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US 2006/0148850 A1Published application
4-{'3-(Sulfonylamino) phenyl!'1-(cyclymethyl) piperidin-4-ylidene! methyl}benazmide derivativess as delta opioid receptor ligands for the treatment of pain, anxiety and functional gastrointestinal disorder
AssigneeAstraZeneca AB
InventorsWilliam Brown, Andrew Griffin, Christopher Walpole
Life of this patent
Estimating the term…
Abstract
Compounds of general formula: (I) wherein R1, R2, R3, R4 and R5 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
Claims19
A compound of formula I, a pharmaceutically acceptable salt thereof, diastereomers, enantiomers, or mixtures thereof:
- wherein
- R1 is selected from C6-10aryl and C2-6heteroaryl, wherein said C6-10aryl and C2-6heteroaryl are optionally substituted with one or more groups selected from —R, —NO2, —OR, —Cl, —Br, —I, —F, —CF3, —C(═O)R, —C(═O)OH, —NH2, —SH, —NHR, —NR2, —SR, —SO3H, —SO2R, —S(═O)R, —CN, —OH, —C(═O)OR, —C(═O)NR2, —NRC(═O)R, and —NRC(═O)—OR, wherein R is, independently, a hydrogen or C1-6alkyl;
- and
- R2, R3, R4 and R5 are, independently, selected from hydrogen, C1-6alkyl, and C3-6cycloalkyl, wherein said C1-6alkyl and C3-6cycloalkyl are optionally substituted with one or more groups selected from —R, —NO2, —OR, —Cl, —Br, —I, —F, —CF3, —C(═O)R, —C(═O)OH, —NH2, —SH, —NHR, —NR2, —SR, —SO3H, —SO2R, —S(═O)R, —CN, —OH, —C(═O)OR, —C(═O)NR2, —NRC(═O)R, and —NRC(═O)—OR, wherein R is, independently, a hydrogen or C1-6alkyl.
1 more element
(canceled)
A process for preparing a compound of formula I, comprising:
- reacting a compound of formula II with X—S(═O)2—R4 or R4S(═O)2—O—S(═O)2R4.
- wherein
- X is selected from Cl, Br and I;
- R1 is selected from C6-10aryl and C2-6heteroaryl, wherein said C6-10aryl and C2-6heteroaryl are optionally substituted with one or more groups selected from —R, —NO2, —OR, —Cl, —Br, —I, —F, —CF3, —C(═O)R, —C(═O)OH, —NH2, —SH, —NHR, —NR2, —SR, —SO3H, —SO2R, —S(═O)R, —CN, —OH, —C(═O)OR, —C(═O)NR2 —NRC(═O)R, and —NRC(═O)—OR, wherein R is, independently, a hydrogen or C1-6alkyl;
- and
- R2, R3, R4 and R5 are, independently, selected from hydrogen, C1-6alkyl, and C3-6cycloalkyl, wherein said C1-6alkyl and C3-6cycloalkyl are optionally substituted with one or more groups selected from —R, —NO2, —OR, —Cl, —Br, —I, —F, —CF3, —C(═O)R, —C(═O)OH, —NH2, —SH, —NHR, —NR2, —SR, —SO3H, —SO2R, —S(═O)R, —CN, —OH, —C(═O)OR, —C(═O)NR2, —NRC(═O)R, and —NRC(═O)—OR, wherein R is, independently, a hydrogen or C1-6alkyl.
3 more elements
Dependencies are inferred from the claim text.