公开(公告)号：US4612324A

公开(公告)日：1986-09-16

申请号：US576083

申请日：1984-02-01

申请人： Colin H. Cashin ,  Noel A. Roberts ,  Brian P. Tong

发明人： Colin H. Cashin ,  Noel A. Roberts ,  Brian P. Tong

IPC分类号： A61K31/415 ,  C07D233/54 ,  C07D233/64

CPC分类号： C07D233/64 ,  A61K31/415

摘要： Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each individually is hydrogen, or lower alkyl and R.sup.4 is hydroxy, lower alkoxy, aryl-(lower alkoxy), amino, mono(lower alkyl)amino or di(lower alkyl) amino,and pharmaceutically acceptable salts thereof which are useful in the treatment of degenerative joint diseases and of Wilson's disease are described.

摘要翻译： 其中R1，R2和R3各自独立地为氢，或低级烷基，R4为羟基，低级烷氧基，芳基 - （低级烷氧基），氨基，单（低级烷基）氨基或二（低级烷基） ）氨基及其药学上可接受的盐可用于治疗退行性关节疾病和威尔逊氏病。

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。