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11 条记录 (耗时 0.028 秒)

    Device used in parallel microsynthesis
    1.
    发明授权
    Device used in parallel microsynthesis 有权
    平行微合成中使用的装置

    公开(公告)号：US07132081B2

    公开(公告)日：2006-11-07

    申请号：US10296056

    申请日：2001-04-27

    申请人： Beate Diefenbach ,  Holger Deppe ,  Hanns Wurziger ,  Alexander Gross ,  Gregor Schlingloff ,  Andreas Schober ,  Dirk Tomandl

    发明人： Beate Diefenbach ,  Holger Deppe ,  Hanns Wurziger ,  Alexander Gross ,  Gregor Schlingloff ,  Andreas Schober ,  Dirk Tomandl

    IPC分类号： B01L3/00

    CPC分类号： B01L3/50853 ,  B01J19/0046 ,  B01J2219/00286 ,  B01J2219/00317 ,  B01J2219/00333 ,  B01J2219/00585 ,  B01L3/50857 ,  B01L2300/0819 ,  C40B60/14

    摘要： Microwells, which are open on both sides and are arranged two-dimensionally in a microwell matrix (4), are hermetically closed by pressure on both sides using plugs (6) covered with a sealing sheet (11). A layer of elastic material (9), which is arranged between the plug (6) and the sealing sheet (11), guarantees uniform pressure on all the microwells of a microwell matrix (4) which is loosely held by a frame structure (1). Continuous peripheral elevations (2), which protrude in both directions at right angles to the plane of the microwell matrix (4), ensure that the deformable thin layer of elastic material (9) does not escape sideways between the plug (6) and the microwell matrix (4) during the pressing process. A plurality of microwell matrices (4) are held simultaneously by the frame structure (1) and are hermetically closed by a corresponding number of allocated plugs (6), which are fastened to a base plate (7) and a cover plate (8), respectively.

    摘要翻译： 在两侧开口并且在微孔矩阵（4）中二维布置的微孔通过用密封片（11）覆盖的塞子（6）在两侧通过压力气密封闭。 布置在塞子（6）和密封片（11）之间的一层弹性材料（9）保证了均匀的压力，所述的微孔基体（4）的所有微孔被框架结构（1）松动地保持 ）。 在与微孔矩阵（4）的平面成直角的两个方向上突出的连续周边高度（2）确保弹性材料（9）的可变形薄层不会在插头（6）和 微孔基质（4）。 多个微孔矩阵（4）由框架结构（1）同时保持，并被相应数量的分配的塞子（6）气密地封闭，该插头固定到基板（7）和盖板（8）上， ， 分别。

    Soluble recombinant αvβ3 adhesion receptor
    4.
    发明授权
    Soluble recombinant αvβ3 adhesion receptor 有权
    可溶性重组αv＆bgr 3粘附受体

    公开(公告)号：US08067197B2

    公开(公告)日：2011-11-29

    申请号：US10460672

    申请日：2003-06-13

    申请人： Simon L. Goodman ,  Beate Diefenbach ,  Detelv Güssow ,  Raj Mehta ,  Eilish Cullen ,  Alex Brown

    发明人： Simon L. Goodman ,  Beate Diefenbach ,  Detelv Güssow ,  Raj Mehta ,  Eilish Cullen ,  Alex Brown

    IPC分类号： C12N15/09 ,  C07H21/04

    CPC分类号： C07K14/70557 ,  C12N2799/026

    摘要： The invention relates to a novel purified recombinant αVβ3 adhesion receptor which shows an unimpaired ligand binding activity, and a process for preparing said soluble non-membrane bound receptor in excellent yields by recombinant techniques using a baculovirus-insect cell expression system. The so-synthesized soluble receptor may be used very easily as screening tool for new therapeutic compounds which may inhibit the natural αVβ3 adhesion receptor. Such therapeutic compounds which can be discovered very easily, fast and without health risk by means of the soluble receptors according to the invention may be, for example, RGD peptides or non-peptidic compounds mimicking the natural ligand epitopes. The invention relates, furthermore, to a corresponding process for preparing recombinant full-length αVβ3 adhesion receptor in excellent yields, additionally using detergents to dissolve the membrane bound receptor from the surface of the host cell.

    摘要翻译： 本发明涉及一种新型纯化的重组αVb-3粘附受体，其显示出未受损的配体结合活性，以及​​通过使用杆状病毒 - 昆虫细胞表达系统的重组技术以优异的产率制备所述可溶性非膜结合受体的方法。 如此合成的可溶性受体可以非常容易地用作可能抑制天然αV和bgr 3粘附受体的新的治疗化合物的筛选工具。 可以通过本发明的可溶性受体非常容易，快速且没有健康风险发现的这种治疗化合物可以是例如RGD肽或模仿天然配体表位的非肽化合物。 此外，本发明还涉及以优异的产率制备重组全长αV＆bgr 3粘附受体的相应方法，另外使用洗涤剂从宿主细胞表面溶解膜结合受体。

    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
    8.
    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
    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。

    Cyclic adhesion inhibitors
    10.
    发明授权
    Cyclic adhesion inhibitors 失效
    环状粘连抑制剂

    公开(公告)号：US5866540A

    公开(公告)日：1999-02-02

    申请号：US368760

    申请日：1995-01-04

    申请人： Alfred Jonczyk ,  Gunter Holzemann ,  Brunhilde Felding-Habermann ,  Guido Melzer ,  Beate Diefenbach ,  David A. Cheresh ,  Horst Kessler ,  Marion Gurrath ,  Gerhard Muller

    发明人： Alfred Jonczyk ,  Gunter Holzemann ,  Brunhilde Felding-Habermann ,  Guido Melzer ,  Beate Diefenbach ,  David A. Cheresh ,  Horst Kessler ,  Marion Gurrath ,  Gerhard Muller

    IPC分类号： A61K38/00 ,  A61K38/12 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P17/02 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07K7/64 ,  C07K14/75 ,  C07K14/78 ,  C07K7/54

    CPC分类号： C07K14/75 ,  C07K14/78 ,  A61K38/00

    摘要： The present invention relates to pharmaceutical compositions which contain at least one cyclopeptide of formula I (a)-(r):(a) cyclo(-Arg-Gly-Asp-D-Phe-Val-Ala);(b) cyclo(-Arg-Gly-Asp-D-Phe-Leu-Ala);(c) cyclo(-Arg-Gly-Asp-Phe-Val-D-Ala);(d) cyclo(-Arg-Gly-Asp-Phe-Leu-D-Ala);(e) cyclo(-Arg-Gly-Asp-D-Phe-Val-Gly);(f) cyclo(-Arg-Gly-Asp-D-Phe-Leu-Gly);(g) cyclo(-D-Arg-Gly-Asp-Phe-Val-Ala);(h) cyclo(-D-Arg-Gly-Asp-Phe-Val-Gly);(i) cyclo(-Arg-Gly-Asp-Phe-Pro-Gly);(j) cyclo(-Arg-Gly-Asp-Phe-D-Pro-Gly);(k) cyclo(-Arg-Gly-Asp-Phe-Pro-Ala);(l) cyclo(-Arg-Gly-Asp-Phe-D-Pro-Ala);(m) cyclo(-D-Arg-Gly-Asp-Phe-Val);(n) cyclo(-Arg-D-Ala-Asp-Phe-Val);(o) cyclo(-Arg-Gly-Asp-D-Phe-Val);(p) cyclo(-Arg-Ala-Asp-D-Phe-Val);(q) cyclo(-Arg-Gly-Asp-Phe-D-Val);(r) cyclo(-Arg-Gly-D-Asp-Phe-Val);or a salt thereof. The pharmaceutical compositions can be used as cell adhesion inhibitors, e.g., in the treatment of thrombosis, myocardial infarct, apoplexy, arteriosclerosis, inflammations, angina pectoris, and/or tumors.

    摘要翻译： 本发明涉及含有至少一种式I（a） - （r）的环肽的药物组合物：（a）环（-Arg-Gly-Asp-D-Phe-Val-Ala）; （b）环（-Arg-Gly-Asp-D-Phe-Leu-Ala）; （c）环（-Arg-Gly-Asp-Phe-Val-D-Ala）; （d）环（-Arg-Gly-Asp-Phe-Leu-D-Ala）; （e）环（-Arg-Gly-Asp-D-Phe-Val-Gly）; （f）环（-Arg-Gly-Asp-D-Phe-Leu-Gly）; （g）环（-D-Arg-Gly-Asp-Phe-Val-Ala）; （h）环（-D-Arg-Gly-Asp-Phe-Val-Gly）; （i）环（-Arg-Gly-Asp-Phe-Pro-Gly）; （j）环（-Arg-Gly-Asp-Phe-D-Pro-Gly）; （k）环（-Arg-Gly-Asp-Phe-Pro-Ala）; （1）环（-Arg-Gly-Asp-Phe-D-Pro-Ala）; （m）环（-D-Arg-Gly-Asp-Phe-Val）; （n）环（-Arg-D-Ala-Asp-Phe-Val）; （o）环（-Arg-Gly-Asp-D-Phe-Val）; （p）环（-Arg-Ala-Asp-D-Phe-Val）; （q）环（-Arg-Gly-Asp-Phe-D-Val）; （r）环（-Arg-Gly-D-Asp-Phe-Val）; 或其盐。 药物组合物可用作细胞粘附抑制剂，例如用于治疗血栓形成，心肌梗塞，中风，动脉硬化，炎症，心绞痛和/或肿瘤。