7-phenyl-benzo [b] thiophen amide derivatives
AssigneeHoffmann-La Roche Inc.
InventorsAlexander Alanine, Alexander Flohr
Life of this patent
Estimating the term…
Abstract
A compound of the formula 1 Compounds of formula I have a good affinity to the A2A receptor and are useful for the treatment of diseases mediated by this receptor.
Claims16
A compound of the formula
- 9
- wherein
- R is selected from the group phenyl, phenyl substituted by halogen, pyridin 3-or 4-yl, pyridin 3- or 4-yl substituted by lower alkyl and —NR1R2, wherein R1 and R2, together with the N atom to which they are attached, form heterocyclic rings, selected from the group consisting of
- morpholinyl, thiomorpholinyl, piperidinyl and piperazinyl, said heterocyclic rings being unsubstituted or substituted by —(CH2)n-hydroxy, lower alkyl or lower alkoxy;
- and
- n is 0, 1 or 2;
- or a pharmaceutically acceptable acid addition salt thereof.
A process for preparing a compound of formula IA comprising
- a) reacting a compound of formula
- 10
- with a compound of formula
- RC(O)Cl (3)
- forming a compound of formula
- 11
- wherein R is phenyl, phenyl substituted by halogen, pyridin 3-or 4-yl, or pyridin 3-or 4-yl substituted by lower alkyl.
A process for preparing a compound of formula IB comprising
- a) reacting a compound of formula
- 12
- with a compound of formula HNR1R2
- forming a compound of formula
- 13
- wherein R1 and R2, together with the N atom to which they are attached, form heterocyclic rings, selected from the group consisting of morpholinyl, thiomorpholinyl, piperidinyl and piperazinyl, said heterocylic rings being unsubstituted or substituted by —(CH2)n-hydroxy, lower alkyl or lower alkoxy.
A method for the treatment of a disease mediated by the adenosine receptor comprising administering a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof to a person in need of such treatment.
A method for the treatment of diseases related to the adenosine A2A receptor comprising administering a therapeutically effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof to a person in need of such treatment.
Dependencies are inferred from the claim text.