ZA201803050B - Inhibitors of ret - Google Patents

Inhibitors of ret

Info

Publication number
ZA201803050B
ZA201803050B ZA2018/03050A ZA201803050A ZA201803050B ZA 201803050 B ZA201803050 B ZA 201803050B ZA 2018/03050 A ZA2018/03050 A ZA 2018/03050A ZA 201803050 A ZA201803050 A ZA 201803050A ZA 201803050 B ZA201803050 B ZA 201803050B
Authority
ZA
South Africa
Prior art keywords
ret
inhibitors
Prior art date
Application number
ZA2018/03050A
Other languages
English (en)
Inventor
D Brubaker Jason
L Kim Joseph
J Wilson Kevin
Wilson Douglas
V Dipietro Lucian
Original Assignee
Blueprint Medicines Corp
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 Blueprint Medicines Corp filed Critical Blueprint Medicines Corp
Publication of ZA201803050B publication Critical patent/ZA201803050B/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/30Halogen atoms or nitro radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/34One oxygen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/34One oxygen atom
    • C07D239/36One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/38One sulfur atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
ZA2018/03050A 2015-11-02 2018-05-09 Inhibitors of ret ZA201803050B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562249784P 2015-11-02 2015-11-02
US201662367960P 2016-07-28 2016-07-28
PCT/US2016/059879 WO2017079140A1 (en) 2015-11-02 2016-11-01 Inhibitors of ret

Publications (1)

Publication Number Publication Date
ZA201803050B true ZA201803050B (en) 2019-09-25

Family

ID=57286889

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA2018/03050A ZA201803050B (en) 2015-11-02 2018-05-09 Inhibitors of ret

Country Status (31)

Country Link
US (5) US10030005B2 (enExample)
EP (3) EP4292594A3 (enExample)
JP (3) JP6807385B2 (enExample)
KR (1) KR20180073689A (enExample)
CN (2) CN108473468B (enExample)
AU (1) AU2016348402B2 (enExample)
BR (1) BR112018008877B1 (enExample)
CA (1) CA3003721C (enExample)
CL (1) CL2018001181A1 (enExample)
DK (1) DK3371171T3 (enExample)
EA (1) EA038890B1 (enExample)
ES (1) ES2969185T3 (enExample)
FI (1) FI3371171T3 (enExample)
FR (1) FR24C1016I1 (enExample)
HR (1) HRP20231681T1 (enExample)
HU (1) HUE064659T2 (enExample)
IL (3) IL302209B2 (enExample)
LT (1) LT3371171T (enExample)
MX (1) MX384884B (enExample)
MY (1) MY194262A (enExample)
NZ (1) NZ742351A (enExample)
PH (1) PH12018500907A1 (enExample)
PL (1) PL3371171T3 (enExample)
PT (1) PT3371171T (enExample)
RS (1) RS65069B1 (enExample)
SA (1) SA518391496B1 (enExample)
SG (1) SG11201803653QA (enExample)
SI (1) SI3371171T1 (enExample)
TW (2) TWI787018B (enExample)
WO (1) WO2017079140A1 (enExample)
ZA (1) ZA201803050B (enExample)

Families Citing this family (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102971322B (zh) 2010-05-20 2016-02-17 阵列生物制药公司 作为trk激酶抑制剂的大环化合物
RU2019102203A (ru) 2012-07-11 2019-03-05 Блюпринт Медсинс Корпорейшн Ингибиторы рецептора фактора роста фибробластов
US9499522B2 (en) 2013-03-15 2016-11-22 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
DK3057969T3 (en) 2013-10-17 2018-09-24 Blueprint Medicines Corp COMPOSITIONS USED FOR TREATMENT OF DISEASES RELATED TO ENZYMETE KIT
AU2014339972B9 (en) 2013-10-25 2019-05-30 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
US9695165B2 (en) 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
WO2016127074A1 (en) 2015-02-06 2016-08-11 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as ret inhibitors
CN108349969B (zh) 2015-07-16 2022-05-10 阵列生物制药公司 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡啶化合物
RU2018106483A (ru) 2015-07-24 2019-08-26 Блюпринт Медсинс Корпорейшн Соединения, подходящие для лечения расстройств, связанных с kit и pdgfr
WO2017035354A1 (en) 2015-08-26 2017-03-02 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to ntrk
RS65069B1 (sr) 2015-11-02 2024-02-29 Blueprint Medicines Corp Inhibitori ret-a
CN108431008A (zh) 2015-11-19 2018-08-21 蓝图药品公司 可用于治疗与ntrk相关的病症的化合物和组合物
US10183928B2 (en) 2016-03-17 2019-01-22 Blueprint Medicines Corporation Inhibitors of RET
KR102426043B1 (ko) 2016-04-15 2022-07-27 블루프린트 메디신즈 코포레이션 액티빈 수용체 유사 키나아제의 저해제
JP7000349B2 (ja) 2016-05-13 2022-02-04 インスティテュート デ メディシナ モレキュラー ジョアオ ロボ アントゥネス Ilc3細胞に関連する疾患を処置する方法
WO2018017983A1 (en) * 2016-07-22 2018-01-25 Blueprint Medicines Corporation Compounds useful for treating disorders related to ret
WO2018022761A1 (en) * 2016-07-27 2018-02-01 Blueprint Medicines Corporation Substituted cyclopentane-amides for treating disorders related to ret
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
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
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
WO2018183712A1 (en) 2017-03-31 2018-10-04 Blueprint Medicines Corporation Pyrrolo[1,2-b]pyridazine compounds and compositions useful for treating disorders related to kit and pdgfr
WO2018213329A1 (en) 2017-05-15 2018-11-22 Blueprint Medicines Corporation Combinations of ret inhibitors and mtorc1 inhibitors and uses thereof for the treatment of cancer mediated by aberrant ret activity
TWI812649B (zh) 2017-10-10 2023-08-21 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
JP7278273B2 (ja) 2017-10-18 2023-05-19 ブループリント メディシンズ コーポレイション アクチビン受容体様キナーゼの阻害剤としての置換ピロロピリジン
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
US11472802B2 (en) 2018-01-18 2022-10-18 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors
PT3773589T (pt) 2018-04-03 2024-02-06 Blueprint Medicines Corp Inibidor de ret para utilização no tratamento de cancro com alteração de ret
CN112703014A (zh) 2018-08-10 2021-04-23 缆图药品公司 Egfr突变型癌症的治疗
WO2020035065A1 (zh) * 2018-08-17 2020-02-20 南京明德新药研发有限公司 作为ret抑制剂的吡唑衍生物
WO2020055672A1 (en) 2018-09-10 2020-03-19 Array Biopharma Inc. Fused heterocyclic compounds as ret kinase inhibitors
WO2020114474A1 (zh) * 2018-12-06 2020-06-11 苏州信诺维医药科技有限公司 一种杂环化合物、其应用及含其的药物组合物
CN111285882B (zh) * 2018-12-07 2022-12-02 四川科伦博泰生物医药股份有限公司 稠环化合物、包含其的药物组合物及其制备方法和用途
CN111484479B (zh) * 2019-01-25 2023-06-13 四川科伦博泰生物医药股份有限公司 氮杂环化合物、包含其的药物组合物及其制备方法和用途
CN111499613B (zh) * 2019-01-31 2023-05-12 浙江海正药业股份有限公司 N-甲酰胺衍生物、其制备方法及其在医药上的用途
CN113316578B (zh) 2019-02-19 2023-10-31 四川科伦博泰生物医药股份有限公司 杂环化合物、包含其的药物组合物及其制备方法和用途
ES3023310T3 (en) * 2019-04-03 2025-05-30 Guangzhou Baiyunshan Pharmaceutical Holdings Co Ltd Baiyunshan Pharmaceutical General Factory Nitrogen-containing spiro derivative as ret inhibitor
CN111808077B (zh) 2019-04-12 2023-05-02 浙江海正药业股份有限公司 哌嗪酰胺衍生物,其制备方法及其在医药上的用途
EP4302761A3 (en) 2019-04-12 2024-03-27 Blueprint Medicines Corporation Crystalline forms of (s)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1h-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazinyl)-pyrimidin-5-yl)ethan-1-amine and methods of making
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
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
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
CN113135896B (zh) * 2020-01-18 2024-12-06 正大天晴药业集团股份有限公司 作为ret抑制剂的甲基吡唑类衍生物
CN111440151A (zh) * 2020-03-25 2020-07-24 魏威 制备抗肿瘤药普拉赛替尼的方法
CN111362923A (zh) * 2020-03-25 2020-07-03 魏威 制备ret抑制剂普拉塞替尼的方法、以及普拉塞替尼的中间体及其制备方法
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
AU2021276206B2 (en) * 2020-05-20 2024-12-12 Tyk Medicines, Inc. Compound used as RET kinase inhibitor and application thereof
MX2022015022A (es) 2020-05-29 2023-03-08 Blueprint Medicines Corp Composiciones farmaceuticas de pralsetinib.
EP4157829A1 (en) * 2020-05-29 2023-04-05 Blueprint Medicines Corporation Solid forms of pralsetinib
CN111777595A (zh) * 2020-07-22 2020-10-16 上海希迈医药科技有限公司 一种环己烷甲酰胺类化合物的新晶型及其制备方法
WO2022086899A1 (en) 2020-10-19 2022-04-28 Teva Pharmaceuticals International Gmbh Solid state forms of pralsetinib and process for preparation thereof
WO2022117448A1 (en) 2020-12-03 2022-06-09 Sandoz Ag Crystalline forms of pralsetinib
AR124245A1 (es) * 2020-12-04 2023-03-01 Blueprint Medicines Corp Método para preparar pralsetinib
CN113072541B (zh) * 2021-04-02 2022-07-08 山东四环药业股份有限公司 一种靶向药物blu-667的制备方法
CA3222177A1 (en) 2021-06-03 2022-12-08 Fundacao D. Anna De Sommer Champalimaud E Dr. Carlos Montez Champalimaud Neuro-mesenchyme units control ilc2 and obesity via a brain-adipose circuit
TW202345806A (zh) 2022-03-31 2023-12-01 美商艾伯維有限公司 噻唑并〔5,4-b〕吡啶malt-1抑制劑
CN115057822B (zh) * 2022-07-14 2023-05-02 上海优合贝德医药科技有限公司 一种普拉替尼中间体2097133-31-6的新合成方法
CN117466901A (zh) * 2022-07-23 2024-01-30 浙江海正药业股份有限公司 哌嗪酰胺衍生物的晶型及其制备方法和用途
CN119768181A (zh) 2022-08-24 2025-04-04 东丽株式会社 用于癌的治疗和/或预防的药品
WO2024206858A1 (en) 2023-03-30 2024-10-03 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
IT202300006819A1 (it) 2023-04-06 2024-10-06 Olon Spa Processo per preparare pralsetinib in forma amorfa, e relativi intermedi in forma cristallina.
WO2024229406A1 (en) 2023-05-04 2024-11-07 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
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ras抑制劑
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

Family Cites Families (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2001237041B9 (en) 2000-02-17 2005-07-28 Amgen Inc. Kinase inhibitors
US20060116381A1 (en) * 2002-07-24 2006-06-01 Fagin James A 4-4(methylpiperazin-1-ylmethyl)-n-[4-methyl-3-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-ben-zamide for treating mutated-ret kinase associated diseases
PT1696920E (pt) 2003-12-19 2015-01-14 Plexxikon Inc Compostos e métodos para o desenvolvimento de moduladores de ret
US8227455B2 (en) * 2005-04-18 2012-07-24 Rigel Pharmaceuticals, Inc. Methods of treating cell proliferative disorders
WO2006128042A2 (en) 2005-05-26 2006-11-30 The Johns Hopkins University Methods of identifying mutations in nucleic acid
WO2007023382A2 (en) 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors
US20090227598A1 (en) 2006-01-24 2009-09-10 Buser-Doepner Carolyn A Ret Tyrosine Kinase Inhibition
US20090048214A1 (en) * 2006-11-15 2009-02-19 Rigel Pharmaceuticals, Inc Methods for Treating Renal Tumors Using 2, 4-Pyrimidinediamine Drug and Prodrug Compounds
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
CN101801958B (zh) 2007-07-19 2014-01-29 默沙东公司 作为蛋白质激酶抑制剂的杂环酰胺化合物
NZ582879A (en) * 2007-07-31 2012-03-30 Vertex Pharma Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof
WO2009100536A1 (en) 2008-02-15 2009-08-20 Methylgene Inc. Inhibitors of kinase activity with 1,2-di-cyclyl substituted alkyne structures
CA2730190A1 (en) 2008-07-14 2010-01-21 Queen's University At Kingston Pharmaceutical compositions comprising ret inhibitors and methods for the treatment of cancer
AU2010229140A1 (en) * 2009-03-24 2011-11-10 Msd K.K. Novel aminopyridine derivatives having Aurora A selective inhibitory action
CA2765044A1 (en) * 2009-06-09 2010-12-16 California Capital Equity, Llc Benzyl substituted triazine derivatives and their therapeutical applications
EP2493460A4 (en) 2009-10-30 2013-04-24 Ariad Pharma Inc METHOD AND COMPOSITIONS FOR THE TREATMENT OF CANCER
EA024729B1 (ru) 2009-11-13 2016-10-31 Джиноско Киназные ингибиторы
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
CA2846496C (en) 2011-09-02 2020-07-14 The Regents Of The University Of California Substituted pyrazolo[3,4-d]pyrimidines and uses thereof
US20130096136A1 (en) 2011-09-30 2013-04-18 Methylgene Inc. Inhibitors of Protein Tyrosine Kinase Activity
US10023855B2 (en) 2011-10-31 2018-07-17 Macrogen, Inc. Fusion protein comprising C-terminal domain of RET protein and use thereof as a diagnosing marker
WO2013071093A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
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
TWI577677B (zh) * 2012-04-25 2017-04-11 拉夸里亞創藥股份有限公司 作爲ttx-s阻斷劑之吡咯並吡啶酮衍生物
WO2013170159A1 (en) 2012-05-10 2013-11-14 Synta Pharmaceuticals Corp. Treating cancer with hsp90 inhibitory compounds
RU2019102203A (ru) 2012-07-11 2019-03-05 Блюпринт Медсинс Корпорейшн Ингибиторы рецептора фактора роста фибробластов
CN104619841A (zh) 2012-07-26 2015-05-13 日本国立癌症研究中心 Cep55基因与ret基因的融合基因
CN104703600A (zh) 2012-09-07 2015-06-10 埃克塞里艾克西斯公司 用于治疗肺腺癌的met、vegfr和ret的抑制剂
SG10201704588XA (en) * 2012-09-25 2017-07-28 Chugai Pharmaceutical Co Ltd Ret inhibitor
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
TWI629266B (zh) 2012-12-28 2018-07-11 藍印藥品公司 纖維母細胞生長因子受體之抑制劑
EA027861B1 (ru) 2013-02-25 2017-09-29 Бристол-Майерс Сквибб Компани C-3 алкил- и алкенилмодифицированные производные бетулиновой кислоты или их фармацевтические соли, противовирусная фармацевтическая композиция и фармацевтическая композиция для лечения вич на их основе
US9499522B2 (en) 2013-03-15 2016-11-22 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
HUE033423T2 (en) * 2013-03-15 2017-11-28 Glaxosmithkline Ip Dev Ltd Pyridine derivatives as rearranged during transfection (ret) kinase inhibitors
WO2015006875A1 (en) 2013-07-18 2015-01-22 Methylgene Inc. Process for the preparation of substituted pyrimidines
TW201542825A (zh) 2013-08-20 2015-11-16 Nat Cancer Ct 在肺癌辨識出的新穎融合基因
DK3057969T3 (en) 2013-10-17 2018-09-24 Blueprint Medicines Corp COMPOSITIONS USED FOR TREATMENT OF DISEASES RELATED TO ENZYMETE KIT
US9334263B2 (en) 2013-10-17 2016-05-10 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
AU2014339972B9 (en) 2013-10-25 2019-05-30 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
GB201321146D0 (en) 2013-11-29 2014-01-15 Cancer Rec Tech Ltd Quinazoline compounds
US9695165B2 (en) 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
US9688680B2 (en) 2014-08-04 2017-06-27 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
PT3191450T (pt) 2014-09-10 2019-05-29 Glaxosmithkline Ip Dev Ltd Derivados de piridona como inibidores da quinase rearranjada durante a transfecção (ret)
KR20170046180A (ko) 2014-09-10 2017-04-28 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 형질감염 중 재배열 (ret) 억제제로서의 신규 화합물
AU2015345054B2 (en) 2014-11-14 2020-03-05 Nerviano Medical Sciences S.R.L. 6-amino-7-bicyclo-7-deaza-purine derivatives as protein kinase inhibitors
WO2016127074A1 (en) 2015-02-06 2016-08-11 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as ret inhibitors
CN108349969B (zh) 2015-07-16 2022-05-10 阵列生物制药公司 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡啶化合物
RU2018106483A (ru) 2015-07-24 2019-08-26 Блюпринт Медсинс Корпорейшн Соединения, подходящие для лечения расстройств, связанных с kit и pdgfr
WO2017035354A1 (en) 2015-08-26 2017-03-02 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to ntrk
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
JP2018534933A (ja) 2015-11-02 2018-11-29 ヤンセン ファーマシューティカ エヌ.ベー. 抗il1rap抗体、il1rapとcd3を結合する二重特異性抗原結合分子、及びその使用
KR20180069903A (ko) 2015-11-02 2018-06-25 파이브 프라임 테라퓨틱스, 인크. Cd80 세포외 도메인 폴리펩타이드 및 이들의 암 치료에서의 용도
RS65069B1 (sr) * 2015-11-02 2024-02-29 Blueprint Medicines Corp Inhibitori ret-a
CN108431008A (zh) 2015-11-19 2018-08-21 蓝图药品公司 可用于治疗与ntrk相关的病症的化合物和组合物
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
US10183928B2 (en) 2016-03-17 2019-01-22 Blueprint Medicines Corporation Inhibitors of RET
KR102356433B1 (ko) 2016-04-01 2022-01-27 시그날 파마소티칼 엘엘씨 치환된 아미노퓨린 화합물, 이의 조성물, 및 그것에 의한 치료 방법
KR102426043B1 (ko) 2016-04-15 2022-07-27 블루프린트 메디신즈 코포레이션 액티빈 수용체 유사 키나아제의 저해제
IL289793B2 (en) 2016-04-15 2023-03-01 Cancer Research Tech Ltd Heterocyclic compounds as ret kinase inhibitors
SMT202200348T1 (it) 2016-04-15 2022-11-18 Cancer Research Tech Ltd Composti eterociclici come inibitori della chinasi ret
WO2018017983A1 (en) 2016-07-22 2018-01-25 Blueprint Medicines Corporation Compounds useful for treating disorders related to ret
WO2018022761A1 (en) 2016-07-27 2018-02-01 Blueprint Medicines Corporation Substituted cyclopentane-amides for treating disorders related to ret
WO2018049233A1 (en) 2016-09-08 2018-03-15 Nicolas Stransky Inhibitors of the fibroblast growth factor receptor in combination with cyclin-dependent kinase inhibitors
JP2018052878A (ja) 2016-09-29 2018-04-05 第一三共株式会社 ピリジン化合物
CN106749231B (zh) 2016-10-09 2019-03-01 南京纳丁菲医药科技有限公司 萘啶化合物和药物组合物及它们的应用
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
WO2018102455A1 (en) 2016-12-01 2018-06-07 Ignyta, Inc. Methods for the treatment of cancer
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
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
WO2018183712A1 (en) 2017-03-31 2018-10-04 Blueprint Medicines Corporation Pyrrolo[1,2-b]pyridazine compounds and compositions useful for treating disorders related to kit and pdgfr
GB201705971D0 (en) 2017-04-13 2017-05-31 Cancer Res Tech Ltd Inhibitor compounds
WO2018213329A1 (en) 2017-05-15 2018-11-22 Blueprint Medicines Corporation Combinations of ret inhibitors and mtorc1 inhibitors and uses thereof for the treatment of cancer mediated by aberrant ret activity
US10934300B2 (en) 2017-06-23 2021-03-02 San Diego State University (Sdsu) Foundation Atropisomerism for enhanced kinase inhibitor selectivity
CN109180677A (zh) 2017-06-30 2019-01-11 厦门大学 取代芳基醚类化合物、其制备方法、药用组合物及其应用
CA3068122A1 (en) 2017-07-07 2019-01-10 Nipd Genetics Public Company Limited Target-enriched multiplexed parallel analysis for assessment of tumor biomarkers
SG11202005590PA (en) 2017-12-19 2020-07-29 Turning Point Therapeutics Inc Macrocyclic compounds for treating disease
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
US11472802B2 (en) 2018-01-18 2022-10-18 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors
CN111971286B (zh) 2018-01-18 2023-04-14 阿雷生物药品公司 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物
PT3773589T (pt) 2018-04-03 2024-02-06 Blueprint Medicines Corp Inibidor de ret para utilização no tratamento de cancro com alteração de ret
CN112703014A (zh) 2018-08-10 2021-04-23 缆图药品公司 Egfr突变型癌症的治疗

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