EA199901095A1 - SULPHATE SALT OF HIV PROTEASE INHIBITOR THAT HAS IMPROVED ORAL ABSORBTION AND BIOAVAILABILITY - Google Patents

SULPHATE SALT OF HIV PROTEASE INHIBITOR THAT HAS IMPROVED ORAL ABSORBTION AND BIOAVAILABILITY

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
Russian (ru)
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/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

  • 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

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.This invention relates to a sulphate salt of an HIV protease inhibitor, Compound A, which is applicable in the treatment of AIDS, ARS (SAH) or HIV infection in adults and children. More specifically, this invention provides a sulfate salt of an HIV protease inhibitor, Compound A, having significantly improved solubility in dilute HCl (dihydrate) solution, which results in much greater oral absorption and bioavailability in animal models. Methods for obtaining this sulfate salt of specific inhibitory compounds of HIV protease are also described. The international application was published together with an international search report.

EA199901095A 1997-05-29 1998-05-26 SULPHATE SALT OF HIV PROTEASE INHIBITOR THAT HAS IMPROVED ORAL ABSORBTION AND BIOAVAILABILITY EA199901095A1 (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
EA199901095A1 true EA199901095A1 (en) 2000-08-28

Family

ID=26311845

Family Applications (1)

Application Number Title Priority Date Filing Date
EA199901095A EA199901095A1 (en) 1997-05-29 1998-05-26 SULPHATE SALT OF HIV PROTEASE INHIBITOR THAT HAS IMPROVED ORAL ABSORBTION AND BIOAVAILABILITY

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
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
BR9809498A (en) 2000-06-20
NO995822D0 (en) 1999-11-26
HUP0004621A2 (en) 2002-03-28
AU730245B2 (en) 2001-03-01

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