OPTICALLY ACTIVE DERIVATIVES OF BENZOPYRANE, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD FOR TREATMENT OF ESTROGEN-SENSITIVE DISEASES
FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to new optically active derivatives of benzopyrane of the formula: wherein R1 and R2 are taken independently among group consisting of hydroxyl and radical that can be transformed to hydroxyl in vivo, such as acyloxy-group, -...
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Zusammenfassung: | FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to new optically active derivatives of benzopyrane of the formula: wherein R1 and R2 are taken independently among group consisting of hydroxyl and radical that can be transformed to hydroxyl in vivo, such as acyloxy-group, -OR4,-OC(O)R7 or -OC(O)OR4 (wherein R4 represents alkyl, alkenyl, alkynyl or aryl; and R7 represents amino-, alkylamino-group, aminoalkyl and alkylsulfanyl); and R3 represents -CH2- or -CH2CH2-; or its pharmaceutically acceptable salt wherein indicated compound or salt are optically active since they comprise above 50% (by mass relatively all stereoisomers) of 2S stereoisomers. These compounds elicit inhibitory activity with respect to sexual steroid and can be used in treatment of estrogen-sensitive diseases, such as mammary gland cancer and endometrial cancer. Prepared stereoisomers show good stability in storage and bioavailability as compared with their racemic mixtures. EFFECT: improved treatment method, valuable medicinal properties of compounds. 17 cl, 5 dwg, 3 tbl, 23 ex |
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