Organic compounds
    1.
    发明授权
    Organic compounds 有权
    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

    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。

    Organic Compounds
    2.
    发明申请
    Organic Compounds 审中-公开
    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

    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。

    Use of an Adrenal Hormone-Modifying Agent
    4.
    发明申请
    Use of an Adrenal Hormone-Modifying Agent 审中-公开
    使用肾上腺激素修饰剂

    公开(公告)号:US20140171392A1

    公开(公告)日:2014-06-19

    申请号:US14079018

    申请日:2013-11-13

    IPC分类号: C07F9/6506 C07D487/04

    摘要: The present invention relates to a method of treating a disease or disorder characterised 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.

    摘要翻译: 本发明涉及治疗受试者特征为增加的应激激素水平和/或降低雄激素激素水平的疾病或病症的方法,包括向受试者施用治疗有效量的由式(I)表示的化合物:其中 n为1或3; 其中R a和R b独立地为 - (C 1 -C 4)烷基或 - (C 1 -C 4)烷基 - (C 5 -C 7)芳基),其中R a为 并且R b任选被 - (C 1 -C 4)烷氧基取代; R 1,R 2和R 3独立地是氢,卤素,氰基或 - (C 6 -C 10)芳基,其中所述 - (C 6 -C 10)芳基任选被卤素取代,条件是不大于1个, ,R3为氢; R4和R5是氢; 或其药学上可接受的盐。

    Use of an adrenal hormone-modifying agent
    5.
    发明授权
    Use of an adrenal hormone-modifying agent 有权
    使用肾上腺激素调节剂

    公开(公告)号:US08609862B2

    公开(公告)日:2013-12-17

    申请号:US13521548

    申请日:2011-01-13

    IPC分类号: A61K31/4188 C07D235/02

    摘要: The present invention relates to a method of treating a disease or disorder characterised 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.

    摘要翻译: 本发明涉及治疗受试者特征为增加的应激激素水平和/或降低雄激素激素水平的疾病或病症的方法,包括向受试者施用治疗有效量的由式(I)表示的化合物:其中 n为1或3; 其中R a和R b独立地为 - (C 1 -C 4)烷基或 - (C 1 -C 4)烷基 - (C 5 -C 7)芳基),其中R a为 并且R b任选被 - (C 1 -C 4)烷氧基取代; R 1,R 2和R 3独立地是氢,卤素,氰基或 - (C 6 -C 10)芳基,其中所述 - (C 6 -C 10)芳基任选被卤素取代,条件是不大于1个, ,R3为氢; R4和R5是氢; 或其药学上可接受的盐。

    USE OF AN ADRENAL HORMONE-MODIFYING AGENT
    6.
    发明申请
    USE OF AN ADRENAL HORMONE-MODIFYING AGENT 有权
    使用ADRENAL HORMONE-MODIFYING AGENT

    公开(公告)号:US20120295888A1

    公开(公告)日:2012-11-22

    申请号:US13521548

    申请日:2011-01-13

    摘要: The present invention relates to a method of treating a disease or disorder characterised 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.

    摘要翻译: 本发明涉及治疗受试者特征为增加的应激激素水平和/或降低雄激素激素水平的疾病或病症的方法,包括向受试者施用治疗有效量的由式(I)表示的化合物:其中 n为1或3; 其中R a和R b独立地为 - (C 1 -C 4)烷基或 - (C 1 -C 4)烷基 - (C 5 -C 7)芳基),其中R a为 并且R b任选被 - (C 1 -C 4)烷氧基取代; R 1,R 2和R 3独立地是氢,卤素,氰基或 - (C 6 -C 10)芳基,其中所述 - (C 6 -C 10)芳基任选被卤素取代,条件是不大于1个, ,R3为氢; R4和R5是氢; 或其药学上可接受的盐。

    Organic compounds
    7.
    发明授权
    Organic compounds 有权
    有机化合物

    公开(公告)号:US09278969B2

    公开(公告)日:2016-03-08

    申请号:US14459567

    申请日:2014-08-14

    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。

    Organic Compounds
    8.
    发明申请
    Organic Compounds 有权
    有机化合物

    公开(公告)号:US20140357621A1

    公开(公告)日:2014-12-04

    申请号:US14459567

    申请日:2014-08-14

    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。

    Organic compounds
    9.
    发明授权
    Organic compounds 有权
    有机化合物

    公开(公告)号:US08835646B2

    公开(公告)日:2014-09-16

    申请号:US13927514

    申请日:2013-06-26

    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。

    Organic Compounds
    10.
    发明申请
    Organic Compounds 有权
    有机化合物

    公开(公告)号:US20130287789A1

    公开(公告)日:2013-10-31

    申请号:US13927514

    申请日:2013-06-26

    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。