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    TASTE-MODIFIED CREATINE SALTS, COMPOUNDS, COMPOSITIONS AND USES THEREOF
    8.
    发明申请
    TASTE-MODIFIED CREATINE SALTS, COMPOUNDS, COMPOSITIONS AND USES THEREOF 审中-公开

    公开(公告)号：WO2018208647A1

    公开(公告)日：2018-11-15

    申请号：PCT/US2018/031319

    申请日：2018-05-07

    Applicant: AUGUSTA UNIVERSITY RESEARCH INSTITUTE, INC.

    Inventor： LEBEDYEVA, Iryna ,  KLUG, Christopher

    IPC: A61K31/221 ,  C07C279/14

    Abstract: Provided are embodiments of creatine and creatine ethyl ester (CEE) salts where the anion is an artificial (non-saccharide) taste-modifier. These compounds represent stable white non-hygroscopic solids or semisolids that can readily dissolve in water and buffer solutions. Synthesis of novel creatine salts using environmentally safe solvents such as ethanol resulted in the formation of products in quantitative yields with sodium or potassium chloride as a byproduct. The creatine and creatine alkyl eater derivative salts are stable sweet-tasting compounds that are more palatable to a consumer than creatine or derivatives thereof.

    EFFLUX-PUMP INHIBITORS AND THERAPEUTIC USES THEREOF
    10.
    发明申请
    EFFLUX-PUMP INHIBITORS AND THERAPEUTIC USES THEREOF 审中-公开
    EFFLUX-PUMP抑制剂及其治疗用途

    公开(公告)号：WO2017042099A1

    公开(公告)日：2017-03-16

    申请号：PCT/EP2016/070727

    申请日：2016-09-02

    Applicant: BASILEA PHARMACEUTICA AG

    Inventor： GAUCHER, Bérangère ,  DREIER, Jürg

    IPC: C07D295/088 ,  C07C279/14 ,  C07C211/27 ,  C07C211/29 ,  C07C217/16 ,  C07C217/48 ,  C07C217/58 ,  C07C235/50 ,  C07C237/08 ,  A61K31/5375 ,  A61P31/04

    CPC classification number: C07D295/088 ,  C07C211/27 ,  C07C211/29 ,  C07C217/16 ,  C07C217/18 ,  C07C217/48 ,  C07C217/58 ,  C07C235/50 ,  C07C237/08 ,  C07C279/14

    Abstract: The present invention relates to compounds of formula I or pharmaceutically acceptable salt, solvate or hydrate thereof wherein ASC is -N(R8)ASC-1; ASC-1 is C 2 -C 5 alkylene-N(R9a)R9b or C(=O)-C 1 -C 4 alkylene-N(R9a)R9b, wherein in alkylene in both cases one -CH 2 - moiety is optionally replaced by -CH(N(R9a)R9b)- or -N(R9a)- or -CH(CH 3 )-; AR1, AR2 represent phenyl; L1 represents -CH=CH-, -CH 2 -0-, -(CH 2 ) 2 -O-, -0-CH 2 -, -C(CH 3 ) 2 -, -(CH 2 ) 2 - or -CH=CH-CH 2 -; L2 represents C 1 -C 7 alkylene, wherein one or more -CH2- moieties in the alkylene are optionally replaced independently by -N(R9a)-, -CH(N(R9a)R9b)-, or -C(=O)-, wherein within L2 there are no adjacent -C(=O)-moieties or adjacent -N(R9a)- moieties, and wherein the terminal moiety of L2 is not -N(R9a)-, or L2 represents -O-C 2 -C 6 alkylene-; the other definitions are as defined in the claims; and their use in methods of treating a subject with a microbial infection or susceptible to a microbial infection.

    Abstract translation: 本发明涉及式I化合物或其药学上可接受的盐，溶剂化物或水合物，其中ASC是-N（R8）ASC-1; ASC-1是C 2 -C 5亚烷基-N（R 9a）R 9b或C（= O）-C 1 -C 4亚烷基-N（R 9a）R 9b，其中在两种情况下的亚烷基中，一个-CH 2 - 部分任选地被 -CH（N（R9a）R9b） - 或-N（R9a） - 或-CH（CH3） - ; AR1，AR2表示苯基; L 1表示-CH = CH-，-CH 2 O - ， - （CH 2）2-O-，-O-CH 2 - ， - C（CH 3）2 - ， - （CH 2） CH = CH-CH 2 - ; L2表示C1-C7亚烷基，其中亚烷基中一个或多个-CH 2 - 部分任选被-N（R 9a） - ， - CH（N（R9a）R9b） - 或-C（= O） - 取代， 其中在L2内不存在相邻的-C（= O） - 或相邻的-N（R 9a） - 部分，并且其中L 2的末端部分不是-N（R 9a） - ，或者L 2代表-OC 2 -C 6亚烷基 - ; 其他定义如权利要求中所定义; 以及它们用于治疗微生物感染或易受微生物感染的受试者的方法。

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