Entries |
Document | Title | Date |
20080249083 | NOVEL GENES RELATED TO GLUTAMINYL CYCLASE - Novel glutaminyl-peptide cyclotransferase-like proteins (QPCTLs), which are isoenzymes of glutaminyl cyclase (QC, EC 2.3.2.5), and to isolated nucleic acids coding for these isoenzymes, all of which are useful for the discovery of new therapeutic agents, for measuring cyclase activity, and for determining the inhibitory activity of compounds against these glutaminyl cyclase isoenzymes. | 10-09-2008 |
20080255102 | Phenylaminopropanol Derivatives and Methods of Their Use - The present invention is directed to phenylaminopropanol derivatives of formula I: | 10-16-2008 |
20080269204 | Compounds and Methods of Use Thereof - Benzolactam boronic acid compounds and pharmaceutical formulations are described along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) in a subject in need thereof. | 10-30-2008 |
20080280888 | Antibiotics Derivatives - The invention relates to antibiotic derivatives of formula I | 11-13-2008 |
20080300240 | PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS - Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. The compounds have the general structure: | 12-04-2008 |
20080306053 | MODULATION OF CHEMOSENSORY RECEPTORS AND LIGANDS ASSOCIATED THEREWITH - The present invention provides screening methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors as well as modifiers capable of modulating chemosensory receptors and their ligands. | 12-11-2008 |
20090005368 | Ethanol or 1,2-Ethanediol Cyclohexyl Antibiotic Derivatives - The invention relates to antibiotic ethanol or 1,2-ethanediol cyclohexyl derivatives of formula (I) wherein R1 represents (C | 01-01-2009 |
20090012068 | Condensed Imidazole Derivatives as Aldosterone Synthase Inhibitors - The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R | 01-08-2009 |
20090029975 | 1,3-BENZOTHIAZINONE DERIVATIVE AND USE THEREOF - A compound represented by the formula (I) or a salt thereof: (I) wherein R | 01-29-2009 |
20090036433 | Heterocyclic Compounds, their Preparation and their Use as Antibacterials - Tricyclic nitrogen containing compounds of formula (I) and their use as antibacterials. | 02-05-2009 |
20090042869 | SIGNAL-DEPENDENT SPLICING OF TISSUE FACTOR PRE-mRNA IN PLATELET CELLS - The invention relates to therapeutic target recognition, development, and validation of a compound capable of directly or indirectly modulating TF pre-mRNA splicing in a platelet cell and the use of a platelet TF pre-mRNA splicing modulator for the treatment of a subject suffering from, or thought to be suffering from, disordered coagulation. | 02-12-2009 |
20090054417 | COMPOUNDS AND COMPOSITIONS AS MODULATORS OF STEROID HORMONE NUCLEAR RECEPTORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activation of steroid hormone nuclear receptors. | 02-26-2009 |
20090054418 | Antibacterial Agents - 2H-chromen-2-one derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein. | 02-26-2009 |
20090062265 | Pyrrolo-Quinoxalinone Derivatives as Antibacterials - Tricyclic nitrogen containing compounds and their use as antibacterials. | 03-05-2009 |
20090069307 | Use of a pyridine compound for the preparation of a medicament for the treatment of skin lesions - The present invention relates to use of a pyridine compound of the following formula [I]: wherein R is a substituted pyridyl group having the following formula: R | 03-12-2009 |
20090082343 | 1,3-BENZOTHIAZINONE DERIVATIVES AND USE THEREOF - This invention provides a compound represented by the formula (I): | 03-26-2009 |
20090093468 | Peptide Deformylase Inhibitors - Benzothiazine compounds of the general formula (I) and pharmaceutically acceptable salts or esters thereof are peptide deformylase inhibitors useful in the treatment or prevention of infections and other diseases in which peptide deformylases are involved, especially in the treatment of bacterial and parasitic infections, for example infections fully or partly caused by microorganisms belonging to | 04-09-2009 |
20090093469 | Phenylaminopropanol Derivatives and Methods of Their Use - The present invention is directed to phenylaminopropanol derivatives of formula I: | 04-09-2009 |
20090131418 | SPIROAZACYCLIC COMPOUNDS AS MONOAMINE RECEPTOR MODULATORS - The present invention relates to spiroazacyclic compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds. | 05-21-2009 |
20090137566 | Substituted Piperdines as Renin Inhibitors - The invention relates to substituted 3,4- or higher substituted piperididine compounds, the use thereof for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; pharmaceutical formulations or products comprising said compounds, and/or a method of treatment comprising administering said compounds, a method for the manufacture of said compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis. The compounds preferably have the formula I, | 05-28-2009 |
20090137567 | Methods for Treating Blood Disorders - Methods of treating blood disorders are described. | 05-28-2009 |
20090137568 | Tryclic Nitrogen Containing Compounds and their Use as Antibacterials - Tricyclic nitrogen containing compounds of formula (I) and their use as antibacterials. | 05-28-2009 |
20090176772 | METHOD OF REVERSING LEFT VENTRICULAR REMODELING - The present invention relates to method of reversing left ventricle remodeling by combined administration of therapeutically effective amounts ranolazine and at least one co-remodeling agent, which may be an ACE inhibitor, an ARB, or a beta-blocker. The method finds utility in the treatment of heart failure. This invention also relates to pharmaceutical formulations that are suitable for such combined administration. | 07-09-2009 |
20090186882 | CGRP RECEPTOR ANTAGONISTS - The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions. | 07-23-2009 |
20090192144 | Imidazo Compounds - The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof in which R, R | 07-30-2009 |
20090192145 | Spiro-Imidazo Compounds - Novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R | 07-30-2009 |
20090215756 | FORMULATIONS CONTAINING LOSARTAN AND/OR ITS SALTS - The invention relates, in general, to new formulations and dosage units containing losartan and/or its salts (e.g., losartan potassium) that are useful for the therapeutic treatment (including prophylactic treatment) of mammals, including humans, and a process for making the same. The process generally includes (i) mixing and blending losartan potassium and a first portion of at least one of pre-gelatinized starch, microcrystalline cellulose and magnesium stearate to the mixture of step (i); (ii) compacting the mixture obtained in step (i) to form an agglomerate; (iii) breaking apart the agglomerate in order to obtain a granulate; (iv) adding lactose monohydrate and a second portion of at least one of pre-gelatinized starch, microcrystalline cellulose and magnesium stearate to the granulate and blending; and (v) tableting the granulate mixture into tablets. The process can further include coating the prepared tablets with a suitable coating material. | 08-27-2009 |
20090239851 | Benzothiazinone Derivatives and their Use as Antibacterial Agents - The present invention relates to novel benzothiazin derivatives and their use as antibacterial agents in infectious diseases of mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and leprosy caused by mycobacteria. | 09-24-2009 |
20090270374 | DERIVATIVES AND ANALOGS OF N-ETHYLQUINOLONES AND N-ETHYLAZAQUINOLONES - Bicyclic nitrogen containing compounds and their use as antibacterials. | 10-29-2009 |
20090270375 | SPIRO ANTIBIOTIC DERIVATIVES - The invention relates to compounds of formula (I) wherein R | 10-29-2009 |
20090275565 | Substituted aralkyl derivatives - The present invention relates to novel substituted aralkyl derivatives of the general formula (I) and (IIIa), their derivatives, their analogs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, pharmaceutical compositions containing them, use of these compounds in medicine and the intermediates involved in their preparation. | 11-05-2009 |
20090318428 | HETEROARYL DERIVATIVES AS PROTEIN KINASE INHIBITORS - Objects of the present invention are the compounds of formula I | 12-24-2009 |
20100004229 | Potassium Channel Inhibitors - The present invention relates to pyridin-3-yl pyridin-3-amine compounds and derivatives thereof having the structure formula (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like. | 01-07-2010 |
20100004230 | AZATRICYCLIC COMPOUNDS AND THEIR USE - Tricyclic nitrogen containing compounds and their use as antibacterials. | 01-07-2010 |
20100009975 | BENZOXAZINES, BENZOTHIAZINES, AND RELATED COMPOUNDS HAVING NOS INHIBITORY ACTIVITY - The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions. | 01-14-2010 |
20100009976 | BENZOTHIAZIN-3-ONE COMPOUND AND INTERMEDIATE THEREFOR - A medicine which contains as an active ingredient a benzothiazin-3-one-compound represented by the formula (1): | 01-14-2010 |
20100022520 | MALONYL-COA ACETYLTRANSFERASE INHIBITORS AGAINST ANTIBIOTIC RESISTANT BACTERTIA - Compounds characterized by thiolactone or thiomorpholino cores display useful antibiotic and radioprotective properties. The latter properties are believed to arise from an ability of the compounds to inhibit proteins involved in apoptosis. | 01-28-2010 |
20100029623 | 4-(1-AMINO-ETHYL)-CYCLOHEXYLAMINE DERIVATIVES - The invention relates to compounds of formula (I) wherein R | 02-04-2010 |
20100056502 | COMPOUNDS - Tricyclic nitrogen containing compounds and their use as antibacterials. | 03-04-2010 |
20100081650 | Antimicrobial Compounds - Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man. | 04-01-2010 |
20100087424 | TRICYCLIC NITROGEN CONTAINING HETEROCYCLES AS ANTIBACTERIAL AGENTS - Tricyclic nitrogen containing compounds and their use as antibacterials. | 04-08-2010 |
20100093707 | ACID AMIDE DERIVATIVES, PROCESS FOR THEIR PRODUCTION AND PESTICIDES CONTAINING THEM - The present invention relates to an acid amid derivative of the formula (I) or a salt thereof: | 04-15-2010 |
20100120754 | IDENTIFICATION AND USE OF SMALL MOLECULES TO MODULATE TRANSCRIPTION FACTOR FUNCTION AND TO TREAT TRANSCRIPTION FACTOR ASSOCIATED DISEASES - The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor. | 05-13-2010 |
20100130484 | NOVEL BICYCLIC SULFONAMIDE DERIVATIVES WHICH ARE L-CPT1 INHIBITORS - The invention is concerned with novel heterobicyclic derivatives of formula (I) | 05-27-2010 |
20100137290 | OXAZOLIDINONE ANTIBIOTIC DERIVATIVES - The invention relates to antibacterial compounds of formula I | 06-03-2010 |
20100144717 | 2-QUINOLINONE AND 2-QUINOXALINONE-DERIVATIVES AND THEIR USE AS ANTIBACTERIAL AGENTS - The present invention relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, to their use in the treatment of bacterial infections, and to their methods of preparation. | 06-10-2010 |
20100152172 | 2,4-PYRIMIDINEDIAMINE COMPOUNDS FOR TREATING OR PREVENTING AUTOIMMUNE DISEASES - The present invention provides 3-hydroxyphenyl-2,4-pyrimidinediamine compounds of formula I, as well as related compositions and methods for treating a variety of autoimmune diseases. | 06-17-2010 |
20100179134 | PYRIMIDINEDIAMINE KINASE INHIBITORS - The present invention provides pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also provided are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders. | 07-15-2010 |
20100179135 | 3-AMINO-6-(1-AMINO-ETHYL)-TETRAHYDROPYRAN DERIVATIVES - Antibacterial compounds including 3-amino-6-(1-amino-ethyl)-tetrahydropyran derivatives are provided, and methods of treatment or prevention of bacterial infection with such compounds are provided. | 07-15-2010 |
20100184751 | HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF TUBERCULOSIS - Tricyclic nitrogen-containing compounds of Formula (I) or pharmaceutically acceptable salts, solvates or N-oxides thereof: | 07-22-2010 |
20100197670 | AMIDINE, THIOUREA AND GUANIDINE DERIVATIVES OF 2-AMINOBENZOTHIAZOLES AND AMINOBENZOTHIAZINES FOR THEIR USE AS PHARMACOLOGICAL AGENTS FOR THE TREATMENT OF NEURODEGENERATIVE PATHOLOGIES - Amidine, thiourea and guanidine derivatives of appropriately substituted 2-aminobenzothiazoles, 2-amino-3,1-4H-benzothiazines and 3-amino-1,4-3H-benzothiazines, as understood from formula (I), the related pharmaceutically acceptable salts and solvates thereof: | 08-05-2010 |
20100222334 | Pharmaceutical Formulation of Valsartan - The present invention relates to a pharmaceutical composition in a form of suspension for oral administration comprising valsartan or its pharmaceutically acceptable salts and at least one or two or more of the components selected from glycerol or syrup or the mixture thereof, a preservative, a buffer system and a suspending/stabilizing agent. The present invention further relates to the therapeutic uses of the pharmaceutical composition. | 09-02-2010 |
20100286130 | ANTIMICROBIAL COMPOUNDS, THEIR SYNTHESIS AND THEIR USE FOR TREATMENT OF MAMMALIAN INFECTIONS - The present invention relates to compounds of Formula (I) | 11-11-2010 |
20100305110 | CONDENSED IMIDAZOLE DERIVATIVES AS ALDOSTERONE SYNTHASE INHIBITORS - The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferable pharmaceutically acceptable salts, thereof, in which R, R | 12-02-2010 |
20100324030 | 5-Quinoline derivatives having an anti-bacterial activity - The present invention describes novel anti-bacterial compounds of the formula (I). | 12-23-2010 |
20100331318 | AZATRICYCLIC ANTIBIOTIC COMPOUNDS - The invention relates to antibacterial compounds of formula I | 12-30-2010 |
20110003798 | COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS - The invention provides a novel class of 2,7-naphthyridin derivatives; pharmaceutical compositions comprising such compounds and methods of using such compounds to treat o prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT*, c-Kit, RET, TrkA, TrkB, TrkC-GR-1R, Alk, c-FMS or combinations thereof. | 01-06-2011 |
20110009394 | TRICYCLIC NITROGEN COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS - Tricyclic nitrogen containing compounds and their use as antibacterials. | 01-13-2011 |
20110009395 | BACE INHIBITORS - The present invention provides BACE inhibitors of Formula I: | 01-13-2011 |
20110021509 | PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS - Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. The compounds have the general structure: | 01-27-2011 |
20110034445 | FUNGICIDE HYDROXIMOYL-HETEROCYCLES DERIVATIVES - The present invention relates to hydroximoyl-heterocycle derivatives, their process of preparation, intermediate compounds for their preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. | 02-10-2011 |
20110039836 | TRICYCLIC ANTIBIOTICS - The invention relates to antibacterial compounds of formula (I) | 02-17-2011 |
20110046119 | THERAPEUTIC TREATMENT - A combination comprising candesartan and rosuvastatin for the prevention or treatment of atherosclerosis and for the prevention of cardiovascular events is described. | 02-24-2011 |
20110071142 | IDENTIFICATION AND USE OF SMALL MOLECULES TO MODULATE TRANSCRIPTION FACTOR FUNCTION AND TO TREAT TRANSCRIPTION FACTOR ASSOCIATED DISEASES - The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor. The present invention also relates to various compounds described herein (e.g., a compound of Formula XI), their pharmaceutically acceptable salts and to methods of using said compounds as described herein. | 03-24-2011 |
20110071143 | FUSED TRIAZOLE AMINES AS P2X7 MODULATORS - Compounds of the formula I: | 03-24-2011 |
20110082132 | [4-(1-AMINO-EHTYL) - CYCLOHEXYL] -METHYL-AMINE AND [6-(1-AMINO-EHTYL) -TETRAHYDRO-PYRAN-3-YL] -METHYL-AMINE DERIVATIVES AS ANTIBACTERIALS - The invention relates to antibacterial compounds of formula I | 04-07-2011 |
20110082133 | PYRIDONE COMPOUNDS - [Problems] A useful compound which can be used as a pharmaceutical, in particular, an agent for treating peripheral arterial occlusive disease is provided. | 04-07-2011 |
20110092492 | IMIDAZO COMPOUNDS - Heterocyclic compounds of the formula (I) and salts, preferably pharmaceutically acceptable salts thereof, are provided in which R, R | 04-21-2011 |
20110118241 | 6-Pyridin-3-YL-3,4-Dihydro-1H-Quinolin-2-One Derivatives and Related Compounds as Inhibitors of the Human Aldosterone Synthase CYP11B2 - The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 β-hydroxylase (CYP11 B1). | 05-19-2011 |
20110136794 | NOVEL PYRROLE DERIVATIVE HAVING, AS SUBSTITUENTS, UREIDO GROUP, AMINOCARBONLY GROUP AND BICYCLIC GROUP WHICH MAY HAVE SUBSTITUENT - A compound represented by the following formula (1) or a salt thereof: | 06-09-2011 |
20110136795 | TRICYCLIC ALKYLAMINOMETHYLOXAZOLIDINONE DERIVATIVES - The invention relates to antibacterial compounds of formula I | 06-09-2011 |
20110160193 | New Benzothiazinone Derivatives and Their Use as Antibacterial Agents - The present invention relates to novel benzothiazinone derivatives and their use as antibacterial agents in infectious diseases of mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and leprosy caused by mycobacteria. The present invention aims at the generation of new compounds with activity against mycobacteria as potential new tuberculosis drugs to overcome problems concerning resistance and drug intolerance. The solution of the present invention is a compound of formula I | 06-30-2011 |
20110183968 | ANTIFUNGAL COMPOUNDS CONTAINING BENZOTHIAZINONE, BENZOXAZINONE OR BENZOXAZOLINONE AND PROCESS THEREOF - The present invention discloses novel compounds of the Formula (1), comprising benzothiazinone, benzoxazinone or benzoxazolinone moieties having antifungal activity, method for preparing these compounds and the use of these compounds as antifungal agents in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds. | 07-28-2011 |
20110190278 | BICYCLIC HETEROCYCLIC DERIVATIVE - The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt thereof, being useful as a renin inhibitor. | 08-04-2011 |
20110195961 | TRICYCLIC OXAZOLIDINONE ANTIBIOTIC COMPOUNDS - The invention relates to antibacterial compounds of formula I | 08-11-2011 |
20110251185 | BENZOXAZINES AND RELATED NITROGEN-CONTAINING HETEROBICYCLIC COMPOUNDS USEFUL AS MINERALOCORTICOID RECEPTOR MODULATING AGENTS - The present invention relates to a compound, useful as a mineralocorticoid receptor-modulating agent, of the following formula [I]: | 10-13-2011 |
20110257165 | BICYCLIC PYRAZOLES AS PROTEIN KINASE INHIBITORS - 3,4-diaryl-bicyclicpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer. | 10-20-2011 |
20110269749 | TRICYCLIC CARBAMATE JAK INHIBITORS - The present disclosure relates to 2,4-pyrimidinediamines substituted with tricyclic carbamates and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, such as JAK2 or JAK3, is therapeutically useful. | 11-03-2011 |
20110281854 | MORPHOLINE COMPOUNDS - Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans. | 11-17-2011 |
20120028969 | BICYCLIC ACETYL-COA CARBOXYLASE INHIBITORS AND USES THEREOF - The present invention provides compounds of formula (I); | 02-02-2012 |
20120094984 | FUSED AMINODIHYDROTHIAZINE DERIVATIVES - A compound represented by the general formula: | 04-19-2012 |
20120108576 | THIAZOLE COMPOUNDS AND METHODS OF USE - The present invention provides compounds, salts and hydrates of Formula I, | 05-03-2012 |
20120108577 | COMPOUNDS FOR THE TREATMENT OF MULTI-DRUG RESISTANT BACTERIAL INFECTIONS - The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. | 05-03-2012 |
20120122855 | BENZOXAZINES, BENZOTHIAZINES, AND RELATED COMPOUNDS HAVING NOS INHIBITORY ACTIVITY - The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions. | 05-17-2012 |
20120149691 | Pyrrolo [1,2-b] Pyridazine Derivatives as Janus Kinase Inhibitors - The invention provides compounds of formula I: | 06-14-2012 |
20120165322 | RHO KINASE INHIBITORS - The present invention relates to compounds of formula (I): | 06-28-2012 |
20120190672 | FUSED AMINODIHYDROTHIAZINE DERIVATIVES - The present invention relates to a fused aminodihydrothiazine derivative of formula (I): | 07-26-2012 |
20120220574 | METHODS OF UTILIZING ARYLPIPERAZINE DERIVATIVES - The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression. | 08-30-2012 |
20120245152 | 3-(BIARYOXY)PROPIONIC ACID DERIVATIVE - A compound of the general formula (I): | 09-27-2012 |
20120245153 | MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION - Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and use thereof. | 09-27-2012 |
20120245154 | SUBSTITUTED AMINOTHIAZINE DERIVATIVE - The present invention relates to an agent for treating or preventing disease induced by production, secretion and/or deposition of amyloid β protein, for example, a compound of formula (I), wherein, R | 09-27-2012 |
20120245155 | FUSED HETEROCYCLIC COMPOUND HAVING AMINO GROUP - The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-βproteins. | 09-27-2012 |
20120258961 | 4-AMINO-1,3-THIAZINE OR OXAZINE DERIVATIVE - The present invention provide a medicament for treating the diseases induced by production, secretion or deposition of amyloid-β proteins, for example, a compound of the following formula (I) wherein R | 10-11-2012 |
20120270864 | 2-QUINOLINONE AND 2-QUINOXALINONE-DERIVATIVES AND THEIR USE AS ANTIBACTERIAL AGENTS - The present invention relates to compounds of Formula (I): | 10-25-2012 |
20130012501 | PYRIMIDINEDIAMINE KINASE INHIBITORS - Disclosed embodiments provide pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders. | 01-10-2013 |
20130053373 | Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, | 02-28-2013 |
20130131049 | COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION - Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: | 05-23-2013 |
20130131050 | FUSED HETEROCYCLIC COMPOUND AND APPLICATION THEREOF - The present invention provides a compound useful for the prophylaxis or treatment of eicosanoid-associated diseases such as atherosclerosis, atherothrombosis, diabetes, obesity, asthma, fever, pain, cancer, rheumatism, osteoarthritis, atopic dermatitis and the like, and having superior pharmacological action, physicochemical properties and the like. | 05-23-2013 |
20130203740 | FUSED AMINODIHYDROTHIAZINE DERIVATIVES - The present invention relates to a fused aminodihydrothiazine derivative of formula (I): | 08-08-2013 |
20130203741 | FUSED AMINODIHYDROTHIAZINE DERIVATIVES - A compound represented by the general formula: | 08-08-2013 |
20130231333 | ESTROGEN RECEPTOR MODULATORS AND USES THEREOF - Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors. | 09-05-2013 |
20130245007 | 2-PIPERAZIN-1-YL-4H-1,3-BENZOTHIAZIN-4-ONE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF MAMMALIAN INFECTIONS - The present invention relates to new 2-piperazin-1-yl-4H-1,3-benzothiazin-4-one derivatives and their use for the treatment of mammalian infections caused by bacteria, especially diseases like tuberculosis (TB), Buruli ulcer and leprosy that result from infection with closely related mycobacteria. (I). | 09-19-2013 |
20130261111 | TETRAHYDROPYRROLOTHIAZINE COMPOUNDS - The present invention provides compounds of Formula I: | 10-03-2013 |
20130274251 | 2-(2-PHENYLETHENYL) 1,3-BENZODIAZEPINE COMPOUNDS USEFUL FOR THE TREATMENT OF CANCER - The present invention provides compounds of formula (1) acting as protein kinase (PK) and receptor kinase (RK) signaling modulators. The invention further provides methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as anti-cancer agents for preventions and treatments of PK- and RK-related disorders, in particular cancer. (I) wherein A is H or CN; Z is S, SO or S0 | 10-17-2013 |
20130296308 | Heterocyclic Substituted Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds - Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, | 11-07-2013 |
20130338152 | FLUOROPHENYL BICYCLIC HETEROARYL COMPOUNDS - The present invention provides a compound the invention, and its use as a IGF-1R inhibitor. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 12-19-2013 |
20140094454 | TETRAHYDROPYRROLOTHIAZINE COMPOUNDS - The present invention provides compounds of Formula I: | 04-03-2014 |
20140107109 | AMINO-DIHYDROTHIAZINE AND AMINO-DIOXIDO DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE ANTAGONISTS AND METHODS OF USE - The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: | 04-17-2014 |
20140142091 | FUSED AMINODIHYDROTHIAZINE DERIVATIVES - The present invention relates to a fused aminodihydrothiazine derivative of formula (I): | 05-22-2014 |
20140142092 | COMPOUNDS AND METHODS FOR SKIN REPAIR - The disclosure provides compositions and methods for wound healing and scar reduction. The compositions and methods of the invention include at least one mixed EP2/EP4 agonist set forth herein. Wounds and or scars that can be treated by the compositions and methods of the invention can arise from events such as surgery, trauma, disease, mechanical injury, burn, radiation, poisoning, and the like. | 05-22-2014 |
20140142093 | TRICYCLIC OXAZOLIDINONE ANTIBIOTIC COMPOUNDS - The present invention relates to antibacterial compounds of formula (I) wherein “----” is a bond or is absent, V is CH, CR | 05-22-2014 |
20140142094 | KINASE INHIBITORS - This disclosure relates to compounds, methods for their preparation, pharmaceutical compositions including these compounds and methods for the treatment of cellular proliferative disorders, including, but not limited to cancer. The method includes administering to the patient a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof. | 05-22-2014 |
20140163015 | HEXAHYDROPYRANO[3,4-d][1,3]THIAZIN-2-AMINE COMPOUNDS - The present invention provides compounds of Formula I, and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure | 06-12-2014 |
20140163016 | BENZOXAZINES, BENZOTHIAZINES, AND RELATED COMPOUNDS HAVING NOS INHIBITORY ACTIVITY - The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions. | 06-12-2014 |
20140171425 | QUINAZOLINE-2,4-DIONE DERIVATIVES - The invention relates to antibacterial compounds of formula (I), wherein R | 06-19-2014 |
20140179690 | FUSED AMINODIHYDROTHIAZINE DERIVATIVES - The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; R is monofluoromethyl or difluoromethyl; and pharmaceutically acceptable salts thereof; which compound has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia. | 06-26-2014 |
20140206676 | SUBSTITUTED 4-(1H-PYRAZOL-4-YL)BENZYL ANALOGUES AS POSITIVE ALLOSTERIC MODULATORS OF MACHR M1 RECEPTORS - In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M | 07-24-2014 |
20140235625 | 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. | 08-21-2014 |
20140275044 | TETRAHYDROPYRROLOTHIAZINE COMPOUNDS - The present invention provides a compound of Formula I: | 09-18-2014 |
20140303152 | BENZOTHIAZINETHIONE DERIVATIVES AND PREPARATION METHODS AND USES THEREOF - Benzothiazinethione derivatives of formula (I), their preparative methods and uses are provided. Benzothiazinethione derivatives of the invention have significant effect of inhibiting | 10-09-2014 |
20140309218 | 3,7-DISUBSTITUTED OCTAHYDRO-2H-PYRIDO[4,3-E][1,3]OXAZIN-2-ONE ANTIBIOTICS - The invention relates to antibacterial compounds of formula I | 10-16-2014 |
20140323474 | Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds - The present invention provides compounds of Formula I, and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure | 10-30-2014 |
20140364426 | Heteroaryl-Substituted Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds - The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, | 12-11-2014 |
20140371212 | BACE INHIBITORS - The present invention provides a compound of Formula III: | 12-18-2014 |
20150038497 | BRIDGED BICYCLIC AMINO THIAZINE DIOXIDE COMPOUNDS AS INHIBITORS OF BETA-SECRETASE AND METHODS OF USE THEREOF - The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: | 02-05-2015 |
20150072975 | TRICYCLIC ANTIBIOTICS - The present invention relates to antibacterial compounds of formula I: | 03-12-2015 |
20150087637 | Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, | 03-26-2015 |
20150133438 | Heterocyclic Substituted Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds - Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, | 05-14-2015 |
20150291621 | 2-Amino-6-Methyl-4,4a,5,6-Tetrahydropyrano[3,4-d][1,3]Thiazin-8a(8H)-yl-1,- 3-Thiazol-4-yl Amides - The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, | 10-15-2015 |
20150329506 | 4,6-DIARYLAMINOTHIAZINES AS BACE1 INHIBITORS AND THEIR USE FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION - Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: (I) wherein R | 11-19-2015 |
20150344500 | C2,C6 OXACYCLIC-FUSED THIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE - In its many embodiments, the present invention provides certain C2-ring-substituted iminothiazine compounds, including compounds Formula (I): (structurally represented) or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and, wherein R1, R2, R3, R4, X, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed. | 12-03-2015 |
20150353547 | Antibacterial Oxadiazolone Derivatives - The invention relates to antibacterial compounds of formula I | 12-10-2015 |
20150353571 | 1,3-BENZOTHIAZINONE SULFOXIDE AND SULFONE COMPOUNDS - A compound, having the following formula: | 12-10-2015 |
20150376207 | Substituted Phenyl Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds - The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, | 12-31-2015 |
20160002264 | Carbocyclic- And Heterocyclic-Substituted Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds - The present invention provides compounds of formula I, | 01-07-2016 |
20160060276 | QUINOLONE DERIVATIVES - The invention relates to antibacterial compounds of formula I | 03-03-2016 |
20160075722 | Antibacterial Biaromatic Derivatives - The invention relates to antibacterial compounds of formula I (I) wherein R is H, cyano, alkoxy, cyanomethoxy, cycloalkylmethoxy, hydroxyalkoxy, alkoxyalkoxy, alkoxycarbonyl, 2-ethoxy-2-oxoethoxy, 2-(methylamino)-2-oxoethoxy, (1-cyanocyclobutyl)methoxy, 3-hydroxy-pyrrolidin-1-yl or 3,4-dihydroxycyclopentyl)methoxy; U | 03-17-2016 |
20160102084 | COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful. | 04-14-2016 |
20160152637 | 2-Amino-6-Methyl-4,4a,5,6-Tetrahydropyrano[3,4-d][1,3]Thiazin-8a(8H)-yl-1,- 3-Thiazol-4-yl Amides | 06-02-2016 |
20160158243 | IGF-1R SIGNALING PATHWAY INHIBITORS USEFUL IN THE TREATMENT OF NEURODEGENERATIVE DISEASES - The present invention provides compounds acting as Insulin/IGF signaling modulators useful in the treatment of neurodegenerative diseases and disorders. The invention provides pharmaceutical compositions including such compounds, and methods of using these compounds and compositions for the treatment of neurodegenerative diseases, in particular neurodegenerative diseases caused by proteotoxicity such as Alzheimer's disease. | 06-09-2016 |
20160176849 | N-CYANOMETHYLAMIDES AS INHIBITORS OF JANUS KINASE | 06-23-2016 |
20170233410 | A TETRAHYDROPYRROLO[3,4-D][1,3]THIAZINE-DERIVATIVE AS BACE INHIBITOR | 08-17-2017 |