The present invention aims to demonstrate that a soluble pharmaceutical formulation can be prepared of N,N'-Diamino-diphenyl sulfone which is useful in the development of an ideal drug for use against cerebral infarction, epilepsy, traumatic spinal cord injury, cranio-encephalic trauma, leprosy, Pneumocystis carinii infections and any condition which requires rapid and complete absorption of the compound. As a representative example of this application, the dissolution of N,N'-Diamino-diphenyl sulfone was evaluated as a neuroprotector in a model of acute cerebral infarction in rats. In this study, N,N'-Diamino-diphenyl sulfone showed significant prevention of brain damage, without presenting adverse effects in animals. It is also shown that the soluble pharmaceutical formulations prepared in this manner produce peak blood levels 30 minutes from oral administration and immediately via the intravenous route.

Altagracia Martinez; Marina

Rios Castaneda; Luis Camilo

Kravzov Jinich; Jaime

Diaz Ruiz; Maria de los ngeles Araceli

Universidad Autonoma Metropolitana

Soluble pharmaceutical formulations of N,N'-diaminodiphenyl sulfone for optimal use in the treatment of various diseases

Novel pyrazine derivatives are disclosed. The compounds possess a potent platelet aggregation-inhibiting activity and are effective for preventing diseases caused by aggregation of the platelet, for example, myocardial infarction and cerebral thromobsis. Representative examples of the pyrazine derivatives includes 2,3-bis(p-chlorophenyl)-5-methylpyrazine, 2,3-bis(p-methoxyphenyl)-5-methylpyrazine, 2,3-diphenyl-5-benzylpyrazine, 2,3-diphenyl-5-(p-methoxybenzyl)pyrazine, 2,3-bis(p-methoxyphenyl)-5-isopropylpyrazine, 2,3-bis(p-methoxyphenyl)-5-(2-thienylmethyl)pyrazine and 2,3-bis(p-methoxyphenyl)-5,6-dimethylpyrazine.The pyrazine derivatives can be generally prepared by heating a benzil derivative and a 1,2-diaminoethane derivative to produce a dihydropyrazine derivative and heating the resulting compound with sulfur at 100.degree.-180.degree. C.

Terumo Kabushiki Kaisha

Pyrazine derivatives useful as platelet aggregation inhibitors

diphenyl

infarction

diphenyl/infarction

Soluble pharmaceutical formulations of N,N'-diaminodiphenyl sulfone for optimal use in the treatment of various diseases

Pyrazine derivatives useful as platelet aggregation inhibitors

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