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1. 发明授权

US06566491B2 Cyclopeptide derivatives 有权
标题翻译：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。

2. 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。

3. 发明授权

US5849692A Cyclic peptides containing Arg-Gly-Asp, and derivatives thereof, as adhesion inhibitors 失效
标题翻译：含有Arg-Gly-Asp及其衍生物的环状肽作为粘合抑制剂
公开(公告)号：US5849692A
公开(公告)日：1998-12-15
申请号：US616770
申请日：1996-03-15
申请人： Alfred Jonczyk , Gunter Holzemann , Brunhilde Felding-Habermann , Friedrich Rippmann , Beate Diefenbach , Horst Kessler , Roland Haubner , Jochen Wermuth
发明人： Alfred Jonczyk , Gunter Holzemann , Brunhilde Felding-Habermann , Friedrich Rippmann , Beate Diefenbach , Horst Kessler , Roland Haubner , Jochen Wermuth
IPC分类号： A61K38/00 , A61K38/08 , A61K38/12 , A61P9/00 , A61P19/00 , A61P35/00 , C07K1/113 , C07K1/22 , C07K7/52 , C07K7/64 , C07K14/75 , C07K14/78 , C07K17/08
CPC分类号： C07K14/75 , A61K38/00
摘要： The invention relates to novel cyclopeptides of the formula I cyclo-(Arg-B-Asp-D-E) I in which B, D, and E have the meanings defined herein, 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 and in tumor therapy.
摘要翻译：本发明涉及式I环 - （Arg-B-Asp-D-E）Iin的新型环肽，其中B，D和E具有本文定义的含义及其盐。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和肿瘤治疗。

4. 发明授权

US06169072A Cyclic adhesion inhibitors 有权
标题翻译：环状粘连抑制剂
公开(公告)号：US06169072A
公开(公告)日：2001-01-02
申请号：US09164585
申请日：1998-10-01
申请人： Alfred Jonczyk , G{umlaut over (u)}nter Hölzemann , Brunhilde Felding-Habermann , Friedrich Rippmann , Beate Diefenbach , Horst Kessler , Roland Haubner , Jochen Wermuth
发明人： Alfred Jonczyk , G{umlaut over (u)}nter Hölzemann , Brunhilde Felding-Habermann , Friedrich Rippmann , Beate Diefenbach , Horst Kessler , Roland Haubner , Jochen Wermuth
IPC分类号： A61K3800
CPC分类号： C07K14/75 , A61K38/00
摘要： The invention relates to novel cyclopeptides of the formula I cyclo-(Arg-B-Asp-D-E) I in which B, D, and E have the meanings defined herein, and their salts. These compounds act as interin inhibitors and can be used, in particular, for the prophylaxis and treatment of disorders of the circulation and in tumor therapy.
摘要翻译：本发明涉及式Iin的新型环肽，其中B，D和E具有本文定义的含义及其盐。这些化合物用作中间体抑制剂，特别可用于预防和治疗循环障碍和肿瘤治疗。

5. 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。

6. 发明授权

US5866540A Cyclic adhesion inhibitors 失效
标题翻译：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。

7. 发明授权

US5747457A Linear adhesion inhibitors 失效
标题翻译：线粘附抑制剂
公开(公告)号：US5747457A
公开(公告)日：1998-05-05
申请号：US329820
申请日：1994-10-27
申请人： Alfred Jonczyk , Brunhilde Felding-Habermann , Beate Diefenbach , Friedrich Rippmann
发明人： Alfred Jonczyk , Brunhilde Felding-Habermann , Beate Diefenbach , Friedrich Rippmann
IPC分类号： A61K38/00 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/08 , A61K38/10 , A61K38/16 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07K1/113 , C07K1/22 , C07K5/062 , C07K5/072 , C07K5/083 , C07K5/093 , C07K5/103 , C07K5/113 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/46 , C07K14/75 , C07K17/02 , A61K38/04 , C07K5/00 , C07K16/00
CPC分类号： C07K14/46 , C07K14/75 , A61K38/00
摘要： Linear peptides of the formula I X-A-Cys(R.sup.1)-B-Z I, in which A, B, R.sup.1, X and Z are as defined, are highly active inhibitors of the binding of the blood platelet integrin GP IIbIIIa (a.sub.IIb .beta..sub.3) to natural ligands and are suitable, inter alia, for the prophylaxis and for the treatment of circulatory disorders, thrombosis, myocardial infarction, coronary heart disease, arteriosclerosis, atherosclerosis, tumors and osteolytic diseases, and have a supporting effect in wound healing processes.
摘要翻译：式I XA-Cys（R1）-BZ I（其中A，B，R1，X和Z如上所定义）的线性肽是血小板整合素GP IIbIIIa（aIIbβ3）结合的高度活性抑制剂，适用于预防和治疗循环障碍，血栓形成，心肌梗死，冠心病，动脉硬化，动脉粥样硬化，肿瘤和溶骨性疾病，并且在伤口愈合过程中具有支持作用。

8. 发明授权

US5705481A Cyclopeptides 失效
标题翻译：环肽
公开(公告)号：US5705481A
公开(公告)日：1998-01-06
申请号：US436601
申请日：1995-05-08
申请人： Alfred Jonczyk , Gunter Holzemann , Brunhilde Felding-Habermann , Friedrich Rippmann , Guido Melzer , Beate Diefenbach
发明人： Alfred Jonczyk , Gunter Holzemann , Brunhilde Felding-Habermann , Friedrich Rippmann , Guido Melzer , Beate Diefenbach
IPC分类号： A61K38/00 , C07K7/64 , C07K14/75 , A61K38/08 , A61K38/12
CPC分类号： C07K14/75 , C07K7/64 , A61K38/00
摘要： The invention relates to novel cyclopeptides of the formula I cyclo-(A-B-C-D-Arg) I in which A and B are each independently of one another Ala, Asn, Asp, Arg, Cys, Gln, Glu, Gly, His, Ile, Leu, Lys, Met, Phe, Pro, Ser, Thr, Trp, Tyr or Val; C is Asp or Asp(O--C.sub.1-4 -alkyl); and D is Gly or Ala; at least two of the amino acid radicals stated being present in the D-form;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 and in tumor therapy.
摘要翻译：本发明涉及式I环 - （ABCD-Arg）Iin的新型环肽，其中A和B各自独立地为Ala，Asn，Asp，Arg，Cys，Gln，Glu，Gly，His，Ile，Leu，Lys ，Met，Phe，Pro，Ser，Thr，Trp，Tyr或Val; C是Asp或Asp（O-C 1-4 - 烷基）; D为Gly或Ala; 所述至少两个所述氨基酸基团以D-形式存在; 和它们的盐。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和肿瘤治疗。

9. 发明授权

US08067197B2 Soluble recombinant αvβ3 adhesion receptor 有权
标题翻译：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。

10. 发明授权

US06559144B2 Bicyclic amino acids 失效
标题翻译：双环氨基酸
公开(公告)号：US06559144B2
公开(公告)日：2003-05-06
申请号：US09842004
申请日：2001-04-26
申请人： Beate Diefenbach , Simon L. Goodman , Joachim März , Peter Raddatz , Friedrich Rippmann , Matthias Wiesner
发明人： Beate Diefenbach , Simon L. Goodman , Joachim März , Peter Raddatz , Friedrich Rippmann , Matthias Wiesner
IPC分类号： A61K31536
CPC分类号： C07D405/12 , C07D265/36 , C07D319/20 , C07D413/12
摘要： Compounds of the formula I in which X, Y, Z, R1, R2, R3, R4, R5, R7, R8, R11, m and n have the meanings stated in claim 1, and their physiologically acceptable salts can be used as integrin inhibitors, in particular for the prophylaxis and treatment of circulatory disorders, for thrombosis, myocardial infarct, coronary heart disease, arteriosclerosis, osteoporosis, for pathological processes maintained or propagated by angiogenesis, and in tumour therapy.
摘要翻译： X，Y，Z，R 1，R 2，R 3，R 4，R 5，R 7，R 8，R 11，m和n具有权利要求1所述含义的式Iin化合物，其生理学上可接受的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，心肌梗塞，冠心病，动脉硬化，骨质疏松症，通过血管发生维持或繁殖的病理过程以及肿瘤治疗。

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