C2-CARBOCYCLIC IMINOTHIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE

摘要

In its many embodiments, the present invention provides certain C2-carbocyclic iminothiazine dioxide compounds, including compounds Formula (I); or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, ring A, RA, m, ring B, RB, n, ring C, RC and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.;

主权项

1. A compound, or a pharmaceutically acceptable salt thereof, said compound having the structural Formula (I): or a tautomer thereof having the structural Formula (I′): or pharmaceutically acceptable salt thereof, wherein: R1 is selected from the group consisting of H, halogen, lower alkyl, and lower heteroalkyl, wherein said lower alkyl and said lower heteroalkyl is optionally substituted with one or more halogen; R2 is selected from the group consisting of H, lower alkyl, lower cycloalkyl, and lower heteroalkyl, wherein said lower alkyl, lower cycloalkyl, and said lower heteroalkyl are optionally substituted with one or more halogen; ring A is selected from the group consisting of phenyl, pyridinyl, pyridazinyl, pyrimidinyl, and pyrazinyl; m is 0, 1, 2, or 3; each RA (when present) is independently selected from the group consisting of halogen, —CN, —CH3, —CH2CH3, —CH(CH3)2, cyclopropyl, —CH2OCH3, —CF3, —CHF2, —CH2F, —OCH3, —O-cyclopropyl, —O—CH2-cyclopropyl, —OCF3, —OCHF2, and —OCH2F; ring B is heteroaryl; n is 0, 1, 2, or 3; each RB (when present) is independently selected from the group consisting of halogen, —CN, —OH, —CH3, —CH2CH3, —CH(CH3)2, cyclopropyl, —CH2-cyclopropyl, —CH2OCH3, —C≡CH, —C≡C—CH3, —CF3, —CHF2, —CH2F, —OCH3, —OCH2CH3, —O-cyclopropyl, —O—CH2-cyclopropyl, —OCH2—C≡C—H, —OCH2—C≡C—CH3, —OCF3, —OCHF2, —OCH2F, and —OCH2CH2F; ring C is selected from the group consisting of cyclopropyl and cyclobutyl; p is 0, 1, or 2; and each RC (when present) is independently selected from the group consisting of: halogen, —OH, —CN, lower alkyl, and lower alkoxy, where said lower alkyl and said lower alkoxy are each optionally substituted with 1 to 3 fluorine.