JP2018535967A5 - - Google Patents
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- 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.)
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- 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) | 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) | IL288519B2 (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 (83)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102015402B1 (ko) | 2010-05-20 | 2019-08-28 | 어레이 바이오파마 인크. | Trk 키나제 저해제로서의 매크로시클릭 화합물 |
| NZ703495A (en) | 2012-07-11 | 2018-02-23 | Blueprint Medicines Corp | Inhibitors of the fibroblast growth factor receptor |
| WO2014160521A1 (en) | 2013-03-15 | 2014-10-02 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| LT3057969T (lt) | 2013-10-17 | 2018-07-10 | Blueprint Medicines Corporation | Kompozicijos, naudojamos gydyti sutrikimams, susijusiems su kit |
| 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 |
| WO2016127074A1 (en) | 2015-02-06 | 2016-08-11 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as ret inhibitors |
| HUE053067T2 (hu) | 2015-07-16 | 2021-06-28 | Array Biopharma Inc | Helyettesített pirazolo[1,5-A]piridin vegyületek, mint RET kináz inhibitorok |
| AU2016297754A1 (en) | 2015-07-24 | 2018-02-15 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to KIT and PDGFR |
| CA2995997A1 (en) | 2015-08-26 | 2017-03-02 | Blueprint Medicines Corporation | Compounds and compositions useful for treating disorders related to ntrk |
| NZ742351A (en) | 2015-11-02 | 2023-03-31 | Blueprint Medicines Corp | Inhibitors of ret |
| MX2018006195A (es) | 2015-11-19 | 2018-09-05 | Blueprint Medicines Corp | Compuestos y composiciones utiles para el tratamiento de trastornos relacionados con ntrk. |
| 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 |
| WO2018017983A1 (en) * | 2016-07-22 | 2018-01-25 | 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 |
| 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 |
| TWI752098B (zh) | 2016-10-10 | 2022-01-11 | 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 |
| US11168090B2 (en) | 2017-01-18 | 2021-11-09 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| US11040979B2 (en) | 2017-03-31 | 2021-06-22 | Blueprint Medicines Corporation | Substituted pyrrolo[1,2-b]pyridazines for treating disorders related to KIT and PDGFR |
| CN110891573A (zh) * | 2017-05-15 | 2020-03-17 | 缆图药品公司 | Ret抑制剂和mtorc1抑制剂的组合及其用于治疗由异常ret活性介导的癌症的用途 |
| 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 |
| EP3697786B1 (en) | 2017-10-18 | 2022-08-31 | Blueprint Medicines Corporation | Substituted pyrrolopyridines as inhibitors of activin receptor-like kinase |
| EP3740490A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| CA3087972C (en) | 2018-01-18 | 2023-01-10 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| EP3773589B1 (en) | 2018-04-03 | 2023-11-01 | Blueprint Medicines Corporation | Ret inhibitor for use in treating cancer having a ret alteration |
| EP3833372A4 (en) | 2018-08-10 | 2022-06-08 | Blueprint Medicines Corporation | TREATMENT OF EGFR MUTANT CANCER |
| 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 |
| JP2022500383A (ja) | 2018-09-10 | 2022-01-04 | 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縮合複素環式化合物 |
| 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 |
| EP3950688B1 (en) * | 2019-04-03 | 2025-01-15 | 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 |
| ES2966512T3 (es) | 2019-04-12 | 2024-04-22 | Blueprint Medicines Corp | Formas cristalinas de (S)-1-(4-fluorofenil)-1-(2-(4-(6-(1-metil-1H-pirazol-4-il)pirrolo[2,1-f][1,2,4]triazin-4-il)piperazinil)-pirimidin-5-il)etan-1-amina y métodos de elaboración |
| EP4424312A3 (en) | 2019-04-12 | 2025-01-08 | Blueprint Medicines Corporation | Pyrrolotriazine derivatives for treating kit- and pdgfra-mediated diseases |
| 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 |
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| CN111440151A (zh) * | 2020-03-25 | 2020-07-24 | 魏威 | 制备抗肿瘤药普拉赛替尼的方法 |
| 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 |
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| JP2024522938A (ja) | 2021-06-03 | 2024-06-21 | フンダサン デー．アンナ ジ ソーメル チャンパリマウド エー ドクトル カルロス モンテス チャンパリマウド | 脳－脂肪回路を介してｉｌｃ２および肥満度を制御する神経－間葉単位 |
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| 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 |
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