US2022281825A1PendingUtilityA1
Heterocyclic compounds for the treatment of arenavirus infection
Est. expiryJul 12, 2036(~10 yrs left)· nominal 20-yr term from priority
Inventors:Kenneth MccormackMichael Bruno PleweNadezda SokolovaGregory HenkelEric BrownVidyasagar Reddy GantlaYoung-Jun Shin
A61K 31/519A61K 31/5377A61K 31/4985C07D 473/00A61K 31/4184C07D 405/04C07D 235/20A61P 31/14C07D 249/18A61K 31/454A61K 31/5025A61K 31/7105A61K 31/437C07D 487/04A61K 31/423C07D 413/00A61K 31/4192A61K 31/52A61K 45/06C07D 261/20C07D 231/56C07D 471/08C07D 235/06A61K 31/53A61K 31/4439C07D 403/14A61K 31/416A61K 31/7056A61K 31/439C07D 471/04A61K 31/713C07D 209/08C07D 403/04
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Claims
Abstract
The invention relates to compounds of structural formula Iwherein A, D, and E are independently N or C—R3, G, H, and J are independently N or C, K is N or C—H, L is N, N—R3 or C—R3, and A, D, E, G, H, J, K, and L together cannot have more than 4 N, R1 is selected from (C6 to C10) aryl, (C2 to C9) heteroaryl, and 5-indolyl, wherein each of the said (C6 to C10) aryl and (C2 to C9) heteroaryl is substituted with at least one R4a group, and wherein said (C2 to C9) heteroaryl is C-attached, and R2 is selected from the group consisting of
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A method of treating arenavirus infection comprising administration of a therapeutically effective amount of a compound of Structural Formula I
or a pharmaceutically acceptable salt, and a pharmaceutically acceptable carrier, diluent, or vehicle thereof, wherein:
A, D, E, and K are independently N or C—R 3 ;
G, H, and J are independently N or C;
L is N, N—R 3 , or C—R 3 ;
and A, D, E, G, H, J, K, and L together cannot have more than 4 N;
and when G and H are C, and A, D, E, and K are C—R 3 then J and L together cannot be N;
R 1 is selected from (C 6 to C 10 ) aryl and (C 2 to C 9 ) heteroaryl, wherein
each of the said (C 6 to C 10 ) aryl and (C 2 to C 9 ) heteroaryl is optionally substituted with at least one R 4 group, and wherein said (C 2 to C 9 ) heteroaryl is C-attached;
R 2 is selected from (C 6 to C 10 ) aryl and (C 2 to C 9 ) heteroaryl, wherein
each of the said (C 6 to C 10 ) aryl and (C 2 to C 9 ) heteroaryl is optionally substituted with at least one R 4 group;
each of the R 3 is independently selected from hydrogen, halogen, cyano, OH, CF 3 , (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, (C 2 to C 9 ) heteroaryl, —C(O)R 5 , —C(O)NR 6a R 6b , —NR 6a R 6b , —S(O) m R 5 , —S(O) m NR 6a R 6b , —NR 6a S(O) m R 5 , —(CH 2 ) n C(O)OR 5 , —(CH 2 ) n C(O)NR 6a R 6b , —OC(O)R 5 , —NR 6a C(O)R 5 , and —NR 6c C(O)NR 5a R 5b , wherein
each of the said (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl is optionally substituted with at least one R 4 group;
R 4 is independently selected from hydrogen, halogen, cyano, OH, CF 3 , (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, (C 2 to C 9 ) heteroaryl, —C(O)R 5 , —C(O)NR 6a R 6b , —NR 6a R 6b , —S(O) m R 5 , —S(O) m NR 6a R 6b , —NR 6a S(O) m R 5 , —(CH 2 ) n C(O)OR 5 , —(CH 2 ) n C(O)NR 6a R 6b , —OC(O)R 5 , —NR 6a C(O)R 5 , and —NR 6c C(O)NR 6a R 6b , wherein
each of the said (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl is optionally substituted with at least one R 7 group;
each of the R 5 is independently selected from hydrogen, (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl, wherein
each of the said (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl is optionally substituted with at least one R 7 group;
each of the R 6 , R 6b , and R 6c are independently selected from hydrogen, (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl,
or R 6a and R 6b may be taken together with the nitrogen atom to which they are attached to form a 4 to 8 membered cycloheteroalkyl ring, wherein
said 4 to 8 membered cycloheteroalkyl ring has 1 to 3 ring heteroatoms selected from the group consisting of N, O, and S, and wherein
the said 4 to 8 membered cycloheteroalkyl ring is optionally substituted with at least one R 7 group;
R 7 is independently selected from hydrogen, halogen, OH, CF 3 , (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, cyano, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, (C 2 to C 9 ) heteroaryl, —C(O)R 8 , —C(O)NR 9a R 9b , —NR 9a R 9b , —S(O) m R 8 , —S(O) m NR 9a R 9b , —NR 9a S(O) m R 8 , —(CH 2 ) n C(O)OR 8 , —(CH 2 ) n C(O)N(R 9a R 9b ), —OC(O)R 8 , —NR 9a C(O)R 8 , and —NR 9a C(O)N(R 9a R 9b ), wherein
each of the said (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl, is optionally substituted with at least one R 10 group;
each of the R 8 is independently selected from hydrogen, (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl, wherein
each of the said (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl is optionally substituted with at least one R 10 group;
each of the R 9a , R 9b , and R 9c are independently selected from hydrogen, (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, (C 2 to C 9 ) heteroaryl,
or R 9a and R 9b may be taken together with the nitrogen atom to which they are attached to form a 4 to 8 membered cycloheteroalkyl ring, wherein
said 4 to 8 membered cycloheteroalkyl ring has 1 to 3 ring heteroatoms selected from the group consisting of N, O, and S, and wherein
the said 4 to 8 membered cycloheteroalkyl ring is optionally substituted;
R 10 is independently selected from hydrogen, halogen, cyano, OH, CF 3 , (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl, wherein
each of the said (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl is optionally substituted;
m is 0, 1, or 2;
n is 0, 1, 2, 3, 4, 5, or 6.
2 . The method of claim 1 , wherein:
R 2 is selected from the group consisting of
wherein
R 4b is selected from (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, (C 2 to C 9 ) heteroaryl, —C(O)R 5 , wherein
each of the said (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl is optionally substituted with at least one R 7 group.
3 . The method of claim 2 , wherein:
R 4b is selected from the group consisting of isopropoxy, cyclopropoxy, tert-butoxy, cyclopropylmethoxy, (2-hydroxypropan)-2-yl, (1-hydroxycyclopropan)-1-yl, (1-hydroxycyclobutan)-1-yl, difluoromethoxy, methoxyethoxy, difluoromethyl, cyclopropyl, acetyl, n-propyloxy, n-butyloxy, isobutyloxy, sec-butyloxy, cyclobutyloxy, cyclopentyloxy, (1-hydroxycyclopentan)-1-yl, hydroxyethoxy, ethoxyethoxy, isopropoxyethoxy, isopropyl, n-propyl, n-butyl, isobutyl, sec-butyl, cyclobutyl, cyclopentyl, tert-butyl, propanoyl, isobutanoyl, sec-butanoyl, tert-butanoyl, cyclopropanoyl, cyclobutanoyl, and cyclopentanoyl.
4 . The method of claim 1 , wherein:
G and H are C; J and L are N; K is C—R 3 .
5 . The method of claim 1 , wherein:
G and J are C; H and L are N; K is C—R 3 .
6 . The method of claim 5 , wherein:
A, D, and E are C—R 3 .
7 . The method of claim 1 , wherein:
A, D, and E are independently C—R 3 ; G and H are C; J, K, and L are N.
8 . A method of treating arenavirus infection comprising administration of a therapeutically effective amount of a compound selected from the group consisting of
9 . The method of claim 8 , wherein the compound is selected from the group consisting of
10 . The method of claim 2 including administrating a therapeutic amount of a therapeutic agent selected from the group consisting of Ribavirin, viral RNA-dependent-RNA-polymerase inhibitors, Triazavirin, small interfering RNAs (siRNAs) and microRNAs, vaccines, and immunomodulators.
11 . The method of claim 9 including administrating a therapeutic amount of a therapeutic agent selected from the group consisting of Ribavirin, viral RNA-dependent-RNA-polymerase inhibitors, Triazavirin, small interfering RNAs (siRNAs) and microRNAs, vaccines, and immunomodulators.
12 . A compound of Structural Formula I
or a pharmaceutically acceptable salt, and a pharmaceutically acceptable carrier, diluent, or vehicle thereof, wherein:
A, D, and E are independently N or C—R 3 ;
G, H, and J are independently N or C;
K is N or C—H;
L is N, N—R 3 , or C—R 3 ;
and A, D, E, G, H, J, K, and L together cannot have more than 4 N;
and when G and H are C, and A, D, E, and K are C—R 3 then J and L together cannot be N;
R 1 is selected from (C 6 to C 10 ) aryl, (C 2 to C 9 ) heteroaryl, and 5-indolyl, wherein
each of the said (C 6 to C 10 ) aryl and (C 2 to C 9 ) heteroaryl is substituted with at least one R 4a group, and wherein said (C 2 to C 9 ) heteroaryl is C-attached;
with the proviso that R 1 is not selected from the group consisting of substituted 3-carbamoyl-2-phenyl-1-benzofuran-5-yl, substituted 1,3,4-oxadiazolyl, substituted 1,3,4-triazolyl, substituted 1,3,4-thiadiazolyl, substituted oxazoyl, substituted thiazoyl, substituted 1H-pyrazol-4-yl, substituted 1H-pyrazol-5-yl, optionally substituted 1-phenyl-1H-imidazol-5-yl, 4-{[(2-aminoethyl)amino]methyl}phenyl, (2-amino-1,3-benzoxazol)-5-yl; (2-amino-1,3-benzoxazol)-4-yl, 2-chloropyridyl-3-yl, 2-methylpyridinyl-4-yl, 2-fluoropyridyl-4-yl, 6-aminopyridyl-3-yl, 6-methoxypyridyl-3-yl, pyridyl-4-yl-N-oxide, 3,4-difluorophenyl, and substituted 1H-pyrrol-3-yl;
R 2 is selected from the group consisting of
each of the R 3 is independently selected from hydrogen, halogen, cyano, OH, CF 3 , (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, (C 2 to C 9 ) heteroaryl, —C(O)R 5 , —C(O)NR 6a R 6b , —NR 6a R 6b , —S(O) m R 5 , —S(O) m NR 6a R 6b , —NR 6a S(O) m R 5 , —(CH 2 ) n C(O)OR 5 , —(CH 2 ) n C(O)NR 6a R 6b , —OC(O)R 5 , —NR 6a C(O)R 5 , and —NR 6c C(O)NR 5a R 5b , wherein
each of the said (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl is optionally substituted with at least one R 7 group;
R 4a is independently selected from halogen, cyano, OH, CF 3 , (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, (C 3 to C 10 ) cycloalkyl, (C to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, (C 2 to C 9 ) heteroaryl, —C(O)R 5 , —NR 6a R 6b , —S(O) m R 5 , —S(O) m NR 6a R 6b , —NR 6a S(O) m R 5 , —OC(O)R 5 , —NR 6a C(O)R 5 , and —NR 6c C(O)NR 6a R 6b , wherein
each of the said (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl is optionally substituted with at least one R 7 group;
R 4b is selected from the group consisting of
isopropoxy, cyclopropoxy, tert-butoxy, cyclopropylmethoxy, (2-hydroxypropan)-2-yl, (1-hydroxycyclopropan)-1-yl, (1-hydroxycyclobutan)-1-yl, difluoromethoxy, methoxyethoxy, difluoromethyl, cyclopropyl, acetyl, n-propyloxy, n-butyloxy, isobutyloxy, sec-butyloxy, cyclobutyloxy, cyclopentyloxy, (1-hydroxycyclopentan)-1-yl, hydroxyethoxy, ethoxyethoxy, isopropoxyethoxy, isopropyl, n-propyl, n-butyl, sec-butyl, cyclobutyl, cyclopentyl, propanoyl, isobutanoyl, sec-butanoyl, tert-butanoyl, cyclopropanoyl, cyclobutanoyl, and cyclopentanoyl;
each of the R 5 is independently selected from hydrogen, (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl, wherein
each of the said (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl is optionally substituted with at least one R 7 group;
each of the R 6a , R 6b , and R 6c are independently selected from hydrogen, (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl,
or R 6a and R 6b may be taken together with the nitrogen atom to which they are attached to form a 4 to 8 membered cycloheteroalkyl ring, wherein
said 4 to 8 membered cycloheteroalkyl ring has 1 to 3 ring heteroatoms selected from the group consisting of N, O, and S, and wherein
the said 4 to 8 membered cycloheteroalkyl ring is optionally substituted with at least one R 7 group;
R 7 is independently selected from hydrogen, halogen, OH, CF 3 , (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, cyano, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, (C 2 to C 9 ) heteroaryl, —C(O)R 8 , —C(O)NR 9a R 9b , —NR 9a R 9b , —S(O) m R 8 , —S(O) m NR 9a R 9b , —NR 9a S(O) m R 8 , —(CH 2 ) n C(O)OR 8 , —(CH 2 ) n C(O)N(R 9a R 9b ), —OC(O)R 8 , —NR 9a C(O)R 8 , and —NR 9a C(O)N(R 9a R 9b ), wherein
each of the said (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl, is optionally substituted with at least one R 10 group;
each of the R 8 is independently selected from hydrogen, (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl, wherein
each of the said (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl is optionally substituted with at least one R 10 group;
each of the R 9a , R 9b , and R 9c are independently selected from hydrogen, (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, (C 2 to C 9 ) heteroaryl,
or R 9a and R 9b may be taken together with the nitrogen atom to which they are attached to form a 4 to 8 membered cycloheteroalkyl ring, wherein
said 4 to 8 membered cycloheteroalkyl ring has 1 to 3 ring heteroatoms selected from the group consisting of N, O, and S, and wherein
the said 4 to 8 membered cycloheteroalkyl ring is optionally substituted;
R 10 is independently selected from hydrogen, halogen, cyano, OH, CF 3 , (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl, wherein
each of the said (C 1 to C 6 ) alkyl, (C 2 to C 6 ) alkenyl, (C 2 to C 6 ) alkynyl, (C 1 to C 6 ) alkoxy, aryloxy, (C 3 to C 10 ) cycloalkyl, (C 5 to C 10 ) cycloalkenyl, (C 2 to C 9 ) cycloheteroalkyl, (C 6 to C 10 ) aryl, and (C 2 to C 9 ) heteroaryl is optionally substituted;
m is 0, 1, or 2;
n is 1, 2, 3, 4, 5, or 6;
with the proviso that
the following compounds are excluded:
13 . The compound of claim 12 , wherein R 4b is isopropoxy.
14 . The compound of claim 12 , wherein:
G and H are C; J and L are N; K is C—H.
15 . The compound of claim 13 , wherein:
G and H are C; J and L are N; K is C—H.
16 . The compound of claim 14 , wherein:
D and E are independently C—R 3 ; A is N.
17 . The compound of claim 14 , wherein:
A and E are independently C—R 3 ; D is N.
18 . The compound of claim 14 , wherein:
E is C—R 3 ; A and D are N.
19 . The compound of claim 12 , wherein:
G and H are C; J is N; K is CH; L is C—R 3 .
20 . The compound of claim 12 , wherein:
G and H are C; J and K are N; L is C—R 3 .
21 . The compound of claim 12 , wherein:
G, H, and J are C; K and L are independently is N or N—R 3 .
22 . The compound of claim 12 , wherein:
G and J are C; H and L are N; K is C—H.
23 . The compound of claim 13 , wherein:
G and J are C; H and L are N; K is C—H.
24 . The compound of claim 22 , wherein:
A, D, and E are C—R 3 .
25 . The compound of claim 23 , wherein:
A, D, and E are independently C—R 3 .
26 . The compound of claim 23 , wherein:
A is N; D and E are independently C—R 3 .
27 . The compound of claim 23 , wherein:
A and D are independently C—R 3 ; E is N.
28 . The compound of claim 12 , wherein:
A, D, and E are independently C—R 3 , G and H are C; J, K, and L are N.
29 . The compound of claim 13 , wherein:
A, D, and E are independently C—R 3 ; G and H are C; J, K, and L are N.
30 . The compound of claim 12 , wherein:
A, D, and E are independently C—R 3 ; G and J are C; H, K, and L are N.
31 . A compound selected from the group consisting of
32 . The compound of claim 31 , wherein the compound is selected from the group consisting of
33 . The compound of claim 12 , wherein said compound is incorporated into a composition comprising a therapeutically effective amount of said compound, and a pharmaceutically acceptable carrier, diluent, or vehicle.
34 . The compound of claim 32 , wherein said compound is incorporated into a composition comprising a therapeutically effective amount of said compound, and a pharmaceutically acceptable carrier, diluent, or vehicle.Cited by (0)
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