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WO1996000068A3 - Combination therapy for hiv infection - Google Patents

Combination therapy for hiv infection Download PDF

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Publication number
WO1996000068A3
WO1996000068A3 PCT/US1995/007690 US9507690W WO9600068A3 WO 1996000068 A3 WO1996000068 A3 WO 1996000068A3 US 9507690 W US9507690 W US 9507690W WO 9600068 A3 WO9600068 A3 WO 9600068A3
Authority
WO
WIPO (PCT)
Prior art keywords
hiv
combination therapy
hiv infection
combination
infection
Prior art date
Application number
PCT/US1995/007690
Other languages
French (fr)
Other versions
WO1996000068A2 (en
Inventor
Emilio A Emini
Joel R Huff
Original Assignee
Merck & Co 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 Merck & Co Inc filed Critical Merck & Co Inc
Priority to SK1639-96A priority Critical patent/SK163996A3/en
Priority to EP95923935A priority patent/EP0767664A2/en
Priority to CZ963751A priority patent/CZ375196A3/en
Priority to MX9700036A priority patent/MX9700036A/en
Priority to JP8503245A priority patent/JPH10503178A/en
Priority to AU28638/95A priority patent/AU2863895A/en
Priority to KR1019960707469A priority patent/KR970703770A/en
Priority to FI965196A priority patent/FI965196A7/en
Publication of WO1996000068A2 publication Critical patent/WO1996000068A2/en
Publication of WO1996000068A3 publication Critical patent/WO1996000068A3/en
Priority to NO965591A priority patent/NO965591D0/en

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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • A61K31/708—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

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

Abstract

The combination of the HIV protease inhibitor Compound J and one or more of nevarapine or an α-APA derivative is useful in theinhibition of HIV protease, the inhibition of HIV reverse transcriptase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
PCT/US1995/007690 1994-06-27 1995-06-23 Combination therapy for hiv infection WO1996000068A2 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
SK1639-96A SK163996A3 (en) 1994-06-27 1995-06-23 Combinated medicament and pharmaceutical composition containing its, used to therapy of hiv infection
EP95923935A EP0767664A2 (en) 1994-06-27 1995-06-23 Combination therapy for hiv infection
CZ963751A CZ375196A3 (en) 1994-06-27 1995-06-23 Combination of active compounds against hiv and pharmaceutical composition containing thereof
MX9700036A MX9700036A (en) 1994-06-27 1995-06-23 Combination therapy for hiv infection.
JP8503245A JPH10503178A (en) 1994-06-27 1995-06-23 Combination therapy for HIV infection
AU28638/95A AU2863895A (en) 1994-06-27 1995-06-23 Combination therapy for hiv infection
KR1019960707469A KR970703770A (en) 1994-06-27 1995-06-23 Combination therapy for HIV infection
FI965196A FI965196A7 (en) 1994-06-27 1995-06-23 Combination therapy for HIV infection
NO965591A NO965591D0 (en) 1994-06-27 1996-12-27 Combination treatment of HIV infection

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US26708594A 1994-06-27 1994-06-27
US267,085 1994-06-27

Publications (2)

Publication Number Publication Date
WO1996000068A2 WO1996000068A2 (en) 1996-01-04
WO1996000068A3 true WO1996000068A3 (en) 1996-02-22

Family

ID=23017251

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1995/007690 WO1996000068A2 (en) 1994-06-27 1995-06-23 Combination therapy for hiv infection

Country Status (14)

Country Link
EP (1) EP0767664A2 (en)
JP (1) JPH10503178A (en)
AU (1) AU2863895A (en)
CA (1) CA2193221A1 (en)
CZ (1) CZ375196A3 (en)
FI (1) FI965196A7 (en)
HU (1) HUT76546A (en)
IL (1) IL114208A0 (en)
MX (1) MX9700036A (en)
NO (1) NO965591D0 (en)
PL (1) PL317876A1 (en)
SK (1) SK163996A3 (en)
WO (1) WO1996000068A2 (en)
ZA (1) ZA955269B (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6689761B1 (en) 1995-02-01 2004-02-10 Merck & Co., Inc. Combination therapy for HIV infection
US6045829A (en) * 1997-02-13 2000-04-04 Elan Pharma International Limited Nanocrystalline formulations of human immunodeficiency virus (HIV) protease inhibitors using cellulosic surface stabilizers
EP0872233A1 (en) * 1997-04-14 1998-10-21 Janssen Pharmaceutica N.V. Antiretroviral compositions with improved bioavailability
GB2324242A (en) * 1997-04-18 1998-10-21 Atindra Nath Chakrabarty Medicaments for treating viral infections
AU775360B2 (en) 1999-09-24 2004-07-29 Janssen Pharmaceutica N.V. Antiviral compositions
CN108291861B (en) 2015-09-23 2021-10-12 马尔文帕纳科 Particle characterization

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
JAMES E. F. REYNOLDS: "Martindale; The Extra Pharmacopoeia, Thirtieth edition", THE PHARMACEUTICAL PRESS, LONDON *
KARL D. HARGRAVE, JOHN R. PROUDFOOT ET AL: "NOVEL NON-NUCLEOSIDE INHIBITORS OF HIV-1 REVERSE TRANSCRIPTASE. 1. TRICYCLIC PYRIDOBENZO- AND DIPYRIDODIAZEPINONES", J. MED. CHEM., vol. 34, USA, pages 2231 - 2241 *
RUDI PAUWELS, KOEN ANDRIES ET AL: "POTENT AND HIGHLY SELECTIVE HUMAN IMMUNODEFICIENCY VIRUS TYPE 1 (HIV-1) INHIBITION BY A SERIES OF ALFA-ANILINOPHENYLACETAMIDE DERIVATIVES TARGETED AT HIV-1 REVERSE TRANSCRIPTASE", PROC. NATL. SCI., vol. 90, no. 5, 1 March 1993 (1993-03-01), USA, pages P1711 - P1715 *
VACCA, DORSEY ET AL: "L-735,524: An orally bioavailable human immunodeficieny virus type 1 protease inhibitor", PROC. NATL. ACAD. SCI., vol. 91, no. 9, USA, pages 4096 - 4100 *

Also Published As

Publication number Publication date
WO1996000068A2 (en) 1996-01-04
NO965591L (en) 1996-12-27
HUT76546A (en) 1997-09-29
CA2193221A1 (en) 1996-01-04
FI965196L (en) 1996-12-23
HU9603567D0 (en) 1997-02-28
FI965196A0 (en) 1996-12-23
FI965196A7 (en) 1996-12-23
JPH10503178A (en) 1998-03-24
SK163996A3 (en) 1997-08-06
EP0767664A2 (en) 1997-04-16
AU2863895A (en) 1996-01-19
MX9700036A (en) 1997-04-30
NO965591D0 (en) 1996-12-27
PL317876A1 (en) 1997-04-28
ZA955269B (en) 1996-02-02
IL114208A0 (en) 1995-10-31
CZ375196A3 (en) 1997-07-16

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