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    OCTAPEPTIDE ANALOGS OF SOMATOSTATIN HAVING THREONINE AT THE SIXTH POSITION
    5.
    发明授权
    OCTAPEPTIDE ANALOGS OF SOMATOSTATIN HAVING THREONINE AT THE SIXTH POSITION 失效
    生长抑素OKTAPEPTIDANALOGE在位置6苏氨酸

    公开(公告)号：EP0457888B1

    公开(公告)日：1996-07-10

    申请号：EP91901181.7

    申请日：1990-12-04

    申请人： The Administrators of The Tulane Educational Fund

    发明人： COY, David, H. ,  MURPHY, William, A.

    IPC分类号： C07K14/655 ,  A61K38/16

    CPC分类号： C07K14/6555 ,  A61K38/00 ,  Y02A50/471 ,  Y10S930/16 ,  Y10S930/26

    摘要： A compound of the formula: wherein each A1 and A2, independently, is H, C1-12 alkyl, C7-10 phenylalkyl, R1CO (where R1 is C1-20 alkyl, C3-20 alkenyl, C3-20 alkinyl, phenyl, naphthyl, or C7-10 phenylalkyl), or R2OCO (where R2 is C1-10 alkyl or C7-10 phenylalkyl), provided that when one of A1 or A2 is R1CO or R2OCO, the other must be H; each X1 and X2, independently, is H, F, Cl, Br, OH, CH3, or CF3, provided that at least one of X1 and X2 must be H; A3 is Phe or Tyr; and A4 is OH, NH2, or NH-R3 (wherein R3 is a saturated aliphatic C1-8 alkyl); or a pharmaceutically acceptable salt thereof. A therapeutic composition containing the compound of the present invention and a method of using the same are also described.

    INHIBIN AND METHOD OF PURIFYING SAME
    7.
    发明授权
    INHIBIN AND METHOD OF PURIFYING SAME 失效
    抑制素与其清洗。

    公开(公告)号：EP0232326B1

    公开(公告)日：1994-10-05

    申请号：EP86904699.5

    申请日：1986-07-17

    申请人： THE SALK INSTITUTE FOR BIOLOGICAL STUDIES

    发明人： LING, Nicholas, Chai-Kwan ,  YING, Shao-Yao ,  ESCH, Fred, Stephen ,  GUILLEMIN, Roger, Charles, Louis

    IPC分类号： C07K7/06 ,  C07K7/08 ,  C07K7/10 ,  C07K13/00 ,  C07K15/00

    CPC分类号： C07K14/575 ,  A61K38/00 ,  Y10S930/26

    摘要： Two 32,000-dalton proteins with inhibin activity were isolated from porcine follicular fluid using heparin-Sepharose affinity chromatography, followed by gel filtration on Sephacryl S-200 and then four steps of reverse-phase high-performance liquid chromatography. Each isolated molecule is composed of two chains having molecular weights of about 18,000 and about 14,000 daltons, respectively, which are bound together by disulfide bonding. Microsequencing revealed the NH2-terminal portion of the 18K chain of both to be Ser-Thr-Ala-Pro-Leu-Pro-Trp-Pro-Trp-Ser-Pro-Ala-Ala-Leu-Arg-Leu-Leu-Gln-Arg-Pro-Pro-Glu-Glu-Pro-Ala-Val, of one of the 14K chains to be Gly-Leu-Glu-Cys-Asp-Gly-Arg-Thr-Asn-Leu-Cys-Cys-Arg-Gln-Gln-Phe-Phe-Ile-Asp-Phe-Arg-Leu-Ile-Gly-Trp, and of the other 14K chain to be Gly-Leu-Glu-Cys-Asp-Gly-Lys-Val-Asn-Ile-Cys-Cys-Lys-Lys-Gln-Phe-Phe-Val-Ser-Phe-Lys-Asp-Ile-Gly-Trp-Asn-Asp-Trp-Ile-Ile-Ala-Pro. Both proteins have now been completely characterized, each having a first chain 134 residues long linked by disulfide bonding to a second chain 116 or 115 residues long. The first chain is believed to be glycosylated, which accounts for the disparity between the number of residues and the apparent molecular weight of 18K. These 32K proteins specifically inhibit basal secretion of FSH, but not of LH, in a rat anterior pituitary monolayer culture system. The half-maximal effective dose of one is 450 pg/ml and of the other is 900 pg/ml.

    VERFAHREN ZUR GEWINNUNG VON INSULIN-VORLÄUFERN AUS REAKTIONSGEMISCHEN, DIE BEI DER FALTUNG VON INSULIN-VORLÄUFERN AUS DEN ENTSPRECHENDEN S-SULFONATEN ANFALLEN
    10.
    发明授权
    VERFAHREN ZUR GEWINNUNG VON INSULIN-VORLÄUFERN AUS REAKTIONSGEMISCHEN, DIE BEI DER FALTUNG VON INSULIN-VORLÄUFERN AUS DEN ENTSPRECHENDEN S-SULFONATEN ANFALLEN 失效
    通过制备相应的S-磺酸盐制备胰岛素前体的反应混合物中制备胰岛素前体的方法

    公开(公告)号：EP0245267B1

    公开(公告)日：1990-11-28

    申请号：EP86900761.7

    申请日：1986-01-11

    申请人： HOECHST AKTIENGESELLSCHAFT

    发明人： GRAU, Ulrich

    IPC分类号： C07K7/10 ,  C07K7/40

    CPC分类号： C07K14/625 ,  Y10S930/26

    摘要： Process for producing insulin precursors having the formula (I), wherein R is hydrogen or the presequence Pm-Qn-, P is a sequence of natural amino acids wherein m is comprised between 0 and 50, K represents natural basic amino acids and n is an integer comprised between 1 and 4, Y represents -LysB29-ZB30-, wherein Z represents Ala, Thr or Ser, the bridge from A-1 to A-21 is an insulin-A-chain and the bridge from B-1 to B-30 is an insulin-B-chain. X is a bridge linked by the amino group from A-1 to the insulin-A-chain and to the epsilon-amino group of B-29 - case wherein OH is bound to the free bound of ZB30 - or bound by the carboxyl group of B-30 to the insulin-B-chain. Said insulin precursors are prepared from reaction mixtures which result from the preparation of insulin precursors by plaiting S-sulphonates having the formula (II), wherein R, X and Y have the signification given hereabove. Said process is characterized in that the false recombinant products contained in the reaction mixture are precipitated when the mixture is brought to a pH comprised between 4 and 6. The precipitate is then separated by a conventional process and transformed by sulfitolysis into the S-sulphonate having the formula (II), and the latter is again subjected to plaiting.