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WO1993014752A1 - TRAITEMENT D'UNE INFECTION PAR $i(M. FERMENTANS) - Google Patents

TRAITEMENT D'UNE INFECTION PAR $i(M. FERMENTANS) Download PDF

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Publication number
WO1993014752A1
WO1993014752A1 PCT/GB1993/000125 GB9300125W WO9314752A1 WO 1993014752 A1 WO1993014752 A1 WO 1993014752A1 GB 9300125 W GB9300125 W GB 9300125W WO 9314752 A1 WO9314752 A1 WO 9314752A1
Authority
WO
WIPO (PCT)
Prior art keywords
group
denotes
carbon
optionally substituted
sulphur
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
PCT/GB1993/000125
Other languages
English (en)
Inventor
Peter Charles Thomas Hannan
Peter John O'hanlon
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.)
SmithKline Beecham Ltd
Original Assignee
SmithKline Beecham Ltd
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 SmithKline Beecham Ltd filed Critical SmithKline Beecham Ltd
Priority to JP5513015A priority Critical patent/JPH07503243A/ja
Priority to EP93902424A priority patent/EP0621778A1/fr
Publication of WO1993014752A1 publication Critical patent/WO1993014752A1/fr
Anticipated expiration legal-status Critical
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
    • A61K31/41—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
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • 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
    • A61K31/42—Oxazoles
    • 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
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants

Definitions

  • This present application relates to a method for treating Mycoplasma fermentans-ia ⁇ ce ⁇ infections and to compositions for use in such treatment.
  • Mycoplasma fermentans has in the past been suspected of being a human pathogen, having been occasionally isolated from human urogenital tract, from bone marrow of leukaemic patients, from synovial effusions of rheumatoid patients, as well as from tissue cultures. More recently, AIDS researchers have identified a strain of mycoplasma, since identified as M. fermentans, which it is thought may act as co-factor in the pathogenesis of AIDS (Science, vol 248, 11th May 1990). In addition, these same mycoplasma have been implicated in fulminant infections of non-AIDS patients (Amer. J. Trop. Med., Hyg, 42(5), 1990, 399). The provision of a chemotherapeutic agent with activity against M. fermentans would therefore be of assistance in the treatment of such patients.
  • the present invention provides a method of treating humans infected with M. fermentans, in particular humans also infected with HIV, which method comprises treating humans in need of such therapy with an anti-mycoplasmal effective amount of a compound of formula (I):
  • a group R which is a 5-membered heterocyclic group having a 6 ⁇ -electron system with up to four heteroatoms which may be selected from oxygen, sulphur and nitrogen, and optionally substituted with two substituents R ⁇ and ⁇ which may be the same or different and is each selected from (C ⁇ _2 ⁇ )alkyl, (C2-8)alkenyl, (C3 tine7)cycloalkyl, aryl(C ⁇ _ g)alkyl, aryl or heterocyclyl, each of which may be optionally substituted; or
  • the invention provides for the use of a compound of formula (I) as hereinbefore defined in the manufacture of a medicament for treating M. fermentans - induced infection.
  • 'aryl' includes for example phenyl and naphthyl optionally substituted with up to five, preferably up to three, groups selected from halogen, optionally substituted (C ⁇ _g)alkyl, phenyl,
  • heterocyclyl' includes for example single or fused rings comprising up to four hetero-atoms in each ring selected from oxygen, nitrogen and sulphur and optionally substituted with up to three groups.
  • the heterocyclic ring comprises from 4 to 7 ring atoms, preferably 5 or 6 atoms.
  • Suitable substituents for 'heterocyclyl' and for heterocyclyl groups specifically named herein are selected from halogen, optionally substituted (C ⁇ _g)alkyl, (C i-.g)alkoxy, halo(C;i-.g)alkyl, hydroxy, amino, mono- or di(C-]_.g)alkylam_no, carboxy, (C ⁇ .g)alkoxycarbonyl, (C _ g)alkoxycarbonyl(C ⁇ _g)alkyl, aryl or oxo.
  • 'halogen' refers to fluorine, chlorine, bromine or iodine.
  • Suitable substituents for alkyl, alkenyl or cycloalkyl include for example halogen, hydroxy, (C ⁇ _g)alkoxy, carboxy and salts thereof, (C- ⁇ . g)alkoxycarbonyl, carbamoyl, mono- or di(C-i L .g)alkylcarbamoyl, sulphamoyl, mono- and di-(C-L_g)alkylsulphamoyl, amino, mono- and di-
  • R* denotes a group:
  • the group R ⁇ denotes a group of the formula:
  • R ⁇ denotes an optionally substituted isoxazol-5-yl, a fur-2-yl, a fur-3-yl or a pyridyl group bonded by a carbon atom thereof to the oxazolyl moiety.
  • Preferred substituents for the isoxazol-5-yl group include (C-j.. g)alkyl, and for the fur-2-yl group include cyano.
  • Example of such compounds are disclosed in EP 0 399 645 and WO 91/09856 (both to Beecham Group pic).
  • Compounds of formula (I) in which R° denotes the group -CO ⁇ are described in WO 91/09855 (Beecham Group pic).
  • compositions which comprises a compound of formula (I) (hereinafter referred to as the 'drug') together with a pharmaceutically acceptable carrier or excipient.
  • the compositions may be formulated for administration by any route, and would depend on the disease being treated.
  • the compositions may be in the form of tablets, capsules, powders, granules, lozenges, liquid or gel preparations, such as oral, topical or sterile parenteral suspensions.
  • Tablets and capsules for oral administration may be in unit dose presentation form, and may contain conventional excipients such as binding agents, for example syrup, acacia, gelatin, sorbitol, tragacanth, or polyvinyl-pyrollidone; fillers, for example lactose, sugar, maize-starch, calcium phosphate, sorbitol or glycine; tabletting lubricants, for example magnesium stearate, talc, polyethylene glycol or silica; disintegrants, for example potato starch, or acceptable wetting agents such as sodium lauryl sulphate.
  • the tablets may be coated according to methods well known in normal pharmaceutical practice.
  • Oral liquid preparations may be in the form of, for example, aqueous or oily suspensions, solutions, emulsions, syrups or elixirs, or may be presented as a dry product for reconstitution with water or other suitable vehicle before use.
  • Such liquid preparations may contain conventional additives such as suspending agents, for example sorbitol, syrup, methyl cellulose, glucose syrup, gelatin, hydrogenated edible fats; emulsifying agents, for example lecithin, sorbitan monooleate, or acacia; non-aqueous vehicles (which may include edible oils), for example almond oil, fractionated coconut oil, oily esters such as glycerine, propylene glycol, or ethyl alcohol; preservatives, for example methyl or propyl p-hydroxybenzoate or sorbic acid, and if desired conventional flavouring or colouring agents.
  • suspending agents for example sorbitol, syrup, methyl cellulose, glucose syrup, gelatin, hydrogenated edible fats
  • emulsifying agents for example lecithin, sorbitan monooleate, or acacia
  • non-aqueous vehicles which may include edible oils
  • almond oil fractionated coconut oil
  • oily esters such as glycerine, prop
  • Cream or ointment formulations that may be used for the drug are conventional formulations well known in the art, for example, as described in standard text books of pharmaceutics and cosmetics, such as Harry's Cosmeticology published by Leonard Hill Books, and the British Pharmacopoeia.
  • Suppositories will contain conventional suppository bases, e.g. cocoa-butters or other glyceride.
  • fluid unit dosage forms are prepared utilizing the drug and a sterile vehicle. The drug, depending on the vehicle and concentration used, can be suspended in the vehicle.
  • adjuvants such as a local anaesthetic, preservative and buffering agents can be dissolved in the vehicle.
  • the composition can be frozen after filling into the vial and water removed under vacuum. The dry lypophilized powder is then sealed in the vial.
  • the drug can be sterilised by exposure to ethylene oxide before suspending in the sterile vehicle.
  • a surfactant or wetting agent is included in the composition to facilitate uniform distribution of the drug.
  • the drug may be made up into a suspension in a suitable liquid carrier, such as water, glycerol, diluted ethanol, propylene glycol, polyethylene glycol or fixed oils.
  • a suitable liquid carrier such as water, glycerol, diluted ethanol, propylene glycol, polyethylene glycol or fixed oils.
  • the drug is formulated as a suspension in a suitable, sterile aqueous or non-aqueous vehicle.
  • Additives for instance buffers such as sodium metabisulphite or disodium edetate; preservatives including bactericidal and fungicidal agents, such as phenylmercuric acetate or nitrate, benzalkonium chloride or chlorhexidine, and thickening agents such as hypromellose may also be included.
  • compositions administered topically will, of course, depend on the size of the area being treated. For the ears and eyes each dose will typically be in the range from 10 to 100 mg of the drug.
  • compositions may contain from 0.1% to 99% by weight, preferably from 10-60% by weight, of the drug.depending on the method of administration. Where the compositions are in unit dose form, each dosage unit will preferably contain from 50-500 mg, of the drug.
  • the dosage as employed for adult human treatment will preferably range from 100 mg to 3 g, per day, for instance 250 mg to 2 g of the drug per day, depending on the route and frequency of administration.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Certains dérivés de normonyle peuvent être utilisés pour traiter des infections induites par M. fermentans.
PCT/GB1993/000125 1992-01-22 1993-01-20 TRAITEMENT D'UNE INFECTION PAR $i(M. FERMENTANS) Ceased WO1993014752A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP5513015A JPH07503243A (ja) 1992-01-22 1993-01-20 エム・ファーメンタンス感染症の治療
EP93902424A EP0621778A1 (fr) 1992-01-22 1993-01-20 TRAITEMENT D'UNE INFECTION PAR $i(M. FERMENTANS)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB9201391.1 1992-01-22
GB929201391A GB9201391D0 (en) 1992-01-22 1992-01-22 Method of treatment

Publications (1)

Publication Number Publication Date
WO1993014752A1 true WO1993014752A1 (fr) 1993-08-05

Family

ID=10709071

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB1993/000125 Ceased WO1993014752A1 (fr) 1992-01-22 1993-01-20 TRAITEMENT D'UNE INFECTION PAR $i(M. FERMENTANS)

Country Status (5)

Country Link
EP (1) EP0621778A1 (fr)
JP (1) JPH07503243A (fr)
AU (1) AU3361293A (fr)
GB (1) GB9201391D0 (fr)
WO (1) WO1993014752A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7649098B2 (en) 2006-02-24 2010-01-19 Lexicon Pharmaceuticals, Inc. Imidazole-based compounds, compositions comprising them and methods of their use
US7825150B2 (en) 2007-09-06 2010-11-02 Lexicon Pharmaceuticals, Inc. Compositions and methods for treating immunological and inflammatory diseases and disorders

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0087953A2 (fr) * 1982-02-27 1983-09-07 Beecham Group Plc Composés 1-normon-2-yl-hétérocycliques antibactériens
WO1992002518A1 (fr) * 1990-08-01 1992-02-20 Beecham Group Plc Derives de mupirocine

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0087953A2 (fr) * 1982-02-27 1983-09-07 Beecham Group Plc Composés 1-normon-2-yl-hétérocycliques antibactériens
WO1992002518A1 (fr) * 1990-08-01 1992-02-20 Beecham Group Plc Derives de mupirocine

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ARCH. PATH. LAB. MED. vol. 115, May 1991, pages 464 - 466 HAYES M.M. ET AL. 'In vitro antimicrobial susceptibilty testing for the newly identified AIDS- associated Mycoplasma' *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7649098B2 (en) 2006-02-24 2010-01-19 Lexicon Pharmaceuticals, Inc. Imidazole-based compounds, compositions comprising them and methods of their use
US8093267B2 (en) 2006-02-24 2012-01-10 Lexicon Pharmaceuticals, Inc. Methods of treating rheumatoid arthritis
US7825150B2 (en) 2007-09-06 2010-11-02 Lexicon Pharmaceuticals, Inc. Compositions and methods for treating immunological and inflammatory diseases and disorders

Also Published As

Publication number Publication date
GB9201391D0 (en) 1992-03-11
AU3361293A (en) 1993-09-01
JPH07503243A (ja) 1995-04-06
EP0621778A1 (fr) 1994-11-02

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