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61. 发明授权

US07786105B2 Pyrimidine compounds and use thereof 有权
标题翻译：嘧啶化合物及其用途
公开(公告)号：US07786105B2
公开(公告)日：2010-08-31
申请号：US11628658
申请日：2005-06-03
申请人： Herve Geneste , Andreas Haupt , Wilfried Braje , Wilfried Lubisch , Gerd Steiner
发明人： Herve Geneste , Andreas Haupt , Wilfried Braje , Wilfried Lubisch , Gerd Steiner
IPC分类号： C07D401/12 , C07D413/12 , C07D417/12 , A61K31/506
CPC分类号： C07D417/12 , C07D401/12 , C07D413/12
摘要： The invention relates to pyrimidine compounds of general formula (I), and to the use of these compounds of general formula (I) and of the physiologically compatible acid addition salts of compounds (I) for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor antagonists or agonists.
摘要翻译：本发明涉及通式（I）的嘧啶化合物，以及这些化合物（I）的化合物和化合物（I）的生理上相容的酸加成盐在制备用于治疗疾病的药剂中的用途，对多巴胺D3受体拮抗剂或激动剂的影响。

62. 发明授权

US08268815B2 Pyrimidine compounds and use thereof 失效
标题翻译：嘧啶化合物及其用途
公开(公告)号：US08268815B2
公开(公告)日：2012-09-18
申请号：US12842776
申请日：2010-07-23
申请人： Hervè Geneste , Andreas Haupt , Wilfried Braje , Wilfried Lubisch , Gerd Steiner
发明人： Hervè Geneste , Andreas Haupt , Wilfried Braje , Wilfried Lubisch , Gerd Steiner
IPC分类号： C07D401/12 , C07D413/12 , C07D417/12 , A61K31/506 , A61P25/36
CPC分类号： C07D417/12 , C07D401/12 , C07D413/12
摘要： The invention relates to compounds of formula (I) and the use of these compounds.
摘要翻译：本发明涉及式（I）化合物和这些化合物的用途。

63. 发明授权

US07723384B2 Keto lactam compounds and use thereof 有权
标题翻译：酮内酰胺化合物及其用途
公开(公告)号：US07723384B2
公开(公告)日：2010-05-25
申请号：US10582285
申请日：2004-12-10
申请人： Wilfried Lubisch , Andreas Haupt , Wilfried Braje , Herve Geneste
发明人： Wilfried Lubisch , Andreas Haupt , Wilfried Braje , Herve Geneste
IPC分类号： C07D403/12 , C07D401/12 , C07D223/16 , A61K31/55
CPC分类号： C07D401/12 , C07D223/16 , C07D403/12
摘要： The invention relates to novel keto lactam compounds, hydrogenated derivatives and tautomers thereof. These compounds have valuable therapeutic properties and are particularly suited for treating diseases that respond to the modulation of the dopamine D3 receptor. The keto lactams have general formula (I), wherein: (a) represents a group of formulas (b) or (c), wherein D is bound to the nitrogen atom and W, Rp and Rq have the meanings cited in Claim 1; —B— represents a bond or (d), wherein Rm and Rn have the meanings cited in Claim 1; (e) represents a single bond or a double bond; Rv, Rw, Rx and Ry have the meanings cited in Claim 1; D represents a linear or branched 2 to 10-membered alkylene chain that can have, as chain members, a heteroatom group K, which is selected among O, S, S(O), S(O)2, N—R8, CO—O, C(O)NR8 and/or 1 or 2 non-adjacent carbonyl groups and which can have a cycloalkane diyl group and/or a double or triple bond; (f) represents a saturated or monounsaturated monocyclic nitrogen heterocyclic compound having 5 to 8 cyclic members or a bicyclic saturated nitrogen heterocyclic compound having 7 to 12 cyclic members.
摘要翻译：本发明涉及新型酮内酰胺化合物，氢化衍生物及其互变异构体。这些化合物具有有价值的治疗特性，特别适用于治疗对多巴胺D3受体调节作出反应的疾病。酮内酰胺具有通式（I），其中：（a）表示式（b）或（c）中的基团，其中D与氮原子结合，W，Rp和Rq具有权利要求1所述的含义; -B-表示键或（d），其中Rm和Rn具有权利要求1中引用的含义; （e）表示单键或双键; Rv，Rw，Rx和Ry具有权利要求1中引用的含义; D表示可以具有作为链成员的选自O，S，S（O），S（O）2，N-R8，CO（C 1 -C 6）中的杂原子基团K的直链或支链2至10元亚烷基链 -O，C（O）NR 8和/或1或2个不相邻的羰基，并且其可具有环烷烃二基和/或双键或三键; （f）表示具有5〜8个环状成员的饱和或单不饱和单环氮杂环化合物或具有7〜12个环状成员的双环饱和氮杂环化合物。

64. 发明授权

US06387912B1 Utilization of pyrimidine derivatives for preventing and treating cerebral ischaemia 失效
标题翻译：利用嘧啶衍生物预防和治疗脑缺血
公开(公告)号：US06387912B1
公开(公告)日：2002-05-14
申请号：US09889162
申请日：2001-07-11
申请人： Gerd Steiner , Kurt Schellhaas , Wilfried Lubisch , Uta Holzenkamp , Dorothea Starck , Monika Knopp , Laszlo Szabo , Franz Emling , Francisco Javier Garcia-Ladona , Hans-Peter Hofmann , Liliane Unger
发明人： Gerd Steiner , Kurt Schellhaas , Wilfried Lubisch , Uta Holzenkamp , Dorothea Starck , Monika Knopp , Laszlo Szabo , Franz Emling , Francisco Javier Garcia-Ladona , Hans-Peter Hofmann , Liliane Unger
IPC分类号： A61K31513
CPC分类号： A61K31/505
摘要： Use of pyrimidine derivatives of the formula I where the substituents are as defined in the description, and of their physiologically tolerated salts for producing medicaments for the prophylaxis and treatment of cerebral ischemia and strokes.
摘要翻译：使用式I的嘧啶衍生物，其中取代基如说明书中所定义，以及它们用于制备用于预防和治疗脑缺血和中风的药物的生理学耐受盐。

65. 发明申请

US20100298326A1 Carboxamide compounds and their use as calpain inhibitors 有权
公开(公告)号：US20100298326A1
公开(公告)日：2010-11-25
申请号：US11990652
申请日：2007-12-28
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： A61K31/5377 , C07D401/02 , A61K31/455 , C07D413/14 , C07D401/14 , A61K31/465 , A61P25/16 , A61P13/12 , A61P27/12 , A61P35/00 , A61P31/18
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.

66. 发明授权

US07320979B2 N-[(piperazinyl)hetaryl]arylsulfonamide compounds 失效
公开(公告)号：US07320979B2
公开(公告)日：2008-01-22
申请号：US10823317
申请日：2004-04-13
申请人： Wilfried M. Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Hervé Geneste , Liliane Unger , Daryl R. Sauer , Sean C. Turner
发明人： Wilfried M. Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Hervé Geneste , Liliane Unger , Daryl R. Sauer , Sean C. Turner
IPC分类号： A61K31/496 , A61K31/506 , C07D213/72 , C07D213/74 , C07D239/48
CPC分类号： C07D213/76 , C07D213/74 , C07D239/69 , C07D401/04 , C07D487/08
摘要： The invention relates to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula I in which Q is a bivalent, 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Ra which is/are selected, independently of each other, from halogen, CN, NO2, CO2R4, COR5, C1-C4-alkyl and C1-C4-haloalkyl; Ar is phenyl or a 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Rb, which is/are selected from halogen, NO2, CN, CO2R4, COR5, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl and C1-C4-haloalkyl, with it also being possible for two radicals Rb which are bonded to adjacent C atoms of Ar to be together C3-C4-alkylene; R1 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy-C1-C4-alkyl, C3-C4-alkenyl or C3-C4-alkynyl; with the radicals n, R1, R2, R3, R4 and R5 having the meanings given in the patent claims, to the N-oxides and to the physiologically tolerated acid addition salts of these compounds and to pharmaceutical compositions which comprise at least one N-[(piperazinyl)hetaryl]arylsulfonamide compound as claimed in one of claims 1 to 10 and/or at least one physiologically tolerated acid addition salt of I and/or an N-oxide of I, where appropriate together with physiologically acceptable carriers and/or auxiliary substances for treating diseases which respond to influencing by dopamine D3 receptor antagonists or agonists, in particular for treating diseases of the central nervous system and disturbances of kidney function.

67. 发明授权

US08436034B2 Carboxamide compounds and their use as calpain inhibitors 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：US08436034B2
公开(公告)日：2013-05-07
申请号：US11990652
申请日：2007-12-28
申请人： Andreas Kling , Wilfried Hornberger , Helmut Mack , Achim Moeller , Volker Nimmrich , Dietmar Seeman , Wilfried Lubisch
发明人： Andreas Kling , Wilfried Hornberger , Helmut Mack , Achim Moeller , Volker Nimmrich , Dietmar Seeman , Wilfried Lubisch
IPC分类号： A61K31/4155 , A61K31/4178 , C07D403/04
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。

68. 发明授权

US07799809B2 Carboxamide compounds and their use as calpain inhibitors 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：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。

69. 发明申请

US20080234329A1 Carboxamide compounds and their use as calpain inhibitors 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：US20080234329A1
公开(公告)日：2008-09-25
申请号：US12070941
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： A61K31/4439 , 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R 1，R 2，R 3，R 3，R 3， >，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，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。

70. 发明授权

US07728012B2 Carboxamide compounds and their use as calpain inhibitors 有权
公开(公告)号：US07728012B2
公开(公告)日：2010-06-01
申请号：US12070941
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.

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