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公开(公告)号：US11701373B2
公开(公告)日：2023-07-18
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
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 , 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 , 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 , C07F7/08 , C07F7/081 , C07F9/091 , C07F9/117 , C07F9/5442 , C07F9/5728 , C07F9/62 , C07F9/65031 , C07F9/65522 , C07F9/650952 , C07F9/655345 , C07B2200/05 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2602/10 , C07C2603/74
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.-
公开(公告)号：US10709719B2
公开(公告)日：2020-07-14
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 , A61K31/135 , 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：US10308652B2
公开(公告)日：2019-06-04
申请号：US15558708
申请日：2016-03-17
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Stephen T. Wrobleski , Gregory D. Brown , Shuqun Lin , Jingwu Duan , Zhonghui Lu , Murali T. G. Dhar , Hai-Yun Xiao , Andrew J. Tebben
IPC: C07D487/14 , C07D491/147 , A61K31/5025 , A61P37/00 , C07D471/14 , C07D487/06 , A61P29/00 , A61P27/00
Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is N; W is: —(CR3R3)2-5-, —(CR3R3)x-Y—(CR3R3)y-, —Y—(CR3R3)2-3-Y—, —CR3R3-Y—(CR3R3)2-Y—, —Y—(CR3R3)2-Y—CR3R3-; and Y, R1, R2, R3, R5, R6, R8, x, and y are define herein. Also disclosed are methods of using such compounds as modulators of TNFα, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
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公开(公告)号：US20170042917A1
公开(公告)日：2017-02-16
申请号：US15337843
申请日：2016-10-28
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 , A61K31/351 , A61K31/415 , A61K31/381 , A61K31/44 , A61K31/137 , A61K31/166 , A61K31/4406 , A61K31/4409 , A61K31/4402 , A61K31/4965 , A61K31/165 , A61K31/4174 , A61K31/426 , A61K31/337 , A61K31/47 , A61K31/505 , A61K31/27 , A61K31/17 , A61K31/352 , A61K31/15 , A61K31/661 , A61K31/222 , A61K31/24 , A61K31/135
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：US09458171B2
公开(公告)日：2016-10-04
申请号：US14590233
申请日：2015-01-06
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Jingwu Duan , T. G. Murali Dhar , Bin Jiang , Zhonghui Lu , Hai-Yun Xiao
IPC: C07D417/14 , C07D471/10 , C07D493/04 , C07D207/12 , C07D207/16 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D405/06 , C07D417/06 , C07D487/04 , C07D403/12 , C07D401/14 , C07D413/14 , C07D405/12 , C07D407/12 , C07D407/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/10
CPC classification number: C07D207/12 , C07D207/16 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D407/12 , C07D407/14 , C07D409/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/10 , C07D493/04 , C07D493/08
Abstract: Described are 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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Patent Agency Ranking
公开(公告)号：US20140235591A1
公开(公告)日：2014-08-21
申请号：US14185164
申请日：2014-02-20
Applicant: Bristol-Myers Squibb Company
Inventor： T. G. Murali Dhar , Hai-Yun Xiao , Alaric J. Dyckman , Eric J. Chan , Marta Dabros , Daniel Richard Roberts
IPC: C07F9/09 , C07C215/42
CPC classification number: C07D207/50 , C07B2200/07 , C07B2200/13 , C07C25/22 , C07C49/67 , C07C215/42 , C07C2601/08 , C07C2602/10 , C07F9/117
Abstract: Disclosed are compounds of Formula (I) and/or a salt thereof; wherein R is —OH or —OP(O)(OH)2. 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）和/或其盐的化合物; 其中R是-OH或-OP（O）（OH）2。 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：US11059784B2
公开(公告)日：2021-07-13
申请号：US16636662
申请日：2018-08-08
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Alaric J. Dyckman , Ling Li , T. G. Murali Dhar , Hai-Yun Xiao
IPC: C07D213/53 , C07D207/12 , A61P37/06 , C07D211/96 , C07D211/40
Abstract: Disclosed are compounds of Formula (I): (I) or a salt thereof, wherein: X is CH or N; Y is CH or N; R1 is —OH or —OP(O)(OH)2; L is —CR3═N—O—CRaRa— or CRaR—O—N═CR3; L2 is a bond, —C(O)—, or S(O)2—; and R2, R3, Ra, m, and n 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：US11058696B2
公开(公告)日：2021-07-13
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：US20190218193A1
公开(公告)日：2019-07-18
申请号：US16329399
申请日：2017-08-31
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： David Marcoux , Hai-Yun Xiao , T.G. Murali Dhar , Alaric J. Dyckman
IPC: C07D277/84 , C07D261/20 , C07D333/74 , C07D417/10 , C07F9/117 , C07D417/14
CPC classification number: C07D277/84 , C07D261/20 , C07D277/60 , C07D333/50 , C07D333/74 , C07D417/06 , C07D417/10 , C07D417/14 , C07F9/117 , C07F9/65324 , C07F9/6541 , C07F9/655354
Abstract: Disclosed are compounds of Formula (I), Formula (II), Formula (III), and Formula (IV) or salts thereof, wherein R2 is —OH or —OP(O)(OH)2; and R1 is 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：US20170304332A1
公开(公告)日：2017-10-26
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 , C07F9/6553 , C07F9/655 , C07F9/6509 , C07F9/6503 , C07F9/62 , C07F9/572 , C07F9/54 , C07F9/117 , C07F9/09 , C07F7/08 , C07D333/16 , C07D319/20 , C07D311/76 , C07D311/58 , C07D309/12 , C07D309/06 , C07D305/08 , C07D277/24 , C07D241/12 , C07D241/04 , C07D239/26 , C07D231/20 , C07D231/12 , C07D217/24 , C07D215/14 , C07D215/12 , C07D213/70 , C07D213/69 , C07D213/38 , C07D213/32 , C07D209/46 , C07C323/29 , C07C323/25 , C07C321/28 , C07C321/22 , C07C321/16 , C07C317/32 , C07C317/28 , C07C275/26 , C07C271/34 , C07C251/54 , C07C251/52 , C07C251/50 , C07C251/44 , C07C251/42 , C07C251/38 , C07C235/46 , C07C233/65 , C07C233/41 , C07C219/24 , C07C217/74 , C07C217/58 , C07C217/52 , C07C215/42 , A61K31/661 , A61K31/505 , A61K31/4965 , A61K31/47 , A61K31/4409 , A61K31/4406 , A61K31/4402 , A61K31/44 , A61K31/426 , A61K31/4174 , A61K31/415 , A61K31/381 , A61K31/352 , A61K31/351 , A61K31/337 , A61K31/27 , A61K31/24 , A61K31/222 , A61K31/17 , A61K31/166 , A61K31/165 , A61K31/15 , A61K31/137 , A61K31/135 , C07C2601/04 , C07C2601/08 , C07C2603/74 , C07C2602/10 , C07C2601/02
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.
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