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Drug, Bio-affecting And Body Treating Compositions > Designated Organic Active Ingredient Containing (doai) > Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai > Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbon Atoms > Additional Hetero Ring Containing > Ring Nitrogen In The Additional Hetero Ring (e.g., Oxazole, Etc.) > The Additional Hetero Ring Consists Of Two Nitrogens And Three Carbons The Additional Hetero Ring Consists Of Two Nitrogens And Three CarbonsThe Additional Hetero Ring Consists Of Two Nitrogens And Three Carbons patent applications listed are from June 2005 to current and include Date, Patent Application Number, Patent Title, Patent Abstract summary and are linked to the corresponding patent application page.02/01/07 - 20070027190 - Antibacterial fab i inhibitors Disclosed herein are antibacterial compounds that inhibit fabl, a NADH-dependent enoyl [acyl carrier protein] reductase enzyme in the fatty acid biosynthesis pathway. The compounds are represented by structural formulas Ia and Ib: R1 and R2 are independently monocyclic aryl or heteroaryl groups, wherein the groups represented by R1 and R2 ... 01/25/07 - 20070021468 - Preparation and use of 2-substituted-5-oxo-3-pyrazolidinecarboxylates A method is disclosed for preparing a 2-substituted-5-oxo-3-pyrazolidinecarboxylate compound of Formula I. The method comprises contacting a succinic acid derivative of the formula R1OC(O)C(H)(X)C(R2a)(R2b)C(O)Y (i.e. Formula II) wherein X and Y are leaving groups and L, R1, R2a and R2b are as defined in the disclosure, with a substituted hydrazine ... 01/11/07 - 20070010561 - Prenylation inhibitors and methods of their synthesis and use The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same. ... 12/28/06 - 20060293364 - Niacin receptor agonists, compositions containing such compounds and methods of treatment as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included. ... 12/21/06 - 20060287366 - Treating pain using selective antagonists of persistent sodium current The present invention provides methods of treating chronic pain in a mammal by administering to the mammal an effective amount of a selective persistent sodium channel antagonist that has at least 20-fold selectivity for persistent sodium current relative to transient sodium current. ... 12/21/06 - 20060287365 - Substituted arylpyrazoles This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides. ... 11/30/06 - 20060270712 - Mag expression promoters wherein each symbol is as defined in the specification, an optically active form thereof or a pharmaceutically acceptable salt thereof. As a compound of the formula (I), 4-[α-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid is exemplified. The MAG expression promoter of the present invention is useful as an agent for the prophylaxis and/or treatment of ... 11/23/06 - 20060264476 - Farnesyltransferase inhibitors are useful for inhibiting farnesyltransferase. Also disclosed are farnesyltransferase-inhibiting compositions and methods of inhibiting farnesyltransferase in a patient. ... 11/23/06 - 20060264475 - Compounds, compositions and methods for inhibiting or treating hiv-1 There is disclosed a structural genus of compounds, defined according to coordinates in three-dimensional space, that bind amino moieties on neighboring residues in a tyrosine residue 29 pocket of the matrix protein component of the HIV-1 preintegration complex (PIC), thereby preventing the PIC from binding to karyopherin α and preventing ... 11/23/06 - 20060264474 - Pyrazole derivatives as gamma-secretase inhibitors useful in the treatment of alzheimer's disease The compounds of formula (I): inhibit gamma-secretase and hence are of utility in the treatment or prevention of Alzheimer's disease. ... 11/16/06 - 20060258717 - Organic compounds wherein R1. is hydrogen, lower alkyl, halogen with an atomic number of 9 to 35 or amino optionally mono- or disubstituted by lower alkyl, R2. and R3. independently of one another are hydrogen or lower alkyl, R4. is hydrogen, hydroxy, lower alkyl, lower alkoxy or halogen with an atomic number ... 11/02/06 - 20060247280 - Compounds and methods Compounds of this invention are non-peptide, reversible inhibitors of type 2 methionine aminopeptidase, useful in treating conditions mediated by angiogenesis, such as cancer, haemangioma, proliferative retinopathy, rheumatoid arthritis, atherosclerotic neovascularization, psoriasis, ocular neovascularization and obesity. ... 10/26/06 - 20060241152 - Imidazoline derivatives having cb1-antagonistic activity wherein the symbols have the meanings given in the specification. ... 10/19/06 - 20060235054 - 2-thio-substituted imidazole derivatives and their use in pharmaceutics in which the radicals R1, R2 R3 and m are as defined in the description. The compounds according to the invention have immunomodulating and/or cytokine-release-inhibiting action and are therefore suitable for treating disorders associated with a disturbed immune system. ... 10/05/06 - 20060223864 - Thiadiazoles as cxc- and cc- chemokine receptor ligands and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, ... 09/21/06 - 20060211739 - Use of selective p2x7 receptor antagonists wherein D, R1 and R2 are as defined in claim 1, for the treatment of neuropathic pain, chronic inflammatory pain, inflammation, neurodegeneration and for promoting neuroregeneration, ... 09/21/06 - 20060211738 - Certain substituted diphenyl ureas, as modulators of kinase activity Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided ... 08/31/06 - 20060194846 - [1,2,4]-dithiazoli(di)ne derivatives, inducers of gluthathione-s-transferase and nadph quinone oxido-reductase, for prophylaxis and treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular wherein wherein the symbols have the meanings given in the specification. ... 08/31/06 - 20060194845 - Use of alk 5 inhibitors to modulate or inhibit myostatin activity leading to increased lean tissue accretion in animals to an animal for a time sufficient to cause the desired effect. ... 08/17/06 - 20060183780 - Pyrazole compounds useful in the treatment of inflammation There is provided a compound of formula (I), wherein R1, R2, R3, X and Y have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a lipoxygenase (e.g. 15-lipoxygenase) is desired and/or required, and ... 08/03/06 - 20060173048 - Imidazole derivatives wherein R1, R2, R3 and X are as defined in the specification, methods of preparation thereof and uses thereof, which compounds are useful for preventing and treating mGluR 2 receptor mediated disorders. ... 07/20/06 - 20060160864 - Acrylamide derivative, process for producing the same, and use or a salt thereof. The compound has excellent CCR5 antagonistic activity and thus is useful as a prophylactic and/or therapeutic medicine for HIV infection into human peripheral blood monocyte, especially for AIDS. ... 07/13/06 - 20060154968 - Treating neurological disorders using selective antagonists of persistent sodium current The present invention provides methods of treating neurological disorders in a mammal by administering to the mammal an effective amount of a selective persistent sodium channel antagonist that has at least 20-fold selectivity for persistent sodium current relative to transient sodium current. ... 07/13/06 - 20060154967 - Chemical compounds A compound of formula (I):, where A is an ortho-substituted ring selected from a number of specified rings; R1 is halogen, cyano, nitro, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy or C1-4 haloalkoxy or optionally substituted C2-4 alkenyl, optionally substituted C2-4 alkynyl or optionally substituted SO2(C1-4 alkyl) (where the optionally substituted ... 07/06/06 - 20060148859 - Substituted pyridyloxyalkylamides and their use as fungicides Fungicidal compounds of the general formula (1), or the corresponding pyridine N-oxide, wherein X, Y, R1, R2, R3, R4 and R5 are as defined in the description. ... 07/06/06 - 20060148858 - 1, 2-azole derivatives with hypoglycemic and hypolipidemic activity A compound represented by the formula (1) wherein ring A is a ring optionally having 1 to 3 substituents; ring B is a 1,2-azole ring which may further have 1 to 3 substituents; Xa, Xb and Xc are the same or different and each is a bond, —O—, —S— and ... 06/15/06 - 20060128761 - Novel triazole compounds as transforming growth factor (tgf) inhibitors Novel triazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-β signaling pathway. They are useful in the treatment of various TGF-related disease states ... 06/15/06 - 20060128760 - Use of mglur5 antagonists for the treatment of gerd The present invention relates to the use of metabotropic glutamate receptor 5 antagonists for the inhibition of transient lower esophageal sphincter relaxations. A further aspects of the invention is directed to the use of metabotropic glutamate receptor 5 antagonists for the treatment of gastro, esophageal reflux disease, as well as ... 05/25/06 - 20060111403 - Cyano anthranilamide insecticides This invention provides compounds of Formula (I), N-oxides and suitable salts thereof INSERT FORMULA I HERE wherein R1 is Me, Cl, Br or F; R2 is F, Cl, Br, C1-C4 haloalkyl or C1-C4 haloalkoxy; R3 is F, Cl or Br; R4 is H or C1-C4 alkyl, C3-C4 alkenyl, C3-C4 alkynyl, ... 05/11/06 - 20060100248 - Blockade of voltage dependent sodium channels Compounds of Formula I and pharmaceutically acceptable salts thereof, are capable of blockading voltage-dependent sodium channels and are useful in particular, in treating glaucoma and multiple sclerosis. ... 04/06/06 - 20060074109 - Use of inhibitors of 24-hydroxylase in the treatment of cancer The present invention relates to a method of treating cancer in a subject. The method comprises administering to a subject suffering from cancer a therapeutically effective amount of a 24-hydroxylase inhibitor. In certain embodiments, the 24-hydroxylase inhibitor can be coadministered with calcitriol. ... 03/30/06 - 20060069130 - Novel crystals Obtaining the crystal of 4,6-dimethyl-4′-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]nicotinanilide having excellent activity of inhibiting Ca2+ release-activated Ca2+ channel and suppressing IL-2 production to find that the compound includes the presence of two types of polymorphic crystals and that any of the crystals is preferable as a raw material for producing pharmaceutical compositions. ... 03/09/06 - 20060052421 - Conjugation agent are described, wherein Sx is —S—, —SO— or —SO2—; Rs is a carbon-containing substituent that does not include a cyano group; each R is a substituent, with at least one R having a reaction site that is not a carboxylic acid; n is 0-5; each A is carbon or nitrogen, ... 02/23/06 - 20060040994 - Substituted amide beta secretase inhibitors R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering ... 02/02/06 - 20060025454 - Prenylation inhibitors and methods of their synthesis and use The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same. ... 01/26/06 - 20060019997 - Triazole compounds and their use as metabotropic glutamate receptor antagonists wherein P, Q, X1, X2, X3, X4 X7, X8, R1, R2, R3, m, n, and p are as defined as in formula I, or salts, or hydrates thereof, processes for their preparation and new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of ... 01/19/06 - 20060014802 - Substituted arylpyrazoles wherein X, R1, R2, R3, R4, R5, R6, R7 and R9 are as described herein, and one or more further biologically active compounds as desribed herein, particularly anti-parasitic agents. ... 01/19/06 - 20060014801 - Prevention and treatment of cognitive impairment using (r)-(-)-5-methyl-1-nicotynoyl-2-pyrazoline (mnp) and analogs The invention provides methods for improving cognitive function in a subject by administering (R)-(−)-5-methyl-1-nicotinoyl-2-pyrazoline (MNP) or an analog to a subject in need of such treatment. The invention is useful for treatment of cognitive impairment such as mild cognitive impairment (MCI) as well as other conditions. ... 01/12/06 - 20060009495 - Diary 1,2,4-triazole derivatives as a highly selective cyclooxygenase-2 inhibitor Wherein, R1, R2, R3, R4, R5, W and A is as defined in this specification. ... 01/05/06 - 20060004060 - Control of arthropods in rodents The present invention provides a method for controlling ectoparasites of small rodents, thereby preventing the transmission of diseases by arthropod vectors. ... 12/22/05 - 20050282868 - Substituted anthranilamides for controlling invertebrate pests This invention provides compounds of Formula (I), and N-oxides and salts thereof (I) wherein A, B, R1 through R5, R7 through R9, X and Y are as defined in the disclosure. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a ... 12/08/05 - 20050272779 - Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists to pharmaceutical formulations containing the compounds, and to the use of the compounds in the prevention and/or treatment of mGluR5 receptor-mediated disorders. ... 12/01/05 - 20050267164 - Imidazolidinone compounds in which R1, R2, Al, A2, X, Y, m, n, p, x and y are as defined herein. Also disclosed are pharmaceutical compositions each containing one or more of these compounds, and use thereof in treating enteroviral infection. ... 11/17/05 - 20050256170 - Ep2 receptor agonists R2 is either: —CO2H (carboxy); —CONH2; —CH2-OH; or tetrazol-5-yl. ... 11/17/05 - 20050256169 - Nitric oxide scavengers Therapeutic compositions capable of removing excess nitric oxide are provided. The therapeutic compositions include nitronyl nitroxide monoradicals, B12 derivatives, flavonoid derivatives, the like and combinations thereof. The therapeutic compositions can be utilized in a number of suitable applications, such as to prevent or treat intradialytic hypotension during dialysis. ... 11/03/05 - 20050245580 - Novel substituted dihydro 3-halo-1h-pyrazole-t-carboxylates, their preparation and use wherein X is N and R2, R3 and n are as defined in the disclosure. ... 10/20/05 - 20050234106 - Cycloalkyl inhibitors of potassium channel function Novel cycloalkyl compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and ... 10/06/05 - 20050222213 - Alpha(trifluoromethyl-substituted aryloxy, arylamino, arylthio or arylmethyl)-trifluoromethyl-substituted phenylacetic acids and derivatives as antidiabetic agents or a pharmaceutically acceptable salt or prodrug thereof, are provided, and are useful for the treatment of metabolic disorders. ... 10/06/05 - 20050222212 - Compounds and methods Compounds of this invention are non-peptide, reversible inhibitors of bacterial methionine aminopeptidases, useful in treating bacterial infections. ... 09/29/05 - 20050215598 - Phenylalanine derivatives Ar is an optionally substituted aromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders. ... 09/29/05 - 20050215597 - Composition for controlling house insect pest and method for controlling house insect pest The present invention provides a composition for controlling a house insect pest, such as termites, ants or cockroaches, which comprises, as active ingredients, at least two compounds selected from the group consisting of (a) a certain pyridine compound, (b) a benzoylurea compound, (c) a pyrethroid compound and (d) a certain ... 09/22/05 - 20050209287 - Triazole derivatives and method of using the same to treat hiv infections wherein R1, R2 and R3 are independently selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, aryl and heteroaryl and X1 and X2 are independently a bond or an linker group of 1 to 6 atoms and may be optional substituted or oxidized, or a prodrug, a pharmaceutically acceptable ... 09/22/05 - 20050209286 - Rxr activating molecules Disclosed are molecules that activate an RXR receptor, wherein the molecule comprises an RXR binding portion which binds the RXR receptor and comprises a side pocket contacting residue which contacts a side-pocket 1 of an RXR receptor. ... 09/22/05 - 20050209285 - Compounds and compositions as protein kinase inhibitors The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, PDGF-R, lck, SAPK2α, p38, TGFβ, ... 09/01/05 - 20050192319 - Spot-on formulations for combating parasites In particular this invention provides for spot-on compositions for the treatment or prophylaxis of parasite infestations in mammals or birds which comprise: (1) a composition comprising (A) an effective amount of a 1-phenylpyrazole derivative; and (B) an effective amount of emamectin, latidectin or lepimectin; (2) an acceptable liquid carrier vehicle; ... 08/25/05 - 20050187260 - 2-pyrrolidin-2-yl-[1,3,4]-oxadiazole compounds and their use as anti-depressants a method for their production, pharmaceutical compositions containing them, and methods of using them, especially for treating pain and/or depression. ... 08/25/05 - 20050187259 - Imidazoline derivatives having cb1-antagonistic activity wherein the symbols have the meanings given in the specification. ... 08/04/05 - 20050171164 - 5-substituted-alkylaminopyrazole derivatives as pesticides The invention relates to the use for the control of pests, of a compound which is a 5-substituted-alkylaminopyrazole derivative of formula (I) or a salt thereof: wherein the various symbols are as defined in the description, to novel 5-substituted-alkylaminopyrazole derivatives and pesticidal compositions thereof, and to processes for their preparation. ... 07/28/05 - 20050165063 - Amine compounds and use thereof z represents an optionally substituted monocyclic or polycyclic aromatic ring. In the formula (6), B represents NR25R26. In the above formulae, R1 to R26 each represents hydrogen, alkyl, alkenyl or alkynyl. ... 07/14/05 - 20050154029 - Human g protein-coupled receptors and modulators thereof for the treatment of metabolic-related disorders The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the ... 07/14/05 - 20050154028 - Cyclic urea derivatives with 5-ht2c receptor activity Compounds of formula (I) or a pharmaceutically acceptable salt thereof, having 5HT2C receptor activity, are disclosed: wherein a is 0,1,2,3,4 or 5; b is 1,2 or 3; Y is nitrogen or carbon; A is oxygen, nitrogen, —CONH—, —NHCO— or together with R2 form a benzoxazolone group; R1 is halogen, C1-6alkyl, ... 06/16/05 - 20050131028 - Methods and compositions for the extended duration treatment of pain, inflammation and inflammation-related disorders A method is disclosed for providing extended duration treatment or prevention of pain, inflammation and inflammation-related disorders in a subject in need of such extended duration treatment or prevention by administering to the subject a Cox-2 selective inhibitor having certain added substituent groups. Also disclosed is a method for extending ... 06/09/05 - 20050124664 - Urea thiadiazole inhibitors of plasminogen activator inhibior-1 or a pharmaceutically-acceptable salt, prodrug, stereoisomer or solvate thereof, wherein: A is aryl o heteroaryl, and R1-R12, are defined herein. The invention also pertains to pharmaceutical compositions and compounds within the scope of formula (I) as well as medicaments and articles of manufacture comprising compounds of formula (I). ... ### FreshPatents.com Support |