CN102015613B - 曲前列素一水合物 - Google Patents
曲前列素一水合物 Download PDFInfo
- 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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- Prior art keywords
- qianlie
- monohydrate
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- anhydrous
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Classifications
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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
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)
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 |
Family
ID=41037724
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 (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=) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005058329A1 (en) * | 2003-12-16 | 2005-06-30 | United Therapeutics Corporation | Use of treprostinil to improve kidney functions |
| WO2005099680A2 (en) * | 2004-04-12 | 2005-10-27 | United Therapeutics, Inc. | Use of treprostinil to treat neuropathic diabetic foot ulcers |
| CN1822826A (zh) * | 2003-05-22 | 2006-08-23 | 联合治疗公司 | 化合物和释放前列环素类似物的方法 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| GB9300763D0 (en) * | 1993-01-15 | 1993-03-03 | Leo Pharm Prod Ltd | Chemical compound |
| 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 |
| KR20050024121A (ko) * | 2003-09-04 | 2005-03-10 | 동아제약주식회사 | 7-카르복시메틸옥시-3',4',5-트리메톡시 플라본.일수화물, 이의 제조방법 및 용도 |
| CN1917866B (zh) | 2003-12-16 | 2010-12-15 | 联合治疗公司 | 曲前列环素或它的衍生物,或其药学上可接受的盐在制备治疗和预防缺血性损害的药物中的用途 |
| US8747897B2 (en) * | 2006-04-27 | 2014-06-10 | Supernus Pharmaceuticals, Inc. | Osmotic drug delivery system |
| CN101495122B (zh) | 2006-05-15 | 2011-10-05 | 联合治疗公司 | 使用定量吸入器给予曲前列尼 |
| US20090036465A1 (en) | 2006-10-18 | 2009-02-05 | United Therapeutics Corporation | Combination therapy for pulmonary arterial hypertension |
| CA2678258A1 (en) | 2007-02-09 | 2008-08-14 | United Therapeutics Corporation | Treprostinil treatment for interstitial lung disease and asthma |
| WO2008118946A1 (en) | 2007-03-27 | 2008-10-02 | Atherogenics, Inc. | Methods and compositions using certain phenolic derivatives for the treatment of diabetes |
| KR20160048222A (ko) * | 2007-12-17 | 2016-05-03 | 유나이티드 세러퓨틱스 코오포레이션 | 레모둘린?의 활성 성분인 트레프로스티닐의 개선된 제조 방법 |
-
2009
- 2009-05-07 US US12/437,054 patent/US8350079B2/en active Active
- 2009-05-07 JP JP2011508505A patent/JP6219016B2/ja active Active
- 2009-05-07 EP EP09743053.2A patent/EP2300408B1/en active Active
- 2009-05-07 CA CA2723540A patent/CA2723540C/en active Active
- 2009-05-07 CN CN2009801161262A patent/CN102015613B/zh active Active
- 2009-05-07 WO PCT/US2009/002818 patent/WO2009137066A1/en not_active Ceased
- 2009-05-07 KR KR1020107027068A patent/KR20110010753A/ko not_active Ceased
- 2009-05-07 EP EP15190454.7A patent/EP3002274A1/en not_active Withdrawn
- 2009-05-07 ES ES09743053.2T patent/ES2575565T3/es active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1822826A (zh) * | 2003-05-22 | 2006-08-23 | 联合治疗公司 | 化合物和释放前列环素类似物的方法 |
| WO2005058329A1 (en) * | 2003-12-16 | 2005-06-30 | United Therapeutics Corporation | Use of treprostinil to improve kidney functions |
| WO2005099680A2 (en) * | 2004-04-12 | 2005-10-27 | United Therapeutics, Inc. | Use of treprostinil to treat neuropathic diabetic foot ulcers |
Non-Patent Citations (1)
| Title |
|---|
| The Intramolecular Asymmetric Pauson-Khand Cyclization as a Novel and General tereoselective Route to Benzindene Prostacyclins: Synthesis of UT-15 (Treprostinil);Robert M. Moriarty, et al.;《The Journal of Organic Chemistry》;20040219;第69卷(第6期);第1890-1902页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| US8350079B2 (en) | 2013-01-08 |
| 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 |
| CA2723540C (en) | 2016-01-05 |
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