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Class 544/336 - 1,4-diazines


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the six-membered hetero ring has nitrogens
No. of patents: 810
Last issue date: 05/22/2012


  2                    
NumberTitleIssue Date
72591634-(6-membered)-heteroaryl acyl pyrrolidine derivatives as HCV inhibitors
Novel anti-viral agents of Formula wherein: A represents OR1, NR1R2, or R1 wherein R1 and R2 are hydrogen, C1-6alkyl, aryl...
08/21/2007
7259179Kinase inhibitors
A compound of the general formula: or pharmaceutically acceptable salts, hydrates, solvates, crystal forms or diastereomers thereof is described. A method of treating protein kinase-associated disease states usin...
08/21/2007
72561883-aminoalkyl-2-aryl-indole derivatives and their use as GnRH antagonists
The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use of a compound of the present invention in the manufacture of a medicam...
08/14/2007
7250414Diphenylmethyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, e, m, n, Ar1, R1, R2, R3, R4a, R4b, R5 and R6 are as defined ...
07/31/2007
RE39754Benzamide derivatives and pharmaceutical compositions containing same
The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune...
07/31/2007
7229988Dialkylhydroxybenzoic acid derivatives containing metal chelating groups and their therapeutic uses
The present invention provides novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups and the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen spe...
06/12/2007
7223762Beta-amino acid derivatives-inhibitors of leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, su...
05/29/2007
72207532,7-substituted octahydro-1H-pyrido[1,2-a]pyrazine derivatives as ligands for serotonin receptors
Substituted pyrido[1,2-a]pyrazines of general formula I; wherein Ar and Ar1 represent various carbocyclic and heterocyclic aromatic rings; A represents O, S, SO, SO2, CHOH, C═O, or —(CR3R4); and n is 0–2, as well as ...
05/22/2007
72207411,4-diazabicycloalkane derivatives, their preparation and use
This invention relates to novel 1,4-diazabicycloalkane 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 modulators of the mono...
05/22/2007
7220783Para-terphenyl compounds
The present invention provides a selective suppressor of the IgE production comprising a compound which suppresses the IgE production in a process from a differentiation of a mature B cell into an antibody-producing cell to the production of an antibody and which do...
05/22/2007
72207401,4-diazabicyclo[3.2.2]nonabenzoxazole, -benzothiazole and benzimidazole derivatives, preparation and therapeutic use thereof
Compound corresponding to the general formula (I) in which X represents an oxygen or sulphur atom or an NH group and R1, R2, R3 and R4 each represent a hydrogen or halo...
05/22/2007
7220735Benzimidazolone histamine Hantagonists
Disclosed are novel compounds of the formula wherein R1 is benzimidazolone derivative, M1 and M2 are optionally substituted carbon or nitrogen, R2 includes optionally s...
05/22/2007
7217714CCR5 modulators
Compounds of Formula 1 [Region α]−[Region β]−[Region γ]−[Region δ]   (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and m...
05/15/2007
7214701Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ...
05/08/2007
7208169Biphenyl carboxamides
The invention relates to novel biphenylcarboxamides of the formula (I) in which R1, R2, m, n, R3, Y and A are as defined in the disclosure, to a plurality...
04/24/2007
7205302Heterocyclic compound derivatives and medicines
The present invention provides a compound which is useful as a PGI2 receptor agonist, and a pharmaceutical composition. The present invention is directed to a pharmaceutical composition comprising a compound represented by the following formula [1]...
04/17/2007
7202244Chk-1 inhibitors
Disclosed are novel inhibitors of Chk-1 and methods of using the same for therapy. ...
04/10/2007
7202368Process for the preparation of 4-(benzimidazolymethylamino) benzamidines
A process for preparing an optionally substituted 4-benzimidazol-2-ylmethylamino)benzamidine, the process comprising: (a) condensing an optionally suitably substituted diaminobenzene with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)phenylamino...
04/10/2007
7196084Cdc25 phosphatase inhibitors
The invention concerns novel cdc25 phosphatase inhibitors, and in particular cdc25-C, which correspond to the general formula (I) wherein: A represents a carbocyclic aryl radical optionally substituted 1 to 3 times by one or more radicals independently selected amon...
03/27/2007
7186847Process for the direct preparation of pyrrolo[3,4-c]pyrroles
The present invention relates to a process for the direct preparation of pyrrolo[3,4-c]pyrroles (DPPs) of the formula (1), pigment compositions containing them and their use for coloring high molecluar weight organic materials, such as plastics and paints. The obtai...
03/06/2007
7186843Aminomethylpyrrolidine derivatives having aromatic substituents
This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of th...
03/06/2007
71798075-substituted-2-arylpyrazines
Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators or CRF receptors. Compounds of the invention are provided by the following formula: The 5-substituted-2-aryl...
02/20/2007
7176200Derivatives of sulphonamides, their preparation and use as medicaments
The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the ph...
02/13/2007
7176312Kinase inhibitor scaffolds and methods for their preparation
General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, bor...
02/13/2007
7173131Anthryl derivative group substituted compound, and organic luminescent device making use of same
An anthryl derivative group substituted compound having a specific chemical structure is provided. This compound is used for producing an organic luminescent device which can emit luminescent hues with a very high purity and effect light emission with a high lumines...
02/06/2007
7160872Methods to treat conditions mediated by chemokine receptors
The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV-infected cells as well as othe...
01/09/2007
7160896Therapeutic acridone and acridine compounds
The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is ═O, L is —H, alpha single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bon...
01/09/2007
7153868N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a c...
12/26/2006
7153815Insecticide containing hydrazone derivative as the active ingredient and novel hydrazone derivative
A insecticide characterized by containing as active ingredient a hydrazone derivative of formula (I) wherein A and Q are an aryl or a heterocyclic group, W is oxygen atom, an aminylene, an alkylene group, an oxya...
12/26/2006
7153857Arylpiperazines and arylpiperidines and their use as metalloproteinase inhibiting agents
Compounds of the formula I useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13. ...
12/26/2006
7148311Liquid crystal polymers
Liquid crystal polyester derived from phenylene-naphthalene monomers and one or more comonomers display an improved balance of properties, including low melt viscosity, fast cycle time in molding, very low mold shrinkage, high tensile and/or flexural strength, solve...
12/12/2006
7145004Method for the production of monohydro-perfluoroalkanes, bis(perfluoroalkyl)phosphinates and perfluoroalkylphosphonates
The present invention relates to a process for the preparation of monohydroperfluoroalkanes, bis(perfluoroalkyl)phosphinates and perfluoroalkylphosphonates which comprises at least the treatment of at least one perfluoroalkylphosphorane with at least one base in a s...
12/05/2006
7135499Active substance combinations having insecticidal and acaricidal properties
The present invention relates to novel insecticidally and acaricidally active compound combinations of N2-[1,1-dimethyl-2-(methylsulphonyl)ethyl]-3-iodo-N1-{2-methyl-4-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl}phthalamide of the form...
11/14/2006
7125878Substituted pyrroline kinase inhibitors
The present invention is directed to novel substituted pyrroline compounds useful as kinase inhibitors and methods for treating or ameliorating a kinase mediated disorder. ...
10/24/2006
7122550Protein kinase inhibitors
A compound of the general formula: or pharmaceutically acceptable salts, hydrates, solvates, crystal forms of diastereomers thereof is described. A method of treating protein kinase-associated disease states usin...
10/17/2006
7119203Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors
This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metallop...
10/10/2006
7105505Benzimidazole derivatives useful as histamine H3 antagonists
Disclosed are novel compounds of the formula wherein R1 is optionally substituted benzimidazolyl or a derivative thereof; R2 is optionally substituted aryl or heteroaryl; M1 and M...
09/12/2006
7105671Substituted-cycloalkyl and oxygenated-cycloalkyl glucokinase activators
2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a polar ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of...
09/12/2006
7102014Pigment dispersants based on diketopyrrolopyrrole compounds and pigment preparations
The invention provides novel pigment dispersants of the formula (I): in which Q is a radical of the formula (Ia): s is a number from 0.1 to 4.0 and n is a...
09/05/2006
7101915P-terphenyl compounds
The present invention provides a selective suppressor of the IgE production comprising a compound which suppresses the IgE production in a process from a differentiation of a mature B cell into an antibody-producing cell to the production of an antibody and which do...
09/05/2006
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