发明名称 Inhibitors of rho associated protein kinases (ROCK) and methods of use
摘要 Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.
申请公布号 US9409868(B2) 申请公布日期 2016.08.09
申请号 US201314374445 申请日期 2013.01.24
申请人 H. Lee Moffin Cancer Center and Research Institute, Inc. 发明人 Schonbrunn Ernst;Li Rongshi;Sebti Said M.
分类号 C07D231/56;C07D213/40;C07D213/36;A61K45/06;A61K31/416;A61K31/4418;A61N5/10 主分类号 C07D231/56
代理机构 Meunier Carlin & Curfman LLC 代理人 Meunier Carlin & Curfman LLC
主权项 1. A compound having the chemical structure shown in Formula IV wherein R is H, alkyl, acetyl, or heteroalkyl; R1 is H, alkyl, acetyl, or heteroalkyl; R8 and R9 are, independently of one another, H, —OH, acetyl, —C(O)NH2, alkyl, cycloalkyl, hereterocycloalkyl, aryl, or heteroaryl, wherein any one of the alkyl, cycloalkyl, hereterocycloalkyl, aryl, or heteroaryl groups is optionally substituted with one or more of —OH, —NO2, —NH2, —NR6R7, carbonyl, alkoxy, alkyl, —OCX3, —OCHX2, —OCH2X, or halogen, or both R8 together form a carbonyl; and R10 is cycloalkyl, aryl, or heteroaryl, any of which is optionally substituted with one or more of —OH, —C(O)NH2, —C(O)CH3, —NO2, —NH2, —NR6R7, carbonyl, alkyl, alkoxy, alkylalkoxy, alkoxylalkoxy, halogenated alkoxyl, cycloalkyl, heterocycloalkyl, heteroarylcarbonyl, aryl, heteroaryl, —OCX3, —OCHX2, —OCH2X, —OSO2CH3, or -tosyl; R6 and R7 are, independently, H, alkyl, —SO2CH3, —C(O)CH3, or —C(O)NH2; X is independently H or halogen; and n is 2 or 3.
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