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公开(公告)号：US20080260638A1
公开(公告)日：2008-10-23
申请号：US11872367
申请日：2007-10-15
IPC分类号： A61K38/31 , C07K14/655 , A61P35/00 , A61K51/08
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 labeled 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，提供了可用于药物筛选方法的标记化合物。 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。
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公开(公告)号：US20110269683A1
公开(公告)日：2011-11-03
申请号：US13159020
申请日：2011-06-13
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. By incorporating radioiodine or the like in these SSTR2-selective SRIF antagonists, a labeled 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. Because they block the receptor function, they can be used therapeutically to block certain physiological effects which SSTR2 mediates.
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。 通过在这些SSTR2选择性SRIF拮抗剂中引入放射性碘等，提供了可用于药物筛选方法的标记化合物。 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。 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。
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公开(公告)号：US20080299040A1
公开(公告)日：2008-12-04
申请号：US12104318
申请日：2008-04-16
CPC分类号： C07K14/655 , A61K38/00 , G01N2333/655
摘要： The invention is directed to somatostatin analogs which are receptor antagonists of the somatostatin receptor, including receptor-selective antagonists, especially sst2-selective antagonists. Related compounds and compositions are included, including antagonists complexed with or conjugated to radioactive nuclides. The antagonists of the invention are useful in diagnosing and treating neoplastic and non-neoplastic mammalian diseases; such methods, and kits, are encompassed.
摘要翻译： 本发明涉及作为生长抑素受体的受体拮抗剂的生长抑素类似物，包括受体选择性拮抗剂，特别是sst2选择性拮抗剂。 包括相关化合物和组合物，包括与放射性核素复合或缀合的拮抗剂。 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; 包括这些方法和试剂盒。
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公开(公告)号：US08691761B2
公开(公告)日：2014-04-08
申请号：US12104318
申请日：2008-04-16
CPC分类号： C07K14/655 , A61K38/00 , G01N2333/655
摘要： The invention is directed to somatostatin analogs which are receptor antagonists of the somatostatin receptor, including receptor-selective antagonists, especially sst2-selective antagonists. Related compounds and compositions are included, including antagonists complexed with or conjugated to radioactive nuclides. The antagonists of the invention are useful in diagnosing and treating neoplastic and non-neoplastic mammalian diseases; such methods, and kits, are encompassed.
摘要翻译： 本发明涉及作为生长抑素受体的受体拮抗剂的生长抑素类似物，包括受体选择性拮抗剂，特别是sst2选择性拮抗剂。 包括相关化合物和组合物，包括与放射性核素复合或缀合的拮抗剂。 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; 包括这些方法和试剂盒。
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公开(公告)号：US08501687B2
公开(公告)日：2013-08-06
申请号：US13159020
申请日：2011-06-13
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. By incorporating radioiodine or the like in these SSTR2-selective SRIF antagonists, a labeled 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. Because they block the receptor function, they can be used therapeutically to block certain physiological effects which SSTR2 mediates.
摘要翻译： 与其他克隆的SRIF受体相比，SRIF肽拮抗剂对于SSTR2是选择性的，并且与克隆的人受体SSTR2以高亲和力结合但不激活受体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。 通过在这些SSTR2选择性SRIF拮抗剂中引入放射性碘等，提供了可用于药物筛选方法的标记化合物。 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。 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。
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公开(公告)号：US07960342B2
公开(公告)日：2011-06-14
申请号：US11872367
申请日：2007-10-15
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 labeled 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止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，提供了可用于药物筛选方法的标记化合物。 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。
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