Takeda Chemical Industries, Inc.

Hiroshi Fukase

Satoshi Horii

Yukihiko Kameda

Eiji Higashide

Toru Hasegawa

Kazunori Hatano

Hidesuke Iwasaki

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

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

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

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 aminocyclitols, namely the compounds of the formula ##STR1## wherein X is hydroxyl group, a halogen or an acyloxy group; Y is hydrogen or a halogen; and OR.sup.1 is an optionally protected hydroxyl group; and their production. These aminocyclitols are important intermediates for preparing valiolamine having .alpha.-glucosidase inhibitory activity.

Aminocyclitols and their production

Method for production of peptide, and its intermediate

A novel antibiotic C-2801-X represented by the formula ##STR1## is produced by cultivating a microorganism of the genus Streptomyces. The compound is useful in the treatment of mammals, including human beings, suffering from urinary tract infections, respiratory tract infections, colitis, septicema, purulent diseases, etc.

Growing community of inventors

Osaka, Japan

Hiroshi Fukase