2-amino-3-aroyl-4,5 alkylthiophenes: agonist allosteric enhancers at human A1 adenosine receptors
OwnerJoel M. Linden, Ray A. Ollson +1inventors
InventorsJoel M. Linden, Ray A. Ollson, Peter J. Scammells
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Abstract
The present invention relates to a compound of formula (I): wherein: R3 is selected from the group consisting of 1-napthyl, 2-napthyl and cycloalkylphenyl; and R4 and R5 taken together form a ring having from 5 to 10 carbon atoms. Additionally, the invention provides a therapeutic method for preventing or treating a pathological condition or symptom in a mammal subject, such as a human, wherein increased angiogenesis is desired, comprising administering to a mammal in need of such therapy an effective amount of the aforementioned thiophene selective adenosine A1 allosteric enhancer.
Claims5
A pharmaceutical formulation comprising a compound of the formula (I):
- wherein:
- R3 is cycloalkylphenyl;
- and
- R4 and R5 are taken together to form a ring having 5 to 10 carbon atoms.
A pharmaceutical formulation comprising a compound of the formula (I):
- wherein:
- R3 is selected from the group consisting of 1-napthyl, 2-napthyl and cycloalkylphenyl;
- and
- R4 and R5 are taken together to form a ring having 5 to 10 carbon atoms, wherein said 1-napthyl and 2-napthyl are substituted with one or more (C1–C6)alkyl groups, (C2–C6)alkenyl groups, (C1–C6)alkanoyl groups, (C1–C6)alkanoyloxy groups, (C3–C6)cycloalkyl groups, (C3–C6)cycloalkenyl groups, halo(C1–C6)alkyl groups, (C1–C6)alkoxy groups, (C1–C6)alkoxycarbonyl groups, (C3–C6)cycloalkyl(C1–C6)alkyl groups, (C2–C6)alkynyl groups or halogens.
Dependencies are inferred from the claim text.