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    GLUTAMINASE INHIBITORS
    61.
    发明申请
    GLUTAMINASE INHIBITORS 审中-公开

    公开(公告)号：US20170290815A1

    公开(公告)日：2017-10-12

    申请号：US15516002

    申请日：2015-10-01

    申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education ,  Cornell University

    发明人： Lee A. McDermott ,  Prema C. Iyer ,  Richard A. Cerione ,  William P. Katt

    IPC分类号： A61K31/433 ,  C07D417/14 ,  C07D417/12 ,  A61K31/4535 ,  C07D285/135

    CPC分类号： A61K31/433 ,  A61K31/4535 ,  C07D285/135 ,  C07D401/14 ,  C07D417/12 ,  C07D417/14

    摘要： A compound, or a pharmaceutically acceptable salt thereof, having a structure of: wherein A is a ring; Y1 and Y2 are each independently N or C with the proper valency; X1 and X2 are each independently —NH—, —O—, —CH2—O—, —NH—CH2—, or —N(CH3)—CH2—, provided that when at least one of X1 and X2 is —CH2—O—, —NH—CH2—, or —N(CH3)—CH2— then the —CH2— is directly connected to A; a and b are each independently 0 or 1; c and d are each independently 0 or 1; Z1 and Z2 are each independently a heterocyclic; and R1 and R2 are each independently optionally substituted alkyl, optionally substituted aralkyl, optionally substituted cycloalkyl, amino, optionally substituted heteroaralkyl, optionally substituted alkylalkoxy, optionally substituted alkylaryloxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocycloalkyl; provided that if Y1 and Y2 are each C, then a is 1 and b is 1; provided that if Y1 and Y2 are each N, then a is 0 and b is 0; provided that if Y1 is N and Y2 is C, then a=0 and b=1; provided that if Y1 is C and Y2 is N, then a=1 and b=0; provided that if c=0 and d=0, then R1 and R2 are both amino; provided that if c is 1 and d is 1, then both R1 and R2 are not amino; provided that if c is 0 and d is 1, then R1 is amino and R2 is optionally substituted alkyl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted heteroaralkyl, optionally substituted alkylalkoxy, optionally substituted alkylaryloxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocycloalkyl; and provided that if c is 1 and d is 0, then R2 is amino and R1 is optionally substituted alkyl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted heteroaralkyl, optionally substituted alkylalkoxy, optionally substituted alkylaryloxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocycloalkyl.

    Implantable Polymeric Device for Sustained Release of Sufentanil
    66.
    发明申请
    Implantable Polymeric Device for Sustained Release of Sufentanil 审中-公开
    用于持续释放舒芬太尼的可植入聚合物

    公开(公告)号：US20170014515A1

    公开(公告)日：2017-01-19

    申请号：US15238614

    申请日：2016-08-16

    申请人： ANTECIP BIOVENTURES II LLC

    发明人： Herriot Tabuteau

    IPC分类号： A61K47/34 ,  A61K9/00 ,  A61K31/4535

    摘要： Extended release of sufentanil is provided by implanting a device containing sufentanil into a mammal or human being. The device may include a solid biocompatible polymer matrix, and sufentanil may be encapsulated within the polymer matrix. The polymer matrix comprises a plurality of pores configured to allow contact between the sufentanil and a physiological fluid of a mammal into which the device is implanted to thereby release sufentanil in vivo from the device into the mammal. The devices may be used to treat opioid addiction or pain.

    摘要翻译： 通过将含有舒芬太尼的装置植入哺乳动物或人类来提供舒芬太尼的延长释放。 该装置可以包括固体生物相容性聚合物基质，舒芬太尼可以包封在聚合物基质内。 聚合物基质包括构造成允许舒芬太尼与装置植入的哺乳动物的生理液体之间的接触的多个孔，从而将体内的舒芬太尼从装置释放到哺乳动物中。 这些装置可用于治疗阿片样物质成瘾或疼痛。