OXINDOLE COMPOUNDS CARRYING A NITROGEN-BOUND SPIRO SUBSTITUENT AND USE THEREOF FOR TREATING VASOPRESSIN-RELATED DISEASES
    5.
    发明公开
    OXINDOLE COMPOUNDS CARRYING A NITROGEN-BOUND SPIRO SUBSTITUENT AND USE THEREOF FOR TREATING VASOPRESSIN-RELATED DISEASES 审中-公开
    用氮氧化物结合态螺取代基和其用于疾病介导加压素治疗的羟吲哚衍生物

    公开(公告)号:EP3143024A1

    公开(公告)日:2017-03-22

    申请号:EP15724210.8

    申请日:2015-05-15

    摘要: The present invention also relates to pharmaceutical compositions comprising the novel substituted oxindole derivatives of the formula I, and to their use for the treatment of vasopressin-related disorders.

    摘要翻译: 本发明涉及下式的新的羟吲哚substituiertem衍生物我worin A是选自苯基和6-元杂芳基含有1个或2个氮原子作为环成员,其中环A带有一个取代基R 6和R 7任选的一种取代基的环; B是选自苯基和单环或双环杂芳环含有选自O,N和S的作为环成员,其中环B可以带有1,2或3个取代基R 8 1,2或3个杂原子的环; ,-CH2CH2 - ,--CH.sub.2O-- - X1,X2,X3和X4,海誓山盟unabhängig,从-CH 2 - , - O-,-S(O)C - , - NH-,-C(O)中选择 ,-OCH 2,-S(O)CCH 2 - , - CH 2 S(O)C-,CH 2 NH-,-NHCH 2 - , - CH 2 C(O) - 和C(O)CH 2 - ; X5是NH,CH 2或O; 和c。其中,R1 R2(R3)一,(R 4)B,R5,R6,R7和R8是如权利要求中所定义。 因此,本发明涉及药物组合物,包含式I的新颖substituiertem的羟吲哚衍生物I,及其用于加压素相关的病症的治疗中使用

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V
    9.
    发明授权
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V 有权
    CARBOXAMIDVERBINDUNGEN UND IHRE VERWENDUNG ALS CALPAIN-HEMMER V

    公开(公告)号:EP2648731B1

    公开(公告)日:2017-01-25

    申请号:EP11796664.8

    申请日:2011-12-08

    摘要: 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, X, 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 benzyl or hetaryl-methyl, X is a single bond or an oxygen atom, R2 is C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6-heterocycloalkyl-C1-C2-alkyl, phenyl, phenyl-C1-C3-alkyl, pyridin-2-yl-C1-C3-alkyl or CH2—C(O)OCH3, R3 and R4 independently of one another are halogen, CN, CF3, CHF2, CH2F, C1-C2-alkyl or C1-C2-alkoxy, and m and n independently of one another are 0 or 1.

    摘要翻译: 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,X,m和n具有权利要求书和说明书中所述的含义,其互变异构体,其水合物和药学上合适的盐 它们。 在这些化合物中,优选其中R 1为任选取代的苄基或杂芳基 - 甲基,X为单键或氧原子,R 2为C 1 -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,苯基-C 1 -C 3烷基,吡啶-2-基-C 1 -C 3 - 烷基或CH 2 -C(O)OCH 3,R 3和R 4彼此独立地是卤素,CN,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。

    NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
    10.
    发明公开
    NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
    NEUARTIGE INHIBITORVERBINDUNGEN DER PHOSPHODIESTERASE TYP 10A

    公开(公告)号:EP2970328A1

    公开(公告)日:2016-01-20

    申请号:EP14709320.7

    申请日:2014-03-12

    CPC分类号: C07D495/04

    摘要: The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: (I). In formula I the variables X
    1 is CH or N, X
    2 is O or S and where R
    1 , R
    2 , R
    3 , R
    4 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

    摘要翻译: 本发明涉及式I化合物,N-氧化物,互变异构体,前药及其药学上可接受的盐:在式I中,变量X1是CH或N,X2是O或S,并且其中R1,R2,R3 R4和Q如权利要求中所定义。 式I化合物,N-氧化物,互变异构体,其前药和药学上可接受的盐是10A型磷酸二酯酶的抑制剂。 因此,本发明还涉及式I化合物,N-氧化物,互变异构体,前药和其药学上可接受的盐在制备药物中的用途,因此其适用于治疗或控制医学病症 选自神经障碍和精神障碍,用于改善与这种障碍相关的症状并降低这种障碍的风险。