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1. 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。

2. 发明授权

US4654338A 1,2,4-thiadiazines 失效
标题翻译： 1,2,4-噻二嗪
公开(公告)号：US4654338A
公开(公告)日：1987-03-31
申请号：US716050
申请日：1985-03-26
申请人： Stuart D. Jones , Wilfred R. Tully , Peter D. Kennewell
发明人： Stuart D. Jones , Wilfred R. Tully , Peter D. Kennewell
IPC分类号： C07D233/61 , A61K31/415 , A61K31/54 , A61P25/20 , C07D285/18 , C07D413/04 , C07D417/04
CPC分类号： C07D285/18
摘要： Novel 1,2,4-thiadiazines of the formula ##STR1## wherein R.sub.3 is selected from the group consisting of hydrogen, --OH, --CF.sub.3, alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms optionally substituted with alkyl of 1 to 6 carbon atoms and ##STR2## R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms or taken together with the nitrogen to which they are attached form a saturated heterocycle of 4 to 8 carbon atoms optionally containing a heteroatom of the group consisting of --O--, --S-- and ##STR3## and R' is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.5 is ##STR4## R.sub.4 is selected from the group consisting of hydrogen, halogen and alkyl and alkoxy of 1 to 3 carbon atoms, R.sub.6 is selected from the group consisting of hydrogen, halogen and alkyl of 1 to 3 carbon atoms with the proviso that R.sub.6 may represent halogen only when R.sub.3 is hydrogen, --OH, alkyl and alkoxy of 1 to 6 carbon atoms or cycloalkyl of 3 to 6 carbon atoms optionally substituted with alkyl of 1 to 6 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable anxiolytic activity and novel intermediates.
摘要翻译：式Ⅰ的新的1,2,4-噻二嗪其中R 3选自氢，-OH，-CF 3，烷基，烷氧基和1至6个碳原子的烷硫基，3至6个碳原子的环烷基任选被1至6个碳原子的烷基取代的原子，且R 1和R 2分别选自氢和1至3个碳原子的烷基，或与它们所连接的氮一起形成饱和杂环 4至8个碳原子，任选地含有-O - ， - S-和＆lt; IMAGE＆gt;的杂原子，R'是氢或1至3个碳原子的烷基，R 5选自由氢，卤素和1至3个碳原子的烷基和烷氧基组成的基团，R 6选自氢，卤素和1至3个碳原子的烷基，条件是R 6可以仅在R3是氢时表示卤素， -OH，1至6个碳原子的烷基和烷氧基或3至6个碳的环烷基任选被1至6个碳原子的烷基取代的原子及其无毒的药学上可接受的具有显着抗焦虑活性的酸加成盐和新的中间体。

3. 发明授权

US4643999A 2-substituted imidazo[1,2-c]pyrimidines having anxiolytic properties 失效
标题翻译：具有抗焦虑性质的2-取代咪唑并[1,2-c]嘧啶
公开(公告)号：US4643999A
公开(公告)日：1987-02-17
申请号：US681948
申请日：1984-12-14
申请人： Wilfred R. Tully
发明人： Wilfred R. Tully
IPC分类号： A61K31/505 , A61P25/20 , C07C45/51 , C07C45/63 , C07C49/76 , C07D487/04 , C07D471/02
CPC分类号： C07D487/04 , C07C45/515 , C07C45/63 , C07C49/76
摘要： Novel imidazo[1,2-c]pyrimidines of the formula ##STR1## wherein R is an aryl of 6 to 12 carbon atoms, R.sub.1 is selected from the group consisting of hydrogen and alkyl, alkoxy and alkylthio of 1 to 5 carbon atoms when R.sub.2 and R.sub.3 together form a carbon-nitrogen bond or R.sub.1 and R.sub.2 together are .dbd.0 when R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and alkenyl of 2 to 5 carbon atoms, R.sub.4 is selected from the group consisting of alkoxy and alkylthio of 1 to 5 carbon atoms, R.sub.5 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anxiolytic properties.
摘要翻译：式I的新型咪唑并[1,2-c]嘧啶其中R是6至12个碳原子的芳基，R 1选自氢和1至5个碳原子的烷基，烷氧基和烷硫基当R3选自氢，1至5个碳原子的烷基和2至5个碳原子的烯基时，当R 2和R 3一起形成碳 - 氮键或R 1和R 2一起为= 0时，R 4选自由1至5个碳原子的烷氧基和烷硫基组成的组，R5选自氢和1至5个碳原子的烷基及其无毒的药学上可接受的具有抗焦虑性质的酸加成盐。

4. 发明授权

US4472400A Triazoloquinazolones having antihistaminic and bronchospasmolytic activity 失效
标题翻译：具有抗组胺和支气管扩张活性的三氮唑喹唑啉酮
公开(公告)号：US4472400A
公开(公告)日：1984-09-18
申请号：US420798
申请日：1982-09-21
申请人： Wilfred R. Tully , Robert Westwood , David A. Rowlands , Stephen Clements-Jewery
发明人： Wilfred R. Tully , Robert Westwood , David A. Rowlands , Stephen Clements-Jewery
IPC分类号： A61K31/505 , A61K31/535 , A61K31/55 , A61P11/08 , A61P43/00 , C07D239/95 , C07D239/96 , C07D487/04
CPC分类号： C07D487/04 , C07D239/95 , C07D239/96
摘要： Novel triazoloquinazolones of the formula ##STR1## wherein R and R' are individually selected from the group consisting of hydrogen, halogen, nitro and alkyl and alkoxy of 1 to 3 carbon atoms, Y is selected from the group consisting of alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 4 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, aryl of 6 to 8 carbon atoms and aralkyl of 7 to 8 carbon atoms, B is an alkylene of 1 to 3 carbon atoms, X is selected from the group consisting of ##STR2## R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, aryl of 6 to 8 carbon atoms, aralkyl of 7 to 8 carbon atoms, aminoalkyl of 2 to 4 carbon atoms, mono- and dialkylaminoalkyl with each alkyl having 2 to 4 carbon atoms, piperidinoalkyl of 1 to 4 alkyl carbon atoms, morpholinoalkyl of 1 to 4 alkyl carbon atoms and piperazinylalkyl of 1 to 4 alkyl carbon atoms or R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached form a saturated mono- or bicyclic heterocyclic ring with 4 to 8 carbon atoms optionally substituted with 1 to 2 methyls and optionally containing in the ring a heteroatom selected from --O--, --S-- and ##STR3## and R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, hydroxyalkyl of 1 to 3 carbon atoms, alkoxycarbonyl of 2 to 5 carbon atoms, aryl of 6 to 8 carbon atoms and aralkyl of 7 to 8 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antihistaminic and bronchospasmolytic activity and their preparation and intermediates.
摘要翻译：新颖的式（I）的三唑并喹唑酮其中R和R'分别选自氢，卤素，硝基和1至3个碳原子的烷基和烷氧基，Y选自1至 6个碳原子，2至4个碳原子的烯基，3至8个碳原子的环烷基，6至8个碳原子的芳基和7至8个碳原子的芳烷基，B是1至3个碳原子的亚烷基，选择X 来自由 R 1和R 2组成的组分别选自氢，1至6个碳原子的烷基，3至8个碳原子的环烷基，6至8个碳原子的芳基，7至8个的芳烷基碳原子数2〜4个的氨基烷基，碳原子数2〜4的烷基的单烷氧基氨基烷基和二烷基氨基烷基，1〜4个碳原子的哌啶子基烷基，1〜4个的烷基碳原子的吗啉代烷基，1〜4个碳原子的哌嗪基烷基原子或R1和R2与它们一起的氮一起重新连接形成具有4至8个碳原子的饱和单环或双环杂环，任选被1至2个甲基取代，并且任选地在环中含有选自-O - ， - S-和的杂原子，并且R 3选自由氢，1〜3个碳原子的烷基，1〜3个碳原子的羟基烷基，2〜5个碳原子的烷氧基羰基，6〜8个碳原子的芳基和7〜8个碳原子的芳烷基组成的组及其无毒的，具有抗组胺和支气管痉挛分解活性的药学上可接受的酸加成盐及其制备和中间体。

5. 发明授权

US4925846A 2-thiazolyl-imidazo[1,2,-a]pyrimidines 失效
标题翻译： 2-噻唑基 - 咪唑并[1,2-a]嘧啶
公开(公告)号：US4925846A
公开(公告)日：1990-05-15
申请号：US57493
申请日：1987-06-03
申请人： Robert M. J. Deacon , Roger J. Gillespie , Colin R. Gardner , Wilfred R. Tully
发明人： Robert M. J. Deacon , Roger J. Gillespie , Colin R. Gardner , Wilfred R. Tully
IPC分类号： A61K31/505 , A61P3/04 , A61P25/20 , A61P25/26 , 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 R.sub.1 is thiazol-2-yl optionally substituted by 1 or 2 alkyl of 1 to 3 carbon atoms optionally substituted by one or more fluorine or --COOAlk, Alk is alkyl of 1 to 3 carbon atoms, R.sub.2 and R.sub.3 are individually selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms and alkenyl of 2 to 5 carbon atoms or R.sub.2 and R.sub.3 together form alkylene of 3 to 5 carbon atoms, X is oxygen or sulfur and R.sub.4 is alkyl of 1 to 3 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having minor tranquillizing activity and useful for the treatment of obesity and cognitive impairment.
摘要翻译：选自下列化合物的化合物其中R 1为任选被1或2个碳原子数为1或2的烷基取代的噻唑-2-基，其任选被一个或多个氟或-COOAlk，Alk 是1〜3个碳原子的烷基，R2和R3分别选自氢，1〜3个碳原子的烷基和2〜5个碳原子的链烯基，或R2和R3一起形成3〜5个碳原子的亚烷基 X是氧或硫，R4是1至3个碳原子的烷基，它们的无毒的药学上可接受的酸加成盐具有较小的镇静作用，可用于治疗肥胖和认知障碍。

6. 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.

7. 发明授权

US4810828A Anti-inflammatory imidazole compounds 失效
标题翻译：抗炎咪唑化合物
公开(公告)号：US4810828A
公开(公告)日：1989-03-07
申请号：US080407
申请日：1987-07-31
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 the remaining substituents are as defined hereinbelow and its non-toxic, pharmaceutically acceptable acid addition salts having anti-inflammatory activity and their preparation.
摘要翻译：选自下列化学式的化合物的化合物其中R 1选自下列基团的化合物，其余的取代基如下文所定义，及其无毒的药学上可接受的酸加成盐，其具有抗炎症活动及其制备。

8. 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。

9. 发明授权

US4703049A 2-(1,2,4-oxadiazol-5-yl) and 2-(1,3,4-thiadiazol-2-yl-imidazo[1,2-a]pyrimidines 失效
标题翻译： 2-（1,2,4-恶二唑-5-基）和2-（1,3,4-噻二唑-2-基 - 咪唑并[1,2-a]嘧啶
公开(公告)号：US4703049A
公开(公告)日：1987-10-27
申请号：US808844
申请日：1985-12-12
申请人： Roger J. Gillespie , Wilfred R. Tully
发明人： Roger J. Gillespie , Wilfred R. Tully
IPC分类号： A61K31/505 , A61K31/519 , A61P25/20 , A61P25/22 , C07D487/04 , A61K31/415 , C07D235/02
CPC分类号： C07D487/04
摘要： Novel compounds selected from the group consisting of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of 1,2,4-oxadiazol-5-yl and 1,3,4-thiadiazol-2-yl, both optionally substituted with alkyl of 1 to 3 carbon atoms or alkenyl of 2 to 5 carbon atoms and 1,2,4-oxadiazol-3-yl and 1,3,4-oxadiazol-2-yl, both optionally substituted with alkenyl of 2 to 5 carbon atoms, alkyl of 1 to 3 carbon atoms or alkyl of 1 to 3 carbon atoms substituted with at least one fluorine, R.sub.2 and R.sub.3 are individually selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms and alkenyl of 2 to 5 carbon atoms or together form alkylene of 3 to 5 carbon atoms, X is selected from the group consisting of --O-- and --S--, R.sub.4 is alkyl of 1 to 3 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anxiolytic sedative and hypnotic activity and a novel process and novel intermediates therefor.
摘要翻译：选自下式的新型化合物其中R 1选自1,2,4-恶二唑-5-基和1,3,4-噻二唑-2-基，其均为任选取代的具有1至3个碳原子的烷基或2至5个碳原子的链烯基和1,2,4-恶二唑-3-基和1,3,4-恶二唑-2-基，其任选被2至5个的烯基取代碳原子数1〜3的烷基或被至少一个氟取代的1〜3个碳原子的烷基，R2和R3分别选自氢，1〜3个碳原子的烷基和2〜 5个碳原子或一起形成3至5个碳原子的亚烷基，X选自-O-和-S-，R4是1至3个碳原子的烷基及其无毒的药学上可接受的酸加成盐具有抗焦虑镇静和催眠活性，并具有新颖的过程和新颖的中间体。

10. 发明授权

US4390697A Process for the preparation of triazoloquinazolinones 失效
标题翻译：三唑并喹唑啉酮的制备方法
公开(公告)号：US4390697A
公开(公告)日：1983-06-28
申请号：US317858
申请日：1981-11-03
申请人： Wilfred R. Tully
发明人： Wilfred R. Tully
IPC分类号： C07D239/95 , C07D487/04
CPC分类号： C07D487/04 , C07D239/95
摘要： A novel process for the preparation of triazoloquinazolinones of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, fluorine, chlorine, bromine, --NO.sub.2, --CF.sub.3, --CH.sub.3 and --OCH.sub.3, n is an integer from 2 to 5, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and hydroxyalkyl of 1 to 5 carbon atoms or taken together with the nitrogen atom which they are attached form a saturated heterocycle optionally containing another heteroatom and optionally substituted with at least one member of the group consisting of hydroxy, alkyl and hydroxy alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, acyl of an aliphatic carboxylic acid of 1 to 5 carbon atoms, alkoxycarbonyl of 2 to 6 carbon atoms, aryl and aryl substituted with halogen or --CF.sub.3 and their non-toxic, pharmaceutically acceptable acid addition salts having antihistaminic and bronchospasmolytic activity and novel intermediates.
摘要翻译：一种制备式（I）的三唑并喹唑啉酮的新方法，其中X选自氢，氟，氯，溴，-NO 2，-CF 3，-CH 3和-OCH 3，n是2的整数至5，R 1和R 2分别选自氢，1至5个碳原子的烷基和1至5个碳原子的羟烷基，或与它们所连接的氮原子一起形成饱和杂环，任选地含有另外的杂原子并且任选被至少一个由1-5个碳原子的羟基，烷基和羟基烷基，3至6个碳原子的环烷基，1至5个碳原子的脂族羧酸的酰基，2个烷氧基羰基，至6个碳原子，被卤素或-CF 3取代的芳基和芳基及其具有抗组胺和支气管痉挛分解活性的无毒，药学上可接受的酸加成盐和新的中间体。

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