CN100432070C - 新颖的磺酰胺类化合物及其作为内皮素受体拮抗剂的应用 - Google Patents

新颖的磺酰胺类化合物及其作为内皮素受体拮抗剂的应用 Download PDF

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Publication number
CN100432070C
CN100432070C CNB018204813A CN01820481A CN100432070C CN 100432070 C CN100432070 C CN 100432070C CN B018204813 A CNB018204813 A CN B018204813A CN 01820481 A CN01820481 A CN 01820481A CN 100432070 C CN100432070 C CN 100432070C
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pyrimidyl
phenyl
acid
bromo
oxyethyl group
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CN1524079A (zh
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马丁·博利
克里斯托夫·博斯
瓦尔特·菲施利
马丁内·克洛泽尔
托马斯·韦勒
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Actelion Pharmaceuticals Ltd
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Actelion Pharmaceuticals Ltd
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  • Organic Chemistry (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CNB018204813A 2000-12-18 2001-12-04 新颖的磺酰胺类化合物及其作为内皮素受体拮抗剂的应用 Expired - Lifetime CN100432070C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EPPCT/EP00/12890 2000-12-18
EP0012890 2000-12-18

Publications (2)

Publication Number Publication Date
CN1524079A CN1524079A (zh) 2004-08-25
CN100432070C true CN100432070C (zh) 2008-11-12

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CNB018204813A Expired - Lifetime CN100432070C (zh) 2000-12-18 2001-12-04 新颖的磺酰胺类化合物及其作为内皮素受体拮抗剂的应用

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US (2) US7094781B2 (enExample)
EP (2) EP1693372A1 (enExample)
JP (1) JP4245130B2 (enExample)
KR (1) KR100819668B1 (enExample)
CN (1) CN100432070C (enExample)
AR (1) AR035610A1 (enExample)
AT (1) ATE323079T1 (enExample)
AU (1) AU2002227984B8 (enExample)
BE (1) BE2014C019I2 (enExample)
BR (1) BRPI0116237B8 (enExample)
CA (1) CA2431675C (enExample)
CY (2) CY1105060T1 (enExample)
DE (1) DE60118782T2 (enExample)
DK (1) DK1345920T3 (enExample)
ES (1) ES2260318T3 (enExample)
FR (1) FR14C0017I2 (enExample)
HU (1) HU229403B1 (enExample)
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MY (1) MY129150A (enExample)
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PT (1) PT1345920E (enExample)
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Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002053557A1 (en) * 2000-12-18 2002-07-11 Actelion Pharmaceuticals Ltd Novel sulfamides and their use as endothelin receptor antagonists
MXPA04005510A (es) * 2001-12-07 2006-02-24 Vertex Pharma Compuestos basados en pirimidina utiles como inhibidores de gsk-3.
AU2003285321B2 (en) * 2002-12-02 2010-04-08 Actelion Pharmaceuticals Ltd Pyrimidine-sulfamides and their use as endothelian receptor antagonist
HRP20120901T1 (hr) 2004-03-05 2012-12-31 F. Hoffmann - La Roche Ag Diaminopirimidini kao p2x3 i p2x2/3
UA90269C2 (ru) 2004-04-02 2010-04-26 Мицубиси Танабе Фарма Корпорейшн Тетрагидрохинолиновые производные и способ их получения
TW200628467A (en) * 2004-11-11 2006-08-16 Actelion Pharmaceuticals Ltd Novel sulfamides
US8183277B2 (en) 2005-07-29 2012-05-22 Tibotec Pharmaceuticals Ltd. Macrocylic inhibitors of hepatitis C virus
DK1912997T3 (da) 2005-07-29 2012-01-02 Tibotec Pharm Ltd Makrocycliske inhibitorer af hepatitis C virus
JP4850912B2 (ja) 2005-09-01 2012-01-11 エフ．ホフマン−ラ ロシュ アーゲー Ｐ２ｘ３およびｐ３ｘ２／３モジュレーターとしてのジアミノピリミジン
WO2007025901A1 (en) 2005-09-01 2007-03-08 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
CA2619919C (en) 2005-09-01 2014-04-01 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
PT1928409E (pt) 2005-09-12 2012-11-27 Actelion Pharmaceuticals Ltd Composição farmacêutica estável que compreende uma pirimidina-sulfamida
AR062501A1 (es) 2006-08-29 2008-11-12 Actelion Pharmaceuticals Ltd Composiciones terapeuticas
US7983024B2 (en) 2007-04-24 2011-07-19 Littelfuse, Inc. Fuse card system for automotive circuit protection
MX2010001837A (es) * 2007-08-17 2010-03-10 Actelion Pharmaceuticals Ltd Derivados de 4-pirimidinasulfamida.
JP5466507B2 (ja) 2007-09-27 2014-04-09 興和株式会社 テトラヒドロキノリン化合物を有効成分とする貧血の予防及び／又は治療剤
US8541433B2 (en) * 2008-02-20 2013-09-24 Actelion Pharmaceuticals, Ltd. Combination comprising macitentan and paclitaxel for treating multi-drug resistant ovarian cancer
SG192485A1 (en) * 2008-07-08 2013-08-30 Incyte Corp 1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase
ES2652590T3 (es) * 2008-08-13 2018-02-05 Actelion Pharmaceuticals Ltd. Composiciones terapéuticas que contienen macitentan
US8791090B2 (en) 2009-03-31 2014-07-29 Kowa Company, Ltd. Prophylactic and/or therapeutic agent for anemia comprising tetrahydroquinoline compound as active ingredient
SG178828A1 (en) 2009-08-10 2012-04-27 Univ Texas Treatment of brain metastases with inhibitors of endothelin receptors in combination with a cytotoxic chemotherapy agent
ES2608670T3 (es) 2009-08-17 2017-04-12 Memorial Sloan-Kettering Cancer Center Derivados de 2-(pirimidin-5-il)-tiopirimidina como moduladores de Hsp70 y Hsc70 para el tratamiento de trastornos proliferativos
WO2011078143A1 (ja) * 2009-12-22 2011-06-30 塩野義製薬株式会社 ピリミジン誘導体およびそれらを含有する医薬組成物
EP2965757A1 (en) 2011-02-04 2016-01-13 Actelion Pharmaceuticals Ltd. Pharmaceutical compositions for treating malignant glioma
JP2016510781A (ja) * 2013-03-15 2016-04-11 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ＲＯＲｃモジュレーターとしてのアリールスルファミド及びスルファミン酸誘導体
AR095727A1 (es) * 2013-03-27 2015-11-04 Actelion Pharmaceuticals Ltd Preparación de intermediarios de pirimidina
DE14721256T1 (de) 2013-04-22 2017-03-16 Sandoz Ag Pharmazeutische zusammensetzungen mit kristallinem macitentan
WO2014198178A1 (zh) * 2013-06-14 2014-12-18 杭州普晒医药科技有限公司 马西替坦晶体及其制备方法、其药物组合物和用途
AR096865A1 (es) * 2013-07-12 2016-02-03 Actelion Pharmaceuticals Ltd Proceso para la preparación de un intermediario 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
CN103819411A (zh) * 2014-03-14 2014-05-28 成都克莱蒙医药科技有限公司 一种马西替坦中间体新的制备方法
EP3143013B1 (en) 2014-05-13 2019-12-18 Memorial Sloan Kettering Cancer Center Hsp70 modulators and methods for making and using the same
US20170158645A1 (en) * 2014-07-15 2017-06-08 Olon S.P.A. Amorphous form and new crystalline forms of macitentan
CN104447572A (zh) * 2014-12-15 2015-03-25 南京艾德凯腾生物医药有限责任公司 一种马西替坦的制备方法
WO2016203489A1 (en) 2015-06-15 2016-12-22 Megafine Pharma (P) Ltd. Process for the preparation of macitentan and intermediates thereof
ZA201605808B (en) 2015-08-26 2017-08-30 Cipla Ltd Process for preparing an endothelin receptor antagonist
CN105388244B (zh) * 2015-12-10 2017-03-08 合肥久诺医药科技有限公司 一种马西替坦有关物质的高效液相色谱分析方法
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
WO2017191565A1 (en) * 2016-05-04 2017-11-09 Shilpa Medicare Limited Process for preparation of macitentan
CN107868055B (zh) * 2016-09-28 2020-02-07 普济生物科技（台州）有限公司 一种马西替坦的制备方法
CN106478520B (zh) * 2016-10-11 2018-09-11 合肥久诺医药科技有限公司 一种马西替坦杂质标准品的合成方法
CN106478522A (zh) * 2016-10-11 2017-03-08 合肥久诺医药科技有限公司 一种马西替坦杂质标准品的制备方法
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
BR112019020693B1 (pt) 2017-04-03 2023-11-28 Syngenta Participations Ag Compostos derivados de oxadiazol microbiocidas, suas composições, método para controlar ou prevenir a infestação de plantas úteis por microrganismos fitopatogênicos utilizando tais compostos e seus usos
CN107141238A (zh) * 2017-06-16 2017-09-08 吴宁怡 一种马西替坦中间体的制备方法
AU2018372752B2 (en) 2017-11-21 2023-02-02 Wuxi Biocity Biopharmaceutics Co., Ltd. Pyrimidine sulfamide derivative and preparation method and medical application thereof
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
CN108653292B (zh) * 2018-07-03 2019-05-24 中国人民解放军总医院 一种化合物在治疗或预防高原病中的用途
CN108997223B (zh) * 2018-08-09 2020-06-30 浙江先锋科技股份有限公司 5-(4-溴苯基)-4，6-二氯嘧啶的制备方法
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
CA3123990A1 (en) 2018-12-21 2020-06-25 Actelion Pharmaceuticals Ltd Pharmaceutical composition for the treatment of pulmonary arterial hypertension
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
TW202103703A (zh) 2019-04-05 2021-02-01 瑞士商艾克泰聯製藥有限公司 用於治療門脈肺高血壓之方法
WO2020233694A1 (zh) * 2019-05-22 2020-11-26 石家庄智康弘仁新药开发有限公司 一种嘧啶磺酰胺类化合物的晶型及其制备方法
HUE068040T2 (hu) 2019-07-05 2024-12-28 Tecnimede Sociedade Tecnico Medicinal Sa Préselt macitentán készítmények, eljárások és ezek felhasználása
BR112022010311A2 (pt) 2019-11-29 2022-08-16 Actelion Pharmaceuticals Ltd Métodos de tratamento de hipertensão arterial pulmonar
TW202317119A (zh) 2021-06-11 2023-05-01 瑞士商艾克泰聯製藥有限公司 用於口服投予之分散錠
EP4154873A1 (en) 2021-09-22 2023-03-29 Sanovel Ilac Sanayi Ve Ticaret A.S. The tablet comprising macitentan
CN119255805A (zh) 2022-05-22 2025-01-03 爱杜西亚药品有限公司 用于治疗高血压的阿普昔腾坦
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
CN120187431A (zh) 2022-11-07 2025-06-20 埃科特莱茵药品有限公司 用于治疗肺动脉高血压的马西替坦和他达拉非的组合
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0475039A2 (en) * 1990-08-13 1992-03-18 General Electric Company Ortho ester-capped polyphenylene ethers and copolymers prepared therefrom
EP0601781A2 (en) * 1992-12-02 1994-06-15 General Electric Company Polyarylene sulfide and epoxy-functionalized siloxane blends

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2801584A1 (de) * 1978-01-14 1979-07-19 Bayer Ag Halogensubstituierte pyrimidin (2)yl-thiono-thiol-phosphor(phosphon)- saeureester, verfahren zu ihrer herstellung und ihre verwendung als insektizide und akarizide
RU2086544C1 (ru) 1991-06-13 1997-08-10 Хоффманн-Ля Рош АГ Бензолсульфонамидные производные пиримидина или их соли, фармацевтическая композиция для лечения заболеваний, связанных с активностью эндотелина
TW394761B (en) 1993-06-28 2000-06-21 Hoffmann La Roche Novel Sulfonylamino Pyrimidines
US5523204A (en) 1993-12-10 1996-06-04 Becton Dickinson And Company Detection of nucleic acids in cells by strand displacement amplification
WO1996016963A1 (de) * 1994-11-25 1996-06-06 F. Hoffmann-La Roche Ag Sulfonamide und deren verwendung als heilmittel
TW313568B (enExample) * 1994-12-20 1997-08-21 Hoffmann La Roche
US5739333A (en) * 1995-05-16 1998-04-14 Tanabe Seiyaku Co., Ltd. Sulfonamide derivative and process for preparing the same
ATE201202T1 (de) 1995-12-20 2001-06-15 Yamanouchi Pharma Co Ltd Arylethensulfonamid-derivate und diese enthaltende medikamente
TWI284642B (en) * 1999-01-18 2007-08-01 Hoffmann La Roche Novel heterocyclic sulfonamides
ES2295048T3 (es) * 1999-09-03 2008-04-16 Actelion Pharmaceuticals Ltd. Bis-sulfonamidas.
IL149529A0 (en) * 1999-12-22 2002-11-10 Actelion Pharmaceuticals Ltd Butyne diol derivatives
AU2001263850A1 (en) * 2000-04-20 2001-11-07 Actelion Pharmaceuticals Ltd Pyrimidine-sulfonamides having endothelin-antagonist activity
AU2001265871A1 (en) * 2000-04-25 2001-11-07 Actelion Pharmaceuticals Ltd Substituted sulfonylaminopyrimidines
WO2002053557A1 (en) * 2000-12-18 2002-07-11 Actelion Pharmaceuticals Ltd Novel sulfamides and their use as endothelin receptor antagonists

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0475039A2 (en) * 1990-08-13 1992-03-18 General Electric Company Ortho ester-capped polyphenylene ethers and copolymers prepared therefrom
EP0601781A2 (en) * 1992-12-02 1994-06-15 General Electric Company Polyarylene sulfide and epoxy-functionalized siloxane blends

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