BR9809498A - Compound, process for its production, pharmaceutical composition, process for its production, and processes for treating HIV infection, for treating AIDS, for inhibiting a hiv protease, and for producing an ethanolate solvate. - Google Patents

Compound, process for its production, pharmaceutical composition, process for its production, and processes for treating HIV infection, for treating AIDS, for inhibiting a hiv protease, and for producing an ethanolate solvate.

Info

Publication number
BR9809498A
BR9809498A BR9809498-0A BR9809498A BR9809498A BR 9809498 A BR9809498 A BR 9809498A BR 9809498 A BR9809498 A BR 9809498A BR 9809498 A BR9809498 A BR 9809498A
Authority
BR
Brazil
Prior art keywords
production
treating
compound
processes
hiv protease
Prior art date
Application number
BR9809498-0A
Other languages
Portuguese (pt)
Inventor
David Askin
R Scott Hoerrner
Robert M Purick
Paul Reider
Richard J Varsolona
Ralph P 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 BR9809498A publication Critical patent/BR9809498A/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

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

Abstract

"COMPOSTO CRISTALINO, PROCESSO PARA SUA PRODUçãO, COMPOSIçãO FARMACêUTICA, PROCESSO PARA SUA PRODUçãO, E, PROCESSOS PARA TRATAMENTO DE INFECçãO PELO HIV, PARA TRATAMENTO DA AIDS E PARA INIBIçãO DE UMA HIV PROTEASE". Esta invenção diz respeito a um sal de sulfato de um inibidor da HIV protease, Composto (A) que é útil no tratamento da infecção de AIDS, ARC ou HIV em adultos e crianças. Mais especificamente, a invenção fornece um sal de sulfato do inibidor da HIV protease, Composto (A), tendo solubilidade substancialmente melhorada em solução diluída de HC1 (ácido gástrico), que resulta em absorção oral e biodisponibilidade muito maiores em modelos de animais. Processos para produzir o sal de sulfato dos compostos específicos inibidores de HIV protease, também são apresentados."CRYSTALLINE COMPOUND, PROCESS FOR ITS PRODUCTION, PHARMACEUTICAL COMPOSITION, PROCESS FOR ITS PRODUCTION, AND, PROCESSES FOR TREATING HIV INFECTION, FOR TREATING AIDS AND FOR INHIBITING HIV PROTEASE". This invention relates to a sulfate salt of an HIV protease inhibitor, Compound (A) which is useful in the treatment of AIDS, ARC or HIV infection in adults and children. More specifically, the invention provides a sulfate salt of the HIV protease inhibitor, Compound (A), having substantially improved solubility in diluted HCl (gastric acid) solution, which results in much greater oral absorption and bioavailability in animal models. Processes for producing the sulfate salt of specific HIV protease inhibitor compounds are also presented.

BR9809498-0A 1997-05-29 1998-05-26 Compound, process for its production, pharmaceutical composition, process for its production, and processes for treating HIV infection, for treating AIDS, for inhibiting a hiv protease, and for producing an ethanolate solvate. BR9809498A (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
BR9809498A true BR9809498A (en) 2000-06-20

Family

ID=26311845

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9809498-0A BR9809498A (en) 1997-05-29 1998-05-26 Compound, process for its production, pharmaceutical composition, process for its production, and processes for treating HIV infection, for treating AIDS, for inhibiting a hiv protease, and for producing an ethanolate solvate.

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
JP2003514910A (en) 1999-11-24 2003-04-22 メルク エンド カムパニー インコーポレーテッド Gamma-hydroxy-2- (fluoroalkylaminocarbonyl) -1-piperazinepentanamides as HIV protease inhibitors
US20020082421A1 (en) * 2000-09-14 2002-06-27 Abdel-Magid Ahmed F. Novel solid salt forms of N-[2-[4-[2-(1- methylethoxy)phenyl]-1-piperazinyl]-2-oxo-1piperidineacetamide

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0734387B1 (en) * 1993-12-15 2002-04-10 Merck & Co. Inc. Hiv protease inhibitors

Also Published As

Publication number Publication date
EP0986554A1 (en) 2000-03-22
KR20010013042A (en) 2001-02-26
HRP980283A2 (en) 1999-08-31
BG103923A (en) 2000-06-30
IS5240A (en) 1999-11-09
HUP0004621A3 (en) 2002-04-29
EA199901095A1 (en) 2000-08-28
EE9900543A (en) 2000-06-15
AU7595998A (en) 1998-12-30
WO1998054178A1 (en) 1998-12-03
CN1257497A (en) 2000-06-21
IL132779A0 (en) 2001-03-19
JP3267632B2 (en) 2002-03-18
NO995822L (en) 2000-01-28
TR199902816T2 (en) 2000-02-21
JP2000513747A (en) 2000-10-17
TW438799B (en) 2001-06-07
CA2291086A1 (en) 1998-12-03
ID23858A (en) 2000-05-25
SK163299A3 (en) 2000-07-11
PL336847A1 (en) 2000-07-17
PE75099A1 (en) 1999-08-11
NO995822D0 (en) 1999-11-26
HUP0004621A2 (en) 2002-03-28
AU730245B2 (en) 2001-03-01

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Legal Events

Date Code Title Description
FA10 Dismissal: dismissal - article 33 of industrial property law
B11Y Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette]