Pharmacologically active derivatives of p-guanidinobenzoic acid

Details Pharmacologically active derivatives of p-guanidinobenzoic acid Pharmacologically active derivatives of p-guanidinobenzoic acid

1990-06-26

1991-12-31

Dentz, Bernard

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

544165, 548200, C07C22960

Patent

active

050774280

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, --OCONR.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: 4283418 (1981-08-01), Fujii et al.
patent: 4359046 (1982-11-01), Shaw, Jr.
patent: 4423069 (1983-12-01), Kaminski et al.
patent: 4843094 (1989-06-01), Imaki et al.
Chemical Abstracts, vol. 93, No. 5, Aug. 4, 1980, p. 393, No. 40319n Columbus, Ohio, U.S.; N. Masayuki et al: Inverse substrates Part VII "Inverse substrate" for trypsin-like enzymes, J. Pharmacobio-DYN 1980 3(4), 213-19.
Chemical Abstracts, vol. 94, No. 15, Apr. 13, 1981, p. 661, No. 121139, 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, Elseview/North-Holland Biomedical Press; S. Fujii et al., "New Synethetic 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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