HRP940286A2 - Hiv proteaze inhibitors useful for the treatment of aids - Google Patents

Hiv proteaze inhibitors useful for the treatment of aids Download PDF

Info

Publication number
HRP940286A2
HRP940286A2 HR08/059,038A HRP940286A HRP940286A2 HR P940286 A2 HRP940286 A2 HR P940286A2 HR P940286 A HRP940286 A HR P940286A HR P940286 A2 HRP940286 A2 HR P940286A2
Authority
HR
Croatia
Prior art keywords
alkyl
substituted
unsubstituted
aryl
hydroxy
Prior art date
Application number
HR08/059,038A
Other languages
English (en)
Croatian (hr)
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 HRP940286A2 publication Critical patent/HRP940286A2/hr

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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic 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
    • C07C237/20Carboxylic 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00Systems containing two condensed rings
    • C07C2602/02Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04One of the condensed rings being a six-membered aromatic ring
    • C07C2602/08One 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
HR08/059,038A 1993-05-07 1994-05-05 Hiv proteaze inhibitors useful for the treatment of aids HRP940286A2 (en)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
HRP940286A2 true HRP940286A2 (en) 1996-08-31

Family

ID=22020419

Family Applications (1)

Application Number Title Priority Date Filing Date
HR08/059,038A HRP940286A2 (en) 1993-05-07 1994-05-05 Hiv proteaze inhibitors useful for the treatment of aids

Country Status (20)

Country Link
US (3) US5413999A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EP (1) EP0696277A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
JP (1) JPH08509980A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CN (2) CN1126469A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AU (1) AU676563B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
BG (1) BG100114A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
BR (1) BR9406576A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CA (1) CA2161334A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CZ (1) CZ290095A3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
FI (1) FI955315A0 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
HR (1) HRP940286A2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
HU (1) HUT73135A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IL (1) IL109503A0 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MX (1) MX9403380A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
NO (1) NO954427L (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PL (1) PL311635A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
SK (1) SK136395A3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
TW (1) TW256830B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
WO (1) WO1994026717A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ZA (1) ZA943104B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)

Families Citing this family (147)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5413999A (en) * 1991-11-08 1995-05-09 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
US5717097A (en) * 1991-11-08 1998-02-10 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
CA2140929C (en) 1992-08-25 2006-09-12 Michael L. Vazquez 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
EP0734387B1 (en) * 1993-12-15 2002-04-10 Merck & Co. Inc. Hiv protease inhibitors
TW472047B (en) * 1994-02-04 2002-01-11 Merck & Co Inc Process for making HIV protease inhibitors
US5856485A (en) * 1994-04-20 1999-01-05 Lonza Ag Process for preparing 2-piperazinecarboxylic acid derivatives
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
ATE163642T1 (de) * 1994-11-04 1998-03-15 Yamakawa Chemical Ind Verfahren zur herstellung von optisch aktiven piperazinderivaten und zwischenprodukten für ihre herstellung
DE59609835D1 (de) * 1995-01-23 2002-12-05 Lonza Ag Visp Verfahren zur herstellung von 1,4,5,6-tetrahydropyrazin-2-carbonsäureamiden
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
US6037157A (en) 1995-06-29 2000-03-14 Abbott Laboratories Method for improving pharmacokinetics
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
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
CA2279669A1 (en) * 1995-12-15 1997-06-16 Enzo Therapeutics, Inc. Property effecting and/or property exhibiting constructs for the expression of non-native nucleic acid processing components 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
EP0912170A4 (en) * 1996-05-02 2003-04-09 Merck & Co Inc HIV PROTEASE INHIBITORS USEFUL IN AIDS TREATMENT
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
JP2001520657A (ja) 1997-04-15 2001-10-30 アドバンスド バイラル リサーチ コーポレイション Hiv感染用コンビネーションセラピー
US5981759A (en) * 1997-06-20 1999-11-09 Merck & Co., Inc. Process for indinavir intermediate
US6576664B1 (en) * 1997-08-18 2003-06-10 Bristol-Myers Squibb Pharma Company 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
US6417185B1 (en) 1998-06-19 2002-07-09 Chiron Corporation Inhibitors of glycogen synthase kinase 3
US7045519B2 (en) * 1998-06-19 2006-05-16 Chiron Corporation Inhibitors of glycogen synthase kinase 3
US6194391B1 (en) * 1998-06-24 2001-02-27 Emory University 3′-azido-2′,3′-dideoxyuridine administration to treat HIV and related test protocol
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
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
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
WO2000045844A1 (en) * 1999-02-03 2000-08-10 Franco Lori Use of hydroxyurea and a reverse transcriptase inhibitor to induce autovaccination by autologous hiv
HU229501B1 (hu) * 1999-06-04 2014-01-28 Abbvie Inc HIV proteáz gátló vegyületet tartalmazó gyógyszerkészítmények
AU5771500A (en) * 1999-06-28 2001-01-31 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).
JP2003514910A (ja) 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 Hivプロテアーゼ阻害剤としてのガンマ−ヒドロキシ−2−(フルオロアルキルアミノカルボニル)−1−ピペラジンペンタンアミド類
KR100861885B1 (ko) * 2000-01-19 2008-10-09 아보트 러보러터리즈 개선된 약제학적 조성물
US6476034B2 (en) * 2000-02-22 2002-11-05 Bristol-Myers Squibb Company Antiviral azaindole derivatives
AU5929101A (en) * 2000-04-28 2001-11-12 Us Gov Health & Human Serv Improved immunogenicity using a combination of dna and vaccinia virus vector vaccines
US6448245B1 (en) 2000-05-04 2002-09-10 The United States Of America As Represented By 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
WO2003079972A2 (en) 2002-02-22 2003-10-02 New River Parmaceuticals Inc. Active agent delivery systems and methods for protecting and administering active agents
US6531617B2 (en) 2000-10-24 2003-03-11 Merck & Co., Inc. Process for preparing hydroxychomanones and cis-aminochromanols
ATE526339T1 (de) 2001-01-22 2011-10-15 Merck Sharp & Dohme Nukleosidderivate als inhibitoren der rna- abhängigen viralen rna-polymerase
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
US20060094006A1 (en) * 2002-05-01 2006-05-04 Genoveffa Franchini Immunotherapy regimens in hiv-infected patients
CN100475819C (zh) * 2002-05-16 2009-04-08 泰博特克药品有限公司 一种拟多晶型hiv蛋白酶抑制剂
US7115652B2 (en) * 2002-06-17 2006-10-03 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
CA2489095A1 (en) * 2002-06-17 2003-12-24 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
WO2005123087A2 (en) 2004-06-15 2005-12-29 Merck & Co., Inc. C-purine nucleoside analogs as inhibitors of rna-dependent rna viral polymerase
MX2007000481A (es) * 2004-07-14 2007-03-29 Ptc Therapeutics Inc Metodos para tratar hepatitis c.
US7781478B2 (en) * 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7868037B2 (en) * 2004-07-14 2011-01-11 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7772271B2 (en) * 2004-07-14 2010-08-10 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7645881B2 (en) * 2004-07-22 2010-01-12 Ptc Therapeutics, Inc. Methods for treating hepatitis C
EP2258376B1 (en) 2004-07-27 2019-02-27 Gilead Sciences, Inc. Phosphonate analogs of HIV inhibitor compounds
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
WO2007021886A2 (en) * 2005-08-10 2007-02-22 Oklahoma Medical Research Foundation Truncated memapsin 2 for use for treating alzheimer's disease
GB2443591B (en) * 2005-09-07 2010-04-28 Secr Defence 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
AU2007342367B2 (en) 2007-01-05 2012-12-06 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection
KR101518079B1 (ko) 2007-03-12 2015-05-06 넥타르 테라퓨틱스 올리고머-프로테아제 억제제 컨주게이트
GB0709791D0 (en) * 2007-05-22 2007-06-27 Angeletti P Ist Richerche Bio Antiviral agents
NZ582086A (en) * 2007-06-29 2012-07-27 Gilead Sciences Inc Therapeutic compositions and the use thereof
CN101743004A (zh) * 2007-06-29 2010-06-16 吉里德科学公司 治疗用组合物及其用途
GB0718575D0 (en) * 2007-09-24 2007-10-31 Angeletti P Ist Richerche Bio Nucleoside derivatives as inhibitors of viral polymerases
US20100093811A1 (en) * 2007-09-25 2010-04-15 Coburn Craig A Hiv protease inhibitors
GB0720503D0 (en) * 2007-10-22 2007-11-28 Angeletti P Ist Richerche Bio New compound
EP2262538B1 (en) * 2008-03-12 2014-12-10 Nektar Therapeutics Oligomer-amino acid conjugate
ES2467108T3 (es) 2008-12-09 2014-06-11 Gilead Sciences, Inc. Moduladores de receptores tipo toll
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
US8497383B2 (en) 2009-05-27 2013-07-30 Merck Sharp & Dohme Corp. HIV protease inhibitors
US20120108501A1 (en) 2009-06-12 2012-05-03 Nektar Therapeutics Protease Inhibitors
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
US20130052221A1 (en) 2010-02-26 2013-02-28 The Govt. of the U.S, as represented by The Sec. of The Dept. of Health and Human Services Dna-protein vaccination protocols
MX2012013628A (es) 2010-06-04 2012-12-17 Bristol Myers Squibb Co Amidas c-28 de derivados del acido betulinico c-3 modificados como inhibidores de la maduracion del virus de inmunodeficiencia humana (vih).
WO2011153315A1 (en) 2010-06-04 2011-12-08 Bristol-Myers Squibb Company Modified c-3 betulinic acid derivatives as hiv maturation inhibitors
EP2601174B1 (en) 2010-08-06 2014-11-26 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
ES2585396T3 (es) 2010-12-02 2016-10-05 VIIV Healthcare UK (No.5) Limited Alquilamidas como inhibidores de la unión del VIH
HRP20151212T1 (hr) 2011-01-31 2015-12-04 Bristol-Myers Squibb Company C-28 AMINI C-3 MODIFICIRANIH DERIVATA BETULINSKE KISELINE KAO INHIBITORI SAZRIJEVANJA HIV-a P
MY162186A (en) 2011-01-31 2017-05-31 Viiv Healthcare Uk (No 4) Ltd C-17 and c-3 modified triterpenoids with hiv maturation inhibitory activity
US8685982B2 (en) 2011-04-12 2014-04-01 Bristol-Myers Squibb Company 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
WO2013033059A1 (en) 2011-08-29 2013-03-07 Bristol-Myers Squibb Company Spiro bicyclic diamine derivatives as hiv attachment inhibitors
CN103814042B (zh) 2011-09-21 2015-08-19 百时美施贵宝公司 具有抗病毒活性的桦木酸衍生物
US9133157B2 (en) 2011-10-26 2015-09-15 Merck Canada Inc. HIV protease inhibitors
US8906889B2 (en) 2012-02-15 2014-12-09 Bristol-Myers Squibb Company C-3 cycloalkenyl triterpenoids with HIV maturation inhibitory activity
WO2013138436A1 (en) 2012-03-14 2013-09-19 Bristol-Myers Squibb Company Cyclolic 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
WO2014025854A1 (en) 2012-08-09 2014-02-13 Bristol-Myers Squibb Company Piperidine amide derivatives as hiv attachment inhibitors
ES2616432T3 (es) 2012-08-09 2017-06-13 VIIV Healthcare UK (No.5) Limited Derivados de alquenos tricíclicos como inhibidores de la unión del VIH
EP2895482B1 (en) 2012-09-11 2016-10-19 Merck Sharp & Dohme Corp. Hiv protease inhibitors
WO2014123889A1 (en) 2013-02-06 2014-08-14 Bristol-Myers Squibb Company C-19 modified triterpenoids with hiv maturation inhibitory activity
US9249180B2 (en) 2013-02-25 2016-02-02 Bristol-Myers Squibb Company C-3 alkyl and alkenyl modified betulinic acid derivatives
WO2015013835A1 (en) 2013-07-31 2015-02-05 Merck Sharp & Dohme Corp. Piperazine derivatives as hiv protease inhibitors
WO2015095276A1 (en) 2013-12-19 2015-06-25 Merck Sharp & Dohme Corp. Hiv protease inhibitors
WO2015095265A1 (en) 2013-12-19 2015-06-25 Merck Sharp & Dohme Corp. Hiv protease inhibitors
DE102014202609B4 (de) 2014-02-13 2020-06-04 tooz technologies GmbH Aminkatalysierte Thiolhärtung von Epoxidharzen
EP3113780B1 (en) 2014-03-06 2019-08-14 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
NZ724644A (en) 2014-04-11 2023-07-28 Viiv Healthcare Uk No 4 Ltd 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.
PL3166607T3 (pl) 2014-07-11 2023-02-20 Gilead Sciences, Inc. Modulatory receptorów toll-podobnych do leczenia hiv
WO2016069955A1 (en) 2014-10-29 2016-05-06 Wisconsin Alumni Research Foundation Boronic acid inhibitors of hiv protease
JP2017533934A (ja) 2014-11-14 2017-11-16 ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド C17アリール置換ベツリン酸類似体
WO2016077561A1 (en) 2014-11-14 2016-05-19 Bristol-Myers Squibb Company Oxolupene derivatives
WO2016168447A1 (en) 2015-04-14 2016-10-20 VIIV HEALTHCARE (No.4) LIMITED Methods of producing an hiv maturation inhibitor
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
EP0486478A3 (en) * 1984-08-06 1992-08-12 The Upjohn Company Renin-inhibiting peptides
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
IE902446A1 (en) * 1989-07-26 1991-02-13 Abbott Lab Peptidyl aminodiol renin inhibitors
US5063208A (en) * 1989-07-26 1991-11-05 Abbott Laboratories Peptidyl aminodiol renin inhibitors
IL95380A0 (en) * 1989-09-05 1991-06-30 Abbott Lab Peptidyl difluorodiol renin inhibitors
GB8927913D0 (en) * 1989-12-11 1990-02-14 Hoffmann La Roche Amino acid derivatives
GB8927915D0 (en) * 1989-12-11 1990-02-14 Hoffmann La Roche Novel alcohols
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
IE20010533A1 (en) * 1990-11-20 2003-03-05 Abbott Lab Intermediates for preparing 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
CA2104602A1 (en) * 1991-02-22 1992-08-23 Carl N. Hodge Substituted .alpha.-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
EP0528661A3 (en) * 1991-08-16 1993-06-02 Merck & Co. Inc. Hiv protease inhibitors with n-terminal polyether substituents
WO1993008184A1 (en) * 1991-10-23 1993-04-29 Merck & Co., Inc. Hiv protease inhibitors
US5413999A (en) * 1991-11-08 1995-05-09 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
SG52731A1 (en) * 1991-11-08 1998-09-28 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
DE69304393T2 (de) * 1992-04-01 1997-03-20 Searle & Co 2- und 3-Amino und Azidoderivate von 1,5-Iminozuckern als antivirale Arzneimittel
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
US5413999A (en) 1995-05-09
IL109503A0 (en) 1994-08-26
CA2161334A1 (en) 1994-11-24
HUT73135A (en) 1996-06-28
CN1126469A (zh) 1996-07-10
PL311635A1 (en) 1996-03-04
SK136395A3 (en) 1996-06-05
BR9406576A (pt) 1996-01-30
US5527799A (en) 1996-06-18
FI955315L (fi) 1995-11-06
EP0696277A1 (en) 1996-02-14
FI955315A7 (fi) 1995-11-06
TW256830B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 1995-09-11
NO954427D0 (no) 1995-11-06
HU9503170D0 (en) 1996-01-29
WO1994026717A1 (en) 1994-11-24
AU676563B2 (en) 1997-03-13
AU6669294A (en) 1994-12-12
FI955315A0 (fi) 1995-11-06
NO954427L (no) 1996-01-08
US5668132A (en) 1997-09-16
JPH08509980A (ja) 1996-10-22
BG100114A (bg) 1996-04-30
ZA943104B (en) 1995-11-06
CZ290095A3 (en) 1996-05-15
MX9403380A (es) 1995-01-31
CN1176250A (zh) 1998-03-18

Similar Documents

Publication Publication Date Title
HRP940286A2 (en) Hiv proteaze inhibitors useful for the treatment of aids
EP0617968B1 (en) HIV protease inhibitors in pharmaceutical combinations for the treatment of AIDS
EP0541168B1 (en) HIV protease inhibitors useful for the treatment of aids
EP0766674B1 (en) New hiv protease inhibitors
HK1006060B (en) Hiv protease inhibitors useful for the treatment of aids
CZ158696A3 (en) Hiv-protease inhibitors and pharmaceutical compositions containing thereof
US5650412A (en) HIV protease inhibitors useful for the treatment of AIDS
GB2288801A (en) HIV protease inhibitors useful for the treatment of aids
AU711713B2 (en) HIV protease inhibitors useful for the treatment of AIDS
US5811462A (en) HIV Protease inhibitors useful for the treatment of AIDS
US5717097A (en) HIV protease inhibitors useful for the treatment of AIDS
HK1009248B (en) Hiv protease inhibitors in pharmaceutical combinations for the treatment of aids
RU2171254C2 (ru) Способ получения производных пиперазинилпентанамида и производное пиперазинилпентанамида

Legal Events

Date Code Title Description
A1OB Publication of a patent application
AIPI Request for the grant of a patent on the basis of a substantive examination of a patent application
OBST Application withdrawn