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)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (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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ID=41037724

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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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CN102697790A (zh) 2003-05-22 2012-10-03 联合治疗公司 化合物和释放前列环素类似物的方法
WO2009078965A1 (en) 2007-12-17 2009-06-25 United Therapeutics Corporation An improved process to prepare treprostinil, the active ingredient in remodulin
KR20160132501A (ko) 2010-03-15 2016-11-18 유나이티드 세러퓨틱스 코오포레이션 폐고혈압의 치료
CN103261142B (zh) 2010-06-03 2014-12-10 联合治疗公司 曲前列环素的制备
ES2581762T3 (es) 2011-03-02 2016-09-07 United Therapeutics Corporation Síntesis de producto intermedio para la producción de treprostinil
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
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
WO2014159050A1 (en) * 2013-03-14 2014-10-02 United Therapeutics Corporation Solid forms of treprostinil
EP2970081A4 (en) 2013-03-15 2016-10-12 United Therapeutics Corp SALTS OF TREPROSTINIL
WO2014160638A1 (en) 2013-03-25 2014-10-02 United Therapeutics Corporation Process of making prostacyclin compounds with linker thiol and pegylated forms
CA2911172C (en) 2013-04-30 2021-10-19 United Therapeutics Corporation Controlled release pharmaceutical formulations
US9469600B2 (en) 2013-10-25 2016-10-18 Insmed Incorporated Prostacyclin compounds, compositions and methods of use thereof
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
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
EP3452170A4 (en) 2016-05-05 2020-04-01 Liquidia Technologies, Inc. TREPROSTINIL IN POWDER FORM FOR TREATING PULMONAL HYPERTENSION
WO2018058124A1 (en) 2016-09-26 2018-03-29 United Therapeutics Corporation Treprostinil prodrugs
CN110381930A (zh) 2016-12-05 2019-10-25 康赛制药公司 曲前列环素及其盐的经皮和透皮施用
CN112739679B (zh) 2018-09-18 2024-03-12 伊莱利利公司 曲前列环素的特丁胺盐
CN119632930A (zh) 2019-04-29 2025-03-18 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
JP7365073B2 (ja) * 2019-05-21 2023-10-19 ジァンスー フォアフロント ファーマシューティカル カンパニー，リミテッド トレプロスチニルナトリウムの新規な結晶形および製造方法
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
IL296567A (en) 2020-04-17 2022-11-01 United Therapeutics Corp Terfostinil for use in the treatment of interstitial lung disease
AU2021289336B2 (en) 2020-06-09 2025-08-28 Mannkind 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
KR102849520B1 (ko) 2020-12-14 2025-08-25 유나이티드 쎄러퓨틱스 코포레이션 트레프로스티닐 프로드러그로 질환을 치료하는 방법
WO2022187352A1 (en) 2021-03-03 2022-09-09 United Therapeutics Corporation A dry powder composition of trestinil and its prodrug thereof and further comprising comprising (e)-3,6-bis[4-(n-carbonyl-2-propenyl)amidobutyl]-2,5-diketopiperazine (fdkp)
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
CN121241041A (zh) 2023-01-19 2025-12-30 联合治疗公司 曲前列尼尔类似物及相关制备和使用方法
US20260166056A1 (en) 2024-12-13 2026-06-18 United Therapeutics Corporation Treprostinil formulations and their uses

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

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