PL311635A1 - Hiv protease inhibitors useful in treating aids - Google Patents

Hiv protease inhibitors useful in treating aids

Info

Publication number
PL311635A1
PL311635A1 PL94311635A PL31163594A PL311635A1 PL 311635 A1 PL311635 A1 PL 311635A1 PL 94311635 A PL94311635 A PL 94311635A PL 31163594 A PL31163594 A PL 31163594A PL 311635 A1 PL311635 A1 PL 311635A1
Authority
PL
Poland
Prior art keywords
protease inhibitors
hiv protease
inhibitors useful
treating aids
aids
Prior art date
Application number
PL94311635A
Other languages
English (en)
Inventor
Joseph P Vacca
Bruce D Dorsey
James P Guare
M Katharine Holloway
Randall W Hungate
Rhonda B Levin
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 PL311635A1 publication Critical patent/PL311635A1/xx

Links

Classifications

    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic 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
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
PL94311635A 1993-05-07 1994-04-26 Hiv protease inhibitors useful in treating aids PL311635A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/059,038 US5413999A (en) 1991-11-08 1993-05-07 HIV protease inhibitors useful for the treatment of AIDS
PCT/US1994/004621 WO1994026717A1 (en) 1993-05-07 1994-04-26 Hiv protease inhibitors useful for the treatment of aids

Publications (1)

Publication Number Publication Date
PL311635A1 true PL311635A1 (en) 1996-03-04

Family

ID=22020419

Family Applications (1)

Application Number Title Priority Date Filing Date
PL94311635A PL311635A1 (en) 1993-05-07 1994-04-26 Hiv protease inhibitors useful in treating aids

Country Status (20)

Country Link
US (3) US5413999A (OSRAM)
EP (1) EP0696277A1 (OSRAM)
JP (1) JPH08509980A (OSRAM)
CN (2) CN1126469A (OSRAM)
AU (1) AU676563B2 (OSRAM)
BG (1) BG100114A (OSRAM)
BR (1) BR9406576A (OSRAM)
CA (1) CA2161334A1 (OSRAM)
CZ (1) CZ290095A3 (OSRAM)
FI (1) FI955315A7 (OSRAM)
HR (1) HRP940286A2 (OSRAM)
HU (1) HUT73135A (OSRAM)
IL (1) IL109503A0 (OSRAM)
MX (1) MX9403380A (OSRAM)
NO (1) NO954427L (OSRAM)
PL (1) PL311635A1 (OSRAM)
SK (1) SK136395A3 (OSRAM)
TW (1) TW256830B (OSRAM)
WO (1) WO1994026717A1 (OSRAM)
ZA (1) ZA943104B (OSRAM)

Families Citing this family (147)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5717097A (en) * 1991-11-08 1998-02-10 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
US5413999A (en) * 1991-11-08 1995-05-09 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
AU680635C (en) 1992-08-25 2007-05-17 G.D. Searle Llc Hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
IL111584A0 (en) * 1993-11-18 1995-01-24 Merck & Co Inc Prodrugs of an inhibitor of hiv protease and pharmaceutical compositions containing them
AU692509B2 (en) * 1993-12-15 1998-06-11 Merck & Co., Inc. HIV protease inhibitors
TW472047B (en) * 1994-02-04 2002-01-11 Merck & Co Inc Process for making HIV protease inhibitors
WO1995029169A2 (de) * 1994-04-20 1995-11-02 Lonza Ag Verfahren zur herstellung von 2-piperazincarbonsäurederivaten
US5489685A (en) * 1994-05-12 1996-02-06 Merck & Co., Ltd. Method of synthesizing furo[2,3-b]pyridine carboxylic acid esters
UA49803C2 (uk) * 1994-06-03 2002-10-15 Дж.Д. Сьорль Енд Ко Спосіб лікування ретровірусних інфекцій
US20030207813A1 (en) * 1996-12-09 2003-11-06 G.D. Searle Retroviral protease inhibitor combinations
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
ES2116029T3 (es) * 1994-11-04 1998-07-01 Yamakawa Chemical Ind Procedimiento para preparar derivados de piperazina opticamente activos e intermedios para prepararlos.
US5939549A (en) * 1995-01-23 1999-08-17 Lonza Ag Process for the production of 1,4,5,6-tetrahydropyrazine-2-carboxylic acid amides
US6689761B1 (en) * 1995-02-01 2004-02-10 Merck & Co., Inc. Combination therapy for HIV infection
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
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
JP3665976B2 (ja) * 1995-06-29 2005-06-29 東レ・ファインケミカル株式会社 光学分割剤およびそれを用いた光学活性Ｎ−ｔｅｒｔ−ブチル−２−ピペラジンカルボキシアミドの製造法
US6037157A (en) 1995-06-29 2000-03-14 Abbott Laboratories Method for improving pharmacokinetics
GB2307683A (en) * 1995-10-31 1997-06-04 Merck & Co Inc HIV protease inhibitors useful for the treatment of AIDS
US5914332A (en) 1995-12-13 1999-06-22 Abbott Laboratories Retroviral protease inhibiting compounds
CA2190304A1 (en) * 1995-12-15 1997-06-16 Elazar Rabbani Property effecting and/or property exhibiting compositions for therapeutic and diagnostic uses
US5883252A (en) * 1996-01-26 1999-03-16 Vertex Pharmaceuticals Incorporated Aspartyl protease inhibitors
US5846978A (en) * 1996-05-02 1998-12-08 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
US5811462A (en) * 1996-05-02 1998-09-22 Merck & Co., Inc. HIV Protease inhibitors useful for the treatment of AIDS
JP2000509389A (ja) * 1996-05-02 2000-07-25 メルク エンド カンパニー インコーポレーテッド Ａｉｄｓの治療に有効なｈｉｖプロテアーゼインヒビター
US5747540A (en) * 1996-10-21 1998-05-05 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
US5783709A (en) * 1996-10-31 1998-07-21 Merck & Co., Inc. Stereoselective process for making substituted amino acid derivatives
ZA9710071B (en) * 1996-11-21 1998-05-25 Abbott Lab Pharmaceutical composition.
US6232333B1 (en) 1996-11-21 2001-05-15 Abbott Laboratories Pharmaceutical composition
US6645961B1 (en) * 1997-03-07 2003-11-11 Merck & Co., Inc. Dry granulation formulation for an HIV protease inhibitor
ATE383161T1 (de) 1997-04-15 2008-01-15 Advanced Viral Res Corp Kombination von product r mit einem antiviralen mittel in der behandlung von hiv infektionen
US5981759A (en) * 1997-06-20 1999-11-09 Merck & Co., Inc. Process for indinavir intermediate
HRP980443A2 (en) * 1997-08-18 1999-10-31 Carl P. Decicco Novel inhibitors of aggrecanase and matrix metalloproteinases for the treatment of arthritis
US6180634B1 (en) 1997-11-13 2001-01-30 Merck & Co., Inc. Combination therapy for the treatment of AIDS
US6143742A (en) * 1997-12-11 2000-11-07 Fuisz Technologies Ltd Treatment for necrotizing infections
GB2336841A (en) 1998-04-28 1999-11-03 Merck & Co Inc Preparation of cis-(is,2r)-indanediol by the microbial reduction of 1,2-indanedione
US7045519B2 (en) * 1998-06-19 2006-05-16 Chiron Corporation Inhibitors of glycogen synthase kinase 3
EP1087963B1 (en) 1998-06-19 2004-08-25 Chiron Corporation Inhibitors of glycogen synthase kinase 3
MXPA00012842A (es) * 1998-06-24 2004-06-22 Univ Emory Uso de 3'-azido-2',3'-didesoxiuridina en combinacion de drogas adicionales contra el vih para la manufactura de un medicamento para el tratamiento del vih.
US6538006B1 (en) 1998-07-08 2003-03-25 Pharmacia Corporation Retroviral protease inhibitors
GB2341385A (en) 1998-09-14 2000-03-15 Merck & Co Inc Recovery of iodide from chemical process waste water
US7635690B2 (en) * 1999-01-22 2009-12-22 Emory University HIV-1 mutations selected for by β-2′,3′-didehydro-2′,3′-dideoxy-5-fluorocytidine
US7115584B2 (en) * 1999-01-22 2006-10-03 Emory University HIV-1 mutations selected for by β-2′,3′-didehydro-2′,3′-dideoxy-5-fluorocytidine
WO2000045844A1 (en) * 1999-02-03 2000-08-10 Franco Lori Use of hydroxyurea and a reverse transcriptase inhibitor to induce autovaccination by autologous hiv
DE60029219T2 (de) * 1999-06-04 2007-06-28 Abbott Laboratories, Abbott Park Verbesserte arzneizubereitungen enthaltend ritonavir
WO2001000663A2 (en) * 1999-06-28 2001-01-04 Oklahoma Medical Research Foundation Catalytically active recombinant memapsin and methods of use thereof
US6589962B1 (en) 1999-07-20 2003-07-08 Merck & Co., Inc. Alpha-hydroxy-gamma-[[(carbocyclic-or heterocyclic-substituted)amino]carbonyl]alkanamide derivatives and uses thereof
EP1202626A4 (en) * 1999-07-20 2002-10-30 Merck & Co Inc ALPHA HYDROXY GAMMA (CARBOZYCLIC OR HETEROCYCLICALLY SUBSTITUTED) AMINOCARBONYLALKANAMIDE DERIVATIVES AND THEIR USE
NL1012825C2 (nl) * 1999-08-13 2001-02-23 Faculteit Geneeskunde Universi Farmaceuticum voor de behandeling van virale infecties in het bijzonder van het humane immunodeficiency virus (HIV).
DE60036961T2 (de) * 1999-11-24 2008-08-28 Merck & Co., Inc. Gamma-hydroxy-2-(fluoralkylaminocarbonyl)-1-piperazinpentanamide als hiv-proteasehemmer
IL150265A0 (en) 2000-01-19 2002-12-01 Abbott Lab Improved pharmaceutical formulations comprising one or more solubilized hiv protease inhibiting compounds
US6476034B2 (en) 2000-02-22 2002-11-05 Bristol-Myers Squibb Company Antiviral azaindole derivatives
JP2003531865A (ja) * 2000-04-28 2003-10-28 アメリカ合衆国 Ｄｎａおよびワクシニアウイルスベクターワクチンの組み合わせを用いた免疫原性の改善
WO2001082919A2 (en) 2000-05-04 2001-11-08 The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Methods of and compounds for inhibiting calpains
US6384244B2 (en) 2000-05-18 2002-05-07 Merck & Co., Inc. Process for preparing cis- aminochromanols
US6482952B2 (en) 2000-06-20 2002-11-19 Merck & Co., Inc. Process for preparing acetonides
US6573262B2 (en) 2000-07-10 2003-06-03 Bristol-Myers Sqibb Company Composition and antiviral activity of substituted indoleoxoacetic piperazine derivatives
US6531617B2 (en) 2000-10-24 2003-03-11 Merck & Co., Inc. Process for preparing hydroxychomanones and cis-aminochromanols
US6777395B2 (en) 2001-01-22 2004-08-17 Merck & Co., Inc. Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase of hepatitis C virus
US20030207910A1 (en) 2001-02-02 2003-11-06 Tao Wang Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
US7202092B2 (en) * 2001-07-13 2007-04-10 Roche Diagnostics Operations, Inc. Indinavir derivatives useful in immunoassay
US20030191121A1 (en) * 2001-08-09 2003-10-09 Miller Ross A. Piperazine carboxamide intermediates of HIV protease inhibitors and processes for their preparation
AU2003216049B2 (en) * 2002-01-17 2008-07-17 Merck Sharp & Dohme Corp. Hydroxynaphthyridinone carboxamides useful as HIV integrase inhibitors
US20040067216A1 (en) * 2002-02-22 2004-04-08 Karki Shyam B. Hiv protease inhibitors supported on cation exchange resins for oral administration
CN1649614A (zh) 2002-02-22 2005-08-03 新河药品股份有限公司 活性剂传递系统和保护及施用活性剂的方法
US20060094006A1 (en) * 2002-05-01 2006-05-04 Genoveffa Franchini Immunotherapy regimens in hiv-infected patients
PT2314591E (pt) 2002-05-16 2014-09-19 Janssen R & D Ireland Formas pseudopolimórficas de um inibidor de protease de vih
WO2003106405A1 (en) * 2002-06-01 2003-12-24 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
US7115652B2 (en) * 2002-06-17 2006-10-03 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
US8876532B2 (en) 2002-07-31 2014-11-04 Dentsply International Inc. Bone repair putty
US7199240B2 (en) * 2002-12-11 2007-04-03 Merck & Co., Inc. Reductive alkylation of saturated cyclic amines
EP1758453B1 (en) 2004-06-15 2014-07-16 Merck Sharp & Dohme Corp. C-purine nucleoside analogs as inhibitors of rna-dependent rna viral polymerase
US7868037B2 (en) * 2004-07-14 2011-01-11 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7781478B2 (en) * 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7772271B2 (en) * 2004-07-14 2010-08-10 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US8013006B2 (en) * 2004-07-14 2011-09-06 Ptc Therapeutics, Inc. Methods for treating hepatitis C
JP2008507518A (ja) * 2004-07-22 2008-03-13 ピーティーシー セラピューティクス，インコーポレーテッド Ｃ型肝炎を治療するためのチエノピリジン
PL216369B1 (pl) 2004-07-27 2014-03-31 Gilead Sciences Pochodne fosfonianowe, kompozycje farmaceutyczne zawierające te pochodne oraz zastosowanie tych pochodnych do wytwarzania leku do hamowania wirusa HIV
US20060100209A1 (en) * 2004-11-09 2006-05-11 Chong-Hui Gu Formulations of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione
US20060100432A1 (en) * 2004-11-09 2006-05-11 Matiskella John D Crystalline materials of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione
UA87884C2 (uk) * 2004-12-03 2009-08-25 Мерк Энд Ко., Инк. Безводна кристалічна калієва сіль інгібітора віл-інтегрази
US7598380B2 (en) * 2005-08-03 2009-10-06 Bristol-Myers Squibb Company Method of preparation of azaindole derivatives
EP1922083A2 (en) * 2005-08-10 2008-05-21 Oklahoma Medical Research Foundation Truncated memapsin 2 for use for treating alzheimer's disease
US20090087456A1 (en) * 2005-09-07 2009-04-02 James Edward Eyles Adjuvanted vaccine
GB0519871D0 (en) * 2005-09-30 2005-11-09 Secr Defence Immunogenic agents
US7851476B2 (en) * 2005-12-14 2010-12-14 Bristol-Myers Squibb Company Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-YL)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-C]pyridin-3-YL]-1,2-dioxoethyl]-piperazine
US7807671B2 (en) * 2006-04-25 2010-10-05 Bristol-Myers Squibb Company Diketo-piperazine and piperidine derivatives as antiviral agents
US8323664B2 (en) * 2006-07-25 2012-12-04 The Secretary Of State For Defence Live vaccine strains of Francisella
CA2673649A1 (en) 2007-01-05 2008-07-17 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Nucleoside aryl phosphoramidates for the treatment of rna-dependent rna viral infection
AU2008226823B2 (en) 2007-03-12 2014-03-13 Nektar Therapeutics Oligomer-protease inhibitor conjugates
GB0709791D0 (en) * 2007-05-22 2007-06-27 Angeletti P Ist Richerche Bio Antiviral agents
KR20100028656A (ko) * 2007-06-29 2010-03-12 길리애드 사이언시즈, 인코포레이티드 치료 조성물 및 그의 용도
WO2009006199A1 (en) * 2007-06-29 2009-01-08 Gilead Sciences, Inc. Therapeutic compositions and the use thereof
GB0718575D0 (en) * 2007-09-24 2007-10-31 Angeletti P Ist Richerche Bio Nucleoside derivatives as inhibitors of viral polymerases
EP2203420A1 (en) * 2007-09-25 2010-07-07 Merck Sharp & Dohme Corp. Hiv protease inhibitors
GB0720503D0 (en) * 2007-10-22 2007-11-28 Angeletti P Ist Richerche Bio New compound
US9095620B2 (en) * 2008-03-12 2015-08-04 Nektar Therapeutics Reagents
SG172060A1 (en) 2008-12-09 2011-07-28 Gilead Sciences Inc Modulators of toll-like receptors
GB0900455D0 (en) 2009-01-13 2009-02-11 Secr Defence Vaccine
GB0901411D0 (en) 2009-01-29 2009-03-11 Secr Defence Treatment
GB0901423D0 (en) 2009-01-29 2009-03-11 Secr Defence Treatment
GB0906234D0 (en) 2009-04-14 2009-05-20 Secr Defence Vaccine
WO2010138338A1 (en) 2009-05-27 2010-12-02 Merck Sharp & Dohme Corp. Hiv protease inhibitors
EP2440249A2 (en) 2009-06-12 2012-04-18 Nektar Therapeutics Covalent conjugates comprising a protease inhibitor, a water-soluble, non-peptidic oligomer and a lipophilic moiety
DE102010004957A1 (de) 2010-01-14 2011-07-21 Universitätsklinikum Jena, 07743 Biologisch wirksame Moleküle zur Beeinflussung von Virus-, Bakterien-, Parasiten-infizierten Zellen und/oder Tumorzellen und Verfahren zu deren Anwendung
US20110223131A1 (en) 2010-02-24 2011-09-15 Gilead Sciences, Inc. Antiviral compounds
WO2011106705A2 (en) 2010-02-26 2011-09-01 The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Dna-protein vaccination protocols
CN102985438B (zh) 2010-06-04 2016-05-18 百时美施贵宝公司 作为hiv成熟抑制剂的经修饰c-3桦木酸衍生物的c-28酰胺
ES2612452T3 (es) 2010-06-04 2017-05-17 VIIV Healthcare UK (No.5) Limited Derivados de ácido betulínico C-3 modificados como inhibidores de la maduración del VIH
US8450361B2 (en) 2010-08-06 2013-05-28 Bristol-Myers Squibb Company Substituted indole and azaindole oxoacetyl piperazinamide derivatives
US9079834B2 (en) 2010-10-28 2015-07-14 Merck Canada Inc. HIV protease inhibitors
US8912195B2 (en) 2010-12-02 2014-12-16 Bristol-Myers Squibb Company Alkyl amides as HIV attachment inhibitors
US8846647B2 (en) 2011-01-31 2014-09-30 Bristol-Myers Squibb Company C-17 and C-3 modified triterpenoids with HIV maturation inhibitory activity
CA2826257A1 (en) 2011-01-31 2012-08-09 Bristol-Myers Squibb Company C-28 amines of c-3 modified betulinic acid derivatives as hiv maturation inhibitors
EP2696937B1 (en) 2011-04-12 2017-05-17 VIIV Healthcare UK (No.5) Limited Thioamide, amidoxime and amidrazone derivatives as hiv attachment inhibitors
EP2751119B1 (en) 2011-08-29 2016-11-23 VIIV Healthcare UK (No.5) Limited Fused bicyclic diamine derivatives as hiv attachment inhibitors
US8664213B2 (en) 2011-08-29 2014-03-04 Bristol-Myers Squibb Company Spiro bicyclic diamine derivatives as HIV attachment inhibitors
TW201317255A (zh) 2011-09-21 2013-05-01 必治妥美雅史谷比公司 具抗病毒活性之新穎樺木酸衍生物
EP2771332B1 (en) 2011-10-26 2016-06-29 Merck Canada Inc. Thiophen and thiazol sulfonamid derivatives as HIV protease inhibitors for the treatment of AIDS
US8906889B2 (en) 2012-02-15 2014-12-09 Bristol-Myers Squibb Company C-3 cycloalkenyl triterpenoids with HIV maturation inhibitory activity
US9193725B2 (en) 2012-03-14 2015-11-24 Bristol-Meyers Squibb Company Cyclic hydrazine derivatives as HIV attachment inhibitors
US8889854B2 (en) 2012-05-07 2014-11-18 Bristol-Myers Squibb Company C-17 bicyclic amines of triterpenoids with HIV maturation inhibitory activity
US9655888B2 (en) 2012-08-09 2017-05-23 VIIV Healthcare UK (No.5) Limited Tricyclic alkene derivatives as HIV attachment inhibitors
US9505752B2 (en) 2012-08-09 2016-11-29 Viiv Healthcare Uk (No. 5) Limited Piperidine amide derivatives as HIV attachment inhibitors
RU2015113091A (ru) 2012-09-11 2016-11-10 Мерк Шарп И Доум Корп. Ингибиторы протеазы вич
EP2953960A1 (en) 2013-02-06 2015-12-16 Bristol-Myers Squibb Company C-19 modified triterpenoids with hiv maturation inhibitory activity
SG11201506445PA (en) 2013-02-25 2015-09-29 Bristol Myers Squibb Co C-3 alkyl and alkenyl modified betulinic acid derivatives useful in the treatment of hiv
WO2015013835A1 (en) 2013-07-31 2015-02-05 Merck Sharp & Dohme Corp. Piperazine derivatives as hiv protease inhibitors
EP3082822B1 (en) 2013-12-19 2020-01-15 Merck Sharp & Dohme Corp. Hiv protease inhibitors
EP3083609B1 (en) 2013-12-19 2018-08-15 Merck Sharp & Dohme Corp. Hiv protease inhibitors
DE102014202609B4 (de) 2014-02-13 2020-06-04 tooz technologies GmbH Aminkatalysierte Thiolhärtung von Epoxidharzen
WO2015134366A1 (en) 2014-03-06 2015-09-11 Merck Sharp & Dohme Corp. Hiv protease inhibitors
WO2015138220A1 (en) 2014-03-10 2015-09-17 Merck Sharp & Dohme Corp. Piperazine derivatives as hiv protease inhibitors
AU2015243500B2 (en) 2014-04-11 2017-03-30 ViiV Healthcare UK (No.4) Limited Triterpenoids with HIV maturation inhibitory activity, substituted in position 3 by a non-aromatic ring carrying a haloalkyl substituent
WO2015195776A1 (en) 2014-06-19 2015-12-23 Bristol-Myers Squibb Company Betulinic acid derivatives with hiv maturation inhibitory activity
WO2016001907A1 (en) 2014-07-02 2016-01-07 Prendergast Patrick T Mogroside iv and mogroside v as agonist/stimulator/un-blocking agent for toll-like receptor 4 and adjuvant for use in human/animal vaccine and to stimulate immunity against disease agents.
NZ728072A (en) 2014-07-11 2018-06-29 Gilead Sciences Inc Modulators of toll-like receptors for the treatment of hiv
EP3212196A4 (en) 2014-10-29 2018-07-11 Wisconsin Alumni Research Foundation Boronic acid inhibitors of hiv protease
RU2017118576A (ru) 2014-11-14 2018-12-14 ВАЙВ ХЕЛТКЕР ЮКей (N5) ЛИМИТЕД C-17-арил-замещённые аналоги бетулиновой кислоты
AU2015346303B2 (en) 2014-11-14 2018-03-15 VIIV Healthcare UK (No.5) Limited Oxolupene derivatives
RU2017134461A (ru) 2015-04-14 2019-05-14 ВАЙВ ХЕЛТКЕР ЮКей (N4) ЛИМИТЕД Способы получения ингибитора созревания HIV
WO2016183420A1 (en) 2015-05-13 2016-11-17 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Methods and compositions for inducing an immune response using conserved element constructs
EP3349757A1 (en) 2015-09-15 2018-07-25 Gilead Sciences, Inc. Modulators of toll-like recptors for the treatment of hiv
AR107512A1 (es) 2016-02-04 2018-05-09 VIIV HEALTHCARE UK Nº 5 LTD Triterpenoides modificados en c-3 y c-17 como inhibidores del vih-1
US10239847B1 (en) 2016-03-03 2019-03-26 Cellactin Method for 2-oxothiazolidine-4-carboxylic acid for cellular glutathione
CN108324716A (zh) * 2018-04-18 2018-07-27 日照市普达医药科技有限公司 一种含有茚地那韦的抗hiv药物及制备方法
EP4551247A1 (en) 2022-07-07 2025-05-14 The United States of America, as represented by the Secretary, Department of Health and Human Services Immunogens and methods for inducing an immune response

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4198509A (en) * 1978-10-30 1980-04-15 E. R. Squibb & Sons, Inc. Mercaptoacylpiperazine carboxylic acid compounds
DE3134933A1 (de) * 1981-09-03 1983-03-31 Hoechst Ag, 6230 Frankfurt "harnstoffderivate, verfahren zu ihrer herstellung und diese enthaltende medikamente sowie deren verwendung"
US4661473A (en) * 1984-03-27 1987-04-28 Merck & Co., Inc. Renin inhibitors containing peptide isosteres
FI88400C (fi) * 1984-08-06 1993-05-10 Upjohn Co Foerfarande foer framstaellning av renin inhiberande peptider
CA1290097C (en) * 1985-07-24 1991-10-01 Merck & Co., Inc. Peptide enzyme inhibitors
IL89900A0 (en) * 1988-04-12 1989-12-15 Merck & Co Inc Hiv protease inhibitors useful for the treatment of aids and pharmaceutical compositions containing them
IL90218A0 (en) * 1988-05-13 1989-12-15 Abbott Lab Retroviral protease inhibitors
DK414389A (da) * 1988-08-24 1990-02-26 Merck & Co Inc Farmaceutisk praeparat indeholdende et aminosyrederivat med renin-inhibitorisk virkning
IL91307A0 (en) * 1988-08-24 1990-03-19 Merck & Co Inc Hiv protease inhibitors and pharmaceutical compositions for the treatment of aids containing them
CA2010531A1 (en) * 1989-03-06 1990-09-06 Werner Neidhart Amino acid derivatives
US5063208A (en) * 1989-07-26 1991-11-05 Abbott Laboratories Peptidyl aminodiol renin inhibitors
IE902446A1 (en) * 1989-07-26 1991-02-13 Abbott Lab Peptidyl aminodiol renin inhibitors
IL95380A0 (en) * 1989-09-05 1991-06-30 Abbott Lab Peptidyl difluorodiol renin inhibitors
GB8927915D0 (en) * 1989-12-11 1990-02-14 Hoffmann La Roche Novel alcohols
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
CA2055685A1 (en) * 1990-11-19 1992-05-20 Samuel L. Graham Hiv protease inhibitors having polyether substituents
IE913840A1 (en) * 1990-11-20 1992-05-20 Abbott Lab Retroviral protease inhibiting compounds
EP0492136A3 (en) * 1990-12-20 1993-05-26 American Cyanamid Company Retroviral protease inhibitors derived from 3-chloro-2-chloromethyl-1-propene
EP0572547A1 (en) * 1991-02-22 1993-12-08 The Du Pont Merck Pharmaceutical Company SUBSTITUTED $g(a)-AMINOALDEHYDES AND DERIVATIVES
US5430041A (en) * 1991-05-10 1995-07-04 Hoffmann-La Roche Inc. Amino acid derivatives having antiviral activity
US5192764A (en) * 1991-05-30 1993-03-09 Research Foundation Of State Of N.Y. Pyrazinone n-oxide nucleosides and analogs thereof
US5169952A (en) * 1991-07-02 1992-12-08 Merck & Co., Inc. Stereoselective production of hydroxyamide compounds from chiral α-amino epoxides
JPH05208947A (ja) * 1991-08-16 1993-08-20 Merck & Co Inc Ｎ末端にポリエーテル置換基を有するｈｉｖプロテアーゼ抑制剤
WO1993008184A1 (en) * 1991-10-23 1993-04-29 Merck & Co., Inc. Hiv protease inhibitors
DK0541168T3 (da) * 1991-11-08 1998-05-11 Merck & Co Inc HIV-proteaseinhibitorer, som er egnede til behandling af AIDS
US5413999A (en) * 1991-11-08 1995-05-09 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
CA2091151A1 (en) * 1992-03-13 1993-09-14 Kwan Y. Hui Retroviral protease inhibitors
DK0566557T3 (da) * 1992-04-01 1996-11-04 Searle & Co 2- og 3-amino- og azidoderivater af 1,5- iminosukkere som antivirale forbindelser
GB2270914A (en) 1992-09-14 1994-03-30 Merck & Co Inc HIV protease inhibitor compounds
US5430150A (en) * 1992-12-16 1995-07-04 American Cyanamid Company Retroviral protease inhibitors

Also Published As

Publication number Publication date
WO1994026717A1 (en) 1994-11-24
CA2161334A1 (en) 1994-11-24
NO954427D0 (no) 1995-11-06
US5527799A (en) 1996-06-18
ZA943104B (en) 1995-11-06
JPH08509980A (ja) 1996-10-22
HU9503170D0 (en) 1996-01-29
IL109503A0 (en) 1994-08-26
HUT73135A (en) 1996-06-28
FI955315L (fi) 1995-11-06
NO954427L (no) 1996-01-08
BG100114A (bg) 1996-04-30
CN1176250A (zh) 1998-03-18
US5413999A (en) 1995-05-09
AU6669294A (en) 1994-12-12
HRP940286A2 (en) 1996-08-31
FI955315A0 (fi) 1995-11-06
BR9406576A (pt) 1996-01-30
AU676563B2 (en) 1997-03-13
FI955315A7 (fi) 1995-11-06
TW256830B (OSRAM) 1995-09-11
US5668132A (en) 1997-09-16
CN1126469A (zh) 1996-07-10
MX9403380A (es) 1995-01-31
CZ290095A3 (en) 1996-05-15
EP0696277A1 (en) 1996-02-14
SK136395A3 (en) 1996-06-05

Similar Documents

Publication Publication Date Title
PL311635A1 (en) Hiv protease inhibitors useful in treating aids
KR100190517B1 (en) Hiv protease inhibitors
HU9601508D0 (en) Dp-iv-serine protease inhibitors
ZA929869B (en) Hiv protease inhibitors
HU9202842D0 (en) Climotripsine-type proteases and inhibitors
NZ248332A (en) Hiv protease inhibitor and its use
HU9302080D0 (en) Amine-diole protease inhibitors
EP0604182A3 (en) HIV protease inhibiting compounds.
IL102428A0 (en) Inhibitors of hiv protease useful for the treatment of aids
FI935777A7 (fi) AIDSin hoitamisessa käyttökelpoiset HIV-proteaasin inhibiittorit
HU9303677D0 (en) Inhibitors of hiv protease useful for the treatment of aids
EP0691345A3 (en) Combinations of HIV protease inhibitors
IL105973A0 (en) Inhibitors of hiv protease useful for the treatment of aids
ZA925023B (en) Inhibitors of HIV protease useful for the treatment of AIDS
ZA914136B (en) Hiv protease inhibitors and processes for their preparation
EP0443560A3 (en) Hiv protease inhibitors
GB9515802D0 (en) Hiv protease inhibitors useful for the treatment of aids
ZA945234B (en) Process for making HIV protease inhibitors
AU6828894A (en) Hiv protease inhibitors
EP0594586A4 (en) Hiv protease inhibitors
GB9318445D0 (en) Hiv protease in inhibitor compounds
EP0575500A4 (en) Hiv protease inhibitors
GB9613488D0 (en) HIV protease inhibitors useful in the treatment of aids
SG49247A1 (en) Hiv protease inhibitors
HU0900220D0 (en) Hiv protease inhibitors