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BENZOTHIOPHENE DERIVATIVES AND COMPOSITIONS THEREOF AS SELECTIVE ESTROGEN RECEPTOR DEGRADERS

The present invention relates to compounds of formula I: in which n, m, X, Y 1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.

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Amorphous benzothiophenes, methods of preparation, and methods of use

The instant invention provides an amorphous form of a compound of formula I. wherein: R1and R3are independently hydrogen, -CH3,-CO(C1-C6alkyl), or -COAr, wherein Ar is optionally substituted phenyl; R2is selected from the group consisting of pyrrolidinyl, hexamethyleneimino, and piperidinyl; or a pharmaceutically acceptable salt or solvate thereof. Methods of preparing the material, as well as methods of using same, are also provided.

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Intermediates and processes for preparing benzothiophene compounds

The present invention provides a novel process for preparing a compound of formula I STR1 wherein R1 and R2 combine to form C4 -C6 polymethylene, –CH2 CH(CH3)CH2 CH2 –, –CH2 C(CH3)2 CH2 CH2 –, or –CH2 CH2 OCH2 CH2 –; or a pharmaceutically acceptable salt or solvate thereof. Also provided intermediates of formulae II and IV STR2 wherein Z is a leaving group.

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Inhibition of bone loss by 3-(4-acrylamidobenzoyl) benzo?b!-thiophenes

This invention relates to 3-(4-acrylamidobenzoyl)benzo?b! thiophenes, to the process for their preparation, to pharmaceutical compositions and to their use for modifying the balance between bone resorption and bone production in a mammal. The compounds useful in this invention are represented by the formula STR1 wherein R1 and R2 are independently hydrogen or lower alkyl containing 1-8 carbon atoms, or R1 and R2 together with the interposed nitrogen forms a 5-7 membered ring optionally containing an additional heteroatom selected from nitrogen, sulfur or oxygen.

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Benzothiophene compounds, intermediates, compositions, and methods

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.

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Process for preparing benzoic acids

An improved process for the preparation of 4[(2-piperidin-1-yl)ethoxy]benzoic acid derivatives, comprising reacting a haloalkyl amine of formula (III) with a compound of formula (IV) in the presence of a hydrated inorganic base in an appropriate solvent.

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Anti-mitotic agents which inhibit tubulin polymerization

Methoxy and ethoxy substituted 3-aroyl-2-arylbenzo?b!thiophenes and benzo?b!thiophene analogues are described for use in inhibiting tubulin polymerization. The compounds’ use for treating tumor cells is also described.

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Diarylvinyl sulfoxides

The present invention is directed to new diarylvinyl sulfoxides.

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Glucopyranoside benzothiophenes

A compound of the formula STR1 or a pharmaceutically acceptable salt or solvate thereof. Also provided by the invention are methods of use of the above compounds, and processes for the preparation thereof.

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Methods of use for inhibiting bone loss and lowering serum cholesterol

A method of inhibiting bone loss or resorption, or lowering serum cholesterol, comprising administering to a human in need thereof a compound having the formula STR1 or a pharmaceutically acceptable salt or solvate thereof, in a low dosage amount. Also encompased by the invention is a a pharmaceutical formulation in unit dosage form comprising, per unit dosage, a low dosage amount.

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