公开(公告)号：US20190016688A1

公开(公告)日：2019-01-17

申请号：US16100193

申请日：2018-08-09

申请人： Roche Palo Alto LLC

发明人： Chris Allen Broka ,  David Scott Carter ,  Michael Patrick Dillon ,  Ronald Charles Hawley ,  Alam Jahangir ,  Clara Jeou Jen Lin ,  Daniel Warren Parish

IPC分类号： C07D239/49 ,  C07D239/48 ,  C07D417/12 ,  C07D413/12 ,  A61K31/505 ,  C07D405/12 ,  C07D403/12

摘要： Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein X is O, D, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

公开(公告)号：US09505726B2

公开(公告)日：2016-11-29

申请号：US14547632

申请日：2014-11-19

申请人： Roche Palo Alto LLC

发明人： Chris Allen Broka ,  Ronald Charles Hawley

IPC分类号： A61K31/166 ,  C07C233/64 ,  C07D241/12 ,  C07C237/32 ,  C07D265/30 ,  C07D405/14 ,  C07D417/12 ,  C07C237/42 ,  C07D213/56 ,  C07D213/61 ,  C07D213/81 ,  C07D231/14 ,  C07D241/24 ,  C07D261/18 ,  C07D263/34 ,  C07D277/56 ,  C07D285/06 ,  C07D295/125 ,  C07D307/68 ,  C07D309/08 ,  C07D333/38 ,  C07D401/12 ,  C07D403/12

CPC分类号： C07D241/12 ,  C07C237/32 ,  C07C237/42 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/56 ,  C07D213/61 ,  C07D213/81 ,  C07D231/14 ,  C07D241/24 ,  C07D261/18 ,  C07D263/34 ,  C07D265/30 ,  C07D277/56 ,  C07D285/06 ,  C07D295/125 ,  C07D307/68 ,  C07D309/08 ,  C07D333/38 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14 ,  C07D417/12

摘要： Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.

公开(公告)号：US09849136B2

公开(公告)日：2017-12-26

申请号：US15459361

申请日：2017-03-15

申请人： Roche Palo Alto LLC

发明人： Li Chen ,  Michael Patrick Dillon ,  Lichun Feng ,  Ronald Charles Hawley ,  Minmin Yang

IPC分类号： A01N61/00 ,  A61K31/00 ,  A61K31/5377 ,  A61K31/426 ,  A61K31/428 ,  A61K31/421 ,  A61K31/42 ,  A61K31/425 ,  A61K31/501

CPC分类号： A61K31/5377 ,  A61K31/42 ,  A61K31/421 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K31/501 ,  C07D261/08 ,  C07D263/32 ,  C07D275/02 ,  C07D277/30 ,  C07D277/56 ,  C07D277/66 ,  C07D413/14 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14

摘要： A method for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor with compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is an optionally substituted thiazole, oxazole, isothiazole or isoxazole and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein.

公开(公告)号：US09617254B2

公开(公告)日：2017-04-11

申请号：US15093320

申请日：2016-04-07

申请人： Roche Palo Alto LLC

发明人： Li Chen ,  Michael Patrick Dillon ,  Lichun Feng ,  Ronald Charles Hawley ,  Minmin Yang

IPC分类号： A01N61/00 ,  A61K31/00 ,  C07D417/14 ,  C07D261/08 ,  C07D263/32 ,  C07D275/02 ,  C07D277/30 ,  C07D277/66 ,  C07D417/12 ,  C07D277/56 ,  C07D413/14 ,  C07D417/10

CPC分类号： A61K31/5377 ,  A61K31/42 ,  A61K31/421 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K31/501 ,  C07D261/08 ,  C07D263/32 ,  C07D275/02 ,  C07D277/30 ,  C07D277/56 ,  C07D277/66 ,  C07D413/14 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14

摘要： Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.

公开(公告)号：US20170096416A1

公开(公告)日：2017-04-06

申请号：US15383245

申请日：2016-12-19

申请人： Roche Palo Alto LLC

发明人： Li Chen ,  Michael Patrick Dillon ,  Lichun Feng ,  Ronald Charles Hawley ,  Minmin Yang

IPC分类号： C07D405/14 ,  C07D401/10 ,  C07D403/12 ,  C07D401/14 ,  C07D231/12 ,  C07D231/56

CPC分类号： C07D405/14 ,  C07D213/12 ,  C07D213/14 ,  C07D231/12 ,  C07D231/56 ,  C07D401/10 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

摘要： Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted pyrazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.

公开(公告)号：US20130296310A1

公开(公告)日：2013-11-07

申请号：US13932419

申请日：2013-07-01

申请人： Roche Palo Alto LLC

发明人： Li Chen ,  Michael Patrick Dillon ,  Lichun Feng ,  Ronald Charles Hawley ,  Minmin Yang

IPC分类号： C07D277/30 ,  C07D275/02 ,  C07D277/66 ,  C07D277/56 ,  C07D261/08 ,  C07D413/14 ,  C07D417/14 ,  C07D417/10 ,  C07D263/32 ,  C07D417/12

CPC分类号： A61K31/5377 ,  A61K31/42 ,  A61K31/421 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K31/501 ,  C07D261/08 ,  C07D263/32 ,  C07D275/02 ,  C07D277/30 ,  C07D277/56 ,  C07D277/66 ,  C07D413/14 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14

摘要： Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.

摘要翻译： 式I化合物或其药学上可接受的盐，其中R1是式A或式B的基团，X，R2，R3，R4，R5，R6，Ra和Rb如本文所定义。 还提供了使用该化合物治疗由P2X3和/或P2X2 / 3受体拮抗剂介导的疾病的方法和制备本发明化合物的方法。

公开(公告)号：US20130225570A1

公开(公告)日：2013-08-29

申请号：US13866212

申请日：2013-04-19

申请人： Roche Palo Alto LLC

发明人： Chris Allen Broka ,  David Scott Carter ,  Michael Patrick Dillon ,  Anthony P.D.W. Ford ,  Ronald Charles Hawley ,  Alam Jahangir ,  Amy Geraldine Moore ,  Daniel Warren Parish

IPC分类号： A61K31/505 ,  A61K31/538 ,  A61K31/506

CPC分类号： A61K31/506 ,  A61K31/505 ,  A61K31/513 ,  A61K31/538 ,  Y10S514/826

摘要： Methods for treating respiratory and gastrointestinal diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

摘要翻译： 用于治疗由P2X3和/或P2X2 / 3受体拮抗剂介导的呼吸道和胃肠道疾病的方法，所述方法包括向有需要的受试者施用有效量的式（I）化合物或其药学上可接受的盐， 其中D，X，Y，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如本文所定义。

公开(公告)号：US20230100975A1

公开(公告)日：2023-03-30

申请号：US17655843

申请日：2022-03-22

申请人： Roche Palo Alto LLC

发明人： Chris Allen Broka ,  David Scott Carter ,  Michael Patrick Dillon ,  Ronald Charles Hawley ,  Alam Jahangir ,  Clara Jeou Jen Lin ,  Daniel Warren Parish

IPC分类号： C07D239/49 ,  C07D239/48 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/505

摘要： Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein X is O, D, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

公开(公告)号：US20180141919A1

公开(公告)日：2018-05-24

申请号：US15842759

申请日：2017-12-14

申请人： Roche Palo Alto LLC

发明人： Chris Allen Broka ,  David Scott Carter ,  Michael Patrick Dillon ,  Ronald Charles Hawley ,  Alam Jahangir ,  Clara Jeou Jen Lin ,  Daniel Warren Parish

IPC分类号： C07D239/49 ,  C07D417/12 ,  C07D413/12 ,  C07D409/12 ,  A61K31/505 ,  C07D403/12 ,  C07D239/48 ,  C07D405/12 ,  A61K31/506

CPC分类号： C07D239/49 ,  A61K31/505 ,  A61K31/506 ,  C07D239/48 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein X is O, D, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

公开(公告)号：US20170143672A1

公开(公告)日：2017-05-25

申请号：US15422121

申请日：2017-02-01

申请人： Roche Palo Alto LLC

发明人： Michael Patrick Dillon ,  Ronald Charles Hawley ,  Li Chen ,  Lichun Feng ,  Minmin Yang

IPC分类号： A61K31/41 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/5377

CPC分类号： A61K31/41 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/5377 ,  C07D241/12 ,  C07D257/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D407/10 ,  C07D409/12 ,  C07D413/10 ,  C07D417/10 ,  C07D417/12 ,  C07D471/04 ,  C07D491/10 ,  C07D491/107 ,  C07D498/08

摘要： A method of antagonizing P2X3 and/or P2X2/3 receptors or treating a disease misregulation of P2X3 and/or P2X2/3 receptors treating a patient with a compound of formula I wherein R1, R2, R3, R4, R5 and R6 are as defined herein, or a pharmaceutically acceptable salt thereof wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5 and R6 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.