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1. 发明授权

US06326403B1 Diacylhydrazine derivatives as integrin inhibitors 失效
标题翻译：二酰肼衍生物作为整联蛋白抑制剂
公开(公告)号：US06326403B1
公开(公告)日：2001-12-04
申请号：US09743605
申请日：2001-01-12
申请人： Günter Hölzemann , Simon Goodman , Horst Kessler , Christoph Gibson , Jörg Simon Schmitt
发明人： Günter Hölzemann , Simon Goodman , Horst Kessler , Christoph Gibson , Jörg Simon Schmitt
IPC分类号： C07C24338
CPC分类号： C07D271/113 , C07C281/06 , C07D235/30
摘要： Compounds of the formula I wherein X, Y, Z, R1 and R2 are as defined in claim 1, and their salts and solvates, can be used as integrin inhibitors in particular for the prophylaxis and treatment of circulatory disorders, for thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, for pathological processes which are maintained or propagated by angiogenesis and in tumour therapy.
摘要翻译：式I中X，Y，Z，R 1和R 2的化合物如权利要求1所定义，其盐和溶剂合物可用作整联蛋白抑制剂，特别用于预防和治疗循环系统疾病，血栓形成，心肌梗塞，冠状动脉心脏病，动脉硬化，通过血管发生和肿瘤治疗保持或传播的病理过程。

2. 发明授权

US06649613B1 Diacylhydrazine derivatives 失效
标题翻译：二酰肼衍生物
公开(公告)号：US06649613B1
公开(公告)日：2003-11-18
申请号：US10030691
申请日：2002-01-14
申请人： Günter Hölzemann , Simon Goodman , Horst Kessler , Christoph Gibson , Gabór Sulyok
发明人： Günter Hölzemann , Simon Goodman , Horst Kessler , Christoph Gibson , Gabór Sulyok
IPC分类号： C07C24338
CPC分类号： C07D213/74 , C07C243/24 , C07C279/18 , C07C281/02 , C07C2603/18
摘要： Diacylhydrazine derivatives of general formula (I) wherein X, Y, Z, R1, 2 and R3 are as defined herein, and their physiologically acceptable salts or solvates thereof, are integrin inhibitors and can be used to combat thromboses, myocardial infarcts, coronary cardiac diseases, arteriosclerosis, inflammations, tumors, osteoporosis, infections, and restenosis following angioplasty or during pathological processes that are maintained or propagated by angiogenesis.
摘要翻译：其中X，Y，Z，R 1，R 2和R 3如本文所定义的通式（I）的二酰基肼衍生物及其生理上可接受的盐或溶剂合物是整联蛋白抑制剂，可用于抗血栓形成，心肌梗死，冠心病，动脉硬化，炎症，肿瘤，骨质疏松症，感染和血管成形术后或病理过程中的再狭窄等。

3. 发明授权

US07655624B2 Peptide and peptide mimetic conjugates with integrin-inhibitor properties 有权
标题翻译：具有整合素抑制剂性质的肽和肽模拟物缀合物
公开(公告)号：US07655624B2
公开(公告)日：2010-02-02
申请号：US10344669
申请日：2001-08-02
申请人： Joerg Meyer , Berthold Nies , Michel Dard , Guenter Hoelzemann , Horst Kessler , Martin Kantlehner , Ulrich Hersel , Christoph Gibson , Gabor Sulyok
发明人： Joerg Meyer , Berthold Nies , Michel Dard , Guenter Hoelzemann , Horst Kessler , Martin Kantlehner , Ulrich Hersel , Christoph Gibson , Gabor Sulyok
IPC分类号： A61K38/12 , A61F2/02
CPC分类号： A61K47/6435 , A61K47/6425
摘要： The invention relates to compounds of formula (1) B-Q-X1, wherein B is bioactive cell adhesive mediating molecule. Q is absent or is an inorganic spacer molecule and X1 is an anchor molecule, selected from the group Lys-(CO—CH2—(CH2)n—PO3H2)2(I), -Lys-[-Lys-(CO—CH2—(CH2)a—PO3H2)2]2(ii) or -Lys-(Lys[-Lys-(CO—CH2—(CH2)n—PO3H2]2 (iii), and n independently represents 0, 1, 2 or 3, wherein a free amino group of group B is linked in peptide form to a free carboxyl group of the spacer molecule Q or of the anchor molecule X1, or a free amino group of the radical Q is linked in peptide form to a free carboxyl group of the radical X1. The invention also relates to the salts thereof. The inventive compounds can be used as integrin inhibitors for the treatment of illnesses, deficiencies, 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：本发明涉及式（1）B-Q-X1的化合物，其中B是生物活性细胞粘附介导分子。 Q不存在或是无机间隔分子，X1是选自Lys-（CO-CH 2 - （CH 2）n -PO 3 H 2）2（I），-Lys - [ - Lys-（CO-CH 2） - （CH 2）a-PO 3 H 2）2] 2（ⅱ）或-Lys-（Lys [-Lys-（CO-CH 2 - （CH 2）n -PO 3 H 2] 2（ⅲ），n独立地表示0,1,2 或3，其中B族的游离氨基以间隔分子Q或锚分子X1的游离羧基形式连接，或者基团Q的游离氨基以肽形式连接至游离氨基本发明还涉及其盐。本发明化合物可用作整联蛋白抑制剂，用于治疗由植入物引起的疾病，缺血性和溶骨性疾病如骨质疏松症，血栓形成，心肌梗塞和动脉硬化，除了加速和加强植入物或组织中生物相容性表面的整合过程。

4. 发明授权

US07276482B2 Peptide and peptide mimetic derivatives with integrin-inhibitors properties II 有权
标题翻译：具有整合蛋白抑制剂性质的肽和肽模拟衍生物II
公开(公告)号：US07276482B2
公开(公告)日：2007-10-02
申请号：US10344668
申请日：2001-08-02
申请人： Joerg Meyer , Berthold Nies , Michel Dard , Guenter Hoelzemann , Horst Kessler , Martin Kantlehner , Ulrich Hersel , Christoph Gibson , Gabor Sulyok
发明人： Joerg Meyer , Berthold Nies , Michel Dard , Guenter Hoelzemann , Horst Kessler , Martin Kantlehner , Ulrich Hersel , Christoph Gibson , Gabor Sulyok
IPC分类号： A61K38/10
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 (SEQ ID NO: 1) (ii), Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys (SEQ ID NO: 2) (iii), Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys (SEQ ID NO: 3) (iv), Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg (SEQ ID NO: 4) (v), Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn (SEQ ID NO: 5) (vi), Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg (SEQ ID NO: 6) (vii), wherein (i) X, Y, Z, R2, R3, R4, A, Ar, Hal, Het, Het1, 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 illness, 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：本发明涉及式（I）BQX 1的化合物，其中B是选自（i）和Thr-Trp-Tyr-Lys-Ile-Ala的生物活性的细胞粘附介导分子 -Ph-Gln-Arg-Asn-Arg-Lys（SEQ ID NO：1）（ii），Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys（SEQ ID NO：）（iii），Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys（SEQ ID NO：3）（iv），Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln -Arg-Asn-Arg（SEQ ID NO：4）（v），Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn（SEQ ID NO：5）（vi） -Tyr-Lys-Ile-Ala-Phe-Gln-Arg（SEQ ID NO：6）（vii），其中（i）X，Y，Z，R 2，R 3 A，Ar，Hal，Het，Het 1，n，m，o，p，q，s，t具有引用的含义在权利要求1中，Q不存在或是有机间隔分子，X 1是选自权利要求1所述的基团的锚定分子及其盐，其可以用作整联蛋白抑制剂，特别是用于治疗由植入物和溶骨性疾病引起的疾病，缺陷和炎症例如骨质疏松症，血栓形成，心肌梗死和动脉硬化，以及植入物或组织中生物相容性表面的整合过程的加速和加强。

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

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。

7. 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。

8. 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。

9. 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。

10. 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。

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