发明名称 ALDOSTERONE SYNTHASE INHIBITORS
摘要 The present invention relates to compounds of formula (I):;;and pharmaceutically acceptable salts thereof, wherein R1, R2. R3, R4, R5, R6, R7, W, Y, m and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
申请公布号 US2014323468(A1) 申请公布日期 2014.10.30
申请号 US201414262828 申请日期 2014.04.28
申请人 BALESTRA Michael;BURKE Jennifer;CHEN Zhidong;COGAN Derek;FADER Lee;GUO Xin;MCKIBBEN Bryan;MARSHALL Daniel Richard;NEMOTO Peter Allen;YU Hui 发明人 BALESTRA Michael;BURKE Jennifer;CHEN Zhidong;COGAN Derek;FADER Lee;GUO Xin;MCKIBBEN Bryan;MARSHALL Daniel Richard;NEMOTO Peter Allen;YU Hui
分类号 C07D498/04;C07D471/04 主分类号 C07D498/04
代理机构 代理人
主权项 1. A compound of the formula Iwherein: R1 is selected from —NH2, —NHCH3 and —CH3; X is selected from C and O; Y and W are selected from C and N, wherein if Y is N, then W is C and R4 is an electron pair and if W is N, then Y is C and R5 is an electron pair; R2 and R3 are independently selected from —H, —F, —OH and C1-4 alkyl, when X is C; R2 and R3 is an electron pair when X is O; R4 is the group of —(CRaRb)p(A)0-1(CRaRb)qB, wherein: p and q are independently selected from integers between 0 and 5, but p+q is always equal or less than 6; A is selected from O, S and NRe; B is selected from: —H;—OH;—CN;halogen;—SO2Rc;—C(O)Rc;—CO2Rc;—NRcSO2Rd;—SO2NRcRd;—CONRcRd;—NRcCORd; —NRcRd;-Phenyl, optionally substituted with 1 to 3 groups selected from halogen, —CN, —CH2CN, —NRcC(O)Rd, —SO2C1-3alkyl, —C(O)NRcRd, C1-4alkoxy, —SO2NRcRd, —CO2Rc, —NRcSO2Rd—(CH2)0-3SO2C1-3alkyl and C1-3alkyl, wherein said C1-3alkyl is optionally substituted with —OH, halogen or —OCH3;-heteroaryl optionally substituted with 1 to 2 groups independently selected from, —OH, C1-3alkoxy, —(CH2)0-2morpholin-4-yl and C1-6alkyl wherein said C1-6alkyl is optionally substituted with —OH, —CN, C1-3alkoxy-N(Re)2, —CON(Re)2, —SO2C1-3alkyl, —SO2N(Re)2 or halogen; and—C3-7 cycloalkyl, optionally partially unsaturated, wherein up to 3 ring constituting carbons of the cycloalkyl can be optionally replaced with a group selected from O, S, N, NRe, SO, SO2 and CO; and wherein the resulting cycloalkyl or heterocyclyl is optionally substituted with 1 to 3 groups selected from —OH, oxo, —CN, C1-3alkoxy, —N(Re)2, —CON(Re)2, —CO2C1-4alkyl, —C(O)C1-3alkyl, —SO2C1-3alkyl, —SO2N(Re)2, halogen and C1-6alkyl, wherein the C1-6alkyl is optionally substituted with —OH; R5 is selected from —H;—C1-6alkyl optionally substituted with —OH, oxo, —OC1-6alkyl or —OCH2phenyl;—C3-6 cycloalkyl, wherein up to 3 ring constituting carbons can be optionally replaced with a group selected from O, S, N, NRe, SO, SO2 or CO and wherein the resulting cycloalkyl or heterocyclyl is optionally substituted with —OH, —CN, halogen or C1-3alkyl, wherein the C1-3alkyl is optionally substituted with —OH;—CO2Rc;—CN;—CF3;-halogen;—(CRaRb)0-2OC1-3alkyl;—C(O)NRcRd;—CH2Ophenyl, wherein the phenyl is optionally substituted with halogen;-Phenyl, optionally substituted with halogen or SO2C1-3alkyl;—CRaRbNHRe; and-heteroaryl, optionally substituted with C1-3alkyl; R6 and R7 are independently selected from H, —Cl, —F, —CN and —CH3; wherein at least one of R6 or R7 is H; Ra and Rb are independently selected from —H;—C1-6alkyl;—C3-7cycloalkyl wherein up to 3 ring constituting carbons can be optionally replaced with a group selected from O, S, NRe, SO, SO2 and CO;—OH;—CN;-halogen; and—OC1-3alkyl; or Ra and Rb, attached to the same or different atom, along with the atoms that they are attached to can form a C3-7cycloalkyl ring in which up to 3 ring constituting carbon atoms can be optionally replaced with a group selected from O, S, NRe, SO, SO2 and CO; Rc and Rd are independently selected from: —H;—C1-6alkyl optionally substituted with —OH, oxo, —CN, C1-3alkoxyl, —N(Re)2, —CON(Re)2, —SO2C1-3alkyl, —SO2N(Re)2, halogen, heterocyclyl or heteroaryl;—C3-7cycloalkyl optionally substituted with —OH, —CN, C1-6alkyl, C1-3alkoxyl, —N(Re)2, —CON(Re)2, —SO2C1-3alkyl, —SO2N(Re)2 or halogen; wherein up to 3 ring constituting carbon atoms of the ring can be optionally replaced with a group selected from O, S, NRe, SO, SO2 and CO;—(CH2)0-1phenyl, optionally substituted with 1 to 3 groups selected from —OH, —CN, C1-6alkyl, C1-3alkoxyl, —N(Re)2, —CON(Re)2, —SO2C1-3alkyl, —SO2N(Re)2 and halogen;-heteroaryl optionally substituted with 1 to 2 groups independently selected from —OH, —CN, C1-6alkyl, C1-3alkoxyl, —N(Re)2, —CON(Re)2, —SO2C1-3alkyl, —SO2N(Re)2 and halogen;—SO2C1-3alkyl; and—CO2C1-3alkyl; or Rc and Rd along with the atoms that they are attached to can form a C3-7cycloalkyl ring in which up to 3 ring constituting carbon atoms can be optionally replaced by O, S, N, NRe, SO, SO2 or CO, wherein the cycloalkyl or heterocyclyl ring formed can be optionally substituted with one to three groups selected from —OH, —CN, C1-6alkyl, C1-3alkoxyl, —N(Re)2, —CON(Re)2, —SO2C1-3alkyl, —SO2N(Re)2 and halogen, wherein if the ring is substituted with two groups on the same carbon, the groups may join to form a spiro ring; each Re is independently selected from: —H;—C1-6alkyl optionally substituted with —OH, —CN or halogen;—COC1-3alkyl;—CO2C1-4alkyl; and—SO2C1-3alkyl; m is 0 or 1; and n is 0 or 1; wherein if m is 1, then n is 1 and X is O; or a salt thereof.
地址 New Fairfield CT US