JP5252404B2 - ピラジン化合物、その使用及び調製方法 - Google Patents

ピラジン化合物、その使用及び調製方法 Download PDF

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JP5252404B2
JP5252404B2 JP2009524774A JP2009524774A JP5252404B2 JP 5252404 B2 JP5252404 B2 JP 5252404B2 JP 2009524774 A JP2009524774 A JP 2009524774A JP 2009524774 A JP2009524774 A JP 2009524774A JP 5252404 B2 JP5252404 B2 JP 5252404B2
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alkyl
compound
hydroxyl
substituted
alkoxy
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JP2010501003A5 (enExample
JP2010501003A (ja
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ティナ マリー モーウィック
アンソニー エス プロコポウィッツ
ワン マオ
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ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
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JP2009524774A 2006-08-16 2007-08-15 ピラジン化合物、その使用及び調製方法 Expired - Fee Related JP5252404B2 (ja)

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Application Number Priority Date Filing Date Title
US82254606P 2006-08-16 2006-08-16
US60/822,546 2006-08-16
PCT/US2007/075946 WO2008022164A2 (en) 2006-08-16 2007-08-15 Pyrazine compounds, their use and methods of preparation

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JP2010501003A JP2010501003A (ja) 2010-01-14
JP2010501003A5 JP2010501003A5 (enExample) 2010-09-30
JP5252404B2 true JP5252404B2 (ja) 2013-07-31

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US (1) US8318723B2 (enExample)
EP (1) EP2061762B1 (enExample)
JP (1) JP5252404B2 (enExample)
AT (1) ATE517868T1 (enExample)
CA (1) CA2660560A1 (enExample)
WO (1) WO2008022164A2 (enExample)

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI1966202T1 (sl) 2005-12-13 2012-01-31 Incyte Corp S heteroarilom substituirani pirolo (2,3-b)piridini in pirolo (2,3-b)pirimidini kot zaviralci janus kinaze
EP2173752B2 (en) 2007-06-13 2022-07-13 Incyte Holdings Corporation Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
SI2252597T1 (sl) 2008-02-01 2014-07-31 Akinion Pharmaceuticals Ab Derivati pirazina in njihova uporaba kot inhibitorji protein kinaze
EP2322528A4 (en) * 2008-06-19 2011-11-02 Univ Kanazawa Nat Univ Corp INTERMEDIATE PRODUCT FOR STEMONAMIDE SYNTHESIS AND PHARMACEUTICAL COMPOSITION FOR THE PREVENTION AND / OR TREATMENT OF CANCER
US8987251B2 (en) 2008-08-19 2015-03-24 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
TWI496779B (zh) * 2008-08-19 2015-08-21 Array Biopharma Inc 作為pim激酶抑制劑之三唑吡啶化合物
CL2009001884A1 (es) * 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
CN106967070A (zh) 2009-05-22 2017-07-21 因塞特控股公司 作为jak抑制剂的化合物
CA2762174C (en) 2009-05-22 2018-02-20 Incyte Corporation N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
EP3715347B1 (en) 2010-03-10 2021-12-22 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
NZ603686A (en) 2010-05-21 2014-11-28 Incyte Corp Topical formulation for a jak inhibitor
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
JP5917544B2 (ja) 2010-11-19 2016-05-18 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Jak阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン
WO2012120415A1 (en) 2011-03-04 2012-09-13 Novartis Ag Tetrasubstituted cyclohexyl compounds as kinase inhibitors
UY33930A (es) 2011-03-04 2012-10-31 Novartis Ag Inhibidores novedosos de quinasas
TWI577676B (zh) 2011-06-20 2017-04-11 英塞特控股公司 作為jak抑制劑之吖丁啶基苯基、吡啶基或吡基羧醯胺衍生物
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲jak抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
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UA120499C2 (uk) 2013-08-07 2019-12-26 Інсайт Корпорейшн Лікування захворювань із застосуванням лікарських форм з уповільненим вивільненням для інгібітора jak1
AR097431A1 (es) 2013-08-23 2016-03-16 Incyte Corp Compuestos de carboxamida de furo y tienopiridina útiles como inhibidores de quinasas pim
CN106573927B (zh) * 2014-03-18 2019-09-27 豪夫迈·罗氏有限公司 氧杂环庚烷-2-基-吡唑-4-基-杂环基-甲酰胺化合物和使用方法
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
US9822124B2 (en) 2014-07-14 2017-11-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
US9920032B2 (en) 2015-10-02 2018-03-20 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
US11542256B2 (en) 2017-09-03 2023-01-03 Angion Biomedica Corp. Vinylheterocycles as Rho-associated coiled-coil kinase (ROCK) inhibitors
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
MD3746429T2 (ro) 2018-01-30 2022-08-31 Incyte Corp Procedee pentru prepararea de (1-(3-fluoro-2-(trifluorometil)izonicotinil)piperidin-4-onă)
HUE067471T2 (hu) 2018-03-30 2024-10-28 Incyte Corp Gennyes verejtékmirigy-gyulladás kezelése jak inhibitorok alkalmazásával
WO2020210428A1 (en) * 2019-04-09 2020-10-15 Baylor College Of Medicine Novel inhibitors of flavivirus protease for prevention and treatment of zika, dengue and other flavivirus infections
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002060492A1 (en) * 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
GB0119865D0 (en) * 2001-08-14 2001-10-10 Cancer Res Campaign Tech DNA-PK inhibitors
US7015227B2 (en) * 2002-06-21 2006-03-21 Cgi Pharmaceuticals, Inc. Certain amino-substituted monocycles as kinase modulators
WO2005026129A1 (en) * 2003-09-15 2005-03-24 Gpc Biotech Ag Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
KR101206843B1 (ko) * 2003-12-03 2012-11-30 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 튜불린 저해제
US20080194574A1 (en) * 2003-12-16 2008-08-14 Axxima Pharmaceuticals Ag Pyrazine Derivatives As Effective Compounds Against Infectious Diseases
WO2006051311A1 (en) * 2004-11-12 2006-05-18 Galapagos Nv Nitrogen heteroaromatic compounds which bind to the active site of protein kinase enzymes
CA2626479A1 (en) * 2005-11-03 2007-05-18 Irm Llc Protein kinase inhibitors

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