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Attorney: Morris; Michael


Number of patents: 75
Last date: October 21, 2008

1    
NumberTitleIssue Date
7439258Viral polymerase inhibitors
A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S...
10/21/2008
RE40525Hepatitis C inhibitor tri-peptides
A racemate diastereoisomer and optical isomer 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 may be optionally substituted wi...
09/30/2008
7386398Hepatitis C Virus NS5B polymerase inhibitor binding pocket
The HCV NS5B polymerase, when complexed with certain inhibitors, adopts a conformation in which the finger loop region defined by amino acid residues 18 to 35 is displaced to expose a binding pocket defined generally by amino acid residues 392, 393, 395, 396, 399, 4...
06/10/2008
7375090Glucopyranosyloxy-pyrazoles, pharmaceutical compositions containing these compounds, the use thereof and processed for the preparation thereof
The present invention relates to glucopyranosyloxy-pyrazoles of general formula wherein R1 to R6 and R7a, R7b, R7c are defined as in claim 1, the tauto...
05/20/2008
7371732Glucopyranosyloxy-substituted aromatic compounds, medicaments containing such compounds, their use and process for their manufacture
The present invention relates to glucopyranosyloxy-substituted aromatic groups of general formula wherein R1 to R6 and R7a, R7b, R7c are defined as in clai...
05/13/2008
7371753Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
Disclosed are new dihydropteridinones of general formula (I) wherein the groups R1 to R5, Ra to Rc, W, Q1 and Q2 have the meanings given in the claims and sp...
05/13/2008
7335657Cytokine inhibitors
Disclosed are compounds of formula (I) Where Ar1, X, Y, Q, W, R3, R4, R5, R6 and Ry are defined herein. The compounds of the invention inhibit production of ...
02/26/2008
7332614Process for cross coupling indoles
The present invention provides a process for making a compound of general formula I: wherein: R=H or C1-8alkyl X=C3-C8cycloalky...
02/19/2008
7332491Dihydropteridione derivatives, process for their manufacture and their use as medicament
Disclosed are new dihydropteridinones of general formula (I) whereby the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and specificat...
02/19/2008
7326719Cathepsin S inhibitors
This invention relates to peptidyl compounds of the formulas (I) and (II) active as cathepsin S, a cysteine protease, inhibitors. The compounds are selective, reversible inhibitors of the cathepsin S are therefore useful in the treatment of autoimmune and other dise...
02/05/2008
7323567RSV polymerase inhibitors
Compounds or enantiomers of formula (I) or a salt thereof: wherein R1, R2, R3, R4 and R5 are as defined herein, are useful for the manufacture of a medicamen...
01/29/2008
7323470Viral polymerase inhibitors
An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein wherein A, B, R2, R3, M1, M2, M3, M4, Y1 ...
01/29/2008
7322810Method for identifying compounds that inhibit the activity of Myc
Method for identifying compounds useful for the therapy of cancers in which the activity of Myc is causally involved. The method is based on measuring the activity of the E3 ligase HectH9, which is required for ubiquitination and activation of Myc. ...
01/29/2008
7312030Adaptation sites of porcine reproductive and respiratory syndrome virus
A method for determining the capability of an arterivirus to replicate in a permissive cell is disclosed. The method includes determining an amino acid at a position that corresponds to an amino acid of a protein of a porcine reproductive and respiratory syndrome vi...
12/25/2007
7312211Pryanone compounds useful as reversible inhibitors of cysteine proteases
Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and othe...
12/25/2007
7294457Direct binding assay for identifying inhibitors of HCV polymerase
A method for identifying compounds binding to HCV polymerase comprising the steps of: contacting said HCV polymerase or an analog thereof with a probe formula I: wherein A is O, S, N, NR1, or CR1
11/13/2007
7291733Substituted tricyclic heterocycles and their uses
Disclosed are substituted tricyclic heterocycle compounds of the formulas (I), (II) and (III) shown below, wherein R1, R2, R3 and R4 are described herein, which are active as anti-inflammatory agents. Also disclosed are me...
11/06/2007
7285545Cytokine inhibitors
Disclosed are compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as...
10/23/2007
7279475Fluorinated di-aryl urea compounds
Disclosed are compounds of formula(I): wherein R1, R2, W and X of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus...
10/09/2007
7276491Anticoagulant and fibrinolytic therapy using p38 MAP kinase inhibitors
Disclosed are methods for a treating a disease or condition relating to blood coagulation and fibrinolysis using p38 MAP kinase inhibitors. ...
10/02/2007
7265222Process of making di-aryl urea compounds
Disclosed is a process of making compounds of formula(I): wherein R1, R2, R3, R4 and Ra of formula(I) are defined herein. The product compounds inhibit production of cy...
09/04/2007
7262206Cycloalkyl—containing 5-acylindolinones, the preparation thereof and their use as medicaments
The present invention relates to cycloalkyl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined as in claims 1 to 6, the tautomers, the enantiomers, th...
08/28/2007
7247496Process for determining the particle size distribution of an aerosol and apparatus for carrying out such a process
The measurement of the particle size distribution of an aerosol is of crucial importance in pharmaceutical development. A prerequisite for this is a valid method, e.g. the cascade impactor method described in the pharmacopoeias. It requires measurement of the active...
07/24/2007
7241758Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory disease...
07/10/2007
72418896-formyl-tetrahydropteridines, process for their manufacture and use thereof as medicaments
Disclosed are 6-formyl-tetrahydropteridines of the formula (I) wherein the groups R1 to R6 have the meanings given in the claims and specification, the isomers thereof, methods of preparing ...
07/10/2007
7241801Viral polymerase inhibitors
A compound, represented by formula (I): wherein A, B, R1, R2, R3, R5, R6, R7, R9, and R10 are as defined herein, or an enant...
07/10/2007
7238807Process for the manufacture of fused piperazin-2-one derivatives
Disclosed are processes for the preparation of fused piperazin-2-one derivatives of general formula (I) wherein the groups R1 to R5, A1 and A2 have the meanings given i...
07/03/2007
7235654Methods for modulating IKKα activity
A method for modulating NF-κB dependent gene transcription in a cell comprised of modulating IKKα protein activity in the cell. The present invention also provides siRNA compositions and methods thereof for modulating NF-κB dependent gene transcription. ...
06/26/2007
7226747Method of identifying substances which modulate interleukin 4(IL-4) signaling
The present invention relates to a method to identify substances and a use of such substances which can modulate IL-4 dependent signaling involved in tumor diseases, preferably Hodgkin Lymphomas or inflammatory airway diseases, preferably asthma and a method for det...
06/05/2007
7223785Viral polymerase inhibitors
An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein wherein A, B, R2, R3, L, M1, M2, M3, M4, Y
05/29/2007
7214703Pyrrolidinohydrochinazolines
Disclosed are compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein the groups Ar1, Ar2, A, R1, R2, R3, E1
05/08/2007
7214802Anti-cytokine heterocyclic compounds
Disclosed compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chr...
05/08/2007
7211575Methods of treating cytokine mediated diseases
Disclosed are methods of treating acute and chronic inflammation in the lung caused by inhalation of smoke, endometriosis, Behcet's disease, uveitis, ankylosing spondylitis, pancreatitis, cancer, Lyme disease, sepsis, chronic obstructive pulmonary disease, traumatic...
05/01/2007
7208309Inhibitor-resistant HCV NS3 protease
An inhibitor-resistant HCV NS3 protease is provided which is useful to screen for compounds having therapeutic value against drug resistant HCV strains. In particular, the inhibitor-resistant HCV NS3 protease comprises an amino acid sequence which is mutated in the ...
04/24/2007
7208508Use of bradycardiac substances in the treatment of myocardial diseases associated with hypertrophy and novel medicament combinations
The present invention relates to the new use of bradycardiac substances such as a Ca++ channel blocker, beta-receptor blocker or if channel blocker, the if channel blockers being preferred, optionally in combination with a cardioacti...
04/24/2007
7189743Prodrugs of 1-methyl-2-(4-amidinophenylaminomethyl)-benzimidazol-5-yl-carboxylic acid-(N-2-pyridyl-N-2-hydroxycarbonylethyl)-amide
The present invention relates to new compounds of general formula having thrombin-inhibiting activity. Exemplary are: 1-Methyl-2-[4-(N-hydroxyamidino)-phenylaminomethyl]-benzimidazol-5-yl-carboxylic ...
03/13/2007
7183280Bicyclic imidazole derivatives, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to bicyclic imidazole compounds of general formula wherein R1 to R3 and A are defined as in claims 1 to 8, the tautomers, the enantiomers, the ste...
02/27/2007
7176231Aryl-containing 5-acylindolinones, the preparation thereof and their use as medicaments
The present invention relates to aryl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined herein, the tautomers, the enantiomers, the diastereomers, the mixtures the...
02/13/2007
7169934(R) 2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(carboxymethylamino)-1 (pyrrolidinocarbonyl)-ethyl]-benzimidazole, the monohydrochloride thereof, preparation thereof and the use as pharmaceutical composition
Crystalline forms of the compounds (R)-2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(carboxymethylamino)-1-(pyrrolidinocarbonyl)-ethyl]-benzimidazole and the monohydrochloride thereof, processes for the preparation thereof and the use thereof as pharmaceutical compo...
01/30/2007
7164018Polymers based on N-carbamyl-N'-dimethylsilyl methyl-piperazine traceless linkers for the solid phase synthesis of phenyl based libraries
The present invention relates to polymers characterized by novel silicon linkers based on the carbamyl piperazine moiety, methods of preparing these polymers and their use in the solid phase synthesis of compounds or libraries of compounds embracing a phenyl ring in...
01/16/2007
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