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1. 发明申请

US20100210656A1 NOVEL sEH INHIBITORS AND THEIR USE 有权
标题翻译：新型抑制剂及其用途
公开(公告)号：US20100210656A1
公开(公告)日：2010-08-19
申请号：US12682073
申请日：2008-10-10
申请人： Yun Ding , Reema K. Thalji , Joseph P. Marino, JR.
发明人： Yun Ding , Reema K. Thalji , Joseph P. Marino, JR.
IPC分类号： A61K31/53 , C07D401/04 , C07D251/18 , C07D409/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D251/52 , A61P9/10 , A61P9/00 , A61P9/04 , A61P11/06 , A61P11/00 , A61P3/10 , A61P3/04
CPC分类号： C07D241/46 , C07D251/18 , C07D251/52 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/04
摘要： The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R4, R5, R6, A, B, Y, Z, n, and m are defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are sEH inhibitors and can be used in the treatment of diseases mediated by the sEH enzyme, such as hypertension. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting sEH and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及新型sEH抑制剂及其在治疗由sEH酶介导的疾病中的用途。具体地，本发明涉及式I化合物：其中R1，R2，R4，R5，R6，A，B，Y，Z，n和m定义如下，及其药学上可接受的盐。本发明的化合物是sEH抑制剂，可用于治疗由sEH酶介导的疾病，例如高血压。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物来抑制sEH和与之相关的病症的治疗方法。

2. 发明授权

US08008483B2 sEH inhibitors and their use 有权
标题翻译： sEH抑制剂及其用途
公开(公告)号：US08008483B2
公开(公告)日：2011-08-30
申请号：US12682077
申请日：2008-10-10
申请人： Yun Ding , Reema K. Thalji , Joseph P. Marino, Jr.
发明人： Yun Ding , Reema K. Thalji , Joseph P. Marino, Jr.
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , A61K31/53 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/06 , A61P11/00 , A61P13/12 , A61P1/16
CPC分类号： C07D401/04 , C07D251/54 , C07D401/14 , C07D403/04 , C07D409/14
摘要： The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, R5a, R6a A, B, Y, x, and m are defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are sEH inhibitors and can be used in the treatment of diseases mediated by the sEH enzyme, such as hypertension. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting sEH and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及新型sEH抑制剂及其在治疗由sEH酶介导的疾病中的用途。具体地，本发明涉及式I化合物及其药学上可接受的盐，其中R1，R2，R3，R5a，R6aA，B，Y，x和m定义如下。本发明的化合物是sEH抑制剂，可用于治疗由sEH酶介导的疾病，例如高血压。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物来抑制sEH和与之相关的病症的治疗方法。

3. 发明申请

US20100249137A1 Novel sEH Inhibitors and Their Use 有权
标题翻译：新型sEH抑制剂及其用途
公开(公告)号：US20100249137A1
公开(公告)日：2010-09-30
申请号：US12757089
申请日：2010-04-09
申请人： Yun DING , Reema K. Thalji , Joseph P. Marino, JR.
发明人： Yun DING , Reema K. Thalji , Joseph P. Marino, JR.
IPC分类号： A61K31/53 , C07D251/18 , A61P1/16 , A61P9/10 , A61P9/12 , A61P9/04 , A61P11/06 , A61P5/50 , A61P3/04 , A61P3/10
CPC分类号： C07D241/46 , C07D251/18 , C07D251/52 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/04
摘要： The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to (Cis)-N-{[4-cyano-2-(trifluoromethyl)phenyl]methyl}-3-{[4-methyl-6-(methylamino)-1,3,5-triazin-2-yl]amino}cyclohexanecarboxamide; or a pharmaceutically acceptable salt thereof, and N-{[4-cyano-2-(trifluoromethyl)phenyl]methyl}-3-{[4-methyl-6-(methylamino)-1,3,5-triazin-2-yl]amino}cyclohexanecarboxamide; or a pharmaceutically acceptable salt thereof.The compounds of the invention can be used in the treatment of diseases mediated by the sEH enzyme, such as hypertension, asthma, and COPD. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting sEH and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及新型sEH抑制剂及其在治疗由sEH酶介导的疾病中的用途。具体地，本发明涉及（C 1）-N - {[4-氰基-2-（三氟甲基）苯基]甲基} -3 - {[4-甲基-6-（甲基氨基）-1,3,5-三嗪 -2-基]氨基}环己烷甲酰胺; 或其药学上可接受的盐和N - {[4-氰基-2-（三氟甲基）苯基]甲基} -3 - {[4-甲基-6-（甲基氨基）-1,3,5-三嗪-2-基 - 吡啶-2-基]氨基}环己烷甲酰胺; 或其药学上可接受的盐。本发明的化合物可用于治疗由sEH酶介导的疾病，如高血压，哮喘和COPD。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物来抑制sEH和与之相关的病症的治疗方法。

4. 发明申请

US20100210628A1 NOVEL sEH INHIBITORS AND THEIR USE 有权
标题翻译：新型抑制剂及其用途
公开(公告)号：US20100210628A1
公开(公告)日：2010-08-19
申请号：US12682077
申请日：2008-10-10
申请人： Yun Ding , Reema K. Thalji , Joseph P. Marino, JR.
发明人： Yun Ding , Reema K. Thalji , Joseph P. Marino, JR.
IPC分类号： A61K31/55 , C07D403/04 , A61K31/53 , C07D403/14 , C07D413/14 , A61K31/5377 , C07D401/14 , A61P3/10 , A61P3/04 , A61P1/16 , A61P9/00 , A61P11/06
CPC分类号： C07D401/04 , C07D251/54 , C07D401/14 , C07D403/04 , C07D409/14
摘要： The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, R5a, R6a A, B, Y, x, and m are defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are sEH inhibitors and can be used in the treatment of diseases mediated by the sEH enzyme, such as hypertension. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting sEH and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及新型sEH抑制剂及其用于治疗由sEH酶介导的疾病的用途。具体地，本发明涉及式I化合物及其药学上可接受的盐，其中R1，R2，R3，R5a，R6aA，B，Y，x和m定义如下。本发明的化合物是sEH抑制剂，可用于治疗由sEH酶介导的疾病，例如高血压。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物来抑制sEH和与之相关的病症的治疗方法。

5. 发明授权

US07304082B2 1,2,4-triazole derivatives, compositions, process of making and methods of use 失效
标题翻译： 1,2,4-三唑衍生物，组合物，制备方法和使用方法
公开(公告)号：US07304082B2
公开(公告)日：2007-12-04
申请号：US11186519
申请日：2005-07-21
申请人： Joseph P. Marino, Jr. , Scott K. Thompson , Daniel Frank Veber
发明人： Joseph P. Marino, Jr. , Scott K. Thompson , Daniel Frank Veber
IPC分类号： A61K31/4196 , C07D249/14
CPC分类号： C07D405/12 , A61K31/4196 , A61K31/422 , A61K31/4439 , C07D249/14 , C07D409/12
摘要： Compounds of this invention are non-peptide, reversible inhibitors of type 2 methionine aminopeptidase, useful in treating conditions mediated by angiogenesis, such as cancer, haemangioma, proliferative retinopathy, rheumatoid arthritis, atherosclerotic neovascularization, psoriasis, ocular neovascularization and obesity.
摘要翻译：本发明化合物是可用于治疗由血管发生介导的病症，例如癌症，血管瘤，增殖性视网膜病变，类风湿性关节炎，动脉粥样硬化新生血管形成，牛皮癣，眼新生血管形成和肥胖的2型甲硫氨酸氨基肽酶的非肽可逆抑制剂。

6. 发明授权

US08212032B2 sEH inhibitors and their use 有权
标题翻译： sEH抑制剂及其用途
公开(公告)号：US08212032B2
公开(公告)日：2012-07-03
申请号：US12757089
申请日：2010-04-09
申请人： Yun Ding , Reema K. Thalji , Joseph P. Marino, Jr.
发明人： Yun Ding , Reema K. Thalji , Joseph P. Marino, Jr.
IPC分类号： C07D251/50 , A61K31/53 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/06 , A61P11/00 , A61P13/12
CPC分类号： C07D241/46 , C07D251/18 , C07D251/52 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/04
摘要： The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to (Cis)-N-{[4-cyano-2-(trifluoromethyl)phenyl]methyl}-3-{[4-methyl-6-(methylamino)-1,3,5-triazin-2-yl]amino}cyclohexanecarboxamide; or a pharmaceutically acceptable salt thereof, and N-{[4-cyano-2-(trifluoromethyl)phenyl]methyl}-3-{[4-methyl-6-(methylamino)-1,3,5-triazin-2-yl]amino}cyclohexanecarboxamide; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及新型sEH抑制剂及其在治疗由sEH酶介导的疾病中的用途。具体地，本发明涉及（C 1）-N - {[4-氰基-2-（三氟甲基）苯基]甲基} -3 - {[4-甲基-6-（甲基氨基）-1,3,5-三嗪 -2-基]氨基}环己烷甲酰胺; 或其药学上可接受的盐和N - {[4-氰基-2-（三氟甲基）苯基]甲基} -3 - {[4-甲基-6-（甲基氨基）-1,3,5-三嗪-2-基 - 吡啶-2-基]氨基}环己烷甲酰胺; 或其药学上可接受的盐。

7. 发明授权

US08173805B2 sEH inhibitors and their use 有权
标题翻译： sEH抑制剂及其用途
公开(公告)号：US08173805B2
公开(公告)日：2012-05-08
申请号：US12682073
申请日：2008-10-10
申请人： Yun Ding , Reema K. Thalji , Joseph P. Marino, Jr.
发明人： Yun Ding , Reema K. Thalji , Joseph P. Marino, Jr.
IPC分类号： C07D251/54 , C07D403/12 , C07D403/14 , A61K31/53 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/06 , A61P11/00 , A61P13/12
CPC分类号： C07D241/46 , C07D251/18 , C07D251/52 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/04
摘要： The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R4, R5, R6, A, B, Y, Z, n, and m are defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are sEH inhibitors and can be used in the treatment of diseases mediated by the sEH enzyme, such as hypertension. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting sEH and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及新型sEH抑制剂及其在治疗由sEH酶介导的疾病中的用途。具体地，本发明涉及式I化合物：其中R1，R2，R4，R5，R6，A，B，Y，Z，n和m定义如下，及其药学上可接受的盐。本发明的化合物是sEH抑制剂，可用于治疗由sEH酶介导的疾病，例如高血压。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物来抑制sEH和与之相关的病症的治疗方法。

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