Title:
NONSTEROIDAL ESTROGEN DERIVATIVES
Document Type and Number:
WIPO Patent Application WO/1997/032837
Kind Code:
A1
Abstract:
Compounds of general formula (I) exhibiting an estrogenic activity and/or anti-estrogenic activity, geometrical isomers of them, and pharmaceutically acceptable salts thereof, wherein R0 is hydrogen or a hydroxyl-protecting group; R1 is hydrogen, halogeno, C1-C6 alkyl, hydroxyl or protected hydroxyl; R2 is hydrogen or -(CH2)k-X-R3; the solid lines with short dashes are each a single bond or a double bond; A is (1) methylene, oxygen or a single bond, or (2) methyne; E is (1) -GR7- or -CO-, or (2) =CR7- or nitrogen; and Z is carboxyl, carbamoyl, hydroxyaminocarbonyl, hydroxymethyl or a protected functional group derived therefrom.
Inventors:
YAMAMOTO MICHIHIRO (JP)
NAKAHIRA HIROYUKI (JP)
WATANABE SHOJI (JP)
KATSUMATA TAKASHI (JP)
NAKAHIRA HIROYUKI (JP)
WATANABE SHOJI (JP)
KATSUMATA TAKASHI (JP)
Application Number:
PCT/JP1997/000600
Publication Date:
September 12, 1997
Filing Date:
February 27, 1997
Export Citation:
Assignee:
SUMITOMO PHARMA (JP)
YAMAMOTO MICHIHIRO (JP)
NAKAHIRA HIROYUKI (JP)
WATANABE SHOJI (JP)
KATSUMATA TAKASHI (JP)
YAMAMOTO MICHIHIRO (JP)
NAKAHIRA HIROYUKI (JP)
WATANABE SHOJI (JP)
KATSUMATA TAKASHI (JP)
International Classes:
C07C59/52; C07C69/732; C07C69/734; C07D295/092; (IPC1-7): C07C39/38; A61K31/045; A61K31/085; A61K31/095; A61K31/165; A61K31/185; A61K31/235; A61K31/27; A61K31/35; A61K31/47; C07C59/52; C07C69/732; C07C69/734; C07C235/32; C07C259/06; C07C271/06; C07C317/46; C07C323/51; C07D217/16; C07D311/58
Foreign References:
| US5032588A | 1991-07-16 | |||
| JPS5053359A | 1975-05-12 |
Other References:
CHEM. PHARM. BULL., (1994), Vol. 42, No. 4, YVES L. JANIN et al., "Synthesis and Biological Properties of New Benz(h)Isoquinoline Derivatives", p. 892-895.
J. MEDICINAL CHEM., (1978), Vol. 21, No. 12, ALEXANDER C. GOUDIE et al., "4-(6-Methoxy-2-Naphthyl)Butan-2-One and Related Analogues, a Novel Structural Class of Antiinflammatory Compounds", p. 1260-1264.
J. MEDICINAL CHEM., (1972), Vol. 15, No. 11, R.R. CRENSHAW et al., "Potential Antifertility Agents. 2. Tetrazole Derivatives of Nonsteriodal Estrogens", pages 1179-1180.
BULL. SOC. CHIM. FR., (1976), No. 5-6, Part 2, RENE MALZIEU, "Nouvelle Synthese en Serie Estrogene", p. 879-882.
J. MEDICINAL CHEM., (1978), Vol. 21, No. 12, ALEXANDER C. GOUDIE et al., "4-(6-Methoxy-2-Naphthyl)Butan-2-One and Related Analogues, a Novel Structural Class of Antiinflammatory Compounds", p. 1260-1264.
J. MEDICINAL CHEM., (1972), Vol. 15, No. 11, R.R. CRENSHAW et al., "Potential Antifertility Agents. 2. Tetrazole Derivatives of Nonsteriodal Estrogens", pages 1179-1180.
BULL. SOC. CHIM. FR., (1976), No. 5-6, Part 2, RENE MALZIEU, "Nouvelle Synthese en Serie Estrogene", p. 879-882.
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