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MXPA03010538A - Nuevas formulaciones que inhiben la proteasa aspartilo. - Google Patents

Nuevas formulaciones que inhiben la proteasa aspartilo.

Info

Publication number
MXPA03010538A
MXPA03010538A MXPA03010538A MXPA03010538A MXPA03010538A MX PA03010538 A MXPA03010538 A MX PA03010538A MX PA03010538 A MXPA03010538 A MX PA03010538A MX PA03010538 A MXPA03010538 A MX PA03010538A MX PA03010538 A MXPA03010538 A MX PA03010538A
Authority
MX
Mexico
Prior art keywords
hiv
present
compounds
relates
protease
Prior art date
Application number
MXPA03010538A
Other languages
English (en)
Inventor
Roger D Tung
Mark A Murcko
Govinda Rao Bhisetti
Original Assignee
Vertex Pharma
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 Vertex Pharma filed Critical Vertex Pharma
Publication of MXPA03010538A publication Critical patent/MXPA03010538A/es

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    • 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
    • C07D207/18—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—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 one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
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    • 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
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    • 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
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    • A61P31/18—Antivirals for RNA viruses for HIV
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    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
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    • C07C311/12—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
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    • C07C311/18—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
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    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
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    • C07C311/39—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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  • Pyrrole Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Indole Compounds (AREA)
  • Peptides Or Proteins (AREA)

Abstract

La presente invención se refiere a una nueva clase de sulfonamidas, las cuales son inhibidoras de las proteasa aspartilo, en una de sus modalidades, la presente invención se refiere a una nueva clase de inhibidores de la proteasa aspartilo de VIH caracterizados por sus características estructurales especificas y fisicoquímicas La presente invención también se refiere a composiciones farmaceúricas que comprenden estos compuestos. Los compuestos y las composiciones farmacéuticas de la presente invención son particularmente bien adecuados para la inhibición de la actividad de las proteasas VIH-1 y VIH-2 y consecuentemente, pueden ser usados de manera provechosa como agentes antivirales contra los viruses VIH-1 y VIH-2. Esta invención también se refiere a los métodos para inhibir la actividad de la proteasa aspartilo VIH usando los compuestos de la presente invención y a los metodos para proteger los compuestos para la actividad anti- VIH.
MXPA03010538A 1992-09-08 2003-11-17 Nuevas formulaciones que inhiben la proteasa aspartilo. MXPA03010538A (es)

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Families Citing this family (307)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040122000A1 (en) 1981-01-07 2004-06-24 Vertex Pharmaceuticals Incorporated. Inhibitors of aspartyl protease
US6878728B1 (en) 1999-06-11 2005-04-12 Vertex Pharmaceutical Incorporated Inhibitors of aspartyl protease
US5962490A (en) 1987-09-25 1999-10-05 Texas Biotechnology Corporation Thienyl-, furyl- and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin
US5736509A (en) * 1990-12-14 1998-04-07 Texas Biotechnology Corporation Cyclic peptide surface feature mimics of endothelin
ATE199109T1 (de) * 1992-03-27 2001-02-15 Akiko Itai Verfahren zur analyse der struktur von stabilen zusammengesetzten biopolymerligandmolekuelen
US6046190A (en) * 1992-08-25 2000-04-04 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
DK0656887T3 (da) 1992-08-25 1999-07-05 Searle & Co Hydroxyethylaminosulfonamider til anvendelse som inhibitorer af retrovirale proteaser
US6743929B1 (en) 1992-08-25 2004-06-01 G. D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US7141609B2 (en) 1992-08-25 2006-11-28 G.D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US5968942A (en) 1992-08-25 1999-10-19 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US5783701A (en) * 1992-09-08 1998-07-21 Vertex Pharmaceuticals, Incorporated Sulfonamide inhibitors of aspartyl protease
IS2334B (is) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
DK0666843T3 (da) * 1992-10-30 2000-03-20 Searle & Co Sulfonylalkanoylaminohydroxyethylaminosulfaminsyrer, der kan anvendes som inhibitorer af retrovirale proteaser
CA2142997A1 (en) 1992-10-30 1994-05-11 Michael L. Vazquez Hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors
US5484926A (en) * 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
US5846993A (en) * 1992-12-22 1998-12-08 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
US6541498B2 (en) 1993-05-20 2003-04-01 Texas Biotechnology Benzenesulfonamides and the use thereof to modulate the activity of endothelin
US6376523B1 (en) 1994-05-20 2002-04-23 Texas Biotechnology Corporation Benzenesulfonamides and the use thereof to modulate the activity of endothelin
US6342610B2 (en) 1993-05-20 2002-01-29 Texas Biotechnology Corp. N-aryl thienyl-, furyl-, and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin
US6030991A (en) * 1993-05-20 2000-02-29 Texas Biotechnology Corp. Benzenesulfonamides and the use thereof to modulate the activity of endothelin
US6613804B2 (en) 1993-05-20 2003-09-02 Encysive Pharmaceuticals, Inc. Biphenylsulfonamides and derivatives thereof that modulate the activity of endothelin
US5798355A (en) * 1995-06-07 1998-08-25 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity
US5846981A (en) * 1993-05-28 1998-12-08 Gpi Nil Holdings Inc. Inhibitors of rotamase enzyme activity
US7831470B1 (en) * 1996-09-04 2010-11-09 Walker Digital, Llc Method and apparatus for facilitating electronic commerce through providing cross-benefits during a transaction
US5750648A (en) * 1993-08-20 1998-05-12 G.D. Searle & Co. Retroviral protease inhibitors and combinations thereof
IL110752A (en) * 1993-09-13 2000-07-26 Abbott Lab Liquid semi-solid or solid pharmaceutical composition for an HIV protease inhibitor
US5559158A (en) * 1993-10-01 1996-09-24 Abbott Laboratories Pharmaceutical composition
US5602119A (en) * 1993-10-29 1997-02-11 Vazquez; Michael L. Succinoylamino hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors
US5527829A (en) * 1994-05-23 1996-06-18 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
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
AU4700896A (en) 1995-01-20 1996-08-07 G.D. Searle & Co. Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
US5831117A (en) 1995-01-20 1998-11-03 G. D. Searle & Co. Method of preparing retroviral protease inhibitor intermediates
US5756533A (en) * 1995-03-10 1998-05-26 G.D. Searle & Co. Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US6140505A (en) 1995-03-10 2000-10-31 G. D. Searle & Co. Synthesis of benzo fused heterocyclic sulfonyl chlorides
EP1188766A1 (en) 1995-03-10 2002-03-20 G.D. Searle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US5776971A (en) 1995-03-10 1998-07-07 G.D. Searle & Co. Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US7339078B2 (en) * 1995-03-10 2008-03-04 G.D. Searle Llc Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US6861539B1 (en) * 1995-03-10 2005-03-01 G. D. Searle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US6407134B1 (en) 1995-03-10 2002-06-18 G. D. Searle & Co. Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
BR9607625A (pt) * 1995-03-10 1999-06-15 Searle & Co Inibidores de protease retroviral sulfonamida hidroxietilamino de aminoácido heterociclocarbonila
US6143788A (en) * 1995-03-10 2000-11-07 G.D. Searle & Co. Bis-amino acid hydroxyethlamino sulfonamide retroviral protease inhibitors
US6150556A (en) * 1995-03-10 2000-11-21 G. D. Dearle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US5691372A (en) 1995-04-19 1997-11-25 Vertex Pharmaceuticals Incorporated Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease
US5859031A (en) * 1995-06-07 1999-01-12 Gpi Nil Holdings, Inc. Small molecule inhibitors of rotamase enzyme activity
US5696135A (en) * 1995-06-07 1997-12-09 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity effective at stimulating neuronal growth
US6037157A (en) * 1995-06-29 2000-03-14 Abbott Laboratories Method for improving pharmacokinetics
US5942253A (en) 1995-10-12 1999-08-24 Immunex Corporation Prolonged release of GM-CSF
US5801197A (en) * 1995-10-31 1998-09-01 Gpi Nil Holdings, Inc. Rotamase enzyme activity inhibitors
DE69619067T2 (de) 1995-11-17 2002-10-02 Ajinomoto Co., Inc. Verfahren zur Herstellung von 3-Amino-2-oxo-1-Halogenpropan-Derivaten
US5646180A (en) * 1995-12-05 1997-07-08 Vertex Pharmaceuticals Incorporated Treatment of the CNS effects of HIV
US5914332A (en) 1995-12-13 1999-06-22 Abbott Laboratories Retroviral protease inhibiting compounds
US5977117A (en) 1996-01-05 1999-11-02 Texas Biotechnology Corporation Substituted phenyl compounds and derivatives thereof that modulate the activity of endothelin
EE04093B1 (et) * 1996-03-22 2003-08-15 Glaxo Group Limited HIV proteaasi inhibiitorit VX 478 ja vees lahustuva vitamiin E derivaati vitamiin E-TPGSi sisaldavad preparaadid
MY126358A (en) * 1996-03-22 2006-09-29 Glaxo Group Ltd Compositions comprising vx478 and a water soluble tocopherol derivative such as vitamin e-tpgs
US6730679B1 (en) 1996-03-22 2004-05-04 Smithkline Beecham Corporation Pharmaceutical formulations
US5958905A (en) * 1996-03-26 1999-09-28 Texas Biotechnology Corporation Phosphoramidates, phosphinic amides and related compounds and the use thereof to modulate the activity of endothelin
US5804585A (en) 1996-04-15 1998-09-08 Texas Biotechnology Corporation Thieno-pyridine sulfonamides derivatives thereof and related compounds that modulate the activity of endothelin
EA001457B1 (ru) * 1996-06-25 2001-04-23 Глаксо Груп Лимитед Комбинации, содержащие vx478, зидовудин и/или 1592u89, для применения при лечении вич
CA2258956A1 (en) * 1996-06-25 1997-12-31 Glaxo Group Limited Combinations comprising vx478, zidovudine, ftc and/or 3tc for use in the treatment of hiv
US5925759A (en) * 1996-09-05 1999-07-20 Agouron Pharmaceuticals, Inc. Methods of making HIV-protease inhibitors and intermediates for making HIV-protease inhibitors
US5705647A (en) * 1996-09-05 1998-01-06 Agouron Pharmaceuticals, Inc. Intermediates for making HIV-protease inhibitors
US5962725A (en) 1996-09-05 1999-10-05 Agouron Pharmaceuticals, Inc. Intermediate compounds useful for making HIV protease inhibitors such as nelfinavir
US5786378A (en) * 1996-09-25 1998-07-28 Gpi Nil Holdings, Inc. Heterocyclic thioesters
US5801187A (en) * 1996-09-25 1998-09-01 Gpi-Nil Holdings, Inc. Heterocyclic esters and amides
US6218424B1 (en) 1996-09-25 2001-04-17 Gpi Nil Holdings, Inc. Heterocyclic ketone and thioester compounds and uses
IN183408B (es) * 1996-11-20 1999-12-25 Kuraray Co
ZA9710071B (en) * 1996-11-21 1998-05-25 Abbott Lab Pharmaceutical composition.
US6232333B1 (en) 1996-11-21 2001-05-15 Abbott Laboratories Pharmaceutical composition
NZ336386A (en) * 1996-12-31 2001-09-28 Guilford Pharm Inc An urea or carbamate derivative of heterocyclic thioester useful for effecting neuronal activity
EA002593B1 (ru) 1996-12-31 2002-06-27 Гилфорд Фармасьютикалз Инк. N-связанные сульфонамиды гетероциклических тиоэфиров
US5935989A (en) 1996-12-31 1999-08-10 Gpi Nil Holdings Inc. N-linked ureas and carbamates of heterocyclic thioesters
US5874449A (en) * 1996-12-31 1999-02-23 Gpi Nil Holdings, Inc. N-linked sulfonamides of heterocyclic thioesters
US5721256A (en) * 1997-02-12 1998-02-24 Gpi Nil Holdings, Inc. Method of using neurotrophic sulfonamide compounds
US5846979A (en) 1997-02-28 1998-12-08 Gpi Nil Holdings, Inc. N-oxides of heterocyclic esters, amides, thioesters, and ketones
US6001851A (en) * 1997-03-13 1999-12-14 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
SG100767A1 (en) 1997-04-28 2003-12-26 Texas Biotechnology Corp Sulfonamides for treatment of endothelin-mediated disorders
US5783705A (en) * 1997-04-28 1998-07-21 Texas Biotechnology Corporation Process of preparing alkali metal salys of hydrophobic sulfonamides
IL132630A0 (en) * 1997-05-08 2001-03-19 Smithkline Beecham Corp Protease inhibitors
US6274602B1 (en) 1998-06-03 2001-08-14 Gpi Nil Holdings, Inc. Heterocyclic thioester and ketone hair growth compositions and uses
US6271244B1 (en) 1998-06-03 2001-08-07 Gpi Nil Holdings, Inc. N-linked urea or carbamate of heterocyclic thioester hair growth compositions and uses
US20010049381A1 (en) 1997-06-04 2001-12-06 Gpl Nil Holdings, Inc., Pyrrolidine derivative hair growth compositions and uses
US6187784B1 (en) 1998-06-03 2001-02-13 Gpi Nil Holdings, Inc. Pipecolic acid derivative hair growth compositions and uses
US6187796B1 (en) 1998-06-03 2001-02-13 Gpi Nil Holdings, Inc. Sulfone hair growth compositions and uses
US5945441A (en) 1997-06-04 1999-08-31 Gpi Nil Holdings, Inc. Pyrrolidine carboxylate hair revitalizing agents
GB9712253D0 (en) * 1997-06-13 1997-08-13 Glaxo Group Ltd Antiviral compound
BR9810456A (pt) 1997-06-27 2001-09-25 Fujisawa Pharmaceutical Co Composto de sulfonamida, método para sua obtenção e seu uso farmacêutico
US6084107A (en) * 1997-09-05 2000-07-04 Agouron Pharmaceuticals, Inc. Intermediates for making HIV-protease inhibitors
US6576231B2 (en) * 1997-09-12 2003-06-10 Schering Ag Methods for treating HIV-Infected Patients by the Administration of GM-CSF and a protease inhibitor
US6180634B1 (en) * 1997-11-13 2001-01-30 Merck & Co., Inc. Combination therapy for the treatment of AIDS
BR9814484A (pt) * 1997-12-24 2000-10-10 Vertex Pharma "pró-drogas de inibidores de aspartil protease"
US6436989B1 (en) * 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
WO1999033795A1 (en) * 1997-12-24 1999-07-08 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
AU2010299A (en) * 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs os aspartyl protease inhibitors
GB9805898D0 (en) * 1998-03-20 1998-05-13 Glaxo Group Ltd Process for the sythesis of hiv protease inhibitors
US6251906B1 (en) 1998-05-15 2001-06-26 Abbott Laboratories Retroviral protease inhibiting compounds
US6172087B1 (en) 1998-06-03 2001-01-09 Gpi Nil Holding, Inc. N-oxide of heterocyclic ester, amide, thioester, or ketone hair growth compositions and uses
EP1085853A1 (en) 1998-06-03 2001-03-28 GPI NIL Holdings, Inc. Heterocyclic ester and amide hair growth compositions and uses
US6331537B1 (en) 1998-06-03 2001-12-18 Gpi Nil Holdings, Inc. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds
EP1084106A1 (en) 1998-06-03 2001-03-21 GPI NIL Holdings, Inc. N-linked sulfonamides of heterocyclic carboxylic acids or carboxylic acid isosteres
NZ508855A (en) * 1998-06-19 2003-10-31 Vertex Pharma Sulfonamide inhibitors of HIV aspartyl protease
PT1088098E (pt) 1998-06-23 2011-05-25 Univ Illinois Medicamento para tratar mam?feros infectados com hiv
AU4862799A (en) 1998-07-08 2000-02-01 G.D. Searle & Co. Retroviral protease inhibitors
US6713290B2 (en) 1998-07-24 2004-03-30 Samsung Fine Chemicals Co., Ltd. Process for preparing optically pure (S)-3-hydroxy-γ-butyrolactone
EP1100954B1 (en) 1998-07-24 2002-10-09 Samsung Fine Chemicals Co., Ltd. Continuous process for preparing optically pure (s)-3,4-dihydroxybutyric acid derivatives
US6384056B1 (en) 1998-08-14 2002-05-07 Gpi Nil Holdings, Inc. Heterocyclic thioesters or ketones for vision and memory disorders
US6337340B1 (en) 1998-08-14 2002-01-08 Gpi Nil Holdings, Inc. Carboxylic acids and isosteres of heterocyclic ring compounds having multiple heteroatoms for vision and memory disorders
US6335348B1 (en) 1998-08-14 2002-01-01 Gpi Nil Holdings, Inc. Nitrogen-containing linear and azepinyl/ compositions and uses for vision and memory disorders
US6506788B1 (en) 1998-08-14 2003-01-14 Gpi Nil Holdings, Inc. N-linked urea or carbamate of heterocyclic thioesters for vision and memory disorders
US6376517B1 (en) 1998-08-14 2002-04-23 Gpi Nil Holdings, Inc. Pipecolic acid derivatives for vision and memory disorders
US6333340B1 (en) 1998-08-14 2001-12-25 Gpi Nil Holdings, Inc. Small molecule sulfonamides for vision and memory disorders
US6399648B1 (en) 1998-08-14 2002-06-04 Gpi Nil Holdings, Inc. N-oxides of heterocyclic ester, amide, thioester, or ketone for vision and memory disorders
US6218423B1 (en) 1998-08-14 2001-04-17 Gpi Nil Holdings, Inc. Pyrrolidine derivatives for vision and memory disorders
US7338976B1 (en) 1998-08-14 2008-03-04 Gpi Nil Holdings, Inc. Heterocyclic esters or amides for vision and memory disorders
US6339101B1 (en) 1998-08-14 2002-01-15 Gpi Nil Holdings, Inc. N-linked sulfonamides of N-heterocyclic carboxylic acids or isosteres for vision and memory disorders
US6395758B1 (en) 1998-08-14 2002-05-28 Gpi Nil Holdings, Inc. Small molecule carbamates or ureas for vision and memory disorders
US6462072B1 (en) 1998-09-21 2002-10-08 Gpi Nil Holdings, Inc. Cyclic ester or amide derivatives
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
TNSN00027A1 (fr) 1999-02-12 2005-11-10 Vertex Pharma Inhibiteurs de l'aspartyle protease
DK1159278T3 (da) * 1999-02-12 2006-04-10 Vertex Pharma Inhibitorer af aspartylprotease
AR031520A1 (es) * 1999-06-11 2003-09-24 Vertex Pharma Un compuesto inhibidor de aspartilo proteasa, una composicion que lo comprende y un metodo para tratar un paciente con dicha composicion
GB9914821D0 (en) * 1999-06-24 1999-08-25 Glaxo Group Ltd Compounds
CZ300031B6 (cs) 1999-10-06 2009-01-14 Tibotec Pharmaceuticals Ltd. Hexahydrofuro[2,3-b]furan-3-yl-N-{3-[(1,3-benzodioxol-5-ylsulfonyl) (isobutyl)amino]-1-benzyl-2-hydroxypropyl}karbamát a farmaceutický prípravek s jeho obsahem
EP2314564A3 (en) 1999-12-23 2012-04-04 Ampac Fine Chemicals LLC Improved preparation of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride and other derivatives of 2-hydroxy-1,3-diamines
US6548706B2 (en) 1999-12-23 2003-04-15 Aerojet Fine Chemicals Llc Preparation of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl) -p-nitrobenzenesulfonylamide hydrochloride and other derivatives of 2-hydroxy-1,3-diamines
US6391919B1 (en) 2000-01-12 2002-05-21 Bristol-Myers Squibb Pharma Company Bis-amino acid sulfonamides containing substituted benzyl amines HIV protease inhibitors
ES2304990T3 (es) 2000-01-19 2008-11-01 Abbott Laboratories Formulaciones farmaceuticas de inhibidores de la proteasa del vih mejoradas.
PE20020276A1 (es) * 2000-06-30 2002-04-06 Elan Pharm Inc COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER
US6617310B2 (en) 2000-07-19 2003-09-09 Bristol-Myers Squibb Pharma Company Phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines
KR100870184B1 (ko) * 2001-02-14 2008-11-24 티보텍 파마슈티칼즈 리미티드 광범위 2-(치환된-아미노)-벤조티아졸 설폰아미드 ｈｉｖ프로티아제 억제제
US6756063B2 (en) 2001-03-29 2004-06-29 Zoltan Laboratories, Llc Methods and compositions for the treatment of human and animal cancers
BR0208796A (pt) 2001-04-09 2004-03-09 Tibotec Pharm Ltd Inibidores 2-(amino substituìdo)-benzoxazol sulfonamida hiv protease de amplo espectro
US6696494B2 (en) 2001-10-22 2004-02-24 Enanta Pharmaceuticals, Inc. α-hydroxyarylbutanamine inhibitors of aspartyl protease
AU2003202914A1 (en) * 2002-01-07 2003-07-24 Sequoia Pharmaceuticals Broad spectrum inhibitors
EP1490090A4 (en) 2002-02-22 2006-09-20 New River Pharmaceuticals Inc SYSTEMS FOR DELIVERING ACTIVE AGENTS AND METHODS FOR PROTECTING AND DELIVERING ACTIVE AGENTS
US7157489B2 (en) * 2002-03-12 2007-01-02 The Board Of Trustees Of The University Of Illinois HIV protease inhibitors
CN101074242A (zh) 2002-04-26 2007-11-21 吉里德科学公司 Hiv蛋白酶抑制剂化合物的膦酸酯类似物的细胞蓄积及这类化合物
US7462636B2 (en) * 2002-05-17 2008-12-09 Tibotec Pharmaceuticals Ltd Broadspectrum substituted benzisoxazole sulfonamide HIV protease inhibitors
US7132568B2 (en) * 2002-06-17 2006-11-07 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
US7115652B2 (en) * 2002-06-17 2006-10-03 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
KR100994759B1 (ko) * 2002-08-14 2010-11-16 티보텍 파마슈티컬즈 광역스펙트럼의 치환된 옥신돌 설폰아미드 ｈｉｖ프로테아제 저해제
UY27967A1 (es) * 2002-09-10 2004-05-31 Pfizer Acetil 2-hindroxi-1,3-diaminoalcanos
ES2535975T3 (es) * 2002-10-03 2015-05-19 Novaremed Ltd. Compuestos para su uso en el tratamiento de enfermedades autoinmunitarias, enfermedades inmunoalérgicas y rechazo de trasplantes de órganos o tejidos
US6713639B1 (en) 2002-10-28 2004-03-30 Council Of Scientific And Industrial Research Process for preparing enantiomerically pure (S)-3-hydroxy-gamma-butyrolactone
US7109217B2 (en) * 2002-11-12 2006-09-19 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
DOP2003000765A (es) * 2002-11-27 2004-05-31 Elan Fharmaceuticals Inc Ureas substituidas y carbamatos utiles para el tratamiento de la enfermedad de alzheimer (substituted ureas and carbamates useful in the treatment of alzheimer`s disease
US7427636B2 (en) * 2003-04-25 2008-09-23 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
CN101410120A (zh) * 2003-04-25 2009-04-15 吉里德科学公司 抗炎的膦酸酯化合物
US20050261237A1 (en) * 2003-04-25 2005-11-24 Boojamra Constantine G Nucleoside phosphonate analogs
CA2523083C (en) 2003-04-25 2014-07-08 Gilead Sciences, Inc. Antiviral phosphonate analogs
US7452901B2 (en) 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
US7432261B2 (en) * 2003-04-25 2008-10-07 Gilead Sciences, Inc. Anti-inflammatory phosphonate compounds
WO2004096285A2 (en) * 2003-04-25 2004-11-11 Gilead Sciences, Inc. Anti-infective phosphonate conjugates
WO2005002626A2 (en) * 2003-04-25 2005-01-13 Gilead Sciences, Inc. Therapeutic phosphonate compounds
US7470724B2 (en) * 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
US7407965B2 (en) * 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
US20090247488A1 (en) * 2003-04-25 2009-10-01 Carina Cannizzaro Anti-inflammatory phosphonate compounds
KR20060022647A (ko) 2003-04-25 2006-03-10 길리애드 사이언시즈, 인코포레이티드 키나아제 억제 포스포네이트 유사체
US8025899B2 (en) 2003-08-28 2011-09-27 Abbott Laboratories Solid pharmaceutical dosage form
US8377952B2 (en) 2003-08-28 2013-02-19 Abbott Laboratories Solid pharmaceutical dosage formulation
EP1671937A4 (en) * 2003-09-19 2007-08-08 Ube Industries METHOD FOR PRODUCING A NITRILE COMPOUND, CARBOXYLIC COMPOUND OR CARBOXYLATE COMPOUND
CN100432038C (zh) * 2003-09-19 2008-11-12 宇部兴产株式会社 腈化合物、羧酸化合物或羧酸酯化合物的制备方法
US7427624B2 (en) * 2003-10-24 2008-09-23 Gilead Sciences, Inc. Purine nucleoside phosphorylase inhibitory phosphonate compounds
US7432273B2 (en) * 2003-10-24 2008-10-07 Gilead Sciences, Inc. Phosphonate analogs of antimetabolites
US20050131042A1 (en) * 2003-12-11 2005-06-16 Flentge Charles A. HIV protease inhibiting compounds
US8193227B2 (en) 2003-12-11 2012-06-05 Abbott Laboratories HIV protease inhibiting compounds
BRPI0418031A (pt) * 2003-12-22 2007-04-17 Gilead Sciences Inc inibidores de quinase fosfonato-substituìdos
US20050153990A1 (en) * 2003-12-22 2005-07-14 Watkins William J. Phosphonate substituted kinase inhibitors
KR20060127906A (ko) * 2003-12-22 2006-12-13 길리애드 사이언시즈, 인코포레이티드 4'-치환된 카보버와 아바카비어 유도체 및 ｈｉｖ와 ｈｃｖ항바이러스 활성을 갖는 관련 화합물
US7772411B2 (en) 2003-12-23 2010-08-10 Tibotec Pharmaceuticals Ltd. Process for the preparation of (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-yl (1S,2R)-3[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate
US7200207B2 (en) * 2004-03-13 2007-04-03 Intrado Inc. Communication network for providing emergency services
JP4939396B2 (ja) * 2004-03-26 2012-05-23 ノヴァレメッド リミテッド Ａｉｄｓ及び他のウイルス性疾患及びｈｉｖ関連感染症の改善又はその治療用化合物及びそのような化合物を含む組成物、そのような疾患及び感染症の治療方法及びそのような化合物及び組成物の製造方法
AP2412A (en) 2004-07-27 2012-06-01 Gilead Sciences Inc Phosphonate analogs of HIV inhibitor compounds.
US20060135510A1 (en) * 2004-10-13 2006-06-22 The Trustees Of The University Of Pennsylvania Use of amprenavir as a radiation sensitizer
US20060116397A1 (en) * 2004-10-13 2006-06-01 The Trustees Of The University Of Pennsylvania Use of saquinavir as a radiation sensitizer
CA2588517A1 (en) 2004-12-01 2006-06-08 Devgen N.V. 5-carboxamido substituted thiazole derivatives that interact with ion channels, in particular with ion channels from the kv family
JP4326575B2 (ja) 2004-12-17 2009-09-09 デブゲン・エヌ・ブイ 殺線虫性組成物
US20080194554A1 (en) * 2005-03-11 2008-08-14 Mclean Ed W Hiv Protease Inhibitors
US20080009517A1 (en) * 2005-10-13 2008-01-10 The Trustees Of The University Of Pennsylvania Use of nelfinavir as a radiation sensitizer
DK2026775T3 (en) * 2006-05-09 2015-06-29 Novaremed Ltd USE OF SYK tyrosine kinase inhibitors for treating cell proliferative DISORDERS
MX2009009850A (es) 2007-03-12 2009-09-24 Nektar Therapeutics Conjugados de inhibidor de oligomero-proteasa.
DK2152667T3 (da) 2007-04-27 2011-05-16 Tibotec Pharm Ltd Fremgangsmåder til fremstilling af N-isobutyl-n-(2-hydroxy-3-amin-4-phenylbutyl)-p-nitrobenzenesulfonylamid-derivater
US20090075942A1 (en) * 2007-09-13 2009-03-19 Protia, Llc Deuterium-enriched fosamprenavir
GB2452952A (en) * 2007-09-20 2009-03-25 Npil Pharmaceuticals N-[2-Hydroxy-3-(hydroxycarbonylamino)-3-methyl]-N-methyl-sulphonamide derivatives via N-[2-oxo-3-(hydroxycarbonylamino)-3-methyl]-N-methyl-imine skeleton
JP2010540517A (ja) * 2007-09-25 2010-12-24 メルク・シャープ・エンド・ドーム・コーポレイション Ｈｉｖプロテアーゼ阻害剤
GB0804213D0 (en) * 2008-03-06 2008-04-16 New Era Biotech Ltd A method of printing or preventing pain
EP2262538B1 (en) * 2008-03-12 2014-12-10 Nektar Therapeutics Oligomer-amino acid conjugate
EP2116236A1 (en) 2008-04-21 2009-11-11 Université de Mons-Hainaut Bisbenzamidine derivatives for use as antioxidant
US8039514B2 (en) * 2008-06-05 2011-10-18 Asahi Kasei Pharma Corporation Sulfonamide compounds and use thereof
US8791135B2 (en) 2008-07-01 2014-07-29 Purdue Research Foundation Nonpeptide HIV-1 protease inhibitors
EP2307435B1 (en) 2008-07-08 2012-06-13 Gilead Sciences, Inc. Salts of hiv inhibitor compounds
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
US8802734B2 (en) * 2009-09-09 2014-08-12 Novaremed Limited Method of treating or preventing pain
WO2011061590A1 (en) 2009-11-17 2011-05-26 Hetero Research Foundation Novel carboxamide derivatives as hiv 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
US20120328568A1 (en) 2010-02-12 2012-12-27 Emory University Compositions and uses of lectins
MX2012010174A (es) 2010-03-02 2012-11-30 Amakem Nv Inhibidores novedosos de rock.
CN102190638A (zh) * 2010-03-16 2011-09-21 中国科学院上海药物研究所 联芳基醇二胺类化合物、其药物组合物、制备方法及应用
CN104203275A (zh) 2010-06-09 2014-12-10 疫苗技术股份有限公司 用于增强抗逆转录病毒治疗的hiv感染者的治疗性免疫
WO2011161256A1 (en) 2010-06-25 2011-12-29 Facultes Universitaires Notre Dame De La Paix Beta carboline derivatives useful in the treatment of proliferative disorders
US8785648B1 (en) 2010-08-10 2014-07-22 The Regents Of The University Of California PKC-epsilon inhibitors
US9511071B2 (en) 2010-08-18 2016-12-06 Emory University Compounds and compositions for ossification and methods related thereto
WO2012022780A1 (en) 2010-08-19 2012-02-23 Université Libre de Bruxelles 18-beta-glycyrrhetinic acid derivatives with anti-tumor activity
EP2614055A2 (en) 2010-09-10 2013-07-17 Lupin Limited Process for preparation of substantially pure fosamprenavir calcium and its intermediates
US9079834B2 (en) 2010-10-28 2015-07-14 Merck Canada Inc. HIV protease inhibitors
EP2632466A4 (en) 2010-10-29 2014-03-19 Univ Emory CHINAZOLINE DERIVATIVES, COMPOSITIONS THEREOF AND USES THEREOF
GB201019043D0 (en) 2010-11-10 2010-12-22 Protea Biopharma N V Use of 2',5'-oligoadenylate derivative compounds
WO2012075362A2 (en) 2010-12-03 2012-06-07 Emory University Chemokine cxcr4 receptor modulators and used related thereto
CN102584748B (zh) * 2011-01-13 2015-02-11 浙江九洲药业股份有限公司 夫沙那韦中间体的制备方法
US8691777B2 (en) 2011-01-27 2014-04-08 Emory University Combination therapy
EP2678052B1 (en) 2011-02-24 2018-09-26 Emory University Jab1 blocking compositions for ossification and methods related thereto
WO2012116135A2 (en) 2011-02-24 2012-08-30 Emory University Noggin blocking compositions for ossification and methods related thereto
WO2012135296A2 (en) 2011-03-31 2012-10-04 Emory University Imidazolyl amide compounds and uses related thereto
EP2699539B1 (en) 2011-04-21 2019-03-06 Emory University Cyclopropyl derivatives and methods of use
GB201107223D0 (en) 2011-04-29 2011-06-15 Amakem Nv Novel rock inhibitors
AU2012252433A1 (en) 2011-05-09 2013-11-07 Universiteit Antwerpen Activity-based probes for the urokinase plasminogen activator
GB201108225D0 (en) 2011-05-17 2011-06-29 Amakem Nv Novel KBC inhibitors
CA2839956A1 (en) 2011-06-20 2012-12-27 Emory University Prostaglandin receptor ep2 antagonists, derivatives, compositions, and uses related thereto
WO2013011485A1 (en) 2011-07-20 2013-01-24 Ranbaxy Laboratories Limited Process for the preparation of sulfonamides useful as retroviral protease inhibitors
GB201113689D0 (en) 2011-08-09 2011-09-21 Amakem Nv Novel PDE4 inhibitors
US9040567B2 (en) 2011-08-19 2015-05-26 Emory University BAX agonist, compositions, and methods related thereto
GB201114854D0 (en) 2011-08-29 2011-10-12 Amakem Nv Novel rock inhibitors
JP2014525425A (ja) 2011-08-31 2014-09-29 アマケン エンヴェー 新規のｒｏｃｋキナーゼ阻害剤
EA025881B1 (ru) 2011-09-30 2017-02-28 Онкодизайн С.А. Макроциклические ингибиторы flt3-киназы
HUE029728T2 (en) 2011-09-30 2017-03-28 Ipsen Pharma Sas Macrocyclic LRRK2 kinase inhibitors
WO2013059928A1 (en) 2011-10-26 2013-05-02 Merck Canada Inc. Hiv protease inhibitors
GB201119358D0 (en) 2011-11-10 2011-12-21 Lewi Paulus J Disubstituted triazine dimers for treatment and/or prevention of infectious diseases
ES2958619T3 (es) 2012-01-30 2024-02-12 Univ Gent Compuestos anti-invasivos
GB201204756D0 (en) 2012-03-19 2012-05-02 Lewi Paulus J Triazines with suitable spacers for treatment and/or prevention of HIV infections
US20150110723A1 (en) 2012-05-31 2015-04-23 Emory University Quinazoline derivatives, compositions, and uses related thereto
CN104487429B (zh) 2012-07-27 2017-07-14 爱默蕾大学 杂环黄酮衍生物、组合物及与其相关的方法
CA2882831A1 (en) 2012-09-11 2014-03-20 Merck Sharp & Dohme Corp. Hiv protease inhibitors
US9877981B2 (en) 2012-10-09 2018-01-30 President And Fellows Of Harvard College NAD biosynthesis and precursors for the treatment and prevention of cancer and proliferation
JP2015536940A (ja) 2012-10-29 2015-12-24 シプラ・リミテッド 抗ウイルス性ホスホネート類似体及びその製造方法
ES2823237T3 (es) 2012-11-05 2021-05-06 Univ Emory Derivados de 7,8-dihidroxiflavona y de flavona 7,8-sustituida, composiciones y métodos relacionados con los mismos
WO2014072419A1 (en) 2012-11-08 2014-05-15 Universiteit Antwerpen Novel anti-hiv compounds
ES2629762T3 (es) 2013-01-29 2017-08-14 Redx Pharma Plc Derivados de piridina como inhibidores de ROCK suaves
JP2016510797A (ja) 2013-03-15 2016-04-11 オンコデザイン エス．ア． 大環状塩誘導性キナーゼ阻害剤
WO2015013835A1 (en) 2013-07-31 2015-02-05 Merck Sharp & Dohme Corp. Piperazine derivatives as hiv protease inhibitors
SI3043803T1 (sl) 2013-09-11 2022-09-30 Emory University Nukleotidne in nukleozidne sestave in njihova uporaba
US10188738B2 (en) 2013-10-16 2019-01-29 Université Libre de Bruxelles Formulations useful in the treatment of proliferative diseases affecting the respiratory tract
US10159755B2 (en) 2013-11-12 2018-12-25 Vrije Universiteit Brussel RNA transcription vector and uses thereof
WO2015095276A1 (en) 2013-12-19 2015-06-25 Merck Sharp & Dohme Corp. Hiv protease inhibitors
EP3113780B1 (en) 2014-03-06 2019-08-14 Merck Sharp & Dohme Corp. Hiv protease inhibitors
WO2015150472A2 (en) 2014-04-01 2015-10-08 Université Libre de Bruxelles New strategies for treating melanoma
WO2015150337A1 (en) 2014-04-01 2015-10-08 Amakem Nv Lim kinase inhibitors
US9980936B2 (en) 2014-05-05 2018-05-29 Emory University BH4 antagonists and methods related thereto
EP3143005B1 (en) 2014-05-16 2021-07-07 Emory University Chemokine cxcr4 and ccr5 receptor modulators and used related thereto
EP3180003B1 (en) 2014-07-01 2022-01-12 The Regents of the University of California Pkc-epsilon inhibitors
US10023602B2 (en) 2014-07-08 2018-07-17 Universiteit Gent Hamamelitannin analogues and uses thereof
BR112017005299A2 (pt) 2014-09-17 2017-12-12 Ipsen Pharma Sas inibidores de lrrk2 cinase macrocíclicos
MY186523A (en) 2014-09-17 2021-07-24 Oncodesign Sa Macrocyclic rip2 kinase inhibitors
US9738664B2 (en) 2014-10-29 2017-08-22 Wisconsin Alumni Research Foundation Boronic acid inhibitors of HIV protease
WO2016083490A1 (en) 2014-11-27 2016-06-02 Remynd Nv Compounds for the treatment of amyloid-associated diseases
SG10202013032YA (en) 2014-12-15 2021-02-25 Univ Emory Phosphoramidates for the treatment of hepatitis b virus
SG11201705069YA (en) 2014-12-26 2017-07-28 Univ Emory N4-hydroxycytidine and derivatives and anti-viral uses related thereto
WO2016146651A1 (en) 2015-03-16 2016-09-22 Oncodesign Sa Macrocyclic activin-like receptor kinase inhibitors
ES2927894T3 (es) 2015-04-28 2022-11-11 Newsouth Innovations Pty Ltd Direccionamiento de NAD+ para tratar el deterioro cognitivo, inducido por quimioterapia y radioterapia, neuropatías e inactividad
EP4272820A3 (en) 2015-05-29 2024-01-03 Emory University 2-amino-n'-benzylideneacetohydrazides and derivatives for the management of cftr protein mediated diseases
DK3423113T3 (da) 2016-02-29 2020-11-30 Oncodesign Sa Radiomærket makrocyklisk egfr-hæmmer
WO2017157882A1 (en) 2016-03-14 2017-09-21 Université Catholique de Louvain Serine biosynthetic pathway inhibitors
JP7129703B2 (ja) 2016-04-28 2022-09-02 エモリー ユニバーシティー アルキン含有ヌクレオチド及びヌクレオシド治療組成物並びにそれらに関連した使用
US11166967B2 (en) 2016-05-19 2021-11-09 Universiteit Antwerpen Bis(acetamidophenyl) guanidinophenylethylphosphonates for use in the prevention and/or treatment of PAR-related diseases
BE1023757B1 (nl) 2016-06-30 2017-07-12 Yun NV Bewaring van micro-organismen
WO2018065387A1 (en) 2016-10-04 2018-04-12 Universiteit Gent Novel hamamelitannin analogues and uses thereof
EP3532488A4 (en) 2016-10-14 2020-04-29 Emory University NANOPARTICLES WITH MOLECULES FOR BINDING OR BLOCKING PD-L1 AND USED IN THE TREATMENT OF CANCER
WO2018081442A1 (en) 2016-10-26 2018-05-03 Emory University Polyoxometalate complexes and uses in managing cancer
EP3544952B1 (en) 2016-11-24 2024-11-06 Universiteit Antwerpen Halogenated benzotropolones as atg4b inhibitors
WO2018111580A1 (en) 2016-12-13 2018-06-21 Emory University Polypeptides for managing viral infections
US20190388426A1 (en) 2017-01-30 2019-12-26 Université de Liège Perk and ire-1a inhibitors against neurodevelopmental disorders
EP3585387A4 (en) 2017-02-21 2020-08-12 Emory University CHEMIOKIN CXCR4 RECEIVER MODULATORS AND THEIR USES
PL3621963T3 (pl) 2017-05-11 2024-05-20 Remynd N.V. Związki do leczenia epilepsji, zaburzeń neurodegeneracyjnych i innych zaburzeń oun
EP3634407A1 (en) 2017-05-11 2020-04-15 Remynd N.V. Inhibitors of pde6delta for use in the prevention and/or treatment of epilepsy and/or neurodegenerative disorders
PL3661937T3 (pl) 2017-08-01 2021-12-20 Gilead Sciences, Inc. Formy krystaliczne ((s)-((((2r,5r)-5-(6-amino-9h-puryn-9-ylo)-4-fluoro-2,5-dihydrofuran-2-ylo)oksy)metylo)(fenoksy)fosforylo)-l-alaninianu etylu (gs-9131) do leczenia zakażeń wirusowych
AU2018367909B2 (en) 2017-11-17 2022-03-10 Cellix Bio Private Limited Compositions and methods for the treatment of eye disorders
WO2019113462A1 (en) 2017-12-07 2019-06-13 Emory University N4-hydroxycytidine and derivatives and anti-viral uses related thereto
CA3135420A1 (en) 2018-04-05 2019-10-10 Universiteit Hasselt Selective pde4d inhibitors against demyelinating diseases
CN112654367B (zh) 2018-06-29 2023-08-04 再青春生物医药公司 用于年龄相关性和/或变性疾病的药物组合
EP4344743A3 (en) 2018-08-07 2024-06-19 Emory University Heterocyclic flavone derivatives, compositions, and methods related thereto
EP3843845A4 (en) 2018-08-29 2022-05-11 University Of Massachusetts INHIBITION OF PROTEIN KINASE FOR THE TREATMENT OF FRIEDREICH'S ATAXIA
AU2020242053C1 (en) 2019-03-20 2025-11-13 Emory University Prostaglandin receptor EP2 antagonists, derivatives, and uses related thereto
AU2020274407B2 (en) 2019-05-14 2023-09-28 Suzhou Four Health Pharmaceuticals Co., Ltd Quinazoline-2,4-dione derivatives as PARP inhibitors
EP3976029A4 (en) 2019-05-24 2023-06-14 Emory University ASPARAGINE ENDOPEPTIDASE (AEP) INHIBITORS, COMPOSITIONS AND USES THEREOF
MX2022010413A (es) 2020-02-24 2022-09-07 Univ Leuven Kath Compuestos de pirrolopiridina e imidazopiridina antivirales.
GB202003240D0 (en) 2020-03-05 2020-04-22 Ecosynth Nv Antiviral treatment
EP4121121A4 (en) 2020-03-16 2024-09-25 Emory University RADIONUCLIDE TRACERS OF 1-AMINO-3,4-DIFLUOROCYCLOPENTAN-1-CARBOXYLIC ACID, DERIVATIVES AND USES THEREOF
US20230218644A1 (en) 2020-04-16 2023-07-13 Som Innovation Biotech, S.A. Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus
US12083099B2 (en) 2020-10-28 2024-09-10 Accencio LLC Methods of treating symptoms of coronavirus infection with viral protease inhibitors
WO2022157381A1 (en) 2021-01-25 2022-07-28 Universiteit Hasselt Phloretin for use in the treatment of neurodegenerative and demyelinating diseases
PE20241304A1 (es) 2021-07-30 2024-06-24 Confo Therapeutics N V Compuestos para el tratamiento del dolor, en particular el dolor neuropatico, y/u otras enfermedades o trastornos que se asocian con at2r y/o senalizacion mediada por at2r
EP4387629A1 (en) 2021-08-18 2024-06-26 Katholieke Universiteit Leuven KU Leuven Research & Development 6-substituted- and 6,7-disubstituted-7-deazapurine ribonucleoside analogues
WO2023046900A1 (en) 2021-09-23 2023-03-30 Katholieke Universiteit Leuven Ribonucleoside analogues against -sars-cov-2
WO2023105283A1 (en) 2021-12-08 2023-06-15 Fundacio Privada Institut De Recerca De La Sida - Caixa Nucleoside reverse transcriptase inhibitors for use in down syndrome and alzheimer`s disease therapy
US11541071B1 (en) 2021-12-16 2023-01-03 Ascletis BioScience Co., Ltd Nucleoside derivatives and methods of use thereof
WO2023111683A1 (en) 2021-12-16 2023-06-22 Ascletis Bioscience Co., Ltd. N4-hydroxycytidine derivatives and use thereof as antiviral agent
US11760722B2 (en) 2022-01-18 2023-09-19 Ascletis Bioscience Co., Ltd. Inhibitors of cysteine proteases and methods of use thereof
WO2023139402A1 (en) 2022-01-18 2023-07-27 Ascletis Bioscience Co., Ltd. Inhibitors of cysteine proteases and methods of use thereof
WO2023180567A1 (en) 2022-03-24 2023-09-28 Fundacion Privada Institut De Recerca De La Sida-Caixa Cyclodextrins for use in coronavirus infection therapy
WO2023241799A1 (en) 2022-06-15 2023-12-21 Université Libre de Bruxelles Flavanols for use in the treatment of retroviral infections
WO2024009120A1 (en) 2022-07-08 2024-01-11 Ascletis Bioscience Co., Ltd. Triazine derivatives and methods of use thereof
CN115504968B (zh) 2022-11-21 2023-04-18 歌礼生物科技（杭州）有限公司 三嗪衍生物
WO2024193451A1 (en) 2023-03-17 2024-09-26 Ascletis BioScience Co., Ltd Triazine derivatives, method of making and method of using thereof
WO2025104221A1 (en) 2023-11-15 2025-05-22 Université Libre de Bruxelles Uses of protein tyrosine phosphatase receptor kappa inhibitors
WO2026013165A1 (en) 2024-07-10 2026-01-15 Université Libre de Bruxelles Combination of ship2 inhibitor and plk1 inhibitor for use in the treatment of cancer

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3743722A (en) 1971-07-14 1973-07-03 Abbott Lab Anti-coagulant isolation
FR2459235A1 (fr) * 1979-06-14 1981-01-09 Sanofi Sa Nouveaux derives de sulfonyl-aniline, leur procede de preparation et leur application therapeutique
JPS5946252A (ja) * 1982-09-09 1984-03-15 Dainippon Ink & Chem Inc 含フツ素アミノカルボキシレ−トおよびその製法
JPS5948449A (ja) * 1982-09-13 1984-03-19 Dainippon Ink & Chem Inc 直鎖状含フツ素アニオン化合物およびその製造方法
JPS6171830A (ja) * 1984-09-17 1986-04-12 Dainippon Ink & Chem Inc 界面活性剤組成物
US4616088A (en) * 1984-10-29 1986-10-07 E. R. Squibb & Sons, Inc. Amino acid ester and amide renin inhibitor
US4629724A (en) 1984-12-03 1986-12-16 E. R. Squibb & Sons, Inc. Amino acid ester and amide renin inhibitors
DE3635907A1 (de) * 1986-10-22 1988-04-28 Merck Patent Gmbh Hydroxy-aminosaeurederivate
NL8800100A (nl) * 1987-01-21 1988-08-16 Sandoz Ag Nieuwe peptidederivaten en werkwijzen voor het bereiden en toepassen van deze derivaten.
CA1340588C (en) 1988-06-13 1999-06-08 Balraj Krishan Handa Amino acid derivatives
IL91780A (en) 1988-10-04 1995-08-31 Abbott Lab History of the amine of the xenon-preventing xanine acid, the process for their preparation and the pharmaceutical preparations containing them
WO1990007330A1 (en) 1989-01-06 1990-07-12 The Regents Of The University Of California Selection method for specific useful pharmaceutical compounds
US5354866A (en) * 1989-05-23 1994-10-11 Abbott Laboratories Retroviral protease inhibiting compounds
US5151438A (en) * 1989-05-23 1992-09-29 Abbott Laboratories Retroviral protease inhibiting compounds
IE902295A1 (en) * 1989-07-07 1991-01-16 Abbott Lab Amino acid analog cck antagonists
GB8927913D0 (en) * 1989-12-11 1990-02-14 Hoffmann La Roche Amino acid derivatives
JPH07502970A (ja) * 1990-06-01 1995-03-30 ザ・デュポン・メルク・ファーマシュウティカル・カンパニー １，４―ジアミノ―２，３―ジヒドロキシブタン類
TW225540B (es) * 1990-06-28 1994-06-21 Shionogi & Co
DE69126987T2 (de) 1990-11-19 1998-03-05 Monsanto Co Retrovirale protease-inhibitoren
DK0813867T3 (da) * 1990-11-19 2005-10-03 Monsanto Co Retrovirale proteaseinhibitorer
EP0558673B1 (en) * 1990-11-19 1996-04-17 Monsanto Company Retroviral protease inhibitors
ATE196759T1 (de) 1990-11-19 2000-10-15 Monsanto Co Inhibitoren retroviraler proteasen
IE913840A1 (en) * 1990-11-20 1992-05-20 Abbott Lab Retroviral protease inhibiting compounds
ATE163926T1 (de) * 1991-11-08 1998-03-15 Merck & Co Inc Hiv-protease-inhibitoren verwendbar in der aids- behandlung
ATE141265T1 (de) * 1992-05-20 1996-08-15 Searle & Co Verfahren zur herstellung von intermediaten in der synthese von retroviralen protease inhibitoren
WO1993023379A1 (en) * 1992-05-21 1993-11-25 Monsanto Company Retroviral protease inhibitors
KR100296462B1 (ko) * 1992-08-25 2001-10-24 죤 에이치. 뷰센 레트로바이러스프로테아제억제제로서유용한술포닐알칸오일아미노히드록시에틸아미노술폰아미드
DK0656887T3 (da) * 1992-08-25 1999-07-05 Searle & Co Hydroxyethylaminosulfonamider til anvendelse som inhibitorer af retrovirale proteaser
EP0656886B1 (en) * 1992-08-25 1997-06-25 G.D. Searle & Co. N-(alkanoylamino-2-hydroxypropyl)-sulfonamides useful as retroviral protease inhibitors
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
IS2334B (is) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
DK0666843T3 (da) * 1992-10-30 2000-03-20 Searle & Co Sulfonylalkanoylaminohydroxyethylaminosulfaminsyrer, der kan anvendes som inhibitorer af retrovirale proteaser
CA2142997A1 (en) * 1992-10-30 1994-05-11 Michael L. Vazquez Hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors
WO1994018192A1 (en) * 1993-02-12 1994-08-18 Merck & Co., Inc. Piperazine derivatives as hiv protease inhibitors
TW281669B (es) * 1993-02-17 1996-07-21 Chugai Pharmaceutical Co Ltd

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DE10199024I1 (de) 2001-07-12
DE69333012D1 (de) 2003-07-03
IL106927A0 (en) 1993-12-28
US5585397A (en) 1996-12-17
RU2135496C1 (ru) 1999-08-27
HK1012631A1 (en) 1999-08-06
EP0885887A2 (en) 1998-12-23
AP9300572A0 (en) 1993-10-31
CY2164B1 (en) 2002-08-23
US20060189810A1 (en) 2006-08-24
CN1061339C (zh) 2001-01-31
AP390A (en) 1995-08-02
PT885887E (pt) 2003-10-31
HK1023561A1 (en) 2000-09-15
GR3030719T3 (en) 1999-11-30
IL106927A (en) 2001-01-11
GEP20012579B (en) 2001-11-26
NO950876D0 (no) 1995-03-07
TW254927B (es) 1995-08-21
CZ289475B6 (cs) 2002-01-16
LTIP917A (en) 1994-11-25
DE69324369D1 (de) 1999-05-12
HU228198B1 (en) 2013-01-28
JP3012002B2 (ja) 2000-02-21
US20030069222A1 (en) 2003-04-10
FI120685B (fi) 2010-01-29
US20080293727A1 (en) 2008-11-27
WO1994005639A1 (en) 1994-03-17
ES2131589T3 (es) 1999-08-01
NO2001012I1 (no) 2001-07-23
ES2200243T3 (es) 2004-03-01
EP0659181A1 (en) 1995-06-28
DK0659181T3 (da) 1999-10-18
NL300039I2 (nl) 2001-09-03
US20100210603A1 (en) 2010-08-19
MY142901A (en) 2011-01-31
DK0885887T3 (da) 2003-09-22
UA44694C2 (uk) 2002-03-15
DE69324369T2 (de) 1999-08-26
BG62488B1 (bg) 1999-12-30
EP0659181B1 (en) 1999-04-07
FI951059A0 (fi) 1995-03-07
HU9500685D0 (en) 1995-04-28
DE10199024I2 (de) 2006-04-06
SK281360B6 (sk) 2001-02-12
US5856353A (en) 1999-01-05
RO118747B1 (ro) 2003-10-30
LT3302B (en) 1995-06-26
JPH08501299A (ja) 1996-02-13
ATE241602T1 (de) 2003-06-15
ATE178598T1 (de) 1999-04-15
BR1100824A (pt) 1999-08-31
AU691160B2 (en) 1998-05-14
FI951059L (fi) 1995-04-18
SG43862A1 (en) 1997-11-14
NZ256238A (en) 1997-04-24
EP0885887A3 (en) 1999-02-03
PH31251A (en) 1998-05-05
US7608632B2 (en) 2009-10-27
HUT71892A (en) 1996-02-28
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RU95109928A (ru) 1997-03-20
AU4852093A (en) 1994-03-29
LU90736I2 (fr) 2001-05-07
PL185635B1 (pl) 2003-06-30
CA2143208A1 (en) 1994-03-17
EP0885887B1 (en) 2003-05-28
DE69333012T2 (de) 2004-04-01
SK29395A3 (en) 1995-09-13
IS2334B (is) 2008-02-15
CO4870779A1 (es) 1999-12-27
NO950876L (no) 1995-05-08
CA2143208C (en) 2003-01-07
US6372778B1 (en) 2002-04-16
BG99540A (bg) 1995-11-30
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NZ314376A (en) 1998-10-28
CN1087347A (zh) 1994-06-01
IS4068A (is) 1994-03-09
CZ58795A3 (en) 1995-12-13

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