ZA200501513B - Beta-lactamase inhibitor prodrug - Google Patents
Beta-lactamase inhibitor prodrug Download PDFInfo
- Publication number
- ZA200501513B ZA200501513B ZA200501513A ZA200501513A ZA200501513B ZA 200501513 B ZA200501513 B ZA 200501513B ZA 200501513 A ZA200501513 A ZA 200501513A ZA 200501513 A ZA200501513 A ZA 200501513A ZA 200501513 B ZA200501513 B ZA 200501513B
- Authority
- ZA
- South Africa
- Prior art keywords
- prodrug
- beta
- composition
- hydroxymethyl
- substance
- Prior art date
Links
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- 230000000813 microbial effect Effects 0.000 description 1
- 238000003801 milling Methods 0.000 description 1
- 239000002480 mineral oil Substances 0.000 description 1
- 235000010446 mineral oil Nutrition 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 230000003020 moisturizing effect Effects 0.000 description 1
- 238000012544 monitoring process Methods 0.000 description 1
- 229940041009 monobactams Drugs 0.000 description 1
- 239000012452 mother liquor Substances 0.000 description 1
- 238000010172 mouse model Methods 0.000 description 1
- 238000002663 nebulization Methods 0.000 description 1
- 239000012299 nitrogen atmosphere 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
- 206010034674 peritonitis Diseases 0.000 description 1
- 239000012071 phase Substances 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- ABVRVIZBZKUTMK-JSYANWSFSA-M potassium clavulanate Chemical compound [K+].[O-]C(=O)[C@H]1C(=C/CO)/O[C@@H]2CC(=O)N21 ABVRVIZBZKUTMK-JSYANWSFSA-M 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 125000004742 propyloxycarbonyl group Chemical group 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 description 1
- 150000003856 quaternary ammonium compounds Chemical class 0.000 description 1
- 238000010791 quenching Methods 0.000 description 1
- VMXUWOKSQNHOCA-UKTHLTGXSA-N ranitidine Chemical compound [O-][N+](=O)\C=C(/NC)NCCSCC1=CC=C(CN(C)C)O1 VMXUWOKSQNHOCA-UKTHLTGXSA-N 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
- 230000000979 retarding 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
- 206010040872 skin infection Diseases 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
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 239000011343 solid material Substances 0.000 description 1
- 239000011877 solvent mixture Substances 0.000 description 1
- 238000002798 spectrophotometry method Methods 0.000 description 1
- 238000012453 sprague-dawley rat model Methods 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 239000008174 sterile solution Substances 0.000 description 1
- 239000011550 stock solution Substances 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
- 230000002194 synthesizing effect Effects 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
- 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
- 230000035899 viability Effects 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 238000003260 vortexing Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 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)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40564002P | 2002-08-23 | 2002-08-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200501513B true ZA200501513B (en) | 2006-09-27 |
Family
ID=31946909
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200501513A ZA200501513B (en) | 2002-08-23 | 2005-02-21 | Beta-lactamase inhibitor prodrug |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US7091197B2 (es) |
| EP (1) | EP1534717B1 (es) |
| JP (1) | JP2005539037A (es) |
| KR (1) | KR20050037583A (es) |
| CN (1) | CN1688589A (es) |
| AP (1) | AP2005003231A0 (es) |
| AR (1) | AR041028A1 (es) |
| AT (1) | ATE349452T1 (es) |
| AU (1) | AU2003250489A1 (es) |
| BR (1) | BR0313683A (es) |
| CA (1) | CA2494953A1 (es) |
| DE (1) | DE60310733D1 (es) |
| EA (1) | EA007540B1 (es) |
| EC (1) | ECSP055625A (es) |
| GT (1) | GT200300179A (es) |
| HR (1) | HRP20050162A2 (es) |
| IL (1) | IL166719A0 (es) |
| IS (1) | IS7693A (es) |
| MA (1) | MA27387A1 (es) |
| MX (1) | MXPA05001446A (es) |
| NO (1) | NO20051497L (es) |
| NZ (1) | NZ538340A (es) |
| OA (1) | OA12909A (es) |
| PA (1) | PA8579701A1 (es) |
| PE (1) | PE20040899A1 (es) |
| PL (1) | PL375988A1 (es) |
| TN (1) | TNSN05054A1 (es) |
| TW (1) | TWI250162B (es) |
| UY (1) | UY27947A1 (es) |
| WO (1) | WO2004018484A1 (es) |
| ZA (1) | ZA200501513B (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0410936A (pt) * | 2003-06-05 | 2006-06-27 | Pfizer Prod Inc | pró-fármaco inibidor da beta-lactamase |
| US20060105941A1 (en) * | 2004-11-12 | 2006-05-18 | Allergan, Inc. | Mixed antibiotic codrugs |
| WO2007012319A1 (de) * | 2005-07-29 | 2007-02-01 | 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 |
| CA2860672A1 (en) * | 2012-01-06 | 2013-07-11 | University Of South Florida | Compositions, methods of use, and methods of treatment |
| 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 |
| AU559689B2 (en) * | 1981-09-22 | 1987-03-19 | Kureha Kagaku Kogyo K.K. | Penicillin derivative |
| 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 |
| BRPI0410936A (pt) | 2003-06-05 | 2006-06-27 | Pfizer Prod Inc | pró-fármaco inibidor da beta-lactamase |
-
2003
- 2003-08-06 PA PA20038579701A patent/PA8579701A1/es unknown
- 2003-08-11 CN CNA038243164A patent/CN1688589A/zh active Pending
- 2003-08-11 EP EP03792574A patent/EP1534717B1/en not_active Expired - Lifetime
- 2003-08-11 WO PCT/IB2003/003582 patent/WO2004018484A1/en active IP Right Grant
- 2003-08-11 KR KR1020057002983A patent/KR20050037583A/ko active IP Right Grant
- 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 PL PL03375988A patent/PL375988A1/xx unknown
- 2003-08-11 JP JP2004530453A patent/JP2005539037A/ja not_active Abandoned
- 2003-08-11 OA OA1200500051A patent/OA12909A/en unknown
- 2003-08-11 NZ NZ538340A patent/NZ538340A/en unknown
- 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 DE DE60310733T patent/DE60310733D1/de not_active Expired - Lifetime
- 2003-08-11 EA EA200500398A patent/EA007540B1/ru unknown
- 2003-08-11 MX MXPA05001446A patent/MXPA05001446A/es unknown
- 2003-08-11 AT AT03792574T patent/ATE349452T1/de not_active IP Right Cessation
- 2003-08-19 PE PE2003000840A patent/PE20040899A1/es not_active Application Discontinuation
- 2003-08-21 AR ARP030103023A patent/AR041028A1/es unknown
- 2003-08-21 UY UY27947A patent/UY27947A1/es not_active Application Discontinuation
- 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
- 2005-02-21 HR HR20050162A patent/HRP20050162A2/xx not_active Application Discontinuation
- 2005-02-23 EC EC2005005625A patent/ECSP055625A/es unknown
- 2005-02-23 TN TNP2005000054A patent/TNSN05054A1/fr unknown
- 2005-02-23 MA MA28119A patent/MA27387A1/fr unknown
- 2005-03-21 NO NO20051497A patent/NO20051497L/no not_active Application Discontinuation
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