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Attorney: Thies; J. Eric


Number of patents: 86
Last date: April 24, 2012

1      
NumberTitleIssue Date
8163770Benzoxathiin derivative
Disclosed is a compound represented by the formula (I) below and a pharmaceutically acceptable salt thereof. This compound is useful for treatment of obesity, diabetes and the like. [In the formula (I), Ar represents a benzen...
04/24/2012
8158791Aza-substituted spiro derivatives
A compound of the following formula (I) or its pharmaceutically-acceptable salt is provided: [wherein X, Y, Z and W each independently represent a methine group or a nitrogen atom, provided that a case where all of X, Y, Z ...
04/17/2012
8158652Substituted pyridone derivative
Compounds of a formula (I) [wherein, A represents formula (III-1) R3 is a hydrogen, lower alkyl et al; m is 0 or 1; R1 is a hydrogen atom, halogen atom et al, R2 is a hydrogen et ...
04/17/2012
8138206Piperidine derivative
Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically a...
03/20/2012
81016181,4-substituted piperazine derivatives
A compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 represents a branched lower alkyl group having from 3 to 9 carbon atoms or ...
01/24/2012
8044070Heteroaryloxy nitrogenous saturated heterocyclic derivative
Provided are compounds of a formula (I) and their pharmaceutically-acceptable salts: wherein X1, X2 and X3 each independently represent N or CH; W represents the following formula (II):
10/25/2011
8030495Cyclopropyl pyrrolidine orexin receptor antagonists
The present invention is directed to cyclopropyl proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved....
10/04/2011
8003797Pyridine carboxamide orexin receptor antagonists
The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The inven...
08/23/2011
7985758Piperidine derivatives for treatment of Alzheimer's disease
Compounds of formula (I) modulate the activity of gamma secretase and hence find use in treatment or prevention of Alzheimer's disease and related conditions. ...
07/26/2011
7960402Carbamoyl-substituted spiro derivative
A compound represented by, e.g. the formula (I): [wherein X, Y, Z, and W each independently represent optionally substituted methine; A, B, and D each independently represent —C(O)—, etc.; Q represents a methine or a ni...
06/14/2011
7960394Quinazoline derivative
This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) wherein R1 represents a lower alkyl group et al; R2 and R3 are same and different and represents hyd...
06/14/2011
7951797Substituted diazepan orexin receptor antagonists
The present invention is directed to substituted diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The inve...
05/31/2011
7902369Diaryl-substituted five-membered heterocycle derivative
The present invention provides the compounds represented by formula (I): (I) or pharmaceutical salts thereof, wherein: X1 represents oxygen atoms and the like, X2
03/08/2011
7846946Heteroatom-linked substituted piperidines and derivatives thereof useful as histamine Hantagonists
Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF o...
12/07/2010
7879882Thiazolyl mglur5 antagonists and methods for their use
The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy pro...
02/01/2011
7879880Substituted aniline derivatives useful as histamine H3 antagonists
Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein M1 is M
02/01/2011
7875636Pyridyl amide T-type calcium channel antagonists
The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed...
01/25/2011
7858800Biaryl derivatives
The present invention relates to a compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 is a linear or branched alkoxy group, a cycloalkoxy group, a linear o...
12/28/2010
7855294Cycloalkanopyridine derivative
Provided are cycloalkanopyridine derivatives of formula [I]: [wherein the symbols are the same as those stated in the description]. The compounds act as a nociceptin receptor antagonist, and are useful as medicines for dise...
12/21/2010
7855201Morpholine carboxamide prokineticin receptor antagonists
The present invention is directed to morpholine carboxamide compounds which are antagonists of prokineticin receptors, in particular antagonists of prokineticin 2 receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorder...
12/21/2010
7834182Piperidine 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...
11/16/2010
7829586Aryl-substituted nitrogen-containing heterocyclic compounds
Disclosed is an aryl-substituted nitrogen-containing heterocyclic compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof. This compound serves as nociceptin receptor antagonist and is useful as a pharmaceutical agent for treating...
11/09/2010
7790731Crystal form of 2-methyl-3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone
The present invention is directed to a form I crystal of 2-methyl 3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone that is useful for example in the treatment of sleep disorders or various sleep disorder-associated diseases. ...
09/07/2010
7745452Quinazolinone T-type calcium channel antagonists
The present invention is directed to quinazolinone compounds of the formula I: wherein R1, R2, R3, X1, X2 X3 are defined herein. These compounds are antagoni...
06/29/2010
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
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
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
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
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
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
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
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
7482457Substituted quinoline-4-carboxylic hydrazides as NK-2/NK-3 receptor ligands
The present invention discloses a compound of formula (I): wherein: R1 is an aryl or heteroaryl ring; R2 is hydroxy, C1-6 alkoxy, C1-6 alkyl, amino, NR′R″ or C1-6 alkyl-NR′R″ where R′ and R″ are inde...
01/27/2009
7468393Diarylsulfones 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. ...
12/23/2008
7462619Pyridazine, pyrimidine and pyrazine ethyne compounds
In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted or unsubstituted six membered heterocyclic ring that includes at least two nitrogen atoms. The ring additionally inc...
12/09/2008
7400400Method for monitoring particle size
The present invention provides methods for the use of visible and/or near-infrared spectroscopic methodology to monitor and control processes for the generation of particles, including processes that provide for a reduction in particle size and processes that result...
07/15/2008
7393959Di-aryl substituted pyrrole modulators of metabotropic glutamate receptor-5
Pyrrole compounds of Formula (I): and pharmaceutically acceptable salts thereof (where A, B, R11, R12, R13, W, X, Y and Z are as defined herein), which are substituted directly, or by a bridge, with i) a heteroaryl moiety containing ...
07/01/2008
7381725Pyridazine derivatives as ligands for GABA receptors
A class of pyridazine derivatives, substituted in the 4-position by an optionally substituted heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of b...
06/03/2008
7371767Heteroaryl substituted pyrrole modulators of metabotropic glutamate receptor-5
Pyrrole 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, ...
05/13/2008
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