FR2393804A1 - 1,1-dioxydes de l'acide penicillanique et de ses esters utiles comme inhibiteurs de la b-lactamase - Google Patents

1,1-dioxydes de l'acide penicillanique et de ses esters utiles comme inhibiteurs de la b-lactamase

Info

Publication number
FR2393804A1
FR2393804A1 FR787816893A FR7816893A FR2393804A1 FR 2393804 A1 FR2393804 A1 FR 2393804A1 FR 787816893 A FR787816893 A FR 787816893A FR 7816893 A FR7816893 A FR 7816893A FR 2393804 A1 FR2393804 A1 FR 2393804A1
Authority
FR
France
Prior art keywords
penicillanic acid
dioxides
lactamase inhibitors
beta
esters 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
FR787816893A
Other languages
English (en)
Other versions
FR2393804B1 (fr
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 Inc
Original Assignee
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=FR2393804(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to FR7537160A priority Critical patent/FR2293805A1/fr
Application filed by Pfizer Inc filed Critical Pfizer Inc
Publication of FR2393804A1 publication Critical patent/FR2393804A1/fr
Application granted granted Critical
Publication of FR2393804B1 publication Critical patent/FR2393804B1/fr
Granted legal-status Critical Current

Links

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
    • 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
    • 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

L'invention concerne des 1,1-dioxydes d'acide et d'esters pénicillaniques utiles comme inhibiteurs de la beta -lactamase. Les composés de l'invention sont des 1,1-dioxydes d'acide pénicillanique et d'esters correspondants facilement hydrolysables in vivo et des dérivés de 1,1-dioxyde de l'acide pénicillanique dont le radical carboxy est protégé par un groupe protecteur classique du radical carboxy des pénicillines qui sont des intermédiaires utiles pour la synthèse du 1,1-dioxyde de l'acide pénicillanique. Les 1,1-dioxydes d'acide et d'esters pénicillaniques de l'invention sont des agents antibactériens, capables également d'accroître l'efficacité de divers antibiotiques du type beta -lactame vis-à-vis des bactéries productrices de beta -lactamase.
FR787816893A 1974-12-05 1978-06-06 1,1-dioxydes de l'acide penicillanique et de ses esters utiles comme inhibiteurs de la b-lactamase Granted FR2393804A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
FR7537160A FR2293805A1 (fr) 1974-12-05 1975-12-04 Pile ou batterie d'accumulateurs electrochimique

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
FR2393804A1 true FR2393804A1 (fr) 1979-01-05
FR2393804B1 FR2393804B1 (fr) 1980-11-07

Family

ID=27122691

Family Applications (2)

Application Number Title Priority Date Filing Date
FR787816893A Granted FR2393804A1 (fr) 1974-12-05 1978-06-06 1,1-dioxydes de l'acide penicillanique et de ses esters utiles comme inhibiteurs de la b-lactamase
FR787826789A Granted FR2393805A1 (fr) 1977-06-07 1978-09-19 1-oxyde de l'acide penicillanique et de ses esters utiles comme intermediaires chimiques

Family Applications After (1)

Application Number Title Priority Date Filing Date
FR787826789A Granted FR2393805A1 (fr) 1977-06-07 1978-09-19 1-oxyde de l'acide penicillanique et de ses esters utiles comme intermediaires chimiques

Country Status (35)

Country Link
AR (1) AR224111A1 (fr)
AT (2) AT360649B (fr)
AU (1) AU513636B2 (fr)
BE (1) BE867859A (fr)
BG (2) BG34615A3 (fr)
CH (1) CH634073A5 (fr)
CS (1) CS208472B2 (fr)
DD (2) DD148585A5 (fr)
DE (2) DE2824535C3 (fr)
DK (1) DK155740C (fr)
EG (1) EG13869A (fr)
FI (1) FI66003C (fr)
FR (2) FR2393804A1 (fr)
GB (1) GB2000138B (fr)
GR (1) GR72255B (fr)
HK (1) HK13184A (fr)
HU (1) HU180042B (fr)
IE (1) IE47079B1 (fr)
IL (2) IL54867A (fr)
IN (1) IN149747B (fr)
IT (1) IT1096381B (fr)
KE (1) KE3355A (fr)
LU (1) LU79774A1 (fr)
MY (1) MY8500092A (fr)
NL (2) NL180009C (fr)
NO (2) NO151746C (fr)
NZ (1) NZ187476A (fr)
OA (1) OA05964A (fr)
PH (3) PH26810A (fr)
PL (1) PL114501B1 (fr)
PT (1) PT68146A (fr)
SE (2) SE436206B (fr)
SG (1) SG65383G (fr)
SU (1) SU860706A1 (fr)
YU (1) YU41829B (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2442053A2 (fr) * 1977-06-07 1980-06-20 Pfizer Composition pharmaceutique a base d'acide 7-(d-2-(4-ethylpiperazine-2,3-dione-1-carboxamido)-2-(4-hydroxyphenyl) acetamido) -3- ((1-methyl-5-tetrazolyl) thiomethyl)-3-desacetoxymethylcephalosporanique et de 1,1-dioxyde d'acide penicillanique
FR2465736A1 (fr) * 1979-09-26 1981-03-27 Pfizer Composes penam acetoxymethyles et composition pharmaceutique les contenant

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LU77306A1 (fr) * 1977-05-09 1979-01-18
DK155942C (da) * 1977-12-23 1989-10-23 Pfizer Analogifremgangsmaade til fremstilling af 6-aminopenicillansyre-1,1-dioxid og fysiologisk acceptable syreadditions- og basesalte deraf.
JPS54126735A (en) * 1978-03-24 1979-10-02 Toyama Chem Co Ltd Bactericidal composition for medical use
US4241050A (en) * 1978-09-01 1980-12-23 Pfizer Inc. Penam 1,1-dioxides as beta-lactamase inhibitors
CA1158639A (fr) * 1978-12-11 1983-12-13 Eric M. Gordon Acide 6-bromopenicillanique sulfone
IE49881B1 (en) * 1979-02-13 1986-01-08 Leo Pharm Prod Ltd B-lactam intermediates
US4714761A (en) * 1979-03-05 1987-12-22 Pfizer Inc. 6,6-dihalopenicillanic acid 1,1-dioxides and process
SE449103B (sv) * 1979-03-05 1987-04-06 Pfizer Sett att framstella penicillansyra-1,1-dioxid samt estrar derav
US4420426A (en) 1979-03-05 1983-12-13 Pfizer Inc. 6-Alpha-halopenicillanic acid 1,1-dioxides
GB2045236A (en) * 1979-03-26 1980-10-29 Hoechst Uk Ltd Oxapenem derivatives
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
IE49768B1 (en) * 1979-05-21 1985-12-11 Leo Pharm Prod Ltd 6beta-halopenicillanic acid derivatives
DE3051044C2 (fr) * 1979-06-19 1989-03-30 Leo Pharmaceutical Products Ltd. A/S (Loevens Kemiske Fabrik Produktionsaktieselskab), Ballerup, Dk
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
US4432903A (en) * 1980-09-08 1984-02-21 Pfizer Inc. Bis-esters of methanediol with penicillins and penicillanic acid 1,1-dioxide
US4488994A (en) * 1980-09-08 1984-12-18 Pfizer Inc. Bis-esters of methanediol with penicillins and penicillanic acid 1,1-dioxide
US4474698A (en) * 1980-12-11 1984-10-02 Pfizer Inc. Process for preparing esters of penicillanic acid sulfone
US4419284A (en) * 1981-03-23 1983-12-06 Pfizer Inc. Preparation of halomethyl esters (and related esters) of penicillanic acid 1,1-dioxide
EP0069962B1 (fr) * 1981-07-15 1985-01-02 Kanebo, Ltd. Ester d'acide 1,1-dioxopénicillanique, procédé pour sa production et son application comme inhibiteur de bêta-lactamase
PT76527B (en) * 1982-04-19 1985-12-09 Gist Brocades Nv A process for the preparation of penicillanic acid 1,1-dioxide and derivatives thereof
US4502988A (en) * 1983-08-08 1985-03-05 Eli Lilly And Company Oxidation process
EP0139047A1 (fr) * 1983-10-18 1985-05-02 Gist-Brocades N.V. Procédé de préparation de 1,1-dioxyde d'acide 6,6-dibromopénicillanique
US4647457A (en) * 1983-12-16 1987-03-03 Hoffmann-La Roche Inc. Penicillanic acid derivatives
EP0262202B1 (fr) * 1986-04-10 1992-07-01 Leo Pharmaceutical Products Ltd. A/S (Lovens Kemiske Fabrik Produktionsaktieselskab) Procede servant a preparer des derives d'acide penicillanique
GB8808701D0 (en) * 1988-04-13 1988-05-18 Erba Carlo Spa Beta-lactam derivatives
CN102977120B (zh) * 2012-12-14 2015-05-27 江西富祥药业股份有限公司 一种舒巴坦匹酯制备及结晶方法

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 (fr) * 1977-05-09 1979-01-18
AU3796278A (en) * 1977-07-13 1980-01-17 Glaxo Group Ltd Penams and azetidinones

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
NV6015C *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2442053A2 (fr) * 1977-06-07 1980-06-20 Pfizer Composition pharmaceutique a base d'acide 7-(d-2-(4-ethylpiperazine-2,3-dione-1-carboxamido)-2-(4-hydroxyphenyl) acetamido) -3- ((1-methyl-5-tetrazolyl) thiomethyl)-3-desacetoxymethylcephalosporanique et de 1,1-dioxyde d'acide penicillanique
FR2465736A1 (fr) * 1979-09-26 1981-03-27 Pfizer Composes penam acetoxymethyles et composition pharmaceutique les contenant

Also Published As

Publication number Publication date
BG34614A3 (en) 1983-10-15
DE2824535A1 (de) 1978-12-14
PH26810A (en) 1992-11-05
YU117078A (en) 1983-01-21
PL207396A1 (pl) 1979-06-04
SE8305916L (sv) 1983-10-27
IL54867A0 (en) 1978-08-31
IL62168A0 (en) 1981-03-31
NL7806126A (nl) 1978-12-11
NL930064I1 (nl) 1993-09-01
FI66003B (fi) 1984-04-30
FI781800A (fi) 1978-12-08
DE2857263B2 (de) 1981-04-23
ATA128580A (de) 1981-02-15
IT1096381B (it) 1985-08-26
SE8305916D0 (sv) 1983-10-27
MY8500092A (en) 1985-12-31
CS208472B2 (en) 1981-09-15
FR2393804B1 (fr) 1980-11-07
HK13184A (en) 1984-02-24
OA05964A (fr) 1981-06-30
CH634073A5 (en) 1983-01-14
NO152448B (no) 1985-06-24
FI66003C (fi) 1984-08-10
AR224111A1 (es) 1981-10-30
NO823126L (no) 1978-12-08
NO151746B (no) 1985-02-18
HU180042B (en) 1983-01-28
DK251478A (da) 1978-12-08
FR2393805A1 (fr) 1979-01-05
NO152448C (no) 1985-10-02
NZ187476A (en) 1982-08-17
KE3355A (en) 1983-12-16
PH21116A (en) 1987-07-16
DK155740C (da) 1989-10-23
DK155740B (da) 1989-05-08
LU79774A1 (fr) 1980-01-22
SE7806628L (sv) 1978-12-08
IL54867A (en) 1981-11-30
DE2824535C3 (de) 1981-01-22
BG34615A3 (en) 1983-10-15
IE47079B1 (en) 1983-12-14
AU3683878A (en) 1979-12-06
PT68146A (en) 1978-07-01
NO781970L (no) 1978-12-08
NL930064I2 (nl) 1994-04-18
SG65383G (en) 1985-03-29
PH16465A (en) 1983-10-20
IN149747B (fr) 1982-04-03
BE867859A (fr) 1978-12-06
AT364084B (de) 1981-09-25
YU41829B (en) 1988-02-29
FR2393805B1 (fr) 1984-02-24
IT7824270A0 (it) 1978-06-06
NO151746C (no) 1985-06-05
DD148585A5 (de) 1981-06-03
GR72255B (fr) 1983-10-06
DE2857263C3 (de) 1981-12-17
DD140888A5 (de) 1980-04-02
NL180009C (nl) 1986-12-16
EG13869A (en) 1983-03-31
IE781140L (en) 1978-12-07
AU513636B2 (en) 1980-12-11
GB2000138A (en) 1979-01-04
GB2000138B (en) 1982-03-03
AT360649B (de) 1981-01-26
SE447995B (sv) 1987-01-12
ATA411278A (de) 1980-06-15
SE436206B (sv) 1984-11-19
DE2824535B2 (de) 1980-05-14
PL114501B1 (en) 1981-02-28
SU860706A1 (ru) 1981-08-30

Similar Documents

Publication Publication Date Title
FR2393804A1 (fr) 1,1-dioxydes de l'acide penicillanique et de ses esters utiles comme inhibiteurs de la b-lactamase
IE801007L (en) Penicillins
FI931888A (fi) Kramploesande cykliska fruktopyranossulfiter -och sulfater
MY127641A (en) Cephalosporin antibiotics
FR2361406A1 (fr) Esters de cephalosporines
FR2373546A1 (fr) Derives thio-oxime de cephalosporines et de penicillines, utiles comme inhibiteurs de b-lactamases
SE8500965D0 (sv) Mellanprodukter for framstellning av beta-laktamasinhibitorer
ES8103094A1 (es) Un procedimiento para la preparacion de 1,1-dioxido de acidopenicilanico y esteres del mismo
DE3265082D1 (en) Beta-lactamase inhibiting 2-beta-substituted-2-alpha-methyl-(5r) penam-3-alpha-carboxylic acid 1,1-dioxides and intermediates therefor
ES455404A1 (es) Un procedimiento para la preparacion de nuevos derivados de beta-lactama.
SE8001689L (sv) 6-beta-substituerade penicillansyror med beta-laktamas-inhibitorverkan
FR2355848A1 (fr) 7-(a-(2,3-dihydro-2-oxobenzimidazol-1-yl-carbonylamino) arylacetamido) cephalosporines
IE820342L (en) Penicillins
IE852246L (en) Penicillins
DE3062787D1 (en) Novel process for the preparation of 6-aminopenicillanic acid-1,1-dioxide and its salts
ES8301236A1 (es) Un procedimiento para la preparacion de derivados del acido 2 beta-clorometil-2 alfa-metilpenam-3 alfa-carboxilico.
IL67523A0 (en) Bis-hydroxymethyl carbonate bridged penicillins and pharmaceutical compositions containing them
FR2431861A1 (fr) Composition destinee a l'hygiene buccale
ES476259A1 (es) Un procedimiento para la preparacion de un compuesto.
ITMI950971A1 (it) Derivati aminotiazolici di cefalosporine aventi attivita' antibatterica
JPS5664795A (en) Preparation of cephalosporin analog

Legal Events

Date Code Title Description
CC Supplementary protection certificate (spc) laid open to the public (law of 25 june 1990)

Free format text: 92C0343, 920527

CB Supplementary protection certificate (spc) granted (law of 25 june 1990)

Free format text: 92C0343, 780606

CL Concession to grant licences