Sesquiterpene derivatives having progesterone receptor binding i

Details Sesquiterpene derivatives having progesterone receptor binding i Sesquiterpene derivatives having progesterone receptor binding i

1997-06-19

1998-10-06

Fan, Jane

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

549299, A61K 31365, C07D30792

Patent

active

058178163

ABSTRACT:
Sesquiterpene derivatives, represented by the following formulae (I) and (II), having progesterone receptor binding inhibitory activity are disclosed. They can be used as therapeutic and prophylactic agents for progesterone-related diseases, for example, as a carcinostatic agent for breast cancer or ovarian cancer, a therapeutic agent for hysteromyoma, endometriosis, meningioma, or myeloma, an abortifacient, an oral contraceptive pill, or a therapeutic or prophylactic agent for osteoporosis or climacteric disturbance. These compounds have no steroid skeleton and, hence, are considered to be advantageously free from side effect inherent in steroid such as found in conventional progesterone receptor binding inhibitors having a steroid skeleton. ##STR1## wherein R.sup.1 represents a hydrogen atom, a halogen atom, C.sub.1 -C.sub.5 alkoxy, or phenylthio; R.sup.2 represents C.sub.1 -C.sub.5 alkoxy or C.sub.2 -C.sub.5 alkanoyloxy; and ---- with letters a, b, c, d, and e attached thereto represent a double bond or a single bond; R.sup.3 has the same meaning as R.sup.2 ; and R.sup.4 represents C.sub.1 -C.sub.5 alkoxy.

REFERENCES:
patent: 5663196 (1997-09-01), Sari et al.
patent: 5712306 (1998-01-01), Tabata et al.
F. Bohlmann et al., Phytochemistry, 17 (7), 1173-1178 (1978).

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