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US 2017/0362252 A1Published application
Spirocyclic Heterocycle Compounds Useful as HIV Integrase Inhibitors
AssigneeMerck Sharp & Dohme Corp.
InventorsThomas H. Graham, Mark W. Embrey, Abbas Walji, Sherman T. Waddell
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Abstract
The present invention relates to Spirocyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, B, X, R1, R2, R3 and R4 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
Claims20
A compound having the formula:
- or a pharmaceutically acceptable salt thereof,
- wherein:
- A is —NHC(O)— or 5- or 6-membered monocyclic heteroaryl;
- B is C3-C7 cycloalkyl or 3 to 8-membered heterocycloalkyl, which can be optionally substituted with R5;
- X is C1-C4 alkylene;
- R1 is —N(C1-C6 alkyl)2 or R1 and an R3 group, together with the atoms to which they are attached, combine to form a 4 to 7-membered heterocycloalkyl, which can be optionally substituted with R5;
- R2 represents up to 3 optional substitutents, each independently selected from halo, C1-C6 alkyl, —O—(C1-C6 alkyl) and C1-C6 haloalkyl;
- each occurrence of R3 is independently selected from H, C1-C6 alkyl, —OH, —O—(C1-C6 alkyl), C1-C6 haloalkyl, C3-C7 cycloalkyl, —S—(C1-C6 alkyl), —NH2, —NH(C1-C6 alkyl) and —N(C1-C6 alkyl)2;
- R4 is selected from H, C1-C6 alkyl, C3-C7 cycloalkyl, —(C1-C4 alkylene)-O—(C1-C6 alkyl) and C1-C6 haloalkyl;
- R5 represents one or more groups, each independently selected from halo, C1-C6 alkyl, C1-C6 haloalkyl, 3 to 8-membered monocyclic heterocycloalkyl, 6 to 10-membered bicyclic heterocycloalkyl, —O—(C1-C6 alkyl), —O—(C6-C10 aryl), —O—(C1-C6 alkylene)-O—(C1-C6 alkyl), —O—(C1-C6 haloalkyl), —O—(C1-C6 alkylene)-O—(C1-C6 alkylene)-O—(C1-C6 alkyl), —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)2, —S(O)2(C1-C6 alkyl), —NHS(O)2—(C1-C6 alkyl), —S(O)2NH—(C1-C6 alkyl), —OC(O)—(C1-C6 haloalkyl), —(C1-C6 alkylene)p-C(O)O—(C1-C6 alkyl), —(C1-C6 alkylene)p-C(O)—(C1-C6 alkyl), —(C1-C6 alkylene)p-C(O)N(R6)2, C1-C6 hydroxyalkyl, —P(O)(OR8)2, and —CN;
- each occurrence of R6 is independently selected from H, C1-C6 alkyl, C3-C7 cycloalkyl, C1-C6 haloalkyl and —(C1-C6 alkylene)p-R7;
- each occurrence of R7 is independently selected from H, C1-C6 alkyl, —O—(C1-C6 alkyl), C3-C7 cycloalkyl, 5- or 6-membered monocyclic heteroaryl and 3 to 8-membered monocyclic heterocycloalkyl;
- each occurrence of R8 is independently selected from H and C1-C6 alkyl;
- and
- each occurrence of p is independently 0 or 1.
12 more elements
A compound selected from:
- or a pharmaceutically acceptable salt thereof.
(canceled)
(canceled)
Dependencies are inferred from the claim text.