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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 > Five-membered Hetero Ring Containing At Least One Nitrogen Ring Atom (e.g., 1,2,3-triazoles, Etc.) > Tetrazoles (including Hydrogenated) > Pyrazoles PyrazolesPyrazoles 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.01/25/07 - 20070021486 - Derivatives of n-' (1,5-diphenyl-1h-pyrazol-3-yl) sulfonamide with cb1 receptor affinity Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 are as defined herein. The invention also relates to the preparation method thereof and to the use of same in therapeutics. ... 01/25/07 - 20070021485 - Aryl (or heteroaryl) azolylcarbinols effective to treat the subject, wherein the compound is administered in a suitable form. ... 01/18/07 - 20070015812 - Factor xa inhibitors wherein A, X1 to X3, Y1 to Y3, Z, R1, R2, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit coagulation factor Xa and can be used as medicaments. ... 01/18/07 - 20070015811 - 5(s)-substituted pyrazoline compounds, their preparation and use as medicaments The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals. ... 01/18/07 - 20070015810 - 5(r)-substituted pyrazoline compounds, their preparation and use as medicaments The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals. ... 01/18/07 - 20070015809 - Histone deacetylase inhibitors wherein the substituents are as defined herein. ... 01/18/07 - 20070015808 - Pharmaceutical formulations of endo-n-(9-methyl-9-azabicyclo[3,3. 1]non-3-yl)-1-methyl-1h-indazole-3-carboxamide hydrochloride A pharmaceutical formulation suitable for multi-dose administration comprising endo-N-(9-methyl-9-azabicyclo[3.3.1]non-3-yl)-1-methyl-1H-indazole-3-carboxanide hydrochloride, a preservative selected from the group consisting of alkyl paraben and phenol, and a buffer selected from the group consisting of acetate and phosphate buffers is disclosed. ... 12/21/06 - 20060287379 - Derivatives of 3-hydroxy-4-(cyclyl-alkylaminoalkyl)-5-phenyl-1h-pyrazole as antagonists of the gonadotropin releasing hormone (gnrh) for use in the treatment of sex hormone related conditions, such as prostatic of uterine cancer The invention relates to a group of novel pyrazole compounds of Formula (I): wherein: R1, R2, R3, M and R5 are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds ... 12/14/06 - 20060281803 - Pyrazole modulators of metabotropic glutamate receptors The present invention is directed to compounds which are allosteric modulators of metabotropic glutamate receptors, including the mGluR5 receptor, and which are useful in the treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to ... 12/07/06 - 20060276527 - Combination therapies for the treatment of cancer Lonidamine or a lonidamine analog is administered with one or more additional anti-cancer agents or surgery or radiation to treat cancer or is administered alone or in combination to treat cancer, optionally in a sustained release formulation, and improve patient outcome. ... 11/23/06 - 20060264493 - Tetracyclic pyrazole derivatives as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them The present invention provides a method for treating diseases caused by and/or associated with an altered protein kinase activity which comprises administering to a mammal in need thereof an effective amount of a tetracyclic pyrazole. The invention also provides specific tetracyclic pyrazole derivatives, useful intermediates, a library comprising at least ... 11/16/06 - 20060258729 - Antibacterial pyrazole carboxylic acid hydrazides Methods and compositions comprising pyrazole carboxylic acid hydrazide compounds are described that are useful for treating bacterial infections, inhibiting bacterial growth, and inhibiting the activity of bacterial DNA polymerase III. ... 11/02/06 - 20060247293 - Agent 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 transient retinal ischemia eye. Therefore, the medicament of the present invention has a ... 11/02/06 - 20060247292 - Benzocycloheptene derivatives, process for their production and their use as anti-inflammatory agents process for their production, and their use as anti-inflammatory agents. ... 10/26/06 - 20060241165 - Method and kit for regulation of microvascular tone Methods and kits for regulating arterial microvascular tone in which a COX-2 inhibitor and a cannabinoid receptor agonist are co-administered to a subject. ... 10/19/06 - 20060235066 - Aqueous suspension preparation of bactericide for folieage application The present invention provides an aqueous suspension formulation containing (RS)—N-[2-(1,3-dimethylbutyl)thiophene-3-yl]-1-methyl-3-trifluoromethyl-1H-pyrazole-4-carboxamide and having high rain resistance and stable residual effectiveness. A aqueous suspension formulation for foliar application fungicide of the present invention contains a fungicidal active ingredient, (RS)—N-[2-(1,3-dimethylbutyl)thiophene-3-yl]-1-methyl-3-trifluoromethyl-1H-pyrazole-4-carboxamide, and a polyoxyalkylene rosin acid ester or liquid paraffin, and has improved rain ... 09/28/06 - 20060217431 - Composition comprising a combined thromboxane receptor antagonist and thromboxane synthase inhibitor and a cox-2 inhibitor The invention relates to a pharmaceutical composition comprising a combined thromboxane receptor antagonist and thromboxane synthase inhibitor and a COX-2 inhibitor. In addition a method of treating cyclooxygenase dependent disorders, including inflammation, pain and/or rheumatic diseases, and/or neoplasia is described. ... 09/21/06 - 20060211756 - Novel heterocycle derivatives useful as selective androgen receptor modulators (sarms) The present invention is directed to novel heterocycle derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. ... 08/31/06 - 20060194861 - Cyclooxygenase-2 selective inhibitors, compositions and methods of use The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a ... 08/31/06 - 20060194860 - Pharmaceutical compositions containing aryl or heteroaryl azolylcarbinol compounds wherein R1, R2, R3 and R4 have the meanings given in the description. Related methods of treating or inhibiting pain and other conditions or disorders are also provided. ... 08/17/06 - 20060183785 - Biaryl substituted pyrazoles as sodium channel blockers Biaryl substituted pyrazole compounds are sodium channel blockers useful for the treatment of pain and other conditions. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treatment of conditions, including ... 08/03/06 - 20060173062 - Use of selective cyclooxygenase-2 inhibitors for the treatment of endometriosis The instant invention is directed to the use of cyclooxygenase-2 selective inhibitors to treat or prevent endometriosis; the use of cyclooxygenase-2 selective inhibitors to prevent, retard and/or reverse the development of endometriotic lesions in patients at risk for the development of such lesions; the use of cyclooxygenase-2 selective inhibitors to ... 07/27/06 - 20060167075 - Modulators of faah Methods for inhibiting the activity of FAAH and methods for preventing and/or treating certain disorders, e.g., anxiety disorders, sleep disorders and weight disorders, by administering celecoxib, valdecoxib or certain structurally related compounds at a dosage that is sufficient to treat and/or prevent the disorder are described. ... 07/27/06 - 20060167074 - Methods and compositions for the treatment of psychiatric disorders A method for the prevention, treatment, or inhibition of a psychiatric disorder, in particular schizophrenia, is described which comprises administering a COX-2 inhibitor or prodrug thereof to a subject. Moreover, a method for the prevention, treatment, or inhibition of a psychiatric disorder, in particular schizophrenia or depressive disorders, is disclosed ... 07/20/06 - 20060160874 - Heterobicyclic pyrazole derivatives as kinase inhibitors Bicyclo-pyrazoles of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer. ... 07/06/06 - 20060148877 - Pharmaceutical formulations of celcoxib Liquid formulations of celecoxib have been found to provide faster pain relief than conventional solid formulations of celecoxib. The present invention provides combinations of excipients in which celecoxib is highly soluble for formulation as pharmaceutical compositions. ... 07/06/06 - 20060148876 - Nr3b1 nuclear receptor binding 3-substituted pyrazoles The present invention relates to compounds according to the general formula (I) which bind to the NR3B1 receptor and act as antagonists or agonists of the NR3B1 receptor. The invention further relates to the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and the ... 06/29/06 - 20060142368 - Compounds and methods for inducing apoptosis in proliferating cells Compounds useful for inducing apoptosis in proliferative cells, particularly cancer cells, including but not limited to prostate cancer, leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, bladder cancer, lymphoma, and breast cancer. These compounds are particularly useful in the treatment of androgen-independent cancers, including ... 06/29/06 - 20060142367 - Pyrazole compound has an excellent controlling activity against noxious arthropods. ... 06/22/06 - 20060135589 - 1h-indazole-3-carboxamide compounds as cyclin dependent kinase (cdk) inhibitors or NR7R8 or NR7R9 may each form a heterocyclic group having from 5 to 12 ring members; but excluding the compounds N-[(morpholin-4-yl)phenyl-1H-indazole-3-carboxamide and N-[4-(acetylaminosulphonyl)phenyl-1H-indazole-3-carboxamide. ... 06/08/06 - 20060122251 - Use of dioxindoindazoles and dioxoloindazoles for treating glaucoma Novel dioxinoindazole compounds and dioxoloindazole compounds are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions of one or more of the compounds of the present invention. ... 06/08/06 - 20060122250 - Novel processes for the preparation of cgrp-receptor antagonists and intermediates thereof The invention relates to novel processes for the preparation of small molecule antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”) and intermediates thereof. ... 06/08/06 - 20060122249 - Condensed heterocyclic pyrazole derivatives as kinase inhibitors Bicyclo-pyrazole compound of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, processes for their preparation, combinatorial libraries comprising a plurality of them and pharmaceutical compositions thereof, are herewith disclosed: the compounds of the invention are useful, in therapy, as protein kinase inhibitors, for instance in the ... 06/01/06 - 20060116414 - Disubstituted pyrazolyl carboxanilides R, R1, R2 and R3 are as defined in the description, a plurality of processes for preparing these substances and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation. ... 05/25/06 - 20060111422 - Novel pyrazole-based hmg coa reductase inhibitors Novel compounds and pharmaceutical compositions useful as hypocholesterolemic and hypolipidemic agents are described. More specifically, potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (“HMG CoA reductase”) are described. Methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, Alzheimer's Disease, benign prostatic ... 05/25/06 - 20060111421 - Method of treating or preventing myocardial ischemia-reperfusion injury using nf-kb inhibitors The present invention concerns a method of treatment or prevention of myocardial ischemia-reperfusion injury by diagnosing that a person is in need of treatment or prevention of myocardial ischemia-reperfusion injury and administering a therapeutically effective amount of a ligand which modulates NF-kB transcription factor by interaction with estrogen receptor ER-α, ... 05/25/06 - 20060111420 - Sorbicillactone-a derivatives for the treatment of tumour and viral diseases are described, as well as methods for their production. Sorbicillacton A and sorbicillacton-A-derivatives, in cellular culture models, exhibit antitumour- and antiviral properties. Furthermore, sorbicillacton A has inflammation inhibiting properties. Finally, the synthesis of sorbicillacton A and its derivatives is described. ... 05/25/06 - 20060111419 - Novel fused indazole compounds represents a double bond or a single bond; R1a represents a hydrogen atom, etc.; the ring A represents a benzene ring, a naphthalene ring or a 5- to 10-membered aromatic heterocyclic ring, etc.; and R2a, R2b and R2c each independently represent (1) a hydrogen atom, (2) a halogen atom, (3) ... 05/18/06 - 20060106084 - [(1h-indazol-3-yl)methyl]phenols and (hydroxyphenyl)(1h-indazol-3-yl)methanones wherein A and R1-R10 are as defined in the specification, or a N-oxide thereof or a pharmaceutically acceptable salt thereof or a prodrug thereof. ... 05/18/06 - 20060106083 - Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them Compounds which are indazole derivatives and pharmaceutically acceptable salts thereof, together with pharmaceutical compositions comprising them, as well as combinatorial libraries of indazole derivatives, as set forth in the specification, are disclosed; these compounds or compositions may be useful in the treatment of diseases caused by and/or associated with an ... 05/18/06 - 20060106082 - Nitrooxyderivatives of cyclooxygenase-2 inhibitors for the treatment and/or prophylaxis of inflammatory processes. ... 05/11/06 - 20060100260 - Substituted pyrazoline carboxanilides for use as pesticides in which R1, R2, R3 and R4 are as defined in the disclosure, to a plurality of processes for preparing these compounds and to their use for controlling pests. ... 04/27/06 - 20060089399 - Pyrazolyl carboxanilides for controlling unwanted microorganisms in which R1, G and n are as defined in the disclosure, to a plurality of processes for preparing these substances, to their use for controlling unwanted microorganisms, and to novel intermediates and their preparation. ... 04/13/06 - 20060079566 - Pdk-1/akt signaling inhibitors wherein X is selected from the group consisting of alkyl and haloalkyl; Ar is an aryl radical selected from the group consisting of phenyl, biphenyl, naphthyl, anthryl, phenanthryl, and fluorenyl; and wherein Ar is optionally substituted with one or more radicals selected from the group consisting of halo, C1-C4 alkyl, ... 04/06/06 - 20060074122 - Novel aminoindazole derivatives as medicaments and pharmaceutical compositions including them R5, R6 and R7 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, OR8, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1-6C)alkyl, (1-6C)alkoxy, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl, ... 04/06/06 - 20060074121 - Bicyclic and bridged nitrogen heterocycles Compounds are provided that act as potent modulators of one or more of the CCR1, CCR2 and CCR3 receptors. The compounds are generally fused-, spiro- or bridged-nitrogen heterocycles having an aryl and heteroaryl component and are useful in pharmaceutical compositions, methods for the treatment of CCR1-, CCR2- and/or CCR3-mediated diseases, ... 04/06/06 - 20060074120 - Selective non-steroidal glucocorticoid receptor modulators The present invention encompasses compounds of Formula (I) or pharmaceutically acceptable salts or hydrates thereof, which are useful as novel non-steroidal selective glucocorticoid receptor modulators for treating a variety of autoimmune and inflammatory diseases or conditions, and possess advantages over steroidal glucocorticoid ligands with respect to undesireable side-effects, efficacy, toxicity ... 03/30/06 - 20060069147 - Sulfonamides, sulfamates and sulfamides as gamma-secretase inhibitors inhibit the processing of APP by gamma-secretase, and hence are useful in treating or preventing Alzheimer's disease. ... 03/16/06 - 20060058366 - Jnk inhibitor [wherein R1 represents substituted or unsubstituted aryl or the like and R2 represents a hydrogen atom, NR3R4 (wherein R3 and R4 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkanoyl or the like), carboxy, lower alkenyl or the like] or a pharmaceutically ... 03/09/06 - 20060052432 - Pharmaceutical compositions with improved dissolution The invention relates to methods of screening mixtures containing a pharmaceutical compound and an excipient to identify properties of the pharmaceutical compound/excipient combination that retard solid-state nucleation. The invention further relates to increasing the solubility, dissolution and bioavailability of a drug with low solubility in gastric fluids conditions by combining ... 02/23/06 - 20060041002 - Guanylhydrazone compounds, compositions, methods of making and using salts thereof; compositions comprising one or more of the compounds and/or salts thereof; methods of using; and methods of making. ... 02/09/06 - 20060030613 - Indole, indazole and indoline derivatives as cetp inhibitors wherein —X—Y—, R1 to R11 and n are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are mediated by CETP inhibitors. ... 02/09/06 - 20060030612 - Indazoles useful in treating cardiovascular diseases that are useful in the treatment or inhibition of LXR mediated diseases. ... 02/02/06 - 20060025467 - 3-amino-1-arylpropyl indoles as monoamine reuptake inhibitors wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds. ... 02/02/06 - 20060025466 - Indazole-aminoacetonitrile derivatives having special pesticidal activity wherein Ar1, Ar2, R4, R5, R6, R7, R8, W, X, a and b have the significances given in the specification, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals. ... 01/26/06 - 20060020011 - Arylpyrrolidine derivatives as nk-1 /ssri antagonists are useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors. ... 01/19/06 - 20060014817 - Cck-1 receptor modulators There are provided by the present invention certain pyrazole based CCK-1 receptor modulators. ... 01/19/06 - 20060014816 - Tricyclic pyrazole kinase inhibitors Compounds of the present invention are useful for inhibiting protein tyrosine kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds. ... 01/19/06 - 20060014815 - Process for making pyrazole compounds This invention relates to a process for making pyrazole compounds of formula I. ... 01/05/06 - 20060004076 - Co-administration of dehydroepiandrosterone (dhea) congener with pharmaceutically active agents for treating inflammation The present invention is related to therapeutic uses of dehydroepiandrosterone (DHEA) congeners. More specifically, the present invention relates to the co-administration of a dehydroepiandrosterone (DHEA) congener in combination with at least one other pharmaceutically active agent to reduce inflammation. ... 12/22/05 - 20050282880 - Novel 1h-indazole compounds Wherein R1 is a C6-C14 aromatic cyclic hydrocarbon group etc.; R2, R4 and R5 each independently represent a hydrogen atom, a halogen atom, a cyano group etc.; L is a single bond, or a C1-C6 alkylene group etc.; X is a single bond, or a group represented by —CO—NH— or ... 12/15/05 - 20050277687 - Combination of selected analgesics and cox-ii inhibitors Combinations of certain analgesics with certain COX-II inhibitors, related pharmaceutical compositions, including advantageous galenical forms containing these combinations, and to the use thereof in methods of treatment, in particular for the treatment of pain. ... 12/08/05 - 20050272796 - Prevention and treatment of benign prostatic hyperplasia using lonidamine and lonidamine analogs A method for treatment or prophylaxis of benign prostatic hyperplasia by administration of lonidamine or a lonidamine analog is provided. Also provided are unit dosage forms of lonidamine or an analog, useful for such treatment and prophylaxis. ... 12/08/05 - 20050272795 - Prevention and treatment of benign prostatic hyperplasia A method for treatment or prophylaxis of benign prostatic hyperplasia by administration of lonidamine or a lonidamine analog is provided. Also provided are unit dosage forms of lonidamine or an analog, useful for such treatment and prophylaxis. ... 12/08/05 - 20050272794 - Pyrazole derivatives, compositions containing such compounds and methods of use Pyrazoles having a naphthyl group attached are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included. ... 12/08/05 - 20050272793 - Pyrazole compounds and uses related thereto Substituted pyrazoles are provided that are useful for the treatment of, for example, diabetes, obesity and metabolic syndrome. ... 12/01/05 - 20050267190 - Solid-state form of celecoxib having enhanced bioavailability The selective cyclooxygenase-2 inhibitory drug celecoxib is provided in amorphous form. Also provided is a celecoxib drug substance wherein the celecoxib is present, in at least a detectable amount, as amorphous celecoxib. Also provided is a celecoxib-crystallization inhibitor composite comprising particles of amorphous celecoxib or a celecoxib drug substance of ... 12/01/05 - 20050267189 - Celecoxib compositions Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising particulate celecoxib in an amount of about 10 mg to about 1000 mg in intimate mixture with one or more pharmaceutically acceptable excipients. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and ... 11/24/05 - 20050261353 - Acylsemicarbazides as cyclin dependent kinase inhibitors useful as anti-cancer and anti-proliferative agents that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of ... 11/17/05 - 20050256180 - Substituted pyrazolyl compounds for the treatment of inflammation The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis. ... 11/03/05 - 20050245589 - Pyrazole phenyl derivatives and X1, X2, R1 to R15 and n are as defined in the description, and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are ... 11/03/05 - 20050245588 - Octahydro-2-h-naphtho[1,2-f]indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included. ... 10/27/05 - 20050239860 - Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade The present invention relates to compounds, and prodrugs thereof, compositions and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade. ... 10/27/05 - 20050239859 - Novel medical uses of 4,5-dihydro-1h-pyrazole derivatives having cb1- antagonistic activity wherein the group Bb represents sulfonyl or carbonyl, and the substituents R, R1, R2 and R3, and the group Aa are defined as shown in the description. ... 10/27/05 - 20050239858 - Pyrazole derivatives as gnrh inhibitors The invention relates to a group of novel thieno-pyrrole compounds of Formula (I); wherein: R1, R2, R5, R6, R6a, R7, R8, A, B and M are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods ... 10/20/05 - 20050234119 - Antiparasitical agents and methods for treating, preventing and controlling external parasites in animals This invention provides for antiparasitical agents and methods for treating, preventing and controlling external parasites in animals. ... 10/13/05 - 20050228034 - Tetrahydro-indazole cannabinoid modulators and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease. ... 10/06/05 - 20050222240 - Crystalline pyrazoles The present invention relates to crystal forms of 4-[5-(4-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]-benzenesulfonamide and methods for preparation, interconversion, and isolation of such crystals. ... 10/06/05 - 20050222239 - Pyrazole-amine compounds for the treatment of neurodegenerative disorders wherein R1, R3, R4, R5, R6, R7 and R8 are as defined. Compounds of the Formula I have activity inhibiting production of Aβ-peptide. The invention also relates to pharmaceutical compositions and methods of treating disorders and diseases, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising ... 10/06/05 - 20050222238 - Deuterated substituted pyrazolylbenzylsulfonamides and medicaments comprising said compounds The invention concerns deuterated substituted pyrazolyl benzylsulfonamides as well as pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated substituted pyrazolyl benzylsulfonamides for the treatment of symptoms of osteoarthritis and rheumatoid arthritis as well as for the prevention and treatment of neoplasia, in particular adenomatous colorectal ... 09/29/05 - 20050215613 - Preferential inhibition of release of pro-inflammatory cytokines in which R is H, alkyl, aryl, cyclyl, heteroaryl, or heterocyclyl; each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, or pyrrolyl; each of R1, R2, R3, R4, R5, and R6, independently, is R′, nitro, halogen, —C(O)—OR′, —C(O)—SR′, —C(O)—NR′R″, —(CH2)mOR′, —(CH2)mSR′, —(CH2)mNR′R″, —(CH2)mCN, —(CH2)mC(O)—OR′, —(CH2)mC(O)H, or R1 and ... 09/29/05 - 20050215612 - Novel fused pyrazolyl compound wherein A, Ar1, Ar2, R1, R2, R3, and R4, are as defined herein. Also disclosed is a pharmaceutical composition containing an effective amount of the above-described fused pyrazolyl compound. ... 09/29/05 - 20050215611 - Combination therapy for treating cyclooxygenase-2 mediated diseases in patients at risk of thrombotic cardiovascular events The present invention encompasses a method for treating a chronic cyclooxygenase-2 mediated disease or condition and reducing the risk of a thrombotic cardiovascular event in a human patient in need of such treatment and at risk of a thrombotic cardiovascular event comprising orally concomitantly or sequentially administering to said patient ... 09/22/05 - 20050209297 - Pyrazole derivatives wherein R1, R2, R3, and R4 are as defined, and their pharmaceutically acceptable salts. Compounds of formula 1 are indicated to have activity inhibiting cdk5, cdk2, and GSK-3. Pharmaceutical compositions and methods comprising compounds of formula 1 for treating and preventing diseases and conditions comprising abnormal cell growth, such as ... 09/22/05 - 20050209296 - 1,2-diaza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof The present invention relates to derivatives of 1,2-diaza-dibenzoazulene, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory actions, especially to the inhibition of tumour necrosis factor-α (TNF-α) production and the inhibition of interleukin-1 (IL-1) production as well as ... 09/15/05 - 20050203160 - Indolyl derivatives and R1 to R15 and n are as defined in the description, and all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which ... 09/01/05 - 20050192332 - Pyrazolecarboxylic acid tricyclic derivatives, preparation and pharmaceutical compositions containing same in which R1 represents a C3-C15 carboxyl radical or an NR2R3 group. The invention also relates to the method for preparing the compounds of formula (I), pharmaceutical compositions containing them. The compounds of formula (I) are active on cannabinoid CB1 receptors. ... 09/01/05 - 20050192331 - Small molecule modulators of hepatocyte growth factor (scatter factor) activity and pharmaceutically acceptable derivatives thereof, wherein R1, R2 and B are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases in which HGF/SF or the activities ... 08/25/05 - 20050187279 - Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water/electrolyte homeostasis, sensory processing, memory, ... 08/25/05 - 20050187278 - Treatment or prevention of vascular disorders with cox-2 inhibitors in combination with cyclic amp-specific phosphodiesterase inhibitors A method is described for the prevention and/or treatment of vascular disorders and vascular disorder-related complications in a subject, the method comprising administering to the subject a Cox-2 inhibitor in combination with a cAMP-specific PDE inhibitor. Also described are therapeutic and pharmaceutical compositions and kits that are useful in the ... 08/18/05 - 20050182121 - Thio semicarbazone and semicarbozone inhibitors of cysteine proteases and methods of their use The present invention relates to thio semicarbazone and semicarbazone inhibitors of cysteine proteases and methods of using such compounds to prevent and treat protozoan infections such as trypanosomiasis, malaria and leishmaniasis. The compounds also find use in inhibiting cysteine proteases associated with carcinogenesis, including cathepsins B and L. ... 08/18/05 - 20050182120 - Pyrazolyl biphenyl carboxamides and the use thereof for controlling undesirable microorganisms a plurality of processes for preparing these substances and their use for controlling undesirable microorganisms, and also novel intermediates and their preparation. ... 08/18/05 - 20050182119 - Substituted pyrazoline derivatives The present invention relates to new substituted pyrazoline compounds, pharmaceutical compositions containing such compounds and the use of these compounds for the treatment of cancer, in particular for the treatment of brain cancer, bone cancer, lip cancer, mouth cancer, esophageal cancer, stomach cancer, liver cancer, bladder cancer, pancreas cancer, ovary ... 08/11/05 - 20050176799 - Pyrazole derivatives, their preparation and their use in pharmaceuticals in which X, R1, R1a, R2, R3, R4 and n are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I ... 08/04/05 - 20050171180 - Heterocyclic sulfonamide inhibtors of beta amyloid production containing an azole wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; ... 08/04/05 - 20050171179 - 1,3,5-trisubstituted 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity wherein the symbols have the meanings given in the specification. ... 07/28/05 - 20050165081 - Use of anastrozole for the treatment of post-menopausal women having early breast cancer The invention provides the use of anastrozole, or a pharmaceutically acceptable salt thereof, in the preparation of a medicament for the reduction of the rate of recurrence of cancer in a woman having early breast cancer. The invention further provides the use of anastrozole, or a pharmaceutically acceptable salt thereof, ... 07/21/05 - 20050159471 - Compositions of a benzenesulfonamide or methylsulfonylbenzene cyclooxygenase-2 selective inhibitor and a cholinergic agent for the treatment of reduced blood flow or trauma to the central nervous system The present invention provides methods and compositions for the treatment of central nervous system damage in a subject. More particularly, the invention provides a combination therapy for the treatment of a central nervous system ischemic condition or a central nervous system traumatic injury comprising the administration to a subject of ... 07/07/05 - 20050148649 - Substituted arylpyrazoles This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which there is at least one fluorine attached to the cyclopropyl ring, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides. ... 07/07/05 - 20050148648 - Modulators of atp-binding cassette transporters The present invention also provides pharmaceutical compositions, methods and kits associated with Formula I, useful for as modulators, and for the treatments of disease and disease conditions associated with ABC transporter proteins. ... 06/30/05 - 20050143443 - Pyrrole and pyrazole daao inhibitors at least one of X and Y is (CR6R7)n. D-serine or cycloserine may be coadministered along with the compound of formula I. ... 06/30/05 - 20050143442 - Novel fused pyrrolocarbazoles The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles. ... 06/30/05 - 20050143441 - Novel medical combination treatment of obesity involving 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity wherein the group Bb represents sulfonyl or carbonyl, and the substituents R, R1, R2 and R3, and the group Aa are defined as shown in the description. Preferred lipase inhibitors are orlistat, panclicins, ATL-962 and/or lipstatin. ... 06/23/05 - 20050137245 - Novel fused pyrrolocarbazoles The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles. ... 06/23/05 - 20050137244 - Topical formulations comprising 1-n-arylpyrazole derivatives and amitraz The present invention provides for, inter alia, novel topical formulations comprising at least one 1-N-arypyrazole derivative and amitraz and to methods for treating, controlling, or preventing parasite infestations on mammals or birds The inventive formulations include spot-on, pour-on or spray formulations and may include a further ectoparasiticide, such as an ... 06/23/05 - 20050137243 - Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water/electrolyte homeostasis, sensory processing, memory, ... 06/16/05 - 20050131050 - Substituted pyrazolyl benzenesulfonamides for the treatment of inflamation wherein R2 is selected from hydrido, alkyl, haloalkyl, alkoxycaronyl, cyano, cyanoalkyl, carboxyl, aminocaronyl, alkylaminocarbonyl, cycloalklaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, amioncarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R3 is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R4 is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R4 ... 06/16/05 - 20050131049 - Derivatives of aryl (or heteroaryl) azolylcarbinoles for the treatment of urinary incontinence Derivatives of aryl(or heteroaryl)azolylcarbinoles of general formula (I), in which Ar represents a phenyl radical or a thienyl radical, optionally substituted, R1 represents a hydrogen atom or a lower alkyl group, R2 represents a dialkylaminoalkyl or azaheterocylclylalkyl and Het represents an azole unsubstituted or optionally substituted by one or two ... 06/16/05 - 20050131048 - Enhancement of bone growth and inhibition of bone resorption each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, or pyrrolyl; each of R1, R2, R3, R4, R5, and R6, independently, is H, halogen, R, C(O)OH, C(O)OR, C(O)SH, C(O)SR, C(O)NH2, C(O)NHR, C(O)NRR′, ROH, ROR′, RSH, RSR′, NHR, NRR′, RNHR′, or RNR′R″; or R1 and R2 together, R3 and ... 06/02/05 - 20050119324 - Methods of treating atherosclerosis using nf-kb inhibitors The present invention concerns a method of treating atherosclerosis by diagnosing that a person is in need of treatment for atherosclerosis and administering a therapeutically effective amount of a ligand which modulates NF-kB transcription factor by interaction with estrogen receptor ER-α, estrogen receptor ER-β, or both ER-α and ER-β estrogen ... ### FreshPatents.com Support |