Abstract: The invention relates to new pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention also relates to the process for producing such compounds and key intermediates used in the process. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention also provides a method for manufacture of medicaments useful in the treatment of such disorders.

Abstract: The present invention relates to new pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention al so relates to the process for producing such compounds. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention al so provides a method for manufacture of medicaments useful in the treatment of such disorders.

Abstract: The present invention relates to new pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention also relates to the process for producing such compounds. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention also provides a method for manufacture of medicaments useful in the treatment of such disorders.

Abstract: The present invention relates to new pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention al so relates to the process for producing such compounds. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention al so provides a method for manufacture of medicaments useful in the treatment of such disorders.

Abstract: The present invention relates to new pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention also relates to the process for producing such compounds. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention also provides a method for manufacture of medicaments useful in the treatment of such disorders.

Abstract: The present invention relates to the indole derivatives of formula (I), wherein R1-R6 and X are defined in the claims and optical antipodes or racemates and/or salts thereof which are selective antagonists of bradykinin B1 to process for producing these compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.

Abstract: The present invention relates to new 4-benzylidene-piperidin derivatives of formula (I), useful as NMDA, in a particular NR2B subunit containing receptor antagonists and analgesica.

Abstract: The new benzoyl urea derivatives of formula (I) wherein the meaning of X and Y independently are hydrogen atom, hydroxy, benzyloxy, amino, nitro, C1-C4 alkylsulfonamido optionally substituted with a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted with a halogen atom or halogen atoms, C1-C4 alkoxy, aroyl-carbamoyl optionally substituted with halogen atom or C1-C4 alkyl or C1-C4 alkoxycarbonyl group, or the neighboring X and Y groups optionally form together with one or more identical or different additional hetero atom and —CH? and/or —CH2— groups an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably morpholine, pyrrole, pyrrolidine, oxo- or thioxo-pyrrolidine, pyrazole, pyrazolidine, imidazole, imidazolidine, oxo- or thioxo-imidazole or imidazolidine, 1,4-oxazine, oxazole, oxazolidine, triazole, oxo- or thioxo-oxazolidine, or 3-oxo-1,4-oxazine ring, V and Z independently are hydrogen or halogen atom, cyano, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl, hydroxy o

Abstract: The present invention relates therefore first to new indole-2-carboxamidine derivatives of formula (I)—wherein the meaning of X is hydrogen or halogen atom, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl group, Y, V and Z independently are hydrogen or halogen atom, hydroxy, cyano, C1-C4 alkylsulfonamido optionally substituted by a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted by a halogen atom or halogen atoms, trifluoromethyl, trifluoromethoxy, C1-C4 alkyl, C1-C4 alkoxy group, or the neighboring V and Z groups in given case together with one or more identical or different additional hetero atom and —CH? and/or —CH2— groups can form an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably benzene, dioxolane ring, A, B and C independently are substituted carbon atom or one of them is nitrogen atom, and the salts thereof.

Abstract: The new kynurenic acid amide derivatives of formula (I): and optical antipodes, racemates and the salts thereof are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor.

Abstract: The present invention relates to new 4-benzylidene-piperidin derivatives of formula (I), useful as NMDA, in a particular NR2B subunit containing receptor antagonists and analgesica.

Abstract: The invention relates to new heterocyclic carboxylic acid amide derivatives of formula (I)—wherein the meaning of X is hydrogen or halogen atom, hydroxy, cyano, C1-C4 alkylsulfonamido optionally substituted by a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted by a halogen atom or halogen atoms, arylsulfonamido groups, is —CH? group or —N? atom, Z is one or more hydrogen or halogen atom, C1-C4 alkyl, C1-C4 alkoxy, cyano, trifluromethyl, trifluoromethoxy group and to the salts thereof, which are antagonists of NMDA receptor or are intermediates for preparing thereof.

Abstract: The present invention relates to a compound of formula (I): wherein: V and U are hydrogen, halogen, C1-C4 alkylamino, or together form a group that contains one or more heteroatoms, and that taken together with one or more: (a) hydrogen atoms; (b) carbon atoms; (c) —CH? groups; (d) —CH2— groups; or (e) additional heteroatoms of the same or different type; or any combination thereof, form a 4-7 membered homocyclic or heterocyclic ring, wherein the homocyclic or heterocyclic ring may combine with the phenyl group to form a bicyclic ring, and wherein the homocyclic or heterocyclic ring or the bicyclic ring may contain one or more oxo, thioxo, amino, mercapto, trifluoromethyl, C1-C4 alkyl, ?S or —SH groups; W: is —CO—, —CH2— or —CH2—(C1-C4 alkyl)-; X: is —CO—; Y: is —O—, C1-C4 alkylene, C1-C4 alkynylene, cycloalkylene, aminocarbonyl, —NH—, —N(C1-C4 alkyl)-, -C1-C4 alkylene-N(C1-C4 alkyl)-, —CH2O—, —CH(OH)— or —OCH2—; Z: is hydrogen, halogen, nitro, amino, C1-C4 alkyl, C1-C4 alkoxy, cyano, trifluorometh

Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3 and R4 groups is hydroxy, and the others are each hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a nitrogen atom, or pharmaceutically acceptable salts thereof formed with acids or bases.

Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) where two of the neighboring R1, R2, R3 and R4 groups form an imidazole ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.

Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein two of the neighboring R1, R2, R3 and R4 groups form an oxo-oxazolidine ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.

Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3 and R4 groups is hydroxy, and the others are each hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.

Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) where two of the neighboring R1, R2, R3 and R4 groups form an imidazole ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.

Abstract: New Formula (I) compounds are disclosed having NR2B selective NMDA receptor antagonist activity: wherein one of the neighboring R1, R2, R3 and R4 groups is OH or NH2 and the others are each hydrogen , or two of the neighboring R1, R2 R3 and R4 groups in given case together with one or more identical or different additional hetero atom and —CH? and/or —CH2— groups forms a 5-6 membered homo- or heterocyclic ring, preferably pyrrole, pyrazole, imidazole, oxazole, oxo-oxazolidine, or 3-oxo-1,4-oxazine ring, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by hydroxy group, and/or in given case phenyl or phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), anilino, phenyl-(C1-C4 alkylamino), [phenyl-(C1-C4 alkyl)]-amino, benzoyl, hydroxy-diphenylmethyl, C1-C4 alkoxycarbonyl-phenoxymethyl or benzhydrylidene group, optionally substitut

Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3 and R4 groups is hydroxy, and the others are each hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a nitrogen atom, or pharmaceutically acceptable salts thereof formed with acids or bases.