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1. 发明申请

WO2004055024A1 3-SUBSTITUIERTE 3,4-DIHYDRO-THIENO[2,3-D]PYRIMIDIN-4-ON-DERIVATE, IHRE HERSTELLUNG UND VERWENDUNG 审中-公开
标题翻译： 3-取代的-3,4-二氢 - 噻吩并[2,3-d]嘧啶-4-酮衍生物，其生产和使用
公开(公告)号：WO2004055024A1
公开(公告)日：2004-07-01
申请号：PCT/EP2003/014423
申请日：2003-12-17
申请人： ABBOTT GMBH & CO. KG , BAKKER, Margaretha , HORNBERGER, Wilfried , KLING, Andreas , LANGE, Udo , MACK, Helmut , MOELLER, Achim , MUELLER, Reinhold , SCHELLHAAS, Kurt , SCHMIDT, Martin , STEINER, Gerd , WICKE, Karsten
发明人： BAKKER, Margaretha , HORNBERGER, Wilfried , KLING, Andreas , LANGE, Udo , MACK, Helmut , MOELLER, Achim , MUELLER, Reinhold , SCHELLHAAS, Kurt , SCHMIDT, Martin , STEINER, Gerd , WICKE, Karsten
IPC分类号： C07D495/14
CPC分类号： C07D495/14
摘要： Die erfindung betrifft 3,4-Dihydro-thieno[2,3-d]pyrimidin-4-on-Derivate, die in 3-Position mit 5-gliedrigem Heteroaryl substituierte sind, das mit einem Aryl- oder Heteroarylrest kondensiert sein kann, wobei das Heteroaryl und gegebenenfalls der kondensierte Aryl- oder Heteroarylrest 1,2 oder 3 unabhängig voneinander unter C 1-5 -Alkyl, C 1-5 -Alkoxy, C 1-5 -Alkylthio, Halogen, CN, Halogen-C 1-5 -alkyl, Halogen-C 1-5 alkoxy, Hydroxy, -NH 2, -N(R6) 2 , -NH(R6), Aryl, Aryloxy, Aralkyl, Aralkyloxy und Heteroaryl ausgewählte Substituenten tragen können, wobei die Substituenten Aryl, Aryloxy, Aralkyl, Aralkyloxy und Heteroaryl 1,2 oder 3 unabhängig voneinander unter C 1-5 -Alkythio, Halogen, CN, Halogen-C 1-5 -alkyl, Halogen-C 1-5 alkoxy, Hydroxy, -NH 2 , -N(R6) 2 und -NH(R6) ausgewählte Substituenten tragen können. Die Herstellung und Verwendung dieser Derivate, insbesondere zu therapeutischen Zwecken, z.B. bei der Behandlulng von Depressionen, werden ebenfalls beschrieben.
摘要翻译：本发明涉及3,4-二氢 - 噻吩并[2,3-d]嘧啶-4-酮衍生物，已被在其中可以与芳基稠合或杂芳基的5元杂芳基的3-位被取代，其中从C 1-5烷基，C 1-5 - 烷氧基，C 1-5 - 烷硫基，卤素，CN，卤代C 1-5烷基，卤素独立地选自杂芳基和任选稠合的芳基或杂芳基被1,2或3个取代基 C 1-5烷氧基，羟基，-NH 2，-N（R 6）2，-NH（R 6），芳基，芳氧基，芳烷基，芳烷氧基和杂芳基可以带有一个取代基中选择，其中取代基的芳基，芳氧基，芳烷基，芳烷氧基和杂芳基1， 2个或3个选自C 1-5 - 烷基硫基，卤素，CN，卤代C 1-5烷基，卤代C 1-5烷氧基，羟基，-NH 2，-N（R 6）2和-NH（R 6）独立地选择的取代基携带选自取代基可以。制备和使用这些衍生物的，并且特别是用于治疗目的，例如在抑郁症的Behandlulng，也有所说明。

2. 发明申请

WO2010094755A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 审中-公开
标题翻译：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：WO2010094755A1
公开(公告)日：2010-08-26
申请号：PCT/EP2010/052102
申请日：2010-02-19
申请人： ABBOTT GMBH & CO. KG , KLING, Andreas , MACK, Helmut , JANTOS, Katja , MOELLER, Achim , HORNBERGER, Wilfried , HUTCHINS, Charles, W. , ABBOTT LABORATORIES
发明人： KLING, Andreas , MACK, Helmut , JANTOS, Katja , MOELLER, Achim , HORNBERGER, Wilfried , HUTCHINS, Charles, W.
IPC分类号： C07D277/22 , C07D401/04 , C07D413/04 , C07D417/04 , A61K31/4439 , A61P25/00 , A61P35/00 , A61P31/18
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-R 2 is selected from formulae (1), (2) and (3) and R 1 , R 2 , R 3a , R 3b , Y 1 , Y 2 , Y 3 , Y 4 , X, Q, m, k, R w and R w* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y 1 , Y 2 , Y 3 and Y 4 are CR y , or one or two of the variables Y 1 to Y 4 are a nitrogen atom and the remaining variables are CR y , wherein the radicals Ry may be identical or different and have the meanings mentionend 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。羧酰胺化合物是通式（I）的化合物，其中W-R2选自式（1），（2）和（3），R1，R2，R3a，R3b，Y1，Y2，Y3，Y4，X ，Q，m，k，Rw和Rw *具有权利要求书中提及的含义，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。

3. 发明申请

WO2009083581A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 审中-公开
标题翻译：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：WO2009083581A1
公开(公告)日：2009-07-09
申请号：PCT/EP2008/068313
申请日：2008-12-29
申请人： ABBOTT GMBH & CO. KG , HORNBERGER, Wilfried , MACK, Helmut , KLING, Andreas , MOELLER, Achim , VOGG, Barbara , DELZER, Jürgen , BACKFISCH, Gisela , BEYERBACH, Armin
发明人： HORNBERGER, Wilfried , MACK, Helmut , KLING, Andreas , MOELLER, Achim , VOGG, Barbara , DELZER, Jürgen , BACKFISCH, Gisela , BEYERBACH, Armin
IPC分类号： C07D405/14 , C07D491/052 , A61K31/4439 , A61P25/00
CPC分类号： C07D405/14 , C07D491/052
摘要： The present invention relates to novel carboxamide compounds of the formula (I) and their use for the manufacture of a medicament. The carboxamide compounds are prodrugs of 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 the rest of the variables is as defined in the claims.
摘要翻译：本发明涉及式（I）的新型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抑制剂（钙依赖性半胱氨酸蛋白酶）的前药。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疾病的用途，其余变量如权利要求中所定义。

4. 发明申请

WO2010128102A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 审中-公开
标题翻译：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：WO2010128102A1
公开(公告)日：2010-11-11
申请号：PCT/EP2010/056166
申请日：2010-05-06
申请人： ABBOTT GMBH & CO. KG , MACK, Helmut , KLING, Andreas , JANTOS, Katja , MOELLER, Achim , HORNBERGER, Wilfried , HUTCHINS, Charles, W.
发明人： MACK, Helmut , KLING, Andreas , JANTOS, Katja , MOELLER, Achim , HORNBERGER, Wilfried , HUTCHINS, Charles, W.
IPC分类号： C07D207/26 , C07D211/76 , C07D233/34 , C07D239/10 , A61K31/4412
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 R 1 , R 2 , R 3a , R 3b , R 4 , 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 R 1 , r, R 2b , R 3a , R 3b , R 4 , 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 CH 2 -CH 2 , CH 2 -CH 2 -CH 2 , N(R y# )-CH2, N(R y# )-CH 2 -CH 2 or CH=CH-CH=, each optionally having 1 or 2 H-atoms replaced with identical or different radicals R y , wherein R y and R y# 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具有权利要求书和描述中所述的含义，其互变异构体和药学上合适的盐它们。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，包括其互变异构体和药学上合适的盐它们。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。

5. 发明申请

WO2008080969A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 审中-公开
标题翻译：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：WO2008080969A1
公开(公告)日：2008-07-10
申请号：PCT/EP2007/064617
申请日：2007-12-28
申请人： ABBOTT GMBH & CO. KG , KLING, Andreas , HORNBERGER, Wilfried , MACK, Helmut , MOELLER, Achim , NIMMRICH, Volker , SEEMANN, Dietmar , LUBISCH, Wilfried
发明人： KLING, Andreas , HORNBERGER, Wilfried , MACK, Helmut , MOELLER, Achim , NIMMRICH, Volker , SEEMANN, Dietmar , LUBISCH, Wilfried
IPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D493/04 , A61K31/4439 , A61P25/00
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 R 1 , R 2 , R 3a , R 3b , W, Y and X have the meanings mentioned in the claims and 15 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, R 1 , R 3a , R 3b , R 2 , R y , R w and R w6 * 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R 1，R 2，R 3，R 3，R 3b， W，Y和X具有权利要求书中提及的含义，和15的描述，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，R 1，R 3a，R 3b， R 2，R 2，R 2，W 2和R 6具有如下的含义：权利要求书，n为0,1或2，其互变异构体及其药学上合适的盐。

6. 发明申请

WO2012089828A2 HETEROCYCLIC COMPOUNDS AND THEIR USE AS GLYCOGEN SYNTHASE KINASE-3 INHIBITORS 审中-公开
标题翻译：杂环化合物及其作为糖原合成酶激酶-3抑制剂的用途
公开(公告)号：WO2012089828A2
公开(公告)日：2012-07-05
申请号：PCT/EP2011/074272
申请日：2011-12-30
申请人： ABBOTT GMBH & CO. KG , TURNER, Sean, Colm , MACK, Helmut , BAKKER, Margaretha, Henrica, Maria , VAN GAALEN, Marcel , HOFT, Carolin , HORNBERGER, Wilfried
发明人： TURNER, Sean, Colm , MACK, Helmut , BAKKER, Margaretha, Henrica, Maria , VAN GAALEN, Marcel , HOFT, Carolin , HORNBERGER, Wilfried
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , A61K31/4709 , A61P25/28 , A61P25/16
CPC分类号： C07D471/04 , A61P25/16 , A61P25/28 , C07D215/46 , C07D401/12 , C07D401/14 , C07D405/14
摘要： The present invention relates to novel heterocyclic compounds of formula (I), wherein the variables are as defined in the claims or the description, which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), compositions containing the compounds, their use for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a compound that modulates, preferably inhibits, the activity of glycogen synthase kinase 3β, and methods of treatment of medical disorders susceptible to treatment with a compound that modulates glycogen synthase kinase 3β activity using the compounds.
摘要翻译：本发明涉及式（I）的新型杂环化合物，其中各变量如权利要求或描述中所定义，其可用于抑制糖原合酶激酶3（GSK-3）含有这些化合物的组合物，它们在制备药物中的用途，所述药物用于治疗对用调节，优选抑制糖原合酶激酶3β的活性的化合物治疗敏感的医学病症，以及治疗对用使用该化合物调节糖原合酶激酶3β活性的化合物。

7. 发明申请

WO2011076811A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 审中-公开
标题翻译：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
申请人： ABBOTT GMBH & CO. KG , ABBOTT LABORATORIES , KLING, Andreas , JANTOS, Katja , MACK, Helmut , MÖLLER, Achim , HORNBERGER, Wilfried , BACKFISCH, Gisela , LAO, Yanbin , NIJSEN, Marjoleen
发明人： KLING, Andreas , JANTOS, Katja , MACK, Helmut , MÖLLER, Achim , HORNBERGER, Wilfried , BACKFISCH, Gisela , LAO, Yanbin , NIJSEN, Marjoleen
IPC分类号： 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分类号： C07D401/04 , C07D207/28 , C07D401/14 , C07D409/14 , C07D417/14
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 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.
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 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。

8. 发明申请

WO2012076639A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V 审中-公开
标题翻译：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
申请人： ABBOTT GMBH & CO. KG , ABBOTT LABORATORIES , KLING, Andreas , JANTOS, Katja , MACK, Helmut , MÖLLER, Achim , HORNBERGER, Wilfried , LAO, Yanbin , BACKFISCH, Gisela , NIJSEN, Marjoleen
发明人： KLING, Andreas , JANTOS, Katja , MACK, Helmut , MÖLLER, Achim , HORNBERGER, Wilfried , LAO, Yanbin , BACKFISCH, Gisela , NIJSEN, Marjoleen
IPC分类号： A61K31/4439 , C07D401/04 , A61P25/28
CPC分类号： C07D401/04 , A61K31/4439 , C07D401/14 , Y02A50/411
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 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.
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。

9. 发明申请

WO2011076812A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS IV 审中-公开
标题翻译：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
申请人： ABBOTT GMBH & CO. KG , ABBOTT LABORATORIES , KLING, Andreas , JANTOS, Katja , MACK, Helmut , MÖLLER, Achim , HORNBERGER, Wilfried , BACKFISCH, Gisela , LAO, Yanbin , NIJSEN, Marjoleen
发明人： KLING, Andreas , JANTOS, Katja , MACK, Helmut , MÖLLER, Achim , HORNBERGER, Wilfried , BACKFISCH, Gisela , LAO, Yanbin , NIJSEN, Marjoleen
IPC分类号： C07D401/04 , A61K31/4439 , A61P25/00
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 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.
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。

10. 发明申请

WO2009027392A1 4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS 审中-公开
标题翻译： 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：WO2009027392A1
公开(公告)日：2009-03-05
申请号：PCT/EP2008/061135
申请日：2008-08-26
申请人： ABBOTT GMBH & CO. KG , MACK, Helmut , TEUSCH, Nicole , MÜLLER, Bernhard K. , HORNBERGER, Wilfried , JARVIS, Michael F. , SAUER, Daryl
发明人： MACK, Helmut , TEUSCH, Nicole , MÜLLER, Bernhard K. , HORNBERGER, Wilfried , JARVIS, Michael F. , SAUER, Daryl
IPC分类号： C07D213/56 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , A61K31/44 , A61K31/4427 , A61P9/00 , A61P25/00 , A61P35/00 , A61P29/00
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). R 1 and R 2 are, independently of each other, hydrogen, hydroxy, cyano, C 1 -C 8 -alkyl, C 1 - C 8 -haloalkyl, C 1 -C 8 -alkoxy or C 1 -C 8 -haloalkoxy; R 3 , R 4 , R 5 and R 6 are, independently of each other, hydrogen, hydroxy, halogen, cyano, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -haloalkoxy, amino, C 1 -C 8 -alkylamino or di-(C 1 -C 8 -alkyl)-amino; R 7 is hydrogen, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, aryl or aryl-C 1 -C 8 -alkyl; R 8 is a group of the formula -X-W, where X is a single bond, C 1 -C 4 -alkylene or C 1 -C 4 -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; R 9 is a group of the formula -Y-Z, where Z is hydrogen, halogen, OR 11 , NR 12 R 13 , S(O) m -R 14 , phenyl which may carry 1, 2, 3 or 4 substituents R 15 or a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring; and Y is linear or branched C 1 C 4 -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-XW的基团，其中X是单键，C1-C4-亚烷基或C1-C4-亚烷基-O-，其中三个最后提及的基团中的亚烷基可以是直链或支链的，并且可以部分或完全卤化和/或可以被羟基取代和/或可被氧原子中断; 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的杂原子和任选的1或2个羰基 ; R9是式-YZ的基团，其中Z是氢，卤素，OR11，NR12R13，S（O）m -R14，可以携带1,2,3或4个取代基R15或5-或6-元的苯基饱和，部分不饱和或芳族杂环; 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。

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