US2018127388A1PendingUtilityA1
Therapeutic compounds
Est. expiryApr 20, 2032(~5.7 yrs left)· nominal 20-yr term from priority
Inventors:Kerim BabaogluGediminas BrizgysJacob ChaXiaowu ChenHongyan GuoRandall L. HalcombXiaochun HanRichard HuangHongtao LiuRyan McfaddenMichael L. MitchellYingmei QiPaul A. RoethleLianhong XuHong Yang
A61P 31/18A61K 31/497A61K 31/551C07D 277/68C07D 498/04A61K 31/496A61K 31/428A61K 31/4439A61K 31/4985A61K 31/4375A61K 31/436A61K 31/538C07D 487/04A61K 31/4741C07D 417/10C07D 491/06A61K 31/501A61K 31/4709A61K 31/5383A61K 31/437C07D 277/82C07D 471/04A61K 31/506A61K 31/553A61K 31/513A61K 31/5377A61K 45/06C07D 417/14A61K 31/454C07D 417/04A61K 31/444C07D 277/66
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Claims
Abstract
Compounds disclosed herein including compounds of formula I′: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A compound of formula I′:
wherein:
R 4 is selected from aryl, heterocycle and heteroaryl, wherein any aryl, heterocycle and heteroaryl of R 4 is optionally substituted with one or more groups each independently selected from halo, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 1 -C 6 )haloalkyl, (C 3 -C 7 )cycloalkyl, —(C 1 -C 6 )alkyl-(C 3 -C 7 )cycloalkyl, —OH, —O(C 1 -C 6 )alkyl, —SH, —S(C 1 -C 6 )alkyl, NH 2 , —NH(C 1 -C 6 )alkyl and —N((C 1 -C 6 )alkyl) 2 , wherein (C 1 -C 6 )alkyl is optionally substituted with hydroxy, —O(C 1 -C 6 )alkyl, cyano or oxo;
A is phenyl, monocyclic heteroaryl or monocyclic heterocycle, wherein any phenyl, monocyclic heteroaryl or monocyclic heterocycle of A is optionally substituted with one or more Z 1a groups, and B is aryl, heteroaryl or heterocycle, wherein any aryl, heteroaryl or heterocycle of B is optionally substituted with one or more Z 1b groups; or A and B together form a bicyclic aryl, bicyclic heteroaryl or bicyclic heterocycle, wherein bicyclic aryl, bicyclic heteroaryl or bicyclic heterocycle is optionally substituted with one or more Z 1b groups;
each Z 1a is independently selected from halo, (C 1 -C 3 )alkyl, (C 2 -C 3 )alkenyl, (C 2 -C 3 )alkynyl, (C 1 -C 3 )haloalkyl, (C 3 -C 7 )carbocycle, heterocycle, —O(C 1 -C 3 )alkyl, —O(C 2 -C 3 )alkenyl, —O(C 2 -C 3 )alkynyl, —NR c R d , —NR a C(O)R a , —C(O)OR b and —C(O)NR c R d , wherein any (C 3 -C 7 )carbocycle and heterocycle of Z 1a is optionally substituted with one or more halogen or (C 1 -C 6 )alkyl;
each Z 1b is independently selected from halo, CN, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, (C 1 -C 6 )haloalkyl, (C 3 -C 7 )carbocycle, heteroaryl, heterocycle, aryl(C 1 -C 6 )alkyl-, —OH, —O(C 1 -C 6 )alkyl, —O(C 2 -C 6 )alkenyl, —O(C 2 -C 6 )alkynyl, —NR c R d , —NR a C(O)R a , —C(O)OR b and —C(O)NR c R d , wherein any (C 3 -C 7 )carbocycle and heterocycle of Z 1b is optionally substituted with one or more halogen or (C 1 -C 6 )alkyl; and
R a , R b , R c and R d are each independently H or (C 1 -C 6 )alkyl;
or a salt thereof.
2 . The compound of claim 1 wherein the configuration of the —OC(CH 3 ) 3 group as shown in formula I′ is the (S) stereochemistry.
3 . The compound of claim 1 wherein R 4 is selected from aryl, heterocycle and heteroaryl, wherein any aryl, heterocycle and heteroaryl of R 4 is optionally substituted with one or more halo or (C 1 -C 6 )alkyl.
4 . The compound claim 1 wherein R 4 is selected from aryl and heterocycle, wherein any aryl and heterocycle of R 4 is optionally substituted with one or more chloro, fluoro or methyl.
5 . The compound of claim 1 wherein R 4 is:
6 . The compound of claim 1 wherein R 4 is:
7 . The compound of claim 1 wherein A is phenyl, monocyclic N-heteroaryl or monocyclic heterocycle, wherein any phenyl, monocyclic N-heteroaryl or monocyclic heterocycle of A is optionally substituted with one or more Z 1a groups, and B is aryl, heteroaryl or heterocycle, wherein any aryl, heteroaryl or heterocycle of B is optionally substituted with one or more Z 1b groups.
8 . The compound of claim 1 wherein A is monocyclic N-heteroaryl, wherein monocyclic N-heteroaryl is optionally substituted with one or more Z 1a groups, and B is aryl, heteroaryl or heterocycle, wherein any aryl, heteroaryl or heterocycle of B is optionally substituted with one or more Z 1b groups.
9 . The compound of claim 1 wherein A is pyridinyl, pyrimidinyl or pyrazinyl, wherein pyridinyl, pyrimidinyl or pyrazinyl is optionally substituted with one or more Z 1a groups, and B is aryl, heteroaryl or heterocycle, wherein any aryl, heteroaryl or heterocycle of B is optionally substituted with one or more Z 1b groups.
10 . The compound of claim 1 wherein A is pyridinyl, pyrimidinyl or pyrazinyl and B is aryl, heteroaryl or heterocycle, wherein any aryl, heteroaryl or heterocycle of B is optionally substituted with one or more Z 1b groups.
11 . The compound of claim 1 wherein A and B together form a bicyclic aryl, bicyclic heteroaryl or bicyclic heterocycle, wherein bicyclic aryl, bicyclic heteroaryl or bicyclic heterocycle is optionally substituted with one or more Z 1b groups.
12 . The compound of claim 1 wherein A and B together form a bicyclic heteroaryl, wherein bicyclic heteroaryl is optionally substituted with one or more Z 1b groups.
13 . The compound of claim 1 wherein A and B together form a pyrrolopyridinyl, pyrazolopyridinyl or indazolyl, wherein pyrrolopyridinyl, pyrazolopyridinyl or indazolyl is optionally substituted with one or more Z 1b groups.
14 . The compound of claim 1 wherein A-B is selected from:
15 . The compound of claim 1 wherein the salt is a pharmaceutically acceptable salt.
16 . The compound of claim 1 which is selected from:
and pharmaceutically acceptable salts thereof.
17 . The compound of claim 1 wherein A-B is selected from:
18 . The compound of claim 1 wherein A-B is selected from:
19 . The compound of claim 1 wherein A-B is selected from:
20 . The compound of claim 1 which is selected from:
and pharmaceutically acceptable salts thereof.
21 . The compound of claim 1 which is selected from:
and pharmaceutically acceptable salts thereof.
22 . A pharmaceutical composition comprising a compound of formula I′ as described in claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
23 . A method of treating an HIV infection in a mammal comprising administering a compound of formula I′ as described in claim 1 , or a pharmaceutically acceptable salt thereof, to the mammal.
24 . A method for treating an HIV infection in a mammal comprising administering to the mammal in need thereof a therapeutically effective amount of a compound of formula I′ as described in claim 1 , or a pharmaceutically acceptable salt thereof, in combination with a therapeutically effective amount of one or more additional therapeutic agents selected from the group consisting HIV protease inhibiting compounds, HIV non-nucleoside inhibitors of reverse transcriptase, HIV nucleoside inhibitors of reverse transcriptase, HIV nucleotide inhibitors of reverse transcriptase, HIV integrase inhibitors, gp41 inhibitors, CXCR4 inhibitors, gp120 inhibitors, CCR5 inhibitors, capsid polymerization inhibitors, and other drugs for treating HIV, and combinations thereof.Join the waitlist — get patent alerts
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