이미다조[4,5-d]피리다진의 유도체, 이의 제법 및 이의 치료적 응용
본 발명은 R1이 H, (C1-C6)알킬-; 히드록시-(C1-C6)알킬-; NH2-(C1-C6)알킬-; NH-(C1-C6)알킬-(C1-C6)알킬-; N((C1-C6)알킬)2-(C1-C6)알킬-; (C2-C6)알케닐-; (C2-C6)알키닐-; 페닐(C1-C6)알킬-; (C3-C10)시클로알킬(C1-C6)알킬-; (C3-C10)원 헤테로시클로알킬(C1-C6)알킬-; (C5-C10)원 헤테로아릴(C1-C6)알킬-; (C3-C10)원 헤테로시클로알킬-NH-(C1-C16)알킬-; 및 (C3-C10)원 헤테로시클로알킬-N(C(O)-(C1-C6...
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Zusammenfassung: | 본 발명은 R1이 H, (C1-C6)알킬-; 히드록시-(C1-C6)알킬-; NH2-(C1-C6)알킬-; NH-(C1-C6)알킬-(C1-C6)알킬-; N((C1-C6)알킬)2-(C1-C6)알킬-; (C2-C6)알케닐-; (C2-C6)알키닐-; 페닐(C1-C6)알킬-; (C3-C10)시클로알킬(C1-C6)알킬-; (C3-C10)원 헤테로시클로알킬(C1-C6)알킬-; (C5-C10)원 헤테로아릴(C1-C6)알킬-; (C3-C10)원 헤테로시클로알킬-NH-(C1-C16)알킬-; 및 (C3-C10)원 헤테로시클로알킬-N(C(O)-(C1-C6)알킬)-(C1-C16)알킬-을 나타내고; R2가 할로겐 원자, (C1-C6)알킬- 기 또는 다른 잘 정의된 기를 나타내고; R3이 중수소 원자; H, (C1-C6)알킬-; (C2-C6)알케닐-; (C2-C6)알키닐-; (C1-C6)알킬티오-; -OR6; -NR7R8; (C3-C10)원 헤테로시클로알킬-; (C5-C10)원 헤테로아릴-; -(C6-C10)원 아릴; 및 (C3-C10)시클로알킬-을 나타내는 화학식 I의 화합물에 관한 것이다. 본 발명은 또한 이들 화합물의 중간체, 이들의 제조 방법, 이들을 포함하는 의약 및 제약 조성물, 및 특히 TLR7 및/또는 TLR8 작용제로서의 이들의 치료적 용도, 및 백신에서의 이들의 용도에 관한 것이다.
The present invention relates to a compound of formula (I) wherein R1 represents H, (C1-C6)alkyl-; hydroxy-(C1-C6)alkyl-; NH2-(C1-C6)alkyl-; NH-(C1-C6)alkyl-(C1-C6)alkyl-; N((C1-C6)alkyl)2-(C1-C6)alkyl-; (C2-C6)alkenyl-; (C2-C6)alkynyl-; phenyl(C1-C6)alkyl-; (C3-C10)cycloalkyl(C1-C6)alkyl-; (C3-C10)membered heterocycloalkyl(C1-C6)alkyl-; (C5-C10)membered heteroaryl(C1-C6)alkyl-; (C3-C10)membered heterocycloalkyl-NH-(C1-C16)alkyl-; and (C3-C10)membered heterocycloalkyl-N(C(O)-(C1-C6)alkyl)-(C1-C16)alkyl-; R2 represents a halogen atom, a (C1-C6)alkyl- group or other well defined groups; and R3 represents a deuterium atom; H, (C1-C6)alkyl-; (C2-C6)alkenyl-; (C2-C6)alkynyl-; (C1-C6)alkylthio-; -OR6; -NR7R8; (C3-C10)membered heterocycloalkyl-; (C5-C10)membered heteroaryl-; -(C6-C10)membered aryl; and (C3-C10)cycloalkyl-. The present invention further relates to intermediates of these compounds, processes for their preparation, a medicament and a pharmaceutical composition comprising them, and their therapeutic uses, in particular as TLR7 and/or TLR8 agonists, as well as their use in a vaccine. |
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