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Class 514/252.05 - The additional hetero ring is a five-membered nitrogen hetero ring


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the additional hetero ring has five
No. of patents: 291
Last issue date: 05/29/2012


1                
NumberTitleIssue Date
8188085Antifungal agents
Novel derivatives of enfumafungin are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as a...
05/29/2012
81832412-oxo-1-pyrrolidine derivatives
The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals. ...
05/22/2012
8178538Pyridazinones
The present invention is concerned with novel pyridazinones of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologicall...
05/15/2012
8153634Carbinol derivatives having cyclic linker
[Object] To provide a novel LXRβ agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that ar...
04/10/2012
8044053Sulfonamide substituted pyrazoline compounds, their preparation and use as CB1 modulators
The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.
10/25/2011
8017610Phenylpyrrole derivative
The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof:
09/13/2011
8008301Histamine H3 receptor agents, preparation and therapeutic uses
The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine—H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invent...
08/30/2011
8003650Hydrazide compound and harmful arthropod-controlling agent containing the same
Disclosed is a hydrazine compound represented by the formula (1) below, which has an excellent control activity against a harmful arthropod. (1) (In the formula, R1, R5, R6 and R7 represent a hydrogen atom or the like; R
08/23/2011
8003649Bicyclic derivatives for use in the treatment of androgen receptor associated conditions-155
The invention concerns bicyclic compounds of Formula I wherein the integers X1, X2, X3, Ring A, R4, R5 and m are as defined in the description. The present invention al...
08/23/2011
7943619Isoxazolo-pyridazine derivatives
The invention relates to isoxazolo-pyridazine compounds, in particular those of formula I as described above and to a pharmaceutically acceptable salts thereof, having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, pharmaceutic...
05/17/2011
7875615Substituted triazole derivatives as oxytocin antagonists
The present invention relates to a class of substituted 1,2,4-triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety ...
01/25/2011
7790724c-fms kinase inhibitors
The invention is directed to compounds of Formula II: wherein A, R1, R2, R3, R4, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmac...
09/07/2010
7772235mGluR5 modulators
The present invention is directed to compounds of formula I: Wherein R1 to R5, X and Z are further defined in the description. The invention also relates to processes for the preparation of the compoun...
08/10/2010
7759349Control of parasites in animals by the use of imidazo[1,2-b]pyridazine derivatives
Novel imidazo[1,2-b]pyridazine compounds useful for controlling parasites in animals and methods of treatment of parasite infestation in animals using the compounds are disclosed. ...
07/20/2010
7678796MGluR5 modulators I
The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds. ...
03/16/2010
7666871Oxazole derivatives as histamine H3 receptor agents, preparation and therapeutic uses
The present invention discloses novel aryl oxazole compounds of Formula I (I), or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing and using such compounds. In anothe...
02/23/2010
7511042Triazole compounds
Disclosed are compounds of formula (I) Where Ar1, X, R3, R4, R5 and R6 are defined herein. The compounds of the invention inhibit production of cytokines and are thus u...
03/31/2009
7452885Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and ...
11/18/2008
7432254Method for treating glaucoma IC
Provided is a method of treating or ameliorating or preventing glaucoma, decreasing intraocular pressure or improving or amemliorting ocular accommodation in an animal, including a human comprising administering an intraocular pressure decreasing or accommodation im...
10/07/2008
7429581Pyrazole-derivatives as factor Xa inhibitors
The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is...
09/30/2008
7399765Substituted diazabicycloalkane derivatives
Compounds of formula (I) Z-Ar1—Ar2  (I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substitute...
07/15/2008
7396831Vanilloid receptor ligands and their use in treatments
Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascu...
07/08/2008
7368573Triamide-substituted heterobicyclic compounds
This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R1-R7, X1, m and n are as defined in the specification, as well as pharmaceutical compositions comprising the ...
05/06/2008
7361654Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory- and immune-associated disea...
04/22/2008
7335753Bifunctional heterocyclic compounds and methods of making and using same
The invention provides a family of bifunctional heterocyclic compounds useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. The invention also provides methods of making the bifunctional heterocyclic compounds, and methods of using...
02/26/2008
7335658Pyridazine derivatives and their use as therapeutic agents
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): ...
02/26/2008
7323480Substituted triazoles as modulators of PPAR and methods of their preparation
The present invention is directed to certain novel triazole compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof. The present invention is also directed to methods of making and using such compounds and p...
01/29/2008
7309701Pyridazinone derivatives as pharmaceuticals and pharmaceutical compositions containing them
The present invention relates to novel pyridazinone derivatives of the general formula (I) wherein A is A1 or A2; ...
12/18/2007
7288542Non-nucleoside reverse transcriptase inhibitors
The present invention relates to a compounds according to formula I, methods for treating diseases mediated by human immunodeficieny virus by administration of a compound according to formula I and pharmaceutical compositions for treating diseases mediated by human ...
10/30/2007
7259175Peroxisome proliferator activated receptor modulators
The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I: wherein: (a) R5 is selected from the group consisting of (C1-C6) alkyl, (C1-C
08/21/2007
7253170Pyrazole-amine compounds useful as kinase inhibitors
The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5...
08/07/2007
7253169Aza compounds, pharmaceutical compositions and methods of use
The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities. ...
08/07/2007
7241760Heteroaryl-substituted imidazole derivatives
The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3 and R4 are described hereinbelow. These compounds can be used in the tr...
07/10/2007
7223760Substituted triazole compounds
Novel substituted triazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ...
05/29/2007
7214678Arylsulfanyl and heteroarylsulfanyl derivatives for treating pain
According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.
05/08/2007
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
71867222-heteroaryl-3,4-dihydro-2h-pyrrole derivatives and the use thereof as pesticides
Novel Δ1-pyrrolines of the Formula (I) in which R1, R2, R3 and Het have the meanings given in the description, a plurality of processes for prep...
03/06/2007
7179812Diazine derivatives
The present invention provides compounds of formula (I): their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, ph...
02/20/2007
7179806Δ1-pyrrolines used as pesticides
The invention relates to novel Δ1-pyrrolines of the formula (I) in which R1, R2, R3, m, and Q have the meanings given in the disclosure, to a plurality of processes fo...
02/20/2007
7173044Imidazoline derivatives having CB-antagonistic activity
The present invention relates to 1,2,4-tri-substituted imidazoline derivatives, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazoline derivatives, to methods for the preparation of these intermediates,...
02/06/2007
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