ES2901114T3

Inhibitors of -amino- -carboxymuconic acid semialdehyde decarboxylase

Abstract

A compound represented by formula (I): **(See formula)** or a pharmaceutically acceptable salt or tautomer thereof, wherein: X is O, OH or Cl; L is -(CH2)mY(CH2)p-; Y is O, N or S(O)q; R1 is C6-C10 aryl or heteroaryl, wherein aryl and heteroaryl are substituted with Ra and Rb, and optionally substituted with one or more Re; one of Ra and Rb is hydrogen and the other is -(CH2)rCO2Rx, -OCH2CO2Rx, -(CH2)rtetrazol, -(CH2)roxadiazolone, -(CH2)rtetrazolone, -(CH2)rthiadiazolol, -(CH2)risoxazole- 3-ol, -(CH2)rP(O)(OH)ORx, -(CH2)rS(O)2OH, -(CH2)rC(O)NHCN, or -(CH2)rC(O)NHS(O)2alkyl ; Rc is C1-C6 alkyl, C1-C6 haloalkyl, halogen, -CN, -ORx, -CO2Rx or NO2; Rd is methyl, cyclohexyl, pyridinyl, thiazolyl, phenyl, or thienyl, wherein each cyclohexyl, pyridinyl, thiazolyl, phenyl, or thienyl is optionally substituted with one or more substituents independently selected from halogen, C1-C6 alkyl, C1-C6 hydroxyalkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 haloalkoxy, -OH, CN and amino; each Rx is independently each occurrence of hydrogen or C1-C6 alkyl; each Re is independently C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halogen, -ORy, C1-C6 haloalkyl, -NHRz, -OH, or -CN; Rf is H or is absent; each Ry and Rz is independently hydrogen, C1-C6 alkyl or C1-C6 haloalkyl; m is 0, 1 or 2; p is 1 or 2, where m + p < 3; q is 0, 1 or 2; r is 0 or 1; and the dotted line is an optional double bond; provided that Rc is not -CN when X is O, L is -SCH2- and Rd is optionally substituted phenyl; and that Rc is not C1-C6 alkyl when X is O, L is -SCH2- and Rd is methyl.

ES2901114T3, drawing sheet 1
Sheet 1 of 10

Term

8.9 yearsto projected expiry

Projected expiry 28 August 2035, counted from filing; an application has no term until it is granted.

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10 sheets

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