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Attorney: Levis; John F.


Number of patents: 89
Last date: May 01, 2012

1      
NumberTitleIssue Date
8168615Prodrugs of piperazine and substituted piperidine antiviral agents
This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R
05/01/2012
8124615Diketo substituted pyrrolo[2,3-C]pyridines
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketo fused azolopiperidine and azolopiperazine derivatives of Formula I: that possess ...
02/28/2012
8119389strain
The present invention relates to a process for preparing (2R,3S)-1-halo-2-hydroxy-3-(protected)amino-4-substituted butane comprising contacting a mutagenized Rhodococcus erythropolis having ATCC deposit no. PTA-6648 with (3S)-1-halo-2-oxo-3-(protected)amino-4...
02/21/2012
8067420Substituted pyrazinone melanin concentrating hormone receptor-1 antagonists and methods
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1
11/29/2011
8039486Indole, azaindole and related heterocyclic N-substituted piperazine derivatives
This invention provides compounds of Formula I, including pharmaceutically acceptable salts thereof, having drug and bio-affecting properties, their pharmaceutical compositions and method of use. These compounds possess unique antiviral activity, whether used alone ...
10/18/2011
7981913Isophthalates as beta-secretase inhibitors
There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, t...
07/19/2011
7977362Alpha-(N-benzenesulfonamido)cycloalkyl derivatives
Disclosed are compounds, pharmaceutical compositions containing the compounds, methods for using the compounds and processes for making the compounds. More specifically, the disclosure relates to alpha-(N-benzenesulfonamido)cycloalkyl compounds that may inhibit one ...
07/12/2011
7968718Process for preparing triazole substituted azaindoleoxoacetic piperazine derivatives and novel salt forms produced therein
A process is provided for preparing triazole substituted azaindoleoxoacetic piperazine derivative. Novel intermediates produced in the above process, and novel N-1 and amorphous forms of a 1,2,3-triazole substituted azaindoloxoacetic piperazine derivatives and proce...
06/28/2011
7960406Diketo substituted pyrrolo[2,3-c] pyridines
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketo fused azolopiperidine and azolopiperazine derivatives of Formula I: that possess ...
06/14/2011
7915283Indole, azaindole and related heterocyclic 4-alkenyl piperidine amides
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with new piperidine 4-alkenyl derivatives that possess unique antiviral activity. More particul...
03/29/2011
7902218Substituted tetrahydroisoquinolines as β-secretase inhibitors
There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 are as defined herein...
03/08/2011
7902204Diazaindole-dicarbonyl-piperazinyl antiviral agents
The invention comprises substituted diazaindole-dicarbonyl-piperazinyl derivatives of general Formula I wherein: Q is selected from the group consisting of
03/08/2011
7851476Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1-1,2,4-triazol-1-YL)-1-[(phosphonooxy)methyl]-1-pyrrolo[2,3-]pyridin-3-YL]-1,2-dioxoethyl]-piperazine
Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c]pyridin-3-yl]-1,2-dioxoethyl]-piperazine its salts and solvates thereof are herein set forth, as ar...
12/14/2010
7829711Crystalline materials of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-C]pyridine-3-yl]-ethane-1,2-dione
The instant invention provides crystalline materials of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione; processes for the production of such crystalline materials; pharmaceutical composition...
11/09/2010
7820820Method of preparation of azaindole derivatives
A method of preparing azaindole compounds for antiviral use having the formula ...
10/26/2010
7807676Diketo-Piperazine and Piperidine derivatives as antiviral agents
This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity. Mor...
10/05/2010
7807671Diketo-piperazine and piperidine derivatives as antiviral agents
This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity usef...
10/05/2010
7776863Methods of treating HIV infection
The invention encompasses pharmaceutical compositions and methods for using Compound 1 in combination with other agents for treating patients with AIDS or HIV infection. ...
08/17/2010
7772221Diaminopropane derived macrocycles as inhibitors of β amyloid production
There is provided a series of macrocyclic diaminopropanes of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, m, n, W, X, Y, Z and L as defin...
08/10/2010
7745625Prodrugs of piperazine and substituted piperidine antiviral agents
This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exis...
06/29/2010
7745470Isophthalates as beta-secretase inhibitors
There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, t...
06/29/2010
7745463Alkene piperidine derivatives as antiviral agents
This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with alkene piperidine derivatives that possess unique antiviral activity. More particularly,...
06/29/2010
7732434Macrocyclic acyl guanidines as beta-secretase inhibitors
There is provided a series of heterocyclic-containing macrocyclic acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R1, R2, R3...
06/08/2010
7723338Crystalline forms of 1-benzoyl-4-[2-[4,7-dimethoxy-1-[(phosphonooxy)methyl]-1-pyrrolo[2,3-C]pyridin-3-yl]-1,2-dioxoethyl]-piperazine
The instant disclosure provides crystalline forms of 1-benzoyl-4-[2-[4,7-dimethoxy-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c]pyridin-3-yl]-1,2-dioxoethyl]-piperazine, salts and solvates thereof. The present disclosure also generally relates to pharmaceutical composi...
05/25/2010
7714019Indole, azaindole and related heterocyclic pyrrolidine derivatives
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido piperazine derivatives. These compounds possess unique antiviral activity, whether u...
05/11/2010
7678793Azolo triazines and pyrimidines
Corticotropin releasing factor (CRF) antagonists of formula I or II: and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or hear...
03/16/2010
7678784Oxime-containing macrocyclic acyl guanidines as β-secretase inhibitors
There is provided a series of oxime-containing macrocyclic acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, R4, ...
03/16/2010
7662823Pharmaceutical formulations of substituted azaindoleoxoacetic piperazine derivatives
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activi...
02/16/2010
7612069Acyl guanidines as beta-secretase inhibitors
There is provided a series of substituted acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and R5
11/03/2009
7601751Indole acetic acid acyl guanidines as β-secretase inhibitors
There is provided a series of substituted acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R...
10/13/2009
7601715Process for preparing triazole substituted azaindoleoxoacetic piperazine derivatives and novel salt forms produced therein
A process is provided for preparing triazole substituted azaindoleoxoacetic piperazine derivative. Novel intermediates produced in the above process, and novel N-1 and amorphous forms of a 1,2,3-triazole substituted azaindoloxoacetic piperazine derivatives and proce...
10/13/2009
7598380Method of preparation of azaindole derivatives
A method of preparing azaindole compounds for antiviral use having the formula ...
10/06/2009
7582468Process for preparing (2R,3S)-1,2-epoxy-3-(protected)amino-4-substituted butane and intermediates thereof
The present invention relates to a process for preparing (2R,3S)-1-halo-2-hydroxy-3-(protected)amino-4-substituted butane comprising contacting a mutagenized Rhodococcus erythropolis having ATCC deposit no. PTA-6648 with (3S)-1-halo-2-oxo-3-(protected)amino-4...
09/01/2009
7572810Alkene piperidine derivatives as antiviral agents
This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with alkene piperidine derivatives that possess unique antiviral activity. More particularly,...
08/11/2009
7557137Gamma-lactams as beta-secretase inhibitors
There is provided a series of novel substituted gamma-lactams of Formula (I) wherein R1, R2, R3, R4 and R5 are defined herein, their pharmaceutical compositions and met...
07/07/2009
7550445Aripiprazole complex formulation and method
An aripiprazole formulation is provided which includes the antipsychotic agent aripiprazole in the form of an inclusion complex in a β-cyclodextrin, preferably, sulfobutyl ether β-cyclodextrin (SBECD), which in the form of an injectable produces reversible general...
06/23/2009
7531552Indole, azaindole and related heterocyclic pyrrolidine derivatives
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido piperazine derivatives. These compounds possess unique antiviral activity, whether u...
05/12/2009
7504399Piperazine enamines as antiviral agents
This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with indole and azaindole piperazine enamine derivatives that possess unique antiviral activi...
03/17/2009
7501420Composition and antiviral of substituted azaindoleoxoacetic piperazine derivatives
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activi...
03/10/2009
75014194-Squarylpiperazine derivatives as antiviral agents
This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with 4-squarylpiperazine derivatives that possess unique antiviral activity. More particularl...
03/10/2009
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