JP2020508339A5 - - Google Patents
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- Publication number
- JP2020508339A5 JP2020508339A5 JP2019546291A JP2019546291A JP2020508339A5 JP 2020508339 A5 JP2020508339 A5 JP 2020508339A5 JP 2019546291 A JP2019546291 A JP 2019546291A JP 2019546291 A JP2019546291 A JP 2019546291A JP 2020508339 A5 JP2020508339 A5 JP 2020508339A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- dosage form
- diuretic
- per day
- 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
Links
- 150000003839 salts Chemical class 0.000 claims 44
- 239000002552 dosage form Substances 0.000 claims 19
- 229960002003 hydrochlorothiazide Drugs 0.000 claims 14
- JZUFKLXOESDKRF-UHFFFAOYSA-N Chlorothiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NCNS2(=O)=O JZUFKLXOESDKRF-UHFFFAOYSA-N 0.000 claims 12
- 239000002934 diuretic Substances 0.000 claims 12
- 230000001882 diuretic effect Effects 0.000 claims 12
- 239000004072 C09CA03 - Valsartan Substances 0.000 claims 10
- 229960000528 amlodipine Drugs 0.000 claims 10
- 229960004699 valsartan Drugs 0.000 claims 10
- HTIQEAQVCYTUBX-UHFFFAOYSA-N amlodipine Chemical compound CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1Cl HTIQEAQVCYTUBX-UHFFFAOYSA-N 0.000 claims 9
- 229940030600 antihypertensive agent Drugs 0.000 claims 9
- 239000002220 antihypertensive agent Substances 0.000 claims 9
- 239000003814 drug Substances 0.000 claims 9
- SJSNUMAYCRRIOM-QFIPXVFZSA-N valsartan Chemical compound C1=CC(CN(C(=O)CCCC)[C@@H](C(C)C)C(O)=O)=CC=C1C1=CC=CC=C1C1=NN=N[N]1 SJSNUMAYCRRIOM-QFIPXVFZSA-N 0.000 claims 8
- 208000020832 chronic kidney disease Diseases 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- JIVPVXMEBJLZRO-CQSZACIVSA-N 2-chloro-5-[(1r)-1-hydroxy-3-oxo-2h-isoindol-1-yl]benzenesulfonamide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC([C@@]2(O)C3=CC=CC=C3C(=O)N2)=C1 JIVPVXMEBJLZRO-CQSZACIVSA-N 0.000 claims 6
- 229960001523 chlortalidone Drugs 0.000 claims 6
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 5
- 229940125364 angiotensin receptor blocker Drugs 0.000 claims 5
- 239000000480 calcium channel blocker Substances 0.000 claims 5
- 239000005458 thiazide-like diuretic Substances 0.000 claims 5
- 206010020772 Hypertension Diseases 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 4
- 208000015658 resistant hypertension Diseases 0.000 claims 3
- 208000007530 Essential hypertension Diseases 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 230000007211 cardiovascular event Effects 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 238000010586 diagram Methods 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 206010007558 Cardiac failure chronic Diseases 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000003037 Diastolic Heart Failure Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
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/EP2017/078371 WO2018153513A1 (en) | 2017-02-27 | 2017-11-06 | Combinations of a 4-pyrimidinesulfamide derivative with active ingredients for the treatment of endothelin related diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020508339A JP2020508339A (ja) | 2020-03-19 |
| JP2020508339A5 true JP2020508339A5 (OSRAM) | 2020-12-17 |
| JP7223701B2 JP7223701B2 (ja) | 2023-02-16 |
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 After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Country Status (29)
| Country | Link |
|---|---|
| US (5) | US11174247B2 (OSRAM) |
| EP (3) | EP3658140B1 (OSRAM) |
| JP (3) | JP7223701B2 (OSRAM) |
| KR (3) | KR102700778B1 (OSRAM) |
| CN (3) | CN110325186A (OSRAM) |
| AU (2) | AU2017400276B2 (OSRAM) |
| BR (2) | BR112019017658A2 (OSRAM) |
| CA (2) | CA3053991A1 (OSRAM) |
| CL (3) | CL2019002464A1 (OSRAM) |
| DK (2) | DK3658140T3 (OSRAM) |
| ES (2) | ES3038007T3 (OSRAM) |
| FI (2) | FI3658140T3 (OSRAM) |
| HR (2) | HRP20250921T1 (OSRAM) |
| HU (2) | HUE072288T2 (OSRAM) |
| IL (4) | IL315563A (OSRAM) |
| LT (2) | LT3658140T (OSRAM) |
| MA (2) | MA49664A (OSRAM) |
| MX (3) | MX392313B (OSRAM) |
| MY (2) | MY199557A (OSRAM) |
| NZ (1) | NZ757344A (OSRAM) |
| PH (2) | PH12019501937A1 (OSRAM) |
| PL (2) | PL3658140T3 (OSRAM) |
| PT (2) | PT3658140T (OSRAM) |
| RS (2) | RS67082B1 (OSRAM) |
| SG (3) | SG11201907435PA (OSRAM) |
| SI (2) | SI3658140T1 (OSRAM) |
| TW (2) | TWI786089B (OSRAM) |
| UA (1) | UA126122C2 (OSRAM) |
| WO (2) | WO2018153513A1 (OSRAM) |
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 |
| LT3658140T (lt) | 2017-02-27 | 2025-08-25 | Idorsia Pharmaceuticals Ltd | Aprocitentano ir kitų veikliųjų sudedamųjų dalių deriniai, skirti atsparios hipertenzijos gydymui |
| PL3716979T3 (pl) * | 2017-11-30 | 2025-08-04 | Idorsia Pharmaceuticals Ltd | Połączenie pochodnej 4-pirymidynosulfamidu z inhibitorem sglt-2 do leczenia chorób związanych w endoteliną |
| WO2020069521A1 (en) | 2018-09-28 | 2020-04-02 | Flow Medical Corporation | Catheter apparatus |
| MA54522B1 (fr) | 2018-12-21 | 2024-07-31 | Actelion Pharmaceuticals Ltd | Macitentan pour le traitement de l'hypertension artérielle pulmonaire |
| 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 |
| EP4056182A1 (en) * | 2019-11-07 | 2022-09-14 | Crystal Pharmaceutical (Suzhou) Co., Ltd. | Crystal form of aprocitentan, preparation method therefor and use thereof |
| WO2021237004A1 (en) | 2020-05-21 | 2021-11-25 | Teva Pharmaceuticals International Gmbh | Solid state forms of aprocitentan and process for preparation thereof |
| US11730735B2 (en) | 2020-07-10 | 2023-08-22 | Astrazeneca Ab | Combination of zibotentan and dapagliflozin for the treatment of endothelin related diseases |
| 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 |
| WO2023227490A1 (en) | 2022-05-22 | 2023-11-30 | Idorsia Pharmaceuticals Ltd | Aprocitentan for the treatment of hypertension |
| 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 |
|---|---|---|---|---|
| DE59409631D1 (de) | 1993-07-15 | 2001-02-15 | Hoffmann La Roche | Pharmazeutische Kombination, die einen Hemmer des Renin-Angiotensin-Systems und einen Endothelin-Antagonisten enthält |
| BRPI0116237B8 (pt) | 2000-12-18 | 2021-05-25 | Actelion Pharmaceuticals Ltd | "composto de sulfamida, composição farmacêutica contendo o mesmo e seu uso como medicamento antagonista de receptor de endotelina". |
| 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 |
| WO2007146900A2 (en) | 2006-06-15 | 2007-12-21 | 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. |
| CA2697057A1 (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 |
| EP3215138A4 (en) | 2014-11-07 | 2018-11-21 | 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 |
| LT3658140T (lt) | 2017-02-27 | 2025-08-25 | Idorsia Pharmaceuticals Ltd | Aprocitentano ir kitų veikliųjų sudedamųjų dalių deriniai, skirti atsparios hipertenzijos gydymui |
| PL3716979T3 (pl) | 2017-11-30 | 2025-08-04 | Idorsia Pharmaceuticals Ltd | Połączenie pochodnej 4-pirymidynosulfamidu z inhibitorem sglt-2 do leczenia chorób związanych w endoteliną |
| MA54522B1 (fr) * | 2018-12-21 | 2024-07-31 | Actelion Pharmaceuticals Ltd | Macitentan pour le traitement de l'hypertension artérielle pulmonaire |
-
2017
- 2017-11-06 LT LTEPPCT/EP2017/078371T patent/LT3658140T/lt unknown
- 2017-11-06 UA UAA201909965A patent/UA126122C2/uk unknown
- 2017-11-06 SI SI201731613T patent/SI3658140T1/sl unknown
- 2017-11-06 MY MYPI2019004938A patent/MY199557A/en unknown
- 2017-11-06 CN CN201780087445.XA patent/CN110325186A/zh active Pending
- 2017-11-06 BR BR112019017658-6A patent/BR112019017658A2/pt not_active Application Discontinuation
- 2017-11-06 DK DK17794712.4T patent/DK3658140T3/da active
- 2017-11-06 CA CA3053991A patent/CA3053991A1/en active Pending
- 2017-11-06 IL IL315563A patent/IL315563A/en unknown
- 2017-11-06 MA MA049664A patent/MA49664A/fr unknown
- 2017-11-06 KR KR1020237016438A patent/KR102700778B1/ko active Active
- 2017-11-06 HU HUE17794712A patent/HUE072288T2/hu unknown
- 2017-11-06 US US16/489,227 patent/US11174247B2/en active Active
- 2017-11-06 ES ES17794712T patent/ES3038007T3/es active Active
- 2017-11-06 PT PT177947124T patent/PT3658140T/pt unknown
- 2017-11-06 HR HRP20250921TT patent/HRP20250921T1/hr unknown
- 2017-11-06 IL IL268850A patent/IL268850B2/en unknown
- 2017-11-06 PL PL17794712.4T patent/PL3658140T3/pl unknown
- 2017-11-06 KR KR1020197028199A patent/KR102568472B1/ko active Active
- 2017-11-06 AU AU2017400276A patent/AU2017400276B2/en active Active
- 2017-11-06 RS RS20250776A patent/RS67082B1/sr unknown
- 2017-11-06 EP EP17794712.4A patent/EP3658140B1/en active Active
- 2017-11-06 MX MX2019010222A patent/MX392313B/es unknown
- 2017-11-06 WO PCT/EP2017/078371 patent/WO2018153513A1/en not_active Ceased
- 2017-11-06 FI FIEP17794712.4T patent/FI3658140T3/fi active
- 2017-11-06 JP JP2019546291A patent/JP7223701B2/ja active Active
- 2017-11-06 SG SG11201907435PA patent/SG11201907435PA/en unknown
- 2017-11-06 NZ NZ757344A patent/NZ757344A/en unknown
-
2018
- 2018-02-26 SI SI201831162T patent/SI4014976T1/sl unknown
- 2018-02-26 EP EP18708945.3A patent/EP3585391A1/en not_active Withdrawn
- 2018-02-26 CN CN201880014146.8A patent/CN110381948A/zh active Pending
- 2018-02-26 PL PL21202979.7T patent/PL4014976T3/pl unknown
- 2018-02-26 JP JP2019546286A patent/JP2020508338A/ja active Pending
- 2018-02-26 KR KR1020197028200A patent/KR102577375B1/ko active Active
- 2018-02-26 RS RS20241269A patent/RS66200B1/sr unknown
- 2018-02-26 US US16/489,194 patent/US10919881B2/en active Active
- 2018-02-26 DK DK21202979.7T patent/DK4014976T3/da active
- 2018-02-26 ES ES21202979T patent/ES3006308T3/es active Active
- 2018-02-26 BR BR112019017644-6A patent/BR112019017644A2/pt not_active Application Discontinuation
- 2018-02-26 CA CA3053994A patent/CA3053994A1/en active Pending
- 2018-02-26 MX MX2019010221A patent/MX2019010221A/es unknown
- 2018-02-26 SG SG11201907604UA patent/SG11201907604UA/en unknown
- 2018-02-26 AU AU2018225309A patent/AU2018225309B2/en active Active
- 2018-02-26 HU HUE21202979A patent/HUE069231T2/hu unknown
- 2018-02-26 FI FIEP21202979.7T patent/FI4014976T3/fi active
- 2018-02-26 SG SG10202111695RA patent/SG10202111695RA/en unknown
- 2018-02-26 TW TW107106403A patent/TWI786089B/zh active
- 2018-02-26 MA MA047596A patent/MA47596A/fr unknown
- 2018-02-26 LT LTEP21202979.7T patent/LT4014976T/lt unknown
- 2018-02-26 EP EP21202979.7A patent/EP4014976B1/en active Active
- 2018-02-26 TW TW111142832A patent/TWI854353B/zh active
- 2018-02-26 IL IL297993A patent/IL297993B2/en unknown
- 2018-02-26 MY MYPI2019004939A patent/MY208610A/en unknown
- 2018-02-26 CN CN202311718027.XA patent/CN117946011A/zh active Pending
- 2018-02-26 WO PCT/EP2018/054627 patent/WO2018154101A1/en not_active Ceased
- 2018-02-26 PT PT212029797T patent/PT4014976T/pt unknown
- 2018-02-26 HR HRP20241461TT patent/HRP20241461T1/hr unknown
-
2019
- 2019-08-22 PH PH12019501937A patent/PH12019501937A1/en unknown
- 2019-08-22 PH PH12019501938A patent/PH12019501938A1/en unknown
- 2019-08-22 IL IL26885219A patent/IL268852A/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
-
2020
- 2020-06-30 CL CL2020001762A patent/CL2020001762A1/es unknown
-
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
-
2022
- 2022-12-16 JP JP2022201112A patent/JP7520951B2/ja active Active
-
2023
- 2023-05-17 US US18/319,402 patent/US12297189B2/en active Active
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