Abstract: Disclosed are a novel rebamipide prodrug, a method for preparing the same, and use thereof. Also, a pharmaceutical composition comprising the novel rebamipide prodrug as an active ingredient is provided. The rebamipide prodrug is increased 25-fold in absorption rate compared to rebamipide itself, and can be applied to the prophylaxis or therapy of gastric ulcer, acute gastritis, chronic gastritis, xerophthalmia, cancer, osteoarthritis, rheumatoid arthritis, or obesity.

Abstract: The present invention provides a novel pyridine derivative, a pharmaceutically acceptable salt thereof, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient. The pyridine derivative according to the present invention inhibits Raf kinase (B-Raf, Raf-1, or B-RafV600E) and a vascular endothelial growth factor receptor (VEGFR2) involved in angiogenesis, and thus, can be favorably used for the prevention or treatment of melanoma, colorectal cancer, prostate cancer, thyroid cancer, lung cancer, pancreatic cancer, ovarian cancer, or the like, which is induced by RAS mutation.

Abstract: The present invention provides a novel pyridine derivative, a pharmaceutically acceptable salt thereof, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient. The pyridine derivative according to the present invention inhibits Raf kinase (B-Raf, Raf-1, or B-RafV600E) and a vascular endothelial growth factor receptor (VEGFR2) involved in angiogenesis, and thus, can be favorably used for the prevention or treatment of melanoma, colorectal cancer, prostate cancer, thyroid cancer, lung cancer, pancreatic cancer, ovarian cancer, or the like, which is induced by RAS mutation.

Abstract: Disclosed are a novel rebamipide prodrug, a method for preparing the same, and use thereof. Also, a pharmaceutical composition comprising the novel rebamipide prodrug as an active ingredient is provided. The rebamipide prodrug is increased 25-fold in absorption rate compared to rebamipide itself, and can be applied to the prophylaxis or therapy of gastric ulcer, acute gastritis, chronic gastritis, xerophthalmia, cancer, osteoarthritis, rheumatoid arthritis, or obesity.

Abstract: A pyrimidinedione derivative of formula (I) or a pharmaceutically acceptable salt thereof exhibits excellent inhibitory activity against hepatitis C virus.

Abstract: A pyrimidinedione derivative of formula (I) or a pharmaceutically acceptable salt thereof exhibits excellent inhibitory activity against hepatitis C virus.

Abstract: The present invention relates to pyrimidinedione derivatives of following formula (I) which are useful as antiviral agents, especially as agents for treatment of AIDS, pharmaceutically acceptable salts thereof, process for the preparation thereof and pharmaceutical compositions containing the same, wherein R represents cyclopropyl; cyclobutyl; cyclohexyl; unsubstituted or mono-, di- or trisubstituted phenyl with a group selected from hydroxy, C1–C4 alkyl, C1–C4 alkoxy, halogen, trifluoromethyl, cyano and amino; 1- or 2-naphthyl; 9-anthracenyl; 2-anthraquinonyl; unsubstituted or substituted pyridyl with a group selected from C1–C4 alkyl, C1–C4 alkoxy, cyano and halogen; 2-, 3- or 4-quinolinyl; oxiranyl; 1-benzotriazolyl; 2-benzoxazolyl; furanyl substituted with C1–C4 alkoxycarbonyl; C1–C4 alkylcarbonyl; or benzoyl, R1 represents halogen or C1–C4 alkyl, R2 and R3 represent independently hydrogen or C1–C4 alkyl, X represents oxygen atom, and Y represents oxygen atom, sulfur atom or carbonyl.

Abstract: The present invention relates to a novel compound of formula (I) and its pharmaceutically acceptable acid addition salt, and process for the preparation thereof, which have strong antitumor activities and very low toxicity: wherein R1 and R2 are independently hydrogen, C1-C4 alkyl, C1-C4 alkylcarboxyl, C1-C4 alkylcarbonyl, C1-C4 alkoxy, C1-C4 hydroxyalkyl, C1-C4 aminoalkyl or C1-C4 hydroxyiminoalkyl, or R1 and R2 are fused to form C3-C4 unsaturated ring; R3, R4, R5, R6 and R7 are independently hydrogen, halogen, hydroxy, nitro, amino, C1-C4 alkyl, C1-C4 alkylcarboxyl, C1-C4 alkylcarbonyl, C1-C4 alkoxy, C1-C4 thioalkoxy; R8 is C1-C4 alkyl; Y is oxygen, sulphur, amino, subsitituted amino or C1-C4 thioalkyl; Z is C1-C4 alkoxy, C1-C4 alkyl, C1-C4 alkylamino or C1-C4 thioalkoxy; X1 and X2 are independently CH or nitrogen; and —N═C— and —C═Y— may form a single bond or a double bond provided that if —N═C— forms a single bond, —C═Y&md

Abstract: The present invention relates to new 9-aminoacridine derivatives of general formula (I), wherein A is hydrogen or (II) (wherein X is oxygen or sulfur, R1, R2, R3, R4 and R5 are independently hydrogen, halogen, nitro, amino, hydroxy, C1-C4 lower alkylhydroxy, C1-C4 lower alkylamino, C1-C8 alkyl, C1-C4 lower alkoxy or C1-C4 lower alkyloxycarbonyl and m and n are independently an integer of 0, 1 or 2), R6, R7, R8 and R9 are independently C1-C8 alkyl or C1-C4 lower alkoxy, and Y is hydrogen, amino, —N═CHR′(wherein R′ is hydrogen, benzyl, C1-C8 alkyl or C1-C6 lower alkylamino), (III) (wherein R″ is hydrogen, benzyl, C1-C8 alkyl or C1-C6 lower alkylamino, and R′″ is hydrogen, benzyl, C1-C8 alkyl or amino protecting group) or (IV) (wherein, X is as defined above, R1′, R2′, R3′, R4′ and R5′ are independently hydrogen, halogen, nitro, amino, hydroxy, C1-C4 lower alkylhydroxy, C1-C4 lower alkylamino, C1-C8 alkyl, C1-C4 lower alkoxy or C1-C4 lower al

Abstract: The present invention relates to a novel compound of the general formula (I) and its pharmaceutically acceptable acid addition salt, and process for the preparation thereof, which have strong antimumor activities and very low toxicity.

Abstract: The present invention relates to new 9-aminoacridine derivatives of general formula (I), wherein A is hydrogen or (II) (wherein X is oxygen or sulfur, R1, R2, R3, R4 and R5 are independently hydrogen, halogen, nitro, amino, hydroxy, C1-C4 lower alkylhydroxy, C1-C4 lower alkylamino, C1-C8 alkyl, C1-C4 lower alkoxy or C1-C4 lower alkyloxycarbonyl and m and n are independently an integer of 0, 1 or 2), R6, R7, R8 and R9 are independently C1-C8 alkyl or C1-C4 lower alkoxy, and Y is hydrogen, amino, -N═CHR′(wherein R′ is hydrogen, benzyl, C1-C8 alkyl or C1-C6 lower alkylamino), (III) (wherein R″ is hydrogen, benzyl, C1-C8 alkyl or C1-C6 lower alkylamino, and R′″ is hydrogen, benzyl, C1-C8 alkyl or amino protecting group) or (IV) (wherein, X is as defined above, R1′, R2′, R3′, R4′ and R5′ are independently hydrogen, halogen, nitro, amino, hydroxy, C1-C4 lower alkylhydroxy, C1-C4 lower alkylamino, C1-C8 alkyl, C1-C4 lower alkoxy or C1-C4 lower alkylcar

Abstract: The present invention relates to novel compound having strong antimumor activities of the general formula(I) ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, substituted or unsubstituted C.sub.1 -C.sub.8 alkyl, substituted or unsubstituted C.sub.3 -C.sub.6 cycloalkyl, substituted or unsubstituted C.sub.2 -C.sub.8 unsaturated alkyl, ketone, substituted or unsubstituted aryl, substituted or unsubstituted C.sub.1 -C.sub.4 alkoxy, substituted or unsubstituted arylhydroxy, substituted or unsubstituted amino, C.sub.1 -C.sub.4 lower ester, C.sub.1 -C.sub.4 lower thioester, thiol, substituted or unsubstituted carboxyl, epoxy, substituted or unsubstituted C.sub.1 -C.sub.4 lower thioalkoxy; or R.sub.1 and R.sub.2 are fused to form C.sub.3 -C.sub.4 saturated or unsaturated chain; R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen, halogen, hydroxy, nitro, C.sub.1 -C.sub.4 lower ester, C.sub.1 -C.sub.4 lower alkyl, C.sub.1 -C.sub.4 lower thioalkyl, substituted or unsubstituted C.

Abstract: The present invention relates to novel compound of general formula (I) and pharmaceutically acceptable salts thereof, and process for the preparation of such derivatives and to pharmaceutical compositions containing the same as active ingredients. ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 represents independently hydrogen atom, halogen atom, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 thioalkyl, C.sub.3 -C.sub.8 optionally substituted cyclicalkyl, unsaturated alkyl, substituted alkyl hydroxyl or aryl hydroxyl, C.sub.1 -C.sub.10 alkylamine, nitro, C.sub.1 -C.sub.4 lower ester, C.sub.1 -C.sub.4 lower alkoxy, C.sub.1 -C.sub.4 lower thioalkoxy; Z represents oxygen atom, sulfur atom, carbon atom and carbonyl group; X represents oxygen atom, sulfur atom; n represents an integer of 1-3; and (sub)cycloalk(en)yl represents ##STR2## in which R.sub.4 and R.sub.