SG52731A1 - Hiv protease inhibitors useful for the treatment of aids - Google Patents

Hiv protease inhibitors useful for the treatment of aids

Info

Publication number
SG52731A1
SG52731A1 SG1996008456A SG1996008456A SG52731A1 SG 52731 A1 SG52731 A1 SG 52731A1 SG 1996008456 A SG1996008456 A SG 1996008456A SG 1996008456 A SG1996008456 A SG 1996008456A SG 52731 A1 SG52731 A1 SG 52731A1
Authority
SG
Singapore
Prior art keywords
opt
substd
aryl
halo
alkoxy
Prior art date
Application number
SG1996008456A
Other languages
English (en)
Inventor
Joseph P Vacca
Bruce D Dorsey
James P Guare
Katharine M Holloway
Randall W Hungate
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
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of SG52731A1 publication Critical patent/SG52731A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 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
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/10Heterocyclic 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic 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
    • C07D217/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (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)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
SG1996008456A 1991-11-08 1992-11-02 Hiv protease inhibitors useful for the treatment of aids SG52731A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US78950891A 1991-11-08 1991-11-08
US88382592A 1992-05-15 1992-05-15

Publications (1)

Publication Number Publication Date
SG52731A1 true SG52731A1 (en) 1998-09-28

Family

ID=27120923

Family Applications (1)

Application Number Title Priority Date Filing Date
SG1996008456A SG52731A1 (en) 1991-11-08 1992-11-02 Hiv protease inhibitors useful for the treatment of aids

Country Status (27)

Country Link
EP (1) EP0541168B1 (lv)
JP (1) JPH0733373B2 (lv)
KR (1) KR100273623B1 (lv)
AT (1) ATE163926T1 (lv)
AU (1) AU659234B2 (lv)
BG (1) BG61725B1 (lv)
CA (2) CA2081970C (lv)
CY (1) CY2090B1 (lv)
CZ (1) CZ287610B6 (lv)
DE (1) DE69224703T2 (lv)
DK (1) DK0541168T3 (lv)
ES (1) ES2112880T3 (lv)
FI (2) FI106025B (lv)
GR (1) GR3026334T3 (lv)
HK (1) HK1006060A1 (lv)
HU (1) HU220866B1 (lv)
IL (1) IL103613A (lv)
LV (1) LV12208B (lv)
NO (1) NO303383B1 (lv)
NZ (1) NZ244986A (lv)
PL (1) PL171340B1 (lv)
RO (1) RO115726B1 (lv)
RU (1) RU2131416C1 (lv)
SG (1) SG52731A1 (lv)
SK (1) SK281864B6 (lv)
UA (1) UA45945C2 (lv)
WO (1) WO1993009096A1 (lv)

Families Citing this family (74)

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US20040122000A1 (en) 1981-01-07 2004-06-24 Vertex Pharmaceuticals Incorporated. Inhibitors of aspartyl protease
USH1649H (en) 1987-07-31 1997-05-06 Barrish; Joel C. HIV protease inhibitor combinations
US5413999A (en) * 1991-11-08 1995-05-09 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
DE69333270T2 (de) 1992-03-11 2004-08-05 Narhex Ltd. Aminderivate von oxo- und hydroxy- substituierten kohlenwasserstoffen
US5888992A (en) 1992-03-11 1999-03-30 Narhex Limited Polar substituted hydrocarbons
WO1993018006A1 (en) 1992-03-11 1993-09-16 Narhex Limited Amine derivatives of oxo- and hydroxy-substitued hydrocarbons
US6071895A (en) 1992-03-11 2000-06-06 Narhex Limited Polar-substituted hydrocarbons
US5559256A (en) * 1992-07-20 1996-09-24 E. R. Squibb & Sons, Inc. Aminediol protease inhibitors
KR100336699B1 (ko) 1992-08-25 2002-05-13 윌리암스 로저 에이 레트로바이러스 프로테아제 저해제로서 유용한히드록시에틸아미노 술폰아미드
US7141609B2 (en) 1992-08-25 2006-11-28 G.D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US5783701A (en) * 1992-09-08 1998-07-21 Vertex Pharmaceuticals, Incorporated Sulfonamide inhibitors of aspartyl protease
IS2334B (is) 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
US5430150A (en) * 1992-12-16 1995-07-04 American Cyanamid Company Retroviral protease inhibitors
US5463067A (en) * 1993-07-16 1995-10-31 Merck & Co., Inc. Process for making HIV protease inhibitors
IL110255A (en) * 1993-07-16 1998-12-06 Merck & Co Inc Creation and resolution of 2 tert-butylcarboxamidopiprazine
IL110752A (en) * 1993-09-13 2000-07-26 Abbott Lab Liquid semi-solid or solid pharmaceutical composition for an HIV protease inhibitor
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IL111584A0 (en) * 1993-11-18 1995-01-24 Merck & Co Inc Prodrugs of an inhibitor of hiv protease and pharmaceutical compositions containing them
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US5733882A (en) * 1994-01-17 1998-03-31 Smithkline Beecham Corporation Retroviral protease inhibitors
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US5728840A (en) * 1994-03-04 1998-03-17 Merck & Co., Inc. Process for making an epoxide
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EP0756593B1 (de) * 1994-04-20 2000-09-20 Lonza Ag Verfahren zur herstellung von 2-piperazincarbonsäurederivaten
ES2181774T3 (es) * 1994-04-22 2003-03-01 Koei Chemical Co Procedimiento para producir n-terc-butil-2-piperazinocarboxamida.
UA49803C2 (uk) * 1994-06-03 2002-10-15 Дж.Д. Сьорль Енд Ко Спосіб лікування ретровірусних інфекцій
US5476874A (en) * 1994-06-22 1995-12-19 Merck & Co., Inc. New HIV protease inhibitors
IL114808A (en) * 1994-08-11 1999-10-28 Merck & Co Inc Combinations of protease inhibitors for the treatment of hiv infection and aids
GB2292146A (en) * 1994-08-11 1996-02-14 Merck & Co Inc HIV protease inhibitors useful for the treatment of AIDS
US5612217A (en) * 1994-10-25 1997-03-18 Merck & Co., Inc. Streptomyces sp. MA 7074 (ATCC 55605) used for microbial synthesis of HIV protease inhibitors
WO1996012492A1 (en) * 1994-10-25 1996-05-02 Merck & Co., Inc. Microbial synthesis of hiv protease inhibitors
DE4446025A1 (de) * 1994-12-22 1996-06-27 Basf Ag 2-Caroxamido-1,4,5,6-tetrahydropyrazine
DK0805803T3 (da) * 1995-01-23 2003-02-17 Lonza Ag Fremgangsmåde til fremstilling af 1,4,5,6-tetrahydropyrazin-2-carboxylsyreamider
US5508404A (en) * 1995-03-15 1996-04-16 Merck & Co., Inc. Reductive amination process
US5618937A (en) * 1995-03-15 1997-04-08 Merck & Co., Inc. Process to make HIV protease inhibitor from (2S)-4-picolyl-2-piperazine-t-butylcarboxamide
US5691372A (en) * 1995-04-19 1997-11-25 Vertex Pharmaceuticals Incorporated Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease
US5612484A (en) * 1995-05-18 1997-03-18 Merck & Co., Inc. Process for making HIV protease inhibitors
US5605819A (en) * 1995-05-19 1997-02-25 Merck & Co., Inc. Quantitative conversion of indene to (1S,2R) indene oxide and (1S,2R)-indandiol by combination of haloperoxidase bioconversion and chemical steps
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US6004957A (en) * 1995-06-07 1999-12-21 Vertex Pharmaceuticals, Incorporated Sulfonamide inhibitors of aspartyl protease
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US6645961B1 (en) 1997-03-07 2003-11-11 Merck & Co., Inc. Dry granulation formulation for an HIV protease inhibitor
US6436989B1 (en) 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
JP2002515501A (ja) * 1998-05-15 2002-05-28 アボット・ラボラトリーズ レトロウイルスプロテアーゼの阻害化合物
US6251906B1 (en) 1998-05-15 2001-06-26 Abbott Laboratories Retroviral protease inhibiting compounds
AP1717A (en) 1998-06-19 2007-01-30 Vertex Pharma Sulfonamide inhibitors of aspartyl protease.
WO2000002862A1 (en) 1998-07-08 2000-01-20 G.D. Searle & Co. Retroviral protease inhibitors
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GB8927913D0 (en) * 1989-12-11 1990-02-14 Hoffmann La Roche Amino acid derivatives
CA2032259A1 (en) * 1989-12-18 1991-06-19 Wayne J. Thompson Hiv protease inhibitors useful for the treatment of aids

Also Published As

Publication number Publication date
EP0541168A1 (en) 1993-05-12
HU220866B1 (en) 2002-06-29
NZ244986A (en) 1995-10-26
IL103613A (en) 1999-05-09
BG98745A (bg) 1995-03-31
DE69224703T2 (de) 1998-10-15
IL103613A0 (en) 1993-04-04
RU2131416C1 (ru) 1999-06-10
NO941696L (lv) 1994-06-24
BG61725B1 (bg) 1998-04-30
CA2081970C (en) 1997-07-08
FI942112A (fi) 1994-05-06
CY2090B1 (en) 2002-04-05
FI981591A (fi) 1998-07-10
FI942112A0 (fi) 1994-05-06
FI106025B (fi) 2000-11-15
DE69224703D1 (de) 1998-04-16
DK0541168T3 (da) 1998-05-11
CA2195027C (en) 2000-01-11
LV12208A (lv) 1999-01-20
JPH05279337A (ja) 1993-10-26
CZ287610B6 (cs) 2001-01-17
SK52394A3 (en) 1995-02-08
GR3026334T3 (en) 1998-06-30
HK1006060A1 (en) 2003-07-10
CA2195027A1 (en) 1993-05-09
NO303383B1 (no) 1998-07-06
JPH0733373B2 (ja) 1995-04-12
LV12208B (lv) 1999-03-20
SK281864B6 (sk) 2001-08-06
AU2819992A (en) 1993-05-13
ATE163926T1 (de) 1998-03-15
HU9401424D0 (en) 1994-08-29
RO115726B1 (ro) 2000-05-30
ES2112880T3 (es) 1998-04-16
PL171340B1 (pl) 1997-04-30
FI981591A0 (fi) 1992-11-03
UA45945C2 (uk) 2002-05-15
EP0541168B1 (en) 1998-03-11
NO941696D0 (no) 1994-05-06
KR100273623B1 (ko) 2000-12-15
AU659234B2 (en) 1995-05-11
CA2081970A1 (en) 1993-05-09
CZ111094A3 (en) 1995-03-15
WO1993009096A1 (en) 1993-05-13
HUT70519A (en) 1995-10-30

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