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    Cyclic azapeptides with angiogenic effect
    1.
    发明授权
    Cyclic azapeptides with angiogenic effect 失效
    具有血管生成作用的环状氮杂肽

    公开(公告)号：US06534478B1

    公开(公告)日：2003-03-18

    申请号：US09446974

    申请日：2000-03-23

    申请人： Alfred Jonczyk ,  Simon Goodman ,  Horst Kessler ,  Jochen Wermuth ,  Jörg Schmitt

    发明人： Alfred Jonczyk ,  Simon Goodman ,  Horst Kessler ,  Jochen Wermuth ,  Jörg Schmitt

    IPC分类号： A61K3800

    CPC分类号： C07K7/56 ,  A61K38/00

    摘要： Compounds of the formula I cyclo-(aArg-aGly-aAsp-aX-aY)  I in which aArg, aGly, aAsp, aX and aY have the meanings indicated in claim 1, and their salts, can be used as integrin inhibitors, in particular for the prophylaxis and treatment of diseases of the circulation, in thrombosis, cardiac infarct, coronary heart diseases, arteriosclerosis, in pathological processes which are supported or propagated by angiogenesis and in tumour therapy.

    摘要翻译： aArg，aGly，aAsp，aX和aY具有权利要求1所述含义的式Ⅰin化合物及其盐可用作整联蛋白抑制剂，特别是用于预防和治疗血栓形成疾病， 心肌梗死，冠心病，动脉硬化，血管生成和肿瘤治疗支持或传播的病理过程。

    Cyclic adhesion inhibitors
    5.
    发明授权
    Cyclic adhesion inhibitors 失效
    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。

    Cyclic adhesion inhibitors
    6.
    发明授权
    Cyclic adhesion inhibitors 有权
    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。

    Cyclopeptide derivatives with integrin inhibitor properties
    8.
    发明授权
    Cyclopeptide derivatives with integrin inhibitor properties 有权
    具有整合素抑制剂性质的环肽衍生物

    公开(公告)号：US06610826B1

    公开(公告)日：2003-08-26

    申请号：US09581575

    申请日：2000-06-15

    申请人： Jörg Meyer ,  Alfred Jonczyk ,  Berthold Nies ,  Horst Kessler ,  Dirk Finsinger ,  Martin Kantlehner

    发明人： Jörg Meyer ,  Alfred Jonczyk ,  Berthold Nies ,  Horst Kessler ,  Dirk Finsinger ,  Martin Kantlehner

    IPC分类号： C07K510

    CPC分类号： C07K7/64 ,  A61K38/00 ,  Y02P20/125

    摘要： Compounds of the formula I R—Q—X  I, in which R, Q, and X are as defined herein, can be used as integrin inhibitors. In particular, compounds of formula I are suitable for the treatment of disorders caused by implants, defects, inflammations and of osteolytic disorders such as osteoporosis, thrombosis, cardiac infarct and arteriosclerosis. These compounds are also suitable for the acceleration and reinforcement of the integration process of implants and biocompatible surfaces into tissue.

    摘要翻译： R，Q和X如本文所定义的式Iin化合物可用作整联蛋白抑制剂。 特别地，式I化合物适用于治疗由植入物，缺陷，炎症和溶骨性疾病如骨质疏松症，血栓形成，心肌梗死和动脉硬化引起的疾病。 这些化合物也适用于加速和加强植入物和生物相容性表面进入组织的整合过程。

    Cyclopeptide derivatives
    9.
    发明授权
    Cyclopeptide derivatives 有权
    环肽衍生物

    公开(公告)号：US06566491B2

    公开(公告)日：2003-05-20

    申请号：US09051603

    申请日：1998-08-18

    申请人： Alfred Jonczyk ,  Simon Lawrence Goodman ,  Beate Diefenbach ,  Arne Sutter ,  Horst Kessler

    发明人： Alfred Jonczyk ,  Simon Lawrence Goodman ,  Beate Diefenbach ,  Arne Sutter ,  Horst Kessler

    IPC分类号： A61K3812

    CPC分类号： C07K7/64 ,  A61K38/00 ,  C07K14/75 ,  Y02P20/55

    摘要： The invention relates to compounds of the formula (I) R1—Q1—X—Q2—R2, in which: Q1, Q2, each independent of one another, are missing or are —NH—(CH2)n—CO—; R1, R2, each independent of one another, are missing or are cyclo-(Arg-Gly-Asp-Z), wherein Z is missing in side chain of Q1 or Q2 of if Q1 and/or Q2 missing, is bound to X, at least one of the groups R1 or R2 always having to be included; X is —CO—R18—CO—, and if R1—Q1— or R2—Q2— are missing is R10, R13, Het-CO or a flourescent pigment residue linked through a —CONH—, —COO—, NH—C(═S)—N—, —NH—C(═O)—NH—, —SO2 NH—or —NHCO— bond; and Z, R10, R13, R16, R18, Het and n have the meaning given in claim 1. The invention also relates to the salts of said compounds. These compounds and their salts can be used as integrin inhibitors, in particular for the prevention and treatment of circulatory diseases, thrombosis, heart infarct, coronary heart diseases, arteriosclerosis, angiogenic diseases and in tumor therapy.

    摘要翻译： 本发明涉及式（I）的化合物：R1-Q1-X-Q2-R2，其中：Q1，Q2彼此独立地缺失或是-NH-（CH2）n-CO-; R1，R2各自独立，缺失或是环 - （Arg-Gly-Asp-Z），其中如果Q1和/或Q2缺失，则Q1或Q2侧链中缺失Z，与X 总是必须包括R1或R2组中的至少一个; X是-CO-R18-CO-，如果R1-Q1-或R2-Q2-缺失，则是R10，R13，Het-CO或通过-CONH-，-COO-，NH-C连接的荧光色素残基 （= S）-N-，-NH-C（= O）-NH-，-SO 2 NH-或-NHCO-键; Z，R10，R13，R16，R18，Het和n具有权利要求1中给出的含义。本发明还涉及所述化合物的盐。 这些化合物及其盐可用作整联蛋白抑制剂，特别是用于预防和治疗循环系统疾病，血栓形成，心脏梗塞，冠心病，动脉硬化，血管发生疾病和肿瘤治疗。