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US 2011/0212968 A1Published application
Phenethylamide derivatives and their heterocyclic analogues
OwnerHamed Aissaoui, Christoph Boss +6inventors
InventorsHamed Aissaoui, Christoph Boss, Christine Brotschi, Ralf Koberstein, Romain Siegrist, Thierry Sifferlen, Daniel Trachsel, Jodi T. Williams
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Abstract
The invention relates to novel phenethylamide derivatives and their wherein A, B, R1, R2 and R3 are as described in the application, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
Claims18
A compound of formula (I)
- wherein
- R1 represents hydrogen, hydroxy or (C3-6)cycloalkyl-amino;
- R2 represents hydrogen or (C1-4)alkyl;
- R3 represents (C3-6)cycloalkyl or (C3-6)cycloalkyl-(C1-4)alkyl;
- or a (C1-4)alkyl-group, which group is unsubstituted or monosubstituted with (C1-4)alkoxy, hydroxy, NR4R5, C(O)NR4R5 or COOR6;
- or a (C1-4)fluoroalkyl-group;
- R4 represents hydrogen or (C1-4)alkyl;
- R5 represents hydrogen or (C1-4)alkyl;
- R6 represents (C1-4)alkyl;
- A represents aryl or heterocyclyl, wherein the aryl or heterocyclyl is independently unsubstituted or mono-, di-, or tri-substituted, wherein the substituents are indepen-dently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, (C1-4)alkylthio, hydroxy, amino, halogen, (C1-4)fluoroalkyl, and (C1-4)fluoroalkoxy;
- or A represents a benzo[1,3]dioxolyl- or a 2,3-dihydro-benzo[1,4]dioxinyl-group wherein said groups are unsubstituted, mono- or di-substituted with halogen;
- or A represents a 5H-[1,3]dioxolo[4,5-f]indole group;
- B represents a group selected from
- wherein
- X represents hydrogen, (C1-4)alkyl, (C3-6)cycloalkyl, (C1-4)alkoxy, R4R5N—CH2—, NR4R5, or halogen;
- Y represents hydrogen or (C1-4)alkyl;
- D represents aryl, wherein the aryl is unsubstituted or mono-, di-, or tri-substituted, wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, hydroxy-(C1-4)alkyl, (C1-2)alkoxy-(C1-4)alkoxy, halogen, (C1-4)fluoroalkyl, NMe2, (C1-4)alkyl-C(O)NH— and cyano;
- or D represents heterocyclyl, wherein the heterocyclyl is unsubstituted or mono- or di-substituted, wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, hydroxy-(C1-4)alkyl, halogen, and (C1-4)alkyl-thio;
- with the proviso that A represents an optionally mono- or disubstituted indol-3-yl group, wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy and halogen, if B represents a group of formula
- in a free or a pharmaceutically acceptable salt form.
17 more elements
(canceled)
A method the treatment or prophylaxis of a disease or disorder selected from the group consisting of:
- sleep disorders;
- stress related syndromes;
- psychoactive substance use, abuse, seeking, and reinstatement;
- cognitive dysfunctions in the healthy population;
- psychiatric and neurologic disorders;
- eating disorders;
- and drinking disorders.
4 more elements
(canceled)
Dependencies are inferred from the claim text.