TW201716415A - 作為蛋白質激酶之調節劑的掌性二芳基巨環 - Google Patents

作為蛋白質激酶之調節劑的掌性二芳基巨環 Download PDF

Info

Publication number
TW201716415A
TW201716415A TW105121035A TW105121035A TW201716415A TW 201716415 A TW201716415 A TW 201716415A TW 105121035 A TW105121035 A TW 105121035A TW 105121035 A TW105121035 A TW 105121035A TW 201716415 A TW201716415 A TW 201716415A
Authority
TW
Taiwan
Prior art keywords
alkyl
nhs
nhc
group
cycloalkyl
Prior art date
Application number
TW105121035A
Other languages
English (en)
Chinese (zh)
Inventor
景榮 崔
一山 李
埃文W 羅杰斯
大勇 翟
維 鄧
珍 翁
Original Assignee
Tp生物醫藥公司
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Tp生物醫藥公司 filed Critical Tp生物醫藥公司
Publication of TW201716415A publication Critical patent/TW201716415A/zh

Links

Classifications

    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW105121035A 2015-07-02 2016-07-01 作為蛋白質激酶之調節劑的掌性二芳基巨環 TW201716415A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562188043P 2015-07-02 2015-07-02
US201662353728P 2016-06-23 2016-06-23

Publications (1)

Publication Number Publication Date
TW201716415A true TW201716415A (zh) 2017-05-16

Family

ID=57609146

Family Applications (1)

Application Number Title Priority Date Filing Date
TW105121035A TW201716415A (zh) 2015-07-02 2016-07-01 作為蛋白質激酶之調節劑的掌性二芳基巨環

Country Status (13)

Country Link
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
HRP20140309T1 (hr) 2008-10-22 2014-05-09 Array Biopharma, Inc. SUPSTITUIRANI SPOJEVI PIRAZOLO[1,5-a]PIRIMIDINA KAO INHIBITORI TRK KINAZE
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
KR102015402B1 (ko) 2010-05-20 2019-08-28 어레이 바이오파마 인크. Trk 키나제 저해제로서의 매크로시클릭 화합물
AU2015209239C1 (en) 2014-01-24 2026-05-07 Turning Point Therapeutics, Inc. Diaryl macrocycles as modulators of protein kinases
JP6914834B2 (ja) 2014-11-16 2021-08-04 アレイ バイオファーマ インコーポレイテッド (S)−N−(5−((R)−2−(2,5−ジフルオロフェニル)−ピロリジン−1−イル)−ピラゾロ[1,5−a]ピリミジン−3−イル)−3−ヒドロキシピロリジン−1−カルボキサミド硫酸水素塩の結晶形
MX2017017097A (es) 2015-07-02 2018-05-23 Tp Therapeutics Inc Macrociclos diarílicos quirales como moduladores de proteínas quinasas.
PL3319969T3 (pl) * 2015-07-06 2024-06-24 Turning Point Therapeutics, Inc. Diarylowe polimorfy makrocykliczne
LT3733187T (lt) * 2015-07-21 2024-12-10 Turning Point Therapeutics, Inc. Chiralinis diarilo makrociklas ir jo panaudojimas vėžio gydymui
TN2018000138A1 (en) 2015-10-26 2019-10-04 Array Biopharma Inc Point mutations in trk inhibitor-resistant cancer and methods relating to the same
AU2017246554B2 (en) 2016-04-04 2022-08-18 Loxo Oncology, Inc. Liquid formulations of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
KR102566858B1 (ko) 2016-05-18 2023-08-11 어레이 바이오파마 인크. (s)-n-(5-((r)-2-(2,5-디플루오로페닐)피롤리딘-1-일)-피라졸로[1,5-a]피리미딘-3-일)-3-히드록시피롤리딘-1-카르복사미드의 제조 방법
EP3481835A4 (en) * 2016-07-05 2020-02-26 Blade Therapeutics, Inc. CALPAIN MODULATORS AND THERAPEUTIC USE THEREOF
RU2019105587A (ru) 2016-07-28 2020-08-28 Тёрнинг Поинт Терапьютикс, Инк. Макроциклические ингибиторы киназ
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
CA3069232A1 (en) 2017-07-28 2019-01-31 Turning Point Therapeutics, Inc. Macrocyclic compounds and uses thereof
CN110945000B (zh) 2017-08-23 2021-09-03 正大天晴药业集团股份有限公司 含有氨基吡唑并嘧啶的大环化合物及其药物组合物和用途
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
US11098046B2 (en) 2017-11-10 2021-08-24 Angex Pharmaceutical, Inc. Macrocyclic compounds as TRK kinase inhibitors and uses thereof
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
CN111511749B (zh) * 2018-01-30 2022-02-08 上海吉倍生物技术有限公司 具有大环分子结构的化合物及其用途
MX2020010116A (es) * 2018-03-28 2020-11-06 Fochon Biosciences Ltd Compuestos macrociclicos como inhibidores de quinasas del receptor de tropomiosina (trk).
DK3783000T3 (da) * 2018-04-18 2022-08-01 Hitgen Inc Makrocyklisk kinasehæmmer
CN111918868B (zh) * 2018-05-04 2022-12-30 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
WO2020063965A1 (zh) * 2018-09-29 2020-04-02 南京明德新药研发有限公司 作为选择性Trk抑制剂的吡唑并嘧啶衍生物
HRP20250048T1 (hr) 2018-10-22 2025-03-28 Alumis Inc. Inhibitori tyk2 i 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
IL286248B2 (en) * 2019-03-11 2025-12-01 Alumis Inc Tyk2 inhibitors and uses thereof
EA202192625A1 (ru) * 2019-03-26 2022-03-21 Вентикс Байосайенсес, Инк. Лиганды псевдокиназы tyk2
WO2020233645A1 (zh) * 2019-05-21 2020-11-26 浙江海正药业股份有限公司 大环类衍生物、及其制备方法和用途
US20220411439A1 (en) * 2019-06-19 2022-12-29 Turning Point Therapeutics, Inc. Polymorphs of a macrocyclic kinase inhibitor
WO2020257165A1 (en) * 2019-06-19 2020-12-24 Turning Point Therapeutics, Inc. Macrocycles for use in treating disease
WO2020257189A1 (en) * 2019-06-19 2020-12-24 Turning Point Therapeutics, Inc. Macrocycles for 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
WO2021098703A1 (zh) 2019-11-18 2021-05-27 南京明德新药研发有限公司 作为高选择性ros1抑制剂的化合物及其应用
TW202133856A (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
JP7670711B2 (ja) * 2019-11-27 2025-04-30 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 ジアリール大環状化合物を含む併用療法
EP4069700B1 (en) * 2019-12-03 2024-07-03 Turning Point Therapeutics, Inc. Macrocycles for use in treating disease
JP2023504866A (ja) * 2019-12-13 2023-02-07 ▲賽▼▲諾▼哈勃▲薬▼▲業▼(成都)有限公司 大環構造を有するフッ素含有複素環誘導体およびその用途
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
JP2023528907A (ja) * 2020-06-04 2023-07-06 シンノハブ ファーマシューティカル カンパニー,リミティド 大環状構造を有する化合物及びその使用
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
WO2022060973A1 (en) * 2020-09-16 2022-03-24 Alumis, Inc. Tyk2 inhibitors and uses thereof
WO2022117090A1 (zh) * 2020-12-03 2022-06-09 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
KR20250056969A (ko) 2022-09-07 2025-04-28 수저우 랑루이 바이오파마슈티컬 씨오 엘티디 마크로시클릭 이미다조[1,2-b]피리다진 유도체 및 이의 제조 방법과 용도
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

Family Cites Families (58)

* 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
DE3861031D1 (de) 1987-03-07 1990-12-20 Bayer Ag Verfahren zur herstellung von 5-amino-4,6-dihalogenpyridinen.
DK0690843T3 (da) 1993-03-25 2000-11-13 Upjohn Co Fornyl- eller cyanosubstituerede indolderivater med dopaninerg aktivitet
PL182124B1 (pl) 1993-12-07 2001-11-30 Lilly Co Eli Nowe zwiazki oraz srodek farmaceutyczny przeznaczony do leczenia powiklan cukrzycowych lub do leczenia nowotworów PL PL PL PL PL PL PL PL
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
DE60113865T2 (de) 2000-07-31 2006-07-20 Vernalis Research Ltd., Winnersh Piperazin derivate
DE60112611T2 (de) 2000-12-08 2006-06-14 Ortho Mcneil Pharm Inc Makroheterocyclische verbindungen als kinase inhibitoren
WO2002076925A2 (en) 2001-03-23 2002-10-03 Eli Lilly And Company Non-imidazole aryl alkylamines compounds as histamine h3 receptor antagonists, preparation and therapeutic uses
AU2003299651A1 (en) 2002-12-11 2004-06-30 Merck And Co., Inc. Tyrosine kinase inhibitors
CA2735420C (en) 2008-09-08 2016-06-28 Merck Patent Gmbh Macrocyclic pyrimidines as protein kinase inhibitors
RS53350B (sr) * 2008-09-22 2014-10-31 Array Biopharma, Inc. Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze
HRP20140309T1 (hr) * 2008-10-22 2014-05-09 Array Biopharma, Inc. SUPSTITUIRANI SPOJEVI PIRAZOLO[1,5-a]PIRIMIDINA KAO INHIBITORI TRK KINAZE
CN102271515B (zh) * 2008-10-31 2014-07-02 健泰科生物技术公司 吡唑并嘧啶jak抑制剂化合物和方法
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
JP5624148B2 (ja) 2009-10-13 2014-11-12 エランコ・アニマル・ヘルス・アイルランド・リミテッド 大環状インテグラーゼ阻害剤
WO2011071725A1 (en) 2009-12-07 2011-06-16 Boehringer Ingelheim International Gmbh Heterocyclic compounds containing a pyrrolopyridine or benzimidazole core
WO2011071716A1 (en) 2009-12-07 2011-06-16 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
KR102015402B1 (ko) 2010-05-20 2019-08-28 어레이 바이오파마 인크. Trk 키나제 저해제로서의 매크로시클릭 화합물
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
US8637516B2 (en) * 2010-09-09 2014-01-28 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
BR112014003798A2 (pt) 2011-08-19 2017-03-01 Merck Sharp & Dohme método para fabricar um composto, e, composto
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
BR112014007622A2 (pt) 2011-09-30 2017-04-04 Oncodesign Sa inibidores de flt3 cinase macrocíclicos
RU2014120166A (ru) 2011-10-20 2015-11-27 ГЛЭКСОСМИТКЛАЙН ЭлЭлСи Замещенные бициклические аза-гетероциклы и их аналоги в качестве модуляторов сиртуина
WO2013132376A1 (en) 2012-03-06 2013-09-12 Pfizer Inc. Macrocyclic derivatives for the treatment of proliferative diseases
IN2014DN07384A (enExample) 2012-03-09 2015-04-24 Lexicon Pharmaceuticals Inc
NZ630719A (en) 2012-03-09 2017-01-27 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
ES2634014T3 (es) 2013-01-30 2017-09-26 Bayer Pharma Aktiengesellschaft Isotiazoles sustituidos con amino
CN105358534A (zh) 2013-04-23 2016-02-24 斯洛文尼亚莱柯制药股份有限公司 8-氯-1-甲基-苯并[d]吖庚因的新合成方法、新的中间体及其生产方法
JPWO2015012328A1 (ja) 2013-07-24 2017-03-02 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
AU2015209239C1 (en) 2014-01-24 2026-05-07 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
ES2983908T3 (es) 2014-12-15 2024-10-28 Cmg Pharmaceutical Co Ltd Compuestos heteroarílicos de anillo condensado y su uso como inhibidores de TRK
CN107531666A (zh) 2015-02-20 2018-01-02 里格尔药品股份有限公司 Gdf‑8抑制剂
US10155765B2 (en) 2015-03-12 2018-12-18 Merck Sharp & Dohme Corp. Carboxamide inhibitors of IRAK4 activity
WO2016144846A1 (en) 2015-03-12 2016-09-15 Merck Sharp & Dohme Corp. Pyrazolopyrimidine inhibitors of irak4 activity
MX2017014222A (es) 2015-05-05 2018-08-15 Bayer Pharma AG Derivados de ciclohexano sustituido con amido.
MX2017017097A (es) 2015-07-02 2018-05-23 Tp Therapeutics Inc Macrociclos diarílicos quirales como moduladores de proteínas quinasas.
PL3319969T3 (pl) 2015-07-06 2024-06-24 Turning Point Therapeutics, Inc. Diarylowe polimorfy makrocykliczne
LT3733187T (lt) 2015-07-21 2024-12-10 Turning Point Therapeutics, Inc. Chiralinis diarilo makrociklas ir jo panaudojimas vėžio gydymui
TN2018000138A1 (en) 2015-10-26 2019-10-04 Array Biopharma Inc Point mutations in trk inhibitor-resistant cancer and methods relating to the same
AU2017228385B2 (en) 2016-03-04 2021-11-04 Vanderbilt University Substituted indole Mcl-1 inhibitors
RU2019105587A (ru) 2016-07-28 2020-08-28 Тёрнинг Поинт Терапьютикс, Инк. Макроциклические ингибиторы киназ
US11384150B2 (en) 2016-12-14 2022-07-12 Development Center For Biotechnology Antibody-drug conjugates and uses thereof
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
CA3069232A1 (en) 2017-07-28 2019-01-31 Turning Point Therapeutics, Inc. Macrocyclic compounds and uses thereof

Also Published As

Publication number Publication date
RU2732405C2 (ru) 2020-09-16
RU2018103907A (ru) 2019-08-05
US20190284209A1 (en) 2019-09-19
EP3317285B1 (en) 2021-01-27
JP2018519343A (ja) 2018-07-19
EP3317285A1 (en) 2018-05-09
IL256377A (en) 2018-02-28
CN107735399A (zh) 2018-02-23
KR20180023970A (ko) 2018-03-07
JP6871903B2 (ja) 2021-05-19
US20180186813A1 (en) 2018-07-05
KR102599788B1 (ko) 2023-11-07
US10316044B2 (en) 2019-06-11
AU2016287568A1 (en) 2018-01-04
ES2864839T3 (es) 2021-10-14
CA2989327A1 (en) 2017-01-05
EP3317285A4 (en) 2019-02-27
WO2017004342A1 (en) 2017-01-05
RU2018103907A3 (enExample) 2019-10-07
US11008337B2 (en) 2021-05-18
AU2016287568B2 (en) 2020-08-20
AU2020217336A1 (en) 2020-08-27
MX2017017097A (es) 2018-05-23
CN107735399B (zh) 2021-01-26

Similar Documents

Publication Publication Date Title
CN107735399B (zh) 作为蛋白质激酶的调节剂的手性二芳基大环
CN111511746B (zh) 用于治疗疾病的巨环化合物
CN104507926B (zh) 丝氨酸/苏氨酸激酶抑制剂
WO2024041606A1 (zh) 具有抗kras突变肿瘤活性的化合物
TW202430162A (zh) 具有抗kras突變腫瘤活性的化合物
TW202346297A (zh) 具有抗kras突變腫瘤活性的化合物
TW201815799A (zh) 巨環激酶抑制劑
TW202525800A (zh) Ras抑制劑
CN106573906A (zh) 哌啶‑二酮衍生物
CN106536503A (zh) 一种酪氨酸激酶抑制剂及其用途
CN109745321B (zh) 包含fgfr4抑制剂的药物组合物
TW201930313A (zh) 巨環激酶抑制劑及其用途
TW202112783A (zh) 三環類化合物及其用途
TW202413377A (zh) 吲唑巨環化合物及其用途
WO2020257165A1 (en) Macrocycles for use in treating disease
WO2025148870A1 (zh) Ras抑制剂
CN114555597B (zh) 异柠檬酸脱氢酶(idh)抑制剂
CN114853679A (zh) 一种苯并咪唑类enl蛋白抑制剂及其制备方法和用途
WO2025218798A1 (zh) Kras g12d降解剂及其制备方法和应用
KR20210146320A (ko) 신규 아자인돌 유도체
HK1230591B (zh) 一种酪氨酸激酶抑制剂及其用途
HK1210166A1 (en) Fused tricyclic amide compounds as multiple kinase inhibitors
HK1231407B (zh) 作为蛋白质激酶的调节剂的二芳基巨环
HK1210166B (en) Fused tricyclic amide compounds as multiple kinase inhibitors