HK1023561A1 - Sulfonamide inhibitors of hiv-aspartyl protease - Google Patents

Sulfonamide inhibitors of hiv-aspartyl protease

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Publication number
HK1023561A1
HK1023561A1 HK00100689A HK00100689A HK1023561A1 HK 1023561 A1 HK1023561 A1 HK 1023561A1 HK 00100689 A HK00100689 A HK 00100689A HK 00100689 A HK00100689 A HK 00100689A HK 1023561 A1 HK1023561 A1 HK 1023561A1
Authority
HK
Hong Kong
Prior art keywords
hiv
aspartyl protease
sulfonamide inhibitors
sulfonamide
inhibitors
Prior art date
Application number
HK00100689A
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 HK1023561A1 publication Critical patent/HK1023561A1/xx

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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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C307/00—Amides of sulfuric acids, i.e. compounds having singly-bound oxygen atoms of sulfate groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
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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
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/12—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
    • C07C311/13—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic rings
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    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—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
    • 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
    • C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C311/37—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
    • C07C311/38—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
    • 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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    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
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HK00100689A 1992-09-08 1998-12-17 Sulfonamide inhibitors of hiv-aspartyl protease HK1023561A1 (en)

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Families Citing this family (301)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6878728B1 (en) 1999-06-11 2005-04-12 Vertex Pharmaceutical Incorporated Inhibitors of aspartyl protease
US20040122000A1 (en) 1981-01-07 2004-06-24 Vertex Pharmaceuticals 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
US5642292A (en) * 1992-03-27 1997-06-24 Akiko Itai Methods for searching stable docking models of biopolymer-ligand molecule complex
US5968942A (en) 1992-08-25 1999-10-19 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
PT810209E (pt) * 1992-08-25 2002-09-30 Searle & Co Hidroxietilamino-sulfonamidas de alfa- e beta-aminoacidos uteis como inibidores de protease retroviral
US7141609B2 (en) * 1992-08-25 2006-11-28 G.D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US6046190A (en) * 1992-08-25 2000-04-04 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
US6743929B1 (en) 1992-08-25 2004-06-01 G. D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
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
US5783701A (en) * 1992-09-08 1998-07-21 Vertex Pharmaceuticals, Incorporated Sulfonamide inhibitors of aspartyl protease
ATE211462T1 (de) * 1992-10-30 2002-01-15 Searle & Co N-substituierte hydroxyethylaminosulfamidsäure- derivate verwendbar als inhibitoren retroviraler proteasen
EP0885880A3 (de) * 1992-10-30 1999-10-06 G.D. Searle & Co. Sulfonylalkanoylaminohydroxyethylaminosulfamidsäuren verwendbar als retrovirale Proteasehemmer
US5846993A (en) * 1992-12-22 1998-12-08 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
US5484926A (en) * 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
US6030991A (en) * 1993-05-20 2000-02-29 Texas Biotechnology Corp. 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
US6541498B2 (en) 1993-05-20 2003-04-01 Texas Biotechnology 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
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
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
US5831117A (en) 1995-01-20 1998-11-03 G. D. Searle & Co. Method of preparing retroviral protease inhibitor intermediates
EP1586558A3 (de) * 1995-01-20 2005-10-26 G.D. Searle LLC. Bis-sulfonamid-hydroxyethylamino-Derivate als Inhibitoren retroviraler Proteasen
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
US6861539B1 (en) 1995-03-10 2005-03-01 G. D. Searle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US6143788A (en) * 1995-03-10 2000-11-07 G.D. Searle & Co. Bis-amino acid hydroxyethlamino sulfonamide retroviral protease inhibitors
US7339078B2 (en) * 1995-03-10 2008-03-04 G.D. Searle Llc 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
US6150556A (en) * 1995-03-10 2000-11-21 G. D. Dearle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
EP1188766A1 (de) 1995-03-10 2002-03-20 G.D. Searle & Co. Verbindungen der Struktur bis-Aminosäure-Hydroxyethylamino-Sulfonamid als Inhibitoren der retroviralen Protease
US6407134B1 (en) 1995-03-10 2002-06-18 G. D. Searle & Co. Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
AU717598B2 (en) 1995-03-10 2000-03-30 G.D. Searle & Co. Heterocyclecarbonyl 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
EP0774453B1 (de) 1995-11-17 2002-02-06 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
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
DK0906107T3 (da) * 1996-03-22 2003-05-05 Glaxo Group Ltd Formuleringer indeholdende VX478 og en vandopløselig Vitamin E-forbindelse såsom Vitamin E-TPGS
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
PL330747A1 (en) * 1996-06-25 1999-05-24 Glaxo Group Ltd Vx478, zidovudin, ftc and/or 3tc containing combinations for use in treating hiv infections
WO1997049410A1 (en) * 1996-06-25 1997-12-31 Glaxo Group Limited Combinations comprising vx478, zidovudine and/or 1592u89 for use in the treatment of hiv
US5962725A (en) 1996-09-05 1999-10-05 Agouron Pharmaceuticals, Inc. Intermediate compounds useful for making HIV protease inhibitors such as nelfinavir
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
US6218424B1 (en) 1996-09-25 2001-04-17 Gpi Nil Holdings, Inc. Heterocyclic ketone and thioester compounds and uses
US5801187A (en) 1996-09-25 1998-09-01 Gpi-Nil Holdings, Inc. Heterocyclic esters and amides
US5786378A (en) * 1996-09-25 1998-07-28 Gpi Nil Holdings, Inc. Heterocyclic thioesters
IN183408B (de) * 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
US6121273A (en) * 1996-12-31 2000-09-19 Gpi Nil Holdings, Inc N-linked sulfonamides of heterocyclic thioesters
US5935989A (en) 1996-12-31 1999-08-10 Gpi Nil Holdings Inc. N-linked ureas and carbamates of heterocyclic thioesters
SK57899A3 (en) 1996-12-31 2000-05-16 Guilford Pharm 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
HU227183B1 (en) 1997-04-28 2010-09-28 Encysive Pharmaceuticals Inc Sulfonamide derivatives and pharmaceutical compositions containing them for the 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
EP0983228A4 (de) * 1997-05-08 2002-08-07 Smithkline Beecham Corp Proteaseinhibitoren
US5945441A (en) 1997-06-04 1999-08-31 Gpi Nil Holdings, Inc. Pyrrolidine carboxylate hair revitalizing agents
US6274602B1 (en) 1998-06-03 2001-08-14 Gpi Nil Holdings, Inc. Heterocyclic thioester and ketone hair growth compositions and uses
US6187796B1 (en) 1998-06-03 2001-02-13 Gpi Nil Holdings, Inc. Sulfone 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
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
GB9712253D0 (en) * 1997-06-13 1997-08-13 Glaxo Group Ltd Antiviral compound
RU2199532C2 (ru) 1997-06-27 2003-02-27 Фудзисава Фармасьютикал Ко., Лтд. Сульфонамидное соединение
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
US6436989B1 (en) * 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
AU2012199A (en) * 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
WO1999033792A2 (en) * 1997-12-24 1999-07-08 Vertex Pharmaceuticals Incorporated Prodrugs os aspartyl protease inhibitors
CN1110492C (zh) * 1997-12-24 2003-06-04 沃泰克斯药物股份有限公司 天冬氨酰蛋白酶抑制剂的前药
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
PL348661A1 (en) 1998-06-03 2002-06-03 Gpi Nil Holdings N-linked sulfonamides of n-heterocyclic carboxylic acids or carboxylic acid isosteres
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 (de) 1998-06-03 2001-03-28 GPI NIL Holdings, Inc. Haarwuchszusammensetzungen basiernd auf heterozyklischem ester und amid und anwendungen
US6331537B1 (en) 1998-06-03 2001-12-18 Gpi Nil Holdings, Inc. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds
WO1999065870A2 (en) * 1998-06-19 1999-12-23 Vertex Pharmaceuticals Incorporated Sulfonamide inhibitors of aspartyl protease
JP4776775B2 (ja) 1998-06-23 2011-09-21 アメリカ合衆国 Ｈｉｖ感染哺乳動物を治療するための医薬組成物
US6538006B1 (en) 1998-07-08 2003-03-25 Pharmacia Corporation 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
EP1100953B1 (de) * 1998-07-24 2002-10-09 Samsung Fine Chemicals Co., Ltd. Kontinuierliches Verfahren zur Herstellung von optisch reinem (S)-3-Hydroxy-gamma-Butyrolacton
US6384056B1 (en) 1998-08-14 2002-05-07 Gpi Nil Holdings, Inc. Heterocyclic thioesters or ketones 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
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
US6333340B1 (en) 1998-08-14 2001-12-25 Gpi Nil Holdings, Inc. Small molecule sulfonamides 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
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
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
US7338976B1 (en) 1998-08-14 2008-03-04 Gpi Nil Holdings, Inc. Heterocyclic esters or amides 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
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
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
TWI260322B (en) 1999-02-12 2006-08-21 Vertex Pharma Inhibitors of aspartyl protease
JP4814427B2 (ja) * 1999-02-12 2011-11-16 バーテックス 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のインヒビター
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
RU2247123C2 (ru) * 1999-10-06 2005-02-27 Тиботек Фармасьютикалз Лтд. Гексагидрофуро [2,3-b] фуран-3-ил-n-{3-[(1,3-бензодиоксол-5- илсульфонил)(изобутил)амино]-1-бензил -2-гидроксипропил}карбамат, фармацевтическая композиция на их основе, способы ингибирования и способ лечения
ATE401298T1 (de) 1999-12-23 2008-08-15 Ampac Fine Chemicals Llc Verbessertes verfahren zur herstellung von 2s,3s- n-isobutyl-n-(2-hydroxy-3-amino-4-phenylbutyl)- - nitrobenzenesulfonylamid hydrochlorid und anderen derivaten von 2-hydroxy-1,3-diamin
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
PT1248600E (pt) 2000-01-19 2008-08-25 Abbott Lab Formulações farmacêuticas melhoradas de inibidores da protease do vih
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
US7659404B2 (en) * 2001-02-14 2010-02-09 Tibotec Pharmaceuticals Ltd. Broad spectrum 2-(substituted-amino)-benzothiazole sulfonamide HIV protease inhibitors
US6756063B2 (en) 2001-03-29 2004-06-29 Zoltan Laboratories, Llc Methods and compositions for the treatment of human and animal cancers
PL367084A1 (en) 2001-04-09 2005-02-21 Tibotec Pharmaceuticals Ltd. Broadspectrum 2-(substituted-amino)-benzoxazole sulfonamide hiv protease inhibitors
US6696494B2 (en) 2001-10-22 2004-02-24 Enanta Pharmaceuticals, Inc. α-hydroxyarylbutanamine inhibitors of aspartyl protease
EP1472536A4 (de) * 2002-01-07 2007-02-14 Sequoia Pharmaceuticals Inhibitoren mit breitem spektrum
IL163666A0 (en) 2002-02-22 2005-12-18 New River Pharmaceuticals Inc Active agent delivery systems and methods for protecting and administering active agents
US7157489B2 (en) * 2002-03-12 2007-01-02 The Board Of Trustees Of The University Of Illinois HIV protease inhibitors
PL211979B1 (pl) 2002-04-26 2012-07-31 Gilead Sciences Pochodne fosfonianowe, ich zastosowanie w leczeniu zakażenia wirusem HIV i chorób wpływających na białe krwinki, oraz kompozycje farmaceutyczne zawierające te związki
DE60315984T2 (de) * 2002-05-17 2008-05-29 Tibotec Pharmaceuticals Ltd. Substituierte benzisoxazolsulfonamide mit breitbändiger hiv-protease hemmender wirkung
WO2003106405A1 (en) * 2002-06-01 2003-12-24 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
US7115652B2 (en) * 2002-06-17 2006-10-03 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
CA2493940C (en) * 2002-08-14 2011-11-22 Tibotec Pharmaceuticals Ltd. Broadspectrum substituted oxindole sulfonamide hiv protease inhibitors
UY27967A1 (es) * 2002-09-10 2004-05-31 Pfizer Acetil 2-hindroxi-1,3-diaminoalcanos
WO2004031129A2 (en) * 2002-10-03 2004-04-15 New Era Biotech, Ltd. Compounds for use in the treatment of autoimmune diseases, immuno-allergical diseases and organ or tissue transplantation rejection
US6713639B1 (en) 2002-10-28 2004-03-30 Council Of Scientific And Industrial Research Process for preparing enantiomerically pure (S)-3-hydroxy-gamma-butyrolactone
AU2003291308B2 (en) * 2002-11-12 2009-06-18 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
MXPA05005649A (es) * 2002-11-27 2005-08-16 Elan Pharm Inc Ureas y carbamatos sustituidos.
WO2004096286A2 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Antiviral phosphonate analogs
US7407965B2 (en) * 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
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
US7427636B2 (en) * 2003-04-25 2008-09-23 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
MXPA05011296A (es) 2003-04-25 2006-01-24 Gilead Sciences Inc Conjugados de fosfonato inhibidores de la cinasa.
US20090247488A1 (en) * 2003-04-25 2009-10-01 Carina Cannizzaro Anti-inflammatory phosphonate compounds
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
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
US7300924B2 (en) * 2003-04-25 2007-11-27 Gilead Sciences, Inc. Anti-infective phosphonate analogs
US8377952B2 (en) 2003-08-28 2013-02-19 Abbott Laboratories Solid pharmaceutical dosage formulation
US8025899B2 (en) 2003-08-28 2011-09-27 Abbott Laboratories Solid pharmaceutical dosage form
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
EP1671937A4 (de) * 2003-09-19 2007-08-08 Ube Industries Verfahren zur herstellung einer nitrilverbindung, carbonsäureverbindung oder carboxylatverbindung
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
US8193227B2 (en) 2003-12-11 2012-06-05 Abbott Laboratories HIV protease inhibiting compounds
US20050131042A1 (en) * 2003-12-11 2005-06-16 Flentge Charles A. HIV protease inhibiting compounds
US7432272B2 (en) * 2003-12-22 2008-10-07 Gilead Sciences, Inc. Antiviral analogs
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
RS51073B (sr) 2003-12-23 2010-10-31 Tibotec Pharmaceuticals Ltd. Proces za pripremanje (3r,3as,6ar)-heksahidrofuro│2,3-b│ furan-3-il (1s,2r)-3-││(4-aminofenil) sulfonil│(izobutil) amino │-1-benzil-2-hidroksipropilkarbamata
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
WO2006110157A2 (en) 2004-07-27 2006-10-19 Gilead Sciences, Inc. Nucleoside phosphonate conjugates as anti hiv agents
US20060116397A1 (en) * 2004-10-13 2006-06-01 The Trustees Of The University Of Pennsylvania Use of saquinavir as a radiation sensitizer
US20060135510A1 (en) * 2004-10-13 2006-06-22 The Trustees Of The University Of Pennsylvania Use of amprenavir as a radiation sensitizer
KR20070094754A (ko) 2004-12-01 2007-09-21 데브젠 엔브이 이온 채널, 특히 Ｋｖ 패밀리로부터의 이온 채널과상호작용하는 5-카복사미도 치환된 티아졸 유도체
US20080146445A1 (en) 2004-12-17 2008-06-19 Devgen Nv Nematicidal Compositions
EP1855672A4 (de) * 2005-03-11 2011-11-30 Glaxosmithkline Llc Hiv-proteasehemmer
US20080009517A1 (en) * 2005-10-13 2008-01-10 The Trustees Of The University Of Pennsylvania Use of nelfinavir as a radiation sensitizer
WO2007129226A2 (en) * 2006-05-09 2007-11-15 New Era Biotech Ltd Use of syk tyrosine kinase inhibitors for the treatment of cell proliferative disorders
AU2008226823B2 (en) 2007-03-12 2014-03-13 Nektar Therapeutics Oligomer-protease inhibitor conjugates
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
AU2008305678A1 (en) * 2007-09-25 2009-04-02 Merck Sharp & Dohme Corp. HIV protease inhibitors
GB0804213D0 (en) * 2008-03-06 2008-04-16 New Era Biotech Ltd A method of printing or preventing pain
EP2262538B1 (de) * 2008-03-12 2014-12-10 Nektar Therapeutics Oligomer-aminosäure konjugate
EP2116236A1 (de) 2008-04-21 2009-11-11 Université de Mons-Hainaut Bisbenzamidinderivate als Antioxidationsmittel
US8039514B2 (en) * 2008-06-05 2011-10-18 Asahi Kasei Pharma Corporation Sulfonamide compounds and use thereof
EP2307345A4 (de) * 2008-07-01 2012-05-02 Purdue Research Foundation Nichtpeptidinhibitoren der hiv-1-protease
PL2307435T3 (pl) 2008-07-08 2012-11-30 Gilead Sciences Inc Sole związków inhibitorów HIV
JP2012528160A (ja) 2009-05-27 2012-11-12 メルク・シャープ・エンド・ドーム・コーポレイション Ｈｉｖプロテアーゼ阻害薬
WO2010144869A2 (en) 2009-06-12 2010-12-16 Nektar Therapeutics Protease inhibitors
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
BR112012021889B1 (pt) 2010-03-02 2022-01-11 Ph Pharma Co., Ltd Compostos de amidas heterocíclicas e composição que as compreende para a prevenção ou o tratamento de doenças oculares
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
CN114010776A (zh) 2010-06-09 2022-02-08 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
JP2013533239A (ja) 2010-06-25 2013-08-22 ファキュルテ ユニヴェルシテール ノートル−ダム ド ラ ペ 増殖性疾患の治療に有用なβカルボリン誘導体
US8785648B1 (en) 2010-08-10 2014-07-22 The Regents Of The University Of California PKC-epsilon inhibitors
EP2605804B1 (de) 2010-08-18 2017-03-15 Emory University Verbindungen und zusammensetzungen für verknöcherungen und entsprechende verfahren
WO2012022780A1 (en) 2010-08-19 2012-02-23 Université Libre de Bruxelles 18-beta-glycyrrhetinic acid derivatives with anti-tumor activity
US8877947B2 (en) 2010-09-10 2014-11-04 Lupin Limited Process for preparation of substantially pure fosamprenavir calcium and its intermediates
WO2012055031A1 (en) 2010-10-28 2012-05-03 Merck Canada Inc. Hiv protease inhibitors
CA2816022C (en) 2010-10-29 2019-09-10 Emory University Quinazoline derivatives, compositions, and uses related thereto
GB201019043D0 (en) 2010-11-10 2010-12-22 Protea Biopharma N V Use of 2',5'-oligoadenylate derivative compounds
ES2607604T3 (es) 2010-12-03 2017-04-03 Emory University Moduladores del receptor CXCR4 de quimiocina y usos relacionados con los mismos
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
CA2826773C (en) 2011-02-24 2019-07-16 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
WO2012145234A2 (en) 2011-04-21 2012-10-26 Emory University Cyclopropyl derivatives and methods of use
GB201107223D0 (en) 2011-04-29 2011-06-15 Amakem Nv Novel rock inhibitors
US20140079632A1 (en) 2011-05-09 2014-03-20 Universiteit Antwerpen Activity-based probes for the urokinase plasminogen activator
GB201108225D0 (en) 2011-05-17 2011-06-29 Amakem Nv Novel KBC inhibitors
EP2721011B1 (de) 2011-06-20 2017-09-06 Emory University Prostaglandinrezeptor-ep2-antagonisten, derivate davon, zusammensetzungen damit und verwendungen davon
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
CA2848726C (en) 2011-08-19 2019-09-10 Emory University Bax agonist, compositions, and methods related thereto
GB201114854D0 (en) 2011-08-29 2011-10-12 Amakem Nv Novel rock inhibitors
MX2014002395A (es) 2011-08-31 2014-06-05 Amakem Nv Inhibidores de rock suaves, novedosos.
US9090630B2 (en) 2011-09-30 2015-07-28 Oncodesign S.A. Macrocyclic FLT3 kinase inhibitors
JP6082397B2 (ja) 2011-09-30 2017-02-15 イプセン ファルマ ソシエテ パール アクシオン サンプリフィエＩｐｓｅｎ Ｐｈａｒｍａ Ｓ．Ａ．Ｓ． マクロ環状ｌｒｒｋ２キナーゼ阻害剤
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
EP2810198B1 (de) 2012-01-30 2023-07-12 Universiteit Gent Antiinvasive verbindungen
GB201204756D0 (en) 2012-03-19 2012-05-02 Lewi Paulus J Triazines with suitable spacers for treatment and/or prevention of HIV infections
WO2013181135A1 (en) 2012-05-31 2013-12-05 Emory University Quinazoline derivatives, compositions, and uses related thereto
WO2014018741A1 (en) 2012-07-27 2014-01-30 Emory University Heterocyclic flavone derivatives, compositions, and methods related thereto
JP2015527403A (ja) 2012-09-11 2015-09-17 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Ｈｉｖプロテアーゼ阻害剤
WO2014059034A2 (en) 2012-10-09 2014-04-17 President And Fellows Of Harvard College Nad biosynthesis and precursors for the treatment and prevention of cancer and proliferation
AU2013340559B2 (en) 2012-10-29 2018-03-15 Cipla Limited Antiviral phosphonate analogues and process for preparation thereof
EP2914585B1 (de) 2012-11-05 2018-03-07 Emory University 7,8-dihydroxyflavon und 7,8-substituierte flavonderivate, zusammensetzungen und zugehörige verfahren
WO2014072419A1 (en) 2012-11-08 2014-05-15 Universiteit Antwerpen Novel anti-hiv compounds
SG11201505867PA (en) 2013-01-29 2015-08-28 Amakem Nv Pyridine derivatives as soft rock inhibitors
AU2014230125A1 (en) 2013-03-15 2015-10-29 Oncodesign S.A. Macrocyclic salt-inducible kinase inhibitors
WO2015013835A1 (en) 2013-07-31 2015-02-05 Merck Sharp & Dohme Corp. Piperazine derivatives as hiv protease inhibitors
DK3043803T3 (da) 2013-09-11 2022-08-01 Univ Emory Nukleotid- og nucleosidsammensætninger og deres anvendelse
EP3057619A1 (de) 2013-10-16 2016-08-24 Université Libre de Bruxelles Formulierungen zur behandlung proliferativer erkrankungen des atemtrakts
PT3336192T (pt) 2013-11-12 2022-03-10 Univ Brussel Vrije Vetor de transcrição de rna e utilizações do mesmo
US9834526B2 (en) 2013-12-19 2017-12-05 Merck Sharp & Dohme Corp. HIV protease inhibitors
WO2015134366A1 (en) 2014-03-06 2015-09-11 Merck Sharp & Dohme Corp. Hiv protease inhibitors
US20170165240A1 (en) 2014-04-01 2017-06-15 Université Libre de Bruxelles New strategies for treating melanoma
WO2015150337A1 (en) 2014-04-01 2015-10-08 Amakem Nv Lim kinase inhibitors
AU2015256266B2 (en) 2014-05-05 2019-01-17 Emory University BH4 antagonists and methods related thereto
EP3143005B1 (de) 2014-05-16 2021-07-07 Emory University Chemokin-cxcr4- und -ccr5-rezeptormodulatoren und verwendungen im zusammenhang damit
EP3180003B1 (de) 2014-07-01 2022-01-12 The Regents of the University of California Pkc-epsilon-inhibitoren
EP3166955B1 (de) 2014-07-08 2018-05-02 Universiteit Gent Hamamelitanninanaloga und verwendungen davon
CA2958782C (en) 2014-09-17 2024-01-09 Oncodesign S.A. Macrocyclic rip2 kinase inhibitors
JP2017529365A (ja) 2014-09-17 2017-10-05 オンコデザイン エス．ア． 大環状ｌｒｒｋ２キナーゼ阻害剤
WO2016069955A1 (en) 2014-10-29 2016-05-06 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
IL280459B2 (en) 2014-12-15 2023-03-01 Univ Emory Phosphoramidates for the treatment of hepatitis b virus
CN107427529A (zh) 2014-12-26 2017-12-01 埃莫里大学 N4‑羟基胞苷和衍生物及与其相关的抗病毒用途
WO2016146651A1 (en) 2015-03-16 2016-09-22 Oncodesign Sa Macrocyclic activin-like receptor kinase inhibitors
CN108025187A (zh) 2015-04-28 2018-05-11 新南创新私人有限公司 靶向nad+以治疗化学疗法和放射疗法引发的认知损害、神经病变和不活动
EP3302455B1 (de) 2015-05-29 2020-09-16 Emory University 2-amino-n'-benzylidenacetohydrazide und derivate zur verwaltung von cftr-protein-vermittelten krankheiten
ES2833959T3 (es) 2016-02-29 2021-06-16 Oncodesign Sa Inhibidor del EGFR macrocíclico radiomarcado
WO2017157882A1 (en) 2016-03-14 2017-09-21 Université Catholique de Louvain Serine biosynthetic pathway inhibitors
EA201892448A1 (ru) 2016-04-28 2019-06-28 Эмори Юниверсити Алкинсодержащие нуклеотидные и нуклеозидные терапевтические композиции и связанные с ними способы применения
JP2019516715A (ja) 2016-05-19 2019-06-20 ユニバーシタット アントウェルペン Ｐａｒ関連疾患の予防および／または治療における使用のためのビス（アセトアミドフェニル）グアニジノフェニルエチルホスホネート
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 (de) 2016-10-14 2020-04-29 Emory University Nanopartikel mit molekülen zur bindung oder blockierung von pd-l1 und verwendung bei der behandlung von krebs
CN110049866B (zh) 2016-10-26 2022-04-05 爱默蕾大学 多金属氧酸盐络合物在制备用于治疗癌症的药物组合物中的用途以及该药物组合物
EP3544952B1 (de) 2016-11-24 2024-11-06 Universiteit Antwerpen Halogenierte benzotropolone als atg4b-inhibitoren
AU2017377993A1 (en) 2016-12-13 2019-07-04 Emory University Polypeptides for managing viral infections
WO2018138358A1 (en) 2017-01-30 2018-08-02 Université de Liège Perk and ire-1a inhibitors against neurodevelopmental disorders
CN110545814A (zh) 2017-02-21 2019-12-06 爱默蕾大学 趋化因子cxcr4受体调节剂及其相关用途
PL3621963T3 (pl) 2017-05-11 2024-05-20 Remynd N.V. Związki do leczenia epilepsji, zaburzeń neurodegeneracyjnych i innych zaburzeń oun
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
RU2761436C1 (ru) 2017-11-17 2021-12-08 Целликс Био Прайвет Лимитед Композиции и способы лечения нарушений со стороны органа зрения
KR102626210B1 (ko) 2017-12-07 2024-01-18 에모리 유니버시티 N4-하이드록시사이티딘 및 유도체 및 이와 관련된 항-바이러스 용도
US20210145838A1 (en) 2018-04-05 2021-05-20 Universiteit Hasselt Selective pde4d inhibitors against demyelinating diseases
EP3813882B1 (de) 2018-06-29 2023-08-09 Rejuvenate Biomed Pharmazeutische kombination mit biguanid und einem acetylcholinesterasehemmer zur verwendung bei altersbedingten erkrankungen
ES2974972T3 (es) 2018-08-07 2024-07-02 Univ Emory Derivados heterocíclicos de flavona, composiciones y métodos relacionados con los mismos
US20210292766A1 (en) 2018-08-29 2021-09-23 University Of Massachusetts Inhibition of Protein Kinases to Treat Friedreich Ataxia
JP7370032B2 (ja) 2019-05-14 2023-10-27 スーヂョウ フォー ヘルス ファーマスーティカルズ カンパニー リミテッド Ｐａｒｒ阻害剤としてのキナゾリン―２．４―ジオン誘導体
CN115175909A (zh) 2020-02-24 2022-10-11 鲁汶天主教大学 吡咯并吡啶和咪唑并吡啶抗病毒化合物
GB202003240D0 (en) 2020-03-05 2020-04-22 Ecosynth Nv Antiviral treatment
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
WO2023006893A1 (en) 2021-07-30 2023-02-02 Confo Therapeutics N.V. Compounds for the treatment of pain, in particular neuropathic pain, and/or other diseases or disorders that are associated with at2r and/or at2r mediated signaling
WO2023021132A1 (en) 2021-08-18 2023-02-23 Katholieke Universiteit Leuven 6-substituted- and 6,7-disubstituted-7-deazapurine ribonucleoside analogues
EP4405357A1 (de) 2021-09-23 2024-07-31 Katholieke Universiteit Leuven KU Leuven Research & Development Ribonukleosidanaloga gegen -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
KR200498007Y1 (ko) 2022-01-20 2024-05-17 주식회사 다우기업 내용물 유출 방지 기능이 향상된 윤활유 용기
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
US20240025885A1 (en) 2022-07-08 2024-01-25 Ascletis BioScience Co., Ltd Triazine derivatives and methods of use thereof
CN116514783A (zh) 2022-11-21 2023-08-01 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

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 (de) * 1990-06-28 1994-06-21 Shionogi & Co
AU9053191A (en) * 1990-11-19 1992-06-11 Monsanto Company Retroviral protease inhibitors
ATE196759T1 (de) 1990-11-19 2000-10-15 Monsanto Co Inhibitoren retroviraler proteasen
ES2059289T3 (es) 1990-11-19 1997-10-16 Monsanto Co Inhibidores de la proteasa retroviral.
CA2096407C (en) * 1990-11-19 2007-10-02 Kathryn Lea Reed Retroviral protease inhibitors
IE20010533A1 (en) * 1990-11-20 2003-03-05 Abbott Lab Intermediates for preparing retroviral protease inhibiting compounds
IL103613A (en) 1991-11-08 1999-05-09 Merck & Co Inc VIH protease inhibitors, and the process of preparing intermediates and pharmaceutical preparations containing them.
AU676479B2 (en) * 1992-05-20 1997-03-13 G.D. Searle & Co. Method for making intermediates useful in synthesis of retroviral protease inhibitors
EP1447398A1 (de) * 1992-05-21 2004-08-18 Monsanto Company Inhibitoren von Retroviraler Protease
JP4091654B2 (ja) * 1992-08-25 2008-05-28 ジー．ディー．サール、リミテッド、ライアビリティ、カンパニー レトロウイルスプロテアーゼ阻害剤として有用なスルホニルアルカノイルアミノヒドロキシエチルアミノスルホンアミド
ES2103488T3 (es) * 1992-08-25 1997-09-16 Searle & Co N-(alcanoilamino-2-hidroxipropil)sulfonamidas utiles como inhibidores de proteasas retrovirales.
PT810209E (pt) * 1992-08-25 2002-09-30 Searle & Co Hidroxietilamino-sulfonamidas de alfa- e beta-aminoacidos uteis como inibidores de protease retroviral
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
EP0885880A3 (de) * 1992-10-30 1999-10-06 G.D. Searle & Co. Sulfonylalkanoylaminohydroxyethylaminosulfamidsäuren verwendbar als retrovirale Proteasehemmer
ATE211462T1 (de) * 1992-10-30 2002-01-15 Searle & Co N-substituierte hydroxyethylaminosulfamidsäure- derivate verwendbar als inhibitoren retroviraler proteasen
AU6135294A (en) * 1993-02-12 1994-08-29 Merck & Co., Inc. Piperazine derivatives as hiv protease inhibitors
TW281669B (de) * 1993-02-17 1996-07-21 Chugai Pharmaceutical Co Ltd

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US7608632B2 (en) 2009-10-27
SK281360B6 (sk) 2001-02-12
EP0885887A2 (de) 1998-12-23
US5856353A (en) 1999-01-05
CY2164B1 (en) 2002-08-23
CZ289475B6 (cs) 2002-01-16
WO1994005639A1 (en) 1994-03-17
EP0659181A1 (de) 1995-06-28
US6372778B1 (en) 2002-04-16
PL185635B1 (pl) 2003-06-30
US20030069222A1 (en) 2003-04-10
EP0885887A3 (de) 1999-02-03
FI120685B (fi) 2010-01-29
PH31251A (en) 1998-05-05
DE69333012T2 (de) 2004-04-01
LTIP917A (en) 1994-11-25
KR100262056B1 (ko) 2000-07-15
PL307858A1 (en) 1995-06-26
BR1100824A (pt) 1999-08-31
UA44694C2 (uk) 2002-03-15
PT885887E (pt) 2003-10-31
NO303444B1 (no) 1998-07-13
GR3030719T3 (en) 1999-11-30
FI951059A0 (fi) 1995-03-07
LU90736I2 (fr) 2001-05-07
ATE178598T1 (de) 1999-04-15
DK0659181T3 (da) 1999-10-18
LT3302B (en) 1995-06-26
HU228198B1 (en) 2013-01-28
IL106927A0 (en) 1993-12-28
RU95109928A (ru) 1997-03-20
US20100210603A1 (en) 2010-08-19
NO2001012I1 (no) 2001-07-23
CA2143208A1 (en) 1994-03-17
BG99540A (bg) 1995-11-30
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JPH08501299A (ja) 1996-02-13
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CO4870779A1 (es) 1999-12-27
US20060189810A1 (en) 2006-08-24
US20080293727A1 (en) 2008-11-27
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MY142901A (en) 2011-01-31
HK1012631A1 (en) 1999-08-06
DK0885887T3 (da) 2003-09-22
DE69324369T2 (de) 1999-08-26
AU4852093A (en) 1994-03-29
DE10199024I1 (de) 2001-07-12
DE69333012D1 (de) 2003-07-03
ES2131589T3 (es) 1999-08-01
SK29395A3 (en) 1995-09-13
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AU691160B2 (en) 1998-05-14
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HUT71892A (en) 1996-02-28
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NO950876L (no) 1995-05-08
GEP20012579B (en) 2001-11-26
AP390A (en) 1995-08-02
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CA2143208C (en) 2003-01-07
ATE241602T1 (de) 2003-06-15
RU2135496C1 (ru) 1999-08-27
IL106927A (en) 2001-01-11
MXPA03010538A (es) 2011-12-16
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DE10199024I2 (de) 2006-04-06
IS4068A (is) 1994-03-09
CN1087347A (zh) 1994-06-01
IS2334B (is) 2008-02-15
RO118747B1 (ro) 2003-10-30
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NO950876D0 (no) 1995-03-07
JP3012002B2 (ja) 2000-02-21
TW254927B (de) 1995-08-21
BG62488B1 (bg) 1999-12-30
NZ314376A (en) 1998-10-28
US5585397A (en) 1996-12-17

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