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57- 4-23- 57-Disubstituted 4-aminopyrido23-dpyrimidine compounds and their use as adenosine kinase inhibitors

机译:57- 4- [23-] 57-双取代的4-氨基吡啶[23-d]嘧啶化合物及其作为腺苷激酶抑制剂的用途

摘要

The present invention requires the treatment of the compound of pharmaceutical compositions, a therapeutically effective amount, including in combination with acceptable carriers for the compounds of the method of inhibiting adenosine kinase by administering a compound of formula I, a therapeutically effective amount of a pharmaceutically It is in a mammal comprising administering to a mammal a method for treating cerebral ischemia, epilepsy, trauma perception, inflammation and sepsis, the method for producing the compound, and R 1, R 2, R 3 and R 4 to a to each defined as provides a compound of formula.; Formula I; Wherein; R 1 and R 2 are independently H, lower alkyl, C 1 -C 6 alkoxy C 1 -C 6 alkyl, aryl C 1 -C 6 alkyl, -C (O) C 1 -C 6 alkyl, -C each other ( O) aryl, -C (O) a 5 to 7 membered ring containing 1 or 2 additional heteroatoms selected from O, N or S bonded together with the nitrogen to which they are attached, selected from heterocyclic or optionally and forming;; R 3 is lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocyclic group, heteroarylalkyl or heterocycloalkyl (wherein heterocyclic aryl and heteroaryl groups are either directly or It is selected from the group consisting of indirect coupling is by) by a ring carbon;; R 4 is lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocyclic group heteroarylalkyl or is selected from the group consisting of heterocycloalkyl;; --- line represents a double bond that is optionally present is a suitable atom maintained.
机译:本发明需要治疗有效量的药物组合物的化合物,包括与通过给予式I化合物抑制腺苷激酶的方法的化合物的可接受的载体组合的治疗有效量的药物。在哺乳动物中,包括对哺乳动物施用治疗脑缺血,癫痫,创伤知觉,炎症和败血症的方法,制备该化合物的方法,以及R 1, R 2,< / Sup> R 3 和R 4 分别定义为提供式的化合物。一级方程式其中R 1 和R 2 独立地为H,低级烷基,C 1 -C 6 烷氧基C 1 -C 6 烷基,芳基C 1 -C 6 烷基,-C(O)C 1 < / Sub> -C 6 烷基,彼此-C(O)芳基,-C(O)5至7元环,其中包含1个或2个选自O,N或S的其他杂原子与它们连接的氮,选自杂环或任选地形成的; R 3 是低级烷基,低级烯基,低级炔基,环烷基,芳基,芳基烷基,杂芳基,杂环基,杂芳基烷基或杂环烷基(其中杂环芳基和杂芳基是直接的或选自以下基团)由间接偶合组成的是由一个环碳; R 4 为低级烷基,低级烯基,低级炔基,环烷基,芳基,芳基烷基,杂芳基,杂环基杂芳基烷基或选自杂环烷基; ---线表示任选存在的双键,其是保持的合适原子。

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