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Attorney: Krovatin; William


Number of patents: 114
Last date: July 20, 2010

1      
NumberTitleIssue Date
7759492Enantioselective synthesis of 13-oxotricyclo[8.2.1.0.] trideca-3(8),4,6-triene-5-carboxylates
An enantioselective route to compounds of formula I is disclosed: The compounds of formula I are key intermediates in the synthesis of compounds useful in treatment of Alzheimer's disease. ...
07/20/2010
7696192Tricyclic anilide spirolactam CGRP receptor antagonists
The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, J, K, T, U, V, W, X, Y, Z, R4, R5a, R5b, R
04/13/2010
7659300Monocyclic anilide spirolactam CGRP receptor antagonists
The present invention is directed to compounds of Formula I: I (where A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treat...
02/09/2010
7659264CGRP receptor antagonists
The present invention is directed to compounds of Formula I: Formula I: I and Formula II: (where variables R1, R2, R3, R4, A, B, J, Q, T, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and use...
02/09/2010
7655675Gamma-secretase inhibitors
Compounds of formula I: inhibit the processing of APP by gamma-secretase and hence find use in treatment of Alzheimer's disease. ...
02/02/2010
7655644Piperidine and azetidine derivatives as GlyT1 inhibitors
The present invention provides compounds of formula (I), wherein both p's are one or two, R1 is generally heteroaryl or cycloalkyl, R2 is C3-6cycloalkyl or phenyl and R3 is heteroaryl, and pharmaceutically acceptable salts...
02/02/2010
7645790Hydroisoindoline tachykinin receptor antagonists
The present invention is directed to certain hydroisoindoline compounds of formula I which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formula...
01/12/2010
7645756Nitrogenous fused heteroaromatic ring derivative
The invention provides a compound or its pharmaceutically-acceptable salt of formula wherein A1 is a hydrogen, etc.; j and k are 0 or 1; is a double bond, etc.; is a doub...
01/12/2010
7632832CGRP receptor antagonists
Compounds of Formula I: (where variables R1, R2, R3, R7, G, J, Q, T, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster...
12/15/2009
7626056Cyclohexanesulfonyl derivatives as GlyT1 inhibitors to treat schizophrenia
The present invention provides compounds of formula I: wherein R1 is an alkyl, phenyl, heterocyclyl, cycloalkyl, alkoxy, ester, amino or amide group; R2 is a phenyl, heterocycly...
12/01/2009
7625901Substituted monocyclic CGRP receptor antagonists
Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, R
12/01/2009
7595344Sulphones which modulate the action of gamma secretase
Disclosed are sulphones which modulate the action of gamma-secretase. The compounds are useful in the treatment or prevention of Alzheimer's disease. ...
09/29/2009
7595316Heteroaryloxy nitrogenous saturated heterocyclic derivative
Compound of the formula: (I) [wherein each of X1, X2 and X3 independently represents N or CH, W represents the formula (II):(II) or the formula (III):(III) and Y represents a group of the formula (IV):(IV)], or a pharmacologically ac...
09/29/2009
7592456Arylsulfonylnaphthalene derivatives as 5HTantagonists
Compounds of formula (I) are potent and selective 5-HT2A antagonists, useful in treatment of a variety of adverse conditions of the CNS. ...
09/22/2009
75923603-fluoro-piperidines as NMDA/NR2B antagonists
Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for treating conditions such as, for example, Parkinson's disease, Alzheimer's disease, migraine, epilepsy and pain. ...
09/22/2009
7592337Di-aryl substituted tetrazole modulators of metabotropic glutamate receptor-5
Tetrazole compounds substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ri...
09/22/2009
7589116Biaryl substituted pyrazoles as sodium channel blockers
Biaryl substituted pyrazole compounds are sodium channel blockers useful for the treatment of pain and other conditions. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more therapeutical...
09/15/2009
7576122Ophthalmic compositions for treating ocular hypertension
This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the us...
08/18/2009
7576083Morpholinyl piperidine glycine transporter inhibitors
The present invention is directed to morpholinyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunctio...
08/18/2009
7572822Biaryl substituted triazoles as sodium channel blockers
Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, eit...
08/11/2009
7572792Azetidine glycine transporter inhibitors
The present invention is directed to azetidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and disease...
08/11/2009
7569592Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5
Pyrazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia,...
08/04/2009
7563816Ophthalmic compositions for treating ocular hypertension
This invention relates to potent potassium channel blocker compounds of Formula (I) or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the ...
07/21/2009
7563807Removal of aldehyde impurity by reactive polystyrene resini
A purification method in the preparation of a substituted 8-arylquinoline, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, utilizes a polystyrene-based sulfonylhydrazine reactive resin to remove an aldehyde impurity. ...
07/21/2009
7550481Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of Alzheimer's disease
The present invention is directed to phenylamide and pyridylamide derivative compounds of which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. ...
06/23/2009
7550470Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogen...
06/23/2009
7547720Ophthalmic compositions for treating ocular hypertension
This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use...
06/16/2009
7547693Piperidine derivative
Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/conge...
06/16/2009
7544815Process for making hydroisoindoline tachykinin receptor antagonists
The present invention is directed to a process for preparing certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The compounds are useful in the treatment of cer...
06/09/2009
7534784CGRP receptor antagonists
The present invention is directed to compounds of Formula I: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CG...
05/19/2009
7528163Ophthalmic compositions for treating ocular hypertension
This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use...
05/05/2009
7521455Fused ring 4-oxopyrimidine derivative
The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circ...
04/21/2009
7514459Gamma-secretase inhibitors
Compounds of formula I: are potent inhibitors of gamma-secretase and hence find use in treatment or prevention of diseases associated with deposition of β-amyloid. ...
04/07/2009
7514253URA5 gene and methods for stable genetic integration in yeast
A novel gene encoding P. pastoris orotate-phosphoribosyl transferase (URA5) is disclosed. Methods for producing and selecting yeast strains capable of stable genetic integration of heterologous sequences into the host genome are also provided. ...
04/07/2009
7507836Benzamide modulators of metabotropic glutamate receptors
The present invention is directed to compounds which are allosteric modulators of metabotropic glutamate receptors, including the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate...
03/24/2009
7495029Prodrugs of (2R)-2-propyloctanoic acid for the treatment of stroke
Disclosed are prodrugs of (2R)-2-propyloctanoic acid, and pharmaceutical compositions comprising them, which may be effective in modulating multiple events in the biochemical cascade of stroke. Also disclosed are methods of treating patients who have had a stroke, o...
02/24/2009
7494983Ophthalmic compositions for treating ocular hypertension
This invention relates to potent potassium channel blocker compounds of structural Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relate...
02/24/2009
7491713CGRP receptor antagonists
Compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, D, G, J, Q, T, W, X and Y are as defined herein) useful ...
02/17/2009
7485640Imidazopyrazinones as GABA-A receptor anxiolytics
The present invention discloses a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein —U—V— represents —CH═CH—, or —CH2—CH2—, —N═CH— or —CH═N—; X1 represents hydrogen, halog...
02/03/2009
74824568-(3-Biaryl)phenylquinoline phosphodiesterase-4 inhibitors
Novel substituted 8-phenylquinolines represented by Formula (I), wherein the phenyl group at the 8-position contains an aryl or heteroaryl substituent in the meta position, are PDE4 inhibitors. ...
01/27/2009
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