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1. 发明授权

US08598211B2 Carboxamide compounds and their use as calpain inhibitors IV 有权
标题翻译：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。

2. 发明申请

US20100226915A1 AGER-Peptides and Use Thereof 有权
标题翻译： AGER-肽及其用途
公开(公告)号：US20100226915A1
公开(公告)日：2010-09-09
申请号：US11795282
申请日：2006-01-18
申请人： Alfred Hahn , Ralph Loebbert , Nicole Teusch , Achim Möller
发明人： Alfred Hahn , Ralph Loebbert , Nicole Teusch , Achim Möller
IPC分类号： A61K39/395 , C07K16/18 , G01N33/566 , A61K39/00 , A61K31/7088 , A61K38/43 , C12N15/63 , C12N1/00 , C12N5/16 , C12P21/06 , C07K14/00
CPC分类号： C07K16/2803 , A61K39/395 , A61K45/06 , A61K2039/505 , A61K2039/507 , C07K7/08 , C07K2317/24 , C12N15/85 , C12P21/005 , C12P21/02 , G01N33/564 , G01N33/566 , G01N2333/70503 , G01N2500/00
摘要： The present invention relates to the identification, functionality and use of domains from the N terminus of the receptor for Advanced Glycation End Products (AGER). These domains, called receptor mulitimerization epitope (RME), are highly conserved in all AGER protein sequences. They represent the mediators for AGER self-association and heteromerization with other proteins. The invention likewise relates to the identification, functionality and use of peptides derived from the C domain of AGER (AGER-CDP). The AGER RMEs and AGER-CDPs of the invention are suitable as target for identifying AGER ligands which modulate the natural ligand interaction; as immunogen for active or passive immunization of individuals, as diagnostic means for identifying immunogenic reactions, and as peptide ligands for modulating protein-protein interactions involving AGER.
摘要翻译：本发明涉及来自高级糖化终产物（AGER）的受体的N末端的结构域的鉴定，功能和用途。称为受体多聚表位（RME）的这些结构域在所有AGER蛋白质序列中都是高度保守的。它们代表AGER与其他蛋白质自身结合和异源化的介质。本发明同样涉及衍生自AGER（AGER-CDP）的C结构域的肽的鉴定，功能和用途。本发明的AGER RME和AGER-CDP适用于鉴定调节天然配体相互作用的AGER配体的靶标; 作为用于个体的主动或被动免疫的免疫原，作为用于鉴定免疫原性反应的诊断手段，以及用于调节涉及AGER的蛋白质 - 蛋白质相互作用的肽配体。

3. 发明授权

US06630493B1 Heterocyclically substituted amides, their preparation and use 有权
标题翻译：杂环取代的酰胺，其制备和用途
公开(公告)号：US06630493B1
公开(公告)日：2003-10-07
申请号：US09673087
申请日：2000-10-11
申请人： Wilfried Lubisch , Achim Möller , Hans-Jörg Treiber , Monika Knopp
发明人： Wilfried Lubisch , Achim Möller , Hans-Jörg Treiber , Monika Knopp
IPC分类号： A01N4340
CPC分类号： C07D213/82 , C07D233/90 , C07D239/28 , C07D239/30 , C07D277/56 , C07D401/04
摘要： Amides of the general formula I and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the meanings stated in the description, their preparation and use as calpain inhibitors.
摘要翻译：通式I的酰胺及其互变异构体和异构体形式，可能的对映异构体和非对映体形式，以及可能的生理上可耐受的盐，其中变量具有描述中所述的含义，其制备和用作钙蛋白酶抑制剂。

4. 发明授权

US06380220B1 Derivatives from piperidine-keto acid, their preparation and use 失效
标题翻译：衍生物来自哌啶酮酸，其制备和用途
公开(公告)号：US06380220B1
公开(公告)日：2002-04-30
申请号：US09284543
申请日：1999-04-15
申请人： Wilfried Lubisch , Achim Möller , Jürgen Delzer
发明人： Wilfried Lubisch , Achim Möller , Jürgen Delzer
IPC分类号： A61K31445
CPC分类号： C07D401/06 , C07D211/62 , C07D401/12
摘要： Piperidineketocarboxylic acid derivatives of the general formula I and their tautomeric and isomeric forms, and physiologically tolerable salts thereof, where the variables have the meanings given in the description, preparation of these compounds and their use as drugs.
摘要翻译：通式I的哌啶酮羧酸衍生物及其互变异构体和异构体形式及其生理上可耐受的盐，其中变量具有说明书中给出的含义，这些化合物的制备及其作为药物的用途。

5. 发明申请

US20120282423A1 Joined Veneer Strip 审中-公开
标题翻译：加盟单板带
公开(公告)号：US20120282423A1
公开(公告)日：2012-11-08
申请号：US13518880
申请日：2010-12-22
申请人： Achim Möller , Andreas Wagner
发明人： Achim Möller , Andreas Wagner
IPC分类号： B27D1/10 , B32B21/14 , B32B38/00 , B32B7/14 , B32B38/10 , B32B37/02
CPC分类号： B27D1/10 , B27D1/04 , B27D3/00 , B30B15/061 , Y10T156/1041 , Y10T156/1052 , Y10T156/12 , Y10T428/19
摘要： The invention relates to veneer strips made of individual veneer layers (1), wherein adjacent veneer layers overlap (7) and comprise a joint (4) having a wedge-shaped cross-section in the region of the overlapping. The veneer layers are connected to each other by means of adhesive. The invention further relates to a method, to a device for performing the method, and to a use of the veneer strips.
摘要翻译：本发明涉及由单独的单板层（1）制成的单板条，其中相邻的单板层重叠（7）并且包括在重叠区域中具有楔形横截面的接头（4）。薄板层通过粘合剂相互连接。本发明还涉及一种方法，一种用于执行该方法的装置以及该单板条的使用。

6. 发明授权

US06472587B1 PRODUCTION OF A 5-(2-CHLORO-4-(TRIFLUOROMETHYL)PHENOXY)-2-NITROBENZOIC ACID OR 7-CHLORO-3-METHYLLQUINOLINE-8-CARBOXYLIC ACID-TOLERANT PLANT BY EXPRESSING AN EXOGENOUS 5-(2-CHLORO-4-(TRIFLUOROMETHYL)PHENOXY)-2-NITROBENZOIC ACID OR 7-CHLORO-3-METHYLLQUINOLINE-8-CARBOXYLIC ACID-BINDING ANTIBODY IN THE PLANT 失效
标题翻译：除草剂结合多肽在植物中的表达以产生除草剂耐受性
公开(公告)号：US06472587B1
公开(公告)日：2002-10-29
申请号：US09381464
申请日：1999-09-21
申请人： Jens Lerchl , Achim Möller , Ralf-Michael Schmidt , Helmut Schiffer , Udo Rabe , Udo Conrad
发明人： Jens Lerchl , Achim Möller , Ralf-Michael Schmidt , Helmut Schiffer , Udo Rabe , Udo Conrad
IPC分类号： A01H500
CPC分类号： C07K16/44 , C07K2319/00 , C12N15/8209 , C12N15/8258 , C12N15/8274
摘要： Process for production of herbicide-tolerant plants by expressing an exogenous herbicide-binding polypeptide in plants or plant organs. The invention furthermore relates to the use of the corresponding nucleic acids which encode a polypeptide, an antibody or parts of an antibody with herbicide-binding properties in transgenic plants, and the thus transformed plant itself.
摘要翻译：通过在植物或植物器官中表达外源性除草剂结合多肽来生产除草剂耐受性植物的方法。本发明还涉及编码多肽，抗体或抗体在转基因植物中具有除草剂结合性质的抗体或部分的相应核酸的用途，以及由此转化的植物本身。

7. 发明授权

US06448254B1 Substituted amides, their production and their use 失效
标题翻译：取代酰胺，其生产和使用
公开(公告)号：US06448254B1
公开(公告)日：2002-09-10
申请号：US09647677
申请日：2000-10-03
申请人： Wilfried Lubisch , Achim Möller , Hans-Jörg Treiber , Monika Knopp
发明人： Wilfried Lubisch , Achim Möller , Hans-Jörg Treiber , Monika Knopp
IPC分类号： C07C31121
CPC分类号： C07D213/56 , C07C311/21 , C07D215/36 , C07D239/70 , C07D239/96
摘要： Amides of the general formula I and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the following meanings: R1 [sic] can be C1-C6-alkyl, phenyl, naphthyl, quinolyl, pyridyl, pyrimidyl, pyridazyl, quinazolyl and quinoxalyl, where the rings can additionally be substituted by up to 2 radicals R4 [sic], and R2 [sic] is —(CH2)m—R8 [sic], where R8 [sic] can be phenyl, cyclohexyl- or indolyl and m=1 to 6, and X is a bond, —CH2—, —CH2CH2—, —CH═CH—, —C≡C—, —CONH—, —SO2NH— [sic], and and [sic] R1—X [sic] together are also and R3 [sic] is hydrogen and CO—NR6R7 [sic], R4 [sic] is hydrogen, C1-C4-alkyl [sic], which is branched and unbranched, and —O—C1-C4-alkyl [sic]; R5 [sic] is hydrogen, C1-C4-alkyl [sic], which is branched or unbranched, and —O—C1-C4-alkyl [sic]; R6 [sic] is hydrogen, C1-C6-alkyl, which is branched and unbranched, and R7 [sic] is hydrogen, C1-C6-alkyl, which is branched or unbranched, and n is is [sic] a number 0, 1 or 2.
摘要翻译：通式I的酰胺及其互变异构体和异构体形式，可能的对映异构体和非对映体形式，以及可能的生理上可耐受的盐，其中变量具有以下含义：R 1 [C 1-6]可以是C 1 -C 6 - 烷基，苯基，萘基，喹啉基，吡啶基，嘧啶基，哒嗪基，喹唑啉基和喹喔啉基，其中环可以另外被至多2个基团R 4 [sic]取代，并且R 2是 - （CH 2）m -R 8 [sic]，其中R 8 [ ]可以是苯基，环己基或吲哚基并且m = 1至6，X是键，-CH 2 - ， - CH 2 CH 2 - ， - CH = CH - ， - C≡C - ， - CONH - ， - SO 2 NH- ]，并且R 1-X [sic]一起也是且R 3 [sic]是氢且CO-NR 6 R 7 [sic]，R 4 [sic]是氢，C 1 -C 4 - 烷基[ 非支链和-O-C 1 -C 4 - 烷基[sic]; R 5 [sic]是氢，C 1 -C 4 - 烷基[sic]，其是支链或非支链的，和-O-C 1 -C 4 - 烷基[ R 6是氢，C 1 -C 6 - 烷基，其是支链和非支链的，并且R 7 [sic]是氢，C 1 -C 6 - 烷基，其是支链或不分支，而且是数字0，1或2。

8. 发明授权

US09051304B2 Carboxamide compounds and their use as calpain inhibitors V 有权
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：US09051304B2
公开(公告)日：2015-06-09
申请号：US12972663
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： C07D401/04 , C07D401/14 , C07D207/28 , C07D409/14 , C07D417/14
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 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 C1-C3-alkyl, C1-C3-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, or phenyl-C1-C3-alkyl, 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 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。

9. 发明申请

US20110152265A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V 有权
标题翻译：羧酰胺化合物及其作为钙抑制剂V
公开(公告)号：US20110152265A1
公开(公告)日：2011-06-23
申请号：US12972663
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： A61K31/5355 , C07D401/04 , A61K31/4439 , A61P25/28 , A61P25/16 , A61P25/08 , A61P9/00 , A61P13/12 , A61P31/18 , A61P33/06 , C07D413/14
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 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 C1-C3-alkyl, C1-C3-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, or phenyl-C1-C3-alkyl, 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 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。

10. 发明授权

US07956093B2 Substituted amides, their preparation and use 有权
标题翻译：取代酰胺，其制备和使用
公开(公告)号：US07956093B2
公开(公告)日：2011-06-07
申请号：US11897057
申请日：2007-08-29
申请人： Wilfried Lubisch , Achim Möller , Hans-Jörg Treiber , Monika Knopp
发明人： Wilfried Lubisch , Achim Möller , Hans-Jörg Treiber , Monika Knopp
IPC分类号： A61K31/165
CPC分类号： C07D213/82 , A61K31/195 , A61K31/5375 , C07C229/38 , C07C237/22 , C07C237/32 , C07C2601/14 , C07D295/155
摘要： An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts.
摘要翻译：式I的酰胺及其互变异构形式，可能的对映体和非对映体形式，E和Z形式以及可能的生理上耐受的盐。

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