| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 544309000 | At 2-position and at 4- or 6-position | 36 |
| 20100087641 | Method and Materials for Quaternary Amine Catalyzed Bisulfite Conversion of Cytosine to Uracil - The invention provides methods and materials for the conversion of cytosine to uracil. A nucleic acid, such a gDNA, is reacted with bisulfate, such as magnesium bisulfite, in the presence of a quaternary amine catalyst. Examples of suitable quaternary amine catalysts include but are not limited to quaternary ammonium compounds, quaternary alkyl ammonium salts, quaternary alkyl ammonium halides, quaternary methyl ammonium bromide, quaternary ammonium chloride, tetraethyl ammonium hydroxide, tetraethylammonium chloride, tetrabutyl ammonium chloride, tetrabutyl ammonium bromide. The invention also contemplates kits of premeasured ingredients for carrying out the methods of the invention either on an individual sample or on a plurality of samples. | 04-08-2010 |
| 20140135497 | SYNTHESIS OF 2,4-DICHLORO-5-TRIFLUOROMETHYL-PYRIMIDINE - This invention relates to a novel method for the synthesis of 2,4-dichloro-5-trifluoromethyl-pyrimidine useful as intermediate in the manufacture of pharmaceutically active ingredients. | 05-15-2014 |
| 20160376241 | 5-(TRIFLUOROMETHYL)PYRIMIDINE DERIVATIVES AND METHOD FOR PRODUCING SAME - Provided are 5-(trifluoromethyl)pyrimidine derivatives useful as intermediates for pharmaceuticals and agrochemicals and as intermediates for electronic materials and methods for producing the same. 2,4-dichloro-5-(trifluoromethyl)pyrimidine is reacted with 2,2,2-trifluoroethanol, benzyl alcohol, or benzenethiol to obtain the intended 2-(2,2,2-trifluoroethoxy)-4-chloro-5-(trifluoromethyl)pyrimidine, 2-benzyloxy-4-chloro-5-(trifluoromethyl)pyrimidine, 2,4-bis(2,2,2-trifluoroethoxy)-5-(trifluoromethyl)pyrimidine, or 2-chloro-4-phenylthio-5-(trifluoromethyl)pyrimidine. | 12-29-2016 |
| 544310000 | Additional hetero ring which is unsaturated | 10 |
| 20090137802 | A2B ADENOSINE RECEPTOR ANTAGONISTS - Disclosed are processes for the synthesis of novel compounds that are A | 05-28-2009 |
| 20100029941 | PREPARATION OF (R)-3-AMINOPIPERIDINE DIHYDROCHLORIDE - Described herein are methods for making chiral derivatives of 3-aminopiperidine, including the production of such derivatives in quantities exceeding 1 kilogram. The chiral 3-aminopiperidine derivatives include (R)-3-aminopiperidine derivatives which may be used to synthesize inhibitors of Dipeptidyl Peptidase IV. (R)-3-Aminopiperidine dihydrochloride is prepared by reducing (R)-3-aminopiperidin-2-one hydrochloride with lithium aluminum hydride. The preparation of (R)-3-aminopiperidin-2-one hydrochloride starting from (R)-methyl-2,5-diaminopentanoate dihydrochloride or (R)-2,5-diaminopentanoic acid hydrochloride is also described. | 02-04-2010 |
| 20100204471 | MAPK/ERK KINASE INHIBITORS - Compounds, pharmaceutical compositions, kits and methods are provided for use with MEK that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. | 08-12-2010 |
| 20110060141 | REGIOSELECTIVE PREPARATION OF SUBSTITUTED PYRIMIDINES - The present invention relates to a method of making pyrimidines of formula (III), wherein X1, X2, R1 and R2 have the meanings as defined herein. | 03-10-2011 |
| 20110077402 | ADMINISTRATION OF DIPEPTIDYL PEPTIDASE INHIBITORS - Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions. | 03-31-2011 |
| 20110184173 | Pyripyropene Derivatives Having An ACAT2-Inhibiting Activity - The present invention is a compound having the general formula (I), (II), or (III) or a pharmacologically acceptable salt, solvate, or hydrate thereof, and a pharmaceutical composition containing such a compound, or its pharmacologically acceptable ester, or other pharmacologically acceptable derivative thereof as an active ingredient. The compound has an excellent ACAT 2-inhibiting activity by a mechanism different from that of a statin drug and is useful as a therapeutic or prophylactic agent for obesity, adiposis, hyperlipidemia, hypercholesterolemia, disorder of lipid metabolism, and arteriosclerosis, as well as obesity-derived hyperlipidemia, hypercholesterolemia, disorder of lipid metabolism, arteriosclerosis, and hypertension. | 07-28-2011 |
| 20130079518 | REGIOSELECTIVE PREPARATION OF SUBSTITUTED PYRIMIDINES - The present invention relates to a method of making pyrimidines of formula (III) wherein X1, X2, R1 and R2 have the meanings as defined herein. | 03-28-2013 |
| 20130261301 | Fungicide - The invention relates to fungicides and can be used for treating diseases caused by fungi, and also for preventing damage to various materials and agricultural products by fungi. The fungicide is a 2,4-dioxo-5-(2-hydroxy-3,5-dichlorobenzylidiene)amino-1,3-pyrimidine salt of general formula: (A) or a dimer thereof: (B), where X is selected from the series consisting of: Na | 10-03-2013 |
| 20160060252 | 5-METHYLURIDINE METHOD FOR PRODUCING FESTINAVIR - The NRTI compound festinavir is made using 5-methyluridine as a starting material, followed by Claisen rearrangement. | 03-03-2016 |
| 20160130260 | TERT-BUTYL SULPHOXIDE METHOD FOR PRODUCING FESTINAVIR - Tert-butyl sulphoxide method for producing festinavir is set forth. | 05-12-2016 |
| 544311000 | Nitrogen attached directly or indirectly to the diazine ring by nonionic bonding | 20 |
| 20090137803 | 5-PROTECTED AMINOPYRIMIDINE COMPOUND, PRODUCTION METHOD THEREOF AND INTERMEDIATE THEREFOR - The present invention provides a production method of 5-aminopyrimidine compound represented by the formula (5) by reacting a glycine compound represented by the formula (1) with t-butoxybisdimethylaminomethane, dimethylformamidedimethylacetal or dimethylformamidediethylacetal to produce a dialkylaminomethylene compound represented by the formula (2), reacting the compound of formula (2) in the presence of an acid to produce a hydroxymethylene compound represented by the formula (3), and reacting the compound of formula (3) with an amidine compound represented by the formula (4) or a salt thereof. | 05-28-2009 |
| 20090171084 | PRODUCTION METHOD OF AMINOPYRIMIDINE COMPOUND - Aminopyrimidine compounds represented by formula (3) may be efficiently prepared by reacting an azlactone compound represented by formula (1) with an amidine compound represented by formula (2) or a salt thereof: | 07-02-2009 |
| 20100222586 | Methods for Producing Sulfonic Acid Diamides - The present invention relates to a process for preparing sulfuric diamides of the general formula I | 09-02-2010 |
| 20110009631 | Phenethanolamine Derivatives for Treatment of Respiratory Diseases - Compounds of the formula (II) and (IV) are provided, which may be employed as intermediates for making compounds useful in treating respiratory diseases. | 01-13-2011 |
| 20110098472 | PROCESSES FOR THE PREPARATION OF URACIL DERIVATIVES - The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof. | 04-28-2011 |
| 20130261302 | Agent for Inducing Endogenous Interferon - The invention relates to medicine and can be used for treating a range of diseases in the treatment of which interferon is used. The agent for inducing endogenous interferon is comprised of the compound 6-(3-methoxycarbonyl phenyl) amino-2,4 (1H, 3H)-pyrimidinedione C | 10-03-2013 |
| 20150018553 | PROCESSES FOR THE PREPARATION OF URACIL DERIVATIVES - The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof. | 01-15-2015 |
| 544312000 | 5-position is unsubstituted or alkyl substituted only | 13 |
| 20080293941 | Method For Production Of 1-Alkyl-3-Phenyluracils - The present invention relates to a process for preparing 1-alkyl-3-phenyluracils of the formula I | 11-27-2008 |
| 20090156812 | PREPARATIONS CONTAINING AMINO ACIDS AND OROTIC ACID - The present invention describes compounds produced from an orotic acid molecule and an amino acid molecule. The compounds being in the form of amino acid orotate compounds bound by an amide linkage and produced by one of two disclosed methods; 1) reacting orotic acid or derivatives thereof with a thionyl halide, and then combining the acyl halide with an amino acid in the presence of dichloromethane and a DMAP catalyst; or 2) protecting the carboxylic acid of an amino acid and then combining the amino acid with a DCC activated orotic acid, followed by removal of the carboxylic acid protecting group. The resulting amino acid orotate amide has an enhanced stability in solution as compared to a related ester. In addition, specific benefits are conferred by the particular amino acid used to form the compounds in addition to, and separate from, the orotate substituent. | 06-18-2009 |
| 20090306379 | POLYMORPHS OF BENZOATE SALT OF 2-[[6-[(3r)-3-AMINO-1- PIPERIDINYL]-3,4-DIHYDRO-3- METHYL-2,4-DIOXO-1(2H)-PYRIMIDINYL]METHYL]-BENZONITRILE AND METHODS OF USE THEREFORE - Compositions comprising Compound I, wherein the Compound I is present in one or more polymorphic forms. Also provided are kits and articles of manufacture with compositions comprising one or more polymorphs of Compound I, and methods of using the compositions to treat various diseases. | 12-10-2009 |
| 20110112293 | Purification Strategy for Direct Nucleophilic Procedures - The present invention provides novel and advantageous processes for preparing and purifying chemical compounds such as pharmaceuticals. The processes comprise a nucleophilic substitution reaction with a moiety X wherein the leaving group L of a substrate S in the reaction is covalently attached to a purification moiety M. This concept offers a convenient and lime-saving way to purity the desired product S-X from non-reacted precursors S-L-M and by-products L-M. | 05-12-2011 |
| 20110152522 | METHOD FOR THE PRODUCTION OF 3-PHENYL(THIO) URACILS AND DITHIOURACILS - The present invention relates to a process for preparing 3-phenyl(thio)uracils and -dithiouracils of the formula I | 06-23-2011 |
| 20110306764 | CRYSTALLINE FORM OF AN ORGANIC COMPOUND - The present invention is directed to a crystalline form of 2-[6-[3(R)-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-ylmethyl]-benzonitrile, a process for the preparation of said crystalline form and the use thereof in the manufacture of a pharmaceutical composition. | 12-15-2011 |
| 20120022257 | PROCESSES FOR PREPARING HIV REVERSE TRANSCRIPTASE INHIBITORS - Disclosed is a method for preparing HIV reverse transcriptase inhibitors which inhibit replication of HIV in HIV infected cells, and novel intermediate compounds used therein. | 01-26-2012 |
| 20120197017 | Pharmaceutical compositions containing paclitaxel orotate - This invention is related to orotic acid compounds of taxane cytotoxic agents and in particular to the conversion of the taxanes to their orotate esters. More particularly the pharmaceutical compositions of paclitaxel orotate and docetaxel orotate provide a strategy to minimize body weight loss during primary chemotherapy and improve patient outcomes and quality of life. | 08-02-2012 |
| 20120197018 | POLYMORPHS OF SUCCINATE SALT OF 2-[6-(3-AMINO-PIPERIDIN-1-YL)-3-METHYL-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN- -1-YLMETHY]-4-FLUOR-BENZONITRILE AND METHODS OF USE THEREFOR - Compositions comprising the succinate salt of 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile (referred to herein as Compound I) which has the formula: | 08-02-2012 |
| 20120226040 | METHODS FOR THE SYNTHESIS OF UNSYMMETRICAL CYCLOAKYL SUBSTITUTED XANTHINES - The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A | 09-06-2012 |
| 20130203991 | Pyrimidine Sulphonamide Derivatives as Chemokine Receptor Modulators - A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders. | 08-08-2013 |
| 20140066623 | Ribosome Structure and Protein Synthesis Inhibitors - The invention provides methods for producing high resolution crystals of ribosomes and ribosomal subunits as well as crystals produced by such methods. The invention also provides high resolution structures of ribosomal subunits either alone or in combination with protein synthesis inhibitors. The invention provides methods for identifying ribosome-related ligands and methods for designing ligands with specific ribosome-binding properties as well as ligands that may act as protein synthesis inhibitors. Thus, the methods and compositions of the invention may be used to produce ligands that are designed to specifically kill or inhibit the growth of any target organism. | 03-06-2014 |
| 20150360215 | PHOSPHINE LIGANDS FOR CATALYTIC REACTIONS - The disclosure is directed to: (a) phosphacycle ligands; (b) catalyst compositions comprising phosphacycle ligands; and (c) methods of using such phosphacycle ligands and catalyst compositions in bond forming reactions. | 12-17-2015 |
| 544314000 | Additional chalcogen attached directly or indirectly to the diazine ring by nonionic bonding | 3 |
| 20110060142 | Novel compositions and processes for preparing 5-amino or substituted amino 1,2,3-triazoles and triazole orotate formulations - New polymorphs of 5-amino or substituted amino 1,2,3-triazole and substituted derivatives thereof, of orotates of the carboxyamidotriazoles, of formulations of the triazoles and orotic acid in the ratio of 1:1 to 1:4 (base:acid) and of safer processes of the preparation of the same are disclosed. The compounds are useful in the control and treatment of diseases including, but not limited to solid cancers, macular degeneration, retinopathy, chronic myeloid leukemia, AIDS and diseases which rely on aberrant signal transduction. The improved processes to prepare the orotate formulations use stable, efficient and safer starting azide intermediate materials in the synthesis of new polymorphs of carboxyamidotriazole. | 03-10-2011 |
| 20120029193 | POLYMERIZABLE MONOMERS - A monomer of formula (1) is provided wherein R | 02-02-2012 |
| 20130225815 | Fluoroalkylation Methods And Reagents - A method of forming a fluorinated molecular entity includes reacting in a reaction mixture an aromatic halide, copper, a fluoroalkyl group, and a ligand. The aromatic halide includes an aromatic group and a halogen substituent bonded to the aromatic group. The ligand includes at least one group-V donor selected from phosphorus and an amine. The overall molar ratio of copper to aromatic halide in the reaction mixture is from 0.2 to 3. The method further includes forming a fluoroalkylarene including the aromatic group and the fluoroalkyl group bonded to the aromatic group. A composition, which may be used in the method, consists essentially of copper, the fluoroalkyl group, and the ligand, where the molar ratio of copper to the fluoroalkyl group is approximately 1. | 08-29-2013 |
