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公开(公告)号：US10377768B2
公开(公告)日：2019-08-13
申请号：US15587934
申请日：2017-05-05
Applicant: Merck Sharp & Dohme Corp. , Lycera Corporation
Inventor： Thomas D. Aicher , Kenneth J. Barr , Blair T. Lapointe , Vladimir Simov , Karin A. Stein , William D. Thomas , Peter L. Toogood , Chad A. Van Huis , Catherine M. White
IPC: C07D498/04 , C07D413/06 , C07D471/04
Abstract: The invention provides tetrahydronaphthyridine 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 tetrahydronaphthyridine and related compounds.
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公开(公告)号：US09657033B2
公开(公告)日：2017-05-23
申请号：US14398061
申请日：2013-05-07
Applicant: Merck Sharp & Dohme Corp. , Lycera Corporation
Inventor： Thomas D. Aicher , Kenneth J. Barr , Blair T. Lapointe , Vladimir Simov , Karin A. Stein , William D. Thomas , Peter L. Toogood , Chad A. Van Huis , Catherine M. White
IPC: A61K31/397 , C07D498/04 , C07D413/06 , C07D471/04
CPC classification number: C07D498/04 , C07D413/06 , C07D471/04
Abstract: The invention provides tetrahydronaphthyridine 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 tetrahydronaphthyridine and related compounds.
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公开(公告)号：US10745364B2
公开(公告)日：2020-08-18
申请号：US16270882
申请日：2019-02-08
Applicant: Merck Sharp & Dohme Corp. , Lycera Corporation
Inventor： Thomas D. Aicher , Chad A. VanHuis , William D. Thomas , John K. MacLean , Brian M. Andresen , Kenneth J. Barr , Corey E. Bienstock , Neville J. Anthony , Matthew Daniels , Kun Liu , Yuan Liu , Catherine M. White , Blair T. Lapointe , Nunzio Sciammetta , Vladimir Simov
IPC: C07D265/36 , C07D413/14 , C07D215/58 , C07D401/06 , C07D401/12 , C07D413/04 , C07D471/04 , A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/538 , A61K45/06 , C07D413/06 , C07D413/12 , C07D417/06 , C07D487/04
Abstract: The invention provides certain bicylic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2, R3, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.
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4.发明申请2-ACYLAMIDOMETHYL AND SULFONYLAMIDOMETHYL BENZOXAZINE CARBAMATES FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE 有权2-氨基甲酰乙酰和亚磺酰氨基苯甲酰胺碳酸酯抑制罗尔玛活性和治疗疾病公开(公告)号：US20160304505A1
公开(公告)日：2016-10-20
申请号：US15103407
申请日：2014-12-19
Applicant: MERCK SHARP & DOHME CORP. , LYCERA CORPORATION
Inventor： Thomas D. Aicher , Chad A. VanHuis , John MacLean , Brian M. Andresen , Kenneth J. Barr , Corey Bienstock , Neville J. Anthony , Matthew Daniels , Yuan Liu , Catherine White , Blair T. Lapointe , Nunzio Sciammetta , Vladimir Simov , Wesley B. Trotter , Kun Liu
IPC: C07D413/12 , A61K31/538 , C07D265/36 , C07D413/14 , C07D498/04 , C07D513/04 , C07D487/04 , C07D417/12 , A61K45/06 , C07D471/04
CPC classification number: C07D413/12 , A61K31/538 , A61K45/06 , C07D265/36 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04
Abstract: The invention provides certain benzoxazine compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, Ra, Rb, Rc, Rd, Rg, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.
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公开(公告)号：US09809561B2
公开(公告)日：2017-11-07
申请号：US15103414
申请日：2014-12-19
Applicant: Merck Sharp & Dohme Corp. , Lycera Corporation
Inventor： Thomas D. Aicher , Chad A. VanHuis , William D. Thomas , John K. MacLean , Brian M. Andresen , Kenneth J. Barr , Corey E. Bienstock , Neville J. Anthony , Matthew Daniels , Kun Liu , Yuan Liu , Catherine M. White , Blair T. Lapointe , Nunzio Sciammetta , Vladimir Simov
IPC: C07D265/36 , C07D413/14 , C07D215/58 , C07D401/06 , C07D401/12 , C07D413/04 , C07D471/04 , A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/538 , A61K45/06 , C07D413/06 , C07D413/12 , C07D417/06 , C07D487/04
CPC classification number: C07D265/36 , A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/538 , A61K45/06 , C07D215/58 , C07D401/06 , C07D401/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D471/04 , C07D487/04
Abstract: The invention provides certain bicylic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2, R3, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.
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Patent Agency Ranking
6.发明申请CARBAMATE BENZOXAZINE PROPIONIC ACIDS AND ACID DERIVATIVES FOR MODULATION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE 有权用于调节罗丹明活性和疾病治疗的碳酸酯苯并咪唑酸和酸衍生物公开(公告)号：US20160311787A1
公开(公告)日：2016-10-27
申请号：US15103409
申请日：2014-12-19
Applicant: MERCK SHARP & DOHME CORP. , LYCERA CORPORATION
Inventor： Thomas D. Aicher , Chad A. VanHuis , John MacLean , Brian M. Andresen , Kenneth J. Barr , Corey Bienstock , Matthew Daniels , Kun Liu , Yuan Liu , Catherine White , Nunzio Sciammetta , Vladimir Simov
IPC: C07D265/36 , C07D413/12 , C07D417/12 , C07D471/04 , C07D513/04 , A61K31/538 , C07D487/04
CPC classification number: C07D265/36 , A61K31/538 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
Abstract: The invention provides certain benzoxazine compounds of the Formula (I) or pharmaceutically acceptable salts thereof wherein R1, R2, Ra1, Ra2, Rb1, Rb2, Rc, Rd, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.
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7.发明授权Bicyclic sulfone compounds for inhibition of RORgamma activity and the treatment of disease 有权用于抑制RORGAMMA活性和治疗疾病的双环砜化合物公开(公告)号：US09266827B2
公开(公告)日：2016-02-23
申请号：US14398068
申请日：2013-05-03
Applicant: Merck Sharp & Dohme Corp. , Lycera Corporation
Inventor： Thomas D. Aicher , Kenneth Jay Barr , Vladimir Simov , William D. Thomas , Peter L. Toogood , Chad A. Van Huis
IPC: C07D233/72 , C07D263/22 , C07D207/12 , C07C317/40 , A61K31/10 , A61K31/16 , A61K31/47 , C07C311/30 , C07D263/44 , C07D207/27 , C07D209/52 , C07D211/96 , C07D213/82 , C07D215/38 , C07D217/22 , C07D223/16 , C07D231/18 , C07D401/12 , C07D471/04 , C07D491/052
CPC classification number: C07C317/40 , C07C311/30 , C07C2601/02 , C07C2601/14 , C07C2602/00 , C07C2602/10 , C07C2602/22 , C07C2602/42 , C07D207/12 , C07D207/27 , C07D209/52 , C07D211/96 , C07D213/82 , C07D215/38 , C07D217/22 , C07D223/16 , C07D231/18 , C07D233/72 , C07D263/22 , C07D263/44 , C07D401/12 , C07D471/04 , C07D491/052
Abstract: The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.
Abstract translation: 本发明提供双环砜化合物，药物组合物，抑制RORY活性的方法，减少受试者中iL-17的量，以及使用这种双环砜化合物治疗免疫疾病和炎症性疾病。 本发明的另一方面提供了治疗患有医学病症的受试者的方法。 该方法包括向受试者施用治疗有效量的本文所述的一种或多种双环砜化合物。 在某些其它实施方案中，疾病是类风湿性关节炎。
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公开(公告)号：US20190292159A1
公开(公告)日：2019-09-26
申请号：US16270882
申请日：2019-02-08
Applicant: Merck Sharp & Dohme Corp. , Lycera Corporation
Inventor： Thomas D. Aicher , Chad A. VanHuis , William D. Thomas , John K. MacLean , Brian M. Andresen , Kenneth J. Barr , Corey E. Bienstock , Neville J. Anthony , Matthew Daniels , Kun Liu , Yuan Liu , Catherine M. White , Blair T. Lapointe , Nunzio Sciammetta , Vladimir Simov
IPC: C07D265/36 , C07D413/12 , A61K31/4709 , C07D413/06 , C07D487/04 , C07D417/06 , C07D471/04 , C07D413/04 , C07D401/12 , C07D401/06 , C07D215/58 , C07D413/14 , A61K45/06 , A61K31/538 , A61K31/4375 , A61K31/47
Abstract: The invention provides certain bicylic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2, R3, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.
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公开(公告)号：US10221146B2
公开(公告)日：2019-03-05
申请号：US15730997
申请日：2017-10-12
Applicant: Merck Sharp & Dohme Corp. , Lycera Corporation
Inventor： Thomas D. Aicher , Chad A. VanHuis , William D. Thomas , John K. MacLean , Brian M. Andresen , Kenneth J. Barr , Corey E. Bienstock , Neville J. Anthony , Matthew Daniels , Kun Liu , Yuan Liu , Catherine M. White , Blair T. Lapointe , Nunzio Sciammetta , Vladimir Simov
IPC: C07D265/36 , C07D413/14 , C07D215/58 , C07D401/06 , C07D401/12 , C07D413/04 , C07D471/04 , A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/538 , A61K45/06 , C07D413/06 , C07D413/12 , C07D417/06 , C07D487/04
Abstract: The invention provides certain bicyclic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2, R3, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.
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10.发明申请公开(公告)号：US20170313722A1
公开(公告)日：2017-11-02
申请号：US15587934
申请日：2017-05-05
Applicant: Merck Sharp & Dohme Corp. , Lycera Corporation
Inventor： Thomas D. Aicher , Kenneth J. Barr , Blair T. Lapointe , Vladimir Simov , Karin A. Stein , William D. Thomas , Peter L. Toogood , Chad A. VanHuis , Catherine M. White
IPC: C07D498/04 , C07D471/04 , C07D413/06
CPC classification number: C07D498/04 , C07D413/06 , C07D471/04
Abstract: The invention provides tetrahydronaphthyridine 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 tetrahydronaphthyridine and related compounds.
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