公开(公告)号：US12129243B2

公开(公告)日：2024-10-29

申请号：US18513400

申请日：2023-11-17

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： C07D471/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04

摘要： Methods are provided for modulating MRGPRX2 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：US20240246980A1

公开(公告)日：2024-07-25

申请号：US18496540

申请日：2023-10-27

申请人： Escient Pharmaceuticals, Inc.

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

IPC分类号： C07D487/04 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/5025 ,  A61K31/5377 ,  C07D401/04 ,  C07D471/04 ,  C07D519/00

CPC分类号： C07D487/04 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/5025 ,  A61K31/5377 ,  C07D401/04 ,  C07D471/04 ,  C07D519/00

摘要： Methods are provided for modulating MRGPRD generally, or for treating a MRGPRD dependent condition more specifically, by contacting the MRGPRD 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 salt, isomer, hydrate, solvate or isotope thereof, wherein A, B, C, D, L, R1, R2, R3, R4, m, n, and p are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

公开(公告)号：US20240124416A1

公开(公告)日：2024-04-18

申请号：US18513418

申请日：2023-11-17

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： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04

摘要： Methods are provided for modulating MRGPRX2 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：US11952346B2

公开(公告)日：2024-04-09

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

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

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：US20240059667A1

公开(公告)日：2024-02-22

申请号：US18192313

申请日：2023-03-29

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： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04 ,  C07D471/04

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04 ,  C07D471/04

摘要： Methods are provided for modulating MRGPRX2 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：US20240351987A1

公开(公告)日：2024-10-24

申请号：US18615563

申请日：2024-03-25

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 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

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

摘要： Methods are provided for modulating MRGPR X2 generally, or for treating a MRGPR X2 dependent condition more specifically, by contacting the MRGPR X2 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 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：US20240124414A1

公开(公告)日：2024-04-18

申请号：US18513387

申请日：2023-11-17

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： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04

摘要： Methods are provided for modulating MRGPRX2 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：US11840521B2

公开(公告)日：2023-12-12

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 ,  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：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.