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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. 发明申请

US20080045529A1 Use Of Thienopyrimidines 审中-公开
标题翻译：噻吩并嘧啶的使用
公开(公告)号：US20080045529A1
公开(公告)日：2008-02-21
申请号：US10577908
申请日：2004-10-14
申请人： Hans-Michael Eggenweiler , Alfred Jonczyk , Gerhard Barnickel , Wilfried Rautenberg , Helga Drosdat , Arne Sutter
发明人： Hans-Michael Eggenweiler , Alfred Jonczyk , Gerhard Barnickel , Wilfried Rautenberg , Helga Drosdat , Arne Sutter
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/497 , A61P29/00 , A61P37/00 , C07D295/00 , C07D239/20 , A61P35/00 , A61P27/02 , A61K31/519
CPC分类号： C07D495/04 , A61K31/505
摘要： The invention relates to compounds of formula (I), wherein R1, R2, R3, R4, X and n have the meanings cited in claim (1). Said compounds are inhibitors of tyrosinkinases, especially TIE-2, and Raf-Kinases and can be used, for example, in the treatment of tumours.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 4， >，X和n具有权利要求（1）中引用的含义。所述化合物是酪氨酸酶，特别是TIE-2和Raf-激酶的抑制剂，可以用于例如肿瘤的治疗。

4. 发明申请

US20070225347A1 Imidazole Derivatives 审中-公开
标题翻译：咪唑衍生物
公开(公告)号：US20070225347A1
公开(公告)日：2007-09-27
申请号：US10593295
申请日：2005-03-15
申请人： Guenter Hoelzemann , Helene Crassier , Alfred Jonczyk , Wolfgang Staehle , Arne Sutter , Wilfried Rautenberg , Francesc Mitjans , Elisabet Rosell-Vives , Jaume Adan , Marta Riera
发明人： Guenter Hoelzemann , Helene Crassier , Alfred Jonczyk , Wolfgang Staehle , Arne Sutter , Wilfried Rautenberg , Francesc Mitjans , Elisabet Rosell-Vives , Jaume Adan , Marta Riera
IPC分类号： C07D233/00 , C07D233/66
CPC分类号： C07D233/90
摘要： Compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, X and X′ have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.
摘要翻译：式（I）的化合物，其中R 1，R 2，R 3，R 4， R 5，R 6，R 7，R 8，R 9， R 10，R 11，X和X'具有权利要求1所示的含义，是酪氨酸激酶，特别是TIE-2和Raf激酶的抑制剂，可以是尤其用于治疗肿瘤。

5. 发明申请

US20110244506A1 EGFR DEPENDENT MODULATION OF CHEMOKINE EXPRESSION AND INFLUENCE ON THERAPY AND DIAGNOSIS OF TUMORS AND SIDE EFFECTS THEREOF 审中-公开
标题翻译： EGFR依赖性调节化疗药物的表达及对治疗的影响及其对肿瘤及其副作用的诊断
公开(公告)号：US20110244506A1
公开(公告)日：2011-10-06
申请号：US12986490
申请日：2011-01-07
申请人： Arne Sutter , Joyce Behrens
发明人： Arne Sutter , Joyce Behrens
IPC分类号： C12Q1/02
CPC分类号： G01N33/574 , G01N33/5023 , G01N33/5082 , G01N33/57484 , G01N33/6863 , G01N33/6893 , G01N2800/20 , G01N2800/52
摘要： The invention relates to diagnosis and therapy of tumors utilizing the epidermal growth factor (EGFR) by means of chemical inhibitors or monoclonal antibodies. The invention relates also to skin irritations, preferably skin rash, in conjunction and associated with the treatment of tumor cells that utilize EGF receptor with anti-cancer agents. The invention is also directed to methods of predicting the efficiency of a tumor therapy/tumor response in a patient based on the treatment with EGFR inhibitors, especially anti-EGFR antibodies. The invention further relates to a method of determining the optimum dose of an anti-cancer agent in EGFR related tumor therapy.
摘要翻译：本发明涉及通过化学抑制剂或单克隆抗体利用表皮生长因子（EGFR）诊断和治疗肿瘤。本发明还涉及皮肤刺激，优选皮肤疹，并且与利用EGF受体与抗癌剂的肿瘤细胞的治疗有关。本发明还涉及基于用EGFR抑制剂，特别是抗EGFR抗体治疗来预测患者肿瘤治疗/肿瘤反应效率的方法。本发明还涉及确定EGFR相关肿瘤治疗中抗癌剂的最佳剂量的方法。

6. 发明申请

US20050070529A1 Use of type 4 phosphodiesterase inhibitors in myocardial diseases 审中-公开
标题翻译：在心肌疾病中使用4型磷酸二酯酶抑制剂
公开(公告)号：US20050070529A1
公开(公告)日：2005-03-31
申请号：US10467793
申请日：2002-01-15
申请人： Arne Sutter , Thomas Ehring , Thomas Welge , Klause Minck , Claudia Wilm , Michael Gassen , Hans-Michael Eggenweiler , Michael Wolf , Pierre Schelling , Norbert Beier , Joachim Leibrock
发明人： Arne Sutter , Thomas Ehring , Thomas Welge , Klause Minck , Claudia Wilm , Michael Gassen , Hans-Michael Eggenweiler , Michael Wolf , Pierre Schelling , Norbert Beier , Joachim Leibrock
IPC分类号： A61K31/50 , A61K31/501 , A61K31/535 , A61K31/5395 , A61K31/54 , A61K31/549 , A61P9/00 , A61P29/00 , A61P37/02
CPC分类号： A61K31/50 , A61K31/5395 , A61K31/549
摘要： The invention relates to the use of type 4 phosphodiesterase inhibitors to treat myocardial diseases.
摘要翻译：本发明涉及使用4型磷酸二酯酶抑制剂来治疗心肌疾病。

7. 发明申请

US20080199850A1 Egfr Dependent Modulation of Chemokine Expression and Influence on Therapy and Diagnosis of Tumors and Side Effects Thereof 审中-公开
标题翻译：趋化因子表达的Egfr依赖性调节和对肿瘤治疗和诊断及其副作用的影响
公开(公告)号：US20080199850A1
公开(公告)日：2008-08-21
申请号：US12089819
申请日：2006-10-11
申请人： Arne Sutter , Joyce Behrens
发明人： Arne Sutter , Joyce Behrens
IPC分类号： C12Q1/00
CPC分类号： G01N33/574 , G01N33/5023 , G01N33/5082 , G01N33/57484 , G01N33/6863 , G01N33/6893 , G01N2800/20 , G01N2800/52
摘要： The invention relates to diagnosis and therapy of tumors utilizinging the epidermal growth factor (EGFR) by means of chemical inhibitors or monoclonal antibodies. The invention relates also to skin irritations, preferably skin rash, in conjunction and associated with the treatment of tumor cells that utilize EGF receptor with anti-cancer agents. The invention is also directed to methods of predicting the efficiency of a tumor therapy/tumor response in a patient based on the treatment with EGFR inhibitors, especially anti-EGFR antibodies. The invention further relates to a method of determining the optimum dose of an anti-cancer agent in EGFR related tumor therapy.
摘要翻译：本发明涉及通过化学抑制剂或单克隆抗体利用表皮生长因子（EGFR）的肿瘤的诊断和治疗。本发明还涉及皮肤刺激，优选皮肤疹，并且与利用EGF受体与抗癌剂的肿瘤细胞的治疗有关。本发明还涉及基于用EGFR抑制剂，特别是抗EGFR抗体治疗来预测患者肿瘤治疗/肿瘤反应效率的方法。本发明还涉及确定EGFR相关肿瘤治疗中抗癌剂的最佳剂量的方法。

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