[go: up one dir, main page]

SG10202000191YA - Diaryl macrocycles as modulators of protein kinases - Google Patents

Diaryl macrocycles as modulators of protein kinases

Info

Publication number
SG10202000191YA
SG10202000191YA SG10202000191YA SG10202000191YA SG10202000191YA SG 10202000191Y A SG10202000191Y A SG 10202000191YA SG 10202000191Y A SG10202000191Y A SG 10202000191YA SG 10202000191Y A SG10202000191Y A SG 10202000191YA SG 10202000191Y A SG10202000191Y A SG 10202000191YA
Authority
SG
Singapore
Prior art keywords
modulators
protein kinases
macrocycles
diaryl
diaryl macrocycles
Prior art date
Application number
SG10202000191YA
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 SG10202000191YA publication Critical patent/SG10202000191YA/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic 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
    • C07D498/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (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)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
SG10202000191YA 2014-01-24 2015-01-23 Diaryl macrocycles as modulators of protein kinases SG10202000191YA (en)

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
SG10202000191YA true SG10202000191YA (en) 2020-03-30

Family

ID=53682127

Family Applications (2)

Application Number Title Priority Date Filing Date
SG10202000191YA SG10202000191YA (en) 2014-01-24 2015-01-23 Diaryl macrocycles as modulators of protein kinases
SG11201605929RA SG11201605929RA (en) 2014-01-24 2015-01-23 Diaryl macrocycles as modulators of protein kinases

Family Applications After (1)

Application Number Title Priority Date Filing Date
SG11201605929RA SG11201605929RA (en) 2014-01-24 2015-01-23 Diaryl macrocycles as modulators of protein kinases

Country Status (35)

Country Link
US (6) US9714258B2 (en)
EP (6) EP3636649B1 (en)
JP (5) JP6490713B2 (en)
KR (1) KR102402179B1 (en)
CN (3) CN110317214B (en)
AP (1) AP2016009383A0 (en)
AU (2) AU2015209239B2 (en)
CA (1) CA2936079C (en)
CL (1) CL2016001876A1 (en)
CY (1) CY1121850T1 (en)
DK (3) DK3636649T3 (en)
EA (2) EA201892241A1 (en)
ES (3) ES2976459T3 (en)
FI (2) FI3636649T3 (en)
FR (1) FR25C1013I1 (en)
HR (3) HRP20240503T1 (en)
HU (4) HUE060554T2 (en)
IL (2) IL246860B (en)
LT (3) LT3572416T (en)
MX (2) MX392904B (en)
MY (1) MY193524A (en)
NL (1) NL301322I2 (en)
NO (1) NO2025015I1 (en)
NZ (2) NZ722375A (en)
PE (1) PE20160931A1 (en)
PH (1) PH12016501463B1 (en)
PL (3) PL3636649T3 (en)
PT (3) PT3572416T (en)
RS (3) RS63829B1 (en)
SG (2) SG10202000191YA (en)
SI (3) SI3572416T1 (en)
SM (3) SMT201900388T1 (en)
UA (1) UA121206C2 (en)
WO (1) WO2015112806A2 (en)
ZA (2) ZA201604654B (en)

Families Citing this family (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2738026C (en) 2008-09-22 2017-01-24 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors
AU2009308465B2 (en) 2008-10-22 2015-02-12 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrimidine compounds as TRK kinase inhibitors
AR077468A1 (en) 2009-07-09 2011-08-31 Array Biopharma Inc PIRAZOLO COMPOUNDS (1,5-A) PYRIMIDINE SUBSTITUTED AS TRK-QUINASA INHIBITORS
DK2918588T3 (en) 2010-05-20 2017-08-28 Array Biopharma Inc Macrocyclic compounds as TRK kinase inhibitors
CN110317214B (en) 2014-01-24 2022-11-22 特普医药公司 Diaryl macrocycles as modulators of protein kinases
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
MA44936A1 (en) 2015-06-01 2021-09-30 Loxo Oncology Inc Methods of diagnosing and treating cancer
US10316044B2 (en) * 2015-07-02 2019-06-11 Tp Therapeutics, Inc. Chiral diaryl macrocycles as modulators of protein kinases
RU2765181C2 (en) * 2015-07-06 2022-01-26 Тёрнинг Поинт Терапьютикс, Инк. Polymorphic form of diaryl macrocycle
EA035049B1 (en) 2015-07-16 2020-04-22 Аррэй Байофарма Инк. SUBSTITUTED PYRAZOLO[1,5-a]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS
EP4480543A3 (en) * 2015-07-21 2025-02-12 Turning Point Therapeutics, Inc. Chiral diaryl macrocycle and use thereof in the treatment of cancer
KR20180102544A (en) 2015-10-26 2018-09-17 더 리전츠 오브 더 유니버시티 오브 콜로라도, 어 바디 코퍼레이트 TRK Inhibitors - Point Mutation in Resistant Cancer and Related Methods
WO2017106505A1 (en) * 2015-12-15 2017-06-22 University Of South Florida Gas5 binding compounds, formulations, and uses thereof
NZ747135A (en) 2016-04-04 2025-05-02 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
PL3439663T3 (en) 2016-04-04 2024-11-18 Loxo Oncology, Inc. Methods of treating pediatric cancers
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
RS61463B1 (en) 2016-05-18 2021-03-31 Loxo Oncology Inc Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
CN109715165A (en) 2016-07-28 2019-05-03 Tp生物医药公司 Huge ring kinase inhibitor
JOP20190077A1 (en) 2016-10-10 2019-04-09 Array Biopharma Inc Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
TWI704148B (en) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
JOP20190092A1 (en) 2016-10-26 2019-04-25 Array Biopharma Inc PROCESS FOR THE PREPARATION OF PYRAZOLO[1,5-a]PYRIMIDINES AND SALTS THEREOF
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
US11168090B2 (en) 2017-01-18 2021-11-09 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors
TWI808958B (en) * 2017-01-25 2023-07-21 美商特普醫葯公司 Combination therapy involving diaryl macrocyclic compounds
JOP20190213A1 (en) 2017-03-16 2019-09-16 Array Biopharma Inc Macrocyclic compounds as ros1 kinase inhibitors
CN107586796B (en) * 2017-07-20 2021-08-06 暨明医药科技（苏州）有限公司 Synthesis method of (R) -2- (1-aminoethyl) -4-fluorophenol
AU2018306328B2 (en) * 2017-07-28 2023-03-09 Turning Point Therapeutics, Inc. Macrocyclic compounds and uses thereof
TWI791053B (en) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 Crystalline forms of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile and pharmaceutical composition thereof
TWI876442B (en) 2017-10-10 2025-03-11 美商絡速藥業公司 Formulations of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile
MA50456A (en) 2017-10-26 2020-09-02 Array Biopharma Inc MACROCYCLIC KINASE TRK INHIBITOR FORMULATIONS
CN109516999B (en) * 2017-11-01 2021-08-17 郑州泰基鸿诺医药股份有限公司 Compounds useful as protein kinase modulators and uses thereof
AU2018364938B2 (en) * 2017-11-10 2021-11-11 Angex Pharmaceutical, Inc. Macrocyclic compounds as TRK kinase inhibitors and uses thereof
JOP20200152A1 (en) * 2017-12-19 2022-10-30 Turning Point Therapeutics Inc Macrocyclic compounds for treating disease
WO2019126122A1 (en) 2017-12-19 2019-06-27 Tp Therapeutics, Inc. Macrocyclic kinase inhibitors and their use
WO2019120194A1 (en) 2017-12-22 2019-06-27 深圳市塔吉瑞生物医药有限公司 Substituted pyrazolo[1,5-a]pyrimidine compound and pharmaceutical composition and use thereof
US11472802B2 (en) 2018-01-18 2022-10-18 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors
CN111971286B (en) 2018-01-18 2023-04-14 阿雷生物药品公司 Substituted pyrrolo [2,3-d ] pyrimidine compounds 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 (en) * 2018-01-23 2019-08-01 深圳市塔吉瑞生物医药有限公司 Substituted pyrazolo[1,5-a]pyrimidine macrocyclic compound
TW201932472A (en) * 2018-01-30 2019-08-16 大陸商上海吉倍生物技術有限公司 Compound having macrocyclic molecular structure and use thereof
CN110156813B (en) * 2018-02-13 2023-07-25 北京诺诚健华医药科技有限公司 Heterocyclic compounds as TRK inhibitors
MX2020010116A (en) * 2018-03-28 2020-11-06 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
CN110386944B (en) * 2018-04-16 2021-10-29 深圳市塔吉瑞生物医药有限公司 Di (hetero) aryl macrocycles for inhibiting protein kinase activity
WO2019206069A1 (en) * 2018-04-25 2019-10-31 北京普祺医药科技有限公司 Diaryl macrocyclic compound and pharmaceutical composition, and use thereof
CN111918868B (en) * 2018-05-04 2022-12-30 正大天晴药业集团股份有限公司 Diaryl macrocycles as protein kinase modulators
CN110627812B (en) 2018-06-25 2022-10-11 北京诺诚健华医药科技有限公司 Heterocyclic compounds as TRK inhibitors
JP7286755B2 (en) 2018-07-31 2023-06-05 ロクソ オンコロジー， インコーポレイテッド (S)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1H-pyrazole - Spray-dried dispersions and formulations of 4-carboxamides
JP2022500383A (en) 2018-09-10 2022-01-04 アレイ バイオファーマ インコーポレイテッド Condensed heterocyclic compound as a RET kinase inhibitor
CN110950889B (en) * 2018-09-27 2022-04-05 北京赛林泰医药技术有限公司 Multi-target kinase inhibitor and preparation method and application thereof
CN112955453B (en) * 2018-09-29 2022-04-19 山东绿叶制药有限公司 Pyrazolopyrimidine derivatives as selective Trk inhibitors
SI3870579T1 (en) 2018-10-22 2025-03-31 Alumis Inc. Tyk2 inhibitors and uses thereof
CN111171049B (en) * 2018-11-09 2021-06-04 山东轩竹医药科技有限公司 Tyrosine kinase inhibitors and uses thereof
AU2019375825B2 (en) * 2018-11-09 2022-09-15 Shandong Xuanzhu Pharma Co., Ltd. Macrocyclic tyrosine kinase inhibitor and uses thereof
CN113164475A (en) * 2018-11-19 2021-07-23 达纳-法伯癌症研究公司 Macrocyclic inhibitors of DYRK1A
US12180207B2 (en) 2018-12-19 2024-12-31 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 (en) * 2019-02-21 2021-09-10 山东轩竹医药科技有限公司 Macrocyclic kinase inhibitors and uses thereof
EP3938369A4 (en) * 2019-03-11 2023-01-25 Alumis Inc. TYK2 INHIBITORS AND THEIR USES
JP7595582B2 (en) * 2019-03-26 2024-12-06 ベンティックス バイオサイエンシーズ，インク． TYK2 pseudokinase ligand
WO2020233645A1 (en) * 2019-05-21 2020-11-26 浙江海正药业股份有限公司 Macrolide derivatives, preparation method and application thereof
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
PH12021553174A1 (en) * 2019-06-19 2022-08-01 Turning Point Therapeutics Inc Polymorphs of a macrocyclic kinase inhibitor
CN113773335B (en) * 2019-06-21 2024-12-03 成都海博为药业有限公司 A compound as a protein kinase inhibitor and its preparation method and use
MX2021015770A (en) * 2019-06-21 2022-04-12 Janssen Pharmaceutica Nv MACROCYCLIC MCL-1 INHIBITORS.
WO2021027503A1 (en) * 2019-08-12 2021-02-18 罗欣药业(上海)有限公司 Tricyclic compound, preparation method therefor, and intermediate and use thereof
WO2021063276A1 (en) * 2019-09-30 2021-04-08 浙江海正药业股份有限公司 Macrocyclic derivative, preparation method therefor and use thereof
TW202133855A (en) * 2019-11-27 2021-09-16 美商特普醫葯公司 Combination therapy involving diaryl macrocyclic compounds
KR20220134522A (en) 2019-11-27 2022-10-05 터닝 포인트 테라퓨틱스, 인크. Combination therapy involving diaryl macrocyclic compounds
AU2020395136A1 (en) * 2019-12-03 2022-07-07 Turning Point Therapeutics, Inc. Macrocycles for use in treating disease
EP4069369A4 (en) 2019-12-06 2024-02-14 Schrödinger, Inc. CYCLIC COMPOUNDS AND METHODS OF USE
JP2023509886A (en) 2019-12-27 2023-03-10 シュレーディンガー， インコーポレイテッド Cyclic compounds and methods of use thereof
CN113045587A (en) * 2019-12-27 2021-06-29 成都倍特药业股份有限公司 Crystal form of macrocyclic compound and preparation method thereof
CN113135938B (en) * 2020-01-19 2022-06-14 山东轩竹医药科技有限公司 Substituted macrocyclic tyrosine kinase inhibitors and uses thereof
IL295938A (en) * 2020-03-02 2022-10-01 Turning Point Therapeutics Inc Therapeutic uses of macrocyclic compounds
KR20230020983A (en) 2020-05-04 2023-02-13 암젠 인코포레이션 Heterocyclic compounds as triggering receptors expressed on myeloid cell 2 agonists and methods of use
WO2021223748A1 (en) * 2020-05-08 2021-11-11 山东轩竹医药科技有限公司 Crystal form of macrocyclic tyrosine kinase inhibitor and preparation method therefor
WO2021244609A1 (en) * 2020-06-04 2021-12-09 成都倍特药业股份有限公司 Compound having macrocyclic structure and use thereof
MX2023000503A (en) * 2020-07-10 2023-02-09 Blossomhill Therapeutics Inc MACROCYCLES AND THEIR USE.
EP4211140A1 (en) 2020-09-10 2023-07-19 Schrödinger, Inc. Heterocyclic pericondensed cdc7 kinase inhibitors for the treatment of cancer
WO2022164789A1 (en) 2021-01-26 2022-08-04 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disoders
WO2022182845A1 (en) * 2021-02-25 2022-09-01 Blossomhill Therapeutics, Inc. Macrocycles and their use
TW202300150A (en) 2021-03-18 2023-01-01 美商薛定諤公司 Cyclic compounds and methods of using same
CN113754657B (en) * 2021-09-22 2023-01-17 广州白云山医药集团股份有限公司白云山制药总厂 Crystal form of macrocyclic compound, preparation method and application thereof
CN116063326A (en) * 2021-11-02 2023-05-05 赛诺哈勃药业（成都）有限公司 Amino-containing macrocycles as protein kinase modulators
CN116514813A (en) * 2021-12-31 2023-08-01 轩竹生物科技股份有限公司 Preparation method of tyrosine kinase inhibitor and intermediate thereof
MX2024008413A (en) * 2022-01-05 2024-09-17 Blossomhill Therapeutics Inc MACROCYCLIC COMPOUNDS AND USE AS KINASE INHIBITORS.
CN115746023B (en) * 2022-10-27 2024-08-09 复旦大学 Heterocyclic macrocyclic compound containing indazole structure as protein kinase inhibitor and preparation method thereof
WO2025059027A1 (en) 2023-09-11 2025-03-20 Schrödinger, Inc. Cyclopenta[e]pyrazolo[1,5-a]pyrimidine derivatives as malt1 inhibitors

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
EP0281841B1 (en) 1987-03-07 1990-11-14 Bayer Ag Process for preparation of 5-amino-4,6-dihalogenopyridines
DE69425736T2 (en) 1993-03-25 2001-04-12 Pharmacia & Upjohn Co., Kalamazoo Formyl- or cyano-substituted indole derivatives with a dopaminergic effect
FR2746309B1 (en) 1996-03-22 1998-04-17 Oreal COMPOSITION FOR DYEING KERATIN FIBERS CONTAINING PYRAZOLOPYRIMIDINEOXO; THEIR USE FOR DYEING AS COUPLER, DYEING PROCESSES
GB9800569D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
FR2793791B1 (en) 1999-05-19 2002-01-25 Univ Paris 7 Denis Diderot NOVEL INHIBITOR COMPOUNDS SPECIFIC TO A2 PHOSPHOLIPASES
AU8395501A (en) 2000-07-31 2002-02-13 Hoffmann La Roche Piperazine derivatives
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
US7550470B2 (en) 2002-12-11 2009-06-23 Merck & Co. Inc. Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors
JP5749645B2 (en) 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 Macrocyclic pyrimidines as protein kinase inhibitors
CA2738026C (en) 2008-09-22 2017-01-24 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors
AU2009308465B2 (en) 2008-10-22 2015-02-12 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrimidine compounds as TRK kinase inhibitors
PE20110828A1 (en) 2008-10-31 2011-11-22 Genentech Inc PYRAZOLOPYRIMIDINE COMPOUNDS AS JAK 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 (en) 2009-07-09 2011-08-31 Array Biopharma Inc PIRAZOLO COMPOUNDS (1,5-A) PYRIMIDINE SUBSTITUTED AS TRK-QUINASA INHIBITORS
US20110029480A1 (en) * 2009-08-03 2011-02-03 IntelliCubes, Inc. Method of Compiling Multiple Data Sources into One Dataset
JP5643332B2 (en) 2009-12-07 2014-12-17 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Heterocyclic compounds containing a pyrrolopyridine or benzimidazole core
JP2013512952A (en) 2009-12-07 2013-04-18 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Heterocyclic compounds containing indole cores
SA111320200B1 (en) 2010-02-17 2014-02-16 ديبيوفارم اس ايه Bicyclic Compounds and their Uses as Dual C-SRC / JAK Inhibitors
DK2918588T3 (en) 2010-05-20 2017-08-28 Array Biopharma Inc Macrocyclic compounds as TRK kinase inhibitors
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
RU2014110399A (en) 2011-08-19 2015-09-27 Мерк Шарп И Доум Корп. HCV CRYSTAL FORMS OF PROTEASIC INHIBITOR
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
CN103930427B (en) * 2011-09-30 2016-03-09 昂科迪塞恩股份有限公司 Large ring FLT3 kinase inhibitor
CA2852936A1 (en) 2011-10-20 2013-04-25 Glaxosmithkline Llc Substituted bicyclic aza-heterocycles and analogues as sirtuin modulators
CN104169286B (en) 2012-03-06 2016-06-08 辉瑞大药厂 Be used for the treatment of the macrocyclic derivatives of proliferative diseases
JP6418950B2 (en) 2012-03-09 2018-11-07 レクシコン ファーマシューティカルズ インコーポレイテッド Pyrazolo [1,5-a] pyrimidine compounds, compositions containing them, and methods of using them
KR102085121B1 (en) * 2012-03-09 2020-03-05 렉시컨 파마슈티컬스 인코퍼레이티드 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
HK1215250A1 (en) 2013-01-30 2016-08-19 Bayer Pharma Aktiengesellschaft Amino-substituted isothiazoles
CN105358534A (en) 2013-04-23 2016-02-24 斯洛文尼亚莱柯制药股份有限公司 Novel synthetic process to 8-chloro-1-methyl-benzo[d]azepine, novel intermediates and the production thereof
EP3026051A4 (en) 2013-07-24 2017-03-08 Takeda Pharmaceutical Company Limited Heterocyclic compound
WO2015073267A1 (en) 2013-11-15 2015-05-21 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
CN110317214B (en) 2014-01-24 2022-11-22 特普医药公司 Diaryl macrocycles as modulators of protein kinases
WO2016070241A1 (en) 2014-11-03 2016-05-12 Ctxt Pty Ltd Triazine compounds, compositions and synthesis
CN107207514B (en) 2014-12-15 2020-01-24 康联制药有限公司 Fused heteroaryl compounds and their use as TRK inhibitors
ES2928084T3 (en) 2015-02-20 2022-11-15 Rigel Pharmaceuticals Inc GDF-8 inhibitors
US10329294B2 (en) 2015-03-12 2019-06-25 Merck Sharp & Dohme Corp. Pyrazolopyrimidine inhibitors of IRAK4 activity
WO2016144844A1 (en) 2015-03-12 2016-09-15 Merck Sharp & Dohme Corp. Carboxamide inhibitors of irak4 activity
CR20170509A (en) 2015-05-05 2018-04-16 Bayer Pharma AG CYCLHEXAN DERIVATIVES REPLACED WITH AMIDO
US10316044B2 (en) 2015-07-02 2019-06-11 Tp Therapeutics, Inc. Chiral diaryl macrocycles as modulators of protein kinases
RU2765181C2 (en) 2015-07-06 2022-01-26 Тёрнинг Поинт Терапьютикс, Инк. Polymorphic form of diaryl macrocycle
EP4480543A3 (en) 2015-07-21 2025-02-12 Turning Point Therapeutics, Inc. Chiral diaryl macrocycle and use thereof in the treatment of cancer
KR20180102544A (en) 2015-10-26 2018-09-17 더 리전츠 오브 더 유니버시티 오브 콜로라도, 어 바디 코퍼레이트 TRK Inhibitors - Point Mutation in Resistant Cancer and Related Methods
EP3423435B1 (en) 2016-03-04 2023-08-23 Vanderbilt University Substituted indole mcl-1 inhibitors
CN109715165A (en) 2016-07-28 2019-05-03 Tp生物医药公司 Huge ring kinase inhibitor
EP3555137A1 (en) 2016-12-14 2019-10-23 Development Center for Biotechnology Antibody-drug conjugates and uses thereof
TWI808958B (en) 2017-01-25 2023-07-21 美商特普醫葯公司 Combination therapy involving diaryl macrocyclic compounds
AU2018306328B2 (en) 2017-07-28 2023-03-09 Turning Point Therapeutics, Inc. Macrocyclic compounds and uses thereof

Also Published As

Publication number Publication date
PL3097107T3 (en) 2020-01-31
IL268820A (en) 2019-10-31
HRP20240503T1 (en) 2024-07-05
CL2016001876A1 (en) 2017-02-03
LT3097107T (en) 2019-07-25
MY193524A (en) 2022-10-18
MX2016009588A (en) 2017-05-15
SI3636649T1 (en) 2024-07-31
WO2015112806A3 (en) 2015-11-12
PH12016501463A1 (en) 2017-02-06
JP2022133462A (en) 2022-09-13
MX2020001360A (en) 2020-03-20
ES2976459T3 (en) 2024-08-01
AU2019279951B2 (en) 2021-08-12
SI3572416T1 (en) 2023-02-28
DK3097107T3 (en) 2019-07-08
JP7356546B2 (en) 2023-10-04
HUE060554T2 (en) 2023-03-28
PE20160931A1 (en) 2016-09-21
US20170334929A1 (en) 2017-11-23
PT3097107T (en) 2019-07-19
HRP20191283T1 (en) 2019-10-18
HUE045208T2 (en) 2019-12-30
ZA201604654B (en) 2020-10-28
EP3097107A2 (en) 2016-11-30
HK1231407A1 (en) 2017-12-22
CN106170289A (en) 2016-11-30
DK3572416T3 (en) 2022-12-12
SG11201605929RA (en) 2016-08-30
PH12016501463B1 (en) 2017-02-06
LT3636649T (en) 2024-04-10
US20170002023A1 (en) 2017-01-05
EP3636648A1 (en) 2020-04-15
EP4338739A3 (en) 2024-05-29
PL3572416T3 (en) 2023-02-27
US20220112213A1 (en) 2022-04-14
FR25C1013I1 (en) 2025-06-20
CN110317214A (en) 2019-10-11
HUE066590T2 (en) 2024-08-28
IL246860A0 (en) 2016-08-31
CY1121850T1 (en) 2020-07-31
ES2933350T3 (en) 2023-02-06
CN110317214B (en) 2022-11-22
KR20160111395A (en) 2016-09-26
US10618912B2 (en) 2020-04-14
EA201691492A1 (en) 2017-06-30
AU2019279951A1 (en) 2020-01-16
FIC20250015I1 (en) 2025-03-20
US10246466B2 (en) 2019-04-02
IL268820B (en) 2021-10-31
JP2021063121A (en) 2021-04-22
CN110317213A (en) 2019-10-11
RS65417B1 (en) 2024-05-31
MX392904B (en) 2025-03-24
US20240140964A1 (en) 2024-05-02
LT3572416T (en) 2022-12-27
HUS2500016I1 (en) 2025-04-28
SMT202300008T1 (en) 2023-03-17
EP3572416A1 (en) 2019-11-27
ES2735729T3 (en) 2019-12-20
CA2936079C (en) 2022-07-19
RS59059B1 (en) 2019-08-30
EP4338739A2 (en) 2024-03-20
EA201892241A1 (en) 2019-02-28
US9714258B2 (en) 2017-07-25
US20200216465A1 (en) 2020-07-09
EP3636649A1 (en) 2020-04-15
NO2025015I1 (en) 2025-03-13
JP6490713B2 (en) 2019-03-27
EA031863B1 (en) 2019-03-29
EP3572416B1 (en) 2022-09-21
JP2019104748A (en) 2019-06-27
KR102402179B1 (en) 2022-05-25
SMT201900388T1 (en) 2019-09-09
CA2936079A1 (en) 2015-07-30
NZ722375A (en) 2022-11-25
FI3636649T3 (en) 2024-05-02
UA121206C2 (en) 2020-04-27
AP2016009383A0 (en) 2016-08-31
AU2015209239B2 (en) 2019-09-12
PL3636649T3 (en) 2024-05-06
PT3572416T (en) 2022-12-06
CN106170289B (en) 2019-07-23
IL246860B (en) 2019-09-26
EP3636649B1 (en) 2024-02-14
JP2023179539A (en) 2023-12-19
CN110317213B (en) 2022-10-18
EP3097107A4 (en) 2017-08-09
EP3097107B1 (en) 2019-04-17
SI3097107T1 (en) 2019-08-30
HRP20221518T1 (en) 2023-02-17
JP2017503867A (en) 2017-02-02
SMT202400175T1 (en) 2024-07-09
EP3636650A1 (en) 2020-04-15
ZA202004100B (en) 2023-12-20
RS63829B1 (en) 2023-01-31
NZ761094A (en) 2023-02-24
US20190169207A1 (en) 2019-06-06
PT3636649T (en) 2024-04-09
DK3636649T3 (en) 2024-05-21
WO2015112806A2 (en) 2015-07-30
NL301322I2 (en) 2025-05-27
AU2015209239A1 (en) 2016-07-14

Similar Documents

Publication Publication Date Title
HUS2500016I1 (en) Diaryl macrocycles as modulators of protein kinases
IL256377A (en) Chiral diaryl macrocycles as modulators of protein kinases
IL259421B (en) Modulators of ror-gamma
IL252417A0 (en) Methods of modulating drug plasma levels using erythrohydroxybupropion
IL247234A0 (en) Modulators of caspase-6
GB201620640D0 (en) Vacuum-deposited modification of polymer surfaces
EP3200955A4 (en) Methods of polishing
HK40109104A (en) Diaryl macrocycles as modulators of protein kinases
SG11201607445QA (en) Methods of modulating wars2
PT3377106T (en) Modulation of ciliogenesis
GB201418230D0 (en) Construction of surfaces
GB201407888D0 (en) Novel specific kinase modulators
GB201406276D0 (en) Making of land