Abstract: An anti-cancer composition comprising a 5-fluorouracil and uracil.

Abstract: A phenylalanylvalylarginine derivative represented by the formula, ##STR1## wherein R.sub.1 represents hydrogen or benzoyl and R.sub.2 represents naphthyl. The above compound is useful as an excellent substrate for various enzymes, such as trypsin, plasmin, kallikrein, urokinase, Cl-esterase and the like. Accordingly, the activity of enzymes can be measured by use of said compound as a substrate.

Abstract: A prolylphenylalanylarginine derivative represented by the formula, ##STR1## wherein R.sub.1 represents hydrogen or benzoyl; R.sub.2 represents naphthyl or 6-bromo-2-naphthyl. The above compound is useful as an excellent substrate for various enzymes, such as trypsin, plasmin, kallikrein, urokinase, Clesterase and the like. Accordingly, the activity of enzymes can be measured by use of said compound as a substrate.

Abstract: Guanidinobenzoic acid derivatives represented by the general formula [I] ##STR1## wherein R.sup.1, R.sup.2 and Z are as defined hereinafter, having antiplasmin and anti-trypsin activities and process for their preparation as well as a pharmaceutical composition and a method of inhibiting the activity of plasmin and trypsin is disclosed.

Abstract: A valylleucyllysine derivative represented by the formula, ##STR1## wherein R.sub.1 represents hydrogen or benzoyl and R.sub.2 represented naphthyl. The above compound is useful as an excellent substrate for various anzymes, such as, trypsin, plasmin, kallikrein, urokinase, Cl-esterase and the like. Accordingly, the activity of enzymes can be measured by use of said compound as a substrate.

Abstract: A process for purification of crude kallikrein utilizing a specific affinity of kallikrein to p-aminobenzamidine, which comprises bringing a solution, containing kallikrein and contaminated by other undesirable enzymes and proteins, into contact with a water-insoluble carrier combined with p-aminobenzamidine, exclusively eluting out the other enzymes and proteins from the carrier by the use of a buffer solution of lower NaCl concentration and then exclusively eluting out kallikrein by the use of a buffer solution of higher NaCl concentration.

Abstract: An oral antilipemic agent comprising a pharmaceutically effective amount of at least one of acidic polyamino acids having a molecular weight of 10,000 to 100,000 and pharmaceutically acceptable salts thereof, and an adjuvant.

Abstract: Guanidinobenzoic acid compounds represented by the formula ##STR1## wherein R and Z are as defined hereinafter, having anti-plasmin and anti-trypsin activities and processes for preparing the same as well as a pharmaceutical composition and a method of inhibiting the activity of plasmin and a trypsin is disclosed.

Abstract: Amino- or guanidino-1,2,3,4-tetrahydro-1-naphthoic esters represented by the formula, ##STR1## wherein R.sub.1 is --NH.sub.2 or ##STR2## R.sub.3 is --H, --R.sub.4, --O--R.sub.4, --NHCOCH.sub.3, a halogen, --CN, ##STR3## --COOH, --COOR.sub.4, ##STR4## or --(CH.sub.2).sub.n --COOCH.sub.2 --CO--R.sub.5 ; R.sub.5 is --O--R.sub.4, --NH.sub.2 or ##STR5## n is 0, 1 or 2, and R.sub.4 is a lower alkyl, or pharmaceutically acceptable acid addition salts thereof. Owing to their inhibitory activity on proteolytic enzymes the said esters and acid addition salts thereof are useful in the therapy of diseases caused by such enzymes.

Abstract: Amino- or guanidino-phenylpropionic ester derivatives represented by the formula: ##STR1## wherein R is --NH.sub.2 or ##STR2## R.sup.1 is hydrogen or a lower alkyl group, and R.sup.2 is an unsubstituted or a lower-alkyl-, carboxyalkyl-, lower-alkoxy-, lower-alkoxycarbonyl- or halogen-substituted phenyl group or an unsubstituted or a halogen-substituted naphthyl group, and acid addition salts thereof are novel compounds exhibiting a specific enzyme-inhibitory activity to proteolytic enzymes and, therefore, they are useful as the therapeutic agent of diseases induced by abnormal activation of these enzymes. The above-mentioned compounds can be produced by subjecting a nitrocinnamic acid derivative represented by the formula: ##STR3## and a phenol derivative or a naphthol derivative represented by the formula:HO--R.sup.

Abstract: 5-Fluorouracil derivatives and a process for their preparation are provided. The 5-fluorouracil derivatives according to the invention have the general formula: ##STR1## R.sub.1 and R.sub.2 are the same or different and are hydrogen or ##STR2## with the proviso that both R.sub.1 and R.sub.2 are not hydrogen at the same time. A.sub.1, A.sub.2 and A.sub.3 are independently selected from hydrogen, and optionally substituted alkoxy and phenyloxy; at least one of A.sub.1, A.sub.2 and A.sub.3 being other than hydrogen. The 5-fluorouracil derivative is prepared by condensing 5-fluorouracil with a halide of the formula: ##STR3## in the presence of a base. The 5-fluorouracils according to the invention show anti-tumor activity.

Abstract: A 5-fluoropyrimidin-4-one derivative represented by the formula ##STR1## wherein R is straight-chain or branched-chain alkyl having 4 to 18 carbon atoms, straight-chain or branched-chain alkenyl having 2 to 18 carbon atoms, alkylene oxido having 3 to 10 carbon atoms, aryl or aralkyl;Processes for preparing the derivative;An anti-tumor composition containing the derivative as an effective component and an excipient.

Abstract: A 5-fluoropyrimidin-4-one derivative represented by the formula ##STR1## wherein R is straight-chain or branched-chain alkyl having 4 to 18 carbon atoms, straight-chain or branched-chain alkenyl having 2 to 18 carbon atoms, alkylene oxido having 3 to 10 carbon atoms, aryl or aralkyl;Processes for preparing the derivative;An anti-tumor composition containing the derivative as an effective component and an excipient.

Abstract: A method for isolating and purifying a physiologically active substance contained in a tissue or a body fluid using an insoluble type naturally occurring proteolytic enzyme inhibitor or an insoluble type proteolytic enzyme alone or in combination with the insoluble type naturally occurring proteolytic enzyme inhibitor is disclosed.

Abstract: Guanidinobenzoic acid derivatives represented by formula (I) ##STR1## wherein R.sup.1, R.sup.2 and Z are as defined hereinafter, having anti-plasmin and anti-trypsin activities, intermediates useful for the synthesis thereof and processes for preparing the same.

Abstract: An anti-inflammatory composition comprises an anti-inflammatorily effective amount of a reaction product of a blood with a protease.