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1. 发明申请

WO2008104474A1 DIAMINOPYRIMIDINES 审中-公开
标题翻译：二氨基嘧啶
公开(公告)号：WO2008104474A1
公开(公告)日：2008-09-04
申请号：PCT/EP2008/051944
申请日：2008-02-18
申请人： F. HOFFMANN-LA ROCHE AG , DILLON, Michael Patrick , DU BOIS, Daisy Joe , JAHANGIR, Alam
发明人： DILLON, Michael Patrick , DU BOIS, Daisy Joe , JAHANGIR, Alam
IPC分类号： C07D239/48 , A61K31/505 , A61P13/10
CPC分类号： C07D239/48
摘要： Compounds of formula (I) wherein R 1 and R 2 are as defined herein. Also disclosed are methods of making and using the subject compounds.
摘要翻译：其中R 1和R 2的式（I）化合物如本文所定义。还公开了制备和使用本发明化合物的方法。

2. 发明申请

WO2010066629A2 NOVEL AZAINDOLES 审中-公开
标题翻译：新型锌
公开(公告)号：WO2010066629A2
公开(公告)日：2010-06-17
申请号：PCT/EP2009/066311
申请日：2009-12-03
申请人： F. HOFFMANN-LA ROCHE AG , DILLON, Michael Patrick , DU BOIS, Daisy Joe , HAWLEY, Ronald Charles , LAI, Yingjie , WANG, Beihan
发明人： DILLON, Michael Patrick , DU BOIS, Daisy Joe , HAWLEY, Ronald Charles , LAI, Yingjie , WANG, Beihan
IPC分类号： C07D487/04 , A61K31/505 , A61P25/04 , A61P11/00 , A61P11/06 , A61P1/00 , A61P13/00 , A61P15/00
CPC分类号： C07D487/04
摘要： The application discloses compounds of the Formula (A) wherein: or a pharmaceutically acceptable salt thereof, wherein, R a , R b R c , R d , R e , R f , R g , R h and R i are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X 3 and/or a P2X 2/3 receptor antagonist and methods of making the compounds.
摘要翻译：本申请公开了式（A）的化合物，其中：或其药学上可接受的盐，其中R a，R b R c，R d，R e，R f，R g，Rh和R 1如本文所定义。还提供了使用该化合物治疗与P2X3和/或P2X2 / 3受体拮抗剂相关疾病的方法和制备该化合物的方法。

3. 发明申请

WO2007025900A1 DIAMINOPYRIMIDINES AS P2X3 AND P3X2/3 MODULATORS 审中-公开
标题翻译：作为P2X3和P3X2 / 3调节剂的二氨基嘧啶
公开(公告)号：WO2007025900A1
公开(公告)日：2007-03-08
申请号：PCT/EP2006/065525
申请日：2006-08-21
申请人： F. HOFFMANN-LA ROCHE AG , DILLON, Michael Patrick , JAHANGIR, Alam , LUI, Alfred Sui-Ting , WILHELM, Robert Stephen
发明人： DILLON, Michael Patrick , JAHANGIR, Alam , LUI, Alfred Sui-Ting , WILHELM, Robert Stephen
IPC分类号： C07D239/48 , C07D401/12 , A61K31/506 , A61P11/00 , A61P13/00
CPC分类号： C07D401/12 , C07D239/48 , C07D471/04
摘要： Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein A, D, E, G, J, X, Y, Z 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 compounds.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中A，D，E，G，J，X，Y，ZR 6，R 7和R 7， SUP> 8 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该化合物的方法。

4. 发明申请

WO2007025925A1 DIAMINOPYRIMIDINES AS P2X3 AND P2X2/3 MODULATORS 审中-公开
标题翻译：作为P2X3和P2X2 / 3调节剂的二氨基嘧啶
公开(公告)号：WO2007025925A1
公开(公告)日：2007-03-08
申请号：PCT/EP2006/065606
申请日：2006-08-23
申请人： F. HOFFMANN-LA ROCHE AG , BROKA, Chris Allen , CARTER, David Scott , DILLON, Michael Patrick , FORD, Anthony P.D.W. , HAWLEY, Ronald Charles , JAHANGIR, Alam , MOORE, Amy Geraldine , PARISH, Daniel Warren
发明人： BROKA, Chris Allen , CARTER, David Scott , DILLON, Michael Patrick , FORD, Anthony P.D.W. , HAWLEY, Ronald Charles , JAHANGIR, Alam , MOORE, Amy Geraldine , PARISH, Daniel Warren
IPC分类号： A61K31/505 , A61K31/506 , A61P11/00 , A61P11/06 , A61P1/00
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 P2X 3 and/or a P2X 2/3 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, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined herein.
摘要翻译：用于治疗由P2X 3和/或P2X 3/3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，R 8， >如本文所定义。

5. 发明申请

WO2007025901A1 DIAMINOPYRIMIDINES AS P2X3 AND P2X2/3 MODULATORS 审中-公开
标题翻译：作为P2X3和P2X2 / 3调节剂的二氨基嘧啶
公开(公告)号：WO2007025901A1
公开(公告)日：2007-03-08
申请号：PCT/EP2006/065526
申请日：2006-08-21
申请人： F. HOFFMANN-LA ROCHE AG , DILLON, Michael Patrick , JAHANGIR, Alam , LIN, Clara Jeou Jen
发明人： DILLON, Michael Patrick , JAHANGIR, Alam , LIN, Clara Jeou Jen
IPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , A61K31/506 , A61P11/00 , A61P13/00
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12
摘要： Compounds and methods for treating diseases mediated by a P2X 3 and/or a P2X 2/3 receptor antagonist, the compounds being of formula (I) wherein D, X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined herein.
摘要翻译：用于治疗P2X 3和/或P2X 2/3受体拮抗剂介导的疾病的化合物和方法，式（I）化合物其中D，X，R R 1，R 2，R 3，R 4，R 5，R 5，R 5， R 6，R 7和R 8如本文所定义。

6. 发明申请

WO2009077365A1 NOVEL IMIDAZOLE-SUBSTITUTED ARYLAMIDES 审中-公开
标题翻译：新咪唑取代的芳纶
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
发明人： 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。

7. 发明申请

WO2008081012A1 SPIROPIPERIDINE DERIVATIVES AS NK3 ANTAGONISTS 审中-公开
标题翻译：作为NK3拮抗剂的螺吡啶衍生物
公开(公告)号：WO2008081012A1
公开(公告)日：2008-07-10
申请号：PCT/EP2008/050005
申请日：2008-01-02
申请人： F. HOFFMANN-LA ROCHE AG , CAROON, Joanie Marie , DILLON, Michael Patrick , HAN, Bo , NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter
发明人： CAROON, Joanie Marie , DILLON, Michael Patrick , HAN, Bo , NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter
IPC分类号： C07D498/10 , A61K31/537 , A61P25/00
CPC分类号： C07D498/10
摘要： The present invention relates to a compound of formula (I) wherein R 1 is hydrogen or lower alkyl; R 2 is lower alkyl, lower hydroxyalkyl or -(CHR 5 ) x -A; R 5 is hydrogen, lower alkyl or lower hydroxyalkyl, or is heteroaryl optionally substituted by lower alkyl; A is cycloalkyl, aryl, heterocyclyl or heteroaryl, which rings are optionally substituted one or more R 6 , wherein R 6 is lower alkyl, lower alkoxy, lower alkylsulfonyl, cyano, halogen, lower alkyl substituted by halogen or lower alkoxy substituted by halogen, or is aryl, heterocyclyl or heteroaryl optionally substituted by lower alkyl or is cycloalkyl optionally substituted by lower alkyl; x is 0, 1, 2 or 3; or R 1 , R 2 may form together with the N-atom heterocyclyl or heteroaryl, which rings are optionally substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, lower alkylsulfonyl, halogen, cycloalkyl, benzyl or aryl; R 3 is hydrogen or halogen; R 4 is hydrogen or lower alkyl; R 7 is hydrogen, halogen or lower alkyl; m is 1 or 2; when m is 2, R 3 may be the same or not; n is 1 or 2; o is 1 or 2; when o is 2, R 7 may be the same or not; or to a pharmaceutically suitable acid addition salt thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及其中R 1为氢或低级烷基的式（I）化合物; R 2是低级烷基，低级羟基烷基或 - （CHR 5 O）x -A; R 5为氢，低级烷基或低级羟烷基，或为任选被低级烷基取代的杂芳基; A是环烷基，芳基，杂环基或杂芳基，该环任选被一个或多个R 6取代，其中R 6是低级烷基，低级烷氧基，低级烷基磺酰基，氰基，卤素，被卤素取代的低级烷基或被卤素取代的低级烷氧基，或被任选被低级烷基取代的芳基，杂环基或杂芳基或任选被低级烷基取代的环烷基; x为0,1,2或3; 或R 1，R 2可以与N-原子杂环基或杂芳基一起形成，该环任选被一个或多个选自以下的取代基取代：低级烷基低级烷氧基，低级烷基磺酰基，卤素，环烷基，苄基或芳基; R 3是氢或卤素; R 4是氢或低级烷基; R 7是氢，卤素或低级烷基; m为1或2; 当m为2时，R 3可以相同或不相同; n为1或2; o是1或2; 当o为2时，R 7可以相同或不相同; 或其药学上适合的酸加成盐。已经发现，本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

8. 发明申请

WO2009077367A1 NOVEL PYRAZOLE-SUBSTITUTED ARYLAMIDES 审中-公开
标题翻译：新型吡唑取代的芳纶
公开(公告)号：WO2009077367A1
公开(公告)日：2009-06-25
申请号：PCT/EP2008/066989
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
发明人： CHEN, Li , DILLON, Michael Patrick , FENG, Lichun , HAWLEY, Ronald Charles , YANG, Minmin
IPC分类号： C07D213/12 , C07D213/14 , C07D401/14 , A61K31/33 , A61P25/06
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, R 1 is optionally substituted pyrazolyl, and R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X 3 and/or a P2X 2/3 receptor antagonists and methods of making the compounds.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中R 1为任选取代的吡唑基，R 2，R 3，R 4，R 5，R 6，R 7和R 8如本文所定义。还公开了使用该化合物治疗与P2X3和/或P2X2 / 3受体拮抗剂相关疾病的方法和制备该化合物的方法。

9. 发明申请

WO2009077366A1 TRIAZOLE-SUBSTITUTED ARYLAMIDE DERIVATIVES AND THEIR USE AS P2X3 AND /OR P2X2/3 PURINERGIC RECEPTOR ANTAGONISTS 审中-公开
标题翻译：三唑取代的亚氨酰胺衍生物及其作为P2X3和/或P2X2 / 3纯化受体拮抗剂的用途
公开(公告)号：WO2009077366A1
公开(公告)日：2009-06-25
申请号：PCT/EP2008/066987
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
发明人： CHEN, Li , DILLON, Michael Patrick , FENG, Lichun , HAWLEY, Ronald Charles , YANG, Minmin
IPC分类号： C07D249/06 , C07D403/12 , C07D403/14 , A61K31/4192 , A61K31/497 , A61P11/00 , A61P13/02 , A61P29/00
CPC分类号： C07D403/12 , C07D249/06 , C07D401/14
摘要： Compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein, R 1 is optionally substituted triazolyl, and R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X 3 and/or a P2X 2/3 receptor antagonists and methods of making the compounds.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中R 1为任选取代的三唑基，R 2，R 3，R 4，R 5，R 6，R 7和R 8如本文所定义。还公开了使用该化合物治疗与P2X3和/或P2X2 / 3受体拮抗剂相关疾病的方法和制备该化合物的方法。

10. 发明申请

WO2010149634A1 NOVEL INDOLE, INDAZOLE AND BENZIMIDAZOLE ARYLAMIDES AS P2X3 AND/OR P2X2/3 ANTAGONISTS 审中-公开
标题翻译：新型吲哚，茚满和苯并咪唑类ARYLAMIDES作为P2X3和/或P2X2 / 3拮抗剂
公开(公告)号：WO2010149634A1
公开(公告)日：2010-12-29
申请号：PCT/EP2010/058757
申请日：2010-06-22
申请人： F. HOFFMANN-LA ROCHE AG , DILLON, Michael Patrick , KRAUSS, Nancy Elisabeth
发明人： DILLON, Michael Patrick , KRAUSS, Nancy Elisabeth
IPC分类号： C07D401/04 , C07D401/14 , A61K31/4439 , A61K31/497 , A61P13/00 , A61P29/00 , A61P1/04 , A61P11/00
CPC分类号： C07D401/14 , A61K31/497 , C07D401/04 , C07D401/10
摘要： Compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein, X, Y, Z, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X 3 and/or a P2X 2/3 receptor antagonists and methods of making the compounds.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中X，Y，Z，R 1，R 2，R 3，R 4和R 5如本文所定义。还公开了使用该化合物治疗与P2X3和/或P2X2 / 3受体拮抗剂相关疾病的方法和制备该化合物的方法。

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