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Pirazolopirimidona and pirazolopiridona as inhibitors of tanquirasa
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
申请号:
ARP130101979
公开号:
AR091272A1
申请日:
2013.06.05
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
The compounds of formula (1) are useful in the treatment of cancer. Claim 1: Compound of formula (1) wherein: Q and X are, independently at each occurrence, N or CH; R¹ is selected from the group consisting of hydrogen, C₁₋₆ alkyl,hydroxyalkyl C₁₋₆,dihydroxy-C₁₋₆-alkyl,1,1,1-endosulfan-4-international labour organization or tetrahydropyridine-4-international Labour Organization; R2 is other formula (2) or (3);And selected from cr8308; r83090 or nr830808;where R⁵ is hydrogen, C₁₋₆ alkyl,-Oh o-cn; R3 was selected from (I) H (II) c83218c83326262 tar group;(Iii) haloalquilo C(IV) halogen, (V) Alcoy c83218331-832626;(vi) S (O) ₂R³ᵃ where R³ᵃ is C₁₋₆ alkyl,cycloalkyl C₃₋₆,C₁₋₃-alkyl-cycloalkyl-C₃₋₆ or NH₂ or (vii) CONR³ᶜR³ᶜ in which R³ᵇ and R³ᶜ are independently hydrogen, C₁₋₃-alkyl or R³ᵇ and R³ᶜ together with the nitrogen to which they are attached form a cyclic amine; R⁴ is selected from the group consisting of: (i) hydrogen, (ii) C₁₋₆ alkyl,(iii) C₁₋₆ haloalkyl optionally substituted with hydroxyl, (iv) C₃₋₇ cycloalkyl,(V) cicloalquil C -alquilo C(Vi) bicicloalquilo C(vii) the residue of formula (4) in which R⁶ is independently selected from the group consisting of: (a) C₁₋₆ alkyl,(b) C₁₋₆ haloalkyl optionally substituted with hydroxyl, (c) C₁₋₆ hydroxyalkyl,(D) dihidroxi-alquilo C(E) alcoxi C -alquilo C(F) cicloalquilo C(G) acilo C(H) halo (i) ciano (j) NO(K) carboxilo (l) alcoxicarbonilo C(m) Conr8308; (m) conr8308; (74r8308; (75808); ercycloalkyl C₃₋₆,C₁₋₃-alkyl cycloalkyl Cilo or NH₂,(o) 8308; 7495; 8308;where R⁴ᵇ and R⁴ᶜ are independently C₁₋₆ alkyl or hydrogen, (p) OR⁴ᵈ where R⁴ᵈ is selected from the group consisting of: (i) hydrogen, (ii) C₁₋₆ alkyl,(Iii) alcoxi C -alquilo C(Iv) hidroxialquilo Coptionally further replacing said hydroxyalkyl with halogen, (v) dihydroxy-C₁₋₆-alkyl,(vi) (alkylene) ₂₋₆NR⁴ᵉCR⁴ᶠ in which R⁴ᵉ and R⁴ᶠ are independently hydrogen or C₁₋₆ alkyl or R⁴ᵉ and R⁴ᶠ together with the nitrogen to which they are attached form a cyclic amine option
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