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21. 发明专利

AU2018348161A1 Crystalline forms 未知
公开(公告)号：AU2018348161A1
公开(公告)日：2020-03-19
申请号：AU2018348161
申请日：2018-10-10
申请人： ARRAY BIOPHARMA INC
发明人： METCALF ANDREW T , FRY DAVID , MCFADDIN ELIZABETH A , KOLAKOWSKI GABRIELLE R , HAAS JULIA , TANG TONY P , JIANG YUTONG
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
摘要： Provided herein are compound of Formula I-IV and pharmaceutically acceptable salts thereof which exhibit rearranged during transfection (RET) kinase inhibition. In particular, provided herein are novel crystalline forms of 4-(6-(4-((6-methoxypyridin-3-yl)methyl)piperazin-1-yl)pyridin-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula I), 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula II), 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-(6-methoxynicotinoyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula III), 6-(2-hydroxy-2-methylpropoxy)-4-(6-(4-hydroxy-4-(pyridin-2-ylmethyl)piperidin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula IV), and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds, processes for making the compounds, and the use of the compounds in therapy. More particularly, the application relates to novel crystalline forms of Formula I-IV and pharmaceutically acceptable salts thereof useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

22. 发明专利

CL2019000942A1 Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret. 未知
公开(公告)号：CL2019000942A1
公开(公告)日：2019-11-15
申请号：CL2019000942
申请日：2019-04-08
申请人： ARRAY BIOPHARMA INC
发明人： ANDREWS STEVEN W , ARONOW SEAN , BLAKE JAMES F , BRANDHUBER BARBARA J , COOK ADAM , HAAS JULIA , JIANG YUTONG , KOLAKOWSKI GABRIELLE R , MCFADDIN ELIZABETH A , MCKENNEY MEGAN L , MCNULTY OREN T , MORENO DAVID A , TANG TONY P , REN LI , METCALF ANDREW T , COLLIER JAMES , RAMANN GINELLE A , WALLS SHANE M
IPC分类号： A61K31/437 , A61P35/00 , C07D471/04
摘要： COMPUESTOS DE PIRAZOLO[1,5-A]PIRIDINA SUSTITUIDOS COMO INHIBIDORES DE LA QUINASA RET

23. 发明专利

PE20191613A1 COMPUESTOS DE PIRAZOLO[1,5-A]PIRIDINA SUSTITUIDOS COMO INHIBIDORES DE LA QUINASA RET 未知
公开(公告)号：PE20191613A1
公开(公告)日：2019-11-05
申请号：PE2019000791
申请日：2017-10-10
申请人： ARRAY BIOPHARMA INC
发明人： ANDREWS STEVEN W , ARONOW SEAN , BLAKE JAMES F , BRANDHUBER BARBARA J , COLLIER JAMES , COOK ADAM , HAAS JULIA , JIANG YUTONG , KOLAKOWSKI GABRIELLE R , MCFADDIN ELIZABETH A , MCKENNEY MEGAN L , MCNULTY OREN T , METCALF ANDREW T , MORENO DAVID A , RAMANN GINELLE A , TANG TONY P , REN LI , WALLS SHANE M
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
摘要： Se refiere a compuestos de pirazolo[1,5-a]piridina sustituidos de formula I, donde X1, X2, X3 y X4 son independientemente CH, CCH3, CF o N; A es H, CN, CI, metilo, etilo o ciclopropilo; B es H, alquilo de C1-C6 opcionalmente sustituido con 1-3 fluoros, entre otros; D es un anillo heterociclico de 4-7 miembros monociclicos saturado que tiene un Nitrogeno; Ra es C1-C6 alquilo, hidroxi C1-C6 alquilo o C1-C6 alquil-; y Rb es un hidroxi o hetCicbCH2-. Tiene como compuestos preferidos: 1 -(5-(3-ciano-6-metoxipirazolo[1,5-a]piridin-4-il) piridin-2-il)-4-etil-N-isopropilpiperidin-4-carboxamida; (S)-(1-(5-(3-ciano-6-etoxipirazolo[1,5-a]piridin-4-il)piridin-2-il)piperidin-3-il)carbamato; entre otros. Estos compuestos son inhibidores de la quinasa RET y son utiles para el tratamiento de enfermedades proliferativas como diversos tipos de cancer. Ademas, se incluyen composiciones que contienen dichos compuestos.

25. 发明专利

UY37927A PROCESO PARA LA PREPARACIÓN DE 6-(2-HIDROXI-2-METILPROPOXI)-4-(6-(6-((6-METOXIPIRIDIN-3-IL)METIL)-3,6-DIAZABICICLO[3.1.1]HEPTAN-3-IL)PIRIDIN-3-IL)PIRAZOLO[1,5-A]PIRIDINA-3-CARBONITRILO 未知
公开(公告)号：UY37927A
公开(公告)日：2019-04-30
申请号：UY37927
申请日：2018-10-10
申请人： ARRAY BIOPHARMA INC , LOXO ONCOLOGY INC
发明人： METCALF ANDREW T , KOLAKOWSKI GABRIELLE R , EARY CHARLES TODD , SPENCER STACEY , CRANE ZACK , CHANDO KATELYN , ASSELIN SYLVIE , LIU WEIDONG , WELCH MIKE , COOK ADAM , MORENO DAVID A , TANG TONY P
IPC分类号： C07D471/08 , C07D401/14 , C07D471/04
摘要： En algunas formas de realización, en la presente se provee un proceso para preparar un compuesto de Fórmula I o una sal farmacéuticamente aceptable del mismo, como se divulga en la presente.

26. 发明专利

SG11201810171SA KRAS G12C INHIBITORS 未知
公开(公告)号：SG11201810171SA
公开(公告)日：2018-12-28
申请号：SG11201810171S
申请日：2017-05-17
申请人： MIRATI THERAPEUTICS INC , ARRAY BIOPHARMA INC
发明人： FISCHER JOHN , FELL JAY , BLAKE JAMES , HINKLIN RONALD , MEJIA MACEDONIO , HICKEN ERIK , CHICARELLI MARK , GAUDINO JOHN , VIGERS GUY , BURGESS LAURENCE , MARX MATTHEW , CHRISTENSEN JAMES , LEE MATTHEW , SAVECHENKOV PAVEL , ZECCA HENRY , TANG TONY P
IPC分类号： A61K31/445 , C07D231/56 , C07D295/185
摘要： The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

27. 发明专利

AU2017266911A1 KRas G12C inhibitors 未知
公开(公告)号：AU2017266911A1
公开(公告)日：2018-12-06
申请号：AU2017266911
申请日：2017-05-17
申请人： ARRAY BIOPHARMA INC , MIRATI THERAPEUTICS INC
发明人： FISCHER JOHN P , FELL JAY BRADFORD , BLAKE JAMES F , HINKLIN RONALD JAY , MEJIA MACEDONIO J , HICKEN ERIK JAMES , CHICARELLI MARK JOSEPH , GAUDINO JOHN J , VIGERS GUY P A , BURGESS LAURENCE E , MARX MATTHEW ARNOLD , CHRISTENSEN JAMES GAIL , LEE MATTHEW RANDOLF , SAVECHENKOV PAVEL , ZECCA HENRY J , TANG TONY P
IPC分类号： C07D231/56 , A61K31/445 , C07D295/185
摘要： The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

28. 发明专利

CO2017006674A2 Pirazolo[1,5-a]pirazinas 4,6-sustituidas como inhibidores de janus cinasas. 未知
公开(公告)号：CO2017006674A2
公开(公告)日：2017-10-20
申请号：CO2017006674
申请日：2017-06-30
申请人： CELGENE CORP , ARRAY BIOPHARMA INC
发明人： BOYS MARK LAURENCE , BURGESS LAURENCE E , HICKEN ERIK JAMES , KRASER CHRISTOPHER F , LAIRD ELLEN , ROBINSON JOHN E , GAUDINO JOHN , ALLEN SHELLEY , CHICARELLI MARK J , RIEGER ROBERT ANDREW , PHENEGER JED , FELL JAY BRADFORD , FISCHER JOHN P , HINKLIN RONALD JAY , TANG TONY P , SATOH YOSHITAKA , LEFTHERIS KATERINA , RAHEJA RAJ K , BENNETT BRYDON L
IPC分类号： C07D487/04 , A61K31/4985 , A61P29/00 , A61P37/00
摘要： PIRAZOLO[1,5-A]PIRAZINAS 4,6-SUSTITUIDAS COMO INHIBIDORES DE JANUS CINASAS RESUMEN – OBJETO Y FINALIDAD DE LA INVENCIÓN Compuestos de Fórmula I: y estereoisómeros y sales solvatos farmacéuticamente aceptables de estos en los que R1, R2, R3 y R4 tienen los significados dados en la memoria descriptiva, son inhibidores de una o más JAK cinasas y son útiles en el tratamiento de enfermedades y trastornos relacionados con la JAK cinasa, tales como enfermedades autoinmunitarias, rechazo del trasplante de órganos¬, tejidos y células, así como también neoplasias y trastornos hematológicos y sus comorbilidades. Sector: Ciencias médicas y farmacéuticas

29. 发明专利

HK1223877A1 絲氨酸/蘇氨酸激酶抑制劑未知
公开(公告)号：HK1223877A1
公开(公告)日：2017-08-11
申请号：HK16111117
申请日：2016-09-22
申请人： GENENTECH INC , ARRAY BIOPHARMA INC
发明人： BLAKE JAMES F , COOK ADAM , GUNAWARDANA INDRANI W , HUNT KEVIN W , LYON MICHAEL , METCALF ANDREW T , MOHR PETER J , MORENO DAVID A , NEWHOUSE BRAD , REN LI , TANG TONY P , THOMAS ALLEN A , SCHWARZ JACOB , SCHMIDT JANE , GAZZARD LEWIS , CHEN HUIFEN
IPC分类号： A61K20060101 , A61P20060101 , C07D20060101

30. 发明专利

SG11201704542SA 4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS 未知
公开(公告)号：SG11201704542SA
公开(公告)日：2017-07-28
申请号：SG11201704542S
申请日：2015-12-04
申请人： ARRAY BIOPHARMA INC , CELGENE CORP
发明人： ALLEN SHELLEY , BOYS MARK LAURENCE , CHICARELLI MARK J , FELL JAY BRADFORD , FISCHER JOHN P , GAUDINO JOHN , HICKEN ERIK JAMES , HINKLIN RONALD JAY , KRASER CHRISTOPHER F , LAIRD ELLEN , ROBINSON JOHN E , TANG TONY P , BURGESS LAURENCE E , RIEGER ROBERT ANDREW , PHENEGER JED , SATOH YOSHITAKA , LEFTHERIS KATERINA , RAHEJA RAJ K , BENNETT BRYDON L
IPC分类号： A61K31/4985 , C07D487/04 , A61P29/00 , A61P37/00
摘要： Compounds of Formula I:and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R 1 , R 2 , R 3 and R 4 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of JAK kinase-associated diseases and disorders, such as autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.

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