22nd week of 2009 patent applcation highlights part 44 |
Patent application number | Title | Published |
20090137494 | Tumor-activated prodrug compounds and treatment - The compound (W-Z-M) according to the invention comprises a component (M) chosen from the group consisting of markers and therapeutic agents possessing an intracellular active site (A.S.), linked to a ligand (W-Z) comprising an arm (Z) linked to a terminal group (W), characterized in that the linkage between the arm (Z) of the ligand (W-Z) and the component (M) prevents intracellular entry of the compound (W-Z-M) and/or inhibits expression of the marker (M), in that said linkage can be selectively cleaved by factors secreted by target cells so as to permit expression of the marker (M) or entry of the therapeutic agent (M) into said target cells, and in that the terminal group (W) provides for the stability of the compound (W-Z-M) in the serum and circulating blood. | 2009-05-28 |
20090137495 | Organic Compounds and Their Uses - The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases. | 2009-05-28 |
20090137496 | Use of Active Ingredients Containing Hydroxystilbene for Preventing and/or Treating Osteoporosis - The invention relates to the use of a combination of active ingredients containing hydroxystilbene, selected from resveratrol and piceatannol precursors and functional derivatives thereof, in addition to the use of the stereoisomeric forms of said ingredients, in the form of salts or phenol respectively, for producing an agent for the prevention and/or treatment of osteoporosis. | 2009-05-28 |
20090137497 | ACTIVE INGREDIENT COMBINATIONS OF GLUCOSYL GLYCERIDES AND CREATINE AND/OR CREATININE - Active ingredient combinations of one or more glucosyl glycerides and one or more substances selected from creatine, creatinine, creatine phosphate, creatine sulfate, creatine acetate, creatine ascorbate, and creatine derivatives whose carboxyl group is esterified by a mono- or polyfunctional alcohol, and cosmetic preparations comprising these active ingredient combinations. | 2009-05-28 |
20090137498 | SUBSTITUTED BENZENE DERIVATIVES OR SALTS THEREOF - There are provided compounds having an anticoagulant action on the basis of inhibition of activated blood coagulation factor X and being useful as anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism. Effective ingredients are the compounds such as 4′-bromo-2′-[(5-chloro-2-pyridyl)carbamoyl]-6′-β-D-galactopyranosyloxy-1-isopropylpiperidine-4-carboxanilide, 2′-(2-acetamido-2-deoxy-β-D-glucopyranosyloxy)-4′-bromo-6′-[(5-chloro-2-pyridyl)carbamoyl]-1-isopropylpiperidine-4-carboxanilide, etc. or salts thereof. | 2009-05-28 |
20090137499 | BENZYLPHENYL GLUCOPYRANOSIDE DERIVATIVE - The present invention relates to a benzylphenyl glucopyranoside derivative having an excellent inhibitory effect on human SGLT1 and/or SGLT2 activity. There is provided a compound or a pharmacologically acceptable salt thereof represented by the following general formula (I): | 2009-05-28 |
20090137500 | RNA interference mediated inhibition of gene expression using chemically modified short interfering nucleic acid (siNA) - The present invention concerns methods and reagents useful in modulating gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to synthetic chemically modified small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules capable of mediating RNA interference (RNAi) against target nucleic acid sequences. The small nucleic acid molecules are useful in the treatment of any disease or condition that responds to modulation of gene expression or activity in a cell, tissue, or organism. | 2009-05-28 |
20090137501 | Resistance Genes - Genes involved in immune resistance to infection and uses thereof are described. In particular genes which are involved in resistance to HIV infection and in slowing disease progression in infected individuals are described. | 2009-05-28 |
20090137502 | Riproximin, a Novel Type II Ribosome-Inactivating Protein and Uses Thereof - Described is a novel type II ribosome-inactivating protein, riproximin, as well as nucleic acid molecules encoding said protein. Furthermore, therapeutic uses of riproximin are described. | 2009-05-28 |
20090137503 | Pharmacological modulation of telomere length in cancer cells for prevention and treatment of cancer - Acyclic nucleoside analogs such as acyclovir, ganciclovir, penciclovir and the corresponding pro-drugs, i.e., valacyclovir, valganciclovir and famciclovir, respectively have been identified as inhibitors or antagonists of both telomerase (encoded by TERT) and reverse transcriptase encoded by L-1 (LINE-1) RT, and as useful for treating or preventing cancers induced or mediated by the two enzymes. Method of treating or preventing such cancers in patients involves administration of a therapeutically effective amount of a composition having an inhibitor or antagonist of the reverse transcriptases in cells of the patients. The inhibitor or antagonist blocks lengthening of telomeres in telomerase positive and telomerase negative cells. Methods and kits for detecting pathologically proliferating cells expressing TERT and L1RT are also disclosed. | 2009-05-28 |
20090137504 | MICRORNA TARGET SITE BLOCKING OLIGOS AND USES THEREOF - The present invention related to nucleic acids designed to prevent the binding of endogenous or exogenous microRNA and diagnostic and therapeutic uses thereof. | 2009-05-28 |
20090137505 | Method for Predicting and Identifying Target mRnas Controlled By Functional Rnas and Method of Using the Same - It is intended to identify or estimate miRNAs and one or more target genes (target mRNAs) targeted thereby. | 2009-05-28 |
20090137506 | RNA Interference Mediated Inhibition of Cyclic Nucleotide Type 4 Phosphodiesterase (PDE4B) Gene Expression Using Short Interfering Nucleic Acid (siNA) - The invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression and/or activity, including PDE4B1, PDE4B2, and PDE4B3. The invention relates to double stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA), and multifunctional siNA molecules capable of mediating RNA interference (RNAi) against cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression, including cocktails of such small nucleic acid molecules and lipid nanoparticle (LNP) formulations of such small nucleic acid molecules. Such small nucleic acid molecules are useful, for example, in providing compositions to prevent, inhibit, or reduce inflammatory, respiratory, and autoimmune diseases, traits, and conditions, and/or other disease states associated with PDE4B gene expression or activity in a subject or organism. | 2009-05-28 |
20090137507 | RNA INTERFERENCE MEDIATED INHIBITION OF ANGIOPOIETIN GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) - This invention relates to compounds, compositions, and methods useful for modulating Angiopoietin gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of Angiopoietin gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of Angiopoietin genes, such as Angiopoietin-1 (Ang-1), Angiopoietin-2 (Ang-2), Angiopoietin-3 (Ang-3), and Angiopoietin-4 (Ang-4). | 2009-05-28 |
20090137508 | RNA INTERFERENCE MEDIATED INHIBITION OF POLYCOMB GROUP PROTEIN EZH2 GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) - This invention relates to compounds, compositions, and methods useful for modulating polycomb group protein EZH2 gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of polycomb group protein EZH2 gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of polycomb group protein EZH2 genes, such as EZH2. | 2009-05-28 |
20090137509 | RNA INTERFERENCE MEDIATED INHIBITION OF PROLIFERATION CELL NUCLEAR ANTIGEN (PCNA) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) - This invention relates to compounds, compositions, and methods useful for modulating PCNA gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of PCNA gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of PCNA genes. The small nucleic acid molecules are useful in the treatment of cancer or restenosis or other proliferative diseases, disorders, or conditions. | 2009-05-28 |
20090137510 | RNA INTERFERENCE MEDIATED INHIBITION OF NF-KAPPA B/ REL-A GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) - This invention relates to compounds, compositions, and methods useful for modulating NF-kappa B, REL-A, REL-B, REL, NKkappaB1, or NFkappaB2 gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of NF-kappa B, REL-A, REL-B, REL, NKkappaB1, or NFkappaB2 gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of NF-kappa B, REL-A, REL-B, REL, NKkappaB1, or NFkappaB2 genes, such as NF-kappa B and/or REL-A. | 2009-05-28 |
20090137511 | RNA INTERFERENCE MEDIATED INHIBITION OF PLACENTAL GROWTH FACTOR GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) - This invention relates to compounds, compositions, and methods useful for modulating placental growth factor (e.g., PGF-1 or PlGF-1, PGF-2 or PlGF-2, and/or PGF-3 or PlGF-3) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of placental growth factor gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of placental growth factor genes. | 2009-05-28 |
20090137512 | RNA Interference Mediated Inhibition of Cyclin D1 Gene Expression Using Short Interfering Nucleic Acid (siNA) - This invention relates to compounds, compositions, and methods useful for modulating cyclin (e.g., cyclin D1) and/or cyclin dependent kinase (CDK) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of cyclin (e.g., cyclin D1) and/or cyclin dependent kinase (CDK) gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of cyclin (e.g., cyclin D1) and/or cyclin dependent kinase (CDK) genes. | 2009-05-28 |
20090137513 | RNA Interference Mediated Inhibition of Acetyl-CoA-Carboxylase Gene Expression Using Short Interfering Nucleic Acid (siNA) - This invention relates to compounds, compositions, and methods useful for modulating acetyl-CoA carboxylase gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of acetyl-CoA carboxylase gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of acetyl-CoA carboxylase genes. | 2009-05-28 |
20090137514 | METHODS AND COMPOSITIONS FOR SILENCING GENES WITHOUT INDUCING TOXICITY - The present invention provides methods of post-transcriptional gene silencing which involve the use of a first dsRNA having substantial sequence identity to a target nucleic acid and a short, second dsRNA which inhibits dsRNA-mediated toxicity. These methods can be used to prevent or treat a disease or infection by silencing a gene associated with the disease or infection. The invention also provides methods for identifying nucleic acid sequences that modulate a detectable phenotype, including the function of a cell, the expression of a gene, or the biological activity of a target polypeptide. | 2009-05-28 |
20090137516 | COMPOSITIONS AND METHODS OF TREATING DYSLIPIDEMIA - The invention relates to the treatment of subjects for the purpose of reducing serum LDL, VLDL, triglycerides and fatty acids, by administering agents which reduce the activity of the bile acid pathway component SHP. Methods and pharmaceutical preparations comprising such agents are provided. | 2009-05-28 |
20090137517 | SENSITIZING A CELL TO CANCER TREATMENT BY MODULATING THE ACTIVITY OF A NUCLEIC ACID ENCODING RPS27L PROTEIN - The present invention refers to a method of sensitizing a cell to cancer treatment comprising modulating the activity of a nucleic acid which encodes the RPS27L protein by use of an oligonucleotide which is a RNAi agent or an antisense nucleotide molecule. The oligonucleotides of the present invention can be used in combination with at least one cytostatic drug for, e.g., chemotherapy. The present invention further refers to an expression vector comprising an oligonucleotide used in the method of the present invention as well as to a pharmaceutical comprising the oligonucleotides together with at least one chemotherapeutic agent used in the method of the present invention. | 2009-05-28 |
20090137518 | Therapeutic Antiangiogenic Endostatin Compositions - Endostatin compositions capable of inhibiting endothelial cell proliferation, inhibiting angiogenesis and causing tumor regression are described. Specifically, amino acid sequences of endostatin proteins and nucleic acid sequences coding for endostatin proteins are provided. | 2009-05-28 |
20090137519 | SEMI-SOFT C-CLASS IMMUNOSTIMULATORY OLIGONUCLEOTIDES - The invention relates to specific C-Class semi-soft CpG immunostimulatory oligonucleotides that are useful for stimulating an immune response. In particular the oligonucleotides are useful for treating allergy, such as allergic rhinitis and asthma, cancer and infectious disease, such as hepatitis B and hepatitis C. | 2009-05-28 |
20090137520 | A1 ADENOSINE RECEPTOR AGONISTS - Disclosed are novel compounds that are A | 2009-05-28 |
20090137521 | Certain Compounds, Compositions and Methods - The present invention provides certain tetrahydrouridine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of making and using such compounds. | 2009-05-28 |
20090137522 | Pharmaceutical Composition on Basis of Reverse Transcriptase Inhibitor and Meldonium - Novel pharmaceutical compositions which contain one of the reverse transcriptase inhibitors, viz., Zidovudine, Lamivudine or Stavudine in clinically efficacious amount and Meldonium as well as pharmaceutically applicable excipients. It has been proved that inclusion of Meldonium in these pharmaceutical compositions essentially diminishes the cardio- and neuro-toxicity of the reverse transcriptase inhibitor. | 2009-05-28 |
20090137523 | Compositions for External Application, Containing Adenosyl Cobalamin for Improvement of Skin Diseases - The present invention relates to a composition for external application for improving a skin disease (e.g. psoriasis). Said composition contains adenosyl cobalamin (coenzyme B12), opt. in admixture with other cobalamins. Preferable said composition is present in the form of liposomal preparations, which are made of a phospholipid and cholesterol. | 2009-05-28 |
20090137524 | SUBSTITUTED ARYLPYRAZOLES - This invention relates to a combination product comprising a compound of formula I | 2009-05-28 |
20090137525 | Glycosaminoglycan Composition and Method for Treatment and Prevention of Interstitial Cystitis - The invention provides compositions and methods useful for the treatment and/or prevention of interstitial cystitis and/or a related urinaly tract condition in man or in animals. Specifically, provided are compositions specially formulated for direct instillation into the bladder and/or parenteral use in the treatment and/or prevention of interstitial cystitis. Compositions adapted for direct instillation into the bladder and/or for systemic administration are provided comprised of therapeutic amounts of: chondroitin sulfate in combination with hyaluronan (hyaluronic acid) are provided. Compositions adapted for direct instillation into the bladder and/or for systemic administration are also provided comprised of therapeutic amounts of: chondroitin sulfate, hyaluronan (hyaluronic acid) and N-acetyl D-glucosamine. | 2009-05-28 |
20090137526 | Purification Method for Biomaterial - The present disclosure relates to methods for purifying chitin or chitosan, particularly for obtaining medical grade materials suitable for use in biocompatible devices,formulations, or other materials. Chitosan separation and purification methods are taught for obtaining high purity and fractionated bio-compatible medical grade materials. Chemistries and solvent systems are taught for the use in counter current chromatography, liquid/liquid or other microfluidic separation systems. | 2009-05-28 |
20090137527 | Compositions and methods for modulating immune function - The invention relates to methods of modulating immune function, suppressing immune response, treating autoimmune diseases or autoimmune disorders, and treating diseases, sequelae or pathological conditions mediated by an activation of the immune system comprising administering a compound of formula A, a compound of any one of formulae 1-49, a lipoxin compound, or an oxylipin compound. | 2009-05-28 |
20090137528 | Novel phosphonic acid compounds as inhibitors of serine proteases - The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders. | 2009-05-28 |
20090137529 | SUBSTITUTED ESTERS AS CANNABINOID-1 RECEPTOR MODULATORS - The compounds of the present invention are prodrugs of modulators of the Cannabinoid-1 (CB 1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the Cannabinoid-1 (CB 1) receptor. In particular, compounds of the present invention are 5 prodrugs of antagonists or inverse agonists of the CB 1 receptor. The invention is concerned with the use of these compounds to be converted to compounds that modulate the Cannabinoid-1 (CB 1) receptor. As such, the compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-10 Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. | 2009-05-28 |
20090137530 | Amine Compound and Use Thereof for Medical Purposes - A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. | 2009-05-28 |
20090137531 | Aryl Amide Sphingosine 1- - The present invention provides compounds that have antagonist activity at the S1P | 2009-05-28 |
20090137532 | Aldolase-inhibiting aromatic compounds - The invention relates to novel aldolase-inhibiting compounds that can be advantageously used as medicaments (in therapeutic doses), especially for treating certain cancers, due to the inhibition efficacy thereof. An inventive compound corresponds to general formula (I) wherein the aldehyde group (—CHO) and the phenol group (—OH) are linked to two carbon atoms adjacent to the same aromatic chain, i.e., the first aromatic chain, and R is a phosphate group or a phosphate group mimetic linked to a carbon atom of the second aromatic chain. | 2009-05-28 |
20090137533 | Convenience Kit for Eyelid Treatment - The present invention offers an eyelid treatment kit used for convenient combination therapy for improving overall eyelid hygiene while also providing for adjunctive eyelid therapy. The eyelid treatment kit comprises low dose doxycycline hyclate tablets, a non-irritating eyelid cleansing composition, an anti-bacterial eyelid preparation and at least one pair of moist heat goggles and/or one pair of moisture chamber goggles. The eyelid treatment kit further comprises instruction sheets containing dosage and administration information on the doxycycline hyclate coupled with information on improving eyelid hygiene. The various embodiments of the eyelid treatment kit of the invention facilitate treatment of dry eyes due to infected eyelids, and proper cleansing of the eyelids to prevent recurring infections. | 2009-05-28 |
20090137534 | Skin treatment compositions and methods - A skin treatment composition or cosmetic product comprising a) two or more active components, namely, at least one dermatological acid and at least one meroterpene and b) a dermatologically acceptable carrier. | 2009-05-28 |
20090137535 | Substituted oxazolidinone derivatives - This invention relates to novel compounds that are substituted oxazolidinones derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel oxazolidinones compounds that are derivatives of rivaroxaban. The invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and condition that are beneficially treated by administering a selective inhibitor of factor Xa, such as rivaroxaban. | 2009-05-28 |
20090137536 | METHOD FOR TREATING AND PREVENTING HYPERPARATHYROIDISM - This invention relates to a method for treating or preventing hyperthyroidism associated with aging and/or with Aging-Related Vitamin D Deficiency (ARVDD) syndrome by administering a sufficient amount of an active vitamin D compound utilizing a variety of effective treatment protocols. The invention further relates to treating or preventing one or more of the following conditions, e.g., (1) primary vitamin D deficiency, (2) 1,25-(OH) | 2009-05-28 |
20090137537 | THERAPEUTIC GESTAGENS FOR THE TREATMENT OF PREMENSTRUAL DYSPHORIC DISORDER - A method of treating premenstrual dysphoric disorders comprising administering to a patient in need of such treatment daily from day 1 to day 24 3 mg of drospirenone and 0.02 mg of ethinylestradiol. | 2009-05-28 |
20090137538 | METHOD OF TREATING ATROPHIC VAGINITIS - This invention relates to a method and pharmaceutical composition useful in treating a condition responsive to hormone replacement therapy. Specifically, the invention is related to the long term treatment of symptoms associated with atrophic vaginitis. The composition contains effective amounts of an estrogen, a progesterone compound and a pharmaceutically accepted vehicle, carrier and/or diluent. | 2009-05-28 |
20090137539 | TOPICAL OPHTHALMIC OR OTIC SOLUTION FORMULATIONS CONTAINING MOXIFLOXACIN HYDROCHLORIDE AND DEXAMETHASONE PHOSPHATE - Topical ophthalmic and otic solution compositions of moxifloxacin and dexamethasone phosphate are disclosed. | 2009-05-28 |
20090137540 | COMPOSITIONS FOR THE TREATMENT OF GASTROINTESTINAL INFLAMMATION - Provided herein are methods for treating, preventing or alleviating the symptoms of and inflammation associated with inflammatory diseases and conditions of the gastrointestinal tract, for example, those involving the esophagus. Also provided herein are pharmaceutical compositions useful for the methods of the present invention. | 2009-05-28 |
20090137541 | Novel Series of Imidazolyl Substituted Steroidal and Indan-1-One Derivatives - The present invention provides a novel series of imidazolyl substituted steroidal and indan-1-one derivatives and salts thereof having the following general structural formulae (A and B) | 2009-05-28 |
20090137542 | Alpha-glucosidase inhibitors from fungal hydroxylation of tibolone and hydroxytibolones - Sixteen new and one known metabolites were obtained by incubation of tibolone and hydroxytibolones with various fungi. Their structures were elucidated by means of a homo and heteronuclear 2D NMR and by HREI-MS techniques. The relative stereochemistry was deduced by 2D NOESY experiment. These metabolites have shown promising inhibitory activities against α-glucosidase enzyme. Seven metabolites exhibited potent inhibitory activity against the α-glucosidase enzyme and were thus found useful in the treatment of diabetes mellitus and other diseases related to the activity of α-glucosidase enzyme. | 2009-05-28 |
20090137543 | METHOD AND COMPOUNDS FOR MODULATING INSULIN PRODUCTION - The present invention provides screening methods for the detection of agents that affect various aspects of β-cell biology, particularly insulin gene expression. Screening methods are also provided for detection of agents that affect β-cell differentiation from progenitor cells. Additionally, agents identified using such methods are provided and are useful for increasing insulin gene expression and reducing lipotoxicity. | 2009-05-28 |
20090137544 | Formation and rejuvenation of organs and alcohol damaged organ regeneration through stem cell nutrients - Mechanisms nourish stem cells for organ regeneration and prevent alcohol related diseases such as Fetal Alcohol Syndrome (FAS) and Liver Sclerosis. These stem cell nutrients have been found to positively affect the skin, liver, brain neurons, pancreas, and the GI tract. Cholesterol supplementation prevents fetal alcohol spectrum defects (FASD) in alcohol-exposed zebra fish embryos. Using the zebra fish model, alcohol was found to interfere with embryonic development by disrupting cholesterol-dependent activation of a critical signaling molecule, sonic hedgehog (Shh). Cholesterol supplementation of the alcohol-exposed embryos restored the functionality of the molecular pathway and prevented development of FASD-like defects. Novel biomarkers were identified for diagnosing alcohol related diseases by lipid chemical analysis and Raman Spectroscope. | 2009-05-28 |
20090137545 | Compounds - The present invention relates to compounds of general formula I | 2009-05-28 |
20090137546 | Anti-Hypercholesterolemic Compounds - This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events. | 2009-05-28 |
20090137547 | Heterobicyclic metalloprotease inhibitors - The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors. | 2009-05-28 |
20090137548 | 1,3-Oxazolidin-2-One Derivatives Useful as Cetp Inhibitors - Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B. | 2009-05-28 |
20090137549 | Novel compounds useful for the treatment of degenerative & inflamatory diseases - The present invention relates to compounds that are inhibitors of PDE1A, a phosphodiesterase that is involved in the modulation of the degradation of cartilage, joint degeneration and diseases involving such degradation and/or inflammation. | 2009-05-28 |
20090137550 | Novel Compounds - This invention relates to a novel group of 8-Alkyl/Aryl-4-aryl-2-N-(alkylamino)-N″-substituted-N′-cyanoguanidino-8H-pyrido[2,3-d]pyrimidin-7-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and pharmaceutical compositions for use in such therapy. | 2009-05-28 |
20090137551 | Substituted Bicyclolactam Compounds - The invention provides compounds of formula (1), | 2009-05-28 |
20090137552 | Organic Compound - The invention relates to a new crystalline form II of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of crystalline form II of N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. The invention relates to the amorphous forms of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of amorphous N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. | 2009-05-28 |
20090137553 | Thiazepine Oxazolidinones as Antibacterial Agents - The present invention relates to a new class of oxazolidinone derivatives, to their use as antibacterial agents, to pharmaceutical compositions containing these compounds and to methods for their preparation. | 2009-05-28 |
20090137554 | 1,4,5,6-TETRAHYDRO -PYRROLO[2,3-d]AZEPINES AND -IMIDAZO[4,5-d]AZEPINES AS MODULATORS OF NUCLEAR RECEPTOR ACTIVITY - Disclosed are chemical entities including compounds of Formula I | 2009-05-28 |
20090137555 | Compounds and Compositions as Protein Kinase Inhibitors - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases and disorders associated with kinase activity, particularly diseases associated with the activity of CDK1, CDK2, CDK4, CDK5, GSK3β, Bcr-abl, Flt-3, c-Kit, PDGFRβ, Src, Mek1 and CK1. | 2009-05-28 |
20090137556 | COSMETIC AND PHARMACEUTICAL COMPOSITIONS COMPRISING ACE INHIBITORS AND/OR ANGIOTENSIN II RECEPTOR ANTAGONISTS - In one aspect, the present invention relates to use of an ACE inhibitor and/or angiotensin II receptor antagonist for the preparation of a medicament for the treatment of a dermatological disorder, particularly by topical application of said ACE inhibitor and/or angiotensin II receptor antagonist. The present invention also provides cosmetic methods for improving and/or maintaining the skin tone of an individual suffering from, or at risk of suffering from, a dermatological disorder, said method comprising contacting the skin of said individual with an ACE inhibitor and/or angiotensin II receptor antagonist. | 2009-05-28 |
20090137557 | Calcilytic Compounds - Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided. | 2009-05-28 |
20090137558 | Pyridine based compounds useful as intermediates for pharmaceutical or agricultural end-products - The present invention relates to substituted pyridine compounds of Formula (I) and derivatives thereof, and to a process for preparing these substituted pyridines. The invention also relates to the use of the substituted pyridines as intermediates in the production of pharmaceutical, chemical and agro-chemical products. | 2009-05-28 |
20090137559 | BAZEDOXIFENE ASCORBATE - The present invention is directed to bazedoxifene ascorbate, compositions containing the same, dispersions thereof, preparations thereof, and uses thereof. | 2009-05-28 |
20090137560 | IMIDAZOLE COMPOUNDS HAVING PHARMACEUTICAL ACTIVITY TOWARDS THE SIGMA RECEPTOR - The present invention relates to compounds of formula (I), | 2009-05-28 |
20090137561 | Substituted biphenyl GPR40 modulators - The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: | 2009-05-28 |
20090137562 | SUBSTITUTED BENZYL AMINE COMPOUNDS - Certain substituted benzyl amine compounds are histamine H | 2009-05-28 |
20090137563 | PROCESS FOR THE PREPARTION OF OLANZAPINE - The invention relates to a process for the preparation of 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno-[2,3-b][1,5]benzodiazepine (olanzapine) of the formula (I) by reacting 4-amino-2-methyl-10H-thieno [2,3-b][1/5]benzodiazepine hydrochloride of the formula (II) with N-methylpiperazine in an organic solvent, which comprises carrying out the reaction in the mixture of toluene and 1,3-dimethyl-2-imidazolidinone. The invention also encompasses new 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno [2,3-b][1,5]benzodiazepine dihydrochloride trihydrate of the formula (IB), the preparation thereof and pharmaceutical compositions comprising said new compound. | 2009-05-28 |
20090137564 | 5-[(3,3,3-Trifluoro-2-hydroxy-1-arylpropyl)amino]-1H-quinolin-2-ones, A Process for Their Production and Their Use as Anti-inflammatory Agents - The present invention relates to compounds of formula I, | 2009-05-28 |
20090137565 | Method for treatment of movement disorders - The invention is directed to methods of treating movement disorders by administering an effective amount of the compound of formula (I) to patients in need thereof. More particularly, the invention is directed to a method for treating myoclonus including administering to a patient a compound of formula (I), wherein the myoclonus is not alcohol responsive essential myoclonus with dystonia. In some embodiments, the myoclonus is posthypoxic myoclonus. The invention is also directed to a method for treating dystonia, essential tremor cerebellar tremor, a tic, or chorea, including administering to a patient a compound of formula (I). | 2009-05-28 |
20090137566 | Substituted Piperdines as Renin Inhibitors - The invention relates to substituted 3,4- or higher substituted piperididine compounds, the use thereof for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; 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 activity of renin; pharmaceutical formulations or products comprising said compounds, and/or a method of treatment comprising administering said compounds, a method for the manufacture of said compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis. The compounds preferably have the formula I, | 2009-05-28 |
20090137567 | Methods for Treating Blood Disorders - Methods of treating blood disorders are described. | 2009-05-28 |
20090137568 | Tryclic Nitrogen Containing Compounds and their Use as Antibacterials - Tricyclic nitrogen containing compounds of formula (I) and their use as antibacterials. | 2009-05-28 |
20090137569 | Administration of (3S)-N-hydroxy-4-(sulfonyl)-2,2-dimethyl-3-thiomorpholine carboxamide or (S)-N_hydroxy-4-[4_(but-2-ynyloxy)phenylsulfonyl]-2,2-dimethyl thimomorpholine-3-carboxamide for preventing and/or treating inflammatory skin pathologies/afflictions - Inflammatory skin pathologies/afflictions, e.g., eczema or psoriasis, are prevented and/or treated by administering to a subject in need of such treatment, a thus effective amount of at least one compound of following formula (I): | 2009-05-28 |
20090137570 | INHIBITORS OF CATHEPSIN S - The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. | 2009-05-28 |
20090137571 | SUBSTITUTED MORPHOLINE AND THIOMORPHOLINE DERIVATIVES - The present invention relates to morpholine and thiomorpholine derivatives or the general formula I or pharmaceutically acceptable salts thereof and their use. | 2009-05-28 |
20090137572 | 2-substituted-4-heteroaryl-pyrimidines useful for the treatment of proliferative disorders - The present invention relates to selected substituted pyrimidines their preparation, pharmaceutical compositions containing them and their use as inhibitors of one or more protein kinases, and hence their use in the treatment of proliferative disorders, viral disorders and/or other disorders. | 2009-05-28 |
20090137573 | 1,3-Disubstituted 4-methyl-1H-pyrrole-2-carboxamides and their Use in Medicaments - 1,3-disubstituted 4-methyl-1H-pyrrole-2-carboxamides corresponding to formula I | 2009-05-28 |
20090137574 | Combination Therapy Using an 11Beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitor and an Antihypertensive Agent for the Treatment of Metabolic Syndrome and Related Diseases and Disorders - Combination therapy comprising the administration of an 11β-hydroxysteroid dehydrogenase type 1 inhibitor and an antihypertensive agent useful for treating, preventing and reducing the risk of developing insulin resistance, dyslipidemia, obesity, hypertension and other related diseases and disorders. | 2009-05-28 |
20090137575 | 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 Alzheimer's disease. | 2009-05-28 |
20090137576 | Novel Piperidine Derivative - Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) | 2009-05-28 |
20090137577 | HETEROCYCLIC COMPOUNDS - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I | 2009-05-28 |
20090137578 | ENANTIOMERICALLY PURE BETA AGONISTS, PROCESS FOR THE MANUFACTURE THEREOF AND USE THEREOF AS MEDICAMENTS - Enantiomerically pure compounds of general formula 1 | 2009-05-28 |
20090137579 | Mesylate salt of an IKK inhibitor - The present invention is directed to the compound of formula (II), | 2009-05-28 |
20090137580 | Fused Heterocyclic Derivatives and Use Thereof - The present invention provides a fused heterocyclic derivative showing a potent kinase inhibitory activity and use thereof. A compound represented by the formula: | 2009-05-28 |
20090137581 | Heterocyclic compounds and their uses - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 2009-05-28 |
20090137582 | Pyrazolo-pyridinone derivatives and methods of use - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of pro-inflammatory cytokine mediated diseases, and in particular, p38 activity mediated inflammation and related conditions. The compounds have a general Formula I | 2009-05-28 |
20090137583 | 2-AMINOQUINAZOLINE DERIVATIVES - The present invention provides 2-aminoquinazoline derivatives represented by formula (I): | 2009-05-28 |
20090137584 | SULFONYL BENZIMIDAZOLE DERIVATIVES - This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, R | 2009-05-28 |
20090137585 | N-ACYLSULFONAMIDE APOPTOSIS PROMOTERS - N-Benzoyl arylsulfonamides having the formula | 2009-05-28 |
20090137586 | COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - This invention relates to compounds of the Formula (I): | 2009-05-28 |
20090137587 | Phenylpyridone Derivative - A compound represented by the formula (I) is contained as an active ingredient: | 2009-05-28 |
20090137588 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 2009-05-28 |
20090137589 | Stereoisomerically Enriched 3-Aminocarbonyl Bicycloheptene Pyrimidinediamine Compounds And Their Uses - The present invention provides stereoisomers and stereoisomeric mixtures of 3-aminocarbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers. | 2009-05-28 |
20090137590 | N-LINKED HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS - Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. | 2009-05-28 |
20090137591 | COMPOUNDS AND COMPOSITIONS 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, particularly the activity of PPARδ. | 2009-05-28 |
20090137592 | MORPHOLINES AS SELECTIVE INHIBITORS OF CYTOCHROME P450 2A13 - A method of inhibiting formation of cancerous metabolites, of inhibiting cytochrome P450 2A13 from forming carcinogen metabolites, and/or inhibiting formation of cancerous lung cells in a subject can include: providing a morpholine compound that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6; administering a therapeutically effective amount of the morpholine compound or derivative to the subject. The morpholine compound or derivative can be substantially more selective for interacting with the cytochrome P450 2A13 over the cytochrome P450 2A6. The morpholine compound or derivative can also be substantially non-interactive with other physiological components. The morpholine compound or derivative can include a structure that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6, such as Compounds 1-34 of Formulas A-D. | 2009-05-28 |
20090137593 | 4-AMINO-2,6-DIMETHYLPHENOL COMPOUND, PROCESS FOR ITS PREPARATION AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - A 4-amino-2,6-dimethylphenol compound having the formula given in the description, acid-addition salts thereof, a process for preparing them, pharmaceutical composition comprising them and its use as anti-pyretic and anti-nociceptive agents. | 2009-05-28 |
20090137594 | Pentafluorosulphanyl-Substituted Compound And Its Use For Producing Medicaments - The present invention relates to pentafluorosulphanyl-substituted compounds, methods for their production, medicaments containing such compounds and the use of such compounds for producing medicaments. | 2009-05-28 |