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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Hauptverfasser: LJABRI FERNAN, GOT'E SIL'VAN, MERAN IV
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creator LJABRI FERNAN
GOT'E SIL'VAN
MERAN IV
description 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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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. 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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. 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subjects ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
STEROIDS
title OPTICALLY ACTIVE DERIVATIVES OF BENZOPYRANE, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD FOR TREATMENT OF ESTROGEN-SENSITIVE DISEASES
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