JP2017508766A5 - - Google Patents
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- JP2017508766A5 JP2017508766A5 JP2016558339A JP2016558339A JP2017508766A5 JP 2017508766 A5 JP2017508766 A5 JP 2017508766A5 JP 2016558339 A JP2016558339 A JP 2016558339A JP 2016558339 A JP2016558339 A JP 2016558339A JP 2017508766 A5 JP2017508766 A5 JP 2017508766A5
- Authority
- JP
- Japan
- Prior art keywords
- benzamide
- trifluoromethyl
- methyl
- phenylimidazo
- pyrazol
- 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.)
- Pending
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- -1 imidazothiazolyl Chemical group 0.000 claims 51
- 125000000217 alkyl group Chemical group 0.000 claims 27
- 125000000623 heterocyclic group Chemical group 0.000 claims 24
- 229910052739 hydrogen Inorganic materials 0.000 claims 23
- 239000001257 hydrogen Substances 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 18
- 150000002431 hydrogen Chemical group 0.000 claims 15
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 9
- 125000003226 pyrazolyl group Chemical group 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 6
- 125000002971 oxazolyl group Chemical group 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 102000015336 Nerve Growth Factor Human genes 0.000 claims 4
- 108010025020 Nerve Growth Factor Proteins 0.000 claims 4
- 125000002393 azetidinyl group Chemical group 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000004857 imidazopyridinyl group Chemical group N1C(=NC2=C1C=CC=N2)* 0.000 claims 4
- 125000000842 isoxazolyl group Chemical group 0.000 claims 4
- 229940053128 nerve growth factor Drugs 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 125000000335 thiazolyl group Chemical group 0.000 claims 4
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 239000000460 chlorine Substances 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 239000011737 fluorine Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 208000016192 Demyelinating disease Diseases 0.000 claims 2
- 206010012305 Demyelination Diseases 0.000 claims 2
- 206010067601 Dysmyelination Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical group CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
- 101150111783 NTRK1 gene Proteins 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 208000007536 Thrombosis Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 230000006378 damage Effects 0.000 claims 2
- 230000004064 dysfunction Effects 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 208000037803 restenosis Diseases 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000001305 1,2,4-triazol-3-yl group Chemical group [H]N1N=C([*])N=C1[H] 0.000 claims 1
- 125000004066 1-hydroxyethyl group Chemical group [H]OC([H])([*])C([H])([H])[H] 0.000 claims 1
- 125000005330 8 membered heterocyclic group Chemical group 0.000 claims 1
- SFFADAMZFAATCL-UHFFFAOYSA-N C1(=CC=CC=C1)C=1N=C2N(C=CC=C2)C1NC(C1=CC=C(C=C1)OC(F)(F)F)=O Chemical compound C1(=CC=CC=C1)C=1N=C2N(C=CC=C2)C1NC(C1=CC=C(C=C1)OC(F)(F)F)=O SFFADAMZFAATCL-UHFFFAOYSA-N 0.000 claims 1
- RPEZXBNSHYRNCX-UHFFFAOYSA-N CC=1N=C(OC1)C=1C=C(C(=O)NC2=C(N=C3N2C=CC=C3)C3=CC=CC=C3)C=CC1C(F)(F)F Chemical compound CC=1N=C(OC1)C=1C=C(C(=O)NC2=C(N=C3N2C=CC=C3)C3=CC=CC=C3)C=CC1C(F)(F)F RPEZXBNSHYRNCX-UHFFFAOYSA-N 0.000 claims 1
- REVGBOTYDSGISF-UHFFFAOYSA-N CNC(=O)C1=CC=2N(C=C1)C(=C(N2)C2=CC=CC=C2)NC(=O)C2=CC(=C(C=C2)C(F)(F)F)C2=NN(C=C2)C Chemical compound CNC(=O)C1=CC=2N(C=C1)C(=C(N2)C2=CC=CC=C2)NC(=O)C2=CC(=C(C=C2)C(F)(F)F)C2=NN(C=C2)C REVGBOTYDSGISF-UHFFFAOYSA-N 0.000 claims 1
- QPVLLQUDWADQBA-UHFFFAOYSA-N FC1=C(C=C(C(Cl)=C1)C1=NC=CC=N1)C(=O)NC1=C(N=C2C=CC=CN12)C1=CC=CC=C1 Chemical compound FC1=C(C=C(C(Cl)=C1)C1=NC=CC=N1)C(=O)NC1=C(N=C2C=CC=CN12)C1=CC=CC=C1 QPVLLQUDWADQBA-UHFFFAOYSA-N 0.000 claims 1
- HHMKUHNKLXBXGU-UHFFFAOYSA-N FC1=C(C=CC(=C1)C(F)(F)F)C(=O)NC1=C(N=C2C=CC=CN12)C1=CC=CC=C1 Chemical compound FC1=C(C=CC(=C1)C(F)(F)F)C(=O)NC1=C(N=C2C=CC=CN12)C1=CC=CC=C1 HHMKUHNKLXBXGU-UHFFFAOYSA-N 0.000 claims 1
- UFCQAORTJKBJIM-UHFFFAOYSA-N FC1=C(C=CC(=C1)C(F)(F)F)C(=O)NC1=C(N=C2SC=CN12)C1=CC=CC=C1 Chemical compound FC1=C(C=CC(=C1)C(F)(F)F)C(=O)NC1=C(N=C2SC=CN12)C1=CC=CC=C1 UFCQAORTJKBJIM-UHFFFAOYSA-N 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- 230000001594 aberrant effect Effects 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 229910017464 nitrogen compound Inorganic materials 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2014/074143 | 2014-03-26 | ||
| PCT/CN2014/074143 WO2015143652A1 (en) | 2014-03-26 | 2014-03-26 | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| PCT/US2015/022004 WO2015148373A2 (en) | 2014-03-26 | 2015-03-23 | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017508766A JP2017508766A (ja) | 2017-03-30 |
| JP2017508766A5 true JP2017508766A5 (enExample) | 2018-05-10 |
Family
ID=54193893
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016558347A Pending JP2017512786A (ja) | 2014-03-26 | 2015-03-23 | ＴｒｋＡキナーゼ阻害薬、その組成物および方法 |
| JP2016558339A Pending JP2017508766A (ja) | 2014-03-26 | 2015-03-23 | ＴｒｋＡキナーゼ阻害薬、その組成物および方法 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016558347A Pending JP2017512786A (ja) | 2014-03-26 | 2015-03-23 | ＴｒｋＡキナーゼ阻害薬、その組成物および方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US9862716B2 (enExample) |
| EP (2) | EP3122345B1 (enExample) |
| JP (2) | JP2017512786A (enExample) |
| KR (2) | KR20160131119A (enExample) |
| CN (2) | CN106456581A (enExample) |
| AU (2) | AU2015236363A1 (enExample) |
| CA (2) | CA2942957A1 (enExample) |
| MX (2) | MX2016012481A (enExample) |
| RU (2) | RU2016141647A (enExample) |
| WO (3) | WO2015143652A1 (enExample) |
Families Citing this family (20)
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| CN105418615B (zh) * | 2015-12-09 | 2018-02-02 | 北京工业大学 | 苯甲酰胺衍生物及制备和应用 |
| US11701345B2 (en) | 2017-06-19 | 2023-07-18 | University Of Maryland, Baltimore | Car activator agents for cyclophosphamide-based treatments of cancer |
| CA3075813A1 (en) | 2017-10-04 | 2019-04-11 | Dana-Farber Cancer Institute, Inc. | Small molecule inhibition of transcription factor sall4 and uses thereof |
| KR20190043437A (ko) | 2017-10-18 | 2019-04-26 | 씨제이헬스케어 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
| SG11202005237SA (en) * | 2017-12-15 | 2020-07-29 | Pyramid Biosciences Inc | 5-(2-(2,5-difluorophenyl)pyrrolidin-1 -yl)-3-(1h-pyrazol-1-yl)pyrazolo[1,5-a]pyrimidine derivatives and related compounds as trk kinase inhibitors for treating cancer |
| FI3904350T3 (fi) | 2018-04-12 | 2023-11-15 | Bayer Ag | N-(syklopropyylimetyyli)-5-(metyylisulfonyyli)-n-{1-[1-(pyrimidin-2-yyli)-1h-1,2,4-triatsol-5-yyli]etyyli}bentsamidijohdannaisia ja vastaavia pyridiinikarboksamidijohdannaisia tuholaistorjunta-aineina |
| KR102129114B1 (ko) * | 2018-07-26 | 2020-07-02 | 주식회사 온코파마텍 | TrkA 저해 활성을 갖는 화합물 및 이를 유효성분으로 함유하는 통증의 예방 또는 치료용 약학적 조성물 |
| JP7472103B2 (ja) * | 2018-08-22 | 2024-04-22 | クルゲン（シャンハイ），インク． | トロポミオシン受容体キナーゼ（ｔｒｋ）分解化合物とその使用方法 |
| US11969472B2 (en) | 2018-08-22 | 2024-04-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| KR102195348B1 (ko) | 2018-11-15 | 2020-12-24 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물 |
| CN111269233A (zh) * | 2018-12-05 | 2020-06-12 | 上海轶诺药业有限公司 | 一类咪唑并芳环类化合物的制备和应用 |
| EA202192575A1 (ru) | 2019-03-21 | 2022-01-14 | Онксео | Соединения dbait в сочетании с ингибиторами киназ для лечения рака |
| UY38911A (es) | 2019-10-09 | 2021-05-31 | Bayer Ag | Compuestos de heteroarilo-triazol como pesticidas, formulaciones, usos y métodos de uso de los mismos |
| CN114761006A (zh) | 2019-11-08 | 2022-07-15 | Inserm(法国国家健康医学研究院) | 对激酶抑制剂产生耐药性的癌症的治疗方法 |
| TW202134226A (zh) | 2019-11-18 | 2021-09-16 | 德商拜耳廠股份有限公司 | 作為殺蟲劑之新穎雜芳基-三唑化合物 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| EP4110772A4 (en) | 2020-02-26 | 2024-04-03 | Cullgen (Shanghai), Inc. | TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHODS OF USE |
| CN115916771B (zh) * | 2020-04-02 | 2025-04-01 | 浙江华海药业股份有限公司 | 多靶点的抗肿瘤化合物及其制备方法和应用 |
| TW202210467A (zh) | 2020-05-28 | 2022-03-16 | 美商美國禮來大藥廠 | TrkA抑制劑 |
| CN113666862B (zh) * | 2021-08-18 | 2024-05-31 | 山东大学 | 一种通过镍催化不对称硝化反应制备手性3-硝基吲哚类化合物的方法 |
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| US9079859B2 (en) | 2011-01-21 | 2015-07-14 | Auckland Uniservices Limited | Synthetic lethal targeting of glucose transport |
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| CN102796103A (zh) | 2011-05-23 | 2012-11-28 | 南京英派药业有限公司 | 6-（芳基甲酰）咪唑并[1,2-a]嘧啶和6-（芳基甲酰）[1,2,4]三唑并[4,3-a]嘧啶作为Hedgehog抑制剂及其应用 |
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| TWI652014B (zh) * | 2013-09-13 | 2019-03-01 | 美商艾佛艾姆希公司 | 雜環取代之雙環唑殺蟲劑 |
-
2014
- 2014-03-26 WO PCT/CN2014/074143 patent/WO2015143652A1/en not_active Ceased
-
2015
- 2015-03-23 RU RU2016141647A patent/RU2016141647A/ru not_active Application Discontinuation
- 2015-03-23 US US15/129,206 patent/US9862716B2/en active Active
- 2015-03-23 JP JP2016558347A patent/JP2017512786A/ja active Pending
- 2015-03-23 WO PCT/US2015/022004 patent/WO2015148373A2/en not_active Ceased
- 2015-03-23 JP JP2016558339A patent/JP2017508766A/ja active Pending
- 2015-03-23 RU RU2016141645A patent/RU2016141645A/ru not_active Application Discontinuation
- 2015-03-23 MX MX2016012481A patent/MX2016012481A/es unknown
- 2015-03-23 CA CA2942957A patent/CA2942957A1/en not_active Abandoned
- 2015-03-23 CN CN201580027483.7A patent/CN106456581A/zh active Pending
- 2015-03-23 AU AU2015236363A patent/AU2015236363A1/en not_active Abandoned
- 2015-03-23 KR KR1020167029497A patent/KR20160131119A/ko not_active Withdrawn
- 2015-03-23 CA CA2942817A patent/CA2942817A1/en not_active Abandoned
- 2015-03-23 WO PCT/US2015/021952 patent/WO2015148354A2/en not_active Ceased
- 2015-03-23 CN CN201580027484.1A patent/CN106456582A/zh active Pending
- 2015-03-23 EP EP15769224.5A patent/EP3122345B1/en active Active
- 2015-03-23 EP EP15769051.2A patent/EP3122344B1/en active Active
- 2015-03-23 MX MX2016012483A patent/MX2016012483A/es unknown
- 2015-03-23 US US15/128,793 patent/US9862707B2/en active Active
- 2015-03-23 AU AU2015236438A patent/AU2015236438A1/en not_active Abandoned
- 2015-03-23 KR KR1020167029495A patent/KR20160132114A/ko not_active Withdrawn
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