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US 11,858,876 B2Granted
CCL2 inhibitors
AssigneeLapko Inc
InventorsBruce Kovacs, Kamron Shahbahrami, George Nicola
Life of this patent
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Abstract
Compounds, pharmaceutically acceptable salts, and pharmaceutical compositions thereof are disclosed that are useful for inhibition of the biological activity of CCL2, as well as methods of treatment for diseases involving the biological activity of CCL2.
Claims8
A compound according to Formula 1 below:
- wherein
- X is 1-3;
- Y is 1-3;
- R1 is methyl, ethyl, propyl, butyl, or haloalkyl;
- R2 and R2′ are independently selected from methyl, propyl, butyl, alkoxy, haloalkyl, and hydrogen or R2 and R2′ may be fused into a heterocyclic ring with 5 or 6 members;
- R3 is methyl, ethyl, alkoxy, carboxylic acid, or haloalkyl;
- and
- R4 is hydrogen, hydroxyl or halogen,
- or a pharmaceutically acceptable salt, addition compound or pro-drug thereof.
6 more elements
A pharmaceutical combination comprising a therapeutically effective amount of a composition comprising:
- (a) a first compound according to Formula 1 below
- wherein
- X is 1;
- Y is 1-3;
- R1 is methyl, ethyl, CHF2, or CF3;
- R2 and R2′ are independently selected from methyl, ethyl, n-propyl, 2-propyl, tert-butyl, alkoxy and hydrogen;
- R3 is methyl, ethyl, hydroxyl, carboxylic acid, alkoxy, haloalkyl, or hydrogen;
- and
- R4 is hydrogen, hydroxyl or halogen,
- or a pharmaceutically acceptable salt, addition compound or pro-drug thereof;
- and
- (b) a second compound selected from the group consisting of Non-steroidal anti-inflammatory drugs, Immunomodulatory agents, Anti-malarials, Antibiotics, Anti-TNF alpha agents, Anti-CD20 agents, Anti-diarrheal drugs, Antidepressants, Anti-psychotics, Anti-fungals, Anti-helminthics, T lymphocyte activation inhibitors, Anti-IL-1 agents, Glucocorticoids, Anti-cytokine/chemokine monoclonal antibodies, Sex steroids and receptor modulators, Anti-cellular surface receptor monoclonal antibodies, Aminosalicylic acid derivatives, Anticholinergic agents, Adrenergic agonists, Corticosteroids, Anti-neoplastic chemotherapeutic agents, Phosphodiesterase inhibitors, Leukotriene pathway modulators, Monoclonal antibodies directed against human immunoglobulins, Adrenergic antagonists, Calcium channel antagonists, Dopamine agonists, Serotonin agonists, Dopamine antagonists, Serotonin antagonists, Monoamine reuptake inhibitors, Protease inhibitors, Histamine antagonists, Proton pump inhibitors, and HMG-CoA reductase inhibitors.
9 more elements
Dependencies are inferred from the claim text.