Method for attaching polyethylene glycol to macromolecules
    5.
    发明授权
    Method for attaching polyethylene glycol to macromolecules 失效
    将聚乙二醇与大分子连接的方法

    公开(公告)号:US06677438B1

    公开(公告)日:2004-01-13

    申请号:US09462190

    申请日:2000-07-21

    IPC分类号: C07K100

    摘要: A process for attaching a polyethylene glycol compound to a macromolecule to prepare a conjugate or adduct between the polyethylene glycol compound and the macromolecule is described. The process comprises the steps of (1) preparing an activated PEG or an activated PEG derivative by incorporating an acrylic ester, an acrylic thioester or an acrylamido group into the PEG or PEG derivative; (2) reacting the activated PEG or PEG derivative with a macromolecular material comprising one or more sulphydryl groups, primary amino groups and/or secondary amino groups and (3) recovering the conjugate of the PEG or PEG derivative and the macromolecular material.

    摘要翻译: 描述了将聚乙二醇化合物连接到大分子以制备聚乙二醇化合物和大分子之间的缀合物或加合物的方法。 该方法包括以下步骤:(1)通过在丙二醇或PEG衍生物中加入丙烯酸酯,丙烯酸酯或丙烯酰胺基来制备活化的PEG或活化的PEG衍生物; (2)使活化的PEG或PEG衍生物与包含一个或多个巯基,伯氨基和/或仲氨基的大分子物质反应,和(3)回收PEG或PEG衍生物和高分子材料的共轭物。

    Drug delivery agents incorporating mitomycin
    6.
    发明授权
    Drug delivery agents incorporating mitomycin 失效
    掺入丝裂霉素的药物递送剂

    公开(公告)号:US5738864A

    公开(公告)日:1998-04-14

    申请号:US602733

    申请日:1996-02-20

    CPC分类号: A61K47/4823 A61K47/48338

    摘要: A conjugate of a carrier polymer and aziridine ring containing mitomycin (MMC) drug molecules is prepared by coupling the MMC molecules via their aziridine imino groups to spacer groups that terminate in protected amino groups, deprotecting said amino groups, recovering and purifying the spacer-MMC derivatives, and then coupling these derivatives via said deprotected amino groups to the carrier polymer. Alternatively, the MMC may first be treated with an activating agent, e.g. carbodiimidazole, to form an activated MMC derivative which is then coupled directly to spacer groups linked to the carrier polymer.

    摘要翻译: PCT No.PCT / IB94 / 00259 Sec。 371日期1996年2月20日 102(e)1996年2月20日PCT PCT 1994年8月17日PCT公布。 公开号WO95 / 05200 日期1995年2月23日载体聚合物和含有丝裂霉素(MMC)药物分子的氮丙啶环的缀合物是通过将MMC分子经由它们的氮丙啶亚氨基团偶联到终止于保护的氨基的间隔基团,将所述氨基脱保护,回收和 纯化间隔基MMC衍生物,然后将这些衍生物通过所述去保护的氨基偶联到载体聚合物上。 或者,MMC可以首先用活化剂处理,例如, 碳二咪唑,以形成活化的MMC衍生物,然后直接与连接至载体聚合物的间隔基团偶联。

    High polymers containing nicotinic acid, process for their preparation
and their use
    7.
    发明授权
    High polymers containing nicotinic acid, process for their preparation and their use 失效
    含有烟酸的高聚合物,其制备方法及其用途

    公开(公告)号:US4166902A

    公开(公告)日:1979-09-04

    申请号:US867889

    申请日:1978-01-09

    IPC分类号: C08B31/02 C08F8/30 C08F31/02

    CPC分类号: C08B31/02 C08F8/30

    摘要: New polymers consisting of a macromolecular structure of soluble starch to which 15-30% of nicotinic acid radicals are bound through covalent ester bonds. These polymers are gradually hydrolized in biological environment by setting free nicotinic acid and non toxic polysaccharide residues. These polymers have a therapeutic activity similar to that of nicotinic acid, but by far more long lasting and devoid of collateral effects.

    摘要翻译: 由可溶性淀粉的大分子结构组成的新型聚合物,其中15-30%的烟酸基团通过共价酯键结合。 这些聚合物通过设置游离烟酸和无毒多糖残基在生物环境中逐渐水解。 这些聚合物具有类似于烟酸的治疗活性,但是具有更长的持久性和无附着作用。

    Polymer-platinum compounds
    8.
    发明授权
    Polymer-platinum compounds 失效
    聚合物 - 铂化合物

    公开(公告)号:US5985916A

    公开(公告)日:1999-11-16

    申请号:US62372

    申请日:1998-04-17

    IPC分类号: A61K47/48 A61K31/28

    CPC分类号: A61K47/48207 A61K47/48192

    摘要: A polymer-platinum compound for use in tumor treatment is described. The compound is composed of a biodegradable diamido-diamine polymer linked to a platinum species. The platinum species is released from the polymer to yield a platinum species having anti-tumor activity.

    摘要翻译: 描述了用于肿瘤治疗的聚合物 - 铂化合物。 该化合物由与铂族物质连接的可生物降解的二酰氨基二胺聚合物组成。 铂族物质从聚合物中释放出来,产生具有抗肿瘤活性的铂族物质。

    High molecular weight polyesterpolycarbonates and the use thereof for
the preparation of bioerosible matrices
    9.
    发明授权
    High molecular weight polyesterpolycarbonates and the use thereof for the preparation of bioerosible matrices 失效
    高分子量聚酯聚碳酸酯及其在生物可吸收基质的制备中的应用

    公开(公告)号:US5698661A

    公开(公告)日:1997-12-16

    申请号:US637646

    申请日:1996-06-24

    CPC分类号: A61K9/1647 C08G63/64

    摘要: Polyesterpolycarbonates of formula (I) ##STR1## wherein a is an integer from 2 to 300; R.sub.1 and R.sub.2, which can be the same or different, are each a polyester residue of formula (II) ##STR2## with x and y being integers from 0 to 100, and the ratio of (x/x+y)*100 being between 0 and 100, with the proviso that x and y are not 0 at the same time; R.sub.3 and R.sub.4 being aliphatic hydrocarbon residues of 1 to 4 carbon atoms; R.sub.5 being an aliphatic hydrocarbon residue having from 2 to 18 carbon atoms or a cycloaliphatic hydrocarbon residue having from 3 to 8 carbon atoms; or a polyoxyalkylene residue of formula (III): ##STR3## wherein R.sub.6 is hydrogen or methyl, n is an integer from 1 to 3 and m is an integer from 1 to 200; and the two --R.sub.3 --COO and --R.sub.4 --COO groups are randomly distributed in the polyester residue, with the polyesterpolycarbonates of formula (I) having an intrinsic viscosity of greater than 0.45 dl/g when measured in chloroform at 32.degree. C. and being useful as bioerosible matrices for the controlled release of drugs.

    摘要翻译: PCT No.PCT / EP94 / 03560 Sec。 371日期1996年6月24日 102(e)1996年6月24日PCT 1994年10月28日PCT PCT。 公开号WO95 / 12629 日期:1995年5月11日式(I)的聚酯聚碳酸酯其中a是2至300的整数; R 1和R 2可以相同或不同,分别为式(II)的聚酯残基,其中x和y为0至100的整数,并且(x / x + y)* 100的比例为 在0和100之间,条件是x和y不同时为0; R 3和R 4是1至4个碳原子的脂族烃残基; R5是具有2至18个碳原子的脂族烃残基或具有3至8个碳原子的脂环族烃残基; 或式(III)的聚氧化烯残基:其中R 6为氢或甲基,n为1至3的整数,m为1至200的整数; 并且两个-R3-COO和-R4-COO基团随机分布在聚酯残基中,当在32℃的氯仿中测量时,式(I)的聚酯聚碳酸酯的特性粘度大于0.45dl / g, 作为药物受控释放的生物可吸收基质是有用的。

    Polycarbonates and the use thereof for the preparation of bioerosible
matrices
    10.
    发明授权
    Polycarbonates and the use thereof for the preparation of bioerosible matrices 失效
    聚碳酸酯及其在生物可活性基质的制备中的应用

    公开(公告)号:US5463012A

    公开(公告)日:1995-10-31

    申请号:US157153

    申请日:1993-12-13

    摘要: Polycarbonates of formula (I) wherein a is an integer from 2 to 300; R.sup.1 and R.sup.2 are the same or different and are independently a polyester residue of formula (III) wherein x and y are integers from 1 to 50, R.sup.4 and R.sup.5, which are the same or different, are aliphatic straight or branched hydrocarbon chains having from 1 to 4 carbon atoms, R.sup.6 is an aliphatic or alicyclic straight or branched chain having from 2 to 18 carbon atoms, or a polyoxyalkylene residue of formula (II), the two groups --R.sup.4 --COO and --R.sup.5 --COO being randomly distributed in the polyester residue, x and y being in any possible ratio from 0 to 100, are synthesized by reacting dihydroxy compounds with 1,1'-carbonyldiimidazole. They are useful for the preparation of bioerosible matrices for biologically active compounds. ##STR1##

    摘要翻译: PCT No.PCT / EP92 / 01262 Sec。 371日期:1993年12月10日 102(e)日期1993年12月10日PCT提交1992年6月5日PCT公布。 出版物WO92 / 22600 PCT 日期:1992年12月23日。式(I)的聚碳酸酯,其中a为2至300的整数; R 1和R 2相同或不同,并且独立地是式(III)的聚酯残基,其中x和y是1至50的整数,R 4和R 5相同或不同,是具有 1至4个碳原子,R6是具有2至18个碳原子的脂族或脂环族直链或支链或式(II)的聚氧化烯残基,两个-R4-COO和-R5-COO基团随机分布在 通过使二羟基化合物与1,1'-羰基二咪唑反应来合成聚酯残基x和y以0至100的任何可能的比例。 它们可用于制备生物活性化合物的生物可溶性基质。 (一)图像(二)<图像>(三)