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Class 514/235.5 - Ring nitrogen in the additional hetero ring


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter in which the additional hetero ring contains
No. of patents: 673
Last issue date: 05/29/2012


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NumberTitleIssue Date
81880793-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as ther...
05/29/2012
8178528Histamine 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 and intermediates for preparing such compounds. In another embod...
05/15/2012
8173651Pyridine compounds
This invention features compounds of formula (I): pharmaceutical compositions of the compounds, and methods of using the compounds for the treatment of, inter alia, IL-12-related diseases and disorders. ...
05/08/2012
8148373Compounds
The present invention relates to spirocyclic amide derivatives of the formula I, pharmaceutically acceptable salts thereof, a process for their preparation, pharmaceutical compositions containing them, and their use in ther...
04/03/2012
8129376Piperidine derivatives as inhibitors of stearoyl-CoA desaturase
The present invention relates to piperidine 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. ...
03/06/2012
8124605Compositions and methods for modulating a kinase cascade
The invention relates to compounds and methods for modulating one or more components of a kinase cascade. ...
02/28/2012
8097624Cycloalkyl derivatives of 3-hydroxy-4-pyridinones
The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological...
01/17/2012
8076329Histamine H3-receptor ligands and their therapeutic applications
The present patent application concerns compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for ...
12/13/2011
8071594Substituted diketopiperazines and their use as oxytocin antagonists
Compounds of formula (1) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is 2-methyl-1,3-oxazol-4-yl and R4 and R5 together with the notrogen atom to which they are a...
12/06/2011
8063043Salts of N-[6-cis-2,6-dimethylmorpholin-4-yl)pyridine-3-yl]-2-methyl-4′-(trifluoromethoxy)[1,1′-biphenyl]-3-carboxamide
Salts of N-[6-(cis-2,6-dimethylmorpholin-4-yl)pyridine-3-yl]-2-methyl-4′-(trifluoromethoxy)[1,1′-biphenyl]-3-carboxamide are prepared and characterized. ...
11/22/2011
8026237Pyrrole derivatives as pharmaceutical agents
Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of di...
09/27/2011
8017607N-substituted-pyrrolidines as inhibitors of MDM2-P-53 interactions
There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, and R5 are as described herein and enantiomers and pharmaceutically a...
09/13/2011
801296911C-labeled benzyl-lactam compounds and their use as imaging agents
The invention relates to “C-labeled compounds, their preparation, compositions comprising an effective amount of a “C-labeled compound, and the use of a “C-labeled compound as a radiopharmaceutical for positron emission tomography. ...
09/06/2011
8012970Derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine, synthesis process and uses thereof
The present invention concerns pyrrole compounds, derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine (BM212). The invention concerns the use of the described compounds as antitubercular agents having high activity and low t...
09/06/2011
8008296Histamine 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 invention d...
08/30/2011
8003642Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient
The compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof specifically binds CCR5, so it is useful for preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, ne...
08/23/2011
8003641Compositions and methods of treating cell proliferation disorders
The invention relates to compounds and methods for treating cell proliferation disorders. ...
08/23/2011
7998959Modulators of 11-β hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same
The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1 and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydr...
08/16/2011
7964596Therapeutic compounds
Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein Y, A, B, and J are as described. Methods, compositions, and medicaments related thereto are also disclosed....
06/21/2011
7956052Modulators of ATP-binding cassette transporters
Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The ...
06/07/2011
7951804Piperidinyl compounds
Novel compounds of the formula (I) in which D, E, Q, T, X, Y, Z, Z′, R1, R4 and R4′ have the meanings indicated, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic dis...
05/31/2011
7947680Adamantyl diamide derivatives and uses of same
The present invention provides adamantyl-diamide derivatives of formula (I): wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and ...
05/24/2011
7939529Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof
The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. More specifically, the invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoe...
05/10/2011
7935697Compositions for modulating a kinase cascade and methods of use thereof
The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridi...
05/03/2011
7932252Aryl sulfonamides
The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases. ...
04/26/2011
7928103Compounds which modulate the CB2 receptor
Compounds of formula (I) are disclosed. Compounds according to the invention are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
04/19/2011
7906510Amide derivative and pharmaceutical composition containing the same
Disclosed is a compound having a strong affinity to serotonin-4 receptors, which is useful as an enterokinesis-promoting agent or a digestive tract function-improving agent. Specifically, disclosed is a compound represented by Formula (1) or a pharmaceutically accep...
03/15/2011
7902191Histamine H3 receptor antagonists, preparation and therapeutic uses
The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceuti...
03/08/2011
7893061Alkyne-substituted pyridone compounds and methods of use
The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The...
02/22/2011
7893062Pyrrolidine derivatives as dual NK1/NK3 receptor antagonists
The invention relates to pyrrolidine derivatives of formula wherein R1, R2, R3, n, and o are defined in the specification and to pharmaceu...
02/22/2011
7879852Melanocortin receptor agonists
The present invention relates to a compound of the following formula 1, pharmaceutically acceptable salt and isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient....
02/01/2011
7858621Compounds, isomer thereof, or pharmaceutically acceptable salts thereof as vanilloid receptor antagonist; and pharmaceutical compositions containing the same
This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention pro...
12/28/2010
7851470Composition and methods for modulating a kinase cascade
The invention relates to compounds and methods for modulating one or more components of a kinase cascade. ...
12/14/2010
7838523Certain substituted amides, method of making, and method of use thereof
At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical c...
11/23/2010
7825115Cyclic urea compounds, preparation thereof and pharmaceutical use thereof as kinase inhibitors
The disclosure relates to a cyclic urea compound of formula I: as defined herein, to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use as an inhibitor on a protein kinase. ...
11/02/2010
7812020Substituted pyridine derivatives
The present invention relates to pyridine derivatives of the general formula (I) and their use as openers of the KCNQ family potassium ion channels for the treatment of CNS disorders. ...
10/12/2010
7812021Pyrrolidine aryl-ether as NK3 receptor antagonists
The invention relates to a compound of general formula wherein Ar, R1, R2, R3, R4, n, o, p, s, X and are as def...
10/12/2010
7807672Compounds that are ERK inhibitors
Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a do...
10/05/2010
7781435Imidazole compounds for the treatment of neurological disorders
The present invention relates to compounds of Formula I wherein R1, R2, R3, R4, R6, R7 and A are as defined. Compounds of Formula I have activity inhibiting ...
08/24/2010
7723332Aryl sulfonamides useful for modulation of the progesterone receptor
In one embodiment, compounds of the following structure are described, wherein R1to R7are described herein. Also provided are methods for preparing these compounds and methods of contraception; treating ...
05/25/2010
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