Class / Patent application number | Description | Number of patent applications / Date published |
514266300 | Chalcogen bonded directly to a ring carbon of the 1,3-diazine ring of the quinazoline ring system | 51 |
20080234299 | Quinazolinones - Compounds of the formula (I), in which R, R | 09-25-2008 |
20080249116 | QUINAZOLINONE DERIVATIVES AS ALDH-2 INHIBITORS - Disclosed are novel quinazolinone derivatives, useful as ALDH-2 inhibitors for treating mammals for various disease states, such as treatment for cocaine dependency or alcohol dependency. | 10-09-2008 |
20080255164 | Novel 2-Aminopyrimidinone Derivatives And Their Use - This invention relates to novel compounds having the structural formula I below: (I) and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia. | 10-16-2008 |
20080287473 | NOVEL MOLECULES FOR REGULATING CELL DEATH - The present invention provides compounds capable of regulating apoptosis, e.g., via regulating mitochondrial fission or fusion. The present invention also provides methods of screening for compounds capable of regulating apoptosis and methods of treating conditions association with apoptosis. | 11-20-2008 |
20080306095 | Control of Ectoparasites - Disclosed is a method of controlling ectoparasites that infest companion and livestock animals by applying to the animal an effective amount of 4-tert-butylphenethyl quinazolin-4-yl ether or 4-chloro-5-ethyl-2-methyl-N-[(4-tert-butylphenyl)methyl]pyrazole-3-carboxamide or 5-chloro-N-[2-[4-(2-ethoxyethyl)-2,3-dimethylphenoxy]ethyl]-6-ethyl-4-pyrimidinamine or 4-chloro-3-ethyl-1-methyl-N-[4-(p-tolyloxy)benzyl]pyrazole-5-carboxamide. | 12-11-2008 |
20090036473 | NOVEL QUINAZOLINONE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel quinazolinone derivatives having medical utility, to use of the quinazolinone derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the quinazolinone derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of K | 02-05-2009 |
20090054470 | USE OF MITOCHONDRIAL ELECTRON TRANSPORT INHIBITORS TO CONTROL FOULING ORGANISMS - The present invention relates to the use of mitochondrial electron transport inhibitors (METI's) to control or combat fouling organisms. More particularly, the present invention relates to the use of mitochondrial electron transport inhibitors for protecting materials against fouling by marine or freshwater fouling organisms and an antifouling composition suitable for use therefore. This invention thus relates to the field of protection of materials that are exposed to humid or aqueous environments. | 02-26-2009 |
20090137614 | Pharmaceutical combination comprising vitamin k - It is found that compounds having PPARδ agonistic activity induced abnormal blood coagulation or muscular disorder. A pharmaceutical combination comprising vitamin K and a compound having PPARδ agonistic activity can prevent the abnormal blood coagulation. A pharmaceutical composition comprising vitamin K can prevent muscular disorder. | 05-28-2009 |
20090163525 | SUBSTITUTED QUINAZOLINES WITH ANTI-CANCER ACTIVITY - The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man. | 06-25-2009 |
20090215801 | Novel 2-Aminopyrimidinone Derivatives And Their Use - This invention relates to novel compounds having the structural formula I below: (I) and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia. | 08-27-2009 |
20090281128 | CASPASE INHIBITORS AND USES THEREOF - The present invention relates to compounds of formula I: | 11-12-2009 |
20090291973 | Novel Quinazoline Derivatives and Their Medical Use - This invention relates to novel quinazoline derivatives having medical utility, to use of the quinazoline derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the quinazoline derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of K | 11-26-2009 |
20090318478 | QUINAZOLINE DERIVATIVES - The invention discloses quinazoline derivatives or salts thereof, which possess PDE9-inhibiting activity and are useful as treating agents of dysuria and the like, the derivatives being represented by the formula (I) | 12-24-2009 |
20100029695 | METHOD OF TREATING DERMATITIS COMPRISING ADMINISTERING A CHYMASE INHIBITOR - A medicament safe and free from side effects, for the prevention or treatment of dermatitis exhibiting a biphasic inflammation reaction or dermatitis induced by repeated exposure to an antigen, which suppresses the progress of the condition and improves the quality of life of the patient, which medicament treats dermatitis exhibiting a biphasic inflammation reaction or dermatitis induced by repeated exposure to an antigen by including a quiazoline derivative having the formula (I) or (II) or its pharmaceutically acceptable salt as an effective ingredient: | 02-04-2010 |
20100063073 | Methods and Compositions Utilizing Quinazolinones - Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity. | 03-11-2010 |
20100152213 | COMPOUND THAT IS A DUAL INHIBITOR OF ENZYMES PDE7 AND/OR PDE4, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - The invention relates to a series of dual inhibitors of enzymes PDE7 and PDE4, having formula (I) and to the use thereof in the production of pharmaceutical compositions for the treatment of inflammatory and/or autoimmune processes. | 06-17-2010 |
20100197705 | Quinazolinone Derivatives Useful as Vanilloid Antagonists - There is described a new polymorphic form of 4-(7-Hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile having structural formula I(B) and to a method of preparing it. | 08-05-2010 |
20100197706 | DERIVATIVES OF 1-OXO-1,2-DIHYDROISOQUINOLINE-5-CARBOXAMIDES AND OF 4-OXO-3,4-DIHYDROQUINAZOLINE-8-CARBOXAMIDES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPEUTICS - The present invention relates to derivatives of 1-oxo-1,2-dihydroisoquinoline-5-carboxamides and of 1-oxo-3,4-dihydroquinazoline-8-carboxamides, to the preparation thereof and to the therapeutic use thereof. | 08-05-2010 |
20100216823 | Spirocyclic Derivatives - The invention provides compounds of formula (I): | 08-26-2010 |
20100249158 | SUBSTITUTED AMINO-QUINAZOLINONES, MEDICAMENTS COMPRISING SAID COMPOUND, THEIR USE AND THEIR METHOD OF MANUFACTURE - The present invention relates to substituted amino-quinazolinones of general formula (I) wherein the groups R | 09-30-2010 |
20100267752 | 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses 3-hydroquinazolin-4-one derivatives for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cancer, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like. | 10-21-2010 |
20110009434 | CRYSTALS OF ISOPROPYL ESTER OF N-(2,6-DICHLOROBENZOYL)-4-[6-(METHYLAMINO)METHYL -1-METHYL-2,4-DIOXO-1,4-DIHYDROQUINAZOLINE-3(2H)-YL]-L- PHENYLALANINE HYDROCHLORIDE, PRODUCTION METHOD THEREOF AND USE THEREOF - Crystals of isopropyl ester of N-(2,6-dichlorobenzoyl)-4-[6-(methylamino)methyl-1-methyl-2,4-dioxo-1,4-dihydroquinazoline-3(2H)-yl]-L-phenylalanine hydrochloride are useful as α4 integrin inhibitors. | 01-13-2011 |
20110160231 | DIHYDROOROTATE DEHYDROGENASE AS ANTIFUNGAL DRUG TARGET AND QUINAZOLINONE-BASED INHIBITORS THEREOF - A method of identifying an antifungal agent which targets a DHODH protein (alias PyrE, dihydroorotate dehydrogenase, EC: 1.3.99.11) of a fungus comprising contacting a candidate substance with a fungal DHODH protein and determining whether the candidate substance binds or modulates the DHODH protein, wherein binding or modulation indicates that the candidate substance is an antifungal agent. Specific examples concern | 06-30-2011 |
20120046307 | ALLOSTERIC PROTEIN KINASE MODULATORS - The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family. | 02-23-2012 |
20120077829 | PARENTERAL SOLUTIONS CONTAINING METOLAZONE - Disclosed herein are parenteral solutions containing 7-halo-1,2,3,4-tetrahydro-3-aryl-6-quinazoline sulfonamide in N,N-dimethylactamide, polyethylene glycol and D | 03-29-2012 |
20120077830 | CASPASE INHIBITORS AND USES THEREOF - This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula I: | 03-29-2012 |
20120122902 | PYRIMIDINE DERIVATIVE, PREPARATION METHOD AND USE THEREOF - A pyrimidine derivative and the preparation method and usethereof. The said pyrimidine derivative is a diaryl pyrimidine derivative or a diaryl benzo pyrimidine derivative which has the structure shown as the Formula I and IV. | 05-17-2012 |
20130030013 | PHARMACEUTICAL PREPARATION COMPRISING PHENYLALANINE DERIVATIVE - The disclosed pharmaceutical preparation comprises a compound represented by the chemical formula (A) or a pharmaceutically acceptable salt thereof, which is dispersed in a matrix consisting of a water-soluble high molecular weight substance; and Crospovidone: | 01-31-2013 |
20130053408 | METHODS AND COMPOSITIONS UTILIZING QUINAZOLINONES - Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity. | 02-28-2013 |
20130184296 | PARENTERAL SOLUTIONS CONTAINING METOLAZONE - Disclosed herein are parenteral solutions containing 7-halo-1,2,3,4-tetrahydro-3-aryl-6-quinazoline sulfonamide in N,N-dimethylacetamide, polyethylene glycol and D | 07-18-2013 |
20130296349 | QUINAZOLINONE INHIBITORS OF DYNEIN - Compounds of formula (I) in which R | 11-07-2013 |
20140171455 | Reduction of Microglia-Mediated Neurotoxicity by Kv1.3 Inhibition - Methods for deterring microglia-mediated neurotoxicity in a human or non-human animal subjects comprising the step of inhibiting or blocking the intermediate-conductance calcium-activated potassium channel Kv1.3 in microglia, such as in subjects how suffer from neurodegenerative diseases (e.g., Alzheimer's Disease) or ischemic/anoxic/hypoxic conditions. The inhibition or blocking of the KCa1.3 channels may be accomplished by administering a substance that inhibits Kv1.3 in microglia. Examples of Kv1.3 inhibiting substances include certain 5-phenoxyalkoxypsoralens, such as (4-Phenoxybutoxy)psoralen (PAP-1) as well as certain 4-phenoxybutoxy-substituted heterocyclic compounds. | 06-19-2014 |
20140206705 | CRYSTALS OF SALTS OF PHENYLALANINE DERIVATIVES - Provided is a crystal of a salt of the compound represented by formula (I), which is excellent in its solubility in water. In particular, also provided is a crystal of hydrochloride, hydrobromate, sulfate, nitrate, p-toluenesulfonate or methanesulfonate of the compound represented by formula (I). | 07-24-2014 |
20140357652 | RHO KINASE INHIBITORS - Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds. | 12-04-2014 |
20160038491 | Controlled Release Auris Sensory Cell Modulator Compositions and Methods for the Treatment of Otic Disorders - Disclosed herein are compositions and methods for the treatment of otic diseases or conditions with auris sensory cell modulating agent compositions and formulations administered locally to an individual afflicted with an otic disease or condition, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s). | 02-11-2016 |
20160122362 | INHIBITORS OF PLASMODIUM FALCIPARUM EQUILIBRATIVE NUCLEOSIDE TRANSPORTER TYPE I AS ANTI-PARASITIC COMPOUNDS - Inhibitors of | 05-05-2016 |
20160136146 | COMPOSITIONS AND METHODS FOR TREATING PRIMARY EFFUSION LYMPHOMA - Methods for treating primary effusion lymphoma (PEL) are provided. The methods include administering to a patient in need thereof an effective amount of an immunomodulatory compound. Suitable immunomodulatory compounds include compounds having the formula: | 05-19-2016 |
514266310 | Carbocyclic ring bonded directly to a ring carbon of the quinazoline ring system | 14 |
20090209562 | Fused ring 4-oxopyrimidine derivative - The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circulatory diseases, or nervous system diseases. | 08-20-2009 |
20090233951 | Parenteral solutions containing metolazone - Disclosed herein are parenteral solutions containing 7-halo-1,2,3,4-tetrahydro-3-aryl-6-quinazoline sulfonamide in N,N-dimethylactamide, polyethylene glycol and D | 09-17-2009 |
20100063075 | Aryl-quinazoline/aryl-2amino-phenyl methanone derivatives - A compound of formula (1): wherein R1, R2, R3 and Y are as defined herein, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, useful for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable. | 03-11-2010 |
20100234404 | P-38 Kinase Inhibitors - Compounds and compositions for modulating the activity of p38 kinases are provided, including p38α, and p38β kinase. Methods for treating, preventing or ameliorating one or more symptoms of a p38 kinase mediated disease or disorder are also provided. | 09-16-2010 |
20100249161 | 2- ( 2 -HYDROXYPHENYL) -QUINAZOLIN-4-ONES USEFUL FOR TREATING OBESITY AND DIABETES - The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful, inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith. | 09-30-2010 |
20100261741 | Quinazolinone T-Type Calcium Channel Antagonists - The present invention is directed to quinazolinone compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved. | 10-14-2010 |
20120088782 | LPA RECEPTOR ANTAGONIST - A compound of the general formula (I): | 04-12-2012 |
20120129877 | USE OF QUINAZOLINE DERIVATIVES FOR NEURODEGENERATIVE DISEASES - The present invention relates to the use of a series of quinazoline-derived compounds to produce a medicament for the treatment and/or prevention of neurological and/or neurodegenerative diseases, such as Parkinson's disease or Alzheimer's disease. The present invention also relates to a method for the treatment and/prevention of neurological and/neurodegenerative diseases comprising the administration of a therapeutically effective amount of said compounds. | 05-24-2012 |
20130150387 | SUBSTITUTED AMINO-QUINAZOLINONES, MEDICAMENTS COMPRISING SAID COMPOUND, THEIR USE AND THEIR METHOD OF MANUFACTURE - The present invention relates to substituted amino-quinazolinones of general formula (I) wherein the groups R | 06-13-2013 |
20130281473 | SUBSTITUTED ISOQUINOLINONES AND QUINAZOLINONES - The invention relates to substituted nitrogen containing bicyclic heterocycles of the formula (I) | 10-24-2013 |
20140256754 | QUINAZOLINES AS B-GLUCURONIDASE NOVEL INHIBITORS - Quinazoline derivatives 1-25, (2-[3,4-bis(methyloxy)phenyl]quinazolin-4-(3H)-one) and 2-[2-(ethyloxy)phenyl]quinazoline-4-(3H)-one) are reported as β-glucuronidase inhibitors useful in the treatment of β-glucuronidase hyperactivity disorders. | 09-11-2014 |
20140371248 | SMALL MOLECULE ACTIVATORS OF HslV PROTEASE FOR DEVELOPMENT OF NOVEL ANTIMICROBIALS - HslVU is the proteasome-related system composed of HslV peptidase and HslU chaperone. It is involved in intracellular proteolysis. The presence of HslVU homologs in pathogenic microbes and its absence in human makes it an antimicrobial drug target. The functional HslVU complex forms when HslV dodecamer is flanked at both ends by HslU hexamers. In the HslVU complex, intercalation of C-termini residues of HslU subunits into the clefts between adjacent HslV subunits results in allosteric activation of HslV. We identified small molecules capable of activating HslV peptidase in the absence of its natural activator HslU. Quinazoline and chromone derivatives were suggested by ligand docking to bind at the HslU C-termini intercalation pockets in the HslV. This was confirmed by HslV activation assays with these compounds that gave ED | 12-18-2014 |
20160031831 | SUBSTITUTED BICYCLIC DIHYDROPYRIMIDINONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY - Substituted bicyclic dihydropyrimidinones of formula 1 | 02-04-2016 |
20160039772 | QUINAZOLINE-2,4(1H,3H)-DIONE DERIVATIVES - This invention relates to novel Quinazoline-2,4(1H,3H)-dione derivatives of Formula (I): | 02-11-2016 |