Process for preparing nitrooxyderivative of naproxen
    32.
    发明申请
    Process for preparing nitrooxyderivative of naproxen 失效
    制备萘普生硝基氧化酶的方法

    公开(公告)号:US20060173005A1

    公开(公告)日:2006-08-03

    申请号:US10523722

    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 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PR 13或芳基杂芳基,所述方法包括使式(B)化合物<?in-line-formula description =“在线式 “end =”lead“?> R-COOZ(B)<?in-line-formula description =”In-line Formulas“end =”tail“?>其中R如上所定义,Z是氢或选择阳离子 其中R1-R12和m,n,o,p,q,r,s分别为:Li +,Na +,K +,Ca ++,Mg ++,四烷基铵,四烷基鏻与式(C) 如上所定义,Y是合适的离去基团。

    Nitroderivatives of polysaccharides
    33.
    发明授权
    Nitroderivatives of polysaccharides 失效
    多糖的硝基衍生物

    公开(公告)号:US07005508B2

    公开(公告)日:2006-02-28

    申请号:US10362811

    申请日:2001-08-10

    CPC分类号: C08B37/0075 C08B37/0063

    摘要: The present invention provides a new class of compounds presenting a high compatibility with tissues and organic fluids. Such new compounds are polysaccharides essentially formed of units of uronic acid and/or hexosamine, containing nitro groups —ONO2 covalently bonded to the saccharide structure. Preferably, the polysaccharides according to the invention are prevalently formed of disaccharide repeating units formed of uronic acid and hexosamine. These compounds, in psychological conditions, selectively release NO, allowing a reduction in the amount of NO needed to achieve a determined therapeutical effect. This result has been achieved by functionalizing polysaccharides essentially formed of units of uronic acid and/or hexosamine, with subsituents containing a ONO2 ? group.

    摘要翻译: 本发明提供了与组织和有机流体具有高相容性的新类化合物。 这些新化合物是基本上由糖醛酸和/或己糖胺的单元形成的多糖,其含有与糖结构共价结合的硝基-ONO 2。 优选地,根据本发明的多糖优选由由糖醛酸和己糖胺形成的二糖重复单元形成。 这些化合物在心理条件下选择性地释放NO,允许减少实现确定的治疗效果所需的NO量。 通过官能化基本上由糖醛酸和/或己糖胺形成的多糖来实现该结果,其中含有ONO的取代基包含ONO 2? 组。

    Nitric oxide releasing steroids
    36.
    发明授权
    Nitric oxide releasing steroids 有权
    一氧化氮释放类固醇

    公开(公告)号:US08933062B2

    公开(公告)日:2015-01-13

    申请号:US12525970

    申请日:2008-01-28

    CPC分类号: C07J41/005

    摘要: The invention relates to nitrooxyderivative of corticosteroids of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof R—(Z)a—Rx  (I) wherein R is the corticosteroid residue of formula (II): wherein: R1 is OH, R2—CH3, or R1 and R2 are taken together to form a group of formula (III) R3 is Cl or F; R4 is H or F; wherein R1, R2, R3 and R4 can be linked to the correspondent carbon atoms of the steroidal structure in position α or β; with the proviso that: when R1 and R2 are the group of formula (III) then R3 is F and R4 is H or F; The compounds are useful in the treatment of respiratory diseases, inflammatory diseases, dermatological diseases and ocular diseases.

    摘要翻译: 本发明涉及通式(I)的糖皮质激素及其药学上可接受的盐或立体异构体的硝基氧基衍生物R-(Z)a-Rx(I)其中R是式(II)的皮质类固醇残基:其中:R1是OH,R2 -CH 3或R 1和R 2一起形成式(III)的基团,R 3为Cl或F; R4是H或F; 其中R 1,R 2,R 3和R 4可以连接到甾族结构在位置α或bgr中的相应碳原子。 条件是:当R 1和R 2是式(III)的基团时,R 3是F且R 4是H或F; 该化合物可用于治疗呼吸系统疾病,炎性疾病,皮肤病和眼部疾病。