التفاصيل البيبلوغرافية
| العنوان: |
AMINO-BENZAZOLES AS P2Y1 RECEPTOR INHIBITORS WITH PYRIDINE RING AND HETEROCYCLIC COMPONENTS |
| Document Number: |
20080275090 |
| تاريخ النشر: |
November 6, 2008 |
| Appl. No: |
12/104732 |
| Application Filed: |
April 17, 2008 |
| مستخلص: |
The present invention provides novel amino-benzazoles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity. |
| Inventors: |
Herpin, Timothy F. (Princeton, NJ, US); Morton, George C. (Collegeville, PA, US); Rehfuss, Robert P. (North Wales, PA, US); Lawrence, R. Michael (Yardley, PA, US); Poss, Michael A. (Lawrenceville, NJ, US); Roberge, Jacques Y. (Princeton, NJ, US); Gungor, Timur (Pennington, NJ, US) |
| Claim: |
1. A compound of Formula (I): [chemical expression included] or a stereoisomer or a pharmaceutically acceptable salt thereof wherein: ring A is [chemical expression included] X1 is NR11, O or S(O)p; X2 is CR11a or N; X3 is CR11a or N; X4 is CR11b or N; X5 is CR11b or N; ring E is selected from phenyl, pyridinyl, pyrimidyl, pyrazinyl, and pyridazinyl, and is substituted with 0-4 R1 as R1, R2, R3 and R4; ring B is pyridine substituted with 0-4 R7, or a 5- to 6-membered heteroaryl comprising: carbon atoms and 1-4 ring heteroatoms selected from O, N, NR6 and S(O)p, and said heteroaryl is substituted with 0-4 R7; R1 is, independently at each occurrence, F, Br, I, OCF3, CF3, —CF2CF3, —(CRfRf)t—ORc, CN, NO2, —(CRfRf)r—NR8R9, —(CRfRf)r—C(O)Rc—, —(CRfRf)r—C(O)ORc, —(CRfRf)r—C(O)NR8R9, —C(O)NR8(CRfRf)tNR8R9, —NR10(CRfRf)nC(O)Rd, —NR10CO(CRfRf)nORc, —S(O)pNR8R9, —NR10S(O)pRd, —S(O)Rd, —S(O)2Rd, —N(C1-4 alkyl)3+Cl−, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, —(CRfRf)r—C3-10 carbocycle substituted with 0-3 Rb, or —(CRfRf)r-5- to 12-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O, and S(O)p, and substituted with 0-3 Rb; alternatively, two nitrogen or oxygen containing R1s on two adjacent carbon atoms of ring E combined with the carbon atoms to which they are attached form a 5- or 6-membered carbocycle or heterocycle comprising: carbon atoms and 0-3 heteroatoms selected from N, NH, O and S(O)p, to form said carbocycle or heterocycle which is substituted with 0-2 Rb; Y is O or S(O)p; R5 is a C3-10 carbocycle phenyl substituted with 0-3 Rb, or a 5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb; R6 is H, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, (C1-6 alkyl)C(O)—, (C3-6 cycloalkyl)C1-3 alkyl-C(O)—, (C3-6 cycloalkyl)C(O)—, phenyl-C(O)—, benzyl-C(O)—, benzyl-S(O)2—, (C1-6 alkyl)NHC(O)—, (C1-6 alkyl)2NC(O)—, phenyl-NHC(O)—, benzyl-NHC(O)—, (phenyl)(C1-6 alkyl)NC(O)—, (benzyl)(C1-6 alkyl)NC(O)—, (C1-6 alkyl)-S(O)2—, phenyl-S(O)2—, —(CH2)r—C3-10 carbocycle substituted with 0-3 Rb or —(CH2)r-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb; R7 is H, F, Cl, Br, I, OCF3, CF3, ORc, SRc, CN, NO2, —NR8R9, —C(O)Rc, —C(O)ORc, —C(O)NR8R9, —NR10C(O)Rd, —S(O)pNR8R9, —S(O)Rd, —S(O)2Rd, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, —(CH2)r—C3-10 carbocycle substituted with 0-3 Rb, or —(CH2)r-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb; alternatively, two carbon, nitrogen or oxygen containing R7s on the two adjacent carbon atoms of ring B are combined to form a 5- to 7-membered carbocyclic or heterocyclic ring comprising: carbon atoms and 0-3 ring heteroatoms selected from O, N, NR6a and S(O)p, said carbocyclic or heterocyclic ring being substituted with 0-3 R7a; alternatively, R6 may combine with an R7 on an adjacent carbon atom to form a 5- to 7-membered carbocyclic or heterocyclic ring comprising: carbon atoms and 0-3 ring heteroatoms selected from O, N, NR6a and S(O)p, said carbocyclic or heterocyclic ring being substituted with 0-3 R7a; R6a is H, C1-4 alkyl, (C1-4 alkyl)C(O)—, phenyl-C(O)—, benzyl-C(O)—, benzyl-S(O)2—, (C1-4 alkyl)NHC(O)—, (C1-4 alkyl)2NC(O)—, phenyl-NHC(O)—, benzyl-NHC(O)—, (C1-4 alkyl)-S(O)2—, phenyl-S(O)2—, phenyl substituted with 0-3 Rb or benzyl substituted with 0-3 Rb; R7a is H, F, Cl, Br, I, OCF3, CF3, ORc, SRc, CN, NO2, —NR8R9, —C(O)Rc, —C(O)ORc, —C(O)NR8R9, —NR10(O)Rd, —S(O)pNR8R9, —S(O)Rd, —S(O)2Rd, C1-4 alkyl, phenyl substituted with 0-3 Rb or benzyl substituted with 0-3 Rb; R8 is independently at each occurrence, H, C1-6 alkyl substituted with 0-2 Rj, C(O)Rk, —C(O)ORk, —C(O)NRiRi, —C(O)O—(C1-4 alkyl)-C(O)ORk, —S(O)Rk), —(CRfRf)r—C3-10 carbocycle substituted with 0-3 Rj, or —(CRfRf)r-5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rj; R9 is, independently at each occurrence, H, C1-6 alkyl, or —(CH2)n—C3-10 carbocycle substituted with 0-2 Rj, or —(CH2)r-5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-2 Rj; alternatively, R8 and R9, when attached to the same nitrogen, combine to form a 5- to 10-membered heterocyclic ring comprising: carbon atoms and 0-2 additional heteroatoms selected from N, NRi, O and S(O)p; R10 is, independently at each occurrence, H, C1-6 alkyl substituted with 0-2 R10a, C2-6 alkenyl substituted with 0-2 R10a, C2-6 alkynyl substituted with 0-2 R10a, —(CH2)r—C3-10 carbocycle substituted with 0-3 Re, or —(CH2)r-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Re; R10a is, independently at each occurrence, H, C1-4 alkyl, ORc, Cl, F, Br, I, ═O, CF3, CN, NO2, —C(O)Rc, —C(O)ORc, —C(O)NR8R9 or —S(O)pRd; R11 is H, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, —C(O)Rc, —C(O)ORc, —C(O)NR8R9, —C(O)O—(C1-4 alkyl)-C(O)ORk, —S(O)2Rk, —S(O)2NR8R9, —(CH2)r—C3-10 carbocycle substituted with 0-3 Rb, or —(CH2)-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O, and S(O)p, and substituted with 0-3 Rb; R11a is H, F, Cl, Br, I, OCF3, CF3, ORc, SRc, CN, NO2, —NR8R9, —C(O)Rc, —C(O)ORc, —C(O)NR8R9, —NR10C(O)Rd, —S(O)pNR8R9, —S(O)Rd, —S(O)2Rd, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, —(CH2)r—C3-10 carbocycle substituted with 0-3 Rb, or —(CH2)r-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb; R11b is H, F, Cl, Br, I, OCF3, CF3, —CF2CF3, —(CRfRf)r—ORc, SRc, CN, NO2, —(CRfRf)r—NR8R9, —(CRfRf)r—C(O)Rc, —(CRfRf)r—C(O)ORc, —(CRfRf)r—C(O)NR8R9, —C(O)NR8(CRfRf)tNR8R9, —NR10(CRfRf)nC(O)Rd, —NR10CO(CRfRf)nORc, —S(O)pNR8R9, —NR10S(O)pRd, —S(O)Rd, —S(O)2Rd, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, —(CH2)r—C3-10 carbocycle substituted with 0-3 Rb, or —(CH2)r-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb; R13 is H, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, —C(O)Rc, —C(O)ORc, —C(O)NR8R9, —S(O)2Rk, —S(O)2NR8R9, —(CH2)r—C3-10 carbocycle substituted with 0-3 Rb, or —(CH2)r-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb; Ra is, independently at each occurrence, H, F, OCF3, CF3, ORc, SRc, CN, —NR8R9, —C(O)Rc, —C(O)ORc, —C(O)NR8R9, —NR10C(O)Rb, —S(O)pNR8R9, —S(O)Rd or —S(O)2Rd; Rb is, independently at each occurrence, H, F, Cl, Br, I, ORc, SRc, CN, NO2, CF3, OCF3, —C(O)Rc—C(O)ORc, —C(O)NR8R9, —NR10C(O)Rd, —S(O)pNR8R9, —S(O)pRd, —NR8R9, —Si(Me)3, C1-C4 haloalkyl, C1-C4 haloalkyloxy-, C1-C4 alkyloxy-, C1-C4 alkylthio-, C1-C4 alkyl-C(O)—, C1-C4 alkyl-O—C(O)—, C1-C4 alkyl-C(O)NH—, C1-6 alkyl substituted with 0-2 Rj, C2-6 alkenyl substituted with 0-2 Rj, C2-6 alkynyl substituted with 0-2 Rj, —(CH2)r—C3-10 carbocycle substituted with 0-3 Rj or —(CH2)r-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, wherein said heterocycle is substituted with 0-3 Rj; alternatively, two Rb groups attached to adjacent atoms, together with the atoms to which they are attached, form a 5- to 7-membered carbocyclic or heterocyclic ring comprising: carbon atoms and 0-2 heteroatoms selected from N, O and S(O)p, 0-1 carbonyl and 0-3 double bonds; Rc is, independently at each occurrence, H, C1-6 alkyl substituted with 0-2 Rj, C2-6 alkenyl substituted with 0-2 Rj, C2-6 alkynyl substituted with 0-2 Rj, —(CH2)r—C6-10 aryl substituted with 0-2 Re, or —(CH2)r-5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-2 Re; Rd is, independently at each occurrence, CF3, OH, C1-4 alkoxy, C1-6 alkyl substituted with 0-2 Rj, —(CH2)r—C3-10 carbocycle substituted with 0-2 Re, or —(CH2)r-5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-2 Re; Re is, independently at each occurrence, H, ═O, ORg, F, Cl, Br, I, CN, NO2, —NR8R9, —C(O)Rf, —C(O)ORf, —NR8C(O)Rf, —C(O)NR8R9, —SO2NR8R9, —NR8SO2NR8R9, —NR8SO2—C1-4 alkyl, —NR8SO2CF3, —NR8SO2-phenyl, —S(O)2CF3, —S(O)p—C1-4 alkyl, —S(O)p-phenyl, —(CF2)rCF3, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or —(CH2)n-phenyl; Rf is, independently at each occurrence, H, C1-6 alkyl or —(CH2)n-phenyl; Rg is, independently at each occurrence, H, ═O, ORf, F, Cl, Br, I, CN, NO2, —NR9R9, —C(O)Rh, —C(O)ORh, —NR9C(O)Rh, —C(O)NR9R9, —SO2NR9R9, —NR9SO2NR9R9, —NR9SO2—C1-4 alkyl, —NR9SO2CF3, —NR9SO2-phenyl, —S(O)2CF3, —S(O)p—C1-4 alkyl, —S(O)p-phenyl, —(CF2)rCF3, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or —(CH2)n-phenyl; Rh is, independently at each occurrence, H, C1-6 alkyl or —(CH2)n-phenyl; Ri is, independently at each occurrence, H, C1-6 alkyl, or —(CH2)r—C6-10 aryl substituted with 0-2 Rj or —(CH2)r-5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-2 Rj; Rj is, independently at each occurrence, H, ═O, ORf, F, Cl, Br, I, CN, NO2, —NRfRh, —C(O)Rh, —C(O)ORh, —NRfC(O)Rh, —C(O)NRfRh, —SO2NRfRh, —NRfSO2—C1-4 alkyl, —NRfSO2CF3, —NRfSO2-phenyl, —S(O)2CF3, —S(O)p—C1-4 alkyl, —S(O)p-phenyl, —(CF2)rCF3, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or —(CH2)n-phenyl; Rk is, independently at each occurrence, C1-6 alkyl, —(CH2)r—C6-10 aryl substituted with 0-2 Rj or —(CH2)r-5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-2 Rj; n, at each occurrence, is selected from 0, 1, 2, 3 and 4; p, at each occurrence, is selected from 0, 1 and 2; r, at each occurrence, is selected from 0, 1, 2, 3 and 4; and t, at each occurrence, is selected from 1, 2, 3 and 4; provided that: when ring B is [chemical expression included] and ring A is [chemical expression included] ring E is phenyl substituted with ORc or SRc, then Rc is other than aryl or heteroaryl. |
| Claim: |
2. A compound of Formula (Ia): [chemical expression included] or a stereoisomer or a pharmaceutically acceptable salt thereof, wherein: ring B is pyridine substituted with 0-4 R7, or a 5- to 6-membered heteroaryl comprising: carbon atoms and 1-3 ring heteroatoms selected from O, N, NR6 and S(O)p, and said heteroaryl is substituted with 0-3 R7; X is NR11, O or S; R1, R2, R3 and R4 are, independently at each occurrence, H, F, Br, I, OCF3, CF3, CN, NO2, —NR8R9, —C(O)Rc, —C(O)ORc, —C(O)NR8R9, —NR10C(O)Rd, —S(O)pNR8R9, —S(O)Rd, —S(O)2Rd, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, —(CH2)r—C3-10 carbocycle substituted with 0-3 Rb or —(CH2)r-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb; alternatively, each of R1, R2, R3 and R4 are selected to contain carbon, nitrogen or oxygen and R1+R2, R2+R3, or R3+R4, are combined with the carbon atoms to which they are attached to form a 5- or 6-membered carbocycle or heterocycle comprising: carbon atoms and 0-3 additional heteroatoms selected from N, NH, O and S(O)p, and substituted with 0-2 Rb; Y is NR12, O or S; R5 is a C3-10 carbocycle substituted with 0-3 Rb, or a 5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb; R6 is H, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, (C1-6 alkyl)C(O)—, (C3-6 cycloalkyl)C1-3 alkyl-C(O)—, (C3-6 cycloalkyl)C(O)—, phenyl-C(O)—, benzyl-C(O)—, benzyl-S(O)2—, (C1-6 alkyl)NHC(O)—, (C1-6 alkyl)2NC(O)—, phenyl-NHC(O)—, benzyl-NHC(O)—, (phenyl)(C1-6 alkyl)NC(O)—, (benzyl)(C1-6 alkyl)NC(O)—, (C1-6 alkyl)-S(O)2—, phenyl-S(O)2—, —(CH2)r—C3-10 carbocycle substituted with 0-3 Rb or —(CH2)r-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb; R7 is H, F, Cl, Br, I, OCF3, CF3, ORc, SRc, CN, NO2, —NR8R9, —C(O)Rc, —C(O)ORc—, —C(O)NR8R9, —NR10C(O)Rd, —S(O)pNR8R9, —S(O)Rd, —S(O)2Rd, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, —(CH2)r—C3-10 carbocycle substituted with 0-3 Rb or —(CH2)r-5 to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb; alternatively, two carbon, nitrogen or oxygen containing R7s on two adjacent carbon atoms of ring B are combined to form a 5- to 7-membered carbocyclic or heterocyclic ring comprising: carbon atoms and 0-3 ring heteroatoms selected from O, N, NR6a and S(O)p, said carbocyclic or heterocyclic ring being substituted with 0-3 R7a; alternatively, R6 may combine with an R7 on an adjacent carbon atom to form a 5- to 7-membered carbocyclic or heterocyclic ring comprising: carbon atoms and 0-3 ring heteroatoms selected from O, N, NR6a and S(O)p, said carbocyclic or heterocyclic ring being substituted with 0-3 R7a; R6a is H, C1-4 alkyl, (C1-4 alkyl)C(O)—, phenyl-C(O)—, benzyl-C(O)—, benzyl-S(O)2—, (C1-4 alkyl)NHC(O)—, (C1-4 alkyl)2NC(O)—, phenyl-NHC(O)—, benzyl-NHC(O)—, (C1-4 alkyl)-S(O)2—, phenyl-S(O)2—, phenyl substituted with 0-3 Rb or benzyl substituted with 0-3 Rb; R7a is H, F, Cl, Br, I, OCF3, CF3, ORc, SRc, CN, NO2, —NR8R9, —C(O)Rc, —C(O)ORc, —C(O)NR8R9, —NR10C(O)Rd, —S(O)pNR8R9, —S(O)Rd, —S(O)2Rd, C1-4 alkyl, phenyl substituted with 0-3 Rb or benzyl substituted with 0-3 Rb; R8 is, independently at each occurrence, H, C1-6 alkyl, C1-6 alkyl)C(O)—, —(CH2)n-phenyl, (C1-4 alkyl)OC(O)—, (C6-10 aryl)-CH2—OC(O)—, (C6-10 aryl)-CH2—C(O), (C1-4 alkyl)-C(O)O—(C1-4 alkyl)-OC(O)—, (C6-10 aryl)-C(O)O—(C1-4 alkyl)-OC(O)—, (C1-6 alkyl)-NHC(O)—, (C6-10aryl)-NHC(O)—, (5- to 10-membered heteroaryl)-NHC(O)—, (5- to 10-membered heteroaryl)-CH2—OC(O)—, (5- to 10-membered heteroaryl)-C(O)—, (C6-10 aryl)-(C1-4 alkyl)-C(O)—, (C1-6 alkyl)-S(O)2—, (C6-10 aryl)-S(O)2—, (5- to 10-membered heteroaryl)-S(O)2— or (C6-10 aryl)-(C1-4 alkyl)-S(O)2—, wherein each of said phenyl, aryl and heteroaryl may be substituted with 0-2 Rg; R9 is, independently at each occurrence, H, C1-6 alkyl or —(CH2)n-phenyl; alternatively, R8 and R9, when attached to the same nitrogen combine to form a 5- to 10-membered heterocyclic ring comprising: carbon atoms and 0-2 additional heteroatoms selected from N O and S(O)p; R10 is, independently at each occurrence, H, C1-6 alkyl substituted with 0-2 R10a, C2-6 alkenyl substituted with 0-2 R10a, C2-6 alkynyl substituted with 0-2 R10a, —(CH2)r—C3-10 carbocycle substituted with 0-3 Re, or —(CH2)r-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Re; R10a is, independently at each occurrence, H, C1-4 alkyl, ORc, Cl, F, Br, I, ═O, CF3, CN, NO2, —C(O)Rc, —C(O)ORc, —C(O)NR8R9 or —S(O)pRd; R11 is H, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, (C1-6 alkyl)C(O)—, (C3-6 cycloalkyl)C1-3 alkyl-C(O)—, (C3-6 cycloalkyl)C(O)—, phenyl-C(O)—, benzyl-C(O)—, benzyl-S(O)2—, (C1-6 alkyl)NHC(O)—, (C1-6 alkyl)2NC(O)—, phenyl-NHC(O)—, benzyl-NHC(O)—, (phenyl)(C1-6 alkyl)NC(O)—, (benzyl)(C1-6 alkyl)NC(O)—, (C1-6 alkyl)-S(O)2—, phenyl-S(O)2—, —(CH2)r—C3-10 carbocycle substituted with 0-3 Rb or —(CH2)-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O, and S(O)p, and substituted with 0-3 Rb; R12 is H, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, (C1-6 alkyl)C(O)—, (C3-6 cycloalkyl)C1-3 alkyl-C(O)—, (C3-6 cycloalkyl)C(O)—, phenyl-C(O)—, benzyl-C(O)—, benzyl-S(O)2—, (C1-6 alkyl)NHC(O)—, (C1-6 alkyl)2NC(O)—, phenyl-NHC(O)—, benzyl-NHC(O)—, (phenyl)(C1-6 alkyl)NC(O)—, (benzyl)(C1-6 alkyl)NC(O)—, (C1-6 alkyl)-S(O)2—, phenyl-S(O)2—, —(CH2)r—C3-10 carbocycle substituted with 0-3 Rb or —(CH2)r-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb; Ra is, independently at each occurrence, H, F, OCF3, CF3, ORc, SRc, CN, —NR8R9, —C(O)NR8R9, —NR10C(O)Rb, —S(O)pNR8R9, —S(O)Rd or —S(O)2Rd; Rb is, independently at each occurrence, H, F, Cl, Br, I, ORc, SRc, CN, NO2, CF3, —SO2Rd, —NR8R9, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C1-C4 haloalkyl, C1-C4 haloalkyloxy-, C1-C4 alkyloxy-, C1-C4 alkylthio-, C1-C4 alkyl-C(O)—, C1-C4 alkyl-O—C(O)— or C1-C4 alkyl-C(O)NH—; Rc is, independently at each occurrence, H, C1-4 alkyl, —(CH2)r—C6-10 aryl substituted with 0-2 Re, or —(CH2)r-5- to 10-membered heterocycle containing from 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-2 Re; Rd is, independently at each occurrence, CF3, OH, C1-4 alkoxy, C1-6 alkyl, —(CH2)r—C3-10 carbocycle substituted with 0-2 Re, or —(CH2)r-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-2 Re; Re is, independently at each occurrence, H, ═O, ORg, F, Cl, Br, I, CN, NO2, —NR8R9, —C(O)Rf, —C(O)ORf, —NR8C(O)Rf, —C(O)NR8R9, —SO2NR8R9, —NR8SO2NR8R9, —NR8SO2—C1-4 alkyl, —NR8SO2CF3, —NR8SO2-phenyl, —S(O)2CF3, —S(O)p—C1-4 alkyl, —S(O)p-phenyl, —(CF2)rCF3, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl; Rf is, independently at each occurrence, H, C1-6 alkyl or —(CH2)n-phenyl; Rg is, independently at each occurrence, H, ═O, ORf, F, Cl, Br, I, CN, NO2, —NR9R9, —C(O)Rh, —C(O)ORh, —NR9C(O)Rh, —C(O)NR9R9, —SO2NR9R9, —NR9SO2NR9R9, —NR9SO2—C1-4 alkyl, —NR9SO2CF3, —NR9SO2-phenyl, —S(O)2CF3, —S(O)p—C1-4 alkyl, —S(O)p-phenyl, (CF2)rCF3, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl; Rh is, independently at each occurrence, H, C1-6 alkyl or —(CH2)n-phenyl; n, at each occurrence, is selected from 0, 1, 2, 3 and 4; p, at each occurrence, is selected from 0, 1 and 2; and r, at each occurrence, is selected from 0, 1, 2, 3 and 4; provided that: when ring B is [chemical expression included] and ring A is [chemical expression included] ring E is phenyl substituted with ORc or SRc and Rc is other than aryl or heteroaryl. |
| Claim: |
3. A compound according to claim 2 wherein: ring B is pyridine substituted with 0-3 R7 or R7 is a 5- to 6-membered heteroaryl comprising: carbon atoms and 1-3 ring heteroatoms selected from O, N, NR6 and S(O)p, and said heteroaryl is substituted with 0-2 R7; R1, R2, R3, and R4 are, independently at each occurrence, H, F, Br, I, OCF3, CF3, —CF2CF3, —(CRfRf)t—ORc, CN, NO2, —(CRfRf)r—NR8R9, —(CRfRf)r—C(O)Rc, —(CRfRf)r—C(O)ORc, —(CRfRf)r—C(O)NR8R9, —C(O)NR8(CRfRf)tNR8R9, —NR10(CRfRf)nC(O)Rd, —NR10CO(CRfRf)nORc, —S(O)pNR8R9, —NR10S(O)pRd, —S(O)Rd, —S(O)2Rd, —N(C1-4 alkyl)3+Cl−, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, —(CRfRf)r—C3-10 carbocycle substituted with 0-3 Rb or —(CRfRf)r-5- to 12-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb; and alternatively, R1+R2, R2+R3, or R3+R4, combined with the carbon atoms to which they are attached, form a 5- or 6-membered carbocycle or heterocycle comprising: carbon atoms and 0-3 additional heteroatoms selected from N, NH, O and S(O)p, and substituted with 0-2 Rb. |
| Claim: |
4. A compound according to claim 3, wherein: one of the R1, R2, R3 and R4 groups is —(CRfRf)t—ORc, —(CRfRf)r—ORc, —(CRfRf)r, —NR8R9, —(CRfRf)r—C(O)ORc, —(CRfRf)r—C(O)NR8R9, —C(O)NR8(CRfRf)tNR8R9, —NR10(CRfRf)nC(O)Rd or —NR10CO(CRfRf)nORc; remaining of the R1, R2, R3 and R4 groups are, independently at each occurrence, H, F, Br, I, OCF3, CF3, —CF2CF3, —(CRfRf)t—ORc, CN, NO2, —(CRfRf)r—NR8R9, —(CRfRf)r—C(O)Rc, —(CRfRf)r—C(O)ORc, —S(O)pNR8R9, —R10S(O)pRd, —S(O)Rd, —S(O)2Rd, —N(C1-4 alkyl)3+Cl−, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, —(CRfRf)r—C3-10 carbocycle substituted with 0-3 Rb, or —(CRfRf)r-5- to 12-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb; and alternatively, each of R1, R2, R3 and R4 are selected to contain carbon, nitrogen or oxygen and R1+R2, R2+R3, or R3+R4, together with the carbon atoms to which they are attached, form a 5- or 6-membered carbocycle or heterocycle comprising: carbon atoms and 0-3 additional heteroatoms selected from N, NH, O and S(O)p, and substituted with 0-2 Rb. |
| Claim: |
5. A compound according to claim 4, wherein: one of the R1, R2, R3 and R4 groups is NHBn, —NH(4-OMe-Bn), —NH(4-CF3-Bn), —NH(4-OCF3-Bn), CO2Et, —CO2-neopentyl, —CO2CH2CH═CH2, —CH(Me)OCH2C(Me)2CH2NMe2, —CH(Me)OBn, —CH(Me)O(4-i-Pr-Bn), —CH(Me)O(3-CF3-Bn), —CH(Me)O(4-CF3-Bn), —CH(Me)O(4-OPh-Bn), —CH(Me)O(3,5-diCl-Bn), —CH(Me)OCH2(1-Bn-piperidin-4-yl), —CH2NHBn, —CH2NH(4-CF3-Bn), —CH2N(Me)Bn, —CH(Me)NHCH2-pyridin-2-yl, —CH(Me)NHCH2-pyridin-4-yl, —CH(Me)NHCH2(6-Cl-pyridin-3-yl), —CH(Me)N(Me)(i-Bu), —CH(Me)N(Me)Bn, —CH(Me)N(Me)(4-OMe-Bn), —CH(Me)N(Me)(4-F-Bn), —CH(Me)N(Me)(3-Cl-Bn), —CH(Me)N(Me)(4-Cl-Bn), —CH(Me)N(Me)(3-CF3-Bn), —CH(Me)N(Me)(4-CF3-Bn), —CH(Me)N(Me)(3,4-diCl-Bn), —CH(Me)N(Me)CH2CH2Ph, —CH(Me)N(Me)CH2-pyridin-2-yl, —CH(Me)N(Me)CH2-pyridin-3-yl, —CH(Me)N(Me)CH2-pyridin-4-yl, —CH(Me)N(Me)CH2-furan-2-yl, —CH(Me)N(Me)CH2-thien-2-yl, —CH(Me)N(Me)CH2-(5-Me-thien-2-yl), —CH(Me)N(Me)CH2-(5-Cl-thien-2-yl), —CH(Me)N(Et)Bn, —CH(Me)N(Et)(4-Me-Bn), —CH(Me)N(Et)(2-Cl-Bn), —CH(Me)N(Bn)CH2CN, —CH(Me)N(Bn)CH2CH2OH, —CH(Me)N(Bn)CH2CO2Me, —CH(Me)N(Bn)CH2CONMe2, —CH(Me)N(Bn)CH2CON(Me)(Bn), —CH(Me)-isoindolin-2-yl, —CH(Me)-(1,2,3,4-tetrahydroisoquinolin-2-yl), —CH(Me)(4-Bn-piperazin-1-yl), —CONH-neopentyl, —CONHBn, —CONH(4-CF3-Bn), —CONH(4-NO2-phenethyl), —CONHCH2CH2NHPh, —NHCOCH2OBn, —NHCOCH2O-(4-t-Bu-Ph), —NHCO(4-Ph-Ph), —NHCO(5-(3,5-diCl-OPh)-2-furanyl) or —NHCOC(Me)2O(-4-Cl-Ph). |
| Claim: |
6. A compound according to claim 3, wherein: ring B is pyridine substituted with 0-2 R7; R8 is, independently at each occurrence, H, C1-6 alkyl substituted with 0-2 Rj, —C(O)Rk, —C(O)ORk, —C(O)NRiRi, —S(O)Rk, —(CRfRf)r—C3-10 carbocycle substituted with 0-2 Rj, or —(CRfRf)r-5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-2 Rj; R9 is, independently at each occurrence, H, C1-4 alkyl or —(CH2)n-phenyl; alternatively, R8 and R9, when attached to the same nitrogen, combine to form a 5- to 10-membered heterocyclic ring comprising: carbon atoms and 0-2 additional heteroatoms selected from N, NRi, O and S(O)p; R10 is, independently at each occurrence, H, C1-6 alkyl substituted with 0-2 R10a, C2-6 alkenyl substituted with 0-2 R10a, C2-6 alkynyl substituted with 0-2 R10a, —(CH2)r-phenyl substituted with 0-3 Re or —(CH2)r-5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Re; R11 is H, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, —C(O)Rc, —C(O)NR8R9, S(O)2Rk, —(CH2)r-phenyl substituted with 0-3 Rb, or —(CH2)r-5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb; and R13 is H, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, —C(O)Rc, —C(O)NR8R9, —S(O)2Rk, —(CH2)r-phenyl substituted with 0-3 Rb or —(CH2)r-5 to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb. |
| Claim: |
7. A compound according to claim 4, wherein ring B is pyridine substituted with 0-2 R7. |
| Claim: |
8. A compound according to claim 5, wherein: Y is O or S; R5 is phenyl with 0-3 Rb or a 5-6 membered heterocycle substituted with 0-3 Rb and selected from pyridinyl, furanyl, thienyl, pyrrolyl, pyrazolyl, pyrazinyl, imidazolyl, isoxazolyl, oxazolyl, thiazolyl and triazinyl; alternatively, R5 is [chemical expression included] R10 is, independently at each occurrence, H, C1-4 alkyl, phenyl or benzyl; and R11 is H, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, (C1-4 alkyl)C(O)—, benzyl-C(O)—, benzyl-S(O)2—, (C1-4 alkyl)-S(O)2— or benzyl. |
| Claim: |
9. A compound of Formula (Ib) or (Ib′): [chemical expression included] or a stereoisomer or a pharmaceutically acceptable salt thereof, wherein: X is NR11; R1, R2, R3, and R4 are, independently at each occurrence, H, F, Br, I, CF3, OCF3, —CH2ORc, —CH2CH2ORc, —CH(C1-4 alkyl)ORc, CN, NO2, —NR8R9, —CH2NR8R9, —CH2CH2NR8R9, —CH(C1-4 alkyl)NR8R9, —C(O)Rc, —C(O)ORc, —C(O)NR8R9, —C(O)NR8(CRfRf)tNR8R9, —NR10(CRfRf)C(O)Rd, —NR10CO(CRfRf)nORc, —S(O)pNR8R9, —NR10S(O)pRd, —S(O)Rd, —S(O)2Rd, —N(C1-4 alkyl)3+Cl−, C1-6 alkyl substituted with 0-2 Ra, C2-6 alkenyl substituted with 0-2 Ra, C2-6 alkynyl substituted with 0-2 Ra, —(CRfRf)r—C3-7 cycloalkyl substituted with 0-3 Rb, —(CRfRf)r-phenyl substituted with 0-3 Rb or —(CRfRf)r-5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb; alternatively, each of R1, R2, R3 and R4 are selected to contain carbon, nitrogen or oxygen and R1+R2, R2+R3, or R3+R4, and combined with the carbon atoms to which they are attached, form a 5- or 6-membered carbocycle or heterocycle comprising: carbon atoms and 0-3 additional heteroatoms selected from N, NH, O and S(O)p, and substituted with 0-2 Rb; Y is NR12, O or S; R5 is phenyl substituted with 0-3 Rb or a 5-6 membered heterocycle substituted with 0-3 Rb and selected from pyridinyl, furanyl, thienyl, pyrrolyl, pyrazolyl, pyrazinyl, imidazolyl, isoxazolyl, oxazolyl, thiazolyl and triazinyl; alternatively, R5 is [chemical expression included] R7 is H, F, Cl, Br, OCF3, CF3, ORc, SRc, CN, NO2, —NR8R9, —C(O)Rc, —C(O)ORc, —C(O)NR8R9, —NR10C(O)Rd, —S(O)pNR8R9, —S(O)Rd, —S(O)2Rd, C1-4 alkyl substituted with 0-1 Ra, C2-4 alkenyl substituted with 0-1 Ra, C2-4 alkynyl substituted with 0-1 Ra, —(CH2)r—C3-7 cycloalkyl substituted with 0-3 Rb —(CH2)r-phenyl substituted with 0-3 Rb, or —(CH2)r-5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rb; R8 is, independently at each occurrence, H, C1-6 alkyl substituted with 0-2 Rj, —C(O)Rk, —C(O)ORk, —C(O)NRiRi, —S(O)2Rk—(CRfRf)r-phenyl substituted with 0-3 Rj or —(CRfRf)r-5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rj; R9 is, independently at each occurrence, H, C1-6 alkyl —(CRfRf)r-phenyl substituted with 0-3 Rj, or —(CRfRf)r-5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-3 Rj; alternatively, R8 and R9, when attached to the same nitrogen, combine to form a 5- to 10-membered heterocyclic ring comprising: carbon atoms and 0-2 additional heteroatoms selected from N, NRi, O and S(O)p; R10 is, independently at each occurrence, H, C1-4 alkyl, phenyl or benzyl; R11 is H, C1-4 alkyl substituted with 0-1 Ra, C2-4 alkenyl substituted with 0-1 Ra, C2-4 alkynyl substituted with 0-1 Ra, (C1-4 alkyl)C(O)—, phenyl-C(O)—, benzyl-C(O)—, benzyl-S(O)2—, (C1-4 alkyl)-S(O)2—, phenyl-S(O)2—, phenyl or benzyl; R12 is H, C1-4 alkyl substituted with 0-1 Ra, C2-4 alkenyl substituted with 0-1 Ra, C2-4 alkynyl substituted with 0-1 Ra, (C1-4 alkyl)C(O)—, phenyl-C(O)—, benzyl-C(O)—, benzyl-S(O)2—, (C1-4 alkyl)-S(O)2—, phenyl-S(O)2—, phenyl or benzyl; Ra is, independently at each occurrence, H, F, OCF3, CF3, ORc, SRc, CN, —NR8R9, —C(O)Rc, —C(O)ORc, —C(O)NR8R9, —NR10C(O)Rb, —S(O)pNR8R9, —S(O)Rd or —S(O)2Rd; Rb is, independently at each occurrence, H, F, Cl, Br, I, ORc, SRc, CN, NO2, CF3, —C(O)ORc, —SO2Rd, —NR8R9, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C1-C4 haloalkyl, C1-C4 haloalkyloxy-, C1-C4 alkyloxy-, C1-C4 alkylthio-, C1-C4 alkyl-C(O)—, C1-C4 alkyl-O—C(O)—, C1-C4 alkyl-C(O)NH— or —(CH2)n-phenyl substituted with Rj; Rc is, independently at each occurrence, H, C1-6 alkyl substituted with 0-2 Rj, C2-6 alkenyl substituted with 0-2 Rj, C2-6 alkynyl substituted with 0-2 Rj—(CH2)r—C6-10 aryl substituted with 0-2 Re, or (CH2)r-5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-2 Re; Rd is, independently at each occurrence, CF3, OH, C1-4 alkoxy, C1-6 alkyl substituted with 0-2 Rj—(CH2)r—C3-10 carbocycle substituted with 0-2 Re or —(CH2)r-5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-2 Re; Re is, independently at each occurrence, H, ═O, ORg, F, Cl, Br, I, CN, NO2, —NR8R9, —C(O)Rf, —C(O)ORf, —NR8C(O)Rf, —C(O)NR8R9, —SO2NR8R9, —NR8SO2NR8R9, —NR8SO2—C1-4 alkyl, —NR8SO2CF3, —NR8SO2-phenyl, —S(O)2CF3, —S(O)p—C1-4 alkyl, —S(O)p-phenyl, —(CF2)rCF3, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or —(CH2)n-phenyl; Rf is, independently at each occurrence, H, C1-6 alkyl or —(CH2)n-phenyl; Rg is, independently at each occurrence, H, ═O, ORf, F, Cl, Br, I, CN, NO2, —NR9R9, —C(O)Rh, —C(O)ORh, —NR9C(O)Rh, —C(O)NR9R9, —SO2NR9R9, —NR9SO2NR9R9, —NR9SO2—C1-4 alkyl, —NR9SO2CF3, —NR9SO2-phenyl, —S(O)2CF3, —S(O), —C1-4 alkyl, —S(O)p-phenyl, (CF2)rCF3, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or —(CH2)n-phenyl; Rh is, independently at each occurrence, H, C1-6 alkyl or —(CH2)n-phenyl; Ri is, independently at each occurrence, H, C1-6 alkyl or —(CH2)n-phenyl substituted with 0-2 Rj; Rj is, independently at each occurrence, H, ═O, ORf, F, Cl, Br, X, CN, NO2, —NRfRh, —C(O)Rh, —C(O)ORh, —NRfC(O)Rh, C(O)NRfRh, —SO2NRfRh, —NRfSO2—C1-4 alkyl, —NRfSO2CF3, —NRfSO2-phenyl, —S(O)2CF3, —S(O), —C1-4 alkyl, —S(O)p-phenyl, —(CF2)rCF3, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or —(CH2)n-phenyl; Rk is, independently at each occurrence, C1-6 alkyl —(CH2)r-phenyl substituted with 0-2 Rj, or —(CH2)r-5-10 membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, O and S(O)p, and substituted with 0-2 Rj; n, at each occurrence, is selected from 0, 1, 2, 3 and 4; p, at each occurrence, is selected from 0, 1 and 2; r, at each occurrence, is selected from 0, 1, 2, 3 and 4; and t, at each occurrence, is selected from 1, 2, 3 and 4. |
| Claim: |
10. A compound according to claim 9, wherein the compound is of Formula (Ib): [chemical expression included] or a stereoisomer or a pharmaceutically acceptable salt thereof. |
| Claim: |
11. A compound according to claim 9, wherein the compound is of Formula (Ic): [chemical expression included] or a stereoisomer or a pharmaceutically acceptable salt thereof, wherein: X is NH or NC1-4 alkyl; R1, R2, R3, and R4 are, independently at each occurrence, H, F, Br, CF3, CN, OCF3, NH2, NHC1-4 alkyl, N(C1-4 alkyl)2, NO2, NHBn, —CH2OC1-4 alkyl, —CH(C1-4 alkyl)OC1-4 alkyl, —CH(C1-4 alkyl)OCH2C(Me)2CH2N(C1-4 alkyl)2, —CH(C1-4 alkyl)O-benzyl, —CH(C1-4 alkyl)OCH2(1-Bn-piperidin-4-yl), —CH2NH-benzyl, —CH2N(C1-4 alkyl)2, —CH2N(C1-4 alkyl)-benzyl, —CH(C1-4 alkyl)NH-benzyl, —CH2(4-Bn-piperazin-1-yl), —CH(C1-4 alkyl)NH(CH2)n-(5- to 6-membered heteroaryl), —CH(C1-4 alkyl)N(C1-4 alkyl)2, —CH(C1-4 alkyl)N(C1-4 alkyl)(CH2)n-phenyl, —CH(C1-4 alkyl)N(C1-4 alkyl)(CH2)n-(5- to 6-membered heteroaryl), —CH(C1-4 alkyl)N(benzyl)(CH2)tCN, —CH(C1-4 alkyl)N(benzyl)(CH2)tOH, —CH(C1-4 alkyl)N(benzyl)(CH2)tOC1-4 alkyl, —CH(C1-4 alkyl)N(benzyl)(CH2)tCO2C1-4 alkyl, —CH(C1-4 alkyl)N(benzyl)(CH2)tCONH2—CH(C1-4 alkyl)N(benzyl)(CH2)tCONHC1-4 alkyl, —CH(C1-4 alkyl)N(benzyl)(CH2)tCON(C1-4 alkyl)2, —CH(C1-4 alkyl)N(benzyl))(CH2)tCON(C1-4 alkyl)(benzyl)-CH(C1-4 alkyl)-isoindolin-2-yl, —CH(C1-4 alkyl)-(1,2,3,4-tetrahydroisoquinolin-2-yl), —CH(C1-4 alkyl)(4-Bn-piperazin-1-yl), —COC1-4 alkyl, —CO-phenyl, —CO-(5- to 6-membered heteroaryl), —CO(4-Bn-piperazin-1-yl), —CO2H, —CO2C1-6 alkyl, —CO2C2-6 alkenyl, —CONH2, —CONHC1-6 alkyl, —CON(C1-4 alkyl)2, —CONH-benzyl, —CON(C1-4 alkyl)-benzyl, —CONH-phenethyl, —CONHCH2CH2NH-phenyl, —NHCOC1-4 alkyl, —NHCO—C3-6 cylcoalkyl, —NHCO-phenyl, —NHCO-benzyl, —NHCO-phenethyl, —NHCOCH2OC1-4-alkyl, —NHCOCH2O-phenyl, —NHCOCH2O-benzyl, —NHCO(5-phenoxy-furan-2-yl), —NHCOC(Me)2O-phenyl, —NHCO2C1-4 alkyl, —NHCO2-phenyl, —NHCO2-benzyl, —NHSO2(C1-4 alkyl), C1-6 alkyl substituted with 0-1 Ra, C2-6 alkenyl substituted with 0-1 Ra, phenyl, benzyl, 4-morpholinyl 1-pyrazolyl, 1-imidazolyl or —NEt3+Cl−; wherein phenyl, benzyl, phenethyl, phenoxy and benzoxy are substituted with 0-3 Re; wherein the 5- to 6-membered heteroaryl is selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, triazolyl, tetrazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl and triazinyl, and substituted with 0-3 Re; alternatively, each of R1, R2, R3 and R4 are selected to contain carbon, nitrogen or oxygen and R1+R2, R2+R3, or R3+R4, combined with the carbon atoms to which they are attached, form a 5- or 6-membered carbocycle or heterocycle comprising: carbon atoms and 0-3 additional heteroatoms selected from N, NH, O and S(O)p, and substituted with 0-2 Rb; R5 is phenyl substituted with 0-2 Rb; alternatively, R5 is [chemical expression included] R7 is H, F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, CF3, OCF3, NH2, NHC1-4 alkyl, N(C1-4 alkyl)2, CO2H, —CO2C1-4 alkyl, —CONH2, —CONHC1-4 alkyl or —CON(C1-4 alkyl)2; Ra is, independently at each occurrence, H, F, OCF3, CF3, OH, OC1-4 alkyl, CN, NH2, NHC1-4 alkyl, N(C1-4 alkyl)2, —CONH2, —CONHC1-4 alkyl or —CON(C1-4 alkyl)2; Rb is, independently at each occurrence, F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, CF3, OCF3, NH2, NHC1-4 alkyl, N(C1-4 alkyl)2, CO2H, —CO2C1-4 alkyl, —CONH2, —CONHC1-4 alkyl or —CON(C1-4 alkyl)2; Re is, independently at each occurrence, F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, CF3, OCF3, NH2, NHC1-4 alkyl, N(C1-4 alkyl)2, NO2, CO2H, —CO2C1-4 alkyl, —CONH2, —CONHC1-4 alkyl, —CON(C3-4 alkyl)2, Ph, Bn or OPh; n, at each occurrence, is selected from 0, 1, 2 and 3; and t, at each occurrence, is selected from 1, 2 and 3. |
| Claim: |
12. A compound according to claim 9, wherein: R1 is H, Me, t-Bu, F, Br, CN, NH2, NO2, —CH2OH, —CH(Me)OH, —CO2Me, —CH2NH(4-CF3-Bn), —CH2N(Me)Et, —CH2N(Me)Bn, —CH2N(Me)(4-CF3-Bn), —CH2(4-Bn-piperazin-1-yl), —CH(Me)N(Me)(Bn), —CO(4-Bn-1-piperazinyl), —CONH2, —CONH-neopentyl, —CONHBn, —CONH(4-CF3-Bn), —CON(Me)Et, —CON(Me)Bn or —NEt3+Cl−; R2 is H, Me, i-Pr, t-Bu, vinyl, Ph, F, Br, CF3, OCF3, CN, NMe2, NO2, —COMe, —COPh, —CO-thien-2-yl, —CO2Me, —CO2Et, —CO2-neopentyl, —CO2CH2CH═CH2, —CH2OH, —CH2OEt, —CH(Me)OH, —CH(Me)OMe, —CH(Me)OCH2C(Me)2CH2N(Me)2, —CH(Me)OBn, —CH(Me)O(4-i-Pr-Bn), —CH(Me)O(3-CF3-Bn), —CH(Me)O(4-CF3-Bn), —CH(Me)O(4-OPh-Bn), —CH(Me)O(3,5-diCl-Bn), —CH(Me)OCH2(1-Bn-piperidin-4-yl), —C(Me)2OH, —CH2NHBn, —CH2NH(4-CF3-Bn), —CH2N(Me)Bn, —CH(Me)NHCH2-pyridin-2-yl, —CH(Me)NHCH2-pyridin-4-yl, —CH(Me)NHCH2(6-Cl-pyridin-3-yl), —CH(Me)N(Me)(i-Bu), —CH(Me)N(Me)Bn, —CH(Me)N(Me)(4-OMe-Bn), —CH(Me)N(Me)(4-F-Bn), —CH(Me)N(Me)(3-Cl-Bn), —CH(Me)N(Me)(4-Cl-Bn), —CH(Me)N(Me)(3-CF3-Bn), —CH(Me)N(Me)(4-CF3-Bn), —CH(Me)N(Me)(3,4-diCl-Bn), —CH(Me)N(Me)CH2CH2Ph, —CH(Me)N(Me)CH2-pyridin-2-yl, —CH(Me)N(Me)CH2-pyridin-3-yl, —CH(Me)N(Me)CH2-pyridin-4-yl, —CH(Me)N(Me)CH2-furan-2-yl, —CH(Me)N(Me)CH2-thien-2-yl, —CH(Me)N(Me)CH2-(5-Me-thien-2-yl), —CH(Me)N(Me)CH2-(5-Cl-thien-2-yl), —CH(Me)N(Et)Bn, —CH(Me)N(Et)(4-Me-Bn), —CH(Me)N(Et)(2-Cl-Bn), —CH(Me)N(Bn)CH2CN, —CH(Me)N(Bn)CH2CH2OH, —CH(Me)N(Bn)CH2CO2Me, —CH(Me)N(Bn)CH2CONMe2, —CH(Me)N(Bn)CH2CON(Me)(Bn), —CH(Me)-isoindolin-2-yl, —CH(Me)-(1,2,3,4-tetrahydroisoquinolin-2-yl), —CH(Me)(4-Bn-piperazin-1-yl), —CONH-neopentyl, —CONHBn, —CONH(4-CF3-Bn), —CONH(4-NO2-phenethyl), —CONHCH2CH2NHPh, 4-morpholinyl or 1-pyrazolyl; R3 is H, Me, t-Bu, Ph, F, Br, CF3, NO2, —CO-2-thienyl or 1-imidazolyl; R4 is H, Me, Et, i-Pr, F, Br, CF3, NO2, NH2, NHMe, NHBn, —NH(4-OMe-Bn), —NH(4-CF3-Bn), —NH(4-OCF3-Bn), —CO2Me, —NHCO-t-Bu, —NHCO-cyclopropyl, —NHCO-phenethyl, —NHCOCH2OMe, —NHCOCH2OPh, —NHCOCH2OBn, —NHCOCH2O-(4-t-Bu-Ph), —NHCO(4-Ph-Ph), —NHCO(5-(3,5-diCl-OPh)-furan-2-yl), —NHCOC(Me)2O(-4-Cl-Ph), —NHCO2Et or —NHSO2(i-Pr); alternatively, [chemical expression included] is [chemical expression included] R5 is Ph, 2-Et, 3-Et-Ph, 2-i-Pr-Ph, 2-t-Bu-Ph, 3-F-Ph, 2-Cl-Ph, 3-Cl-Ph, 3-Br-Ph, 3-CN-Ph, 2-CF3-Ph, 3-CF3-Ph, 2-OCF3-Ph, 3-OCF3-Ph, 3-Ph-Ph, 2,3-diCl-Ph, 2,5-diCl-Ph, 3,5-diCl-Ph, 2-F-3-CF3-Ph, 2-F-5-CF3-Ph, 2-Cl-5-CF3-Ph or 3,5-diCF3-Ph; and R7 is H, Cl, OMe, NHMe, —CO2Me or —CONH2. |
| Claim: |
13. A compound according to claim 9, wherein the compound is of Formula (Ib′): [chemical expression included] or a stereoisomer or a pharmaceutically acceptable salt thereof. |
| Claim: |
14. A compound according to claim 11, wherein the compound is of Formula (Ic′), or a stereoisomer or a pharmaceutically acceptable salt thereof, wherein: X is NH, NC1-4 alkyl, O or S; R1, R2, R3, and R4 are, independently at each occurrence, H, F, Br, CF3, CN, OCF3, NH2, NHC1-4 alkyl, N(C1-4 alkyl)2, NO2, NHBn, —CH2OC1-4 alkyl, —CH(C1-4 alkyl)OC1-4 alkyl, —CH(C1-4 alkyl)OCH2C(Me)2CH2N(C1-4 alkyl)2, —CH(C1-4 alkyl)O-benzyl, —CH(C1-4 alkyl)OCH2(1-Bn-piperidin-4-yl), —CH2NH-benzyl, —CH2N(C1-4 alkyl)2, —CH2N(C1-4 alkyl)-benzyl, —CH(C1-4 alkyl)NH-benzyl, —CH2(4-Bn-piperazin-1-yl), —CH(C1-4 alkyl)NH(CH2)n-(5- to 6-membered heteroaryl), —CH(C1-4 alkyl)N(C1-4 alkyl)2, —CH(C1-4 alkyl)N(C1-4 alkyl)(CH2)n-phenyl, —CH(C4 alkyl)N(C1-4 alkyl)(CH2)n-(5- to 6-membered heteroaryl), —CH(C1-4 alkyl)N(benzyl)(CH2)tCN, —CH(C1-4 alkyl)N(benzyl)(CH2)tOH, —CH(C1-4 alkyl)N(benzyl)(CH2)tOC1-4 alkyl, —CH(C1-4 alkyl)N(benzyl)(CH2)tCO2C1-4 alkyl, —CH(C1-4 alkyl)N(benzyl)(CH2)tCONH2, —CH(C1-4 alkyl)N(benzyl)(CH2)tCONHC1-4 alkyl, —CH(C1-4 alkyl)N(benzyl)(CH2)tCON(C1-4 alkyl)2, —CH(C1-4 alkyl)N(benzyl))(CH2)tCON(C1-4 alkyl)(benzyl), —CH(C1-4 alkyl)-isoindolin-2-yl, —CH(C1-4 alkyl)-(1,2,3,4-tetrahydroisoquinolin-2-yl), —CH(C1-4 alkyl)(4-Bn-piperazin-1-yl), —COC1-4 alkyl, —CO-phenyl, —CO-(5- to 6-membered heteroaryl), —CO(4-Bn-piperazin-1-yl), —CO2H, —CO2C1-6 alkyl, —CO2C2-6 alkenyl, —CONH2, —CONHC1-6 alkyl, —CON(C1-4 alkyl)2, —CONH-benzyl, —CON(C1-4 alkyl)-benzyl, —CONH-phenethyl, —CONHCH2CH2NH-phenyl, —NHCOC4 alkyl, —NHCO—C3-6 cycloalkyl, —NHCO-phenyl, —NHCO-benzyl, —NHCO-phenethyl, —NHCOCH2OC1-4 alkyl, —NHCOCH2O-phenyl, —NHCOCH2O-benzyl, —NHCO(5-phenoxy-furan-2-yl), —NHCOC(Me)2O-phenyl, —NHCO2C1-4 alkyl, —NHCO2-phenyl, —NHCO2-benzyl, —NHSO2(C1-4 alkyl), C1-6 alkyl substituted with 0-1 Ra, C2-6 alkenyl substituted with 0-1 Ra, phenyl, benzyl, 4-morpholinyl, 1-pyrazolyl, 1-imidazolyl or —NEt3+Cl−; wherein phenyl, benzyl, phenethyl, phenoxy and benzoxy are substituted with 0-3 Re; wherein the 5- to 6-membered heteroaryl is selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, triazolyl, tetrazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl and triazinyl, and substituted with 0-3 Re; alternatively, each of R1, R2, R3 and R4 are selected to contain carbon, nitrogen or oxygen and R1+R2, R2+R3, or R3+R4, combined with the carbon atoms to which they are attached, form a 5- or 6-membered carbocycle or heterocycle comprising: carbon atoms and 0-3 additional heteroatoms selected from N, NH, O and S(O)p, and substituted with 0-2 Rb; R5 is phenyl substituted with 0-2 Rb; alternatively, R5 is [chemical expression included] R7 is H, F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, CF3, OCF3, NH2, NHC1-4 alkyl, N(C1-4 alkyl)2, CO2H, —CO2C1-4 alkyl, —CONH2, —CONHC1-4 alkyl or —CON(C1-4 alkyl)2; Ra is, independently at each occurrence, H, F, OCF3, CF3, OH, OC1-4 alkyl, CN, NH2, NHC1-4 alkyl, N(C1-4 alkyl)2, —CONH2, —CONHC1-4 alkyl or —CON(C1-4 alkyl)2; Rb is, independently at each occurrence, F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, CF3, OCF3, NH2, NHC1-4 alkyl, N(C1-4 alkyl)2, CO2H, —CO2C1-4 alkyl, —CONH2, —CONHC1-4 alkyl or —CON(C1-4 alkyl)2; Re is, independently at each occurrence, F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, CF3, OCF3, NH2, NHC1-4 alkyl, N(C1-4 alkyl)2, NO2, CO2H, —CO2C1-4 alkyl, —CONH2, —CONHC1-4 alkyl, —CON(C1-4 alkyl)2, Ph, Bn or OPh; n, at each occurrence, is selected from 0, 1, 2 and 3; and t, at each occurrence, is selected from 1, 2 and 3; provided that: i) when R7 is H or CF3, then R1, R2, R3 or R4 are other than phenoxy; and ii) when R7 is H, Cl or CF3, then R5 is other than phenyl. |
| Claim: |
15. A compound according to claim 9, wherein: R1 is H, Me, t-Bu, F, Br, CN, NH2, NO2, —CH2OH, —CH(Me)OH, —CO2Me, —CH2NH(4-CF3-Bn), —CH2N(Me)Et, —CH2N(Me)Bn, —CH2N(Me)(4-CF3-Bn), —CH2(4-Bn-piperazin-1-yl), —CH(Me)N(Me)(Bn), —CO(4-Bn-1-piperazinyl), —CONH2, —CONH-neopentyl, —CONHBn, —CONH(4-CF3-Bn), —CON(Me)Et, —CON(Me)Bn or —NEt3+Cl−; R2 s H, Me, i-Pr, t-Bu, vinyl, Ph, F, Br, CF3, OCF3, CN, NMe2, NO2, —COMe, —COPh, —CO-thien-2-yl, —CO2Me, —CO2Et, —CO2-neopentyl, —CO2CH2CH═CH2, —CH2OH, —CH2OEt, —CH(Me)OH, —CH(Me)OMe, —CH(Me)OCH2C(Me)2CH2N(Me)2, —CH(Me)OBn, —CH(Me)O(4-i-Pr-Bn), —CH(Me)O(3-CF3-Bn), —CH(Me)O(4-CF3-Bn), —CH(Me)O(4-OPh-Bn), —CH(Me)O(3,5-diCl-Bn), —CH(Me)OCH2(1-Bn-piperidin-4-yl), —C(Me)2OH, —CH2NHBn, —CH2NH(4-CF3-Bn), —CH2N(Me)Bn, —CH(Me)NHCH2-pyridin-2-yl, —CH(Me)NHCH2-pyridin-4-yl, —CH(Me)NHCH2(6-Cl-pyridin-3-yl), —CH(Me)N(Me)(i-Bu), —CH(Me)N(Me)Bn, —CH(Me)N(Me)(4-OMe-Bn), —CH(Me)N(Me)(4-F-Bn), —CH(Me)N(Me)(3-Cl-Bn), —CH(Me)N(Me)(4-Cl-Bn), —CH(Me)N(Me)(3-CF3-Bn), —CH(Me)N(Me)(4-CF3-Bn), —CH(Me)N(Me)(3,4-diCl-Bn), —CH(Me)N(Me)CH2CH2Ph, —CH(Me)N(Me)CH2-pyridin-2-yl, —CH(Me)N(Me)CH2-pyridin-3-yl, —CH(Me)N(Me)CH2-pyridin-4-yl, —CH(Me)N(Me)CH2-furan-2-yl, —CH(Me)N(Me)CH2-thien-2-yl, —CH(Me)N(Me)CH2-(5-Me-thien-2-yl), —CH(Me)N(Me)CH2-(5-Cl-thien-2-yl), —CH(Me)N(Et)Bn, —CH(Me)N(Et)(4-Me-Bn), —CH(Me)N(Et)(2-Cl-Bn), —CH(Me)N(Bn)CH2CN, —CH(Me)N(Bn)CH2CH2OH, —CH(Me)N(Bn)CH2CO2Me, —CH(Me)N(Bn)CH2CONMe2, —CH(Me)N(Bn)CH2CON(Me)(Bn), —CH(Me)-isoindolin-2-yl, —CH(Me)-(1,2,3,4-tetrahydroisoquinolin-2-yl), —CH(Me)(4-Bn-piperazin-1-yl), —CONH-neopentyl, —CONHBn, —CONH(4-CF3-Bn), —CONH(4-NO2-phenethyl), —CONHCH2CH2NHPh, 4-morpholinyl or 1-pyrazolyl; R3 is H, Me, t-Bu, Ph, F, Br, CF3, NO2, —CO-2-thienyl or 1-imidazolyl; R4 is H, Me, F, i-Pr, F, Br, CF3, NO2, NH2, NHMe, NHBn, —NH(4-OMe-Bn), —NH(4-CF3-Bn), —NH(4-OCF3-Bn), —CO2Me, —NHCO-t-Bu, —NHCO-cyclopropyl, —NHCO-phenethyl, —NHCOCH2OMe, —NHCOCH2OPh, —NHCOCH2OBn, —NHCOCH2O-(4-t-Bu-Ph), —NHCO(4-Ph-Ph), —NHCO(5-(3,5-diCl-OPh)-furan-2-yl), —NHCOC(Me)2O(-4-Cl-Ph), —NHCO2Et or —NHSO2(i-Pr); alternatively, [chemical expression included] is [chemical expression included] R5 is Ph, 2-Et, 3-Et-Ph, 2-i-Pr-Ph, 2-t-Bu-Ph, 3-F-Ph, 2-Cl-Ph, 3-Cl-Ph, 3-Br-Ph, 3-CN-Ph, 2-CF3-Ph, 3-CF3-Ph, 2-OCF3-Ph, 3-OCF3-Ph, 3-Ph-Ph, 2,3-diCl-Ph, 2,5-diCl-Ph, 3,5-diCl-Ph, 2-F-3-CF3-Ph, 2-F-5-CF3-Ph, 2-Cl-5-CF3-Ph, 3,5-diCF3Ph or [chemical expression included] and R7 is H, Cl, OMe, NHMe, —CO2Me or —CONH2; provided that: i) when R7 is H, then R2 is other than OPh; and ii) when R7 is H or Cl, then R5 is other than phenyl. |
| Claim: |
16. A compound according to claim 1, wherein the compound is selected from the group consisting of: [2-(2-tert-butyl-phenoxy)-pyridin-3-yl]-(5-methyl-benzooxazol-2-yl)-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-5-chlorobenzo[d]oxazol-2-amine; 5-tert-butyl-N-(2-(2-tert-butylphenoxy)pyridin-3-yl)benzo[d]oxazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-5-phenylbenzo[d]oxazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-5-(1H-imidazol-1-yl)-7-methyl-1H-benzo[d]imidazol-2-amine; (2-(2-(2-tert-butylphenoxy)-6-methoxypyridin-3-ylamino)-1H-benzo[d]imidazol-5-yl)(thiophen-2-yl)methanone; N-(2-(2-tert-butylphenoxy)-6-methoxypyridin-3-yl)-5-(1H-imidazol-1-yl)-7-methyl-1H-benzo[d]imidazol-2-amine; 5-tert-butyl-N-(2-(3-(trifluoromethyl)phenoxy)pyridin-3-yl)benzo[d]oxazol-2-amine; 5-phenyl-N-(2-(3-(trifluoromethyl)phenoxy)pyridin-3-yl)benzo[d]oxazol-2-amine; thiophen-2-yl(2-(2-(3-(trifluoromethyl)phenoxy)pyridin-3-ylamino)-3H-benzo[d]imidazol-5-yl)methanone; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-methylbenzo[d]oxazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-1H-naphtho[2,3-d]imidazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-1H-naphtho[1,2-d]imidazol-2-amine; [2-(2-tert-butyl-phenoxy)-pyridin-3-yl]-(6,7-dihydro-1H-5,8-dioxa-1,3-diaza-cyclopenta[b]naphthalen-2-yl)-amine; [2-(2-tert-butyl-phenoxy)-pyridin-3-yl]-(5H-[1,3]dioxolo[4′,5′:4,5]benzo[1,2-d]imidazol-6-yl)-amine; N-(2-(2-tert-butylphenoxy)-6-methoxy-pyridin-3-yl)-1H-naphtho[1,2-d]imidazol-2-amine; [2-(2-tert-butyl-phenoxy)-6-methoxy-pyridin-3-yl]-(7,8-dihydro-1H-6,9-dioxa-1,3-diaza-cyclopenta[a]naphthalen-2-yl)-amine; [2-(2-tert-butyl-phenoxy)-6-methoxy-pyridin-3-yl]-(6,7-dihydro-1H-5,8-dioxa-1,3-diaza-cyclopenta[b]naphthalen-2-yl)-amine; [2-(2-tert-butyl-phenoxy)-6-methoxy-pyridin-3-yl]-(5H-[1,3]dioxolo[4′,5′:4,5]benzo[1,2-d]imidazol-6-yl)-amine; (7,8-dihydro-1H-6,9-dioxa-1,3-diaza-cyclopenta[a]naphthalen-2-yl)-[2-(3-trifluoromethyl-phenoxy)-pyridin-3-yl]-amine; (6,7-dihydro-1H-5,8-dioxa-1,3-diaza-cyclopenta[b]naphthalen-2-yl)-[2-(3-trifluoromethyl-phenoxy)-pyridin-3-yl]-amine; (5H-[1,3]dioxolo[4′,5′:4,5]benzo[1,2-d]imidazol-6-yl)-[2-(3-trifluoromethyl-phenoxy)-pyridin-3-yl]-amine; [2-(2-tert-butyl-phenoxy)-pyridin-3-yl]-(7,8-dihydro-1H-6,9-dioxa-1,3-diaza-cyclopenta[a]naphthalen-2-yl)-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-methylbenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-5-methylbenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-7-methylbenzo[d]thiazol-2-amine; 6-tert-butyl-N-(2-(2-tert-butylphenoxy)pyridin-3-yl)benzo[d]thiazol-2-amine; 5-tert-butyl-N-(2-(2-tert-butylphenoxy)pyridin-3-yl)benzo[d]thiazol-2-amine; 7-tert-butyl-N-(2-(2-tert-butylphenoxy)pyridin-3-yl)benzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(trifluoromethyl)benzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(trifluoromethoxy)benzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-phenylbenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)naphtho[1,2-d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-4,6-dimethylbenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-4,6-dichlorobenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-4-methyl-6-(trifluoromethoxy)benzo[d]thiazol-2-amine; methyl 5-(6-tert-butyl-1H-benzo[d]imidazol-2-ylamino)-6-(2-tert-butylphenoxy)picolinate; 5-(6-tert-butyl-1H-benzo[d]imidazol-2-ylamino)-6-(2-tert-butylphenoxy)picolinamide; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-1H-imidazo[4,5-b]pyridin-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-morpholino-1H-benzo[d]imidazol-2-amine; 6-tert-butyl-N-(2-(2,2-dimethyl-2,3-dihydrobenzofuran-7-yloxy)pyridin-3-yl)-1H-benzo[d]imidazol-2-amine; N2-(2-(2-tert-butylphenoxy)pyridin-3-yl)benzo[d]oxazole-2,4-diamine; N-(2-(2-tert-butylphenoxy)pyridine-3-yl)-1-methyl-1H-pyrrolo[2,3-b]pyridine-5-amine; N-(1-benzylpiperidin-4-yl)-2-(2-(2-tert-butylphenoxy)pyridin-3-ylamino)-3H-benzo[d]imidazole-5-carboxamide; N-(2-benzo[d][1,3]dioxol-5-yl)ethyl)-2-(2-(2-tert-butylphenoxy)pyridin-3-ylamino)-3H-benzo[d]imidazole-5-carboxamide; (4-benzylpiperazin-1-yl)(2-(2-(2-tert-butylphenoxy)pyridin-3-ylamino)-3H-benzo[d]imidazol-4-yl)methanone; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(1-(piperidin-1-yl)ethyl)-1H-benzo[d]imidazol-2-amine; 6-(1-(4-benzylpiperazin-1-yl)ethyl)-N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-1H-benzo[d]imidazol-2-amine; 7-((4-benzylpiperazin-1-yl)methyl)-N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-1H-benzo[d]imidazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(1-(isoindolin-2-yl)ethyl)-1H-benzo[d]imidazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(1-((6-chloropyridin-3-yl)methylamino)ethyl)-1H-benzo[d]imidazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(1-(pyridin-3-ylmethylamino)ethyl)-1H-benzo[d]imidazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(1-(methyl(pyridin-3-ylmethyl)amino)ethyl)-1H-benzo[d]imidazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(1-(methyl(pyridin-4-ylmethyl)amino)ethyl)-1H-benzo[d]imidazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(1-(pyridin-4-ylmethylamino)ethyl)-1H-benzo[d]imidazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(1-(methyl(pyridin-2-ylmethyl)amino)ethyl)-1H-benzo[d]imidazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(1-(pyridin-2-ylmethylamino)ethyl)-1H-benzo[d]imidazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(1-((furan-2-ylmethyl)(methyl)amino)ethyl)-1H-benzo[d]imidazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(1-(3,4-dihydroisoquinolin-2(1H)-yl)ethyl)-1H-benzo[d]imidazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(1-(((5-chlorothiophen-2-yl)methyl)(methyl)amino)ethyl)-1H-benzo[d]imidazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(1-(methyl((5-methylthiophen-2-yl)methyl)amino)ethyl)-1H-benzo[d]imidazol-2-amine; 6-(1-((1-benzylpiperidin-4-yl)methoxy)ethyl)-N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-1H-benzo[d]imidazol-2-amine; 1-(2-(2-(2-tert-butylphenoxy)pyridine-3-ylamino)benzo[d]thiazol-6-yl)ethanone; 2,2-dibromo-1-(2-(2-(2-tert-butylphenoxy)pyridine-3-ylamino)benzo[d]thiazol-6-yl)ethanone; 1-(2-(2-(2-tert-butylphenoxy)pyridine-3-ylamino)benzo[d]thiazol-6-yl)ethanol; 6-(1-(benzyl(methyl)amino)ethyl)-N-(2-(2-tert-butylphenoxy)pyridin-3-yl)benzo[d]thiazol-2-amine; 6-(1-((4-(trifluoromethyl)benzyl)(methyl)amino)ethyl)-N-(2-(2-tert-butylphenoxy)pyridin-3-yl)benzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(1-(((5-chlorothiophen-2-yl)methyl)(methyl)amino)ethyl)benzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridine-3-yl)benzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridine-3-yl)-5-(trifluoromethyl)benzo[d]thiazol-amine; N-(2-(2-tert-butylphenoxy)pyridine-3-yl)-6-methoxybenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridine-3-yl)-6-isopropylbenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridine-3-yl)benzo[d]thiazol-6-amine; 6-bromo-N-(2-(2-tert-butylphenoxy)pyridin-3-yl)benzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-4-(methylthio)benzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-7-fluoro-4-methylbenzo[d]thiazol-2-amine; 5-(benzyloxy)-N-(2-(2-tert-butylphenoxy)pyridin-3-yl)benzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-5-methoxybenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-7-chloro-4-methoxybenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-4-methoxybenzo[d]thiazol-2-amine; 6-bromo-N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-4-fluorobenzo[d]thiazol-2-amine; [2-(2-tert-butyl-phenoxy)-pyridin-3-yl]-(6,7-dihydro-5,8-dioxa-1-thia-3-aza-cyclopenta[b]naphthalen-2-yl)-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(1H-pyrazol-1-yl)benzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-chlorobenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-5-chlorobenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-4-chlorobenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-fluorobenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-ethoxybenzo[d]thiazol-2-anine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-nitrobenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-5,6-dimethylbenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-4,6-difluorobenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-methoxy-4-methylbenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-4,6,7-trimethylbenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-4,7-dimethylbenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-4-ethylbenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-4-isopropylbenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-4,5-dimethylbenzo[d]thiazol-2-amine; 4-bromo-N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-isopropylbenzo[d]thiazol-2-amine; methyl 2-(2-(2-tert-butylphenoxy)pyridin-3-ylamino)benzo[d]thiazole-4-carboxylate; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-5-chloro-4-methylbenzo[d]thiazol-2-amine; ethyl 2-(2-(2-tert-butylphenoxy)pyridin-3-ylamino)benzo[d]thiazole-6-carboxylate; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-phenoxybenzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-7-chloro-6-methylbenzo[d]thiazol-2-amine; 6-(benzyloxy)-N-(2-(2-tert-butylphenoxy)pyridin-3-yl)benzo[d]thiazol-2-amine; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-4-fluoro-6-methylbenzo[d]thiazol-2-amine; N-(2-(2-(2-tert-butylphenoxy)pyridine-3-ylamino)benzo[d]oxazol-4-yl)-2-phenoxyacetamide; N-(2-(2-(2-tert-butylphenoxy)pyridin-3-ylamino)benzo[d]oxazol-4-yl)cyclopropanecarboxamide; N-(2-(2-(2-tert-butylphenoxy)pyridin-3-ylamino)benzo[d]oxazol-4-yl)pivalamide; N-(2-(2-(2-tert-butylphenoxy)pyridin-3-ylamino)benzo[d]oxazol-4-yl)-2-methoxyacetamide; N-(2-(2-(2-tert-butylphenoxy)pyridin-3-ylamino)benzo[d]oxazol-4-yl)propane-2-sulfonamide; N4-benzyl-N2-(2-(2-tert-butylphenoxy)pyridin-3-yl)benzo[d]oxazole-2,4-diamine; N4-(4-(trifluoromethyl)benzyl)-N2-(2-(2-tert-butylphenoxy)pyridin-3-yl)benzo[d]oxazole-2,4-diamine; N4-(4-methoxybenzyl)-N2-(2-(2-tert-butylphenoxy)pyridin-3-yl)benzo[d]oxazole-2,4-diamine; N2-(2-(2-tert-butylphenoxy)pyridin-3-yl)-N4-methylbenzo[d]oxazole-2,4-diamine; N4-(4-(trifluoromethoxy)benzyl)-N2-(2-(2-tert-butylphenoxy)pyridin-3-yl)benzo[d]oxazole-2,4-diamine; 2-(4-tert-butylphenoxy)-N-(2-(2-(2-tert-butylphenoxy)pyridin-3-ylamino)benzo[d]oxazol-4-yl)acetamide; 2-(benzyloxy)-N-(2-(2-(2-tert-butylphenoxy)pyridin-3-ylamino)benzo[d]oxazol-4-yl)acetamide; N-(2-(2-(2-tert-butylphenoxy)pyridin-3-ylamino)benzo[d]oxazol-4-yl)-5-(3,5-dichlorophenoxy)furan-2-carboxamide; biphenyl-4-carboxylic acid {2-[2-(2-tert-butyl-phenoxy)-pyridin-3-ylamino]-benzooxazol-4-yl}-amide; ethyl 2-(2-(2-tert-butylphenoxy)pyridin-3-ylamino)benzo[d]oxazol-4-ylcarbamate; N-(2-(2-(2-tert-butylphenoxy)pyridin-3-ylamino)benzo[d]oxazol-4-yl)-3-phenylpropanamide; N-(2-(2-(2-tert-butylphenoxy)pyridin-3-ylamino)benzo[d]oxazol-4-yl)-2-(4-chlorophenoxy)-2-methylpropanamide; N-{2-[[2-(2-tert-butyl-phenoxy)-pyridin-3-yl]-(3-phenyl-propionyl)-amino]-benzooxazol-4-yl}-3-phenyl-propionamide; N-(2-(2-tert-butylphenoxy)pyridin-3-yl)-6-(1-methoxyethyl)benz[d]thiazol-2-amine; and tert-butyl 6-bromobenzo[d]thiazol-2-yl(2-(2-tert-butylphenoxy)pyridin-3-yl)carbamate; and a stereoisomer or pharmaceutically acceptable salt of any of the foregoing. |
| Claim: |
17. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 1. |
| Claim: |
18. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 16. |
| Current U.S. Class: |
514/338 |
| Current International Class: |
61; 07; 07 |
| رقم الانضمام: |
edspap.20080275090 |
| قاعدة البيانات: |
USPTO Patent Applications |