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US 6,180,632 B2Granted
Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases
AssigneeAventis Pharmaceuticals Products Inc.
InventorsMichael R. Myers, Wei He, Alfred P. Spada, Martin P. Maguire
Life of this patent
Estimating the term…
Abstract
This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.
Claims79
A compound of formula I
- wherein X is L1 or L2Z2;
- L1 is (CR3aR3b)r or (CR3aR3b)m-Z3-(CR3′a/R3′b)n;
- L2 is (CR3a/R3b)p-Z4-(CR3′a/R3′b), or ethenyl,
- Z1 is N;
- Z2 is cycloalkyl, substituted cycloalkyl, cycloalkenyl, substituted cycloalkenyl, heterocyclyl, substituted beterocyclyl, heterocyclenyl or substituted heterocyclenyl;
- Z3 is O, NR4 or SO;
- Z4 is O, NH, S, SO S2 or a bond;
- m is 0 or 1;
- n is 2 or 3, and n+m=2 or 3;
- p and q are independently 0, 1, 2, 3 or 4, and p+q=0, 1, 2, 3 or 4 when Z4 is a bond, and p+q=0, 1, 2 or 3 when Z4 is other than a bond;
- r is 2, 3 or 4;
- R1a and R1b are independently alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, hydroxy, acyloxy, alkoxy, substituted alkoxy, cycloalkoxy, substituted cycloalkyloxy, heterocyclyloxy, substituted heterocyclyloxy, heterocyclylcarbonyloxy, substituted heterocyclylcarbonyloxy, aryloxy, substituted aryloxy, heteroaryloxy, substituted heteroaryloxy, cyano, R5R6N- or acylR5N-, or one of R1a and R1b is hydrogen or halo and the other is alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, hydroxy, acyloxy, alkoxy, substituted alkoxy, cycloalkyloxy, substituted cycloalkyloxy, heterocyclyloxy, substituted heterocyclyloxy, heterocyclylcarbonyloxy, substituted heterocyclylcarbonyloxy, aryloxy, substituted aryloxy, heteroaryloxy, substituted heteroaryloxy, cyano, R5R6N- or acylR5N-;
- R1c is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, hydroxy, acyloxy, alkoxy, substituted alkoxy, cycloalkyloxy, substituted cycloalkyloxy, heterocyclyloxy, substituted heterocyclyloxy, aryloxy, substituted aryloxy, heteroaryloxy, substituted heteroaryloxy, halo, cyano, R5R6N- or acylR5N-;
- R3a, R3b, R3′a and R3′b are independently hydrogen or alkyl;
- R4 is hydrogen, alkyl or acyl;
- and
- R5 and R6 are independently hydrogen or alkyl, or R5 and R6 taken together with the nitrogen atom to which R5 and R6 are attached form a heterocyclyl, or
- an N-oxide thereof, hydrate thereof, solvate thereof, prodrug thereof, or a pharmaceutically acceptable salt thereof.
15 more elements
Dependencies are inferred from the claim text.