发明名称 PHTHALAZINES AS POTASSIUM ION CHANNEL INHIBITORS
摘要 A compound of formula (I);;wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
申请公布号 US2014303168(A1) 申请公布日期 2014.10.09
申请号 US201414200063 申请日期 2014.03.07
申请人 BRISTOL-MYERS SQUIBB COMPANY 发明人 Finlay Heather;Adisechan Ashok Kumar;Gunaga Prashantha;Lloyd John;Srinivasu Pothukanuri
分类号 C07D405/14;C07D403/04;C07D401/04;A61K31/506;C07D401/14;A61K31/502 主分类号 C07D405/14
代理机构 代理人
主权项 1. A compound of formula I or an enantiomer, diastereomer, tautomer, or salt thereof wherein: A is —(CH2)m—R2, —CH(R26)—R2, —(CH2)n−1—O—R2, —(CH2)n−1—NR25—R2, —CH(R26)—CO2—R2, or —(CH2)n−1—NR25—C2—R2;R1 is C1-10 alkyl substituted with 1-2 —OH, haloC1-10 alkyl, C2-12 alkenyl, C3-10 cycloalkyl, wherein the cycloalkyl may be substituted with 0-2 R13; orR1 isany of which may be substituted with 0-2 R13; R2 is phenyl, cyclopentyl, cyclohexyl, pyridinyl, pyrazinyl, pyridazinyl, pyrimidinyl, piperidinyl, pyridinone, pyrrolidinyl, tetrahydropyrans, or thiazolyl, any of which are substituted with 0-2 R2a;R2a, at each occurrence, is independently H, —OH, F, Cl, Br, I, C1-10alkyl, C1-10alkoxy, haloC1-10 alkyl, C3-10 cycloalkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10aryl, a 4- to 12-membered heteroaryl, a 4- to 12-membered heterocyclyl, a 4- to 12-membered heteroaryl-C1-10 alkyl, —CN, —NO2, —(CH2)m—SO2R14, —NR14SO2R14, ═O, —CONR14R14, —(CH2)m—SO2NR14R14, —(CH2)m—NR14SO2R14, —(CH2)n—NR14SO2NR14R14, —NR14SO2NR14R14, —CO2NR14R14, —NR14CO2NR14R14, —NR14COR14, —SO2NR14COR14, —SO2NR14CONR14R14, —NR14CO2R14, —CO2R14, —NR14R14, NR14CONR14R14, —C(═NOR14)NR14R14, —CONR14OR14 or —NCOR14, wherein the alkyl, cycloalkyl, alkenyl, alkoxy, aryl, heteroaryl and heterocyclyl may be substituted with 0-2 R14a, and the heteroaryl and heterocyclyl consist of carbon atoms and 1, 2, 3, or 4 heteroatoms independently selected from the group consisting of N, S, or O;R3 is phenyl, pyridinyl, pyrimidinyl, or dihydropyran, tetrahydropyran any of which may be substituted with 0-1 R3a;R3a is halo, CN, NH2, —O—C1-3alkyl, or morpholinyl;R13, at each occurrence, is independently H, —OH, F, Cl, Br, I, CN, C1-10 alkyl, C1-10 alkoxy, haloC1-10 alkyl, C3-10 cycloalkyl, C2-12 alkenyl, C2-12 alkynyl, C6-10aryl, a 4- to 12-membered heteroaryl, a 4- to 12-membered heterocyclyl, a 4- to 12-membered heteroaryl-C1-10 alkyl, —CN, —NO2, —(CH2)m—SO2R14, —NR14SO2R14, ═O, —CONR14R14, —(CH2)m—SO2NR14R14, —(CH2)m—NR14SO2R14, —(CH2)n—NR14SO2NR14R14, —NR14SO2NR14R14, —CO2NR14R14, —NR14CO2NR14R14, —NR14COR14, —SO2NR14COR14, —SO2NR14CONR14R14, —NR14CO2R14, —CO2R14, —NR14R14, NR14CONR14R14, —C(═NOR14)NR14R14, —CONR14OR14 or —NCOR14, OR14, wherein the alkyl, cycloalkyl, alkenyl, alkoxy, aryl, heteroaryl and heterocyclyl may be substituted with 0-2 R14a, and the heteroaryl and heterocyclyl consist of carbon atoms and 1, 2, 3, or 4 heteroatoms independently selected from the group consisting of N, S, or O;R14, at each occurrence, is independently selected from hydrogen, C1-10 alkyl, C3-10 cycloalkyl, C6-10 aryl, a 4- to 12-membered heteroaryl or a 4- to 12-membered heterocyclyl, wherein the alkyl, cycloalkyl, aryl, heteroaryl and heterocyclyl may be substituted with 0-3 R14a and the heteroaryl and heterocyclyl consist of carbon atoms and 1, 2, 3, or 4 heteroatoms independently selected from the group consisting of N, S, or O; oralternatively, two R14's are taken together with the atoms to which they are attached to form a cyclic ring, wherein the cyclic ring may be substituted with 0-1 R14a and optionally contain 1, 2, 3, or 4 heteroatoms independently selected from the group consisting of N, S, or O;R14a, at each occurrence, is independently selected from F, Cl, Br, I, C1-10 alkyl, haloC1-10alkyl, C6-10 aryl, C3-10cycloalkyl, a 4- to 12-membered heteroaryl, a 4- to 12-membered heterocyclyl, F, Cl, Br, I, —CN, —NO2, —CO2R26, —CO2NR24R24, —OCF3, —OR25, ═O, —CONR24R24, —COR24, —SO2R24, —NR24R24, —NR24CO2R24, —SO2NR24R24, or C6-10arylC1-10alkyl, wherein the heteroaryl and heterocyclyl consist of carbon atoms and 1, 2, 3, or 4 heteroatoms independently selected from the group consisting of N, S, or O;R24, at each occurrence, is independently selected from hydrogen, C1-10alkyl, C3-6cycloalkyl, or phenyl; orR25, at each occurrence, is independently selected from hydrogen, C1-10alkyl, C3-6cycloalkyl, or phenyl;R26, at each occurrence, is independently selected from hydrogen, C1-10alkyl, C3-6cycloalkyl, or phenyl;m is 0 to 4;n is 0 to 4; orn−1 is 2 to 4.
地址 Princeton NJ US