Aryl pyrimidine derivatives and uses thereof
US5958934A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Nov 21, 1997 |
| Grant date | Sep 28, 1999 |
| Priority date | — |
| Expiry date | Nov 21, 2017 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D239/42
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT.sub.2B -antagonists. The 5-HT.sub.2B antagonist is a compound of the formula: ##STR1## wherein: R.sup.1 is hydrogen, alkyl, lower alkoxy, hydroxyalkyl, cycloalkyl, cycloalkyl lower alkyl, alkenyl, lower thioalkoxy, halo, fluoroalkyl, --NR.sup.6 R.sup.7, --CO.sub.2 R.sup.8, --O(CH.sub.2).sub.n R.sup.9, or lower alkyl optionally substituted with hydroxy, alkoxy, halo, or aryl; in which PA2 n is 1, 2, or 3; PA2 R.sup.6 and R.sup.7 are hydrogen or lower alkyl; PA2 R.sup.8 is hydrogen or lower alkyl; and PA1 R.sup.9 is hydrogen, lower alkyl, hydroxy, hydroxy lower alkyl, lower alkenyl, or lower alkoxy; PA1 R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halo, or lower fluoroalkyl; PA1 R.sup.3 is optionally substituted aryl other than pyridyl, thienyl, or furanyl; PA1 R.sup.4 is hydrogen, lower alkyl, cycloalkyl, alkenyl, acyl, amino, amido, aryl, --(CH.sub.2).sub.m NR.sup.10 R.sup.11, or lower alkyl optionally substituted by amino, monosubstituted amino, disubstituted amino, hydroxy, carboxy, aryl, lower alkoxy, amido, …
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.