公开(公告)号：US08486974B2

公开(公告)日：2013-07-16

申请号：US12808693

申请日：2008-12-19

申请人： John Francis Gilmer ,  Louise Clune-Moriarty ,  Maeve Lally

发明人： John Francis Gilmer ,  Louise Clune-Moriarty ,  Maeve Lally

IPC分类号： A61K31/4406 ,  C07D405/12

CPC分类号： C07D493/04

摘要： Aspirin is one of the most widely used drugs in the treatment of inflammation, pain and fever. It has more recently found application in the prevention of heart attacks and stroke and is being studied as a cancer chemopreventative agent. Despite its value aspirin continues to be underutilized because it causes gastric bleeding. The technology under development potentially removes this problem. It is designed to reduce contact between the drug and the intestinal lining. An isosorbide aspirinate prodrug compound is thus provided. The compound has the general structure as shown in general formula (I) wherein Y is a C1-C8 alkyl ester, a C1-C8 alkoxy ester, a C3-C10 cycloalkyl ester, an arylester, a C1-C8 alkylaryl ester or —C(O)ORring, wherein Rring is a 5-membered aromatic or nonaromatic 5-member ring having at least one heteroatom substituted for a carbon of the ring system, which can be unsubstituted or substituted with at least one nitric oxide releasing group.

摘要翻译： 阿司匹林是治疗炎症，疼痛和发烧最广泛使用的药物之一。 最近发现应用于预防心脏病发作和中风，并正在研究中作为癌症化学预防剂。 尽管阿司匹林的价值仍然不足，因为它导致胃出血。 正在开发的技术可能会消除这个问题。 它旨在减少药物和肠内膜之间的接触。 因此提供了异山梨醇阿司匹林前药化合物。 该化合物具有通式（I）所示的一般结构，其中Y为C1-C8烷基酯，C1-C8烷氧基酯，C3-C10环烷基酯，芳基酯，C1-C8烷基芳基酯或-C （O）ORring，其中Rring是具有至少一个取代环系的碳的杂原子的5元芳族或非芳族5元环，其可以是未取代的或被至少一个一氧化氮释放基团取代。

公开(公告)号：US20110046182A1

公开(公告)日：2011-02-24

申请号：US12808693

申请日：2008-12-19

申请人： John Francis Gilmer ,  Louise Clune-Moriarty ,  Maeve Lally

发明人： John Francis Gilmer ,  Louise Clune-Moriarty ,  Maeve Lally

IPC分类号： A61K31/443 ,  C07D493/04 ,  C07D261/02 ,  C07D285/06 ,  C07D405/12 ,  A61K31/34 ,  A61K31/422 ,  A61K31/433 ,  A61P25/28 ,  A61P9/00 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D493/04

摘要： Aspirin is one of the most widely used drugs in the treatment of inflammation, pain and fever. It has more recently found application in the prevention of heart attacks and stroke and is being studied as a cancer chemopreventative agent. Despite its value aspirin continues to be underutilized because it causes gastric bleeding. The technology under development potentially removes this problem. It is designed to reduce contact between the drug and the intestinal lining. An isosorbide aspirinate prodrug compound is thus provided. The compound has the general structure as shown in general formula (I) wherein Y is a C1-C8 alkyl ester, a C1-C8 alkoxy ester, a C3-C10 cycloalkyl ester, an arylester, a C1-C8 alkylaryl ester or —C(O)ORring, wherein Rring is a 5-membered aromatic or nonaromatic 5-member ring having at least one heteroatom substituted for a carbon of the ring system, which can be unsubstituted or substituted with at least one nitric oxide releasing group.

摘要翻译： 阿司匹林是治疗炎症，疼痛和发烧最广泛使用的药物之一。 最近发现应用于预防心脏病发作和中风，并正在研究中作为癌症化学预防剂。 尽管阿司匹林的价值仍然不足，因为它导致胃出血。 正在开发的技术可能会消除这个问题。 它旨在减少药物和肠内膜之间的接触。 因此提供了异山梨醇阿司匹林前药化合物。 该化合物具有通式（I）所示的一般结构，其中Y为C1-C8烷基酯，C1-C8烷氧基酯，C3-C10环烷基酯，芳基酯，C1-C8烷基芳基酯或-C （O）ORring，其中Rring是具有至少一个取代环系的碳的杂原子的5元芳族或非芳族5元环，其可以是未取代的或被至少一个一氧化氮释放基团取代。