WO1998040357A3 - Hiv protease inhibitors - Google Patents

Hiv protease inhibitors Download PDF

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Publication number
WO1998040357A3
WO1998040357A3 PCT/US1998/004735 US9804735W WO9840357A3 WO 1998040357 A3 WO1998040357 A3 WO 1998040357A3 US 9804735 W US9804735 W US 9804735W WO 9840357 A3 WO9840357 A3 WO 9840357A3
Authority
WO
WIPO (PCT)
Prior art keywords
hiv protease
protease inhibitors
hiv
compounds
hiv virus
Prior art date
Application number
PCT/US1998/004735
Other languages
French (fr)
Other versions
WO1998040357A2 (en
Inventor
Kim F Albizati
Siegfried Reich
Michael D Varney
Kanyin E Zhang
Takuo Kobayashi
Original Assignee
Agouron Pharma
Japan Tobacco Inc
Kim F Albizati
Siegfried Reich
Michael D Varney
Kanyin E Zhang
Takuo Kobayashi
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 to EEP199900416A priority Critical patent/EE04114B1/en
Priority to EA199900823A priority patent/EA002378B1/en
Priority to KR10-1999-7008331A priority patent/KR100511089B1/en
Priority to BR9808867-0A priority patent/BR9808867A/en
Priority to AU64575/98A priority patent/AU743078B2/en
Priority to HU0001380A priority patent/HUP0001380A3/en
Priority to EP98910300A priority patent/EP0970055A2/en
Priority to MXPA99008395A priority patent/MXPA99008395A/en
Priority to APAP/P/1999/001648A priority patent/AP1358A/en
Priority to IL13187098A priority patent/IL131870A0/en
Application filed by Agouron Pharma, Japan Tobacco Inc, Kim F Albizati, Siegfried Reich, Michael D Varney, Kanyin E Zhang, Takuo Kobayashi filed Critical Agouron Pharma
Priority to NZ337706A priority patent/NZ337706A/en
Priority to CA002284163A priority patent/CA2284163A1/en
Priority to SK1222-99A priority patent/SK283636B6/en
Priority to JP53974598A priority patent/JP2001516350A/en
Publication of WO1998040357A2 publication Critical patent/WO1998040357A2/en
Publication of WO1998040357A3 publication Critical patent/WO1998040357A3/en
Priority to UA99095049A priority patent/UA57772C2/en
Priority to IL131870A priority patent/IL131870A/en
Priority to NO19994415A priority patent/NO315555B1/en
Priority to IS5176A priority patent/IS5176A/en
Priority to BG103727A priority patent/BG63540B1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/14—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/22—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D309/14—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/36—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
    • C07D335/02—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (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)
  • Pyrrole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
PCT/US1998/004735 1997-03-13 1998-03-12 Hiv protease inhibitors WO1998040357A2 (en)

Priority Applications (19)

Application Number Priority Date Filing Date Title
NZ337706A NZ337706A (en) 1997-03-13 1998-03-12 A process for making a HIV protease inhibitor, pharmaceutical composition and salt thereof used in the treatment of the AIDS
EA199900823A EA002378B1 (en) 1997-03-13 1998-03-12 Hiv protease inhibitors
BR9808867-0A BR9808867A (en) 1997-03-13 1998-03-12 Hiv protease inhibitors
AU64575/98A AU743078B2 (en) 1997-03-13 1998-03-12 HIV protease inhibitors
HU0001380A HUP0001380A3 (en) 1997-03-13 1998-03-12 Isoquinoline derivatives as hiv protease inhibitors, and pharmaceutical compositions containing them
EP98910300A EP0970055A2 (en) 1997-03-13 1998-03-12 Hiv protease inhibitors
MXPA99008395A MXPA99008395A (en) 1997-03-13 1998-03-12 Hiv protease inhibitors.
CA002284163A CA2284163A1 (en) 1997-03-13 1998-03-12 Hiv protease inhibitors
IL13187098A IL131870A0 (en) 1997-03-13 1998-03-12 Hiv protease inhibitors
EEP199900416A EE04114B1 (en) 1997-03-13 1998-03-12 HIV protease inhibitors
KR10-1999-7008331A KR100511089B1 (en) 1997-03-13 1998-03-12 HIV protease inhibitors
APAP/P/1999/001648A AP1358A (en) 1997-03-13 1998-03-12 1-Aryl-2-Hydroxy-3-Isoquinoline Carboxamide HIV Protease Inhibitors, Their Preparation and Use.
SK1222-99A SK283636B6 (en) 1997-03-13 1998-03-12 Decahydroisoquinolinecarboxamide derivatives, pharmaceutical preparations containing them and their use
JP53974598A JP2001516350A (en) 1997-03-13 1998-03-12 HIV protease inhibitor
UA99095049A UA57772C2 (en) 1997-03-13 1998-12-03 HIV protease inhibitors
IL131870A IL131870A (en) 1997-03-13 1999-09-10 Isoquinolinecarboxamide derivatives, pharmaceutical compositions comprising them and their use for the preparation of medicaments for inhibiting hiv protease
NO19994415A NO315555B1 (en) 1997-03-13 1999-09-10 HIV protease inhibitors, salt and its use, as well as pharmaceutical preparations
IS5176A IS5176A (en) 1997-03-13 1999-09-10 Antiviral protease inhibitors
BG103727A BG63540B1 (en) 1997-03-13 1999-09-13 Hiv protease inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US81595197A 1997-03-13 1997-03-13
US08/815,951 1997-03-13

Publications (2)

Publication Number Publication Date
WO1998040357A2 WO1998040357A2 (en) 1998-09-17
WO1998040357A3 true WO1998040357A3 (en) 1998-11-26

Family

ID=25219265

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1998/004735 WO1998040357A2 (en) 1997-03-13 1998-03-12 Hiv protease inhibitors

Country Status (35)

Country Link
EP (1) EP0970055A2 (en)
JP (1) JP2001516350A (en)
KR (1) KR100511089B1 (en)
CN (1) CN1179948C (en)
AP (1) AP1358A (en)
AR (1) AR012556A1 (en)
AU (1) AU743078B2 (en)
BG (1) BG63540B1 (en)
BR (1) BR9808867A (en)
CA (1) CA2284163A1 (en)
CO (1) CO4940496A1 (en)
CZ (1) CZ296647B6 (en)
EA (1) EA002378B1 (en)
EE (1) EE04114B1 (en)
GE (1) GEP20022764B (en)
HR (1) HRP980112A2 (en)
HU (1) HUP0001380A3 (en)
IL (2) IL131870A0 (en)
IS (1) IS5176A (en)
MX (1) MXPA99008395A (en)
MY (1) MY117535A (en)
NO (1) NO315555B1 (en)
NZ (1) NZ337706A (en)
OA (1) OA11196A (en)
PA (1) PA8448801A1 (en)
PE (1) PE58799A1 (en)
PL (1) PL192786B1 (en)
SA (1) SA98181116B1 (en)
SK (1) SK283636B6 (en)
SV (1) SV1998000038A (en)
TR (1) TR199902508T2 (en)
TW (1) TW200517112A (en)
UA (1) UA57772C2 (en)
WO (1) WO1998040357A2 (en)
ZA (1) ZA982047B (en)

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995009843A1 (en) * 1993-10-07 1995-04-13 Agouron Pharmaceuticals, Inc. Hiv protease inhibitors

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995009843A1 (en) * 1993-10-07 1995-04-13 Agouron Pharmaceuticals, Inc. Hiv protease inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
MARK LONGER ET AL: "Preformulation studies of a novel HIV protease inhibitor,AG1343", JOURNAL OF PHARMACEUTICAL SCIENCES., vol. 84, no. 9, September 1995 (1995-09-01), WASHINGTON US, pages 1090 - 1093, XP002076199 *

Also Published As

Publication number Publication date
CO4940496A1 (en) 2000-07-24
HUP0001380A2 (en) 2000-09-28
IS5176A (en) 1999-09-10
IL131870A0 (en) 2001-03-19
KR20000076236A (en) 2000-12-26
EE9900416A (en) 2000-04-17
SV1998000038A (en) 1999-02-15
CA2284163A1 (en) 1998-09-17
CZ296647B6 (en) 2006-05-17
EA002378B1 (en) 2002-04-25
AU743078B2 (en) 2002-01-17
HUP0001380A3 (en) 2001-12-28
BG103727A (en) 2000-04-28
CZ319199A3 (en) 2000-06-14
KR100511089B1 (en) 2005-08-31
SA98181116B1 (en) 2006-10-04
EA199900823A1 (en) 2000-04-24
EP0970055A2 (en) 2000-01-12
PL192786B1 (en) 2006-12-29
JP2001516350A (en) 2001-09-25
NO994415L (en) 1999-11-10
MY117535A (en) 2004-07-31
NZ337706A (en) 2001-04-27
NO315555B1 (en) 2003-09-22
NO994415D0 (en) 1999-09-10
SK283636B6 (en) 2003-11-04
TW200517112A (en) 2005-06-01
UA57772C2 (en) 2003-07-15
BR9808867A (en) 2000-07-11
WO1998040357A2 (en) 1998-09-17
AP1358A (en) 2004-12-03
EE04114B1 (en) 2003-08-15
AR012556A1 (en) 2000-11-08
PL335672A1 (en) 2000-05-08
AP9901648A0 (en) 1999-09-30
AU6457598A (en) 1998-09-29
PE58799A1 (en) 1999-07-12
CN1253548A (en) 2000-05-17
IL131870A (en) 2006-04-10
BG63540B1 (en) 2002-04-30
HRP980112A2 (en) 1998-12-31
SK122299A3 (en) 2000-05-16
OA11196A (en) 2003-05-21
TR199902508T2 (en) 2000-02-21
ZA982047B (en) 1998-09-28
MXPA99008395A (en) 2003-08-12
CN1179948C (en) 2004-12-15
PA8448801A1 (en) 2000-05-24
GEP20022764B (en) 2002-08-26

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