Nanoparticles and microparticles of non-linear hydrophilic-hydrophobic
multiblock copolymers
    3.
    发明授权
    Nanoparticles and microparticles of non-linear hydrophilic-hydrophobic multiblock copolymers 失效
    非线性亲水疏水多嵌段共聚物的纳米颗粒和微粒

    公开(公告)号:US6007845A

    公开(公告)日:1999-12-28

    申请号:US582993

    申请日:1996-03-25

    摘要: Particles are provided that are not rapidly cleared from the blood stream by the macrophages of the reticuloendothelial system, and that can be modified to achieve variable release rates or to target specific cells or organs. The particles have a core of a multiblock copolymer formed by covalently linking a multifunctional compound with one or more hydrophobic polymers and one or more hydrophilic polymers, and contain a biologically active material. The terminal hydroxyl group of the poly(alkylene glycol) can be used to covalently attach onto the surface of the particles biologically active molecules, including antibodies targeted to specific cells or organs, or molecules affecting the charge, lipophilicity or hydrophilicity of the particle. The surface of the particle can also be modified by attaching biodegradable polymers of the same structure as those forming the core of the particles. The typical size of the particles is between 180 nm and 10,000 nm, preferably between 180 nm and 240 nm, although microparticles can also be formed as described herein. The particles can include magnetic particles or radiopaque materials for diagnostic imaging, biologically active molecules to be delivered to a site, or compounds for targeting the particles. The particles have a prolonged half-life in the blood compared to particles not containing poly(alkylene glycol) moieties on the surface.

    摘要翻译: PCT No.PCT / US94 / 08287 Sec。 371日期1996年1月22日 102(e)日期1996年1月22日PCT提交1994年7月22日PCT公布。 公开号WO95 / 03356 日期1995年2月2日提供了不被网状内皮系统的巨噬细胞迅速从血液中清除的颗粒,并且可以修饰以实现可变释放速率或靶向特定细胞或器官。 颗粒具有通过共价连接多官能化合物与一种或多种疏水性聚合物和一种或多种亲水性聚合物形成的多嵌段共聚物的核心,并含有生物活性材料。 聚(亚烷基二醇)的末端羟基可用于共价附着到颗粒表面上的生物活性分子,包括靶向特定细胞或器官的抗体或影响颗粒的电荷,亲油性或亲水性的分子。 颗粒的表面也可以通过连接与形成颗粒核心的那些相同结构的可生物降解的聚合物来进行改性。 颗粒的典型尺寸在180nm和10,000nm之间,优选在180nm和240nm之间,尽管也可以如本文所述形成微粒。 颗粒可以包括用于诊断成像的磁性颗粒或不透射线的材料,要递送到位点的生物活性分子或用于靶向颗粒的化合物。 与不含表面上的聚(亚烷基二醇)部分的颗粒相比,颗粒在血液中具有延长的半衰期。

    Method for producing a modified peptide
    5.
    发明授权
    Method for producing a modified peptide 有权
    生产修饰肽的方法

    公开(公告)号:US07138489B2

    公开(公告)日:2006-11-21

    申请号:US10500018

    申请日:2003-04-10

    CPC分类号: C07K14/60 C07K14/465

    摘要: The present invention is a method for producing a peptide or a protein in which a side chain contains a modified amino acid residue, which comprises chemically producing a peptide fragment containing an amino acid residue having a modified side chain using an weak acid-cleavable resin, producing a peptide fragment containing no amino acid residue having a modified side chain using a genetic recombination method or/and an enzymatic method, and condensing the resulting two kinds of peptide fragments and, according to the present invention, a peptide or a protein containing modification such as acylation, glycosylation and phosphorylation can be obtained effectively and at high quality.

    摘要翻译: 本发明是一种生产肽或蛋白质的方法,其中侧链含有修饰的氨基酸残基,其包括使用弱酸可裂解树脂化学制备含有具有改性侧链的氨基酸残基的肽片段, 使用遗传重组法或/或酶法产生不含具有修饰侧链的氨基酸残基的肽片段,并将得到的两种肽片段缩合,根据本发明,将肽或含有蛋白质的修饰 可以有效和高质量地获得酰化,糖基化和磷酸化等功能。

    Medicinal compositions for nasal absorption
    6.
    发明申请
    Medicinal compositions for nasal absorption 审中-公开
    用于鼻吸收的药物组合物

    公开(公告)号:US20050014681A1

    公开(公告)日:2005-01-20

    申请号:US10496624

    申请日:2002-11-26

    摘要: A pharmaceutical composition for nasal administration exhibits an improved bioavailability of a biologically active polypeptide, the active ingredient of the pharmaceutical composition. Specifically, the composition is prepared by uniformly dispersing and embedding a biologically active acidic polypeptide having an isoelectric point of 7 or lower on the surfaces of a polyvalent metal compound carrier with the help of an additive capable of dispersing and embedding the polypeptide on the surfaces of the carrier. The polyvalent metal compound carrier is a metal compound with a valent of 2 or higher that is either insoluble or little soluble in water, examples being aluminum compounds, calcium compounds, magnesium compounds, silicone compounds, iron compounds, and zinc compounds.

    摘要翻译: 用于鼻腔给药的药物组合物表现出生物活性多肽(药物组合物的活性成分)的改善的生物利用度。 具体地说,通过在多价金属化合物载体的表面上均匀分散并包埋等电点为7以下的生物活性的酸性多肽,借助于能够将多肽分散并嵌入到 承运人 多价金属化合物载体是不溶于水或几乎不溶于水的价格为2或更高的金属化合物,例如铝化合物,钙化合物,镁化合物,硅氧烷化合物,铁化合物和锌化合物。

    CNP analog peptides and their use
    7.
    发明授权
    CNP analog peptides and their use 失效
    CNP类似物及其用途

    公开(公告)号:US5434133A

    公开(公告)日:1995-07-18

    申请号:US828450

    申请日:1992-01-31

    CPC分类号: C07K14/58 A61K38/00 Y02P20/55

    摘要: Novel peptides represented by the general formula: ##STR1## and physiologically acceptable acid addition salts thereof; where (A) represents H-, H-Gly, H-Lys-Gly, H-Ser-Lys-Gly, H-Leu-Ser-Lys-Gly, H-Gly-Leu-Ser-Lys-Gly, H-ser, H-Ser-Ser, H-Arg-Ser-Ser, H-Arg-Arg-Ser-Ser, H-Leu-Arg-Arg-Ser-Ser, H-Ser-Leu-Arg-Arg-Ser-Ser;(B) represents H-Cys or Pmp;(C) represents Phe-, pCl-Phe, pF-Phe, pNO.sub.2 -Phe or Cha;(D) represents Ile, Val, Aib, tLeu, Gly or Leu;(E) represents Lys or Arg;(F) represents Ile, Leu or Met;(G) represents Ser or Ala;(H) represents Met or Gln;(I) represents --OH, -Asn-OH, -Asn-Ser-OH, -Asn-Ser-Phe-OH, -Asn-Ser-Phe-Arg-OH or -Asn-Ser-Phe-Arg-Tyr-OH; and the symbol " . . . " represents a disulfide bond;provided that 1) .alpha.-hANP, 2) .alpha.-hANP (7-28) and 3) CNP-22 are excluded from the scope of that general formula.Also disclosed are agents for suppressing the growth of vascular smooth muscle cells that contains those peptides as effective ingredients.

    摘要翻译: 由通式表示的新肽:其加成盐; 其中(A)表示H,H-Gly,H-Lys-Gly,H-Ser-Lys-Gly,H-Leu-Ser-Lys-Gly,H-Gly-Leu-Ser-Lys-Gly, Ser,H-Ser-Ser,H-Arg-Ser-Ser,H-Arg-Arg-Ser-Ser,H-Leu-Arg-Arg-Ser-Ser,H-Ser-Leu-Arg-Arg- 塞尔 (B)代表H-Cys或Pmp; (C)表示Phe-,pCl-Phe,pF-Phe,pNO2-Phe或Cha; (D)代表Ile,Val,Aib,tLeu,Gly或Leu; (E)表示Lys或Arg; (F)表示Ile,Leu或Met; (G)表示Ser或Ala; (H)表示Met或Gln; (I)表示-OH,-Asn-OH,-Asn-Ser-OH,-Asn-Ser-Phe-OH,-Asn-Ser-Phe-Arg-OH或-Asn-Ser-Phe-Arg-Tyr- 哦; 符号“......”代表二硫键; 条件是1)α-hANP,2)α-hANP(7-28)和3)CNP-22被排除在该通式的范围之外。 还公开了抑制含有那些肽作为有效成分的血管平滑肌细胞生长的药剂。