JP2017505801A5 - - Google Patents
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- Publication number
- JP2017505801A5 JP2017505801A5 JP2016551796A JP2016551796A JP2017505801A5 JP 2017505801 A5 JP2017505801 A5 JP 2017505801A5 JP 2016551796 A JP2016551796 A JP 2016551796A JP 2016551796 A JP2016551796 A JP 2016551796A JP 2017505801 A5 JP2017505801 A5 JP 2017505801A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- formula
- salt
- aprotic organic
- polar
- 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
- 150000001875 compounds Chemical class 0.000 claims 18
- 238000000034 method Methods 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 9
- 239000003960 organic solvent Substances 0.000 claims 8
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims 6
- XJHCXCQVJFPJIK-UHFFFAOYSA-M caesium fluoride Chemical compound [F-].[Cs+] XJHCXCQVJFPJIK-UHFFFAOYSA-M 0.000 claims 6
- FPGGTKZVZWFYPV-UHFFFAOYSA-M tetrabutylammonium fluoride Chemical compound [F-].CCCC[N+](CCCC)(CCCC)CCCC FPGGTKZVZWFYPV-UHFFFAOYSA-M 0.000 claims 6
- 239000000460 chlorine Chemical group 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 4
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims 3
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- GQHTUMJGOHRCHB-UHFFFAOYSA-N 2,3,4,6,7,8,9,10-octahydropyrimido[1,2-a]azepine Chemical compound C1CCCCN2CCCN=C21 GQHTUMJGOHRCHB-UHFFFAOYSA-N 0.000 claims 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 125000001246 bromo group Chemical group Br* 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 239000011737 fluorine Chemical group 0.000 claims 1
- 229910052731 fluorine Chemical group 0.000 claims 1
- LPNYRYFBWFDTMA-UHFFFAOYSA-N potassium tert-butoxide Chemical compound [K+].CC(C)(C)[O-] LPNYRYFBWFDTMA-UHFFFAOYSA-N 0.000 claims 1
- 0 *c1c(-c(cc2)ccc2Br)c(OCCOc(nc2)ncc2Br)ncn1 Chemical compound *c1c(-c(cc2)ccc2Br)c(OCCOc(nc2)ncc2Br)ncn1 0.000 description 1
- SEMLWTLQHMDXTE-UHFFFAOYSA-N FC1=C(c(cc2)ccc2Br)C(OCCOc(nc2)ncc2Br)=NCN1 Chemical compound FC1=C(c(cc2)ccc2Br)C(OCCOc(nc2)ncc2Br)=NCN1 SEMLWTLQHMDXTE-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14155137.4 | 2014-02-14 | ||
| EP14155137.4A EP2907811A1 (en) | 2014-02-14 | 2014-02-14 | Process for manufacturing pyrimidine sulfamide derivatives |
| PCT/EP2015/053047 WO2015121397A1 (en) | 2014-02-14 | 2015-02-13 | Process for manufacturing pyrimidine sulfamide derivatives |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017044868A Division JP6421209B2 (ja) | 2014-02-14 | 2017-03-09 | ピリミジンスルファミド誘導体の製造方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017505801A JP2017505801A (ja) | 2017-02-23 |
| JP2017505801A5 true JP2017505801A5 (enExample) | 2018-03-22 |
| JP6431922B2 JP6431922B2 (ja) | 2018-11-28 |
Family
ID=50073084
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016551796A Active JP6431922B2 (ja) | 2014-02-14 | 2015-02-13 | ピリミジンスルファミド誘導体の製造方法 |
| JP2017044868A Active JP6421209B2 (ja) | 2014-02-14 | 2017-03-09 | ピリミジンスルファミド誘導体の製造方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017044868A Active JP6421209B2 (ja) | 2014-02-14 | 2017-03-09 | ピリミジンスルファミド誘導体の製造方法 |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US9938244B2 (enExample) |
| EP (3) | EP2907811A1 (enExample) |
| JP (2) | JP6431922B2 (enExample) |
| KR (2) | KR102406358B1 (enExample) |
| CN (2) | CN107162988B (enExample) |
| AR (2) | AR099434A1 (enExample) |
| AU (2) | AU2015217000B2 (enExample) |
| BR (2) | BR112016018581B1 (enExample) |
| CA (1) | CA2937277C (enExample) |
| CL (2) | CL2016002008A1 (enExample) |
| CY (1) | CY1123319T1 (enExample) |
| DK (1) | DK3105220T3 (enExample) |
| EA (2) | EA032460B1 (enExample) |
| ES (2) | ES2906458T3 (enExample) |
| HK (1) | HK1243405A1 (enExample) |
| HR (1) | HRP20201450T1 (enExample) |
| HU (1) | HUE050974T2 (enExample) |
| IL (1) | IL251126A0 (enExample) |
| LT (1) | LT3105220T (enExample) |
| MX (2) | MX377801B (enExample) |
| NZ (1) | NZ724273A (enExample) |
| PL (1) | PL3105220T3 (enExample) |
| PT (1) | PT3105220T (enExample) |
| SA (1) | SA516371640B1 (enExample) |
| SG (2) | SG10201701994RA (enExample) |
| SI (1) | SI3105220T1 (enExample) |
| TW (2) | TWI666203B (enExample) |
| WO (1) | WO2015121397A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR095727A1 (es) | 2013-03-27 | 2015-11-04 | Actelion Pharmaceuticals Ltd | Preparación de intermediarios de pirimidina |
| EP2907811A1 (en) * | 2014-02-14 | 2015-08-19 | Actelion Pharmaceuticals Ltd. | Process for manufacturing pyrimidine sulfamide derivatives |
| CN105461638A (zh) * | 2015-12-10 | 2016-04-06 | 合肥久诺医药科技有限公司 | 一种马西替坦晶型及其制备方法 |
| CN105461639B (zh) * | 2015-12-10 | 2018-03-09 | 合肥久诺医药科技有限公司 | 一种高纯度马西替坦的精制方法 |
| AU2017400276B2 (en) * | 2017-02-27 | 2024-01-11 | Idorsia Pharmaceuticals Ltd | Combinations of a 4-pyrimidinesulfamide derivative with active ingredients for the treatment of endothelin related diseases |
| ES3035734T3 (en) | 2017-11-30 | 2025-09-08 | Idorsia Pharmaceuticals Ltd | Combination of a 4-pyrimidinesulfamide derivative with an sglt-2 inhibitor for the treatment of endothelin related diseases |
| CN109232546B (zh) * | 2018-09-25 | 2020-09-04 | 中国人民解放军总医院 | 一种嘧啶磺酰胺类衍生物的医药用途 |
| 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 |
| EP4153574A1 (en) | 2020-05-21 | 2023-03-29 | Teva Pharmaceuticals International GmbH | Solid state forms of aprocitentan and process for preparation thereof |
| 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 |
| JP2025517798A (ja) | 2022-05-25 | 2025-06-10 | イドルシア・ファーマシューティカルズ・リミテッド | ナトリウム （５－（４－ブロモフェニル）－６－（２－（（５－ブロモピリミジン－２－イル）オキシ）エトキシ）ピリミジン－４－イル）（スルファモイル）アミドの結晶形 |
| WO2025102245A1 (zh) * | 2023-11-14 | 2025-05-22 | 浙江天宇药业股份有限公司 | 一种双重内皮素受体拮抗剂阿普昔腾坦的合成方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3921918A1 (de) * | 1989-07-04 | 1991-01-17 | Hoechst Ag | Verfahren zur herstellung von 2,4,6-trifluor-1,3,5-triazin |
| WO2002053557A1 (en) | 2000-12-18 | 2002-07-11 | Actelion Pharmaceuticals Ltd | Novel sulfamides and their use as endothelin receptor antagonists |
| TR200103716A2 (tr) * | 2001-12-25 | 2003-07-21 | Ba�Lama Al� | Zenginleştirilmiş dizel yakıt kompozisyonu |
| KR100940432B1 (ko) | 2002-01-02 | 2010-02-10 | 액테리온 파마슈티칼 리미티드 | 엔도텔린 길항제로 유용한 신규한 알칸설폰아마이드 |
| MX2010001837A (es) * | 2007-08-17 | 2010-03-10 | Actelion Pharmaceuticals Ltd | Derivados de 4-pirimidinasulfamida. |
| ES2435804T3 (es) | 2009-02-13 | 2013-12-23 | Bayer Intellectual Property Gmbh | Pirimidinas condensadas como inhibidores de Akt |
| WO2010144477A2 (en) * | 2009-06-12 | 2010-12-16 | Auspex Pharmaceuticals, Inc. | Sulfonylurea modulators of endothelin receptor |
| KR101471047B1 (ko) * | 2012-11-21 | 2014-12-08 | 주식회사 메디켐코리아 | 고순도 보센탄의 개선된 제조방법 |
| CN103012279B (zh) * | 2012-11-27 | 2015-01-28 | 浙江工业大学 | 一种4,5,6-三氟嘧啶化合物的制备方法 |
| AR095727A1 (es) | 2013-03-27 | 2015-11-04 | Actelion Pharmaceuticals Ltd | Preparación de intermediarios de pirimidina |
| CN103724281A (zh) * | 2013-12-03 | 2014-04-16 | 镇江圣安医药有限公司 | N-[5-（4-溴苯基）-6-[2-[（5-溴-2-嘧啶基）氧基]乙氧基]-4-嘧啶基]-n′-丙基磺酰胺的新型衍生物及其应用 |
| EP2907811A1 (en) | 2014-02-14 | 2015-08-19 | Actelion Pharmaceuticals Ltd. | Process for manufacturing pyrimidine sulfamide derivatives |
-
2014
- 2014-02-14 EP EP14155137.4A patent/EP2907811A1/en not_active Withdrawn
-
2015
- 2015-02-13 SG SG10201701994RA patent/SG10201701994RA/en unknown
- 2015-02-13 AU AU2015217000A patent/AU2015217000B2/en active Active
- 2015-02-13 KR KR1020177006399A patent/KR102406358B1/ko active Active
- 2015-02-13 TW TW106114126A patent/TWI666203B/zh not_active IP Right Cessation
- 2015-02-13 HR HRP20201450TT patent/HRP20201450T1/hr unknown
- 2015-02-13 CN CN201710130956.7A patent/CN107162988B/zh active Active
- 2015-02-13 EA EA201790343A patent/EA032460B1/ru not_active IP Right Cessation
- 2015-02-13 BR BR112016018581-1A patent/BR112016018581B1/pt active IP Right Grant
- 2015-02-13 SI SI201531349T patent/SI3105220T1/sl unknown
- 2015-02-13 EP EP15706185.4A patent/EP3105220B1/en active Active
- 2015-02-13 DK DK15706185.4T patent/DK3105220T3/da active
- 2015-02-13 WO PCT/EP2015/053047 patent/WO2015121397A1/en not_active Ceased
- 2015-02-13 US US15/118,046 patent/US9938244B2/en active Active
- 2015-02-13 HU HUE15706185A patent/HUE050974T2/hu unknown
- 2015-02-13 EA EA201691618A patent/EA032933B1/ru not_active IP Right Cessation
- 2015-02-13 KR KR1020167025089A patent/KR102261695B1/ko active Active
- 2015-02-13 MX MX2017003134A patent/MX377801B/es unknown
- 2015-02-13 JP JP2016551796A patent/JP6431922B2/ja active Active
- 2015-02-13 EP EP17159638.0A patent/EP3214082B1/en active Active
- 2015-02-13 CN CN201580008410.3A patent/CN105992762B/zh active Active
- 2015-02-13 ES ES17159638T patent/ES2906458T3/es active Active
- 2015-02-13 ES ES15706185T patent/ES2819504T3/es active Active
- 2015-02-13 PT PT157061854T patent/PT3105220T/pt unknown
- 2015-02-13 MX MX2016010486A patent/MX368014B/es active IP Right Grant
- 2015-02-13 BR BR122017005939-4A patent/BR122017005939B1/pt active IP Right Grant
- 2015-02-13 CA CA2937277A patent/CA2937277C/en active Active
- 2015-02-13 LT LTEP15706185.4T patent/LT3105220T/lt unknown
- 2015-02-13 NZ NZ724273A patent/NZ724273A/en unknown
- 2015-02-13 PL PL15706185T patent/PL3105220T3/pl unknown
- 2015-02-13 SG SG11201606667VA patent/SG11201606667VA/en unknown
- 2015-02-13 TW TW104105167A patent/TWI663155B/zh active
- 2015-02-13 AR ARP150100449A patent/AR099434A1/es active IP Right Grant
-
2016
- 2016-08-09 SA SA516371640A patent/SA516371640B1/ar unknown
- 2016-08-10 CL CL2016002008A patent/CL2016002008A1/es unknown
-
2017
- 2017-03-03 AR ARP170100539A patent/AR107801A2/es unknown
- 2017-03-03 CL CL2017000505A patent/CL2017000505A1/es unknown
- 2017-03-09 JP JP2017044868A patent/JP6421209B2/ja active Active
- 2017-03-13 IL IL251126A patent/IL251126A0/en active IP Right Grant
- 2017-04-12 AU AU2017202446A patent/AU2017202446B2/en not_active Ceased
-
2018
- 2018-02-27 HK HK18102771.1A patent/HK1243405A1/en unknown
-
2020
- 2020-09-04 CY CY20201100833T patent/CY1123319T1/el unknown
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