| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 548302700 | Bicyclo ring system having the diazole ring as one of the cyclos | 81 |
| 20090069570 | Novel Process for Producing Ramosetron or Its Salt - [Problems] To provide a novel process for producing ramosetron or its salt that is useful as a pharmaceutical, especially as a therapeutic and/or preventive agent for digestive symptoms caused by administration of an anti-malignant tumor agent, diarrheal-type irritable bowel syndrome, diarrheal symptoms of irritable bowel syndrome, etc.
| 03-12-2009 |
| 20100174092 | NOVEL 5 SUBSTITUTED HYDANTOINS - The present invention relates to 5-substituted hydantoins, a process for the preparation of 5-substituted hydantoins and the use of 5-substituted hydantoins in the preparation of enantiomerically enriched α-amino acids. Furthermore, the present invention relates to the preparation of pharmaceutically active products such as perindopril and ramipril using the novel 5-substituted hydantoins. | 07-08-2010 |
| 20110112303 | Process - A process for preparing the S or R enantiomer of a compound of formula A, | 05-12-2011 |
| 20120077985 | PROCESS FOR PRODUCING FUSED IMIDAZOLE COMPOUND, REFORMATSKY REAGENT IN STABLE FORM, AND PROCESS FOR PRODUCING THE SAME - The present invention provides an industrially advantageous process for producing a steroid C | 03-29-2012 |
| 20130123509 | PROCESS FOR THE PREPARATION OF DIMIRACETAM - The invention relates to a method of manufacture of dimiracetam (2,5-dioxohexahydro-1 H-pyrrolo[1,2-a]imidazole), characterized in that a 4-oxo-butanoic acid ester is condensed with glycinamide in a one-pot reaction with a controlled pH. The reaction may be performed in aqueous solution or in an anhydrous lower alcohol solution. | 05-16-2013 |
| 20140100373 | PRODUCTION METHOD OF IMIDAZOLE DERIVATIVES - The present invention provides an advantageous production method of an imidazole derivative, which is suitable for industrial production. | 04-10-2014 |
| 548303100 | At least three ring hetero atoms in the bicyclo ring system (e.g., furo- imidazole, (1,2-a) imidazole, pyrazo (1,2-a) imidazolidine, etc.) | 12 |
| 20090043106 | Manufacture of Lactones - The present invention relates to a process for the manufacture of cyclic monocarboxylic esters (lactones) and related compounds by hydrogenation of cyclic dicarboxylic acid anhydrides in the presence of metal catalysts. | 02-12-2009 |
| 20140206886 | Enantioselective N-heterocyclic carbene-catalyzed annulation reactions with imidazolidinones - Enantiomeric bicyclic lactone compounds as can be prepared via an N-heterocyclic carbene-catalyzed annulation reaction. | 07-24-2014 |
| 548303400 | Four ring nitrogens in the bicyclo ring system (e.g., glycolurile, etc.) | 5 |
| 20100016610 | FRICTIONLESS MOLECULAR ROTARY MOTORS - A rotaxane consisting of a cucurbituril and an uncharged guest molecule, having low or null affinity therebetween is provided as well as processes for providing the same. Various uses as energy converters (“frictionless” molecular motors), biochips and biosensors using the same are also provided. | 01-21-2010 |
| 20130012721 | METHODS FOR THE PURIFICATION OF CUCURBITURIL - A method for purifying a cucurbituril from a mixture. The method includes the step of forming a complex between the cucurbituril and a cucurbituril guest. The complex has altered physical and/or chemical properties to the cucurbituril which allow the complex to be separated from at least one other component of the mixture. The mixture includes the cucurbituril, the other component and a solvent. | 01-10-2013 |
| 20140371466 | PATTERN-FORMING METHOD, AND COMPOSITION FOR FORMING RESIST UNDERLAYER FILM - Providing a method for forming a pattern capable of forming a resist underlayer film that can be easily removed using an alkali liquid while maintaining etching resistance is objected to. Provided by the present invention is a method for forming a pattern, the method including: (1) forming a resist underlayer film on a substrate using a composition for forming a resist underlayer film containing a compound having an alkali-cleavable functional group; (2) forming a resist pattern on the resist underlayer film; (3) forming a pattern on the substrate by dry etching of the resist underlayer film and the substrate, using the resist pattern as a mask; and (4) removing the resist underlayer film with an alkali liquid. | 12-18-2014 |
| 20160090388 | PROCESS FOR THE PRODUCTION OF SPEHERICAL TETRANITROGLYCOURIL - A spherical morphology of the high explosive tetranitroglycoluril (TNGU) has been discovered. This new morphology exhibits approximately a twofold improvement in the response of the material to impact, more than a one and a half fold improvement in friction and the same high resistance to electrostatic discharge over non-spherical TNGU produced by other methods. | 03-31-2016 |
| 20160176878 | NOVEL PREPARATION OF TETRANITROGLYCOLURIL | 06-23-2016 |
| 548303700 | The other cyclo is a five-membered hetero ring having one sulfur and four carbons (e.g., cis-tetrahydro-2-oxothieno [3,4-d]-imidazoline 4-valeric acid or biotin, etc.) | 5 |
| 20100160645 | POLY(ETHYLENE GLYCOL) CONTAINING CHEMICALLY DISPARATE ENDGROUPS - The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof. | 06-24-2010 |
| 20120065406 | Improved Preparation Method for D-Biotin - The invention discloses the improved preparation method for D-Biotin. If the composite method takes the malonic acid diester as the raw material, the finial biotin will be generated with impurities. The features of the invention refers to the improved preparation method for D-Biotin includes: firstly, (3aS,4S,6aR)-1,3-dibenzyl-4-(ω,ω,ω-3 -alkoxycarbonyl bytyl)-4H-1H-thiophene[3,4-d]iminazole-2,4(1H)-ketone is got after the methane tricarboxylic acid trialkyl ester and (3aR,8aS,8bS)-1,3-dibenzyl-2-oxo-10H-iminazole[3,4-d]thiophene[1,2-a]sulfuryl halide have the condensation reaction in the alkaline environment and then D-Biotin can be got after the reaction process of hydrolysis, decarboxylation and closed loop. The invention succeeds in greatly improving the biotin quality from the original basis and simultaneously avoids the generation of impurities and the occurrence of side reaction. | 03-15-2012 |
| 20140249319 | CHEMICAL CROSSLINKERS AND COMPOSITIONS THEREOF - Chemical crosslinkers and methods of their synthesis are disclosed. | 09-04-2014 |
| 20150011777 | METHOD FOR PREPARING D-BIOTIN - Abstract The invention discloses a D-biotin preparation method. In the prior art, with a synthesis method utilizing malonic acid diester as raw materials, impurities are also produced along with the obtained D-biotin. The D-biotin preparation method is characterized in that with the presence of dimethyl sulfoxide and inorganic base as catalysts, methane tricarboxylic acid trialkyl ester and (3aR, 8aS, 8bS)-1,3-dibenzyl-2-oxo-10H-iminazole [3,4-d] thiophene [1,2-a] sulfuryl halide are subjected to condensation reaction in methylbenzene solvent to obtain intermediate (3 aS,4S,6aR)- 1,3 -dibenzyl-4-(ω,ω,ω-3-methoxycarbonylbutyl)-4H- 1H-thiophene[3,4-d]iminazol e-2,4(1H)-ketone, and the D-biotin is obtained after the intermediate is treated by the aftertreatment method. By the D-biotin preparation method, production of the impurities is avoided, quality of the biotin is greatly improved on the existing basis, and side reaction is avoided too. | 01-08-2015 |
| 548304100 | Having -C(=O)-HN-, wherein substitution may be made for H, attached directly or indirectly to the bicyclo ring system by acyclic nonionic bonding (e.g., biotin amide, biotinylglycine, etc.) | 1 |
| 20120330028 | METHOD FOR PREPARING POLYBIOTINYLATED COMPOUNDS - The present invention relates to a novel method for preparing compounds having the formula (I), | 12-27-2012 |
| 548304400 | The other ring is a benzene ring | 63 |
| 20090299074 | BENZO[b]THIOPHEN DERIVATIVES AND PROCESS FOR THEIR PRODUCTION - The invention provides benzo[b]thiophene derivatives useful as production intermediates for chymase inhibitors, and a process for their production. | 12-03-2009 |
| 20100130748 | SNAR PROCESS FOR PREPARING BENZIMIDAZOLE COMPOUNDS - Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-2 and their synthetic intermediates: wherein X | 05-27-2010 |
| 20100145065 | PROCESS FOR PREPARING BENZIMIDAZOLE COMPOUNDS - Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-1 and their synthetic intermediates: wherein Z, X | 06-10-2010 |
| 20100286406 | 1,3- DIALKYLBENZIMIDAZOLE HALOGENIDES EXHIBITING REGENERATIVE, ANTI-INFLAMMATORY, AND ANTIMICROBIAL ACTIVITY - The invention relates to medicine, veterinary, and cosmetology, in particular, to medications used to accelerate tissue regeneration processes, particularly in the presence of inflammatory processes attended by infection with pathogenic microflora, and may be used in pharmaceutics and cosmetology. | 11-11-2010 |
| 20110319631 | PROCESS FOR PREPARING BENZIMIDAZOLE COMPOUNDS - Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ib-1: | 12-29-2011 |
| 20110319632 | PROCESS FOR PREPARING BENZIMIDAZOLE COMPOUNDS - Provided are compounds having Formula VIIIa-1: | 12-29-2011 |
| 20120253049 | NOVEL HYDROGEN SULFATE SALT - The present invention relates to Compound 1 hydrogen sulfate salt and solvates, crystalline forms and amorphous forms thereof, and to processes for their preparation. | 10-04-2012 |
| 20130245279 | PROCESSES FOR PREPARING BENZIMIDAZOLE COMPOUNDS - Provided are processes for the preparation of benzimidazole structures having Formula VIIIb-1: | 09-19-2013 |
| 20160159747 | METHOD FOR PREPARATION OF BENZIMIDAZOLE DERIVATIVES - The present invention provides a method for preparing a compound with a benzimidazole structure with an excellent yield using a low-cost starting material, not requiring an additional separation process, or not using a dangerous reagent during the manufacturing process. Furthermore, the present invention also provides an intermediate and a final product produced by the preparing method. | 06-09-2016 |
| 20160168104 | PREPARATION OF AND FORMULATION COMPRISING A MEK INHIBITOR | 06-16-2016 |
| 548304700 | Additional hetero ring attached directly or indirectly to the diazole ring by nonionic bonding (e.g., methyl( 5-[2-(2-thienyl)-1,3-dioxolan -2-yl]-1H-benzimidazol-2-yl) carbamate, etc.) | 20 |
| 20110137045 | BENZIMIDAZOLE DERIVATIVES - Provided herein are compounds in accord with Formula I: | 06-09-2011 |
| 548305100 | The additional hetero ring is a cyclo in a polycyclo ring system (e.g., benzofuranyl-benzimidazole, etc.) | 13 |
| 20110251401 | POLYPHENYLENE HOST COMPOUNDS - Polyphenylene compounds such as compounds represented by Formula I may be used in electronic devices such as organic light-emitting devices. For example, the compounds may be used as host materials in a light-emitting layer. | 10-13-2011 |
| 20140206887 | Light-Emitting Element and Electronic Device - An object is to provide a light-emitting element with high emission efficiency which includes a novel carbazole derivative that has a wide energy gap and can be used for a transport layer or a host material in a light-emitting element. A carbazole derivative in which the 4-position of dibenzothiophene or dibenzofuran is bonded to the 2- or 3-position of carbazole has been able to be provided by use of the carbazole derivative. Further, a light-emitting element having high emission efficiency has been able to be provided by use of the carbazole derivative. | 07-24-2014 |
| 20150329527 | PYRAZOLE LINKED BENZIMIDAZOLE CONJUGATES AND A PROCESS FOR PREPARATION THEREOF - Pyrazole linked benzimidazole conjugates and a method for synthesis of one or more compounds having a pyrazole linked benzimidazole conjugate, particularly pyrazole linked benzimidazole conjugates that are useful as potential antitumor agents against human cancer cell lines, such as leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer. The process comprises the step of oxidative cyclization of o-phenylenediamines and 3-phenyl-1H-pyrazole-5-carbaldehydes with sodium metabisulphite in ethanol/methanol solvent system at a desired temperature for a period of time to obtain the pyrazole linked benzimidazole conjugate. | 11-19-2015 |
| 548305400 | The additional polycyclo ring system contains a 1,3-diazole [e.g., bis (benzimidazol-2-yl) stilene, etc.] | 10 |
| 20090023931 | ALANINE RACEMASE CHIRAL BINAPHTHOL DERIVATIVE WITH POWERFUL HYDROGEN BOND DONOR, AND OPTICAL RESOLUTION AND OPTICAL TRANSFORMATION METHODS USING THE SAME - Disclosed is an alanine racemase chiral binaphthol derivative having the ability to recognize amino alcohols selectively on the basis of chirality and transform amino acids from an L-form into a D-form. Methods for the optical resolution of amino acid or amino alcohol and for the optical transformation of D- and L-forms of amino acids using the binaphthol derivative are also provided. | 01-22-2009 |
| 20090023932 | Process for the Preparation of Telmisartan - The present invention encompasses a method for the preparation of Telmisartan comprises, through Telmisartan dihydrochloride comprises i) Condensing 4-Methyl-2-n-propyl-1H-benzimidazole-6-carboxylic acid with N-Methyl-O-phenylenediamine dihydrochloride to yields 4-methyl-6 (1-methyl benzimidazol-2-yl)-2-n-propyl 1H-benzimidazole ii) Treating 4-methyl-6-(1-methylbenzimidazol-2-yl)-2-n-propyl-1H-benzimidazole with 4′-(bromomethyl)-2-biphenyl-2-carboxylate in presence of a base in an organic solvent and isolating the ester as acid addition salt iii) Converting ester acid addition salt to Telmisartan dihydrochloride and iv) Converting Telmisartan dihydrochloride to Telmisartan. | 01-22-2009 |
| 20090124814 | Process for preparing telmisartan - Provided are processes for preparing telmisartan-alkyl ester and telmisartan using environmentally friendly organic solvents that are easily removed from the reaction mixture, wherein a telmisartan alkyl ester is isolated and hydrolyzed to form telmisartan or the telmisartan is prepared using a synthesis in a single reaction vessel. | 05-14-2009 |
| 20110190508 | PREPARATION OF 1,7'-DIMETHYL-2'-PROPYL-2,5'-BI-1H-BENZIMIDAZOLE - The invention relates to a process for preparing 1,7′-dimethyl-2′-propyl-2,5′-bi-1H-benzimidazole of formula (I) | 08-04-2011 |
| 20130102788 | Method for Synthesizing 1,3,5-Tri-(N-Phenylbenzimidazolyl) Benzene - The present invention relates to efficient synthetic method of 1,3,5-tris (N-Phenylbenzimidazole) Benzene and pertains to the field of synthesis of organic light-emitting materials. The method and process of the patent are as following: 1,3,5-tris (N-Phenyl-N Phenylammonium) Benzamide is treated by shrinking agent but no high temperature required, and then high purity product can be reached after raw material dissolved. The reaction only takes a few minutes and through recrystallization the purity can be over 99%, and then the material with stable crystal phase reached after sublimation step. The method introduced by the present patent is easy to operate, and with high in yield and purity, which adapt industrial production and has important significance for the industrialization. | 04-25-2013 |
| 20130137878 | PROCESS FOR MANUFACTURE OF TELMISARTAN - A process for preparing telmisartan by reacting 2-n-propyl-4-methyl-6-(1′-methylbenzimidazol-2′-yl)benzimidazole with a compound of formula (IV) | 05-30-2013 |
| 20130190508 | CATALYSTS CONTAINING N-HETEROCYCLIC CARBENES FOR ENANTIOSELECTIVE SYNTHESIS - Novel N-heterocyclic carbene ligand precursors, N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are provided. Metal-carbene complexes comprising N-heterocyclic carbene ligands can be chiral, which are useful for catalyzing enantioselective synthesis. Methods for the preparation of the N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are given. | 07-25-2013 |
| 20140316144 | ANTIVIRAL COMPOUNDS - The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds. | 10-23-2014 |
| 20150322047 | Crystal Forms - The present invention features crystalline forms of Compound I. In one embodiment, a crystalline form of Compound I has characteristic peaks in the PXRD pattern as shown in one of FIGS. | 11-12-2015 |
| 20160185722 | METHOD FOR PRODUCING META-XYLYLENEDIAMINES AND METHOD FOR PRODUCING BISAMIDE COMPOUND - A method for producing meta-xylylenediamines includes a reaction step in which monohalogenated benzenes, formaldehydes, and an amide compound having a primary amide group or a secondary amide group are allowed to react in the presence of an acidic liquid, a dehalogenation step in which the halogen atom derived from the monohalogenated benzenes is replaced with a hydrogen atom, and a deprotection step in which the primary amide group or the secondary amide group derived from the amide compound is converted to an amino group. In the reaction step, the acidic liquid contains inorganic acid, the equivalent ratio of the hydrogen atom of the inorganic acid relative to the monohalogenated benzenes is more than 16; the acidic liquid has an inorganic acid concentration of more than 80 mass %; and the reaction temperature is more than 40° C. | 06-30-2016 |
| 548306100 | The additional hetero ring contains nitrogen as the only ring hetero atom [e.g., 2-(2`-imidazolin-2`-yl)-benzimidazole; 1-p-chlorophenyl-3- pyrrolidin-1`- yl-propyl benzimidazolone, etc.] | 3 |
| 20090048452 | SUBSTITUTED HYDANTOINS - This invention relates to compounds of formula I: | 02-19-2009 |
| 20110071302 | PROCESS FOR PREPARING INTERMEDIATE COMPOUND FOR SYNTHESIZING AN ANTIULCERANT - The present invention relates a novel method of preparing an intermediate which is useful for synthesizing an antiulcerant. The present invention provides a method of preparing an intermediate of an antiulcerant which can obtain a high purity compound in high yield, with reduced production cost/time as compared to a conventional method. | 03-24-2011 |
| 20140024838 | 2-((R)-2-METHYLPYRROLIDIN-2-YL)-1H-BENZIMIDAZOLE-4-CARBOXAMIDE CRYSTALLINE FORM 1 - 2-((R)-2-Methylpyrrolidin-2-yl)-1H-benzimidazole-4-carboxamide Crystalline Form 1, ways to make it, compositions comprising it and made using it, and methods of treating patients having disease using it are disclosed. | 01-23-2014 |
| 20090048452 | SUBSTITUTED HYDANTOINS - This invention relates to compounds of formula I: | 02-19-2009 |
| 20110071302 | PROCESS FOR PREPARING INTERMEDIATE COMPOUND FOR SYNTHESIZING AN ANTIULCERANT - The present invention relates a novel method of preparing an intermediate which is useful for synthesizing an antiulcerant. The present invention provides a method of preparing an intermediate of an antiulcerant which can obtain a high purity compound in high yield, with reduced production cost/time as compared to a conventional method. | 03-24-2011 |
| 20140024838 | 2-((R)-2-METHYLPYRROLIDIN-2-YL)-1H-BENZIMIDAZOLE-4-CARBOXAMIDE CRYSTALLINE FORM 1 - 2-((R)-2-Methylpyrrolidin-2-yl)-1H-benzimidazole-4-carboxamide Crystalline Form 1, ways to make it, compositions comprising it and made using it, and methods of treating patients having disease using it are disclosed. | 01-23-2014 |
| 548306100 | The additional hetero ring contains nitrogen as the only ring hetero atom [e.g., 2-(2-imidazolin-2-yl)-benzimidazole; 1-p-chlorophenyl-3- pyrrolidin-1- yl-propyl benzimidazolone, etc.] | 3 |
| 20090048452 | SUBSTITUTED HYDANTOINS - This invention relates to compounds of formula I: | 02-19-2009 |
| 20110071302 | PROCESS FOR PREPARING INTERMEDIATE COMPOUND FOR SYNTHESIZING AN ANTIULCERANT - The present invention relates a novel method of preparing an intermediate which is useful for synthesizing an antiulcerant. The present invention provides a method of preparing an intermediate of an antiulcerant which can obtain a high purity compound in high yield, with reduced production cost/time as compared to a conventional method. | 03-24-2011 |
| 20140024838 | 2-((R)-2-METHYLPYRROLIDIN-2-YL)-1H-BENZIMIDAZOLE-4-CARBOXAMIDE CRYSTALLINE FORM 1 - 2-((R)-2-Methylpyrrolidin-2-yl)-1H-benzimidazole-4-carboxamide Crystalline Form 1, ways to make it, compositions comprising it and made using it, and methods of treating patients having disease using it are disclosed. | 01-23-2014 |
| 20090048452 | SUBSTITUTED HYDANTOINS - This invention relates to compounds of formula I: | 02-19-2009 |
| 20110071302 | PROCESS FOR PREPARING INTERMEDIATE COMPOUND FOR SYNTHESIZING AN ANTIULCERANT - The present invention relates a novel method of preparing an intermediate which is useful for synthesizing an antiulcerant. The present invention provides a method of preparing an intermediate of an antiulcerant which can obtain a high purity compound in high yield, with reduced production cost/time as compared to a conventional method. | 03-24-2011 |
| 20140024838 | 2-((R)-2-METHYLPYRROLIDIN-2-YL)-1H-BENZIMIDAZOLE-4-CARBOXAMIDE CRYSTALLINE FORM 1 - 2-((R)-2-Methylpyrrolidin-2-yl)-1H-benzimidazole-4-carboxamide Crystalline Form 1, ways to make it, compositions comprising it and made using it, and methods of treating patients having disease using it are disclosed. | 01-23-2014 |
| 548306400 | Chalcogen bonded directly to ring carbon of the diazole ring | 4 |
| 20090012305 | 2-[[1-[[(2,3-Dihydro-2-Oxo-1H-Benzimidazol-5-Yl)Amino]Carbonyl]-2-Oxopropyl]Azo]-Benzoic Acid and a Process For Its Preparation - The present invention is directed to 2-[[1-[[(2,3-dihydro-2-oxo-1H-benzimidazol-5-yl)amino]carbonyl]-2-oxo-propyl]azo]-benzoic acid (C.I. Pigment Yellow 151): (I), characterized by a ΔE* (black/white) in masstone below 22.0±0.7, a process for its preparation and its use for pigmenting macromolecular organic materials of natural or synthetic origin. The pigment has high opacity and high color strength. | 01-08-2009 |
| 20110190509 | Processes for the Preparation of Bendamustine - New methods for the preparation of bendamustine, and the pharmaceutical salts thereof, are described. Novel compounds useful for the preparation of bendamustine are also described. | 08-04-2011 |
| 20110282072 | SELF-ASSEMBLED NANOSTRUCTURES - An alkylated benzimidazolone compound of the formula: | 11-17-2011 |
| 548307100 | The chalcogen is sulfur | 1 |
| 20130303781 | PROCESS FOR PREPARATION OF TRICLABENDAZOLE - The present invention discloses a method for preparing Triclabendazole comprising condensing N-(4,5-dichloro-2-ni-trophenyl)acetamide with 2,3-dichlorophenol to obtain 4-chloro-5(2,3-dichlorophenoxy)-2-nitrophenyl acetamide and it to obtain 4-chloro-5(2,3-dichlorophenoxy)-2-nitroaniline; reducing 4-chloro-5(2,3-dichlorophenoxy)-2-nitroaniline in presence of Raney nickel to obtain 4-chloro-5-(2,3-dichlorophenoxy)benzene-1,2-diamine of; cyclising 4-chloro-5-(2,3-dichlorophenoxy)benzene-1,2-diamine in presence of carbondisulfide to obtain 6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazole-2-thiol; methylating 6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazole-2-thiol using a methylating agent to obtain triclabendazole methanesulfonate salt; converting triclabendazole methanesulfonate salt to hydrochloride salt of Triclabendazole and hydrolysing it to obtain Triclabendazole. | 11-14-2013 |
| 548307400 | Nitrogen attached directly to the diazole ring by nonionic bonding | 2 |
| 20130345436 | method for preparing 2-(N-substituted)-amino-benzimidazole derivatives - A method for preparing 2-(N-substituted)-amino-benzimidazole derivatives is provided, which comprises the following steps: (1) reacting a compound of 2-(N-protecting group)-O-aryl diamine with a compound of N-phenoxycarbonyl monosubstituted amine to obtain a compound of 2-(N-protecting group)-amino aryl urea; (2) in a suitable organic solvent, performing dehydrating cyclization reaction of the compound of 2-(N-protecting group)-amino aryl urea in the presence of an organic base and dichloro triphenylphosphine prepared by triphenylphosphine oxide with oxalyl chloride or diphosgene or triphosgene, or dibromo triphenylphosphine prepared by triphenylphosphine oxide with bromine, to produce a compound of 1-protecting group-2-(N-substituted)-amino-benzimidazole; (3) deprotecting the resulting compound of 1-protecting group-2-(N-substituted)-amino-benzimidazole to obtain the compound 2-(N-substituted)-amino-benzimidazole. | 12-26-2013 |
| 548308700 | Having -C(=X)-X-, wherein the X`s are the same or diverse chalcogens, attached indirectly to the diazole ring by acyclic nonionic bonding | 1 |
| 548309100 | Chalcogen bonded directly to the benzene ring of the bicyclo ring system | 1 |
| 20130303782 | PROCESS FOR PREPARATION OF ALBENDAZOLE - The present invention discloses a novel, cost-effective process for preparation of a benzimidazole carbamates compound. Specifically, it relates to the process for the preparation of anti-parasite bulk drug albendazole. The process comprises a) thiocyanating 2-nitroaniline of formula VI with ammonium thiocyanated in presence of a halogen to obtain 2-nitro-4-thiocyanoaniline of formula V; b)propylating 2-nitro-4-thiocyanoaniline of formula V with propylbromide in presence of n-propanol and a base in absence of a phase transfer catalyst to obtain 4-propylthio-2-nitroaniline of formula III; C) reducing the nitro group of 4-propylthio-2-nitroaniline prepared in step b) by reacting an aqueous alkali metal sulphide or an alkaline metal sulphide to obtain 4-propylthio-o-phenylenediamine of formula II; and d)condensing 4-propylthio-o-phenylenediamine of formula II with alkali or alkaline earth metal salt of methylcyano carbamate in presence of an acid to form Albendazole of formula I. | 11-14-2013 |
| 548309400 | Having -C(=X)-, wherein X is chalcogen, bonded directly to the diazole ring | 1 |
| 20160108002 | UNIVERSAL READER MOLECULE FOR RECOGNITION TUNNELING - Some embodiments of the present disclosure are directed to a compound 5(6)-mercapto-1H-benzo[d]imidazole-2-carboxamide (“BIA”) which yields enhanced signals for recognition tunneling. Other embodiments are directed toward methods for producing such compounds as well as apparatuses and systems which utilize such compounds for recognition tunneling for molecule identification/sequencing (for example). | 04-21-2016 |
| 548309700 | Nitrogen attached indirectly to the diazole ring by acyclic nonionic bonding | 3 |
| 20110207939 | FACTOR VIIA INHIBITOR - The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed. | 08-25-2011 |
| 20140142321 | Benzimidazole Derivatives As PI3 Kinase Inhibitors - This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer. | 05-22-2014 |
| 20140221667 | FACTOR VIIA INHIBITOR - The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed. | 08-07-2014 |
| 548310100 | Chalcogen attached indirectly to the diazole ring by acyclic nonionic bonding | 19 |
| 20100048912 | Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity - Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3β-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3β-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer. | 02-25-2010 |
| 20100048913 | Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity - Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3β-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3β-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer. | 02-25-2010 |
| 20100048914 | Novel C-17-Heteroaryl Steroidal Cyp17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity - Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3β-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3β-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP 17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer. | 02-25-2010 |
| 20120165543 | PROCESS FOR THE PRODUCTION OF BENDAMUSTINE ALKYL ESTER, BENDAMUSTINE, AND DERIVATIVES THEREOF - Methods are provided for the production of bendamustine alkyl ester, bendamustine, as well as derivatives thereof. With the methods the production of these compounds is possible in reproducibly high yields. To this end, hydroxyl-group-containing esters are used as the starting material, whose hydroxyl groups are substituted in a simple way by halogen groups. This substitution is possible in the presence of (i) oxalyl chloride and (ii) dialkylformamide, dialkyl acetamide or dimethyl sulfoxide. In a subsequent reaction, the resulting esters can be hydrolyzed to form the acid. | 06-28-2012 |
| 20130144068 | Methods for the Sterilization of Bendamustine - The present application is directed to methods of sterilizing bendamustine and its pharmaceutically acceptable salt forms. Preferred sterilization methods include dry heat sterilization, gamma irradiation, and e beam radiation. Sterile pharmaceutical compositions are also described. | 06-06-2013 |
| 20130158273 | PREPARATION OF BENDAMUSTINE AND ITS SALTS - The present application relate to processes for the preparation of bendamustine and its pharmaceutically acceptable salts. | 06-20-2013 |
| 20130184471 | Process for the preparation of bendamustine hydrochloride and related compounds - The present invention relates to a process for preparing bendamustine hydrochloride, derivatives and related compounds thereof. | 07-18-2013 |
| 20130204009 | PROCESS FOR PREPARING BENZOIC ACID ESTERS - There is provided a more industrially advantageous process for preparing novel pyridine derivatives expected to be used as medicines. A process for preparing 3-[(6-hydroxy-1-methyl-1H-benzimidazol-2-yl)methoxy]benzoic acid esters as intermediates with high quality, in short steps and in a high yield, as well as novel benzoic acid esters as their precursors and a process for preparing the same. | 08-08-2013 |
| 20130217888 | PROCESS FOR PREPARING BENDAMUS TINE HYDROCHLORIDE MONOHYDRATE - The present invention provide processes for the preparation of Bendamustine hydrochloride monohydrate of formula (I) | 08-22-2013 |
| 20130310571 | METHODS FOR THE PREPARATION OF BENDAMUSTINE - Improved methods for the preparation and purification of bendamustine hydrochloride are described; such as method of preparing bendamustine hydrochloride comprising contacting a compound of formula HBI: with thionyl chloride | 11-21-2013 |
| 20130317234 | Process for Preparation of Intermediates of Bendamustine - The present invention relates to a process for the preparation of 4-{5-{Bis-(2-hydroxyl-ethyl)-amino}-1-methyl-1H-Benzoimidazol-2yl}-butyric acid alkyl ester of formula IV, a key intermediate in the process for the preparation of Bendamustine HCl (I) | 11-28-2013 |
| 20140031560 | PROCESS FOR THE PREPARATION OF BENDAMUSTINE - The present invention relates to a method for preparation of alkyl 4-[5-[bis(2-hydroxyethyl)amino]-1-methyl-1H-benzimidazol-2-yl]butanoate (7) from 2-fluoro-5-nitroaniline, comprising the steps of: (a) conversion of 2-fluoro-5-nitroaniline to 5-(2-fluoro-5-nitroanilino)-5-oxopentanoic acid (1) using glutaric anhydride, conversion of compound (1) to methylammonium 5-[2-(methylamino)-5-nitroanilino]-5-oxopentanoate (2) using methylamine; conversion of compound (2) to 5-[2-(methylamino)-5-nitroanilino]-5-oxopentanoic acid (3) and condensation of compound (3) to 4-(1-methyl-5-nitro-1H-benzimidazol-2-yl)butanoic acid (4); (b) esterification of the product (4) of step a) to alkyl 4-(1-methyl-5-nitro1H-benzimidazol-2-yl)butanoate (5); (c) reduction of the product of step b) to alkyl 4-(5-amino-1-methyl-1H-benzimidazol-2-yl)butanoate (6), and (d) conversion of the product of step c) to alkyl 4-[5-[bis(2-hydroxyethyl)amino]-1-methyl-1H-benzimidazol-2-yl]butanoate (7) | 01-30-2014 |
| 20140121383 | PROCESS FOR THE PREPARATION OF BENDAMUSTINE HYDROCHLORIDE - The present invention relates to an improved process for the synthesis of bendamustine, in particular, bendamustine hydrochloride of the formula (VI) and its intermediate 1-Methyl-5-[bis(2-chloroethyl)amino]-1H-benzimidazol-2-yl]lithium butanoate of formula (V), both having a purity of ≧99%, which is simple, convenient, economical, does not use hazardous chemicals and industrially viable. | 05-01-2014 |
| 20140121384 | PROCESS FOR BENDAMUSTINE HYDROCHLORIDE - The present invention provides a process for the preparation of 1H-benzimidazol-1-methyl-5-N,N-di(2-hydroxyethyl)-2-butanoic acid ethyl ester. The present invention also provides a process for the preparation of bendamustine hydrochloride. The present invention further provides a process for the purification of bendamustine hydrochloride. | 05-01-2014 |
| 20140275566 | PROCESS FOR DRYING BENDAMUSTINE HYDROCHLORIDE MONOHYDRATE - Wet bendamustine hydrochloride monohydrate may be dried by a two stage process wherein rapid drying is first carried out to provide a partially dried product, which is then further dried using an inert gas of controlled relative humidity to yield dry bendamustine hydrochloride monohydrate. | 09-18-2014 |
| 20140275567 | PROCESS FOR PREPARING ALKYL ESTERS OF 4-(5-(BIS(2-HYDROXYETHYL)AMINO)-1-METHYL-1H-BENZO[D]IMIDAZOL-2-YL)BUTYRIC ACID - An alkyl ester of 4-(5-(bis(2-hydroxyethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butyric acid, such as ethyl 4-(5-(bis(2-hydroxyethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoate, is obtained by reacting an alkyl ester of 4-(5-amino-1-methyl-1H-benzo[d]imidazol-2-yl)butyric acid with 2-hydroxyacetaldehyde under reducing conditions. | 09-18-2014 |
| 20150105561 | PROCESS FOR THE PREPARATION OF BENDAMUSTINE HYDROCHLORIDE - The present invention relates to an improved process for the synthesis of bendamustine, in particular, bendamustine hydrochloride of the formula (VI) and its intermediate 1-methyl-5-[bis(2-chloroethyl)amino]-1H-benzimidazol-2-yl]lithium butanoate of formula (V), both having a purity of ≧99%, which is simple, convenient, economical, does not use hazardous chemicals and is industrially viable. | 04-16-2015 |
| 20160016912 | BENDAMUSTINE DERIVATIVES AND METHODS OF USING SAME - The present invention is directed to bendamustine esters and bendamustine amides and their use for the treatment of cancer. | 01-21-2016 |
| 20160194289 | PROCESS FOR DRYING BENDAMUSTINE HYDROCHLORIDE MONOHYDRATE | 07-07-2016 |
| 548310700 | Benzene ring bonded directly at the 2- position of the diazole ring | 4 |
| 20080275250 | Factor Viia Inhibitor - The present invention relates to novel inhibitors or Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed. | 11-06-2008 |
| 20110040101 | ALANINE RACEMASE CHIRAL BINAPHTHOL DERIVATIVE WITH POWERFUL HYDROGEN BOND DONOR, AND OPTICAL RESOLUTION AND OPTICAL TRANSFORMATION METHODS USING THE SAME - Disclosed is an alanine racemase chiral binaphthol derivative having the ability to recognize amino alcohols selectively on the basis of chirality and transform amino acids from an L-form into a D-form. Methods for the optical resolution of amino acid or amino alcohol and for the optical transformation of D- and L-forms of amino acids using the binaphthol derivative are also provided. | 02-17-2011 |
| 20140114076 | MATERIALS FOR ORGANIC ELECTROLUMINESCENCE DEVICES - The present invention relates to substituted benzo[c]phenanthrene derivatives and to the production and to the use thereof in electronic devices, and to the electronic devices themselves. The present invention relates in particular to benzo[c]phenanthrene derivatives substituted with at least one aromatic unit or at least one diarylamino unit. | 04-24-2014 |
| 20150099890 | Polyphenylene Host Compounds - Polyphenylene compounds such as compounds represented by Formula 1 may be used in electronic devices such as organic light-emitting devices. For example, the compounds may be used as host materials in a light-emitting layer. | 04-09-2015 |
