| Entries |
| Document | Title | Date |
|---|
| 20080200446 | Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof - The present invention provides compounds represented by the structural formula (I): | 08-21-2008 |
| 20080207585 | Substituted Azetidinone Compounds, Processes for Preparing the Same, Formulations and Uses Thereof - The present invention provides compounds represented by the structural formula (I): | 08-28-2008 |
| 20080234248 | Substituted Azetidinone Compounds, Processes for Preparing the Same, Formulations and Uses Thereof - The present invention provides compounds represented by the structural formula (I): | 09-25-2008 |
| 20080242653 | Cyclopropyl amine derivatives - Compounds of formula (I) | 10-02-2008 |
| 20080255084 | Combination of Organic Compounds - The invention relates to a combination, such as a combined preparation or a pharmaceutical composition, respectively comprising
| 10-16-2008 |
| 20080261942 | COMBINATIONS OF BILE ACID SEQUESTRANT(S) AND STEROL ABSORPTION INHIBITOR(S) AND TREATMENTS FOR VASCULAR INDICATIONS - The present invention provides compositions, therapeutic combinations and methods including: (a) at least one bile acid sequestrant; and (b) at least one substituted azetidinone or substituted β-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols. | 10-23-2008 |
| 20080269188 | Oatp-C Gene C463a Polymorphism Underlies Variable Response to Statin Therapy - The present invention relates to a method for determining variable response to statin therapy in patients afflicted with or susceptible to develop cardiovascular diseases, hypercholesterolemia, Diabetes and metabolic disorders involving high baseline plasma lipid level such as high LDL-C level, comprising detecting the presence or absence of the Pro 155T hr (C463A) variant in the Organic Anion Transporting Polypeptide-C(OATP-C) gene, wherein the presence of said variant is indicative of superior response to statin therapy. It also concerns tailored treatment of different populations of patients according to the Pro155Thr (C463A) variant genotype. | 10-30-2008 |
| 20080275020 | PHARMACEUTICAL FORMULATION - The instant invention provides a pharmaceutical composition comprised of a cholesterol absorption inhibitor and an HMG-CoA reductase inhibitor, one or more anti-oxidants, microcrystalline cellulose, hydroxypropyl methylcellulose, magnesium stearate and lactose. The composition need not contain ascorbic acid in order to obtain desirable stability. | 11-06-2008 |
| 20080280869 | Pyrazole or Triazole Compounds and Their Use for the Manufacture of a Medicament for Treating Somatic Mutation-Related Diseases - The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA. | 11-13-2008 |
| 20080280870 | Beta-Lactamyl Phenylalanine, Cysteine, and Serine Vasopressin Antagonists - Substituted 2-(azetidin-2-on-1-yl)alkoxyalkylalkanoic acids and 2-(azetidin-2-on-1-yl)arylalkylalkanoic acids, and analogs and derivatives thereof are described. Methods for using the described compounds, and pharmaceutical compositions thereof, to treat disease states responsive to antagonism of one or more vasopressin receptors are also described. | 11-13-2008 |
| 20080300233 | Pharmaceutical Composition Comprising Simvastatin and Ezetimibe - The present invention relates to the field of pharmaceutical technology and in particular to novel dosage forms of medicaments containing as active ingredients simvastatin and ezetimibe, or pharmaceutically acceptable salts thereof. The present pharmaceutical compositions are characterized in that the contact of the compositions with oxygen is substantially reduced, such as by coating the composition, providing a medicament useful for the treatment and prevention of atherosclerosis and related conditions, in an environment having an essentially reduced oxygen or humidity, respectively, content. | 12-04-2008 |
| 20080318920 | DEUTERIUM-ENRICHED EZETIMIBE - The present application describes deuterium-enriched ezetimibe, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 12-25-2008 |
| 20090023701 | Cytokine Inhibitors - Disclosed are compounds of formula (I) | 01-22-2009 |
| 20090054393 | METHODS FOR TREATING DISORDERS ASSOCIATED WITH HYPERLIPIDEMIA IN A MAMMAL - The invention is directed to methods for treating hyperlipidemia in a mammal. The methods involve combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, BMS-201038 and implitade) and a cholesterol absorption inhibitor (CAI) (for example, ezetimibe). Co-administration of the MTP inhibitor with the CAI produces a therapeutic benefit, for example, a reduction in the concentration of cholesterol and/or triglycerides in the blood stream, but with fewer or reduced side effects than when higher dosages of the MTP inhibitor are used during monotherapy to provide the same or similar therapeutic benefit. | 02-26-2009 |
| 20090069285 | Diphenylazetidinone Derivatives Possessing Cholesterol Absorption Inhibitor Activity - 2-azetidinone derivatives and pharmaceutical compositions containing them. The compounds are useful in the treatment of hyperlipidemic conditions, atherosclerosis, Alzheimers' disease and cholesterol associated tumours. | 03-12-2009 |
| 20090105208 | Substituted Piperazines as CB1 Antagonists - Compounds of Formula (I): | 04-23-2009 |
| 20090131395 | BIPHENYLAZETIDINONE CHOLESTEROL ABSORPTION INHIBITORS - The invention relates to a chemical genus of 4-biphenyl-1-phenylazetidin-2-ones useful in the treatment of hypercholesterolemia and other disorders. The compounds have the general formula I: | 05-21-2009 |
| 20090131396 | TREATMENT OF CARDIOVASCULAR DISEASE AND DYSLIPIDEMIA USING SECRETORY PHOSPHOLIPASE A2 (SPLA2) INHIBITORS AND SPLA2 INHIBITOR COMBINATION THERAPIES - Administration of sPLA | 05-21-2009 |
| 20090137546 | Anti-Hypercholesterolemic Compounds - This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events. | 05-28-2009 |
| 20090137547 | Heterobicyclic metalloprotease inhibitors - The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors. | 05-28-2009 |
| 20090143351 | SUBSTITUTED AZETIDINONES - Compounds are provided which have the structure | 06-04-2009 |
| 20090149437 | THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS - A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions. | 06-11-2009 |
| 20090156572 | Nitrogen-containing heterocyclic compound and use thereof - The present invention relates to a compound represented by the formula | 06-18-2009 |
| 20090170825 | BETA-LACTAMYLALKANOIC ACIDS FOR TREATING PREMENSTRUAL DISORDERS - 0-lactamyl alkanoic acids are described. Methods for treating various premenstrual disorders using or more O-lactamyl alkanoic acids are also described. | 07-02-2009 |
| 20090186866 | THERAPEUTIC BETA-LACTAMS - Compounds comprising | 07-23-2009 |
| 20090192135 | Human Niemann Pick C1-Like 1 Gene (NPC1L1) Polymorphisms and Methods of Use Thereof - The present invention relates to the identification and use of single nucleotide polymorphisms and haplotypes in the Niemann Pick C1-Like 1 (NPC1L1) gene. In particular, methods are provided for correlating NPC1L1 polymorphisms and haplo-types with the responsiveness of a pharmaceutically active compound administered to a human subject. The invention further relates to a method for estimating the responsiveness of a pharmaceutically active compound administered to a human subject which method comprises determining at least one polymorphism in the NPC1L1 gene. The methods are based on determining polymorphisms in the NPC1L1 gene and correlating the responsiveness of a pharmaceutically active compound in the human by reference to one or more polymorphism in NPC1L1. The invention further relates to isolated nucleic acids comprising within their sequence the polymorphisms as defined herein, to nucleic acid primers and oligonucleotide probes capable of hybridizing to such nucleic acids and to a diagnostic kit comprising one or more of such primers and probes for detecting a polymorphism in the NPC1L1 gene. | 07-30-2009 |
| 20090197858 | HYPERCHOLESTROLEMIA AND TENDINOUS INJURIES - This invention provides compositions and methods of inhibiting, suppressing, or treating a tendinous or musculoskeletal soft tissue injury. The invention further provides a method of ameliorating symptoms associated with a tendinous or musculoskeletal soft tissue injury. Additionally, the invention provides methods for evaluating the risk of developing a tendinous or musculoskeletal soft tissue injury. | 08-06-2009 |
| 20090209510 | Novel Method of Treating Hyperlipidemia - A pharmaceutical composition useful for a prevention and/or treatment of hyperlipidemia, which comprises combining an effective amount of squalene synthase inhibitor and HMG-CoA reductase inhibitor is provided. | 08-20-2009 |
| 20090215740 | THERAPEUTIC SUBSTITUTED BETA-LACTAMS - A compound having a structure | 08-27-2009 |
| 20090221546 | INHIBITORS OF FACTOR XA AND OTHER SERINE PROTEASES INVOLVED IN THE COAGULATION CASCADE - Compounds useful as intermediates for synthesis of compounds of Formula (1): | 09-03-2009 |
| 20090247499 | SULFONYLATED PIPERAZINES AS CANNABINOID-1 RECEPTOR MODULATORS - Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequalae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness. | 10-01-2009 |
| 20090253672 | Cathepsin Cysteine Protease Inhibitors - This invention relates to a novel class of compounds, represented by the formula (I) below, wherein the meanings of R1, R2, R3, R4, R5, R6, R7, X and Y are indicated therein, which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsms K L, S and B These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis, osteoarthritis and rheumatoid arthritis | 10-08-2009 |
| 20090253675 | PHARMACEUTICAL FORMULATION - The instant invention provides a pharmaceutical composition comprised of a cholesterol absorption inhibitor and an HMG-CoA reductase inhibitor, one or more anti-oxidants, microcrystalline cellulose, hydroxypropyl methylcellulose, magnesium stearate and lactose. The composition need not contain ascorbic acid in order to obtain desirable stability. | 10-08-2009 |
| 20090264399 | HETEROCYCLIC JANUS KINASE 3 INHIBITORS - The invention relates to compound of the formula (I) or its salt, wherein —R | 10-22-2009 |
| 20090264402 | NOVEL DIPHENYLAZETIDINONE SUBSTITUTED BY PIPERAZINE-1-SULFONIC ACID AND HAVING IMPROVED PHARMACOLOGICAL PROPERTIES - The invention therefore relates to the compound of the formula I | 10-22-2009 |
| 20090275551 | Fluvastatin for the treatment of patients with a history of muscle related side effects with other statins - The present disclosure relates to method of using fluvastatin, alone or in combination with ezetimibe, be used to (1) lower cholesterol level, (2) treat hypercholesterolemia, (3) treat mixed dyslipidemia and/or (4) inhibit cholesterol biosynthesis in patients who experienced muscle-related side effects (MRSE). The present disclosure also relates to a pharmaceutical composition comprising ezetimibe and fluvastatin. | 11-05-2009 |
| 20090312302 | Compositions and methods for treating nonalcoholic fatty liver disease-associated disorders - The invention relates to compositions containing cholesterol absorption inhibitors alone or in combination with other therapeutic agents for treating non-alcoholic fatty liver disease-associated disorders by administering a therapeutically effective amount of the compositions to a subject in need thereof. | 12-17-2009 |
| 20090318404 | SUBSTITUTED BETA-LACTAMS - Disclosed herein is a compound comprising | 12-24-2009 |
| 20100016273 | Use of Ezetimibe in the Prevention and Treatment of Cholesterol Gallstones - This invention discloses the use of compounds of the azetidinone family in the prevention or treatment of cholesterol gallstone disease of the biliary tree in mammals. This invention is in the general area of cholesterol stones disease in the biliary tree and gallbladder. In particular, the invention evidences that the use of drugs that specifically block cholesterol intestinal absorption inhibit the onset of cholesterol stone disease in the biliary tree. These drugs act by decreasing biliary cholesterol secretion, and at the same time increasing the biliary flow and the hepatic secretion of endogenous compounds (e.g. bile salts, phospholipids) into the bile, hi turn, these endogenous compounds contribute to inhibiting cholesterol precipitation and the formation of gallstones in the biliary tree. | 01-21-2010 |
| 20100016274 | BETA-LACTAM CANNABINOID RECEPTOR MODULATORS - Described herein are substituted 2-(azetidin-2-on-1-yl)alkanoic acids, alkanedioic acids and 2-hydroxyalkyl alkanoic acids, and 2-acyl alkanoic acids, and derivatives thereof, that are capable of modulating activity at the cannabinoid-1 (CB1) and/or cannabinoid-2 (CB2) receptor. Also described herein are methods for treating mammals in need of relief from disease states associated with and responsive to modulation of the CB1 and/or CB2 receptor activity. | 01-21-2010 |
| 20100029607 | Substituted Piperazines as CB1 Antagonists - Compounds of Formula (I): | 02-04-2010 |
| 20100035857 | ANTI-HYPERCHOLESTEROLEMIC COMPOUNDS - This invention provides cholesterol absorption inhibitors of Formula I:I and the pharmaceutically acceptable salts thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events. | 02-11-2010 |
| 20100048529 | New 2-Azetidinone Derivatives Useful In The Treatment Of Hyperlipidaemic Conditions - The invention relates to compounds of formula (I) and pharmaceutically acceptable salts, solvates, and prodrugs thereof, and to their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia. The invention also relates to processes for their manufacture and pharmaceutical compositions containing them. | 02-25-2010 |
| 20100069347 | HETEROCYCLYL-SUBSTITUTED ANTI-HYPERCHOLESTEROLEMIC COMPOUNDS - This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts thereof, wherein R | 03-18-2010 |
| 20100075943 | 1-ADAMANTYLAZETIDIN-2-ONE DERIVATIVES AND DRUGS CONTAINING SAME - It is to provide a novel compound useful for preventing and/or treating diseases that involves 11β-hydroxysteroid dehydrogenase 1, particularly diabetes, insulin resistance, diabetes complication, obesity, dyslipidemia, hypertension, fatty liver, or metabolic syndrome. It is an 1-adamantyl azetidin-2-one derivative represented by the following general formula (1) or salt thereof, or their solvate. | 03-25-2010 |
| 20100081643 | NOVEL CYCLIC BENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS - Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. | 04-01-2010 |
| 20100087415 | INHIBITORS OF STORE OPERATED CALCIUM RELEASE - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity. | 04-08-2010 |
| 20100099657 | Diphenylazetidinone Derivatives Possessing Cholesterol Absorption Inhibitory Activity - Compounds of formula (I) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described. | 04-22-2010 |
| 20100125059 | 1-BIARYLAZETIDINONE DERIVATIVE - The object of the present invention is to provide a compound having an excellent cholesterol-lowering effect and to provide a drug for the treatment, prevention of onset, or prevention of progress of lipid metabolism disorder, hyperlipidemia, or atherosclerosis. | 05-20-2010 |
| 20100137273 | Novel 2-Azetidinone Derivatives As Cholesterol Absorption Inhibitors For The Treatment Of Hyperlipidaemic Conditions - Compounds of formula (I): (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described. | 06-03-2010 |
| 20100144694 | 1,2-DIAZETIDIN-3-ONE DERIVATIVES AND DRUGS CONTAINING SAME | 06-10-2010 |
| 20100144696 | Stabilized pharmaceutical compositions containing a calcium channel blocker - The present invention provides a pharmaceutical composition containing a calcium channel blocker of the following formula or a pharmacologically acceptable salt thereof and a pharmacologically acceptable alkaline material which is added to an extent such that an aqueous solution or dispersion solution of said pharmaceutical composition containing a calcium channel blocker has a pH of at least 8: | 06-10-2010 |
| 20100144698 | SUBSTITUTED AZETIDINONES - Compounds are provided which have the structure | 06-10-2010 |
| 20100152156 | 2-Azetidinone Derivatives For The Treatment Of Hyperlipidaemic Diseases - The invention relates to novel 2-azetidinone derivatives of formula (I) and to pharmaceutically acceptable salts, solvates and prodrugs thereof. The compounds are cholesterol absorption inhibitors, useful in the treatment of hyperlipidaemic conditions. The invention also relates to processes for their manufacture and to pharmaceutical compositions containing them. | 06-17-2010 |
| 20100160281 | MONOCARBAMS - The invention relates to compounds of formula (I): | 06-24-2010 |
| 20100160282 | NOVEL DIPHENYLAZETIDINONES, PROCESS FOR THEIR PREPARATION, MEDICAMENTS COMPRISING THESE COMPOUNDS AND THEIR USE - Compounds of the formula I, | 06-24-2010 |
| 20100160283 | HETEROARYL-SUBSTITUTED ALKYNE COMPOUNDS AND METHOD OF USE - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I | 06-24-2010 |
| 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. | 07-01-2010 |
| 20100197651 | Pyridazinone compounds - The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. | 08-05-2010 |
| 20100204195 | Pharmaceutical Compositions and Process for Making Them - Amorphous HMG CoA reductase inhibitors, especially amorphous atorvastatin, are described. Also described are pharmaceutical combinations comprising amorphous HMG CoA reductase inhibitors in combination with cholesterol absorption inhibitors or fibrates. A method of manufacturing the compositions using a hot melt extrusion process are also described. | 08-12-2010 |
| 20100216759 | Novel 2-Azetidinone Derivatives And Their Use As Cholesterol Absorption Inhibitors For The Treatment Of Hyperlipidaemia - Compounds of formula (I) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described. | 08-26-2010 |
| 20100216761 | NOVEL AZETIDINONES USEFUL AS INHIBITORS OF ELASTASE - The invention is directed to novel azetidinones selected from 2-(S)-[4-(((2-(Dimethylamino)ethyl)ethylamino)carbonyl)phenoxy]-3,3-diethyl-N-[1-(R)-(4-(trifluoromethoxy)phenyl)butyl]-4-oxo-1-azetidin ecarboxamide, 2-(S)-[4-(((2-(Dimethylamino)ethyl)ethylamino)carbonyl)phenoxy]-3,3-diethyl-N-[1-(R)-(4-(trifluoromethyl)phenyl)butyl]-4-oxo-1-azetidinecarboxamide, and analogs thereof, and pharmaceutically acceptable salts thereof, and their use in the treatment of diseases associated with an excess of elastase, including emphysema, bronchial inflammation, chronic bronchitis, cystic fibrosis, acute respiratory distress syndrome, rheumatoid arthritis, osteoarthritis; glomerulonephritis, spondylitis, lupus, psoriasis, atherosclerosis, sepsis, septicemia, shock, myocardial infarction, reperfusion injury, and periodontitis. | 08-26-2010 |
| 20100234342 | EZETIMIBE COMPOSITIONS - This invention is a novel pharmaceutical composition of ezetimibe or a pharmaceutically acceptable salt thereof comprising one or more pharmaceutically acceptable excipients having high bioavailability with improved solubility and dissolution rate which is stable throughout the shelflife, methods for their preparation, and methods for treatment using the same. | 09-16-2010 |
| 20100261698 | ORGANIC COMPOUNDS - The present invention provides novel organic compounds of Formula I: | 10-14-2010 |
| 20100267685 | Methods For The Prophylaxis And/or Treatment Of Thromboembolic Disorders By Combination Therapy With Substituted Oxazolidinones - The invention relates to combinations of A) oxazolidinones of formula (I) and B) other active ingredients, to a method for producing said combinations and to the use thereof as medicaments, in particular for the treatment and/or prophylaxis of thrombo-embolic diseases. | 10-21-2010 |
| 20100292203 | HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS - Disclosed are compounds of the formula I | 11-18-2010 |
| 20100292204 | SULPHUR CONTAINING PYRAZOLE DERIVATIVES AS SELECTIVE CANNABINOID CB1 RECEPTOR ANTAGONISTS - The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB | 11-18-2010 |
| 20100305087 | ACTIVE PHARMACEUTICAL INGREDIENT ON A SOLID SUPPORT, AMORPHOUS AND WITH AN IMPROVED SOLUBILITY - A combination preparation comprising an active pharmaceutical ingredient (API) and a pharmaceutically acceptable solid support, wherein said solid support is in a water-insoluble particulate form and comprises a material selected from silicic acid, aluminum hydroxide and titanium hydroxide is disclosed. The API is a compound having both, at least one hydrophobic structural moiety causing the API to have a low solubility in water or in an aqueous solution, and multiple hydrophilic groups arranged to form multiple intermolecular interactions to the solid support involving polar or ionic or hydrogen bonding. The hydrophilic groups of the API are independently equal or different and comprise at least one of the groups consisting of OH- and halogen-groups. The API is bound to the solid support by adsorption, and a major proportion of said API is in an amorphous state. Related pharmaceuticals and methods of preparation also are disclosed. | 12-02-2010 |
| 20100317642 | PHARMACEUTICAL COMPOSITION OF ORLISTAT - A stable pharmaceutical composition comprising dispersion blend comprising 20 to 60% by weight of orlistat and 40% to 80% by weight of water soluble polymer carrier selected from hydroxypropyl methyl cellulose, methylcellulose, hydroxyethyl cellulose, hydroxypropyl cellulose or hydroxypropyl methylcellulose and the like. | 12-16-2010 |
| 20100317643 | JANUS KINASE INHIBITOR COMPOUNDS AND METHODS - The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, B, D, R | 12-16-2010 |
| 20100331293 | HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjogren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 12-30-2010 |
| 20110046105 | Heterocycle-substituted imidazolidine-2,4-diones, process for preparation thereof, medicaments comprising them and use thereof - The invention relates to compounds of formula (I) wherein the groups R and R′, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs. | 02-24-2011 |
| 20110059934 | COMPOUNDS AND COMPOSITIONS USEFUL FOR THE TREATMENT OF PARASITIC DISEASES - The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria. | 03-10-2011 |
| 20110059935 | Beta-LACTAMYL VASOPRESSIN V1a ANTAGONISTS - Novel 2-(azetidin-2-on-1-yl)alkanedioic acid derivatives and 2-(azetidin-2-on-1-yl)alkoxyalkanoic acid derivatives are described for use in the treatment of disease states responsive to antagonism of the vasopressin V | 03-10-2011 |
| 20110059936 | C-MET PROTEIN KINASE INHIBITORS - The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides processes for preparing the compounds of this invention, pharmaceutically acceptable compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of various disorders. | 03-10-2011 |
| 20110059939 | THERAPEUTIC COMPOUNDS - Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, a dashed line represent the presence or absence of a double bond, are disclosed, wherein J | 03-10-2011 |
| 20110077232 | COMPOSITIONS COMPRISING ATORVASTATIN 4-(NITROOXY) BUTYL ESTER AND A HYPOLIPIDEMIC DRUG - The present invention relates to compositions comprising atorvastatin 4-(nitrooxy) butyl ester and a hypolipidemic, in particular ezetimibe and fenofibrate. The invention discloses also their use as cholesterol-reducing drugs, as drugs having immunosuppressive properties, antioxidant, antithrombotic and anti-inflammatory activity, effects on endothelial function, and for treating and/or preventing acute coronary syndromes, stroke, atherosclerosis, neurodegenerative disorders, such as Alzheimer's and Parkinson's disease as well as autoimmune diseases, such as multiple sclerosis. | 03-31-2011 |
| 20110086833 | METHODS FOR TREATING SPINAL MUSCULAR ATROPHY - The present invention provides nucleic acid constructs, methods for identifying and validating compounds that increase the inclusion of exon 7 of SMN2 into mRNA transcribed from the SMN2 gene, compounds and pharmaceutical compositions that increase levels of SMN protein produced from the SMN2 gene, and methods for use thereof in treating of SMA. | 04-14-2011 |
| 20110105457 | HETEROCYCLIC COMPOUND HAVING INHIBITORY ACTIVITY ON PI3K - The purpose of the present invention is to provide a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prevention/treatment of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. This was achieved by providing a substituted 2-amino-5,6-nitrogenated fused ring compound shown in the present specification, or a pharmaceutically acceptable salt thereof. | 05-05-2011 |
| 20110112063 | PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS - The invention provides novel pyrimidine derivatives of formula I and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-IR) or analplastic lymphoma kinase (ALK). | 05-12-2011 |
| 20110130378 | EZETIMIBE PROCESS AND COMPOSITION - The present invention describes a process for producing ezetimibe (EZT) from a protected compound, including a step of deprotecting the 4-(p-hydroxyphenyl) protection group by catalytic hydrogenation, wherein the catalyst is used in an amount of 0.7 wt.-% or lower, relative to the weight of the compound used for the deprotection reaction. After carrying out a step of deprotection reaction, the process preferably comprises: (a) the reaction product is dissolved or extracted in ethyl acetate, and (b) the ethyl acetate solution is washed with an aqueous salt solution. The invention further describes a process for obtaining pure EZT, wherein raw EZT is dissolved in a solvent at a concentration of lower than 0.1 g/ml, and a crystallization step is carried out from this solution. These measures, respectively alone and particularly in combination contribute to attain ezetimibe (EZT) free of critical impurities described herein, and thus to use exceptionally pure ezetimibe (EZT) to be formulated into a pharmaceutical composition together with a pharmaceutically acceptable carrier or excipient. | 06-02-2011 |
| 20110144081 | PYRROLIDINE DERIVATIVES - The present invention relates to compounds of formula | 06-16-2011 |
| 20110152233 | PYRROLIDINE COMPOUNDS - The present application relates to compounds of formula | 06-23-2011 |
| 20110183956 | PROCESS FOR THE SYNTHESIS OF EZETIMIBE AND INTERMEDIATES USEFUL THEREFOR - The present invention discloses novel and useful intermediates for the synthesis of ezetimibe (EZT), which intermediates share a characteristic Z-isomeric structure. Based on Z-5-(4-fluorophenyl)-pent-4-enoic acid, and proceeding the synthesis through further Z-intermediates, a total synthesis is presented to obtained final ezetimibe in high yields. | 07-28-2011 |
| 20110207710 | TREATMENT OF CARDIOVASCULAR DISEASE AND DYSLIPIDEMIA USING SECRETORY PHOSPHOLIPASE A2 (SPLA2) INHIBITORS AND SPLA2 INHIBITOR COMBINATION THERAPIES - Administration of sPLA | 08-25-2011 |
| 20110230457 | Substituted Isoquinolinones and Quinazolinones - The invention relates to substituted nitrogen containing bicyclic heterocycles of the formula (I) | 09-22-2011 |
| 20110230460 | THIENOTRIAZOLODIAZEPINE DERIVATIVES ACTIVE ON APO A - The invention relates to new thienotriazolodiazepine derivatives of the formula (1) wherein R | 09-22-2011 |
| 20110257149 | FORMULATION FOR ORAL TRANSMUCOSAL ADMINISTRATION OF LIPID-LOWERING DRUGS - The invention relates to a formulation for delivering by oral transmucosal administration at least one lipid-lowering active principle, preferably from the statin family, said formulation including said active principle in the base or salt form, an aqueous alcohol solution titrating at least 30° alcohol, and optionally a pH correcting agent and/or an antioxidant, said active principle being in a stable and completely dissolved state in the aqueous alcohol solution. The invention also relates to a method of preparing said formulation and to the use thereof, preferably in single-dose packaging, for treating and preventing hyperlipemia and/or cardiovascular conditions. | 10-20-2011 |
| 20110263558 | Azetidines as MEK Inhibitors for the Treatment of Proliferative Diseases - Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer. | 10-27-2011 |
| 20110269735 | GENETIC POLYMORPHISMS ASSOCIATED WITH STATIN RESPONSE AND CARDIOVASCULAR DISEASES, METHODS OF DETECTION AND USES THEREOF - The present invention provides compositions and methods based on genetic polymorphisms that are associated with response to statin treatment, particularly for reducing the risk of cardiovascular disease, especially coronary heart disease (such as myocardial infarction) and stroke. For example, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by these nucleic acid molecules, reagents and kits for detecting the polymorphic nucleic acid molecules and variant proteins, and methods of using the nucleic acid molecules and proteins as well as methods of using reagents and kits for their detection. | 11-03-2011 |
| 20110288064 | METHODS FOR TREATING DISORDERS ASSOCIATED WITH HYPERLIPIDEMIA IN A MAMMAL - The invention is directed to methods for treating hyperlipidemia in a mammal. The methods involve combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, BMS-201038 and implitade) and a cholesterol absorption inhibitor (CAI) (for example, ezetimibe). Co-administration of the MTP inhibitor with the CAI produces a therapeutic benefit, for example, a reduction in the concentration of cholesterol and/or triglycerides in the blood stream, but with fewer or reduced side effects than when higher dosages of the MTP inhibitor are used during monotherapy to provide the same or similar therapeutic benefit. | 11-24-2011 |
| 20110288065 | AMINOPYRAZINE DERIVATIVE AND MEDICINE - The present invention relates to a compound represented by general formula [1] satisfying the following (I) or (II), or a pharmaceutical acceptable salt of the compound. | 11-24-2011 |
| 20110306586 | NMDA Receptor Modulators and Uses Thereof - Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorder such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed. | 12-15-2011 |
| 20120004208 | BENZOYL-PIPERIDINE DERIVATIVES AS DUAL MODULATORS OF THE 5-HT2A AND D3 RECEPTORS - The present invention relates to compounds of the general formula | 01-05-2012 |
| 20120010181 | COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF—or combinations thereof. | 01-12-2012 |
| 20120015925 | NOVEL BENZOTHIAZEPINE AND BENZOTHIEPINE COMPOUNDS - A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided. A benzothiazepine or benzothiepine compound represented by the following formula (1A) having a thioamide bond and a quaternary ammonium substituent: | 01-19-2012 |
| 20120015926 | COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof. | 01-19-2012 |
| 20120015928 | Amido Compounds And Their Use As Pharmaceuticals - The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess. | 01-19-2012 |
| 20120028951 | PYRIDAZINONE COMPOUNDS - The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I | 02-02-2012 |
| 20120058984 | PYRIMIDINE DERIVATIVES USED AS ITK INHIBITORS - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): | 03-08-2012 |
| 20120071458 | METHODS FOR TREATING OBESITY - The invention is directed to methods for treating and/or controlling obesity in a patient. The methods involve combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, AEGR-733 and implitapide) and a cholesterol absorption inhibitor (CAI) (for example, ezetimibe). | 03-22-2012 |
| 20120071459 | BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS - The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes. | 03-22-2012 |
| 20120094972 | HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 04-19-2012 |
| 20120101078 | AMIDE DERIVATIVES AS NEUROPEPTIDE Y5 RECEPTOR LIGANDS - Disclosed are a series of neuropeptide Y Y5 receptor ligands, and as such are useful to treat disorders related to mood, stress, ADHD, cognition, stress and dementia. | 04-26-2012 |
| 20120135975 | Substituted Esters as Cannabinoid-1 Receptor Modulators - Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness. | 05-31-2012 |
| 20120135976 | PROCESS FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION COMPRISING EZETIMIBE - The present invention belongs to the field of pharmaceutical industry and relates to a process for preparing dosage forms containing ezetimibe, comprising the steps of:
| 05-31-2012 |
| 20120149673 | INHIBITORS OF STORE OPERATED CALCIUM RELEASE - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity. | 06-14-2012 |
| 20120277204 | PYRIDAZINONE COMPOUNDS - The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I | 11-01-2012 |
| 20120302540 | 3-SPIROCYCLIC PIPERIDINE DERIVATIVES AS GHRELIN RECEPTOR AGONISTS - The invention relates to derivatives of formula (I), | 11-29-2012 |
| 20120309734 | COMBRETASTATIN DERIVATIVES AND USES THEREFOR - Cancer is one of the major causes of death worldwide. Although many advances have been made in the treatment and management of the disease, the existence of chemotherapy-resistance means there is still a great need to develop new strategies and drugs for its treatment. Provided herein are synthetic derivatives of combretastatin A-4, in particular those in which the aromatic rings are locked into a non-isomerisable active conformation, thus resulting in improved, stable compounds. The novel compounds are structurally related to combretastatin A-4 (CA-4) and lock the rings into the known active conformation by means of a four membered nitrogen containing heterocyclic ring, such as a beta-lactam ring, incorporated into the standard CA-4 structure. The compounds exhibit potent anti-cancer activity. | 12-06-2012 |
| 20120309736 | NOVEL CYCLIC BENZIMIDAZOLE DERIVATIVES USEFUL ANTI-DIABETIC AGENTS - Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. | 12-06-2012 |
| 20120316147 | NOVEL PYRIDINE DERIVATIVES - The invention relates to a compound of formula (I) | 12-13-2012 |
| 20130005701 | SUBSTITUTED OXAZOLIDINONES AND THEIR USE IN THE FIELD OF BLOOD COAGULATION - The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) | 01-03-2013 |
| 20130023513 | Methods and Compositions for Treating Cardiovascular Disorders - The invention generally relates to methods of treating a patient having, and/or at risk of, cardiovascular or cerebrovascular disorders. Such methods may include administering a MetAP2 inhibitor at a dose that does not substantially modulate angiogenesis. | 01-24-2013 |
| 20130023514 | SUBSTITUTED PYRROLOTRIAZINES AS PROTEIN KINASE INHIBITORS - The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) pyrrolotriazines inhibit protein kinase activity thereby making them useful as anticancer agents. | 01-24-2013 |
| 20130023515 | NOVEL SPIROPIPERIDINE PROLYLCARBOXYPEPTIDASE INHIBITORS - Compounds of structural formula (I) are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders. | 01-24-2013 |
| 20130040927 | CHOLESTEROL ABSORPTION INHIBITOR AND OMEGA 3 FATTY ACIDS FOR THE REDUCTION OF CHOLESTEROL AND FOR THE PREVENTION OR REDUCTION OF CARDIOVASCULAR, CARDIAC AND VASCULAR EVENTS - A composition and a method of treatment for the reduction of risk factors for cardiovascular disease utilizing a combination of lipid lowering cholesterol absorption inhibitors, e.g. azetidinones, with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight including a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA represent about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught. | 02-14-2013 |
| 20130040929 | NOVEL PROLYLCARBOXYPEPTIDASE INHIBITORS - Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders. | 02-14-2013 |
| 20130040930 | NOVEL AMIDE DERIVATIVE AND USE THEREOF AS MEDICINE - Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) | 02-14-2013 |
| 20130059830 | NOVEL PROLYLCARBOXYPEPTIDASE INHIBITORS - Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders. | 03-07-2013 |
| 20130065875 | SMALL MOLECULE INHIBITORS OF HEPATITIS C VIRUS - The invention provides derivatives and analogues of triazatetracyclo[7.7.0.0 | 03-14-2013 |
| 20130072468 | SUBSTITUTED PIPERAZINES AS CB1 ANTAGONISTS - Compounds of Formula (I): | 03-21-2013 |
| 20130090323 | HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 04-11-2013 |
| 20130090324 | NOVEL PROLYLCARBOXYPEPTIDASE INHIBITORS - Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders. | 04-11-2013 |
| 20130102582 | COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING CORONARY HEART DISEASE - The invention pertains to a method of determining a statin dosage for an individual in need of treatment with a statin, comprising determining a SLCO1B1 genotype from a nucleic acid sample of the individual, said genotype comprising the presence or absence of the SLCO1B1-056 polymorphism, and determining an ApoE genotype or phenotype identifying an ApoE polymorphism selected from the group consisting of ApoE2, ApoE3, ApoE4, and any combination thereof, wherein the combination of a SLCO1B1 genotype identifying the presence of the SLCO1B1-056 C polymorphism and the ApoE genotype or phenotype identifying one of the ApoE3/4 or ApoE4/4 genotypes indicates the statin dosage. | 04-25-2013 |
| 20130109666 | METHODS FOR TREATING POST TRAUMATIC STRESS DISORDER | 05-02-2013 |
| 20130143859 | NOVEL PROLYLCARBOXYPEPTIDASE INHIBITORS - Compounds of structural formulas I-1 and I-2 are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders. | 06-06-2013 |
| 20130184249 | PYRROLIDINE DERIVATIVES - The present invention relates to compounds of formula | 07-18-2013 |
| 20130203728 | PYRROLIDINE COMPOUNDS - The present application relates to compounds of formula | 08-08-2013 |
| 20130210794 | NANOSTRUCTURED EZETIMIBE COMPOSITIONS, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - The present invention is directed to nanostructured Ezetimibe compositions, process for the preparation thereof and pharmaceutical compositions containing them. The nanoparticles of Ezetimibe according to the invention have an average particle size of less than about 400 nm. The stable nanostructured particles of the invention are presented by increased solubility, dissolution rate, permeability and bioequivalent or enhanced biological performance compared to the marketed drug. Ezetimibe is an anti-hyperlipidemic medication that is used to lower cholesterol levels. It acts by decreasing cholesterol absorption in the intestine. | 08-15-2013 |
| 20130217660 | NOVEL PROLYLCARBOXYPEPTIDASE INHIBITORS - Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders. | 08-22-2013 |
| 20130231322 | THERAPEUTIC SUBSTITUTED BETA-LACTAMS - A compound having a structure | 09-05-2013 |
| 20130289013 | IMIDAZO[1,2-a]PYRIDINE COMPOUNDS - Imidazo[1,2-a]pyridines are disclosed. Compounds of the invention are useful therapeutic agents and their inclusion in pharmaceutical formulations and use in methods of treatment are disclosed. | 10-31-2013 |
| 20130316999 | SUBSTITUTED OXAZOLIDINONES AND THEIR USE IN THE FIELD OF BLOOD COAGULATION - The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) | 11-28-2013 |
| 20130331369 | 3-Spirocyclic Piperidine Derivatives as Ghrelin Receptor Agonists - The invention relates to derivatives of formula (I), | 12-12-2013 |
| 20130338131 | PROCESS FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION COMPRISING A LOW SOLUBLE PHARMACEUTICALLY ACTIVE INGREDIENT - The present invention belongs to the field of pharmaceutical industry and relates to a process for preparing a pharmaceutical composition comprising a pharmaceutically active ingredient (API) that is poorly soluble in water, a pharmaceutical composition obtained according to said process, to a dosage form comprising said pharmaceutical composition and to the use of said dosage forms for the treatment of hypercholesterolemia. | 12-19-2013 |
| 20140018342 | GAMMA SECRETASE INHIBITORS - Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease. | 01-16-2014 |
| 20140031332 | Biomarkers for Sensitive Detection of Statin-Induced Muscle Toxicity - The present invention inter alia provides a method, and uses thereof, of predicting statin-induced muscle toxicity or its complications, such as myalgia, myopathy and rhabdomyolysis, by detecting the lipid concentrations or lipid ratios of a biological sample and comparing it to a control. This method has identified lipid markers that are more specific and sensitive in detecting these statin-induced muscle toxicity than the currently utilized clinical markers. Also provided is an antibody towards said lipids, and the use thereof for predicting, diagnosing, statin-induced muscle toxicity. The invention additionally relates to kits comprising lipids and/or an antibody thereto, for use in the prediction and/or diagnosis of statin-induced muscle toxicity. | 01-30-2014 |
| 20140051674 | NEW COMPOUNDS - The present invention encompasses compounds of general formula (1) | 02-20-2014 |
| 20140066423 | POLYCYCLIC BETA LACTAM DERIVATIVES FOR THE TREATMENT OF CANCER - Provided herein are polycyclic β-lactam compounds, compositions thereof and methods for the treatment and prevention of diseases such as cancer, including pancreatic cancer and pancreatic cancers resistant to mainline chemotherapeutic agents. | 03-06-2014 |
| 20140080800 | Inhibitors of Histone Deacetylase - The present invention relates to compounds of formula (I): | 03-20-2014 |
| 20140088072 | EXTENDED RISK ASSESSMENT PANEL FOR INDIVIDUALIZED TREATMENT OF CARDIOVASCULAR DISEASE, AND METHODS RELATED THERETO - Disclosed is a personalized diagnostic and treatment solution for cardiovascular disease. The invention comprises an extended CVD risk assessment panel, combining tests for traditional and new important risk markers, and methods for devising a personalized treatment plan for a patient via the use of a CVD diagnosis and treatment protocol algorithm. The new important risk markers include HDL subpopulation profile by two-dimensional gel-electrophoresis, plasma sterols, direct measurement of sdLDL-C, determination of CRP molecular forms, glycated albumin as a percentile of total albumin, and other specialized testing pertaining to apolipoprotein E and Factor V Leiden genotyping, NT-proBNP and adiponectin. This solution provides a more complete risk assessment of an individual than merely measuring traditional CVD risk markers, and enables the healthcare practitioner to optimize therapy for patients with or without established CVD. This solution presents the advantages of greater accuracy, savings in time and cost over existing testing and treatment methods. | 03-27-2014 |
| 20140088073 | METHODS FOR DETERMINING WHETHER A PATIENT SHOULD BE ADMINISTERED A DRUG THAT INHIBITS CHOLESTEROL ABSORPTION - The invention generally relates to methods for determining whether a patient should be administered a drug that inhibits cholesterol absorption. In certain aspects, methods of the invention involve obtaining a sample from a patient, conducting an assay on the sample to obtain a level of a cholesterol absorption marker, and comparing the level to a reference level, in which a level above the reference level indicates that the patient should be administered a drug that inhibits cholesterol absorption. | 03-27-2014 |
| 20140128362 | GENETIC POLYMORPHISMS ASSOCIATED WITH VENOUS THROMBOSIS AND STATIN RESPONSE, METHODS OF DETECTION AND USES THEREOF - The present invention provides compositions and methods based on genetic polymorphisms that are associated with response to statin treatment (particularly for reducing the risk of venous thrombosis). For example, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by these nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and variant proteins, and methods of using the nucleic acid molecules and proteins as well as methods of using reagents for their detection. | 05-08-2014 |
| 20140135305 | METHODS FOR TREATING SPINAL MUSCULAR ATROPHY - The present invention provides nucleic acid constructs, methods for identifying and validating compounds that increase the inclusion of exon 7 of SMN2 into mRNA transcribed from the SMN2 gene, compounds and pharmaceutical compositions that increase levels of SMN protein produced from the SMN2 gene, and methods for use thereof in treating of SMA. | 05-15-2014 |
| 20140155371 | MULTICOMPONENT CRYSTALLINE SYSTEM OF EZETIMIBE AND PROLINE - Provided is a crystalline composition comprising a mixture of a compound of formula 1 (Ezetimibe) and proline or proline derivatives, or a hydrate/solvate thereof, as well as a process for obtaining the same. And a process for the purification of Ezetimibe is also disclosed. | 06-05-2014 |
| 20140162996 | NOVEL MODULATORS OF DEVELOPMENT OF ADIPOCYTE AND CANCER CELLS - One aspect of the disclosure relates to derivatives of aryl and heterocyclic ureido aryl and heterocyclic carboxamido isobutyric acids, dichlorophenyl urea, curcumin, and 1,3-diazetidine-2,4-dione, and pharmaceutical compositions thereof. The derivatives disclosed herein can modulate development of adipocytes and various cancer cells, including resistant cancer cells and cancer stem cells. Another aspect of the disclosure relates to the use of the derivatives and pharmaceutical compositions disclosed herein in treatment of obesity and various cancers. | 06-12-2014 |
| 20140200205 | NEW THIO DERIVATIVES BEARING LACTAMS AS POTENT HDAC INHIBITORS AND THEIR USES AS MEDICAMENTS - The present invention relates to novel amide compounds of Formula (I), and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC is responsive, and the pharmaceutical composition containing such compounds. | 07-17-2014 |
| 20140213571 | TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES - The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. | 07-31-2014 |
| 20140221333 | BTK INHIBITORS - Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders. | 08-07-2014 |
| 20140235605 | GENETIC POLYMORPHISMS ASSOCIATED WITH STATIN RESPONSE AND CARDIOVASCULAR DISEASES, METHODS OF DETECTION AND USES THEREOF - The present invention provides compositions and methods based on genetic polymorphisms that are associated with response to statin treatment, particularly for reducing the risk of cardiovascular disease, especially coronary heart disease (such as myocardial infarction) and stroke. For example, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by these nucleic acid molecules, reagents and kits for detecting the polymorphic nucleic acid molecules and variant proteins, and methods of using the nucleic acid molecules and proteins as well as methods of using reagents and kits for their detection. | 08-21-2014 |
| 20140235607 | COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING CORONARY HEART DISEASE - The invention pertains to a method of determining a statin dosage for an individual in need of treatment with a statin, comprising determining a SLCO1B1 genotype from a nucleic acid sample of the individual, said genotype comprising the presence or absence of the SLCO1B1-056 polymorphism, and determining an ApoE genotype or phenotype identifying an ApoE polymorphism selected from the group consisting of ApoE2, ApoE3, ApoE4, and any combination thereof, wherein the combination of a SLCO1B1 genotype identifying the presence of the SLCO1B1-056 C polymorphism and the ApoE genotype or phenotype identifying one of the ApoE3/4 or ApoE4/4 genotypes indicates the statin dosage. | 08-21-2014 |
| 20140275004 | PYRROLOPYRIMINDINE CDK9 KINASE INHIBITORS - Disclosed are compound of Formula (Ia), | 09-18-2014 |
| 20150011525 | SOLID DISPERSION OF POORLY SOLUBLE COMPOUNDS COMPRISING CROSPOVIDONE AND AT LEAST ONE WATER-SOLUBLE POLYMER - A stable ternary solid dispersion composition with enhanced physical stability and/or bioavailability comprising: (a) about 1% wt. to about 50% wt. of one or more poorly soluble active pharmaceutical ingredient (API) which belongs to Biopharmaceutics Classification System (BCS) class II and/or IV; (b) about 11% wt. to about 50% wt. of at least one water-soluble polymer; and (c) about 20% wt. to about 99% wt. of crosslinked polyvinylpyrrolidone (crospovidone, a water-insoluble polymer). The solid dispersion is capable of inhibiting crystallization of API in solid state and/or aqueous gastrointestinal tract (GIT) medium. Also disclosed is a method of preparation of such solid dispersion composition by fusion or solvent or fusion-solvent method. | 01-08-2015 |
| 20150018329 | PHARMACEUTICALLY ACTIVE PYRAZOLO-TRIAZINE DERIVATIVES - The present invention relates to pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase. | 01-15-2015 |
| 20150105364 | NMDA Receptor Modulators and Uses Thereof - Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorder such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed. | 04-16-2015 |
| 20150105365 | HETEROARYL LINKED QUINOLINYL MODULATORS OF RORgammat - The present invention comprises compounds of Formula I. | 04-16-2015 |
| 20150111865 | Trk-INHIBITING COMPOUND - An object of the present invention is to provide a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I): | 04-23-2015 |
| 20150133422 | NOVEL 4-(INDOL-3-YL)-PYRAZOLE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE - The present invention embodiments relate to compound of Formula I | 05-14-2015 |
| 20150328228 | NOVEL 4-(INDOL-3-YL)-PYRAZOLE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE - The present invention relates to compound of Formula I | 11-19-2015 |
| 20150329561 | Amido Compounds And Their Use As Pharmaceuticals - The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess. | 11-19-2015 |
| 20150336969 | NMDA Receptor Modulators and Uses Thereof - Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorder such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed. | 11-26-2015 |
| 20150368252 | SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF - Disclosed are compounds having enhanced potency in the modulation of NMD A receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed. | 12-24-2015 |
| 20150368253 | SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF - Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed. | 12-24-2015 |
| 20150368254 | SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF - Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed. | 12-24-2015 |
| 20150376195 | SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF - Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed. | 12-31-2015 |
| 20160002224 | NOVEL INDOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS - Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. | 01-07-2016 |
| 20160068482 | CARBAMATE DERIVATIVES OF LACTAM BASED N-ACYLETHANOLAMINE ACID AMIDASE (NAAA) INHIBITORS - Described herein are compounds and pharmaceutical compositions which inhibit N-acylethanolamine acid amidase (NAAA). Described herein are methods for synthesizing the compounds set forth herein and methods for formulating these compounds as pharmaceutical compositions which include these compounds. Also described herein are methods of inhibiting NAAA in order to sustain the levels of palmitoylethanolamide (PEA) and other N-acylethanolamines (NAE) that are substrates for NAAA, in conditions characterized by reduced concentrations of NAE. Also, described here are methods of treating and ameliorating pain, inflammation, inflammatory diseases, and other disorders in which modulation of fatty acid ethanolamides is clinically or therapeutically relevant or in which decreased levels of NAE are associated with the disorder. | 03-10-2016 |
| 20160068483 | AMIDE DERIVATIVES OF LACTAM BASED N-ACYLETHANOLAMINE ACID AMIDASE (NAAA) INHIBITORS - Described herein are compounds and pharmaceutical compositions which inhibit N-acylethanolamine acid amidase (NAAA). Described herein are methods for synthesizing the compounds set forth herein and methods for formulating these compounds as pharmaceutical compositions which include these compounds. Also described herein are methods of inhibiting NAAA in order to sustain the levels of palmitoylethanolamide (PEA) and other N-acylethanolamines (NAE) that are substrates for NAAA, in conditions characterized by reduced concentrations of NAE. Also, described here are methods of treating and ameliorating pain, inflammation, inflammatory diseases, and other disorders in which modulation of fatty acid ethanolamides is clinically or therapeutically relevant or in which decreased levels of NAE are associated with the disorder. | 03-10-2016 |
| 20160122359 | SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF - Disclosed are compounds having enhanced potency in the modulation of NMD A receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed. | 05-05-2016 |
| 20160136149 | HETEROARYL LINKED QUINOLINYL MODULATORS OF RORyt - The present invention comprises compounds of Formula I. | 05-19-2016 |
| 20160137606 | NOVEL PYRIDINE DERIVATIVES - The invention relates to a compound of formula (I) | 05-19-2016 |
| 20160151382 | Cooperative Medication Combination Systems | 06-02-2016 |
| 20160185769 | Bromodomain Inhibitors - The present invention provides for compounds of formula (I). wherein R | 06-30-2016 |
| 20160194307 | COMPOUNDS USEFUL AS IMMUNOMODULATORS | 07-07-2016 |
| 20160250184 | GLUCAGON RECEPTOR ANTAGONIST COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE | 09-01-2016 |
| 20170231956 | SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF | 08-17-2017 |
| 20220133624 | METHOD FOR PRODUCING ORAL DISINTEGRATING FILM COMPRISING POORLY SOLUBLE DRUG - The present disclosure relates to a method for producing an oral disintegrating film by a 3D printing technology which utilizes a hot-melt pneumatic extrusion method, and when a mixture including a poorly soluble drug, a film-forming polymer, and a plasticizer confirmed in the present disclosure was produced as an oral disintegrating film using the production method of the present disclosure, it was confirmed that the production method was simplified because the production process became one process, the production costs were decreased, and a poorly soluble drug having a problem in that bioavailability deteriorated due to an existing low solubility could obtain excellent solubility. | 05-05-2022 |
