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C6-aryl and heteroaryl substituted pyrido[2,3-D] pyrimidin-7-ones

The present invention provides substituted 2-aminopyridines of formula I, wherein R1, A1, W, X, and Y are as defined in the specification, useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent kinases 4 (Cdk4).
Owner:PFIZER INC

Treatment of autoimmune disorders

The present invention relates to the use of a compound of formula I wherein R2 is R-NH wherein R is a branched or unbranched alkyl radical, a piperidinyl group or pyrrolidinyl group, each of which may be optionally substituted by one or more -OH, halogen, amino or hydroxyalkyl groups; R6 is phenylamino, benzylamino or pyridyl-methylamino, indan-5-amino, where in each case the aryl group may be unsubstituted or substituted by one or more -OR'', halogen, NO2, amino or COOR' groups, wherein R' and R'' are each independently H or a branched or unbranched alkyl group; and R9 is a branched or unbranched alkyl group or a cycloalkyl group; in the treatment of an autoimmune disorder. The invention further relates to a method of treating an autoimmune disorder comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I.
Owner:CYCLACEL

Pharmaceutical compositions for the treatment of CNS and other disorders

InactiveUS20060014750A1Ease of detectabilityEasy to prepareBiocideNervous disorderDiseaseΑ7 nicotinic receptor
The present invention relates to a method of treating disorders of the central nervous system (CNS) and other disorders in a mammal, including a human, by administering to the mammal a CNS-penetrant α7 nicotinic receptor agonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant α7 nicotinic receptor agonist.
Owner:PFIZER INC

Compounds

A compound of formula I, or a pharmaceutically acceptable salt or ester thereof,wherein R1 is selected from: aryl; heteroaryl; —NHR3; fused aryl-C4-7-heterocycloalkyl; —CONR4R5; —NHCOR6; —C3-7-cycloalkyl; —O—C3-7-cycloalkyl; —NR3R6; and optionally substituted —C1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7-heterocycloalkyl are each optionally substituted;R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl, C3-7-cycloalkyl, heteroaryl, C4-7 heterocycloalkyl and halogen, wherein said C1-6-alkyl, C2-6-alkenyl, aryl, heteroaryl and C4-7-heterocycloalkyl are each optionally substituted;R3 is selected from aryl, heteroaryl, C4-7-heterocycloalkyl, C3-7-cycloalkyl, fused aryl-C4-7-heterocycloalkyl and C1-6-alkyl, each of which is optionally substituted;R4 and R5 are each independently hydrogen, or optionally substituted C3-7-cycloalkyl, aryl, heteroaryl, C1-6-alkyl or C3-6-heterocycloalkyl; or R4 and R5 together with the N to which they are attached form a C3-6-heterocycloalkyl ring;each R6 is independently selected from C1-6-alkyl, C3-7 cycloalkyl, C4-7-heterocycloalkyl, aryl and heteroaryl, each of which is optionally substitutedeach R7 is selected from hydrogen, optionally substituted C1-6-alkyl and C3-7-cycloalkyl;each of R8 and R9 is independently hydrogen or optionally substituted C1-6-alkyl; orR8 and R9 together with the N to which they are attached form a C4-6-heterocycloalkyl;each R10 is selected from C3-7-cycloalkyl and optionally substituted C1-6-alkyl;each R11 is independently selected from C1-6-alkyl, C3-7-cycloalkyl, C1-6 alkyl-C3-7-cycloalkyl, C4-7-heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted;A is selected from halogen, —NR4SO2R5, —CN, —OR6, —NR4R5, —NR7R11, hydroxyl, —CF3, —CONR4R5, —NR4COR5, —NR7(CO)NR4R5, —NO2, —CO2H, —CO2R6, —SO2R6, —SO2NR4R5, —NR4COR5, —NR4COOR5, C1-6-alkyl and —COR6.Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula I.
Owner:LIFEARC
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