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1. 发明申请

WO2009129311A2 SOMATOSTATIN RECEPTOR 2 ANTAGONISTS 审中-公开
标题翻译： SOMATOSTATIN受体2拮抗剂
公开(公告)号：WO2009129311A2
公开(公告)日：2009-10-22
申请号：PCT/US2009040672
申请日：2009-04-15
申请人： SALK INST FOR BIOLOGICAL STUDI , UNIV BERN , UNIV HOSPITAL BASEL , RIVIER JEAN E F , ERCHEGYI JUDIT , REUBI JEAN CLAUDE , MAECKE HELMUT R
发明人： RIVIER JEAN E F , ERCHEGYI JUDIT , REUBI JEAN CLAUDE , MAECKE HELMUT R
IPC分类号： C07K14/655 , C07K7/06
CPC分类号： C07K14/655 , A61K38/00 , G01N2333/655
摘要： Described herein are somatostatin analogs that are receptor antagonists of the somatostatin receptor, including SSTR2-selective antagonists. Related compounds, kits and methods, including antagonists complexed with or conjugated to radioactive nuclides and uses thereof. The antagonists of the invention are useful in diagnosing and treating neoplastic and non-neoplastic mammalian diseases.
摘要翻译：本文描述了生长抑素类似物，其是生长抑素受体的受体拮抗剂，包括SSTR2-选择性拮抗剂。相关化合物，试剂盒和方法，包括与放射性核素复合或缀合的拮抗剂及其用途。本发明的拮抗剂可用于诊断和治疗肿瘤和非肿瘤性哺乳动物疾病。

2. 发明申请

WO2008048942A3 RECEPTOR(SSTR2)-SELECTIVE SOMATOSTATIN ANTAGONISTS 审中-公开
标题翻译：受体（SSTR2） - 选择性SOMATOSTATIN拮抗剂
公开(公告)号：WO2008048942A3
公开(公告)日：2008-09-18
申请号：PCT/US2007081430
申请日：2007-10-15
申请人： SALK INST FOR BIOLOGICAL STUDI , RIVIER JEAN E F , ERCHEGYI JUDIT , REUBI JEAN CLAUDE , MAECKE HELMUT R
发明人： RIVIER JEAN E F , ERCHEGYI JUDIT , REUBI JEAN CLAUDE , MAECKE HELMUT R
IPC分类号： C07K14/655 , C07K7/06
CPC分类号： C07K14/655 , A61K38/00
摘要： SRIF peptide antagonists, which are selective for SSTR2 in contrast to the other cloned SRIF receptors and which bind with high affinity to the cloned human receptor SSTR2 but do not activate the receptor, have many useful functions. Because they do not bind with significant affinity to SSTR1, SSTR3, SSTR4 or SSTR5, their administration avoids potential undesirable side effects. Because they block the receptor function, they can be used therapeutically to block certain physiological effects which SSTR2 mediates. By incorporating radioiodine or the like in these SSTR2-selective SRIF antagonists, a laebled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, highly radioactive moieties can be N-terminally coupled, complexed or chelated thereto.
摘要翻译：与其他克隆的SRIF受体相比，SRIF肽拮抗剂对SSTR2具有选择性，并且与克隆的人受体SSTR2具有高亲和力但不激活受体的结合具有许多有用的功能。因为它们不与SSTR1，SSTR3，SSTR4或SSTR5具有显着的亲合力结合，所以它们的给药避免了潜在的不良副作用。因为它们阻断受体功能，它们可以用于治疗性地阻断SSTR2介导的某些生理作用。通过在这些SSTR2选择性SRIF拮抗剂中引入放射性碘等，可以提供用于药物筛选方法的成熟的化合物。或者，为了在治疗中使用，高度放射性的部分可以与其N-末端偶联，复合或螯合。

3. 发明申请

WO2004009614A3 RECEPTOR (SSTR4)- SELECTIVE SOMATOSTATIN ANALOGS 审中-公开
标题翻译：受体（SSTR4） - 选择性SOMATOSTATIN ANALOGS
公开(公告)号：WO2004009614A3
公开(公告)日：2006-08-03
申请号：PCT/US0322600
申请日：2003-07-18
申请人： SALK INST FOR BIOLOGICAL STUDI , RIVIER JEAN E F , REUBI JEAN CLAUDE , ERCHEGYI JUDIT , RIEK ROLAND
发明人： RIVIER JEAN E F , REUBI JEAN CLAUDE , ERCHEGYI JUDIT , RIEK ROLAND
IPC分类号： A61K38/00 , A61K38/12 , C07K14/655
CPC分类号： C07K14/655 , A61K38/00
摘要： Analogs of SRIF which are selective for SSTR4 in contrast to the other cloned SRIF receptors are useful in determining tissue and cellular expression of the receptor SSTR4 and its biological role in regulating tumor growth. SRIF analog peptides, such as des-AA 1,2,4,5,12,13 [Ala 7 ] -SRIF; des-AA 1,2,4,5,12,13 [Aph 7 ] -SRIF, des-AA 1'2,4,5,12,13 [Aph 7 ] Cbm-SRIF; desAA 1,4,5,12,13 [Tyr 2 Ala 7 ] -Cbm-SRIF, and des-AA 1'2,4,5,12,13 [Tyr 7 , C B Me-L2Nal 8 ]-SRIF, and counterparts incorporating D-Cys 3 and/or DTrp 8 and/or Ala 11 , bind with high affinity to the cloned human receptor SSTR4 and activate the receptor, but they do not bind with significant affinity to human SSTR1, SSTR2, SSTR3 or SSTR5. By incorporating an iodinated tyrosine in position-2 in these SSTR4-selective SRIF analogs, a labeled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, cytotoxins or highly radioactive elements can be N-terminally coupled or complexed thereto.
摘要翻译：与其他克隆的SRIF受体相比，选择性SSTR4的SRIF的类似物可用于确定受体SSTR4的组织和细胞表达及其在调节肿瘤生长中的生物学作用。 SRIF类似物肽，如des-AA 1,2,4,5,12,13，[Ala 7] -SRIF; des-AA 1,2,4,5,12,13 [Aph] 7RIF，des-AA 1,2,4,5,12 ，13β-Cpm-SRIF; desAA 1,4,5,12,13 [Tyr 2] Ala 7-C bm-SRIF和des-AA 1 '2,4,5,12,13 [Tyr 7]，C B 2 Me-L2 Nal 8 -SRIF，和结合D-Cys 3和/或DTrp 8和/或Ala 11的对应物以高亲和力结合克隆的人受体SSTR4并激活受体，但它们不以与人SSTR1，SSTR2，SSTR3或SSTR5的显着亲和力结合。通过在这些SSTR4选择性SRIF类似物中加入位置2的碘化酪氨酸，可以提供用于药物筛选方法的标记化合物。或者，为了用于治疗，细胞毒素或高度放射性元素可以是N-末端偶联或与其复合的。

4. 发明申请

WO9700063A3 UROCORTIN PEPTIDES 审中-公开
标题翻译：胭脂虫肽
公开(公告)号：WO9700063A3
公开(公告)日：1997-01-23
申请号：PCT/US9610240
申请日：1996-06-12
申请人： SALK INST FOR BIOLOGICAL STUDI , VALE WYLIE W JR , VAUGHAN JOAN , DONALDSON CYNTHIA J , LEWIS KATHY A , SAWCHENKO PAUL , RIVIER JEAN E F , PERRIN MARILYN H
发明人： VALE WYLIE W JR , VAUGHAN JOAN , DONALDSON CYNTHIA J , LEWIS KATHY A , SAWCHENKO PAUL , RIVIER JEAN E F , PERRIN MARILYN H
IPC分类号： G01N33/50 , A61K38/00 , A61K38/22 , A61P3/00 , A61P9/02 , A61P9/10 , A61P9/12 , A61P15/04 , A61P25/22 , A61P25/28 , A61P29/00 , A61P37/02 , A61P43/00 , C07K14/575 , C07K16/26 , C12N15/09 , G01N33/15 , G01N33/53 , A61K
CPC分类号： C07K14/57509 , A61K38/00
摘要： Urocortin (Ucn) is a native mammalian peptide generally related to Urotensin I and Corticotropin Releasing Factor (CRF). Human Ucn has the formula: Asp-Asn-Pro-Ser-Leu-Ser-Ile-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Thr-Leu-Leu-Glu-Leu-Ala-Arg-Thr-Gln-Ser-Gln-Arg-Glu-Arg-Ala-Glu-Gln-Asn-Arg-Ile-Ile-Phe-Asp-Ser-Val-NH2 (SEQ ID NO:15). Rat-derived Ucn is identical but for 2 substitutions, Asp2 for Asn2 and Pro4 for Ser4. Ucn or analogs thereof or pharmaceutically acceptable salts can be administered to humans and other mammals to achieve substantial elevation of ACTH, β-endorphin, β-lipotropin, other products of the pro-opiomelanocortin gene and corticosterone. They can also be used to lower blood pressure over an extended period of time, as stimulants to elevate mood and to improve memory and learning performance, as well as diagnostically. Shortened fragments may be administered to release endogenous CRF and/or Ucn in the brain and peripherally. Ucn antagonists can be used to block the action of Ucn and/or CRF, as can antibodies to Ucn. Labelled Ucn agonists and antagonists can be used in drug screening assays along with CRF receptors; they may also be used diagnostically along with Ucn antibodies.

5. 发明申请

WO2012088397A3 CYCLIC CRF ANTAGONIST PEPTIDES 审中-公开
公开(公告)号：WO2012088397A3
公开(公告)日：2012-09-13
申请号：PCT/US2011066787
申请日：2011-12-22
申请人： SALK INST FOR BIOLOGICAL STUDI , RIVIER JEAN E F
发明人： RIVIER JEAN E F
IPC分类号： C07K14/00
CPC分类号： C07K14/47 , A61K38/00 , C07K14/57509
摘要： Cyclic CRF antagonist peptides having improved properties of "drugability". The peptides are 33 residues in length with a lactam bond between the residues in position 22 and 25; however, they may be N-terminally shortened by up to 3 residues.
摘要翻译：循环CRF拮抗剂肽具有改善的“药物性”性质。所述肽的长度为33个残基，位置22和25之间的残基之间具有内酰胺键; 然而，它们可以被N末端缩短多达3个残基。

6. 发明专利

AU2007311137A1 Receptor(SSTR2)-selective somatostatin antagonists 未知
公开(公告)号：AU2007311137A1
公开(公告)日：2008-04-24
申请号：AU2007311137
申请日：2007-10-15
申请人： SALK INST FOR BIOLOGICAL STUDI , UNIV BERN , UNIV HOSPITAL BASEL
发明人： REUBI JEAN CLAUDE , RIVIER JEAN E F , ERCHEGYI JUDIT , MAECKE HELMUT R
IPC分类号： C07K7/06 , C07K14/655
摘要： SRIF peptide antagonists, which are selective for SSTR2 in contrast to the other cloned SRIF receptors and which bind with high affinity to the cloned human receptor SSTR2 but do not activate the receptor, have many useful functions. Because they do not bind with significant affinity to SSTR1, SSTR3, SSTR4 or SSTR5, their administration avoids potential undesirable side effects. Because they block the receptor function, they can be used therapeutically to block certain physiological effects which SSTR2 mediates. By incorporating radioiodine or the like in these SSTR2-selective SRIF antagonists, a laebled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, highly radioactive moieties can be N-terminally coupled, complexed or chelated thereto.

7. 发明专利

ES2410207T3 Antagonistas de la somatostatina selectivos para receptor(SSTR2) 未知
公开(公告)号：ES2410207T3
公开(公告)日：2013-07-01
申请号：ES07854075
申请日：2007-10-15
申请人： SALK INST FOR BIOLOGICAL STUDI , UNIV BERN , UNIV HOSPITAL BASEL
发明人： RIVIER JEAN E F , ERCHEGYI JUDIT , REUBI JEAN CLAUDE , MAECKE HELMUT R
IPC分类号： C07K14/655 , C07K7/06
摘要： Un péptido análogo de somatostatina (SRIF) cíclico que se une selectivamente al receptor de SRIF SSTR2,péptido que tiene una de las siguientes secuencias de aminoácidos en las que el extremo C está amidado:**Fórmula** en las que Cpa significa cloro-Phe, Aph (Hor) significa 4-[(2,6-dioxo-hexahidro-pirimidina-4-carbonil)-amino]-fenilalanina y Aph (Cbm) significa 4-ureido-fenilalanina.

8. 发明专利

AU2009236211A1 Somatostatin receptor 2 antagonists 未知
公开(公告)号：AU2009236211A1
公开(公告)日：2009-10-22
申请号：AU2009236211
申请日：2009-04-15
申请人： SALK INST FOR BIOLOGICAL STUDI , UNIV BERN , UNIV HOSPITAL BASEL
发明人： ERCHEGYI JUDIT , REUBI JEAN CLAUDE , MAECKE HELMUT R , RIVIER JEAN E F
IPC分类号： C07K14/655 , C07K7/06
摘要： Described herein are somatostatin analogs that are preceptor antagonists oft the somatostatin preceptor, including SSTR2-selective antagonists. Related compounds, kits and methods, including antagonists complexed with or conjugated to radioactive nuclides and uses thereof. The antagonists of the invention are useful in diagnosing and treating neoplastic and non-neoplastic mammalian diseases.

9. 发明专利

CA2666642C RECEPTOR(SSTR2)-SELECTIVE SOMATOSTATIN ANTAGONISTS 未知
公开(公告)号：CA2666642C
公开(公告)日：2015-11-17
申请号：CA2666642
申请日：2007-10-15
申请人： SALK INST FOR BIOLOGICAL STUDI , UNIV BERN , UNIV HOSPITAL BASEL
发明人： RIVIER JEAN E F , ERCHEGYI JUDIT , REUBI JEAN CLAUDE , MAECKE HELMUT R
IPC分类号： C07K14/655 , C07K7/06
摘要： SRIF peptide antagonists, which are selective for SSTR2 in contrast to the other cloned SRIF receptors and which bind with high affinity to the cloned human receptor SSTR2 but do not activate the receptor, have many useful functions. Because they do not bind with significant affinity to SSTR1, SSTR3, SSTR4 or SSTR5, their administration avoids potential undesirable side effects. Because they block the receptor function, they can be used therapeutically to block certain physiological effects which SSTR2 mediates. By incorporating radioiodine or the like in these SSTR2-selective SRIF antagonists, a laebled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, highly radioactive moieties can be N-terminally coupled, complexed or chelated thereto.

10. 发明专利

AU2009236211B2 Somatostatin receptor 2 antagonists 未知
公开(公告)号：AU2009236211B2
公开(公告)日：2013-12-19
申请号：AU2009236211
申请日：2009-04-15
申请人： SALK INST FOR BIOLOGICAL STUDI , UNIV BERN , UNIV HOSPITAL BASEL
发明人： RIVIER JEAN E F , REUBI JEAN CLAUDE , ERCHEGYI JUDIT , MAECKE HELMUT R
IPC分类号： C07K14/655 , C07K7/06
摘要： Described herein are somatostatin analogs that are receptor antagonists of the somatostatin receptor, including SSTR2-selective antagonists. Related compounds, kits and methods, including antagonists complexed with or conjugated to radioactive nuclides and uses thereof. The antagonists of the invention are useful in diagnosing and treating neoplastic and non-neoplastic mammalian diseases.

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