Back to results
US 2025/0074907 A1Published application
Inhibitors of sars-cov-2
AssigneeThe Texas A&M University System
InventorsJames SACCHETTINI, Arjun ACHARYA, Armando FLORES, Inna KRIEGER, Maloy PARAI, Nian ZHOU, Radha BAM, Pradeep Kumar JAISWAL, Su TANG, Xuelin BIAN, Zhe SHI
Life of this patent
Estimating the term…
Abstract
Described herein are compounds, and methods for the treatment of coronavirus infection.
Claims22
A compound defined by Formula (I) below.
- or a pharmaceutically acceptable salt or prodrug thereof, wherein, as valence and stability permit,
- Ra and Rb are independently selected from aryl or heteroaryl, each optionally substituted with one or more substituents individually chosen from R5;
- Rc is chosen from the following groups:
- A and D are independently selected from CR6, and N;
- E and G are independently selected from CR6, N, NR6, S, and O;
- M is selected from C, CR6, S, and SR6;
- the dotted lines represent single or double bonds as valence and stability permit;
- Rd is selected from aryl, heteroaryl, cycloalkyl, and cycloheteroalkyl, each optionally substituted with one or more substituents individually chosen from R5;
- R5 is, individually for each occurrence, chosen from hydroxy, halogen, —CN, —NO2, amino, alkylamino, dialkylamino, alkyl, haloalkyl;
- alkylthio;
- haloalkylthio;
- alkoxy, haloalkoxy, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl, haloalkoxycarbonyl, alkylaminocarbonyl, heteroalkylaminocarbonyl, dialkylaminocarbonyl, heterodialkylaminocarbonyl, sulfonamido, and sulfoximino;
- R6 is, individually for each occurrence, chosen from hydrogen, alkyl, haloalkyl;
- alkenyl, haloalkenyl, alkynyl, and haloalkynyl;
- and
- R10 is chosen from H or —OH.
13 more elements
(canceled)
A compound defined by any of Formula (A-1)-(A-20)
- or pharmaceutically acceptable salts or prodrugs thereof, wherein, as valence and stability permit,
- Rc is chosen from the following groups:
- A and D are independently selected from CR6, and N;
- E, G, Q, T, and U are independently selected from CR6, N, NR6, S, and O;
- Xa—Xd, and Ya—Yd are independently selected from CR6, N, NR6, N═O, S, and O;
- M is selected from C, CR6, S, and SR6;
- the dotted lines represent single or double bonds as valence and stability permit;
- Rd is selected from aryl, heteroaryl, cycloalkyl, and cycloheteroalkyl, each optionally substituted with one or more substituents individually chosen from R5;
- R1, R2, R3, and R4 are each individually chosen from hydrogen, hydroxy, halogen, —CN, —NO2, amino, alkylamino, dialkylamino, alkyl, haloalkyl;
- alkylthio;
- haloalkylthio;
- alkoxy, haloalkoxy, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl, haloalkoxycarbonyl, alkylaminocarbonyl, heteroalkylaminocarbonyl, dialkylaminocarbonyl, and heterodialkylaminocarbonyl;
- R5 is, individually for each occurrence, chosen from hydroxy, halogen, —CN, —NO2, amino, alkylamino, dialkylamino, alkyl, haloalkyl;
- alkylthio;
- haloalkylthio;
- alkoxy, haloalkoxy, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl, haloalkoxycarbonyl, alkylaminocarbonyl, heteroalkylaminocarbonyl, dialkylaminocarbonyl, heterodialkylaminocarbonyl, sulfonamido, and sulfoximino;
- R6 is, individually for each occurrence, chosen from hydrogen, alkyl, haloalkyl;
- alkenyl, haloalkenyl, alkynyl, and haloalkynyl;
- R7 is chosen from hydrogen, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl group, each optionally substituted with one or more substituents individually chosen from R5;
- R8 and R9 are independently selected from —NR6R6, —OH, ═O, and H, wherein at least one of R8 or R9 is selected from —NR6R6, —OH, and ═O;
- and
- R10 and R11 are independently selected from H or —OH.
19 more elements
(canceled)
A compound defined by Formula (XIII) below
- or a pharmaceutically acceptable salt or prodrug thereof, wherein, as valence and stability permit,
- Ar1 and Ar2 are independently selected from aryl or heteroaryl, each optionally substituted with one or more substituents individually chosen from R5;
- Z is optionally present, and selected from —NH(CH2)n—, —CH(CH2)n—, and —CH2(CH2)n—;
- n is an integer selected from 1 to 6;
- X is —CONH—;
- Y is optionally present and selected from aryl, heteroaryl, each optionally substituted with one or more substituents individually chosen from R5;
- R is selected from aryl, heteroaryl, cycloalkyl, and cycloheteroalkyl, each optionally substituted with one or more substituents individually chosen from R5;
- and
- R5 is, individually for each occurrence, chosen from hydroxy, halogen, —CN, —NO2, amino, alkylamino, dialkylamino, alkyl, haloalkyl;
- alkylthio;
- haloalkylthio;
- alkoxy, haloalkoxy, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl, haloalkoxycarbonyl, alkylaminocarbonyl, heteroalkylaminocarbonyl, dialkylaminocarbonyl, heterodialkylaminocarbonyl, sulfonamido, and sulfoximino.
9 more elements
(canceled)
A compound defined by Formula (B-1) to Formula (B-20) below
- or pharmaceutically acceptable salts or prodrugs thereof, wherein, as valence and stability permit,
- Z is optionally present, and selected from —NH(CH2)n—, —CH(CH2)n—, and —CH2(CH2)n—;
- n is an integer selected from 1 to 6;
- X is —CONH—;
- Y is optionally present and selected from aryl, heteroaryl, each optionally substituted with one or more substituents individually chosen from R5;
- R is selected from aryl, heteroaryl, cycloalkyl, and cycloheteroalkyl, each optionally substituted with one or more substituents individually chosen from R5;
- R1, R2, R3, and R4 are each individually chosen from hydrogen, hydroxy, halogen, —CN, —NO2, amino, alkylamino, dialkylamino, alkyl, haloalkyl;
- alkylthio;
- haloalkylthio;
- alkoxy, haloalkoxy, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl, haloalkoxycarbonyl, alkylaminocarbonyl, heteroalkylaminocarbonyl, dialkylaminocarbonyl, and heterodialkylaminocarbonyl;
- and
- R5 is, individually for each occurrence, chosen from hydroxy, halogen, —CN, —NO2, amino, alkylamino, dialkylamino, alkyl, haloalkyl;
- alkylthio;
- haloalkylthio;
- alkoxy, haloalkoxy, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl, haloalkoxycarbonyl, alkylaminocarbonyl, heteroalkylaminocarbonyl, dialkylaminocarbonyl, heterodialkylaminocarbonyl, sulfonamido, and sulfoximino;
- R6 is, individually for each occurrence, chosen from hydrogen, alkyl, haloalkyl;
- alkenyl, haloalkenyl, alkynyl, and haloalkynyl;
- R7 is chosen from hydrogen, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl group, each optionally substituted with one or more substituents individually chosen from R5;
- R8 and R9 are independently selected from —NR6R6, —OH, ═O, and H, wherein at least one of R8 or R9 is selected from —NR6R6, —OH, and ═O;
- R11 are independently selected from H or —OH;
- Q, T, and U are independently selected from CR6, N, NR, S, and O;
- and
- Xa—Xd, and Ya—Yd are independently selected from CR6, N, NR6, N═O, S, and O.
20 more elements
(canceled)
Dependencies are inferred from the claim text.