摘要 |
A compound of Formula I:
wherein:
X is CHC(R 13 Y'Y), CR 6' R 6 , S, NR 6 , or O;
R 2 , R 2' , R 4' , and R 4" are each independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, aryl, heterocyclic, heteroaromatic or a prodrug moiety;
R 4 is NR 4' R 4" , alkyl, alkenyl, alkynyl, hydroxyl, halogen, or hydrogen;
R 2' , R 3 , R 10 , R 11 and R 12 are each hydrogen or a pro-drug moiety;
R 5 is hydroxyl, hydrogen, thiol, alkanoyl, aroyl, alkaroyl, aryl, heteroaromatic, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, alkyl carbonyloxy, or aryl carbonyloxy;
R 6 and R 6' are each independently hydrogen, methylene, absent, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
R 7 is ethyl, perhalogenated alkenyl, substituted pyridinyl, pyrazinyl, furanyl, or pyrazolyl;
R 8 is hydrogen, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
R 9 -CH 2 NR 9a R 9b ;
R 9a and R 9b are each independently hydrogen, alkyl, alkenyl or linked to form a heterocycle;
R 13 is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl; and
Y' and Y are each independently hydrogen, halogen, hydroxyl, cyano, sulfhydryl, amino, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl, or a pharmaceutically acceptable salt thereof. |
申请人 |
PARATEK PHARMACEUTICALS, INC. |
发明人 |
NELSON, MARK, L.;AMOO, VICTOR;KIM, OAK, K.;ABATO, PAUL;OHEMENG, KWASI;ASSEFA, HAREGWEIN;BERNIAC, JOEL;BHATIA, BEENA;BOWSER, TODD;CHEN, JACKSON;GRIER, MARK;HONEYMAN, LAURA;ISMAIL, MOHAMED, Y.;MECHICHE, RACHID;MATHEWS, JUDE |