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
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- 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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Emergency Medicine (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (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)
- Hydrogenated Pyridines (AREA)
- Medicines Containing Plant Substances (AREA)
- Peptides Or Proteins (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 (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013503862A (ja) * | 2009-09-08 | 2013-02-04 | シグネーチャー セラピューティクス,インク. | 酵素切断可能なケトン修飾オピオイドプロドラッグとその任意選択のインヒビターとを含んでなる組成物 |
| US20110262355A1 (en) | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | 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 |
| CA2795222A1 (en) * | 2010-04-21 | 2011-10-27 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
| WO2011141490A1 (en) | 2010-05-10 | 2011-11-17 | Euro-Celtique S.A. | Combination of active loaded granules with additional actives |
| SG184523A1 (en) | 2010-05-10 | 2012-11-29 | Euro Celtique Sa | Pharmaceutical compositions comprising hydromorphone and naloxone |
| MX340188B (es) | 2010-05-10 | 2016-06-30 | Euro-Celtique S A * | Elaboracion de granulos sin activos y tabletas que comprenden los mismos. |
| AU2012205733B2 (en) * | 2011-01-11 | 2015-10-08 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
| EP2683394B1 (en) | 2011-03-09 | 2021-01-06 | Signature Therapeutics, Inc. | Active agent prodrugs with heterocyclic linkers |
| WO2012122420A2 (en) | 2011-03-09 | 2012-09-13 | Pharmacofore, Inc. | Opioid prodrugs with heterocyclic linkers |
| JP5977355B2 (ja) * | 2011-09-29 | 2016-08-24 | エコール ノルマル シュペリウール ドゥ リヨン | ペプチダーゼの蛍光発生基質 |
| IN2014DN03009A (es) | 2011-10-26 | 2015-05-08 | Kempharm Inc | |
| JP6232135B2 (ja) | 2013-11-13 | 2017-11-15 | ユーロ−セルティーク エス.エイ. | 疼痛およびオピオイドによる腸機能障害症候群の治療のためのヒドロモルホンおよびナロキソン |
| WO2015081891A1 (en) | 2013-12-06 | 2015-06-11 | Baikang (Suzhou) Co., Ltd | Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs |
| 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 |
| US11633492B2 (en) * | 2017-11-24 | 2023-04-25 | Byondis B.V. | Process for the synthesis of linker-drug vc-seco-DUBA |
| US10799496B2 (en) | 2018-07-13 | 2020-10-13 | Alkermes Pharma Ireland Limited | 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 |
| US10717712B2 (en) * | 2018-07-27 | 2020-07-21 | 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 |
| KR20230174213A (ko) | 2021-03-09 | 2023-12-27 | 엔사이스 바이오사이언시즈 인크. | 나파모스타트의 변형된 방출 조성물 및 그의 사용 방법 |
| CN117715632A (zh) | 2021-03-09 | 2024-03-15 | 恩赛斯生物科学股份有限公司 | 包含酶可裂解的前药和萘莫司他的组合物及其使用方法 |
| 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 |
| MX2024003466A (es) | 2021-09-29 | 2024-06-04 | Ensysce Biosciences Inc | Profarmacos de metadona escindibles por enzimas y metodos de uso de los mismos. |
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| US20110262355A1 (en) | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
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| CA2795222A1 (en) * | 2010-04-21 | 2011-10-27 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
| AU2012205733B2 (en) * | 2011-01-11 | 2015-10-08 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
| WO2012096886A1 (en) * | 2011-01-11 | 2012-07-19 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
| EP2683394B1 (en) * | 2011-03-09 | 2021-01-06 | Signature Therapeutics, Inc. | Active agent prodrugs with heterocyclic linkers |
| WO2012122420A2 (en) * | 2011-03-09 | 2012-09-13 | Pharmacofore, Inc. | Opioid prodrugs with heterocyclic linkers |
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2010
- 2010-04-21 JP JP2012527871A patent/JP2013503862A/ja active Pending
- 2010-04-21 AU AU2010293028A patent/AU2010293028B2/en active Active
- 2010-04-21 BR BR112012005124-5A patent/BR112012005124B1/pt active IP Right Grant
- 2010-04-21 SG SG2012016036A patent/SG179026A1/en unknown
- 2010-04-21 PH PH1/2012/500485A patent/PH12012500485A1/en unknown
- 2010-04-21 RU RU2012108874/04A patent/RU2600736C2/ru active
- 2010-04-21 EP EP10815769.4A patent/EP2475429B1/en active Active
- 2010-04-21 MX MX2012002847A patent/MX348262B/es active IP Right Grant
- 2010-04-21 CA CA2773340A patent/CA2773340C/en active Active
- 2010-04-21 CN CN201080048158.6A patent/CN102695545B/zh active Active
- 2010-04-21 WO PCT/US2010/031956 patent/WO2011031350A1/en not_active Ceased
- 2010-04-21 US US13/393,470 patent/US9493477B2/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
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| CN102695545B (zh) | 2016-08-17 |
| JP6778234B2 (ja) | 2020-10-28 |
| US9493477B2 (en) | 2016-11-15 |
| JP2018172387A (ja) | 2018-11-08 |
| JP2016041698A (ja) | 2016-03-31 |
| IL218498A (en) | 2017-03-30 |
| BR112012005124B1 (pt) | 2021-11-09 |
| EP2475429A4 (en) | 2013-04-03 |
| SG179026A1 (en) | 2012-04-27 |
| CA2773340A1 (en) | 2011-03-17 |
| BR112012005124A2 (pt) | 2020-08-25 |
| WO2011031350A1 (en) | 2011-03-17 |
| EP2475429A1 (en) | 2012-07-18 |
| RU2012108874A (ru) | 2013-09-20 |
| IL218498A0 (en) | 2012-07-31 |
| US20120230916A1 (en) | 2012-09-13 |
| AU2010293028B2 (en) | 2014-12-18 |
| RU2600736C2 (ru) | 2016-10-27 |
| CN102695545A (zh) | 2012-09-26 |
| US10028945B2 (en) | 2018-07-24 |
| PH12012500485A1 (en) | 2012-10-22 |
| US20170119754A1 (en) | 2017-05-04 |
| MX2012002847A (es) | 2012-08-23 |
| HK1172283A1 (zh) | 2013-04-19 |
| CA2773340C (en) | 2019-07-23 |
| AU2010293028A1 (en) | 2012-04-05 |
| EP2475429B1 (en) | 2015-07-29 |
| JP2013503862A (ja) | 2013-02-04 |
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