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1. 发明申请

US20100222325A1 Inhibitors of Bruton's Tyrosine Kinase 有权
标题翻译： Bruton酪氨酸激酶抑制剂
公开(公告)号：US20100222325A1
公开(公告)日：2010-09-02
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： A61K31/4725 , C07D413/14 , C07D401/14 , C07D401/10 , A61P29/00 , A61P37/00 , A61K31/5377 , A61K31/496 , A61K31/502
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 Formulae 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 Formulae I-III and at least one carrier, diluent or excipient.
摘要翻译：本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。

2. 发明授权

US08299077B2 Inhibitors of Bruton's tyrosine kinase 有权
标题翻译： Bruton酪氨酸激酶抑制剂
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。

3. 发明授权

US08481540B2 Inhibitors of bruton's tyrosine kinase 失效
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.

4. 发明申请

US20120040949A1 Inhibitors of Bruton's Tyrosine Kinase 失效
标题翻译： Bruton酪氨酸激酶抑制剂
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。

5. 发明授权

US08501732B2 Aminomethyl quinolone compounds 有权
标题翻译：氨甲基喹诺酮化合物
公开(公告)号：US08501732B2
公开(公告)日：2013-08-06
申请号：US13546039
申请日：2012-07-11
申请人： Joseph A. Bilotta , Adrian Wai-Hing Cheung , Fariborz Firooznia , Kevin Richard Guertin , Stuart Hayden , Nancy-Ellen Haynes , Christine M. Lukacs-Lesburg , Nicholas Marcopulos , Eric Mertz , Lida Qi , Yimin Qian , Sung-Sau So , Jenny Tan , Kshitij C. Thakkar
发明人： Joseph A. Bilotta , Adrian Wai-Hing Cheung , Fariborz Firooznia , Kevin Richard Guertin , Stuart Hayden , Nancy-Ellen Haynes , Christine M. Lukacs-Lesburg , Nicholas Marcopulos , Eric Mertz , Lida Qi , Yimin Qian , Sung-Sau So , Jenny Tan , Kshitij C. Thakkar
IPC分类号： A61K31/55 , A61K31/551 , A61K31/5375 , A61K31/5377 , A61K31/4427 , A61K31/435 , A61K31/47 , C07D243/08 , C07D401/02 , C07D413/02 , C07D413/14 , C07D471/00 , C07D215/00
CPC分类号： C07D215/48 , C07D215/233 , C07D401/12 , C07D405/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
摘要翻译：本发明涉及JNK抑制剂和用于抑制JNK和治疗JNK介导的病症的相应方法，制剂和组合物。本申请公开了如下式I所述的JNK抑制剂：其中变量如本文所定义。本文公开的化合物和组合物可用于调节JNK的活性并治疗与JNK活性相关的疾病。公开了用于抑制JNK和治疗JNK介导的病症等的方法和制剂，以及本文公开的化合物，以及制备所述化合物的方法和相应的组合物。

6. 发明授权

US08188090B2 Naphthylacetic acids 失效
标题翻译：萘乙酸
公开(公告)号：US08188090B2
公开(公告)日：2012-05-29
申请号：US12614497
申请日：2009-11-09
申请人： Fariborz Firooznia , Tai-An Lin , Sung-Sau So , Baoxia Wang , HongYing Yun
发明人： Fariborz Firooznia , Tai-An Lin , Sung-Sau So , Baoxia Wang , HongYing Yun
IPC分类号： A61K31/445 , A61K31/4965 , A01N43/40 , C07D241/04 , C07D295/00 , C07D205/00
CPC分类号： C07D295/192 , C07D213/74 , C07D239/42 , C07D295/18 , C07D401/12 , C07D487/10
摘要： The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein X, Q and R1-R3 are defined in the detailed description and claims. The invention is also concerned with the compounds of formula Z: and pharmaceutically acceptable salts and esters thereof, wherein R1-R3 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I and Z as well as pharmaceutical compositions containing such compounds. The compounds of formula I and Z are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
摘要翻译：本发明涉及式I化合物及其药学上可接受的盐和酯，其中X，Q和R 1 -R 3在详细描述和权利要求书中定义。本发明还涉及式Z化合物及其药学上可接受的盐和酯，其中R1-R3在详细描述和权利要求书中定义。此外，本发明涉及制备和使用式I和Z化合物的方法以及含有这些化合物的药物组合物。式I和Z的化合物是CRTH2受体的拮抗剂或部分激动剂，可用于治疗与该受体相关的疾病和病症如哮喘。

7. 发明授权

US08153644B2 Diacylglycerol acyltransferase inhibitors 有权
标题翻译：二酰基甘油酰基转移酶抑制剂
公开(公告)号：US08153644B2
公开(公告)日：2012-04-10
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： A61K31/506 , A61K31/4525 , A61K31/443 , A61K31/421 , C07D239/34 , C07D239/42 , C07D211/22 , C07D413/14 , C07D263/34
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.
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。

8. 发明申请

US20100168419A1 Diacylglycerol Acyltransferase Inhibitors 审中-公开
标题翻译：二酰基甘油酰基转移酶抑制剂
公开(公告)号：US20100168419A1
公开(公告)日：2010-07-01
申请号：US12722065
申请日：2010-03-11
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： C07D417/14 , C07D413/14 , C07D413/12 , C07D239/48 , C07D417/12 , C07D401/12
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。

9. 发明申请

US20070197582A1 IMIDAZO[[1, 5-A] PYRIDINE DERIVATIVES AND METHODS FOR TREATING ALDOSTERONE MEDIATED DISEASES 失效
标题翻译：咪唑并[[1,5-A]吡啶衍生物和治疗阿托品酮介导性疾病的方法
公开(公告)号：US20070197582A1
公开(公告)日：2007-08-23
申请号：US11739290
申请日：2007-04-24
申请人： Fariborz Firooznia
发明人： Fariborz Firooznia
IPC分类号： A61K31/4745 , C07D471/02
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。

10. 发明授权

US06423727B1 Certain thiol inhibitors of endothelin-converting enzyme 失效
标题翻译：某些内皮素转化酶的硫醇抑制剂
公开(公告)号：US06423727B1
公开(公告)日：2002-07-23
申请号：US09690060
申请日：2000-10-16
申请人： Stéphane De Lombaert , Cynthia Anne Fink , Fariborz Firooznia , Denton Wade Hoyer , Arco Yingcheu Jeng
发明人： Stéphane De Lombaert , Cynthia Anne Fink , Fariborz Firooznia , Denton Wade Hoyer , Arco Yingcheu Jeng
IPC分类号： A01N4340
CPC分类号： C07D239/26 , A61K31/165 , A61K31/44 , A61K31/47 , C07D209/20 , C07D213/56 , C07D307/54 , C07D307/81 , C07D333/24 , C07D333/60
摘要： Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula wherein the variables have the meanings as defined hereinbefore.
摘要翻译：作为内皮素转化酶抑制剂公开的是所述变体具有如上所定义含义的化合物。

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