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1. 发明申请

WO2008116620A1 8-OXY-QUINOLINE DERIVATIVES AS BRADYKININ B2 RECEPTOR MODULATORS 审中-公开
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：WO2008116620A1
公开(公告)日：2008-10-02
申请号：PCT/EP2008/002316
申请日：2008-03-22
申请人： JERINI AG , GIBSON, Christoph , TRADLER, Thomas , SCHNATBAUM, Karsten , PFEIFER, Jochen , LOCARDI, Elsa , SCHARN, Dirk , PASCHKE, Matthias , REIMER, Ulf , RICHTER, Uwe , HUMMEL, Gerd , REINEKE, Ulrich
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 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/4709 , A61P29/00
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。

2. 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。

3. 发明申请

WO2004030664A2 NEW COMPOUNDS FOR THE INHIBITION OF UNDESIRED CELL PROLIFERATION AND USE THEREOF 审中-公开
标题翻译：用于抑制未感染细胞增殖的新化合物及其用途
公开(公告)号：WO2004030664A2
公开(公告)日：2004-04-15
申请号：PCT/EP2003/010415
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
CPC分类号： A61K31/17 , Y02A50/401 , Y02A50/406 , Y02A50/409 , Y02A50/411 , Y02A50/465 , Y02A50/471 , 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) or (V).
摘要翻译：本发明涉及式（I），（II），（III），（IV）或（V）的化合物。

4. 发明申请

WO0214350A3 PEPTIDE AND PEPTIDE MIMETIC DERIVATIVES WITH INTEGRIN INHIBITOR PROPERTIES II 审中-公开
标题翻译：肽和拟肽衍生物与整合酶抑制剂特点II
公开(公告)号：WO0214350A3
公开(公告)日：2002-09-19
申请号：PCT/EP0108931
申请日：2001-08-02
申请人： MERCK PATENT GMBH , MEYER JOERG , NIES BERTHOLD , DARD MICHEL , HOELZEMANN GUENTER , KESSLER HORST , KANTLEHNER MARTIN , HERSEL ULRICH , GIBSON CHRISTOPH , SULYOK GABOR
发明人： MEYER JOERG , NIES BERTHOLD , DARD MICHEL , HOELZEMANN GUENTER , KESSLER HORST , KANTLEHNER MARTIN , HERSEL ULRICH , GIBSON CHRISTOPH , SULYOK GABOR
IPC分类号： A61L27/00 , A61K38/00 , A61P41/00 , C07K7/06 , C07K7/08 , C07K14/78 , A61K31/195 , A61K38/39 , A61L33/00 , C07C279/18
CPC分类号： C07K7/06 , A61K38/00 , C07K14/78 , Y02P20/125
摘要： The invention relates to compounds of formula (I) B-Q-X1, wherein B is a bioactive, cell adhesive mediating molecule, selected from the group (i) and Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys (ii), Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys (iii), Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys (iv), Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg (v), Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn (vi), Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg (vii), wherein (i) X, Y, Z, R , R , R , A, Ar, Hal, Het, Het , n, m, o, p, q, s, t have the meanings cited in Claim 1, Q is absent or is an organic spacer molecule, X1 is an anchor molecule selected from the group cited in Claim 1, and the salts thereof, which can be used as integrin inhibitors particularly for treatment of illnesses, deficiencies and inflammations caused by implants and osteolytic illnesses such as osteoporosis, thrombosis, cardiac infarction and arteriosclerosis, in addition to the acceleration and strengthening of the integration process of implants or the biocompatible surface in tissue.
摘要翻译：式（I）的化合物：BQ-X1，其中B是生物活性，zelladhäsionsvermittelndes分子从组（i）和Thr-TRP-酪氨酸 - 赖氨酸 - 异亮氨酸 - 丙氨酸 - 苯丙氨酸 - 谷氨酰胺 - 精氨酸 - 天冬酰胺 - 精氨酸 - 赖氨酸选择（ii）中，TRP-酪氨酸 - 赖氨酸 - 异亮氨酸 - 丙氨酸 - 苯丙氨酸 - 谷氨酰胺 - 精氨酸 - 天冬酰胺 - 精氨酸 - 赖氨酸（iii）中，酪氨酸 - 赖氨酸 - 异亮氨酸 - 丙氨酸 - 苯丙氨酸 - 谷氨酰胺 - 精氨酸 - 天冬酰胺 - 精氨酸 - 赖氨酸（ⅳ ），苏氨酸-TRP-酪氨酸 - 赖氨酸 - 异亮氨酸 - 丙氨酸 - 苯丙氨酸 - 谷氨酰胺 - 精氨酸 - 天冬酰胺 - 精氨酸（v），苏氨酸-TRP-酪氨酸 - 赖氨酸 - 异亮氨酸 - 丙氨酸 - 苯丙氨酸 - 谷氨酰胺 - 精氨酸 - 天冬酰胺（VI）， THR-TRP-酪氨酸 - 赖氨酸 - 异亮氨酸 - 丙氨酸 - 苯丙氨酸 - 谷氨酰胺 - 精氨酸（VII），其中对于（I）中X，Y，Z，R <2>，R <3>，R <4>中，A中，Ar 中，Hal中，Het中，Het <1>中，n，M，O，p，Q，S，T具有权利要求1中所示的含义，Q不存在或者为有机间隔分子，X 1是锚定分子，权利要求在从所选择的图1是指定的组，以及它们的盐可以用作整联蛋白抑制剂，特别是用于引起植入物，缺陷，炎症和溶骨性疾病如骨质疏松症，血栓形成，心脏梗塞和动脉粥样硬化的疾病的治疗，并且还为INTEGRA的加速和强化植入物或生物相容的表面的onsprozesses在所述组织中。

5. 发明申请

WO2007003411A3 KININ ANTAGONISTS FOR TREATING BLADDER DYSFUNCTION 审中-公开
标题翻译：用于处理刀片功能的KININ ANTAGONISTS
公开(公告)号：WO2007003411A3
公开(公告)日：2007-05-18
申请号：PCT/EP2006006504
申请日：2006-07-04
申请人： JERINI AG , GIBSON CHRISTOPH , HUMMEL GERD , KNOLLE JOCHEN , REINEKE ULRICH , TRADLER THOMAS
发明人： GIBSON CHRISTOPH , HUMMEL GERD , KNOLLE JOCHEN , REINEKE ULRICH , TRADLER THOMAS
IPC分类号： A61K45/00 , A61K38/08 , A61P13/10
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 Bl 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。

6. 发明申请

WO2005080406A3 COMPOUNDS FOR THE INHIBITION OF UNDESIRED CELL PROLIFERATION AND USE THEREOF 审中-公开
公开(公告)号：WO2005080406A3
公开(公告)日：2005-09-01
申请号：PCT/EP2004/014461
申请日：2004-12-18
申请人： JERINI AG , KNOLLE, Jochen , SCHUTKOWSKI, Mike , HUMMEL, Gerd , TRADLER, Thomas , JOBRON, Laurence , CHRISTNER, Claudia , GIBSON, Christoph , ZISCHINSKY, Gunther , RICHTER, Uwe
发明人： KNOLLE, Jochen , SCHUTKOWSKI, Mike , HUMMEL, Gerd , TRADLER, Thomas , JOBRON, Laurence , CHRISTNER, Claudia , GIBSON, Christoph , ZISCHINSKY, Gunther , RICHTER, Uwe
IPC分类号： A61K31/665
摘要： The present invention is related to compounds having the formula (I), wherein R1, R2, R3, R4, R5, X1, X2, T, U, V, W, Y and n are as defined in the claims, pharmaceutical compositions comprising the compounds and the use of the compounds for manufacturing a medicament for the use in the treatment of diseases involving an abnormal cell proliferation, an undesired cell proliferation, an abnormal mitosis and/or an undesired mitosis, the disease being selected from neurodegenerative diseases, stroke, inflammatory diseases, immune based disorders, infectious diseases, heart diseases, cardiovascular diseases and cell proliferative diseases.

7. 发明申请

WO2005063259A1 COMPOUNDS FOR THE INHIBITION OF UNDESIRED CELL PROLIFERATION AND USE THEREOF 审中-公开
标题翻译：用于抑制未感染细胞增殖的化合物及其用途
公开(公告)号：WO2005063259A1
公开(公告)日：2005-07-14
申请号：PCT/EP2004/014460
申请日：2004-12-18
申请人： JERINI AG , KNOLLE, Jochen , SCHUTKOWSKI, Mike , HUMMEL, Gerd , TRADLER, Thomas , JOBRON, Laurence , CHRISTNER, Claudia , GIBSON, Christoph , ZISCHINSKY, Gunther
发明人： KNOLLE, Jochen , SCHUTKOWSKI, Mike , HUMMEL, Gerd , TRADLER, Thomas , JOBRON, Laurence , CHRISTNER, Claudia , GIBSON, Christoph , ZISCHINSKY, Gunther
IPC分类号： A61K31/675
CPC分类号： C07F9/591 , C07F9/655354 , C07F9/65583 , C07F9/65586
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 A 1 -A 9 , Q, R 1 -R 11 , T, U, V, W 1 -W 3 , X 1 , X 2 , 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 deseases 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 -A 9，Q，R 1 -R 11， T，U，V，W 1 -W 3，X 1，X 2，Y和Z如权利要求和描述中所定义，包含该化合物的药物组合物和该化合物的用途制备用于治疗涉及异常细胞增殖，不期望的细胞增殖，异常有丝分裂和/或不期望的有丝分裂的疾病的药物。

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. 发明申请

WO2004026815A2 NEW COMPOUNDS FOR THE INHIBITION OF ROTAMASES AND USE THEREOF 审中-公开
标题翻译：酚醛衍生物及其作为ROTAMASE抑制剂的用途
公开(公告)号：WO2004026815A2
公开(公告)日：2004-04-01
申请号：PCT/EP2003/010406
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： C07C275/34
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 Z 1 , Z 2 , Z 3 and Z 4 are each and independently selected from the group comprising C(O)-, -C(S)-, -C(O)-NR 10 -, -C(S)-NR 11 -, -C(N-CN)-NR 12 -, -S(O)-, -S(O 2 )-, -S(O)-NR 13 -, and S(O 2 )-NR 14 -, -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。

10. 发明申请

WO2007003411A2 USE OF KININ ANTAGONISTS 审中-公开
标题翻译：使用KININ ANTAGONISTS
公开(公告)号：WO2007003411A2
公开(公告)日：2007-01-11
申请号：PCT/EP2006/006504
申请日：2006-07-04
申请人： JERINI AG , GIBSON, Christoph , HUMMEL, Gerd , KNOLLE, Jochen , REINEKE, Ulrich , TRADLER, Thomas
发明人： GIBSON, Christoph , HUMMEL, Gerd , KNOLLE, Jochen , REINEKE, Ulrich , TRADLER, Thomas
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 Bl 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。

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