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1. 发明申请

US20080221039A1 Kinin Antagonists For Treating Bladder Dysfunction 审中-公开
标题翻译： Kinin拮抗剂治疗膀胱功能障碍
公开(公告)号：US20080221039A1
公开(公告)日：2008-09-11
申请号：US11994897
申请日：2006-07-04
申请人： Christoph Gibson , Gerd Hummel , Jochen Knolle , Ulrich Reineke , Thomas Tradler
发明人： Christoph Gibson , Gerd Hummel , Jochen Knolle , Ulrich Reineke , Thomas Tradler
IPC分类号： A61K38/08 , C07K7/06 , A61K38/10 , A61P13/10 , C07K7/08
CPC分类号： A61K38/08 , A61K45/06
摘要： The present invention is related to the use of a kinin receptor antagonist for the manufacture of a medicament for the treatment and/or prevention of bladder dysfunction, whereby the kinin receptor is selected from the group comprising B1 and B2 receptors.
摘要翻译：本发明涉及激肽受体拮抗剂在制备用于治疗和/或预防膀胱功能障碍的药物中的用途，其中激肽受体选自B1和B2受体。

2. 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。

3. 发明申请

US20080194524A1 Compounds For the Inhibition of Undesired Cell Proliferation and Use Thereof 审中-公开
标题翻译：化合物用于抑制不需要的细胞增殖及其使用
公开(公告)号：US20080194524A1
公开(公告)日：2008-08-14
申请号：US10583442
申请日：2004-12-18
申请人： Jochen Knolle , Mike Schutkowski , Gerd Hummel , Thomas Tradler , Laurence Jobron , Claudia Christner , Christoph Gibson , Gunther Zischinsky
发明人： Jochen Knolle , Mike Schutkowski , Gerd Hummel , Thomas Tradler , Laurence Jobron , Claudia Christner , Christoph Gibson , Gunther Zischinsky
IPC分类号： A61K31/675 , A61P35/00 , A61P29/00 , A61P37/00 , A61P31/00 , A61P9/00 , A61P25/00 , C07F9/6553 , C07F9/59 , C07F9/6558
CPC分类号： C07F9/65586 , C07F9/59 , C07F9/655354 , C07F9/65583
摘要： The present invention is related to compounds having formula (I) wherein the dashed line indicates a single or double bond or is absent and wherein A1-A9, Q, R1-R11, T, U, V, W1-W3, X1, X2, Y and Z are as defined in the claims and description, pharmaceutical compositions comprising the compounds and the use of the compounds for the manufacture of a medicament for the treatment of diseases involving abnormal cell proliferation, undesired cell proliferation, abnormal mitosis and/or undesired mitosis.
摘要翻译：本发明涉及具有式（I）的化合物，其中虚线表示单键或双键或不存在，并且其中A 1至Q 9，Q，R T 1，U，V，W 1 -W 3，X 1，...， X和Z如权利要求和说明书所定义，包含该化合物的药物组合物和该化合物在制备用于治疗涉及到疾病的药物中的用途异常细胞增殖，不期望的细胞增殖，异常有丝分裂和/或不期望的有丝分裂。

4. 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。

5. 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。

6. 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。

7. 发明授权

US08501787B2 Compounds for the inhibition of angiogenesis and use thereof 有权
标题翻译：用于抑制血管生成的化合物及其用途
公开(公告)号：US08501787B2
公开(公告)日：2013-08-06
申请号：US10593801
申请日：2005-03-24
申请人： Grit Zahn , Roland Stragies , Frank Osterkamp , Gunther Zischinsky , Jochen Knolle , Gerd Hummel , Sascha Birkner , Ulrich Reineke
发明人： Grit Zahn , Roland Stragies , Frank Osterkamp , Gunther Zischinsky , Jochen Knolle , Gerd Hummel , Sascha Birkner , Ulrich Reineke
IPC分类号： A61K31/4439 , C07D401/12
CPC分类号： C07D405/14 , C07D401/12
摘要： This invention is directed to compounds of structure (I). Particularly this invention is directed to compounds of structure (VIII) wherein the variables are defined as in the description. These compounds are integrin inhibitors and are useful in the treatment of diseases in which an inhibition of angiogenesis is desired.
摘要翻译：本发明涉及结构（I）的化合物。特别地，本发明涉及结构（VIII）的化合物，其中变量如描述中所定义。这些化合物是整联蛋白抑制剂，可用于治疗需要抑制血管生成的疾病。

8. 发明申请

US20070155712A1 Compounds for the inhibition of angiogenesis and use thereof 有权
标题翻译：用于抑制血管生成的化合物及其用途
公开(公告)号：US20070155712A1
公开(公告)日：2007-07-05
申请号：US10593801
申请日：2005-03-24
申请人： Grit Zahn , Roland Stragies , Frank Osterkamp , Gunther Zischinsky , Jochen Knolle , Gerd Hummel , Sascha Birkner , Ulrich Reineke
发明人： Grit Zahn , Roland Stragies , Frank Osterkamp , Gunther Zischinsky , Jochen Knolle , Gerd Hummel , Sascha Birkner , Ulrich Reineke
IPC分类号： A61K31/551 , A61K31/55 , A61K31/4965 , A61K31/395 , A61K31/4172 , A61K31/4184 , A61K31/505 , A61K31/40
CPC分类号： C07D405/14 , C07D401/12
摘要： This invention is directed to compounds of structure (I). Particularly this invention is directed to compounds of structure (VIII) wherein the variables are defined as in the description. These compounds are integrin inhibitors and are useful in the treatment of diseases in which an inhibition of angiogenesis is desired.
摘要翻译：本发明涉及结构（I）的化合物。特别地，本发明涉及结构（VIII）的化合物，其中变量如描述中所定义。这些化合物是整联蛋白抑制剂，可用于治疗需要抑制血管生成的疾病。

9. 发明申请

US20060252813A1 Apparatus for curing a composite laminate 审中-公开
标题翻译：用于固化复合层压板的装置
公开(公告)号：US20060252813A1
公开(公告)日：2006-11-09
申请号：US10540013
申请日：2003-12-23
申请人： Jochen Knolle , Mike Schumtkowski , Gerd Hummel , Thomas Tradler , Laurence Jobron , Claudia Christner , Roland Stragies
发明人： Jochen Knolle , Mike Schumtkowski , Gerd Hummel , Thomas Tradler , Laurence Jobron , Claudia Christner , Roland Stragies
IPC分类号： A61K31/405 , C07D405/02 , C07D209/18
CPC分类号： C07D409/12 , A61K31/16 , C07C335/08 , C07C335/12 , C07C335/16 , C07C335/18 , C07D207/16 , C07D209/18 , C07D209/42 , C07D215/36 , C07D317/66 , C07D333/34 , C07D333/38 , C07D333/60
摘要： The present invention is related to a compound of formula (I): A-B-E-D (I), wherein: A is selected from the group consisting Ra-L1-K-L2; and (II) B is either present or absent, but if B is present then B is (III), E is (IV), D is selected from the group comprising —(CR1Rm)rC(O)H, —(CR1Rm)rC—N, —CR1Rm)rNHNHC(O)NR5R6, —(CR1Rm)rC(O)(CRnRo)rc(O)OR7, —(CR1Rm)rC(O)(CrnRo)rC(O)NR8R9, —(CR1Rm)rCH(OH)(CrnRo)rC(O)U, —(CR1Rm)rC(O)W—(CR1Rm)rC(O)CH2W, —(CR1Rm)rC(O)haloalkyl, and —(CR1Rm)rC(O)(CRnRo)r—CHN2, and the use of said compounds as an inhibitor to rotamases.
摘要翻译：本发明涉及式（I）化合物：A-B-E-D（I），其中：A选自R a-L-1 -K-L 2; 和（II）B存在或不存在，但如果存在B，则B是（III），E是（IV），D选自 - （CR 1） C（O）H， - （CR 1），其中R 1，R 2，R 3， CN，-CR 1，...，...，NHNHC（O）NR 5 R 6， C（O）（CR）n（R 1）其中R 1，R 2，R 2， C（O）OR 7， - （CR 1）， - （CR 1） C（O）（O）（C 1 -C 6）C（O）NR 8 （CR 1）（CH 2）n（CH 2）CH（OH）（C 1 -C 6） C（O）U， - （CR 1），O（R 1） C（O）W - （CR 1）CH 2）C（O）CH （O）卤代烷基，和 - （CR 1）2， - （CR 1） C（O）（CR）R（O）R（CH 2） -CHN 2 N 2，以及所述化合物作为旋转异构酶抑制剂的用途。

10. 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。

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