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Attorney: Walton; Kenneth R.


Number of patents: 55
Last date: April 03, 2012

1    
NumberTitleIssue Date
8148349Nucleoside cyclic phosphoramidates for the treatment of RNA-dependent RNA viral infection
The present invention provides nucleoside cyclic phosphoramidates of formula (I), pharmaceutical compositions comprising the compounds of formula (I) and methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treat...
04/03/2012
8071568Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection
The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for...
12/06/2011
7981879HIV integrase inhibitors
Compounds of Formula I are inhibitors of FHV integrase and inhibitors of FHV replication (I), wherein m, n, X, R1, R2, R3, R4, R5, R6, R7; R8, R9 and R10 ar...
07/19/2011
7968564HIV integrase inhibitors
Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the...
06/28/2011
7968553Tetrahydro-4H-pyrido[1,2-a] pyrimidines useful as HIV integrase inhibitors
Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula A: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1,...
06/28/2011
7939537HIV integrase inhibitors
Pyridopyrimidine carboxamide compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein R1, R2, R3, R4, R5 and R6 are ...
05/10/2011
7879815Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection
The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for...
02/01/2011
7834062Aminoalkylphenols, methods of using and making the same
The present invention relates to Mannich base antimalarial aminoalkylphenol compounds and their use against protozoa of the genus Plasmodium, particularly emerging strains of drug-resistant Plasmodia. This invention further relates to compositions containing ...
11/16/2010
7820680HIV integrase inhibitors
Bicyclic uracils and related compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the compounds are of Formula I: wherein a, b, Y, R1, R2, R3 and R...
10/26/2010
7820660N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are def...
10/26/2010
7807684HIV reverse transcriptase inhibitors
Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts are useful in the i...
10/05/2010
7795250Indole derivatives as antiviral agents
The present invention relates to indole compounds of the formula (I): wherein R1, R2, R3, R4, A, E and X are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepat...
09/14/2010
7795247Tetracyclic indole derivatives as antiviral agents
The present invention relates to tetracyclic indole compounds of formula (I): wherein R1, R2, A, Ar, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical comp...
09/14/2010
7781454Non-nucleoside reverse transcriptase inhibitors
Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein V, W, X, Y, Z, R1, R2, R4, R5, R6, ring A, ring B, j and k are defined herein. The compounds o...
08/24/2010
7754731Potassium salt of an HIV integrase inhibitor
Potassium salts of Compound A and methods for their preparation are disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the...
07/13/2010
7741315HIV integrase inhibitors
Tricyclic compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by...
06/22/2010
7632821Ribonucleoside cyclic acetal derivatives for the treatment of RNA-dependent RNA viral infection
The present invention provides ribonucleoside 2′,3′-cyclic acetals of structural formula I which are precursors or prodrugs of inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors of inhibitors of RNA-dependent RNA viral replication a...
12/15/2009
7619086HIV integrase inhibitors
Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein Z, R1, R2, R3, R4, R5, R6, R7, R8 and...
11/17/2009
7598264HIV integrase inhibitors
Hydroxy (tetra- or hexa-)hydronaphthyridine dione compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein a, R1?, R2?, R3?, R4? and R5? are defined herein. The compounds are useful in the prevention and treatment of infe...
10/06/2009
7595063Compressed tablet formulation
This invention relates to a 50% drug loaded compressed tablet formulation for efavirenz. Efavirenz is a non-nucleoside reverse trancriptase inhibitor being studied clinically for use in the treatment of HIV infections and AIDS. ...
09/29/2009
7589127Aminoalkylphenols, methods of using and making the same
The present invention relates to Mannich base antimalarial aminoalkylphenol compounds and their use against protozoa of the genus Plasmodium, particularly emerging strains of drug-resistant Plasmodia. This invention further relates to compositions containing ...
09/15/2009
RE40794Crystalline forms of carbapenem antibiotics and methods of preparation
A process for preparing a crystalline, carbapenem monosodium salt of formula IIa: characterized by the steps a) adding about 10 to 30% of an organic solvent to an aqueous solution of the carbapenem, b) cooling the resulting solut...
06/23/2009
7538112HIV integrase inhibitors
Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R1, R2, R3, R4, R5
05/26/2009
7534767C-purine nucleoside analogs as inhibitors of RNA-dependent RNA viral polymerase
The present invention provides C-purine nucleoside analogs and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependen...
05/19/2009
7517532Dihydroxypyridopyrazine-1,6-dione compounds useful as HIV integrase inhibitors
8,9-Dihydroxydihydropyridopyrazine-1,6-diones and 8,9-dihydroxypyridopyrazine-1,6-diones are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the pyridopyrazinediones are of Formula (I): (I), wherein R1, R2, R
04/14/2009
7476666HIV integrase inhibitors
Bicyclic pyrazoles of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein Z is O or N(R8); n is an integer equal to zero or 1; and R1, R2, R3, R
01/13/2009
7459452Dihydroxypyrimidine carboxamide inhibitors of HIV integrase
4,5-Dihydroxypyrimidine-6-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. Thes...
12/02/2008
7435735Hydroxy pyridopyrrolopyrazine dione compounds useful as HIV integrase inhibitors
Hydroxy-substituted pyridopyrrolopyrazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I): (I) wherein a, b, A, B, R1, R2, R3, R4...
10/14/2008
7435734N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are def...
10/14/2008
7414045Substituted pyrimido[1,2-a]azepines useful as HIV integrase inhibitors
Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula (A): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12
08/19/2008
73997638-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as HIV integrase inhibitors
8-Hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds are inhibitors of HIV integrase and inhibitors of HIV replication. More particularly, the compounds are of Formula (I): wherein R1, R2, R3, R4, R5 and R6 ...
07/15/2008
7339054Process for preparing branched ribonucleosides from 1,2-anhydroribofuranose intermediates
A process is provided for the preparation of branched-chain ribonucleosides of formula (I): from the 1,2-anhydroderivatives of formula (II). wherein PG is a hydroxyl protecting gr...
03/04/2008
7323460N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides useful as HIV integrase inhibitors
N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and inhibitors of HIV replication. The naphthyridine carboxamides are of Formula (I): wherein R1′, R
01/29/2008
7323453Methods of inhibiting orthopoxvirus replication with nucleoside compounds
The present invention provides methods of inhibiting orthopoxvirus replication and/or treating orthopoxvirus infection with certain nucleoside compounds and derivatives thereof. These compounds are particularly useful as inhibitors of vaccinia virus and variola viru...
01/29/2008
7323449Thionucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
The present invention provides thionucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependen...
01/29/2008
7279487Hydroxynaphthyridinone carboxamides useful as HIV integrase inhibitors
Hydroxynaphthyridinone carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein L, R1a, R1b, R1c, R2a, R2b
10/09/2007
7232819Dihydroxypyrimidine carboxamide inhibitors of HIV integrase
4,5-Dihydroxypyrimidine-6-carboxamides of formula (I); are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These compounds are useful in the prevent...
06/19/2007
7217713N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4
05/15/2007
7199240Reductive alkylation of saturated cyclic amines
Saturated cyclic amines (e.g., piperazines and piperidines) are reductively alkylated with an N-containing heteroaryl carbaldehyde using an alkylcarboxylic acid and a borohydride to obtain a product comprising an N-((N-containing heteroaryl)methyl)-substituted cycli...
04/03/2007
7169780N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula (I): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These compounds are useful...
01/30/2007
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