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公开(公告)号：US07498300B2
公开(公告)日：2009-03-03
申请号：US10763935
申请日：2004-01-22
IPC分类号： A61K38/00
CPC分类号： C07K14/47 , A61K38/00 , C07K14/57509
摘要： CRF peptide analogs that bind to CRFR1 with an affinity far greater than they bind to CRFR2. These analogs exhibit CRF agonist activity. One exemplary analog that may be made by solid-phase synthesis is (cyclo 31-34)[Ac-Pro4, D-Phe12, Nle21,38, Glu31, Lys34]-r/hCRF(4-41).
摘要翻译： 结合CRFR1的CRF肽类似物的亲和力远远大于它们与CRFR2结合的亲和力。 这些类似物表现出CRF激动剂活性。 可以通过固相合成制备的一个示例性类似物是（环31-34）[Ac-Pro4，D-Phe12，Nle21,38，Glu31，Lys34] -r / hCRF（4-41）。
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公开(公告)号：US07851588B2
公开(公告)日：2010-12-14
申请号：US12366816
申请日：2009-02-06
IPC分类号： A61K38/12
CPC分类号： C07K14/47 , A61K38/00 , C07K14/57509
摘要： CRF peptide analogs that bind to CRFR1 with an affinity far greater than they bind to CRFR2. Some of these analogs exhibit CRF agonist activity. One exemplary analog that may be made by solid-phase synthesis is:(cyclo 31-34)[Ac-Pro4,D-Phe12,Nle18,21,Glu31,Lys34]-sucker urotensin(4-41).
摘要翻译： 结合CRFR1的CRF肽类似物的亲和力远远大于它们与CRFR2结合的亲和力。 这些类似物中的一些表现出CRF激动剂活性。 可以通过固相合成制备的一个示例性类似物是：（环31-34）[Ac-Pro4，D-Phe12，Nle18,21，Glu31，Lys34]刺激性尿素转运蛋白（4-41）。
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公开(公告)号：US07141546B1
公开(公告)日：2006-11-28
申请号：US10210889
申请日：2002-07-31
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。
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公开(公告)号：US4661472A
公开(公告)日：1987-04-28
申请号：US732531
申请日：1985-05-09
申请人： Jean E. F. Rivier , Janos I. Varga , Arnold T. Hagler , R. Scott Struthers , Marilyn H. Perrin , Catherine L. Rivier , Wylie W. Vale, Jr.
发明人： Jean E. F. Rivier , Janos I. Varga , Arnold T. Hagler , R. Scott Struthers , Marilyn H. Perrin , Catherine L. Rivier , Wylie W. Vale, Jr.
IPC分类号： A61K38/04 , A61K38/00 , A61K38/22 , A61K38/27 , A61P5/00 , C07K7/06 , C07K7/23 , C07K14/00 , C07K14/575 , A61K37/43
CPC分类号： C07K7/23 , A61K38/00 , Y10S930/13
摘要： Peptides which inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. These peptides may be used to treat steroid-dependent tumors, such as prostatic and mammary tumors. The peptides are cyclic analogs of the decapeptide GnRH wherein there is a covalent bond between the residue in the 4-position and the residue in the 10-position. Examples of such bonds include the disulfide linkage between Cys residues, an amide linkage between a side chain amino group and a side chain carboxyl group, a dicarba linkage between side-chain alkyl groups, and a carba linkage between a side-chain alkyl group and a side-chain sulfhydryl group.
摘要翻译： 抑制垂体分泌促性腺激素并抑制性腺释放类固醇的肽。 施用有效量的这种GnRH拮抗剂防止雌性哺乳动物卵的排卵和/或性腺释放类固醇。 这些肽可用于治疗类固醇依赖性肿瘤，例如前列腺和乳腺肿瘤。 肽是十肽GnRH的环状类似物，其中在4-位的残基与10位的残基之间存在共价键。 这些键的实例包括Cys残基之间的二硫键，侧链氨基和侧链羧基之间的酰胺键，侧链烷基之间的二链键和侧链烷基与侧链烷基之间的碳键 侧链巯基。
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公开(公告)号：US06214797B1
公开(公告)日：2001-04-10
申请号：US08981189
申请日：1997-12-10
申请人： Wylie W. Vale, Jr. , Joan Vaughan , Cynthia J. Donaldson , Kathy A. Lewis , Paul Sawchenko , Jean E. F. Rivier , Marilyn H. Perrin
发明人： Wylie W. Vale, Jr. , Joan Vaughan , Cynthia J. Donaldson , Kathy A. Lewis , Paul Sawchenko , Jean E. F. Rivier , Marilyn H. Perrin
IPC分类号： A61K3817
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, &bgr;-endorphin, &bgr;-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.
摘要翻译： Urocortin（Ucn）是通常与促进素I和促皮质素释放因子（CRF）相关的天然哺乳动物肽。 人Ucn具有下式：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）。 大鼠衍生的Ucn是相同的，但是对于2个取代，As 2的Asp 2和Ser 4的Pro 4。 可以将Ucn或其类似物或药学上可接受的盐施用于人和其它哺乳动物，以实现ACTH，β-内啡肽，β-促脂解素，前 - 肌内注射皮质酮基因和皮质酮的其它产物的显着升高。 它们也可用于在较长时间内降低血压，作为兴奋剂提高心情，提高记忆力和学习表现以及诊断。 可以施用缩短的片段以释放脑中和外周的内源性CRF和/或Ucn。 Ucn拮抗剂可用于阻断Ucn和/或CRF的作用，以及Ucn的抗体。 标记的Uc激动剂和拮抗剂可与CRF受体一起用于药物筛选测定; 它们也可以与Ucn抗体一起在诊断上使用。
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公开(公告)号：US09035022B2
公开(公告)日：2015-05-19
申请号：US13996186
申请日：2011-12-22
申请人： Jean E. F. Rivier
发明人： Jean E. F. Rivier
IPC分类号： A61K38/00 , C07K14/47 , C07K14/575
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。
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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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公开(公告)号：US07019109B2
公开(公告)日：2006-03-28
申请号：US10099240
申请日：2002-03-15
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。
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