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US 7,030,134 B2Granted
Pyrazolopyridinyl pyridine and pyrimidine therapeutic compounds
AssigneeSmithKline Beecham Corporation
InventorsKristjan Gudmundsson, Brian A. Johns
Life of this patent
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Abstract
The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
Claims22
A compound of formula (I):
- wherein:
- R1 is selected from the group consisting of halo, Ay, Het, —NR7R8, —NR7Ay, —NHHet, —NHR10Ay and —NHR10Het;
- each R7 and R8 are the same or different and are independently selected from the group consisting of H, alkyl, alkenyl, cycloalkyl, cycloalkenyl, —OR9, —C(O)R9, —CO2R9, —C(O)NR9R11, —C(S)NR9R11, —C(NH)NR9R11, —SO2R10, —SO2NR9R11, —R10cycloalkyl, —R10OR9, —CH(R10OR9)2, —R10C(O)R9, —R10CO2R9, —R10C(O)NR9R11, —R10C(S)NR9R11, —R10C(NH)NR9R11, —R10SO2R10, —R10SO2NR9R11, —R10SO2NHCOR9, —R10NR9R11, —R10NHCOR9, —R10NHSO2R9 and —R10NHC(NH)NR9R11 and;
- each R9 and R11 are the same or different and are independently selected from the group consisting of H, alkyl, cycloalkyl, —R10cycloalkyl, —R10OH, —R10(OR10)w where w is 1–10, and —R10NR10R10;
- each R10 is the same or different and is independently selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl and cycloalkenyl;
- Ay is aryl;
- Het is a 5- or 6-membered heterocyclic or heteroaryl group;
- n is 0, 1 or 2;
- R2 is selected from the group consisting of halo, alkyl, alkenyl, cycloalkyl, cycloalkenyl, Ay, Het, —OR7, —OAy, —OHet, —OR10Het, —S(O)nR9, —S(O)nAy, —S(O)nHet, —S(O)nNR7R8, —NR7R8, —NHHet, —NHR10Ay, —NHR10Het, —R10NR7R8 and —R10NR7Ay;
- Y is CH;
- R3 and R4 are the same or different and are each independently selected from the group consisting of H, halo, alkyl, alkenyl, cycloalkyl, Ay, Het, —OR7, —OAy, —C(O)R7, C(O)Ay, —CO2R7, —CO2Ay, —SO2NHR9, —NR7R8, —NR7Ay, —NHHet, —NHR10Het —R10OR7, —R10OAy, —R10NR7R8 and —R10NR7Ay;
- q is 0, 1, 2, 3, 4 or 5;
- each R5 is the same or different and is independently selected from the group consisting of halo, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, Ay, Het, —OR7, —OAy, —OHet, —C(O)R9, —C(O)Ay, —C(O)Het, —CO2R9, —C(O)NR7R8, —C(O)NR7Ay, —C(O)NHR10Het, —C(S)NR9R11, —C(NH)NR7R8, —C(NH)NR7Ay, —S(O)nR9, —S(O)2NR7R8, —S(O)2NR7Ay, —NR7R8, —NR7Ay, —NHHet, —NHR10Ay, —NHR10Het, —R10cycloalkyl, —R10OR9, —R10C(O)R9, —R10CO2R9, —R10C(O)NR9R11, —R10C(S)NR9R11, —R10C(NH)NR9R11, —R10SO2R9, —R10SO2NR9R11, —R10SO2NHCOR9, —R10NR7R8, —R10NR7 Ay, —R10NHC(NH)NR9R11, cyano, nitro and azido;
- or
- two adjacent R5 groups together with the atoms to which they are bonded form a C5-6 cycloalkyl or aryl;
- p is 1, 2 or 3;
- and
- each R6 is the same or different and is independently selected from the group consisting of halo, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, Ay, Het, —OR7, —OAy, —OHet, —OR10Ay, —OR10Het, —C(O)R9, —C(O)Ay, —C(O)Het, —CO2R9, —C(O)NR7R8, —C(O)NR7Ay, —C(O)NHR10Ay, —C(O)NHR10Het, —C(S)NR9R11, —C(NH)NR7R8, —C(NH)NR7Ay, —S(O)nR9, —S(O)nAy, —S(O)nHet, —S(O)2NR7R8, —S(O)2NR7Ay, —NR7R8, —NR7Ay, —NHHet, —NHR10Ay, —NHR10Het, —R10cycloalkyl, —R10Ay, —R10Het, —R10OR9, —R10—O—C(O)R9, —R10—O—C(O)Ay, —R10—O—C(O)Het, —R10—O—S(O)nR9, —R10C(O)R9, —R10CO2R9, —R10C(O)NR9R11, —R10C(S)NR9R11, —R10C(NH)NR9R11, —R10SO2R9, —R10SO2NR9R11, —R10SO2NHCOR9, —R10NR7R8, —R10NR7Ay, —R10NHC(NH)NR9R11, cyano, nitro and azido;
- or
- two adjacent R6 groups together with the atoms to which they are bonded form a C5-6 cycloalkyl or a 5- or 6-membered heterocyclic group containing 1 or 2 heteroatoms;
- or
- R6 is in the 6 position and R6 and R1 together with the atoms to which they are bonded form a C5-6 cycloalkyl or a 5- or 6-membered heterocyclic group containing 1 or 2 heteroatoms;
- wherein when Y is CH, R3 is not —NR7Ay;
- or a pharmaceutically acceptable salt or solvate thereof.
21 more elements
Dependencies are inferred from the claim text.