Claims
- 1. A compound of formula I whereinW is SO2, CO, CONH, CSNH or (CH2)x; X is O, SOy or NR13; Y is CR14; Z is CR15; m and x are each independently 0 or an integer of 1,2 or 3; n is an integer of 1, 2 or 3; p is an integer of 1; R1 is halogen, CN, OR16, CO2R17, CONR18R19, CNR20NR21R22, SO2NR23R24, SOwR25, or a C1-C6alkyl, C2-C8alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, cycloheteroalkyl, phenyl or heteroaryl group each optionally substituted; R2, R3, R5, R6, R7, R8, R9, R10 and R11 are each independently H or an optionally substituted C1-C6alkyl group; R4 is H, CNR26NR27R28 or a C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, cycloheteroalkyl, aryl or heteroaryl group each optionally substituted; R12 is an optionally substituted C1-C6alkyl, aryl or heteroaryl group; y and w are each 0 or an integer of 1 or 2; R13 is H or a C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, cycloheteroalkyl, aryl or heteroaryl group each optionally substituted; R14 and R15 are each independently H, halogen or a C1-C6alkyl, aryl, heteroaryl or C1-C6alkoxy group each optionally substituted; R16 is H, COR29 or a C1-C8alkyl, C2-C6alkenyl, C2-C6alkynyl, aryl or heteroaryl group each optionally substituted; R17 and R29 are each independently H or a C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, cycloheteroalkyl, aryl or heteroaryl group each optionally substituted; R18, R19, R20, R21, R22, R26, R27 and R28 are each independently H or an optionally substituted C1-C6alkyl group; R23and R24 are each independently H or a C1-C6alkyl, aryl or heteroaryl group each optionally substituted; and R25 is an optionally substituted C1-C6alkyl, aryl, or heteroaryl group; or the stereoisomers thereof or the pharmaceutically acceptable salts thereof.
- 2. The compound according to claim 1 wherein W is SO2.
- 3. The compound according to claim 1 wherein X is O.
- 4. The compound according to claim 1 wherein n is 1.
- 5. The compound according to claim 2 wherein R12 is an aryl or heteroaryl group each optionally substituted.
- 6. The compound according to claim 5 wherein X is O and n is 1.
- 7. The compound according to claim 6 selected from the group consisting of1-(phenylsulfonyl)-4-[(2S)-pyrrolidin-2-ylmethoxy]-1H-indole; 1-[(5-chlorothien-2-yl)sulfonyl]-4-[(2S)-pyrrolidin-2-ylmethoxy]-1H-indole; 1-[(2-fluorophenyl)sulfonyl)-4-[(2S)-pyrrolidin-2-ylmethoxy]-1H-indole; 1-[(3-fluorophenyl)sulfonyl)-4-[(2S)-pyrrolidin-2-ylmethoxy]-1H-indole; 1-[(4-fluorophenyl)sulfonyl)-4-[(2S)-pyrrolidin-2-ylmethoxy]-1H-indole; 1-[(3,4-dimethoxyphenyl)sulfonyl)-4-[(2S)-pyrrolidin-2-ylmethoxy]-1H-indole; 4-[(4-[2S)-pyrrolidin-2-ylmethoxy]-1H-indole-1-yl)sulfonyl)aniline; 1-(phenylsulfonyl)-4-[(2R)-pyrrolidin-2-ylmethoxy]-1H-indole; 1-(phenylsulfonyl)-5-(pyrrolidin-2-ylmethoxy)-1H-indole; 1-(phenylsulfonyl)-6-(pyrrolidin-2-ylmethoxy)-1H-indole; the stereoisomers thereof; and the pharmaceutically acceptable salts thereof.
- 8. A pharmaceutical composition which comprises a pharmaceutically acceptable carrier and an effective amount of a compound of formula I whereinW is SO2, CO, CONH, CSNH or (CH2)x; X is O, SOyor NR13; Y is CR14; Z is CR15; m and x are each independently 0 or an integer of 1, 2 or 3; n is an integer of 1, 2 or 3; p is an integer of 1; R1 is halogen, CN, OR16, CO2R17, CONR18R19, CNR20NR21R22, SO2NR23R24, SOwR25, or a C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, cycloheteroalkyl, phenyl or heteroaryl group each optionally substituted; R2, R3, R5, R6, R7, R8, R9, R10 and R11 are each independently H or an optionally substituted C1-C6alkyl group; R4 is H, CNR26NR27R28 or a C1-C8alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, cycloheteroalkyl, aryl or heteroaryl group each optionally substituted; R12 is an optionally substituted C1-C6alkyl, aryl or heteroaryl group; y and w are each 0 or an integer of 1 or 2; R13 is H or a C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, cycloheteroalkyl, aryl or heteroaryl group each optionally substituted; R14 and R15 are each independently H, halogen or a C1-C6alkyl, aryl, heteroaryl or C1-C6alkoxy group each optionally substituted; R16 is H, COR29 or a C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, aryl or heteroaryl group each optionally substituted; R17 and R29 are each independently H or a C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, cycloheteroalkyl, aryl or heteroaryl group each optionally substituted; R18, R19, R20, R21, R22, R26, R27 and R28 are each independently H or an optionally substituted C1-C6alkyl group; R23 and R24 are each independently H or a C1-C6alkyl, aryl or heteroaryl group each optionally substituted; and R25 is an optionally substituted C1-C6alkyl, aryl, or heteroaryl group; or the stereoisomers thereof or the pharmaceutically acceptable salts thereof.
- 9. The composition according to claim 8 having a formula I compound wherein W is SO2.
- 10. The composition according to claim 9 having a formula I wherein X is O.
- 11. The composition according to claim 9 having a formula I compound wherein n is 1.
- 12. The composition according to claim 11 having a formula I compound selected from the group consisting of:1-(phenylsulfonyl)-4-[(2S)-pyrrolidin-2-ylmethoxy]-1H-indole; 1-[(5-chlorothien-2-yl)sulfonyl]-4-[(2S)-pyrrolidin-2-ylmethoxy]-1H-indole; 1-[(2-fluorophenyl)sulfonyl)-4-[(2S)-pyrrolidin-2-ylmethoxy]-1H-indole; 1-[(3-fluorophenyl)sulfonyl)-4-[(2S)-pyrrolidin-2-ylmethoxy]-1H-indole; 1-[(4-fluorophenyl)sulfonyl)-4-[(2S)-pyrrolidin-2-ylmethoxy]-1H-indole; 1-[(3,4-dimethoxyphenyl)sulfonyl)-4-[(2S)-pyrrolidin-2-ylmethoxy]-1H-indole; 4-({4-[2S)-pyrrolidin-2-ylmethoxyl-1H-indole-1-yl}sulfonyl)aniline; 1-(phenylsulfonyl)-4-[(2R)-pyrrolidin-2-ylmethoxy]-1H-indole; 1-(phenylsulfonyl)-5-(pyrrolidin-2-ylmethoxy)-1H-indole; 1-(phenylsulfonyl)-6-(pyrrolidin-2-ylmethoxy)-1H-indole; the stereoisomers thereof; and the pharmaceutically acceptable salts thereof.
Parent Case Info
This application claims priority from copending application Ser. No. 60/285,644, filed on Apr. 20, 2001, the entire disclosure of which is hereby incorporated by reference.
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Number |
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US |