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1. 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。

2. 发明授权

US4547507A Benzothiopyranopyridinones 失效
标题翻译：苯并噻喃并吡啶酮
公开(公告)号：US4547507A
公开(公告)日：1985-10-15
申请号：US512964
申请日：1983-07-12
申请人： David A. Rowlands , Roger J. Gillespie , Ian R. Ager , Stephen Clements-Jewery , Colin R. Gardner
发明人： David A. Rowlands , Roger J. Gillespie , Ian R. Ager , Stephen Clements-Jewery , Colin R. Gardner
IPC分类号： A61K31/435 , A61P25/18 , A61P25/24 , A61P25/26 , C07D211/78 , C07D495/04 , C07D513/14 , A61K31/38 , C07D513/22
CPC分类号： C07D495/04 , C07D211/78
摘要： Novel benzothiopyranopyridinones of the formula ##STR1## wherein A,B,C and D are individually selected from the group consisting of hydrogen, alkyl and alkoxy of 1 to 6 carbon atoms, nitro, halogen, amino and acylamino of 2 to 7 carbon atoms or A and B or C and D taken with the carbon atoms to which they are attached form a benzene ring, R is selected from the group consisting of hydrogen and R', R' is selected from the group consisting of alkyl of 1 to 9 carbon atoms, alkenyl of 2 to 9 carbon atoms optionally substituted with an --OH, cycloalkyl of 3 to 9 carbon atoms, phenyl, aralkyl of 7 to 9 carbon atoms and --(CH.sub.2).sub.n --Z, n is an integer from 1 to 4, Z is selected from the group consisting of cycloalkyl and cycloalkenyl of 3 to 9 carbon atoms, dioxanyl, 2-oxobenzimidazolyl, benzoyl, halo substituted benzoyl, cyano, alkoxy carbonyl of 2 to 7 carbon atoms and carbamoyl and their non-toxic, pharmaceutically acceptable acid addition salts having antipsychotic and antidepressant and antidopaminergic activity.
摘要翻译：式其中A，B，C和D分别选自氢原子，1至6个碳原子的烷基和烷氧基，硝基，卤素，氨基和2至7个碳原子的酰基氨基的新的苯并噻喃并吡啶酮或A和B或C和D与其所连接的碳原子取代形成苯环，R选自氢和R'，R'选自1至9的烷基碳原子数为2〜9的碳原子的链烯基，任选被-OH取代，3〜9个碳原子的环烷基，苯基，7〜9个碳原子的芳烷基和 - （CH2）nZ，n为1〜4的整数， Z选自环烷基和3至9个碳原子的环烯基，二烷基，2-氧代苯并咪唑基，苯甲酰基，卤素取代的苯甲酰基，氰基，2-7个碳原子的烷氧基羰基和氨基甲酰基，它们的无毒，药学上可接受的具有抗精神病药和抗抑郁药和抗生素的酸加成盐抗病毒活性。

3. 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。

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