BRPI0520493A2 - usos de uma enzima, de um composto antifolato e de um agente de resgate de rota de folato, sistema terapêutico, e, métodos ex vivo para clivar um grupo l-glutamato terminal de um composto, para determinar a taxa e/ou extensão de clivagem de um composto e para clivar um composto - Google Patents
usos de uma enzima, de um composto antifolato e de um agente de resgate de rota de folato, sistema terapêutico, e, métodos ex vivo para clivar um grupo l-glutamato terminal de um composto, para determinar a taxa e/ou extensão de clivagem de um composto e para clivar um compostoInfo
- Publication number
- BRPI0520493A2 BRPI0520493A2 BRPI0520493-3A BRPI0520493A BRPI0520493A2 BR PI0520493 A2 BRPI0520493 A2 BR PI0520493A2 BR PI0520493 A BRPI0520493 A BR PI0520493A BR PI0520493 A2 BRPI0520493 A2 BR PI0520493A2
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- cleave
- enzyme
- antifolate
- therapeutic system
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 11
- 238000000034 method Methods 0.000 title abstract 6
- 108090000790 Enzymes Proteins 0.000 title abstract 4
- 102000004190 Enzymes Human genes 0.000 title abstract 4
- 230000003432 anti-folate effect Effects 0.000 title abstract 3
- 229940127074 antifolate Drugs 0.000 title abstract 3
- 239000004052 folic acid antagonist Substances 0.000 title abstract 3
- 239000003795 chemical substances by application Substances 0.000 title abstract 2
- 229940014144 folate Drugs 0.000 title abstract 2
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 title abstract 2
- 235000019152 folic acid Nutrition 0.000 title abstract 2
- 239000011724 folic acid Substances 0.000 title abstract 2
- 230000001225 therapeutic effect Effects 0.000 title abstract 2
- WHUUTDBJXJRKMK-VKHMYHEASA-L L-glutamate group Chemical group N[C@@H](CCC(=O)[O-])C(=O)[O-] WHUUTDBJXJRKMK-VKHMYHEASA-L 0.000 title 1
- 238000003776 cleavage reaction Methods 0.000 title 1
- 230000037361 pathway Effects 0.000 title 1
- 230000007017 scission Effects 0.000 title 1
- 230000000694 effects Effects 0.000 abstract 2
- 239000012634 fragment Substances 0.000 abstract 2
- 108010062699 gamma-Glutamyl Hydrolase Proteins 0.000 abstract 2
- 230000001988 toxicity Effects 0.000 abstract 1
- 231100000419 toxicity Toxicity 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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/43—Enzymes; Proenzymes; Derivatives thereof
- A61K38/46—Hydrolases (3)
- A61K38/48—Hydrolases (3) acting on peptide bonds (3.4)
- A61K38/4813—Exopeptidases (3.4.11. to 3.4.19)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Gastroenterology & Hepatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
USOS DE UMA ENZIMA, DE UM COMPOSTO ANTIFOLATO E DE UM AGENTE DE RESGATE DE ROTA DE FOLATO, SISTEMA TERAPêUTICO, E, METODOS EK VIVO PARA CLIVAR UM GRUPO L-GLUTAMATO TERMINAL DE UM COMPOSTO, PARA DETERMINAR A TAXA E/OU EXTENSãO DE CLIVAGEM DE UM COMPOSTO E PARA CLIVAR UM COMPOSTO. Um método para combater toxicidade causada por um composto antifolato de Fórmula I, em um indivíduo que tem sido administrado com o composto. O método compreende administrar ao indivíduo uma enzima que possui atividade de carbóxi-peptidase G. Um método de clivagem de um composto compreendendo um fragmento estrutural de Fórmula IV, o método compreendendo contatar o composto compreendendo o fragmento estrutural de Fórmula IV com uma enzima que possui atividade de carbóxi-peptidase G.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/GB2005/003297 WO2007023243A2 (en) | 2005-08-24 | 2005-08-24 | Cleavage of antifolate compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0520493A2 true BRPI0520493A2 (pt) | 2009-05-12 |
Family
ID=36615646
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0520493-3A BRPI0520493A2 (pt) | 2005-08-24 | 2005-08-24 | usos de uma enzima, de um composto antifolato e de um agente de resgate de rota de folato, sistema terapêutico, e, métodos ex vivo para clivar um grupo l-glutamato terminal de um composto, para determinar a taxa e/ou extensão de clivagem de um composto e para clivar um composto |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP1917027A2 (pt) |
| AU (1) | AU2005335876A1 (pt) |
| BR (1) | BRPI0520493A2 (pt) |
| CA (1) | CA2619992A1 (pt) |
| IL (1) | IL189498A0 (pt) |
| MX (1) | MX2008002648A (pt) |
| WO (1) | WO2007023243A2 (pt) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8546425B2 (en) | 2008-09-17 | 2013-10-01 | Purdue Research Foundation | Folate receptor binding conjugates of antifolates |
| ES2554623T3 (es) | 2008-12-30 | 2015-12-22 | Arqule, Inc. | Compuestos de 5,6-dihidro-6-fenilbenzo[f]isoquinolin-2-amina sustituida |
| US20170239250A1 (en) | 2016-02-19 | 2017-08-24 | Eagle Pharmaceuticals, Inc. | Pemetrexed formulations |
| WO2018031967A1 (en) | 2016-08-12 | 2018-02-15 | L.E.A.F. Holdings Group Llc | Polyglutamated antifolates and uses thereof |
| EA201990473A1 (ru) | 2016-08-12 | 2019-07-31 | Эл.И.Эй.Эф. ХОЛДИНГС ГРУП ЭлЭлСи | Полиглутамированные антифолаты и их применение |
| EP3749311A4 (en) * | 2018-02-07 | 2022-07-06 | L.E.A.F Holdings Group LLC | PEMETREXED POLYGLUTAMATE GAMMA COMPOSITIONS AND THEIR USES |
| WO2019157123A1 (en) | 2018-02-07 | 2019-08-15 | L.E.A.F. Holdings Group Llc | Alpha polyglutamated aminopterin and uses thereof |
| CA3090506A1 (en) | 2018-02-07 | 2019-08-15 | L.E.A.F. Holdings Group Llc | Alpha polyglutamated tetrahydrofolates and uses thereof |
| US12076402B2 (en) | 2018-02-07 | 2024-09-03 | L.E.A.F. Holdings Group Llc | Alpha polyglutamated antifolates and uses thereof |
| US12220431B2 (en) | 2018-02-07 | 2025-02-11 | L.E.A.F. Holdings Group Llc | Gamma polyglutamated antifolates and uses thereof |
| CA3090389A1 (en) | 2018-02-07 | 2019-08-15 | L.E.A.F. Holdings Group Llc | Alpha polyglutamated raltitrexed and uses thereof |
| EP3749316A4 (en) | 2018-02-07 | 2021-10-27 | L.E.A.F Holdings Group LLC | ALPHA-POLYGLUTAMATED PRALATREXATE AND USES THEREOF |
| EP3749312A4 (en) * | 2018-02-07 | 2022-02-23 | L.E.A.F Holdings Group LLC | ALPHA-POLYGLUTAMATED LOMETREXOLE AND USES THEREOF |
| CN111954529A (zh) | 2018-02-07 | 2020-11-17 | L.E.A.F.控股集团公司 | α聚谷氨酸化氨甲蝶呤及其用途 |
| US11779584B2 (en) | 2018-02-07 | 2023-10-10 | L.E.A.F. Holdings Group Llc | Alpha polyglutamated pemetrexed and uses thereof |
| EP3749318A4 (en) * | 2018-02-07 | 2022-07-06 | L.E.A.F Holdings Group LLC | GAMMA-POLYGLUTAMATED RALTITREXED AND ITS USES |
| CN111936145A (zh) | 2018-02-14 | 2020-11-13 | L.E.A.F.控股集团公司 | γ聚谷氨酸化氨甲蝶呤及其用途 |
| US11771700B2 (en) | 2018-02-14 | 2023-10-03 | L.E.A.F. Holdings Group Llc | Gamma polyglutamated lometrexol and uses thereof |
| EP3752156A4 (en) | 2018-02-14 | 2021-10-27 | L.E.A.F Holdings Group LLC | GAMMA-POLYGLUTAMIZED PRALATREXATE AND USES THEREOF |
| CA3090943A1 (en) | 2018-02-14 | 2019-08-22 | L.E.A.F. Holdings Group Llc | Gamma polyglutamated aminopterin and uses thereof |
| US12048766B2 (en) | 2018-02-14 | 2024-07-30 | L.E.A.F. Holdings Group Llc | Gamma polyglutamated tetrahydrofolates and uses thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0404487D0 (en) * | 2004-02-28 | 2004-03-31 | Protherics Molecular Design Lt | Use of enzyme |
-
2005
- 2005-08-24 BR BRPI0520493-3A patent/BRPI0520493A2/pt not_active Application Discontinuation
- 2005-08-24 EP EP05775448A patent/EP1917027A2/en not_active Withdrawn
- 2005-08-24 CA CA002619992A patent/CA2619992A1/en not_active Abandoned
- 2005-08-24 AU AU2005335876A patent/AU2005335876A1/en not_active Abandoned
- 2005-08-24 MX MX2008002648A patent/MX2008002648A/es unknown
- 2005-08-24 WO PCT/GB2005/003297 patent/WO2007023243A2/en not_active Ceased
-
2008
- 2008-02-13 IL IL189498A patent/IL189498A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2619992A1 (en) | 2007-03-01 |
| EP1917027A2 (en) | 2008-05-07 |
| IL189498A0 (en) | 2008-06-05 |
| AU2005335876A1 (en) | 2007-03-01 |
| WO2007023243A2 (en) | 2007-03-01 |
| MX2008002648A (es) | 2008-03-14 |
| WO2007023243A3 (en) | 2007-09-07 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B11A | Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing | ||
| B11Y | Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette] |