Nuclear receptor binding agents
AssigneeGTx, Inc.
InventorsJames T. DALTON, Christina BARRETT, Duane D. MILLER, Seoung-Soo HONG, Yali HE, Michael L. MOHLER, Ramesh NARAYANAN, Zhongzhi WU
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Abstract
The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.
Claims31
A nuclear receptor binding agent (NRBA) compound or its isomer, pharmaceutically acceptable salt, N-oxide, ester, hydrate or any combination thereof, represented by the structure of formula VI:
- wherein
- X is CO;
- R1 and R3, are independently halogen, —CHO, —CHNOH, CH═CHCO2H, hydroxyalkyl group of 1 to 7 carbon atoms, hydroxyl, alkoxy group of 1 to 7 carbon atoms, cyano, CF3, NH2, NHR, NHCOR, sulfonamide, SO2R, aryl or protected hydroxyl;
- R2 is —CHO, —CHNOH, CH═CHCO2H, hydroxyalkyl, hydroxyl, alkoxy, cyano, CF3, NH2, NHR, NHCOR, sulfonamide, SO2R, aryl, or protected hydroxyl;
- R8, R9, and R10 are independently hydrogen, halogen, CHO, CHNOH, CH═CHCO2H, hydroxyalkyl group of 1 to 7 carbon atoms, hydroxyl, alkoxy group of 1 to 7 carbon atoms, cyano, CF3, NH2, NHR, NHCOR, sulfonamide, SO2R, aryl, or protected hydroxyl;
- R is alkyl group of 1 to 7 carbon atoms, hydrogen, haloalkyl group of 1 to 7 carbon atoms, dihaloalkyl group of 1 to 7 carbon atoms, trihaloalkyl group of 1 to 7 carbon atoms, CH2F, CHF2, CF3, CF2CF3, aryl, phenyl, halogen, alkenyl group of 1 to 7 carbon atoms, CN, NO2, or OH;
- and
- j, k, l are independently 1-5.
Dependencies are inferred from the claim text.