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Attorney: Datlow; Philip I.


Number of patents: 116
Last date: January 24, 2012

1      
NumberTitleIssue Date
8101765Process for preparing acyclic HCV protease inhibitors
Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are potent active agents for the treatment of hepatitis C virus (HCV) infection: The disclosed processes use SNAr-ty...
01/24/2012
8067438Hepatitis C inhibitor compounds
Compounds of formula (I): wherein B, X, R3, L0, L1, L2, R2, R1 and RC are defined herein. The compounds are useful as inhibitors of HCV NS3 protea...
11/29/2011
8030309Viral polymerase inhibitors
An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R
10/04/2011
8017771Process for preparing acyclic HCV protease inhibitors
Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are potent active agents for the treatment of hepatitis C virus (HCV) infection: The disclosed processes use SNAr-ty...
09/13/2011
7951773Ring-closing metathesis process for the preparation of macrocyclic peptides
Disclosed is a process for preparing a compound of formula (I) by protecting the secondary amide nitrogen atom in the compound of formula (III) to obtain (IV) wherein PGN is a suitable nitrogen protecting group, ring-closing the compound of formula (IV) b...
05/31/2011
7939667Hepatitis C inhibitor compounds
Compounds of formula (I): wherein B, X, R3, L0, L1, L2, R2, R1 and RC are defined herein. The compounds are useful as inhibitors of HCV NS3 protea...
05/10/2011
7902183Thiazolyl-dihydro-indazole
The present invention encompasses compounds of general formula (1) wherein R1 to R5 are defined as in claim 1, which are suitable for the treatment of diseases characterized by exce...
03/08/2011
7893084Viral polymerase inhibitors
An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; represen...
02/22/2011
7893049Thiazolyl-dihydro-indazole
The present invention encompasses compounds of general formula (1) wherein R1 to R6 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessi...
02/22/2011
RE42164Hepatitis C inhibitor tri-peptides
Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of w...
02/22/2011
7884246Process for preparing substituted anisidines
Disclosed is a process for preparing substituted anisidines of formula I starting from substituted cyclic hydroxy-ketones II via aromatization through a substituted oxime intermediate IV in which R is C1-C6 alkyl or halogen, and Alk is C1
02/08/2011
7879851Viral polymerase inhibitors
An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R
02/01/2011
7851625Process for preparing 2,3-disubstituted indoles
Disclosed are processes for making 2, 3 disubstituted indole compounds such as compounds of general formula I comprised of the steps of a) reacting a bromoindole compound (i) with a dialkoxyl C1-5 borane in the presence ...
12/14/2010
7838711Process for continuous ruthenium-catalysed metathesis
The invention relates to a process for carrying out metathesis reactions, wherein the process is carried out continuously and a ruthenium-containing catalyst is used. ...
11/23/2010
7838207Surrogate cell-based system and method for assaying the activity of hepatitis C virus NS3 protease
The present invention concerns the development of a cell-based assay system having improved sensitivity to HCV NS3 protease activity when compared to known assays, which is useful for screening test compounds capable of modulating (particularly inhibiting) HCV NS3 p...
11/23/2010
RE41894Hepatitis C inhibitor tri-peptides
Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of w...
10/26/2010
7807670Inhibitors of papilloma virus
A compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein: A,; X, W, R1, Y; R3; and R4 are as defined herein. The compounds of the invention may be used as in...
10/05/2010
7767818Hepatitis C inhibitor dipeptide analogs
Compounds of formula (I): wherein R1, R2, R3, R4, n and m are as defined herein. The compounds are useful as inhibitors of HCV NS3 protease. ...
08/03/2010
7759365Piperidine-substituted indoles
Disclosed are novel piperidine-substituted indoles- or heteroderivatives thereof of the formula 1: wherein R1, R5, R6, R7, A, B, D-E, Y, i, j, n and m are defined as below.
07/20/2010
7754481Keratinocytes useful for the treatment of wounds
The invention relates to new keratinocytes which may be cultured in vitro and the advantageous use thereof for preparing a product which can be used to treat acute and chronic wounds. ...
07/13/2010
7749961Macrocyclic peptides active against the hepatitis C virus
Compounds of formula (I): wherein R1, R2, X, R3, D, and the dotted line b are as defined herein; or a pharmaceutically acceptable salt or ester thereof, are useful as inhibitors of the HCV N...
07/06/2010
RE41356Hepatitis C inhibitor tri-peptides
Racemates, diastereolsomers and optical isomers of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C
05/25/2010
7709480Pyrimidine derivatives
The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterized ...
05/04/2010
7705146Hepatitis C inhibitor peptide analogs
The invention relates to compounds of formula (I) wherein R′, R2, R3, R4, R5, R6, Y, n and m are as defined herein. The compounds are useful for the treatment and prevention of hepatitis C viral infections in ...
04/27/2010
7696242Hepatitis C inhibitor peptide analogs
Compounds of formula (I): wherein R1, R2, R3, R4, R5, Y, n and m are as defined herein. The compounds are useful as inhibitors of HCV NS3 protease. ...
04/13/2010
7695734Extended release tablet formulation containing pramipexole or a pharmaceutically acceptable salt thereof
An extended release tablet formulation comprising pramipexole or a pharmaceutically acceptable salt thereof in a matrix comprising at least one water swelling polymer other than pregelatinized starch. ...
04/13/2010
7642381Two step process for preparing substituted anisidines
The process of the present invention can be briefly summarized as depicted in the following scheme: R1 is C1-Calkyl, R2 is C1-C6alkyl and Hal is a halogen atom. ...
01/05/2010
7642235Macrocyclic peptides active against the hepatitis C virus
Compounds of formula I: wherein D, R4, R3, L0, L1, L2, R2 and RC are defined herein; or a pharmaceutically acceptable salt thereof, useful as inhi...
01/05/2010
7608614Process for preparing macrocyclic compounds
Intermediates of the formula QUIN: and methods for their preparation are described. The intermediate compounds are useful for preparing active agents for the treatment of hepatitis C virus (HCV) infection. ...
10/27/2009
7601714Pyrimidine derivatives useful as inhibitors of PKC-theta
Disclosed are novel compounds of formula (I): wherein X, Y, R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of dis...
10/13/2009
7589115Derivatives of [6,7-dihydro-5-imidazo[1,2-α]imidazole-3-sulfonylamino]-propionamide
Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-propionamide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease. ...
09/15/2009
7589114Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonyl]-azetidine-carboxylic acids, esters and amides
Derivatives of 6,7-dihydro-5H-imidazo[1,2-α]imidazole-3-sulfonyl]-azetidine-carboxylic acids, esters and amides which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease. ...
09/15/2009
7585845Hepatitis C inhibitor compounds
Compounds of formula (I): wherein B, X, R3, L0, L1, L2, R2, R1 and RC are defined herein. The compounds are useful as inhibitors of HCV NS3 protea...
09/08/2009
7572921Substituted benzylimidazoles useful for the treatment of inflammatory diseases
The invention comprises a class of derivatives of substituted benzylimidazoles of the formula (I) and methods for making the same. These compounds are useful for the treatment of inflammatory conditions. ...
08/11/2009
7569574Purine derivatives, the preparation thereof and their use as pharmaceutical compositions
The invention relates to new purine derivatives of general formula wherein R1 to R4 are defined as in the claims, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts ther...
08/04/2009
7550494Small molecules useful in the treatment of inflammatory disease
Compounds of the formula I which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary are: ...
06/23/2009
7550473Pyrimidine derivatives useful as inhibitors of PKC-theta
Disclosed are novel compounds of formula (I): wherein R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases ...
06/23/2009
7544806Piperidine-substituted indoles-or heteroderivatives thereof
Accordingly, one object of the present invention are novel piperidine-substituted indoles- or heteroderivatives thereof of the formula 1: wherein R1, R5, R6, A, B, D-E, X-W-V, Y, i, j, n and...
06/09/2009
7544798Process for preparing macrocyclic compounds
Disclosed is a multi-step process for preparing a macrocyclic compound of the formula (I): wherein Q is a radical of the following formula: and the other variables are as defined ...
06/09/2009
7534812Process for preparation of isochroman and derivatives thereof
The present invention relates to an improved process for preparing compounds of formula 1 on an industrial scale, wherein R1, R2 and R3 are independently C1-6-alkyl, C2-6
05/19/2009
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