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55 条记录 (耗时 0.028 秒)

    1,2-Diphenyl-3,5-ditrifluoroacetyloxy-4-butyl-5-hydroxy-3-pyrazoline
    3.
    发明授权
    1,2-Diphenyl-3,5-ditrifluoroacetyloxy-4-butyl-5-hydroxy-3-pyrazoline 失效
    1,2-二苯基-3,5-二
    三氟乙酰氧基-4-丁基-5-羟基-3-吡唑啉

    公开(公告)号：US4139709A

    公开(公告)日：1979-02-13

    申请号：US777073

    申请日：1977-03-14

    申请人： Nicolae S. Bodor ,  Kenneth B. Sloan

    发明人： Nicolae S. Bodor ,  Kenneth B. Sloan

    IPC分类号： C07D231/34 ,  C07D231/08

    CPC分类号： C07D231/34

    摘要： The compound 1,2-Diphenyl-3,5-ditrifluoroacetyloxy-4-butyl-5-hydroxy-3-pyrazoline is disclosed as an intermediate useful in the preparation of selected pro-phenylbutazone derivatives.Such selected pro-phenylbutazone derivatives are novel, transient, pro-drug forms of phenylbutazone and oxyphenbutazone having the following formulae wherein R, R.sub.2, R.sub.4, R.sub.5, X and Y are as defined herein: ##STR1## The above-identified compounds exhibit anti-inflammatory activity in warm-blooded animals. Upon administration to warm-blooded animals, these compounds pass through the gastrointenstinal tract and cleave in the bloodstream, thus releasing phenylbutazone or oxyphenbutazone in an anti-inflammatory effective amount at their therapeutic site or sites of activity.

    Anti-inflammatory and anti-ulcer compounds and process
    9.
    发明授权
    Anti-inflammatory and anti-ulcer compounds and process 失效
    抗炎和抗溃疡的化合物和工艺

    公开(公告)号：US4440754A

    公开(公告)日：1984-04-03

    申请号：US152588

    申请日：1980-05-23

    申请人： John R. J. Sorenson

    发明人： John R. J. Sorenson

    IPC分类号： A61K31/60 ,  C07D231/34 ,  A61K33/34 ,  A61K31/30

    CPC分类号： A61K31/60 ,  C07D231/34 ,  Y10S514/825 ,  Y10S514/925

    摘要： Disclosed herein are anti-inflammatory and anti-ulcer copper coordination compounds and a process for using them in the treatment of arthritis and gastrointestinal ulcers in animal bodies. The copper coordination compounds utilized are the reaction products of copper salts with:1. aromatic carboxylic acids or their alkaline earth salts;2. heterocyclic carboxylic acids or their alkaline earth salts;3. amino acids or their alkaline earth salts;4. amines; and5. suitably substituted steroids.The process disclosed comprises administering to experimental animals, orally or parentrally (subcutaneously), in controlled dosages, the aforementioned copper coordination compounds for the treatment of inflammation (i.e., arthritis) and ulcers of the gastrointestinal tract.

    摘要翻译： 本文公开了抗炎和抗溃疡铜配位化合物及其用于治疗动物体内的关节炎和胃肠溃疡的方法。 所使用的铜配位化合物是铜盐与以下物质的反应产物：1.芳族羧酸或其碱土金属盐; 杂环羧酸或其碱土金属盐; 氨基酸或其碱土金属盐; 胺; 和5.适当取代的类固醇。 所公开的方法包括以受控剂量口服或母体（皮下）施用实验动物，用于治疗炎症（即关节炎）和胃肠道溃疡的上述铜配位化合物。

    Novel transient pro-drug forms of phenylbutazone and oxyphenbutazone in compositions and methods of use
    10.
    发明授权
    Novel transient pro-drug forms of phenylbutazone and oxyphenbutazone in compositions and methods of use 失效

    公开(公告)号：US4169147A

    公开(公告)日：1979-09-25

    申请号：US840291

    申请日：1977-10-07

    申请人： Nicholas S. Bodor ,  Kenneth B. Sloan

    发明人： Nicholas S. Bodor ,  Kenneth B. Sloan

    IPC分类号： C07D231/34 ,  A61K31/44 ,  A61K31/415 ,  A61K31/455

    CPC分类号： C07D231/34 ,  Y02P20/55 ,  Y10S514/87

    摘要： There is provided, novel, transient, pro-drug forms of phenylbutazone and oxyphenbutazone having the following formula: ##STR1## wherein R represents a member selected from the group consisting of a C.sub.1 -C.sub.2 O-alkylsulfonyl group, an aryl(phenyl, p-tolyl, naphthyl)sulfonyl group, a nicotinoyl group, an iso-nicotinoyl group, a picolinoyl group, an N-protected naturally occurring amino acid residue, wherein the protective group on the amino group of the amino acid residue is removable via hydrogenolysis or hydrolysis, and an amino acid residue containing a C.sub.1 -C.sub.2 N,N-dialkylamino or a C.sub.4 -C.sub.6 cycloalkylamino group. ##STR2## wherein X and Y each represent a member selected from the group consisting of a hydrogen atom and a --OR.sub.1 group, with the proviso that either X or Y is a hydrogen atom and that R.sub.2 is a member selected from the same or different groups represented by R.sub.1 ; and wherein R.sub.1 represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.2 O-alkylsulfonyl group, an aryl(phenyl, p-tolyl, naphthyl)sulfonyl group, a --CH.sub.2 COOM group, wherein M represents an alkali or alkaline earth metal (Na, K, Ca, Mg), a --CO-R.sub.3 group, wherein R.sub.3 represents a member selected from the group consisting of a straight or branched C.sub.1 -C.sub.5 alkyl group, a C.sub.1 -C.sub.2 alkoxy group, a phenyl group, a substituted phenyl group, whose substituents are selected from the group consisting of a 2,3, or 4-hydroxy group, a 2,3, or 4-acetyloxy group, and a 2,3, or 4-acetylamino group, a 2,3, or 4-pyridyl group, a 1,2, or 5-imidazolyl group, a residue of an N-protected naturally occurring amino acid, wherein the protective group on the amino group of the amino acid is removable via hydrogenolysis or hydrolysis, and an amino acid residue containing a C.sub.1 -C.sub.2 N, N-dialkylamino or C.sub.4 -C.sub.5 cycloalkylamino group. ##STR3## wherein X or Y represents a member selected from the group consisting of a hydrogen atom and a -OR.sub.1 group, wherein R.sub.1 is as defined above with the proviso that either X or Y is a hydrogen atom, wherein R.sub.4 represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, an aryl group (phenyl, styryl), a 2,3, or 4-methoxyphenyl group, and a -CH.dbd.CH.sub.2 group; and wherein R.sub.5 represents a member selected from the group consisting of a --OOC- R.sub.6 group, a ##STR4## group, and a -COOM group, wherein M represents an alkali or alkaline earth metal (Na, K, Ca, Mg), wherein R.sub.6 represents a member selected from the group consisting of R.sub.4 as defined above, with the proviso that R.sub.6 cannot be a hydrogen atom, and wherein R.sub.7 and R.sub.8 each represent a C.sub.1 -C.sub.3 alkyl group.The above-identified compounds exhibit anti-inflammatory activity in warm-blooded animals. Upon administration to warm-blooded animals, these compounds pass through the gastrointestinal tract and "cleave" in the bloodstream, thus releasing phenylbutazone or oxyphenbutazone in an anti-inflammatory effective amount at their therapeutic site or sites of activity.