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。

公开(公告)号：US20140357621A1

公开(公告)日：2014-12-04

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： C07D471/04 ,  A61K31/55 ,  A61K45/06 ,  A61K31/437 ,  C07D487/04 ,  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。

公开(公告)号：US08835646B2

公开(公告)日：2014-09-16

申请号：US13927514

申请日：2013-06-26

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： A61K31/4188 ,  C07D487/04 ,  A61K31/5377 ,  A61K45/06 ,  C07D471/04 ,  A61K31/454

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。

公开(公告)号：US20130287789A1

公开(公告)日：2013-10-31

申请号：US13927514

申请日：2013-06-26

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： C07D487/04 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/4188 ,  A61K45/06

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。

公开(公告)号：US07713991B2

公开(公告)日：2010-05-11

申请号：US11739290

申请日：2007-04-24

申请人： Fariborz Firooznia

发明人： Fariborz Firooznia

IPC分类号： A01N43/42 ,  A61K31/44

CPC分类号： C07D471/04

摘要： Compounds of the formula (I) provide pharmacological agents which are inhibitors of the P450 enzyme, aldosterone synthase, and thus may be employed for the treatment of aldosterone mediated conditions. Accordingly, the compounds of formula (I) may be employed for prevention, delay of progression, or 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. Preferred are the compounds of formula (I) which are selective inhibitors of aldosterone synthase devoid of undesirable side effects due to general inhibition of cytochrome P450 enzymes.

摘要翻译： 式（I）的化合物提供作为P450酶抑制剂醛固酮合成酶的药理学试剂，因此可用于治疗醛固酮介导的病症。 因此，式（I）化合物可用于预防，延缓进展或治疗低钾血症，高血压，充血性心力衰竭，肾功能衰竭，特别是慢性肾功能衰竭，再狭窄，动脉粥样硬化，综合征X，肥胖症，肾病 ，心肌梗塞后，冠心病，胶原增多，纤维化和高血压和内皮功能障碍后重塑。 由于通常抑制细胞色素P450酶，优选式（I）化合物是醛固酮合酶的选择性抑制剂，没有不希望的副作用。

公开(公告)号：US20090170864A1

公开(公告)日：2009-07-02

申请号：US12113261

申请日：2008-05-01

申请人： David Robert Bolin ,  Adrian Wai-Hing Cheung ,  Fariborz Firooznia ,  Matthew Michael Hamilton ,  Lee Apostle McDermott ,  Yimin Qian ,  Jenny Tan ,  Weiya Yun

发明人： David Robert Bolin ,  Adrian Wai-Hing Cheung ,  Fariborz Firooznia ,  Matthew Michael Hamilton ,  Lee Apostle McDermott ,  Yimin Qian ,  Jenny Tan ,  Weiya Yun

IPC分类号： C07D413/14 ,  C07D413/02 ,  C07D417/02 ,  C07D417/14 ,  A61K31/496 ,  A61K31/4439 ,  A61P3/00 ,  A61P3/10 ,  A61K31/421 ,  C07D263/34

CPC分类号： C07D263/34 ,  C07D231/14 ,  C07D277/56 ,  C07D307/68 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

摘要： Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.

摘要翻译： 本文提供式（I）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗疾病，例如肥胖症，II型糖尿病和代谢综合征。

公开(公告)号：US20090105273A1

公开(公告)日：2009-04-23

申请号：US12113295

申请日：2008-05-01

申请人： David Robert Bolin ,  Adrian Wai-Hing Cheung ,  Fariborz Firooznia ,  Matthew Michael Hamilton ,  Lee Aopstle McDermott ,  Yimin Qian ,  Jenny Tan ,  Weiya Yun

发明人： David Robert Bolin ,  Adrian Wai-Hing Cheung ,  Fariborz Firooznia ,  Matthew Michael Hamilton ,  Lee Aopstle McDermott ,  Yimin Qian ,  Jenny Tan ,  Weiya Yun

IPC分类号： A61K31/497 ,  C07D263/36 ,  A61K31/422 ,  C07D401/02 ,  A61P3/10 ,  A61K31/445 ,  C07D413/06

CPC分类号： C07D263/34 ,  C07D231/14 ,  C07D249/06 ,  C07D277/56 ,  C07D307/68 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

摘要： Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.

公开(公告)号：US07223866B2

公开(公告)日：2007-05-29

申请号：US10534631

申请日：2003-11-17

申请人： Fariborz Firooznia

发明人： Fariborz Firooznia

IPC分类号： C07D471/02 ,  C07D491/02 ,  C07D498/02 ,  C07D513/02 ,  C07D515/02

CPC分类号： C07D471/04

摘要： Compounds of the formula (I) provide pharmacological agents which are inhibitors of the P450 enzyme, aldosterone synthase, and thus may be employed for the treatment of aldosterone mediated conditions. Accordingly, the compounds of formula (I) may be employed for prevention, delay of progression, or 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. Preferred are the compounds of formula (I) which are selective inhibitors of aldosterone synthase devoid of undesirable side effects due to general inhibition of cytochrome P450 enzymes.

摘要翻译： 式（I）的化合物提供作为P450酶抑制剂醛固酮合成酶的药理学试剂，因此可用于治疗醛固酮介导的病症。 因此，式（I）化合物可用于预防，延缓进展或治疗低钾血症，高血压，充血性心力衰竭，肾功能衰竭，特别是慢性肾功能衰竭，再狭窄，动脉粥样硬化，综合征X，肥胖症，肾病 ，心肌梗塞后，冠心病，胶原增多，纤维化和高血压和内皮功能障碍后重塑。 由于通常抑制细胞色素P450酶，优选式（I）化合物是醛固酮合酶的选择性抑制剂，没有不希望的副作用。

公开(公告)号：US06426354B1

公开(公告)日：2002-07-30

申请号：US09690061

申请日：2000-10-16

申请人： Cynthia Anne Fink ,  Fariborz Firooznia

发明人： Cynthia Anne Fink ,  Fariborz Firooznia

IPC分类号： A61K3144

CPC分类号： C07D271/06 ,  A61K31/44 ,  C07D213/55 ,  C07D263/32 ,  C07D277/30 ,  C07D333/24 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14

摘要： Novel thiol derivatives of formula I or of the formula Ia wherein the variables have the meanings as defined hereinbefore.

摘要翻译： 式Ior的式Ior的新型硫醇衍生物，其变量具有如上所定义的含义。

公开(公告)号：US08481540B2

公开(公告)日：2013-07-09

申请号：US13207481

申请日：2011-08-11

申请人： Steven Joseph Berthel ,  Roland Joseph Billedeau ,  Christine E. Brotherton-Pleiss ,  Fariborz Firooznia ,  Stephen Deems Gabriel ,  Xiaochun Han ,  Ramona Hilgenkamp ,  Saul Jaime-Figueroa ,  Buelent Kocer ,  Francisco Javier Lopez-Tapia ,  Yan Lou ,  Lucja Orzechowski ,  Timothy D. Owens ,  Jenny Tan ,  Peter Michael Wovkulich

发明人： Steven Joseph Berthel ,  Roland Joseph Billedeau ,  Christine E. Brotherton-Pleiss ,  Fariborz Firooznia ,  Stephen Deems Gabriel ,  Xiaochun Han ,  Ramona Hilgenkamp ,  Saul Jaime-Figueroa ,  Buelent Kocer ,  Francisco Javier Lopez-Tapia ,  Yan Lou ,  Lucja Orzechowski ,  Timothy D. Owens ,  Jenny Tan ,  Peter Michael Wovkulich

IPC分类号： A01N43/58 ,  A61K31/50 ,  C07D237/00

CPC分类号： C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107

摘要： This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, and Y4, are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.