N-substituted-2-pyridylindoles

C - Chemistry – Metallurgy – 07 – D

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260/280.3, 260/2

C07D 401/00 (2006.01) C07D 401/04 (2006.01) C07D 401/14 (2006.01) C07D 491/04 (2006.01) C07D 491/056 (2006.01)

Patent

CA 1197249

Abstract of the Disclosure N-Substituted-2-Pyridylindoles The invention concerns thromboxan synthetase inhibitors of the formula I Image (I) wherein R1 represents hydrogen or lower alkyl; Ar represents pyridyl unsubstituted or substituted by lower alkyl, carboxy, lower alkoxy- carbonyl or carbamoyl; R2 and R3 independently represent hydrogen, lower alkyl, halogen, trifluoromethyl, hydroxy, lower alkoxy, carboxy lower alkyl, lower alkoxycarbonyl lower alkyl, carboxy, lower alkoxycarbonyl, or lower alkyl-(thio, sulfinyl or sulfonyl), or R2 and R3 together on adjacent carbon atoms represent lower alkylene- dioxy; A represents alkylene of 1 to 12 carbon atoms, alkenylene of 2 to 12 carbon atoms, alkynylene of 2 to 12 carbon atoms, lower alkylenephenylene lower alkylene, lower alkylenephenylene, phenylene lower alkylene, phenylene, a direct bond, lower alkylene-(thio or oxy)-lower alkylene,(thio or oxy)-phenylene, lower alkylene-(thio or oxy)-phenylene, phenylene-(thio or oxy)-lower alkylene or phenylene lower alkenylene; B represents carboxy, lower alkoxy- carbonyl, carbamoyl, mono- or di-lower alkylcarbamoyl, hydroxymethyl, hydroxycarbamoyl, 5-tetrazolyl or formyl; the N-oxides and salts thereof. They are prepared, for example, by ring closing a compound of the formula Image

415716

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