Abstract: A method for introducing hydroxyl groups into vitamin D compound at the 1.alpha.- and/or 25-positions in the presence of a cyclodextrin compound by the use of a reaction mixture containing a microorganism being capable of hydroxylating vitamin D compound or a enzyme produced from the microorganism, is disclosed.

Abstract: Mucor circinelloides f. griseo-cyanus IFO 4563 is cultivated in a medium containing 6-O-methylerythromycin A as a substrate to obtain 14-hydroxy-6-O-methyl-erythromycin A. This compound and its salt have anti-bacterial activity.

Abstract: Tripeptide derivatives of the formula ##STR1## wherein R is a formyl group or a dimethoxymethyl group have antitumor and enzyme inhibition effects.

Abstract: A method for introducing hydroxyl groups into vitamin D compounds at 1.alpha.- and/or 25-positions by use of a solution containing the mycelium of Actinomycetales being capable of hydroxylating vitamin D compound or the enzyme produced from the mycelium, is disclosed.

Abstract: Method for the treatment of systemic mycosis of mammals comprises administering (S)-2-amino-5-hydroxy-4-oxopentanoicacid in a therapeutically effective amount to said mammals suffering from mycosis, typically candidosis.

Abstract: This invention is directed to novel peptide derivatives. Said peptide derivatives are useful as a substrate for the activity assay of enzymes of the group EC 3. 4. 22, for example, cathepsin L, cathepsin B and cathepsin H. Said peptide derivatives which contain L-methionine radical are prepared according to the methods conventional in peptide chemistry. As typical examples are mentioned D-leucyl-L-tyrosyl-L-methionine-.beta.-naphthylamide formate, .beta.-alanyl-L-tyrosyl-L-methionine-.beta.-naphthylamide formate and succinyl-L-tyrosyl-L-methionine-p-nitroanilide.

Abstract: Novel erythromycin B derivatives of the formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are each hydrogen or methyl, and the pharmaceutically acceptable acid addition salts thereof are disclosed. They exhibit excellent in vivo antibacterial activity against Gram-positive bacteria.

Abstract: Novel erythromycin A derivatives of the formula ##STR1## wherein R is hydrogen or methyl, and the pharmaceutically acceptable acid addition salts thereof are disclosed. They exhibit excellent antibacterial activity against erythromycin resistant bacteria, Gram-positive bacteria and Mycoplasma species.

Abstract: An epoxysuccinyl amino acid derivative of the formula ##STR1## wherein R.sup.1 is hydrogen, alkali metal, benzyl or cycloalkyl having 5 to 6 carbon atoms, R.sup.2 is alkyl having 3 to 4 carbon atoms, R.sup.3 is hydrogen, benzyloxycarbonyl, acetyl or benzoyl, and n is an integer of 2 to 7. The subject compounds exhibit inhibitory activity towards thiol protease, especially, calcium-activated neutral thiol protease which exists in excess in muscle tissues of mammals afflicted with muscular dystrophy.

Abstract: An epoxysuccinyl amino acid derivative of the formula ##STR1## wherein R.sup.1 is hydrogen or alkali metal, R.sup.2 is isobutyl, R.sup.3 is hydrogen or benzyloxycarbonyl, and n is an integer of 5 to 7. The subject compounds exhibit inhibitory activity towards thiol protease, especially, calcium-activated neutral thiol protease which exists in excess in muscle tissues of mammals afflicted with muscular dystrophy.

Abstract: The epoxysuccinic acid derivatives of this invention are prepared by esterification of an epoxysuccinic acid or a halide thereof, by partial hydrolysis of an epoxysuccinic acid diester, by amidation of an epoxysuccinic acid monoester, or by hydrolysis of an epoxysuccinic acid amide monoester. These epoxysuccinic acid derivatives have excellent thiol protease inhibitory activity and anti-inflammatory activity without the acceleration of vascular permeability.

Abstract: An epoxysuccinic acid derivative of the formula ##STR1## wherein R.sup.1 is hydrogen, alkali metal, alkyl having 1-2 carbon atoms, cycloalkyl having 5-6 carbon atoms or benzyl, R.sup.2 is alkyl having 3-4 carbon atoms or benzyl, R.sup.3 is hydrogen or methyl, and R.sup.4 is alkyl having 1-10 carbon atoms, phenyl, benzyl, phenethyl, cycloalkyl having 3-6 carbon atoms or a group of the formula ##STR2## wherein R.sup.5 is hydrogen, alkyl having 1-4 carbon atoms or said alkyl substituted with hydroxy, methylmercapto, phenyl, hydroxyphenyl, indolyl, an optionally protected carboxy, an optionally protected amino or an optionally protected guanidino, and R.sup.6 is hydroxy, alkalimetaloxy, alkoxy having 1-2 carbon atoms, benzyloxy, amino or dimethylamino, or R.sup.3 and R.sup.4 taken together with the nitrogen atom to which they are attached form a 5-6 membered heterocyclic ring, or said heterocyclic ring substituted with a protected carboxy.

Abstract: A novel compound of the formula ##STR1## and the salts thereof, derived from dianemycin, are useful as antiprotozoal and antibacterial agents.

Abstract: The novel antibiotics represented by the formula ##STR1## wherein either (a) R.sup.1 is hydroxy and R.sup.2 is hydrogen, or (b) R.sup.1 is methoxy and R.sup.2 is hydroxy, and the salt thereof, are produced by the cultivation of the organism Streptomyces hygroscopicus TM-531 under aerobic conditions. They are separated from coproduced Antibiotic TM-531 as disclosed in U.S. Pat. No. 4,269,971 and from each other by chromatography on silica gel.

Abstract: An epoxysuccinic acid derivative of the formula ##STR1## wherein R.sup.1 is hydrogen, alkali metal, alkyl having 1-2 carbon atoms, cycloalkyl having 5-6 carbon atoms or benzyl, R.sup.2 is alkyl having 3-4 carbon atoms or benzyl, R.sup.3 is hydrogen or methyl, and R.sup.4 is alkyl having 1-10 carbon atoms, phenyl, benzyl, phenethyl or cycloalkyl having 3-6 carbon atoms or R.sup.3 and R.sup.4 taken together with the nitrogen atom to which they are attached form a 5-6 membered heterocyclic ring, or said heterocyclic ring substituted with a protected carboxy.

Abstract: Novel erythromycin compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or methyl, and a pharmaceutically acceptable salt thereof are disclosed. They exhibit excellent antibacterial activity against Gram-positive bacteria, acid stability and in vivo activity.

Abstract: Antibiotic TM-531 having the formula: ##STR1## TM-531 is effective against gram-positive bacteria, plant pathogenic microorganisms and protozoa.

Abstract: Novel lonomycin derivatives, prepared by reacting lonomycin or its salt with an alkali or an alkali metal borohydride, show antibacterial, antiviral and antiprotozoal activity, and have decreased toxicity as compared with lonomycin.

Abstract: Novel oligosaccharide substances, TAI-A and TAI-B, possessing a strong inhibitory activity to amylase and invertase are obtained by inoculating a seed of the strain of Streptomyces calvus TM-521 into aqueous nutrient medium, cultivating this with shaking or by a submerged culture method with aeration, and separating the produced amylase inhibitors TAI-A and TAI-B from the cultured broth.

Abstract: A new polyether group antibiotic, TM-481, having the estimated empirical formula C.sub.42-45 H.sub.71-75 O.sub.14-15 Na and possessing an antibacterial activity against pathogenic microorganisms, particularly Gram-positive bacteria is obtained by culturing a TM-481 producing microorganism of the Streptomyces ribosidificus group in a nutrient medium therefor.