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US 6,040,331 AGranted
Nerve cell protective agents
AssigneeMochida Pharmaceutical Co., Ltd.
InventorsIchiro Yamamoto, Manabu Itoh, Masato Shimojo, Yasunobu Yumiya, Takafumi Mukaihira, Yasushige Akada
Life of this patent
Estimating the term…
Abstract
The invention provides novel benzindole derivatives, processes for producing them, as well as a neuroprotective agent, an agent to prevent or treat diseases involving the degeneration, retraction or death of neurons, and an analgesic, each containing the benzindole derivatives as an active ingredient. ##STR1##
Claims13
A compound represented by the following formula (I) or a salt thereof:
- ##STR295## where R.sup.1 represents a hydrogen atom or a straight-chained, branched or cyclic alkyl group having 1-4 carbon atoms which may be substituted by any group selected from the group consisting of one carboxyl group, one alkoxycarbonyl group having 1-4 carbon atoms and one hydroxyl group;
- R represents a phenyl group which may be mono- or disubstituted by any group selected from the group consisting of a halogen atom, an alkyl group having 1-4 carbon atoms which may be substituted by one hydroxyl group, an alkoxyl group having 1-4 carbon atoms which may be substituted by one hydroxyl group, an optionally protected hydroxyl group, a nitro group, an optionally protected amino group, an acetylamino group, a cyano group, an optionally protected carboxyl group, an alkoxycarbonyl group having 1-4 carbon atoms, a carbamoyl group and a trifluoromethyl group;
- either one of R.sup.3 and R.sup.4 represents a hydrogen atom and the other represents a group represented by the following formula (II):
- --NR.sup.6 R.sup.7 (II)
- (where R.sup.6 and R.sup.7 each represent a hydrogen atom, a phenyl group, a benzyl group, an alkyl group having 1-4 carbon atoms which may be monosubstituted by any group selected from the group consisting of one hydroxyl group, one amino group, one carboxyl group and one alkoxycarbonyl group having 1-4 carbon atoms, a formyl group, an alkanoyl group having 1-4 carbon atoms which may be monosubstituted by an amino group, or a benzoyl group which may be monosubstituted by an amino group;
- R.sup.6 and R.sup.7 may form a pyrrolidine, piperidine, morpholine, or piperazine ring together with the nitrogen atom to which they are bound, provided that the nitrogen atom at the 4-position of the piperazine ring where a hydrogen atom is substituted may be substituted by any group selected from the group consisting of an oxalo group, and alkoxyoxalyl group having 1-4 carbon atoms, an alkanoyl group having 1-4 carbon atoms which may be substituted by one hydroxyl group and an alkyl group having 1-4 carbon atoms);
- R.sup.5 represents a hydrogen atom, a halogen atom, an alkyl group having 1-4 carbon atoms, an optionally protected hydroxyl group, a cyano group, a nitro group or an alkoxyl group having 1-4 carbon atoms which may be monosubstituted by a group selected from the group consisting of one carboxyl group, one alkoxycarbonyl group having 1-4 carbon atoms and one hydroxyl group;
- when R.sup.4 is a hydrogen atom, R.sup.6 and R.sup.7 is not a formyl group, an alkanoyl group having 1-4 carbon atoms which may be monosubstituted by an amino group, or a benzoyl group which may be monosubstituted by an amino group;
- and a pharmaceutically acceptable carrier thereof.
6 more elements
Dependencies are inferred from the claim text.