Process for preparing nitrooxyalkyl substituted esters of carboxylic acids, intermediates useful in said process and preparation thereof
    4.
    发明授权
    Process for preparing nitrooxyalkyl substituted esters of carboxylic acids, intermediates useful in said process and preparation thereof 失效
    制备硝基氧基烷基取代的羧酸酯的方法,可用于所述方法的中间体及其制备方法

    公开(公告)号:US07723382B2

    公开(公告)日:2010-05-25

    申请号:US10522986

    申请日:2003-08-06

    摘要: The present invention refers to a process for preparing a compound of general formula (A), as reported in the description, wherein R is a radical of a drug and R1-R12 are hydrogen or alkyl groups, m, n, o, q, r and s are each independently an integer from 0 to 6, and p is 0 or 1, and X is O, S, SO, SO2, NR13 or PR13 or an aryl, heteroaryl group, said process comprising reacting a compound of formula (B) R—COOZ (B) wherein R is as defined above and Z is hydrogen or a cation selected from: Li+, Na+, K+, Ca++, Mg++, tetralkylammonium, tetralkylphosphonium, with a compound of formula (C), as reported in the description, wherein R1-R12 and m, n, o, p, q, r, s are as defined above and Y is a suitable leaving group.

    摘要翻译: 本发明涉及制备通式(A)化合物的方法,如说明书所述,其中R为药物基团,R 1 -R 12为氢或烷基,m,n,o,q, r和s各自独立地为0〜6的整数,p为0或1,X为O,S,SO,SO 2,NR 13或PR 13或芳基杂芳基,所述方法包括使式 B)R-COOZ(B)其中R如上所定义,Z是氢或选自:Li +,Na +,K +,Ca ++,Mg ++,四烷基铵,四烷基鏻与式(C)化合物的阳离子,如 其描述其中R1-R12和m,n,o,p,q,r,s如上所定义,Y是合适的离去基团。

    Process for preparing nitrooxyderivatives of naproxen
    5.
    发明授权
    Process for preparing nitrooxyderivatives of naproxen 失效
    制备萘普生硝基氧化酶的方法

    公开(公告)号:US07199258B2

    公开(公告)日:2007-04-03

    申请号:US10523722

    申请日:2003-08-06

    IPC分类号: C07C203/04

    摘要: The present invention refers to a process for preparing a compound of general formula (A), as reported in the description, wherein R is a radical of naproxen or bromonaproxen and R1–R12 are hydrogen or alkyl groups, m, n, o, q, r and s are each independently an integer from 0 to 6, and p is 0 or 1, and and X is O, S, SO, SO2, NR13 or PR13 or an aryl, heteroaryl group, said process comprising reacting a compound of formula (B) R—COOZ  (B) wherein R is as defined above and Z is hydrogen or a cation selected from: Li+, Na+, K+, Ca++, Mg++, tetralkylammonium, tetralkylphosphonium, with a compound of formula (C), as reported in the description, wherein R1–R12 and m, n, o, p, q, r, s are as defined above and Y is a suitable leaving group.

    摘要翻译: 本发明涉及制备通式(A)化合物的方法,如说明书中所报导的,其中R是萘普生或溴苯丙酮的基团,R 1 -R 12, / SUB>为氢或烷基,m,n,o,q,r和s各自独立地为0至6的整数,p为0或1,X为O,S,SO,SO NR 2,NR 13或NR 13或芳基杂芳基,所述方法包括使式

    Liquid-suspension controlled-release pharmaceutical composition
    10.
    发明授权
    Liquid-suspension controlled-release pharmaceutical composition 失效
    液体悬浮液控释药物组合物

    公开(公告)号:US5527545A

    公开(公告)日:1996-06-18

    申请号:US165307

    申请日:1993-12-10

    摘要: Disclosed is a liquid-suspension controlled-release enteric-coated pharmaceutical formulation for the administration of naproxen, comprising (a) microgranules of naproxen and an excipient; (b) four successive coats of polymeric hydrophilic and hydrophobic materials, at least the innermost of said coats imparting controlled-release properties to said naproxen according to a predetermined release profile, and at least the outermost of said coats imparting resistance to dissolution in gastric fluids; and (c) a liquid administration vehicle. This composition enables the oral administration of naproxen as a single daily dose the adjustment of the dosage to a patient's requirements, and avoids detrimental effects of prolonged contact of naproxen with the gastric mucosa thus aiding oral intake and minimizing the drug's typical side effects.

    摘要翻译: 公开了一种用于施用萘普生的液体 - 悬液控释肠溶衣制剂,其包含(a)萘普生微粒和赋形剂; (b)四个连续的聚合亲水和疏水材料的涂层,至少最内层的所述涂层根据预定的释放曲线赋予所述萘普生的控制释放性能,并且至少所述涂层的最外面赋予对胃液中溶解的抵抗力 ; 和(c)液体给药载体。 该组合物能够以单次日剂量口服给予萘普生,根据患者的要求调整剂量,并避免萘普生与胃粘膜长时间接触的有害作用,从而有助于口服摄入并使药物的典型副作用最小化。