26th week of 2010 patent applcation highlights part 57 |
Patent application number | Title | Published |
20100168064 | NOVEL HYDROPHILIC DERIVATIVES OF 2-ARYL-4-QUINOLONES AS ANTICANCER AGENTS - 2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120 (Na+ form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and Λ/, Λ/-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities. | 2010-07-01 |
20100168065 | QUINOLINONE DERIVATIVES AS PARP AND TANK INHIBITORS - The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) | 2010-07-01 |
20100168066 | NOVEL INSECTICIDES - Compounds of formula (I) wherein the substituents are as defined in claim ( | 2010-07-01 |
20100168067 | BIOMARKERS FOR BISPHOSPHONATE-RESPONSIVE BONE DISORDERS - This invention relates to the finding that the presence of polymorphisms in and around the farnesyl diphosphate synthase (FDPS) gene is predictive of the densitometric response of patients with bone disorders, such as osteoporosis, subsequent to commencing treatment with amino-bisphosphonates. Methods relating to the identification of individuals having bone disorders which are responsive to bisphosphonates and predicting the responsiveness of individuals with bone disorders to treatment with a bisphosphonate are provided. | 2010-07-01 |
20100168068 | MAO-B INHIBITORS USEFUL FOR TREATING OBESITY - The invention provides novel compounds of formulae I and II: | 2010-07-01 |
20100168069 | INSECT REPELLENT - The invention provides an insect repellent composition that repels flies, gnats, mosquitoes, lice, ticks, and fleas. The insect repellent composition includes an effective amount of a phosphorous containing compound having the formula (RO) | 2010-07-01 |
20100168070 | COMPOUNDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE - The invention relates to substituted 1,2-ethylenediamines of general formula (I), | 2010-07-01 |
20100168071 | EXTENDED ESTROGEN DOSING CONTRACEPTIVE REGIMEN - A contraceptive kit comprising a package containing daily dosages of: (a) a first composition containing a progestin in an amount equivalent to about 0.3 to about 1.5 mg norethindrone acetate and an estrogen in an amount equivalent to about 5 to about 20 mcg of ethinyl estradiol for about 22 to about 26 days; (b) a second composition containing an estrogen in an amount equivalent to about 5 to about 20 mcg of ethinyl estradiol for about 2 to about 3 days and an optional third composition that is a placebo provided that (i) if estrogen administration is continuous then the first composition is administered for 25 to 26 days, the second composition is administered for 2 to 3 days and no third composition is administered and (ii) if estrogen administration is not continuous then the first composition is administered for 22 to 24 days, the second composition is administered for 2 to 3 days and the third composition is administered for 1 to 4 days. The total cycle length is 28 days, with the first composition administered on day 1 of the menstrual cycle, defined as the first day of menstrual bleeding, or on the first Sunday after the first day of the menstrual cycle. | 2010-07-01 |
20100168072 | Drug Combinations for the Treatment of Duchenne Muscular Dystrophy - Combinations comprising (or consisting essentially of) one or more compounds of the formula (I) or (II) with one or more ancillary compounds, to processes for preparing the combinations, and to various therapeutic uses of the combinations. Also provided are pharmaceutical compositions containing the combinations as well as a method of treatment of Duchenne muscular dystrophy, Becker muscular dystrophy or cachexia using the combinations. | 2010-07-01 |
20100168073 | METHOD FOR TREATING AND/OR PREVENTING RETINAL DISEASES WITH SUSTAINED RELEASE CORTICOSTEROIDS - The present invention relates to a method for administering a corticosteroid to a posterior segment of an eye. In the method, a sustained release device is implanted to deliver the corticosteroid to the eye. The aqueous corticosteroid concentration remains less than vitreous corticosteroid concentration during release of the corticosteroid from the device. | 2010-07-01 |
20100168074 | Freezable Unit Dosage Delivery System and Method of Preparation - A freezable unit dosage delivery system, method of preparation, a solid unit dosage, method of treating symptoms and conditions, and kit is disclosed. The freezable unit dosage delivery system includes a composition, preferably containing one or more medicinal ingredients, having a freezing point less than 5° C.; a storage container comprising one or more cavity, each configured to receive a unit dosage quantity of the composition; and a sealing sheet for sealing engagement with the storage container. Upon freezing, the unit dosage quantity solidifies into a solid unit dosage that may be administered one of orally, rectally or vaginally for the local or systemic treatment of symptoms and conditions in a human. | 2010-07-01 |
20100168075 | Novel 2-Azetidinone Derivatives As Cholesterol Absorption Inhibitors For The Treatment Of Hyperlipidaemic Conditions - The application relates to novel 2-azetidinone derivatives of formula (I) and pharmaceutically acceptable salts, solvates and prodrugs thereof. The compounds are cholesterol absorption inhibitors and are useful in the treatment of hyperlipidaemic conditions, including atherosclerosis, Alzheimers' disease and cholesterol associated tumours. The application also relates to pharmaceutical formulations comprising such compounds and to processes for their preparation. | 2010-07-01 |
20100168076 | DIPHENYL SUBSTITUTED ALKANES - The instant invention provides compounds of Formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents. | 2010-07-01 |
20100168077 | Novel Pyridine Derivatives, Processes for Preparing Them, Pharmaceutical Compositions Thereof - The present invention concerns 2-amino pyridine derivatives of formula 1 processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals. | 2010-07-01 |
20100168078 | S1P RECEPTOR MODULATORS FOR TREATING MULTIPLE SCLEROSIS - The present invention relates uses of an S1P receptor modulator such as 2-substituted 2-amino-propane-1,3-diol or 2-amino-propanol derivatives, e.g. a compound comprising a group of formula X | 2010-07-01 |
20100168079 | Biaryl Benzylamine Derivatives - The present invention relates to biaryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them. | 2010-07-01 |
20100168080 | NOVEL COMPOUNDS USEFUL AS CC CHEMOKINE RECEPTOR LIGANDS - The present invention relates to novel morpholine, oxazapane and piperidine derivatives that act as ligands for CC chemokine receptors, such as CCR1. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds. | 2010-07-01 |
20100168081 | GALANTAMINE AS A NEUROPROTECTIVE DRUG FOR RETINAL GANGLION CELLS - The present invention relates to the use of galantamine for neuroprotection of retinal ganglion cells. | 2010-07-01 |
20100168082 | Heterobicyclic Carboxamides as inhibitors for kinases - The invention relates to novel organic compounds of formula (I) | 2010-07-01 |
20100168083 | ADAMANTANE DERIVATIVES FOR THE TREATMENT OF THE METABOLIC SYNDROME - Novel substituted adamantane based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome. | 2010-07-01 |
20100168084 | Therapeutic compounds and related methods of use - Methods of using compounds that are HAT inhibitors are described herein. | 2010-07-01 |
20100168085 | Dopamine and agonists and antagonists thereof for modulation of suppressive activity of CD4+CD25+ regulatory T cells - Compositions and methods for modulation of the suppressive activity of CD4+CD25+regulatory T cells (Treg) on CD4+CD25− effector T cells (Teff) are provided. An agent selected from: (i) dopamine; (ii) a dopamine precursor; (iii) a D1-R agonist; (iv) a D2-R antagonist; (v) a combination of (i) and (ii); or (vi) a combination of (i), (ii) or (iii) with (iv), down-regulates the suppressive activity of Treg and is useful for treatment of cancer. An agent selected from (i) a dopamine D2-R agonist, (ii) a dopamine D1-R antagonist, and (iii) a combination of (i) and (ii), up-regulates the suppressive activity of Treg and is useful for treatment of an autoimmune disease or for controlling graft rejection in tissue/organ transplantation. | 2010-07-01 |
20100168086 | 7,8,10,10A-TETRAHYDRO-6H-BENZO[C]CHROMEN-9(6AH)-ONE MODULATORS OF CANNABINOID RECEPTORS - The present invention relates to new 7,8,10,10a-tetrahydro-6H-benzo[c]chromen-9(6aH)-one modulators of cannabinoid receptors, pharmaceutical compositions thereof, and methods of use thereof. | 2010-07-01 |
20100168087 | BENZO[1,2,3]THIADIAZINE DERIVATES - The present invention relates to new benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the general Formula (I), medicaments containing such compounds and the use thereof in the medicine. Benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the general Formula (I) are suitable for the prevention or treatment of the diseases of the central nervous system. | 2010-07-01 |
20100168088 | PYRROLIDINE DERIVATIVES AS NK-3 RECEPTOR ANTAGONISTS - The present invention relates to a compound of formula I | 2010-07-01 |
20100168089 | UTILIZATION OF TACE INHIBITORS FOR THE TREATMENT OF ACNE - An in vitro method of screening for candidate compounds for the preventive or curative treatment of acne entails determination of the ability of a compound to inhibit the expression or the activity of TACE, and also to the administration of inhibitors of the expression or of the activity of this enzyme, in the treatment of acne. | 2010-07-01 |
20100168090 | Active Ingredient Combinations With Insecticidal and Acaricidal Properties - The novel active compound combinations comprising compounds of the formula (I-1) or (I-2) and the agonists or antagonists of nicotinergic acetylcholine receptors listed in the description have very good insecticidal and/or acaricidal properties. | 2010-07-01 |
20100168091 | Imidazole Amines As Inhibitors Of Beta-secretase - The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated 3-amyloid deposits or 3-amyloid levels in a patient. | 2010-07-01 |
20100168092 | PHARMACEUTICAL COMPOSITION WITH ANTI-DIABETIC ACTION - The invention relates to medicine, in particular to searching and developing novel medicinal agent for treating pancreatic diabetes. The invention is based on the development of more effective and less toxic medicinal agents based on indole derivatives which exhibit antidiabetic, hypolipidemic, hypoglycemic, hypocholesterolemic activity and insulin resistance-improving actions and the structure of which differs from the structure of traditionally used compounds. The inventive indole derivatives are also low-toxic and easily tolerated. | 2010-07-01 |
20100168093 | SUBSTITUTED 3-AMINO-4 -HYDROXY PYRROLIDINES COMPOUNDS, THEIR PREPARATION AND USE AS MEDICAMENTS - The present invention relates to substituted pyrrolidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animal. | 2010-07-01 |
20100168094 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators. | 2010-07-01 |
20100168095 | MULTI-CYCLIC CINNAMIDE DERIVATIVES - The present invention provides a compound represented by the formula (I): | 2010-07-01 |
20100168096 | ACYLGUANIDINE DERIVATIVE OR SALT THEREOF - [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT | 2010-07-01 |
20100168097 | Non-Nucleoside Reverse Transcriptase Inhibitors - Compounds of Formula I: Formula (I); are HIV reverse transcriptase inhibitors, wherein R | 2010-07-01 |
20100168098 | Viral Polymerase Inhibitors - The present invention relates to compounds represented by formula (I) wherein A, B, D, E, R | 2010-07-01 |
20100168099 | 1H-QUINOLIN-4-ONE COMPOUNDS, WITH AFFINITY FOR THE GABA RECEPTOR, PROCESSES, USES AND COMPOSITIONS - The invention provides new 1H-quinolin-4-one compounds of formula (I), wherein R | 2010-07-01 |
20100168100 | QUINOLINE DERIVATIVES AS P13 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives. | 2010-07-01 |
20100168101 | OXINDOLE HYDRAZIDE MODULATORS OF PROTEIN TYROSINE PHOSPHATASES (PTPS) - The present invention is related to the use of oxindole hydrazide derivatives of formula (I) for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, obesity, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of oxindole hydrazide derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs, in particular of PTP1B, TC-PTP, SHP and GLEPP-1. The present invention is furthermore related to novel oxindole hydrazide derivatives and method of preparation thereof. | 2010-07-01 |
20100168102 | Amide Derivatives as Kinase Inhibitors - The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar | 2010-07-01 |
20100168103 | DIARYL PIPERIDINE COMPOUNDS AS CALCIUM CHANNEL BLOCKERS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of diaryl piperidine compounds are disclosed of the general formula (I) where X is a linker and Y may be C, O, S or N. | 2010-07-01 |
20100168104 | HIV INHIBITING 5-AMIDO SUBSTITUTED PYRIMIDINES - This invention concerns pyrimidine derivatives of formula | 2010-07-01 |
20100168105 | Spirocyclopropyl Piperidine Derivatives - Disclosed herein is at least one piperidine derivative, at least one pharmaceutical composition comprising at least one piperidine derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith | 2010-07-01 |
20100168106 | Amino-5-(5-membered)heteroarylimidazolone Compounds And The Use Thereof For Beta-secretase Modulation - The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I | 2010-07-01 |
20100168107 | IMIDAZOLE COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS - The present invention relates to compounds of the Formula I | 2010-07-01 |
20100168108 | PHENYL DERIVATIVES AND METHODS OF USE - Novel phenyl compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, genitourinary disorders, inflammation, glaucoma, auto-immune diseases, ischemic conditions, immune-related disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, and as an appetite stimulant. | 2010-07-01 |
20100168109 | PHARMACEUTICAL COMPOSITIONS OF 1,2,4-OXADIAZOLE BENZOIC ACID AND THEIR USE FOR THE TREATMENT OF DISEASE - Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith. | 2010-07-01 |
20100168110 | Novel Compounds - The present invention discloses a novel thyroid like compounds of formula (I), wherein R | 2010-07-01 |
20100168111 | POLYMORPHIC FORM OF 5 CHLORO N {[(5S) 2 OXO 3 [4 (3 OXOMORPHOLIN 4 YL)PHENYL]OXA-ZOLIDIN 5 YL]-METHYL}THIOPHENE 2 CARBOXAMIDE - A polymorphic form of rivaroxaban, 5-chloro-N-{[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]oxa-zolidin-5-yl]-methyl}thiophene-2-carboxamide (termed form APO-A), processes for the preparation thereof, and compositions and formulations comprising form APO-A are provided. Also provided are compositions comprising a crystalline form of rivaroxaban and solvents selected from C3 to C6 ketones, C3 to C4 amides and mixtures thereof. | 2010-07-01 |
20100168112 | 2-Substituted and 4-substituted aryl nitrone compounds - The present invention provides aryl nitrones, compositions comprising the same and methods of their use for the treatment or prevention of oxidative, ischemic, ischemia/reperfusion-related and chemokine mediated conditions. | 2010-07-01 |
20100168113 | Pharmaceutical Compounds - This invention relates to novel substituted nitrocatechol derivatives, their use in the treatment of some central and peripheral nervous system disorders and pharmaceutical compositions containing them. | 2010-07-01 |
20100168114 | INVERTEBRATE ACETYLCHOLINESTERASE INHIBITORS - Methods for determining invertebrate- and insect-specific, such as mosquito-specific, residues of acetylcholinesterases are provided herein. The methods can be used to design pesticides and insecticides that are specific for the invertebrate or insect (e.g., mosquito) enzymes, resulting in reduced toxicity concerns for mammals. Compositions for inhibiting invertebrate and insect (e.g., mosquito) acetylcholinesterases and methods for preparing the same are also provided. | 2010-07-01 |
20100168115 | USE OF TRIAZINE DERIVATIVES FOR THE MANUFACTURE OF A MEDICAMENT HAVING A CICATRISING OR ANGIOGENIC EFFECT - The present patent application relates to the use of triazine derivatives as cicatrising or angiogenic agents, wherein the triazine is a molecule of formula (I). | 2010-07-01 |
20100168116 | 3,6-SUBSTITUTED IMIDAZOL[1,2-B]PYRIDAZINE ANALOGS FOR TREATING ALLERGIC AND INFLAMMATORY DISEASES - Methods for treating an allergic or inflammatory disease or other Syk-mediated disease or Syk-mediated condition characterized by administering a composition which contains a therapeutically effective amount of a 3,6-substituted imidazol[1,2-b]pyridazine compound. | 2010-07-01 |
20100168117 | A PROCESS FOR THE PREPARATION OF THE STABLE, AMORPHOUS CALCIUM SALT OF (6S)-N(5)-METHYL-5,6,7,8-TETRAHYDROFOLIC ACID - A process for the preparation of an aqueous solution of the calcium salt of (6S)-N(5)-methyl-5,6,7,8-tetrahydrofolic acid, whereby (6S)-5,6,7,8-tetrahydrofolic acid having a content of the corresponding (6R)-diastereoisomer in the range from 4% by weight to 8% by weight is methylated in water comprises: treating the methylated reaction mixture with calcium chloride; crystallizing the calcium salt of (6RS)-N(5)-methyl-5,6,7,8-tetrahydrofolic acid from the resulting aqueous solution; and obtaining an aqueous solution of the calcium salt of (6S)-N(5)-methyl-5,6,7,8-tetrahydrofolic acid. | 2010-07-01 |
20100168118 | Methods to Treat Cancer with 10-propargyl-10-deazaaminopterin and Methods for Assessing Cancer for Increased Sensitivity to 10-propargyl-10-deazaaminopterin - The present invention relates to a method for assessing the sensitivity of a patient's cancer to treatment with 10-propargyl-10-deazaminopterin and a method for selecting a patient for treatment of cancer with 10-propargyl-10-deazaminopterin, by determining the amount of a selected polypeptide expressed by the cancer and comparing the amount with the amount of the selected polypeptide expressed by a reference cancer, wherein the polypeptide includes a member of folate pathways within cells and may include at least one of reduced folate carrier-1 enzyme (RFC-1), dihydrofolate reductase (DHFR), folylpoly-gamma-glutamate synthetase (FPGS), thymidylate synthase (TS), γ-glutamyl hydrolase (GGH), and glycinamide ribonucleotide formyltransferase (GARFT). The present invention also relates to the use of 10-propargyl-10-deazaminopterin in the treatment of multiple myeloma. | 2010-07-01 |
20100168119 | COMPOSITIONS AND METHODS FOR MINIMIZING OR REDUCING AGONIST-INDUCED DESENSITIZATION - Methods and compositions are provided for preventing or reversing loss of the therapeutic effect of a drug, where the loss is associated with the repeated administration of the drug to a patient. The method includes administering to the patient a dopamine receptor agonist or partial agonist or a drug that increases the extracellular level of dopamine by enhancing release of dopamine, decreasing the removal of dopamine from the extracellular space, enhancing the synthesis of dopamine within the brain, or decreasing metabolic degradation of dopamine; and also administering to the patient an opioid receptor antagonist in an ultra-low dose amount, wherein the ultra-low dose amount is effective to prevent or reverse loss of therapeutic effects associated with the repeated administration of the drug to the patient. The methods are useful for various treatments, including treating Parkinson's Disease, Restless Leg Syndrome, depression, schizophrenia, psychostimulant drug abuse, or attention deficit disorder. | 2010-07-01 |
20100168120 | SALTS OF PYRIDAZINE COMPOUNDS - The invention relates to stable and substantially purified synthetic pharmaceutically acceptable acid addition salts of pyridazine compounds of the formula I wherein R10 is hydrogen, hydroxyl, alkyl, alkoxy, alkenyl, alkynyl, alkylene, aryl, heteroaryl, sulfonyl, sulfinyl, sulfenyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, =0, ═S, carboxyl, carbonyl, carbamoyl, carboxamide, or phosphonate, and R11 is alkyl, alkoxy, alkenyl, alkynyl, alkylene, alkenylene, alkenyloxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfonyl, sulfinyl, sulfenyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, =0, ═S, phosphonate, carboxyl, carbonyl, carbamoyl, carboxamide, or ureido. The invention also relates to formulations, dosage forms and compositions comprising the salts, and methods of using the salts, formulations, dosage forms and compositions. | 2010-07-01 |
20100168121 | COMPOUNDS WITH 5-HT1A ACTIVITY USEFUL FOR TREATING DISORDERS OF THE OUTER RETINA - Compositions and methods for treating disorders of the outer retina with compounds with 5-HT | 2010-07-01 |
20100168122 | XANTHINE DERIVATIVES AS SELECTIVE HM74A AGONISTS - The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for manufacture of said derivatives, pharmaceutical formulations containing these compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial | 2010-07-01 |
20100168123 | AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: | 2010-07-01 |
20100168124 | NOVEL HETEROCYCLIC SUBSTITUTED PYRIDINE COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY - The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: | 2010-07-01 |
20100168125 | INDOLIZINES AND AZA-ANALOG DERIVATIVES THEREOF AS CNS ACTIVE COMPOUNDS - The present application relates to indolizine-based compounds of the general formula (I) and aza-analogs thereof, which have medical utility, for example as antipsychotics. | 2010-07-01 |
20100168126 | Cosmetic Use of 1-Aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine Carbomamides and Related Compounds - Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging. | 2010-07-01 |
20100168127 | Cosmetic Use of 1-Aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine Carbomamides and Related Compounds - Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging. | 2010-07-01 |
20100168128 | SMALL-MOLECULE INHIBITORS OF THE ANDROGEN RECEPTOR - The present invention provides a method of inhibiting an androgen receptor by administering a compound of Formula I: | 2010-07-01 |
20100168129 | DRUGS WITH ANTICHOLESTATIC ACTIVITY - New compounds belonging to the structural formula (I) are described. | 2010-07-01 |
20100168130 | Diarylmethyl Piperazine Derivatives, Preparations Thereof and Uses Thereof - Compounds of general formula: | 2010-07-01 |
20100168131 | NOVEL COMPOUNDS - Disclosed are N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives and their use as pharmaceuticals. | 2010-07-01 |
20100168132 | QUINUCLIDINE DERIVATIVES AND THEIR USE AS MUSCARINIC M3 RECEPTOR ANTAGONISTS - Compounds of Formula (I) ; in salt or zwitterionic form wherein R | 2010-07-01 |
20100168133 | USE OF SUBSTITUTED QUINOLINE DERIVATIVES FOR THE TREATMENT OF DRUG RESISTANT MYCOBACTERIAL DISEASES - The present invention relates to the use of a substituted quinoline derivative for the preparation of a medicament for the treatment of an infection with a drug resistant | 2010-07-01 |
20100168134 | PYRIDYL PIPERIDINE OREXIN RECEPTOR ANTAGONISTS - The present invention is. directed to pyridyl piperidine compounds of formula (I) which are antagonists of orexin receptors, and which are useful' in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 2010-07-01 |
20100168135 | Method of Inducing Cleavage of Amyloid Precursor Protein to Form a Novel Fragment - The present invention provides a method of inducing cleavage of amyloid precursor protein to produce an approximately 17 kilodalton carboxy-terminal fragment of amyloid precursor protein in a subject, the method comprising administering a heterocyclic compound or a pharmaceutically acceptable salt, hydrate or prodrug thereof to a subject in need thereof, wherein the approximately 17 kilodalton fragment includes the carboxyterminal amino acid sequence of amyloid precursor protein and amyloid-beta amino acid sequence. Also provided is a screening method for identifying compounds induce cleavage of amyloid precursor protein to produce the approximately 17 kilodalton carboxy-terminal fragment of amyloid precursor protein. | 2010-07-01 |
20100168136 | ALKYLSULFONE DERIVATIVES - A compound having activity to inhibit production and/or secretion of β-amyloid protein, and is useful for prevention and/or treatment of various diseases associated with abnormal production and/or secretion of β-amyloid protein, the compound represented by the general formula (I): | 2010-07-01 |
20100168137 | COMBINATION FOR USE IN THE TREATMENT OF INFLAMMATORY DISORDERS - There is provided combination products comprising (a) pemirolast, or a pharmaceutically-acceptable salt or solvate thereof; and (b) ramatroban, or a pharmaceutically-acceptable salt or solvate thereof. Such combination products find particular utility in the treatment of atherosclerosis and related conditions. | 2010-07-01 |
20100168138 | Anti-Viral Compounds - Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection. | 2010-07-01 |
20100168139 | INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA - Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo. | 2010-07-01 |
20100168140 | Easily Absorbable Oral Preparations of Xanthine Derivatives - An object of the present invention is to provide an easily absorbable oral preparation containing a xanthine derivative or a pharmaceutically acceptable salt thereof and a fatty acid or a fatty acid derivative for the purpose of providing an easily absorbable oral preparation containing the xanthine derivative of which absorbability has been enhanced by dissolving the xanthine derivative that shows adenosine A | 2010-07-01 |
20100168141 | AZETIDINE ANALOGUES NUCLEOSIDASE AND PHOSPHORYLASE INHIBITORS - Azetidine analogues of nucleosidase and nucleoside phosphorylase inhibitors having the general formula (I), the use of these compounds as pharmaceuticals, pharmaceutical compositions containing the compounds, methods of treating certain diseases using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds wherein W and X are each independently selected from hydrogen, CH | 2010-07-01 |
20100168142 | SALTS OF 4-ANILINE QUINAZOLINE DERIVATIVE - The present invention relates to salt forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide, methods for preparation thereof, pharmaceutical compositions comprising the same and their use thereof. The salt forms of the present invention, which possess excellent tumor inhibitory activity, good bioavailability and low toxicity in an animal body, are suitable for the use of preparation of anti-tumor medicaments. | 2010-07-01 |
20100168143 | QUINAZOLINE DERIVATIVES - The invention provided a compound of formula (I) for use in the treatment of disease, in particular proliferative diseases such as cancer and for use in the preparation of medicaments for use in the treatment of proliferative diseases; the invention also processes for the preparation of such compounds, as well as pharmaceutical compositions containing them as active ingredient. | 2010-07-01 |
20100168144 | INHIBITORS OF PROTEIN KINASES - The present invention relates to inhibitors of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to methods of preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases. formula (I). | 2010-07-01 |
20100168145 | FUSED IMIDAZOLE DERIVATIVES AND USE THEREOF AS ALDOSTERONE SYNTHASE INHIBITORS - The patent application relates to new heterocyclic compounds of the general formula (I) in which A, R, R | 2010-07-01 |
20100168146 | Composition Comprising (R)-Spiro[L-Azabicyclo[2.2.2]Octane-3,2'(3'H)-Furo[2,3-B]Pyridine (AZD0328) and its Use in the Treatment of Alzheimer's Disease, ADHD or Cognitive Dysfunction - A pharmaceutical composition comprising (R)-spiro[1-azabicyclo[2.2.2]octane-3,2′(3′H)-furo[2,3-b]pyridine (AZD0328) and its use in the treatment of subjects suffering from schizophrenia, Alzheimer's disease or other conditions with impaired cognitive function. | 2010-07-01 |
20100168147 | Medicinal Compositions Comprising Buprenorphine And Naloxone - There is provided a composition for the treatment of pain in human patients wherein said composition comprises buprenorphine to naloxone in a ratio by weight of from 2.1:1 to 8:1, the amount of buprenorphine and naloxone being suitable to provide analgesia, the composition being in a transdermal or transmucosal dosage form. Also provided are an associated method and use. | 2010-07-01 |
20100168148 | Pharmaceutical formulation containing gelling agent - Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient. | 2010-07-01 |
20100168149 | Camptothecin Analogue Compounds, a Process for Their Preparation and Pharmaceutical Compositions Containing Them - Compound of formula (I): | 2010-07-01 |
20100168150 | Camptothecin Analogue Compounds, a Process for Their Preparation and Pharmaceutical Compositions Containing Them. - Compound of formula (I): | 2010-07-01 |
20100168151 | NOVEL PROCESSES FOR PREPARING 6-(DIFLUOROMETHOXY)[1]BENZOFURO[3,2-C]PYRIDINE-9-CARBALDEHYDE, A NOVEL INTERMEDIATE FOR THE SYNTHESIS OF PDE IV INHIBITORS - The present invention relates to novel processes for preparing 6-(difluoromethoxy)[1] benzofuro[3,2-c]pyridine-9-carbaldehyde, which is a novel and useful intermediate for preparing compounds with PDE4 inhibitory activity, such as 3,5-dichloro-4-(6-difluoromethoxybenzo[4,5]furo[3,2-c]pyridin-9-ylcarboxamido)-1-pyridiniumolate. | 2010-07-01 |
20100168152 | Fat regulation - The present invention provides methods and compounds for regulating fat metabolism and achieving fat homeostasis in a subject. Methods and compound for regulating body weight, reducing body fat, and inducing weight loss are also provided, as are methods and compounds for treating or preventing obesity and for preventing or treating conditions associated with altered fat metabolism including, e.g., obesity, diabetes, atherosclerosis, etc. | 2010-07-01 |
20100168153 | Salts and crystall forms of 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]q- uinolin-1-yl)-phenyl]-propionitrile - The invention relates to particular crystalline forms of 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile, its hydrates and solvates, its salts and hydrates and solvates of its salts, certain processes for their preparation, pharmaceutical compositions containing these crystalline forms, and their use in diagnostic methods or, preferably, for the therapeutic treatment of warm-blooded animals, especially humans, and their use as an intermediate or for the preparation of pharmaceutical preparations for use in diagnostic methods or, preferably, for the therapeutic treatment of warm-blooded animals, especially humans. | 2010-07-01 |
20100168154 | 1-SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUND - Provided is a compound useful as an N-type Ca | 2010-07-01 |
20100168155 | DERIVATIVES OF IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS - The present invention is related to a compound of formula (I): | 2010-07-01 |
20100168156 | Novel Benzoxathiine Derivative - Disclosed is a compound represented by the formula (I) below and a pharmaceutically acceptable salt thereof. | 2010-07-01 |
20100168157 | PREVENTIVE AND THERAPEUTIC MEDICAMENT FOR GASTROESOPHAGEAL REFLUX DISEASE - The compound of the following formula: | 2010-07-01 |
20100168158 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 2010-07-01 |
20100168159 | HETERO COMPOUND | 2010-07-01 |
20100168160 | Genipin Derivatives and Uses Thereof - Genipin derivatives and pharmaceutical compositions thereof that inhibit the activity of uncoupling protein-2 (UCP2) and are useful in treating deficient first-phase insulin secretion, non-insulin dependent diabetes mellitus, and ischemia in a mammal are disclosed. | 2010-07-01 |
20100168161 | DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL)PHENOL AS AGONISTS OF THE BETA2 ADRENERGIC RECEPTOR - The present relates to compounds of formula (I): | 2010-07-01 |
20100168162 | SELECTIVE INHIBITORS OF AKT AND METHODS OF USING SAME - The present invention describes an improved method for screening compounds for activity in inhibiting the enzymatic activity of Akt1 protein kinase, also known as Protein Kinase B, an enzyme that is believed to play a key role in the inhibition of apoptosis and thus in the etiology of cancer and other conditions, including neurodegenerative diseases. In general, the method comprises: (1) providing a plurality of compounds suspected of having Akt1 kinase inhibitory activity; (2) modeling the docking of each of the plurality of the compounds with a target binding site derived from the crystal structure of a ternary complex involving Akt1, a nonhydrolyzable ATP analogue, and a peptide substrate derived from a physiological AKT substrate such that the protein active site is defined including those residues within a defined distance from the nonhydrolyzable ATP analogue; (3) ranking the docked compounds by goodness of fit; (4) further selecting compounds from compounds high ranked by goodness of fit in docking by using one or more screening criteria; (5) optionally, visually analyzing structures of compounds selected in step (4) to remove any compounds with improbable docking geometry; and (6) experimentally testing the selected compounds from step (4) or step (5), if step (5) is performed, to determine their inhibitory activity against Akt1 in order to select compounds with Akt1 inhibitory activity. The invention also encompasses pharmaceutical compositions including compounds whose inhibitory activity against Akt1 is discovered by the screening method, as well as methods of use of the pharmaceutical compositions to treat cancer and other conditions. | 2010-07-01 |
20100168163 | CYCLIC-ALKYLAMINE DERIVATIVES AS INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 - The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, t, R | 2010-07-01 |