MC2021A1 - PREPARATION OF ACYLIC DERIVATIVES FOR USE IN PARTICULAR FOR THE MANUFACTURE OF MEDICAMENTS - Google Patents

PREPARATION OF ACYLIC DERIVATIVES FOR USE IN PARTICULAR FOR THE MANUFACTURE OF MEDICAMENTS

Info

Publication number
MC2021A1
MC2021A1 MC892042A MC2042A MC2021A1 MC 2021 A1 MC2021 A1 MC 2021A1 MC 892042 A MC892042 A MC 892042A MC 2042 A MC2042 A MC 2042A MC 2021 A1 MC2021 A1 MC 2021A1
Authority
MC
Monaco
Prior art keywords
compounds
preparation
image
substituted
heterocycle
Prior art date
Application number
MC892042A
Other languages
French (fr)
Inventor
Allen Albrecht Harry
Dalton Keith Dennis
Martin Konzelmann Frederick
Loreen Rossman Pamela
Wei Chung-Chen
Weigele Manfred
Yang Roxana
Original Assignee
Hoffmann La Roche
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
Priority claimed from US07/197,943 external-priority patent/US5336768A/en
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MC2021A1 publication Critical patent/MC2021A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D501/00—Heterocyclic 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; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D501/14—Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16—Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/20—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • C07D501/24—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
    • C07D501/38—Methylene radicals, substituted by nitrogen atoms; Lactams thereof with the 2-carboxyl group; Methylene radicals substituted by nitrogen-containing hetero rings attached by the ring nitrogen atom; Quaternary compounds thereof
    • C07D501/46—Methylene radicals, substituted by nitrogen atoms; Lactams thereof with the 2-carboxyl group; Methylene radicals substituted by nitrogen-containing hetero rings attached by the ring nitrogen atom; Quaternary compounds thereof with the 7-amino radical acylated by carboxylic acids containing hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D501/00—Heterocyclic 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; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D501/14—Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16—Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/18—7-Aminocephalosporanic or substituted 7-aminocephalosporanic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D501/00—Heterocyclic 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; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D501/14—Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16—Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/20—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • C07D501/24—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
    • C07D501/26—Methylene radicals, substituted by oxygen atoms; Lactones thereof with the 2-carboxyl group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D501/00—Heterocyclic 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; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D501/14—Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16—Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/20—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • C07D501/24—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
    • C07D501/26—Methylene radicals, substituted by oxygen atoms; Lactones thereof with the 2-carboxyl group
    • C07D501/32—Methylene radicals, substituted by oxygen atoms; Lactones thereof with the 2-carboxyl group with the 7-amino radical acylated by an araliphatic carboxylic acid, which is substituted on the aliphatic radical by hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D501/00—Heterocyclic 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; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D501/14—Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16—Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/20—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • C07D501/24—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
    • C07D501/26—Methylene radicals, substituted by oxygen atoms; Lactones thereof with the 2-carboxyl group
    • C07D501/34—Methylene radicals, substituted by oxygen atoms; Lactones thereof with the 2-carboxyl group with the 7-amino radical acylated by carboxylic acids containing hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D501/00—Heterocyclic 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; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D501/14—Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16—Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/20—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • C07D501/24—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
    • C07D501/38—Methylene radicals, substituted by nitrogen atoms; Lactams thereof with the 2-carboxyl group; Methylene radicals substituted by nitrogen-containing hetero rings attached by the ring nitrogen atom; Quaternary compounds thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D501/00—Heterocyclic 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; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D501/14—Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16—Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/20—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • C07D501/24—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
    • C07D501/38—Methylene radicals, substituted by nitrogen atoms; Lactams thereof with the 2-carboxyl group; Methylene radicals substituted by nitrogen-containing hetero rings attached by the ring nitrogen atom; Quaternary compounds thereof
    • C07D501/44—Methylene radicals, substituted by nitrogen atoms; Lactams thereof with the 2-carboxyl group; Methylene radicals substituted by nitrogen-containing hetero rings attached by the ring nitrogen atom; Quaternary compounds thereof with the 7-amino radical acylated by an araliphatic carboxylic acid, which is substituted on the aliphatic radical by hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Communicable Diseases (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Cephalosporin Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Tension Adjustment In Filamentary Materials (AREA)
  • Communication Cables (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Acyl derivatives of the general formula <IMAGE> in which R<1> denotes a substituted N-heterocycle of the formulae <IMAGE> in which R<1><0> represents one of the groups <IMAGE> and Q represents a substituted quinolinyl or naphthyridinyl group, where the N-heterocycle can optionally be substituted by one or more lower alkyl groups; and in which R<2> additionally represents hydrogen, lower alkoxy, lower alkylthio or lower alkanoylamino, R<3> represents an acyl group, m represents 0, 1 or 2 and A represents a pharmaceutically tolerable anion, and easily hydrolysable esters and pharmaceutically tolerable salts of these compounds and hydrates of the compounds of the formula I or of their esters and salts and a process for their preparation and pharmaceutical preparations which contain this compound, and also intermediates for the preparation of these compounds, and additionally the use of the compounds for the control of diseases and for the production of the preparations mentioned are described. The products have antibiotic activity.
MC892042A 1988-03-31 1989-03-29 PREPARATION OF ACYLIC DERIVATIVES FOR USE IN PARTICULAR FOR THE MANUFACTURE OF MEDICAMENTS MC2021A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US17547188A 1988-03-31 1988-03-31
US07/197,943 US5336768A (en) 1988-05-24 1988-05-24 Antibacterial cephalosporin compounds
EP89102071 1989-02-07

Publications (1)

Publication Number Publication Date
MC2021A1 true MC2021A1 (en) 1990-02-23

Family

ID=27232316

Family Applications (1)

Application Number Title Priority Date Filing Date
MC892042A MC2021A1 (en) 1988-03-31 1989-03-29 PREPARATION OF ACYLIC DERIVATIVES FOR USE IN PARTICULAR FOR THE MANUFACTURE OF MEDICAMENTS

Country Status (16)

Country Link
EP (1) EP0335297B1 (en)
JP (1) JPH01299290A (en)
KR (1) KR890014562A (en)
AT (1) ATE135357T1 (en)
AU (1) AU624810B2 (en)
DE (1) DE58909620D1 (en)
DK (1) DK154589A (en)
FI (1) FI891498A (en)
HU (1) HUT49889A (en)
IL (1) IL89785A0 (en)
IS (1) IS3452A7 (en)
MC (1) MC2021A1 (en)
NO (1) NO171915C (en)
NZ (1) NZ228498A (en)
PT (1) PT90163B (en)
YU (1) YU63689A (en)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5147871A (en) * 1986-07-03 1992-09-15 Hoffmann La-Roche, Inc. Anti-bacterial cephalosporin compounds
US5180719A (en) * 1988-10-24 1993-01-19 Norwich Eaton Pharmaceuticals, Inc. Antimicrobial quinolonyl lactam esters
US5328908A (en) * 1988-10-24 1994-07-12 Procter & Gamble Pharmaceuticals, Inc. Antimicrobial quinolone thioureas
EP0366189A3 (en) * 1988-10-24 1992-01-02 Norwich Eaton Pharmaceuticals, Inc. Novel antimicrobial lactam-quinolones
US5273973A (en) * 1988-10-24 1993-12-28 Norwich Eaton Pharmaceuticals, Inc. Antimicrobial quinolonyl esters
US5491139A (en) * 1988-10-24 1996-02-13 The Procter & Gamble Company Antimicrobial quinolonyl lactams
CA2001203C (en) * 1988-10-24 2001-02-13 Thomas P. Demuth, Jr. Novel antimicrobial dithiocarbamoyl quinolones
GB8907617D0 (en) * 1989-04-05 1989-05-17 Celltech Ltd Drug delivery system
US5162523A (en) * 1989-07-21 1992-11-10 Hoffmann-La Roche Inc. Cephalosporin antibacterial compounds
US5159077A (en) * 1989-07-21 1992-10-27 Hoffmann-La Roche Inc. Penam antibacterial compounds
WO1991016327A1 (en) * 1990-04-18 1991-10-31 Norwich Eaton Pharmaceuticals, Inc. Antimicrobial quinolonyl lactams
EP0492277A3 (en) * 1990-12-20 1992-10-14 F. Hoffmann-La Roche Ag Cephalosporin derivatives
CZ73194A3 (en) * 1991-10-01 1994-11-16 Procter & Gamble Pharma Process for preparing anti-microbial quinolonyl-lactams
EP0550775A1 (en) * 1992-01-07 1993-07-14 F. Hoffmann-La Roche Ag Cephalosporin derivatives
JPH05230068A (en) * 1992-02-07 1993-09-07 Kyoto Yakuhin Kogyo Kk 3-di-substituted carbamoyloxymethylcephalosporin compound, its production and intermediate compound
DE4234078A1 (en) * 1992-10-09 1994-04-14 Bayer Ag Quinolonecarboxylic acids
CA2108609A1 (en) * 1992-11-12 1994-05-13 Scott L. Dax Cephalosporin derivatives
US7847093B2 (en) 2003-04-16 2010-12-07 Sandoz Ag Processes for the preparations of cefepime

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3706746A (en) * 1968-11-07 1972-12-19 Ciba Geigy Corp O-desacetyl derivatives of 7-n-acylamino-cephalosphoranic acids
US4525473A (en) * 1983-03-30 1985-06-25 Bristol-Myers Company Cephalosporins
DE3409431A1 (en) * 1983-10-08 1985-04-18 Hoechst Ag, 6230 Frankfurt CEPHALOSPORINE DERIVATIVES AND METHOD FOR THEIR PRODUCTION
NZ211223A (en) * 1984-03-05 1988-02-12 Teijin Ltd Cephalosporins and pharmaceutical compositions
DE3506159A1 (en) * 1985-02-22 1986-08-28 Bayer Ag, 5090 Leverkusen NEW CEPHALOSPORINE, METHOD FOR THEIR PRODUCTION AND THEIR USE IN MEDICINAL PRODUCTS
ZA874696B (en) * 1986-07-03 1988-01-04 F. Hoffmann-La Roche & Co. Aktiengesellschaft Acyl derivatives
ZA877987B (en) * 1986-11-12 1988-08-31 Ici Pharma Antibiotic compounds
EP0366189A3 (en) * 1988-10-24 1992-01-02 Norwich Eaton Pharmaceuticals, Inc. Novel antimicrobial lactam-quinolones

Also Published As

Publication number Publication date
EP0335297A2 (en) 1989-10-04
YU63689A (en) 1991-06-30
NO891350L (en) 1989-10-02
IL89785A0 (en) 1989-09-28
PT90163A (en) 1989-11-10
EP0335297A3 (en) 1991-07-31
ATE135357T1 (en) 1996-03-15
AU3227189A (en) 1989-10-12
JPH01299290A (en) 1989-12-04
NO171915C (en) 1993-05-19
IS3452A7 (en) 1989-10-02
EP0335297B1 (en) 1996-03-13
AU624810B2 (en) 1992-06-25
KR890014562A (en) 1989-10-24
FI891498A (en) 1989-10-01
FI891498A0 (en) 1989-03-29
DE58909620D1 (en) 1996-04-18
NO171915B (en) 1993-02-08
NO891350D0 (en) 1989-03-30
DK154589A (en) 1989-10-01
DK154589D0 (en) 1989-03-30
NZ228498A (en) 1991-08-27
HUT49889A (en) 1989-11-28
PT90163B (en) 1994-06-30

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