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31. 发明专利

AT176904T 未知
公开(公告)号：AT176904T
公开(公告)日：1999-03-15
申请号：AT94919491
申请日：1994-06-13
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： HOEGER CARL A , RIVIER JEAN E F , PORTER JOHN S
IPC分类号： A61K38/04 , A61K38/00 , C07C277/08 , C07C279/18 , C07C279/24 , C07C279/28 , C07C313/30 , C07D249/14 , C07K1/00 , C07K7/02 , C07K7/06 , C07K7/23 , C07C227/16 , C07C229/36
摘要： Methods of making unnatural amino acids are provided which unnatural amino acids can be incorporated into peptides which either inhibit or promote the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. These unnatural amino acids are useful in the synthesis of peptides and have the formula (a): where W is (CH2)n or n is an integer from 1 to 6; j=1, 2 or 3, and preferably, Y is N-CN, X is NH and R2 is alkyl, modified alkyl, alkenyl, alkynyl, aryl or methyl pyridyl. Disclosed are peptides that are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions.

32. 发明专利

PH31215A Methods of making amino acids useful in preparing GnRH analogs. 未知
公开(公告)号：PH31215A
公开(公告)日：1998-05-05
申请号：PH48477
申请日：1994-06-17
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： HOEGER CARL A , PORTER JOHN S , RIVIER JEAN E F
IPC分类号： A61K38/00 , A61K38/04 , C07C277/08 , C07C279/18 , C07C279/24 , C07C279/28 , C07C313/30 , C07D249/14 , C07K1/00 , C07K7/02 , C07K7/06 , C07K7/23
摘要： Methods of making unnatural amino acids are provided which unnatural amino acids can be incorporated into peptides which either inhibit or promote the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. These unnatural amino acids are useful in the synthesis of peptides and have the formula (a): where W is (CH2)n or n is an integer from 1 to 6; j=1, 2 or 3, and preferably, Y is N-CN, X is NH and R2 is alkyl, modified alkyl, alkenyl, alkynyl, aryl or methyl pyridyl. Disclosed are peptides that are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions.

33. 发明专利

CA2223792A1 UROCORTIN PEPTIDES 未知
公开(公告)号：CA2223792A1
公开(公告)日：1997-01-03
申请号：CA2223792
申请日：1996-06-12
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： LEWIS KATHY A , DONALDSON CYNTHIA J , VAUGHAN JOAN , RIVIER JEAN E F , PERRIN MARILYN H , SAWCHENKO PAUL , VALE WYLIE W JR
IPC分类号： G01N33/50 , A61K38/00 , A61K38/22 , A61P3/00 , A61P9/02 , A61P9/10 , A61P9/12 , A61P15/04 , A61P25/22 , A61P25/28 , A61P29/00 , A61P37/02 , A61P43/00 , C07K14/575 , C07K16/26 , C12N15/09 , G01N33/15 , G01N33/53 , C12N15/16 , C07H21/00 , C12Q1/68 , G01N33/566 , G01N33/74
摘要： Urocortin (Ucn) is a native mammalian peptide generally related to Urotensin I and Corticotropin Releasing Factor (CRF). Human Ucn has the formula: Asp-Asn-Pro-Ser-Leu-Ser-Ile-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Thr-Leu-Leu-Glu-Leu-Ala-Arg-Thr-Gln-Ser-Gln-Arg-Glu-Arg-Ala-Glu-Gln-Asn-Arg-Ile-Ile-Phe-Asp-Ser-Val-NH2 (SEQ ID NO:15). Rat-derived Ucn is identical but for 2 substitutions, Asp2 for Asn2 and Pro4 for Ser4. Ucn or analogs thereof or pharmaceutically acceptable salts can be administered to humans and other mammals to achieve substantial elevation of ACTH, .beta.-endorphin, .beta.-lipotropin, other products of the pro-opiomelanocortin gene and corticosterone. They can also be used to lower blood pressure over an extended period of time, as stimulants to elevate mood and to improve memory and learning performance, as well as diagnostically. Shortened fragments may be administered to release endogenous CRF and/or Ucn in the brain and peripherally. Ucn antagonists can be used to block the action of Ucn and/or CRF, as can antibodies to Ucn. Labelled Ucn agonists and antagonists can be used in drug screening assays along with CRF receptors; they may also be used diagnostically along with Ucn antibodies.

34. 发明专利

CA2206258A1 AMINO ACIDS FOR MAKING BETIDES AND METHODS OF SCREENING AND MAKING BETIDE LIBRARIES 未知
公开(公告)号：CA2206258A1
公开(公告)日：1996-06-20
申请号：CA2206258
申请日：1995-12-15
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： PORTER JOHN S , RIVIER JEAN E F
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 , C07C233/83 , C07C235/12 , C07C235/52 , C07C237/12 , C07C323/41 , C07D233/32 , C07D233/90 , C07D239/06
摘要： Compounds termed "betides" mimic peptides and contain one or more residues of aminoglycine, C.alpha.-aminoalanine, aminosarcosine or the like wherein the side chain amino group has been acylated and optionally also alkylated. Generally, betides have the formula: XN-X1-X2-X3-Xm-X4-X5-X6-XC, where XN is an acyl or other N-terminal group or a peptide up to about 50 amino acids in length having such a group; XC is OH, NH2 or other C-terminal group or a peptide up to about 50 amino acids in length having such a group; and X1-X6 are each independently a betidamino acid or .alpha.-amino acid or des-X; and Xm is a peptide up to about 50 amino acids or des-X; provided however that at least one of X1-X6 is a betidamino acid residue having formula (I), wherein Ro is H or CH3, R and R2 are H or lower alkyl, and R3 is an acyl group, an isocyanate or isothiocyanate group, a sulfonyl group or the like. To make a betide, an aminoglycine residue is subjected to side chain acylation, and optionally also alkylation, after it is coupled into a peptide intermediate. By synthesizing betides with multiples substituents at one or more positions in an otherwise peptidic chain, efficient screening of betides which mimic peptides having a large number of different natural or unnatural amino acid substituents at a particular position, and optionally both D- and L-isomers thereof, is possible.

35. 发明专利

AU1938795A Gnrh antagonists 未知
公开(公告)号：AU1938795A
公开(公告)日：1995-10-09
申请号：AU1938795
申请日：1995-03-03
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： RIVIER JEAN E F , PORTER JOHN S , HOEGER CARL A , JIANG GUANGCHENG , RIVIER CATHERINE L
IPC分类号： A61K38/00 , A61P13/02 , A61P15/00 , A61P29/00 , A61P31/12 , A61P35/00 , A61P37/04 , C07K7/06 , C07K7/23 , A61K38/09
摘要： Analogs of the decapeptide GnRH which include two significantly modified amino acids at positions 5 and 6 inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads and may be used to treat steroid-dependent tumors. Particularly effective peptides which are soluble in water at physiologic pH and which have a low tendency to gel when administered in vivo have the following formula: Ac- beta -D-2NAL-(4Cl)D-Phe-D-3PAL-Ser-Aph(Q1)(3-amino-1,2,4 triazole)-D-Aph(Q2)(3-amino 1,2,4-triazole)-Leu-Lys (isopropyl)-Pro-D-Ala-NH2, where Q1 and Q2 are amino acids, such as Gly, beta -Ala, Ala, D-Ala, Ser, Aib, Ahx and Gab. Examples of other GnRH antagonists include Ac- beta -D-2NAL-(4Cl)D-Phe-D-3PAL-Ser-Aph(Atz)-D-Aph(Ac)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2, Ac- beta -D-2NAL-(4Cl)D-Phe-D-3PAL-Ser-Aph( beta -Ala)(3-amino-1,2,4 triazole)-D-Aph( beta -Ala)(3-amino-1,2,4 triazole)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2, Ac- beta -D-2NAL-(4Cl)D-Phe-D-3PAL-Ser-Aph(Ac-D-Ser)-D-Aph(Ac-D-Ser)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2, and Ac- beta -D-2NAL-(4Cl)D-Phe-D-3PAL-Ser-Aph(Ac)-D-Aph(Ac)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2.

36. 发明专利

CA2165566A1 CONOTOXINS HAVING ACETYLCHOLIN RECEPTOR BINDING PROPERTIES 未知
公开(公告)号：CA2165566A1
公开(公告)日：1995-01-12
申请号：CA2165566
申请日：1994-06-27
申请人： SALK INST FOR BIOLOGICAL STUDI , UNIV UTAH RES FOUND
发明人： OLIVERA BALDOMERO , RIVIER JEAN E F , CRUZ LOURDES , ABOGADIE FE , HOPKINS CHRIS E , DYKERT JOHN , TORRES JOSEP L
IPC分类号： A61K38/00 , A61K39/00 , A61P21/00 , C07K14/435 , C12N15/12 , C07K7/08 , A61K38/10 , A61K38/17 , G01N33/566
摘要： Substantially pure conotoxins are provided which inhibit synaptic transmissi ons at the neuromuscular junctions and which are useful both in vivo and in assays because they specifically target particular recep tors, such as the acetylcholine receptor, and ion channe ls. The peptides are of such length that they can be made by chemical synthesis. The y also may be made using recombinant DNA techniques, and the DNA encoding such conotoxins having pesticidal properties can be incorpo rated as plant defense genes into plant species of inter est.

37. 发明专利

ZA94896B GnRH antagonists XII 未知
公开(公告)号：ZA94896B
公开(公告)日：1994-10-04
申请号：ZA94896
申请日：1994-02-09
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： RIVIER JEAN E F , RIVIER CATHERINE L
IPC分类号： A61K38/00 , C07K7/23 , C07K , A61K , C07B

38. 发明专利

CA1329762C POTENTIATION OF ERYTHROPOIESIS 未知
公开(公告)号：CA1329762C
公开(公告)日：1994-05-24
申请号：CA582960
申请日：1988-11-14
申请人： SALK INST FOR BIOLOGICAL STUDI , UNIV CALIFORNIA , SCRIPPS CLINIC RES
发明人： YU JOHN C , YU ALICE L , VAUGHAN JOAN , RIVIER JEAN E F , VALE WYLIE W JR
IPC分类号： A61K38/00 , A61K38/04 , A61K38/22 , A61P7/00 , C07K14/435 , C07K14/575 , C12Q1/02 , A61K35/28 , A61K37/38 , A61K37/43
摘要： POTENTIATION OF ERYTHROPOIESIS A method for modulating the rate of erythropoiesis in human hematopoietic progenitor cells. FRP is found to be an efficacious potentiator of, and inhibin a suppressor of, erythropoietin-induced differentiation. FRP and inhibin are shown to be functional antagonists of each other, and thus represent an effective means for modulating erythropoiesis in a number of disease states which are directly caused by or associated with an abnormal rate of erythropoiesis.

39. 发明专利

CA1304193C GRF ANALOGS V 未知
公开(公告)号：CA1304193C
公开(公告)日：1992-06-23
申请号：CA556019
申请日：1988-01-07
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： VAUGHAN JOAN , SPIESS JOACHIM , RIVIER JEAN E F , VALE WYLIE W JR
IPC分类号： A61K38/00 , C07K14/60 , C07K7/10 , A61K37/02
摘要： GRF ANALOGS V The invention provides peptides which are particularly potent in stimulating the release of pituitary GH in fish and amphibians and which have a substantial portion or all of the following sequence: His-Ala-Asp-Gly-R5-Phe-Asn-Lys-Ala-Tyr-Arg-Lys-Ala-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Tyr-Leu-His-Thr-Leu-R27-R28-R29-R30-R31-Gly-R33-R34-R35-R36-R37-R38-R39-R40-R41-R42-R43-R44-Ser wherein R5 is Met, Leu, Val, Nva, Gln, Thr, Ile or Nle; R27 is Met, Leu, Val, Nva, Gln, Thr, Ile or Nle; R28 is Ala, Ser or Asn; R29 is Lys or Arg; R30 is Arg or Gln; R31 is Val or Gln; R33 is Gly or Glu; R34 is Gly, Arg or Ser; R35 is Ser or Asn; R36 is Met, Leu, Val, Nva, Gln, Thr, Ile or Nle; R37 is Ile or Glu; R38 is Glu, Gln or Arg; R39 is Asp, Arg or Gly; R40 is Asp, Ser or Ala; R41 is Asn, Arg or Lys; R42 is Glu, Phe, Ala or Val; R43 is Pro, Asn or Arg; R44 is Leu or Ala. A sequence beginning at the C-terminus and extending part way or all the way to residue R27 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.

40. 发明专利

CA1288195C GNRH ANTAGONISTS IX 未知
公开(公告)号：CA1288195C
公开(公告)日：1991-08-27
申请号：CA508151
申请日：1986-05-01
申请人： SALK INST FOR BIOLOGICAL STUDI
发明人： RIVIER JEAN E F , VARGA JANOS I , HAGLER ARNOLD T , STRUTHERS RICHARD S , PERRIN MARILYN H , RIVIER CATHERINE L , VALE WYLIE W JR
IPC分类号： A61K38/04 , A61K38/00 , A61K38/22 , A61K38/27 , A61P5/00 , C07K7/06 , C07K7/23 , C07K14/00 , C07K14/575 , C07K7/64
摘要： GnRH ANTAGONISTS IX 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 of such GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. These peptides may be used to treat steroid-dependent tumors, such as prostatic and mammary tumors. The peptides are cyclic analogs of the decapeptide GnRH wherein there is a covalent bond between the residue in the 4-position and the residue in the 10-position. Examples of such bonds include the disulfide linkage between Cys residues, an amide linkage between a side chain amino group and a side chain carboxyl group, a dicarba linkage between side-chain alkyl groups, and a carba linkage between a side-chain alkyl group and a side-chain sulfhydryl group. An amide linkage with the 4-position residue having the carboxyl group side chain is preferred, with Asp and daP being most preferred.

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