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    O-substituted hydroxyaryl derivatives
    3.
    发明申请
    O-substituted hydroxyaryl derivatives 有权
    O-取代的羟基芳基衍生物

    公开(公告)号：US20060094718A1

    公开(公告)日：2006-05-04

    申请号：US10515622

    申请日：2003-06-05

    申请人： Susumu Muto ,  Akiko Itai

    发明人： Susumu Muto ,  Akiko Itai

    IPC分类号： A61K31/5377 ,  C07D413/02

    CPC分类号： C07D209/48 ,  C07D211/62 ,  C07D213/803 ,  C07D265/22 ,  C07D265/26 ,  C07D269/00 ,  C07D273/00 ,  C07D277/46 ,  C07D295/185 ,  C07D295/205 ,  C07D309/10 ,  C07D317/60 ,  C07K5/06052 ,  C07K5/06078 ,  C07K5/06086 ,  C07K5/06113 ,  C07K5/06191

    摘要： A medicament having inhibitory activity against NF-κB activation which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in a main chain is 2 to 5 (said connecting group may be substituted), “A” represents an acyl group which may be substituted, (provided that unsubstituted acetyl group and unsubstituted acryloyl group are excluded,) or a C1 to C6 alkyl group which may be substituted, or A may bind to connecting group X to form a cyclic structure which may be substituted, “E” represents an aryl group which may be substituted or a heteroaryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above.

    摘要翻译： 一种具有抑制NF-κB活化活性的药物，其特征在于，含有选自下述通式（I）表示的化合物及其药理学可接受的盐及其水合物及其溶剂合物作为活性成分的物质 ：其中X表示主链中的原子数为2〜5的连接基（所述连接基可以被取代），“A”表示可以被取代的酰基（条件是未取代的乙酰基和未取代的丙烯酰基 或者可以被取代的C 1〜C 6烷基，或者A可以与连接基团X结合形成可以被取代的环状结构， “E”表示可以被取代的芳基或可以被取代的杂芳基，环Z表示可以具有一个或多个取代基的芳族，除了由式-OA表示的基团之外，其中A具有相同的I 如上所定义的基团和由式-XE表示的基团，其中X和E各自具有与上述定义相同的含义，或除了由式-OA表示的基团之外可具有一个或多个取代基的杂芳烃，其中A 具有与上述相同的含义和由式-XE表示的基团，其中X和E各自具有与上述相同的含义。

    Novel synthesis of cyclic compounds
    4.
    发明授权
    Novel synthesis of cyclic compounds 失效
    环状化合物的新型合成

    公开(公告)号：US4996315A

    公开(公告)日：1991-02-26

    申请号：US465682

    申请日：1990-01-16

    申请人： George P. Speranza ,  Jiang-Jen Lin

    发明人： George P. Speranza ,  Jiang-Jen Lin

    IPC分类号： C07D269/00 ,  C07D273/01

    CPC分类号： C07D269/00

    摘要： Novel cyclic ester-amides having the formula: ##STR1## where R is an alkyl group having from 2 to 5 carbon atoms, and x ranges from 2 to 6 by reacting a polyethylene glycol monoamine having the formula NH.sub.2 --(CH.sub.2 CH.sub.2 O).sub.x --H, where x is as above, with at least one dicarboxylic acid, where the dicarboxylic acid is selected from the group consisting of glutaric, adipic, pimelic acids and mixtures thereof. The a molar ratio of polyethylene glycol monoamine to dicarboxylic acid should be about 1:1. Catalysts may be optionally used, and may include such compounds as titanium alkoxides; and zinc, manganese and antimony salts of carboxylic acids. This method is anticipated to be a useful step in a new preparation of valuable cyclic products.

    摘要翻译： 具有下式的新型环状酯 - 酰胺：其中R是具有2至5个碳原子的烷基，x在2-6范围内通过使具有式NH 2 - （CH 2 CH 2 O）x H的聚乙二醇单胺反应，其中 x是至少一种二羧酸，其中二羧酸选自戊二酸，己二酸，庚二酸及其混合物。 聚乙二醇单胺与二羧酸的摩尔比应为约1:1。 可以任选地使用催化剂，并且可以包括诸如烷氧基钛的化合物; 和羧酸的锌，锰和锑盐。 预计这种方法是有价值的循环产物的新制备中的有用步骤。

    NOVEL PROCESS FOR PREPARATION OF LINEZOLID AND ITS NOVEL INTERMEDIATES
    6.
    发明申请
    NOVEL PROCESS FOR PREPARATION OF LINEZOLID AND ITS NOVEL INTERMEDIATES 有权
    制备线粒体及其新型中间体的新方法

    公开(公告)号：US20130324719A1

    公开(公告)日：2013-12-05

    申请号：US13820568

    申请日：2012-02-21

    申请人： Raghu Mitra Alla ,  Ajay Kumar Dubey ,  Aruna Kumari Sirigiri ,  Naga Kama Kumar Mareedu

    发明人： Raghu Mitra Alla ,  Ajay Kumar Dubey ,  Aruna Kumari Sirigiri ,  Naga Kama Kumar Mareedu

    IPC分类号： C07D263/06

    CPC分类号： C07D263/06 ,  A61K31/5377 ,  C07D263/14 ,  C07D263/20 ,  C07D265/30 ,  C07D269/00 ,  C07D413/10

    摘要： A novel process for preparing oxazolidinone antibacterial agent Linezolid including key intermediates of oxazolidinones comprising: reacting 3-fluoro-4-morpholinyl aniline with R-epichlorohydrin; carbonylation to form oxazolidinone derivative; acetylation of (5R)-5-(chloromethyl)-3-(3-fluoro-4-morpholinophenyl-oxazolidin-2-one with sodium acetate to get novel intermediate; hydrolysis of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl acetate; mesylation of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methanol; reaction of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl methane sulphonate with potassium phthalimide; hydrolysis of (S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl phthalimide with hydrazine hydrate; acetylation of (S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl amine with acetic anhydride yields Linezolid in high yield.

    摘要翻译： 一种制备恶唑烷酮抗菌剂利奈唑胺的新方法，包括恶唑烷酮的关键中间体，包括：使3-氟-4-吗啉基苯胺与R-表氯醇反应; 羰基化形成恶唑烷酮衍生物; （5R）-5-（氯甲基）-3-（3-氟-4-吗啉代苯基 - 恶唑烷-2-酮与乙酸钠的乙酰化得到新的中间体;（R）-3-（3-氟-4- （R）-3-（3-氟-4-吗啉代苯基）-2-氧代-5-恶唑烷基甲醇的甲磺酰化;（R）-3-（ 3-（3-氟-4-吗啉代苯基）-2-氧代-5-恶唑烷基甲基甲磺酸盐与邻苯二甲酰亚胺钾的水解;（S）-3-（3-氟-4-吗啉代苯基）-2-氧代-5-恶唑烷基甲基邻苯二甲酰亚胺 与水合肼反应;（S）-3-（3-氟-4-吗啉代苯基）-2-氧代-5-恶唑烷基甲基胺与乙酸酐的乙酰化，以高产率得到利奈唑胺。

    Dibenzooxazepines and dibenzothiazepines
    9.
    发明授权
    Dibenzooxazepines and dibenzothiazepines 失效
    二苯并咪唑和二苯并噻吩

    公开(公告)号：US3723463A

    公开(公告)日：1973-03-27

    申请号：US3723463D

    申请日：1971-08-17

    申请人： SQUIBB & SONS INC

    发明人： YALE H ,  BERNSTEIN J

    IPC分类号： C07D267/18 ,  C07D267/20 ,  C07D267/22 ,  C07D269/00 ,  C07D281/12 ,  C07D283/00 ,  C07D403/06 ,  C07D93/42 ,  C07D93/44

    CPC分类号： C07D403/06 ,  C07D267/18 ,  C07D267/20 ,  C07D267/22 ,  C07D269/00 ,  C07D281/12 ,  C07D283/00

    摘要： WHEREIN R, R1 and R2 are hydrogen, lower alkyl, phenyl or phenyl-lower alkyl; R3 and R4 are hydrogen, halogen, lower alkyl, trifluoromethyl, or lower alkoxy; X is oxygen or sulfur, r is 2 to 5; m is 0 or 1; n and p are each 0, 1 or 2; provided that the sum of m + n + p being from 1 to 3, and that when m equals 1 and n and p are each O, X is sulfur.

    Therapeutically active compounds utilizable as ataractic agents and as sedatives and hypotensive agents having the formula

    摘要翻译： 可用作无定形剂的治疗活性化合物，以及作为镇静剂和降血糖剂，​​其具有式WHEREIN R，R 1和R 2是氢，低级烷基，苯基或苯基 - 低级烷基; R3和R4是氢，卤素，低级烷基，三氟甲基或低级烷氧基; X为氧或硫，r为2至5; m为0或1; n和p各自为0,1或2; 条件是m + n + p的总和为1至3，当m等于1且n和p各自为O时，X为硫。