| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 540544000 | The hetero ring contains chalcogen | 63 |
| 20090082560 | AMINODIHYDROTHIAZINE DERIVATIVES - A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): | 03-26-2009 |
| 20100076186 | PROCESS FOR PREPARING HETEROCYCLES - Provided is a process for preparing a heterocycle by catalytic reaction of an aromatic dinitrile with an amino alcohol, wherein the process includes: initially charging into a reaction vessel the amino alcohol and a catalyst to produce a reaction mixture; adding the aromatic dinitrile into the reaction mixture, which is maintained at a reaction temperature, wherein no solvent other than the amino alcohol of formula (III) is added to the reaction mixture prior to and/or during the catalytic reaction; and after completion of the catalytic reaction, completely replacing, or substantially completely replacing, unreacted amino alcohol with a nonpolar solvent to obtain the heterocycle, wherein the unreacted amino alcohol is present in an amount of not more than 20 wt. %, preferably 3-10 wt. % or less, based on a total weight of the heterocycle. | 03-25-2010 |
| 20100249399 | AMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME - Disclosed is a compound having a strong affinity to serotonin-4 receptors, which is useful as an enterokinesis-promoting agent or a digestive tract function-improving agent. Specifically, disclosed is a compound represented by Formula (1) or a pharmaceutically acceptable salt thereof. Also specifically disclosed is a pharmaceutical composition containing a compound represented by Formula (1) or a pharmaceutically acceptable salt thereof. [In Formula (1), Ar represents a group represented by Formula (Ar-1) or Formula (Ar-2).] | 09-30-2010 |
| 20100267946 | PRODRUGS OF GABA ANALOGS, COMPOSITIONS AND USES THEREOF - The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders. | 10-21-2010 |
| 20100298557 | PYRAZOLOPYRIMIDINE COMPOUND - Disclosed is a novel compound having Syk and/or Abl inhibitory activities, which is useful for prevention/treatment of allergic diseases, autoimmune diseases, arthritides and cancers. Specifically disclosed is a pyrazolopyrimidine compound represented by the formula [I] or [III] below, a tautomer thereof, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, or a solvent of any of them. | 11-25-2010 |
| 20110196150 | Arylmethoxy Isoindoline Derivatives and Compositions Comprising and Methods of Using the Same - Provided are 4′-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed. | 08-11-2011 |
| 20120016116 | AMINODIHYDROTHIAZINE DERIVATIVES - A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): | 01-19-2012 |
| 20120022249 | AMINODIHYDROTHIAZINE DERIVATIVES - A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): | 01-26-2012 |
| 20120029188 | Substituted Aniline Derivatives - The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections. | 02-02-2012 |
| 20120095216 | 3-[1,4]OXAZEPANE-4-PYRIMIDONE DERIVATIVES - A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: | 04-19-2012 |
| 20120190845 | FUSED COMPOUNDS THAT INHIBIT VANILLOID RECEPTOR SUBTYPE 1 (VR1) RECEPTOR - The present invention discloses novel compounds of general formula (I) | 07-26-2012 |
| 20120253035 | 1,4-OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS - The present invention relates to 1,4 Oxazepines of formula I | 10-04-2012 |
| 20130072677 | NOVEL HYDROXAMIC ACID DERIVATIVE - Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including | 03-21-2013 |
| 20130197217 | 1, 2, 4-TRIAZOLONE DERIVATIVE - The present invention provides a 1,2,4-triazolone derivative represented by Formula (1A) having an antagonistic activity on the arginine-vasopressin 1b receptor or a pharmaceutically acceptable salt thereof and provides a pharmaceutical composition comprising the compound or the salt as an active ingredient, in particular, a therapeutic or preventive agent exhibiting favorable pharmacokinetics in a disease such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, or alopecia. | 08-01-2013 |
| 20130253186 | HETEROARYLOXYHETEROCYCLYL COMPOUNDS AS PDE10 INHIBITORS - Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like. | 09-26-2013 |
| 20130303755 | AMINODIHYDROTHIAZINE DERIVATIVES - A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): | 11-14-2013 |
| 20140039181 | METHOD FOR PRODUCING N-SUBSTITUTED AMINE COMPOUNDS THROUGH CATALYZED ALKYLATION - The invention relates to a method for producing a N-substituted amine compound by catalyzed alkylation. The method uses amine and alcohol or two kinds of amines as the reaction materials, employs composite metal oxides catalyst at a reaction temperature of 80-180° C. to catalyze the reaction for 6-36 hours, so as to produce the N-substituted amine compound. The reaction condition of the method of the invention is relatively moderate, using a catalyst made of cheap non-noble metals, which is non-caustic and easy to be separated and reused. The reaction does not need any medium and has relatively high conversion rate and selectivity. | 02-06-2014 |
| 20140058097 | PHARMACEUTICAL COMPOSITION FOR TREATING ALZHEIMER'S DISEASE - A pharmaceutical composition for treating Alzheimer's disease containing a compound represented by the general formula (I): | 02-27-2014 |
| 20140107335 | Cyclic Amines - The present invention is directed to novel cyclic amines which inhibit the P2X | 04-17-2014 |
| 20140336374 | PROCESS AND INTERMEDIATES FOR THE PRODUCTION OF CCR2 ANTAGONISTS - The present invention relates to a process for the production of novel antagonists for CCR2 (CC chemokine receptor 2) and intermediates thereof. | 11-13-2014 |
| 20150011751 | NOVEL TRIAZINE DERIVATIVE - To provide a novel triazine derivative represented by the following formula (I):
| 01-08-2015 |
| 20150011752 | TRIAZINE COMPOUNDS AS PI3 KINASE AND MTOR INHIBITORS - Compounds of formula I | 01-08-2015 |
| 20150344436 | PKM2 MODULATORS AND METHODS FOR THEIR USE - Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. | 12-03-2015 |
| 20160060240 | CHROMENONE DERIVATIVES - The invention concerns chromenone derivatives of Formula I | 03-03-2016 |
| 20160096810 | ENANTIOSELECTIVE SYNTHESIS OF DIALKYLATED N,O-HETEROCYCLES BY PALLADIUM-CATALYZED ALLYLIC ALKYLATION - This invention provides enantioenriched N,O-heterocyclic compounds with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): | 04-07-2016 |
| 20160200721 | AROMATIC HETEROCYCLYLAMINE DERIVATIVE HAVING TRPV4-INHIBITING ACTIVITY | 07-14-2016 |
| 540545000 | Plural nitrogens in the heterocyclic ring | 8 |
| 20090124800 | PROCESS FOR THE PREPARATION OF [1,4,5]-OXADIAZEPINE DERIVATIVES - A process for the preparation of [1,4,5]-oxadiazepine derivatives by reaction of 4,5-diacyl-[1,4,5]-oxadiazepines with a base. | 05-14-2009 |
| 20090192307 | INHIBITORS OF PROTEIN KINASES - The present invention is directed to a compound having the formula | 07-30-2009 |
| 20090299059 | Novel Compound Having Heterocyclic Ring - The invention provides a novel oxazolidinone derivative represented by the formula (I): | 12-03-2009 |
| 20100048890 | CONJUGATED SMALL MOLECULES - Provided herein are linker compounds and conjugates that include the linker compounds. In one embodiment, the linker compounds comprise 2 or 3 residues of 6-aminohexanoic acid and optionally 7-10 residues of polyethyleneglycol (PEG). The linker compounds are useful in forming conjugates with one or more components useful in biopharmaceutical or bioanalytical applications. In particular, the biopharmaceutically useful compounds are kinase inhibitors. The conjugates described herein have utility in a variety of diagnostic, separation, and therapeutic applications. | 02-25-2010 |
| 20100179318 | PROCESS TO MAKE LESTAURTINIB - A process to make lestaurtinib, also known as (9S-(9α,10β,12α))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-(hydroxymethyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3′,2′,1′-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one is disclosed. | 07-15-2010 |
| 20110207925 | PROCESS FOR THE PREPARATION OF [1,4,5]-OXADIAZEPINE DERIVATIVES - A process for the preparation of [1,4,5]-oxadiazepine derivatives by reaction of 4,5-diacyl-[1,4,5]-oxadiazepines with a base. | 08-25-2011 |
| 20120184734 | SUBSTITUTED POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE - This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity. | 07-19-2012 |
| 20120208997 | NOVEL COMPOUND HAVING HETEROCYCLIC RING - The invention provides a novel oxazolidinone derivative represented by the formula (I): | 08-16-2012 |
| 540546000 | Polycyclo ring system which contains the hetero ring as one of the cyclos | 29 |
| 20120253036 | AGENT FOR TREATING FIBROMYALGIA - An agent for treating fibromyalgia containing a 5-HT | 10-04-2012 |
| 540547000 | Tricyclo ring system which contains the hetero ring as one of the cyclos | 19 |
| 20080200671 | Crystal form of asenapine maleate - The invention relates to an orthorhombic crystal form of compound trans-5-chloro-2,3,3a, 12b-tetrahydro-2-methyl-1H-dibenz [2,3:6,7] oxepino [4,5-c] pyrrole (Z)-2-butenedioate, to methods for the preparation of this crystal form and to pharmaceutical compositions comprising an orthorhombic crystal form. | 08-21-2008 |
| 20110021771 | INHIBITORS OF HISTONE DEACETYLASE - This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification. | 01-27-2011 |
| 540548000 | At least three ring hetero atoms in the tricyclo ring system | 4 |
| 20110313150 | CHIRAL DISULFONIMIDES - Chiral disulfonimides having the formula I to III, | 12-22-2011 |
| 20140058098 | BENZOXAZEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z | 02-27-2014 |
| 20140275523 | PROCESS FOR MAKING BENZOXAZEPIN COMPOUNDS - Processes are described for the preparation of PI3K inhibitor, GDC-0032, Formula I, having the structure: | 09-18-2014 |
| 20160052933 | BENZOXAZEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z | 02-25-2016 |
| 540551000 | Nitrogen bonded directly to ring carbon of the hetero ring | 13 |
| 20090076262 | PROCESS FOR PREPARING QUETIAPINE AND QUETIAPINE FUMARATE - The invention comprises a process for preparing quetiapine and/or its salts, including, quetiapine fumarate. The process generally comprises reacting dibenzothiazepinone (dibenzo[bf][1,4]thiazepin-11(10H)-one) with phosphorous oxychloride in the presence of triethylamine in an aromatic organic solvent such as toluene or, preferably, xylene at reflux temperature to obtain an aromatic hydrocarbon solution of 11-chloro-dibenzo[bf][1,4]thiazepine. Thereafter, the 11-chloro-dibenzo[bf][1,4]thiazepine is reacted with 2-(2-piperazin-1-ylethoxy)-ethanol to yield, following several processing steps, quetiapine. Compound I can then be further reacted with fumaric acid at elevated temperature to yield quetiapine fumarate. The resulting quetiapine fumarate obtained is suitable for use in pharmaceutical preparations. | 03-19-2009 |
| 20090118497 | Crystallization Process of Quetiapine Hemifumarate - The present invention relates to a process for preparing crystalline quetiapine hemifumarate, which comprises crystallizing or re-crystallizing quetiapine hemifumarate from a mixture of water and a water soluble alcohol. | 05-07-2009 |
| 20090156802 | Quetiapine Hemifumarate Purification by Crystallization - The present invention relates to a process for preparing and purifying crystalline quetiapine hemifumarate, which comprises preparing crystalline quetiapine hemifumarate via a crystalline salt, which is not a salt of fumaric acid. | 06-18-2009 |
| 20090275747 | METHODS FOR THE PREPARATION OF SALTS OF 2-[2-(4-DIBENZO[B,F][1,4]THIAZEPIN-11-YL-1-PIPERAZINYL)ETHOXYL]ETHANOL (QUETIAPINE) AND FOR THE PURIFICATION THEREOF - A method for the preparation of salts of 2-[2-(4-dibenzo[b,fj[1,4]thiazepin-11-yl-1-piperazinyl)ethoxy]ethanol (quetiapine) from the quetiapine base and the respective acid, wherein the salt is precipitated from a mixture of solvents, the mixture being either a mixture of an aromatic hydrocarbon and a ketone or ester, or that of an aromatic hydrocarbon, water and a ketone or ester. The salts of quetiapine are purified by partial crystallization, wherein only a part of the salt of quetiapine is dissolved in a C | 11-05-2009 |
| 20100016579 | Crystalline forms of quetiapine hemifumarate - The present invention relates to novel crystalline forms of quetiapine hemifumarate, denominated quetiapine hemifumarate form II and quetiapine hemifumarate form III. These novel crystalline forms of quetiapine hemifumarate have been characterized by methods including x-ray powder diffraction (XRD), Fourier transform IR spectroscopy (FTIR), differential scanning calorimetry (DSC), and thermal gravimetric analysis (TGA). Methods for preparation of the novel crystalline quetiapine hemifumarate form II as its chloroform solvate and its dichloromethane solvate, form III as its chloroform solvate, and form I are provided. | 01-21-2010 |
| 20100168416 | POLYCYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed. | 07-01-2010 |
| 20110112290 | PROCESS FOR THE PREPARATION OF QUETIAPINE - The invention relates to a method for the preparation of 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f]-1,4-thiazepine and pharmaceutically acceptable salts thereof comprising the reaction of 1-[2-(hydroxyethoxy)-ethyl]piperazine with dibenzo[b,f][1,4]thiazepin-11-ylamine. | 05-12-2011 |
| 20110118460 | PROCESS FOR THE SYNTHESIS OF QUETIAPINE - The present invention relates to a process for the synthesis of quetiapine. In particular, a process is provided for the synthesis of quetiapine of formula (A) comprising reacting dibenzo[b,f][1,4]thiazepin-11(10H)-one, intermediate (I) with phosphorous oxychloride to give 11-chlorodibenzo[b,f][1,4]thiazepine, intermediate (II) wherein the said reaction of intermediate (I) to intermediate (II) is performed in an organic solvent in the presence of a mixture of an organic base together with an inorganic base. | 05-19-2011 |
| 20110230657 | PROCESS FOR PREPARING QUETIAPINE FUMARATE-TOLUENE-WATER - The present invention relates to an improved process for preparing Quetiapine fumarate of formula (I). | 09-22-2011 |
| 20120071649 | PROCESS FOR THE PREPARATION OF QUETIAPINE FUMARATE - The present invention relates to an improved process for the preparation of quetiapine and pharmaceutically acceptable salts. It also relates to improved process for the preparation of intermediates of quetiapine. | 03-22-2012 |
| 20120095217 | FLUORINE CONTAINING COMPOUNDS AND METHODS OF USE THEREOF - Fluorinated compounds and methods of making fluorinated compounds are described herein. | 04-19-2012 |
| 20120202991 | DIBENZOTHIAZEPINE DERIVATIVES AND USES THEREOF - 424 - Compounds the following formula: | 08-09-2012 |
| 20140066618 | Method Of Forming An Aerosol For Inhalation Delivery - The present invention relates to the inhalation delivery of aerosols containing small particles. Specifically, it relates to a method of forming an aerosol for use in inhalation therapy. The method involves: (a) heating a substrate coated with a composition comprising a drug to form a vapor, wherein the coated composition is in the form of a film less than 10 μthick; and, (b) allowing the vapor to cool, thereby forming an aerosol, which is used in inhalation therapy. In another aspect, a method of forming an aerosol for use in inhalation therapy is provided, wherein the method comprises: (a) heating a substrate coated with a composition comprising a drug to form a vapor in less than 100 milliseconds, wherein the vapor has a mass greater than 0.1 mg; and, (b) allowing the vapor to cool, thereby forming an aerosol, which is used in inhalation therapy | 03-06-2014 |
| 540552000 | Bicyclo ring system which contains the hetero ring as one of the cyclos | 9 |
| 20090292119 | METHODS FOR SYNTHESIZING BENZOTHIAZEPINE COMPOUNDS - The present invention provides improved methods for synthesizing novel benzothiazepine compounds. In particular, the invention relates to a new method that generally is used to make the substituted 2,3,4,5-tetrahydro-1,4-benzothiazepine compounds of a general formula | 11-26-2009 |
| 20100152440 | NOVEL ANTI-ARRHYTHMIC AND HEART FAILURE DRUGS THAT TARGET THE LEAK IN THE RYANODINE RECEPTOR (RyR2) - The present invention provides novel 1,4-benzothiazepine intermediates and derivatives, methods for synthesizing same, and methods for assaying same. The present invention also provides methods for using these novel compounds to limit or prevent a decrease in the level of RyR2-bound FKBP12.6 in a subject; to prevent exercise-induced sudden cardiac death in a subject; and to treat or prevent heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia in a subject. The present invention further provides methods for identifying an agent that enhances binding of RyR2 and FKBP12.6, and agents identified by these methods. Additionally, the present invention provides methods for identifying agents for use in treating or preventing heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia, and in preventing exercise-induced sudden cardiac death. Also provided are agents identified by such methods. | 06-17-2010 |
| 20100174065 | COMPOUNDS - The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders. | 07-08-2010 |
| 20110282054 | PYRAZINOOXAZEPINE DERIVATIVES - Provided is a compound having a serotonin 5-HT | 11-17-2011 |
| 20110288291 | PYRAZINOOXAZEPINE DERIVATIVES - Provided is a compound having a serotonin 5-HT | 11-24-2011 |
| 20140018533 | NOVEL FURANONE DERIVATIVE - To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I): | 01-16-2014 |
| 20140121368 | PROCESS FOR PREPARING BENZOTHIAZEPINES FROM GAMMA-AMINOALKYLBENZENES - The invention provides a process for preparing a 2,3,4,5-tetrahydro[1.4]benzothiazepine of formula: | 05-01-2014 |
| 20150105549 | INTERMEDIATES TO PREPARE HERBICIDAL PYRIMIDONE DERIVATIVES - Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, | 04-16-2015 |
| 20160039777 | CRYSTAL MODIFICATIONS OF ELOBIXIBAT - The present invention relates to crystal modifications of N-{(2R)-2-[({[3,3-dibutyl-7-(methyl-thio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl]oxy}acetyl)amino]-2-phenylethanolyl}glycine (elobixibat), more specifically crystal modifications I, IV, MeOH-1, EtOH-1, 1-PrOH-1 and 2-PrOH-1. The invention also relates to a process for the preparation of these crystal modifications and to a pharmaceutical composition comprising crystal modification IV. | 02-11-2016 |
