51st week of 2008 patent applcation highlights part 47 |
Patent application number | Title | Published |
20080312159 | Dendrimeric peptides, pharmaceutical compositions and methods of using the same - Novel dendrimeric peptide compounds are disclosed that have a formula represented by the following formula I: | 2008-12-18 |
20080312160 | METHOD OF TREATING ENTERITIS, INTESTINAL DAMAGE, AND DIARRHEA FROM C. DIFFICILE WITH AN A2A ADENOSINE RECEPTOR AGONIST - A therapeutic method for treating intestinal damage, enteritis, diarrhea, or a combination thereof caused by a | 2008-12-18 |
20080312161 | Compounds For Stabilizing Factor VII Polypeptide Formulations -
The invention relates to novel compounds with formula I and their use in stabilization of Factor Vila or other Factor VII polypeptides, particularly in aqueous liquid compositions thereof. | 2008-12-18 |
20080312162 | Methods and Compositions for Enzyme-Specific Activation of Carbohydrate-Conjugated Prodrugs - Methods for the targeted activation of prodrugs by enzymes, which cleave a linkage between a carbohydrate conjugate and a drug. Means to target the activation of prodrugs to specific cells by linking the enzyme to an antibody molecule. Carbohydrate conjugates of geldanamycin. | 2008-12-18 |
20080312163 | Treatment of pulmonary hypertension with carbonic anhydrase inhibitors - This disclosure relates generally to methods and pharmaceutical compositions useful in treating pulmonary hypertension. In one embodiment, for example, the disclosure provides a method for treating pulmonary hypertension comprising administering a therapeutically effective dose of a carbonic anhydrase inhibitor to a patient in need of treatment. The disclosure finds utility in the fields of medicine and pharmacology. | 2008-12-18 |
20080312164 | ISOTHIOCYANATES AND GLUCOSINOLATE COMPOUNDS AND ANTI-TUMOR COMPOSITIONS CONTAINING SAME - The present invention provides glucosinolate and isothiocyante compounds and related methods for synthesizing these compounds and analogs. In certain embodiments, these glucosinolate and isothiocyanate compounds are useful and chemopreventive and or chemotherapeutic agents. | 2008-12-18 |
20080312165 | Process for obtaining pure monosialoganglioside GM1 for medical use - A process for preparing pure monosialoganglioside GM1 in the form of its sodium salt. There is provided a process for the isolation and purification of monosialoganglioside GM1 comprising (a) separation of GM1 from a lipidic mixture containing the monosialoganglioside GM1 as the main ganglioside component by ion exchange column-chromatography using an eluent comprising potassium or caesium ions, (b) recovery of the solute from the eluted solution, (c) diafiltration of an aqueous solution of the recovered solute, and (d) second diafiltration after the addition of 1 M NaCl, and recovering GM1. The purity level of GM1 obtained is higher than 99.0%. | 2008-12-18 |
20080312166 | Reversal core pharmaceutical system and method - A medication delivery system is disclosed to mitigate or reverse the pharmacologic effect of a medication beyond the desired therapeutic window. The system provides sequential delivery of medications including a first agent which induces a physiologic change, a second agent for reversing the physiologic change, and a medication release delaying agent for delaying the release of the second agent so that, upon receipt of the medication delivery system into the body the first agent is released before the second agent so that the physiologic effect of the first agent is mitigated by the second agent. The system can be a pill with the first agent comprising an outer medication and the second agent an inner medication with the medication release delaying agent intermediate the outer medication and the inner medication. In an example, the first agent can comprise a sleep aid and the second agent an arousal agent. | 2008-12-18 |
20080312167 | 4'' Amino Linked Macrolides Useful for the Treatment of Microbial Infections - The present invention relates to 15-membered macrolides substituted at the 4″ position of formula (I) | 2008-12-18 |
20080312168 | Novel Dispersible Tablet Composition - The present invention relates to a novel dispersible tablet composition, which comprises of a pharmacologically active ingredient and at least one excipient, which reduces the sedimentation rate of active ingredient. This invention further relates to a process for the preparation of a dispersible tablet of a pharmacologically active ingredient. | 2008-12-18 |
20080312169 | Cosmetic use of D-ribose - D-ribose is incorporated into a cosmetic composition and applied to the skin to reduce the length and area of wrinkles and to improve the complexion of the skin. | 2008-12-18 |
20080312170 | Fibrinolysin of Agkistrodon Acutus Venom and its Usage - The present invention relates to a fibrinolysin gene of Agkistrodon acutus, a vector containing the said gene and the host cell which transformed by the vector. The fibrinolysin could be used in treating diseases caused by thrombus. The fibrinolysin FII is purified from the crude venom of Agkistrodon acutus, and the corresponding gene is cloned. It is recommended to produce the fibrionolysin by the yeast expression system. The activity of the fibrionlysin is also determined. The advantages of this invention are that the expression level and activity of the fibrinolysin are both high and the quality of the fibrinolysin is stable. | 2008-12-18 |
20080312171 | Tetracycline-Dependent Regulation of Rna Interference - The present invention relates to a tetracycline dependent gene regulatory system or composition controlling the expression of a target gene in a cell and to methods using said system or composition. The present invention more specifically discloses compositions, vectors and methods allowing tetracycline-controlled expression of short-hairpin RNAs (shRNAs), and demonstrates inducible, reversible and stable RNA interference (RNAi) using the same in a cell. The invention can be used to cause reversible control of the expression of any gene and may therefore find applications in the fields of mammalian, in particular human, genetics and molecular therapeutics, in cell and gene therapy, research as well as in genetic studies using transgenic animals. | 2008-12-18 |
20080312172 | Anti-IL-6 Antibodies, Compositions, Methods and Uses - The present invention relates to at least one novel chimeric, humanized or CDR-grafted anti-IL-6 antibodies derived from the murine CLB-8 antibody, including isolated nucleic acids that encode at least one such anti-IL-6 antibody, vectors, host cells, transgenic animals or plants, and methods of making and using thereof, including therapeutic compositions, methods and devices. | 2008-12-18 |
20080312173 | Treatment of HSV-related pathologies using plasmids that make ssDNA - A composition for treatment of HSV-related pathologies including an expression vector for altering expression of a target sequence in an HSV-infected cell by production of single-stranded cDNA (ssDNA) in the cell in vivo suspended for topical application to an affected site in a suitable delivery vehicle. The expression vector is comprised of a cassette comprising a sequence of interest, an inverted tandem repeat, and a primer binding site 3′ to the inverted tandem repeat, and a reverse transcriptase/RNAse H coding gene, and is transfected into the infected cells for inhibition of HSV replication. The resulting ssDNA binds to the target sequence to alter expression of the target sequence for such purposes as gene activation or inactivation using duplex or triplex binding of nucleic acids, site-directed mutagenesis, interruption of cellular function by binding to specific cellular proteins, or interfering with RNA splicing functions. | 2008-12-18 |
20080312174 | WATER SOLUBLE CROSSLINKED POLYMERS - Compositions for siRNA delivery are described which include water soluble degradable crosslinked cationic polymers having a water soluble polyethylene glycol component, a cationic polyethyleneimine component and a degradable unit component. The composition may be used to deliver siRNA to cells, particularly cancer cells. The composition may be applied to a solid surface such as a multiwell plate so that the delivery of siRNA may be carried out on the solid surface. | 2008-12-18 |
20080312175 | METHODS AND COMPOSITIONS FOR REGULATING HDAC4 ACTIVITY - The present invention provides methods and compositions for modulating HDAC4 activity and modulating the activity of proteins downstream of HDAC4 in the muscle transcriptional pathway in a cell by modulating HDAC4 activity. Further provided are methods and compositions for treating muscle atrophy and/or inflammation by inhibiting HDAC4 activity. | 2008-12-18 |
20080312176 | GENE SILENCING - Methods are disclosed for gene silencing (e.g. post transcriptional gene silencing) in an organism using small RNA molecules. | 2008-12-18 |
20080312177 | SERCA2 THERAPEUTIC COMPOSITIONS AND METHODS OF USE - The present invention provides methods for treating urinary incontinence, urethral sphincter dysfunction and/or bladder dysfunction by delivering a therapeutic adeno-associated virus (AAV)-SERCA2 composition to a subject in need thereof. | 2008-12-18 |
20080312178 | Human G-Protein Receptor HGBER32 - Human G-protein coupled receptor polypeptides and DNA (RNA) encoding such polypeptides and a procedure for producing such polypeptides by recombinant techniques is disclosed. Also disclosed were methods for utilizing such polypeptides for identifying antagonists and agonists to such polypeptides and methods of using the agonists and antagonists therapeutically to treat conditions related to the underexpression and overexpression of the G-protein coupled receptor polypeptides, respectively. Also disclosed are diagnostic methods for detecting a mutation in the G-protein coupled receptor nucleic acid sequences and an altered level of the soluble form of the receptors. | 2008-12-18 |
20080312179 | High level expression of recombinant human erythropoietin having a modified 5'-UTR - The present invention provides an expression construct capable of producing high levels of erythropoietin in mammalian cells. More particularly, the expression construct includes an erythropoietin coding region fused to a unique 5′-UTR sequence and a truncated 3′-UTR. The present invention also provides methods of synthesizing large amounts of erythropoietin and in increasing serum erythropoietin level in individuals in need thereof. | 2008-12-18 |
20080312180 | Methods to Protect Skeletal Muscle Against Injury - Disclosed herein are compositions and methods for the treatment of skeletal muscle and/or the protection of skeletal muscle against injury. The adenosine A | 2008-12-18 |
20080312181 | Composition and Methods for Skin Care - Compositions useful in the treatment of skin atrophy and improvement of skin appearance and texture are disclosed. The methods include the topical administration of vitamin D3 or specific vitamin D3 analogs as an essential ingredient either on its own or in combination with cADPR and or nicotinamide. The compositions are particularly effective in preventing and treating signs of chronological and or photoaging including fine lines, wrinkles and discoloration. | 2008-12-18 |
20080312182 | OPHTHALMIC COMPOSITION WITH HYALURONIC ACID AND POLYMERIC BIGUANIDE - An ophthalmic composition comprising 0.5 ppm to 3 ppm of poly(hexamethylene biguanide), and 0.002 wt. % to 0.03 wt. % of hyaluronic acid. The weight ratio of hyaluronic acid to poly(hexamethylene biguanide) in the composition is from 45:1 to 120:1. The invention is also directed to a method of cleaning, disinfecting or packaging contact lenses with the composition, or to a method of rewetting contact lenses with the composition. | 2008-12-18 |
20080312183 | Dutpase Inhibitors - Deoxyuridine derivatives of the formula (I) where R | 2008-12-18 |
20080312184 | Composition for Preventing Plant Diseases and Method for Preventing the Diseases - The present invention is to provide a composition for preventing plant diseases which comprises at least Component I and Component II, is capable of obtaining a synergic effect that cannot be expected with each single component, is capable of markedly increasing a control effect in a much smaller amount of chemicals against various plant pathogens, and causes no phytotoxicity suffering. | 2008-12-18 |
20080312185 | SUBSTITUTED 3-AMINO-THIENO[2,3-b]PYRIDINE-2-CARBOXYLIC ACID AMIDE COMPOUNDS AND PROCESSES FOR PREPARING AND THEIR USES - Disclosed are methods of treating cancer by administration of compounds according to formula (I): | 2008-12-18 |
20080312186 | KETONES AND REDUCED KETONES AS THERAPEUTIC AGENTS FOR THE TREATMENT OF BONE CONDITIONS - The present invention pertains to certain ketones and reduced ketones and derivatives thereof which, inter alia, inhibit osteoclast survival, formation, and/or activity; and/or inhibit bone resorption, and more particularly to compounds of the formulae and pharmaceutically acceptable salts, amides, esters, and ethers thereof, wherein: Ar1, R | 2008-12-18 |
20080312187 | PHOSPHOINOSITIDE MODULATION FOR THE TREATMENT OF ALZHEIMER'S DISEASE - The present invention relates to methods of treating Alzheimer's Disease which utilize agents that increase neuronal phosphotidylinositol 4,5-biphosphate (PIP2), and to differentiated stem cell-based assay systems that may be used to identify agents that modulate phosphoinositide levels and thereby treat a variety of diseases. It is based, at least in part, on the discovery that edelfosine, an agent that increases PIP2 levels by inhibiting an enzyme that catalyzes PIP2 breakdown, decreases levels of neurotoxic A&bgr;42 peptide, particularly in cells expressing a mutant presenilin gene associated with Familial Alzheimer's Disease. | 2008-12-18 |
20080312188 | Glycogen synthase kinase-3 inhibitors - Novel compounds designed to allow interactions with binding sites of GSK-3 and hence are capable of inhibiting GSK-3 activity, via inhibition of substrate binding are disclosed. Further disclosed are pharmaceutical compositions including same and methods of using same in the treatment of GSK-3 mediated conditions. | 2008-12-18 |
20080312189 | Cadasil Treatment with Cholinesterase Inhibitors - The invention provides methods for treating and/or preventing cerebral autosomal dominant arteriopathy with subcortical infarcts and leukoencephalopathy (CADASIL) in a patient in need thereof by administering a therapeutically effective amount of at least one cholinesterase inhibitor. The invention also provides methods for treating and/or preventing neurovascular diseases caused by one or more mutations of the human Notch3 gene by administering a therapeutically effective amount of at least one cholinesterase inhibitor. In one embodiment, the cholinesterase inhibitor is donepezil, a stereoisomer thereof and/or a pharmaceutically acceptable salt thereof. The methods of the invention may further include administering a therapeutically effective amount of an HMG-CoA reductase inhibitor | 2008-12-18 |
20080312190 | Organophosphoric Derivatives Useful as Anti-Parasitic Agents - The present invention relates to novel phosphonic acid compounds having the structural formula (I): wherein: (a) R is a group of 1 to 5 substituents independently selected from the group consisting of fluoro, chloro, bromo, C | 2008-12-18 |
20080312191 | Novel Urokinase Inhibitors - The present invention relates to novel compounds with inhibitory activity towards urokinase plasminogen activator (uPA); to methods for preparation of said uPA inhibitor compounds; to pharmaceutical compositions comprising said uPA inhibitor compounds; to the use of said uPA inhibitor compounds as a medicament and the use of said uPA inhibitor compounds for the preparation of a medicament for the treatment of conditions chosen from the group comprising cancer, tumour growth, tumour invasion, tumour metastasis, diabetic retinopathy, hemorrhagic atherosclerosis and inflammatory conditions, such as rheumatoid arthritis and psoriasis. | 2008-12-18 |
20080312192 | Diaryl Urea Derivatives in the Treatment of Protein Kinase Dependent Diseases - The invention relates to the use of diaryl urea derivatives for the manufacture of pharmaceutical compositions for the treatment of RET dependent disorders, especially RET dependent tumour diseases. The invention further relates to novel N-[4-(pyrimidin-4-yloxy)-phenyl]-N′-phenyl-urea derivatives and their use in the treatment of the animal or human body, especially in the treatment of a protein kinase dependent disease, to pharmaceutical compositions comprising such novel N-[4-(pyrimidin-4-yloxy)-phenyl]-N′-phenyl-urea derivatives and to the use of such novel N-[4-(pyrimidin-4-yloxy)-phenyl]-N′-phenyl-urea derivatives for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as tumour diseases. | 2008-12-18 |
20080312193 | Substituted Tetracycline Compounds for Treatment of Inflammatory Skin Disorders - Methods and compositions for the treatment of skin disorders (e.g., acne, rosacea) are described. | 2008-12-18 |
20080312194 | Methods and compositions for normalizing meibomian gland secretions - The present invention provides non-aqueous compositions for normalizing meibomian gland secretions, and methods of use thereof. The present invention further provides compositions and methods for treating and/or preventing the signs and/or symptoms of dry eye disease. | 2008-12-18 |
20080312195 | Preservatives - The invention relates to clear, liquid preservatives, which contain a) one or several 1-hydroxy-4-methyl-6-alkyl-2(1H)-pyridones and/or one or several salts thereof. wherein alkyl represents a linear, branched or cyclic alkyl group having 1-12 carbon atoms, and b) one or several alcohols containing one or several aromatic groups. | 2008-12-18 |
20080312196 | Topical wart removal composition - A non-aqueous liquid composition for topical application to warts and other fibroids, papillomas, and other growths for the removal of same is defined by a non-aqueous solution of: (a) at least one keratolytic compound or agent, (b) an adhesive, (c) a dermal regeneration promoter, and (d) a solvent. The composition is applied to the growth or growth site on a daily basis for about at least seven days. The composition can be applied directly to the site or via an impregnated bandage. | 2008-12-18 |
20080312197 | PHARMACEUTICAL PRODUCTS CONTAINING HORMONES AND A 25-HYDROXY VITAMIN D COMPOUND - The present invention relates to pharmaceutical products containing progestins in combination with the 25 hydroxy Vitamin D compounds. The 25 hydroxy Vitamin D compounds are preferably administered with the progestins. In OC and HRT regimens, the 25 hydroxy Vitamin D compounds can be administered daily, or on a non-daily basis, and if so, preferably when the progestin dosages are the highest in the cycle. | 2008-12-18 |
20080312198 | PHARMACEUTICAL PRODUCTS CONTAINING HORMONES AND A 25-HYDROXY VITAMIN D COMPOUND - The present invention relates to pharmaceutical products containing progestins in combination with the 25 hydroxy Vitamin D compounds. The 25 hydroxy Vitamin D compounds are preferably administered with the progestins. In OC and HRT regimens, the 25 hydroxy Vitamin D compounds can be administered daily, or on a non-daily basis, and if so, preferably when the progestin dosages are the highest in the cycle. | 2008-12-18 |
20080312199 | Treatments of therapy resistant diseases and drug combinations for treating the same - The present invention provides novel methods and kits for diagnosing the presence of cancer within a patient, and for determining whether a subject who has cancer is susceptible to different types of treatment regimens. The cancers to be tested include, but are not limited to, prostate, breast, lung, gastric, ovarian, bladder, lymphoma, mesothelioma, medullablastoma, glioma, and AML. Identification of therapy-resistant patients early in their treatment regimen can lead to a change in therapy in order to achieve a more successful outcome. One embodiment of the present invention is directed to a method for diagnosing cancer or predicting cancer-therapy outcome by detecting the expression levels of multiple markers in the same cell at the same time, and scoring their expression as being above a certain threshold, wherein the markers are from a particular pathway related to cancer, with the score being indicative or a cancer diagnosis or a prognosis for cancer-therapy failure. This method can be used to diagnose cancer or predict cancer-therapy outcomes for a variety of cancers. The markers can come from any pathway involved in the regulation of cancer, including specifically the PcG pathway and the “stemness” pathway. The markers can be mRNA, microRNA, DNA, or protein. | 2008-12-18 |
20080312200 | Medicament Comprising A Hormone Combination - The present invention relates to the use of a hormone combination of ethinyl oestradiol or oestradiol as oestrogen component and at least one metabolite of chlormadinone acetate selected from the group consisting of 3α-hydroxy-6-chloro-17α-acetoxy-4,6-pregnadien-20-one (3α-hydroxychlormadinone acetate), 3β-hydroxy-6-chloro-17α-acetoxy-4,6-pregnadien-20-one (3β-hydroxychlormadinone acetate), 3α-hydroxy-17α-acetoxy-5β-pregnan-20-one and 3β-hydroxy-17α-acetoxy-5β-pregnan-20-one, optionally mixed with chlormadinone acetate as gestagen component for producing a medicament at least for alleviating menstrual cycle-dependent mood swings and optionally for hormonal contraception in women. | 2008-12-18 |
20080312201 | Reduced Toxicity Methotrexate Formulations and Methods for Using the Same - Methods of using methotrexate (MTX) active agents in which reduced host toxicity is observed are provided. In the subject methods, an effective amount of an MTX active agent is administered to the host in conjunction with the administration of an MTX toxicity reducing agent of the present invention. Also provided are compositions for use in practicing the subject methods, e.g., pharmaceutical compositions having reduced toxicity, in which the MTX active agent is combined with an MTX toxicity reducing agent that reduces the level of undesired MTX toxicity while maintaining an effective MTX anti-proliferative activity. Also provided are methods of using the subject methods and compositions in the treatment of a variety of different disease conditions. | 2008-12-18 |
20080312202 | 6-SUBSTITUTED ESTRADIOL DERIVATIVES AND METHODS OF USE - A compound having the structure: | 2008-12-18 |
20080312203 | Bicyclic 6-Alkylidene-Penems as Beta-Lactamase Inhibitors - The present invention provides a compound of formula I | 2008-12-18 |
20080312204 | SOLUBLE FORMS OF AMOXICILLIN AND TREATMENT OF ANIMALS - A solid mixture or aqueous solution of amoxicillin antibacterial agent with a material that aids in its dissolution in water to render it ingestive and palatable. | 2008-12-18 |
20080312205 | METHOD AND INTERMEDIATES FOR THE PREPARATION OF DERIVATIVES OF N (1-BENZHYDRYLAZETIDIN-3-YL)-N-PHENYLMETHYLSULFONAMIDE - The invention relates to a novel method for the synthesis of N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-(3,5-difluorophenyl)methylsulfonamide. | 2008-12-18 |
20080312206 | Chemical Compounds-149 - The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula which possess CSF 1R kinase inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man. | 2008-12-18 |
20080312207 | Compounds - Compounds of Formula (I) wherein: R1 is methyl; R2 is selected from —C (O) NR4R5, SO2NR4R5, S (O) pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C) alkyl and HET-2; R5 is hydrogen or (1-4C) alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them and processes for their preparation are also described. | 2008-12-18 |
20080312208 | Pyridine Analogues - The present invention relates to certain new pyridin analogues of Formula (I) Chemical formula should be inserted here. Please see paper copy Formula (I) to processes for preparing such compounds, to their utility as P2Y | 2008-12-18 |
20080312209 | Piperazine Heteroaryl Derivatives as Gpr38 Agonists - The invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof, | 2008-12-18 |
20080312210 | USE OF A SPECIFIC CYCLIC AMINE DERIVATIVE OR THE PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF FOR THE TREATMENT OR PREVENTION OF HEART FAILURE - The present invention provides the use in a pharmaceutical composition of a specific cyclic amine derivative, or its pharmaceutically acceptable salts, for the treatment of heart failure of any aetiology. | 2008-12-18 |
20080312211 | Antibacterial Pyrrolopyridines, Pyrrolopyrimidines and Pyrroloazepines-154 - Compounds of formula (I) and their pharmaceutically acceptable salts are described: formula (I). Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described. | 2008-12-18 |
20080312212 | Organic Compounds - A compound of formula (I) | 2008-12-18 |
20080312213 | 7-Pyrazolylbenzazepines Having Affinity For D3 Receptor - Compounds of formula (I) or a salt thereof are disclosed: | 2008-12-18 |
20080312214 | Inhibitors of the 11-Beta-Hydroxysteroid Dehydrogenase Type 1 Enzyme - Methods for treating a mammal suffering from glucocorticoid-related diseases and conditions, comprising administering to the mammal an effective amount of a selective inhibitor of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme activity, wherein the inhibitor is a compound of formula (I): | 2008-12-18 |
20080312215 | Substituted [1,4]-diazepanes as CXCR3 antagonists and their use in the treatment of inflammatory disorders - CXCR3 inhibitors of formula | 2008-12-18 |
20080312216 | PIPERAZINE AND [1,4]DIAZEPAN DERIVATIVES AS NK ANTAGONISTS - The present invention relates to a compound of formula I | 2008-12-18 |
20080312217 | Organic Compounds - A Compound of formula (I) | 2008-12-18 |
20080312218 | FUSED TETRACYCLIC MGLUR1 ANTAGONISTS AS THERAPEUTIC AGENTS - In its many embodiments, the present invention provides tetracyclic compounds of formula I or formula II (wherein the various moieties are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimers disease. | 2008-12-18 |
20080312219 | Biologically active methylene blue derivatives - The present invention relates to a phenothiazinium compound of Formula (I): | 2008-12-18 |
20080312220 | Oxadiazole Derivatives with Crth2 Receptor Activity - Compounds of formula are CRTH2 ligands, useful for treatment of inflammatory, autoimmune, respiratory or allergy disease: wherein R | 2008-12-18 |
20080312221 | QUINOLINE DERIVATIVE AND QUINAZOLINE DERIVATIVE INHIBITING SELF-PHOSPHORYLATION OF HEPATOCYTUS PROLIFERATOR RECEPTOR, AND MEDICINAL COMPOSITION CONTAINING THE SAME - An objective of the present invention is to provide compounds having potent antitumor activity. The compounds of the present invention are represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: | 2008-12-18 |
20080312222 | 4-Benzyledene-Piperidin Derivatives - The present invention relates to new 4-benzylidene-piperidin derivatives of formula (I), useful as NMDA, in a particular NR2B subunit containing receptor antagonists and analgesica. | 2008-12-18 |
20080312223 | Thiazole And Isothiazole Derivatives That Modulate The Activity Of CDK, GSK And Aurora Kinases - The invention provides a compound of the formula (I): or a salt, N-oxide, tautomer or solvate thereof, wherein X is CR | 2008-12-18 |
20080312224 | Oxaphenanthrene Derivatives - The invention relates to compounds of the formula (I), in which R | 2008-12-18 |
20080312225 | Triazolophthalazines - The compounds of formula (I) | 2008-12-18 |
20080312226 | Amide Compound - There is provided a FAAH inhibitor and a prophylactic or therapeutic agent for cerebrovascular disorders or sleep disorders comprising it. The prophylactic or therapeutic agent comprises a compound of the formula (I | 2008-12-18 |
20080312227 | Substituted Pyrido(2,3-D) Pyrimidine Derivatives Useful as Medicines for the Treatment of Autoimmune Disorders - This invention relates to a group of trisubstituted pyrido(2,3-d)pyrimidine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These derivatives are also useful in preventing or treating cardiovascular disorders, disorders of the central nervous system, TNF-α related disorders and cell proliferative disorders. | 2008-12-18 |
20080312228 | PYRIMIDINE COMPOUND AND MEDICAL USE THEREOF - The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I] | 2008-12-18 |
20080312229 | Organic Compounds - There are provided according to the invention compounds of formula (I) | 2008-12-18 |
20080312230 | Organic Compounds - There are provided according to the invention compounds of formula (I), | 2008-12-18 |
20080312231 | Substituted Sulfonamide Compounds - Substituted sulfonamide compounds corresponding to formula I | 2008-12-18 |
20080312232 | Substituted amide derivatives and methods of use - Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes. | 2008-12-18 |
20080312233 | Therapeutic Morpholino-Substituted Compounds - Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation. The compounds are useful in treating PI 3-kinase-dependent conditions including cardiovascular diseases such as coronary artery occlusion, stroke, acute coronary syndrome, acute myocardial infarction, vascular restenosis, atherosclerosis, and unstable angina; respiratory diseases such as asthma, chronic obstructive pulmonary diseases (COPD), and bronchitis; inflammatory disorders; neoplasms including cancers such as glioma, prostate cancer, small cell lung cancer, and breast cancer; and diseases linked to disordered white blood cell function, such as autoimmune and inflammatory diseases. | 2008-12-18 |
20080312234 | NOVEL COMPOUNDS, ISOMER THEREOF, OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AS VANILLOID RECEPTOR ANTAGONIST; AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME - This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on. | 2008-12-18 |
20080312235 | Pyridine Derivatives -
The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain. | 2008-12-18 |
20080312236 | 3-Heteroaryl-3-Hydroxy-2-Amino-Propyl Amines And Related Compounds Having Analgesic And/Or Immuno Stimlant Activity - Compounds of the formula | 2008-12-18 |
20080312237 | Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same - Compounds are disclosed that have a formula represented by the following: | 2008-12-18 |
20080312238 | 4-Arylazo-3,5-Diamino-Pyrazole Compounds and Use Thereof - A series of mono- and binuclear 4-arylazo-3,5-diamino-pyrazoles which are useful for inhibition of cyclin-dependent kinases (preferably CDK9). Hence they can be used as antimitotic-, pro-apoptotic and antiinflammatory drugs, in particular, in chemotherapy of cancer and asthma, therapy of psoriasis and parasitoses as those caused by fungi or protists, treatment of Alzheimer's disease or as anti neurodegenerative drugs, or to suppress immunostimulation. These compounds are useful in a variety of utilities, including as intermediates in the preparation of flame-retardants, diagnostic reagents and therapeutics, including antivirals and immunosuppressors. | 2008-12-18 |
20080312240 | Bicyclic Piperazines as Metabotropic Glutatmate Receptor Antagonists - The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: | 2008-12-18 |
20080312241 | Cicletanine and PKC inhibitors in the treatment of pulmonary and cardiac disorders - Embodiments of the present invention are related to novel therapeutic drugs, drug combinations, and associated methods for treating or preventing pulmonary disease, including pulmonary hypertension, pulmonary fibrosis, asthma and COPD, and heart failure, together with other pulmonary and cardiovascular diseases and their complications. More particularly, aspects of the present invention are related to the use of cicletanine and ruboxistaurin as monotherapies or in combination with other agents for treatment of disease. Cicletanine may be used as pure (+) or (−) enantiomers or as a racemic or non-racemic mixture of those enantiomers. | 2008-12-18 |
20080312242 | 7-ARYL-3, 9-DIAZABICYCLO(3.3.1)NON-6-ENE DERIVATIVES AND THEIR USE AS RENIN INHIBITORS IN THE TREATMENT OF HYPERTENSION, CARDIOVASCULAR OR RENAL DISEASES - The invention relates to novel 3,9-diazabicyclo[3.3.1]nonene derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors or renin. | 2008-12-18 |
20080312243 | IMIDAZOLES AND TRIAZOLES, THEIR PREPARATION, AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to imidazoles and triazoles of general formula | 2008-12-18 |
20080312244 | Squaric Acid Derivatives as Protein Kinase Inhibitors - Compounds of the formula I, in which R, X, R | 2008-12-18 |
20080312245 | Methods and compositions for treating acne and other infectious diseases - The present invention provides a composition comprising metronidazole, ketoconazole, and lincomycin and methods of treating infectious skin diseases such as acne by topically administering the composition. | 2008-12-18 |
20080312246 | Substituted Piperazines as Metabotropic Glutamate Receptor Antagonists - The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: | 2008-12-18 |
20080312247 | SUBSTITUTED PIPERAZINES - Disclosed herein are substituted piperazine late Na | 2008-12-18 |
20080312248 | Pyrimidinyl Aryl Urea Derivatives Being Fgf Inhibitors - The invention relates to heteroaryl aryl ureas of the formula IA, | 2008-12-18 |
20080312249 | KMUP-1 CAPABLE OF TREATING HYPERTENSION - A pharmaceutical composition for treating the hypertension is provided. The pharmaceutical composition comprises a chemical compound of 7-[2-[4-(2-Chlorobenzene)piperazinyl]ethyl]-1,3-dimethyl xanthine and one of a pharmaceutical acceptable salt thereof and a solvate thereof, wherein the chemical compound treats the hypertension by cGMP-dependent inhibition on Rho kinase. | 2008-12-18 |
20080312250 | Combination Comprising a Bcrp Inhibitor and 4- (4-Methylpiperazin-1-Ylmethyl)-N-[4-Methyl-3- (4-Pyridin-3-Yl) Pyrimidin-2-Ylamino) Phenyl] -Benzamide - The present invention relates to a combination which comprises a BCRP inhibitor and Compound I of formula (I), | 2008-12-18 |
20080312251 | Aminopyrimidine Compounds and Their Salts, Process for Preparation and Pharmaceutical Use Thereof - The present invention provides aminopyrimidine compounds of formula (I) and their salts, wherein R | 2008-12-18 |
20080312252 | Combination of Organic Compounds - The invention provides a pharmaceutical combination comprising:
| 2008-12-18 |
20080312253 | Pharmaceutical compositions containing pyrazole derivatives for treating as serotonin antagonist - The present invention relates to a pharmaceutical composition containing a pyrazole derivative as an active ingredient, which has antagonistic activity against serotonin 5-HT | 2008-12-18 |
20080312254 | Process for the Preparation of Ziprasidone - The invention relates to processes for the preparation of substantially pure ziprasidone. The invention also relates to the preparation of acid addition salts of ziprasidone. More particularly, it relates to the preparation of substantially pure hydrochloride salt of ziprasidone. The invention also relates to pharmaceutical compositions that include the substantially pure ziprasidone or ziprasidone hydrochloride and use of said compositions for treating schizophrenia. | 2008-12-18 |
20080312255 | PIPERDINE COMPOUNDS AND USES THEREOF-911 - Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described. | 2008-12-18 |
20080312256 | Organic Compounds - The present invention provides compounds of the formula | 2008-12-18 |
20080312257 | Triazolopyrimidine derivatives as ADP P2Y12 receptor antagonists - The present invention is directed to novel bicyclic triazolopyrimidine compounds of Formula (I) or a form thereof: | 2008-12-18 |
20080312258 | METABOLITES OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE - The present invention provides active metablites of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 2008-12-18 |
20080312259 | SALTS OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE - The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 2008-12-18 |