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US 2006/0142281 A1Published application
Indolinone derivatives
AssigneeTheravance, Inc.
InventorsJohn Griffin, Roger Briesewitz, Jonathan Wray
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I) in which R1, R2, R3 and R4 have the meanings given in the specification, are receptor tyrosine kinase inhibitors useful in the treatment of proliferative disorders, such as cancer.
Claims24
A compound of formula (I)
- wherein:
- (i) R1 represents a hydrogen atom or a (1-4C)alkyl group;
- and R2 represents a group of formula -A1-NR5R6 in which each of R5 and R6 independently represents a hydrogen atom or a (1-4C)alkyl group and A1 represents (CH2)m, (CH2)n-A2-(CH2)p or (CH2CH2O)qCH2CH2 in which m is an integer of from 2 to 10, each of n and p is an integer of from 1 to 6, A2 is CH═CH, phenylene, biphenylene, cyclohexylene or piperazinylene and q is 1, 2 or 3;
- (ii) R1 and R2 together represent -A3-NR7-A4- in which each of A3 and A4 independently represents (CH2)r or (CH2CH2O)sCH2CH2 in which r is an integer of from 2 to 6, s is 1, 2 or 3, and R7 represents a hydrogen atom or a (1-4C)alkyl group;
- (iii) R1 and R2 together with the nitrogen atom to which they are attached represent a piperidinyl group, which piperidinyl group bears a substituent of formula -A5-R8 at the 4 position, in which A5 represents (1-4C)alkylene and R8 represents piperidin-4-yl;
- or
- (iv) R1 and R2 together with the nitrogen atom to which they are attached represent a pyrrolidinyl, piperidinyl or morpholino group;
- and
- R3 and R4 each independently represents a hydrogen atom, a halogen atom, a (1-4C)alkyl group, a (1-4C)alkoxy group, a phenyl group which is unsubstituted or substituted by one or two substituents selected independently from a halogen atom, a (1-4C)alkyl group and a (1-4C)alkoxy group, a group of formula R8S(O)2NR9—, a group of formula R10N(R11)S(O)2—, a group of formula R12C(O)N(R13)— or a group of formula R14N(R15)C(O)— in which each of R8, R10, R12 and R14 independently represents a (1-4C)alkyl group or a phenyl group which is unsubstituted or substituted by one or two substituents selected independently from a halogen atom, a (1-4C)alkyl group and a (1-4C)alkoxy group, and each of R9, R11, R13 and R15 independently represents a hydrogen atom or a (1-4C)alkyl group;
- or a pharmaceutically-acceptable salt thereof.
7 more elements
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Dependencies are inferred from the claim text.