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    • 4. 发明申请
    • SMALL MOLECULE INHIBITORS OF INFLUENZA A AND B VIRUS AND RESPIRATORY SYNCYTIAL VIRUS REPLICATION
    • 小儿甲型和乙型流感病毒与呼吸道合胞病毒复制的小分子抑制剂
    • WO2010128163A3
    • 2010-11-11
    • PCT/EP2010/056304
    • 2010-05-07
    • PIKE PHARMA GMBHKESSLER, UlrichRANADHEERA, CharlèneJOUBERT, MurielGIETHLEN, BrunoGARRIDO, Fabrice
    • KESSLER, UlrichRANADHEERA, CharlèneJOUBERT, MurielGIETHLEN, BrunoGARRIDO, Fabrice
    • C07D333/22C07D409/04C07D417/04C07D417/12C07D417/14G01N33/68
    • Compounds according to the invention are 2-(3-Q 5 -4-Q 4 -5-Q 3 -thien-2-yl)-4-R 3 -5-R 2 -1,3-thiazol, 2-(3-Q 5 -4-Q 4 - 5-Q 3 -fur-2-yl)-4-R 3 -5-R 2 -1,3-thiazol, 2-(3-Q 5 -4-Q 4 -5-Q 3 -thien-2-yl)-5-R 2 -1,3,4-thiadiazol, 2-(3-Q 5 -4-Q 4 -5-Q 3 -fur-2-yl)-5-R 2 -1,3,4-thiadiazol, 2-(2-Q 3 -4-Q 5 -1,3-thiazol-5-yl)4-R 3 -5-R 2 -1,3-thiazol, 2-(2-Q 3 -4-Q 5 -1,3-oxazol-5-yl)4- R 3 -5-R 2 -1,3-thiazol, 2-(4-Q 4 -5-Q 3 -1,3-thiazol-2-yl)4-R 3 -5-R 2 -1,3-thiazol, 2-(4-Q 4 -5-Q 3 -1,3-oxazol-2-yl)4-R 3 -5- R 2 -1,3-thiazol, 2-(4-Q 5 -5-Q 4 -3-Q 2 -thien-3-yl)4-R 3 -5-R 2 -1,3-thiazol, 2-(4-Q 5 -5-Q 4 -3-Q 2 -fur-3-yl)4-R 3 -5-R 2 -1,3-thiazol, 2-benzo[b]thiophen-2-yl4-R 3 -5-R 2 -1,3-thiazol, 2-benzo[b]furan-2-yl4-R 3 -5-R 2 -1,3-thiazol, 2-(3-Q 5 -4- Q 4 -5-Q 3 -thien-2-yl)-6-Z 2 -1,3-benzo[d]thiazol, 2-(3-Q 5 -4-Q 4 -5-Q 3 -thien-2-yl)-6-Z 2 -1,3-benzo[d]oxazol, 2-(2-Z 5 -3- Z 6 -4-Z 7 -phenyl)4-R 3 -5-R 2 -1,3-thiazol, 2-(5-Z 8 -6-Z 7 -3-pyridyl)4-R 3 -5-R 2 -1,3-thiazol, 2-(3-R 3 -4-R 2 -phenyl)-3-Q 5 - 4-Q 4 -5-Q 3 -thiophen, 2-(3-R 3 -4-R 2 -phenyl)-3-Q 5 -4-Q 4 -5-Q 3 -furan, N-Z 9 -N-(4-R 3 -5-R 2 -1,3-thiazol-2-yl)-3-Q 5 -4-Q 4 - 5-Q 3 -thien-2-yl-carboxamid, N-Z 9 -N-(4-R 3 -5-R 2 -1,3-thiazol-2-yl)-3-Q 5 -4-Q 4 -5-Q 3 -fur-2-yl-carboxamid, 5-(3-Q 5 -4- Q 4 -5-Q 3 -thien-2-yl)4-R 4 -2-R 2 -1,3-thiazol, 5-(3-Q 5 -4-Q 4 -5-Q 3 -fur-2-yl)4-R 4 -2-R 2 -1,3-thiazol, 2-(3-Q 5 -4-Q 4 -5-Q 3 - thien-2-yl)-3-R 4 -4-R 3 -5-R 2 -thiophen, 2-(3-Q 5 -4-Q 4 -5-Q 3 -fur-2-yl)-3-R 4 -4-R 3 -5-R 2 -thiophen; wherein R 2 , R 3, R 4 , Q 2 , Q 3 , Q 4 , Q 5 , Z 2 , Z 5 , Z 6 , Z 7 , Z 8 and Z 9 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-Q 5 -4-Q 4 -5 -Q 3) -2-噻吩-2-基)-4-R 3 -5-R 2 -1,3-噻唑,2-(3-Q 5) -4-Q 4 -5-Q 3 - 呋喃-2-基)-4-R 3 -5- R 2 -1,3-噻唑,2-(3-Q 5 -4-Q 4 -5 -Q 3) - 噻吩-2-基)-5-R 2 -1,3,4-噻二唑,2-(3-Q 5 -4-Q -5-Q 3 -fur-2-yl)-5-R 2 -1,3,4-噻二唑,2- (2-Q 3 -4-Q 5 -1,3-噻唑-5-基)-4-R 3 -5-R 2-(2-Q 3 -4-Q 5 -1,3-恶唑-5-基)-1,3-噻唑,2-(2-Q 3 -4 -Q 5 -1,3-恶唑-5-基) (4-Q 4 -Q-4-Q-4)-5-R 2 -1,3-噻唑,2-(4-Q 4 -5 -Q -1,3-噻唑-2-基)-4-R 3 -5-R 2 -1,3-噻唑,2 - (4-Q 4 -5-Q 3 -1,3-恶唑-2-基)-4-R 3 -5- R 2 -1,3-噻唑,2-(4-Q 5 -5 -Q 4 -3-Q 2) - 噻吩-3-基)4-R 3 -5-R 2 -1,3-噻唑,2-(4-Q- 5 -5-Q 4 -3-Q 2-呋喃-3-基)-4-R 3 -5-R 2 -1,3-噻唑,2-苯并[b]噻吩-3-基, 2-苯并呋喃-2-基] -4-呋喃-2-基] -4,5-二氢吡啶并[2,3-b]呋喃-2-基] -5-R 2 -1,3-噻唑,2-(3-Q 5 -4 -Q 4 -5) -β-噻吩-2-基)-6-Z 2 -1,3-苯并[d]噻唑,2-(3-Q 5) 功能 -4-Q 4 -5-Q 3 噻吩-2-基)-6-Z 2 -1, 3-苯并[d]恶唑,2-(2-Z5-Z-4-Z7-苯基)4 -R 5 -5-R 2 -1,3-噻唑,2-(5-Z 8 -6 -Z) 3-(3-吡啶基)-4-R 3 -5-R 2 -1,3-噻唑,2-(3-R 3) -4-R 2 - 苯基)-3-Q 5 -4-Q 4 -Q-5-Q- 2-(3-R 3 -4-R 2 - 苯基)-3-Q 5 - 4-Q 4 -5-Q 3 - 呋喃,NZ 9-N-(4-R 3) -5-R 2 -1,3-噻唑-2-基)-3-Q 5 -4-Q 4-5 - N 3 - 噻吩-2-基 - 甲酰胺,NZ 9-N-(4-R 3 -5-R 2) 功能 -1,3-噻唑-2-基)-3- -5-Q-4-Q-5-Q 3 - 呋喃-2-基 - 甲酰胺,5-(3-Q- -5-Q-4-Q-5-Q 3 -thien-2-yl)4-R 4 -s- 2-R 2 -1,3-噻唑,5-(3-Q 5 -4 -Q 4 -5 -Q) 呋喃-2-基)4-R 4 -2-R 2 -1,3-噻唑,2-(3-Q- -5-Q 3 - 噻吩-2-基)-3-R 4 - -4-R 3 -5-R 2 - 噻吩,2-(3-Q 5 -4 -Q 4) / SUP> -5-Q 3 -fur -2-基)-3-R 4 -4-R 3 -5-R 2 - 噻吩; 其中R 2,R 3,R 4,Q 2,Q 3,R 4,R 4, Q 4,Q 5,Z 2,Z 5,Z 6,Z 5,Z 5,Z 5,Z 5,Z 5, ,Z 7,Z 8和Z 9如说明书中所定义。 所述化合物对于治疗和/或预防人类,哺乳动物和/或鸟类中的A型和/或B型流感感染以及治疗和/或预防人类,哺乳动物和/或鸟类中的呼吸道合胞体病毒感染是特别有利的。