41st week of 2009 patent applcation highlights part 42 |
Patent application number | Title | Published |
20090253635 | PEPTIDES AND PEPTIDOMIMETICS HAVING ANTI-PROLIFERATIVE ACTIVITY AND/OR THAT AUGMENT NUCLEIC ACID DAMAGING AGENTS OR TREATMENTS - This invention provides compounds including peptides and peptidomimetics that can be used to treat cell proliferative disorders, such as those associated with benign and malignant tumor cells. While the invention is not limited to any particular mechanism, the compounds of the invention appear to function at least in part by inhibiting G2 cell cycle checkpoint. Thus, invention compounds can be used to inhibit cell growth alone or be used in combination with a nucleic acid damaging treatment to inhibit cell growth. | 2009-10-08 |
20090253636 | Novel Antifungal Agent - It is intended to provide a novel peptide which can exert higher antifungal effect also on a patient whose organ function is impaired with no side effect problems. The peptide comprises the following amino acid sequence: (1) SEQ ID NO:1: Lys-Arg-Leu-Phe-Arg-Arg-Trp-Gln-Trp-Arg-Tyr, (2) SEQ ID NO:2: Arg-Arg-Trp-Gln-Trp-Arg-Met-Lys-Lys-Tyr, (3) SEQ ID NO:3: Lys-Arg-Trp-Gln-TTp-Arg-Leu-Tyr, or (4) SEQ ID NO:4: Lys-Arg-Leu-Phe-Lys-Tyr, an antifungal agent comprising the peptide, a composition having a fungicidal and/or growth inhibitory action against fungus containing an effective amount of the peptide as an active ingredient, a medical apparatus/device which contains the peptide, whereby a fungicidal action is conferred, and a fungicidal and/or growth inhibiting method against fungus comprising administering the peptide and the like. | 2009-10-08 |
20090253637 | SMALL PEPTIDES FOR THE TREATMENT OF ALZHEIMER'S DISEASE AND OTHER BETA-AMYLOID PROTEIN DISORDERS - Use of a peptide or pharmaceutical composition comprising Leu-Ala-Phe-Val-Leu-Arg-Lys-amide having at least one D amino acid for the reduction of beta-amyloid protein, modulating APP processing, modulating activity of APP secretases, treatment of beta-amyloid protein diseases and the treatment of Alzheimer's disease. | 2009-10-08 |
20090253638 | Somatostatin Antagonists - The invention features somatostatin antagonists having a D-amino acid at the second residue. | 2009-10-08 |
20090253639 | OPIORPHIN PEPTIDE DERIVATIVES AS POTENT INHIBITORS OF ENKEPHALIN-DEGRADING ECTOPEPTIDASES - The present invention relates to modified opiorphin peptides as new inhibitors of metallo-ectopeptidases. | 2009-10-08 |
20090253640 | INHIBITORS OF POLYISOPRENYLATED METHYLATED PROTEIN METHYL ESTERASE - Inhibitors of the enzyme prenylated methylated protein methyl esterase (PMPMEase), the last step in the prenylation process for many eukaryotic proteins, having the general structure R | 2009-10-08 |
20090253641 | METHODS FOR PREVENTING OR TREATING INSULIN RESISTANCE - The invention provides methods of preventing or treating insulin resistance in a mammalian subject. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide having at least one net positive charge; a minimum of four amino acids; a maximum of about twenty amino acids; a relationship between the minimum number of net positive charges (p | 2009-10-08 |
20090253642 | MIMICKING THE METABOLIC EFFECTS OF CALORIC RESTRICTION BY ADMINISTRATION OF GLUCOSE ANTI-METABOLITES - Methods of maintaining and/or attenuating a decline in the quality of life of a mammal comprising the step of administering to the mammal a composition comprising an effective amount of mannoheptulose wherein the effective amount of mannoheptulose provides a dosage to the mammal on a daily basis from about 0.001 gram per kilogram of body weight of the mammal to about 1 gram per kilogram of body weight of the mammal. | 2009-10-08 |
20090253643 | EQUOL LEVEL REGULATOR - An object of the invention is to provide a medical drug, a food and drink having a role in regulating the concentration of equal in vivo and being capable of taking for a long time with high safety and provide a selective medium for a microorganism having conversion ability to equal and a method of detecting the same. Provided are an equal concentration-raising or reducing agent containing a carbohydrate as an active ingredient; use of a carbohydrate for producing the equal concentration-raising or reducing agent; a method of raising or reducing the concentration of equal by administrating a carbohydrate in an effective dose; a selective medium containing a carbohydrate for a microorganism having conversion ability to equal; and a method of detecting a microorganism having conversion ability to equal by use of the selective medium. | 2009-10-08 |
20090253644 | Radiosensitizer - A radiosensitizer comprising, as an active ingredient, at least one kind of compound selected from the group consisting of a compound represented by the following general formula ( | 2009-10-08 |
20090253645 | METHODS AND MATERIALS FOR TREATING AND PREVENTING INFLAMMATION OF MUCOSAL TISSUE - The invention involves methods and materials for treating and preventing non-invasive fungus-induced mucositis. Specifically, the invention involves administrating an antifungal agent such that it contact mucus in an amount, at a frequency, and for a duration effective to prevent, reduce, or eliminate non-invasive fungus-induced rhinosinusitis. This invention also provides methods and materials for diagnosing non-invasive fungus-induced rhinosinusitis and culturing non-invasive fungus from a mammalian mucus sample as well as specific antifungal formulations and medical devices for treating and preventing non-invasive fungus-induced rhinosinusitis. In addition, the invention provides methods and materials for treating and preventing other non-invasive fungus-induced mucositis conditions such as chronic otitis media, chronic colitis, and Crohn's disease. Further, the invention involves methods and materials for treating and preventing chronic asthma symptoms. | 2009-10-08 |
20090253646 | PAN-SELECTIN INHIBITOR WITH ENHANCED PHARMACOKINETIC ACTIVITY - Compounds, compositions and methods are provided for treatment of diseases or complications associated therewith, in which a selectin plays a role. More specifically, particular glycomimetics and uses thereof are described. For example, use of particular glycomimetics for treating sickle cell disease or a cancer involving a selectin, or complications associated with either, is described. | 2009-10-08 |
20090253647 | 2-PROPYNYL ADENOSINE ANALOGS WITH MODIFIED 5'-RIBOSE GROUPS HAVING A2A AGONIST ACTIVITY - The invention provides compounds having the following general formula (I): | 2009-10-08 |
20090253648 | Tricyclic-Nucleoside Compounds for Treating Viral Infections - Disclosed are compounds represented by formulae I, II, and III, and the compositions and methods thereof for treating viral infections caused by a Flaviviridae family virus. | 2009-10-08 |
20090253649 | Agents Containing Folic Acid, Vitamin B6 and Vitamin B12, and the Use Thereof - (EN) The invention relates to agents that contain folic acid, vitamin B6 and vitamin B12. and to the use thereof in hyperhomocysteinemia for controlling homocysteine levels. The agents are mainly suitable for the preventive and acute treatment of vascular diseases, of pregnant women and neurodegenerative diseases and are particularly advantageous in cases where the homocysteine levels to be controlled are found in an individual suffering from renal failure or being treated with immune suppressors. The invention particularly relates to pharmaceutical agents and food supplements comprising a corresponding active ingredient combination and to agents in the form of commercial packages containing corresponding combination preparations or monopreparations for the combined use. | 2009-10-08 |
20090253650 | Teat antiseptic prepared from polysaccharide gel with bactericidal and immuno-stimulating activity isolated from durian fruit-rind - A teat antiseptic having bactericidal activity against bacteria causing bovine mastitis. A post-milking teat dip and teat seal were prepared using polysaccharide gel with bactericidal, immuno-stimulating and wound healing activity isolated from durian fruit rind as active ingredient. | 2009-10-08 |
20090253651 | DRUG DELIVERY SYSTEM BASED ON REGIOSELECTIVELY AMIDATED HYALURONIC ACID - New drug delivery systems (DDS) are described containing hyaluronic acid and a therapeutic agent, wherein the therapeutic agent is linked, directly or via a linker, to 6-aminohyaluronic acid and where the linkage of the drug or linker with 6-aminohyaluronic acid is realised by an amide bond. Preferred therapeutic agents for use in the present DDS are anti-inflammatory, antibiotic, antitumor drugs. Preferred linkers are: succinic acid, succinic acid linked to aminoacids, succinic acid linked to peptides. The DDS are stable and free of undesired reaction by-products and impurities, and show a high level of pharmacological efficacy. | 2009-10-08 |
20090253652 | PHOSPHATE-BINDING CHITOSAN AND USES THEREOF - The present invention provides compositions and methods for removing phosphate from a subject using chitosan. The present invention also provides compositions and methods for treating hyperphosphatemia based on phosphate-binding chitosan. | 2009-10-08 |
20090253653 | ANALOGS OF BENZOQUINONE-CONTAINING ANSAMYCINS AND METHODS OF USE THEREOF - The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting 17-ammonium hydroquinone ansamycin analog. | 2009-10-08 |
20090253654 | CHOLINERGIC ENHANCERS WITH IMPROVED BLOOD-BRAIN BARRIER PERMEABILITY FOR THE TREATMENT OF DISEASES ACCOMPANIED BY COGNITIVE IMPAIRMENT - The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g., galantamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugs”, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments. | 2009-10-08 |
20090253655 | QUINOLINONE FARNESYL TRANSFERASE INHIBITORS FOR THE TREATMENT OF SYNUCLEINOPATHIES AND OTHER INDICATIONS - Novel quinolinone farnesyl transferase inhibitors are provided. These new compounds are useful in the treatment or prevention of synucleinopathies, such as Parkinson's Disease, Diffuse Lewy Body Disease, multiple system atrophy, and disorders of brain iron concentration including pantothenate kinase-associated neurodegeneration (e.g., PANK1), or other neurodegenerative/neurological diseases. Provided compounds are also useful in the treatment of proliferative diseases such as cancer, and in the treatment of neurological diseases, such as cognitive impairment, depression, and anxiety. | 2009-10-08 |
20090253656 | BCRP/ABCG2 INHIBITOR - The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. | 2009-10-08 |
20090253657 | Use of Clodronic Acid for Treatment Podotrochlosis - The invention describes the use of clodronic acid, its addition salts or esters as active ingredient for the preparation of a pharmaceutical for treating podotrochlosis with associated osteoporosis in horses. | 2009-10-08 |
20090253658 | Fat Accumulation Inhibitor - To provide a fat accumulation inhibitor and a food or drink for inhibiting fat accumulation, a visceral fat accumulation inhibitor and a food or drink for inhibiting visceral fat accumulation, or an agent for accelerating increase and/or inhibiting decrease of an adiponectin concentration in blood and a food or drink for accelerating increase and/or inhibiting decrease of an adiponectin concentration in blood. | 2009-10-08 |
20090253659 | Cycloalkylidene Compounds As Modulators of Estrogen Receptor - The present invention relates to novel compounds with a variety of therapeutic uses, more particularly novel substituted cyclic alkylidene compounds that are particularly useful for selective estrogen receptor modulation. | 2009-10-08 |
20090253660 | Minocycline Compounds and Methods of Use Thereof - Methods and compositions for using a tetracycline compound to treat bacterial infections are described. In one embodiment, for example, the invention provides a method of treating a subject for an infection, comprising administering to said subject an effective amount of 9-[(2,2-dimethyl-propyl amino)-methyl]-minocycline or a salt thereof, such that said subject is treated, wherein said infection is selected from the group consisting of MSSA, MRSA, B-streptococci, Viridans Streptococci, | 2009-10-08 |
20090253661 | OCULAR AGENTS - A method to reduce or ameliorate an ocular condition, such as ocular scarring that may occur after ocular surgery or another non-surgical ocular inflammatory or other condition, by topically administering doxycycline as the sole active agent to a patient in need thereof under conditions to reduce or ameliorate the ocular condition. | 2009-10-08 |
20090253662 | GENETIC RISK ASSESSMENT IN HEART FAILURE: IMPACT OF GENETIC VARIATION OF ALDOSTERONE SYNTHASE PROMOTER POLYMORPHISM - The invention provides methods for (a) reducing mortality associated with heart failure; (b) improving oxygen consumption; (c) treating heart failure; (d) treating hypertension; (e) improving the quality of life in a heart failure patient; (f) inhibiting left ventricular remodeling; (g) reducing hospitalizations related to heart failure; (h) improving exercise tolerance; (j) increasing left ventricular ejection fraction; (Ic) decreasing levels of B-type natriuretic protein; (l) treating renovascular diseases; (m) treating end-stage renal diseases; (n) reducing cardiomegaly; (o) treating diseases resulting from oxidative stress; (p) treating endothelial dysfunctions; (q) treating diseases caused by endothelial dysfunctions; or (r) treating cardiovascular diseases; in a patient in need thereof, wherein the patient has a −344 (T/T) polymorphism or a −344 (C/C) polymorphism in an aldosterone synthase CYP11B2 gene, comprising administering to the patient (i) at least one antioxidant compound or a pharmaceutically acceptable salt thereof; (ii) at least one nitric oxide enhancing compound; and (iii) optionally the best current therapy for the treatment of cardiovascular diseases. In one embodiment the antioxidant is a hydralazine compound or a pharmaceutically acceptable salt thereof and the nitric oxide enhancing compound is isosorbide dinitrate and/or isosorbide mononitrate. | 2009-10-08 |
20090253663 | SKIN EXTERNAL PREPARATION CONTAINING TRITERPENIC ACID - Disclosed is a skin external preparation containing a triterpenic acid typified by ursolic acid. For obtaining a skin external preparation having excellent storage stability by improving the dissolution stability of the triterpenic acid and the like, 4-alkylresorcinol such as 4-n-butylresorcinol is added into a skin external preparation containing a triterpenic acid and the like such as benzyl ursolate. | 2009-10-08 |
20090253664 | COMBINATION ANDOLAST/GLUCOCORTICOIDS - The invention relates to the combination of Andolast, a calcium-activated potassium channel opener and glucocorticoids for the treatment of patients suffering for airway diseases. Pharmaceutical compositions comprising Andoalst and glucocorticoids are also disclosed. | 2009-10-08 |
20090253665 | METHOD OF TREATMENT OF DISEASE USING AN ADENOSINE A1 RECEPTOR ANTAGONIST AND AN ALDOSTERONE INHIBITOR - Pharmaceutical compositions comprising an aldosterone inhibitor and an adenosine A | 2009-10-08 |
20090253666 | COMPOSITION COMPRISING SARSASAPOGENIN - The présent invention relates to a composition comprising sarsasapogenin or a plant extract containing it in order to improve the gêneral state of the skin and in particular to improve and/or embellish any part of the body showing a déficit in lipids. More particularly, the invention is directed to a cosmetic method to improve the figure, comprising the step of topically applying to the skin a cosmetic or dermopharmaceutical composition comprising sarsasapogenin to favour the expansion and/or the formation of the subcutaneous adipose tissue, and/or to favour the lipid synthesis in the epidermis. | 2009-10-08 |
20090253667 | 18 ,21-Didesoxymacbecin Derivatives for the Treatment of Cancer - The present invention relates to 18,21-didesoxymacbecin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pre-treatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies. | 2009-10-08 |
20090253668 | Hair Loss Prevention by Natural Amino Acid and Peptide Complexes - This invention relates to certain skin and hair care agents of formula (I), derived from natural amino acids and peptides. These agents provide multi-functional treatment of enzyme-related skin, hair and scalp problems, for example, hair aging including premature hair loss and hair graying; male pattern baldness; hair loss from dandruff; alopecia; split ends, acne, darkened skin, dark circles around eyes, stretch marks, wrinkles and fine lines, loss of collagen, loss of skin pliability and combinations thereof: | 2009-10-08 |
20090253669 | Substituted Sulfonamide Compounds - Substituted sulfonamide compounds corresponding to the formula I: | 2009-10-08 |
20090253670 | AMIDE DERIVATIVES AS POSITIVE ALLOSTERIC MODULATORS AND METHODS OF USE THEREOF - The invention relates to novel amide derivatives that are positive allosteric modulators of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions. | 2009-10-08 |
20090253671 | TRICYCLIC DERIVATIVES OF AZETIDINE AND PYRROLE WITH ANTIBACTERIAL ACTIVITY - Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described. | 2009-10-08 |
20090253672 | Cathepsin Cysteine Protease Inhibitors - This invention relates to a novel class of compounds, represented by the formula (I) below, wherein the meanings of R1, R2, R3, R4, R5, R6, R7, X and Y are indicated therein, which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsms K L, S and B These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis, osteoarthritis and rheumatoid arthritis | 2009-10-08 |
20090253673 | Substituted Pyrazoles as Ghrelin Receptor Antagonists - Certain novel N-acylated spiropiperidine derivatives are ligands of the human ghrelin receptor(s) and, in particular, are antagonists/inverse agonists of the human ghrelin receptor. They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of the ghrelin receptor, such as obesity, diabetes, and metabolic syndrome. | 2009-10-08 |
20090253674 | Substituted Triazole Derivatives As Oxytocin Antagonists - The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction. | 2009-10-08 |
20090253675 | PHARMACEUTICAL FORMULATION - The instant invention provides a pharmaceutical composition comprised of a cholesterol absorption inhibitor and an HMG-CoA reductase inhibitor, one or more anti-oxidants, microcrystalline cellulose, hydroxypropyl methylcellulose, magnesium stearate and lactose. The composition need not contain ascorbic acid in order to obtain desirable stability. | 2009-10-08 |
20090253676 | Heteroaryl Benzamide Derivatives for Use as GLK Activators in the Treatment of Diabetes - Compounds of Formula (I): | 2009-10-08 |
20090253677 | HIV Integrase Inhibitors - The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV. | 2009-10-08 |
20090253678 | MACROCYCLIC PYRIMIDINE DERIVATIVES - Macrocyclic pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions, and disorders using such compounds and compositions are described herein. | 2009-10-08 |
20090253679 | NEW IMIDAZOLONE DERIVATIVES, PREPARATION THEREOF AS DRUGS, PHARMACEUTICAL COMPOSITIONS, AND USE THEREOF AS PROTEIN KINASE INHIBITORS, IN PARTICULAR CDC7 - The present invention relates to imidazolone derivatives of formula (I) | 2009-10-08 |
20090253680 | SELECTED CGRP-ANTAGONISTS, PROCESSES FOR PREPARING THEM AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to the CGRP-antagonists of general formula I | 2009-10-08 |
20090253681 | HIV Integrase Inhibitors - Compounds of Formula I are inhibitors of FHV integrase and inhibitors of FHV replication (I), wherein m, n, X, R | 2009-10-08 |
20090253682 | HETEROCYCLIC DERIVATIVES FOR MODULATION OF CALCIUM CHANNELS - Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions. | 2009-10-08 |
20090253683 | 7-MEMBERED RING COMPOUND AND METHOD OF PRODUCTION AND PHARMACEUTICAL APPLICATION THEREOF - A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved: | 2009-10-08 |
20090253684 | LEUKOTRIENE B4 INHIBITORS - Provided herein are compounds of the formula (I): | 2009-10-08 |
20090253685 | Product comprising at least one Cdc25 phosphatase inhibitor in combination with at least one other anti-cancer agent - A subject of the invention is a product comprising at least one Cdc25 phosphatase inhibitor in combination with at least one other anti-cancer agent for a therapeutic use which is simultaneous, separate or spread over time in the treatment of cancer. | 2009-10-08 |
20090253686 | UNSOLVATED BENZODIAZEPINE COMPOSITIONS AND METHODS - The present invention relates to systems and methods for generating new forms of benzodiazepine and benzodiazepine related compounds as well as new compounds and formulations generated by such methods. In particular, the present invention provides high throughput systems and methods for generating and identifying new crystalline benzodiazepine and benzodiazepine related polymorphs and new unsolvated, solvated, and other forms of the compounds that find use as improved drugs and drug formations. | 2009-10-08 |
20090253687 | Fused Heterocyclic Compounds and Their Use as Mineralocorticoid Receptor Ligands - The present invention relates to wherein each symbol is as defined in the specification. The compound has a superior mineral corticoidreceptorantagonistic action and is useful as an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like, a compound having a fused heterocycle, or a prodrug thereof, or a salt thereof; and an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like. | 2009-10-08 |
20090253688 | Semicarbazide derivatives as kinase inhibitors - The present invention relates to semicarbazide derivatives of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient. | 2009-10-08 |
20090253689 | Organic Compounds - New compounds of the Formula (I): | 2009-10-08 |
20090253690 | PHARMACEUTICALLY EFFECTIVE COMPOUNDS - The subject invention relates to carboxamidine derivatives, to pharmaceutical compositions containing the carboxamidine derivatives of the invention, and the use thereof for the treatment of vascular diseases and in the preparation of pharmaceutical compositions for the treatment of vascular diseases. | 2009-10-08 |
20090253691 | TRISUBSTITUTED 1,2,4-TRIAZOLES - The present invention relates to 3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). | 2009-10-08 |
20090253692 | CRYSTALLINE FORM OF N-[[4-FLUORO-2-(5-METHYL-1H-1,2,4-TRIAZOL-1-YL)PHENYL]METHYL]-4,6,7,9-TET- RAHYDRO-3-HYDROXY-9,9-DIMETHYL-4-OXO-PYRIMIDO[2,1-C][1,4]OXAZINE-2-CARBOXA- MIDE, SODIUM SALT MONOHYDRATE - Disclosed is a crystalline form of N-[[4-fluoro-2-(5-methyl-1H-1,2,4-triazol-1-yl)phenyl]methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide, sodium salt monohydrate. Also disclosed are at least one pharmaceutical composition comprising at least one crystalline form of N-[[4-fluoro-2-(5-methyl-1H-1,2,4-triazol-1-yl)phenyl]methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide, sodium salt monohydrate, and at least one method of using at least one crystalline form of N-[[4-fluoro-2-(5-methyl-1H-1,2,4-triazol-1-yl)phenyl]methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide, sodium salt monohydrate to treat AIDS or HIV infection. | 2009-10-08 |
20090253693 | 2H-BENZO[b][1,4]OXAZIN-3(4H)-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: | 2009-10-08 |
20090253694 | Fused hetrocyclic compounds - This invention provides fused heterocyclic compounds, pharmaceutical compositions of the compounds, and methods of using the compounds for the treatment of, inter alia, IL-12 related disease and disorders. | 2009-10-08 |
20090253695 | Hydroxyalkyl Substituted Imidazonaphthyridines - Certain imidazonaphthyridines with a hydroxymethyl or hydroxyethyl substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for preferentially inducing IFN-α biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed. | 2009-10-08 |
20090253696 | SUBSTITUTED PYRIDO(3,2-D) PYRIMIDINES AND PHARMACEUTICAL COMPOSITIONS FOR TREATING VIRAL INFECTIONS - This invention provides di-, tri- and tetra-substituted pyrido(3,2-d)pyrimidine derivatives with specific substituting patterns, their pharmaceutically acceptable salts, N-oxides, solvates, pro-drugs and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular being highly active antiviral agents. The invention also provides use of such derivatives in the treatment of viral infections and pathologic conditions associated therewith, including hepatitis C. | 2009-10-08 |
20090253697 | Novel Indole Derivatives, Preparation Thereof as Medicinal Products and Pharmaceutical Compositions, and Especially as KDR Inhibitors - The disclosure relates to compounds of formula (I): | 2009-10-08 |
20090253698 | Brain, Spinal and Nerve Injury Treatment - A treatment for brain, spinal and nerve injury comprising use of a substance P receptor antagonist optionally in combination with a magnesium compound. There is also provided a formulation for use in this treatment comprising a substance P receptor antagonist and a magnesium compound. | 2009-10-08 |
20090253699 | Compounds for Nonsense Suppression, and Methods for Their Use - The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA. | 2009-10-08 |
20090253700 | N-'4-4(4-MORPHOLINYL) PHENYL!- '(4-PIPERIDINYL) METHYL! CARBOXAMIDE DERIVATIVES AND THEIR USE AS GLYCINE TRANSPORTER INHIBITORS - The invention provides a compound of formula (I) or a salt or solvate thereof: | 2009-10-08 |
20090253701 | ORGANIC COMPOUNDS - Disclosed are δ-amino-γ-hydroxy-ω-aryl-alkanoic acid amide compounds of formula (I) | 2009-10-08 |
20090253702 | FAST ACTING NARATRIPTAN COMPOSITION - The present invention relates to pharmaceutical compositions containing Naratriptan, a compound selected from the group consisting of 2-HPOD, 2-HPHM, 4-PPED, 4-BPED and 2-PPED, and optionally, a pharmaceutically acceptable excipient. | 2009-10-08 |
20090253703 | ORGANIC COMPOUNDS - Disclosed are δ-amino-γ-hydroxy-ω-aryl-alkanoic acid amide compounds of formula (I) | 2009-10-08 |
20090253704 | PYRROLOTRIAZINONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses pyrrolotriazinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: | 2009-10-08 |
20090253705 | HYDROXYMETHYL PYRROLIDINES AS BETA 3 ADRENERGIC RECEPTOR AGONISTS - The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor. | 2009-10-08 |
20090253706 | Methods and Compositions for the Treatment of Rheumatoid Arthritis and Other Inflammatory Diseases - Compositions and methods for the treatment of inflammatory diseases are disclosed. | 2009-10-08 |
20090253707 | HETEROANNELATED ANTHRAQUINONE DERIVATIVES AND THE SYNTHESIS METHOD THEREOF - A heteroannelated anthraquinone derivative compound is provided. The heteroannelated anthraquinone derivative compound is represented by a formula (I): | 2009-10-08 |
20090253708 | 2-ALKYNYL-6-PYRIDIN-2-YL-PYRIDAZINONES, 2-ALKYNYL-6-PYRIDIN-2-YL-DIHYDROPYRIDAZINONES, 2-ALKYNYL-6-PYRIMIDIN-2-YL-PYRIDAZINONES AND 2-ALKYNYL-6-PYRIMIDIN-2-YL-DIHYDROPYRIDAZINONES AND THEIR USE AS FUNGICIDES - This invention relates to certain novel 2-alkynyl-6-pyridin-2-yl-pyridazinones, 2-alkynyl-6-pyridin-2-yl-dihydropyridazinones, 2-alkynyl-6-pyrimidin-2-yl-pyridazinones and 2-alkynyl-6-pyrimidin-2-yl-dihydropyridazinones and to the use of these compounds for control of fungal pathogens of plants and mammals. | 2009-10-08 |
20090253709 | SYNTHESIS, TELOMERASE INHIBITION AND CYTOTOXIC STUDIES ON 2,7-DISUBSTITUTED ANTHRAQUINONE DERIVATIVES - An series of 2,7-disubstituted anthraquinone derivatives including a formula I are provided. | 2009-10-08 |
20090253710 | NMDA Receptor Antagonists for Neuroprotection - Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: | 2009-10-08 |
20090253711 | HETEROCYCLYL-3-SULFONYLINDAZOLES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS - The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor. | 2009-10-08 |
20090253712 | AQUEOUS SOLVENT SYSTEM FOR SOLUBILIZATION OF AZOLE COMPOUNDS - A pharmaceutical composition includes: | 2009-10-08 |
20090253714 | Methods of reducing risk of infection from pathogens - Prophylactic treatment methods are provided for protection of individuals and/or populations against infection from airborne pathogens. In particular, prophylactic treatment methods are provided comprising administering amiloride, benzamil, phenamil or pharmaceutically acceptable salts thereof to one or more members of a population at risk of exposure to or already exposed to one or more airborne pathogens, either from natural sources or from intentional release of pathogens into the environment. | 2009-10-08 |
20090253715 | HETEROARYL-CONTAINING ISOFLAVONES AS AROMATASE INHIBITORS - Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I: | 2009-10-08 |
20090253716 | AMINO-IMIDAZOLONES FOR THE INHIBITION OF BETA-SECRETASE - The present invention provides an amino-imidazolone compound of formula I | 2009-10-08 |
20090253717 | Inhibitors of p97 - One aspect of the invention relates to compounds that inhibit the activity of p97, such as by binding covalently to a cysteine residue in the active site. In certain embodiments, the invention relates to the treatment of disease, such as cancer, comprising administering a compound of the invention. | 2009-10-08 |
20090253718 | Pharmaceutical Compounds - The invention provides a compound having the formula (I): | 2009-10-08 |
20090253719 | CRYSTALLINE SALT FORMS OF ANTIFOLATE COMPOUNDS AND METHODS OF MANUFACTURING THEREOF - The present invention provides methods of preparing antifolate compounds. The inventive methods can particularly be use for preparing compounds exhibiting improved bioavailability, making the compound particularly useful in pharmaceutical compositions. The compounds prepared according to the inventive methods are useful in the treatment of multiple conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis. | 2009-10-08 |
20090253720 | ANTIFOLATE COMPOSITIONS - The present invention provides pharmaceutical compositions comprising an antifolate compound. The composition exhibit improved bioavailability, and they particularly incorporate beneficial excipients that increase solubility and bioavailability, such as cyclodextrins or compounds formed of fatty acid esters of glycerol and polyethylene glycol esters. The pharmaceutical compositions are useful in the treatment of multiple conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis. | 2009-10-08 |
20090253721 | Combined treatment with radiation and an epidermal growth factor receptor kinase inhibitor - The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient a therapeutically effective amount of an EGFR kinase inhibitor, combined with treating the patient simultaneously or sequentially with radiation therapy, with or without additional agents or treatments, such as other anti-cancer drugs. A preferred example of an EGFR kinase inhibitor that can be used in practicing this invention is the compound erlitinib HCl (also known as Tarceva™). | 2009-10-08 |
20090253722 | AQUEOUS PHARMACEUTICAL FORMULATION - The invention concerns a stable aqueous pharmaceutical composition comprising 5-[(2RS)-2-cyclopropyl-7,8-dimethoxy-2H-1-benzopyran-5-ylmethyl]-pyrimidine-2,4-diamine in form of the water soluble methanesulfonic acid salt, a physiological sodium chloride solution, ethanol and Povidone 12 PF, the liquid having a pH of over and above 4.8, but not higher than 5.2, and wherein the oxygen amount is controlled to be 0.8 ppm or less; which can be sterilized by filtration and/or by heated treatment, stored for longer time periods and which can be use for bolus injection or diluted for i.v. infusion. | 2009-10-08 |
20090253723 | PROTEIN KINASE INHIBITORS - Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed. | 2009-10-08 |
20090253724 | THERAPEUTIC OR PROPHYLACTIC AGENT FOR LEUKEMIA - A therapeutic or prophylactic agent for leukemia is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for leukemia according to the present invention shows the excellent absorbability and in vivo stability when orally administered, and exhibits prominent therapeutic or prophylactic effects. | 2009-10-08 |
20090253725 | ACETYL CoA CARBOXYLASE INHIBITORS - The present invention relates to acetyl coenzyme-A carboxylase (“ACC”) inhibiting compounds of the formula | 2009-10-08 |
20090253726 | TRI-, TETRA-SUBSTITUTED-3-AMINOPYRROLIDINE DERIVATIVE - A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided. The compound provided is represented by formula (I): | 2009-10-08 |
20090253727 | NOCICEPTIN ANALOGS - A compound of the having the general formula (I) or general formula (II): | 2009-10-08 |
20090253728 | Methods and Compositions for Treating Nociceptive Pain - The present invention provides methods and compositions useful for the treatment and prevention of pain. | 2009-10-08 |
20090253729 | Analgesic Agent - A pharmaceutical preparation useful for alleviating or treating a pain, e.g., a chronic pain (particularly, a neuropathic pain) is provided. The pharmaceutical preparation contains (a) a propionic acid-derived nonsteroidal anti-inflammatory agent (e.g., ibuprofen), (b) a non-pyrazolone antipyretic analgesic agent (e.g., acetaminophen), and (c) an opioid analgesic agent (e.g., codeine phosphate, dihydrocodeine phosphate). The pharmaceutical preparation may contain 5 to 100 parts by weight of the antipyretic analgesic agent (b) or 0.5 to 500 parts by weight of the analgesic agent (c) relative to 100 parts by weight of the anti-inflammatory agent (a). The pharmaceutical preparation may be substantially free from a nontoxic N-methyl-D-aspartate receptor antagonist and may contain 20 to 80 parts by weight of the antipyretic analgesic agent (b) and 1 to 100 parts by weight of the analgesic agent (c) relative to 100 parts by weight of the anti-inflammatory agent (a). | 2009-10-08 |
20090253731 | Method of identifying therapeutic agents - The present invention relates to a method of identifying agents suitable for use in treating epilepsy and other brain disorders, including but not limited to bipolar disorder, schizophrenia and depression. The invention further relates to methods of treatment based on the use of agents so identifiable. | 2009-10-08 |
20090253732 | Production Of Polyketides And Other Natural Products - The present invention relates to production of polyketides and other natural products and to libraries of compounds and individual novel compounds. Therefore in aspect the present invention provides 17-desmethylrapamycin and analogues thereof, methods for their production, including recombinant strains, and isolation and uses of the compounds of the invention. In a further aspect the present invention provides for the use of 17-desmethylrapamycin and analogues thereof in the induction or maintenance of immunosuppression, the stimulation of neuronal regeneration or the treatment of cancer, B-cell malignancies, fungal infections, transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation vascular disease and fibrotic diseases, and in the regulation of wound healing. | 2009-10-08 |
20090253733 | RAPAMYCIN CARBONATE ESTERS - Certain embodiments include carbonate esters of rapamycin at position 42 that are synthesized by a lipase catalyzed regio-specific process. These compounds or a pharmaceutically acceptable salt thereof are useful in the treatment of organ and tissue transplant rejection, autoimmune disease, proliferative disorder, restenosis, cancer, or microbial infection. | 2009-10-08 |
20090253734 | INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. | 2009-10-08 |
20090253735 | 2-ARYL-6-PHENYLIMIDAZO[1,2-a]PYRIDINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The present invention is related to a compound of formula (I) | 2009-10-08 |
20090253736 | AZAINDOLE DERIVATIVES AS CFTR MODULATORS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 2009-10-08 |