Non-aqueous injectable formulations for extended release of somatotropin
    2.
    发明授权
    Non-aqueous injectable formulations for extended release of somatotropin 有权
    用于延长生长激素释放的非水性注射用制剂

    公开(公告)号:US07048938B2

    公开(公告)日:2006-05-23

    申请号:US10793232

    申请日:2004-03-04

    Abstract: The present invention provides compositions which allow for the extended release and enhanced bioavailability of biologically-active polypeptides following parenteral delivery to an animal. More particularly, it concerns compositions comprising biologically-active somatotropin formulated for extended release, methods of preparing these compositions, and methods of using the same. These compositions comprise somatotropin, a bioavailability-enhancing constituent (BEC), and a substantially non-aqueous, hydrophobic excipient. The BEC may comprise (i) amino acids or amino acid derivatives, such as histidine-HCl; (ii) hydroxamate derivatives, such as histidine hydroxamate or suberohydroxamic acid; (iii) non-reducing carbohydrates, such as trehalose or trehalose octaacetate; (iv) oxo-acid salts, such as a mixture of monobasic and dibasic sodium phosphate; or (v) a mixture of two or more compounds from within the foregoing classes (i)–(iv).

    Abstract translation: 本发明提供了允许在肠胃外输送到动物后的生物活性多肽的延长释放和增强的生物利用度的组合物。 更具体地,涉及包含用于延长释放的生物活性生长激素配制剂,制备这些组合物的方法和使用该组合物的方法的组合物。 这些组合物包含生长激素,生物利用度增加成分(BEC)和基本上非水性的疏水性赋形剂。 BEC可以包含(i)氨基酸或氨基酸衍生物,例如组氨酸-HCl; (ii)异羟肟酸衍生物,例如羟肟酸组氨酸或苏泊酸肟酸; (iii)非还原性碳水化合物,例如海藻糖或海藻糖八乙酸酯; (iv)含氧酸盐,例如一元和二元磷酸钠的混合物; 或(v)来自上述(i) - (iv)类的两种或更多种化合物的混合物。

    Antibiotic peptides
    5.
    发明授权
    Antibiotic peptides 失效
    抗生素肽

    公开(公告)号:US5889148A

    公开(公告)日:1999-03-30

    申请号:US700449

    申请日:1996-08-27

    CPC classification number: C07K14/43563 A61K38/00

    Abstract: The present invention relates to novel antibiotic peptides which possess antibacterial and/or antifungal activities causing no cytotoxicity, and to antibacterial and/or antifungal agents containing said peptides as active ingredients. In accordance with the present invention, it has been discovered that a number of chemically-synthesized peptides which are derived from Tenecin, show superior antibacterial and/or antifungal activities, while causing no untoward effects, and they can be applied for the development of antibacterial and/or antifungal agents.

    Abstract translation: PCT No.PCT / KR96 / 00034 Sec。 371日期:1996年8月27日 102(e)日期1996年8月27日PCT 1996年3月11日PCT公布。 出版物WO97 / 02286 日期1997年1月23日本发明涉及具有不引起细胞毒性的抗细菌和/或抗真菌活性的新型抗生素肽以及含有所述肽作为活性成分的抗细菌剂和/或抗真菌剂。 根据本发明,已经发现,从Tenecin衍生的多种化学合成的肽显示出优异的抗菌和/或抗真菌活性,同时不会产生不利影响,并且它们可用于开发抗菌剂 和/或抗真菌剂。

    Linear therapeutic peptides
    6.
    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

    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。

    Substrate assisted catalysis
    10.
    发明授权
    Substrate assisted catalysis 失效
    底物辅助催化

    公开(公告)号:US5371190A

    公开(公告)日:1994-12-06

    申请号:US90902

    申请日:1993-07-12

    Abstract: Novel enzyme mutants are disclosed which are derived from a precursor enzyme by replacing or modifying at least one catalytic functional group of an amino acid residue in a precursor enzyme. Such mutant enzymes have a catalytic preference for substrates which provide the replaced or modified catalytic group or its equivalent such that the substrate together with the enzyme mutant assists in its own catalysis.

    Abstract translation: 公开了通过置换或修饰前体酶中氨基酸残基的至少一个催化官能团而衍生自前体酶的新型酶突变体。 这样的突变酶对提供替代或修饰的催化基团或其等同物的底物具有催化倾向,使得底物与酶突变体一起有助于其自身的催化。

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