JP2018532690A5 - - Google Patents
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- JP2018532690A5 JP2018532690A5 JP2018502144A JP2018502144A JP2018532690A5 JP 2018532690 A5 JP2018532690 A5 JP 2018532690A5 JP 2018502144 A JP2018502144 A JP 2018502144A JP 2018502144 A JP2018502144 A JP 2018502144A JP 2018532690 A5 JP2018532690 A5 JP 2018532690A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- optionally substituted
- fluoro
- hetcyc
- 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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Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562193448P | 2015-07-16 | 2015-07-16 | |
| US62/193,448 | 2015-07-16 | ||
| US201562274018P | 2015-12-31 | 2015-12-31 | |
| US62/274,018 | 2015-12-31 | ||
| PCT/US2016/042576 WO2017011776A1 (en) | 2015-07-16 | 2016-07-15 | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018532690A JP2018532690A (ja) | 2018-11-08 |
| JP2018532690A5 true JP2018532690A5 (enExample) | 2019-08-29 |
| JP6816100B2 JP6816100B2 (ja) | 2021-01-20 |
Family
ID=56507905
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018502144A Active JP6816100B2 (ja) | 2015-07-16 | 2016-07-15 | 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 |
Country Status (25)
| Country | Link |
|---|---|
| US (7) | US10023570B2 (enExample) |
| EP (1) | EP3322706B1 (enExample) |
| JP (1) | JP6816100B2 (enExample) |
| KR (1) | KR20180041135A (enExample) |
| CN (1) | CN108349969B (enExample) |
| AU (1) | AU2016291676B2 (enExample) |
| BR (1) | BR112018000808A2 (enExample) |
| CA (1) | CA2992586A1 (enExample) |
| CL (1) | CL2018000119A1 (enExample) |
| DK (1) | DK3322706T3 (enExample) |
| EA (1) | EA035049B1 (enExample) |
| ES (1) | ES2857081T3 (enExample) |
| HR (1) | HRP20210177T1 (enExample) |
| HU (1) | HUE053067T2 (enExample) |
| IL (1) | IL256898B (enExample) |
| LT (1) | LT3322706T (enExample) |
| MX (1) | MX378957B (enExample) |
| PH (1) | PH12018500121A1 (enExample) |
| PL (1) | PL3322706T3 (enExample) |
| PT (1) | PT3322706T (enExample) |
| RS (1) | RS61485B1 (enExample) |
| SI (1) | SI3322706T1 (enExample) |
| TN (1) | TN2018000027A1 (enExample) |
| WO (1) | WO2017011776A1 (enExample) |
| ZA (1) | ZA201800771B (enExample) |
Families Citing this family (80)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2918588B1 (en) | 2010-05-20 | 2017-05-03 | Array Biopharma, Inc. | Macrocyclic compounds as TRK kinase inhibitors |
| US10202365B2 (en) | 2015-02-06 | 2019-02-12 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors |
| DK3322706T3 (da) * | 2015-07-16 | 2021-02-01 | Array Biopharma Inc | Substituerede pyrazolo[1,5-a]pyridin-forbindelser som ret-kinaseinhibitorer |
| EA038890B1 (ru) | 2015-11-02 | 2021-11-03 | Блюпринт Медсинс Корпорейшн | Ингибиторы ret |
| AR107912A1 (es) | 2016-03-17 | 2018-06-28 | Blueprint Medicines Corp | Inhibidores de ret |
| 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 |
| JP2018052878A (ja) | 2016-09-29 | 2018-04-05 | 第一三共株式会社 | ピリジン化合物 |
| JOP20190077A1 (ar) * | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| 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 |
| CA3049136C (en) | 2017-01-18 | 2022-06-14 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| 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 |
| MY201941A (en) | 2017-08-21 | 2024-03-25 | Taiho Pharmaceutical Co Ltd | Fusion protein of dctn1 protein with ret protein |
| 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 |
| 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 |
| WO2019143994A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| CA3087578C (en) | 2018-01-18 | 2023-08-08 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| CA3087354C (en) | 2018-01-18 | 2023-01-03 | 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 |
| EP3833372A4 (en) | 2018-08-10 | 2022-06-08 | Blueprint Medicines Corporation | TREATMENT OF EGFR MUTANT CANCER |
| CN112996794A (zh) | 2018-09-10 | 2021-06-18 | 阿雷生物药品公司 | 作为ret激酶抑制剂的稠合杂环化合物 |
| TW202017927A (zh) * | 2018-09-26 | 2020-05-16 | 大陸商重慶複創醫藥研究有限公司 | 作爲RET激酶抑制劑的取代的[1,2,4]三唑[1,5-a]吡啶化合物 |
| JP2022503932A (ja) * | 2018-09-27 | 2022-01-12 | フォチョン・ファーマシューティカルズ・リミテッド | Ｒｅｔキナーゼ阻害剤としての置換イミダゾ［１，２－ａ］ピリジン及び［１，２，４］トリアゾロ［１，５－ａ］ピリジン化合物 |
| WO2020064009A1 (zh) | 2018-09-30 | 2020-04-02 | 北京志健金瑞生物医药科技有限公司 | 取代吡唑稠环类衍生物及其制备方法和应用 |
| US11034669B2 (en) | 2018-11-30 | 2021-06-15 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| EP3878852A4 (en) * | 2018-12-06 | 2021-12-15 | Shenzhen TargetRx, Inc. | SUBSTITUTED PYRAZOLO [1,5-A] PYRIDINE COMPOUND, COMPOSITION THEREOF, AND USE THEREOF |
| JP7457709B2 (ja) * | 2018-12-07 | 2024-03-28 | サンシャイン・レイク・ファーマ・カンパニー・リミテッド | Ｒｅｔ阻害剤、医薬組成物、およびその使用 |
| 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 |
| JP7457708B2 (ja) * | 2018-12-07 | 2024-03-28 | サンシャイン・レイク・ファーマ・カンパニー・リミテッド | Ｒｅｔ阻害剤、医薬組成物およびその使用 |
| CN111592538A (zh) * | 2019-02-21 | 2020-08-28 | 南京明德新药研发有限公司 | 作为ret抑制剂的脂肪环衍生物 |
| 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 |
| AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| CN113474343B (zh) * | 2019-04-03 | 2024-01-23 | 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抑制剂的吡唑并吡啶类化合物及其应用 |
| 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 |
| WO2020228756A1 (zh) * | 2019-05-14 | 2020-11-19 | 上海翰森生物医药科技有限公司 | 含二并环类衍生物抑制剂、其制备方法和应用 |
| CA3142368A1 (en) * | 2019-06-10 | 2020-12-17 | Js Innopharm (Shanghai) Ltd | Heterocyclic compounds as kinase inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof |
| WO2021008455A1 (zh) * | 2019-07-12 | 2021-01-21 | 首药控股(北京)有限公司 | Ret选择性抑制剂及其制备方法和用途 |
| US12338253B2 (en) | 2019-08-05 | 2025-06-24 | Applied Pharmaceutical Science, Inc. | Nitrogen-containing polycyclic fused ring compound, pharmaceutical composition thereof, preparation method therefor and use thereof |
| WO2021043209A1 (zh) * | 2019-09-04 | 2021-03-11 | 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 |
| CN112574236B (zh) * | 2019-09-29 | 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 |
| WO2021057963A1 (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 |
| CN112679405B (zh) * | 2019-10-17 | 2023-12-15 | 南京富润凯德生物医药有限公司 | 一种(s)-7-氧杂-2-氮杂螺[4.5]癸烷衍生物的制备方法 |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| 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 |
| AU2020410900B2 (en) * | 2019-12-27 | 2024-06-13 | Tyk Medicines, Inc. | Compound used as RET kinase inhibitor and application thereof |
| 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 |
| 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 |
| 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 |
| 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 |
| CN113620944B (zh) * | 2020-05-07 | 2024-10-15 | 广东东阳光药业股份有限公司 | 新型的ret抑制剂、其药物组合物及其用途 |
| CN111548349A (zh) * | 2020-05-13 | 2020-08-18 | 厦门云凡医药科技有限公司 | 一种ret激酶抑制剂中间体及其制备方法 |
| CN113683611B (zh) * | 2020-05-18 | 2025-02-11 | 广东东阳光药业股份有限公司 | 新的ret抑制剂、其药物组合物及其用途 |
| KR20230017234A (ko) | 2020-05-29 | 2023-02-03 | 블루프린트 메디신즈 코포레이션 | 프랄세티닙의 고체 형태 |
| EP4190781A4 (en) * | 2020-07-28 | 2023-12-27 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | SALT AND CRYSTAL FORM OF A PYRIMIDINE COMPOUND AND PROCESS FOR PRODUCTION THEREOF |
| JP2023538517A (ja) * | 2020-08-05 | 2023-09-08 | シーフォー セラピューティクス， インコーポレイテッド | Ｒｅｔの標的分解のための化合物 |
| WO2022037643A1 (zh) * | 2020-08-20 | 2022-02-24 | 江苏正大丰海制药有限公司 | 作为ret激酶抑制剂的杂芳环化合物及其制备和应用 |
| CN114181205B (zh) * | 2020-09-14 | 2024-06-11 | 励缔(杭州)医药科技有限公司 | 吡唑并吡啶类化合物或其盐及其制备方法和用途 |
| CN114315824B (zh) * | 2020-09-29 | 2025-03-07 | 南京药石科技股份有限公司 | 一种6-溴-4-甲氧基吡唑并[1,5-a]吡啶-3-甲腈的制备方法 |
| JP7590550B2 (ja) * | 2020-09-29 | 2024-11-26 | 広州白雲山医薬集団股▲フン▼有限公司白雲山制薬総廠 | ピラゾロピリジン系化合物の結晶及びその調製方法 |
| CN114478519B (zh) * | 2020-10-23 | 2024-06-11 | 励缔(杭州)医药科技有限公司 | 吡唑并吡啶类化合物或其盐及其制备方法和用途 |
| CA3198559A1 (en) * | 2020-11-13 | 2022-05-19 | Hua Dong | Crystal form of free base of inhibitor containing bicyclic ring derivative and preparation method and application of crystal form |
| CN114478586A (zh) * | 2020-11-13 | 2022-05-13 | 上海翰森生物医药科技有限公司 | 一种含二并环类衍生物抑制剂盐或晶型及其制备方法和应用 |
| 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 |
| 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 |
| KR20240132251A (ko) | 2021-10-22 | 2024-09-03 | 유니버시티 오브 휴스턴 시스템 | 상피 조직의 만성 염증성 손상, 화생, 이형성증 및 암을 치료하기 위한 방법 및 조성물 |
| CN115772170B (zh) * | 2021-12-03 | 2025-05-16 | 徐诺药业(南京)有限公司 | 一种吡唑并[1,5-a]吡啶衍生物及其制备方法和应用 |
| US20250263409A1 (en) * | 2022-04-25 | 2025-08-21 | Eli Lilly And Company | Fgfr2 inhibitor compounds |
| WO2023216237A1 (en) * | 2022-05-13 | 2023-11-16 | Js Innomed Holdings Ltd. | Heterocyclic compounds as kinase inhibitors, compositions, and methods of use thereof |
| JP2025525917A (ja) * | 2022-08-03 | 2025-08-07 | ブリストル－マイヤーズ スクイブ カンパニー | Ｒｅｔタンパク質を調節するための化合物 |
| CN117229292B (zh) * | 2022-10-18 | 2025-08-15 | 药雅科技(上海)有限公司 | Ret抑制剂的制备及其应用 |
| CN115925680B (zh) * | 2022-12-02 | 2024-01-23 | 浙江工业大学 | 一种含三氟甲基的吡啶类化合物及其制备方法和应用 |
| WO2025034912A2 (en) * | 2023-08-07 | 2025-02-13 | Cogent Biosciences, Inc. | Compounds for fgfr inhibition |
| CN119118956A (zh) * | 2024-09-11 | 2024-12-13 | 上海电力大学 | 一种苯甘氨酸衍生物及其合成方法和应用 |
Family Cites Families (264)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4783443A (en) | 1986-03-03 | 1988-11-08 | The University Of Chicago | Amino acyl cephalosporin derivatives |
| US5877016A (en) | 1994-03-18 | 1999-03-02 | Genentech, Inc. | Human trk receptors and neurotrophic factor inhibitors |
| US5844092A (en) | 1994-03-18 | 1998-12-01 | Genentech, Inc. | Human TRK receptors and neurotrophic factor inhibitors |
| DE69736428T2 (de) | 1996-05-08 | 2007-08-30 | Biogen Idec Ma Inc., Cambridge | RET-LIGAND 3 (RetL3), UM NEURALES UND RENALES WACHSTUM ZU STIMULIEREN |
| 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 |
| MXPA02012602A (es) | 2000-06-22 | 2003-05-14 | Genentech Inc | Anticuerpos monoclonales agonistas anti-trk-c. |
| AU2002334355A1 (en) | 2001-09-06 | 2003-03-18 | 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 |
| US20090143399A1 (en) | 2003-10-14 | 2009-06-04 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Protein Kinase Inhibitors |
| WO2005044835A1 (en) | 2003-10-27 | 2005-05-19 | Genelabs Technologies, Inc. | METHODS FOR PREPARING 7-(2'-SUBSTITUTED-ß-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 |
| PT1687305E (pt) | 2003-11-21 | 2008-10-17 | Novartis Ag | Derivados de 1h-imidazoquinolina como inibidores de proteína quinase |
| BRPI0416935A (pt) | 2003-11-28 | 2007-01-16 | Novartis Ag | derivados de diaril ureia no tratamento de doenças dependentes de quìnase de proteìna |
| DK1696920T3 (en) | 2003-12-19 | 2015-01-19 | Plexxikon Inc | RELATIONS AND PROCEDURES FOR THE DEVELOPMENT OF LAW 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 |
| PE20051089A1 (es) | 2004-01-22 | 2006-01-25 | Novartis Ag | Derivados de pirazolo [1,5-a] pirimidin-7-il-amina como inhibidores de quinasa de proteina |
| US20050222171A1 (en) | 2004-01-22 | 2005-10-06 | Guido Bold | Organic compounds |
| 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 |
| CN101052629A (zh) * | 2004-08-02 | 2007-10-10 | Osi制药公司 | 芳基－氨基取代的吡咯并嘧啶多激酶抑制化合物 |
| 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 |
| EP1874731A4 (en) | 2005-04-15 | 2009-08-05 | Cylene Pharmaceuticals Inc | CHINOBENZOXAZINANALOGA AND METHOD FOR THE APPLICATION |
| AU2006248780B2 (en) | 2005-05-16 | 2010-06-03 | Astrazeneca Ab | Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors |
| US20100047777A1 (en) | 2005-05-26 | 2010-02-25 | The Johns Hopkins University | Methods for identifying mutations in coding and non-coding dna |
| CN101233129A (zh) | 2005-05-31 | 2008-07-30 | 普法尔家族联合企业（1996.7.9） | 取代的联芳杂环衍生物作为蛋白激酶抑制剂治疗癌症及其他疾病 |
| US7541367B2 (en) | 2005-05-31 | 2009-06-02 | Janssen Pharmaceutica, N.V. | 3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders |
| ITRM20050290A1 (it) | 2005-06-07 | 2006-12-08 | Lay Line Genomics Spa | Uso di molecole in grado di inibire il legame tra ngf e il suo recettore trka come analgesici ad effetto prolungato. |
| 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 |
| AU2006284096B2 (en) | 2005-08-25 | 2012-03-29 | Avro Life Sciences, Inc. | Polymer conjugates of K-252a and derivatives thereof |
| US7803806B2 (en) | 2005-11-03 | 2010-09-28 | 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 |
| US7795273B2 (en) | 2005-12-08 | 2010-09-14 | Novartis Ag | Pyrazolo[1,5-a]pyridine-3-carboxylic acids as EphB and VEGFR2 kinase inhibitors |
| EP1968579A1 (en) | 2005-12-30 | 2008-09-17 | Astex Therapeutics Limited | Pharmaceutical compounds |
| US20090227598A1 (en) | 2006-01-24 | 2009-09-10 | Buser-Doepner Carolyn A | Ret Tyrosine Kinase Inhibition |
| AU2007209689B2 (en) | 2006-01-27 | 2012-03-15 | Shanghai Hengrui Pharmaceutical Co. Ltd. | Pyrrolo [3,2-c] pyridine-4-one 2-indolinone protein kinase inhibitors |
| RU2008140382A (ru) | 2006-03-16 | 2010-04-27 | Новартис АГ (CH) | Гетероциклические органические соединения, например, для лечения меланомы |
| TWI409267B (zh) | 2006-03-17 | 2013-09-21 | Ambit Biosciences Corp | 治療疾病用之咪唑并噻唑化合物 |
| CN101410387B (zh) | 2006-03-27 | 2013-12-18 | 内尔维阿诺医学科学有限公司 | 作为激酶抑制剂的吡啶基-和嘧啶基-取代的吡咯-、噻吩-和呋喃-衍生物 |
| EP2018167A4 (en) | 2006-05-15 | 2010-07-14 | Irm Llc | COMPOSITIONS AND METHODS AS INHIBITORS OF FGF RECEPTOR KINASES |
| CA2652442C (en) | 2006-05-18 | 2014-12-09 | Eisai R & D Management Co., Ltd. | Antitumor agent for thyroid cancer |
| US8063225B2 (en) | 2006-08-14 | 2011-11-22 | Chembridge Corporation | Tricyclic compound derivatives useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders |
| US20110195072A1 (en) | 2006-09-12 | 2011-08-11 | Anne Boulay | 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 |
| EP3048099A3 (en) | 2006-11-15 | 2016-09-21 | YM BioSciences Australia Pty Ltd | Inhibitors of kinase activity |
| PE20121126A1 (es) | 2006-12-21 | 2012-08-24 | Plexxikon Inc | Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa |
| CA2673736A1 (en) | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
| 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 |
| JP2010516692A (ja) | 2007-01-19 | 2010-05-20 | バイエル・ヘルスケア・エルエルシー | 化学療法剤に対し抵抗性を有する癌の処置 |
| 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 |
| EP2152688A1 (en) | 2007-05-04 | 2010-02-17 | Irm Llc | Compounds and compositions as c-kit and pdgfr kinase inhibitors |
| WO2008138184A1 (fr) | 2007-05-14 | 2008-11-20 | Shanghai Hengrui Pharmaceutical Co.Ltd. | Dérivés de pyrrolo-azacycles, leur procédé de fabrication et leur utilisation en tant qu'inhibiteurs de protéine kinases |
| WO2009003136A1 (en) | 2007-06-26 | 2008-12-31 | Rigel Pharmaceuticals, Inc. | Substituted pyrimidine-2, 4 -diamines for treating cell proliferative disorders |
| BRPI0814818A2 (pt) | 2007-07-09 | 2019-09-10 | Astrazeneca Ab | composto, uso de um composto, métodos para produzir um efeito anti-proliferativo e um efeito inibitório de mtor quinase em uma animal de sangue quente, método para tratar doenças, e, composição farmacêutica |
| US20100209488A1 (en) | 2007-07-16 | 2010-08-19 | The Regents Of The University Of California | Protein kinase modulating compounds and methods for making and using them |
| BRPI0814423B1 (pt) | 2007-07-17 | 2022-04-19 | Plexxikon, Inc | Compostos que modulam quinase e composição farmacêutica compreendendo os mesmos |
| 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 |
| PL2176231T3 (pl) | 2007-07-20 | 2017-04-28 | Nerviano Medical Sciences S.R.L. | Podstawione pochodne indazolu aktywne jako inhibitory kinazy |
| WO2009017838A2 (en) | 2007-08-01 | 2009-02-05 | Exelixis, Inc. | Combinations of jak-2 inhibitors and other agents |
| JP5703466B2 (ja) | 2007-08-07 | 2015-04-22 | パーデュー・リサーチ・ファウンデーションＰｕｒｄｕｅ Ｒｅｓｅａｒｃｈ Ｆｏｕｎｄａｔｉｏｎ | キナーゼ阻害薬およびその使用 |
| 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 |
| JP2011501760A (ja) | 2007-10-23 | 2011-01-13 | ノバルティス アーゲー | 呼吸器疾患の処置のためのｔｒｋｂ抗体の使用 |
| EP2215091B1 (en) | 2007-12-04 | 2016-03-30 | 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 |
| CN102015769B (zh) | 2008-01-17 | 2014-12-10 | Irm责任有限公司 | 改进的抗-trkb抗体 |
| US20090227556A1 (en) | 2008-01-31 | 2009-09-10 | Eisai R&D Management Co., Ltd. | Receptor tyrosine kinase inhibitors comprising pyridine and pyrimidine derivatives |
| TW200938542A (en) | 2008-02-01 | 2009-09-16 | 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 |
| US20100029657A1 (en) * | 2008-02-29 | 2010-02-04 | Wyeth | Bridged, Bicyclic Heterocyclic or Spiro Bicyclic Heterocyclic Derivatives of Pyrazolo[1, 5-A]Pyrimidines, Methods for Preparation and Uses Thereof |
| KR101713501B1 (ko) * | 2008-03-17 | 2017-03-07 | 암비트 바이오사이언시즈 코포레이션 | Ｒａｆ 키나아제 조절제로서의 퀴나졸린 유도체 및 그의 사용방법 |
| JP5628145B2 (ja) | 2008-03-19 | 2014-11-19 | ケムブリッジ・コーポレーション | 新規チロシンキナーゼ阻害剤 |
| US8822500B2 (en) | 2008-03-19 | 2014-09-02 | Chembridge Corporation | Tyrosine kinase inhibitors |
| JP5767101B2 (ja) | 2008-03-28 | 2015-08-19 | 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３，４−ジヒドロ−２ｈ−ピラジノ［１，２−ａ］インドール−１−オン誘導体、これらの調製方法、およびこれらを含む医薬組成物 |
| 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 |
| ES2554513T3 (es) | 2008-05-23 | 2015-12-21 | Novartis Ag | Derivados de quinolinas y quinoxalinas como inhibidores de la proteína tirosina quinasa |
| JP5767965B2 (ja) | 2008-06-10 | 2015-08-26 | プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． | キナーゼを調節する５ｈ−ピロロ［２，３−ｂ］ピラジン誘導体、およびその適応症 |
| US20110212053A1 (en) | 2008-06-19 | 2011-09-01 | Dapeng Qian | Phosphatidylinositol 3 kinase inhibitors |
| EP2313091A4 (en) | 2008-07-14 | 2012-04-04 | Univ Kingston | PHARMACEUTICAL COMPOSITIONS WITH RET-HEMMERN AND METHOD FOR THE TREATMENT OF CANCER |
| US8946226B2 (en) | 2008-07-29 | 2015-02-03 | Nerviano Medical Sciences S.R.L. | Use of CDK inhibitor for the treatment of glioma |
| CN102100126B (zh) | 2008-09-01 | 2014-04-16 | 夏普株式会社 | 有机电致发光面板、有机电致发光显示器、有机电致发光照明装置和它们的制造方法 |
| 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 |
| ES2536730T3 (es) | 2008-09-19 | 2015-05-28 | Nerviano Medical Sciences S.R.L. | Derivados de 3,4-dihidro-2H-pirrolo[1,2-a]pirazin-1-ona |
| SI2350075T1 (sl) | 2008-09-22 | 2014-06-30 | Array Biopharma, Inc. | Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji |
| WO2010036629A2 (en) | 2008-09-26 | 2010-04-01 | National Health Research Institutes | Fused multicyclic compounds as protein kinase inhibitors |
| SG10201914059WA (en) | 2008-10-22 | 2020-03-30 | Array Biopharma Inc | Substituted pyrazolo[1,5-a]pyrimidine compounds as trk kinase inhibitors |
| 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 |
| US8912194B2 (en) | 2008-11-24 | 2014-12-16 | Nerviano Medical Sciences S.R.L. | CDK inhibitor for the treatment of mesothelioma |
| 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 |
| TWI410418B (zh) | 2009-04-29 | 2013-10-01 | Ind Tech Res Inst | 氮雜薁化合物、藥學組合物與抑制一細胞中蛋白質激酶之活性的方法 |
| EP3009428B1 (en) | 2009-05-08 | 2018-02-21 | Astellas Pharma Inc. | Diamino heterocyclic carboxamide compound |
| EP2440058A4 (en) | 2009-06-12 | 2012-11-21 | Dana Farber Cancer Inst Inc | MELTED HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF |
| ES2679379T3 (es) | 2009-06-15 | 2018-08-24 | Nerviano Medical Sciences S.R.L. | Derivados de pirimidinilpirrolopiridinona sustituidos, proceso para su preparación y su uso como inhibidores de cinasa |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| HRP20190016T1 (hr) * | 2009-08-17 | 2019-03-08 | Intellikine, Llc | Heterociklički spojevi i njihova upotreba |
| KR101256018B1 (ko) | 2009-08-20 | 2013-04-18 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물 |
| US20120157451A1 (en) * | 2009-08-28 | 2012-06-21 | Genentech, Inc | Raf inhibitor compounds and methods of use thereof |
| EP2470532A1 (en) * | 2009-08-28 | 2012-07-04 | Array Biopharma, Inc. | 1h-pyrazolo [ 3, 4-b]pyridine compounds for inhibiting raf kinase |
| 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 |
| US8404677B2 (en) | 2009-10-29 | 2013-03-26 | Genosco | Kinase inhibitors |
| WO2011060295A1 (en) | 2009-11-13 | 2011-05-19 | Genosco | Kinase inhibitors |
| KR101094446B1 (ko) | 2009-11-19 | 2011-12-15 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노［3,2-ｄ］피리미딘 화합물 |
| CA2784807C (en) | 2009-12-29 | 2021-12-14 | 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 |
| US8772279B2 (en) | 2010-01-29 | 2014-07-08 | Nerviano Medical Sciences S.R.L. | 6,7-dihydroimidazo[1,5-a]pyrazin-8(5H)-one derivatives as protein kinase modulators |
| EP2528925B1 (en) | 2010-01-29 | 2017-07-05 | Hanmi Science Co., Ltd. | THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY ON PROTEIN KINASES |
| ES2594927T3 (es) | 2010-02-18 | 2016-12-23 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Métodos para prevenir las metástasis cancerosas |
| TWI619713B (zh) | 2010-04-21 | 2018-04-01 | 普雷辛肯公司 | 用於激酶調節的化合物和方法及其適應症 |
| JP2013526543A (ja) * | 2010-05-12 | 2013-06-24 | アッヴィ・インコーポレイテッド | ピロロピリジン系およびピロロピリミジン系キナーゼ阻害薬 |
| EP2918588B1 (en) | 2010-05-20 | 2017-05-03 | Array Biopharma, Inc. | Macrocyclic compounds as TRK kinase inhibitors |
| 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 |
| 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 |
| EP2668190B1 (en) | 2011-01-26 | 2016-08-17 | Nerviano Medical Sciences S.r.l. | Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors |
| WO2012101029A1 (en) | 2011-01-26 | 2012-08-02 | Nerviano Medical Sciences S.R.L. | Tricyclic derivatives, process for their preparation and their use as kinase inhibitors |
| 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 |
| EP2678336B1 (en) | 2011-02-24 | 2016-04-20 | Nerviano Medical Sciences S.r.l. | Thiazolylphenyl-benzenesulfonamido derivatives as kinase inhibitors |
| JP5959541B2 (ja) | 2011-02-25 | 2016-08-02 | ノバルティス アーゲー | Ｔｒｋ阻害剤としてのピラゾロ［１，５−ａ］ピリジン |
| 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 |
| EP2699564B1 (en) | 2011-04-19 | 2016-12-14 | 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 |
| ES2611779T3 (es) | 2011-05-12 | 2017-05-10 | Nerviano Medical Sciences S.R.L. | Derivados de indazol sustituidos activos como inhibidores de quinasas |
| SI2712358T1 (sl) | 2011-05-13 | 2017-03-31 | Array Biopharma, Inc. | Spojine pirolidinil sečnine, pirolidinil tiosečnine in pirolidinil gvanidina kot inhibitorji kinaze trka |
| 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 |
| EP2740742B1 (en) | 2011-08-04 | 2018-03-14 | National Cancer Center | Fusion gene of kif5b gene and ret gene, and method for determining effectiveness of cancer treatment targeting fusion gene |
| WO2013028817A1 (en) | 2011-08-23 | 2013-02-28 | Foundation Medicine , Inc. | Novel kif5b-ret fusion molecules and uses thereof |
| MX370814B (es) | 2011-09-02 | 2020-01-08 | Univ California | Pirazolo[3,4-d]pirimidinas sustituidas y usos de las mismas. |
| WO2013036232A2 (en) | 2011-09-08 | 2013-03-14 | Deciphera Pharmaceuticals, Llc | Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases |
| 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 |
| US20150306086A1 (en) | 2011-11-14 | 2015-10-29 | Tesaro, Inc. | Modulating certain tyrosine kinases |
| EP2749642A4 (en) | 2011-11-30 | 2015-03-04 | Nat Cancer Ct | INDUCED MALIGNE STEM CELLS |
| 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 |
| BR112014015720B1 (pt) | 2011-12-30 | 2020-03-17 | Hanmi Pharm. Co., Ltd. | Derivados de tieno[3,2-d]pirimidina, composição farmacêutica e uso dos mesmos para a prevenção ou tratamento de uma doença causada por ativação anormal de uma proteína quinase |
| 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 |
| ES2605388T3 (es) | 2012-04-26 | 2017-03-14 | Ono Pharmaceutical Co., Ltd. | Compuesto inhibidor de Trk |
| AU2013259267A1 (en) | 2012-05-10 | 2014-11-06 | Synta Pharmaceuticals Corp. | Treating cancer with Hsp90 inhibitory compounds |
| ES2751944T3 (es) | 2012-05-23 | 2020-04-02 | Nerviano Medical Sciences Srl | Proceso para la preparación de N-[5-(3,5-difluoro-bencil)-1H-indazol-3-il]-4-(4-metil-piperazin-1-il)-2-(tetrahidro-piran-4-ilamino)-benzamida |
| 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 |
| US8802697B2 (en) | 2012-07-11 | 2014-08-12 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| JPWO2014017491A1 (ja) | 2012-07-26 | 2016-07-11 | 国立研究開発法人国立がん研究センター | Ｃｅｐ５５遺伝子とｒｅｔ遺伝子との融合遺伝子 |
| DK2880025T3 (en) | 2012-08-02 | 2019-03-18 | Nerviano Medical Sciences Srl | SUBSTITUTED PYROLES ACTIVE AS KINase INHIBITORS |
| US20140121239A1 (en) | 2012-09-07 | 2014-05-01 | Exelixis, Inc. | Method of treating lung adenocarcinoma |
| SG11201502211QA (en) | 2012-09-25 | 2015-05-28 | 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 |
| AR093457A1 (es) | 2012-11-12 | 2015-06-10 | Cephalon Inc | Derivados de bendamustina y metodos para utilizarlos |
| 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 |
| RU2664541C2 (ru) | 2012-11-13 | 2018-08-20 | Эррэй Биофарма Инк. | Бициклические соединения мочевины, тиомочевины, гуанидина и цианогуанидина, пригодные для лечения боли |
| US9809578B2 (en) | 2012-11-13 | 2017-11-07 | Array Biopharma Inc. | Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors |
| WO2014078322A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| WO2014078331A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-(arylalkyl)-n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| WO2014078408A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9790178B2 (en) | 2012-11-13 | 2017-10-17 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| WO2014078328A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| ES2664331T3 (es) | 2012-11-13 | 2018-04-19 | Array Biopharma, Inc. | Compuestos de N-pirrolidinilo, N'-pirazolilurea, tiourea, guanidina y cianoguanidina como inhibidores de la cinasa Trka |
| US9828360B2 (en) | 2012-11-13 | 2017-11-28 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| JP2016502536A (ja) | 2012-11-29 | 2016-01-28 | イェダ リサーチ アンド デベロップメント カンパニー リミテッド | 腫瘍転移を防止し、がんを処置および予後診断し、推定転移阻害剤である薬剤を同定する方法 |
| CN103848785B (zh) | 2012-12-04 | 2016-07-13 | 上海医药集团股份有限公司 | 一类氘代3-氰基喹啉类化合物、其药用组合物、制备方法及其用途 |
| FR3000493A1 (fr) | 2012-12-28 | 2014-07-04 | Oribase Pharma | Nouveaux inhibiteurs de proteines kinases |
| FR3000492B1 (fr) | 2012-12-28 | 2015-09-11 | Oribase Pharma | Nouveaux derives azaindole en tant qu'inhibiteurs multikinases |
| FR3000494B1 (fr) | 2012-12-28 | 2015-08-21 | Oribase Pharma | Nouveaux derives d'azaindoles en tant qu'inhibiteurs de proteines kinases |
| RU2671847C2 (ru) | 2012-12-28 | 2018-11-07 | Кристалдженомикс, Инк. | Производные 2,3-дигидро-изоиндол-1-она и способы их применения в качестве ингибиторов тирозинкиназы брутона |
| HUE042591T2 (hu) | 2013-02-19 | 2019-07-29 | Ono Pharmaceutical Co | TRK-gátló vegyület |
| US20160151461A1 (en) | 2013-03-14 | 2016-06-02 | The Trustees Of The University Of Pennsylvania | Cardio-Metabolic and Vascular Effects of GLP-1 Metabolites |
| WO2014160521A1 (en) | 2013-03-15 | 2014-10-02 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| US8937071B2 (en) | 2013-03-15 | 2015-01-20 | Glaxosmithkline Intellectual Property Development Limited | Compounds as rearranged during transfection (RET) inhibitors |
| PE20151538A1 (es) | 2013-03-15 | 2015-11-18 | Glaxosmithkline Ip Dev Ltd | Nuevos compuestos como inhibidores de reorganizado durante la transfeccion (ret) |
| WO2014184069A1 (en) | 2013-05-14 | 2014-11-20 | Nerviano Medical Sciences S.R.L. | Pyrrolo[2,3-d]pyrimidine derivatives, process for their preparation and their use as kinase inhibitors |
| CA2912568A1 (en) | 2013-05-30 | 2014-12-04 | 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 |
| US20150057335A1 (en) | 2013-08-20 | 2015-02-26 | National Cancer Center | Novel fusion genes identified in lung cancer |
| RU2016111675A (ru) | 2013-08-30 | 2017-10-04 | Эмбит Байосайенсиз Корпорейшн | Соединения биарилацетамида и способы их применения |
| ES2683127T3 (es) | 2013-10-17 | 2018-09-25 | Blueprint Medicines Corporation | Composiciones útiles para tratar trastornos relacionados con la KIT |
| WO2015058129A1 (en) | 2013-10-17 | 2015-04-23 | 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 |
| EP3076966A2 (en) | 2013-12-02 | 2016-10-12 | BerGenBio AS | Use of kinase inhibitors |
| EP3087070B1 (en) * | 2013-12-26 | 2017-11-08 | Ignyta, Inc. | Pyrazolo[1,5-a]pyridine derivatives and methods of their use |
| WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
| EP3636649B1 (en) | 2014-01-24 | 2024-02-14 | Turning Point Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
| EP3738952A1 (en) | 2014-02-14 | 2020-11-18 | Exelixis, Inc. | Crystalline solid forms of n-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use |
| US10231965B2 (en) | 2014-02-20 | 2019-03-19 | Ignyta, Inc. | Molecules for administration to ROS1 mutant cancer cells |
| US20170044622A1 (en) | 2014-04-18 | 2017-02-16 | Blueprint Medicines Corporation | Pik3ca fusions |
| WO2015161277A1 (en) | 2014-04-18 | 2015-10-22 | Blueprint Medicines Corporation | Met fusions |
| PT3154959T (pt) | 2014-05-15 | 2019-09-24 | Array Biopharma Inc | 1-((3s,4r)-4-(3-fluorofenil)-1-(2-metoxietil)-pirrolidin-3-il)-3-(4-metil-3-(2-metilpirimidin-5-il)-1-fenil-1h-pirazol-5-il)ureia como inibidor da cinase trka |
| US10246750B2 (en) | 2014-06-10 | 2019-04-02 | Blueprint Medicines Corporation | Method for detection of a TECR:PKN1 or an ANXA4:PKN1 gene fusion |
| WO2015191666A2 (en) | 2014-06-10 | 2015-12-17 | Blueprint Medicines Corporation | Raf1 fusions |
| EP3169804B3 (en) | 2014-07-17 | 2019-09-18 | Blueprint Medicines Corporation | Fgr fusions |
| EP3169809B1 (en) | 2014-07-17 | 2020-04-29 | Blueprint Medicines Corporation | Prkc fusions |
| AU2015291522B2 (en) | 2014-07-17 | 2018-12-06 | Sunshine Lake Pharma Co., Ltd. | Substituted urea derivatives and pharmaceutical uses thereof |
| WO2016011144A1 (en) | 2014-07-17 | 2016-01-21 | Blueprint Medicines Corporation | Tert fusions |
| WO2016022569A1 (en) | 2014-08-04 | 2016-02-11 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| KR20170042591A (ko) | 2014-08-18 | 2017-04-19 | 오노 야꾸힝 고교 가부시키가이샤 | Trk 저해 화합물의 산부가염 |
| WO2016038519A1 (en) | 2014-09-08 | 2016-03-17 | Glaxosmithkline Intellectual Property Development Limited | Crystalline forms of 2-(4-(4-ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-n-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)acetamide |
| US9879021B2 (en) | 2014-09-10 | 2018-01-30 | Glaxosmithkline Intellectual Property Development Limited | Compounds as rearranged during transfection (RET) inhibitors |
| PL3191450T3 (pl) | 2014-09-10 | 2019-08-30 | Glaxosmithkline Intellectual Property Development Limited | Pochodne pirydonu jako inhibitory kinazy rearanżowanej podczas transfekcji (ret) |
| TWI538914B (zh) | 2014-10-03 | 2016-06-21 | 國立交通大學 | 蛋白質激酶之選擇性抑制劑、其醫藥組成物及其用途 |
| CA2967125C (en) | 2014-11-14 | 2022-10-25 | Nerviano Medical Sciences S.R.L. | 6-amino-7-bicyclo-7-deaza-purine derivatives as protein kinase inhibitors |
| US10799505B2 (en) | 2014-11-16 | 2020-10-13 | Array Biopharma, Inc. | Crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-A]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate |
| WO2016081450A1 (en) | 2014-11-18 | 2016-05-26 | Blueprint Medicines Corporation | Prkacb fusions |
| EP3233840B1 (en) | 2014-12-16 | 2018-11-21 | Eudendron S.r.l. | Heterocyclic derivatives modulating activity of certain protein kinases |
| US10202365B2 (en) | 2015-02-06 | 2019-02-12 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors |
| KR101675984B1 (ko) | 2015-02-23 | 2016-11-14 | 한양대학교 에리카산학협력단 | 티에노디아제핀 유도체 또는 이의 약학적으로 허용가능한 염, 및 이를 유효성분으로 포함하는 약학적 조성물 |
| WO2016141169A1 (en) | 2015-03-03 | 2016-09-09 | Caris Mpi, Inc. | Molecular profiling for cancer |
| US10364247B2 (en) | 2015-04-21 | 2019-07-30 | Ruijin Hospital Affiliated To Shanghai Jiao Tong University School Of Medicine | Preparation and use of novel protein kinase inhibitors |
| GB201512365D0 (en) | 2015-07-15 | 2015-08-19 | King S College London | Novel therapy |
| DK3322706T3 (da) * | 2015-07-16 | 2021-02-01 | Array Biopharma Inc | Substituerede pyrazolo[1,5-a]pyridin-forbindelser som ret-kinaseinhibitorer |
| 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 |
| EA038890B1 (ru) | 2015-11-02 | 2021-11-03 | Блюпринт Медсинс Корпорейшн | Ингибиторы ret |
| US20190002988A1 (en) | 2015-12-08 | 2019-01-03 | Boehringer Ingelheim International Gmbh | Method of using a ret fusion gene as a biomarker to select non small cell lung cancer (nsclc) and thyroid cancer patients for a cancer treatment |
| 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 |
| EP3269370B1 (en) | 2016-02-23 | 2020-01-08 | Taiho Pharmaceutical Co., Ltd. | Novel condensed pyrimidine compound or salt thereof |
| 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 |
| AR107912A1 (es) | 2016-03-17 | 2018-06-28 | Blueprint Medicines Corp | Inhibidores de ret |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| SG11201808878UA (en) | 2016-04-15 | 2018-11-29 | Cancer Research Tech Ltd | Heterocyclic compounds as ret kinase inhibitors |
| EP3442535B1 (en) | 2016-04-15 | 2022-06-01 | Cancer Research Technology Limited | Heterocyclic compounds as ret kinase inhibitors |
| 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 |
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