Thiazolylbenzofuran derivatives, processes for the...

C - Chemistry – Metallurgy – 07 – D

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C07D 417/04 (2006.01) A61K 31/425 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/55 (2006.01) C07D 417/14 (2006.01) C07D 513/04 (2006.01)

Patent

CA 2076192

ABSTRACT OF THE DISCLOSURE There are described compounds of the formula: Image (I) wherein R1 is lower alkyl optionally susbstituted with halogen, lower alklyamino or lower alkyl(acyl)a- mino; cyclo(lower)alkyl; tricycloalkyl; aryl optionally substituted with lower alkoxy; or a heterocyclic group; R2 is hydrogen or halogen or R1 and R2 are taken together with the adjacent atoms to form cycloalken ring or an N-containing heterocyclic group optionally substituted with acyl, R3 is hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy, R4 is hydrogen; acyl, cyano, aryl optionally substituted with hydroxy(lower)alkyl, halo(lower)a- lkyl, cyano(lower)alkyl, heterocyclic(lower)alkyl or acyl; or lower alkyl which may be substituted with substituent(s) selected from the group consisting of halogen, cyano, hydroxy, lower alkylsulfonyloxy, arylsulfonyloxy, acyl, acyl(lower)alkylthio and aryl optionally substituted with halo(lower)alkyl, cyano(lower)alkyl, heterocyclic(lower)alkyl, cyano, acyl, acyl(lower)alkyl, a heterocyclic group or (lower alkylsulfinyl) (lower alkylthio)lower alkenyl; A is lower alkylene, lower alkenylene or a single bond, X is a single bond, O or S, and Y is O or S, provided that A is lower alkylene or lower alkenyle- ne, or X is O or S when R1 is lower alkyl or aryl and R2 is hydrogen, and pharmaceutically acceptable salts thereof. The preparation of these compounds, pharmaceutical compositions containing them and their use for the therapeutic treatment and/or prevention of allergy or inflammation are also disclosed. These compounds are particularly useful for the prevention and/or treatment of asthma, psoriasis, hepatitis, bronchitis, gastritis, esophagitis, pancreatitis, arthritis, nephritis, inflammatory bowel disease, shock (e.g. septic shock, anaphylactic shock), arteriosclerosis, myocardial infarction, cerebral vasospasm, rhinitis, conjunctivitis, eczema, ischemic cerebral disease, chronic obstructive lung disease, cerebral edema, adult respiratory distress syndrome, neonatal pulmonary hypertension, Chrohn's diseases, dermatitis, rheumatism, gastric ulcer, peptic ulcer, gout and the like.

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