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61. 发明授权

US5026685A NPY peptide analogs 失效
标题翻译： NPY肽类似物
公开(公告)号：US5026685A
公开(公告)日：1991-06-25
申请号：US219596
申请日：1988-07-15
申请人： Jaroslav H. Boublik , Jean E. F. Rivier , Marvin R. Brown , Neal A. Scott
发明人： Jaroslav H. Boublik , Jean E. F. Rivier , Marvin R. Brown , Neal A. Scott
IPC分类号： A61K38/00 , C07K14/575
CPC分类号： C07K14/57545 , A61K38/00
摘要： Human Neuropeptide Y(NPY) has the formula: H-Tyr-Pro-Ser-Lys-Pro-Asp-Asn-Pro-Gly-Glu-Asp-Ala- Pro-Ala-Glu-Asp-Met-Ala-Arg-Tyr-Tyr-Ser-Ala-Leu-Arg-His-Tyr- Ile-Asn-Leu-Ile-Thr-Arg-Gln-Arg-Tyr-NH.sub.2. Porcine and rat NPY have the same sequence except for Leu instead of Met in the 17-position. Porcine PYY is homologous having 11 different residues. NPY analogs wherein the N-terminus is shortened and which may contain one or more specific subsitutions for the naturally occurring residues, or pharmaceutically acceptable salts thereof, dispersed in a pharmaceutically acceptable liquid or solid carrier, can be administered to mammals, including humans, to substantially lower blood pressure over an extended period of time or to counteract hypertension.
摘要翻译：人神经肽Y（NPY）具有下式：H-Tyr-Pro-Ser-Lys-Pro-Asp-Asn-Pro-Gly-Glu-Asp-Ala- Pro-Ala-Glu-Asp-Met-Ala-Arg- Tyr-Tyr-Ser-Ala-Leu-Arg-His-Tyr-Ile-Asn-Leu-Ile-Thr-Arg-Gln-Arg-Tyr-NH2。猪和大鼠NPY具有相同的序列，除了Leu而不是17位的Met。猪PYY具有11个不同残基的同源物。 NPY类似物，其中N末端被缩短并且可以含有分散在药学上可接受的液体或固体载体中的天然存在的残基或其药学上可接受的盐的一个或多个特异性亚基，可以包括人哺乳动物在较长时间内显着降低血压或抵抗高血压。

62. 发明授权

US5002931A GRF analogs VII 失效
标题翻译： GRF类似物VII
公开(公告)号：US5002931A
公开(公告)日：1991-03-26
申请号：US53235
申请日：1987-05-22
申请人： Jean E. F. Rivier , Wylie W. Vale, Jr. , Catherine L. Rivier
发明人： Jean E. F. Rivier , Wylie W. Vale, Jr. , Catherine L. Rivier
IPC分类号： A61K38/00 , A61K38/04 , A61K38/25 , A61P5/00 , A61P15/00 , A61P35/00 , A61P43/00 , C07K14/00 , C07K14/575 , C07K14/60 , C07K14/61
CPC分类号： C07K14/60 , A61K38/00
摘要： 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: (B)R.sub.1 -R.sub.2 -R.sub.3 -Ala-Ile-Phe-Thr-R.sub.8 -Ser-(Q.sub.1)R.sub.10 - Arg-R.sub.12. (Q.sub.2)R.sub.13 -Leu-R.sub.15 -Gln-Leu-Ser-(Q.sub.3)Ala-Arg. R.sub.21 -(Q.sub.4)R.sub.22 -Leu-Gln-Asp-Ile-R.sub.27 -R.sub.28 -Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-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; B is H, C.sup.a Me, N.sup.a Me, desamino, Ac or For; R.sub.2 is Ala, D-Ala, NMA or D-NMA; R.sub.3 is Asp or D-Asp; R.sub.8 is Ser, Asn, Lys, Arg, Asp or Gln; R.sub.10 is Tyr, D-Tyr or Phe; R.sub.12 is Arg or Lys; R.sub.13 is Ile, Val, Leu or Ala; R.sub.15 is Gly or Ala; R.sub.21 is Lys, D-Lys or D-Arg; R.sub.22 is Leu, Ile, Ala or Val; R.sub.27 is Met, D-Met, Ala, Nle, Ile, Leu, Nva or Val; R.sub.28 is Asn or Ser; R.sub.42 is Phe, Ala or Val; R.sub.43 is Asn or Arg; R.sub.44 is a natural amino acid; Q.sub.1 -Q.sub.4 are either H or C.sup.a Me, provided however that any or all of the residues between R.sub.30 and R.sub.44, inclusive, may be deleted.These peptides as well as their nontoxic salts may also be used diagnostically.

63. 发明授权

US4784987A GRF analogs VI 失效
标题翻译： GRF类似物VI
公开(公告)号：US4784987A
公开(公告)日：1988-11-15
申请号：US60149
申请日：1987-06-10
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 , A61K37/43 , C07K7/10
CPC分类号： C07K14/60 , A61K38/00 , Y10S930/12
摘要： The invention provides peptides which are potent in stimulating the release of pituitary GH in fish and amphibians which have a substantial portion or all of the following sequence: R.sub.1 -R.sub.2 -R.sub.3 -R.sub.4 -R.sub.5 -Phe-R.sub.7 -R.sub.8 -R.sub.9 -Tyr-Arg-R.sub.12 -R.sub.13 -Leu-R.sub.15 -Gln-Leu-R.sub.18 -Ala-Arg-Lys-R.sub.22 -Leu-R.sub.24 -R.sub.25 -R.sub.26 -R.sub.27 -R.sub.28 -R.sub.29 -R.sub.30 -R.sub.31 -Gly-R.sub.33 -R.sub.34 -R.sub.35 -R.sub.36 -R.sub.37 -R.sub.38 -R.sub.39 -R.sub.40 -R.sub.41 -R.sub.42 -R.sub.43 -R.sub.44 -Ser wherein R.sub.1 is N-Me Tyr, Tyr, desNH.sub.2 -Tyr, D-Tyr, N-Et Tyr, N-Ip Tyr, N-Me His, His, desNH.sub.2 -His, D-His, N-Et His, and N-Ip His; R.sub.2 is Ala, D-Ala or D-NMA; R.sub.3 is Asp or D-Asp; R.sub.4 is Gly or Ala; R.sub.5 and R.sub.27 are selected from the group consisting of Met, Leu, Val, Nva, Gln, Thr, Ile, Ala, Arg, Asn, Asp, Cys, Glu, Gly, His, Nle, Lys, Phe, Pro, Ser, Tyr and Trp; R.sub.7 is Asn or Thr; R.sub.8 is Lys, Asn or Ser; R.sub. 9 is Ala or Ser; R.sub.12 is Lys or Arg; R.sub.13 is Ala, Val or Ile; R.sub.15 is Gly or Ala; R.sub.18 is Ser or Tyr; R.sub.22 is Tyr or Leu; R.sub.24 is His or Gln; R.sub.25 is Thr, Asp, or Glu; R.sub.26 is Leu or Ile; R.sub.28 is Ala, Ser or Asn; R.sub.29 is Lys or Arg; R.sub.30 is Arg or Gln; R.sub.31 is Val or Gln; R.sub.33 is Gly or Glu; R.sub.34 is Gly, Arg or Ser; R.sub.35 is Ser or Asn; R.sub.36 is Met, Leu, Val, Nva, Gln, Thr, Ile or Nle; R.sub.37 is Ile or Glu; R.sub.38 is Glu, Gln or Arg; R.sub.39 is Asp, Arg or Gly; R.sub.40 is Asp, Ser or Ala; R.sub.41 is Asn, Arg or Lys; R.sub.42 is Glu, Phe, Ala or Val; R.sub.43 is Pro, Asn or Arg; R.sub.44 is Leu or Ala; provided however that at least one of the following is present: R.sub.7 is Asn, R.sub.8 is Lys, R.sub.13 is Ala, R.sub.22 is Tyr and R.sub.25 is Thr; and provided further that any or all of the residues after R.sub.27 may be deleted. A 29-residue peptide beginning at the N-terminus may be preferred. These peptides, as well as their nontoxic salts, are considered to be particularly useful in aquiculture.
摘要翻译：本发明提供了有效刺激鱼和两栖类垂体GH释放的肽，其具有以下相当大部分或全部序列：R1-R2-R3-R4-R5-Phe-R7-R8-R9-Tyr- Arg-R12-R13-Leu-R15-Gln-Leu-R18-Ala-Arg-Lys-R22-Leu-R24-R25-R26-R27-R28-R29-R30-R31-Gly-R33-R34-R35 -R36-R37-R38-R39-R40-R41-R42-R43-R44-Ser其中R1是N-Me Tyr，Tyr，desNH2-Tyr，D-Tyr，N-Et Tyr，N-Ip Tyr，我是他的，他的，他的，他的，他的，N-Et他和N-Ip他; R2是Ala，D-Ala或D-NMA; R3是Asp或D-Asp; R4是Gly或Ala; R5和R27选自Met，Leu，Val，Nva，Gln，Thr，Ile，Ala，Arg，Asn，Asp，Cys，Glu，Gly，His，Nle，Lys，Phe，Pro，Ser， Tyr和Trp; R7为Asn或Thr; R8为Lys，Asn或Ser; R 9是Ala或Ser; R12为Lys或Arg; R13是Ala，Val或Ile; R15是Gly或Ala; R18为Ser或Tyr; R22是Tyr或Leu; R24是His或Gln; R25是Thr，Asp或Glu; R26是Leu或Ile; R28是Ala，Ser或Asn; R29为Lys或Arg; R30是Arg或Gln; R31为Val或Gln; R33是Gly或Glu; R34是Gly，Arg或Ser; R35是Ser或Asn; R36是Met，Leu，Val，Nva，Gln，Thr，Ile或Nle; R37是Ile或Glu; R38是Glu，Gln或Arg; R39为Asp，Arg或Gly; R40是Asp，Ser或Ala; R41是Asn，Arg或Lys; R42是Glu，Phe，Ala或Val; R43是Pro，Asn或Arg; R44是Leu或Ala; 但是存在以下中的至少一种：R7是Asn，R8是Lys，R13是Ala，R22是Tyr，R25是Thr; 并进一步提供R27之后的任何或全部残基可被删除。从N末端开始的29个残基的肽可能是优选的。这些肽以及它们的无毒盐被认为在水产养殖中特别有用。

64. 发明授权

US4619914A GNRH antagonists IIIB 失效
标题翻译： GNRH拮抗剂IIIB
公开(公告)号：US4619914A
公开(公告)日：1986-10-28
申请号：US583093
申请日：1984-02-23
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： A61K38/00 , C07K7/23 , A61K37/43 , C07K7/20
CPC分类号： 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 -D-Trp-Ser-R.sub.5 -R.sub.6 -Leu-Arg-Pro-R.sub.10wherein X is hydrogen or an acyl group having 7 or less carbon atoms; R.sub.1 is dehydro-Pro, D-pGlu, D-Phe, D-Trp or .beta.-D-NAL; R.sub.2 is Cl-D-Phe, F-D-Phe, C.sup..alpha. Me-4-Cl-D-Phe, NO.sub.2 -D-Phe, Cl.sub.2 -D-Phe or Br-D-Phe; R.sub.5 is Tyr, I-Tyr, CH.sub.3 -Phe, F-Phe or Cl-Phe; R.sub.6 is a D-isomer of a lipophilic amino acid or is 4-NH.sub.2 -D-Phe, 4-gua-D-Phe, D-His, D-Lys, D-Orn, D-Har or D-Arg; and R.sub.10 is Gly-NH.sub.2, D-Ala-NH.sub.2 or NH-Y, with Y being lower alkyl, cycloalkyl, fluoro lower alkyl or ##STR1## where Q is H or lower alkyl. When R.sub.1 is .beta.-D-NAL, R.sub.6 is 4-NH.sub.2 -D-Phe, 4-gua-D-Phe, D-His, D-Lys, D-Orn, D-Har or D-Arg. When R.sub.5 is Tyr or 2-Cl-Phe, either (a) Orn, AAL or aBu is substituted for Ser, or (b) R.sub.1 is .beta.-D-NAL and R.sub.6 is D-His or 4-gua-D-Phe. N.sup..alpha. Me-Leu may optionally be substituted for Leu.
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。肽具有以下结构：X-R1-R2-D-Trp-Ser-R5-R6-Leu-Arg-Pro-R10，其中X是氢或具有7个或更少碳原子的酰基; R1是脱氢-Pro，D-pGlu，D-Phe，D-Trp或β-D-NAL; R2是Cl-D-Phe，F-D-Phe，CαMe-4-Cl-D-Phe，NO2-D-Phe，Cl2-D-Phe或Br-D-Phe; R5是Tyr，I-Tyr，CH3-Phe，F-Phe或C1-Phe; R6是亲脂性氨基酸的D-异构体，或者是4-NH2-D-Phe，4-gua-D-Phe，D-His，D-Lys，D-Orn，D-Har或D-Arg; 并且R 10是Gly-NH 2，D-Ala-NH 2或NH-Y，其中Y是低级烷基，环烷基，氟低级烷基或者其中Q是H或低级烷基。当R 1是β-D-NAL时，R 6是4-NH 2 -D-Phe，4-gua-D-Phe，D-His，D-Lys，D-Orn，D-Har或D-Arg。当R5为Tyr或2-Cl-Phe时，（a）Orn，AAL或aBu取代Ser，或（b）R1为β-D-NAL，R6为D-His或4-胍-D-Phe 。 NαMe-Leu可以任选地被Leu取代。

65. 发明授权

US4569927A GnRH Antagonists IV 失效
标题翻译： GnRH拮抗剂IV
公开(公告)号：US4569927A
公开(公告)日：1986-02-11
申请号：US612072
申请日：1984-05-21
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： A61K38/00 , C07K7/23 , A61K37/02
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 prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. The peptides have the structure:X-R.sub.1 -(W)D-Phe-R.sub.3 -R.sub.4 -R.sub.5 -R.sub.6 -R.sub.7 -Arg-Pro-R.sub.10wherein X is hydrogen or an acyl group having 7 or less carbon atoms; R.sub.1 is dehydro-Pro, D-pGlu, D-Phe, D-Trp of .beta.-D-NAL; W is F, Cl, Cl.sub.2 Br, NO.sub.2 or C.sup..alpha. Me-Cl; R.sub.3 is (N.sup.in For)D-Trp or D-Trp which is substituted in the 5- or 6-position with NO.sub.2, NH.sub.2, OCH.sub.3, F, Cl, Br or CH.sub.3 ; R.sub.4 is Ser, Orn, AAL or aBu; R.sub.5 is Tyr, Arg, (3F)Phe, (2F)Phe, (3I)Tyr, (3CH.sub.3)Phe, (2CH.sub.3)Phe, (3Cl)Phe or (2Cl)Phe; R.sub.6 is (4NH.sub.2)D-Phe, D-Lys, D-Orn, D-Har, D-His, (4gua)D-Phe, D-Tyr, a D-isomer of a lipophilic amino or D-Arg; R.sub.7 is Leu, NML, Nle or Nva; and R.sub.10 is Gly-NH.sub.2, D-Ala-NH.sub.2 or NH-Y, with Y being lower alkyl, cycloalkyl, fluoro lower alkyl or ##STR1## where Q is H or lower alkyl, provided however that when R.sub.5 is Arg, R.sub.6 is D-Tyr.
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。肽具有以下结构：X-R1-（W）D-Phe-R3-R4-R5-R6-R7-Arg-Pro-R10，其中X是氢或具有7个或更少碳原子的酰基; R1是β-D-NAL的脱氢-Pro，D-pGlu，D-Phe，D-Trp; W是F，Cl，Cl 2 Br，NO 2或CαMe-Cl; R3为（NO2，NH2，OCH3，F，Cl，Br或CH3）在5-或6-位被取代的（NinFor）D-Trp或D-Trp; R4是Ser，Orn，AAL或aBu; R5是Tyr，Arg，（3F）Phe，（2F）Phe，（3I）Tyr，（3CH3）Phe，（2CH3）Phe，（3Cl）Phe或（2Cl）Phe; R6是（4NH2）D-Phe，D-Lys，D-Orn，D-Har，D-His，（4gua）D-Phe，D-Tyr，亲脂性氨基或D-Arg的D-异构体; R7是Leu，NML，Nle或Nva; 并且R 10是Gly-NH 2，D-Ala-NH 2或NH-Y，其中Y是低级烷基，环烷基，氟低级烷基或者其中Q是H或低级烷基，或者如果R5是Arg，则R6是 D-Tyr

66. 发明授权

US4518586A GRF Analogs III 失效
标题翻译： GRF类似物III
公开(公告)号：US4518586A
公开(公告)日：1985-05-21
申请号：US545094
申请日：1983-10-25
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： C12P21/00 , A23K1/16 , A61K38/00 , A61K38/04 , A61K38/18 , A61K38/22 , A61K38/25 , C07K14/00 , C07K14/575 , C07K14/60 , C07K14/61 , C12P21/02 , C07C103/52 , A61K37/02
CPC分类号： C07K14/60 , A23K20/147 , A61K38/00 , Y10S930/12
摘要： Human parcreatic GRF(hpGRF), rat hypothalamic GRF(rGRF) and porcine hypothalamic GRF(pGRF) 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 -Leu-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 -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 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 or D-Ala; 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.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.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 either R.sub.17 or R.sub.23 is D-Leu or R.sub.25 is either D-Glu or D-Asp and that any or all of the residues between R.sub.29 and R.sub.44, inclusive, may be deleted; or a nontoxic salt thereof. 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），大鼠下丘脑GRF（rGRF）和猪下丘脑GRF（pGRF）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-Leu-R15-Gln-R17-R18-Al-Arg-Lys-Leu-R23-R24-R25-Ile-R27-R28-Arg-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或D-Ala; 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; R17是Leu或D-Leu; R18是Tyr或Ser; R23为Leu或D-Leu; R 24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; 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R17或R23是D-Leu或R25是D-Glu或D-Asp，并且R29和R44之间的任何或全部残基可以被缺失; 或其无毒盐。 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-CHOOR，其中R和R'是低级烷基，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。

67. 发明授权

US4393050A Analogs of extended N-terminal somatostatin 失效
标题翻译：延长N末端生长抑素的类似物
公开(公告)号：US4393050A
公开(公告)日：1983-07-12
申请号：US258878
申请日：1981-04-29
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： C07K14/575 , A61K38/00 , A61K38/04 , A61P5/00 , A61P5/02 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S514/866 , Y10S514/926 , Y10S514/927 , Y10S930/16
摘要： Somatostatin-28 has the formula: ##STR1## Analogs have been synthesized that are more potent than somatostatin-28, and these analogs 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. In the analogs, Leu may be substituted in the 8-position in combination with D-Trp in the 22-position and/or Tyr in the 25-position. D-Cys may also be substituted in the 28-position, and D-Ser may be substituted in the 27-position. Certain residues may also be deleted. D-Trp.sup.22 somatostation-28 has surprisingly been found to be insulin-selective when administered in vivo and is useful for the treatment of insulinoma.
摘要翻译：生长抑素-28具有以下分子式：H-Ser-Ala-Asn-Ser-Asn-Pro-Ala-Met-Ala-Pro-Arg-Glu-Arg-Lys- 分散在药学上可接受的液体或固体载体中的这些类似物或其药学上可接受的盐可以以与生长抑素相同的方式施用于哺乳动物。在类似物中，Leu可以在D位的8位上与22位和/或25位的Tyr结合取代。 D-Cys也可以在28位被取代，D-Ser可以在27位被取代。某些残基也可能被删除。 D-Trp22生长激素-28在体内给药时已被惊人地发现是胰岛素选择性的，并且可用于治疗胰岛素瘤。

68. 发明授权

US4382922A Peptides affecting gonadal function 失效
标题翻译：影响性腺功能的肽
公开(公告)号：US4382922A
公开(公告)日：1983-05-10
申请号：US353237
申请日：1982-03-01
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 , C07K7/16 , C07K7/23 , A61K37/00 , C07C103/52
CPC分类号： C07K7/23 , C07K7/16 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： LRF analogs having a modified D-Phe residue in the 6-position act as superagonists exhibiting potencies many times more than that of LRF. The peptides or their nontoxic salts can be administered by intravenous, subcutaneous, sublingual, oral, intravaginal, intranasal or rectal routes. The peptides can be used to regulate fertility in male and female mammals, including human beings.The peptides are represented by the following formula:p-Glu-His-Trp-Ser-Ty-R.sub.1 -Leu-Arg-Pro-NH-CH.sub.2 -CH.sub.3wherein R.sub.1 is selected from the group consisting of methyl-D-Phe, nitro-D-Phe, and methyoxy-D-Phe.
摘要翻译：在6位具有修饰的D-Phe残基的LRF类似物作为表现出比LRF多很多倍的潜能的超级拮抗剂。肽或其无毒盐可以通过静脉内，皮下，舌下，口服，阴道内，鼻内或直肠途径施用。这些肽可用于调节男性和女性哺乳动物（包括人类）的生育力。肽由下式表示：p-Glu-His-Trp-Ser-Ty-R1-Leu-Arg-Pro-NH-CH2-CH3，其中R1选自甲基-D-Phe，硝基 -D-Phe和甲氧基-D-Phe。

69. 再颁专利

USRE30548E Peptides which effect release of hormones 失效
标题翻译：影响激素释放的肽
公开(公告)号：USRE30548E
公开(公告)日：1981-03-17
申请号：US071559
申请日：1979-08-31
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 , C07K14/655
CPC分类号： C07K14/6555 , A61K38/00
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. .Iadd.

70. 发明授权

US4218439A Peptide which inhibits gonadal function 失效
标题翻译：抑制性腺功能的肽
公开(公告)号：US4218439A
公开(公告)日：1980-08-19
申请号：US917781
申请日：1978-06-26
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： A method for preventing reproduction by administering to male mammals a peptide which inhibits the secretion of gonadotropins by the pituitary gland and inhibits the release of steroids by the gonads. The peptide has the structure:p--Glu--His--Trp--Ser--Tyr--D--Trp--Leu--Arg--Pro--NH--CH.sub.2 --CH.sub.3.
摘要翻译：一种通过向雄性哺乳动物施用抑制垂体分泌促性腺激素并抑制由性腺释放类固醇的肽来预防繁殖的方法。肽具有以下结构：p-Glu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-NH-CH2-CH3。

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