Anthranilic acid derivatives and their use as activators of the hm74a receptor
AssigneeSmithKline Beecham Corporation
InventorsMatthew Campbell, Richard Hatley, Jag Heer, Andrew Mason, Ivan Pinto, Shahzad Rahman, Ian Smith
Life of this patent
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Abstract
Therapeutically active anthranilic acid derivatives of Formula (I), processes for the preparation of said derivatives, pharmaceutical formulations containing the compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.
Claims28
A compound selected from a compound of Formula (I):
- or a salt, solvate or physiologically functional derivative thereof, wherein:
- R1 is hydrogen, halogen or C1-C3alkyl;
- R2 is a 9 or 10-member saturated, partially saturated or unsaturated bi-cyclic ring system optionally including from 1 to 3 heteroatoms independently selected from S, O and N;
- Z is —(CH2)n—, —CH═CH—(CH2)m—, —(CH2)pNHC(O)—, —(CH2)pNHC(O)NH—, —(CH2)pNHC(O)O—, —(CH2)pSO2NR3—, —(CH2)pNR3SO2—, —(CH2)pO— or —O—;
- n is 2, 3 or 4;
- m is 0, 1 or 2;
- p is 1 or 2;
- and
- R3 represents hydrogen or C1-C4alkyl, with the proviso that when R1 is H, Z is —(CH2)n— and n is 2 or 3, R2 is other than indol-3-yl.
20-26. (canceled)
A method for the treatment of a human or animal subject having a condition where under-activation of the HM74A receptor contributes to the condition or where activation of the receptor will be beneficial, which method comprises administering to said human or animal subject an effective amount of a compound of Formula (Ia):
- or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof, wherein:
- R1 is hydrogen, halogen or C1-C3alkyl;
- R2 is a 9 or 10-member saturated, partially saturated or unsaturated bi-cyclic ring system optionally including from 1 to 3 heteroatoms independently selected from S, O and N;
- Z is —(CH2)n—, —CH═CH—(CH2)m—, —(CH2)pNHC(O)—, —(CH2)pNHC(O)NH—, —(CH2)pNHC(O)O—, —(CH2)pSO2NR3—, —(CH2)pNR3SO2—;
- or —O—;
- n is 2, 3 or 4;
- m is 0, 1 or 2;
- p is 1 or 2;
- and
- R3 is hydrogen or C1-C4alkyl.
A method for the treatment of a human or animal subject having a disorder of lipid metabolism or having an inflammatory disease, which method comprises administering to said human or animal subject an effective amount of a compound of Formula (Ia):
- or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof, wherein:
- R1 is hydrogen, halogen or C1-C3alkyl;
- R2 is a 9 or 10-member saturated, partially saturated or unsaturated bi-cyclic ring system optionally including from 1 to 3 heteroatoms independently selected from S, O and N;
- Z is —(CH2)n—, —CH═CH—(CH2)m—, —(CH2)pNHC(O)—, —(CH2)pNHC(O)NH—, —(CH2)pNHC(O)O—, —(CH2)pSO2NR3—, —(CH2)pNR3SO2—;
- or —O—;
- n is 2, 3 or 4;
- m is 0, 1 or 2;
- p is 1 or 2;
- and
- R3 is hydrogen or C1-C4alkyl.
Dependencies are inferred from the claim text.