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    Antifibrotic effects of oxetanyl sulfoxides
    51.
    发明授权
    Antifibrotic effects of oxetanyl sulfoxides 有权

    公开(公告)号：US09676738B2

    公开(公告)日：2017-06-13

    申请号：US15293107

    申请日：2016-10-13

    申请人： University of Pittsburgh—Of the Commonwealth System of Higher Education ,  Medical University of South Carolina

    发明人： Peter Wipf ,  Carol A. Feghali-Bostwick

    IPC分类号： C07D305/08 ,  C07D305/06

    CPC分类号： C07D305/08 ,  C07D305/06

    摘要： A compound, or a pharmaceutically acceptable salt thereof, having a structure of wherein Z is aryl or substituted aryl, heteroaryl, or substituted heteroaryl; X is —S—, —S(O)—, or S(O)2—; R20 and R21 are each independently H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, or halogenated alkyl; one of R22, R23, and R24 is —O— and the others of R22, R23 and R24 are independently —CH2—, or —C(R13)— wherein R13 is alkyl, alkenyl, alkynyl, trialkylsilyl group, or —(CH2)mOR15, wherein R15 is alkyl or an aryl and m is an integer in the range of 1 to 10; and R25 is H, alkyl, substituted alkyl, halogen, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, C1-C3 alkoxy, aryloxy, or —(CH2)qOR17, wherein R17 is alkyl an aryl and q is an integer in the range of 1 to 10.

    BIFUNCTIONAL COMPOUNDS
    52.
    发明申请
    BIFUNCTIONAL COMPOUNDS 有权
    双功能化合物

    公开(公告)号：US20160176836A1

    公开(公告)日：2016-06-23

    申请号：US14880862

    申请日：2015-10-12

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

    发明人： Peter Wipf ,  Joel S. Greenberger ,  Michael W. Epperly ,  Melissa M. Sprachman ,  Julie Pamela Goff

    IPC分类号： C07D305/06 ,  C07K5/097 ,  C07D405/12

    CPC分类号： C07D305/06 ,  C07D205/04 ,  C07D405/12 ,  C07D405/14 ,  C07K5/06078 ,  C07K5/0812 ,  C07K5/0823

    摘要： A compound having the formula: wherein X is S, SO or SO2; one of R1, R2, and R3 is O and the others of R1, R2 and R3 are independently, the same or different, CH2, or CR13 wherein, R13 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)mOR15, wherein R15 is an alkyl group or an aryl group and m is an integer in the range of 1 to 10, and one of R5, R6, and R7 is O and the others of R5, R6 and R7 are independently, the same or different, CH2, or CR14 wherein, R14 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)nOR16, wherein R16 is an alkyl group or an aryl group and n is an integer in the range of 1 to 10; R4 and R8 are independently, the same or different, H, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group, a C1-C3 alkoxy group, an aryloxy group, or —(CH2)qOR17, wherein R17 is an alkyl group or an aryl group and q is an integer in the range of 1 to 10, provided that R4 is not a C1-C3 alkoxy group or an aryloxy group when R1 or R3 is O and R8 is not a C1-C3 alkoxy group or an aryloxy group when R5 or R7 is O; R9, R10, R11 and R12 are independently, the same or different, H, an alkyl group, an alkenyl group, an alkynyl group, or an aryl group.

    摘要翻译： 具有下式的化合物：其中X是S，SO或SO 2; R 1，R 2和R 3中的一个为O，R 1，R 2和R 3中的一个独立地为相同或不同的CH 2或CR 13，其中R 13为烷基，烯基，炔基，三烷基甲硅烷基 或 - （CH 2）m OR 15，其中R 15是烷基或芳基，m是1至10的整数，R 5，R 6和R 7中的一个是O，而其中R 5，R 6和 R7独立地相同或不同，CH2或CR14，其中R14是烷基，烯基，炔基，三烷基甲硅烷基或 - （CH2）nOR16，其中R16是烷基或芳基 n为1〜10的整数， R4和R8独立地相同或不同，为氢，烷基，烯基，炔基，芳基，杂芳基，C1-C3烷氧基，芳氧基或 - （CH2）qOR17 其中R 17为烷基或芳基，q为1〜10的整数，条件是当R 1或R 3为O时，R 4不为C 1 -C 3烷氧基或芳氧基，且R 8不为 当R 5或R 7为O时，C 1 -C 3烷氧基或芳氧基; R 9，R 10，R 11和R 12独立地为相同或不同的H，烷基，烯基，炔基或芳基。

    NOVEL TLR4 INHIBITORS FOR THE TREATMENT OF HUMAN INFECTIOUS AND INFLAMMATORY DISORDERS
    54.
    发明申请
    NOVEL TLR4 INHIBITORS FOR THE TREATMENT OF HUMAN INFECTIOUS AND INFLAMMATORY DISORDERS 有权
    新型TLR4抑制剂治疗人类感染性和炎症性疾病

    公开(公告)号：US20150250809A1

    公开(公告)日：2015-09-10

    申请号：US14717349

    申请日：2015-05-20

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

    发明人： Peter Wipf ,  Matthew D. Neal ,  Sodhi P. Chhinder ,  David J. Hackam

    IPC分类号： A61K31/7024 ,  A61K31/7034 ,  A61K31/7028

    CPC分类号： A61K31/7028 ,  A61K31/351 ,  A61K31/7008 ,  A61K31/7024 ,  A61K31/7034

    摘要： The present invention relates to methods of treating infectious, inflammatory and post-traumatic disorders by administering various compounds newly discovered to have TLR4 inhibitory activity. In addition to methods of treatment, the present invention further provides for pharmaceutical compositions comprising said compounds, together with a suitable pharmaceutical carrier. Because TLR4 is the most upstream receptor in the pro-inflammatory LPS signaling cascade, treatments of the invention, which inhibit or antagonize TLR4 action, may avoid the pitfalls associated with other cytokine inhibitors that act further down the pathway and accordingly play a less specific (and perhaps non-critical) role.

    摘要翻译： 本发明涉及通过施用新发现的具有TLR4抑制活性的各种化合物来治疗感染性，炎性和创伤后疾病的方法。 除了治疗方法之外，本发明还提供包含所述化合物以及合适的药物载体的药物组合物。 因为TLR4是促炎性LPS信号级联中最上游的受体，因此抑制或拮抗TLR4作用的本发明的治疗可以避免与其他细胞因子抑制剂相关的陷阱，其进一步沿着该途径起作用并因此发挥较少的特异性 也许是非关键的）角色。

    Selective potassium channel agonists
    56.
    发明授权
    Selective potassium channel agonists 有权

    公开(公告)号：US11358930B2

    公开(公告)日：2022-06-14

    申请号：US17048878

    申请日：2019-03-08

    申请人： University of Pittsburgh—Of the Commonwealth System of Higher Education

    发明人： Peter Wipf

    IPC分类号： C07C271/26 ,  C07C271/38 ,  C07D213/38 ,  C07D213/61 ,  A61P27/16 ,  A61P25/08

    摘要： Selective potassium channel agonists and methods of use thereof are disclosed. A compound, or a pharmaceutically acceptable salt thereof, having a formula I wherein R1 is H or optionally-substituted alkyl; R2 is optionally-substituted C1-C6 alkyl or optionally-substituted cyclopropyl; R3 and R4 are each independently H or optionally-substituted alkyl; R5 is H, optionally-substituted alkyl, acyl, or alkoxycarbonyl; R6 and R7 are each independently H, optionally-substituted alkyl, or R6 and R7 together form a carbocycle; R8 is substituted phenyl or optionally-substituted pyridinyl, provided that if R8 is substituted phenyl, then R2 is optionally-substituted cyclopropyl; and R9, R10 and R11 are each independently H, halo, or optionally-substituted alkyl.