Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-12-02
2000-12-26
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514258, 514261, 514245, 544211, 544262, 544277, 544278, C07C23364, C07D47334, C07D48704, A61K 31166, A61K 3152
Patent
active
061660167
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to novel amide derivatives.
PRIOR ART
The derivatives of the invention are novel compounds which have not been published in any literature. An object of this invention is to provide compounds useful as medicine.
DISCLOSURE OF THE INVENTION
The present invention provides novel derivatives represented by the following formula (1). ##STR3##
In the formula (1), ring A represents a benzene ring, a naphthalene ring, a pyridine ring or a furan ring; when ring A is other than a benzene ring, R.sup.1, R.sup.2 and R.sup.3 are all hydrogen atoms, and when ring A is a benzene ring, R.sup.1, R.sup.2 and R.sup.3 are the same or different and independently represent hydrogen, lower alkoxy, halogen, nitro, lower alkyl, halogen-substituted lower alkyl, phenyl, phenoxy, lower alkanoyloxy, hydroxy, lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl.
Further, R.sup.4 represents a heterocyclic group selected from the group consisting of: substituents selected from the group consisting of lower alkyl, phenyl, phenyl(lower)alkyl, phenylthiophenyl and halogen; the 6-position and one of whose nitrogen atoms may have a phenyl(lower)alkyl group as a substituent; and one of whose nitrogen atoms may have a lower alkyl or phenyl(lower)alkyl group as a substituent.
Further, R.sup.5 represents a hydrogen atom or a group represented by ##STR4## wherein A, R.sup.1, R.sup.2 and R.sup.3 are as defined above.
Examples of the groups in the formula (1) are shown below. As regards the groups, the term "lower" means C.sub.1-6.
The lower alkyl group includes straight- or branched-chain lower alkyl groups such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, hexyl and the like.
The lower alkoxy group includes methoxy, ethoxy, propoxy, isopropoxy, butoxy, pentyloxy, hexyloxy and the like.
The phenyl(lower)alkyl group includes benzyl, 1-phenylethyl, 2-phenylethyl, 3-phenylpropyl, 4-phenylbutyl, 5-phenylpentyl, 6-phenylhexyl and the like.
The halogen atom includes fluorine, chlorine, bromine and iodine.
The halogen-substituted lower alkyl group includes trifluoromethyl, pentafluoroethyl, heptafluoropropyl, nonafluorobutyl, undecafluoropentyl, tridecafluorohexyl and the like.
The (lower)alkanoyloxy group includes acetoxy, propionyloxy, butyryloxy, valeryloxy, hexanoyloxy, heptanoyloxy and the like.
The lower alkylthio group includes methylthio, ethylthio, propylthio, butylthio, pentylthio, hexylthio and the like.
The lower alkylsulfinyl group includes methylsulfinyl, ethylsulfinyl, propylsulfinyl, butylsulfinyl, pentylsulfinyl, hexylsulfinyl and the like.
The lower alkylsulfonyl group includes methylsulfonyl, ethylsulfonyl, propylsulfonyl, butylsulfonyl, pentylsulfonyl, hexylsulfonyl and the like.
Of the heterocyclic groups represented by R.sup.4, examples of (1) lower alkyl-substituted thieno[3,2-d]pyrimidin-4-yl groups are 2-methylthieno[3,2-d]pyrimidin-4-yl, 2-ethylthieno[3,2-d]pyrimidin-4-yl, 2-n-propylthieno[3,2-d]pyrimidin-4-yl, 2-n-butylthieno[3,2-d]pyrimidin-4-yl, 2-n-pentylthieno[3,2-d]pyrimidin-4-yl, 2-n-hexylthieno[3,2-d]pyrimidin-4-yl and the like.
Of the heterocyclic groups represented by R.sup.4, examples of (2) pyrazolo[1,5-a]-1,3,5-triazin-4-yl groups optionally having one or two substituents selected from the group consisting of lower alkyl, phenyl, phenyl(lower)alkyl, phenylthiophenyl and halogen include unsubstituted pyrazolo[1,5-a]-1,3,5-triazin-4-yl and the following substituted groups: 2-ethylpyrazolo[1,5-a]-1,3,5-triazin-4-yl, 2-n-propylpyrazolo[1,5-a]-1,3,5-triazin-4-yl, 2-n-butylpyrazolo[1,5-a]-1,3,5-triazin-4-yl, 2-n-pentylpyrazolo[1,5-a]-1,3,5-triazin-4-yl, 2-n-hexylpyrazolo[1,5-a]-1,3,5-triazin-4-yl, 2-phenylpyrazolo[1,5-a]-1,3,5-triazin-4-yl, 2-benzylpyrazolo[1,5-a]-1,3,5-triazin-4-yl, 2-(2-phenylethyl)pyrazolo[1,5-a]-1,3,5-triazin-4-yl, 2-(3-phenylpropyl)pyrazolo[1,5-a]-1,3,5-triazin-4-yl, 2-(4-phenylbutyl)pyrazolo[1,5-a]-1,3,5-triazin-4-yl, 2-(5-phenylpentyl)pyrazolo[1,5-a]-1,3,5-triazin-4-yl, 2-(6-phenylhexyl)pyrazolo[1,5-a]-1,3,5-tria
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Iwamoto Takeshi
Okamura Takashi
Shibutani Tadao
Shoji Yasuo
Yasuda Tsuneo
Otsuka Pharmaceutical Factory Inc.
Rao Deepak R.
Shah Mukund J.
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