BR112015013085A2 - métodos de síntese de um análogo de prostaciclina - Google Patents

métodos de síntese de um análogo de prostaciclina

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Publication number
BR112015013085A2
BR112015013085A2 BR112015013085A BR112015013085A BR112015013085A2 BR 112015013085 A2 BR112015013085 A2 BR 112015013085A2 BR 112015013085 A BR112015013085 A BR 112015013085A BR 112015013085 A BR112015013085 A BR 112015013085A BR 112015013085 A2 BR112015013085 A2 BR 112015013085A2
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BR
Brazil
Prior art keywords
processes
present
generate
methods
traditional methods
Prior art date
Application number
BR112015013085A
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English (en)
Inventor
Chambournier Gilles
William Endres Gregory
Mahmoud Mahmoud Hussein
William Hering Kirk
James Krell Ii Thomas
Fedij Victor
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Cayman Chemical Co 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.)
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Publication date
Application filed by Cayman Chemical Co Inc filed Critical Cayman Chemical Co Inc
Publication of BR112015013085A2 publication Critical patent/BR112015013085A2/pt

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    • 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
    • C07C205/00Compounds containing nitro groups bound to a carbon skeleton
    • C07C205/49Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups
    • C07C205/57Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C41/00Preparation of ethers; Preparation of compounds having groups, groups or groups
    • C07C41/01Preparation of ethers
    • C07C41/18Preparation of ethers by reactions not forming ether-oxygen bonds
    • C07C41/26Preparation of ethers by reactions not forming ether-oxygen bonds by introduction of hydroxy or O-metal groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C41/00Preparation of ethers; Preparation of compounds having groups, groups or groups
    • C07C41/01Preparation of ethers
    • C07C41/34Separation; Purification; Stabilisation; Use of additives
    • C07C41/44Separation; Purification; Stabilisation; Use of additives by treatments giving rise to a chemical modification
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/27Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation
    • C07C45/29Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation of hydroxy groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/09Preparation of carboxylic acids or their salts, halides or anhydrides from carboxylic acid esters or lactones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/347Preparation of carboxylic acids or their salts, halides or anhydrides by reactions not involving formation of carboxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41Preparation of salts of carboxylic acids
    • C07C51/412Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D301/00Preparation of oxiranes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D301/00Preparation of oxiranes
    • C07D301/32Separation; Purification
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D303/00Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02Compounds containing oxirane rings
    • C07D303/12Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms
    • C07D303/14Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by free hydroxyl radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D303/00Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02Compounds containing oxirane rings
    • C07D303/12Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms
    • C07D303/16Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by esterified hydroxyl radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/14Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D317/18Radicals substituted by singly bound oxygen or sulfur atoms
    • C07D317/22Radicals substituted by singly bound oxygen or sulfur atoms etherified
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Cardiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Epoxy Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

resumo da patente de invenção para: “métodos de síntese de um análogo de prostaciclina”. a presente invenção proporciona processos de preparação de um análogo de prostaciclina da fórmula i ou um sal farmacêuticamente aceitável do mesmo, em que r10 é um alquila c1-6 linear ou ramificado. os processos da presente invenção compreendem etapas que geram melhores rendimentos e menor número de subprodutos do que os métodos tradicionais. os processos da presente invenção empregam reagentes (por exemplo, o reagente oxidante) que são menos tóxicos do que os usados nos métodos tradicionais (por exemplo, cloreto de oxalila). muitos dos processos da presente invenção geram intermediários com melhor e.e. e pureza química; eliminando, portanto, a necessidade de etapas de cromatografia adicionais. ademais, os processos da presente invenção são escaláveis para gerar quantidades comerciais do composto final.
BR112015013085A 2012-12-07 2013-12-06 métodos de síntese de um análogo de prostaciclina BR112015013085A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261734672P 2012-12-07 2012-12-07
US201361777882P 2013-03-12 2013-03-12
PCT/US2013/073474 WO2014089385A2 (en) 2012-12-07 2013-12-06 Methods of synthesizing a prostacyclin analog

Publications (1)

Publication Number Publication Date
BR112015013085A2 true BR112015013085A2 (pt) 2017-07-11

Family

ID=49881039

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015013085A BR112015013085A2 (pt) 2012-12-07 2013-12-06 métodos de síntese de um análogo de prostaciclina

Country Status (21)

Country Link
US (4) US20150315114A1 (pt)
EP (2) EP3398931B1 (pt)
JP (2) JP6342414B2 (pt)
KR (1) KR20150091170A (pt)
CN (3) CN110590547A (pt)
AU (2) AU2013355130B2 (pt)
BR (1) BR112015013085A2 (pt)
CA (1) CA2893604A1 (pt)
CL (1) CL2015001535A1 (pt)
DK (1) DK2928858T3 (pt)
EA (1) EA034309B1 (pt)
ES (1) ES2664026T3 (pt)
HK (1) HK1212323A1 (pt)
IL (1) IL239172B (pt)
MX (2) MX369094B (pt)
NZ (1) NZ708130A (pt)
PE (1) PE20160090A1 (pt)
PH (2) PH12015501258B1 (pt)
SG (2) SG10201600303WA (pt)
TW (1) TWI634104B (pt)
WO (1) WO2014089385A2 (pt)

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Publication number Priority date Publication date Assignee Title
CN110590547A (zh) * 2012-12-07 2019-12-20 开曼化学股份有限公司 前列环素衍生物的合成方法
WO2014110491A1 (en) 2013-01-11 2014-07-17 Theratrophix Llc Prodrugs of treprostinil
US9505737B2 (en) 2013-01-11 2016-11-29 Corsair Pharma, Inc. Treprostinil derivative compounds and methods of using same
EP3068752A1 (en) * 2013-11-13 2016-09-21 Cayman Chemical Company Incorporated Amine salts of a prostacyclin analog
HU231184B1 (hu) 2014-10-08 2021-07-28 CHINOIN Gyógyszer és Vegyészeti Termékek Gyára Zrt. Treprostinil-nátrium-monohidrát és eljárás ennek előállítására
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
KR102541885B1 (ko) 2016-09-26 2023-06-12 유나이티드 쎄러퓨틱스 코포레이션 트레프로스티닐 프로드럭
EP3498283A1 (en) 2017-12-14 2019-06-19 Ipsol AG Glycosidic derivatives of treprostinil
HU231296B1 (hu) 2018-03-09 2022-09-28 Chinoin Zrt Eljárás treprostinil-dietanol-amin só B polimorf formájának előállítására
EP4017588A1 (en) 2019-08-23 2022-06-29 United Therapeutics Corporation Treprostinil prodrugs
IL296567A (en) 2020-04-17 2022-11-01 United Therapeutics Corp Terfostinil for use in the treatment of interstitial lung disease
WO2021252446A1 (en) 2020-06-09 2021-12-16 United Therapeutics Corporation Fumaryl diketopiperidine prodrugs of treprostinil
KR20220030006A (ko) 2020-09-02 2022-03-10 바이오플러스 주식회사 미용 조성물을 포함하는 마스크 및 그 제조 방법
WO2022132655A1 (en) 2020-12-14 2022-06-23 United Therapeutics Corporation Methods of treating disease with treprostinil prodrugs
US11884640B2 (en) * 2021-06-02 2024-01-30 Chirogate International Inc. Processes and intermediates for the preparations of benzoprostacyclin analogues and benzoprostacyclin analogues prepared therefrom

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CN110590547A (zh) * 2012-12-07 2019-12-20 开曼化学股份有限公司 前列环素衍生物的合成方法
EP3068752A1 (en) * 2013-11-13 2016-09-21 Cayman Chemical Company Incorporated Amine salts of a prostacyclin analog

Also Published As

Publication number Publication date
JP2016504303A (ja) 2016-02-12
US9908834B2 (en) 2018-03-06
EP2928858B1 (en) 2018-01-31
TWI634104B (zh) 2018-09-01
WO2014089385A3 (en) 2014-08-28
EA034309B1 (ru) 2020-01-27
PH12015501258A1 (en) 2015-08-17
US10450257B2 (en) 2019-10-22
CN104837806A (zh) 2015-08-12
SG10201600303WA (en) 2016-02-26
US20180141889A1 (en) 2018-05-24
AU2018233009B2 (en) 2020-01-23
JP6342414B2 (ja) 2018-06-13
MX2015006972A (es) 2016-02-11
ES2664026T3 (es) 2018-04-18
IL239172B (en) 2020-01-30
SG11201504430TA (en) 2015-07-30
HK1212323A1 (en) 2016-06-10
KR20150091170A (ko) 2015-08-07
TW201422577A (zh) 2014-06-16
AU2018233009A1 (en) 2018-10-18
PE20160090A1 (es) 2016-02-20
US20170297995A1 (en) 2017-10-19
IL239172A0 (en) 2015-07-30
CA2893604A1 (en) 2014-06-12
WO2014089385A2 (en) 2014-06-12
MX369094B (es) 2019-10-29
US20150315114A1 (en) 2015-11-05
NZ708130A (en) 2020-01-31
EA201591093A1 (ru) 2015-09-30
AU2013355130A1 (en) 2015-06-11
PH12018500562A1 (en) 2019-03-04
MX2019009102A (es) 2019-09-16
JP2018162250A (ja) 2018-10-18
AU2013355130B2 (en) 2018-06-21
CN107098925A (zh) 2017-08-29
CL2015001535A1 (es) 2016-01-15
CN110590547A (zh) 2019-12-20
US20200002261A1 (en) 2020-01-02
DK2928858T3 (en) 2018-02-19
EP2928858A2 (en) 2015-10-14
CN107098925B (zh) 2019-09-13
EP3398931A1 (en) 2018-11-07
PH12015501258B1 (en) 2015-08-17
EP3398931B1 (en) 2020-04-08

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Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

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