公开(公告)号：US08299077B2

公开(公告)日：2012-10-30

申请号：US12711312

申请日：2010-02-24

申请人： Steven Berthel ,  Fariborz Firooznia ,  Daniel Fishlock ,  Jun-Bae Hong ,  Yan Lou ,  Matthew Lucas ,  Timothy D. Owens ,  Keshab Sarma ,  Zachary Kevin Sweeney ,  Joshua Paul Gergely Taygerly

发明人： Steven Berthel ,  Fariborz Firooznia ,  Daniel Fishlock ,  Jun-Bae Hong ,  Yan Lou ,  Matthew Lucas ,  Timothy D. Owens ,  Keshab Sarma ,  Zachary Kevin Sweeney ,  Joshua Paul Gergely Taygerly

IPC分类号： A61K31/502 ,  C07D237/32

CPC分类号： C07D401/10 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

摘要： This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formula I-III: wherein, variables Q, R, X, X′, Y1, Y2, Y2′, Y3, Y4, Y5, m, and n 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-III and at least one carrier, diluent or excipient.

摘要翻译： 该申请公开了根据通式I-III的5-苯基-1H-吡啶-2-酮，6-苯基-2H-哒嗪-3-酮和5-苯基-1H-吡嗪-2-酮衍生物：其中， 变量Q，R，X，X'，Y1，Y2，Y2'，Y3，Y4，Y5，m和n如本文所述限定Btk。 本文公开的化合物可用于调节Btk的活性并治疗与过量Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病，例如类风湿性关节炎。 还公开了含有式I-III化合物和至少一种载体，稀释剂或赋形剂的组合物。

公开(公告)号：US08115011B2

公开(公告)日：2012-02-14

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： C07D231/00 ,  C07D231/56

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.

公开(公告)号：US08058299B2

公开(公告)日：2011-11-15

申请号：US12113222

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： A61K31/445 ,  A61K31/496 ,  A61K31/422 ,  C07D263/30 ,  C07D413/02

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

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：US20090099201A1

公开(公告)日：2009-04-16

申请号：US12113275

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

CPC分类号： C07D263/34 ,  C07D231/14 ,  C07D401/12 ,  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.

公开(公告)号：US20070270433A1

公开(公告)日：2007-11-22

申请号：US11801972

申请日：2007-05-11

申请人： John A. Brinkman ,  Adrian Wai-Hing Cheung ,  Fariborz Firooznia ,  Kevin Richard Guertin ,  Nicholas Marcopulos ,  Lida Qi ,  Jagdish Kumar Racha ,  Ramakanth Sarabu ,  Jenny Tan ,  Jefferson Wright Tilley

发明人： John A. Brinkman ,  Adrian Wai-Hing Cheung ,  Fariborz Firooznia ,  Kevin Richard Guertin ,  Nicholas Marcopulos ,  Lida Qi ,  Jagdish Kumar Racha ,  Ramakanth Sarabu ,  Jenny Tan ,  Jefferson Wright Tilley

IPC分类号： A61K31/519 ,  A61K31/496 ,  C07D498/02

CPC分类号： C07D513/04 ,  C07D521/00

摘要： There are presented compounds of the formula or a pharmaceutically acceptable salt thereof, which are active adenosine A2B receptor antagonists and useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.

摘要翻译： 呈现下式的化合物或其药学上可接受的盐，它们是活性腺苷A2B受体拮抗剂，可用于治疗糖尿病，糖尿病性视网膜病变，哮喘和腹泻。

公开(公告)号：US20070123504A1

公开(公告)日：2007-05-31

申请号：US11601429

申请日：2006-11-17

申请人： David Bolin ,  Adrian Cheung ,  Fariborz Firooznia ,  Matthew Hamilton ,  Shiming Li ,  Lee McDermott ,  Yimin Qian ,  Weiya Yun

发明人： David Bolin ,  Adrian Cheung ,  Fariborz Firooznia ,  Matthew Hamilton ,  Shiming Li ,  Lee McDermott ,  Yimin Qian ,  Weiya Yun

IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/497 ,  A61K31/427 ,  C07D417/02 ,  C07D413/02

CPC分类号： C07D413/14 ,  C07D413/12 ,  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：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。

公开(公告)号：US08211914B2

公开(公告)日：2012-07-03

申请号：US12638244

申请日：2009-12-15

申请人： David Robert Bolin ,  Adrian Wai-Hing Cheung ,  Fariborz Firooznia ,  Nicholas Marcopulos ,  Yimin Qian

发明人： David Robert Bolin ,  Adrian Wai-Hing Cheung ,  Fariborz Firooznia ,  Nicholas Marcopulos ,  Yimin Qian

IPC分类号： A61K31/445 ,  C07D413/12

CPC分类号： C07D413/12 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14

摘要： Provided herein are amides containing at least a four ring structure, which are inhibitors of diacylglycerol acyltransferase and are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.

摘要翻译： 本文提供了含有至少四环结构的酰胺，其是二酰基甘油酰基转移酶的抑制剂，并且可用于治疗疾病，例如肥胖症，II型糖尿病和代谢综合征。

公开(公告)号：US20120040949A1

公开(公告)日：2012-02-16

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： A61K31/502 ,  C07D413/14 ,  C07D403/14 ,  C07D487/10 ,  A61P37/00 ,  C07D491/107 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/501 ,  A61P29/00 ,  C07D401/14 ,  C07D417/14

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.

摘要翻译： 本申请公开了根据通式I的6-（2-羟基甲基 - 苯基）-2-甲基-2H-哒嗪-3-酮衍生物：其中，变量X，R和Y4如本文所述定义，其抑制Btk 。 本文公开的化合物可用于调节Btk的活性并治疗与过量Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎性和自身免疫疾病，例如类风湿性关节炎。 还公开了含有式I化合物和至少一种载体，稀释剂或赋形剂的组合物。

公开(公告)号：US07714126B2

公开(公告)日：2010-05-11

申请号：US11601429

申请日：2006-11-17

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

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

IPC分类号： C07D279/00

CPC分类号： C07D413/14 ,  C07D413/12 ,  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。