Class / Patent application number | Description | Number of patent applications / Date published |
548531000 | The -C(=X)- is part of a -C(=X)X- group, wherein the X's are the same or diverse chalcogens (e.g., pyrrole-3-carboxylic acid, etc.) | 41 |
20080207921 | Organic Compounds - The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula III, | 08-28-2008 |
20090137819 | Method of Producing Optically Active 4-Amino-3-Substituted Phenylbutanoic Acid - The present invention provides a method of producing a compound (IIa) or a compound (IIb), provides a method of producing a compound (IIIa) or a compound (IIIb), provides a method of producing a compound (Va) or its salt or a compound (Vb) or its salt, provides a method of producing a compound (IIIa) or a compound (IIIb), further, provides a method of producing a compound (Va) or its salt or a compound (Vb) or its salt including these production methods. | 05-28-2009 |
20090281332 | PROCESS FOR PRODUCING ESTER OR ALCOHOL - Provided is a process for producing an ester or alcohol using a fluoroimidinium sulfonate derivative represented by the general formula (9) or a fluoroimidinium carboxylate derivative represented by the general formula (6) and using as a raw material alcohol involving inversion of steric configuration. Further provided are a fluoroimidinium sulfonate derivative represented by the general formula (9), and a process for producing the same. | 11-12-2009 |
20090312560 | PROCESSES FOR MAKING PREGABALIN AND INTERMEDIATES THEREFOR - Processes for making a diester compound of formula (B) and for converting it to pregabalin, especially via a compound of formula (2), can provide several advantages. | 12-17-2009 |
20090326246 | Method for Production of Optically Active 3-Amino-Nitrogenated Compound - Aiming at production of an optically active 3-amino nitrogen-containing compound which is useful as an intermediate in synthesis of medicines and pesticides, in particular, an optically active 1-protected-3-aminopyrrolidine derivative, from an inexpensive and readily available raw material by a process which is efficient and can be practiced industrially, an optically active 3-amino nitrogen-containing compound is produced by performing a reaction of an optically active 3-substituted nitrogen-containing compound with ammonia, methylamine, ethylamine or dimethylamine in the presence of water. In addition, a 1-protected-3-aminopyrrolidine derivative is produced by performing a reaction of an optically active 1-protected-3-(sulfonyloxy)pyrrolidine derivative with ammonia, methylamine, ethylamine, or dimethylamine in the presence of methanol, ethanol, n-propanol, or isopropanol under a pressure of less than 30 barr. | 12-31-2009 |
20100076203 | Succinic acid diester derivative, process for production thereof, and use of the derivative in the production of pharmaceutical preparation - The present invention provides with a process of preparing an optically active succinimide derivative, which is a key intermediate for production of ranirestat. A compound (3) is easily prepared by treating the derivative of succinic acid diester of the formula (2): | 03-25-2010 |
20100152462 | PROCESS FOR THE PREPARATION OF PYROLLIDINE-3-CARBOXYLIC ACIDS - The invention relates to a novel process for the preparation of (3S,4S)- or (3R,4R)-1-benzyl-4-(halogen-aryl)-pyrrolidine-3-carboxylic acids of formula I | 06-17-2010 |
20110144354 | Process for Preparation of Darifenacin and Intermediates Used in the Process - Disclosed herein is a process for the preparation of darifenacin and physiologically acceptable salts thereof. Also disclosed is a compound of formula X: wherein R is linear or branched C | 06-16-2011 |
20110190511 | Methods For Preparing Fluoroalkyl Arylsulfinyl Compounds And Fluorinated Compounds Thereto - Novel preparative methods for fluoroalkyl arylsulfinyl compounds are disclosed. Fluorinated compounds as useful fluorinated compounds, intermediates, or builing blocks are disclosed. Useful applications of the fluoroalkyl arylsulfinyl compounds are shown. | 08-04-2011 |
20110224444 | PROCESS FOR PRODUCTION OF ARALKYLOXYPYRROLIDINE DERIVATIVE - The present invention provides a process for producing a 3-aralkyloxypyrrolidine derivative which is important for production of pharmaceutical products and the like. In the present invention, a N-protected-3-hydroxypyrrolidine is converted into a N-protected-3-aralkyloxypyrrolidine by allowing an aralkyl halide to act in the presence of a base and at least one of a metal halide and a phase-transfer catalyst followed by deprotecting a N-protecting group to convert it to a 3-aralkyloxypyrrolidine derivative and subsequently treating the derivative in a solvent containing a polar solvent, thereby obtaining the 3-aralkyloxypyrrolidine derivative as a crystal. According to the present invention, a 3-aralkyloxypyrrolidine derivative of high purity can be produced conveniently and efficiently on an industrial scale. | 09-15-2011 |
20110245508 | Processes For Making Pregabalin And Intermediates Therefor - Processes for making a diester compound of formula (B) and for converting it to pregabalin, especially via a compound of formula (2), can provide several advantages. | 10-06-2011 |
20120022271 | NOVEL METHOD FOR PRODUCING OPTICALLY ACTIVE PYRROLIDINE COMPOUND | 01-26-2012 |
20120283448 | METHOD FOR PRODUCING 3,4-DISUBSTITUTED PYRROLIDINE DERIVATIVE AND PRODUCTION INTERMEDIATE THEREOF - Provided is an inexpensive and industrially advantageous method for preparing (3R,4S)-3-(N-substituted aminomethyl)-4-fluoropyrrolidine or an enantiomer thereof which can be an intermediate for producing pharmaceuticals. It relates to a method for preparing (3R,4S)-3-(N-substituted cyclopropylaminomethyl)-4-fluoropyrrolidine derivative or ait's enantiomer, or their salts, comprising a step of fluorinating a 4-hydroxy-3-(N-substituted aminomethyl)pyrrolidine derivative represented by the general formula (1) or an enantiomer thereof using a sulfur tetrafluoride derivative. | 11-08-2012 |
20130158275 | NEW PROCESS FOR THE PREPARATION OF INTERMEDIATES USEFUL FOR THE MANUFACTURE NEP INHIBITORS - The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising -amino- -biphenyl- -methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof. | 06-20-2013 |
20130217892 | Use Of N-Substituted 2-Pyrrolidone-4-Carboxylic Acid Esters And Solvents - The invention relates to the use of one or more N-substituted 2-pyrrolidone-4-carbonic acid esters of formula (1), where R1 and R2 independently represent linear, branched, or cyclic C1-C6 alkyl, as (a) solvent(s). Said compounds can be used as solvents in industrial applications, e.g. for the production of varnishes and paints, in chemical syntheses, for cleaning or degreasing, in petrochemical processes, in the electronics and photovoltaic industries, or in pesticide preparations, for example. | 08-22-2013 |
548532000 | And is bonded directly to a ring carbon which is adjacent to the ring nitrogen of the five-membered hetero ring (e.g., 4-hydroxy proline, etc.) | 21 |
20080312456 | PROCESS FOR THE SYNTHESIS OF PEPTIDES CONTAINING A 4-HYDROXY-PROLINE SUBSTRUCTURE - The present invention relates to processes for preparing peptides and to intermediates involved in such processes, e.g. a process for preparing a compound of formula VIII | 12-18-2008 |
20090306407 | Pyrrolidine analogue for preventing neurogenic pain and method for production thereof | 12-10-2009 |
20100152463 | Methods for Preparing Fluoroalkyl Arylsulfinyl Compounds and Fluorinated Compounds Thereto - Novel preparative methods for fluoroalkyl arylsulfinyl compounds are disclosed. Fluorinated compounds as useful fluorinated compounds, intermediates, or building blocks are disclosed. Useful applications of the fluoroalkyl arylsulfinyl compounds are shown. | 06-17-2010 |
20100222599 | PROCESSES FOR THE PREPARATION OF SGLT2 INHIBITORS - Provided are processes for the preparation of complexes that are useful in purifying compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The processes can reduce the number of steps needed to obtain the target compounds and the complexes formed in the processes are typically provided in a crystalline form. | 09-02-2010 |
20110015408 | SULFONYLPYRROLIDINE MODULATORS OF ANDROGEN RECEPTOR FUNCTION AND METHOD - Compounds are provided which are useful in the treatment of androgen receptor-associated conditions, such as age-related diseases, which compounds have the structure | 01-20-2011 |
20110166365 | Collagen peptide, dipeptide and malady inhibitor - A problem that the present invention is to solve is to provide: a main body of a peptide molecule which is effective for inhibition of various maladies such as osteoporosis, osteoarthritis and pressure ulcer, particularly, a dipeptide which is easy to absorb into a body in an intestine; a collagen peptide which comprises the dipeptide as an essential dipeptide; and a malady inhibitor which comprises the dipeptide as an essential effective component. As a means of solving such a problem, a collagen peptide according to the present invention is characterized by comprising a dipeptide having a structure of Hyp-Gly as an essential dipeptide. A dipeptide according to the present invention is characterized by having a structure of Hyp-Gly. A malady inhibitor according to the present invention is characterized by comprising a dipeptide having a structure of Hyp-Gly as an essential effective component. | 07-07-2011 |
548533000 | Additional -C(=X) bonded directly to the five-membered hetero ring (e.g., N n-butyryl-L-proline, etc.) | 11 |
20080255369 | Synthesis of Renin Inhibitors Involving a Cycloaddition Reaction - The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula III, | 10-16-2008 |
20100145071 | SMALL MOLECULE INHIBITORS OF ROTAMASE ENZYME ACTIVITY - This invention relates to neurotrophic compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity. | 06-10-2010 |
20100174096 | Methods for Production of Optically Active Fluoropyrrolidine Derivatives - Useful industrial methods for producing optically active fluoropyrrolidine derivatives as useful fluorinated intermediates are disclosed. | 07-08-2010 |
20100228037 | Process for Preparing Allylmercaptocaptopril (Cpssa) and Related Asymmetrical Disulfides - A novel process of preparing allyl-containing asymmetric disulfides, and particularly therapeutically active allyl-containing asymmetric disulfides such as allylmercaptocaptopril (CPSSA) is disclosed. | 09-09-2010 |
20110028736 | Zofenopril Calcium - The present invention relates to zofenopril calcium form A substantially free of other forms of zofenopril calcium and to zofenopril calcium having a chemical purity of more than 98.5%. The present invention also relates to methods of preparing such zofenopril calcium. It further relates to compositions comprising such zofenopril calcium. Zofenopril calcium, (4S)-1-[(2S)-3-benzoylthio-2-methylpropionyl]-4-(phenylthio)-L-proline calcium salt, has the following structure: | 02-03-2011 |
20110077412 | Process for separating the diastereomers of RSS-snd SSS-N- a [1-carboxy -3-Phenylpropyl] lysylproline - A process for separating the diastereomers of RSS— and SSS—N-α[1-carboxy-3-phenylpropyl]lysylproline is described. Previous chromatographic processes for separating the diastereomers of this peptide active substance, such as for example adsorption chromatography, exhibited disadvantages with regard to the solvents used and throughput. These disadvantages do not occur if basic ion exchangers are used in the chromatographic separation of the diastereomers. In particular, purely aqueous solutions may be used as the eluent. | 03-31-2011 |
20110124881 | PROCESS OF FORMING A PYRROLE COMPOUND - Disclosed is a process of forming a pyrrole compound. The process comprises contacting an α-carbonyl oxime compound 1 | 05-26-2011 |
20110201825 | Method for Producing Fluorosulfuric Acid Ester - Fluorosulfuric acid esters can be produced by reacting alcohols with sulfuryl fluoride (SO | 08-18-2011 |
20110251403 | Method for Manufacturing Hydroxyl Group Substitution Product - In the present invention, a hydroxyl group substitution product is manufactured by reaction of an alcohol with sulfuryl fluoride (SO | 10-13-2011 |
20140163241 | NOVEL CRYSTALLINE FORMS - The present invention relates to two novel crystalline forms of zofenopril calcium, to processes for their preparation and their use in pharmaceutical compositions. | 06-12-2014 |
20160145208 | Preparation method for pyrrolidine-2-carboxylic acid derivatives - The present invention relates to the field of medical synthesis, in particular to a preparation method for pyrrolidine-2-carboxylic acid derivatives. The present invention adopts the following technical solution: providing a compound having a structure of formula (E), wherein R is R | 05-26-2016 |
548534000 | Chalcogen bonded directly to the other ring carbon which is adjacent to the ring nitrogen of the five-membered hetero ring (e.g., 2-pyrrolidone-5 carboxylic acid, etc.) | 1 |
20100331552 | ACID SALT OF TOLTERODINE HAVING EFFECTIVE STABILITY FOR TRANSDERMAL DRUG DELIVERY SYSTEM - The present invention relates to an acid salt of tolterodine with superior stabililty and useful as a transdermal drug delivery system. More specifically, the present invention relates to a novel acid salt of tolterodine with superior stabililty to the conventional acid salts of tolterodine, which is useful as a pharmaceutical composition for the treatment of overactive bladder and can be formulated into a transdermal drug delivery system. | 12-30-2010 |
548535000 | The five-membered hetero ring is further unsubstituted or alkyl substituted only (e.g., proline, etc.) | 3 |
20120142941 | COMPOSITION FOR ALLEVIATING ULTRAVIOLET RADIATION-INDUCED DAMAGE - Disclosed are: a composition for alleviating ultraviolet irradiation-induced damage, which can be used on a daily based and is stable and safe; and a pharmaceutical preparation, a cosmetic and a food composition, each of which comprises the composition. The composition for alleviating ultraviolet irradiation-induced damage contains one or more compounds selected from the group consisting of D-glutamic acid, L-glutamic acid, D-proline, D-cystine, L-cystine, and derivatives and/or salts of the aforementioned compounds. The composition can be used as an external formulation for the skin, a cosmetic composition, an anti-wrinkle agent, a sunscreen agent, a pharmaceutical composition for treating and/or preventing skin diseases, a food composition, or a pharmaceutical composition for preventing or treating cataract. | 06-07-2012 |
20130116446 | FUNCTIONALIZED NON-PHENOLIC AMINO ACIDS AND ABSORBABLE POLYMERS THEREFROM - The present invention relates to compound of formula I, which are functionalized, non-phenolic amino acids, and polymers formed from the same. | 05-09-2013 |
20160152564 | METHOD FOR STEPWISE SEPARATING AMINO ACID ACTIVE INGREDIENTS OF CAMELLIA NITIDISSIMA CHI | 06-02-2016 |
548536000 | Additional -C(=X)- bonded directly to the five-membered hetero ring (e.g., pyrrole-3,4-dicarboxylic acid esters, etc.) | 5 |
20090023935 | Process for Producing 3,4-Disubstituted Pyrrolidine Derivative and Production Intermediate Thereof - An industrially advantageous process for the production of (3R,4S)-3-cyclopropylaminomethyl-4-fluoropyrrolidine or an enantiomer thereof that is useful as an intermediate for the production of novel antimicrobial agents 10-(3-cyclopropylaminomethyl-4-fluoropyrrolidinyl)pyridobenzoxazine carboxylic acid derivatives. | 01-22-2009 |
20110213161 | Preparation of Protected Alpha-Keto Beta-Amino Esters and Amides - The invention provides β-sulfonamide α-keto esters and amides in which the α-keto is protected as a 1,3-dithiolane derivative. Also provided are methods for preparing such esters and amides and for incorporating them into peptides. | 09-01-2011 |
20110275833 | Novel 4-Fluoropyrrolidine-2-Carbonyl Fluoride Compounds and Their Preparative Methods - Novel 4-fluoropyrrolidine-2-carbonyl fluoride compounds as useful fluorinated intermediates are disclosed. Their preparative methods are also disclosed. Useful applications of the 4-fluoropyrrolidine-2-carbonyl fluorides are shown. | 11-10-2011 |
20120220784 | PROCESS FOR REDUCTION OF ALPHA-ACYLOXY SULFIDE DERIVATIVES - The present invention provides an efficient and scalable process to prepare the compound of formula 4 by reduction of the corresponding α-acyloxy sulfides. | 08-30-2012 |
20130217893 | METHOD FOR PRODUCING 3,4-DISUBSTITUTED PYRROLIDINE DERIVATIVE - The present invention provides an inexpensive and industrially advantageous method for producing an optically active form of an anti-(3S,4R)-3-alkylcarbamoyl-4-hydroxypyrrolidine derivative or it's enantiomer, which is a key intermediate for producing a high-quality optically active form of (3R,4S)-3-alkylaminomethyl-4-fluoropyrrolidine or it's enantiomer useful as an intermediate for producing pharmaceuticals. | 08-22-2013 |