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53 条记录 (耗时 0.049 秒)

    4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS
    3.
    发明申请
    4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS 审中-公开
    4-（4-吡啶基） - 苯甲酸酯及其作为岩石活性调节剂的用途

    公开(公告)号：US20150105386A1

    公开(公告)日：2015-04-16

    申请号：US14523296

    申请日：2014-10-24

    申请人： AbbVie Deutschland GmbH & Co KG ,  AbbVie Inc.

    发明人： Helmut Mack ,  Nicole Teusch ,  Bernhard K. Muller ,  Wilfried Hornberger ,  Michael F. Jarvis ,  Daryl Sauer ,  Steven L. Swann, Jr. ,  Dominique Bonafoux ,  Ryan Keddy ,  Adrian Donald Hobson ,  Anil Vasudevan

    IPC分类号： C07D401/12 ,  C07D213/56

    CPC分类号： C07D401/12 ,  C07D213/56 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

    摘要： The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs). R1 and R2 are, independently of each other, hydrogen, hydroxy, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-haloalkoxy; R3, R4, R5 and R6 are, independently of each other, hydrogen, hydroxy, halogen, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy, C1-C8-haloalkoxy, amino, C1-C8-alkylamino or di-(C1-C8-alkyl)-amino; R7 is hydrogen, C1-C8-alkyl, C1-C8-haloalkyl, aryl or aryl-C1-C8-alkyl; R8 is a group of the formula —X—W, where X is a single bond, C1-C4-alkylene or C1-C4-alkylene-O—, where the alkylene group in the three last-mentioned radicals may be linear or branched and may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or may be interrupted by an oxygen atom; and W is a cyclic radical selected from phenyl and a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring which contains as ring members 1, 2 or 3 heteroatoms selected O, S, and N and optionally 1 or 2 carbonyl groups; R9 is a group of the formula —Y—Z, where Z is hydrogen, halogen, OR11, NR12R13, S(O)m—R14, phenyl which may carry 1, 2, 3 or 4 substituents R15 or a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring; and Y is linear or branched C1C4-alkylene which may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or a phenyl ring; or, in case Z is phenyl or the 5- or 6-membered heterocyclic ring as defined above, Y can also be a single bond.

    摘要翻译： 本发明涉及式（I）的新型4-（4-吡啶基） - 苯甲酰胺。 化合物I具有有价值的治疗特性，特别适用于治疗对Rho激酶（ROCK）的调节作用的疾病。 R 1和R 2彼此独立地为氢，羟基，氰基，C 1 -C 8 - 烷基，C 1 -C 8 - 卤代烷基，C 1 -C 8 - 烷氧基或C 1 -C 8 - 卤代烷氧基; R3，R4，R5和R6彼此独立地为氢，羟基，卤素，氰基，C1-C8-烷基，C1-C8-卤代烷基，C1-C8-烷氧基，C1-C8-卤代烷氧基，氨基，C1- C 8 - 烷基氨基或二 - （C 1 -C 8 - 烷基） - 氨基; R 7是氢，C 1 -C 8 - 烷基，C 1 -C 8 - 卤代烷基，芳基或芳基-C 1 -C 8 - 烷基; R8是式-X-W的基团，其中X是单键，C1-C4-亚烷基或C1-C4-亚烷基-O-，其中三个最后提到的基团中的亚烷基可以是直链或支链 并且可以部分或完全卤化和/或可以被羟基取代和/或可以被氧原子中断; 并且W是选自苯基和5-或6-元饱和，部分不饱和或芳族杂环的环状基团，其包含作为环成员1,2或3的选自O，S和N的杂原子和任选的1或2个羰基 ; R 9是式-Y-Z的基团，其中Z是氢，卤素，OR 11，NR 12 R 13，S（O）m -R 14，可带有1,2,3或4个取代基R 15或5-或6的苯基 饱和的，部分不饱和的或芳族的杂环; Y是可部分或完全卤化和/或可被羟基和/或苯环取代的直链或支链C 1 -C 4亚烷基; 或者Z为苯基或上述5-或6-元杂环的情况下，Y也可以是单键。

    Carboxamide compounds and their use as calpain inhibitors
    7.
    发明授权
    Carboxamide compounds and their use as calpain inhibitors 有权
    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：US09567325B2

    公开(公告)日：2017-02-14

    申请号：US14522454

    申请日：2014-10-23

    申请人： AbbVie Deutschland GmbH & Co. KG ,  AbbVie Inc.

    发明人： Andreas Kling ,  Helmut Mack ,  Katja Jantos ,  Achim Moeller ,  Wilfried Hornberger ,  Charles W. Hutchins

    IPC分类号： C07D277/30 ,  C07D417/04 ,  C07D413/04 ,  C07D401/04

    CPC分类号： C07D417/04 ,  C07D277/30 ,  C07D401/04 ,  C07D413/04

    摘要： The present invention relates to novel carboxamide compounds and their use as 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 and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds.The carboxamide compounds are compounds of the general formula I in which W—R2 is selected from and R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw and Rw* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y1, Y2, Y3 and Y4 are CRy, or one or two of the variables Y1 to Y4 are a nitrogen atom and the remaining variables are CRy, wherein the radicals Ry may be identical or different and have the meanings mentioned in the claims.

    摘要翻译： 本发明涉及新的羧酰胺化合物及其作为药物的用途。 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钙蛋白酶活性升高相关的疾病的用途，以及通过施用有效量的这些羧酰胺化合物中的至少一种来进行治疗和/或预防性治疗的方法。 羧酰胺化合物是其中W-R2选自并且R 1，R 2，R 3a，R 3b，Y 1，Y 2，Y 3，Y 4，X，Q，m，k，Rw和Rw *具有通式I的化合物 权利要求中提及的其互变异构体及其药学上合适的盐。 在这些化合物中，优选其中Y1，Y2，Y3和Y4为CRy，或变量Y1至Y4中的一个或两个为氮原子，剩余的变量为CRy，其中基团Ry可以相同或不同，并且具有 意思是在权利要求中提及。

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS
    9.
    发明申请
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 有权
    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：US20150099786A1

    公开(公告)日：2015-04-09

    申请号：US14570996

    申请日：2014-12-15

    申请人： AbbVie Deutschland GmbH & Co. KG ,  AbbVie Inc.

    发明人： Helmut Mack ,  Andreas Kling ,  Katja Jantos ,  Achim Moeller ,  Wilfried Hornberger ,  Charles W. Hutchins

    IPC分类号： C07D417/12 ,  C07D213/81 ,  C07D401/06 ,  C07D211/78 ,  C07D233/32 ,  C07D401/12 ,  C07D207/28 ,  C07D275/03

    CPC分类号： C07D207/22 ,  C07D207/26 ,  C07D207/28 ,  C07D211/76 ,  C07D211/78 ,  C07D213/81 ,  C07D233/32 ,  C07D233/34 ,  C07D239/10 ,  C07D275/03 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

    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, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH2—CH2, CH2—CH2—CH2, N(Ry#)—CH2, N(Ry#)—CH2—CH2 or CH═CH—CH═, each optionally having 1 or 2 H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# have the meanings mentioned in the claims.

    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 3a，R 3b，R 4，Q，Y，A和X具有权利要求和说明书中所述的含义及其互变异构体及其药学上合适的盐。 特别地，化合物具有通式Ia和Ib，其中R1，r，R2b，R3a，R3b，R4，Y和X具有权利要求中提及的含义，包括其互变异构体及其药学上合适的盐。 在这些化合物中，优选其中Y为CH2-CH2，CH2-CH2-CH2，N（Ry＃）-CH2，N（Ry＃）-CH2-CH2或CH = CH-CH≡，各自任选具有1 或2个H原子被相同或不同的基团Ry取代，其中Ry和Ry＃具有权利要求中提及的含义。