Abstract: The invention relates to C-3 substituted kynurenic acid derivatives with the general formula (I) wherein R1 is C1-7alkyl-, R6R7N—C1-7alkyl-, C6-10aryl-C1-7alkyl group; R2 is H or C1-7alkyl group; or R1 and R2 with the nitrogen atom to which they are attached form a saturated or partially saturated 5-7 membered, optionally benzofused heterocyclic ring, optionally comprising additional N, O, S heteroatoms and optionally being substituted; R3 is —OH, C1-7alkyl-O—, —NH2, C1-7alkyl-NH—, C6-10aryl-C1-7alkyl-NH— or —NH— —(CH2)n—NR8R9 group wherein n is an integer from 1 to 3; R4 is H, C1-7alkyl-, C6-10aryl group or a halogen atom; R5 is H or C6-10aryl group; R6 is C1-7alkyl group; R7 is C1-7alkyl group; or R6 and R7 with the nitrogen atom to which they are attached form a saturated or partially saturated 5-7 membered, optionally benzofused heterocyclic ring, optionally comprising additional N, O, S heteroatoms and optionally being substituted; R8 is C1-7alkyl group; R9 is C1-7alkyl group; R8 and R9 with the nitrogen

Abstract: The present invention is related to 8-hydroxy-quinoline derivatives having multidrug-resistance reversing activity with improved selectivity and increased cytotoxicity towards multidrug-resistant cancer cells, preparation thereof and use of the same in the treatment of cancer, especially multidrug-resistant variants thereof.

Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi

Abstract: The invention relates to pyridazinone and pyridone compounds having formula (I) or (I?), and pharmaceutically acceptable salts, hydrates, and solvates thereof wherein R1/R4 and X and X3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.

Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi

Abstract: The present invention is related to 8-hydroxy-quinoline derivatives having multidrug-resistance reversing activity with improved selectivity and increased cytotoxicity towards multidrug-resistant cancer cells, preparation thereof and use of the same in the treatment of cancer, especially multidrug-resistant variants thereof.

Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi

Abstract: The invention relates to C-3 substituted kynurenic acid derivatives with the general formula (I) wherein R1 is C1-7alkyl-, R6R7N-C1-7alkyl group; C6-10aryl-C1-7alkyl group; R2 is H or C1-7alkyl group; or R1 and R2 with the nitrogen atom to which they are attached form a saturated or partially saturated 5-7 membered, optionally benzofused heterocyclic ring, optionally comprising additional N, O, S heteroatoms and optionally being substituted; R3 is —OH, C1-7alkyl-O—, —NH2, C1-7alkyl-NH—, C6-10aryl-C1-7alkyl-NH— or —NH—(CH2)n—NR8R9 group wherein n is an integer from 1 to 3; R4 is H, C6-10aryl group or a halogen atom; R5 is H or C6-10aryl group; R6 is C1-7alkyl group; R7 is C1-7alkyl group; or R6 and R7 with the nitrogen atom to which they are attached form a saturated or partially saturated 5-7 membered, optionally benzofused heterocyclic ring, optionally comprising additional N, O, S heteroatoms and optionally being substituted; R8 is C1-7alkyl group; R9 is C1-7alkyl group; R8 and R9 with the nitrogen atom to

Abstract: The invention relates to pyridazinone and pyridone compounds having formula (I) or (I?), and pharmaceutically acceptable salts, hydrates, and solvates thereof wherein R1/R4 and X and X3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.

Abstract: The invention relates to pyridazinone and pyridone compounds having formula (I) or (I?), and pharmaceutically acceptable salts, hydrates, and solvates thereof wherein R1/R4 and X and X3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.

Abstract: The invention relates to new morphine derivatives deuterated at the 7,8-position of the morphine ring, furthermore to a process for the preparation thereof, and to pharmaceutical compositions comprising them. The new deuterated morphine derivatives show high and selective ?-opioid receptor binding activity leading to the benefit of higher analgesic activity at lower dosages inducing thereby reduced adverse effects compared to the hydrogenated derivatives. The compounds of the invention are useful for example in the treatment of pain or can be used as antitussive agents with a reduced risk of the possibility of drug abuse.

Abstract: The invention relates to pyridazinone and pyridone compounds having formula (I) or (I?), and pharmaceutically acceptable salts, hydrates, and solvates thereof wherein R1/R4 and X and X3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.

Abstract: A compound for treating a metabolic syndrome, comprising a structure of a 6Cs unit-3Cs unit-6Cs unit (C6-C3-C6) as shown in formula I, wherein: when R1 and R2 are both hydrogens, C3 has only single bonds; when R1 is an oxygen and R2 is one selected from a group consisting of an alkoxy, a benzyloxy and a halogen, C3 has only single bonds; when R1 is a deuterium and R2 is one selected from a group consisting of a hydrogen, an alkoxy, a benzyloxy and a halogen, C3 has one of a single bond and a double bond.

Abstract: The invention relates to pyridazinone and pyridone compounds having formula (I) or (I?), and pharmaceutically acceptable salts, hydrates, and solvates thereof (I) wherein R1/R4 and X and X3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.

Abstract: The invention relates to new morphine derivatives deuterated at the 7,8-position of the morphine ring, furthermore to a process for the preparation thereof, and to pharmaceutical compositions comprising them. The new deuterated morphine derivatives show high and selective ?-opioid receptor binding activity leading to the benefit of higher analgesic activity at lower dosages inducing thereby reduced adverse effects compared to the hydrogenated derivatives. The compounds of the invention are useful for example in the treatment of pain or can be used as antitussive agents with a reduced risk of the possibility of drug abuse.

Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi

Abstract: The invention relates to pyridazinone and pyridone compounds having formula (I) or (I?), and pharmaceutically acceptable salts, hydrates, and solvates thereof (I) wherein R1/R4 and X and X3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.

Abstract: The invention is directed to kynurenic acid analogues and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing said compounds for treating the symptoms of Huntington's disease and preventing the development of the symptoms.

Abstract: The invention relates to chiral cyclic ?-amino acids of Formula (I) and their salts formed with pharmaceutically acceptable acids or bases, wherein the main meanings of the substituents are as follows: R stands for C1-4 Alk; X stands for —COOH, —CONH2, —CONH(C1-4 Alk), —CON(C1-4 Alk)2, —COO(C1-4 Alk), —COPhe-O—(C1-4 Alk) or —CH2OH; Y stands for —NH2, —NHBoc, —NHFmoc, —NH(C1-4 Alk), —N(C1-4 Alk)2, —NHCH2Ph, or Ar—NH—C(?X0)—N(R0)— wherein Ar stands for a phenyl group substituted by C1-4 alkoxy or halogen, X0 stands for O or S, and R0 stands for hydrogen or benzyl; and X+Y stands for —CONH— vagy —CON(Boc)-; with the proviso that when X stands for —COOH, then Y may be only different from —NH2. The invention also relates to pharmaceutical compositions having multidrug-resistance reversing effect that contain one or more compound(s) of Formula (I) or a salt thereof and inert pharmaceutical carriers and/or auxiliary agents. The invention also relates to carboxylic acids of Formula (XX) and their salts.

Abstract: The invention relates to chiral cyclic ?-amino acids of Formula (I) and their salts formed with pharmaceutically acceptable acids or bases, wherein the main meanings of the substituents are as follows: R stands for C1-4 Alk; X stands for —COOH, —CONH2, —CONH(C1-4 Alk), —CON(C1-4 Alk)2, —COO(C1-4 Alk), —COPhe-O-(C1-4 Alk) or —CH2OH; Y stands for —NH2, —NHBoc, —NHFmoc, —NH(C1-4 Alk), —N(C1-4 Alk)2, —NHCH2Ph, or Ar—NH—C(=X0)—N(R0)— wherein Ar stands for a phenyl group substituted by C1-4 alkoxy or halogen, X0 stands for O or S, and R0 stands for hydrogen or benzyl; and X+Y stands for —CONH— vagy —CON(Boc)-; with the proviso that when X stands for —COOH, then Y may be only different from —NH2. The invention also relates to pharmaceutical compositions having multidrug-resistance reversing effect that contain one or more compound(s) of Formula (I) or a salt thereof and inert pharmaceutical carriers and/or auxiliary agents. The invention also relates to carboxylic acids of Formula (XX) and their salts.