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11.发明申请公开(公告)号：US20160340351A1
公开(公告)日：2016-11-24
申请号：US15105713
申请日：2014-12-18
申请人： Brian M. ANDRESEN , Kenneth L. ARRINGTON , Ryan D. OTTE , John Michael ELLIS , John W. BUTCHER , Alan B. NORTHRUP , Joel S. ROBICHAUD , Jacques Yves GAUTHIER , Jean-Francois FOURNIER , MERCK SHARP & DOHME CORP.
发明人： Brian M. Andresen , Kenneth L. Arrington , Ryan D. Otte , John Michael Ellis , John W. Butcher , Alan B. Northrup , Joel S. Robichaud , Jacques Yves Gauthier , Jean-Francois Fournier
IPC分类号： C07D417/14 , C07D417/12 , A61K31/5377 , A61K31/506 , A61K31/538
CPC分类号： C07D417/14 , A61K31/506 , A61K31/5377 , A61K31/538 , C07D417/12
摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring B, and the subscript r are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
摘要翻译： 本发明提供了式（I）的某些噻唑取代的氨基杂芳基化合物或其药学上可接受的盐，其中R1，R2，R3，R4，环B和下标r如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）介导的疾病或病症的方法。
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公开(公告)号：US11685761B2
公开(公告)日：2023-06-27
申请号：US16771814
申请日：2018-12-17
申请人： Merck Sharp & Dohme Corp. , Brian M. Andresen , Frank Bennett , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Jongwon Lim , Min Lu , Benjamin Wesley Trotter , Wen-Lian Wu
发明人： Brian M. Andresen , Frank Bennett , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Jongwon Lim , Min Lu , Benjamin Wesley Trotter , Wen-Lian Wu
IPC分类号： C07H21/00 , A61P37/04 , C07H21/02 , A61K31/7084 , C07H21/04
CPC分类号： C07H21/00 , A61K31/7084 , A61P37/04 , C07H21/02 , C07H21/04 , C07B2200/07
摘要： A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Za, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, R8a, and R9 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of 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
发明人： 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分类号： 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
摘要： 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：US09969749B2
公开(公告)日：2018-05-15
申请号：US15515383
申请日：2015-09-25
发明人： Michael D. Altman , Brian M. Andresen , Jason D. Brubaker , Matthew L. Childers , Anthony Donofrio , Thierry Fischmann , Craig R. Gibeau , Solomon D. Kattar , Charles A. Lesburg , Jongwon Lim , John K. F. MacLean , Umar F. Mansoor , Alan B. Northrup , John M. Sanders , Luis Torres
IPC分类号： C07D498/04 , A61K45/06 , A61K31/517 , C07D403/04 , C07D239/94 , C07D401/04 , A61K31/5377 , C07D405/14 , C07D401/14 , C07D413/04 , C07D405/04 , C07D471/04 , A61K31/5383 , C07D491/048 , C07D417/04 , C07D409/04
CPC分类号： C07D498/04 , A61K31/517 , A61K31/5377 , A61K31/5383 , A61K45/06 , A61P37/00 , C07D239/94 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D491/048 , A61K2300/00
摘要： The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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15.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
发明人： 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分类号： C07D413/12 , A61K31/538 , C07D265/36 , C07D413/14 , C07D498/04 , C07D513/04 , C07D487/04 , C07D417/12 , A61K45/06 , C07D471/04
CPC分类号： C07D413/12 , A61K31/538 , A61K45/06 , C07D265/36 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04
摘要： 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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16.发明申请公开(公告)号：US20150353535A1
公开(公告)日：2015-12-10
申请号：US14653488
申请日：2013-12-19
发明人： Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Kaleen Konrad Childers , Maria Emilia Di Francesco , John Michael Ellis , Andrew M. Haidle , Yuan Liu , Alan B. Northrup , Brendan O'Boyle , Ryan D. Otte , Michael H. Reutershan , Dilrukshi Vitharana , Hyun Chong Woo
IPC分类号： C07D417/14 , A61K31/444
CPC分类号： C07D417/14 , A61K31/444 , A61K45/06
摘要： The invention provides certain thiazole-substituted aminopyridine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, Cy, and the subscript t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
摘要翻译： 本发明提供了式（I）（I）的某些噻唑取代的氨基吡啶化合物或其药学上可接受的盐，其中R1，R2，R3，R4，R5，R6，Cy和下标t如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）介导的疾病或病症的方法。
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17.发明申请3-CYCLOHEXENYL AND CYCLOHEXYL SUBSTITUTED INDOLE AND INDAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF 有权3-环己基和环己基取代的吲哚和吲哚酮化合物作为RORGAMAMT抑制剂及其用途公开(公告)号：US20150191434A1
公开(公告)日：2015-07-09
申请号：US14421057
申请日：2013-08-14
发明人： Kenneth J. Barr , John K. Maclean , Hongjun Zhang , Richard T. Beresis , Dongshan Zhang , Brian M. Andresen , Neville J. Anthony , Blair T. Lapointe , Nunzio Sciammetta
IPC分类号： C07D231/56 , C07D471/04 , A61K31/437 , C07D403/06 , C07D413/06 , A61K31/404 , A61K31/496 , C07D405/12 , C07D401/06 , A61K31/454 , C07D209/26 , A61K31/416 , A61K31/5377
CPC分类号： C07D231/56 , A61K31/404 , A61K31/416 , A61K31/437 , A61K31/454 , A61K31/496 , A61K31/5377 , C07D209/26 , C07D401/06 , C07D403/06 , C07D405/12 , C07D413/06 , C07D471/04 , Y02A50/409
摘要： The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
摘要翻译： 本发明涉及式I化合物及其药学上可接受的盐或溶剂化物。 这些化合物可用于治疗RORGAMMT介导的疾病或病症。
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公开(公告)号：US20210206796A1
公开(公告)日：2021-07-08
申请号：US16771814
申请日：2018-12-17
申请人： Brian M. ANDRESEN , Frank BENNETT , Wonsuk CHANG , Matthew Lloyd CHILDERS , Jared N. CUMMING , Jongwon LIM , Min LU , Benjamin Wesley TROTTER , Wen-Lian WU , Merck Sharp & Dohme Corp.
发明人： Brian M. Andresen , Frank Bennett , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Jongwon Lim , Min Lu , Benjamin Wesley Trotter , Wen-Lian Wu
摘要： A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Za, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, R8a and R9 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.
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公开(公告)号：US20180030005A1
公开(公告)日：2018-02-01
申请号：US15730997
申请日：2017-10-12
发明人： 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分类号： C07D265/36 , A61K31/4375 , C07D417/06 , C07D413/14 , C07D413/12 , C07D413/06 , C07D413/04 , C07D401/12 , C07D401/06 , C07D215/58 , A61K45/06 , A61K31/538 , A61K31/4709 , A61K31/47 , C07D471/04 , C07D487/04
CPC分类号： 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 , Y02A50/409
摘要： 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：US09783511B2
公开(公告)日：2017-10-10
申请号：US15103409
申请日：2014-12-19
发明人： 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分类号： C07D265/36 , A61K31/538 , C07D413/12 , C07D513/04 , C07D417/12 , C07D471/04 , C07D487/04
CPC分类号： C07D265/36 , A61K31/538 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： 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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