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1.发明授权N-sulfonylated tetrahydroquinolines and related bicyclic compounds for inhibition of RORγ activity and the treatment of disease 有权N-磺酰化四氢喹啉和相关双环化合物，用于抑制RORγ活性和治疗疾病公开(公告)号：US09512111B2
公开(公告)日：2016-12-06
申请号：US13883419
申请日：2011-11-08
Applicant: Gary D. Glick , Peter L. Toogood , Arthur G. Romero , Chad A. Van Huis , Thomas D. Aicher , Carl Kaub , Matthew N. Mattson , William D. Thomas , Karin A. Stein , Erik Krogh-Jespersen , Zhan Wang
Inventor： Gary D. Glick , Peter L. Toogood , Arthur G. Romero , Chad A. Van Huis , Thomas D. Aicher , Carl Kaub , Matthew N. Mattson , William D. Thomas , Karin A. Stein , Erik Krogh-Jespersen , Zhan Wang
IPC: C07D413/06 , C07D209/08 , C07D209/34 , C07D215/58 , C07D231/56 , C07D241/50 , C07D265/36 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/12 , C07D471/04
CPC classification number: C07D413/06 , C07D209/08 , C07D209/34 , C07D215/58 , C07D231/56 , C07D241/50 , C07D265/36 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/12 , C07D471/04
Abstract: The invention provides tetrahydroquinoline and related compounds, pharmaceutical compositions, methods of inhibiting RORγ activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydroquinoline and related compounds are provided.
Abstract translation: 本发明提供了四氢喹啉及其相关化合物，药物组合物，抑制RORγ活性的方法，减少受试者中IL-17的量，以及使用这些四氢喹啉及相关化合物治疗免疫疾病和炎症性疾病。
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公开(公告)号：US07449486B2
公开(公告)日：2008-11-11
申请号：US11252232
申请日：2005-10-17
Applicant: Jeremy Hans , Eli M. Wallace , Qian Zhao , Joseph P. Lyssikatos , Thomas D. Aicher , Ellen R Laird , John Robinson , Shelley Allen
Inventor： Jeremy Hans , Eli M. Wallace , Qian Zhao , Joseph P. Lyssikatos , Thomas D. Aicher , Ellen R Laird , John Robinson , Shelley Allen
IPC: A61K31/433 , C07D285/12
CPC classification number: C07D285/12 , C07D271/107 , C07D401/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07F9/201 , C07F9/65392
Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
Abstract translation: 本发明涉及有丝分裂驱动蛋白抑制剂，特别是KSP，以及制备这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用抑制剂和药物组合物治疗和预防各种疾病的方法。
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公开(公告)号：US08022222B2
公开(公告)日：2011-09-20
申请号：US12161366
申请日：2007-01-24
Applicant: Thomas D. Aicher , Steven Armen Boyd , Mark Joseph Chicarelli , Kevin Ronald Condroski , Rustam Ferdinand Garrey , Ronald Jay Hinklin , Ajay Singh , Timothy M. Turner
Inventor： Thomas D. Aicher , Steven Armen Boyd , Mark Joseph Chicarelli , Kevin Ronald Condroski , Rustam Ferdinand Garrey , Ronald Jay Hinklin , Ajay Singh , Timothy M. Turner
IPC: C07D417/00 , A61K31/44
CPC classification number: C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
Abstract: Provided are compounds of formula I wherein R2, L, Z, Y, G and R1 are as defined herein, that are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.
Abstract translation: 提供式I化合物，其中R 2，L，Z，Y，G和R 1如本文所定义，其可用于治疗和/或预防由缺乏葡萄糖激酶水平的活性介导的疾病或病症，或可由 激活葡萄糖激酶，包括但不限于糖尿病，葡萄糖耐量降低，IFG（空腹血糖受损）和IFG（空腹血糖受损）），以及其他疾病和病症如本文讨论的疾病和病症。
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公开(公告)号：US20120270803A1
公开(公告)日：2012-10-25
申请号：US13538698
申请日：2012-06-29
Applicant: Jeremy Hans , Eli M. Wallace , Qian Zhao , Joseph P. Lyssikatos , Thomas D. Aicher , Ellen R. Laird , John Robinson , Shelley Allen
Inventor： Jeremy Hans , Eli M. Wallace , Qian Zhao , Joseph P. Lyssikatos , Thomas D. Aicher , Ellen R. Laird , John Robinson , Shelley Allen
IPC: A61K31/433 , A61K31/4439 , A61K38/55 , A61P35/02 , A61P35/00
CPC classification number: C07D285/12 , C07D271/107 , C07D401/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07F9/201 , C07F9/65392
Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
Abstract translation: 本发明涉及有丝分裂驱动蛋白抑制剂，特别是KSP，以及制备这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用抑制剂和药物组合物治疗和预防各种疾病的方法。
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公开(公告)号：US20110281874A1
公开(公告)日：2011-11-17
申请号：US13191994
申请日：2011-07-27
Applicant: Thomas D. AICHER , Steven Armen BOYD , Mark Joseph CHICARELLI , Kevin Ronald CONDROSKI , Ronald Jay HINKLIN , Ajay SINGH
Inventor： Thomas D. AICHER , Steven Armen BOYD , Mark Joseph CHICARELLI , Kevin Ronald CONDROSKI , Ronald Jay HINKLIN , Ajay SINGH
IPC: A61K31/5377 , A61K31/497 , A61K31/519 , A61K31/506 , A61K31/437 , A61P3/10 , A61K31/4439 , C07D495/04 , C07D471/04 , C07D417/14 , C07D498/04 , C07D417/12 , A61K31/496 , A61K31/4545
CPC classification number: C07D417/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D513/04
Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
Abstract translation: 提供了可用于治疗和/或预防由缺乏水平的葡糖激酶活性（例如糖尿病）介导的疾病的化合物。 还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法，或者可以通过激活葡糖激酶治疗。
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Patent Agency Ranking
公开(公告)号：US20110201651A1
公开(公告)日：2011-08-18
申请号：US13093729
申请日：2011-04-25
Applicant: Jeremy Hans , Eli M. Wallace , Qian Zhao , Joseph P. Lyssikatos , Thomas D. Aicher , Ellen R. Laird , John Robinson , Shelley Allen
Inventor： Jeremy Hans , Eli M. Wallace , Qian Zhao , Joseph P. Lyssikatos , Thomas D. Aicher , Ellen R. Laird , John Robinson , Shelley Allen
IPC: A61K31/4439 , C07D417/04 , A61P29/00 , A61P37/06 , A61P19/02 , A61P1/00
CPC classification number: C07D285/12 , C07D271/107 , C07D401/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07F9/201 , C07F9/65392
Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
Abstract translation: 本发明涉及有丝分裂驱动蛋白抑制剂，特别是KSP，以及制备这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用抑制剂和药物组合物治疗和预防各种疾病的方法。
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公开(公告)号：US20080182992A1
公开(公告)日：2008-07-31
申请号：US12043456
申请日：2008-03-06
Applicant: Jeremy Hans , Eli M. Wallace , Qian Zhao , Joseph P. Lyssikatos , Thomas D. Aicher , Ellen R. Laird , John Robinson , Shelley Allen
Inventor： Jeremy Hans , Eli M. Wallace , Qian Zhao , Joseph P. Lyssikatos , Thomas D. Aicher , Ellen R. Laird , John Robinson , Shelley Allen
IPC: C07D285/12 , C07D271/10
CPC classification number: C07D285/12 , C07D271/107 , C07D401/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07F9/201 , C07F9/65392
Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
Abstract translation: 本发明涉及有丝分裂驱动蛋白抑制剂，特别是KSP，以及制备这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用抑制剂和药物组合物治疗和预防各种疾病的方法。
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公开(公告)号：US08623895B2
公开(公告)日：2014-01-07
申请号：US13538698
申请日：2012-06-29
Applicant: Jeremy Hans , Eli M. Wallace , Qian Zhao , Joseph P. Lyssikatos , Thomas D. Aicher , Ellen R Laird , John Robinson , Shelley Allen
Inventor： Jeremy Hans , Eli M. Wallace , Qian Zhao , Joseph P. Lyssikatos , Thomas D. Aicher , Ellen R Laird , John Robinson , Shelley Allen
IPC: A61K31/433 , A61K31/4439 , C07D417/12 , C07D285/12
CPC classification number: C07D285/12 , C07D271/107 , C07D401/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07F9/201 , C07F9/65392
Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
Abstract translation: 本发明涉及有丝分裂驱动蛋白抑制剂，特别是KSP，以及制备这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用抑制剂和药物组合物治疗和预防各种疾病的方法。
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公开(公告)号：US08022223B2
公开(公告)日：2011-09-20
申请号：US12282600
申请日：2007-03-23
Applicant: Thomas D. Aicher , Steven Armen Boyd , Mark Joseph Chicarelli , Kevin Ronald Condroski , Ronald Jay Hinklin , Ajay Singh
Inventor： Thomas D. Aicher , Steven Armen Boyd , Mark Joseph Chicarelli , Kevin Ronald Condroski , Ronald Jay Hinklin , Ajay Singh
IPC: C07D417/00 , C07D401/00
CPC classification number: C07D417/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D513/04
Abstract: Provided are compounds of formula I that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes meilitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
Abstract translation: 提供式I化合物，其可用于治疗和/或预防由缺乏葡萄糖激酶水平的活性介导的疾病，例如糖尿病。 还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法，或者可以通过激活葡糖激酶治疗。
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公开(公告)号：US07956073B2
公开(公告)日：2011-06-07
申请号：US12043456
申请日：2008-03-06
Applicant: Jeremy Hans , Eli M. Wallace , Qian Zhao , Joseph P. Lyssikatos , Thomas D. Aicher , Ellen R Laird , John Robinson , Shelley Allen
Inventor： Jeremy Hans , Eli M. Wallace , Qian Zhao , Joseph P. Lyssikatos , Thomas D. Aicher , Ellen R Laird , John Robinson , Shelley Allen
IPC: A61K31/433 , C07D285/12
CPC classification number: C07D285/12 , C07D271/107 , C07D401/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07F9/201 , C07F9/65392
Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
Abstract translation: 本发明涉及有丝分裂驱动蛋白抑制剂，特别是KSP，以及制备这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用抑制剂和药物组合物治疗和预防各种疾病的方法。
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