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    Octapeptide bombesin analogs
    5.
    发明授权
    Octapeptide bombesin analogs 失效
    八肽铃蟾肽类似物

    公开(公告)号：US06307017B1

    公开(公告)日：2001-10-23

    申请号：US09260846

    申请日：1999-03-02

    Applicant: David H. Coy ,  Jacques-Pierre Moreau ,  Sun Hyuk Kim

    Inventor： David H. Coy ,  Jacques-Pierre Moreau ,  Sun Hyuk Kim

    IPC: A61K3800

    CPC classification number: C07K7/086 ,  A61K38/00 ,  C07K7/02 ,  C07K7/18 ,  C07K14/57572 ,  C07K14/685

    Abstract: A linear (i.e., non-cyclic) analog of biologically active amphibian bombesin, mammalian gastrin-releasing peptide (GRP), or mammalian growth hormone releasing factor (GRF), having an active site and a binding site responsible for the binding of the peptide to a receptor on a target cell. Cleavage of a peptide bond in the active site of naturally occurring bombesin, GRP, or GRF is unnecessary for in vivo biological activity. The analog has one of the following modifications: (a) a deletion of an amino acid residue within the active site and a modification of an amino acid residue outside of the active site, (b) a replacement of two amino acid residues within the active site with a synthetic amino acid, a &bgr;-amino acid, or a &ggr;-amino acid residue, or (c) a non-peptide bond instead of a peptide bond between an amino acid residue of the active site and an adjacent amino acid residue.

    Abstract translation: 具有活性位点和负责肽结合的结合位点的生物活性水陆两栖铃蟾肽，哺乳动物胃泌素释放肽（GRP）或哺乳动物生长激素释放因子（GRF）的线性（即非循环）类似物 到目标细胞上的受体。 在天然存在的铃蟾肽，GRP或GRF的活性位点中肽键的切割对于体内生物活性是不必要的。 类似物具有以下修饰之一：（a）活性位点内的氨基酸残基的缺失和活性位点之外的氨基酸残基的修饰，（b）在活性位点内置换两个氨基酸残基 具有合成氨基酸，β-氨基酸或γ-氨基酸残基的位点，或（c）非肽键代替活性位点的氨基酸残基与相邻氨基酸残基之间的肽键 。

    Linear therapeutic peptides
    7.
    发明授权
    Linear therapeutic peptides 失效
    线性治疗肽

    公开(公告)号：US5767236A

    公开(公告)日：1998-06-16

    申请号：US387634

    申请日：1995-02-13

    Applicant: Sun Hyuk Kim ,  Jacques-Pierre Moreau

    Inventor： Sun Hyuk Kim ,  Jacques-Pierre Moreau

    IPC: A61K38/00 ,  C07K7/08 ,  C07K5/00 ,  C07K7/00 ,  C07K15/00

    CPC classification number: C07K7/086 ,  A61K38/00

    Abstract: The invention features linear therapeutic peptides of the following formula: ##STR1## in which A.sup.1 is a D-.alpha.-aromatic amino acid or a D-.alpha.-tethered amino acid; A.sup.2 is Gln, His, 1-methyl-His, or 3-methyl-His; A.sup.3 is the D- or L-isomer selected from Nal, Trp, Phe, and p-X-Phe, where X is F, Cl, Br, NO.sub.2, OH or CH.sub.3 ; A.sup.4 is Ala, Val, Leu, Ile, Nle, or .alpha.-aminobutyric acid; A.sup.5 is Val, Ala, Leu, Ile, Nle, Thr, or .alpha.-aminobutyric acid; A.sup.6 is Gly, Sar, .beta.-Ala, or the D-isomer selected from Ala, N-methyl-Ala, Trp, and Nal; A.sup.7 is His, 1-methyl-His, 3-methyl-His, Lys, or .epsilon.-alkyl-Lys; A.sup.8 is Leu, Ile, Val, Nle, .alpha.-aminobutyric acid, Trp, Pro, Nal, Chx-Ala, Phe, or p-X-Phe, where X is F, Cl, Br, NO.sub.2, OH or CH.sub.3 ; A.sup.9 is Met, Met-oxide, Leu, Ile, Nle, .alpha.-aminobutyric acid, or Cys; each R.sub.1 and R.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, or COE.sub.1, where E.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkynyl, phenyl, 3,4-dihydroxyphenylalkyl, naphthyl, or C.sub.7-10 phenylalkyl; provided that when either R.sub.1 or R.sub.2 is COE.sub.1, the other must be H; and R.sub.3 is OH, NH.sub.2, C.sub.1-12 alkoxy, C.sub.7-10 phenylalkoxy, C.sub.11-20 naphthylalkoxy, C.sub.1-12 alkylamino, C.sub.7-10 phenylalkylamino, C.sub.11-20 naphthylalkylamino; or a pharmaceutically acceptable salt of such peptides.

    Abstract translation: 本发明的特征在于线性治疗肽，其具有以下结构式：其中A1是D-α-芳香族氨基酸或D-α-被束缚氨基酸的 A2是Gln，His，1-甲基-He或3-甲基-He; A3是选自Nal，Trp，Phe和p-X-Phe的D-或L-异构体，其中X是F，Cl，Br，NO 2，OH或CH 3; A4是Ala，Val，Leu，Ile，Nle或α-氨基丁酸; A5是Val，Ala，Leu，Ile，Nle，Thr或α-氨基丁酸; A6是Gly，Sar，β-Ala或选自Ala，N-甲基-Ala，Trp和Nal的D-异构体; A7是His，1-甲基-He，3-甲基-His，Lys或ε-烷基-Ilu; A8是Leu，Ile，Val，Nle，α-氨基丁酸，Trp，Pro，Nal，Chx-Ala，Phe或p-X-Phe，其中X是F，Cl，Br，NO 2，OH或CH 3; A9是Met，Met-氧化物，Leu，Ile，Nle，α-氨基丁酸或Cys; 每个R1和R2独立地是H，C1-12烷基，C7-10苯基烷基或COE1，其中E1是C1-20烷基，C3-20烯基，C3-20炔基，苯基，3,4-二羟基苯基烷基，萘基 或C7-10苯基烷基; 条件是当R1或R2是COE1时，另一个必须是H; 并且R 3是OH，NH 2，C 1-12烷氧基，C 7-10苯基烷氧基，C 11-20萘基烷氧基，C 1-12烷基氨基，C 7-10苯基烷基氨基，C 11-20萘基烷基氨基; 或这些肽的药学上可接受的盐。

    Ionic molecular conjugates of biodegradable polyesters and bioactive polypeptides
    9.
    发明授权
    Ionic molecular conjugates of biodegradable polyesters and bioactive polypeptides 失效
    生物降解聚酯和生物活性多肽的离子分子共轭物

    公开(公告)号：US5672659A

    公开(公告)日：1997-09-30

    申请号：US464735

    申请日：1995-06-29

    Applicant: Shalaby W. Shalaby ,  Steven A. Jackson ,  Jacques-Pierre Moreau

    Inventor： Shalaby W. Shalaby ,  Steven A. Jackson ,  Jacques-Pierre Moreau

    IPC: A61K9/52 ,  A61K38/00 ,  A61K47/48 ,  C07K7/23 ,  A61K9/16 ,  A61K37/02

    CPC classification number: A61K47/482 ,  A61K47/48284 ,  C07K7/23 ,  A61K38/00 ,  Y10S514/80 ,  Y10S514/806 ,  Y10S514/807 ,  Y10S514/808 ,  Y10S514/809 ,  Y10S514/963

    Abstract: A composition including a polyester containing one or more free COOH groups ionically conjugated with a bioactive polypeptide comprising at least one effective ionogenic amine, wherein the polyester contains a member selected from the group of L-lactic acid, D-lactic acid, DL-lactic acid, .epsilon.-caprolactone, p-dioxanone, .epsilon.-caprolic acid, alkylene oxalate, cycloalkylene oxalate, alkylene succinate, .beta.-hydroxybutyrate, substituted or unsubstituted trimethylene carbonate, 1,5-dioxopan-2-one, 1,4-dioxepan-2-one, glycolide, glycolic acid, L-lactide, D-lactide, DL-lactide, meso-lactide, and any optically active isomers, racemates or copolymers thereof, and at least 50%, by weight, of the polypeptide present in the composition is ionically conjugated to said polyester.

    Abstract translation: PCT No.PCT / US94 / 00148 Sec。 371日期：1995年6月29日 102（e）日期1995年6月29日PCT 1994年1月5日PCT PCT。 出版物WO94 / 15587 日期1994年7月21日包含含有一种或多种游离COOH基团的组合物的组合物，所述游离COOH基团与包含至少一种有效的离子型胺的生物活性多肽离子地缀合，其中所述聚酯包含选自L-乳酸，D-乳酸 酸，DL-乳酸，ε-己内酯，对二恶烷酮，ε-己内酯，草酸亚烷基酯，草酸亚环烷基酯，琥珀酸亚烷基酯，β-羟基丁酸酯，取代或未取代的三亚甲基碳酸亚乙酯，1,5-二氧杂戊-2-酮，1 ，4-二氧杂环庚烷-2-酮，乙交酯，乙醇酸，L-丙交酯，D-丙交酯，DL-丙交酯，内消旋丙交酯及其任何光学活性异构体，外消旋体或其共聚物，和至少50重量％ 存在于组合物中的多肽与所述聚酯离子共轭。

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