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1. 发明申请

WO2003092744A3 BENZOTHIENYL ANALOGUE OF SOMATOSTATIN, SELECTIVE FOR CERTAIN SOMATOSTATIN RECEPTORS 审中-公开
公开(公告)号：WO2003092744A3
公开(公告)日：2003-11-13
申请号：PCT/EP2003/004847
申请日：2003-05-02
申请人： BIOSYNTHEMA INC. , MAECKE, Helmut, Robert , REUBI, Jean, Claude , DE JONG, Marion , KRENNING, Eric, Paul , GINJ, Mihaela
发明人： MAECKE, Helmut, Robert , REUBI, Jean, Claude , DE JONG, Marion , KRENNING, Eric, Paul , GINJ, Mihaela
IPC分类号： A61K51/08
摘要： The invention relates to a peptide compound having an improved binding affinity to somatostatin receptors, comprising a peptide and a chelating group covalently linked to a free amino group of said peptide, wherein said peptide is or comprises a somatostatin analogue carrying a 3-benzothienylalanine residue in its 3-position. The invention further relates to said peptide compound labelled with a detectable element or with a therapeutic radionuclide, as well as to a diagnostic method and to a method for the therapeutic treatment of tumors, by using the labelled compounds.

2. 发明申请

WO0018440A8 SOMATOSTATIN RECEPTOR RADIOLIGAND WITH INCREASED UPTAKE 审中-公开
标题翻译：增加摄入的生长抑素受体RADIOLIGAND
公开(公告)号：WO0018440A8
公开(公告)日：2000-08-24
申请号：PCT/US9922337
申请日：1999-09-24
申请人： MALLINCKRODT INC , JONG MARION DE , BREEMAN WOUT A , VISSER THEOFILUS JOHANNES , KRENNING ERIC PAUL , SRINIVASAN ANANTHACHARI
发明人： DE JONG MARION , BREEMAN WOUT A , VISSER THEOFILUS JOHANNES , KRENNING ERIC PAUL , SRINIVASAN ANANTHACHARI
IPC分类号： G01N33/534 , A61K47/48 , A61K51/00 , A61K51/08 , A61P35/00 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/575 , G01N33/566
CPC分类号： A61K51/088 , A61K51/083
摘要： A radioligand comprising a peptide capable of binding to a receptor wherein the peptide is coupled to at least one chelating agent, which chelating agent is not coordinated to a metal ion under physiological conditions and a composition comprising said radioligand as a diagnostic or pharmaceutical and a kit for the detection of receptors.
摘要翻译：包含能够与受体结合的肽的放射性配体，其中所述肽与至少一种螯合剂偶联，所述螯合剂在生理条件下不与金属离子配位，并且包含所述放射性配体作为诊断剂或药物的组合物和试剂盒用于检测受体。

3. 发明申请

WO0018440A9 SOMATOSTATIN RECEPTOR RADIOLIGAND WITH INCREASED UPTAKE 审中-公开
公开(公告)号：WO0018440A9
公开(公告)日：2000-10-12
申请号：PCT/US9922337
申请日：1999-09-24
申请人： MALLINCKRODT INC , JONG MARION DE , BREEMAN WOUT A , VISSER THEOFILUS JOHANNES , KRENNING ERIC PAUL , SRINIVASAN ANANTHACHARI
发明人： DE JONG MARION , BREEMAN WOUT A , VISSER THEOFILUS JOHANNES , KRENNING ERIC PAUL , SRINIVASAN ANANTHACHARI
IPC分类号： G01N33/534 , A61K47/48 , A61K51/00 , A61K51/08 , A61P35/00 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/575 , G01N33/566
CPC分类号： A61K51/088 , A61K51/083
摘要： A radioligand comprising a peptide capable of binding to a receptor wherein the peptide is coupled to at least one chelating agent, which chelating agent is not coordinated to a metal ion under physiological conditions and a composition comprising said radioligand as a diagnostic or pharmaceutical and a kit for the detection of receptors.

4. 发明申请

WO2003099864A1 USE OF MONOCARBOXYLATE TRANSPORTER PROTEIN FOR THYROID HORMONE TRANSPORT 审中-公开
标题翻译：单羧酸运输蛋白用于甲状腺激素运输的用途
公开(公告)号：WO2003099864A1
公开(公告)日：2003-12-04
申请号：PCT/NL2003/000384
申请日：2003-05-23
申请人： STICHTING TOT BEVORDERING VAN DE WETENSCHAP DER ENDOCRINOLOGIE , FRIESEMA, Edith, Catharina, Hendrika , VISSER, Theofilus, Johannes , KRENNING, Eric, Paul
发明人： FRIESEMA, Edith, Catharina, Hendrika , VISSER, Theofilus, Johannes , KRENNING, Eric, Paul
IPC分类号： C07K14/47
CPC分类号： C07K14/47
摘要： The invention provides a use of a monocarboxylate transporter protein or a functional part, derivative and/or analogue thereof for altering transport of a thyroid hormone or a functional part, derivative and/or analogue thereof across a membrane. Said monocarboxylate transporter protein preferably comprises MCT-8. An isolated molecule capable of specifically binding at least part of an MCT protein, at least part of a ligand of an MCT protein, or a nucleic acid encoding said MCT and/or ligand, is also herewith provided. Regulation of the bioavailability of thyroid hormone in a tissue enables interfering with (metabolic) diseases. Hence, the invention also provides pharmaceutical compositions comprising a compound capable of binding said MCT protein, or capable of influencing the binding or transporting of a ligand of said MCT protein. Methods for diagnosis and/or treatment of a disease such as a disorder of thyroid metabolism, non-thyroidal illness, obesity or cardiovascular illness are also provided, as well as bioassays for identifying or detecting a candidate drug capable of binding to or influencing at least part of said MCT protein.
摘要翻译：本发明提供单羧酸转运蛋白或其功能部分，衍生物和/或类似物用于改变跨膜的甲状腺激素或其功能部分，衍生物和/或类似物的转运的用途。所述单羧酸转运蛋白优选包含MCT-8。还提供了能够特异性结合至少部分MCT蛋白，至少部分MCT蛋白质配体或编码所述MCT和/或配体的核酸的分离分子。调节组织中甲状腺激素的生物利用度可以干预（代谢）疾病。因此，本发明还提供了包含能够结合所述MCT蛋白的化合物或能够影响所述MCT蛋白的配体的结合或转运的药物组合物。还提供了用于诊断和/或治疗诸如甲状腺代谢紊乱，非甲状腺疾病，肥胖或心血管疾病的疾病的方法，以及用于鉴定或检测至少能够结合或影响的候选药物的生物测定所述MCT蛋白的一部分。

5. 发明申请

WO2003092744A2 PEPTIDE COMPOUND HAVING IMPROVED BINDING AFFINITY TO SOMATOSTATIN RECEPTORS 审中-公开
标题翻译： SOMATOSTATIN的苯并噻唑类似物，选择某些SOMATOSTATIN受体
公开(公告)号：WO2003092744A2
公开(公告)日：2003-11-13
申请号：PCT/EP2003/004847
申请日：2003-05-02
申请人： BIOSYNTHEMA INC. , MAECKE, Helmut, Robert , REUBI, Jean, Claude , DE JONG, Marion , KRENNING, Eric, Paul , GINJ, Mihaela
发明人： MAECKE, Helmut, Robert , REUBI, Jean, Claude , DE JONG, Marion , KRENNING, Eric, Paul , GINJ, Mihaela
IPC分类号： A61K51/08
CPC分类号： A61K51/088 , A61K51/083
摘要： The invention relates to a peptide compound having an improved binding affinity to somatostatin receptors, comprising a peptide and a chelating group covalently linked to a free amino group of said peptide, wherein said peptide is or comprises a somatostatin analogue carrying a 3-benzothienylalanine residue in its 3-position. The invention further relates to said peptide compound labelled with a detectable element or with a therapeutic radionuclide, as well as to a diagnostic method and to a method for the therapeutic treatment of tumors, by using the labelled compounds.
摘要翻译：本发明涉及对生长抑素受体具有改善的结合亲和力的肽化合物，其包含与所述肽的游离氨基共价连接的肽和螯合基团，其中所述肽是或包含携带3-苯并噻吩丙氨酸残基的生长抑素类似物其3位。本发明还涉及用可检测元件或治疗性放射性核素标记的所述肽化合物，以及通过使用标记的化合物的诊断方法和治疗肿瘤的方法。

6. 发明申请

WO0181426A3 RGD (ARG-GLY-ASP) COUPLED TO (NEURO)PEPTIDES 审中-公开
标题翻译： RGD（ARG-GLY-ASP）与（NEURO）PEPTIDES联用
公开(公告)号：WO0181426A3
公开(公告)日：2002-06-27
申请号：PCT/EP0104764
申请日：2001-04-26
申请人： MALLINCKRODT INC , DE JONG MARION , KRENNING ERIC PAUL , VAN HAGEN PETRUS MARTINUS
发明人： DE JONG MARION , KRENNING ERIC PAUL , VAN HAGEN PETRUS MARTINUS
IPC分类号： C07K14/00 , A61K47/48 , A61K51/08 , C07K5/09 , C07K5/10 , C07K7/00 , C07K7/08 , C07K7/22 , C07K7/64 , C07K14/575 , C07K14/595 , C07K14/655 , C07K14/75 , C07K14/78 , C07K19/00
CPC分类号： C07K5/1019 , A61K47/62 , A61K51/082 , A61K51/083 , A61K51/088 , C07K5/0817 , C07K7/086 , C07K7/22 , C07K14/575 , C07K14/57563 , C07K14/595 , C07K14/655 , C07K14/6555 , C07K14/75 , C07K14/78 , C07K19/00
摘要： The invention relates to compounds having a binding affinity for both the alpha v beta 3 receptor and a (neuro)peptide receptor, in particular the somatostatin receptor, which compound comprises a first peptide part comprising at least once the amino acid sequence Arg-Gly-Asp, and a second peptide part coupled thereto, optionally via a linker, which second peptide part is a (neuro)peptide.
摘要翻译：本发明涉及对αvβ3受体和（神经）肽受体，特别是生长抑素受体具有结合亲和力的化合物，该化合物包含第一肽部分，其包含至少一次氨基酸序列Arg-Gly- Asp和与其偶联的第二肽部分，任选地经由接头，其中第二肽部分是（神经）肽。

7. 发明申请

WO0105383A3 INHIBITION OF RENAL UPTAKE OF RADIOMOLECULES WITH A COMBINATION OF LYSINE AND ARGININE 审中-公开
标题翻译：抑制含有赖氨酸和阿奇霉素的放射性分子的肾脏摄取
公开(公告)号：WO0105383A3
公开(公告)日：2001-07-19
申请号：PCT/EP0006917
申请日：2000-07-17
申请人： MALLINCKRODT INC , KRENNING ERIC PAUL , JONG MARION DE , VALKEMA ROELF
发明人： KRENNING ERIC PAUL , DE JONG MARION , VALKEMA ROELF
IPC分类号： A61K38/00 , A61K31/195 , A61K31/198 , A61K51/08 , A61P13/12 , A61P43/00 , A61K47/48 , A61K51/06 , A61P35/00
CPC分类号： A61K51/088 , A61K31/195 , A61K51/083 , A61K2300/00
摘要： The invention relates to the use of the combination of a first compound which is lysine, or an amino acid or other proteinaceous moiety having a free amino group with a pKa substantially similar or equal to that of lysine, or pharmaceutically acceptable salts or carboxyl derivatives thereof, and a second compound, which is a positively charged compound, or pharmaceutically acceptable salts or carboxyl derivatives thereof, for the preparation of a composition for inhibiting renal uptake of substances, in particular proteins or peptides, that may be damaging to the kidneys, and that are used for therapeutical or diagnostic purposes. The combination consists advantageously of lysine and arginine.
摘要翻译：本发明涉及使用赖氨酸的第一化合物或具有游离氨基的氨基酸或其它蛋白质部分与基本上等于赖氨酸的pKa或其药学上可接受的盐或羧基衍生物的pKa的组合和作为带正电的化合物的第二化合物或其药学上可接受的盐或羧基衍生物，用于制备可能损害肾脏的物质特别是蛋白质或肽的肾摄取的组合物，以及用于治疗或诊断目的。该组合有利地由赖氨酸和精氨酸组成。

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