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1. 发明申请

WO2013079493A1 AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS 审中-公开
标题翻译：作为LRRK2调节剂的氨基嘧啶衍生物
公开(公告)号：WO2013079493A1
公开(公告)日：2013-06-06
申请号：PCT/EP2012/073761
申请日：2012-11-28
申请人： F. HOFFMANN-LA ROCHE AG , BAKER-GLENN, Charles , CHAMBERS, Mark , CHAN, Bryan K. , CHEN, Huifen , ESTRADA, Anthony , SHORE, Daniel , SWEENEY, Zachary
发明人： BAKER-GLENN, Charles , CHAMBERS, Mark , CHAN, Bryan K. , CHEN, Huifen , ESTRADA, Anthony , SHORE, Daniel , SWEENEY, Zachary
IPC分类号： C07D239/42 , C07D239/48 , A61K31/505
CPC分类号： C07D413/12 , C07D239/42 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12
摘要： Compounds of the formula (I), or pharmaceutically acceptable salts thereof, wherein m, n. X, 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 LRRK2 receptor, such as Parkinson's disease.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中m，n。 X，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LRRK2受体（例如帕金森病）相关的疾病的方法。

2. 发明申请

WO2018096159A1 OXADIAZOLONES AS TRANSIENT RECEPTOR POTENTIAL CHANNEL INHIBITORS 审中-公开
公开(公告)号：WO2018096159A1
公开(公告)日：2018-05-31
申请号：PCT/EP2017/080571
申请日：2017-11-27
申请人： F. HOFFMANN-LA ROCHE AG , GENENTECH, INC. , PARAZA PHARMA, INC. , BEAUMIER, Francis , DERY, Martin , LAROUCHE-GAUTHIER, Robin
发明人： BEAUMIER, Francis , DERY, Martin , LAROUCHE-GAUTHIER, Robin , CHEN, Huifen , SHORE, Daniel , VILLEMURE, Elisia , VOLGRAF, Matthew , HU, Baihua , LU, Aijun , CRIDLAND, Andrew , WARD, Stuart
IPC分类号： C07D471/04 , C07D473/30 , C07D487/04 , C07D498/04 , C07D513/04 , A61K31/519 , A61K31/522 , A61K31/53 , A61K31/4985 , A61K31/5025 , A61P29/00 , A61P13/00 , A61P25/00
摘要： The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

3. 发明申请

WO2016142310A1 TRICYCLIC DLK INHIBITORS AND USES THEREOF 审中-公开
标题翻译： TRICYCLIC DLK抑制剂及其用途
公开(公告)号：WO2016142310A1
公开(公告)日：2016-09-15
申请号：PCT/EP2016/054725
申请日：2016-03-07
申请人： F. HOFFMANN-LA ROCHE AG , GENENTECH, INC.
发明人： ESTRADA, Anthony , HUESTIS, Malcolm , KELLAR, Terry , PATEL, Snahel , SHORE, Daniel , SIU, Michael
IPC分类号： C07D491/14 , A61K31/436 , A61K31/519 , A61K31/5383 , A61K31/553 , A61P25/28
CPC分类号： C07D498/14 , A61K31/5383 , A61K31/553 , A61K45/06 , C07D491/14 , C07D519/00
摘要： The invention relates to compounds of formula (I) and salts thereof, wherein ring A and R 1 -R 2 have any of the values defined in the specification. The compounds and salts are useful for treating DLK mediated disorders. The invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof, as well as methods of using said compounds, salts, or compositions as DLK inhibitors and for treating neurodegeneration diseases and disorders.
摘要翻译：本发明涉及式（I）化合物及其盐，其中环A和R1-R2具有说明书中定义的任何值。化合物和盐可用于治疗DLK介导的病症。本发明还提供包含式（I）化合物或其药学上可接受的盐的药物组合物，以及使用所述化合物，盐或组合物作为DLK抑制剂和治疗神经变性疾病和病症的方法。

4. 发明申请

WO2015052264A1 SUBSTITUTED HETEROCYCLIC SULFONAMIDE COMPOUNDS USEFUL AS TRPA1 MODULATORS 审中-公开
标题翻译：取代的杂环磺酰胺化合物有用作TRPA1调节剂
公开(公告)号：WO2015052264A1
公开(公告)日：2015-04-16
申请号：PCT/EP2014/071593
申请日：2014-10-09
申请人： F. HOFFMANN-LA ROCHE AG , GENENTECH, INC.
发明人： CHEN, Huifen , CHU, Yanyan , DO, Steven , ESTRADA, Anthony , HU, Baihua , KOLESNIKOV, Aleksandr , LIN, Xingyu , LYSSIKATOS, Joseph P. , SHORE, Daniel , VERMA, Vishal , WANG, Lan , WU, Guosheng , YUEN, Po-wai
IPC分类号： C07D403/12 , C07D401/14 , C07D401/12 , C07D403/14 , C07D417/12 , C07D451/02 , C07D491/048 , C07D207/48 , A61K31/4025 , A61P29/00
CPC分类号： C07D207/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D417/12 , C07D451/02 , C07D491/048
摘要： The invention is concerned with the compounds of formula I or II: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I or II as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
摘要翻译：本发明涉及式I或II化合物及其盐。此外，本发明涉及制备方法和使用式I或II化合物的方法以及含有这些化合物的药物组合物。该化合物可用于治疗TRPA1介导的疾病和病症，例如疼痛。

5. 发明申请

WO2018015410A1 BICYCLIC PROLINE COMPOUNDS 审中-公开
标题翻译：双环脯氨酸化合物
公开(公告)号：WO2018015410A1
公开(公告)日：2018-01-25
申请号：PCT/EP2017/068170
申请日：2017-07-18
申请人： F. HOFFMANN-LA ROCHE AG , GENENTECH, INC.
发明人： VERMA, Vishal , SHORE, Daniel , VOLGRAF, Matthew , ESTRADA, Anthony A. , LYSSIKATOS, Joseph
IPC分类号： C07D401/14 , C07D401/12 , A61K31/439 , A61P11/00
摘要： The invention is concerned with the compounds of formula (I) and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
摘要翻译：本发明涉及式（I）化合物及其盐。另外，本发明涉及制备方法和使用式（I）化合物的方法以及含有这些化合物的药物组合物。该化合物可用于治疗由TRPA1介导的疾病和病症，例如疼痛。

6. 发明申请

WO2018162607A1 OXADIAZOLE TRANSIENT RECEPTOR POTENTIAL CHANNEL INHIBITORS 审中-公开
公开(公告)号：WO2018162607A1
公开(公告)日：2018-09-13
申请号：PCT/EP2018/055690
申请日：2018-03-07
申请人： F. HOFFMANN-LA ROCHE AG , GENENTECH, INC.
发明人： CHEN, Huifen , SAFINA, Brian , SHORE, Daniel , TERRETT, Jack , VILLEMURE, Elisia , VOLGRAF, Matthew , WARD, Stuart , LU, Aijun , LAROUCHE-GAUTHIER, Robin , BEAUMIER, Francis , DERY, Martin , CONSTANTINEAU-FORGET, Lea , GRAND-MAITRE, Chantal , LEPISSIER, Luce
IPC分类号： C07D471/04 , C07D473/04 , C07D487/04 , A61K31/519 , A61K31/522 , A61P25/04 , A61P29/00
摘要： The invention relates to compounds of formula I: (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

7. 发明申请

WO2016128529A1 1-(HET)ARYLSULFONYL-(PYRROLIDINE OR PIPERIDINE)-2-CARBOXAMIDE DERIVATIVES AND THEIR USE AS TRPA1 ANTAGONISTS 审中-公开
标题翻译： 1-（HET）ARYLSULFONYL-（吡咯烷或哌啶）-2-羧酰胺衍生物及其作为TRPA1拮抗剂的用途
公开(公告)号：WO2016128529A1
公开(公告)日：2016-08-18
申请号：PCT/EP2016/052950
申请日：2016-02-12
申请人： F. HOFFMANN-LA ROCHE AG , GENENTECH, INC.
发明人： ESTRADA, Anthony , VOLGRAF, Matthew , CHEN, Huifen , KOLESNIKOV, Aleksandr , VILLEMURE, Elisia , VERMA, Vishal , WANG, Lan , SHORE, Daniel , DO, Steven , YUEN, Po-wai , HU, Baihua , WU, Guosheng , LIN, Xingyu , LU, Aijun
IPC分类号： C07D403/12 , C07D401/14 , C07D405/14 , C07D401/12 , C07D403/14 , C07D409/14 , C07D417/12 , C07D417/14 , A61K31/4025 , A61K31/402 , A61K31/4545 , A61P29/00 , A61P11/00 , A61P11/06 , A61P11/14 , A61P17/04 , A61P19/02 , A61P27/16
CPC分类号： C07D417/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/12 , C07F9/65127
摘要： The invention is concerned with the compounds of formula I and salts thereof and other compounds of formulas II-IX as disclosed herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formulas I-IX as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain or asthma.
摘要翻译：本发明涉及式I化合物及其盐和本文公开的式II-IX的其它化合物。此外，本发明涉及制造方法和使用式I-IX化合物的方法以及含有这些化合物的药物组合物。该化合物可用于治疗由TRPA1介导的疾病和病症，例如疼痛或哮喘。

8. 发明申请

WO2013139882A1 PYRAZOLOPYRIDINES FOR TREATMENT OF PARKINSONS DISEASE 审中-公开
标题翻译：用于治疗帕金森病的吡唑啉酮
公开(公告)号：WO2013139882A1
公开(公告)日：2013-09-26
申请号：PCT/EP2013/055878
申请日：2013-03-21
申请人： F. HOFFMANN-LA ROCHE AG , GENENTECH, INC.
发明人： CHAN, Bryan , ESTRADA, Anthony , SHORE, Daniel , SWEENEY, Zachary
IPC分类号： C07D471/04 , A61K31/437 , A61P25/16
CPC分类号： C07D471/04
摘要： The invention relates to a compound of formula (1A) or (1B), or a pharmaceutically acceptable salt thereof, Wherein R 1 is a group selected from alkyl, monocyclic heterocycloalkyl, bicyclic heterocycloalkyl and cycloalkyl, each of which is optionally substituted by one or more groups selected from alkyl, halo and cycloalkyl; for formula (1A): one, two or three of X 1 , X 2 , X 3 and X 4 are N, and the remainder are each independently CR 2 ; or for formula (1B): X 4 is C or N; and one or two of X 1 , X 2 and X 3 are independently selected from N and NR 8 , and the remainder are each independently CR 2 ; such that X 1 , X 2 ,X 3 ,X 4 and N form a heteroaryl group; each R 2 is independently selected from H, alkyl, CN, halo, heteroaryl, heterocycloalkyl, cycloalkyl, OR 4 , CONR 5 R 6 and SO 2 R 7 , wherein said alkyl, heteroaryl, heterocycloalkyl and cycloalkyl groups are each optionally further substituted by one or more groups selected from alkyl, halo and OR 9 ; each R 8 is independently selected from H and alkyl, wherein said alkyl group is optionally further substituted by one or more groups selected from CN, halo, heteroaryl, heterocycloalkyl, cycloalkyl, OR 4 , CONR 5 R 6 and SO 2 R 7 ; R 4 , R 5 , R 6 , R 7 and R 9 are each independently selected from H and alkyl; or R 5 and R 6 together with the nitrogen to which they are attached are linked to form a cyclic group which optionally further comprises one or more heteroatoms selected from O, N and S; with the proviso that when the compound is of formula (IB), the compound is other than 3-(5-isopropyl-4H-1,2,4-triazol-3-yl)-N- (tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[4,3-c]pyridin-4-amine or 3-(5-cyclopropyl-4H-,2,4-triazol-3-yl)-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[4,3-c]pyridin-4-amine. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula (1A) and (1B).
摘要翻译：本发明涉及式（1A）或（1B）化合物或其药学上可接受的盐，其中R1是选自烷基，单环杂环烷基，双环杂环烷基和环烷基的基团，其各自任选被一个或多个选自烷基，卤代和环烷基的基团; 对于式（1A）：X1，X2，X3和X4中的一个，两个或三个是N，其余各自独立地是CR 2; 或式（1B）：X4为C或N; X1，X2和X3中的一个或两个独立地选自N和NR8，其余各自独立地为CR2; 使得X1，X2，X3，X4和N形成杂芳基; 每个R 2独立地选自H，烷基，CN，卤素，杂芳基，杂环烷基，环烷基，OR 4，CONR 5 R 6和SO 2 R 7，其中所述烷基，杂芳基，杂环烷基和环烷基各自任选进一步被一个或多个选自烷基，卤素和OR9; 每个R 8独立地选自H和烷基，其中所述烷基任选被一个或多个选自CN，卤素，杂芳基，杂环烷基，环烷基，OR4，CONR5R6和SO2R7的基团进一步取代; R4，R5，R6，R7和R9各自独立地选自H和烷基; 或者R 5和R 6与它们所连接的氮一起连接形成环状基团，任选地还包含一个或多个选自O，N和S的杂原子; 条件是当化合物为式（IB）时，该化合物不同于3-（5-异丙基-4H-1,2,4-三唑-3-基）-N-（四氢-2H-吡喃-2-基）吡啶-4-基）-1H-吡唑并[4,3-c]吡啶-4-胺或3-（5-环丙基-4H-，2,4-三唑-3-基）-N-（四氢-2H-吡喃 -4-基）-1H-吡唑并[4,3-c]吡啶-4-胺。其它方面涉及药物组合物，治疗用途和制备式（1A）和（1B）化合物的方法。

9. 发明申请

WO2013079494A1 2-PHENYLAMINOPYRIMIDINE DERIVATIVES AS KINASE LRRK2 MODULATORS FOR THE TREATMENT OF PARKINSON'S DISEASE 审中-公开
标题翻译：作为激素治疗帕金森病的激素LRRK2调节剂的2-苯基亚氨基嘧啶衍生物
公开(公告)号：WO2013079494A1
公开(公告)日：2013-06-06
申请号：PCT/EP2012/073762
申请日：2012-11-28
申请人： F. HOFFMANN-LA ROCHE AG , BAKER-GLENN, Charles , BURDICK, Daniel Jon , CHAMBERS, Mark , CHAN, Bryan K. , CHEN, Huifen , ESTRADA, Anthony , GUNZNER-TOSTE, Janet , SHORE, Daniel , SWEENEY, Zachary , WANG, Shumei , ZHAO, Guiling
发明人： BAKER-GLENN, Charles , BURDICK, Daniel Jon , CHAMBERS, Mark , CHAN, Bryan K. , CHEN, Huifen , ESTRADA, Anthony , GUNZNER-TOSTE, Janet , SHORE, Daniel , SWEENEY, Zachary , WANG, Shumei , ZHAO, Guiling
IPC分类号： C07D239/47 , C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D487/04 , C07D498/08 , C07D491/107 , A61K31/505 , A61K31/506 , A61P25/16
CPC分类号： C07D498/18 , C07D239/47 , C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D487/04 , C07D491/107 , C07D498/08 , C07D498/10
摘要： Specific Compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein m, X, R, R 2 , R 3 , R, R 6 and R 7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
摘要翻译：式（I）的具体化合物或其药学上可接受的盐，其中m，X，R，R 2，R 3，R 6，R 6和R 7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LRRK2受体（例如帕金森病）相关的疾病的方法。

10. 发明申请

WO2011151360A1 AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS 审中-公开
标题翻译：作为LRRK2调节剂的氨基嘧啶衍生物
公开(公告)号：WO2011151360A1
公开(公告)日：2011-12-08
申请号：PCT/EP2011/059009
申请日：2011-06-01
申请人： F. HOFFMANN-LA ROCHE AG , BAKER-GLENN, Charles , BURDICK, Daniel Jon , CHAMBERS, Mark , CHAN, Bryan K. , CHEN, Huifen , ESTRADA, Anthony , GUNZNER, Janet L. , SHORE, Daniel , SWEENEY, Zachary Kevin , WANG, Shumei , ZHAO, Guiling
发明人： BAKER-GLENN, Charles , BURDICK, Daniel Jon , CHAMBERS, Mark , CHAN, Bryan K. , CHEN, Huifen , ESTRADA, Anthony , GUNZNER, Janet L. , SHORE, Daniel , SWEENEY, Zachary Kevin , WANG, Shumei , ZHAO, Guiling
IPC分类号： C07D403/14 , C07D473/16 , A61K31/52
CPC分类号： C07D413/14 , C07D403/14 , C07D413/12 , C07D473/16 , C07D498/06 , C07D498/08
摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R 1 , R 2 , R 3 , R 5 , R 6 and R 7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
摘要翻译：式I化合物或其药学上可接受的盐，其中m，n。 X，R 1，R 2，R 3，R 5，R 6和R 7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LRRK2受体（例如帕金森病）相关的疾病的方法。

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