JP5925809B2 - 三環系ピロロ誘導体、その調製方法およびそのキナーゼ阻害剤としての使用 - Google Patents

三環系ピロロ誘導体、その調製方法およびそのキナーゼ阻害剤としての使用 Download PDF

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JP5925809B2
JP5925809B2 JP2013550833A JP2013550833A JP5925809B2 JP 5925809 B2 JP5925809 B2 JP 5925809B2 JP 2013550833 A JP2013550833 A JP 2013550833A JP 2013550833 A JP2013550833 A JP 2013550833A JP 5925809 B2 JP5925809 B2 JP 5925809B2
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formula
compound
methyl
pyrrolo
quinazoline
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JP2014503567A (ja
JP2014503567A5 (cg-RX-API-DMAC10.html
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カルダレツリ,マリーナ
アンジヨリニ,マウロ
ベリア,イタロ
ブラスカ,マリア・ガブリエツラ
カスシエツリ,フランチエスコ
ダレツシオ,ロベルト
ロンバルデイ・ボルジア,アンドレア
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ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ
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JP2013550833A 2011-01-26 2012-01-19 三環系ピロロ誘導体、その調製方法およびそのキナーゼ阻害剤としての使用 Active JP5925809B2 (ja)

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EP11152190.2 2011-01-26
EP11152190 2011-01-26
PCT/EP2012/050773 WO2012101032A1 (en) 2011-01-26 2012-01-19 Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors

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JP2014503567A5 JP2014503567A5 (cg-RX-API-DMAC10.html) 2015-03-05
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JP2015203440A Active JP6118383B2 (ja) 2011-01-26 2015-10-15 三環系ピロロ誘導体、その調製方法およびそのキナーゼ阻害剤としての使用

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US (2) US8975267B2 (cg-RX-API-DMAC10.html)
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JP (2) JP5925809B2 (cg-RX-API-DMAC10.html)
CN (1) CN103339134B (cg-RX-API-DMAC10.html)
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Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
WO2012080990A1 (en) * 2010-12-17 2012-06-21 Nerviano Medical Sciences S.R.L. Substituted pyrazolo-quinazoline derivatives as kinase inhibitors
RU2591191C2 (ru) 2011-01-26 2016-07-10 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Трициклические пирроло производные, способ их получения и их применение в качестве ингибиторов киназы
GB201216018D0 (en) 2012-09-07 2012-10-24 Cancer Rec Tech Ltd Pharmacologically active compounds
GB201216017D0 (en) 2012-09-07 2012-10-24 Cancer Rec Tech Ltd Inhibitor compounds
ES2649156T3 (es) 2013-01-14 2018-01-10 Incyte Holdings Corporation Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim
TW201932456A (zh) 2013-01-15 2019-08-16 美商英塞特控股公司 適用作pim激酶抑制劑之噻唑甲醯胺及吡啶甲醯胺化合物
MX2016002367A (es) 2013-08-23 2016-10-28 Incyte Corp Compuestos de carboxamida de furo y tienopiridina utiles como inhibidores de cinasas pim.
GB201403536D0 (en) * 2014-02-28 2014-04-16 Cancer Rec Tech Ltd Inhibitor compounds
EP3125920B1 (en) 2014-04-04 2020-12-23 Del Mar Pharmaceuticals Dianhydrogalactitol, diacetyldianhydrogalactitol or dibromodulcitol to treat non-small-cell carcinoma of the lung and ovarian cancer
MX368767B (es) * 2014-04-07 2019-10-15 Netherlands Translational Res Center B V (5,6-dihidro)pirimido[4,5-e]indolizinas.
WO2016010897A1 (en) 2014-07-14 2016-01-21 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
EP3283642B1 (en) 2015-04-17 2023-10-11 Netherlands Translational Research Center Holding B.V. Prognostic biomarkers for ttk inhibitor chemotherapy
ITRM20150212A1 (it) * 2015-05-15 2016-11-15 Univ Degli Studi Di Palermo 4,5,6,9-tetraidropirrolo[2',3':3,4] cicloepta[1,2-d] isossazoli, procedimento per la loro produzione e loro uso come antitumorali
US9540347B2 (en) 2015-05-29 2017-01-10 Incyte Corporation Pyridineamine compounds useful as Pim kinase inhibitors
WO2017011776A1 (en) 2015-07-16 2017-01-19 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
TWI734699B (zh) 2015-09-09 2021-08-01 美商英塞特公司 Pim激酶抑制劑之鹽
CN105130980B (zh) * 2015-09-09 2018-05-22 沈阳药科大学 N-3-苯并咪唑噻唑胺类衍生物及其制备方法与应用
US9920032B2 (en) 2015-10-02 2018-03-20 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
EP3368039A1 (en) 2015-10-26 2018-09-05 The Regents of The University of Colorado, A Body Corporate Point mutations in trk inhibitor-resistant cancer and methods relating to the same
HUE068971T2 (hu) 2016-04-04 2025-02-28 Loxo Oncology Inc (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-A]pirimidin-3-il) -3-hidroxipirrolidin-1-karboxamid folyékony készítményei
LT3439663T (lt) 2016-04-04 2024-10-10 Loxo Oncology, Inc. Vaikų vėžio gydymo būdai
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
PT3800189T (pt) 2016-05-18 2023-07-27 Array Biopharma Inc Preparação de (s)-n-(5-((r)-2-(2,5- difluoropenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3- il)-3-hidroxipirrolidina-1-carboxamida
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
CN110267960B (zh) 2017-01-18 2022-04-26 阿雷生物药品公司 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
CN114213421A (zh) 2017-04-01 2022-03-22 晟科药业(江苏)有限公司 1h-咪唑[4,5-h]喹唑啉类化合物作为蛋白激酶抑制剂
GB201709840D0 (en) 2017-06-20 2017-08-02 Inst Of Cancer Research: Royal Cancer Hospital Methods and medical uses
TWI876442B (zh) 2017-10-10 2025-03-11 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
US10596161B2 (en) 2017-12-08 2020-03-24 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
US11603374B2 (en) 2018-01-18 2023-03-14 Array Biopharma Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
EP3740490A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors
CA3087972C (en) 2018-01-18 2023-01-10 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
WO2020028258A1 (en) 2018-07-31 2020-02-06 Loxo Oncology, Inc. Spray-dried dispersions and formulations of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoro propan-2-yl)-1h-pyrazole-4-carboxamide
CN112996794A (zh) 2018-09-10 2021-06-18 阿雷生物药品公司 作为ret激酶抑制剂的稠合杂环化合物
US12180207B2 (en) 2018-12-19 2024-12-31 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of FGFR tyrosine kinases
EP3898615A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
KR102866207B1 (ko) * 2019-08-02 2025-09-29 청두 사이노젠 바이오-파마슈티컬 테크놀로지 코., 엘티디. 단백질 키나제 억제제로 작용하는 1h-[1, 2, 3]트리아졸로[4, 5-h] 퀴나졸린 화합물
EP4069369A4 (en) 2019-12-06 2024-02-14 Schrödinger, Inc. CYCLIC COMPOUNDS AND METHODS OF USE THEREOF
US20240018157A1 (en) 2019-12-27 2024-01-18 Schrödinger, Inc. Cyclic compounds and methods of using same
JP2023541047A (ja) 2020-09-10 2023-09-27 シュレーディンガー, インコーポレイテッド がんの治療のための複素環式ペリ縮環cdc7キナーゼ阻害剤
CN114685520B (zh) * 2020-12-25 2024-08-30 武汉誉祥医药科技有限公司 三并环化合物及其药物组合物和应用
EP4284804A1 (en) 2021-01-26 2023-12-06 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders
TW202300150A (zh) 2021-03-18 2023-01-01 美商薛定諤公司 環狀化合物及其使用方法
WO2023113478A1 (en) * 2021-12-15 2023-06-22 Sillajen, Inc. Methods of treating neoplastic diseases
US20250049926A1 (en) * 2021-12-15 2025-02-13 Sillajen, Inc. Pharmaceutical compositions comprising modified betacyclodextrins
WO2025059027A1 (en) 2023-09-11 2025-03-20 Schrödinger, Inc. Cyclopenta[e]pyrazolo[1,5-a]pyrimidine derivatives as malt1 inhibitors

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL115833A (en) 1994-11-25 1998-10-27 Zeneca Ltd 6,6-Dihalo-3,3-dimethyl-5-hydroxy-7,7,7-trifluoroheptanoic acids and their alkyl esters useful as intermediates for insecticides and their preparation
MY125533A (en) * 1999-12-06 2006-08-30 Bristol Myers Squibb Co Heterocyclic dihydropyrimidine compounds
MXPA04008130A (es) 2002-02-19 2004-11-26 Pharmacia Corp Derivados triciclicos de pirazol para el tratamiento de la inflamacion.
ME00142B (me) * 2003-05-22 2010-10-10 Nerviano Medical Sciences Srl Derivati pirazolo-hinazolina, postupci za njihovo dobijanje i njihova upotreba kao inhibitora kinaze
CN1897950A (zh) 2003-10-14 2007-01-17 惠氏公司 稠合芳基和杂芳基衍生物及其使用方法
WO2008065054A1 (en) * 2006-11-28 2008-06-05 Nerviano Medical Sciences S.R.L. Tricyclic indoles and (4,5-dihydro) indoles
JP5542445B2 (ja) 2006-12-04 2014-07-09 江▲蘇▼先声▲薬▼物研究有限公司 3−ピロロシクロへキシリデン−2−ジヒドロインドリノン誘導体およびその用途
BRPI0720588B8 (pt) * 2006-12-21 2021-05-25 Nerviano Medical Sciences Srl derivados de pirazol-quinazolina substituídos, processo para sua preparação e seu uso como inibidores da quinase
AR067535A1 (es) * 2007-07-16 2009-10-14 Novartis Ag Derivados de lactama tetraciclicos
CA2711644A1 (en) 2008-01-07 2009-07-16 Synta Pharmaceuticals Corp. Compounds for inflammation and immune-related uses
US8546410B2 (en) * 2008-05-05 2013-10-01 Abbvie Inc. Heteroaryl-fused macrocyclic pyrimidine derivatives
JP5542133B2 (ja) * 2008-06-26 2014-07-09 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ ピラゾロ−キナゾリン
CN102105151B (zh) * 2008-07-29 2013-12-18 内尔维阿诺医学科学有限公司 Cdk抑制剂在治疗神经胶质瘤中的应用
CN102105152B (zh) * 2008-07-29 2012-10-17 内尔维阿诺医学科学有限公司 包含cdks抑制剂和抗肿瘤剂的治疗组合
CN102223885B (zh) * 2008-11-24 2013-04-03 内尔维阿诺医学科学有限公司 用于治疗间皮瘤的cdk抑制剂
EP2408776B1 (en) * 2009-03-20 2014-01-08 Nerviano Medical Sciences S.r.l. Use of a kinase inhibitor for the treatment of thymoma
US8586598B2 (en) * 2009-04-29 2013-11-19 Nerviano Medical Sciences S.R.L. CDK inhibitor salts
AR076784A1 (es) * 2009-05-26 2011-07-06 Nerviano Medical Sciences Srl Combinacion terapeutica que comprende un inhibidor de plk1 y un agente antineoplasico
US8648078B2 (en) * 2009-07-29 2014-02-11 Nerviano Medical Sciences S.R.L. PLK inhibitor salts
ES2539972T3 (es) * 2010-07-30 2015-07-07 Nerviano Medical Sciences S.R.L. Isoxazolo-quinazolinas como moduladores de la actividad de proteina cinasa
WO2012080990A1 (en) * 2010-12-17 2012-06-21 Nerviano Medical Sciences S.R.L. Substituted pyrazolo-quinazoline derivatives as kinase inhibitors
RU2591191C2 (ru) 2011-01-26 2016-07-10 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Трициклические пирроло производные, способ их получения и их применение в качестве ингибиторов киназы

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BR112013018515A2 (pt) 2016-10-18
EP2668190B1 (en) 2016-08-17
US20150141408A1 (en) 2015-05-21
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US20130296305A1 (en) 2013-11-07
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