DE3573251D1 - 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
DE3573251D1
DE3573251D1 DE8585108258T DE3573251T DE3573251D1 DE 3573251 D1 DE3573251 D1 DE 3573251D1 DE 8585108258 T DE8585108258 T DE 8585108258T DE 3573251 T DE3573251 T DE 3573251T DE 3573251 D1 DE3573251 D1 DE 3573251D1
Authority
DE
Germany
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
DE8585108258T
Other languages
German (de)
English (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
Application granted granted Critical
Publication of DE3573251D1 publication Critical patent/DE3573251D1/de
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)
DE8585108258T 1984-07-05 1985-07-03 Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans, intermediates thereto, and processes Expired DE3573251D1 (en)

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 (1)

Publication Number Publication Date
DE3573251D1 true DE3573251D1 (en) 1989-11-02

Family

ID=27090564

Family Applications (1)

Application Number Title Priority Date Filing Date
DE8585108258T Expired DE3573251D1 (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 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EP (1) EP0170090B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AU (1) AU578391B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CA (1) CA1301150C (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
DE (1) DE3573251D1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
DK (1) DK160501C (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ES (1) ES8704443A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
FI (1) FI83215C (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
GR (1) GR851653B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
HK (1) HK39790A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
HU (1) HU193995B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IE (1) IE58136B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IL (1) IL75721A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MX (1) MX160445A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
NO (1) NO171209C (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
NZ (1) NZ212641A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PT (1) PT80773B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
SU (2) SU1450742A3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)

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
KR100334695B1 (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
KR970011390B1 (ko) * 1992-01-23 1997-07-10 도레이 가부시키가이샤 모르피난 유도체와 약리학적으로 허용되는 이의 산 부가염 및 이를 함유하는 약제학적 조성물
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
CA2143864C (en) * 1993-07-23 2006-01-24 Hiroshi Nagase Morphinan derivatives and pharmaceutical use thereof
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
EP2266564B1 (en) 1997-12-22 2013-03-13 Euro-Celtique S.A. Pharmaceutical oral dosage form comprising a combination of an opioid agonist and an opioid antagonist
EP1149836B1 (en) * 2000-04-27 2003-02-26 Oliver Yoa-Pu Hu Polynalbuphine derivatives
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
CN1271072C (zh) * 2001-08-23 2006-08-23 阿克佐诺贝尔公司 14－羟基去吗啡酮衍生物的制备方法
US20040033253A1 (en) * 2002-02-19 2004-02-19 Ihor Shevchuk Acyl opioid antagonists
SI1492505T1 (sl) * 2002-04-05 2015-10-30 Euro-Celtique S.A. Farmacevtski pripravek, ki vsebuje oksikodon in nalokson
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
EP1809104A4 (en) * 2004-09-23 2009-04-29 Alexander Michalow METHODS FOR REGULATING NEUROTRANSMITTER SYSTEMS BY INDUCING COUNTER-ADAPTATIONS
EP2319499A1 (en) * 2005-01-28 2011-05-11 Euro-Celtique S.A. Alcohol resistant dosage forms
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
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
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.
KR20130105935A (ko) * 2008-07-07 2013-09-26 유로-셀티큐 에스.에이. 요폐의 치료를 위한 아편유사제 길항제의 용도
SMT201900023T1 (it) 2009-03-10 2019-02-28 Euro Celtique Sa Composizioni farmaceutiche a rilascio immediato comprendenti ossicodone e naloxone
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
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
WO2011008636A1 (en) * 2009-07-15 2011-01-20 Mallinckrodt Inc. 3-oxy-hydromorphone derivatives
AU2011327113B9 (en) * 2010-11-12 2015-07-30 Shionogi & Co., Ltd. Crystalline 6,7-unsaturated-7-carbamoyl morphinane derivative, and method for producing same
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
UA116567C2 (uk) 2013-07-23 2018-04-10 Євро-Селтік С.А. Комбінація оксикодону та налоксону для застосування в лікуванні болю у пацієнтів, які страждають від болю та захворювання, що призводить до дисбактеріозу кишечнику та/або підвищує ризик кишкової бактеріальної транслокації
NZ731591A (en) 2014-11-25 2018-06-29 Kempharm Inc Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxycodone
HK1244209A1 (zh) 2014-12-02 2018-08-03 Kempharm, Inc. 羟吗啡酮的苯甲酸缀合物、苯甲酸衍生物缀合物和杂芳基羧酸缀合物、其前药、制备和使用方法
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
WO2020012245A1 (en) 2018-07-13 2020-01-16 Alkermes Pharma Ireland Limited Thienothiophene-naltrexone prodrugs for long-acting injectable compositions
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
US10975099B2 (en) 2018-11-05 2021-04-13 Alkermes Pharma Ireland Limited Thiophene compounds 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 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) *
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
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
AU578391B2 (en) 1988-10-20
US4668685A (en) 1987-05-26
EP0170090B1 (en) 1989-09-27
HK39790A (en) 1990-06-01
SU1450742A3 (ru) 1989-01-07
FI852659L (fi) 1986-01-06
SU1508960A3 (ru) 1989-09-15
IL75721A (en) 1990-04-29
NO171209B (no) 1992-11-02
NO171209C (no) 1993-02-10
PT80773A (en) 1985-08-01
DK160501C (da) 1991-08-26
CA1301150C (en) 1992-05-19
DK306885A (da) 1986-01-06
HUT40132A (en) 1986-11-28
EP0170090A1 (en) 1986-02-05
HU193995B (en) 1987-12-28
FI852659A0 (fi) 1985-07-04
IE851683L (en) 1986-01-05
NZ212641A (en) 1988-10-28
ES8704443A1 (es) 1987-04-01
IL75721A0 (en) 1985-11-29
FI83215C (fi) 1991-06-10
IE58136B1 (en) 1993-07-14
PT80773B (pt) 1987-10-20
GR851653B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 1985-11-26
MX160445A (es) 1990-03-02
AU4451685A (en) 1986-01-09
ES544852A0 (es) 1987-04-01
NO852699L (no) 1986-01-06
FI83215B (fi) 1991-02-28
DK306885D0 (da) 1985-07-04
DK160501B (da) 1991-03-18

Similar Documents

Publication Publication Date Title
DE3573251D1 (en) Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans, intermediates thereto, and processes
PL265523A1 (en) Method of obtaining novel derivatives of allanilproline
GB8415092D0 (en) Ester derivatives
IL84951A (en) Derivatives of 3-oxobutaneamide as intermediates for the preparation of pyrrolidone derivatives
PL255499A1 (en) Method of obtaining novel derivatives of quinazolinodione
PL253089A1 (en) Method of obtaining novel derivatives of iminotriazolidine
AU552478B2 (en) Ester derivatives of oxicams
ZA855058B (en) Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans,intermediates thereto,and processes
AU5106585A (en) Anilide derivatives of substituted arylaceticacids
GB8616293D0 (en) Isomaleimide & isophthalimide derivatives of chromophors
PL257564A1 (en) Method of obtaining novel derivatives of thiocyanopyrimidine
EP0173960A3 (en) Muramylpeptide active ester derivatives
PL265906A1 (en) Method of obtaining novel derivatives of bromine dichloroimidazole
GB2176189B (en) Derivatives of 11-desoxy-17a-oxicorticosterone
ZA826339B (en) Ester derivatives of n-arylsulfinyl-n-phosphonomethylglycinates
PL254117A1 (en) Method of obtaining novel derivatives of oxycames
EP0158957A3 (en) Allophanic-acid ester derivatives
ZA85240B (en) Esters of cephalosporin derivatives
ZA826338B (en) Ester derivatives of n-arylsufinyl-n-phosphonomethylglycinonitrile
PL256440A1 (en) Method of obtaining novel nitrogen derivatives of keto compounds
PL252772A1 (en) Method of obtaining novel derivatives of 1-phenylindole
PL255588A1 (en) Method of obtaining novel derivatives of iminacetamide
PL257892A1 (en) Method of obtaining novel derivatives of 2-oxindolo-1-carbonamide
PL256441A1 (en) Method of obtaining novel alkylidenedioylic derivatives
GB8517570D0 (en) Protection of tubular steel structures

Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8327 Change in the person/name/address of the patent owner

Owner name: THE DU PONT MERCK PHARMACEUTICAL CO., WILMINGTON,

8328 Change in the person/name/address of the agent

Free format text: VON KREISLER, A., DIPL.-CHEM. SELTING, G., DIPL.-ING. WERNER, H., DIPL.-CHEM. DR.RER.NAT. FUES, J., DIPL.-CHEM. DR.RER.NAT. BOECKMANN GEN. DALLMEYER, G., DIPL.-ING. HILLERINGMANN, J., DIPL.-ING. JOENSSON, H., DIPL.-CHEM. DR.RER.NAT. MEYERS, H., DIPL.-CHEM. DR.RER.NAT., PAT.-ANWAELTE, 5000 KOELN

8339 Ceased/non-payment of the annual fee