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1. 发明申请

US20080260638A1 RECEPTOR(SSTR2)-SELECTIVE SOMATOSTATIN ANTAGONISTS 有权
标题翻译：受体（SSTR2） - 选择性SOMATOSTATIN拮抗剂
公开(公告)号：US20080260638A1
公开(公告)日：2008-10-23
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： A61K38/31 , 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。

2. 发明申请

US20050245438A1 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：US20050245438A1
公开(公告)日：2005-11-03
申请号：US11041676
申请日：2005-01-24
申请人： Jean Rivier , Jean Reubi , Judit Erchegyi , Roland Riek
发明人： Jean Rivier , Jean Reubi , Judit Erchegyi , Roland Riek
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-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。

3. 发明申请

US20080299040A1 SOMATOSTATIN RECEPTOR 2 ANTAGONISTS 有权
标题翻译： SOMATOSTATIN受体2拮抗剂
公开(公告)号：US20080299040A1
公开(公告)日：2008-12-04
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： A61K51/08 , C07K7/64 , A61P35/00 , A61K38/12
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。

4. 发明授权

US4552864A Gonadoliberin derivatives process for the preparation and pharmaceutical compositions thereof 失效
标题翻译：用于制备其性腺素的衍生物方法及其药物组合物
公开(公告)号：US4552864A
公开(公告)日：1985-11-12
申请号：US608261
申请日：1984-05-04
申请人： Ferenc Antoni , Judit Erchegyi , Aniko Horvath , Gyorgi Keri , Imre Mezo , Karoly Nikolics , Janos Seprodi , Andras Szell , Balazs Szoke , Istvan Teplan
发明人： Ferenc Antoni , Judit Erchegyi , Aniko Horvath , Gyorgi Keri , Imre Mezo , Karoly Nikolics , Janos Seprodi , Andras Szell , Balazs Szoke , Istvan Teplan
IPC分类号： A61K38/00 , C07K7/23 , C07K14/00 , C07K14/575 , A61K37/00
CPC分类号： C07K7/23 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： The invention relates to new gonadoliberin derivatives of the formula (I)Glp-His-Trp-Ser-Tyr-X-Leu-Arg-Pro-Y, (I)whereinY represents a glycine-amide group or an -NH-alkyl group having 1 to 4 carbon atoms in the alkyl moiety,X stands for a D-thyroxyl, D-thyronyl or D-4-chlorophenylalanyl group,and acid addition salts and metal complexes thereof.The new nona- and decapeptide derivatives have an excellent luteinizing and folliculus stimulating hormone releasing activity, and they can therefore be used as active ingredients in pharmaceutical compositions for human or veterinary application.
摘要翻译： PCT No.PCT / HU83 / 00028 Sec。 371日期1984年1月11日 102（e）日期1984年1月11日PCT提交1983年5月25日PCT公布。出版物WO83 / 04250 1983年12月8日，本发明涉及式（I）Glp-His-Trp-Ser-Tyr-X-Leu-Arg-Pro-Y，（I）的新的性腺激肽衍生物，其中Y代表甘氨酰胺基团或在烷基部分具有1至4个碳原子的-NH-烷基，X表示D-甲醛，D-甲苯甲酰或D-4-氯苯丙氨酰基，以及其酸加成盐和金属络合物。新的非 - 和十肽衍生物具有优异的促黄体激素和促卵泡激素释放活性，因此它们可以用作用于人或兽医应用的药物组合物中的活性成分。

5. 发明申请

US20110269683A1 RECEPTOR(SSTR2)-SELECTIVE SOMATOSTATIN ANTAGONISTS 有权
标题翻译：受体（SSTR2） - 选择性SOMATOSTATIN拮抗剂
公开(公告)号：US20110269683A1
公开(公告)日：2011-11-03
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 , A61P35/00 , A61P43/00 , C07K7/64
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。

6. 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。

7. 发明授权

US4751215A Process for increasing the sexual activity of birds and useful domestic mammals and for preparing spermatozoa suitable to their propagation 失效
标题翻译：增加鸟类和有用的家养哺乳动物的性活动和准备适合其繁殖的精子的过程
公开(公告)号：US4751215A
公开(公告)日：1988-06-14
申请号：US852217
申请日：1986-04-15
申请人： Janos Seprodi , Zsolt Vadasz , Peter Peczely , Istvan Teplan , Judit Erchegyi , Tibor Muray , Istvan Gyorvari
发明人： Janos Seprodi , Zsolt Vadasz , Peter Peczely , Istvan Teplan , Judit Erchegyi , Tibor Muray , Istvan Gyorvari
IPC分类号： A61K38/04 , A61D19/00 , A61K38/00 , A61K38/22 , A61P15/00 , C07K7/23 , A61K37/24
CPC分类号： C07K7/23 , A61D19/00 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： The invention relates to a process for increasing the sexual activity of birds and useful domestic mammals and for preparing spermatozoa suitable to their propagation. The process of the invention comprises treating sexually mature male birds or useful domestic mammals at least twice and at most four times with 0.1 to 5 .mu.g/kg of body weight of a compound of the general formula (I),Glp-His-Trp-Ser-Tyr-X.sub.1 -Leu-Arg-Pro-X.sub.4 (I)whereinX.sub.1 stands for a glycyl group, a natural or synthetic aminoacid or aminoacid derivative of D configuration, an -Asp-Q group of L configuration, wherein Q is attached to the .alpha.-carbonyl moiety of the aspartyl group and represents a C.sub.1-5 alkylamide, an arylamide, a C.sub.1-4 alkoxy or a benzyloxy group; andX.sub.4 stands for a glycylamide or a C.sub.1-4 alkylamide group,while keeping a pause of at least 30 hours and at most 72 hours between the consecutive treatments.The process of the invention can mainly be used in such large-scale breedings, where artificial insemination is employed but it can be used also for any domestic bird or cought wild-fowl and ornamental bird as well as useful domestic mammal under the conditions of the natural reproduction or artificial insemination.
摘要翻译：本发明涉及增加鸟类和有用的家养哺乳动物的性活性以及制备适于其繁殖的精子的方法。本发明的方法包括用0.1至5μg/ kg体重的通式（I）的化合物，Glp-His-Trp，将性成熟的雄性鸟类或有用的家用哺乳动物处理至少两次，最多四次 -Ser-Tyr-X1-Leu-Arg-Pro-X4（I）其中X1表示甘氨酰基，D构型的天然或合成氨基酸或氨基酸衍生物，L构型的-Asp-Q基团，其中Q为连接到天冬氨酰基的α-羰基部分，并且表示C1-5烷基酰胺，芳基酰胺，C1-4烷氧基或苄氧基; 并且X 4代表甘氨酰酰胺或C 1-4烷基酰胺基团，同时在连续处理之间保持至少30小时和至多72小时的停顿。本发明的方法主要用于大规模种植，其中人工授精使用，但也可用于任何家禽或被驯养的野禽和观赏鸟以及有用的国内哺乳动物自然繁殖或人工授精。

8. 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。

9. 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。

10. 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。

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