44th week of 2009 patent applcation highlights part 46 |
Patent application number | Title | Published |
20090270338 | DIARYL-CYCLYLALKYL DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity are disclosed. Specifically, a series of compounds of substituted or unsubstituted N-cyclylalkyl-diphenylpropanamide derivatives as shown in formula (1). | 2009-10-29 |
20090270339 | Unit Dose Form of Glufosfamide - A lyophilized unit dose form containing about 2 g of glufosfamide is useful in treatment of cancer and other hyper-proliferative diseases. | 2009-10-29 |
20090270340 | METHODS OF ADMINISTERING ANTITUMOR AGENT COMPRISING DEOXYCYTIDINE DERIVATIVE - Antitumor treatment regimens comprising: administering, to a patient diagnosed with cancer, an antitumor agent comprising 4-amino-1-(2-cyano-2-deoxy-β-D-arabinofuranosyl)-2(1H)-pyrimidinone, or a salt thereof, by way of continuous intravenous infusion, in an amount of 2.0 to 4.0 mg per m | 2009-10-29 |
20090270341 | PRODUCT COMPRISING A TRANSDUCTION INHIBITOR OF HETEROTRIMERIC G PROTEIN SIGNALS COMBINED WITH ANOTHER ANTI-CANCER AGENT FOR THERAPEUTIC USE IN THE TREATMENT OF CANCER - A composition for treating cancer comprising an anti-tumorally effective amount of a product comprising at least one transduction inhibitor of heterotrimeric G protein signals and at least one other anti-cancer agent selected from the group consisting of prenyltransferase inhibitors, taxol and its analogues, gemcitabine and camptothecin and its analogues, administered simultaneously, separately or spread over a period of time and a pharmaceutical carrier. | 2009-10-29 |
20090270342 | IMMUNOREGULATORY AGENT - An object of the present invention is to provide an immunoregulatory agent, which can be continuously ingested on daily diet and has no fear of causing side effects, and a method for regulating immunity. The present invention solves the above object by providing an immunoregulatory agent comprising lactosucrose as an effective ingredient and a method for regulating immunity using lactosucrose. | 2009-10-29 |
20090270343 | Polysaccharide Extract of Lentinus and Pharmaceutical, Cosmetic or Nutraceutical Compositions Comprising Such an Extract - The present invention relates to a polysaccharide extract derived from a mushroom of the | 2009-10-29 |
20090270344 | Structure and bioactivity of the polysaccharides and oligomers in medicinal plant Dendrobium huoshanense - Compositions and methods are disclosed relating to use of fractions, polysaccharides, and oligosaccharides of | 2009-10-29 |
20090270345 | POLYMERIC ARTIFICIAL TEAR SYSTEM - The present invention relates to artificial tear formulations and ophthalmic formulations suitable for drug delivery. The formulations comprise galactomannans such as guar or hydroxypropyl guar and a borate source such as boric acid. The formulations further comprise a cis-diol such as sorbitol that interferes with the cross-linking of galactomannan and borate. Optionally, the formulations are substantially free of divalent cations. | 2009-10-29 |
20090270346 | PROTECTIVE GEL BASED ON CHITOSAN AND OXIDIZED POLYSACCHARIDE - Bodily tissue and structures may be protected using a fluid layer containing a mixture of chitosan and oxidized polysaccharide. The mixture forms a protective gel layer via in situ crosslinking. Compared to crosslinking using a low molecular weight aldehyde such as glutaraldehyde or genipin, oxidized polysaccharides appear to provide faster gelation while avoiding the use of potentially less bioacceptable low molecular weight aldehydes. | 2009-10-29 |
20090270347 | METHODS OF PRODUCING MICROPARTICLES - Methods of producing microparticles, and especially chitin microparticles (CMP), are disclosed that involve reducing the size of (larger) particles using a (high shear) microfluidising instrument. | 2009-10-29 |
20090270348 | Sulfoalkyl Ether Cyclodextrin Compositions - SAE-CD compositions are provided, along with methods of making and using the same. The SAE-CD composition comprises a sulfoalkyl ether cyclodextrin and less than 100 ppm of a phosphate, wherein the SAE-CD composition has an absorption of less than 0.5 A.U. due to a drug-degrading agent, as determined by UV/vis spectrophotometry at a wavelength of 245 nm to 270 nm for an aqueous solution containing 300 mg of the SAE-CD composition per mL of solution in a cell having a 1 cm path length. | 2009-10-29 |
20090270349 | Physical Mode of Action Pesticide - A physical mode of action pesticide for application on plants and in soils, and methods of manufacture and application, comprising an active ingredient in the form of a polymer in a concentration of less than 0.1% wt., a surfactant, a co-solvent and a diluent in a hydrocolloid suspension. The suspension polymer is preferably a polysaccharide having a molecular weight of 10,000 to 25,000,000, and preferably in the range of about 600,000. The pesticide preferably also includes a targeting ingredient for directing the active ingredient to a particular target. | 2009-10-29 |
20090270350 | Pyridinone Pyrazole Urea and Pyrimidinone Pyrazole Urea Derivatives - This invention is directed generally to substituted pyridinone and pyrimidinone compounds that generally inhibit p38 kinase, TNF, and/or cyclooxygeπase activity. Such substituted pyridinone and pyrimidinone compounds include compounds generally corresponding in structure to the following formula: wherein Z, n, R | 2009-10-29 |
20090270351 | PHOSPHORUS DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS - The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the phosphorus derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the phosphorus derivatives in vivo. | 2009-10-29 |
20090270352 | Tenofovir Disoproxil Hemi-Fumaric Acid Co-Crystal - The present invention provides a novel crystalline form of Tenofovir disoproxil fumarate (Tenofovir DF), designated Co-crystal TDFA 2:1, methods for the preparation thereof and its use in pharmaceutical applications, in particular in anti-HIV medicaments. The crystalline form TDFA 2:1 can be used in combination with other anti-HIV medicaments such as Efavirenz, Emtricitabine, Ritonavir and/or TMC114. | 2009-10-29 |
20090270353 | COMPOUNDS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS - The invention relates to compounds of structural formula (I): | 2009-10-29 |
20090270354 | Method of removing ticks from the skin and reducing the risk of bites - Compositions and method of using the same for the removal of ticks embedded in the skin or tissue of a human or animal host and for preventing ticks from attaching themselves to and biting humans or other animals. | 2009-10-29 |
20090270355 | Compounds - The present invention relates to a compound which is N-(4-{4-[(6-butyl-8-quinolinyl)oxy]-1-piperidinyl}butyl)ethanesulfonamide | 2009-10-29 |
20090270356 | COMPOSITIONS AND TREATMENTS OF HEART FAILURE IN NON-HUMAN MAMMAL ANIMALS - The invention relates to new compositions comprising an aldosterone antagonist according to a particular posology for the treatment of heart failure in non-human mammal animals. | 2009-10-29 |
20090270357 | Method and use of nanoparticles to bind biocides in paints - This invention relates to the use of a combination of selected substances in paint to prevent the settlement and growth of different biofouling organisms with a reduced negative effect on the ecosystems compared to present methods. | 2009-10-29 |
20090270358 | PHARMACEUTICAL FORMULATION OF CLAVULANIC ACID - The present invention generally relates to stable pharmaceutical compositions, and methods of making and administering such compositions. In one aspect, the invention features stabilized pharmaceutical compositions that include pharmaceutically active ingredients such as potassium clavulanate or Clavitesse™, preferably in an immediate-release solid dosage form or an extended-release solid dosage form. Also provided are methods for making and using such immediate-release and stabilized compositions or extended-release and stabilized compositions. | 2009-10-29 |
20090270359 | SUBSTITUTED PYRAZOLE DERIVATIVES - The present invention provides a novel pyrazole derivative and an androgen receptor antagonist containing the derivative. The present invention provides a compound represented by the formula (I′) | 2009-10-29 |
20090270360 | DICARBOXAMIDE DERIVATIVES - The invention is concerned with novel dicarboxamide derivatives of formula (I) | 2009-10-29 |
20090270361 | Substituted pyrazole derivatives and use thereof - The present invention aims to provide a novel pyrazole derivative and a pharmaceutical agent containing the same. The present invention provides a compound represented by the formula (I′) | 2009-10-29 |
20090270362 | BICYCLIC MGLUR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME - In one aspect, the invention relates to bicyclic MGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2009-10-29 |
20090270363 | 2-Aryl- and 2-Heteroarylthiazolyl Compounds, Methods for Their Preparation and Use Thereof - The present invention discloses fused bicyclic 2-aryl- or 2-heteroarylthiazolyl compounds and their pharmaceutically acceptable salts and esters thereof, which are useful for inhibiting the growth of cancerous cells, inhibiting human breast carcinoma tumor growth in particular and to treat diseases or disorders associated with securin, including elevated securin levels. | 2009-10-29 |
20090270364 | SUBSTITUTED PYRIMIDINE DERIVATIVES - The present application describes substituted pyrimidine compounds of formula (I) | 2009-10-29 |
20090270365 | BENZAMIDE DERIVATIVE OR SALT THEREOF - There is provided a compound having a capsaicin receptor VR1 inhibitory activity and useful as a therapeutic agent for various pains including inflammatory pain and neurogenic pain, migraine, cluster headache, bladder diseases including overactive bladder, and the like. | 2009-10-29 |
20090270366 | Benzoimidazole compounds - Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H | 2009-10-29 |
20090270367 | SUBSTITUTED HYDROXYETHYLAMINE ASPARTYL PROTEASE INHIBITORS - The invention relates to novel compounds and also to methods of treating at least one disease, disorder, or condition associated with amyloidosis using such compounds. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein. | 2009-10-29 |
20090270368 | Angiogenesis inhibition by cephalotaxine alkaloids, derivatives, compositions and uses thereof - The invention relates to compositions and methods useful in treating or preventing angiogenic disease. The invention provides for compositions comprising cephalotaxine alkaloids as antiangiogenic agents for treatment of a host with an angiogenic disease or for prophylactic treatment of a host to inhibit the onset or progression of an angiogenic disease. | 2009-10-29 |
20090270369 | BICYCLOAMINE DERIVATIVES - Compounds represented by formula (I) and pharmaceutically acceptable salts thereof have excellent sodium channel inhibitory action and are useful as therapeutic agents and analgesics for various kinds of neuralgia, neuropathy, epilepsy, insomnia, premature ejaculation and the like. | 2009-10-29 |
20090270370 | FUSED HETEROCYCLIC COMPOUNDS - Certain fused pyrrole- and pyrazole-containing heterocyclic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases. | 2009-10-29 |
20090270371 | QUINOLINE DERIVATIVES USEFUL IN THE TREATMENT OF MGLUR5 RECEPTOR-MEDIATED DISORDERS - Compounds of formula (I): and/or enantiomers and/or racemates and/or diastereomers and/or pharmaceutically acceptable salts thereof formed with acids or bases, to the process for their preparation, to the intermediates of the preparation process, to the pharmaceutical formulations containing these compounds and to their use in the prevention and/or treatment of mGluR5 receptor-mediated disorders. | 2009-10-29 |
20090270372 | NOVEL DERIVATIVES OF BENZIMIDAZOLE AND IMIDAZO-PYRIDINE AND THEIR USE AS MEDICAMENTS - A subject of the present Application is novel derivatives of benzimidazole and imidazopyridine which have a good affinity for certain sub-types of melanocortin receptors, in particular the MC4 receptors. They are particularly useful for treating pathological conditions and diseases in which one or more melanocortin receptors are involved. The invention also relates to pharmaceutical compositions containing said products. | 2009-10-29 |
20090270373 | TREATMENT OF DOWN SYNDROM WITH BENZODIAZEPINE RECEPTOR ANTAGONISTS - Pharmaceutical compositions and methods of treating Down Syndrome, mental retardation or both are provided. The pharmaceutical compositions comprise one or more benzodiazepine receptor antagonists, such as flumazenil. | 2009-10-29 |
20090270374 | DERIVATIVES AND ANALOGS OF N-ETHYLQUINOLONES AND N-ETHYLAZAQUINOLONES - Bicyclic nitrogen containing compounds and their use as antibacterials. | 2009-10-29 |
20090270375 | SPIRO ANTIBIOTIC DERIVATIVES - The invention relates to compounds of formula (I) wherein R | 2009-10-29 |
20090270376 | HETEROCYCLIC JANUS KINASE 3 INHIBITORS - The present invention provides a compound of formula (I) having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases inflammatory diseases, and allergic diseases. The compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia). | 2009-10-29 |
20090270377 | COMBINATION CANCER CHEMOTHERAPY - Provided is a method for improving treatment of a neoplastic condition by combining a therapeutically effective amount of a polyADP-ribose polymerase inhibitor with a therapeutically effective amount of a compound which triggers the release of nucleolin from the G-quadruplexes in rDNA. As specifically exemplified, the compound which increases nucleolin binding is a substituted quinobenzoxazine analog, for example CX-3543. | 2009-10-29 |
20090270378 | NOVEL TETRAHYDROPYRIDOTHIOPHENES - Compounds of a certain formula (I), in which Ra and Rb have the meanings indicated in the description, are novel effective compounds with anti-proliferative and/or apoptosis inducing activity. | 2009-10-29 |
20090270379 | QUINOLONE DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS - The present invention is directed to quinolone derivatives, useful as antimicrobial compounds, pharmaceutical compositions comprising said derivatives and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes | 2009-10-29 |
20090270380 | 3,4,5-Substituted Piperidines as Renin Inhibitors - The application relates to novel substituted piperidines of the general formula (II) in which R | 2009-10-29 |
20090270381 | Non-steroidal progesterone receptor modulators - The present invention relates to non-steroidal progesterone receptor modulators of the general formula I, | 2009-10-29 |
20090270382 | Soluble epoxide hydrolase inhibitors - Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases. | 2009-10-29 |
20090270383 | Novel Oxabispidine Compounds And Their Use In The Treatment Of Cardiac Arrhythmias - There is provided compounds of formula (I), wherein R | 2009-10-29 |
20090270384 | MORPHOLINE DOPAMINE AGONISTS - The present invention provides for compounds of formula (I), (Ia) and (Ib) | 2009-10-29 |
20090270385 | SUBSTITUTED ARYLCYCLOPENTENES AS THERAPEUTIC AGENTS - Compounds comprising | 2009-10-29 |
20090270386 | THERAPEUTIC COMPOUNDS - Compounds comprising | 2009-10-29 |
20090270387 | SUBSTITUTED ARYLCYCLOPENTENES AS THERAPEUTIC AGENTS - Compounds comprising | 2009-10-29 |
20090270388 | FUSED AZOLE-PYRIMIDINE DERIVATIVES - The present invention relates to novel fused azolepyriimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity. | 2009-10-29 |
20090270389 | Pyrimidinyl pyridone inhibitors of kinases - This application discloses novel pyrimidinyl pyridone derivatives according to formula I, wherein A, R | 2009-10-29 |
20090270390 | PYRIMIDINE DERIVATIVES - The invention concerns pyrimidine derivatives of Formula (I) wherein each of p, R | 2009-10-29 |
20090270391 | THIENOPYRIDINE DERIVATIVE, OR QUINOLINE DERIVATIVE, OR QUINAZOLINE DERIVATIVE, HAVING c-MET AUTOPHOSPHORYLATION INHIBITING POTENCY - An objective of the present invention is to provide compounds having antitumor activity. According to the present invention, there is provided compounds represented by formula (I) and pharmaceutically acceptable salts thereof, and solvates thereof: | 2009-10-29 |
20090270392 | SUBSTITUTED GAMMA LACTAMS AS THERAPEUTIC AGENTS - Therapeutic compounds, compositions, medicaments, and methods are disclosed herein. | 2009-10-29 |
20090270393 | Iminopyridine Derivatives and Use Thereof - The present invention aims to provide an iminopyridine derivative compound having an α | 2009-10-29 |
20090270394 | CYCLYLAMINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity are disclosed. Specifically, a series of compounds of substituted or unsubstituted cyclylamine derivatives as shown in formulas (1). | 2009-10-29 |
20090270395 | EP4 Receptor Agonist, Compositions and Methods Thereof - This invention relates to potent selective agonists of the EP | 2009-10-29 |
20090270396 | THERAPEUTIC COMPOUNDS - Compounds comprising | 2009-10-29 |
20090270397 | Methods and compositions for the treatment of cancers, such as melanomas and gliomas - A method of potentiating the efficacy of an antineoplastic agent such as temozolomide, comprises the administration of an antifolate agent as defined herein. Also disclosed are compositions, including pharmaceutical compositions, comprising the antineoplastic agent and an antifolate agent, and the use of such compounds and compositions thereof to treat a variety of cancers, such as melanoma. Unit dosage forms and kits are also contemplated and disclosed. | 2009-10-29 |
20090270398 | Compounds, Compositions and Methods Comprising Pyridazine Derivatives - The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or encompassed by formula I) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease. | 2009-10-29 |
20090270399 | NOVEL PYRIDAZINE DERIVATIVES AND MEDICINES CONTAINING THE SAME AS EFFECTIVE INGREDIENTS - This invention relates to pyridazine derivatives represented by the formula (1): | 2009-10-29 |
20090270400 | PAINKILLING ASSOCIATION COMPRISING A DIHYDROIMIDAZOPYRAZINE DERIVATIVE - The invention relates to a product comprising (1R)-1-[(({2R)-2-amino-3-[(8S)-8-(cyclohexylmethyl) -2-phenyl-5,6-dihydroimidazo [1,2-a]pyrazin-7(8H)-yl]-3-oxopropyl}dithio)methyl]-2-[(8S)-8-(cyclohexylmethyl) -2-phenyl-5,6-dihydrolmidazo[1,2-a]pyrazin-7(8H)-yl]-2-oxoethylamine in association with an analgesic agent selected from morphine, the similar or a morphine derivative, sodium channel inhibitors, non-steroidal antiflammatory agents (AINS), glutamatergic system inhibitors, tricycle antidepressants and gabaergic derivatives for simultaneous therapeutic use which is separated or out over the time for pain treatment or prevention. | 2009-10-29 |
20090270401 | USE OF A DIHYDROIMIDAZOPYRAZOINE DERIVATIVE FOR TREATING OR PREVENTING PAIN - The invention relates to the use of (1R)-1-[({(2R)-2-amino-3-[(8S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazine-7(8H)-yl]-3-oxopropyl}dithio)methyl]-2-[(8S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazine-7(8H)-yl]-2-oxoethylamine or an pharmaceutically acceptable salt thereof for preparing a drug for preventing or treating pain. | 2009-10-29 |
20090270402 | Novel triazolopyridazines - The present invention is directed to novel compounds of formula (I) | 2009-10-29 |
20090270403 | NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINYL DERIVATIVE AND ITS MEDICAL USE - This invention relates to a novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivative and its use in the manufacture of pharmaceutical compositions. The compound of the invention is found to be a cholinergic ligand at the nicotinic acetylcholine receptors. | 2009-10-29 |
20090270404 | OXYMETHYLENE ARYL COMPOUNDS AND USES THEREOF - Use of oxymethylene aryl GPR119 agonists and DPP IV inhibitors for the treatment of diabetic diseases, including Type II diabetes and other diseases associated with poor glycemic control are provided. | 2009-10-29 |
20090270405 | QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders. | 2009-10-29 |
20090270407 | FUNGICIDAL ISOXAZOLIDINES - Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, | 2009-10-29 |
20090270408 | AMIDE DERIVATIVES AS POSITIVE ALLOSTERIC MODULATORS AND METHODS OF USE THEREOF - The invention relates to novel amide derivatives that are PAMs of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions. | 2009-10-29 |
20090270409 | COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119. | 2009-10-29 |
20090270410 | BENZAZOLE ANALOGUES AND USES THEREOF - The present invention relates to compounds of the general formulas (I), (Ia) and (II) and salts and physiologically functional derivatives thereof, | 2009-10-29 |
20090270411 | PHENANTHRIDINE DERIVATIVES AS BRADYKININ ANTAGONISTS - The present invention relates to new phenanthridine derivatives of formula (I), wherein the variables are as defined in the specification, to processes for producing the same, to pharmacological compositions containing the same and to their use in therapy or prevention of painful and inflammatory processes. | 2009-10-29 |
20090270412 | PYRIDO[3,4-B]INDOLES AND METHODS OF USE - This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 2009-10-29 |
20090270413 | DI-T-BUTYLPHENYL PIPERAZINES AS CALCIUM CHANNEL BLOCKERS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity are disclosed. Specifically, a series of compounds containing di-t-butyl phenyl piperazine derivatives of the general formula (1). | 2009-10-29 |
20090270414 | 2,3,4,9- TETRAHYDRO-1H-CARBAZOLE DERIVATIVES AS CRTH2 RECEPTOR ANTAGONISTS - The invention relates to novel tetrahydro-1H-carbazole derivatives 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 methods of treatment comprising administration of said compounds to patients. | 2009-10-29 |
20090270415 | COMPOUNDS THAT INHIBIT PROTEASE CATHEPSIN S AND HCV REPLICATION - The present invention is directed to compounds that have the dual property of acting as cathepsin S inhibitors and of inhibiting HCV replication. Such compounds are therefore useful in treating disease states that include hepatitis C, Alzheimer's disease, and autoimmune disorders. The present invention is also directed to pharmaceutical compositions containing these compounds, and processes for preparing the compounds. | 2009-10-29 |
20090270416 | N-OXIDES OF DIARYLUREA DERIVATIVES AND THEIR USE AS Chk1 INHIBITORS FOR THE TREATMENT OF CANCER - The invention provides a Chk-1 kinase inhibiting compound of the formula (I) or a salt, solvate or tautomer thereof, wherein: G is CH | 2009-10-29 |
20090270417 | Organic Compounds - Novel 3,4-di-, 3,3,4-di-, 3,4,4,-tri- and 3,3,4,4-tetra-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula (I) wherein the substituents are as described in the specification. | 2009-10-29 |
20090270418 | PYRAZOLE PYRAZINE AMINE COMPOUNDS AS KINASE INHIBITORS, COMPOSITIONS THEREOF AND METHODS OF TREATMENT THEREWITH - Provided herein are Pyrazole Pyrazine Amine Compounds having the following structure: | 2009-10-29 |
20090270419 | COMBINATIONS OF CLASS-I SPECIFIC HISTONE DEACETYLASE INHIBITORS WITH PROTEASOME INHIBITORS - The present invention is concerned with combinations of a proteasome inhibitor and a class-I specific histone deacetylase inhibitor for inhibiting the growth of tumor cells, useful in the treatment of cancer. | 2009-10-29 |
20090270420 | METHODS FOR INHIBITING CARDIAC PAI-1 - The invention relates to methods of inhibiting cardiac PAI-1 by administering a PAI-1 antagonist. | 2009-10-29 |
20090270421 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having K | 2009-10-29 |
20090270422 | GPR119 receptor agonists in methods of increasing bone mass and of treating osteoporosis and other conditions characterized by low bone mass, and combination therapy relating thereto - The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. The present invention further relates to the use of a GPR119 receptor agonist in combination with a dipeptidyl peptidase IV (DPP-IV) inhibitor for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. A GPR119 receptor agonist and the combination of a GPR119 receptor agonist and a DPP-IV inhibitor promote bone formation in an individual. | 2009-10-29 |
20090270423 | ANTIBACTERIAL SMALL MOLECULES AND METHODS FOR THEIR SYNTHESIS - The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. | 2009-10-29 |
20090270424 | Crystalline N-(4-(4-aminothieno[2,3-d]pyrimidin-5-yl)phenyl)-N'-(2-fluoro-5-(trifluor- omethyl)phenyl)urea hydrochloride - A crystalline N-(4-(4-aminothieno[2,3-d]pyrimidin-5-yl)phenyl)-N′-[2-fluoro-5-(trifluoromethyl)phenyl)urea hydrochloride, ways to make it, compositions comprising it, and methods of treatment using it are disclosed. | 2009-10-29 |
20090270425 | 3-(DIHYDRO-1H-PYRAZOLO[4,3-D]PYRIMIDIN-5-YL)-4-PROPOXYBENZENESULFONAMIDE DERIVATIVES AND METHODS OF USE - This invention relates to novel 3-(dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxybenzenesulfonamide compounds, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of cyclic guanosine 3′,5′-monophosphate specific phosphodiesterase (cGMP-specific PDE), in particular PDE5. | 2009-10-29 |
20090270426 | P13 Kinase Antagonists - The present invention provides novel PI3-Kinase antagonists and methods of use thereof. | 2009-10-29 |
20090270427 | PURINE DERIVATIVES - The present invention relates to compounds of formula 1 | 2009-10-29 |
20090270428 | CYCLOPROPANECARBOXYLATE ESTERS OF ACYCLOVIR - The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, methods of using the same, processes for preparing the same, and intermediates thereof. | 2009-10-29 |
20090270429 | ANTIVIRAL FORMULATION - A topical antiviral composition comprising acyclovir, penciclovir and/or omaciclovir in a glucocorticoid-free pharmaceutical carrier comprising 15 to 25 weight % propylene glycol and 10 to 25 weight % isopropyl C | 2009-10-29 |
20090270430 | Pyridopyrimidinone Inhibitors of Pl3Kalpha - The invention is directed to Compounds of Formula I: | 2009-10-29 |
20090270431 | Cyclopentenol Nucleoside Compounds Intermediates for their Synthesis and Methods of Treating Viral Infections - The present invention relates to compounds according to the structure (I), Where B is formula (Ia), formula (Ib) or formula (Ic); A is H, OR | 2009-10-29 |
20090270432 | 7-[2-[4-(6-FLUORO-3-METHYL-1,2-BENZISOXAZOL-5-YL)-1-PIPERAZINYL]ETHYL]-2-(- 1-PROPYNYL)-7H-PYRAZOLO-[4,3-e]-[1,2,4]-TRIAZOLO-[1,5-c]-PYRIMIDIN-5-AMINE - The compound having the structural formula I | 2009-10-29 |
20090270433 | 2,3-DIHYDRO-IMINOISOINDOLE DERIVATIVES - A compound represented by the following general formula (1), or a salt thereof has serine protease inhibiting activity, and particularly excellent inhibiting activity against clotting factor VIIa. This compound or a salt thereof is useful as therapeutic and/or prophylactic agents for diseases associated with thrombus formation. | 2009-10-29 |
20090270434 | AZACYCLOALKANE DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis. | 2009-10-29 |
20090270435 | Spiroketone Acetyl-CoA Carboxylase Inhibitors - The invention provides compounds of Formula (1) or a pharmaceutically acceptable salt of said compound, wherein R | 2009-10-29 |
20090270436 | SPIROCHROMANON DERIVATIVES - The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-b]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3: R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a machine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases. | 2009-10-29 |
20090270437 | Use of Buprenorphine or N-Alkylated Derivatives Thereof for Wound Healing - This invention relates to opioid compounds such as burenorphine or N-alkylated derivatives thereof for wound healing. | 2009-10-29 |
20090270438 | Novel compositions and formulations - There is provided according to the invention a non-pressurised pharmaceutical liquid solution spray composition comprising: (i) buprenorphine; and a solvent comprising ethanol which composition is substantially free of chloride. There is also provided according to the invention a non-pressurised pharmaceutical liquid solution spray formulation comprising: (i) buprenorphine; (ii) a solvent comprising ethanol; and (iii) one or more antioxidants each of a molar ratio of antioxidant:buprenorphine between 0.2:1 and 25:1. | 2009-10-29 |