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51. 发明专利

DD202694A5 未知
公开(公告)号：DD202694A5
公开(公告)日：1983-09-28
申请号：DD23919682
申请日：1982-04-21
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： RIVIER JEAN E F , VALE WYLIE W
IPC分类号： C07K14/575 , A61K38/00 , A61K38/04 , A61P43/00 , C07C231/00 , C07K1/113 , C07K7/06 , C07K7/16 , C07K7/23 , C07C103/52
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 or dehydro D-Pro; R2 is D-Phe, Cl-D-Phe, dichloro-D-Phe, CF3-D-Phe, F-D-Phe, difluoro-D-Phe, AcNH-D-Phe, NO2-D-Phe, dinitro-D-Phe, Br-D-Phe, dibromo-D-Phe, CH3-S-D-Phe, OCH3-D-Phe or CH3-D-Phe; R3 is D-Trp or B-D-NAL; R4 is a D-isomer amino acid and preferably B-D-NAL; R5 is Leu or N Me-Leu; and R6 is Gly-NH2 or NHCH2CH3; provided however that either R3 or R4 is B-D-NAL.

52. 发明专利

CA1110232A PEPTIDE WHICH INHIBITS GONADAL FUNCTION 未知
公开(公告)号：CA1110232A
公开(公告)日：1981-10-06
申请号：CA307047
申请日：1978-07-10
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： RIVIER CATHERINE L , RIVIER JEAN E F , VALE WYLIE W JR
IPC分类号： A61K38/00 , C07K7/23 , C07C103/52
摘要： A method for preventing reproduction by administering to male or female 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:

53. 发明专利

CA1102313A SOMATOSTATIN ANALOGS WITH DISSOCIATED BIOLOGICAL ACTIVITIES 未知
公开(公告)号：CA1102313A
公开(公告)日：1981-06-02
申请号：CA279918
申请日：1977-06-06
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： VALE WYLIE W JR , RIVIER JEAN E F , BROWN MARVIN R
IPC分类号： C07K7/08 , A61K38/00 , A61K38/04 , A61K38/22 , A61K38/28 , A61P5/00 , C07K14/575 , C07K14/655 , C07C103/52
摘要： The present invention relates to peptides having dissociated biological activity in respect to the inhibition of growth hormone, insulin, and glucagon secretion. The peptides are analogs of somatostatin.

54. 发明专利

CA1064912A PHARMACEUTICALLY ACTIVE PEPTIDE AND METHOD OF USE THEREOF 未知
公开(公告)号：CA1064912A
公开(公告)日：1979-10-23
申请号：CA203805
申请日：1974-07-02
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： GUILLEMIN ROGER C L , BRAZEAU PAUL E JR , BURGUS ROGER C , LING NICHOLAS C , RIVIER JEAN E F , VALE WYLIE W JR
IPC分类号： C07K14/575 , A61K38/00 , C07K1/113 , C07K14/655 , C07K17/08 , C07C103/52
摘要： Novel peptides of the formula (I) , and (II) R-Cys-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys-OH, where R is an acylating agent or hydrogen, are prepared by a method comprising the steps of preparing an ester of N.alpha. protected Cys amino acid and a chloromethylated resin, de-protecting said Cys amino acid and stepwise coupling N.alpha. protected amino acids to said Cys to form a resin coupled peptide having the structure R-Cys- Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys-resin where R is an acylating agent or hydrogen. The novel peptides display an inhibitory influence on the growth promoting function of the mammalian pituitary gland.

55. 发明专利

AU2011348220A1 Cyclic CRF antagonist peptides 未知
公开(公告)号：AU2011348220A1
公开(公告)日：2013-07-11
申请号：AU2011348220
申请日：2011-12-22
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： RIVIER JEAN E F
IPC分类号： C07K14/00 , A61K38/22
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.

56. 发明专利

AT319742T 未知
公开(公告)号：AT319742T
公开(公告)日：2006-03-15
申请号：AT95943747
申请日：1995-12-12
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： RIVIER JEAN E F
IPC分类号： G01N33/15 , A61K38/00 , A61K38/04 , A61K45/00 , A61P25/00 , A61P29/00 , A61P35/00 , C07K14/575 , G01N33/50 , G01N33/566 , G01N33/68 , G01N33/74
摘要： Improved CRF antagonist peptides have the formula: (cyclo 30-33)DPheHisLeuLeuArgGluVal LeuGluNleAlaArgAlaGluGlnLeu LeuNleGluIleIleNH2 wherein R30 is Cys or Glu; R33 is Cys, Lys or Orn; provided that when R30 is Cys, R33 is Cys and when R30 is Glu, R33 is Lys or Orn. The N-terminus may be extended by Asp-Leu-Thr. Lys may be substituted for Arg23 and its side chain connected by a lactam bridge to Glu20 to form a dicyclic peptide. Specific CRF antagonists disclosed include (cyclo 30-33) [D-Phe12, Nle21,38, Glu30, Lys33]rCRF(12-41); (cyclo 30-33) [D-Phe12, Nle21,38, Glu30, Orn33]rCRF(12-41), (cyclo 30-33) [D-Phe12, Nle21,38, Cys30,33]rCRF (12-41) and (bicyclo 20-23,30-33) [D-Phe12, Nle21,38, Lys23,33, Glu30]-rCRF(12-41).

57. 发明专利

CA2420184C CONOTOXINS 未知
公开(公告)号：CA2420184C
公开(公告)日：2004-09-21
申请号：CA2420184
申请日：1994-06-27
申请人： UNIV UTAH RES FOUND , SALK INST FOR BIOLOGICAL STUDI
发明人： OLIVERA BALDOMERO M , RIVIER JEAN E F , CRUZ LOURDES J , HOPKINS CHRIS E , DYKERT JOHN , TORRES JOSEP L , ABOGADIE FE
IPC分类号： A61K38/10 , A61K38/17 , A61P25/00 , C07K7/08 , C07K14/435 , G01N33/566
摘要： A substantially pure conotoxin which is highly selective for a specific human receptor, which conotoxin is selected from the group consisting of: Glu-Ser-Glu-Glu-Gly-Gly-Ser-Asn-Ala-Thr-Lys-Lys-Pro- Tyr-Ile-Leu (SEQ ID NO:13) wherein Glu in the 1-position is pGlu and the C-terminus is amidated; Gly-Glu-Xaa-Xaa-Va1-Ala-Lys-Met-Ala-Ala-Xaa-Leu-Ala- Arg-Xaa-Asn-Ile-Ala-Lys-Gly-Cys-Lys-Val-Asn-Cys-Tyr- Pro (SEQ ID NO:12) wherein Xaa is Gla; Ser-Thr-Ser-Cys-Met-Glu-Ala-Gly-Ser-Tyr-Cys-Gly-Ser- Thr-Thr-Arg-Ile-Cys-Cys-Gly-Tyr-Cys-Ala-Tyr-Phe-Gly- Lys-Lys-Cys-Ile-Asp-Tyr-Pro-Ser-Asn (SEQ ID NO:11); Cys-Lys-Thr-Tyr-Ser-Lys-Tyr-Cys-Xaa-Ala-Asp-Ser-Xaa- Cys-Cys-Thr-Xaa-Gln-Cys-Val-Arg-Ser-Tyr-Cys-Thr-Leu- Phe (SEQ ID NO:10) wherein Xaa is Gla and the C-terminus is amidated; His-Xaa-Xaa-Cys-Cys-Leu-Tyr-Gly-Lys-Cys-Arg-Arg-Tyr- Xaa-Gly-Cys-Ser- Ser-Ala-Ser-Cys-Cys-Gln (SEQ ID NO:9) wherein Xaa is 4Hyp; Gly-Cys-Cys-Ser-His-Pro-Ala-Cys-Ser-Gly-Lys-Tyr-Gln- Xaa-Tyr-Cys-Arg- Xaa- Ser (SEQ ID NO:8) wherein Xaa is Gla and the C-terminus is amidated; and Gly-Xaa-Ser-Phe-Cys-Lys-Ala-Asp-Glu-Lys-Xaa-Cys-Glu- Tyr-His-Ala-Asp-Cys-Cys-Asn-Cys-Cys-Leu-Ser-Gly-Ile- Cys-Ala-Xaa-Ser-Thr-Asn-Trp-Ile-Leu-Pro-Gly-Cys-Ser- Thr-Ser-Ser-Phe-Phe-Lys-Ile (SEQ ID NO:7) wherein Xaa is 4Hyp. These conotoxins may be used to prepare medicaments for the treatment of neuromuscular disorders. Some may be used for rapid reversible immobilisation of muscles or for diagnosing myasthenia gravis or Lambert-Eaton myasthenic syndrome.

58. 发明专利

AU4524401A Receptor-selective somatostatin analogs 未知
公开(公告)号：AU4524401A
公开(公告)日：2001-06-25
申请号：AU4524401
申请日：2000-12-13
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： RIVIER JEAN E F , REUBI JEAN CLAUDE
IPC分类号： A61P5/04 , A61P35/00 , C07K7/64 , C07K14/655 , C07K7/00
摘要： Analogs of SRIF which are selective for SSTR3 in contrast to the other cloned SRIF receptors. These analogs are useful in determining the tissue and cellular expression of the receptor SSTR3 and its biological role in the endocrine, exocrine and nervous system, as well as in regulating tumor growth. SRIF analog peptides, such as des-AA1,2,4,5,12,13[NbetaMeD-Agl8(2-naphthoyl) ]-SRIF and counterparts incorporating D-Cys3 and/or Tyr7, inhibit the binding of a universal SRIF radioligand to the cloned human receptor SSTR3, but they do not bind with significant affinity to human SSTR1, SSTR2, SSTR4 or SSTR5. By incorporating an iodinated tyrosine in position-2 or in position-11 in these SSTR3-selective SRIF analogs, a labeled compound useful in drug-screening methods is provided. Because the N-terminus accommodates bulky moieties without loss of selectivity, a cytotoxin or a complexing agent to accept a radioactive nuclide may be present at the N-terminus. Alternatively, the binding affinity may be improved without detriment to the selectivity by adding a carbamoyl moiety at the N-terminus and/or replacing Phe11 with Aph or substituted Aph.

59. 发明专利

CA1340964C CRF ANALOGS 未知
公开(公告)号：CA1340964C
公开(公告)日：2000-04-18
申请号：CA611353
申请日：1989-09-14
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： VALE WYLIE W JR , RIVIER JEAN E F
IPC分类号： A61K38/04 , A61K38/00 , A61P1/00 , A61P9/12 , A61P25/00 , A61P25/02 , C07K14/575 , C07K14/00 , A61K38/35 , C07K14/695
摘要： Analogs of CRF, which are based upon hCRF, 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-Ser-Gln-Glu-Pro-Pro-Ile-Ser- Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-D-Glu-Met- Thr-Lys-Ala-Asp-Gln-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn-Arg- Lys-Leu-Leu-Asp-Ile-Ala-NH2. In the analogs, 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.

60. 发明专利

AU700904B2 Amino acids for making betides and methods of screening and making betide libraries 未知
公开(公告)号：AU700904B2
公开(公告)日：1999-01-14
申请号：AU4469396
申请日：1995-12-15
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： RIVIER JEAN E F , PORTER JOHN S
IPC分类号： G01N33/48 , A61K38/00 , C07C233/47 , C07C233/56 , C07C235/42 , C07C271/22 , C07C279/14 , C07K1/04 , C07K1/10 , C07K7/06 , C07K7/23 , C07K14/575 , C07K14/655 , G01N33/68

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