US20180153847A1 - Treprostinil prodrugs - Google Patents

Treprostinil prodrugs Download PDF

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Publication number
US20180153847A1
US20180153847A1 US15/716,007 US201715716007A US2018153847A1 US 20180153847 A1 US20180153847 A1 US 20180153847A1 US 201715716007 A US201715716007 A US 201715716007A US 2018153847 A1 US2018153847 A1 US 2018153847A1
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US
United States
Prior art keywords
treprostinil
prodrug
group
canceled
alkyl
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.)
Abandoned
Application number
US15/716,007
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English (en)
Inventor
Ken Phares
Hitesh Batra
Liang Guo
Adam Marc SILVERSTEIN
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
Original Assignee
United Therapeutics Corp
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by United Therapeutics Corp filed Critical United Therapeutics Corp
Priority to US15/716,007 priority Critical patent/US20180153847A1/en
Assigned to UNITED THERAPEUTICS CORPORATION reassignment UNITED THERAPEUTICS CORPORATION ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: BATRA, HITESH, GUO, LIANG, PHARES, KEN, SILVERSTEIN, ADAM MARC
Publication of US20180153847A1 publication Critical patent/US20180153847A1/en
Priority to US17/140,705 priority patent/US11672775B2/en
Priority to US18/141,170 priority patent/US20230255922A1/en
Abandoned legal-status Critical Current

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    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • 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
    • 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
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/221—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/222—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/265—Esters, e.g. nitroglycerine, selenocyanates of carbonic, thiocarbonic, or thiocarboxylic acids, e.g. thioacetic acid, xanthogenic acid, trithiocarbonic acid
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0021—Intradermal administration, e.g. through microneedle arrays, needleless injectors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
US15/716,007 2016-09-26 2017-09-26 Treprostinil prodrugs Abandoned US20180153847A1 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
US15/716,007 US20180153847A1 (en) 2016-09-26 2017-09-26 Treprostinil prodrugs
US17/140,705 US11672775B2 (en) 2016-09-26 2021-01-04 Treprostinil prodrugs
US18/141,170 US20230255922A1 (en) 2016-09-26 2023-04-28 Treprostinil prodrugs

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662399737P 2016-09-26 2016-09-26
US15/716,007 US20180153847A1 (en) 2016-09-26 2017-09-26 Treprostinil prodrugs

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US17/140,705 Continuation US11672775B2 (en) 2016-09-26 2021-01-04 Treprostinil prodrugs

Publications (1)

Publication Number Publication Date
US20180153847A1 true US20180153847A1 (en) 2018-06-07

Family

ID=60120132

Family Applications (3)

Application Number Title Priority Date Filing Date
US15/716,007 Abandoned US20180153847A1 (en) 2016-09-26 2017-09-26 Treprostinil prodrugs
US17/140,705 Active 2038-02-20 US11672775B2 (en) 2016-09-26 2021-01-04 Treprostinil prodrugs
US18/141,170 Pending US20230255922A1 (en) 2016-09-26 2023-04-28 Treprostinil prodrugs

Family Applications After (2)

Application Number Title Priority Date Filing Date
US17/140,705 Active 2038-02-20 US11672775B2 (en) 2016-09-26 2021-01-04 Treprostinil prodrugs
US18/141,170 Pending US20230255922A1 (en) 2016-09-26 2023-04-28 Treprostinil prodrugs

Country Status (9)

Country Link
US (3) US20180153847A1 (fr)
EP (1) EP3515430A1 (fr)
JP (2) JP7220650B2 (fr)
KR (1) KR102541885B1 (fr)
CN (1) CN110678174A (fr)
AU (1) AU2017330099B2 (fr)
CA (1) CA3038276A1 (fr)
IL (1) IL265588A (fr)
WO (1) WO2018058124A1 (fr)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020223237A1 (fr) * 2019-04-29 2020-11-05 Insmed Incorporated Compositions de poudre sèche de promédicaments de tréprostinil et méthodes d'utilisation de celles-ci
WO2021041320A1 (fr) 2019-08-23 2021-03-04 United Therapeutics Corporation Promédicaments de tréprostinil
US10995055B2 (en) 2013-10-25 2021-05-04 Insmed Incorporated Prostacyclin compounds, compositions and methods of use thereof
US11148997B2 (en) 2014-11-18 2021-10-19 Insmed Incorporated Methods of manufacturing treprostinil and treprostinil derivative prodrugs
WO2021211916A1 (fr) 2020-04-17 2021-10-21 United Therapeutics Corporation Tréprostinil destiné à être utilisé dans le traitement d'une pneumopathie interstitielle
WO2022132655A1 (fr) 2020-12-14 2022-06-23 United Therapeutics Corporation Méthodes de traitement d'une maladie à l'aide de promédicaments tréprostinil
WO2022187352A1 (fr) 2021-03-03 2022-09-09 United Therapeutics Corporation Composition de poudre sèche de treprostinil et son promédicament et comprenant en outre de l'(e)-3,6-bis[4-(n-carbonyl-2-propényl)amidobutyl]-2,5-dicétopipérazine (fdkp)
WO2023154705A1 (fr) 2022-02-08 2023-08-17 United Therapeutics Corporation Polythérapie à base de tréprostinil iloprost
US11793780B2 (en) 2020-06-09 2023-10-24 United Therapeutics Corporation Prodrugs of treprosiinil

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022194195A1 (fr) * 2021-03-16 2022-09-22 江苏恒瑞医药股份有限公司 Dérivé de tréprostinil et son utilisation
CN116444377A (zh) * 2022-01-07 2023-07-18 广州楷石医药有限公司 一种氧化氮供体型曲前列尼尔类衍生物及其药物组合物和用途
CN115894240A (zh) * 2022-10-14 2023-04-04 广州楷石医药有限公司 曲前列尼尔的前体药物及其应用

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US20150166503A1 (en) * 2013-01-11 2015-06-18 Corsair Pharma, Inc. Treprostinil derivative compounds and methods of using same

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Cited By (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11795135B2 (en) 2013-10-25 2023-10-24 Insmed Incorporated Prostacyclin compounds, compositions and methods of use thereof
US10995055B2 (en) 2013-10-25 2021-05-04 Insmed Incorporated Prostacyclin compounds, compositions and methods of use thereof
US11148997B2 (en) 2014-11-18 2021-10-19 Insmed Incorporated Methods of manufacturing treprostinil and treprostinil derivative prodrugs
US11458098B2 (en) 2019-04-29 2022-10-04 Insmed Incorporated Dry powder compositions of treprostinil prodrugs and methods of use thereof
WO2020223237A1 (fr) * 2019-04-29 2020-11-05 Insmed Incorporated Compositions de poudre sèche de promédicaments de tréprostinil et méthodes d'utilisation de celles-ci
US11759425B2 (en) 2019-04-29 2023-09-19 Insmed Incorporated Dry powder compositions of treprostinil prodrugs and methods of use thereof
US11634443B2 (en) 2019-08-23 2023-04-25 United Therapeutics Corporation Treprostinil prodrugs
WO2021041320A1 (fr) 2019-08-23 2021-03-04 United Therapeutics Corporation Promédicaments de tréprostinil
WO2021211916A1 (fr) 2020-04-17 2021-10-21 United Therapeutics Corporation Tréprostinil destiné à être utilisé dans le traitement d'une pneumopathie interstitielle
US20210330621A1 (en) 2020-04-17 2021-10-28 United Therapeutics Corporation Treatment for interstitial lung disease
US11826327B2 (en) 2020-04-17 2023-11-28 United Therapeutics Corporation Treatment for interstitial lung disease
US11793780B2 (en) 2020-06-09 2023-10-24 United Therapeutics Corporation Prodrugs of treprosiinil
WO2022132655A1 (fr) 2020-12-14 2022-06-23 United Therapeutics Corporation Méthodes de traitement d'une maladie à l'aide de promédicaments tréprostinil
US11826328B2 (en) 2020-12-14 2023-11-28 United Therapeutics Corporation Stable treprostinil prodrugs
WO2022187352A1 (fr) 2021-03-03 2022-09-09 United Therapeutics Corporation Composition de poudre sèche de treprostinil et son promédicament et comprenant en outre de l'(e)-3,6-bis[4-(n-carbonyl-2-propényl)amidobutyl]-2,5-dicétopipérazine (fdkp)
WO2023154705A1 (fr) 2022-02-08 2023-08-17 United Therapeutics Corporation Polythérapie à base de tréprostinil iloprost

Also Published As

Publication number Publication date
AU2017330099A1 (en) 2019-04-18
CA3038276A1 (fr) 2018-03-29
KR20190092372A (ko) 2019-08-07
JP7220650B2 (ja) 2023-02-10
JP2019536741A (ja) 2019-12-19
KR102541885B1 (ko) 2023-06-12
IL265588A (en) 2019-05-30
WO2018058124A1 (fr) 2018-03-29
AU2017330099B2 (en) 2023-08-10
US20230255922A1 (en) 2023-08-17
JP2022188082A (ja) 2022-12-20
US11672775B2 (en) 2023-06-13
US20210121433A1 (en) 2021-04-29
CN110678174A (zh) 2020-01-10
EP3515430A1 (fr) 2019-07-31

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