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1. 发明申请

WO2010138589A1 BICYCLIC PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE 审中-公开
标题翻译： PI10K PI3K抑制剂PI3K抑制剂化合物的选择性及其使用方法
公开(公告)号：WO2010138589A1
公开(公告)日：2010-12-02
申请号：PCT/US2010/036199
申请日：2010-05-26
申请人： GENENTECH, INC. , F. HOFFMANN-LA ROCHE AG , CASTANEDO, Georgette , CHAN, Bryan , GOLDSTEIN, David Michael , KONDRU, Rama K. , LUCAS, Matthew C. , PALMER, Wylie Solang , PRICE, Stephen , SAFINA, Brian , SAVY, Pascal Pierre Alexandre , SEWARD, Eileen Mary , SUTHERLIN, Daniel P. , SWEENEY, Zachary Kevin
发明人： CASTANEDO, Georgette , CHAN, Bryan , GOLDSTEIN, David Michael , KONDRU, Rama K. , LUCAS, Matthew C. , PALMER, Wylie Solang , PRICE, Stephen , SAFINA, Brian , SAVY, Pascal Pierre Alexandre , SEWARD, Eileen Mary , SUTHERLIN, Daniel P. , SWEENEY, Zachary Kevin
IPC分类号： C07D487/04 , C07D491/04 , C07D513/04 , A61K31/519 , A61P35/00 , A61P9/00 , A61P29/00 , A61P25/00
CPC分类号： C07D513/04 , C07D487/04 , C07D491/04 , C07D495/04
摘要： Formula (I) ((Ia) and (Ib)) compounds wherein (i) X 1 is N and X 2 is S, (ii) X 1 is CR 7 and X 2 is S, (iii) X 1 is N and X 2 is NR 2 , or (iv) X 1 is CR 7 and X 2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula (I) for in vitro, in situ , and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译：式（I）（（Ia）和（Ib））化合物，其中（i）X1是N，X2是S，（ii）X1是CR7，X2是S，（iii）X1是N，X2是NR2，或 iv）X1是CR7，X2是O，包括立体异构体，互变异构体，代谢物和药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗由脂质激酶如炎症，免疫学和癌症介导的病症。公开了使用式（I）化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

2. 发明申请

WO2011101429A1 PYRIDO[3,2-D]PYRIMIDINE PI3K DELTA INHIBITOR COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：吡咯并[3,2-D]吡嗪PI3K DELTA抑制剂化合物及其使用方法
公开(公告)号：WO2011101429A1
公开(公告)日：2011-08-25
申请号：PCT/EP2011/052384
申请日：2011-02-18
申请人： F. HOFFMANN-LA ROCHE AG , CASTANEDO, Georgette , CHAN, Bryan , LUCAS, Matthew C. , SAFINA, Brian , SUTHERLIN, Daniel P. , SWEENEY, Zachary Kevin
发明人： CASTANEDO, Georgette , CHAN, Bryan , LUCAS, Matthew C. , SAFINA, Brian , SUTHERLIN, Daniel P. , SWEENEY, Zachary Kevin
IPC分类号： C07D471/04 , A61K31/519 , A61P35/00
CPC分类号： C07D471/04 , C07D491/107
摘要： Formula (I) compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译：式（I）化合物，包括立体异构体，几何异构体，互变异构体，代谢物及其药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗由脂质激酶如炎症，免疫学障碍和癌症介导的病症。公开了使用式（I）化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理条件中的这种疾病的方法。

3. 发明申请

WO2020061377A1 SPIROCYCLIC 2,3-DIHYDRO-7-AZAINDOLE COMPOUNDS AND USES THEREOF 审中-公开
公开(公告)号：WO2020061377A1
公开(公告)日：2020-03-26
申请号：PCT/US2019/052023
申请日：2019-09-19
申请人： GENENTECH, INC. , F. HOFFMANN-LA ROCHE AG
发明人： MALHOTRA, Sushant , STIVALA, Craig , WEI, BinQing , CHAN, Bryan , HEFFRON, Timothy , LAINCHBURY, Michael , MADIN, Andrew , PANCHAL, Terry Aaron , SEWARD, Eileen Mary , BLENCH, Toby , CARTWRIGHT, Matthew W. , DECHAUX, Elsa Amandine , ELLIOTT, Richard , GANCIA, Emanuela
IPC分类号： A61K31/437 , A61P35/00 , C07D471/04
摘要： Spirocyclic 2,3-dihydro-7-azaindole compounds of formula (I), variations thereof, and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the spirocyclic 2,3-dihydro-7-azaindole compounds.

4. 发明申请

WO2018183964A1 ISOQUINOLINES AS INHIBITORS OF HPK1 审中-公开
公开(公告)号：WO2018183964A1
公开(公告)日：2018-10-04
申请号：PCT/US2018/025573
申请日：2018-03-30
申请人： GENENTECH, INC. , F. HOFFMANN-LA ROCHE AG
发明人： CHAN, Bryan , DROBNICK, Joy , GAZZARD, Lewis , HEFFRON, Timothy , LIANG, Jun , MALHOTRA, Sushant , MENDONCA, Rohan , RAJAPAKSA, Naomi , STIVALA, Craig , TELLIS, John , WANG, Weiru , WEI, BinQing , ZHOU, Aihe , CARTWRIGHT, Matthew W. , LAINCHBURY, Michael , GANCIA, Emanuela , SEWARD, Eileen , MADIN, Andrew , FAVOR, David , FONG, Kin Chiu , HU, Yonghan , GOOD, Andrew
IPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , C07D487/14 , C07D217/22 , C07D401/04 , C07D409/14 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/04 , C07D491/04 , C07D498/04 , C07D513/04 , C07D519/00
摘要： Isoquinoline compounds and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1 -dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1 -dependent disorders, methods for enhancing an immune response, and methods for preparing the isoquinoline compounds.

5. 发明申请

WO2018183956A1 NAPHTHYRIDINES AS INHIBITORS OF HPK1 审中-公开
公开(公告)号：WO2018183956A1
公开(公告)日：2018-10-04
申请号：PCT/US2018/025562
申请日：2018-03-30
申请人： GENENTECH, INC. , F. HOFFMANN-LA ROCHE AG
发明人： CHAN, Bryan , DANIELS, Blake , DROBNICK, Joy , GAZZARD, Lewis , HEFFRON, Timothy , HUESTIS, Malcolm , LIANG, Jun , MALHOTRA, Sushant , MENDONCA, Rohan , RAJAPAKSA, Naomi , SIU, Michael , STIVALA, Craig , TELLIS, John , WANG, Weiru , WEI, BinQing , ZHOU, Aihe , CARTWRIGHT, Matthew W. , GANCIA, Emanuela , JONES, Graham , LAINCHBURY, Michael , MADIN, Andrew , SEWARD, Eileen , FAVOR, David , FONG, Kin Chiu , HU, Yonghan , GOOD, Andrew , HU, Baihua , LU, Aijun
IPC分类号： C07D471/04 , C07D519/00 , A61K31/4375 , A61P35/00
摘要： Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibitng HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.

6. 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。

7. 发明申请

WO2018167147A1 AZAINDOLES AS INHIBITORS OF HPK1 审中-公开
公开(公告)号：WO2018167147A1
公开(公告)日：2018-09-20
申请号：PCT/EP2018/056390
申请日：2018-03-14
申请人： F. HOFFMANN-LA ROCHE AG , GENENTECH, INC.
发明人： HEFFRON, Timothy , MALHOTRA, Sushant , WEI, BinQing , CHAN, Bryan , GAZZARD, Lewis , GANCIA, Emanuela , LAINCHBURY, Michael , MADIN, Andrew , SEWARD, Eileen , HU, Yonghan
IPC分类号： C07D471/04 , A61P35/00 , A61K31/437 , A61K31/5377 , A61K31/496 , A61K31/506
摘要： Azaindole compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1- dependent disorders, methods for enhancing an immune response, and methods for preparing the azaindole compounds.

8. 发明申请

WO2010003133A2 CDK MODULATORS 审中-公开
标题翻译： CDK调制器
公开(公告)号：WO2010003133A2
公开(公告)日：2010-01-07
申请号：PCT/US2009/049637
申请日：2009-07-02
申请人： EXELIXIS INC. , BAHCECI, Suleyman , CHAN, Bryan , CHAN, Diva, Sze-ming , CHEN, Jeff , FORSYTH, Timothy, Patrick , FRANZINI, Maurizio , JAMMALAMADAKA, Vasu , JEONG, Joon, Won , JONES, Lisa, Renee , KELLEY, Ryan, Michael , KIM, Moon, Hwan , LEAHY, James, W. , MAC, Morrison, B. , NOGUCHI, Robin, Tammie , RAO, Pallavi , RIDGWAY, Brian, Hugh , XU, Wei , WANG, Yong
发明人： BAHCECI, Suleyman , CHAN, Bryan , CHAN, Diva, Sze-ming , CHEN, Jeff , FORSYTH, Timothy, Patrick , FRANZINI, Maurizio , JAMMALAMADAKA, Vasu , JEONG, Joon, Won , JONES, Lisa, Renee , KELLEY, Ryan, Michael , KIM, Moon, Hwan , LEAHY, James, W. , MAC, Morrison, B. , NOGUCHI, Robin, Tammie , RAO, Pallavi , RIDGWAY, Brian, Hugh , XU, Wei , WANG, Yong
IPC分类号： A61K31/437
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： A compound according to Formula I : or a pharmaceutically-acceptable salt thereof, wherein R1, R3, A, B and D are as defined in the specification; pharmaceutical compositions thereof, and methods of use thereof.
摘要翻译：根据式I的化合物或其药学上可接受的盐，其中R 1，R 3，A，B和D如说明书中所定义; 其药物组合物及其使用方法。

9. 发明申请

WO2010132272A2 DRIVING METHODS AND WAVEFORMS FOR ELECTROPHORETIC DISPLAYS 审中-公开
标题翻译：电动显示器的驱动方法和波形
公开(公告)号：WO2010132272A2
公开(公告)日：2010-11-18
申请号：PCT/US2010/033906
申请日：2010-05-06
申请人： SIPIX IMAGING, INC. , SPRAGUE, Robert , CHAN, Bryan , PHAM, Tin , LIN, Craig , PERI, Manasa
发明人： SPRAGUE, Robert , CHAN, Bryan , PHAM, Tin , LIN, Craig , PERI, Manasa
IPC分类号： G09G3/38 , G02F1/167
CPC分类号： G09G3/2003 , G09G3/344 , G09G3/3446 , G09G2300/0452 , G09G2310/061 , G09G2310/068 , G09G2320/0252
摘要： This application is directed to driving methods for electrophoretic displays. The driving methods and waveforms have the advantage that they provide a clean and smooth transition from one image to another image, without flashing or other undesired visual interruptions. The methods also provide faster image transitions. In an embodiment, a method drives a display device from a first image to a second image wherein images of a first color are displayed with a background of a second color, which method comprises driving pixels of the first color directly to the second color before driving pixels of the second color directly to the first color.
摘要翻译：本申请涉及电泳显示器的驱动方法。驱动方法和波形的优点在于，它们可以从一个图像到另一个图像提供干净平滑的过渡，而不会出现闪烁或其他不期望的视觉中断。这些方法也提供了更快的图像转换。在一个实施例中，一种方法将显示设备从第一图像驱动到第二图像，其中以第二颜色的背景显示第一颜色的图像，该方法包括在驾驶之前将第一颜色的像素直接驱动到第二颜色第二种颜色的像素直接到第一种颜色。

10. 发明申请

WO2012038743A1 PYRAZOLOPYRIDINES AS INHIBITORS OF THE KINASE LRRK2 审中-公开
标题翻译：作为激酶LRRK2的抑制剂的吡唑啉酮
公开(公告)号：WO2012038743A1
公开(公告)日：2012-03-29
申请号：PCT/GB2011/051773
申请日：2011-09-21
申请人： MEDICAL RESEARCH COUNCIL TECHNOLOGY , GENENTECH INC. , CHAN, Bryan , CHEN, Huifen , ESTRADA, Anthony , SHORE, Daniel , SWEENEY, Zachary , McIVER, Edward
发明人： CHAN, Bryan , CHEN, Huifen , ESTRADA, Anthony , SHORE, Daniel , SWEENEY, Zachary , McIVER, Edward
IPC分类号： C07D471/04 , A61K31/437 , A61P25/28 , A61P35/00
CPC分类号： C07D471/04
摘要： The present invention relates to compounds of formula I, or pharmaceutically acceptable salts or esters thereof, (Formula I) wherein R 1 is selected from: aryl; heteroaryl; -NHR 3 ; fused aryl-C 4_7 -heterocycloalkyl; -CONR 4 R 5 ; - NHCOR 6 ; -C 3-7- cycloalkyl,-NR 3 R 6 ; -OR 3 ; OH; NR 4 R 5 ; and alkyl optionally substituted with a substituent selected from R 11 and a group A; wherein said aryl, heteroaryl, fused aryl-C 4-7 -heterocycloalkyl and C 4-7 - heterocycloalkyi are each optionally substituted with one or more substituents selected from C 1-6 -alkyl, C 3-7 -cycloalkyl, heteroaryl, C 4-7 -heterocycloalkyl, aryl and a group A, and said C 1-6 -alkyl, C 3-7 -cycloalkyl, heteroaryl, C 4-7 -heterocycloalkyl, and aryl substituents are in turn each optionally substituted with one or more groups selected from R 11 and a group A; R 2 is selected from hydrogen, aryl, C 1-6 -alkyl, C 2- 6-alkenyl, C 3-7 -cycloalkyl, heteroaryl, heterocycloalkyi, fused aryl-C 4-7 -rheterocycloalkyl and halogen, wherein said C 1-6 -alkyl, C 2-6 -alkenyl, aryl, heteroaryl, fused aryl-C 4-7 -heterocycloalkyl and C 4-7 -heterocycloalkyl are each optionally substituted with one or more substituents selected from R 11 and A. Further aspects relate to pharmaceutical compositions and therapeutic uses of said compounds.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐或酯，（式I）其中R 1选自：芳基; 杂; -NHR 3; 稠合芳基-C 4-7 - 杂环烷基; -CONR4R5; - NHCOR6; -C3-7环烷基，-NR3R6; OR 3; 哦; NR4R5; 和任选被选自R 11和A A的取代基取代的烷基; 其中所述芳基，杂芳基，稠合芳基C 4-7 - 杂环烷基和C 4-7 - 杂环烷基各自任选被一个或多个选自C 1-6 - 烷基，C 3-7 - 环烷基，杂芳基，C 4-7 - 杂环烷基，芳基和A基团，所述C 1-6 - 烷基，C 3-7 - 环烷基，杂芳基，C 4-7 - 杂环烷基和芳基取代基又分别被一个或多个选自R 11和A ; R 2选自氢，芳基，C 1-6 - 烷基，C 2-6烯基，C 3-7 - 环烷基，杂芳基，杂环烷基，稠合芳基-C 4-7-杂环烷基和卤素，其中所述C 1-6 - 烷基，C 2 -6-烯基，芳基，杂芳基，稠合芳基C 4-7 - 杂环烷基和C 4-7 - 杂环烷基各自任选被一个或多个选自R 11和A的取代基取代。其它方面涉及药物组合物和所述化合物的治疗用途。

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