Abstract: Compounds represented by formula (I) and the formula (IV) have an inhibitory activity of MMP-9 production, therefore, are useful as a medicine agent with fewer side effects than conventional MMP enzyme activity inhibitors, as a prophylactic and therapeutic drug for oncogenic angiogenesis, chronic rheumatoid arthritis, vascular intimal thickening after a percutaneous coronary transluminal angioplasty, vascular atherosclerosis, hemorrhagic apoplexy, acute myocardial infarction, chronic heart failure, aneurysm, lung cancer metastasis, adult respiratory distress syndrome, asthma, interstitial pulmonary fibrosis, chronic rhinosinusitis, bronchitis or chronic obstructive pulmonary disease (COPD).

Abstract: Compounds represented by formula (I) and the formula (IV) have an inhibitory activity of MMP-9 production, therefore, are useful as a medicine agent with fewer side effects than conventional MMP enzyme activity inhibitors, as a prophylactic and therapeutic drug for oncogenic angiogenesis, chronic rheumatoid arthritis, vascular intimal thickening after a percutaneous coronary transluminal angioplasty, vascular atherosclerosis, hemorrhagic apoplexy, acute myocardial infarction, chronic heart failure, aneurysm, lung cancer metastasis, adult respiratory distress syndrome, asthma, interstitial pulmonary fibrosis, chronic rhinosinusitis, bronchitis or chronic obstructive pulmonary disease (COPD).

Abstract: An erythromycin A derivative represented by Formula wherein R1 is a group represented by the formula: a group represented by the formula: (c) pyridylacetyl, (d) cycloalkylmethyl or (e) 1,2 bis-(ethoxycarbonyl)vinyl, R2 is the same group as defined for R1, hydrogen, alkyl, alkanoyl, alkoxycarbonyl, R1 and R2 together may form ═CH—R14, or R1 and R2 together with the nitrogen atom to which they are attached may form: R3 is hydrogen, alkyl or cinnamyl, R4 is hydrogen, acetyl, ethylsuccinyl or nicotinoyl, A is —OC(═O)—R17, —OC(═O)—CH2—R17, —OC(═O)—NH—R17, —O—R17 or —OC(═O)—O—R17, and R5 and R6 are each hydrogen or alkyl.

Abstract: An erythromycin A derivative represented by the formula: wherein n is an integer of from 1 to 8, R1 is a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, R2 is a pyridylmethyl group, a quinolylmethyl group, a pyridylsulfonyl group or quinolylsulfonyl group, R3 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or a cinnamyl group, R4 is a cladinosyloxy group or a group represented by the formula: wherein m is 0 or 1, R5 is a pyridyl group, a quinolyl group, a phenyl group, a phenyl group substituted with one, two or three members selected from alkyl groups having 1 to 6 carbon atoms, a nitro group, alkoxy groups having 1 to 3 carbon atoms and halogen atoms, or a pyridyl or quinolyl group substituted with one or two members selected from alkyl groups having 1 to 6 carbon atoms, a nitro group, alkoxy groups having 1 to 3 carbon atoms and halogen atoms; or a pharmaceutically acceptable salt thereof.

Abstract: An erythromycin A derivative represented by Formula (I): ##STR1## (wherein n is an integer of 2 to 4, R.sup.1 is a pyridylmethyl group, a furylmethyl group, a thienylmethyl group, a quinolylmethyl group or a benzyl group having 1 to 3 substitutents selected from the group consisting of an alkyl group having 1 to 5 carbon atoms, a nitro group, an alkoxy group having 1 to 5 carbon atoms, an amino group and an amino group substituted by 1 or 2 alkyl groups having 1 to 5 carbon atoms, R.sup.2 is the same group as defined for R.sup.1, a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an acetyl group or a pyridylacetyl group, and R.sup.3 is an alkyl group having 1 to 5 carbon atoms or a cinnamyl group) or a pharmaceutically acceptable salt thereof has a strong antibacterial activity against not only known erythromycin-sensitive bacteria but also erythromycin-resistant bacteria and Haemophilus influenzae.

Abstract: An erythromycin A derivative represented by Formula (I): ##STR1## wherein R is a pyridyl group, a quinolyl group, a nitrophenyl group or a methoxyphenyl group, or a pharmaceutically acceptable salt thereof has a strong antibacterial activity not only against erythromycin-sensitive bacteria but also against certain erythromycin-resistant bacteria and Haemophilus influenzae.

Abstract: An erythromycin A derivative represented by the formula (I): ##STR1## ?wherein R.sup.1 is a group represented by the formula: --OCOCH.sub.2 Y (wherein Y is a pyridyl group, a quinolyl group, a p-nitrophenyl group or a group represented by the formula: --NR.sup.4 R.sup.5 (wherein R.sup.4 and R.sup.5 may be the same or different, and are each a hydrogen atom, a methyl group, a pyridylmethyl, a quinolylmethyl group or a benzyloxycarbonyl group)) or a cladinosyloxy group, R.sup.2 is a hydrogen atom, or R.sup.1 and R.sup.2 together form an oxo group, R.sup.3 is a hydrogen atom, an acetyl group, an ethylsuccinyl group or a nicotinoyl group! or a pharmaceutically acceptable salt thereof has a strong antibacterial activity against not only Gram-positive bacteria but also some Gram-negative bacteria, in particular, Haemophilus influenzae which is a serious factor of infectious diseases in the respiratory organs.

Abstract: Object: To provide novel macrolide antibiotics having a strong antibacterial activity. Constitution: 5-O-desosaminylerythronolide A derivatives represented by the formula: ##STR1## [wherein -A- - is a group of --N(R.sup.3)-- (wherein R.sup.3 is a hydrogen atom or an alkyl group having 1-3 carbon atoms) or a group represented by --N.dbd., and R.sup.1 and R.sup.2 are each a hydrogen atom or an alkyl group having 1-3 carbon atoms] which is a tricyclic carbamate of 5-0-desosaminylerythronolide A derivative having a ketone at the 3-position, being substituted by a methoxy group at the 6-position, and a pharmaceutically acceptable acid addition salt thereof; and a compound represented by the formula: ##STR2## (wherein R.sup.4 is an acetyl group or a propionyl group) which is an intermediate useful for the preparation of the 3-ketone forms of 5-O-desosaminylerythronolide A derivatives.

Abstract: Object:Provision of novel macrolide antibiotics having a strong antibacterial activity.Construction:Compounds represented by the formula: ##STR1## which are obtained by introducing a certain substituted carbonyloxy group into 5-O-desosaminylerythronolide derivatives at the 3-position; and pharmaceutically acceptable acid addition salts thereof.

Abstract: A novel macloride antibiotic having a potent antibacterial activity, represented by the formula: ##STR1## which is obtained by introducing a specific aryloxy or alkoxy group into the 3-position of a 5-O-desosaminylerythronolide derivative; or phamaceutically acceptable acid addition salts thereof.

Abstract: Object: To provide a novel macrolide antibiotic having a strong antibacterial activity.Constitution: 11-Amino-3,11-dideoxy-3-oxo-5-O-desosaminyl-6-O-methylerythronolide A 11-N,12-O-cyclic carbamate which has a ketone at the 3-position and a methylated hydroxyl group at the 6-position of a 5-O-desosaminylerythronolide A derivative, and pharmaceutically acceptable acid addition salts thereof.

Abstract: Provision of novel macrolide antibiotics having a strong antibacterial activity.Construction:Compounds represented by the formula: ##STR1## which are obtained by introducing a carbamoyl group into 5-O-desosaminyl-6-O-methylerythronolide derivatives at the 3-position; and pharmaceutically acceptable acid addition salts thereof.

Abstract: This invention provides 6-O-methylerythromycin A derivatives represented by the following formula ##STR1## (wherein R.sup.1 and R.sup.2 each represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, and A represents a nitrogen atom or a N.fwdarw.O group) and their pharmaceutically acceptable salts. The erythromycin A derivatives have a strong antimicrobial activity against Gram-negative bacteria and have a much stronger activity against Gram-positive bacteria than previously known compounds.

Abstract: Erythromycins showing an extremely relieved bitterness at administration and an improved absorbability in vivo when orally administered are provided.A compound having a group represented by the following formula:--O--CO--O--[(CH.sub.2).sub.m --O].sub.n --R(wherein R represents an alkyl group having from 1 to 12 carbon atoms, m represents an integer of from 2 to 4, and n represents an integer of from 1 to 7) at the 2'-position of erythromycins or a salt thereof.

Abstract: A 6-O-methylerythromycin A oxime derivative represented by the formula ##STR1## wherein X is a substituted benzyl group, a substituted phenyl group, an .alpha.-methylbenzyl group, an .alpha.-methylphenethyl group, a diphenylmethyl group, a trityl group, a dibenzosuberanyl group, or a group of the formula --(CH.sub.2).sub.n --R, and Y is a hydrogen atom, a substituted phenyl group or a 2-aminothiazol-4-ylmethylcarbonyl group, and a pharmaceutically acceptable salt thereof are disclosed. These compounds have antibacterial activity against erythromycin resistant bacteria.

Abstract: Erthromycin A derivatives represented by the general formula ##STR1## wherein R.sup.1 is a group of the formula R.sup.7 CH.sub.2 -- (wherein R.sup.7 is a hydrogen group or a lower alkyl group) or a group of the formula R.sup.8 O-- (wherein R.sup.8 is a lower alkyl group), R.sup.2 is R.sup.8, a cycloalkyl group, a phenyl group or an aralkyl group.), or R.sup.2 and R.sup.7 together form an alkylene group, R.sup.3 is a hydrogen atom, a lower alkyl group, a phenyl group or an aralkyl group, or R.sup.3 and R.sup.7 together form an alkylene group, or R.sup.2 and R.sup.3 together form an alkylene group, R.sup.4 is a lower alkyl group, R.sup.5 is a substituted silyl group, and R.sup.6 is a hydrogen atom or R.sup.5, are disclosed. These compounds are useful as intermediates for the synthesis of antibacterial agents.

Abstract: Erythromycin derivatives represented by the general formula ##STR1## wherein R.sup.1 is a hydrogen atom or a methyl group, R.sup.2 is a hydrogen atom or a hydroxy group, R.sup.3 is a hydrogen atom, a lower alkanoyl group, an alkoxycarbonyl group or an alkylsuccinyl group, and the salts thereof are disclosed. These compounds have antibacterial activity.

Abstract: A novel 6-O-methylerythromycin A derivative represented by the formula ##STR1## and the salts thereof are disclosed. These compounds are useful as intermediates for preparation of 6-O-methylerythromycin A and useful as antibiotics.

Abstract: A method for the selective methylation of a hydroxy group at the 6-position of an erythromycin A derivative which comprises converting an erythromycin A derivative into an erythromycin A 9-oxime derivative, and reacting the resulting ethythromycin A 9-oxime derivative with an methylating agent.

Abstract: A method for the selective methylation of the hydroxy group at the 6-position of erythromycin A derivatives which comprises reacting a compound represented by the formula R-X (wherein R is a 2-alkenyl group, a benzyl group or a substituted benzyl group, and X is a halogen atom), reacting the resulting quaternary salt compound with a methylating agent, and then eliminating R groups of the resulting compound to give 6-O-methylerythromycin A 9-oxime, is disclosed.