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Publication Number
US-12577241-B2
Publication Date
2026-03-17
Expiration Date
Abstract
The present invention provides a compound represented by the following Formula (I):wherein ring A is a C5-C7 non-aromatic carbocycle or a 5- to 7-membered non-aromatic heterocycle; ring B is a benzene ring or the like; Q is —NHC(O)— or a 5-membered aromatic heterocycle; R1 is each independently halogen or the like; R2a and R2b are each independently hydrogen, alkyl, or haloalkyl; R3 is alkyl or the like; R4 and R5 are each independently hydrogen or the like; R6 is each independently halogen, alkyl, haloalkyl, alkyloxy, haloalkyloxy, or alkyloxyalkyl; n is an integer of 1 to 3; and m is an integer of 0 to 3.
Core Innovation
The invention is directed to a compound represented by a structural Formula in which ring A is a C5-C7 non-aromatic carbocycle that may be further fused with a phenyl ring, a 3- to 7-membered non-aromatic carbocycle, or a 3- to 7-membered non-aromatic heterocycle, and may form a spiro ring of a 3- to 7-membered non-aromatic carbocycle and a 3- to 7-membered non-aromatic heterocycle. Ring B is a phenyl ring or a pyridinyl ring. Q is defined as specific rings in which substituents are constrained by permitted options for R1, R2a, R2b, R3, R4, R5, and R6, with integer parameters n and m.
The structural constraints specify that R1 is independently halogen, C1-4alkyl, haloC1-4alkyl, C1-4alkyloxy, cyano, or haloC1-4alkyloxy; R2a and R2b are independently hydrogen, C1-4alkyl, or haloC1-4alkyl; R3 is C1-4alkyl or haloC1-4alkyl; and R4 and R5 are independently hydrogen or C1-4alkyl. R6 is independently halogen, C1-4alkyl, haloC1-4alkyl, C1-4alkyloxy, haloC1-4alkyloxy, or C1-4alkyloxyC1-4alkyl, with an alternative where two R6 groups on a non-adjacent atom together form a C1-C3 bridge.
The invention also expressly includes pharmaceutically acceptable salts of the defined compounds. A second structural family is represented by Formula (IA) where ring A is limited to a C5-C6 non-aromatic carbocycle, ring B is defined as a phenyl ring or a pyridinyl ring, and m and n are limited within the specified integer ranges. In both Formula frameworks, the non-aromatic heterocycle is defined as a non-aromatic heterocycle containing 1 or 2 heteroatoms selected from O, S, and N.
Claims Coverage
The provided claim set includes two independent compound claims, one defining a compound by a general Formula and one defining a compound represented by Formula (IA). Across the independent claims, the main inventive features concern the ring A/ring B/Q framework and enumerated substituent options, including an optional C1-C3 bridge formed from two R6 groups.
Formula-defined compound with constrained ring a, ring b, q, and substituent groups
A compound represented by a Formula wherein ring A is a C5-C7 non-aromatic carbocycle, optionally fused or spiro, ring B is a phenyl ring or a pyridinyl ring, and Q is of defined rings with substituent constraints for R1, R2a/R2b, R3, R4/R5, and R6, including an alternative where two R6 groups form a C1-C3 bridge; n is an integer of 1 to 3 and m is an integer of 0 to 3, including pharmaceutically acceptable salts.
Formula (IA)-defined compound with constrained ring a, ring b, q, and substituent groups
A compound represented by Formula (IA) wherein ring A is a C5-C6 non-aromatic carbocycle, ring B is a phenyl ring or a pyridinyl ring, and Q is one of the defined rings with substituent constraints for R1, R2a/R2b, R3, and R6, including an alternative where two R6 groups form a C1-C3 bridge; n is an integer of 1 to 3 and m is an integer of 0 to 2, including pharmaceutically acceptable salts.
Across the independent claims, the inventive coverage centers on Formula-defined compounds and Formula (IA)-defined compounds where ring A, ring B, and Q are defined, while substituent variables are constrained to specific enumerated groups and may additionally form a C1-C3 bridge. Both independent claims expressly include pharmaceutically acceptable salts.
Stated Advantages
Long-acting integrase inhibitor with a high resistance barrier.
Integrase inhibitory activity.
Cell proliferation inhibitory activity.
Long in vivo half-life and low clearance.
Solubility and metabolic stability.
Reduced cytotoxicity/side effects, including CYP inhibition and QT interval prolongation/arrhythmia.
Documented Applications
Anti-HIV uses as an HIV integrase inhibitor, including treatment and/or prevention.
Pharmaceutical composition uses comprising an effective amount of a compound and pharmaceutically acceptable additive, carrier or diluent.
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