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1. 发明公开

EP0039919A1 Benzoxazole and benzothiazole derivatives with anti-allergic activity 有权
标题翻译：苯并恶唑和苯并噻唑衍生物抗逆转录酶Wirkung。
公开(公告)号：EP0039919A1
公开(公告)日：1981-11-18
申请号：EP81103497.4
申请日：1981-05-07
申请人： USV PHARMACEUTICAL CORPORATION
发明人： Brown, Richard E. , Georgiev, Vasil St. , Loev, Bernard
IPC分类号： A61K31/42 , A61K31/425 , C07D263/58 , C07D277/68 , C07D413/12 , C07D498/04 , C07D513/04
CPC分类号： C07D263/58 , C07D265/36 , C07D277/68
摘要： An anti-allergic compound of the formula:
wherein,

X is S or O R 1 and R 2 are each H, R 3 , OR 4 , halogen, cyano, COOR 4 , methanesulfonyl, nitro, trifluoromethyl or taken together, methylenedioxy, wherein R 3 is loweralkyl orcycloalkyl of 3 to 7 carbon atoms and R 4 is hydrogen or lower alkyl; and
R is -Z-O-R 3 ; -Z-N(R 5 R 6 ); Z 1 -O-Z 2 -N(R 5 R 6 ); -Z- heterocycle; -Z 1 -O-Z 2 -heterocycle; or-Z-O-C 6 H 4 R 1 wherein each of R 5 and R 6 are hydrogen or lower alkyl, or when taken together with the nitrogen to which they are attached R 5 and R 6 form a nitrogen-heterocyclic ring, R 1 and R 3 have the meaning hereinbefore described, and Z,Z 1 and Z 2 are each branched or unbranched alkylene chain containing from 2 to about 6 carbon atoms in the principal chain and a total of up to about 12 carbon atoms; Z 1 and Z 2 when taken together with a hetero atom form a saturated heterocyclic ring; and heterocycle represents a heterocyclic ring containing one or more of the hetero atoms, oxygen, nitrogen and sulfur and acid addition and conjugate salts thereof.
摘要翻译：一种下式的抗过敏化合物：其中，... X为S或O ... R 1和R 2各自为H，R 3，OR 4，卤素，氰基，COOR 4，甲磺酰基，硝基，三氟甲基或一起取代亚甲二氧基其中R3是3-7个碳原子的低级烷基或环烷基，R4是氢或低级烷基; 和... R是-Z-O-R3; -Z-N（R 5 R 6）; ž<1> -O-Z <2> -N（R 5 R 6）; -Z-杂环; -Z <1> -O-Z <2> - 杂环; 或-ZO-C 6 H 4 R 1，其中R 5和R 6各自为氢或低级烷基，或者当与其连接的氮一起连接时，R 5和R 6形成氮杂环，R 1和R 3具有上述含义，Z Z 1和Z 2分别是在主链中含有2至约6个碳原子且总共至多约12个碳原子的支链或非支链亚烷基链; Z 1和Z 2与杂原子一起形成饱和杂环; 杂环表示含有一个或多个杂原子，氧，氮和硫及其酸加成和共轭盐的杂环。

2. 发明公开

EP0039920A3 Triazaloquinoxalin-1,4-diones 有权
标题翻译： Triazaloquinoxalin -1,4-二酮
公开(公告)号：EP0039920A3
公开(公告)日：1982-01-27
申请号：EP81103498
申请日：1981-05-07
申请人： USV PHARMACEUTICAL CORPORATION
发明人： Brown, Richard E. , Georgiev, Vasil St. , Kropp, Philip , Loev, Bernard
IPC分类号： C07D487/04 , C07D471/14 , C07D495/14 , C07D491/14 , C07D241/44 , A61K31/495 , C07D471/04 , C07D249/00 , C07D241/00 , C07D221/00 , C07D333/00 , C07D307/00
CPC分类号： C07D471/04 , C07D241/44 , C07D471/14 , C07D487/04
摘要： Anti-allergic compounds of the formulae
wherein,
X is S or O; R 1 and R 2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, aralkyl, sulfonamido, halogen, alkoxy, alkenyloxy, alkynyloxy, cyano, hydroxy, acyloxy, nitro, amino, alkylamino, alkanoylamino, carbalkoxyamino, methanesulfonyl, carboxy, carbalkoxy, trihalomethyl, or taken together, methylenedioxy; R 3 and R 4 is hydrogen, alkyl, alkenyl, alkynyl, aryl, acyl, aralkyl, cycloalkyl, cycloalkyl CH 2 -, or carbalkoxy; and Z forms a heterocyclic ring with the two carbon atoms to which it is attached;and intermediates for their preparation.
摘要翻译：下式的抗过敏化合物其中X是S或O; 烷基，链烯基，炔基，环烷基，芳基，芳烷基，亚磺酰氨基，卤素，烷氧基，烯氧基，炔氧基，氰基，羟基，酰氧基，硝基，氨基，烷基氨基，烷酰基氨基，三卤代甲基，或者合在一起，亚甲二氧基; R3和R4是氢，烷基，链烯基，炔基，芳基，酰基，芳烷基，环烷基，环烷基CH2-或烷氧羰基; Z与其所连接的两个碳原子形成杂环;以及用于其制备的中间体。

3. 发明授权

EP0039920B1 Triazaloquinoxalin-1,4-diones 有权
标题翻译： Triazaloquinoxalin -1,4-二酮
公开(公告)号：EP0039920B1
公开(公告)日：1984-07-25
申请号：EP81103498.2
申请日：1981-05-07
申请人： USV PHARMACEUTICAL CORPORATION
发明人： Brown, Richard E. , Georgiev, Vasil St. , Kropp, Philip , Loev, Bernard
IPC分类号： C07D487/04 , C07D471/14 , A61K31/495
CPC分类号： C07D471/04 , C07D241/44 , C07D471/14 , C07D487/04

4. 发明授权

EP0039919B1 Benzoxazole and benzothiazole derivatives with anti-allergic activity 有权
标题翻译：具有抗过敏活性的苯并唑和苯并噻唑衍生物
公开(公告)号：EP0039919B1
公开(公告)日：1983-12-28
申请号：EP81103497.4
申请日：1981-05-07
申请人： USV PHARMACEUTICAL CORPORATION
发明人： Brown, Richard E. , Georgiev, Vasil St. , Loev, Bernard
IPC分类号： A61K31/42 , A61K31/425 , C07D263/58 , C07D277/68 , C07D413/12 , C07D498/04 , C07D513/04
CPC分类号： C07D263/58 , C07D265/36 , C07D277/68

5. 发明公开

EP0039920A2 Triazaloquinoxalin-1,4-diones 有权
标题翻译： Triazolochinoxalin -1,4-二酮。
公开(公告)号：EP0039920A2
公开(公告)日：1981-11-18
申请号：EP81103498.2
申请日：1981-05-07
申请人： USV PHARMACEUTICAL CORPORATION
发明人： Brown, Richard E. , Georgiev, Vasil St. , Kropp, Philip , Loev, Bernard
IPC分类号： C07D487/04 , C07D471/14 , A61K31/495
CPC分类号： C07D471/04 , C07D241/44 , C07D471/14 , C07D487/04
摘要： Anti-allergic compounds of the formulae
wherein,

X is S or O;
R 1 and R 2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, aralkyl, sulfonamido, halogen, alkoxy, alkenyloxy, alkynyloxy, cyano, hydroxy, acyloxy, nitro, amino, alkylamino, alkanoylamino, carbalkoxyamino, methanesulfonyl, carboxy, carbalkoxy, trihalomethyl, or taken together, methylenedioxy;
R 3 and R 4 is hydrogen, alkyl, alkenyl, alkynyl, aryl, acyl, aralkyl, cycloalkyl, cycloalkyl CH 2 -, or carbalkoxy; and
Z forms a heterocyclic ring with the two carbon atoms to which it is attached;and intermediates for their preparation.
摘要翻译：式的抗过敏化合物，其中X为S或O; R1和R2是氢，烷基，烯基，炔基，环烷基，芳基，芳烷基，亚磺酰氨基，卤素，烷氧基，烯氧基，炔氧基，氰基，羟基，酰氧基，硝基，氨基，烷基氨基，烷酰基氨基，烷氧基氨基，甲磺酰基，羧基，三卤代甲基，或一起取代亚甲二氧基; R3和R4是氢，烷基，烯基，炔基，芳基，酰基，芳烷基，环烷基，环烷基，环烷基CH2-或碳烷氧基; Z与其所连接的两个碳原子形成杂环; 和中间体的制备。

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