Non-steroidal, tetracylic compounds for estrogen-related treatments

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United States of America Patent

PATENT NO 6686371
APP PUB NO 20030144313A1
SERIAL NO

10240129

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The invention provides non-steroidal estrogenic compounds with estrogenic and anti-estrogenic compounds effects for treatment of estrogen-deficiency related disorders, which compounds are having formula (I) wherein, one of R.sup.a or R.sup.b is 'R.sup.e ; R.sup.e and 'R.sup.e are OH, optionally independently etherified or esterified; X is N or --C(R.sup.1)--, wherein R.sup.1 is H.sub.1 halogen, CN, optionally substituted aryl, (1C-4C)alkyl, (2C-4C)alkenyl, (2C-4C)alkynyl or (3C-6C)cycloalkyl, which alkyl, alkenyl, alkynyl and cycloalkyl groups can optionally be substituted with one or more halogens; Y is N or --C(R.sup.2)--, with the proviso that X and Y are not both N, wherein R.sup.2 has the same meaning as defined for R.sup.1 ; Z is C(R.sup.3,'R.sup.3)-- or --C(R.sup.4,.varies.R.sup.4)--C(R.sup.5,'R.sup.5)--, wherein R.sup.3, 'R.sup.3, R.sup.4, 'R.sup.4, R.sup.5, and 'R.sup.5, independently arc H, (1C-4C)alkyl, (2C-4C)alkenyl or (3C-6C) cycloalkyl, which alkyl, alkenyl and cycloalkyl groups can optionally be substituted with one or more halogens. These compounds are useful for estrogen-receptor related treatments in view of a desirable profile of activity for estrogen .alpha. and estrogen .beta. receptors. ##STR1##

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Patent Owner(s)

  • N.V. ORGANON

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
De, Zwart Eduard Willem Oss, NL 2 8
Loozen, Hubert Jan Jozef Uden, NL 26 30
Mestres, Jordi Edinburgh, GB 5 11
Veeneman, Gerrit Herman Schaijk, NL 11 22

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