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    • 6. 发明申请
    • Pyrimidin-2-one compounds and their use as dopamine d3 receptor ligands
    • 嘧啶-2-酮化合物及其作为多巴胺d3受体配体的用途
    • US20060235004A1
    • 2006-10-19
    • US10548931
    • 2004-03-12
    • Herve GenesteAndreas KlingWilfried BrajeAndreas HauptLillian Unger
    • Herve GenesteAndreas KlingWilfried BrajeAndreas HauptLillian Unger
    • A61K31/551A61K31/513C07D403/14C07D413/14C07D417/14
    • C07D239/36C07D239/52C07D239/54C07D239/553C07D239/56C07D401/12C07D403/14C07D405/14C07D409/14
    • The invention relates to pyrimidin 2-one compounds of general formula (I), in addition to the derivatives and tautomers of (I) and the physiologically acceptable salts of said compounds. In said formula, A represents linear or branched C3-C6 alkene, which can have a double bond or triple bond and/or a group Z, which is not adjacent to the nitrogen atom of the pyrimidinone ring and is selected from O, S, C(O), NR3, C(O)NR3, NR3C(O), OC(O) and C(O)O; B represents a group of the formula (II), in which X stands for CH2 or N and Y stands for CH2 or CH2CH2, or X—Y can also jointly represent C═CH, C═CH—CH2 or CH—CH═CH; R1 and R2 are defined as cited in the description and the claims; and Ar represents an optionally substituted aromatic group. The invention also relates to a pharmaceutical agent, containing at least one compound (I) and the tautomers, derivatives and/or acid addition salts of said compound, optionally together with physiologically acceptable carriers and/or auxiliary agents. The invention also relates to the use of compounds of formula (I), and their tautomers, derivatives and pharmacologically acceptable acid addition salts for producing a phrmaceutical agent for treating diseases which respond to the influence of dopamine D3 receptor ligands.
    • 除了(I)的衍生物和互变异构体以及所述化合物的生理学上可接受的盐之外,本发明涉及通式(I)的嘧啶-2-酮化合物。 在所述式中,A表示可以具有双键或三键和/或不相邻的基团Z的直链或支链C 3 -C 6亚烷基 选自O,S,C(O),NR 3,C(O)NR 3,NR 3, C(O),OC(O)和C(O)O; B表示式(II)的基团,其中X代表CH 2或N,Y代表CH 2或CH 2, CH 2或XY也可以共同表示C-CH,C-CH-CH 2 CH或CH-CH-CH; R 1和R 2定义如说明书和权利要求书中所引用的; 并且Ar表示任选取代的芳族基团。 本发明还涉及含有至少一种化合物(I)和所述化合物的互变异构体,衍生物和/或酸加成盐,任选地与生理上可接受的载体和/或辅助剂一起的药剂。 本发明还涉及式(I)化合物及其互变异构体,衍生物和药理学上可接受的酸加成盐的用途,用于制备用于治疗对多巴胺D 3的影响作出反应的疾病的药物制剂 受体配体。
    • 7. 发明申请
    • CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS IV
    • 羧酰胺化合物及其作为抑制剂的用途IV
    • US20110152325A1
    • 2011-06-23
    • US12972679
    • 2010-12-20
    • Andreas KlingKatja JantosHelmut MackAchim MöllerWilfried HornbergerGisela BackfischYanbin LaoMarjoleen Nijsen
    • Andreas KlingKatja JantosHelmut MackAchim MöllerWilfried HornbergerGisela BackfischYanbin LaoMarjoleen Nijsen
    • A61K31/4439C07D401/04A61P25/28A61P25/00A61P25/08A61P25/04A61P13/12A61P35/00A61P31/18A61P37/02A61P33/06
    • C07D401/04C07D401/14C07D413/14
    • The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.The carboxamide compounds are compounds of the general formula I in which R1, R2, R3 R4, R5, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R1 is optionally substituted phenyl-C1-C2-alkyl or hetaryl-C1-C2-alkyl, R2 is optionally substituted aryl, hetaryl, aryl-C1-C6-alkyl, aryl-C2-C6-alkenyl or hetaryl-C1-C4-alkyl, R3 is C3-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6-heterocycloalkyl-C1-C2-alkyl, phenyl-C1-C3-alkyl, pyridin-2-yl-C1-C3-alkyl or 1,3-benzoxazol-2-yl-methyl, R4 and R5 independently of one another are halogen, CF3, CHF2, CH2F, C1-C2-alkyl or C1-C2-alkoxy, and m and n independently of one another are 0 or 1.
    • 本发明涉及新的羧酰胺化合物及其用于制备药物的用途。 羧酰胺化合物是钙蛋白酶(钙依赖性半胱氨酸蛋白酶)的抑制剂。 因此,本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。 羧酰胺化合物是通式I的化合物,其中R 1,R 2,R 3,R 4,R 5,m和n具有权利要求书和描述中所述的含义,其互变异构体,其水合物及其药学上合适的盐。 在这些化合物中,优选其中R 1为任选取代的苯基-C 1 -C 2 - 烷基或杂芳基-C 1 -C 2烷基,R 2为任选取代的芳基,杂芳基,芳基-C 1 -C 6 - 烷基,芳基-C 2 -C 6 - 烯基 或杂芳基-C 1 -C 4 - 烷基,R 3是C 3 -C 4 - 烷基,C 1 -C 4 - 卤代烷基,C 2 -C 4 - 烯基,C 3 -C 6 - 环烷基,C 3 -C 6 - 环烷基-C 1 -C 2烷基,C 3 -C 6 - 杂环烷基-C 1 -C 2 - 烷基,苯基-C 1 -C 3 - 烷基,吡啶-2-基-C 1 -C 3 - 烷基或1,3-苯并恶唑-2-基 - 甲基,R 4和R 5彼此独立地是卤素 ,CF 3,CHF 2,CH 2 F,C 1 -C 2 - 烷基或C 1 -C 2 - 烷氧基,m和n彼此独立地为0或1。