JP5990595B2 - トロポミオシンレセプターキナーゼ(Trk)阻害剤としての置換されたピラゾロ[1,5−a]ピリジン - Google Patents

トロポミオシンレセプターキナーゼ(Trk)阻害剤としての置換されたピラゾロ[1,5−a]ピリジン Download PDF

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JP5990595B2
JP5990595B2 JP2014545388A JP2014545388A JP5990595B2 JP 5990595 B2 JP5990595 B2 JP 5990595B2 JP 2014545388 A JP2014545388 A JP 2014545388A JP 2014545388 A JP2014545388 A JP 2014545388A JP 5990595 B2 JP5990595 B2 JP 5990595B2
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pyridine
pyrazolo
carboxamide
pyrrolidin
difluorophenyl
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JP2015500275A5 (enExample
JP2015500275A (ja
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プラディプ クマール サスマル,
プラディプ クマール サスマル,
シャハダット アハメド,
シャハダット アハメド,
アショク テヒム,
アショク テヒム,
ビディヤダール パラドカール,
ビディヤダール パラドカール,
プラサナ エム. ダッタトレヤ,
プラサナ エム. ダッタトレヤ,
ナンジェゴウダ ジャガデーシュ マビナハリ,
ナンジェゴウダ ジャガデーシュ マビナハリ,
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ドクター レディズ ラボラトリーズ リミテッド
ドクター レディズ ラボラトリーズ リミテッド
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    • C07ORGANIC CHEMISTRY
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    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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    • A61K31/635Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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JP2014545388A 2011-12-12 2012-12-12 トロポミオシンレセプターキナーゼ(Trk)阻害剤としての置換されたピラゾロ[1,5−a]ピリジン Expired - Fee Related JP5990595B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN4329/CHE/2011 2011-12-12
IN4329CH2011 2011-12-12
PCT/IB2012/003012 WO2013088256A1 (en) 2011-12-12 2012-12-12 Substituted pyrazolo[1,5-a] pyridine as tropomyosin receptor kinase (trk) inhibitors

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JP2015500275A JP2015500275A (ja) 2015-01-05
JP2015500275A5 JP2015500275A5 (enExample) 2015-11-05
JP5990595B2 true JP5990595B2 (ja) 2016-09-14

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EP (2) EP2791138B1 (enExample)
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KR (2) KR101849143B1 (enExample)
CN (1) CN104114553B (enExample)
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BR (1) BR112014014276A2 (enExample)
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Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8450322B2 (en) 2008-09-22 2013-05-28 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds as Trk kinase inhibitors
TR201807039T4 (tr) 2008-10-22 2018-06-21 Array Biopharma Inc Trk kinaz inhibitörleri olarak sübstitüe edilmiş pirazolo[1,5-]pirimidin bileşikleri.
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
ES2628418T3 (es) 2010-05-20 2017-08-02 Array Biopharma, Inc. Compuestos macrocíclicos como inhibidores de la TRK cinasa
US9045478B2 (en) * 2011-12-12 2015-06-02 Dr. Reddy's Laboratories Ltd. Substituted pyrazolo[1,5-a] pyridine as tropomyosin receptor kinase (Trk) inhibitors
TWI663159B (zh) * 2013-12-10 2019-06-21 美商健臻公司 原肌球蛋白相關之激酶(trk)抑制劑
JP2016540811A (ja) 2013-12-20 2016-12-28 ファイザー・リミテッドPfizer Limited N−アシルピペリジンエーテルトロポミオシン関連キナーゼ阻害剤
CN103819343B (zh) * 2014-02-17 2016-03-23 青岛农业大学 化合物2-烯丙基-4-氟-6-硝基苯酚的制备方法和农用生物活性
WO2015143652A1 (en) * 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
WO2015159175A1 (en) 2014-04-15 2015-10-22 Pfizer Inc. Tropomyosin-related kinase inhibitors containing both a 1h-pyrazole and a pyrimidine moiety
EP3140298A1 (en) 2014-05-07 2017-03-15 Pfizer Inc. Tropomyosin-related kinase inhibitors
EP3139743B1 (en) * 2014-05-08 2018-03-14 Bayer CropScience Aktiengesellschaft Pyrazolopyridine sulfonamides as nematicides
WO2015200341A1 (en) 2014-06-23 2015-12-30 Dr. Reddy's Laboratories Ltd. Substituted imidazo[1,2-a]pyridine compounds useful for the treatment of pain
WO2016009296A1 (en) 2014-07-16 2016-01-21 Pfizer Inc. N-acylpiperidine ether tropomyosin-related kinase inhibitors
WO2016020784A1 (en) 2014-08-05 2016-02-11 Pfizer Inc. N-acylpyrrolidine ether tropomyosin-related kinase inhibitors
PT3699181T (pt) 2014-11-16 2023-04-05 Array Biopharma Inc Forma cristalina de hidrogenossulfato de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
SG11201704872RA (en) 2014-12-18 2017-07-28 Genzyme Corp Pharmaceutical formulations of tropomyosin related kinase (trk) inhibitors
CN104672121B (zh) * 2015-02-16 2017-10-24 上海华默西医药科技有限公司 2r‑(2,5‑二氟苯基)吡咯烷盐酸盐的制备方法
UA118822C2 (uk) * 2015-05-29 2019-03-11 Вуксі Фортуне Фармасьютікал Ко., Лтд Інгібітор янус-кінази
TN2018000138A1 (en) 2015-10-26 2019-10-04 Array Biopharma Inc Point mutations in trk inhibitor-resistant cancer and methods relating to the same
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
CN109414442B (zh) 2016-04-04 2024-03-29 洛克索肿瘤学股份有限公司 一种化合物的液体制剂
DK3800189T3 (da) 2016-05-18 2023-07-31 Loxo Oncology Inc Fremstilling af (s)-n-(5-((r)-2-(2,5-difluorphenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidin-1-carboxamid
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
JP7046940B2 (ja) 2016-10-28 2022-04-04 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド 神経栄養因子チロシンキナーゼ受容体阻害剤として用いられるアミノピラゾロピリミジン化合物
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
EP3621615B1 (en) * 2017-05-12 2023-11-15 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2018218051A1 (en) 2017-05-25 2018-11-29 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2018218042A1 (en) 2017-05-25 2018-11-29 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US10246439B2 (en) 2017-05-25 2019-04-02 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US10800760B2 (en) 2017-05-31 2020-10-13 Nantbio, Inc. Trk inhibition
US10738033B2 (en) 2017-05-31 2020-08-11 Nantbio, Inc. Trk inhibition
CN109824566A (zh) * 2017-07-19 2019-05-31 浙江师范大学 一种(r)-2-(2,5-二氟苯基)吡咯烷的合成方法
WO2019046186A1 (en) 2017-08-28 2019-03-07 Enanta Pharmaceuticals, Inc. INHIBITORS OF KINASE 1 REGULATING THE APOPTOTIC SIGNAL CONTAINING TETRAZOLES AND METHODS OF USE THEREOF
EP3700576A1 (en) 2017-10-26 2020-09-02 Array Biopharma Inc. Formulations of a macrocyclic trk kinase inhibitor
CN109867668B (zh) * 2017-12-02 2021-03-26 广东东阳光药业有限公司 一种吡唑[1,5-a]吡啶化合物的晶型及其药物组合物和用途
CN109867671B (zh) * 2017-12-02 2020-07-07 广东东阳光药业有限公司 一种吡唑[1,5-a]吡啶化合物的晶型及其药物组合物和用途
CN109867672B (zh) * 2017-12-02 2020-07-07 广东东阳光药业有限公司 吡唑[1,5-a]吡啶衍生物的盐及其用途
WO2019125967A1 (en) * 2017-12-20 2019-06-27 Sunshine Lake Pharma Co., Ltd. Salts of pyrazolo[1,5-a]pyridine derivative and use thereof
CN108218754B (zh) * 2018-01-23 2021-05-07 广东赛烽医药科技有限公司 一种2-(2,5-二氟苯基)吡咯烷的制备方法
MX2020008273A (es) * 2018-02-06 2020-11-24 Univ Miami Inhibidores de la cinasa del complejo de activacion transcripcional notch ("nack") y metodos para el uso de los mismos.
CA3095366A1 (en) 2018-03-29 2019-10-03 Loxo Oncology, Inc. Treatment of trk-associated cancers
US11008304B2 (en) 2018-05-02 2021-05-18 Enanta Pharmaceuticals, Inc. Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2019213239A1 (en) 2018-05-02 2019-11-07 Enanta Pharmaceuticals Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
GB201811825D0 (en) 2018-07-19 2018-09-05 Benevolentai Bio Ltd Organic compounds
CN108794370A (zh) * 2018-07-31 2018-11-13 上海弈柯莱生物医药科技有限公司 一种拉罗替尼中间体的制备方法
US10968199B2 (en) 2018-08-22 2021-04-06 Enanta Pharmaceuticals, Inc. Cycloalkyl-containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
GB201813791D0 (en) 2018-08-23 2018-10-10 Benevolental Bio Ltd Organic compounds
CN111171019A (zh) * 2018-11-13 2020-05-19 上海轶诺药业有限公司 一类五元并六元杂环化合物及其作为蛋白受体激酶抑制剂的用途
WO2020106707A1 (en) 2018-11-19 2020-05-28 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
CN109593802B (zh) * 2018-12-24 2021-10-01 上海健康医学院 一种(r)-2-(2,5-二氟苯基)吡咯烷或其盐的制备方法
KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
US11466033B2 (en) 2019-03-25 2022-10-11 Enanta Pharmaceuticals, Inc. Substituted pyridines as apoptosis signal-regulating kinase 1 inhibitors
CN110015980A (zh) * 2019-05-14 2019-07-16 大连联化化学有限公司 一种合成叔丁基亚磺酰胺的方法
JP7261428B2 (ja) * 2019-06-05 2023-04-20 クワンチョウ ジョーヨー ファーマテック カンパニー,リミティド ピロロピリミジン類化合物及びその使用
CN110751853B (zh) * 2019-10-25 2021-05-18 百度在线网络技术(北京)有限公司 停车位数据的有效性识别方法和装置
JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム(インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル) キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
WO2021132577A1 (ja) * 2019-12-27 2021-07-01 日本たばこ産業株式会社 アシルスルファミド化合物及びその医薬用途
CN115315254A (zh) 2020-01-22 2022-11-08 博善人工智能生物科技有限公司 药物组合物及其用途
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN115297863A (zh) 2020-01-22 2022-11-04 博善人工智能生物科技有限公司 包含咪唑并[1,2-b]哒嗪化合物的表面药物组合物
CA3173804A1 (en) * 2020-05-15 2021-11-18 Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd Fused aza-heterocyclic amide compound and use thereof
WO2022026565A1 (en) * 2020-07-29 2022-02-03 Ideaya Biosciences, Inc. Cyclized acetamido derivatives as dna polymerase theta inhibitors
CN112979646B (zh) * 2021-03-08 2022-01-14 北京富龙康泰生物技术有限公司 一种咪唑并吡啶类衍生物
WO2022234287A1 (en) 2021-05-06 2022-11-10 Benevolentai Bio Limited Imidazopyridazine derivatives useful as trk inhibitors
WO2023083356A1 (zh) * 2021-11-15 2023-05-19 石药集团中奇制药技术(石家庄)有限公司 固体形式的氮杂稠环酰胺类化合物及其用途
CN116115618B (zh) * 2021-11-15 2025-07-08 石药集团中奇制药技术(石家庄)有限公司 一种治疗肿瘤的药物
CN115772170B (zh) * 2021-12-03 2025-05-16 徐诺药业(南京)有限公司 一种吡唑并[1,5-a]吡啶衍生物及其制备方法和应用
CN120677154A (zh) * 2022-11-30 2025-09-19 缆图药品公司 用于治疗荨麻疹的作为野生型c-kit激酶抑制剂的n-苯基-吡唑并[1,5-a]吡啶-3-甲酰胺衍生物
JP2025541191A (ja) * 2022-12-07 2025-12-18 サード ハーモニック バイオ, インコーポレイテッド C-kitキナーゼ阻害剤としての化合物及び組成物

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002501506A (ja) * 1997-05-03 2002-01-15 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー ドーパミンd▲下3▼受容体のモジュレーターとしてのテトラヒドロイソキノリン誘導体
JP2003231687A (ja) 2002-02-04 2003-08-19 Japan Tobacco Inc ピラゾリル縮合環化合物及びその医薬用途
JP4602076B2 (ja) * 2002-06-04 2010-12-22 ネオジェネシス ファーマシューティカルズ インコーポレイテッド 抗ウイルス剤としてのピラゾロ[1,5a]ピリミジン化合物
JP4511352B2 (ja) 2002-07-25 2010-07-28 ファイザー・インク 抗癌薬として有用なイソチアゾール誘導体
US7141568B2 (en) 2003-07-09 2006-11-28 Pfizer Italia S.R.L. Pyrrolo[3,4-c]pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
RU2008127263A (ru) * 2005-12-08 2010-01-20 Новартис АГ (CH) ПИРАЗОЛ [1,5-a] ПИРИДИН-3-КАРБОНОВЫЕ КИСЛОТЫ В КАЧЕСТВЕ ИНГИБИТОРОВ EphB-И VEGFR2-КИНАЗЫ
WO2009008748A1 (en) 2007-07-11 2009-01-15 Auckland Uniservices Limited Pyrazolo[1,5-a]pyridines and their use in cancer therapy
AU2009246687B2 (en) 2008-05-13 2012-08-09 Irm Llc Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors
TR201807039T4 (tr) 2008-10-22 2018-06-21 Array Biopharma Inc Trk kinaz inhibitörleri olarak sübstitüe edilmiş pirazolo[1,5-]pirimidin bileşikleri.
CA2828219A1 (en) 2011-02-25 2012-08-30 Irm Llc Pyrazolo [1,5-a] pyridines as trk inhibitors
US9045478B2 (en) * 2011-12-12 2015-06-02 Dr. Reddy's Laboratories Ltd. Substituted pyrazolo[1,5-a] pyridine as tropomyosin receptor kinase (Trk) inhibitors

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