CA2937277C - Process for manufacturing pyrimidine sulfamide derivatives - Google Patents

Process for manufacturing pyrimidine sulfamide derivatives Download PDF

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Publication number
CA2937277C
CA2937277C CA2937277A CA2937277A CA2937277C CA 2937277 C CA2937277 C CA 2937277C CA 2937277 A CA2937277 A CA 2937277A CA 2937277 A CA2937277 A CA 2937277A CA 2937277 C CA2937277 C CA 2937277C
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Canada
Prior art keywords
compound
formula
salt
aprotic organic
reaction
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Active
Application number
CA2937277A
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English (en)
French (fr)
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CA2937277A1 (en
Inventor
Stefan Abele
Jacques-Alexis Funel
Ivan SCHINDELHOLZ
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Idorsia Pharmaceuticals Ltd
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Idorsia Pharmaceuticals Ltd
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=50073084&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2937277(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Idorsia Pharmaceuticals Ltd filed Critical Idorsia Pharmaceuticals Ltd
Publication of CA2937277A1 publication Critical patent/CA2937277A1/en
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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/56One oxygen atom and one sulfur atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/18Sulfonamides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/34One oxygen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Compositions Of Macromolecular Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
CA2937277A 2014-02-14 2015-02-13 Process for manufacturing pyrimidine sulfamide derivatives Active CA2937277C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14155137.4A EP2907811A1 (en) 2014-02-14 2014-02-14 Process for manufacturing pyrimidine sulfamide derivatives
EP14155137.4 2014-02-14
PCT/EP2015/053047 WO2015121397A1 (en) 2014-02-14 2015-02-13 Process for manufacturing pyrimidine sulfamide derivatives

Publications (2)

Publication Number Publication Date
CA2937277A1 CA2937277A1 (en) 2015-08-20
CA2937277C true CA2937277C (en) 2021-07-06

Family

ID=50073084

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2937277A Active CA2937277C (en) 2014-02-14 2015-02-13 Process for manufacturing pyrimidine sulfamide derivatives

Country Status (28)

Country Link
US (1) US9938244B2 (2)
EP (3) EP2907811A1 (2)
JP (2) JP6431922B2 (2)
KR (2) KR102406358B1 (2)
CN (2) CN105992762B (2)
AR (2) AR099434A1 (2)
AU (2) AU2015217000B2 (2)
BR (2) BR112016018581B1 (2)
CA (1) CA2937277C (2)
CL (2) CL2016002008A1 (2)
CY (1) CY1123319T1 (2)
DK (1) DK3105220T3 (2)
EA (2) EA032933B1 (2)
ES (2) ES2819504T3 (2)
HK (1) HK1243405A1 (2)
HR (1) HRP20201450T1 (2)
HU (1) HUE050974T2 (2)
IL (1) IL251126A0 (2)
LT (1) LT3105220T (2)
MX (2) MX377801B (2)
NZ (1) NZ724273A (2)
PL (1) PL3105220T3 (2)
PT (1) PT3105220T (2)
SA (1) SA516371640B1 (2)
SG (2) SG10201701994RA (2)
SI (1) SI3105220T1 (2)
TW (2) TWI666203B (2)
WO (1) WO2015121397A1 (2)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
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
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
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
KR102568472B1 (ko) 2017-02-27 2023-08-18 이도르시아 파마슈티컬스 리미티드 엔도텔린 관련 질환의 치료를 위한 4-피리미딘술파미드 유도체와 활성 성분의 조합물
KR20260037123A (ko) 2017-11-30 2026-03-17 이도르시아 파마슈티컬스 리미티드 엔도텔린 관련 질병의 치료를 위한 sglt-2 저해제와의 4-피리미딘설파미드 유도체의 병용
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
AU2020378025A1 (en) * 2019-11-07 2022-06-23 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
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
US20250340520A1 (en) 2022-05-25 2025-11-06 Idorsia Pharmaceuticals Ltd Crystalline forms of sodium (5-(4-bromophenyl)-6-(2-((5-bromopyrimidin-2-yl)oxy)ethoxy)pyrimidin-4-yl)(sulfamoyl)amide
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)

* Cited by examiner, † Cited by third party
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
HU229403B1 (en) 2000-12-18 2013-12-30 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
DE60224223T2 (de) * 2002-01-02 2008-12-04 Actelion Pharmaceuticals Ltd. Neue alkylsulfonamide als endothelinantagonisten
MX2010001837A (es) 2007-08-17 2010-03-10 Actelion Pharmaceuticals Ltd Derivados de 4-pirimidinasulfamida.
US20130310362A1 (en) 2009-02-13 2013-11-21 Bayer Pharma Aktiegesellschaft Fused pyrimidines
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

Also Published As

Publication number Publication date
AU2015217000A1 (en) 2016-09-29
CY1123319T1 (el) 2021-12-31
MX377801B (es) 2025-03-11
HUE050974T2 (hu) 2021-01-28
SG11201606667VA (en) 2016-09-29
EP3214082B1 (en) 2021-11-10
CA2937277A1 (en) 2015-08-20
BR122017005939B1 (pt) 2022-12-20
NZ724273A (en) 2020-06-26
BR112016018581B1 (pt) 2022-11-16
BR112016018581A2 (pt) 2017-08-08
CN107162988B (zh) 2020-08-21
HRP20201450T1 (hr) 2020-12-25
WO2015121397A1 (en) 2015-08-20
AU2017202446B2 (en) 2019-03-28
CN105992762B (zh) 2019-04-16
LT3105220T (lt) 2020-10-12
SG10201701994RA (en) 2017-05-30
CN107162988A (zh) 2017-09-15
JP2017125055A (ja) 2017-07-20
SA516371640B1 (ar) 2019-09-08
US20160368882A1 (en) 2016-12-22
EA032933B1 (ru) 2019-08-30
AU2017202446A1 (en) 2017-05-04
MX2016010486A (es) 2016-10-31
MX368014B (es) 2019-09-13
JP6421209B2 (ja) 2018-11-07
KR20170029656A (ko) 2017-03-15
AU2015217000B2 (en) 2019-02-14
KR102261695B1 (ko) 2021-06-07
TW201613877A (en) 2016-04-16
BR122017005939A2 (pt) 2019-09-10
TW201730157A (zh) 2017-09-01
EA201790343A1 (ru) 2017-06-30
AR099434A1 (es) 2016-07-20
TWI663155B (zh) 2019-06-21
BR112016018581A8 (pt) 2021-06-22
EP3105220B1 (en) 2020-07-01
US9938244B2 (en) 2018-04-10
KR20160122213A (ko) 2016-10-21
PL3105220T3 (pl) 2020-12-28
DK3105220T3 (da) 2020-09-07
EP3214082A1 (en) 2017-09-06
SI3105220T1 (sl) 2020-10-30
TWI666203B (zh) 2019-07-21
ES2906458T3 (es) 2022-04-18
CL2016002008A1 (es) 2017-02-03
EP2907811A1 (en) 2015-08-19
IL251126A0 (en) 2017-04-30
NZ729685A (en) 2020-11-27
JP2017505801A (ja) 2017-02-23
CN105992762A (zh) 2016-10-05
EA032460B1 (ru) 2019-05-31
EA201691618A1 (ru) 2017-01-30
HK1243405A1 (en) 2018-07-13
AR107801A2 (es) 2018-06-06
CL2017000505A1 (es) 2017-11-24
JP6431922B2 (ja) 2018-11-28
KR102406358B1 (ko) 2022-06-07
ES2819504T3 (es) 2021-04-16
EP3105220A1 (en) 2016-12-21
PT3105220T (pt) 2020-09-23

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