RS64122B1 - Kristalni oblik (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamid hidrogensulfata - Google Patents

Kristalni oblik (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamid hidrogensulfata

Info

Publication number
RS64122B1
RS64122B1 RS20230253A RSP20230253A RS64122B1 RS 64122 B1 RS64122 B1 RS 64122B1 RS 20230253 A RS20230253 A RS 20230253A RS P20230253 A RSP20230253 A RS P20230253A RS 64122 B1 RS64122 B1 RS 64122B1
Authority
RS
Serbia
Prior art keywords
crystalline form
trka
trk
cancer
pain
Prior art date
Application number
RS20230253A
Other languages
English (en)
Serbian (sr)
Inventor
Alisha B Arrigo
Derrick Juengst
Khalid Shah
Original Assignee
Array Biopharma 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=54848892&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RS64122(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of RS64122B1 publication Critical patent/RS64122B1/sr

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P25/28Drugs 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12QMEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/48Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
    • C12Q1/485Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12YENZYMES
    • C12Y207/00Transferases transferring phosphorus-containing groups (2.7)
    • C12Y207/10Protein-tyrosine kinases (2.7.10)
    • C12Y207/10001Receptor protein-tyrosine kinase (2.7.10.1)
    • 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
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90Enzymes; Proenzymes
    • G01N2333/91Transferases (2.)
    • G01N2333/912Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • G01N2333/91205Phosphotransferases in general
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00Detection or diagnosis of diseases
    • G01N2800/52Predicting or monitoring the response to treatment, e.g. for selection of therapy based on assay results in personalised medicine; Prognosis
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Immunology (AREA)
  • Analytical Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
RS20230253A 2014-11-16 2015-11-16 Kristalni oblik (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamid hidrogensulfata RS64122B1 (sr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462080374P 2014-11-16 2014-11-16
US201562169545P 2015-06-01 2015-06-01
EP20169707.5A EP3699181B1 (en) 2014-11-16 2015-11-16 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

Publications (1)

Publication Number Publication Date
RS64122B1 true RS64122B1 (sr) 2023-05-31

Family

ID=54848892

Family Applications (1)

Application Number Title Priority Date Filing Date
RS20230253A RS64122B1 (sr) 2014-11-16 2015-11-16 Kristalni oblik (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamid hidrogensulfata

Country Status (30)

Country Link
US (5) US10799505B2 (OSRAM)
EP (2) EP3699181B1 (OSRAM)
JP (2) JP6914834B2 (OSRAM)
KR (1) KR102649887B1 (OSRAM)
CN (2) CN107428760B (OSRAM)
AU (1) AU2015346046B2 (OSRAM)
BR (1) BR112017010141A2 (OSRAM)
CA (1) CA2967951C (OSRAM)
CL (1) CL2017001249A1 (OSRAM)
CO (1) CO2017005483A2 (OSRAM)
CR (1) CR20170263A (OSRAM)
DK (1) DK3699181T3 (OSRAM)
ES (1) ES2941630T3 (OSRAM)
FI (1) FI3699181T3 (OSRAM)
HK (1) HK1244483A1 (OSRAM)
HR (1) HRP20230271T1 (OSRAM)
HU (1) HUE061448T2 (OSRAM)
IL (2) IL290905B2 (OSRAM)
LT (1) LT3699181T (OSRAM)
MX (2) MX376478B (OSRAM)
PH (2) PH12017500900A1 (OSRAM)
PL (1) PL3699181T3 (OSRAM)
PT (1) PT3699181T (OSRAM)
RS (1) RS64122B1 (OSRAM)
SG (1) SG11201703962XA (OSRAM)
SI (1) SI3699181T1 (OSRAM)
TW (2) TWI746426B (OSRAM)
UA (1) UA123044C2 (OSRAM)
WO (1) WO2016077841A1 (OSRAM)
ZA (1) ZA201703501B (OSRAM)

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2350075B1 (en) 2008-09-22 2014-03-05 Array Biopharma, Inc. Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors
KR101853026B1 (ko) 2008-10-22 2018-04-27 어레이 바이오파마 인크. TRK 키나아제 억제제로서 치환된 피라졸로[1,5­a] 피리미딘 화합물
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
CN105693720B (zh) 2010-05-20 2019-01-18 阵列生物制药公司 作为trk激酶抑制剂的大环化合物
WO2015017533A1 (en) * 2013-07-30 2015-02-05 Blueprint Medicines Corporation Ntrk2 fusions
US20160053301A1 (en) 2014-08-22 2016-02-25 Clearfork Bioscience, Inc. Methods for quantitative genetic analysis of cell free dna
TWI746426B (zh) 2014-11-16 2021-11-21 美商亞雷生物製藥股份有限公司 (S)-N-(5-((R)-2-(2,5-二氟苯基)-吡咯啶-1-基)-吡唑并[1,5-a]嘧啶-3-基)-3-羥基吡咯啶-1-甲醯胺硫酸氫鹽結晶型
KR20180021745A (ko) 2015-06-01 2018-03-05 록쏘 온콜로지, 인코포레이티드 암을 진단하고 치료하는 방법
EP3322706B1 (en) 2015-07-16 2020-11-11 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
TN2018000138A1 (en) 2015-10-26 2019-10-04 Array Biopharma Inc Point mutations in trk inhibitor-resistant cancer and methods relating to the same
HUE068971T2 (hu) * 2016-04-04 2025-02-28 Loxo Oncology Inc (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-A]pirimidin-3-il) -3-hidroxipirrolidin-1-karboxamid folyékony készítményei
RS65988B1 (sr) 2016-04-04 2024-10-31 Loxo Oncology Inc Postupak lečenja pedijatrijskih karcinoma
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
SI3458456T1 (sl) * 2016-05-18 2021-04-30 Loxo Oncology, Inc. Priprava (S)-N-(5-((R)-2-(2,5-difluorofenil) pirolidin-1-il) pirazolo (1,5-A) pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida
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
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
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
US10180422B1 (en) 2017-08-22 2019-01-15 Scripps Health Methods of treating a neuroendocrine tumor
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
ES3042417T3 (en) 2017-10-31 2025-11-20 Assia Chem Ind Ltd Salts and solid state forms of larotrectinib
CN107987082B (zh) * 2017-11-14 2019-09-20 苏州东南药业股份有限公司 一种Larotrectinib的制备方法及其中间体
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
WO2019143994A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
CN111971286B (zh) 2018-01-18 2023-04-14 阿雷生物药品公司 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物
TW201938169A (zh) 2018-01-18 2019-10-01 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[3,4-d]嘧啶化合物
CN109575025B (zh) 2018-01-23 2020-09-11 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
WO2019157065A1 (en) 2018-02-06 2019-08-15 University Of Miami Inhibitors of the notch transcriptional activation complex kinase ("nack") and methods for use of the same
CA3095366A1 (en) 2018-03-29 2019-10-03 Loxo Oncology, Inc. Treatment of trk-associated cancers
WO2019220352A1 (en) * 2018-05-15 2019-11-21 Dr. Reddy’S Laboratories Limited Amorphous solid dispersion of larotrectinib sulfate and process thereof
CN110294761B (zh) * 2018-06-08 2020-09-08 南京雷正医药科技有限公司 作为Trk激酶抑制剂的取代的吡唑并[1,5-a]嘧啶化合物
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
CN110857304B (zh) * 2018-08-24 2021-05-18 北京富龙康泰生物技术有限公司 Trk抑制剂、其制备方法和用途
ES2922314T3 (es) 2018-09-10 2022-09-13 Array Biopharma Inc Compuestos heterocíclicos condensados como inhibidores de cinasa RET
CN111138333B (zh) * 2018-11-02 2023-05-23 上海复星星泰医药科技有限公司 一种(r)-2-(2,5-二氟苯基)-吡咯烷的制备方法
CN109232582B (zh) * 2018-11-28 2021-02-05 安礼特(上海)医药科技有限公司 拉洛替尼硫酸氢盐晶型及其制备和应用
TWI736037B (zh) 2018-11-29 2021-08-11 美商輝瑞股份有限公司 化學化合物
CN109608464B (zh) * 2018-12-12 2021-09-24 上海健康医学院 一种放射性碘标记Larotrectinib化合物及其制备方法和应用
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
CN109593803A (zh) * 2018-12-24 2019-04-09 上海健康医学院 (r)-2-(2,5-二氟苯基)吡咯烷或其盐的制备方法
CN111057729B (zh) * 2019-06-03 2023-08-29 弈柯莱生物科技(上海)股份有限公司 一种(r)-2-(2,5-二氟苯基)吡咯烷及其制备方法和应用
CN110804059B (zh) * 2019-09-30 2024-03-12 郑州泰基鸿诺医药股份有限公司 氨基甲酸酯类化合物、药物组合物及其应用
CN110981779B (zh) * 2019-11-23 2021-02-26 武汉理工大学 R-2-(2,5-二氟苯基)吡咯烷的合成方法
CN111087398A (zh) * 2019-12-24 2020-05-01 上海万巷制药有限公司 一种制备拉罗替尼中间体的清洁工艺
CN111302997B (zh) * 2020-04-15 2022-03-29 江苏恒沛药物科技有限公司 “一锅法”制备拉罗替尼中间体的方法
WO2021250174A1 (en) * 2020-06-10 2021-12-16 Epics Therapeutics Synthesis of (2s,5r)-5-(2-chlorophenyl)-1-(2'-methoxy-[1,1'-biphenyl]-4-carbonyl)pyrrolidine-2-carboxylic acid
CN111763211A (zh) * 2020-08-05 2020-10-13 安庆多辉生物科技有限公司 拉罗替尼盐酸盐、制备方法与应用
RU2764955C1 (ru) * 2021-01-11 2022-01-24 Федеральное государственное бюджетное научное учреждение "Томский национальный исследовательский медицинский центр" Российской академии наук ("Томский НИМЦ") Способ комбинированного лечения метастатического колоректального рака у больных с резектабельными метастазами в печени и при отсутствии мутаций в генах KRAS и BRAF
RU2760174C1 (ru) * 2021-01-11 2021-11-22 Федеральное государственное бюджетное научное учреждение "Томский национальный исследовательский медицинский центр" Российской академии наук ("Томский НИМЦ") Способ комбинированного лечения метастатического колоректального рака у больных с резектабельными метастазами в печени и при наличии мутаций в генах KRAS и BRAF
WO2022168115A1 (en) * 2021-02-05 2022-08-11 Mylan Laboratories Limited A process for the preparation of larotrectinib or its salts
IT202100003887A1 (it) 2021-02-19 2022-08-19 Olon Spa Procedimento per la preparazione di larotrectinib ad elevato grado di purezza
CN114478345B (zh) * 2022-02-10 2024-06-14 中瀚(齐河县)生物医药科技有限公司 一种(r)-2-(2,5-二氟苯基)吡咯烷的制备方法
WO2024023836A1 (en) * 2022-07-27 2024-02-01 Mylan Laboratories Limited Polymorphic form of larotrectinib sulfate

Family Cites Families (198)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ234143A (en) 1989-06-28 1991-10-25 Mcneil Ppc Inc Aqueous pharmaceutical suspension formulation for administering substantially insoluble pharmaceutical agents
RO118291B1 (ro) 1993-11-30 2003-04-30 Searle & Co Derivati de pirazol 1,3,4,5 - tetrasubstituiti si compozitie farmaceutica care ii contine
US5844092A (en) 1994-03-18 1998-12-01 Genentech, Inc. Human TRK receptors and neurotrophic factor inhibitors
US5430021A (en) 1994-03-18 1995-07-04 Pharmavene, Inc. Hydrophobic drug delivery systems
US5877016A (en) 1994-03-18 1999-03-02 Genentech, Inc. Human trk receptors and neurotrophic factor inhibitors
CA2206201A1 (en) 1996-05-29 1997-11-29 Yoshiaki Isobe Pyrazole derivatives and their pharmaceutical use
JP3898296B2 (ja) 1996-08-28 2007-03-28 ポーラ化成工業株式会社 ピロロピラゾロピリミジン化合物及びこれを有効成分とする医薬
ATE283270T1 (de) 1997-04-25 2004-12-15 Takeda Chemical Industries Ltd Condensierte pyridazine derivate,deren herstellung und verwendung
UA74546C2 (en) 1999-04-06 2006-01-16 Boehringer Ingelheim Ca Ltd Macrocyclic peptides having activity relative to hepatitis c virus, a pharmaceutical composition and use of the pharmaceutical composition
US6534085B1 (en) 1999-09-23 2003-03-18 Bioresponse L.L.C. Phytochemicals for promoting weight loss
DK1292680T3 (da) 2000-06-22 2010-03-08 Genentech Inc Agonist-anti-TrkC monoklonale antistoffer
TWI312347B (en) 2001-02-08 2009-07-21 Eisai R&D Man Co Ltd Bicyclic nitrogen-containing condensed ring compounds
NZ529612A (en) 2001-05-30 2006-03-31 Genentech Inc Anti-NGF antibodies for the treatment of various disorders
US7101572B2 (en) 2001-12-07 2006-09-05 Unilab Pharmatech, Ltd. Taste masked aqueous liquid pharmaceutical composition
US20030199525A1 (en) 2002-03-21 2003-10-23 Hirst Gavin C. Kinase inhibitors
AU2003227437A1 (en) 2002-04-23 2003-11-10 Shionogi And Co., Ltd. PYRAZOLO(1,5-a)PYRIMIDINE DERIVATIVE AND NAD(P)H OXIDASE INHIBITOR CONTAINING THE SAME
US7449488B2 (en) 2002-06-04 2008-11-11 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
ITMI20021620A1 (it) 2002-07-23 2004-01-23 Novuspharma Spa Composto ad ativita' antitumorale
JP4024624B2 (ja) 2002-08-26 2007-12-19 富士通株式会社 半導体装置の製造方法及び製造装置
EP1537116B1 (en) 2002-09-04 2010-06-02 Schering Corporation Pyrazolopyrimidines suitable for the treatment of cancer diseases
US7119200B2 (en) 2002-09-04 2006-10-10 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7196078B2 (en) 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
US8580782B2 (en) 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
WO2004052315A2 (en) 2002-12-11 2004-06-24 Merck & Co., Inc. Tyrosine kinase inhibitors
WO2004052286A2 (en) 2002-12-11 2004-06-24 Merck & Co., Inc. Tyrosine kinase inhibitors
GB0303910D0 (en) 2003-02-20 2003-03-26 Merck Sharp & Dohme Therapeutic agents
US20070037150A1 (en) 2003-02-21 2007-02-15 The Johns Hopkins University Tyrosine kinome
JP2004277337A (ja) 2003-03-14 2004-10-07 Sumitomo Pharmaceut Co Ltd ピラゾロ[1,5−a]ピリミジン誘導体
EP1608652A1 (en) 2003-03-31 2005-12-28 Vernalis (Cambridge) Limited Pyrazolopyrimidine compounds and their use in medicine
US20060094699A1 (en) 2003-04-11 2006-05-04 Kampen Gita Camilla T Combination therapy using an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor and a glucocorticoid receptor agonist to minimize the side effects associated with glucocorticoid receptor agonist therapy
EP1615697A2 (en) 2003-04-11 2006-01-18 Novo Nordisk A/S New pyrazolo[1,5-a] pyrimidine derivatives and pharmaceutical use thereof
WO2004089415A2 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S COMBINATIONS OF AN 11β-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITOR AND A GLUCOCORTICOID RECEPTOR AGONIST
EP1619203A1 (en) 2003-04-28 2006-01-25 Galpharma Co., Ltd. Galectin 9-inducing factor
PA8603801A1 (es) 2003-05-27 2004-12-16 Janssen Pharmaceutica Nv Derivados de la quinazolina
JP2005008581A (ja) 2003-06-20 2005-01-13 Kissei Pharmaceut Co Ltd 新規なピラゾロ[1,5−a]ピリミジン誘導体、それを含有する医薬組成物およびそれらの用途
EA009517B1 (ru) 2003-06-27 2008-02-28 Байер Кропсайенс Аг Пиразолопиримидины
UA115960C2 (uk) 2003-07-15 2018-01-25 Емджен, Інк., Людські анти-ngf нейтралізуючі антитіла як селективні інгібітори метаболічних шляхів фактора росту нервової тканини (ngf)
US7491794B2 (en) 2003-10-14 2009-02-17 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
CA2543116A1 (en) 2003-10-27 2005-05-19 Genelabs Technologies, Inc. Methods for preparing 7-(2'-substituted-.szlig.-d-ribofuranosyl)-4-(nr2r3)-5-(substituted ethyn-1-yl)-pyrrolo[2,3-d]pyrimidine derivatives
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
PE20051046A1 (es) 2003-11-28 2006-01-11 Novartis Ag Derivados de diaril-urea en el tratamiento de enfermedades dependientes de la quinasa de proteina
ES2305887T3 (es) 2003-12-18 2008-11-01 Janssen Pharmaceutica Nv Derivados de pirido y pirimidopirimidinas como agentes antiproliferativos.
ES2527118T3 (es) 2003-12-19 2015-01-20 Plexxikon Inc. Compuestos y procedimientos de desarrollo de moduladores de Ret
WO2005068424A1 (en) 2004-01-20 2005-07-28 Cell Therapeutics Europe S.R.L. Indolinone derivatives as receptor tyrosine kinase ihibitors
US20050222171A1 (en) 2004-01-22 2005-10-06 Guido Bold Organic compounds
WO2005099363A2 (en) 2004-03-26 2005-10-27 Whitehead Institute For Biomedical Research Methods of diagnosing, preventing and treating cancer metastasis
UA91677C2 (ru) 2004-03-30 2010-08-25 Интермюн, Инк. Макроциклические соединения как ингибиторы вирусной репликации
PE20060664A1 (es) 2004-09-15 2006-08-04 Novartis Ag Amidas biciclicas como inhibidores de cinasa
KR20070090172A (ko) 2004-11-04 2007-09-05 버텍스 파마슈티칼스 인코포레이티드 단백질 키나아제의 억제제로서 유용한피라졸로[1,5-a]피리미딘
JO3088B1 (ar) 2004-12-08 2017-03-15 Janssen Pharmaceutica Nv مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف
DE102005003687A1 (de) 2005-01-26 2006-07-27 Sphingo Tec Gmbh Immunoassay zur Bestimmung der Freisetzung von Neurotensin in die Zirkulation
CN101119996A (zh) 2005-02-16 2008-02-06 阿斯利康(瑞典)有限公司 化学化合物
WO2006087538A1 (en) 2005-02-16 2006-08-24 Astrazeneca Ab Chemical compounds
KR20070120963A (ko) 2005-03-21 2007-12-26 일라이 릴리 앤드 캄파니 이미다조피리다진 화합물
JP2008540335A (ja) 2005-04-27 2008-11-20 アストラゼネカ・アクチエボラーグ ピラゾリル・ピリミジン誘導体の疼痛治療における使用
US20080287437A1 (en) 2005-05-16 2008-11-20 Astrazeneca Ab Pyrazolylaminopyrimidine Derivatives Useful as Tyrosine Kinase Inhibitors
CN100406650C (zh) 2005-06-05 2008-07-30 徐斌 一种抗特大变位的模块式梳型桥梁伸缩缝装置
ITRM20050290A1 (it) 2005-06-07 2006-12-08 Lay Line Genomics Spa Uso di molecole in grado di inibire il legame tra ngf e il suo recettore trka come analgesici ad effetto prolungato.
US20070025540A1 (en) 2005-07-07 2007-02-01 Roger Travis Call center routing based on talkativeness
CN101263156A (zh) 2005-07-25 2008-09-10 因特蒙公司 C型肝炎病毒复制的新颖大环抑制剂
US20100216798A1 (en) 2005-07-29 2010-08-26 Astellas Pharma Inc Fused heterocycles as lck inhibitors
EP1909760A1 (en) 2005-08-03 2008-04-16 Eastman Chemical Company Tocopheryl polyethylene glycol succinate powder and process for preparing same
CA2619365A1 (en) 2005-08-22 2007-03-01 Amgen Inc. Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators
US20070049591A1 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Inhibitors of MAPK/Erk Kinase
HRP20140218T4 (hr) 2005-08-25 2017-06-16 Creabilis Therapeutics S.P.A. Polimerni konjugati k-252a i njihovi derivati
DE102005042742A1 (de) 2005-09-02 2007-03-08 Schering Ag Substituierte Imidazo[1,2b]pyridazine als Kinase-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
US20070078136A1 (en) 2005-09-22 2007-04-05 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
TWI421078B (zh) 2005-10-06 2014-01-01 Merck Sharp & Dohme 關卡激酶抑制劑及其用途
TW200745128A (en) 2005-10-06 2007-12-16 Schering Corp Pyrazolopyrimidines as protein kinase inhibitors
WO2007057782A2 (en) 2005-10-11 2007-05-24 Centre National De La Recherche Scientifique (Cnrs) 3 -hydroxyflavone derivatives for the detection and the quantification of cell apoptosis
CN101415705B (zh) 2005-10-11 2011-10-26 因特蒙公司 抑制丙型肝炎病毒复制的化合物和方法
JP5376950B2 (ja) 2005-10-21 2013-12-25 エクセリクシス, インク. カゼインキナーゼii(ck2)モジュレーターとしてのピリミジオン類
WO2007057399A2 (en) 2005-11-15 2007-05-24 Boehringer Ingelheim International Gmbh Treatment of cancer with indole derivatives
GB0524436D0 (en) 2005-11-30 2006-01-11 Novartis Ag Organic compounds
JP5474354B2 (ja) 2005-12-30 2014-04-16 アステックス、セラピューティックス、リミテッド 医薬化合物
WO2007084815A2 (en) 2006-01-19 2007-07-26 Janssen Pharmaceutica, N.V. Substituted thienopyrimidine kinase inhibitors
EP1978958A4 (en) 2006-01-24 2009-12-02 Merck & Co Inc RET tyrosine kinase Inhibition
KR100846988B1 (ko) 2006-03-06 2008-07-16 제일약품주식회사 신규한 티에노피리미딘 유도체 또는 이의 약학적으로허용가능한 염, 이의 제조방법 및 이를 함유하는 약학조성물
JP2009529047A (ja) 2006-03-07 2009-08-13 アレイ バイオファーマ、インコーポレイテッド ヘテロ二環系ピラゾール化合物およびその使用
GB0606805D0 (en) 2006-04-04 2006-05-17 Novartis Ag Organic compounds
BRPI0710874A2 (pt) 2006-04-26 2012-02-14 Hoffmann La Roche compostos de tienopirimidina, processos de produção dos referidos compostos, composições farmacêuticas contendo os mesmos, kit, produto, e usos dos compostos
EP2036557B1 (en) 2006-05-18 2015-10-21 Eisai R&D Management Co., Ltd. Antitumor agent for thyroid cancer
EP1873157A1 (en) 2006-06-21 2008-01-02 Bayer Schering Pharma Aktiengesellschaft Pyrazolopyrimidines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
TW201345908A (zh) 2006-07-05 2013-11-16 Mitsubishi Tanabe Pharma Corp 吡唑并〔1,5-a〕嘧啶化合物
US20100029619A1 (en) 2006-08-04 2010-02-04 Takeda Pharmaceutical Company Limted Fused heterocyclic compound
US7531539B2 (en) 2006-08-09 2009-05-12 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
WO2008030579A2 (en) 2006-09-07 2008-03-13 Biogen Idec Ma Inc. Irak modulators for treating an inflammatory condition, cell proliferative disorder, immune disorder
WO2008031551A2 (en) 2006-09-12 2008-03-20 Novartis Forschungsstiftung, Zweigniederlassung Non-neuroendocrine cancer therapy
KR20090073121A (ko) 2006-09-29 2009-07-02 노파르티스 아게 Pi3k 지질 키나제 억제제로서의 피라졸로피리미딘
US20100041662A1 (en) 2006-10-30 2010-02-18 Sandrine Ferrand Heterocyclic compounds as antiinflammatory agents
MX2009004700A (es) 2006-11-06 2009-05-15 Supergen Inc Derivados de imidazo[1,2-b]piridazin y pirazolo[1,5-a] pirimidina y su uso como inhibidores de proteina cinasa.
US20080234267A1 (en) 2007-03-20 2008-09-25 Karen Elizabeth Lackey Compounds and Methods of Treatment
US20080234262A1 (en) 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
EP2137187A1 (en) 2007-03-28 2009-12-30 Inovacia AB Pyrazolo [1,5-a]pyrimidines as inhibitors of stearoyl-coa desaturase
EP2137184B1 (en) 2007-04-03 2013-05-08 Array Biopharma, Inc. Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors
US8338417B2 (en) 2007-05-04 2012-12-25 Irm Llc Compounds and compositions as c-kit and PDGFR kinase inhibitors
AU2008265104B2 (en) 2007-06-21 2013-09-12 Janssen Pharmaceutica Nv Indolin-2-ones and aza-indolin-2-ones
PL2176231T3 (pl) 2007-07-20 2017-04-28 Nerviano Medical Sciences S.R.L. Podstawione pochodne indazolu aktywne jako inhibitory kinazy
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
US7988967B2 (en) 2007-08-10 2011-08-02 Regeneron Pharmaceuticals, Inc. High affinity human antibodies to human nerve growth factor
AU2008312631A1 (en) 2007-10-16 2009-04-23 Wyeth Llc Thienopyrimidine and pyrazolopyrimidine compounds and their use as mTOR kinase and PI3 kinase inhibitors
JP2011501760A (ja) 2007-10-23 2011-01-13 ノバルティス アーゲー 呼吸器疾患の処置のためのtrkb抗体の使用
EP2217601A1 (en) 2007-11-08 2010-08-18 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyridazines for use as protein kinase inhibitors
CA2706946A1 (en) 2007-11-28 2009-06-04 Schering Corporation 2-fluoropyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
CN102015769B (zh) 2008-01-17 2014-12-10 Irm责任有限公司 改进的抗-trkb抗体
US20090227556A1 (en) 2008-01-31 2009-09-10 Eisai R&D Management Co., Ltd. Receptor tyrosine kinase inhibitors comprising pyridine and pyrimidine derivatives
BRPI0912668A2 (pt) 2008-05-13 2016-01-26 Irm Llc composto e composições como inibidores de quinase
CN102105151B (zh) 2008-07-29 2013-12-18 内尔维阿诺医学科学有限公司 Cdk抑制剂在治疗神经胶质瘤中的应用
EP2350075B1 (en) 2008-09-22 2014-03-05 Array Biopharma, Inc. Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors
KR101853026B1 (ko) 2008-10-22 2018-04-27 어레이 바이오파마 인크. TRK 키나아제 억제제로서 치환된 피라졸로[1,5­a] 피리미딘 화합물
EP2348860B1 (en) 2008-10-31 2015-05-27 Genentech, Inc. Pyrazolopyrimidine jak inhibitor compounds and methods
WO2010058006A1 (en) 2008-11-24 2010-05-27 Nerviano Medical Sciences S.R.L. Cdk inhibitor for the treatment of mesothelioma
DK2881402T3 (en) 2009-02-12 2017-08-28 Cell Signaling Technology Inc Mutant ROS expression in human liver cancer
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
ES2594927T3 (es) 2010-02-18 2016-12-23 INSERM (Institut National de la Santé et de la Recherche Médicale) Métodos para prevenir las metástasis cancerosas
KR20130043104A (ko) 2010-04-06 2013-04-29 카리스 라이프 사이언스 룩셈부르크 홀딩스 질병용 순환 생물학적 지표들
US8383793B2 (en) 2010-04-15 2013-02-26 St. Jude Children's Research Hospital Methods and compositions for the diagnosis and treatment of cancer resistant to anaplastic lymphoma kinase (ALK) kinase inhibitors
TWI510487B (zh) 2010-04-21 2015-12-01 Plexxikon Inc 用於激酶調節的化合物和方法及其適應症
CN105693720B (zh) 2010-05-20 2019-01-18 阵列生物制药公司 作为trk激酶抑制剂的大环化合物
ES2910305T3 (es) 2010-08-19 2022-05-12 Zoetis Belgium S A Anticuerpos anti-NGF y su uso
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
UY33597A (es) 2010-09-09 2012-04-30 Irm Llc Compuestos y composiciones como inhibidores de la trk
JP2014005206A (ja) 2010-10-22 2014-01-16 Astellas Pharma Inc アリールアミノヘテロ環カルボキサミド化合物
NZ611076A (en) 2010-12-01 2015-09-25 Alderbio Holdings Llc Anti-ngf compositions and use thereof
JP5959541B2 (ja) 2011-02-25 2016-08-02 ノバルティス アーゲー Trk阻害剤としてのピラゾロ[1,5−a]ピリジン
WO2012125668A1 (en) * 2011-03-17 2012-09-20 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
WO2012125667A1 (en) * 2011-03-17 2012-09-20 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
CN105130967B (zh) 2011-05-13 2018-04-17 阵列生物制药公司 作为trka激酶抑制剂的吡咯烷基脲和吡咯烷基硫脲化合物
US8656365B2 (en) 2011-09-01 2014-02-18 Infosys Limited Systems, methods, and computer-readable media for measuring quality of application programming interfaces
TW201312526A (zh) 2011-09-02 2013-03-16 Wintek Corp 觸控顯示面板
WO2013059740A1 (en) 2011-10-21 2013-04-25 Foundation Medicine, Inc. Novel alk and ntrk1 fusion molecules and uses thereof
BR112014011465A2 (pt) 2011-11-14 2017-05-09 Tesaro Inc modulação de determinadas quinases de tirosina
CA2858958C (en) 2011-12-12 2016-10-04 Dr. Reddy's Laboratories Ltd. Substituted pyrazolo[1,5-a]pyridine as tropomyosin receptor kinase (trk) inhibitors
WO2013161919A1 (ja) 2012-04-26 2013-10-31 小野薬品工業株式会社 Trk阻害化合物
MX355409B (es) 2012-05-23 2018-04-18 Nerviano Medical Sciences Srl Proceso para la preparacion de n- [5- (3,5-difluoro-bencil) -1h-indazol-3-il] -4- (4-metil-piperazin-1-il) -2- (tetrahidro-piran-4-ilamino) -benzamida.
TWI585088B (zh) 2012-06-04 2017-06-01 第一三共股份有限公司 作爲激酶抑制劑之咪唑并[1,2-b]嗒衍生物
EP2689778A1 (en) 2012-07-27 2014-01-29 Pierre Fabre Medicament Derivatives of azaindoles or diazaindoles for treating pain
US20150218652A1 (en) 2012-08-31 2015-08-06 The Regents Of The Unversity Of Colorado, A Body Corporate Methods for diagnosis and treatment of cancer
CN104703600A (zh) 2012-09-07 2015-06-10 埃克塞里艾克西斯公司 用于治疗肺腺癌的met、vegfr和ret的抑制剂
US20140084039A1 (en) 2012-09-24 2014-03-27 Electro Scientific Industries, Inc. Method and apparatus for separating workpieces
JP2014082984A (ja) 2012-10-23 2014-05-12 Astellas Pharma Inc 新規ntrk2活性化変異の検出法
AU2013337264B2 (en) 2012-11-05 2018-03-08 Foundation Medicine, Inc. Novel fusion molecules and uses thereof
US9604980B2 (en) 2012-11-07 2017-03-28 Nerviano Medical Sciences S.R.L. Substituted pyrimidinyl and pyridinyl-pyrrolopyridinones, process for their preparation and their use as kinase inhibitors
US9809578B2 (en) 2012-11-13 2017-11-07 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors
US9790210B2 (en) 2012-11-13 2017-10-17 Array Biopharma Inc. N-(monocyclic aryl),N'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
WO2014078372A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078328A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078322A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9969694B2 (en) 2012-11-13 2018-05-15 Array Biopharma Inc. N-(arylalkyl)-N′-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
US9822118B2 (en) 2012-11-13 2017-11-21 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
MX365733B (es) 2012-11-13 2019-06-12 Array Biopharma Inc Compuestos de n-pirrolidinil, n' -pirazolil-urea, tiourea, guanidina y cianoguanidina como inhibidores de trka cinasa.
RU2664541C2 (ru) 2012-11-13 2018-08-20 Эррэй Биофарма Инк. Бициклические соединения мочевины, тиомочевины, гуанидина и цианогуанидина, пригодные для лечения боли
US20150290233A1 (en) 2012-11-29 2015-10-15 Yeda Research And Development Co.Ltd. At The Weizmann Institute Of Science Methods of preventing tumor metastasis, treating and prognosing cancer and identifying agents which are putative metastasis inhibitors
US9127055B2 (en) 2013-02-08 2015-09-08 Astellas Pharma Inc. Method of treating pain with anti-human NGF antibody
BR122017003181A2 (pt) 2013-02-19 2019-09-10 Ono Pharmaceutical Co composto inibidor de trk, composição farmacêutica e medicamento compreendendo dito composto e seu uso para profilaxia e/ou terapia de doença relacionada à trk e/ou para inibir trk
WO2014130975A1 (en) 2013-02-22 2014-08-28 Bastian Boris C Fusion polynucleotides and fusion polypeptides associated with cancer and particularly melanoma and their uses as therapeutic and diagnostic targets
WO2014134096A1 (en) 2013-02-27 2014-09-04 Oregon Health & Science University Methods of treating cancers characterized by aberrent ros1 activity
WO2014152777A2 (en) 2013-03-15 2014-09-25 Insight Genetics, Inc. Methods and compositions for the diagnosis and treatment of cancers resistant to ros1 inhibitors
WO2014150751A2 (en) 2013-03-15 2014-09-25 Novartis Ag Biomarkers associated with brm inhibition
EP3421613B1 (en) 2013-03-15 2020-08-19 The Board of Trustees of the Leland Stanford Junior University Identification and use of circulating nucleic acid tumor markers
EP2968551B1 (en) 2013-03-15 2021-05-05 The Trustees of Columbia University in the City of New York Fusion proteins and methods thereof
AR095308A1 (es) 2013-03-15 2015-10-07 Glaxosmithkline Ip Dev Ltd Compuesto de 2-piridona, composición farmacéutica que lo comprende y su uso para preparar un medicamento
CN118910253A (zh) 2013-04-17 2024-11-08 生命技术公司 与癌症相关的基因融合体和基因变异体
ES2646019T3 (es) 2013-05-14 2017-12-11 Nerviano Medical Sciences S.R.L. Derivados de 6-amino-7-deaza-purina, proceso para su preparación y su uso como inhibidores de cinasa
TWI610923B (zh) 2013-07-11 2018-01-11 Betta Pharmaceuticals Co Ltd 酪氨酸蛋白激酶調節劑及其應用方法
JP6534930B2 (ja) 2013-07-26 2019-06-26 公益財団法人がん研究会 Ntrk3融合体の検出法
WO2015017533A1 (en) 2013-07-30 2015-02-05 Blueprint Medicines Corporation Ntrk2 fusions
US9511050B2 (en) 2013-10-24 2016-12-06 Georgetown University Methods and compositions for treating cancer
WO2015064621A1 (ja) 2013-10-29 2015-05-07 公益財団法人がん研究会 新規融合体及びその検出法
WO2015112806A2 (en) 2014-01-24 2015-07-30 Tp Therapeutics, Inc. Diaryl macrocycles as modulators of protein kinases
MX375372B (es) 2014-02-05 2025-03-06 VM Oncology LLC COMPOSICIONES DE COMPUESTOS DE MOLÉCULA PEQUEÑA Y USO DE LOS MISMOS COMO INHIBIDORES TrKA.
TWI672141B (zh) 2014-02-20 2019-09-21 美商醫科泰生技 投予ros1突變癌細胞之分子
HUE045340T2 (hu) 2014-05-15 2019-12-30 Array Biopharma Inc 1-((3S,4R)-4-(3-fluorfenil)-1-(2-metoxietil)pirrolidin-3-il)-3-(4-metil-3-(2- metilpirimidin-5-il)-1-fenil-1H-pirazol-5-il)karbamid mint TrkA kináz inhibitor
WO2015183837A1 (en) 2014-05-27 2015-12-03 Brian Haynes Compositions, methods, and uses related to ntrk2-tert fusions
US20170114415A1 (en) 2014-05-30 2017-04-27 The Regents Of The University Of Colorado, A Body Corporate Activating ntrk1 gene fusions predictive of kinase inhibitor therapy
BR112017001677A2 (pt) 2014-08-01 2018-07-17 Pharmacyclics Llc biomarcadores para predizer resposta de dlbcl ao tratamento com um inibidor de btk
TWI560185B (en) 2014-08-18 2016-12-01 Ono Pharmaceutical Co Acid addition salt of trk inhibitor compound
CN114920840A (zh) 2014-10-14 2022-08-19 诺华股份有限公司 针对pd-l1的抗体分子及其用途
TWI746426B (zh) 2014-11-16 2021-11-21 美商亞雷生物製藥股份有限公司 (S)-N-(5-((R)-2-(2,5-二氟苯基)-吡咯啶-1-基)-吡唑并[1,5-a]嘧啶-3-基)-3-羥基吡咯啶-1-甲醯胺硫酸氫鹽結晶型
PL3233863T3 (pl) 2014-12-15 2024-11-12 Cmg Pharmaceutical Co., Ltd. Związki heteroarylowe ze skondensowanymi pierścieniami i ich zastosowanie jako inhibitorów trk
WO2016187508A2 (en) 2015-05-20 2016-11-24 The Broad Institute Inc. Shared neoantigens
MA43943A (fr) 2015-05-29 2018-12-12 Ignyta Inc Compositions et procédés pour traiter des patients avec des cellules mutantes rtk
KR20180021745A (ko) * 2015-06-01 2018-03-05 록쏘 온콜로지, 인코포레이티드 암을 진단하고 치료하는 방법
AU2015101722A4 (en) 2015-06-19 2016-05-19 Macau University Of Science And Technology Oncogenic ros1 and alk kinase inhibitor
US9782400B2 (en) 2015-06-19 2017-10-10 Macau University Of Science And Technology Oncogenic ROS1 and ALK kinase inhibitor
GB201511546D0 (en) 2015-07-01 2015-08-12 Immatics Biotechnologies Gmbh Novel peptides and combination of peptides for use in immunotherapy against ovarian cancer and other cancers
ES2864839T3 (es) 2015-07-02 2021-10-14 Turning Point Therapeutics Inc Macrociclos de diarilo quirales como moduladores de proteína quinasas
TN2018000138A1 (en) 2015-10-26 2019-10-04 Array Biopharma Inc Point mutations in trk inhibitor-resistant cancer and methods relating to the same
WO2017127835A2 (en) 2016-01-22 2017-07-27 The Medicines Company Aqueous formulations and methods of preparation and use thereof
TW201733580A (zh) 2016-03-11 2017-10-01 小野藥品工業股份有限公司 Trk抑制劑抵抗性的癌治療劑
HUE068971T2 (hu) 2016-04-04 2025-02-28 Loxo Oncology Inc (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-A]pirimidin-3-il) -3-hidroxipirrolidin-1-karboxamid folyékony készítményei
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
CN109475545A (zh) 2016-04-19 2019-03-15 埃克塞里艾克西斯公司 三阴性乳腺癌治疗方法
SI3458456T1 (sl) 2016-05-18 2021-04-30 Loxo Oncology, Inc. Priprava (S)-N-(5-((R)-2-(2,5-difluorofenil) pirolidin-1-il) pirazolo (1,5-A) pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida
WO2017201156A1 (en) 2016-05-18 2017-11-23 Duke University Method of treating kras wild-type metastatic colorectal cell carcinoma using cabozantinib plus panitumumab
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
EP3700576A1 (en) 2017-10-26 2020-09-02 Array Biopharma Inc. Formulations of a macrocyclic trk kinase inhibitor

Also Published As

Publication number Publication date
HRP20230271T1 (hr) 2023-06-09
CA2967951A1 (en) 2016-05-19
MX2020011079A (es) 2020-11-09
US10172861B2 (en) 2019-01-08
TWI767858B (zh) 2022-06-11
PH12017500900A1 (en) 2017-12-04
JP2017535550A (ja) 2017-11-30
US20180021342A1 (en) 2018-01-25
IL290905B1 (en) 2023-05-01
KR20170082628A (ko) 2017-07-14
CN113354649B (zh) 2024-12-10
EP3218380A1 (en) 2017-09-20
US20160137654A1 (en) 2016-05-19
FI3699181T3 (fi) 2023-03-28
ZA201703501B (en) 2021-09-29
EP3218380B1 (en) 2021-03-17
TW201625636A (zh) 2016-07-16
JP6914834B2 (ja) 2021-08-04
DK3699181T3 (da) 2023-03-20
AU2015346046B2 (en) 2020-06-25
SG11201703962XA (en) 2017-06-29
US9782414B2 (en) 2017-10-10
IL252270B (en) 2022-04-01
IL252270A0 (en) 2017-07-31
TW202206436A (zh) 2022-02-16
EP3699181B1 (en) 2023-03-01
MX376478B (es) 2025-03-07
US10285993B2 (en) 2019-05-14
AU2015346046A1 (en) 2017-06-08
PT3699181T (pt) 2023-04-05
PL3699181T3 (pl) 2023-05-22
US10799505B2 (en) 2020-10-13
SI3699181T1 (sl) 2023-06-30
JP2021169496A (ja) 2021-10-28
CR20170263A (es) 2017-10-18
RU2723990C2 (ru) 2020-06-18
BR112017010141A2 (pt) 2018-03-06
CL2017001249A1 (es) 2017-12-15
KR102649887B1 (ko) 2024-03-22
CN107428760B (zh) 2021-04-27
WO2016077841A1 (en) 2016-05-19
UA123044C2 (uk) 2021-02-10
HK1244483A1 (zh) 2018-08-10
RU2017120846A (ru) 2018-12-18
NZ731909A (en) 2023-11-24
US20180207162A1 (en) 2018-07-26
US10813936B2 (en) 2020-10-27
CN107428760A (zh) 2017-12-01
MX2017006412A (es) 2017-09-12
LT3699181T (lt) 2023-05-10
US20170165267A1 (en) 2017-06-15
EP3699181A1 (en) 2020-08-26
IL290905B2 (en) 2023-09-01
IL290905A (en) 2022-04-01
TWI746426B (zh) 2021-11-21
US20200000807A1 (en) 2020-01-02
CO2017005483A2 (es) 2017-11-30
RU2017120846A3 (OSRAM) 2019-05-08
CN113354649A (zh) 2021-09-07
ES2941630T3 (es) 2023-05-24
PH12021550809A1 (en) 2022-02-14
CA2967951C (en) 2023-11-07
HUE061448T2 (hu) 2023-07-28

Similar Documents

Publication Publication Date Title
US10813936B2 (en) 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
AU2017246554B2 (en) 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
TR201807101T4 (tr) İmidazo[4,5-c]kinolin-2-on bileşikler ve kanserin tedavi edilmesinde kullanımları.
KR20210102261A (ko) Am2 수용체 억제제로서의 복소환식 스피로-화합물
HK40036794B (en) 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
HK40036794A (en) 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
RU2723990C9 (ru) Кристаллическая форма (s)-n-(5-((r)-2-(2,5-дифторфенил)-пирролидин-1-ил)-пиразоло[1,5-a]пиримидин-3-ил)-3-гидроксипирролидин-1-карбоксамида гидросульфата