利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

26 条记录 (耗时 0.042 秒)

    GALANTAMINE AMINO ACID AND PEPTIDE PRODRUGS AND USES THEREOF
    2.
    发明申请
    GALANTAMINE AMINO ACID AND PEPTIDE PRODRUGS AND USES THEREOF 审中-公开
    甘氨酸氨基酸和肽类产品及其用途

    公开(公告)号：US20120184532A1

    公开(公告)日：2012-07-19

    申请号：US13386335

    申请日：2010-07-23

    申请人： Richard Franklin ,  Bernard T. Golding ,  Robert G. Tyson

    发明人： Richard Franklin ,  Bernard T. Golding ,  Robert G. Tyson

    IPC分类号： A61K31/55 ,  A61P25/28 ,  A61P1/12 ,  A61P1/08 ,  C07D491/048 ,  A61P1/00

    CPC分类号： C07D491/06

    摘要： Prodrugs of galantamine or its 3-hydroxy metabolite with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and methods for treating a memory or cognition disorder with the galantamine prodrugs are provided herein. Prodrugs having side chains of valine, phenylalanine, tyrosine or para amino benzoic acid and mono-, di- and tripeptides thereof are preferred. Additionally, methods for avoiding or minimizing the adverse gastrointestinal side effects associated with galantamine administration, as well as improving the pharmacokinetics of galantamine are provided herein.

    摘要翻译： 本文提供加兰他敏或其具有氨基酸或短肽的3-羟基代谢物的前药，含有这些前药的药物组合物和用加兰他敏前药治疗记忆障碍或认知障碍的方法。 具有缬氨酸，苯丙氨酸，酪氨酸或对氨基苯甲酸侧链的前药和其一，二和三肽是优选的。 此外，本文提供了用于避免或最小化与加兰他敏施用相关的不良胃肠道副作用以及改善加兰他敏的药代动力学的方法。

    GALANTAMINE AMINO ACID AND PEPTIDE PRODRUGS AND USES THEREOF
    5.
    发明申请
    GALANTAMINE AMINO ACID AND PEPTIDE PRODRUGS AND USES THEREOF 审中-公开
    甘氨酸氨基酸和肽类产品及其用途

    公开(公告)号：US20110098278A1

    公开(公告)日：2011-04-28

    申请号：US12843003

    申请日：2010-07-23

    申请人： Richard Franklin ,  Bernard T. Golding ,  Robert G. Tyson

    发明人： Richard Franklin ,  Bernard T. Golding ,  Robert G. Tyson

    IPC分类号： A61K31/55 ,  C07D491/06 ,  A61P25/28

    CPC分类号： C07D491/06

    摘要： Prodrugs of galantamine or its 3-hydroxy metabolite with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and methods for treating a memory or cognition disorder with the galantamine prodrugs are provided herein. Prodrugs having side chains of valine, phenylalanine, tyrosine or para amino benzoic acid and mono-, di- and tripeptides thereof are preferred. Additionally, methods for avoiding or minimizing the adverse gastrointestinal side effects associated with galantamine administration, as well as improving the pharmacokinetics of galantamine are provided herein.

    摘要翻译： 本文提供加兰他敏或其具有氨基酸或短肽的3-羟基代谢物的前药，含有这些前药的药物组合物和用加兰他敏前药治疗记忆障碍或认知障碍的方法。 具有缬氨酸，苯丙氨酸，酪氨酸或对氨基苯甲酸侧链的前药和其一，二和三肽是优选的。 此外，本文提供了用于避免或最小化与加兰他敏施用相关的不良胃肠道副作用以及改善加兰他敏的药代动力学的方法。

    PRODRUGS OF GUANFACINE
    6.
    发明申请
    PRODRUGS OF GUANFACINE 审中-公开
    关系准则

    公开(公告)号：US20110065796A1

    公开(公告)日：2011-03-17

    申请号：US12882813

    申请日：2010-09-15

    申请人： Rhys Whomsley ,  Richard Franklin ,  Bernard T. Golding ,  Robert G. Tyson

    发明人： Rhys Whomsley ,  Richard Franklin ,  Bernard T. Golding ,  Robert G. Tyson

    IPC分类号： A61K31/198 ,  C07C279/22 ,  A61K31/165 ,  C07C279/26 ,  A61P1/00 ,  A61P25/00 ,  A61P9/00

    CPC分类号： C07C279/22 ,  C07B2200/07 ,  C07C279/24

    摘要： Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration, as well as improving the pharmacokinetics of guanfacine are provided herein.

    摘要翻译： 本发明提供了具有氨基酸或短肽的胍法辛的前药，含有这些前药的药物组合物和用胍法酰前药治疗ADHD / ODD（注意缺陷多动障碍和对抗性蔑视障碍）提供治疗益处的方法。 此外，本文提供了用于最小化或避免与胍法卡因给药相关的不良胃肠道副作用以及改善胍法辛的药代动力学的方法。

    AMINO ACID AND PEPTIDE PRODRUGS OF OPIOID ANALGESICS WITH REDUCED GI SIDE-EFFECTS
    7.
    发明申请
    AMINO ACID AND PEPTIDE PRODRUGS OF OPIOID ANALGESICS WITH REDUCED GI SIDE-EFFECTS 审中-公开
    具有减少胃肠道功能障碍的阿片类药物的氨基酸和肽类产品

    公开(公告)号：US20090192095A1

    公开(公告)日：2009-07-30

    申请号：US12356034

    申请日：2009-01-19

    申请人： Richard Franklin ,  Bernard T. Golding ,  Robert G. Tyson

    发明人： Richard Franklin ,  Bernard T. Golding ,  Robert G. Tyson

    IPC分类号： A61K38/05 ,  A61K31/485 ,  A61K31/55 ,  A61K31/4355 ,  C07D223/04 ,  C07D489/08 ,  C07D491/08 ,  A61P1/00

    CPC分类号： C07D223/04 ,  A61K47/542 ,  A61K47/65 ,  C07D489/08 ,  C07D489/12

    摘要： 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 peptide of 1-5 amino acids in length, 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.

    摘要翻译： 本发明涉及减少受试者胃肠道副作用的方法，胃肠道副作用与阿片样物质镇痛剂的给药有关。 所述方法包括向受试者口服阿片样物质前药或其药学上可接受的盐，其中阿片样物质前药由通过氨基甲酸酯键与长度为1-5个氨基酸的肽共价结合的阿片样物质止痛剂组成，其中口服给药 ，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。

    Tetracyclic compounds for enhancing biosynthesis of erythropoietin, compositions containing same, and methods of use thereof
    8.
    发明授权
    Tetracyclic compounds for enhancing biosynthesis of erythropoietin, compositions containing same, and methods of use thereof 失效
    用于增强促红细胞生成素生物合成的四环化合物，含有它们的组合物及其使用方法

    公开(公告)号：US5985913A

    公开(公告)日：1999-11-16

    申请号：US69693

    申请日：1998-04-29

    申请人： Jonathan Gareth Williams ,  David R. Houck ,  David Edward Smith ,  Daniel Lee Rathbone ,  David Charles Billington ,  Bernard T. Golding ,  Eric W. Collington ,  John Kitchin ,  Nicholas Rich

    发明人： Jonathan Gareth Williams ,  David R. Houck ,  David Edward Smith ,  Daniel Lee Rathbone ,  David Charles Billington ,  Bernard T. Golding ,  Eric W. Collington ,  John Kitchin ,  Nicholas Rich

    IPC分类号： A61K31/352 ,  C07D311/94 ,  A61K31/35 ,  A61K31/365 ,  C07D311/78

    CPC分类号： C07D311/94 ,  A61K31/352

    摘要： The present invention provides a compound in substantially pure form having the structure: ##STR1## wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 may independently be hydrogen, halogen, nitro, CF.sub.3, hydroxy, C.sub.1-5 alkyl, aryl or OR.sub.9, wherein R.sub.9 is C.sub.1-5 alkyl, wherein R.sub.10 is COC.sub.1-5 alkyl; or wherein any two consecutive R groups may be members of a C.sub.5 -C.sub.6 membered ring, and wherein the intracyclic-dashed line represents a covalent bond which may be present or absent, with the proviso that when R.sub.10 is present, the exocyclic-covalent bond is absent, and when R.sub.10 is absent, the exocyclic-covalent bond is present, and with the proviso that when R.sub.10 is absent, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 cannot all be hydrogen and when R.sub.10 is absent, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 cannot all be hydrogen when either R.sub.1, R.sub.2, R.sub.3, or R.sub.4 is hydroxy, or R2 is carboethoxy. The present invention further provides a composition comprising the compound described above in an amount effective to modulate cellular expression of a mammalian gene encoding erythropoietin and a carrier.

    摘要翻译： 本发明提供具有以下结构的基本上纯的形式的化合物：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8各自独立地为氢，卤素，硝基，CF 3，羟基，C 1-5烷基 ，芳基或OR9，其中R9为C1-5烷基，其中R10为COC1-5烷基; 或其中任何两个连续的R基团可以是C 5 -C 6的环的成员，并且其中所述环内虚线表示可以存在或不存在的共价键，条件是当R 10存在时，所述环外共价键为 当不存在R 10时，存在环外共价键，条件是当R 10不存在时，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8不能全部为氢，当R 10为 当R 1，R 2，R 3或R 4为羟基或R 2为乙氧基乙氧基时，R 5，R 6，R 7和R 8不能全部为氢。 本发明还提供一种包含上述化合物的组合物，其量可有效调节编码促红细胞生成素和载体的哺乳动物基因的细胞表达。

    Substituted quinazolines for reducing platelet count
    9.
    发明授权
    Substituted quinazolines for reducing platelet count 有权
    取代喹唑啉用于减少血小板计数

    公开(公告)号：US08304420B2

    公开(公告)日：2012-11-06

    申请号：US11946536

    申请日：2007-11-28

    申请人： Richard Franklin ,  Bernard T. Golding ,  Peter A. Cicala

    发明人： Richard Franklin ,  Bernard T. Golding ,  Peter A. Cicala

    IPC分类号： A61K31/517

    CPC分类号： C07D487/04 ,  C07D239/84

    摘要： This invention relates to the discovery of prodrugs of 3-or 5-substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting the formation of blood platelets. An example of a compound of the present invention is methyl 2-(2-amino-5,6- dichloroquinazolin-3 (4H)-yl)-2-methylpropanoate or the 3,3-demethyl anagrelide open-ringed analog.

    摘要翻译： 本发明涉及降低选择性血小板降低剂阿那格雷的3或5-取代的类似物的前药，其具有降低心血管副作用的潜力，因此应该导致改善的患者依从性和治疗骨髓增生性疾病的安全性。 更具体地，本发明涉及在人类中作为血小板降低剂具有效用的某些咪唑并喹唑啉衍生物的前药。 本发明化合物通过抑制血小板的形成起作用。 本发明化合物的实例是2-（2-氨基-5,6-二氯喹唑啉-3（4H） - 基）-2-甲基丙酸甲酯或3,3-去甲基阿那格雷开环类似物。

    NOVEL CARBAMATE AMINO ACID AND PEPTIDE PRODRUGS OF OPIATES AND USES THEREOF
    10.
    发明申请
    NOVEL CARBAMATE AMINO ACID AND PEPTIDE PRODRUGS OF OPIATES AND USES THEREOF 审中-公开
    新型卡氨酸氨基酸和肽类的优点及其用途

    公开(公告)号：US20120270847A1

    公开(公告)日：2012-10-25

    申请号：US13383831

    申请日：2010-07-16

    申请人： Richard Franklin ,  Bernard T. Golding ,  Robert G. Tyson

    发明人： Richard Franklin ,  Bernard T. Golding ,  Robert G. Tyson

    IPC分类号： A61K31/55 ,  C07D223/04 ,  A61K31/625 ,  C07D403/12 ,  C07D411/12 ,  A61P25/04 ,  C07D405/12

    CPC分类号： C07D223/04

    摘要： 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.

    摘要翻译： 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。