Class / Patent application number | Description | Number of patent applications / Date published |
544384000 | Chalcogen bonded directly to piperazine ring carbon | 18 |
20120016125 | METHOD FOR PREPARING DIPEPTIDYL PEPTIDASE-IV INHIBITOR AND INTERMEDIATE - The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention is able to reduce preparation costs by using low cost reagents on reaction and is able to be used in mass production by improving yield. | 01-19-2012 |
20120016126 | METHOD FOR MANUFACTURING DIPEPTIDYL PEPTIDASE-IV INHIBITOR AND INTERMEDIATE - The present invention relates to an improved method for manufacturing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention allows reduction of production costs by reacting low cost reagents, improves yield and is adaptable for mass production. | 01-19-2012 |
20120088915 | STEREOSELECTIVE METHODS, CATALYSTS AND INTERMEDIATES FOR THE SYNTHESIS OF (-)-NUTLIN-3 AND RELATED COMPOUNDS - The present invention provides methods and intermediates are provided for the preparation of (−)-Nutlin-3. Methods and intermediates are also provided for the enantioselective addition of aryl nitromethanes to aldimines. Bis(amidine) catalysts for the use in these and other reactions are also provided. | 04-12-2012 |
20150025241 | METHOD FOR PREPARING DIPEPTIDYL PEPTIDASE-IV INHIBITOR AND INTERMEDIATE - The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention is able to reduce preparation costs by using low cost reagents on reaction and is able to be used in mass production by improving yield. | 01-22-2015 |
544385000 | Plural chalcogens bonded directly to piperazine ring carbons | 14 |
20090043099 | Methods and compositions for derepression of IAP-inhibited caspase - The invention provides isolated agents having novel chemical structures and possessing superior activity as derepressors of IAP inhibited caspase. The invention further provides a method of derepressing an IAP-inhibited caspase. The invention further provides assay methods employing labeled compounds of the invention, especially fluorescent labeled compounds. | 02-12-2009 |
20100087642 | Catalysis of Diketopiperazine Synthesis - Provided is a method for the synthesis of N-protected bis-3,6-[4-aminobutyl]-2,5-diketopiperazine including the step of heating a solution of ε-amino protected lysine in the presence of a catalyst selected from the group consisting of sulfuric acid, phosphoric acid, and phosphorus pentoxide. | 04-08-2010 |
20110144336 | Method for Preparation of Piperazindione Derivatives - A process for preparing piperazinedione derivatives of the formula I | 06-16-2011 |
20120178935 | Catalysis of Diketopiperazine Synthesis - Provided is a method for the synthesis of N-protected bis-3,6-[4-aminobutyl]-2,5-diketopiperazine including the step of heating a solution of ε-amino protected lysine in the presence of a catalyst selected from the group consisting of sulfuric acid, phosphoric acid, and phosphorus pentoxide. | 07-12-2012 |
20130012710 | Formation of N-Protected bis-3,6-(4-aminoalkyl)-2,5,diketopiperazine - The disclosed embodiments detail improved methods for the synthesis of diketopiperazines from amino acids. In particular improved methods for the cyclocondensation and purification of N-protected 3,6-(aminoalkyl)-2,5-diketopiperazines from N-protected amino acids. Disclosed embodiments describe methods for the synthesis of 3,6-bis-[N-protected aminoalkyl]-2,5-diketopiperazine comprising heating a mixture of an amino acid in the presence of a catalyst in an organic solvent. The catalyst is selected from the group comprising sulfuric acid, phosphoric acid, p-toluenesulfonic acid, 1-propylphosphonic acid cyclic anhydride, tributyl phosphate, phenyl phosphonic acid and phosphorous pentoxide among others. The solvent is selected from the group comprising: dimethylacetamide, N-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme, ethyldiglyme, m-cresol, p-cresol, o-cresol, xylenes, ethylene glycol and phenol among others. | 01-10-2013 |
20130072684 | TREATMENT OF T-CELL MEDIATED DISEASES - The invention provides a method of treating T-cell mediated diseases and a method of inhibiting the activation of T-cells using certain diketopiperazines. The invention also provides methods of synthesizing diketopiperazines and pharmaceutical compositions comprising certain diketopiperazines. The invention further provides methods of making improved pharmaceutical compositions of proteins and peptides by either increasing or decreasing the content of diketopiperazines in the compositions and the resultant improved pharmaceutical compositions. | 03-21-2013 |
20130289278 | Methods for the synthesis of activated ethylfumarates and their use as intermediates - Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphosphoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput. | 10-31-2013 |
20130296566 | REACTOR FOR PRODUCING PHARMACEUTICAL PARTICLES IN A PRECIPITATION PROCESS - Reactors, reactor systems and methods for producing particles in a precipitation process are provided. The reactor includes a housing defining a reaction chamber, a stator assembly including two or more stators, a rotor assembly including two or more rotors, the rotor assembly configured for rotation about an axis of rotation relative to the stator assembly, a first inlet to supply a first reactant material to the reaction chamber at a first radial location, a second inlet to supply a second reactant material to the reaction chamber at a second radial location different from the first radial location, wherein the first and second reactant materials react to produce precipitation of particles in the reaction chamber, and an outlet to supply the particles formed in the reaction chamber. | 11-07-2013 |
20140243530 | Catalysis of Diketopiperazine Synthesis - Provided is a method for the synthesis of N-protected bis-3,6-[4-aminobutyl]-2,5-diketopiperazine including the step of heating a solution of ε-amino protected lysine in the presence of a catalyst selected from the group consisting of sulfuric acid, phosphoric acid, and phosphorus pentoxide. | 08-28-2014 |
20150073149 | Formation of N-Protected bis-3,6-(4-aminoalkyl)-2,5,diketopiperazine - The disclosed embodiments detail improved methods for the synthesis of diketopiperazines from amino acids. In particular improved methods for the cyclocondensation and purification of N-protected 3,6-(aminoalkyl)-2,5-diketopiperazines from N-protected amino acids. Disclosed embodiments describe methods for the synthesis of 3,6-bis-[N-protected aminoalkyl]-2,5-diketopiperazine comprising heating a mixture of an amino acid in the presence of a catalyst in an organic solvent. The catalyst is selected from the group comprising sulfuric acid, phosphoric acid, p-toluenesulfonic acid, 1-propylphosphonic acid cyclic anhydride, tributyl phosphate, phenyl phosphonic acid and phosphorous pentoxide among others. The solvent is selected from the group comprising: dimethylacetamide, N-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme, ethyldiglyme, m-cresol, p-cresol, o-cresol, xylenes, ethylene glycol and phenol among others. | 03-12-2015 |
20150297584 | LEARNING AND MEMORY IMPROVER - The present invention aims to provide antidementia agents which are free from the problem of side effects and are excellent in safety. The present invention also aims to provide agents for improving learning and memory which are useful for improvement of learning and memory and can be ingested continuously. The present invention provides antidementia agents and agents for improving learning and memory, each comprising a cyclic dipeptide with the 2,5-diketopiperazine structure as an active ingredient. | 10-22-2015 |
20160130218 | 4-BENZYL-1-PHENETHYL-PIPERAZINE-2,6-DIONE PREPARATION METHOD, AND INTERMEDIATE AND PREPARATION METHOD THEREOF - The present invention provides a key new intermediate (a compound of formula III) of 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound), a pharmaceutically acceptable salt thereof and a preparation method thereof. The present invention additionally discloses a method for preparing 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound) from the formula III compound, said method overcoming the shortcomings of current formula IV compound preparation methods, such as low production volumes, low purity, high energy consumption, high costs, and inability to achieve industrialized production, and provides a formula IV compound preparation method which is simple, economical, environmentally-friendly and easy to produce industrially; the reaction solvent of the method is easily recycled and the method can produce the formula IV compound at high production rates and with high purity. | 05-12-2016 |
20160145224 | PROCESS FOR THE PREPARATION OF AN ANTIDEPRESSANT AND THE INTERMEDIATES THEREOF - The present invention relates to a process for the preparation of 1-[2-(2,4-dimethylphenylsulphanyl)phenyl]piperazine of formula (I), also known as vortioxetine, salts thereof, and intermediates useful for its synthesis. | 05-26-2016 |
20160159753 | Methods for the synthesis of activated ethylfumarates and their use as intermediates - Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphophoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput. | 06-09-2016 |