JP2018500342A5 - - Google Patents
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- JP2018500342A5 JP2018500342A5 JP2017533767A JP2017533767A JP2018500342A5 JP 2018500342 A5 JP2018500342 A5 JP 2018500342A5 JP 2017533767 A JP2017533767 A JP 2017533767A JP 2017533767 A JP2017533767 A JP 2017533767A JP 2018500342 A5 JP2018500342 A5 JP 2018500342A5
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- alkyl
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- pharmaceutically acceptable
- acceptable salt
- compound according
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- 125000000217 alkyl group Chemical group 0.000 claims description 57
- 150000001875 compounds Chemical class 0.000 claims description 44
- 150000003839 salts Chemical class 0.000 claims description 37
- 229910052799 carbon Inorganic materials 0.000 claims description 18
- 229910052736 halogen Inorganic materials 0.000 claims description 18
- 150000002367 halogens Chemical class 0.000 claims description 18
- 229910052739 hydrogen Inorganic materials 0.000 claims description 18
- 229910052760 oxygen Inorganic materials 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 10
- 125000004432 carbon atom Chemical group C* 0.000 claims description 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
- 125000005842 heteroatom Chemical group 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 10
- 239000003814 drug Substances 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 229910052717 sulfur Inorganic materials 0.000 claims description 8
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims description 6
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 5
- 208000035475 disorder Diseases 0.000 claims description 5
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims description 3
- 206010061306 Nasopharyngeal cancer Diseases 0.000 claims description 3
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims description 3
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 2
- 206010003571 Astrocytoma Diseases 0.000 claims description 2
- 206010004593 Bile duct cancer Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 206010014733 Endometrial cancer Diseases 0.000 claims description 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 2
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims description 2
- 208000032612 Glial tumor Diseases 0.000 claims description 2
- 206010018338 Glioma Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010025323 Lymphomas Diseases 0.000 claims description 2
- 206010027406 Mesothelioma Diseases 0.000 claims description 2
- 208000034578 Multiple myelomas Diseases 0.000 claims description 2
- 208000001894 Nasopharyngeal Neoplasms Diseases 0.000 claims description 2
- 206010029260 Neuroblastoma Diseases 0.000 claims description 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010033963 Parathyroid tumour Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 208000015634 Rectal Neoplasms Diseases 0.000 claims description 2
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 2
- 208000008938 Rhabdoid tumor Diseases 0.000 claims description 2
- 101100465401 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) SCL1 gene Proteins 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 229940035676 analgesics Drugs 0.000 claims description 2
- 239000000730 antalgic agent Substances 0.000 claims description 2
- 230000003474 anti-emetic effect Effects 0.000 claims description 2
- 239000000043 antiallergic agent Substances 0.000 claims description 2
- 229940125683 antiemetic agent Drugs 0.000 claims description 2
- 239000002111 antiemetic agent Substances 0.000 claims description 2
- 210000000013 bile duct Anatomy 0.000 claims description 2
- 208000026900 bile duct neoplasm Diseases 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 208000006990 cholangiocarcinoma Diseases 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 230000001120 cytoprotective effect Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 201000004101 esophageal cancer Diseases 0.000 claims description 2
- 201000003444 follicular lymphoma Diseases 0.000 claims description 2
- 201000010175 gallbladder cancer Diseases 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 201000010536 head and neck cancer Diseases 0.000 claims description 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 239000002955 immunomodulating agent Substances 0.000 claims description 2
- 229940121354 immunomodulator Drugs 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 208000007538 neurilemmoma Diseases 0.000 claims description 2
- 229940127084 other anti-cancer agent Drugs 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 206010038038 rectal cancer Diseases 0.000 claims description 2
- 201000001275 rectum cancer Diseases 0.000 claims description 2
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims description 2
- 206010039667 schwannoma Diseases 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 201000002510 thyroid cancer Diseases 0.000 claims description 2
- 208000017997 tumor of parathyroid gland Diseases 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- FVLAYJRLBLHIPV-UHFFFAOYSA-N pyrimidin-5-amine Chemical compound NC1=CN=CN=C1 FVLAYJRLBLHIPV-UHFFFAOYSA-N 0.000 claims 5
- -1 1,3-dimethyl-1H-pyrazol-5-yl Chemical group 0.000 claims 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 208000002454 Nasopharyngeal Carcinoma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- HNYOPLTXPVRDBG-UHFFFAOYSA-N barbituric acid Chemical compound O=C1CC(=O)NC(=O)N1 HNYOPLTXPVRDBG-UHFFFAOYSA-N 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 201000011216 nasopharynx carcinoma Diseases 0.000 claims 1
- 0 N*(CCC1)C1=O Chemical compound N*(CCC1)C1=O 0.000 description 7
- 125000003545 alkoxy group Chemical group 0.000 description 5
- 125000004438 haloalkoxy group Chemical group 0.000 description 3
- 125000001188 haloalkyl group Chemical group 0.000 description 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 3
- 239000000203 mixture Substances 0.000 description 2
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- CLWFDFUVIUSTHL-UHFFFAOYSA-N Cc(cc(nc1)OC)c1-c1cnc(NCc2c(CCO3)c3ccc2F)[n]2c1nnc2 Chemical compound Cc(cc(nc1)OC)c1-c1cnc(NCc2c(CCO3)c3ccc2F)[n]2c1nnc2 CLWFDFUVIUSTHL-UHFFFAOYSA-N 0.000 description 1
- DNXQPHQAMCRLAS-UHFFFAOYSA-N Cc(nc1)c[n]1-c1cnc(NCc2c(CCO3)c3ccc2F)[n]2c1nnc2 Chemical compound Cc(nc1)c[n]1-c1cnc(NCc2c(CCO3)c3ccc2F)[n]2c1nnc2 DNXQPHQAMCRLAS-UHFFFAOYSA-N 0.000 description 1
- ZQROGAWPFDGNBR-UHFFFAOYSA-N Cc1n[n](C)c(-c2cnc(NCc3c(CCO4)c4ccc3F)[n]3c2nnc3)c1 Chemical compound Cc1n[n](C)c(-c2cnc(NCc3c(CCO4)c4ccc3F)[n]3c2nnc3)c1 ZQROGAWPFDGNBR-UHFFFAOYSA-N 0.000 description 1
- XLIBABIFOBYHSV-UHFFFAOYSA-N Cc1ncccc1-c1cnc(NCc2c(CCO3)c3ccc2F)[n]2c1nnc2 Chemical compound Cc1ncccc1-c1cnc(NCc2c(CCO3)c3ccc2F)[n]2c1nnc2 XLIBABIFOBYHSV-UHFFFAOYSA-N 0.000 description 1
- DTZWAJBMXDSNSI-UHFFFAOYSA-N Cc1ncccc1-c1cnc(NCc2c(cc[o]3)c3ccc2F)[n]2c1nnc2 Chemical compound Cc1ncccc1-c1cnc(NCc2c(cc[o]3)c3ccc2F)[n]2c1nnc2 DTZWAJBMXDSNSI-UHFFFAOYSA-N 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2014/094644 | 2014-12-23 | ||
| CN2014094644 | 2014-12-23 | ||
| CN2015095320 | 2015-11-23 | ||
| CNPCT/CN2015/095320 | 2015-11-23 | ||
| PCT/IB2015/059843 WO2016103155A1 (en) | 2014-12-23 | 2015-12-21 | Triazolopyrimidine compounds and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018500342A JP2018500342A (ja) | 2018-01-11 |
| JP2018500342A5 true JP2018500342A5 (cg-RX-API-DMAC7.html) | 2019-02-07 |
| JP6736559B2 JP6736559B2 (ja) | 2020-08-05 |
Family
ID=55071101
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017533767A Active JP6736559B2 (ja) | 2014-12-23 | 2015-12-21 | トリアゾロピリミジン化合物およびその使用 |
Country Status (40)
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA032416B1 (ru) * | 2014-12-23 | 2019-05-31 | Новартис Аг | Соединения триазолопиримидина и их применения |
| US11786533B2 (en) | 2016-06-01 | 2023-10-17 | Epizyme, Inc. | Use of EZH2 inhibitors for treating cancer |
| ES2798424T3 (es) * | 2016-06-20 | 2020-12-11 | Novartis Ag | Compuestos de triazolopiridina y usos de estos |
| EP3472166A1 (en) | 2016-06-20 | 2019-04-24 | Novartis AG | Imidazopyrimidine compounds useful for the treatment of cancer |
| JP7042812B2 (ja) * | 2016-06-20 | 2022-03-28 | ノバルティス アーゲー | トリアゾロピリミジン化合物の結晶形態 |
| TN2019000010A1 (en) | 2016-07-12 | 2020-07-15 | Revolution Medicines Inc | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors |
| CN106831601A (zh) * | 2017-01-13 | 2017-06-13 | 河北博伦特药业有限公司 | 一种2‑氨基甲基嘧啶盐酸盐及其衍生物的合成方法 |
| CA3051054A1 (en) | 2017-01-23 | 2018-07-26 | Revolution Medicines, Inc. | Pyridine compounds as allosteric shp2 inhibitors |
| CA3051206A1 (en) | 2017-01-23 | 2018-07-26 | Revolution Medicines, Inc. | Bicyclic compounds as allosteric shp2 inhibitors |
| US10266542B2 (en) | 2017-03-15 | 2019-04-23 | Mirati Therapeutics, Inc. | EZH2 inhibitors |
| WO2018170290A1 (en) * | 2017-03-15 | 2018-09-20 | Fulcrum Therapeutics, Inc. | Compositions and methods for increasing fmr1 expression |
| KR20190129851A (ko) * | 2017-03-16 | 2019-11-20 | 지앙수 헨그루이 메디슨 컴퍼니 리미티드 | 헤테로아릴[4,3-c]피리미딘-5-아민 유도체, 이의 제조 방법 및 이의 의학적 용도 |
| CN110944628A (zh) | 2017-06-02 | 2020-03-31 | Epizyme股份有限公司 | 使用ezh2抑制剂治疗癌症 |
| WO2019062435A1 (zh) * | 2017-09-28 | 2019-04-04 | 中国科学院上海药物研究所 | 三氮唑并嘧啶、三氮唑并吡啶化合物及其组合物用于治疗prc2介导的疾病 |
| CN109575013A (zh) * | 2017-09-28 | 2019-04-05 | 中国科学院上海药物研究所 | 三氮唑并嘧啶、三氮唑并吡啶化合物及其组合物用于治疗prc2介导的疾病 |
| RU2020115095A (ru) | 2017-10-12 | 2021-11-12 | Революшн Медсинз, Инк. | Пиридиновые, пиразиновые и триазиновые соединения в качестве аллостерических ингибиторов shp2 |
| CN109867645B (zh) * | 2017-12-05 | 2021-09-14 | 中国医学科学院药物研究所 | 一种2,2-二氟-2,3-二氢取代苯并呋喃类化合物的合成方法 |
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| CN109942556A (zh) * | 2017-12-21 | 2019-06-28 | 上海青煜医药科技有限公司 | 嘧啶酮化合物及其应用 |
| EP3743416B1 (en) * | 2018-01-23 | 2023-03-15 | Basf Se | Halogenation of pyridine derivatives |
| HUE059536T2 (hu) * | 2018-01-31 | 2022-11-28 | Mirati Therapeutics Inc | PRC2-inhibitorok |
| CN110156787B (zh) * | 2018-02-13 | 2021-11-02 | 中国科学院上海药物研究所 | 一种三氮唑并嘧啶衍生化合物、包含其的药物组合物及其用途 |
| CN110563722A (zh) * | 2018-06-06 | 2019-12-13 | 上海青煜医药科技有限公司 | 吡啶或哒嗪并环化合物及其应用 |
| CN110734436A (zh) * | 2018-07-19 | 2020-01-31 | 上海青煜医药科技有限公司 | 嘧啶或吡嗪并环化合物及其应用 |
| CN113272303B (zh) * | 2018-11-30 | 2024-09-17 | 上海拓界生物医药科技有限公司 | 嘧啶并五元氮杂环类衍生物、其制备方法及其在医药上的应用 |
| CN111518100A (zh) * | 2019-02-02 | 2020-08-11 | 上海青煜医药科技有限公司 | 环丙烯并苯并呋喃取代的氮杂芳基化合物及其应用 |
| CN114144230B (zh) | 2019-03-15 | 2024-04-23 | 弗尔康医疗公司 | 作为eed和prc2调节剂的大环唑并吡啶衍生物 |
| KR102875195B1 (ko) * | 2019-04-03 | 2025-10-22 | 케미테라스, 인크. | 티민 핵산 염기를 베이스로 하는 트리아졸로피리미딘류 및 그 제조 방법 |
| EP3959214A1 (en) * | 2019-04-22 | 2022-03-02 | Mirati Therapeutics, Inc. | Naphthyridine derivatives as prc2 inhibitors |
| EP3969639B1 (en) | 2019-05-13 | 2025-03-12 | Ecolab Usa Inc. | 1,2,4-triazolo[1,5-a] pyrimidine derivative as copper corrosion inhibitor |
| CN114269748A (zh) * | 2019-06-05 | 2022-04-01 | 米拉蒂医疗股份有限公司 | 作为用于治疗癌症的PRC2抑制剂的咪唑并[1,2-c]嘧啶衍生物 |
| US20220305021A1 (en) * | 2019-06-05 | 2022-09-29 | Athenex, Inc. | Methods of treating and/or preventing psoriasis |
| AU2020315401B2 (en) | 2019-07-16 | 2025-05-22 | The Regents Of The University Of Michigan | Imidazopyrimidines as EED inhibitors and the use thereof |
| CN112409385B (zh) * | 2019-08-22 | 2024-08-13 | 上海青煜医药科技有限公司 | 氮杂芳基化合物及其应用 |
| WO2021057853A1 (en) * | 2019-09-26 | 2021-04-01 | Novartis Ag | Aza-quinoline compounds and uses thereof |
| CN118652256A (zh) * | 2019-11-01 | 2024-09-17 | 上海科技大学 | Eed抑制剂及其制备方法和用途 |
| CN113004233B (zh) * | 2019-12-18 | 2022-12-20 | 南京优氟医药科技有限公司 | 一种用于制备prc2抑制剂的化合物、其制备方法和用途 |
| CN111333655B (zh) * | 2020-04-13 | 2021-07-13 | 武汉工程大学 | 一种三唑并嘧啶类化合物及其制备方法和应用 |
| CN113636993B (zh) * | 2020-05-11 | 2022-08-19 | 苏州亚盛药业有限公司 | (5-氟-2,3-二氢苯并呋喃-4-基)甲胺或其盐的制备方法及其中间体 |
| JP2023527823A (ja) * | 2020-05-28 | 2023-06-30 | ノバルティス アーゲー | ＰＲＣ２媒介性疾患又は障害の治療に使用するためのＮ－（（５－フルオロ－２，３－ジヒドロベンゾフラン－４－イル）メチル）－８－（２－メチルピリジン－３－イル）－［１，２，４］トリアゾロ［４，３－ｃ］ピリミジン－５－アミン又はその薬学的に許容できる塩の投与計画 |
| CN114907385A (zh) | 2021-02-10 | 2022-08-16 | 上海青煜医药科技有限公司 | 氮杂芳基化合物、其制备方法及应用 |
| WO2023016511A1 (zh) * | 2021-08-11 | 2023-02-16 | 上海青煜医药科技有限公司 | 氮杂芳基化合物、其制备方法及应用 |
| CN117384153A (zh) * | 2022-07-12 | 2024-01-12 | 上海赛岚生物科技有限公司 | 一类甲基转移酶抑制剂及其用途 |
| WO2024215699A1 (en) * | 2023-04-11 | 2024-10-17 | Oric Pharmaceuticals, Inc. | Treatment of t-cell lymphoma |
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