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19 条记录 (耗时 0.022 秒)

    Insoluble oxidation reagent
    4.
    发明授权
    Insoluble oxidation reagent 失效
    不溶氧化试剂

    公开(公告)号：US3959190A

    公开(公告)日：1976-05-25

    申请号：US479654

    申请日：1974-06-17

    申请人： Ned M. Weinshenker

    发明人： Ned M. Weinshenker

    IPC分类号： C07C45/29 ,  C07C45/30 ,  C08F8/34 ,  C08J9/36 ,  C08F28/04

    CPC分类号： C07C45/30 ,  C07C45/29 ,  C08F8/22 ,  C08F8/34 ,  Y10S521/921

    摘要： A polymeric sulfide oxidation reagent comprising a cross-linked polymeric resin carrying a plurality of lower alkyl sulfide groups, its preparation and its use as a co-reactant for the oxidation of primary and secondary alcohols are disclosed.

    摘要翻译： 公开了一种聚合硫化物氧化试剂，其包含携带多个低级烷基硫醚基团的交联聚合物树脂，其制备方法及其作为用于伯和仲醇氧化的共反应物的用途。

    Cobalamin conjugates for anti-tumor therapy
    5.
    发明授权
    Cobalamin conjugates for anti-tumor therapy 有权
    钴胺素共轭物用于抗肿瘤治疗

    公开(公告)号：US07232805B2

    公开(公告)日：2007-06-19

    申请号：US10659501

    申请日：2003-09-10

    申请人： Ned M. Weinshenker ,  Frederick G. West ,  Barbara A. Araneo ,  Weiping Li

    发明人： Ned M. Weinshenker ,  Frederick G. West ,  Barbara A. Araneo ,  Weiping Li

    IPC分类号： A01N43/04 ,  A61K31/70 ,  C07G3/00 ,  C07G11/00 ,  C07H15/00 ,  C07H17/00

    CPC分类号： A61K47/551

    摘要： The present invention provides a cobalamin-drug conjugate suitable for the treatment of tumor related diseases. Cobalamin is indirectly covalently bound to an anti-tumor drug via a cleavable linker and one or more optional spacers. Cobalamin is covalently bound to a first spacer or the cleavable linker via the 5′-OH of the cobalamin ribose ring. The drug is bound to a second spacer of the cleavable linker via an existing or added functional group on the drug. After administration, the conjugate forms a complex with transcobalamin (any of its isoforms). The complex then binds to a receptor on a cell membrane and is taken up into the cell. Once in the cell, an intracellular enzyme cleaves the conjugate thereby releasing the drug. Depending upon the structure of the conjugate, a particular class or type of intracellular enzyme affects the cleavage. Due to the high demand for cobalamin in growing cells, tumor cells typically take up a higher percentage of the conjugate than do normal non-growing cells. The conjugate of the invention advantageously provides a reduced systemic toxicity and enhanced efficacy as compared to a corresponding free drug.

    摘要翻译： 本发明提供了一种适用于治疗肿瘤相关疾病的钴胺素药物缀合物。 钴胺素通过可裂解连接体和一个或多个任选的间隔物间接共价结合抗肿瘤药物。 钴胺素通过钴胺核糖环的5'-OH共价结合到第一间隔物或可切割的接头。 药物通过药物上现有或添加的官能团与可切割接头的第二间隔物结合。 给药后，缀合物与转钴胺素（其任何同种型）形成复合物。 然后，该复合物与细胞膜上的受体结合，并被吸收到细胞中。 一旦在细胞中，细胞内酶切割缀合物从而释放药物。 根据缀合物的结构，细胞内酶的特定类别或类型影响切割。 由于对生长细胞中钴胺素的高需求，肿瘤细胞通常占有比正常非生长细胞更高的缀合物百分比。 与相应的游离药物相比，本发明的缀合物有利地提供降低的全身毒性和增强的功效。

    Pharmaceutical composition containing prostadienoic acid for regulating gastric secretion
    6.
    发明授权
    Pharmaceutical composition containing prostadienoic acid for regulating gastric secretion 失效
    含有前列腺素的药物组合物用于调节胃分泌

    公开(公告)号：US4115545A

    公开(公告)日：1978-09-19

    申请号：US823811

    申请日：1977-08-11

    申请人： Ned M. Weinshenker ,  Niels H. Anderson

    发明人： Ned M. Weinshenker ,  Niels H. Anderson

    IPC分类号： C07C405/00 ,  C07D307/935 ,  A61K31/22 ,  A61K31/19 ,  A61L9/04

    CPC分类号： C07D307/935 ,  C07C405/00 ,  C07C405/0041

    摘要： Novel alkyl diethers of prostaglandins of the formula; ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 and R.sub.6 are hydrogen when Y is a single bond and R.sub.2 and R.sub.6 are absent when Y is a double bond; R.sub.3 is keto, ##STR2## R'.sub.9 is hydrogen or lower alkyl; R'.sub.10 is lower alkyl; R'.sub.11 is lower alkyl; Z.sub.1 is cis or trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --; Z.sub.2 is trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --; X is a single bond or a double bond and X is a single bond when R.sub.4 and R.sub.5 are hydrogen; Y is a single bond or a double bond; n is 1 to 5, m is 0 to 4; and the non-toxic salts. The prostaglandin ethers possess valuable pharmacological properties as modifiers of smooth muscle activity, gastric secretion, blood pressure, lipolysis and the reproductive system. The compounds also induce labor and menses and they can be used for the relief of asthma and nasal congestion. The compounds are also useful as platelet anti-clumping agents and for the inhibition of peptic ulcers.

    摘要翻译： 式中前列腺素的新型烷基二醚; 其中R1是氢或低级烷基; 当Y是单键时，R2和R6是氢，当Y是双键时R2和R6不存在; R3是酮基，R'9是氢或低级烷基; R'10是低级烷基; R11为低级烷基; Z 1是顺式或反式-CH = CH-或-CH 2 CH 2 - ; Z2是反式-CH = CH-或-CH2CH2-; X是单键或双键，当R4和R5是氢时X是单键; Y是单键或双键; n为1〜5，m为0〜4; 和无毒盐。 前列腺素醚具有作为平滑肌活动，胃分泌，血压，脂肪分解和生殖系统改性剂的有价值的药理学性质。 这些化合物还可以诱发劳动和月经，并可用于缓解哮喘和鼻塞。 该化合物也可用作血小板抗凝块剂和抑制消化性溃疡。

    Cyclodextrins as carriers
    8.
    发明授权
    Cyclodextrins as carriers 失效
    环糊精作为载体

    公开(公告)号：US5068227A

    公开(公告)日：1991-11-26

    申请号：US298634

    申请日：1989-01-18

    申请人： Ned M. Weinshenker

    发明人： Ned M. Weinshenker

    IPC分类号： A61K47/48 ,  C08B37/16 ,  G01N33/531 ,  G01N33/532

    CPC分类号： B82Y5/00 ,  A61K47/48961 ,  A61K47/48969 ,  C08B37/0012 ,  G01N33/531 ,  G01N33/532 ,  Y10T436/13

    摘要： Cyclodextrins can be coupled to biorecognition molecules such as antibodies. The cyclodextrins so coupled provide a cavity or complexation zone into which active agents such as labels, drugs and the like may be incorporated. The active agent forms a noncovalently bonded inclusion complex within the cavity of the cyclodextrin. It remains associated with the cyclodextrin and the coupled biorecognition molecule and thus can be delivered to the other half of the biospecific recognition pair. A process for producing these materials is also disclosed. The process includes the steps of activating a primary hydroxyl site on a cyclodextrin; linking a biorecognition molecule to the activated primary hydroxyl site on the cyclodextrin in either a direct covalent linkage or through a covalently linked spacer; and introducing a guest molecule (active agent) into the cavity of the derivatized cyclodextrin to form an inclusion complex.

    摘要翻译： 环糊精可以与生物识别分子如抗体偶联。 如此耦合的环糊精提供空腔或络合区，其中可以并入活性剂如标签，药物等。 活性剂在环糊精的空腔内形成非共价键合的包合络合物。 它仍然与环糊精和偶联生物识别分子相关联，因此可以被递送到生物特异性识别对的另一半。 还公开了这些材料的制造方法。 该方法包括在环糊精上活化伯羟基位点的步骤; 将生物识别分子与直链共价键或通过共价连接的间隔基上的环糊精上的活化的伯羟基位点连接; 并将客体分子（活性剂）引入到衍生化的环糊精的空腔中以形成包合物。

    Alkyl diethers of prostaglandins
    9.
    发明授权
    Alkyl diethers of prostaglandins 失效
    前列腺素的烷基二醚

    公开(公告)号：US4055593A

    公开(公告)日：1977-10-25

    申请号：US570621

    申请日：1975-04-23

    申请人： Ned M. Weinshenker ,  Niels H. Andersen

    发明人： Ned M. Weinshenker ,  Niels H. Andersen

    IPC分类号： C07C405/00 ,  C07D307/935 ,  C07C177/00

    CPC分类号： C07D307/935 ,  C07C405/00 ,  C07C405/0041

    摘要： Novel alkyl diethers of prostaglandins of the formula; ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 and R.sub.6 are hydrogen when Y is a single bond and R.sub.2 and R.sub.6 are absent when Y is a double bond; R.sub.3 is keto, ##STR2## R.sub.4 is hydrogen or ##STR3## R'.sub.9 is hydrogen or lower alkyl; R'.sub.10 is lower alkyl; R'.sub.11 is lower alkyl; Z.sub.1 is cis or trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --; Z.sub.2 is trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --; X is a single bond or a double bond and X is a single bond when R.sub.4 and R.sub.5 are hydrogen; Y is a single bond or a double bond; n is 1 to 5, m is 0 to 4; and the non-toxic salts. The prostaglandin ethers possess valuable pharmacological properties as modifiers of smooth muscle activity, gastric secretion, blood pressure, lipolysis and the reproductive system. The compounds also induce labor and menses and they can be used for the relief of asthma and nasal congestion. The compounds are also useful as platelet anti-clumping agents and for the inhibition of peptic ulcers.

    摘要翻译： 式中前列腺素的新型烷基二醚; 其中R1是氢或低级烷基; 当Y是单键时，R2和R6是氢，当Y是双键时R2和R6不存在; R 3是酮基，R 4是氢或R 1是氢或低级烷基; R'10是低级烷基; R11为低级烷基; Z 1是顺式或反式-CH = CH-或-CH 2 CH 2 - ; Z2是反式-CH = CH-或-CH2CH2-; X是单键或双键，当R4和R5是氢时X是单键; Y是单键或双键; n为1〜5，m为0〜4; 和无毒盐。 前列腺素醚具有作为平滑肌活动，胃分泌，血压，脂肪分解和生殖系统改性剂的有价值的药理学性质。 这些化合物还可以诱发劳动和月经，并可用于缓解哮喘和鼻塞。 该化合物也可用作血小板抗凝块剂和抑制消化性溃疡。