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
Links
- IYNWSQDZXMGGGI-NUEKZKHPSA-N 3-hydroxymorphinan Chemical class C1CCC[C@H]2[C@H]3CC4=CC=C(O)C=C4[C@]21CCN3 IYNWSQDZXMGGGI-NUEKZKHPSA-N 0.000 title abstract 3
- -1 benzoate ester Chemical class 0.000 title abstract 2
- 229940002612 prodrug Drugs 0.000 title abstract 2
- 239000000651 prodrug Substances 0.000 title abstract 2
- 239000000543 intermediate Substances 0.000 title 1
- 229940035676 analgesics Drugs 0.000 abstract 1
- 239000000730 antalgic agent Substances 0.000 abstract 1
- 239000003887 narcotic antagonist Substances 0.000 abstract 1
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)
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 (en:Method) |
EP (1) | EP0170090B1 (en:Method) |
AU (1) | AU578391B2 (en:Method) |
CA (1) | CA1301150C (en:Method) |
DE (1) | DE3573251D1 (en:Method) |
DK (1) | DK160501C (en:Method) |
ES (1) | ES8704443A1 (en:Method) |
FI (1) | FI83215C (en:Method) |
GR (1) | GR851653B (en:Method) |
HK (1) | HK39790A (en:Method) |
HU (1) | HU193995B (en:Method) |
IE (1) | IE58136B1 (en:Method) |
IL (1) | IL75721A (en:Method) |
MX (1) | MX160445A (en:Method) |
NO (1) | NO171209C (en:Method) |
NZ (1) | NZ212641A (en:Method) |
PT (1) | PT80773B (en:Method) |
SU (2) | SU1450742A3 (en:Method) |
Families Citing this family (51)
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 |
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 |
DK0577847T3 (da) * | 1992-01-23 | 1999-06-23 | Toray Industries | Morphinanderivat og medicinsk anvendelse deraf |
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 |
JP3843456B2 (ja) * | 1993-07-23 | 2006-11-08 | 東レ株式会社 | モルヒナン誘導体および医薬用途 |
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 |
DE69834268T2 (de) | 1997-12-22 | 2007-04-12 | Euro-Celtique S.A. | Peroral zu verabreichende Arzneiform enthaltend eine Kombination von einem Opioid Agonisten und Naltrexon |
US6375957B1 (en) | 1997-12-22 | 2002-04-23 | Euro-Celtique, S.A. | Opioid agonist/opioid antagonist/acetaminophen combinations |
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 |
AU2002331163B2 (en) * | 2001-08-23 | 2008-02-21 | Merck Sharp & Dohme B.V. | Process for the Preparation of a 14-hydroxynormorphinone Compound |
US20040033253A1 (en) * | 2002-02-19 | 2004-02-19 | Ihor Shevchuk | Acyl opioid antagonists |
EP1639997A1 (en) | 2002-04-05 | 2006-03-29 | Euro-Celtique S.A. | Matrix for sustained, invariant and independant 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 |
WO2006034343A2 (en) * | 2004-09-23 | 2006-03-30 | Alexander Michalow | methods for regulating neurotransmitter systems by inducing counteradaptationS |
BRPI0606339A2 (pt) * | 2005-01-28 | 2009-06-16 | Euro Celtique Sa | formas farmacêuticas resistentes a álcool |
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 |
CN101627014B (zh) * | 2007-03-09 | 2013-04-24 | 株式会社绿十字 | 用于预防或治疗帕金森病的(+)-3-羟基吗啡喃的口服可生物利用前药 |
EP2317991B1 (en) * | 2008-07-07 | 2017-05-03 | Euro-Celtique S.A. | Use of opioid antagonists for treating urinary retention |
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 |
US8623888B2 (en) * | 2009-07-15 | 2014-01-07 | Mallinckrodt Llc | 3-oxy-hydromorphone derivatives |
KR101486686B1 (ko) * | 2010-11-12 | 2015-01-26 | 시오노기세야쿠 가부시키가이샤 | 6,7-불포화-7-카르바모일 모르피난 유도체의 결정 및 그의 제조 방법 |
AU2012328837B2 (en) | 2011-10-26 | 2015-07-09 | Kempharm, Inc. | Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof |
JP2016525138A (ja) | 2013-07-23 | 2016-08-22 | ユーロ−セルティーク エス.エイ. | 疼痛および腸内ディスバイオシスをもたらす疾患および/または腸内細菌移行に対するリスクを高める疾患に罹患している患者における痛みの治療への使用のためのオキシコドンおよびナロキソンの組み合わせ |
US9850252B2 (en) | 2014-11-25 | 2017-12-26 | Kempharm, Inc. | Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxycodone, prodrugs, methods of making and use thereof |
US9682076B2 (en) | 2014-12-02 | 2017-06-20 | 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 |
WO2020012245A1 (en) | 2018-07-13 | 2020-01-16 | Alkermes Pharma Ireland Limited | Thienothiophene-naltrexone prodrugs for long-acting injectable compositions |
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 |
US10975099B2 (en) | 2018-11-05 | 2021-04-13 | Alkermes Pharma Ireland Limited | Thiophene compounds 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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE224197C (en:Method) * | ||||
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 |
-
1985
- 1985-05-14 US US06/733,464 patent/US4668685A/en not_active Expired - Lifetime
- 1985-06-27 CA CA000485661A patent/CA1301150C/en not_active Expired - Lifetime
- 1985-07-03 EP EP85108258A patent/EP0170090B1/en not_active Expired
- 1985-07-03 AU AU44516/85A patent/AU578391B2/en not_active Ceased
- 1985-07-03 DE DE8585108258T patent/DE3573251D1/de not_active Expired
- 1985-07-04 NZ NZ212641A patent/NZ212641A/xx unknown
- 1985-07-04 SU SU853920678A patent/SU1450742A3/ru active
- 1985-07-04 PT PT80773A patent/PT80773B/pt not_active IP Right Cessation
- 1985-07-04 IE IE168385A patent/IE58136B1/en not_active IP Right Cessation
- 1985-07-04 DK DK306885A patent/DK160501C/da not_active IP Right Cessation
- 1985-07-04 ES ES544852A patent/ES8704443A1/es not_active Expired
- 1985-07-04 IL IL75721A patent/IL75721A/xx not_active IP Right Cessation
- 1985-07-04 NO NO852699A patent/NO171209C/no unknown
- 1985-07-04 GR GR851653A patent/GR851653B/el unknown
- 1985-07-04 FI FI852659A patent/FI83215C/fi not_active IP Right Cessation
- 1985-07-04 HU HU852607A patent/HU193995B/hu not_active IP Right Cessation
- 1985-07-05 MX MX6144A patent/MX160445A/es unknown
-
1987
- 1987-07-03 SU SU874202841A patent/SU1508960A3/ru active
-
1990
- 1990-05-24 HK HK397/90A patent/HK39790A/xx unknown
Also Published As
Publication number | Publication date |
---|---|
EP0170090A1 (en) | 1986-02-05 |
IE58136B1 (en) | 1993-07-14 |
DK160501C (da) | 1991-08-26 |
AU4451685A (en) | 1986-01-09 |
HUT40132A (en) | 1986-11-28 |
ES544852A0 (es) | 1987-04-01 |
MX160445A (es) | 1990-03-02 |
HK39790A (en) | 1990-06-01 |
DE3573251D1 (en) | 1989-11-02 |
GR851653B (en:Method) | 1985-11-26 |
DK160501B (da) | 1991-03-18 |
NZ212641A (en) | 1988-10-28 |
US4668685A (en) | 1987-05-26 |
NO852699L (no) | 1986-01-06 |
FI852659L (fi) | 1986-01-06 |
HU193995B (en) | 1987-12-28 |
SU1508960A3 (ru) | 1989-09-15 |
IE851683L (en) | 1986-01-05 |
CA1301150C (en) | 1992-05-19 |
NO171209C (no) | 1993-02-10 |
IL75721A0 (en) | 1985-11-29 |
NO171209B (no) | 1992-11-02 |
SU1450742A3 (ru) | 1989-01-07 |
IL75721A (en) | 1990-04-29 |
FI83215B (fi) | 1991-02-28 |
FI83215C (fi) | 1991-06-10 |
PT80773A (en) | 1985-08-01 |
PT80773B (pt) | 1987-10-20 |
DK306885A (da) | 1986-01-06 |
AU578391B2 (en) | 1988-10-20 |
DK306885D0 (da) | 1985-07-04 |
EP0170090B1 (en) | 1989-09-27 |
FI852659A0 (fi) | 1985-07-04 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FD1A | Patent lapsed |
Effective date: 19970203 |