MXPA05001446A - Profarmaco inhibidor de beta-lactamasa. - Google Patents
Profarmaco inhibidor de beta-lactamasa.Info
- Publication number
- MXPA05001446A MXPA05001446A MXPA05001446A MXPA05001446A MXPA05001446A MX PA05001446 A MXPA05001446 A MX PA05001446A MX PA05001446 A MXPA05001446 A MX PA05001446A MX PA05001446 A MXPA05001446 A MX PA05001446A MX PA05001446 A MXPA05001446 A MX PA05001446A
- Authority
- MX
- Mexico
- Prior art keywords
- prodrug
- beta
- hydroxymethyl
- oxo
- heptane
- Prior art date
Links
- 239000000651 prodrug Substances 0.000 title claims abstract description 193
- 229940002612 prodrug Drugs 0.000 title claims abstract description 193
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- 229940126813 beta-lactamase inhibitor Drugs 0.000 title description 10
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- NNYHKYDYHWSHKQ-UHFFFAOYSA-N 4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid Chemical compound OC(=O)C1CSC2CCN12 NNYHKYDYHWSHKQ-UHFFFAOYSA-N 0.000 claims description 37
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- 239000012729 immediate-release (IR) formulation Substances 0.000 description 1
- 239000012535 impurity Substances 0.000 description 1
- 230000002779 inactivation Effects 0.000 description 1
- 238000011081 inoculation Methods 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 210000004731 jugular vein Anatomy 0.000 description 1
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 1
- 230000002147 killing effect Effects 0.000 description 1
- 210000002429 large intestine Anatomy 0.000 description 1
- 239000011344 liquid material Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- CCERQOYLJJULMD-UHFFFAOYSA-M magnesium;carbanide;chloride Chemical compound [CH3-].[Mg+2].[Cl-] CCERQOYLJJULMD-UHFFFAOYSA-M 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000004949 mass spectrometry Methods 0.000 description 1
- 208000004396 mastitis Diseases 0.000 description 1
- OKKJLVBELUTLKV-VMNATFBRSA-N methanol-d1 Chemical compound [2H]OC OKKJLVBELUTLKV-VMNATFBRSA-N 0.000 description 1
- 150000004702 methyl esters Chemical class 0.000 description 1
- 229960003085 meticillin Drugs 0.000 description 1
- 230000000813 microbial effect Effects 0.000 description 1
- 239000002480 mineral oil Substances 0.000 description 1
- 235000010446 mineral oil Nutrition 0.000 description 1
- 239000003595 mist Substances 0.000 description 1
- 229940041009 monobactams Drugs 0.000 description 1
- 239000012452 mother liquor Substances 0.000 description 1
- 229940100692 oral suspension Drugs 0.000 description 1
- 239000006174 pH buffer Substances 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 229920002866 paraformaldehyde Polymers 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 229950009506 penicillinase Drugs 0.000 description 1
- 206010034674 peritonitis Diseases 0.000 description 1
- 239000008177 pharmaceutical agent Substances 0.000 description 1
- 239000012071 phase Substances 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- 229950010765 pivalate Drugs 0.000 description 1
- 239000008389 polyethoxylated castor oil Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000151 polyglycol Polymers 0.000 description 1
- 239000010695 polyglycol Substances 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 238000000634 powder X-ray diffraction Methods 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 150000003856 quaternary ammonium compounds Chemical class 0.000 description 1
- 230000001373 regressive effect Effects 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 208000023504 respiratory system disease Diseases 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 239000012056 semi-solid material Substances 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 238000010583 slow cooling Methods 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 239000011343 solid material Substances 0.000 description 1
- 239000007892 solid unit dosage form Substances 0.000 description 1
- 239000011877 solvent mixture Substances 0.000 description 1
- 238000004611 spectroscopical analysis Methods 0.000 description 1
- 239000008174 sterile solution Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000001384 succinic acid Substances 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- LPQZKKCYTLCDGQ-WEDXCCLWSA-N tazobactam Chemical compound C([C@]1(C)S([C@H]2N(C(C2)=O)[C@H]1C(O)=O)(=O)=O)N1C=CN=N1 LPQZKKCYTLCDGQ-WEDXCCLWSA-N 0.000 description 1
- 229960003865 tazobactam Drugs 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 210000001541 thymus gland Anatomy 0.000 description 1
- DBGVGMSCBYYSLD-UHFFFAOYSA-N tributylstannane Chemical compound CCCC[SnH](CCCC)CCCC DBGVGMSCBYYSLD-UHFFFAOYSA-N 0.000 description 1
- 210000002438 upper gastrointestinal tract Anatomy 0.000 description 1
- 210000001635 urinary tract Anatomy 0.000 description 1
- 238000001291 vacuum drying Methods 0.000 description 1
- 230000035899 viability Effects 0.000 description 1
- 238000003260 vortexing Methods 0.000 description 1
- 238000010792 warming Methods 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 239000011592 zinc chloride Substances 0.000 description 1
- 235000005074 zinc chloride Nutrition 0.000 description 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
-
- 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
-
- 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
- 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
- C07D499/21—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 a nitrogen atom 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
- C07D499/44—Compounds with an amino radical acylated by carboxylic acids, attached in position 6
- C07D499/48—Compounds with an amino radical acylated by carboxylic acids, attached in position 6 with a carbon chain, substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, attached to the carboxamido radical
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)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40564002P | 2002-08-23 | 2002-08-23 | |
| PCT/IB2003/003582 WO2004018484A1 (en) | 2002-08-23 | 2003-08-11 | Beta-lactamase inhibitor prodrug |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MXPA05001446A true MXPA05001446A (es) | 2005-06-06 |
Family
ID=31946909
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MXPA05001446A MXPA05001446A (es) | 2002-08-23 | 2003-08-11 | Profarmaco inhibidor de beta-lactamasa. |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US7091197B2 (https=) |
| EP (1) | EP1534717B1 (https=) |
| JP (1) | JP2005539037A (https=) |
| KR (1) | KR20050037583A (https=) |
| CN (1) | CN1688589A (https=) |
| AP (1) | AP2005003231A0 (https=) |
| AR (1) | AR041028A1 (https=) |
| AT (1) | ATE349452T1 (https=) |
| AU (1) | AU2003250489A1 (https=) |
| BR (1) | BR0313683A (https=) |
| CA (1) | CA2494953A1 (https=) |
| DE (1) | DE60310733D1 (https=) |
| EA (1) | EA007540B1 (https=) |
| EC (1) | ECSP055625A (https=) |
| GT (1) | GT200300179A (https=) |
| HR (1) | HRP20050162A2 (https=) |
| IL (1) | IL166719A0 (https=) |
| IS (1) | IS7693A (https=) |
| MA (1) | MA27387A1 (https=) |
| MX (1) | MXPA05001446A (https=) |
| NO (1) | NO20051497D0 (https=) |
| NZ (1) | NZ538340A (https=) |
| OA (1) | OA12909A (https=) |
| PA (1) | PA8579701A1 (https=) |
| PE (1) | PE20040899A1 (https=) |
| PL (1) | PL375988A1 (https=) |
| TN (1) | TNSN05054A1 (https=) |
| TW (1) | TWI250162B (https=) |
| UY (1) | UY27947A1 (https=) |
| WO (1) | WO2004018484A1 (https=) |
| ZA (1) | ZA200501513B (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004108733A1 (en) * | 2003-06-05 | 2004-12-16 | Pfizer Products Inc. | Beta-lactamase inhibitor prodrug |
| US20060105941A1 (en) * | 2004-11-12 | 2006-05-18 | Allergan, Inc. | Mixed antibiotic codrugs |
| EP1913378A1 (de) * | 2005-07-29 | 2008-04-23 | Sigma-Aldrich Production GmbH | Ionisierungsadditive enthaltende lc/ms-blends |
| WO2010118968A1 (en) | 2009-04-16 | 2010-10-21 | Nicox S.A. | No-donor aspirin derivatives |
| WO2013056163A1 (en) * | 2011-10-14 | 2013-04-18 | The Regents Of The University Of California | Beta-lactamase inhibitors |
| CN104159587A (zh) * | 2012-01-06 | 2014-11-19 | 南佛罗里达大学 | 组合物、使用方法、以及治疗方法 |
| CN109422765B (zh) * | 2017-09-05 | 2020-08-28 | 香港理工大学深圳研究院 | C类β-内酰胺酶抑制剂及其制备方法和应用 |
Family Cites Families (24)
| 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 |
| GB1267936A (en) | 1969-05-28 | 1972-03-22 | Beecham Group Ltd | DERIVATIVES OF alpha-AMINOPENICILLINS |
| 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 |
| GB1315566A (en) | 1970-11-06 | 1973-05-02 | Leo Pharm Prod Ltd | Penicillanic acid derivatives |
| CA996929A (en) | 1971-04-05 | 1976-09-14 | Kohzi Nakano | Acyloxyalkyl ester derivatives of penicillin |
| GB1433131A (en) | 1972-03-13 | 1976-04-22 | Astra Laekemedel Ab | Penicillins |
| GB1426717A (en) | 1972-03-13 | 1976-03-03 | Astra Laekemedel Ab | Penicillins |
| US4397783A (en) | 1979-03-05 | 1983-08-09 | Pfizer Inc. | Process for converting 6,6-disubstituted penicillanic acid derivatives to the 6-β-congeners |
| DE2927004A1 (de) * | 1979-07-04 | 1981-05-27 | Bayer Ag, 5090 Leverkusen | Penicillansaeure-1,1-dioxide, ihre herstellung und ihre verwendung als arzneimittel als arzneimittel |
| 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 |
| JPS5849387A (ja) | 1981-09-17 | 1983-03-23 | Sankyo Co Ltd | ７−メトキシセフアロスポリン化合物およびその製法 |
| DE3274453D1 (en) * | 1981-09-22 | 1987-01-15 | Kureha Chemical Ind Co Ltd | Penicillin derivatives |
| US4406887A (en) | 1981-10-13 | 1983-09-27 | Bristol-Myers Company | Method for treating resistant bacteria including anaerobes |
| US4428935A (en) * | 1982-05-24 | 1984-01-31 | Pfizer Inc. | Penicillanic acid dioxide prodrug |
| 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 |
| DE3901405A1 (de) | 1989-01-19 | 1990-07-26 | Hoechst Ag | Cephalosporinderivate und verfahren zu ihrer herstellung |
| 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 |
| GB9208492D0 (en) | 1992-04-16 | 1992-06-03 | Glaxo Spa | Heterocyclic compounds |
| WO2004108733A1 (en) | 2003-06-05 | 2004-12-16 | Pfizer Products Inc. | Beta-lactamase inhibitor prodrug |
-
2003
- 2003-08-06 PA PA20038579701A patent/PA8579701A1/es unknown
- 2003-08-11 MX MXPA05001446A patent/MXPA05001446A/es unknown
- 2003-08-11 KR KR1020057002983A patent/KR20050037583A/ko not_active Abandoned
- 2003-08-11 DE DE60310733T patent/DE60310733D1/de not_active Expired - Lifetime
- 2003-08-11 PL PL03375988A patent/PL375988A1/xx unknown
- 2003-08-11 EP EP03792574A patent/EP1534717B1/en not_active Expired - Lifetime
- 2003-08-11 NZ NZ538340A patent/NZ538340A/en unknown
- 2003-08-11 WO PCT/IB2003/003582 patent/WO2004018484A1/en not_active Ceased
- 2003-08-11 HR HR20050162A patent/HRP20050162A2/xx not_active Application Discontinuation
- 2003-08-11 AU AU2003250489A patent/AU2003250489A1/en not_active Abandoned
- 2003-08-11 CA CA002494953A patent/CA2494953A1/en not_active Abandoned
- 2003-08-11 JP JP2004530453A patent/JP2005539037A/ja not_active Abandoned
- 2003-08-11 CN CNA038243164A patent/CN1688589A/zh active Pending
- 2003-08-11 AT AT03792574T patent/ATE349452T1/de not_active IP Right Cessation
- 2003-08-11 AP AP2005003231A patent/AP2005003231A0/xx unknown
- 2003-08-11 BR BR0313683-3A patent/BR0313683A/pt not_active IP Right Cessation
- 2003-08-11 EA EA200500398A patent/EA007540B1/ru unknown
- 2003-08-11 OA OA1200500051A patent/OA12909A/en unknown
- 2003-08-19 PE PE2003000840A patent/PE20040899A1/es not_active Application Discontinuation
- 2003-08-21 UY UY27947A patent/UY27947A1/es not_active Application Discontinuation
- 2003-08-21 AR ARP030103023A patent/AR041028A1/es unknown
- 2003-08-22 TW TW092123156A patent/TWI250162B/zh not_active IP Right Cessation
- 2003-08-22 GT GT200300179A patent/GT200300179A/es unknown
- 2003-08-25 US US10/648,408 patent/US7091197B2/en not_active Expired - Fee Related
-
2005
- 2005-02-07 IL IL16671905A patent/IL166719A0/xx unknown
- 2005-02-10 IS IS7693A patent/IS7693A/is unknown
- 2005-02-21 ZA ZA200501513A patent/ZA200501513B/en unknown
- 2005-02-23 EC EC2005005625A patent/ECSP055625A/es unknown
- 2005-02-23 MA MA28119A patent/MA27387A1/fr unknown
- 2005-02-23 TN TNP2005000054A patent/TNSN05054A1/fr unknown
- 2005-03-21 NO NO20051497A patent/NO20051497D0/no not_active Application Discontinuation
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