02nd week of 2009 patent applcation highlights part 48 |
Patent application number | Title | Published |
20090012011 | Novel Compounds - This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain substituted pyrrolidines, according to Formula I | 2009-01-08 |
20090012012 | Intratracheal administration of endothelin-suppressing agents for the treatment of respiratory disorders - The subject invention is directed to the treatment of respiratory disorders by intratracheal administration of an effective amount of an agent that suppresses the activity of endothelin. Such agents may take the form of: 1) an endothelin-converting enzyme (ECE) inhibitor such as phosphoramidon, or 2) an endothelin receptor antagonist such as bosentan, tezosentan, sitaxsentan, atrasentan, darusentan, clazosentan, or BQ-123. Respiratory disorders include emphysema, asthma, bronchitis, bronchiectasis, pneumonia, adult respiratory distress syndrome, neonatal respiratory distress syndrome, bronchopulmonary dysplasia, interstitial fibrosis, cystic fibrosis, persistent pulmonary hypertension of the newborn, and neoplasia. The treatment is intended for a variety of mammals, such as premature neonates to adult humans. | 2009-01-08 |
20090012013 | Steroid modified solatrioses - The invention pertains to steroid modified solatrioses and the synthesis thereof as well as to intermediate compounds useful for the synthesis of the steroid modified solatrioses. | 2009-01-08 |
20090012014 | Compound, Composition and a Process Thereof - The present invention provides a novel steroidal glycoside for management of rheumatic and inflammatory disease conditions. In addition, the present invention also provides a process for preparation of steroidal glycoside from plant fenugreek. Further, the invention also provides a pharmaceutical composition of the steroidal glycoside for management of rheumatic disease conditions and its associated disorders. | 2009-01-08 |
20090012015 | LARGE DOSE RIBAVRIN FORMULATONS - The present invention is related to pharmaceutical dosage forms of ribavirin which are designed to increase patient compliance to a ribavirin therapy. Examples of such dosage forms include 400 mg to 600 mg tablets. These dosage forms are bioequivalent to multiple doses of tablets containing small amounts of ribavirin. | 2009-01-08 |
20090012016 | Short Interfering Rna and Micro-Rna Compounds and Methods of Designing, Making, and Using the Same - Methods of identifying, designing and synthesizing uniquely targeting siRNA nucleotide sequences for a target mRNA sequence of a target species are disclosed. Methods of identifying, designing and synthesizing miRNA nucleotide sequences that does not function as a siRNA nucleotide sequence for mRNA of a target species are disclosed. Method of inhibiting expression of a target mRNA molecule are disclosed sequence. siRNA molecules including uniquely targeting siRNA molecules and RISCs comprising the same are disclosed. miRNA molecules that do not function as siRNA nucleotide sequences for mRNA of a target species are disclosed. | 2009-01-08 |
20090012017 | Polypeptide Complex that Regulates Cell Cycle and Anergy - An active ubiquitin E3 ligase, GRAIL, is crucial in the induction of anergy in cells of the immune system, and in the regulation of cellular proliferation. GRAIL is shown to associate with, and be regulated by Otubain isoforms, including OTUBAIN-1 (DOG, the Destabilizer of GRAIL) and an alternative reading frame splice variant of OTUBAIN-1 (SOG, the Stabilizer of GRAIL). These proteins play opposing roles in the regulation of GRAIL auto-ubiquitination and consequently on its ability to induce anergy and regulate cellular proliferation. DOG serves as an adaptor protein, recruiting the DUB USP8. One major substrate for USP8 is the Ras exchange factor Ras-GRF1, and this protein can be found in a complex with USP8 and GRAIL, which complex is ubiquitinated by GRAIL. | 2009-01-08 |
20090012018 | Inhibition of pancretic cancer cell growth - The present invention relates to compositions and methods for inhibition of signal transduction pathways in cancer cells. In particular, the present invention provides methods and compositions comprising Wnt and Hedgehog pathway inhibitors for reducing proliferation of adenocarcinoma cells. | 2009-01-08 |
20090012019 | Methods and Compositions Related to TR4 - Disclosed are compositions and methods related to TR4 and aging. | 2009-01-08 |
20090012020 | Inhibiting formation of atherosclerotic lesions - The invention features a method of inhibiting formation of atherosclerotic lesions by administering to a mammal, e.g., a human patient who has been identified as suffering from or at risk of developing atherosclerosis, a compound that reduces expression or activity of AFABP. | 2009-01-08 |
20090012021 | Delivery of Sirna by Neutral Lipid Compositions - The present invention relates to the fields of molecular biology and drug delivery. In certain embodiments, the present invention provides methods for the delivery of a siNA (e.g., a siRNA) to a cell via a neutral (non-charged) liposome. These methods may be used to treat a disease, such as cancer. | 2009-01-08 |
20090012022 | Hybrid Interfering Rna - The invention relates to a hybrid interfering RNA molecule comprising a duplex RNA and a single stranded DNA molecule and its use in the ablation of mRNA and in polymerase chain reactions. | 2009-01-08 |
20090012023 | DECOY-OLIGNUCLEOTIDE INHIBITION OF CD40-EXPRESSION - The present invention relates to decoy oligonucleotides with the nucleic acid sequence according to SEQ ID NO: 1 to 36 and their use as pharmaceutical agents. | 2009-01-08 |
20090012024 | Stem Cell Markers - We disclose gene markers of stem cells, typically prostate stem cells, and in particular cancer stem cells, for example prostate cancer stem cells; therapeutic agents and diagnostic assays based on said stem cell genes; and including screening assays to identify therapeutic agents. | 2009-01-08 |
20090012025 | Methods and Compositions for Treatment of Sepsis - Methods of treatment of sepsis are disclosed. These methods comprise administering to a subject a composition comprising at least one siRNA directed against at least one gene encoding a pro-apoptotic polypeptide. The pro-apoptotic polypeptide, in some aspects, can be other than Fas or caspase-8. In some embodiments, an siRNA can be directed against a pro-apoptotic component of the mitochondrial pathway, such as a pro-apoptotic bcl-2 protein. In some aspects, an siRNA can be directed against a BH3-only bcl-2 protein, while in other aspects, siRNAs can be directed against multi BH domain Bcl-2 family members such as bax and bak. In some embodiments, an siRNA can be directed against a death receptor pathway molecule such as FADD. In various configurations, a composition can also comprise a cationic lipid such as DOTAP, or nanoparticles comprising a cyclodextrin-containing polycation and a polymer such as a poly(ethylene glycol). | 2009-01-08 |
20090012026 | Association Between the Tdoa Gene and Osteoarthritis - The present invention arises from the identification of an association between the TDOA gene and osteoarthritis (OA). It therefore relates to diagnostic techniques for determining a patient's susceptibility to develop OA by detecting all or part of the TDOA gene, its precursors or products (mRNA, cDNA, genomic DNA, or protein). In particular, the invention relates to methods and materials for analysing allelic variation in the TDOA gene, and to the use of TDOA polymorphisms in the identification of an individuals' risk to develop OA. The TDOA protein has been found to bind to α-paxillin, a protein involved in integrin signal transduction which itself is a process with strong links to OA. The invention is thus also directed to methods for identifying modulators of OA, which modulate the TDOA gene or interfere with TDOA:α-paxillin binding. | 2009-01-08 |
20090012027 | BIODEGRADABLE POLYPHOSPHORAMIDATES FOR CONTROLLED RELEASE OF BIOACTIVE SUBSTANCES - The present invention is directed to a series of new polycationic biodegradable polyphosphoramidates. Process for making the polymers, compositions containing these polymers and bioactive ligands to enhance the cellular uptake ad intracellular trafficking, articles and methods for delivery of drugs and genes using these polymers are described. A gene delivery system based on these polymers is prepared by complex coacervation of nucleic acid (DNA or RNA) with polymers. Targeting ligands and molecules that could facilitate gene transfer can be conjugated to polymers to achieve selective and enhanced gene delivery. The current invention also provides a complex composition with buffering capacity. | 2009-01-08 |
20090012028 | Polyglutamic acids functionalized by cationic groups and hydrophobic groups and applications thereof, in particular therapeutic applications thereof - The present invention relates to novel biodegradable materials based on modified polyamino acids that are useful in particular in the vectorization of active principle(s) (APs). The invention is also directed to novel pharmaceutical, cosmetic, health-food or plant-protection compositions based on these polyamino acids. | 2009-01-08 |
20090012029 | Cyst Nematode Resistant Transgenic Plants - Compositions and methods for providing cyst nematode resistance are provided. One aspect provides transgenic plants or cells comprising an inhibitory nucleic acid specific for one or more cyst nematode esophageal gland cell polypeptides. Other aspects provide transgenic plants or cells resistant to at least two different cyst nematode species. | 2009-01-08 |
20090012030 | RNAi-MEDIATED INHIBITIN OF HTRA1 FOR TREATMENT OF MACULAR DEGENERATION - RNA interference is provided for inhibition of HTRA1 mRNA expression for treating patients with an HTRA1-mediated ocular disorder. In particular, methods are provided for treating age-related macular degeneration (AMD) and using interfering RNA molecules that attenuate expression of HTRA1 in patients having AMD or at risk of developing AMD. | 2009-01-08 |
20090012031 | EZH2 Cancer Markers - The present invention relates to therapeutic targets for cancer. In particular, the present invention relates to small molecules and nucleic acids that target EZH2 expression in prostate cancer. | 2009-01-08 |
20090012032 | GENES AND POLYPEPTIDES RELATING TO HUMAN COLON CANCERS - The present application provides novel human genes RNF43 whose expression is markedly elevated in colorectal cancers, as well as CXADRL1 and GCUD1 whose expression is markedly elevated in gastric cancers compared to corresponding non-cancerous tissues. The genes and polypeptides encoded by the genes can be used, for example, in the diagnosis of a cell proliferative disease, and as target molecules for developing drugs against the disease. | 2009-01-08 |
20090012033 | Delivery of Biologically Active Materials Using Core-Shell Tecto(Dendritic Polymers) - The present invention concerns core-shell tecto (dendritic polymers) that are associated with biologically active materials (such as nucleic acids for use for RNAi and in transfection). Also included are formulations for their use. The constructs are useful for the delivery of drugs to an animal or plant and may be in vivo, in vitro or ex vivo. | 2009-01-08 |
20090012034 | Non-Nucleoside reverse transcriptase inhibitors - Compounds of formula I, wherein R | 2009-01-08 |
20090012035 | DENDRIMER CONJUGATES OF AGONISTS AND ANTAGONISTS OF THE GPCR SUPERFAMILY - Disclosed are conjugates comprising a dendrimer and a ligand, which is a functionalized congener of an agonist or antagonist of a receptor of the G-protein coupled receptor (GPCR) superfamily, for example, wherein the functionalized congener is an A | 2009-01-08 |
20090012036 | Stable S-adenosyl-L-methionine - Stable compositions of defined non-racemic diastereomeric ratios of S-adenosyl-L-methionine, methods for their synthesis and methods for their uses are described. The compositions according to the invention are very stable and are valuable for use as active constituents in pharmaceutical compositions. | 2009-01-08 |
20090012037 | Antiviral Compounds - The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds. | 2009-01-08 |
20090012038 | Methods for microbial biofilm destruction and interference with microbial cellular physiology - The formation and maintenance of microbial biofilms is shown to be dependent on signaling pathways mediated by cyclic di-GMP. In the absence of such signaling, microbes detach from a biofilm, and thereby become more readily treatable with conventional antibiotics. Chemical or biological means that interfere with cyclic-di-GMP signaling induce biofilm dissolution, providing for a new class of antibiotics. In one embodiment of the invention, the biofilm inhibitor is an analog of cyclic-di-GMP, which competitively or non-competitively blocks signaling. In another embodiment of the invention, the biofilm inhibitor is a genetic sequence that interferes with cyclic-di-GMP synthesis or signaling. | 2009-01-08 |
20090012039 | Use of methylcobalamin nasal spray to treat disorders - A method of treating a disorder by nasally administering methylcobalamin, with or without folinic acid. The disorders addressed are: a) attention deficit hyperactivity disorder (ADHD); b) anxiety, depression, stress and chronic stress; c) socialization problems, mood problems, behavior problems, memory problems; d) dislexia, depth perception problems, color viewing problems, visual and auditory processing problems, light modulation problems, night vision problems; e) speech problems such as finding words, apraxia, and articulation problems, sleep regulation problems, eye or muscle movement problems; and f) chronic fatigue problems, digestion problems, sensitivity to chemicals, viral infection, inflammatory conditions such as rheumatoid arthritis, sciatica, and fibromyalgia, asthma, irritable bowel, colitis, tinnitus, migraines, nail biting, autoimmune problems. In some embodiments, the disorders that are particularly addressed are ADHD, anxiety, stress and chronic stress, and irritable bowel. | 2009-01-08 |
20090012040 | BIOCOMPATIBLE POLYMERS, PROCESS FOR THEIR PREPARATION AND COMPOSITIONS CONTAINING THEM - A process for treating fibroses including administering a therapeutically effective amount of a pharmaceutical composition which includes at least one biocompatible polymer of the following general formula (I): A | 2009-01-08 |
20090012041 | Use of cyclodextrin for treatment and prevention of bronchial inflammatory diseases - The invention provides the use of a cyclodextrin compound for the manufacturing of a medicament for the treatment or prevention of bronchial inflammatory diseases, particularly for asthma. | 2009-01-08 |
20090012042 | Hydroxypropyl-Sulfobutyl-Beta-Cyclodextrin, the Preparation Method, the Analytical Method, and the Pharmacutical Application Thereof - Hydroxypropyl-sulfobutyl-&bgr;-cyclodextrin, the preparation method, analytical method, and the pharmaceutical application thereof. The hydroxypropyl-sulfobutyl-&bgr;-cyclodextrin is a derivate of cyclodextrin which is substituted by hydroxypropyl group and sulfobutyl group: n-(2,3,6-O-2-hydroxypropyl)-m-(2,3,6-O-sulfobutyl)-&bgr;-cyclodextrin. The number of substituent groups per mole cyclodextrin is n hydroxypropyl groups and m sulfobutyl groups. “n” represents the average substituent degree of hydroxypropyl groups; “m” represents the average substituent degree of sulfobutyl groups; “n+m=z” is the gross average substituent degree, in which n is a random integer chosen from 1, 2, 3, 4, 5, 6, 7, 8, 9; m is a random integer chosen from 1, 2, 3, 4, 5, 6, 7, 8, 9; and the gross average substituent degree z is a random integer chosen from 2, 3, 4, 5, 6, 7, 8, 9, 10. The present invention shows low haemolysis and low toxicity. | 2009-01-08 |
20090012043 | INHIBITORS OF POLYSIALIC ACID DE-N-ACETYLASE AND METHODS FOR USING THE SAME - The invention relates to inhibitors of polysialic (PSA) de-N-acetylase, methods of their production and use. The methods involve use of a PSA de-N-acetylase inhibitor for modifying the growth of cells, such as inhibiting the growth of cancer cells. The compositions include an inhibitor of a PSA de-N-acetylase, such as N-substituted derivatives of the amino sugars hexosamine and neuraminic acid, as well as conjugates and aggregates. Also provided are pharmaceutical compositions that include a PSA de-N-acetylase inhibitor of the invention. Kits containing one or more inhibitor compositions of the invention, as well as methods of preparing the compositions also are provided. | 2009-01-08 |
20090012044 | Novel Hiv Protease Inhibitors - The present invention provides novel HIV protease inhibitors containing substituted borane, carborane or metallacarborane clusters with 6 to 12 boron atoms in each cluster. The charge of each borane, carborane or metallacarborane cluster is 0, −1 or −2. The number of borane, carborane or metallacarborane clusters in the inhibitor molecule is 1 to 9, and the carborane clusters in metallacarborane inhibitors are coordinated to transition metal atom, selected from the group containing cobalt, iron, nickel and ruthenium. In the cluster, heteroatoms can be present, such as nitrogen, phosphorus, silicon, germanium, tin and sulphur. The present invention covers pharmaceutical compositions containing these inhibitors and their use, both in vitro and in vivo. They are characterized by high effectiveness and stability. | 2009-01-08 |
20090012045 | Methods of Treating Cell Proliferative Disorders - The present disclosure provides methods for the treatment of cell proliferative disorders by administration of a RET kinase inhibitor. Cell proliferative disorders treatable by the methods include, thyroid tumors. | 2009-01-08 |
20090012046 | Methods of Treating Mutated Hiv - Nucleotide-competing reverse transcriptase inhibitors (NcRTI) bind to the active site of HIV reverse transcriptase (RT) in competition with the next incoming nucleotide. To further investigate the impact of RT inhibitor resistance mutations on the activity of NcRTIs, the susceptibility of >6000 recent clinical isolates for a prototype compound, NcRTI-1, was determined. Over 80% of the profiled clinical isolates remained susceptible for NcRTI-1 (FC<4). No cross-resistance was observed between NcRTI-1 and currently used RT inhibitors, apart from limited cross-resistance with 3TC/FTC. | 2009-01-08 |
20090012047 | Crystalline forms of ibandronate sodium - Provided are crystalline forms of ibandronate sodium, as well as processes for the preparation thereof. | 2009-01-08 |
20090012048 | Methods for diagnosing and treating a mycobacterium avium subspecies paratuberculosis infection - The present invention relates to | 2009-01-08 |
20090012049 | Use of an Unsaponifiable Extract of Plant Pulp in the Treatment of Skin Ageing. - The field of the present invention relates to the use of an unsaponifiable extract of plant pulp in the preparation of a cosmetic, pharmaceutical or nutraceutical product intended for treating and/or preventing skin disorders associated with ageing. | 2009-01-08 |
20090012050 | Quinone Derivative 2,3-Dimethoxy-5-Methyl-6-(10-Hydroxydecyl)-1,4-Benzoquinone for the Treatment of Muscular Dystrophies - Use of idebenone for the preparation of a medicament for the treating of a muscular dystrophy in particular for treating and/or preventing weakness and/or loss of skeletal muscle tissue and/or cardiomyopathy associated with a muscular dystrophy. | 2009-01-08 |
20090012051 | EXTERNAL PREPARATION - The present invention provides an external preparation which comprises 7-[2-(3,5-dichloro-4-pyridyl)-1-oxoethyl]-4-methoxy-spiro[1,3-benzodioxol-2,1′-cyclopentane] represented by Formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient, comprising 0.5 to 15% by mass of a solvent component in which the solubility of the active ingredient is 4 mg/mL or more, and the like. | 2009-01-08 |
20090012052 | METHOD FOR TREATING ER+ BREAST CANCER - A method for selecting a female breast cancer patient for AT | 2009-01-08 |
20090012053 | Use of LXR agonists for the treatment of osteoarthritis - Disclosed herein are methods of preventing and treating osteoarthritis through the use of LXR agonists. | 2009-01-08 |
20090012054 | Cephem Compounds and Use as Antimicrobial Agents - The present invention provides a compound of the formula [I]: wherein R1 is lower alkyl, etc. and R2 is hydrogen, etc., or R1 and R2 are bonded together to form lower alkylene; R3 is a group represented by wherein R6 and R7 are independently optionally protected amino, etc.; m and n are independently an integer of 0 to 6; R8 and R9 are independently optionally protected amino, etc., and q and r are independently an integer of 0 to 6, or R8 and R9, together with the adjacent alkylene(s) and the nitrogen atom, form saturated nitrogen-containing heterocycle optionally having substituent(s); R4 is lower alkyl, etc.; and R5 is amino, etc., or a pharmaceutically acceptable salt thereof. | 2009-01-08 |
20090012055 | Organic compounds - Novel substituted piperidines of the general formulae (I) and (II) | 2009-01-08 |
20090012056 | Quinoline Compounds Capable of Binding the Cb2 and/or the 5-Ht6 Receptor - The present invention relates to novel quinoline derivatives such as compounds of the formula (I) which possess antagonist potency for the 5-HT | 2009-01-08 |
20090012057 | Cardiovascular Compounds Comprising Nitric Oxide Enhancing Groups, Compositions and Methods of Use - The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one nitric oxide enhancing group, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia. The cardiovascular compounds are angiotensin II antagonists, aldosterone antagonists, endothelin antagonists, hydralazine compounds, neutral endopeptidase inhibitors and renin inhibitors. The nitric oxide enhancing groups are nitroxides and/or heterocyclic nitric oxide donors. | 2009-01-08 |
20090012058 | Prophylactic or Therapeutic Agents For Allergic Ophthalmic Diseases or Allergic Nasal Diseases, Comprising Tricyclic Triazolobenzazepine Derivative - The present invention provides a pharmaceutical composition for use in the prophylaxis or treatment of allergic ophthalmic diseases or allergic nasal diseases, which comprises 7,8-dimethoxy-4(5H),10-dioxo-1H-1,2,3-triazolo[4,5-c][1]benzazepine, 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H),10-dioxo-2H-1,2,3-triazolo[4,5-c][1]benzazepine or a pharmaceutically acceptable salt thereof. The pharmaceutical composition according to the present invention has few side effects, exerts strong prophylactic and therapeutic effects in the late phase exhibiting pharmaceutical resistance to conventional instillations, and can be used appropriately for topical applications. | 2009-01-08 |
20090012059 | DIPEPTIDYL PEPTIDASE INHIBITORS - Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: | 2009-01-08 |
20090012060 | Antitumor Agent - The present invention provides an antitumor agent and the like, which comprises as an active ingredient, a pyrimidine derivative represented by Formula (I): | 2009-01-08 |
20090012061 | A Method of Treating Cancer - The present invention relates to a method of treating cellular proliferative diseases, in particular cancer, which comprises administering a modulator of the activity of the mitotic kinesin KSP, wherein the activity of the KSP modulator is dependent on the presence of microtubules. It is believed that the KSP modulators utilized in the instant method bind to the KSP protein in a previously unreported manner, since the compounds do not bind competitively with respect to either microtubules or ATP, the substrates of KSP. The modulators useful in the instant methods are furthermore not active against the non-microtubule stimulated activity of KSP. Cellular proliferative diseases that may be treated using the method disclosed herein are, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation. | 2009-01-08 |
20090012062 | Novel Substituted Pyrazinone Derivatives for Use in Mch-1 Mediated Diseases - The present invention concerns aryl and heteroaryl substituted pyrazinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I) | 2009-01-08 |
20090012063 | Novel imidazole derivatives - The invention is concerned with novel imidazole derivatives of formula (I), | 2009-01-08 |
20090012064 | Compositions controlling pH range of release and/or release rate - The present invention provides a composition controlling a pH range of release and/or a release rate, which contains (i) a thienotriazolodiazepine compound of the formula (I) | 2009-01-08 |
20090012065 | Therapeutic applications of pro-apoptotic benzodiazepines - Benzodiazepine compounds, and methods for using those compounds are provided. Some of the benzodiazepine compounds include 1,4-benzodiazepine-2-one and 1,4-benzodiazepine-2,5-dione compounds of the following structures: | 2009-01-08 |
20090012066 | Method of Use of Deacetylase Inhibitors - The present invention provides methods of treating and/or preventing pathologic cardiac hypertrophy and heart failure comprising administering hydroxamate compounds which are deacetylase inhibitors. | 2009-01-08 |
20090012067 | Modulation of Hypothalamic Atp-Sensitive Potassium Channels - Provided are methods of increasing K | 2009-01-08 |
20090012068 | Condensed Imidazole Derivatives as Aldosterone Synthase Inhibitors - The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R | 2009-01-08 |
20090012069 | Novel Antidiabetic Compounds - Disclosed are novel compounds of general formula (I) where the symbols are as defined in the specification, their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The compounds are useful in the treatment of diabetes and related diseases. | 2009-01-08 |
20090012070 | PESTICIDAL HETEROCYCLES - It has now been found that certain novel heterocyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R | 2009-01-08 |
20090012071 | 4-SUBSTITUTED-1H-ISOTHIAZOLO[5,4-B][1,4]OXAZINO[2,3,4-IJ]QUINOLINE-7,8(2H,9H)-DIONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS - The present invention provides compounds of the formula that possess antimicrobial activity. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity. Particular compounds provided herein are also potent and/or selective inhibitors of microbial DNA synthesis and reproduction. The invention provides anti-microbial compositions, including pharmaceutical compositions, containing a compound of the invention and one or more or more carriers. The invention provides pharmaceutical compositions containing a 4-substituted- | 2009-01-08 |
20090012072 | FLUOROQUINOLONE COMPOSITIONS - The invention relates to pharmaceutical compositions comprising (i) a fluoroquinolone, (ii) a salt formed between a carboxylate anion and a divalent metal cation, (iii) a liquid comprising an organic solvent selected from the group consisting of glycerol, propylene glycol, glycerol formal, and (iv) optionally water. The invention further relates to methods of treating or preventing a condition in an animal comprising administering to the animal in need thereof a pharmaceutical composition of the invention. | 2009-01-08 |
20090012073 | N-AROYL CYCLIC AMINES - Disclosed are N-aroyl cyclic amine derivatives having the formula: | 2009-01-08 |
20090012074 | Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to modulation of the Dopamine D3 receptor - The present invention relates to aromatic compounds of the formula I | 2009-01-08 |
20090012075 | Fluorinated Arylamide Derivatives - The present invention relates to a novel class of fluorinated arylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives 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 hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo. | 2009-01-08 |
20090012076 | Tyrosine kinase inhibitors - The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. | 2009-01-08 |
20090012077 | Novel Compound - 827 - The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases, including cathepsins B, K, C, F, H, L, O, S, W and X. Of particular interest are diseases associated with Cathepsin K. | 2009-01-08 |
20090012078 | Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases - Novel fused pyrazine compounds are disclosed that have a formula represented by the following: | 2009-01-08 |
20090012079 | Triazolopyridine Compounds - A compound of formula (Ia): or a pharmaceutically acceptable salt and/or solvate (including hydrate) thereof, or a compound of formula (Ib): or a pharmaceutically acceptable salt and/or solvate (including hydrate) thereof, and the use of a compound of formula (Ia) or (Ib) in the treatment of a TNF-mediated disease, disorder, or condition, or a p38-mediated disease, disorder, or condition, in particular the allergic and non-allergic airway diseases, more particularly obstructive or inflammatory airways diseases, preferably chronic obstructive pulmonary disease. | 2009-01-08 |
20090012080 | Sirtuin modulating compounds - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 2009-01-08 |
20090012081 | Agents for promoting the proliferation or differentiation of stem cells or neural progenitor cells - An agent for promoting the proliferation or differentiation of a stem cell and/or neural progenitor cell, comprising a compound represented by Formula: | 2009-01-08 |
20090012082 | Mediators of Hedgehog Signaling Pathways, Compositions and Uses Related Thereto - The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. | 2009-01-08 |
20090012083 | N-AROYL CYCLIC AMINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS - Disclosed are N-aroyl cyclic amine derivatives having the formula: | 2009-01-08 |
20090012084 | 3-CINNOLINECARBOXAMIDE DERIVATIVES AND THEIR USE FOR TREATING CANCER - The invention relates to chemical compounds of formula (I): | 2009-01-08 |
20090012085 | DOSAGE FORMS AND METHODS OF TREATMENT USING A TYROSINE KINASE INHIBITOR - This invention provides dosage forms of a compound of formula 1, 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, or pharmaceutically acceptable salts or solvates thereof. The invention further provides methods of treating abnormal cell growth in a patient, such as cancers, by administering the dosage forms to the patient. The invention further provides methods of treating an angiogenesis- or VEGF-related ophthalmic disorder in a patient, by administering the dosage form to the patient. | 2009-01-08 |
20090012086 | Use of Non-Peptidic Nk1 Receptor Antagonists for the Production of Apoptosis in Tumor Cells - The invention relates to the use of substance P antagonists and, in particular, the use of non-peptidic NK1 receptor antagonists for the treatment of cancer and, more specifically, human melanoma, neuroblastoma, glioma, human Hodgkin's lymphoma KM-H2, lymphoblastic leukaemia, human rhabdomyosarcoma, human breast carcinoma, human Burkitt's lymphoma, human lung carcinoma, human Ewing's sarcoma, human glioma and human osteosarcoma. | 2009-01-08 |
20090012087 | New Aza-Bicyclohexane Compounds Useful As Inhibitors Of Thrombin - This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production. | 2009-01-08 |
20090012088 | Compounds for the Treatment of Neurodegeneration and Stroke - Compounds and related methods for synthesis, and the use of compounds for the treatment of neurodegenerative diseases are disclosed. Compounds are disclosed in connection with PARG and/or PARP inhibition. Therapeutic applications are relevant for preventing or inhibiting neurological cell death for a variety of neurodegenerative conditions including Parkinson's disease, ischemia, and stroke. Also disclosed is a high-throughput screen for identifying compounds capable of inhibiting PARG and/or PARP. | 2009-01-08 |
20090012089 | Oxazolidinone Compounds and Their Use as Metabotropic Glutamate Receptor Potentiators - The present invention is directed to compounds of Formula I: | 2009-01-08 |
20090012090 | Radiohalogenated Benzamide Derivatives And Their Use In Tumor Diagnosis And Tumor Therapy - This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention. | 2009-01-08 |
20090012091 | Oximide derivatives and their therapeutical application - The present invention relates to a compound represented as the following Formula (I) and a pharmaceutical composition thereof | 2009-01-08 |
20090012092 | Hiv Inhibiting 1,2,4-Triazin-6-One Derivatives - The present invention relates to HIV replication inhibitors of formula | 2009-01-08 |
20090012093 | Receptor Function Regulator - The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like. | 2009-01-08 |
20090012094 | DIARYLAMINE-CONTAINING COMPOUNDS AND COMPOSITIONS, AND THEIR USE AS MODULATORS OF C-KIT RECEPTORS - Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors. | 2009-01-08 |
20090012095 | HUMAN N-TYPE CALCIUM CHANNEL BLOCKERS - This invention features a method for modulating human N-type calcium channel α | 2009-01-08 |
20090012096 | PHARMACEUTICAL COMPOSITION FOR REDUCING THE AREA OF MYOCARDIAL INFARCTION AND ITS USE - This invention relates to a pharmaceutical composition for preventing and curing myocardium ischemia and reducing area of myocardial infarction, its pharmaceutical preparation and applications. The composition includes (a) levocarnitine or its derivatives, and (b) trimetazidine or its medicative salts. The quantity of levocarnitine or its derivatives, and trimetazidine or its medicative salts in the composition is effective amount for treating myocardial ischemia and reducing the area of myocardial infarction. | 2009-01-08 |
20090012097 | Polycyclic 1,2,3,4-Tetrahydro-Isoquinoline Derivatives and Compositions Comprising Them As Ppar Modulators - 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 the Peroxisome Proliferator-Activated Receptor (PPAR) families. | 2009-01-08 |
20090012098 | 5-HT1A RECEPTOR SUBTYPE AGONIST - The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT | 2009-01-08 |
20090012099 | Novel Compounds - Disclosed is a method for use of phenyl sulfone compounds of formula (I) in the treatment of Alzheimer's disease and age related cognitive decline. | 2009-01-08 |
20090012100 | Selective Insecticides Based on Substituted Cyclic Ketoenols and Safeners - The present invention relates to the use of selective insecticidal compositions, characterized in that they comprise an effective amount of an active compound combination comprising
| 2009-01-08 |
20090012101 | Mucarinic Agonists and Methods of Use Thereof - A method of forming analogs of CDD-0304, i.e., tetra(ethyleneglycol) (4-methoxy-1,2,5-thiadiazol-3-yl)[3-(1-methyl-1,2,4,5-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl]ether hydrochloride includes one or more of the following steps: a) replacing the tetrahydropyridine moiety with one of the following heterocyclic rings, including quinuclidine, [2.2.1]-exo-azabicy-cloheptane, [2.2.1]-endo-azabicycloheptane and terahydropyrimidine; b) varying the length of the linking group by replacing the tetra(ethylene) glycol moiety with one of: ethylene glycol, di(ethylene) glycol, penta(ethylene) glycol, or diether diol; and/or, c) replacing the 1,2,5-thiadiazole moiety with an ester isostere. Also, a method for an asymmetric analog CCD-0304 includes replacing at least one moiety with an ester isostere and at least a second moiety with an ammonium isostere. Also, such analogs compounds and their uses are disclosed. | 2009-01-08 |
20090012102 | Imidazo[1,2-C]Pyrimidinylacetic Acid Derivatives - The present invention relates to an imidazo[1,2-c]pyrimidinylacetic acid derivative and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The imidazo[1,2-c]pyrimidinylacetic acid derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis. | 2009-01-08 |
20090012103 | SUBSTITUTED HETEROCYCLIC COMPOUNDS - The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): | 2009-01-08 |
20090012104 | Inhibitors of 5'-Methylthioadenosine Phosphorylase and 5'-Methylthioadenosine/S-Adenosylhomocysteine Nucleosidase - Described are compounds of the general formula (I), VI and (VII). Also described are pharmaceutical compositions comprising the compounds identified. The compounds and pharmaceutical compositions described are inhibitors of 5′-methylthioadenosine/S-adenosylhomocystein nucleosidase (MTAN) and/or 5′-methylthioadenosine phosphorylase (MTAP). Methods of treatment using the compounds and pharmaceutical compositions described are also provided for preventing and/or treating disease states and/or conditions by inhibiting MTAN and/or MTAP in patients. | 2009-01-08 |
20090012105 | Combination of Mtor Inhibitor and Antipolate Compound - Use of a combination of an mTOR inhibitor and an antifolate compound. | 2009-01-08 |
20090012106 | Methods, compositions, and kits for organ protection during systemic anticancer therapy - Methods, compositions, and kits are presented for local tissue protection during systemic administration of anticancer therapeutic agents. | 2009-01-08 |
20090012107 | Antiviral Compounds and Methods of Using Thereof - Disclosed herein are compounds which exhibit antiviral activity against a plurality of viruses belonging to different families such as Bornaviridae, Filoviridae, Paramyxoviridae, Rhabdoviridae, Arenaviridae, Bunyaviridae, Orthomyxoviridae, and Poxviridae. Thus, methods of preventing, inhibiting, or reducing the viral activity of various viruses are provided as well as methods of treating viral infections. | 2009-01-08 |
20090012108 | SALT OF 4-[[4-[[4-(2-CYANOETHENYL)-2,6-DIMETHYLPHENYL]AMINO]-2-PYRIMIDINYL]AMINO]BENZONITRILE - The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethyl-phenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation. | 2009-01-08 |
20090012109 | CYCLOPAMINE ANALOGS - The invention provides novel derivatives of cyclopamine having the following formula: | 2009-01-08 |
20090012110 | MORPHINE COMPOUNDS FOR PHARMACEUTICAL COMPOSITIONS - The invention relates to new morphine compounds of the formula: | 2009-01-08 |