Abstract: Anti-viral compounds effective in inhibiting replication of Hepatitis C virus ("HCV").
1. A compound of Formula I, or a pharmaceutically acceptable salt thereof, wherein: X is C3-C12carbocycle or 3- to 12-membered heterocycle, and is optionally substituted with one or more RA; L1 and L2 are each independently selected from bond; or C1-C6alkylene, C2- C6alkenylene or C2-C6alkynylene, each of which is independently optionally substituted at each occurrence with one or more RL; L3 is bond or -Ls-K-Ls'-, wherein K is selected from bond, -O-, -S-, -N(RB)-, - C(O)-, -S(O)2- -S(O)- -OS(O)-, -OS(O)2-, -S(O)2O-, -S(O)O-, -C(O)O-, - OC(O)-, -OC(O)O- -C(O)N(RB)-, -N(RB)C(O)-, -N(RB)C(O)O-, - OC(O)N(RB)-, -N(RB)S(O)-, -N(RB)S(O)2-, -S(O)N(RB)- -S(O)2N(RB)-, - C(O)N(RB)C(O)-, -N(RB)C(O)N(RB')-, -N(RB)SO2N(RB')- or N(RB)S(O)N(RB')-; A and B are each independently C3-C12carbocycle or 3- to 12-membered heterocycle, and are each independently optionally substituted with one or more RA; D is C3-C12carbocycle or 3- to 12-membered heterocycle, and is optionally substituted with one or more RA; Y is selected from -T'-C(R1R2)N(R5)-T-RD, -T'-C(R3R4)C(R6R7)-T-RD, -LK-T-RD, or -LK-E; R1 and R2 are each independently Rc, and R5 is RB; or R1 is Rc, and R2 and R5, taken togemer with the atoms to which they are attached, form a 3- to 12-membered heterocycle which is optionally substituted with one or more RA; R3, R4, R6, and R7 are each independently Rc; or R3 and R6 are each independently Rc, and R4 and R7, taken together with the atoms to which they are attached, form a 3- to 12-membered carbocycle or heterocycle which is optionally substituted with one or more RA; Z is selected from -T'-C(R8R9)N(R12)-T-RD, -T'-C(R10R11)C(R13R14)-T-RD, -Lk-T- RD, or -LK-E; R8 and R9 are each independently Rc, and R12 is RB; or R8 is Rc, and R9 and R12, taken together with the atoms to which they are attached, form a 3- to 12-membered heterocycle which is optionally substituted with one or more RA; R10, R11, R13, and R14 are each independently Rc; or R10 and R13 are each independently Rc, and R11 and R14, taken together with the atoms to which they are attached, form a 3- to 12-membered carbocycle or heterocycle which is optionally substituted with one or more RA; T and T are each independently selected at each occurrence from bond, -Ls-, -Ls- M-Ls'-, or -Ls-M-Ls'-M'-Ls"-, wherein M and M' are each independently selected at each occurrence from bond, -O-, -S-, -N(RB)-, -C(O)-, -S(O)2-, - S(O)-, -OS(O)-, -OS(O)2- -S(O)2O-, -S(O)O-, -C(O)O-, -OC(O)-, - OC(O)CK -C(O)N(RB)-, -N(RB)C(O)-, -N(RB)C(O)O-, -OC(O)N(RB)-, - N(RB)S(O)-, -N(RB)S(O)2- -S(O)N(RB)-, -S(O)2N(RB)-, -C(O)N(RB)C(O)-, - N(RB)C(O)N(RB')-, -N(RB)SO2N(RB')-, -N(RB)S(O)N(RB'K C3-C12carbocycle or 3- to 12-membered heterocycle, and wherein said C3-Ci2carbocycle and 3- to 12-membered heterocycle are each independently optionally substituted at each occurrence with one or more RA; LK is independently selected at each occurrence from bond, -LS-N(RB)C(O)-LS'- or - LS-C(O)N(RB)-LS'-; or C1-C6alkylene, C2-C6alkenylene or C2-C6alkynylene, each of which is independently optionally substituted at each occurrence with one or more RL; or C3-C12carbocycle or 3- to 12-membered heterocycle, each of which is independently optionally substituted at each occurrence with one or more RA; E is independently selected at each occurrence from C3-C12carbocycle or 3- to 12- membered heterocycle, and is independently optionally substituted at each occurrence with one or more RA; RD is each independently selected at each occurrence from hydrogen or RA; RA is independently selected at each occurrence from halogen, nitro, oxo, phosphonoxy, phosphono, thioxo, cyano, or -LS-RE, wherein two adjacent RA, taken together with the atoms to which they are attached and any atoms between the atoms to which they are attached, can optionally form carbocycle or heterocycle; RB and RB' are each independently selected at each occurrence from hydrogen; or Cr C6alkyl, C2-C6alkenyl or C2-C6alkynyl, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano or 3- to 6-membered carbocycle or heterocycle; or 3- to 6-membered carbocycle or heterocycle; wherein each 3- to 6-membered carbocycle or heterocycle in RB or RB' is independendy optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C1-C6haloalkyl, C2-C6haloalkenyl or C2-C6haloalkynyl; Rc is independently selected at each occurrence from hydrogen, halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl or cyano; or C1-C6alkyl, C2-C6alkenyl or C2-C6alkynyl, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano or 3- to 6-membered carbocycle or heterocycle; or 3- to 6-membered carbocycle or heterocycle; wherein each 3- to 6-membered carbocycle or heterocycle in Rc is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C1- C6haloalkyl, C2-C6haloalkenyl or C2-C6haloalkynyl; RE is independently selected at each occurrence from -O-Rs, -S-Rs, -C(O)Rs, - OC(O)Rs, -C(O)ORs, -N(RsRs'), -S(O)Rs, -SO2Rs, -C(O)N(RsRs'), - N(Rs)C(O)Rs', -N(Rs)C(O)N(Rs'Rs"), -N(Rs)SO2Rs', -SO2N(RsRs'), - N(Rs)SO2N(Rs'Rs"), -N(Rs)S(O)N(Rs'Rs"), -0S(O)-RS, -OS(O)2-Rs, - S(O)2ORs, -S(O)ORs, -OC(O)ORs, -N(Rs)C(O)ORs', -OC(O)N(RsRs'), - N(Rs)S(O)-Rs', -S(O)N(RsRs') or -C(O)N(RS)C(O)-Rs'; or d-Caalkyl, C2- C6alkenyl or C2-C6alkynyl, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl or cyano; or C3-C6carbocycle or 3- to 6-membered heterocycle, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C1-C6haloalkyl, C2-C6haloalkenyl or C2-C6haloalkynyl; RL is independently selected at each occurrence from halogen, nitro, oxo, phosphonoxy, phosphono, thioxo, cyano, -O-Rs, -S-Rs, -C(O)Rs, -OC(O)Rs, - C(O)ORs, -N(RsRs'), -S(O)Rs, -SO2Rs, -C(O)N(RsRs') or -N(Rs)C(O)Rs'; or C3-C6carbocycle 3- to 6-membered heterocycle, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C1- C6haloalkyl, C2-C6haloalkenyl or C2-C6haloalkynyl; Ls, Ls' and Ls" are each independently selected at each occurrence from bond; or C1- C6alkylene, C2-C6alkenylene or C2-C6alkynylene, each of which is independently optionally substituted at each occurrence with one or more RL; and Rs, Rs' and Rs" are each independently selected at each occurrence from hydrogen; C1-C6alkyl, C2-C6alkenyl or C2-C6alkynyl, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano or 3- to 6-membered carbocycle or heterocycle; or 3- to 6-membered carbocycle or heterocycle; wherein each 3- to 6-membered carbocycle or heterocycle in Rs, Rs' or Rs' is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C1-C6haloalkyl, C2-C6haloalkenyl or C2-C6haloalkynyl; with the proviso that said compound is not: dimethyl (2S,2'S)-1,1,-((2S,2'S)-2,2'-(4,4'-((2S,5S)-l-(4-fluorophenyl)pyrrolidine-2,5- diyl)bis(4,1 -phenylene))bis(azanediyl)bis(oxomethylene)bis(pyrrolidine-2,1 -diyl))bis(3- methyl-1 -oxobutane-2,1 -diyl)dicarbamate, dimethyl (2S,2,S)-1,1-((2S,2'S)-2,2'-(4,4'-((2S,5S)-l-(4-tert-butylphenyl)pyrrolidine- 2,5-diyl)bis(4,1 -phenylene))bis(azanediyl)bis(oxomethylene)bis(pyrrolidine-2,1 -diyl))bis(3- methyl-1 -oxobutane-2,1 -diyl)dicarbamate, dimethyl (2S,2,S)-1,1'-((2S)2'S)-2,2'-(4,4,-((2R,5R)-l-(4-rert-butylphenyl)pyrrolidine- 2,5-diyl)bis(4,1 -phenylene))bis(azanediyl)bis(oxomethylene)bis(pyrrolidine-2,1 -diyl))bis(3- methyl-1 -oxobutane-2,1 -diyl)dicarbamate, or methyl [(2S)-l-{(2S)-2-[4-(4-{5-(4-{2-[(2S)-l-{(2S)-2-[(methoxycarbonyl)amino]-3- methylbutanoyl} pyrrolidin-2-yl] -1 H-imidazol-4-yl} phenyl)-1 - [6-(piperidin-1 -yl)pyridin-3- yl] -1 H-pyrrol-2-yl} phenyl)-1 H-imidazol-2-yl]pyrrolidin-1 -yl} - 3-methyl-1 -oxobutan-2- yl]carbamate; with the further proviso that A is not which is optionally substituted with one or more RA; or B is not which is optionally substituted with one or more RA; wherein Z1 is independently selected at each occurrence from O, S, NH or CH2, and Z2 is independently selected at each occurrence from N or CH.
2. The compound or salt of claim 1, wherein: A is selected from C5-C6carbocycle, 5- to 6-membered heterocycle, and is optionally substituted with one or more RA; B is selected from C5-C6carbocycle, 5- to 6-membered heterocycle, and is optionally substituted with one or more RA; D is selected from C5-C6carbocycle or 5- to 6-membered heterocycle, and is optionally substituted with one or more RA; Z1 is independently selected at each occurrence from O, S, NH or CH2; Z2 is independently selected at each occurrence from N or CH; Z3 is independently selected at each occurrence from N or CH; Z4 is independently selected at each occurrence from O, S, NH or CH2; and W1, W2, W3, W4, W5 and W6 are each independently selected at each occurrence from CH or N..
3. The compound or salt of claim 1, wherein: A is selected from C5-C6carbocycle, 5- to 6-membered heterocycle, and is optionally substituted with one or more RA; B is selected from C5-C6carbocycle, 5- to 6-membered heterocycle, and is optionally substituted with one or more RA; D is selected from C5-C6carbocycle or 5- to 6-membered heterocycle, and is optionally substituted with one or more RA; Z1 is independently selected at each occurrence from O, S, NH or CH2; Z2 is independently selected at each occurrence from N or CH; and W1, W2, W3, W4, W5 and W6 are each independently selected at each occurrence from CH or N.
4. The compound or salt of claim 1, wherein: A and B are each independently C5-C6carbocycle or 5- to 6-membered heterocycle, and are each independently optionally substituted with one or more RA', D is selected from C5-C6carbocycle or 5- to 6-membered heterocycle, and is optionally substituted with one or more RA; and wherein X3 is N and is directly linked to - L3-D, and X is optionally substituted with one or more RA, and two adjacent RA on X, taken together with the ring atoms to which they are attached, optionally form a 5- to 6-membered carbocycle or heterocycle.
5. The compound or salt of claim 1, wherein: wherein the nitrogen ring atom is directly linked to -L3-D, and wherein X is optionally substituted with one or more RA; L1, L2 and L3 are bond; A and B are each independently and are each independently optionally substituted with one or more RA; D is C3-C12carbocycle or 3- to 12-membered heterocycle, and is optionally substituted with one or more RA; Y is -G-C(RiR2)N(R5)-T-RD, -G-C(R3R4)C(R6R7)-T-RD, N(RB)C(O)C(R,R2)N(R5)-T-RD, or -N(RB)C(O)C(R3R4)C(R6R7)-T-RD; Z is -G-C(R8R9)N(R12)-T-RD, -G-C(R10R11)C(R13R14)-T-RD, N(RB)C(O)C(R8R9)N(RI2)-T-RD, or -N(RB)C(O)C(R10R11)C(R13R14)-T-RD; R1 is Rc, and R2 and R5, taken together with the atoms to which they are attached, form a 3- to 12-membered heterocycle which is optionally substituted with one or more RA; R3 and R6 are each independently Rc, and R4 and R7, taken together with the atoms to which they are attached, form a 3- to 12-membered carbocycle or heterocycle which is optionally substituted with one or more RA; R8 is Rc, and R9 and R12, taken together with the atoms to which they are attached, form a 3- to 12-membered heterocycle which is optionally substituted with one or more RA; R10 and R13 are each independently Rc, and R11 and R14, taken together with the atoms to which they are attached, form a 3- to 12-membered carbocycle or heterocycle which is optionally substituted with one or more RA; G is each independently C5-C6carbocycle or 5- to 6-membered heterocycle, and is each independently optionally substituted with one or more RA; T is each independently selected at each occurrence from bond, -Ls-, -Ls-M-Ls'-, or -Ls-M-Ls'-M'-Ls"-, wherein M and M' are each independently selected at each occurrence from bond, -O-, -S-, -N(RB)-, -C(O)-, -S(O)2- -S(O)-, -OS(O)-, - OS(O)2-, -S(O)2O-, -S(O)O-, -C(O)O- -OC(O)-, -OC(O)O-, -C(O)N(RB)-, - N(RB)C(O)-, -N(RB)C(O)O-, -OC(O)N(RB)-, -N(RB)S(O)-, -N(RB)S(O)2-, - S(O)N(RB)-, -S(O)2N(RB)-, -C(O)N(RB)C(O)-, -N(RB)C(O)N(RB')-, - N(RB)SO2N(RB')-, -N(RB)S(O)N(RB')-, C3-C12carbocycle or 3- to 12-membered heterocycle, and wherein said C3-C12carbocycle and 3- to 12-membered heterocycle are each independently optionally substituted at each occurrence with one or more RA; RD is each independently selected at each occurrence from hydrogen or RA; RA is independently selected at each occurrence from halogen, nitro, oxo, phosphonoxy, phosphono, thioxo, cyano, or -LS-RE; RB and RB' are each independently selected at each occurrence from hydrogen; or C1- C6alkyl, C2-C6alkenyl or C2-C6alkynyl, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano or 3- to 6-membered carbocycle or heterocycle; or 3- to 6-membered carbocycle or heterocycle; wherein each 3- to 6-membered carbocycle or heterocycle in RB or RB' is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano, C1-C6a]kyl, C2-C6alkenyl, C2-C6alkynyl, C1-C6haloalkyl, C2-C6haloalkenyl or C2-C6haloalkynyl; Rc is independently selected at each occurrence from hydrogen, halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl or cyano; or C1-C6alkyl, C2-C6alkenyl or C2-C6alkynyl, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano or 3- to 6-membered carbocycle or heterocycle; or 3- to 6-membered carbocycle or heterocycle; wherein each 3- to 6-membered carbocycle or heterocycle in Rc is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C1- C6haloalkyl, C2-C6haloalkenyl or C2-C6haloalkynyl; RE is independently selected at each occurrence from -O-Rs, -S-Rs, -C(O)Rs, - OC(O)Rs, -C(O)ORs, -N(RsRs'), -S(O)Rs, -SO2Rs, -C(O)N(RsRs'), - N(Rs)C(O)Rs', -N(Rs)C(O)N(Rs'Rs"), -N(RS)SO2RS', -SO2N(RsRs'), - N(Rs)SO2N(Rs'Rs"), -N(Rs)S(O)N(Rs'Rs"), -OS(O)-Rs, -0S(O)2-Rs, - S(O)2ORs, -S(O)ORs, -OC(O)ORs, -N(Rs)C(O)ORs', -OC(O)N(RsRs'), - N(Rs)S(O)-Rs', -S(O)N(RsRs') or -C(O)N(RS)C(O)-RS'; or C1-C6alkyl, C2- C6alkenyl or C2-C6alkynyl, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl or cyano; or C3-C6carbocycle or 3- to 6-membered heterocycle, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C1-C6haloalkyl, C2-C6haloalkenyl or C2-C6haloalkynyl; RL is independently selected at each occurrence from halogen, nitro, oxo, phosphonoxy, phosphono, thioxo, cyano, -O-Rs, -S-Rs, -C(O)Rs, -OC(O)Rs, - C(O)ORs, -N(RsRs'), -S(O)Rs, -SO2Rs, -C(O)N(RsRs') or -N(Rs)C(O)Rs'; or C3-C6carbocycle 3- to 6-membered heterocycle, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C1- C6haloalkyl, C2-C6haloalkenyl or C2-C6haloalkynyl; Ls, Ls' and Ls" are each independently selected at each occurrence from bond; or C1- C6alkylene, C2-C6alkenylene or C2-C6alkynylene, each of which is independently optionally substituted at each occurrence with one or more RL; and Rs, Rs' and Rs'' are each independently selected at each occurrence from hydrogen; C1-C6alkyl, C2-C6alkenyl or C2-C6alkynyl, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano or 3- to 6-membered carbocycle or heterocycle; or 3- to 6-membered carbocycle or heterocycle; wherein each 3- to 6-membered carbocycle or heterocycle in Rs, Rs' or Rs' is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C1-C6haloalkyl, C2-C6haloalkenyl or C2-C6haloalkynyl.
6. The compound or salt of claim 5, wherein: T is independently selected at each occurrence from -C(O)-Ls'-M'-Ls"- or - N(RB)C(O)-LS'-M'-LS"-; and Ls' is each independently C1-C6alkylene, and is independently optionally substituted at each occurrence with one or more RL.
7. The compound or salt of claim 5, wherein: Y is -N(RB)C(O)C(R1R2)N(R5)-T-RD; Z is -N(RB)C(O)C(R8R9)N(R12)-T-RD; T is independently selected at each occurrence from -C(O)-Ls'-M'-Ls"-; and D is C5-C6carbocycle, 5- to 6-membered heterocycle, or 6- to 10-membered bicycles, and is substituted with one or more RA.
8. The compound or salt of claim 7, wherein T is independendy selected at each occurrence from -C(O)-LS'-N(RB)C(O)-LS"- or -C(O)-Ls'-N(RB)C(O)O-Ls"-; and R2 and R5, taken together with the atoms to which they are attached, form which is optionally substituted with one or more RA; and R9 and R12, taken together with the atoms to which they are attached, form which is optionally substituted with one or more RA.
9. The compound or salt of claim 5, wherein: Y is -G-C(R1R2)N(R5)-T-RD; Z is -G-C(R8R9)N(R12)-T-RD; G is each independently and is each independently optionally substituted with one or more RA; T is independently selected at each occurrence from -C(O)-Ls'-M'-Ls"-; and D is C5-C6carbocycle, 5- to 6-membered heterocycle, or 6- to 10-membered bicycles, and is substituted with one or more RA.
10. The compound or salt of claim 9, wherein T is independently selected at each occurrence from -C(O)-Ls'-N(RB)C(O)-Ls"- or -C(O)-Ls'-N(RB)C(O)O-Ls"-; and R2 and R5, taken together with the atoms to which they are attached, form which is optionally substituted with one or more RA; and R9 and R12, taken together with the atoms to which they are attached, form which is optionally substituted with one or more RA.
11. The compound or salt of claim 1, wherein said compound has Formula IA, wherein: RNB is each independently selected from RB; Rc' is each independently selected from Rc; RD' is each independently selected from RD; R2 and R5, taken together with the atoms to which they are attached, form a 3- to 12- membered heterocycle which is optionally substituted with one or more RA; R9 and R12, taken together with the atoms to which they are attached, form a 3- to 12-membered heterocycle which is optionally substituted with one or more RA, and A and B are each independently and are each independently optionally substituted with one or more RA.
12. The compound or salt of claim 11, wherein X is and is optionally substituted with one or more RA, wherein X3 is N and is directly linked to -L3-D, and wherein L1, L2 and L3 are bond.
13. The compound or salt of claim 1, wherein said compound has Formula IB, wherein: Rc' is each independently selected from Rc; RD' is each independently selected from RD; R2 and R5, taken together with the atoms to which they are attached, form a 3- to 12- membered heterocycle which is optionally substituted with one or more RA; R9 and R12, taken together with the atoms to which they are attached, form a 3- to 12-membered heterocycle which is optionally substituted with one or more RA; A is and is optionally substituted with one or more RA; and B is and is optionally substituted with one or more RA.
14. The compound or salt of claim 13, wherein X is and is optionally substituted wim one or more RA, wherein X3 is N and is directly linked to -L3-D, and wherein L1, L2 and L3 are bond.
15. The compound or salt of claim 1, wherein: X is C3-C12carbocycle or 3- to 12-membered heterocycle, and is optionally substituted with one or more RA; L1 and L2 are each independendy selected from bond; or C1-C6alkylene, C2- C6alkenylene or C2-C6alkynylene, each of which is independently optionally substituted at each occurrence with one or more RL; L3 is bond or -Ls-K-Ls'-, wherein K is selected from bond, -O-, -S-, -N(RB)-, - C(O)-, -S(O)2-, -S(O)-, -OS(O)-, -OS(O)2- -S(O)2O-, -S(O)O- -C(O)O-, - OC(O)-, -OC(O)O-, -C(O)N(RB)-, -N(RB)C(O)-, -N(RB)C(O)O-, - OC(O)N(RB)-, -N(RB)S(O)-, -N(RB)S(O)2- -S(O)N(RB)-, -S(O)2N(RB)-, - C(O)N(RB)C(O)-, -N(RB)C(O)N(RB')- -N(RB)SO2N(RB')-, or N(RB)S(O)N(RB')-; A and B are each independently C3-C12carbocycle or 3- to 12-membered heterocycle, and are each independently optionally substituted with one or more RA; D is C3-C12carbocycle or 3- to 12-membered heterocycle, which is substituted with J and optionally substituted with one or more RA, wherein J is C3-C12carbocycle or 3- to 12-membered heterocycle and is optionally substituted with one or more RA, or J is -SF5; Y is selected from -T'-C(R1R2)N(R5)-T-RD, -T'-C(R3R4)C(R6R7)-T-RD, -LK-T-RD, or -LK-E; RI and R2 are each independently Re, and Rs is RB; or Ri is Re, and R2 and Rs, taken together with the atoms to which they are attached, form a 3- to 12-membered heterocycle which is optionally substituted with one or more RA", R3, R4, R6, and R7 are each independently Rc; or R3 and R6 are each independently Rc, and R4 and R7, taken together with the atoms to which they are attached, form a 3- to 12-membered carbocycle or heterocycle which is optionally substituted with one or more RA; Z is selected from -T'-C(R8R9)N(R12)-T-RD, -T'-C(R10R11)C(R13R14)-T-RD, -Lk-T- RD, or -LK-E; R8 and R9 are each independently Rc, and R12 is RB; or R8 is Rc, and R9 and R12, taken together with the atoms to which they are attached, form a 3- to 12-membered heterocycle which is optionally substituted with one or more RA; R10, R11, R13, and R14 are each independently Rc; or R10 and R13 are each independently Rc, and R11 and R14, taken together with the atoms to which they are attached, form a 3- to 12-membered carbocycle or heterocycle which is optionally substituted with one or more RA; T and 1" are each independently selected at each occurrence from bond, -Ls-, -Ls- M-Ls'-, or -Ls-M-Ls'-M'-Ls"-, wherein M and M' are each independently selected at each occurrence from bond, -O-, -S-, -N(RB)-, -C(O)-, -S(O)2-, - S(O)-, -OS(O)-, -OS(O)2- -S(O)2O-, -S(O)O-, -C(O)O-, -OC(O)-, - OC(O)O-, -C(O)N(RB)-, -N(RB)C(O)-, -N(RB)C(O)O-, -OC(O)N(RB)-, - N(RB)S(O)-, -N(RB)S(O)2- -S(O)N(RB)-, -S(O)2N(RB)-, -C(O)N(RB)C(O)-, - N(RB)C(O)N(RB')-, -N(RB)SO2N(RB')-, -N(RB)S(O)N(RB')-, C3-C12carbocycle or 3- to 12-membered heterocycle, and wherein said C3-C12carbocycle and 3- to 12-membered heterocycle are each independently optionally substituted at each occurrence with one or more RA; LK is independently selected at each occurrence from bond, -Ls-N(RB)C(O)-Ls'- or - Ls-C(O)N(RB)-Ls'-; or C1-C6alkylene, C2-C6alkenylene or C2-C6alkynylene, each of which is independently optionally substituted at each occurrence with one or more RL; or C3-C12carbocycle or 3- to 12-membered heterocycle, each of which is independently optionally substituted at each occurrence with one or more RA; E is independently selected at each occurrence from C3-C12carbocycle or 3- to 12- membered heterocycle, and is independently optionally substituted at each occurrence with one or more RA; RD is each independently selected at each occurrence from hydrogen or RA; RA is independently selected at each occurrence from halogen, nitro, oxo, phosphonoxy, phosphono, thioxo, cyano, or -LS-RE, wherein two adjacent RA, taken together with the atoms to which they are attached and any atoms between the atoms to which they are attached, can optionally form carbocycle or heterocycle; RB and RB' are each independently selected at each occurrence from hydrogen; or C1- C6alkyl, C2-C6alkenyl or C2-C6alkynyl, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano or 3- to 6-membered carbocycle or heterocycle; or 3- to 6-membered carbocycle or heterocycle; wherein each 3- to 6-membered carbocycle or heterocycle in RB or RB' is independendy optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C1-C6haloalkyl, C2-C6haloalkenyl or C2-C6haloalkynyl; Rc is independently selected at each occurrence from hydrogen, halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl or cyano; or C1-C6alkyl, C2-C6alkenyl or C2-C6alkynyl, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano or 3- to 6-membered carbocycle or heterocycle; or 3- to 6-membered carbocycle or heterocycle; wherein each 3- to 6-membered carbocycle or heterocycle in Rc is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C1- C6haloalkyl, C2-C6haloalkenyl or C2-C6haloalkynyl; RE is independently selected at each occurrence from -O-Rs, -S-Rs, -C(O)Rs, - OC(O)Rs, -C(O)ORs, -N(RsRs'), -S(O)Rs, -SO2Rs, -C(O)N(RsRs'), - N(Rs)C(O)Rs', -N(Rs)C(O)N(Rs'Rs"), -N(Rs)SO2Rs', -SO2N(RsRs'), - N(Rs)SO2N(Rs'Rs"), -N(Rs)S(O)N(Rs'Rs"), -OS(O)-Rs, -OS(O)2-Rs, - S(O)2ORs, -S(O)ORs, -OC(O)ORs, -N(Rs)C(O)ORs', -OC(O)N(RsRs'), - N(Rs)S(O)-Rs', -S(O)N(RsRs') or -C(O)N(Rs)C(O)-Rs'; or C1-C6alkyl, C2- C6alkenyl or C2-C6alkynyl, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl or cyano; or C3-C6carbocycle or 3- to 6-membered heterocycle, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C1-C6haloalkyl, C2-C6haloalkenyl or C2-C6haloalkynyl; RL is independendy selected at each occurrence from halogen, nitro, oxo, phosphonoxy, phosphono, thioxo, cyano, -O-Rs, -S-Rs, -C(O)Rs, -OC(O)Rs, - C(O)ORs, -N(RsRs'), -S(O)Rs, -SO2Rs, -C(O)N(RsRs') or -N(Rs)C(O)Rs'; or C3-C6carbocycle 3- to 6-membered heterocycle, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C1- C6haloalkyl, C2-C6haloalkenyl or C2-C6haloalkynyl; Ls, Ls' and Ls" are each independently selected at each occurrence from bond; or C1- C6alkylene, C2-C6alkenylene or C2-C6alkynylene, each of which is independently optionally substituted at each occurrence with one or more RL; and Rs, Rs' and Rs" are each independently selected at each occurrence from hydrogen; C1-C6alkyl, C2-C6alkenyl or C2-C6alkynyl, each of which is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano or 3- to 6-membered carbocycle or heterocycle; or 3- to 6-membered carbocycle or heterocycle; wherein each 3- to 6-membered carbocycle or heterocycle in Rs, Rs' or Rs' is independently optionally substituted at each occurrence with one or more substituents selected from halogen, hydroxy, mercapto, amino, carboxy, nitro, oxo, phosphonoxy, phosphono, thioxo, formyl, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C1-C6haloalkyl, C2-C6haloalkenyl or C2-C6haloalkynyl.
16. The compound or salt of claim 15, wherein D is C5-C6carbocycle or 5- to 6- membered heterocycle and is optionally substituted with one or more RA, and J is C3- C6carbocycle or 3- to 6-membered heterocycle and is optionally substituted with one or more RA.
17. The compound or salt of claim 15, wherein D is and each RN is independently selected from RD.
18. The compound or salt of claim 15, wherein X is and is optionally substituted with one or more RA, wherein X3 is N and is directly linked to -L3-D, and wherein L1, L2 and L3 are bond.
| # | Name | Date |
|---|---|---|
| 1 | 1423-kolnp-2013-(09-05-2013)-SPECIFICATION.pdf | 2013-05-09 |
| 2 | 1423-kolnp-2013-(09-05-2013)-FORM-5.pdf | 2013-05-09 |
| 3 | 1423-kolnp-2013-(09-05-2013)-FORM-3.pdf | 2013-05-09 |
| 4 | 1423-kolnp-2013-(09-05-2013)-FORM-2.pdf | 2013-05-09 |
| 5 | 1423-kolnp-2013-(09-05-2013)-FORM-1.pdf | 2013-05-09 |
| 6 | 1423-kolnp-2013-(09-05-2013)-DESCRIPTION (COMPLETE).pdf | 2013-05-09 |
| 7 | 1423-kolnp-2013-(09-05-2013)-CORRESPONDENCE.pdf | 2013-05-09 |
| 8 | 1423-kolnp-2013-(09-05-2013)-CLAIMS.pdf | 2013-05-09 |
| 9 | 1423-kolnp-2013-(09-05-2013)-ABSTRACT.pdf | 2013-05-09 |
| 10 | 1423-KOLNP-2013-(08-11-2013)-PRIORITY DOCUMENT.pdf | 2013-11-08 |
| 11 | 1423-KOLNP-2013-(08-11-2013)-PRIORITY DOCUMENT-1.1.pdf | 2013-11-08 |
| 12 | 1423-KOLNP-2013-(08-11-2013)-PA.pdf | 2013-11-08 |
| 13 | 1423-KOLNP-2013-(08-11-2013)-FORM-3.pdf | 2013-11-08 |
| 14 | 1423-KOLNP-2013-(08-11-2013)-CORRESPONDENCE.pdf | 2013-11-08 |
| 15 | 1423-KOLNP-2013-(08-11-2013)-ASSIGNMENT.pdf | 2013-11-08 |
| 16 | 1423-KOLNP-2013-FORM-18.pdf | 2014-05-06 |
| 17 | 1423-KOLNP-2013-(31-07-2014)-PA.pdf | 2014-07-31 |
| 18 | 1423-KOLNP-2013-(31-07-2014)-CORRESPONDENCE.pdf | 2014-07-31 |
| 19 | GPA.pdf | 2014-11-28 |
| 20 | Form 6.pdf | 2014-11-28 |
| 21 | 1423-KOLNP-2013-(22-12-2014)-PA.pdf | 2014-12-22 |
| 22 | 1423-KOLNP-2013-(22-12-2014)-CORRESPONDENCE.pdf | 2014-12-22 |
| 23 | 1423-KOLNP-2013-(22-12-2014)-ASSIGNMENT.pdf | 2014-12-22 |
| 24 | 1423-KOLNP-2013-FER.pdf | 2017-10-24 |
| 25 | 1423-KOLNP-2013-AbandonedLetter.pdf | 2018-05-18 |
| 1 | MotherClaimsinitial_24-10-2017.pdf |
| 2 | MotherClaimsamended1_24-10-2017.pdf |