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Class 514/248 - Polycyclo ring system having a 1,2- or 1,4-diazine as one of the cyclos


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the six-membered heterocyclic ring
No. of patents: 1001
Last issue date: 05/15/2012


1                      
NumberTitleIssue Date
81785332-oxo-1-pyrrolidine derivatives, processes for preparing them and their uses
The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals. ...
05/15/2012
8178534cMET inhibitors
Compounds of the following formula are provided for use with cMET: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; meth...
05/15/2012
8173655Bicyclic anilide heterocyclic CGRP receptor antagonists
Compounds of formula I: (wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 and Y are as described herein) which are antagonists of CGRP receptors and whic...
05/08/2012
8173654Triazolopyridazine compounds
The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyro...
05/08/2012
8168636Polycyclic heteroaryl substituted triazoles useful as Axl inhibitors
Polycyclic 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 diseases or conditio...
05/01/2012
8168635Modulators of central nervous system neurotransmitters
Disclosed are agents having pharmacological activity against cellular receptors and intracellular signaling, particularly receptors and signaling pathways of central nervous system (CNS) neurotransmitters. Also disclosed are related methods and compositions for the ...
05/01/2012
8163749Six-membered heterocycles useful as serine protease inhibitors
The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, R3 and R11 are as defined her...
04/24/2012
8153632Oxygen linked pyrimidine derivatives
The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions con...
04/10/2012
8143253Organic compounds
Compounds of formula I in free or salt or solvate form, where R1, R2 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical c...
03/27/2012
8129381Caspase inhibitors and uses thereof
The present invention relates to compounds of formula I: useful as inhibitors of caspases. The present invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for preparing the ...
03/06/2012
8129382Compounds, methods and pharmaceutical compositions for inhibiting PARP
The present invention provides compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.
03/06/2012
8129380Phthalazinone derivatives
A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; X and Y are selected from CH and CH, CF and CH, CH and CF and N and CH respectively; RC
03/06/2012
8119635Diazabicyclic central nervous system active agents
Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals. ...
02/21/2012
8114874Substituted acetylenic imidazo[1,2-B]pyridazine compounds as kinase inhibitors
This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use. In particular, the compounds include embodiments in ...
02/14/2012
8101612Phthalazine compounds and methods of use
The present invention comprises a new class of compounds useful for the prophylaxis and treatment of p38 kinase mediated diseases and related inflammatory conditions. The compounds have a general Formula II wherein L1
01/24/2012
8097627Multiply-substituted tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents
The invention relates to multiply-substituted tetrahydronaphthalene derivatives of formula (I) process for their production and their use as anti-inflammatory agents. ...
01/17/2012
8093247Heteroaryl sulfonamides and CCR2
Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in...
01/10/2012
8088773Therapeutic compositions and methods
The present invention relates in general to therapeutic compositions and methods of use. In preferred embodiments, the invention relates to the field of eye health. In some embodiments, the invention relates to the prevention and treatment of macular degeneration by...
01/03/2012
8076336Triazolopyridazines as PAR1 inhibitors, production thereof, and use as medicaments
The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, Q1, Q2 and Q3 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-ac...
12/13/2011
8063049Inhibitors of MEK
This invention concerns to N-(2-aylamino)aryl sulfonamides, which are inhibitors of MEK, methods of using such compounds in the treatment of hyperproliferative diseases, and to pharmaceutical compositions containing such compounds. ...
11/22/2011
8063047Pyridazine compounds and methods
The invention relates to novel chemical compounds of Formula I compositions and methods of using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions com...
11/22/2011
8063048Acetylenyl-pyrazolo-pyrimidine derivatives
The present invention relates to compounds of formula (I): wherein R1 to R3, A, M, L, E, G, and J are as defined in the description and claims. The invention also relates to a process for the manufactu...
11/22/2011
8058274Heterocycles as potassium channel modulators
Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods...
11/15/2011
8044050Imidazo[1,2-a]azines and their use as pharmaceuticals
The present invention relates to derivatives of imidazo[1,2-a]azines of formula I, in which R, R1 to R3, X, Y and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO...
10/25/2011
8044049Fused heterocyclic derivative and use thereof
The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the specifica...
10/25/2011
8034812Imidazopyridazine derivative having kinase inhibitory activity and pharmaceutical agent thereof
The present invention provides an imidazopyridazine derivative compound having a potent kinase inhibitory activity and a pharmaceutical agent thereof useful for treatment or prevention of cancer and the like. One such compound is represented by the formula:
10/11/2011
8030305Triazolopyridazines as kinase modulators
The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyro...
10/04/2011
8030306Azabicyclic heterocycles as cannabinoid receptor modulators
The present application describes CB-1 inverse agonists according to Formula (I) and (Ia), pharmaceutical compositions comprising at least one compound according to Formula (I) or (Ia), and optionally one or more additional therapeutic agents and methods of treatmen...
10/04/2011
8003647(Aza)indole derivative and use thereof for medical purposes
The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by...
08/23/2011
8003646Substituted triazolo-pyridazine derivatives
This invention relates to novel substituted triazolo-pyridazines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treat...
08/23/2011
7994167Pentafluorosulphanyl-substituted compound and its use for producing medicaments
The present invention relates to pentafluorosulphanyl-substituted compounds, methods for their production, medicaments containing such compounds and the use of such compounds for producing medicaments. ...
08/09/2011
7989452Stable hydrazalazine pharmaceutical compositions
The present invention relates to stable and highly purified stable hydralazine hydrochloride compositions and stable hydralazine-containing pharmaceutical compositions. A sterile aqueous injectable pharmaceutical composition suitable for parenteral administration is...
08/02/2011
7981889Phthalazinone derivatives
Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X═NRX then n is 1 or 2 and if X═CR
07/19/2011
7981892Disubstituted phthalazine hedgehog pathway antagonists
The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer. ...
07/19/2011
7981890Phthalazinone derivatives
A compound of the formula (I): wherein RH represents one or more optional substituents on the fused cyclohexene ring; R1 is selected from H and halo; RN is selected from H and optionally sub...
07/19/2011
7981891Aurora kinase modulators and method of use
The present invention relates to chemical compounds having a general formula I wherein A1-8, D′, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediate...
07/19/2011
7977333Substituted pyridines and pyridazines with angiogenesis inhibiting activity
Substituted and pyridines and pyridazines having angiogenesis inhibiting activity and the generalized structural formula wherein the ring containing A, B, D, E, and L is phenyl or a nitrogen-containing heterocycle; groups X...
07/12/2011
7977334Beta-agonists, methods for the preparation thereof and their use as pharmaceutical compositions
The present invention relates to new beta-agonists of general formula (I) wherein the groups R1 to R7 have the meanings given in the claims and specification, the tautomers, the enantiomers, the diaste...
07/12/2011
7943615Fused aminopiperidines as dipeptidyl peptidase-4 inhibitors for the treatment or prevention of diabetes
The present invention is directed to novel substituted fused aminopiperidines of structural formula (I) which are inhibitors of the dipeptidyl peptidase-4 enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-4 enzy...
05/17/2011
7932253Immunomodulating oxopyrrazolocinnolines as CD80 inhibitors
N-(1-Aza-bicyclo[2.2.2]oct-3-yl)-4-(6,9-difluoro-3-oxo-1,3-dihydro-pyrazolo[4,3-c]cinnolin-2-yl)-benzamide is a CD80 antagonist, useful in the treatment of diseases which benefit from immuno-inhibition. ...
04/26/2011
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