47th week of 2008 patent applcation highlights part 50 |
Patent application number | Title | Published |
20080287345 | Polymyxin derivatives and uses thereof - The present invention relates to a polymyxin derivative wherein R1, R2 and R3 are optional and R1, R2, R3, R5, R8 and R9 are cationic or neutral amino acid residues selected so that the total number of positive charges at physiological pH is at least two but no more than three; and to a combination product comprising at least two such derivatives. The invention further relates to a method for treating, alleviating or ameliorating an infection in a subject, caused by a Gram-negative bacterium by administering a therapeutically effective amount of a derivative according to the present invention to said subject; to a method for sensitizing Gram-negative bacteria to an antibacterial agent by administering, simultaneously or sequentially in any order a therapeutically effective amount of said antibacterial agent and a derivative according to the present invention to said subject; to methods for developing novel antibiotics; for reducing the nephrotoxicity, for improving the pharmacokinetic properties of natural polymyxins and octapeptins; and for sensitizing clinically important bacteria to a host defence mechanism complement present in serum. Finally, the invention relates to a process for preparing such polymyxin derivatives. | 2008-11-20 |
20080287346 | Bioactive peptides - The present invention provides a cytotoxic 7 to 25-mer peptide with three or more cationic residues which has one or more non-generic bulky and lipophilic amino acids, as well as esters, amides, salts and cyclic derivatives thereof as well as methods of preparing the peptides, pharmaceutical compositions containing them, and their use as medicaments, particularly as antibacterial or antitumor agents. | 2008-11-20 |
20080287347 | Novel Lipopeptides as Antibacterial Agents - The present invention relates to novel lipopeptide compounds. The invention also relates to pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The invention also relates to methods of producing these novel lipopeptide compounds and intermediates used in producing these compounds. | 2008-11-20 |
20080287348 | Soluble Hybrid Prion Proteins And Their Use In The Diagnosis, Prevention And Treatment Of Transmissible Spongiform Encephalopathies - The present invention relates to a soluble hybrid protein, comprising at least a first polypeptide sequence derived from a prion protein PrP | 2008-11-20 |
20080287349 | Fibroblast growth factor 20 and methods of use thereof - The present invention relates to compositions and methods for preventing and treating a disease (e.g., a joint disease, ischemic stroke, hemorrhagic stroke, trauma, spinal cord damage, heavy metal or toxin poisoning, or neurodegenerative diseases). More particularly, the present invention provides methods for preventing and/or treating a disease (e.g., a joint disease, ischemic stroke, hemorrhagic stroke, trauma, spinal cord damage, heavy metal or toxin poisoning, or neurodegenerative diseases) by using compositions comprising FGF-20, a fragment, a derivative, a variant, a homolog, or an analog thereof. | 2008-11-20 |
20080287350 | Aequorin-Containing Compositions and Methods of Using Same - Compositions containing aequorin and methods for their use in preventing and/or alleviating symptoms and disorders related to calcium imbalance are provided by the present invention. | 2008-11-20 |
20080287351 | Nfkb Transcriptional Activity Inhibitory Agent and Anti-Inflammatory Agent and a Steroid Action Enhancing Agent - It is intended to surely and effectively inhibit the transcriptional activity of NFκB and to obtain a more effective anti-inflammatory effect. Further, it is intended to obtain an equivalent effect even if the amount used of a steroid agent is reduced. | 2008-11-20 |
20080287352 | Anti-Histone H1 Monoclonal Antibody and Hybridoma for the Production Thereof - The present invention discloses anti-histone H1 monoclonal antibodies, hybridomas for the production thereof, and polypeptides, which are useful for suppressing, predicting, or diagnosing transplant rejection in organ transplantation. | 2008-11-20 |
20080287353 | Peptides and proteins for early liver development and antibodies thereto - Early developing stage-specific liver proteins and the genes coding for them that have been isolated and sequenced are provided, and these genes and proteins can be utilized to diagnose and/or treat a wide variety of liver disorders and other ailments. Since the early developing liver proteins of the invention arise during embryogenesis when the liver and other organs are in transition from an undifferentiated state to a differentiated one, these proteins are involved in tissue differentiation and thus can be utilized in methods of diagnosing and treating a variety of liver diseases and other disorders including those relating to oncogenesis and tissue repair. Antibodies recognizing early developing liver proteins and peptides are also provided. | 2008-11-20 |
20080287354 | Prosaposin as a neurotrophic factor - Prosaposin, saposin C and various peptide fragments of saposin C stimulate neurite outgrowth in vitro. In addition, prosaposin and saposin C promote increased myelination ex vivo. Prosaposin is present in large neurons of the brain, including both upper and lower motor neurons. | 2008-11-20 |
20080287355 | Amylin and Amylin Agonists For Treating Psychiatric Diseases and Disorders - Methods and compositions for treating psychiatric diseases and disorders are disclosed. The methods provided generally involve the administration of an amylin or an amylin agonist to a subject in order to treat psychiatric diseases and disorders, and conditions associated with psychiatric diseases and disorders. | 2008-11-20 |
20080287356 | Chimeric Proteins, Their Preparation and Pharmaceutical Compositions Containing Them - The present invention relates to a chimeric protein comprising a cell-targeting agent and a | 2008-11-20 |
20080287357 | Conjugate Comprising P21 Protein for the Treatment of Cancer - The P21 protein is used as a medicament in the treatment of cancer. A conjugate comprises a first region comprising the P21 protein, or a homologue or functional fragment thereof; and a second region comprising a translocation factor. | 2008-11-20 |
20080287358 | Regulatory T Cell Mediator Proteins and Uses Thereof - The present invention relates to novel regulatory T cell proteins. One protein, designated PD-L3, resembles members of the PD-L1 family, and co-stimulates αCD3 proliferation of T cells in vitro. A second, TNF-like, protein has also been identified as being upregulated upon αCD3/αGITR stimulation. This protein has been designated T | 2008-11-20 |
20080287359 | CADHERIN-11-MEDIATED MODULATION OF HAIR GROWTH - The present invention provides for methods of inhibiting hair growth, comprising decreasing the level of CAD1 1 mRNA and/or protein in hair follicle cells of a subject. The present invention further provides for methods of promoting hair growth, comprising increasing the level of CADI 1 mKNA and/or protein in hair follicle cells of a subject. The invention also provides for transgenic animals with aberrancies in CADI 1 expression, and for assay systems (including transgenic animals and cell-based systems) that may be used to identify agents that decrease or increase CADI 1 expression. | 2008-11-20 |
20080287360 | COMPOSITIONS AND METHODS FOR TREATING MALARIA WITH CUPREDOXIN AND CYTOCHROME - The present invention relates to cupredoxin and cytochrome and their use, separately or together, to inhibit the spread of parasitemia in mammalian red blood cells and other tissues infected by the malaria parasite, and in particular the parasitemia of human red blood cells by | 2008-11-20 |
20080287361 | Compositions and methods of using CRMP-1 and its fragments for treating cancer - The present invention discloses a method for treating cancer by using hCRMP1 and/or active fragments thereof, as well as the active fragments of hCRMP1 that are capable of inhibiting cell proliferation, invasive activity, and metastasis of cancer. The method can also be used prior to, or in combination with, the administration a chemotherapy agent. A vector capable of expressing an hCRMP1, a variant of hCRMP1, a fragment of hCRMP1 or a variant of a fragment of hCRMP1 is also disclosed. | 2008-11-20 |
20080287362 | Compositions and Methods for the Detection of Trypanosoma Cruzi Infection - Compositions comprising fusion polypeptides of | 2008-11-20 |
20080287363 | Novel Cc-Chemokine Antagonists - A novel CC-chemokine binding protein is isolated from the saliva of | 2008-11-20 |
20080287364 | Bitter Taste Receptors - The present invention relates to bitter-taste receptors and their role in bitter taste transduction. The invention also relates to assays for screening molecules that modulate, e.g. suppress or block, bitter taste transduction, or enhance bitter taste response. | 2008-11-20 |
20080287365 | DRUG AND METHOD FOR PROLIFERATING NATURAL KILLER CELLS - Natural Killer (NK) cells are obtained by administering a Toll-like receptor ligand such as polyinosinic-polycytidylic acid into the peritoneal cavity of an animal to which lactoferrin has been administered to proliferate NK cells in the peritoneal cavity and collecting NK cells from the peritoneal cavity. | 2008-11-20 |
20080287366 | Parenteral formulations of a peptide for the treatment of systemic lupus erythematosus - The subject invention provides a pharmaceutical composition comprising an aqueous carrier; from 0.1 mg/ml to 20 mg/ml of the composition of a pharmaceutically acceptable salt of a peptide having the structural formula | 2008-11-20 |
20080287367 | Non-Toxic Biofilm Inhibitor - The present invention relates to a composition and method for preventing or inhibiting biofilm formation on biotic or abiotic surfaces. The composition comprises a peptide based on the C-terminal receptor binding domain of | 2008-11-20 |
20080287368 | Methods and Compositions For the Prevention and Treatment of Kidney Disease - The invention provides compositions for preventing or treating kidney disease comprising vitamin E, vitamin C, and a carotenoid and methods for preventing and treating kidney disease comprising administering such compositions to an animal susceptible to or suffering from kidney disease. In a preferred embodiment, the composition is admixed with one or more food ingredients to produce a food composition useful for preventing or treating kidney disease. | 2008-11-20 |
20080287369 | Compositions and Methods for Viscosupplementation - The invention provides viscosupplementation compositions that include hyaluronic acid, or a polymer thereof and tribonectin. Such compositions are useful for the lubrication and chondroprotection of mammalian joints. | 2008-11-20 |
20080287370 | Boronic Acid Salts Useful in Parenteral Formulations - Salts of a peptide boronic acid drug, for example of Cbz-(R)-Phe-(S)—Pro-(R)-Mpg-B(OH) | 2008-11-20 |
20080287371 | MACROCYCLIC ANTAGONISTS OF THE MOTILIN RECEPTOR FOR MODULATION OF THE MIGRATING MOTOR COMPLEX - The present invention relates to novel conformationally-defined macrocyclic compounds that bind to and/or are functional modulators of the motilin receptor including subtypes, isoforms and/or variants thereof. These macrocyclic compounds are useful as therapeutics for a range of gastrointestinal disorders, in particular those in which suppression or inhibition of the migrating motor complex (MMC) is effective or malfunction of gastric motility or increased motilin secretion is observed, such as hypermotilinemia, imitable bowel syndrome, dyspepsia, including gallbladder dyspepsia, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, | 2008-11-20 |
20080287372 | Use of Ketogenic Compounds for Treatment of Age-Associated Memory Impairment - This invention relates to the field of therapeutic agents for the treatment of Age-Associated Memory Impairment (AAMI). In particular, the present invention utilizes compositions comprising at least one compound capable of elevating ketone body concentrations in a mammal (e.g., ketogenic compounds), administered in an amount effective for treatment or prevention of loss of cognitive function caused by reduced neuronal metabolism in AAMI. In one embodiment, the composition includes medium chain triglycerides (MCT). In another embodiment, the compositions are administered in the presence of carbohydrate. The present invention also relates to oral dosage forms, in particular, a nutritional drink comprising at least one compound capable of elevating ketone body concentrations in a mammal. | 2008-11-20 |
20080287373 | Topical skin treating kits - A kit comprising a soap-free cleanser and a topical composition which comprises clindamycin or a pharmaceutically acceptable salt or ester thereof, and a pharmaceutically acceptable carrier, formulations and packages thereof, and methods of using the same to treat various skin disorders. | 2008-11-20 |
20080287374 | BREAST CANCER-RESISTANT PROTEIN INHIBITOR - The invention provides a cancer cell useful in screening BCRP-inhibitors, and a BCRP-inhibitor. | 2008-11-20 |
20080287375 | Selective Glycosidase Inhibitors, Methods of Making Inhibitors, and Uses Thereof - The invention comprises compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions containing the compounds or prodrugs of the compounds. The invention also comprises animal models and methods of making the animal models for studying diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc, and treatment of such diseases and disorders. The invention also comprises methods of treating such diseases and disorders. The invention also comprises methods of making the compounds, and methods of making selective glycosidase inhibitors. | 2008-11-20 |
20080287376 | Ketolide Derivatives as Antibacterial Agents - The present invention provides ketolide derivatives, which can be used as antibacterial agents. In particular, compounds described herein can be used for treating or preventing conditions caused by or contributed to by Gram-positive, Gram-negative or anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, | 2008-11-20 |
20080287377 | Composition Based on Triethyl Citrate for the Prevention of Enzymatic Hydrolysis of Triglycerides - The invention concerns a composition for topical use for the protection of triglycerides against enzymatic hydrolysis, which contains triethyl citrate as an active ingredient either pure or in combination with some synergists. The triethyl citrate is in a quantity in weight expressed as a percentage from 0.1 to 99.9, preferably from 0.2 to 50 percent or even better a weight expressed as a percentage from 1.0 to 25.0. The claims are also directed to the use of triethylcitrate for the treatment of acne and seborrheic dermatitis, for the protection of triglycerides in alimentary products and for treatment of aesthetic cutaneous effects in the cosmic field. | 2008-11-20 |
20080287378 | Solid state forms of 5-azacytidine and processes for preparation thereof - The present invention provides novel crystalline forms of 5-deazacytidine, and pharmaceutical compositions comprising these novel forms. The invention also provides methods for the preparation of the novel forms and compositions. | 2008-11-20 |
20080287379 | Oligonucleotide Complex Compositions and Methods of Use as Gene Alteration Tools - Compositions and methods of treatments of cells are provided for altering the phenotype of a cell by administering an oligonucleotide complex to the cell, the complex having two strands and chemical modifications. | 2008-11-20 |
20080287380 | Antisense Oligonucleotides Against Cpla2, Compositions and Uses Thereof - Antisense oligonucleotides against cPLA | 2008-11-20 |
20080287381 | Injectable Agent for the Targeted Treatment of Retinal Ganglion Cells - The present invention relates to the targeted treatment of retinal ganglion cells (RGC). | 2008-11-20 |
20080287382 | Oligoribonucleotides and methods of use thereof for treatment of alopecia, acute renal failure and other diseases - The invention relates to a double-stranded compound, preferably an oligoribonucleotide, which down-regulates the expression of a human p53 gene. The invention also relates to a pharmaceutical composition comprising the compound, or a vector capable of expressing the oligoribonucleotide compound, and a pharmaceutically acceptable carrier. The present invention also contemplates a method of treating a patient suffering from alopecia or acute renal failure or other diseases comprising administering to the patient the pharmaceutical composition in a therapeutically effective dose so as to thereby treat the patient. The alopecia may be induced by chemotherapy or radiotherapy, and the patient may be suffering from cancer, in particular breast cancer. | 2008-11-20 |
20080287383 | NUCLEIC ACID COMPOUNDS FOR INHIBITING ERBB GENE EXPRESSION AND USES THEREOF - The present disclosure provides meroduplex ribonucleic acid molecules (mdRNA) capable of decreasing or silencing ERBB gene expression. An mdRNA of this disclosure comprises at least three strands that combine to form at least two non-overlapping double-stranded regions separated by a nick or gap wherein one strand is complementary to an ERBB mRNA. In addition, the meroduplex may have at least one uridine substituted with a 5-methyluridine, a nucleoside replaced with a locked nucleic acid, or optionally other modifications, and any combination thereof. Also provided are methods of decreasing expression of an ERBB gene in a cell or in a subject to treat an ERBB-related disease. | 2008-11-20 |
20080287384 | Methods of Identifying Agents Having Antiangiogenic Activity - Provided are assays and methods of identifying antiangiogenic agents including contacting an endothelial cell with a putative antiangiogenic agent and assaying for activation of Rap-1 in the endothelial cell. Also provided are methods of inhibiting angiogenesis and treating conditions associated with improper angiogenesis. Compositions comprising activators of Rap-1 and methods of activating the Rap-1 signaling pathway are also provided. Methods of inhibiting chemotaxis and angiogenesis by contacting cells with Rho inhibitors are provided. | 2008-11-20 |
20080287385 | Inhibitor oligonucleotides and their use for specific repression of a gene - A double-strand oligonucleotide including two complementary oligonucleotide sequences forming a hybrid, each including at one of their 3′ or 5′ ends, one to five unpaired nucleotides forming single-strand ends extending beyond the hybrid, one of the oligonucleotide sequences being substantially complementary to a target sequence belonging to a DNA or RNA molecule to be specifically repressed, the target sequence belonging to a DNA or RNA molecule of a gene coding an angiogenic factor. | 2008-11-20 |
20080287386 | Oligoribonucleotides and methods of use thereof for treatment of fibrotic conditions and other diseases - The invention relates to a double-stranded compound, preferably an oligoribonucleotide (siRNA), which down-regulates the expression of a human TGaseII gene at the post-transcriptional level. The invention also relates to a pharmaceutical composition comprising the compound, or a vector capable of expressing the oligoribonucleotide compound, and a pharmaceutically acceptable carrier. The present invention also contemplates a method of treating a patient suffering from a fibrotic disease such as pulmonary, kidney and liver fibrosis or ocular, scarring comprising administering to the patient the pharmaceutical composition in a therapeutically effective dose so as to thereby treat the patient. The invention also relates to treatment of fibrotic and other diseases by use of antibodies to TGaseII polypeptide. | 2008-11-20 |
20080287387 | Method for Producing Sterile Polynucleotide Based Medicaments - The present invention relates to a novel method for producing formulations comprising a polynucleotide, block copolymer and cationic surfactant. The formulations produced by the current method are suitable for use in polynucleotide based medicaments. A suitable method of production disclosed herein additionally comprises cold filtering a mixture of a polynucleotide, block copolymer and cationic surfactant, thereby sterilizing the formulation. The method of the present invention also eliminates the need for thermal cycling of the formulation, thereby reducing the time and expense required to produce large quantities of a formulation during commercial manufacturing. The present invention also relates to novel cationic lipids. | 2008-11-20 |
20080287388 | Human G-Protein Coupled Receptor - A human G-protein coupled receptor polypeptide and DNA (RNA) encoding such polypeptide and a procedure for producing such polypeptide by recombinant techniques is disclosed. Also disclosed are methods for utilizing such polypeptide for identifying antagonists and agonists to such polypeptide. Antagonists and agonists may be used therapeutically to inhibit or stimulate the G-protein coupled receptor. Also disclosed are assays for detecting mutations in the nucleic acid sequence encoding the G-protein coupled receptor. | 2008-11-20 |
20080287389 | Nucleoside analogs in combination therapy of herpes simplex infections - A pharmaceutical product comprising a nucleoside analogue active against herpes simplex virus, such as acyclovir/valaciclovir or peniclovir/famciclovir, and an immunosuppressant, as a combined preparation for simultaneous, separate or sequential use in the treatment and/or prevention of herpes simplex virus infections. | 2008-11-20 |
20080287390 | Pyrazolidinol compounds - The invention provides the use of an optionally hydroxyl-protected 4-hydroxy or hydroperoxy-3,5-dioxopyrazolidine or an equivalent wherein a pyrazolidine ring attached oxygen is replaced by a sulphur, or a physiologically acceptable salt thereof, for the manufacture of a medicament for use in drug therapy or prophylaxis. Additionally, the invention provides a method of combating HIV infection which comprises administering to an HIV-infected patient a T-lymphocyte growth suppressing agent, preferably a pyrazolidinol, in an amount sufficient to suppress T-lymphocyte growth in said patient for a period sufficient to reduce the T-lymphocyte concentration in lymph nodes in said patient. | 2008-11-20 |
20080287391 | Cell Fusion Promoter and Utilization of the Same - It is intended to provide a regeneration promoter for regenerating a tissue with the use of somatic stem cells. It is also intended to provide a cell fusion promoter safely usable in vivo. Namely, it is intended to provide a cell fusion promoter comprising ATP or its metabolite. A cell fusion promoter comprising ATP or its metabolite and a method of producing fused cells in the presence of ATP or its metabolite. A medicinal composition for regenerating or improving the function of a tissue or an organ, which suffers from dysfunction or hypofunction due to injury or denaturation, by using stem cells. This composition comprises ATP or its metabolite and a pharmaceutically acceptable carrier. | 2008-11-20 |
20080287392 | Wound-Healing Pharmaceutical Compositions in the Form of a Cream Based on Amino Acids and Sodium Hyaluronate - This invention relates to wound-healing pharmaceutical or cosmetic (anti-skin aging) compositions in the form of a cream based on amino acids and sodium hyaluronate. | 2008-11-20 |
20080287393 | External Skin Composition - The external skin care composition of the present invention comprises N-acetylglucosamine and at least one member selected from the group consisting of retinoid and pro-vitamin A. | 2008-11-20 |
20080287394 | Hiv Integrase Inhibitors - Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R | 2008-11-20 |
20080287395 | Phospholipid Compositions for Contact Lens Care and Preservation of Pharmaceutical Compositions - The use of certain synthetic phospholipids to preserve pharmaceutical compositions from microbial contamination is described. The synthetic phospholipids have unique molecular arrangements wherein a phosphate group is linked to a quaternary ammonium functionality via a substituted-propenyl group, and the quaternary ammonium functionality is further linked to at least one long hydrocarbon chain. Such molecular arrangements are what make the phospholipids of formula (I) highly water soluble, e.g., the length of the hydrocarbon chain assists to maintain solubility and efficacy of the molecules for the uses described herein. The synthetic phospholipids described herein have been found to be particularly useful as antimicrobial preservatives for ophthalmic, otic and nasal pharmaceutical compositions, especially ophthalmic compositions. These compounds may also be utilized to disinfect contact lenses. The invention is based in-part upon a finding that the antimicrobial activity of the synthetic phospholipids is affected by the ionic strength of the compositions in which the compounds are contained. The provision of compounds having limited ionic strengths is therefore preferred. | 2008-11-20 |
20080287396 | Phosphonated Fluoroquinolones, Antibacterial Analogs Thereof, and Methods for the Prevention and Treatment of Bone and Joint Infections - The present invention relates to phosphonated fluoroquinolones, antibacterial analogs thereof, and methods of using such compounds. These compounds are useful as antibiotics for prevention and/or the treatment of bone and joint infections, especially for the prevention and/or treatment of osteomyelitis. | 2008-11-20 |
20080287397 | Pyrrolopyrimidine Derivatives Substituted with Cyclic Amino Group - An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. This problem can be solved with a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by formula [I] below which has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved. | 2008-11-20 |
20080287398 | COLD MENTHOL RECEPTOR-1 ANTAGONISTS - The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described. | 2008-11-20 |
20080287399 | Substituted Aminopyridines and Uses Thereof | 2008-11-20 |
20080287400 | Low Dosage Forms Of Risedronate Or Its Salts - Oral dosage forms comprising risedronate or a salt thereof, a chelating agent, and means for effecting delayed release of the risedronate (or salt) immediate release of the oral dosage form to the small intestine of the mammal subject and pharmaceutically effective absorption of the bisphosphonate with or without food or beverages. The present invention substantially alleviates the interaction between the risedronate (or salt) and food or beverages, which interaction results in the active ingredient not being available for absorption. The resulting oral dosage form may thus be taken with or without food. Further, disclosed is delivery of risedronate and the chelating agent to the small intestine, substantially alleviating the upper GI irritation associated with bisphosphonate therapies. These benefits simplify previously complex treatment regimens and can lead to increased patient compliance with bisphosphonate therapies. | 2008-11-20 |
20080287401 | Methods for Synthesizing and Purifying Aminoalkyl Tetracycline Compounds - Methods for the synthesis and purification of 9-amino alkyl tetracycline compounds are described. | 2008-11-20 |
20080287402 | Use of a glial attenuator to prevent amplified pain responses caused by glial priming - The use of a glial attenuator, such as ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine), to prevent the negative consequences of glial priming is described. In particular, the present invention is directed to a method of treating a subject with ibudilast to prevent amplified pain responses to inflammation or injury as a result of glial priming following an initial glial activating event. | 2008-11-20 |
20080287403 | USE OF INHIBITORS OF THE RENIN-ANGIOTENSIN SYSTEM IN THE PREVENTION OF CARDIOVASCULAR EVENTS - Use of an inhibitor of the renin-angiotensin system or a pharmaceutically acceptable derivative thereof, optionally together with an other antihypertensive, a cholesterol lowering agent, a diuretic or aspirin, in the manufacture of a medicament for the prevention of cardiovascular events; a method of preventing cardiovascular events comprising administering to a patient in need of such prevention an effective amount of an inhibitor of the renin angiotensin system or a pharmaceutically acceptable derivative thereof, optionally together with an other antihypertensive, a cholesterol lowering agent, a diuretic or aspirin; and a combination product containing an an inhibitor of the renin-angiotensin system or a pharmaceutically acceptable derivative thereof and a cholesterol lowering agent. | 2008-11-20 |
20080287404 | High Purity 17Alpha-Cyanomethyl-17Beta-Hydroxy-Estra-4,9-Diene-3- One and Process For the Syntheses Thereof - The invention relates to a new process for the synthesis of high purity 17α-cyanomethyl-17β-hydroxy-estra-4,9-diene-3-one (further on dienogest) of formula (I) from 3-methoxy-17-hydroxy-estra-2,5(10)-diene of formula (V). The invention relates also to the high purity 17α-cyanomethyl-17β-hydroxy-estra-4,9-diene-3-one and pharmaceutical compositions containing that as active ingredient. The pharmaceutical compositions according to this invention contain high purity dienogest of formula (I) in which the total amount of impurities is less than 0.1%, while the amount of 4-bromo-dienogest is under the detection limit (0.02%) as active ingredient or at least one of the active ingredients and auxiliary materials, which are commonly used in practice, such as carriers, excipients or diluents. According to our invention the dienogest of formula (I) is synthesized the following way: i) 3-methoxy-17-hydroxy-estra-2,5(10)-diene of formula (V) is reacted with aluminum isopropylate in the presence of cyclohexanone in an inert organic solvent under heating; ii) the so obtained 3-methoxy-estra-2,5(10)-diene-17-one of formula (IV) is reacted with cyanomethyl lithium at a temperature between 0 and −30° C.; iii) the obtained 3-methoxy-17α-cyanomethyl-17β-hydroxy-estra-2,5(10)-diene of formula (III) is reacted with a strong organic acid in tetrahydrofuran solution; iv) the obtained 17α-cyanomethyl-17β-hydroxy-estr-5(10)-ene-3-one of formula (II) is reacted with 1-1.5 equivalent of pyridinium tribromide in pyridine solution at a temperature between 0 and 60° C., then the obtained crude dienogest of formula (I) is purified by recrystallization and preparative HPLC. | 2008-11-20 |
20080287405 | Compositions and Methods Relating to Protein Kinase Inhibitors - The present invention relates to compounds useful for treating fibrotic disorders, methods for their discovery, and their therapeutic use. In particular, the present invention provides pyrazolopyrimidine compounds and related compounds and methods of using pyrazolopyrimidine derivatives and related compounds as therapeutic agents to treat a number of conditions associated with fibrotic disorders. | 2008-11-20 |
20080287406 | Compositions and methods for treating medical conditions - The invention features methods, compositions, and kits for the treatment of pain, pruritus, immunoinflammatory disorders, musculoskeletal disorders, and the reduction of serum C reactive protein (CRP) in a patient having a disease or conditions associated with an increased CRP level. The methods, compositions, and kits of the invention provide for a combination therapy including an SSRI and a corticosteroid. | 2008-11-20 |
20080287407 | Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use - The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs. | 2008-11-20 |
20080287408 | ENDOMETRIOSIS TREATMENT - A pharmaceutical composition comprises at least one nonlipoidal internal phase and at least one lipoidal external phase that is bioadhesive to a vaginal mucosal surface, and comprises danazol in an amount of about 3% to about 30% by weight of the composition, wherein upon application of the composition to the vaginal mucosal surface the danazol is released over a period of about 1 to about 10 days. The composition is useful for intravaginal administration to treat a condition such as endometriosis for which danazol is indicated. | 2008-11-20 |
20080287409 | PHENYL AND PYRIDINYL-1,2,4-OXADIAZOLONE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention comprises phenyl and pyridinyl 1,2,4-oxadiazolone compounds their physiologically acceptable salts and physiologically functional derivatives that exhibit peroxisome proliferator activator receptor (PPAR) delta agonist activity. Also described and claimed are processes for their preparation and their use as pharmaceuticals. These are compounds of formula I, | 2008-11-20 |
20080287410 | PYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF PKC-THETA - Disclosed are novel compounds of formula (I): | 2008-11-20 |
20080287411 | Optically active dihydropyridine derivative - The optically active compound (R)-2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 3-(1-diphenylmethylazetidin-3-yl) ester 5-isopropyl ester or a pharmacologically acceptable salt thereof, and a method using the compound or its salt to treat circulatory diseases. | 2008-11-20 |
20080287412 | THERAPEUTIC COMBINATION OF AMLODIPINE AND BENAZEPRIL/BENAZEPRILAT - The present invention especially relates to the use of a combination comprising | 2008-11-20 |
20080287413 | NEW CRYSTALLINE FORMS - There are provided crystalline forms of the compounds Ph(3-Cl)(5-OCHF | 2008-11-20 |
20080287414 | Mitotic Kinesin Inhibitors - The present invention relates to tricyclic pyrazoles according to Formula (I) that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. | 2008-11-20 |
20080287415 | Bicycloheteroaryl compounds as P2X7 modulators and uses thereof - Compounds are disclosed that have a formula represented by the following: | 2008-11-20 |
20080287416 | Organic Compounds - There are provided according to the invention compounds of formula (I) | 2008-11-20 |
20080287417 | PHARMACEUTICAL COMPOSITIONS COMPRISING A POORLY WATER-SOLUBLE ACTIVE INGREDIENT, A SURFACTANT AND A WATER-SOLUBLE POLYMER - Solid composition comprising (a) an anionic surfactant in combination with a water-soluble and basic polymer, or (b) a cationic surfactant in combination with a water-soluble and acidic polymer, and (c) at least one poorly water-soluble pharmaceutically active ingredient, and solid or liquid dosage forms, especially tablets, coated tablets, capsules or suppositories or aqueous solutions comprising the solid composition. The surfactant/polymer system is soluble in water and solubilises the active ingredient so that good bioavailability with therapeutical quantities may be attained. Aqueous solutions are suitable for nasal, parenteral or ophthalmic treatments. | 2008-11-20 |
20080287418 | Extended Release Compositions and Methods for Their Manufacture - Extended release formulations of quetiapine and its pharmaceutically salts, and methods for manufacture of the formulations, may include the use of polymers selected for their physical and chemical characteristics. The formulations may include polymers selected to cause solid dosage forms of the formulations to conform to preselected quetiapine release criteria. The formulations may include non-polymer materials that may affect quetiapine release. | 2008-11-20 |
20080287419 | APOPTOSIS PROMOTERS - Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed. | 2008-11-20 |
20080287420 | CYCLOPAMINE LACTAM ANALOGS AND METHODS OF USE THEREOF - The present invention relates to steroidal alkaloids useful in the treatment of hedgehog pathway related disorders, particularly cancer. | 2008-11-20 |
20080287421 | 3,3-SPIROINDOLINONE DERIVATIVES - There are provided compounds of the general formulas | 2008-11-20 |
20080287422 | Constrained Compounds as CGRP-Receptor Antagonists - The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors. | 2008-11-20 |
20080287423 | Use of Azapaullones For Preventing and Treating Pancreatic Autoimmune Disorders - This invention relates to the use of azapaullones, particularly in combination with immunomodulating agents, in the prevention, and/or treatment of pancreatic autoimmune disorders, e.g. type I diabetes or LADA and neurodegenerative disorders. | 2008-11-20 |
20080287424 | AZOLYLACYLGUANIDINES AS beta-SECRETASE INHIBITORS - The present invention provides an azolylacylquanidine compound of formula I | 2008-11-20 |
20080287425 | Method for Controlling Chinch Bugs - The present invention relates to a method for controlling chinch bugs comprising introducing to a locus where chinch bug control is needed or expected to be needed a composition comprising a nitroguanidine insecticide. | 2008-11-20 |
20080287426 | Method of Inducing Resistance to Harmful Fungi - The present invention relates to a method of inducing plant tolerance to harmful fungi comprising the application to the plants, the soil, in which the plant grows or is to be grown and/or the seeds of the plant, of an effective amount of an active compound that inhibits the mitochondrial breathing chain at the level of the b/c | 2008-11-20 |
20080287427 | Bicyclic Amides as Kinase Inhibitors - The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising en a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases. | 2008-11-20 |
20080287428 | Novel Heterocyclidene Acetamide Derivative - A compound represented by formula (I′): | 2008-11-20 |
20080287429 | Dissolution of Arterial Cholesterol Plaques by Pharmacologically Induced Elevation of Endogenous Bile Salts - A group of pharmaceutical substances induce elevation of endogenous bile salts and acids via different mechanisms. The elevated circulating bile salts exert a beneficial effect in atherosclerosis by acting both as atherolytic and antiatherogenic agents. The result of the elevated circulating endogenous bile salt is the dissolution of cholesterol/lipidic aggregates of the atherosclerotic plaques. | 2008-11-20 |
20080287430 | Furan Compounds Useful As Ep1 Receptor Antagonists - Compounds of formula (I) or a pharmaceutically acceptable derivative thereof | 2008-11-20 |
20080287431 | Heterocyclic Compound and Anti-Malignant-Tumor Agent Containing the Same as Active Ingredient - Heterocyclic compounds represented by the formula I and anti-malignant-tumor agents containing the heterocyclic compounds as effective components: | 2008-11-20 |
20080287432 | Compounds and Compositions as Protein Kinase Inhibitors - The invention provides a novel class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the AbI, Bcr-AbI, Aurora-A, SGK, Tie-2, Trk-B, FGFR3, c-kit, b-RAF, c-RAF, DYRK2, Fms, Fyn and PDGFRalpha and PDGFR&bgr; kinases. | 2008-11-20 |
20080287433 | DERIVATIVES OF ARTEMISININ, AND THEIR USES IN THE TREATMENT OF MALARIA - A new artemisinin derivatives, of following general formula (I): | 2008-11-20 |
20080287434 | New amino-alkyl-amide derivatives as CCR3 receptor ligands - The invention relates to a compound of the general formula (I), | 2008-11-20 |
20080287435 | Active Ingredient Combinations Having Insecticide and Acaricide Properties - The novel active compound combinations of certain cyclic ketoenols and ethiprole have very good insecticidal and acaricidal properties. | 2008-11-20 |
20080287436 | Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof - The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. More specifically, the invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. | 2008-11-20 |
20080287437 | Pyrazolylaminopyrimidine Derivatives Useful as Tyrosine Kinase Inhibitors - This invention relates to novel compounds having the formula (I): | 2008-11-20 |
20080287438 | Agent for preventing or treating neuropathy - The present invention provides an agent for preventing or treating neuropathy having superior action and low toxicity. This agent comprises a compound represented by the formula: wherein ring A is a 5-membered aromatic heterocycle containing 2 or more nitrogen atoms, which may further have substituent(s); B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a divalent acyclic hydrocarbon group; Z is —O—, —S—, —NR | 2008-11-20 |
20080287439 | Pyrimidine compounds - The present invention relates to substituted pyrimidines of formula I, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders and/or viral disorders. | 2008-11-20 |
20080287440 | Novel Antifungal Triazole Derivatives - Disclosed herein are antifungal triazole derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same. The triazole derivatives of Chemical Formula 1 or pharmaceutically acceptable salts thereof according to the present invention have excellent inhibitory activity against a broad spectrum of fungi, in addition to being safe to the body, and thus are very useful in the treatment and prevention of fungal infection. | 2008-11-20 |
20080287441 | ALPHA-(TRIFLUOROMETHYL-SUBSTITUTED ARYLOXY, ARYLAMINO, ARYLTHIO OR ARYLMETHYL)-TRIFLUOROMETHYL-SUBSTITUTED PHENYLACETIC ACIDS AND DERIVATIVES AS ANTIDIABETIC AGENTS - Compounds having a formula: | 2008-11-20 |
20080287442 | Organic Compounds - 14-O—[(((C | 2008-11-20 |
20080287443 | Treatment of Subgingival Pocket Infections - Use of a morpholino compound having the general formula (I) wherein R1 is a straight or branched alkyl group containing (8) to (16) carbon atoms at the 2- or 3-position of the morpholino ring, and R2 is a straight or branched alkyl group containing (2) to (10) carbon atoms, substituted with a hydroxy group except in the alpha-position, or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment of an infected sub-gingival pocket. | 2008-11-20 |
20080287444 | PYRAZOLE COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS - This invention describes novel pyrazole compounds of formula III: | 2008-11-20 |