ANTIPICORNAVIRAL PYRIDAZINAMINES

• Main Authors: STOKBROEKX, RAYMOND ANTOINE, LUYCKX, MARCEL GEREBERMUS MARIA, GRAUWELS, GILBERT ARTHUR JULES, VAN, DER EYCKEN CYRIEL ALPHONS MARIA
• Format: Patent
• Language: English; Korean
• Published: 01.05.1999
• Edition: 6
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

본 발명은 항피코르나바이러스 활성을 갖는 하기 일반식(I)의 피페리딘일, 피롤리딘일, 아제핀일 및 피페라진일 피리다진, 이의 부가염 및 입체 화학적 이성체 형태; 이들의 제조방법; 이들을 함유하는 약학적 조성물에 관한 것이며, 본 화합물은 바이러스성 질환을 치료하는데 유용하다. 상기식에서, X는 CH 또는 N 이고; R은 수소, 알킬, 할로, 하이드록시, 트리플루오로메틸, 시아노, 알킬옥시, 알킬티오, 알킬술피닐, 알킬술포닐, 알킬옥시카르보닐, 알킬카르보닐 또는 아릴이고; R및 R는 각각 수소 또는 알킬이고; Alk 는 알칸디일이고; R및 R는 각각 수소, 알킬 또는 할로이고; Het 는 을 나타낸다. Piperidinyl, pyrrolidinyl, azepinyl and piperazinyl pyridazines of formula wherein X represents CH or N; R represents hydrogen, C1-4alkyl, halo, hydroxy, trifluoromethyl, cyano, C1-4alkyloxy, C1-4alkylthio, C1-4alkylsulfinyl, C1-4alkylsulfonyl, C1-4alkyloxycarbonyl, C1-4alkylcarbonyl or aryl; R and R represent hydrogen or C1-4alkyl; Alk represents C1-4alkanediyl; R and R represent hydrogen, C1-4alkyl or halo; and Het represents the addition salts and stereochemically isomeric forms thereof, said compounds having antipicornaviral activity. Pharmaceutical compositions containing these compounds as active ingredient, and methods of preparing said compounds and pharmaceutical compositions.