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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：US20180221344A1
公开(公告)日：2018-08-09
申请号：US15749611
申请日：2016-08-02
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Hai-Yun Xiao , T.G. Murali Dhar , Bin Jiang , Jingwu Duan
IPC: A61K31/4184 , A61K31/4188 , A61P37/02
CPC classification number: A61K31/4184 , A61K31/4188 , A61P37/02 , C07D487/04 , C07D487/14
Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: Ring A is 3- to 6-membered carbocyclic or heterocyclic ring; X is CR1 or N; Y is —(CR5R5)m—; Z is —(CR5R5)n—; and q, R1, R2, R3, R4, R6, R7, R8, R9, and R10 are defined 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：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：US20160251309A1
公开(公告)日：2016-09-01
申请号：US15148222
申请日：2016-05-06
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： T.G. Murali Dhar , Hai-Yun Xiao
IPC: C07D207/50 , C07C25/22 , C07C49/67
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.
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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：US10335392B2
公开(公告)日：2019-07-02
申请号：US15749611
申请日：2016-08-02
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Hai-Yun Xiao , T.G. Murali Dhar , Bin Jiang , Jingwu Duan
IPC: C07D487/04 , C07D487/14 , A61K31/4184 , A61K31/4188 , A61P37/02
Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: Ring A is 3- to 6-membered carbocyclic or heterocyclic ring; X is CR1 or N; Y is —(CR5R5)m—; Z is —(CR5R5)n—; and q, R1, R2, R3, R4, R6, R7, R8, R9, and R10 are defined 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：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：US09487481B2
公开(公告)日：2016-11-08
申请号：US15148222
申请日：2016-05-06
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： T. G. Murali Dhar , Hai-Yun Xiao
IPC: C07C25/22 , C07C49/67 , C07D207/50
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.
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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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