CA2723540C - Treprostinil monohydrate - Google Patents

Treprostinil monohydrate Download PDF

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Publication number
CA2723540C
CA2723540C CA2723540A CA2723540A CA2723540C CA 2723540 C CA2723540 C CA 2723540C CA 2723540 A CA2723540 A CA 2723540A CA 2723540 A CA2723540 A CA 2723540A CA 2723540 C CA2723540 C CA 2723540C
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CA
Canada
Prior art keywords
treprostinil
monohydrate
water
anhydrous
solid
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CA2723540A
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English (en)
French (fr)
Other versions
CA2723540A1 (en
Inventor
David A. Walsh
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.)
United Therapeutics Corp
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United Therapeutics Corp
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Publication of CA2723540A1 publication Critical patent/CA2723540A1/en
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Publication of CA2723540C publication Critical patent/CA2723540C/en
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Classifications

    • 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

Landscapes

  • 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)
  • Urology & Nephrology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular 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)
CA2723540A 2008-05-08 2009-05-07 Treprostinil monohydrate Active CA2723540C (en)

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
CA2723540A1 CA2723540A1 (en) 2009-11-12
CA2723540C true CA2723540C (en) 2016-01-05

Family

ID=41037724

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2723540A Active CA2723540C (en) 2008-05-08 2009-05-07 Treprostinil monohydrate

Country Status (8)

Country Link
US (1) US8350079B2 (enExample)
EP (2) EP3002274A1 (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)

Families Citing this family (33)

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ES2670872T3 (es) * 2003-05-22 2018-06-01 United Therapeutics Corporation Polimorfo de una sal de dietanolamina de treprostinil
EP3287434A1 (en) 2007-12-17 2018-02-28 United Therapeutics Corporation Process to prepare treprostinil, the active ingredient in remodulin ®
US8609728B2 (en) 2010-03-15 2013-12-17 United Therapeutics Corporation Treatment for pulmonary hypertension
US8481782B2 (en) 2010-06-03 2013-07-09 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
WO2014159050A1 (en) * 2013-03-14 2014-10-02 United Therapeutics Corporation Solid forms of treprostinil
WO2014150203A1 (en) 2013-03-15 2014-09-25 United Therapeutics Corporation Salts of treprostinil
US9102660B2 (en) 2013-03-25 2015-08-11 United Therapeutics Corporaiton Process of making prostacyclin compounds with linker thiol and pegylated forms
US9758465B2 (en) * 2013-04-30 2017-09-12 United Therapeutics Corporation Controlled release pharmaceutical formulations
EA031604B1 (ru) 2013-10-25 2019-01-31 Инсмед Инкорпорейтед Трепростинильные соединения, композиции и способы их использования
AU2015274377B2 (en) * 2014-06-13 2020-07-23 United Therapeutics Corporation Treprostinil formulations
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
ES2873873T3 (es) 2014-11-18 2021-11-04 Insmed Inc Métodos de fabricación de treprostinilo y profármacos derivados de treprostinilo
EP3452170A4 (en) 2016-05-05 2020-04-01 Liquidia Technologies, Inc. DRY POWDER OF TREPROSTINIL FOR THE TREATMENT OF PULMONARY HYPERTENSION
WO2018058124A1 (en) 2016-09-26 2018-03-29 United Therapeutics Corporation Treprostinil prodrugs
WO2018106632A1 (en) 2016-12-05 2018-06-14 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
CA3138530A1 (en) 2019-04-29 2020-11-05 Insmed Incorporated Dry powder compositions of treprostinil prodrugs and methods of use thereof
WO2020233588A1 (zh) * 2019-05-21 2020-11-26 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
JP2022546314A (ja) 2019-08-23 2022-11-04 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
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
US11793780B2 (en) 2020-06-09 2023-10-24 United Therapeutics Corporation Prodrugs of treprosiinil
US11447440B2 (en) 2020-10-29 2022-09-20 Chirogate International Inc. Treprostinil monohydrate crystals and methods for preparation thereof
WO2022132655A1 (en) 2020-12-14 2022-06-23 United Therapeutics Corporation Methods of treating disease with treprostinil prodrugs
IL305510A (en) 2021-03-03 2023-10-01 United Therapeutics Corp A dry powder preparation of terprostinil and its prodrug that will additionally contain (E)-3,6-bis[4-(N-carbonyl-2-propenyl)amidobiotyl]-2,5-dictopiperazine (FDKP)
AU2023219692A1 (en) 2022-02-08 2024-08-01 United Therapeutics Corporation Treprostinil iloprost combination therapy
US20250288597A1 (en) 2022-04-29 2025-09-18 Zhaoke Pharmaceutical (Guangzhou) Co., Ltd Treprostinil soft mist inhalant
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

Family Cites Families (23)

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US4306075A (en) * 1980-03-28 1981-12-15 The Upjohn Company Composition and process
GB8814438D0 (en) * 1988-06-17 1988-07-20 Wellcome Found Compounds for use in medicine
USRE39706E1 (en) * 1993-01-15 2007-06-26 Leo Pharma A/S Crystalline form of a vitamin D analogue
JP3215338B2 (ja) * 1995-12-15 2001-10-02 三菱化学株式会社 アミノベンゼンスルホン酸誘導体一水和物及びその製造方法
IT1282733B1 (it) * 1996-05-20 1998-03-31 Flarer S A Composizioni farmaceutiche contenenti ciclosporina ed un veicolante comprendente almeno un estere dell'acido alfa-glicerofosforico
US6441245B1 (en) 1997-10-24 2002-08-27 United Therapeutics Corporation Process for stereoselective synthesis of prostacyclin derivatives
EP1045695B1 (en) 1997-11-14 2004-03-24 United Therapeutics Corporation Use of 9-deoxy-2', 9-alpha-methano-3- oxa-4,5,6- trinor-3, 7-(1',3'-interphenylene) -13,14-dihydro- prostaglandin f 1? to treat peripheral vascular disease
US6017922A (en) * 1998-05-18 2000-01-25 U.S. Bioscience, Inc. Thermally stable trimetrexates and processes for producing the same
US6521212B1 (en) * 1999-03-18 2003-02-18 United Therapeutics Corporation Method for treating peripheral vascular disease by administering benzindene prostaglandins by inhalation
US6700025B2 (en) 2001-01-05 2004-03-02 United Therapeutics Corporation Process for stereoselective synthesis of prostacyclin derivatives
US6803386B2 (en) 2002-01-16 2004-10-12 United Therapeutics Corporation Prostacyclin derivative containing compositions and methods of using the same for the treatment of cancer
US6756117B1 (en) 2002-12-20 2004-06-29 The United States Of America As Represented By The United States Department Of Energy Photonic polymer-blend structures and method for making
ES2670872T3 (es) * 2003-05-22 2018-06-01 United Therapeutics Corporation Polimorfo de una sal de dietanolamina de treprostinil
KR20050024121A (ko) * 2003-09-04 2005-03-10 동아제약주식회사 7-카르복시메틸옥시-3',4',5-트리메톡시 플라본.일수화물, 이의 제조방법 및 용도
ES2331187T3 (es) 2003-12-16 2009-12-23 United Therapeutics Corporation Utilizacion de treprostinil para mejorar las funciones renales.
EP1696900B1 (en) * 2003-12-16 2010-07-14 United Therapeutics Corporation Use of treprostinil to treat ischemic lesions
CN101287457B (zh) * 2004-04-12 2011-11-16 联合治疗公司 Treprostinil用于治疗神经性糖尿病的足部溃疡的用途
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CA2654492C (en) 2006-05-15 2017-06-27 United Therapeutics Corporation Treprostinil administration using a metered dose inhaler
US20090036465A1 (en) * 2006-10-18 2009-02-05 United Therapeutics Corporation Combination therapy for pulmonary arterial hypertension
JP2010518122A (ja) 2007-02-09 2010-05-27 ユナイテッド セラピューティクス コーポレーション 間質性肺疾患および喘息のためのトレプロスチニル処置
WO2008118946A1 (en) 2007-03-27 2008-10-02 Atherogenics, Inc. Methods and compositions using certain phenolic derivatives for the treatment of diabetes
EP3287434A1 (en) * 2007-12-17 2018-02-28 United Therapeutics Corporation Process to prepare treprostinil, the active ingredient in remodulin ®

Also Published As

Publication number Publication date
ES2575565T3 (es) 2016-06-29
EP2300408A1 (en) 2011-03-30
WO2009137066A1 (en) 2009-11-12
JP2011519927A (ja) 2011-07-14
CN102015613B (zh) 2013-07-31
KR20110010753A (ko) 2011-02-07
EP3002274A8 (en) 2016-07-13
EP3002274A1 (en) 2016-04-06
US8350079B2 (en) 2013-01-08
JP6219016B2 (ja) 2017-10-25
CA2723540A1 (en) 2009-11-12
US20090281189A1 (en) 2009-11-12
EP2300408B1 (en) 2016-04-13
CN102015613A (zh) 2011-04-13

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