公开(公告)号：US20200239437A1

公开(公告)日：2020-07-30

申请号：US16635593

申请日：2018-08-03

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Alaric J. Dyckman ,  Dharmpal S. Dodd ,  Tasir Shamsul Haque ,  Brian K. Whiteley ,  John L. Gilmore

IPC: C07D401/14 ,  C07D405/14 ,  C07D409/14

Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: Y is Formula (II), or Formula (III); R1, R2, R2a, R2b, R2c, R3, R4, R5, m, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

公开(公告)号：US20190262311A1

公开(公告)日：2019-08-29

申请号：US16330964

申请日：2017-09-08

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Alaric J. Dyckman ,  Dharmpal S. Dodd ,  Tasir Shamsul Haque ,  Louis J. Lombardo ,  John E. Macor ,  Christopher P. Mussari ,  Laxman Pasunoori ,  Michael A. Poss ,  Sreekantha Ratna Kumar ,  Shoshana L. Posy ,  David R. Tortolani ,  Brian K. Whiteley ,  Ramesh Kumar Sistla ,  Subramanya Hegde ,  Anupama Kandhi Ramachandra Reddy

IPC: A61K31/404 ,  A61P37/06 ,  A61P29/00 ,  A61K9/00

Abstract: Disclosed are compounds of Formula (I) N-oxide, or salt thereof, wherein R1, R2, R3, R4, R5, m, n, and p are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

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。

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。

公开(公告)号：US09115054B2

公开(公告)日：2015-08-25

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: C07C215/42 ,  C07F9/117

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。

公开(公告)号：US12187723B2

公开(公告)日：2025-01-07

申请号：US17609443

申请日：2020-05-07

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Alaric J. Dyckman ,  Laxman Pasunoori ,  Sreekantha Ratna Kumar ,  Srinivasan Kunchithapatham Duraisamy ,  Pitani Veera Venkata Srinivas ,  Vikram Bhogadi ,  Subramanya Hegde

IPC: C07D471/04 ,  C07D519/00

Abstract: Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, R1, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

公开(公告)号：USRE49893E1

公开(公告)日：2024-04-02

申请号：US17584155

申请日：2022-01-25

Applicant: Bristol-Myers Squibb Company

Inventor： Alaric J. Dyckman ,  Dharmpal S. Dodd ,  Tasir Shamsul Hague ,  Louis J. Lombardo ,  John E. Macor ,  Christopher P. Mussari ,  Laxman Pasunoori ,  Sreekantha Ratna Kumar ,  Trevor C. Sherwood ,  Shoshana L. Posy ,  Ramesh Kumar Sistla ,  Subramanya Hegde ,  Anupama Kandhi Ramachandra Reddy

IPC: A61K31/4196 ,  A61K31/437 ,  A61K31/4427 ,  A61K45/06 ,  C07D249/00 ,  C07D471/04

CPC classification number: A61K31/4196 ,  A61K31/437 ,  A61K31/4427 ,  A61K45/06 ,  C07D249/00 ,  C07D471/04

Abstract: Disclosed are compounds of Formula (I)




or a salt thereof, wherein R1, R2, R3, R4, R5, m, n, and p are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

公开(公告)号：US20230098244A1

公开(公告)日：2023-03-30

申请号：US17699944

申请日：2022-03-21

Applicant: Bristol-Myers Squibb Company

Inventor： Alaric J. Dyckman ,  Dharmpal S. Dodd ,  Christopher P. Mussari ,  Trevor C. Sherwood ,  John L. Gilmore ,  Tsair Shamsul Haque ,  Brian K. Whiteley ,  David R. Tortolani ,  Shoshana L. Posy ,  John E. Macor ,  Louis J. Lombardo ,  Ramesh Kumar Sistla ,  Anupama Kandhi Ramachandra Reddy ,  Subramanya Hegde ,  Laxman Pasunoori ,  Sreekantha Ratna Kumar

IPC: C07D498/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

Abstract: Disclosed are compounds of Formula (I) or salts thereof, wherein Ring Het, R1, R2, R3, R4, R5, m, n, and p are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

公开(公告)号：US11447466B2

公开(公告)日：2022-09-20

申请号：US16635593

申请日：2018-08-03

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Alaric J. Dyckman ,  Dharmpal S. Dodd ,  Tasir Shamsul Haque ,  Brian K. Whiteley ,  John L. Gilmore

IPC: A61K31/4545 ,  A61P29/00 ,  A61P37/00 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: Y is Formula (II), or Formula (III); R1, R2, R2a, R2b, R2c, R3, R4, R5, m, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

公开(公告)号：US20210403468A1

公开(公告)日：2021-12-30

申请号：US17287612

申请日：2019-10-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： John L. GILMORE ,  Shoshana L. Posy ,  Alaric J. Dyckman

IPC: C07D471/04 ,  C07D519/00 ,  C07D401/14

Abstract: Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein X is CR1 or N; and G, A, R1; and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.