发明名称 SUBSTITUTED ISOQUINOLINES AS CRTH2 RECEPTOR MODULATORS
摘要 The invention provides certain substituted isoquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters. The invention also provides pharmaceutical compositions comprising for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.;
申请公布号 US2015353498(A1) 申请公布日期 2015.12.10
申请号 US201314432462 申请日期 2013.09.26
申请人 HUANG Xianhai;PALANI Anandan;RAO Ashwin U.;ZHANG Hongjun;ZHOU Wei;MERCK SHARP & DOHME CORP. 发明人 Huang Xianhai;Palani Anandan;Rao Ashwin U.;Zhang Hongjun;Zhou Wei
分类号 C07D217/24;C07D401/06;C07D413/14;A61K31/4725;C07D413/04;A61K31/472;A61K31/496 主分类号 C07D217/24
代理机构 代理人
主权项 1. A compound of the Formula (I) wherein: Z is a bond or —N(H)—; RA is —OH, —N(H)—S(O)2—RA1, or —N(H)—S(O)2—N(H)RA1 RA1 is C1-C6 alkyl, C3-C6 cycloalkyl, or phenyl, wherein RA1 is unsubstituted or substituted by 1 to 3 fluoro or C1-C3 alkyl; the subscript n is 1, 2, 3, or 4; M is a bond or C1-C3 alkylene; ring AH is A. phenyl; orB. a 5- to 6-membered heteroaryl containing 1 to 3 heteroatoms selected from the group consisting of N, O, and S; each R2 is independently selected from the group consisting of halo, C1-C3 alkyl, C1-C3 fluoroalkyl, C3-C6 cycloalkyl, C1-C3 alkoxy, and —CN; the subscript b is 0, 1, 2, 3, 4, or 5; Rq1, Rq2, Rq3, and Rq4 are independently selected from the group consisting of H, halo, and C1-C3 alkyl; R1 is A. a group of the formula —C(O)N(R3)(R4), wherein1. R3 and R4 are independently (a.) H, or(b.) —Z—R5C, wherein Z is a bond or C1-C3 alkylene;R5C is (i) C5-C10 mono or bicyclic carbocyclyl, (ii.) 5- to 10-membered mono- or bicyclic heterocyclyl containing 1 to 3 heteroatoms selected from N and O; (iii.) 5- to 10-membered mono or bicyclic heteroaryl containing 1 to 3 heteroatoms selected from N and O; wherein said carbocyclyl, heterocyclyl, and heteroaryl of R5C is unsubstituted or substituted by 1 to 4 R5A moieties selected from the group consisting of halo, C1-C3 alkyl, C1-C3 fluoroalkyl, C1-C3 alkoxy, and —CN; or2. R3 and R4 together with the N atom to which they are attached form R5H, wherein R5H is selected from the group consisting of: ring Ar is aryl, pyridyl, or pyrimidyl;each R7 is independently selected from the group consisting of halo, C1-C3 alkyl, C1-C3 fluoroalkyl, C1-C3 alkoxy, and —CN;each R8 is independently selected from the group consisting of H and C1-C3 alkyl;the subscript u1 is 0, 1 or 2;the subscript u2 is 0, 1, 2, or 3; orB. a moiety selected from the group consisting of: Y is a bond or C1-C3 alkylene;R6 is H, C1-C3 alkyl, or C3-C6 cycloalkyl;Rcy is: 1. C6-C10 mono or bicyclic carbocyclyl;2. 5- to 9-membered mono- or bicyclic heterocyclyl containing 1 to 3 heteroatoms selected from the group consisting of N and O;3. 5- to 9-membered mono- or bicyclic heteroaryl containing 1 to 3 heteroatoms selected N and O; wherein Rcy is unsubstituted or substituted by 1 to 3 R9 moieties which are independently selected from the group consisting of halo, C1-C3 alkyl, Cr C3 fluoroalkyl, C1-C3 alkoxy, and —CN, or wherein two R9 moieties are geminally substituted on a common ring carbon of RcY, the two geminally substituted R9 moieties, together with said common carbon atom, form —C(O)—;or a pharmaceutically acceptable salt thereof.
地址 Rahway NJ US