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    • 3. 发明申请
    • SMALL MOLECULE INHIBITORS OF INFLUENZA A AND B VIRUS AND RESPIRATORY SYNCYTIAL VIRUS REPLICATION
    • 流感病毒A和B病毒的小分子抑制剂和呼吸道同种病毒复制
    • WO2010128163A2
    • 2010-11-11
    • PCT/EP2010056304
    • 2010-05-07
    • PIKE PHARMA GMBHKESSLER ULRICHRANADHEERA CHARLENEJOUBERT MURIELGIETHLEN BRUNOGARRIDO FABRICE
    • KESSLER ULRICHRANADHEERA CHARLENEJOUBERT MURIELGIETHLEN BRUNOGARRIDO FABRICE
    • C07D333/22
    • C07D417/04C07D333/22C07D409/04C07D417/12C07D417/14
    • Compounds according to the invention are 2-(3-Q5-4-Q4-5-Q3-thien-2-yl)-4-R3-5-R2-1,3-thiazol, 2-(3-Q5-4-Q4- 5-Q3-fur-2-yl)-4-R3-5-R2-1,3-thiazol, 2-(3-Q5-4-Q4-5-Q3-thien-2-yl)-5-R2-1,3,4-thiadiazol, 2-(3-Q5-4-Q4-5-Q3-fur-2-yl)-5-R2-1,3,4-thiadiazol, 2-(2-Q3-4-Q5-1,3-thiazol-5-yl)4-R3-5-R2-1,3-thiazol, 2-(2-Q3-4-Q5-1,3-oxazol-5-yl)4- R3-5-R2-1,3-thiazol, 2-(4-Q4-5-Q3-1,3-thiazol-2-yl)4-R3-5-R2-1,3-thiazol, 2-(4-Q4-5-Q3-1,3-oxazol-2-yl)4-R3-5- R2-1,3-thiazol, 2-(4-Q5-5-Q4-3-Q2-thien-3-yl)4-R3-5-R2-1,3-thiazol, 2-(4-Q5-5-Q4-3-Q2-fur-3-yl)4-R3-5-R2-1,3-thiazol, 2-benzo[b]thiophen-2-yl4-R3-5-R2-1,3-thiazol, 2-benzo[b]furan-2-yl4-R3-5-R2-1,3-thiazol, 2-(3-Q5-4- Q4-5-Q3-thien-2-yl)-6-Z2-1,3-benzo[d]thiazol, 2-(3-Q5-4-Q4-5-Q3-thien-2-yl)-6-Z2-1,3-benzo[d]oxazol, 2-(2-Z5-3- Z6-4-Z7-phenyl)4-R3-5-R2-1,3-thiazol, 2-(5-Z8-6-Z7-3-pyridyl)4-R3-5-R2-1,3-thiazol, 2-(3-R3-4-R2-phenyl)-3-Q5- 4-Q4-5-Q3-thiophen, 2-(3-R3-4-R2-phenyl)-3-Q5-4-Q4-5-Q3-furan, N-Z9-N-(4-R3-5-R2-1,3-thiazol-2-yl)-3-Q5-4-Q4- 5-Q3-thien-2-yl-carboxamid, N-Z9-N-(4-R3-5-R2-1,3-thiazol-2-yl)-3-Q5-4-Q4-5-Q3-fur-2-yl-carboxamid, 5-(3-Q5-4- Q4-5-Q3-thien-2-yl)4-R4-2-R2-1,3-thiazol, 5-(3-Q5-4-Q4-5-Q3-fur-2-yl)4-R4-2-R2-1,3-thiazol, 2-(3-Q5-4-Q4-5-Q3- thien-2-yl)-3-R4-4-R3-5-R2-thiophen, 2-(3-Q5-4-Q4-5-Q3-fur-2-yl)-3-R4-4-R3-5-R2-thiophen; where R2, R3, R4, Q2, Q3, Q4, Q5, Z2, Z5, Z6, Z7, Z8 and Z9 are as defined in the description. Said compounds are particularly advantageous for treating and/or preventing influenza type A and/or influenza type B infections in humans, mammals and/or birds, and for treating and/or preventing respiratory syncytial virus infections in humans, mammals and/or birds.
    • 根据本发明的化合物是2-(3-Q5-4-Q4-5-Q3-噻吩-2-基)-4-R3-5-R2-1,3-噻唑,2-(3-Q5-4 -Q4-5-Q3-呋喃-2-基)-4-R3-5-R2-1,3-噻唑,2-(3-Q5-4-Q4-5-Q3-噻吩-2-基) - 2-(3-Q5-4-Q4-5-Q3-呋喃-2-基)-5-R2-1,3,4-噻二唑,2-(2 -Q3-4-Q5-1,3-噻唑-5-基)4-R3-5-R2-1,3-噻唑,2-(2-Q3-4-Q5-1,3-恶唑-5-基) 吡啶-2-基)-4-(3-(3-(4-(4-(4-(甲基氨基-2-甲氧基苯基) ,2-(4-Q4-5-Q3-1,3-恶唑-2-基)4-R3-5-R2-1,3-噻唑,2-(4-Q5-5-Q4-3-Q2 噻吩-3-基)4-R3-5-R2-1,3-噻唑,2-(4-Q5-5-Q4-3-Q2-呋喃-3-基)4-R3-5-R2- 1,3-苯并[b]噻吩-2-基-4-R3-5-R2-1,3-噻唑,2-苯并[b]呋喃-2-基] -4-R3-5-R2-1, 2-(3-Q5-4-Q4-5-Q3-噻吩-2-基)-6-Z2-1,3-苯并[d]噻唑,2-(3-Q5-4-Q4) -5-Q3-噻吩-2-基)-6-Z2-1,3-苯并[d]恶唑,2-(2-Z5-3-Z6-4-Z7-苯基)4-R3-5-R2 -2-(5-Z8-6-Z7-3-吡啶基)4-R3-5-R2-1,3-噻唑,2-(3-R3-4-R2-苯基) - 3-Q5-4-Q4-5-Q3-噻吩,2-(3-R3-4-R2-苯基)-3-Q5-4-Q4-5-Q3-呋喃,N-Z9-N-(4 -R3-5-R2-1,3-噻唑-2-基)-3-Q5-4-Q4-5-Q 3-噻吩-2-基甲酰胺,N-Z9-N-(4-R3-5-R2-1,3-噻唑-2-基)-3-Q5-4-Q4-5-Q3-毛 - 2-(3-(3-Q5-4-Q4-5-Q3-噻吩-2-基)4-R4-2-R2-1,3-噻唑,5-(3-Q5-4- Q4-5-Q3-呋喃-2-基)4-R4-2-R2-1,3-噻唑,2-(3-Q5-4-Q4-5-Q3-噻吩-2-基)-3- R4-4-R3-5-R2-噻吩,2-(3-Q5-4-Q4-5-Q3-呋喃-2-基)-3-R4-4-R3-5-R2-噻吩; 其中R2,R3,R4,Q2,Q3,Q4,Q5,Z2,Z5,Z6,Z7,Z8和Z9如说明书中所定义。 所述化合物在人,哺乳动物和/或鸟类中治疗和/或预防A型流感和/或B型流感以及用于治疗和/或预防人,哺乳动物和/或鸟类中的呼吸道合胞病毒感染特别有利。