Nicotinamide acids, amides, and their mimetics active as...

Details Nicotinamide acids, amides, and their mimetics active as... Nicotinamide acids, amides, and their mimetics active as...

C - Chemistry, Metallurgy

07

D

C07D 213/82 (2006.01) A61P 11/06 (2006.01) C07D 401/12 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01) C07D 413/12 (2006.01)

Patent

CA 2369462

Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: Image wherein j is 0 or 1, k is 0 or 1, m is 0, 1, or 2; n is 1 or 2; A is selected from the partial Formulas: <IMGs> where q is 1, 2, or 3, W3 is -O-; -N(R9)-; or -OC(=O)-; R7 is selected from - H; -(C1-C6) alkyl, -(C2-C6) alkenyl, or -(C2-C6) alkynyl substituted by 0 to 3 substituents R10; -(CH2)u-(C3-C7) cycloalkyl where a is 0, 1 or 2, substituted by 0 to 3 R10; and phenyl or benzyl substituted by 0 to 3 R14; R8 is tetrazol-5-yl; 1,2,4-triazol-3-yl; 1,2,4- triazol-3-on-5-yl; 1,2,3- triazol-5-yl; imidazol-2-yl; imidazol-4-yl; imidazolidin-2-on-4-yl; 1,3,4- oxadiazolyl; 1,3,4- oxadiazol-2-on-5-yl; 1,2,4-oxadiazol-3-yl; 1,2,4-oxadiazol-5-on-3-yl; 1,2,4- oxadiazol-5-yl; 1,2,4-oxadiazol-3-on-5-yl; 1,2,5-thiadiazolyl; 1,3,4-thiadiazolyl; morpholinyl; parathiazinyl; oxazolyl; isoxazolyl; thiazolyl; isothiazolyl; pyrrolyl; pyrazolyl; succinimidyl; glutarimidyl; pyrrolidonyl; 2-piperidonyl; 2-pyridonyl; 4-pyridonyl; pyridazin-3-onyl; pyridyl; pyrimidinyl; pyrazinyl; pyridazinyl; indolyl; indolinyl; isoindolinyl; benzo[b]furanyl; 2,3- dihydrobenzofuranyl; 1,3-dihydroisobenzofuranyl; 2H-1-benzopyranyl; 2-H-chromenyl; chromanyl; benzothienyl; 1H-indazolyl; benzimidazolyl; benzoxazolyl; benzisoxazolyl; benzothiazolyl; benzotriazolyl; benzotriazinyl; phthalazinyl; 1,8-naphthyridinyl; quinolinyl; isoquinolinyl; quinazolinyl; quinoxalinyl; pyrazolo[3,4-d]pyrimidinyl; pyrimido[4,5-d]pyrimidinyl; imidazo[1,2-a]pyridinyl; pyridopyridinyl; pteridinyl; or 1H-purinyl; or A is selected from phosphorous and sulfur acid groups; W is -O-; -S(=O)r- , where t is 0, 1, or 2; or -N(R3)-; Y is =(R1a)-, or -(N Image (O)k] where k is 0 or 1; R4, R5 and R6 are (1) -H; provided that R5 and R6 are not both -H at the same time, -F; -Cl; -(C2-C4) alkynyl; -R16; -OR16; -S(=O)p R16; - C(=O)R16, -C(=O)OR16; -OC(=O)R16; -CN; -NO2; -C(=O)NR16R17; -OC(=O)NR16R17; -NR12a C(=O)NR16R17; -NR12a C(=NR12)NR16R17; -NR12a C(=NCN)NR15R16; -NR12a C(=N-NO2)NR15R16; -C(=NR12a)NR15R16; -CH2C(=NR12a)NR16R17; -OC(=NR12a)NR16R17; -OC(=N- NO2)NR15R16; -NR16R17; -CH2NR16R17; -NR12a C(=O)R16; -NR12a C(=O)OR16; =NOR16; -NR12a S(=O)p R17; -S(=O)p NR16R17; and -CH2C(=NR12a)NR16R17; (2) -(C1-C4)alkyl including dimethyl and -(C1-C4)alkoxy substituted with 0 to 3 substituents -F or -Cl; or 0 or 1 substituent (C1-C2) alkoxycarbonyl-, (C1-C2) alkylcarbonyl-, or (C1-C2) alkylcarbonyloxy-; or (3) an aryl or heterocyclic moiety; or (4) R5 and R6 are taken together to form a moiety of partial Formulas (1.3.1) through (1.3.15): <IMGs> or a pharmaceutically acceptable salt thereof.

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