Compounds and method for blocking transmission of malarial parasite

A compound of formula (I):

• wherein A is CR5 or N,
• B is CR3═CR4 or NR6,
• R1 is C6-10 aryl or heteroaryl substituted with at least one substituent selected from —CN, cyanomethyl, —SO2R13, —SO2NHR15, and —CONR11R12, optionally further in combination with one or more substituents selected from halo, C1-12 alkyl, alkoxy, a heterocyclyl group selected from the group consisting of optionally substituted piperazinyl, morpholinyl, pyrrolinidyl, and diazepinyl, or an aryl bicyclic lactam of the formula:
• wherein the aryl group of the aryl bicyclic lactam is optionally substituted with at least one substituent selected from —CN, cyanomethyl, —SO2R13, —SO2NH2, and —CONR11R12 optionally further in combination with one or more substituents selected from halo, C1-12 alkyl, alkoxy, 2-(dimethylamino)ethyl)amino, dimethylamino, a heterocyclyl group selected from the group consisting of optionally substituted piperazinyl, morpholinyl, pyrrolinidyl, azetidinyl and diazepinyl,
• R2 is selected from 2-amino-5-pyridinyl, 4-pyridinyl, 2-amino-5-pyrimidinyl, 3-pyridyl, quinolin-3-yl, 5-pyrimidinyl, 2-acetylamino-5-pyridyl, 2-amino-4-methylpyrimidin-5-yl, 1-piperazinyl, indol-5-yl, 1H-imdazol-5-yl, 4-aminophenyl, 1,2,3,6-tetrahydropyridin-4-yl, 1H-pyrazol-4-yl, N-methyl-pyrazol-4-yl, 1H-benzo[d]imidazol-5-yl, 4-sulfonylaminophenyl, 2-dimethylaminopyrimidin-5-yl, 3-trifluoromethylphenyl, bromo, 3-aminophenyl, vinyl, 4-aminocarbonylphenyl, 3-cyanophenyl, 3-hydroxyphenyl, 3-trifluoromethyl-5-pyridyl, tetrazolyl, 4-chlorophenyl, 4-fluorophenyl, 4-methoxyphenyl, 3-aminocarbonylphenyl, 3-acetylphenyl, 3-cyano-4-chlorophenyl, 3-cyano-5-methylphenyl, 3-hydroxy-4-chlorophenyl, 4-hydroxymethylphenyl, 3-amino-4-chlorophenyl, 2,3-dihydrobenzofuran-6-yl, 1-methyl-1H-indol-5-yl, benzo[d][1,3]dioxo-5-yl, 4-fluorophenyl, 4-hydroxyphenyl, morpholin-1-yl, benzo[b]thiophen-1-yl, 4-methylsulfonylphenyl, benzo[c][1,2,5]oxadiazol-5-yl, 2-(piperidin-1-yl)-3-pyridinyl, 4-carboxyphenyl, 2-methyl-5-pyridyl, 4-methylsulfonylphenyl, 4-dimethylaminocarbonylphenyl, 4-phenylphenyl, 4-methylphenyl, 3-chloro-5-pyridyl, (3-pyrrolidin-1-yl)phenyl, 4-([piperizin-1-yl]carbonyl)phenyl, 4-([morpholin-1-yl]carbonyl)phenyl, 2-hydroxypyrimidin-5-yl, 3-aminosulfonylphenyl, 2-oxo-1,2,3,4,tetrahydroisoquinolin-6-yl, 2-oxo-1,2,3,4,-tetrahydroquinolin-6-yl, 4-(methylaminocarbonyl)phenyl, 1-oxoindolin-5-yl, 2-oxoindolin-5-yl, 1-oxoisoindolin-5-yl, 2-amino-4-pyridyl, 4-aminomethylphenyl, 3-methoxy-4-chlorophenyl, 3-methylphenyl, 3-methoxyphenyl, phenyl, 5-indolinone, 5-isoindolinone, 2-hydroxy-4-chlorophenyl, 4-cyanophenyl, 4-azetidinylphenyl, 4-ethylphenyl, 3-fluorophenyl, 3-chlorophenyl, 3-dimethylaminomethylphenyl, 3-cyano-4-fluorophenyl, 3-amino-4-fluorophenyl, 4-(1-hydroxy-1-ethylphenyl, 3-methyl-5-pyridyl, 2-acetylamio-5-pyridyl, 2-oxoindolin-5-yl, benzimidazolin-5-yl, 3-dimethylamino-1-propargyl, 2-pyrrolyl, N-methyl-2-pyrrolyl, 2-thiopheneyl, 3-thiopheneyl, 3-furanyl, and 3-aminosulfonylphenyl,
• R3 and R4 are independently selected from hydrogen, hydroxyl, OR5, halogen, optionally substituted C6-10 aryl, and optionally substituted C1-6 alkyl,
• R5 is hydrogen, C1-12 alkyl, C6-10 aryl, halogen, hydroxyl, or OR16,
• R6 is hydrogen, C1-12 alkyl, C2-12 hydroxyalkyl, C1-6 acyl-C1-6 alkyl, or C6-10 aryl,
• R7-R10 are independently selected from hydrogen, C1-12 alkyl, C3-8 cycloalkyl, CH2COOR13, and H2N(CH2)n— wherein n is an integer of 2-6,
• R11 and R12 selected from the group consisting of hydrogen, C1-12 alkyl and C3-10 cycloalkyl or, taken together with the N to which they are bound, form an optionally substituted 4-7 membered heterocyclyl ring containing O or N atoms, and
• R13 is C1-12 alkyl,
• R15 is hydrogen or C1-12 alkyl,
• R16 is C1-12 alkyl, C1-6 acyl, or C6-10 aryl,
• or a pharmaceutically acceptable salt thereof,
• with the proviso that when A is CH, B is CR3═CR4, R3 and R4 are each hydrogen, and R2 is 2-amino-5-pyridyl, R1 is not 3-cyanophenyl or 3-aminosulfonylphenyl.