ATE241602T1 - Sulfonamide inhibitore von hiv-aspartyl protease - Google Patents

Sulfonamide inhibitore von hiv-aspartyl protease

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Publication number
ATE241602T1
ATE241602T1 AT98113921T AT98113921T ATE241602T1 AT E241602 T1 ATE241602 T1 AT E241602T1 AT 98113921 T AT98113921 T AT 98113921T AT 98113921 T AT98113921 T AT 98113921T AT E241602 T1 ATE241602 T1 AT E241602T1
Authority
AT
Austria
Prior art keywords
inhibiters
sulfonamide
hiv
aspartyl protease
aspartyl
Prior art date
Application number
AT98113921T
Other languages
German (de)
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
Application granted granted Critical
Publication of ATE241602T1 publication Critical patent/ATE241602T1/de

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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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    • 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
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
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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
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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
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    • 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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AT98113921T 1992-09-08 1993-09-07 Sulfonamide inhibitore von hiv-aspartyl protease ATE241602T1 (de)

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Families Citing this family (305)

* 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
EP0656887B1 (en) * 1992-08-25 1998-10-28 G.D. Searle & Co. 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
US6743929B1 (en) 1992-08-25 2004-06-01 G. D. Searle & Co. Sulfonylalkanoylamino 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
US6046190A (en) * 1992-08-25 2000-04-04 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
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
IS2334B (is) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
DE69331421T2 (de) 1992-10-30 2002-08-01 G.D. SEARLE & CO., CHICAGO N-substituierte Hydroxyethylaminosulfamidsäure-Derivate verwendbar als Inhibitoren retroviraler Proteasen
EP0885881B1 (en) * 1992-10-30 2003-03-12 G.D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfamic acids useful as retroviral protease inhibitors
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
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
US6376523B1 (en) 1994-05-20 2002-04-23 Texas Biotechnology Corporation Benzenesulfonamides and the use thereof to 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
US6541498B2 (en) 1993-05-20 2003-04-01 Texas Biotechnology Benzenesulfonamides and the use thereof to modulate the activity of endothelin
US5846981A (en) * 1993-05-28 1998-12-08 Gpi Nil Holdings Inc. Inhibitors of rotamase enzyme activity
US5798355A (en) * 1995-06-07 1998-08-25 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
US5831117A (en) 1995-01-20 1998-11-03 G. D. Searle & Co. Method of preparing retroviral protease inhibitor intermediates
JP4014220B2 (ja) 1995-01-20 2007-11-28 ジー．ディー．サール アンド カンパニー ビス−スルホンアミドヒドロキシエチルアミノ レトロ ウイルスプロテアーゼインヒビター
US6140505A (en) 1995-03-10 2000-10-31 G. D. Searle & Co. Synthesis of benzo fused heterocyclic sulfonyl chlorides
US5756533A (en) * 1995-03-10 1998-05-26 G.D. Searle & Co. 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
US6150556A (en) * 1995-03-10 2000-11-21 G. D. Dearle & 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
PL184771B1 (pl) * 1995-03-10 2002-12-31 Searle & Co Związek stanowiący hydroksyetyloaminosulfonamid pirolidynokarbonyloaminokwasu, kompozycja zawierająca ten związek, jego zastosowanie do wytwarzania kompozycji do leczenia infekcji retrowirusowej i sposób zapobiegania replikacji retrowirusa in vitro
EP1188766A1 (en) 1995-03-10 2002-03-20 G.D. Searle & Co. 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
US6143788A (en) * 1995-03-10 2000-11-07 G.D. Searle & Co. Bis-amino acid hydroxyethlamino sulfonamide retroviral protease inhibitors
US5776971A (en) * 1995-03-10 1998-07-07 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
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
US6730679B1 (en) 1996-03-22 2004-05-04 Smithkline Beecham Corporation Pharmaceutical formulations
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
NZ331645A (en) * 1996-03-22 2000-02-28 Glaxo Group Ltd Compositions comprising an HIV protease inhibitor such as VX 478 and a water soluble vitamin E compound such as 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
CN1306430A (zh) * 1996-06-25 2001-08-01 葛兰素集团有限公司 用于治疗hiv感染的含有vx478、叠氮胸苷和/或1592u89的复方制剂
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
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
US5925759A (en) * 1996-09-05 1999-07-20 Agouron Pharmaceuticals, Inc. Methods of making HIV-protease inhibitors and intermediates for making HIV-protease inhibitors
US5786378A (en) * 1996-09-25 1998-07-28 Gpi Nil Holdings, Inc. Heterocyclic thioesters
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
IN183408B (en, 2012) * 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
JP2002515050A (ja) 1996-12-31 2002-05-21 ジーピーアイ エヌアイエル ホールディングス インコーポレイテッド ヘテロ環式チオエステルのｎ−結合尿素およびカルバメート
US5874449A (en) * 1996-12-31 1999-02-23 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
JP2002515051A (ja) 1996-12-31 2002-05-21 ジーピーアイ エヌアイエル ホールディングス インコーポレイテッド ヘテロ環式チオエステルのｎ−結合スルホンアミド
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
US5783705A (en) * 1997-04-28 1998-07-21 Texas Biotechnology Corporation Process of preparing alkali metal salys of hydrophobic sulfonamides
ATE292129T1 (de) 1997-04-28 2005-04-15 Encysive Pharmaceuticals Inc Sulfonamide für die behandlung von störungen durch endothelin vermittelt
KR20010012325A (ko) * 1997-05-08 2001-02-15 스튜어트 알. 수터, 스티븐 베네티아너, 피터 존 기딩스 프로테아제 억제제
US6187796B1 (en) 1998-06-03 2001-02-13 Gpi Nil Holdings, Inc. Sulfone hair growth compositions and uses
US6274602B1 (en) 1998-06-03 2001-08-14 Gpi Nil Holdings, Inc. Heterocyclic thioester and ketone hair growth compositions and uses
US5945441A (en) 1997-06-04 1999-08-31 Gpi Nil Holdings, Inc. Pyrrolidine carboxylate hair revitalizing agents
US6187784B1 (en) 1998-06-03 2001-02-13 Gpi Nil Holdings, Inc. Pipecolic acid derivative hair growth compositions and uses
US20010049381A1 (en) 1997-06-04 2001-12-06 Gpl Nil Holdings, Inc., Pyrrolidine 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
WO1999000372A1 (en) 1997-06-27 1999-01-07 Fujisawa Pharmaceutical Co., Ltd. Sulfonamide compounds and medicinal use thereof
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
HUP0101598A3 (en) * 1997-12-24 2002-08-28 Vertex Pharmaceuticals Inc Cam Prodrugs of aspartyl protease inhibitors and medicaments containing them
AU2010299A (en) * 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs os aspartyl protease inhibitors
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
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
US6331537B1 (en) 1998-06-03 2001-12-18 Gpi Nil Holdings, Inc. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic 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
BR9815882A (pt) 1998-06-03 2002-09-17 Gpi Nil Holding Inc Sulfonamidas ligadas por n de ácido carboxìlicos n-heterocìclicos ouou de isósteros de ácidos carboxìlicos
AU770459B2 (en) 1998-06-03 2004-02-19 Gpi Nil Holdings, Inc. Heterocyclic ester and amide hair growth compositions and uses
AU767728B2 (en) * 1998-06-19 2003-11-20 Vertex Pharmaceuticals Incorporated Sulfonamide inhibitors of aspartyl protease
ES2362404T5 (es) 1998-06-23 2015-11-25 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Ensayo de aptitud y métodos para reducir la resistencia del VIH a terapia
WO2000002862A1 (en) 1998-07-08 2000-01-20 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
CN1316008A (zh) 1998-07-24 2001-10-03 三星精密化学株式会社 制备α－(1,4)－连接的寡糖的方法
US7338976B1 (en) 1998-08-14 2008-03-04 Gpi Nil Holdings, Inc. Heterocyclic esters or amides 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
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
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
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
US6395758B1 (en) 1998-08-14 2002-05-28 Gpi Nil Holdings, Inc. Small molecule carbamates or ureas 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
US6218423B1 (en) 1998-08-14 2001-04-17 Gpi Nil Holdings, Inc. Pyrrolidine derivatives for vision and memory disorders
US6384056B1 (en) 1998-08-14 2002-05-07 Gpi Nil Holdings, Inc. Heterocyclic thioesters or ketones 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
US6462072B1 (en) 1998-09-21 2002-10-08 Gpi Nil Holdings, Inc. Cyclic ester or amide derivatives
US7635690B2 (en) * 1999-01-22 2009-12-22 Emory University HIV-1 mutations selected for by β-2′,3′-didehydro-2′,3′-dideoxy-5-fluorocytidine
US7115584B2 (en) * 1999-01-22 2006-10-03 Emory University HIV-1 mutations selected for by β-2′,3′-didehydro-2′,3′-dideoxy-5-fluorocytidine
TNSN00027A1 (fr) 1999-02-12 2005-11-10 Vertex Pharma Inhibiteurs de l'aspartyle protease
PT1159278E (pt) * 1999-02-12 2006-06-30 Vertex Pharma Inibidores de aspartil-protease
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
ATE398623T1 (de) * 1999-10-06 2008-07-15 Tibotec Pharm Ltd Hexahydrofuro-2,3-b furan-3-yl-n- 3-,(1,3- benzodioxol-5-ylsulfonyl)(isobutyl)amino -1- benzyl-2-hydroxypropyl carbamat als retrovirusproteasehemmer
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
PT1917958E (pt) 2000-01-19 2012-08-16 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
WO2002083657A2 (en) * 2001-02-14 2002-10-24 Tibotec Pharmaceuticals Ltd. Broadspectrum 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
CA2442870C (en) * 2001-04-09 2011-08-02 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
CA2473231A1 (en) * 2002-01-07 2003-08-07 Sequoia Pharmaceuticals Resistance-repellent retroviral protease inhibitors
EP2316469A1 (en) 2002-02-22 2011-05-04 Shire LLC Delivery system and methods for protecting and administering dextroamphetamine
US7157489B2 (en) * 2002-03-12 2007-01-02 The Board Of Trustees Of The University Of Illinois HIV protease inhibitors
AU2003228707A1 (en) 2002-04-26 2003-11-10 Gilead Sciences, Inc. Method and compositions for identifying anti-hiv therapeutic compounds
SI1517899T1 (sl) * 2002-05-17 2008-02-29 Tibotec Pharm Ltd Substituirani benzoksazol sulfonamidi sirokega spektra, ki so HIV proteazni inhibitorji
US7115652B2 (en) * 2002-06-17 2006-10-03 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
CA2489095A1 (en) * 2002-06-17 2003-12-24 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
PL375307A1 (en) * 2002-08-14 2005-11-28 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
SI1546088T1 (sl) * 2002-10-03 2015-04-30 Novaremed Ltd. Spojine za uporabo v zdravljenju avtoimunskih bolezni, imunoalergijskih bolezni in zavrnitve transpalantata organa ali tkiva
US6713639B1 (en) 2002-10-28 2004-03-30 Council Of Scientific And Industrial Research Process for preparing enantiomerically pure (S)-3-hydroxy-gamma-butyrolactone
WO2004043916A1 (en) * 2002-11-12 2004-05-27 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
WO2004050609A1 (en) * 2002-11-27 2004-06-17 Elan Pharmaceutical, Inc. Substituted ureas and carbamates
US7452901B2 (en) 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
CA2522845A1 (en) * 2003-04-25 2004-11-11 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
US7300924B2 (en) * 2003-04-25 2007-11-27 Gilead Sciences, Inc. Anti-infective phosphonate analogs
US20090247488A1 (en) * 2003-04-25 2009-10-01 Carina Cannizzaro Anti-inflammatory phosphonate compounds
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
WO2005002626A2 (en) * 2003-04-25 2005-01-13 Gilead Sciences, Inc. Therapeutic phosphonate compounds
US7407965B2 (en) * 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
EA014685B1 (ru) 2003-04-25 2010-12-30 Джилид Сайэнс, Инк. Фосфонатсодержащие антивирусные соединения (варианты) и фармацевтическая композиция на их основе
US7432261B2 (en) * 2003-04-25 2008-10-07 Gilead Sciences, Inc. Anti-inflammatory 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
US7470724B2 (en) * 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
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
WO2005044279A1 (en) * 2003-10-24 2005-05-19 Gilead Sciences, Inc. Purine nucleoside phosphonate conjugates
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
US20070281907A1 (en) * 2003-12-22 2007-12-06 Watkins William J Kinase Inhibitor Phosphonate Conjugates
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
ME01059B (me) 2003-12-23 2012-10-20 Janssen Sciences Ireland Uc 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
CA2560922C (en) * 2004-03-26 2014-01-07 New Era Biotech, Ltd. Improvements in or relating to compounds for use in the treatment of aids and other viral diseases and hiv-related infections and compositions containing such compounds, methods of treating such diseases and infections and methods of making such compounds and compositions
HRP20110527T1 (hr) 2004-07-27 2011-08-31 Gilead Sciences Nukleozid-fosfonatni konjugati kao sredstva protiv hiv-a
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
US20080125432A1 (en) 2004-12-01 2008-05-29 Devgen Nv 5-Carboxamido Substituted Thiazole Derivatives that Interact With Ion Channels, In Particular With Ion Channels From the Kv Family
WO2006063848A1 (en) 2004-12-17 2006-06-22 Devgen N.V. Nematicidal compositions
WO2006104646A1 (en) * 2005-03-11 2006-10-05 Smithkline Beecham Corporation 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
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
SI2152667T1 (sl) 2007-04-27 2011-06-30 Tibotec Pharm Ltd Postopki za pripravo N-izobutil-N(2-hidroksi-3-amino-4-fenilbutil)-p- nitrobenzensulfonilamidnih derivatov
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
US20100093811A1 (en) * 2007-09-25 2010-04-15 Coburn Craig A Hiv protease inhibitors
GB0804213D0 (en) * 2008-03-06 2008-04-16 New Era Biotech Ltd A method of printing or preventing pain
US9095620B2 (en) * 2008-03-12 2015-08-04 Nektar Therapeutics Reagents
EP2116236A1 (en) 2008-04-21 2009-11-11 Université de Mons-Hainaut Bisbenzamidine derivatives for use as antioxidant
DK2292592T3 (da) * 2008-06-05 2012-10-08 Asahi Kasei Pharma Corp Sulfonamidforbindelse og anvendelse deraf
WO2010002994A1 (en) 2008-07-01 2010-01-07 Purdue Research Foundation Nonpeptide hiv-1 protease inhibitors
KR101642527B1 (ko) 2008-07-08 2016-07-25 길리애드 사이언시즈, 인코포레이티드 Ｈｉｖ 억제제 화합물의 염
AU2010254415B2 (en) 2009-05-27 2013-07-04 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
WO2011100528A2 (en) 2010-02-12 2011-08-18 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
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
CA2803697A1 (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
EP2605804B1 (en) 2010-08-18 2017-03-15 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
WO2012032389A2 (en) * 2010-09-10 2012-03-15 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
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
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
CA2827392A1 (en) 2011-02-24 2012-08-30 Emory University Noggin blocking compositions for ossification and methods related thereto
US9365523B2 (en) 2011-03-31 2016-06-14 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
JP2014518859A (ja) 2011-05-09 2014-08-07 ユニバーシタット アントウェルペン ウロキナーゼプラスミノーゲン活性化因子に対する活性依存型プローブ
GB201108225D0 (en) 2011-05-17 2011-06-29 Amakem Nv Novel KBC inhibitors
WO2012177618A1 (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
EP2744775B1 (en) 2011-08-19 2018-03-07 Emory University Bax agonist, compositions, and methods related thereto
GB201114854D0 (en) 2011-08-29 2011-10-12 Amakem Nv Novel rock inhibitors
SG11201400117QA (en) 2011-08-31 2014-03-28 Amakem Nv Novel soft rock inhibitors
KR20140095477A (ko) 2011-09-30 2014-08-01 입센 파마 에스.에이.에스 마크로시클릭 lrrk2 키나제 억제제
MX347765B (es) 2011-09-30 2017-05-12 Oncodesign Sa Inhibidores macrociclicos de la quinasa flt3.
US9133157B2 (en) 2011-10-26 2015-09-15 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
US9290427B2 (en) 2012-01-30 2016-03-22 Universiteit Gent Anti-invasive compounds
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
CN104755475B (zh) 2012-09-11 2016-12-28 默沙东公司 Hiv蛋白酶抑制剂
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
CA2889903C (en) 2012-10-29 2021-03-09 Manjinder Singh Phull Antiviral phosphonate analogues and process for preparation thereof
CN104812744B (zh) 2012-11-05 2017-12-01 爱默蕾大学 7,8‑二羟黄酮和7,8‑取代的黄酮衍生物、组合物及其相关方法
WO2014072419A1 (en) 2012-11-08 2014-05-15 Universiteit Antwerpen Novel anti-hiv compounds
HUE033962T2 (en) 2013-01-29 2018-01-29 Redx Pharma Plc Pyridine derivatives as soft rock (RHO kinase) inhibitors
SG11201507493SA (en) 2013-03-15 2015-10-29 Oncodesign Sa Macrocyclic salt-inducible kinase inhibitors
WO2015013835A1 (en) 2013-07-31 2015-02-05 Merck Sharp & Dohme Corp. Piperazine derivatives as hiv protease inhibitors
EP4094767A1 (en) 2013-09-11 2022-11-30 Emory University Nucleotide and nucleoside therapeutic compositions and uses related thereto
US10188738B2 (en) 2013-10-16 2019-01-29 Université Libre de Bruxelles Formulations useful in the treatment of proliferative diseases affecting the respiratory tract
CA3191243A1 (en) 2013-11-12 2015-05-21 Vrije Universiteit Brussel Rna transcription vector and uses thereof
WO2015095276A1 (en) 2013-12-19 2015-06-25 Merck Sharp & Dohme Corp. Hiv protease inhibitors
WO2015134366A1 (en) 2014-03-06 2015-09-11 Merck Sharp & Dohme Corp. Hiv protease inhibitors
WO2015150337A1 (en) 2014-04-01 2015-10-08 Amakem Nv Lim kinase inhibitors
US20170165240A1 (en) 2014-04-01 2017-06-15 Université Libre de Bruxelles New strategies for treating melanoma
AU2015256266B2 (en) 2014-05-05 2019-01-17 Emory University BH4 antagonists and methods related thereto
WO2015175855A1 (en) 2014-05-16 2015-11-19 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
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
WO2016042087A1 (en) 2014-09-17 2016-03-24 Oncodesign S.A. 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
CN107428792B (zh) 2014-12-15 2023-01-24 埃默里大学 用于治疗乙型肝炎病毒的磷酰胺
CA2972259A1 (en) 2014-12-26 2016-06-30 Emory University 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
EP3288637B1 (en) 2015-04-28 2022-09-14 NewSouth Innovations Pty Limited Targeting nad+ to treat chemotherapy and radiotherapy induced cognitive impairment, neuropathies and inactivity
US10555918B2 (en) 2015-05-29 2020-02-11 Emory University 2-amino-N′-benzylideneacetohydrazides and derivatives for the management of CFTR protein mediated diseases
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
US11192914B2 (en) 2016-04-28 2021-12-07 Emory University Alkyne containing nucleotide and nucleoside therapeutic compositions and uses related thereto
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
WO2018071911A1 (en) 2016-10-14 2018-04-19 Emory University Nanoparticles having molecules that bind or block pd-l1 and uses in treating cancer
WO2018081442A1 (en) 2016-10-26 2018-05-03 Emory University Polyoxometalate complexes and uses in managing cancer
US10738002B2 (en) 2016-11-24 2020-08-11 Universitair Ziekenhuis Antwerpen Halogenated benzotropolones as ATG4B inhibitors
US10898544B2 (en) 2016-12-13 2021-01-26 Emory University Polypeptides for managing viral infections
EP3573608A1 (en) 2017-01-30 2019-12-04 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
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
US11548881B2 (en) 2017-05-11 2023-01-10 Remynd N.V. Compounds for the treatment of epilepsy, neurodegenerative disorders and other CNS disorders
US10851125B2 (en) 2017-08-01 2020-12-01 Gilead Sciences, Inc. Crystalline forms of ethyl ((S)-((((2R,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-2,5-dihydrofuran-2-yl)oxy)methyl)(phenoxy)phosphoryl(-L-alaninate
RU2761436C1 (ru) 2017-11-17 2021-12-08 Целликс Био Прайвет Лимитед Композиции и способы лечения нарушений со стороны органа зрения
WO2019113462A1 (en) 2017-12-07 2019-06-13 Emory University N4-hydroxycytidine and derivatives and anti-viral uses related thereto
WO2019193091A1 (en) 2018-04-05 2019-10-10 Universiteit Hasselt Selective pde4d inhibitors against demyelinating diseases
MA53007A (fr) 2018-06-29 2021-05-05 Rejuvenate Biomed Association pharmaceutique destinée à être utilisée dans des maladies liées à l'âge et/ou dégénératives
PL3833343T3 (pl) 2018-08-07 2024-06-24 Emory University Heterocykliczne pochodne flawonu, kompozycje, i sposoby z nimi związane
WO2020047229A1 (en) 2018-08-29 2020-03-05 University Of Massachusetts Inhibition of protein kinases to treat friedreich ataxia
EP3941916B1 (en) 2019-03-20 2025-10-01 Emory University Prostaglandin receptor ep2 antagonists, derivatives, and uses related thereto
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
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
WO2021209563A1 (en) 2020-04-16 2021-10-21 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
US20240368133A1 (en) 2021-07-30 2024-11-07 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
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
EP4405357A1 (en) 2021-09-23 2024-07-31 Katholieke Universiteit Leuven KU Leuven Research & Development 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
US20240025885A1 (en) 2022-07-08 2024-01-25 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

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
WO1990007329A1 (en) 1989-01-06 1990-07-12 The Regents Of The University Of California Selection method for pharmacologically active 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 (en, 2012) * 1990-06-28 1994-06-21 Shionogi & Co
DK0558630T3 (da) 1990-11-19 1998-05-11 Monsanto Co Retrovirale proteaseinhibitorer
WO1993023388A1 (en) * 1992-05-20 1993-11-25 G.D. Searle & Co. Method for making intermediates useful in synthesis of retroviral protease inhibitors
AU662114B2 (en) 1990-11-19 1995-08-24 Monsanto Company Retroviral protease inhibitors
DE69124110T2 (de) * 1990-11-19 1997-06-05 Monsanto Co Retrovirale protease inhibitoren
JPH06503092A (ja) 1990-11-19 1994-04-07 モンサント　カンパニー レトロウイルスプロテアーゼ阻害剤
IE913840A1 (en) * 1990-11-20 1992-05-20 Abbott Lab Retroviral protease inhibiting compounds
ES2112880T3 (es) 1991-11-08 1998-04-16 Merck & Co Inc Inhibidores de la proteasa de vih utiles para el tratamiento del sida.
WO1993023379A1 (en) * 1992-05-21 1993-11-25 Monsanto Company Retroviral protease inhibitors
EP0656887B1 (en) * 1992-08-25 1998-10-28 G.D. Searle & Co. Hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
WO1994004491A1 (en) * 1992-08-25 1994-03-03 G.D. Searle & Co. N-(alkanoylamino-2-hydroxypropyl)-sulfonamides useful as retroviral protease inhibitors
ATE161828T1 (de) * 1992-08-25 1998-01-15 Searle & Co Sulfonylalkanoylaminohydroxyethylaminosulfonami e verwendbar als retrovirale protease-inhibitoren
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
DE69331421T2 (de) * 1992-10-30 2002-08-01 G.D. SEARLE & CO., CHICAGO N-substituierte Hydroxyethylaminosulfamidsäure-Derivate verwendbar als Inhibitoren retroviraler Proteasen
EP0885881B1 (en) * 1992-10-30 2003-03-12 G.D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfamic acids useful as retroviral protease inhibitors
WO1994018192A1 (en) * 1993-02-12 1994-08-18 Merck & Co., Inc. Piperazine derivatives as hiv protease inhibitors
MY128102A (en) * 1993-02-17 2007-01-31 Chugai Pharmaceutical Co Ltd Indolin-2-one-derivatives

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DE10199024I2 (de) 2006-04-06
CA2143208C (en) 2003-01-07
ES2131589T3 (es) 1999-08-01
JPH08501299A (ja) 1996-02-13
GR3030719T3 (en) 1999-11-30
MY142901A (en) 2011-01-31
DK0885887T3 (da) 2003-09-22
HUT71892A (en) 1996-02-28
AP9300572A0 (en) 1993-10-31
IS2334B (is) 2008-02-15
DE10199024I1 (de) 2001-07-12
DE69333012D1 (de) 2003-07-03
LT3302B (en) 1995-06-26
PH31251A (en) 1998-05-05
HU228198B1 (en) 2013-01-28
NL300039I2 (nl) 2001-09-03
BR1100824A (pt) 1999-08-31
GEP20012579B (en) 2001-11-26
TW254927B (en, 2012) 1995-08-21
KR100262056B1 (ko) 2000-07-15
PL307858A1 (en) 1995-06-26
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US20030069222A1 (en) 2003-04-10
IS4068A (is) 1994-03-09
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WO1994005639A1 (en) 1994-03-17
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EP0659181A1 (en) 1995-06-28
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UA44694C2 (uk) 2002-03-15
LU90736I2 (fr) 2001-05-07
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SK29395A3 (en) 1995-09-13
ATE178598T1 (de) 1999-04-15

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