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    Oxazole and isoxazole derivatives having anti-arthritic activity
    1.
    发明授权
    Oxazole and isoxazole derivatives having anti-arthritic activity 失效
    恶唑和具有抗关节炎活性的异恶唑衍生物

    公开(公告)号：US4774253A

    公开(公告)日：1988-09-27

    申请号：US917566

    申请日：1986-10-10

    申请人： Peter J. Machin ,  John M. Osbond ,  Christopher R. Self ,  Carey E. Smithen ,  Brian P. Tong

    发明人： Peter J. Machin ,  John M. Osbond ,  Christopher R. Self ,  Carey E. Smithen ,  Brian P. Tong

    IPC分类号： C07D261/08 ,  C07D263/32 ,  C07D413/04 ,  A61K31/42 ,  C07D261/06 ,  C07D263/30

    CPC分类号： C07D413/04 ,  C07D261/08 ,  C07D263/32

    摘要： Oxazole and isoxazole derivatives of the formula ##STR1## wherein A is C.sub.1-6 -alkylene, Het is a 2-R-oxazol-5-yl, 5-R-oxazol-2-yl, 4-R-oxazol-2-yl, 2-R-oxazol-4-yl, 3-R-isoxazol-5-yl or 5-R-isoxazol-3-yl group which is optionally substituted on the heterocyclic ring by a C.sub.1-6 -alkyl group, R is phenyl or thienyl monosubstituted or disubstituted by halogen, trifluoromethyl or C.sub.1-6 -alkylthio, R.sup.1 and R.sup.2 each is a C.sub.1-6 -alkyl group and R.sup.3 is a hydroxy or C.sub.1-6 -alkoxy group or a group of the formula --NR.sup.4 R.sup.5 in which R.sup.4 and R.sup.5 each is a hydrogen atom or a C.sub.1-6 -alkyl group or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached is a 5-membered or 6-membered saturated heteromonocyclic ring which may contain an oxygen or sulphur atom or an additional nitrogen atom, and pharmaceutically acceptable salts of the compounds of formula I in which R.sup.3 is a hydroxy group with bases, have anti-arthritic activity.

    摘要翻译： 下式的恶唑和异恶唑衍生物其中A是C 1-6 - 亚烷基，Het是2-R唑恶基，5-R唑-2-基，4-R-恶唑-2 芳基，2-R-恶唑-4-基，3-R-异恶唑-5-基或5-R-异恶唑-3-基，其在杂环上被C 1-6 - 烷基任意取代， R是苯基或被卤素，三氟甲基或C 1-6 - 烷硫基单取代或二取代的噻吩基，R 1和R 2各自是C 1-6 - 烷基，R 3是羟基或C 1-6 - 烷氧基或式 - NR4R5其中R4和R5各自为氢原子或C1-6烷基或R4和R5与它们所连接的氮原子一起为可含有氧的5元或6元饱和杂单环 或硫原子或另外的氮原子，以及其中R3是具有碱基的羟基的式I化合物的药学上可接受的盐具有抗关节炎活性。

    Substituted phenyl ketones
    3.
    发明授权
    Substituted phenyl ketones 失效
    取代苯基酮

    公开(公告)号：US4105852A

    公开(公告)日：1978-08-08

    申请号：US741001

    申请日：1976-11-11

    申请人： Cedric H. Hassall ,  William H. Johnson ,  Antonin Krohn ,  Carey E. Smithen ,  William A. Thomas

    发明人： Cedric H. Hassall ,  William H. Johnson ,  Antonin Krohn ,  Carey E. Smithen ,  William A. Thomas

    IPC分类号： A61K38/00 ,  C07D213/50 ,  C07D243/24 ,  C07D249/08 ,  C07K5/06 ,  C07K5/065 ,  C07K5/068 ,  C07K5/072 ,  C07K5/078 ,  C07D233/64

    CPC分类号： C07K5/06191 ,  C07D213/50 ,  C07D243/24 ,  C07D249/08 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06086 ,  C07K5/06095 ,  C07K5/06104 ,  C07K5/06165 ,  A61K38/00 ,  Y10S514/906

    摘要： This invention is directed toward pharmacologically active compounds of the formula ##STR1## wherein A represents a nitrogen atom which may be substituted by a methyl, cyclopropylmethyl, di(C.sub.1-4 alkyl)aminoethyl, methoxymethyl or hydroxyethyl group and B represents a carbonyl group or A and B together represent a grouping of the formula ##STR2## in which R.sup.a represents a hydrogen atom or a lower alkyl or hydroxymethyl group and X represents a nitrogen atom or C--R.sup.b wherein R.sup.b represents a hydrogen atom or a lower alkyl or hydroxymethyl group; R represents a halogen atom or a nitro or trifluoromethyl group; R.sup.1 represents a hydrogen atom or a lower alkyl group; R.sup.2 represents an acyl group derived from a naturally occurring amino acid (all such groups which contain an asymmetric carbon atom having the L- or D,L-configuration) and R.sup.3 represents a phenyl, halophenyl or 2-pyridyl group and acid addition salts thereof.Also provided are methods for their preparation and intermediates thereof. These compounds exhibit activity as anticonvulsants, muscle relaxants and sedative.

    摘要翻译： 本发明涉及下式的药理学活性化合物，其中A表示可被甲基，环丙基甲基，二（C 1-4烷基）氨基乙基，甲氧基甲基或羟乙基取代的氮原子，B表示羰基或A 和B一起表示其中R a表示氢原子或低级烷基或羟甲基并且X表示氮原子的式“IMAGE”或其中R b表示氢原子或低级烷基或羟甲基的C-R b的基团; R表示卤素原子或硝基或三氟甲基; R1表示氢原子或低级烷基; R2表示衍生自天然存在的氨基酸的酰基（所有这些基团含有具有L或D的不对称碳原子，L构型），R 3表示苯基，卤代苯基或2-吡啶基，其酸加成盐 。