LT3636649T - Diarilo makrociklai kaip proteinkinazių moduliatoriai - Google Patents

Diarilo makrociklai kaip proteinkinazių moduliatoriai

Info

Publication number
LT3636649T
LT3636649T LTEP19212110.1T LT19212110T LT3636649T LT 3636649 T LT3636649 T LT 3636649T LT 19212110 T LT19212110 T LT 19212110T LT 3636649 T LT3636649 T LT 3636649T
Authority
LT
Lithuania
Prior art keywords
modulators
protein kinases
macrocycles
diaryl
diaryl macrocycles
Prior art date
Application number
LTEP19212110.1T
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 LT3636649T publication Critical patent/LT3636649T/lt

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)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
LTEP19212110.1T 2014-01-24 2015-01-23 Diarilo makrociklai kaip proteinkinazių moduliatoriai LT3636649T (lt)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
LT3636649T true LT3636649T (lt) 2024-04-10

Family

ID=53682127

Family Applications (3)

Application Number Title Priority Date Filing Date
LTEP15740510.1T LT3097107T (lt) 2014-01-24 2015-01-23 Diarilo makrociklai, kaip proteinkinazių moduliatoriai
LTEP19169041.1T LT3572416T (lt) 2014-01-24 2015-01-23 Diarilo makrociklai, kaip baltymų kinazių moduliatoriai
LTEP19212110.1T LT3636649T (lt) 2014-01-24 2015-01-23 Diarilo makrociklai kaip proteinkinazių moduliatoriai

Family Applications Before (2)

Application Number Title Priority Date Filing Date
LTEP15740510.1T LT3097107T (lt) 2014-01-24 2015-01-23 Diarilo makrociklai, kaip proteinkinazių moduliatoriai
LTEP19169041.1T LT3572416T (lt) 2014-01-24 2015-01-23 Diarilo makrociklai, kaip baltymų kinazių moduliatoriai

Country Status (32)

Country Link
US (6) US9714258B2 (lt)
EP (6) EP3097107B1 (lt)
JP (5) JP6490713B2 (lt)
KR (1) KR102402179B1 (lt)
CN (3) CN106170289B (lt)
AP (1) AP2016009383A0 (lt)
AU (2) AU2015209239B2 (lt)
CA (1) CA2936079C (lt)
CL (1) CL2016001876A1 (lt)
CY (1) CY1121850T1 (lt)
DK (3) DK3572416T3 (lt)
EA (2) EA201892241A1 (lt)
ES (3) ES2933350T3 (lt)
FI (1) FI3636649T3 (lt)
HK (1) HK1231407A1 (lt)
HR (3) HRP20221518T1 (lt)
HU (3) HUE066590T2 (lt)
IL (2) IL246860B (lt)
LT (3) LT3097107T (lt)
MX (2) MX2016009588A (lt)
MY (1) MY193524A (lt)
NZ (2) NZ761094A (lt)
PE (1) PE20160931A1 (lt)
PH (1) PH12016501463A1 (lt)
PL (3) PL3097107T3 (lt)
PT (3) PT3636649T (lt)
RS (3) RS65417B1 (lt)
SG (2) SG11201605929RA (lt)
SI (3) SI3097107T1 (lt)
UA (1) UA121206C2 (lt)
WO (1) WO2015112806A2 (lt)
ZA (2) ZA201604654B (lt)

Families Citing this family (86)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2350075T3 (pl) 2008-09-22 2014-07-31 Array Biopharma Inc Podstawione związki imidazo[1,2b]pirydazynowe jako inhibitory kinaz Trk
BRPI0919873B8 (pt) 2008-10-22 2021-05-25 Array Biopharma Inc compostos de pirazol[1,5-a]pirimidina substituídos como inibidores da trk quinase, seus processos de preparação e composições farmacêuticas
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
LT3205654T (lt) 2010-05-20 2019-05-27 Array Biopharma, Inc. Makrocikliniai junginiai kaip trk kinazės slopikliai
HRP20221518T1 (hr) 2014-01-24 2023-02-17 Turning Point Therapeutics, Inc. Diaril makrociklični spojevi kao modulatori protein kinaza
PL3699181T3 (pl) 2014-11-16 2023-05-22 Array Biopharma, Inc. Postać krystaliczna wodorosiarczanu (s)-n-(5-((r)-2-(2,5-difluorofenylo) - pirolidyn-1-ylo)-pirazolo[1,5-a]pirimidyn-3-ylo)-3-hydroksypirolidyno-1-karboksyamidu
US10758525B2 (en) 2015-01-22 2020-09-01 MyoKardia, Inc. 4-methylsulfonyl-substituted piperidine urea compounds
EP3303631A1 (en) 2015-06-01 2018-04-11 Loxo Oncology Inc. Methods of diagnosing and treating cancer
MX2017017097A (es) * 2015-07-02 2018-05-23 Tp Therapeutics Inc Macrociclos diarílicos quirales como moduladores de proteínas quinasas.
PT3319969T (pt) * 2015-07-06 2024-06-17 Turning Point Therapeutics Inc Polimorfo de macrociclo de diarilo
CA2992586A1 (en) 2015-07-16 2017-01-19 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
RU2020123800A (ru) * 2015-07-21 2020-10-02 Тёрнинг Поинт Терапьютикс, Инк. Хиральные диарильные макроциклы и их применение
EP3368039A1 (en) 2015-10-26 2018-09-05 The Regents of The University of Colorado, A Body Corporate Point mutations in trk inhibitor-resistant cancer and methods relating to the same
US11278521B2 (en) 2015-12-15 2022-03-22 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
GEP20227339B (en) 2016-04-04 2022-01-25 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-hydro-xypyrrolidine-1-carboxamide
EP3439663B1 (en) 2016-04-04 2024-07-17 Loxo Oncology, Inc. Methods of treating pediatric cancers
CA3024603A1 (en) 2016-05-18 2017-11-23 Charles Todd Eary Process for the preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide and salts thereof
BR112019001607A2 (pt) * 2016-07-28 2019-04-30 Tp Therapeutics, Inc. inibidores macrocíclicos de quinases
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
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
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
WO2018136661A1 (en) 2017-01-18 2018-07-26 Andrews Steven W SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS
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
PT3658148T (pt) 2017-07-28 2024-08-26 Turning Point Therapeutics Inc Compostos macrocíclicos e utilizações dos mesmos
TW202410896A (zh) 2017-10-10 2024-03-16 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
MA50456A (fr) 2017-10-26 2020-09-02 Array Biopharma Inc Formulations d'un inhibiteur de kinase trk macrocyclique
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
TW201927790A (zh) * 2017-11-10 2019-07-16 美商安捷克斯製藥公司 作為trk激酶抑制劑之巨環化合物及其用途
EP3728270A4 (en) 2017-12-19 2021-06-23 Turning Point Therapeutics, Inc. MACROCYCLIC KINASE INHIBITORS AND THEIR USES
MX2020006490A (es) 2017-12-19 2020-08-17 Turning Point Therapeutics Inc Compuestos macrociclicos para tratar enfermedades.
WO2019120194A1 (zh) * 2017-12-22 2019-06-27 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
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
CA3087972C (en) 2018-01-18 2023-01-10 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
WO2019143991A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS
WO2019144885A1 (zh) * 2018-01-23 2019-08-01 深圳市塔吉瑞生物医药有限公司 取代的吡唑并[1,5-a]嘧啶类的大环化合物
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
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
AU2019241260B2 (en) * 2018-03-28 2022-06-16 Fochon Biosciences, Ltd. Macrocyclic compounds as TRK kinases inhibitors
CA3095366A1 (en) 2018-03-29 2019-10-03 Loxo Oncology, Inc. Treatment of trk-associated cancers
JP7092405B2 (ja) * 2018-04-16 2022-06-28 深▲チェン▼市塔吉瑞生物医薬有限公司 キナーゼ活性を阻害するためのジ(ヘテロ)アリール大環状化合物
EP3786167B1 (en) * 2018-04-25 2024-08-21 Primegene (Beijing) Co., Ltd. Diaryl macrocyclic compound and pharmaceutical composition, and use thereof
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
KR102653681B1 (ko) 2018-07-31 2024-04-03 록쏘 온콜로지, 인코포레이티드 (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의분무-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
CN112955453B (zh) * 2018-09-29 2022-04-19 山东绿叶制药有限公司 作为选择性Trk抑制剂的吡唑并嘧啶衍生物
AU2019364336B2 (en) 2018-10-22 2023-11-16 Alumis Inc. TYK2 inhibitors and uses thereof
CN113166155A (zh) * 2018-11-09 2021-07-23 山东轩竹医药科技有限公司 大环类酪氨酸激酶抑制剂及其用途
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
WO2020106685A1 (en) * 2018-11-19 2020-05-28 Dana-Farber Cancer Institute, Inc. Macrocyclic inhibitors of dyrk1a
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
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
BR112021017996A2 (pt) * 2019-03-11 2021-11-16 Esker Therapeutics Inc Inibidores de tyk2 e seus usos
CN113727984B (zh) * 2019-05-21 2024-03-15 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
WO2020257189A1 (en) * 2019-06-19 2020-12-24 Turning Point Therapeutics, Inc. Macrocycles for treating disease
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
ES2975083T3 (es) * 2019-06-21 2024-07-03 Janssen Pharmaceutica Nv Inhibidores macrocíclicos de MCL-1
CN113773335A (zh) * 2019-06-21 2021-12-10 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
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
WO2021063276A1 (zh) * 2019-09-30 2021-04-08 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
AU2020391222A1 (en) 2019-11-27 2022-06-30 Turning Point Therapeutics, Inc. Combination therapy involving diaryl macrocyclic compounds
EP4065395A4 (en) 2019-11-27 2024-02-14 Turning Point Therapeutics, Inc. COMBINATION THERAPY WITH DIARYL MACROCYCLIC COMPOUNDS
KR20220133869A (ko) 2019-12-03 2022-10-05 터닝 포인트 테라퓨틱스, 인크. 질환 치료에 사용하기 위한 거대고리
EP4069369A4 (en) 2019-12-06 2024-02-14 Schrödinger, Inc. CYCLIC COMPOUNDS AND METHODS OF USE THEREOF
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
CA3161339A1 (en) 2019-12-27 2021-07-01 Schrodinger, 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
EP4114530A4 (en) * 2020-03-02 2024-04-17 Turning Point Therapeutics, Inc. THERAPEUTIC USES OF MACROCYCLIC COMPOUNDS
EP4148055A4 (en) * 2020-05-08 2023-10-11 Shandong Xuanzhu Pharma Co., Ltd. CRYSTAL FORM OF A MACROCYCLIC TYROSINE KINASE INHIBITOR AND PROCESS FOR PRODUCTION THEREOF
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
IL299732A (en) * 2020-07-10 2023-03-01 Blossomhill Therapeutics Inc Macrocycles and their use
WO2022055963A1 (en) 2020-09-10 2022-03-17 Schrödinger, Inc. Heterocyclic pericondensed cdc7 kinase inhibitors for the treatment of cancer
US20240148732A1 (en) 2021-01-26 2024-05-09 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders
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
CN116063326A (zh) * 2021-11-02 2023-05-05 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
WO2023133375A1 (en) * 2022-01-05 2023-07-13 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
AU8395501A (en) 2000-07-31 2002-02-13 Hoffmann La Roche Piperazine derivatives
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
MX2011002470A (es) 2008-09-08 2011-04-05 Merck Patent Gmbh Pirimidinas macrociclicas como inhibidores de aurora cinasa.
PL2350075T3 (pl) 2008-09-22 2014-07-31 Array Biopharma Inc Podstawione związki imidazo[1,2b]pirydazynowe jako inhibitory kinaz Trk
BRPI0919873B8 (pt) 2008-10-22 2021-05-25 Array Biopharma Inc compostos de pirazol[1,5-a]pirimidina substituídos como inibidores da trk quinase, seus processos de preparação e composições farmacêuticas
AU2009308675A1 (en) 2008-10-31 2010-05-06 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
US9150577B2 (en) 2009-12-07 2015-10-06 Boehringer Ingelheim International Gmbh Heterocyclic compounds containing an indole core
EP2509979B1 (en) 2009-12-07 2016-05-25 Boehringer Ingelheim International GmbH Heterocyclic compounds containing a pyrrolopyridine or benzimidazole core
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
LT3205654T (lt) 2010-05-20 2019-05-27 Array Biopharma, Inc. Makrocikliniai junginiai kaip trk kinazės slopikliai
US8637516B2 (en) 2010-09-09 2014-01-28 Irm Llc Compounds and compositions as TRK inhibitors
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
EP2744331A4 (en) 2011-08-19 2015-01-21 Merck Sharp & Dohme METHOD AND INTERMEDIATE PRODUCTS FOR THE MANUFACTURE OF MACROLACTAMEN
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
AU2012325909B2 (en) 2011-10-20 2016-06-09 Glaxosmithkline Llc Substituted bicyclic aza-heterocycles and analogues as sirtuin modulators
LT2822953T (lt) * 2012-03-06 2017-04-10 Pfizer Inc. Makrocikliniai dariniai, skirti proliferacinių ligų gydymui
ES2676826T3 (es) * 2012-03-09 2018-07-25 Lexicon Pharmaceuticals, Inc. Compuestos basados en imidazo[1,2-b]piridazina, composiciones que los comprenden y usos de los mismos
NZ630721A (en) 2012-03-09 2016-12-23 Lexicon Pharmaceuticals Inc Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use
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
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
WO2015012328A1 (ja) 2013-07-24 2015-01-29 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
HRP20221518T1 (hr) 2014-01-24 2023-02-17 Turning Point Therapeutics, Inc. Diaril makrociklični spojevi kao modulatori protein kinaza
WO2016070241A1 (en) 2014-11-03 2016-05-12 Ctxt Pty Ltd Triazine compounds, compositions and synthesis
EP4420732A2 (en) 2014-12-15 2024-08-28 CMG Pharmaceutical Co., Ltd. Fused ring heteroaryl compounds and their use as trk inhibitors
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
MX2017017097A (es) 2015-07-02 2018-05-23 Tp Therapeutics Inc Macrociclos diarílicos quirales como moduladores de proteínas quinasas.
PT3319969T (pt) 2015-07-06 2024-06-17 Turning Point Therapeutics Inc Polimorfo de macrociclo de diarilo
RU2020123800A (ru) 2015-07-21 2020-10-02 Тёрнинг Поинт Терапьютикс, Инк. Хиральные диарильные макроциклы и их применение
EP3368039A1 (en) 2015-10-26 2018-09-05 The Regents of The University of Colorado, A Body Corporate 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
BR112019001607A2 (pt) 2016-07-28 2019-04-30 Tp Therapeutics, Inc. inibidores macrocíclicos de quinases
EP3555137A1 (en) 2016-12-14 2019-10-23 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
PT3658148T (pt) 2017-07-28 2024-08-26 Turning Point Therapeutics Inc Compostos macrocíclicos e utilizações dos mesmos

Also Published As

Publication number Publication date
CY1121850T1 (el) 2020-07-31
CN110317214A (zh) 2019-10-11
NZ761094A (en) 2023-02-24
MX2020001360A (es) 2020-03-20
EP3572416B1 (en) 2022-09-21
HRP20221518T1 (hr) 2023-02-17
EP3636649A1 (en) 2020-04-15
EP3572416A1 (en) 2019-11-27
HUE060554T2 (hu) 2023-03-28
AU2015209239B2 (en) 2019-09-12
JP7356546B2 (ja) 2023-10-04
RS65417B1 (sr) 2024-05-31
PT3572416T (pt) 2022-12-06
HRP20191283T1 (hr) 2019-10-18
IL268820B (en) 2021-10-31
HUE066590T2 (hu) 2024-08-28
AU2019279951B2 (en) 2021-08-12
JP2022133462A (ja) 2022-09-13
HUE045208T2 (hu) 2019-12-30
US20200216465A1 (en) 2020-07-09
PT3097107T (pt) 2019-07-19
ZA201604654B (en) 2020-10-28
CN110317213B (zh) 2022-10-18
PL3572416T3 (pl) 2023-02-27
EP3636649B1 (en) 2024-02-14
MY193524A (en) 2022-10-18
ES2976459T3 (es) 2024-08-01
US20170334929A1 (en) 2017-11-23
US10246466B2 (en) 2019-04-02
EA201892241A1 (ru) 2019-02-28
PH12016501463B1 (en) 2017-02-06
CL2016001876A1 (es) 2017-02-03
KR20160111395A (ko) 2016-09-26
US20220112213A1 (en) 2022-04-14
EP3636648A1 (en) 2020-04-15
US20170002023A1 (en) 2017-01-05
EP4338739A2 (en) 2024-03-20
RS63829B1 (sr) 2023-01-31
LT3097107T (lt) 2019-07-25
US20240140964A1 (en) 2024-05-02
ES2933350T3 (es) 2023-02-06
HK1231407A1 (zh) 2017-12-22
CA2936079C (en) 2022-07-19
JP6490713B2 (ja) 2019-03-27
UA121206C2 (uk) 2020-04-27
AP2016009383A0 (en) 2016-08-31
EA031863B1 (ru) 2019-03-29
PE20160931A1 (es) 2016-09-21
US9714258B2 (en) 2017-07-25
SG11201605929RA (en) 2016-08-30
CN106170289B (zh) 2019-07-23
LT3572416T (lt) 2022-12-27
WO2015112806A2 (en) 2015-07-30
JP2017503867A (ja) 2017-02-02
SI3572416T1 (sl) 2023-02-28
IL268820A (en) 2019-10-31
CN106170289A (zh) 2016-11-30
US10618912B2 (en) 2020-04-14
DK3572416T3 (da) 2022-12-12
ES2735729T3 (es) 2019-12-20
EP3097107B1 (en) 2019-04-17
SI3097107T1 (sl) 2019-08-30
CA2936079A1 (en) 2015-07-30
IL246860A0 (en) 2016-08-31
DK3097107T3 (da) 2019-07-08
JP2023179539A (ja) 2023-12-19
MX2016009588A (es) 2017-05-15
SI3636649T1 (sl) 2024-07-31
EP3097107A2 (en) 2016-11-30
PL3097107T3 (pl) 2020-01-31
RS59059B1 (sr) 2019-08-30
JP2019104748A (ja) 2019-06-27
WO2015112806A3 (en) 2015-11-12
IL246860B (en) 2019-09-26
EP3636650A1 (en) 2020-04-15
PL3636649T3 (pl) 2024-05-06
CN110317214B (zh) 2022-11-22
CN110317213A (zh) 2019-10-11
HRP20240503T1 (hr) 2024-07-05
NZ722375A (en) 2022-11-25
EP3097107A4 (en) 2017-08-09
US20190169207A1 (en) 2019-06-06
PH12016501463A1 (en) 2017-02-06
KR102402179B1 (ko) 2022-05-25
JP2021063121A (ja) 2021-04-22
DK3636649T3 (da) 2024-05-21
AU2019279951A1 (en) 2020-01-16
SG10202000191YA (en) 2020-03-30
EA201691492A1 (ru) 2017-06-30
PT3636649T (pt) 2024-04-09
AU2015209239A1 (en) 2016-07-14
EP4338739A3 (en) 2024-05-29
FI3636649T3 (fi) 2024-05-02
ZA202004100B (en) 2023-12-20

Similar Documents

Publication Publication Date Title
IL268820B (en) Diaryl macrocycles as protein kinase modulators
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