公开(公告)号：US4885283A

公开(公告)日：1989-12-05

申请号：US126643

申请日：1987-12-01

申请人： Michael J. Broadhurst ,  Balraj K. Handa ,  William H. Johnson ,  Geoffrey Lawton ,  Peter J. Machin

发明人： Michael J. Broadhurst ,  Balraj K. Handa ,  William H. Johnson ,  Geoffrey Lawton ,  Peter J. Machin

IPC分类号： A61K38/00 ,  C07K5/06

CPC分类号： C07K5/06191 ,  A61K38/00

摘要： The invention relates compounds of the formula ##STR1## wherein R.sup.1 -R.sup.5 and X have the significance given in the description, and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme collagenase and can be used in the form of medicaments for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis.

公开(公告)号：US4387100A

公开(公告)日：1983-06-07

申请号：US237612

申请日：1981-02-24

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 ,  A61K31/41 ,  A61K31/415 ,  C07D233/61

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--CH.dbd.CH--C*H.sub.2 -- (a), 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 ##STR2## 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-CH = CH-C * H 2 - （a）的基团，其中双键为反式，并且带有星号的碳原子与Z连接，Z为含有一个的5元芳族杂环 或更多的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 描述了一组式（IMAGE）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。