Chiral catalysts for reduction of ketones and process for their
preparation
    2.
    发明授权
    Chiral catalysts for reduction of ketones and process for their preparation 失效
    用于还原酮的手性催化剂及其制备方法

    公开(公告)号:US5264585A

    公开(公告)日:1993-11-23

    申请号:US966658

    申请日:1992-10-26

    CPC classification number: C07D207/08 C07D495/04 C07F5/025

    Abstract: The chiral catalyst of general structure 1, or its enantiomer ##STR1## is prepared by treating the corresponding N-carboxy anhydride of structure 2 ##STR2## with an aryl metal, especially a phenyl metal such as an aryl magnesium halide, aryl lithium, aryl zinc or aryl cesium, to form a 1,1-diaryl- methanol of structure 3 ##STR3## followed by treatment with a compound of structure, 4 ##STR4## The catalyst, wherein R is aromatic, is novel and in some cases superior to the catalyst wherein R is alkyl or aralkyl in directing the chirality of diborane, borane-dimethyl sulfide or borane-tetrahydrofuran reductions of ketones to secondary alcohols.

    Abstract translation: 一般结构1或其对映异构体1的手性催化剂通过用芳基金属,特别是苯基金属如芳基卤化镁,芳基锂处理结构2的相应N-羧酸酐来制备 ,芳基锌或芳基铯,以形成结构3的1,1-二芳基 - 甲醇3,然后用结构化合物4处理。其中R是芳族的催化剂是新颖的,并且在 一些情况优于催化剂,其中R是烷基或芳烷基,用于指导乙硼烷,硼烷 - 二甲基硫醚或甲硼烷 - 四氢呋喃减少酮对仲醇的手性。

    Preparation of Lipid Nanoparticles
    4.
    发明申请
    Preparation of Lipid Nanoparticles 审中-公开
    脂质纳米颗粒的制备

    公开(公告)号:US20130037977A1

    公开(公告)日:2013-02-14

    申请号:US13639628

    申请日:2011-04-07

    CPC classification number: A61K9/1271 A61K9/127 A61K9/1272 A61K9/1277

    Abstract: The present invention provides a process for producing lipid nanoparticles encapsulating therapeutic products, said process comprising: a) providing one or more aqueous solutions in one or more reservoirs; b) providing one or more organic solutions in one or more reservoirs, wherein one or more of the organic solutions contains a lipid and wherein one or more of the aqueous solutions and/or one or more of the organic solutions includes therapeutic products; c) mixing said one or more aqueous solutions with said one or more organic solutions in a first mixing region, wherein said first mixing region is a Multi-Inlet Vortex Mixer (MIVM), wherein said one or more aqueous solutions and said one or more organic solutions are introduced tangentially into a mixing chamber within the MIVM so as to substantially instantaneously produce a lipid nanoparticle solution containing lipid nanoparticles encapsulating therapeutic products.

    Abstract translation: 本发明提供了一种制备包封治疗产品的脂质纳米颗粒的方法,所述方法包括:a)在一个或多个储存器中提供一种或多种水溶液; b)在一个或多个储存器中提供一种或多种有机溶液,其中一种或多种有机溶液含有脂质,并且其中一种或多种水溶液和/或一种或多种有机溶液包括治疗产品; c)在第一混合区域中将所述一种或多种水溶液与所述一种或多种有机溶液混合,其中所述第一混合区域是多入口涡旋混合器(MIVM),其中所述一种或多种水溶液和所述一种或多种 将有机溶液切向引入MIVM内的混合室中,从而基本上即时产生含有包封治疗产品的脂质纳米颗粒的脂质纳米颗粒溶液。

    Synthesis of hydroxysulfone and related compounds
    5.
    发明授权
    Synthesis of hydroxysulfone and related compounds 失效
    羟基砜及相关化合物的合成

    公开(公告)号:US5760249A

    公开(公告)日:1998-06-02

    申请号:US704195

    申请日:1996-08-28

    CPC classification number: C07D495/04

    Abstract: This invention is concerned with an improved process for the synthesis of hydroxysulfone, which is a key intermediate in the synthesis of carbonic anhydrase inhibitors, especially dorzolamide. Carbonic anhydrase inhibitors are known to be effective in treating elevated intraocular pressure or glaucoma.

    Abstract translation: 本发明涉及合成羟基砜的改进方法,羟基砜是合成碳酸酐酶抑制剂,特别是多佐胺的关键中间体。 已知碳酸酐酶抑制剂在治疗眼压升高或青光眼方面是有效的。

    Process of synthesizing N-acyl auxiliaries
    6.
    发明授权
    Process of synthesizing N-acyl auxiliaries 失效
    合成N-酰基助剂的方法

    公开(公告)号:US5594134A

    公开(公告)日:1997-01-14

    申请号:US414541

    申请日:1995-03-31

    CPC classification number: C07D201/02

    Abstract: A process of synthesizing N-acyl auxiliary compounds is disclosed. A compound of the formula: ##STR1## is reacted with an anhydride in the presence of a lithium salt and an amine base to produce the N-acylated auxiliary.

    Abstract translation: 公开了合成N-酰基辅助化合物的方法。 在锂盐和胺碱的存在下,使下式的化合物与一种酸酐反应得到N-酰化的辅助物。

    Pyridyl ethylation of lactam derivatives
    9.
    发明授权
    Pyridyl ethylation of lactam derivatives 失效
    内酰胺衍生物的吡啶基乙基化

    公开(公告)号:US5686607A

    公开(公告)日:1997-11-11

    申请号:US702486

    申请日:1996-08-29

    CPC classification number: C07D401/06

    Abstract: The invention is a highly efficient synthesis for making compounds of formula (iv) wherein R is C.sub.1-4 alkyl or benzyl; and R.sup.1, when present, is C.sub.1-4 alkyl, OH, O--C.sub.1-4 alkyl, or S--C.sub.1-4 alkyl; which are useful intermediates for making compounds such as those represented in formula (I). ##STR1##

    Abstract translation: PCT No.PCT / US94 / 10518 Sec。 371日期:1996年8月29日 102(e)日期1996年8月29日PCT 1994年9月16日PCT公布。 WO95 / 25088 PCT公开 日期1995年9月21日本发明是制备其中R为C 1-4烷基或苄基的式(ⅳ)化合物的高效合成; 当存在时,R 1为C 1-4烷基,OH,O-C 1-4烷基或S-C 1-4烷基; 它们是用于制备化合物如式(I)中所示的那些的有用的中间体。 (iv)(I)

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