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.
Claims23
A compound of the formula (I):
- wherein:
- R3 is a cycloalkylphenyl;
- and
- R4 and R5 are taken together to form a ring having 5 to 10 carbon atoms.
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.
A method for enhancing adenosine A1 receptors in a mammal, including a human, by administering to said mammal an effective amount of a compound of 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 ring atoms.
A method for promoting angiogenesis in a mammal, including a human, by administering to said mammal an effective amount of a compound of 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 about 5 to about 10 ring atoms.
A method of treating ischemic disease in a mammal, including a human, by administering to said mammal an effective amount of a compound of formula (I):
- wherein:
- R3 is selected from the group consisting of 1-napthyl, 2-napthyl and cycloalkylphenyl;
- and
- R4 and R5 are taken together form a ring having about 5 to about 10 ring atoms.
Dependencies are inferred from the claim text.