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US 2010/0076015 A1Published application
Aminopyridine Derivatives
AssigneeVantia Limited
InventorsDavid Michael Evans, Christine Elizabeth Allan, John Horton, David Philip Rooker
Life of this patent
Estimating the term…
Abstract
The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (such as asthma or COPD); and methods of treating patients with such compounds; wherein R1-R11 are as defined herein.
Claims13
A compound of formula (I):
- wherein:
- R1 and R2 are independently selected from H, OH, (C1-C10)alkyl, (C1-C6)alkoxy, (C2-C6)alkenyl, (C3-C10)cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aryl(C1-C4)alkyl- and heteroaryl(C1-C4)alkyl-;
- R3 is selected from H, (C1-C10)alkyl and (C2-C6)alkenyl;
- R4 and R5 are selected from H, (C1-C10)alkyl, (C2-C6)alkenyl, (C3-C10)cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aryl(C1-C4)alkyl- and heteroaryl(C1-C4)alkyl-;
- R6 and R7 are selected from H, (C1-C10)alkyl, (C2-C6)alkenyl, (C3-C10)cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aryl(C1-C4)alkyl-, aryl(C2-C4)alkenyl-, heteroaryl(C1-C4)alkyl-, —SO2(C1-C6)alkyl, —SO2aryl and —SO2arylC1-C4)alkyl;
- or R6 and R7 together with the nitrogen atom to which they are attached may form a 4-7 membered N-containing ring, optionally containing one further heteroatom selected from N, O and S, and optionally substituted with 1 or 2 substituents independently selected from (C1-C6)alkyl, (C1-C6)alkoxy, halo, CN and hydroxyl, said N-containing ring may also optionally be fused to an aryl group;
- or R4 and R6 together with the atoms to which they are attached may form a saturated or partially unsaturated 4-7 membered N-containing ring, optionally containing one further heteroatom selected from N, O and S, and optionally substituted on carbon with 1 or 2 substituents independently selected from (C1-C6)alkyl, (C1-C6)alkoxy, halo, CN and hydroxyl;
- or R5 is absent and R4 and R6 together with the atoms to which they are attached may form a 5, 6, 9 or 10 membered mono- or bi-cyclic N-containing aromatic ring, optionally containing one further heteroatom selected from N, O and S, and optionally substituted on carbon with 1, 2 or 3 substituents independently selected from (C1-C6)alkyl, (C1-C6)alkoxy, halo, CN, aryl, COOR14 and hydroxyl;
- or R4 and R6 may together form a group according to formula II or formula III:
- R8, R9 and R10 are independently selected from H, (C1-C10)alkyl, halo, hydroxyl and (C1-C6)alkoxy;
- R11 is selected from H and (C1-C6)alkyl;
- R12 is selected from H and (C1-C6)alkyl;
- R13 is selected from H, (C1-C6)alkyl, (C1-C6)alkoxy, OH, CN, CF3, COOR14, halo and NR14R15;
- R14 and R15 are independently selected from H and (C1-C6)alkyl;
- f and g are independently selected from 0, 1, 2 and 3, such that f+g=1, 2 or 3;
- h is selected from 1 and 2;
- wherein:
- alkyl may optionally be substituted with 1 or 2 substituents independently selected from (C3-C10)cycloalkyl, (C1-C6)alkoxy, OH, CN, CF3, COOR14, halo and NR14R15;
- alkenyl may optionally be substituted with 1 or 2 substituents independently selected from (C3-C10)cycloalkyl, (C1-C6)alkoxy, OH, CN, CF3, COOR14, halo and NR14R15;
- alkoxy may optionally be substituted with 1 or 2 substituents independently selected from (C3-C10)cycloalkyl, OH, CN, CF3, COOR14, halo and NR14R15;
- cycloalkyl is a non-aromatic mono- or bi-cylic hydrocarbon ring, optionally fused to an aryl group, wherein said cycloalkyl ring optionally contains, where possible, up to 2 double bonds;
- and wherein, unless otherwise stated, said cycloalkyl may optionally be substituted with 1 or 2 substituents independently selected from (C1-C6)alkyl, (C1-C6)alkoxy, OH, CN, CF3, COOR14 , halo and NR14R15;
- heterocycloalkyl is a C-linked or N-linked 3 to 10 membered non-aromatic, mono- or bi-cyclic ring, wherein said heterocycloalkyl ring contains, where possible, 1, 2 or 3 heteroatoms independently selected from N, NR14, S(O)q and O;
- and said heterocycloalkyl ring optionally contains, where possible, 1 or 2 double bonds, and is optionally substituted on carbon with 1 or 2 substituents independently selected from (C1-C6)alkyl, (C1-C6)alkoxy, OH, CN, CF3, halo, COOR14, NR14R15 and aryl;
- aryl is a single or fused aromatic ring system containing 6 or 10 carbon atoms;
- wherein, unless otherwise stated, each occurrence of aryl may be optionally substituted with up to 5 substituents independently selected from (C1-C6)alkyl, (C1-C6)alkoxy, OH, halo, CN, COOR14, CF3 and NR14R15;
- heteroaryl is a 5, 6, 9 or 10 membered mono- or bi-cyclic aromatic ring, containing 1 or 2 N atoms and, optionally, an NR14 atom, or one NR14 atom and an S or an O atom, or one S atom, or one O atom;
- wherein, unless otherwise stated, said heteroaryl may be optionally substituted with 1, 2 or 3 substituents independently selected from (C1-C6)alkyl, (C1-C6)alkoxy, OH, halo, CN, COOR14, CF3 and NR14R15;
- q is 0, 1 or 2;
- and tautomers, stereoisomers, pharmaceutically acceptable salts and solvates thereof.
27 more elements
Dependencies are inferred from the claim text.