JP2017518981A5 - - Google Patents
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- JP2017518981A5 JP2017518981A5 JP2016567819A JP2016567819A JP2017518981A5 JP 2017518981 A5 JP2017518981 A5 JP 2017518981A5 JP 2016567819 A JP2016567819 A JP 2016567819A JP 2016567819 A JP2016567819 A JP 2016567819A JP 2017518981 A5 JP2017518981 A5 JP 2017518981A5
- Authority
- JP
- Japan
- Prior art keywords
- trka
- composition
- pain
- cancer
- compound
- 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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- 201000011510 cancer Diseases 0.000 claims description 30
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- BGKSBHPSVMJTFL-IZZNHLLZSA-N 1-[(3S,4R)-4-(3-fluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl]-3-[4-methyl-5-(2-methylpyrimidin-5-yl)-2-phenylpyrazol-3-yl]urea Chemical compound FC=1C=C(C=CC1)[C@H]1[C@@H](CN(C1)CCOC)NC(=O)NC1=C(C(=NN1C1=CC=CC=C1)C=1C=NC(=NC1)C)C BGKSBHPSVMJTFL-IZZNHLLZSA-N 0.000 claims description 4
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- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 4
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- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims description 4
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- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims description 4
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- PFKFTWBEEFSNDU-UHFFFAOYSA-N carbonyldiimidazole Chemical compound C1=CN=CN1C(=O)N1C=CN=C1 PFKFTWBEEFSNDU-UHFFFAOYSA-N 0.000 claims description 3
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- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims description 2
- 239000002144 L01XE18 - Ruxolitinib Substances 0.000 claims description 2
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- 229940125681 anticonvulsant agent Drugs 0.000 claims description 2
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- MKRTXPORKIRPDG-UHFFFAOYSA-N diphenylphosphoryl azide Chemical compound C=1C=CC=CC=1P(=O)(N=[N+]=[N-])C1=CC=CC=C1 MKRTXPORKIRPDG-UHFFFAOYSA-N 0.000 claims description 2
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- ZVHNDZWQTBEVRY-UHFFFAOYSA-N momelotinib Chemical compound C1=CC(C(NCC#N)=O)=CC=C1C1=CC=NC(NC=2C=CC(=CC=2)N2CCOCC2)=N1 ZVHNDZWQTBEVRY-UHFFFAOYSA-N 0.000 claims description 2
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- HFNKQEVNSGCOJV-OAHLLOKOSA-N ruxolitinib Chemical compound C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 HFNKQEVNSGCOJV-OAHLLOKOSA-N 0.000 claims description 2
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- ZVQOOHYFBIDMTQ-UHFFFAOYSA-N [methyl(oxido){1-[6-(trifluoromethyl)pyridin-3-yl]ethyl}-lambda(6)-sulfanylidene]cyanamide Chemical compound N#CN=S(C)(=O)C(C)C1=CC=C(C(F)(F)F)N=C1 ZVQOOHYFBIDMTQ-UHFFFAOYSA-N 0.000 description 8
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- CMIBUZBMZCBCAT-HOTGVXAUSA-N (2s,3s)-2,3-bis[(4-methylbenzoyl)oxy]butanedioic acid Chemical compound C1=CC(C)=CC=C1C(=O)O[C@H](C(O)=O)[C@@H](C(O)=O)OC(=O)C1=CC=C(C)C=C1 CMIBUZBMZCBCAT-HOTGVXAUSA-N 0.000 description 1
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- OTNVGWMVOULBFZ-UHFFFAOYSA-N sodium;hydrochloride Chemical compound [Na].Cl OTNVGWMVOULBFZ-UHFFFAOYSA-N 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
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- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 1
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461993426P | 2014-05-15 | 2014-05-15 | |
| US61/993,426 | 2014-05-15 | ||
| PCT/US2015/030795 WO2015175788A1 (en) | 2014-05-15 | 2015-05-14 | 1-((3s,4r)-4-(3-fluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)-3-(4-methyl-3-(2-methylpyrimidin-5-yl)-1-phenyl-1h-pyrazol-5-yl)urea as a trka kinase inhibitor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019048124A Division JP2019085427A (ja) | 2014-05-15 | 2019-03-15 | ＴｒｋＡキナーゼ阻害剤としての１−（（３Ｓ，４Ｒ）−４−（３−フルオロフェニル）−１−（２−メトキシエチル）ピロリジン−３−イル）−３−（４−メチル−３−（２−メチルピリミジン−５−イル）−１−フェニル−１Ｈ−ピラゾール−５−イル）尿素 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017518981A JP2017518981A (ja) | 2017-07-13 |
| JP2017518981A5 true JP2017518981A5 (enExample) | 2018-10-25 |
| JP6499672B2 JP6499672B2 (ja) | 2019-04-10 |
Family
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Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016567819A Active JP6499672B2 (ja) | 2014-05-15 | 2015-05-14 | ＴｒｋＡキナーゼ阻害剤としての１−（（３Ｓ，４Ｒ）−４−（３−フルオロフェニル）−１−（２−メトキシエチル）ピロリジン−３−イル）−３−（４−メチル−３−（２−メチルピリミジン−５−イル）−１−フェニル−１Ｈ−ピラゾール−５−イル）尿素 |
| JP2019048124A Pending JP2019085427A (ja) | 2014-05-15 | 2019-03-15 | ＴｒｋＡキナーゼ阻害剤としての１−（（３Ｓ，４Ｒ）−４−（３−フルオロフェニル）−１−（２−メトキシエチル）ピロリジン−３−イル）−３−（４−メチル−３−（２−メチルピリミジン−５−イル）−１−フェニル−１Ｈ−ピラゾール−５−イル）尿素 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019048124A Pending JP2019085427A (ja) | 2014-05-15 | 2019-03-15 | ＴｒｋＡキナーゼ阻害剤としての１−（（３Ｓ，４Ｒ）−４−（３−フルオロフェニル）−１−（２−メトキシエチル）ピロリジン−３−イル）−３−（４−メチル−３−（２−メチルピリミジン−５−イル）−１−フェニル−１Ｈ−ピラゾール−５−イル）尿素 |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US10835533B2 (enExample) |
| EP (2) | EP3154959B1 (enExample) |
| JP (2) | JP6499672B2 (enExample) |
| KR (2) | KR102321883B1 (enExample) |
| CN (2) | CN109970614B (enExample) |
| AU (2) | AU2015259075B2 (enExample) |
| CA (1) | CA2949160C (enExample) |
| CL (1) | CL2016002900A1 (enExample) |
| CR (1) | CR20160583A (enExample) |
| CY (1) | CY1122075T1 (enExample) |
| DK (1) | DK3154959T3 (enExample) |
| ES (1) | ES2746530T3 (enExample) |
| HR (1) | HRP20191593T1 (enExample) |
| HU (1) | HUE045340T2 (enExample) |
| IL (1) | IL248924B (enExample) |
| LT (1) | LT3154959T (enExample) |
| MA (1) | MA40434B1 (enExample) |
| MX (2) | MX2016014945A (enExample) |
| MY (1) | MY191956A (enExample) |
| NZ (1) | NZ727418A (enExample) |
| PH (2) | PH12016502242A1 (enExample) |
| PL (1) | PL3154959T3 (enExample) |
| PT (1) | PT3154959T (enExample) |
| RS (1) | RS59286B1 (enExample) |
| RU (1) | RU2719489C2 (enExample) |
| SG (2) | SG10201903532XA (enExample) |
| SI (1) | SI3154959T1 (enExample) |
| SM (1) | SMT201900522T1 (enExample) |
| UA (1) | UA122126C2 (enExample) |
| WO (1) | WO2015175788A1 (enExample) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2350075T1 (sl) | 2008-09-22 | 2014-06-30 | Array Biopharma, Inc. | Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji |
| BRPI0919873B8 (pt) | 2008-10-22 | 2021-05-25 | Array Biopharma Inc | compostos de pirazol[1,5-a]pirimidina substituídos como inibidores da trk quinase, seus processos de preparação e composições farmacêuticas |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| SMT201700372T1 (it) | 2010-05-20 | 2017-09-07 | Array Biopharma Inc | Composti macrociclici come inibitori di trk chinasi |
| SMT201800061T1 (it) | 2013-11-28 | 2018-05-02 | Kyorin Seiyaku Kk | Derivati dell'urea o loro sali farmacologicamente accettabili utili come io agonisti del recettore del peptide formile di tipo i (fprl-1) |
| US10231965B2 (en) | 2014-02-20 | 2019-03-19 | Ignyta, Inc. | Molecules for administration to ROS1 mutant cancer cells |
| MA40434B1 (fr) | 2014-05-15 | 2019-09-30 | Array Biopharma Inc | 1-((3s,4r)-4-(3-fluorophényl)-1-(2-méthoxyéthyl)pyrrolidin-3-yl)-3-(4-méthyl-3-(2-méthylpyrimidin-5-yl)-1-phényl-1h-pyrazol-5-yl)urée comme inhibiteur de la kinase trka |
| WO2016021629A1 (ja) | 2014-08-06 | 2016-02-11 | 塩野義製薬株式会社 | ＴｒｋＡ阻害活性を有する複素環および炭素環誘導体 |
| CA2967951C (en) | 2014-11-16 | 2023-11-07 | 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 |
| EP3722441A1 (en) | 2015-06-01 | 2020-10-14 | Loxo Oncology Inc. | Method of diagnosing a cancer for a treatment with a trk inhibitor |
| EP3330256B1 (en) * | 2015-07-07 | 2021-06-16 | Shionogi & Co., Ltd. | HETEROCYCLIC DERIVATIVE HAVING TrkA-INHIBITING ACTIVITY |
| HRP20210177T1 (hr) | 2015-07-16 | 2021-03-19 | Array Biopharma, Inc. | Supstituirani spojevi pirazolo[1,5-a]piridina kao inhibitori ret kinaze |
| EP3368039A1 (en) | 2015-10-26 | 2018-09-05 | The Regents of The University of Colorado, A Body Corporate | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| MX2018007266A (es) | 2015-12-18 | 2018-11-09 | Ignyta Inc | Combinaciones para el tratamiento del cancer. |
| WO2017135399A1 (ja) * | 2016-02-04 | 2017-08-10 | 塩野義製薬株式会社 | ＴｒｋＡ阻害活性を有する含窒素複素環および炭素環誘導体 |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| BR112018070017A2 (pt) | 2016-04-04 | 2019-02-05 | Loxo Oncology Inc | métodos de tratamento de cânceres pediátricos |
| PT3439662T (pt) | 2016-04-04 | 2024-09-30 | Loxo Oncology Inc | Formulações líquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida |
| PT3458456T (pt) | 2016-05-18 | 2020-12-07 | Array Biopharma Inc | Preparação de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidino-1-carboxamida |
| 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 |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| CN110267960B (zh) | 2017-01-18 | 2022-04-26 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物 |
| 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 |
| WO2018199166A1 (ja) | 2017-04-27 | 2018-11-01 | 持田製薬株式会社 | 新規テトラヒドロナフチルウレア誘導体 |
| CN107245073B (zh) * | 2017-07-11 | 2020-04-17 | 中国药科大学 | 4-(芳杂环取代)氨基-1h-3-吡唑甲酰胺类flt3抑制剂及其用途 |
| BR112020000793A2 (pt) | 2017-07-19 | 2020-07-14 | Ignyta, Inc. | composições farmacêuticas e formas de dosagem |
| JP2019026646A (ja) * | 2017-08-03 | 2019-02-21 | 塩野義製薬株式会社 | 含窒素複素環および炭素環誘導体を含有する、疼痛の治療および／または予防用医薬組成物 |
| JP6916562B2 (ja) * | 2017-08-11 | 2021-08-11 | テリジーン リミテッドＴｅｌｉｇｅｎｅ Ｌｔｄ． | 化合物、その薬学的に許容される塩、溶媒和物、立体異性体及び互変異性体、並びに薬物組成物、過剰増殖性障害治療剤、過剰増殖性障害予防剤、薬物、癌治療剤、癌予防剤、及びキナーゼシグナル伝達調節剤 |
| JP7134983B2 (ja) | 2017-09-15 | 2022-09-12 | 持田製薬株式会社 | テトラヒドロナフチルウレア誘導体の結晶 |
| TWI876442B (zh) | 2017-10-10 | 2025-03-11 | 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 |
| JP7311498B2 (ja) | 2017-10-17 | 2023-07-19 | イグナイタ インコーポレイテッド | 薬学的組成物および剤形 |
| CA3080157A1 (en) | 2017-10-26 | 2019-05-02 | Array Biopharma Inc. | Formulations of a macrocyclic trk kinase inhibitor |
| CA3087972C (en) | 2018-01-18 | 2023-01-10 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| CN111971286B (zh) | 2018-01-18 | 2023-04-14 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物 |
| CN111630054B (zh) | 2018-01-18 | 2023-05-09 | 奥瑞生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物 |
| TWI804585B (zh) | 2018-03-05 | 2023-06-11 | 美商必治妥美雅史谷比公司 | 苯基吡咯啶酮甲醯肽2受體促效劑 |
| WO2019191659A1 (en) | 2018-03-29 | 2019-10-03 | Loxo Oncology, Inc. | Treatment of trk-associated cancers |
| CN108794484B (zh) * | 2018-04-28 | 2020-04-24 | 北京施安泰医药技术开发有限公司 | [1,2,4]三唑并[4,3-a]吡嗪衍生物、其药物组合物、制备方法和应用 |
| JP7083436B2 (ja) | 2018-07-12 | 2022-06-13 | ▲ザン▼州片仔▲ファン▼薬業股▲フン▼有限公司 | ピロリジニル尿素誘導体とＴｒｋＡ関連疾患への使用 |
| KR102612513B1 (ko) | 2018-07-31 | 2023-12-12 | 록쏘 온콜로지, 인코포레이티드 | (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의 분무-건조된 분산물 및 제제 |
| TWI714231B (zh) * | 2018-09-04 | 2020-12-21 | 美商美國禮來大藥廠 | 2,6-二胺基吡啶化合物 |
| US11964988B2 (en) | 2018-09-10 | 2024-04-23 | Array Biopharma Inc. | Fused heterocyclic compounds as RET kinase inhibitors |
| WO2020083377A1 (zh) * | 2018-10-26 | 2020-04-30 | 南京明德新药研发有限公司 | 吡咯烷基脲衍生物及其应用 |
| JP2022515198A (ja) | 2018-12-19 | 2022-02-17 | アレイ バイオファーマ インコーポレイテッド | ＦＧＦＲチロシンキナーゼの阻害剤としての置換ピラゾロ［１，５－ａ］ピリジン化合物 |
| WO2020131674A1 (en) | 2018-12-19 | 2020-06-25 | Array Biopharma Inc. | 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer |
| MX2021009863A (es) | 2019-03-21 | 2021-11-12 | Onxeo | Una molecula dbait en combinacion con inhibidor de quinasa para el tratamiento del cancer. |
| WO2021089791A1 (en) | 2019-11-08 | 2021-05-14 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| AU2020398180A1 (en) | 2019-12-05 | 2021-09-16 | Illumina, Inc. | Rapid detection of gene fusions |
| WO2021138391A1 (en) | 2019-12-30 | 2021-07-08 | Tyra Biosciences, Inc. | Indazole compounds |
| CN114945565A (zh) | 2020-01-10 | 2022-08-26 | 漳州片仔癀药业股份有限公司 | 一种吡咯烷基脲衍生物的晶型及其应用 |
| EP4089087B1 (en) | 2020-01-10 | 2024-07-03 | Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd. | Method for preparing pyrrolidinyl urea derivative |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| EP4323353A4 (en) * | 2021-04-12 | 2025-04-02 | Cullgen (Shanghai), Inc. | TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHODS OF USE |
Family Cites Families (84)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ299242A (en) | 1995-09-11 | 1997-12-19 | Nihon Nohyaku Co Ltd | N-phenyl-n'-(phenyl substituted imidazol-5-yl, -oxazol-4-yl, and -thiazol-4-yl)urea derivatives |
| CA2206201A1 (en) | 1996-05-29 | 1997-11-29 | Yoshiaki Isobe | Pyrazole derivatives and their pharmaceutical use |
| US6083986A (en) | 1996-07-26 | 2000-07-04 | Icagen, Inc. | Potassium channel inhibitors |
| US5998424A (en) | 1997-06-19 | 1999-12-07 | Dupont Pharmaceuticals Company | Inhibitors of factor Xa with a neutral P1 specificity group |
| JP2001521934A (ja) | 1997-11-03 | 2001-11-13 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | 抗炎症薬としての芳香族ヘテロ環式化合物 |
| US7329670B1 (en) | 1997-12-22 | 2008-02-12 | Bayer Pharmaceuticals Corporation | Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas |
| AU739642B2 (en) | 1997-12-22 | 2001-10-18 | Bayer Healthcare Llc | Inhibition of p38 kinase activity using substituted heterocyclic ureas |
| AU762077B2 (en) | 1997-12-22 | 2003-06-19 | Bayer Healthcare Llc | Inhibition of p38 kinase activity using aryl and heteroaryl substituted heterocyclic ureas |
| US6197798B1 (en) | 1998-07-21 | 2001-03-06 | Novartis Ag | Amino-benzocycloalkane derivatives |
| WO2000039116A1 (en) | 1998-12-25 | 2000-07-06 | Teikoku Hormone Mfg. Co., Ltd. | Aminopyrazole derivatives |
| UA73492C2 (en) | 1999-01-19 | 2005-08-15 | Aromatic heterocyclic compounds as antiinflammatory agents | |
| US6387900B1 (en) | 1999-08-12 | 2002-05-14 | Pharmacia & Upjohn S.P.A. | 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents |
| JP2003512349A (ja) | 1999-10-15 | 2003-04-02 | デュポン ファーマシューティカルズ カンパニー | ケモカイン受容体活性のモジュレーターとしてのベンジルシクロアルキルアミン |
| US6410533B1 (en) | 2000-02-10 | 2002-06-25 | Genzyme Corporation | Antibacterial compounds |
| BR0111878A (pt) | 2000-06-30 | 2005-05-24 | Bristol Myers Squibb Co | N-ureido-(heterociclo-alquil)-piperidinas como moduladores da atividade de receptores de quimiocinas |
| JP2004534017A (ja) | 2001-04-27 | 2004-11-11 | バーテックス ファーマシューティカルズ インコーポレイテッド | Ｂａｃｅのインヒビター |
| GB0110901D0 (en) | 2001-05-02 | 2001-06-27 | Smithkline Beecham Plc | Novel Compounds |
| AU2002363250A1 (en) | 2001-11-01 | 2003-05-12 | Icagen, Inc. | Pyrazole-amides and-sulfonamides |
| WO2003045920A1 (en) | 2001-11-27 | 2003-06-05 | Merck & Co., Inc. | 4-aminoquinoline compounds |
| SE0104248D0 (sv) | 2001-12-14 | 2001-12-14 | Astrazeneca Ab | Method of treatment |
| CN1678608A (zh) | 2002-07-02 | 2005-10-05 | 先灵公司 | 新的神经肽yy5受体拮抗剂 |
| ATE497391T1 (de) | 2002-10-08 | 2011-02-15 | Rinat Neuroscience Corp | Verfahren zur behandlung von postoperativen schmerzen durch verabreichung eines antikörpers gegen nervenwachstumsfaktor und diesen enthaltende zusammensetzungen |
| EP1556389B9 (en) | 2002-10-30 | 2015-09-09 | Astellas Pharma Inc. | Cephem compounds |
| US7144911B2 (en) | 2002-12-31 | 2006-12-05 | Deciphera Pharmaceuticals Llc | Anti-inflammatory medicaments |
| WO2005024755A2 (en) | 2002-12-31 | 2005-03-17 | Deciphera Pharmaceuticals, Llc. | Medicaments for the treatment of neurodegenerative disorders or diabetes |
| US7202257B2 (en) | 2003-12-24 | 2007-04-10 | Deciphera Pharmaceuticals, Llc | Anti-inflammatory medicaments |
| US20040171075A1 (en) | 2002-12-31 | 2004-09-02 | Flynn Daniel L | Modulation of protein functionalities |
| SI1658269T1 (sl) | 2003-06-12 | 2009-04-30 | Abbott Lab | Kondenzirane spojine za inhibicijo vaniloidnega receptorja podvrste (VR1) receptorja |
| EP1684762A4 (en) | 2003-11-13 | 2009-06-17 | Ambit Biosciences Corp | UREA DERIVATIVES AS MODULATORS OF KINASE |
| US20080220497A1 (en) | 2003-12-24 | 2008-09-11 | Flynn Daniel L | Modulation of protein functionalities |
| JP4573223B2 (ja) | 2004-01-23 | 2010-11-04 | 東レ・ファインケミカル株式会社 | 光学活性ｔｒａｎｓ−４−アミノ−１−ベンジル−３−ピロリジノールの製造方法 |
| CN101010315A (zh) * | 2004-04-30 | 2007-08-01 | 拜耳制药公司 | 用于治疗癌症的取代的吡唑基脲衍生物 |
| EP1831228A1 (en) | 2004-12-20 | 2007-09-12 | AstraZeneca AB | Novel pyrazole derivatives and their use as modulators of nicotinic acetylcholine receptors |
| AU2005325676A1 (en) | 2004-12-23 | 2006-08-03 | Deciphera Pharmaceuticals, Llc | Anti-inflammatory medicaments |
| EP2942349A1 (en) | 2004-12-23 | 2015-11-11 | Deciphera Pharmaceuticals, LLC | Enzyme modulators and treatments |
| EP1836188A1 (en) | 2004-12-30 | 2007-09-26 | Astex Therapeutics Limited | Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases |
| WO2010104488A1 (en) | 2009-02-19 | 2010-09-16 | University Of Connecticut | Novel hetero pyrrole analogs acting on cannapinoid receptors |
| GB0510141D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B3 |
| US20060281768A1 (en) | 2005-06-10 | 2006-12-14 | Gaul Michael D | Thienopyrimidine and thienopyridine kinase modulators |
| EP1960394A2 (en) | 2005-11-15 | 2008-08-27 | Bayer HealthCare AG | Pyrazolyl urea derivatives useful in the treatment of cancer |
| US7514435B2 (en) | 2005-11-18 | 2009-04-07 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| US20110195110A1 (en) | 2005-12-01 | 2011-08-11 | Roger Smith | Urea compounds useful in the treatment of cancer |
| ATE434605T1 (de) | 2005-12-01 | 2009-07-15 | Hoffmann La Roche | Inhibitoren des serotonintransporters (sert) |
| GB0607953D0 (en) | 2006-04-21 | 2006-05-31 | Novartis Ag | Organic compounds |
| WO2008016811A2 (en) | 2006-07-31 | 2008-02-07 | Neurogen Corporation | Aminopiperidines and realted compounds |
| GB0615619D0 (en) | 2006-08-05 | 2006-09-13 | Astrazeneca Ab | Chemical process for preparation of intermediates |
| WO2008021859A1 (en) | 2006-08-09 | 2008-02-21 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| US7897762B2 (en) | 2006-09-14 | 2011-03-01 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of proliferative diseases |
| US8188113B2 (en) | 2006-09-14 | 2012-05-29 | Deciphera Pharmaceuticals, Inc. | Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| US7790756B2 (en) | 2006-10-11 | 2010-09-07 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases |
| RU2009142851A (ru) | 2007-04-20 | 2011-05-27 | ДЕСИФЕРА ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи (US) | Ингибиторы киназы, пригодные для лечения миелопролиферативных заболеваний и других пролиферативных заболеваний |
| WO2008150899A1 (en) | 2007-05-29 | 2008-12-11 | Emory University | Combination therapies for treatment of cancer and inflammatory diseases |
| NZ582443A (en) | 2007-07-12 | 2011-04-29 | Novartis Ag | Oral pharmaceutical solutions containing telbivudine |
| ITMI20071731A1 (it) | 2007-09-06 | 2009-03-07 | Univ Degli Studi Genova | Nuovi derivati ureici dell'acido 1h-pirazol-4-carbossilico con attivita inibente nei confronti della chemiotassi di neutrofili |
| AU2009246687B2 (en) | 2008-05-13 | 2012-08-09 | Irm Llc | Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors |
| EP2336105B9 (en) | 2008-09-19 | 2014-09-17 | Takeda Pharmaceutical Company Limited | Nitrogen-containing heterocyclic compound and use of same |
| SI2350075T1 (sl) | 2008-09-22 | 2014-06-30 | Array Biopharma, Inc. | Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji |
| CN102177136A (zh) | 2008-10-09 | 2011-09-07 | 弗·哈夫曼-拉罗切有限公司 | 吡咯烷n-苄基衍生物 |
| BRPI0919873B8 (pt) | 2008-10-22 | 2021-05-25 | Array Biopharma Inc | compostos de pirazol[1,5-a]pirimidina substituídos como inibidores da trk quinase, seus processos de preparação e composições farmacêuticas |
| CN102264706A (zh) | 2008-11-19 | 2011-11-30 | 梅里亚有限公司 | 二聚的1-芳基吡唑衍生物 |
| EP2376495A4 (en) | 2008-12-08 | 2012-10-31 | Vm Pharma Llc | COMPOSITIONS OF PROTEIN RECEPTOR TYROSINE KINASE INHIBITORS |
| RU2505540C2 (ru) | 2008-12-23 | 2014-01-27 | Эббви Инк. | Антивирусные соединения |
| WO2010125799A1 (ja) | 2009-04-27 | 2010-11-04 | 塩野義製薬株式会社 | Pi3k阻害活性を有するウレア誘導体 |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| WO2011032291A1 (en) | 2009-09-18 | 2011-03-24 | Zalicus Pharmaceuticals Ltd . | Selective calcium channel modulators |
| SMT201700372T1 (it) | 2010-05-20 | 2017-09-07 | Array Biopharma Inc | Composti macrociclici come inibitori di trk chinasi |
| RU2606131C2 (ru) * | 2011-05-13 | 2017-01-10 | Эррэй Биофарма Инк. | СОЕДИНЕНИЯ ПИРРОЛИДИНИЛМОЧЕВИНЫ И ПИРРОЛИДИНИЛТИОМОЧЕВИНЫ КАК ИНГИБИТОРЫ КИНАЗЫ TrkA |
| EP2770987B1 (en) | 2011-10-27 | 2018-04-04 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| WO2013096226A1 (en) | 2011-12-19 | 2013-06-27 | Abbvie Inc. | Trpv1 antagonists |
| WO2013176970A1 (en) | 2012-05-22 | 2013-11-28 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
| KR20150060724A (ko) | 2012-09-28 | 2015-06-03 | 머크 샤프 앤드 돔 코포레이션 | Erk 억제제인 신규 화합물 |
| EP2900223B1 (en) | 2012-09-28 | 2017-10-25 | Merck Sharp & Dohme Corp. | Novel compounds that are erk 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 |
| US9809578B2 (en) | 2012-11-13 | 2017-11-07 | Array Biopharma Inc. | Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors |
| WO2014078378A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9822118B2 (en) | 2012-11-13 | 2017-11-21 | Array Biopharma Inc. | Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| SG11201503731SA (en) | 2012-11-13 | 2015-06-29 | Array Biopharma Inc | Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain |
| WO2014078323A1 (en) * | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-pyrrolidinyl, n'-pyrazolyl- 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 |
| 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 |
| WO2014078325A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-(monocyclic aryl),n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9790178B2 (en) | 2012-11-13 | 2017-10-17 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| WO2015039333A1 (en) | 2013-09-22 | 2015-03-26 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
| MA40434B1 (fr) | 2014-05-15 | 2019-09-30 | Array Biopharma Inc | 1-((3s,4r)-4-(3-fluorophényl)-1-(2-méthoxyéthyl)pyrrolidin-3-yl)-3-(4-méthyl-3-(2-méthylpyrimidin-5-yl)-1-phényl-1h-pyrazol-5-yl)urée comme inhibiteur de la kinase trka |
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2015
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- 2015-05-14 CN CN201811493142.0A patent/CN109970614B/zh active Active
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- 2015-05-14 HU HUE15726455A patent/HUE045340T2/hu unknown
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- 2015-05-14 UA UAA201612765A patent/UA122126C2/uk unknown
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- 2015-05-14 NZ NZ727418A patent/NZ727418A/en unknown
- 2015-05-14 MY MYPI2016704187A patent/MY191956A/en unknown
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- 2015-05-14 KR KR1020197019130A patent/KR102321883B1/ko active Active
- 2015-05-14 SM SM20190522T patent/SMT201900522T1/it unknown
- 2015-05-14 RS RSP20191168 patent/RS59286B1/sr unknown
- 2015-05-14 KR KR1020167035164A patent/KR101998461B1/ko active Active
- 2015-05-14 US US15/311,148 patent/US10835533B2/en active Active
- 2015-05-14 JP JP2016567819A patent/JP6499672B2/ja active Active
- 2015-05-14 ES ES15726455T patent/ES2746530T3/es active Active
- 2015-05-14 WO PCT/US2015/030795 patent/WO2015175788A1/en not_active Ceased
- 2015-05-14 PT PT15726455T patent/PT3154959T/pt unknown
- 2015-05-14 SG SG11201609550PA patent/SG11201609550PA/en unknown
- 2015-05-14 DK DK15726455.7T patent/DK3154959T3/da active
- 2015-05-14 CN CN201580032260.XA patent/CN106459013B/zh active Active
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2016
- 2016-11-11 PH PH12016502242A patent/PH12016502242A1/en unknown
- 2016-11-13 IL IL248924A patent/IL248924B/en active IP Right Grant
- 2016-11-14 MX MX2019012600A patent/MX2019012600A/es unknown
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2019
- 2019-02-27 AU AU2019201400A patent/AU2019201400A1/en not_active Abandoned
- 2019-03-15 JP JP2019048124A patent/JP2019085427A/ja active Pending
- 2019-03-19 EP EP19163878.2A patent/EP3564236A1/en not_active Withdrawn
- 2019-09-25 CY CY20191101009T patent/CY1122075T1/el unknown
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2020
- 2020-01-23 PH PH12020500171A patent/PH12020500171A1/en unknown
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