Class / Patent application number | Description | Number of patent applications / Date published |
514254040 | The additional five-membered hetero ring consists of three ring carbons, and of nitrogen and chalcogen in adjacent ring positions (e.g., isoxazolyl, isothiazolyl, etc.) | 53 |
20080255148 | THERAPEUTIC AGENT FOR SENILE DEMENTIA - A therapeutic/preventive agent for cognitive dysfunctions, which comprises as an active ingredient an imide derivative of the following formula [1]: | 10-16-2008 |
20080269246 | METHOD FOR TREATING PEDIATRIC BIPOLAR DISORDER - The present invention, in one aspect, relates to a method of using piperazinyl-heterocyclic compounds of the formula I, as defined below, for enhancing cognition in a mammal, including a human, for example a mammal afflicted with psychosis, autism, dementia, or mental retardation, comprising administering an effective amount of a compound of formula I (for example, ziprasidone) to the mammal. In another aspect, the present invention is directed to a method for reducing or ameliorating in a mammal, including a human, afflicted with a disorder or condition selected from autism, mental retardation, obsessive-compulsive disorder, and dementia, positive symptoms (e.g. excessive aggression, disinhibited sexual behavior, inappropriate sexual behavior, agitation, compulsive behavior such as head banging, lip biting, self mutilation, or stereotypic behavior) associated with the aforementioned disorders or conditions, which method comprises administering an effective amount of a compound of formula I (for example, ziprasidone) to the mammal. In another aspect, the present invention is directed to a method for treating pediatric bipolar disorder in a mammal, including a human, which method comprises administering an effective amount of a compound of formula I (for example, ziprasidone) to the mammal. | 10-30-2008 |
20090062303 | DEUTERIUM-ENRICHED ZIPRASIDONE - The present application describes deuterium-enriched ziprasidone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-05-2009 |
20090076027 | DEUTERIUM-ENRICHED LURASIDONE - The present application describes deuterium-enriched lurasidone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090137605 | POLYMORPHIC FORMS OF ZIPRASIDONEAND ITS HYDROCHLORIDE SALT AND PROCESS FOR PREPARATION THEREOF - The present invention is related to crystalline forms of ziprasidone and its hydrochloride salt and an amorphous form of ziprasidone hydrochloride and the process for the preparation thereof. The crystalline forms and amorphous form of the invention are suitable for pharmaceutical purposes in the treatment of psychosis. The processes of the invention are simple, non-hazardous and commercially suitable. | 05-28-2009 |
20090143404 | Pharmaceutical composition - A preparation for oral administration comprising: a pregelatinized starch comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1′R,2′S,3′R,4′S)-2,3-bicyclo[2,2,1]-heptanedicarboxyimide hydrochloride (lurasidone) represented by the formula (1) as an active ingredient; a water-soluble excipient; and a water-soluble polymeric binder, the preparation exhibiting an invariant level of elution behavior even when the content of its active ingredient is varied. | 06-04-2009 |
20090163514 | BENZISOXAZOLE PIPERAZINE COMPOUNDS AND METHODS OF USE THEREOF - The invention includes benzisoxazole piperazine compositions and methods of using them for modulating sleep. | 06-25-2009 |
20090176800 | IN VIVO SCREENING METHOD OF THERAPEUTIC AGENT FOR MEMORY/LEARNING DYSFUNCTIONS BY SCHIZOPHRENIA - A method of evaluating memory/learning functions with the use of a model with glutamic acid N-methyl-D-aspartate (NMDA) type receptor hypofunction as an animal model for schizophrenia and with the use of reference memory task, wherein there has been found concrete means for detecting any differences in activity between typical anti-psychosis drugs and atypical anti-psychosis drugs is found. | 07-09-2009 |
20090286806 | ISOXAZOLE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type or T-type calcium channel activity are disclosed. Specifically, a series of isoxazole containing compounds are disclosed of the general formula (1) where Z is N or CHNR | 11-19-2009 |
20100075984 | DICARBONYLIC COMPOUNDS WITH ANTIBACTERIAL ACTIVITY - Compounds of formula (I), and their pharmaceutically acceptable salts and solvates, wherein X represents —O—, —NH—, —S—, —NHC(═O)— or —NHC(═S)—; R1 represents —H or a hydrocarbon chain; R2 represents —H, alkoxy, amino, a hydrocarbon chain or a radical of a cycle; R3 represents —H, a hydrocarbon chain or a radical of a cycle; R4 represents —H or a hydrocarbon chain; alternatively R3 and R4 form together a cycle; R5 and R6 represent —H or halogen, and R7 represents —H, a hydrocarbon chain or heteroaryl, are useful against bacterial infections in animals, including humans. | 03-25-2010 |
20100075985 | BENZO[D]ISOXAZOL-3-YL-PIPERAZIN DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS - The present invention provides compounds of the general formula (I), having affinity and selectivity for the dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the therapeutic and/or prophylactic treatment of cognitive disorders. | 03-25-2010 |
20100081668 | POLYMORPHS OF 5--6-CHLORO-1,3-DIHYDRO-2H-INDOL-2-ONE HYDROBROMIDE AND PROCESSES FOR PREPARATION THEREOF - The present invention provides pharmaceutically applicable compounds and polymorphs belonging to the ziprasidone hydrobromide compound group with antipsychotic effect. The present invention provides hydrobromide polymorphs of 5-{-2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-ethyl}-6-chloro-1,3-dihydro-2H-indol-2-one, ziprasidone of Formula (I) having neuroleptic activity. | 04-01-2010 |
20100105697 | THERAPEUTIC AGENTS - The present invention is directed to therapeutic agents of the formula (I) which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction. wherein; R | 04-29-2010 |
20100240676 | THIAZOLE DERIVATIVES - Compounds of the formula (I), in which R | 09-23-2010 |
20100280045 | NOVEL COMPOUNDS - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): | 11-04-2010 |
20110124659 | CYCLOALKANE DERIVATIVE - The present invention relates to a novel cycloalkane derivative which has a useful psychotropic action with less side effect. | 05-26-2011 |
20110166156 | Prodrugs for the Treatment of Schizophrenia and Bipolar Disease - Compounds of Formula I and Formula II and their use for the treatment of neurological and psychiatric disorders including schizophrenia and manic or mixed episodes associated with bipolar I disorder with or without psychotic features is disclosed. | 07-07-2011 |
20110183993 | CYCLOALKANE DERIVATIVE - The present invention relates to a novel cycloalkane derivative which has an excellent psychotropic action. | 07-28-2011 |
20110212975 | ANTIVIRAL COMPOUNDS AND METHODS OF MAKING AND USING THEREOF - Compounds which exhibit antiviral activity, particularly against influenza virus, and methods of making and using thereof are described herein. In one embodiment, the compounds are heterocyclic amides containing piperazine and isozazole rings and optionally substituted with one or more substituents. The compounds can be formulated with one or more pharmaceutically acceptable excipients to form compositions suitable for enteral or parenteral administration. The compounds are preferably used to treat or prevent Influenza A infections, such as H1N1, H2N2, H3N2, H5N1, H7N7, H1N2, H9N2, H7N2, H7N3, and H10N7. | 09-01-2011 |
20110237602 | METHOD FOR TREATING SCHIZOPHRENIA AND RELATED DISEASES - The invention relates to a method for treating schizophrenia and/or related diseases comprising administering lurasidone and a mGluR2 ligand to a mammal in need thereof. | 09-29-2011 |
20110306620 | Heteroarylpiperidine And-Piperazine Derivatives - Heteroarylpiperidine and -piperazine derivatives of the formula (I), | 12-15-2011 |
20120142701 | COMPOUNDS AND METHODS FOR THE TREATMENT OF PROLIFERATIVE DISEASES - Cell-based and cell-free assays are disclosed that detect compounds that promote aggregation of proteins, glycoproteins, and protein-nucleic acid complexes. Also disclosed are pharmaceutical formulations useful for treating or preventing viral infections, bacterial infections, cancer, and diseases involving hyper-proliferative cells. | 06-07-2012 |
20120149715 | COMPOUNDS AND METHODS FOR THE TREATMENT OF VIRAL INFECTIONS - High throughput and virtual screening methods are disclosed that can identify potential anti-viral agents. The virtual screening methods identify agents that interact with a viral nucleoprotein binding site. The high throughput methods identify compounds that inhibit viral infection by binding to viral nucleoprotein. Also disclosed are pharmaceutical formulations useful for treating or preventing viral infections, especially influenza A. | 06-14-2012 |
20120165341 | THERAPEUTIC AGENT FOR SENILE DEMENTIA - A therapeutic/preventive agent for cognitive dysfunctions, which comprises as an active ingredient an imide derivative of the following formula [1]: | 06-28-2012 |
20120220603 | SUBSTITUTED HETEROCYCLIC DERIVATIVES FOR THE TREATMENT OF PAIN AND EPILEPSY - Compounds of formula (I) which are useful in ameliorating conditions characterized by unwanted sodium and/or calcium channel activity, particularly unwanted Na | 08-30-2012 |
20120316181 | HEXAHYDRO-1H-4,7-METHANOISOINDOLE-1,3-DIONE COMPOUNDS - The present invention is directed to therapeutic agents which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction. | 12-13-2012 |
20130172365 | ARYLOSULFONAMIDES FOR THE TREATMENT OF CNS DISEASES - Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system. | 07-04-2013 |
20130178481 | HEXAHYDRO-1H-4,7-METHANOISOINDOLE-1,3-DIONE COMPOUNDS - The present invention is directed to therapeutic agents which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction. | 07-11-2013 |
20130217699 | PARASITICIDAL DIHYDROISOXAZOLE COMPOUNDS - Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds. | 08-22-2013 |
20130345236 | PHARMACEUTICAL COMPOSITIONS PROVIDING ENHANCED DRUG CONCENTRATIONS - A drug in a solubility-improved form is combined with a concentration-enhancing polymer in a sufficient amount so that the combination provides substantially enhanced drug concentration in a use environment relative to a control comprising the same amount of the same solubility-improved form of drug without the concentration-enhancing polymer. | 12-26-2013 |
20140031364 | PHENYL-ISOXAZOL DERIVATIVES AND PREPARATION PROCESS THEREOF - Disclosed are a phenyl-isoxazol derivative compound, which is useful as a treatment material for virus infection, especially, infection of an influenza virus, or its pharmaceutically acceptable derivative, a preparation method thereof, and an illness treatment pharmaceutical composition including the compound as an active ingredient. | 01-30-2014 |
20140113911 | BENZOPYRONE DERIVATIVE AND USE THEREOF - The present invention relates to the field of pharmaceutical chemistry, and in particular, to a benzopyrone derivative and a use thereof. The benzopyrone derivative is compound having a structure of formula (I) or a pharmaceutically acceptable salt thereof. It has been found by experiments that, this type of compounds is useful in prevention or treatment of neuropsychical diseases. | 04-24-2014 |
20140113912 | TREATMENT AND MANAGEMENT OF CNS DISORDERS - The present disclosure relates to methods of treating certain CNS disorders. The present disclosure also relates to biomarkers for monitoring or predicting the efficacy of a treatment for a CNS disorder by lurasidone, or a pharmaceutically acceptable salt, solvate, clathrate or stereoisomer thereof. | 04-24-2014 |
20140171441 | PHARMACEUTICAL COMPOSITIONS WITH ENHANCED PERFORMANCE - Pharmaceutical compositions of a low-solubility drug and lower alkanoate-, phthalate- and trimellitate esters of hydroxypropyl methyl cellulose and lower alkanoate- and succinate esters of cellulose and methyl cellulose are disclosed that provide enhanced concentrations of the drug in a use environment. | 06-19-2014 |
20140171442 | ALICYCLIC[C] BENZOPYRONE DERIVATIVES AND USES THEREOF - Disclosed are alicyclic[c]benzopyrone derivatives and use thereof. The alicyclic[c]benzopyrone derivatives are compounds represented by formula I or their salts. The present compounds not only significantly improve high activity induced by MK-801, but also effectively improve clambering symptom induced by Apomorphine and do not cause EPS within effective dose. These in vitro targets and in vivo pharmacological models are closely related to diseases of the nervous system caused by dopamine dysfunction, especially schizophrenia. Therefore the present compounds can be used for the treatment of central nervous system diseases, especially schizophrenia. ED | 06-19-2014 |
20140235651 | PHARMACEUTICAL COMPOSITION - A preparation for oral administration comprising: a pregelatinized starch comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1′R,2′S,3′R,4′S)-2,3-bicyclo[2,2,1]-heptanedicarboxylmide hydrochloride (lurasidone) represented by the formula (1) as an active ingredient; a water-soluble excipient; and a water-soluble polymeric binder, the preparation exhibiting an invariant level of elution behavior even when the content of its active ingredient is varied. | 08-21-2014 |
20140256740 | COMPOUNDS AND METHODS - The present invention relates to novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ. | 09-11-2014 |
20140275113 | CRYSTALLINE FORMS OF TRYOSINE KINASE INHIBITORS AND THEIR SALTS - The invention relates to various polymorphic forms and amorphous form of sodium 4-((3-(4-cyclohexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl)amino)benzate, including the polymorphic form A, mixtures of the polymorphs, process for the preparation thereof and the use thereof in a pharmaceutical composition containing thereof. | 09-18-2014 |
20140343076 | PHARMACEUTICAL COMPOSITIONS OF LURASIDONE - The present invention relates to pharmaceutical compositions of lurasidone or salts thereof. In particular, the invention relates to pharmaceutical compositions of lurasidone or salts thereof with one or more acids. The invention also relates to processes for the preparation of such compositions and use thereof for treatment of schizophrenia, bipolar disorders or senile dementia. | 11-20-2014 |
20140350029 | LURASIDONE NOVEL DOSAGE REGIMENS AND USE THEREOF FOR THE TREATMENT, PREVENTION, AND/OR MANAGEMENT OF AT LEAST ONE CNS DISORDER - Dosage regimens for at least one compound chosen from Iurasidone and pharmaceutically acceptable salts, solvates, clathrates, and stereoisomers thereof are disclosed as are kits and methods for treatment and/or prevention of at least one CNS disorder such as, for example, mixed depression and bipolar disorder, and management of at least one CNS disorder, such as improving quality of life and reversing impairment in learning and memory associated with schizophrenia, comprising administering to a patient a therapeutically or prophylactically effective amount of at least one compound chosen from lurasidone and pharmaceutically acceptable salts, solvates, clathrates, and stereoisomers thereof. | 11-27-2014 |
20140371235 | SMALL MOLECULES TARGETING ANDROGEN RECEPTOR NUCLEAR LOCALIZATION AND/OR LEVEL IN PROSTATE CANCER - A method for treating prostate cancer in a subject, comprising administering a therapeutically effective amount of at least one agent to the subject, wherein the agent is selected from:
| 12-18-2014 |
20140371236 | AGENT FOR TREATMENT OF SCHIZOPHRENIA - The present invention provides a novel method for treatment of schizophrenia which can improve wide-ranging symptoms of schizophrenia, especially positive symptoms and negative symptoms without being accompanied by extrapyramidal symptoms, which comprises orally administering as an active compound (1R,23,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-piperazinylmethyl]-1-cyclohexylmethyl]-2,3-bicyclo[2.2.1]heptanedicarboxyimide or a pharmaceutically acceptable salt thereof (e.g., hydrochloride) at a daily dose of 5 mg to 120 mg once a day to a patient with schizophrenia, and a therapeutic agent to be used in said method. | 12-18-2014 |
20150018368 | PROCESS FOR PREPARING BENZISOTHIAZOL-3-YL-PIPERAZIN-1-YL-METHYL-CYCLO HEXYLMETHANISOINDOL-1,3-DIONE AND ITS INTERMEDIATES - The present invention discloses process for preparing benzisothiazol-3-yl-piperazin-1-yl-methyl-cyclo hexyl-methan-isoindol-1,3-dione and intermediates thereof. | 01-15-2015 |
20150072993 | Parasiticidal Dihydroisoxazole Compounds - Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds. | 03-12-2015 |
20150126523 | ANTIPARISITIC AND PESTICIDAL ISOXAZOLINE COMPOUNDS - The present invention relates to novel and inventive isoxazoline of formula (I) and salts thereof: | 05-07-2015 |
20150133468 | METHANETHIONE COMPOUNDS HAVING ANTIVIRAL ACTIVITY - A compound of formula (I) is useful as an antiviral agent, in particular for the treatment of influenza. A method for preparing the compound of formula (I) and a composition including the compound of formula (I) are described. | 05-14-2015 |
20150297586 | USE OF BENZO FIVE-MEMBERED NITROGEN HETEROCYCLIC PIPERAZINE OR PIPERIDINE DERIVATIVES - This invention relates to the use of a compound in formula (I) and its salts acceptable pharmaceutically in preparation of vasodilative drugs: | 10-22-2015 |
20150336985 | FUNGICIDAL HETEROCYCLIC COMPOUNDS - Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, | 11-26-2015 |
20150368718 | METHOD OF TREATMENT BASED ON POLYMORPHISMS OF THE KCNQ1 GENE - The invention provides methods for the administration of compounds capable of prolonging a QTc interval and methods for predicting whether an individual is predisposed to such QTc prolongation. | 12-24-2015 |
20150374684 | COMPOSITION AND METHOD FOR TREATMENT OF DEPRESSION AND PSYCHOSIS IN HUMANS - Compositions and methods for the treatment of depression and psychoses in humans are disclosed. More particularly, the invention is directed to formulations containing antipsychotic and/or antidepressant medications and also containing an NMDAR antagonist. The present Invention Is also directed to methods tor the treatment of humans suffering from depression and other psychoses, including, schizophrenia, by administration of the inventive compositions in antidepressant and/or antipsychotic effective amounts. | 12-31-2015 |
20160002182 | CRYSTALLINE FORMS OF TRYOSINE KINASE INHIBITORS AND THEIR SALTS - The invention relates to various polymorphic forms and amorphous form of sodium 4-((3-(4-cyclohexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl)amino)benzate, including the polymorphic form A, mixtures of the polymorphs, process for the preparation thereof and the use thereof in a pharmaceutical composition containing thereof. | 01-07-2016 |
20160158228 | SUSTAINED-RELEASE FORMULATION FOR INJECTION - The present invention relates to a composition comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1′R,2′S,3′R,4′S)-2,3-bicyclo[2,2,1]heptanedicarboximide or a pharmaceutically acceptable acid addition salt thereof. In detail, the composition relates to a sustained release formulation for injection which maintains an effective blood level of the above-mentioned compound. | 06-09-2016 |
20160193205 | METHOD OF TREATMENT FOR MENTAL DISORDERS | 07-07-2016 |