Substituted pyridines as inhibitors of human immunodeficiency virus replication
US10189816B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Aug 10, 2016 |
| Grant date | Jan 29, 2019 |
| Priority date | — |
| Expiry date | Aug 10, 2036 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K2300/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Disclosed are compounds of Formula (I), including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS. In the compounds of formula (I), R1 is selected from hydrogen, alkyl, or cycloalkyl; R2 is selected from tetrahydroisoquinolinyl and is substituted with 1 R6 substituent and also with 0-3 halo or alkyl substituents; R3 is selected from azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, homopiperidinyl, homopiperazinyl, or homomorpholinyl, and is substituted with 0-3 substituents selected from cyano, halo, alkyl, haloalkyl, alkoxy, and haloalkoxy; R4 is selected from alkyl or haloalkyl; R5 is alkyl; R6 is selected from Ar1, (Ar1)alkyl, (chromanyl)alkyl, cyanocycloalkyl or (dihydrobenzodioxinyl)alkyl; and Ar1 is phenyl substituted with 0-5 substituents selected from cyano, halo, alkyl, cycloalkyl, haloalkyl, hydroxy, alkoxy, haloalkoxy, (hydroxy)alkoxy, (alkoxy)alkoxy, phenoxy, benzyloxy, carboxy, phenyl, and cyanocycloalkyl.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.