EA199901095A1 - Сульфатная соль ингибитора вич протеазы, имеющая улучшенную пероральную абсорбцию и биодоступность - Google Patents

Сульфатная соль ингибитора вич протеазы, имеющая улучшенную пероральную абсорбцию и биодоступность

Info

Publication number
EA199901095A1
EA199901095A1 EA199901095A EA199901095A EA199901095A1 EA 199901095 A1 EA199901095 A1 EA 199901095A1 EA 199901095 A EA199901095 A EA 199901095A EA 199901095 A EA199901095 A EA 199901095A EA 199901095 A1 EA199901095 A1 EA 199901095A1
Authority
EA
Eurasian Patent Office
Prior art keywords
hiv protease
protease inhibitor
bioavailability
sulphate salt
improved oral
Prior art date
Application number
EA199901095A
Other languages
English (en)
Inventor
Дэвид Аскин
Р. Скотт Хернер
Роберт М. Пьюрик
Пол Рейдер
Ричард Дж. Варсолона
Ральф П. Воланте
Original Assignee
Мерк Энд Ко., Инк.
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 Мерк Энд Ко., Инк. filed Critical Мерк Энд Ко., Инк.
Publication of EA199901095A1 publication Critical patent/EA199901095A1/ru

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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (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)

Abstract

Данное изобретение относится к сульфатной соли ингибитора ВИЧ протеазы, соединения A, которая применима в лечении СПИДа, ARS (САК) или инфекции ВИЧ у взрослых и детей. Более конкретно, данное изобретение обеспечивает сульфатную соль ингибитора ВИЧ протеазы, соединения A, имеющую значительно улучшенную растворимость в разбавленном растворе HCl (дигидрате), что приводит к гораздо большей пероральной абсорбции и биодоступности в моделях животных. Описаны также способы получения этой сульфатной соли конкретных ингибиторных соединений ВИЧ протеазы.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA199901095A 1997-05-29 1998-05-26 Сульфатная соль ингибитора вич протеазы, имеющая улучшенную пероральную абсорбцию и биодоступность EA199901095A1 (ru)

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
EA199901095A1 true EA199901095A1 (ru) 2000-08-28

Family

ID=26311845

Family Applications (1)

Application Number Title Priority Date Filing Date
EA199901095A EA199901095A1 (ru) 1997-05-29 1998-05-26 Сульфатная соль ингибитора вич протеазы, имеющая улучшенную пероральную абсорбцию и биодоступность

Country Status (22)

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

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001038332A1 (en) * 1999-11-24 2001-05-31 Merck & Co., Inc. Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides as hiv protease inhibitors
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
CZ288312B6 (en) * 1993-12-15 2001-05-16 Merck & Co Inc HIV-protease inhibitors and pharmaceutical preparations in which they are comprised

Also Published As

Publication number Publication date
KR20010013042A (ko) 2001-02-26
AU730245B2 (en) 2001-03-01
IL132779A0 (en) 2001-03-19
TR199902816T2 (xx) 2000-02-21
BR9809498A (pt) 2000-06-20
EE9900543A (et) 2000-06-15
ID23858A (id) 2000-05-25
HUP0004621A3 (en) 2002-04-29
NO995822D0 (no) 1999-11-26
JP3267632B2 (ja) 2002-03-18
PL336847A1 (en) 2000-07-17
BG103923A (en) 2000-06-30
JP2000513747A (ja) 2000-10-17
HRP980283A2 (en) 1999-08-31
NO995822L (no) 2000-01-28
PE75099A1 (es) 1999-08-11
WO1998054178A1 (en) 1998-12-03
CA2291086A1 (en) 1998-12-03
HUP0004621A2 (hu) 2002-03-28
AU7595998A (en) 1998-12-30
TW438799B (en) 2001-06-07
IS5240A (is) 1999-11-09
CN1257497A (zh) 2000-06-21
EP0986554A1 (en) 2000-03-22
SK163299A3 (en) 2000-07-11

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