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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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
plain
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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United Therapeutics Corp
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/58—Unsaturated compounds containing ether groups, groups, groups, or groups
    • C07C59/72—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings and other rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/42—Separation; Purification; Stabilisation; Use of additives
    • C07C51/487—Separation; Purification; Stabilisation; Use of additives by treatment giving rise to chemical modification
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- 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
    • C07C2603/14—Benz[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)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (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

Country Status (8)

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

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CA2526534C (en) 2003-05-22 2011-07-12 United Therapeutics Corporation Compounds and methods for delivery of prostacyclin analogs
CN103274926B (zh) 2007-12-17 2016-08-10 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
JP5681276B2 (ja) 2010-03-15 2015-03-04 ユナイテッド セラピューティクス コーポレイション 肺高血圧症のための治療
WO2011153363A1 (en) 2010-06-03 2011-12-08 United Therapeutics Corporation Treprostinil production
EP2681204B1 (en) 2011-03-02 2016-04-27 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
EP2970091A4 (en) * 2013-03-14 2017-02-08 United Therapeutics Corporation Solid forms of treprostinil
JP2016516693A (ja) 2013-03-15 2016-06-09 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塩
CN105228451B (zh) 2013-03-25 2018-03-30 联合治疗公司 制备具有硫醇连接子和聚乙二醇化形式的前列环素化合物的方法
CN105407883A (zh) 2013-04-30 2016-03-16 联合治疗学有限公司 控释药物制剂
HRP20210351T1 (hr) 2013-10-25 2021-04-30 Insmed Incorporated Spojevi prostaciklina
JP2017517550A (ja) * 2014-06-13 2017-06-29 ユナイテッド セラピューティクス コーポレイション トレプロスチニル製剤
WO2016038532A1 (en) * 2014-09-09 2016-03-17 Mylan Laboratories Limited Amorphous treprostinil diethanolamine
HU231184B1 (hu) * 2014-10-08 2021-07-28 CHINOIN Gyógyszer és Vegyészeti Termékek Gyára Zrt. Treprostinil-nátrium-monohidrát és eljárás ennek előállítására
CN107108427A (zh) 2014-10-20 2017-08-29 联合治疗学有限公司 用于制备前列环素衍生物的中间体的合成
US10343979B2 (en) 2014-11-18 2019-07-09 Insmed Incorporated Methods of manufacturing treprostinil and treprostinil derivative prodrugs
IL310250B2 (en) 2016-05-05 2025-09-01 Liquidia Tech Inc Terpostinil in dry powder form for the treatment of pulmonary hypertension
CA3038276A1 (en) 2016-09-26 2018-03-29 United Therapeutics Corporation Treprostinil prodrugs
EP3548010A1 (en) 2016-12-05 2019-10-09 Corsair Pharma, Inc. Dermal and transdermal administration of treprostinil and salts thereof
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
US12435023B2 (en) * 2019-05-21 2025-10-07 Shanghai Forefront Pharmceutical Co., Ltd. Crystal form of Treprostinil sodium salt and preparation method therefor
CN114616225A (zh) 2019-08-23 2022-06-10 联合治疗公司 曲前列环素前药
US11339110B2 (en) 2019-12-19 2022-05-24 Chirogate International Inc. Efficient crystallization process for preparing ultrapure Treprostinil and crystal prepared therefrom
WO2021211916A1 (en) 2020-04-17 2021-10-21 United Therapeutics Corporation Treprostinil for use in the treatment of intersitial lung disease
EP4161909A1 (en) 2020-06-09 2023-04-12 United Therapeutics Corporation Fumaryl diketopiperidine prodrugs of treprostinil
US11447440B2 (en) 2020-10-29 2022-09-20 Chirogate International Inc. Treprostinil monohydrate crystals and methods for preparation thereof
CN117062605A (zh) 2020-12-14 2023-11-14 联合治疗公司 使用曲前列环素前药治疗疾病的方法
CN117479946A (zh) 2021-03-03 2024-01-30 联合治疗公司 含曲前列环素及其前药并还包含(e)-3,6-双[4-(n-羰基-2-丙烯基)酰胺丁基]-2,5-二酮哌嗪(fdkp)的干粉组合物
WO2023154705A1 (en) 2022-02-08 2023-08-17 United Therapeutics Corporation Treprostinil iloprost combination therapy
EP4516297A1 (en) 2022-04-29 2025-03-05 Zhaoke Pharmaceutical (Guangzhou) Co., Ltd Treprostinil soft mist inhalant
AU2024208919A1 (en) 2023-01-19 2025-07-17 United Therapeutics Corporation Treprostinil analogs

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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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WO2005058329A1 (en) * 2003-12-16 2005-06-30 United Therapeutics Corporation Use of treprostinil to improve kidney functions
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Also Published As

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

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