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PE20190918A1 - Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret - Google Patents

Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret

Info

Publication number
PE20190918A1
PE20190918A1 PE2019000790A PE2019000790A PE20190918A1 PE 20190918 A1 PE20190918 A1 PE 20190918A1 PE 2019000790 A PE2019000790 A PE 2019000790A PE 2019000790 A PE2019000790 A PE 2019000790A PE 20190918 A1 PE20190918 A1 PE 20190918A1
Authority
PE
Peru
Prior art keywords
ring
pyridine
fluoros
saturated
nitrogen atoms
Prior art date
Application number
PE2019000790A
Other languages
English (en)
Inventor
Steven W Andrews
Sean Aronow
Barbara J Brandhuber
Adam Cook
Julia Haas
Yutong Jiang
Gabrielle R Kolakowski
Elizabeth A Mcfaddin
Megan L Mckenney
Oren T Mcnulty
Andrew T Metcalf
David A Moreno
Tony P Tang
Li Ren
James F Blake
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
Application filed by Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of PE20190918A1 publication Critical patent/PE20190918A1/es

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    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/4995—Pyrazines or piperazines forming part of bridged ring 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Pyridine Compounds (AREA)

Abstract

Se refiere a compuestos de pirazolo[1,5-A] piridina sustituidos de Formula (I) y sus sales y solvatos farmaceuticamente aceptables, en donde: X1, X2, X3 y X4 pueden ser CH, CF, CCH3 o N; A es H, CN, Cl, ciclopropilo, entre otros; B es H, C1-C6 alquilo opcionalmente sustituido con 1-3 fluoros, hidroxi C2-C6 alquilo en donde la porcion alquilo esta opcionalmente con 1-3 fluoros o un anillo de C3-C6 cicloalquilideno, entre otros; el anillo D es (i) un anillo heterociclico de 4-7 miembros saturados que tiene dos atomos de nitrogeno del anillo, (ii) un anillo heterociclico en puente de 7-9 miembros saturado que tiene dos atomos de nitrogeno, y un tercer heteroatomo que es O, (iii) un anillo heteroespirociclico de 7-11 miembros saturados que tiene dos atomos de nitrogeno, entre otros; E puede ser H, C1-C6 alquilo sustituido opcionalmente con 1-3 fluoros, entre otros. Son compuestos preferidos 4-(6-(bencilpiperazin-1-il) piridin-3-il)-6-hidroxipirazolo[1,5-a]piridin -3-carbonitrilo; (S)-6-(2,3-dihidroxipropoxi)-4-(6-(4-((6-metoxipiridin-3-il)metil)piperazin-1-il)piridin-3-il)pirazolo[1,5-a]piridin-3-carbonitrilo. Dichos compuestos van a modular la actividad de la quinasa redispuesta durante la transfeccion (RET) y son utiles en el tratamiento del cancer.
PE2019000790A 2016-10-10 2017-10-10 Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret PE20190918A1 (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201662406252P 2016-10-10 2016-10-10
US201762447850P 2017-01-18 2017-01-18
US201762491164P 2017-04-27 2017-04-27
US201762554817P 2017-09-06 2017-09-06
US201762566093P 2017-09-29 2017-09-29
PCT/US2017/055983 WO2018071447A1 (en) 2016-10-10 2017-10-10 Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors

Publications (1)

Publication Number Publication Date
PE20190918A1 true PE20190918A1 (es) 2019-06-26

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PE2019000790A PE20190918A1 (es) 2016-10-10 2017-10-10 Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret

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Country Link
US (8) US10112942B2 (es)
EP (2) EP3753939A1 (es)
JP (6) JP6776446B2 (es)
KR (1) KR102143899B1 (es)
CN (2) CN114163437B (es)
AU (1) AU2017342022B2 (es)
BR (1) BR112019007144B8 (es)
CA (1) CA3039760C (es)
CL (1) CL2019000941A1 (es)
CO (1) CO2019004650A2 (es)
CR (1) CR20190218A (es)
CY (1) CY1123201T1 (es)
DK (1) DK3523301T3 (es)
DO (1) DOP2019000090A (es)
EC (1) ECSP19032676A (es)
ES (1) ES2805087T3 (es)
HR (1) HRP20201008T1 (es)
HU (1) HUE051424T2 (es)
IL (2) IL265916B (es)
JO (1) JOP20190076B1 (es)
LT (1) LT3523301T (es)
MA (1) MA53675A (es)
MD (1) MD3523301T2 (es)
MX (2) MX376465B (es)
MY (1) MY195573A (es)
NZ (1) NZ752793A (es)
PE (1) PE20190918A1 (es)
PH (1) PH12019500775A1 (es)
PL (1) PL3523301T3 (es)
PT (1) PT3523301T (es)
RS (1) RS60536B1 (es)
SA (1) SA519401541B1 (es)
SG (1) SG11201903144PA (es)
SI (1) SI3523301T1 (es)
TN (1) TN2019000110A1 (es)
TW (1) TWI704148B (es)
UA (1) UA125030C2 (es)
WO (1) WO2018071447A1 (es)
ZA (1) ZA202004040B (es)

Families Citing this family (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2012013467A (es) 2010-05-20 2013-04-29 Array Biopharma Inc Compuestos macrociclicos como inhibidores de trk cinasa.
US10202365B2 (en) 2015-02-06 2019-02-12 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors
WO2017011776A1 (en) 2015-07-16 2017-01-19 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
RS65069B1 (sr) 2015-11-02 2024-02-29 Blueprint Medicines Corp Inhibitori ret-a
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
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
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
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
TWI876442B (zh) * 2017-10-10 2025-03-11 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
TWI783057B (zh) * 2017-10-10 2022-11-11 美商絡速藥業公司 製備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-甲腈的方法
EP3740490A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors
CA3087972C (en) 2018-01-18 2023-01-10 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
US11603374B2 (en) 2018-01-18 2023-03-14 Array Biopharma Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
ES2970041T3 (es) 2018-04-03 2024-05-24 Blueprint Medicines Corp Inhibidor de RET para su uso en el tratamiento del cáncer que tiene una alteración de RET
CN108658981A (zh) * 2018-06-01 2018-10-16 成都福柯斯医药技术有限公司 一种6-溴-4-甲氧基氢-吡唑[1,5-a]吡啶-3-甲腈的合成方法
CN112996794A (zh) 2018-09-10 2021-06-18 阿雷生物药品公司 作为ret激酶抑制剂的稠合杂环化合物
TW202028209A (zh) * 2018-09-27 2020-08-01 大陸商重慶複創醫藥研究有限公司 作為RET激酶抑制劑的取代的咪唑[1,2-a]吡啶和[1,2,4]三唑[1,5-a]吡啶化合物
KR20210070286A (ko) * 2018-09-30 2021-06-14 베이징 즈지엔진루이 셩우이야오 커지 요우시엔공스 치환된 피라졸 융합고리계 유도체 및 이의 제조 방법과 응용
JP7347853B2 (ja) * 2018-12-06 2023-09-20 深▲チェン▼市塔吉瑞生物医薬有限公司 置換ピラゾロ［１，５－ａ］ピリジン化合物、該化合物を含む組成物およびその使用
US12209085B2 (en) 2018-12-07 2025-01-28 Sunshine Lake Pharma Co., Ltd. RET inhibitors, pharmaceutical compositions and uses thereof
US12312348B2 (en) * 2018-12-07 2025-05-27 Sunshine Lake Pharma Co., Ltd. RET inhibitors, pharmaceutical compositions and uses thereof
AU2020226422B2 (en) * 2019-02-19 2025-07-31 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Heterocyclic compound, pharmaceutical composition comprising same, preparation method therefor, and use thereof
CN111635400A (zh) * 2019-03-02 2020-09-08 察略盛医药科技(上海)有限公司 吡唑并[1,5-a]吡啶类衍生物、及其制备方法和用途
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
US12297197B2 (en) * 2019-04-03 2025-05-13 Guangzhou Baiyunshan Pharmaceutical Holdings Co., Ltd. Baiyunshan Pharmaceutical General Factory Pyrazolopyridine compound as RET inhibitor and application thereof
WO2020207941A1 (en) * 2019-04-09 2020-10-15 F. Hoffmann-La Roche Ag Heterocyclic compounds as inhibitors of monoacylglycerol lipase (magl)
CN116444515A (zh) 2019-05-14 2023-07-18 上海翰森生物医药科技有限公司 含二并环类衍生物抑制剂、其制备方法和应用
CN111961034A (zh) * 2019-05-20 2020-11-20 浙江同源康医药股份有限公司 用作ret激酶抑制剂的化合物及其应用
US20220220128A1 (en) * 2019-06-10 2022-07-14 Js Innopharm (Shanghai) Ltd Heterocyclic compounds as kinase inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof
GB201908511D0 (en) 2019-06-13 2019-07-31 Adorx Therapeutics Ltd Hydroxamate compounds
US11666570B2 (en) * 2019-07-11 2023-06-06 The Board Of Trustees Of The Leland Stanford Junior University Diagnosis and regulation of epidermal differentiation and cancer cell activity
EP3998265A4 (en) * 2019-07-12 2022-11-16 Shouyao Holdings (Beijing) Co., Ltd. SELECTIVE RET INHIBITOR, METHOD FOR PREPARATION AND USE
KR20220042293A (ko) * 2019-08-05 2022-04-05 베이징 즈지엔진루이 셩우이야오 커지 요우시엔공스 질소 함유 다환 축합 고리계 화합물, 이의 약학 조성물, 제조 방법 및 용도
CN112442050B (zh) * 2019-09-04 2024-08-09 广东东阳光药业股份有限公司 一种ret抑制剂、其药物组合物及其用途
WO2021057970A1 (zh) * 2019-09-29 2021-04-01 广东东阳光药业有限公司 一种ret抑制剂、其药物组合物及其用途
CN112574235B (zh) * 2019-09-29 2024-01-16 广东东阳光药业股份有限公司 一种ret抑制剂、其药物组合物及其用途
JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
WO2021088911A1 (zh) * 2019-11-08 2021-05-14 杭州邦顺制药有限公司 作为ret激酶抑制剂的3、6二氮杂双环[3.1.1]庚烷衍生物
CN112851664B (zh) * 2019-11-12 2024-03-29 浙江海正药业股份有限公司 吡唑[1,5-a]吡啶-3-腈化合物及其在医药上的用途
CN112939967B (zh) * 2019-12-11 2024-08-27 深圳众格生物科技有限公司 吡唑并[1,5-a]吡啶类化合物及其制备方法和应用
CN111004257B (zh) * 2019-12-24 2021-06-29 武汉九州钰民医药科技有限公司 制备RET抑制剂Selpercatinib的方法
CN113045569B (zh) * 2019-12-27 2022-04-19 浙江同源康医药股份有限公司 用作ret激酶抑制剂的化合物及其应用
CN113121524B (zh) 2019-12-31 2023-04-25 南京创济生物医药有限公司 杂环亚砜亚胺化合物及其中间体、制备方法和应用
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN111269229B (zh) * 2020-03-27 2021-02-12 苏州信诺维医药科技有限公司 一种治疗癌症的化合物
CN111285887B (zh) * 2020-03-27 2020-11-17 苏州信诺维医药科技有限公司 一种螺环化合物
CN111410662B (zh) * 2020-03-27 2020-12-29 苏州信诺维医药科技有限公司 一种酪氨酸激酶抑制剂
CN111233899B (zh) * 2020-03-27 2020-12-29 苏州信诺维医药科技有限公司 一种ret抑制剂
CN113527291B (zh) * 2020-04-13 2025-07-22 广东东阳光药业股份有限公司 Ret抑制剂、其药物组合物及其用途
CN113527290B (zh) * 2020-04-13 2025-07-22 广东东阳光药业股份有限公司 一种ret抑制剂、其药物组合物及其用途
CN113527292B (zh) * 2020-04-13 2025-07-22 广东东阳光药业股份有限公司 一种ret抑制剂、其药物组合物及其用途
TWI865765B (zh) * 2020-04-17 2024-12-11 美商絡速藥業公司 結晶ret抑制劑
CN113620945B (zh) * 2020-05-07 2024-08-23 广东东阳光药业股份有限公司 Ret抑制剂、其药物组合物及其在药物中的应用
BR112022024382A2 (pt) 2020-05-29 2023-05-02 Blueprint Medicines Corp Formas sólidas de pralsetinibe
CN113880865A (zh) * 2020-07-01 2022-01-04 上海艾力斯医药科技股份有限公司 吡唑[1,5-a]吡啶类化合物及其制备方法与应用
WO2022020279A1 (en) 2020-07-21 2022-01-27 Teva Pharmaceuticals International Gmbh Solid state forms of selpercatinib and process for preparation thereof
WO2022032026A1 (en) 2020-08-05 2022-02-10 C4 Therapeutics, Inc. Compounds for targeted degradation of ret
EP4201936A4 (en) * 2020-08-20 2024-02-21 Jiangsu Chia Tai Fenghai Pharmaceutical Co., Ltd. HETEROAROMATIC RING COMPOUND AS A RET KINASE INHIBITOR AND PRODUCTION AND USE THEREOF
WO2022046867A1 (en) 2020-08-25 2022-03-03 Loxo Oncology, Inc. Osimertinib and selpercatinib combinations for the treatment of egfr- and ret-associated cancers
CN114249724B (zh) * 2020-09-25 2023-05-26 鲁南制药集团股份有限公司 一种唑吡坦中间体的制备方法
WO2022069357A1 (en) 2020-10-01 2022-04-07 Sandoz Ag Crystalline form of selpercatinib
EP4245757A4 (en) * 2020-11-13 2024-10-09 Shanghai Hansoh Biomedical Co., Ltd. Crystal form of free base of inhibitor containing bicyclic ring derivative and preparation method and application of crystal form
CN114478586A (zh) * 2020-11-13 2022-05-13 上海翰森生物医药科技有限公司 一种含二并环类衍生物抑制剂盐或晶型及其制备方法和应用
CN114621256A (zh) * 2020-12-11 2022-06-14 深圳众格生物科技有限公司 吡唑并[1,5-a]吡啶类化合物及其制备方法和应用
TW202237118A (zh) 2020-12-14 2022-10-01 美商絡速藥業公司 用於預防腦轉移之組合物及方法
AU2021402927A1 (en) 2020-12-18 2023-06-29 Loxo Oncology, Inc. Ret inhibitor combination therapy for treating cancer
TW202237086A (zh) 2020-12-18 2022-10-01 美商絡速藥業公司 以ret抑制劑及鉑劑治療癌症之方法
TWI818424B (zh) * 2021-02-08 2023-10-11 大陸商北京志健金瑞生物醫藥科技有限公司 含氮多環稠環類化合物，其藥物組合物、製備方法和用途
CN113321668A (zh) * 2021-06-21 2021-08-31 江苏慧聚药业有限公司 塞尔帕替尼的合成
CN115594678B (zh) * 2021-07-09 2024-11-15 北京志健金瑞生物医药科技有限公司 含氮多环稠环类化合物的制备方法及其中间体和用途
CN113387947B (zh) * 2021-07-12 2022-07-01 中国科学院成都生物研究所 调节雌激素受体合成活性的吡唑并吡啶衍生物
US20230233691A1 (en) 2021-10-22 2023-07-27 University Of Houston System Methods and compositions for treating chronic inflammatory injury, metaplasia, dysplasia and cancers of epithelial tissues
US20230183266A1 (en) * 2021-12-13 2023-06-15 Loxo Oncology, Inc. Crystalline forms of ret inhibitor and preparation thereof
JP2025525917A (ja) * 2022-08-03 2025-08-07 ブリストル－マイヤーズ スクイブ カンパニー Ｒｅｔタンパク質を調節するための化合物
AU2023329563A1 (en) 2022-08-24 2025-02-27 Toray Industries, Inc. Medicament for treatment and/or prevention of cancer
CN117229292B (zh) * 2022-10-18 2025-08-15 药雅科技(上海)有限公司 Ret抑制剂的制备及其应用
CR20250458A (es) 2023-03-30 2025-11-21 Revolution Medicines Inc Composiciones para inducir la hidrólisis de ras gtp y sus usos
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
CN119504796A (zh) * 2024-11-20 2025-02-25 南通大学附属医院 一种具有抗肿瘤活性的化合物及其应用

Family Cites Families (262)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4783443A (en) 1986-03-03 1988-11-08 The University Of Chicago Amino acyl cephalosporin derivatives
US5877016A (en) 1994-03-18 1999-03-02 Genentech, Inc. Human trk receptors and neurotrophic factor inhibitors
US5844092A (en) 1994-03-18 1998-12-01 Genentech, Inc. Human TRK receptors and neurotrophic factor inhibitors
TR199802252T2 (xx) 1996-05-08 1999-02-22 Biogen, Inc N�ral ve renal geli�menin uyar�lmas� i�in ret ligand� (RetL)
US6677135B1 (en) 1996-05-08 2004-01-13 Biogen, Inc. Ret ligand (RetL) for stimulating neutral and renal growth
US6682921B1 (en) 1996-08-21 2004-01-27 New York University Crystals of the tyrosine kinase domain of non-insulin receptor tyrosine kinases
US6531152B1 (en) 1998-09-30 2003-03-11 Dexcel Pharma Technologies Ltd. Immediate release gastrointestinal drug delivery system
AU7103900A (en) 1999-09-01 2001-03-26 Biogen, Inc. Ret ligand 5 (retl5) compositions and uses thereof
FI20000403A0 (fi) 2000-02-22 2000-02-22 Hannu Sariola GDNF perhesukuisten yhdisteiden käyttö kivessyövän hoitoon tarkoitettujen tuotteiden valmistamiseksi
CA2412494C (en) 2000-06-22 2012-10-23 Genentech, Inc. Agonist anti-trk-c monoclonal antibodies
WO2003020698A2 (en) 2001-09-06 2003-03-13 Prochon Biotech Ltd. Protein tyrosine kinase inhibitors
US7466344B2 (en) 2002-06-07 2008-12-16 Scimeasure Analytical Systems, Inc. High-speed low noise CCD controller
ITMI20021620A1 (it) 2002-07-23 2004-01-23 Novuspharma Spa Composto ad ativita' antitumorale
BR0312873A (pt) 2002-07-24 2005-06-28 Univ Cincinnati 4-(4-metilpiperazin-1-ilmetil)-n-[4-metil-3-(4-piridin-3-il) pirimidin-2-ilamino)fenil] benzamida para tratamento de doenças associadas com ret cinase mutante
DE602004021472D1 (en) 2003-02-20 2009-07-23 Smithkline Beecham Corp Pyrimiidinverbindungen
JP2005106669A (ja) 2003-09-30 2005-04-21 Olympus Corp 生体関連物質の反応・測定システム
US20090143399A1 (en) 2003-10-14 2009-06-04 Arizona Board Of Regents On Behalf Of The University Of Arizona Protein Kinase Inhibitors
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
CA2546117A1 (en) 2003-11-21 2005-06-16 Novartis Ag 1h-imidazoquinoline derivatives as protein kinase inhibitors
EP1689376A2 (en) 2003-11-28 2006-08-16 Novartis AG Diaryl urea derivatives in the treatment of protein kinase dependent diseases
SI1696920T1 (sl) 2003-12-19 2015-02-27 Plexxikon Inc. Spojine in postopki za razvoj modulatorjev ret
GB0330043D0 (en) 2003-12-24 2004-01-28 Pharmacia Italia Spa Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions comprising them
GB0330042D0 (en) 2003-12-24 2004-01-28 Pharmacia Italia Spa Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions them
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
AR049769A1 (es) 2004-01-22 2006-09-06 Novartis Ag Derivados de pirazolo(1,5-a)pirimidin 7-il-amina para utilizarse en el tratamiento de enfermedades dependientes de la quinasa de proteina
WO2005099363A2 (en) 2004-03-26 2005-10-27 Whitehead Institute For Biomedical Research Methods of diagnosing, preventing and treating cancer metastasis
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
TW200615268A (en) 2004-08-02 2006-05-16 Osi Pharm Inc Aryl-amino substituted pyrrolopyrimidine multi-kinase inhibiting compounds
PE20060664A1 (es) 2004-09-15 2006-08-04 Novartis Ag Amidas biciclicas como inhibidores de cinasa
WO2006050076A1 (en) 2004-10-29 2006-05-11 Janssen Pharmaceutica, N.V. Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
DE102005003687A1 (de) 2005-01-26 2006-07-27 Sphingo Tec Gmbh Immunoassay zur Bestimmung der Freisetzung von Neurotensin in die Zirkulation
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
EP1848506A2 (en) 2005-02-18 2007-10-31 Attenuon, LLC Pyrimidine-fused diazepine derivatives and indole-fused pteridines
GB0507575D0 (en) * 2005-04-14 2005-05-18 Novartis Ag Organic compounds
CA2604787A1 (en) 2005-04-15 2006-10-26 Cylene Pharmaceuticals, Inc. Quinobenzoxazine analogs and methods of using thereof
AU2006248780B2 (en) 2005-05-16 2010-06-03 Astrazeneca Ab Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors
WO2006128042A2 (en) 2005-05-26 2006-11-30 The Johns Hopkins University Methods of identifying mutations in nucleic acid
EP1896462A2 (en) 2005-05-31 2008-03-12 The Pfahl Family Trust (Dated 9 July 1996) Substituted biarylheterocycle derivatives as protein kinase inhibitors for the treatment of cancer and other diseases
WO2006130673A1 (en) 2005-05-31 2006-12-07 Janssen Pharmaceutica, N.V. 3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders
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.
MY153898A (en) 2005-06-22 2015-04-15 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
GB0515026D0 (en) 2005-07-21 2005-08-31 Novartis Ag Organic compounds
ES2444003T5 (es) 2005-08-25 2017-07-05 Creabilis Therapeutics S.P.A. Conjugados poliméricos de K-252A y sus derivados
EP1948647A1 (en) 2005-11-03 2008-07-30 SGX Pharmaceuticals, Inc. Pyrimidinyl-thiophene kinase modulators
US20070149523A1 (en) 2005-11-14 2007-06-28 Jan Ehlert Thiazole Analogues and Uses Thereof
EP1785420A1 (en) 2005-11-14 2007-05-16 4Sc Ag Thiazole analogues and uses thereof
WO2007057399A2 (en) 2005-11-15 2007-05-24 Boehringer Ingelheim International Gmbh Treatment of cancer with indole derivatives
WO2007057397A1 (en) 2005-11-15 2007-05-24 Boehringer Ingelheim International Gmbh Treatment of cancer
GB0524436D0 (en) 2005-11-30 2006-01-11 Novartis Ag Organic compounds
EP1963316A2 (en) 2005-12-08 2008-09-03 Novartis AG Pyrazolo[1,5-a]pyridine-3-carboxylic acids as ephb and vegfr2 kinase inhibitors
US8399442B2 (en) 2005-12-30 2013-03-19 Astex Therapeutics Limited Pharmaceutical compounds
EP1978958A4 (en) 2006-01-24 2009-12-02 Merck & Co Inc RET tyrosine kinase Inhibition
DK1973910T3 (da) 2006-01-27 2013-08-12 Shanghai Hengrui Pharm Co Ltd Pyrrolo[3,2-c]pyridin-4-on-2-indolinon-proteinkinaseinhibitorer
AU2007227602A1 (en) 2006-03-16 2007-09-27 Novartis Ag Heterocyclic organic compounds for the treatment of in particular melanoma
KR101449057B1 (ko) 2006-03-17 2014-10-10 암비트 바이오사이언시즈 코포레이션 질환 치료용 이미다졸로티아졸 화합물
US8263604B2 (en) 2006-03-27 2012-09-11 Nerviano Medical Sciences S.R.L. Pyridyl- and pyrimidinyl-substituted pyrrole-, thiophene- and furane-derivatives as kinase inhibitors
KR20080109095A (ko) 2006-05-15 2008-12-16 아이알엠 엘엘씨 Ｆｇｆ 수용체 키나제 억제제를 위한 조성물 및 방법
CA2652442C (en) 2006-05-18 2014-12-09 Eisai R & D Management Co., Ltd. Antitumor agent for thyroid cancer
US8063225B2 (en) 2006-08-14 2011-11-22 Chembridge Corporation Tricyclic compound derivatives useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders
EP2067039A2 (en) 2006-09-12 2009-06-10 Novartis Forschungsstiftung, Zweigniederlassung Friedrich Miescher Institute for Biomedical Research Non-neuroendocrine cancer therapy
CN101553482B (zh) 2006-09-15 2013-11-20 艾科睿制药公司 激酶抑制剂化合物
US20120225057A1 (en) 2006-10-11 2012-09-06 Deciphera Pharmaceuticals, Llc Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases
EP1918291A1 (en) 2006-10-30 2008-05-07 Novartis AG 3-Aminocarbonyl-substituted fused pyrazolo-derivatives as protein kinase modulators
HUE035868T2 (en) 2006-11-15 2018-05-28 Ym Biosciences Australia Pty Inhibitors of kinase activity
WO2008079909A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
BRPI0720695A2 (pt) 2006-12-21 2014-02-18 Plexxikon Inc Compostos e métodos para modulação de cinase, e indicações para estes
US20080199426A1 (en) 2007-01-11 2008-08-21 Sukhatme Vikas P Methods and compositions for the treatment and diagnosis of vascular inflammatory disorders or endothelial cell disorders
CA2675979A1 (en) 2007-01-19 2008-07-24 Bayer Healthcare Llc Treatment of cancers having resistance to chemotherapeutic agents
US20080234267A1 (en) 2007-03-20 2008-09-25 Karen Elizabeth Lackey Compounds and Methods of Treatment
US20110189167A1 (en) 2007-04-20 2011-08-04 Flynn Daniel L Methods and Compositions for the Treatment of Myeloproliferative Diseases and other Proliferative Diseases
CN101720322A (zh) 2007-05-04 2010-06-02 Irm责任有限公司 作为c-kit和pdgfr激酶抑制剂的化合物和组合物
WO2008138184A1 (fr) 2007-05-14 2008-11-20 Shanghai Hengrui Pharmaceutical Co.Ltd. Dérivés de pyrrolo-azacycles, leur procédé de fabrication et leur utilisation en tant qu'inhibiteurs de protéine kinases
WO2009003136A1 (en) 2007-06-26 2008-12-31 Rigel Pharmaceuticals, Inc. Substituted pyrimidine-2, 4 -diamines for treating cell proliferative disorders
KR20100031639A (ko) 2007-07-09 2010-03-23 아스트라제네카 아베 증식성 질환의 치료용 삼중 치환된 피리미딘 유도체
WO2009012262A1 (en) 2007-07-16 2009-01-22 The Regents Of The University Of California Protein kinase modulating compounds and methods for making and using them
MX2010000617A (es) 2007-07-17 2010-05-17 Plexxikon Inc Compuestos y metodos para modulacion de cinasa, e indicaciones de estos.
AU2008279776B2 (en) 2007-07-19 2013-05-23 Merck Sharp & Dohme Corp. Heterocyclic amide compounds as protein kinase inhibitors
CA2693901C (en) 2007-07-20 2015-12-29 Nerviano Medical Sciences S.R.L. Substituted indazole derivatives active as kinase inhibitors
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
ES2547229T3 (es) 2007-08-07 2015-10-02 Purdue Research Foundation Inhibidores de cinasa y usos de los mismos
EP2025678A1 (en) 2007-08-17 2009-02-18 Oncalis AG Pyrazolo[3,4-d]pyrimidine compounds and their use as modulators of protein kinase
WO2009042646A1 (en) 2007-09-24 2009-04-02 Curis, Inc. Anti-proliferative agents
MX2010004494A (es) 2007-10-23 2010-08-30 Novartis Ag Uso de anticuerpos de trkb para el tratamiento de trastornos respiratorios.
US8598172B2 (en) 2007-12-04 2013-12-03 Nerviano Medical Sciences S.R.L. Substituted dihydropteridin-6-one derivatives, process for their preparation and their use as kinase inhibitors
CN101459004B (zh) 2007-12-14 2011-02-09 深圳富泰宏精密工业有限公司 电子装置的按键面板结构及制造该按键面板结构的方法
PE20091326A1 (es) 2008-01-17 2009-09-18 Irm Llc Anticuerpos anti-trkb mejorados
JP2009203226A (ja) 2008-01-31 2009-09-10 Eisai R & D Management Co Ltd ピリジン誘導体およびピリミジン誘導体を含有するレセプターチロシンキナーゼ阻害剤
TW200942537A (en) 2008-02-01 2009-10-16 Irm Llc Compounds and compositions as kinase inhibitors
WO2009103076A1 (en) 2008-02-15 2009-08-20 Oxigene, Inc. Methods and compositions for enhancing the efficacy of rtk inhibitors
JP5628145B2 (ja) 2008-03-19 2014-11-19 ケムブリッジ・コーポレーション 新規チロシンキナーゼ阻害剤
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
WO2009143018A2 (en) 2008-05-19 2009-11-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
GEP20125502B (en) 2008-05-23 2012-04-25 Novartis Ag Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors
WO2009155052A1 (en) * 2008-05-28 2009-12-23 Wyeth 3-substituted-1h-pyrrolo[2,3-b]pyridine and 3-substituted-1h-pyrrolo[3,2-b]pyridine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
JP5767965B2 (ja) 2008-06-10 2015-08-26 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼを調節する５ｈ−ピロロ［２，３−ｂ］ピラジン誘導体、およびその適応症
EP2303890A4 (en) 2008-06-19 2012-04-11 Progenics Pharm Inc INHIBITORS OF PHOSPHATIDYLINOSITE-3-KINASE
EP2313091A4 (en) 2008-07-14 2012-04-04 Univ Kingston PHARMACEUTICAL COMPOSITIONS WITH RET-HEMMERN AND METHOD FOR THE TREATMENT OF CANCER
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
KR101246656B1 (ko) 2008-09-01 2013-03-25 샤프 가부시키가이샤 유기 일렉트로루미네센스 패널, 유기 일렉트로루미네센스 디스플레이, 유기 일렉트로루미네센스 조명 및 그들의 제조 방법
WO2010028254A2 (en) 2008-09-05 2010-03-11 Auspek Pharmaceuticals, Inc. Substituted quinazoline inhibitors of growth factor receptor tyrosine kinases
EP2161271A1 (en) 2008-09-08 2010-03-10 Università Degli Studi Di Milano - Bicocca Alpha-carboline inhibitors of NMP-ALK, RET, and Bcr-Abl
ES2536730T3 (es) 2008-09-19 2015-05-28 Nerviano Medical Sciences S.R.L. Derivados de 3,4-dihidro-2H-pirrolo[1,2-a]pirazin-1-ona
SI2350075T1 (sl) 2008-09-22 2014-06-30 Array Biopharma, Inc. Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji
EP2331530B8 (en) 2008-09-26 2013-12-25 National Health Research Institutes Fused multicyclic compounds as protein kinase inhibitors
ES2900243T3 (es) 2008-10-22 2022-03-16 Array Biopharma Inc Compuestos de pirazolo[1,5-a]pirimidina sustituidos como inhibidores de trk quinasa
WO2010054058A1 (en) 2008-11-06 2010-05-14 Ambit Bioscience Corporation Imidazolothiazole compounds as modulators of protein kinase
CN102223885B (zh) 2008-11-24 2013-04-03 内尔维阿诺医学科学有限公司 用于治疗间皮瘤的cdk抑制剂
KR101061599B1 (ko) 2008-12-05 2011-09-02 한국과학기술연구원 비정상 세포 성장 질환의 치료를 위한 단백질 키나아제 저해제인 신규 인다졸 유도체, 이의 약학적으로 허용가능한염 및 이를 유효성분으로 함유하는 약학적 조성물
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
US8492374B2 (en) 2009-04-29 2013-07-23 Industrial Technology Research Institute Azaazulene compounds
SI3009428T1 (en) 2009-05-08 2018-04-30 Astellas Pharma Inc. DIAMINO HETEROCYCLIC CARBOSAMIDE COMPOUNDS
EP2440058A4 (en) 2009-06-12 2012-11-21 Dana Farber Cancer Inst Inc MELTED HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF
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
PE20170003A1 (es) 2009-08-17 2017-03-15 Intellikine Llc Compuestos heterociclicos y usos de los mismos
KR101256018B1 (ko) 2009-08-20 2013-04-18 한국과학기술연구원 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물
FR2951172B1 (fr) * 2009-10-13 2014-09-26 Pf Medicament Derives pyrazolopyridines en tant qu'agent anticancereux
KR101147550B1 (ko) 2009-10-22 2012-05-17 한국과학기술연구원 단백질 키나아제 저해활성을 가지는 2,7-치환된 티에노［3,2-ｄ］피리미딘 화합물
KR101116756B1 (ko) 2009-10-27 2012-03-13 한국과학기술연구원 단백질 키나아제 저해활성을 갖는 신규의 1,6-치환된 인돌 화합물
KR101690358B1 (ko) 2009-10-29 2017-01-09 제노스코 키나아제 억제제
MX2012005332A (es) 2009-11-13 2012-10-15 Oscotec Inc Inhibidores de cinasa.
KR101094446B1 (ko) 2009-11-19 2011-12-15 한국과학기술연구원 단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노［3,2-ｄ］피리미딘 화합물
EP2937345B1 (en) 2009-12-29 2018-03-21 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
US8772279B2 (en) 2010-01-29 2014-07-08 Nerviano Medical Sciences S.R.L. 6,7-dihydroimidazo[1,5-a]pyrazin-8(5H)-one derivatives as protein kinase modulators
KR101483215B1 (ko) 2010-01-29 2015-01-16 한미약품 주식회사 단백질 키나아제 저해활성을 갖는 비시클릭 헤테로아릴 유도체
AU2011210116B2 (en) 2010-01-29 2014-02-06 Catholic University Industry Academic Cooperation Foundation Thieno[3,2-d]pyrimidine derivatives having inhibitory activity on protein kinases
EP2536414B1 (en) 2010-02-18 2016-07-13 INSERM (Institut National de la Santé et de la Recherche Médicale) Method for preventing cancer metastasis
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
MX2012013467A (es) 2010-05-20 2013-04-29 Array Biopharma Inc Compuestos macrociclicos como inhibidores de trk cinasa.
US8637516B2 (en) 2010-09-09 2014-01-28 Irm Llc Compounds and compositions as TRK inhibitors
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
WO2012037155A2 (en) 2010-09-13 2012-03-22 Gtx, Inc. Tyrosine kinase inhibitors
WO2012047017A2 (ko) 2010-10-05 2012-04-12 크리스탈지노믹스(주) 2,3-디히드로-이소인돌-1-온 유도체 및 이를 포함하는 조성물
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
JP5925808B2 (ja) 2011-01-26 2016-05-25 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 三環式誘導体、これらの調製方法およびこれらのキナーゼ阻害剤としての使用
RU2591191C2 (ru) 2011-01-26 2016-07-10 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Трициклические пирроло производные, способ их получения и их применение в качестве ингибиторов киназы
CN102093421B (zh) 2011-01-28 2014-07-02 北京康辰药业有限公司 一种含磷取代基的喹啉类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
SI2672967T1 (sl) 2011-02-07 2018-12-31 Plexxikon Inc. Spojine in postopki za kinazno modulacijo in indikacije zanjo
ES2580961T3 (es) 2011-02-24 2016-08-30 Nerviano Medical Sciences S.R.L. Derivados Tiazolilfenil-bencenosulfonamido como Inhibidores de Cinasa
EA201391230A1 (ru) 2011-02-25 2014-01-30 АйАрЭм ЭлЭлСи Соединения и композиции в качестве ингибиторов trk
WO2012135631A1 (en) 2011-03-30 2012-10-04 Arrien Pharmaeuticals Llc Substituted 5-(pyrazin-2-yl)-1h-pyrazolo [3, 4-b] pyridine and pyrazolo [3, 4-b] pyridine derivatives as protein kinase inhibitors
EP2693881B1 (en) 2011-04-01 2019-09-04 University of Utah Research Foundation Substituted n-phenylpyrimidin-2-amine analogs as inhibitors of the axl kinase
EP2702055A1 (en) 2011-04-11 2014-03-05 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
AR086042A1 (es) * 2011-04-28 2013-11-13 Galapagos Nv Compuesto util para el tratamiento de enfermedades degenerativas e inflamatorias y composicion farmaceutica
SG194911A1 (en) 2011-05-12 2013-12-30 Nerviano Medical Sciences Srl Substituted indazole derivatives active as kinase inhibitors
RS55582B1 (sr) 2011-05-13 2017-06-30 Array Biopharma Inc Jedinjenja pirolidinil uree, pirolidinil tiouree i pirolidinil guanidina kao inhibitori trka kinaze
RU2477723C2 (ru) 2011-06-16 2013-03-20 Общество С Ограниченной Ответственностью "Фьюжн Фарма" Ингибиторы протеинкиназ (варианты), их применение для лечения онкологических заболеваний и фармацевтическая композиция на их основе
CN102827073A (zh) * 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
WO2013016720A2 (en) 2011-07-28 2013-01-31 Gerinda Therapeutics, Inc. Novel substituted biarylheterocycle derivatives as protein kinase inhibitors for the treatment of cancer and other diseases
US8912200B2 (en) 2011-07-28 2014-12-16 Nerviano Medical Sciences S.R.L. Alkynyl substituted pyrimidinyl-pyrroles active as kinases inhibitors
US9216172B2 (en) 2011-08-04 2015-12-22 National Cancer Center Method for determining effectiveness of cancer treatment by assessing the presence of a KIF5B-RET chimeric gene
EP2748192B2 (en) 2011-08-23 2022-04-20 Foundation Medicine, Inc. Kif5b-ret fusion molecules and uses thereof
WO2013077921A2 (en) 2011-09-02 2013-05-30 The Regents Of The University Of California Substituted pyrazolo[3,4-d]pyrimidines and uses thereof
WO2013036232A2 (en) 2011-09-08 2013-03-14 Deciphera Pharmaceuticals, Llc Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases
US8846712B2 (en) * 2011-09-12 2014-09-30 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013042137A1 (en) 2011-09-19 2013-03-28 Aurigene Discovery Technologies Limited Bicyclic heterocycles as irak4 inhibitors
CN102408411B (zh) 2011-09-19 2014-10-22 北京康辰药业股份有限公司 一种含喹啉基的羟肟酸类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
ES2660265T3 (es) 2011-10-07 2018-03-21 Nerviano Medical Sciences S.R.L. Derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1(2h)-ona 4-alquil-sustituidos como inhibidores de cinasa
ES2639064T3 (es) 2011-10-07 2017-10-25 Nerviano Medical Sciences S.R.L. Derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1(2h)-ona sustituidos como inhibidores de cinasa
AU2012339753A1 (en) 2011-11-14 2014-06-19 Tesaro, Inc. Modulating certain tyrosine kinases
TW201335372A (zh) 2011-11-30 2013-09-01 Nat Cancer Ct 誘導惡性幹細胞
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
US9156852B2 (en) 2011-12-30 2015-10-13 Hanmi Pharm. Co., Ltd Thieno[3,2-D]pyrimidine derivatives having inhibitory activity for protein kinases
JP2015109806A (ja) 2012-03-22 2015-06-18 アステラス製薬株式会社 新規ｒｅｔ融合体の検出法
US9242977B2 (en) 2012-04-26 2016-01-26 Ono Pharmaceutical Co., Ltd. Trk-inhibiting compound
JP2015516439A (ja) 2012-05-10 2015-06-11 シンタ ファーマシューティカルズ コーポレーション Ｈｓｐ９０阻害化合物で癌を治療すること
EP2855460B1 (en) 2012-05-23 2017-11-08 Nerviano Medical Sciences S.r.l. Process for the preparation of n-[5-(3,5-difluoro-benzyl)-1h-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide
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
ES2916220T3 (es) 2012-07-11 2022-06-29 Blueprint Medicines Corp Inhibidores del receptor de factor de crecimiento de fibroblasto
EP2878672A4 (en) 2012-07-26 2016-02-17 Nat Cancer Ct FUSIONSGEN OF CEP55-GEN AND RET-GEN
US9688661B2 (en) 2012-08-02 2017-06-27 Nerviano Medical Sciences S.R.L. Substituted pyrroles active as kinases inhibitors
US20140121239A1 (en) 2012-09-07 2014-05-01 Exelixis, Inc. Method of treating lung adenocarcinoma
MX389105B (es) 2012-09-25 2025-03-20 Chugai Pharmaceutical Co Ltd Inhibidor de quinasas reordenadas durante la transfeccion (ret).
ES2755772T3 (es) 2012-11-07 2020-04-23 Nerviano Medical Sciences Srl Pirimidinil y piridinilpirrolopiridinonas sustituidas, proceso para su preparación y su uso como inhibidores de cinasas
SG11201503560TA (en) 2012-11-12 2015-06-29 Ignyta Inc Bendamustine derivatives and methods of using same
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
ES2664331T3 (es) 2012-11-13 2018-04-19 Array Biopharma, Inc. Compuestos de N-pirrolidinilo, N'-pirazolilurea, tiourea, guanidina y cianoguanidina como inhibidores de la cinasa Trka
WO2014078417A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078331A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-(arylalkyl)-n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9790178B2 (en) 2012-11-13 2017-10-17 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
CA2891334C (en) 2012-11-13 2021-10-19 Array Biopharma Inc. Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain
US9828360B2 (en) 2012-11-13 2017-11-28 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
WO2014078408A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
BR112015002626A2 (pt) 2012-11-29 2017-09-26 Yeda Res & Dev métodos para prevenção de metástases tumorais, tratamento e prognostico do câncer e identificação dos agentes que são inibidores da metástase putativa
CN103848785B (zh) 2012-12-04 2016-07-13 上海医药集团股份有限公司 一类氘代3-氰基喹啉类化合物、其药用组合物、制备方法及其用途
FR3000494B1 (fr) 2012-12-28 2015-08-21 Oribase Pharma Nouveaux derives d'azaindoles en tant qu'inhibiteurs de proteines kinases
FR3000492B1 (fr) 2012-12-28 2015-09-11 Oribase Pharma Nouveaux derives azaindole en tant qu'inhibiteurs multikinases
PT2940014T (pt) 2012-12-28 2018-11-28 Crystalgenomics Inc Derivado 2,3-di-hidro-isoindol-1-ona como supressor da quinase btk e composição farmacêutica incluindo o mesmo
FR3000493A1 (fr) 2012-12-28 2014-07-04 Oribase Pharma Nouveaux inhibiteurs de proteines kinases
TW201443037A (zh) * 2013-01-09 2014-11-16 Gilead Sciences Inc 治療用化合物
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
WO2014160524A1 (en) 2013-03-14 2014-10-02 The Trustees Of The University Of Pennsylvania Cardio- metabolic and cascular effects of glp-1 metabolites
WO2014160521A1 (en) 2013-03-15 2014-10-02 Blueprint Medicines Corporation Piperazine derivatives and their use as kit modulators
DK2970191T3 (en) 2013-03-15 2017-03-20 Glaxosmithkline Ip Dev Ltd PYRIDINE DERIVATIVES RIGHT (REARRANGED DURING TRANSFECTION) -KINASE INHIBITORS
US8937071B2 (en) 2013-03-15 2015-01-20 Glaxosmithkline Intellectual Property Development Limited Compounds as rearranged during transfection (RET) inhibitors
EP3842424B1 (en) * 2013-03-15 2024-12-11 The Trustees of Columbia University in the City of New York Map kinase modulators and uses thereof in the tretament of tauopathies
JP6397897B2 (ja) 2013-05-14 2018-09-26 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 ピロロ［２，３−ｄ］ピリミジン誘導体、その製造方法及びキナーゼ阻害剤としてのその使用
TW201533028A (zh) 2013-05-30 2015-09-01 Plexxikon Inc 用於激酶調節之化合物及其適應症
EP3027654B1 (en) 2013-07-30 2019-09-25 Blueprint Medicines Corporation Pik3c2g fusions
US10407509B2 (en) 2013-07-30 2019-09-10 Blueprint Medicines Corporation NTRK2 fusions
WO2015025866A1 (ja) 2013-08-20 2015-02-26 独立行政法人国立がん研究センター 肺がんで見出された新規融合遺伝子
SG11201601341QA (en) 2013-08-30 2016-03-30 Ambit Biosciences Corp Biaryl acetamide compounds and methods of use thereof
US9334263B2 (en) 2013-10-17 2016-05-10 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
SG11201602937UA (en) 2013-10-17 2016-05-30 Blueprint Medicines Corp Compositions useful for treating disorders related to kit
SMT202200292T1 (it) 2013-10-25 2022-09-14 Blueprint Medicines Corp Inibitori del recettore del fattore di crescita dei fibroblasti
GB201321146D0 (en) 2013-11-29 2014-01-15 Cancer Rec Tech Ltd Quinazoline compounds
US9801880B2 (en) 2013-12-02 2017-10-31 Bergenbio As Use of kinase inhibitors
WO2015108992A1 (en) 2014-01-15 2015-07-23 Blueprint Medicines Corporation Heterobicyclic compounds and their use as fgfr4 receptor inhibitors
US9714258B2 (en) 2014-01-24 2017-07-25 Tp Therapeutics, Inc. Diaryl macrocycles as modulators of protein kinases
CA3181899A1 (en) 2014-02-14 2015-08-20 Exelixis, Inc. Crystalline solid forms of n-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use
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
US20170044621A1 (en) 2014-04-18 2017-02-16 Blueprint Medicines Corporation Met fusions
EP3132056B1 (en) 2014-04-18 2021-11-24 Blueprint Medicines Corporation Pik3ca fusions
WO2015175788A1 (en) 2014-05-15 2015-11-19 Array Biopharma Inc. 1-((3s,4r)-4-(3-fluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)-3-(4-methyl-3-(2-methylpyrimidin-5-yl)-1-phenyl-1h-pyrazol-5-yl)urea as a trka kinase 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
US10370725B2 (en) 2014-07-17 2019-08-06 Blueprint Medicines Corporation FGR fusions
WO2016011147A1 (en) 2014-07-17 2016-01-21 Blueprint Medicines Corporation Prkc fusions
US10370723B2 (en) 2014-07-17 2019-08-06 Blueprint Medicines Corporation TERT fusions
US10065934B2 (en) 2014-07-17 2018-09-04 Sunshine Lake Pharma Co., Ltd. Substituted urea derivatives and pharmaceutical uses thereof
WO2016022569A1 (en) 2014-08-04 2016-02-11 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
CN106573913B (zh) 2014-08-18 2019-11-19 小野药品工业株式会社 抑制Trk的化合物的酸加成盐
JP2017527574A (ja) 2014-09-08 2017-09-21 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ ２−（４−（４−エトキシ−６−オキソ−１，６−ジヒドロピリジン−３−イル）−２−フルオロフェニル）−ｎ−（５−（１，１，１−トリフルオロ−２−メチルプロパン−２−イル）イソオキサゾール−３−イル）アセトアミドの結晶形
MY181913A (en) 2014-09-10 2021-01-14 Glaxosmithkline Ip Dev Ltd Pyridone derivatives as rearranged during transfection (ret) kinase inhibitors
MX381233B (es) 2014-09-10 2025-03-12 Glaxosmithkline Ip Dev Ltd Nuevos compuestos como inhibidores de reorganizado durante la transfección (ret).
TWI538914B (zh) 2014-10-03 2016-06-21 國立交通大學 蛋白質激酶之選擇性抑制劑、其醫藥組成物及其用途
WO2016075224A1 (en) * 2014-11-14 2016-05-19 Nerviano Medical Sciences S.R.L. 6-amino-7-bicyclo-7-deaza-purine derivatives as protein kinase inhibitors
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
EP3221700B1 (en) 2014-11-18 2022-06-22 Blueprint Medicines Corporation Prkacb fusions
EP3233840B1 (en) 2014-12-16 2018-11-21 Eudendron S.r.l. Heterocyclic derivatives modulating activity of certain protein kinases
US10202365B2 (en) 2015-02-06 2019-02-12 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors
KR101675984B1 (ko) 2015-02-23 2016-11-14 한양대학교 에리카산학협력단 티에노디아제핀 유도체 또는 이의 약학적으로 허용가능한 염, 및 이를 유효성분으로 포함하는 약학적 조성물
US20180045727A1 (en) 2015-03-03 2018-02-15 Caris Mpi, Inc. Molecular profiling for cancer
US10364247B2 (en) 2015-04-21 2019-07-30 Ruijin Hospital Affiliated To Shanghai Jiao Tong University School Of Medicine Preparation and use of novel protein kinase inhibitors
GB201512365D0 (en) 2015-07-15 2015-08-19 King S College London Novel therapy
WO2017011776A1 (en) 2015-07-16 2017-01-19 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
EP3120851A1 (en) 2015-07-21 2017-01-25 Pangaea Biotech S.L. 4-amino-6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)-pyrido[2,3-d]pyrimidin-7(8h)-one for treatment of solid cancers
KR101766194B1 (ko) 2015-08-07 2017-08-10 한국과학기술연구원 RET 키나아제 저해제인 신규 3-(이속사졸-3-일)-피라졸로[3,4-d]피리미딘-4-아민 화합물
WO2017027883A1 (en) 2015-08-13 2017-02-16 San Diego State University Research Foundation Atropisomerism for increased kinase inhibitor selectivity
MA41559A (fr) 2015-09-08 2017-12-26 Taiho Pharmaceutical Co Ltd Composé de pyrimidine condensé ou un sel de celui-ci
WO2017049462A1 (zh) 2015-09-22 2017-03-30 合肥中科普瑞昇生物医药科技有限公司 一类新型的flt3激酶抑制剂及其用途
CN105255927B (zh) 2015-09-30 2018-07-27 温州医科大学附属第一医院 一种kiaa1217-ret融合基因
RS65069B1 (sr) 2015-11-02 2024-02-29 Blueprint Medicines Corp Inhibitori ret-a
US20190002988A1 (en) 2015-12-08 2019-01-03 Boehringer Ingelheim International Gmbh Method of using a ret fusion gene as a biomarker to select non small cell lung cancer (nsclc) and thyroid cancer patients for a cancer treatment
WO2017122815A1 (ja) 2016-01-15 2017-07-20 公益財団法人がん研究会 新規融合体及びその検出法
TWI620748B (zh) 2016-02-05 2018-04-11 National Health Research Institutes 氨基噻唑化合物及其用途
WO2017145050A1 (en) 2016-02-23 2017-08-31 Glaxosmithkline Intellectual Property Development Limited Pyridylpyridone derivative useful as a ret kinase inhibitor in the treatment of ibs and cancer
DK3269370T3 (da) 2016-02-23 2020-04-06 Taiho Pharmaceutical Co Ltd Hidtil ukendt kondenseret pyrimidinforbindelse eller salt deraf
WO2017161269A1 (en) 2016-03-17 2017-09-21 Blueprint Medicines Corporation Inhibitors of ret receptor tyrosine kinases
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
PT3442535T (pt) * 2016-04-15 2022-09-05 Cancer Research Tech Ltd Compostos heterocíclicos como inibidores da ret quinase
HUE056135T2 (hu) 2016-04-15 2022-01-28 Cancer Research Tech Ltd RET kináz inhibitor heterociklusos vegyületek
TWI704148B (zh) * 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret

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