Takeda Chemical Industries, Inc.

Satoshi Horii

Hiroshi Fukase

Yukihiko Kameda

Eiji Higashide

Takashi Iwasa

Hiroichi Yamamoto

Nariakira Mizokami

Yutaka Kuwada

Ikuo Nogami

Toru Hasegawa

Masahiko Yoneda

Disclosed is a novel inosose compound represented by the general formula: ##STR1## wherein X.sup.1 and X.sup.2 are both halogen; X.sup.1 is hydrogen and X.sup.2 is halogen; or X.sup.1 is --SQ.sup.1 and X.sup.2 is --SQ.sup.2 (each of Q.sup.1 and Q.sup.2 is lower alkyl or Q.sup.1 and Q.sup.2 may form lower alkylene), R.sup.1 is a protective group for hydroxyl and Y is .dbd.O, .dbd.N--Z (Z is hydroxyl which may be protected) or ##STR2## (A is hydrogen or an amine residue), particularly to the compound wherein the symbol Y is oxygen. The inosose compound is useful as intermediates for production of valiolamine and the N-substituted derivatives thereof, which have potent .alpha.-glucosidase inhibiting activities and are useful as preventives or therapeutics for symptoms of hyperglycemia and various diseases derived therefrom in human and animals, such as diabetes, obesity and hyperlipemia.

Inosose derivatives, production and use thereof

Novel pseudo-aminosugars, or 5-amino-1-hydroxymethyl-1,2,3,4-cyclohexanetetrol, their production and use. These pseudo-aminosugars exhibit excellent .alpha.-glucosidase inhibitory activity and are useful for hyperglycemic symptoms and various disorders caused by hyperglycemia.

Pseudo-aminosugars, their production and use

A novel valiolamine derivative of the formula (I): ##STR1## where R stands for hydrogen or .beta.-D-glucopyranosyl group is useful for a starting material of valiolamine which can be converted to more potent .alpha.-glucosidase inhibiting compounds. The valiolamine derivative is obtained by cultivating Streptomyces hygroscopics in a culture medium and recovering the valiolamine derivative produced and accumulated from the culture broth.

Valiolamine derivatives and production thereof

The novel inosose derivatives ##STR1## wherein Y.sup.1 stands for hydroxyl group and Y.sup.2 stands for hydrogen atom, or Y.sup.1 and Y.sup.2 are joined to form a bond between carbon and carbon atoms, and R.sup.1 and is a protective group for hydroxyl group, are useful as a starting material for producing valienamine, valiolamine and their N-substituted derivatives.

Inosose derivatives and production thereof

A compound of the formula: ##STR1## wherein A is a chain hydrocarbon group having 1 to 10 carbon atoms optionally substituted by hydroxyl, phenoxy, thienyl, furyl, pyridyl, cyclohexyl or an optionally substituted phenyl group, or a cyclic hydrocarbon group having 3 to 7 carbon atoms optionally substituted by hydroxyl, B is hydrogen or hydroxyl, and their production and use. These compounds exhibit excellent inhibitory activity against .alpha.-glucoside hydrolase, thus are useful for hyperglycemic symptoms and various disorders caused by hyperglycemia.

N-substituted pseudo-aminosugars, their production and use

Novel peptide B-52653 having the formula: ##STR1## which is produced by cultivating a microorganism belonging to the genus Streptomyces and being capable of producing B-52653 in a culture medium, whereby B-52653 is elaborated and accumulated in the cultured broth and is recovered. B-52653 is useful as a germicide or disinfectant, and a possibility of the present substance as an antifibrotic agent is suggested.

Antimicrobial peptide

A compound of the general formula: ##STR1## wherein A is hydrogen or a hydroxyl group; B is (1) a group of the formula; ##STR2## (2) a group of the formula; ##STR3## or (3) a group of the formula; ##STR4## or a pharmaceutically acceptable salt thereof is novel and possesses excellent inhibitory activity against .alpha.-glucoside hydrolase and are useful for hyperglycemic symptoms and various disorders caused by hyperglycemia.

N-substituted pseudo-aminosugars and pharmaceutical compositions

Streptomyces albulus subsp. ochragerus subsp. nov. culture for making

A compound of the formula: ##STR1## wherein A is a chain hydrocarbon group having 1 to 10 carbon atoms optionally substituted by hydroxyl, phenoxy, thienyl, furyl, pyridyl, cyclohexyl or an optionally substituted phenyl group; or a cyclic hydrocarbon group having 3 to 7 carbon atoms optionally substituted by hydroxyl, and their production and use. These compounds exhibit excellent inhibitory activity against glucoside hydrolase, thus are useful for hyperglycemic symptoms and various disorders caused by hyperglycemia.

Valienamine derivatives, their production and use

The peptide compound represented by the formula: ##STR1## which is useful as a germicide or disinfectant, is produced by reducing a compound of the formula: ##STR2## wherein Y is amino group which may optionally be protected; R.sup.1 is hydrogen or protective group; and R.sup.2 is hydrogen or protective group; and subjecting the reduction product compound to deprotection reaction when required. A compound of the formula: ##STR3## wherein Z is amino group which may optionally be protected; R.sup.1 is hydrogen or protective group; and R.sup.2 is hydrogen or protective group, is a useful as intermediate for production of the first-mentioned compound.

Alanyl-2-(5-hydroxy-2-oxo-pyrrolidin-3-yl)glycine

Novel 2-methylcephalosporin derivatives and production thereof. These cephalosporin derivatives exhibit excellent antibacterial activities against gram-positive and gram-negative bacteria, thus being of value as a prophylactic or therapeutic agent for infections observed in man and animals.

Growing community of inventors

Sakai, Japan

Satoshi Horii