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51. 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。

52. 发明授权

US06534478B1 Cyclic azapeptides with angiogenic effect 失效
标题翻译：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。

53. 发明授权

US06280760B1 Peptide-coated implants and methods for producing same 有权
标题翻译：肽涂覆植入物及其制备方法
公开(公告)号：US06280760B1
公开(公告)日：2001-08-28
申请号：US09423347
申请日：1999-11-22
申请人： Jorg Meyer , Alfred Jonczyk , Berthold Nies , Horst Kessler , Dirk Finsinger , Martin Kantlehner
发明人： Jorg Meyer , Alfred Jonczyk , Berthold Nies , Horst Kessler , Dirk Finsinger , Martin Kantlehner
IPC分类号： A61L2700
CPC分类号： C12N5/0068 , A61K35/12 , A61L27/34 , C12N5/0654 , C12N2533/50 , C08L89/00
摘要： The invention describes the possibility of the biofunctionalization of biomaterials, in particular implants, by their made-to-measure coating with synthesized cell- or tissue-selective RGD peptides which in vitro stimulate the adhesion of mainly those cell species which in each case are intended to accomplish the tissue integration of the appropriate biomaterial.
摘要翻译：本发明描述了通过其合成的细胞或组织选择性RGD肽的生物材料（特别是植入物）的生物功能化生物功能化的可能性，所述细胞或组织选择性RGD肽体外刺激主要在每种情况下被预期的那些细胞种类的粘附完成适当生物材料的组织整合。

54. 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。

55. 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。

56. 发明授权

US4812555A Peptides possessing renin inhibitory activity 失效
标题翻译：具有肾素抑制活性的肽
公开(公告)号：US4812555A
公开(公告)日：1989-03-14
申请号：US171973
申请日：1988-03-22
申请人： Peter Raddatz , Gunter Holzemann , Alfred Jonczyk , Claus J. Schmitges , Klaus O. Minck
发明人： Peter Raddatz , Gunter Holzemann , Alfred Jonczyk , Claus J. Schmitges , Klaus O. Minck
IPC分类号： C07K7/06 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07C67/00 , C07C231/00 , C07C237/12 , C07C237/22 , C07C239/00 , C07C269/00 , C07C301/00 , C07C303/40 , C07C309/18 , C07C313/00 , C07D233/54 , C07K1/113 , C07K5/00 , C07K5/02 , C07K5/06 , C07K5/08 , C07K5/10 , C07K14/81 , A61K37/02
CPC分类号： C07D233/64 , C07K5/00 , C07K5/0227 , Y10S530/86
摘要： New peptides of the formula IX--Z--NR.sup.2 --CHR.sup.3 --CHOH--(CHR.sup.4).sub.n --CO--Ewherein X, Z, R.sup.2, R.sup.3, R.sup.4, E and n are as defined herein and their salts inhibit the activity of human plasma renin.
摘要翻译：式XZ-NR2-CHR3-CHOH-（CHR4）n-CO-E的新肽，其中X，Z，R2，R3，R4，E和n如本文所定义，并且它们的盐抑制人血浆肾素的活性。

57. 发明授权

US08846931B2 Bipyridyl derivatives 有权
标题翻译：联吡啶衍生物
公开(公告)号：US08846931B2
公开(公告)日：2014-09-30
申请号：US13808369
申请日：2011-06-07
申请人： Guenter Hoelzemann , Dieter Dorsch , Alfred Jonczyk , Christiane Amendt , Frank Zenke
发明人： Guenter Hoelzemann , Dieter Dorsch , Alfred Jonczyk , Christiane Amendt , Frank Zenke
IPC分类号： C07D401/14 , A61K45/06 , C07D213/74 , A61K31/496 , C07D471/04 , A61K31/5377 , A61K31/444 , A61K31/4545
CPC分类号： C07D401/14 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K45/06 , C07D213/74 , C07D471/04
摘要： The present invention relates to novel bipyridyl derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.
摘要翻译：本发明涉及式（I）的新型联吡啶衍生物和其中ATP消耗蛋白质如激酶的信号转导的抑制，调节和/或调节起到特别是TGF-β抑制剂的作用的用途受体激酶，以及这些化合物用于治疗激酶诱导的疾病，特别是用于治疗肿瘤的用途。

58. 发明申请

US20140038960A1 Hetaryl-[1,8]naphthyridine derivatives 有权
标题翻译：芳基 - [1,8]萘啶衍生物
公开(公告)号：US20140038960A1
公开(公告)日：2014-02-06
申请号：US14046703
申请日：2013-10-04
申请人： Alfred Jonczyk , Dieter Dorsch , Guenter Hoelzemann , Christiane Amendt , Frank Zenke
发明人： Alfred Jonczyk , Dieter Dorsch , Guenter Hoelzemann , Christiane Amendt , Frank Zenke
IPC分类号： C07D401/14 , C07D471/04 , C07D413/14
CPC分类号： C07D471/04 , A61K31/4375 , C07D401/14 , C07D413/14 , C07D519/00
摘要： Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
摘要翻译：其中R 1，R 2，W 1，W 3，W 5和W 6具有权利要求1的含义的式（I）的新型杂芳基 - [1,8]二氮杂萘衍生物是ATP消耗蛋白质的抑制剂，用于治疗肿瘤。

59. 发明申请

US20130102603A1 2,4-DIARYL - SUBSTITUTED [1,8] NAPHTHYRIDINES AS KINASE INHIBITORS FOR USE AGAINST CANCER 有权
标题翻译： 2,4-DIARYL - 取代[1,8]萘啶类作为激酶使用抗癌剂
公开(公告)号：US20130102603A1
公开(公告)日：2013-04-25
申请号：US13807119
申请日：2011-05-31
申请人： Dieter Dorsch , Alfred Jonczyk , Guenter Hoelzemann , Christiane Amendt , Frank Zenke
发明人： Dieter Dorsch , Alfred Jonczyk , Guenter Hoelzemann , Christiane Amendt , Frank Zenke
IPC分类号： C07D491/048 , A61K31/5377 , A61K31/517 , A61K31/519 , C07D471/04 , A61K31/4375
CPC分类号： C07D491/048 , A61K31/4375 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D471/04 , C07D519/00
摘要： The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.
摘要翻译：本发明涉及式（I）的新颖的[1,8]萘啶衍生物，以及这样的化合物的用途，其中ATP消耗蛋白质如激酶的信号转导的抑制，调节和/或调节起着重要的作用，特别是 TGF-β受体激酶的抑制剂，以及这些化合物用于治疗激酶诱导的疾病，特别是用于治疗肿瘤的用途。

60. 发明申请

US20120295902A1 Hetaryl-[1,8]naphthyridine derivatives 有权
标题翻译：芳基 - [1,8]萘啶衍生物
公开(公告)号：US20120295902A1
公开(公告)日：2012-11-22
申请号：US13574282
申请日：2010-12-17
申请人： Alfred Jonczyk , Dieter Dorsch , Guenter Hoelzemann , Christiane Amendt , Frank Zenke
发明人： Alfred Jonczyk , Dieter Dorsch , Guenter Hoelzemann , Christiane Amendt , Frank Zenke
IPC分类号： C07D471/04 , A61K31/444 , A61K31/4545 , A61K31/5377 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/4375 , A61K31/501 , A61K31/538 , A61K31/4725 , C07D213/75 , C07D213/81 , C07F5/02 , C12N9/99 , A61P35/00 , A61P35/04 , A61P43/00 , A61P9/00 , A61P31/18 , A61P25/28 , A61P9/10 , A61P29/00 , A61P17/02 , A61P19/08 , A61P25/00 , A61K31/4709
CPC分类号： C07D471/04 , A61K31/4375 , C07D401/14 , C07D413/14 , C07D519/00
摘要： Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
摘要翻译：其中R 1，R 2，W 1，W 3，W 5和W 6具有权利要求1的含义的式（I）的新型杂芳基 - [1,8]二氮杂萘衍生物是ATP消耗蛋白质的抑制剂，用于治疗肿瘤。

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