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US 2009/0023763 A1Published application
Condensed Pyridine Derivatives Useful as A2B Adenosine Receptor Antagonists
OwnerBernat Vidal Juan, Paul Robert Eastwood +1inventors
InventorsBernat Vidal Juan, Paul Robert Eastwood, Jacob Gonzalez Rodriguez
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Abstract
New antagonists of the A2B adenosine receptor represented by formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as antagonists of the A2B adenosine receptor.
Claims28
A method for treating a subject afflicted with a pathological condition or disease susceptible to amelioration by antagonism of the A2B adenosine receptor comprising administering to said subject an effective amount of a compound of formula (I)
- wherein:
- A represents an optionally substituted monocyclic or polycyclic aryl or heteroaryl group,
- B represents an optionally substituted monocyclic nitrogen-containing heterocyclic group,
- and either
- a) R1 represents a hydrogen atom and R2 represents a group chosen from —NH2 and optionally substituted alkynyl groups
- or
- b) R2, R1 and the —NH— group to which R1 is attached form a moiety chosen from the moieties of formulae (IIa), (IIb), (IIc), (IId) and (IIe):
- wherein:
- Ra is a group chosen from a hydrogen atom, halogen atoms and groups chosen from optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, —OR3, —SR3, —COOR3, —CONR3R4, —NR3R4, —NR3COR4 and —CN groups wherein R3 and R4 are independently chosen from a hydrogen atom and lower alkyl groups or cycloalkyl groups, and
- Rb is a group chosen from a hydrogen atom and groups chosen from optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl and optionally substituted heteroaryl groups.
7 more elements
A compound of formula (I)
- wherein:
- A represents an optionally substituted monocyclic or polycyclic aryl or heteroaryl group,
- B represents an optionally substituted monocyclic nitrogen-containing heterocyclic group,
- and either
- a) R1 represents a hydrogen atom and R2 represents a group chosen from —NH2 and optionally substituted alkynyl groups,
- or
- b) R2, R1 and the —NH— group to which R1 is attached, form a moiety chosen from the moieties of formulae (IIa), (IIb), (IIc) and (IId):
- wherein:
- Ra is a group chosen from a hydrogen atom, halogen atoms and groups chosen from optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, —OR3, —SR3, —COOR3, —CONR3R4, —NR3R4, —NR3COR4 and —CN groups, wherein R3 and R4 are independently chosen from a hydrogen atoms and lower alkyl groups or cycloalkyl groups, and
- Rb is a group chosen from a hydrogen atom and groups chosen from optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl and optionally substituted heteroaryl groups.
7 more elements
Dependencies are inferred from the claim text.