Nothing Special   »   [go: up one dir, main page]

SMT202300008T1 - Diaril macrociclici come modulatori di protein chinasi - Google Patents

Diaril macrociclici come modulatori di protein chinasi

Info

Publication number
SMT202300008T1
SMT202300008T1 SM20230008T SMT202300008T SMT202300008T1 SM T202300008 T1 SMT202300008 T1 SM T202300008T1 SM 20230008 T SM20230008 T SM 20230008T SM T202300008 T SMT202300008 T SM T202300008T SM T202300008 T1 SMT202300008 T1 SM T202300008T1
Authority
SM
San Marino
Prior art keywords
modulators
protein kinases
macrocycles
diaryl
diaryl macrocycles
Prior art date
Application number
SM20230008T
Other languages
English (en)
Inventor
Jingrong Jean Cui
Yishan Li
Evan W Rogers
Dayong Zhai
Original Assignee
Turning Point Therapeutics Inc
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 Turning Point Therapeutics Inc filed Critical Turning Point Therapeutics Inc
Publication of SMT202300008T1 publication Critical patent/SMT202300008T1/it

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
    • C07D498/12Heterocyclic 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
    • C07D498/18Bridged 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
SM20230008T 2014-01-24 2015-01-23 Diaril macrociclici come modulatori di protein chinasi SMT202300008T1 (it)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201461931506P 2014-01-24 2014-01-24
US201462049326P 2014-09-11 2014-09-11
US201562106301P 2015-01-22 2015-01-22
EP19169041.1A EP3572416B1 (en) 2014-01-24 2015-01-23 Diaryl macrocycles as modulators of protein kinases

Publications (1)

Publication Number Publication Date
SMT202300008T1 true SMT202300008T1 (it) 2023-03-17

Family

ID=53682127

Family Applications (3)

Application Number Title Priority Date Filing Date
SM20230008T SMT202300008T1 (it) 2014-01-24 2015-01-23 Diaril macrociclici come modulatori di protein chinasi
SM20190388T SMT201900388T1 (it) 2014-01-24 2015-01-23 Macrocicli diarilici come modulatori delle protein chinasi
SM20240175T SMT202400175T1 (it) 2014-01-24 2015-01-23 Macrocicli diarilici come modulatori di protein chinasi

Family Applications After (2)

Application Number Title Priority Date Filing Date
SM20190388T SMT201900388T1 (it) 2014-01-24 2015-01-23 Macrocicli diarilici come modulatori delle protein chinasi
SM20240175T SMT202400175T1 (it) 2014-01-24 2015-01-23 Macrocicli diarilici come modulatori di protein chinasi

Country Status (33)

Country Link
US (6) US9714258B2 (it)
EP (6) EP3636650A1 (it)
JP (5) JP6490713B2 (it)
KR (1) KR102402179B1 (it)
CN (3) CN110317213B (it)
AP (1) AP2016009383A0 (it)
AU (2) AU2015209239B2 (it)
CA (1) CA2936079C (it)
CL (1) CL2016001876A1 (it)
CY (1) CY1121850T1 (it)
DK (3) DK3636649T3 (it)
EA (2) EA031863B1 (it)
ES (3) ES2933350T3 (it)
FI (1) FI3636649T3 (it)
HK (1) HK1231407A1 (it)
HR (3) HRP20240503T1 (it)
HU (3) HUE066590T2 (it)
IL (2) IL246860B (it)
LT (3) LT3636649T (it)
MX (2) MX2016009588A (it)
MY (1) MY193524A (it)
NZ (2) NZ761094A (it)
PE (1) PE20160931A1 (it)
PH (1) PH12016501463B1 (it)
PL (3) PL3636649T3 (it)
PT (3) PT3572416T (it)
RS (3) RS65417B1 (it)
SG (2) SG10202000191YA (it)
SI (3) SI3572416T1 (it)
SM (3) SMT202300008T1 (it)
UA (1) UA121206C2 (it)
WO (1) WO2015112806A2 (it)
ZA (2) ZA201604654B (it)

Families Citing this family (88)

* 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
JP5600111B2 (ja) 2008-10-22 2014-10-01 アレイ バイオファーマ、インコーポレイテッド TRKキナーゼ阻害剤としての置換ピラゾロ[1,5−a]ピリミジン化合物
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
CN110003209B (zh) 2010-05-20 2022-01-25 阵列生物制药公司 作为trk激酶抑制剂的大环化合物
SMT202300008T1 (it) * 2014-01-24 2023-03-17 Turning Point Therapeutics Inc Diaril macrociclici come modulatori di protein chinasi
US10799505B2 (en) 2014-11-16 2020-10-13 Array Biopharma, Inc. Crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-A]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
US10758525B2 (en) 2015-01-22 2020-09-01 MyoKardia, Inc. 4-methylsulfonyl-substituted piperidine urea compounds
MA41667A1 (fr) 2015-06-01 2018-08-31 Loxo Oncology Inc Procede de diagnostic et de traitement du cancer
ES2864839T3 (es) * 2015-07-02 2021-10-14 Turning Point Therapeutics Inc Macrociclos de diarilo quirales como moduladores de proteína quinasas
RU2765181C2 (ru) 2015-07-06 2022-01-26 Тёрнинг Поинт Терапьютикс, Инк. Полиморфная форма диарильного макроцикла
US10023570B2 (en) 2015-07-16 2018-07-17 Array Biopharma Inc. Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors
FI3733187T3 (fi) 2015-07-21 2024-12-18 Turning Point Therapeutics Inc Kiraalinen diaryylimakrosykli ja sen käyttö syövän hoidossa
MX2018005087A (es) 2015-10-26 2019-05-16 Loxo Oncology Inc Mutaciones puntuales en cáncer resistente a trk y métodos relacionados con las mismas.
WO2017106505A1 (en) * 2015-12-15 2017-06-22 University Of South Florida Gas5 binding compounds, formulations, and uses thereof
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
SI3439662T1 (sl) 2016-04-04 2024-11-29 Loxo Oncology, Inc. Tekoče formulacije (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin -1-il)-pirazološ1,5-aćpirimidin-3-il)-3-hidroksipirolidin-1-karboksamida
HRP20241295T1 (hr) 2016-04-04 2024-12-06 Loxo Oncology, Inc. Postupci za liječenje pedijatrijskih karcinoma
HRP20230704T1 (hr) 2016-05-18 2023-10-27 Loxo Oncology, Inc. Priprava (s)-n-(5-((r)-2-(2,5-difluorfenil)pirolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida
WO2018022911A1 (en) * 2016-07-28 2018-02-01 Tp Therapeutics, Inc. Macrocycle kinase inhibitors
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
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
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
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
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
EP3700576A1 (en) 2017-10-26 2020-09-02 Array Biopharma Inc. Formulations of a macrocyclic trk kinase inhibitor
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
AU2018364938B2 (en) * 2017-11-10 2021-11-11 Angex Pharmaceutical, Inc. Macrocyclic compounds as TRK kinase inhibitors and uses thereof
WO2019126122A1 (en) 2017-12-19 2019-06-27 Tp Therapeutics, Inc. Macrocyclic kinase inhibitors and their use
MX2020006490A (es) 2017-12-19 2020-08-17 Turning Point Therapeutics Inc Compuestos macrociclicos para tratar enfermedades.
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
US11524963B2 (en) 2018-01-18 2022-12-13 Array Biopharma Inc. Substituted pyrazolo[3,4-d]pyrimidines as RET kinase inhibitors
CN111615514B (zh) 2018-01-18 2022-10-11 奥瑞生物药品公司 作为ret激酶抑制剂的取代的吡唑并[4,3-c]吡啶化合物
TWI802635B (zh) 2018-01-18 2023-05-21 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咯并[2,3-d]嘧啶化合物
US11345703B2 (en) 2018-01-23 2022-05-31 Shenzhen Targetrx, Inc. Substituted pyrazolo[1,5-a]pyrimidine macrocyclic compound
WO2019149131A1 (zh) * 2018-01-30 2019-08-08 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
CN110156813B (zh) * 2018-02-13 2023-07-25 北京诺诚健华医药科技有限公司 作为trk抑制剂的杂环化合物
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
MA52218A (fr) 2018-03-29 2021-02-17 Loxo Oncology Inc Traitement de cancers associés à trk
CN110386944B (zh) * 2018-04-16 2021-10-29 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白激酶活性的二(杂)芳基大环化合物
CN111902417B (zh) * 2018-04-25 2023-07-28 北京普祺医药科技股份有限公司 一种二芳基巨环化合物、药物组合物以及其用途
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
CN110627812B (zh) 2018-06-25 2022-10-11 北京诺诚健华医药科技有限公司 作为trk抑制剂的杂环化合物
KR102612513B1 (ko) 2018-07-31 2023-12-12 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
CA3111984A1 (en) 2018-09-10 2020-03-19 Array Biopharma Inc. Fused heterocyclic compounds as ret kinase inhibitors
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
EP3870579B1 (en) 2018-10-22 2024-10-02 Alumis Inc. Tyk2 inhibitors and uses thereof
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
JP7190036B2 (ja) * 2018-11-09 2022-12-14 シャントン、シュアンチュー、ファーマ、カンパニー、リミテッド 大環状チロシンキナーゼ阻害剤及びその用途
CA3119638A1 (en) * 2018-11-19 2020-05-28 Dana-Farber Cancer Institute, Inc. Macrocyclic inhibitors of dyrk1a
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
CN113490666A (zh) 2018-12-19 2021-10-08 奥瑞生物药品公司 作为fgfr酪氨酸激酶的抑制剂的取代的吡唑并[1,5-a]吡啶化合物
CN111592541B (zh) * 2019-02-21 2021-09-10 山东轩竹医药科技有限公司 大环类激酶抑制剂及其用途
WO2020185755A1 (en) * 2019-03-11 2020-09-17 Fronthera U.S. Pharmaceuticals Llc Tyk2 inhibitors and uses thereof
AU2020247990A1 (en) 2019-03-26 2021-11-11 Ventyx Biosciences, Inc. TYK2 pseudokinase ligands
JP7318009B2 (ja) * 2019-05-21 2023-07-31 浙江海正薬業股▲ふん▼有限公司 マクロライド誘導体、その製造方法および用途
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
PE20220135A1 (es) * 2019-06-19 2022-01-27 Turning Point Therapeutics Inc Polimorfos de un inhibidor de cinasas macrociclicas
CN113773335B (zh) * 2019-06-21 2024-12-03 成都海博为药业有限公司 一种作为蛋白质激酶抑制剂的化合物及其制备方法和用途
MA56505A (fr) * 2019-06-21 2022-04-27 Janssen Pharmaceutica Nv Inhibiteurs macrocycliques de mcl-1
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
CN114423762B (zh) * 2019-09-30 2024-03-29 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
MX2022006366A (es) 2019-11-27 2022-06-22 Turning Point Therapeutics Inc Terapia de combinacion que implica compuestos de diarilo macrociclico.
IL293206A (en) * 2019-11-27 2022-07-01 Turning Point Therapeutics Inc Combination therapy involving diaryl macrocyclic compounds
AU2020395136A1 (en) 2019-12-03 2022-07-07 Turning Point Therapeutics, Inc. Macrocycles for use in treating disease
WO2021113492A1 (en) 2019-12-06 2021-06-10 Schrödinger, Inc. Cyclic compounds and methods of using same
CN113045587A (zh) * 2019-12-27 2021-06-29 成都倍特药业股份有限公司 一种大环结构化合物的晶型及其制备方法
PH12022551523A1 (en) 2019-12-27 2024-01-29 Schra–Dinger Inc Cyclic compounds and methods of using same
CN113135938B (zh) * 2020-01-19 2022-06-14 山东轩竹医药科技有限公司 取代的大环类酪氨酸激酶抑制剂及其用途
BR112022017425A2 (pt) * 2020-03-02 2022-11-29 Turning Point Therapeutics Inc Usos terapêuticos de compostos macrocíclicos
PE20230609A1 (es) * 2020-05-04 2023-04-13 Amgen Inc Compuestos heterociclicos como agonistas del receptor de activacion expresado en las celulas mieloides 2 y metodos de uso
CN113620974B (zh) * 2020-05-08 2023-01-31 山东轩竹医药科技有限公司 大环类酪氨酸激酶抑制剂的晶型及其制备方法
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
CA3187834A1 (en) * 2020-07-10 2022-01-13 Blossomhill Therapeutics, Inc. Macrocycles and their use
CN116490507A (zh) 2020-09-10 2023-07-25 薛定谔公司 用于治疗癌症的杂环包缩合cdc7激酶抑制剂
JP2024505890A (ja) 2021-01-26 2024-02-08 シュレーディンガー, インコーポレイテッド がん、自己免疫及び炎症性障害の治療に有用な三環式化合物
WO2022182845A1 (en) * 2021-02-25 2022-09-01 Blossomhill Therapeutics, Inc. Macrocycles and their use
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
WO2023078267A1 (zh) * 2021-11-02 2023-05-11 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
IL314070A (en) * 2022-01-05 2024-09-01 Blossomhill Therapeutics Inc Macrocyclic compounds and use as kinase inhibitors
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 (55)

* 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.
EP0690843B1 (en) 1993-03-25 2000-08-30 PHARMACIA & UPJOHN COMPANY Formyl- or cyano- substituted indole derivatives having dopaminergic activity
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
EP1325008B1 (en) 2000-07-31 2005-10-05 F. Hoffmann-La Roche Ag Piperazine derivatives
CA2441080A1 (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
US7550470B2 (en) 2002-12-11 2009-06-23 Merck & Co. Inc. Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors
JP5749645B2 (ja) * 2008-09-08 2015-07-15 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung タンパク質キナーゼ阻害剤としての大環状ピリミジン
US8450322B2 (en) 2008-09-22 2013-05-28 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds as Trk kinase inhibitors
JP5600111B2 (ja) 2008-10-22 2014-10-01 アレイ バイオファーマ、インコーポレイテッド TRKキナーゼ阻害剤としての置換ピラゾロ[1,5−a]ピリミジン化合物
SG194397A1 (en) 2008-10-31 2013-11-29 Genentech Inc Pyrazolopyrimidine jak inhibitor compounds and methods
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
US20110029480A1 (en) * 2009-08-03 2011-02-03 IntelliCubes, Inc. Method of Compiling Multiple Data Sources into One Dataset
WO2011071725A1 (en) 2009-12-07 2011-06-16 Boehringer Ingelheim International Gmbh Heterocyclic compounds containing a pyrrolopyridine or benzimidazole core
EP2509980A1 (en) 2009-12-07 2012-10-17 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
CN110003209B (zh) * 2010-05-20 2022-01-25 阵列生物制药公司 作为trk激酶抑制剂的大环化合物
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
JP2014524442A (ja) 2011-08-19 2014-09-22 メルク・シャープ・アンド・ドーム・コーポレーション Hcvプロテアーゼ阻害剤の結晶形態
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
HUE027318T2 (en) 2011-09-30 2016-10-28 Oncodesign Sa Macrocyclic FLT3 kinase inhibitors
CA2852936A1 (en) 2011-10-20 2013-04-25 Glaxosmithkline Llc Substituted bicyclic aza-heterocycles and analogues as sirtuin modulators
DK2822953T5 (en) 2012-03-06 2017-09-11 Pfizer Macrocyclic derivatives for the treatment of proliferative diseases
AU2013230119B2 (en) * 2012-03-09 2017-02-23 Lexicon Pharmaceuticals, Inc. Imidazo [1, 2 - b] pyridazine - based compounds, compositions comprising them, and uses thereof
ES2676224T3 (es) 2012-03-09 2018-07-17 Lexicon Pharmaceuticals, Inc. Compuestos a base de pirazolo[1,5-a]pirimidina, composiciones que los comprenden y métodos para usarlos
GB201205669D0 (en) 2012-03-30 2012-05-16 Agency Science Tech & Res Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof
EP2951174B1 (en) 2013-01-30 2017-04-26 Bayer Pharma Aktiengesellschaft Amino-substituted isothiazoles
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
WO2015073267A1 (en) 2013-11-15 2015-05-21 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
SMT202300008T1 (it) 2014-01-24 2023-03-17 Turning Point Therapeutics Inc Diaril macrociclici come modulatori di protein chinasi
WO2016070241A1 (en) 2014-11-03 2016-05-12 Ctxt Pty Ltd Triazine compounds, compositions and synthesis
US9701681B2 (en) 2014-12-15 2017-07-11 Cmg Pharmaceutical Co., Ltd. Fused ring heteroaryl compounds and their use as Trk inhibitors
EP3259264B1 (en) 2015-02-20 2022-07-27 Rigel Pharmaceuticals, Inc. Gdf-8 inhibitors
EP3267996B1 (en) 2015-03-12 2020-11-11 Merck Sharp & Dohme Corp. Pyrazolopyrimidine inhibitors of irak4 activity
US10155765B2 (en) 2015-03-12 2018-12-18 Merck Sharp & Dohme Corp. Carboxamide inhibitors of IRAK4 activity
TN2017000467A1 (en) 2015-05-05 2019-04-12 Bayer Pharma AG Amido-substituted cyclohexane derivatives
ES2864839T3 (es) 2015-07-02 2021-10-14 Turning Point Therapeutics Inc Macrociclos de diarilo quirales como moduladores de proteína quinasas
RU2765181C2 (ru) 2015-07-06 2022-01-26 Тёрнинг Поинт Терапьютикс, Инк. Полиморфная форма диарильного макроцикла
FI3733187T3 (fi) 2015-07-21 2024-12-18 Turning Point Therapeutics Inc Kiraalinen diaryylimakrosykli ja sen käyttö syövän hoidossa
MX2018005087A (es) 2015-10-26 2019-05-16 Loxo Oncology Inc Mutaciones puntuales en cáncer resistente a trk y métodos relacionados con las mismas.
BR112018067775B1 (pt) 2016-03-04 2024-02-15 Vanderbilt University Compostos inibidores de mcl-1 indol substituídos, composição farmacêutica compreendendo ditos compostos e usos terapêuticos dos mesmos
WO2018022911A1 (en) 2016-07-28 2018-02-01 Tp Therapeutics, Inc. Macrocycle kinase inhibitors
WO2018112027A1 (en) 2016-12-14 2018-06-21 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
PE20160931A1 (es) 2016-09-21
EP3097107A4 (en) 2017-08-09
RS63829B1 (sr) 2023-01-31
US20190169207A1 (en) 2019-06-06
EP3572416A1 (en) 2019-11-27
US20170334929A1 (en) 2017-11-23
UA121206C2 (uk) 2020-04-27
JP2019104748A (ja) 2019-06-27
CN106170289B (zh) 2019-07-23
LT3097107T (lt) 2019-07-25
HK1231407A1 (zh) 2017-12-22
AU2015209239A1 (en) 2016-07-14
SI3097107T1 (sl) 2019-08-30
US20240140964A1 (en) 2024-05-02
MX2020001360A (es) 2020-03-20
DK3572416T3 (da) 2022-12-12
KR102402179B1 (ko) 2022-05-25
JP2017503867A (ja) 2017-02-02
US10246466B2 (en) 2019-04-02
AU2019279951B2 (en) 2021-08-12
SI3572416T1 (sl) 2023-02-28
PH12016501463A1 (en) 2017-02-06
JP2021063121A (ja) 2021-04-22
SMT201900388T1 (it) 2019-09-09
US10618912B2 (en) 2020-04-14
US20170002023A1 (en) 2017-01-05
CA2936079A1 (en) 2015-07-30
KR20160111395A (ko) 2016-09-26
EP3097107B1 (en) 2019-04-17
IL246860A0 (en) 2016-08-31
PT3097107T (pt) 2019-07-19
CN110317214B (zh) 2022-11-22
JP6490713B2 (ja) 2019-03-27
PT3636649T (pt) 2024-04-09
EP4338739A2 (en) 2024-03-20
HRP20240503T1 (hr) 2024-07-05
IL246860B (en) 2019-09-26
ES2933350T3 (es) 2023-02-06
CN106170289A (zh) 2016-11-30
NZ761094A (en) 2023-02-24
CN110317213A (zh) 2019-10-11
SMT202400175T1 (it) 2024-07-09
AP2016009383A0 (en) 2016-08-31
US20220112213A1 (en) 2022-04-14
WO2015112806A2 (en) 2015-07-30
HRP20221518T1 (hr) 2023-02-17
CA2936079C (en) 2022-07-19
US20200216465A1 (en) 2020-07-09
ZA202004100B (en) 2023-12-20
EP3572416B1 (en) 2022-09-21
EP3636650A1 (en) 2020-04-15
EP3636648A1 (en) 2020-04-15
EA031863B1 (ru) 2019-03-29
CL2016001876A1 (es) 2017-02-03
DK3636649T3 (da) 2024-05-21
DK3097107T3 (da) 2019-07-08
PH12016501463B1 (en) 2017-02-06
HUE066590T2 (hu) 2024-08-28
PL3636649T3 (pl) 2024-05-06
HUE060554T2 (hu) 2023-03-28
LT3636649T (lt) 2024-04-10
EP4338739A3 (en) 2024-05-29
ZA201604654B (en) 2020-10-28
IL268820B (en) 2021-10-31
EA201691492A1 (ru) 2017-06-30
CN110317214A (zh) 2019-10-11
WO2015112806A3 (en) 2015-11-12
HUE045208T2 (hu) 2019-12-30
HRP20191283T1 (hr) 2019-10-18
MX2016009588A (es) 2017-05-15
SI3636649T1 (sl) 2024-07-31
CY1121850T1 (el) 2020-07-31
IL268820A (en) 2019-10-31
EA201892241A1 (ru) 2019-02-28
JP2023179539A (ja) 2023-12-19
ES2735729T3 (es) 2019-12-20
PL3097107T3 (pl) 2020-01-31
RS65417B1 (sr) 2024-05-31
SG11201605929RA (en) 2016-08-30
LT3572416T (lt) 2022-12-27
FI3636649T3 (fi) 2024-05-02
JP7356546B2 (ja) 2023-10-04
NZ722375A (en) 2022-11-25
PT3572416T (pt) 2022-12-06
EP3636649B1 (en) 2024-02-14
PL3572416T3 (pl) 2023-02-27
AU2015209239B2 (en) 2019-09-12
CN110317213B (zh) 2022-10-18
RS59059B1 (sr) 2019-08-30
ES2976459T3 (es) 2024-08-01
EP3097107A2 (en) 2016-11-30
US9714258B2 (en) 2017-07-25
SG10202000191YA (en) 2020-03-30
MY193524A (en) 2022-10-18
EP3636649A1 (en) 2020-04-15
AU2019279951A1 (en) 2020-01-16
JP2022133462A (ja) 2022-09-13

Similar Documents

Publication Publication Date Title
HK1231407A1 (zh) 作為蛋白質激酶的調節劑的二芳基巨環
IL256377A (en) Diaryl chiral macrocycles as protein kinase modulators
IL283582A (en) ror - gamma modulators
IL280905A (en) Use of erythrohydroxybibopropion to increase drug level in plasma
HK1256599A1 (zh) ROR-γ的調節劑
IL247234A0 (en) Caspase-6 modulators
SG11201607445QA (en) Methods of modulating wars2
PT3377106T (pt) Modulação da ciliogénese
GB201418230D0 (en) Construction of surfaces