Pyrimidine compound and pharmaceutically acceptable salts thereo

Details Pyrimidine compound and pharmaceutically acceptable salts thereo Pyrimidine compound and pharmaceutically acceptable salts thereo

1992-03-30

1994-10-25

Ford, John M.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

5142358, 5142282, 514275, 514252, 544 585, 544295, 544 60, 544 62, 544122, 544324, 544323, C07D23948, C07D40102, C07D40114, A61K 31505

Patent

active

053589459

DESCRIPTION:

BRIEF SUMMARY
FIELD OF THE INVENTION

This invention relates to novel pyrimidines or their pharmaceutically acceptable salts thereof, and novel therapeutic agents for neurological diseases of the peripheral and central nervous systems of animals containing the above compounds as active ingredients.


PRIOR ART

Japanese Patent Publication No. 23,394/1971 discloses that aminopyrimidines represented by the following formula ##STR2## wherein A represents an alkylene group having up to 16 carbon atoms, or a lower alkylene group substituted by an amino group or C.sub.2-5 acylamino group, M represents H, Na, K, NH.sub.4, Mg, Ca or an organic basic ammoniun salt, and n is a value equal to the atomic valency of M, have interesting therapeutic activity, particularly as an anti-melanchoric agent and psychoanaleptic agent in the filed of psychosis. Japanese Laid-Open Patent Publication No. 22044/1976 discloses that dichloro-lower aliphatic carboxylic acid salts of 2-isopropylaminopyrimidine, such as 2-isopropyl-aminopyrimidine dicloroacetate, are useful as a therapeutic agent for a neurological disease. Japanese Laid-Open Patent Publication No. 100477/1977 (Patent Publication No. 28548/1984) discloses that 2-isopropylaminopyrimidine phosphate is useful as a therapeutic agent for a neurological disease. Japanese Laid-Open Patent Publication No. 157575/1979 discloses a process for producing 2-chloropyrimidine in a high yield. A working example in this patent publication describes the preparation of 2-chloropyrimidine in a yield of 69%. Japanese Laid-Open Patent Publication No. 393/1980 discloses a process for producing 2-isopropylamino-pyrimidine in a high yield. A working example of this patent publication describes the preparation of 2-isopropylaminopyrimidine in a yield of 60%.
Japanese Laid-Open Patent Publication No. 122768/1980 discloses that a hydroxy derivative of 2-isopropylaminopyrimidine represented by the following formula ##STR3## wherein A.sup.4, A.sup.5 and A.sup.6 each represent H or OH, and at least one of them represents OH, is useful in the field of nerve regeneration and for treatment of myodystrophy.
Japanese Laid-Open Patent Publication No. 145670/1980 discloses that 2-isopropylaminohalogenopyrimidines represented by the following formula ##STR4## wherein A.sup.4', A.sup.5' and A.sup.6' each represent H or a halogen atom, and at least one of them is a halogen atom, are useful for treatment of various neurological diseases and myodystrophy.
Japanese Laid-Open Patent Publication No. 145,671/1980 discloses a process for producing a hydroxy derivative of 2-isopropylaminopyrimidine. Japanese Laid-Open Patent Publication No. 151,571/1980 discloses that 2-isopropylamino-5-halogenopyrimidines are interesting in the treatment of neurological diseases.
Japanese Laid-Open Patent Publication No. 10177/1981 discloses a process for producing 2-isopropylaminopyrimidine substantially in a quantitative yield by aminolyzing 2-methylsulfornylpyrimidine with isopropylamine.
Japanese Laid-Open Patent Publication No. 26880/1981 discloses a process for producing 2-isopropylaminopyrimidine which comprises reacting bis (isopropylguanidine) sulfate with 1,1,3,3-tetraethoxypropane.
Japanese Laid-Open Patent Publication No. 90,013/1981 describes a therapeutic agent for myodystropy, myopathy, muscle rigidity and/or dysfunction of neuro-musclar transmission comprising substituted derivative of pyrimidine or its therapeutically acceptable salt of its metabolite as an active ingredient. However, it merely discloses various salts such as an or 2-isopropylaminopyrimidine orthophosphate as an active compound.
Japanese Laid-Open Patent Publication No. 65873/1986 discloses that 2-piperazinopyrimidine derivatives of the following formula ##STR5## wherein R.sup.1 is H or aralkyl, and Y is a divalent organic group defined in the claim of this patent publication are useful as a herbicide for paddies and upland farms.
The present inventors previously provided a novel therapeutic agent for neurological diseases comprising a specified 2-piperazinopyrimid

REFERENCES:
Campbell et al, Chemical Abstracts, vol. 97, entry 2/6224b (1982).
Abraham et al., Chemical Abstracts, 70:76976p (1969).
Geerts et al., Chemical Abstracts, 80:107548p (1974).
Naar et al, Chemical Abstracts, 83:43369h (1975).
Warczykowska et al, Chem. Abstracts, 94:3979c (1981).
Fujiwara et al., Chem. Abstracts, 107:198362p (1987).
Tomino et al., Chem. Abstracts, 114:23983j (1991).

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