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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。
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公开(公告)号:US08143278B2
公开(公告)日:2012-03-27
申请号:US12519703
申请日:2007-12-14
申请人: Qi-Ying Hu , Gary Michael Ksander
发明人: Qi-Ying Hu , Gary Michael Ksander
IPC分类号: C07D401/02 , C07D413/14 , C07D417/04 , A61K31/4709
CPC分类号: C07D401/04 , C07D413/14 , C07D417/04
摘要: The present invention provides a compound of formula I: said compound is inhibitor of aldosterone synthase, and/or 11beta-hydroxylase (CYP11B1), and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase and/or CYP11B1. 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抑制剂和/或11b-羟化酶(CYP11B1),因此可用于治疗由醛固酮合酶和/或CYP11B1介导的病症或疾病。 最后,本发明还提供药物组合物。
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公开(公告)号:US20100093711A1
公开(公告)日:2010-04-15
申请号:US12519703
申请日:2007-12-14
申请人: Qi-Ying Hu , Gary Michael Ksander
发明人: Qi-Ying Hu , Gary Michael Ksander
IPC分类号: A61K31/5415 , A61K31/4709 , C07D403/04 , C07D417/04 , A61P3/04 , A61P9/04 , A61P3/10
CPC分类号: C07D401/04 , C07D413/14 , C07D417/04
摘要: The present invention provides a compound of formula I: said compound is inhibitor of aldosterone synthase, and/or 11beta-hydroxylase (CYP11B1), and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase and/or CYP11B1. 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抑制剂和/或11b-羟化酶(CYP11B1),因此可用于治疗由醛固酮合酶和/或CYP11B1介导的疾病或疾病。 最后,本发明还提供药物组合物。
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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.
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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。
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公开(公告)号:US20100048562A1
公开(公告)日:2010-02-25
申请号:US12519697
申请日:2007-12-14
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。
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公开(公告)号:US20090264420A1
公开(公告)日:2009-10-22
申请号:US12438811
申请日:2007-08-23
申请人: Gary Michael Ksander , Qi-Ying Hu
发明人: Gary Michael Ksander , Qi-Ying Hu
IPC分类号: A61K31/519 , C07D487/04 , A61K31/551 , A61P9/00 , A61P3/00
CPC分类号: C07D487/04
摘要: The present invention provides a compound of formula I: said compound is inhibitor of aldosterone synthase, and/or 11 beta-hydroxylase (CYPL11B1), and/or aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase, aromatase, or CYPL11B1. 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抑制剂和/或11β-羟化酶(CYPL11B1)和/或芳香酶,因此可用于治疗由醛固酮介导的病症或疾病 合酶,芳香酶或CYPL11B1。 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。
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公开(公告)号:US20100240641A1
公开(公告)日:2010-09-23
申请号:US12301935
申请日:2007-05-24
IPC分类号: A61K31/551 , C07D487/04 , A61K31/4985 , A61P25/36 , A61P25/34 , A61P25/00 , A61P5/00 , A61P3/04 , A61P13/12 , A61P9/10 , A61P9/12
CPC分类号: C07D487/04
摘要: The present invention provides a compound of formula I: Said compound is inhibitor of CYP11B2 and/or CYP11B1, and thus can be employed for the treatment of a disorder or disease mediated by CYP11B2 and/or CYP11B1.
摘要翻译: 本发明提供式I化合物:所述化合物是CYP11B2和/或CYP11B1的抑制剂,因此可用于治疗由CYP11B2和/或CYP11B1介导的疾病或疾病。
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公开(公告)号:US20100041722A1
公开(公告)日:2010-02-18
申请号:US12519707
申请日:2007-12-14
申请人: Qi-Ying Hu , Gary Michael Ksander
发明人: Qi-Ying Hu , Gary Michael Ksander
IPC分类号: A61K31/4245 , C07D233/54 , C07D403/04 , C07D271/06 , A61K31/4164 , A61K31/4178 , A61P9/12
CPC分类号: C07D413/04 , C07D233/64 , C07D233/90 , C07D405/04 , C07D413/14
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. 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介导的疾病或疾病。 最后,本发明还提供药物组合物。
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公开(公告)号:US09278969B2
公开(公告)日:2016-03-08
申请号:US14459567
申请日:2014-08-14
申请人: Gary Michael Ksander , Erik Meredith , Lauren Monovich , Julien Papillon , Fariborz Firooznia , Qi-Ying Hu
发明人: Gary Michael Ksander , Erik Meredith , Lauren Monovich , Julien Papillon , Fariborz Firooznia , Qi-Ying Hu
IPC分类号: C07D401/02 , C07D401/10 , A61K31/437 , A61K31/4353 , C07D471/04 , C07D487/04 , A61K31/4188 , A61K31/454 , A61K31/5377 , A61K45/06 , A61K31/55
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。
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