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    HSV PRIMASE INHIBITORS
    43.
    发明申请
    HSV PRIMASE INHIBITORS 审中-公开

    公开(公告)号：WO0058270A2

    公开(公告)日：2000-10-05

    申请号：PCT/CA0000324

    申请日：2000-03-23

    申请人： BOEHRINGER INGELHEIM CA LTD ,  SIMONEAU BRUNO ,  LIUZZI MICHELE ,  MENTRUP ANTON

    发明人： SIMONEAU BRUNO ,  LIUZZI MICHELE ,  MENTRUP ANTON

    IPC分类号： C07D295/18 ,  A61K31/165 ,  A61K31/167 ,  A61K31/4402 ,  A61K31/4453 ,  A61K31/52 ,  A61K31/522 ,  A61K31/535 ,  A61P31/22 ,  C07C235/00 ,  C07C235/60 ,  C07C235/62 ,  C07C235/64 ,  C07C237/30 ,  C07C237/38 ,  C07C237/40 ,  C07C237/42 ,  C07C237/44 ,  C07C247/18 ,  C07D213/30 ,  C07D213/40 ,  C07D295/192

    CPC分类号： C07D295/192 ,  A61K31/52 ,  A61K31/535 ,  C07C235/64 ,  C07C237/30 ,  C07C237/38 ,  C07C237/40 ,  C07C237/44 ,  C07C247/18 ,  C07C2601/14 ,  C07D213/30 ,  C07D213/40 ,  A61K2300/00

    摘要： The invention provides compounds of formula (1) that are active against the HSV primase enzyme: wherein R1 is hydroxy or amino; R2 is hydrogen, halo, (C1-4)alkyl or (C1-4)alkoxy; R3 is hydrogen, halo, (C1-4)alkyl, (C1-4)alkoxy, amino or azido; R4 has the same significance as R2; R5 is hydrogen or (C1-4)alkyl; and R is (C1-7)alkyl, (C3-6)cycloalkyl, {phenyl(C1-7)alkyl}, {phenyl(C1-7)alkoxy}, {{(monocyclic heterocyclo)-{(C1-7)alkoxy}}, CH(W)C(O){O-(C1-4)alkyl} wherein W is hydrogen or (C1-7)alkyl, or (A) wherein Y is hydrogen or (C1-7)alkyl, and Z is (C1-7)alkyl, (C3-6) cycloalkyl, {(C3-6)cycloalkyl}-{(C1-7)alkyl}, phenyl(C1-7)alkyl or {{(monocyclic heterocyclo)-{(C1-7)alkyl}}, or Y and Z together with the nitrogen atom to which they are attached represent, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl or 1-(4-methylpiperazinyl); with the provisos that (1) when R is CH(W)C(O)-{O-(C1-4)alkyl} as defined herein, then R5 is hydrogen; and (2) at least one of R2, R3 and R4 is other than hydrogen.

    摘要翻译： 本发明提供对HSV引物酶具有活性的式（1）化合物：其中R1是羟基或氨基; R2是氢，卤素，（C1-4）烷基或（C1-4）烷氧基; R3是氢，卤素，（C1-4）烷基，（C1-4）烷氧基，氨基或叠氮基; R4与R2具有相同的意义; R5是氢或（C1-4）烷基; （C 1-7）烷基，（C 3-6）烷基}，{苯基（C 1-7）烷氧基}，{（（单环杂环） - {（C 1-7） 烷氧基}}，CH（W）C（O）{O-（C1-4）烷基}其中W是氢或（C1-7）烷基，或（A）其中Y是氢或（C1-7）烷基， 并且Z是（C 1-7）烷基，（C 3-6）环烷基，{（C 3-6）环烷基} - {（C 1-7）烷基}，苯基（C 1-7）烷基或{{（单环杂环） {（C 1-7）烷基}}或Y和Z与它们所连接的氮原子一起代表1-吡咯烷基，1-哌啶基，4-吗啉基或1-（4-甲基哌嗪基） 条件是（1）当R是本文定义的CH（W）C（O） - {O-（C 1-4）烷基}时，则R 5是氢; 和（2）R2，R3和R4中的至少一个不是氢。

    METHOD OF PRODUCING NANOPARTICLE SUSPENSIONS
    49.
    发明申请
    METHOD OF PRODUCING NANOPARTICLE SUSPENSIONS 审中-公开
    制备纳米悬浮液的方法

    公开(公告)号：WO2011110990A1

    公开(公告)日：2011-09-15

    申请号：PCT/IB2011/050942

    申请日：2011-03-07

    申请人： BASF SE ,  BASF (CHINA) COMPANY LIMITED ,  ENGEL, Robert ,  GERLINGER, Wolfgang ,  BRÄSE, Stefan ,  MULLER, Thierry ,  BELENKI, Christina ,  SCHUCHMANN, Heike ,  GEDRAT, Marion

    发明人： ENGEL, Robert ,  GERLINGER, Wolfgang ,  BRÄSE, Stefan ,  MULLER, Thierry ,  BELENKI, Christina ,  SCHUCHMANN, Heike ,  GEDRAT, Marion

    IPC分类号： B01J13/02 ,  B01F17/00 ,  C07C69/36 ,  C07C69/38 ,  C07C55/06 ,  C07C55/08 ,  C07C271/08 ,  C07C235/00

    CPC分类号： C07C271/08 ,  B01F17/0007 ,  B01F17/0021 ,  C07C69/36 ,  C07C69/38 ,  C07C233/56

    摘要： Method of producing a nanoparticle suspension with the steps (i) preparation of an emulsion of a disperse polar phase, where the aqueous phase comprises one or more precursor substances forming the nanoparticles, in a continuous organic phase in the presence of an emulsifier stabilizing the emulsion, (ii) conversion of the one or more precursor substances to nanoparticles in the disperse aqueous phase, (iii) breaking of the emulsion and phase separation, where the nanoparticle suspension is obtained as one phase, (iv) separation off of the nanoparticle suspension, (v) optionally isolation of the nanoparticles from the nanoparticle suspension, wherein the emulsifier is selected from compounds of the general formula (I) in which X is O, NH, Y is C(O), NH, R is a saturated or a mono- or polyunsaturated, linear or branched hydrocarbon radical having 6 to 30 carbon atoms and R 1 is hydrogen or C 1 -C 4 -alkyl, and R 2 is a saturated or a mono- or polyunsaturated, linear or branched hydrocarbon radical having 1 to 30 carbon atoms, preferably 6 to 30 carbon atoms, R 3 is C 1 -C 4 -alkyl, n is 0 or 1, and the breaking of the emulsion is effected by splitting the emulsifier.

    摘要翻译： 制备纳米颗粒悬浮液的方法，步骤（i）在稳定乳液的乳化剂存在下，在连续的有机相中，制备分散极性相的乳液，其中水相包含一种或多种形成纳米颗粒的前体物质 ，（ii）将一种或多种前体物质转化为分散水相中的纳米颗粒，（iii）破乳和相分离，其中纳米颗粒悬浮液作为一相获得，（iv）将纳米颗粒悬浮液分离 ，（v）任选地从纳米颗粒悬浮液中分离纳米颗粒，其中所述乳化剂选自X为O，NH，Y为C（O），NH，R为饱和的或通式 具有6至30个碳原子的单或多不饱和的直链或支链烃基，R 1是氢或C 1 -C 4 - 烷基，R 2是饱和的或单不饱和的或不饱和的，直链或支链的烃基 具有1至30个碳原子，优选6至30个碳原子的二烷基，R 3是C 1 -C 4 - 烷基，n是0或1，并且通过分裂乳化剂来实现乳液的断裂。

    Histone Deacetylase Inhibitors
    50.
    发明申请
    Histone Deacetylase Inhibitors 审中-公开
    组蛋白脱乙酰酶抑制剂

    公开(公告)号：WO2007095584A3

    公开(公告)日：2009-05-22

    申请号：PCT/US2007062152

    申请日：2007-02-14

    申请人： HARVARD COLLEGE ,  DANA FARBER CANCER INST INC ,  BRADNER JAMES ELLIOT ,  MAZITSCHEK RALPH

    发明人： BRADNER JAMES ELLIOT ,  MAZITSCHEK RALPH

    IPC分类号： C07C309/00 ,  C07C233/00 ,  C07C235/00 ,  C07C327/00

    CPC分类号： A61K31/231 ,  A61K9/0014 ,  A61K31/165 ,  A61K31/337 ,  C07C235/78 ,  C07C259/06 ,  C07D319/06 ,  C07D413/12

    摘要： In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for exmaple. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.

    摘要翻译： 鉴于需要开发新的治疗剂，本发明提供了新的组蛋白脱乙酰酶抑制剂。 这些化合物包括酯键，使它们对酯酶的失活敏感。 因此，这些化合物特别可用于治疗皮肤病。 当化合物达到血流时，酯酶或具有酯酶活性的酶将化合物切割成具有大大降低的活性的生物活性片段或片段。理想地，这些降解产物表现出短的血清和/或全身半衰期并被快速消除。 这些化合物及其药物组合物特别可用于治疗皮肤T细胞淋巴瘤，神经纤维瘤病，牛皮癣，脱发，皮肤色素沉着和皮炎。 本发明还提供了制备本发明化合物及其中间体的方法。