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| OF THE INVENTION As used herein, the term "alkyl" denotes a straight or branched chain alkyl ... |
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| OF THE INVENTION One aspect of the present invention provides the compound pradimicin Q and its ... |
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| Inhibitor of absorption of digestion product of food and drink |
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| Hydantoin derivatives for treating complications of diabetes |
| OF PREFERRED EMBODIMENTS The invention will now be further explained with reference to M... |
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| OF THE INVENTION Although the present invention is described below with reference to examples, the ... |
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| Formulation for administration of steroid compounds |
| OF THE INVENTION By 5.beta. steroid is meant .alpha. ET, .beta. ET, and ED. In addition certain ... |
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Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredient
| Details |
Inventors: Tanouchi, Tadao; Kawamura, Masanori; Ajima, Akio; Mohri, Tetsuya; Hayashi, Masaki; Terashima, Hiroshi; Hirata, Fumio; Morimura, Takeshi;
Assignee: Ono Pharmaceutical Co., Ltd. (Osaka, JP)
Primary Examiner: Gerstl; Robert
Assistant Examiner:
Attorney, Agent or Firm: Sughrue, Mion, Zinn, Macpeak and Seas
The rhodanine derivatives of the general formula: ##STR1## wherein (I) R.sup.1 and R.sup.2 are taken together to represent a tetramethylene or pentamethylene group; (II) R.sup.1 represents a hydrogen atom, and R.sup.2 represents (1) a cycloalkyl or cycloalkenyl group of 4-7 carbon atoms which is unsubstituted or substituted by at least one alkyl group of 1-4 carbon atoms, (2) an anthryl or naphthyl group, (3) a phenyl group which is unsubstituted or substituted, (4) a heterocyclic group containing at least one of nitrogen, oxygen and sulfur atoms which is unsubstituted or substituted (5) a ##STR2## group (wherein R.sup.4 represents a hydrogen atom, a halogen atom, phenyl group or an alkyl group of 1-5 carbon atoms; and R.sup.5 represents a hydrogen atom, a phenyl group or an alkyl group of 1-5 carbon atoms) or ##STR3## group; or (III) R.sup.1 and R.sup.2, which may be the same or different with each other, each represents a phenyl group which is unsubstituted or substituted; and R.sup.3 represents a hydrogen atom, an alkyl group of 1-12 carbon atoms, an aralkyl group of 7-13 carbon atoms, a cycloalkyl or cycloalkenyl group of 4-7 carbon atoms which is unsubstituted or substituted by at least one alkyl group of 1-4 carbon atoms, or a phenyl group which is unsubstituted or substituted, possess a strong inhibitory activity on aldose reductase. |
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DETAILED DESCRIPTION We claim: 1.
An aldose reductase inhibitor containing, as an active ingredient, 3-carboxymethyl-5-(2-methylcinnamylidene)rhodanine or non-toxic salts of an acid thereof.
2.
A rhodanine derivative which is 3-carboxymethyl-5-(2-methylcinnamylidene)rhodanine and non-toxic salts of an acid thereof.
3.
A compound as described in claim 2, which is (E,E)-3-carboxymethyl-5-(2-methylcinnamylidene)rhodanine N-methyl-D-glucamine salt.
4.
An aldose reductase inhibitor as described in claim 1, wherein the active ingredient is (E,E)-3-carboxymethyl-5-(2-methylcinnamylidene)rhodanine N-methyl-D-glucamine salt.
5.
A method of inhibiting production of aldose reductase in mammals which comprises administering a therapeutically effective amount of at least one rhodanine derivative represented by the general formula: ##STR13## wherein R.
sup.
2 represents a ##STR14## group, wherein R.
sup.
4 represents a hydrogen atom, a halogen atom, a phenyl group or an alkyl group of 1 to 5 carbon atoms; and R.
sup.
5 represents a hydrogen atom, a phenyl group or an alkyl group of 1 to 5 carbon atoms, and R.
sup.
3 represents a hydrogen atom, an alkyl group of 1 to 12 carbon atoms, an aralkyl group of 7 to 13 carbon atoms, a cycloalkyl or cycloalkenyl group of 4 to 7 carbon atoms which is unsubstituted or substituted by at least one alkyl group of 1 to 4 carbon atoms, or a phenyl group which is unsubstituted or substituted by at least one of the substituents, (a) a halogen atoms, (b) a trifluoromethyl group, (c) a hydroxyl group, (d) a nitro group, (e) a carboxyl group, (f) an amino group which may be substituted by alkyl group(s) of 1 to 4 carbon atoms, (g) an alkyl, alkoxy or alkylthio group of 1 to 5 carbon atoms, (h) a phenyl group, (i) a 5- to 10-membered mono- or bicyclic heterocyclic group containing one or two nitrogen, oxygen or sulfur atom(s) which is unsubstituted or substituted by at least one of the above-described substituents (c) to (h), or (j) an alkyl group of 1 to 4 carbon atoms which is substituted by at least one of the above-described substituents (c), (h) and (i) or, when R
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