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1. 发明申请

US20050101526A1 Cyclic peptidomimetic urokinase receptor antagonists 有权
公开(公告)号：US20050101526A1
公开(公告)日：2005-05-12
申请号：US11018311
申请日：2004-12-22
申请人： Olaf Wilhelm , Horst Kessler , Markus Burgle , Nils Potthoff , Niko Schmiedeberg
发明人： Olaf Wilhelm , Horst Kessler , Markus Burgle , Nils Potthoff , Niko Schmiedeberg
IPC分类号： A61K38/00 , A61K38/12 , C07K7/64 , C12N9/72
CPC分类号： C12N9/6462 , A61K38/00 , C07K7/64 , C12Y304/21073
摘要： The present invention relates to cyclic peptides as inhibitors of urokinase binding to the urokinase receptor. Said cyclic peptides are suitable as pharmaceutical active substances for disorders mediated by urokinase and its receptor.

2. 发明授权

US07045504B2 Cyclic peptidomimetic urokinase receptor antagonists 有权
标题翻译：循环肽模拟尿激酶受体拮抗剂
公开(公告)号：US07045504B2
公开(公告)日：2006-05-16
申请号：US11018311
申请日：2004-12-22
申请人： Olaf Wilhelm , Horst Kessler , Markus Buergle , Nils Potthoff , Niko Schmiedeberg
发明人： Olaf Wilhelm , Horst Kessler , Markus Buergle , Nils Potthoff , Niko Schmiedeberg
IPC分类号： A61K38/00
CPC分类号： C12N9/6462 , A61K38/00 , C07K7/64 , C12Y304/21073
摘要： The present invention relates to cyclic peptides as inhibitors of urokinase binding to the urokinase receptor. Said cyclic peptides are suitable as pharmaceutical active substances for disorders mediated by urokinase and its receptor.
摘要翻译：本发明涉及作为尿激酶结合尿激酶受体的抑制剂的环肽。所述环肽适合作为尿激酶及其受体介导的病症的药物活性物质。

3. 发明申请

US20060105943A1 Cyclic peptidomimetic urokinase receptor antagonists 有权
公开(公告)号：US20060105943A1
公开(公告)日：2006-05-18
申请号：US11321534
申请日：2005-12-30
申请人： Olaf Wilhelm , Horst Kessler , Markus Buergle , Nils Potthoff , Niko Schmiedeberg
发明人： Olaf Wilhelm , Horst Kessler , Markus Buergle , Nils Potthoff , Niko Schmiedeberg
IPC分类号： A61K38/12
CPC分类号： C12N9/6462 , A61K38/00 , C07K7/64 , C12Y304/21073
摘要： The present invention relates to cyclic peptides as inhibitors of urokinase binding to the urokinase receptor. Said cyclic peptides are suitable as pharmaceutical active substances for disorders mediated by urokinase and its receptor.

4. 发明授权

US06906032B1 Cyclic peptidomimetic urokinase receptor antagonists 失效
标题翻译：循环肽模拟尿激酶受体拮抗剂
公开(公告)号：US06906032B1
公开(公告)日：2005-06-14
申请号：US10031401
申请日：2000-07-19
申请人： Olaf Wilhelm , Horst Kessler , Markus Bürgle , Nils Potthoff , Niko Schmiedeberg
发明人： Olaf Wilhelm , Horst Kessler , Markus Bürgle , Nils Potthoff , Niko Schmiedeberg
IPC分类号： A61K38/00 , A61K38/12 , C07K7/64 , C12N9/72
CPC分类号： C12N9/6462 , A61K38/00 , C07K7/64 , C12Y304/21073
摘要： The present invention relates to cyclic peptides as inhibitors of urokinase binding to the urokinase receptor. Said cyclic peptides are suitable as pharmaceutical active substances for disorders mediated by urokinase and its receptor.
摘要翻译：本发明涉及作为尿激酶结合尿激酶受体的抑制剂的环肽。所述环肽适合作为尿激酶及其受体介导的病症的药物活性物质。

5. 发明授权

US07314863B2 Cyclic peptidomimetic urokinase receptor antagonists 有权
标题翻译：循环肽模拟尿激酶受体拮抗剂
公开(公告)号：US07314863B2
公开(公告)日：2008-01-01
申请号：US11321534
申请日：2005-12-30
申请人： Olaf Wilhelm , Horst Kessler , Markus Buergle , Nils Potthoff , Niko Schmiedeberg
发明人： Olaf Wilhelm , Horst Kessler , Markus Buergle , Nils Potthoff , Niko Schmiedeberg
IPC分类号： A61K38/00
CPC分类号： C12N9/6462 , A61K38/00 , C07K7/64 , C12Y304/21073
摘要： The present invention relates to cyclic peptides as inhibitors of urokinase binding to the urokinase receptor. Said cyclic peptides are suitable as pharmaceutical active substances for disorders mediated by urokinase and its receptor.
摘要翻译：本发明涉及作为尿激酶结合尿激酶受体的抑制剂的环肽。所述环肽适合作为尿激酶及其受体介导的病症的药物活性物质。

6. 发明申请

US20090215025A1 SMALL PEPTIDIC AND PEPTIDO-MIMETIC AFFINITY LIGANDS FOR FACTOR VIII AND FACTOR VIII-LIKE PROTEINS 审中-公开
标题翻译：用于因子VIII和因子VIII样蛋白的小肽和肽 - 亲和力配体
公开(公告)号：US20090215025A1
公开(公告)日：2009-08-27
申请号：US12096503
申请日：2006-12-07
申请人： Sebastian Knor , Horst Kessler , Charlotte Hauser , Alexey Khrenov , Evgueni Saenko
发明人： Sebastian Knor , Horst Kessler , Charlotte Hauser , Alexey Khrenov , Evgueni Saenko
IPC分类号： C12Q1/00 , C07K5/117 , C07K7/06 , C07K5/113 , C07D209/20 , C12N9/96
CPC分类号： C07K5/0205 , C07K5/0812 , C07K5/0821 , C07K5/1016 , C07K5/1024 , C07K7/02
摘要： The present invention pertains to compounds that show a high affinity to Factor VIII and Factor VIII-like proteins, and their uses. The compounds are characterized by the general Formula B-Q-X, wherein B represents a dipeptide, tripeptide, or a peptidomimetic; Q represents a spacer and X represents an anchoring molecule; Q and X are optional. These compounds can be used for coating a solid support material. The resulting coated solid support material can be used for purifying Factor VIII by means of affinity chromatography methods. In addition, the compounds of the present invention may be used for stabilizing Factor VIII and for enhancing its activity. The present invention thus pertains also to methods for manufacturing a stabilized Factor VIII containing medicament of increased activity. The inventive compounds can furthermore be used in diagnostic kits and as research tools.
摘要翻译：本发明涉及对因子VIII和因子VIII样蛋白表现出高亲和力的化合物及其用途。该化合物的特征在于通式B-Q-X，其中B代表二肽，三肽或拟肽; Q表示间隔基，X表示锚定分子; Q和X是可选的。这些化合物可用于涂覆固体支持材料。所得的包被的固体支持物质可用于通过亲和层析方法纯化因子VIII。此外，本发明的化合物可用于稳定因子VIII并提高其活性。因此，本发明也涉及制备具有增加的活性的含有稳定因子VIII的药物的方法。本发明化合物还可用于诊断试剂盒和研究工具。

7. 发明授权

US07276482B2 Peptide and peptide mimetic derivatives with integrin-inhibitors properties II 有权
标题翻译：具有整合蛋白抑制剂性质的肽和肽模拟衍生物II
公开(公告)号：US07276482B2
公开(公告)日：2007-10-02
申请号：US10344668
申请日：2001-08-02
申请人： Joerg Meyer , Berthold Nies , Michel Dard , Guenter Hoelzemann , Horst Kessler , Martin Kantlehner , Ulrich Hersel , Christoph Gibson , Gabor Sulyok
发明人： Joerg Meyer , Berthold Nies , Michel Dard , Guenter Hoelzemann , Horst Kessler , Martin Kantlehner , Ulrich Hersel , Christoph Gibson , Gabor Sulyok
IPC分类号： A61K38/10
CPC分类号： C07K7/06 , A61K38/00 , C07K14/78 , Y02P20/125
摘要： The invention relates to compounds of formula (I) B-Q-X1, wherein B is a bioactive, cell adhesive mediating molecule, selected from the group (i) and Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys (SEQ ID NO: 1) (ii), Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys (SEQ ID NO: 2) (iii), Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys (SEQ ID NO: 3) (iv), Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg (SEQ ID NO: 4) (v), Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn (SEQ ID NO: 5) (vi), Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg (SEQ ID NO: 6) (vii), wherein (i) X, Y, Z, R2, R3, R4, A, Ar, Hal, Het, Het1, n, m, o, p, q, s, t have the meanings cited in claim 1, Q is absent or is an organic spacer molecule, X1 is an anchor molecule selected from the group cited in claim 1, and the salts thereof, which can be used as integrin inhibitors particularly for treatment of illness, deficiencies and inflammations caused by implants and osteolytic illnesses such as osteoporosis, thrombosis, cardiac infarction and arteriosclerosis, in addition to the acceleration and strengthening of the integration process of implants or the biocompatible surface in tissue.
摘要翻译：本发明涉及式（I）BQX 1的化合物，其中B是选自（i）和Thr-Trp-Tyr-Lys-Ile-Ala的生物活性的细胞粘附介导分子 -Ph-Gln-Arg-Asn-Arg-Lys（SEQ ID NO：1）（ii），Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys（SEQ ID NO：）（iii），Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys（SEQ ID NO：3）（iv），Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln -Arg-Asn-Arg（SEQ ID NO：4）（v），Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn（SEQ ID NO：5）（vi） -Tyr-Lys-Ile-Ala-Phe-Gln-Arg（SEQ ID NO：6）（vii），其中（i）X，Y，Z，R 2，R 3 A，Ar，Hal，Het，Het 1，n，m，o，p，q，s，t具有引用的含义在权利要求1中，Q不存在或是有机间隔分子，X 1是选自权利要求1所述的基团的锚定分子及其盐，其可以用作整联蛋白抑制剂，特别是用于治疗由植入物和溶骨性疾病引起的疾病，缺陷和炎症例如骨质疏松症，血栓形成，心肌梗死和动脉硬化，以及植入物或组织中生物相容性表面的整合过程的加速和加强。

8. 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。

9. 发明授权

US4612302A Clinical use of somatostatin analogues 失效
标题翻译：生长抑素类似物的临床应用
公开(公告)号：US4612302A
公开(公告)日：1986-09-16
申请号：US550978
申请日：1983-11-14
申请人： Sandor Szabo , Klaus W. Usadel , Horst Kessler
发明人： Sandor Szabo , Klaus W. Usadel , Horst Kessler
IPC分类号： A61K38/00 , A61K38/31 , C07K14/655 , A61K37/24 , C07K7/26
CPC分类号： C07K14/6555 , A61K38/31 , Y10S514/806 , Y10S930/16 , Y10S930/26
摘要： A method of increasing the clearance of particles from the blood stream of a vertebrate, which comprises administering to a vertebrate having a surplus of particles in the blood stream of the vertebrate an amount of a somatostatin analogue sufficient to increase phagocytosis in the vertebrate is disclosed along with a method treating vascular lesions or deterioration of biological membranes comprising the step of administering to a human or other mammal suspected of having one or more vascular lesions or of having deterioration of a biological membrane in the liver of said human or mammal an amount of a somatostatin analogue sufficient to reduce the number or severity of said lesions or to prevent further deterioration or reduce the extent of deterioration of said membrane.
摘要翻译：一种从脊椎动物的血流中增加颗粒间隙的方法，其包括向脊椎动物的血流中具有多余颗粒的脊椎动物施用足以增加脊椎动物吞噬作用的生长抑素类似物的量包括处理血管病变或生物膜恶化的方法，包括向疑似患有一种或多种血管病变的人或其他哺乳动物施用或在所述人或哺乳动物的肝脏中使生物膜变质的步骤生长抑素类似物足以减少所述病变的数量或严重程度，或防止进一步恶化或降低所述膜的恶化程度。

10. 发明申请

US20100240072A1 Cancer Imaging and Treatment 失效
标题翻译：癌症成像与治疗
公开(公告)号：US20100240072A1
公开(公告)日：2010-09-23
申请号：US12675151
申请日：2008-09-01
申请人： Hans Jürgen Wester , Horst Kessler , Oliver Demmer , Ingrid Dijkgraaf
发明人： Hans Jürgen Wester , Horst Kessler , Oliver Demmer , Ingrid Dijkgraaf
IPC分类号： G01N33/567 , C07K7/64
CPC分类号： A61K51/08 , A61K47/55 , A61K51/088
摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, comprises the structure: [(P1-S1j)p-L-(S2q-P2)r]t wherein: P1 and P2, which may be the same or different, are cyclic oligopeptide moieties, at least one of P1 and P2 having the motif B-Arg or B-(Me) Arg within the cyclic moiety, wherein B is a basic amino acid, a derivative thereof, or phenylalanine or a derivative thereof; S1 and S2 are spacer groups, which may be the same or different; L is a linker moiety containing at least two functional groups for attachment of the cyclic oligopeptides or spacer groups; n and q are independently 0 or 1; p and r are independently integers of 1 or more; and t is an integer of 1 or more, provided that, when t, p or r is greater than 1, the cyclic oligopeptide moiety, spacer group and/or the value of j or q may be the same or different between the multiple (P1-S1j) moieties or multiple (S2q-P2) moieties.
摘要翻译：化合物或其药学上可接受的盐或酯包含以下结构：[（P1-S1j）pL-（S2q-P2）r] t其中：P1和P2可以相同或不同，是环状寡肽部分在环状部分中具有基序B-Arg或B（Me）Arg的P1和P2中的至少一个，其中B是碱性氨基酸，其衍生物或苯丙氨酸或其衍生物; S1和S2是间隔基，其可以相同或不同; L是含有至少两个用于连接环状寡肽或间隔基团的官能团的连接体部分; n和q独立地为0或1; p和r独立地为1或更大的整数; 并且t为1或更大的整数，条件是当t，p或r大于1时，环状寡肽部分，间隔基团和/或j或q的值可以在多个 P1-S1j）部分或多个（S2q-P2）部分。

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