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1. 发明申请

US20090104116A1 COMPOUNDS FOR THE INHIBITION OF INTEGRINS AND USE THEREOF 有权
标题翻译：用于抑制整合及其使用的化合物
公开(公告)号：US20090104116A1
公开(公告)日：2009-04-23
申请号：US12162798
申请日：2007-01-31
申请人： Gunter Zischinsky , Roland Stragies , Frank Osterkamp , Dirk Scharn , Gerd Hummel , Holger Kalkhof , Grit Zahn , Doerte Vossmeyer , Claudia Christner-Albrecht , Ulrich Reineke
发明人： Gunter Zischinsky , Roland Stragies , Frank Osterkamp , Dirk Scharn , Gerd Hummel , Holger Kalkhof , Grit Zahn , Doerte Vossmeyer , Claudia Christner-Albrecht , Ulrich Reineke
IPC分类号： A61K51/04 , C07D401/12 , A61K31/4427 , C07D471/04 , A61K31/4375 , A61K49/04 , A61P35/00 , A61K49/10 , A61K31/535 , C07D265/08 , C12N9/00
CPC分类号： C07D401/12 , C07D471/04
摘要： The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; Ψ is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.
摘要翻译：本发明涉及式（I）化合物，其中A是非芳族杂环，Ar不存在或亚苯基; Psi是式（II）的基团，R2是疏水部分; 并且G是含有一个或多个选自NH，OH和碱性部分的部分的基团。化合物是整联蛋白的抑制剂，特别是纤连蛋白受体α5β1的拮抗剂，可用作抗血管生成剂。

2. 发明授权

US08309735B2 Heterocyclic compounds for the inhibition of integrins and use thereof 有权
标题翻译：用于抑制整联蛋白的杂环化合物及其用途
公开(公告)号：US08309735B2
公开(公告)日：2012-11-13
申请号：US12300530
申请日：2007-05-14
申请人： Gunther Zischinsky , Roland Stragies , Frank Osterkamp , Dirk Scharn , Gerd Hummel , Holger Kalkhof , Grit Zahn , Doerte Vossmeyer , Claudia Christner-Albrecht , Ulrich Reineke
发明人： Gunther Zischinsky , Roland Stragies , Frank Osterkamp , Dirk Scharn , Gerd Hummel , Holger Kalkhof , Grit Zahn , Doerte Vossmeyer , Claudia Christner-Albrecht , Ulrich Reineke
IPC分类号： C07D213/72 , A61K31/44
CPC分类号： C07D405/12 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of formula (I) wherein: A is a radical selected from the group comprising aromatic heterocyclic 5-membered ring systems; Ar is a radical selected from the group comprising optionally substituted 5- and 6-membered aromatic ring systems, whereby the ring system contains 0, 1, 2 or 3 heteroatoms selected from the group comprising N, O and S; Z is a linker and Ψ is a radical of formula (II) and their use for the inhibition of integrin.
摘要翻译：本发明涉及式（I）化合物，其中：A是选自芳族杂环5元环系的基团; Ar是选自包含任选取代的5元和6元芳族环系的基团，其中该环体系含有0,1,2或3个选自N，O和S的杂原子; Z是连接体，Ψ是式（II）的基团及其用于抑制整联蛋白的用途。

3. 发明授权

US08927534B2 Compounds for the inhibition of integrins and use thereof 有权
标题翻译：用于抑制整联蛋白的化合物及其用途
公开(公告)号：US08927534B2
公开(公告)日：2015-01-06
申请号：US12162798
申请日：2007-01-31
申请人： Gunther Zischinsky , Roland Stragies , Frank Osterkamp , Dirk Scharn , Gerd Hummel , Holger Kalkhof , Grit Zahn , Doerte Vossmeyer , Claudia Christner-Albrecht , Ulrich Reineke
发明人： Gunther Zischinsky , Roland Stragies , Frank Osterkamp , Dirk Scharn , Gerd Hummel , Holger Kalkhof , Grit Zahn , Doerte Vossmeyer , Claudia Christner-Albrecht , Ulrich Reineke
IPC分类号： C07D401/12 , C07D471/04
CPC分类号： C07D401/12 , C07D471/04
摘要： The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; Ψ is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.
摘要翻译：本发明涉及式（I）化合物，其中A是非芳族杂环，Ar不存在或亚苯基; Ψ是式（II）的基团，R 2是疏水部分; 并且G是含有一个或多个选自NH，OH和碱性部分的部分的基团。化合物是整联蛋白的抑制剂，特别是纤连蛋白受体α5β1的拮抗剂，可用作抗血管生成剂。

4. 发明申请

US20090203745A1 HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF INTEGRINS AND USE THEREOF 有权
标题翻译：用于抑制整合及其使用的杂环化合物
公开(公告)号：US20090203745A1
公开(公告)日：2009-08-13
申请号：US12300530
申请日：2007-05-14
申请人： Gunther Zischinsky , Roland Stragies , Frank Osterkamp , Dirk Scharn , Gerd Hummel , Holger Kalkhof , Grit Zahn , Doerte Vossmeyer , Claudia Christner-Albrecht , Ulrich Reineke
发明人： Gunther Zischinsky , Roland Stragies , Frank Osterkamp , Dirk Scharn , Gerd Hummel , Holger Kalkhof , Grit Zahn , Doerte Vossmeyer , Claudia Christner-Albrecht , Ulrich Reineke
IPC分类号： A61K31/4439 , A61K31/427 , A61K31/422 , A61K31/4192 , C07D417/12 , C07D413/12 , C07D403/12
CPC分类号： C07D405/12 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of formula (I) wherein: A is a radical selected from the group comprising aromatic heterocyclic 5-membered ring systems; Ar is a radical selected from the group comprising optionally substituted 5- and 6-membered aromatic ring systems, whereby the ring system contains 0, 1, 2 or 3 heteroatoms selected from the group comprising N, O and S; Z is a linker and Ψ is a radical of formula (II) and their use for the inhibition of integrin.
摘要翻译：本发明涉及式（I）化合物，其中：A是选自芳族杂环5元环系的基团; Ar是选自包含任选取代的5元和6元芳族环系的基团，其中该环体系含有0,1,2或3个选自N，O和S的杂原子; Z是接头，Psi是式（II）的基团及其用于抑制整联蛋白的用途。

5. 发明申请

US20110065760A1 COMPOUNDS FOR THE INHIBITION OF ROTAMASES AND USE THEREOF 审中-公开
标题翻译：化合物用于抑制ROTAMASES及其用途
公开(公告)号：US20110065760A1
公开(公告)日：2011-03-17
申请号：US12624308
申请日：2009-11-23
申请人： Jochen KNOLLE , Mike Schutkowski , Gerd Hummel , Thomas Tradler , Laurence Jobron , Claudia Christner , Dirk Scharn , Roland Stragies , Christoph Gibson , Frank Osterkamp
发明人： Jochen KNOLLE , Mike Schutkowski , Gerd Hummel , Thomas Tradler , Laurence Jobron , Claudia Christner , Dirk Scharn , Roland Stragies , Christoph Gibson , Frank Osterkamp
IPC分类号： A61K31/428 , C07C275/34 , A61K31/17 , C07C311/13 , A61K31/18 , C07C311/08 , C07C233/29 , A61K31/167 , C07C211/48 , A61K31/137 , C07C271/58 , A61K31/27 , C07D277/66 , A61P31/00 , A61P35/00 , A61P29/00 , A61P9/00 , C12N9/99
CPC分类号： A61K31/155 , A61K31/135 , A61K31/165 , A61K31/17 , A61K31/18 , Y02A50/401 , Y02A50/406 , Y02A50/409 , Y02A50/411 , Y02A50/465 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483
摘要： The present invention is related to a compound of the formula (I), (II), (III), (IV), (V): wherein Z1, Z2, Z3 and Z4 are each and independently selected from the group comprising C(O)—, —C(S)—, —C(O)—NR10—, —C(S)—NR11—, —C(N—CN)—NR12—, —S(O)—, —S(O2)—, —S(O)—NR13—, and S(O2)—NR14—, —O—, —S— or are each and individually absent; X is a spacer and is independently selected from the group comprising -M1-L1-K-L2-M2-, wherein Y. is selected from the group comprising alkyl, substituted alkyl, straight alkyl, substituted straight alkyl, branched alkyl, substituted branched alkyl, straight alkenyl, substituted straight alkenyl, branched alkenyl, substituted branched alkenyl, straight alkynyl, substituted straight alkynyl, branched alkynyl, substituted branched alkynyl, cycloalkyl, substituted cycloalkyl, cycloalkenyl, substituted cycloalkenyl, heterocyclyl, substituted heterocyclyl, mono-unsaturated heterocyclyl, poly-unsaturated heterocyclyl, mono-substituted poly-unsaturated heterocyclyl, poly-substituted poly-unsaturated heterocyclyl, mono-substituted mono-unsaturated heterocyclyl, poly-substituted mono-unsaturated heterocyclyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl, wherein Y is different from a peptide or is absent.
摘要翻译：本发明涉及式（I），（II），（III），（IV），（V））的化合物：其中Z 1，Z 2，Z 3和Z 4各自独立地选自C（（O） - ， - C（O） - ， - C（O） - ， - （C 1 -C 6）（O）-NR 13 - 和S（O 2）-NR 14 - ， - O - ， - S-或各自不存在; X是间隔基，并且独立地选自-M1-L1-K-L2-M2-，其中Y选自烷基，取代的烷基，直链烷基，取代的直链烷基，支链烷基，取代的支链烷基，直链烯基，取代的直链烯基，支链烯基，取代的支链烯基，直链炔基，取代的直链炔基，支链炔基，取代的支链炔基，环烷基，取代的环烷基，环烯基，取代的环烯基，杂环基，取代的杂环基，单不饱和杂环基，多取代的多不饱和杂环基，多取代的多不饱和杂环基，单取代的单不饱和杂环基，多取代的单不饱和杂环基，芳基，取代的芳基，杂芳基和取代的杂芳基，其中Y是不同于肽或不存在。

6. 发明申请

US20070054904A1 Phenol derivatives and their use as rotamase inhibitors 审中-公开
标题翻译：苯酚衍生物及其作为旋转异构酶抑制剂的用途
公开(公告)号：US20070054904A1
公开(公告)日：2007-03-08
申请号：US10528139
申请日：2003-09-18
申请人： Jochen Knolle , Mike Schutkowski , Gerd Hummel , Thomas Tradler , Laurence Jobron , Claudia Christner , Dirk Scharn , Roland Stragies , Christoph Gibson , Frank Osterkamp
发明人： Jochen Knolle , Mike Schutkowski , Gerd Hummel , Thomas Tradler , Laurence Jobron , Claudia Christner , Dirk Scharn , Roland Stragies , Christoph Gibson , Frank Osterkamp
IPC分类号： A61K31/277 , A61K31/17
CPC分类号： A61K31/155 , A61K31/135 , A61K31/165 , A61K31/17 , A61K31/18 , Y02A50/401 , Y02A50/406 , Y02A50/409 , Y02A50/411 , Y02A50/465 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483
摘要： The present invention is related to a compound of the formula (I), (II), (III), (IV), (V): wherein Z1, Z2, Z3 and Z4 are each and independently selected from the group comprising C(O)—, —C(S)—, —C(O)—NR10—, —C(S)—NR11—, —C(N—CN)—NR12—, —S(O)—, —S(O2)—, —S(O)—NR13—, and —S(O2)—NR14—, —O—, —S— or are each and individually absent; X is a spacer and is independently selected from the group comprising -M1-L1-K-L2-M2-, wherein Y. is selected from the group comprising alkyl, substituted alkyl, straight alkyl, substituted straight alkyl, branched alkyl, substituted branched alkyl, straight alkenyl, substituted straight alkenyl, branched alkenyl, substituted branched alkenyl, straight alkynyl, substituted straight alkynyl, branched alkynyl, substituted branched alkynyl, cycloalkyl, substituted cycloalkyl, cycloalkenyl, substituted cycloalkenyl, heterocyclyl, substituted heterocyclyl, mono-unsaturated heterocyclyl, poly-unsaturated heterocyclyl, mono-substituted poly-unsaturated heterocyclyl, poly-substituted poly-unsaturated heterocyclyl, mono-substituted mono-unsaturated heterocyclyl, poly-substituted mono-unsaturated heterocyclyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl, wherein Y is different from a peptide or is absent.
摘要翻译：本发明涉及式（I），（II），（III），（IV），（V）的化合物：其中Z 1，Z 2， Z，Z 3和Z 4各自独立地选自C（O） - ， - C（S） - ， - C（O）-NR C（S）-NR 11 - ， - C（N-CN）-NR 12 - ， - S（O ） - ， - （O 2 - ） - ， - S（O）-NR 13 - 和-S（O）2 - NR 14 - ， - O - ， - S-或各自不存在; X是间隔基，并且独立地选自-M1-L1-K-L2-M2-，其中Y选自烷基，取代的烷基，直链烷基，取代的直链烷基，支链烷基，取代的支链烷基，直链烯基，取代的直链烯基，支链烯基，取代的支链烯基，直链炔基，取代的直链炔基，支链炔基，取代的支链炔基，环烷基，取代的环烷基，环烯基，取代的环烯基，杂环基，取代的杂环基，单不饱和杂环基，多取代的多不饱和杂环基，多取代的多不饱和杂环基，单取代的单不饱和杂环基，多取代的单不饱和杂环基，芳基，取代的芳基，杂芳基和取代的杂芳基，其中Y是不同于肽或不存在。

7. 发明授权

US08410134B2 8-oxy-quinoline derivatives as bradykinin B2 receptor modulators 失效
标题翻译： 8-氧 - 喹啉衍生物作为缓激肽B2受体调节剂
公开(公告)号：US08410134B2
公开(公告)日：2013-04-02
申请号：US12532703
申请日：2008-03-22
申请人： Christoph Gibson , Thomas Tradler , Karsten Schnatbaum , Jochen Pfeifer , Elsa Locardi , Dirk Scharn , Matthias Paschke , Ulf Reimer , Uwe Richter , Gerd Hummel , Ulrich Reineke
发明人： Christoph Gibson , Thomas Tradler , Karsten Schnatbaum , Jochen Pfeifer , Elsa Locardi , Dirk Scharn , Matthias Paschke , Ulf Reimer , Uwe Richter , Gerd Hummel , Ulrich Reineke
IPC分类号： A61K31/04 , C07D215/38
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is related to compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein A is a 6-membered heteroaryl having from 1 to 3 heteroatoms, each independently selected from N or O and the other substituents are defined as in the claims.
摘要翻译：本发明涉及式（I）化合物或其药理学上可接受的盐，溶剂合物或水合物，其中A为具有1至3个杂原子的6元杂芳基，各自独立地选自N或O，且其它取代基如权利要求中所定义。

8. 发明授权

US08029979B2 Method for determining the substrate specificity of an enzyme 有权
标题翻译：确定酶底物特异性的方法
公开(公告)号：US08029979B2
公开(公告)日：2011-10-04
申请号：US11474283
申请日：2006-06-26
申请人： Jens Schneider-Mergener , Mike Schutkowski , Ulf Reimer , Liying Dong , Soren Panse , Dirk Scharn , Frank Osterkamp , Gerd Hummel , Laurence Jobron
发明人： Jens Schneider-Mergener , Mike Schutkowski , Ulf Reimer , Liying Dong , Soren Panse , Dirk Scharn , Frank Osterkamp , Gerd Hummel , Laurence Jobron
IPC分类号： C12Q1/00
CPC分类号： C12Q1/37 , C12Q1/34 , C12Q1/42 , C12Q1/44 , C12Q1/48 , C12Q1/485
摘要： The invention relates to a method for determining the substrate specificity of an enzymatic activity comprising the following steps: providing an assembly comprising a plurality of amino acid sequences on a planar surface of a support material, whereby the amino acids are directionally immobilized; contacting and/or incubating of an enzymatic activity with the assembly; and detection of a reaction between one of the amino acid sequences that are immobilized on the assembly and the enzymatic activity. According to the invention, during the reaction of the enzymatic activity with the assembly, a change in the molecular weight of at least one of the amino acid sequences takes place.
摘要翻译：本发明涉及一种用于确定酶活性的底物特异性的方法，包括以下步骤：在载体材料的平坦表面上提供包含多个氨基酸序列的组合，由此氨基酸定向固定; 将酶活性与组合物接触和/或孵育; 以及检测固定在组合物上的氨基酸序列之一与酶活性之间的反应。根据本发明，在酶活性与组装反应期间，发生至少一个氨基酸序列的分子量的变化。

9. 发明授权

US08071810B2 C5a receptor antagonists 失效
标题翻译： C5a受体拮抗剂
公开(公告)号：US08071810B2
公开(公告)日：2011-12-06
申请号：US11915892
申请日：2006-05-30
申请人： Karsten Schnatbaum , Dirk Scharn , Elsa Locardi , Thomas Polakowski , Uwe Richter , Ulrich Reineke , Gerd Hummel
发明人： Karsten Schnatbaum , Dirk Scharn , Elsa Locardi , Thomas Polakowski , Uwe Richter , Ulrich Reineke , Gerd Hummel
IPC分类号： C07C275/00 , C07C273/00
CPC分类号： C07C275/40 , C07C235/40 , C07C275/26 , C07C275/30 , C07C2602/08 , C07C2602/10 , C07D207/327 , C07D213/40 , C07D213/61 , C07D215/40 , C07D235/06 , C07D237/08 , C07D239/42 , C07D241/42 , C07D311/20 , C07D335/02
摘要： The present invention is related to a compound, preferably a C5a receptor antagonist, having the following structure, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21 and R22 are individually and independently selected from the group comprising H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, substituted arylalkyl, heteroarylalkyl, substituted heteroarylalkyl, alkoxyl, substituted alkoxyl, aryloxy, substituted aryloxy, arylalkyloxy, substituted arylalkyloxy, acyloxy, substituted acyloxy, halogen, hydroxyl, nitro, cyano, acyl, substituted acyl, mercapto, alkylthio, substituted alkylthio, amino, substituted amino, alkylamino, substituted alkylamino, bisalkyl amino, substituted bisalkyl amino, cyclic amino, substituted cyclic amino, carbamoyl (—CONH2), substituted carbamoyl, carboxyl, carbamate, alkoxycarbonyl, substituted alkoxycarbonyl, acylamino, substituted acylamino, sulfamoyl (—SO2NH2), substituted sulfamoyl, haloalkyl, haloalkyloxy, —C(O)H, trialkylsilyl and azido.
摘要翻译：本发明涉及具有以下结构的化合物，优选C5a受体拮抗剂：R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R11，R12，R13，R14，R15， R16，R17，R18，R19，R20，R21和R22各自独立地选自H，烷基，取代的烷基，烯基，取代的烯基，炔基，取代的炔基，环烷基，取代的环烷基，杂环基，取代的杂环基，芳基，取代的芳基，杂芳基，取代的杂芳基，芳基烷基，取代的芳基烷基，杂芳基烷基，取代的杂芳基烷基，烷氧基，取代的烷氧基，芳氧基，取代的芳氧基，芳基烷氧基，取代的芳基烷氧基，酰氧基，取代的酰氧基，卤素，羟基，硝基，氰基，酰基，巯基，烷硫基，取代的烷硫基，氨基，取代的氨基，烷基氨基，取代的烷基氨基，双烷基氨基，取代的双烷基氨基，环状氨基，取代的环状氨基，氨基甲酰基（-CONH 2）氨基甲酰基，羧基，氨基甲酸酯，烷氧基羰基，取代的烷氧基羰基，酰氨基，取代的酰氨基，氨磺酰基（-SO2NH2），取代的氨磺酰基，卤代烷基，卤代烷氧基，-C（O）H，三烷基甲硅烷基和叠氮基。

10. 发明申请

US20100234344A1 8-OXY-QUINOLINE DERIVATIVES AS BRADYKININ B2 RECEPTOR MODULATORS 失效
标题翻译： 8-O-喹啉衍生物作为BRADYKININ B2受体调节剂
公开(公告)号：US20100234344A1
公开(公告)日：2010-09-16
申请号：US12532703
申请日：2008-03-22
申请人： Christoph Gibson , Thomas Tradler , Karsten Schinatbaum , Jochen Pfeifer , Elsa Locardi , Dirk Scharn , Mathias Paschke , Ulf Reimer , Uwe Richter , Gerd Hummel , Ulrich Reineke
发明人： Christoph Gibson , Thomas Tradler , Karsten Schinatbaum , Jochen Pfeifer , Elsa Locardi , Dirk Scharn , Mathias Paschke , Ulf Reimer , Uwe Richter , Gerd Hummel , Ulrich Reineke
IPC分类号： A61K31/4709 , A61K31/541 , A61K31/5355 , A61K31/5377 , A61K31/496 , C07D417/14 , C07D413/14 , C07D401/14 , A61P9/00 , A61P1/18 , A61P13/12 , A61P1/16 , A61P3/00 , A61P37/08 , A61P5/00 , A61P35/00 , A61P7/00 , C12N5/071 , G01N33/53
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is related to compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein A is a 6-membered heteroaryl having from 1 to 3 heteroatoms, each independently selected from N or O and the other substituents are defined as in the claims.
摘要翻译：本发明涉及式（I）化合物或其药理学上可接受的盐，溶剂合物或水合物，其中A为具有1至3个杂原子的6元杂芳基，各自独立地选自N或O，且其它取代基如权利要求中所定义。

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