Naphthyl compounds, intermediates, compositions, and methods
US5574190A · kind A · utility
Assignee
Inventor
Key dates
| Filing date | Jun 6, 1995 |
| Grant date | Nov 12, 1996 |
| Priority date | — |
| Expiry date | Jun 6, 2015 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02P20/55
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The present invention provides pharmaceutically active compounds formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl); PA1 R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), or halo; PA1 R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; and PA1 n is 2 or 3; and or a pharmaceutically acceptable salt thereof. Also provided are compounds of formula II ##STR2## wherein R.sup.1a is --H or --OR.sup.5 in which R.sup.5 is a hydroxy protecting group. PA1 R.sup.2a is --H, halo, or --OR.sup.6 in which R.sup.6 is a hydroxy protecting group; and PA1 R.sup.4 is --OH or --CHO; or a pharmaceutically acceptable salt thereof. Further provided are pharmaceutical compositions of compounds of formula I, and methods of using formula I compounds for, inter alia, alleviating the symptoms of post menopausal syndrome and hormonally-dependent cancer, particularly, breast cancer.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.