摘要 |
Disclosed are 6-amino-purine derivatives as represented by the general Formula I or a pharmaceutically acceptable salt thereof, wherein: A is a substituted or unsubstituted benzo[1,3]dioxole group, indanone or indane group; B is a substituted or unsubstituted aryl, heteroaryl, heterocyclic, or carbocyclic group such as a piperidine, homopiperidine, piperazine, pyrrolidine or azetidine group; R1 is hydrogen, alkyl, aryl, heteroaryl, amino, or halo; and wherein the other substituents are as defined hererin. Of particular importance are the compounds 9-[2-(1-acetylpiperidin-4-yl)ethyl]-8-[(6-bromo-1,3-benzodioxol-5-yl)thio]-9H-purin-6-amine, 4-(2-{ 6-amino-8-[(6-bromo-1,3-benzodioxol-5-yl)thio]-9H-purin-9-yl} ethyl)piperidine-1-carbaldehyde, (2S)-1-[4-(2-{ 6-amino-8-[(6-bromo-1,3-benzodioxol-5-yl)thio]-9H-purin-9-yl} ethyl)piperidin-1-yl]-1-oxopropan-2-ol, 2-[4-(2-{ 6-amino-8-[(6-bromo-1,3-benzodioxol-5-yl)thio]-9H-purin-9-yl} ethyl)piperidin-1-yl]-2-oxoethanol, 6-({ 9-[2-(1-acetylpiperidin-4-yl)ethyl]-6-amino-9H-purin-8-yl} thio )-1,3-benzodioxole-5-carbonitrile, and (2R)-1-[4-(2-{ 6-amino-8-[(6-bromo-1,3-benzodioxol-5-yl)thio]-9H-purin-9-yl} ethyl)piperidin-1-yl]-1-oxopropan-2-ol. Further disclosed is a pharmaceutical composition comprising a compound as defined above for the treatment of a disorder chosen from inflammatory diseases, infections, autoimmune disorders, stroke, ischemia, cardiac disorders, neurological disorders, fibrogenetic disorders, proliferative disorders, tumors, leukemias, neoplasms, cancers, carcinomas, metabolic diseases, and malignant disease.
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申请人 |
MYREXIS, INC. |
发明人 |
BAJJI, ASHOK C;KIM, SE-HO;MARKOVITZ, BENJAMIN;TROVATO, RICHARD;TANGALLAPALLY, RAJENDRA;ANDERSON, MARK B;WETTSTEIN, DANIEL;SHENDEROVICH, MARK;VANECKO, JOHN A |