Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-12-19
1997-10-28
Richter, Johann
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514398, 5483175, 5483185, 548165, A10K 31415, A01N 4350, C07D23302, C07D23390
Patent
active
056818432
ABSTRACT:
Parabanic acid derivatives, pharmaceutically acceptable salts thereof, and therapeutic agents containing said compounds as an effective component are useful pharmaceuticals for the treatment of diabetic complications such as diabetic neuropathy, diabetic cataracts and retinopathy, diabetic nephropathy, diabetic dermopathy, and other diabetic microangiopathy. The compounds of the present invention are represented by the following general formula (I): ##STR1## wherein R is hydrogen, lower alkyl or benzyl; X is substituted phenyl, optionally substituted benzothiazolyl, optionally substituted naphthyl, optionally substituted pyridyl, anthraquinonyl, phthalimide, or thienyl; and n is an integer from 1 to 3. The compounds of the present invention exhibit excellent inhibitory action towards aldose reductase with a high enzyme selectivity. Accordingly, they are useful as drugs for the therapy and prevention of various types of diabetic complications without substantially inhibitory aldehyde reductase.
REFERENCES:
patent: 4096130 (1978-06-01), Kraft et al.
patent: 4647574 (1987-03-01), Ienaga et al.
patent: 4683240 (1987-07-01), Ienaga et al.
patent: 4985453 (1991-01-01), Ishii et al.
"Pathologic Biochemistry and Clinics of Free Radicals, Inflammation and Antiinflammation," Nippon Rinsho, vol. 46, No. 10, pp. 93-97 (1988).
Yonnezawa, et al., Nippon Kagaku Zasshi, 89, No. 8, pp. 62-64 (1968.
Patton, J. Org. Chem., 32, No. 2, pp. 383-388 (1967).
K. Ogawa, et al., "Synthesis of substituted 2, 4-dioxo-thienopyrimidin-1-acetic acids and their evaluation as aldose reductase inhibitors", European Journal of Medicinal Chemistrychimica Therapeutica, vol. 28, No. 10, 1993, pp. 769-781.
Morrison and Boyd, Organic Chemistry, Allyn and Bacon, Inc., Boston (1965), pp. 806, 808, 847-848.
Kotani Takayuki
Nagaki Yasuhiro
Okamoto Kaoru
Nippon Zoki Pharmaceutical Co. Ltd.
Oswecki Jane C.
Richter Johann
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