摘要:
Adriamycin derivatives represented by formula (I) ##STR1## wherein R denotes a divalent hydrocarbon group,CD denotes a cyclodextrin residue,m is 1 to 8, andn is 0 to 8.The compounds exhibit excellent anti-cancer activity over a wide administration range, have low toxicity and sustained release, and maintain activity for a long period of time; thus, they are quite useful as an anti-cancer agent.
摘要:
4-Hydroxypyridine derivative represented by the following formula ##STR1## wherein R represents a methyl group or an isopropyl group, and the method for preparing the derivative comprising the step of cultivating a strain belonging to Streptomyces karnatakensis are disclosed. Also disclosed are the pharmaceutical composition comprising the same and a method for treating circulatory diseases comprising the step of administering said compound to a patient.
摘要:
Tylosin derivatives represented by the following general formula (I): ##STR1## [wherein R denotes a hydrogen atom, acetyl, propionyl or a radical of Si(R.sup.2).sub.3 (in which R.sup.2 is a lower alkyl group), and R.sup.1 stands for a hydrogen atom or a radical of Si(R.sup.2 .sub.3 ] are useful as intermediates for the synthesis of 4"-acyl derivatives of tylosin because, after introduction of any desired acyl group at the 4"-hydroxyl group, the silyl protective group can be readily removed without liberation of the acyl group. This invention also provides processes for producing the tylosin derivatives. More specifically, it provides a melthod of selectively protecting 2'- and 4"'-hydroxyl groups of tylosin (those of higher reactivity among the hydroxyl groups involved); a method of selectively protecting only the 4"'-hydroxyl group of tylosin; a method of selectively protecting the 3- and 4"'-hydroxyl groups of 2'-O-acyltylosin; and a method of protecting 3-, 2'- and 4"'-hydroxyl groups of tylosin.
摘要:
Compounds of the formula (I) ##STR1## wherein R is a hydrogen atom or a C.sub.1-6 alkyl group and n is an integer of 0 or 1, and pharmaceutical preparations thereof are provided. These pharmaceutical preparations are useful for the prevention or treatment of diseases associated with an abnormality in immunological regulatory function or vascularization.
摘要:
A compound of the following formula is provided: ##STR1## wherein A represents a carbonyl group which may be protected; B represents an aldehyde group which may be protected; R.sup.1 represents a hydroxyl group which may be protected; R.sup.2 represents a hydrogen atom or acyl group; W represents a hydrogen atom, hydroxyl group, lower alkanoyloxy group or substituted sulfonyloxy group; Y represents a hydrogen atom, halogen atom, hydroxyl group or substituted sulfonyloxy group; and broken line "-------" represents a double bond or single bond. This compound is useful for producing 3,4'-dideoxymycaminosyltylonolide useful as an antimicrobial agent.
摘要:
An angolamycin derivative represented by the following formula ##STR1## wherein X represents an acetyl, methanesulfonyl, methylthio, benzoyl or methoxy group. This compound is useful as a medicament such as antibacterial agent and an animal feed additive.
摘要:
A process for producing 2-azetidinone derivatives represented by formula ##STR1## wherein R.sup.1 denotes a protecting group of a hydroxyl group,Z denotes a hydrogen atom or a protecting group of an amino group, andQ denotes ##STR2## in which X denotes a halogen atom, Y denotes a halogen atom or OR.sup.2, R.sup.2 denotes a hydrogen atom or a protecting group of a carboxyl group, and Y.sup.2 denotes OR.sup.3 or SR.sup.4 in which R.sup.3 denotes a hydrogen atom, a protecting group of a carboxyl group or an ester residue and R.sup.4 denotes an ester residue.
摘要:
14-Trifluoromethanesulfonyloxydaunomycin represented by the following formula ##STR1## and its salt. This compound is useful as an intermediate for production of adriamycin.
摘要:
Antibiotic Mer-AF1032A represented by the following formula (I) and its isomer antibiotic Mer-AF1032B are disclosed. Also disclosed are a method for preparing the antibiotics comprising the cultivation of a strain belonging to genus Penicillium and a pharmaceutical composition comprising one of these antibiotics and useful as an antifungal agent. ##STR1##
摘要:
Salicylamide derivatives represented by formulae (1a) and (1b); intermediates in the production thereof; a process for producing the same; and drugs containing the same as the active ingredient. The salicylamide derivatives represented by formulae (1a) and (1b) are useful as anti-inflammatory agents and immunosuppressive agents which exert an effect of inhibiting the activation of NF-&kgr;B with little side effects.