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61. 发明授权

US4728726A GRF analogs IIIb 失效
标题翻译： GRF类似物IIIb
公开(公告)号：US4728726A
公开(公告)日：1988-03-01
申请号：US939342
申请日：1986-12-08
申请人： Jean E. F. Rivier , Wylie W. Vale, Jr.
发明人： Jean E. F. Rivier , Wylie W. Vale, Jr.
IPC分类号： A61K38/00 , C07K14/60 , C07K7/10
CPC分类号： C07K14/60 , A61K38/00 , Y10S930/12 , Y10S930/32
摘要： Human GRF(hGRF), rat GRF(rGRF), porcine GRF(pGRF), ovine GRF(oGRF) and bovine GRF(bGRF) have been earlier characterized and synthesized. The invention provides synthetic peptides which are extremely potent in stimulating the release of pituitary GH in animals, including humans, which have resistance to enzymatic degradation in the body, and which contain the sequence: R.sub.1 -R.sub.2 -R.sub.3 -Ala-Ile-Phe-Thr-R.sub.8 -Ser-R.sub.10 -Arg-R.sub.12 -R.sub.13 -R.sub.14 -R.sub.15 -Gln-R.sub.17 -R.sub.18 -Ala-Arg-Lys-Leu-R.sub.23 -R.sub.24 -R.sub.25 -Ile-R.sub.27 -R.sub.28 -R.sub.29 -R.sub.30 -R.sub.31 -R.sub.32, wherein R.sub.1 is Tyr, D-Tyr, Met, Phe, D-Phe, pCl-Phe, Leu, His or D-His having either a C.sup.a Me or N.sup.a Me substitution or being unsubstituted; R.sub.2 is Ala, D-Ala or D-NMA; R.sub.3 is Asp or D-Asp; R.sub.8 is Ser, Asn, D-Ser or D-Asn; R.sub.10 is Tyr or D-Tyr; R.sub.12 is Arg or Lys; R.sub.13 is Ile or Val; R.sub.14 is Leu or D-Leu, R.sub.15 is Gly or D-Ala; R.sub.17 is Leu or D-Leu; R.sub.18 is Tyr or Ser; R.sub.23 is Leu or D-Leu; R.sub.24 is His or Gln; R.sub.25 is Glu, Asp, D-Glu or D-Asp; R.sub.27 is Met, D-Met, Ala, Nle, Ile, Leu, Nva or Val; R.sub.28 is Asn, Ser or desR.sub.28 ; R.sub.29 is Arg, D-Arg or desR.sub.29 ; R.sub.30 is Gln or desR.sub.30 ; R.sub.31 is Glu or desR.sub.31 ; and R.sub.32 is Gly or desR.sub.32. These peptides as well as their nontoxic salts may also be used diagnostically.
摘要翻译：人GRF（hGRF），大鼠GRF（rGRF），猪GRF（pGRF），羊GRF（oGRF）和牛GRF（bGRF）已被早期表征和合成。本发明提供了合成肽，其在刺激体内对酶降解的动物（包括人）的垂体GH的释放方面非常有效，并且含有以下序列：R1-R2-R3-Ala-Ile-Phe- Thr-R8-Ser-R10-Arg-R12-R13-R14-R15-Gln-R17-R18-Al-Arg-Lys-Leu-R23-R24-R25-Ile-R27-R28-R29-R30-R31 -R32，其中R1是具有CaMe或NaMe取代或未取代的Tyr，D-Tyr，Met，Phe，D-Phe，pCl-Phe，Leu，His或D-His; R2是Ala，D-Ala或D-NMA; R3是Asp或D-Asp; R8是Ser，Asn，D-Ser或D-Asn; R10是Tyr或D-Tyr; R12是Arg或Lys; R13是Ile或Val; R14为Leu或D-Leu，R15为Gly或D-Ala; R17是Leu或D-Leu; R18是Tyr或Ser; R23为Leu或D-Leu; R24是His或Gln; R25是Glu，Asp，D-Glu或D-Asp; R27是Met，D-Met，Ala，Nle，Ile，Leu，Nva或Val; R28为Asn，Ser或desR28; R29是Arg，D-Arg或desR29; R30是Gln或desR30; R31是Glu或desR31; 而R32是Gly或desR32。这些肽以及它们的无毒盐也可以在诊断上使用。

62. 发明授权

US4626523A GRF analogs II 失效
标题翻译： GRF类似物II
公开(公告)号：US4626523A
公开(公告)日：1986-12-02
申请号：US742736
申请日：1985-06-10
申请人： Wylie W. Vale, Jr. , Jean E. F. Rivier
发明人： Wylie W. Vale, Jr. , Jean E. F. Rivier
IPC分类号： A23K1/16 , A61K38/00 , C07K14/60 , C07K7/10 , A61K37/24
CPC分类号： C07K14/60 , A23K20/147 , A61K38/00 , Y10S930/32
摘要： Human pancreatic GRF(hpGRF) and rat hypothalamic GRF(rhGRF) have been earlier characterized and synthesized. The invention provides synthetic peptides which are extremely potent in stimulating the release of pituitary GH in animals, including humans, which are resistant to enzymatic degradation in the body, and which have the sequence: R.sub.1 -Ala-R.sub.3 -Ala-Ile-Phe-Thr-R.sub.8 -Ser-R.sub.10 -Arg-R.sub.12 -R.sub.13 -Leu-R.sub.15 -Gln-Leu-R.sub.18 -Ala-Arg-Lys-Leu-Leu-R.sub.24 -R.sub.25 -Ile-R.sub.27 -R.sub.28 -Arg-Gln-Gln-Gly-Glu-R.sub.34 -Asn-Gln-Glu-R.sub.38 -R.sub.39 -R.sub.40 -Arg-R.sub.42 -R.sub.43 -R.sub.44 -Y wherein R.sub.1 is Tyr, D-Tyr, Met, Phe, D-Phe, pCl-Phe, Leu, His or D-His having either a C.sup.a Me or N.sup.a Me substitution; R.sub.3 is Asp or D-Asp; R.sub.8 is Ser, Asn, D-Ser or D-Asn; R.sub.10 is Tyr or D-Tyr; R.sub.12 is Arg or Lys; R.sub.13 is Ile or Val; R.sub.15 is Gly or D-Ala; R.sub.18 is Tyr or Ser; R.sub.24 is His or Gln; R.sub.25 is Glu or Asp; R.sub.27 is Met, Ala, Nle, Ile, Leu, Nva or Val; R.sub.28 is Asn or Ser; R.sub.34 is Arg or Ser; R.sub.38 is Gln or Arg; R.sub.39 is Arg or Gly; R.sub.40 is Ser or Ala; R.sub.42 is Phe or Ala; R.sub.43 is Asn or Arg; R.sub.44 is a natural amino acid. Any or all of the residues between R.sub.28 and R.sub.44, inclusive, can be deleted, and the carboxyl moiety of the amino acid residue at the C-terminus can be the radical --COOR,--CRO,--CONHNHR,--CON(R) (R') or --CH.sub.2 OR, with R and R' being lower alkyl, fluoro lower alkyl or hydrogen. These peptides as well as nontoxic salts thereof may be administered to animals, including humans and cold-blooded animals, to stimulate the release of GH and may be used diagnostically.
摘要翻译：人胰腺GRF（hpGRF）和大鼠下丘脑GRF（rhGRF）已被早期表征和合成。本发明提供了合成肽，其在刺激对包括人在内的动物（包括人）在内的动物体内释放垂体GH是非常有效的，其具有以下序列：R1-Ala-R3-Ala-Ile-Phe- Thr-R8-Ser-R10-Arg-R12-R13-Leu-R15-Gln-Leu-R18-Aa-Arg-Lys-Leu-Leu-R24-R25-Ile-R27-R28-Arg-Gln-Gln -Gly-Glu-R34-Asn-Gln-Glu-R38-R39-R40-Arg-R42-R43-R44-Y其中R1是Tyr，D-Tyr，Met，Phe，D-Phe，pCl-Phe，Leu ，His或D-His具有CaMe或NaMe取代基; R3是Asp或D-Asp; R8是Ser，Asn，D-Ser或D-Asn; R10是Tyr或D-Tyr; R12是Arg或Lys; R13是Ile或Val; R15是Gly或D-Ala; R18是Tyr或Ser; R24是His或Gln; R25是Glu或Asp; R27是Met，Ala，Nle，Ile，Leu，Nva或Val; R28为Asn或Ser; R34是Arg或Ser; R38是Gln或Arg; R39是Arg或Gly; R40是Ser或Ala; R42是Phe或Ala; R43是Asn或Arg; R44是天然氨基酸。可以缺失R28和R44之间的任何或全部残基，其中C末端的氨基酸残基的羧基部分可以是基团-COOR，-CRO，-CONHNHR，-CON（R）（ R'）或-CH 2 OR，其中R和R'为低级烷基，氟低级烷基或氢。这些肽及其无毒盐可以施用于动物，包括人和冷血动物，以刺激GH的释放并且可以在诊断上使用。

63. 发明授权

US4528190A GRF Analogs IV 失效
标题翻译： GRF类似物IV
公开(公告)号：US4528190A
公开(公告)日：1985-07-09
申请号：US611844
申请日：1984-05-18
申请人： Wylie W. Vale, Jr. , Jean E. F. Rivier
发明人： Wylie W. Vale, Jr. , Jean E. F. Rivier
IPC分类号： C07K14/575 , A23K1/16 , A61K38/00 , A61K38/04 , A61K38/18 , A61K38/22 , A61K38/25 , A61P5/00 , C07K14/00 , C07K14/60 , C07K14/61 , C07C103/52 , A61K37/02
CPC分类号： C07K14/60 , A23K20/147 , A61K38/00 , Y10S930/12
摘要： Human GRF(hGRF), rat GRF(rGRF) porcine GRF(pGRF) and bovine GRF(bGRF) have been earlier characterized and synthesized. The invention provides synthetic peptides which are extremely potent in stimulating the release of pituitary GH in animals, including humans, which have resistance to enzymatic degradation in the body, and which have the sequence: R.sub.1 -R.sub.2 -R.sub.3 -Ala-Ile-Phe-Thr-R.sub.8 -Ser-R.sub.10 -Arg-R.sub.12 -R.sub.13 -R.sub.14 -R.sub.15 -Gln-R.sub.17 -R.sub.18 -Ala-Arg-Lys-Leu-R.sub.23 -R.sub.24 -R.sub.25 -Ile-R.sub.27 -R.sub.28 -R.sub.29 -Gln-Gln-Gly-Glu-R.sub.34 -Asn-Gln-Glu-R.sub.38 -R.sub.39 -R.sub.40 -Arg-R.sub.42 -R.sub.43 -R.sub.44 wherein R.sub.1 is Tyr, D-Tyr, Met, Phe, D-Phe, pCl-Phe, Leu, His or D-His having either a C.sup..alpha. Me or N.sup..alpha. Me substitution or being unsubstituted; R.sub.2 is Ala, D-Ala or D-NMA; R.sub.3 is Asp or D-Asp; R.sub.8 is Ser, Asn, D-Ser or D-Asn; R.sub.10 is Tyr or D-Tyr; R.sub.12 is Arg or Lys; R.sub.13 is Ile or Val; R.sub.14 is Leu or D-Leu; R.sub.15 is Gly or D-Ala; R.sub.17 is Leu or D-Leu; R.sub.18 is Tyr or Ser; R.sub.23 is Leu or D-Leu; R.sub.24 is His or Gln; R.sub.25 is Glu, Asp, D-Glu or D-Asp; R.sub.27 is Met, D-Met, Ala, Nle, Ile, Leu, Nva or Val; R.sub.28 is Asn or Ser; R.sub.29 is Arg or D-Arg; R.sub.34 is Arg or Ser; R.sub.38 is Gln or Arg; R.sub.39 is Arg or Gly; R.sub.40 is Ser or Ala; R.sub.42 is Phe, Ala or Val; R.sub.43 is Asn or Arg; R.sub.44 is a natural amino acid; provided however that any or all of the residues between R.sub.28 and R.sub.44, inclusive, may be deleted and provided also that R.sub.2 is D-NMA and/or R.sub.14 is D-Leu and/or R.sub.29 is D-Arg. These peptides as well as their nontoxic salts may also be used diagnostically.
摘要翻译：人GRF（hGRF），大鼠GRF（rGRF）猪GRF（pGRF）和牛GRF（bGRF）已被早期表征和合成。本发明提供了合成肽，其在刺激体内对酶降解的抗性的动物（包括人）中的垂体GH的释放方面非常有效，并且具有以下顺序：R1-R2-R3-Ala-Ile-Phe- Thr-R8-Ser-R10-Arg-R12-R13-R14-R15-Gln-R17-R18-Al-Arg-Lys-Leu-R23-R24-R25-Ile-R27-R28-R29-Gln-Gln -Gly-Glu-R34-Asn-Gln-Glu-R38-R39-R40-Arg-R42-R43-R44，其中R1是Tyr，D-Tyr，Met，Phe，D-Phe，pCl-Phe，Leu，His 或具有CαMe或NαMe取代或未被取代的D-His; R2是Ala，D-Ala或D-NMA; R3是Asp或D-Asp; R8是Ser，Asn，D-Ser或D-Asn; R10是Tyr或D-Tyr; R12是Arg或Lys; R13是Ile或Val; R14是Leu或D-Leu; R15是Gly或D-Ala; R17是Leu或D-Leu; R18是Tyr或Ser; R23为Leu或D-Leu; R24是His或Gln; R25是Glu，Asp，D-Glu或D-Asp; R27是Met，D-Met，Ala，Nle，Ile，Leu，Nva或Val; R28为Asn或Ser; R29为Arg或D-Arg; R34是Arg或Ser; R38是Gln或Arg; R39是Arg或Gly; R40是Ser或Ala; R42是Phe，Ala或Val; R43是Asn或Arg; R44是天然氨基酸; 但是R28和R44之间的任何或全部残基（包括端值）可以被缺失，并且还提供R2是D-NMA和/或R14是D-Leu和/或R29是D-Arg。这些肽以及它们的无毒盐也可以在诊断上使用。

64. 发明授权

US4489061A Treatment of male mammals 失效
标题翻译：治疗雄性哺乳动物
公开(公告)号：US4489061A
公开(公告)日：1984-12-18
申请号：US423734
申请日：1982-09-27
申请人： Catherine L. Rivier , Jean E. F. Rivier , Wylie W. Vale, Jr.
发明人： Catherine L. Rivier , Jean E. F. Rivier , Wylie W. Vale, Jr.
IPC分类号： A61K38/00 , C07K7/23 , A61K37/00
CPC分类号： C07K7/23 , A61K38/00 , Y10S930/13
摘要： Peptides which are LRF analogs that inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads can be effective to suppress androgen-dependent behavior when administered to male mammals. The peptides are LRF antagonists having a binding affinity at least about 15 times that exhibited by LRF and having an ICR.sub.50 of less than 1/1. Examples of peptides which may be used are those having the structure:R.sub.1 -R.sub.2 -R.sub.3 -D-Trp-Ser-Tyr-R.sub.4 -Leu-Arg-Pro-Gly-NH.sub.2 wherein R.sub.1 is selected from the group consisting of hydrogen, formyl, acetyl, acrylyl, benzoyl and allyl; R.sub.2 is selected from the group consisting of dehydro Pro, dehydro D-Pro, Thz and D-Thz; R.sub.3 is selected from the group consisting of pCl-D-Phe, pF-D-Phe, pNO.sub.2 -D-Phe and 3,4 Cl-D-Phe; R.sub.4 is selected from the group consisting of D-Trp and (imBzl) D-His; and Leu may be substituted by N.alpha.MeLeu.Effective suppression of androgen-dependent behavior is achieved at a daily dosage level of not more than about 3 mg. per Kg. of body weight.
摘要翻译：作为抑制垂体分泌促性腺激素并抑制性腺释放类固醇的LRF类似物的肽在施用于雄性哺乳动物时可有效抑制雄激素依赖性行为。肽是LRF拮抗剂，其结合亲和力至少约为LRF显示的约15倍，ICR50小于1/1。可以使用的肽的实例是具有以下结构的那些：R1-R2-R3-D-Trp-Ser-Tyr-R4-Leu-Arg-Pro-Gly-NH2，其中R1选自氢，甲酰基，乙酰基，丙烯酰基，苯甲酰基和烯丙基; R2选自脱氢Pro，脱氢D-Pro，Thz和D-Thz; R3选自pCl-D-Phe，pF-D-Phe，pNO 2 -D-Phe和3,4 C-D-Phe; R4选自D-Trp和（imBz1）D-His; Leu可被NαMeLeu取代。在不超过约3mg的日剂量水平下实现雄激素依赖性行为的有效抑制。每公斤的体重。

65. 发明授权

US4428942A Analogs of somatostatin 失效
标题翻译：生长抑素类似物
公开(公告)号：US4428942A
公开(公告)日：1984-01-31
申请号：US378748
申请日：1982-05-17
申请人： Jean E. F. Rivier , Wylie W. Vale, Jr. , Marvin R. Brown
发明人： Jean E. F. Rivier , Wylie W. Vale, Jr. , Marvin R. Brown
IPC分类号： A61K38/00 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/16 , Y10S930/26
摘要： Somatostatin-14 has the formula: ##STR1## Analogs that are more potent than somatostatin-14 in increasing electrolyte absorption in the gut without suppressing the secretion of GH, insulin and glucagon, or pharmaceutically acceptable salts thereof, dispersed in a pharmaceutically acceptable liquid or solid carrier, can be administered to mammals in the same manner as somatostatin to increase absorbtion of electrolytes for the treatment of diarrhea. In particular of the analogs, certain substitutions are made for Phe in the 11-position, sometimes in combination with deletions in the 4- and 5-positions and in the 12- and 13-positions. D-Cys may also be substituted in the 3- or 14-position. There may be some substitutions in the 6- and 10-positions, and the residues in the 1- and/or 2-positions may also be deleted or substituted.
摘要翻译：生长抑素-14具有以下分子式：在增加电解质吸收的肠道中比抑制生长抑素-14更有效的类似物，而不抑制分散在药学上可接受的液体中的GH，胰岛素和胰高血糖素或其药学上可接受的盐的分泌，固体载体可以以与生长抑素相同的方式施用于哺乳动物以增加用于治疗腹泻的电解质的吸收。特别是类似物，对11位的Phe进行某些取代，有时与4位和5位以及12位和13位的缺失相结合。 D-Cys也可以在3-或14-位取代。在6-位和10位可能有一些取代，1-和/或2-位的残基也可以被缺失或取代。

66. 发明授权

US4409208A GnRH antagonists 失效
标题翻译： GnRH拮抗剂
公开(公告)号：US4409208A
公开(公告)日：1983-10-11
申请号：US256063
申请日：1981-04-21
申请人： Jean E. F. Rivier , Wylie W. Vale, Jr.
发明人： Jean E. F. Rivier , Wylie W. Vale, Jr.
IPC分类号： C07K14/575 , A61K38/00 , A61K38/04 , A61P43/00 , C07C231/00 , C07K1/113 , C07K7/16 , C07K7/23 , A61K37/00 , C07C103/52
CPC分类号： C07K7/16 , C07K7/23 , A61K38/00 , Y10S514/80 , 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 prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. The peptides have the structure.X-R.sub.1 -R.sub.2 -R.sub.3 -Ser-Tyr-R.sub.4 -R.sub.5 -Arg-Pro-R.sub.6wherein X is hydrogen or an acyl group having 7 or less carbon atoms; R.sub.1 is dehydro Pro or dehydro D-Pro; R.sub.2 is D-Phe, Cl-D-Phe, dichloro-D-Phe, CF.sub.3 -D-Phe, F-D-Phe, difluoro-D-Phe, AcNH-D-Phe, NO.sub.2 -D-Phe, dinitro-D-Phe, Br-D-Phe, dibromo-D-Phe, CH.sub.3 -S-D-Phe, OCH.sub.3 -D-Phe or CH.sub.3 -D-Phe; R.sub.3 is D-Trp or .beta.-(naphthyl)-D-Ala; R.sub.4 is a D-isomer aromatic amino acid or .beta.-(naphthyl)-D-Ala; R.sub.5 is Leu or N.alpha.Me-Leu; and R.sub.6 is Gly-NH.sub.2 or NHCH.sub.2 CH.sub.3 ; provided however that either R.sub.3 or R.sub.4 is .beta.-(naphthyl)-D-Ala.
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。施用有效量防止雌性哺乳动物卵的排卵和/或性腺释放类固醇。肽具有结构。 X-R1-R2-R3-Ser-Tyr-R4-R5-Arg-Pro-R6其中X是氢或具有7个或更少碳原子的酰基; R1是脱氢Pro或脱氢D-Pro; R2是D-Phe，C1-D-Phe，二氯-D-Phe，CF3-D-Phe，FD-Phe，二氟-D-Phe，AcNH-D-Phe，NO2-D-Phe，二硝基-D- Phe，Br-D-Phe，二溴-D-Phe，CH3-SD-Phe，OCH3-D-Phe或CH3-D-Phe; R3是D-Trp或β-（萘基）-D-Ala; R4是D-异构体芳族氨基酸或β-（萘基）-D-Ala; R5是Leu或NαMe-Leu; R6为Gly-NH2或NHCH2CH3; 但是R3或R4是β-（萘基）-D-Ala。

67. 发明授权

US4377574A Contraceptive treatment of male mammals 失效
标题翻译：雄性哺乳动物的避孕治疗
公开(公告)号：US4377574A
公开(公告)日：1983-03-22
申请号：US272968
申请日：1981-06-12
申请人： Catherine L. Rivier , Jean E. F. Rivier , Wylie W. Vale, Jr.
发明人： Catherine L. Rivier , Jean E. F. Rivier , Wylie W. Vale, Jr.
IPC分类号： A61K38/00 , C07K7/23 , A61K37/00 , C07C103/52
CPC分类号： C07K7/23 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： Peptides which are LRF analogs that inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads can be effective contraceptives when administered to male mammals. The peptides are LRF antagonists having a binding affinity at least about 15 times that exhibited by LRF and having an ICR.sub.50 of less than 1/l. Examples of peptides which may be used are those having the structure:R.sub.1 --R.sub.2 --R.sub.3 --D--Trp--Ser--Tyr--R.sub.4 --Leu--Arg--Pro--Gly--NH.sub.2wherein R.sub.1 is selected from the group consisting of hydrogen, formyl, acetyl, acrylyl, benzoyl and allyl; R.sub.2 is selected from the group consisting of dehydro Pro, dehydro D--Pro, Thz and D--Thz; R.sub.3 is selected from the group consisting of pCl--D--Phe, pF--D--Phe, pNO.sub.2 --D--Phe and 3,4 Cl--D--Phe; R.sub.4 is selected from the group consisting of D--Trp and (imBzl) D--His; and Leu may be substituted by N MeLeu.Effective contraception is achieved at a daily dosage level of not more than about 3 mg. per Kg. of body weight.
摘要翻译：作为LRP类似物的肽，其通过垂体抑制促性腺激素的分泌并且抑制性腺释放类固醇在施用于雄性哺乳动物时可以是有效的避孕药。肽是LRF拮抗剂，其结合亲和力至少约为LRF显示的约15倍，ICR50小于1 / l。可以使用的肽的实例是具有以下结构的那些：R1-R2-R3-D-Trp-Ser-Tyr-R4-Leu-Arg-Pro-Gly-NH2，其中R1选自氢，甲酰基，乙酰基，丙烯酰基，苯甲酰基和烯丙基; R2选自脱氢Pro，脱氢D-Pro，Thz和D-Thz; R3选自pCl-D-Phe，pF-D-Phe，pNO 2 -D-Phe和3,4 C-D-Phe; R4选自D-Trp和（imBz1）D-His; Leu可被N MeLeu取代。在不超过约3mg的日剂量水平下实现有效的避孕。每公斤的体重。

68. 发明授权

US4372884A Pharmaceutically active peptides 失效
标题翻译：药学活性肽
公开(公告)号：US4372884A
公开(公告)日：1983-02-08
申请号：US675149
申请日：1976-04-08
申请人： Marvin R. Brown , Jean E. F. Rivier , Wylie W. Vale, Jr.
发明人： Marvin R. Brown , Jean E. F. Rivier , Wylie W. Vale, Jr.
IPC分类号： C07K14/575 , A61K38/00 , A61K38/04 , A61P5/00 , C07K1/113 , C07K14/655 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S930/16
摘要： Various peptides are described which inhibit the secretion of growth hormone by the pituitary gland and inhibit the release of glucagon and insulin by the pancreas.
摘要翻译：描述了抑制垂体生长激素分泌并抑制胰高血糖素和胰岛素释放的各种肽。

69. 发明授权

US4105603A Peptides which effect release of hormones 失效
标题翻译：影响释放HORMONES的肽
公开(公告)号：US4105603A
公开(公告)日：1978-08-08
申请号：US781580
申请日：1977-03-28
申请人： Wylie W. Vale, Jr. , Jean E. F. Rivier , Marvin R. Brown
发明人： Wylie W. Vale, Jr. , Jean E. F. Rivier , Marvin R. Brown
IPC分类号： A61K38/00 , A61K38/04 , A61K38/22 , A61P5/00 , C07K7/06 , C07K14/575 , C07K14/655 , C08L37/00 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/16 , Y10S930/26
摘要： The present invention relates to peptides which possess biological activity in respect to the inhibition of growth hormone, insulin secretion and glucagon secretion are provided. The peptides have fewer amino acid components than somatostatin and some of the peptides have dissociated activity.

70. 发明授权

US08084413B2 Urocortin-III and uses thereof 有权
标题翻译： Urocortin-III及其用途
公开(公告)号：US08084413B2
公开(公告)日：2011-12-27
申请号：US12266430
申请日：2008-11-06
申请人： Wylie W. Vale, Jr. , Kathy A. Lewis , Marilyn H. Perrin , Koichi S. Kunitake , Jean E. Rivier , Jozsef Gulyas
发明人： Wylie W. Vale, Jr. , Kathy A. Lewis , Marilyn H. Perrin , Koichi S. Kunitake , Jean E. Rivier , Jozsef Gulyas
IPC分类号： C07K14/00
CPC分类号： A61K38/2228 , A61K38/00 , C07K14/57509 , C07K14/695
摘要： A search of the public human genome database identified a human EST, GenBank accession number AW293249, which has high homology to known pufferfish urocortin sequences. The full length sequence was amplified from human genomic DNA and sequenced. Sequence homology comparisons of the novel sequence with human urocortin I and urocortin II revealed that the sequence encoded a novel human urocortin, which was designated urocortin III (UcnIII). While urocortin III does not have high affinity for either CRF-R1 or CRF-R2, the affinity for CRF-R2 is greater than the affinity for CRF-R1. Urocortin III is capable stimulating cyclic AMP production in cells expressing CRF-R2α or β. Thus, the affinity is high enough that urocortin III could act as a native agonist of CRF-R2. However, it is also likely that urocortin III is a stronger agonist of a yet to be identified receptor.
摘要翻译：公众人类基因组数据库的搜索确定了人类EST，GenBank登录号AW293249，其与已知的河豚urocortin序列具有高同源性。从人类基因组DNA扩增全长序列并进行测序。新序列与人尿皮质素I和尿皮质素II的序列同源性比较显示，该序列编码了一种新的人类urocortin，其命名为urocortin III（UcnIII）。虽然urocortin III对CRF-R1或CRF-R2没有高亲和力，但CRF-R2的亲和力大于对CRF-R1的亲和力。 Urocortin III能够刺激表达CRF-R2α或bgr的细胞中的环AMP产生。因此，亲和力足够高，使得尿皮质素III可以作为CRF-R2的天然激动剂。然而，urocortin III也可能是未被鉴定的受体的更强的激动剂。

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