182133-43-3Relevant academic research and scientific papers
MODULATORS OF ESTROGEN RECEPTOR PROTEOLYSIS AND ASSOCIATED METHODS OF USE
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, (2018/08/20)
The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a cereblon, Von Hippel-Lindau ligase-binding moiety, Inhibitors of Apotosis Proteins, or mouse double-minute homolog 2 ligand, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
Treatment of central nervous system disorders with selective estrogen receptor modulators
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, (2008/06/13)
The present invention provides a method of treating depression, mood swings, or Alzheimer's disease in a patient in need of such treatment by administering a selective estrogen receptor modulating compound of the formula in which R1 and R2 are independently hydroxy and alkoxy of one to four carbon atoms; and R3 and R4 are independently methyl or ethyl, or R3 and R4, taken together with the nitrogen atom to which they are attached, form a pyrrolidino, methyl-pyrrolidino, dimethylpyrrolidino, piperidino, morpholino, or hexamethyleneimino ring.
Benzothiophene compounds, intermediates, compositions, and methods
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, (2008/06/13)
The present invention provides intermediate compounds and processes for the preparation of compounds of formula I STR1 wherein R1a is --H or --OR7a in which R7a is --H or a hydroxy protecting group; R2a is --H, halo, or --OR8a in which R8a is --H or a hydroxy protecting group; R3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; and Z is --O-- or --S--; or a pharmaceutically acceptable salt thereof.
Benzothiophene compounds, intermediates, compositions, and methods
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, (2008/06/13)
The present invention provides a method for inhibiting endometriosis comprising administering to a woman an effective amount of a compound of formula I STR1 wherein R1a is --H or --OR7a in which R7a is --H or a hydroxy protecting group; R2a is --H, halo, or --OR8a in which R8a is --H or a hydroxy protecting group; R3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; and Z is --O-- or --S--; or a pharmaceutically acceptable salt thereof.
Benzothiophene compounds, intermediates, compositions, and methods
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, (2008/06/13)
A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I wherein R1a is --H or --OR7a in which R7a is --H or a hydroxy protecting group; R2a is --H, halo, or --OR8a in which R8a is --H or a hydroxy protecting group; R3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; and Z is --O-- or --S--; or a pharmaceutically acceptable salt thereof, and further comprising administering to said woman an effective amount of progestin.
Benzothiophene compounds, intermediates, compositions, and methods
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, (2008/06/13)
A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I wherein R1a is -H or -OR7a in which R7a is -H or a hydroxy protecting group; R2a is -H, halo, or -OR8a in which R8a is -H or a hydroxy protecting group; R3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; and Z is -O-or -S-; or a pharmaceutically acceptable salt thereof, and further comprising administering to said woman an effective amount of estrogen.
