Mission Viejo CA
Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.
Methods and compositions for inhibiting or preventing spermatogenesis in a male mammal. Also disclosed are compounds and formulations for use in such methods.
Identification Of Nuclear Receptor-Dependent Coregulator Recruitment
Elliott Klein - Danbury CT, US Weizhen Wang - Newport Coast CA, US Roshantha Chandraratna - Laguna Hills CA, US
International Classification:
C12Q001/68
US Classification:
435/006000
Abstract:
Methods for identifying molecules that modulate nuclear receptor transactivation activity. Also disclosed are methods for detecting endogenous nuclear receptor co-factors with increased sensitivity.
Yang-Dar Yuan - Irvine CA, US Scott Thacher - Costa Mesa CA, US Elliott Klein - Danbury CT, US Roshantha Chandraratna - Laguna Hills CA, US
Assignee:
Allergan Sales, Inc. - Irvine CA
International Classification:
A61K031/47 A61K031/353 A61K031/38
US Classification:
514/311000, 514/432000, 514/456000
Abstract:
The current invention relates to methods for treating hyperlipidemia in mammals, including humans. More specifically, the current invention relates to the use of retinoid or retinoid derivative that is able to act as an antagonist or inverse agonist of a retinoid receptor to treat hyperlipidemia.
Methods Of Detecting Dissociated Nuclear Hormone Receptor Ligands
Elliott Klein - Danbury CT, US Weizhen Wang - Newport Coast CA, US Roshantha Chandraratna - Laguna Hills CA, US
International Classification:
G01N033/567
US Classification:
435/007210
Abstract:
The present invention provides a method of identifying an effective agent that dissociates nuclear hormone receptor activities. The method includes the steps of contacting a nuclear hormone receptor with one or more agents under conditions suitable for forming a test complex containing nuclear hormone receptor dimer, coactivator and corepressor; assaying for coactivator association with the test complex; and assaying for corepressor association with the test complex, where coactivator association combined with corepressor association indicates that at least one of the agents is an effective agent that dissociates nuclear hormone receptor activities.
Methods and compositions for inhibiting or preventing spermatogenesis in a male mammal. Also disclosed are compounds and formulations for use in such methods.
Synthesis And Use Of Retinoid Compounds Having Negative Hormone And/Or Antagonist Activities
Elliott Klein - Marina Del Rey CA, US Andrew Standeven - Ventura CA, US Sunil Nagpal - Lake Forest CA, US Roshantha Chandraratna - Mission Viejo CA, US
Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.
Yang-Dar Yuan - Irvine CA, US Scott Thacher - Costa Mesa CA, US Elliott Klein - Danbury CT, US Roshantha Chandraratna - Laguna Hills CA, US
Assignee:
Allergan, Inc. - Irvine CA
International Classification:
A61K031/47 A61K031/382 A61K031/353
US Classification:
514312000, 514456000, 514432000
Abstract:
The current invention relates to methods for treating hyperlipidemia in mammals, including humans. More specifically, the current invention relates to the use of retinoid or retinoid derivative that is able to act as an antagonist or inverse agonist of a retinoid receptor to treat hyperlipidemia.
Workers Compensation Employer Liability Products Liability General Liability Defense Subrogation Administrative and Public Oil & Gas Insurance Labor-Employment Environmental and Natural Resources Litigation: Personal Injury
ISLN:
905839064
Admitted:
1979
University:
State University of New York at Buffalo, B.A., 1975
Law School:
State University of New York at Buffalo, J.D., 1978