Abstract: The present invention provides a therapeutic and/or preventive agent against gastroparesis symptom which is appropriate for continuous medication and which comprises a compound represented by formula (1): (wherein R1 represents a C1-C6 alkyl group and R2 represents a C1-C6 alkyl group) or a pharmaceutically acceptable salt thereof as an active ingredient. The erythromycin derivative of the formula (1) has an efficacy of improving gastroparesis and this action of the derivative in improving gastroparesis symptom is not found in ABT-229, a different motilin agonist erythromycin derivative. Further, the compound of the formula (1) is also appropriate for long-term clinical use because of its much weaker antibacterial action than that of erythromycin. Accordingly, the present invention provides a pharmaceutical agent that is safe and exhibits potent therapeutic and/or preventive effect in an effort to improve symptomatic gastroparesis.

Abstract: A compound of Formula (1) or a pharmaceutically acceptable salt thereof: wherein R1 represents a C1-C6 alkyl group and R2 represents a C1-C6 alkyl group, while unlike a laxative, is effective in the treatment of constipation.

Abstract: The present invention provides a therapeutic and/or preventive agent against gastroparesis symptom which is appropriate for continuous medication and which comprises a compound represented by formula (1): (wherein R1 represents a C1-C6 alkyl group and R2 represents a C1-C6 alkyl group) or a pharmaceutically acceptable salt thereof as an active ingredient. The erythromycin derivative of the formula (1) has an efficacy of improving gastroparesis and this action of the derivative in improving gastroparesis symptom is not found in ABT-229, a different motilin agonist erythromycin derivative. Further, the compound of the formula (1) is also appropriate for long-term clinical use because of its much weaker antibacterial action than that of erythromycin. Accordingly, the present invention provides a pharmaceutical agent that is safe and exhibits potent therapeutic and/or preventive effect in an effort to improve symptomatic gastroparesis.

Abstract: A pharmaceutical composition, and a method using the composition, for prevention and/or treatment of fatty liver or hepatic disease, the composition comprising, as an active ingredient, a compound of the formula (1): where R1 is a hydrogen atom, an acyl group, or an arylalkoxycarbonyl group; and R2 and R3 are each independently a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, or a substituted or unsubstituted alkynyl group, or R2 and R3 may combine to form a cycloalkyl group.

Abstract: Herein provided is a method for evaluating the antioxidant potential of a biological sample comprising the steps of: (a) collecting a sample containing at least oxidizable substrates from a living body; (b) initiating an oxidation reaction of said oxidizable substrates; (c) continuing said oxidation reaction; and (d) quantifying oxidation products formed from said oxidizable substrates by determining the rate of said oxidation reaction during the progress thereof or by performing an assay after said oxidation reaction has been stopped, wherein said steps (b) and (c) are performed in the presence of one or more antioxidant components.

Abstract: The present invention provides a therapeutic and/or preventive agent for defecation dysfunction, which is suitable for continuous medication and comprises as an active ingredient a compound of Formula (1) or a pharmaceutically acceptable salt thereof: (wherein R1 represents a C1-C6 alkyl group and R2 represents a C1-C6 alkyl group). The above erythromycin derivative of Formula (1) has an improving effect on defecation dysfunction; and this improving effect on defecation dysfunction leads to acceleration of normal defecation, unlike a laxative. Further, the above compound of Formula (1) is also suitable for long-term clinical use because of its weaker antibacterial action than erythromycin. Thus, the present invention provides an agent having a safe and potent therapeutic and/or preventive effect on defecation dysfunction.

Abstract: An object of the present invention is to provide a pharmaceutical composition and a method for preventing or treating a respiratory disease. The pharmaceutical composition comprises a compound represented by formula (1): or a pharmaceutically acceptable salt thereof as an active ingredient.

Abstract: Herein provided is a novel pharmaceutical composition for ameliorating the vascular tone-regulating function of vascular endothelium, comprising a compound represented by formula (1): wherein R1 represents a hydrogen atom or an acyl or arylalkyloxycarbonyl group; R2 and R3 are identical or different and represent an optionally substituted alkyl group, an optionally substituted alkenyl group or an optionally substituted alkynyl group; or R2 and R3 may together form a cycloalkyl group.

Abstract: A pharmaceutical composition comprising a compound represented by the following formula: 1

Abstract: 2,3-Dihydrobenzofuran derivatives of general formula (1): wherein R1 represents a hydrogen atom or an acyl group; R2, R3 and R4 represent a hydrogen atom, a lower alkyl group or a lower alkenyl group; R5 and R6 combine to form a cycloalkyl group or a saturated heterocyclic group containing one or more oxygen atoms or sulfur atoms, provided that R2 and R3 can not simultaneously represent a t-butyl group, or optically active isomers or pharmaceutically acceptable salts thereof are useful as therapeutic or prophylactic agents for various renal diseases and as organ preservatives.

Abstract: 2,3-Dihydrobenzofuran derivatives of general formula 1

Abstract: An intimal thickening inhibitory agent comprising, as an active ingredient, a compound represented by formula (1): wherein x represents an oxygen atom or a group of formula (2) —S—(O)n  (2) wherein n represents an integer of from 0 to 2, R1 represents a hydrogen atom or an acyl group; R2 represents a hydrogen atom, a lower alkyl group or a lower alkenyl group; R3 represents a lower alkyl group; and R4, R5, and R6, which may be the same or different, each represent a hydrogen atom or a substituted or unsubstituted alkyl group; or R3 and R4 may be taken together to form a 5-membered ring; or R5 and R6 may be taken together to form a cycloalkyl group; provided that R6 is nil when R3 and R4 are taken together to form benzofuran or benzo[b]thiophene.

Abstract: Herein disclosed are prophylactic/therapeutic agents for atherosclerosis containing a compound of general formula (1): wherein R1 represents a hydrogen atom or an acyl group, R2 represents a lower alkyl group, R3 represents a hydrogen atom or a lower alkyl group, and R4, R5 and R6 represent a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group or an aryl group, or R2 and R4 together with the oxygen atom may form a furan or dihydrofuran ring, or R5 and R6 may combine to form a cycloalkyl group or a heterosubstituted cycloalkyl group in which one or more methylene groups of the cycloalkyl group are replaced by oxygen, sulfur or alkyl-substituted nitrogen atoms, a possible optically active isomer or a pharmaceutically acceptable salt thereof, as an active ingredient.

Abstract: 2,3-Dihydrobenzofuran derivatives of general formula (1): wherein R1 represents a hydrogen atom or an acyl group; R2, R3 and R4 represent a hydrogen atom, a lower alkyl group or a lower alkenyl group; R5 and R6 represent a hydrogen atom or an optionally substituted alkyl group, or R5 and R6 combine to form a cycloalkyl group or a saturated heterocyclic group containing one or more oxygen atoms or alkyl-substituted nitrogen atoms, provided that R2 and R3 can not simultaneously represent a t-butyl group, or optically active isomers or pharmaceutically acceptable salts thereof are useful as therapeutic or prophylactic agents for various renal diseases and as organ preservatives.

Abstract: Herein disclosed are prophylactic/therapeutic agents for atherosclerosis containing a compound of general formula (1): ##STR1## wherein R.sup.1 represents a hydrogen atom or an acyl group, R.sup.2 represents a lower alkyl group, R.sup.3 represents a hydrogen atom or a lower alkyl group, and R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group or an aryl group, or R.sup.2 and R.sup.4 together with the oxygen atom may form a furan or dihydrofuran ring, or R.sup.5 and R.sup.6 may combine to form a cycloalkyl group or a heterosubstituted cycloalkyl group in which one or more methylene groups of the cycloalkyl group are replaced by oxygen, sulfur or alkyl-substituted nitrogen atoms, a possible optically active isomer or a pharmaceutically acceptable salt thereof, as an active ingredient.

Abstract: Herein disclosed are therapeutic agents for renal diseases and organ preservatives containing a compound represented by the general formula (1): ##STR1## wherein X represents an oxygen atom or a group represented by the general formula (2): ##STR2## where n represents an integer from 0 to 2, R.sub.1 represents a hydrogen atom or an acyl group, R.sub.2 represents a hydrogen atom, a lower alkyl group or a lower alkenyl group, R.sub.3 represents a lower alkyl group, R.sub.4, R.sub.5 and R.sub.6, which may be the same or different, each represents a hydrogen atom or an optionally substituted alkyl group, and R.sub.6 further represents a formyl, carboxyl, lower alkoxycarbonyl or optionally substituted carbamoyl group, or R.sub.3 and R.sub.4 may be taken together to form a five-membered ring, or R.sub.5 and R.sub.6 may be taken together to form a cycloalkyl group, provided that when the five-membered ring formed by R.sub.3 and R.sub.4 and the benzene ring form benzofuran or benzo[b]thiophene, R.sub.6 is absent.

Abstract: An intimal thickening inhibitory agent comprising, as an active ingredient, a compound represented by formula (1): ##STR1## wherein X represents an oxygen atom or a group of formula (2): ##STR2## wherein n represents an integer of from 0 to 2, R.sub.1 represents a hydrogen atom or an acyl group; R.sub.2 represents a hydrogen atom, a lower alkyl group or a lower alkenyl group; R.sub.3 represents a lower alkyl group; and R.sub.4, R.sub.5, and R.sub.6, which may be the same or different, each represent a hydrogen atom or a substituted or unsubstituted alkyl group; or R.sub.3 and R.sub.4 may be taken together to form a 5-membered ring; or R.sub.5 and R.sub.6 may be taken together to form a cycloalkyl group; provided that R.sub.6 is nil when R.sub.3 and R.sub.4 are taken together to form benzofuran or benzo[b]thiophene.

Abstract: Compounds represented by the general formula (I), as well as intermediates for the synthesis of thereof: ##STR1## where R.sup.1 is a hydrogen atom or an acyl group; R.sup.2 is a lower alkyl group; R.sup.3 is a hydrogen atom or a lower alkyl group; R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl or aryl group; R.sup.2 and R.sup.4, when taken together, may form a 5-membered ring; R.sup.5 and R.sup.6, when taken together, may form a cycloalkyl group or a heterocyclic group in which at least one methylene on the ring of a cycloalkyl group is substituted by an oxygen atom, a sulfur atom or an alkyl-substituted nitrogen atom, provided that R.sup.6 is not present if the ring formed by R.sup.2 and R.sup.4 taken together is a benzofuran ring.

Abstract: Compounds represented by the general formula (I), as well as intermediates for the synthesis of thereof: ##STR1## where R.sup.1 is a hydrogen atom or an acyl group; R.sup.2 is a lower alkyl group; R.sup.3 is a hydrogen atom or a lower alkyl group; R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl or aryl group; R.sup.2 and R.sup.4, when taken together, may form a 5-membered ring; R.sup.5 and R.sup.6, when taken together, may form a cycloalkyl group or a heterocyclic group in which at least one methylene on the ring of a cycloalkyl group is substituted by an oxygen atom, a sulfur atom or an alkyl-substituted nitrogen atom, provided that R.sup.6 is not present if the ring formed by R.sup.2 and R.sup.4 taken together is a benzofuran ring.

Abstract: Compounds represented by the general formula as well as intermediates for the synthesis of thereof: ##STR1## where R.sup.1 is a hydrogen atom or an acyl group; R.sup.2 is a lower alkyl group; R.sup.3 is a hydrogen atom or a lower alkyl group; R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl or aryl group; R.sup.2 and R.sup.4, when taken together, may form a 5-membered ring; R.sup.5 and R.sup.6, when taken together, may form a cycloalkyl group or a heterocyclic group in which at least one methylene on the ring of a cycloalkyl group is substituted by an oxygen atom, a sulfur atom or an alkyl-substituted nitrogen atom, provided that R.sup.6 is not present if the ring formed by R.sup.2 and R.sup.4 taken together is a benzofuran ring.