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    • 5. 发明授权
    • Bifunctional synthetic molecules
    • 双功能合成分子
    • US08354116B2
    • 2013-01-15
    • US11820172
    • 2007-06-18
    • Stephen G. CarterKanu PatelZhen ZhuLixin Qiao
    • Stephen G. CarterKanu PatelZhen ZhuLixin Qiao
    • A61K9/00A61K8/02
    • C07D213/80C07C69/612C07C233/87C07C2601/14C07D207/16C07D217/26C07D233/06C07D233/24C07D233/50C07D417/04
    • The synthesis and use of bifunctional molecules to improve the topical and transdermal delivery efficiency of various types of therapeutic agents or agents designed to promote the transdermal delivery of those therapeutic agents either into the skin tissue or into the systemic circulation. Three major classes of molecules are covalently joined as bifunctional substances; chemical vasodilators, passive dermal penetration enhancers and therapeutic or diagnostic drugs. Chemical vasodilators may be delivered into the skin to increasing the blood flow in a tissue that has compromised circulation or they may be used as part of a delivery vehicle to promote the delivery of the drug. Passive dermal penetration enhancers are those chemicals that promote the passive penetration of drugs and other chemicals through the stratum corneum and epidermis of the skin tissue. Drugs and diagnostic agents are the third group of chemicals that are candidates for the linkage of molecules.
    • 双功能分子的合成和使用以改善各种类型治疗剂或试剂的局部和透皮递送效率,所述治疗剂或试剂旨在促进将这些治疗剂透皮递送至皮肤组织或进入体循环。 三大类分子共价连接成双功能物质; 化学血管扩张剂,被动皮肤渗透增强剂和治疗或诊断药物。 化学血管扩张剂可以被递送到皮肤中以增加已经损害循环的组织中的血液流动,或者它们可以用作递送载体的一部分以促进药物的递送。 被动皮肤渗透增强剂是促进药物和其他化学物质通过角质层和皮肤组织表皮的被动穿透的化学物质。 药物和诊断剂是作为分子连接的候选物的第三组化学品。
    • 9. 发明申请
    • Aralkyl ester soft drugs
    • 芳烷酯软药
    • US20070135505A1
    • 2007-06-14
    • US11652365
    • 2007-01-11
    • Paul Erhardt
    • Paul Erhardt
    • A61K31/4164A61K31/4166
    • C07D451/06A61K9/0048A61K31/4164A61K31/4166A61K45/06C07D209/28C07D211/90C07D223/22C07D233/50C07D233/76C07D261/16C07D277/56C07D401/06C07D405/12C07D473/06C07D475/08A61K2300/00
    • The present invention describes a method for programming a specific course and rate of metabolism for a parent drug compound that leads to an inactive or very weakly active and nontoxic metabolite when the modified drug compound is administered. The parent drug compound is modified by forming one or more of a predetermined chemical arrangement within the parent drug structure where the chemical arrangement is A-Φ-R—X—R′; where A is absent or is a tether moiety which allows for a metabolically stable chemical connection to be made to the parent drug compound; Φ is a substituted aryl or heteroaryl system that is already present within the parent drug compound or is specifically added to the parent drug compound via A; R is an alkyl or alkene containing chain either branched or unbranched from 0 to 10 carbons that is either also already present within the parent drug compound or is specifically added to the parent drug compound via connection to Φ; X is a carboxyl, sulfoxyl or phosphatyl function that is specifically added to the parent drug compound via connection to R; and, R′ is an added alkyl, alkenyl, or aralkyl group either branched or unbranched containing from 1 to 10 carbons, other common leaving group, or a structural element already present as an inherent portion of the parent drug compound.
    • 本发明描述了当施用改性药物化合物时,导致导致非活性或非常弱活性和无毒代谢物的母体药物的特定途径和代谢速率的方法。 母体药物化合物通过在化学排列是A-Phi-R-X-R'的母体药物结构内形成预定化学排列中的一种或多种进行改性; 其中A不存在或是能够与母体药物化合物进行代谢稳定的化学连接的系链部分; Phi是已经存在于母体药物中的取代的芳基或杂芳基体系,或通过A特异性地添加到母体药物化合物中; R是含有0〜10个碳原子的支链或不含支链的烷基或烯烃,其也已经存在于母体药物化合物中,或通过与Phi连接而特异性地添加到母体药物化合物中; X是通过与R连接而特异性地添加到母体药物化合物中的羧基,亚砜基或磷酰基官能团; R'是含有1至10个碳的支链或非支链的烷基,链烯基或芳烷基,其它常用的离去基团或已经作为母体药物化合物的固有部分存在的结构元件。