Claims
- 1. A compound having a Formula I:
- 2. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein:
X is
(1) —CH2—, (2) —C(O)—, (3) —CH(ORa)—, or (4) not present.
- 3. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein:
X is
—CH(ORa)—.
- 4. The compound according to claim 3, or a pharmaceutically acceptable salt thereof, wherein n is 1.
- 5. The compound according to claim 2, or a pharmaceutically acceptable salt thereof, wherein:
X is
(1) —CH2—, (2) —C(O)—, or (3) not present.
- 6. The compound according to claim 5, or a pharmaceutically acceptable salt thereof, wherein n is 1.
- 7. The compound according to claim 2, or a pharmaceutically acceptable salt thereof, wherein:
X is
(1) —CH2—, (2) —C(O)—, or (3) not present; and R1 is
(1) R7, (2) C(O)R7, (15) CO2Rb, (16) C(O)N(ORb)Rc, (17) C(O)NRcRd, (18) a 3- to 8-membered heterocycle containing 1 to 4 heteroatoms, optionally substituted by 1 to 4 groups, each group independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, NRcRd, oxo, thiono, ORa, S(O)niRa (where ni=0, 1 or 2), C(O)Ra, C(O)NRcRd, cyano, (C0-C6alkyl)aryl, CO2Rb, or halogen, and each group is saturated, partly unsaturated or fully unsaturated, wherein the heteroatoms are each independently oxygen, sulfur, or nitrogen, in which the nitrogen optionally has an Rc substituent, (19) a benzene ring fused to a 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms, optionally substituted by 1 to 4 groups each independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, amino, oxo, thiono, C(O)NRcRd, cyano, CO2Rb or halogen, each group is saturated, partly unsaturated, or fully unsaturated, wherein the heteroatoms are each independently oxygen, sulfur, or nitrogen, in which the nitrogen optionally has an Rc substituent, and wherein the benzene/heterocycle fused ring is attached at any site to X or to the tetrapeptide, or (20) a 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms fused to a second 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms, each heterocyclic ring independently optionally substituted by 1 to 4 groups, each group independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, amino, oxo, thiono, C(O)NRcRd, cyano, CO2Rb or halogen, wherein each heterocycle is saturated, partly unsaturated or fully unsaturated, and wherein each heteroatom independently is oxygen, sulfur, or nitrogen, and the nitrogen optionally has an Rc substituent.
- 8. The compound according to claim 7, or a pharmaceutically acceptable salt thereof, wherein n is 1.
- 9. The compound according to claim 2, or a pharmaceutically acceptable salt thereof, wherein:
X is
(1) —CH2—, (2) —C(O)—, or (3) not present; RI is
(1) R7, (9) C(O)R7, (10) CO2Rb, (11) C(O)N(ORb)Rc, (12) C(O)NRcRd, (13) a 3- to 8-membered heterocycle containing 1 to 4 heteroatoms, optionally substituted by 1 to 4 groups, each group independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, NRcRd, oxo, thiono, ORa, S(O)niRa (where ni=0, 1 or 2), C(O)Ra, C(O)NRcRd, cyano, (C0-C6alkyl)aryl, CO2Rb, or halogen, and each group is saturated, partly unsaturated or fully unsaturated, wherein the heteroatoms are each independently oxygen, sulfur, or nitrogen, in which the nitrogen optionally has an Rc substituent, (14) a benzene ring fused to a 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms, optionally substituted by 1 to 4 groups each independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, amino, oxo, thiono, C(O)NRcRd, cyano, CO2Rb or halogen, each group is saturated, partly unsaturated, or fully unsaturated, wherein the heteroatoms are each independently oxygen, sulfur, or nitrogen, in which the nitrogen optionally has an Rc substituent, and wherein the benzene/heterocycle fused ring is attached at any site to X or to the tetrapeptide, or (15) a 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms fused to a second 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms, each heterocyclic ring independently optionally substituted by 1 to 4 groups, each group independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, amino, oxo, thiono, C(O)NRcRd, cyano, CO2Rb or halogen, wherein each heterocycle is saturated, partly unsaturated or fully unsaturated, and wherein each heteroatom independently is oxygen, sulfur, or nitrogen, and the nitrogen optionally has an Rc substituent; and R2 is
(1) optionally substituted C2-C12alkyl, (2) optionally substituted C2-C12alkenyl, (3) optionally substituted C2-C12alkynyl, or (4) (CH2)nii—O—(CH2)mii—CH3, wherein the optional substituents on the C2-C12alkyl, C2-C12alkenyl, and C2-C12alkynyl are 1 to 5 groups and each group independently is
(a) CO2Ra, (b) C(O)Rb, (c) C(O)N(ORb)Rc, (d) C(O)NRcRd, (e) C(O)NRcNRcRd, (f) C(O)NRcSO2R7, (g) C3-C8cycloalkyl, (h) C2-C5alkenyl, (i) cyano, (j) ═NORa, (k) ═NNRbRc, (l) ═NNRbS(O)niR7, (m) N(ORb)C(O)NRbRc, (n) N(ORb)C(O)R7, (o) NHC(O)N(ORb)Rc, (p) NRcCO2Rb, (q) NRcC(O)NRcRd, (r) NRcC(S)NRcRd, (s) NRcC(O)R7, (t) NRbS(O)niR7, (u) NRcCH2CO2Ra, (v) NRcC(S)R7,
(x) NRcC(O)CH2OH, (y) NRcC(O)CH2SH, (z) NRcCH2CH(OH)R7, (aa) NRcP(O)(ORa)R7, (bb) NY1Y2, wherein Y1 and Y2 are independently H or methyl, (cc) NO2, (dd) N(ORb)C(O)Rb, (ee) C1-C3alkanoylamino, (ff) ORa, (gg) OS(O)niR7, (hh) oxo, (ii) OCO2Rb, (jj) OC(O)NRcRd, (kk) P(O)(ORa)2, (l) P(O)(ORa)R7, (mm) SC(O)R7, (nn) S(O)niR7, (oo) SR7, (pp) S(O)niNRcRd, (qq) diazo, (rr) C1-C5 perfluoroalkyl, (ss) B(O)(ORa)ORa, (tt) halogen, (uu) aryl(C0-C5alkyl), wherein the aryl is optionally substituted with 1 to 3 groups, wherein each group independently is Rf, or (xxii) a 3- to 6-membered heterocycle containing from 1 to 4 heteroatoms, each heteroatom independently is oxygen, sulfur or nitrogen, wherein the heterocycle is optionally substituted by 1 to 3 groups, wherein each group independently is Rf, and the heterocycle is saturated or partly unsaturated.
- 10. The compound according to claim 9, or a pharmaceutically acceptable salt thereof, wherein n is 1.
- 11. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein:
R3 each independently is
(1) hydrogen, (2) halogen, (3) ORa, (4) C1-C4alkyl, or (5) aryl; and Ra is
(1) hydrogen, (2) optionally substituted C1-C6alkyl, (3) optionally substituted C3-C6alkenyl, (4) optionally substituted C2-C4alkanoyl, (5) optionally substituted C3-C4alkenoyl, (6) optionally substituted aroyl, (7) optionally substituted aryl, (8) optionally substituted C5-C6cycloalkanoyl, (9) optionally substituted C1-C4alkylsulfonyl, (10) optionally substituted C5-C6cycloalkyl, (11) optionally substituted C5-C6cycloalkenyl, wherein the optional substituents on the C1-C6alkyl, C3-C6alkenyl, C2-C4alkanoyl, C3-C4alkenoyl, aroyl, aryl, C5-C6cycloalkanoyl, C1-C4alkylsulfonyl, C5-C6cycloalkyl and C5-C6cycloalkenyl are from 1 to 10 groups, wherein each group independently is hydroxy, methoxy, aryl methoxy, NRxRx, CO2Rb, CONRcRd, or halogen, (12) CF3, (13) arylsulfonyl optionally substituted with 1 to 3 groups, wherein each group independently is methyl, CF3, nitro, halogen or cyano, or (14) a 5- or 6-membered heterocycle containing 1 to 3 heteroatoms, wherein each heteroatom is oxygen, sulfur or nitrogen, wherein the heterocycle is optionally substituted by 1 to 3 groups, wherein each group independently is methyl, CF3, NMe2, C(O)NRcRd, cyano, CO2Rb or halogen, and wherein the heterocycle is saturated or partly unsaturated.
- 12. The compound according to claim 11, or a pharmaceutically acceptable salt thereof, wherein:
R3 each independently is
(1) hydrogen, (2) halogen, (3) ORa, (4) C1-C4alkyl, or (5) aryl; Ra is
(1) hydrogen, (2) optionally substituted C1-C6alkyl, (3) optionally substituted C3-C6alkenyl, (5) optionally substituted C2-C4alkanoyl, (6) optionally substituted C3-C4alkenoyl, (8) optionally substituted aroyl, (9) optionally substituted aryl, (10) optionally substituted C5-C6cycloalkanoyl, (12) optionally substituted C1-C4alkylsulfonyl, (13) optionally substituted C5-C6cycloalkyl, (14) optionally substituted C5-C6cycloalkenyl, wherein the optional substituents on the C1-C6alkyl, C3-C6alkenyl, C2-C4alkanoyl, C3-C4alkenoyl, aroyl, aryl, C5-C6cycloalkanoyl, C1-C4alkylsulfonyl, C5-C6cycloalkyl and C5-C6cycloalkenyl are from 1 to 10 groups, wherein each group independently is hydroxy, methoxy, aryl methoxy, NRxRx, CO2Rb, CONRcRd, or halogen, (15) CF3, (16) arylsulfonyl optionally substituted with 1 to 3 groups, wherein each group independently is methyl, CF3, nitro, halogen or cyano, or (17) a 5- or 6-membered heterocycle containing 1 to 3 heteroatoms, wherein each heteroatom is oxygen, sulfur or nitrogen, wherein the heterocycle is optionally substituted by 1 to 3 groups, wherein each group independently is methyl, CF3, NMe2, C(O)NRcRd, cyano, CO2Rb or halogen, and wherein the heterocycle is saturated or partly unsaturated; X is
(1) —CH2—, (2) —C(O)—, (3) ═CH—, or (4) not present; and R1 is
(1) R7, (2) C(O)R7, (3) CN, (4) CO2Rb, (5) C(O)N(ORb)Rc, (6) C(O)NRcRd, (7) NHCO2Rb, (8) NHC(O)NRcRd, (9) (C0-C4alkyl)ORa, (10) (C0-C4alkyl)OCO2Rb, (11) (C0-C4alkyl)OC(O)NRcRd, (12) C(O)NRcNRcRd, (13) C(O)NRcSO2Rb, (14) OS(O)niR7, (15) NRbS(O)niR7, (16) a 3- to 8-membered heterocycle containing 1 to 4 heteroatoms, optionally substituted by 1 to 4 groups, each group independently is C1-C6alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, NRcRd, oxo, thiono, ORa, S(O)niRa, C(O)Ra, C(O)NRcRd, cyano, (C0-C6alkyl)aryl, CO2Rb, or halogen, and each group is saturated, partly unsaturated or fully unsaturated, wherein the heteroatoms are each independently oxygen, sulfur, or nitrogen, in which the nitrogen optionally has an Rc substituent, (17) a benzene ring fused to a 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms, optionally substituted by 1 to 4 groups each independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, amino, oxo, thiono, C(O)NRcRd, cyano, CO2Rb or halogen, each group is saturated, partly unsaturated, or fully unsaturated, wherein the heteroatoms are each independently oxygen, sulfur, or nitrogen, in which the nitrogen optionally has an Rc substituent, and wherein the benzene/heterocycle fused ring is attached at any site to X or to the tetrapeptide, or (18) a 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms fused to a second 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms, each heterocyclic ring independently optionally substituted by 1 to 4 groups, each group independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, amino, oxo, thiono, C(O)NRcRd, cyano, CO2Rb or halogen, wherein each heterocycle is saturated, partly unsaturated or fully unsaturated, and wherein each heteroatom independently is oxygen, sulfur, or nitrogen, and the nitrogen optionally has an Rc substituent.
- 13. The compound according to 12, or a pharmaceutically acceptable salt thereof, wherein n is 1.
- 14. The compound according to claim 11, or a pharmaceutically acceptable salt thereof, wherein:
R3 each independently is
(1) hydrogen, (2) halogen, (3) ORa, (4) C1-C4alkyl, or (5) aryl; Ra is
(1) hydrogen, (2) optionally substituted C1-C6alkyl, (3) optionally substituted C3-C6alkenyl, (5) optionally substituted C2-C4alkanoyl, (6) optionally substituted C3-C4alkenoyl, (8) optionally substituted aroyl, (9) optionally substituted aryl, (10) optionally substituted C5-C6cycloalkanoyl, (12) optionally substituted C1-C4alkylsulfonyl, (13) optionally substituted C5-C6cycloalkyl, (14) optionally substituted C5-C6cycloalkenyl, wherein the optional substituents on the C1-C6alkyl, C3-C6alkenyl, C2-C4alkanoyl, C3-C4alkenoyl, aroyl, aryl, C5-C6cycloalkanoyl, C1-C4alkylsulfonyl, C5-C6cycloalkyl and C5-C6cycloalkenyl are from 1 to 10 groups, wherein each group independently is hydroxy, methoxy, aryl methoxy, NRxRx, CO2Rb, CONRcRd, or halogen, (15) CF3, (16) arylsulfonyl optionally substituted with 1 to 3 groups, wherein each group independently is methyl, CF3, nitro, halogen or cyano, or (17) a 5- or 6-membered heterocycle containing 1 to 3 heteroatoms, wherein each heteroatom is oxygen, sulfur or nitrogen, wherein the heterocycle is optionally substituted by 1 to 3 groups, wherein each group independently is methyl, CF3, NMe2, C(O)NRcRd, cyano, CO2Rb or halogen, and wherein the heterocycle is saturated or partly unsaturated; X is
(1) —CH2—, (2) —C(O)—, (3) ═CH—, or (4) not present; and R1 is
(1) R7, (2) C(O)R7, (4) CO2Rb, (5) C(O)N(ORb)Rc, (6) C(O)NRcRd, (16) a 3- to 8-membered heterocycle containing 1 to 4 heteroatoms, optionally substituted by 1 to 4 groups, each group independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, NRcRd, oxo, thiono, ORa, S(O)niRa, C(O)Ra, C(O)NRcRd, cyano, (C0-C6alkyl)aryl, CO2Rb, or halogen, and each group is saturated, partly unsaturated or fully unsaturated, wherein the heteroatoms are each independently oxygen, sulfur, or nitrogen, in which the nitrogen optionally has an Rc substituent, (17) a benzene ring fused to a 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms, optionally substituted by 1 to 4 groups each independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, amino, oxo, thiono, C(O)NRcRd, cyano, CO2Rb or halogen, each group is saturated, partly unsaturated, or fully unsaturated, wherein the heteroatoms are each independently oxygen, sulfur, or nitrogen, in which the nitrogen optionally has an Rc substituent, and wherein the benzene/heterocycle fused ring is attached at any site to X or to the tetrapeptide, or (18) a 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms fused to a second 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms, each heterocyclic ring independently optionally substituted by 1 to 4 groups, each group independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, amino, oxo, thiono, C(O)NRcRd, cyano, CO2Rb or halogen, wherein each heterocycle is saturated, partly unsaturated or fully unsaturated, and wherein each heteroatom independently is oxygen, sulfur, or nitrogen, and the nitrogen optionally has an Rc substituent.
- 15. The compound according to claim 14, or a pharmaceutically acceptable salt thereof, wherein n is 1.
- 16. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein:
R6 each independently is
(1) O, (2) S, or (3) H; X is
(1) —CH2—, (2) —C(O)—, (3) ═CH—, or (4) not present; and R1 is
(1) R7, (2) C(O)R7, (3) CN, (4) CO2Rb, (5) C(O)N(ORb)Rc, (6) C(O)NRcRd, (7) NHCO2Rb, (8) NHC(O)NRcRd, (9) (C0-C4alkyl)ORa, (10) (C0-C4alkyl)OCO2Rb, (11) (C0-C4alkyl)OC(O)NRcRd, (12) C(O)NRcNRcRd, (13) C(O)NRcSO2Rb, (14) OS(O)niR7, (15) NRbS(O)niR7, (16) a 3- to 8-membered heterocycle containing 1 to 4 heteroatoms, optionally substituted by 1 to 4 groups, each group independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, NRcRd, oxo, thiono, ORa, S(O)niRa, C(O)Ra, C(O)NRcRd, cyano, (C0-C6alkyl)aryl, CO2Rb, or halogen, and each group is saturated, partly unsaturated or fully unsaturated, wherein the heteroatoms are each independently oxygen, sulfur, or nitrogen, in which the nitrogen optionally has an Rc substituent, (17) a benzene ring fused to a 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms, optionally substituted by 1 to 4 groups each independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, amino, oxo, thiono, C(O)NRcRd, cyano, CO2Rb or halogen, each group is saturated, partly unsaturated, or fully unsaturated, wherein the heteroatoms are each independently oxygen, sulfur, or nitrogen, in which the nitrogen optionally has an Rc substituent, and wherein the benzene/heterocycle fused ring is attached at any site to X or to the tetrapeptide, or (18) a 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms fused to a second 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms, each heterocyclic ring independently optionally substituted by 1 to 4 groups, each group independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, amino, oxo, thiono, C(O)NRcRd, cyano, CO2Rb or halogen, wherein each heterocycle is saturated, partly unsaturated or fully unsaturated, and wherein each heteroatom independently is oxygen, sulfur, or nitrogen, and the nitrogen optionally has an Rc substituent.
- 17. The compound according to claim 16, or a pharmaceutically acceptable salt thereof, wherein n is 1.
- 18. The compound according to claim 16, or a pharmaceutically acceptable salt thereof wherein:
R3 each independently is
(1) hydrogen, (2) halogen, (3) ORa, (4) C1-C4alkyl, or (5) C1-C4aryl; R6 each independently is
(1) O, (2) S, or (3) H; X is
(1) —CH2—, (2) —C(O)—, (3) ═CH—, or (4) not present; and R1 is
(1) R7, (2) C(O)R7, (3) CN, (4) CO2Rb, (5) C(O)N(ORb)Rc, (6) C(O)NRcRd, (7) NHCO2Rb, (8) NHC(O)NRcRd, (9) (C0-C4alkyl)ORa, (10) (C0-C4alkyl)OCO2Rb, (11) (C0-C4alkyl)OC(O)NRcRd, (12) C(O)NRcNRcRd, (13) C(O)NRcSO2Rb, (14) OS(O)niR7, (15) NRbS(O)niR7, wherein ni is from 0 to 2, (16) a 3- to 8-membered heterocycle containing 1 to 4 heteroatoms, optionally substituted by 1 to 4 groups, each group independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, NRcRd, oxo, thiono, ORa, S(O)niRa (where ni=0, 1 or 2), C(O)Ra, C(O)NRcRd, cyano, (C0-C6alkyl)aryl, CO2Rb, or halogen, and each group is saturated, partly unsaturated or fully unsaturated, wherein the heteroatoms are each independently oxygen, sulfur, or nitrogen, in which the nitrogen optionally has an Rc substituent, (17) a benzene ring fused to a 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms, optionally substituted by 1 to 4 groups each independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, amino, oxo, thiono, C(O)NRcRd, cyano, CO2Rb or halogen, each group is saturated, partly unsaturated, or fully unsaturated, wherein the heteroatoms are each independently oxygen, sulfur, or nitrogen, in which the nitrogen optionally has an Rc substituent, and wherein the benzene/heterocycle fused ring is attached at any site to X or to the tetrapeptide, or (18) a 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms fused to a second 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms, each heterocyclic ring independently optionally substituted by 1 to 4 groups, each group independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, amino, oxo, thiono, C(O)NRcRd, cyano, CO2Rb or halogen, wherein each heterocycle is saturated, partly unsaturated or fully unsaturated, and wherein each heteroatom independently is oxygen, sulfur, or nitrogen, and the nitrogen optionally has an Rc substituent.
- 19. The compound according to claim 18, or a pharmaceutically acceptable salt thereof, wherein n is 1 or 2.
- 20. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein X is —CH2—.
- 21. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein X is —C(O)—.
- 22. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein X is not present.
- 23. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein R1 is a 3- to 8-membered heterocycle containing 1 to 4 heteroatoms, optionally substituted by 1 to 4 groups, each group independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, NRcRd, oxo, thiono, ORa, S(O)niRa (where ni=0, 1 or 2), C(O)Ra, C(O)NRcRd, cyano, (C0-C6alkyl)aryl, CO2Rb, or halogen, and each group is saturated, partly unsaturated or fully unsaturated, wherein the heteroatoms are each independently oxygen, sulfur, or nitrogen, in which the nitrogen optionally has an Rc substituent.
- 24. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein RI is a benzene ring fused to a 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms, optionally substituted by 1 to 4 groups each independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, amino, oxo, thiono, C(O)NRcRd, cyano, CO2Rb or halogen, each group is saturated, partly unsaturated, or fully unsaturated, wherein the heteroatoms are each independently oxygen, sulfur, or nitrogen, in which the nitrogen optionally has an Rc substituent, and wherein the benzene/heterocycle fused ring is attached at any site to X or to the tetrapeptide.
- 25. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein R1 is a 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms fused to a second 4- to 8-membered heterocyclic ring with from 1 to 4 heteroatoms, each heterocyclic ring independently optionally substituted by 1 to 4 groups, each group independently is C1-C5alkyl, C2-C5alkenyl, C1-C5perfluoroalkyl, amino, oxo, thiono, C(O)NRcRd, cyano, CO2Rb or halogen, wherein each heterocycle is saturated, partly unsaturated or fully unsaturated, and wherein each heteroatom independently is oxygen, sulfur, or nitrogen, and the nitrogen optionally has an Rc substituent.
- 26. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier.
- 27. A method for the treatment of protozoal infections comprising the step of administering, to a host in need of such treatment, a non-toxic amount of a compound according to claim 1, or a salt thereof, effective to inhibit a histone deacetylase activity of the infecting protozoa.
- 28. A method for the prevention of protozoal infections comprising the step of administering to a host a non-toxic effective preventative amount of a compound according to claim 1, or a salt thereof.
- 29. The compound according to claim 3, or a pharmaceutically acceptable salt thereof, wherein n is 2.
- 30. The compound according to claim 5, or a pharmaceutically acceptable salt thereof, wherein n is 2.
- 31. The compound according to claim 7, or a pharmaceutically acceptable salt thereof, wherein n is 2.
- 32. The compound according to claim 9, or a pharmaceutically acceptable salt thereof, wherein n is 2.
- 33. The compound according to 12, or a pharmaceutically acceptable salt thereof, wherein n is 2.
- 34. The compound according to claim 14, or a pharmaceutically acceptable salt thereof, wherein n is 2.
- 35. The compound according to claim 16, or a pharmaceutically acceptable salt thereof, wherein n is 2.
Parent Case Info
[0001] This is a continuation-in-part of U.S. patent application No. 09/614,793, filed Jul. 12, 2000, which claims the benefit of U.S. Patent Application No. 60/145,329, filed Jul. 23, 1999.
Provisional Applications (1)
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Number |
Date |
Country |
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60145329 |
Jul 1999 |
US |
Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
09614793 |
Jul 2000 |
US |
Child |
10066451 |
Jan 2002 |
US |