| 摘要 |
The present invention relates to azetidine amide derivatives derivatives of formula (I);
wherein rings A1 A2 and A3 are as described in the description, to pharmaceutically acceptable salts thereof, to their preparation, to pharmaceutical compositions containing one or more compounds of formula (I), and to their use as pharmaceuticals, especially to their use as orexin receptor antagonists. |
| 主权项 |
1. A compound of formula (I) wherein the carbon atom at position 2 of the azetidine ring is in absolute (S)-configuration; ring A3 represents a meta di-substituted 5-membered heteroarylene ring containing one, two or three heteroatoms; wherein at least one of said heteroatoms is nitrogen, and the remaining is/are independently selected from oxygen, sulfur and nitrogen; ring A2 represents phenyl or 6-membered heteroaryl; wherein said phenyl or 6-membered heteroaryl is independently unsubstituted, or mono-, di-, or tri-substituted; wherein the substituents are independently selected from (C1-4)alkyl, (C1-4)alkoxy, halogen, (C1-3)fluoroalkyl, (C1-3)fluoroalkoxy, and (C3-6)cycloalkyl-oxy-; ring A1 represents phenyl or 5- or 6-membered heteroaryl, wherein said phenyl or 5- or 6-membered heteroaryl independently is mono-, di-, or tri-substituted; wherein
one of said substituents is attached in ortho-position to the point of attachment of A1 to the rest of the molecule; wherein said substituent is phenyl or 5- or 6-membered heteroaryl; wherein said phenyl or 5- or 6-membered heteroaryl substituent is independently unsubstituted, mono-, di-, or tri-substituted, wherein the substituents are independently selected from (C1-4)alkyl, (C1-4)alkoxy, halogen, (C1-3)fluoroalkyl, and (C1-3)fluoroalkoxy;and the other of said substituents, if present, is/are independently selected from (C1-4)alkyl, (C1-4)alkoxy, halogen, (C1-3)fluoroalkyl, (C1-3)fluoroalkoxy and dimethylamino; or a pharmaceutically acceptable salt thereof. |
