Class 514/249 - 1,4-diazine as one of the cyclos

Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein a 1,4-diazine ring is a part of the
No. of patents: 1503
Last issue date: 05/29/2012

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Number	Title	Issue Date
8188082	5,6,7,8-tetrahydro-imidazo[1,5-α]pyrazine derivatives The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I), wherein X represents CH2 or O; R1 represents a phenyl group, which group is independently mono-, di-, or tri-substituted wherein the substituents are...	05/29/2012
8178536	Sirtuin modulating compounds Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, dis...	05/15/2012
8178535	Substituted sulfonamide compounds having bradykinin 1 receptor activity and use thereof as medicaments Substituted sulfonamide compounds corresponding to the formula I′ wherein m, n, p, X, Y, Z, R1, RA and RB have specified meanings, processes for their preparation, pharmaceutical compositions containing these compounds, a...	05/15/2012
8173656	Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a vari...	05/08/2012
8168637	Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment of diabetes The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabet...	05/01/2012
8163751	Acylated indanyl amines and their use as pharmaceuticals The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1-R4 have the meanings given in the description, A is CH2, CHO...	04/24/2012
8163750	Fluorene derivatives, compositions containing the same and use thereof as inhibitors of the protein chaperone HSP 90 The present invention relates to compounds of formula (I): wherein R1, R2, R2′, L, Het, p and p′ are as defined herein, compositions containing them, and their use as medicinal products. ...	04/24/2012
8158629	Indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, and preparation and uses thereof The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of ...	04/17/2012
8158628	Sulfonylated 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine compounds and their use as pharmaceuticals Sulfonylated tetrahydroazolopyrazine compounds corresponding to the formula I wherein R1, R2a, R2b, R3a, R3b, R4, R8, R9a, R9b	04/17/2012
8148376	3, 4-dihydroquinoxalin-2(1H)-ones for use as stearoyl CoA desaturase inhibitors The present invention discloses 3,4-dihydroquinoxalin-2(1H)-ones for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases r...	04/03/2012
8143254	Methods for modulating ion channels In one embodiment, the invention provides an ion having the formula: (I) In another embodiment, the invention provides a method for modulating potassium, sodium, and cyclic nucleotide-modulated ion channels in a mammal in need thereof. In a further embodiment, the i...	03/27/2012
8133890	Combination of brimonidine and timolol for topical ophthalmic use Disclosed are pharmaceutical compositions comprising brimondine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressur...	03/13/2012
8129384	Imidazo[1,2-a]pyrazines as orexin receptor antagonists This invention relates to imidazopyrazine substituted piperidine derivatives and their use as pharmaceuticals. ...	03/06/2012
8129383	Aminopterin dosage forms and methods for inflammatory disorders There is disclosed dosage forms and methods for treating a patient with an inflammatory disorder with a therapeutically effective amount of aminopterin, or a pharmaceutically acceptable salt thereof, that achieve efficacy without concomitant toxicity. Specifically, ...	03/06/2012
8119636	Pyrrolopyrazine kinase inhibitors The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-i...	02/21/2012
8119637	Substituted pyrrolo[2,3-b]pyrazines and methods for kinase modulation, and indications therefor Compounds active on Fms and/or Kit protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of Fms and/or Kit protein kinases, wherein the compounds have formula I:	02/21/2012
8110576	Substituted pyrrolo[2,3b]pyrazines and methods for treatment of raf protein kinase-mediated indications Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described, wherein the compounds have the formula: In certain aspects and embodiments, the descr...	02/07/2012
8106050	Derivatives of pyrrolo-pyrazines having a kinase inhibitory activity and their biological applications The invention relates to pyrrolo[2,3b]-pyrazine derivatives having the general Formula (I) wherein R2 and R3 are identical or different and represent H, C1-C6 alkyl, said alkyl being a straight or branched-chain alkyl, which can be substituted, R6 is an optionally s...	01/31/2012
8106052	Luminescence-based methods and probes for measuring cytochrome P450 activity The present invention provides methods, compositions, substrates, and kits useful for analyzing the metabolic activity in cells, tissue, and animals and for screening test compounds for their effect on cytochrome P450 activity. In particular, a one-step and two-step...	01/31/2012
8106051	Utilities of amide compounds Compounds having an activity to enhance the expression of apoAI are provided, which are used as medicaments. Compounds of formula (I): in which ring A and Ar1 are independently a monocyclic or bicyclic aro...	01/31/2012
8101614	Substituted pyrrolo [1,2-a] pyrazines as calcium channel blockers The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV), wherein L1, R1, R2, R3, R4	01/24/2012
8101613	6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are def...	01/24/2012
8080550	Anesthetic compositions and methods of use The invention generally relates to anesthetic compositions comprising low doses of a selective a-2 adrenergic receptor agonists in combination with anesthetic agents. The invention also relates to methods of using these compositions; in particular, the use of these ...	12/20/2011
8071597	Pyrazine compounds and uses as PI3K inhibitors The present invention is related to pyrazine derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidne...	12/06/2011
8071598	3,9-diazabicyclo[3.3.1]nonane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors 3,9-diazabicyclo[3.3.1]nonane derivatives, useful as monoamine neurotransmitter re-uptake inhibitors. Also, use of these compounds in a method for therapy and in pharmaceutical compositions comprising the compounds. The 3,9-diazabicyclo[3.3.1]nonane derivatives have...	12/06/2011
8071599	Methods of treatment of chronic pain using eszopiclone The invention relates to the use of eszopiclone for the treatment of low-level, chronic pain and fatigue associated with pain. ...	12/06/2011
8067415	Compounds useful as antagonists of CCR2 The present invention provides compounds of general formula (I) or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are usefu...	11/29/2011
8067416	Methods and compositions for the treatment of metabolic disorders The present invention is directed to a novel methods and compositions for the therapeutic intervention in hyperphenylalaninemia. More specifically, the specification describes methods and compositions for treating various types of phenylketonurias using compositions...	11/29/2011
8034813	Polymorphs of brimonidine pamoate A brimonidine (5-bromo-6-(2-imidazolidinylideneamino)quinoxaline) pamoate polymorph exhibits characteristics disclosed herein. The brimonidine pamoate polymorph is included in a composition, device, or implant for use in the treatment or control of elevated intraocu...	10/11/2011
8030307	Bicyclic, C5-substituted proline derivatives as inhibitors of the hepatitis C virus NS3 protease The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4...	10/04/2011
8030308	Bicyclic sulfonamide derivatives which are L-CPT 1 inhibitors The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y are as defined in the descripti...	10/04/2011
8012974	Pyrrolopyrazinyl urea kinase inhibitors The present invention relates to the use of novel pyrrolopyrazinyl urea derivatives of Formula I, wherein the variables R1, R2, R3, R4, and R5 are defined as described ...	09/06/2011
8008298	Pyrrolopyrazine kinase inhibitors The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1, R, and X are defined as described herein, which inhibit JAK and SYK and are useful for the tre...	08/30/2011
7994168	Hexahydro-pyrazino[1,2-A]pyrimidine-4,7-dione derivatives substituted with amino acids The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives substituted with amino acids, and to the physiologically tolerated salts thereof, processes for their preparation and their use as medicaments. ...	08/09/2011
7994169	3,4-diaminopyridine derivatives for use as catalysts The present invention relates to 3,4-diaminopyridine derivatives of formula (I) wherein R1 and R2 are, independently of each other, electron donors, wherein R2...	08/09/2011
7994170	1,3-dihydro-imidazo[4,5-C]quinolin-2-ones as lipid kinase inhibitors The invention relates to novel organic compounds of formula (I) processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof—alone or in combin...	08/09/2011
7989453	Indole derivatives and their use as medicament The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumors. ...	08/02/2011
7981893	Heteroaryl compounds, compositions thereof, and methods of treatment therewith Provided herein are Heteroaryl Compounds having the following structure: wherein R1, R2, L, X, Y, Z, Q, A and B are as defined herein, compositions comprising an effective amou...	07/19/2011
7977335	Methods of preventing and reducing the severity of stress-associated conditions The present invention provides a method of preventing or reducing the severity of a stress-associated condition in a subject by systemically administering to the subject an effective amount of brimonidine or a pharmaceutically acceptable salt, ester, amide, stereois...	07/12/2011
7964600	Indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, and preparation and uses thereof The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of ...	06/21/2011

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Class 514/249 - 1,4-diazine as one of the cyclos