AU578391B2 - Substituted benzoate ester prodrug derivatives of 3- hydroxymorphinans, intermediates thereto, and processes - Google Patents

Substituted benzoate ester prodrug derivatives of 3- hydroxymorphinans, intermediates thereto, and processes

Info

Publication number
AU578391B2
AU578391B2 AU44516/85A AU4451685A AU578391B2 AU 578391 B2 AU578391 B2 AU 578391B2 AU 44516/85 A AU44516/85 A AU 44516/85A AU 4451685 A AU4451685 A AU 4451685A AU 578391 B2 AU578391 B2 AU 578391B2
Authority
AU
Australia
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.)
Ceased
Application number
AU44516/85A
Other languages
English (en)
Other versions
AU4451685A (en
Inventor
Elie Gabriel Shami
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.)
Bristol Myers Squibb Pharma Co
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 AU4451685A publication Critical patent/AU4451685A/en
Application granted granted Critical
Publication of AU578391B2 publication Critical patent/AU578391B2/en
Assigned to DU PONT MERCK PHARMACEUTICAL COMPANY, THE reassignment DU PONT MERCK PHARMACEUTICAL COMPANY, THE Alteration of Name(s) in Register under S187 Assignors: E.I. DU PONT DE NEMOURS AND COMPANY
Anticipated expiration legal-status Critical
Ceased 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)
AU44516/85A 1984-07-05 1985-07-03 Substituted benzoate ester prodrug derivatives of 3- hydroxymorphinans, intermediates thereto, and processes Ceased AU578391B2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US62792384A 1984-07-05 1984-07-05
US627923 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
US733464 1985-05-14

Publications (2)

Publication Number Publication Date
AU4451685A AU4451685A (en) 1986-01-09
AU578391B2 true AU578391B2 (en) 1988-10-20

Family

ID=27090564

Family Applications (1)

Application Number Title Priority Date Filing Date
AU44516/85A Ceased AU578391B2 (en) 1984-07-05 1985-07-03 Substituted benzoate ester prodrug derivatives of 3- hydroxymorphinans, intermediates thereto, and processes

Country Status (18)

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

Families Citing this family (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4673679A (en) * 1986-05-14 1987-06-16 E. I. Du Pont De Nemours And Company Use of prodrugs of 3-hydroxymorphinans to prevent bitter taste upon buccal, nasal or sublingual administration
DK107688D0 (da) * 1988-03-01 1988-03-01 Novo Industri As Carbaminsyreestere af substituerede 7-hydroxy-2,3,4,5-tetrahydro-1h-3-benzazepiner
US6702705B1 (en) 1988-05-04 2004-03-09 Igen International, Inc. Prodrugs activated by targeted catalytic proteins
DK24089D0 (da) * 1989-01-20 1989-01-20 Hans Bundgaard Novel prodrug derivatives of biologically active agents containing hydroxyl groups or nh-acidic groups
US6258360B1 (en) * 1989-05-04 2001-07-10 Igen International, Inc. Prodrugs activated by targeted catalytic proteins
JPH06510529A (ja) * 1991-08-05 1994-11-24 イゲン，インコーポレーテッド 目標とする触媒性たんぱく質により活性化されるプロドラッグ
US5968551A (en) * 1991-12-24 1999-10-19 Purdue Pharma L.P. Orally administrable opioid formulations having extended duration of effect
DE69321525T2 (de) * 1992-01-23 1999-03-04 Toray Industries, Inc., Tokio/Tokyo Morphinan-derivate und medizinische verwendung
TW372972B (en) * 1992-10-23 1999-11-01 Novartis Ag Antiretroviral acyl compounds
EP0615756B1 (en) * 1993-03-15 2001-06-27 National Science Council Nalbuphine esters and long-acting pharmaceutical compositions containing them
NZ268969A (en) * 1993-07-23 1997-06-24 Toray Industries Morphinan derivatives and pharmaceutical compositions
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
US6375957B1 (en) 1997-12-22 2002-04-23 Euro-Celtique, S.A. Opioid agonist/opioid antagonist/acetaminophen combinations
AU773642C (en) 1997-12-22 2006-04-06 Mundipharma Pty Limited Opioid agonist/antagonist combinations
ES2188481T3 (es) * 2000-04-27 2003-07-01 Oliver Yoa-Pu Hu Derivados de polinalbufina.
US6569449B1 (en) 2000-11-13 2003-05-27 University Of Kentucky Research Foundation Transdermal delivery of opioid antagonist prodrugs
CN1525851A (zh) 2001-05-11 2004-09-01 ������ҩ�����޹�˾ 抗滥用阿片样物质控释剂型
WO2003018588A2 (en) * 2001-08-23 2003-03-06 Akzo Nobel N.V. Process for the preparation of a 14-hydroxynormorphinone derivative
US20040033253A1 (en) * 2002-02-19 2004-02-19 Ihor Shevchuk Acyl opioid antagonists
EP2316428A1 (en) 2002-04-05 2011-05-04 Euro-Celtique S.A. Matrix for sustained, invariant and independent release of active compounds
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)
US20080045610A1 (en) * 2004-09-23 2008-02-21 Alexander Michalow Methods for regulating neurotransmitter systems by inducing counteradaptations
AU2005286733B2 (en) * 2004-09-23 2009-11-05 Alexander Michalow Methods for regulating neurotransmitter systems by inducing counteradaptations
AP2274A (en) * 2005-01-28 2011-08-19 Euro Celtiques Sa Alcohol resistant dosage forms.
EP1695700A1 (en) * 2005-02-28 2006-08-30 Euro-Celtique S.A. Dosage form containing oxycodone and naloxone
EP1702558A1 (en) * 2005-02-28 2006-09-20 Euro-Celtique S.A. Method and device for the assessment of bowel function
WO2006126529A1 (ja) * 2005-05-25 2006-11-30 Shionogi & Co., Ltd. ６，７－不飽和－７－カルバモイル置換モルヒナン誘導体
EP1928881A2 (en) 2005-08-19 2008-06-11 Pharmacofore, 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.
KR20130105935A (ko) * 2008-07-07 2013-09-26 유로-셀티큐 에스.에이. 요폐의 치료를 위한 아편유사제 길항제의 용도
KR20140141727A (ko) 2009-03-10 2014-12-10 유로-셀티큐 에스.에이. 옥시코돈 및 날록손을 포함하는 즉시 방출 제약 조성물
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
WO2011008636A1 (en) * 2009-07-15 2011-01-20 Mallinckrodt Inc. 3-oxy-hydromorphone derivatives
EP3560929B1 (en) 2010-11-12 2021-05-19 Shionogi & Co., Ltd Process for preparing 6,7-unsaturated-7-carbamoyl morphinane derivative, and intermediate
JP5769889B2 (ja) 2011-10-26 2015-08-26 ケムファーム・インコーポレーテッド ヒドロモルホンの安息香酸、安息香酸誘導体及びヘテロアリールカルボン酸結合体、そのプロドラッグ、製造法及び使用
WO2015011189A1 (en) 2013-07-23 2015-01-29 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
NZ731591A (en) 2014-11-25 2018-06-29 Kempharm Inc Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxycodone
NZ731586A (en) 2014-12-02 2018-06-29 Kempharm Inc 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
WO2020012248A1 (en) 2018-07-13 2020-01-16 Alkermes Pharma Ireland Limited Novel naphthylenyl compounds for long-acting injectable compositions and related methods
US10807995B2 (en) 2018-07-13 2020-10-20 Alkermes Pharma Ireland Limited Thienothiophene 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
CN114828961B (zh) 2019-08-11 2024-03-29 卡帕制药有限责任公司 通过阿片类己二烯酸酯和任选取代的己二烯酸酯增强阿片受体结合的组合物及方法

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE224197C (enExample) *
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
CH543514A (de) * 1967-08-25 1973-10-31 Hoffmann La Roche Verfahren zur Herstellung von Morphinanderivaten
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
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
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
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
IL75721A (en) 1990-04-29
AU4451685A (en) 1986-01-09
HK39790A (en) 1990-06-01
FI852659L (fi) 1986-01-06
US4668685A (en) 1987-05-26
DK160501C (da) 1991-08-26
EP0170090A1 (en) 1986-02-05
GR851653B (enExample) 1985-11-26
ES544852A0 (es) 1987-04-01
HUT40132A (en) 1986-11-28
NZ212641A (en) 1988-10-28
IE851683L (en) 1986-01-05
NO171209B (no) 1992-11-02
EP0170090B1 (en) 1989-09-27
FI83215B (fi) 1991-02-28
HU193995B (en) 1987-12-28
IL75721A0 (en) 1985-11-29
PT80773B (pt) 1987-10-20
NO852699L (no) 1986-01-06
SU1450742A3 (ru) 1989-01-07
DK306885D0 (da) 1985-07-04
FI83215C (fi) 1991-06-10
MX160445A (es) 1990-03-02
DE3573251D1 (en) 1989-11-02
FI852659A0 (fi) 1985-07-04
DK160501B (da) 1991-03-18
IE58136B1 (en) 1993-07-14
NO171209C (no) 1993-02-10
SU1508960A3 (ru) 1989-09-15
ES8704443A1 (es) 1987-04-01
PT80773A (en) 1985-08-01
DK306885A (da) 1986-01-06
CA1301150C (en) 1992-05-19

Similar Documents

Publication Publication Date Title
AU578391B2 (en) Substituted benzoate ester prodrug derivatives of 3- hydroxymorphinans, intermediates thereto, and processes
AU5647686A (en) Intermediates in the synthesis of acyltripeptide immunostimulants
AU1117788A (en) Benzoxazone derivatives
AU4982185A (en) Novel 5-amino-4-hydroxyvaleryl derivatives
AU4673685A (en) Derivatives of methylene-bisphosphonic acid
AU4584885A (en) Substituted propargyloxyacetonitrile derivatives
AU582381B2 (en) Aethylenediamine monoamide derivatives
AU2504188A (en) Novel intermediates of cephalosporin derivatives
AU4912090A (en) Intermediates useful in the synthesis of 2-oxy-4h-3, 1-benzoxazin-4-one derivative
AU558388B2 (en) Production of n-acylphenylalanines
GB8415092D0 (en) Ester derivatives
AU3797485A (en) Azolyl-aryl-alkanol derivatives
AU4332285A (en) Protection of infra-radiating targets
AU577883B2 (en) Amide derivatives
AU1258988A (en) Esters of oxalofluoride
AU552478B2 (en) Ester derivatives of oxicams
AU4272685A (en) Pyrazolin-5-one derivatives
AU7254087A (en) Alditol ester derivatives of triclopyr
AU5106585A (en) Anilide derivatives of substituted arylaceticacids
AU4901285A (en) 2 - cyanobenzimidazole derivatives
ZA855058B (en) Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans,intermediates thereto,and processes
AU586280B2 (en) Increasing the yield of cereals by means of brassinolide derivatives
AU572611B2 (en) Preparation of derivatives of carbamic acid
AU588795B2 (en) New phenylpropargylamine derivatives
EP0158957A3 (en) Allophanic-acid ester derivatives