CN102015613B - 曲前列素一水合物 - Google Patents

曲前列素一水合物 Download PDF

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Publication number
CN102015613B
CN102015613B CN2009801161262A CN200980116126A CN102015613B CN 102015613 B CN102015613 B CN 102015613B CN 2009801161262 A CN2009801161262 A CN 2009801161262A CN 200980116126 A CN200980116126 A CN 200980116126A CN 102015613 B CN102015613 B CN 102015613B
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qianlie
monohydrate
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anhydrous
solid
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CN102015613A (zh
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大卫·A·沃尔什
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United Therapeutics Corp
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40Unsaturated compounds
    • C07C59/58Unsaturated compounds containing ether groups, groups, groups, or groups
    • C07C59/72Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings and other rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/42Separation; Purification; Stabilisation; Use of additives
    • C07C51/487Separation; Purification; Stabilisation; Use of additives by treatment giving rise to chemical modification
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/02Ortho- or ortho- and peri-condensed systems
    • C07C2603/04Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/14Benz[f]indenes; Hydrogenated benz[f]indenes

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN2009801161262A 2008-05-08 2009-05-07 曲前列素一水合物 Active CN102015613B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US5150908P 2008-05-08 2008-05-08
US61/051,509 2008-05-08
PCT/US2009/002818 WO2009137066A1 (en) 2008-05-08 2009-05-07 Treprostinil monohydrate

Publications (2)

Publication Number Publication Date
CN102015613A CN102015613A (zh) 2011-04-13
CN102015613B true CN102015613B (zh) 2013-07-31

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CN2009801161262A Active CN102015613B (zh) 2008-05-08 2009-05-07 曲前列素一水合物

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Country Link
US (1) US8350079B2 (https=)
EP (2) EP2300408B1 (https=)
JP (1) JP6219016B2 (https=)
KR (1) KR20110010753A (https=)
CN (1) CN102015613B (https=)
CA (1) CA2723540C (https=)
ES (1) ES2575565T3 (https=)
WO (1) WO2009137066A1 (https=)

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CN101903324B (zh) 2007-12-17 2013-07-03 联合治疗公司 一种制备Remodulin中的活性成分曲前列素的改良方法
ES2611187T3 (es) 2010-03-15 2017-05-05 United Therapeutics Corporation Tratamiento para hipertensión pulmonar
JP6046034B2 (ja) 2010-06-03 2016-12-14 ユナイテッド セラピューティクス コーポレイション トレプロスチニルの製造
US20130345471A1 (en) 2011-03-02 2013-12-26 United Therapeutics Corporation Synthesis of intermediate for treprostinil production
CN103193626B (zh) * 2012-01-10 2016-05-11 上海天伟生物制药有限公司 一种前列腺素类似物的晶型及其制备方法和用途
CN103193627B (zh) * 2012-01-10 2016-04-20 上海天伟生物制药有限公司 一种前列腺素类似物的晶型及其制备方法和用途
JP2016517410A (ja) * 2013-03-14 2016-06-16 ユナイテッド セラピューティクス コーポレイション トレプロスチニルの固体形態
CN109608326A (zh) 2013-03-15 2019-04-12 联合治疗公司 曲前列环素的盐
JP6263604B2 (ja) 2013-03-25 2018-01-17 ユナイテッド セラピューティクス コーポレイション チオールリンカーを持つ、ペグ化型のプロスタサイクリン化合物の製造方法
US9758465B2 (en) 2013-04-30 2017-09-12 United Therapeutics Corporation Controlled release pharmaceutical formulations
ES2860975T3 (es) 2013-10-25 2021-10-05 Insmed Inc Compuestos de prostaciclina
ES2908142T3 (es) * 2014-06-13 2022-04-27 United Therapeutics Corp Formulaciones de treprostinil
WO2016038532A1 (en) * 2014-09-09 2016-03-17 Mylan Laboratories Limited Amorphous treprostinil diethanolamine
HU231186B1 (hu) * 2014-10-08 2021-06-28 CHINOIN Gyógyszer és Vegyészeti Termékek Gyára Zrt. Új eljárás treprostinil és sói előállítására
US9593061B2 (en) 2014-10-20 2017-03-14 United Therapeutics Corporation Synthesis of intermediates for producing prostacyclin derivatives
AU2015349969B2 (en) 2014-11-18 2020-02-06 Insmed Incorporated Methods of manufacturing treprostinil and treprostinil derivative prodrugs
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JP7220650B2 (ja) 2016-09-26 2023-02-10 ユナイテッド セラピューティクス コーポレイション トレプロスチニルプロドラッグ
KR20190109399A (ko) 2016-12-05 2019-09-25 코세어 파마 인코포레이티드 트레프로스티닐 및 이의 염의 피부 및 경피 투여
ES2976468T3 (es) 2018-09-18 2024-08-01 Lilly Co Eli Sal de treprostinil erbumina
CN114072136B (zh) 2019-04-29 2024-11-29 英斯梅德股份有限公司 曲前列素前药的干粉组合物及其使用方法
CN112313202A (zh) * 2019-05-21 2021-02-02 江苏众强药业有限公司 曲前列尼尔钠盐新晶型及制备方法
EP4017588A1 (en) 2019-08-23 2022-06-29 United Therapeutics Corporation Treprostinil prodrugs
US11339110B2 (en) 2019-12-19 2022-05-24 Chirogate International Inc. Efficient crystallization process for preparing ultrapure Treprostinil and crystal prepared therefrom
JP2023523557A (ja) 2020-04-17 2023-06-06 ユナイテッド セラピューティクス コーポレイション 間質性肺疾患の治療における使用のためのトレプロスチニル
IL298591A (en) 2020-06-09 2023-01-01 United Therapeutics Corp Pomeryl dictopiperidine prodrugs of treprostinil
US11447440B2 (en) 2020-10-29 2022-09-20 Chirogate International Inc. Treprostinil monohydrate crystals and methods for preparation thereof
KR20250133451A (ko) 2020-12-14 2025-09-05 유나이티드 쎄러퓨틱스 코포레이션 트레프로스티닐 프로드러그로 질환을 치료하는 방법
JP2024510930A (ja) 2021-03-03 2024-03-12 ユナイテッド セラピューティクス コーポレイション トレプロスチニル及びそのプロドラッグの乾燥粉末組成物、及び、さらに(e)-3,6-ビス[4-(n-カルボニル-2-プロペニル)アミドブチル]-2,5-ジケトピペラジン(fdkp)を含む乾燥粉末組成物
WO2023154705A1 (en) 2022-02-08 2023-08-17 United Therapeutics Corporation Treprostinil iloprost combination therapy
EP4516297A4 (en) 2022-04-29 2026-02-25 Zhaoke pharmaceutical guangzhou co ltd Treprostinil Gentle Inhalation Mist
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WO2005099680A2 (en) * 2004-04-12 2005-10-27 United Therapeutics, Inc. Use of treprostinil to treat neuropathic diabetic foot ulcers
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Also Published As

Publication number Publication date
US20090281189A1 (en) 2009-11-12
CA2723540A1 (en) 2009-11-12
EP3002274A1 (en) 2016-04-06
EP2300408B1 (en) 2016-04-13
EP2300408A1 (en) 2011-03-30
CA2723540C (en) 2016-01-05
CN102015613A (zh) 2011-04-13
US8350079B2 (en) 2013-01-08
WO2009137066A1 (en) 2009-11-12
JP6219016B2 (ja) 2017-10-25
ES2575565T3 (es) 2016-06-29
JP2011519927A (ja) 2011-07-14
EP3002274A8 (en) 2016-07-13
KR20110010753A (ko) 2011-02-07

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