Abstract: The present invention provides a protein cross-linking inhibitor containing a compound represented by any of the following formulas (1)-(13), or a pharmaceutically acceptable salt thereof: R3—[—X—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(1) R3—[—X—B(ZR1)—Y—]n—R4,??(2) R3—[—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(3) R3—[—X—B(ZR1)—]n—R4,??(4) R3—[—B(ZR2)—W—]n—R4,??(5) R3—X—B(ZR1)-T[B(ZR2)—W—R4]2,??(6) R3—B(OH)2,??(7) R3—B(ZR1)—X—B(ZR2)—R4,??(8) R3—B(R1)—O—B(R2)—R4,??(9) R3—[—X—B(ZR1)—Y—B(ZR2)—]n—R4,??(10) R3—[—X—B(ZR1)—Y—B(ZR2)—W-Q-]n—R4,??(11) R3—[—P—X—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(12) [R3—X—B(ZR1)—Y]2B(ZR2),??(13) wherein each symbol is as defined in the DESCRIPTION.

Abstract: A bisboron compound represented by the general formula (I): wherein B represents a boron atom, Y represents an oxygen or sulfur atom, R1 and R2 independently represent a monocyclic aromatic group, a polycyclic aromatic group, or a heterocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur atoms, R3 represents a hydrogen atom; —(CH2)m—NR4R5; —CO—(CH2)m—NR4R5; —COCH(NH2)R6; —CHR7R8; —CH2CH(NH2)—R9; quinolyl substituted with C1-C4 alkyl group; or C1-C4 alkyl substituted with pyridyl, piperidino or pyrrolidinyl group, and X represents a monocyclic aromatic group, a polycyclic aromatic group or a heterocyclic group, which may be the same as or different from R1 and R2, or a bifunctional group having a monocyclic aromatic group, polycyclic aromatic group or heterocyclic group bonded to each side of a group selected from the group consisting of a single bond, O, CH2, S, SO2, CH2OCH2, OCH2, OCH2CH2OCH2, OCH2OCH2CH2 and CH2OCH2CH2, or a salt thereof, and a composition for contr

Abstract: The present invention provides a protein cross-linking inhibitor containing a compound represented by any of the following formulas (1)-(13), or a pharmaceutically acceptable salt thereof: R3—[—X—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(1) R3—[—X—B(ZR1)—Y—]n—R4,??(2) R3—[—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(3) R3—[—X—B(ZR1)—]n—R4,??(4) R3—[—B(ZR2)—W—]n—R4,??(5) R3—X—B(ZR1)-T[B(ZR2)—W—R4]2,??(6) R3—B(OH)2,??(7) R3—B(ZR1)—X—B(ZR2)—R4,??(8) R3—B(R1)—O—B(R2)—R4,??(9) R3—[—X—B(ZR1)—Y—B(ZR2)—]n—R4,??(10) R3—[—X—B(ZR1)—Y—B(ZR2)—W-Q-]n—R4,??(11) R3—[—P—X—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(12) [R3—X—B(ZR1)—Y]2B(ZR2),??(13) wherein each symbol is as defined in the DESCRIPTION.

Abstract: A bisboron compound represented by the general formula (I): wherein B represents a boron atom, Y represents an oxygen or sulfur atom, R1 and R2 independently represent a monocyclic aromatic group, a polycyclic aromatic group, or a heterocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur atoms, R3 represents a hydrogen atom; —(CH2)m—NR4R5; —CO—(CH2)m—NR4R5; —COCH(NH2)R6; —CHR7R8; —CH2CH(NH2)—R9; quinolyl substituted with C1-C4 alkyl group; or C1-C4 alkyl substituted with pyridyl, piperidino or pyrrolidinyl group, and X represents a monocyclic aromatic group, a polycyclic aromatic group or a heterocyclic group, which may be the same as or different from R1 and R2, or a bifunctional group having a monocyclic aromatic group, polycyclic aromatic group or heterocyclic group bonded to each side of a group selected from the group consisting of a single bond, O, CH2, S, SO2, CH2OCH2, OCH2, OCH2CH2OCH2, OCH2OCH2CH2 and CH2OCH2CH2, or a salt thereof, and a composition for contr

Abstract: Disclosed herein are phosphoric acid esters of myoinositol, which are represented by the following general formula (I): ##STR1## and their salts, as well as a preparation process thereof. The myoinositol derivatives can each be obtained by causing a phosphorylating agent to act on a myoinositol derivative substituted with catalytic reduction removable substituent groups at the positions other than those desired to be substituted by phosphoric acid residual groups and then catalytically reducing the thus-phosphorylated myoinositol.

Abstract: A process for preparing myoinositol polyphosphoric acid from myoinositol via a polyacylmyoinositol, a process for preparing a polysilyl-polyacylmyoinositol from a polyacylmyoinositol, and a process for preparing an optically active myoinositol polyphosphoric acid from the above product or a polysilylmyoinositol.

Abstract: There are disclosed a novel inositol-1,4,5-triphosphoric acid derivative, inositol-1,3,4-triphosphoric acid derivative, inositol-1,3,4,5-tetraphosphoric acid derivative, and a bonded substance of the same and a protein. They control the metabolic process of an organism concerned with calcium ions to thereby exert a medicinal virtue.

Abstract: Optically active diols and hydroxycarboxylic acids and their esters are produced by deriving 1L-1,2:5,6-di-O-cyclohexylidene-chiro-inositol from 1L-chiro-inositol as an asymmetric source, followed by introduction of a selected class of sterically hindering and asymmetrically reactive groups into the first-mentioned compound and by subsequent reduction of the resulting compound. Seven specific inositols are also derivable from synthesis of those ultimate compounds.

Abstract: A method of synthesizing D-myoinositol-1-phosphate from 1,2-(R.sup.1)-3-R.sup.2 -myoinositol compounds of the formula ##STR1## wherein R.sup.1 is a bridging type protective group bonded to two oxygen atoms at the 1- and 2-position, and R.sup.2 is a protective group coupled to the oxygen atom at the 3-position. D-Myoinositol-1-phosphate is useful as an intermediate for the production of inositol-1,4,5-triphosphate.

Abstract: Disclosed herein are phosphoric acid esters of myoinositol, which are represented by the following general formula (I): ##STR1## and their salts, as well as a preparation process thereof. The myoinositol derivatives can each be obtained by causing a phosphorylating agent to act on a myoinositol derivative substituted with catalytic reduction removable substituent groups at the positions other than those desired to be substituted by phosphoric acid residual groups and then catalytically reducing the thus-phosphorylated myoinositol.

Abstract: A 1-(N-substituted carbamoyl)-5-fluorouracil derivative represented by the following general formula: ##STR1## R is a 4-alkoxycyclohexyl group-containing radical which is 2,3,4-trimethoxycyclohexcylethyl, 2,3,4-trimethoxycyclohexyl, 2,4-dimethoxycyclohexylmethyl, 3,4-dimethoxycyclohexylethyl, 2,4-dimethoxycyclohexyl, 2,4,5-trimethoxycyclohexyl, 3,4-dimethoxycyclohexylmethyl, 3,4,5-trimethoxycyclohexyl, 4-ethoxycyclohexyl or 4-ethoxycyclohexylmethyl. The compounds are carcinostatic agents. The compounds are used in a therapeutically effective amount in the presence of a carrier.

Abstract: N-(6-chloro-2-pyridyl)-3,4-dihydro-2-methyl-4-oxo-2H-1,2-benzothiazine-3-ca rboxamide 1,1-dioxide that is a novel benzothiazine derivative. The compound is characterized by a low degree of toxicity and a low incidence of gastric disorders and useful as an anti-inflammatory agent.

Abstract: N-(6-fluoro-2-pyridyl)-3,4-dihydro-2-methyl-4-oxo-2H-1,2-benzothiazine-3-ca rboxamide 1,1-dioxide that is a novel benzothiazine derivative. The compound is characterized by a low degree of toxicity and a low incidence of gastric disorders and useful as an anti-inflammatory agent.

Abstract: New uracil derivatives of the general formula: ##STR1## wherein R.sup.1 stands for a hydrogen atom or a grouping of the formula: ##STR2## R.sup.2 for a hydrogen atom, an alkyl group or a phenyl group and R.sup.3 for an alkyl group or a phenyl group, with the proviso that when both R.sup.1 and R.sup.2 stand for a hydrogen atom, R.sup.3 stands for a phenyl group or a straight chain alkyl group with 3.about.11 carbon atoms, that when R.sup.1 stands for a hydrogen atom and R.sup.2 for methyl group, R.sup.3 stands for an alkyl group with at least 2 carbon atoms or a phenyl group, and that when R.sup.1 stands for a hydrogen atom and R.sup.3 for methyl group, R.sup.2 stands for an alkyl group with at least 2 carbon atoms or a phenyl group. These uracil derivatives are prepared by reacting 5-fluorouracil with an .alpha.-haloalkyl carboxylate or with an aldehyde diacylate or by hydrolyzing a 1,3-bis(acyloxymethyl)-5-fluorouracil with an acid or alkali.

Abstract: 1-Carbamoyl-5-fluorouracil derivatives represented by the formula ##STR1## wherein R represents alkyl containing 3-8 carbon atoms are effective oral anti-tumor agents with low toxicity.

Abstract: 1-Carbamoyl-5-fluorouracil derivatives represented by the formula ##STR1## wherein R.sub.1 represents methyl, ethyl, phenyl or cyclohexyl and R.sub.2 represents hydrogen or is the same as R.sub.1 are effective anti-metabolites useful in treating lymphatic leukemia L1210, sarcoma 180A and Ehrlich ascites carcinoma in mice.