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1. 发明授权

US07632951B2 Inhibitors of integrin ανβ6 失效
标题翻译：整合素alphanubeta6的抑制剂
公开(公告)号：US07632951B2
公开(公告)日：2009-12-15
申请号：US10471836
申请日：2002-02-21
申请人： Oliver Schadt , Alfred Jonczyk , Wolfgang Staehle , Simon Goodman
发明人： Oliver Schadt , Alfred Jonczyk , Wolfgang Staehle , Simon Goodman
IPC分类号： A61K31/44 , C07D213/02
CPC分类号： C07D213/74 , C07D401/12 , C07D409/12
摘要： Novel biphenyl derivatives of the general formula (I) in which R1, R1′, R1″, R2, R2′, R3 and n are as defined in claim 1, their stereoisomers and their physiologically acceptable salts or solvates are novel integrin inhibitors which preferentially inhibit the αvβ6 integrin receptor. The novel compounds can be used, in particular, as medicaments.
摘要翻译：通式（I）的新型联苯衍生物，其中R 1，R 1'，R 1“，R 2，R 2'，R 3和n如权利要求1中所定义，其立体异构体及其生理学上可接受的盐或溶剂化物是新的整联蛋白抑制剂优先抑制alphavbeta6整联蛋白受体。新化合物特别可用作药物。

2. 发明授权

US07138417B2 Inhibitors of integrin αvβ6 有权
标题翻译：整合素alphavbeta6的抑制剂
公开(公告)号：US07138417B2
公开(公告)日：2006-11-21
申请号：US10503616
申请日：2003-01-15
申请人： Wolfgang Staehle , Oliver Schadt , Alfred Jonczyk , Simon Goodman
发明人： Wolfgang Staehle , Oliver Schadt , Alfred Jonczyk , Simon Goodman
IPC分类号： C07D213/74 , A61K31/4402
CPC分类号： C07D213/74
摘要： Novel biphenyl derivatives of the general formula I in which R1, R1′, R1″, R2, R2′, R3 and n are as defined in Patent claim 1, stereoisomers thereof and physiologically acceptable salts or solvates thereof are novel integrin inhibitors which preferentially inhibit the αvβ6 integrin receptor. The novel compounds can be used, in particular, as medicaments
摘要翻译：通式I的新型联苯衍生物，其中R 1，R 1，R 2，R 1'，R 2， R 3和R 2如专利权利要求1中所定义，其立体异构体和其生理学上可接受的盐或溶剂合物是新的整联蛋白抑制剂，其优先抑制α2/ β6整联蛋白受体。新化合物特别可用作药物

3. 发明授权

US07135587B2 Urea and urethane derivatives as integrin inhibitors 有权
标题翻译：尿素和尿烷衍生物作为整联蛋白抑制剂
公开(公告)号：US07135587B2
公开(公告)日：2006-11-14
申请号：US10450855
申请日：2001-11-30
申请人： Wolfgang Staehle , Alfred Jonczyk , Oliver Schadt , Simon Goodman
发明人： Wolfgang Staehle , Alfred Jonczyk , Oliver Schadt , Simon Goodman
IPC分类号： C07C229/00
CPC分类号： C07D213/74 , C07D235/30
摘要： Novel urea and urethane derivatives of general formula (I) in which R1, R2, R3, R5, R5′, X, Y, B, m, n and o are as defined in Patent Claim 1, and physiologically acceptable salts or solvates thereof are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumors. Osteoporosis, infections and restenosis after angioplasty or in pathological processes maintained or propagated by antiogenesis.
摘要翻译：其中R1，R2，R3，R5，R5'，X，Y，B，m，n和o如专利权利要求1中所定义的通式（I）的新型尿素和氨基甲酸酯衍生物及其生理学上可接受的盐或溶剂合物是整联蛋白抑制剂，可用于对抗血栓形成，心肌梗死，冠心病，动脉硬化，炎症，肿瘤。血管成形术后的骨质疏松症，感染和再狭窄或通过抗血管生成保持或传播的病理过程。

4. 发明申请

US20050153902A1 Inhibitors of integrin avb6 有权
标题翻译：整合素avb6的抑制剂
公开(公告)号：US20050153902A1
公开(公告)日：2005-07-14
申请号：US10503616
申请日：2003-01-15
申请人： Wolfgang Staehle , Oliver Schadt , Alfred Jonczyk , Simon Goodman
发明人： Wolfgang Staehle , Oliver Schadt , Alfred Jonczyk , Simon Goodman
IPC分类号： A61K31/44 , A61K31/4402 , A61P1/04 , A61P1/18 , A61P3/14 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P13/02 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P35/00 , C07D213/74 , A61K38/04 , C07D213/72
CPC分类号： C07D213/74
摘要： Novel biphenyl derivatives of the general formula I in which R1, R1′, R1″, R2, R2′, R3 and n are as defined in Patent claim 1, stereoisomers thereof and physiologically acceptable salts or solvates thereof are novel integrin inhibitors which preferentially inhibit the αvβ6 integrin receptor. The novel compounds can be used, in particular, as medicaments.
摘要翻译：通式I的新型联苯衍生物，其中R 1，R 1，R 1，R 2，R 2， R 3和R 2如在专利权利要求1中所定义，其立体异构体和其生理学上可接受的盐或溶剂合物是优选抑制α-角蛋白6整联蛋白受体的新型整联蛋白抑制剂。新化合物特别可用作药物。

5. 发明授权

US06645991B1 &agr;v&bgr;3 integrin inhibitors 失效
标题翻译： alphavbeta3整合素抑制剂
公开(公告)号：US06645991B1
公开(公告)日：2003-11-11
申请号：US10069187
申请日：2002-06-21
申请人： Alfred Jonczyk , Oliver Schadt , Simon Goodman
发明人： Alfred Jonczyk , Oliver Schadt , Simon Goodman
IPC分类号： C07D21374
CPC分类号： C07D213/74
摘要： The invention describes novel compounds of the formula I which are biologically active as ligands of integrin &agr;v&bgr;3 X—Y—Z—R1—CH2—R2(R4)—CH2—CO—R5 in which X, Y, Z, R1, R2, R4 and R5 are as defined in claim 1, and their physiologically acceptable salts and solvates.
摘要翻译：本发明描述了具有生物活性的新颖的式I化合物，其作为整合素α2β2的配体，其中X，Y，Z，R 1，R 2，R 4和R 5如权利要求1中所定义，及其生理上可接受的盐和溶剂合物。

6. 发明授权

US06683051B1 Pharmaceutical preparation containing a cyclopeptide and a chemotherapeutic agent or an angiogenesis inhibitor 有权
标题翻译：含有环肽和化学治疗剂或血管发生抑制剂的药物制剂
公开(公告)号：US06683051B1
公开(公告)日：2004-01-27
申请号：US09787374
申请日：2001-06-04
申请人： Alfred Jonczyk , Astrid Perschl , Simon Goodman , Sigrid Rösener , Jutta Haunschild
发明人： Alfred Jonczyk , Astrid Perschl , Simon Goodman , Sigrid Rösener , Jutta Haunschild
IPC分类号： A61K3800
CPC分类号： A61K38/12 , A61K2300/00
摘要： The invention relates to a pharmaceutical preparation [lacuna] cyclo(Arg-Gly-Asp-D-Phe-NMe-Val) and/or one of its physiologically acceptable salts and at least one chemotherapeutic agent and/or one of its physiologically acceptable salts and/or an angiogenesis inhibitor and/or one of its physiologically acceptable salts.
摘要翻译：本发明涉及药物制剂[lacuna]环（Arg-Gly-Asp-D-Phe-NMe-Val）和/或其生理上可接受的盐和至少一种化学治疗剂之一和/或其生理上可接受的盐之一和/或血管发生抑制剂和/或其生理上可接受的盐之一。

7. 发明授权

US6001961A Cyclic adhesion inhibitors 失效
标题翻译：环状粘连抑制剂
公开(公告)号：US6001961A
公开(公告)日：1999-12-14
申请号：US694387
申请日：1996-09-16
申请人： Alfred Jonczyk , Simon Goodman , Beate Diefenbach , Arne Sutter , Gunter Holzemann , Horst Kessler , Michael Dechantsreiter
发明人： Alfred Jonczyk , Simon Goodman , Beate Diefenbach , Arne Sutter , Gunter Holzemann , Horst Kessler , Michael Dechantsreiter
IPC分类号： A61K38/00 , A61K38/04 , A61K38/12 , A61P9/00 , A61P31/04 , A61P35/00 , A61P35/04 , A61P39/00 , A61P43/00 , C07K1/113 , C07K7/64 , C07K7/00
CPC分类号： C07K7/64 , A61K38/00
摘要： The invention relates to novel cyclopeptides of the formula Icyclo-(nArg-nGly-nAsp-nD-nE) I,in whichD and E in each case independently of one another are Gly, Ala, .beta.-Ala, Asn, Asp, Asp(OR), Arg, Cha, Cys, Gln, Glu, His, Ile, Leu, Lys, Lys(Ac), Lys(AcNH.sub.2), Lys(AcSH), Met, Nal, Nle, Orn, Phe, 4-Hal-Phe, homo-Phe, Phg, Pro, Pya, Ser, Thr, Tia, Tic, Trp, Tyr or Val, which amino acid residues can also be derivatized,R is alkyl having 1-18 carbon atoms,Hal is F, Cl, Br, I,Ac is alkanoyl having 1-10 carbon atoms, aroyl having 7-11 carbon atoms or aralkanoyl having 8-12 carbon atoms,n denotes no substituent or an alkyl radical R, benzyl or an aralkyl radical having 7-18 carbon atoms on the alpha-amino function of the relevant amino acid residue,with the proviso that at least one amino acid residue has a substituent n and that, where residues of optically active amino acids and amino acid derivatives are involved, both the D and the L forms are included, and also their physiologically acceptable salts.These compounds act as integrin inhibitors and can be used in particular for the prophylaxis and treatment of disorders of the circulation, angiogenic disorders, microbial infections and in tumor therapy.
摘要翻译：本发明涉及式I环 - （nArg-nGly-nAsp-nD-nE）I的新型环肽，其中D和E各自独立地为Gly，Ala，β-Ala，Asn，Asp，Asp （OR），Arg，Cha，Cys，Gln，Glu，His，Ile，Leu，Lys，Lys（Ac），Lys（AcNH 2），Lys（AcSH），Met，Nal，Nle，Orn， -Phe，Phe-Phe，Phg，Pro，Pya，Ser，Thr，Tia，Tic，Trp，Tyr或Val，该氨基酸残基也可被衍生化，R是具有1-18个碳原子的烷基，Hal是F， Cl，Br，I，Ac是具有1-10个碳原子的烷酰基，具有7-11个碳原子的芳酰基或具有8-12个碳原子的芳烷酰基，n表示没有取代基或烷基R，苄基或具有7- 相关氨基酸残基的α-氨基官能团上的18个碳原子，条件是至少一个氨基酸残基具有取代基n，并且当涉及光学活性氨基酸和氨基酸衍生物的残基时，D 并且包括L形式，也包括它们的生理学可接受的盐。这些化合物用作整联蛋白抑制剂，特别可用于预防和治疗循环障碍，血管生成障碍，微生物感染和肿瘤治疗。

8. 发明申请

US20070117849A1 Alfavbeta3 and alfavbet6 integrin antagonists as antifibrotic agents 审中-公开
标题翻译： Alfavbeta3和alfavbet6整合素拮抗剂作为抗纤维化剂
公开(公告)号：US20070117849A1
公开(公告)日：2007-05-24
申请号：US10574215
申请日：2004-09-16
申请人： Simon Goodman , Detlef Schuppan , Eleonora Patsenker , Yury Popov , Michael Bauer , Matthias Wiesner , Alfred Jonczyk
发明人： Simon Goodman , Detlef Schuppan , Eleonora Patsenker , Yury Popov , Michael Bauer , Matthias Wiesner , Alfred Jonczyk
IPC分类号： A61K31/4439 , A61K31/44
CPC分类号： A61K31/00
摘要： This invention relates to inhibition of αv integrins, especially αvβ3 and αvβ6 integrins, by specific antagonists, preferably non-peptidic antagonists, related compounds and compounds with comparable specificity, that downregulate fibrogenesis by inhibiting cell migration and production of pro-fibrogenic molecules (e.g., collagens, TIMP-1) and cytokines (e.g., CTGF) by activated hepatic stellate cells/myofibroblasts, activated epithelia and endothelia. These antagonists alone or in combination with other agents can effectively prevent, mitigate or even reverse development of advanced fibrosis, such as fibrosis/cirrhosis of the liver and fibrosis of other organs, such as lungs, kidneys, intestine, pancreas, skin and arteries.
摘要翻译：本发明涉及通过特异性拮抗剂，优选非肽拮抗剂，相关化合物和具有相当特异性的化合物抑制alphav整合素，特别是alphavbeta3和alphavbeta6整联蛋白，通过抑制细胞迁移和产生促纤维化分子来下调纤维发生（例如，胶原，TIMP-1）和活化的肝星状细胞/肌成纤维细胞，活化的上皮细胞和内皮细胞因子（例如CTGF）。这些单独的或与其它药剂组合的拮抗剂可以有效地预防，减轻或甚至逆转晚期纤维化的发展，例如肝纤维化/肝硬化和其他器官如肺，肾，肠，胰腺，皮肤和动脉的纤维化。

9. 发明授权

US06127335A Cyclic adhesion inhibitors 有权
标题翻译：环状粘连抑制剂
公开(公告)号：US06127335A
公开(公告)日：2000-10-03
申请号：US155721
申请日：1999-04-08
申请人： Alfred Jonczyk , Simon Goodman , Beate Diefenbach , Horst Kessler , Marcus Koppitz
发明人： Alfred Jonczyk , Simon Goodman , Beate Diefenbach , Horst Kessler , Marcus Koppitz
IPC分类号： A61K38/00 , A61K31/00 , A61K38/12 , A61P7/02 , A61P31/00 , A61P31/04 , A61P35/00 , B01D15/08 , B01J20/281 , C07K1/22 , C07K7/64 , C07K14/75 , C07K14/78 , G01N30/88 , C07K5/12
CPC分类号： C07K7/64 , C07K14/75 , A61K38/00
摘要： The invention concerns cyclopeptides of formula (I): Cyclo-(Arg-Gly-Asp-X-Y) in which X is Cha, Nal, Phe, 2-R.sup.1 -Phe, 3-R.sup.1 -Phe, 4-R.sup.1 -Phe, homo-Phe, Phg, Thi, Trp, Tyr or derivatives of Tyr, whereby the OH group can be etherified by alkyl groups containing 1-18 C-atoms and the amino-acid groups given can also be derivatives, R.sup.1 is NH.sub.2, NO.sub.2, I Br, Cl, F, alkyl with 1-18 C-atoms, Ar, Ar--O or.sup.3 H, Y is Gly in which the .alpha. N-atom may be substituted by R.sup.2 and/or the .alpha. C-atom may be substituted by R.sup.3 and/or R.sup.4, with the provision that Gly has at least one of the substituents specified, Ar is phenyl which may be substituted by one or two of groups NH.sub.2, NO.sub.2, I, Br, Cl, F, alkyl with 1-6 C-atoms or .sup.3 H, R.sup.2, R.sup.3 or R.sup.4, independently of each other, are alkyl with 1-18 C-atoms or R.sup.2 and R.sup.3 or R.sup.3 and R.sup.4 together in each case are a branched or unbranched alklyene chain with 3 to 18 C-atoms so that either the .alpha. N-atom or the .alpha. C-atom together with the alkylene chain, or the .alpha. C-atom alone, forms a ring with alkylene chain, whereby, when optically active amino-acid or amino-acid-derivative groups are involved, both the D- and the L-form are included, plus derivatives, in particular the .beta.-ester of aspartic acid or N-guanidine acyl derivatives of arginine or prodrug as well as their physiologically acceptable salts. These compounds act as integrin inhibitors and may be used particularly for the prophylaxis and treatment of circulatory and angiogenic conditions and microbial infections as well as in tumor therapy.
摘要翻译： PCT No.PCT / EP97 / 01657 Sec。 371日期1999年4月8日 102（e）1999年4月8日PCT PCT 1997年4月2日PCT公布。公开号WO97 / 38009 日期：1997年10月16日本发明涉及式（I）的环肽：其中X为Cha，Nal，Phe，2-R1-Phe，3-R1-Phe，4- R1-Phe，hom-Phe，Phg，Thi，Trp，Tyr或Tyr的衍生物，其中OH基团可以被含有1-18个C原子的烷基醚化，并且所给出的氨基酸基团也可以是衍生物，R1 是NH 2，NO 2，I Br，Cl，F，具有1-18个C原子的烷基，Ar，Ar-O或3 H，Y是其中αN原子可以被R 2和/或αC- 原子可以被R 3和/或R 4取代，条件是Gly具有至少一个指定的取代基，Ar是可被一个或两个NH 2，NO 2，I，Br，Cl，F，具有1-6个C原子的烷基或3H，R 2，R 3或R 4彼此独立地是具有1-18个碳原子的烷基或者R 2，R 3或R 3和R 4在每种情况下一起是支链或非支链烷基链具有3至18个C原子，使得αN原子或αC原子与亚烷基链一起，或者单独的αC原子形成具有亚烷基链的环，由此当涉及光学活性氨基酸或氨基酸衍生物基团时，包括D-和L-形式，加上衍生物，特别是β 的天冬氨酸或精氨酸或前药的N-胍酰基衍生物及其生理上可接受的盐。这些化合物作为整合素抑制剂起作用，可用于预防和治疗循环和血管生成病症和微生物感染以及肿瘤治疗。

10. 发明授权

US5693612A Cyclopeptides of the formula I 失效
标题翻译：式I的环肽
公开(公告)号：US5693612A
公开(公告)日：1997-12-02
申请号：US430238
申请日：1995-04-28
申请人： Alfred Jonczyk , Gunter Holzemann , Simon Goodman , Horst Kessler , Roland Haubner , Jochen Wermuth
发明人： Alfred Jonczyk , Gunter Holzemann , Simon Goodman , Horst Kessler , Roland Haubner , Jochen Wermuth
IPC分类号： A61K38/00 , A61K38/08 , A61K38/12 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P19/10 , A61P31/00 , A61P35/00 , A61P43/00 , C07K1/22 , C07K5/02 , C07K5/10 , C07K5/12 , C07K7/52 , C07K7/64 , C07K14/75
CPC分类号： C07K14/75 , C07K5/1019 , C07K7/52 , A61K38/00 , Y10S930/27
摘要： The invention relates to novel cyclopeptides of the formula I cyclo-(Arg-A-Asp-R.sup.1 -R.sup.2) I in which A, R.sup.1 and R.sup.2 have the meaning given in claim 1, and their salts. These compounds act as integrin inhibitors and can be used in particular for the prophylaxis and treatment of disorders of the circulation, bones and in tumour therapy, and as antimicrobial and antiviral active compounds.
摘要翻译：本发明涉及式I环 - （Arg-A-Asp-R1-R2）Iin的新型环肽，其中A，R 1和R 2具有权利要求1中给出的含义及其盐。这些化合物用作整联蛋白抑制剂，特别可用于预防和治疗循环障碍，骨骼和肿瘤治疗以及抗微生物和抗病毒活性化合物。

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