Council of Scientific and Industrial Research

Sangita

Girish Kumar Jain

Man Mohan Singh

Atul Kumar

Suprabhat Ray

Puvvada Sri Ramanchandra Murthy

Novel mercaptophenyl naphthyl methane compounds, their pharmaceutically acceptable salts and compositions comprised thereof are useful for the prevention or treatment of various medical indications associated with estrogen dependent diseases or syndromes related to osteoporosis, bone loss, bone formation, cardiovascular disorders, neurodegenerative disorders, menopausal disorders, physiological disorders, diabetes disorders, prostatic carcinoma, cancer of breast, cancer of uterus, cancer of the cervix and cancer of the colon, threatened or habitual abortion, obesity, ovarian development or function, post-partum lactation and depression.

Mercaptophenyl naphthyl methane compounds and synthesis thereof

The present invention relates to compounds of the formula I in which substituents Rand Rare arranged in trans-configuration: wherein: wherein Y is chosen from NHR, NR, NHCOR, NHSOR, CONHR, CONR, CONR, COOH, COOR, SOR, SOR, SONHR, SONR, a C3-C7 heterocyclic ring, saturated or unsaturated, containing one or two heteroatoms independently selected from the group consisting of O, S and N, optionally being substituted with 1 to 3 substituents independently selected from the group comprising H, OH, halogen, nitro, cyano, SH, SR, trihalo-C1-C6-alkyl, C1-C6-alkyl and C1-C6-alkoxy, preferably NHR, NR, or a nitrogen heterocycle, wherein Ris as defined above, and the esters, ethers, and salts of the compounds of formula I, optionally along pharmaceutically acceptable excipients, a process for the preparation of the same, and a method of preventing and/or treating estrogen-related disease conditions in a subject using compounds of formula 1, or its salts, optionally along with pharmaceutically acceptable excipients.

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