MX348262B - Composiciones que comprenden profarmacos opioides con una cetona modificada que se pueden escindir enzimaticamente e inhibidores opcionales de estos. - Google Patents
Composiciones que comprenden profarmacos opioides con una cetona modificada que se pueden escindir enzimaticamente e inhibidores opcionales de estos.Info
- Publication number
- MX348262B MX348262B MX2012002847A MX2012002847A MX348262B MX 348262 B MX348262 B MX 348262B MX 2012002847 A MX2012002847 A MX 2012002847A MX 2012002847 A MX2012002847 A MX 2012002847A MX 348262 B MX348262 B MX 348262B
- Authority
- MX
- Mexico
- Prior art keywords
- enzyme
- ketone
- compositions
- prodrug
- modified opioid
- Prior art date
Links
- 239000000651 prodrug Substances 0.000 title abstract 5
- 229940002612 prodrug Drugs 0.000 title abstract 5
- 239000003112 inhibitor Substances 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 150000002576 ketones Chemical class 0.000 abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 abstract 3
- 238000013270 controlled release Methods 0.000 abstract 2
- 230000002255 enzymatic effect Effects 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 238000003776 cleavage reaction Methods 0.000 abstract 1
- 229940125532 enzyme inhibitor Drugs 0.000 abstract 1
- 239000002532 enzyme inhibitor Substances 0.000 abstract 1
- 238000003402 intramolecular cyclocondensation reaction Methods 0.000 abstract 1
- 230000007017 scission Effects 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/05—Dipeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Emergency Medicine (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Peptides Or Proteins (AREA)
- Medicines Containing Plant Substances (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
Se describe un método para proporcionar un paciente con liberación controlada de opoide que contienen cetona utilizando un profármaco capaz, tras la activación enzimática y ciclación intramolecular, de liberar el opioide que contiene cetona. La descripción también proporciona tales compuestos de profármacos y composiciones farmacéuticas que comprenden tales compuestos. Tales composiciones farmacéuticas pueden incluir opcionalmente un inhibidor enzimático que interactúa con las enzimas para mediar la liberación controlada enzimáticamente del opioide que contiene cetona del profármaco así como para modificar la separación enzimática del profármaco. También se incluyen métodos para usar tales compuestos y composiciones farmacéuticas.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24061109P | 2009-09-08 | 2009-09-08 | |
| US28814809P | 2009-12-18 | 2009-12-18 | |
| PCT/US2010/031956 WO2011031350A1 (en) | 2009-09-08 | 2010-04-21 | Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2012002847A MX2012002847A (es) | 2012-08-23 |
| MX348262B true MX348262B (es) | 2017-06-05 |
Family
ID=43732738
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2012002847A MX348262B (es) | 2009-09-08 | 2010-04-21 | Composiciones que comprenden profarmacos opioides con una cetona modificada que se pueden escindir enzimaticamente e inhibidores opcionales de estos. |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US9493477B2 (es) |
| EP (1) | EP2475429B1 (es) |
| JP (3) | JP2013503862A (es) |
| CN (1) | CN102695545B (es) |
| AU (1) | AU2010293028B2 (es) |
| BR (1) | BR112012005124B1 (es) |
| CA (1) | CA2773340C (es) |
| IL (1) | IL218498A (es) |
| MX (1) | MX348262B (es) |
| PH (1) | PH12012500485A1 (es) |
| RU (1) | RU2600736C2 (es) |
| SG (1) | SG179026A1 (es) |
| WO (1) | WO2011031350A1 (es) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102695545B (zh) * | 2009-09-08 | 2016-08-17 | 特色疗法股份有限公司 | 包括酶可剪切的酮改性的阿片样物质药物前体以及其可任选的抑制剂的组合物 |
| CA2795222A1 (en) * | 2010-04-21 | 2011-10-27 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
| US20130059914A1 (en) | 2010-04-21 | 2013-03-07 | Signature Therapeutics, Inc. | Compositions Comprising Enzyme-Cleavable Amphetamine Prodrugs and Inhibitors Thereof |
| US20110262355A1 (en) | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
| US9700508B2 (en) | 2010-05-10 | 2017-07-11 | Euro-Celtique S.A. | Pharmaceutical compositions comprising hydromorphone and naloxone |
| PH12012502083A1 (en) | 2010-05-10 | 2017-07-26 | Euro Celtique Sa | Manufacturing of active-free granules and tablets comprising the same |
| EP2568965A1 (en) | 2010-05-10 | 2013-03-20 | Euro-Celtique S.A. | Combination of active loaded granules with additional actives |
| AU2012205733B2 (en) * | 2011-01-11 | 2015-10-08 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
| WO2012122420A2 (en) | 2011-03-09 | 2012-09-13 | Pharmacofore, Inc. | Opioid prodrugs with heterocyclic linkers |
| JP6148182B2 (ja) | 2011-03-09 | 2017-06-14 | シグネーチャー セラピューティクス, インク.Signature Therapeutics, Inc. | 複素環式リンカーを有する活性薬剤プロドラッグ |
| US9605296B2 (en) * | 2011-09-29 | 2017-03-28 | Ecole Normale Superieure De Lyon | Fluorogenic peptidase substrate |
| SG11201401856VA (en) | 2011-10-26 | 2014-05-29 | Kempharm Inc | Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof |
| WO2015071380A1 (en) | 2013-11-13 | 2015-05-21 | Euro-Celtique S.A. | Hydromorphone and naloxone for treatment of pain and opioid bowel dysfunction syndrome |
| US10626156B2 (en) | 2013-12-06 | 2020-04-21 | Jie Han | Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs |
| RU2683274C2 (ru) | 2014-12-02 | 2019-03-27 | Кемфарм, Инк. | Бензойная кислота, производные бензойной кислоты и конъюгаты гетероарилкарбоновой кислоты и оксиморфона, их пролекарства, способы получения и применение |
| PT3713939T (pt) * | 2017-11-24 | 2021-09-16 | Byondis Bv | Processo melhorado para a síntese de fármaco ligante vcseco- duba |
| 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 |
| WO2020023794A1 (en) * | 2018-07-27 | 2020-01-30 | Concentric Analgesics, Inc. | Pegylated prodrugs of phenolic trpv1 agonists |
| US10975099B2 (en) | 2018-11-05 | 2021-04-13 | Alkermes Pharma Ireland Limited | Thiophene compounds for long-acting injectable compositions and related methods |
| IL305493A (en) | 2021-03-09 | 2023-10-01 | Ensysce Biosciences Inc | Compositions comprising enzyme-cleavable prodrugs and controlled release nafamostat and methods of use thereof |
| CN113624665A (zh) * | 2021-07-30 | 2021-11-09 | 中国药科大学 | 一种抗肿瘤候选化合物在治疗结直肠癌药物中的应用及测定方法 |
| CA3230025A1 (en) | 2021-09-29 | 2023-04-06 | Lynn Kirkpatrick | Enzyme-cleavable methadone prodrugs and methods of use thereof |
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| BRPI1015108A2 (pt) | 2009-04-02 | 2016-04-26 | Shire Llc | pró-fármacos de aminoácidos e peptídios ligados a ácido dicarboxílico de opiáceos e seus usos |
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| CN102695545B (zh) * | 2009-09-08 | 2016-08-17 | 特色疗法股份有限公司 | 包括酶可剪切的酮改性的阿片样物质药物前体以及其可任选的抑制剂的组合物 |
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| US20110262355A1 (en) * | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
| US20110262360A1 (en) | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions Comprising Enzyme-Cleavable Phenol-Modified Opioid Prodrugs and Inhibitors Thereof |
| CA2795222A1 (en) * | 2010-04-21 | 2011-10-27 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
| US8497237B2 (en) | 2011-01-11 | 2013-07-30 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
| AU2012205733B2 (en) | 2011-01-11 | 2015-10-08 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
| JP6148182B2 (ja) * | 2011-03-09 | 2017-06-14 | シグネーチャー セラピューティクス, インク.Signature Therapeutics, Inc. | 複素環式リンカーを有する活性薬剤プロドラッグ |
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-
2010
- 2010-04-21 CN CN201080048158.6A patent/CN102695545B/zh active Active
- 2010-04-21 JP JP2012527871A patent/JP2013503862A/ja active Pending
- 2010-04-21 AU AU2010293028A patent/AU2010293028B2/en active Active
- 2010-04-21 US US13/393,470 patent/US9493477B2/en active Active
- 2010-04-21 BR BR112012005124-5A patent/BR112012005124B1/pt active IP Right Grant
- 2010-04-21 WO PCT/US2010/031956 patent/WO2011031350A1/en not_active Ceased
- 2010-04-21 EP EP10815769.4A patent/EP2475429B1/en active Active
- 2010-04-21 PH PH1/2012/500485A patent/PH12012500485A1/en unknown
- 2010-04-21 MX MX2012002847A patent/MX348262B/es active IP Right Grant
- 2010-04-21 SG SG2012016036A patent/SG179026A1/en unknown
- 2010-04-21 RU RU2012108874/04A patent/RU2600736C2/ru active
- 2010-04-21 CA CA2773340A patent/CA2773340C/en active Active
-
2012
- 2012-03-06 IL IL218498A patent/IL218498A/en active IP Right Grant
-
2015
- 2015-09-29 JP JP2015190867A patent/JP2016041698A/ja active Pending
-
2016
- 2016-10-05 US US15/285,818 patent/US10028945B2/en active Active
-
2018
- 2018-05-25 JP JP2018100108A patent/JP6778234B2/ja active Active
Also Published As
| Publication number | Publication date |
|---|---|
| AU2010293028B2 (en) | 2014-12-18 |
| US20120230916A1 (en) | 2012-09-13 |
| MX2012002847A (es) | 2012-08-23 |
| BR112012005124A2 (pt) | 2020-08-25 |
| AU2010293028A1 (en) | 2012-04-05 |
| WO2011031350A1 (en) | 2011-03-17 |
| BR112012005124B1 (pt) | 2021-11-09 |
| EP2475429A4 (en) | 2013-04-03 |
| SG179026A1 (en) | 2012-04-27 |
| JP2013503862A (ja) | 2013-02-04 |
| JP2018172387A (ja) | 2018-11-08 |
| JP6778234B2 (ja) | 2020-10-28 |
| US9493477B2 (en) | 2016-11-15 |
| HK1172283A1 (zh) | 2013-04-19 |
| CN102695545A (zh) | 2012-09-26 |
| RU2012108874A (ru) | 2013-09-20 |
| CA2773340A1 (en) | 2011-03-17 |
| PH12012500485A1 (en) | 2012-10-22 |
| EP2475429B1 (en) | 2015-07-29 |
| RU2600736C2 (ru) | 2016-10-27 |
| US20170119754A1 (en) | 2017-05-04 |
| CA2773340C (en) | 2019-07-23 |
| IL218498A (en) | 2017-03-30 |
| CN102695545B (zh) | 2016-08-17 |
| JP2016041698A (ja) | 2016-03-31 |
| US10028945B2 (en) | 2018-07-24 |
| EP2475429A1 (en) | 2012-07-18 |
| IL218498A0 (en) | 2012-07-31 |
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