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公开(公告)号：WO2013064468A1
公开(公告)日：2013-05-10
申请号：PCT/EP2012/071407
申请日：2012-10-29
申请人： F. HOFFMANN-LA ROCHE AG , ALAM, Muzaffar , DU BOIS, Daisy Joe , HAWLEY, Ronald Charles , KENNEDY-SMITH, Joshua , MINATTI, Ana Elena , PALMER, Wylie Solang , SILVA, Tania , THAKKAR, Kshitij Chhabilbshai , WILHELM, Robert Stephen
发明人： ALAM, Muzaffar , DU BOIS, Daisy Joe , HAWLEY, Ronald Charles , KENNEDY-SMITH, Joshua , MINATTI, Ana Elena , PALMER, Wylie Solang , SILVA, Tania , THAKKAR, Kshitij Chhabilbshai , WILHELM, Robert Stephen
IPC分类号： C07D401/14 , A61K31/44 , A61P29/00
CPC分类号： C07D401/14
摘要： Disclosed are compounds of Formula (I), useful for treatment of autoimmune and inflammatory diseases associated with IL-2 inhibition via modulation of calcium release-activated calcium (CRAC) channels. Also disclosed are methods of making and using the compounds for treatment of diseases associated with CRAC channels.
摘要翻译： 公开了式（I）化合物，其可用于通过调节钙释放激活的钙（CRAC）通道治疗与IL-2抑制相关的自身免疫性和炎性疾病。 还公开了制备和使用化合物治疗与CRAC通道相关疾病的方法。
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公开(公告)号：WO2008055840A1
公开(公告)日：2008-05-15
申请号：PCT/EP2007/061771
申请日：2007-10-31
申请人： F. HOFFMANN-LA ROCHE AG , CHEN, Li , DILLON, Michael Patrick , FENG, Lichun , HAWLEY, Ronald Charles , YANG, Minmin
IPC分类号： C07D263/32 , C07D277/30 , C07D277/66 , C07D401/14 , A61K31/19 , A61P13/00
CPC分类号： C07D401/14 , C07D263/32 , C07D277/30 , C07D277/66
摘要： Compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: R 1 is a group of formula A or formula B; and X, R 2 , R 3 , R 4 , R 5 , R 6 , R a and R b are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X 3 and/or a P2X 2/3 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：R 1是式A或式B的基团; 和X，R 2，R 3，R 4，R 5，R 6， 其中R a，R b和R b如本文所定义。 还提供了使用该化合物治疗由P2X 3和/或P2X 3/3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。
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公开(公告)号：WO2018118668A1
公开(公告)日：2018-06-28
申请号：PCT/US2017/066562
申请日：2017-12-15
申请人： AFFERENT PHARMACEUTICALS, INC. , IBRAHIM, Prabha , HAWLEY, Ronald Charles , FORD, Anthony, P. , SMITH, Steven, A.
IPC分类号： A61K31/505 , C07D239/28
摘要： Provided are novel salts and polymorphs of 5-(2,4-diamino-pyrimidin-5-yloxy)-4-isopropyl-2-methoxy-benzenesulfonamide, which are potentially useful for modulating a condition mediated by a P2X3 or P2X2/3 receptor. Also provided are pharmaceutical formulations and methods of administration and dosing of these salts and polymorphs to subjects in need thereof.
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公开(公告)号：WO2018111738A1
公开(公告)日：2018-06-21
申请号：PCT/US2017/065504
申请日：2017-12-11
申请人： AFFERENT PHARMACEUTICALS, INC. , HAWLEY, Ronald Charles , IBRAHIM, Prabha , FORD, Anthony, P. , GEVER, Joel, R.
IPC分类号： A61K31/505 , C07D239/48
摘要： Disclosed herein are substituted pyrazole-pyrimidine compounds of Formula (I) and variants thereof for the treatment, for example, of diseases associated with P2X purinergic receptors. In one embodiment, the P2X3 and/or P2X2/3 antagonists disclosed herein are potentially useful, for example, for the treatment of visceral organ, cardiovascular and pain-related diseases, conditions and disorders.
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公开(公告)号：WO2013092463A1
公开(公告)日：2013-06-27
申请号：PCT/EP2012/075716
申请日：2012-12-17
申请人： F. HOFFMANN-LA ROCHE AG , ALAM, Muzaffar , DU BOIS, Daisy, Joe , HAWLEY, Ronald, Charles , KENNEDY-SMITH, Joshua , MINATTI, Ana, Elena , THAKKAR, Kshitij, Chhabilbhai , WILHELM, Robert, Stephen
发明人： ALAM, Muzaffar , DU BOIS, Daisy, Joe , HAWLEY, Ronald, Charles , KENNEDY-SMITH, Joshua , MINATTI, Ana, Elena , THAKKAR, Kshitij, Chhabilbhai , WILHELM, Robert, Stephen
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00
CPC分类号： C07D471/04
摘要： Disclosed are compounds of Formula (I), useful for treatment of autoimmune and inflammatory diseases associated with IL-2 inhibition via modulation of calcium release-activated calcium (CRAC) channels. Also disclosed are methods of making and using the compounds for treatment of diseases associated with CRAC channels.
摘要翻译： 公开了式（I）化合物，其可用于通过调节钙释放激活的钙（CRAC）通道治疗与IL-2抑制相关的自身免疫性和炎性疾病。 还公开了制备和使用化合物治疗与CRAC通道相关疾病的方法。
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公开(公告)号：WO2011036130A1
公开(公告)日：2011-03-31
申请号：PCT/EP2010/063838
申请日：2010-09-21
申请人： F. HOFFMANN-LA ROCHE AG , ALAM, Muzaffar , DU BOIS, Daisy Joe , HAWLEY, Ronald Charles , KENNEDY-SMITH, Joshua , MINATTI, Ana Elena , PALMER, Wylie Solang , SILVA, Tania , WILHELM, Robert Stephen
发明人： ALAM, Muzaffar , DU BOIS, Daisy Joe , HAWLEY, Ronald Charles , KENNEDY-SMITH, Joshua , MINATTI, Ana Elena , PALMER, Wylie Solang , SILVA, Tania , WILHELM, Robert Stephen
IPC分类号： C07D209/18 , C07D403/04 , C07D403/10 , C07D403/14 , C07D405/14 , C07D409/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , A61K31/404 , A61P11/00
CPC分类号： C07D403/04 , C07D209/18 , C07D403/10 , C07D403/14 , C07D405/14 , C07D409/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14
摘要： Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 and R 4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with calcium release-activated calcium channels (CRAC).
摘要翻译： 式（I）化合物或其药学上可接受的盐，其中R 1，R 2，R 3和R 4如本文所定义。 还公开了制备化合物和使用该化合物治疗与钙释放激活的钙通道（CRAC）相关的疾病的方法。
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公开(公告)号：WO2010066629A3
公开(公告)日：2011-03-31
申请号：PCT/EP2009066311
申请日：2009-12-03
申请人： HOFFMANN LA ROCHE , DILLON MICHAEL PATRICK , DU BOIS DAISY JOE , HAWLEY RONALD CHARLES , LAI YINGJIE , WANG BEIHAN
IPC分类号： A61K31/505 , A61P1/00 , A61P11/00 , A61P11/06 , A61P13/00 , A61P15/00 , A61P25/04 , C07D487/04
CPC分类号： C07D487/04
摘要： The application discloses compounds of the Formula (A) wherein: or a pharmaceutically acceptable salt thereof, for the treatment of pain, genitourinary conditions, gastroenterological conditions, and respiratory conditions, via inhibition of P2X3 and P2X2/3.
摘要翻译： 本申请公开了通过抑制P2X3和P2X2 / 3，其中：或其药学上可接受的盐用于治疗疼痛，泌尿生殖器疾病，胃肠病学和呼吸状况的化合物。
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公开(公告)号：WO2009077365A1
公开(公告)日：2009-06-25
申请号：PCT/EP2008/066985
申请日：2008-12-08
申请人： F. HOFFMANN-LA ROCHE AG , CHEN, Li , DILLON, Michael Patrick , FENG, Lichun , HAWLEY, Ronald Charles , YANG, Minmin
IPC分类号： C07D233/64 , C07D401/14 , C07D403/12 , A61K31/33 , A61P25/06
CPC分类号： C07D233/64 , C07D401/14 , C07D403/12
摘要： Compounds of the formula (I):wherein R 1 is optionally substituted imidazolyl, and R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X 3 and/or a P2X 2/3 receptor antagonist and methods of making the subject compounds.
摘要翻译： 式（I）化合物：其中R 1为任选取代的咪唑基，R2，R3，R4，R5，R6，R7和R8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。
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公开(公告)号：WO2017160569A1
公开(公告)日：2017-09-21
申请号：PCT/US2017/021477
申请日：2017-03-09
申请人： AFFERENT PHARMACEUTICALS INC. , HAWLEY, Ronald Charles , IBRAHIM, Prabha , FORD, Anthony, P. , GEVER, Joel, R.
IPC分类号： C07D237/02 , C07D253/06 , A61K31/501
摘要： The present disclosure provides pyrimidine compounds and uses thereof, for example, for the treatment of diseases associated with P2X purinergic receptors. In certain aspects, the present disclosure provides P2X3 and/or P2X2/3 antagonists which are useful, for example, for the treatment of visceral organ, cardiovascular and pain-related diseases, conditions and disorders.
摘要翻译： 本公开提供嘧啶化合物及其用途，例如用于治疗与P2X嘌呤能受体相关的疾病。 在某些方面，本公开内容提供了可用于例如治疗内脏器官，心血管和疼痛相关疾病，病症和障碍的P2X3和/或P2X2 / 3拮抗剂。
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公开(公告)号：WO2011073276A1
公开(公告)日：2011-06-23
申请号：PCT/EP2010/069798
申请日：2010-12-15
申请人： EVOTEC AG , HAN, Xiaochun , HAWLEY, Ronald Charles , HOGG, Joan Heather , LIN, Xiao-Fa , TREJO-MARTIN, Teresa Alejandra
发明人： HAN, Xiaochun , HAWLEY, Ronald Charles , HOGG, Joan Heather , LIN, Xiao-Fa , TREJO-MARTIN, Teresa Alejandra
IPC分类号： C07D265/36 , A61K31/538 , A61P11/00 , C07D498/04
CPC分类号： C07D265/36 , C07D498/04
摘要： Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein E, Z, m, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with potassium channel modulation.
摘要翻译： 式（I）化合物或其药学上可接受的盐，其中E，Z，m，R 1，R 2，R 3，R 4和R 5如本文所定义。 还公开了制备化合物和使用该化合物治疗与钾通道调节相关的疾病的方法。
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