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GB2000138A - Therapeutic agents - Google Patents

Therapeutic agents

Info

Publication number
GB2000138A
GB2000138A GB7826308A GB7826308A GB2000138A GB 2000138 A GB2000138 A GB 2000138A GB 7826308 A GB7826308 A GB 7826308A GB 7826308 A GB7826308 A GB 7826308A GB 2000138 A GB2000138 A GB 2000138A
Authority
GB
United Kingdom
Prior art keywords
penicillanic acid
esters
dioxides
dioxide
useful
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
GB7826308A
Other versions
GB2000138B (en
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pfizer Corp Belgium
Pfizer Inc
Original Assignee
Pfizer Corp Belgium
Pfizer Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27122691&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=GB2000138(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer Corp Belgium, Pfizer Inc filed Critical Pfizer Corp Belgium
Publication of GB2000138A publication Critical patent/GB2000138A/en
Application granted granted Critical
Publication of GB2000138B publication Critical patent/GB2000138B/en
Expired legal-status Critical Current

Links

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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
    • A61K31/43—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
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

1,1-Dioxides of penicillanic acid and esters are described which are useful as beta -lactamase inhibitors. These compounds are 1,1-dioxides of penicillanic acid and of corresponding esters which are easily hydrolysable in vivo, derivatives of penicillanic acid 1,1-dioxide, the carboxyl radical of which is protected by a standard protective group of the carboxyl radical of penicillins, which are useful intermediates for the synthesis of penicillanic acid 1,1-dioxide, and 1-oxides of penicillanic acid and of certain of its esters which are useful as chemical intermediates for the synthesis of penicillanic acid 1,1-dioxide and of its esters. These 1,1-dioxides of penicillanic acid and esters are antibacterial agents, also capable of increasing the effectiveness of various antibiotics of the beta -lactam type with respect to bacteria which produce beta -lactamase.
GB7826308A 1977-06-07 1978-06-02 Therapeutic agents Expired GB2000138B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US80432077A 1977-06-07 1977-06-07
US87938178A 1978-02-21 1978-02-21

Publications (2)

Publication Number Publication Date
GB2000138A true GB2000138A (en) 1979-01-04
GB2000138B GB2000138B (en) 1982-03-03

Family

ID=27122691

Family Applications (1)

Application Number Title Priority Date Filing Date
GB7826308A Expired GB2000138B (en) 1977-06-07 1978-06-02 Therapeutic agents

Country Status (35)

Country Link
AR (1) AR224111A1 (en)
AT (2) AT360649B (en)
AU (1) AU513636B2 (en)
BE (1) BE867859A (en)
BG (2) BG34614A3 (en)
CH (1) CH634073A5 (en)
CS (1) CS208472B2 (en)
DD (2) DD148585A5 (en)
DE (2) DE2857263C3 (en)
DK (1) DK155740C (en)
EG (1) EG13869A (en)
FI (1) FI66003C (en)
FR (2) FR2393804A1 (en)
GB (1) GB2000138B (en)
GR (1) GR72255B (en)
HK (1) HK13184A (en)
HU (1) HU180042B (en)
IE (1) IE47079B1 (en)
IL (2) IL54867A (en)
IN (1) IN149747B (en)
IT (1) IT1096381B (en)
KE (1) KE3355A (en)
LU (1) LU79774A1 (en)
MY (1) MY8500092A (en)
NL (2) NL180009C (en)
NO (2) NO151746C (en)
NZ (1) NZ187476A (en)
OA (1) OA05964A (en)
PH (3) PH26810A (en)
PL (1) PL114501B1 (en)
PT (1) PT68146A (en)
SE (2) SE436206B (en)
SG (1) SG65383G (en)
SU (1) SU860706A1 (en)
YU (1) YU41829B (en)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0008917A1 (en) * 1978-09-01 1980-03-19 Pfizer Inc. Penam-3-carboxylic acid 1,1-dioxides, process for their preparation and pharmaceutical compositions
EP0018305A1 (en) * 1979-03-26 1980-10-29 Hoechst Uk Limited Oxapenem derivatives, their preparation, their use, pharmaceutical compositions containing them, diverse initial compounds and their preparation
US4448769A (en) * 1981-07-15 1984-05-15 Kanebo Ltd. Ester of 1,1-dioxopenicillanic acid, and use thereof as β-lactamase inhibitor
US4474698A (en) * 1980-12-11 1984-10-02 Pfizer Inc. Process for preparing esters of penicillanic acid sulfone
US4576754A (en) * 1983-10-18 1986-03-18 Gist-Brocades N.V. Preparation of 6,6-dibromo-penicillanic acid-1,1-dioxide
US4619786A (en) * 1982-04-19 1986-10-28 Gist-Brocades N.V. Preparation of 6-α-bromo- and/or 6,6-dibromo-penicillanic acid-1,1-dioxides
CN102977120A (en) * 2012-12-14 2013-03-20 江西富祥药业股份有限公司 Method for preparing and crystallizing sulbactam pivoxyl

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LU77306A1 (en) * 1977-05-09 1979-01-18
DE2912511C2 (en) * 1977-06-07 1982-06-24 Pfizer Inc., 10017 New York, N.Y. Pharmaceutical composition containing penicillanic acid
DK155942C (en) * 1977-12-23 1989-10-23 Pfizer METHOD OF ANALOGUE FOR THE PREPARATION OF 6-AMINOPENICILLANIC ACID-1,1-DIOXIDE AND PHYSIOLOGICALLY ACCEPTABLE ACID ADDITION AND BASIS SALTS.
JPS54126735A (en) * 1978-03-24 1979-10-02 Toyama Chem Co Ltd Bactericidal composition for medical use
CA1158639A (en) * 1978-12-11 1983-12-13 Eric M. Gordon 6-bromopenicillanic acid sulfone
IE49880B1 (en) * 1979-02-13 1986-01-08 Leo Pharm Prod Ltd Penicillin derivatives
US4714761A (en) * 1979-03-05 1987-12-22 Pfizer Inc. 6,6-dihalopenicillanic acid 1,1-dioxides and process
SE449103B (en) * 1979-03-05 1987-04-06 Pfizer SET TO PENICILLANIC ACID-1,1-DIOXIDE AND ESSERS THEREOF
US4420426A (en) 1979-03-05 1983-12-13 Pfizer Inc. 6-Alpha-halopenicillanic acid 1,1-dioxides
US4377524A (en) 1979-05-16 1983-03-22 Pfizer Inc. Bis-esters of methanediol with penicillins and penicillanic acid 1,1-dioxide
US4244951A (en) * 1979-05-16 1981-01-13 Pfizer Inc. Bis-esters of methanediol with penicillins and penicillanic acid 1,1-dioxide
US4309347A (en) * 1979-05-16 1982-01-05 Pfizer Inc. Penicillanoyloxymethyl penicillanate 1,1,1',1'-tetraoxide
IE49770B1 (en) * 1979-05-21 1985-12-11 Leo Pharm Prod Ltd 6beta-halopenicillanic acid derivatives
DE3051044C2 (en) * 1979-06-19 1989-03-30 Leo Pharmaceutical Products Ltd. A/S (Loevens Kemiske Fabrik Produktionsaktieselskab), Ballerup, Dk
US4256733A (en) * 1979-09-26 1981-03-17 Pfizer Inc. Acetoxymethyl penam compounds 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
IL61880A (en) * 1980-01-21 1984-11-30 Bristol Myers Co 2beta-chloromethyl-2alpha-methylpenam-3alpha-carboxylic acid sulfone derivatives,their preparation and pharmaceutical compositions containing them
US4488994A (en) * 1980-09-08 1984-12-18 Pfizer Inc. Bis-esters of methanediol with penicillins and penicillanic acid 1,1-dioxide
US4432903A (en) * 1980-09-08 1984-02-21 Pfizer Inc. Bis-esters of methanediol with penicillins and penicillanic acid 1,1-dioxide
US4419284A (en) * 1981-03-23 1983-12-06 Pfizer Inc. Preparation of halomethyl esters (and related esters) of penicillanic acid 1,1-dioxide
US4502988A (en) * 1983-08-08 1985-03-05 Eli Lilly And Company Oxidation process
US4647457A (en) * 1983-12-16 1987-03-03 Hoffmann-La Roche Inc. Penicillanic acid derivatives
WO1987006230A1 (en) * 1986-04-10 1987-10-22 Leo Pharmaceutical Products Ltd. A/S Method for preparing penicillanic acid derivatives
GB8808701D0 (en) * 1988-04-13 1988-05-18 Erba Carlo Spa Beta-lactam derivatives

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3197466A (en) * 1961-10-30 1965-07-27 Smith Kline French Lab Penicillin sulfoxides and process
LU77306A1 (en) * 1977-05-09 1979-01-18
EP0000636A1 (en) * 1977-07-13 1979-02-07 Glaxo Group Limited Penem compounds, processes for their preparation, their use in pharmaceutical compositions and azetidinones used in their preparation

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0008917A1 (en) * 1978-09-01 1980-03-19 Pfizer Inc. Penam-3-carboxylic acid 1,1-dioxides, process for their preparation and pharmaceutical compositions
EP0018305A1 (en) * 1979-03-26 1980-10-29 Hoechst Uk Limited Oxapenem derivatives, their preparation, their use, pharmaceutical compositions containing them, diverse initial compounds and their preparation
US4474698A (en) * 1980-12-11 1984-10-02 Pfizer Inc. Process for preparing esters of penicillanic acid sulfone
US4448769A (en) * 1981-07-15 1984-05-15 Kanebo Ltd. Ester of 1,1-dioxopenicillanic acid, and use thereof as β-lactamase inhibitor
US4619786A (en) * 1982-04-19 1986-10-28 Gist-Brocades N.V. Preparation of 6-α-bromo- and/or 6,6-dibromo-penicillanic acid-1,1-dioxides
US4576754A (en) * 1983-10-18 1986-03-18 Gist-Brocades N.V. Preparation of 6,6-dibromo-penicillanic acid-1,1-dioxide
CN102977120A (en) * 2012-12-14 2013-03-20 江西富祥药业股份有限公司 Method for preparing and crystallizing sulbactam pivoxyl
CN102977120B (en) * 2012-12-14 2015-05-27 江西富祥药业股份有限公司 Method for preparing and crystallizing sulbactam pivoxyl

Also Published As

Publication number Publication date
NO151746C (en) 1985-06-05
DE2857263B2 (en) 1981-04-23
FI66003B (en) 1984-04-30
PT68146A (en) 1978-07-01
IL62168A0 (en) 1981-03-31
NO152448C (en) 1985-10-02
YU41829B (en) 1988-02-29
NL7806126A (en) 1978-12-11
MY8500092A (en) 1985-12-31
BE867859A (en) 1978-12-06
PH21116A (en) 1987-07-16
EG13869A (en) 1983-03-31
IE781140L (en) 1978-12-07
BG34615A3 (en) 1983-10-15
OA05964A (en) 1981-06-30
GB2000138B (en) 1982-03-03
AT360649B (en) 1981-01-26
IL54867A0 (en) 1978-08-31
NO152448B (en) 1985-06-24
IT1096381B (en) 1985-08-26
NO781970L (en) 1978-12-08
DD148585A5 (en) 1981-06-03
DD140888A5 (en) 1980-04-02
NL180009C (en) 1986-12-16
HK13184A (en) 1984-02-24
AU3683878A (en) 1979-12-06
FI66003C (en) 1984-08-10
PL114501B1 (en) 1981-02-28
SG65383G (en) 1985-03-29
AR224111A1 (en) 1981-10-30
BG34614A3 (en) 1983-10-15
IL54867A (en) 1981-11-30
FR2393804B1 (en) 1980-11-07
KE3355A (en) 1983-12-16
DE2857263C3 (en) 1981-12-17
GR72255B (en) 1983-10-06
DE2824535B2 (en) 1980-05-14
DK155740C (en) 1989-10-23
IT7824270A0 (en) 1978-06-06
HU180042B (en) 1983-01-28
SE8305916D0 (en) 1983-10-27
ATA411278A (en) 1980-06-15
NL930064I2 (en) 1994-04-18
FI781800A7 (en) 1978-12-08
ATA128580A (en) 1981-02-15
SE7806628L (en) 1978-12-08
YU117078A (en) 1983-01-21
FR2393805B1 (en) 1984-02-24
CS208472B2 (en) 1981-09-15
PH16465A (en) 1983-10-20
LU79774A1 (en) 1980-01-22
NO823126L (en) 1978-12-08
DE2824535C3 (en) 1981-01-22
SE436206B (en) 1984-11-19
SU860706A1 (en) 1981-08-30
CH634073A5 (en) 1983-01-14
AT364084B (en) 1981-09-25
FR2393804A1 (en) 1979-01-05
IN149747B (en) 1982-04-03
DK251478A (en) 1978-12-08
FR2393805A1 (en) 1979-01-05
AU513636B2 (en) 1980-12-11
PH26810A (en) 1992-11-05
DE2824535A1 (en) 1978-12-14
PL207396A1 (en) 1979-06-04
NL930064I1 (en) 1993-09-01
NZ187476A (en) 1982-08-17
SE447995B (en) 1987-01-12
IE47079B1 (en) 1983-12-14
SE8305916L (en) 1983-10-27
DK155740B (en) 1989-05-08
NO151746B (en) 1985-02-18

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Legal Events

Date Code Title Description
CTFF Supplementary protection certificate filed

Free format text: SPC/GB93/049, 930525

CTFG Supplementary protection certificate granted

Free format text: SPC/GB93/049, 931110, EXPIRES:20000826

CTFE Supplementary protection certificate entered into force

Free format text: SPC/GB93/049, 980602, EXPIRES: 20000826

PE20 Patent expired after termination of 20 years

Effective date: 19980601

SPCE Supplementary protection certificate expired

Free format text: SPC/GB93/049, 20000826