Derivatives of p-guantidinobenzoic acid and pharmaceutical agent

Details Derivatives of p-guantidinobenzoic acid and pharmaceutical agent Derivatives of p-guantidinobenzoic acid and pharmaceutical agent

1986-11-12

1989-06-27

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

514517, 558 58, 560 34, A61K 31255, C07C14368

Patent

active

048430943

ABSTRACT:
Compounds presented by the general formula: ##STR1## [wherein when Y is oxygen, R.sup.2 is H, alkyl, alkoxy, alkoxymethyl, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --CH.dbd.CH--COOR.sup.3, halogen, --CF.sub.3, --COR.sup.4, --OCOR.sup.4, --CH.sub.2 OCOR.sup.4, --SO.sub.2 R.sup.4, --OSO.sub.2 R.sup.4, --CONR.sup.5 R.sup.6, --SO.sub.2 NR.sup.5 R.sup.6, --CONH--SO.sub.2 NR.sup.5 R.sup.6, --NHSO.sub.2 R.sup.7, --NO.sub.2, --OH, --CH.sub.2 OH, guanidino, benzyloxy, guanidinophenylthiomethyl, morpholinosulfonylphenoxymethyl, pyridyloxymethyl, or (1,1-dioxothiazol-3-yl)carbonyl, or when Y is sulfur, R.sup.2 is H, alkyl, alkoxy, halogen, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --NO.sub.2, or --SO.sub.2 NR.sup.5 R.sup.6, and n represents an integer of one to five, and when n represents more than two, each of R.sup.2 may be the same group or the different group.] and acid addition salts thereof have inhibitory effect on elastase, and, therefore, are useful for the treatment and/or prevention of diseases induced by abnormal enhancing of degradation of proteins such as elastin and the like, by the action of elastase in mammals, especially in human beings.

REFERENCES:
patent: 3520918 (1970-07-01), Chase et al.
patent: 4359046 (1982-11-01), Shaw, Jr.
patent: 4423069 (1983-12-01), Kaminski et al.
Chemical Abstracts, vol.93, No. 5, 4th Aug. 1980, p. 393, No. 40319n, Columbus, Ohio, U.S.; N. Masayuki et al.: "Inverse Substrates", Part VII.
"Inverse Substrates", for Trypsin-Like Enzymes & J. Pharmacobio-Dyn. 1980, 3(4), 213-19.
Chemical Abstracts, vol. 94, No. 15, Apr. 13th 1981, p. 661, No. 121139b, Columbus, Ohio, U.S.; & JP-A-80 100 356 (Kowa Co., Ltd) 31-07-1980.
Biochimica et Biophysica Acta, vol. 661, 1981, pp. 342-345, Elsevier/North-Holland Biomedical Press; S. Fuji et al. "New Synthetic Inhibitors of Clr., Cl Esterase, Thrombin, Plasmin, Kallikrein and Trypsin".
Journal of Medicinal Chemistry, vol. 29, No. 4, Apr. 1986, pp. 514-519, American Chemical Society, Washington, D.C., U.S.; J. M. Kaminski et al.: "Synthesis and Inhibition of Human Acrosin and Trypsin and Acute Toxicity of Aryl 4-Guanidinobenzoates".

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