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1. 发明授权

US5308865A 2-cyano-3-hydroxy-enamides 失效
标题翻译： 2-氰基-3-羟基 - 烯酰胺
公开(公告)号：US5308865A
公开(公告)日：1994-05-03
申请号：US1564
申请日：1993-01-06
申请人： Robert R. Bartlett , David P. Kay , Elizabeth A. Kuo , Rudolf Schleyerbach , Wilfried Schwab
发明人： Robert R. Bartlett , David P. Kay , Elizabeth A. Kuo , Rudolf Schleyerbach , Wilfried Schwab
IPC分类号： A61K31/165 , A61K31/275 , A61K31/277 , A61P29/00 , C07C255/19 , C07C255/23 , C07C255/26 , C07C255/60 , C07C255/61 , C07C323/41 , C07C255/36
CPC分类号： C07C255/19 , C07C255/23
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of ##STR2## R.sub.13, R.sub.14 and R.sub.15 are individually selected from the group consisting of hydrogen, halogen and alkyl of 1 to 3 carbon atoms, n is an integer from 1 to 3, R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.3, R.sub.4 R.sub.5, R.sub.6 and R.sub.7 are individually selected from the group consisting of hydrogen, halogen, --NO.sub.2, --CN, alkyl, alkylthio and alkoxy of 1 to 6 carbon atoms, alkylcarbonyl of 2 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, ##STR3## m is 0, 1, 2 or 3, n is 1, 2 or 3; Hal, Hal.sub.1, Hal.sub.2 and Hal.sub.3 are individually halogen and ##STR4## R.sub.8, R.sub.9, R.sub.10, R.sub.11 and R.sub.12 are individually any of the groups defined above for R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 or R.sub.4 and R.sub.5 together form --O--CH.sub.2 --O-- and their non-toxic, pharmaceutically acceptable base addition salts having anti-inflammatory activity.
摘要翻译：选自下列化合物的化合物的化合物其中R 1选自下组的化合物：其中R 1选自由下列组成的组：R 1，R 14和R 15分别选自氢，卤素和烷基 1至3个碳原子，n为1至3的整数，R2为氢或1至3个碳原子的烷基，R3，R4 + L，R5，R6和R7分别选自氢，卤素，碳原子数1〜6的烷氧基，碳原子数为2〜6的烷基羰基，碳原子数3〜6的环烷基，（CH 2）m CF 3，O（CH 2）m CF 3，S（CH 2） mCF3， m为0,1,2或3，n为1,2或3; Hal，Hal1，Hal2和Hal3分别为卤素，R8，R9，R10，R11和R12分别是R3，R4，R5，R6和R7中定义的任何基团，R4或R5一起形成-O- CH2-O-及其具有抗炎活性的无毒的药学上可接受的碱加成盐。

2. 发明授权

US5371099A Phenyl carboxamide isoxazoles 失效
标题翻译：苯基甲酰胺异恶唑
公开(公告)号：US5371099A
公开(公告)日：1994-12-06
申请号：US54893
申请日：1993-04-28
申请人： Robert R. Bartlett , Matharu S. Singh , Elizabeth A. Kuo , Rudolf Schleyerbach , Robert Westwood
发明人： Robert R. Bartlett , Matharu S. Singh , Elizabeth A. Kuo , Rudolf Schleyerbach , Robert Westwood
IPC分类号： A61K31/42 , A61P29/00 , C07C235/78 , C07C235/80 , C07C255/60 , C07C323/41 , C07D207/06 , C07D261/18 , C07D295/145 , C07D261/08 , C07D261/12
CPC分类号： C07D295/145 , C07C235/80 , C07C255/60 , C07C323/41 , C07D261/18 , C07C2101/02
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.2 is alkyl of 1 to 3 carbon atoms or cycloalkyl of 3 to 6 carbon atoms, R.sub.3 is --COOR.sub.6, R.sub.6 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.4 is selected from the group consisting of halogen, --CN, --NO.sub.2, --SCH.sub.3, alkylcarbonyl of 1 to 6 alkyl carbon atoms, --CX.sub.3, --WCX.sub.3, --(CH.sub.2).sub.n --CX.sub.3, --(CX.sub.2).sub.n --CX.sub.3, --W--(CX.sub.2).sub.n --CX.sub.3, and --W--(CH.sub.2).sub.n --CX.sub.3, X is halogen, W is --O-- or --S--, n is 1, 2 or 3, R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms and cycloalkyl of 3 to 6 carbon atoms and their salts with non-toxic pharmaceutically acceptable bases with the proviso that if R.sub.2 is alkyl of 1 to 3 carbon atoms, R.sub.1 is hydrogen and R.sub.4 is selected from the group consisting of halogen, --CX.sub.3, --(CH.sub.2).sub.n --CX.sub.3, --(CX.sub.2).sub.n --CX.sub.3, --OCX.sub.3, --O--(CX.sub.2).sub.n --CX.sub.3, and --O--(CH.sub.2).sub.n --CX.sub.3, X is halogen and n is 1, 2 or 3, R.sub.5 cannot be hydrogen having anti-inflammatory activity and their preparation and intermediates.
摘要翻译：选自下式的化合物的化合物其中R 1为氢或1至3个碳原子的烷基，R 2为1至3个碳原子的烷基或3至6个碳原子的环烷基，R 3为 -COOR 6，R 6是氢或1至3个碳原子的烷基，R 4选自卤素，-CN，-NO 2，-SCH 3，1至6个烷基碳原子的烷基羰基，-CX 3，-WCX 3，（CH 2）n -CX 3， - （CX 2）n -CX 3，-W-（CX 2）n -CX 3和-W-（CH 2）n -CX 3，X是卤素，W是-O-或-S-， n为1,2或3，R5选自氢，1至3个碳原子的烷基和3至6个碳原子的环烷基及其与无毒的药学上可接受的碱的盐，条件是如果R2为 1至3个碳原子的烷基，R1是氢，R4选自卤素，-CX3， - （CH2）n -CX3， - （CX2）n -CX3，-OCX3，-O-（CX2） n -CX3和-O-（CH2）n -CX3，X是卤素，n是1,2或3，R5不能是具有抗炎活性的氢及其制备和中间体。

3. 发明授权

US5384423A 3-cycloalkyl-propanamides 失效
标题翻译： 3-环烷基 - 丙酰胺
公开(公告)号：US5384423A
公开(公告)日：1995-01-24
申请号：US51178
申请日：1993-04-22
申请人： Philip T. Hambleton , Charles J. R. Hedgecock , David P. Kay , Elizabeth A. Kuo , Wilfred R. Tully
发明人： Philip T. Hambleton , Charles J. R. Hedgecock , David P. Kay , Elizabeth A. Kuo , Wilfred R. Tully
IPC分类号： A61K31/275 , A61K31/34 , A61K31/357 , A61P29/00 , A61P37/00 , C07C255/19 , C07C255/27 , C07C255/31 , C07C255/60 , C07C323/41 , C07D317/58 , C07D317/66 , C07C255/40
CPC分类号： C07D317/58 , C07C255/27 , C07C255/31 , C07C255/60 , C07C323/41 , C07C2101/02 , C07C2101/04 , C07C2101/06
摘要： A compound selected from the group consisting of all tautomeric forms of a cycloalkyl-propanamide of the formula ##STR1## wherein R.sub.1 is cycloalkyl of 3 to 6 carbon atoms, R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are individually selected from the group consisting of hydrogen, halogen, --NO.sub.2, azido, --CN, alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, --(CH.sub.2).sub.m --CF.sub.3, --O--(CH.sub.2).sub.m --CF.sub.3, --S--(CH.sub.2).sub.m --CF.sub.3, m is an integer from 0 to 3, --CF.sub.2 --Hal, --OCF.sub.2 --Hal, ##STR2## n is an integer from 1 to 3, Hal, Hal.sub.1, and Hal.sub.2 and Hal.sub.3 are individually halogen, and --COR', R' is --OH or alkyl or alkoxy of 1 to 3 carbon atoms or R.sub.4 and R.sub.5 together are --O--CH.sub.2 --O-- and their non-toxic, pharmaceutically acceptable basic salts having anti-inflammatory activity.
摘要翻译：选自下列化合物的化合物：其中R 1为3至6个碳原子的环烷基，R 2为氢或1至3个碳原子的烷基，R 3，R 4， R 5，R 6和R 7分别选自氢，卤素，-NO 2，叠氮基，-CN，烷基，烷氧基和具有1至6个碳原子的烷硫基， - （CH 2）m CF 3，-O- ）m-CF 3，-S-（CH 2）m CF 3，m为0至3的整数，-CF 2-Hal，-OCF 2-Hal，n为1至3的整数，Hal ，Hal1和Hal2和Hal3分别是卤素，-COR'，R'是-OH或1至3个碳原子的烷基或烷氧基，或者R4和R5一起是-O-CH2-O-，它们是无毒的，具有抗炎活性的药学上可接受的碱性盐。

4. 发明授权

US5240960A 3-cycloalkyl-propanamides 失效
标题翻译： 3-环丙基丙酰胺
公开(公告)号：US5240960A
公开(公告)日：1993-08-31
申请号：US785087
申请日：1991-10-30
申请人： Philip T. Hambleton , Charles J. R. Hedgecock , David P. Kay , Elizabeth A. Kuo , Wilfred R. Tully
发明人： Philip T. Hambleton , Charles J. R. Hedgecock , David P. Kay , Elizabeth A. Kuo , Wilfred R. Tully
IPC分类号： A61K31/275 , A61K31/34 , A61K31/357 , A61P29/00 , A61P37/00 , C07C255/19 , C07C255/27 , C07C255/31 , C07C255/60 , C07C323/41 , C07D317/58 , C07D317/66
CPC分类号： C07D317/58 , C07C255/27 , C07C255/31 , C07C255/60 , C07C323/41 , C07C2101/02 , C07C2101/04 , C07C2101/06
摘要： A compound selected from the group consisting of all tautomeric forms of a cycloalky-propanamide of the formula ##STR1## wherein R.sub.1 is cycloalkyl of 3 to 6 carbon atoms, R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are individually selected from the group consisting of hydrogen, halogen, --NO.sub.2, azido, --CN, alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, --(CH.sub.2).sub.m --CF.sub.3, --O--(CH.sub.2).sub.m --CF.sub.3, --S--(CH.sub.2).sub.m --CF.sub.3, m is an integer from 0 to 3, --CF.sub.2 --Hal, --OCF.sub.2 --Hal, ##STR2## n is an integer from 1 to 3, Hal, Hal.sub.1, Hal.sub.2 and Hal.sub.3 are individually halogen, and --COR', R' is --OH or alkyl or alkoxy of 1 to 3 carbon atoms or R.sub.4 and R.sub.5 together are --O--CH.sub.2 --O-- and their non-toxic, pharmaceutically acceptable basic salts having anti-inflammatory activity.
摘要翻译：选自下式的化合物：其中R 1为3至6个碳原子的环烷基，R 2为氢或1至3个碳原子的烷基，R 3，R 4， R 5，R 6和R 7分别选自氢，卤素，-NO 2，叠氮基，-CN，烷基，烷氧基和具有1至6个碳原子的烷硫基， - （CH 2）m CF 3，-O- ）m-CF 3，-S-（CH 2）m CF 3，m为0至3的整数，-CF 2-Hal，-OCF 2-Hal，n为1至3的整数，Hal ，Hal1，Hal2和Hal3分别是卤素，-COR'，R'是-OH或1-3个碳原子的烷基或烷氧基，或者R4和R5一起是-O-CH2-O-及其无毒的，药学上可接受的具有抗炎活性的碱性盐。

5. 发明授权

US5346912A 2-cyano-3-hydroxy-(n-pyridyl)-propenamide compounds 失效
标题翻译： 2-氰基-3-羟基 - （正 - 吡啶基） - 丙烯酰胺化合物
公开(公告)号：US5346912A
公开(公告)日：1994-09-13
申请号：US170372
申请日：1993-12-20
申请人： Elizabeth A. Kuo
发明人： Elizabeth A. Kuo
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4425 , A61P29/00 , A61P35/00 , C07D213/40 , C07D213/75 , C07D213/84 , C07D213/02
CPC分类号： C07D213/75 , Y02P20/55
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein A, B and E are individually selected from the group consisting of .dbd.CH-- and .dbd.N-- with at least one being .dbd.N--, R is selected from the group consisting of cycloalkyl of 3 to 6 carbon atoms, and alkenyl and alkynyl of 2 to 6 carbon atoms, R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.2 and R.sub.3 together are --O--CH.sub.2 --O-- or are individually selected from the group consisting of hydrogen, halogen, --NO.sub.2, --CN, alkyl, alkylthio and alkoxy of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, --COR.sub.4, --(CH.sub.2).sub.m --CX.sub.3, --O--(CH.sub.2).sub.m --CX.sub.3, --S--(CH.sub.2).sub.m --CX.sub.3, --O--(CX.sub.2).sub.m --CX.sub.3 and --S--(CX.sub.2).sub.m --CX.sub.3, R.sub.4 is hydrogen or alkyl or cycloalkyl of up to 6 carbon atoms, X is halogen and m is 0, 1, 2 or 3 and their addition salts with a non-toxic, pharmaceutically acceptable base having anti-flammatory and immulodulatory activity and their preparation.
摘要翻译：选自下列化合物的化合物，其中A，B和E分别选自= CH-和= N-，其中至少一个为N-，R选自由3〜6个碳原子的环烷基和2〜6个碳原子的链烯基和炔基组成，R1为氢或1〜3个碳原子的烷基，R2和R3一起为-O-CH2-O-，或者为分别选自氢，卤素，-NO 2，-CN，烷基，烷硫基和1至6个碳原子的烷氧基，具有3至6个碳原子的环烷基，-COR 4， - （CH 2）m -CX 3，-O - （CH2）m-CX3，-S-（CH2）m-CX3，-O-（CX2）m-CX3和-S-（CX2）m-CX3，R4是氢或最多6碳的烷基或环烷基原子，X是卤素，m是0,1,2或3，它们与具有抗炎和免疫调节活性的无毒的药学上可接受的碱的加成盐及其制备。

6. 发明授权

US5476866A Isoxazoles 失效
标题翻译：异恶唑
公开(公告)号：US5476866A
公开(公告)日：1995-12-19
申请号：US293840
申请日：1994-08-22
申请人： Elizabeth A. Kuo , Robert Westwood
发明人： Elizabeth A. Kuo , Robert Westwood
IPC分类号： A61K31/42 , A61P19/02 , A61P29/00 , A61P35/00 , C07D261/18 , C07D263/30
CPC分类号： C07D261/18
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms; R.sub.2 is cycloalkyl of 3 to 6 carbon atoms; R.sub.4 is selected from the group consisting of halogen, nitrile, nitro, --SCH.sub.3, -alkylcarbonyl of 1 to 6 carbon atoms, cycloalkylcarbonyl of 3 to 6 carbon atoms, --CX.sub.3, --WCX.sub.3, --(CH.sub.2).sub.n CX.sub.3, --(CX.sub.2).sub.n CX.sub.3, --W(CX.sub.2).sub.n CX.sub.3 and a --W(CH.sub.2).sub.n CX.sub.3, in which X is halogen, W is oxygen or sulfur, and n is 1, 2 or 3; and R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms and cycloalkyl of 3 to 6 carbon atoms; with the proviso that if R.sub.5 is hydrogen, R.sub.4 is not --SCH.sub.3 or --CF.sub.3 and their non-toxic pharmaceutically acceptable salts having anti-prolifera-tive, anti-inflammatory and anti-tumor activity.
摘要翻译：选自下式的化合物的化合物其中R 1是氢或1至3个碳原子的烷基; R 2是3至6个碳原子的环烷基; R 4选自卤素，腈，硝基，-SCH 3 - 具有1至6个碳原子的烷基羰基，3至6个碳原子的环烷基羰基，-CX 3，-WCX 3， - （CH 2）n CX 3， - （CX 2） nCX3，-W（CX2）nCX3和-W（CH2）nCX3，其中X是卤素，W是氧或硫，n是1,2或3; 并且R 5选自氢，1至3个碳原子的烷基和3至6个碳原子的环烷基; 条件是如果R5是氢，R4不是-SCH3或-CF3及其无毒的药学上可接受的盐，其具有抗增殖，抗炎和抗肿瘤活性。

7. 发明授权

US5312830A 3-cycloalkyl-prop-2-enamides 失效
标题翻译： 3-环烷基 - 丙-2-烯酰胺
公开(公告)号：US5312830A
公开(公告)日：1994-05-17
申请号：US944830
申请日：1992-09-14
申请人： Elizabeth A. Kuo
发明人： Elizabeth A. Kuo
IPC分类号： A61K31/275 , A61K31/277 , A61P29/00 , A61P37/00 , C07C255/23 , C07C255/31 , C07C317/32 , C07C317/40 , C07C323/41 , C07D213/75 , C07D317/40 , C07D317/58 , C07D317/64 , C07C255/34
CPC分类号： C07D213/75 , C07C255/31 , C07C317/40 , C07C323/41 , C07D317/58 , C07C2101/02
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms, W is selected from the group consisting of --O--, --S--, --SO-- and --SO.sub.2 --, Z and Y are --CH-- or one is --CH-- and the other is --N--, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are individually selected from the group consisting of hydrogen, halogen, methoxy, methylthio, alkyl of 1 to 4 carbon atoms, --WCF.sub.3, --CF.sub.3, --NO.sub.2, --CN--, --W--(CH.sub.2).sub.n --CF.sub.3, --W--(CF.sub.2).sub.n --CF.sub.3, --(CF.sub.2).sub.n --CF.sub.3 and --(CH.sub.2).sub.n --CX.sub.3, is an integer from 1 to 3, X is a halogen or R.sub.3 and R.sub.4 together are --O--(CH.sub.2)--O-- and R.sub.2, R.sub.5 and R.sub.6 are as defined above, R.sub.7 and R.sub.8 are individually hydrogen or alkyl of 1 to 6 carbon atoms, R.sub.9 is cycloalkyl of 3 to 6 carbon atoms and their non-toxic, pharmaceutically acceptable salts with bases.
摘要翻译：选自下列化学式的化合物的化合物其中R 1是氢或1至3个碳原子的烷基，W选自-O - ， - S - ， - SO-和 -SO 2 - ，Z和Y是-CH-或一个是-CH-，另一个是-N-，R 2，R 3，R 4，R 5和R 6分别选自氢，卤素，甲氧基，甲硫基， 1至4个碳原子的烷基，-WCF 3，-CF 3，-NO 2，-CN-，-W-（CH 2）n -CF 3，-W-（CF 2）n -CF 3， - （CF 2）n -CF 3和 - （CH2）n-CX3为1〜3的整数，X为卤素或R3和R4一起为-O-（CH2）-O-，R2，R5和R6如上所定义，R7和R8分别为氢或1至6个碳原子的烷基，R9是3至6个碳原子的环烷基，它们与碱的无毒的药学上可接受的盐。

8. 发明授权

US5506249A Isoxazoles 失效
标题翻译：异恶唑
公开(公告)号：US5506249A
公开(公告)日：1996-04-09
申请号：US350255
申请日：1994-12-05
申请人： Elizabeth A. Kuo , Robert Westwood
发明人： Elizabeth A. Kuo , Robert Westwood
IPC分类号： A61K31/42 , A61P19/02 , A61P29/00 , A61P35/00 , C07D261/18 , A61K31/41 , C07D261/06
CPC分类号： C07D261/18
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms; R.sub.2 is cycloalkyl of 3 to 6 carbon atoms; R.sub.4 is selected from the group consisting of halogen, nitrile, nitro, --SCH.sub.3, -alkylcarbonyl of 1 to 6 carbon atoms, cycloalkylcarbonyl of 3 to 6 carbon atoms, --CX.sub.3, 'WCX.sub.3, --(CH.sub.2).sub.n CX.sub.3, --(CX.sub.2).sub.n CX.sub.3, --W(CX.sub.2).sub.n CX.sub.3 and a --W(CH.sub.2).sub.n CX.sub.3, in which X is halogen, W is oxygen or sulfur, and n is 1, 2 or 3; and R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms and cycloalkyl of 3 to 6 carbon atoms; with the proviso that if R.sub.5 is hydrogen, R.sub.4 is not --SCH.sub.3 or --CF.sub.3 and their non-toxic pharmaceutically acceptable salts having anti-prolifera-tive, anti-inflammatory and anti-tumor activity.
摘要翻译：选自下式的化合物的化合物其中R 1是氢或1至3个碳原子的烷基; R 2是3至6个碳原子的环烷基; R 4选自卤素，腈，硝基，-SCH 3 - 具有1至6个碳原子的烷基羰基，3至6个碳原子的环烷基羰基，-CX 3，WCX 3， - （CH 2）n CX 3， - （CX 2） nCX3，-W（CX2）nCX3和-W（CH2）nCX3，其中X是卤素，W是氧或硫，n是1,2或3; 并且R 5选自氢，1至3个碳原子的烷基和3至6个碳原子的环烷基; 条件是如果R5是氢，R4不是-SCH3或-CF3及其无毒的药学上可接受的盐，其具有抗增殖，抗炎和抗肿瘤活性。

9. 发明授权

US5017574A Novel imidazobenzodiazepines 失效
标题翻译：新型咪唑并二氮杂
公开(公告)号：US5017574A
公开(公告)日：1991-05-21
申请号：US516194
申请日：1990-04-26
申请人： Charles J. R. Hedgecock , Stuart D. Jones , Elizabeth A. Kuo
发明人： Charles J. R. Hedgecock , Stuart D. Jones , Elizabeth A. Kuo
IPC分类号： A61K31/55 , A61P3/04 , A61P25/18 , A61P25/28 , C07D487/04
CPC分类号： C07D487/04
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein the R.sub.1 s are the same and are alkyl of 1 to 3 carbon atoms or together are alkylene of 2 to 5 carbon atoms, X, Y and W are individually --O-- or --S--, R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and phenyl optionally substituted with at least one member of the group consisting of halogen, alkyl and alkoxy of 1 to 3 carbon atoms and --CF.sub.3, R.sub.4 and R.sub.5 are individually selected from the group consisting of hydrogen, halogen, --OH, alkyl and alkoxy of 1 to 3 carbon atoms and --CF.sub.3 with the proviso that when R.sub.1 and R.sub.2 are alkyl, X and Y are the same and their non-toxic, pharmaceutically acceptable acid addition salts having benzodiazepine inverse agonist properties.
摘要翻译：选自下式的化合物的化合物其中R 1相同并且是1至3个碳原子的烷基或一起是2至5个碳原子的亚烷基，X，Y和W分别是 -O-或-S-，R 2是氢或1至3个碳原子的烷基，R 3选自氢，1至5个碳原子的烷基和任选被至少一个成员组成的组的苯基，的卤素，具有1至3个碳原子的烷基和烷氧基和-CF 3，R 4和R 5分别选自氢，卤素，-OH，具有1至3个碳原子的烷基和烷氧基和-CF 3，条件是当R1和R2是烷基时，X和Y是相同的，它们是具有苯并二氮杂反向激动剂性质的无毒的药学上可接受的酸加成盐。

10. 发明授权

US4895866A Anti-inflammatory imidazole compounds 失效
标题翻译：抗炎咪唑化合物
公开(公告)号：US4895866A
公开(公告)日：1990-01-23
申请号：US271732
申请日：1988-11-15
申请人： Dankwart C. Fenske , Elizabeth A. Kuo , Wilfred R. Tully
发明人： Dankwart C. Fenske , Elizabeth A. Kuo , Wilfred R. Tully
IPC分类号： C07D233/64 , A61K31/415 , A61K31/505 , A61P29/00 , A61P37/00 , C07D233/68 , C07D233/70 , C07D233/84 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D233/84 , C07D487/04
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of ##STR2## and --C.tbd.C--R' and the remaining substituents are as defined hereinbelow and its non-toxic, pharmaceutically acceptable acid additon salts having anti-inflammatory activity and their preparation.

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