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1. 发明专利

JP2011057681A C5a RECEPTOR ANTAGONIST 审中-公开
标题翻译： C5a受体拮抗剂
公开(公告)号：JP2011057681A
公开(公告)日：2011-03-24
申请号：JP2010230873
申请日：2010-10-13
申请人： Jerini Ag , イエリニ・アクチェンゲゼルシャフトJerini Ag
发明人： HUMMEL GERD , LOCARDI ELSA , POLAKOWSKI THOMAS , SCHARN DIRK , SCHNATBAUM KARSTEN
IPC分类号： C07K7/54 , A61K38/00 , A61P1/00 , A61P1/04 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P21/04 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/04 , A61P37/02 , A61P37/06 , A61P43/00 , C07K7/06 , C07K7/50 , C07K7/56 , C07K7/64 , C07K14/47 , C07K14/705
CPC分类号： C07K7/56 , C07K14/705
摘要： PROBLEM TO BE SOLVED: To provide a C5a receptor antagonist.
SOLUTION: The present invention relates to the C5a receptor antagonist represented by formula (I) [wherein, in one embodiment, X1 is a radical having a mass of about 1-300 and preferably selected from the group consisting of R5-, R5-CO-, R5-N(R6)-CO-, R5-O-CO-, R5-SO2-, R5-N(R6)-C(NH)-, wherein R5 and R6 are individually and independently selected from the group consisting of H, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl and substituted aryl; X2 and X6 are individually and independently aromatic amino acids, derivatives or analogs thereof, X5 and X7 are individually and independently hydrophobic amino acids, derivatives or analogs thereof].
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供C5a受体拮抗剂。解决方案：本发明涉及由式（I）表示的C5a受体拮抗剂[其中，在一个实施方案中，X 1为质量约1-300的基团，优选选自R5-， R5-CO-，R5-N（R6）-CO-，R5-O-CO-，R5-SO2-，R5-N（R6）-C（NH） - ，其中R5和R6各自独立地选自由H，烷基，取代的烷基，环烷基，取代的环烷基，杂环基，取代的杂环基，芳基和取代的芳基组成的基团; X 2和X 6各自独立地为芳族氨基酸，其衍生物或类似物，X5和X7各自独立地为疏水性氨基酸，其衍生物或类似物]。版权所有（C）2011，JPO＆INPIT

2. 发明专利

JP2011037869A New compound for inhibiting rotamase, and use thereof 审中-公开
标题翻译：用于抑制ROTAMASE的新化合物及其用途
公开(公告)号：JP2011037869A
公开(公告)日：2011-02-24
申请号：JP2010219856
申请日：2010-09-29
申请人： Jerini Ag , イエリニ・アクチェンゲゼルシャフトJerini Ag
发明人： KNOLLE JOCHEN , SCHUTKOWSKI MIKE , HUMMEL GERD , TRADLER THOMAS , JOBRON LAURANCE , CHRISTNER CLAUDIA , SCHARN DIRK , STRAGIES ROLAND , GIBSON CHRISTOPH , OSTERKAMP FRANK
IPC分类号： C07C275/36 , C07D295/12 , A61K31/135 , A61K31/137 , A61K31/155 , A61K31/165 , A61K31/167 , A61K31/17 , A61K31/18 , A61K31/216 , A61K31/22 , A61K31/223 , A61K31/27 , A61K31/277 , A61K31/341 , A61K31/36 , A61K31/381 , A61K31/4164 , A61K31/417 , A61K31/4184 , A61K31/428 , A61K31/4409 , A61K31/47 , A61K31/5375 , A61P1/04 , A61P1/12 , A61P1/16 , A61P7/02 , A61P7/04 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/08 , A61P13/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/14 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/06 , A61P31/10 , A61P31/12 , A61P31/14 , A61P31/16 , A61P31/18 , A61P31/22 , A61P33/00 , A61P33/02 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/06 , A61P43/00 , C07C215/48 , C07C215/76 , C07C215/78 , C07C217/54 , C07C217/58 , C07C233/25 , C07C233/62 , C07C233/75 , C07C271/28 , C07C275/34 , C07C275/40 , C07C275/42 , C07C311/08 , C07C311/13 , C07C317/32 , C07C317/36 , C07C323/32 , C07C323/37 , C07C323/41 , C07C335/18 , C07D213/75 , C07D215/36 , C07D233/64 , C07D235/14 , C07D277/66 , C07D295/18 , C07D295/22 , C07D307/52 , C07D307/68 , C07D317/60 , C07D317/66 , C07D333/28 , C07D333/34
CPC分类号： A61K31/155 , A61K31/135 , A61K31/165 , A61K31/17 , A61K31/18
摘要： PROBLEM TO BE SOLVED: To provide new compounds for inhibiting rotamase.
SOLUTION: Compounds of formulas (I), (II), (III), (IV) and (V), respectively, are provided. Uses of these compounds as pharmaceuticals are also provided.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供新的抑制旋转异构酶的化合物。解决方案：分别提供式（I），（II），（III），（IV）和（V）的化合物。也提供了这些化合物作为药物的用途。版权所有（C）2011，JPO＆INPIT

3. 发明申请

WO2009036996A2 SMALL MOLECULE BRADYKININ B1 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：小分子BRADYKININ B1受体拮抗剂
公开(公告)号：WO2009036996A2
公开(公告)日：2009-03-26
申请号：PCT/EP2008007919
申请日：2008-09-19
申请人： JERINI AG , LOCARDI ELSA , DINKEL KLAUS , SCHAUDT MARCO , RICHTER UWE , SCHARN DIRK , HUMMEL GERD , REINEKE ULRICH , REIMER ULF
发明人： LOCARDI ELSA , DINKEL KLAUS , SCHAUDT MARCO , RICHTER UWE , SCHARN DIRK , HUMMEL GERD , REINEKE ULRICH , REIMER ULF
IPC分类号： C07D207/06 , A61K31/506 , A61P29/00 , C07C209/00 , C07D207/20 , C07D213/82 , C07D213/89 , C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D417/12
CPC分类号： C07D403/12 , C07C237/42 , C07C281/06 , C07C2601/02 , C07D207/06 , C07D207/20 , C07D213/82 , C07D213/89 , C07D239/42 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12
摘要： Disclosed are compounds of formula (I) which are bradykinin B1 receptor (B1R) antagonists. These compounds are useful to treat diseases or relieve adverse symptoms associated with inflammation and pain. The invention encompasses novel compounds and acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases involving inflammation and pain.
摘要翻译：公开了式（I）化合物，其为缓激肽B1受体（B1R）拮抗剂。这些化合物可用于治疗疾病或缓解与炎症和疼痛相关的不良症状。本发明包括新型化合物及其可接受的衍生物，用于预防和治疗涉及炎症和疼痛的疾病的药物组合物和方法。

4. 发明申请

WO2007131764A3 NEW HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF INTEGRINS AND USE THEREOF 审中-公开
标题翻译：用于抑制整合及其使用的新型杂环化合物
公开(公告)号：WO2007131764A3
公开(公告)日：2008-01-10
申请号：PCT/EP2007004283
申请日：2007-05-14
申请人： JERINI AG , ZISCHINSKY GUNTHER , STRAGIES ROLAND , OSTERKAMP FRANK , SCHARN DIRK , HUMMEL GERD , KALKHOF HOLGER , ZAHN GRIT , VOSSMEYER DOERTE , CHRISTNER-ALBRECHT CLAUDIA , REINEKE ULRICH
发明人： ZISCHINSKY GUNTHER , STRAGIES ROLAND , OSTERKAMP FRANK , SCHARN DIRK , HUMMEL GERD , KALKHOF HOLGER , ZAHN GRIT , VOSSMEYER DOERTE , CHRISTNER-ALBRECHT CLAUDIA , REINEKE ULRICH
IPC分类号： C07D401/12 , A61K31/44 , A61P29/00 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
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, 0 and S; Z is a linker and ? 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元芳环体系的基团，其中环系统含有0,1,2或3个选自N，O和S的杂原子; Z是一个连接子？是式（II）的基团及其用于抑制整联蛋白的用途。

5. 发明申请

WO02083933A3 METHOD FOR DETERMINING THE SUBSTRATE SPECIFICITY OF AN ENZYMATIC ACTIVITY AND A DEVICE THEREFOR 审中-公开
标题翻译：法测定酶活活动的底物特异性及其装置
公开(公告)号：WO02083933A3
公开(公告)日：2003-10-16
申请号：PCT/EP0204265
申请日：2002-04-17
申请人： JERINI AG , SCHNEIDER-MERGENER JENS , SCHUTKOWSKI MIKE , REIMER ULF , DONG LIYING , PANSE SOEREN , SCHARN DIRK , OSTERKAMP FRANK , HUMMEL GERD , JOBRON LAURENCE
发明人： SCHNEIDER-MERGENER JENS , SCHUTKOWSKI MIKE , REIMER ULF , DONG LIYING , PANSE SOEREN , SCHARN DIRK , OSTERKAMP FRANK , HUMMEL GERD , JOBRON LAURENCE
IPC分类号： C12Q1/25 , C07K17/02 , C07K17/14 , C12Q1/26 , C12Q1/34 , C12Q1/37 , C12Q1/42 , C12Q1/44 , C12Q1/48 , C12Q1/527 , C12Q1/533 , G01N33/68 , C12Q1/00 , G01N33/543
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: preparation of an assembly comprising a plurality of amino acid sequences on a planar surface of a support material, whereby the amino acid sequences are directionally immobilised; 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 immobilised on the assembly and the enzymatic activity. According to the invention, during the reaction of the enzymatic activity with the assembly, a change to 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包括以下步骤的酶活性的底物特异性：提供阵列，其包含在载体材料上的平坦表面，其中所述氨基酸序列被固定指向的多个氨基酸序列; 接触和/或温育与排列的酶活性; 并检测固定在氨基酸序列的排列和酶促活性之间的反应; 它被提供了酶活性的反应与排列的氨基酸序列中的至少一个的分子量变化进行。

6. 发明申请

WO2005010030A2 C5A RECEPTOR ANTAGONISTS 审中-公开
标题翻译： C5a受体拮抗剂
公开(公告)号：WO2005010030A2
公开(公告)日：2005-02-03
申请号：PCT/EP2004008057
申请日：2004-07-19
申请人： JERINI AG , HUMMEL GERD , LOCARDI ELSA , POLAKOWSKI THOMAS , SCHARN DIRK , SCHNATBAUM KARSTEN
发明人： HUMMEL GERD , LOCARDI ELSA , POLAKOWSKI THOMAS , SCHARN DIRK , SCHNATBAUM KARSTEN
IPC分类号： A61K38/00 , C07K7/06 , C07K7/50 , C07K7/56 , C07K14/47 , C07K14/705 , C07K7/00
CPC分类号： C07K7/56 , C07K14/705
摘要： The invention relates to a C5a receptor antagonist of structure (I), wherein X1 is a radical having a mass of about 1-300 and stands for R5-, R5-CO-, R5-N(R6)-CO-, R5-O-CO-, R5-SO2-, R5-N(R6)-SO2-, R5-N(R6)-, R5-N(R6)-CS-, R5-N(R6)-C(NH)-, R5-CS-, R5-P(O)OH-, R5-B(OH)- or R5-CH=N-O-CH2-CO-, wherein R5/R6 represent H, F, hydroxy, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, arylalkyl, substituted arylalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, acyl, substituted acyl, alkoxy, alkoxyalkyl, substituted alkoxyalkyl, aryloxyalkyl or substituted aryloxyalkyl; X2 = radical (biological bonding properties of a mimicrying phenylalanine unit); X3/X4 = spacer (amino acids, amino-acid analogs and amino-acid derivatives); X5 = radical (biological bonding properties of a mimicrying cyclohexylalanine or homoleucine unit); X6 = radical (biological bonding properties of a mimicrying tryptophan unit); X7 = radical (biological bonding properties of a mimicrying norleucine or phenylalanine unit), a chemical bond being formed between X3 and X7.
摘要翻译： C5a受体拮抗剂，其具有结构（I），其中X为基团具有约1-300的质量，并且其中X 1是R 5 - ，R 5 -CO-，R 5-N（R6）-CO-，R5-O -CO-，R 5 -SO 2 - ，R 5-N（R 6）-SO 2 - ，R 5-N（R6） - ，R 5-N（R6） - CS-，R5-N（R 6）-C（NH） - ， - R5-CS-，R5-P（O）OH-，R 5-B（OH） - ，或R 5-CH = NO-CH 2 CO-，其中R 5 / R 6是H，F，羟基，烷基，取代的烷基，环烷基，取代环烷基，杂环基，取代的杂环基，芳基烷基，取代芳烷基，芳基，取代芳基，杂芳基，取代的杂芳基，酰基，取代酰基，烷氧基，烷氧基烷基，取代的烷氧基烷基，芳氧基烷基或取代的芳氧基，X2 =自由基（生物结合苯丙氨酸的特征部分mimikrierend），X3 / X4 =间隔（氨基酸，氨基酸类似物和氨基酸衍生物），X5 =自由基（生物结合的Cyclohexylalanin-或高亮氨酸单元mimikrierend的特性），X6 =自由基（生物结合色氨酸Einhe的特征它mimikrierend），X7 =正亮氨酸或苯丙氨酸单元mimikrierend的自由基（生物结合特征，一个化学键X3和X7）之间形成。

7. 发明申请

WO2004026815A3 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ROTAMASE抑制剂的用途
公开(公告)号：WO2004026815A3
公开(公告)日：2004-12-02
申请号：PCT/EP0310406
申请日：2003-09-18
申请人： JERINI AG , KNOLLE JOCHEN , SCHUTKOWSKI MIKE , HUMMEL GERD , TRADLER THOMAS , JOBRON LAURENCE , CHRISTNER CLAUDIA , SCHARN DIRK , STRAGIES ROLAND , GIBSON CHRISTOPH , OSTERKAMP FRANK
发明人： KNOLLE JOCHEN , SCHUTKOWSKI MIKE , HUMMEL GERD , TRADLER THOMAS , JOBRON LAURENCE , CHRISTNER CLAUDIA , SCHARN DIRK , STRAGIES ROLAND , GIBSON CHRISTOPH , OSTERKAMP FRANK
IPC分类号： C07D295/12 , A61K31/135 , A61K31/137 , A61K31/155 , A61K31/165 , A61K31/167 , A61K31/17 , A61K31/18 , A61K31/216 , A61K31/22 , A61K31/27 , A61K31/277 , A61K31/341 , A61K31/36 , A61K31/381 , A61K31/4164 , A61K31/4184 , A61K31/428 , A61K31/4409 , A61K31/47 , A61K31/5375 , A61P1/04 , A61P1/12 , A61P1/16 , A61P7/02 , A61P7/04 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/08 , A61P13/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/14 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/06 , A61P31/10 , A61P31/12 , A61P31/14 , A61P31/16 , A61P31/18 , A61P31/22 , A61P33/00 , A61P33/02 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/06 , A61P43/00 , C07C215/76 , C07C215/78 , C07C217/58 , C07C233/25 , C07C233/62 , C07C233/75 , C07C271/28 , C07C275/34 , C07C275/36 , C07C275/40 , C07C275/42 , C07C311/08 , C07C311/13 , C07C317/32 , C07C323/32 , C07C323/37 , C07C323/41 , C07C335/18 , C07D213/75 , C07D215/36 , C07D233/64 , C07D235/14 , C07D277/66 , C07D295/18 , C07D307/52 , C07D307/68 , C07D317/60 , C07D317/66 , C07D333/28 , C07D333/34
CPC分类号： A61K31/155 , A61K31/135 , A61K31/165 , A61K31/17 , A61K31/18
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-Ll-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各自并且独立地选自C （S） - ， - C（O）-NR 10 - ， - C（S）-NR 11 - ，-C（N-CN）-NR 12 - ， - S O2） - ， - S（O）-NR13-和S（O2）-NR14-，-O - ， - S-或各自并且各自不存在; X是间隔基并且独立地选自包含-M1-L1-K-L2-M2-的基团，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，多取代的多不饱和杂环基，单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，不同于肽或不存在。

8. 发明申请

WO2004030664A3 NEW COMPOUNDS FOR THE INHIBITION OF UNDESIRED CELL PROLIFERATION AND USE THEREOF 审中-公开
标题翻译：用于抑制不希望的细胞增殖的新化合物及其用途
公开(公告)号：WO2004030664A3
公开(公告)日：2004-08-12
申请号：PCT/EP0310415
申请日：2003-09-18
申请人： JERINI AG , KNOLLE JOCHEN , SCHUTKOWSKI MIKE , HUMMEL GERD , TRADLER THOMAS , JOBRON LAURENCE , CHRISTNER CLAUDIA , SCHARN DIRK , STRAGIES ROLAND , GIBSON CHRISTOPH , OSTERKAMP FRANK
发明人： KNOLLE JOCHEN , SCHUTKOWSKI MIKE , HUMMEL GERD , TRADLER THOMAS , JOBRON LAURENCE , CHRISTNER CLAUDIA , SCHARN DIRK , STRAGIES ROLAND , GIBSON CHRISTOPH , OSTERKAMP FRANK
IPC分类号： A61K31/17 , A61P43/00
CPC分类号： A61K31/17
摘要： The present invention is related to a compound of the formula (I), (II), (III), (IV) or (V).
摘要翻译：本发明涉及式（I），（II），（III），（IV）或（V）的化合物。

9. 发明专利

BRPI0809231A2 未知
公开(公告)号：BRPI0809231A2
公开(公告)日：2014-09-02
申请号：BRPI0809231
申请日：2008-03-22
申请人： JERINI AG
发明人： GIBSON CHRISTOPH , TRADLER THOMAS , SCHNATBAUM KARSTEN , PFEIFER JOCHEN , LOCARDI ELSA , SCHARN DIRK , PASCHKE MATTHIAS , REIMER ULF , RICHTER UWE , HUMMEL GERD , REINEKE ULRICH
IPC分类号： C07D401/14 , A61K31/4709 , A61P29/00 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is related to a compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein A is a 6-membered heteroaryl having 1 heteroatom, wherein said heteroatom is N, and R 5 -R 8 ; R 17 are as defined in the claims, and their use as bradykinin B 2 receptor modulators.

10. 发明专利

BRPI0706800A2 未知
公开(公告)号：BRPI0706800A2
公开(公告)日：2011-04-05
申请号：BRPI0706800
申请日：2007-01-31
申请人： JERINI AG
发明人： ZISCHINSKY GUNTER , STRAGIES ROLAND , OSTERKAMP FRANK , SCHARN DIRK , HUMMEL GERD , KALKHOF HOLGER , ZAHN GRIT , VOSSMEYER DOERTE , CRISTNER-ALBRECHT CLAUDIA , REINEKE ULRICH
IPC分类号： C07D401/12 , A61K31/4545 , A61P35/00 , 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.

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