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US 7,019,001 B2Granted
Substituted benzothiazole amide derivatives
AssigneeHoffman-La Roche Inc.
InventorsAlexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Abstract
A compound of formula I and a method of treatment of diseases, related to modulation of the adenosine A2 receptor system comprising administering a compound of formula to a person in need of such treatment.
Claims9
A compound of formula
- wherein
- R is lower alkoxy or halogen;
- R11 and R21, together with the N atom to which they are attached, form a heterocyclic ring, said heterocyclic ring being unsubstituted or substituted by lower alkyl, selected from the group consisting of
- 2-oxa-5-aza-bicyclo[2.2.1]heptane,
- 3-endo-hydroxy-8-aza-bicyclo[3.2.1]octane,
- 2-aza-bicyclo[2.2.2]octane,
- 1-oxo-2,8-diaza-spiro[4.5]decane,
- 3-aza-spiro[5.5]undecane,
- 8-aza-spiro[4.5]decane,
- 1-oxa-8-aza-spiro[4.5]decane,
- 1,8,8-trimethyl-3-aza-bicyclo[3.2.1]octane,
- [1,4]oxazepane,
- 2-oxa-5-aza-bicyclo[2.2.2]octane,
- 8-oxa-3-aza-bicyclo[3.2.1]octane,
- 1,4-diaza-bicyclo[3.2.1]octane,
- 2-aza-bicyclo[2.2.1]heptane and
- 3-aza-bicyclo[3.2.1]octane, or
- piperidin-1-yl, substituted by a substituent selected from the group —(CH2)n—NR′S(O)2-lower alkyl, —C(O)NR′2 and —(CH2)n-phenyl, said phenyl ring being unsubstituted or substituted by lower alkyl, and R′ being independently selected from hydrogen and lower alkyl;
- X is —CH2—;
- and
- n is 0, 1, 2, 3 or 4;
- or a pharmaceutically acceptable acid addition salt thereof.
19 more elements
A compound of formula
- wherein
- R is lower alkoxy or halogen;
- R12 is lower alkyl and
- R22 is cycloalkyl, substituted by one or two substituents, selected from the group consisting of halogen, lower alkoxy or hydroxy;
- and
- X is —O— or CH2—;
- or a pharmaceutically acceptable acid addition salt thereof.
4 more elements
A process for preparing a compound of formula IB comprising reaction of a compound of formula
- with phenyl chloroformate and then with a compound of formula
- HNR12R22 (3B)
- forming a compound of formula
- wherein R is lower alkoxy or halogen;
- X is —O— or CH2—;
- R12 is alkyl;
- and
- R22 is cycloalkyl, substituted by one or two substituents selected from the group consisting of halogen, lower alkoxy and hydroxy.
5 more elements
Dependencies are inferred from the claim text.