JP2019522051A5 - - Google Patents
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- JP2019522051A5 JP2019522051A5 JP2019518348A JP2019518348A JP2019522051A5 JP 2019522051 A5 JP2019522051 A5 JP 2019522051A5 JP 2019518348 A JP2019518348 A JP 2019518348A JP 2019518348 A JP2019518348 A JP 2019518348A JP 2019522051 A5 JP2019522051 A5 JP 2019522051A5
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- 239000000725 suspension Substances 0.000 claims description 36
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 33
- 239000003960 organic solvent Substances 0.000 claims description 32
- 150000001875 compounds Chemical class 0.000 claims description 31
- 239000000203 mixture Substances 0.000 claims description 19
- 238000010438 heat treatment Methods 0.000 claims description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 18
- 238000000034 method Methods 0.000 claims description 16
- 229940126062 Compound A Drugs 0.000 claims description 13
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims description 13
- FVLAYJRLBLHIPV-UHFFFAOYSA-N pyrimidin-5-amine Chemical compound NC1=CN=CN=C1 FVLAYJRLBLHIPV-UHFFFAOYSA-N 0.000 claims description 13
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 12
- 239000007787 solid Substances 0.000 claims description 10
- 239000013078 crystal Substances 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 6
- 150000004682 monohydrates Chemical group 0.000 claims description 4
- QDUXGHQYLMWYEL-UHFFFAOYSA-N pyrimidin-5-amine;hydrochloride Chemical compound Cl.NC1=CN=CN=C1 QDUXGHQYLMWYEL-UHFFFAOYSA-N 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- IEBCOOFGQUXLPQ-UHFFFAOYSA-N Cl.N=1N=CN2C(=NC=CC21)N Chemical compound Cl.N=1N=CN2C(=NC=CC21)N IEBCOOFGQUXLPQ-UHFFFAOYSA-N 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
- 239000002111 antiemetic agent Substances 0.000 claims description 2
- 229940125683 antiemetic agent Drugs 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 230000001120 cytoprotective effect Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000002955 immunomodulating agent Substances 0.000 claims description 2
- 229940121354 immunomodulator Drugs 0.000 claims description 2
- 229940127084 other anti-cancer agent Drugs 0.000 claims description 2
- -1 5-fluoro-2,3-dihydrobenzofuran-4-yl Chemical group 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 201000010099 disease Diseases 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 206010003571 Astrocytoma Diseases 0.000 description 1
- 206010004593 Bile duct cancer Diseases 0.000 description 1
- 206010005003 Bladder cancer Diseases 0.000 description 1
- 208000003174 Brain Neoplasms Diseases 0.000 description 1
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- 206010008342 Cervix carcinoma Diseases 0.000 description 1
- YHAMPXCHEHVBSA-UHFFFAOYSA-N Cl.Cc1ncccc1-c1cnc(NCc2c3CCOc3ccc2F)n2cnnc12 Chemical compound Cl.Cc1ncccc1-c1cnc(NCc2c3CCOc3ccc2F)n2cnnc12 YHAMPXCHEHVBSA-UHFFFAOYSA-N 0.000 description 1
- 206010009944 Colon cancer Diseases 0.000 description 1
- 206010014733 Endometrial cancer Diseases 0.000 description 1
- 206010014759 Endometrial neoplasm Diseases 0.000 description 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 description 1
- 208000022072 Gallbladder Neoplasms Diseases 0.000 description 1
- 208000032612 Glial tumor Diseases 0.000 description 1
- 206010018338 Glioma Diseases 0.000 description 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 description 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 1
- 206010025323 Lymphomas Diseases 0.000 description 1
- 206010027406 Mesothelioma Diseases 0.000 description 1
- 208000034578 Multiple myelomas Diseases 0.000 description 1
- 208000001894 Nasopharyngeal Neoplasms Diseases 0.000 description 1
- 206010061306 Nasopharyngeal cancer Diseases 0.000 description 1
- 206010029260 Neuroblastoma Diseases 0.000 description 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 description 1
- 206010033128 Ovarian cancer Diseases 0.000 description 1
- 206010061535 Ovarian neoplasm Diseases 0.000 description 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 description 1
- 206010033963 Parathyroid tumour Diseases 0.000 description 1
- 206010035226 Plasma cell myeloma Diseases 0.000 description 1
- 206010060862 Prostate cancer Diseases 0.000 description 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 1
- 208000015634 Rectal Neoplasms Diseases 0.000 description 1
- 208000006265 Renal cell carcinoma Diseases 0.000 description 1
- 208000008938 Rhabdoid tumor Diseases 0.000 description 1
- 101100465401 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) SCL1 gene Proteins 0.000 description 1
- 206010039491 Sarcoma Diseases 0.000 description 1
- 208000021712 Soft tissue sarcoma Diseases 0.000 description 1
- 208000005718 Stomach Neoplasms Diseases 0.000 description 1
- 208000024770 Thyroid neoplasm Diseases 0.000 description 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 description 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 description 1
- 210000000013 bile duct Anatomy 0.000 description 1
- 208000026900 bile duct neoplasm Diseases 0.000 description 1
- 201000010881 cervical cancer Diseases 0.000 description 1
- 208000006990 cholangiocarcinoma Diseases 0.000 description 1
- 208000029742 colonic neoplasm Diseases 0.000 description 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 201000004101 esophageal cancer Diseases 0.000 description 1
- 201000003444 follicular lymphoma Diseases 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 201000010175 gallbladder cancer Diseases 0.000 description 1
- 206010017758 gastric cancer Diseases 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 208000005017 glioblastoma Diseases 0.000 description 1
- 201000010536 head and neck cancer Diseases 0.000 description 1
- 208000014829 head and neck neoplasm Diseases 0.000 description 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 description 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 description 1
- 208000032839 leukemia Diseases 0.000 description 1
- 201000005202 lung cancer Diseases 0.000 description 1
- 208000020816 lung neoplasm Diseases 0.000 description 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 201000001441 melanoma Diseases 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 208000007538 neurilemmoma Diseases 0.000 description 1
- 201000002528 pancreatic cancer Diseases 0.000 description 1
- 208000008443 pancreatic carcinoma Diseases 0.000 description 1
- 206010038038 rectal cancer Diseases 0.000 description 1
- 201000001275 rectum cancer Diseases 0.000 description 1
- 208000015347 renal cell adenocarcinoma Diseases 0.000 description 1
- 206010039667 schwannoma Diseases 0.000 description 1
- 201000011549 stomach cancer Diseases 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 201000002510 thyroid cancer Diseases 0.000 description 1
- 208000017997 tumor of parathyroid gland Diseases 0.000 description 1
- 208000025421 tumor of uterus Diseases 0.000 description 1
- 201000005112 urinary bladder cancer Diseases 0.000 description 1
- 206010046766 uterine cancer Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2016086350 | 2016-06-20 | ||
| CNPCT/CN2016/086350 | 2016-06-20 | ||
| PCT/CN2017/089003 WO2017219948A1 (en) | 2016-06-20 | 2017-06-19 | Crystalline forms of triazolopyrimidine compound |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019522051A JP2019522051A (ja) | 2019-08-08 |
| JP2019522051A5 true JP2019522051A5 (enExample) | 2020-07-27 |
| JP7042812B2 JP7042812B2 (ja) | 2022-03-28 |
Family
ID=60783815
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019518348A Active JP7042812B2 (ja) | 2016-06-20 | 2017-06-19 | トリアゾロピリミジン化合物の結晶形態 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US11091489B2 (enExample) |
| EP (1) | EP3472168B1 (enExample) |
| JP (1) | JP7042812B2 (enExample) |
| KR (1) | KR102519922B1 (enExample) |
| CN (1) | CN109563100B (enExample) |
| AU (1) | AU2017282871B2 (enExample) |
| CA (1) | CA3027246A1 (enExample) |
| CL (2) | CL2018003734A1 (enExample) |
| ES (1) | ES2975263T3 (enExample) |
| IL (1) | IL263429B (enExample) |
| MX (1) | MX388824B (enExample) |
| RU (1) | RU2754856C2 (enExample) |
| SA (1) | SA518400704B1 (enExample) |
| WO (1) | WO2017219948A1 (enExample) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
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| EP3365340B1 (en) | 2015-10-19 | 2022-08-10 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| HUE060680T2 (hu) | 2015-11-19 | 2023-04-28 | Incyte Corp | Heterociklusos vegyületek mint immunmodulátorok |
| EP3394033B1 (en) | 2015-12-22 | 2020-11-25 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| WO2017192961A1 (en) | 2016-05-06 | 2017-11-09 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| TW201808902A (zh) | 2016-05-26 | 2018-03-16 | 美商英塞特公司 | 作為免疫調節劑之雜環化合物 |
| MD3472167T2 (ro) | 2016-06-20 | 2023-02-28 | Incyte Corp | Compuși heterociclici ca imunomodulatori |
| WO2018013789A1 (en) | 2016-07-14 | 2018-01-18 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| US20180057486A1 (en) | 2016-08-29 | 2018-03-01 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| PE20200005A1 (es) | 2016-12-22 | 2020-01-06 | Incyte Corp | Derivados de tetrahidro imidazo[4,5-c]piridina como inductores de internalizacion pd-l1 |
| EP3558963B1 (en) | 2016-12-22 | 2022-03-23 | Incyte Corporation | Bicyclic heteroaromatic compounds as immunomodulators |
| EP3558973B1 (en) | 2016-12-22 | 2021-09-15 | Incyte Corporation | Pyridine derivatives as immunomodulators |
| MA47123A (fr) | 2016-12-22 | 2021-03-17 | Incyte Corp | Dérivés de benzooxazole en tant qu'mmunomodulateurs |
| EP3558989B1 (en) | 2016-12-22 | 2021-04-14 | Incyte Corporation | Triazolo[1,5-a]pyridine derivatives as immunomodulators |
| PT4043466T (pt) * | 2018-01-31 | 2024-10-14 | Mirati Therapeutics Inc | Inibidores de prc2 |
| 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 |
| PL4212529T3 (pl) | 2018-03-30 | 2025-07-07 | Incyte Corporation | Związki heterocykliczne jako immunomodulatory |
| HRP20230306T1 (hr) | 2018-05-11 | 2023-05-12 | Incyte Corporation | Derivati tetrahidro-imidazo[4,5-c]piridina kao pd-l1 imunomodulatori |
| 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 |
| JP7549597B2 (ja) * | 2019-03-15 | 2024-09-11 | フルクラム セラピューティクス，インコーポレイテッド | Ｅｅｄおよびｐｒｃ２調節物質としての大環状アゾロピリジン誘導体 |
| LT3856341T (lt) * | 2019-04-12 | 2023-12-27 | Blueprint Medicines Corporation | (s)-1-(4-fluorfenil)-1-(2-(4-(6-(1-metil-1h-pirazol-4-il)pirolo[2,1-f] [1,2,4]triazin-4-il)piperazinil)-pirimidin-5-il)etan-1-amino kristalinės formos ir gamybos būdai |
| EP3959214A1 (en) | 2019-04-22 | 2022-03-02 | Mirati Therapeutics, Inc. | Naphthyridine derivatives as prc2 inhibitors |
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| WO2021030162A1 (en) | 2019-08-09 | 2021-02-18 | Incyte Corporation | Salts of a pd-1/pd-l1 inhibitor |
| 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 |
| IL291471B2 (en) | 2019-09-30 | 2025-04-01 | Incyte Corp | Pyrimido[3,2–D]pyrimidine compounds as immunomodulators |
| CN110796297B (zh) * | 2019-10-21 | 2020-11-10 | 浙江大学 | 一种基于平衡度方差和可靠度的电力系统结构优化方法 |
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| CN114426541B (zh) * | 2020-10-29 | 2023-06-30 | 成都先导药物开发股份有限公司 | 氮杂芳基化合物及其用途 |
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| US11780836B2 (en) | 2020-11-06 | 2023-10-10 | Incyte Corporation | Process of preparing a PD-1/PD-L1 inhibitor |
| WO2022099075A1 (en) | 2020-11-06 | 2022-05-12 | Incyte Corporation | Crystalline form of a pd-1/pd-l1 inhibitor |
| WO2022105852A1 (zh) | 2020-11-20 | 2022-05-27 | 江苏恒瑞医药股份有限公司 | 三嗪二酮类衍生物、其制备方法及其在医药上的应用 |
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| ES2722048T3 (es) | 2014-12-23 | 2019-08-07 | Novartis Ag | Compuestos de triazolopirimidina y usos de los mismos |
| MA41272A (fr) | 2014-12-23 | 2017-10-31 | Adama Makhteshim Ltd | 5-fluoro-4-imino-3-(alkyle/alkyle substitué)-1-(arylsulfonyl)-3,4-dihydropyrimidin-2(1h)-one en tant que traitement des semences |
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2017
- 2017-06-19 US US16/311,638 patent/US11091489B2/en active Active
- 2017-06-19 CA CA3027246A patent/CA3027246A1/en active Pending
- 2017-06-19 AU AU2017282871A patent/AU2017282871B2/en active Active
- 2017-06-19 CN CN201780050951.1A patent/CN109563100B/zh active Active
- 2017-06-19 JP JP2019518348A patent/JP7042812B2/ja active Active
- 2017-06-19 MX MX2018016331A patent/MX388824B/es unknown
- 2017-06-19 EP EP17814686.6A patent/EP3472168B1/en active Active
- 2017-06-19 RU RU2019101220A patent/RU2754856C2/ru active
- 2017-06-19 IL IL263429A patent/IL263429B/en unknown
- 2017-06-19 KR KR1020197001451A patent/KR102519922B1/ko active Active
- 2017-06-19 ES ES17814686T patent/ES2975263T3/es active Active
- 2017-06-19 WO PCT/CN2017/089003 patent/WO2017219948A1/en not_active Ceased
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2018
- 2018-12-20 SA SA518400704A patent/SA518400704B1/ar unknown
- 2018-12-20 CL CL2018003734A patent/CL2018003734A1/es unknown
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2020
- 2020-09-02 CL CL2020002277A patent/CL2020002277A1/es unknown
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2021
- 2021-07-09 US US17/371,399 patent/US11548897B2/en active Active
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