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公开(公告)号：US20170157099A1
公开(公告)日：2017-06-08
申请号：US15039116
申请日：2014-11-24
CPC分类号： A61K31/44 , A61K39/02 , C12Q1/18 , G01N33/5008 , G01N33/94 , G01N2333/24 , G01N2333/986 , G01N2560/00
摘要： Described herein are assays for identifying piericidins and piericidin compositions.
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2.发明申请4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide Derivatives as Potent and Selective Inhibitors of 12-Lipoxygenase 审中-公开4 - （（2-羟基-3-甲氧基苄基）氨基）苯磺酰胺衍生物作为12脂氧合酶的有效和选择性抑制剂公开(公告)号：US20170001955A1
公开(公告)日：2017-01-05
申请号：US15028386
申请日：2014-10-10
申请人： EASTERN VIRGINIA MEDICAL SCHOOL , THE REGENTS OF THE UNIVERSITY OF CALIFORNIA SANTA CRUZ , THE UNITED STATES OF AMERICA OF HEALTH AND HUMAN SERVICES , THOMAS JEFFERSON UNIVERSITY
发明人： David J. MALONEY , Diane K. LUCI , Ajit JADHAV , Theodore HOLMAN , Jerry L. NADLER , Michael HOLINSTAT , David TAYLOR-FISHWICK , Anton SIMEONOV , Adam YASGAR
IPC分类号： C07C311/44 , C07D277/52 , C07D417/12 , C07D263/58 , C07D235/30 , C07D217/22 , C07D277/82 , C07D261/16 , C07D217/02 , C07D211/28 , C07D213/76 , C07D239/69 , C07D295/135 , C07D333/36
CPC分类号： C07C311/44 , C07D211/28 , C07D213/76 , C07D217/02 , C07D217/22 , C07D235/30 , C07D239/69 , C07D261/16 , C07D263/58 , C07D277/52 , C07D277/82 , C07D295/135 , C07D333/36 , C07D417/12
摘要： Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells. The compounds can also be used in methods for treating or preventing a 12-lipoxygenase mediated disease or disorder.
摘要翻译： 人类脂氧合酶（LOX）是涉及催化多不饱和脂肪酸的氧化以提供相应的生物活性羟基二十碳四烯酸（HETE）代谢物的含铁酶的家族。 这些类花生酸信号分子参与许多生理反应，如血小板聚集，炎症和细胞增殖。 由于其在皮肤疾病，糖尿病，血小板止血，血栓形成和癌症中的作用，血小板型12-（S）-LOX（12-LOX）是特别有意义的。 本文公开了4 - （（2-羟基-3-甲氧基苄基）氨基）苯磺酰胺类支架的鉴定和药物化学优化。 该化合物显示针对12-LOX的nM效力和相对于脂氧合酶和环加氧酶的优异选择性。 除具有良好的ADME特性之外，化合物还抑制人血小板中PAR-4诱导的聚集和钙动员，并减少小鼠/人β细胞中的12-HETE。 该化合物也可用于治疗或预防12-脂肪氧合酶介导的疾病或病症的方法。
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公开(公告)号：US20160168137A1
公开(公告)日：2016-06-16
申请号：US15048330
申请日：2016-02-19
申请人： THE GENERAL HOSPITAL CORPORATION , THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, SANTA CRUZ , THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERV
发明人： Klaus VAN LEYEN , Theodore R. HOLMAN , David J. MALONEY , Ajit JADHAV , Anton SIMEONOV , Ganesha RAI
IPC分类号： C07D413/04 , C07D277/56 , C07D263/48
CPC分类号： C07D413/04 , A61K31/421 , A61K31/422 , A61K31/4245 , A61K31/426 , A61K31/4709 , A61K31/4725 , C07D213/85 , C07D239/42 , C07D263/48 , C07D277/42 , C07D277/56
摘要： A systematic screening has revealed a family of compounds that exhibit inhibitory effects on 12/15-lipoxygenase. Accordingly, the present invention relates to the use of these compounds for the inhibition of 12/15-lipoxygenase and for the treatment of a condition involving 12/15-lipoxygenase. Exemplary conditions include, but are not limited to, stroke, periventricular leukomalacia, cardiac arrest with resuscitation, atherosclerosis, Parkinson's disease, Alzheimer's disease, and breast cancer.
摘要翻译： 系统筛选揭示了对12 / 15-脂肪氧合酶具有抑制作用的化合物家族。 因此，本发明涉及这些化合物用于抑制12 / 15-脂肪氧合酶和用于治疗涉及12 / 15-脂肪氧合酶的病症的用途。 示例性的病症包括但不限于中风，脑室周围白质软化症，心脏骤停复苏，动脉粥样硬化，帕金森病，阿尔茨海默病和乳腺癌。
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公开(公告)号：US10752581B2
公开(公告)日：2020-08-25
申请号：US16289994
申请日：2019-03-01
申请人： Eastern Virginia Medical School , The Regents of the University of California Santa Cruz , The United States of America Department of Health and Human Services , Thomas Jefferson University
发明人： David J. Maloney , Diane K. Luci , Ajit Jadhav , Theodore Holman , Jerry L. Nadler , Michael Holinstat , David Taylor-Fishwick , Anton Simeonov , Adam Yasgar , Steven McKenzie
IPC分类号： C07C311/44 , A61P7/02 , C07D235/30 , C07D263/58 , C07D277/82 , C07D277/52 , C07D211/28 , C07D213/76 , C07D217/02 , C07D217/22 , C07D239/69 , C07D261/16 , C07D295/135 , C07D333/36 , C07D417/12
摘要： Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells. The compounds can also be used in methods for treating or preventing a 12-lipoxygenase mediated disease or disorder.
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5.发明申请公开(公告)号：US20190276395A1
公开(公告)日：2019-09-12
申请号：US16289994
申请日：2019-03-01
申请人： Eastern Virginia Medical School , The Regents of the University of California Santa Cruz , The United States of America Department of Health and Human Services , Thomas Jefferson University
发明人： David J. MALONEY , Diane K. LUCI , Ajit JADHAV , Theodore HOLMAN , Jerry L. NADLER , Michael HOLINSTAT , David TAYLOR-FISHWICK , Anton SIMEONOV , Adam YASGAR , Steven MCKENZIE
IPC分类号： C07C311/44 , A61P7/02 , C07D333/36 , C07D239/69 , C07D261/16 , C07D295/135 , C07D417/12 , C07D235/30 , C07D213/76 , C07D217/02 , C07D217/22 , C07D277/52 , C07D277/82 , C07D263/58 , C07D211/28
摘要： Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells. The compounds can also be used in methods for treating or preventing a 12-lipoxygenase mediated disease or disorder.
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公开(公告)号：US20190192492A1
公开(公告)日：2019-06-27
申请号：US16140023
申请日：2018-09-24
CPC分类号： A61K31/44 , A61K39/02 , C12Q1/18 , G01N33/5008 , G01N33/94 , G01N2333/24 , G01N2333/986 , G01N2560/00 , Y02A50/406 , Y02A50/473 , Y02A50/475 , Y02A50/481
摘要： Described herein are assays for identifying piericidins and piericidin compositions.
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公开(公告)号：US10266488B2
公开(公告)日：2019-04-23
申请号：US15028386
申请日：2014-10-10
申请人： Eastern Virginia Medical School , THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, SANTA CRUZ , THE UNITED STATES OF AMERICA DEPARTMENT OF HEALTH AND HUMAN SERVICES , Thomas Jefferson University
发明人： David J. Maloney , Diane K. Luci , Ajit Jadhav , Theodore Holman , Jerry L. Nadler , Michael Holinstat , David Taylor-Fishwick , Anton Simeonov , Adam Yasgar , Steven McKenzie
IPC分类号： C07D277/82 , C07D235/30 , C07D263/58 , C07C311/44 , A61P7/02 , C07D277/52 , C07D211/28 , C07D213/76 , C07D217/02 , C07D217/22 , C07D239/69 , C07D261/16 , C07D295/135 , C07D333/36 , C07D417/12
摘要： Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells. The compounds can also be used in methods for treating or preventing a 12-lipoxygenase mediated disease or disorder.
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公开(公告)号：US10080745B2
公开(公告)日：2018-09-25
申请号：US15039116
申请日：2014-11-24
CPC分类号： A61K31/44 , A61K39/02 , C12Q1/18 , G01N33/5008 , G01N33/94 , G01N2333/24 , G01N2333/986 , G01N2560/00 , Y02A50/406 , Y02A50/473 , Y02A50/475 , Y02A50/481
摘要： Described herein are assays for identifying piericidins and piericidin compositions.
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