| 47th week of 2010 patent applcation highlights part 47 |
| Patent application number | Title | Published |
|---|
| 20100298296 | Oligomer-Tricyclic Conjugates - The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer. | 2010-11-25 |
| 20100298297 | Tetrahydropyridothienopyrimidine Compounds and Methods of Use Thereof - This invention relates to compounds of Formula (I), | 2010-11-25 |
| 20100298298 | QUINAZOLINEDIONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USES THEREOF - The invention relates to quinazolinedione derivatives, processes for the preparation thereof and their therapeutic applications. | 2010-11-25 |
| 20100298299 | NON-PEPTIDE DERIVATIVES AS BRADYKININ B1 ANTAGONISTS - The present invention relates to new non-peptide derivatives of formula (I), wherein R | 2010-11-25 |
| 20100298300 | TRIAZOLOPYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE & INFLAMMATORY DISEASES - Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following: | 2010-11-25 |
| 20100298301 | OXAZOLE TYROSINE KINASE INHIBITORS - The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar | 2010-11-25 |
| 20100298302 | NOVEL PROTEIN KINASE MODULATORS - The invention provides compounds that inhibit selected kinases (Pim, Flt and/or CK2 kinases) and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain infections and immunological disorders. | 2010-11-25 |
| 20100298303 | CGRP RECEPTOR ANTAGONISTS - The present invention is directed to compounds of Formula I: | 2010-11-25 |
| 20100298304 | DIAGNOSIS AND TREATMENT OF AUTISM SPECTRUM DISORDERS - The invention relates to methods for diagnosis and treatment of autism spectrum disorders, particularly for autism spectrum disorders characterized by increased head size (circumference) and deficits in social behavior. | 2010-11-25 |
| 20100298305 | TIZANIDINE FOR THE TREATMENT OF POST-TRAUMATIC STRESS DISORDER AND NIGHTMARES - Disclosed herein are methods of treating a psychiatric disorder, such as a sleep disorder, an anxiety disorder, a mood disorder or a perceptual disturbance. In one example, a method of treating a sleep disorder or anxiety disorder includes selecting a subject with a sleep disturbance or anxiety disorder in the absence of an underlying physical disorder and administering a therapeutically effective amount of tizanidine, thereby reducing or inhibiting a symptom of the sleep disorder or anxiety disorder. In another example, a method of treating a mood disorder or a perceptual disturbance is disclosed. This method includes selecting a subject with a mood disorder or perceptual disturbance and administering a therapeutically effective amount of tizanidine, thereby reducing or inhibiting a symptom of the mood disorder or perceptual disturbance. | 2010-11-25 |
| 20100298306 | (1,4-Diaza-bicyclo[3.2.2]non-6-en-4-yl)-heterocyclyl-methanone Ligands for Nicotinic Acetylcholine Receptors, Useful for the Treatment of Disease - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds, which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof. The novel compounds include compounds of formula I: | 2010-11-25 |
| 20100298307 | NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidine derivatives of formula (I) and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 2010-11-25 |
| 20100298308 | Compositions and methods for bone formation and remodeling - The mechanism by which the high bone mass (HBM) mutation (G171V) of the Wnt coreceptor LRP5 regulates the canonical Wnt signaling was investigated. The mutation was previously shown to reduce Dkk protein-1-mediated antagonism, suggesting that the first YWTD repeat domain where G171 is located may be responsible for Dkk protein-mediated antagonism. However, we found that the third YWTD repeat, but not the first repeat domain, is required for DKK1-mediated antagonism. Instead, we found that the G171V mutation disrupted the interaction of LRP5 with Mesd, a chaperon protein for LRP5/6 that is required for the coreceptors' transport to cell surfaces, resulting in less LRP5 molecules on the cell surface. Although the reduction in the level of cell surface LRP5 molecules led to a reduction in Wnt signaling in a paracrine paradigm, the mutation did not appear to affect the activity of coexpressed Wnt in an autocrine paradigm. Together with the observation that osteoblast cells produce autocrine canonical Wnt, Wnt7b, and that osteocytes produce paracrine Dkk1, we believe that the G171V mutation may cause an increase in Wnt activity in osteoblasts by reducing the number of targets for paracrine Dkk1 to antagonize without affecting the activity of autocrine Wnt. | 2010-11-25 |
| 20100298309 | TRICYCLIC TRIAZOLIC COMPOUNDS - The present invention relates to new tricyclic triazolic compounds having a high affinity for sigma-1 receptor as well as to the process for the preparation thereof, to composition comprising them and to their use as medicaments according to compounds of formula (I), Wherein R | 2010-11-25 |
| 20100298310 | Thiazole Derivatives as Kinase Inhibitors - A series of thiazole derivatives which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. | 2010-11-25 |
| 20100298311 | TETRAHYDRONAPHTHALENE DERIVATES, PROCESS FOR PREPARING THEM AND THEIR USE AS ANTIINFLAMMATORY AGENTS - The invention relates to multiply substituted tetrahydronaphthalene derivatives of the formula (Ia) | 2010-11-25 |
| 20100298312 | SUBSTITUTED PYRIMIDINYL-AMINES AS PROTEIN KINASE INHIBITORS - The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway. | 2010-11-25 |
| 20100298313 | METHOD OF USING IMIDAZOLOTHIAZOLE COMPOUNDS FOR THE TREATMENT OF DISEASE - Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases. | 2010-11-25 |
| 20100298314 | NOVEL JNK INHIBITORS - Disclosed are substituted imidazo[1,2-a]pyridines, imidazo[1,2-a]pyrazines, imidazo[1,2-c]pyrimidines and imidazo[1,2-d]triazines compounds of the formula: (1.0) Also disclosed are methods for treating JNK1 and ERK mediated diseases using the compounds of formula 1.0. | 2010-11-25 |
| 20100298315 | NOVEL 6-TRIAZOLOPYRIDAZINESULFANYL BENZOTHIAZOLE AND BENZIMIDAZOLE DERIVATIVES, METHOD FOR PRODUCTION THEREOF AND APPLICATION AS MEDICAMENTS AND PHARMNACEUTICAL COMPOSITIONS AND NOVEL USE AS MET INHIBITORS - The disclosure relates to compounds of formula (I): | 2010-11-25 |
| 20100298316 | Benzothiazoles Having Histamine H3 Receptor Activity - Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings,! of the general formula (1): having histamine H3 antagonistic activity can be used in pharmaceutical compositions. | 2010-11-25 |
| 20100298317 | METHOD OF TREATING POLYCYSTIC KIDNEY DISEASES WITH CERAMIDE DERIVATIVES - A method of treating polycystic kidney disease in a subject comprises administering to the subject an effective amount of a compound represented by Structural Formula (1): or a pharmaceutically acceptable salt thereof. | 2010-11-25 |
| 20100298318 | METHODS AND COMPOSITIONS FOR STIMULATING NEUROGENESIS AND INHIBITING NEURONAL DEGENERATION USING ISOTHIAZOLOPYRIMIDINONES - The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, traumatic nerve injury, and depression. This invention is useful for resear products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells. | 2010-11-25 |
| 20100298319 | PYRIMIDINE SUBSTITUTED PURINE DERIVATIVES - The present invention relates to purine compounds that are useful as kinase inhibitors. More particularly, the present invention relates to purine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative conditions or disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative conditions or disorders including tumours and cancers as well as other disorders or conditions related to or associated with PI3 and/or mTOR kinases. | 2010-11-25 |
| 20100298320 | Pyrido[2,3-b]pyrazin-8-substituted Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc. | 2010-11-25 |
| 20100298321 | BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein. | 2010-11-25 |
| 20100298322 | Quinazolines and Related Heterocyclic Compounds, and Their Therapeutic Use - A compound of the formula (I) wherein X is CR | 2010-11-25 |
| 20100298323 | APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein. | 2010-11-25 |
| 20100298324 | Prolyl Hydroxylase Inhibitors - The invention described herein relates to certain 4-oxo-2-thioxo-1,2,3,4-tetrahydro-7-quinazolinecarboxamide derivatives of formula (I) | 2010-11-25 |
| 20100298325 | PYRIDINE DERIVATIVES FOR THE TREATMENT OF AMYLOID-RELATED DISEASES - a compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof: wherein X and Y are independently NR | 2010-11-25 |
| 20100298326 | Carboxamide compounds and their use as calpain inhibitors - The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. | 2010-11-25 |
| 20100298327 | APREPITANT POLYMORPH MIXTURES - Intimate mixtures of aprepitant crystalline Form I and crystalline Form II, having specific Hweight ratios of the forms. | 2010-11-25 |
| 20100298328 | 1-Heterocyclylamino-2-Hydroxy-3-Amino-Omega-Arylalkanes - 1-Heterocyclylamino-2-hydroxy-3-amino-ω-arylalkanes of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, medicinally active ingredients. | 2010-11-25 |
| 20100298329 | TOLPERISONE AND TOLPERISONE-LIKE DRUGS FOR THE TREATMENT OF K-RAS ASSOCIATED CANCERS - The invention provides compositions and methods for treating cancer. Aspects of the invention relate to therapeutic compositions comprising tolperisone and related compounds. Aspects of the invention relate to methods and compositions for treating Ras-associated cancers. | 2010-11-25 |
| 20100298330 | HALOALLYLAMINE INHIBITORS OF SSAO/VAP-1 AND USES THEREFOR - The present invention is related to the preparation and pharmaceutical In use of novel haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification:(I). The invention also relates to methods of using invention compounds, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases. | 2010-11-25 |
| 20100298331 | TRIAZINONE AND DIAZINONE DERIVATIVES USEFUL AS HSP90 INHIBITORS - The present invention relates to compounds according to formulae (IA) to (ID) and compositions that inhibit the activity of Hsp90. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound. | 2010-11-25 |
| 20100298332 | Substituted Spirocyclic Piperidine Derivatives as Histamine-3 (H3) Receptor Ligands - The present invention provides compounds of Formula (I): | 2010-11-25 |
| 20100298333 | COMBINATION THERAPY FOR THE TREATMENT OF DIABETES AND CONDITIONS RELATED THERETO AND FOR THE TREATMENT OF CONDITIONS AMELIORATED BY INCREASING A BLOOD GLP-1 LEVEL - The present invention concerns combination of an amount of a GPR119 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-1 level in a subject over that provided by the amount of the GPR119 agonist or the amount of the DPP-IV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-1 level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-1 secretagogues. | 2010-11-25 |
| 20100298334 | N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS - The present invention relates to N-(hetero)aryl-pyrrolidine derivatives of Formula I: | 2010-11-25 |
| 20100298335 | Preparations and Methods for Ameliorating or Reducing Presbyopia - This application relates to the use of one or more parasympathomimetic drugs in combination with one or more alpha agonists to create optically beneficial miosis to, for example, temporarily treat presbyopia. The invention provides a pharmaceutical preparation comprising a therapeutically effective amount of one or more parasympathomimetic drugs or cholinesterase inhibitors, or a pharmaceutically acceptable salt thereof, in combination with one or more alpha agonists or antagonists, or a pharmaceutically acceptable salt thereof. The invention further provides for a method for treating, ameliorating or reducing presbyopia of a patient having an eye, comprising administering to said eye a pharmaceutically effective amount of the ophthalmic preparation. | 2010-11-25 |
| 20100298336 | PYRIMIDINES AS NOVEL THERAPEUTIC AGENTS - The present invention features compounds having the Formula (Ia) and (Ib) (e.g., a compound of any of Formulas ((Ia-2)-(Ia-21)), including other tautomers, stereoisomers, E/Z stereoisomers, prodrugs, pharmaceutically acceptable salts, and compositions thereof. The invention also features methods for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient by administering an effective amount of a compound of Formula (Ia) or (Ib). The invention also features a method for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient that includes administering to a patient in need thereof an effective amount of a compound of Formula (IIa) or (IIb) (e.g., a compound of any of Formulas ((IIa-2)-(IIa-6)). The compounds described herein (e.g., a compound of Formulas (Ia), (Ib), (IIa), or (IIb)) can also be used as anticonvulsants. | 2010-11-25 |
| 20100298337 | Organic Compounds - Compounds of formula (I) in free or salt or solvate form, where T | 2010-11-25 |
| 20100298338 | METHOD OF OPTIMIZING THE TREATMENT OF PROLIFERATIVE DISEASES MEDIATED BY THE TYROSINE KINASE RECEPTOR KIT - The invention relates to a method of treating proliferative diseases mediated by the tyrosine kinase receptor KIT, in particular GIST, in a human patient population. | 2010-11-25 |
| 20100298339 | [1,2,4]Triazolo[1,5-a]Pyridine and [1,2,4]Triazolo[1,5-c]Pyrimidine Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain triazolo compounds (referred to herein as TAZ compounds), and especially certain [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-c]pyrimidine compounds, which, inter alia, inhibit AXL receptor tyrosine kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit AXL receptor tyrosine kinase function, and in the treatment of diseases and conditions that are mediated by AXL receptor tyrosine kinase, that are ameliorated by the inhibition of AXL receptor tyrosine kinase function, etc., including proliferative conditions such as cancer, etc. | 2010-11-25 |
| 20100298340 | Thiazol-Guanidine Derivatives Useful As A (Beta)-Related Pathologies - This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia. | 2010-11-25 |
| 20100298341 | Glycine Transporter-1 Inhibitors - The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds. | 2010-11-25 |
| 20100298342 | Spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's Disease - The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved. | 2010-11-25 |
| 20100298343 | 5-LIPOXYGENASE-ACTIVATING PROTEIN (FLAP) INHIBITORS - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases. | 2010-11-25 |
| 20100298344 | Polycationic Compounds And Uses Thereof - Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis. | 2010-11-25 |
| 20100298345 | SYNTHETIC COMPOUNDS AND DERIVATIVES AS MODULATORS OF SMOKING OR NICOTINE INGESTION AND LUNG CANCER - Disclosed are nicotine-related compounds that selectively inhibit cytochrome P-450 2A6 (CYP2A6), selectively inhibit cytochrome P-450 2A13 (CYP2A13), and/or selectively modulate a nicotinic acetylcholine receptor (nAChR). Also disclosed are pharmaceutical compositions comprising a compound of the invention, as well as methods of using the pharmaceutical compositions for treating or preventing a disease or disorder associated with nicotine-ingestion, or a disease or disorder amenable to treatment by selective modulation of nAChRs. | 2010-11-25 |
| 20100298346 | NITROGENOUS HETEROCYCLIC COMPOUNDS WITH INSECTICIDAL ACTIVITY, AND THE PREPARATION AND USE THEREOF - The present invention relates to nitro-containing heterocyclic or ring-opening nitrogenous compounds of formula (A), wherein R | 2010-11-25 |
| 20100298347 | SUBSTITUTED 2-NAPHTHOIC ACIDS AS ANTAGONISTS OF GPR105 ACTIVITY - Substituted 2-naphthoic acids of structural formula are effective as antagonists of the biological activity of GPR105 protein. They are useful for the treatment, control or prevention of disorders responsive to antagonism of this receptor, such as diabetes, particularly, Type 2 diabetes, insulin resistance, hyperglycemia, lipid disorders, obesity, atherosclerosis, and conditions associated with the Metabolic Syndrome. | 2010-11-25 |
| 20100298348 | Method of Decreasing Ubiquitylated Protein Levels - The present invention provides a method of decreasing the level of ubiquitylated protein in a subject, the method comprising administering a heterocyclic compound disclosed herein or a pharmaceutically acceptable salt, hydrate or prodrug thereof to a subject in need thereof. | 2010-11-25 |
| 20100298349 | THIENOPYRIMIDINE COMPOUNDS AND COMPOSITIONS - Compounds of formula (I) are A | 2010-11-25 |
| 20100298350 | Triazolo[4,5-D]Pyrimidine Compounds For Treatment Of Abdominal Aortic Aneurysms - The invention provides triazolo [4,5-d]pyrimidine compounds, acting as P | 2010-11-25 |
| 20100298351 | NOVEL PYRAZOLO [3, 4 -D] PYRIMIDINE DERIVATIVES AS ANTI-CANCER AGENTS - The invention relates to substituted pyrazolo[3,4-d]pyrimidine derivatives of the Formula-(I), or pharmaceutically-acceptable salts thereof, which possess anti-proliferative activity such as anti-cancer activity and are accordingly useful in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of substituted pyrazolo[3,4-d]pyrimidine derivatives, to pharmaceutical compositions containing the compound and to its use in the manufacture of medicaments for the production of an anti-proliferative effect in a warm-blooded animal such as man. | 2010-11-25 |
| 20100298352 | SMALL MOLECULE INHIBITORS OF CANCER STEM CELLS - A method of inhibiting a carcinoma in a subject, comprising administering to the subject at least one therapeutic agent that selectively targets carcinoma stem cells. Illustrative carcinoma stem cell-selective therapeutic agents include CGP74514A, rottlerin, and A-77636. | 2010-11-25 |
| 20100298353 | Famciclovir for the treatment of recurrent herpes labialis using a one-day treatment - A method for the treatment of recurrent herpes labialis in mammals, including humans, which method comprises administering to the mammal in need of such treatment, an effective amount of penciclovir or famciclovir, or a pharmaceutically acceptable salt thereof for a period of one day. | 2010-11-25 |
| 20100298354 | Crystalline Form Of Abacavir That Is Essentially Free Of Solvent - Crystalline form of abacavir that is essentially free of solvent of formula (I), in particular crystalline Form I, and its preparation process which comprises the following steps: a) crystallizing abacavir from a solution of said compound in a (C | 2010-11-25 |
| 20100298355 | 3-[4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL]OCTANE- OR HEPTANE-NITRILE AS JAK INHIBITORS - The present invention relates to the Janus kinase (JAK) inhibitors 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile or 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile, as well as its compositions and methods of use, which is useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, skin disorders, cancer, and other diseases. | 2010-11-25 |
| 20100298356 | SATURATED AND INSATURATED BI- OR TRICYCLIC ARYLOXYACETAMINE DERIVATIVES AND THEIR USE AS FUNGICIDES - Compounds of the general formula (I), wherein the substituents are as defined in claim | 2010-11-25 |
| 20100298357 | MALEATE SALTS OF A QUINAZOLINE DERIVATIVE USEFUL AS AN ANTIANGIOGENIC AGENT - The present invention relates to AZD2171 maleate salt, to particular crystalline forms of AZD2171 maleate salt, to processes for their preparation, to pharmaceutical compositions containing them as active ingredient, to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans, and to their use in methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability. | 2010-11-25 |
| 20100298358 | Naphthamide Derivatives As Multi-Target Protein Kinase Inhibitors and Histone Deacetylase Inhibitors - Isolated compounds of formula I: | 2010-11-25 |
| 20100298359 | GAMMA SECRETASE MODULATORS - This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R | 2010-11-25 |
| 20100298360 | SMALL MOLECULE INHIBITORS OF PDZ INTERACTIONS - The present invention relates to compositions for use in the modulation of PDZ domain interactions with cognate ligands. Methods of assessing and characterizing PDZ domain interactions from various polypeptides also are provided. | 2010-11-25 |
| 20100298361 | Alkylthio Pyrimidines As CRTH2 Antagonists - Provided herein are alkylthio substituted pyrimidine compounds having CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity, useful for the treatment or prophylaxis of diseases associated with CRTH2 activity, including the treatment of allergic diseases, eosinophil-related diseases and basophil-related diseases. | 2010-11-25 |
| 20100298362 | PROCESS FOR THE PREPARATION OF 4-[6-(6-METHANESULFONYL-2-METHYL-PYRIDIN-3-YLAMINO)-5-METHOXY-PYRIMIDIN-4- -YLOXY]-PIPERIDINE-1-CARBOXYLIC ACID ISOPROPYL ESTER - The present invention is directed to a process for the preparation of 4-[6-(6-methanesulfonyl-2-methyl-pyridin-3-ylamino)-5-methoxy-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester, useful as glucose dependent insulinotropic receptor agonist, for the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity. | 2010-11-25 |
| 20100298363 | Use of carboxyamidotriazole (CAI) orotate in macular degeneration - Method and composition of Carboxyamidotriazole orotate for treating age-related macular degeneration and other angiogenesis-dependent diseases. | 2010-11-25 |
| 20100298364 | SALTS 756 - The invention provides salts of 4-(dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate, pharmaceutical compositions containing them and their use in therapy. | 2010-11-25 |
| 20100298365 | TOPICAL ADMINISTRATION CARRIER COMPOSITION AND THERAPEUTIC FORMULATIONS COMPRISING SAME - A topical administration carrier composition including water, glycerin and polysorbate, suitable for use in formulations with active ingredient compositions containing active ingredients such as minoxidil that are susceptible to systemic penetration, and solvents that are susceptible to evaporative loss, when the active ingredient composition is topically applied to the body. The carrier formulation retards the evaporative losses of the solvent component(s) and systemic migration losses of the active ingredient composition, to provide sustained topical action, in relation to formulations lacking the carrier composition of the invention. | 2010-11-25 |
| 20100298366 | CHEMOKINE RECEPTOR BINDING COMPOUNDS - The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR5. These compounds demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV). | 2010-11-25 |
| 20100298367 | Conformationally Constrained Carboxylic Acid Derivatives Useful for Treating Metabolic Disorders - The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I or the general formula III: | 2010-11-25 |
| 20100298368 | ANTAGONISTS OF PGD2 RECEPTORS - Described herein are compounds and pharmaceutical compositions containing such compounds that modulate the PGD | 2010-11-25 |
| 20100298369 | BERBAMINE DERIVATIVES - The invention provides novel berbamine derivatives, and compositions or pharmaceutical compositions thereof. These berbamine derivatives have shown higher potency in killing cancer/tumor cells comparing to berbamine, and can be used in cancer/tumor treatments. | 2010-11-25 |
| 20100298370 | BENZOTHIAZOLYL THIENOPYRIDINE DERIVATIVES AND USES THEREOF - Novel benzothiazolyl thienopyridine compounds are provided and pharmaceutical compositions comprising benzothiazolyl thienopyridine compounds. The benzothiazolyl thienopyridine compounds are capable of inhibiting the interactions between vascular endothelial growth factor (VEGF) and heparan sulfate glycosaminoglycans (HS-GAGs), and are useful for prevention or treatment of diseases and disorders such as inflammation, autoimmune diseases and cancer. | 2010-11-25 |
| 20100298371 | PROCESS FOR PREPARING CHEMICALLY AND CHIRALLY PURE SOLIFENACIN BASE AND ITS SALTS - The present invention provides improved processes for preparing chemically and chirally pure Solifenacin base. The present invention also provides for a composition comprising of a salt of Solifenacin having at least 98% purity. The present invention also disclose certain new salts of Solifenacin as well as well as new polymorphic forms of Solifenacin hydrochloride and Solifenacin oxalate, in pure form. | 2010-11-25 |
| 20100298372 | GAMMA SECRETASE MODULATORS - This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I). | 2010-11-25 |
| 20100298373 | OXADIAZOLE DERIVATIVES ACTIVE ON SPHINGOSINE-1-PHOSPHATE (SIP) - The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders. | 2010-11-25 |
| 20100298374 | NITRILE DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS - Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I | 2010-11-25 |
| 20100298375 | MEDICAMENT COMPRISING A CARBOSTYRIL DERIVATIVE AND DONEPEZIL FOR TREATING ALZHEIMER'S DISEASE - The invention relates to a medicament for treating Alzheimer's disease comprising as active ingredients a carbostyril derivative of the general formula: wherein A is a lower alkylene group, R is a cycloalkyl group, the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double bond, or a salt thereof; and donepezil or a salt thereof. | 2010-11-25 |
| 20100298376 | USE OF NOVEL NEUROPROTECTIVE 3-SUBSTITUTED INDOLONE COMPOSITIONS - The present invention provides compositions and methods of synthesizing optionally substituted 3-substituted indolin-2-ones and methods to employ the resultant compounds to protect against neurodegeneration including diseases such as Alzheimer's disease, Parkinson's disease, or Huntington's disease, and conditions such as ischemic stroke. | 2010-11-25 |
| 20100298377 | NOVEL SUBSTITUTED INDAZOLES, THE PREPARATION THEREOF AND USE OF SAME IN THERAPEUTICS - This disclosure relates to compounds of formula (I): | 2010-11-25 |
| 20100298378 | ARYL-SUBSTITUTED POLYCYCLIC AMINES, METHOD FOR THE PRODUCTION THEREOF, AND USE THEREOF AS A MEDICAMENT - The invention relates to aryl-substituted polycyclic amines of formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; | 2010-11-25 |
| 20100298379 | PHARMACEUTICAL COMPOSITIONS OF 5-HYDROXYTRYPTOPHAN AND SEROTONIN-ENHANCING COMPOUND - This invention relates to novel pharmaceutical compositions comprising a therapeutically effective amount of a slow-release formulation of 5-hydroxytryptophan (5-HTP) and a serotonin-enhancing compound. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for combating CNS disorders, including depressive disorders, bipolar disorders, anxiety disorders, obesity and pain. | 2010-11-25 |
| 20100298380 | N-ARYL-N-PIPERIDIN-4-YLMETHYL-AMIDE DERIVATIVES AND THIER USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - This invention relates to novel N-aryl-N-piperidin-4-ylmethyl amide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. | 2010-11-25 |
| 20100298381 | GAMMA SECRETASE MODULATORS - In its many embodiments, the present invention provides a novel class of 5-membered, nitrogen-containing heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions. | 2010-11-25 |
| 20100298382 | COMPOSITIONS AND METHODS FOR ALLEVIATING DEPRESSION OR IMPROVING COGNITION - This application describes compositions of receptor inhibitors, including antipsychotic agents, for example haloperidol, and methods of use for alleviating clinical depression, improving cognition and/or treating other syndromes, conditions or diseases for which anti-depressant agents are prescribed. Furthermore, this application describes compositions and methods to induce supersensitivity in dopamine D2 and other receptors involved in depression and/or cognition as a means of alleviating clinical depression or improving cognition. | 2010-11-25 |
| 20100298383 | NOVEL BENZIMIDAZOLE DERIVATIVES USEFUL AS SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS) - The present invention is directed to novel benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. | 2010-11-25 |
| 20100298384 | NOVEL OXAZOLIDINONE COMPOUNDS AS ANTIINFECTIVE AGENTS - The present invention relates to novel oxazolidinone compounds of formula (I) with antibacterial activity, their pharmaceutically acceptable salts, their stereoisomers, their prodrugs, pharmaceutical compositions comprising the same and to their use as therapeutic agents | 2010-11-25 |
| 20100298385 | PROTEIN KINASE INHIBITORS USEFUL FOR TREATMENT OF CANCERS - This invention relates to protein kinase inhibitors useful for treating cancers. The present protein kinase inhibitors are those having the structures of the following formula or pharmaceutically acceptable salts thereof. | 2010-11-25 |
| 20100298386 | COMPOSITIONS AND METHODS FOR TREATING MASTITIS - The present disclosure relates to compositions that are effective in controlling or in preventing mastitis in an animal. The disclosed compositions comprise a biocidal system, comprising a primary biocide and a preservative component; a nonionic surfactant having an HLB of from about 10 to about (20); an emollient system comprising an extradermal penetrating agent and an emollient base; a thickening agent; and an aqueous based carrier. | 2010-11-25 |
| 20100298387 | IL-8 Receptor Antagonists - This invention relates to novel compounds, compositions and combinations thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8). | 2010-11-25 |
| 20100298388 | SUBSTITUTED BENAMIDINES AS ANTIBACTERIAL AGENTS - Compounds of formula (IA) or (IB) have antibacterial activity: wherein W is ═C(H)— or ═N—; R | 2010-11-25 |
| 20100298389 | Novel Imaging Tracers for Early Detection and Treatment of Amyloid Plaques Caused by Alzheimer's Disease and Related Disorders - The present invention relates to compounds and methods for imaging and treating Alzheimer's disease or an amyloidosis-associated pathological condition that utilize a novel amyloid imaging tracer for detecting amyloid deposits in a subject suffering from these conditions. In certain embodiments, the invention relates to [N-2[18F]fluoropropyl]-2-(4′-(methylamino)-phenyl)-6-hydroxybenzothiazole (F-18MHT) and dimers thereof. | 2010-11-25 |
| 20100298390 | INHIBITION OF LETHAL FACTOR PROTEASE ACTIVITY FROM ANTHRAX TOXIN - The present invention provides compounds that efficiently and specifically inhibit lethal factor (LF) protease activity of anthrax toxin. | 2010-11-25 |
| 20100298391 | AMIDE COMPOUNDS AND USE THEREOF FOR PLANT DISEASE CONTROL - The present invention provides an amide compound represented by the formula (1): | 2010-11-25 |
| 20100298392 | Isoindoline Derivatives For The Treatment Of Arrhythmias - There is provided compounds of formula I, wherein R | 2010-11-25 |
| 20100298393 | Modulation of Growth Hormone, DHEA, and Cortisol with Positive Modulators of AMPA Type Glutamate Receptors - Methods for modulating the endocrine system of a mammal are provided. In the subject methods, a positive allosteric modulator of AMPA receptors of the hypothalamus are administered to the host. The subject methods find use in applications where it is desired to increase the baseline circulatory level of a growth hormone in a mammalian host. The subject methods also find use in applications where it is desired to increase the circulatory level of DHEA in a mammalian host. Finally, another subject method also finds use in applications where it is desired to decrease the circulatory level of cortisol in a mammalian host. | 2010-11-25 |
| 20100298394 | ANTIFUNGAL AGENTS AS NEUROPROTECTANTS - Provided herein are compounds, compositions and methods for protecting neuronal and glial cells. | 2010-11-25 |
| 20100298395 | UNSUBSTITUTED AND SUBSTITUTED 4-BENZYL-1,3-DIHYDRO-IMIDAZOLE-2-THIONES ACTING AS SPECIFIC OR SELECTIVE ALPHA2 ADRENERGIC AGONISTS AND METHODS FOR USING THE SAME - Compounds of Formula 1 | 2010-11-25 |
