BRPI0410936A - pró-fármaco inibidor da beta-lactamase - Google Patents
pró-fármaco inibidor da beta-lactamaseInfo
- Publication number
- BRPI0410936A BRPI0410936A BRPI0410936-8A BRPI0410936A BRPI0410936A BR PI0410936 A BRPI0410936 A BR PI0410936A BR PI0410936 A BRPI0410936 A BR PI0410936A BR PI0410936 A BRPI0410936 A BR PI0410936A
- Authority
- BR
- Brazil
- Prior art keywords
- beta
- mammal
- present
- lactam antibiotic
- prodrug
- Prior art date
Links
- 239000000651 prodrug Substances 0.000 title abstract 4
- 229940002612 prodrug Drugs 0.000 title abstract 4
- 239000003781 beta lactamase inhibitor Substances 0.000 title 1
- 229940126813 beta-lactamase inhibitor Drugs 0.000 title 1
- 229940126085 β‑Lactamase Inhibitor Drugs 0.000 title 1
- 241000124008 Mammalia Species 0.000 abstract 3
- 239000003782 beta lactam antibiotic agent Substances 0.000 abstract 3
- 239000012453 solvate Substances 0.000 abstract 3
- 239000002132 β-lactam antibiotic Substances 0.000 abstract 3
- 229940124586 β-lactam antibiotics Drugs 0.000 abstract 3
- 238000000034 method Methods 0.000 abstract 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 208000035143 Bacterial infection Diseases 0.000 abstract 1
- 108090000204 Dipeptidase 1 Proteins 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 208000022362 bacterial infectious disease Diseases 0.000 abstract 1
- 102000006635 beta-lactamase Human genes 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 150000003457 sulfones Chemical class 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D499/00—Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
- C07D499/86—Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring with only atoms other than nitrogen atoms directly attached in position 6 and a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
- C07D499/861—Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring with only atoms other than nitrogen atoms directly attached in position 6 and a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with a hydrocarbon radical or a substituted hydrocarbon radical, directly attached in position 6
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- 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
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D309/10—Oxygen atoms
- C07D309/12—Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D319/10—1,4-Dioxanes; Hydrogenated 1,4-dioxanes
- C07D319/12—1,4-Dioxanes; Hydrogenated 1,4-dioxanes not condensed with other rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
"PRó-FáRMACO INIBIDOR DA BETA-LACTAMASE". São descritos pró-fármacos de sulfona do ácido 6-beta-hidro-ximetilpenicilânico com a estrutura em que R é H ou metila, cada X é metileno e Y é O, ou em que R é H, cada X é O e Y é metileno, e seus solvatos. São também descritas formulações farmacêuticas compreendendo um pró-fármaco da presente invenção, ou um seu solvato, um antibiótico de beta-lactama opcional e, pelo menos, um veículo farmaceuticamente aceitável. é ainda descrito um método para aumentar a eficácia terapêutica de um antibiótico de beta-lactama num mamífero através da administração de uma quantidade eficaz de um antibiótico de beta-lactama e uma quantidade para aumento da eficácia de um pró-fármaco da presente invenção, ou um seu solvato. é por outro lado descrito um método para tratar uma infecção bacteriana num mamífero através da administração de uma quantidade terapeuticamente eficaz de uma formulação farmacêutica da presente invenção a um mamífero necessitado daquela.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US47645603P | 2003-06-05 | 2003-06-05 | |
| US49842203P | 2003-08-27 | 2003-08-27 | |
| PCT/IB2004/001824 WO2004108733A1 (en) | 2003-06-05 | 2004-05-24 | Beta-lactamase inhibitor prodrug |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0410936A true BRPI0410936A (pt) | 2006-06-27 |
Family
ID=33514083
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0410936-8A BRPI0410936A (pt) | 2003-06-05 | 2004-05-24 | pró-fármaco inibidor da beta-lactamase |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20050004093A1 (pt) |
| EP (1) | EP1636240A1 (pt) |
| JP (1) | JP2006526612A (pt) |
| AR (1) | AR044482A1 (pt) |
| BR (1) | BRPI0410936A (pt) |
| CA (1) | CA2528065A1 (pt) |
| CL (1) | CL2004001343A1 (pt) |
| MX (1) | MXPA05012895A (pt) |
| NL (1) | NL1026340C2 (pt) |
| PA (1) | PA8604001A1 (pt) |
| PE (1) | PE20050629A1 (pt) |
| TW (1) | TW200504010A (pt) |
| UY (1) | UY28340A1 (pt) |
| WO (1) | WO2004108733A1 (pt) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PA8579701A1 (es) * | 2002-08-23 | 2005-05-24 | Pfizer Prod Inc | Profarmaco inhibidor de beta-lactamasa |
| EP2279796B1 (de) | 2002-10-14 | 2020-12-30 | H. Börger & Co. GmbH | Verfarhen und vorrichtung zum fördern von pulverförmigem material |
| GB201407506D0 (en) | 2014-04-29 | 2014-06-11 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| US9737505B2 (en) | 2014-04-29 | 2017-08-22 | Glaxosmithkline Intellectual Property Development Limited | Prodrug of 1,1′-(1,6-dioxo-1,6-hexanediyl)bis-D-proline |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IE34011B1 (en) * | 1969-03-13 | 1975-01-08 | Leo Pharm Prod Ltd | New penicillin esters |
| IE34019B1 (en) * | 1969-03-18 | 1975-01-08 | Leo Pharm Prod Ltd | New semi-synthetic penicillin esters |
| US3957764A (en) * | 1969-11-11 | 1976-05-18 | Lovens Kemiske Fabrik Produktionsaktieselskab | 6-aminopenicillanic acid derivatives |
| US3862181A (en) * | 1970-10-28 | 1975-01-21 | Squibb & Sons Inc | Process for preparing cephalosporins |
| US4397783A (en) * | 1979-03-05 | 1983-08-09 | Pfizer Inc. | Process for converting 6,6-disubstituted penicillanic acid derivatives to the 6-β-congeners |
| US4287181A (en) * | 1979-10-22 | 1981-09-01 | Pfizer Inc. | Derivatives of 6β-hydroxyalkylpenicillanic acids as β-lactamase inhibitors |
| US4432970A (en) * | 1979-11-23 | 1984-02-21 | Pfizer Inc. | 6-beta-Halopenicillanic acid 1,1-dioxides as beta-lactamase inhibitors |
| GB2076812A (en) * | 1980-05-22 | 1981-12-09 | Ciba Geigy Ag | Penam-dioxide compounds, processes for their manufacture, and their use |
| EP0076066B1 (en) * | 1981-09-22 | 1986-11-26 | Kureha Kagaku Kogyo Kabushiki Kaisha | Penicillin derivatives |
| US4406887A (en) * | 1981-10-13 | 1983-09-27 | Bristol-Myers Company | Method for treating resistant bacteria including anaerobes |
| US4377590A (en) * | 1982-05-10 | 1983-03-22 | Pfizer Inc. | Derivatives of ampicillin and amoxicillin with beta-lactamase inhibitors |
| US4428935A (en) * | 1982-05-24 | 1984-01-31 | Pfizer Inc. | Penicillanic acid dioxide prodrug |
| US4826833A (en) * | 1984-01-30 | 1989-05-02 | Pfizer Inc. | 6-(Substituted)methylene-penicillanic and 6-(substituted)hydroxymethylpenicillanic acids and derivatives thereof |
| US4521533A (en) * | 1984-07-12 | 1985-06-04 | Pfizer Inc. | Salts of 6-alpha-(aminomethyl)penicillanic acid 1,1-dioxide esters and beta-lactam antibiotics |
| US4762921A (en) * | 1985-04-18 | 1988-08-09 | Pfizer Inc. | 6-(1-acyl-1-hydroxymethyl)penicillanic acid derivatives |
| US5200403A (en) * | 1987-07-10 | 1993-04-06 | Farmitalia Carlo Erba S.R.L. | Inhibition of βlactamase with 6 β-(substituted methyl)-penicillanic acid derivatives |
| JPH03206038A (ja) * | 1990-01-08 | 1991-09-09 | Yoshitomi Pharmaceut Ind Ltd | 抗菌剤 |
| GB9001405D0 (en) * | 1990-01-22 | 1990-03-21 | Leo Pharm Prod Ltd | New intermediates,their production and use |
| AU8333991A (en) * | 1990-08-20 | 1992-03-17 | Suntory Limited | Penem compounds |
| GB9208492D0 (en) * | 1992-04-16 | 1992-06-03 | Glaxo Spa | Heterocyclic compounds |
| CA2282461C (en) * | 1997-12-29 | 2004-04-20 | John D. Buynak | 2-.beta.-substituted-6-alkylidene penicillanic acid derivatives as .beta.-lactamase inhibitors |
| ES2237064T3 (es) * | 1999-03-03 | 2005-07-16 | Astur Pharma S.A. | Procedimiento para preparar derivados de acido dioxopenicilanico. |
| PA8579701A1 (es) * | 2002-08-23 | 2005-05-24 | Pfizer Prod Inc | Profarmaco inhibidor de beta-lactamasa |
-
2004
- 2004-05-24 EP EP04734576A patent/EP1636240A1/en not_active Withdrawn
- 2004-05-24 BR BRPI0410936-8A patent/BRPI0410936A/pt not_active IP Right Cessation
- 2004-05-24 WO PCT/IB2004/001824 patent/WO2004108733A1/en not_active Ceased
- 2004-05-24 CA CA002528065A patent/CA2528065A1/en not_active Abandoned
- 2004-05-24 JP JP2006508430A patent/JP2006526612A/ja active Pending
- 2004-05-24 MX MXPA05012895A patent/MXPA05012895A/es not_active Application Discontinuation
- 2004-06-01 CL CL200401343A patent/CL2004001343A1/es unknown
- 2004-06-02 UY UY28340A patent/UY28340A1/es not_active Application Discontinuation
- 2004-06-02 PE PE2004000557A patent/PE20050629A1/es not_active Application Discontinuation
- 2004-06-02 PA PA20048604001A patent/PA8604001A1/es unknown
- 2004-06-03 AR ARP040101928A patent/AR044482A1/es unknown
- 2004-06-04 TW TW093116149A patent/TW200504010A/zh unknown
- 2004-06-04 NL NL1026340A patent/NL1026340C2/nl not_active IP Right Cessation
- 2004-06-07 US US10/862,200 patent/US20050004093A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| NL1026340A1 (nl) | 2004-12-07 |
| MXPA05012895A (es) | 2006-02-22 |
| JP2006526612A (ja) | 2006-11-24 |
| CA2528065A1 (en) | 2004-12-16 |
| PA8604001A1 (es) | 2004-12-16 |
| CL2004001343A1 (es) | 2005-04-22 |
| TW200504010A (en) | 2005-02-01 |
| PE20050629A1 (es) | 2005-08-25 |
| WO2004108733A1 (en) | 2004-12-16 |
| UY28340A1 (es) | 2005-01-31 |
| EP1636240A1 (en) | 2006-03-22 |
| AR044482A1 (es) | 2005-09-14 |
| NL1026340C2 (nl) | 2005-09-14 |
| US20050004093A1 (en) | 2005-01-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE AS 4A, 5A, 6A, 7A E 8A ANUIDADES. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2159 DE 22/05/2012. |