Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1994-04-19
1995-11-07
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514249, 514250, 514255, A61K 31495
Patent
active
054648335
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP93/01144 filed Aug. 12, 1993.
The present invention relates to a novel apoptosis regulating composition.
The apoptosis regulating composition of the invention comprises, as an active ingredient, at least one member of the class consisting of carbostyril derivatives represented by any of the following general formula (1) through general formula (6) (hereinafter referred to as compound (1) through compound (6) respectively) and 6-[4-(3,4-dimethoxybenzoyl)-1-1,2,3,4-tetrahydropyrazyl]-3,4-dihydrocarbos tyril (hereinafter referred to as compound (7)) inclusive of salts thereof. ##STR2## wherein R is a benzoyl group which may optionally have, on the phenyl ring thereof, one to three substituents each selected from the group consisting of lower alkoxy groups, halogen atoms, lower alkyl groups, lower alkanoylamino groups and lower alkylthio groups; a lower alkylenedioxybenzoyl group; a hydrogen atom; a pyridylcarbonyl group; a lower alkanesulfonyl group; a lower alkynyl group; or a phenyl-lower alkyl group which may optionally have, on the phenyl ring thereof, one to three substituents each selected from the group consisting of lower alkoxy groups, halogen atoms and lower alkyl groups; the carbon-carbon bond between the 3 and 4 positions of the carbostyril skeleton is a single bond or a double bond; R.sup.20 is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a phenyl-lower alkyl group; and R.sup.21 is a hydrogen atom or a lower alkoxy group; provided, however, that where both of R.sup.20 and R.sup.21 are hydrogen atoms, R should not be a benzoyl group which may have a lower alkoxy group as a phenyl ring substituent; and salts thereof; ##STR3## wherein R.sup.1 is a group of the formula ##STR4## (R.sup.3 being a hydrogen atom or a benzoyl group and R.sup.4 being an oxo group) and the carbon-carbon bond between the 3 and 4 positions of the carbostyril skeleton is a single bond or a double bond; and salts thereof; ##STR5## wherein R.sup.5 is a lower alkanoyl group, a lower alkoxycarbonyl group, a lower alkoxycarbonyl-lower alkyl group, a phenyl-lower alkyl group having a lower alkanoyloxy group or a hydroxyl group on the phenyl ring thereof, or a benzoyl group which may optionally have, on the phenyl ring thereof, at least one substituent selected from the group consisting of a hydroxyl group and amino groups optionally having a lower alkyl group, or a naphthoyl group, and R.sup.6 is a benzoyl group which may optionally have at least one lower alkoxy group on the phenyl ring thereof; and salts thereof; ##STR6## wherein R.sup.7 is a piperazinyl group, R.sup.8 is a hydrogen atom or a lower alkyl group, R.sup.9 is a hydrogen atom or a phenyl-lower alkyl group, and the carbon,carbon bond between the 3 and 4 positions of the carbostyril skeleton is a single bond or a double bond; and salts thereof; ##STR7## wherein R.sup.22 is a C.sub.1 -C.sub.16 alkyl group, a phenyl-lower alkoxycarbonyl-lower alkyl group, an amido-lower alkyl group which may optionally have at least one lower alkyl group, or a phenyl-lower alkyl group and R.sup.23 is a piperazinyl group which may optionally have a lower alkyl group in the 4 position of the piperazine ring; and salts thereof; ##STR8## wherein R.sup.24 is a hydrogen-atom, a phenyl-lower alkyl group, a benzoyl-lower alkyl group, or a benzoyl group which may optionally have one to three lower alkoxy groups or a lower alkylenedioxy group on the phenyl ring thereof; and salts thereof; and 6-[4-(3,4-Dimethoxybenzoyl)-1-1,2,3,4-tetrahydropirazyl]-3,4-dihydrocarbos tyril and salts thereof;
Regarding the above compounds (1) to (6) and (7) (carbostyril derivatives) and the processes available for production thereof, the descriptions in the following literature can be consulted and are incorporated herein by reference: Japanese Patent Kokai Publication No. 83677/1983, No. 267556/1986, No. 230687/1988, No. 34963/1989, Synopsis of the 111st Congress of Pharmaceutical Society of Japan 29TD11-1 (published Mar. 5, 1991), Japanese P
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Adachi Masakazu
Aihara Koutoku
Akamatsu Seiji
Iba Hitomi
Ichikawa Hiroyuki
Henley III Raymond
MacMillan Keith
Otsuka Pharmaceutical Co. Ltd.
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