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    NOVEL ACYLATING REAGENTS
    31.
    发明申请
    NOVEL ACYLATING REAGENTS 审中-公开
    新型ACYLATING试剂

    公开(公告)号：WO2004043884A2

    公开(公告)日：2004-05-27

    申请号：PCT/US2003/035742

    申请日：2003-11-11

    申请人： ENZON PHARMACEUTICALS, INC.

    发明人： ZHAO, Hong ,  GREENWALD, Richard, B.

    IPC分类号： C07C

    CPC分类号： C07D309/14 ,  C07C69/96 ,  C07C205/43 ,  C07C251/24 ,  C07D207/404 ,  C07D309/12 ,  C07D405/04 ,  C07F7/1852 ,  C08G65/331

    摘要： Novel acylating agents useful for preparing activated nucleophiles such as terminally activated polymers are disclosed. In preferred aspects, the acylating agents are formula (I) and formula (II) and they used to prepare activated polymers such as PEG's for conjugating small molecules, proteins, polypeptides and the like.

    摘要翻译： 公开了用于制备活化的亲核试剂例如末端活化的聚合物的新型酰化剂。 在优选的方面，酰化剂是式（I）和式（II），它们用于制备活化的聚合物，例如用于缀合小分子，蛋白质，多肽等的PEG。

    CHEMOSENSITIZING AGENTS AGAINST CHLOROQUINE RESISTANT PLASMODIUM FALCIPARUM AND METHODS OF MAKING AND USING THEREOF
    34.
    发明申请
    CHEMOSENSITIZING AGENTS AGAINST CHLOROQUINE RESISTANT PLASMODIUM FALCIPARUM AND METHODS OF MAKING AND USING THEREOF 审中-公开
    化学抗性抗药剂及其制备方法及使用方法

    公开(公告)号：WO2002089810A1

    公开(公告)日：2002-11-14

    申请号：PCT/US2001/014574

    申请日：2001-05-07

    申请人： UNITED STATES ARMY MEDICAL RESEARCH AND MATERIEL COMMAND

    发明人： LIN, Ai, J. ,  GUAN, Jian ,  KYLE, Dennis, E. ,  MILHOUS, Wilbur, K.

    IPC分类号： A61K31/5415

    CPC分类号： C07D405/12 ,  C07D223/22 ,  C07D279/24 ,  C07D309/12 ,  C07D417/12

    摘要： A compound having the structural formula or a pharmaceutically acceptable salt or prodrug thereof, wherein X is a substituted or unsubstituted alkyl or a heteroatom; n is 4,5 or 6; Y is a substituted or unsubstituted alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, or wherein R 1 and R 2 are each independently, H, a heteroatom, substituted or unsubstituted alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; and wherein each ring structure are independently substituted or unsubstituted is disclosed. Also disclosed are chemosensitizing agents and methods of modulating, attenuating, reversing, or affecting a cell's or organism's resistance to a given drug such as an antimalarial.

    摘要翻译： 具有结构式的化合物或其药学上可接受的盐或前药，其中X是取代或未取代的烷基或杂原子; n为4,5或6; Y是取代或未取代的烷基，环烷基，杂环烷基，芳基，杂芳基，或其中R1和R2各自独立地是H，杂原子，取代或未取代的烷基，环烷基，杂环烷基，芳基或杂芳基; 并且其中每个环结构独立地被取代或未取代。 还公开了化学增敏剂和调节，减弱，逆转或影响细胞或生物体对给定药物如抗疟药的抗性的方法。

    ORGANIC COMPOUNDS
    37.
    发明申请
    ORGANIC COMPOUNDS 审中-公开
    有机化合物

    公开(公告)号：WO01036367A2

    公开(公告)日：2001-05-25

    申请号：PCT/EP2000/011471

    申请日：2000-11-17

    IPC分类号： C07C69/65 ,  C07D309/12 ,  C07C69/00

    CPC分类号： C07D309/12 ,  C07C69/65

    摘要： There are described new compounds of formula (I) wherein X is hydrogen, halogen, phenyl or C1-4alkyl; Y is fluorine or chlorine; A is -O-, -S- or -N(R1)-, wherein R1 is C1-4alkyl, phenylthio or tolylthio; n is from 1 to 12; m is from 2 to 6; R is hydrogen or one of groups (A) or (B) wherein Het is a saturated or unsaturated , 3- to 7-membered heterocyclic ring that optionally additionally comprises O or S as further hetero atom or the hetero group -N(C1-6alkyl)-; Aryl is phenyl or naphthyl; and R2, R3, R4, R5, R6, R7 and R8 are each independently of the others hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4haloalkyl, C2-6alkenyl, C2-6alkynyl, halogen, hydroxy, cyano, nitro, phenyl, amino, C1-4alkylamino, (C1-4alkyl)2amino, C1-4alkylsulfonyl or arylsulfonyl; in free form or in the form of physiologically tolerable salts. Also described are the preparation and use of such substances in the control of ectoparasites on domestic animals, productive livestock and pets, and ectoparasiticidal compositions for use on such animals.

    摘要翻译： 描述了新的式（I）化合物，其中X是氢，卤素，苯基或C 1-4烷基; Y是氟或氯; A是-O - ， - S-或-N（R 1） - ，其中R 1是C 1-4烷基，苯硫基或甲苯基硫基; n为1〜12; m为2〜6; R是氢或基团（A）或（B）中的一个，其中Het是饱和或不饱和的3-至7-元杂环，其任选地另外包含O或S作为另外的杂原子或杂基-N（C1- 1-6） - ; 芳基是苯基或萘基; 并且R 2，R 3，R 4，R 5，R 6，R 7和R 8各自独立地为氢，C 1-4烷基，C 1-4烷氧基，C 1-4烷硫基，C 1-4卤代烷基，C 2-6烯基，C 2-6炔基，卤素，羟基， 氰基，硝基，苯基，氨基，C 1-4烷基氨基，（C 1-4烷基）2氨基，C 1-4烷基磺酰基或芳基磺酰基; 游离形式或以生理上可耐受的盐的形式。 还描述了这些物质在家畜，生产性家畜和宠物中的外寄生物的控制和用于这些动物的杀寄生虫剂组合物的制备和应用。