Back to results
US 4,727,073 AGranted
Pyrimidine derivatives and composition of the same
AssigneeFujisawa Pharmaceutical Co., Ltd.
InventorsTakao Takaya, Hisashi Takasugi, Atsushi Kuno, Yoshie Sugiyama
Life of this patent
Estimating the term…
Abstract
The invention relates to new pyrimidine derivatives, useful in the treatment of cerebrovascular disease, of the formula: ##STR1## wherein Ar, R.sup.1, R.sup.2 and R.sup.3 are defined in the specification.
Claims11
Pyrimidine derivatives of the formula:
- ##STR14## wherein Ar is phenyl group substituted with 1 to 3 substituent(s) selected from the group consisting of nitro, halo(lower)alkyl, lower alkoxy and a group of the formula:
- ##STR15## (in which l, R.sup.4, R.sup.5 and R.sup.6 are each as defined in the below);
- R.sup.1 is lower alkoxycarbonyl group, lower alkanoyl group, hydroxy(lower)alkyl group or a group selected from the following formulas:
- ##STR16## (in which R.sup.7, R.sup.8, and A are each as defined in the below);
- R.sup.2 is hydrogen, lower alkyl group or a group of the formula:
- ##STR17## (in which Q, R.sup.7 and R.sup.8 are each as defined in the below);
- R.sup.3 is lower alkyl or phenyl group;
- l is an integer of 0, 1 to 6;
- R.sup.4, R.sup.5 and R.sup.6 are each hydrogen or halogen;
- R.sup.7 and R.sup.8 are each hydrogen, optionally substituted N-containing heterocyclic group selected from the group consisting of imidazolinyl and piperidyl or lower alkyl group optionally substituted with 1 to 3 substituent(s) selected from the group consisting of mono- or di(lower)alkylamino, and optionally substituted N-containing heterocyclic group selected from the group consisting of morpholinyl and pyrrolidinyl;
- or
- R.sup.7 and R.sup.8 are taken together to form an optionally substututed N-containing heterocyclic group with the adjacent nitrogen atom selected from the group consisting of 1-piperazinyl, 1-homopiperazinyl, morpholino, thiomorpholino, piperidino, 1,4-diazabicyclo [4.3.0]nonan-4-yl, 1-imidazolyl and phthalimido;
- A and Q are each straight or branched lower alkylene group which may be substituted with a lower alkylidene;
- provided that R.sup.1 is a group of the formula:
- ##STR18## (in which R.sup.7, R.sup.8 and A are each as defined above) when R.sup.2 is hydrogen or lower alkyl group;
- and their pharmaceutically acceptable salts.
13 more elements
Dependencies are inferred from the claim text.