ECSP19032676A - 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
ECSP19032676A
ECSP19032676A ECSENADI201932676A ECDI201932676A ECSP19032676A EC SP19032676 A ECSP19032676 A EC SP19032676A EC SENADI201932676 A ECSENADI201932676 A EC SENADI201932676A EC DI201932676 A ECDI201932676 A EC DI201932676A EC SP19032676 A ECSP19032676 A EC SP19032676A
Authority
EC
Ecuador
Prior art keywords
ret kinase
inhibitors
pyrazole
pyridine compounds
compounds substituted
Prior art date
Application number
ECSENADI201932676A
Other languages
English (en)
Inventor
James F Blake
Barbara J Brandhuber
David A Moreno
Julia Haas
Megan L Mckenney
Adam Cook
Yutong Jiang
Steven W Andrews
Tony P Tang
Sean Aronow
Andrew T Metcalf
Elizabeth A Mcfaddin
Li Ren
Oren T Mcnulty
Gabrielle R Kolakowski
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 ECSP19032676A publication Critical patent/ECSP19032676A/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
    • A61K31/4985—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
    • A61K31/435—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
    • A61K31/496—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
    • A61K31/495—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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Pyridine Compounds (AREA)

Abstract

Se proporciona en la presente compuestos de la Fórmula I y estereoisómeros y sales o solvatos aceptables desde el punto de vista farmacéutico de estos, en donde A, B, X1, X2, X3, X4, Anillo D y E tienen los significados dados en la memoria descriptiva, que son inhibidores de quinasa RET y son útiles en el tratamiento y prevención de enfermedades que se pueden tratara con un inhibidor de quinasa RET, lo que incluye enfermedades y trastornos.
ECSENADI201932676A 2016-10-10 2019-05-09 Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret ECSP19032676A (es)

Applications Claiming Priority (5)

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

Publications (1)

Publication Number Publication Date
ECSP19032676A true ECSP19032676A (es) 2019-07-31

Family

ID=60153575

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSENADI201932676A ECSP19032676A (es) 2016-10-10 2019-05-09 Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret

Country Status (39)

Country Link
US (8) US10112942B2 (es)
EP (2) EP3753939A1 (es)
JP (5) JP6776446B2 (es)
KR (1) KR102143899B1 (es)
CN (2) CN114163437A (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) MX2020011250A (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 (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101852169B1 (ko) 2010-05-20 2018-04-26 어레이 바이오파마 인크. Trk 키나제 저해제로서의 매크로시클릭 화합물
WO2016127074A1 (en) 2015-02-06 2016-08-11 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as ret inhibitors
SI3322706T1 (sl) 2015-07-16 2021-04-30 Array Biopharma, Inc. Substituirane pirazolo(1,5-A)piridinske spojine kot zaviralci ret-kinaze
MY194262A (en) 2015-11-02 2022-11-25 Blueprint Medicines Corp Inhibitors of 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
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
ES2948194T3 (es) 2017-01-18 2023-09-01 Array Biopharma Inc Compuestos de pirazolo[1,5-a]pirazina sustituida como inhibidores de la cinasa RET
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
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
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
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
CN111630054B (zh) 2018-01-18 2023-05-09 奥瑞生物药品公司 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物
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
WO2019143994A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
JP7422084B2 (ja) 2018-04-03 2024-01-25 ブループリント メディシンズ コーポレイション Ｒｅｔ変化を有する癌の処置において使用するためのｒｅｔ阻害剤
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
US11964988B2 (en) 2018-09-10 2024-04-23 Array Biopharma Inc. Fused heterocyclic compounds as RET kinase inhibitors
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
EP3845531A4 (en) * 2018-09-30 2021-11-24 Applied Pharmaceutical Science, Inc. SUBSTITUTED PYRAZOLE-CONDENSED RING DERIVATIVES, METHOD FOR THEIR PRODUCTION AND USE THEREOF
WO2020114388A1 (zh) 2018-12-06 2020-06-11 深圳市塔吉瑞生物医药有限公司 取代的吡唑并[1,5-a]吡啶化合物及包含该化合物的组合物及其用途
US20220135557A1 (en) * 2018-12-07 2022-05-05 Sunshine Lake Pharma Co., Ltd. Ret inhibitors, pharmaceutical compositions and uses thereof
CN111285874B (zh) * 2018-12-07 2024-08-09 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
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
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
BR112021019643A2 (pt) * 2019-04-03 2021-12-07 Guangzhou Baiyunshan Pharmaceutical Holdings Co Ltd Baiyunshan Pharmaceutical General Factory Compostos de pirazolopiridina como inibidores do ret e uso dos mesmos
JP2022532758A (ja) * 2019-05-14 2022-07-19 上▲海▼翰森生物医▲薬▼科技有限公司 二環系誘導体を含む阻害剤、その製造方法及び使用
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
CN114127080B (zh) * 2019-06-10 2023-05-05 捷思英达医药技术（上海）有限公司 作为激酶抑制剂的杂环化合物、包括该杂环化合物的组合物、及其使用方法
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
KR20220018584A (ko) * 2019-07-12 2022-02-15 쇼우야오 홀딩스 (베이징) 코., 엘티디. Ret 선택적 억제제 및 그 제조 방법과 용도
CN113490670B (zh) * 2019-08-05 2023-06-02 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,其药物组合物、制备方法和用途
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
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
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
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
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
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
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
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
CN113527291A (zh) * 2020-04-13 2021-10-22 广东东阳光药业有限公司 Ret抑制剂、其药物组合物及其用途
CN113527290A (zh) * 2020-04-13 2021-10-22 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
CN113527292A (zh) * 2020-04-13 2021-10-22 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
TW202202501A (zh) * 2020-04-17 2022-01-16 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
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
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
EP4245757A1 (en) * 2020-11-13 2023-09-20 Shanghai Hansoh Biomedical Co., Ltd. Crystal form of free base of inhibitor containing bicyclic ring derivative and preparation method and application of crystal form
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
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
WO2022132683A1 (en) 2020-12-18 2022-06-23 Loxo Oncology, Inc. Ret inhibitor combination therapy for treating cancer
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
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
AU2022463015A1 (en) 2021-10-22 2024-05-09 Tract Pharmaceuticals, Inc. Methods and compositions for treating chronic inflammatory injury, metaplasia, dysplasia and cancers of epithelial tissues
KR20240101659A (ko) * 2021-12-13 2024-07-02 록쏘 온콜로지, 인코포레이티드 셀페르카티닙 ret 억제제의 결정질 형태 a 및 그의 제조 방법
WO2024030968A1 (en) * 2022-08-03 2024-02-08 Brystol-Myers Squibb Company Compounds for modulating ret protein
CN117229292A (zh) * 2022-10-18 2023-12-15 药雅科技(上海)有限公司 Ret抑制剂的制备及其应用

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
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
KR100587556B1 (ko) 1996-05-08 2006-06-08 바이오겐 아이덱 엠에이 인코포레이티드 신경 및 신장 증식을 자극하기 위한 ＲＥＴ리간드（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
WO2001016169A2 (en) 1999-09-01 2001-03-08 Biogen, Inc. RET LIGAND 5 (Retl5) FROM HUMAN AND MOUSE
FI20000403A0 (fi) 2000-02-22 2000-02-22 Hannu Sariola GDNF perhesukuisten yhdisteiden käyttö kivessyövän hoitoon tarkoitettujen tuotteiden valmistamiseksi
DK1292680T3 (da) 2000-06-22 2010-03-08 Genentech Inc Agonist-anti-TrkC monoklonale antistoffer
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
JP2005535675A (ja) 2002-07-24 2005-11-24 ユニバーシティ・オブ・シンシナティ 変異型ｒｅｔキナーゼ関連疾患を処置するための４−（４−メチルピペラジン−１−イルメチル）−ｎ−［４−メチル−３−（４−ピリジン−３−イル）ピリミジン−２−イルアミノ］フェニル］−ベンズアミド
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
US7169918B2 (en) 2003-10-27 2007-01-30 Genelabs Technologies, Inc. Methods for preparing 7-(2′-substituted-β-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
AU2004295061B2 (en) 2003-11-21 2008-11-20 Novartis Ag 1H-imidazoquinoline derivatives as protein kinase inhibitors
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
US7504509B2 (en) 2003-12-19 2009-03-17 Plexxikon, Inc. Compounds and methods for development of Ret modulators
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
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
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
CA2575808A1 (en) 2004-08-02 2006-02-16 Osi Pharmaceuticals, 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
CA2608009A1 (en) 2005-05-16 2006-11-23 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
US7541367B2 (en) 2005-05-31 2009-06-02 Janssen Pharmaceutica, N.V. 3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders
CA2650999A1 (en) 2005-05-31 2006-12-07 The Pfahl Family Trust (Dated 9 July 1996) Substituted biarylheterocycle derivatives as protein kinase inhibitors for the treatment of cancer and other diseases
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.
WO2007002433A1 (en) 2005-06-22 2007-01-04 Plexxikon, Inc. Pyrrolo [2, 3-b] pyridine derivatives as protein kinase inhibitors
GB0515026D0 (en) 2005-07-21 2005-08-31 Novartis Ag Organic compounds
SI1919979T2 (sl) 2005-08-25 2017-07-31 Creabilis Therapeutics S.P.A. Polimerni konjugati K-252A in njihovi derivati
WO2007053776A1 (en) 2005-11-03 2007-05-10 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
JP2009518340A (ja) 2005-12-08 2009-05-07 ノバルティス アクチエンゲゼルシャフト ＥｐｈＢおよびＶＥＧＦＲ２キナーゼ阻害剤としてのピラゾロ［１，５−ａ］ピリジン−３−カルボン酸
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
WO2007087245A2 (en) 2006-01-24 2007-08-02 Merck & Co., Inc. Ret tyrosine kinase inhibition
PT1973910E (pt) 2006-01-27 2013-09-06 Shanghai Hengrui Pharm Co Ltd Inibidores de pirrolo [3,2-c] piridina-4-ona 2-indolinona proteína cinase
MX2008011661A (es) 2006-03-16 2008-09-22 Novartis Ag Compuestos organicos heterociclicos para el tratamiento de melanoma en particular.
CN101448843B (zh) 2006-03-17 2012-05-09 埃姆比特生物科学公司 用于疾病治疗的咪唑并噻唑化合物
EA015126B1 (ru) 2006-03-27 2011-06-30 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Пиридил- и пиримидинилзамещённые производные пиррола, тиофена и фурана в качестве ингибиторов киназ
JP2009537520A (ja) 2006-05-15 2009-10-29 アイアールエム・リミテッド・ライアビリティ・カンパニー Ｆｇｆ受容体キナーゼ阻害剤のための組成物および方法
WO2007136103A1 (ja) 2006-05-18 2007-11-29 Eisai R & D Management Co., Ltd. 甲状腺癌に対する抗腫瘍剤
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
AU2007294686B2 (en) 2006-09-15 2013-10-31 Equinox Sciences, Llc Kinase inhibitor compounds
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
SI2848610T1 (en) 2006-11-15 2018-02-28 Ym Biosciences Australia Pty Ltd Inhibitors of kinase activity
EP2094701A2 (en) 2006-12-21 2009-09-02 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
PE20121126A1 (es) 2006-12-21 2012-08-24 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
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
EP2114403A2 (en) 2007-01-19 2009-11-11 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
MX2009011951A (es) 2007-05-04 2009-12-11 Irm Llc Compuestos y composiciones como inhibidores de cinasa c-kit y pdgfr.
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
US20090012045A1 (en) 2007-06-26 2009-01-08 Rigel Pharmaceuticals, Inc. Methods of Treating Cell Proliferative Disorders
JP2010533158A (ja) 2007-07-09 2010-10-21 アストラゼネカ アクチボラグ 化合物類−９４５
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
CN101808994B (zh) 2007-07-17 2013-05-15 普莱希科公司 用于激酶调节的化合物和方法以及其适应症
AU2008279776B2 (en) 2007-07-19 2013-05-23 Merck Sharp & Dohme Corp. Heterocyclic amide compounds as protein kinase inhibitors
PT2176231T (pt) 2007-07-20 2016-12-09 Nerviano Medical Sciences Srl Derivados de indazol substituídos activos como inibidores de quinases
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
WO2009053442A1 (en) 2007-10-23 2009-04-30 Novartis Ag Use of trkb antibodies for the treatment of respiratory disorders
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
EA028621B1 (ru) 2008-01-17 2017-12-29 Новартис Аг АНТИТЕЛО ИЛИ ЕГО АНТИГЕНСВЯЗЫВАЮЩИЙ ФРАГМЕНТ, КОТОРЫЙ СПЕЦИФИЧНО СВЯЗЫВАЕТ РЕЦЕПТОРНУЮ ТИРОЗИНКИНАЗУ (TrkB), ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ЭТО АНТИТЕЛО ИЛИ ЕГО АНТИГЕНСВЯЗЫВАЮЩИЙ ФРАГМЕНТ, И КОМБИНАЦИЯ, ВКЛЮЧАЮЩАЯ УКАЗАННУЮ КОМПОЗИЦИЮ
US20090227556A1 (en) 2008-01-31 2009-09-10 Eisai R&D Management Co., Ltd. Receptor tyrosine kinase inhibitors comprising pyridine and pyrimidine derivatives
TW200942537A (en) 2008-02-01 2009-10-16 Irm Llc Compounds and compositions as kinase inhibitors
US20090209496A1 (en) 2008-02-15 2009-08-20 David Chaplin Methods and compositions for enhancing the efficacy of rtk inhibitors
AU2009226153B2 (en) 2008-03-19 2014-02-20 Chembridge Corporation Novel tyrosine kinase inhibitors
WO2009118411A2 (en) 2008-03-28 2009-10-01 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
JP5351254B2 (ja) 2008-05-23 2013-11-27 ノバルティス アーゲー キノキサリン−およびキノリン−カルボキシアミド誘導体
US20090298820A1 (en) * 2008-05-28 2009-12-03 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
AU2009257635A1 (en) 2008-06-10 2009-12-17 Plexxikon, Inc. 5H-Pyrrolo [2,3-b] pyrazine derivatives for kinase modulation, and indications therefor
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
JP5677296B2 (ja) 2008-07-29 2015-02-25 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 グリオーマの治療のためのｃｄｋ阻害剤の使用
WO2010024006A1 (ja) 2008-09-01 2010-03-04 シャープ株式会社 有機エレクトロルミネセンスパネル、有機エレクトロルミネセンスディスプレイ、有機エレクトロルミネセンス照明、及び、それらの製造方法
US20100075916A1 (en) 2008-09-05 2010-03-25 Auspex 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
WO2010031816A1 (en) 2008-09-19 2010-03-25 Nerviano Medical Sciences S.R.L. 3,4 DIHYDRO-2H-PYRROLO[1,2-a]PYRAZIN-1-ONE DERIVATIVES
JP5503655B2 (ja) 2008-09-22 2014-05-28 アレイ バイオファーマ、インコーポレイテッド Ｔｒｋキナーゼ阻害剤としての置換イミダゾ［１，２ｂ］ピリダジン化合物
EP2331530B8 (en) 2008-09-26 2013-12-25 National Health Research Institutes Fused multicyclic compounds as protein kinase inhibitors
JP5600111B2 (ja) 2008-10-22 2014-10-01 アレイ バイオファーマ、インコーポレイテッド ＴＲＫキナーゼ阻害剤としての置換ピラゾロ［１，５−ａ］ピリミジン化合物
JP5686736B2 (ja) 2008-11-06 2015-03-18 アムビト ビオスシエンセス コルポラチオン プロテインキナーゼモジュレーターとしてのイミダゾロチアゾール化合物
JP2012509859A (ja) 2008-11-24 2012-04-26 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 中皮腫の治療のためのｃｄｋ阻害物質
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
PT2428508E (pt) 2009-05-08 2016-02-29 Kotobuki Pharmaceutical Co Ltd Composto diamino-carboxamida heterocíclico
JP6073677B2 (ja) 2009-06-12 2017-02-01 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド 縮合複素環式化合物およびそれらの使用
EP3045457B1 (en) 2009-06-15 2018-05-09 Nerviano Medical Sciences S.r.l. Substituted pyrimidinylpyrrolopyridinone derivatives, process for their preparation and their use as kinase inhibitors
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
IN2012DN01961A (es) 2009-08-17 2015-08-21 Intellikine Llc
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
ES2658290T3 (es) 2009-10-29 2018-03-09 Genosco Inhibidores de cinasa
CN102811619B (zh) 2009-11-13 2015-04-22 金纳斯克公司 激酶抑制剂
KR101094446B1 (ko) 2009-11-19 2011-12-15 한국과학기술연구원 단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노［3,2-ｄ］피리미딘 화합물
AU2010343102B2 (en) 2009-12-29 2016-03-24 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
KR101483215B1 (ko) 2010-01-29 2015-01-16 한미약품 주식회사 단백질 키나아제 저해활성을 갖는 비시클릭 헤테로아릴 유도체
EP2528918B1 (en) 2010-01-29 2014-09-10 Nerviano Medical Sciences S.r.l. 6,7-dihydroimidazo[1,5-a]pyrazin-8(5h)-one derivatives as protein kinase modulators
WO2011093684A2 (en) 2010-01-29 2011-08-04 Hanmi Holdings Co., Ltd. THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY ON PROTEIN KINASES
JP2013519706A (ja) 2010-02-18 2013-05-30 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル 癌転移を予防するための方法
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
KR101852169B1 (ko) 2010-05-20 2018-04-26 어레이 바이오파마 인크. Trk 키나제 저해제로서의 매크로시클릭 화합물
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
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
BR112013018515B1 (pt) 2011-01-26 2021-06-29 Nerviano Medical Sciences S.R.I Derivados de pirrol tricíclico, processo para sua preparação e seu uso como inibidores da quinase
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
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
AU2012214762B2 (en) 2011-02-07 2015-08-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
ES2580961T3 (es) 2011-02-24 2016-08-30 Nerviano Medical Sciences S.R.L. Derivados Tiazolilfenil-bencenosulfonamido como Inhibidores de Cinasa
BR112013021638A2 (pt) 2011-02-25 2016-08-02 Irm Llc "compostos inibidores de trk, seu uso e composições que os compreendem"
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
PT2693881T (pt) 2011-04-01 2019-12-09 Univ Utah Res Found Análogos de n-fenilpirimidin-2-amina substituídos como inibidores da axl cinase
US9284298B2 (en) 2011-04-11 2016-03-15 Nerviano Medical Sciences S.R.L. Pyrazolyl-pyrimidine derivatives as kinase inhibitors
WO2012143248A1 (en) 2011-04-19 2012-10-26 Nerviano Medical Sciences S.R.L. Substituted pyrimidinyl-pyrroles active as kinase inhibitors
AR086042A1 (es) * 2011-04-28 2013-11-13 Galapagos Nv Compuesto util para el tratamiento de enfermedades degenerativas e inflamatorias y composicion farmaceutica
CA2835478C (en) 2011-05-12 2019-02-05 Nerviano Medical Sciences S.R.L. Substituted indazole derivatives active as kinase inhibitors
NZ618795A (en) 2011-05-13 2015-07-31 Array Biopharma Inc Pyrrolidinyl urea, pyrrolidinyl thiourea and pyrrolidinyl guanidine compounds as trka kinase inhibitors
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
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
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
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
DK2748192T3 (en) 2011-08-23 2019-02-25 Found Medicine Inc KIF5B-RET-FUSION MOLECULES AND APPLICATIONS THEREOF
JP6342805B2 (ja) 2011-09-02 2018-06-13 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 置換ピラゾロ［３，４−ｄ］ピリミジンおよびその用途
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
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
EP2788350B1 (en) 2011-10-07 2017-12-06 Nerviano Medical Sciences S.r.l. 4-ALKYL SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS
WO2013074518A1 (en) 2011-11-14 2013-05-23 Tesaro, Inc. Modulating certain tyrosine kinases
CN104080907A (zh) 2011-11-30 2014-10-01 日本国立癌症研究中心 诱导恶性干细胞
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
AU2012363558C1 (en) 2011-12-30 2019-08-29 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
EP2849751A1 (en) 2012-05-10 2015-03-25 Synta Pharmaceuticals Corp. Treating cancer with hsp90 inhibitory compounds
CA2873979C (en) 2012-05-23 2019-11-12 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
WO2014011900A2 (en) 2012-07-11 2014-01-16 Blueprint Medicines Inhibitors of the fibroblast growth factor receptor
EP2878672A4 (en) 2012-07-26 2016-02-17 Nat Cancer Ct FUSIONSGEN OF CEP55-GEN AND RET-GEN
ES2726833T3 (es) 2012-08-02 2019-10-09 Nerviano Medical Sciences Srl Pirroles sustituidos activos como inhibidores de cinasas
EP2892532B1 (en) 2012-09-07 2019-02-13 Exelixis, Inc. Inhibitors of met, vegfr and ret for use in the treatment of lung adenocarcinoma
DK2902029T3 (en) 2012-09-25 2018-10-29 Chugai Pharmaceutical Co Ltd RET INHIBITOR
EP2917214B1 (en) 2012-11-07 2019-08-28 Nerviano Medical Sciences S.r.l. Substituted pyrimidinyl and pyridinyl-pyrrolopyridinones, process for their preparation and their use as kinase inhibitors
CA2890462A1 (en) 2012-11-12 2014-05-15 Ignyta, Inc. Bendamustine derivatives and methods of using same
US9546156B2 (en) 2012-11-13 2017-01-17 Array Biopharma Inc. N-bicyclic aryl,N'-pyrazolyl urea, thiourea, guanidine cyanoguanidine compounds as TrkA kinase inhibitors
LT2920166T (lt) 2012-11-13 2016-12-12 Array Biopharma, Inc. Bicikliniai karbamido, tiokarbamido, guanidino ir cianoguanidino junginiai, tinkami naudoti skausmo gydymui
WO2014078322A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Thiazolyl and oxazolyl 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
WO2014078325A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-(monocyclic aryl),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
WO2014078408A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9809578B2 (en) 2012-11-13 2017-11-07 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors
DK2922844T3 (en) 2012-11-13 2018-03-05 Array Biopharma Inc N-PYRROLIDINYL, N'-PYRAZOLYL-URINE, THIOURINE, GUANIDINE AND CYANOGUANIDE 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
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
WO2014086284A1 (zh) 2012-12-04 2014-06-12 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
FR3000492B1 (fr) 2012-12-28 2015-09-11 Oribase Pharma Nouveaux derives azaindole en tant qu'inhibiteurs multikinases
ES2696700T3 (es) 2012-12-28 2019-01-17 Crystalgenomics Inc Derivado de 2,3-dihidro-isoindol-1-on como supresor de quinasa BTK y composición farmacéutica que incluye el mismo
FR3000493A1 (fr) 2012-12-28 2014-07-04 Oribase Pharma Nouveaux inhibiteurs de proteines kinases
FR3000494B1 (fr) 2012-12-28 2015-08-21 Oribase Pharma Nouveaux derives d'azaindoles en tant qu'inhibiteurs de proteines kinases
TW201443037A (zh) * 2013-01-09 2014-11-16 Gilead Sciences Inc 治療用化合物
WO2014129431A1 (ja) 2013-02-19 2014-08-28 小野薬品工業株式会社 Ｔｒｋ阻害化合物
WO2014160524A1 (en) 2013-03-14 2014-10-02 The Trustees Of The University Of Pennsylvania Cardio- metabolic and cascular effects of glp-1 metabolites
EP3521284B1 (en) * 2013-03-15 2020-12-02 The Trustees of Columbia University in the City of New York Pyrazine compounds as map kinase modulators and uses thereof
PT2970191T (pt) 2013-03-15 2017-03-23 Glaxosmithkline Ip Dev Ltd Derivados de piridina como inibidores da quinase rearranjada durante transfecção(ret)
EP2970231A1 (en) 2013-03-15 2016-01-20 Blueprint Medicines Corporation Piperazine derivatives and their use as kit modulators
MA38394B1 (fr) 2013-03-15 2018-04-30 Glaxosmithkline Ip Dev Ltd Dérivés pyridine utilisés comme inhibiteurs de la kinase réarrangée au cours de la transfection (ret)
EP2997030B1 (en) 2013-05-14 2017-08-09 Nerviano Medical Sciences S.R.L. Pyrrolo[2,3-d]pyrimidine derivatives, process for their preparation and their use as kinase inhibitors
EP3004060B1 (en) 2013-05-30 2019-11-27 Plexxikon Inc. Compounds for kinase modulation, and indications therefor
EP3027655B1 (en) 2013-07-30 2019-08-21 Blueprint Medicines Corporation Ntrk2 fusions
WO2015017528A1 (en) 2013-07-30 2015-02-05 Blueprint Medicines Corporation Pik3c2g fusions
CN105658814A (zh) 2013-08-20 2016-06-08 日本国立癌症研究中心 在肺癌中检测出的新型融合基因
KR20160055170A (ko) 2013-08-30 2016-05-17 암비트 바이오사이언시즈 코포레이션 바이아릴 아세트아미드 화합물 및 이의 사용 방법
WO2015058129A1 (en) 2013-10-17 2015-04-23 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
CN105658652B (zh) 2013-10-17 2019-04-12 蓝图药品公司 可用于治疗与kit相关的病症的组合物
EP3060560A1 (en) 2013-10-25 2016-08-31 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
GB201321146D0 (en) 2013-11-29 2014-01-15 Cancer Rec Tech Ltd Quinazoline compounds
WO2015082887A2 (en) 2013-12-02 2015-06-11 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
UA121206C2 (uk) 2014-01-24 2020-04-27 Турнінґ Поінт Терапьютикс, Інк. Діарильні макроцикли як модулятори протеїнкіназ
JP6756617B2 (ja) 2014-02-14 2020-09-16 エグゼリクシス， インコーポレイテッド Ｎ−｛４−［（６，７−ジメトキシキノリン−４−イル）オキシ］フェニル｝−ｎ’−（４−フルオロフェニル）シクロプロパン−１，１−ジカルボキサミドの結晶性固体形態、製造プロセス、及び使用方法
US10231965B2 (en) 2014-02-20 2019-03-19 Ignyta, Inc. Molecules for administration to ROS1 mutant cancer cells
WO2015161277A1 (en) 2014-04-18 2015-10-22 Blueprint Medicines Corporation Met fusions
US20170044622A1 (en) 2014-04-18 2017-02-16 Blueprint Medicines Corporation Pik3ca fusions
LT3154959T (lt) 2014-05-15 2019-09-25 Array Biopharma, Inc. 1-((3s,4r)-4-(3-fluorfenil)-1-(2-metoksietil)pirolidin-3-il)-3-(4-metil-3-(2-metilpirimidin-5-il)-1-fenil-1h-pirazol-5-il)karbamidas kaip trka kinazės inhibitorius
EP3155131B1 (en) 2014-06-10 2020-02-12 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
EP3169671B1 (en) 2014-07-17 2019-08-21 Sunshine Lake Pharma Co., Ltd. 1-(5-(tert.-butyl)isoxazol-3-yl)-3-(4-((phenyl)ethynyl)phenyl)urea derivatives and related compounds as flt3 inhibitors for treating cancer
EP3169809B1 (en) 2014-07-17 2020-04-29 Blueprint Medicines Corporation Prkc fusions
EP3169808B1 (en) 2014-07-17 2019-05-22 Blueprint Medicines Corporation Trio:tert fusion in cancer
US9688680B2 (en) 2014-08-04 2017-06-27 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
HUE045237T2 (hu) 2014-08-18 2019-12-30 Ono Pharmaceutical Co TRK-inhibitáló vegyület savaddíciós sója
RU2017111590A (ru) 2014-09-08 2018-10-10 Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед Кристаллические формы 2-(4-(4-этокси-6-оксо-1,6-дигидропиридин-3-ил)-2-фторфенил)-n-(5-(1,1,1-трифтор-2- метилпропан-2-ил)изоксазол-3-ил)ацетамида
JP6538154B2 (ja) 2014-09-10 2019-07-03 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 Ｒｅｔ（ｒｅａｒｒａｎｇｅｄ ｄｕｒｉｎｇ ｔｒａｎｓｆｅｃｔｉｏｎ）キナーゼ阻害剤としてのピリジン誘導体
JP6538153B2 (ja) 2014-09-10 2019-07-03 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 Ｒｅａｒｒａｎｇｅｄ ｄｕｒｉｎｇ ｔｒａｎｓｆｅｃｔｉｏｎ（ｒｅｔ）阻害剤としての新規な化合物
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
PL3218378T3 (pl) * 2014-11-14 2020-10-19 Nerviano Medical Sciences S.R.L. Pochodne 6-amino-7-bicyklo-7-deazapuryny jako inhibitory kinaz białkowych
JP6914834B2 (ja) 2014-11-16 2021-08-04 アレイ バイオファーマ インコーポレイテッド （Ｓ）−Ｎ−（５−（（Ｒ）−２−（２，５−ジフルオロフェニル）−ピロリジン−１−イル）−ピラゾロ［１，５−ａ］ピリミジン−３−イル）−３−ヒドロキシピロリジン−１−カルボキサミド硫酸水素塩の結晶形
WO2016081450A1 (en) 2014-11-18 2016-05-26 Blueprint Medicines Corporation Prkacb fusions
WO2016096709A1 (en) 2014-12-16 2016-06-23 Eudendron S.R.L. Heterocyclic derivatives modulating activity of certain protein kinases
WO2016127074A1 (en) 2015-02-06 2016-08-11 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
WO2016168992A1 (en) 2015-04-21 2016-10-27 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
SI3322706T1 (sl) * 2015-07-16 2021-04-30 Array Biopharma, Inc. Substituirane pirazolo(1,5-A)piridinske spojine kot zaviralci ret-kinaze
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
MY194262A (en) 2015-11-02 2022-11-25 Blueprint Medicines Corp Inhibitors of ret
WO2017097697A1 (en) 2015-12-08 2017-06-15 Boehringer Ingelheim International Gmbh Method using a ret fusion gene as a biomarker to select non-small cell lung cancer (nsclc) and thyroid cancer patients for a cancer treatment
JP6871869B2 (ja) 2016-01-15 2021-05-19 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
LT3269370T (lt) 2016-02-23 2020-03-25 Taiho Pharmaceutical Co., Ltd. Naujas kondensuotas pirimidino junginys arba jo druska
TW201738228A (zh) 2016-03-17 2017-11-01 藍圖醫藥公司 Ｒｅｔ之抑制劑
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
MX2018012609A (es) 2016-04-15 2019-08-01 Cancer Research Tech Ltd Compuestos heterociclicos como inhibidores de la cinasa ret.
PL3442535T3 (pl) * 2016-04-15 2022-10-24 Cancer Research Technology Limited Związki heterocykliczne jako inhibitory kinazy 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
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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