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Class 514/221 - Bicyclo ring system having the seven-membered hetero ring as one of the cyclos


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the polycyclo ring system consists
No. of patents: 648
Last issue date: 05/29/2012


1                      
NumberTitleIssue Date
8188072Benzodiazepinone compounds useful in the treatment of skin conditions
The present invention provides a family of benzodiazepinone compounds and pharmaceutical compositions thereof. The present invention also provides methods of treating certain skin conditions, e.g., atopic dermatitis, rosacea, or psoriasis, by administering a benzodi...
05/29/2012
8168626Benzodiazepine compositions for treating epidermal hyperplasia and related disorders
The present invention provides, for example, pharmaceutical compositions comprising a benzodiazepine compound and an agent selected from the group consisting of a topical steroid, a keratolytic agent, a topical retinoid, a coal tar, and a vitamin D-3 analog. The pha...
05/01/2012
8168625Pharmaceutical composition based on agonist of benzodiazepine
The present invention describes the use of pharmaceutical compounds in pharmaceutical compositions for sublingual administration, including as active ingredient thereof, an agonist of the central receptor of benzodiazepinics chosen among diazepam, lorazepam, bromaze...
05/01/2012
8163738Aminodiazepines as toll-like receptor modulators
Provided are compositions and methods useful for modulation signaling through the Toll-like receptor TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, se...
04/24/2012
8163737CGRP receptor antagonists
The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions. ...
04/24/2012
81586191,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl compounds and their medical use
This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and mod...
04/17/2012
8148366Substituted pyrazolo[3,4-E][diazepin-6-5(H)ones and analogues thereof, their preparation and their use as antibacterial medicaments
The invention relates to nitrogenous heterocyclic compounds of formula (I): in which: R1 represents hydrogen, —(CH2)m—NH2, —(CH2)m—NH(C
04/03/2012
8119631Inhibitors of interleukin-1β converting enzyme
The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmace...
02/21/2012
8119630Benzodiazepine derivatives and pharmaceutical compositions containing them
Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV Formula (I) Wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 ...
02/21/2012
81060421,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives useful as modulator of nicotinic acetylcholine receptors
This invention relates to novel N-oxides of a 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivative and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine rece...
01/31/2012
81015981,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their medical use
This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors.
01/24/2012
8097612Compositions and methods relating to novel compounds and targets thereof
The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and related compounds and methods of using benzodiazepine derivatives and rela...
01/17/2012
8044043CGRP receptor antagonists
The disclosure generally relates to the novel compounds of formula I, including their salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorder...
10/25/2011
8026234Polo-like kinase inhibitors
Compounds of the following formula are provided for use with kinases: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; m...
09/27/2011
8012960Heterocyclic aspartyl protease inhibitors
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as d...
09/06/2011
7985747Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereom...
07/26/2011
7977330Salts and crystal modifications thereof
The invention relates to salts of 1-(2-Fluoro-phenyl)-3-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-urea and crystalline forms thereof, their production and usage, and pharmaceutical preparations containing such salts and crystalline forms. ...
07/12/2011
79603758-chloro-2,3-benzodiazepine derivatives
The invention relates to new 8-chloro-2,3-benzodiazepine derivatives of the general formula (I), wherein R stands for a lower alkyl group or a group of the general formula —NH—R′, wherein R′ stands for a lower alkyl or a lower cycloalkyl group), and pharmace...
06/14/2011
79356951,4-diaza-bicyclo[3.2.2]nonyl heteroaryl derivatives useful as nicotinic acetylcholine receptor ligands
This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl heteroaryl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. ...
05/03/2011
79105788,10-diaza-bicyclo[4.3.1]decane derivatives and their medical use
This invention relates to novel 8,10-diaza-bicyclo[4.3.1]decane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of di...
03/22/2011
7868000Aspartyl protease inhibitors
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein j, k, U, W, R, R1, R2, R3, R4, R6,...
01/11/2011
7851465Compositions and methods relating to novel compounds and targets thereof
The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine compounds, and structurally and functionally related compounds, and methods of using such ...
12/14/2010
7834006Fused polycyclic compounds
The following fused polycyclic compound, analogues thereof or pharmaceutically acceptable salts thereof have an effect of increasing the sugar-transporting capacity and an effect of lowering the blood glucose level and, therefore, they are useful for preventing and/...
11/16/2010
7807666CGRP antagonists
The invention relates to a method for treating irritable bowel syndrome through the use of effective amounts of a compound acting as CGRP antagonist. ...
10/05/2010
78076671,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their medical use
This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors.
10/05/2010
7795248Substituted 7,8-dihydro-1H-pyrimido[4,5-B][1,4]diazepin-4-amines are novel kinase inhibitors
Compounds having the Formula (I) are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment usin...
09/14/2010
7790713Inhibitors of interleukin-1β converting enzyme
The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmace...
09/07/2010
7763606Heterocyclic aspartyl protease inhibitors
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as d...
07/27/2010
7763605[1,4]benzodiazepines as vasopressin V2 receptor antagonists
The invention is directed to novel [1,4]benzodiazepine compounds useful as vasopressin receptor antagonists for treating conditions involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising [1,4]benzodiazepine compound...
07/27/2010
7759338Soluble 1,4 benzodiazepine compounds and stable salts thereof
The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and related compounds and methods of using benzodiazepine derivatives and rela...
07/20/2010
7745431Pharmaceutical composition of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine and uses thereof
Pharmaceutical compositions comprising 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine; or a pharmaceutically acceptable salt thereof. The compositions are used for treating, preventing or delaying the onset of disorders mediated b...
06/29/2010
7718651Inhibitors of FtsZ and uses thereof
The invention relates to inhibitors of FtsZ polymerization and uses thereof. ...
05/18/2010
7700589CGRP antagonists
CGRP antagonists of the formula of which the following are exemplary: (1) 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylic acid-{(R)-1-(3,4-diethyl-benzyl)-2-[4-(1-methyl-piperidin-4-...
04/20/2010
7700588Pharmaceutical compositions comprising midazolam in a high concentration
Compositions of midazolam, a benzodiazapine, in concentrations of 35-100 mg/ml are disclosed for the treatment of anxiety, epilepsy and epileptic seizures, invasive surgical procedures and diagnostic procedures and sedation. These compositions are particularly chara...
04/20/2010
7696196Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereomers, ...
04/13/2010
7696195Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
The present invention relates to the CGRP antagonists of general formula wherein A, X, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, t...
04/13/2010
7678788Diazabicyclic aryl derivatives
This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or diso...
03/16/2010
7662812Diazabicyclic aryl derivatives and their use as chinolinergic ligands at nicotinic acetylcholine receptors
This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the in...
02/16/2010
7655647Substituted lactams as inhibitors of Aβ protein production
This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor prote...
02/02/2010
76328311H-indazoles, benzothiazoles, 1,2-benzoisoxazoles, 1,2-benzoisothiazoles, and chromones and preparation and uses thereof
The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of ...
12/15/2009
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