AR026682A1 - CARBAPENEM COMPOSITE, USE OF THE SAME AND ITS INTERMEDIARY COMPOUND - Google Patents

CARBAPENEM COMPOSITE, USE OF THE SAME AND ITS INTERMEDIARY COMPOUND

Info

Publication number
AR026682A1
AR026682A1 ARP000106344A ARP000106344A AR026682A1 AR 026682 A1 AR026682 A1 AR 026682A1 AR P000106344 A ARP000106344 A AR P000106344A AR P000106344 A ARP000106344 A AR P000106344A AR 026682 A1 AR026682 A1 AR 026682A1
Authority
AR
Argentina
Prior art keywords
carbapenem
formula
compound
antibacterial
compounds
Prior art date
Application number
ARP000106344A
Other languages
Spanish (es)
Original Assignee
Kyoto Pharma Ind
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
Application filed by Kyoto Pharma Ind filed Critical Kyoto Pharma Ind
Publication of AR026682A1 publication Critical patent/AR026682A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D477/00—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring
    • C07D477/10—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with 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
    • C07D477/12—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with 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 hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6
    • C07D477/16—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with 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 hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6 with hetero atoms or carbon atoms 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 3
    • C07D477/20—Sulfur atoms
    • 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

Abstract

Se hallaron muchos compuestos que tienen un esqueleto de carbapenem como agentes para el tratamiento de enfermedades infecciosas, de los cuales algunoscompuestos de carbapenem que tienen una actividad antibacteriana superior están en uso o en desarro llo para su aplicacion práctica. Por otro lado, loscompuestos de carbapenem en uso actualmente muestran una absorcion gástrica insuficiente y se administran como una inyeccion en uso clínico. Un agente oral seadministra más fácil y convenientemente, y es clínicamente muy util. Por ello, existe una fuerte demanda para el desarrollo de un compuesto de carbapenem paraadministracion oral, que tenga una potente actividad antibacteriana y un amplio espectro antibacteriano y que muestre una absorcion g ástrica superior. Uncompuesto de carbapenem de la formula (1) donde: R1 es un grupo acilo de un alfa-aminoácido, donde el amino está opcionalmente sustituído por alquilo inferior;R2 es un átomo de hidrogeno o un alquilo inferior; y R3 es un fenilo op cionalmente sustituido; o una sal farmacéuticamente aceptable del mismo. Un agenteantibacteriano que comprende el compuesto de carbapenem descripto, o una sal farmacéuticamente aceptable del mismo como un ingrediente activo. Dicho agenteantibacterian o está destinado a la administracion oral. Un compuesto de carbapenem de la formula (2) que tiene la estructura de la formula (1) en donde R1 es Hy es de utilidad en la síntesis de dicho derivado de formula (1).Many compounds were found that have a carbapenem skeleton as agents for the treatment of infectious diseases, of which some carbapenem compounds that have superior antibacterial activity are in use or in development for practical application. On the other hand, the carbapenem compounds in use currently show insufficient gastric absorption and are administered as an injection in clinical use. An oral agent is administered more easily and conveniently, and is clinically very useful. Therefore, there is a strong demand for the development of a carbapenem compound for oral administration, which has a potent antibacterial activity and a broad antibacterial spectrum and that shows a superior gastric absorption. A carbapenem compound of the formula (1) wherein: R1 is an acyl group of an alpha-amino acid, where the amino is optionally substituted by lower alkyl; R2 is a hydrogen atom or a lower alkyl; and R3 is an optionally substituted phenyl; or a pharmaceutically acceptable salt thereof. An antibacterial agent comprising the described carbapenem compound, or a pharmaceutically acceptable salt thereof as an active ingredient. Said antibacterial agent or is intended for oral administration. A carbapenem compound of the formula (2) having the structure of the formula (1) wherein R1 is Hy is useful in the synthesis of said derivative of formula (1).

ARP000106344A 1999-12-03 2000-12-01 CARBAPENEM COMPOSITE, USE OF THE SAME AND ITS INTERMEDIARY COMPOUND AR026682A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP34553599 1999-12-03

Publications (1)

Publication Number Publication Date
AR026682A1 true AR026682A1 (en) 2003-02-19

Family

ID=18377257

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP000106344A AR026682A1 (en) 1999-12-03 2000-12-01 CARBAPENEM COMPOSITE, USE OF THE SAME AND ITS INTERMEDIARY COMPOUND

Country Status (4)

Country Link
AR (1) AR026682A1 (en)
AU (1) AU1419501A (en)
CO (1) CO5261620A1 (en)
WO (1) WO2001040228A1 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114716487B (en) * 2022-02-24 2024-03-08 四川农业大学 Furanodiester compound and preparation method and application thereof

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3965099A (en) * 1974-06-26 1976-06-22 Smithkline Corporation Cephalosporin esters with antibacterial activity
US4503040A (en) * 1984-02-27 1985-03-05 Pfizer Inc. 6-(Aminoacyloxymethyl)penicillanic acid 1,1-dioxides as beta-lactamase inhibitors
JP2847693B2 (en) * 1992-06-18 1999-01-20 田辺製薬株式会社 Removal method of carboxyl group protecting group
JPH06298769A (en) * 1993-04-13 1994-10-25 Fujisawa Pharmaceut Co Ltd Ampicillin phenyl ester and its salt
JP2000239275A (en) * 1998-12-25 2000-09-05 Sankyo Co Ltd Carbapenem ester derivative

Also Published As

Publication number Publication date
AU1419501A (en) 2001-06-12
CO5261620A1 (en) 2003-03-31
WO2001040228A1 (en) 2001-06-07

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