MXPA03010538A - Nuevas formulaciones que inhiben la proteasa aspartilo. - Google Patents
Nuevas formulaciones que inhiben la proteasa aspartilo.Info
- Publication number
- MXPA03010538A MXPA03010538A MXPA03010538A MXPA03010538A MXPA03010538A MX PA03010538 A MXPA03010538 A MX PA03010538A MX PA03010538 A MXPA03010538 A MX PA03010538A MX PA03010538 A MXPA03010538 A MX PA03010538A MX PA03010538 A MXPA03010538 A MX PA03010538A
- Authority
- MX
- Mexico
- Prior art keywords
- hiv
- aspartyl protease
- relates
- compounds
- activity
- Prior art date
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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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- 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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- C07C311/16—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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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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Abstract
La presente invención se refiere a una nueva clase de sulfonamidas, las cuales son inhibidoras de las proteasa aspartilo, en una de sus modalidades, la presente invención se refiere a una nueva clase de inhibidores de la proteasa aspartilo de VIH caracterizados por sus características estructurales especificas y fisicoquímicas La presente invención también se refiere a composiciones farmaceúricas que comprenden estos compuestos. Los compuestos y las composiciones farmacéuticas de la presente invención son particularmente bien adecuados para la inhibición de la actividad de las proteasas VIH-1 y VIH-2 y consecuentemente, pueden ser usados de manera provechosa como agentes antivirales contra los viruses VIH-1 y VIH-2. Esta invención también se refiere a los métodos para inhibir la actividad de la proteasa aspartilo VIH usando los compuestos de la presente invención y a los metodos para proteger los compuestos para la actividad anti- VIH.
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Families Citing this family (301)
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 |
EP0633534B1 (en) * | 1992-03-27 | 2001-02-07 | ITAI, Akiko | Method of searching the structure of stable biopolymer-ligand molecule composite |
US5968942A (en) | 1992-08-25 | 1999-10-19 | G. D. Searle & Co. | α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors |
KR100296463B1 (ko) | 1992-08-25 | 2001-10-24 | 죤 에이치. 뷰센 | 레트로바이러스프로테아제저해제로서유용한히드록시에틸아미노술폰아미드 |
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 |
US7141609B2 (en) | 1992-08-25 | 2006-11-28 | G.D. Searle & Co. | α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors |
US5723490A (en) * | 1992-09-08 | 1998-03-03 | Vertex Pharmaceuticals Incorporated | THF-containing sulfonamide inhibitors of aspartyl protease |
IS2334B (is) * | 1992-09-08 | 2008-02-15 | Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) | Aspartyl próteasi hemjari af nýjum flokki súlfonamíða |
US5783701A (en) * | 1992-09-08 | 1998-07-21 | Vertex Pharmaceuticals, Incorporated | Sulfonamide inhibitors of aspartyl protease |
CA2143191A1 (en) * | 1992-10-30 | 1994-05-11 | Michael L. Vazquez | Sulfonylalkanoylamino hydroxyethylamino sulfamic acids useful as retroviral protease inhibitors |
DK0666842T3 (da) * | 1992-10-30 | 1998-11-02 | Searle & Co | Hydroxyethylaminosulfaminsyrederivater til anvendelse som inhibitorer af retrovirale proteaser |
US5484926A (en) * | 1993-10-07 | 1996-01-16 | Agouron Pharmaceuticals, Inc. | HIV protease inhibitors |
US5846993A (en) * | 1992-12-22 | 1998-12-08 | Agouron Pharmaceuticals, Inc. | HIV protease inhibitors |
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 |
US6541498B2 (en) | 1993-05-20 | 2003-04-01 | Texas Biotechnology | 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 |
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 |
AU4700896A (en) | 1995-01-20 | 1996-08-07 | G.D. Searle & Co. | Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors |
US5831117A (en) | 1995-01-20 | 1998-11-03 | G. D. Searle & Co. | Method of preparing retroviral protease inhibitor intermediates |
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 |
US6861539B1 (en) | 1995-03-10 | 2005-03-01 | G. D. Searle & Co. | 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 |
EP1188766A1 (en) | 1995-03-10 | 2002-03-20 | 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 |
US6407134B1 (en) | 1995-03-10 | 2002-06-18 | G. D. Searle & Co. | Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
CN1149223C (zh) * | 1995-03-10 | 2004-05-12 | G·D·瑟尔公司 | 杂环羰基氨基酸羟乙氨基磺酰胺逆转录病毒蛋白酶抑制剂 |
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 |
US5767316A (en) | 1995-11-17 | 1998-06-16 | Ajinomoto Co., Inc. | Process for producing 3-amino-2-oxo-1-halogenopropane derivatives |
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 |
ATE230602T1 (de) * | 1996-03-22 | 2003-01-15 | Glaxo Group Ltd | Zubereitung, enthaltend vx 478 und eine wasserlösliche vitamin e verbindung wie 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 |
IL127350A0 (en) * | 1996-06-25 | 1999-10-28 | Glaxo Group Ltd | Combinations comprising VX478 zidovudine and/or 1592U89 for use in the treatment of HIV |
CO4900074A1 (es) * | 1996-06-25 | 2000-03-27 | Glaxo Group Ltd | Combinaciones antivirales |
US5925759A (en) | 1996-09-05 | 1999-07-20 | Agouron Pharmaceuticals, Inc. | Methods of making HIV-protease inhibitors and intermediates for making HIV-protease inhibitors |
US5705647A (en) * | 1996-09-05 | 1998-01-06 | Agouron Pharmaceuticals, Inc. | Intermediates for making HIV-protease inhibitors |
US5962725A (en) | 1996-09-05 | 1999-10-05 | Agouron Pharmaceuticals, Inc. | Intermediate compounds useful for making HIV protease inhibitors such as nelfinavir |
US5786378A (en) * | 1996-09-25 | 1998-07-28 | Gpi Nil Holdings, Inc. | Heterocyclic thioesters |
US5801187A (en) | 1996-09-25 | 1998-09-01 | Gpi-Nil Holdings, Inc. | Heterocyclic esters and amides |
US6218424B1 (en) | 1996-09-25 | 2001-04-17 | Gpi Nil Holdings, Inc. | Heterocyclic ketone and thioester compounds and uses |
IN183408B (es) * | 1996-11-20 | 1999-12-25 | Kuraray Co | |
US6232333B1 (en) | 1996-11-21 | 2001-05-15 | Abbott Laboratories | Pharmaceutical composition |
ZA9710071B (en) * | 1996-11-21 | 1998-05-25 | Abbott Lab | Pharmaceutical composition. |
SK57899A3 (en) * | 1996-12-31 | 2000-05-16 | Guilford Pharm Inc | N-linked ureas and carbamates of heterocyclic thioesters |
US6121273A (en) * | 1996-12-31 | 2000-09-19 | Gpi Nil Holdings, Inc | N-linked sulfonamides of heterocyclic thioesters |
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 |
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 |
ES2241133T3 (es) | 1997-04-28 | 2005-10-16 | Encysive Pharmaceuticals Inc. | Sulfamidas para el tratamiento de los trastornos inducidos por la endotelina. |
JP2002512621A (ja) * | 1997-05-08 | 2002-04-23 | スミスクライン・ビーチャム・コーポレイション | プロテアーゼ阻害剤 |
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 |
US5945441A (en) | 1997-06-04 | 1999-08-31 | Gpi Nil Holdings, Inc. | Pyrrolidine carboxylate hair revitalizing agents |
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 |
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 |
WO1999033793A2 (en) * | 1997-12-24 | 1999-07-08 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
AU2012199A (en) * | 1997-12-24 | 1999-07-19 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
US6436989B1 (en) * | 1997-12-24 | 2002-08-20 | Vertex Pharmaceuticals, Incorporated | Prodrugs of aspartyl protease inhibitors |
AU2010299A (en) * | 1997-12-24 | 1999-07-19 | Vertex Pharmaceuticals Incorporated | Prodrugs os aspartyl protease inhibitors |
GB9805898D0 (en) * | 1998-03-20 | 1998-05-13 | Glaxo Group Ltd | Process for the sythesis of hiv protease inhibitors |
US6251906B1 (en) | 1998-05-15 | 2001-06-26 | Abbott Laboratories | Retroviral protease inhibiting compounds |
CA2334204A1 (en) | 1998-06-03 | 1999-12-09 | Gpi Nil Holdings, Inc. | Heterocyclic ester and amide hair growth compositions and uses |
ZA9811060B (en) | 1998-06-03 | 1999-12-03 | Guilford Pharm Inc | 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 |
US6331537B1 (en) | 1998-06-03 | 2001-12-18 | Gpi Nil Holdings, Inc. | Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds |
PT1086076E (pt) | 1998-06-19 | 2005-05-31 | Vertex Pharma | Inibidores de sulfonamida de aspartil protease |
EP1088098B2 (en) | 1998-06-23 | 2015-07-01 | THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES | Fitness assay and methods for reducing resistance of hiv to therapy |
EP1095022A1 (en) | 1998-07-08 | 2001-05-02 | 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 |
CA2338752A1 (en) * | 1998-07-24 | 2000-02-03 | Samsung Fine Chemicals Co., Ltd. | Process for preparing optically pure (s)-3,4-dihydroxybutyric acid derivatives |
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 |
US6218423B1 (en) | 1998-08-14 | 2001-04-17 | Gpi Nil Holdings, Inc. | Pyrrolidine 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 |
US6376517B1 (en) | 1998-08-14 | 2002-04-23 | Gpi Nil Holdings, Inc. | Pipecolic acid derivatives for vision and memory disorders |
US6333340B1 (en) | 1998-08-14 | 2001-12-25 | Gpi Nil Holdings, Inc. | Small molecule sulfonamides for vision and memory disorders |
US6399648B1 (en) | 1998-08-14 | 2002-06-04 | Gpi Nil Holdings, Inc. | N-oxides of heterocyclic ester, amide, thioester, or ketone for vision and memory disorders |
US6395758B1 (en) | 1998-08-14 | 2002-05-28 | Gpi Nil Holdings, Inc. | Small molecule carbamates or ureas 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 |
US7338976B1 (en) | 1998-08-14 | 2008-03-04 | Gpi Nil Holdings, Inc. | Heterocyclic esters or amides 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 |
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 |
EP1159278B1 (en) * | 1999-02-12 | 2005-11-30 | Vertex Pharmaceuticals Incorporated | Inhibitors of aspartyl protease |
CO5261510A1 (es) | 1999-02-12 | 2003-03-31 | Vertex Pharma | Inhibidores de aspartil proteasa |
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 |
KR100792391B1 (ko) | 1999-10-06 | 2008-01-08 | 티보텍 파마슈티칼즈 리미티드 | 레트로바이러스 프로테아제 저해제로서의헥사하이드로푸로[2,3-b]푸란-3-일-N-[3-[(1,3-벤조디옥솔-5-일설포닐)(이소부틸)아미노]-1-벤질-2-하이드록시프로필]카바메이트 |
EP1244610B1 (en) | 1999-12-23 | 2008-07-16 | 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 |
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 |
CZ304273B6 (cs) * | 2001-02-14 | 2014-02-12 | Tibotec Pharmaceuticals Ltd. | 2-(Substitovaná-amino)benzothiazolsulfonamidová sloučenina, způsob její přípravy a farmaceutická kompozice s jejím obsahem |
US6756063B2 (en) | 2001-03-29 | 2004-06-29 | Zoltan Laboratories, Llc | Methods and compositions for the treatment of human and animal cancers |
MXPA03009179A (es) | 2001-04-09 | 2004-11-22 | Tibotec Pharm Ltd | 2-(amino sustituido)-benzoxazol sunfonamidas, inhibidores de amplio espectro de la vih proteasa. |
US6696494B2 (en) | 2001-10-22 | 2004-02-24 | Enanta Pharmaceuticals, Inc. | α-hydroxyarylbutanamine inhibitors of aspartyl protease |
CA2472580A1 (en) * | 2002-01-07 | 2003-07-17 | Sequoia Pharmaceuticals | Broad spectrum inhibitors |
CA2477088A1 (en) | 2002-02-22 | 2003-10-02 | 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 |
JP2005523922A (ja) | 2002-04-26 | 2005-08-11 | ギリアード サイエンシーズ, インコーポレイテッド | 非ヌクレオシド逆転写酵素阻害剤 |
US7462636B2 (en) * | 2002-05-17 | 2008-12-09 | Tibotec Pharmaceuticals Ltd | Broadspectrum substituted benzisoxazole sulfonamide HIV protease inhibitors |
US7115652B2 (en) * | 2002-06-17 | 2006-10-03 | Sunesis Pharmaceuticals, Inc. | Aspartyl protease inhibitors |
EP1515944A1 (en) * | 2002-06-17 | 2005-03-23 | Sunesis Pharmaceuticals, Inc. | Aspartyl protease inhibitors |
EP1546153A1 (en) * | 2002-08-14 | 2005-06-29 | 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 |
CA2500935C (en) * | 2002-10-03 | 2014-09-23 | New Era Biotech, Ltd. | Novel 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 |
JP4494212B2 (ja) | 2002-11-12 | 2010-06-30 | メルク・シャープ・エンド・ドーム・コーポレイション | アルツハイマー病の治療用フェニルカルボキサミドベータセクレターゼ阻害剤 |
US7351738B2 (en) * | 2002-11-27 | 2008-04-01 | Elan Pharmaceuticals, Inc. | Substituted ureas and carbamates |
US7300924B2 (en) * | 2003-04-25 | 2007-11-27 | Gilead Sciences, Inc. | Anti-infective phosphonate analogs |
CN101410120A (zh) * | 2003-04-25 | 2009-04-15 | 吉里德科学公司 | 抗炎的膦酸酯化合物 |
US7427636B2 (en) * | 2003-04-25 | 2008-09-23 | Gilead Sciences, Inc. | Inosine monophosphate dehydrogenase inhibitory phosphonate compounds |
CA2522845A1 (en) * | 2003-04-25 | 2004-11-11 | Gilead Sciences, Inc. | Kinase inhibitor phosphonate conjugates |
WO2005002626A2 (en) * | 2003-04-25 | 2005-01-13 | Gilead Sciences, Inc. | Therapeutic phosphonate compounds |
US7470724B2 (en) * | 2003-04-25 | 2008-12-30 | Gilead Sciences, Inc. | Phosphonate compounds having immuno-modulatory activity |
US7429565B2 (en) * | 2003-04-25 | 2008-09-30 | Gilead Sciences, Inc. | Antiviral phosphonate analogs |
US7432261B2 (en) * | 2003-04-25 | 2008-10-07 | Gilead Sciences, Inc. | Anti-inflammatory phosphonate compounds |
US20050261237A1 (en) * | 2003-04-25 | 2005-11-24 | Boojamra Constantine G | Nucleoside phosphonate analogs |
US7407965B2 (en) * | 2003-04-25 | 2008-08-05 | Gilead Sciences, Inc. | Phosphonate analogs for treating metabolic diseases |
US20090247488A1 (en) * | 2003-04-25 | 2009-10-01 | Carina Cannizzaro | Anti-inflammatory phosphonate compounds |
US7452901B2 (en) * | 2003-04-25 | 2008-11-18 | Gilead Sciences, Inc. | Anti-cancer 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 |
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 |
WO2005044308A1 (en) * | 2003-10-24 | 2005-05-19 | Gilead Sciences, Inc. | Phosphonate analogs of antimetabolites |
WO2005044279A1 (en) * | 2003-10-24 | 2005-05-19 | Gilead Sciences, Inc. | Purine nucleoside phosphonate conjugates |
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 |
US20080287471A1 (en) * | 2003-12-22 | 2008-11-20 | Maria Fardis | 4'-Substituted Carbovir And Abacavir-Derivatives As Well As Related Compounds With Hiv And Hcv Antiviral Activity |
US20050153990A1 (en) * | 2003-12-22 | 2005-07-14 | Watkins William J. | Phosphonate substituted kinase inhibitors |
BRPI0418031A (pt) * | 2003-12-22 | 2007-04-17 | Gilead Sciences Inc | inibidores de quinase fosfonato-substituìdos |
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 |
EP1750691B1 (en) * | 2004-03-26 | 2016-08-10 | Novaremed Ltd. | Compounds for treatment of aids and other diseases |
SI2258376T1 (sl) | 2004-07-27 | 2019-04-30 | Gilead Sciences, Inc. | Analogi fosfonata spojin inhibitorjev HIV |
US20060135510A1 (en) * | 2004-10-13 | 2006-06-22 | The Trustees Of The University Of Pennsylvania | Use of amprenavir as a radiation sensitizer |
US20060116397A1 (en) * | 2004-10-13 | 2006-06-01 | The Trustees Of The University Of Pennsylvania | Use of saquinavir as a radiation sensitizer |
BRPI0516915A (pt) | 2004-12-01 | 2008-03-11 | Devgen Nv | derivados de tiazol substituìdos por 5-carboxamido que interagem com canais de ìons, particularmante com canais de ìons da famìlia kv |
DK1941798T3 (da) * | 2004-12-17 | 2012-08-27 | Devgen Nv | Nematicide præparater |
US20080194554A1 (en) * | 2005-03-11 | 2008-08-14 | Mclean Ed W | Hiv Protease Inhibitors |
US20080009517A1 (en) * | 2005-10-13 | 2008-01-10 | The Trustees Of The University Of Pennsylvania | Use of nelfinavir as a radiation sensitizer |
JP5225264B2 (ja) * | 2006-05-09 | 2013-07-03 | ノベアメド・リミテッド | 細胞増殖障害の処置 |
JP5448854B2 (ja) | 2007-03-12 | 2014-03-19 | ウェルズ ファーゴ バンク ナショナル アソシエイション | オリゴマー−プロテアーゼ阻害剤複合体 |
CA2682616A1 (en) | 2007-04-27 | 2008-11-06 | Tibotec Pharmaceuticals Ltd. | Methods for the preparation of n-isobutyl-n-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide derivatives |
US20090075942A1 (en) * | 2007-09-13 | 2009-03-19 | Protia, Llc | Deuterium-enriched fosamprenavir |
GB2452952A (en) * | 2007-09-20 | 2009-03-25 | Npil Pharmaceuticals | N-[2-Hydroxy-3-(hydroxycarbonylamino)-3-methyl]-N-methyl-sulphonamide derivatives via N-[2-oxo-3-(hydroxycarbonylamino)-3-methyl]-N-methyl-imine skeleton |
JP2010540517A (ja) * | 2007-09-25 | 2010-12-24 | メルク・シャープ・エンド・ドーム・コーポレイション | Hivプロテアーゼ阻害剤 |
GB0804213D0 (en) * | 2008-03-06 | 2008-04-16 | New Era Biotech Ltd | A method of printing or preventing pain |
WO2009114151A1 (en) * | 2008-03-12 | 2009-09-17 | Nektar Therapeutics | Oligomer-amino acid and olgomer-atazanavir conjugates |
EP2116236A1 (en) | 2008-04-21 | 2009-11-11 | Université de Mons-Hainaut | Bisbenzamidine derivatives for use as antioxidant |
KR101479371B1 (ko) * | 2008-06-05 | 2015-01-05 | 아사히 가세이 파마 가부시키가이샤 | 술폰아미드 화합물 및 그 용도 |
EP2307345A4 (en) | 2008-07-01 | 2012-05-02 | Purdue Research Foundation | NON-PEPTIDINHIBITORS OF HIV-1 PROTEASE |
EP2307435B1 (en) | 2008-07-08 | 2012-06-13 | Gilead Sciences, Inc. | Salts of hiv inhibitor compounds |
EP2435037B1 (en) | 2009-05-27 | 2014-11-12 | Merck Sharp & Dohme Corp. | Hiv protease inhibitors |
EP2440249A2 (en) | 2009-06-12 | 2012-04-18 | Nektar Therapeutics | Covalent conjugates comprising a protease inhibitor, a water-soluble, non-peptidic oligomer and a lipophilic moiety |
US8802734B2 (en) * | 2009-09-09 | 2014-08-12 | Novaremed Limited | Method of treating or preventing pain |
WO2011061590A1 (en) | 2009-11-17 | 2011-05-26 | Hetero Research Foundation | Novel carboxamide derivatives as hiv inhibitors |
DE102010004957A1 (de) | 2010-01-14 | 2011-07-21 | Universitätsklinikum Jena, 07743 | Biologisch wirksame Moleküle zur Beeinflussung von Virus-, Bakterien-, Parasiten-infizierten Zellen und/oder Tumorzellen und Verfahren zu deren Anwendung |
WO2011100528A2 (en) | 2010-02-12 | 2011-08-18 | Emory University | Compositions and uses of lectins |
PL2542528T3 (pl) | 2010-03-02 | 2013-11-29 | Amakem Nv | Heterocykliczne amidy jako inhibitory ROCK |
CN102190638A (zh) * | 2010-03-16 | 2011-09-21 | 中国科学院上海药物研究所 | 联芳基醇二胺类化合物、其药物组合物、制备方法及应用 |
WO2011156594A2 (en) | 2010-06-09 | 2011-12-15 | Vaccine Technologies, Incorporated | Therapeutic immunization in hiv infected subjects receiving stable antiretroviral treatment |
WO2011161256A1 (en) | 2010-06-25 | 2011-12-29 | Facultes Universitaires Notre Dame De La Paix | Beta carboline derivatives useful in the treatment of proliferative disorders |
US8785648B1 (en) | 2010-08-10 | 2014-07-22 | The Regents Of The University Of California | PKC-epsilon inhibitors |
CA3052927C (en) | 2010-08-18 | 2023-01-03 | Scott D. Boden | 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 |
US8877947B2 (en) | 2010-09-10 | 2014-11-04 | Lupin Limited | Process for preparation of substantially pure fosamprenavir calcium and its intermediates |
EP2632895B1 (en) | 2010-10-28 | 2018-10-03 | Merck Canada Inc. | Hiv protease inhibitors |
WO2012058211A2 (en) | 2010-10-29 | 2012-05-03 | 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 |
US8969381B2 (en) | 2010-12-03 | 2015-03-03 | 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 |
WO2012116135A2 (en) | 2011-02-24 | 2012-08-30 | Emory University | Noggin blocking compositions for ossification and methods related thereto |
US11179500B2 (en) | 2011-02-24 | 2021-11-23 | Emory University | JAB1 inhibitory compositions for ossification and methods related thereto |
EP2691095B1 (en) | 2011-03-31 | 2017-07-05 | 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 |
CA2835217A1 (en) | 2011-05-09 | 2012-11-15 | Universiteit Antwerpen | Activity-based probes for the urokinase plasminogen activator |
GB201108225D0 (en) | 2011-05-17 | 2011-06-29 | Amakem Nv | Novel KBC inhibitors |
US9518044B2 (en) | 2011-06-20 | 2016-12-13 | 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 |
AU2012300834A1 (en) | 2011-08-31 | 2014-04-17 | Amakem Nv | Biphenylcarboxamides as ROCK kinase inhibitors |
ES2569048T3 (es) | 2011-09-30 | 2016-05-06 | Oncodesign S.A. | Inhibidores de quinasa FLT3 macrocíclica |
BR112014007654A8 (pt) | 2011-09-30 | 2018-06-12 | Ipsen Pharma | Inibidores de lrrk2 quinase macrocíclicos. |
WO2013059928A1 (en) | 2011-10-26 | 2013-05-02 | Merck Canada Inc. | Hiv protease inhibitors |
GB201119358D0 (en) | 2011-11-10 | 2011-12-21 | Lewi Paulus J | Disubstituted triazine dimers for treatment and/or prevention of infectious diseases |
ES2958619T3 (es) | 2012-01-30 | 2024-02-12 | Univ Gent | Compuestos anti-invasivos |
GB201204756D0 (en) | 2012-03-19 | 2012-05-02 | Lewi Paulus J | Triazines with suitable spacers for treatment and/or prevention of HIV infections |
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 |
KR20150053971A (ko) | 2012-09-11 | 2015-05-19 | 머크 샤프 앤드 돔 코포레이션 | Hiv 프로테아제 억제제 |
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 |
EP2912047B1 (en) | 2012-10-29 | 2016-08-24 | Cipla Limited | Antiviral phosphonate analogues and process for preparation thereof |
AU2013337742B2 (en) | 2012-11-05 | 2017-11-23 | Emory University | 7,8-dihydoxyflavone and 7,8-substituted flavone derivatives, compositions, and methods related thereto |
WO2014072419A1 (en) | 2012-11-08 | 2014-05-15 | Universiteit Antwerpen | Novel anti-hiv compounds |
RS56089B1 (sr) | 2013-01-29 | 2017-10-31 | Redx Pharma Plc | Derivati piridina kao lako razgradivi rock inhibitori |
EA201591794A1 (ru) | 2013-03-15 | 2015-12-30 | Онкодизайн С.А. | Макроциклические ингибиторы соль-индуцируемых киназ |
WO2015013835A1 (en) | 2013-07-31 | 2015-02-05 | Merck Sharp & Dohme Corp. | Piperazine derivatives as hiv protease inhibitors |
ES2927955T3 (es) | 2013-09-11 | 2022-11-14 | Univ Emory | Composiciones de nucleótidos y nucleósidos y sus usos |
EP3057619A1 (en) | 2013-10-16 | 2016-08-24 | Université Libre de Bruxelles | Formulations useful in the treatment of proliferative diseases affecting the respiratory tract |
CA2929203C (en) | 2013-11-12 | 2023-04-18 | 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 |
AU2015239108A1 (en) | 2014-04-01 | 2016-10-20 | Institut Jules Bordet | New strategies for treating melanoma |
WO2015150337A1 (en) | 2014-04-01 | 2015-10-08 | Amakem Nv | Lim kinase inhibitors |
WO2015171589A1 (en) | 2014-05-05 | 2015-11-12 | 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 |
WO2016003450A1 (en) | 2014-07-01 | 2016-01-07 | The Regents Of The University Of California | Pkc-epsilon inhibitors |
EP3166955B1 (en) | 2014-07-08 | 2018-05-02 | Universiteit Gent | Hamamelitannin analogues and uses thereof |
MX2017003469A (es) | 2014-09-17 | 2017-05-08 | Oncodesign Sa | Inhibidores macrociclicos de cinasa rip2. |
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 |
US9738664B2 (en) | 2014-10-29 | 2017-08-22 | Wisconsin Alumni Research Foundation | Boronic acid inhibitors of HIV protease |
WO2016083490A1 (en) | 2014-11-27 | 2016-06-02 | Remynd Nv | Compounds for the treatment of amyloid-associated diseases |
SG10202013032YA (en) | 2014-12-15 | 2021-02-25 | Univ Emory | Phosphoramidates for the treatment of hepatitis b virus |
KR20230130175A (ko) | 2014-12-26 | 2023-09-11 | 에모리 유니버시티 | N4-하이드록시시티딘, 이와 관련된 유도체 및 이의 항 바이러스적 용도 |
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 |
EP3804706B1 (en) | 2015-05-29 | 2023-08-23 | Emory University | 2-amino-n'-benzylideneacetohydrazides and derivatives for the management of cftr protein mediated diseases |
AU2017226878B2 (en) | 2016-02-29 | 2020-07-23 | Oncodesign Precision Medicine (OPM) | Radiolabeled macrocyclic EGFR inhibitor |
WO2017157882A1 (en) | 2016-03-14 | 2017-09-21 | Université Catholique de Louvain | Serine biosynthetic pathway inhibitors |
EP3448392A4 (en) | 2016-04-28 | 2020-01-15 | Emory University | ALCYNE-CONTAINING NUCLEOTIDES AND NUCLEOSIDES THERAPEUTIC COMPOSITIONS AND USES THEREOF |
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 (en) | 2016-10-14 | 2020-04-29 | Emory University | NANOPARTICLES WITH MOLECULES FOR BINDING OR BLOCKING PD-L1 AND USED IN THE TREATMENT OF CANCER |
US11331297B2 (en) | 2016-10-26 | 2022-05-17 | Emory University | Polyoxometalate complexes and uses in managing cancer |
EP3544952B1 (en) | 2016-11-24 | 2024-11-06 | Universiteit Antwerpen | Halogenated benzotropolones as atg4b inhibitors |
EP3554533B1 (en) | 2016-12-13 | 2021-06-09 | 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 |
AU2018225556A1 (en) | 2017-02-21 | 2019-10-03 | Emory University | Chemokine CXCR4 receptor modulators and uses related thereto |
CN110650955B (zh) | 2017-05-11 | 2023-07-25 | 瑞敏德股份有限公司 | 用于治疗癫痫、神经变性病症和其他cns病症的化合物 |
SI3661937T1 (sl) | 2017-08-01 | 2021-11-30 | Gilead Sciences, Inc. | Kristalinične oblike etil((S)-((((2R,5R)-5-(6-amino-9H-purin-9-IL)-4- fluoro-2,5-dihidrofuran-2-IL)oksi)metil)(fenoksi)fosforil)-L-alaninata (GS-9131) za zdravljenje virusnih okužb |
CA3081553C (en) | 2017-11-17 | 2022-11-15 | Cellix Bio Private Limited | Compositions and methods for the treatment of eye disorders |
CA3082191C (en) | 2017-12-07 | 2021-09-21 | Emory University | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
CA3135420A1 (en) | 2018-04-05 | 2019-10-10 | Universiteit Hasselt | Selective pde4d inhibitors against demyelinating diseases |
WO2020002715A1 (en) | 2018-06-29 | 2020-01-02 | Rejuvenate Biomed | Pharmaceutical combination for use in age-related and/or degenerative diseases |
ES2974972T3 (es) | 2018-08-07 | 2024-07-02 | Univ Emory | Derivados heterocíclicos de flavona, composiciones y métodos relacionados con los mismos |
WO2020047229A1 (en) | 2018-08-29 | 2020-03-05 | University Of Massachusetts | Inhibition of protein kinases to treat friedreich ataxia |
EP3969450B1 (en) | 2019-05-14 | 2023-10-25 | Suzhou Four Health Pharmaceuticals Co., Ltd | Quinazoline-2,4-dione derivatives as parp inhibitors |
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 |
AU2022318349A1 (en) | 2021-07-30 | 2024-02-15 | 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 (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 |
WO2023139402A1 (en) | 2022-01-18 | 2023-07-27 | Ascletis Bioscience Co., Ltd. | Inhibitors of cysteine proteases and methods of use thereof |
US11760722B2 (en) | 2022-01-18 | 2023-09-19 | 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)
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 |
CH676988A5 (es) * | 1987-01-21 | 1991-03-28 | Sandoz Ag | |
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 |
US5151438A (en) * | 1989-05-23 | 1992-09-29 | Abbott Laboratories | Retroviral protease inhibiting compounds |
US5354866A (en) * | 1989-05-23 | 1994-10-11 | 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 |
CA2084087A1 (en) * | 1990-06-01 | 1991-12-02 | Prabhakar Kondaji Jadhav | 1,4-diamino 2,3-dihydroxy butanes |
TW225540B (es) * | 1990-06-28 | 1994-06-21 | Shionogi & Co | |
ES2059295T3 (es) | 1990-11-19 | 1998-06-01 | Monsanto Co | Inhibidores de las proteasas retrovirales. |
DE69126987T2 (de) | 1990-11-19 | 1998-03-05 | Monsanto Co | Retrovirale protease-inhibitoren |
ES2059296T3 (es) | 1990-11-19 | 1996-07-16 | Monsanto Co | Inhibidores de proteasas retrovirales. |
CA2096528C (en) * | 1990-11-19 | 2005-12-06 | Kathryn Lea Reed | Retroviral protease inhibitors |
IE913840A1 (en) * | 1990-11-20 | 1992-05-20 | Abbott Lab | Retroviral protease inhibiting compounds |
DK0541168T3 (da) | 1991-11-08 | 1998-05-11 | Merck & Co Inc | HIV-proteaseinhibitorer, som er egnede til behandling af AIDS |
JP3492362B2 (ja) * | 1992-05-20 | 2004-02-03 | ジー.ディー.サール アンド カンパニー | レトロウイルスプロテアーゼ阻害剤の合成に有用な中間体の製造方法 |
AU667376B2 (en) * | 1992-05-21 | 1996-03-21 | Monsanto Company | Retroviral protease inhibitors |
US5521219A (en) * | 1992-08-25 | 1996-05-28 | G. D. Searle & Co. | Sulfonylalkanoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors |
US5463104A (en) * | 1992-08-25 | 1995-10-31 | G. D. Searle & Co. | Succinoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors |
KR100296463B1 (ko) * | 1992-08-25 | 2001-10-24 | 죤 에이치. 뷰센 | 레트로바이러스프로테아제저해제로서유용한히드록시에틸아미노술폰아미드 |
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 |
DK0666842T3 (da) * | 1992-10-30 | 1998-11-02 | Searle & Co | Hydroxyethylaminosulfaminsyrederivater til anvendelse som inhibitorer af retrovirale proteaser |
CA2143191A1 (en) * | 1992-10-30 | 1994-05-11 | Michael L. Vazquez | 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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1993
- 1993-08-31 IS IS4068A patent/IS2334B/is unknown
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- 1993-09-07 RU RU95109928A patent/RU2135496C1/ru active
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1995
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1997
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1998
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1999
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2000
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2001
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2002
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