Tetracyclic heterocycle compounds useful as HIV integrase inhibitors
AssigneeMerck Sharp & Dohme Corp.
InventorsThomas H. Graham, Tao Yu, Yonglian Zhang, John A. McCauley
Life of this patent
Estimating the term…
Abstract
The present invention relates to Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein A, X, R1, R2, R3 and R7 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Heterocycle Compound, and methods of using the Tetracyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
Claims39
A compound having the formula:
- or a pharmaceutically acceptable salt thereof,
- wherein:
- ----- represents an optional double bond;
- ring A, inclusive of the carbon atom and nitrogen atom to which ring A is fused, is a 5- to 8-membered monocyclic or bicyclic heterocycloalkyl group, which can be optionally and independently substituted on ring A carbon atom with a group selected from C1-C6 alkyl, —O—(C1-C6 alkyl) and C3-C7 cycloalkyl, and which can be optionally and independently substituted on a ring nitrogen atom with a group selected from C1-C6 alkyl, —C(O)—(C1-C6 alkyl) and —S(O)2—(C1-C6 alkyl);
- X is selected from 5 or 6-membered monocyclic heteroaryl and —N(R4)C(O)—;
- R1 is a phenyl group which is optionally substituted with from 1 to 3 groups, each independently selected from C1-C6 alkyl, halo, —O—(C1-C6 alkyl), C1-C6 haloalkyl, —O—(C1-C6 haloalkyl), —CN, —NO2, —N(R4)2, —C(O)OR6, —C(O)N(R4)2 and —NHC(O)R6;
- R2 is selected from H, C1-C6 alkyl, C3-C7 cycloalkyl, halo, C1-C6 haloalkyl, —OR5, —N(R4)2, —C(O)R5, —C(O)N(R4)2 and —NHC(O)R5, wherein said C1-C6 alkyl group is optionally substituted with one or more groups, each independently selected from halo, —OH, —O(C1-C6 alkyl) and —N(R4)2;
- R3 is selected from H, C1-C6 alkyl and —O—(C1-C6 alkyl), —N(R4)2;
- each occurrence of R4 is independently selected from H and C1-C6 alkyl;
- each occurrence of R5 is independently selected from H, C1-C6 alkyl and C3-C7 cycloalkyl;
- each occurrence of R6 is independently selected from H and C1-C6 alkyl;
- and
- R7 is selected from H and C1-C6 alkyl.
A compound having the structure:
- or a pharmaceutically acceptable salt thereof.
A compound having the structure:
- or a pharmaceutically acceptable salt thereof.
A compound having the structure:
- or a pharmaceutically acceptable salt thereof.
A compound having the structure:
- or a pharmaceutically acceptable salt thereof.
A compound having the structure:
- or a pharmaceutically acceptable salt thereof.
A compound having the structure:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.