-
1.
公开(公告)号:US4774253A
公开(公告)日:1988-09-27
申请号:US917566
申请日:1986-10-10
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。
-
公开(公告)号:US4241060A
公开(公告)日:1980-12-23
申请号:US930622
申请日:1978-08-03
申请人: Carey E. Smithen
发明人: Carey E. Smithen
IPC分类号: A61K31/415 , A61K31/4427 , A61K31/445 , A61P31/04 , A61P33/02 , A61P43/00 , C07D233/91 , C07D401/06 , C07D401/12 , C07D413/06 , A61K31/535
CPC分类号: C07D233/91 , Y10S514/862
摘要: Nitroimidazoles of the formula ##STR1## wherein R.sup.1 and R.sup.2 are as hereinafter set forth, are described. The nitroimidazoles are useful as hypoxic-cell radiosensitizers, as well as being useful as antiprotozoal agents.
摘要翻译: 其中R1和R2如下文所述的式“IMAGE”的硝基咪唑被描述。 硝基咪唑可用作缺氧细胞放射增敏剂,也可用作抗原虫药。
-
公开(公告)号:US4105852A
公开(公告)日:1978-08-08
申请号:US741001
申请日:1976-11-11
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 。
-
公开(公告)号:USRE30473E
公开(公告)日:1981-01-06
申请号:US929383
申请日:1978-07-31
IPC分类号: A61K38/00 , C07D213/50 , C07D243/24 , C07D249/08 , C07K5/06 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078
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 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 sedatives.
-
-
-