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1. 发明授权

US09452998B2 Protein kinase C inhibitors and methods of their use 有权
标题翻译：蛋白激酶C抑制剂及其使用方法
公开(公告)号：US09452998B2
公开(公告)日：2016-09-27
申请号：US14818778
申请日：2015-08-05
申请人： Michael Scott Visser , Michael Joseph Luzzio , Julien Papillon
发明人： Michael Scott Visser , Michael Joseph Luzzio , Julien Papillon
IPC分类号： C07D401/14 , A61K31/497 , C07D413/14
CPC分类号： C07D401/14 , A61K31/497 , C07D413/14
摘要： PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.
摘要翻译：公开了PKC抑制剂。 PKC抑制剂可用于治疗PKC相关疾病，包括某些癌症。 PKC抑制剂在较低剂量下具有改善的功效以实现肿瘤消退，改善效力，PK分布，吸收，胃肠道耐受和激酶选择性。

2. 发明授权

US09434754B2 Use of an adrenal hormone-modifying agent 有权
标题翻译：使用肾上腺激素调节剂
公开(公告)号：US09434754B2
公开(公告)日：2016-09-06
申请号：US14079018
申请日：2013-11-13
申请人： Qi-Ying Hu , Gary Michael Ksander , Erik Meredith , Lauren G Monovich , Julien Papillon , Christoph Schumacher
发明人： Qi-Ying Hu , Gary Michael Ksander , Erik Meredith , Lauren G Monovich , Julien Papillon , Christoph Schumacher
IPC分类号： C07D487/04 , C07F9/6506 , A61K31/4188 , A61K31/55
CPC分类号： C07F9/6506 , A61K31/4188 , A61K31/55 , A61P5/00 , C07D487/04
摘要： The present invention relates to a method of treating a disease or disorder characterized by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I):wherein n is 1 or 3; R is hydrogen or —C(O)N(Ra)(Rb) wherein Ra and Rb are independently —(C1-C4) alkyl, or —(C1-C4) alkyl-(C5-C7) aryl, wherein each of Ra and Rb is optionally substituted by —(C1-C4) alkoxy; R1, R2, and R3, are independently hydrogen, halogen, cyano or —(C6-C10) aryl, wherein said —(C6-C10) aryl is optionally substituted by halogen, with the proviso that no more than one of R1, R2, and R3 is hydrogen; and R4 and R5 are hydrogen; or a pharmaceutically acceptable salt thereof.

3. 发明授权

US09242963B2 Organic compounds 有权
标题翻译：有机化合物
公开(公告)号：US09242963B2
公开(公告)日：2016-01-26
申请号：US14677260
申请日：2015-04-02
申请人： Christopher Michael Adams , Qi-Ying Hu , Leslie Wighton McQuire , Julien Papillon
发明人： Christopher Michael Adams , Qi-Ying Hu , Leslie Wighton McQuire , Julien Papillon
IPC分类号： C07D401/04 , A61K31/4439 , A61K45/06 , C07D401/14 , C07D213/61 , C07D401/06 , C07D401/12
CPC分类号： C07D401/14 , A61K31/4439 , A61K45/06 , C07D213/61 , C07D401/04 , C07D401/06 , C07D401/12 , A61K2300/00
摘要： The present invention provides novel organic compounds of Formula (I): methods of use, and pharmaceutical compositions thereof.
摘要翻译：本发明提供式（I）的新型有机化合物：使用方法及其药物组合物。

4. 发明申请

US20150210672A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：US20150210672A1
公开(公告)日：2015-07-30
申请号：US14677260
申请日：2015-04-02
申请人： Christopher Michael ADAMS , Qi-Ying HU , Leslie Wighton MCQUIRE , Julien Papillon
发明人： Christopher Michael ADAMS , Qi-Ying HU , Leslie Wighton MCQUIRE , Julien Papillon
IPC分类号： C07D401/14 , A61K31/4439 , A61K45/06 , C07D401/04
CPC分类号： C07D401/14 , A61K31/4439 , A61K45/06 , C07D213/61 , C07D401/04 , C07D401/06 , C07D401/12 , A61K2300/00
摘要： The present invention provides novel organic compounds of Formula (I): methods of use, and pharmaceutical compositions thereof.
摘要翻译：本发明提供式（I）的新型有机化合物：使用方法及其药物组合物。

5. 发明授权

US08519134B2 Aryl-pyridine derivatives as aldosterone synthase inhibitors 有权
标题翻译：芳基吡啶衍生物作为醛固酮合酶抑制剂
公开(公告)号：US08519134B2
公开(公告)日：2013-08-27
申请号：US13509646
申请日：2010-11-16
申请人： Martin Allan , Sylvie Chamoin , Qi-Ying Hu , Hidetomo Imase , Julien Papillon
发明人： Martin Allan , Sylvie Chamoin , Qi-Ying Hu , Hidetomo Imase , Julien Papillon
IPC分类号： C07D221/02 , A61K31/44
CPC分类号： C07D213/57 , C07D213/30 , C07D213/61 , C07D401/04 , C07D405/04 , C07D409/04
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5和n如本文所定义。本发明还涉及一种制备本发明化合物的方法及其治疗用途。本发明还提供药理活性剂和药物组合物的组合。

6. 发明授权

US08314097B2 Organic compounds 有权
标题翻译：有机化合物
公开(公告)号：US08314097B2
公开(公告)日：2012-11-20
申请号：US11508445
申请日：2006-08-23
申请人： Gary Michael Ksander , Erik Meredith , Lauren G. Monovich , Julien Papillon , Fariborz Firooznia , Qi-Ying Hu
发明人： Gary Michael Ksander , Erik Meredith , Lauren G. Monovich , Julien Papillon , Fariborz Firooznia , Qi-Ying Hu
IPC分类号： A61K31/535 , A61K31/445 , A61K31/415 , A61P9/00 , C07D413/00 , C07D211/32 , C07D235/02 , C07D487/10 , C07D403/00
CPC分类号： C07D471/04 , A61K31/4188 , A61K31/437 , A61K31/454 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D487/04
摘要： The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy. Finally, the present invention also provides a pharmaceutical composition.
摘要翻译：本发明提供式I化合物：所述化合物是醛固酮合成酶和芳香酶的抑制剂，因此可用于治疗由醛固酮合成酶或芳香酶介导的病症或疾病。因此，式I化合物可用于治疗低钾血症，高血压，充血性心力衰竭，心房颤动，肾衰竭，特别是慢性肾衰竭，再狭窄，动脉粥样硬化，综合征X，肥胖症，肾病，心肌梗塞后，冠状动脉心脏病，炎症，胶原蛋白形成增加，纤维化如心脏或心肌纤维化，以及高血压和内皮功能障碍后重塑，男子乳腺发育不良，骨质疏松症，前列腺癌，子宫内膜异位症，子宫肌瘤，功能障碍性子宫出血，子宫内膜增生，多囊卵巢疾病，不育症，纤维囊性乳腺疾病，乳腺癌和纤维囊性乳腺病。最后，本发明还提供药物组合物。

7. 发明申请

US20100048562A1 ORGANIC COMPOUNDS 失效
标题翻译：有机化合物
公开(公告)号：US20100048562A1
公开(公告)日：2010-02-25
申请号：US12519697
申请日：2007-12-14
申请人： Christopher Adams , Qi-Ying Hu , Gary Michael Ksander , Julien Papillon
发明人： Christopher Adams , Qi-Ying Hu , Gary Michael Ksander , Julien Papillon
IPC分类号： A61K31/5377 , C07D233/22 , A61K31/415 , C07D413/02
CPC分类号： C07D233/64 , C07D233/58 , C07D233/88 , C07D233/90 , C07D401/04 , C07D405/04 , C07D409/04 , C07D409/10 , C07D413/04
摘要： The present invention provides a compound of formula I: said compound is inhibitor of aldosterone synthase (CYP11B2), and/or 11 beta-hydroxylase (CYP11B1), and/or aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase, aromatase, or CYP11B1. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, increased formation of collagen, fibrosis and remodeling following hypertension and endothelial dysfunction. Finally, the present invention also provides a pharmaceutical composition.
摘要翻译：本发明提供式I化合物：所述化合物是醛固酮合酶（CYP11B2）和/或11β-羟化酶（CYP11B1）和/或芳香酶的抑制剂，因此可用于治疗疾病或疾病由醛固酮合酶，芳香酶或CYP11B1介导。因此，式I化合物可用于治疗低钾血症，高血压，充血性心力衰竭，肾衰竭，特别是慢性肾功能衰竭，再狭窄，动脉粥样硬化，X综合症，肥胖症，肾病，心肌梗塞后，冠心病增加胶原蛋白的形成，纤维化和高血压和内皮功能障碍后的重塑。最后，本发明还提供药物组合物。

8. 发明申请

US20120277215A1 Organic Compounds 审中-公开
标题翻译：有机化合物
公开(公告)号：US20120277215A1
公开(公告)日：2012-11-01
申请号：US13540113
申请日：2012-07-02
申请人： Gary Michael Ksander , Erik Meredith , Lauren G. Monovich , Julien Papillon , Fariborz Firooznia , Qi-Ying Hu
发明人： Gary Michael Ksander , Erik Meredith , Lauren G. Monovich , Julien Papillon , Fariborz Firooznia , Qi-Ying Hu
IPC分类号： C07D487/04 , A61K31/5377 , A61K31/454 , C07D487/20 , C07D471/04 , A61K31/437 , A61K31/55 , A61P9/12 , A61P9/04 , A61P13/12 , A61P9/10 , A61P3/00 , A61P3/04 , A61P9/00 , A61P29/00 , A61P19/10 , A61P35/00 , A61P15/08 , A61K31/4188
CPC分类号： C07D471/04 , A61K31/4188 , A61K31/437 , A61K31/454 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D487/04
摘要： The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy. Finally, the present invention also provides a pharmaceutical composition.
摘要翻译：本发明提供式I化合物：所述化合物是醛固酮合成酶和芳香酶的抑制剂，因此可用于治疗由醛固酮合成酶或芳香酶介导的病症或疾病。因此，式I化合物可用于治疗低钾血症，高血压，充血性心力衰竭，心房颤动，肾衰竭，特别是慢性肾衰竭，再狭窄，动脉粥样硬化，综合征X，肥胖症，肾病，心肌梗塞后，冠状动脉心脏病，炎症，胶原蛋白形成增加，纤维化如心脏或心肌纤维化，以及高血压和内皮功能障碍后重塑，男子乳腺发育不良，骨质疏松症，前列腺癌，子宫内膜异位症，子宫肌瘤，功能障碍性子宫出血，子宫内膜增生，多囊卵巢疾病，不育症，纤维囊性乳腺疾病，乳腺癌和纤维囊性乳腺病。最后，本发明还提供药物组合物。

9. 发明授权

US08153674B2 Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US08153674B2
公开(公告)日：2012-04-10
申请号：US12295155
申请日：2007-03-27
申请人： Christopher Adams , Julien Papillon , Gary Michael Ksander
发明人： Christopher Adams , Julien Papillon , Gary Michael Ksander
IPC分类号： C07D405/02 , A61K31/4178
CPC分类号： C07D405/04
摘要： The present invention provides a compound of formula (I): said compound is inhibitor of aldosterone synthase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosderosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, increased formation of collagen, cardiac fibrosis and remodeling following hypertension and endothelial dysfunction. Finally, the present invention also provides a pharmaceutical composition.
摘要翻译：本发明提供式（I）化合物：所述化合物是醛固酮合成酶的抑制剂，因此可用于治疗由醛固酮合成酶介导的病症或疾病。因此，式I化合物可用于治疗低钾血症，高血压，充血性心力衰竭，肾功能衰竭，特别是慢性肾衰竭，再狭窄，动脉粥样硬化，X综合征，肥胖症，肾病，心肌梗塞后，冠心病，增加胶原蛋白的形成，心脏纤维化和高血压和内皮功能障碍后重建。最后，本发明还提供药物组合物。

10. 发明申请

US20100261698A1 ORGANIC COMPOUNDS 有权
标题翻译：有机化合物
公开(公告)号：US20100261698A1
公开(公告)日：2010-10-14
申请号：US12492383
申请日：2009-06-26
申请人： Christopher Adams , Qi-Ying Hu , Leslie Wighton McQuire , Julien Papillon
发明人： Christopher Adams , Qi-Ying Hu , Leslie Wighton McQuire , Julien Papillon
IPC分类号： A61K31/4439 , C07D401/04 , C07D413/14 , A61K31/5377 , C07D417/14 , A61K31/541 , A61P1/16 , A61P13/12 , A61P9/12 , A61P9/10 , A61P9/06
CPC分类号： C07D401/14 , A61K31/4439 , A61K45/06 , C07D213/61 , C07D401/04 , C07D401/06 , C07D401/12 , A61K2300/00
摘要： The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof.
摘要翻译：本发明提供式I的新型有机化合物：使用方法及其药物组合物。

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