N-(2-(pyridinyl)-4-pyrimidinyl)-aminomethylenemalonates and analogs
US4018770A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Mar 3, 1975 |
| Grant date | Apr 19, 1977 |
| Priority date | — |
| Expiry date | Mar 3, 1995 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K31/505
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Compounds useful as anti-allergic agents are 2-Q-4-[XZC=C(R)NH]-5-R.sub.1 -6-R.sub.2 -pyrimidines (I), where Q is 4- or 3- or 2-pyridinyl or 4- or 3- or 2-pyridinyl having one or two lower-alkyl substituents or N-oxide thereof, R is hydrogen or lower-alkyl, R.sub.1 is hydrogen, lower-alkyl or cyano, R.sub.2 is hydrogen, lower-alkyl, hydroxy or halo, X and Z are the same or different and are each selected from lower-carbalkoxy, lower-alkanoyl, carbamyl and cyano, or ##STR1## where R.sub.3 and R.sub.4 are each lower-alkyl, or X is hydrogen, are prepared by reacting 4-amino-2-Q-5-R.sub.1 -6-R.sub.2 -pyrimidine (II where Q' is amino) with R'O-C-(R)=CXZ (III). Preparations of II are given. Also shown as intermediates and/or anti-allergic agents are 4-(AcNH)-2-Q-5-R.sub.1 -6-R.sub.2 -pyrimidines (IV) and 4-(R.sub.5 R.sub.6 N)-2-Q-5-R.sub.1 -6-R.sub.2 -pyrimidines (V) where Ac is lower-alkanoyl or lower-carbalkoxy, R.sub.5 is hydrogen, lower-alkyl or lower-hydroxyalkyl, and R.sub.6 is lower-alkyl or lower-hydroxyalkyl.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.