EP0614364A1 - Procedes et compositions destines a traiter des infections a l'aide de (s)-lomefloxacine optiquement pure - Google Patents

Procedes et compositions destines a traiter des infections a l'aide de (s)-lomefloxacine optiquement pure

Info

Publication number
EP0614364A1
EP0614364A1 EP92925403A EP92925403A EP0614364A1 EP 0614364 A1 EP0614364 A1 EP 0614364A1 EP 92925403 A EP92925403 A EP 92925403A EP 92925403 A EP92925403 A EP 92925403A EP 0614364 A1 EP0614364 A1 EP 0614364A1
Authority
EP
European Patent Office
Prior art keywords
lomefloxacin
amount
composition according
pharmaceutically acceptable
adverse effects
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.)
Ceased
Application number
EP92925403A
Other languages
German (de)
English (en)
Other versions
EP0614364A4 (fr
Inventor
James W. Young
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.)
Sumitomo Pharma America Inc
Original Assignee
Sepracor 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
Application filed by Sepracor Inc filed Critical Sepracor Inc
Publication of EP0614364A1 publication Critical patent/EP0614364A1/fr
Publication of EP0614364A4 publication Critical patent/EP0614364A4/fr
Ceased 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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

Definitions

  • Bacterial infections of the lower urinary tract are very common. The majority of urinary tract infections are caused by gram- negative bacteria. Organisms gaining access to the urethra may colonize on the periurethral glands and produce acute and chronic infection. This condition is termed urethritis. Infections of the prostate gland give rise to the condition prostatitis. Enteric, gram-negative organisms are the most common cause of prostate infection. Merck Manual 5th Ed., p. 1610, Merck, Sharpe & Dohme Research Laboratories (1987) .
  • lomefloxacin and quinoline antibiotics have several advantages, they also have disadvantages, namely, adverse effects.
  • the adverse effects of quinoline antibiotics in general include arthropathy, headache, stomach discomfort, gastrointestinal disorders, hypoglycemia, renal and hepatic dysfunction, allergic reactions and respiratory distress, and central nervous system effects including convulsions, increased intracranial pressure, and toxic psychoses.
  • the adverse effects of lomefloxacin in particular, include but are not limited to headache, stomach discomfort, gastrointestinal disorders, and arthropathy, such as cartilage lesions and erosion and abnormalities in bone growth in immature patients.
  • it would be particularly desirable to find a compound with the advantages of the racemic mixture of lomefloxacin which would not have the aforementioned disadvantages.
  • the present invention also encompasses an antibiotic composition for treating infection in a human which comprises, an amount of (S)-lomefloxacin or a pharmaceutically acceptable salt thereof, substantially free of its (R)-stereoisomer, said amount being sufficient to alleviate said infection but insufficient to cause adverse effects associated with lomefloxacin.
  • any suitable route of administration may be employed for providing the patient with an effective dosage of (S)-lomefloxacin.
  • oral, rectal, parenteral, transdermal, subcutaneous. intramuscular, and the like may be employed as appropriate.
  • Dosage forms include tablets, coated tablets, troches, dispersions, suspensions, solutions, caplets, capsules, patches, and the like.
  • the pharmaceutical compositions of the present invention comprise (S)-lomefloxacin as active ingredient, or a pharmaceutically acceptable salt thereof, and may also contain a pharmaceutically acceptable carrier, and optionally, other therapeutic ingredients.
  • (S)-lomefloxacin hydrochloride is a pharmaceutically acceptable salt of (S)-lomefloxacin.
  • the most preferred pharmaceutically acceptable salt of (S)-lomefloxacin is the monohydrochloride salt.
  • salts refers to salts prepared from pharmaceutically acceptable non-toxic acids or bases including inorganic acids and bases and organic acids and bases. Since the compound of the present invention is both basic and acidic, salts may be prepared from pharmaceutically acceptable non-toxic acids or bases including inorganic and organic acids or inorganic and organic bases. Such salts may contain any of the following anions: acetate, benzensulfonate, benzoate, camphorsulfonate, citrate, fumarate, gluconate, hydrobromide, hydrochloride, lactate, maleate, mandelate, mucate, nitrate, pamoate, phosphate, succinate, sulfate, tartrate and the like.
  • a suitable dosage range for use is e.g., from about 100 mg to about 400 mg total daily dose, given as a once daily administration in the morning or in divided doses if required.
  • a dose of 400 mg is given as a once daily administration.
  • a dose range of between about 100 mg to about 200 mg is given as a once daily administration or in divided doses if required.
  • Patients may be upward titrated from below to within this dose range to a satisfactory control of symptoms.
  • (S)-lomefloxacin can be combined as the active ingredient in intimate admixture with a pharmaceutical carrier according to conventional pharmaceutical compounding techniques.

Landscapes

  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Procédés et compositions utilisant l'isomère (S) optiquement pur de loméfloxacine. Ce composé est un médicament puissant destiné à traiter des infections et d'autres maladies nécessitant des antibiotiques, tout en évitant les inconvénients concomitants dus aux effets néfastes qui sont associés au mélange racémique de loméfloxacine.
EP9292925403A 1991-11-27 1992-11-25 Procedes et compositions destines a traiter des infections a l'aide de (s)-lomefloxacine optiquement pure. Ceased EP0614364A4 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US799243 1985-11-18
US79924391A 1991-11-27 1991-11-27
PCT/US1992/010142 WO1993010785A1 (fr) 1991-11-27 1992-11-25 Procedes et compositions destines a traiter des infections a l'aide de (s)-lomefloxacine optiquement pure

Publications (2)

Publication Number Publication Date
EP0614364A1 true EP0614364A1 (fr) 1994-09-14
EP0614364A4 EP0614364A4 (fr) 1994-10-19

Family

ID=25175406

Family Applications (1)

Application Number Title Priority Date Filing Date
EP9292925403A Ceased EP0614364A4 (fr) 1991-11-27 1992-11-25 Procedes et compositions destines a traiter des infections a l'aide de (s)-lomefloxacine optiquement pure.

Country Status (5)

Country Link
EP (1) EP0614364A4 (fr)
JP (1) JPH07503457A (fr)
AU (2) AU3147493A (fr)
CA (1) CA2124443A1 (fr)
WO (1) WO1993010785A1 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6075024A (en) 1991-11-27 2000-06-13 Sepracor Inc. Methods for treating infection using optically pure (S)-lomefloxacin

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU553415B2 (en) * 1983-09-19 1986-07-17 Abbott Japan Co., Ltd. 6-fluoro-1-4-dihydro-4-oxo-7-substituted piperazinyl- quinoline-3-carboxylic acids
JPS60190777A (ja) * 1984-03-12 1985-09-28 Hokuriku Seiyaku Co Ltd 光学活性な６，８−ジフルオロ−１，４−ジヒドロ−４−オキソ−７−置換ピペラジニルキノリン−３−カルボン酸誘導体
JPS618538A (ja) * 1984-06-25 1986-01-16 Shimizu Constr Co Ltd 工場等における空調機構
JP2676521B2 (ja) * 1988-03-22 1997-11-17 北陸製薬株式会社 キノロンカルボン酸化合物ｉ型結晶の製造法
JPH02115182A (ja) * 1988-10-21 1990-04-27 Yoshitomi Pharmaceut Ind Ltd 光学活性ピリドンカルボン酸化合物

Also Published As

Publication number Publication date
WO1993010785A1 (fr) 1993-06-10
JPH07503457A (ja) 1995-04-13
EP0614364A4 (fr) 1994-10-19
CA2124443A1 (fr) 1993-06-10
AU3147493A (en) 1993-06-28
AU1515197A (en) 1997-05-22

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