EP1019056A1 - Combinaisons antivirales contenant le nucleoside carbocyclique 1592u89 - Google Patents

Combinaisons antivirales contenant le nucleoside carbocyclique 1592u89

Info

Publication number
EP1019056A1
EP1019056A1 EP98928261A EP98928261A EP1019056A1 EP 1019056 A1 EP1019056 A1 EP 1019056A1 EP 98928261 A EP98928261 A EP 98928261A EP 98928261 A EP98928261 A EP 98928261A EP 1019056 A1 EP1019056 A1 EP 1019056A1
Authority
EP
European Patent Office
Prior art keywords
combination
amino
purin
cyclopropylamino
cyclopentene
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
EP98928261A
Other languages
German (de)
English (en)
Inventor
Martha Heider St. Clair
David Walter-Triangle Pharmaceuticals BARRY
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.)
Glaxo Group Ltd
Original Assignee
Glaxo Group 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
Priority claimed from GBGB9709945.1A external-priority patent/GB9709945D0/en
Priority claimed from GBGB9719866.7A external-priority patent/GB9719866D0/en
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of EP1019056A1 publication Critical patent/EP1019056A1/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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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

  • the present invention relates to therapeutic combinations of (-)-(l S, 4R) -4-[2-amino-6- (cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol (1592U89) and HIV protease inhibitors, which have anti-HIV activity.
  • the present invention is also concerned with pharmaceutical compositions containing said combinations and their use in the treatment of HIV infections including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors.
  • a further feature of the present invention is a combination comprising 1592U89, at least one HIV protease inhibitor, and a second reverse transcriptase inhibitor, such as lamivudine.
  • the ratios of the components of such combinations will conveniently be the same as the ratios of the relevant compounds in the double combinations of the invention.
  • physiologically functional derivative includes any physiologically acceptable solvate, salt, ether, ester, salt of such ester, or solvates of any such salt, ether, or ester, of 1592U89 or HIV protease inhibitor(s); or any other compound which upon administration to the recipient, is capable of providing (directly or indirectly) such a compound or an antivirally active metabolite or residue thereof.
  • the desired dose may preferably be presented as one, two, three, four, five, six or more sub-doses administered at appropriate intervals throughout the day.
  • a typical unitary dosage may contain 50 mg to 3 g each of 1592U89 and one or more HIV protease inhibitors, advantageously 100 mg to 2 g each of 1592U89 and one or more HIV protease inhibitors.
  • compositions are often prescribed to the patient in "patient packs" containing the whole course of treatment in a single package, usually a blister pack.
  • the invention provides a patient pack comprising in association for separate administration 1592U89 or a physiologically functional derivative thereof together with at least one HIV protease inhibitor or a physiologically functional derivative thereof.
  • Formulations suitable for vaginal administration may be presented as pessaries, tampons, creams, gels, pastes, foams or spray formulations containing in addition to the active ingredient such carriers as are known in the art to be appropriate.
  • HIV RNA PCR (log-ocopies/ml) 4.54 (9) 2.60 (9) 2.60 (8) 2.60 (8) 2.60 (8)
  • Drug release takes place over a period of about 6-8 hours and is complete after 12 hours.
  • a capsule formulation is prepared by admixing the ingredients of formulation D in Example 2 above and filling into a two-part hard gelatin capsule.
  • Formulation B (infra) is prepared in a similar manner.
  • Active Ingredient 200 Hydro chloric Acid Solution 0.1 M or

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

L'invention concerne des combinaisons thérapeutiques de (-)-(1S, 4R)-4-[2-amino-6- (cyclopropylamino)-9H-purin-9-yl] -2-cyclopentène-1-méthanol (1592U89) et des inhibiteurs de la protéase du VIH présentant une activité anti-VIH. L'invention concerne également des compositions pharmaceutiques contenant lesdites combinaisons et leur utilisation dans le traitement des infections par le VIH.
EP98928261A 1997-05-17 1998-05-14 Combinaisons antivirales contenant le nucleoside carbocyclique 1592u89 Ceased EP1019056A1 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GBGB9709945.1A GB9709945D0 (en) 1997-05-17 1997-05-17 A novel salt
GB9709945 1997-05-17
GBGB9719866.7A GB9719866D0 (en) 1997-09-19 1997-09-19 Antiviral Combinations
GB9719866 1997-09-19
PCT/EP1998/002837 WO1998052571A1 (fr) 1997-05-17 1998-05-14 Combinaisons antivirales contenant le nucleoside carbocyclique 1592u89

Publications (1)

Publication Number Publication Date
EP1019056A1 true EP1019056A1 (fr) 2000-07-19

Family

ID=26311542

Family Applications (1)

Application Number Title Priority Date Filing Date
EP98928261A Ceased EP1019056A1 (fr) 1997-05-17 1998-05-14 Combinaisons antivirales contenant le nucleoside carbocyclique 1592u89

Country Status (8)

Country Link
EP (1) EP1019056A1 (fr)
JP (1) JP2001525840A (fr)
AU (1) AU8017298A (fr)
BR (1) BR9809124A (fr)
CA (1) CA2289654A1 (fr)
NO (1) NO995621L (fr)
NZ (1) NZ500868A (fr)
WO (1) WO1998052571A1 (fr)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2779653B1 (fr) * 1998-06-11 2002-12-20 Inst Nat Sante Rech Med Utilisation de composes modulateurs du proteasome en therapie
CA2462875A1 (fr) * 2001-10-05 2003-04-17 Elan Pharmaceuticals, Inc. Allylamides utilises dans le traitement de la maladie d'alzheimer

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
GB9417249D0 (en) * 1994-08-26 1994-10-19 Wellcome Found A novel salt
US5691372A (en) * 1995-04-19 1997-11-25 Vertex Pharmaceuticals Incorporated Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease
US5646180A (en) * 1995-12-05 1997-07-08 Vertex Pharmaceuticals Incorporated Treatment of the CNS effects of HIV
HUP9901024A2 (hu) * 1996-01-26 1999-09-28 Vertex Pharmaceuticals Incorporated Telített azolok oxoszármazékai, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
IL127350A0 (en) * 1996-06-25 1999-10-28 Glaxo Group Ltd Combinations comprising VX478 zidovudine and/or 1592U89 for use in the treatment of HIV

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO9852571A1 *

Also Published As

Publication number Publication date
BR9809124A (pt) 2000-08-01
NZ500868A (en) 2001-08-31
WO1998052571A1 (fr) 1998-11-26
NO995621L (no) 2000-01-14
NO995621D0 (no) 1999-11-16
AU8017298A (en) 1998-12-11
CA2289654A1 (fr) 1998-11-26
JP2001525840A (ja) 2001-12-11

Similar Documents

Publication Publication Date Title
US6417191B1 (en) Synergistic combinations of zidovudine, 1592U89 and 3TC
EP0938321B1 (fr) Combinaisons comprenant du vx478, de la zidovudine et du 3tc pouvant etre utilisees dans le traitement du vih
AU723877C (en) Combinations comprising VX478, zidovudine and/or 1592U89 for use in the treatment of HIV
WO1998052570A1 (fr) Combinaisons antivirales contenant le nucleoside carbocyclique 1592u89
US6432966B2 (en) Antiviral combinations
EP1019056A1 (fr) Combinaisons antivirales contenant le nucleoside carbocyclique 1592u89
EP1113803A1 (fr) Combinaisons antivirales contenant de la lamivudine et de l'abacavir
WO2000018384A2 (fr) Combinaisons antivirales renfermant un ester isopropylique d'acide (s)-2-ethyl-7-fluoro-3-oxo-3,4-dihydro-2h-quinoxaline-1-carboxylique
MXPA98010386A (en) Combinations that include vx478, zidovudina and / or 1592u89 for use in the treatment of
WO2000016754A2 (fr) Combinaisons antivirales
WO2000018383A2 (fr) Combinaisons antivirales renfermant un ester isopropylique d'acide (s)-2-ethyl-7-fluoro-3-oxo-3,4-dihydro-2h-quinoxaline-1-carboxylique

Legal Events

Date Code Title Description
PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

Free format text: ORIGINAL CODE: 0009012

17P Request for examination filed

Effective date: 19991115

AK Designated contracting states

Kind code of ref document: A1

Designated state(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

AX Request for extension of the european patent

Free format text: AL PAYMENT 19991115;LT PAYMENT 19991115;LV PAYMENT 19991115;MK PAYMENT 19991115;RO PAYMENT 19991115;SI PAYMENT 19991115

17Q First examination report despatched

Effective date: 20010206

GRAG Despatch of communication of intention to grant

Free format text: ORIGINAL CODE: EPIDOS AGRA

RIC1 Information provided on ipc code assigned before grant

Free format text: 7A 61K 31/52 A, 7A 61P 31/18 B

RTI1 Title (correction)

Free format text: ANTIVIRAL COMBINATIONS CONTAINING ABACAVIR (1592U89)

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: THE APPLICATION HAS BEEN REFUSED

18R Application refused

Effective date: 20030526