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 (https=) |
| EP (1) | EP2683394B1 (https=) |
| JP (1) | JP6148182B2 (https=) |
| CN (1) | CN103813800B (https=) |
| AU (1) | AU2012225337B2 (https=) |
| BR (1) | BR112013022946A2 (https=) |
| CA (1) | CA2827662C (https=) |
| IL (1) | IL228215B (https=) |
| RU (1) | RU2608305C2 (https=) |
| WO (1) | WO2012122422A2 (https=) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112012005124B1 (pt) * | 2009-09-08 | 2021-11-09 | Signature Therapeutics, Inc. | Pro-fármaco de opioide modificado por cetona, seu método de preparação, sua composição farmacêutica, sua unidade de dose, métodos e usos |
| 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 |
| ES2584634T3 (es) | 2011-01-11 | 2016-09-28 | Signature Therapeutics, Inc. | Composiciones que comprenden un profármaco de oxicodona escindible enzimáticamente |
| WO2012122420A2 (en) | 2011-03-09 | 2012-09-13 | Pharmacofore, Inc. | Opioid prodrugs with heterocyclic linkers |
| AU2012225337B2 (en) | 2011-03-09 | 2016-04-28 | Signature Therapeutics, Inc. | Active agent prodrugs with heterocyclic linkers |
| WO2013045854A1 (fr) | 2011-09-29 | 2013-04-04 | Ecole Normale Superieure De Lyon | Substrat de peptidase fluorogene |
| CN112043835B (zh) * | 2013-12-06 | 2022-10-21 | 韩捷 | 用于含氮和羟基的药物的生物可逆引入基团 |
| 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 |
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| EP3595663A4 (en) | 2017-03-17 | 2021-01-13 | Elysium Therapeutics, Inc. | MULTIPLE SUBUNITY OPIOID PRODRUGS WITH RESISTANCE TO OVERDOSE AND ABUSE |
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| US20220175699A1 (en) * | 2019-03-06 | 2022-06-09 | 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 |
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| US20130059914A1 (en) | 2010-04-21 | 2013-03-07 | Signature Therapeutics, Inc. | Compositions Comprising Enzyme-Cleavable Amphetamine Prodrugs and Inhibitors Thereof |
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| US20110262359A1 (en) | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions comprising enzyme-cleavable prodrugs of active agents 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 |
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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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| ES2584634T3 (es) | 2011-01-11 | 2016-09-28 | Signature Therapeutics, Inc. | Composiciones que comprenden un profármaco de oxicodona escindible enzimáticamente |
| WO2012096886A1 (en) | 2011-01-11 | 2012-07-19 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
| WO2012122420A2 (en) * | 2011-03-09 | 2012-09-13 | Pharmacofore, Inc. | Opioid prodrugs with heterocyclic linkers |
| AU2012225337B2 (en) | 2011-03-09 | 2016-04-28 | Signature Therapeutics, Inc. | Active agent prodrugs with heterocyclic linkers |
-
2012
- 2012-03-08 AU AU2012225337A patent/AU2012225337B2/en active Active
- 2012-03-08 RU RU2013144368A patent/RU2608305C2/ru active
- 2012-03-08 EP EP12754373.4A patent/EP2683394B1/en active Active
- 2012-03-08 WO PCT/US2012/028367 patent/WO2012122422A2/en not_active Ceased
- 2012-03-08 CA CA2827662A patent/CA2827662C/en active Active
- 2012-03-08 CN CN201280011870.8A patent/CN103813800B/zh active Active
- 2012-03-08 US US14/000,594 patent/US9139612B2/en active Active
- 2012-03-08 JP JP2013557882A patent/JP6148182B2/ja active Active
- 2012-03-08 BR BR112013022946A patent/BR112013022946A2/pt not_active Application Discontinuation
-
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 |
| AU2012225337A1 (en) | 2013-05-09 |
| AU2012225337B2 (en) | 2016-04-28 |
| CA2827662C (en) | 2020-07-14 |
| CN103813800A (zh) | 2014-05-21 |
| EP2683394A2 (en) | 2014-01-15 |
| EP2683394A4 (en) | 2015-06-03 |
| JP2014518546A (ja) | 2014-07-31 |
| RU2013144368A (ru) | 2015-04-10 |
| JP6148182B2 (ja) | 2017-06-14 |
| WO2012122422A2 (en) | 2012-09-13 |
| BR112013022946A2 (pt) | 2017-07-18 |
| CN103813800B (zh) | 2017-12-19 |
| RU2608305C2 (ru) | 2017-01-17 |
| US9139612B2 (en) | 2015-09-22 |
| EP2683394B1 (en) | 2021-01-06 |
| WO2012122422A3 (en) | 2014-04-24 |
| US20160002291A1 (en) | 2016-01-07 |
| CA2827662A1 (en) | 2012-09-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FF | Patent granted | ||
| KB | Patent renewed |