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    Quinazolinone Derivatives Useful as Vanilloid Antagonists
    2.
    发明申请
    Quinazolinone Derivatives Useful as Vanilloid Antagonists 有权
    喹唑啉酮衍生物作为香草素拮抗剂有用

    公开(公告)号：US20100197705A1

    公开(公告)日：2010-08-05

    申请号：US12683317

    申请日：2010-01-06

    Applicant: Weichun Chen ,  Hong-Yong Kim ,  Jessica Liang ,  Michael Mutz ,  Mahavir Prashad ,  Christopher Towler ,  Ruoqiu Wu

    Inventor： Weichun Chen ,  Hong-Yong Kim ,  Jessica Liang ,  Michael Mutz ,  Mahavir Prashad ,  Christopher Towler ,  Ruoqiu Wu

    IPC: A61K31/517 ,  C07D239/88 ,  A61P29/00 ,  A61P21/00 ,  A61P19/02

    CPC classification number: C07D239/91 ,  A61K31/517

    Abstract: There is described a new polymorphic form of 4-(7-Hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile having structural formula I(B) and to a method of preparing it.There is further a process or method for the manufacture of a pharmaceutically active quinazolinone compounds of the formula I wherein the symbols have the meanings given in the description, said process comprising reacting a compound of the formula II, wherein R4* is R1*—C(═O)— wherein R1* is independently selected from the group of meanings of R1 as defined for a compound of the formula I so that R1* and R1 are identical to or different from each other, or R4* is especially H, and R1 and R3, R5 and R6 are as defined for a compound of the formula I, or a salt thereof, under simultaneous or sequential condensation and cyclisation conditions with an aniline compound of the formula III, wherein R2 and m are as defined for a compound of the formula I. Further reactions and related embodiments are also claimed and disclosed.

    Abstract translation: 描述了具有结构式I（B）的4-（7-羟基-2-异丙基-4-氧代-4H-喹唑啉-3-基） - 苄腈的新的多晶型物及其制备方法。 还有一种用于制备式I的药学活性喹唑啉酮化合物的方法或方法，其中符号具有在说明书中给出的含义，所述方法包括使式II化合物，其中R4 *是R1 * -C （ΟO） - 其中R 1 *独立地选自如式I化合物所定义的R 1的含义，使得R 1 *和R 1彼此相同或不同，或者R 4 *特别是H，和 R 1和R 3，R 5和R 6如式I化合物或其盐在同时或连续的缩合和环化条件下与式III的苯胺化合物所定义，其中R 2和m如化合物 其他反应和相关实施方案也被要求保护和公开。

    Organic Compounds
    3.
    发明申请
    Organic Compounds 审中-公开
    有机化合物

    公开(公告)号：US20080300410A1

    公开(公告)日：2008-12-04

    申请号：US12093825

    申请日：2006-11-16

    Applicant: Mahavir Prashad ,  Yugang Liu ,  Bin Hu ,  Michael J. Girgis ,  Frank Schaefer

    Inventor： Mahavir Prashad ,  Yugang Liu ,  Bin Hu ,  Michael J. Girgis ,  Frank Schaefer

    IPC: C07D211/32

    CPC classification number: C07D211/26 ,  C07D213/26

    Abstract: The present invention relates to salts of aryl compounds as discussed below and to methods of manufacture thereof, as well as other subject matter. More particularly, the invention relates to salts useful as intermediates for the synthesis of the cinnamanilide of formula (Y): where Ra is selected from H, OH, C1, C2, C3 or C4 alkyl; and R1 is C1, C2, C3 or C4 alkyl.

    Abstract translation: 本发明涉及如下所述的芳基化合物的盐及其制备方法以及其它主题。 更具体地，本发明涉及可用作合成式（Y）的肉桂酰苯胺的中间体的盐：其中R a选自H，OH，C 1，C 2，C 3或C 4烷基; 并且R 1是C 1，C 2，C 3或C 4烷基。

    Chemical process for the preparation of intermediates to obtain n-formyl hydroxy-lamine compounds
    4.
    发明申请
    Chemical process for the preparation of intermediates to obtain n-formyl hydroxy-lamine compounds 失效
    用于制备中间体以获得正甲酰基羟基 - 胺化合物的化学方法

    公开(公告)号：US20070179298A1

    公开(公告)日：2007-08-02

    申请号：US10544919

    申请日：2004-02-20

    Applicant: Mahavir Prashad ,  Hong-Yong Kim ,  Bin Hu ,  Joel Slade ,  Prasad Kapa ,  Michael Girgis

    Inventor： Mahavir Prashad ,  Hong-Yong Kim ,  Bin Hu ,  Joel Slade ,  Prasad Kapa ,  Michael Girgis

    IPC: A61K31/4439 ,  C07D417/02 ,  C07D403/02

    CPC classification number: C07D401/12 ,  C07B2200/07 ,  C07C51/487 ,  C07C239/20 ,  C07C59/01

    Abstract: Improved processes for preparing intermediates useful for preparing antibacterial N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl}-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, which have one or more of the following features: (1) make use of a particular β-lactam intermediate; (2) which make use of a particular resolving agents, enantiomerically pure substituted propionic acids, especially (R)-2-butyl-3-hydroxy-propionic acid; (3) which avoid the use of hydrogen peroxide; and (4) which facilitate selective debenzylation reducing production of waste by-products.

    Abstract translation: 用于制备可用于制备抗菌N- [1-氧代-2-烷基-3-（N-羟基甲酰氨基） - 丙基} - （羰基氨基 - 芳基或 - 杂芳基） - 偶氮基-4-7烷烃或噻唑烷-4-醇的中间体的改进方法，其具有 一个或多个以下特征：（1）利用特定的β-内酰胺中间体; （2），其使用特定的拆分剂，对映体纯的取代的丙酸，特别是（R）-2-丁基-3-羟基 - 丙酸; （3）避免使用过氧化氢; 和（4）促进选择性脱苄基化减少废弃副产物的生产。

    Process for preparing phosphinyloxy propanaminium inner salt derivatives
    6.
    发明授权
    Process for preparing phosphinyloxy propanaminium inner salt derivatives 失效
    制备膦酰氧基丙胺内盐衍生物的方法

    公开(公告)号：US5412137A

    公开(公告)日：1995-05-02

    申请号：US197050

    申请日：1994-02-16

    Applicant: Mahavir Prashad ,  Prasad K. Kapa

    Inventor： Mahavir Prashad ,  Prasad K. Kapa

    IPC: C07F9/09 ,  C07F9/113 ,  C07F9/165 ,  C07F9/173

    CPC classification number: C07F9/173 ,  C07F9/091 ,  C07F9/113 ,  C07F9/1651

    Abstract: A process for preparing compounds of the formula ##STR1## where X.sub.1 and X.sub.2 are independently O or S, andR.sub.1 is as defined herein,R.sub.2, R.sub.3, and R.sub.4 are each independently straight or branched chain (C.sub.1-4)alkyl,and pharmaceutically acceptable salts, physiological hydrolyzable esters, and pro-drug forms thereof, which are useful as hypoglycemic agents.

    Abstract translation: 制备式（I）的化合物的方法，其中X 1和X 2独立地为O或S，R 1如本文所定义，R 2，R 3和R 4各自独立地为直链或支链（C 1-4）烷基 ，以及其可用作降血糖剂的药学上可接受的盐，生理可水解的酯和其前药形式。

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