IL228215B - Active agent prodrugs with heterocyclic linkers - Google Patents
Active agent prodrugs with heterocyclic linkersInfo
- Publication number
- IL228215B IL228215B IL228215A IL22821513A IL228215B IL 228215 B IL228215 B IL 228215B IL 228215 A IL228215 A IL 228215A IL 22821513 A IL22821513 A IL 22821513A IL 228215 B IL228215 B IL 228215B
- Authority
- IL
- Israel
- Prior art keywords
- active agent
- heterocyclic linkers
- agent prodrugs
- prodrugs
- linkers
- Prior art date
Links
- 239000013543 active substance Substances 0.000 title 1
- 229940002612 prodrug Drugs 0.000 title 1
- 239000000651 prodrug Substances 0.000 title 1
Classifications
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06086—Dipeptides with the first amino acid being basic
- C07K5/06095—Arg-amino acid
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
- A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
-
- 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
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/06—Tripeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61K47/62—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 a protein, peptide or polyamino acid
- A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/94—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving narcotics or drugs or pharmaceuticals, neurotransmitters or associated receptors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Gastroenterology & Hepatology (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Neurosurgery (AREA)
- Addiction (AREA)
- Food Science & Technology (AREA)
- Analytical Chemistry (AREA)
- Cell Biology (AREA)
- Pathology (AREA)
- Microbiology (AREA)
- Biotechnology (AREA)
- General Physics & Mathematics (AREA)
- Physics & Mathematics (AREA)
- Crystallography & Structural Chemistry (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161451019P | 2011-03-09 | 2011-03-09 | |
| US201261583523P | 2012-01-05 | 2012-01-05 | |
| PCT/US2012/028367 WO2012122422A2 (en) | 2011-03-09 | 2012-03-08 | Active agent prodrugs with heterocyclic linkers |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL228215B true IL228215B (en) | 2019-01-31 |
Family
ID=46798816
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL228215A IL228215B (en) | 2011-03-09 | 2013-09-01 | Active agent prodrugs with heterocyclic linkers |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US9139612B2 (enExample) |
| EP (1) | EP2683394B1 (enExample) |
| JP (1) | JP6148182B2 (enExample) |
| CN (1) | CN103813800B (enExample) |
| AU (1) | AU2012225337B2 (enExample) |
| BR (1) | BR112013022946A2 (enExample) |
| CA (1) | CA2827662C (enExample) |
| IL (1) | IL228215B (enExample) |
| RU (1) | RU2608305C2 (enExample) |
| WO (1) | WO2012122422A2 (enExample) |
Families Citing this family (35)
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|---|---|---|---|---|
| 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 |
| 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 |
| EP2683394B1 (en) | 2011-03-09 | 2021-01-06 | Signature Therapeutics, Inc. | Active agent 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 |
| WO2015081891A1 (en) | 2013-12-06 | 2015-06-11 | Baikang (Suzhou) Co., Ltd | Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs |
| US11634384B2 (en) | 2014-11-25 | 2023-04-25 | Concentric Analgesics, Inc. | Prodrugs of phenolic TRPV1 agonists |
| US20170056352A1 (en) | 2015-08-25 | 2017-03-02 | Rgenix, Inc. | PHARMACEUTICALLY ACCEPTABLE SALTS OF beta-GUANIDINOPROPIONIC ACID WITH IMPROVED PROPERTIES AND USES THEREOF |
| US10335406B2 (en) | 2015-10-01 | 2019-07-02 | Elysium Therapeutics, Inc. | Opioid compositions resistant to overdose and abuse |
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| EP3554548A4 (en) | 2016-12-19 | 2020-08-19 | The Regents of The University of California | NON-CRUSHABLE PILL FORMULATIONS |
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| CA3056239C (en) | 2017-03-17 | 2023-09-12 | Elysium Therapeutics, Inc. | Polysubunit opioid prodrugs resistant to overdose and abuse |
| CA3091826A1 (en) * | 2018-02-23 | 2019-08-29 | Rhodes Technologies | Novel opioid compounds and uses thereof |
| US10717712B2 (en) | 2018-07-27 | 2020-07-21 | Concentric Analgesics, Inc. | Pegylated prodrugs of phenolic TRPV1 agonists |
| WO2020181000A1 (en) | 2019-03-06 | 2020-09-10 | Ensysce Biosciences, Inc. | Compositions comprising enzyme-cleavable amphetamine prodrugs and inhibitors thereof |
| JP2023505687A (ja) | 2019-12-11 | 2023-02-10 | インスピルナ，インコーポレーテッド | 癌の処置方法 |
| 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 |
| WO2023283256A1 (en) | 2021-07-09 | 2023-01-12 | Aligos Therapeutics, Inc. | Anti-viral compounds |
| US12065428B2 (en) | 2021-09-17 | 2024-08-20 | Aligos Therapeutics, Inc. | Anti-viral compounds |
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| 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 |
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| 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 |
-
2012
- 2012-03-08 EP EP12754373.4A patent/EP2683394B1/en active Active
- 2012-03-08 BR BR112013022946A patent/BR112013022946A2/pt not_active Application Discontinuation
- 2012-03-08 US US14/000,594 patent/US9139612B2/en active Active
- 2012-03-08 RU RU2013144368A patent/RU2608305C2/ru active
- 2012-03-08 CA CA2827662A patent/CA2827662C/en active Active
- 2012-03-08 JP JP2013557882A patent/JP6148182B2/ja active Active
- 2012-03-08 WO PCT/US2012/028367 patent/WO2012122422A2/en not_active Ceased
- 2012-03-08 CN CN201280011870.8A patent/CN103813800B/zh active Active
- 2012-03-08 AU AU2012225337A patent/AU2012225337B2/en active Active
-
2013
- 2013-09-01 IL IL228215A patent/IL228215B/en active IP Right Grant
-
2015
- 2015-08-13 US US14/825,880 patent/US20160002291A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US20140121152A1 (en) | 2014-05-01 |
| WO2012122422A2 (en) | 2012-09-13 |
| JP2014518546A (ja) | 2014-07-31 |
| BR112013022946A2 (pt) | 2017-07-18 |
| CN103813800B (zh) | 2017-12-19 |
| AU2012225337A1 (en) | 2013-05-09 |
| CA2827662A1 (en) | 2012-09-13 |
| RU2608305C2 (ru) | 2017-01-17 |
| AU2012225337B2 (en) | 2016-04-28 |
| EP2683394A4 (en) | 2015-06-03 |
| CN103813800A (zh) | 2014-05-21 |
| WO2012122422A3 (en) | 2014-04-24 |
| RU2013144368A (ru) | 2015-04-10 |
| US20160002291A1 (en) | 2016-01-07 |
| EP2683394B1 (en) | 2021-01-06 |
| JP6148182B2 (ja) | 2017-06-14 |
| US9139612B2 (en) | 2015-09-22 |
| CA2827662C (en) | 2020-07-14 |
| EP2683394A2 (en) | 2014-01-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FF | Patent granted | ||
| KB | Patent renewed |