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公开(公告)号：US20070270433A1
公开(公告)日：2007-11-22
申请号：US11801972
申请日：2007-05-11
Applicant: 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
Inventor： 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: A61K31/519 , A61K31/496 , C07D498/02
CPC classification number: C07D513/04 , C07D521/00
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US08501732B2
公开(公告)日：2013-08-06
申请号：US13546039
申请日：2012-07-11
Applicant: 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
Inventor： 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: 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 classification number: C07D215/48 , C07D215/233 , C07D401/12 , C07D405/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US08324385B2
公开(公告)日：2012-12-04
申请号：US12581950
申请日：2009-10-20
Applicant: David Robert Bolin , Adrian Wai-Hing Cheung , Matthew Michael Hamilton , Nicholas Marcopulos , Lee Apostle McDermott , Yimin Qian
Inventor： David Robert Bolin , Adrian Wai-Hing Cheung , Matthew Michael Hamilton , Nicholas Marcopulos , Lee Apostle McDermott , Yimin Qian
IPC: C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00
CPC classification number: C07D401/04 , C07D213/75 , C07D213/82 , C07D277/46 , C07D277/82 , C07D295/155 , C07D295/185 , C07D295/205 , C07D333/54 , C07D401/12
Abstract: Provided herein are compounds of the formula (I): were RI is phenyl, R2 is hydrogen, halogen or lower alkyl, X is carbon on nitrogen, and R3 is isoquinoline, -amino, or a -4- to 6-membered heterocycloalkyl ring and pharmaceutically acceptable salts thereof, which are active as DGAT inhibitors and therefore find uses in treatment of diseases associated with abnormal metabolism of trigliceride. such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
Abstract translation: 本文提供了式（I）的化合物：R 1是苯基，R 2是氢，卤素或低级烷基，X是氮上的碳，R 3是异喹啉， - 氨基或4-至6-元杂环烷基环 其药学上可接受的盐，其作为DGAT抑制剂是有活性的，因此可用于治疗与三联嘧啶异常代谢有关的疾病。 例如肥胖，II型糖尿病和代谢综合征。
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Patent Agency Ranking
公开(公告)号：US08211914B2
公开(公告)日：2012-07-03
申请号：US12638244
申请日：2009-12-15
Applicant: David Robert Bolin , Adrian Wai-Hing Cheung , Fariborz Firooznia , Nicholas Marcopulos , Yimin Qian
Inventor： David Robert Bolin , Adrian Wai-Hing Cheung , Fariborz Firooznia , Nicholas Marcopulos , Yimin Qian
IPC: A61K31/445 , C07D413/12
CPC classification number: C07D413/12 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US20100113782A1
公开(公告)日：2010-05-06
申请号：US12581950
申请日：2009-10-20
Applicant: David Robert Bolin , Adrian Wai-Hing Cheung , Matthew Michael Hamilton , Nicholas Marcopulos , Lee Apostle McDermott , Yimin Qian
Inventor： David Robert Bolin , Adrian Wai-Hing Cheung , Matthew Michael Hamilton , Nicholas Marcopulos , Lee Apostle McDermott , Yimin Qian
IPC: C07D241/04 , C07D401/04
CPC classification number: C07D401/04 , C07D213/75 , C07D213/82 , C07D277/46 , C07D277/82 , C07D295/155 , C07D295/185 , C07D295/205 , C07D333/54 , C07D401/12
Abstract: Provided herein are compounds of the formula (I): were R1 is phenyl, R2 is hydrogen, halogen or lower alkyl, X is carbon on nitrogen, and R3 is isoquinoline, -amino, or a 4- to 6-membered heterocycloalkyl ring and pharmaceutically acceptable salts thereof, which are active as DGAT inhibitors and therefore find uses in treatment of diseases associated with abnormal metabolism of triglicerides such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
Abstract translation: 本文提供式（I）化合物：其中R 1为苯基，R 2为氢，卤素或低级烷基，X为氮上的碳，R 3为异喹啉， - 氨基或4-至6-元杂环烷基环， 其药学上可接受的盐，其作为DGAT抑制剂是有活性的，因此可用于治疗与三联嘧啶类例如肥胖症，II型糖尿病和代谢综合征的异常代谢相关的疾病。
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公开(公告)号：US20130018043A1
公开(公告)日：2013-01-17
申请号：US13546039
申请日：2012-07-11
Applicant: 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
Inventor： 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: C07D413/14 , A61K31/5377 , C07D471/04 , A61K31/4375 , C07D401/14 , A61K31/55 , A61K31/551 , A61P29/00 , A61P11/06 , A61P3/10 , A61P25/28 , A61P25/16 , A61P9/10 , A61P35/00 , A61P35/02 , A61P13/12 , A61K31/4709
CPC classification number: C07D215/48 , C07D215/233 , C07D401/12 , C07D405/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
Abstract: 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.
Abstract translation: 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。
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![Substituted thiazolo[5,4-d]pyrimidine urea derivatives](/abs-image/US/2011/05/24/US07947692B2/abs.jpg.150x150.jpg)
公开(公告)号：US07947692B2
公开(公告)日：2011-05-24
申请号：US11801972
申请日：2007-05-11
Applicant: 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
Inventor： 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: C07D487/04 , C07D513/04 , A61K31/519 , A61P3/10 , A61P11/06 , A61K31/4353 , A61K31/496 , A61K31/5355 , A61K31/45
CPC classification number: C07D513/04 , C07D521/00
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US20100152445A1
公开(公告)日：2010-06-17
申请号：US12638244
申请日：2009-12-15
Applicant: David Robert Bolin , Adrian Wai-Hing Cheung , Fariborz Firooznia , Nicholas Marcopulos , Yimin Qian
Inventor： David Robert Bolin , Adrian Wai-Hing Cheung , Fariborz Firooznia , Nicholas Marcopulos , Yimin Qian
IPC: C07D413/14 , C07D413/12 , C07D401/14
CPC classification number: C07D413/12 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14
Abstract: 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.
Abstract translation: 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。
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