DUSTIN SIEGEL,RICHARD L. MACKMAN,MICHAEL ONEIL HANRAHAN CLARKE
申请号：
ARP150102330
公开号：
AR101280A1
申请日:
2015.07.22
申请国别(地区):
AR
年份:
2016
代理人:
摘要：
Formulations, methods and compounds of thieno [3,2-d] pyrimidine, furo [3,2-d] pyrimidine, and substituted pyrrolo [3,2-d] pyrimidine of formula (1) are provided herein for the treatment of infections by Pneumovirinae virus, including respiratory syncytial virus infections, as well as methods and intermediates for the synthesis of the thieno [3,2-d] pyrimidine compound, furo [3,2-d] pyrimidine, and pyrrolo [3,2- d] substituted pyrimidine. Claim 1: A compound of the formula (1),or a pharmaceutically acceptable salt thereof, characterized in that: X is selected from the group of O, S, NH, or N (C₁₋₆ alkyl)；R1 was selected from group H, ch832323,f. Ll and nh832222；R2 was selected from F, Cl, or7491；NHR7491,CN, N₃ y；R3 is selected from CN, or74919；C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, -CH₂-O-C₁₋₆ alkyl, -CH₂-S-C₁₋₆ alkyl, C₃₋₄ cycloalkyl, azido, halogen, C₁₋₃ haloalkyl, SRᵃ ,-CH₂-C₃₋₄ cycloalkyl, -O-C₃₋₄ cycloalkyl, and -O-C₁₋₃ haloalkyl； or when R² is ORᵃ,Two or74919 teams at position 2 and position 3 can be combined with furario circle, and the selected structure of formula group is connected with it (2)；R83088 was selected from H-C (= O) r8310a group；-C (3DO) ORY-c (= O) No. 8310； r8311；O r83088 is a formula group (3)；There, each is O, s, NR, 8314n (o) (R),No, No.N (O) (OR)O N-Nr2；W1 and W2,If taken together, - Y3 (r6966) 83223； - Y3；O 1 W1 or W2 with No. 3 underwater Xi is - Y3, 1 W1 or W2 is formula (4)；Or W1 and W2 are a set of independent formulas (4),Where: each Y1, independent, O, s, NR, 8314n (o) (R),No, No.N (O) (OR)O N-Nr2；Each two are independent links, or cr832222,-O-CR832222--NR N (O) (R)No, No.N (O) (OR)N-Nr2S S-S S (O)o S (O)each Y³ is independently O, S, or NR； M1 is 0, 1, 2, or 3； each Rˣ is independently Rʸ or the formula (5) wherein: each M2a, M2b, and M2c is independently 0 or 1； M2d is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12； each Rʸ is independently H, F, Cl, Br, I, OH, R, -C (= Y¹) R, -C (= Y¹) OR, -C (= Y¹) N (R) ₂,-N (R)- N (R)-SR -S (O)
