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1. 发明授权

KR850001159B1 펩타이드의 제조방법 失效
公开(公告)号：KR850001159B1
公开(公告)日：1985-08-16
申请号：KR810001129
申请日：1981-04-04
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： RIVIER CATHERINE LAURE , RIVIER JEAN EDOUARD FREDERIC , VALE JR WYLIE WALKER
IPC分类号： A61K38/04 , A61K38/00 , A61P13/02 , A61P15/00 , C07K7/16 , C07K7/23 , C07K14/00 , C07K14/575 , C07K7/20

2. 发明公开

EP0131007A4 GnRH AGONISTS. 失效
标题翻译： GnRH激动剂。
公开(公告)号：EP0131007A4
公开(公告)日：1987-02-03
申请号：EP84900248
申请日：1983-12-05
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： VALE JR WYLIE WALKER , RIVIER JEAN EDOUARD FREDERIC
IPC分类号： C07K7/06 , C07K7/23 , C07K14/575
CPC分类号： C07K7/23 , Y10S514/80 , Y10S930/13

4. 发明专利

DK165749C 未知
公开(公告)号：DK165749C
公开(公告)日：1993-06-14
申请号：DK433684
申请日：1984-09-11
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： RIVIER JEAN EDOUARD FREDERIC , VALE JR WYLIE WALKER
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 , C07K7/10
摘要： Human pancreatic 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 contain the sequence: R1-R2-R3-Ala-Ile-Phe-Thr-R8-Ser-R10- Arg-R12-R13- Leu-R15- Gln-R17-R18- Ala-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 wherein R1 is a Tyr, D-Tyr, Met, Phe, D-Phe, pCl-Phe, Leu, His or D-His, which has either a C alpha Me or N alpha Me substitution or is unsubstituted; R2 is Ala or D-Ala; R3 is Asp or D-Asp; R8 is Ser, Asn, D-Ser or D-Asn; R10 is Tyr or D-Tyr; R12 is Arg or Lys; R13 is Ile or Val; R15 is Gly or D-Ala; R17 is Leu or D-Leu; R18 is Tyr or Ser; R23 is Leu or D-Leu; R24 is His or Gln; R25 is Glu, Asp, D-Glu or D-Asp; R27 is Met, D-Met, Ala, Nle, Ile, Leu, Nva or Val; R28 is Asn or Ser; R34 is Arg or Ser; R38 is Gln or Arg; R39 is Arg or Gly; R40 is Ser or Ala; R42 is Phe, Ala or Val; R43 is Asn or Arg; R44 is a natural amino acid; provided however that either (a) R1 has a C alpha Me or an N alpha Me substitution or (b) R17 and/or R23 is D-Leu or (c) R25 is either D-Glu or D-Asp and provided also that any or all of the residues between R29 and R44, inclusive, may be deleted; or a nontoxic salt thereof. The C-terminus is preferably amidated. 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.

5. 发明专利

FI923863A0 未知
公开(公告)号：FI923863A0
公开(公告)日：1992-08-28
申请号：FI923863
申请日：1992-08-28
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： RIVIER JEAN EDOUARD FREDERIC , VALE JR WYLIE WALKER
IPC分类号： A61K38/00 , A61K38/35 , A61K38/04 , A61P9/12 , C07K14/575 , C07K14/655 , A61K
摘要： Analogs of CRF, which are based upon rCRF, oCRF, sauvagine and alpha-helical CRF, are disclosed that can be administered to achieve a substantial elevation of ACTH, beta -endorphin, beta -lipotropin, other products of the pro-opiomelanocortin gene and corticosterone levels and/or an increase in blood pressure over an extended period of time. One analog which has been found to be particularly potent is: H-D-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu- Glu-Nle-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn-Arg-Lys-CM L-Nle-Glu-Ile-Ile-NH2. In the analogs of the native 41-residue polypeptides, one or more of the first six N-terminal residues may be deleted and/or the N-terminal alpha-amino group may be acylated by an acylating agent containing up to 7 carbon atoms. A number of other substitutions may also be made throughout the chain. These analogs or pharmaceutically or veterinarily acceptable salts thereof, dispersed in a pharmaceutically or veterinarily acceptable liquid or solid carrier, can be administered to mammals, including humans. These analogs may also be used as stimulants to elevate mood and improve memory and learning, as well as diagnostically.

6. 发明专利

NO168043B 未知
公开(公告)号：NO168043B
公开(公告)日：1991-09-30
申请号：NO851947
申请日：1985-05-15
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： VALE JR WYLIE WALKER , RIVIER JEAN EDOUARD FREDERIC
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 , G01N33/68 , C07K7/10
摘要： Human GRF(hGRF), rat GRF(rGRF), porcine GRF(pGRF) and bovine GRF(bGRF) have been earlier characterized and synthetized. 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: R1-R2-R3-Ala-Ile-Phe-Thr-R8-Ser-R10-Arg-R12-R13-R14-R15-Gln-R17-R18-Al a-Arg-Lys-Le u-R23-R24-R25-Ile-R27-R28-R29-Gln-Gln-Gly-Glu-R34-Asn-Gln-Glu-R38-R39- R40-Arg-R42- R43-R44 wherein R1 is Tyr, D-Tyr, Met, Phe, D-Phe, pCl-Phe, Lou, His or D-His having either a C Me or N Me substitution or being unsubstituted; R2 is Ala, D-Ala or D-NMA; R3 is Asp or D-Asp; R8 is Ser, Asn, D-Ser or D-Asn; R10 is Tyr or D-Tyr; R12 is Arg or Lys; R13 is Ile or Val; R14 is Leu or D-Leu; R15 is Gly or D-Ala; R17 is Leu or D-Leu; R18 is Tyr or Ser; R23 is Leu or D-Leu; R24 is His or Gln; R25 is Glu, Asp, D-Glu or D-Asp; R27 is Met, D-Met, Ala, Nle, Ile, Leu, Nva or Val; R28 is Asn or Ser; R29 is Arg or D-Arg; R34 is Arg or Ser; R34 is Gln or Arg; R39 is Arg or Gly; R40 is Ser or Ala; R42 is Phe, Ala or Val; R43 is Asn or Arg; R44 is a natural amino acid; provided however that any or all of the residues between R28 and R44, inclusive, may be deleted and provided also that R2 is D-NMA and/or R14 is D-Leu and/or R29 in is D-Arg. Those peptides as well as their nontoxic salts may also be used diagnostically.

7. 发明专利

FI906240A0 未知
公开(公告)号：FI906240A0
公开(公告)日：1990-12-18
申请号：FI906240
申请日：1990-12-18
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： RIVIER JEAN EDOUARD FREDERIC , VALE JR WYLIE WALKER , RIVIER CATHERINE LAURE
IPC分类号： A61K38/04 , A61K38/00 , A61P5/00 , C07K14/575 , C07K14/60 , C07K
摘要： The invention provides synthetic peptides which are extremely potent in stimulating the release of pituitary GH in animals, including humans and also resist enzymatic degradation in the body. The peptides have the sequence: (B)R1-R2-R3-Ala-(Q1)R5-Phe-Thr-R8-Ser(Q2)R10-Arg-R12-(Q3)R13-Leu-R15-G ln-(Q4)Leu-R18-(Q5)Ala-Arg-R21-(Q6)R22-(Q7)Leu-R24-R25-(Q8)R26-(Q9)R27 -R28-Arg-Gln-Gln-Gly-Glu-R34-Asn-Gln-Glu-R38-R39-R40-Arg-R42-R43-R44 wherein R1 is Tyr, D-Tyr, Met, Phe, D-Phe, pCl-Phe, Leu, His or D-His; B is H, CaMe, NaMe, desamino, Ac or For; R2 is Ala, D-Ala, NMA or D-NMA; R3 is Asp or D-Asp; R5 is Ile or Leu; R8 is Ser, Asn, Lys, Arg, Asp or Glu; R10 is Tyr, D-Tyr or Phe; R12 is Arg or Lys; R13 is Ile, Val, Leu or Ala; R15 is Gly or Ala; R18 is Ser or Tyr; R21 is Lys, D-Lys, Arg or D-Arg; R22 is Leu, Ile, Ala or Val; R24 is Gln or His; R25 is Asp or Glu; R26 is Ile or Leu; R27 is Met, D-Met, Ala, Nle, Ile, Leu, Nva or Val; R28 is Asn or Ser; R34 is Ser or Arg; R38 is Arg or Gln; R39 is Gly or Arg; R40 is Ala or Ser; R42 is Phe, Ala or Val; R43 is Asn or Arg; R44 is a natural amino acid; Q1-Q9 are either H or CaMe, provided however that one of Q1-Q9 is CaMe. These peptides may also be used diagnostically, and the C-terminus can be shortened to residue-29.

8. 发明专利

DK45990A 未知
公开(公告)号：DK45990A
公开(公告)日：1990-02-21
申请号：DK45990
申请日：1990-02-21
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： RIVIER JEAN EDOUARD FREDERIC , VALE JR WYLIE WALKER
IPC分类号： A61K38/04 , A61K38/00 , A61P9/12 , C07K14/575 , C07K14/695 , C07K7/38
摘要： Analogs of CRF are disclosed that can be administered to achieve a substantial elevation of ACTH, beta -endorphin, beta -lipotropin, other products of the pro-opiomelanocortin gene and corticosterone levels and/or a lowering of blood pressure over an extended period of time. One analog which has been found to be particularly potent is: H-Ser-Glu-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu- Val-Leu-His-Met-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn-Ar g-Lys-Leu-Met-Glu-Ile-Ile-NH2. In the analogs, one or more of the first five N-terminal residues may be deleted or may be substituted by a peptide up to 10 amino acids long and/or by an acylating agent containing up to 7 carbon atoms. A number of other substitutions may also be made throughout the chain. These analogs or pharmaceutically or veterinarily acceptable salts thereof, dispersed in a pharmaceutically or veterinarily acceptable liquid or solid carrier, can be administered to mammals, including humans. These analogs may also be used as stimulants to elevate mood and improve memory and learning.

9. 发明专利

FI882305A0 未知
公开(公告)号：FI882305A0
公开(公告)日：1988-05-17
申请号：FI882305
申请日：1988-05-17
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： RIVIER JEAN EDOUARD FREDERIC , VALE JR WYLIE WALKER , RIVIER CATHERINE LAURE
IPC分类号： A61K38/04 , A61K38/00 , A61K38/25 , A61P5/00 , A61P15/00 , A61P35/00 , A61P43/00 , C07K14/00 , C07K14/575 , C07K14/60 , C07K14/61 , C07K
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)R1-R2-R3-Ala-Ile-Phe-Thr-R8-Ser-(Q1)R10-Arg-R12-(Q2)R13-Leu-R15-Gln -Leu-R18 (Q3)Ala-Arg-R21-(Q4)R22-Leu-R24-R25-Ile-R27-R28-Arg-Gln-Gln-Gly-Glu-R3 4-Asn-Gln- Glu-R38-R39-R40-Arg-R42-R43-R44 wherein R1 is Tyr, D-Tyr, Met, Phe, D-Phe, pCl-Phe, Leu, His or D-His; B is H, C Me, N Me, desamino, Ac or For; R2 is Ala, D-Ala, NMA or D-NMA; R3 is Asp or D-Asp; R8 is Ser, Asn, Lys, Arg, Asp or Gln; R10 is Tyr, D-Tyr or Phe; R12 is Arg or Lys; R13 is Ile, Val, Leu or Ala; R15 is Gly or Ala; R18 is Ser or Tyr; R21 is Lys, D-LyS, Arg or D-Arg; R22 is Leu, Ile, Ala or Val; R24 is Gln or His; R25 is Asp or Glu; R27 is Met, D-Met, Ala, Nle, Ile, Leu, Nva or Val; R28 is Asn or Ser; R34 is Ser or Arg; R38 is Arg or Gln; R39 is Gly or Arg; R40 is Ala or Ser; R42 is Phe, Ala or Val; R43 is Asn or Arg; R44 is a natural amino acid; Q1-Q4 are either H or C Me, provided however that any or all of the residues between R30 and R44, inclusive, may be deleted, and provided also that at least one of Q1-Q4 is C Me and/or R8 is Lys or Arg and/or R21 is D-Lys or D-Arg. These peptides as well as their nontoxic salts may also be used diagnostically.

10. 发明专利

DK150206C 未知
公开(公告)号：DK150206C
公开(公告)日：1987-07-06
申请号：DK166581
申请日：1981-04-13
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： RIVIER CATHERINE LAURE , RIVIER JEAN EDOUARD FREDERIC , VALE JR WYLIE WALKER
IPC分类号： A61K38/04 , A61K38/00 , A61P13/02 , A61P15/00 , C07K7/16 , C07K7/23 , C07K14/00 , C07K14/575 , C07K7/20
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-R1-R2-R3-Ser-Tyr-R4-R5-Arg-Pro-R6 wherein X is hydrogen or an acyl group having 7 or less carbon atoms; R1 is dehydro Pro, dehydro D-Pro, Thz or D-Thz; R2 is D-Phe, D-His, D-Trp, Trp, CI-D-Phe, dichloro-d-Phe, CF3-D-Phe, F-D-Phe, difluoro-D-Phe, AcNH-D-Phe, NO2-D-Phe, di-nitro-D-Phe, Br-D-Phe, dibromo-D-Phe, CH3S-D-Phe, OCH3-D-Phe or CH3-D-Phe; R3 is D-Trp, Trp, D-Phe or D-His; R4 is Gly or a D-isomer amino acid; R5 is Leu or N Me-Leu; and R6 is Gly-NH2 or NHCH2CH3.

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