JP7608480B2 - 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 - Google Patents
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 Download PDFInfo
- Publication number
- JP7608480B2 JP7608480B2 JP2022574179A JP2022574179A JP7608480B2 JP 7608480 B2 JP7608480 B2 JP 7608480B2 JP 2022574179 A JP2022574179 A JP 2022574179A JP 2022574179 A JP2022574179 A JP 2022574179A JP 7608480 B2 JP7608480 B2 JP 7608480B2
- Authority
- JP
- Japan
- Prior art keywords
- treprostinil
- compound
- fdkp
- formula
- protecting group
- 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
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
- C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
-
- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
- A61K31/5575—Eicosanoids, e.g. leukotrienes or prostaglandins having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024221661A JP2025041731A (ja) | 2020-06-09 | 2024-12-18 | 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 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063036561P | 2020-06-09 | 2020-06-09 | |
| US63/036,561 | 2020-06-09 | ||
| PCT/US2021/036335 WO2021252446A1 (en) | 2020-06-09 | 2021-06-08 | Fumaryl diketopiperidine prodrugs of treprostinil |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024221661A Division JP2025041731A (ja) | 2020-06-09 | 2024-12-18 | 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023529828A JP2023529828A (ja) | 2023-07-12 |
| JP2023529828A5 JP2023529828A5 (enExample) | 2024-06-17 |
| JP7608480B2 true JP7608480B2 (ja) | 2025-01-06 |
Family
ID=76731024
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022574179A Active JP7608480B2 (ja) | 2020-06-09 | 2021-06-08 | 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 |
| JP2024221661A Pending JP2025041731A (ja) | 2020-06-09 | 2024-12-18 | 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 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024221661A Pending JP2025041731A (ja) | 2020-06-09 | 2024-12-18 | 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 |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US11793780B2 (enExample) |
| EP (1) | EP4161909A1 (enExample) |
| JP (2) | JP7608480B2 (enExample) |
| KR (2) | KR20250057075A (enExample) |
| CN (1) | CN116113415A (enExample) |
| AU (2) | AU2021289336B2 (enExample) |
| CA (1) | CA3180230A1 (enExample) |
| IL (1) | IL298591A (enExample) |
| WO (1) | WO2021252446A1 (enExample) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2014527050A (ja) | 2011-08-12 | 2014-10-09 | アセンディス ファーマ エー/エス | 担体連結しているトレプロスチニルプロドラッグ |
| JP2016510323A (ja) | 2013-01-11 | 2016-04-07 | コルセア ファーマ インコーポレイテッド | トレプロスチニルのプロドラッグ |
| JP2016522839A (ja) | 2013-03-25 | 2016-08-04 | ユナイテッド セラピューティクス コーポレイション | チオールリンカーを持つ、ペグ化型のプロスタサイクリン化合物の製造方法 |
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| US2485614A (en) | 1946-08-29 | 1949-10-25 | Chicago Bridge & Iron Co | Stabilizing and guide apparatus for lifter roofs |
| US3037116A (en) | 1957-07-26 | 1962-05-29 | Weber Georges | Apparatus for irradiating liquids |
| US3035516A (en) | 1958-08-18 | 1962-05-22 | Lee Brothers Company | Stencil device |
| US3646509A (en) | 1969-08-08 | 1972-02-29 | Texas Instruments Inc | Method for field stacking seismic data and system using write after read bulk data storage |
| US4306075A (en) | 1980-03-28 | 1981-12-15 | The Upjohn Company | Composition and process |
| US4547016A (en) | 1984-08-13 | 1985-10-15 | Eeco Incorporated | Quick release mounting |
| GB8814438D0 (en) | 1988-06-17 | 1988-07-20 | Wellcome Found | Compounds for use in medicine |
| IT1231076B (it) | 1989-09-28 | 1991-11-12 | Pirelli Cavi Spa | Procedimento per la realizzazione di gruppo di connessione separabile per fibre ottiche riunite a nastro e gruppo di connessione con esso realizzato. |
| GB9011588D0 (en) | 1990-05-24 | 1990-07-11 | Wellcome Found | Prostaglandin analogues for use in medicine |
| US6441245B1 (en) | 1997-10-24 | 2002-08-27 | United Therapeutics Corporation | Process for stereoselective synthesis of prostacyclin derivatives |
| KR100638684B1 (ko) | 1997-11-14 | 2006-10-27 | 유나이티드 세러퓨틱스 코오포레이션 | 말초 혈관 질환의 치료를 위한 9-데옥시-2',9-알파-메타노-3-옥사-4,5,6-트리노르-3,7-(1',3'-인터페닐렌)-13,14-디하이드로-프로스타글란딘 에프1의 용도 |
| US6521212B1 (en) | 1999-03-18 | 2003-02-18 | United Therapeutics Corporation | Method for treating peripheral vascular disease by administering benzindene prostaglandins by inhalation |
| EP1164846A1 (en) | 1999-03-31 | 2002-01-02 | United Therapeutics Corporation | Prostaglandin compounds, compositions and methods of treating peripheral vascular disease and pulmonary hypertension |
| 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 |
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| KR20110010753A (ko) | 2008-05-08 | 2011-02-07 | 유나이티드 세러퓨틱스 코오포레이션 | 트레프로스티닐 일수화물 |
| EP2427054A4 (en) | 2009-05-07 | 2014-01-15 | United Therapeutics Corp | SOLID COMPOSITIONS BASED ON PROSTACYCLINE ANALOGS |
| US20120184622A1 (en) | 2009-08-07 | 2012-07-19 | Scipharm Sarl | Composition for the treatment of cystic fibrosis |
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| 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 |
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| CA2710725C (en) | 2010-07-22 | 2017-08-01 | Alphora Research Inc. | Protected aldehydes for use as intermediates in chemical syntheses, and processes for their preparation |
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-
2021
- 2021-06-08 US US17/342,377 patent/US11793780B2/en active Active
- 2021-06-08 AU AU2021289336A patent/AU2021289336B2/en active Active
- 2021-06-08 CA CA3180230A patent/CA3180230A1/en active Pending
- 2021-06-08 KR KR1020257011829A patent/KR20250057075A/ko active Pending
- 2021-06-08 EP EP21736820.8A patent/EP4161909A1/en active Pending
- 2021-06-08 WO PCT/US2021/036335 patent/WO2021252446A1/en not_active Ceased
- 2021-06-08 JP JP2022574179A patent/JP7608480B2/ja active Active
- 2021-06-08 KR KR1020237000402A patent/KR102796323B1/ko active Active
- 2021-06-08 IL IL298591A patent/IL298591A/en unknown
- 2021-06-08 CN CN202180055830.2A patent/CN116113415A/zh active Pending
-
2023
- 2023-10-17 US US18/488,342 patent/US12357599B2/en active Active
-
2024
- 2024-12-18 JP JP2024221661A patent/JP2025041731A/ja active Pending
-
2025
- 2025-06-17 US US19/240,421 patent/US20250302786A1/en active Pending
- 2025-11-27 AU AU2025271417A patent/AU2025271417A1/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2014527050A (ja) | 2011-08-12 | 2014-10-09 | アセンディス ファーマ エー/エス | 担体連結しているトレプロスチニルプロドラッグ |
| JP2016510323A (ja) | 2013-01-11 | 2016-04-07 | コルセア ファーマ インコーポレイテッド | トレプロスチニルのプロドラッグ |
| JP2016522839A (ja) | 2013-03-25 | 2016-08-04 | ユナイテッド セラピューティクス コーポレイション | チオールリンカーを持つ、ペグ化型のプロスタサイクリン化合物の製造方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2025041731A (ja) | 2025-03-26 |
| US20250302786A1 (en) | 2025-10-02 |
| CN116113415A (zh) | 2023-05-12 |
| AU2021289336A1 (en) | 2023-01-05 |
| WO2021252446A1 (en) | 2021-12-16 |
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