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192 条记录 (耗时 0.037 秒)

    Crystal of a benzoxazinone compound
    7.
    发明授权
    Crystal of a benzoxazinone compound 有权
    苯并恶嗪酮化合物的晶体

    公开(公告)号：US08883780B2

    公开(公告)日：2014-11-11

    申请号：US13265599

    申请日：2010-04-22

    申请人： Edwin Aret

    发明人： Edwin Aret

    IPC分类号： C07D265/26 ,  A61K31/536

    CPC分类号： C07D265/26 ,  A61K31/536

    摘要： Disclosed is a crystal of 2-(hexadecyloxy)-6-methyl-4H-3,1-benzoxazin-4-one useful as a preventive or therapeutic agent for obesity and the like. Specifically disclosed is a crystal of 2-(hexadecyloxy)-6-methyl-4H-3,1-benzoxazin-4-one having a powder X-ray diffraction pattern in which characteristic peaks appear at powder X-ray diffraction interplanar spacings (d) of around 16.54±0.2, 13.26±0.2, 4.70±0.2, 4.38±0.2, and 3.67±0.2λ.

    摘要翻译： 公开了可用作肥胖症等的预防或治疗剂的2-（十六烷氧基）-6-甲基-4H-3,1-苯并恶嗪-4-酮的结晶。 具体公开了具有粉末X射线衍射图的2-（十六烷氧基）-6-甲基-4H-3,1-苯并恶嗪-4-酮的晶体，其中在粉末X射线衍射面间距（d ）为16.54±0.2,13.26±0.2,4.70±0.2,4.38±0.2和3.67±0.2λ。

    2-oxy-benzoxazinone derivatives for the treatment of obesity
    8.
    发明授权
    2-oxy-benzoxazinone derivatives for the treatment of obesity 有权
    2-氧基 - 苯并嗪酮衍生物用于治疗肥胖症

    公开(公告)号：US08877750B2

    公开(公告)日：2014-11-04

    申请号：US12952972

    申请日：2010-11-23

    申请人： Harold Francis Hodson ,  Robert Downham ,  Timothy John Mitchell ,  Beverley Jane Carr ,  Christopher Robert Dunk ,  Richard Michael John Palmer

    发明人： Harold Francis Hodson ,  Robert Downham ,  Timothy John Mitchell ,  Beverley Jane Carr ,  Christopher Robert Dunk ,  Richard Michael John Palmer

    IPC分类号： A61K31/535 ,  C07D265/26 ,  C07C271/28

    CPC分类号： C07D265/26 ,  C07C271/28

    摘要： The use of a compound comprising formula (I): or a salt, ester, amide or prodrug thereof in the inhibition of an enzyme whose preferred mode of action is to catalyse the hydrolysis of an ester functionality, e.g. in the control and inhibition of unwanted enzymes in products and processes. The compounds are also useful in medicine e.g. in the treatment of obesity and related conditions. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them. In formula (I) A is a 6-membered aromatic or heteroaromatic ring; and R1 is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative of any of the foregoing groups.

    摘要翻译： 包含式（I）的化合物或其盐，酯，酰胺或前药在抑制其优选作用模式是催化酯官能团水解的酶的用途，例如， 在产品和过程中控制和抑制不需要的酶。 这些化合物也可用于医学，例如 在治疗肥胖和相关情况。 本发明还涉及式（I）中的新化合物，其制备方法和含有它们的药物组合物。 在式（I）中，A是6元芳族或杂芳族环; 烯基，炔基，环烷基，环烯基，芳基，芳基烷基，还原芳基烷基，芳基烯基，杂芳基，杂芳基烷基，杂芳基烯基，还原芳基，还原杂芳基，还原的杂芳基烷基（可以被一个或多个氧原子间隔的烷基） 或任何上述基团的取代衍生物。

    Process for Making 3-Substituted 2-Amino-5-Halobenzamides
    10.
    发明申请
    Process for Making 3-Substituted 2-Amino-5-Halobenzamides 有权
    3-取代的2-氨基-5-卤代苯甲酰胺的制备方法

    公开(公告)号：US20090306372A1

    公开(公告)日：2009-12-10

    申请号：US12373651

    申请日：2007-06-27

    申请人： Richard F. Davis ,  Rafael Shapiro ,  Eric G. Taylor

    发明人： Richard F. Davis ,  Rafael Shapiro ,  Eric G. Taylor

    IPC分类号： C07C231/10 ,  C07D265/26 ,  C07D401/04 ,  C07D231/20 ,  C07D231/14 ,  C07C271/06 ,  C07C271/10

    CPC分类号： C07D401/04 ,  C07C231/02 ,  C07C271/28 ,  C07D231/16 ,  C07D265/26 ,  C07C237/30

    摘要： Disclosed is a method for preparing a compound of Formula 1 by contacting compound of Formula 2 with R1—NH2 in the presence of a carboxylic acid and a method for preparing a compound of Formula 2 by contacting a compound of Formula 4 with phosphorus tribromide. wherein R1 is H, C1-C4 alkyl, cyclopropyl, cyclopropylmethyl or methylcyclopropyl; R2 is CH3 or Cl; R3 is C1-C6 alkyl or C3-C6 alkenyl, each optionally substituted with up to 3 halogen and up to 1 phenyl; and X is Cl or Br. Also disclosed is a method for preparing a compound of Formula 5 wherein R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 that is characterized by preparing the compound of Formula 1 by the method above.

    摘要翻译： 公开了通过在羧酸存在下使式2的化合物与R 1 -NH 2接触来制备式1化合物的方法和通过使式4的化合物与三溴化磷接触来制备式2的化合物的方法。 其中R1是H，C1-C4烷基，环丙基，环丙基甲基或甲基环丙基; R2是CH3或Cl; R 3是C 1 -C 6烷基或C 3 -C 6烯基，各自任选被至多3个卤素和至多1个苯基取代; X为Cl或Br。 还公开了制备式5化合物的方法，其中R 4，R 5，R 6和Z如本公开所定义，使用式1化合物，其特征在于通过上述方法制备式1化合物。