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DERIVATIVES OF 1 H-PYRAZOLO[3,4-B]PYRIDINE AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF PROLIFERATIVE DISORDERS
专利权人:
GALAPAGOS NV
发明人:
SANIÈRE, LAURENT RAYMOND MAURICE,HUCK, JACQUES,DYKES, GRAEME JAMES,SCHMITT, BENOÎT ANTOINE,BLANC, JAVIER,BUTLER, ANNA SARA,BEAUMONT, STÉPHANE NICOLAS ALAIN,BONNATERRE, FLORENCE MARIE-EMILIE
申请号:
SG11201601157X
公开号:
SG11201601157XA
申请日:
2014.08.18
申请国别(地区):
SG
年份:
2016
代理人:
摘要:
Claim 1: a compound according to formula (1), in which X is n or CH, NH L - (c = o) - O - (c = o) NH - CN - r\u00b9 is alkyl, Halo, c\u2081\u208b\u2084 optionally substituted with one or More groups r\u2076\u1d43 selected independently alkoxy optionally substituted with one or c\u2081\u208b\u2084 V R\u2076\u1d47 Aryan groups selected independently, c\u2083\u208b\u2084 cycloalkyl alkyl, phenyl, SO\u2082 c\u2081\u208b\u2084 - or - nr\u2077\u1d43r\u2077\u1d47 R\u00b2 is H,Ciclopropilo c\u2081\u208b\u2084 (alkyl, optionally substituted with one or more c\u2081\u208b\u2084 halo) or alkoxy r\u00b3 is ch\u2083 - or CL -, ch\u2082ch\u2083 r\u2074 is optionally substituted with a c\u2081\u208b\u2082 alkyl substituted with an alkyl c\u2081\u208b\u2082 Oh, oh and a heterocicloalquilo of 5-6 members comprising one Or two heteroatoms selected independently of N, o and SC\u2083\u208b\u2086 cycloalkyl optionally replaced with a Oh each r\u2076\u1d43 is Oh, Halo, or c\u2081\u208b\u2084 alkoxy each r\u2076\u1d47 is Oh, Halo, c\u2081\u208b\u2084 - nr\u2078\u1d43r\u2078\u1d47, alkoxy, or heterocicloalquilo of 5-6 members comprising one or two heteroatoms selected independently of N, o and S, or Pcionalmente substituted with an alkyl c\u2081\u208b\u2084 each r\u2077\u1d43, r\u2077\u1d47 is selected independentlyC\u2081\u208b\u2084 H and alkyl and each r\u2078\u1d43 or r\u2078\u1d47 is selected, so independent of H and alkyl c\u2081\u208b\u2084.Reivindicación 1: Un compuesto de acuerdo con la fórmula (1), en donde X es N o CH L es -NH(C=O)- o -C(=O)NH- R¹ es -CN, halo, alquilo C₁₋₄ opcionalmente sustituido con uno o varios grupos R⁶ᵃ seleccionados de modo independiente, alcoxi C₁₋₄ opcionalmente sustituido con uno o varios grupos R⁶ᵇ seleccionados de modo independiente, cicloalquilo C₃₋₄, fenilo, -SO₂-alquilo C₁₋₄, o -NR⁷ᵃR⁷ᵇ R² es H, ciclopropilo, alquilo C₁₋₄ (opcionalmente sustituido con uno o varios halo) o alcoxi C₁₋₄ R³ es -CH₃, -CH₂CH₃ o Cl R⁴ es alquilo C₁₋₂ opcionalmente sustit
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