JP2018535967A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2018535967A5 JP2018535967A5 JP2018521916A JP2018521916A JP2018535967A5 JP 2018535967 A5 JP2018535967 A5 JP 2018535967A5 JP 2018521916 A JP2018521916 A JP 2018521916A JP 2018521916 A JP2018521916 A JP 2018521916A JP 2018535967 A5 JP2018535967 A5 JP 2018535967A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- pharmaceutically acceptable
- acceptable salt
- independently
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
- 229910052739 hydrogen Inorganic materials 0.000 claims description 54
- 239000001257 hydrogen Substances 0.000 claims description 54
- 150000001875 compounds Chemical class 0.000 claims description 44
- 125000000217 alkyl group Chemical group 0.000 claims description 36
- 150000003839 salts Chemical class 0.000 claims description 32
- 150000002431 hydrogen Chemical group 0.000 claims description 27
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 25
- 125000005843 halogen group Chemical group 0.000 claims description 22
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 20
- 125000000623 heterocyclic group Chemical group 0.000 claims description 18
- 125000003545 alkoxy group Chemical group 0.000 claims description 15
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims description 14
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 14
- 239000008194 pharmaceutical composition Substances 0.000 claims description 14
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 13
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 8
- 239000000203 mixture Substances 0.000 claims description 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 6
- 125000001072 heteroaryl group Chemical group 0.000 claims description 6
- 238000000034 method Methods 0.000 claims description 6
- 125000004104 aryloxy group Chemical group 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 4
- 125000001153 fluoro group Chemical group F* 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 201000011510 cancer Diseases 0.000 claims description 3
- 230000001404 mediated effect Effects 0.000 claims description 3
- 125000004001 thioalkyl group Chemical group 0.000 claims description 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 2
- 125000003342 alkenyl group Chemical group 0.000 claims description 2
- 125000000304 alkynyl group Chemical group 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 2
- 150000003573 thiols Chemical group 0.000 claims description 2
- -1 C 1 -C 6 alkoxy Chemical group 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000001976 Endocrine Gland Neoplasms Diseases 0.000 claims 1
- 208000009018 Medullary thyroid cancer Diseases 0.000 claims 1
- 206010033701 Papillary thyroid cancer Diseases 0.000 claims 1
- 101150077555 Ret gene Proteins 0.000 claims 1
- 201000011523 endocrine gland cancer Diseases 0.000 claims 1
- 230000004927 fusion Effects 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 208000023356 medullary thyroid gland carcinoma Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 208000030045 thyroid gland papillary carcinoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 description 4
- 239000003814 drug Substances 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 230000002159 abnormal effect Effects 0.000 description 2
- 125000002947 alkylene group Chemical group 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 description 1
- 125000004353 pyrazol-1-yl group Chemical group [H]C1=NN(*)C([H])=C1[H] 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562249784P | 2015-11-02 | 2015-11-02 | |
| US62/249,784 | 2015-11-02 | ||
| US201662367960P | 2016-07-28 | 2016-07-28 | |
| US62/367,960 | 2016-07-28 | ||
| PCT/US2016/059879 WO2017079140A1 (en) | 2015-11-02 | 2016-11-01 | Inhibitors of ret |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020202520A Division JP7026196B2 (ja) | 2015-11-02 | 2020-12-07 | Ｒｅｔの阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018535967A JP2018535967A (ja) | 2018-12-06 |
| JP2018535967A5 true JP2018535967A5 (enExample) | 2020-03-26 |
| JP6807385B2 JP6807385B2 (ja) | 2021-01-06 |
Family
ID=57286889
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018521916A Active JP6807385B2 (ja) | 2015-11-02 | 2016-11-01 | Ｒｅｔの阻害剤 |
| JP2020202520A Expired - Fee Related JP7026196B2 (ja) | 2015-11-02 | 2020-12-07 | Ｒｅｔの阻害剤 |
| JP2022020355A Pending JP2022058976A (ja) | 2015-11-02 | 2022-02-14 | Ｒｅｔの阻害剤 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020202520A Expired - Fee Related JP7026196B2 (ja) | 2015-11-02 | 2020-12-07 | Ｒｅｔの阻害剤 |
| JP2022020355A Pending JP2022058976A (ja) | 2015-11-02 | 2022-02-14 | Ｒｅｔの阻害剤 |
Country Status (31)
| Country | Link |
|---|---|
| US (5) | US10030005B2 (enExample) |
| EP (3) | EP4292594A3 (enExample) |
| JP (3) | JP6807385B2 (enExample) |
| KR (1) | KR20180073689A (enExample) |
| CN (2) | CN111423416B (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 (69)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2011256380C1 (en) | 2010-05-20 | 2016-09-08 | Array Biopharma Inc. | Macrocyclic compounds as Trk kinase inhibitors |
| BR112015000653A2 (pt) | 2012-07-11 | 2019-11-05 | Blueprint Medicines Corp | compostos inibidores do receptor de fator de crescimento de fibroblasto, sua composição farmacêutica e seus usos |
| US9499522B2 (en) | 2013-03-15 | 2016-11-22 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| RS57542B1 (sr) | 2013-10-17 | 2018-10-31 | Blueprint Medicines Corp | Kompozicije korisne za lečenje poremećaja povezanih sa kit-om |
| DK3395814T3 (da) | 2013-10-25 | 2022-07-04 | Blueprint Medicines Corp | Hæmmere af fibroblastvækstfaktorreceptoren |
| WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
| US10202365B2 (en) | 2015-02-06 | 2019-02-12 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors |
| JP6816100B2 (ja) | 2015-07-16 | 2021-01-20 | アレイ バイオファーマ、インコーポレイテッド | ＲＥＴキナーゼ阻害物質としての置換ピラゾロ［１，５−ａ］ピリジン化合物 |
| JP2018521076A (ja) | 2015-07-24 | 2018-08-02 | ブループリント メディシンズ コーポレイション | Ｋｉｔ及びｐｄｇｆｒに関連する疾病を治療するのに有用な化合物 |
| CA2995997A1 (en) | 2015-08-26 | 2017-03-02 | Blueprint Medicines Corporation | Compounds and compositions useful for treating disorders related to ntrk |
| TWI787018B (zh) | 2015-11-02 | 2022-12-11 | 美商纜圖藥品公司 | 轉染過程重排之抑制劑 |
| KR20180081790A (ko) | 2015-11-19 | 2018-07-17 | 블루프린트 메디신즈 코포레이션 | Ntrk 관련 장애의 치료에 유용한 화합물 및 조성물 |
| UY37155A (es) | 2016-03-17 | 2017-10-31 | Blueprint Medicines Corp | Inhibidores de ret |
| FI3442977T3 (fi) | 2016-04-15 | 2023-09-26 | Blueprint Medicines Corp | Aktiviinireseptorin kaltaisen kinaasin estäjät |
| AU2017263174A1 (en) | 2016-05-13 | 2018-12-13 | Instituto de Medicina Molecular João Lobo Antunes | Methods of treating diseases associated with ILC3 cells |
| US10227329B2 (en) | 2016-07-22 | 2019-03-12 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
| US10035789B2 (en) * | 2016-07-27 | 2018-07-31 | Blueprint Medicines Corporation | Compounds useful 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 |
| EP3624802A1 (en) * | 2017-05-15 | 2020-03-25 | 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 |
| TW201938169A (zh) | 2018-01-18 | 2019-10-01 | 美商亞雷生物製藥股份有限公司 | 作為RET激酶抑制劑之經取代吡唑并[3,4-d]嘧啶化合物 |
| JP6997876B2 (ja) | 2018-01-18 | 2022-02-04 | アレイ バイオファーマ インコーポレイテッド | Ｒｅｔキナーゼ阻害剤としての置換ピラゾリル［４，３－ｃ］ピリジン化合物 |
| US11603374B2 (en) | 2018-01-18 | 2023-03-14 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| CA3096043A1 (en) | 2018-04-03 | 2019-10-10 | Blueprint Medicines Corporation | Ret inhibitor for use in treating cancer having a ret alteration |
| CN112703014A (zh) | 2018-08-10 | 2021-04-23 | 缆图药品公司 | Egfr突变型癌症的治疗 |
| CN112566907A (zh) * | 2018-08-17 | 2021-03-26 | 南京明德新药研发有限公司 | 作为ret抑制剂的吡唑衍生物 |
| CA3111984A1 (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 |
| BR112021016299A2 (pt) | 2019-02-19 | 2021-10-13 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Composto heterocíclico, composição farmacêutica compreendendo o mesmo, método de preparação do mesmo e uso do mesmo |
| CN113474345B (zh) * | 2019-04-03 | 2023-04-18 | 广州白云山医药集团股份有限公司白云山制药总厂 | 作为ret抑制剂的含氮螺环衍生物 |
| CN113966334B (zh) | 2019-04-12 | 2025-01-21 | 缆图药品公司 | 化合物(i)的晶体形式 |
| 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 |
| 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 |
| CN113698390B (zh) * | 2020-05-20 | 2022-09-27 | 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 |
| CA3183728A1 (en) * | 2020-05-29 | 2021-12-02 | Blueprint Medicines Corporation | Solid forms of pralsetinib |
| BR112022024374A2 (pt) * | 2020-05-29 | 2023-05-02 | Blueprint Medicines Corp | Composições farmacêuticas de pralsetinibe |
| 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 |
| US20230391746A1 (en) | 2020-10-19 | 2023-12-07 | 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 |
| CR20230294A (es) * | 2020-12-04 | 2023-07-26 | 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 |
| IL309027A (en) | 2021-06-03 | 2024-02-01 | Fundac?O D Anna De Sommer Champalimaud E Dr Carlos Montez Champalimaud | Neuro-messenger units that control ILC2 and obesity in brain fat cell circuit findings |
| 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 |
| AU2023329563A1 (en) | 2022-08-24 | 2025-02-27 | Toray Industries, Inc. | Medicament for treatment and/or prevention of cancer |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | 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. |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | 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 |
Family Cites Families (84)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001060816A1 (en) | 2000-02-17 | 2001-08-23 | 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 |
| CN1925855B (zh) | 2003-12-19 | 2010-06-16 | 普莱希科公司 | 开发Ret调节剂的化合物和方法 |
| US8227455B2 (en) * | 2005-04-18 | 2012-07-24 | Rigel Pharmaceuticals, Inc. | Methods of treating cell proliferative disorders |
| US20100047777A1 (en) | 2005-05-26 | 2010-02-25 | The Johns Hopkins University | Methods for identifying mutations in coding and non-coding dna |
| 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 |
| WO2008061201A1 (en) * | 2006-11-15 | 2008-05-22 | 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 |
| EA201000092A1 (ru) | 2007-07-09 | 2010-06-30 | Астразенека Аб | Тризамещенные пиримидиновые производные для лечения пролиферативных заболеваний |
| KR101552742B1 (ko) | 2007-07-19 | 2015-09-11 | 머크 샤프 앤드 돔 코포레이션 | 단백질 키나제 억제제로서의 헤테로사이클릭 아미드 화합물 |
| AU2008282156B2 (en) * | 2007-07-31 | 2014-07-17 | Vertex Pharmaceuticals Incorporated | 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 |
| EP2411011A4 (en) * | 2009-03-24 | 2012-08-15 | Msd Kk | NEW AMINO-PYRIDINE DERIVATIVES WITH SELECTIVE AURORA A INHIBITION |
| CA2765044A1 (en) * | 2009-06-09 | 2010-12-16 | California Capital Equity, Llc | Benzyl substituted triazine derivatives and their therapeutical applications |
| EA201290255A1 (ru) | 2009-10-30 | 2013-04-30 | Ариад Фармасьютикалз, Инк. | Способы и композиции для лечения рака |
| EP2498607B1 (en) | 2009-11-13 | 2016-02-17 | Genosco | Kinase inhibitors |
| KR20140047138A (ko) | 2011-08-04 | 2014-04-21 | 도쿠리츠교세이호진 고쿠리츠간켄큐센터 | Ｋｉｆ5ｂ 유전자와 ｒｅｔ 유전자와의 융합 유전자, 및 당해 융합 유전자를 표적으로 한 암 치료의 유효성을 판정하는 방법 |
| BR112014004213A2 (pt) | 2011-08-23 | 2017-06-20 | Found Medicine Inc | novas moléculas de fusão kif5b-ret e usos das mesmas |
| 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 |
| RU2646754C2 (ru) * | 2012-04-25 | 2018-03-07 | Раквалиа Фарма Инк. | Производные пирролопиридинона в качестве ttx-s блокаторов |
| CA2871540A1 (en) | 2012-05-10 | 2013-11-14 | Synta Pharmaceuticals Corp. | Treating cancer with hsp90 inhibitory compounds |
| BR112015000653A2 (pt) | 2012-07-11 | 2019-11-05 | Blueprint Medicines Corp | compostos inibidores do receptor de fator de crescimento de fibroblasto, sua composição farmacêutica e seus usos |
| 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 |
| ES2726605T3 (es) | 2012-09-07 | 2019-10-08 | Exelixis Inc | Inhibidores de MET, VEGFR y RET para usar en el tratamiento del adenocarcinoma de pulmón |
| JP5759568B2 (ja) * | 2012-09-25 | 2015-08-05 | 中外製薬株式会社 | Ｒｅｔ阻害剤 |
| US9604980B2 (en) | 2012-11-07 | 2017-03-28 | Nerviano Medical Sciences S.R.L. | Substituted pyrimidinyl and pyridinyl-pyrrolopyridinones, process for their preparation and their use as kinase inhibitors |
| 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 |
| KR20150121712A (ko) | 2013-02-25 | 2015-10-29 | 브리스톨-마이어스 스큅 컴퍼니 | Hiv의 치료에 유용한 c-3 알킬 및 알케닐 개질된 베툴린산 유도체 |
| UA115264C2 (uk) * | 2013-03-15 | 2017-10-10 | Глаксосмітклайн Інтеллектьюел Проперті Девелопмент Лімітед | Піридинові похідні як інгібітори реаранжованої у процесі трансфекції (ret) кінази |
| US9499522B2 (en) | 2013-03-15 | 2016-11-22 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| WO2015006875A1 (en) | 2013-07-18 | 2015-01-22 | Methylgene Inc. | Process for the preparation of substituted pyrimidines |
| US20150057335A1 (en) | 2013-08-20 | 2015-02-26 | National Cancer Center | Novel fusion genes identified in lung cancer |
| RS57542B1 (sr) | 2013-10-17 | 2018-10-31 | Blueprint Medicines Corp | Kompozicije korisne za lečenje poremećaja povezanih sa kit-om |
| US9334263B2 (en) | 2013-10-17 | 2016-05-10 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| DK3395814T3 (da) | 2013-10-25 | 2022-07-04 | Blueprint Medicines Corp | Hæmmere af fibroblastvækstfaktorreceptoren |
| GB201321146D0 (en) | 2013-11-29 | 2014-01-15 | Cancer Rec Tech Ltd | Quinazoline compounds |
| WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
| WO2016022569A1 (en) | 2014-08-04 | 2016-02-11 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| 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 |
| RS58813B1 (sr) | 2014-09-10 | 2019-07-31 | Glaxosmithkline Ip Dev Ltd | Piridonski derivati korišćeni kao inhibitori kinaze reorganizovane tokom transfekcije (ret) |
| 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 |
| US10202365B2 (en) | 2015-02-06 | 2019-02-12 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors |
| JP6816100B2 (ja) | 2015-07-16 | 2021-01-20 | アレイ バイオファーマ、インコーポレイテッド | ＲＥＴキナーゼ阻害物質としての置換ピラゾロ［１，５−ａ］ピリジン化合物 |
| JP2018521076A (ja) | 2015-07-24 | 2018-08-02 | ブループリント メディシンズ コーポレイション | Ｋｉｔ及びｐｄｇｆｒに関連する疾病を治療するのに有用な化合物 |
| CA2995997A1 (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 |
| TWI787018B (zh) | 2015-11-02 | 2022-12-11 | 美商纜圖藥品公司 | 轉染過程重排之抑制劑 |
| PE20181310A1 (es) | 2015-11-02 | 2018-08-10 | Janssen Pharmaceutica Nv | Anticuerpos anti-il1rap, moleculas de union a antigenos biespecificas que se unen a il1rap y cd3, y usos de estos |
| JP6936221B2 (ja) | 2015-11-02 | 2021-09-15 | ファイブ プライム セラピューティクス， インコーポレイテッド | Ｃｄ８０細胞外ドメインポリペプチドと、がん治療でのそれらの使用 |
| KR20180081790A (ko) | 2015-11-19 | 2018-07-17 | 블루프린트 메디신즈 코포레이션 | Ntrk 관련 장애의 치료에 유용한 화합물 및 조성물 |
| 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 |
| UY37155A (es) | 2016-03-17 | 2017-10-31 | Blueprint Medicines Corp | Inhibidores de ret |
| CN109069512B (zh) | 2016-04-01 | 2022-06-14 | 西格诺药品有限公司 | 取代的氨基嘌呤化合物、其组合物以及相关治疗方法 |
| EP4104837A3 (en) | 2016-04-15 | 2023-04-26 | Cancer Research Technology Limited | Heterocyclic compounds as ret kinase inhibitors |
| FI3442977T3 (fi) | 2016-04-15 | 2023-09-26 | Blueprint Medicines Corp | Aktiviinireseptorin kaltaisen kinaasin estäjät |
| ES2886587T3 (es) | 2016-04-15 | 2021-12-20 | Cancer Research Tech Ltd | Compuestos heterocíclicos como inhibidores de la quinasa RET |
| US10227329B2 (en) | 2016-07-22 | 2019-03-12 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
| US10035789B2 (en) | 2016-07-27 | 2018-07-31 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
| CN110022900A (zh) | 2016-09-08 | 2019-07-16 | 蓝图药品公司 | 成纤维细胞生长因子受体4抑制剂与细胞周期蛋白依赖性激酶抑制剂的组合 |
| 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 |
| 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 |
| WO2018102455A1 (en) | 2016-12-01 | 2018-06-07 | Ignyta, Inc. | Methods for the treatment of cancer |
| 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 |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| 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 |
| EP3624802A1 (en) | 2017-05-15 | 2020-03-25 | Blueprint Medicines Corporation | Combinations of ret inhibitors and mtorc1 inhibitors and uses thereof for the treatment of cancer mediated by aberrant ret activity |
| WO2018237134A1 (en) | 2017-06-23 | 2018-12-27 | San Diego State University Research 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 |
| EP4095258A1 (en) | 2017-07-07 | 2022-11-30 | Nipd Genetics Public Company Limited | Target-enriched multiplexed parallel analysis for assesment of tumor biomarkers |
| SI3728271T1 (sl) | 2017-12-19 | 2023-01-31 | Turning Point Therapeutics, Inc. | Makrociklične spojine za zdravljenje bolezni |
| JP6997876B2 (ja) | 2018-01-18 | 2022-02-04 | アレイ バイオファーマ インコーポレイテッド | Ｒｅｔキナーゼ阻害剤としての置換ピラゾリル［４，３－ｃ］ピリジン化合物 |
| US11603374B2 (en) | 2018-01-18 | 2023-03-14 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| TW201938169A (zh) | 2018-01-18 | 2019-10-01 | 美商亞雷生物製藥股份有限公司 | 作為RET激酶抑制劑之經取代吡唑并[3,4-d]嘧啶化合物 |
| CA3096043A1 (en) | 2018-04-03 | 2019-10-10 | Blueprint Medicines Corporation | Ret inhibitor for use in treating cancer having a ret alteration |
| CN112703014A (zh) | 2018-08-10 | 2021-04-23 | 缆图药品公司 | Egfr突变型癌症的治疗 |
-
2016
- 2016-11-01 TW TW110148980A patent/TWI787018B/zh active
- 2016-11-01 JP JP2018521916A patent/JP6807385B2/ja active Active
- 2016-11-01 RS RS20240044A patent/RS65069B1/sr unknown
- 2016-11-01 FI FIEP16794885.0T patent/FI3371171T3/fi active
- 2016-11-01 EP EP23201915.8A patent/EP4292594A3/en active Pending
- 2016-11-01 CN CN202010391097.9A patent/CN111423416B/zh active Active
- 2016-11-01 BR BR112018008877-3A patent/BR112018008877B1/pt not_active IP Right Cessation
- 2016-11-01 CA CA3003721A patent/CA3003721C/en active Active
- 2016-11-01 MX MX2018005528A patent/MX384884B/es unknown
- 2016-11-01 SI SI201631796T patent/SI3371171T1/sl unknown
- 2016-11-01 KR KR1020187015706A patent/KR20180073689A/ko not_active Ceased
- 2016-11-01 NZ NZ742351A patent/NZ742351A/en not_active IP Right Cessation
- 2016-11-01 HR HRP20231681TT patent/HRP20231681T1/hr unknown
- 2016-11-01 US US15/340,428 patent/US10030005B2/en active Active
- 2016-11-01 HU HUE16794885A patent/HUE064659T2/hu unknown
- 2016-11-01 CN CN201680076816.XA patent/CN108473468B/zh active Active
- 2016-11-01 MY MYPI2018701728A patent/MY194262A/en unknown
- 2016-11-01 PL PL16794885.0T patent/PL3371171T3/pl unknown
- 2016-11-01 EP EP23201930.7A patent/EP4331585A3/en not_active Withdrawn
- 2016-11-01 LT LTEPPCT/US2016/059879T patent/LT3371171T/lt unknown
- 2016-11-01 ES ES16794885T patent/ES2969185T3/es active Active
- 2016-11-01 AU AU2016348402A patent/AU2016348402B2/en not_active Ceased
- 2016-11-01 DK DK16794885.0T patent/DK3371171T3/da active
- 2016-11-01 WO PCT/US2016/059879 patent/WO2017079140A1/en not_active Ceased
- 2016-11-01 IL IL302209A patent/IL302209B2/en unknown
- 2016-11-01 SG SG11201803653QA patent/SG11201803653QA/en unknown
- 2016-11-01 TW TW105135376A patent/TWI757256B/zh active
- 2016-11-01 PT PT167948850T patent/PT3371171T/pt unknown
- 2016-11-01 EA EA201891087A patent/EA038890B1/ru unknown
- 2016-11-01 EP EP16794885.0A patent/EP3371171B1/en active Active
- 2016-11-01 IL IL288519A patent/IL288519B2/en unknown
-
2018
- 2018-04-24 IL IL258902A patent/IL258902B/en unknown
- 2018-04-27 PH PH12018500907A patent/PH12018500907A1/en unknown
- 2018-05-02 CL CL2018001181A patent/CL2018001181A1/es unknown
- 2018-05-02 SA SA518391496A patent/SA518391496B1/ar unknown
- 2018-05-09 ZA ZA2018/03050A patent/ZA201803050B/en unknown
- 2018-07-20 US US16/041,719 patent/US10584114B2/en active Active
-
2020
- 2020-01-29 US US16/775,646 patent/US11279688B2/en active Active
- 2020-12-07 JP JP2020202520A patent/JP7026196B2/ja not_active Expired - Fee Related
-
2022
- 2022-02-11 US US17/669,785 patent/US20220315560A1/en not_active Abandoned
- 2022-02-14 JP JP2022020355A patent/JP2022058976A/ja active Pending
-
2024
- 2024-01-25 US US18/422,258 patent/US20240417386A1/en active Pending
- 2024-04-19 FR FR24C1016C patent/FR24C1016I1/fr active Active