ES8704443A1 - Un procedimiento para la preparacion de derivados sustituidos ester benzoato de 3-hidroximorfinanos. - Google Patents

Un procedimiento para la preparacion de derivados sustituidos ester benzoato de 3-hidroximorfinanos.

Info

Publication number
ES8704443A1
ES8704443A1 ES544852A ES544852A ES8704443A1 ES 8704443 A1 ES8704443 A1 ES 8704443A1 ES 544852 A ES544852 A ES 544852A ES 544852 A ES544852 A ES 544852A ES 8704443 A1 ES8704443 A1 ES 8704443A1
Authority
ES
Spain
Prior art keywords
hydroxymorphinans
intermediates
processes
prodrug derivatives
ester prodrug
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.)
Expired
Application number
ES544852A
Other languages
English (en)
Other versions
ES544852A0 (es
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.)
EIDP Inc
Original Assignee
EI Du Pont de Nemours and Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by EI Du Pont de Nemours and Co filed Critical EI Du Pont de Nemours and Co
Publication of ES544852A0 publication Critical patent/ES544852A0/es
Publication of ES8704443A1 publication Critical patent/ES8704443A1/es
Expired legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/06—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with a hetero atom directly attached in position 14
    • C07D489/08—Oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/22—Bridged ring systems
    • C07D221/28—Morphinans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/02—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

PROCEDIMIENTO PARA PREPARAR DERIVADOS SUSTITUIDOS ESTERBENZOATO DE 3-HIDROXIMORFINANOS. CONSISTE EN HACER REACCIONAR A UN 3-HIDROXIMORFINANO DE FORMULA (II) CON UN AGENTE DE ACILACION DE FORMULA (III), EN CLORURO DE METILENO O TETRAHIDROFURANO, EN PRESENCIA DE TIETILAMINA O PIRIDINA, ENTRE 0JC Y EL PUNTO DE EBULLICION DEL DISOLVENTE, Y DURANTE 0,5 A 24 HORAS, PARA OBTENER UN COMPUESTO DE FORMULA (I). SIENDO: A, UN ENLACE SENCILLO O DOBLE; R, METILO, ALILO O CICLOPROPILMETILO; R1 Y R2, H U OH; R3 Y R4, H; R6, H, ALQUILO DE C 1 A 4 Y OTROS; Y X E Y, H, OR6 Y NHR6. SE UTILIZA PARA EL TRATAMIENTO DEL DOLOR EN MAMIFEROS.
ES544852A 1984-07-05 1985-07-04 Un procedimiento para la preparacion de derivados sustituidos ester benzoato de 3-hidroximorfinanos. Expired ES8704443A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US62792384A 1984-07-05 1984-07-05
US06/733,464 US4668685A (en) 1984-07-05 1985-05-14 Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans, which are analgesics or narcotic antagonists

Publications (2)

Publication Number Publication Date
ES544852A0 ES544852A0 (es) 1987-04-01
ES8704443A1 true ES8704443A1 (es) 1987-04-01

Family

ID=27090564

Family Applications (1)

Application Number Title Priority Date Filing Date
ES544852A Expired ES8704443A1 (es) 1984-07-05 1985-07-04 Un procedimiento para la preparacion de derivados sustituidos ester benzoato de 3-hidroximorfinanos.

Country Status (18)

Country Link
US (1) US4668685A (es)
EP (1) EP0170090B1 (es)
AU (1) AU578391B2 (es)
CA (1) CA1301150C (es)
DE (1) DE3573251D1 (es)
DK (1) DK160501C (es)
ES (1) ES8704443A1 (es)
FI (1) FI83215C (es)
GR (1) GR851653B (es)
HK (1) HK39790A (es)
HU (1) HU193995B (es)
IE (1) IE58136B1 (es)
IL (1) IL75721A (es)
MX (1) MX160445A (es)
NO (1) NO171209C (es)
NZ (1) NZ212641A (es)
PT (1) PT80773B (es)
SU (2) SU1450742A3 (es)

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US6258360B1 (en) * 1989-05-04 2001-07-10 Igen International, Inc. Prodrugs activated by targeted catalytic proteins
KR100334697B1 (ko) * 1991-08-05 2002-04-27 리차아드제이마세이 표적화된 촉매 단백질에 의해 활성화되는 선구 약제
US5968551A (en) * 1991-12-24 1999-10-19 Purdue Pharma L.P. Orally administrable opioid formulations having extended duration of effect
US6323212B1 (en) * 1992-01-23 2001-11-27 Toray Industries, Inc. Morphinan derivative and its pharmaceutical applications
TW372972B (en) * 1992-10-23 1999-11-01 Novartis Ag Antiretroviral acyl compounds
DE69427551T2 (de) * 1993-03-15 2002-05-16 National Science Council, Taipeh/T'ai-Pei Nalbuphinester und diese enthaltende Arzneimittel mit verzögerter Wirkstoffabgabe
EP0663401B1 (en) * 1993-07-23 2000-06-07 Toray Industries, Inc. Morphinan derivative and medicinal use
US5376662A (en) * 1993-12-08 1994-12-27 Ockert; David M. Method of attenuating nerve injury induced pain
US5869669A (en) * 1996-07-26 1999-02-09 Penick Corporation Preparation of 14-hydroxynormorphinones from normorphinone dienol acylates
US6225321B1 (en) * 1997-06-05 2001-05-01 Oliver Yoa-Pu Hu Long analgesic acting nalbuphine polyester derivative and method of use
ES2412409T3 (es) 1997-12-22 2013-07-11 Euro-Celtique S.A. Forma farmacéutica para dosificación oral que comprende una combinación de un agonista opiáceo y un antagonista opiáceo
US6375957B1 (en) 1997-12-22 2002-04-23 Euro-Celtique, S.A. Opioid agonist/opioid antagonist/acetaminophen combinations
DE60001487T2 (de) * 2000-04-27 2003-12-24 Oliver Yoa-Pu Hu Polynalbuphinderivat
US6569449B1 (en) 2000-11-13 2003-05-27 University Of Kentucky Research Foundation Transdermal delivery of opioid antagonist prodrugs
CA2446550C (en) 2001-05-11 2012-03-06 Endo Pharmaceuticals, Inc. Abuse-resistant controlled-release opioid dosage form
US20040033253A1 (en) * 2002-02-19 2004-02-19 Ihor Shevchuk Acyl opioid antagonists
CA2708900C (en) * 2002-04-05 2019-06-04 Purdue Pharma Pharmaceutical preparation containing oxycodone and naloxone
US20040202717A1 (en) 2003-04-08 2004-10-14 Mehta Atul M. Abuse-resistant oral dosage forms and method of use thereof
US20080020028A1 (en) * 2003-08-20 2008-01-24 Euro-Celtique S.A. Transdermal dosage form comprising an active agent and a salt and a free-base form of an adverse agent
EP1604667A1 (en) * 2004-06-08 2005-12-14 Euro-Celtique S.A. Opioids for the treatment of the restless leg syndrome
EP1604666A1 (en) * 2004-06-08 2005-12-14 Euro-Celtique S.A. Opioids for the treatment of the Chronic Obstructive Pulmonary Disease (COPD)
US20060069086A1 (en) * 2004-09-23 2006-03-30 Alexander Michalow Methods for regulating neurotransmitter systems by inducing counteradaptations
US20080045610A1 (en) * 2004-09-23 2008-02-21 Alexander Michalow Methods for regulating neurotransmitter systems by inducing counteradaptations
KR20090029856A (ko) * 2005-01-28 2009-03-23 유로-셀띠끄 소시에떼 아노님 알코올 저항성 제형
EP1702558A1 (en) * 2005-02-28 2006-09-20 Euro-Celtique S.A. Method and device for the assessment of bowel function
EP1695700A1 (en) * 2005-02-28 2006-08-30 Euro-Celtique S.A. Dosage form containing oxycodone and naloxone
US8163701B2 (en) 2005-08-19 2012-04-24 Signature Therapeutics, Inc. Prodrugs of active agents
GB0606124D0 (en) * 2006-03-28 2006-05-03 Reckitt Benckiser Healthcare Buprenorphine derivatives and uses thereof
BRPI0808651A2 (pt) * 2007-03-09 2014-08-19 Green Cross Corp Pró-medicamentos oralmente biodisponíveis de (+)-3-hidroximorfinano para a prevenção ou o tratamento da doença de parkinson.
PE20110422A1 (es) * 2008-07-07 2011-07-01 Euro Celtique Sa Composicion farmaceutica que comprende antagonistas opioides
PT2405915T (pt) 2009-03-10 2019-01-29 Euro Celtique Sa Composições farmacêuticas de libertação imediata compreendendo oxicodona e naloxona
US10849981B2 (en) 2009-07-02 2020-12-01 KemPham, Inc. Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof
UA102916C2 (uk) 2009-07-02 2013-08-27 Кемфарм, Інк. Композиція на основі кон'югату гідрокодону з бензойною кислотою, похідними бензойної кислоти або гетероарилкарбоновою кислотою, проліки, спосіб лікування від зловживань
US8623888B2 (en) * 2009-07-15 2014-01-07 Mallinckrodt Llc 3-oxy-hydromorphone derivatives
RS59256B1 (sr) * 2010-11-12 2019-10-31 Shionogi & Co Kristalni derivat 6,7-nezasićenog-7-karbamoil morfinana, i postupak njegove proizvodnje
RU2573388C2 (ru) 2011-10-26 2016-01-20 Кемфарм Инк. Бензойная кислота, производные бензойной кислоты и конъюгаты гетероарилкарбоновой кислоты с гидроморфоном, пролекарства, способы получения и их применение
EP3024461B1 (en) 2013-07-23 2020-05-13 Euro-Celtique S.A. A combination of oxycodone and naloxone for use in treating pain in patients suffering from pain and a disease resulting in intestinal dysbiosis and/or increasing the risk for intestinal bacterial translocation
SG11201704178UA (en) 2014-11-25 2017-06-29 Kempharm Inc Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxycodone
CA2969221C (en) 2014-12-02 2021-01-12 Travis Mickle Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxymorphone, prodrugs, methods of making and use thereof
US10155771B2 (en) * 2015-11-04 2018-12-18 Noramco, Inc. Selective reduction of morphinan alkaloids
US10807995B2 (en) 2018-07-13 2020-10-20 Alkermes Pharma Ireland Limited Thienothiophene compounds for long-acting injectable compositions and related methods
US10799496B2 (en) 2018-07-13 2020-10-13 Alkermes Pharma Ireland Limited Naphthylenyl compounds for long-acting injectable compositions and related methods
US11186585B2 (en) 2018-08-17 2021-11-30 Kappa-Pharma LLC Compositions and methods of enhancing opioid receptor engagement by opioid hexadienoates and optionally substituted hexadienoates
WO2020094634A1 (en) 2018-11-05 2020-05-14 Alkermes Pharma Ireland Limited Thiophene prodrugs of naltroxene for long-acting injectable compositions and related methods
CA3149152A1 (en) 2019-08-11 2021-02-18 Kappa-Pharma LLC Compositions and methods of enhancing opioid receptor engagement by opioid hexadienoates and optionally substituted hexadienoates

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE224197C (es) *
US3254088A (en) * 1961-03-14 1966-05-31 Lewenstein Morphine derivative
FR1602610A (en) * 1962-10-10 1971-01-04 10.10.62.-17.4.63. 38445-15209 thebaine derivs
US3332950A (en) * 1963-03-23 1967-07-25 Endo Lab 14-hydroxydihydronormorphinone derivatives
IL26896A (en) * 1966-01-19 1970-11-30 Endo Lab 14 - Hydroxynormorphinins and 14 - Hydroxynormorphinones
GB1097167A (en) * 1966-05-31 1967-12-29 Shionogi & Co 3-hydroxy-6-oxo-n-phenethylmorphinan compounds and their production
CH560194A5 (es) * 1967-08-25 1975-03-27 Hoffmann La Roche
US3654280A (en) * 1968-03-21 1972-04-04 Shionogi & Co L-n allylic-3-hydroxy-6-oxomorphinans
DE2323192A1 (de) * 1972-05-10 1973-12-13 Endo Lab Injizierbare, langwirkende antagonistpraeparate gegen narkotika und rauschgifte
US4161597A (en) * 1976-12-20 1979-07-17 Research Corporation N-alkyl-14-hydroxymorphinans and derivatives
JPS59184163A (ja) * 1983-04-02 1984-10-19 Res Inst For Prod Dev ３−ベンゾイルチオ−１７−メチルモルヒナン
JPS59184183A (ja) * 1983-04-02 1984-10-19 Res Inst For Prod Dev ３−ベンゾイルチオ−４、５α−エポキシ−７α−〔１（Ｒ）−ヒドロキシ−１−メチルブチル〕−６−メトキシ−１７−メチル−６、１４−エンド−エテノモルヒナン
JPS59184182A (ja) * 1983-04-02 1984-10-19 Res Inst For Prod Dev ３−ベンゾイルチオ−４、５α−エポキシ−７α−〔１（Ｒ）−ヒドロキシ−１−メチルベンチル〕−６−メトキシ−１７−メチル−６、１４−エンド−エタノモルヒナン
JPS59186987A (ja) * 1983-04-06 1984-10-23 Res Inst For Prod Dev ３−ベンゾイルチオ−４、５α−エポキシ−７α−〔１（Ｒ）−ヒドロキシ−１−メチルブチル〕−６−メトキシ−１７−メチル−６、１４−エンド−エテノモルヒナン

Also Published As

Publication number Publication date
GR851653B (es) 1985-11-26
DK160501B (da) 1991-03-18
IE851683L (en) 1986-01-05
DE3573251D1 (en) 1989-11-02
DK160501C (da) 1991-08-26
HU193995B (en) 1987-12-28
EP0170090A1 (en) 1986-02-05
MX160445A (es) 1990-03-02
PT80773A (en) 1985-08-01
HK39790A (en) 1990-06-01
SU1508960A3 (ru) 1989-09-15
EP0170090B1 (en) 1989-09-27
SU1450742A3 (ru) 1989-01-07
FI852659L (fi) 1986-01-06
NZ212641A (en) 1988-10-28
CA1301150C (en) 1992-05-19
NO852699L (no) 1986-01-06
PT80773B (pt) 1987-10-20
NO171209C (no) 1993-02-10
AU578391B2 (en) 1988-10-20
FI83215B (fi) 1991-02-28
AU4451685A (en) 1986-01-09
ES544852A0 (es) 1987-04-01
HUT40132A (en) 1986-11-28
DK306885D0 (da) 1985-07-04
FI852659A0 (fi) 1985-07-04
US4668685A (en) 1987-05-26
FI83215C (fi) 1991-06-10
IL75721A (en) 1990-04-29
IL75721A0 (en) 1985-11-29
DK306885A (da) 1986-01-06
IE58136B1 (en) 1993-07-14
NO171209B (no) 1992-11-02

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Legal Events

Date Code Title Description
FD1A Patent lapsed

Effective date: 19970203