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    TRIAZOLE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULAIONT OF THE DOPAMINE D3 RECEPTOR
    2.
    发明申请
    TRIAZOLE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULAIONT OF THE DOPAMINE D3 RECEPTOR 审中-公开
    适用于治疗多巴胺D3受体调节症状的三唑化合物

    公开(公告)号：WO2006058753A1

    公开(公告)日：2006-06-08

    申请号：PCT/EP2005/012856

    申请日：2005-12-01

    Applicant: ABBOTT GMBH & CO. KG ,  UNGER, Liliane ,  HAUPT, Andreas ,  BEYERBACH, Armin ,  DRESCHER, Karla ,  BRAJE, Wilfried ,  DARBYSHIRE, John ,  TURNER, Sean, C. ,  BACKFISCH, Gisela

    Inventor： UNGER, Liliane ,  HAUPT, Andreas ,  BEYERBACH, Armin ,  DRESCHER, Karla ,  BRAJE, Wilfried ,  DARBYSHIRE, John ,  TURNER, Sean, C. ,  BACKFISCH, Gisela

    IPC: A61K31/506 ,  C07D403/12 ,  A61P25/18

    CPC classification number: C07D403/12

    Abstract: The invention relates to compounds of formula (I), wherein n is 1 or 2, Ar is a C-bound 1,2,4-triazol radical which carries a radical R 1 on the remaining carbon atom and a radical R 1a on one of the nitrogen atoms; R 1 is hydrogen, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxymethyl, fluorinated C 1 -C 6 alkyl, fluorinated C 3 -C 6 cycloalkyl, fluorinated C 1 -C 4 alkoxymethyl, or optionally substituted phenyl or 5- or 6-membered heteroaryl; R 1a is hydrogen or C 1 -C 4 alkyl; and R 2 is C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, fluorinated C 1 -C 6 alkyl or fluorinated C 3 -C 6 cycloalkyl; and to the physiologically tolerated acid addition salts of there compounds. The invention also relates to a pharmaceuticaly composition that comprises at least one triazole compound of the formula (I) and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D 3 receptor antagonists or dopamine D 3 agonists, said method comprising administering an effective amount of at least one traizole compound or physiologically tolerated acid addition salt of the formula (I) to a subject in need thereof.

    Abstract translation: 本发明涉及式（I）化合物，其中n是1或2，Ar是在剩余的碳原子上带有自由基R 1的C结合的1,2,4-三唑基 和其中一个氮原子上的基团R 1a; R 1是氢，C 1 -C 6烷基，C 3 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， 氟化C 1 -C 6烷基，氟化C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， 氟化C 1 -C 4烷氧基甲基或任选取代的苯基或5-或6位的C 1 -C 6烷基， 杂芳基; R 1a是氢或C 1 -C 4烷基; R 2是C 1 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基， 氟化C 1 -C 6烷基或氟化C 3 -C 6环烷基; 以及该化合物的生理耐受酸加成盐。 本发明还涉及包含至少一种式（I）的三唑化合物和/或其至少一种生理上耐受的酸加成盐的药物组合物，还涉及治疗有益于多巴胺D 3受体拮抗剂或多巴胺D 3激动剂，所述方法包括给受试者施用有效量的式（I）化合物或生理学耐受的酸加成盐， 需要。

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS
    5.
    发明申请
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 审中-公开
    羧酰胺化合物及其作为钙蛋白酶抑制剂的用途

    公开(公告)号：WO2011076811A1

    公开(公告)日：2011-06-30

    申请号：PCT/EP2010/070418

    申请日：2010-12-21

    Applicant: ABBOTT GMBH & CO. KG ,  ABBOTT LABORATORIES ,  KLING, Andreas ,  JANTOS, Katja ,  MACK, Helmut ,  MÖLLER, Achim ,  HORNBERGER, Wilfried ,  BACKFISCH, Gisela ,  LAO, Yanbin ,  NIJSEN, Marjoleen

    Inventor： KLING, Andreas ,  JANTOS, Katja ,  MACK, Helmut ,  MÖLLER, Achim ,  HORNBERGER, Wilfried ,  BACKFISCH, Gisela ,  LAO, Yanbin ,  NIJSEN, Marjoleen

    IPC: C07D207/28 ,  C07D401/04 ,  C07D401/14 ,  C07D417/14 ,  A61K31/4015 ,  A61K31/4439 ,  A61P25/28 ,  A61P27/08 ,  A61P35/00 ,  A61P13/12 ,  A61P31/00 ,  A61P31/18 ,  A61P25/00 ,  A61P9/00 ,  A61P21/00

    CPC classification number: C07D401/04 ,  C07D207/28 ,  C07D401/14 ,  C07D409/14 ,  C07D417/14

    Abstract: 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 R 1 , R 2 , R 3 R 4 , R 5 , 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 R 1 is optionally substituted phenyl-C 1 -C 2 -alkyl or hetaryl-C 1 -C 2 -alkyl, R 2 is optionally substituted aryl, hetaryl, aryl-C 1 -C 6 -alkyl, aryl-C 2 -C 6 -alkenyl or hetaryl-C 1 -C 4 -alkyl, R 3 is C 1 -C 3 -alkyl, C 1 -C 3 -haloalkyl, C 2 -C 4 -alkenyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl, or phenyl-C 1 -C 3 -alkyl, R 4 and R 5 independently of one another are halogen, CF 3 , CHF 2 , CH 2 F, C 1 -C 2 -alkyl or C 1 -C 2 -alkoxy, and m and n independently of one another are 0 or 1.

    Abstract translation: 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 1 -C 3 - 烷基，C 1 -C 3 - 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烷基或苯基 - C 1 -C 3 - 烷基，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。

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V
    7.
    发明申请
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V 审中-公开
    羧酰胺化合物及其作为钙抑制剂V

    公开(公告)号：WO2012076639A1

    公开(公告)日：2012-06-14

    申请号：PCT/EP2011/072164

    申请日：2011-12-08

    Applicant: ABBOTT GMBH & CO. KG ,  ABBOTT LABORATORIES ,  KLING, Andreas ,  JANTOS, Katja ,  MACK, Helmut ,  MÖLLER, Achim ,  HORNBERGER, Wilfried ,  LAO, Yanbin ,  BACKFISCH, Gisela ,  NIJSEN, Marjoleen

    Inventor： KLING, Andreas ,  JANTOS, Katja ,  MACK, Helmut ,  MÖLLER, Achim ,  HORNBERGER, Wilfried ,  LAO, Yanbin ,  BACKFISCH, Gisela ,  NIJSEN, Marjoleen

    IPC: A61K31/4439 ,  C07D401/04 ,  A61P25/28

    CPC classification number: C07D401/04 ,  A61K31/4439 ,  C07D401/14 ,  Y02A50/411

    Abstract: 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 R 1 , R 2 , R 3 R 4 , 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 R 1 is optionally substituted benzyl or hetaryl-methyl, X is a single bond or an oxygen atom, R 2 is C 1 -C 4 - alkyl, C 1 -C 4 -haloalkyl, C 2 -C 4 -alkenyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl, C 3 -C 6 -heterocycloalkyl-C 1 -C 2 -alkyl, phenyl, phenyl-C 1 -C 3 -alkyl, pyridin-2-yl-C 1 -C 3 -alkyl or CH 2 -C(O)OCH 3 ,R 3 and R 4 independently of one another are halogen, CN, CF 3 , CHF 2 , CH 2 F, C 1 -C 2 -alkyl or C 1 -C 2 -alkoxy, and m and n independently of one another are 0 or 1.

    Abstract translation: 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。

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS IV
    8.
    发明申请
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS IV 审中-公开
    羧酰胺化合物及其作为抑制剂的用途IV

    公开(公告)号：WO2011076812A1

    公开(公告)日：2011-06-30

    申请号：PCT/EP2010/070420

    申请日：2010-12-21

    Applicant: ABBOTT GMBH & CO. KG ,  ABBOTT LABORATORIES ,  KLING, Andreas ,  JANTOS, Katja ,  MACK, Helmut ,  MÖLLER, Achim ,  HORNBERGER, Wilfried ,  BACKFISCH, Gisela ,  LAO, Yanbin ,  NIJSEN, Marjoleen

    Inventor： KLING, Andreas ,  JANTOS, Katja ,  MACK, Helmut ,  MÖLLER, Achim ,  HORNBERGER, Wilfried ,  BACKFISCH, Gisela ,  LAO, Yanbin ,  NIJSEN, Marjoleen

    IPC: C07D401/04 ,  A61K31/4439 ,  A61P25/00

    CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D413/14

    Abstract: 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 R 1 , R 2 , R 3 R 4 , R 5 ,, 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 R 1 is optionally substituted phenyl-C 1 -C 2 -alkyl or hetaryl-C 1 -C 2 -alkyl, R 2 is optionally substituted aryl, hetaryl, aryl-C 1 -C 6 -alkyl, aryl-C 2 -C 6 -alkenyl or hetaryl-C 1 -C 4 -alkyl, R 3 is C 3 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 2 -C 4 -alkenyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl, C 3 -C 6 - heterocycloalkyl-C 1 -C 2 -alkyl, phenyl-C 1 -C 3 -alkyl, pyridin-2-yl-C 1 -C 3 -alkyl or 1,3- benzoxazol-2-yl-methyl, R 4 and R 5 independently of one another are halogen, CF 3 , CHF 2 , CH 2 F, C 1 -C 2 -alkyl or C 1 -C 2 -alkoxy, and m and n independently of one another are 0 or 1.

    Abstract translation: 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具有权利要求书和说明书中所述的含义，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-C1-C3-烷基或1,3-苯并恶唑-2-基 - 甲基，R4和R5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。

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