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    TOPICAL FORMULATIONS
    2.
    发明申请
    TOPICAL FORMULATIONS 审中-公开

    公开(公告)号：WO2020106304A1

    公开(公告)日：2020-05-28

    申请号：PCT/US2019/000066

    申请日：2019-11-20

    Applicant: NFLECTION THERAPEUTICS, INC.

    Inventor： KINCAID, John ,  NEWSAM, John ,  KISAK, Edward ,  WOOTTON, Michael ,  KUSHWAHA, Avadhesh

    IPC: A61K31/166 ,  A61K47/38 ,  A61K9/06

    Abstract: Provided herein are gelled topical formulations for the treatment of skin diseases comprising: a) a MEK inhibitor; b) one or more organic solvents in an amount of about 70% to about 99% by weight; and c) a gelling agent; wherein the one or more organic solvents are selected from the group consisting of C2-6 alcohol, a C2-6 alkylene glycol, a di-(C2-6 alkylene) glycol, a polyethylene glycol, C1-3 alkyl-(OCH2CH2)1-5-OH, DMSO, ethyl acetate, acetone, N-methyl pyrrolidone, benzyl alcohol, glycerin, and an oil; the gelling agent is hydroxypropyl cellulose having a molecular weight ranging from about 40,000 Dato about 2,500,000 Da; and wherein the gelled topical formulation has a viscosity of from 1 to 25,000 cps; and DMSO, when present, is combined with at least one other of said organic solvents such that DMSO is present in an amount of less than 50% by weight.

    PROCESSES FOR PREPARING PYRROLOPYRIDINE-ANILINE COMPOUNDS
    4.
    发明申请
    PROCESSES FOR PREPARING PYRROLOPYRIDINE-ANILINE COMPOUNDS 审中-公开

    公开(公告)号：WO2022159600A1

    公开(公告)日：2022-07-28

    申请号：PCT/US2022/013153

    申请日：2022-01-20

    Applicant: NFLECTION THERAPEUTICS, INC.

    Inventor： HOUGHTON, Michael ,  KINCAID, John

    IPC: A61K31/435 ,  A61K31/4353 ,  A61K31/437 ,  C07D471/00 ,  C07D471/02 ,  C07D471/04

    Abstract: The present disclosure provides processes for preparing a compound of formula (I) from a compound of formula (II) via two steps: 6a) contacting 2-(aminooxy)ethanol (i.e., formula (K)) or a salt thereof (e.g., formula (K-1)), with a base and a silylating agent to form a first mixture including an O-silyl protected compound of formula (K); and 6b) adding a second mixture including a compound of formula (II) or a salt therefore, to the first mixture of step 6a) to form the compound represented by formula (I): The present processes only utilize less than 1.5 equivalents of 2-(aminooxy)ethanol or the salt thereof relative to the compound of formula (II), and therefore reduce the burden to remove excess 2-(aminooxy)ethanol on a large manufacturing scale. Also provided are processes for preparing the compound of formula (K) or (K-1).

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