IL305157B2 - Treprostinil Derivatives and Compositions and Uses Thereof - Google Patents

Treprostinil Derivatives and Compositions and Uses Thereof

Info

Publication number
IL305157B2
IL305157B2 IL305157A IL30515723A IL305157B2 IL 305157 B2 IL305157 B2 IL 305157B2 IL 305157 A IL305157 A IL 305157A IL 30515723 A IL30515723 A IL 30515723A IL 305157 B2 IL305157 B2 IL 305157B2
Authority
IL
Israel
Prior art keywords
compound
hydrogen
co2h
occurrence independently
cycloalkyl
Prior art date
Application number
IL305157A
Other languages
English (en)
Hebrew (he)
Other versions
IL305157A (en
IL305157B1 (en
Original Assignee
Corsair Pharma Inc
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
Priority claimed from US14/742,544 external-priority patent/US9394227B1/en
Application filed by Corsair Pharma Inc filed Critical Corsair Pharma Inc
Publication of IL305157A publication Critical patent/IL305157A/en
Publication of IL305157B1 publication Critical patent/IL305157B1/en
Publication of IL305157B2 publication Critical patent/IL305157B2/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/73Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
    • C07C69/734Ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/222Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7092Transdermal patches having multiple drug layers or reservoirs, e.g. for obtaining a specific release pattern, or for combining different drugs
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • 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
    • A61P37/04Immunostimulants
    • 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
    • C07C53/00Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/132Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing rings
    • C07C53/136Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing rings containing condensed ring systems
    • 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
    • C07C59/01Saturated compounds having only one carboxyl group and containing hydroxy or O-metal groups
    • C07C59/11Saturated compounds having only one carboxyl group and containing hydroxy or O-metal groups containing rings
    • 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
    • C07C59/125Saturated compounds having only one carboxyl group and containing ether groups, groups, groups, or groups
    • C07C59/13Saturated compounds having only one carboxyl group and containing ether groups, groups, groups, or groups containing rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/02Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
    • C07C69/22Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety
    • C07C69/28Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety esterified with dihydroxylic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/67Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids
    • C07C69/675Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids of saturated hydroxy-carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/67Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids
    • C07C69/675Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids of saturated hydroxy-carboxylic acids
    • C07C69/68Lactic acid esters
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/67Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids
    • C07C69/708Ethers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/67Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids
    • C07C69/708Ethers
    • C07C69/712Ethers the hydroxy group of the ester being etherified with a hydroxy compound having the hydroxy group bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/74Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/74Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C07C69/75Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring of acids with a six-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/74Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C07C69/757Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/96Esters of carbonic or haloformic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D305/00Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
    • C07D305/02Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D305/04Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D305/08Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/26Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D307/30Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/02Systems containing only non-condensed rings with a three-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/04Systems containing only non-condensed rings with a four-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/06Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14The ring being saturated
    • 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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (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)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Furan Compounds (AREA)
  • Epoxy Compounds (AREA)
  • Pyrane Compounds (AREA)
IL305157A 2015-06-17 2016-06-14 Treprostinil Derivatives and Compositions and Uses Thereof IL305157B2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201514742579A 2015-06-17 2015-06-17
US14/742,544 US9394227B1 (en) 2015-06-17 2015-06-17 Treprostinil derivatives and compositions and uses thereof
US14/829,180 US9643911B2 (en) 2015-06-17 2015-08-18 Treprostinil derivatives and compositions and uses thereof
PCT/US2016/037383 WO2016205202A1 (en) 2015-06-17 2016-06-14 Treprostinil derivatives and compositions and uses thereof

Publications (3)

Publication Number Publication Date
IL305157A IL305157A (en) 2023-10-01
IL305157B1 IL305157B1 (en) 2024-07-01
IL305157B2 true IL305157B2 (en) 2024-11-01

Family

ID=56204034

Family Applications (4)

Application Number Title Priority Date Filing Date
IL305157A IL305157B2 (en) 2015-06-17 2016-06-14 Treprostinil Derivatives and Compositions and Uses Thereof
IL313291A IL313291A (en) 2015-06-17 2016-06-14 Terpanstinil derivatives and preparations containing them and their uses
IL289276A IL289276B2 (en) 2015-06-17 2016-06-14 Terpanstinil derivatives and preparations containing them and their uses
IL256260A IL256260B (en) 2015-06-17 2017-12-11 Treprostinil derivatives and compositions and uses thereof

Family Applications After (3)

Application Number Title Priority Date Filing Date
IL313291A IL313291A (en) 2015-06-17 2016-06-14 Terpanstinil derivatives and preparations containing them and their uses
IL289276A IL289276B2 (en) 2015-06-17 2016-06-14 Terpanstinil derivatives and preparations containing them and their uses
IL256260A IL256260B (en) 2015-06-17 2017-12-11 Treprostinil derivatives and compositions and uses thereof

Country Status (10)

Country Link
US (11) US9643911B2 (OSRAM)
EP (3) EP3310769B1 (OSRAM)
JP (3) JP7013245B2 (OSRAM)
KR (2) KR102711773B1 (OSRAM)
CN (1) CN108349926A (OSRAM)
CA (1) CA2989317A1 (OSRAM)
ES (2) ES2859749T3 (OSRAM)
HK (1) HK1258913A1 (OSRAM)
IL (4) IL305157B2 (OSRAM)
WO (1) WO2016205202A1 (OSRAM)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9505737B2 (en) 2013-01-11 2016-11-29 Corsair Pharma, Inc. Treprostinil derivative compounds and methods of using same
JP6542128B2 (ja) 2013-01-11 2019-07-10 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
US9394227B1 (en) 2015-06-17 2016-07-19 Corsair Pharma, Inc. Treprostinil derivatives and compositions and uses thereof
US9643911B2 (en) * 2015-06-17 2017-05-09 Corsair Pharma, Inc. Treprostinil derivatives and compositions and uses thereof
IL310250B2 (en) 2016-05-05 2025-09-01 Liquidia Tech Inc Terpostinil in dry powder form for the treatment of pulmonary hypertension
EP3515430A1 (en) 2016-09-26 2019-07-31 United Therapeutics Corporation Treprostinil prodrugs
US20190099383A1 (en) * 2017-09-30 2019-04-04 Samos Pharmaceuticals, Inc. Transdermal Delivery of Selexipag Metabolite
EP3498283A1 (en) * 2017-12-14 2019-06-19 Ipsol AG Glycosidic derivatives of treprostinil
EP4017588A1 (en) 2019-08-23 2022-06-29 United Therapeutics Corporation Treprostinil prodrugs
CN115916212A (zh) 2020-04-17 2023-04-04 联合治疗公司 曲前列尼尔用于治疗间质性肺病
CN117062605A (zh) 2020-12-14 2023-11-14 联合治疗公司 使用曲前列环素前药治疗疾病的方法
CN117479946A (zh) 2021-03-03 2024-01-30 联合治疗公司 含曲前列环素及其前药并还包含(e)-3,6-双[4-(n-羰基-2-丙烯基)酰胺丁基]-2,5-二酮哌嗪(fdkp)的干粉组合物
CN117015524A (zh) * 2021-03-16 2023-11-07 江苏恒瑞医药股份有限公司 一种曲前列环素衍生物及其用途
WO2023154705A1 (en) 2022-02-08 2023-08-17 United Therapeutics Corporation Treprostinil iloprost combination therapy
CN115894240B (zh) * 2022-10-14 2025-02-14 广州楷石医药有限公司 曲前列尼尔的前体药物及其应用
CN115448839B (zh) * 2022-10-14 2025-02-14 广州楷石医药有限公司 一种曲前列尼尔的前体药物
EP4652151A1 (en) * 2023-01-19 2025-11-26 United Therapeutics Corporation Treprostinil analogs
CN117800845A (zh) * 2023-03-28 2024-04-02 广州楷石医药有限公司 一种羟基取代曲前列尼尔衍生物、合成方法及其应用
TW202502721A (zh) * 2023-07-03 2025-01-16 香港商長風藥業(香港)有限公司 一種曲前列環素衍生物、其製備方法及應用

Family Cites Families (100)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3598122A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
US4144317A (en) 1975-05-30 1979-03-13 Alza Corporation Device consisting of copolymer having acetoxy groups for delivering drugs
US4262003A (en) 1975-12-08 1981-04-14 Alza Corporation Method and therapeutic system for administering scopolamine transdermally
US4201211A (en) 1977-07-12 1980-05-06 Alza Corporation Therapeutic system for administering clonidine transdermally
US4338457A (en) 1980-02-28 1982-07-06 The Upjohn Company Composition and process
US4525586A (en) 1980-02-28 1985-06-25 The Upjohn Company Composition and process
US4306075A (en) 1980-03-28 1981-12-15 The Upjohn Company Composition and process
US4420632A (en) 1980-04-15 1983-12-13 The Upjohn Company Composition and process
US4306076A (en) 1980-04-23 1981-12-15 The Upjohn Company Inter-phenylene CBA compounds
US4349689A (en) 1980-12-22 1982-09-14 The Upjohn Company Methano carbacyclin analogs
US4379454A (en) 1981-02-17 1983-04-12 Alza Corporation Dosage for coadministering drug and percutaneous absorption enhancer
DE3333240A1 (de) 1983-09-12 1985-03-28 Schering AG, 1000 Berlin und 4709 Bergkamen Mittel zur transdermalen applikation von arzneimittelwirkstoffen
US4668814A (en) 1984-03-08 1987-05-26 The Upjohn Company Interphenylene carbacyclin derivatives
US4683330A (en) 1984-03-08 1987-07-28 The Upjohn Company Interphenylene carbacyclin derivatives
GB8814438D0 (en) 1988-06-17 1988-07-20 Wellcome Found Compounds for use in medicine
GB8824187D0 (en) 1988-10-14 1988-11-23 Wellcome Found Compounds for use in medicine
US5088977A (en) 1988-12-21 1992-02-18 Drug Delivery Systems Inc. Electrical transdermal drug applicator with counteractor and method of drug delivery
CA2056039A1 (en) 1991-01-22 1992-07-23 Philip L. Fuchs Carbacyclin analogs
US5234690A (en) 1991-08-23 1993-08-10 Cygnus Therapeutic Systems Transdermal drug delivery device using an unfilled microporous membrane to achieve delayed onset
US5869505A (en) 1993-02-02 1999-02-09 Keenan; Robert M. Nicotine metabolites and nicotine dependence
US5853751A (en) 1993-06-23 1998-12-29 Masiz; John J. Molecular transdermal transport system
US5797898A (en) 1996-07-02 1998-08-25 Massachusetts Institute Of Technology Microchip drug delivery devices
IN184589B (OSRAM) 1996-10-16 2000-09-09 Alza Corp
CN1354622A (zh) 1999-03-31 2002-06-19 联合治疗公司 前列腺素类化合物、组合物和治疗外周血管疾病和肺动脉高压的方法
WO2001052823A2 (en) 2000-01-20 2001-07-26 Noven Pharmaceuticals, Inc. Compositions to effect the release profile in the transdermal administration of drugs
US6242482B1 (en) 2000-06-05 2001-06-05 United Therapeutics Corporation Prostaglandin compounds and derivatives thereof, compositions containing the same and method of using the same for the treatment of congestive heart failure
US6635274B1 (en) 2000-10-27 2003-10-21 Biochemics, Inc. Solution-based transdermal drug delivery system
US6700025B2 (en) 2001-01-05 2004-03-02 United Therapeutics Corporation Process for stereoselective synthesis of prostacyclin derivatives
US20030108512A1 (en) 2001-12-10 2003-06-12 Robert Shorr Modified prostaglandin compounds and analogs thereof, compositions containing the same useful for the treatment of cancer
US8246979B2 (en) 2002-07-30 2012-08-21 Ucb Pharma Gmbh Transdermal delivery system for the administration of rotigotine
CA2959852A1 (en) 2003-05-22 2005-01-27 United Therapeutics Corporation Compounds and methods for delivery of prostacyclin analogs
CA2530407A1 (en) * 2003-07-23 2005-02-03 The Regents Of The University Of California Penetration enhancer combinations for transdermal delivery
US7375139B2 (en) 2003-08-18 2008-05-20 Aldred Katherine M Transdermal method and apparatus
JP2005120069A (ja) 2003-10-13 2005-05-12 Anges Mg Inc 炎症性疾患治療薬
JP4906514B2 (ja) 2003-12-16 2012-03-28 ユナイテッド セラピューティクス コーポレイション 腎臓機能改善のためのトレプロスチニルの用途
ATE473736T1 (de) 2003-12-16 2010-07-15 United Therapeutics Corp Verwendung von treprostinil zur behandlung von ischämischen läsionen
DE602005020269D1 (de) 2004-04-12 2010-05-12 United Therapeutics Corp Verwendung von treprostinil zur behandlung von neuropathischen diabetischen fussgeschwüren
WO2006015299A2 (en) 2004-07-30 2006-02-09 Microchips, Inc. Multi-reservoir device for transdermal drug delivery and sensing
WO2006044206A2 (en) 2004-10-08 2006-04-27 Noven Pharmaceuticals, Inc. Transdermal drug delivery device including an occlusive backing
CN101212975A (zh) 2005-06-03 2008-07-02 艾克若克斯Dds有限公司 用于透皮给药的方法和组合物
EA200801369A1 (ru) 2005-12-20 2009-02-27 ТЕЙКОКУ ФАРМА ЮЭсЭй, ИНК. Способы трансдермального введения агониста рецептора индолсеротонина и трансдермальные лекарственные формы для применения этого способа
PT1988910T (pt) 2006-02-28 2018-02-07 Kodiak Sciences Inc Acriloiloxietilfosforilcolina contendo conjugados de polímeros e sua preparação
US8747897B2 (en) 2006-04-27 2014-06-10 Supernus Pharmaceuticals, Inc. Osmotic drug delivery system
US20080200449A1 (en) 2006-05-15 2008-08-21 United Therapeutics Corporation Treprostinil administration using a metered dose inhaler
WO2008002929A2 (en) 2006-06-26 2008-01-03 Inverseon, Inc. Heterologous cross-sensitization for improved agonist activity
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
BRPI0814105A2 (pt) 2007-07-11 2015-02-03 Lexicon Pharmaceuticals Inc Métodos e composições para o tratamento de hipertensão pulmonar e doenças e distúrbios relacionados
KR101898407B1 (ko) 2007-12-17 2018-09-12 유나이티드 세러퓨틱스 코오포레이션 레모둘린®의 활성 성분인 트레프로스티닐의 개선된 제조 방법
WO2009152160A1 (en) 2008-06-10 2009-12-17 Gilead Sciences, Inc. Inhaled carbaprostacyclin and prostacyclin prodrugs for the treatment of pulmonary arterial hypertension
WO2009158010A1 (en) 2008-06-27 2009-12-30 Concert Pharmaceuticals, Inc. Prostacyclin analogs
PT2315587T (pt) 2008-08-13 2018-01-31 Actelion Pharmaceuticals Ltd Produto que contém macitentan, composição farmacêutica que o contém e uso de macitentan
CN106075455A (zh) 2008-12-30 2016-11-09 丹麦国家医院 鉴定发展成器官功能衰竭的风险提高的危重患者的方法及用于其治疗的化合物
JP5649645B2 (ja) 2009-05-07 2015-01-07 ユナイテッド セラピューティクス コーポレイション プロスタサイクリンアナログの固形製剤
WO2011005505A2 (en) 2009-06-22 2011-01-13 Johnson Matthey Public Limited Company Method for the purification of prostaglandins
PT2461812E (pt) 2009-08-07 2014-04-07 Scipharm S Rl Composição para o tratamento da fibrose cística
US9327105B2 (en) * 2010-03-26 2016-05-03 Itrace Biomedical Inc. Active transdermal drug delivery system and the method thereof
EP2552967A4 (en) 2010-04-02 2014-10-08 Amunix Operating Inc BINDING FUSION PROTEINS, BINDING FUSION PROTEIN MEDICINAL CONJUGATES, XTEN MEDICAMENT CONJUGATES, AND METHOD FOR THEIR PREPARATION AND USE
WO2011123830A2 (en) 2010-04-02 2011-10-06 Amunix Operating Inc. Alpha 1-antitrypsin compositions and methods of making and using same
WO2011134478A2 (en) 2010-04-29 2011-11-03 Thrombologic Aps Methods of treatment of patients at increased risk of development of ischemic events and compounds hereof
CA3029711A1 (en) 2010-06-03 2011-12-08 United Therapeutics Corporation Treprostinil production
WO2012006273A1 (en) 2010-07-09 2012-01-12 United Therapeutics Corporation Combination therapies with cox-2 inhibitors and treprostinil
CA2710726C (en) 2010-07-22 2016-02-23 Alphora Research Inc. Synthesis of treprostinil and intermediates useful therein
CA2726599C (en) 2010-12-30 2017-07-25 Alphora Research Inc. Process for treprostinil salt preparation
EP2663313B1 (en) 2011-01-13 2018-08-08 SciPharm S.à r.l. Method for enhancing engraftment of haematopoetic stem cells
BR112013019335B1 (pt) 2011-02-07 2022-05-31 Scipharm Sàrl Nova composição, método para aumentar o nível de camp em um célula e combinação terapêutica, para o tratamento da fibrose cística
WO2012107364A1 (en) 2011-02-07 2012-08-16 Scipharm Sàrl Novel composition for the treatment of cystic fibrosis
KR20140053881A (ko) 2011-04-19 2014-05-08 릭스하스피탈렛 모세관 누출의 예방 및 치료를 위한 수술 동안 투여되는 프로스타시클린 및 그 유사체
CN103987704A (zh) 2011-08-05 2014-08-13 卡德尔治疗公司 类黄酮化合物
WO2013024051A1 (en) 2011-08-12 2013-02-21 Ascendis Pharma A/S Sustained release composition of prostacyclin
US20140249093A1 (en) 2011-08-12 2014-09-04 Ascendis Pharma A/S Carrier-Linked Prodrugs Having Reversible Carboxylic Ester Linkages
CA2843883C (en) * 2011-08-12 2020-04-28 Ascendis Pharma A/S Carrier-linked treprostinil prodrugs
US8524939B2 (en) 2011-08-24 2013-09-03 Chirogate International Inc. Intermediates for the synthesis of benzindene prostaglandins and preparations thereof
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
US9387214B2 (en) 2012-01-13 2016-07-12 United Therapeutics Corporation Method of identifying therapies for pulmonary hypertension
US20150057325A1 (en) 2012-03-30 2015-02-26 Rigshospitalet Compounds capable of modulating/preserving endothelial integrity for use in prevention or treatment of acute traumatic coagulopathy and resuscitated cardiac arrest
US20150087688A1 (en) 2012-04-25 2015-03-26 Ascendis Pharma A/S Prodrugs of hydroxyl-comprising drugs
SMT201700496T1 (it) 2012-06-15 2017-11-15 Scipharm Sarl Processo per la preparazione di treprostinil e suoi derivati
IN2015DN00934A (OSRAM) 2012-08-01 2015-06-12 United Therapeutics Corp
KR20150091170A (ko) 2012-12-07 2015-08-07 카이맨 케미칼 컴파니 인코포레이티드 프로스타사이클린 유사체의 합성 방법
US10080730B2 (en) 2013-01-09 2018-09-25 United Therapeutics Corporation Treatment of vasculopathy with prostacyclin and mesenchymal stem cells
JP6542128B2 (ja) 2013-01-11 2019-07-10 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
US9505737B2 (en) 2013-01-11 2016-11-29 Corsair Pharma, Inc. Treprostinil derivative compounds and methods of using same
KR102405650B1 (ko) 2013-03-15 2022-06-03 유나이티드 세러퓨틱스 코오포레이션 트레프로스티닐의 염
ES2676447T3 (es) 2013-03-25 2018-07-19 United Therapeutics Corporation Procedimiento de fabricación de compuestos de prostaciclina con tiol de unión y formas pegiladas
JP6594857B2 (ja) 2013-04-30 2019-10-23 ユナイテッド セラピューティクス コーポレイション 放出制御製剤
WO2014203278A2 (en) 2013-06-19 2014-12-24 Msn Laboratories Private Limited NOVEL PROCESS FOR THE PREPARATION OF (1R,2R,3aS,9aS)-[[2,3,3a,4,9,9a-HEXAHYDRO-2-HYDROXY-1-[(3S)-3-HYDROXYOCTYL]-1H-BENZ[f]INDEN-5-YL]OXY]ACETIC ACID
MX382833B (es) 2013-10-25 2025-03-13 Insmed Inc Compuestos derivados de prostaciclinas, y el uso de los mismo para el tratamiento de la hipertension pulmonar
EP3068752A1 (en) 2013-11-13 2016-09-21 Cayman Chemical Company Incorporated Amine salts of a prostacyclin analog
WO2015138423A1 (en) 2014-03-11 2015-09-17 Insmed Incorporated Prostacylin compositions and methods for using the same
EP3169660A1 (en) 2014-07-16 2017-05-24 Corsair Pharma, Inc. Treprostinil derivative compounds and methods of using same
HU231186B1 (hu) 2014-10-08 2021-06-28 CHINOIN Gyógyszer és Vegyészeti Termékek Gyára Zrt. Új eljárás treprostinil és sói előállítására
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
TWI540121B (zh) 2014-12-01 2016-07-01 臺灣永光化學工業股份有限公司 曲前列環素二乙醇胺之合成方法及新穎中間體
CA2973147A1 (en) 2015-01-27 2016-08-04 Scipharm Sarl Composition for the treatment of hepatic veno-occlusive disease
US20160243064A1 (en) 2015-02-21 2016-08-25 Gavis Pharmaceuticals Novel oral pharmaceutical compositions of treprostinil
WO2016176555A1 (en) 2015-04-29 2016-11-03 Insmed Incorporated Prostacyclin compounds, compositions and methods of use thereof
US9394227B1 (en) 2015-06-17 2016-07-19 Corsair Pharma, Inc. Treprostinil derivatives and compositions and uses thereof
US9643911B2 (en) 2015-06-17 2017-05-09 Corsair Pharma, Inc. Treprostinil derivatives and compositions and uses thereof
KR20230119035A (ko) 2016-12-05 2023-08-14 코세어 파마 인코포레이티드 트레프로스티닐 및 이의 염의 피부 및 경피 투여

Also Published As

Publication number Publication date
ES2897721T3 (es) 2022-03-02
US11034645B2 (en) 2021-06-15
US20200347006A1 (en) 2020-11-05
EP3835291A1 (en) 2021-06-16
US10988435B2 (en) 2021-04-27
US10246403B2 (en) 2019-04-02
US20180305293A1 (en) 2018-10-25
IL256260A (en) 2018-02-28
CN108349926A (zh) 2018-07-31
US20220055980A1 (en) 2022-02-24
KR20240149440A (ko) 2024-10-14
US9643911B2 (en) 2017-05-09
IL305157A (en) 2023-10-01
US11866402B2 (en) 2024-01-09
US20190241499A1 (en) 2019-08-08
US9957220B2 (en) 2018-05-01
US20180170855A1 (en) 2018-06-21
US20240124385A1 (en) 2024-04-18
IL289276B1 (en) 2023-09-01
CA2989317A1 (en) 2016-12-22
IL313291A (en) 2024-08-01
EP3310769B1 (en) 2021-08-18
EP3310769A1 (en) 2018-04-25
HK1258913A1 (zh) 2019-11-22
US10703706B2 (en) 2020-07-07
WO2016205202A1 (en) 2016-12-22
KR102711773B1 (ko) 2024-09-27
US20200071257A1 (en) 2020-03-05
IL256260B (en) 2022-01-01
IL289276A (en) 2022-02-01
IL305157B1 (en) 2024-07-01
ES2859749T3 (es) 2021-10-04
US20240116847A1 (en) 2024-04-11
KR20180027517A (ko) 2018-03-14
US20160368855A1 (en) 2016-12-22
IL289276B2 (en) 2024-01-01
US20170298001A1 (en) 2017-10-19
JP2018524304A (ja) 2018-08-30
US20210355072A1 (en) 2021-11-18
EP3456715A1 (en) 2019-03-20
JP2024019523A (ja) 2024-02-09
US10464877B2 (en) 2019-11-05
JP2022003057A (ja) 2022-01-11
US11802105B2 (en) 2023-10-31
JP7013245B2 (ja) 2022-01-31
EP3456715B1 (en) 2020-12-16

Similar Documents

Publication Publication Date Title
IL305157B2 (en) Treprostinil Derivatives and Compositions and Uses Thereof
US10759733B2 (en) Treprostinil derivatives and compositions and uses thereof
HK40051910A (en) Treprostinil derivatives and compositions and uses thereof
HK40005474A (en) Treprostinil derivatives and compositions and uses thereof
HK40005474B (en) Treprostinil derivatives and compositions and uses thereof