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11. 发明授权

US4350695A Antihistaminic and bronchospasmolytic triazoloquinazolinones 失效
标题翻译：抗组胺和支气管痉挛性三唑并喹唑啉酮
公开(公告)号：US4350695A
公开(公告)日：1982-09-21
申请号：US234544
申请日：1981-02-13
申请人： Robert Westwood , Wilfred R. Tully , Robert Murdoch
发明人： Robert Westwood , Wilfred R. Tully , Robert Murdoch
IPC分类号： A61K31/505 , A61P11/08 , A61P37/08 , A61P43/00 , C07D239/95 , C07D487/04
CPC分类号： C07D487/04 , C07D239/95 , Y10S514/826
摘要： Novel triazoloquinazolinones of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, --NO.sub.2, methyl, methoxy and --CF.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 and alkyl and hydroxyalkyl of 1 to 5 carbon atoms and taken together with the nitrogen atom to 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 hydroxyalkyl 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 and aryl optionally substituted with a halogen or --CF.sub.3 and their non-toxic, pharmaceutically acceptable acid addition salts having antihistaminic and bronchospasmolytic activity and their preparation.
摘要翻译：式（I）的新型三唑并喹唑啉酮其中X选自氢，卤素，-NO 2，甲基，甲氧基和-CF 3，n为2至5的整数，R 1和R 2各自独立地选自由氢和烷基取代的基团和碳原子数为1〜5的羟基烷基和与它们相连的氮原子一起形成饱和杂环，任选地含有另外的杂原子，任选被至少一个羟基取代的基团取代， 1至5个碳原子的烷基和羟基烷基，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至6个碳原子的烷氧基羰基和任选被卤素或-CF 3取代的芳基，具有抗组胺和支气管扩张活性的无毒，药学上可接受的酸加成盐及其制备。

12. 发明授权

US5063229A Imidazolo [1,2-a]pyrimidines and medical use thereof 失效
标题翻译：咪达唑仑（1,2-A）吡咯烷酮及其医药用途
公开(公告)号：US5063229A
公开(公告)日：1991-11-05
申请号：US435078
申请日：1989-11-09
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## and its non-toxic, pharmaceutically acceptable acid addition salts having anti-inflammatory activity and their preparation.

13. 发明授权

US4588720A Imidazo[1,2-a]pyrimidines 失效
标题翻译：咪唑并[1,2-a]嘧啶
公开(公告)号：US4588720A
公开(公告)日：1986-05-13
申请号：US734590
申请日：1985-05-15
申请人： Wilfred R. Tully
发明人： Wilfred R. Tully
IPC分类号： A61K31/519 , A61P25/18 , A61P25/24 , C07D239/46 , C07D239/70 , C07D239/95 , C07D487/04 , A61K31/415 , C07D239/84 , C07D471/02
CPC分类号： C07D239/47 , C07D239/70 , C07D239/95 , C07D487/04
摘要： Novel imidazo[1,2-a]pyrimidines of the formula ##STR1## wherein R is selected from the group consisting of alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, cycloalkylalkyl of 4 to 12 carbon atoms, aryl of 6 to 12 carbon atoms, thienyl and pyridyl, each of said group being optionally substituted with at least one member of the group consisting of halogen, alkyl of 1 to 5 carbon atoms, alkoxy and alkylthio of 1 to 5 carbon atoms, trifluoromethyl, amino, alkylamino of 1 to 5 alkyl carbon atoms and dialkylamino with alkyl of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 5 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, cycloalkylalkyl of 4 to 12 carbon atoms, benzyl and phenethyl, or taken together form alkylene of 3 to 5 carbon atoms, each of said groups being optionally substituted with at least one member of the group consisting of halogen, alkyl of 1 to 5 carbon atoms, alkoxy and alkylthio of 1 to 5 carbon atoms, trifluoromethyl, amino, alkylamino of 1 to 5 alkyl carbon atoms and dialkylamino with alkyls of 1 to 5 carbon atoms, X is selected from the group consisting of oxygen and sulfur and R.sub.3 is alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts, having anxiolytic activity and novel intermediates.
摘要翻译：具有下式的新型咪唑并[1,2-a]嘧啶其中R选自1至8个碳原子的烷基，2至8个碳原子的链烯基，3至7个碳原子的环烷基， 4至12个碳原子的环烷基烷基，6至12个碳原子的芳基，噻吩基和吡啶基，所述基团各自任选被至少一个由卤素，1至5个碳原子的烷基，烷氧基和烷硫基 1至5个碳原子的三氟甲基，氨基，1至5个碳原子的烷基氨基和二烷基氨基与1至5个碳原子的烷基，R 1和R 2分别选自氢，1至8个碳原子的烷基 2至5个碳原子的烯基，3至7个碳原子的环烷基，4至12个碳原子的环烷基烷基，苄基和苯乙基，或一起形成3至5个碳原子的亚烷基，所述基团各自任选被由卤素组成的组中的至少一个成员 1至5个碳原子的烷基，1至5个碳原子的烷氧基和烷硫基，三氟甲基，氨基，1至5个烷基碳原子的烷基氨基和二烷基氨基与1至5个碳原子的烷基，X选自氧硫和R3是1至5个碳原子的烷基和它们的无毒的药学上可接受的酸加成盐，具有抗焦虑活性和新的中间体。

14. 发明授权

US4532243A Imidazo(1,2-a)pyrimidines and their salts useful for treating anxiety 失效
标题翻译：咪唑（1,2-a）嘧啶及其盐可用于治疗焦虑症
公开(公告)号：US4532243A
公开(公告)日：1985-07-30
申请号：US526046
申请日：1983-08-24
申请人： Wilfred R. Tully
发明人： Wilfred R. Tully
IPC分类号： A61K31/519 , A61P25/18 , A61P25/24 , C07D239/46 , C07D239/70 , C07D239/95 , C07D487/04 , A61K31/505
CPC分类号： C07D239/47 , C07D239/70 , C07D239/95 , C07D487/04
摘要： Novel imidazo[1,2-a]pyrimidines of the formula ##STR1## wherein R is selected from the group consisting of alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, cycloalkylalkyl of 4 to 12 carbon atoms, aryl of 6 to 12 carbon atoms, thienyl and pyridyl, each of said group being optionally substituted with at least one member of the group consisting of halogen, alkyl of 1 to 5 carbon atoms, alkoxy and alkylthio of 1 to 5 carbon atoms, trifluoromethyl, amino, alkylamino of 1 to 5 alkyl carbon atoms and dialkylamino with alkyl of 1 to 5 carbons atoms, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 5 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, cycloalkylalkyl of 4 to 12 carbon atoms, benzyl and phenethyl, or taken together form alkylene of 3 to 5 carbon atoms, each of said groups being optionally substituted with at least one member of the group consisting of halogen, alkyl of 1 to 5 carbon atoms, alkoxy and alkylthio of 1 to 5 carbon atoms, trifluoromethyl, amino, alkylamino of 1 to 5 alkyl carbon atoms and dialkylamino with alkyls of 1 to 5 carbon atoms, X is selected from the group consisting of oxygen and sulfur and R.sub.3 is alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts, having anxiolytic activity and novel intermediates.
摘要翻译：具有下式的新型咪唑并[1,2-a]嘧啶其中R选自1至8个碳原子的烷基，2至8个碳原子的链烯基，3至7个碳原子的环烷基， 4至12个碳原子的环烷基烷基，6至12个碳原子的芳基，噻吩基和吡啶基，所述基团各自任选被至少一个由卤素，1至5个碳原子的烷基，烷氧基和烷硫基 1至5个碳原子的三氟甲基，氨基，1至5个碳原子的烷基氨基和二烷基氨基与1至5个碳原子的烷基，R 1和R 2分别选自氢，1至8个碳原子的烷基 2至5个碳原子的烯基，3至7个碳原子的环烷基，4至12个碳原子的环烷基烷基，苄基和苯乙基，或一起形成3至5个碳原子的亚烷基，所述基团各自任选被由卤素组成的组中的至少一个成员，a 1至5个碳原子的烷基，1至5个碳原子的烷氧基和烷硫基，三氟甲基，氨基，1至5个烷基碳原子的烷基氨基和二烷基氨基与1至5个碳原子的烷基，X选自氧硫和R3是1至5个碳原子的烷基和它们的无毒的药学上可接受的酸加成盐，具有抗焦虑活性和新的中间体。

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