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21. 发明公开

EP2121653A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 有权
标题翻译：甲酰胺化合物和它们作为钙蛋白酶抑制剂的用途
公开(公告)号：EP2121653A1
公开(公告)日：2009-11-25
申请号：EP07866322.6
申请日：2007-12-28
申请人： Abbott GmbH & Co. KG
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 R1, R2, R3a, R3b, 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, 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.

22. 发明公开

EP1716127A2 GUANIDINVERBINDUNGEN UND IHRE VERWENDUNG ALS BINDUNGSPARTNER FÜR 5-HT5-REZEPTOREN 有权
标题翻译： GUIDIDINVERBINDUNGEN UND IHRE VERWENDUNG ALS BINDUNGSPARTNERFÜR5-HT5-REZEPTOREN
公开(公告)号：EP1716127A2
公开(公告)日：2006-11-02
申请号：EP05707406.4
申请日：2005-02-15
申请人： Abbott GmbH & Co. KG
发明人： NETZ, Astrid , AMBERG, Wilhelm , LANGE, Udo , OCHSE, Michael , HUTCHINS, Charles, W. , GARCIA-LADONA, Francisco-Xavier , WERNET, Wolfgang , KLING, Andreas
IPC分类号： C07D277/48 , C07D417/04 , C07D277/82 , C07D285/12 , C07D285/08 , C07D249/14 , C07D237/22 , C07D231/56 , C07D263/28 , C07D261/14 , A61K31/425
CPC分类号： C07D277/48 , C07D231/56 , C07D235/30 , C07D237/22 , C07D249/14 , C07D261/14 , C07D263/28 , C07D263/48 , C07D277/60 , C07D277/82 , C07D285/08 , C07D285/135 , C07D333/36 , C07D417/04 , C07D417/12 , C07D513/04
摘要： The invention relates to guanidine compounds of general formula (I), corresponding enantiomeric, diastereomeric, and/or tautomeric forms thereof, and pharmaceutically acceptable salts thereof. The invention further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors in order to treat diseases modulated by 5-HT5 receptor activity, especially treat neurodegenerative and neuropsychiatric disorders and the signs, symptoms, and malfunctions associated therewith.
摘要翻译：胍化合物（I），它们的对映异构体，非对映体和/或互变异构体和盐是新的。式（I）的胍化合物，其对映异构体，非对映异构体和/或互变异构体和盐是新的。 Q-N（R 2） - C（= NR 3） - N（R 1） - Z-W（I）W：取代的苯基或噻吩基; Z： - （CR 1> zR 2> z）a-（V z）b-（CR 3> zR 4> z）c-; a和c：0-4; b：0或1，a，b和c的和= 1-5; R 1> z至R 4> z：氢，卤素，羟基，1-6C烷基，2-6C烯基或炔基，1-6C亚烷基（3-7C）环烷基，3-7C环烷基，（杂）芳基， -4C亚烷基（杂）芳基或R 1> z / R 2> z和/或R 3> z / R 4> z一起完成3-7元任选取代的（未）饱和碳 - 或杂环基，含有多达3个杂原子（O，N或S）; V z：CO，CONR 5> z，NR 5> zCO，O，S，SO，SO 2，SO 2 NR 5> z，NR 5> zSO 2，CS，CSNR 5> z，NR 5> zCS， OCS，COO，OCO，O，亚乙烯基，C（= CR 6）z R 7 z），CR 6> z = CR 7> z，NR 5> zCONR 5>，OCONR 5> z或NR 5> z; R 1> -R 3>：氢或取代基; Q：二取代的5元杂芳基。 “定义（完全定义）”字段中给出了完整的定义。活动：反义词神经保护; 精神药物; 脑保护; 镇惊; 抗精神病药; 安神; 抗抑郁药; 抑制细胞生长; 止痛; 解酒。没有给出这些活动的测试细节。作用机制：5-羟色胺（5HT）5类受体非竞争性抑制剂。（I）结合5-羟色胺（5HT）5类受体作为非竞争性抑制剂，因此（最终）细胞内钙离子浓度的增加。化合物N-（2-甲氧基苄基）-N' - （1,3-噻唑-2-基）胍（Ia）对于低于50nM的人5-HT 5受体具有结合亲和力（抑制常数）。

23. 发明公开

EP1572698A1 3-SUBSTITUIERTE 3,4-DIHYDRO-THIENO[2,3-D]PYRIMIDIN-4-ONE-DERIVATE, IHRE HERSTELLUNG UND VERWENDUNG 有权
标题翻译： 3-取代的-3,4-二氢THIENO¬2,3-D嘧啶-4-酮衍生物，其生产和使用
公开(公告)号：EP1572698A1
公开(公告)日：2005-09-14
申请号：EP03813137.1
申请日：2003-12-17
申请人： Abbott GmbH & Co. KG
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 , A61K31/519 , A61P25/00
CPC分类号： C07D495/14
摘要： The invention relates to 3,4-dihydro-thieno[2,3-d]pyrimidinde-4-one-derivatives which are substituted at 3-position with 5-membered heteroaryl which can be condensed with an aryl or heteroaryl radical. The heteroaryl and, optionally, the condensed aryl or heteroaryl radical 1,2 or 3 can independently include selected substitutents from C1-5-alkyl, C1-5-alkoxy, C1-5-alkylthio, halogen, CN, halogen-C1-5-alkyl, halogen-C1-5alkoxy, hydroxy, -NH2, -N(R6)2, -NH(R6), aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl, the substituents aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl 1,2 or 3 independently include selected substituents from C1-5-alkythio, halogen, CN, halogen-C1-5-alkyl, halogen-C1-5alkoxy, hydroxy, -NH2, -N(R6)2 and -NH(R6). The invention also relates to the production and use of said derivatives, especially for therapeutical purposes, e.g. in the treatment of depression.

24. 发明授权

EP0866800B1 ANTINEOPLASTIC PEPTIDES 失效
标题翻译： ANTINEOPLASTISCHE PEPTIDE
公开(公告)号：EP0866800B1
公开(公告)日：2004-09-22
申请号：EP96943076.8
申请日：1996-12-11
申请人： Abbott GmbH & Co. KG
发明人： AMBERG, Wilhelm , BARLOZZARI, Teresa , BERNARD, Harald , BUSCHMANN, Ernst , HAUPT, Andreas , HEGE, Hans-Guenther , JANSSEN, Bernd , KLING, Andreas , LIETZ, Helmut , RITTER, Kurt , ULLRICH, Martina , WEYMANN, Jürgen , ZIERKE, Thomas
IPC分类号： C07K7/06 , A61K38/08 , C07K1/00
CPC分类号： A61K38/08

25. 发明公开

EP2516415A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS IV 有权
标题翻译：甲酰胺化合物和它们作为钙蛋白酶抑制剂IV使用
公开(公告)号：EP2516415A1
公开(公告)日：2012-10-31
申请号：EP10798323.1
申请日：2010-12-21
申请人： Abbott GmbH & Co. KG , Abbott Laboratories
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.

26. 发明公开

EP2516393A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 有权
标题翻译：甲酰胺化合物及其作为钙蛋白酶抑制剂
公开(公告)号：EP2516393A1
公开(公告)日：2012-10-31
申请号：EP10795007.3
申请日：2010-12-21
申请人： Abbott GmbH & Co. KG , Abbott Laboratories
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.

27. 发明公开

EP2427429A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 有权
标题翻译：羧甲酰胺化合物及其作为CALPAIN抑制剂的用途
公开(公告)号：EP2427429A1
公开(公告)日：2012-03-14
申请号：EP10715905.5
申请日：2010-05-06
申请人： Abbott GmbH & Co. KG
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：本发明涉及新型羧酰胺化合物及其用于制造药物的用途。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）。本发明因此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病症的用途。羧酰胺化合物是其中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提及的含义的通式（I）的化合物，其互变异构体及其药学上合适的盐。特别地，所述化合物具有通式（Ia）和（Ib），其中R 1，r，R 2b，R 3a，R 3b，R 4，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是部分CH 2 -CH 2，CH 2 -CH 2 -CH 2，N（R y＃）-CH 2，N（R y＃） - CH 2 -CH 2或CH = CH-CH =，各自任选具有1个或2个H原子被相同或不同的基团R y取代，其中R y和R y＃具有权利要求中提及的含义。

28. 发明授权

EP1169338B1 NIEDERMOLEKULARE INHIBITOREN VON KOMPLEMENTPROTEASEN 有权
标题翻译：低分子抑制剂KOMPLEMENTPROTEASEN
公开(公告)号：EP1169338B1
公开(公告)日：2004-11-03
申请号：EP00920597.2
申请日：2000-03-28
申请人： Abbott GmbH & Co. KG
发明人： HILLEN, Heinz , SCHMIDT, Martin , MACK, Helmut , SEITZ, Werner , HAUPT, Andreas , ZECHEL, Johann-Christian , KLING, Andreas
IPC分类号： C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07D409/12 , A61K38/55 , A61P7/02 , C07K5/06
CPC分类号： C07D401/12 , A61K38/00 , C07B43/00 , C07K5/06078

29. 发明授权

EP2238130B1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 有权
标题翻译：羧酸酰胺化合物和它们作为钙蛋白酶抑制剂的用途
公开(公告)号：EP2238130B1
公开(公告)日：2012-05-02
申请号：EP08866203.6
申请日：2008-12-29
申请人： Abbott GmbH & Co. KG
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.

30. 发明公开

EP2398783A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 审中-公开
标题翻译：羧酸酰胺化合物和它们作为钙蛋白酶抑制剂的用途
公开(公告)号：EP2398783A1
公开(公告)日：2011-12-28
申请号：EP10704572.6
申请日：2010-02-19
申请人： Abbott GmbH & Co. KG , 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.

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