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Class 514/234.5 - Plural ring nitrogens in the bicyclo ring system


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter in which the bicyclo ring system contains
No. of patents: 545
Last issue date: 04/24/2012


1                      
NumberTitleIssue Date
81637434-carboxamide indazole derivatives useful as inhibitors of PI3-kinases
The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of P13-kinase activity. ...
04/24/2012
8153629Pharmaceutical compounds
Fused pyrimidines of formula (I): wherein R1-R3, A and n have any of the values described in the specification; and pharmaceutically acceptable salts thereof; have activity as inhibitors of PI3K and ma...
04/10/2012
81432506-7,dialkoxy quinazoline derivatives useful for treatment of cancer related disorders
In view of the great potential the quinazoline class of compounds offer, we started the synthesis and screening of a large number of new chemical entities with novel structural features. It has been surprisingly and unexpectedly found that quinazolines having 3-Ethy...
03/27/2012
8110573Pyrazole compounds that modulate the activity of CDK, GSK and aurora kinases
The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R′, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing t...
02/07/2012
8101607Pharmaceutical compounds
Provided herein are methods of treating diseases or disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase, which method includes administering to a patient in need thereof a compound that is a fused pyrimidine of formula (I):
01/24/2012
8093243Hepatitis C virus inhibitors
The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infec...
01/10/2012
8088767JAK-2 modulators and methods of use
This invention relates to the field of protein tyrosine kinases and inhibitors thereof. In particular, the invention relates to inhibitors of JAK-2, pharmaceutical compositions of the compounds for inhibiting JAK-2, methods of inhibiting JAK-2 in a cell, comprising ...
01/03/2012
8022071Nitrogenous heterocyclic compounds
The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to ...
09/20/2011
8012966Pyrrolo [3,2-c] pyridine-4-one 2-indolinone protein kinase inhibitors
The present invention relates to pyrrolo[3,2-c]pyridine-4-one 2-indolinone compounds of Formula (I) and their pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8X, Y and have ...
09/06/2011
8012965Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseas...
09/06/2011
7998958Substituted N-arylsulfonylheterocyclic amines as gamma-secretase inhibitors
Disclosed are novel gamma secretase inhibitors of the formula: Also disclosed are methods for inhibiting gamma secretase, for treating one or more neurodegenerative diseases, for inhibiting the deposition of beta amyloid prot...
08/16/2011
7968545Compositions useful as inhibitors of voltage-gated ion channels
The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of...
06/28/2011
7939528Heterocycle compounds
The present invention relates to novel compounds which are antagonist or inverse agonists at an opioid receptor. Such compounds are useful in the treatment of obesity and related diseases and/or conditions in mammals, particularly humans. Methods of making and using...
05/10/2011
7888352Phosphoinositide 3-kinase inhibitor compounds and methods of use
Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful fo...
02/15/2011
7879851Viral polymerase inhibitors
An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R
02/01/2011
7875609Urea derivatives, processes for their preparation, their use as medicaments, and pharmaceutical compositions containing them
The present invention provides compounds of Formula (I): in which R1, R′1, R2, R′2, R3, and Y have the meanings given in the description are useful in the treatment...
01/25/2011
7872003Pharmaceutical compounds
Fused pyrimidines of formula (I): wherein R1-R3, A and n have any of the values described in the specification; and pharmaceutically acceptable salts thereof; have activity as inhibitors of PI3K and ma...
01/18/2011
7855203Indazolyl-substituted pyrroline compounds as kinase inhibitors
The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating ...
12/21/2010
7855204Derivatives of gefitinib
This invention relates to novel quinazoline derivatives, their derivatives, pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases ...
12/21/2010
7846929Phosphoinositide 3-kinase inhibitor compounds and methods of use
Compounds of Formulas Ia and Ib, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediate...
12/07/2010
7842692Azaindole derivative having PGD2 receptor antagonistic activity
The present invention creates an azaindole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further providing a therapeutic agent for treating allergic diseases. A c...
11/30/2010
7829559Substituted pyrazole sigma receptor antagonists
The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to pyrazole derivatives of formula (I) and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to thei...
11/09/2010
7820659Cyclohexylimidiazole lactam derivatives as inhibitors of 11-β-hydroxysteroid dehydrogenase 1
The present invention discloses novel compounds of Formula I: (I) having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula ...
10/26/2010
7816350Substituted [1,2,3] triazolo[4,5-D]pyrimidines as cdk inhibitors
The present invention relates to a compound of formula I, or a pharmaceutically acceptable acid salt thereof. The invention further relates to the use of such compounds in the treatment of hyperproliferative skin disorders, v...
10/19/2010
78163515,6-dimethylthieno[2,3-di] pyrimidine derivatives, the preparation method thereof and the pharmaceutical composition comprising the same for anti-virus
Disclosed herein are 5,β-dimethylthieno[2,3-d]pyrimidine derivatives useful as antiviral agents. More particularly, disclosed are 5,β-dimethylthieno[2,3-djpyrimidine derivatives represented by Formula 1, having an excellent inhibitory effect on the proliferation o...
10/19/2010
7807671Diketo-piperazine and piperidine derivatives as antiviral agents
This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity usef...
10/05/2010
7799782P38 inhibitors and methods of use thereof
This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38. ...
09/21/2010
7786114Bis-azaindole derivatives, preparation and pharmaceutical use thereof as kinase inhibitors
Compounds of formula (I): wherein R1, R2, R3, R4, and R5 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and the use thereof as protein kinase inhibitors...
08/31/2010
7781433Pharmaceutical compounds
A thienopyrimidine of formula (I): and the pharmaceutically acceptable salts thereof have activity as inhibitors of PI3K with selectivity for the P110α subtype, and may be used to treat diseases and disorders arising from ...
08/24/2010
7776856Pharmaceutical compounds
Fused pyrimidines of formula (I): where A is a thiophene or furan ring and R1-R3 and n are defined in the specification. These compounds have activity as inhibitors of PI3K and may thus be used to trea...
08/17/2010
7767673N-substituted imidazopyridine c-Kit inhibitors
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-Oxide thereof, are useful in the treatment of cancer. ...
08/03/2010
7767672Aminopyrimidines useful as kinase inhibitors
The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various diseas...
08/03/2010
77547134-benzimidazol-2-ylpyridazin-3-one derivatives
Disclosed are compounds of the general formula (I), where the definition of the substituents A, B, D, E, R1 and R2 are detailed in the description, and the physiologically tolerated salts thereof, a process for the preparation of these compound...
07/13/2010
7750001Immunosuppressive agent and anti-tumor agent comprising heterocyclic compound as active ingredient
A novel method for immunosuppressive in a mammal suffering from an immune disease, including administering to the mammal a therapeutically effective amount of a heterocyclic compound represented by the general formula (I) (wherein X or other variables are as defined...
07/06/2010
7750002Pharmaceutical compounds
Fused pyrimidines of formula (I): wherein R1-R3, A and n have any of the values described in the specification; and pharmaceutically acceptable salts thereof, have activity as inhibitors of PI3K and ma...
07/06/2010
7642256Compounds which potentiate AMPA receptor and uses thereof in medicine
Compounds of formula (I) and salts are provided: along with pharmaceutical compositions, uses in treating a disease or condition mediated by a reduction or imbalance in glutamate receptor function such as schizophrenia or c...
01/05/2010
7622466Azaindole-2-carboxamide derivatives
The present invention relates to compounds of formula (I) wherein R1 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases whi...
11/24/2009
7598243Heterocyclic cyclopentyl tetrahydroisoquinoline and tetrahydropyridopyridine modulators of chemokine receptor activity
The present invention is directed to compounds of the formula I: Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the br...
10/06/2009
7598244[1,2,4]triazolo[1,5,a]pyrimidin-2-ylurea derivative and use thereof
Novel [1,2,4]triazolo[1,5-a]pyrimidine derivative of the general formula (1): (1) its prodrug or a pharmaceutically acceptable salt thereof, which exhibits an antigen presentation inhibiting activity and is useful as a preventive and/or therapeutic agent for immunol...
10/06/2009
7566708Substituted pyrazolo{3,4-D}pyrimidines as p38 map kinase inhibitors
Compounds effective as p38 MAP kinase inhibitors, methods of making the compounds, and methods of using the compounds for treatment of p38 MAP kinase-mediated diseases. ...
07/28/2009
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