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1.发明申请公开(公告)号：US20060025344A1
公开(公告)日：2006-02-02
申请号：US11158348
申请日：2005-06-20
申请人： Birgitte Lange , Thue Schwartz , Thomas Frimurer , Oystein Rist
发明人： Birgitte Lange , Thue Schwartz , Thomas Frimurer , Oystein Rist
IPC分类号： A61K38/22 , C07K14/575
CPC分类号： G01N33/74 , A61K31/00 , A61K38/046 , G01N2333/726 , G01N2500/02
摘要： Compounds of the invention act as inverse agonist ghrelin receptors. Some of the compounds of the invention may have both inverse agonistic and antagonistic properties as they both decrease or eliminate the constitutive activity of he ghrelin receptor and block the effect of ghrelin. Other preferred compounds of the invention have inverse agonistic properties but have little or no antagonistic activity. The compounds are suitable for medical and/or cosmetic use in connection with modulation of feeding behaviors, body composition and reduction of body mass. The invention also relates to methods for identifying inverse agonists for the ghrelin receptor and for monitoring the further development of such compounds.
摘要翻译： 本发明的化合物作为反向激动剂ghrelin受体。 本发明的一些化合物可以具有反向激动和拮抗性质，因为它们都降低或消除了生长素释放肽受体的组成型活性并阻断了生长素释放肽的作用。 本发明的其它优选化合物具有反向激动性质但具有很少或没有拮抗活性。 该化合物适用于与调节进食行为，身体组成和减少体重有关的医疗和/或化妆品用途。 本发明还涉及用于鉴定生长素释放肽受体的反向激动剂并监测这些化合物的进一步发展的方法。
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公开(公告)号：US20110251126A1
公开(公告)日：2011-10-13
申请号：US13062932
申请日：2009-09-11
CPC分类号： A61K38/2271
摘要： Y4 receptor agonists which are selective for the Y4 receptor over the Y1 and Y2 receptors, are useful in the prevention and/or treatment of damage to bowel function caused by radiation therapy, radiation exposure, cytotoxic chemotherapy, inflammation, or ischemia-reperfusion of intestinal mucosa.
摘要翻译： 对Y1和Y2受体的Y4受体有选择性的Y4受体激动剂可用于预防和/或治疗由放射治疗，放射线暴露，细胞毒性化疗，炎症或肠缺血再灌注引起的肠功能损伤 粘膜
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公开(公告)号：US08022035B2
公开(公告)日：2011-09-20
申请号：US12067392
申请日：2005-09-21
IPC分类号： A61K38/22 , C07K14/575
CPC分类号： C07K14/5759 , A61K38/00
摘要： Y4 receptor agonist peptide selected from the group consisting of: [Ala30]PP2-36, [Thr30]PP2-36, [Asn30]PP2-36, [Gln30]PP2-36, [Glu10]PP2-36, [Glu10,Leu17,Thr30]PP2-36, [Nle17,Nle30]PP2-36, [Glu10,Nle17,Nle30]PP2-36, their PP1-36 equivalents, and analogues and derivatives thereof as described in the specification, are selective agonists of the Y4 receptor relative to the Y1 and Y2 receptors, and are useful in the treatment, for example, of obesity and overweight, and conditions in which these are considered contributory factors, and in the treatment of diarrhoea and intestinal hypersecretion.
摘要翻译： Y3受体激动剂肽，其选自：[Ala30] PP2-36，[Thr30] PP2-36，[Asn30] PP2-36，[Gln30] PP2-36，[Glu10] PP2-36，[Glu10，Leu17 ，Thr30] PP2-36，[Nle17，Nle30] PP2-36，[Glu10，Nle17，Nle30] PP2-36，它们的PP1-36当量及其如本说明书所述的其类似物和衍生物是Y4的选择性激动剂 受体相对于Y1和Y2受体，并且可用于例如肥胖和超重的治疗，以及其被认为是促成因素的病症，以及用于治疗腹泻和肠分泌过多的症状。
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公开(公告)号：US07851590B2
公开(公告)日：2010-12-14
申请号：US12067409
申请日：2005-09-21
申请人： Thue Schwartz , Feng Wang
发明人： Thue Schwartz , Feng Wang
IPC分类号： C07K14/435
CPC分类号： C07K14/57545 , A61K38/00 , A61K47/60 , A61K47/61 , A61K47/643 , C07K14/575
摘要： The modified human PP peptides (i) [Lys4,Leu17,Ser30,Gln34]hPP, (ii) Lys4,Leu17,Thr30,Gln34]hPP; and (iii) [Lys4,Leu17,oxidised Met30,Gln34]hPP wherein “oxidised Met” may be the sulfoxide or sulfone, and certain analogues and derivatised forms thereof as referred to in the specification, are selective agonists of the Y2 receptor relative to the Y1 and Y4 receptors, and are useful for, for example, appetite control and therapeutic angiogenesis.
摘要翻译： 修饰的人PP肽（i）[Lys4，Leu17，Ser30，Gln34] hPP，（ii）Lys4，Leu17，Thr30，Gln34] hPP; 和（iii）[Lys4，Leu17，氧化的Met30，Gln34] hPP，其中“氧化的Met”可以是亚砜或砜，并且其在本说明书中提及的某些类似物和衍生形式是Y2受体的选择性激动剂相对于 Y1和Y4受体，并且可用于例如食欲控制和治疗性血管发生。
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公开(公告)号：US20080269114A1
公开(公告)日：2008-10-30
申请号：US10592779
申请日：2005-03-17
申请人： Thue Schwartz
发明人： Thue Schwartz
CPC分类号： C07K14/575 , A61K38/00
摘要： Y4 receptor agonists selective for the Y4 receptor over the Y1 and Y2 receptors are useful for treatment of conditions responsive to activation of Y4 receptors. The Y4 selective agonists (a) are PP-fold peptide or PP-fold peptide mimics which have C— and N-terminal sequence features as specified in the description or (b) have an covalent intramolecular link, or (c) comprise two covalently linked C-terminal Y4 receptor-recognition amino acid sequences each of which comprises the last four residues of a C-terminal receptor recognition sequence of the type (a) agonists.
摘要翻译： 对Y1和Y2受体的Y4受体有选择性的Y4受体激动剂可用于治疗对Y4受体活化作出反应的病症。 Y4选择性激动剂（a）是PP-折叠肽或PP-折叠肽模拟物，其具有如说明书中所述的C-和N-末端序列特征，或（b）具有共价分子内连接，或（c）共价二价 连接的C末端Y4受体识别氨基酸序列，其各自包含类型（a）激动剂的C末端受体识别序列的最后四个残基。
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公开(公告)号：US20080261871A1
公开(公告)日：2008-10-23
申请号：US10592688
申请日：2005-03-17
申请人： Thue Schwartz
发明人： Thue Schwartz
CPC分类号： C07K14/70571 , A61K38/00 , A61K38/22
摘要： Y receptor agonists which are selective for Y2 and Y4 receptors over the Y1 receptor are useful for treatment of, for example obesity, are (a) PP-fold peptides or PP-fold peptides mimics which have (i) a C-terminal Y receptor-recognition amino acid sequence represented by —X-Thr-Arg-X3-Arg-Tyr-C(=0)NR1R2 wherein R1 and R1 are independently hydrogen or C1-C6 alkyl X is Val, Ile, Leu or Ala, and X3 is Gln or Asn, or a conservatively substituted variant thereof in which Thr is replaced by His or Asn and/or Tyr is replaced by Trp or Phe; and/or Arg is replaced by Lys, and (ii) an N-terminal Y receptor-recognition amino acid sequence represented by H2N—X1-Pro-X2—(Glu or Asp)—wherein X1 is not present or is amino acid residue, and X2 is Leu or Ser or conservative substitutions of Leu or Ser, or (b) the said comprise a C-terminal Y receptor-recognition amino acid sequence as defined in (i) above, said Y receptor-recognition sequence being fused to an amphiphilic amino acid sequence domain comprising at least one alpha helical turn adjacent the N-terminus of the said hexapeptide sequence, said turn being constrained in a helical configuration by a covalent intramolecular link, and optionally an N-terminal sequence which commences with a Y receptor-recognition amino acid sequence as defined in (ii) above.
摘要翻译： 对Y 1受体上的Y2和Y4受体有选择性的Y受体激动剂可用于治疗，例如肥胖，（a）PP折叠肽或PP-折叠肽模拟物，其具有（i）C-末端Y受体 由-X-Thr-Arg-X 3 -Arg-Tyr-C（= 0）NR 1 R 2 O 2表示的识别氨基酸序列 其中R 1和R 2独立地是氢或C 1 -C 6烷基X是Val，Ile ，Leu或Ala，X 3是Gln或Asn或其保护性取代的变体，其中Thr被His或Asn替代和/或Tyr被Trp或Phe替代; 和/或Arg被Lys取代，和（ii）由H 2 -X 1 -Pro-X SUP表示的N末端Y受体识别氨基酸序列 > 2 - （Glu或Asp） - 其中X 1不存在或是氨基酸残基，X 2是Leu或Ser或保守取代 Leu或Ser，或（b）所述包含如上述（i）中定义的C末端Y受体识别氨基酸序列，所述Y受体识别序列与两亲氨基酸序列结构域融合，所述两亲性氨基酸序列结构域包含至少一个α 螺旋转相邻于所述六肽序列的N末端，所述转角通过共价分子链接被限制在螺旋构型中，并且任选地由（ii）中定义的Y受体识别氨基酸序列开始的N末端序列 ） 以上。
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公开(公告)号：US20100160226A1
公开(公告)日：2010-06-24
申请号：US12597090
申请日：2008-04-21
CPC分类号： C07K14/575
摘要： Human Pancreatic Polypeptide mutants are provided which have utility, inter alia, for regulation of energy intake or energy metabolism, control of intestinal secretion, decrease of gastrointestinal tract motility, decrease of rate of gastric emptying, treatment of obesity or overweight, or conditions in which obesity or overweight is a contributory factor.
摘要翻译： 提供了人类胰腺多肽突变体，其具有用于调节能量摄入或能量代谢，肠分泌调控，胃肠道运动性降低，胃排空率降低，肥胖或超重治疗，或其中 肥胖或超重是一个促成因素。
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公开(公告)号：US20090186811A1
公开(公告)日：2009-07-23
申请号：US10592722
申请日：2005-03-17
申请人： Thue Schwartz
发明人： Thue Schwartz
CPC分类号： C07K14/70571 , A61K8/64 , A61K38/22 , A61K38/2271 , A61Q19/06
摘要： Y receptor agonists other than PYY 3-36, which are selective for the Y2 receptor over the Y1 and Y4 receptors, and their use in the treatment of conditions responsive to activation of Y2 receptors, are disclosed. Broadly, a Y2-selective agonist is one which (a) is a PP-fold peptide or PP-fold peptide mimic selected from PYY, NPY, PYY mimics and NPY mimics which have a C-terminal Y2 receptor-recognition amino acid sequence and have various modifications relative to the natural peptides or (b) a PP-fold peptide or PP-fold peptide mimic selected from PP and PP-mimics which have a C-terminal Y2 receptor-recognition amino acid sequence and which have various modifications relative to the natural peptide or (c) comprise a C-terminal Y2 receptor-recognition amino acid sequence fused at its N-terminus to an amphiphilic amino acid sequence domain comprising at least one alpha helical turn adjacent the N-terminus of the said Y2 receptor-recognition sequence, said turn being constrained in a helical configuration by a covalent intramolecular link, and (ii), in the case where the agonist has an N-terminal structure analogous to NPY or PYY, having one or more of the modifications listed in (a) above and, in the case where the agonist has an N-terminal structure analogous to PP, having one or more of the modifications listed in (b) above.
摘要翻译： 公开了除YY和Y4受体之外对Y2受体有选择性的PYY 3-36以外的Y受体激动剂及其在治疗对Y2受体活化的反应的条件中的用途。 广泛地，Y2选择性激动剂是（a）是选自具有C末端Y2受体识别氨基酸序列的PYY，NPY，PYY模拟物和NPY模拟物的PP-折叠肽或PP-折叠肽模拟物， 具有相对于天然肽的各种修饰，或（b）选自具有C末端Y2受体识别氨基酸序列的PP和PP-模拟物的PP折叠肽或PP折叠肽模拟物，并且相对于 天然肽或（c）包含在其N-末端与两亲氨基酸序列结构域融合的C-末端Y 2受体识别氨基酸序列，其包含与所述Y2受体结合位点的N末端相邻的至少一个α螺旋转角， 所述转录通过共价分子链接被限制在螺旋构型中，和（ii）在激动剂具有类似于NPY或PYY的N-末端结构的情况下，具有一个或多个在 a）上面和中 激动剂具有类似于PP的N-末端结构，具有上述（b）中列出的一个或多个修饰的情况。
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公开(公告)号：US20090118178A1
公开(公告)日：2009-05-07
申请号：US12067392
申请日：2005-09-21
CPC分类号： C07K14/5759 , A61K38/00
摘要： Y4 receptor agonist peptide selected from the group consisting of: [Ala30]PP2-36, [Thr30]PP2-36, Asn30]PP2-36, [Gln30]PP2-36, [Glu10]PP2-36, [Glu10,Leu17,Thr30]PP2-36, [Nle17,Nle30]PP2-36, [Glu10,Nle17,Nle30]PP2-36, their PP1-36 equivalents, and analogues and derivatives thereof as described in the specification, are selective agonists of the Y4 receptor relative to the Y1 and Y2 receptors, and are useful in the treatment, for example, of obesity and overweight, and conditions in which these are considered contributory factors, and in the treatment of diarrhoea and intestinal hypersecretion.
摘要翻译： 选自以下的Y4受体激动剂肽：[Ala30] PP2-36，[Thr30] PP2-36，Asn30] PP2-36，[Gln30] PP2-36，[Glu10] PP2-36，[Glu10，Leu17， Thr30] PP2-36，[Nle17，Nle30] PP2-36，[Glu10，Nle17，Nle30] PP2-36，它们的PP1-36当量及其如本说明书所述的类似物和衍生物是Y4受体的选择性激动剂 相对于Y1和Y2受体，并且可用于例如肥胖和超重的治疗，以及这些被认为是促成因素的病症，以及用于治疗腹泻和肠分泌过多的症状。
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公开(公告)号：US20080255046A1
公开(公告)日：2008-10-16
申请号：US12067409
申请日：2005-09-21
申请人： Thue Schwartz , Feng Wang
发明人： Thue Schwartz , Feng Wang
CPC分类号： C07K14/57545 , A61K38/00 , A61K47/60 , A61K47/61 , A61K47/643 , C07K14/575
摘要： The modified human PP peptides (i) [Lys4,Leu17,Ser30,Gln34]hPP, (ii) Lys4,Leu17,Thr30,Gln34]hPP; and (iii) [Lys4,Leu17,oxidised Met30,Gln34]hPP wherein “oxidised Met” may be the sulfoxide or sulfone, and certain analogues and derivativatised forms thereof as referred to in the specification, are selective agonists of the Y2 receptor relative to the Y1 and Y4 receptors, and are useful for, for example, appetite control and therapeutic angiogenesis.
摘要翻译： 修饰的人PP肽（i）[Lys4，Leu17，Ser30，Gln34] hPP，（ii）Lys4，Leu17，Thr30，Gln34] hPP; 和（iii）[Lys4，Leu17，氧化的Met30，Gln34] hPP，其中“氧化的Met”可以是亚砜或砜，并且其在本说明书中提及的某些类似物和衍生化形式是Y2受体的选择性激动剂相对于 Y1和Y4受体，并且可用于例如食欲控制和治疗性血管发生。
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