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公开(公告)号：US09359358B2
公开(公告)日：2016-06-07
申请号：US13588776
申请日：2012-08-17
Applicant: James D. Rodgers , Argyrios G. Arvanitis
Inventor： James D. Rodgers , Argyrios G. Arvanitis
IPC: C07D487/04 , A61K31/519 , A61P35/00 , A61P35/02 , C07D473/04
CPC classification number: C07D473/04 , C07D487/04
Abstract: The present invention provides cyclohexyl azetidine derivatives of Formula I: or pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Abstract translation: 本发明提供式I的环己基氮杂环丁烷衍生物或其药学上可接受的盐，以及它们的组合物和使用方法，其调节Janus激酶（JAK）的活性，并且可用于治疗与 JAK包括例如炎症性疾病，自身免疫性疾病，癌症和其它疾病。
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![Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors](/abs-image/US/2016/02/02/US09249145B2/abs.jpg.150x150.jpg)
2.发明授权Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors 有权吡唑-4-基 - 吡咯并[2,3-d]嘧啶的杂环衍生物作为甘油激酶抑制剂公开(公告)号：US09249145B2
公开(公告)日：2016-02-02
申请号：US12872925
申请日：2010-08-31
Applicant: James D. Rodgers , Yun-Long Li , Stacey Shepard , Haisheng Wang
Inventor： James D. Rodgers , Yun-Long Li , Stacey Shepard , Haisheng Wang
IPC: C07D487/04 , A61K31/519 , A61P35/00 , A61P35/02 , A61P35/04 , A61K31/551 , A61P37/06 , A61P29/00 , A61P17/00 , A61P19/00
CPC classification number: C07D487/04
Abstract: The present invention provides heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines of Formula I: and pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Abstract translation: 本发明提供式I的吡唑-4-基 - 吡咯并[2,3-d]嘧啶的杂环衍生物及其药学上可接受的盐，以及它们的组合物和使用方法，其调节Janus激酶的活性 JAK），并且可用于治疗与JAK的活性相关的疾病，包括例如炎症性疾病，自身免疫性疾病，癌症和其他疾病。
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![Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors](/abs-image/US/2015/02/03/US08946245B2/abs.jpg.150x150.jpg)
3.发明授权Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors 有权杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶作为Janus激酶抑制剂公开(公告)号：US08946245B2
公开(公告)日：2015-02-03
申请号：US13076176
申请日：2011-03-30
Applicant: James D. Rodgers , Stacey Shepard , Jordan S. Fridman , Krishna Vaddi
Inventor： James D. Rodgers , Stacey Shepard , Jordan S. Fridman , Krishna Vaddi
IPC: A61K31/519 , C07D471/04 , A61K45/06 , C07D487/04
CPC classification number: A61K31/519 , A61K9/0014 , A61K9/0053 , A61K9/20 , A61K31/573 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D417/04 , C07D471/04 , C07D487/04
Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
Abstract translation: 本发明提供调节Janus激酶活性的杂芳基取代的吡咯并[2,3-b]吡啶和杂芳基取代的吡咯并[2,3-b]嘧啶，可用于治疗与Janus激酶活性有关的疾病， 例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。
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4.发明授权Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors 有权环丁基取代吡咯并吡啶和吡咯并嘧啶衍生物作为JAK抑制剂公开(公告)号：US08933085B2
公开(公告)日：2015-01-13
申请号：US13300094
申请日：2011-11-18
Applicant: James D. Rodgers , Stacey Shepard , Wenyu Zhu , Lixin Shao , Joseph Glenn
Inventor： James D. Rodgers , Stacey Shepard , Wenyu Zhu , Lixin Shao , Joseph Glenn
IPC: C07D487/04 , C07D471/04 , A61K31/519 , A61K31/437 , A61P35/00 , A61P29/00 , A61P37/06 , A61P17/06 , A61P17/08 , A61P19/08 , A61P19/10
CPC classification number: C07D487/04 , C07D471/04
Abstract: The present invention provides cyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I: wherein X, Y, Z, L, A, R5, n and m are defined above, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Abstract translation: 本发明提供式I的环丁基取代的吡咯并嘧啶和吡咯并吡啶：其中X，Y，Z，L，A，R 5，n和m如上定义，以及它们的组成和使用方法，其调节Janus激酶的活性 （JAK），并且可用于治疗与JAK的活性相关的疾病，包括例如炎症性疾病，自身免疫性疾病，癌症和其他疾病。
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![Heteroaryl Substituted Pyrrolo[2,3-B]Pyridines And Pyrrolo[2,3-B]Pyrimidines As Janus Kinase Inhibitors](/abs-image/US/2014/01/16/US20140018374A1/abs.jpg.150x150.jpg)
5.发明申请Heteroaryl Substituted Pyrrolo[2,3-B]Pyridines And Pyrrolo[2,3-B]Pyrimidines As Janus Kinase Inhibitors 有权杂芳基取代的吡咯并[2,3-B]吡啶和吡咯并[2,3-B]嘧啶作为Janus激酶抑制剂公开(公告)号：US20140018374A1
公开(公告)日：2014-01-16
申请号：US14033039
申请日：2013-09-20
Applicant: James D. Rodgers , Stacey Shepard , Jordan S. Fridman , Krishna Vaddi
Inventor： James D. Rodgers , Stacey Shepard , Jordan S. Fridman , Krishna Vaddi
IPC: C07D487/04 , A61K31/519 , A61K45/06
CPC classification number: A61K31/519 , A61K9/0014 , A61K9/0053 , A61K9/20 , A61K31/573 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D417/04 , C07D471/04 , C07D487/04
Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
Abstract translation: 本发明提供调节Janus激酶活性的杂芳基取代的吡咯并[2,3-b]吡啶和杂芳基取代的吡咯并[2,3-b]嘧啶，可用于治疗与Janus激酶活性有关的疾病， 例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。
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Patent Agency Ranking
![3-[4-(7H-pyrrolo[2,3-D]pyrimidin-4-yl)-1H-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors](/abs-image/US/2013/12/10/US08604043B2/abs.jpg.150x150.jpg)
6.发明授权3-[4-(7H-pyrrolo[2,3-D]pyrimidin-4-yl)-1H-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors 有权3- [4-（7H-吡咯并[2,3-D]嘧啶-4-基）-1H-吡唑-1-基]辛烷或庚烷腈作为阻止剂公开(公告)号：US08604043B2
公开(公告)日：2013-12-10
申请号：US12785057
申请日：2010-05-21
Applicant: Yun-Long Li , James D. Rodgers
Inventor： Yun-Long Li , James D. Rodgers
IPC: A01N43/90 , A61K31/519 , C07D487/00
CPC classification number: A61K31/519 , C07D487/04
Abstract: The present invention relates to the Janus kinase (JAK) inhibitors 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile or 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile, as well as its compositions and methods of use, which is useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, skin disorders, cancer, and other diseases.
Abstract translation: 本发明涉及Janus激酶（JAK）抑制剂3- [4-（7H-吡咯并[2,3-d]嘧啶-4-基）-1H-吡唑-1-基]辛腈或3- [4- （7H-吡咯并[2,3-d]嘧啶-4-基）-1H-吡唑-1-基]庚腈，以及其组合物和使用方法，其可用于治疗JAK相关疾病，包括 ，例如炎性和自身免疫性疾病，皮肤病症，癌症和其它疾病。
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![Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d] pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile](/abs-image/US/2013/07/16/US08486902B2/abs.jpg.150x150.jpg)
7.发明授权Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d] pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile 有权3-（4-（7H-吡咯并[2,3-d]嘧啶-4-基）-1H-吡唑-1-基）-3-环戊基丙腈的羟基，酮基和葡糖苷酸衍生物公开(公告)号：US08486902B2
公开(公告)日：2013-07-16
申请号：US12901001
申请日：2010-10-08
Applicant: James D. Rodgers , Adam Shilling , Argyrios G. Arvanitis , Stacey Shepard , Laurine G. Galya , Mei Li , Frank M. Nedza
Inventor： James D. Rodgers , Adam Shilling , Argyrios G. Arvanitis , Stacey Shepard , Laurine G. Galya , Mei Li , Frank M. Nedza
IPC: C07H17/02 , C07D487/04 , A61K31/70 , A61K31/519 , A61P37/06 , A61P35/00 , A61P25/28 , A01N43/04
CPC classification number: C07H17/02 , A61K31/519 , C07D403/04 , C07D405/12 , C07D487/04
Abstract: The present invention provides hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile.
Abstract translation: 本发明提供3-（4-（7H-吡咯并[2,3-d]嘧啶-4-基）-1H-吡唑-1-基）-3-环戊基丙腈的羟基，酮基和葡糖苷酸衍生物。
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![Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2,3-b]pyrimidin-5-yl-amines as janus kinase inhibitors](/abs-image/US/2011/11/08/US08053433B2/abs.jpg.150x150.jpg)
8.发明授权公开(公告)号：US08053433B2
公开(公告)日：2011-11-08
申请号：US11980314
申请日：2007-10-30
Applicant: James D. Rodgers , Haisheng Wang , Andrew P. Combs , Richard B. Sparks
Inventor： James D. Rodgers , Haisheng Wang , Andrew P. Combs , Richard B. Sparks
IPC: A61K31/535 , A61K31/44
CPC classification number: C07D471/04 , C07D487/04
Abstract: The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.
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![Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2,3-b]pyrimidin-4-yl-amines as Janus kinase inhibitors](/abs-image/US/2008/02/26/US07335667B2/abs.jpg.150x150.jpg)
9.发明授权Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2,3-b]pyrimidin-4-yl-amines as Janus kinase inhibitors 有权吡咯并[2,3-b]吡啶-4-基胺和吡咯并[2,3-b]嘧啶-4-基胺作为Janus激酶抑制剂公开(公告)号：US07335667B2
公开(公告)日：2008-02-26
申请号：US11313394
申请日：2005-12-21
Applicant: James D. Rodgers , Haisheng Wang , Andrew P. Combs , Richard B. Sparks
Inventor： James D. Rodgers , Haisheng Wang , Andrew P. Combs , Richard B. Sparks
IPC: A01N43/42 , A61K31/44 , C07D471/02 , C07D491/02 , C07D498/02
CPC classification number: C07D471/04 , C07D487/04
Abstract: The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.
Abstract translation: 本发明提供调节Janus激酶活性的吡咯并[2,3-b]吡啶-4-基胺吡咯并[2,3-b]嘧啶-4-基胺，可用于治疗与活性有关的疾病 的Janus激酶，包括例如免疫相关疾病和癌症。
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10.发明授权Tricyclic-2-pyridone compounds useful as HIV reverse transcriptase inhibitors 有权可用作HIV逆转录酶抑制剂的三环-2-吡啶酮化合物公开(公告)号：US06969721B2
公开(公告)日：2005-11-29
申请号：US10457902
申请日：2003-06-10
Applicant: James D. Rodgers , Haisheng Wang , Mona Patel , Argyrios Arvanitis , Anthony J. Cocuzza
Inventor： James D. Rodgers , Haisheng Wang , Mona Patel , Argyrios Arvanitis , Anthony J. Cocuzza
IPC: A61K20060101 , A61P20060101 , C07D20060101 , C07D471/04 , A61K31/4375
CPC classification number: C07D471/04
Abstract: The present invention relates to tricyclic 2-pyridone compounds of formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
Abstract translation: 本发明涉及可用作HIV逆转录酶抑制剂的式（I）的三环2-吡啶酮化合物或其立体异构形式，立体异构混合物或其药学上可接受的盐形式，以及包含其的药物组合物和诊断试剂盒 ，以及使用该药物治疗病毒感染或作为测定标准品或试剂的方法。
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