Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-10-20
1997-12-30
Berch, Mark L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544267, 544271, A61K 3152, C07D47312, C07D47306, C07D47310
Patent
active
057030855
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to novel xanthine derivatives and pharmaceutically acceptable salts thereof which have adenosine A.sub.2 receptor antagonistic activity and are useful for the treatment or prevention of various kinds of diseases caused by hyperergasia of adenosine A.sub.2 receptors (for example, Parkinson's disease, senile dementia, depression, asthma, and osteoporosis).
BACKGROUND ART
It is known that adenosine exhibits neurotransmitter depressing activity Physiol. Scand., 131, 287(1987)!, and the like, via A.sub.2 receptors. Therefore, adenosine A.sub.2 receptor antagonists (hereinafter referred to as A.sub.2 -antagonists) are expected as therapeutic or preventive agents for various kinds of diseases caused by hyperergasia of adenosine A.sub.2 receptors, for example, therapeutic agents for Parkinson's disease, antidementia agents, antidepressants, anti-asthmatic agents, and therapeutic agents for osteoporosis. ##STR2##
It is known that adenosine antagonistic activity is found in compounds represented by Formula (A) in which R.sup.1a and R.sup.2a independently represent methyl or propyl, R.sup.3a represents hydrogen, and R.sup.4a represents substituted or unsubstituted phenyl, aromatic heterocyclic (1991)!. Further, Japanese Published Examined Patent Application No. 26516/72 discloses, as cerebral stimulants, compounds represented by Formula (B) in which R.sup.1b and R.sup.2b independently represent methyl or ethyl, R.sup.3b represents methyl, y.sup.1b and y.sup.2b represent hydrogen, and Z.sup.b represents phenyl or 3,4,5-trimethoxyphenyl. WO92/06976 discloses, as compounds having an adenosine A.sub.2 receptor antagonistic activity and therapeutic effects on asthma and osteoporosis, compounds represented by Formula (B) in which R.sup.1b and R.sup.2b independently represent hydrogen, propyl, butyl, or allyl, R.sup.3b represents hydrogen or lower alkyl, y.sup.1b and y.sup.2b independently represent hydrogen or methyl, and Z.sup.b represents substituted or unsubstituted phenyl, pyridyl, imidazolyl, furyl, or thienyl. Further, it is known that adenosine A.sub.2 receptor antagonistic activity is found in compounds represented by Formula (B) in which R.sup.1b and R.sup.2b independently represent methyl, ethyl, propyl, or allyl, R.sup.3b represents hydrogen or methyl, y.sup.1b and y.sup.2b represent hydrogen, 36, 1333 (1993)!. Furthermore, among compounds represented by Formula (B) in which R.sup.1b, R.sup.2b and R.sup.3b represent methyl, and y.sup.1b and y.sup.2b represent hydrogen, respectively, also known are a compound 1525 (1986)!, and a compound in which Z.sup.b represents pyridyl, Abst. 60, 1741h (1964)!, although there is no description with regard to the pharmacological activity of any of these compounds.
DISCLOSURE OF THE INVENTION
The present invention relates to xanthine derivatives and pharmaceutically acceptable salts thereof represented by Formula (I): ##STR3## in which R.sup.1, R.sup.2, and R.sup.3 independently represent hydrogen, lower alkyl, lower alkenyl, or lower alkynyl, R.sup.4 represents lower alkyl, or substituted or unsubstituted aryl, R.sup.5 and R.sup.6 independently represent hydrogen, lower alkyl, and lower alkoxy, or R.sup.5 and R.sup.6 are combined together to represent --O--(CH.sub.2)p--O-- (p is an integer of 1 to 3), n represents 0,1, or 2, and m represents 1 or 2.
Hereinafter, the compounds represented by Formula (I) are referred to as Compounds (I). The same shall apply to the compounds represented by other Formulae.
In the definitions of the groups in Formula (I), lower alkyl and the alkyl moiety of lower alkoxy mean straight-chain or branched alkyl group having 1 to 6 carbon atoms such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, neopentyl and hexyl; lower alkenyl means straight-chain or branched alkenyl group having 2-6 carbon atoms such as vinyl, allyl, methacryl, crotyl, 3-butenyl, 2-pentenyl, 4-pentenyl, 2-hexenyl and 5-hexenyl; lower alkynyl means a straight-chain or branched alkynyl group ha
REFERENCES:
Kato's Integrated English-Japanese Medical Dictionary (Nanzando, 1979) p. 757.
Jacobsen J. Med. Chem., vol. 36, No. 10 (1993) 1333-42.
Ichikawa Shunji
Kase Hiroshi
Kitamura Shigeto
Koike Nobuaki
Nakamura Joji
Berch Mark L.
Kyowa Hakko Kogyo Co. Ltd.
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