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
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- 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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- 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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- 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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- 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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- 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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- JDIIGWSSTNUWGK-UHFFFAOYSA-N 1h-imidazol-3-ium;chloride Chemical compound [Cl-].[NH2+]1C=CN=C1 JDIIGWSSTNUWGK-UHFFFAOYSA-N 0.000 description 1
- IWWQROMVQSKLDE-UHFFFAOYSA-N 2-methoxy-n-(methoxymethyl)-n-(trimethylsilylmethyl)ethanamine Chemical compound COCCN(COC)C[Si](C)(C)C IWWQROMVQSKLDE-UHFFFAOYSA-N 0.000 description 1
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- 229910052760 oxygen Inorganic materials 0.000 description 1
- 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
- 239000003029 tricyclic antidepressant agent Substances 0.000 description 1
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 (https=) | 2018-10-25 |
| JP6499672B2 JP6499672B2 (ja) | 2019-04-10 |
Family
ID=53276291
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 (https=) |
| EP (2) | EP3154959B1 (https=) |
| JP (2) | JP6499672B2 (https=) |
| KR (2) | KR102321883B1 (https=) |
| CN (2) | CN106459013B (https=) |
| AU (2) | AU2015259075B2 (https=) |
| CA (1) | CA2949160C (https=) |
| CL (1) | CL2016002900A1 (https=) |
| CR (1) | CR20160583A (https=) |
| CY (1) | CY1122075T1 (https=) |
| DK (1) | DK3154959T3 (https=) |
| ES (1) | ES2746530T3 (https=) |
| HR (1) | HRP20191593T1 (https=) |
| HU (1) | HUE045340T2 (https=) |
| IL (1) | IL248924B (https=) |
| LT (1) | LT3154959T (https=) |
| MA (1) | MA40434B1 (https=) |
| MX (2) | MX2016014945A (https=) |
| MY (1) | MY191956A (https=) |
| NZ (1) | NZ727418A (https=) |
| PH (2) | PH12016502242A1 (https=) |
| PL (1) | PL3154959T3 (https=) |
| PT (1) | PT3154959T (https=) |
| RS (1) | RS59286B1 (https=) |
| RU (1) | RU2719489C2 (https=) |
| SG (2) | SG10201903532XA (https=) |
| SI (1) | SI3154959T1 (https=) |
| SM (1) | SMT201900522T1 (https=) |
| UA (1) | UA122126C2 (https=) |
| WO (1) | WO2015175788A1 (https=) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2350075E (pt) | 2008-09-22 | 2014-06-09 | Array Biopharma Inc | Compostos imidazo[1,2b]piridazina substituídos como inibidores da trk cinase |
| AR074052A1 (es) | 2008-10-22 | 2010-12-22 | Array Biopharma Inc | Compuestos pirazolo{1,5-a}pirimidina sustituida como inhibidores de trk 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 |
| NZ604708A (en) | 2010-05-20 | 2015-05-29 | Array Biopharma Inc | Macrocyclic compounds as trk kinase inhibitors |
| NZ720508A (en) | 2013-11-28 | 2019-03-29 | Kyorin Seiyaku Kk | Urea derivative or pharmacologically acceptable salt thereof |
| US10231965B2 (en) | 2014-02-20 | 2019-03-19 | Ignyta, Inc. | Molecules for administration to ROS1 mutant cancer cells |
| CA2949160C (en) | 2014-05-15 | 2023-03-21 | Array Biopharma Inc. | 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 |
| 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 |
| HUE061448T2 (hu) | 2014-11-16 | 2023-07-28 | Array Biopharma Inc | (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-A]pirimidin-3-il) -3-hidroxipirrolidin-1-karboxamid-hidrogénszulfát kristályos formája |
| WO2016196671A1 (en) | 2015-06-01 | 2016-12-08 | Loxo Oncology, Inc. | Methods of diagnosing and treating cancer |
| JP6812059B2 (ja) * | 2015-07-07 | 2021-01-13 | 塩野義製薬株式会社 | ＴｒｋＡ阻害活性を有する複素環誘導体 |
| BR112018000808A2 (pt) | 2015-07-16 | 2018-09-04 | Array Biopharma Inc | compostos de pirazolo[1,5-a]piridina substituída como inibidores de ret cinase |
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- 2015-05-14 MY MYPI2016704187A patent/MY191956A/en unknown
- 2015-05-14 SM SM20190522T patent/SMT201900522T1/it unknown
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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
- 2016-11-15 CL CL2016002900A patent/CL2016002900A1/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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