Process for preparing nitrooxyalkyl substituted esters of carboxylic acids, intermediates useful in said process and preparation thereof
    1.
    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。

    Substituted dibenzodiazepinones
    2.
    发明授权
    Substituted dibenzodiazepinones 失效
    取代的二苯并二氮杂酮

    公开(公告)号:US4447434A

    公开(公告)日:1984-05-08

    申请号:US462149

    申请日:1983-01-31

    摘要: The specification describes new substituted dibenzodiazepinones of formula ##STR1## wherein R.sub.1 is hydrogen or chlorine atom and R is (1-methyl-4-piperidinyl)methyl, (1-methyl-1,2,5,6-tetrahydro-4-pyridinyl)methyl,1-methyl-1,2,5,6-tetrahydro-4-pyridinyl, (1-methyl-4-piperidinylidene)methyl,(2,3-dehydro-8-methyl-8-aza-bicyclo[3,2,1]oct-3-yl)-methyl, (8-methyl-8-aza-bicyclo[3,2,1]oct-3-ylidene)-methyl or an endo-or exo-(8-methyl-8-azabicyclo[3,2,1]oct-3-yl)methyl each being optionally substituted by one or two methyls on the heterocyclic ring, and the nontoxic, pharmaceutically acceptable acid addition salts thereof, processes for preparing them and pharmaceutical compositions containing these compounds.The compounds of formula I have an antiulcerative effect and an inhibitory effect on the secretion of gastric substances having anticholinergic activity, such as dryness of the mouth and mydriasis.

    摘要翻译: 该说明书描述了式(Ⅰ)的新的取代二苯并二氮杂酮,其中R 1是氢或氯原子,R是(1-甲基-4-哌啶基)甲基,(1-甲基-1,2,5,6-四氢 - 4-吡啶基)甲基,1-甲基-1,2,5,6-四氢-4-吡啶基,(1-甲基-4-亚哌啶基)甲基,(2,3-脱氢-8-甲基-8-氮杂 - 双环[3,2,1]辛-3-基) - 甲基,(8-甲基-8-氮杂 - 双环[3,2,1]辛-3-基) - 甲基或内 - 或外 - - (8-甲基-8-氮杂双环[3,2,1]辛-3-基)甲基,其各自任选被杂环上的一个或两个甲基取代,及其无毒的药学上可接受的酸加成盐,用于 制备它们和含有这些化合物的药物组合物。 式I化合物具有抗溃疡作用和对具有抗胆碱能活性的胃物质分泌的抑制作用,例如口干和散瞳。

    Imidazolylphenyl amidines, pharmaceutical compositions containing same
and use thereof
    6.
    发明授权
    Imidazolylphenyl amidines, pharmaceutical compositions containing same and use thereof 失效
    咪唑基苯基脒,含有其的药物组合物及其应用

    公开(公告)号:US4386099A

    公开(公告)日:1983-05-31

    申请号:US322903

    申请日:1981-11-19

    CPC分类号: C07D233/64

    摘要: This invention relates to imidazolylphenyl amidines, the preparation thereof, and pharmaceutical compositions containing them. More particularly, this invention relates to compounds of the general formula ##STR1## in which R, R.sub.1, R.sub.3, which may be the same or different, each represent a hydrogen atom or a lower alkyl group, and R.sub.2 represents a linear or branched alkyl, alkenyl, or alkynyl group, a cyano group, a hydroxyl group, a substituted or unsubstituted cycloalkyl or cycloaliphatic alkyl group, a bicyclic group, an aralkyl or aryl group optionally substituted by halogen, methyl, methoxy, or methylenedioxy groups, or a substituted or unsubstituted heterocyclylalkyl or heterocyclic group which may also contain a further hetero atom, or a non-toxic, pharmacologically acceptable acid addition salt thereof. These compounds are useful in treating disorders of the gastrointestinal tract.

    摘要翻译: 本发明涉及咪唑基苯基脒,其制备方法和含有它们的药物组合物。 更具体地说,本发明涉及通式“IMAGE”的化合物,其中R,R 1,R 3可以相同或不同,各自表示氢原子或低级烷基,R 2表示直链或支链烷基 ,烯基或炔基,氰基,羟基,取代或未取代的环烷基或脂环族烷基,双环基团,任选被卤素,甲基,甲氧基或亚甲二氧基取代的芳烷基或芳基,或取代 或还可以含有另外的杂原子的未取代的杂环基烷基或杂环基,或其无药学上可接受的酸加成盐。 这些化合物可用于治疗胃肠道疾病。

    Nitric oxide donors capable of reducing toxicity from drugs
    10.
    发明授权
    Nitric oxide donors capable of reducing toxicity from drugs 失效
    能够降低药物毒性的一氧化氮供体

    公开(公告)号:US07087588B2

    公开(公告)日:2006-08-08

    申请号:US10885121

    申请日:2004-07-07

    申请人: Piero del Soldato

    发明人: Piero del Soldato

    CPC分类号: A61K45/06

    摘要: Use of organic compounds containing the —ONO2 function, or inorganic compound containing the —NO group or compositions comprising said compounds to reduce the toxicity caused by drugs to the gastrointestinal and/or renal apparatus, said compounds being characterized in that they are nitric oxide NO donors i.e., when they are put into contact in vitro with cells of the vasal endothelium or platelets.

    摘要翻译: 使用含有-ONO 2 N 2官能团的有机化合物或含有-NO基团的无机化合物或包含所述化合物的组合物以降低由药物引起的对胃肠和/或肾脏装置的毒性,所述化合物为 其特征在于它们是一氧化氮NO供体,即当它们在体外与血管内皮细胞或血小板的细胞接触时。