52nd week of 2009 patent applcation highlights part 48 |
Patent application number | Title | Published |
20090318443 | KINASE INHIBITORS - The present invention provides kinase inhibitors of Formula I. | 2009-12-24 |
20090318444 | TETRAHYDRO- AND DIHYDROQUINAZOLINONES - The present invention relates to the use of tetrahydro- and dihydroquinazolinones of formula I as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases, their use for the manufacture of a pharmaceutical composition and new tetrahydro- and dihydroquinazolinones. | 2009-12-24 |
20090318445 | PDF INHIBITORS - The invention relates to novel compounds that are inhibitors of peptidyl deformylase (PDF). The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and uses of the compounds are also disclosed. | 2009-12-24 |
20090318446 | 4-(1H-Indol-3-yl)-Pyrimidin-2-Ylamine Derivatives and Their Use in Therapy - The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof. The present invention seeks to provide further substituted heteroaryl-substituted pyrimidine derivatives. More specifically, the invention relates to compounds that have broad therapeutic applications in the treatment of a number of different diseases and/or that are capable of inhibiting one or more protein kinases. | 2009-12-24 |
20090318447 | N-[6-(4-MORPHOLINYL)-3-PYRIDINYL]-2-(TETRAHYDRO-2H-PYRAN-4-YL)-N-[(1--4-PI- PERIDINYL) METHYL] ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS GLYT1 TRANSPORT INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL DISORDERS SUCH AS SCHIZOPHRENIA - The invention provides a compound of formula (I) or a salt or solvate thereof: | 2009-12-24 |
20090318448 | Inhibitors of Bruton's Tyrosine Kinase - This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: | 2009-12-24 |
20090318449 | THERAPEUTIC LACTAMS - Compounds comprising | 2009-12-24 |
20090318450 | 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. 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. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. | 2009-12-24 |
20090318451 | MORPHOLINE DOPAMINE AGONISTS FOR THE TREATMENT OF PAIN - The present invention relates to use of a compound of formula (I), (Ia), or (Ib): | 2009-12-24 |
20090318452 | INHIBITORS OF p38 - The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to inhibitors of ZAP70. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders. | 2009-12-24 |
20090318453 | POSTOPERATIVE ADJUVANT CHEMOTHERAPY FOR GASTRIC CANCER - The invention provides a method for treatment of gastric cancer, which method is a postoperative adjuvant chemotherapy for gastric cancer, comprising orally administering, to a patient with gastric cancer in stage II, IIIA, or IIIB in a classification of the stage of gastric cancer, a pharmaceutical composition containing Tegafur, Gimeracil, and Oteracil potassium at a molar ratio of 1:0.4:1, at a dose of 50 to 150 mg/day as Tegafur dose and according to an administration schedule including, from within 45 days after a surgical operation of gastric cancer, drug administration for 28 consecutive days, followed by a rest period of 7 to 14 consecutive days. | 2009-12-24 |
20090318454 | NOVEL ANTIOXIDANTS AND METHODS OF TREATMENT - Formula 1 is an antioxidant compound, wherein R, R1, or D is an antioxidant substituent; R and D are each independently selected from hydrogen or groups containing cysteine, thiols, disulfides, amino acids, amines, amides, or carboxylic acids; when one of R or D is hydrogen, the other includes a thiol, disulfide, or carboxylic acid; A is CO, SO, SO | 2009-12-24 |
20090318455 | COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS - Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system. | 2009-12-24 |
20090318456 | SUBSTITUTED PTERIDINES FOR THE TREATMENT AND PREVENTION OF VIRAL INFECTIONS - Tri-substituted pteridines and tetra-substituted pteridines exhibit a significant and selective activity against certain types of viral infections, in particular they selectively inhibit the replication of the hepatitis C virus, and are useful for the prevention and treatment of such infections. | 2009-12-24 |
20090318457 | Methods of Using hydrates and polymorphs of 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pterid- inyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide - Disclosed are hydrates and polymorphs of 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, processes for preparing them and their use as pharmaceutical compositions. | 2009-12-24 |
20090318458 | NOVEL COMPOUNDS AND USE THEREOF - A semiautomatic vehicle gearbox comprising, for said gearbox, a shift lever ( | 2009-12-24 |
20090318459 | Therapeutic Compositions Comprising a Specific Endothelin Receptor Antagonist and a PDE5 Inhibitor - The invention relates to a product containing the compound of formula (I) below | 2009-12-24 |
20090318460 | AMORPHOUS VARENICLINE TARTRATE AND PROCESS FOR THE PREPARATION THEREOF - The present invention generally relates to an amorphous form of varenicline and its pharmaceutically acceptable salts thereof. More particularly the present invention relates to amorphous forms of varenicline and its L-tartrate salt; a process for their preparation and pharmaceutical compositions comprising the same. | 2009-12-24 |
20090318461 | CRYSTALLINE POLYMORPHISM OF 5-METHYL-2-(PIPERAZIN-1-YL) BENZENESULFONIC ACID - The present invention provides novel crystals of 5-methyl-2-(piperazin-1-yl)benzenesulfonic anhydrate and monohydrate. | 2009-12-24 |
20090318462 | PROTEIN KINASE C ZETA INHIBITION TO TREAT VASCULAR PERMEABILITY - Methods of treating or preventing a disease or disorder in a subject are provided by the present invention which include administering a composition including a therapeutically effective amount of a protein kinase C (PKC) zeta inhibitor. A disease or disorder treated or prevented by administration of a PKC zeta inhibitor is characterized by abnormal vascular permeability. Diseases or disorders treated or prevented by administration of a composition including a therapeutically effective amount of a PKC zeta inhibitor include cancer, an ischemic condition and microvascular complications of a systemic or local condition in the subject, such as diabetes and/or diabetic macular edema. Additionally, methods of inhibiting PKC zeta are provided which include incubating PKC zeta in vivo, in vitro and/or in silico with a PKC zeta inhibitor. | 2009-12-24 |
20090318463 | Indolylmaleimide Derivatives - Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer. | 2009-12-24 |
20090318464 | New Pyridine Analogues V - The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y | 2009-12-24 |
20090318465 | METHOD FOR IDENTIFYING COMPOUNDS THAT ACT AS INSULIN-SENSITIZERS - The present invention relates to a method for identifying compounds that act as insulin-sensitizers. The method can include screening of test compounds in two assays of insulin sensitivity. This method can identify lead compounds for the treatment of disorders caused by insulin resistance to glucose uptake. This invention also includes methods for treating insulin resistance and related disorders. | 2009-12-24 |
20090318466 | COMPOUNDS USEFUL AS PESTICIDES - Compounds useful to control pests are provided. | 2009-12-24 |
20090318467 | NOVEL HETEROARYL CARBOXAMIDE DERIVATIVES - The invention is concerned with novel heteroaryl carboxamide derivatives of formula (I), | 2009-12-24 |
20090318468 | PYRAZOLE COMPOUNDS 436 - There is provided novel compounds of formula (Ia) or (Ib): | 2009-12-24 |
20090318470 | 1-SUBSTITUTED-3-(NAPHTHALEN-1-YLSULFONYL)-5-(PIPERAZIN-1-YL)-1H-INDAZOLE COMPOUNDS AS 5-HYDROXYTRYPTAMINE-6 LIGANDS - The disclosure is directed to compounds of Formula I: | 2009-12-24 |
20090318471 | New Salts and Crystalline Salt Forms of an Indolinone Derivative - The present invention relates to new salts and crystalline salt forms of an indolinone derivative which have valuable pharmacological properties, to a process for their manufacture, to pharmaceutical formulations containing them and to their use as medicament. | 2009-12-24 |
20090318472 | AMINOPYRAZINE DERIVATIVES AND COMPOSITIONS - The present invention relates to aminopyrazine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such aminopyrazine derivatives are useful in the treatment of diseases associated with inappropriate tyrosine and/or serine/threonine kinase activity. | 2009-12-24 |
20090318473 | 5,6-BISARYL-2-PYRIDINE-CARBOXAMIDE DERIVATIVES, PREPARATION AND APPLICATION THEREOF IN THERAPEUTICS AS UROTENSIN II RECEPTOR ANTAGONISTS - The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors. | 2009-12-24 |
20090318474 | PYRIDINE AND PYRIMIDINE DERIVATIVES AS MGLUR 2 ANTAGONISTS - The present invention relates to compounds of formula (I), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: | 2009-12-24 |
20090318475 | Novel, Acyclically Substituted Furopyrimidine Derivatives and Use Thereof - The present application relates to novel, acyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases. | 2009-12-24 |
20090318476 | Azacycloalkane Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase - Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis. Formula (I). | 2009-12-24 |
20090318477 | CHEMICAL COMPOUNDS - The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly Type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds. | 2009-12-24 |
20090318478 | QUINAZOLINE DERIVATIVES - The invention discloses quinazoline derivatives or salts thereof, which possess PDE9-inhibiting activity and are useful as treating agents of dysuria and the like, the derivatives being represented by the formula (I) | 2009-12-24 |
20090318479 | SUBSTITUTED RING FUSED AZINES AND THEIR USE IN CANCER THERAPY - The present invention relates to substituted ring fused azines and methods of using said compounds in treating cancers. More specifically, the present invention relates to the preparation of 4-alkyl-2-(heterocyclic)-azines and their use as cancer agents or drugs for cancer therapy. The compounds of the invention display favourable in vivo and in vitro activity against selected cancers. | 2009-12-24 |
20090318480 | METHOD FOR TREATING CANCER HARBORING EGFR MUTATIONS - The present invention relates to a method of treatment of patients suffering from cancer and harbouring mutations of EGFR in the tumour, for instance an activating mutation of the EGFR or a mutation responsible for resistance or the emergence of acquired resistance to treatment with reversible EGFR and/or HER2 inhibitors or irreversible inhibitors such as CI-1033, EKB-569, HKI-272 or HKI-357, comprising administering an effective amount of the irreversible EGFR inhibitor BIBW2992 (1) 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)-1-oxo-2-buten-1-yl]amino}-7-((S)-tetrahydrofuran-3-yloxy)-quinazoline, to a person in need of such treatment, optionally in combination with the administration of a further chemotherapeutic agent, in combination with radiotherapy, radio-immunotherapy and/or tumour resection by surgery, and to the use of a BIBW 2992 (1) for preparing a pharmaceutical composition for the treatment of patients suffering from cancer and harbouring mutations of EGFR in the tumour. | 2009-12-24 |
20090318481 | Potentiators Of Glutamate Receptors - This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. | 2009-12-24 |
20090318482 | TABLET PREPARATION WITHOUT CAUSING A TABLETING TROUBLE - The present invention provides a tablet without causing a tableting trouble, which is superior in the tablet formability, dissolution property of pharmaceutically active ingredient, and the like. | 2009-12-24 |
20090318483 | Potentiators Of Glutamate Receptors - This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. | 2009-12-24 |
20090318484 | Inhibitors of JNK - The invention relates to prodrugs of JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses prodrugs of JNK inhibitors, as described below in formula I: | 2009-12-24 |
20090318485 | NOVEL INHIBITORS OF RHO KINASE - The present invention relates to compounds and methods which may be useful as inhibitors of Rho kinase for the treatment or prevention of disease. | 2009-12-24 |
20090318486 | Tricyclic spiro derivatives as CRTH2 modulators - The present invention is related to the use of spiro derivatives of Formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of spiro derivatives for the modulation of CRTH2 activity. | 2009-12-24 |
20090318487 | Methods for detection of promoter polymorphism in a UGT gene promoter - The present invention is directed to methods for detecting the presence of genetic polymorphisms that correlate with altered gene expression. More specifically, the present invention is directed to methods for detecting the genetic polymorphisms located in the UGT1A1 promoter. The invention also provides methods for optimizing drug dosages based upon the presence of the polymorphisms. The invention further provides methods of predicting sensitivity to xenobiotics and diagnostic kits for detecting genetic polymorphisms. | 2009-12-24 |
20090318488 | Pharmaceutically acceprable salts of aporphine compounds of carboxyl group-containing agents and methods for preparing the same - The present invention discloses novel pharmaceutically acceptable salts of aporphine compounds and carboxyl-group containing agents. Also, the present invention discloses methods for preparing the pharmaceutically acceptable salts. These pharmaceutically acceptable salts are suitable for use in treating and/or preventing hyperglycemic disease and/or several oxidative stress related diseases. | 2009-12-24 |
20090318489 | Aporphine compounds and pharmaceutical use thereof - The present invention discloses novel aporphine derivatives. Also, the present invention discloses that these novel aporphine derivatives can be used for treating oxidative stress induced diseases such as cardiovascular disease, diabetes, aging, Alzheimer's disease, kidney disease, cancer or brain ischemic disease etc. | 2009-12-24 |
20090318490 | COMPOUNDS AND METHODS FOR PROMOTING SMOKING CESSATION - Compounds and methods for promoting smoking cessation. The compounds may be used to treat a variety of other conditions and disease states. | 2009-12-24 |
20090318491 | Cytisine and Acetylcholine Analogs and Methods of Treating Mood Disorders - The present invention relates to compounds which are derivatives of cytisine or acetylcholine which exhibit activity as agonists, partial agonists or antagonists of nicotinic acetylcholine receptors and may be used in modulating these receptors and in treating mood disorders in patients in need of therapy. | 2009-12-24 |
20090318492 | INDOLE COMPOUNDS HAVING C4-ACIDIC SUBSTITUENTS AND USE THEREOF AS PHOSPHOLIPASE-A2 INHIBITORS - Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject. | 2009-12-24 |
20090318493 | Aryl pyrrolidinyl and piperidinyl ketone derivatives and uses thereof - Aryl and heteroaryl ketone compounds substituted with pyrrolidines and piperidines, that modulate serotonin norepinephrine and/or dopamine neurotransmission. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds. | 2009-12-24 |
20090318494 | PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS - The invention provides a compound of formula (I) or a salt thereof: | 2009-12-24 |
20090318495 | ETHENYL CARBOXAMIDE DERIVATIVES USEFUL AS MICROBIOCIDES - Compounds of the formula (I), which are suitable for use as microbiocides, and in which A is A | 2009-12-24 |
20090318496 | PREPARATION CONTAINING FIBRATE AGENT AND PROCESS FOR PRODUCING THE SAME - A preparation (pharmaceutical composition) reducing a concentration of a free fatty acid and/or fibrinogen in the blood is prepared. The preparation contains a statin agent comprising at least a statin compound having a benzopyridine skeleton (e.g., pitavastatin) and a fibrate agent (e.g., fenofibrate). The preparation is useful as a preventive or treating agent for hyper-free fatty acidemia, metabolic syndrome, or type II diabetes. | 2009-12-24 |
20090318497 | SUBSTITUTED PYRIDYLMETHYL BICYCLICCARBOXYAMIDE COMPOUNDS - This invention provides a compound of the formula (I): wherein A | 2009-12-24 |
20090318498 | PIPERIDYL ACRYLAMIDE ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula I. | 2009-12-24 |
20090318499 | COMPOUNDS HAVING ANALGESIC AND/OR IMMUNOSTIMULANT ACTIVITY - The compounds shown by their structural formulas in the specification have analgesic and or immunostimulant activity in mammals. | 2009-12-24 |
20090318500 | 4-(2, 6-Dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)-amide for the Treatment of Cancer - The invention provides the compound of formula (I) 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)-amide in a substantially crystalline form, therapeutic uses thereof and pharmaceutical compositions containing the crystalline compound. The invention also provides novel pharmaceutical formulations containing 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)-amide and novel processes for preparing the compound. | 2009-12-24 |
20090318501 | Piperidine derivatives as renin inhibitors - The present invention is directed to aspartic protease inhibitors represented by the following structural formula; or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I). Methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using these aspartic protease inhibitors are also disclosed. | 2009-12-24 |
20090318502 | Pharmaceutical Compositions Comprising a Hypoglycemic Agent and Methods of Using Same - The present invention relates to intranasally deliverable compositions comprising a hypoglycemic agent, for example, repaglinide, and to methods of using such compositions in the treatment of various disorders, including, for example, type-2 diabetes. | 2009-12-24 |
20090318503 | BIS-QUATERNARY AMMONIUM SALTS AND METHODS FOR MODULATING NEURONAL NICOTINIC ACETYLCHOLINE RECEPTORS - Provided are bis-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders. | 2009-12-24 |
20090318504 | Use of GAL3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods - This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist. | 2009-12-24 |
20090318505 | FUNGICIDAL COMPOSITIONS - A composition suitable for control of diseases caused by phytopathogens comprising (A) a compound of formula (I) or a tautomer of such a compound; and component (B) and component (C) are pesticides as described in claim | 2009-12-24 |
20090318506 | Sulfonate salts of 2-amino-3-carbethoxyamino-6-(4-fluoro-benzylamino)-pyridine - Flupirtine acid addition salts having the following formula (2), | 2009-12-24 |
20090318507 | Potassium Channel Activators for the Prevention and Treatment of Dystonia and Dystonia Like Symptoms - The present invention is directed to the prevention, reversal and medical treatment of dystonia and dyskinesia as well as other diseases related to movement disorders, both in human beings and animals by administering a neuronal potassium channel opener such as flupirtine, retigabine or maxipost. | 2009-12-24 |
20090318508 | Method for Treating Hair Growth Disorders, Such as Female Pattern Alopecia, and Compositions Useful Therefore - The invention relates to formulations useful in treating hair disorders, improving the health of hair, increasing hair growth, and in increasing the niacin content of hair follicles. Nicotinic acid alkyl esters having a straight chain alkyl group of from 1 to 22 methylene units, preferably from 6 to 16 methylene units, and most preferably from 8 to 14 methyl units, may be used, alone or in combinations for treating these conditions. | 2009-12-24 |
20090318509 | Oxime Derivatives as Inhibitors of Macrophage Migration Inhibitory Factor - Provided are compounds of formula (I) and other compounds. Also provided are pharmaceutical compositions comprising these compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal, and methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. | 2009-12-24 |
20090318510 | TOPICAL DRUG DELIVERY SYSTEM - The present invention relates to compositions for topical delivery of one or more vasoactive vitamins and their methods of preparation and use. More specifically, the composition includes one or more vasoactive vitamins, one or more alkyl hydroxybenzoate preservatives, an alkanol solvent, an alkoxylated alcohol humectant, and a high molecular weight hydrophilic colloid viscosity increasing agent. In various embodiments, the vasoactive vitamins include vitamin B3 compounds. | 2009-12-24 |
20090318511 | SELECTIVE HYDROXAMATE BASED MMP INHIBITORS - The present invention provides a compound of formula (I): | 2009-12-24 |
20090318512 | Methods of maintaining ocular tissue cell membrane integrity using cetylpyridinium chloride - A multi-purpose contact lens care solution having high antimicrobial activity comprising, in an aqueous liquid medium, cetylpyridinium chloride and a non-ionic surfactant. In one embodiment of the invention, the non-ionic surfactant is a poly(oxypropylene)-poly(oxyethylene) block copolymer. The solution may optionally also include additional antimicrobial components, a buffer component, a viscosity inducing component, a surfactant, taurine, propylene glycol and/or a tonicity component. This solution additionally prevents losses in ocular tissue membrane integrity during contact lens wear. | 2009-12-24 |
20090318513 | COMPOUNDS EXHIBITING THROMBOPOIETIN RECEPTOR AGONISM - A compound represented by the general formula (I): | 2009-12-24 |
20090318514 | Novel Pharmaceutical Compositions - The invention provides the use of compounds of formula (I) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, for the manufacture of a medicament for the treatment or prophylaxis of a condition that may be treated with a thyroid receptor agonist or partial agonist wherein R | 2009-12-24 |
20090318515 | SUCCINIMIDE DERIVATIVES AS OCULAR HYPOTENSIVE AGENTS - The invention provides a method for treating ocular disorders associated with ocular hypertension by administrating an effective amount of a pharmaceutical composition comprising a succinimide derivative. | 2009-12-24 |
20090318516 | SOLID FORMS OF (1R,2S,3R)-1-(2-(ISOXAZOL-3-YL)-1H-IMIDAZOL-4-YL)BUTANE-1,2,3,4-TETRAOL AND METHODS OF THEIR USE - Solid forms of (1R,2S,3R)-1-(2-(isoxazol-3-yl)-1H-imidazol-4-yl)butane-1,2,3,4-tetraol and hydrates thereof are disclosed, as well as compositions comprising them and methods of their use. | 2009-12-24 |
20090318517 | Novel Compounds 148 - This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production. | 2009-12-24 |
20090318518 | INDOLE AND INDOLINE CYCLOPROPYL AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS - The invention is directed to indole and indoline cyclopropyl amide derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included. | 2009-12-24 |
20090318519 | PROCESS FOR RELEASE OF BIOLOGICALLY ACTIVE SPECIES - A process for the release of a biologically active species comprising the steps of: providing a mesoporous oxide-based material having structural order and at least one level of porosity; fixing or immobilizing said biologically active species in said ordered mesoporous oxide; and providing said ordered mesoporous oxide with said fixed or immobilized biologically active species in vivo thereby realizing intraluminally induced substantially pH-independent supersaturation of said biologically active species resulting in enhanced transepithelial transport; wherein said biologically active species is a poorly soluble therapeutic drug classified as belonging to Class II or Class IV of the Biopharmaceutical Classification System and said ordered mesoporous oxide has a pore size in the range of 4 to 14 nm. | 2009-12-24 |
20090318520 | USE OF ISOINDOLES FOR THE TREATMENT OF NEUROBEHAVIORAL DISORDERS - The present invention generally relates to the use of drugs for the treatment of neurobehavioral disorders or symptoms of a neurobehavioral disorder associated with dysfunction of the trimonoamine modulating system (TMMS). More specifically, the invention describes methods for the treatment of a neurobehavioral disorder and/or treatment or prevention of symptoms of a neurobehavioral disorder by administering suitable Isoindole derivatives alone or in combination with other agents so as to provide relatively equal inhibitory effect on serotonin, dopamine and norepinephrine transporters. | 2009-12-24 |
20090318521 | Synthesis of 4-Bromomethyl-2'-Formylbiphenyl and 4-Bromomethyl-2'-Hydroxymethylbiphenyl and Its Use in Preparation of Giotensin II Antagonists - 4-bromomethyl-2′-formylbiphenyl and 4-bromomethyl-2′-hydroxymethylbiphenyl are useful starting material for the preparation various angiotenzin II antagonists, which are prepared from 4-bromomethyl-2′-cyanobiphenyl or 4′-bromomethylbiphenylcarboxyilic derivatives using selected hydride reagent. | 2009-12-24 |
20090318522 | THERAPY FOR THE TREATMENT OF DISEASE - Disclosed herein are pharmaceutical compositions comprising oxybutynin, or a free base thereof or a pharmaceutically acceptable salt thereof, and pilocarpine, or a free base thereof or a pharmaceutically acceptable salt thereof. Also disclosed are methods of treating a patient suffering from overactive bladder comprising administering to the patient the above pharmaceutical composition. | 2009-12-24 |
20090318523 | BENZOISOINDOLE DERIVATIVES AND THEIR USE AS EP4 RECEPTOR AGONISTS - The present invention relates to benzoisoindole phenylacetic acid derivatives, corresponding pharmaceutical compositions, preparation processes and uses in medicine as EP4 receptor angonists. | 2009-12-24 |
20090318524 | BICYCLIC TETRAHYDROPYRROLE COMPOUNDS - The present invention relates to substituted bicyclic tetrahydropyrrole compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals. | 2009-12-24 |
20090318525 | Process For Preparing A 3-Pyrrole Substituted 2-Indolinone Malate Salt - The invention relates to the malic acid salt of N-[2-(diethylamino)ethyl]-5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxamide, to the use thereof as an intermediate for preparing the malic acid salt of sunitinib, and to pharmaceutical compositions comprising said malic acid salt of sunitinib. | 2009-12-24 |
20090318526 | Use of cannabinoid receptor agonists as hypothermia inducing drugs for the treatment of ischemia - The present invention relates to the use of a cannabinoid receptor agonist for use in induction of hypothermia in a human being for the prophylaxis and treatment of ischemia. | 2009-12-24 |
20090318527 | INDOLE COMPOUNDS AND METHODS OF USE THEREOF - Novel indole compounds are disclosed. Also disclosed are methods for using the compounds to treat human and animal disease, pharmaceutical compositions of the compounds, and kits including the compounds. | 2009-12-24 |
20090318528 | HYDRATE CRYSTALS - New (2R,4R) monatin monosodium salt hydrate crystals characterized by having specific characteristic X-ray diffraction peaks provide general-purpose, stable, and safe monatin sodium salt crystals incorporating no organic solvent. These crystal may be prepared by a method that requires no organic solvent in the crystallization, separation, and drying steps. These crystal are useful as sweeteners and for the preparation of orally consumed products, such as foods, beverages, pharmaceutical products, topical pharmaceutical products, and feeds containing general-purpose, stable, and safe monatin sodium salt crystals. | 2009-12-24 |
20090318529 | SALINOSPORAMIDES AND METHODS FOR USE THEREOF - The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet | 2009-12-24 |
20090318530 | PHARMACEUTICAL COMPOSITIONS COMPRISING NK1 RECEPTOR ANTAGONISTS AND SODIUM CHANNEL BLOCKERS - The present invention relates to pharmaceutical compositions comprising an NK1 receptor antagonist and a sodium channel blocker compound of formula (I) | 2009-12-24 |
20090318531 | Small Interfering RNA Specific For HCV And Therapeutic Agent For Hepatitis C Comprising The Same - The present invention relates to a therapeutic reagent for hepatitis C comprising HCV specific short interfering RNA (siRNA) as an effective ingredient. The siRNA of the invention is a double-stranded RNA specific for the nucleotide sequence of HCV which induces viral RNA degradation in mammalian cells and thereby inhibits HCV protein expression and replication. The method of the invention, which includes the step of administrating the synthetic siRNA or a DNA vector encoding the RNA, is thus effective for the treatment of HCV carrier by inhibiting HCV gene expression and replication. | 2009-12-24 |
20090318532 | COMPOUNDS AND METHODS FOR MODULATING EXPRESSION OF PTP1B - The present disclosure describes short antisense compounds, including such compounds comprising chemically-modified high-affinity monomers 8-16 monomers in length. Certain such short antisense compound are useful for the reduction of target nucleic acids and/or proteins in cells, tissues, and animals with increased potency and improved therapeutic index. Thus, provided herein are short antisense compounds comprising high-affinity nucleotide modifications useful for reducing a target RNA in vivo. Such short antisense compounds are effective at lower doses than previously described antisense compounds, allowing for a reduction in toxicity and cost of treatment. In addition, the described short antisense compounds have greater potential for oral dosing. | 2009-12-24 |
20090318533 | Annexin A9 (ANXA9) Biomarker and Therapeutic Target in Epithelial Cancer - Amplification of the ANXA9 gene in human chromosomal region 1q21 in epithelial cancers indicates a likelihood of both in vivo drug resistance and metastasis, and serves as a biomarker indicating these aspects of the disease. ANXA9 can also serve as a therapeutic target. Interfering RNAs (iRNAs) (such as siRNA and miRNA) and shRNA adapted to inhibit ANXA9 expression, when formulated in a therapeutic composition, and delivered to cells of the tumor, function to treat the epithelial cancer. | 2009-12-24 |
20090318534 | METHODS AND COMPOSITIONS FOR THE TREATMENT OF SKIN DISEASES AND DISORDERS - The disclosure demonstrates the role of cathelicidin, serine protease and/or vitamin D3 in rosacea pathology. | 2009-12-24 |
20090318535 | BETA -TrCP1, BETA -TrCP2 AND RSK1 OR RSK2 INHIBITORS AND METHODS FOR SENSITIZING TARGET CELLS TO APOPTOSIS - The invention relates to modulating BimEL levels (Bcl-2-Interacting Mediator of cell death, Extra Long isoform) to sensitize cancer cells to cell death or apoptosis. In certain embodiments, the invention relates to increasing BimEL levels. In certain embodiments, the invention relates to inhibitors of at least one of β-TrCP1/2 or RSK1/2 proteins that sensitize tumor cells to chemotherapy-induced death or apoptosis. Additionally, the invention relates to cancer therapies, diagnostics, and methods for identifying novel drugs or drug candidates for increasing BimEL levels. | 2009-12-24 |
20090318536 | METHODS FOR TREATING HYPERCHOLESTEROLEMIA - Disclosed herein are antisense compounds and methods for decreasing LDL-C in an individual having elevated LDL-C. Additionally disclosed are antisense compounds and methods for treating, preventing, or ameliorating hypercholesterolemia and/or atherosclerosis. Further disclosed are antisense compounds and methods for decreasing coronary heart disease risk. Such methods include administering to an individual in need of treatment an antisense compound targeted to a PCSK9 nucleic acid. The antisense compounds administered include gapmer antisense oligonucleotides. | 2009-12-24 |
20090318537 | SILENCING OF TGF BETA TYPE II RECEPTOR EXPRESSION BY SIRNA - The present application is directed to siRNA-based silencing of the type II receptor of TGFβ. siRNAs that target this receptor abrogate the receptor protein and transcript, TGFβ-mediated processes such as fibronectin assembly and cell migration also are inhibited and the molecules of the invention are efficacious in reducing the inflammatory response and matrix deposition. These findings show that siRNAs can be successfully delivered both in vitro and in vivo to regulate the TGFβ type II receptor level and modulate wound response. Methods and compositions exploiting the findings of the present invention have a wide-ranging application, extending from treatment of disorders of the eye to other organs and tissues throughout the body. | 2009-12-24 |
20090318538 | POLYMERIC OLIGONUCLEOTIDE PRODRUGS - Polymer conjugates containing nucleotides and/or oligonucleotides are disclosed. | 2009-12-24 |
20090318539 | Process for Preparing a Particle Comprising a Biological Molecule and a Carrier Polymer - A process for preparing a particle comprising a biological molecule typically a DNA plasmid, and a carrier polymer, typically poly-lactic acid (PLA), in which an organic solvent solution of the biological molecule and the carrier polymer in an organic solvent medium, nearly saturated with the biological molecule, is prepared, then this solution is contacted with an antisolvent substance, typically supercritical carbon dioxide to separate a particle comprising the biological molecule and the carrier polymer. High loadings of the biological molecule in the particle can be achieved. | 2009-12-24 |
20090318540 | NUCLEIC ACIDS FOR EXPRESSING A POLYNUCLEOTIDE OF INTEREST IN MAMMALIAN CANCER CELLS - The invention relates to regulatory polynucleotides derived (i) from rat and human AFP promoter sequences and (ii) from rat and human HIP/PAPI promoter sequences, which regulatory polynucleotides are useful for expressing nucleic acids of interest specifically in mammalian cancer cells, including mammalian cancer liver cells. | 2009-12-24 |
20090318541 | Benzothiophene hydroxamic acid derivatives with carbamate, urea, amide and sulfonamide substitutions - The present invention relates to a novel class of hydroxamic acid derivatives carbamate, urea, amide and sulfonamide substitutions. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo. | 2009-12-24 |
20090318542 | OPHTHAMOLOGICAL DRUGS - The present invention relates generally to ophthamological drugs. More specifically, the invention relates to a method of modifying (derivatizing) ophthamological drugs so as to increase their penetration through the cornea. The invention also relates to drugs modified (derivatized) in accordance with the instant method and to the use of same in treating conditions associated with elevated intraocular pressure, particularly, glaucoma. | 2009-12-24 |
20090318543 | C(10) ETHYL ESTER AND C(10) CYCLOPROPYL ESTER SUBSTITUTED TAXANES - Taxanes having an ethyl ester or cyclopropyl ester substituent at C(10), a keto substituent at C(9), a hydroxy substituent at C(7), a thienyl substituent at C(3′) and a cyclobutyloxycarbamate or cyclopentyloxycarbamate substituent at C(3′), pharmaceutical compositions comprising such taxanes, methods of treatment and administration, and methods of preparation of medicaments comprising the taxanes. | 2009-12-24 |