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Class 514/247 - Hetero ring is six-membered consisting of two nitrogens and four carbon atoms (e.g., pyridazines, etc.)


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the active ingredient has a six-membered
No. of patents: 830
Last issue date: 05/08/2012


1                      
NumberTitleIssue Date
8173653Pyridiazinone derivatives for the treatment of tumours
Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors. ...
05/08/2012
8143252Tetrahalogenated compounds useful as inhibitors of angiogenesis
Methods for inhibiting a neoplasm in a subject and methods of inhibiting undesired angiogenesis that include administering to a subject a therapeutically effective amount of at least one novel tetrahalogenated compound, or a pharmaceutically acceptable salt thereof....
03/27/2012
8138187Substituted heteroaryl derivatives
The invention relates to substituted heteroaryl derivatives, to methods for the production thereof, to medicaments containing said compounds and to the use of substituted heteroaryl derivatives for producing medicaments. ...
03/20/2012
8110575Compounds
The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2, R3 and R4 are defined as in the description, the tautomers, the isomers, the...
02/07/2012
8101610Bisamide inhibitors of hedgehog signaling
The invention provides inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein ring A, ring B, R1, R2,...
01/24/2012
8101611Substituted pyridazines inhibitors of MEK
Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the spe...
01/24/2012
8097625Combination of sedative and a neurotransmitter modulator, and methods for improving sleep quality and treating depression
One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia and/or depression. The first component of the pharmaceutical composition is a GABA receptor ...
01/17/2012
8097626IL-8 receptor antagonists
This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (Il-8). ...
01/17/2012
8084452Substituted enaminocarbonyl compounds used as insecticides
The present application relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects. ...
12/27/2011
8080549Endothelin receptor antagonists
This invention relates to novel endothelin receptor antagonists, derivatives, acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases an...
12/20/2011
8071596Endothelin receptor antagonists
This invention relates to novel endothelin receptor antagonists, derivatives, acceptable acid addition salts, solvates, hydrates and polymorphs thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions...
12/06/2011
8048884Substituted piperazinyl pyrazines and pyridines as 5-HTreceptor antagonists
The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is —C(H)═ or —N═; m is 0, 1 or 2; R1 is optional...
11/01/2011
8048883Polymorphic form of imatinib mesylate and a process for its preparation
This invention discloses a novel stable crystal form of imatinib mesylate, designated by us as α2 Form, which is stable at room temperature and even at higher temperatures up to 120° C. and accelerated stress conditions and, freely soluble in water. Thi...
11/01/2011
8030304Thiazole pyrazolopyrimidines CRF1 receptor antagonists
The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and use thereof as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological diseases, and m...
10/04/2011
8026238Topical antifungal composition
A topical, foamable composition is provided that includes at least one antifungal agent that is able to penetrate the upper layers of skin and is retained in or on an area to be treated for a prolonged period of time, and that has a residual non-volatile component c...
09/27/2011
8026239Cell differentiation inducer
A method of treating a malignant tumor selected from the group consisting of leukemia, colorectal cancer, ovarian cancer, oral cancer, lung carcinoma, breast carcinoma, prostate carcinoma, and melanoma by administering to a patient in need thereof an effective amoun...
09/27/2011
8017609Method for the prevention of thromboembolic disorders
A method for the prevention of thrombotic, embolic and/or hemorrhagic disorders, such as cerebral infarction (stroke) or myocardial infarction, by administering levosimendan or its metabolite (II) or any of their pharmaceutically acceptable salts to a mammal in need...
09/13/2011
7977332Insecticidal N-(heteroarylalkyl)alkanediamine derivatives
Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb, Rc, Rd, b, c, Re
07/12/2011
7923446Biaryl sulfonamides and methods for using same
The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors. ...
04/12/2011
7923447Parenteral solutions containing metolazone
Disclosed herein are parenteral solutions containing 7-halo-1,2,3,4-tetrahydro-3-aryl-6-quinazoline sulfonamide in N,N-dimethylactamide, polyethylene glycol and D5W useful in the treatment of hypertension, heart failure and renal disease leading to edemat...
04/12/2011
7910586Compositions and methods for prevention and treatment of amyloid-β peptide-related disorders
The present invention provides methods and compositions for modulating levels of amyloid-β peptide (Aβ) exhibited by cells or tissues. The invention also provides pharmaceutical compositions and methods of screening for compounds that modulate Aβ levels. The inve...
03/22/2011
7893065Heterocyclic inhibitors of MEK and methods of use thereof
Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, and W are as defined in the specificati...
02/22/2011
7872008Method for treating insulin resistance, abdominal obesity, hypertension, hyperinsulinemia, and elevated blood lipids with a cortisol inhibitor
The invention concerns the use of ketoconazole and derivatives having a corresponding biological activity, and combinations thereof, in the treatment of abdominal obesity, hypertension, hyperinsulinemia, and elevated blood lipids. ...
01/18/2011
7820663Substituted enaminones, their derivatives and uses thereof
The present invention is related substituted enaminones represented by a compound of Formula I that are novel allosteric modulators of α7 nAChRs. The invention also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on ...
10/26/2010
7807674Thyroid hormone analogs
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositi...
10/05/2010
7795258Pyridazine compound and use thereof
A pyridazine compound represented by formula (1): wherein R1 and R2 are same or different and represent a C1-C4 alkyl group; R3 represents a halogen atom, a nitro group, a cyano group, a C1-...
09/14/2010
7732445Myosin light chain kinase inhibitor compounds, compostions and related methods of use
Pyridazinyl compounds, compositions and related methods of use. ...
06/08/2010
7678794Potentiators of glutamate receptors
The present invention provides a compound of formula (I): pharmaceutical compositions thereof, and methods of using the same, processes for preparing the same, and intermediates thereof. ...
03/16/2010
7659272CCR9 inhibitors and methods of use thereof
The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compound...
02/09/2010
7638516Agent for therapeutic treatment of optic nerve diseases and the like
The medicament for therapeutic and/or prophylactic treatment of the present invention has a suppressing action on the retinal degeneration induced by transient retinal ischemia, which is verified by the results for suppressing effect on retinal degeneration in trans...
12/29/2009
7638515Tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents
The invention relates to tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents. ...
12/29/2009
7625898Posaconazole polymer conjugates and methods of treatment using posaconazole and polymer conjugates thereof
Improved posaconazole-based compositions and methods of treating and preventing fungal infections, cancer or metastatic diseases are disclosed. In preferred aspects, the conjugates are PEG-posaconazole conjugates in which the PEG has a molecular weight of about 20,0...
12/01/2009
7618969Compounds which potentiate glutamate receptor and uses thereof in medicine
Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed: wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-...
11/17/2009
7608621N-substituted glycine derivatives: hydroxylase inhibitors
The invention described herein relates to certain pyridazinedione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the in...
10/27/2009
7601715Process for preparing triazole substituted azaindoleoxoacetic piperazine derivatives and novel salt forms produced therein
A process is provided for preparing triazole substituted azaindoleoxoacetic piperazine derivative. Novel intermediates produced in the above process, and novel N-1 and amorphous forms of a 1,2,3-triazole substituted azaindoloxoacetic piperazine derivatives and proce...
10/13/2009
7598247Immunomodulating heterocyclic compounds
Compounds of formula (I) are inhibitors of CD80 and useful in immunomodulation therapy: wherein R1 and R3 independently represent H; F; Cl; Br; —NO2; —CN; C1-C6 alk...
10/06/2009
7595317Barbituric acid derivatives as inhibitors of TNF-α converting enzyme (TACE) and/or matrix metalloproteinases
The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, R2, R3, R4, R
09/29/2009
7595316Heteroaryloxy nitrogenous saturated heterocyclic derivative
Compound of the formula: (I) [wherein each of X1, X2 and X3 independently represents N or CH, W represents the formula (II):(II) or the formula (III):(III) and Y represents a group of the formula (IV):(IV)], or a pharmacologically ac...
09/29/2009
7579350Scaffolds for α-helix mimicry
Functionalized pyridazine derivatives having a low molecular weight and pharmaceutical compositions thereof are useful as alpha-helix mimetics and for treating conditions and/or disorders mediated by alpha-helix-binding receptors and proteins. ...
08/25/2009
7553835Topical antifungal composition
The subject matter relates to a topical, foamable composition including at least one antifungal agent, said composition characterised in that said at least one antifungal agent is able to penetrate the upper layers of skin and is retained in or on an area to be trea...
06/30/2009
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