JP2020508338A5 - - Google Patents
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- Publication number
- JP2020508338A5 JP2020508338A5 JP2019546286A JP2019546286A JP2020508338A5 JP 2020508338 A5 JP2020508338 A5 JP 2020508338A5 JP 2019546286 A JP2019546286 A JP 2019546286A JP 2019546286 A JP2019546286 A JP 2019546286A JP 2020508338 A5 JP2020508338 A5 JP 2020508338A5
- Authority
- JP
- Japan
- Prior art keywords
- bromo
- pyrimidine
- pharmaceutical composition
- compound
- yloxy
- 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
Links
- 239000013078 crystal Substances 0.000 claims 17
- 239000008194 pharmaceutical composition Substances 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 14
- 238000000634 powder X-ray diffraction Methods 0.000 claims 10
- 238000010586 diagram Methods 0.000 claims 9
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims 7
- 239000003814 drug Substances 0.000 claims 6
- DKULOVKANLVDEA-UHFFFAOYSA-N ACT-132577 Chemical compound C=1C=C(Br)C=CC=1C=1C(NS(=O)(=O)N)=NC=NC=1OCCOC1=NC=C(Br)C=N1 DKULOVKANLVDEA-UHFFFAOYSA-N 0.000 claims 5
- 229940079593 drug Drugs 0.000 claims 5
- NVBFHJWHLNUMCV-UHFFFAOYSA-N sulfamide Chemical compound NS(N)(=O)=O NVBFHJWHLNUMCV-UHFFFAOYSA-N 0.000 claims 5
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 4
- 239000007787 solid Substances 0.000 claims 4
- 206010020772 Hypertension Diseases 0.000 claims 3
- 239000004480 active ingredient Substances 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- -1 pyrimidin-2-yloxy Chemical group 0.000 claims 3
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 2
- 239000008101 lactose Substances 0.000 claims 2
- 235000019359 magnesium stearate Nutrition 0.000 claims 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 2
- 239000008108 microcrystalline cellulose Substances 0.000 claims 2
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 1
- 229960001681 croscarmellose sodium Drugs 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 0 Cc(cn1)cnc1OCCOc1ncnc(N*(N)=C)c1-c(cc1)ccc1Br Chemical compound Cc(cn1)cnc1OCCOc1ncnc(N*(N)=C)c1-c(cc1)ccc1Br 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022201112A JP7520951B2 (ja) | 2017-02-27 | 2022-12-16 | ４－ピリミジンスルファミド誘導体の結晶形 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EPPCT/EP2017/054489 | 2017-02-27 | ||
| EP2017054489 | 2017-02-27 | ||
| EP2017061487 | 2017-05-12 | ||
| EPPCT/EP2017/061487 | 2017-05-12 | ||
| PCT/EP2018/054627 WO2018154101A1 (en) | 2017-02-27 | 2018-02-26 | Crystalline forms of the 4-pyrimidinesulfamide derivative aprocitentan |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022201112A Division JP7520951B2 (ja) | 2017-02-27 | 2022-12-16 | ４－ピリミジンスルファミド誘導体の結晶形 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020508338A JP2020508338A (ja) | 2020-03-19 |
| JP2020508338A5 true JP2020508338A5 (cg-RX-API-DMAC7.html) | 2021-04-15 |
Family
ID=60268369
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019546291A Active JP7223701B2 (ja) | 2017-02-27 | 2017-11-06 | ４－ピリミジンスルファミド誘導体の、エンドセリン関連疾患治療用の有効成分との合剤 |
| JP2019546286A Pending JP2020508338A (ja) | 2017-02-27 | 2018-02-26 | ４−ピリミジンスルファミド誘導体の結晶形 |
| JP2022201112A Active JP7520951B2 (ja) | 2017-02-27 | 2022-12-16 | ４－ピリミジンスルファミド誘導体の結晶形 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019546291A Active JP7223701B2 (ja) | 2017-02-27 | 2017-11-06 | ４－ピリミジンスルファミド誘導体の、エンドセリン関連疾患治療用の有効成分との合剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022201112A Active JP7520951B2 (ja) | 2017-02-27 | 2022-12-16 | ４－ピリミジンスルファミド誘導体の結晶形 |
Country Status (29)
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20160045527A1 (en) * | 2014-08-14 | 2016-02-18 | Vivus, Inc. | Treatment of sleep apnea with a combination of a carbonic anhydrase inhibitor and an aldosterone antagonist |
| UA126122C2 (uk) | 2017-02-27 | 2022-08-17 | Ідорсія Фармасьютікалз Лтд | Комбінації похідної 4-піримідинсульфаміду з активними інгредієнтами для лікування захворювань, пов'язаних з ендотеліном |
| US12144811B2 (en) * | 2017-11-30 | 2024-11-19 | Idorsia Pharmaceuticals Ltd | Combination of a 4-pyrimidinesulfamide derivative with an SGLT-2 inhibitor for the treatment of endothelin related diseases |
| WO2020069521A1 (en) | 2018-09-28 | 2020-04-02 | Flow Medical Corporation | Catheter apparatus |
| SI3897646T1 (sl) * | 2018-12-21 | 2024-08-30 | ACTELION PHARMACEUTICALS lTD, | Makitentan za zdravljenje pljučne arterijske hipertenzije |
| TW202042818A (zh) | 2019-01-25 | 2020-12-01 | 瑞士商艾克泰聯製藥有限公司 | 用於治療慢性血栓性肺高血壓之醫藥組成物 |
| CN112569357B (zh) * | 2019-09-30 | 2023-03-28 | 深圳奥萨制药有限公司 | 双重内皮素受体拮抗剂与利尿剂的组合物 |
| CN112679441A (zh) * | 2019-10-18 | 2021-04-20 | 普济生物科技（台州）有限公司 | 阿普昔腾坦的晶型、制备方法及其用途 |
| CN114630668B (zh) * | 2019-11-07 | 2024-02-27 | 苏州科睿思制药有限公司 | 一种Aprocitentan晶型及其制备方法和用途 |
| US12421214B2 (en) | 2020-05-21 | 2025-09-23 | Assia Chemical Industries Ltd. | Solid state forms of aprocitentan and process for preparation thereof |
| CN115803028A (zh) | 2020-07-10 | 2023-03-14 | 阿斯利康(瑞典)有限公司 | 用于治疗慢性肾病的齐泊腾坦和达格列净的组合 |
| CN114644595A (zh) * | 2020-12-19 | 2022-06-21 | 普济生物科技（台州）有限公司 | 阿普昔腾坦的无定型态、其药物组合物和用途 |
| WO2023111797A1 (en) * | 2021-12-17 | 2023-06-22 | Janssen Biotech, Inc. | Pyrimidine sulfamide derivatives and process for manufacturing them |
| JP2025519101A (ja) | 2022-05-22 | 2025-06-24 | イドルシア・ファーマシューティカルズ・リミテッド | 高血圧の治療のための４－ピリミジンスルファミド誘導体の使用 |
| CA3251318A1 (en) | 2022-05-25 | 2023-11-30 | Idorsia Pharmaceuticals Ltd | CRYSTALLINE FORMS OF (5-(4-BROMOPHENYL)-6-(2-((5-BROMOPYRIMIDIN-2-YL)OXY)ETHOXY)PYRIMIDIN-4-YL)(SULFAMOYL) SODIUM AMIDE |
| WO2024140425A1 (zh) * | 2022-12-30 | 2024-07-04 | 苏州科睿思制药有限公司 | 一种阿普昔腾坦晶型及其制备方法和用途 |
| KR20250152723A (ko) | 2024-04-16 | 2025-10-24 | 경북대학교 산학협력단 | 신규한 피리미딘 유도체 화합물 및 이의 용도 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2154277T3 (es) | 1993-07-15 | 2001-04-01 | Hoffmann La Roche | Combinacion farmaceutica que contiene un inhibidor del sistema renina-angiotensina y un antagonista de endotelina. |
| WO2002053557A1 (en) | 2000-12-18 | 2002-07-11 | Actelion Pharmaceuticals Ltd | Novel sulfamides and their use as endothelin receptor antagonists |
| EG24716A (en) | 2002-05-17 | 2010-06-07 | Novartis Ag | Combination of organic compounds |
| US20070196510A1 (en) | 2006-02-17 | 2007-08-23 | Gerber Michael J | Method for treating resistant hypertension |
| EP2029137A2 (en) | 2006-06-15 | 2009-03-04 | Gilead Colorado, Inc. | Antihypertensive therapy method |
| PE20120542A1 (es) | 2006-06-27 | 2012-05-14 | Novartis Ag | Formas de dosificacion solidas de valsartan, amlodipina e hidroclorotiazida y metodo para elaborarlas |
| MX2010001837A (es) * | 2007-08-17 | 2010-03-10 | Actelion Pharmaceuticals Ltd | Derivados de 4-pirimidinasulfamida. |
| WO2009026517A2 (en) | 2007-08-22 | 2009-02-26 | Gilead Colorado, Inc. | Therapy for complications of diabetes |
| CN102614189B (zh) * | 2012-04-17 | 2014-10-22 | 北京哈三联科技股份有限公司 | 含缬沙坦、氨氯地平和氢氯噻嗪的微丸药物组合 |
| EP2907811A1 (en) * | 2014-02-14 | 2015-08-19 | Actelion Pharmaceuticals Ltd. | Process for manufacturing pyrimidine sulfamide derivatives |
| AU2015342929A1 (en) | 2014-11-07 | 2017-05-25 | Abbvie Inc. | Methods of treating CKD using predictors of fluid retention |
| WO2017185142A1 (en) | 2016-04-29 | 2017-11-02 | Adelaide Research & Innovation Pty Ltd | Method for preventing and/or treating atrial fibrillation |
| UA126122C2 (uk) | 2017-02-27 | 2022-08-17 | Ідорсія Фармасьютікалз Лтд | Комбінації похідної 4-піримідинсульфаміду з активними інгредієнтами для лікування захворювань, пов'язаних з ендотеліном |
| US12144811B2 (en) | 2017-11-30 | 2024-11-19 | Idorsia Pharmaceuticals Ltd | Combination of a 4-pyrimidinesulfamide derivative with an SGLT-2 inhibitor for the treatment of endothelin related diseases |
| SI3897646T1 (sl) * | 2018-12-21 | 2024-08-30 | ACTELION PHARMACEUTICALS lTD, | Makitentan za zdravljenje pljučne arterijske hipertenzije |
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2017
- 2017-11-06 UA UAA201909965A patent/UA126122C2/uk unknown
- 2017-11-06 HU HUE17794712A patent/HUE072288T2/hu unknown
- 2017-11-06 JP JP2019546291A patent/JP7223701B2/ja active Active
- 2017-11-06 MY MYPI2019004938A patent/MY199557A/en unknown
- 2017-11-06 IL IL268850A patent/IL268850B2/en unknown
- 2017-11-06 KR KR1020197028199A patent/KR102568472B1/ko active Active
- 2017-11-06 FI FIEP17794712.4T patent/FI3658140T3/fi active
- 2017-11-06 PT PT177947124T patent/PT3658140T/pt unknown
- 2017-11-06 US US16/489,227 patent/US11174247B2/en active Active
- 2017-11-06 BR BR112019017658-6A patent/BR112019017658A2/pt not_active Application Discontinuation
- 2017-11-06 PL PL17794712.4T patent/PL3658140T3/pl unknown
- 2017-11-06 MX MX2019010222A patent/MX392313B/es unknown
- 2017-11-06 RS RS20250776A patent/RS67082B1/sr unknown
- 2017-11-06 HR HRP20250921TT patent/HRP20250921T1/hr unknown
- 2017-11-06 IL IL315563A patent/IL315563A/en unknown
- 2017-11-06 KR KR1020237016438A patent/KR102700778B1/ko active Active
- 2017-11-06 CA CA3053991A patent/CA3053991A1/en active Pending
- 2017-11-06 WO PCT/EP2017/078371 patent/WO2018153513A1/en not_active Ceased
- 2017-11-06 DK DK17794712.4T patent/DK3658140T3/da active
- 2017-11-06 NZ NZ757344A patent/NZ757344A/en unknown
- 2017-11-06 AU AU2017400276A patent/AU2017400276B2/en active Active
- 2017-11-06 EP EP17794712.4A patent/EP3658140B1/en active Active
- 2017-11-06 ES ES17794712T patent/ES3038007T3/es active Active
- 2017-11-06 MA MA049664A patent/MA49664A/fr unknown
- 2017-11-06 CN CN201780087445.XA patent/CN110325186A/zh active Pending
- 2017-11-06 LT LTEPPCT/EP2017/078371T patent/LT3658140T/lt unknown
- 2017-11-06 SI SI201731613T patent/SI3658140T1/sl unknown
- 2017-11-06 SG SG11201907435PA patent/SG11201907435PA/en unknown
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2018
- 2018-02-26 ES ES21202979T patent/ES3006308T3/es active Active
- 2018-02-26 CA CA3053994A patent/CA3053994A1/en active Pending
- 2018-02-26 AU AU2018225309A patent/AU2018225309B2/en active Active
- 2018-02-26 HU HUE21202979A patent/HUE069231T2/hu unknown
- 2018-02-26 SG SG11201907604UA patent/SG11201907604UA/en unknown
- 2018-02-26 SI SI201831162T patent/SI4014976T1/sl unknown
- 2018-02-26 RS RS20241269A patent/RS66200B1/sr unknown
- 2018-02-26 WO PCT/EP2018/054627 patent/WO2018154101A1/en not_active Ceased
- 2018-02-26 EP EP21202979.7A patent/EP4014976B1/en active Active
- 2018-02-26 TW TW111142832A patent/TWI854353B/zh active
- 2018-02-26 US US16/489,194 patent/US10919881B2/en active Active
- 2018-02-26 LT LTEP21202979.7T patent/LT4014976T/lt unknown
- 2018-02-26 MX MX2019010221A patent/MX2019010221A/es unknown
- 2018-02-26 MY MYPI2019004939A patent/MY208610A/en unknown
- 2018-02-26 CN CN202311718027.XA patent/CN117946011A/zh active Pending
- 2018-02-26 EP EP18708945.3A patent/EP3585391A1/en not_active Withdrawn
- 2018-02-26 FI FIEP21202979.7T patent/FI4014976T3/fi active
- 2018-02-26 PT PT212029797T patent/PT4014976T/pt unknown
- 2018-02-26 DK DK21202979.7T patent/DK4014976T3/da active
- 2018-02-26 CN CN201880014146.8A patent/CN110381948A/zh active Pending
- 2018-02-26 TW TW107106403A patent/TWI786089B/zh active
- 2018-02-26 SG SG10202111695RA patent/SG10202111695RA/en unknown
- 2018-02-26 JP JP2019546286A patent/JP2020508338A/ja active Pending
- 2018-02-26 PL PL21202979.7T patent/PL4014976T3/pl unknown
- 2018-02-26 MA MA047596A patent/MA47596A/fr unknown
- 2018-02-26 BR BR112019017644-6A patent/BR112019017644A2/pt not_active Application Discontinuation
- 2018-02-26 KR KR1020197028200A patent/KR102577375B1/ko active Active
- 2018-02-26 HR HRP20241461TT patent/HRP20241461T1/hr unknown
- 2018-02-26 IL IL297993A patent/IL297993B2/en unknown
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2019
- 2019-08-22 PH PH12019501938A patent/PH12019501938A1/en unknown
- 2019-08-22 IL IL26885219A patent/IL268852A/en unknown
- 2019-08-22 PH PH12019501937A patent/PH12019501937A1/en unknown
- 2019-08-27 CL CL2019002464A patent/CL2019002464A1/es unknown
- 2019-08-27 CL CL2019002470A patent/CL2019002470A1/es unknown
- 2019-08-27 MX MX2021007184A patent/MX2021007184A/es unknown
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2020
- 2020-06-30 CL CL2020001762A patent/CL2020001762A1/es unknown
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2021
- 2021-01-12 US US17/146,801 patent/US11680058B2/en active Active
- 2021-09-10 US US17/472,349 patent/US11787782B2/en active Active
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2022
- 2022-12-16 JP JP2022201112A patent/JP7520951B2/ja active Active
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2023
- 2023-05-17 US US18/319,402 patent/US12297189B2/en active Active
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