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    Hydroxylamine bearing amino acid derivatives as collagenase inhibitors
    7.
    发明授权
    Hydroxylamine bearing amino acid derivatives as collagenase inhibitors 失效
    具有氨基酸衍生物的羟胺作为胶原酶抑制剂

    公开(公告)号：US4996358A

    公开(公告)日：1991-02-26

    申请号：US336264

    申请日：1989-04-11

    申请人： Balraj K. Handa ,  William H. Johnson ,  Peter J. Machin

    发明人： Balraj K. Handa ,  William H. Johnson ,  Peter J. Machin

    IPC分类号： C12N9/99 ,  A61K31/16 ,  A61K31/165 ,  A61K31/195 ,  A61K31/22 ,  A61K31/395 ,  A61K38/00 ,  A61P29/00 ,  A61P43/00 ,  C07C67/00 ,  C07C231/00 ,  C07C237/06 ,  C07C237/08 ,  C07C237/12 ,  C07C237/22 ,  C07C259/06 ,  C07C313/00 ,  C07C323/60 ,  C07D207/40 ,  C07D225/02 ,  C07K1/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/068

    CPC分类号： C07K5/06086 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/06052 ,  C07K5/06078 ,  A61K38/00

    摘要： Compounds of the formula ##STR1## wherein A is a group of the formula HN(OH)--CO-- or HCO--N(OH)--; R.sup.1 is a C.sub.2 -C.sub.5 -alkyl; R.sup.2 is the characterizing group of a natural .alpha.-amino acid in which any functional group present may be protected, any amino group present may be acylated and any carboxyl group present may be amidated, with the proviso that R.sup.2 is not hydrogen or methyl; R.sup.3 is hydrogen, amino, hydroxy, mercapto, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.6 -alkylamino, C.sub.1 -C.sub.6 -alkylthio or aryl-(C.sub.1 -C.sub.6 -alkyl), or amino-(C.sub.1 -C.sub.6 -alkyl), hydroxy-(C.sub.1 -C.sub.6 -alkyl), mercapto-(C.sub.1 -C.sub.6 -alkyl) or carboxy-(C.sub.1 -C.sub.6 -alkyl) in which the amino, hydroxy, mercapto or carboxyl group may be protected, the amino group may be acylated or the carboxyl group may be amidated; R.sup.4 is hydrogen or methyl; R.sup.5 is hydrogen or a C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy-C.sub.1 -C.sub.6 -alkyl, di(C.sub.1 -C.sub.6 -alkoxy)-methylene, carboxyl, (C.sub.1 -C.sub.6 -alkyl)-carbonyl, (C.sub.1 -C.sub.6 -alkoxy)carbonyl, arylmethoxycarbonyl, (C.sub.1 -C.sub.6 -alkyl)aminocarbonyl or arylaminocarbonyl; and R.sup.6 is hydrogen or methyl; or R.sup.2 and R.sup.4 taken together are a group of the formula --(CH.sub.2).sub.n -- in which n is a number from 4 to 11; or R.sup.4 and R.sup.6 taken together are a trimethylene; and pharmaceutically acceptable salts of those compounds which are acidic or basic are described. The compounds of formula I possess collagenase inhibitory activity and can be used in the control or prevention of degenerative joint diseases.

    摘要翻译： 式（Ⅰ）化合物其中A为式HN（OH）-CO-或HCO-N（OH） - 的基团; R1是C2-C5-烷基; R2是天然α-氨基酸的表征基团，其中存在的任何官能团可以被保护，任何存在的氨基可以被酰化，并且存在的任何羧基可以被酰胺化，条件是R 2不是氢或甲基; R3是氢，氨基，羟基，巯基，C1-C6-烷基，C1-C4-烷氧基，C1-C6-烷基氨基，C1-C6-烷硫基或芳基 - （C1-C6-烷基）或氨基 - （C1- C6烷基），羟基 - （C1-C6-烷基），巯基 - （C1-C6-烷基）或羧基 - （C1-C6-烷基），其中氨基，羟基，巯基或羧基可被保护 氨基可以被酰化或羧基可以酰胺化; R4是氢或甲基; R 5是氢或C 1 -C 6烷基，C 1 -C 6烷氧基-C 1 -C 6烷基，二（C 1 -C 6 - 烷氧基） - 亚甲基，羧基，（C 1 -C 6 - 烷基） - 羰基，（C 1 -C 6 - 烷氧基）羰基，芳基甲氧基羰基，（C 1 -C 6 - 烷基）氨基羰基或芳基氨基羰基; R6为氢或甲基; 或者R 2和R 4一起是式 - （CH 2）n - 的基团，其中n是4至11的数; 或R4和R6一起是三亚甲基; 和描述了那些酸性或碱性化合物的药学上可接受的盐。 式I化合物具有胶原酶抑制活性，可用于控制或预防退行性关节疾病。

    Azolyl-substituted phenoxy-aminopropanol derivatives
    9.
    发明授权
    Azolyl-substituted phenoxy-aminopropanol derivatives 失效
    唑基取代的苯氧基 - 氨基丙醇衍生物

    公开(公告)号：US4577030A

    公开(公告)日：1986-03-18

    申请号：US475290

    申请日：1983-03-14

    申请人： Peter J. Machin

    发明人： Peter J. Machin

    IPC分类号： A61K31/395 ,  C07C43/23 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/56 ,  C07D233/60 ,  C07D235/06 ,  C07D249/04 ,  C07D249/08 ,  C07D249/18 ,  C07D521/00

    CPC分类号： C07C43/23 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/56 ,  C07D233/56 ,  C07D235/06 ,  C07D249/04 ,  C07D249/08 ,  C07D249/18

    摘要： Phenoxy-aminopropanol derivatives of the formula ##STR1## wherein R is lower alkyl, X is oxygen or sulfur, n is the integer zero or 1, Y is methylene, ethylene or propylene or, when n is zero, Y can also be a group of the formula ##STR2## wherein the double-bond is trans and the carbon atom marked with an asterisk is linked to Z, and Z is a 5-membered aromatic heterocyclic ring which contains one or more nitrogen atoms as the sole hetero atom (s), said heterocyclic ring is linked to Y via a nitrogen atom, and may be substituted by halogen, lower alkyl, lower alkoxy, aryl, cyano or carboxamido, or on adjacent carbon atoms by a group of the formula--(CH.sub.2).sub.4 -- (b)or--CH.dbd.CH--CH.dbd.CH--, (c)and pharmaceutically acceptable acid addition salts thereof are described. A process for the preparation of the compound of formula I and pharmaceutical preparations containing them are also described. The aforementioned compounds and salts possess .beta.-adrenergic blocking activity and antihypertensive activity.

    摘要翻译： 下式的苯氧基 - 氨基丙醇衍生物其中R为低级烷基，X为氧或硫，n为整数0或1，Y为亚甲基，亚乙基或亚丙基，或当n为零时，Y也可为 式中-CH = CH- * CH 2 - （a）的基团，其中双键是反式，并且带有星号的碳原子与Z连接，Z是含有一个或多个的5元芳族杂环 氮原子作为唯一的杂原子，所述杂环通过氮原子与Y连接，并且可以被卤素，低级烷基，低级烷氧基，芳基，氰基或甲酰氨基取代，或在相邻碳原子上被一个基团 描述了式 - （CH 2）4 - （b）或-CH = CH-CH = CH-，（c）及其药学上可接受的酸加成盐。 还描述了制备式I化合物的方法和含有它们的药物制剂。 上述化合物和盐具有β-肾上腺素能阻断活性和抗高血压活性。

    Oxazole and isoxazole derivatives having anti-arthritic activity
    10.
    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。