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Class 514/218 - Hetero ring is seven-membered consisting of two nitrogens and five carbon atoms


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter which contains a seven-membered heterocyclic
No. of patents: 976
Last issue date: 05/29/2012


1                      
NumberTitleIssue Date
8188071Amino substituted pyridines as potent kinase inhibitors
The present invention relates to compounds useful as inhibitors of protein kinase of the following structural formula: The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods...
05/29/2012
8183237Benzenesulfonanilide compounds suitable for treating disorders that respond to modulation of the serotonin 5-HTreceptor
The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I′ and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for trea...
05/22/2012
8173640Compositions and methods for treating, reducing, ameliorating, or preventing infections
Compositions for treating, reducing, ameliorating, or preventing infections comprise a fluoroquinolone having Formulae I-VIII and an additional anti-infective agent. Methods for treating, reducing, ameliorating, or preventing such infection use such compositions. Su...
05/08/2012
8173639Isoquinolinone derivatives as NK3 antagonists
Isoquinolone derivatives of the general formula are provided. The compounds are NK3 antagonists and useful for the treatment of e.g. psychosis and schizophrenia. ...
05/08/2012
81483651,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivative and its medical use
This invention relates to a novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivative and its use in the manufacture of pharmaceutical compositions. The compound of the invention is found to be a cholinergic ligand at the nicotinic acetylcholine receptors. D...
04/03/2012
8138175Heterocyclyl compounds
The invention is concerned with novel heterocyclyl compounds of formula (I): wherein A, X, R3, R4, R5, R6, R7, R8, R9, R10, m, n and p ...
03/20/2012
8114866Derivatives of 1-piperazine- and 1-homopiperazine-carboxylates, preparation method thereof and use of same as inhibitors of the FAAH enzyme
The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the...
02/14/2012
8097611Sulfonyl-derivatives as novel or histone deacetylase
This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, h...
01/17/2012
8093239Imidazopyridine kinase inhibitors
The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents. ...
01/10/2012
8088761Enzyme inhibitors
Compounds of formula (I), are aurora kinase inhibitors: wherein X is —N—, —CH2-N—, —CH2-CH—, or —CH—; R1 is a radical of formula (IA) wherein Z is —CH2-, —NH—, -0-, —S(O)— —S—, —S(O)2 or a divalent monocyclic carbocyclic or heterocycl...
01/03/2012
8084449Dual pharmacophores—PDE4-muscarinic antagonistics
The present invention is directed to novel compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions and their use as dual chromaphores having inhibitory ac...
12/27/2011
8076326N-phenyl- (piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenl-(piperazine or homopiperazine) compounds suitable for treating disorders that respond to modulation of the serotonin 5-HTreceptor
The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable th...
12/13/2011
8071589Dihydrobenzoindazoles
The invention relates to benzoindazole derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility. ...
12/06/2011
8071588Dual pharmacophores—PDE4-muscarinic antagonistics
The present invention relates to novel compounds of Formula (I) and their use in the treatment of respiratory diseases, including anti-inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD),...
12/06/2011
8067408Dual pharmacophores—PDE4-muscarinic antagonistics
The present invention is directed to novel compounds of Formula (I), pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatme...
11/29/2011
8048877Guanidine derivatives and their medical use
This invention relates to novel guanidine derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical com...
11/01/2011
8044040N-heterocyclic inhibitors of TNF-alpha expression
N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharmaceutical...
10/25/2011
8044041Phthalazine derivatives as inhibitors of protein kinase
The present invention relates to novel phthalazine derivatives and, more particularly, to phthalazine derivatives of formula (III) that are useful as protein kinase inhibitors. The invention also relates to methods of preparing the compounds, compositions containing...
10/25/2011
8039463Piperazine derivatives as inhibitors of stearoyl-CoA desaturase
The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds. ...
10/18/2011
8039462Methods and compositons for stimulating neurogenesis and inhibiting neuronal degeneration
The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the t...
10/18/2011
8022064Phenylpentadienoyl derivatives and their use as PAR 1 antagonists
The present invention relates to compounds of general formula (I): wherein: R1 and R2, identical or different, represent: an atom of hydrogen or halogen, CN or NO2, with R1 and R2 not representing hydrogen simul...
09/20/2011
8012959Diaminopyrimidinecarboxamide derivative
A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an ary...
09/06/2011
8012958Methods for treating anxiety related disorders
The present invention relates to methods of and compositions for treating and relieving symptoms and disease associated with indications caused by a physiological drive to alleviate a sensation of anxiety. In one treatment method, methods of, and compositions for, m...
09/06/2011
80082913-aminoalkyl-1,4-diazepan-2-one melanocortin-5 receptor antagonists
The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is benef...
08/30/2011
7981883Substituted spiro-compounds and the use thereof for producing medicaments
The present invention relates to substituted spiro compounds, to processes for preparing them, to medicaments comprising these compounds and to the use of these compounds for producing medicaments. ...
07/19/2011
7968539Quinoline derivatives and uses thereof
This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (su...
06/28/2011
7968538Substituted arylamine compounds and methods of treatment
The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin act...
06/28/2011
7964591Pyridazine derivatives and their use as therapeutic agents
Methods of treating an SCD-mediated skin disorder or condition in a mammal, preferably a human include administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2
06/21/2011
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
7939523Imidazolidinone and imidazolidinethione derivatives
Imidazolidinone and imidazolinethione compounds of formula (I): wherein R1, R2, R3, A1, A2, X, Y, Z, m, n, p, x, and y are defined herein. Also disclosed is a method of...
05/10/2011
7932247Mmuscarinic acetylcholine receptor antagonists
Muscarinic Acetylcholine receptor antagonists and methods of using them are provided. ...
04/26/2011
7928100Quinolone analogs and methods related thereto
The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods o...
04/19/2011
7923444Alkyl substituted homopiperazine derivatives and their use as monoamine neurotransmitter re-uptake inhibitors
This invention relates to novel alkyl substituted homopiperazine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical composit...
04/12/2011
7919489Heterocyclyamide-substituted imidazoles
The invention relates to heterocyclylamide-substituted imidazoles and methods for their preparation, their use for the treatment and/or prophylaxis of diseases as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, i...
04/05/2011
7915253Sulfonyl-substituted bicyclic compounds as modulators of PPAR
Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed. ...
03/29/2011
7897596Allosteric modulators of the Aadenosine receptor
The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allost...
03/01/2011
7893052CGRP receptor antagonists
The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W...
02/22/2011
78883487-membered ring compound and method of production and pharmaceutical application thereof
A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved: a m...
02/15/2011
7884097Methods and compositions comprising diamines as new anti-tubercular therapeutics
Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising novel diamine compositions for the treatment of infectious diseases are provided. In one embodiment, these method...
02/08/2011
7858615(S)-(-)-1-(4-fluoroisoquinolin-5-Yl)Sulfonyl-2-methyl-1,4-homopiperazine hydrochloride dihydrate
The present invention is directed to (S)-(−)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride dihydrate, to a method producing the dihydrate, and to a drug composition containing the dihydrate. The compound of the present invention ha...
12/28/2010
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