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115 条记录 (耗时 0.061 秒)

    Carboxamide compounds and their use as calpain inhibitors
    32.
    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：US07799809B2

    公开(公告)日：2010-09-21

    申请号：US12072065

    申请日：2008-02-22

    申请人： Andreas Kling ,  Wilfried Hornberger ,  Helmut Mack ,  Achim Moeller ,  Volker Nimmrich ,  Dietmar Seemann ,  Wilfried Lubisch

    发明人： Andreas Kling ,  Wilfried Hornberger ,  Helmut Mack ,  Achim Moeller ,  Volker Nimmrich ,  Dietmar Seemann ,  Wilfried Lubisch

    IPC分类号： A61K31/44 ,  C07D221/18 ,  C07D401/00

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D491/048 ,  C07D493/04 ,  C07D513/04

    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, W, Y 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 I-A.a′ and I-A.a″ in which m, E, R1, R3a, R3b, R2, Ry, Rw and Rw6* have the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.

    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R1，R2，R3a，R3b，W，Y和X具有权利要求书和说明书中所述的含义，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.a'和IA.a“，其中m，E，R1，R3a，R3b，R2，Ry，Rw和Rw6 *具有权利要求中提及的含义，n为0， 1或2，其互变异构体及其药学上合适的盐。

    Carboxamide compounds and their use as calpain inhibitors IV
    33.
    发明授权
    Carboxamide compounds and their use as calpain inhibitors IV 有权
    羧甲酰胺化合物及其作为钙蛋白酶抑制剂的用途

    公开(公告)号：US08598211B2

    公开(公告)日：2013-12-03

    申请号：US12972679

    申请日：2010-12-20

    申请人： Andreas Kling ,  Katja Jantos ,  Helmut Mack ,  Achim Möller ,  Wilfried Hornberger ,  Gisela Backfisch ,  Yanbin Lao ,  Marjoleen Nijsen

    发明人： Andreas Kling ,  Katja Jantos ,  Helmut Mack ,  Achim Möller ,  Wilfried Hornberger ,  Gisela Backfisch ,  Yanbin Lao ,  Marjoleen Nijsen

    IPC分类号： A61K31/4439 ,  C07D401/04

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14

    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, 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.

    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，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。

    LOW-MOLECULAR SERINE PROTEASES INHIBITORS COMPRISING POLYHYDROXY-ALKYL AND POLYHYDROXY-CYCLOALKYL RADICALS
    34.
    发明申请
    LOW-MOLECULAR SERINE PROTEASES INHIBITORS COMPRISING POLYHYDROXY-ALKYL AND POLYHYDROXY-CYCLOALKYL RADICALS 审中-公开
    包含聚羟基 - 烷基和聚羟基 - 环烷基基团的低分子丝氨酸蛋白酶抑制剂

    公开(公告)号：US20120190832A1

    公开(公告)日：2012-07-26

    申请号：US13277829

    申请日：2011-10-20

    申请人： Dieter Herr ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger

    发明人： Dieter Herr ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger

    IPC分类号： C07H15/26

    CPC分类号： A61K31/155 ,  C07H7/00 ,  C07H15/00

    摘要： The invention relates to novel amidines and quanidines, the production and use thereof and the use thereof as trypsine-type serine protease competitive inhibitors, especially thrombine and compliment proteases CIs and C1r. The invention also relates to pharmaceutical compositions which contain said compounds as active ingredients, in addition to the use of the compounds as thrombine inhibitors, anticoagulants, compliment inhibitors and anti-inflammatory agents. The novel compositions are characterised by the linkage of a serine protease inhibitor having amidine or guanidine functions with an alkyl radical having two or more hydroxyl functions, whereby said alkyl radical is derived from sugar derivates. Several sugar structural components or components derived from sugar can therefore be linked to each other. Said principle of linking sugar derivates enables oral active compounds to be obtained.

    摘要翻译： 本发明涉及新型脒和喹啉，其生产及其用途及其作为胰蛋白酶型丝氨酸蛋白酶竞争性抑制剂的用途，特别是血栓素和补体蛋白酶CI和C1r。 除了使用化合物作为血栓抑制剂，抗凝剂，补体抑制剂和抗炎剂之外，本发明还涉及含有所述化合物作为活性成分的药物组合物。 该新型组合物的特征在于具有脒或胍功能的丝氨酸蛋白酶抑制剂与具有两个或多个羟基官能团的烷基基团的连接，其中所述烷基衍生自糖衍生物。 因此，几种糖结构成分或来自糖的组分可以彼此连接。 所述连接糖衍生物的原理使得能够获得口服活性化合物。

    4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS
    38.
    发明申请
    4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS 有权
    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：US20100273828A1

    公开(公告)日：2010-10-28

    申请号：US12675430

    申请日：2008-08-26

    申请人： Helmut Mack ,  Nicole Teusch ,  Bernhard K. Müller ,  Wilfried Hornberger ,  Michael F. Jarvis ,  Daryl Sauer ,  Steve Swann, JR. ,  Anil Vasudevan

    发明人： Helmut Mack ,  Nicole Teusch ,  Bernhard K. Müller ,  Wilfried Hornberger ,  Michael F. Jarvis ,  Daryl Sauer ,  Steve Swann, JR. ,  Anil Vasudevan

    IPC分类号： A61K31/4545 ,  A61K31/444 ,  A61K31/4439 ,  A61K31/44 ,  C07D401/02 ,  C07D213/56 ,  A61P25/16 ,  A61K9/00 ,  A61P35/00 ,  A61P11/06 ,  A61P25/00 ,  A61P25/28

    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 from 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，其含有作为环成员1,2或3的选自O，S和N的杂原子以及任选的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。