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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- 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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- 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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- 208000005298 acute pain Diseases 0.000 claims description 2
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- 239000003085 diluting agent Substances 0.000 claims description 2
- 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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- UJLAWZDWDVHWOW-YPMHNXCESA-N tofacitinib Chemical compound C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)C1=NC=NC2=C1C=CN2 UJLAWZDWDVHWOW-YPMHNXCESA-N 0.000 claims description 2
- UCPYLLCMEDAXFR-UHFFFAOYSA-N triphosgene Chemical compound ClC(Cl)(Cl)OC(=O)OC(Cl)(Cl)Cl UCPYLLCMEDAXFR-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
- NTOIKDYVJIWVSU-WOJBJXKFSA-N (2r,3r)-2,3-dihydroxy-2,3-bis(4-methylbenzoyl)butanedioic acid Chemical compound C1=CC(C)=CC=C1C(=O)[C@@](O)(C(O)=O)[C@](O)(C(O)=O)C(=O)C1=CC=C(C)C=C1 NTOIKDYVJIWVSU-WOJBJXKFSA-N 0.000 description 5
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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
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 description 1
- 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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- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 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
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 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 (OSRAM) | 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 (OSRAM) |
| EP (2) | EP3154959B1 (OSRAM) |
| JP (2) | JP6499672B2 (OSRAM) |
| KR (2) | KR102321883B1 (OSRAM) |
| CN (2) | CN109970614B (OSRAM) |
| AU (2) | AU2015259075B2 (OSRAM) |
| CA (1) | CA2949160C (OSRAM) |
| CL (1) | CL2016002900A1 (OSRAM) |
| CR (1) | CR20160583A (OSRAM) |
| CY (1) | CY1122075T1 (OSRAM) |
| DK (1) | DK3154959T3 (OSRAM) |
| ES (1) | ES2746530T3 (OSRAM) |
| HR (1) | HRP20191593T1 (OSRAM) |
| HU (1) | HUE045340T2 (OSRAM) |
| IL (1) | IL248924B (OSRAM) |
| LT (1) | LT3154959T (OSRAM) |
| MA (1) | MA40434B1 (OSRAM) |
| MX (2) | MX2016014945A (OSRAM) |
| MY (1) | MY191956A (OSRAM) |
| NZ (1) | NZ727418A (OSRAM) |
| PH (2) | PH12016502242B1 (OSRAM) |
| PL (1) | PL3154959T3 (OSRAM) |
| PT (1) | PT3154959T (OSRAM) |
| RS (1) | RS59286B1 (OSRAM) |
| RU (1) | RU2719489C2 (OSRAM) |
| SG (2) | SG11201609550PA (OSRAM) |
| SI (1) | SI3154959T1 (OSRAM) |
| SM (1) | SMT201900522T1 (OSRAM) |
| UA (1) | UA122126C2 (OSRAM) |
| WO (1) | WO2015175788A1 (OSRAM) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8450322B2 (en) | 2008-09-22 | 2013-05-28 | Array Biopharma Inc. | Substituted imidazo[1,2b]pyridazine compounds as Trk kinase inhibitors |
| TR201807039T4 (tr) | 2008-10-22 | 2018-06-21 | Array Biopharma Inc | Trk kinaz inhibitörleri olarak sübstitüe edilmiş pirazolo[1,5-]pirimidin bileşikleri. |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| ES2628418T3 (es) | 2010-05-20 | 2017-08-02 | Array Biopharma, Inc. | Compuestos macrocíclicos como inhibidores de la TRK cinasa |
| NZ752095A (en) | 2013-11-28 | 2022-07-01 | Kyorin Seiyaku Kk | Urea derivative or pharmacologically acceptable salt thereof |
| TWI672141B (zh) | 2014-02-20 | 2019-09-21 | 美商醫科泰生技 | 投予ｒｏｓ１突變癌細胞之分子 |
| EP3154959B1 (en) | 2014-05-15 | 2019-07-10 | 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 |
| PT3699181T (pt) | 2014-11-16 | 2023-04-05 | Array Biopharma Inc | Forma cristalina de hidrogenossulfato de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida |
| TN2017000502A1 (en) | 2015-06-01 | 2019-04-12 | Loxo Oncology Inc | Methods of diagnosing and treating cancer |
| EP3330256B1 (en) | 2015-07-07 | 2021-06-16 | Shionogi & Co., Ltd. | HETEROCYCLIC DERIVATIVE HAVING TrkA-INHIBITING ACTIVITY |
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- 2015-05-14 AU AU2015259075A patent/AU2015259075B2/en active Active
- 2015-05-14 KR KR1020167035164A patent/KR101998461B1/ko active Active
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- 2015-05-14 JP JP2016567819A patent/JP6499672B2/ja active Active
- 2015-05-14 NZ NZ727418A patent/NZ727418A/en unknown
- 2015-05-14 RU RU2016149233A patent/RU2719489C2/ru active
- 2015-05-14 SI SI201530875T patent/SI3154959T1/sl unknown
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2016
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2019
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2020
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