Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
The present invention relates to compounds of the formula I in which substituents R2and R3are arranged in trans-configuration:wherein:R1is H or C1-C6 alkyl; C3-C7 cycloalkyl;R2is phenyl, optionally substituted with 1 to 5 substituents independently selected from the group comprising OH, C1-C6-alkyl, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkoxy and phenyl, wherein R4is C1-C6 alkyl;R3is phenyl substituted with OR5wherein R5has the formula (II), (III) or (IV)wherein Y is chosen from NHR4, NR42, NHCOR4, NHSO2R4, CONHR4, CONR4, CONR42, COOH, COOR4, SO2R4, SOR4, SONHR4, SONR42, 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, SR4, trihalo-C1-C6-alkyl, C1-C6-alkyl and C1-C6-alkoxy, preferably NHR4, NR24, or a nitrogen heterocycle, wherein R4is 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.
patent: 5985306 (1999-11-01), Jacobsen et al.
patent: 5994390 (1999-11-01), Jacobsen et al.
patent: 6043269 (2000-03-01), Jacobsen et al.
patent: 6316494 (2001-11-01), Jacobsen et al.
Verma, P et al ‘Mechanism of action of nonsteroidal antiestrogens: a possible link with antiinflammatory activity’ CA 111:224813 (1989).
Branham, Phytoestrogens and mycoestrogens bind to the rat uterine estrogen receptor, J. Nutr. 132:658-664, (2002).
Tripathi et al. STN Accession No. 2005:412580;Document No. 142:411230;abstract of the IN 186459, Filing date Sep. 1, 2001.
Verma et al. STN Accession No. 1989:624813; Document No. 111:224813; abstract of (Indian Journal of Pharmaceutical Sciences, 1989, 51(2), 48-50).
Johnston et al., “Idoxifene Antagonizes Estradiol-dependent MCF-7 Breast Cancer Xenograft Growth through Sustained Induction of Apoptosis,”Cancer Research, vol. 59, pp. 3646-3651, Aug. 1, 1999.
Jordan, et al, “Determination and Pharmacology of an New Hydroxylated Metabolite of Tamoxifen Observed in Patient Sera during Therapy for Advanced Breast Cancer,”Cancer Research, vol. 43, pp. 1446-1450, Mar. 1983.
Blair et al., “The Estrogen Receptor Relative Binding Affinities of 188 Natural and Xenochemicals: Structural Diversity of Ligands,”Toxicology Sciences, vol. 54, pp. 138-153 (2000).
Jain Girish Kumar
Singh Man Mohan
Butler, Esq. Gregory B.
Chandrakumar Nizal S
Counsel of Scientific and Industrial Research
Edwards Angell Palmer & & Dodge LLP
Seaman D. Margaret
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