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1. 发明授权

US08691761B2 Somatostatin receptor 2 antagonists 有权
标题翻译：生长抑素受体2拮抗剂
公开(公告)号：US08691761B2
公开(公告)日：2014-04-08
申请号：US12104318
申请日：2008-04-16
申请人： Jean E. F. Rivier , Judit Erchegyi , Jean Claude Reubi , Helmut R. Maecke
发明人： Jean E. F. Rivier , Judit Erchegyi , Jean Claude Reubi , Helmut R. Maecke
IPC分类号： A61K38/31 , A61P3/10
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。

2. 发明授权

US08501687B2 Receptor(SSTR2)-selective somatostatin antagonists 有权
标题翻译：受体（SSTR2） - 选择性生长抑素拮抗剂
公开(公告)号：US08501687B2
公开(公告)日：2013-08-06
申请号：US13159020
申请日：2011-06-13
申请人： Jean E. F. Rivier , Judit Erchegyi , Jean Claude Reubi , Helmut R. Maecke
发明人： Jean E. F. Rivier , Judit Erchegyi , Jean Claude Reubi , Helmut R. Maecke
IPC分类号： A61K38/31 , A61K3/10 , A61K7/12
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。

3. 发明授权

US07960342B2 Receptor(SSTR2)-selective somatostatin antagonists 有权
标题翻译：受体（SSTR2） - 选择性生长抑素拮抗剂
公开(公告)号：US07960342B2
公开(公告)日：2011-06-14
申请号：US11872367
申请日：2007-10-15
申请人： Jean E. F. Rivier , Judit Erchegyi , Jean Claude Reubi , Helmut R. Maecke
发明人： Jean E. F. Rivier , Judit Erchegyi , Jean Claude Reubi , Helmut R. Maecke
IPC分类号： A61K38/18 , A61K38/31
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。

4. 发明授权

US07238775B2 Receptor(SSTR4)-selective somatostatin analogs 有权
标题翻译：受体（SSTR4） - 选择性生长抑素类似物
公开(公告)号：US07238775B2
公开(公告)日：2007-07-03
申请号：US11041676
申请日：2005-01-24
申请人： Jean E. F. Rivier , Jean Claude Reubi , Judit Erchegyi , Roland Riek
发明人： Jean E. F. Rivier , Jean Claude Reubi , Judit Erchegyi , Roland Riek
IPC分类号： A61K38/00
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-AA1,2,4,5,12,13[Ala7]-SRIF; des-AA1,2,4,5,12,13[Aph7]-SRIF, des-AA1,2,4,5,12,13[Aph7]Cbm-SRIF; des-AA1,2,4,5,12,13[Tyr2,Ala7]-Cbm-SRIF, and des-AA1,2,4,5,12,13[Tyr7,CβMe-L-2Nal8]-SRIF, and counterparts incorporating D-Cys3 and/or D-Trp8 and/or Ala11, 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，例如des-AA 1,2,4,5,12,13，[Ala 7] -SRIF; des-AA 1,2,4,5,12,13 [Aph7] -SRIF，des-AA 1,2,4,5,12 ，13β-Cpm-SRIF; des-AA 1,2,4,5,12,13 [Tyr2]，Ala7-Cbm-SRIF，和des- AA 1,2,4,5,12,13 [Tyr 7]，C 2 H 2 Me-L-2Nal 8， SUP]] - SRIF，以及掺有D-Cys 3和/或D-Trp 8和/或Ala 11的对应物与高结合对克隆的人受体SSTR4的亲和力并激活受体，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。

5. 发明授权

US06579967B1 Receptor-selective somatostatin analogs 有权
标题翻译：受体选择性生长抑素类似物
公开(公告)号：US06579967B1
公开(公告)日：2003-06-17
申请号：US09607546
申请日：2000-06-29
申请人： Jean E. F. Rivier , Jean Claude Reubi
发明人： Jean E. F. Rivier , Jean Claude Reubi
IPC分类号： A61K3831
CPC分类号： C07K14/655 , C07K7/64 , Y10S930/16
摘要： Analogs of SRIF which are selective for SSTR3 in contrast to the other cloned SRIF receptors. These analogs are useful in determining the tissue and cellular expression of the receptor SSTR3 and its biological role in the endocrine, exocrine and nervous system, as well as in regulating tumor growth. SRIF analog peptides, such as des-AA1,2,4,5,12,13[N&bgr;MeD-Agl8(2-naphthoyl) ]-SRIF and counterparts incorporating D-Cys3 and/or Tyr7, inhibit the binding of a universal SRIF radioligand to the cloned human receptor SSTR3, but they do not bind with significant affinity to human SSTR1, SSTR2, SSTR4 or SSTR5. By incorporating an iodinated tyrosine in position-2 or in position-11 in these SSTR3-selective SRIF analogs, a labeled compound useful in drug-screening methods is provided. Because the N-terminus accommodates bulky moieties without loss of selectivity, a cytotoxin or a complexing agent to accept a radioactive nuclide may be present at the N-terminus. Alternatively, the binding affinity may be improved without detriment to the selectivity by adding a carbamoyl moiety at the N-terminus and/or replacing Phe11 with Aph or substituted Aph.
摘要翻译：与其他克隆的SRIF受体相反，SIF3选择性的SRIF的类似物。这些类似物可用于确定受体SSTR3的组织和细胞表达及其在内分泌，外分泌和神经系统中的生物学作用以及调节肿瘤生长。 SRIF类似物，例如des-AA1,2,4,5,12,13 [NbetaMeD-Ag18（2-萘甲酰基）] -SRIF和掺入D-Cys3和/或Tyr7的对应物抑制通用SRIF放射性配体对克隆的人受体SSTR3，但它们不以与人SSTR1，SSTR2，SSTR4或SSTR5的显着亲和力结合。通过在这些SSTR3选择性SRIF类似物中掺入位置2或位置-11中的碘化酪氨酸，提供了可用于药物筛选方法的标记化合物。因为N-末端可以容纳庞大的部分而不丧失选择性，所以在N-末端可以存在接受放射性核素的细胞毒素或络合剂。或者，可以通过在N末端加入氨基甲酰基部分和/或用Aph或取代的Aph代替Phe11而改善结合亲和力而不损害选择性。

6. 发明授权

US07019109B2 SSTR1-selective analogs 失效
标题翻译： SSTR1选择性类似物
公开(公告)号：US07019109B2
公开(公告)日：2006-03-28
申请号：US10099240
申请日：2002-03-15
申请人： Jean E. F. Rivier , Jean Claude Reubi
发明人： Jean E. F. Rivier , Jean Claude Reubi
IPC分类号： C07K7/665 , C07K7/64
CPC分类号： C07K14/6555 , A61K51/083 , A61K51/088
摘要： Analogs of SRIF which are selective for SSTR1 in contrast to the other cloned SRIF receptors. These analogs are useful in determining the tissue and cellular expression of the receptor SSTR1 and its biological role in the endocrine, exocrine and nervous system, as well as in regulating tumor growth. SRIF analog peptides, such as des-AA1,2,5[D-Trp8, NαMeIAmp9, Tyr11]-SRIF and counterparts incorporating Cbm at the N-terminus and/or NαSer13, inhibit the binding of a universal SRIF radioligand to the cloned human receptor SSTR1, but they do not bind with significant affinity to human SSTR2, SSTR3, SSTR4 or SSTR5. By incorporating an iodinated tyrosine in position-2 or in position-11 in these SSTR1-selective SRIF analogs, a labeled compound useful in drug-screening methods is provided. The N-terminus accommodates bulky moieties without loss of selectivity, and a carbamoyl moiety or a conjugating agent that will accept a radioactive nuclide or will link to a cytotoxin may be present at the N-terminus.
摘要翻译：与其他克隆的SRIF受体相反，SRIF的选择性为SSTR1的类似物。这些类似物可用于确定受体SSTR1的组织和细胞表达及其在内分泌，外分泌和神经系统中的生物学作用以及调节肿瘤生长。 SRIF类似物肽，例如des-AA 12,5，D-Trp 8，Nα，Me 3， SUP>，Tyr 11] - SRIF和在N末端和/或NαSer 13结合Cbm的对应物抑制结合与克隆的人受体SSTR1通用的SRIF放射配体，但它们不以与人SSTR2，SSTR3，SSTR4或SSTR5的显着亲和力结合。通过在这些SSTR1选择性SRIF类似物中掺入位置2或位置-11的碘化酪氨酸，提供了可用于药物筛选方法的标记化合物。 N-末端可容纳大量的部分而不损失选择性，并且可以在N-末端存在将接受放射性核素或将连接至细胞毒素的氨基甲酰基部分或共轭试剂。

7. 发明申请

US20120259092A1 NPY ANTAGONISTS 审中-公开
标题翻译： NPY拮抗剂
公开(公告)号：US20120259092A1
公开(公告)日：2012-10-11
申请号：US13444675
申请日：2012-04-11
申请人： David Chatenet , Jean Claude Reubi , Jean E. F. Rivier
发明人： David Chatenet , Jean Claude Reubi , Jean E. F. Rivier
IPC分类号： C07K17/02
CPC分类号： C07K14/57545 , A61K49/0002 , A61K51/088
摘要： Peptidic NPY antagonists selective for Y1 having an organic chelator, such as DOTA, coupled thereto which are useful for diagnostic procedures and receptor-mediated radiotherapy.
摘要翻译：对于具有偶联有机螯合剂（例如DOTA）的Y1选择性的肽NPY拮抗剂可用于诊断程序和受体介导的放射治疗。

8. 发明授权

US07141546B1 CRFR2 selective ligands 有权
标题翻译： CRFR2选择性配体
公开(公告)号：US07141546B1
公开(公告)日：2006-11-28
申请号：US10210889
申请日：2002-07-31
申请人： Jean E. F. Rivier , Wylie W. Vale , Marilyn H. Perrin , Jozsef Gulyas , Dean A. Kirby
发明人： Jean E. F. Rivier , Wylie W. Vale , Marilyn H. Perrin , Jozsef Gulyas , Dean A. Kirby
IPC分类号： A61K38/16 , C07K14/00
CPC分类号： C07K14/4703 , A61K38/00 , G01N33/74 , G01N2500/02
摘要： CRF peptide analogs that bind to CRFR2 with an affinity far greater than they bind to CRFR1. These analogs exhibit CRF antagonist activity, and they can be based upon the native structures of sauvagine, CRF, and urocortin.
摘要翻译：结合CRFR2的CRF肽类似物的亲和力远远大于它们与CRFR1结合的亲和力。这些类似物显示CRF拮抗剂活性，它们可以基于sauvagine，CRF和尿皮质素的天然结构。

9. 发明授权

US06326463B1 Cyclic CRF agonists 有权
标题翻译：循环CRF激动剂
公开(公告)号：US06326463B1
公开(公告)日：2001-12-04
申请号：US09424889
申请日：1999-11-29
申请人： Jean E. F. Rivier
发明人： Jean E. F. Rivier
IPC分类号： A61K3828
CPC分类号： C07K14/57509 , A61K38/00 , G01N33/566 , G01N33/68 , G01N33/74 , G01N2333/5751 , Y10S930/26
摘要： Novel cyclic CRF agonist peptides have the amino acid sequence: (cyclo 30-33)Ac-Ser-Leu-Asp-Leu-Thr-D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Nle-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Glu-Ala-R32-R33-Asn-Arg-Lys-Leu-Nle-Glu-Ile-Ile-NH2 wherein R32 is His, D-His or an equivalent &agr;-amino acid; R33 is Lys or Orn. The N-terminus may be extended by Tyr, D-Tyr or Ile. Lys may be substituted for Arg23, and its side chain connected by a lactam bridge to Glu20 to form a bicyclic peptide. Certain disclosed CRF agonists include: (cyclo 30-33)[Ac-Ser7, D-Phe12, Nle21,38, Glu30, Lys33]r/hCRF(7-41); (cyclo 30-33)[Ac-Ser7, D-Phe12, Nle21,38, Glu30, D-His32, Lys33]r/hCRF(7-41); (bicyclo 20-23, 30-33)[Ac-Ser7, D-Phe12, Nle21,38, Lys23,33, Glu30, D-His32]-r/hCRF(7-41); (cyclo 30-33)[Ac-Ser7, D-Phe12, Nle18,21, Glu30, D-Ala32, Lys33]&agr;-helicale CRF(7-41); and (cyclo 30-33)[Ac-Ser7, D-Phe12, Nle21,38, CML27,40, Glu30, Lys33]r/hCRF(7-41). Labelled agonist such as (cyclo 30-33)[Ac-I125Tyr6, D-Phe12, Nle21,38, Glu30, Lys33]r/hCRF(6-41) and (cyclo 30-33)[Ac-I125D-Tyr6, D-Phe12, Nle21,38, Glu30, D-His32, Lys33]r/hCRF(6-41) are useful in screening for more potent CRF agonists.
摘要翻译：新型循环CRF激动剂肽具有氨基酸序列：（环30-33）Ac-Ser-Leu-Asp-Leu-Thr-D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Nle -Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Glu-Ala-R32-R33-Asn-Arg-Lys-Leu-Nle-Glu-Ile-Ile-NH2，其中R32是His，D-His 或等效的α-氨基酸; R33是Lys或Orn。 N末端可以被Tyr，D-Tyr或Ile延伸。 Lys可以代替Arg23，其侧链通过内酰胺桥连接至Glu20以形成双环肽。某些公开的CRF激动剂包括：（环30-33）[Ac-Ser7，D-Phe12，Nle21,38，Glu30，Lys33] r / hCRF（7-41）; （环30-33）[Ac-Ser7，D-Phe12，Nle21,38，Glu30，D-His32，Lys33] r / hCRF（7-41）; （双环20-23,30-33）[Ac-Ser7，D-Phe12，Nle21,38，Lys23,33，Glu30，D-His32] -r / hCRF（7-41）; （环30-33）[Ac-Ser7，D-Phe12，Nle18,21，Glu30，D-Ala32，Lys33]α-螺旋CRF（7-41）; 和（环30-33）[Ac-Ser7，D-Phe12，Nle21,38，CML27,40，Glu30，Lys33] r / hCRF（7-41）。标记的激动剂如（环30-33）[Ac-I125Tyr6，D-Phe12，Nle21,38，Glu30，Lys33] r / hCRF（6-41）和（环30-33）[Ac-I125D-Tyr6，D -Phe12，Nle21,38，Glu30，D-His32，Lys33] r / hCRF（6-41）可用于筛选更有效的CRF激动剂。

10. 发明授权

US06323312B1 Cyclic CRF antagonist peptides 有权
标题翻译：循环CRF拮抗肽
公开(公告)号：US06323312B1
公开(公告)日：2001-11-27
申请号：US09424127
申请日：1999-11-17
申请人： Jean E. F. Rivier
发明人： Jean E. F. Rivier
IPC分类号： A61K3812
CPC分类号： G01N33/74 , A61K38/00 , C07K14/57509 , G01N33/566 , G01N2333/5751
摘要： Novel cyclic CRF antagonist peptides are created by shortening the N-terminus of a CRF family peptide by 8 residues and adding an acyl group. CML is present in what would be the 27-position of the native CRF sequence, and a cyclizing bond is created between the side chains of the residues in positions 30 and 33. The side chain of Lys, preferably, in position 33 is linked to the side chain of Glu in position 30 by a lactam bridce. Disclosed CRF antagonists include: (cyclo 30-33)[Ac-Asp9, D-Phe12, Nle21,38, CML27,40, Glu30, Lys33]r/hCRF(9-4); (cyclo 30-33)[Ac-Asp9, D-Phe12, CML18,27, Nle21,38, Glu30, Lys33]r-hCRF(9-41); (cyclo 30-33)[Ac-Asp9, D-Phe12, Nle21,38, CML27,37, Glu30, Lys33]r/hCRF(9-41); (cyclo 30-33)[Ac-Asp9, D-Phe12, CML14,27, Nle21,38, Glu30, Lys33]r/hCRF(9-41); (cyclo 30-33)[Ac-Asp9, D-Phe12, Nle21,38, CML27, Glu30, Lys33]r/hCRF(9-41); and (cyclo 30-33)[Ac-Asp9, D-Phe12, Nle21,38, CML27,40, Glu30, Aib32, Lys33]r/hCRF(9-41).
摘要翻译：通过将CRF家族肽的N末端缩短8个残基并加入酰基来产生新的循环CRF拮抗剂肽。 CML存在于天然CRF序列的27位上，并且在位置30和33的残基的侧链之间产生环化键。Lys的侧链优选位于33位与位置30处的Glu的侧链通过内酰胺桥接。公开的CRF拮抗剂包括：（环30-33）[Ac-Asp9，D-Phe12，Nle21,38，CML27,40，Glu30，Lys33] r / hCRF（9-4）; （环30-33）[Ac-Asp9，D-Phe12，CML18,27，Nle21,38，Glu30，Lys33] r-hCRF（9-41）; （环30-33）[Ac-Asp9，D-Phe12，Nle21,38，CML27,37，Glu30，Lys33] r / hCRF（9-41）; （环30-33）[Ac-Asp9，D-Phe12，CML14,27，Nle21,38，Glu30，Lys33] r / hCRF（9-41）; （环30-33）[Ac-Asp9，D-Phe12，Nle21,38，CML27，Glu30，Lys33] r / hCRF（9-41）; 和（环30-33）[Ac-Asp9，D-Phe12，Nle21,38，CML27,40，Glu30，Aib32，Lys33] r / hCRF（9-41）。

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