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BG103923A - Sulphate salt of hiv protease inhibitor with improved peroral absorption and biopresence - Google Patents

Sulphate salt of hiv protease inhibitor with improved peroral absorption and biopresence

Info

Publication number
BG103923A
BG103923A BG103923A BG10392399A BG103923A BG 103923 A BG103923 A BG 103923A BG 103923 A BG103923 A BG 103923A BG 10392399 A BG10392399 A BG 10392399A BG 103923 A BG103923 A BG 103923A
Authority
BG
Bulgaria
Prior art keywords
hiv protease
protease inhibitor
sulphate salt
biopresence
compound
Prior art date
Application number
BG103923A
Other languages
Bulgarian (bg)
Inventor
David Askin
R. Hoerrner
Robert Purick
Paul Reider
Richard Varsolona
Ralph Volante
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
Priority claimed from GBGB9714320.0A external-priority patent/GB9714320D0/en
Application filed by Merck & Co. Inc. filed Critical Merck & Co. Inc.
Publication of BG103923A publication Critical patent/BG103923A/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

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

Abstract

The sulphate salt of HIV protease inhibitor, compound A, has the formula The compound is administered for AIDS, ARC or HIV infections in adults and children. It has better solubility in dilute hydrochloric acid solution (gastric juice) due to which the oral absorption and the biological availability in animal models is considerably increased. The invention also relates to a method for the preparation of specific compounds of HIV protease inhibitors 12 claims
BG103923A 1997-05-29 1999-11-24 Sulphate salt of hiv protease inhibitor with improved peroral absorption and biopresence BG103923A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US4795097P 1997-05-29 1997-05-29
GBGB9714320.0A GB9714320D0 (en) 1997-07-07 1997-07-07 Hiv protease inhibitor
PCT/US1998/010633 WO1998054178A1 (en) 1997-05-29 1998-05-26 Sulfate salt of an hiv protease inhibitor having an improved oral absorption and bioavailability

Publications (1)

Publication Number Publication Date
BG103923A true BG103923A (en) 2000-06-30

Family

ID=26311845

Family Applications (1)

Application Number Title Priority Date Filing Date
BG103923A BG103923A (en) 1997-05-29 1999-11-24 Sulphate salt of hiv protease inhibitor with improved peroral absorption and biopresence

Country Status (22)

Country Link
EP (1) EP0986554A1 (en)
JP (1) JP3267632B2 (en)
KR (1) KR20010013042A (en)
CN (1) CN1257497A (en)
AU (1) AU730245B2 (en)
BG (1) BG103923A (en)
BR (1) BR9809498A (en)
CA (1) CA2291086A1 (en)
EA (1) EA199901095A1 (en)
EE (1) EE9900543A (en)
HR (1) HRP980283A2 (en)
HU (1) HUP0004621A3 (en)
ID (1) ID23858A (en)
IL (1) IL132779A0 (en)
IS (1) IS5240A (en)
NO (1) NO995822L (en)
PE (1) PE75099A1 (en)
PL (1) PL336847A1 (en)
SK (1) SK163299A3 (en)
TR (1) TR199902816T2 (en)
TW (1) TW438799B (en)
WO (1) WO1998054178A1 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60036961T2 (en) * 1999-11-24 2008-08-28 Merck & Co., Inc. GAMMA-HYDROXY-2- (FLUORALKYLAMINOCARBONYL) -1-PIPERAZINE PENTANAMIDE AS AN HIV PROTEASE INHIBITOR
AU2001290743A1 (en) * 2000-09-14 2002-03-26 Ortho-Mcneil Pharmaceutical, Inc. Solid salt forms of n-(2-(4-(2-(1-methylethoxy)phenyl)-1-piperazinyl)ethyl)-2-oxo-1-piperidineacetamide

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR9408305A (en) * 1993-12-15 1997-08-26 Merck & Co Inc Compound pharmaceutical composition processes for the treatment of AIDS and HIV infection for the preparation of HIV infection and for inhibition of HIV protease and combination of compounds

Also Published As

Publication number Publication date
IS5240A (en) 1999-11-09
HRP980283A2 (en) 1999-08-31
PL336847A1 (en) 2000-07-17
EP0986554A1 (en) 2000-03-22
PE75099A1 (en) 1999-08-11
KR20010013042A (en) 2001-02-26
HUP0004621A2 (en) 2002-03-28
CA2291086A1 (en) 1998-12-03
IL132779A0 (en) 2001-03-19
HUP0004621A3 (en) 2002-04-29
CN1257497A (en) 2000-06-21
EA199901095A1 (en) 2000-08-28
JP2000513747A (en) 2000-10-17
BR9809498A (en) 2000-06-20
AU7595998A (en) 1998-12-30
SK163299A3 (en) 2000-07-11
NO995822D0 (en) 1999-11-26
TW438799B (en) 2001-06-07
JP3267632B2 (en) 2002-03-18
NO995822L (en) 2000-01-28
TR199902816T2 (en) 2000-02-21
EE9900543A (en) 2000-06-15
ID23858A (en) 2000-05-25
WO1998054178A1 (en) 1998-12-03
AU730245B2 (en) 2001-03-01

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