Abstract: Novel 2'-deoxy-5-substituted uridine derivative represented by the general formula, ##STR1## wherein R.sub.1 is a hydrogen atom, a benzoyl group or a tetrahydrofuranyl group; R.sub.2 is a fluorine atom or a trifluoromethyl group; and any one of R.sub.3 and R.sub.4 is a hydrogen atom and the other one is an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 2 to 6 carbon atoms, a benzyl group having as the substituents selected from the group consisting of a halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms and a nitro group, or an alkyl group having 1 to 3 carbon atoms having one or two phenyl groups as the substituents.The novel 2'-deoxy-5-substituteduridine derivative possesses excellent antitumor activity with less toxicity, thus it is useful as antitumor agent.

Abstract: This invention relates to a novel chemically synthesized gene including a base sequence coding for the primary amino acid sequence of natutal-type streptokinase, a corresponding plasmid recombinant, corresponding transformant and process for preparing streptokinase by the incubation of the transformant, the invention further relating to novel streptokinase derivative proteins having streptokinase activity and a modified primary amino acid sequence corresponding to the primary amino acid sequence of natural-type streptokinase which is deficient in the amino acid residues at the 373-position to the C-terminus, and wherein at least one of the amino acid residues may be deficient, replaced or inserted; the chemically synthesized gene including a base sequence coding for the derivative protein, plasmid containing the gene, transformant transformed by the plasmid, and process for preparing the streptokinase derivative protein by the incubation of the transformant.

Abstract: Novel polypeptide derivatives, acid-addition salts thereof and complexes thereof, having the activities for inhibiting bone calcium absorption, for lowering the blood level of calcium, as analgesics, for inhibiting secretion of the gastric juice.Pharmaceutical composition can be prepared by formulating, at least one of the novel polypeptide derivatives, acid-addition salts thereof and complexes thereof, together with a proteolytic enzyme inhibitors and/or pharmaceutically acceptable acids.The pharmaceutical composition are quite effective as agents for curing hypercalcemia, for curing Peget's disease, for curing osteoporosis, analgetic agent, anti-ulcerative agent and the like.

Abstract: There is described pyrroloquinoline derivatives of general formula: ##STR1## wherein R' is a C.sub.1 -C.sub.6 alkyl group, R.sup.2 is a group: ##STR2## or group: ##STR3## wherein R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as defined, or salt thereof. These compounds have an antimicrobial activity.

Abstract: Novel synthetic polypeptide derivatives, i.e., novel calcitonin derivatives, having improved basic physiological activities of the corresponding natural calcitonins, i.e., the activity for lowering the blood level of calcium, the activity as an analgesic, as well as the activity for inhibiting the secretion of the gastric juice. Thus these synthetic calcitonins are effective as agents for curing hypercalcemia, analgetic agents, anti-ulcerative agents and the like.

Abstract: A composition for increasing the anti-cancer activity of an anti-cancer compound selected from among 5-fluorouracil and a compound capable of producing 5-fluorouracil in vivo, the composition comprising an effective amount of a pyridine derivative represented by the formula ##STR1## wherein R.sup.1 is hydroxy or acyloxy, R.sup.2 and R.sup.4 are each hydrogen, halogen, amino, carboxyl, carbamoyl, cyano, nitro, lower alkyl, lower alkenyl or lower alkoxycarbonyl, R.sup.3 and R.sup.5 are each hydrogen, hydroxy or acyloxy; when at least one or R.sup.1, R.sup.3 and R.sup.

Abstract: Phenylcarboxylic acid derivatives having a hetero ring in the substituent of the formula: ##STR1## wherein R.sup.1 is halogen, alkyl, cycloalkyl, hydroxy, alkoxy, phenoxy which has a substituent selected from halogen and alkyl, carboxyl, alkylsulfonyloxy, phenylsulfonyloxy optionally substituted by halogen, alkylsulfonyloxyalkoxy, amino, alkanoylamino, benzoylamino, alkenyloxy, phenylalkoxyalkoxy, hydroxyalkoxy, phenylalkoxy having optionally 1 to 3 substituents selected from halogen, alkyl and alkoxy, halogenoalkyl, cycloalkyloxy optionally substituted by hydroxy, alkoxy substituted by cycloalkyl having optionally hydroxy substituent, imidazolylalkyl or imidazolylalkoxy; k is 0 or 1 to 3; or (R.sup.1).sub.k is alkylenedioxy; A is alkylene or alkylenoxy; l is 0 or 1; B is methylene or carbonyl; m is 0 or 1; D is alkylene; E is alkylene or alkenylene; n is 0 or 1; and R.sup.

Abstract: The present invention provides a non-injection type anti-cancer composiiton comprising a 5-fluorouracil type compound and an oxonic acid or a pharmacologically acceptable salt thereof as effective components, the composition being capable of inhibiting inflammation development due to the 5-fluorouracil type compound, and a method of treating a cancer while inhibiting inflammation development due to the 5-fluorouracil type compound.

Abstract: This invention relates to a novel 5-fluorouracil derivative represented by the formula ##STR1## wherein R.sup.y is a hydrogen atom or a specific acyl group, Z is a phenyl-lower alkoxy-lower alkyl group, thienyl-lower alkyl group optionally substituted with halogen atom on the thienyl ring, or a group ##STR2## wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a specific acyl group, phenyl-lower alkyl group having a group R.sup.x OCO-- on the phenyl ring, or a group --(A).sub.n B, R.sup.x being a specific organic group, A being a lower alkylene group, n being 0 or 1, and B being a 5- or 6-membered unsaturated heterocyclic group having 1 to 4 hetero-atoms selected from N, O and S and optionally having a benzene ring, naphthalene ring or pyridine ring condensed therewith, with the proviso that R.sup.1 and R.sup.2 are not hydrogen atoms or specific acyl groups at the same time; to a process for preparing the same; and to an anticancer composition comprising the same as an effective ingredient.

Abstract: A 2-oxa-isocephem compound of the formula (1): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined, pharmaceutically acceptable salts thereof, composition containing the same and processes for preparing the same are disclosed. The compound is useful as an antimicrobial agent.

Abstract: Phenylcarboxylic acid derivatives having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each H, halogen, alkyl, haloalkyl, alkanoyl, cycloalkyl, nitro, amino, --O--D--R.sup.5 (D is alkylene, R.sup.5 is H, amino, morpholino, carboxyl, phthalimido, phenyl, epoxy), substituted or unsubstituted phenoxy, substituted or unsubstituted phenylalkylamino, carboxylalkenyl, or both form alkylenedioxy; R.sup.3 is H, --E--R.sup.6 (E is alkylene, R.sup.6 is H, carboxyl, cyano, OH, phenylalkoxy, or halogen-substituted phenyl, or phenylcarbamoyl), --CO--G--R.sup.7 (G is alkylene, R.sup.7 is H, substituted or unsubstituted phenylcarbamoyl), substituted or unsubstituted benzoyl, alkenyl, carbamoyl, phenyl, or halophenyl; R.sup.4 is H or alkyl; A is alkylene, alkylene condensed with cycloalkyl ring, or alkenylene; B is alkylene or alkenylene; l is 0 or 1.

Abstract: Derivatives of 5-deoxy-fluorouridine are disclosed of formula (1) ##STR1## in which one of R and R is a substituted furanylmethyl or thienylmethyl group; and the other R and R is a lower alkanoyl group with one free amino substituent or a salt thereof.

Abstract: An anticancer compound is disclosed which is represented by the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is a phenyl-lower alkyl optionally having a substituent, phenyl-lower alkenyl or naphthyl-lower alkyl, the other of R.sup.1 and R.sup.2 is hydrogen or acyl, and R.sup.3 is hydrogen, acyl or tetrahydrofuranyl, or represented by the formula ##STR2## wherein R.sup.x is an optionally substituted pyridyl, Y is arylene and .alpha. is a known 5-fluorouracil derivative residue which can be converted to 5-fluorouracil in vivo and which is linked to the carbonyl by an ester or amide linkage.

Abstract: There is described a 2-oxa-isocephem compound of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.4 are as defined, and R.sup.3 is a group of the formula: ##STR2## wherein n, m, R.sup.6, R.sup.7, B.sup.- and l are as defined, or pharmaceutically acceptable salt thereof. The compound has antimicrobial activity.

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

Abstract: A 2-oxa-isocephem compound of the formula (1): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined, pharmaceutically acceptable salts thereof, composition containing the same and processes for preparing the same are disclosed. The compound is useful as an antimicrobial agent.

Abstract: A benzopylpiperazine ester of the following formula: ##STR1## wherein A represents a single bond or an alkylene group, vinylene group, --O--alkylene group or methine group, R.sub.1 represents a bicyclic carbon ring residue which may be substituted with a lower alkyl group, lower alkoxy group, oxo group or nitro group or a halogen atom, or may be partially saturated; a fluorene residue which may contain an oxo group; a fluorenylidene group; an anthracene residue; a phenanthrene residue which may be substituted with a lower alkyl group, or may be partially saturated; a benzofuran residue or thianaphthene residue which may be substituted with a lower alkyl group or lower alkoxy group; a benzopyran residue or benzoazine residue which may be substituted with an oxo group or phenyl group and partially saturated; a phthalimide residue; a benzodiazine residue; an isozazole residue which may be substituted with a lower alkyl group or phenyl group; or an alkylene dioxybenzene residue or xanthene residue; and R.sub.

Abstract: Novel 2'-deoxy-5-substituted uridine derivative represented by the general formula, ##STR1## wherein R.sub.1 is a hydrogen atom, a benzoyl group or a tetrahydrofuranyl group; R.sub.2 is a fluorine atom or a trifluoromethyl group; and any one of R.sub.3 and R.sub.4 is a hydrogen atom and the other one is an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 2 to 6 carbon atoms, a benzyl group having as the substituents selected from the group consisting of a halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms and a nitro group, or an alkyl group having 1 to 3 carbon atoms having one or two phenyl groups as the substituents.The novel 2'-deoxy-5-substituteduridine derivative possesses excellent antitumor activity with less toxicity, thus it is useful as antitumor agent.

Abstract: An anticancer compound is disclosed which is represented by the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is a phenyl-lower alkyl optionally having a substituent, phenyl-lower alkenyl or naphthyl-lower alkyl, the other of R.sup.1 and R.sup.2 is hydrogen or acyl, and R.sup.3 is hydrogen, acyl or tetrahydrofuranyl, or represented by the formula ##STR2## wherein R.sup.x is an optionally substituted pyridyl, Y is arylene and .alpha. is a known 5-fluorouracil derivative residue which can be converted to 5-fluorouracil in vivo and which is linked to the carbonyl by an ester or amide linkage.

Abstract: A 2-oxa-isocephem compound of the formula (1): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined, pharmaceutically acceptable salts thereof, esters of the carboxy group in the 4-position thereof and quaternary ammonium salts thereof, composition containing the same and processes for preparing the same are disclosed. The compound is useful as an antimicrobial compound.