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1. 发明申请

WO2015187451A9 RADIOLABELLED DERIVATIVES OF A 2-AMINO-6-FLUORO-N-[5-FLUORO-PYRIDIN-3-YL]- PYRAZOLO[1,5-A]PYRIMIDIN-3-CARBOXAMIDE COMPOUND USEFUL AS ATR KINASE INHIBITOR, THE PREPARATION OF SAID COMPOUND AND DIFFERENT SOLID FORMS THEREOF 审中-公开
标题翻译：用于ATR激酶抑制剂的2-氨基-6-氟-N- [5-氟-2-吡啶-3-基] - 吡唑并[1,5-A]嘧啶-3-羰氧基化合物的放射性衍生物，制备化合物化合物和不同的固体形式
公开(公告)号：WO2015187451A9
公开(公告)日：2016-05-19
申请号：PCT/US2015032879
申请日：2015-05-28
申请人： VERTEX PHARMA
发明人： AHMAD NADIA , CHARRIER JEAN-DAMIEN , DAVIS CHRIS , ETXEBARRIA I JARDI GORKA , FRAYSSE DAMIEN , KNEGTEL RONALD , PANESAR MANINDER , PIERARD FRANCOISE , PINDER JOANNE , STORCK PIERRE-HENRI , STUDLEY JOHN
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention. The compounds of this invention have formula (I-l) or (I-A); wherein the variables are as defined herein.
摘要翻译：本发明涉及可用作ATR蛋白激酶抑制剂的化合物。本发明涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 和本发明化合物的固体形式。本发明化合物具有式（I-1）或（I-A）; 其中变量如本文所定义。

2. 发明申请

WO2014089379A1 COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE 审中-公开
标题翻译：化合物作为ATR激酶的抑制剂有用
公开(公告)号：WO2014089379A1
公开(公告)日：2014-06-12
申请号：PCT/US2013073457
申请日：2013-12-06
申请人： VERTEX PHARMA
发明人： AHMAD NADIA , BOYALL DEAN , CHARRIER JEAN-DAMIEN , DAVIS CHRIS , DAVIS REBECCA , DURRANT STEVEN , ETXEBARRIA I JARDI GORKA , FRAYSSE DAMIEN , JIMENEZ JUAN-MIGUEL , KAY DAVID , KNEGTEL RONALD , MIDDLETON DONALD , ODONNELL MICHAEL , PANESAR MANINDER , PIERARD FRANCOISE , PINDER JOANNE , SHAW DAVID , STORCK PIERRE-HENRI , STUDLEY JOHN , TWIN HEATHER
IPC分类号： C07D487/04 , A61K31/495 , A61P35/00
CPC分类号： C07D487/04 , C07D453/02 , C07D471/08 , C07D487/08 , C07D491/107 , C07D498/04 , C07D498/10
摘要： The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula (I) or a pharmaceutically acceptable salt, wherein the variables are as devined herein. Moreover, The compounds of this invention have formula (I-A) or a pharmaceutically acceptable salt, wherein the variables are as defined herein.
摘要翻译：本发明涉及可用作ATR蛋白激酶抑制剂的化合物。本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 以及在体外应用中使用化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。本发明的化合物具有式（I）或其药学上可接受的盐，其中变量如本文所述。此外，本发明的化合物具有式（I-A）或其药学上可接受的盐，其中变量如本文所定义。

3. 发明专利

ECSP22052564A TETRAHIDROFURANOS SUSTITUIDOS COMO MODULADORES DE CANALES DE SODIO 未知
公开(公告)号：ECSP22052564A
公开(公告)日：2022-08-31
申请号：ECDI202252564
申请日：2022-07-05
申请人： VERTEX PHARMA
发明人： CHUDYK EWA , DURRANT STEVEN , WRAY CHRISTOPHER , CARVALHO MEIRELES LIDIO , KNEGTEL RONALD , AHMAD NADIA , PULLIN ROBERT , NEUBERT TIMOTHY , HADIDA RUAH SARA S , SCHMIDT YVONNE , BECK ELIZABETH , VIRANI ANISA , PONTILLO JOSEPH , STAMOS DEAN , SKERRATT SARAH , PINDER JOANNE , SHAW DAVID , ETXEBARRIA JARDI GORKA , THOMSON STEPHEN , HURLEY DENNIS , GALAN BHAIRAVI
IPC分类号： C07D405/12
摘要： Se proporcionan compuestos y sus sales farmac?uticamente aceptables, de utilidad como inhibidores de canales de sodio. Tambi?n se proporcionan composiciones farmac?uticas que comprenden los compuestos o sales farmac?uticamente aceptables y m?todos de uso de los compuestos, sales farmac?uticamente aceptables y composiciones farmac?uticas en el tratamiento de diversos trastornos, incluyendo el dolor.

4. 发明专利

AU2020397059A1 Substituted tetrahydrofurans as modulators of sodium channels 未知
公开(公告)号：AU2020397059A1
公开(公告)日：2022-07-21
申请号：AU2020397059
申请日：2020-12-04
申请人： VERTEX PHARMA
发明人： DURRANT STEVEN JOHN , AHMAD NADIA , BECK ELIZABETH MARY , CARVALHO MEIRELES LIDIO , CHUDYK EWA IWONA , ETXEBARRIA JARDI GORKA , GALAN BHAIRAVI , HADIDA RUAH SARA S , HURLEY DENNIS JAMES , KNEGTEL RONALD MARCELLUS , NEUBERT TIMOTHY DONALD , PINDER JOANNE LOUISE , PONTILLO JOSEPH , PULLIN ROBERT , SCHMIDT YVONNE , SHAW DAVID MATTHEW , SKERRATT SARAH , STAMOS DEAN , THOMSON STEPHEN ANDREW , VIRANI ANISA NIZARALI , WRAY CHRISTOPHER
IPC分类号： C07D405/12 , A61K31/443 , A61P29/00 , C07D405/14
摘要： Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.

5. 发明专利

TN2020000001A1 CARBOXAMIDES AS MODULATORS OF SODIUM CHANNELS 未知
公开(公告)号：TN2020000001A1
公开(公告)日：2021-10-04
申请号：TN2020000001
申请日：2018-07-11
申请人： VERTEX PHARMA
发明人： SCHMIDT YVONNE , PATEL URVI , MEIRELES LIDIO MARX CARVALHO , ANDERSON COREY , CAMP JOANNE , ASGIAN LULIANA , ARUMUGAM VIJAYALAKSMI , HADIDA RUAH SARA , AHMAD NADIA , FANNING LEV TYLER , THOMSON STEPHEN , HURLEY DENNIS , SHAW DAVID
IPC分类号： C07D213/81 , A61K31/165 , A61P29/02 , C07C237/42 , C07D213/82
摘要： Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.

7. 发明专利

ECSP20003147A CARBOXAMIDAS COMO MODULADORES DE LOS CANALES DE SODIO 未知
公开(公告)号：ECSP20003147A
公开(公告)日：2020-02-28
申请号：ECDI202003147
申请日：2020-01-15
申请人： VERTEX PHARMA
发明人： CAMP JOANNE LOUISE , CARVALHO MEIRELES LIDIO MARX , URVI PATEL , SCHMIDT YVONNE , FANNING LEV TYLER , ANDERSON COREY , ARUMUGAM VIJAYALAKSMI , AHMAD NADIA , ASGIAN IULIANA LUCI , THOMSON STEPHEN , HADIDA RUAH SARA , SHAW DAVID , HURLEY DENNIS
IPC分类号： A61K31/165 , A61P29/02 , C07C237/42 , C07D213/81 , C07D213/82
摘要： Se proporcionan compuestos y sus sales farmacéuticamente aceptables, de utilidad como inhibidores de canales de sodio. Además, se proporcionan composiciones farmacéuticas que comprenden los compuestos o sales farmacéuticamente aceptables y métodos de uso de los compuestos, sales farmacéuticamente aceptables y composiciones farmacéuticas en el tratamiento de varios trastornos, incluyendo dolor.

8. 发明专利

CO2020000145A2 Carboxamidas como moduladores de los canales de sodio 未知
公开(公告)号：CO2020000145A2
公开(公告)日：2020-01-17
申请号：CO2020000145
申请日：2020-01-08
申请人： VERTEX PHARMA
发明人： HADIDA RUAH SARA SABINA , ANDERSON COREY , AHMAD NADIA , ARUMUGAM VIJAYALAKSMI , ASGIAN IULIANA LUCI , CAMP JOANNE LOUISE , FANNING LEV TYLER DEWEY , HURLEY DENNIS , SCHMIDT YVONNE , SHAW DAVID , PATEL URVI , THOMSON STEPHEN ANDREW , MEIRELES LIDIO MARX CARVALHO
IPC分类号： A61K31/165 , A61P29/02 , C07C237/42 , C07D213/81 , C07D213/82
摘要： RESUMEN Se proporcionan compuestos y sus sales farmacéuticamente aceptables, de utilidad como inhibidores de canales de sodio. Además, se proporcionan composiciones farmacéuticas que comprenden los compuestos o sales farmacéuticamente aceptables y métodos de uso de los compuestos, sales farmacéuticamente aceptables y composiciones farmacéuticas en el tratamiento de varios trastornos, incluyendo dolor.

9. 发明专利

NZ731337A Compounds useful as inhibitors of atr kinase 未知
公开(公告)号：NZ731337A
公开(公告)日：2019-02-22
申请号：NZ73133713
申请日：2013-12-06
申请人： VERTEX PHARMA
发明人： AHMAD NADIA , BOYALL DEAN , CHARRIER JEAN-DAMIEN , DAVIS CHRIS , DAVIS REBECCA , DURRANT STEVEN , ETXEBARRIA I JARDI GORKA , FRAYSSE DAMIEN , JIMENEZ JUAN-MIGUEL , KAY DAVID , KNEGTEL RONALD , MIDDLETON DONALD , ODONNELL MICHAEL , PANESAR MANINDER , PIERARD FRANCOISE , PINDER JOANNE , SHAW DAVID , STORCK PIERRE-HENRI , STUDLEY JOHN , TWIN HEATHER
IPC分类号： C07D487/04 , A61K31/4162 , A61K31/4439 , A61K31/444 , A61K31/495 , A61K31/519 , A61P35/00 , C07D213/75
摘要： Disclosed are 2-amino-6-fluoro-N-(pyridin-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide derivatives and analogues useful as inhibitors of ATR kinase as represented by the general formula (I); or a pharmaceutically acceptable salt thereof, wherein: R1 is–C(J1)2CN or halo; R9 is H; each J1 is independently H, methyl or ethyl; or two occurrences of J1, together with the carbon atom to which they are attached, form a 3-4 membered optionally substituted carbocyclic ring; R2 is H; halo; -CN; NH2; or a methyl or ethyl group optionally substituted with fluoro; or a C1-3aliphatic chain wherein up to two methylene units of the aliphatic chain are optionally replaced with -O-, -NR-, -C(O)-, or –S(O)n; R3 is H; halo; alkyl optionally substituted with 1-3 occurrences of halo; cycloalkyl; heterocyclyl; -CN; or an aliphatic chain wherein up to two methylene units of the aliphatic chain are optionally replaced with -O-, -NR-, -C(O)-, or –S(O)n; R4 is Q1 or an aliphatic chain wherein up to four methylene units of the aliphatic chain are optionally replaced with -O-, -NR-, -C(O)-, or -S(O)n-; R4 is optionally substituted with 0-5 occurrences of JQ; or R3 and R4, taken together with the atoms to which they are bound, form a 5-6 membered aromatic or non-aromatic ring having 0-2 heteroatoms selected from oxygen, nitrogen and sulfur; the ring formed by R3 and R4 is optionally substituted with 0-3 occurrences of JZ; provided that the compound is not 2-amino-6-fluoro-N-[5-fluoro-4-[4-[4-(oxetan-3-yl)piperazine-1-carbonyl]-1-piperidyl]-3-pyridyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide. Also disclosed are the compounds selected from 2-amino-6-fluoro-N-(5-fluoro-4-(4-(4-(3-methyloxetan-3-yl)piperazine-1-carbonyl)piperidin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide; 4-(1-(3-(2-amino-6-fluoropyrazolo[1,5-a]pyrimidine-3-carboxamido)-5-fluoropyridin-4-yl)piperidine-4-carbonyl)-1-methylpiperazine 1-oxide; 2-amino-6-fluoro-N-(5-fluoro-4-(4-(4-(1-methylazetidin-3-yl)piperazine-1-carbonyl)piperidin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide; and 2-amino-6-fluoro-N-(5-fluoro-4-(1-methyl-1H-imidazol-5-yl)pyridin-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide. There is also disclosed a pharmaceutical composition having properties of inhibitor of ATR protein kinase for treating cancer comprising an effective amount of a compound as defined above and a pharmaceutically acceptable carrier.

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