CHELATING AGENTS
    4.
    发明申请
    CHELATING AGENTS 审中-公开
    焊接剂

    公开(公告)号:WO9846276A8

    公开(公告)日:1999-07-22

    申请号:PCT/GB9801078

    申请日:1998-04-14

    CPC classification number: A61K49/103 A61K49/04 A61K51/0478

    Abstract: The invention provides a complexant compound of formula (I): R S(CR 2)nN(R )i(CR 2)nX(CR 2)nN(R )i(CR 2)nSR , (wherein each n, which may be the same or different, is an integer 2, 3 or 4 (preferably 2); each i, which may be the same or different, represents 0 or 1; each R , which may be the same or different, is H or a thiol protecting group, preferably a protecting group; X is O, S, N, NR or a substituted phosphorus (e.g. oxo substituted phosphorus), preferably S or N; each R , which may be the same or different, is hydrogen or an optionally substituted organic group; each R , which may be the same or different, is hydrogen or an optionally substituted organic group; each R , which may be the same or different, is hydrogen or an optionally substituted organic group, or a moiety CR 2 may represent a carbonyl group or two, three or four R S on two different carbons together with those carbons and any intervening atoms may represent an optionally substituted saturated or unsaturated homocyclic or heterocyclic ring; and preferably, at least one CR 2 moiety is other than CH2 or CH(CH3)) or a salt or complex thereof, wherein optionally at least one of the R , R , R and R moieties is coupled directly or indirectly to a vector moiety.

    Abstract translation: 本发明提供式(I)的络合物:R 3 S(CR 1)n N(R 2)i(CR 1)n X(CR 1)n N(R 2)n(CR 1)nSR 3(其中每个n可以相同或不同,为整数2,3或4(优选2);每个i可以是 相同或不同,表示0或1;每个R 3可以相同或不同,为H或硫醇保护基,优选保护基; X为O,S,N,NR 4或 取代的磷(例如氧取代的磷),优选S或N;每个R 4可以相同或不同,是氢或任选取代的有机基团;每个R 2可以相同或不同 是氢或任选取代的有机基团;每个R 1可以相同或不同,为氢或任选取代的有机基团,或部分CR 1可以表示羰基或二,三 或两个不同碳上的四个R 1与这些碳原子一起形成,任何插入的原子可以代表任选的取代基 饱和或不饱和的杂环或杂环; 并且优选地,至少一个CR 1 2部分不是CH 2或CH(CH 3))或其盐或络合物,其中任选地R 1,R 2,R 3, 和R 4部分直接或间接连接到载体部分。

    HETEROCYCLIC CATIONIC LIPIDS
    5.
    发明申请
    HETEROCYCLIC CATIONIC LIPIDS 审中-公开
    杂环阳离子脂

    公开(公告)号:WO99025342A1

    公开(公告)日:1999-05-27

    申请号:PCT/US1998/024340

    申请日:1998-11-13

    CPC classification number: C07D233/22 C07D233/24

    Abstract: Compounds of formula (I) are provided, in which R and R each independently represents a C8-C24 saturated or unsaturated hydrocarbon chain, which is optionally interrupted by form 1 to 3 heteroatom moieties, such as -O-, -S-, -NH- and -NR-. The symbol X represents -CH2-, -O-, -S-, -NH- or -NR-. The R group for each of the -NR- moieties represents an alkyl group having form 1 to 4 carbon atoms. Finally, the subscript n represents the integer 1 or 2, and A- represents an anion, preferably chloride or citrate.

    Abstract translation: 提供式(I)化合物,其中R 1和R 2各自独立地表示C 8 -C 24饱和或不饱和烃链,其任选地被1至3个杂原子部分例如-O- ,-S-,-NH-和-NR-。 符号X表示-CH 2 - , - O - , - S - , - NH-或-NR-。 每个-NR-部分的R基表示具有1至4个碳原子的烷基。 最后,下标n表示1或2的整数,A-表示阴离子,优选为氯化物或柠檬酸盐。

    PROCESS FOR THE PREPARATION OF AMPHIPHILIC IMIDAZOLINIUM COMPOUNDS
    6.
    发明申请
    PROCESS FOR THE PREPARATION OF AMPHIPHILIC IMIDAZOLINIUM COMPOUNDS 审中-公开
    制备咪唑烷酮化合物的方法

    公开(公告)号:WO2016177693A1

    公开(公告)日:2016-11-10

    申请号:PCT/EP2016/059823

    申请日:2016-05-03

    CPC classification number: C07D233/14

    Abstract: The present invention generally relates to improved processes for the preparation of amphiphilic imidazolinium compounds such as 1-[2-(9(Z)-octadecenoyloxy)ethy1]-2-(8(Z)-heptadecenyl)-3-(2-hydroxyethyl)imidazolinium chloride (DOTIM). In particular, the invention relates to processes for the synthesis of such compounds that avoid the need for toxic reagents, are more economical, and result in less waste than conventional methods. DOTIM and similar compounds can be formulated as cationic liposomes, which are useful as chemical vectors for nucleic acid delivery in gene therapy.

    Abstract translation: 本发明一般涉及制备两亲咪唑啉鎓化合物的改进方法,例如1- [2-(9(Z) - 十八烯酰氧基)乙基] -2-(8(Z) - 十六碳烯基)-3-(2-羟基乙基 )咪唑啉氯化物(DOTIM)。 特别地,本发明涉及合成这种化合物的方法,其避免了对有毒试剂的需要,更经济,并且比常规方法减少了浪费。 DOTIM和类似化合物可以配制成阳离子脂质体,其可用作基因治疗中核酸递送的化学载体。

    SUBSTITUTED IMIDAZOLINE COMPOUNDS
    7.
    发明申请
    SUBSTITUTED IMIDAZOLINE COMPOUNDS 审中-公开
    取代的咪唑啉化合物

    公开(公告)号:WO2009048586A1

    公开(公告)日:2009-04-16

    申请号:PCT/US2008/011606

    申请日:2008-10-09

    CPC classification number: C07D233/28

    Abstract: The invention relates to compositions comprising substituted imidazoline compounds including prodrugs, and salts thereof. In some embodiments, the invention relates to the use of these compositions as therapeutic agents, preferably for the treatment of arthritis or cancer. In further embodiments, The invention relates to the pharmaceutical compositions with effective amounts of substituted imidazoline compounds disclosed herein that function as agonist or antagonists of the genetic expression or interactions with transcription factor NF-κB.

    Abstract translation: 本发明涉及包含取代的咪唑啉化合物(包括前药)及其盐的组合物。 在一些实施方案中,本发明涉及这些组合物作为治疗剂的用途,优选用于治疗关节炎或癌症。 在进一步的实施方案中,本发明涉及具有有效量的本文公开的取代的咪唑啉化合物的药物组合物,其作为基因表达的激动剂或拮抗剂或与转录因子NF-κB的相互作用。

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