JPWO2018077246A5 - - Google Patents
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- Publication number
- JPWO2018077246A5 JPWO2018077246A5 JP2019522962A JP2019522962A JPWO2018077246A5 JP WO2018077246 A5 JPWO2018077246 A5 JP WO2018077246A5 JP 2019522962 A JP2019522962 A JP 2019522962A JP 2019522962 A JP2019522962 A JP 2019522962A JP WO2018077246 A5 JPWO2018077246 A5 JP WO2018077246A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- hydroxy
- phenyl
- alkyl
- independently selected
- 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.)
- Granted
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- -1 nitro, hydroxy Chemical group 0.000 claims description 162
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 57
- 125000000217 alkyl group Chemical group 0.000 claims description 47
- 125000001424 substituent group Chemical group 0.000 claims description 45
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 40
- 229910052739 hydrogen Inorganic materials 0.000 claims description 40
- 239000001257 hydrogen Substances 0.000 claims description 40
- 229910052736 halogen Inorganic materials 0.000 claims description 31
- 150000002367 halogens Chemical group 0.000 claims description 30
- 125000001153 fluoro group Chemical group F* 0.000 claims description 26
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 25
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 24
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 21
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 20
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims description 20
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 19
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 19
- 125000003545 alkoxy group Chemical group 0.000 claims description 17
- 125000002971 oxazolyl group Chemical group 0.000 claims description 16
- 125000000335 thiazolyl group Chemical group 0.000 claims description 16
- SBUKLPSBNFWJCU-UHFFFAOYSA-N ClIBr Chemical compound ClIBr SBUKLPSBNFWJCU-UHFFFAOYSA-N 0.000 claims description 15
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 14
- 125000004076 pyridyl group Chemical group 0.000 claims description 13
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 12
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 12
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 12
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 12
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 10
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 8
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims description 7
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 7
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 6
- 125000004852 dihydrofuranyl group Chemical group O1C(CC=C1)* 0.000 claims description 6
- 125000004193 piperazinyl group Chemical group 0.000 claims description 6
- 125000003386 piperidinyl group Chemical group 0.000 claims description 6
- 125000005494 pyridonyl group Chemical group 0.000 claims description 6
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 6
- 125000003507 tetrahydrothiofenyl group Chemical group 0.000 claims description 6
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 5
- 125000002757 morpholinyl group Chemical group 0.000 claims description 5
- 125000003072 pyrazolidinyl group Chemical group 0.000 claims description 5
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 4
- 125000002541 furyl group Chemical group 0.000 claims description 4
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 4
- 125000001544 thienyl group Chemical group 0.000 claims description 4
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims description 4
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims description 3
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims description 3
- 125000004571 thiomorpholin-4-yl group Chemical group N1(CCSCC1)* 0.000 claims description 3
- 125000001246 bromo group Chemical group Br* 0.000 claims description 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 claims 40
- 150000002431 hydrogen Chemical class 0.000 claims 28
- 125000003118 aryl group Chemical group 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 4
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 1
- 102000004278 Receptor Protein-Tyrosine Kinases Human genes 0.000 claims 1
- 108090000873 Receptor Protein-Tyrosine Kinases Proteins 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- YPJKMVATUPSWOH-UHFFFAOYSA-N nitrooxidanyl Chemical group [O][N+]([O-])=O YPJKMVATUPSWOH-UHFFFAOYSA-N 0.000 claims 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 125000003944 tolyl group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 10
- 125000000590 4-methylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 description 2
- 125000005843 halogen group Chemical group 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610970314 | 2016-10-28 | ||
| CN201610970314.3 | 2016-10-28 | ||
| CN201710044000 | 2017-01-21 | ||
| CN201710044000.5 | 2017-01-21 | ||
| PCT/CN2017/108100 WO2018077246A1 (zh) | 2016-10-28 | 2017-10-27 | 用作神经营养因子酪氨酸激酶受体抑制剂的氨基吡唑并嘧啶化合物 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2019537588A JP2019537588A (ja) | 2019-12-26 |
| JP2019537588A5 JP2019537588A5 (https=) | 2022-01-21 |
| JPWO2018077246A5 true JPWO2018077246A5 (https=) | 2022-01-21 |
| JP7046940B2 JP7046940B2 (ja) | 2022-04-04 |
Family
ID=62024344
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019522962A Active JP7046940B2 (ja) | 2016-10-28 | 2017-10-27 | 神経栄養因子チロシンキナーゼ受容体阻害剤として用いられるアミノピラゾロピリミジン化合物 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10829492B2 (https=) |
| EP (1) | EP3533796B1 (https=) |
| JP (1) | JP7046940B2 (https=) |
| KR (1) | KR102616249B1 (https=) |
| CN (1) | CN109890820B (https=) |
| AU (1) | AU2017348826B2 (https=) |
| CA (1) | CA3041942C (https=) |
| DK (1) | DK3533796T3 (https=) |
| ES (1) | ES2896943T3 (https=) |
| HU (1) | HUE057733T2 (https=) |
| MX (1) | MX380283B (https=) |
| PL (1) | PL3533796T3 (https=) |
| PT (1) | PT3533796T (https=) |
| RU (1) | RU2764523C2 (https=) |
| WO (1) | WO2018077246A1 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11286264B2 (en) * | 2017-07-28 | 2022-03-29 | Turning Point Therapeutics, Inc. | Macrocyclic compounds and uses thereof |
| DK3674307T3 (da) | 2017-08-23 | 2023-09-11 | Chia Tai Tianqing Pharmaceutical Group Co Ltd | Makrocyklus indeholdende aminopyrazol og pyrimidin og farmaceutisk sammensætning og anvendelse deraf |
| CN108794370A (zh) * | 2018-07-31 | 2018-11-13 | 上海弈柯莱生物医药科技有限公司 | 一种拉罗替尼中间体的制备方法 |
| CA3122136A1 (en) * | 2018-12-07 | 2021-06-11 | Betta Pharmaceuticals Co., Ltd | Tyrosine kinase inhibitors, compositions and methods there of |
| JP7209415B2 (ja) | 2019-03-19 | 2023-01-20 | セントラル チャイナ ノーマル ユニバーシティ | ピラゾロピリミジン化合物、医薬組成物、及びその使用 |
| CN112979654B (zh) * | 2019-12-16 | 2024-03-19 | 赛诺哈勃药业（成都）有限公司 | 杂芳基稠环化合物、其制备方法及应用 |
| TW202214635A (zh) * | 2020-06-11 | 2022-04-16 | 大陸商貝達藥業股份有限公司 | 酪氨酸激酶抑制劑的鹽型、晶型、藥物組合物及其用途 |
| CN111620881B (zh) * | 2020-07-08 | 2023-03-31 | 浙江合聚生物医药有限公司 | 拉罗替尼衍生物及其制备方法和应用 |
| CN113563343B (zh) * | 2020-07-27 | 2022-05-24 | 杭州邦顺制药有限公司 | 取代的吡唑并[1,5-a]嘧啶化合物及其用途 |
| CN112010860B (zh) * | 2020-08-05 | 2023-03-10 | 南京纳丁菲医药科技有限公司 | 苄氧基吡唑并嘧啶化合物和药物组合物及其应用 |
| CN114437075B (zh) * | 2020-11-03 | 2026-01-30 | 上海瑶琪生物科技有限公司 | 用作ntrk激酶抑制剂的化合物及其应用 |
| CN113200963A (zh) * | 2021-03-31 | 2021-08-03 | 广东石油化工学院 | N-(吡咯基)-3-吡唑基胺及其制备方法 |
| JP7840066B2 (ja) * | 2021-05-03 | 2026-04-03 | ジェービーケーラボ カンパニー リミテッド | ２，６－ジクロロ－４－（４－（４－ヒドロキシシクロヘキシルアミノ）－７ｈ－ピロロ［２，３－ｄ］ピリミジン－５－イル）フェノールを活性成分として含有する、がんを予防、緩和、または処置するための医薬組成物 |
| CN117751121A (zh) * | 2021-07-30 | 2024-03-22 | 正大天晴药业集团股份有限公司 | 氨基吡唑并嘧啶化合物的晶体 |
| WO2023011616A1 (zh) * | 2021-08-06 | 2023-02-09 | 正大天晴药业集团股份有限公司 | 氨基吡唑并嘧啶化合物在治疗trk激酶介导的肿瘤中的用途 |
| CN117088800B (zh) * | 2023-08-18 | 2024-05-28 | 龙曦宁（上海）医药科技有限公司 | 一种5-甲基吡咯烷-3-醇盐酸盐的制备方法 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10356579A1 (de) | 2003-12-04 | 2005-07-07 | Merck Patent Gmbh | Aminderivate |
| WO2009140128A2 (en) | 2008-05-13 | 2009-11-19 | Irm Llc | Compounds and compositions as kinase inhibitors |
| RU2509078C2 (ru) | 2008-07-01 | 2014-03-10 | Дженентек, Инк. | Бициклические гетероциклы в качестве ингибиторов киназы мек |
| 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 |
| WO2012034095A1 (en) * | 2010-09-09 | 2012-03-15 | Irm Llc | Compounds and compositions as trk inhibitors |
| WO2012116217A1 (en) | 2011-02-25 | 2012-08-30 | Irm Llc | Compounds and compositions as trk inhibitors |
| WO2013028263A1 (en) | 2011-08-24 | 2013-02-28 | Glaxosmithkline Llc | Pyrazolopyrimidine derivatives as pi3 kinase inhibitors |
| KR20140105508A (ko) * | 2011-12-12 | 2014-09-01 | 닥터 레디스 레보러터리즈 리미티드 | 트로포미오신 수용체 키나제(Trk) 억제제인 치환된 피라졸로[1,5-a]피리딘 |
| MX362181B (es) | 2013-02-19 | 2019-01-08 | Ono Pharmaceutical Co | Compuesto inhibidor de cinasa del receptor de tropomiosina (trk). |
| WO2014143242A1 (en) | 2013-03-15 | 2014-09-18 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| CN104650092B (zh) * | 2013-11-16 | 2017-11-10 | 广东东阳光药业有限公司 | 取代的杂芳基化合物及其组合物和用途 |
| DK3077397T3 (da) * | 2013-12-06 | 2019-12-16 | Vertex Pharma | 2-amino-6-fluor-n-[5-fluor-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamidforbindelse anvendelig som atr-kinase-inhibitor, dens fremstilling, forskellige faste former og radiomarkerede derivater deraf |
| CA2971024C (en) | 2014-12-15 | 2023-09-26 | Handok Inc. | Fused ring heteroaryl compounds and their use as trk inhibitors |
-
2017
- 2017-10-27 AU AU2017348826A patent/AU2017348826B2/en active Active
- 2017-10-27 KR KR1020197015241A patent/KR102616249B1/ko active Active
- 2017-10-27 WO PCT/CN2017/108100 patent/WO2018077246A1/zh not_active Ceased
- 2017-10-27 PT PT178634101T patent/PT3533796T/pt unknown
- 2017-10-27 HU HUE17863410A patent/HUE057733T2/hu unknown
- 2017-10-27 JP JP2019522962A patent/JP7046940B2/ja active Active
- 2017-10-27 MX MX2019004847A patent/MX380283B/es unknown
- 2017-10-27 PL PL17863410T patent/PL3533796T3/pl unknown
- 2017-10-27 ES ES17863410T patent/ES2896943T3/es active Active
- 2017-10-27 US US16/345,679 patent/US10829492B2/en active Active
- 2017-10-27 DK DK17863410.1T patent/DK3533796T3/da active
- 2017-10-27 RU RU2019114600A patent/RU2764523C2/ru active
- 2017-10-27 CA CA3041942A patent/CA3041942C/en active Active
- 2017-10-27 CN CN201780064022.6A patent/CN109890820B/zh active Active
- 2017-10-27 EP EP17863410.1A patent/EP3533796B1/en active Active
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