Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1987-10-22
1990-09-25
Ford, John M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514215, 514183, 514221, 514254, 540460, 540501, 540521, 544295, 544250, 544256, 544262, 544278, 544279, 544280, 544292, 544287, 544288, 544253, A61K 31505, C07D40304, C07D40314
Patent
active
049593684
DESCRIPTION:
BRIEF SUMMARY
TECHNOLOGICAL FIELD
This invention relates to a novel therapeutic agent for neurological diseases in the peripheral nervous system and the central nervous system of animals. More specifically, it relates to a novel therapeutic agent for neurological diseases comprising a particular 2-piperazinopyrimidine derivative or its pharmaceutically acceptable salt.
BACKGROUND TECHNOLOGY
In the therapy of neurological diseases, namely disorders in the central nervous system and the peripheral nervous system, therapeutic agents for the central nervous system have been vigorously studied and applied. In contrast, very few therapeutic agents for diseases of the peripheral nervous system, especially disorders of peripheral nerves, have been put to practical use worldwide.
Japanese Laid-Open Patent Publication No. 34912/1977 discloses a pharmaceutical comprising a dispersion or solution of ganglioside in a medium, which is effective for pathology attributed to neural stimulus transmission disorders in the central nervous system and the peripheral nervous system. Only ganglioside (a product named Cronassial is sold in Italy), a natural carbohydrate, disclosed in the above-cited laid-open publication and mecobalamin, a kind of vitamin, have so far been applied clinically to diseases of the peripheral nervous system, but no entirely satisfactory effect has been obtained.
Japanese Patent Publication No. 28548/1984 discloses 2-isopropylaminopyrimidine ortho-phosphate represented by the following formula ##STR2## and a therapeutic agent comprising this compound for treatment of peripheral nerve diseases. As far as the present inventors know, the above compound (common name, isaxonine phosphate to be abbreviated hereinafter as isaxonine) is the first synthetic compound which was used in clinical research on peripheral nerve disorders (La Nouvelle Presse Medicale, vol. 16, pages 1189-1280, 1982). It appears that this compound is not actually marketed now. No synthetic compound has been known which is used for treating peripheral nerve disorders.
Factors acting on the growth and regeneration of nerves are known to exist in an animal. They are called a nerve growth factor (NGF) or a neurotrophic factor. These factors are high-molecular proteins, and many problems exist which have to be technically solved in applying them to neurological diseases.
Japanese Laid-Open Patent Publication No. 222424/1984 discloses that a gangliside mixture extracted from the cow brain or a single component in gangliosides acts promotingly on the proliferation of the primary culture of nerve cells or neuroblastoma cells, and the formation and growth of the neurite, and that it has the same effect as mecobalamin in an animal model of neurological disorder. Furthermore, as stated above, ganglioside is actually used clinically for the treatment of disorders in the peripheral nervous system and the central nervous system (not psychopathy).
Ganglioside, however, is a natural extract originated from an animal of a different species, and the antigenicity of itself or a foreign material contained in it becomes a problem. Another problem is that it is very difficult to specify and define it as a uniform stable substance in drug preparation.
Japanese Laid-Open Patent Publication No. 144,765/1984 discloses a 2-(1-piperazinyl)pyrimidine having the following formula (I) ##STR3## wherein one of P and Q represents hydrogen or a hydroxyl or lower alkyl group and the other represents hydrogen, and X represents a group of the formula CO--R.sub.1 in which R.sub.1 is a lower alkyl group, a group of the formula ##STR4## in which R.sub.2 is hydrogen or a lower alkyl, phenyl, p-hydroxyphenyl, benzyl, p-hydroxybenzyl, hydroxymethyl, 1-hydroxyethyl or 3-indolylmethyl group, R.sub.3 is hydrogen, a lower alkylcarbonyl group, a benzoyl group, an acyl group derived from an amino acid selected from glycine, phenylglycine, alanine, valine, leucine, isoleucine, phenylalanine, tyrosine, serine, threonine and tryptophan, or an acyl group derived from a dipeptide comprised of two of t
REFERENCES:
patent: 4535080 (1985-08-01), Audiau et al.
Awaya Akira
Horikomi Kazutoshi
Isayama Shigeru
Kato Kozi
Kitahara Takumi
Ford John M.
Mitsui Petrochemical Industries Ltd.
Mitsui Pharmaceuticals Inc.
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