RU2732405C2 - Хиральные диарильные макроциклы в качестве модуляторов протеинкиназ - Google Patents

Хиральные диарильные макроциклы в качестве модуляторов протеинкиназ Download PDF

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RU2732405C2
RU2732405C2 RU2018103907A RU2018103907A RU2732405C2 RU 2732405 C2 RU2732405 C2 RU 2732405C2 RU 2018103907 A RU2018103907 A RU 2018103907A RU 2018103907 A RU2018103907 A RU 2018103907A RU 2732405 C2 RU2732405 C2 RU 2732405C2
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nhs
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calkyl
cycloalkyl
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Цзинжун Дж. ЦУЙ
Ишань ЛИ
Эван В. РОДЖЕРС
Даюн ЧЖАЙ
Вэй ДЭН
Джейн УНГ
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Тёрнинг Поинт Терапьютикс, Инк.
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/22Heterocyclic 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 four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
RU2018103907A 2015-07-02 2016-06-30 Хиральные диарильные макроциклы в качестве модуляторов протеинкиназ RU2732405C2 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562188043P 2015-07-02 2015-07-02
US62/188,043 2015-07-02
US201662353728P 2016-06-23 2016-06-23
US62/353,728 2016-06-23
PCT/US2016/040329 WO2017004342A1 (en) 2015-07-02 2016-06-30 Chiral diaryl macrocycles as modulators of protein kinases

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RU2018103907A RU2018103907A (ru) 2019-08-05
RU2018103907A3 RU2018103907A3 (enExample) 2019-10-07
RU2732405C2 true RU2732405C2 (ru) 2020-09-16

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US (2) US10316044B2 (enExample)
EP (1) EP3317285B1 (enExample)
JP (1) JP6871903B2 (enExample)
KR (1) KR102599788B1 (enExample)
CN (1) CN107735399B (enExample)
AU (2) AU2016287568B2 (enExample)
CA (1) CA2989327A1 (enExample)
ES (1) ES2864839T3 (enExample)
IL (1) IL256377A (enExample)
MX (1) MX2017017097A (enExample)
RU (1) RU2732405C2 (enExample)
TW (1) TW201716415A (enExample)
WO (1) WO2017004342A1 (enExample)

Families Citing this family (66)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS53350B (sr) 2008-09-22 2014-10-31 Array Biopharma, Inc. Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze
EP2350071B1 (en) 2008-10-22 2014-01-08 Array Biopharma, Inc. SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
PL3205654T3 (pl) 2010-05-20 2019-08-30 Array Biopharma, Inc. Związki makrocykliczne jako inhibitory kinazy TRK
SG10202000191YA (en) 2014-01-24 2020-03-30 Turning Point Therapeutics Inc Diaryl macrocycles as modulators of protein kinases
CN107428760B (zh) 2014-11-16 2021-04-27 阵列生物制药公司 (s)-n-(5-((r)-2-(2,5-二氟苯基)-吡咯烷-1-基)-吡唑并[1,5-a]嘧啶-3-基)-3-羟基吡咯烷-1-甲酰胺硫酸氢盐的晶型
JP6871903B2 (ja) 2015-07-02 2021-05-19 ターニング・ポイント・セラピューティクス・インコーポレイテッドTurning Point Therapeutics,Inc. プロテインキナーゼのモジュレーターとしてのキラルジアリール大環状分子
RU2765181C2 (ru) * 2015-07-06 2022-01-26 Тёрнинг Поинт Терапьютикс, Инк. Полиморфная форма диарильного макроцикла
LT3733187T (lt) 2015-07-21 2024-12-10 Turning Point Therapeutics, Inc. Chiralinis diarilo makrociklas ir jo panaudojimas vėžio gydymui
BR112018008357A2 (en) 2015-10-26 2018-11-27 Loxo Oncology, Inc. dot mutations in trk inhibitor resistant cancer and related methods
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
FI3439662T3 (fi) 2016-04-04 2024-09-04 Loxo Oncology Inc (s)-n-(5-((r)-2-(2,5-difluorifenyyli)pyrrolidin-1-yyli)pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidin nesteformulaatioita
HRP20201984T1 (hr) 2016-05-18 2021-04-16 Loxo Oncology, Inc. Priprema (s)-n-(5-((r)-2-(2,5-difluorofenil)pirolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida
WO2018009417A1 (en) * 2016-07-05 2018-01-11 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
SG11201900163PA (en) * 2016-07-28 2019-02-27 Tp Therapeutics Inc Macrocycle kinase inhibitors
SG10201912574WA (en) 2016-09-28 2020-02-27 Blade Therapeutics Inc Calpain modulators and therapeutic uses thereof
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
JOP20190213A1 (ar) * 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
CN107586796B (zh) * 2017-07-20 2021-08-06 暨明医药科技(苏州)有限公司 (r)-2-(1-氨基乙基)-4-氟苯酚的合成方法
SMT202400343T1 (it) 2017-07-28 2024-11-15 Turning Point Therapeutics Inc Composti macrociclici e loro usi
MX2020001979A (es) * 2017-08-23 2020-03-24 Chia Tai Tianqing Pharmaceutical Group Co Ltd Macrociclo que contiene aminopirazol y pirimidina y composicion farmaceutica y uso de la misma.
CN109516999B (zh) * 2017-11-01 2021-08-17 郑州泰基鸿诺医药股份有限公司 用作蛋白质激酶调节剂的化合物及其应用
JP6986789B2 (ja) * 2017-11-10 2021-12-22 エンジェクス ファーマシューティカル インコーポレイテッド 化合物、その薬学的に許容される塩、化合物の使用および医薬組成物
HUE060711T2 (hu) 2017-12-19 2023-04-28 Turning Point Therapeutics Inc Makrociklusos vegyületek betegségek kezelésére
CN109456331B (zh) 2017-12-22 2020-06-05 深圳市塔吉瑞生物医药有限公司 一种取代的吡唑并[1,5-a]嘧啶化合物及其药物组合物及用途
US11345703B2 (en) 2018-01-23 2022-05-31 Shenzhen Targetrx, Inc. Substituted pyrazolo[1,5-a]pyrimidine macrocyclic compound
TW201932472A (zh) * 2018-01-30 2019-08-16 大陸商上海吉倍生物技術有限公司 具有大環分子結構的化合物及其用途
JP2021519297A (ja) * 2018-03-28 2021-08-10 フォチョン・ファーマシューティカルズ・リミテッドFochon Pharmaceuticals, Ltd. Trkキナーゼ阻害剤としての大環状化合物
DK3783000T3 (da) * 2018-04-18 2022-08-01 Hitgen Inc Makrocyklisk kinasehæmmer
WO2019210835A1 (zh) * 2018-05-04 2019-11-07 正大天晴药业集团股份有限公司 作为蛋白激酶调节剂的二芳基大环化合物
CN110577532B (zh) * 2018-06-08 2022-06-03 江苏威凯尔医药科技有限公司 原肌球蛋白受体激酶抑制剂及其制备方法和应用
WO2019233461A1 (zh) * 2018-06-08 2019-12-12 江苏威凯尔医药科技有限公司 原肌球蛋白受体激酶抑制剂及其制备方法和应用
CN110950889B (zh) * 2018-09-27 2022-04-05 北京赛林泰医药技术有限公司 一种多靶点激酶抑制剂及其制备方法和用途
JP2022511381A (ja) * 2018-09-29 2022-01-31 シャンドン ルイ ファーマシューティカル カンパニー リミテッド 選択的Trk阻害剤としてのピラゾロピリミジン誘導体
SI3870579T1 (sl) 2018-10-22 2025-03-31 Alumis Inc. Inhibitorji tyk2 in njihova uporaba
CN111171049B (zh) * 2018-11-09 2021-06-04 山东轩竹医药科技有限公司 酪氨酸激酶抑制剂及其用途
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
CN111171020A (zh) 2018-11-13 2020-05-19 上海轶诺药业有限公司 一类六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
CN113811534B (zh) * 2019-03-11 2024-10-29 阿鲁米斯公司 Tyk2抑制剂和其用途
US11780842B2 (en) * 2019-03-26 2023-10-10 Ventyx Biosciences, Inc. TYK2 pseudokinase ligands
EP3974434B1 (en) 2019-05-21 2025-11-19 Zhejiang Hisun Pharmaceutical Co., Ltd. Macrolide derivatives, preparation method and application thereof
MX2021015756A (es) * 2019-06-19 2022-01-27 Turning Point Therapeutics Inc Polimorfos de un inhibidor de cinasas macrociclicas.
WO2020257189A1 (en) * 2019-06-19 2020-12-24 Turning Point Therapeutics, Inc. Macrocycles for treating disease
WO2020257165A1 (en) * 2019-06-19 2020-12-24 Turning Point Therapeutics, Inc. Macrocycles for use in treating disease
WO2021027503A1 (zh) * 2019-08-12 2021-02-18 罗欣药业(上海)有限公司 三环类化合物、其制备方法、中间体及应用
US12497412B2 (en) 2019-11-18 2025-12-16 Guangzhou Joyo Pharmatech Co., Ltd. Compound as highly selective ROS1 inhibitor and use thereof
TW202133855A (zh) * 2019-11-27 2021-09-16 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
KR20220134522A (ko) * 2019-11-27 2022-10-05 터닝 포인트 테라퓨틱스, 인크. 디아릴 매크로시클릭 화합물을 수반하는 병용 요법
IL293458A (en) 2019-12-03 2022-07-01 Turning Point Therapeutics Inc Macrocycles for use in treating disease
TWI760005B (zh) * 2019-12-13 2022-04-01 大陸商賽諾哈勃藥業(成都)有限公司 具有大環結構的含氟並雜環衍生物及其用途
CN113045575B (zh) * 2019-12-27 2022-06-17 成都倍特药业股份有限公司 一种化合物的制备方法及其中间体和中间体的制备方法
CN113527298B (zh) * 2020-04-17 2025-01-03 浙江海正药业股份有限公司 大环内酰胺类衍生物、及其制备方法和用途
CN113735856A (zh) * 2020-05-29 2021-12-03 百极弘烨(南通)医药科技有限公司 大环jak抑制剂及其应用
EP4163283A1 (en) * 2020-06-04 2023-04-12 Scinnohub Pharmaceutical Co., Ltd Compound having macrocyclic structure and use thereof
CN114073704B (zh) * 2020-08-14 2023-08-11 赛诺哈勃药业(成都)有限公司 具有大环结构的含氟并杂环衍生物的应用
JP2023541203A (ja) * 2020-09-16 2023-09-28 アルミス インコーポレイテッド Tyk2阻害剤およびその使用
CN114591351B (zh) * 2020-12-03 2023-12-05 成都科岭源医药技术有限公司 一种多环化合物及其制备方法和用途
CN114763360A (zh) * 2021-01-15 2022-07-19 广州百霆医药科技有限公司 手性大环化合物作为蛋白激酶抑制剂及其用途
WO2022218276A1 (zh) * 2021-04-12 2022-10-20 成都倍特药业股份有限公司 含氟大环结构化合物的固体形态、制备方法和应用
WO2023025141A1 (zh) * 2021-08-23 2023-03-02 正大天晴药业集团股份有限公司 含有氨基的大环化合物在治疗trk激酶介导的肿瘤中的用途
CN113582994B (zh) * 2021-09-28 2022-02-11 北京鑫开元医药科技有限公司 具有trk激酶抑制活性的化合物、制备方法、组合物及其用途
CN116063326B (zh) * 2021-11-02 2025-08-05 赛诺哈勃药业(成都)有限公司 作为蛋白激酶调节剂的含氨基大环化合物
WO2023208244A1 (zh) * 2022-04-29 2023-11-02 南京明德新药研发有限公司 大环类化合物及其应用
EP4585598A1 (en) 2022-09-07 2025-07-16 Suzhou Langrui Biopharmaceutical Co., Ltd. Macrocyclic imidazo[1,2-b]pyridazine derivative, preparation method therefor, and use thereof
CN115746023B (zh) * 2022-10-27 2024-08-09 复旦大学 一种作为蛋白激酶抑制剂的含吲唑结构的杂环大环化合物及其制备方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011146336A1 (en) * 2010-05-20 2011-11-24 Array Biopharma Inc. Macrocyclic compounds as trk kinase inhibitors
WO2012034091A1 (en) * 2010-09-09 2012-03-15 Irm Llc Imidazo [1, 2] pyridazin compounds and compositions as trk inhibitors
WO2013132376A1 (en) * 2012-03-06 2013-09-12 Pfizer Inc. Macrocyclic derivatives for the treatment of proliferative diseases
US20140107099A1 (en) * 2008-10-31 2014-04-17 Genentech, Inc. Pyrazolopyrimidine jak inhibitor compounds and methods
EA019558B1 (ru) * 2009-10-13 2014-04-30 Эланко Энимал Хэлс Аиэлэнд Лимитед Макроциклические ингибиторы интегразы

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4838925A (en) 1986-04-25 1989-06-13 E. I. Du Pont De Nemours And Company Heterocyclic acyl sulfonamides
ES2021105B3 (es) 1987-03-07 1991-10-16 Bayer Ag Procedimiento para la obtencion de 5-amino-4,6-dihalogeno piridinas.
ES2149869T3 (es) 1993-03-25 2000-11-16 Upjohn Co Derivados de indol sustituidos por formil o ciano con actividad dopominergica.
YU49200B (sh) 1993-12-07 2004-09-03 Eli Lilly And Company Inhibitori proteinske kinaze c
FR2746309B1 (fr) 1996-03-22 1998-04-17 Oreal Composition de teinture des fibres keratiniques contenant des pyrazolopyrimidineoxo ; leur utilisation pour la teinture comme coupleurs, procedes de teinture
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
FR2793791B1 (fr) 1999-05-19 2002-01-25 Univ Paris 7 Denis Diderot Nouveaux composes inhibiteurs specifiques de phospholipases a2
BR0112918A (pt) 2000-07-31 2003-07-01 Hoffmann La Roche Composto, utilização do mesmo, processo de tratamento de distúrbios, processo para a preparação de composto, composição farmacêutica que compreende esse composto, processo para preparar uma composição e processo de tratamento de obesidade em um ser humano
ES2245994T3 (es) 2000-12-08 2006-02-01 Ortho-Mcneil Pharmaceutical, Inc. Compuestos macro-heterociclicos utilizados como inhibidores de quinasa.
AU2002254114A1 (en) 2001-03-23 2002-10-08 Eli Lilly And Company Non-imidazole aryl alkylamines compounds as histamine h3 receptor antagonists, preparation and therapeutic uses
WO2004052315A2 (en) 2002-12-11 2004-06-24 Merck & Co., Inc. Tyrosine kinase inhibitors
EA201100450A1 (ru) 2008-09-08 2011-10-31 Мерк Патент Гмбх Макроциклические пирамидины в качестве ингибиторов протеинкиназы
RS53350B (sr) * 2008-09-22 2014-10-31 Array Biopharma, Inc. Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze
EP2350071B1 (en) * 2008-10-22 2014-01-08 Array Biopharma, Inc. SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS
WO2010063487A1 (en) 2008-12-05 2010-06-10 Merz Pharma Gmbh & Co. Kgaa Pyrazolopyrimidines, a process for their preparation and their use as medicine
WO2010086040A1 (en) 2009-01-29 2010-08-05 Biomarin Iga, Ltd. Pyrazolo-pyrimidines for treatment of duchenne muscular dystrophy
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
EP2509979B1 (en) 2009-12-07 2016-05-25 Boehringer Ingelheim International GmbH Heterocyclic compounds containing a pyrrolopyridine or benzimidazole core
US9150577B2 (en) 2009-12-07 2015-10-06 Boehringer Ingelheim International Gmbh Heterocyclic compounds containing an indole core
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
WO2012075393A2 (en) 2010-12-02 2012-06-07 President And Fellows Of Harvard College Activators of proteasomal degradation and uses thereof
EP2508607A1 (en) 2011-04-07 2012-10-10 Helmholtz-Zentrum für Infektionsforschung GmbH Medicament for liver regeneration and for treatment of liver failure
WO2013001310A1 (en) 2011-06-30 2013-01-03 Centro Nacional De Investigaciones Oncológicas (Cnio) Macrocyclic compounds and their use as cdk8 inhibitors
JP2014521750A (ja) 2011-08-19 2014-08-28 メルク・シャープ・アンド・ドーム・コーポレーション マクロラクタムを調製するための方法および中間体
WO2013045701A2 (en) 2011-09-29 2013-04-04 L'oreal Dyeing process using a composition comprising a glycosyl iridoid compound and a nucleophile or an amino or thio polymer, composition and devices therefor
WO2013045702A2 (en) 2011-09-29 2013-04-04 L'oreal Dye composition comprising a non-glycosyl iridoid compound and a specific nucleophile or an amino or thio polymer, dyeing process, and device therefor
KR20140078710A (ko) 2011-09-30 2014-06-25 온코디자인 에스.에이. 거대고리 flt3 키나제 억제제
KR20140077963A (ko) 2011-10-20 2014-06-24 글락소스미스클라인 엘엘씨 시르투인 조절제로서의 치환된 비시클릭 아자-헤테로사이클 및 유사체
WO2013134228A1 (en) 2012-03-09 2013-09-12 Lexicon Pharmaceuticals, Inc. PYRAZOLO[1,5-a]PYRIMIDINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE
EP2822559B1 (en) 2012-03-09 2018-05-02 Lexicon Pharmaceuticals, Inc. Imidazo[1,2-b]pyridazine-based compounds, compositions comprising them, and uses thereof
GB201205669D0 (en) 2012-03-30 2012-05-16 Agency Science Tech & Res Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof
JP2016506921A (ja) 2013-01-30 2016-03-07 バイエル ファーマ アクチエンゲゼルシャフト アミノ置換イソチアゾール
EP2989082A1 (en) 2013-04-23 2016-03-02 LEK Pharmaceuticals d.d. Novel synthetic process to 8-chloro-1-methyl-benzo[d]azepine, novel intermediates and the production thereof
WO2015012328A1 (ja) 2013-07-24 2015-01-29 武田薬品工業株式会社 複素環化合物
CN104513253A (zh) * 2013-10-01 2015-04-15 南京波尔泰药业科技有限公司 用于治疗增殖性疾病的大环化合物
WO2015073267A1 (en) 2013-11-15 2015-05-21 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
SG10202000191YA (en) 2014-01-24 2020-03-30 Turning Point Therapeutics Inc Diaryl macrocycles as modulators of protein kinases
WO2016070241A1 (en) 2014-11-03 2016-05-12 Ctxt Pty Ltd Triazine compounds, compositions and synthesis
DK3233863T3 (da) 2014-12-15 2024-07-15 Cmg Pharmaceutical Co Ltd Kondenserede ringheteroarylforbindelser og anvendelse deraf som trk-hæmmere
JP6800158B2 (ja) 2015-02-20 2020-12-16 ライジェル ファーマシューティカルズ, インコーポレイテッド Gdf−8阻害剤
EP3267996B1 (en) 2015-03-12 2020-11-11 Merck Sharp & Dohme Corp. Pyrazolopyrimidine inhibitors of irak4 activity
EP3268367B8 (en) 2015-03-12 2022-11-16 Merck Sharp & Dohme LLC Carboxamide inhibitors of irak4 activity
WO2016177658A1 (en) 2015-05-05 2016-11-10 Bayer Pharma Aktiengesellschaft Amido-substituted cyclohexane derivatives
JP6871903B2 (ja) 2015-07-02 2021-05-19 ターニング・ポイント・セラピューティクス・インコーポレイテッドTurning Point Therapeutics,Inc. プロテインキナーゼのモジュレーターとしてのキラルジアリール大環状分子
RU2765181C2 (ru) 2015-07-06 2022-01-26 Тёрнинг Поинт Терапьютикс, Инк. Полиморфная форма диарильного макроцикла
LT3733187T (lt) 2015-07-21 2024-12-10 Turning Point Therapeutics, Inc. Chiralinis diarilo makrociklas ir jo panaudojimas vėžio gydymui
BR112018008357A2 (en) 2015-10-26 2018-11-27 Loxo Oncology, Inc. dot mutations in trk inhibitor resistant cancer and related methods
EP4292662A3 (en) 2016-03-04 2024-02-21 Vanderbilt University Substituted indole mcl-1 inhibitors
SG11201900163PA (en) 2016-07-28 2019-02-27 Tp Therapeutics Inc Macrocycle kinase inhibitors
JP2020533269A (ja) 2016-12-14 2020-11-19 デベロップメント センター フォー バイオテクノロジー 抗体−薬物複合体およびその使用
TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
SMT202400343T1 (it) 2017-07-28 2024-11-15 Turning Point Therapeutics Inc Composti macrociclici e loro usi

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140107099A1 (en) * 2008-10-31 2014-04-17 Genentech, Inc. Pyrazolopyrimidine jak inhibitor compounds and methods
EA019558B1 (ru) * 2009-10-13 2014-04-30 Эланко Энимал Хэлс Аиэлэнд Лимитед Макроциклические ингибиторы интегразы
WO2011146336A1 (en) * 2010-05-20 2011-11-24 Array Biopharma Inc. Macrocyclic compounds as trk kinase inhibitors
WO2012034091A1 (en) * 2010-09-09 2012-03-15 Irm Llc Imidazo [1, 2] pyridazin compounds and compositions as trk inhibitors
WO2013132376A1 (en) * 2012-03-06 2013-09-12 Pfizer Inc. Macrocyclic derivatives for the treatment of proliferative diseases

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