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    PREPARATION OF DELMOPINOL
    3.
    发明申请
    PREPARATION OF DELMOPINOL 审中-公开
    DELMOPINOL的制备

    公开(公告)号：WO2007091009A2

    公开(公告)日：2007-08-16

    申请号：PCT/GB2007/000053

    申请日：2007-01-10

    Applicant: SINCLAIR PHARMACEUTICALS LIMITED ,  COMELY, Alexander ,  JANE, Llorenç, Rafecas ,  TESSON, Nicolas ,  ESCALE, Atoni, Riera

    Inventor： COMELY, Alexander ,  JANE, Llorenç, Rafecas ,  TESSON, Nicolas ,  ESCALE, Atoni, Riera

    IPC: C07D263/06 ,  C07D265/08 ,  C07D309/04 ,  C07C11/02 ,  C07C19/075 ,  C07C43/04

    CPC classification number: C07D263/06 ,  C07C11/02 ,  C07C17/16 ,  C07C19/075 ,  C07D265/08 ,  C07D309/04

    Abstract: It comprises a process for the production of delmopinol or a pharmaceutically acceptable salt and/or a solvate thereof, by subjecting the compound of formula (II) where R1 and R2 are the same or different, independently selected from the group consisting of H, (C1-C6) alkyl or, alternatively, R1 and R2 form, together with the carbon atom to which they are attached, a (C5-C6) cycloalkyl radical; and R3 is a radical selected from the group consisting of CF3, (C1-C4) alkyl, phenyl, and phenyl mono- ordisubstituted by a radical selected from the group consisting of (C1-C4)-alkyl, halogen and nitro to a deprotection and cyclisation reaction. The process is useful to prepare delmopinol or its salts on an industrial scale. The compound of formula (II) is new and also forms part of the present invention, as well as its preparation process and other new intermediates of said preparation process. .

    Abstract translation: 其包括通过使式（II）化合物（其中R 1和R 2相同或不同）独立选择来制备地莫匹醇或其药学上可接受的盐和/或其溶剂化物的方法 选自H，（C 1 -C 6）烷基或可选地，R 1和R 2与它们所连接的碳原子一起形成（C 5 -C 6）环烷基; 和R3是选自CF3，（C1-C4）烷基，苯基和被选自（C1-C4） - 烷基，卤素和硝基的基团单取代的苯基的基团进行脱保护 和环化反应。 该工艺在工业规模上用于制备地莫匹醇或其盐。 式（II）化合物是新的并且也构成本发明的一部分，以及其制备方法和所述制备方法的其它新中间体。

    POLYOXAZOLINE POLYMERS AND METHODS FOR THEIR PREPARATION, CONJUGATES OF THESE POLYMERS AND MEDICAL USES THEREOF
    5.
    发明申请
    POLYOXAZOLINE POLYMERS AND METHODS FOR THEIR PREPARATION, CONJUGATES OF THESE POLYMERS AND MEDICAL USES THEREOF 审中-公开
    聚氧乙烯聚合物及其制备方法，这些聚合物的结合及其医疗用途

    公开(公告)号：WO2013103297A1

    公开(公告)日：2013-07-11

    申请号：PCT/NL2012/050933

    申请日：2012-12-28

    Applicant: UNIVERSITEIT GENT ,  BENDER ANALYTICAL HOLDING B.V.

    Inventor： HOOGENBOOM, Richard

    IPC: C08G73/02 ,  A61K47/34 ,  A61K47/48 ,  C08L79/02 ,  C07D263/10 ,  C07D265/08

    CPC classification number: A61K47/48192 ,  A61K47/34 ,  A61K47/50 ,  A61K47/51 ,  A61K47/56 ,  A61K47/59 ,  A61K47/64 ,  A61K51/06 ,  A61K51/065 ,  C08G73/0233 ,  C08L79/02

    Abstract: The present invention relates to functionalized ploy(2-oxazoline) polymers, which are very suitable as a carrier and/or delivery vehicle (conjugate) of drugs, such as small therapeutic molecules and bio-pharmaceuticals. These polymers are characterized in that they comprise repeating units that are represented by the following formula -[N(R 1 )-(CHR 2 )m]- wherein R 1 is R 3 -(CHR 4 )n-CONH-R 5 ; R 2 is selectd from H and optionally substituted C 1-5 alkyl; R 3 is CH 2 CO, C(O)O, C(O)NH OR C(S)NH; R 4 is selected from H and optionally substituted C 1-5 alkyl; R 5 is H; an C 1-5 alkyl; aryl; or a moiety comprising a functional group that can be used for conjugation; m is 2 or 3 and n is 1-5; or n is 0 and R 3 is CH 2 . The invention relates further to a conjugate of these polyoxazoline polymers with at least one active moiety, such as a therapeutic moiety, a targeting moiety and/or diagnostic moiety, and to the use of these conjugates in the therapeutic treatment or prophylactic treatment or diagnosis of a disease or disorder.

    Abstract translation: 本发明涉及非常适合作为药物如小的治疗分子和生物药物的载体和/或递送载体（缀合物）的官能化的（2-恶唑啉）聚合物。 这些聚合物的特征在于它们包含由下式表示的重复单元 - [N（R1） - （CHR2）m] - ，其中R1是R3-（CHR4）n-CONH-R5; R2选自H和任选取代的C 1-5烷基; R 3是CH 2 CO，C（O）O，C（O）NH OR C（S）NH; R4选自H和任选取代的C 1-5烷基; R5is H; C 1-5烷基; 芳基; 或包含可用于缀合的官能团的部分; m为2或3，n为1-5; 或n为0且R 3为CH 2。 本发明还涉及这些聚恶唑啉聚合物与至少一个活性部分（例如治疗部分，靶向部分和/或诊断部分）的缀合物，以及这些缀合物在治疗性或预防性治疗或诊断中的用途 疾病或病症

    ARTHROPODICIDAL OXAZINES AND THIAZINES
    10.
    发明申请
    ARTHROPODICIDAL OXAZINES AND THIAZINES 审中-公开
    抗坏血酸氧化酶和噻唑

    公开(公告)号：WO1996022286A2

    公开(公告)日：1996-07-25

    申请号：PCT/US1996000441

    申请日：1996-01-11

    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY ,  LONG, Jeffrey, Keith ,  STEVENSON, Thomas, Martin

    Inventor： E.I. DU PONT DE NEMOURS AND COMPANY

    IPC: C07D265/08

    CPC classification number: C07D413/04 ,  C07D265/08 ,  C07D279/06 ,  C07F7/0812

    Abstract: Compounds of formula (I), and their N-oxides and agriculturally-suitable salts, are disclosed which are useful as arthropodicides wherein: A is selected from the group direct bond, C1-C3 alkylene and C2-C4 alkenylene; Q is selected from the group phenyl, pyridyl, thienyl, furyl and naphthyl, each ring substituted with R , R and R ; each E is independently selected from the group C1-C4 alkyl and C1-C4 haloalkyl; Z is selected from the group O and S; R and R are independently selected from the group H, 1-2 halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, CN and NO2; q is 0, 1, 2 or 3; and R , R and R are as defined in the disclosure. Also disclosed are compositions containing the compounds of formula (I) and a method for controlling arthropods which involves contacting the arthropods or their environment with an effective amount of a compound of formula (I).

    Abstract translation: 公开了式（I）化合物及其N-氧化物和农业上合适的盐，其可用作节肢动物剂，其中：A选自直接键，C1-C3亚烷基和C2-C4亚烯基; Q选自苯基，吡啶基，噻吩基，呋喃基和萘基，每个环被R 3，R 4和R 5取代; 每个E独立地选自C 1 -C 4烷基和C 1 -C 4卤代烷基; Z选自O和S组; R 1和R 2独立地选自H，1-2卤素，C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷氧基，C 1 -C 6卤代烷氧基，C 1 -C 6烷硫基，CN和NO 2 ; q为0,1,2或3; R 3，R 4和R 5如本公开所定义。 还公开了含有式（I）化合物的组合物和控制节肢动物的方法，其包括将节肢动物或其环境与有效量的式（I）化合物接触。

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