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
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Active
Application number
CA2723540A
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English (en)
French (fr)
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CA2723540A1 (en
Inventor
David A. Walsh
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United Therapeutics Corp
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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

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)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports 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)
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 (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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CN101265226B (zh) 2003-05-22 2013-04-24 联合治疗公司 化合物和释放前列环素类似物的方法
KR20160048222A (ko) 2007-12-17 2016-05-03 유나이티드 세러퓨틱스 코오포레이션 레모둘린?의 활성 성분인 트레프로스티닐의 개선된 제조 방법
EP3108888B1 (en) 2010-03-15 2020-02-12 United Therapeutics Corporation Treatment for pulmonary hypertension
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
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
EP2970091A4 (en) * 2013-03-14 2017-02-08 United Therapeutics Corporation Solid forms of treprostinil
US20140275616A1 (en) 2013-03-15 2014-09-18 United Therapeutics Corporation Salts of treprostinil
EP2978313B1 (en) 2013-03-25 2018-02-21 United Therapeutics Corporation Process of making prostacyclin compounds with linker thiol and pegylated forms
CN105407883A (zh) 2013-04-30 2016-03-16 联合治疗学有限公司 控释药物制剂
LT3060041T (lt) 2013-10-25 2021-03-25 Insmed Incorporated Prostaciklino junginiai
CN106573066A (zh) * 2014-06-13 2017-04-19 联合治疗学有限公司 曲前列环素制剂
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
ES2778274T3 (es) 2014-10-20 2020-08-10 United Therapeutics Corp Síntesis de productos intermedios para producir derivados de prostaciclina
JP6866043B2 (ja) 2014-11-18 2021-04-28 インスメッド インコーポレイテッド トレプロスチニルプロドラッグおよびトレプロスチニル誘導体プロドラッグの製造方法
US10898494B2 (en) 2016-05-05 2021-01-26 Liquidia Technologies, Inc. Dry powder treprostinil for the treatment of pulmonary hypertension
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
US20190290597A1 (en) 2016-12-05 2019-09-26 Corsair Pharma, Inc. Dermal and transdermal administration of treprostinil and salts thereof
AU2019344541B2 (en) 2018-09-18 2022-01-06 Eli Lilly And Company Erbumine salt of treprostinil
JP7455144B2 (ja) 2019-04-29 2024-03-25 インスメッド インコーポレイテッド トレプロスチニルプロドラッグの乾燥粉末組成物およびその使用方法
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
AU2021255621A1 (en) 2020-04-17 2022-10-20 United Therapeutics Corporation Treprostinil for use in the treatment of intersitial lung disease
JP7608480B2 (ja) 2020-06-09 2025-01-06 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フマリルジケトピペリジンプロドラッグ
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
AU2022229367A1 (en) 2021-03-03 2023-09-14 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)
US20230263807A1 (en) 2022-02-08 2023-08-24 United Therapeutics Corporation Treprostinil iloprost combination therapy
KR20250002687A (ko) 2022-04-29 2025-01-07 자오커 파마슈티컬 (광저우) 컴퍼니., 리미티드 트레프로스티닐 소프트 미스트 흡입제
AU2024208919A1 (en) 2023-01-19 2025-07-17 United Therapeutics Corporation Treprostinil analogs

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Also Published As

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

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