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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JP2014503567A5 (OSRAM
JP2014503567A (ja
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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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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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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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Application Number Priority Date Filing Date Title
EP11152190 2011-01-26
EP11152190.2 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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JP2015203440A Division 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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JP2014503567A JP2014503567A (ja) 2014-02-13
JP2014503567A5 JP2014503567A5 (OSRAM) 2015-03-05
JP5925809B2 true JP5925809B2 (ja) 2016-05-25

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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 (OSRAM)
EP (1) EP2668190B1 (OSRAM)
JP (2) JP5925809B2 (OSRAM)
CN (1) CN103339134B (OSRAM)
BR (1) BR112013018515B1 (OSRAM)
ES (1) ES2602791T3 (OSRAM)
RU (1) RU2591191C2 (OSRAM)
WO (1) WO2012101032A1 (OSRAM)

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
CA2812223C (en) * 2010-12-17 2019-03-12 Nerviano Medical Sciences S.R.L. Substituted pyrazolo-quinazoline derivatives as kinase inhibitors
EP2668190B1 (en) 2011-01-26 2016-08-17 Nerviano Medical Sciences S.r.l. Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors
GB201216017D0 (en) * 2012-09-07 2012-10-24 Cancer Rec Tech Ltd Inhibitor compounds
GB201216018D0 (en) * 2012-09-07 2012-10-24 Cancer Rec Tech Ltd Pharmacologically active compounds
JP6437452B2 (ja) 2013-01-14 2018-12-12 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｐｉｍキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物
LT2945939T (lt) 2013-01-15 2020-07-27 Incyte Holdings Corporation Triazolkarboksamidai ir piridinkarboksamido junginiai, naudotini kaip pim kinazės inhibitoriai
EP3036238A1 (en) 2013-08-23 2016-06-29 Incyte Corporation Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors
GB201403536D0 (en) * 2014-02-28 2014-04-16 Cancer Rec Tech Ltd Inhibitor compounds
WO2015154064A2 (en) 2014-04-04 2015-10-08 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
CA2944610C (en) 2014-04-07 2024-01-09 Netherlands Translational Research Center B.V. (5,6-dihydro)pyrimido[4,5-e]indolizines
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
CA2981844A1 (en) 2015-04-17 2016-10-20 Netherlands Translational Research Center 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
DK3322706T3 (da) 2015-07-16 2021-02-01 Array Biopharma Inc Substituerede pyrazolo[1,5-a]pyridin-forbindelser som ret-kinaseinhibitorer
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
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
WO2017059251A1 (en) 2015-10-02 2017-04-06 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
JP2018534296A (ja) 2015-10-26 2018-11-22 ロクソ オンコロジー， インコーポレイテッドＬｏｘｏ Ｏｎｃｏｌｏｇｙ， Ｉｎｃ． Ｔｒｋ阻害薬耐性がんにおける点変異およびそれに関連する方法
MX386416B (es) 2016-04-04 2025-03-18 Loxo Oncology Inc Formulaciones liquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida.
RS65988B1 (sr) 2016-04-04 2024-10-31 Loxo Oncology Inc Postupak lečenja pedijatrijskih karcinoma
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
HUE063877T2 (hu) 2016-05-18 2024-02-28 Loxo Oncology Inc (S)-N-(5-((R)-2-(2,5-dlfluorofenil)pirolidin-1-il)plrazolo[1,5-A]pirimidin-3-il) -3-hidroxipirolidin-1-karboxamid elõállítása
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
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
CA3049136C (en) 2017-01-18 2022-06-14 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
KR102444482B1 (ko) * 2017-04-01 2022-09-16 셍커 파마슈티컬스 (지앙수) 엘티디. 단백질 인산화효소 억제제로서의 1h-이미다조[4,5-h]퀴나졸린 화합물
GB201709840D0 (en) 2017-06-20 2017-08-02 Inst Of Cancer Research: Royal Cancer Hospital Methods and medical uses
TWI812649B (zh) 2017-10-10 2023-08-21 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
TW201924683A (zh) 2017-12-08 2019-07-01 美商英塞特公司 用於治療骨髓增生性贅瘤的低劑量組合療法
CA3087578C (en) 2018-01-18 2023-08-08 Array Biopharma Inc. Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors
CA3087354C (en) 2018-01-18 2023-01-03 Array Biopharma Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
WO2019143994A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
KR102545594B1 (ko) 2018-07-31 2023-06-21 록쏘 온콜로지, 인코포레이티드 (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의 분무-건조된 분산물 및 제제
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
JP2022515197A (ja) 2018-12-19 2022-02-17 アレイ バイオファーマ インコーポレイテッド がんを治療するためのｆｇｆｒ阻害剤としての７－（（３，５－ジメトキシフェニル）アミノ）キノキサリン誘導体
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
CN114174301B (zh) * 2019-08-02 2024-03-15 成都赛璟生物医药科技有限公司 1h-[1,2,3]三唑并[4,5-h]喹唑啉类化合物作为蛋白激酶抑制剂
WO2021113492A1 (en) 2019-12-06 2021-06-10 Schrödinger, Inc. Cyclic compounds and methods of using same
WO2021134004A1 (en) 2019-12-27 2021-07-01 Schrodinger, 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
US20240148732A1 (en) 2021-01-26 2024-05-09 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
KR20240107329A (ko) * 2021-12-15 2024-07-09 신라젠(주) 신생물성 질환을 치료하는 방법
JP2024544083A (ja) * 2021-12-15 2024-11-27 シルラジェン，インコーポレイテッド 修飾ベータ－シクロデキストリンを含む医薬組成物
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.
RS20050944A (sr) * 2003-05-22 2008-06-05 Nerviano Medical Sciences S.R.L., 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
ATE547411T1 (de) 2006-12-04 2012-03-15 Jiangsu Simcere Pharmaceutical R & D Co Ltd 3-pyrrolo-cyclohexylen-2-dihydroindolinonderiva e und anwendungen davon
SI2125822T1 (sl) * 2006-12-21 2015-01-30 Nerviano Medical Sciences S.R.L. Substituirani pirazolo-kinazolinski derivati, postopek za njihovo pripravo in njihova uporaba kot inhibitorji kinaze
CN101687869A (zh) * 2007-07-16 2010-03-31 诺瓦提斯公司 作为mk2抑制剂的四环内酰胺衍生物
JP2011509261A (ja) 2008-01-07 2011-03-24 シンタ ファーマシューティカルズ コーポレーション 炎症および免疫関連用途向けの化合物
WO2009137492A1 (en) * 2008-05-05 2009-11-12 Abbott Laboratories Heteroaryl-fused macrocyclic pyrimidine derivatives
WO2009156315A1 (en) * 2008-06-26 2009-12-30 Nerviano Medical Sciences S.R.L. Pyrazolo-quinazolines
US8946226B2 (en) * 2008-07-29 2015-02-03 Nerviano Medical Sciences S.R.L. Use of CDK inhibitor for the treatment of glioma
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
US8912194B2 (en) * 2008-11-24 2014-12-16 Nerviano Medical Sciences S.R.L. CDK inhibitor for the treatment of mesothelioma
JP5650193B2 (ja) * 2009-03-20 2015-01-07 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 胸腺腫の治療のためのキナーゼ阻害剤の使用
ES2660146T3 (es) * 2009-04-29 2018-03-21 Nerviano Medical Sciences S.R.L. Sales del inhibidor de cdk
AR076784A1 (es) * 2009-05-26 2011-07-06 Nerviano Medical Sciences Srl Combinacion terapeutica que comprende un inhibidor de plk1 y un agente antineoplasico
CN103626777B (zh) * 2009-07-29 2015-10-21 内尔维阿诺医学科学有限公司 Plk抑制剂的盐类
JP5997143B2 (ja) * 2010-07-30 2016-09-28 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 タンパク質キナーゼ活性の調整剤としてのイソオキサゾロ−キナゾリン
CA2812223C (en) * 2010-12-17 2019-03-12 Nerviano Medical Sciences S.R.L. Substituted pyrazolo-quinazoline derivatives as kinase inhibitors
EP2668190B1 (en) 2011-01-26 2016-08-17 Nerviano Medical Sciences S.r.l. Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors

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