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公开(公告)号：US10435369B2
公开(公告)日：2019-10-08
申请号：US15806554
申请日：2017-11-08
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： David Marcoux , Myra Beaudoin Bertrand , T. G. Murali Dhar , Michael G. Yang , Zili Xiao , Hai-Yun Xiao , Yeheng Zhu , Carolyn A. Weigelt , Douglas G. Batt
IPC: C07C317/12 , C07C317/44 , A61K31/10 , C07D211/48 , A61P37/00 , C07D205/04 , C07D205/08 , C07D207/10 , C07D207/16 , C07D207/277 , C07D211/96 , C07D213/40 , C07D213/75 , C07D231/08 , C07D241/08 , C07D257/04 , C07D295/195 , C07D307/22 , C07D309/10 , C07D333/48 , C07D335/02 , C07D471/04 , C07D471/10 , C07D213/81 , C07D215/36 , C07D231/06 , C07D231/18 , C07D233/64 , C07D233/76 , C07D233/78 , C07D233/90 , C07D401/04 , C07D401/12 , C07D405/04 , C07C317/20 , C07C317/24 , C07C317/30 , C07D405/12 , C07D249/12 , C07D261/18 , C07D263/20 , C07D207/09 , C07D207/28 , C07D285/06 , C07D211/62 , C07D295/16 , C07D211/78 , C07D213/56 , C07D305/08 , C07F9/09
Abstract: There are described RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.
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公开(公告)号：US20190076450A1
公开(公告)日：2019-03-14
申请号：US16188444
申请日：2018-11-13
Applicant: Bristol-Myers Squibb Company
Inventor： Alaric J. Dyckman , T.G. Murali Dhar , Hai-Yun Xiao , John L. Gilmore , Michael G. Yang , Zili Xiao , David Marcoux
IPC: A61K31/695 , C07F7/08 , A61K31/505 , A61K31/137 , A61K31/15 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/222 , A61K31/24 , A61K31/27 , A61K31/337 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/4965 , A61K31/661 , C07F9/09 , C07F9/572 , C07F9/54 , C07C235/46 , C07C323/25 , C07C217/74 , C07C275/26 , C07D213/38 , C07D209/46 , C07C251/44 , C07C251/42 , C07C251/38 , C07C323/29 , C07D241/04 , C07D215/14 , A61K31/135 , C07D213/69 , C07D213/32 , C07C251/54 , C07C219/24 , C07C217/52 , C07D333/16 , C07D319/20 , C07D311/76 , C07D311/58 , C07D309/12 , C07D309/06 , C07D277/24 , C07D239/26 , C07D231/12 , C07D217/24 , C07C317/28 , C07C271/34 , C07C251/52 , C07C233/41 , C07C217/58 , C07C215/42 , C07F9/655 , C07F9/62 , C07D305/08 , C07D241/12 , C07D231/20 , C07D215/12 , C07D213/70
Abstract: Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
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公开(公告)号：US10166249B2
公开(公告)日：2019-01-01
申请号：US15648250
申请日：2017-07-12
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Alaric J. Dyckman , T. G. Murali Dhar , Hai-Yun Xiao , John L. Gilmore , Michael G. Yang , Zili Xiao , David Marcoux
IPC: A61K31/695 , C07C215/42 , C07C217/52 , C07C217/58 , C07C219/24 , C07C233/41 , C07C251/52 , C07C251/54 , C07C271/34 , C07C317/28 , C07D213/32 , C07D213/69 , C07D213/70 , C07D215/12 , C07D217/24 , C07D231/12 , C07D231/20 , C07D239/26 , C07D241/12 , C07D277/24 , C07D305/08 , C07D309/06 , C07D309/12 , C07D311/58 , C07D311/76 , C07D319/20 , C07D333/16 , C07F7/08 , C07F9/62 , C07F9/655 , A61K31/135 , C07D215/14 , C07D241/04 , C07C323/29 , C07C251/38 , C07C251/42 , C07C251/44 , C07D209/46 , C07D213/38 , C07C275/26 , C07C217/74 , C07C323/25 , C07C235/46 , C07F9/54 , C07F9/572 , C07F9/09 , A61K31/137 , A61K31/15 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/222 , A61K31/24 , A61K31/27 , A61K31/337 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/4965 , A61K31/505 , A61K31/661
Abstract: Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
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公开(公告)号：US20180127368A1
公开(公告)日：2018-05-10
申请号：US15806554
申请日：2017-11-08
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： David Marcoux , Myra Beaudoin Bertrand , T.G. Murali Dhar , Michael G. Yang , Zili Xiao , Hai-Yun Xiao , Yeheng Zhu , Carolyn A. Weigelt , Douglas G Batt
IPC: C07D211/48 , C07D213/40 , C07D295/195 , C07D213/75 , C07D333/48 , C07C317/44 , C07D335/02 , C07D471/04 , C07D307/22 , C07D241/08 , C07D207/10 , C07D207/16 , C07D231/08 , C07D309/10 , C07D211/96 , C07D471/10 , C07D205/04 , C07D207/277 , C07D257/04 , C07D205/08 , A61P37/00
CPC classification number: C07D211/48 , A61P37/00 , C07B2200/05 , C07B2200/07 , C07C317/20 , C07C317/24 , C07C317/30 , C07C317/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/38 , C07C2602/44 , C07C2602/50 , C07C2603/08 , C07C2603/12 , C07C2603/16 , C07C2603/90 , C07D205/04 , C07D205/08 , C07D207/09 , C07D207/10 , C07D207/16 , C07D207/277 , C07D207/28 , C07D211/62 , C07D211/78 , C07D211/96 , C07D213/40 , C07D213/56 , C07D213/75 , C07D213/81 , C07D215/36 , C07D231/06 , C07D231/08 , C07D231/18 , C07D233/64 , C07D233/76 , C07D233/78 , C07D233/90 , C07D241/08 , C07D249/12 , C07D257/04 , C07D261/18 , C07D263/20 , C07D285/06 , C07D295/16 , C07D295/195 , C07D305/08 , C07D307/22 , C07D309/10 , C07D333/48 , C07D335/02 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D471/04 , C07D471/10 , C07F9/091
Abstract: There are described RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.
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公开(公告)号：US20220331346A1
公开(公告)日：2022-10-20
申请号：US17307138
申请日：2021-05-04
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Alaric J. DYCKMAN , T.G. Murali Dhar , Hai-Yun Xiao , John L. Gilmore , Michael G. Yang , Zili Xiao , David Marcoux
IPC: A61K31/695 , C07F7/08 , A61K31/135 , C07D215/14 , C07D241/04 , C07C323/29 , C07C251/38 , C07C251/42 , C07C251/44 , C07D209/46 , C07D213/38 , C07C275/26 , C07C217/74 , C07C323/25 , C07C235/46 , C07F9/54 , C07F9/572 , C07F9/09 , C07C215/42 , C07C217/52 , C07C217/58 , C07C219/24 , C07C233/41 , C07C233/65 , C07C251/50 , C07C251/52 , C07C251/54 , C07C271/34 , C07C317/28 , C07C317/32 , C07C321/16 , C07C321/22 , C07C321/28 , C07D213/32 , C07D213/69 , C07D213/70 , C07D215/12 , C07D217/24 , C07D231/12 , C07D231/20 , C07D239/26 , C07D241/12 , C07D277/24 , C07D305/08 , C07D309/06 , C07D309/12 , C07D311/58 , C07D311/76 , C07D319/20 , C07D333/16 , C07F9/117 , C07F9/62 , C07F9/6503 , C07F9/6509 , C07F9/655 , C07F9/6553 , A61K31/137 , A61K31/15 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/222 , A61K31/24 , A61K31/27 , A61K31/337 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/4965 , A61K31/505 , A61K31/661
Abstract: Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
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Patent Agency Ranking
公开(公告)号：US20200281952A1
公开(公告)日：2020-09-10
申请号：US16879824
申请日：2020-05-21
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Alaric J. Dyckman , T.G. Murali Dhar , Hai-Yun Xiao , John L. Gilmore , Michael G. Yang , Zili Xiao , David Marcoux
IPC: A61K31/695 , C07F7/08 , A61K31/135 , C07D215/14 , C07D241/04 , C07C323/29 , C07C251/38 , C07C251/42 , C07C251/44 , C07D209/46 , C07D213/38 , C07C275/26 , C07C217/74 , C07C323/25 , C07C235/46 , C07F9/54 , C07F9/572 , C07F9/09 , C07C215/42 , C07C217/52 , C07C217/58 , C07C219/24 , C07C233/41 , C07C233/65 , C07C251/50 , C07C251/52 , C07C251/54 , C07C271/34 , C07C317/28 , C07C317/32 , C07C321/16 , C07C321/22 , C07C321/28 , C07D213/32 , C07D213/69 , C07D213/70 , C07D215/12 , C07D217/24 , C07D231/12 , C07D231/20 , C07D239/26 , C07D241/12 , C07D277/24 , C07D305/08 , C07D309/06 , C07D309/12 , C07D311/58 , C07D311/76 , C07D319/20 , C07D333/16 , C07F9/117 , C07F9/62 , C07F9/6503 , C07F9/6509 , C07F9/655 , C07F9/6553 , A61K31/137 , A61K31/15 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/222 , A61K31/24 , A61K31/27 , A61K31/337 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/4965 , A61K31/505 , A61K31/661
Abstract: Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
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公开(公告)号：US20170355698A1
公开(公告)日：2017-12-14
申请号：US15521199
申请日：2015-10-21
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Rajeev S. Bhide , Zheming Ruan , Robert J. Cherney , Lyndon A.M. Cornelius , T.G.Murali Dhar , Hua Gong , David Marcoux , Michael A. Poss , Lan-ying Qin , Qing Shi , Joseph A. Tino
IPC: C07D487/04
CPC classification number: C07D487/04
Abstract: Disclosed are compounds of Formula (I); or a salt thereof; wherein Qi is (i) Cl, Br, I, —CN, —CH3, or —CF3; or (ii) pyrazole, triazole, or pyridinyl, each substituted with R1; Q2 is pyridinyl, indazolyl, isoquinolinyl, or benzo[d]imidazolyl substituted with R2 and R3; and R1, R2, and R3 are defined herein. Also disclosed are methods of using such compounds as modulators of PI3K, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases.
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公开(公告)号：US09522888B2
公开(公告)日：2016-12-20
申请号：US14831439
申请日：2015-08-20
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Alaric J. Dyckman , T. G. Murali Dhar , Hai-Yun Xiao , John L. Gilmore , Michael G. Yang , Zili Xiao , David Marcoux
IPC: C07F9/02 , C07C211/00 , C07D217/24 , C07C215/42 , C07C217/52 , C07C217/58 , C07C219/24 , C07C233/41 , C07C233/65 , C07C251/50 , C07C251/52 , C07C251/54 , C07C271/34 , C07C317/28 , C07C317/32 , C07C321/16 , C07C321/22 , C07C321/28 , C07D213/32 , C07D213/69 , C07D213/70 , C07D215/12 , C07D231/12 , C07D231/20 , C07D239/26 , C07D241/12 , C07D277/24 , C07D305/08 , C07D309/06 , C07D309/12 , C07D311/58 , C07D311/76 , C07D319/20 , C07D333/16 , C07F7/08 , C07F9/117 , C07F9/62 , C07F9/6503 , C07F9/6509 , C07F9/655 , C07F9/6553 , A61K31/135 , C07D215/14 , C07D241/04 , C07C323/29 , C07C251/38 , C07C251/42 , C07C251/44 , C07D209/46 , C07D213/38 , C07C275/26 , C07C217/74 , C07C323/25 , C07C235/46 , C07F9/54 , C07F9/572 , C07F9/09
CPC classification number: A61K31/695 , A61K31/135 , A61K31/137 , A61K31/15 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/222 , A61K31/24 , A61K31/27 , A61K31/337 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/4965 , A61K31/505 , A61K31/661 , C07B2200/05 , C07C215/42 , C07C217/52 , C07C217/58 , C07C217/74 , C07C219/24 , C07C233/41 , C07C233/65 , C07C235/46 , C07C251/38 , C07C251/42 , C07C251/44 , C07C251/50 , C07C251/52 , C07C251/54 , C07C271/34 , C07C275/26 , C07C317/28 , C07C317/32 , C07C321/16 , C07C321/22 , C07C321/28 , C07C323/25 , C07C323/29 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2602/10 , C07C2603/74 , C07D209/46 , C07D213/32 , C07D213/38 , C07D213/69 , C07D213/70 , C07D215/12 , C07D215/14 , C07D217/24 , C07D231/12 , C07D231/20 , C07D239/26 , C07D241/04 , C07D241/12 , C07D277/24 , C07D305/08 , C07D309/06 , C07D309/12 , C07D311/58 , C07D311/76 , C07D319/20 , C07D333/16 , C07F7/081 , C07F9/091 , C07F9/117 , C07F9/5442 , C07F9/5728 , C07F9/62 , C07F9/65031 , C07F9/650952 , C07F9/65522 , C07F9/655345
Abstract: Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Abstract translation: 和/或其盐，其中R1是-OH或-OP（O）（OH）2，X1，X2，X3，R2，R2a，Ra，Rb和Rc在本文中定义。 还公开了使用这种化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫疾病和血管疾病）中的疾病或病症的进展。
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公开(公告)号：US20160052888A1
公开(公告)日：2016-02-25
申请号：US14831439
申请日：2015-08-20
Applicant: Bristol-Myers Squibb Company
Inventor： Alaric J. Dyckman , T.G. Murali Dhar , Hai-Yun Xiao , John L. Gilmore , Michael G. Yang , Zili Xiao , David Marcoux
IPC: C07D217/24 , C07C217/52 , C07D311/58 , C07D311/76 , C07D309/12 , C07D231/12 , C07D333/16 , C07D309/06 , C07D213/69 , C07C217/58 , C07C233/65 , C07D231/20 , C07C321/28 , C07C321/16 , C07D213/70 , C07F7/08 , C07D213/32 , C07D241/12 , C07C321/22 , C07D277/24 , C07D305/08 , C07D215/12 , C07D239/26 , C07C317/32 , C07C317/28 , C07C219/24 , C07C271/34 , C07C233/41 , C07F9/117 , C07C215/42 , C07C251/50 , C07C251/54 , C07C251/52 , C07F9/655 , C07F9/62 , C07F9/6503 , C07F9/6553 , C07F9/6509 , C07D319/20
CPC classification number: A61K31/695 , A61K31/135 , A61K31/137 , A61K31/15 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/222 , A61K31/24 , A61K31/27 , A61K31/337 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/4965 , A61K31/505 , A61K31/661 , C07B2200/05 , C07C215/42 , C07C217/52 , C07C217/58 , C07C217/74 , C07C219/24 , C07C233/41 , C07C233/65 , C07C235/46 , C07C251/38 , C07C251/42 , C07C251/44 , C07C251/50 , C07C251/52 , C07C251/54 , C07C271/34 , C07C275/26 , C07C317/28 , C07C317/32 , C07C321/16 , C07C321/22 , C07C321/28 , C07C323/25 , C07C323/29 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2602/10 , C07C2603/74 , C07D209/46 , C07D213/32 , C07D213/38 , C07D213/69 , C07D213/70 , C07D215/12 , C07D215/14 , C07D217/24 , C07D231/12 , C07D231/20 , C07D239/26 , C07D241/04 , C07D241/12 , C07D277/24 , C07D305/08 , C07D309/06 , C07D309/12 , C07D311/58 , C07D311/76 , C07D319/20 , C07D333/16 , C07F7/081 , C07F9/091 , C07F9/117 , C07F9/5442 , C07F9/5728 , C07F9/62 , C07F9/65031 , C07F9/650952 , C07F9/65522 , C07F9/655345
Abstract: Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Abstract translation: 公开了式（I），（II），（III），（IV）和（V）的化合物：和/或其盐，其中R 1是-OH或-OP（O）（OH）2， X1，X2，X3，R2，R2a，Ra，Rb和Rc在本文中定义。 还公开了使用这种化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫性疾病和血管疾病）中的疾病或病症的进展。
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公开(公告)号：US11332442B2
公开(公告)日：2022-05-17
申请号：US16991357
申请日：2020-08-12
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： William P. Gallagher , John Ryan Coombs , Carlos A. Guerrero , David Marcoux , Qing Shi , Candice Lee Joe , Sanjeewa Rupasinghe , Jason J. Zhu , Srinivas Kalidindi , Sathasivam Shunmugaraj , Moorthy Kandasamy , Siva Sankar Bondigela , Rajappa Vaidyanathan , Shankar Tulsidas Tendulkar , Sankar Kuppusamy , Francisco González-Bobes
IPC: C07D209/60 , C07C315/04 , C07C303/40 , C07C311/03 , C07C317/24
Abstract: The invention generally relates to a process for preparing compounds, including Compound of Formula (I), useful as key intermediates in the preparation of compounds having RORγt antagonist properties.
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