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filingDate 2013-01-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d037b5455dae2e277607eb27a6487e26
publicationDate 2014-09-24-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-089853-A1
titleOfInvention OXADIAZOL INHIBITORS FROM THE PRODUCTION OF LEUCOTRIENS FOR COMBINATION THERAPY, PHARMACEUTICAL COMPOSITION, USE
abstract Claim 1: A combination characterized in that it comprises a compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein: each of R¹ and R² is independently hydrogen, C₁₋₇ alkyl or C₃₋₁₀ carbocycle, with the condition that R¹ and R² are not both hydrogen; R³ is a 5-11 membered heteroaryl ring containing one to three heteroatoms selected from nitrogen, oxygen and sulfur, where the heteroaryl ring is optionally independently substituted with one to three groups selected from C₁₋₅ alkyl optionally substituted with one at three halogen atoms, C₁₋₅ alkoxy, C₁₋₃ hydroxy, halogen, hydroxy, -O-benzyl, oxo, cyano, amino, -NH-C carbo carbocycle, C₁₋₆ alkylamino and C₁₋₃ dialkylamino; R⁴ is hydrogen, C₁₋₃ alkyl, halogen or nitrile; R⁵ is C₁₋₆ alkyl, C₃₋₁₀ carbocycle, 3-11 membered heterocycle, aryl, 5-11 membered heteroaryl, -C (O) -R⁶, hydroxy or -NR⁷R⁸, where each R⁵ is optionally independently substituted with one to three groups selected from R⁹, R¹⁰ and R¹¹; R⁶ is 5-6 membered C₃₋₈ or -NH-heterocycle, each optionally substituted independently with one to three groups selected from R⁹, R¹⁰ and R¹¹; each of R⁷ and R⁸ is independently hydrogen, 5-6 membered heterocycle optionally substituted with C₁₋₆ alkyl, C carbo carbocycle optionally substituted with hydroxy or C₁₋₆ alkyl; R⁹, R¹⁰ and R¹¹ are independently selected from (a) -H, (b) -OH, (c) halogen, (d) -CN, (e) -CF₃, (f) C₁₋₆ alkyl optionally substituted with each other three -OH, -N (R¹²) (R¹³), 3-6 membered heterocycle, C₁₋₆ alkoxy, C₁₋₆-O-C₁₋₆ alkoxy, -CO₂R¹², -C (O) N (R¹²) ( R¹³) or -S (O) ₙ-C₁₋₆ alkyl, (g) C₁₋₆ alkoxy, (h) -N (R¹²) (R¹³), (i) -S (O) ₙ-C₁₋₆ alkyl, (j) -CO₂R¹², (k) -C (O) N (R¹²) (R¹³), (l) -S (O) ₂N (R¹²) (R¹³), (m) a 3-10 membered heterocyclic group optionally substituted with one to three C₁₋₆ alkyl groups, (n) oxo, (o) -C (O) -C₁₋₃ alkyl; each of R¹² and R¹³ is independently selected from -H, -C₁₋₆ alkyl, C₍O₎ₐₗqᵘⁱₗₒ C₁₋₆, and a 3-6 membered heterocyclic group, each of which is optionally independently substituted with each other. three C₁₋₆ alkyl groups, -OH, C₁₋₆ alkoxy, -C (O) N (R¹⁴) (R¹⁵), -S (O) ₙ-C₁₋₆ alkyl, CN, a 3-6 membered heterocyclic group , -O-C₁₋₆ alkyl, CF₃, or; R¹² and R¹³ taken together with the nitrogen ring to which they are attached form a heterocyclyl ring optionally substituted with one to three -OH, CN, -O-C₁₋₆ alkyl or oxo; each of R¹⁴ and R¹⁵ is independently selected from -H and C₁₋₆ alkyl; n is 0, 1 or 2; and an additional pharmaceutically active agent for use in a method of treating cardiovascular disease. Claim 16: The combination according to any one of claims 1 or 13, characterized in that it further comprises more than one additional pharmaceutically active agent selected from a group consisting of statins, HMG-CoA reductase inhibitors, transfer protein inhibitors or antagonists of cholesterol ester (CETP), fibrates, niacin derivatives, Lp-PLA2 inhibitors, antiplatelet and anticoagulants.
priorityDate 2012-02-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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