公开(公告)号：US11667636B2

公开(公告)日：2023-06-06

申请号：US17559084

申请日：2021-12-22

申请人： Escient Pharmaceuticals, Inc.

发明人： Marion Lanier ,  Marcos Sainz ,  Marcus Boehm ,  Liming Huang ,  Esther Martinborough ,  Brandon Selfridge ,  Adam Yeager

IPC分类号： C07D471/04 ,  C07D277/64 ,  C07D333/56 ,  C07D333/54 ,  C07D519/00 ,  C07D231/56 ,  C07D235/06 ,  C07D263/56 ,  C07D409/12 ,  C07D333/58

CPC分类号： C07D471/04 ,  C07D231/56 ,  C07D235/06 ,  C07D263/56 ,  C07D277/64 ,  C07D333/54 ,  C07D333/56 ,  C07D333/58 ,  C07D409/12 ,  C07D519/00

摘要： Methods are provided for modulating MRGPRX2 generally, or for treating a MRGPRX2 dependent condition more specifically, by contacting the MRGPRX2 or administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I):




or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein A, B, C, D, E, G, W, Y, Z, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

公开(公告)号：US20220340530A1

公开(公告)日：2022-10-27

申请号：US17545494

申请日：2021-12-08

申请人： Escient Pharmaceuticals, Inc.

发明人： Marion Lanier ,  Marcus Boehm ,  Liming Huang ,  Esther Martinborough ,  Marcos Sainz ,  Brandon Selfridge ,  Adam Yeager

IPC分类号： C07D213/73 ,  C07D403/04 ,  C07D405/04 ,  C07D239/94 ,  C07D239/48 ,  C07D209/08 ,  C07D471/04 ,  C07D277/56 ,  C07D231/14 ,  C07C255/60 ,  C07D277/62 ,  C07D401/12

摘要： Methods are provided for modulating MRGPRX2 generally, or for treating a MRGPRX2 dependent condition more specifically, by contacting the MRGPRX2 or administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I): or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein D, W, Z, R1, R2 and R3 are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

公开(公告)号：US20230053860A1

公开(公告)日：2023-02-23

申请号：US17531660

申请日：2021-11-19

申请人： Escient Pharmaceuticals, Inc.

发明人： Adam Yeager ,  Brandon Selfridge ,  Marcos Sainz ,  Esther Martinborough ,  Marcus Boehm ,  Liming Huang

IPC分类号： C07D265/30 ,  C07C69/78 ,  C07C255/41 ,  C07D213/79 ,  C07D241/24 ,  C07D261/18 ,  C07D277/64 ,  C07D333/38

摘要： Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q1, Q2, Z, R, R1, R2, R3, R4 and R5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

公开(公告)号：US20220340559A1

公开(公告)日：2022-10-27

申请号：US17559084

申请日：2021-12-22

申请人： Escient Pharmaceuticals, Inc.

发明人： Marion Lanier ,  Marcos Sainz ,  Marcus Boehm ,  Liming Huang ,  Esther Martinborough ,  Brandon Selfridge ,  Adam Yeager

IPC分类号： C07D471/04 ,  C07D277/64 ,  C07D333/56 ,  C07D333/54 ,  C07D333/58 ,  C07D231/56 ,  C07D235/06 ,  C07D263/56 ,  C07D409/12 ,  C07D519/00

摘要： Methods are provided for modulating MRGPRX2 generally, or for treating a MRGPRX2 dependent condition more specifically, by contacting the MRGPRX2 or administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I): or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein A, B, C, D, E, G, W, Y, Z, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

公开(公告)号：US20220177434A1

公开(公告)日：2022-06-09

申请号：US17506447

申请日：2021-10-20

申请人： Escient Pharmaceuticals, Inc.

发明人： Marion Lanier ,  Marcus Boehm ,  Liming Huang ,  Esther Martinborough ,  Marcos Sainz ,  Brandon Selfridge ,  Adam Yeager

IPC分类号： C07D215/44 ,  C07D239/94 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D401/14 ,  C07D417/12 ,  C07D487/04 ,  C07D413/14 ,  C07D471/04

摘要： Methods are provided for modulating MRGPRX2 or a MRGPRX2 ortholog generally, or for treating a MRGPRX2 or a MRGPRX2 ortholog dependent condition more specifically, by contacting the MRGPRX2 or the MRGPRX2 ortholog by administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I): or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein W, Z, R1, R2, R3, R4, R5, R6 and Rx are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

公开(公告)号：US20210340106A1

公开(公告)日：2021-11-04

申请号：US17231834

申请日：2021-04-15

申请人： Escient Pharmaceuticals, Inc.

发明人： Marcos Sainz ,  Adam Yeager ,  Brandon Selfridge ,  Esther Martinborough ,  Marcus Boehm ,  Liming Huang

IPC分类号： C07D215/227 ,  C07D209/46 ,  C07D217/24 ,  C07D209/34 ,  C07D413/12

摘要： Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein m, n, p, t, A, B, Z, R1, R2 and R3 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

公开(公告)号：US20230159474A1

公开(公告)日：2023-05-25

申请号：US17858840

申请日：2022-07-06

申请人： Escient Pharmaceuticals, Inc.

发明人： Adam Yeager ,  Brandon Selfridge ,  Marcos Sainz ,  Esther Martinborough ,  Marcus Boehm ,  Liming Huang

IPC分类号： C07D265/30 ,  C07C69/78 ,  C07C255/41 ,  C07D213/79 ,  C07D241/24 ,  C07D261/18 ,  C07D277/64 ,  C07D333/38

CPC分类号： C07D265/30 ,  C07C69/78 ,  C07C255/41 ,  C07D213/79 ,  C07D241/24 ,  C07D261/18 ,  C07D277/64 ,  C07D333/38 ,  A61K45/06

摘要： Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I):




or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q1, Q2, Z, R, R1, R2, R3, R4 and R5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

公开(公告)号：US11643399B2

公开(公告)日：2023-05-09

申请号：US17531660

申请日：2021-11-19

申请人： Escient Pharmaceuticals, Inc.

发明人： Adam Yeager ,  Brandon Selfridge ,  Marcos Sainz ,  Esther Martinborough ,  Marcus Boehm ,  Liming Huang

IPC分类号： C07D265/30 ,  C07C69/78 ,  C07C255/41 ,  C07D213/79 ,  C07D241/24 ,  C07D261/18 ,  C07D277/64 ,  C07D333/38 ,  A61K45/06

CPC分类号： C07D265/30 ,  C07C69/78 ,  C07C255/41 ,  C07D213/79 ,  C07D241/24 ,  C07D261/18 ,  C07D277/64 ,  C07D333/38 ,  A61K45/06

摘要： Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I):




or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q1, Q2, Z, R, R1, R2, R3, R4 and R5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

公开(公告)号：US20230065217A1

公开(公告)日：2023-03-02

申请号：US17484993

申请日：2021-09-24

申请人： Escient Pharmaceuticals, Inc.

发明人： Marion Lanier ,  Marcus Boehm ,  Liming Huang ,  Esther Martinborough ,  Marcos Sainz ,  Brandon Selfridge ,  Adam Yeager

IPC分类号： C07D215/46 ,  C07D401/12 ,  C07D405/12 ,  C07D513/04 ,  C07D471/04 ,  C07D405/14 ,  C07D417/12 ,  C07D401/14 ,  C07D495/04

摘要： Methods are provided for modulating MRGPR X2 generally, or for treating a MRGPR X2 or a MRGPR X2 ortholog dependent condition, more specifically, by contacting the MRGPR X2 or the MRGPR X2 ortholog by administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I): or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein W, Z, R1, R2, R3, R4, R5, R6 and Rx are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

公开(公告)号：US20210032213A1

公开(公告)日：2021-02-04

申请号：US16831638

申请日：2020-03-26

申请人： Escient Pharmaceuticals, Inc.

发明人： Adam Yeager ,  Brandon Selfridge ,  Marcos Sainz ,  Esther Martinborough ,  Marcus Boehm ,  Liming Huang

IPC分类号： C07D265/30 ,  C07C69/78 ,  C07C255/41 ,  C07D277/64 ,  C07D241/24 ,  C07D213/79 ,  C07D333/38 ,  C07D261/18

摘要： Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I). or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q1, Q2, Z, R, R1, R2, R3, R4 and R5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.