[go: up one dir, main page]

MX386415B - Uso de (s)-n-(5-((r)-2-(2,5-difluorofenil) pirrolidin-1-il)- pirazolo [1,5-a] pirimidin-3-il) -3-hidroxipirrolidina-1- carboxamida para tratar cánceres pediátricos. - Google Patents

Uso de (s)-n-(5-((r)-2-(2,5-difluorofenil) pirrolidin-1-il)- pirazolo [1,5-a] pirimidin-3-il) -3-hidroxipirrolidina-1- carboxamida para tratar cánceres pediátricos.

Info

Publication number
MX386415B
MX386415B MX2018012165A MX2018012165A MX386415B MX 386415 B MX386415 B MX 386415B MX 2018012165 A MX2018012165 A MX 2018012165A MX 2018012165 A MX2018012165 A MX 2018012165A MX 386415 B MX386415 B MX 386415B
Authority
MX
Mexico
Prior art keywords
hydroxypyrrolidine
pyrazolo
difluorophenyl
pyrrolidin
pyrimidin
Prior art date
Application number
MX2018012165A
Other languages
English (en)
Other versions
MX2018012165A (es
Inventor
Mark Reynolds
Michael Cox
Nisha Nanda
SMITH Steven A
Original Assignee
Loxo Oncology 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 Loxo Oncology Inc filed Critical Loxo Oncology Inc
Publication of MX2018012165A publication Critical patent/MX2018012165A/es
Publication of MX386415B publication Critical patent/MX386415B/es

Links

Classifications

    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40—Cyclodextrins; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Physiology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Nutrition Science (AREA)
  • Inorganic Chemistry (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Un método para tratar un cáncer pediátrico en un sujeto que lo necesite. El método incluye administrar al sujeto una cantidad terapéuticamente efectiva de (S)-N-(5-((R)-2-(2,5-difluorofenil)pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida, o una sal farmacéuticamente aceptable de la misma, o una combinación de las mismas.
MX2018012165A 2016-04-04 2017-04-04 Uso de (s)-n-(5-((r)-2-(2,5-difluorofenil) pirrolidin-1-il)- pirazolo [1,5-a] pirimidin-3-il) -3-hidroxipirrolidina-1- carboxamida para tratar cánceres pediátricos. MX386415B (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201662318041P 2016-04-04 2016-04-04
US201662323437P 2016-04-15 2016-04-15
US201662329653P 2016-04-29 2016-04-29
US201662380773P 2016-08-29 2016-08-29
US201762449366P 2017-01-23 2017-01-23
PCT/US2017/025932 WO2017176744A1 (en) 2016-04-04 2017-04-04 Methods of treating pediatric cancers

Publications (2)

Publication Number Publication Date
MX2018012165A MX2018012165A (es) 2019-07-08
MX386415B true MX386415B (es) 2025-03-11

Family

ID=58610006

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2018012165A MX386415B (es) 2016-04-04 2017-04-04 Uso de (s)-n-(5-((r)-2-(2,5-difluorofenil) pirrolidin-1-il)- pirazolo [1,5-a] pirimidin-3-il) -3-hidroxipirrolidina-1- carboxamida para tratar cánceres pediátricos.

Country Status (28)

Country Link
EP (1) EP3439663B1 (es)
JP (1) JP7057343B2 (es)
KR (2) KR20180129911A (es)
CN (1) CN109310694A (es)
AU (1) AU2017246547B2 (es)
BR (1) BR112018070017A2 (es)
CA (1) CA3019661A1 (es)
CL (1) CL2018002807A1 (es)
DK (1) DK3439663T3 (es)
ES (1) ES2987501T3 (es)
FI (1) FI3439663T3 (es)
HR (1) HRP20241295T1 (es)
HU (1) HUE068542T2 (es)
IL (1) IL262005A (es)
LT (1) LT3439663T (es)
MA (1) MA44612B1 (es)
MX (1) MX386415B (es)
PH (1) PH12018502134A1 (es)
PL (1) PL3439663T3 (es)
PT (1) PT3439663T (es)
RS (1) RS65988B1 (es)
RU (1) RU2751636C2 (es)
SG (1) SG11201808676RA (es)
SI (1) SI3439663T1 (es)
TN (2) TN2018000338A1 (es)
UA (1) UA125025C2 (es)
WO (1) WO2017176744A1 (es)
ZA (1) ZA201806684B (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101853026B1 (ko) 2008-10-22 2018-04-27 어레이 바이오파마 인크. ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물
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
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
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
CN109354578A (zh) * 2018-12-06 2019-02-19 浙江师范大学 一种替尼中间体以及替尼的合成方法
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
CN110283858B (zh) * 2019-07-05 2024-01-26 尚科生物医药（上海）有限公司 生物催化制备(s)-2-(2,5-二氟苯基)吡咯烷的方法
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
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
CN111362854B (zh) * 2020-04-30 2021-04-27 安徽德信佳生物医药有限公司 一种拉洛替尼中间体的制备方法
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

Family Cites Families (126)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5844092A (en) 1994-03-18 1998-12-01 Genentech, Inc. Human TRK receptors and neurotrophic factor inhibitors
US5877016A (en) 1994-03-18 1999-03-02 Genentech, Inc. Human trk receptors and neurotrophic factor inhibitors
DK1292680T3 (da) 2000-06-22 2010-03-08 Genentech Inc Agonist-anti-TrkC monoklonale antistoffer
ITMI20021620A1 (it) 2002-07-23 2004-01-23 Novuspharma Spa Composto ad ativita' antitumorale
EP1597251B1 (en) 2003-02-20 2009-06-10 SmithKline Beecham Corporation Pyrimidine compounds
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
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
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
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
PE20060664A1 (es) 2004-09-15 2006-08-04 Novartis Ag Amidas biciclicas como inhibidores de cinasa
DE102005003687A1 (de) 2005-01-26 2006-07-27 Sphingo Tec Gmbh Immunoassay zur Bestimmung der Freisetzung von Neurotensin in die Zirkulation
WO2006087538A1 (en) 2005-02-16 2006-08-24 Astrazeneca Ab Chemical compounds
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
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.
UA95244C2 (ru) 2005-06-22 2011-07-25 Плексикон, Инк. Соединения и способ модулирования активности киназ, и показания для их применения
HRP20140218T4 (hr) 2005-08-25 2017-06-16 Creabilis Therapeutics S.P.A. Polimerni konjugati k-252a i njihovi derivati
WO2007057399A2 (en) 2005-11-15 2007-05-24 Boehringer Ingelheim International Gmbh Treatment of cancer with indole derivatives
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
EP1978958A4 (en) 2006-01-24 2009-12-02 Merck & Co Inc RET tyrosine kinase Inhibition
NZ572202A (en) 2006-03-27 2012-05-25 Nerviano Medical Sciences Srl Pyridyl- and pyrimidinyl-substituted pyrrole-, thiophene- and furane-derivatives as kinase inhibitors
EP2036557B1 (en) 2006-05-18 2015-10-21 Eisai R&D Management Co., Ltd. Antitumor agent for thyroid cancer
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
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.
PE20081581A1 (es) 2006-12-21 2008-11-12 Plexxikon Inc COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA
WO2008079909A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
RU2009122670A (ru) 2006-12-21 2011-01-27 Плекссикон, Инк. (Us) Соединения и способы для модуляции киназ и показания к их применению
US20080234267A1 (en) 2007-03-20 2008-09-25 Karen Elizabeth Lackey Compounds and Methods of Treatment
US8338417B2 (en) 2007-05-04 2012-12-25 Irm Llc Compounds and compositions as c-kit and PDGFR kinase inhibitors
EP2074118A2 (en) 2007-07-09 2009-07-01 AstraZeneca AB Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
SG183036A1 (en) 2007-07-17 2012-08-30 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
CA2693967A1 (en) 2007-07-19 2009-01-29 Schering Corporation Heterocyclic amide compounds as protein kinase inhibitors
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
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
JP5400791B2 (ja) 2007-12-04 2014-01-29 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 置換ジヒドロプテリジン−６−オン誘導体、その製造方法及びキナーゼ阻害剤としてのその使用
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
EP2254886B1 (en) 2008-03-28 2016-05-25 Nerviano Medical Sciences S.r.l. 3,4-dihydro-2h-pyrazino[1,2-a]indol-1-one derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
PE20091846A1 (es) 2008-05-19 2009-12-16 Plexxikon Inc DERIVADOS DE PIRROLO[2,3-d]-PIRIMIDINA COMO MODULADORES DE CINASAS
US8158636B2 (en) 2008-05-19 2012-04-17 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
BRPI0913031A2 (pt) 2008-05-23 2019-11-26 Novartis Ag derivados de quinolina e quinoxalinas como inibidores de proteína tirosina quinase, seus usos e processo de fabricação, bem como composições farmacêuticas e combinação que os compreende
EP2313411A1 (en) 2008-06-10 2011-04-27 Plexxikon, Inc. 5h-pyrr0l0 [2,3-b]pyrazine derivatives for kinase modulation, and indications therefor
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
JP5746032B2 (ja) 2008-09-19 2015-07-08 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ ３，４−ジヒドロ−２Ｈ−ピロロ［１，２−ａ］ピラジン−１−オン誘導体
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
WO2010058006A1 (en) 2008-11-24 2010-05-27 Nerviano Medical Sciences S.R.L. Cdk inhibitor for the treatment of mesothelioma
JO3265B1 (ar) 2008-12-09 2018-09-16 Novartis Ag مثبطات بيريديلوكسى اندولات vegf-r2 واستخدامها لعلاج المرض
WO2010111527A1 (en) 2009-03-26 2010-09-30 Plexxikon, Inc. Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use
ES2570756T3 (es) 2009-06-15 2016-05-20 Nerviano Medical Sciences Srl Derivados pirimidinilpirrolopiridinona sustituidos, proceso para su preparación y su uso como inhibidores de cinasa
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
WO2011092120A1 (en) 2010-01-29 2011-08-04 Nerviano Medical Sciences S.R.L. 6,7- dihydroimidazo [1,5-a] pyrazin-8 (5h) - one derivatives as protein kinase modulators
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
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
US8916577B2 (en) 2011-01-26 2014-12-23 Nerviano Medical Sciences S.R.L. Tricyclic derivatives, process for their preparation and their use as kinase inhibitors
CN103339134B (zh) 2011-01-26 2015-12-23 内尔维阿诺医学科学有限公司 三环吡咯并衍生物、它们的制备方法和它们作为激酶抑制剂的应用
JP5941069B2 (ja) 2011-02-07 2016-06-29 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼ調節のための化合物および方法、ならびにそれに対する適応症
JP6013375B2 (ja) 2011-02-24 2016-10-25 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤としてのチアゾリルフェニル−ベンゼンスルホンアミド誘導体
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
US9284298B2 (en) 2011-04-11 2016-03-15 Nerviano Medical Sciences S.R.L. Pyrazolyl-pyrimidine derivatives as kinase inhibitors
BR112013026137B1 (pt) 2011-04-19 2020-12-01 Nerviano Medical Sciences S.R.L pirimidinil-pirróis substituídos ativos como inibidores da quinase
CA2835478C (en) 2011-05-12 2019-02-05 Nerviano Medical Sciences S.R.L. Substituted indazole derivatives active as kinase inhibitors
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
JP6016915B2 (ja) 2011-07-28 2016-10-26 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤として活性なアルキニル置換ピリミジニルピロール
EP2788351B1 (en) 2011-10-07 2017-06-28 Nerviano Medical Sciences S.r.l. SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASE INHIBITORS
JP6063945B2 (ja) 2011-10-07 2017-01-18 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤としての４−アルキル置換３，４−ジヒドロピロロ［１，２−ａ］ピラジン−１（２Ｈ）−オン誘導体
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
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase 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
RU2019102203A (ru) 2012-07-11 2019-03-05 Блюпринт Медсинс Корпорейшн Ингибиторы рецептора фактора роста фибробластов
RU2666538C2 (ru) 2012-08-02 2018-09-11 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Замещенные пирролы, активные в качестве ингибиторов киназ
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
WO2014071358A2 (en) * 2012-11-05 2014-05-08 Foundation Medicine, Inc. Novel ntrk1 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
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
US9822118B2 (en) 2012-11-13 2017-11-21 Array Biopharma Inc. Bicyclic heteroaryl 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
WO2014078378A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl 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.
US9809578B2 (en) 2012-11-13 2017-11-07 Array Biopharma Inc. 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
RU2664541C2 (ru) 2012-11-13 2018-08-20 Эррэй Биофарма Инк. Бициклические соединения мочевины, тиомочевины, гуанидина и цианогуанидина, пригодные для лечения боли
WO2014078372A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl 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
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
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
US9499522B2 (en) 2013-03-15 2016-11-22 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
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
BR112015028845A2 (pt) 2013-05-30 2017-07-25 Plexxikon Inc compostos para a modulação da quinase e indicações da mesma
WO2015017533A1 (en) 2013-07-30 2015-02-05 Blueprint Medicines Corporation Ntrk2 fusions
US10875930B2 (en) 2013-07-30 2020-12-29 Blueprint Medicines Corporation PIK3C2G fusions
WO2015039006A1 (en) * 2013-09-16 2015-03-19 The General Hospital Corporation Methods of treating cancer
US9334263B2 (en) 2013-10-17 2016-05-10 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
WO2015057873A1 (en) 2013-10-17 2015-04-23 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
PT3395814T (pt) 2013-10-25 2022-07-27 Blueprint Medicines Corp Inibidores do recetor do fator de crescimento de fibroblastos
WO2015108992A1 (en) 2014-01-15 2015-07-23 Blueprint Medicines Corporation Heterobicyclic compounds and their use as fgfr4 receptor inhibitors
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
EP3132054B1 (en) 2014-04-18 2021-06-30 Blueprint Medicines Corporation Met fusions
WO2015161274A1 (en) 2014-04-18 2015-10-22 Blueprint Medicines Corporation Pik3ca fusions
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
US10378063B2 (en) 2014-06-10 2019-08-13 Blueprint Medicines Corporation RAF1 fusions
WO2015191667A1 (en) 2014-06-10 2015-12-17 Blueprint Medicines Corporation Pkn1 fusions
EP3169808B1 (en) 2014-07-17 2019-05-22 Blueprint Medicines Corporation Trio:tert fusion in cancer
US10370724B2 (en) 2014-07-17 2019-08-06 Blueprint Medicines Corporation PRKC fusions
WO2016011141A1 (en) 2014-07-17 2016-01-21 Blueprint Medicines Corporation Fgr fusions
US9688680B2 (en) 2014-08-04 2017-06-27 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
TWI560185B (en) 2014-08-18 2016-12-01 Ono Pharmaceutical Co Acid addition salt of trk inhibitor compound
CA2967125C (en) 2014-11-14 2022-10-25 Nerviano Medical Sciences S.R.L. 6-amino-7-bicyclo-7-deaza-purine derivatives as protein kinase inhibitors
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
EP3221700B1 (en) 2014-11-18 2022-06-22 Blueprint Medicines Corporation Prkacb fusions
MA43943A (fr) 2015-05-29 2018-12-12 Ignyta Inc Compositions et procédés pour traiter des patients avec des cellules mutantes rtk
TN2018000138A1 (en) * 2015-10-26 2019-10-04 Array Biopharma Inc Point mutations in trk inhibitor-resistant cancer and methods relating to the same

Also Published As

Publication number Publication date
UA125025C2 (uk) 2021-12-29
JP2019510827A (ja) 2019-04-18
WO2017176744A1 (en) 2017-10-12
PH12018502134A1 (en) 2019-09-23
ES2987501T3 (es) 2024-11-15
RU2018138579A (ru) 2020-05-12
PL3439663T3 (pl) 2024-11-18
PT3439663T (pt) 2024-10-07
LT3439663T (lt) 2024-10-10
EP3439663A1 (en) 2019-02-13
BR112018070017A2 (pt) 2019-02-05
AU2017246547B2 (en) 2023-02-23
KR20180129911A (ko) 2018-12-05
TN2018000338A1 (en) 2020-01-16
MX2018012165A (es) 2019-07-08
NZ747140A (en) 2025-05-02
CN109310694A (zh) 2019-02-05
SI3439663T1 (sl) 2024-11-29
IL262005A (en) 2018-10-31
RU2018138579A3 (es) 2020-07-30
MA44612B1 (fr) 2024-09-30
JP7057343B2 (ja) 2022-04-19
MA44612A (fr) 2019-02-13
SG11201808676RA (en) 2018-11-29
CL2018002807A1 (es) 2019-03-01
HUE068542T2 (hu) 2025-01-28
RU2751636C2 (ru) 2021-07-15
DK3439663T3 (da) 2024-08-26
HRP20241295T1 (hr) 2024-12-06
ZA201806684B (en) 2025-05-28
WO2017176744A8 (en) 2018-12-13
FI3439663T3 (fi) 2024-08-28
RS65988B1 (sr) 2024-10-31
CA3019661A1 (en) 2017-10-12
TN2019000332A1 (en) 2021-05-07
EP3439663B1 (en) 2024-07-17
KR20210010652A (ko) 2021-01-27

Similar Documents

Publication Publication Date Title
MX386415B (es) Uso de (s)-n-(5-((r)-2-(2,5-difluorofenil) pirrolidin-1-il)- pirazolo [1,5-a] pirimidin-3-il) -3-hidroxipirrolidina-1- carboxamida para tratar cánceres pediátricos.
TN2018000335A1 (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
PH12021550809A1 (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
MX2020011653A (es) Métodos de tratamiento para el abuso de sustancias.
MX2014010590A (es) Terapia de combinacion para trastornos proliferativos.
MX2020008680A (es) Terapia de combinacion con apilimod y agentes glutamatergicos.
IL262964B (en) Preparation of (s)-n-(5-((r)-2-(5,2-difluorophenyl)pyrrolidine-1-yl)pyrazolo[5,1-a]pyrimidin-3-yl)-3-hydroxypyrrolidine- 1-carboxamide and their salts
MX2021004639A (es) Combinaciones de inhibidores de desmetilasa-1 especifica de lisina (lsd1) para uso en el tratamiento de tumores solidos.
EP4353747A3 (en) Combination of zanubrutinib with an anti-cd20 or an anti-pd-1 antibody for use in treating cancer
MX2018001659A (es) Terapia de combinacion que usa irinotecan liposomal y un inhibidor de poli(adp-ribosa) polimerasa (parp) para el tratamiento del cancer.
MX378579B (es) Uso de pridopidina para mejorar la funcion cognitiva y para tratamiento de enfermedad de alzheimer.
WO2018102687A3 (en) Combination therapy for treating cancer
PH12015502616A1 (en) Pharmaceutical combination comprising metformin and dihydroquercetin and its use for the treatment of cancer
MX2018010223A (es) Terapia combinada para tratamiento de cancer de ovario.
WO2018102261A3 (en) Boronic derivatives hydroxamates as anticancer agents
EA202191165A1 (ru) Элацестрант в комбинации с абемациклибом у женщин с раком молочной железы
MX2021011289A (es) Composiciones que comprenden moduladores de isoenzima m2 muscular de piruvato cinasa pkm2 y metodos de tratamiento que usan las mismas.
JOP20180089A1 (ar) طرق علاج سرطانات الأطفال
MX383514B (es) Pirrolo[2,3-d]piridazin-4-onas sustituidas y pirazolo[3,4-d]piridazin-4-onas como inhibidores de la proteína quinasa.
BR112022000734A2 (pt) Método para tratar câncer em um paciente, uso de composto 1, e, composto 1
TH1801006190A (th) สารประกอบสำหรับการผลิตสูตรผสมที่เป็นของเหลวสำหรับการรักษามะเร็งในเด็ก
JOP20180088B1 (ar) صيغ سائلة من (s)-n-(5-((r)-2-(2، 5-داي فلورو فينيل)-بيروليدين-1-يل)-بيرازولو[1، 5-a] بيريميدين-3-يل)-3-هيدروكسي بيروليدين-1-كربوكساميد
HK1233917A1 (en) Methods for treating cancer using tor kinase inhibitor combination therapy