FI955315A - HIV:n proteaasin inhibiittoreita, jotka ovat käyttökelpoisia AIDS'n hoitoon - Google Patents

HIV:n proteaasin inhibiittoreita, jotka ovat käyttökelpoisia AIDS'n hoitoon Download PDF

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Publication number
FI955315A
FI955315A FI955315A FI955315A FI955315A FI 955315 A FI955315 A FI 955315A FI 955315 A FI955315 A FI 955315A FI 955315 A FI955315 A FI 955315A FI 955315 A FI955315 A FI 955315A
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Finland
Prior art keywords
aids
inhibitors
useful
treatment
hiv protease
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FI955315A
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English (en)
Swedish (sv)
Other versions
FI955315A0 (fi
Inventor
Joseph P Vacca
Bruce D Dorsey
James P Guare
M Katharine Holloway
Randall W Hungate
Rhonda B Levin
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Merck & Co Inc
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Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of FI955315A publication Critical patent/FI955315A/fi
Publication of FI955315A0 publication Critical patent/FI955315A0/fi

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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
FI955315A 1993-05-07 1995-11-06 HIV:n proteaasin inhibiittoreita, jotka ovat käyttökelpoisia AIDS'n hoitoon FI955315A0 (fi)

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 (2)

Publication Number Publication Date
FI955315A true FI955315A (fi) 1995-11-06
FI955315A0 FI955315A0 (fi) 1995-11-06

Family

ID=22020419

Family Applications (1)

Application Number Title Priority Date Filing Date
FI955315A FI955315A0 (fi) 1993-05-07 1995-11-06 HIV:n proteaasin inhibiittoreita, jotka ovat käyttökelpoisia AIDS'n hoitoon

Country Status (20)

Country Link
US (3) US5413999A (fi)
EP (1) EP0696277A1 (fi)
JP (1) JPH08509980A (fi)
CN (2) CN1126469A (fi)
AU (1) AU676563B2 (fi)
BG (1) BG100114A (fi)
BR (1) BR9406576A (fi)
CA (1) CA2161334A1 (fi)
CZ (1) CZ290095A3 (fi)
FI (1) FI955315A0 (fi)
HR (1) HRP940286A2 (fi)
HU (1) HUT73135A (fi)
IL (1) IL109503A0 (fi)
MX (1) MX9403380A (fi)
NO (1) NO954427L (fi)
PL (1) PL311635A1 (fi)
SK (1) SK136395A3 (fi)
TW (1) TW256830B (fi)
WO (1) WO1994026717A1 (fi)
ZA (1) ZA943104B (fi)

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
US5843946A (en) 1992-08-25 1998-12-01 G.D. Searle & Co. α-and β-amino acid 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
ES2174921T3 (es) * 1993-12-15 2002-11-16 Merck & Co Inc Inhibidores de la proteasa del vih.
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
US20030207813A1 (en) * 1996-12-09 2003-11-06 G.D. Searle Retroviral protease inhibitor combinations
UA49803C2 (uk) * 1994-06-03 2002-10-15 Дж.Д. Сьорль Енд Ко Спосіб лікування ретровірусних інфекцій
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
DK0710652T3 (da) * 1994-11-04 1998-09-28 Yamakawa Chemical Ind Fremgangsmåde til fremstilling af optisk aktive piperazinderivater og mellemprodukter til fremstillingen
WO1996022981A1 (de) * 1995-01-23 1996-08-01 Lonza Ag 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
CA2279673A1 (en) * 1995-12-15 1997-06-16 Enzo Therapeutics, Inc. Property effecting and/or property exhibiting constructs for the expression of non-native nucleic acids 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
EP0988042B1 (en) 1997-04-15 2008-01-09 Advanced Viral Research Corp. Combination of product r and an antiviral agent in the therapy of hiv infections
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
WO1999065897A1 (en) 1998-06-19 1999-12-23 Chiron Corporation Inhibitors of glycogen synthase kinase 3
WO1999066936A1 (en) * 1998-06-24 1999-12-29 Emory University Use of 3'-azido-2',3'-dideoxyuridine in combination with further anti-hiv drugs for the manufacture of a medicament for the treatment of hiv
WO2000002862A1 (en) 1998-07-08 2000-01-20 G.D. Searle & Co. 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
EP1146904A4 (en) * 1999-02-03 2004-09-15 Franco Lori USE OF HYDROXY URINE AND AN INHIBITOR OF REVERSE TRANSCRIPTASE FOR INDUCING AUTOVACCATION BY AUTOLOGICAL HIV
DK1183026T3 (da) * 1999-06-04 2006-11-06 Abbott Lab Forbedrede farmaceutiske formuleringer omfattende ritonavir
CA2374610A1 (en) * 1999-06-28 2001-01-04 Jordan J. N. Tang 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
JP2003504383A (ja) * 1999-07-20 2003-02-04 メルク エンド カムパニー インコーポレーテッド アルファ−ヒドロキシ−ガンマ−［［（炭素環式−又はヘテロ環式−置換）アミノ］カルボニル］アルカンアミド誘導体及びこれらの使用
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).
US6642237B1 (en) 1999-11-24 2003-11-04 Merck & Co., Inc. Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof
ES2304990T3 (es) 2000-01-19 2008-11-01 Abbott Laboratories Formulaciones farmaceuticas de inhibidores de la proteasa del vih mejoradas.
US6476034B2 (en) 2000-02-22 2002-11-05 Bristol-Myers Squibb Company Antiviral azaindole derivatives
AU2001259291B2 (en) * 2000-04-28 2006-11-23 Aventis Pasteur Limited Improved immunogenicity using a combination of DNA and vaccinia virus vector vaccines
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
HUP0400726A3 (en) 2001-01-22 2007-05-29 Merck & Co Inc Nucleoside derivatives as inhibitors of rna-dependent rna viral 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
ATE370948T1 (de) * 2002-01-17 2007-09-15 Merck & Co Inc Hydroxynaphthyridinoncarbonsäureamide, die sich als inhibitoren der hiv-integrase eignen
JP4625637B2 (ja) 2002-02-22 2011-02-02 シャイア エルエルシー 活性物質送達系及び活性物質を保護し投与する方法
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
AU2003271740B2 (en) * 2002-05-16 2010-05-13 Janssen R&D Ireland Pseudopolymorphic forms of a HIV protease inhibitor
US7115652B2 (en) * 2002-06-17 2006-10-03 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
JP2005529953A (ja) * 2002-06-17 2005-10-06 サネシス ファーマシューティカルズ， インコーポレイテッド アスパルチルプロテアーゼインヒビター
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
CA2568379A1 (en) 2004-06-15 2005-12-29 Merck & Co., Inc. C-purine nucleoside analogs as inhibitors of rna-dependent rna viral polymerase
US7772271B2 (en) * 2004-07-14 2010-08-10 Ptc Therapeutics, Inc. Methods for treating hepatitis C
EP1771169A1 (en) * 2004-07-14 2007-04-11 PTC Therapeutics, Inc. Methods for treating hepatitis c
US7781478B2 (en) * 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7868037B2 (en) * 2004-07-14 2011-01-11 Ptc Therapeutics, Inc. Methods for treating hepatitis C
AU2005275182A1 (en) * 2004-07-22 2006-02-23 Ptc Therapeutics, Inc. Thienopyridines for treating Hepatitis C
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
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
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
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
WO2008012538A2 (en) 2006-07-25 2008-01-31 The Secretary Of State For Defence Live vaccine strains of francisella
JP2010515680A (ja) 2007-01-05 2010-05-13 メルク・シャープ・エンド・ドーム・コーポレイション Ｒｎａ依存性ｒｎａウイルス感染症の治療用としてのヌクレオシドアリールホスホロアミデート
WO2008112289A2 (en) 2007-03-12 2008-09-18 Nektar Therapeutics Oligomer-protease inhibitor conjugates
GB0709791D0 (en) * 2007-05-22 2007-06-27 Angeletti P Ist Richerche Bio Antiviral agents
CA2691736A1 (en) * 2007-06-29 2009-01-08 Gilead Sciences, Inc. Combination of 6-(3-chloro-2-fluorobenzyl)-1-[(2s)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid and lopinavir for the treatment of a viral infection in a human
TW200914011A (en) * 2007-06-29 2009-04-01 Gilead Sciences Inc Therapeutic compositions and methods
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
UY32306A (es) 2008-12-09 2010-07-30 Gilead Sciences Inc Derivados de pteridinona y pirimidinodiazepinona y composiciones farmacéuticas que modulan en forma selectiva los receptores tipo toll, métodos y usos
GB0900455D0 (en) 2009-01-13 2009-02-11 Secr Defence Vaccine
GB0901423D0 (en) 2009-01-29 2009-03-11 Secr Defence Treatment
GB0901411D0 (en) 2009-01-29 2009-03-11 Secr Defence Treatment
GB0906234D0 (en) 2009-04-14 2009-05-20 Secr Defence Vaccine
EP2435037B1 (en) 2009-05-27 2014-11-12 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
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
PT2576586E (pt) 2010-06-04 2015-10-23 Bristol Myers Squibb Co Amidas c-28 de derivados de ácido betulínico c-3 modificadas como inibidores de maturação de hiv
US8754068B2 (en) 2010-06-04 2014-06-17 Bristol-Myers Squibb Company Modified C-3 betulinic acid derivatives as HIV maturation inhibitors
US8450361B2 (en) 2010-08-06 2013-05-28 Bristol-Myers Squibb Company Substituted indole and azaindole oxoacetyl piperazinamide derivatives
EP2632895B1 (en) 2010-10-28 2018-10-03 Merck Canada Inc. Hiv protease inhibitors
EP2646439B1 (en) 2010-12-02 2016-05-25 Bristol-Myers Squibb Company Alkyl amides as hiv attachment inhibitors
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
EP2670764B1 (en) 2011-01-31 2015-09-02 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
ES2616268T3 (es) 2011-08-29 2017-06-12 VIIV Healthcare UK (No.5) Limited Derivados condensados de diamina bicíclica como inhibidores de la unión de VIH
ES2609579T3 (es) 2011-08-29 2017-04-21 VIIV Healthcare UK (No.5) Limited Derivados espiro de diamina bicíclica como inhibidores de la unión del VIH
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
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
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
US9505752B2 (en) 2012-08-09 2016-11-29 Viiv Healthcare Uk (No. 5) Limited Piperidine amide derivatives as HIV attachment inhibitors
US9655888B2 (en) 2012-08-09 2017-05-23 VIIV Healthcare UK (No.5) Limited Tricyclic alkene derivatives as HIV attachment inhibitors
US9315475B2 (en) 2012-09-11 2016-04-19 Merck Sharp & Dohme Corp. HIV protease inhibitors
JP6186010B2 (ja) 2013-02-06 2017-08-23 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｈｉｖ成熟阻害活性を有するｃ−１９修飾トリテルペノイド類
EA027861B1 (ru) 2013-02-25 2017-09-29 Бристол-Майерс Сквибб Компани C-3 алкил- и алкенилмодифицированные производные бетулиновой кислоты или их фармацевтические соли, противовирусная фармацевтическая композиция и фармацевтическая композиция для лечения вич на их основе
WO2015013835A1 (en) 2013-07-31 2015-02-05 Merck Sharp & Dohme Corp. Piperazine derivatives as hiv protease inhibitors
US9737545B2 (en) 2013-12-19 2017-08-22 Merck Sharp & Dohme Corp. HIV protease inhibitors
WO2015095276A1 (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
US9994587B2 (en) 2014-03-06 2018-06-12 Merck Sharp & Dohme Corp. HIV protease inhibitors
EP3116862B1 (en) 2014-03-10 2019-04-17 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.
TWI806081B (zh) 2014-07-11 2023-06-21 美商基利科學股份有限公司 用於治療HIV之toll樣受體調節劑
EP3212196A4 (en) 2014-10-29 2018-07-11 Wisconsin Alumni Research Foundation Boronic acid inhibitors of hiv protease
CA2967684A1 (en) 2014-11-14 2016-05-19 VIIV Healthcare UK (No.5) Limited C17-aryl substituted betulinic acid analogs
US9969767B2 (en) 2014-11-14 2018-05-15 VIIV Healthcare UK (No.5) Limited Oxolupene derivatives
AU2016248235A1 (en) 2015-04-14 2017-10-19 Viiv Healthcare Uk (No 4) Limited Crystalline forms of modified triterpenoid hydrochloride salts with HIV maturation inhibitor activity
EP4276106A3 (en) 2015-05-13 2024-01-24 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
WO2024011033A1 (en) 2022-07-07 2024-01-11 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 (32)

* 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
CA1309555C (en) * 1986-02-27 1992-10-27 Suvit Thaisrivongs Inhibiting peptides having a dihydroxyethylene isostere transitionstate insert
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
EP0357332A3 (en) * 1988-08-24 1991-07-31 Merck & Co. Inc. Renin inhibitors useful for the treatment of aids by inhibition of hiv protease
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
ZA921279B (en) * 1991-02-22 1993-08-23 Du Pont Merck Pharma 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
CA2076204A1 (en) * 1991-08-16 1993-02-17 Samuel L. Graham 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
ES2095032T3 (es) * 1992-04-01 1997-02-01 Searle & Co Derivados 2- y 3-amino y azido de 1,5-iminoazucares como compuestos antivirales.
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

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