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US 2009/0023759 A1Published application
Quinazoline Derivatives as Inhibitors of EGF and/or erbB2 Receptor Tyrosine Kinase
OwnerRobert Hugh Bradburyinventor
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Abstract
A quinazoline derivative of the Formula I: wherein the substituents are as defined in the text for use in the production of an anti-proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man.
Claims29
A quinazoline derivative of Formula I:
- wherein:
- R1 is selected from hydrogen, hydroxy, (1-4C)alkoxy and (1-4C)alkoxy(1-4C)alkoxy;
- G1, G2, G3, G4 and G5 are each, independently, selected from hydrogen and halogeno;
- X1 is selected from SO2, CO, SO2N(R7) and C(R7)2, wherein each R7 is, independently, selected from hydrogen and (1-4C)alkyl;
- Q1 is aryl or heteroaryl, which aryl or heteroaryl group optionally bears one or more substituents independently selected from halogeno, cyano and (1-4C)alkoxy;
- R2, R3, R4 and R5 are each, independently, selected from hydrogen and (1-4C)alkyl, or
- R2 and R3 together with the carbon atom to which they are attached form a cyclopropyl ring, or
- R4 and R5 together with the carbon atom to which they are attached form a cyclopropyl ring;
- R6 is selected from hydrogen and (1-4C)alkyl;
- A is selected from hydrogen, Z-(CR8R9)p— and R10;
- p is 1, 2, 3, or 4;
- R8 and R9 are each, independently, selected from hydrogen and (1-4C)alkyl, or an R8 and an R9 group attached to the same carbon atom form a cyclopropyl ring;
- Z is selected from hydrogen, OR11 and NR12R13;
- R11, R12 and R13 are each, independently, selected from hydrogen and (1-4C)alkyl;
- and
- R10 is selected from (1-4C)alkoxy and NR12R13, wherein R12 and R13 are as defined above,
- wherein any CH2 or CH3 group within a Z or an R10 group optionally bears on each said CH2 or CH3 group one or more substituents independently selected from halogeno, (1-4C)alkyl, hydroxy and (1-4C)alkoxy;
- or a pharmaceutically acceptable salt thereof.
15 more elements
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Dependencies are inferred from the claim text.