Indole derivatives as pde5-inhibitors
AssigneeLilly ICOS LLC
InventorsMark W Orme, Jason Scott Sawyer, Lisa M Schultze
Life of this patent
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Abstract
Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents. 1
Claims25
A compound having a formula
- 26
- wherein R0, independently, is selected from the group consisting of halo and C1-6alkyl;
- R1 is selected from the group consisting of hydrogen, C1-6alkyl, C2-6alkenyl, C0-6alkynyl, haloC1-6-alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-3alkyl, aryl-C1-3alkyl, and heteroarylC1-3alkyl;
- R2 is selected from the group consisting of an optionally substituted monocyclic aromatic ring selected from the group consisting of benzene, thiophene, furan, and pyridine, and an optionally substituted bicyclic ring
- 27
- wherein the fused ring A is a 5- or 6-membered ring, saturated or partially or fully unsaturated, and comprises carbon atoms and optionally one or two heteroatoms selected from oxygen, sulfur, and nitrogen;
- R3 is selected from the group consisting of hydrogen and C1-3alkyl,
- or R1 and R3 together represent a 3- or 4-membered alkyl or alkenyl chain component of a 5- or 6-membered ring;
- X and Y, independently, are selected from the group consisting of C(═O), SO, SO2, C(═S), and C(Ra)21 and with the proviso that at least one of X and Y is different from C(═O);
- Ra is hydrogen, C1-6alkyl, or benzyl;
- and q is 0, 1, 2, 3, or 4,
- and pharmaceutically acceptable salts and solvates thereof.
A compound selected from the group consisting of (6R,12aR)-6-benzo[1,3]dioxol-5-yl-2-methyl-3,4,6,7,12,12a-hexahydro-2H-pyrazino[1′,2′:1,6]pyrido[3,4-b]indol-1-one, (6S,12aR)-6-benzo-[1,3]dioxol-5-yl-2-methyl-3,4,6,7,12,12a-hexahydro-2H-pyrazino[1′,2′:1,6]pyrido[3,4-b]indol-1-one, (6R,12aR)-6-benzo[1,3]dioxol-5-yl-2-methyl-2,3,6,7,12,12a-hexahydropyrazino[1′,2′:1,6]pyrido-[3,4-b]indole-1,4-dithione, (6R,12aS)-6-benzo[1,3]-dioxol-5-yl-2-methyl-2,3,6,7,12,12a-hexahydropyrazino[1′,2′:1,6]pyrido[3,4-b]indole-1,4-dithione, and pharmaceutically acceptable salts and solvates thereof.
A compound selected from the group consisting of
- 31 32
Dependencies are inferred from the claim text.