CA2989317A1 - Treprostinil derivatives and compositions and uses thereof - Google Patents

Treprostinil derivatives and compositions and uses thereof Download PDF

Info

Publication number
CA2989317A1
CA2989317A1 CA2989317A CA2989317A CA2989317A1 CA 2989317 A1 CA2989317 A1 CA 2989317A1 CA 2989317 A CA2989317 A CA 2989317A CA 2989317 A CA2989317 A CA 2989317A CA 2989317 A1 CA2989317 A1 CA 2989317A1
Authority
CA
Canada
Prior art keywords
compound
co2h
hydrogen
occurrence independently
treprostinil
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.)
Pending
Application number
CA2989317A
Other languages
English (en)
French (fr)
Inventor
Xiaoming Zhang
Meenakshi S. Venkatraman
Cyrus K. Becker
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.)
Corsair Pharma Inc
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 CA2989317A1 publication Critical patent/CA2989317A1/en
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters 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
    • C07C69/73—Esters 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
    • C07C69/734—Ethers
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/34—Heterocyclic 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
    • A61K31/341—Heterocyclic 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
    • 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
    • A61K31/35—Heterocyclic 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
    • A61K31/351—Heterocyclic 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
    • 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
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • 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
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • 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
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703—Transdermal 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
    • A61K9/7092—Transdermal patches having multiple drug layers or reservoirs, e.g. for obtaining a specific release pattern, or for combining different drugs
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P37/04—Immunostimulants
    • 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
    • C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/132—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing rings
    • C07C53/136—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing rings containing condensed ring systems
    • 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
    • C07C59/01—Saturated compounds having only one carboxyl group and containing hydroxy or O-metal groups
    • C07C59/11—Saturated compounds having only one carboxyl group and containing hydroxy or O-metal groups containing rings
    • 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
    • C07C59/125—Saturated compounds having only one carboxyl group and containing ether groups, groups, groups, or groups
    • C07C59/13—Saturated compounds having only one carboxyl group and containing ether groups, groups, groups, or groups containing rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/02—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
    • C07C69/22—Esters 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
    • C07C69/28—Esters 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters 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
    • C07C69/67—Esters 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
    • C07C69/675—Esters 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters 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
    • C07C69/67—Esters 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
    • C07C69/675—Esters 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
    • C07C69/68—Lactic acid esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters 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
    • C07C69/67—Esters 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
    • C07C69/708—Ethers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters 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
    • C07C69/67—Esters 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
    • C07C69/708—Ethers
    • C07C69/712—Ethers 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/74—Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/74—Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C07C69/75—Esters 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/74—Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C07C69/757—Esters 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/96—Esters of carbonic or haloformic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D305/00—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
    • C07D305/02—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D305/04—Heterocyclic 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
    • C07D305/08—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic 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
    • C07D307/18—Heterocyclic 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
    • C07D307/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/26—Heterocyclic 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
    • C07D307/30—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic 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
    • C07D309/08—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/04—Systems containing only non-condensed rings with a four-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated
    • 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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (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)
  • Epoxy Compounds (AREA)
  • Furan Compounds (AREA)
  • Pyrane Compounds (AREA)
CA2989317A 2015-06-17 2016-06-14 Treprostinil derivatives and compositions and uses thereof Pending CA2989317A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201514742579A 2015-06-17 2015-06-17
US14/742,579 2015-06-17
US14/742,544 2015-06-17
US14/742,544 US9394227B1 (en) 2015-06-17 2015-06-17 Treprostinil derivatives and compositions and uses thereof
US14/829,180 2015-08-18
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 (1)

Publication Number Publication Date
CA2989317A1 true CA2989317A1 (en) 2016-12-22

Family

ID=56204034

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2989317A Pending CA2989317A1 (en) 2015-06-17 2016-06-14 Treprostinil derivatives and compositions and uses thereof

Country Status (10)

Country Link
US (11) US9643911B2 (OSRAM)
EP (3) EP3835291A1 (OSRAM)
JP (3) JP7013245B2 (OSRAM)
KR (2) KR20240149440A (OSRAM)
CN (1) CN108349926A (OSRAM)
CA (1) CA2989317A1 (OSRAM)
ES (2) ES2859749T3 (OSRAM)
HK (1) HK1258913A1 (OSRAM)
IL (4) IL289276B2 (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
EP3712142B1 (en) 2013-01-11 2022-07-06 Corsair Pharma, Inc. Prodrugs of treprostinil
US9505737B2 (en) 2013-01-11 2016-11-29 Corsair Pharma, Inc. Treprostinil derivative compounds and methods of using same
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
WO2017192993A1 (en) 2016-05-05 2017-11-09 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
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
CN114616225A (zh) * 2019-08-23 2022-06-10 联合治疗公司 曲前列环素前药
US11826327B2 (en) 2020-04-17 2023-11-28 United Therapeutics Corporation Treatment for interstitial lung disease
JP2023553989A (ja) 2020-12-14 2023-12-26 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で疾患を治療する方法
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)
WO2022194195A1 (zh) * 2021-03-16 2022-09-22 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
KR20240141319A (ko) 2022-02-08 2024-09-26 유나이티드 쎄러퓨틱스 코포레이션 트레프로스티닐 일로프로스트 조합 치료 요법
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
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
KR20250139830A (ko) * 2023-01-19 2025-09-23 유나이티드 쎄러퓨틱스 코포레이션 트레프로스티닐 유사체
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
WO2025007744A1 (zh) * 2023-07-03 2025-01-09 长风药业(香港)有限公司 一种曲前列环素衍生物、其制备方法及应用

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
US4683330A (en) 1984-03-08 1987-07-28 The Upjohn Company Interphenylene carbacyclin derivatives
US4668814A (en) 1984-03-08 1987-05-26 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
US20020004065A1 (en) 2000-01-20 2002-01-10 David Kanios Compositions and methods to effect the release profile in the transdermal administration of active agents
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
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
US20070269379A1 (en) * 2003-07-23 2007-11-22 Samir Mitragotri 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
CA2549724C (en) * 2003-12-16 2014-02-11 United Therapeutics Corporation Use of treprostinil to treat and prevent ischemic lesions
DE602004022982D1 (de) 2003-12-16 2009-10-15 United Therapeutics Corp Verwendung von treprostinil zur verbesserung der nierenfunktion
ATE462427T1 (de) 2004-04-12 2010-04-15 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
ES2596809T3 (es) 2004-10-08 2017-01-12 Noven Pharmaceuticals, Inc. Dispositivo de administración transdérmica de fármacos que incluye un refuerzo oclusivo
ES2607454T3 (es) 2005-06-03 2017-03-31 Acrux Dds Pty Ltd Método y composición para el suministro transdérmico de testosterona
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
EP1988910B1 (en) 2006-02-28 2017-12-06 Kodiak Sciences Inc. Acryloyloxyethylphosphorylcholine containing polymer conjugates and their preparation
US8747897B2 (en) 2006-04-27 2014-06-10 Supernus Pharmaceuticals, Inc. Osmotic drug delivery system
KR101390579B1 (ko) 2006-05-15 2014-05-19 유나이티드 세러퓨틱스 코오포레이션 정량 흡입기를 사용한 트레프로스티닐 투여
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
EP2120961A1 (en) 2007-02-09 2009-11-25 United Therapeutics Corporation Treprostinil treatment for interstitial lung disease and asthma
EA201070127A1 (ru) 2007-07-11 2010-08-30 Лексикон Фармасьютикалз , Инк. Способы лечения легочной гипертензии, родственных заболеваний и нарушений и композиции для их осуществления
KR20160048222A (ko) 2007-12-17 2016-05-03 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
US20110294815A1 (en) 2008-06-27 2011-12-01 Harbeson Scott L Prostacyclin analogs
SI3300729T1 (sl) 2008-08-13 2020-02-28 Actelion Pharmaceuticals Ltd. Terapevtski sestavki, ki vsebujejo macitentan
EP2384196B1 (en) 2008-12-30 2017-09-13 Johansson, Pär Methods of identifying critically ill patients at increased risk of development of organ failure and compounds for the treatment hereof
KR101544246B1 (ko) 2009-05-07 2015-08-12 유나이티드 세러퓨틱스 코오포레이션 프로스타시클린 유사체의 고체 제제
US8519178B2 (en) 2009-06-22 2013-08-27 Johnson Matthey Public Limited Company Method for the purification of prostaglandins
KR101729800B1 (ko) 2009-08-07 2017-04-24 에스씨아이팜 에스에이알엘 낭포성 섬유증의 치료를 위한 조성물
US9327105B2 (en) * 2010-03-26 2016-05-03 Itrace Biomedical Inc. Active transdermal drug delivery system and the method thereof
WO2011123830A2 (en) 2010-04-02 2011-10-06 Amunix Operating Inc. Alpha 1-antitrypsin compositions and methods of making and using same
EP3372617B1 (en) 2010-04-02 2024-07-24 Amunix Pharmaceuticals, Inc. Binding fusion proteins, binding fusion protein-drug conjugates, xten-drug conjugates 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
CA2777070C (en) 2010-06-03 2019-11-05 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
DK2663313T3 (en) 2011-01-13 2018-11-26 Scipharm S A R L PROCEDURE FOR IMPROVING ENGRAFTMENT OF HEMATOPOIETIC STEM CELLS
CA2826183C (en) 2011-02-07 2019-05-14 Scipharm Sarl Novel composition for the treatment of cystic fibrosis
WO2012107364A1 (en) 2011-02-07 2012-08-16 Scipharm Sàrl Novel composition for the treatment of cystic fibrosis
US20140044797A1 (en) 2011-04-19 2014-02-13 Rigshospitalet Prostacyclin and analogs thereof administered during surgery for prevention and treatment of capillary leakage
EP2739613A4 (en) 2011-08-05 2015-01-07 Cardero Therapeutics Inc flavonoid
BR112014003240A2 (pt) 2011-08-12 2017-03-01 Ascendis Pharma As composição de prostaciclina com liberação sustentada
JP6092867B2 (ja) * 2011-08-12 2017-03-08 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
CA2843506C (en) 2011-08-12 2020-05-12 Ascendis Pharma A/S Carrier-linked prodrugs having reversible carboxylic ester linkages
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
EP2841109A1 (en) 2012-04-25 2015-03-04 Ascendis Pharma A/S Prodrugs of hydroxyl-comprising drugs
ES2639823T3 (es) 2012-06-15 2017-10-30 Scipharm Sàrl Proceso para la preparación de treprostinilo y derivados del mismo
CA2880808C (en) 2012-08-01 2023-01-24 United Therapeutics Corporation Treatment of pulmonary arterial hypertension with mesenchymal stem cells
CN104837806A (zh) 2012-12-07 2015-08-12 开曼化学股份有限公司 前列环素类似物的合成方法
WO2014110094A1 (en) 2013-01-09 2014-07-17 United Therapeutics Corporation Treatment of vasculopathy with prostacyclin and mesenchymal stem cells
EP3712142B1 (en) 2013-01-11 2022-07-06 Corsair Pharma, Inc. Prodrugs of treprostinil
US9505737B2 (en) 2013-01-11 2016-11-29 Corsair Pharma, Inc. Treprostinil derivative compounds and methods of using same
CN109608326A (zh) 2013-03-15 2019-04-12 联合治疗公司 曲前列环素的盐
WO2014160638A1 (en) 2013-03-25 2014-10-02 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
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
EP3808731A1 (en) 2013-10-25 2021-04-21 Insmed Incorporated Prostacyclin compounds
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
WO2016010538A1 (en) 2014-07-16 2016-01-21 Corsair Pharma, Inc. Treprostinil derivative compounds and methods of using same
HU231184B1 (hu) 2014-10-08 2021-07-28 CHINOIN Gyógyszer és Vegyészeti Termékek Gyára Zrt. Treprostinil-nátrium-monohidrát és eljárás ennek előállítására
CA2967385C (en) 2014-11-18 2023-05-16 Insmed Incorporated Methods of manufacturing treprostinil and treprostinil derivative prodrugs
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
WO2016120311A1 (en) 2015-01-27 2016-08-04 Scipharm Sàrl 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
CA3045917A1 (en) 2016-12-05 2018-06-14 Corsair Pharma, Inc. Dermal and transdermal administration of treprostinil and salts thereof

Also Published As

Publication number Publication date
IL313291A (en) 2024-08-01
KR20180027517A (ko) 2018-03-14
US20220055980A1 (en) 2022-02-24
US20180305293A1 (en) 2018-10-25
US20170298001A1 (en) 2017-10-19
EP3310769A1 (en) 2018-04-25
US20210355072A1 (en) 2021-11-18
US11802105B2 (en) 2023-10-31
IL289276A (en) 2022-02-01
CN108349926A (zh) 2018-07-31
US20200347006A1 (en) 2020-11-05
US10464877B2 (en) 2019-11-05
US20160368855A1 (en) 2016-12-22
JP2022003057A (ja) 2022-01-11
IL305157B2 (en) 2024-11-01
US20240116847A1 (en) 2024-04-11
EP3456715A1 (en) 2019-03-20
US11866402B2 (en) 2024-01-09
WO2016205202A1 (en) 2016-12-22
US20240124385A1 (en) 2024-04-18
EP3456715B1 (en) 2020-12-16
IL256260B (en) 2022-01-01
ES2859749T3 (es) 2021-10-04
HK1258913A1 (zh) 2019-11-22
EP3835291A1 (en) 2021-06-16
US10988435B2 (en) 2021-04-27
US10246403B2 (en) 2019-04-02
EP3310769B1 (en) 2021-08-18
JP2018524304A (ja) 2018-08-30
US20200071257A1 (en) 2020-03-05
JP2024019523A (ja) 2024-02-09
US11034645B2 (en) 2021-06-15
US20180170855A1 (en) 2018-06-21
JP7013245B2 (ja) 2022-01-31
US20190241499A1 (en) 2019-08-08
IL305157B1 (en) 2024-07-01
US9957220B2 (en) 2018-05-01
US10703706B2 (en) 2020-07-07
IL256260A (en) 2018-02-28
ES2897721T3 (es) 2022-03-02
IL289276B2 (en) 2024-01-01
US9643911B2 (en) 2017-05-09
KR20240149440A (ko) 2024-10-14
IL305157A (en) 2023-10-01
KR102711773B1 (ko) 2024-09-27
IL289276B1 (en) 2023-09-01

Similar Documents

Publication Publication Date Title
CA2989317A1 (en) Treprostinil derivatives and compositions and uses thereof
US11407707B2 (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

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20210602

EEER Examination request

Effective date: 20210602

EEER Examination request

Effective date: 20210602

EEER Examination request

Effective date: 20210602

EEER Examination request

Effective date: 20210602

EEER Examination request

Effective date: 20210602

EEER Examination request

Effective date: 20210602

EEER Examination request

Effective date: 20210602

EEER Examination request

Effective date: 20210602

EEER Examination request

Effective date: 20210602