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    • 4. 发明申请
    • NOVEL CARBAMATE AMINO ACID AND PEPTIDE PRODRUGS OF OPIATES AND USES THEREOF
    • 新型卡氨酸氨基酸和肽类的优点及其用途
    • US20120270847A1
    • 2012-10-25
    • US13383831
    • 2010-07-16
    • Richard FranklinBernard T. GoldingRobert G. Tyson
    • Richard FranklinBernard T. GoldingRobert G. Tyson
    • A61K31/55C07D223/04A61K31/625C07D403/12C07D411/12A61P25/04C07D405/12
    • C07D223/04
    • Carbamate linked prodrugs of meptazinol and other opioid analgesics are provided. The prodrug moiety may comprise a single amino acid or short peptide. Additionally, the present invention relates to methods for reducing gastrointestinal side effects in a subject, the gastrointestinal side effects being associated with the administration of an opioid analgesic. The methods comprise orally administering an opioid prodrug or pharmaceutically acceptable salt thereof to a subject, wherein the opioid pro-drug is comprised of an opioid analgesic covalently bonded through a carbamate linkage to a prodrug moiety, and wherein upon oral administration, the prodrug or pharmaceutically acceptable salt minimizes at least one gastrointestinal side effect associated with oral administration of the opioid analgesic alone. Compositions for use with the method are also provided.
    • 提供了美珠坚醇和其他阿片样镇痛药的氨基甲酸酯连接前体药物。 前药部分可以包含单个氨基酸或短肽。 另外,本发明涉及减少受试者胃肠道副作用的方法,胃肠副作用与阿片类镇痛剂的给药有关。 所述方法包括将阿片样物质前药或其药学上可接受的盐口服给予受试者,其中所述阿片类药物由通过氨基甲酸酯键与前药部分共价结合的阿片样物质止痛剂组成,并且其中口服给药前药或药学上 可接受的盐使与单独的阿片样物质镇痛剂的口服给药相关的至少一种胃肠道副作用最小化。 还提供了与该方法一起使用的组合物。
    • 6. 发明申请
    • NOVEL CARBAMATE AMINO ACID AND PEPTIDE PRODRUGS OF OPIOIDS AND USES THEREOF
    • 新型卡氨酸氨基酸和肽类物质及其用途
    • US20110015182A1
    • 2011-01-20
    • US12837788
    • 2010-07-16
    • Richard FranklinBernard T. GoldingRobert G. Tyson
    • Richard FranklinBernard T. GoldingRobert G. Tyson
    • A61K31/55C07D223/04C07D405/12C07D403/12C07D411/12C07D223/10A61P25/04
    • C07D223/04
    • Carbamate linked prodrugs of meptazinol and other opioid analgesics are provided. The prodrug moiety may comprise a single amino acid or short peptide. Additionally, the present invention relates to methods for reducing gastrointestinal side effects in a subject, the gastrointestinal side effects being associated with the administration of an opioid analgesic. The methods comprise orally administering an opioid prodrug or pharmaceutically acceptable salt thereof to a subject, wherein the opioid prodrug is comprised of an opioid analgesic covalently bonded through a carbamate linkage to a prodrug moiety, and wherein upon oral administration, the prodrug or pharmaceutically acceptable salt minimizes at least one gastrointestinal side effect associated with oral administration of the opioid analgesic alone. Compositions for use with the method are also provided.
    • 提供了美珠坚醇和其他阿片样镇痛药的氨基甲酸酯连接前体药物。 前药部分可以包含单个氨基酸或短肽。 另外,本发明涉及减少受试者胃肠道副作用的方法,胃肠副作用与阿片类镇痛剂的给药有关。 所述方法包括将阿片样物质前药或其药学上可接受的盐口服给予受试者,其中所述阿片样物质前药由通过氨基甲酸酯键与前药部分共价结合的阿片类止痛剂组成,并且其中口服给药时,所述前药或药学上可接受的盐 使与阿片类镇痛药单独口服给药相关的至少一种胃肠道副作用最小化。 还提供了与该方法一起使用的组合物。