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Attorney: Winokur; Melvin


Number of patents: 132
Last date: October 23, 2007

1        
NumberTitleIssue Date
7285393Assay for modulation of γ secretase
There is provided an assay for identifying compounds which interact with the γ-secretase complex, in particular compounds that lower the production of Aβ42. ...
10/23/2007
7217740Diarylsulfones as 5-HT2A antagonists
Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS. ...
05/15/2007
7208498Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabet...
04/24/2007
7205336β-secretase inhibitors
The present invention provides compounds that are inhibitors of the proteolytic activity of the enzyme β-secretase, pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, processes for making the compounds, and met...
04/17/2007
7205434Sulphonamides for control of beta-amyloid production
There is disclosed a novel class of sulphonamido-substituted bridged bicycloalkyl derivatives comprising a substitute on the bridgehead position. The compounds modulate the production of the β-amyloid precursor protein, and hence are useful in the treatment of Alzh...
04/17/2007
7202224Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
The present invention provides nucleoside 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-dependent RN...
04/10/2007
7196106Cyanothiophene derivatives, compositions containing such compounds and methods of use
The present invention addresses substituted cyanothiophene derivatives of the formula I: as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are gluc...
03/27/2007
7186746Indoles having anti-diabetic activity
Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipi...
03/06/2007
7183303Gamma-secretase inhibitors
Compounds of formula I: inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease. ...
02/27/2007
717980211-beta-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia
Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: are selective inhibitors of the 11β-HSD1 enzyme. The compounds are useful for the treatment of diabetes, su...
02/20/2007
7176203Imidazo-triazine derivatives as ligands for gaba receptors
A class of imidazo[1,2b][1,2,4]triazine derivatives, substituted at the 7-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having good affinity for t...
02/13/2007
7164003Histamine receptor H4 polynucleotides
Novel splice variants of the human H4 histamine receptor are described. The splice variants have delections of portions of the N-terminal of the wild type H4 receptor. The splice variants are useful in methods for identifying agonists, inverse agonists or antagonist...
01/16/2007
7163932Aryldifluoromethylphosphonic acids for treatment of diabetes
The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compo...
01/16/2007
7160886Acylated piperazine derivatives as melanocortin-4 receptor agonists
Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of disease...
01/09/2007
7161006Sulphones for inhibition of gamma secretase
The invention provides compounds of formula I: which are inhibitors of γ-secretase and hence useful in the treatment or prevention of Alzheimer's disease. ...
01/09/2007
7157478Oxadiazole derivatives for inhibition of gamma secretase
Compounds of formula I: wherein X represents a 5-(R-substituted)-1,2,4-oxadiazole-3-yl moiety are inhibitors of gamma-secretase, and hence useful for treating Alzheimer's disease ...
01/02/2007
7157490Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved...
01/02/2007
7153868N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a c...
12/26/2006
7148222Substituted pyrido-pyridazine derivatives which enhance cognition via the GABA-receptors
The present invention discloses a compound of formula 1, or a pharmaceutically acceptable salt thereof: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen...
12/12/2006
7148236Modulators of acetylcholine receptors
The present invention relates to compounds that modulate neurotransmission by promoting the release of neurotransmitters such as acetylcholine, dopamine and norepinephrine. More particularly, the present invention relates to thio-bridged aryl compounds that are capa...
12/12/2006
7144910Sulfonamides, sulfamates and sulfamides as gamma-secretase inhibitors
Compounds of formula I: inhibit the processing of APP by gamma-secretase, and hence are useful in treating or preventing Alzheimer's disease. ...
12/05/2006
7144887Substituted 1,2,3-triazolo[1,5-a]quinazolines for enhancing cognition
The present invention provides a compound of formula (I) in which R1 is generally hydrogen or CF3, R2 is generally hydrogen, W is a cyclic amine, a heterocycle or a group L-Y—X where L-Y is a linking portion and X is generally an a...
12/05/2006
7138400Sulfamides as gamma-secretase inhibitors
Novel sulfamides of formula (I) are disclosed. The compounds exert an inhibitory action on the processing of APP by gamma-secretase, and are therefore useful in the treatment or prevention of Alzheimer's disease. ...
11/21/2006
7125855Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
The present invention provides nucleoside 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-dependent RN...
10/24/2006
7125873Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabet...
10/24/2006
7115628Bridged piperidine derivatives as melanocortin receptor agonists
Certain novel bridged piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases a...
10/03/2006
7109217Phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
Disclosed are compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzh...
09/19/2006
7105526Benzimidazole derivatives
The present invention relates to novel benzimidazole derivatives which are useful as neuropeptide Y receptor antagonists. ...
09/12/2006
7105499Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
The present invention provides nucleoside derivatives 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-dependent RNA viral infection. They are pa...
09/12/2006
7105509Benzodiazepine derivatives as APP modulators
A novel class of 1,4- and 1,5-benzodiazepines of formula (I) is disclosed. The compounds modulate the processing of amyloid precursor protein by γ-secretase, and hence find use in the treatment or prevention of conditions associated with the deposition of β-amyloi...
09/12/2006
7101895Cyclohexyl sulphone derivatives as gamma-secretase inhibitors
Compounds of formula I: wherein Ar1 and Ar2 are optionally substituted aryl or heteroaryl, L is a bond, ═CH— or —(CHRa)n—, and X is SCN, SR1, S(O)R
09/05/2006
7101871Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabet...
09/05/2006
7101892Sulfone derivatives as 5-HT7 receptor ligands
The present invention relates to sulfone derivatives of formula (I): Ar—SO2—CR2R3-L-N(R1)2I wherein Ar, L, R1, R2 and R3 are as defined herein, and pharma...
09/05/2006
7098239Dipeptidyl peptidase inhibitors for the treatment of diabetes
Compounds having Formula I, including pharmaceutically acceptable salts and prodrugs thereof: (Formula I) are inhibitors of the dipep tidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of DP-IV mediated diseases and conditions, such as non-insulin de...
08/29/2006
70947775-HTreceptor ligands
Compounds of formula I: are antagonists of the human 5-HT2A receptor, and hence useful in treatment or prevention of a variety of neurological conditions. ...
08/22/2006
70912302-aryloxy-2-arylalkanoic acids for diabetes and lipid disorders
A class of 2-aryloxy-2-arylalkanoic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyper...
08/15/2006
7091216Substituted furo[2,3-b]pyridine derivatives
Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are...
08/15/2006
70841562-Aminoquinoline compounds
The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-...
08/01/2006
7060710Isoxazole pyrazoloindane derivatives as cognition enhancing GABAα5 subtype ligands
The present invention provides compounds of formula I: in which: one of X and Y is a nitrogen atom substituted by a group R6′ and the other is a carbon atom substituted by an isoxazole group ...
06/13/2006
7057051Substituted imidazoles as cannabinoid receptor modulators
The use of compounds of the present invention as antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor particularly in the treatment, prevention and suppression of diseases mediated by the Cannabinoid-1 (CB1) receptor. The invention is concerned wi...
06/06/2006
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