Class / Patent application number | Description | Number of patent applications / Date published |
540577000 | Plural nitrogens in the polycyclo ring system | 37 |
20090005556 | Process for Producing Pure Form of 2-Methyl-4-(4-Methyl-1-Piperazinyl)-10H-Thieno[2,3-b] [1,5]Benzodiazepine - Disclosed is a process for producing pure form of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine. The process comprises of reacting 2-(2-aminoanilino)-5-methylthiophene-3-carbonitrile with N-methyl piperazine in conjunction with N-methylpiperazine acid salt, to produce 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine. Also disclosed is a process for obtaining the Polymorphic Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine by crystallizing the crude 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine in a mixture of solvents. | 01-01-2009 |
20130274466 | PROCESS FOR THE PREPARATION OF TETRACYCLIC DERIVATIVES AND INTERMEDIATE PRODUCTS USED IN THE PROCESS - A process for preparation of a compound of formula I or a pharmaceutically acceptable salt thereof, is disclosed. The process involves subjecting a compound of formula II to Ullmann-type conditions to effect an intra-molecular ring closure reaction to form the compound of formula I. The different substituents are as described in the specification. Further, the process can provide an alternate route for the synthesis of asenapine from starting materials that can be readily available. | 10-17-2013 |
540578000 | Three or more hetero atoms in the polycyclo ring system | 17 |
20080207896 | Process For the Manufacture of Mirtazapine - Improved process for manufacturing mirtazapine. A process is described for preparing mirtazapine starting from a compound of formula (II), which is subjected to a ring cyclization, obtaining mirtazapine for pharmaceutical use in crystalline and anhydrous form. | 08-28-2008 |
20080255348 | METHOD FOR THE PREPARATION OF AN ENANTIOMER OF A TETRACYCLIC BENZAZEPINE - The present invention relates to a method for the preparation of mirtazapine and tetracyclic analogous compounds having substantial enantiomeric excess of the R or S form. The invention further relates to a novel intermediate and its use for the preparation of mirtazapine having a substantial enantiomeric excess of the R or S form. The method comprising the steps of a: providing a carboxylic acid compound according to Formula I having a substantial enantiomeric excess of the R or S form, b: converting the carboxylic acid group of compound I into a ketone group, producing a ketone compound of Formula II, c: optionally reducing ketone compound II with a mild reduction agent to form the intermediate hydroxy compound of Formula III and d: forming the mirtazapine of Formula IV by reduction of the ketone compound II or of the hydroxy compound III using a strong reduction agent. | 10-16-2008 |
20080255349 | METHOD FOR THE PREPARATION OF AN ENANTIOMERICALLY PURE BENZAZEPINE - The invention relates to a method for the preparation of a cyclic compound according to formula III comprising reacting a compound according to Formula I and a compound according to formula II, | 10-16-2008 |
20090275749 | PRODUCTION METHOD OF OPTICALLY ACTIVE PIPERAZINE COMPOUND - Provided is a method of producing optically active 1-methyl-3-phenylpiperazine of the formula (11) or salt thereof, comprising the following steps 1 to 4, or steps 5 to 7 and step 4, and a method of producing optically active mirtazapine via this method. | 11-05-2009 |
20090299060 | COMPOUNDS AND METHODS FOR INHIBITING MITOTIC PROGRESSION - This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer. | 12-03-2009 |
20100029934 | PROCESS FOR PRODUCTION OF MIRTAZAPINE - The invention provides a process for production of mirtazapine as a convenient process for obtaining mirtazapine from a reaction mixture obtained by cyclization of 2-(4-methyl-2-phenylpiperazin-1-yl)pyridine-3-methanol with concentrated sulfuric acid, at high purity and in a form suitable for safe use as a drug. | 02-04-2010 |
20100137581 | PROCESS FOR PREPARATION OF SUBSTANTIALLY PURE POLYMORPHIC FORM I OF OLANZAPINE - A process for preparation of substantially pure polymorphic Form I of olazapine consists in that olanzapine starting material is subjected to: a) at least one digestion step in an acidic aqueous medium, with an optional addition of active charcoal, and then to neutralizing to pH within the range from about 6.0 to about 11.0, and b) at least one step of separation of impurities in a water—organic solvent system, followed by crystallization from the solution in methylene chloride, and wherein steps a) and b) are separated by steps of isolation of precipitate of olanzapine and can be accomplished in any order. | 06-03-2010 |
20100179319 | PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE MIRTAZAPINE - The invention provides a process for efficiently producing optically active mirtazapine. Specifically, a process for production of optically active mirtazapine wherein an RS mixture of mirtazapine is optically resolved with optically active tartaric acid in the presence of a solvent. More specifically, a process for production of optically active mirtazapine, characterized by making an RS mixture of mirtazapine contact with optically active tartaric acid in the presence of a solvent, and preferentially crystallizing the optically active mirtazapine salt. The solvent is preferably a mixed solvent consisting of a water-soluble organic solvent and water, and more preferably a mixed solvent consisting of a C1-3 alcohol and water. | 07-15-2010 |
20100274004 | BICYCLIC PIRAZOLE COMPOUNDS AS ANTIBACTERIAL AGENTS - Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection. | 10-28-2010 |
20100274005 | BICYCLIC PYRAZOLE COMPOUNDS AS ANTIBACTERIAL AGENTS - Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection. | 10-28-2010 |
20100280240 | BICYCLIC PYRAZOLE COMPOUNDS AS ANTIBACTERIAL AGENTS - Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection. | 11-04-2010 |
20110201804 | PROCESS FOR THE PREPARATION OF 1- ( 3-HYDROXYMETHYLPYRID-2 -YL ) -2 -PHENYL-4-METHYLPIPERAZINE AND MIRTAZAPINE - Disclosed herein is a process for the manufacture of mirtazapine and intermediates useful in preparing mirtazapine which includes the reduction of 1-(3-carboxypyridyl-2)-4-methyl-2-phenylpiperazine with an organoaluminum hydride. | 08-18-2011 |
20110275801 | HETEROARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES - The present invention provides heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I | 11-10-2011 |
20140046055 | COMPOUNDS AND METHODS FOR INHIBITING MITOTIC PROGRESSION - This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer. | 02-13-2014 |
20160115172 | METHOD FOR PRODUCNG TRICYCLIC COMPOUND, AND TRICYCLIC COMPOUND CAPABLE OF BEING PRODUCED BY SAID PRODUCTION METHOD - An object of the present invention is to provide a method for reproducibly producing a pyrrolopyrimidine ring-containing tricyclic compound in high yield with reduced formation of by-products, and to provide a novel tricyclic compound capable of being obtained by this production method. The present invention provides a method for producing a compound represented by Formula (1) or a salt thereof, the method comprising the steps of: (I) causing an organic borane reagent to act on a compound represented by Formula (2) or a salt thereof, and (II) performing an intramolecular cyclization reaction of the reaction product of step (I) above using a zerovalent palladium catalyst in the presence of an alkali metal hydroxide. | 04-28-2016 |
20160185782 | COMPOUNDS AND METHODS FOR INHIBITING MITOTIC PROGRESSION - This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer. | 06-30-2016 |
20160200639 | INTERMOLECULAR C-H SILYLATION OF UNACTIVATED ARENES | 07-14-2016 |
540579000 | Nitrogen of the hetero ring is shared by an additional cyclo of the polycyclo ring system | 16 |
20090093630 | CHIRAL SYNTHESIS OF DIAZEPINOQUINOLINES - The present invention relates to improved methods of resolution and recrystallization for synthesizing compounds useful as 5HT | 04-09-2009 |
20100121050 | PROCESSES FOR MAKING ZILPATEROL AND SALTS THEREOF - This invention generally relates to processes for making zilpaterol and salts thereof, as well as processes for making intermediates that, inter alia, may be used to make zilpaterol and salts thereof. The zilpaterol and salts prepared in accordance with this invention can be used to increase the rate of weight gain, improve feed efficiency, and/or increase carcass leanness in livestock, poultry, and fish. | 05-13-2010 |
20110213143 | COMPOUND HAVING TAFIA INHIBITORY ACTIVITY - Provided are compounds having superior TAFIa inhibitory activity. Specifically, there are provided compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof: | 09-01-2011 |
20120116076 | SWITCHABLE SOLVENTS AND METHODS OF USE THEREOF - A solvent that reversibly converts from a nonionic liquid mixture to an ionic liquid upon contact with a selected trigger, e.g., contact with CO | 05-10-2012 |
20120253037 | METHODS AND COMPOSITIONS FOR PREPARING NORIBOGAINE FROM VOACANGINE - Disclosed are methods and compositions for preparing and purifying the non-addictive alkaloid noribogaine. | 10-04-2012 |
20130046092 | SWITCHABLE SOLVENTS AND METHODS OF USE THEREOF - A solvent that reversibly converts from a nonionic liquid mixture to an ionic liquid upon contact with a selected trigger, e.g., contact with CO | 02-21-2013 |
20130165647 | STEREOSELECTIVE TOTAL SYNTHESIS OF NORIBOGAINE - This invention relates generally to methods for synthesizing the non-addictive alkaloid noribogaine. | 06-27-2013 |
20130303756 | METHODS AND COMPOSITIONS FOR PREPARING NORIBOGAINE FROM VOACANGINE - Disclosed are methods and compositions for preparing and purifying the non-addictive alkaloid noribogaine. | 11-14-2013 |
20140039182 | COMPOSITIONS AND PROCESSES OF PREPARING AND USING THE SAME - The present invention relates to compositions, for example, the DBU/Hexafluoroacetone hydrate salt, and processes of preparing and using the same for the modification of chemical compounds via the release of trifluoroacetate. The DBU/Hexafluoroacetone hydrate salt can perform trifluoromethylation reactions on chemical compounds, such as carbonyl group-containing compounds. | 02-06-2014 |
20150094466 | SYNTHETIC VOACANGINE - Synthetic voacangine, including in substantially enantiomerically enriched forms, and derivatives thereof are provided. | 04-02-2015 |
20150119570 | PROCESS OF PREPARING ALCAFTADINE - The present invention is related to pure compound of structural formula (VIII), process for the purification of compound of structural formula (VIII) and improved process of preparing alcaftadine compound of structural formula (I). | 04-30-2015 |
20150133655 | METHODS AND COMPOSITIONS FOR PREPARING NORIBOGAINE FROM VOACANGINE - Disclosed are methods and compositions for preparing and purifying the non-addictive alkaloid noribogaine. | 05-14-2015 |
20150315195 | AN IMPROVED PROCESS FOR MAKING ZILPATEROL - This invention generally relates to processes for making zilpaterol and salts thereof, as well as processes for making intermediates that, interalia, may be used to make zilpaterol and salts thereof. | 11-05-2015 |
20150368255 | HALOGENATED INDOLE AND BENZOFURAN DERIVATIVES OF ISOQUINUCLIDENE AND PROCESSES FOR PREPARING THEM - Provided herein are halogenated indole and benzofuran derivatives of isoquinuclidene and intermediates thereto, and processes, preferably enantioselective processes, for preparing such derivatives including processes for preparing (−) and (+) noribogaine, in substantially enantiomerically pure forms. | 12-24-2015 |
20160024075 | INDOLE AND BENZOFURAN FUSED ISOQUINUCLIDENE DERIVATIVES AND PROCESSES FOR PREPARING THEM - Provided herein are indole and benzofuran fused isoquinuclidene derivatives. Also provided herein are processes, preferably enantioselective processes, for preparing such derivatives including processes for preparing (−) and (+) noribogaine or a salt thereof, in substantially enantiomerically pure forms. | 01-28-2016 |
20160083389 | PROCESS OF PREPARING ALCAFTADINE - The present invention relates to an improved process of preparing substantially pure alcaftadine comprising reacting substantially pure compound of structural formula VIII with more than 20 moles of oxidizing reagent in an organic solvent to obtain alcaftadine: | 03-24-2016 |
540580000 | The seven-membered hetero ring shares ring members with one other cyclo only | 2 |
20110046368 | LIGANDS OF 5-HT6 RECEPTORS, A PHARMACEUTICAL COMPOSITION, METHOD FOR THE PRODUCTION AND USE THEREOF - The invention relates to novel ligands of 5-HT | 02-24-2011 |
20140296513 | NOVEL THERAPEUTIC USE OF P75 RECEPTOR ANTAGONISTS - The present disclosure relates to the use of a p75 receptor antagonist or its pharmaceutically acceptable salts for the preparation of a medicament for use in the treatment and/or prevention of overactive bladder. | 10-02-2014 |