Abstract: Pyrazolotriazine compounds of the formula: ##STR1## wherein R.sup.1 is OH or alkanoyloxy; R.sup.2 is H, OH, or SH; R.sup.3 is (1) unsaturated N- or S-containing heterocyclic group optionally having 1-2 substituents of halogen, nitro or phenylthio, (2) naphthyl, (3) phenyl optionally having 1-3 substituents of (i) alkyl, (ii) phenyl, (iii) alkoxycarbonyl, (iv) cyano, (v) nitro, (vi) alkoxy, (vii) phenylalkoxy (viii) phenylthio-alkyl, (ix) phenoxy, (x) ##STR2## R is alkyl, halo-substituted alkyl, phenyl optionally having 1-3 substituents, or pyridyl, and l is 0, 1 or 2, (xi) halogen, (xii) phenylalkyl, (xiii) carboxy, (xiv) alkanoyl, (xv) benzoyl optionally having 1-3 substituents, (xvi) amino, (xvii) OH, (xviii) alkanoyloxy, (xix) ##STR3## or (xx) ##STR4## (A is alkylene), said compounds having a xanthine oxidase inhibitory activity and are useful for the prophylaxis and treatment of gout.

Abstract: A sulfonic acid ester derivative represented by the general formula ##STR1## wherein R.sub.1 is a hydrogen atom, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms, A is a group represented by the general formula ##STR2## (wherein R.sub.2 and R.sub.3 are each alkyl having 1 to 4 carbon atoms) or by the general formula ##STR3## (wherein R.sub.4 and R.sub.5 are each alkyl having 1 to 4 carbon atoms or, when taken together with the carbon atom to which they are attached, form cycloalkyl having 4 to 6 carbon atoms), and l is an integer of from 1 to 3, and a process for preparing the derivative.

Abstract: An automatic analyzer comprising a plurality of sample containers for accommodating different blood samples individually, specific sample container moving means, a plurality of reagent containers for accommodating at least a reagent for an assay of guanase activity, a specific reagent container holding means, a plurality of reaction containers, specific reaction container moving means, specific sample pouring means, specific cleaning vessels, specific stirring means, specific measuring means, specific cleaning means, a specific analog-digital converter, specific counting-calculating means, a specific display means, and specific operation control means, so that the display means produces a signal for excluding the measured blood sample corresponding to a display value when the display value is above a predetermined reference value of guanase activity.

Abstract: This invention relates to a method for determining an enzyme-, an enzyme inhibitor-, an enzyme activator-, or zymogen-activity, which comprises allowing the enzyme to react with a substrate of the formula ##STR1## (wherein R.sub.1 represents an amino acid of an oligopeptide combined in the form of ester through the C-terminal carboxyl group of said amino acid or oligopeptide and R.sub.2 represents a hydrogen or bromine atom) to hydrolyze the substrate, then allowing the hydrolysis product of the formula ##STR2## to react with a FR-ITR salt [Fast Red-ITR salt (N,N'-diethyl-4-methoxymetanilamide diazonium salt)] to form a pigment, and determining the pigment.

Abstract: A pharmaceutical composition is disclosed which comprises a physiologically active substance possessing peptide bonds in its structure and being inactivable by digestive enzymes, the active substances being other than insulin, and a synthetic chymotrypsin inhibitor. The composition is particularly suitable for intestinal absorption of the active substance.

Abstract: Novel benzoyl esters of the following formula (I), and acid addition salts thereof, ##STR1## in which R.sub.1 and R.sub.2 are the same or different and represent a hydrogen atom or a lower alkoxy group, A represents a single bond, a linear or branched lower alkylene group, a lower alkenylene group, R.sub.3 and R.sub.4 are the same or different and represent a hydrogen atom or a lower alkyl group, or R.sub.3 and R.sub.4 join together to form a lower alkylene group, R.sub.5 represents a group of the formula, --X--(CO).sub.

Abstract: An anti-cancer composition for delivering a 5-fluorouracil to cancer tissues in a warm-blooded animal, wherein the cancer is a cancer sensitive to 5-fluorouracil. The composition comprises uracil or a pharmaceutically acceptable salt thereof, and a 5-fluorouracil pro drug selected from the group consisting of 1, 3-bis (2-tetrahydrofuryl)-5-fluorouracil and 3-(2-tetrahydrofuryl)-5-fluorouracil in a small amount of about 0.1 to less than 0.1 mole per mole of uracil or salt thereof.

Abstract: A sulfonic acid ester derivative represented by the general formula ##STR1## wherein R.sub.1 is a hydrogen atom, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms, A is a group represented by the general formula ##STR2## (wherein R.sub.2 and R.sub.3 are each alkyl having 1 to 4 carbon atoms) or by the general formula ##STR3## (wherein R.sub.4 and R.sub.5 are each alkyl having 1 to 4 carbon atoms or, when taken together with the cabon atom to which they are attached, form cycloalkyl having 4 to 6 carbon atoms), and l is an integer of from 1 to 3, and a process for preparing the derivative.

Abstract: An anti-cancer composition for treating cancers sensitive to 5-fluorouracil therapy in warm-blooded animals, comprising 5-fluorouracil and uracil.

Abstract: An anti-cancer composition for delivering 5-fluorouracil to cancer tissues which comprises at least one 5-fluorouracil derivative, and a uracil derivative.

Abstract: A pharmaceutical composition is disclosed which comprises a physiologically active substance possessing peptide bonds in its structure and being inactivable by digestive enzymes, the active substance being other than insulin, and a synthetic chymotrypsin inhibitor. The composition is particularly suitable for intestinal absorption of the active substance.

Abstract: Amidine compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsin, anti-plasmin, anti-kallikrein and anti-thrombin agents. They are also useful as a powerful anti-complement agent.

Abstract: An anti-cancer composition for delivering 5-fluorouracil to cancer tissues in a warm-blooded animal, wherein the cancer is a cancer sensitive to 5-fluorouracil, comprising 1-n-hexylcarbamoyl-5-fluorouracil and uracil (or salt there-of), wherein the composition contains less than 0.1 mole of the 5-fluorouracil per mole of the uracil.

Abstract: Phenyl tetrahydronaphthylcarboxylate of the formula: ##STR1## wherein A is a direct bond, or a lower alkylene, vinylene or imino group; B is a direct bond, a lower alkylene or --NH-lower alkylene group, or an --OCH.sub.2 CO-- residual group; and R is a lower alkyl group, with the proviso that A and B are not direct bonds simultaneously, and A, B and R are not a lower alkylene group, a direct bond and a methyl group, respectively, at the same time, are effectively useful as chymotrypsin inhibitors.

Abstract: Benzoyl indolecarboxylates of the formula: ##STR1## where R.sup.1 is hydrogen, halogen, lower alkyl or lower alkoxy; R.sup.2 is hydrogen, lower alkyl, acetyl or benzoyl; R.sup.3 is hydrogen or lower alkyl; and A is a direct bond, or lower alkylene or vinylene substituted at the 2-, 3- or 5-position of the indole nucleus, are effective agents as chymotrypsin inhibitors.

Abstract: A protein effective in stimulating cell growth activity. The protein has a molecular weight of from 5,000 to about 160,000, is composed predominantly of neutral and acidic amino acids, contains a significant amount of glutamic acid and aspartic acid, and is substantially free of nucleoside phosphotransferase. The protein is useful as wound treatment agent and as promoting agent in the synthesis of DNA. A method of producing the protein and compositions containing the same are also disclosed.

Abstract: A 2'-deoxy-5-fluorouridine derivative represented by the formula; ##STR1## wherein R represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, an acetyloxy group or a halogen atom, and n is an integer of 1 to 3.

Abstract: Amidine derivatives of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, represent each a hydrogen atom or a lower alkyl group, or R.sub.1 and R.sub.2 together with an intermediary carbon atom and/or hetero atom may form a ring; X represents ##STR2## (wherein R.sub.8 represents a hydrogen atom, a lower alkyl group, or --CH.sub.2 COOR.sub.9, where R.sub.9 represents a hydrogen atom or a lower alkyl group; Z represents a single bond, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, or --CH.dbd.CH--); R.sub.3 represents a hydrogen or chlorine atom, methoxy group, nitro group, or amino group; Y represents --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 O--, or --OCH.sub.2 --; R.sub.4 represents a hydrogen atom, methoxy group, benzoyl group, nitro group, or amino group; and R.sub.5, R.sub.6 and R.sub.

Abstract: Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsine, anti-plasmin, anti-kallikrein and anti-thrombin agents. Having strong anti-Cl (Clr, Cls) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula (II)R.sub.1 --COOH (II)with amidinophenol compound (III) and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof.

Abstract: Amidine compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsin, anti-plasmin, anti-kallikrein and anti-thrombin agents. They are also useful as a powerful anti-complement agent.