Class / Patent application number | Description | Number of patent applications / Date published |
549510000 | The hetero ring is four-membered | 55 |
20080200699 | Method for Preparing Docetaxel - The invention concerns a method for preparing docetaxel from paclitaxel, including the following steps: a) deacylating paclitaxel, b) protecting the free hydroxy functions, in 7-, 10- and 2′-position respectively, c) debenzoylating the amine in 3′-position, into a primary amine derived for 10-deacetylbaccatine whereof the hydroxy functions in 7-, 10- and 2′-position are protected, d) functionalizing the amine with a t-butoxycarbonyl In radical to obtain a docetaxel derivative of general formula (I), wherein: X represents protecting radicals or hydrogen atoms, then, if required, e) releasing the initially protected hydroxy functions to obtain docetaxel. | 08-21-2008 |
20080200700 | SEMISYNTHESIS PROCESS FOR THE PREPARATION OF 10 DEACETYL-N-DEBENZOYL-PACLITAXEL - The invention relates to a process for the preparation of 10-deacetyl-N-debenzoyl-paclitaxel (I) | 08-21-2008 |
20080207929 | Method for Preparing Paclitaxel - The invention concerns a method for preparing paclitaxel characterized in that it consists in starting with 10-deacety)-baccatine in accordance with a “one-pot” reaction including the following three steps: a) protecting the hydroxy radical in position 7 of 10-deacetylbaccatine with a silylated radical, then b) acetylating the hydroxy radical in position 10, c) optionally crystallizing the resulting baccatine III derivative, followed by condensation of (4S,5R)-3-N-benzoyl-2RS-methoxy-4-phenyl-1,3-oxazolidine-5-carboxylic acid, by esterifying in position 13 the acetylated 10-baccatine III derivative previously obtained, then opening the oxazolidine of the cyclic side chain and simultaneously releasing the hydroxy radical in position 7. | 08-28-2008 |
20080214847 | Process for the Separation of Paclitaxel and Cephalomannin - Paclitaxel is separated from a mixture containing cephalomannin by column chromatography on silica gel using a solvent mixture containing methyl isobutyl ketone and a less polar solvent as the mobile phase. The less polar solvent can be a (C | 09-04-2008 |
20080221341 | Trisoxetane compound, process for producing the same, and opitcal waveguide using the same - The present invention relates to a trisoxetane compound represented by the following formula (1): | 09-11-2008 |
20080262250 | Semi-Synthesis of Taxane Intermediates and Their Conversion to Paclitaxel and Docetaxel - A process is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis of protected taxane intermediates. | 10-23-2008 |
20080287696 | Process for the Preparation of Synthetic Taxanes - The present invention relates to a process for the preparation of synthetic taxanes, which protects C(7)-OH with lanthanon compounds. Its advantages are simple process and firm & reliable binding. Moreover, no C(7)-acylated taxanes are produced in the subsequent steps, and hydrolysis of C(2′)-ester groups in acylated products becomes readily controllable. In the process for the preparation of synthetic taxanes, tetrahydrofuran is used in the present invention as a medium for acylation, which not only achieves the same effects as pyridine, but also avoids odor, so as to solve the problem regarding the extremely high requirements for the place of production. The present invention can be used for the preparation of not only semi-synthetic taxane using natural taxanes as raw material, but also full-synthetic taxane. | 11-20-2008 |
20090018353 | METHOD FOR PREPARATION OF AMORPHOUS, ANHYDROUS CRYSTALLINE OR HYDRATED CRYSTALLINE DOCETAXEL - This invention is directed to a method for the preparation of docetaxel having an amorphous, anhydrous crystalline, or hydrated crystalline structure. In accordance with the invention, highly pure amorphous, anhydrous crystalline, or hydrated crystalline docetaxel can be produced with a high yield by using a solvent precipitation method, colloid formation method, etc. | 01-15-2009 |
20090216031 | Process for the isolation of paclitaxel - Paclitaxel is isolated by a process including normal phase chromatography using a polyamide stationary phase and a mixture containing a dialkyl ketone and a less polar solvent as a mobile phase. Suitable dialkyl ketones include acetone or methyl isobutyl ketone. Suitable less polar co-solvents include a (C | 08-27-2009 |
20090275762 | Crystalline Forms of Docetaxel and process for Preparation Thereof - New anhydrous crystalline form of docetaxel and process of making anhydrous docetaxel and docetaxel trihydrate are provided. | 11-05-2009 |
20090287005 | DENDRIMER CONJUGATES - The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. | 11-19-2009 |
20090292131 | PROCESSES FOR PREPARATION OF TAXANES AND INTERMEDIATES THEREOF - A paclitaxel intermediate of formula 1: | 11-26-2009 |
20100029957 | Semi-Synthetic Process for the Preparation of Taxane Derivatives - This invention relates to an improved semi-synthetic process for the preparation of taxane derivatives like paclitaxel, docetaxel, canadensol and its derivatives, the process, which has shorten reaction route, simple procedure, high yield and low materials cost, therefore facilitates the commercial manufacture of these derivatives. | 02-04-2010 |
20100099896 | METHOD OF PREPARING DOCETAXEL AND INTERMEDIATES USED THEREIN - The present invention relates to a novel method for preparing docetaxel having anti-tumor and anti-leukemia activity, and intermediates useful for preparing docetaxel. | 04-22-2010 |
20100099897 | STABLE ANHYDROUS CRYSTALLINE DOCETAXEL AND METHOD FOR THE PREPARATION THEREOF - The present invention provides a stable anhydrous crystalline docetaxel which has anti-tumor and anti-leukemia activity, and method for the preparation thereof. | 04-22-2010 |
20100145080 | PURIFICATION OF TAXANES - Disclosed is a method of crystallizing a taxane comprising combining the taxane and methylene chloride to obtain a solution and adding an anti-solvent to the solution to obtain a crystalline taxane, wherein the anti-solvent is selected from the group consisting of hexane and heptane. | 06-10-2010 |
20100160653 | DOCETAXEL POLYMORPHS AND PROCESSES - The present invention provides crystalline polymorphs of docetaxel and processes for preparing them, a method for preparing amorphous docetaxel, and a process for preparing docetaxel. | 06-24-2010 |
20100174098 | 3-ETHYLOXETHANE COMPOUND HAVING HYDROXYL GROUP AND METHOD FOR PRODUCING THE SAME - Disclosed is a 3-ethyloxethane compound having a hydroxyl group which is represented by the following general formula (1). (1) (In the formula, A represents an alkylene group having 3-5 carbon atoms which may have an ether bond or an alkylene group having 3-5 carbon atoms which may be substituted by a hydroxyl group.) The 3-ethyloxethane compound having a hydroxyl group can be produced by reacting a 3-ethyloxethane compound represented by the general formula (2) below, a diol compound represented by the general formula (3) below and a base. (2) (In the formula, X represents a leaving group.) (3) (In the formula, A is as defined above.) | 07-08-2010 |
20100197944 | DOCETAXEL PROCESS AND POLYMORPHS - Processes for preparing substantially pure docetaxel, new crystalline forms of docetaxel and processes for preparation thereof, processes for preparing docetaxel trihydrate, and pharmaceutical compositions comprising docetaxel. | 08-05-2010 |
20100311991 | PROCESS FOR THE PREPARATION OF DOCETAXEL, ITS INTERMEDIATES, AND METHODS FOR PREPARATION THEREOF - The present invention disclosed an process for preparing docetaxel 1, including the following steps: a) hydroxyl acylation reaction of compound 2 and 3 to obtain compound 4; b) deprotection group R | 12-09-2010 |
20100324315 | POLY(CITRIC ACID) FUNCTIONALIZED CARBON NANOTUBE DRUG DELIVERY SYSTEM - A method for synthesizing carbon nanotube drug carriers and the carbon nanotube drug carriers are disclosed. Initially, carbon nanotubes, nitric acid, and sulfuric acid are mixed to oxidize carbon nanotubes in a first mixture. The oxidized carbon nanotubes are then extracted from the first mixture. The oxidized carbon nanotubes and monohydrated citric acid are mixed to synthesize carbon nanotubes grafted with poly(citric acid) in a second mixture. The carbon nanotubes grafted with poly(citric acid) are then extracted from the second mixture. The carbon nanotubes grafted with poly(citric acid) and 4-(dimethylamino)pyridine are dissolved in anhydrous dimethylformamide in a third mixture. Next, a mixture that comprises a drug is added to the third mixture to synthesize the carbon nanotubes grafted with poly(citric acid) and the drug in a fourth mixture. Then, the carbon nanotubes grafted with poly(citric acid) and the drug are extracted from the fourth mixture. | 12-23-2010 |
20110144360 | PREPARATION OF TAXANES FROM 9-DIHYDRO-13-ACETYLBACCATION III - A new process for preparing a compound of Formula V, wherein P is a hydroxy protecting group and R is acetyl, said process including the steps of: i) selectively deacetylating the 10-hydroxy group of 9-dihydro-13-acetylbaccatin III with N,N-dimethylethylenediamine to produce 9-dihydro-10-deacetyl-13-acetyl-baccatin III; ii) concomitantly protecting 7-hydroxy and 10-hydroxy groups of the reaction product of step i); and iii) oxidizing the 9-hydroxy group of the reaction product of step ii) with an oxidizing agent to produce the compound of formula V. | 06-16-2011 |
20110306781 | Method for Producing Optically Active Fluorinated Oxetane - Disclosed is a method of producing an optically active fluorinated oxetane, which can be an important pharmaceutical or agricultural intermediate, by reaction of a fluorinated α-keto ester with an acyl alkenyl ether in the presence of a transition metal complex with an optically active ligand. This method utilizes a catalytic asymmetric synthesis process and does not require a stoichiometric amount of chiral source. It is thus possible to dramatically reduce the amount of use of the asymmetric catalyst especially when the reaction is performed at a high concentration of substrate (with the use of a small amount of reaction solvent) or in the absence of a reaction solvent (under neat conditions). Further, the target optically active fluorinated oxetane can be obtained with high yield and with very high optical purity. The product contains almost no difficult-to-separate impurity and shows high chemical purity. | 12-15-2011 |
20120035379 | METHOD FOR PREPARING TAXANE DERIVATIVES - Provided is a method for preparing a taxane derivative, comprising: carrying out condensation of a phenylisoserine derivatives having a protective group introduced thereto or a mixture of isomers thereof, as a side chain, with a baccatin III derivative or 10-deacetyl-baccatin III derivative to obtain a mixture of isomers; separating the isomers via chromatography; and carrying out a reversion of the stereochemical structure of a selectively separated isomer, which is suitable for producing a taxane derivative in a large scale with high yield. | 02-09-2012 |
20120071674 | SOLVATES OF DOCETAXEL - The present invention provides solvates of 4-acetoxy-2α-benzoyloxy-5β,20-epoxy-1,7β,10β-trihydroxy-9-oxo-tax-11-en-13α-yl (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate and C2-3-alkyl esters of formic acid, process of their preparation and their use in the synthesis of the pharmaceutically pure 4-acetoxy-2α-benzoyloxy-5β,20-epoxy-1,7β,10β-trihydroxy-9-oxo-tax-11-en-13α-yl (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate. | 03-22-2012 |
20120149925 | PROCESS FOR PREPARING TAXOIDS FROM BACCATIN DERIVATIVES USING LEWIS ACID CATALYST - The present invention relates to a process of preparing a taxoid (X) by reacting a protected baccatin derivative (B) with a β-lactam (C) in the presence of one or more Lewis acids and a base agent. The present invention also relates to a process of preparing the protected baccatin derivative (B) from a baccatin derivative (A) comprising a protection reaction catalyzed by one or more Lewis acids with an optional base agent. | 06-14-2012 |
20120232295 | OXETANE-RING-CONTAINING (METH)ACRYLIC ACID ESTER COMPOUND - Provided is a novel oxetane-ring-containing (meth)acrylic ester compound which can give, through polymerization, a cured article being highly flexible or thermally stable. The oxetane-ring-containing (meth)acrylic ester compound is represented by formula (1) below, in which R | 09-13-2012 |
20130046104 | METHOD FOR PREPARING HIGHLY PURE ANHYDROUS CRYSTALLINE DOCETAXEL - A method for preparing highly pure anhydrous crystalline docetaxel is provided. The method for preparing highly pure anhydrous crystalline docetaxel enables preparation of anhydrous crystalline docetaxel that has purity of 99.5% or more, and is useful as an anticancer agent due to remarkably low residual solvent content compared to the standard of residual solvents in drugs. | 02-21-2013 |
20130079533 | Method for Preparing a Polymer Conjugate - Provided herein is a straightforward and efficient method for covalently attaching a polyethylene glycol polymer to a taxane. The method involves, among other things, a step of reacting a taxame with a polyethylene glycol polymer comprising a functional group reactive with a functional group within said taxane in the presence of a coupling reagent and DPTS. The result of the reacting step is the formation of a polyethylene glycol-taxane conjugate. | 03-28-2013 |
20130090484 | PROCESS FOR MAKING AN INTERMEDIATE OF CABAZITAXEL - A novel process of making 7,10-dialkyl-10-DAB of formula (I) | 04-11-2013 |
20130109870 | AMORPHOUS FORM OF CABAZITAXEL AND PROCESS FOR ITS PREPARATION | 05-02-2013 |
20130178639 | CRYSTALLINE FORMS OF DIMETHOXY DOCETAXEL AND METHODS FOR PREPARING THE SAME - The invention relates to anhydrides, solvates and ethanol hetero-solvates and hydrates of dimethoxy docetaxel or (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate of 4-acetoxy-2α-benzoyloxy-5β,20-epoxy-1-hydroxy-7β, 10β-dimethoxy-9-oxo-tax-11-ene-13α-yle, and to the preparation thereof. | 07-11-2013 |
20130211109 | CRYSTALLINE FORMS OF CABAZITAXEL AND PROCESS FOR PREPARATION THEREOF - The present invention provides Crystalline Forms of 4-acetoxy-2α-benzoyloxy-5β-20-epoxy-1-hydroxy-7β,10β-dimethoxy-9-oxotax-11-en-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate, i.e Cabazitaxel. The present invention also discloses methods for the preparation of Crystalline Forms of Cabazitaxel and pharmaceutical compositions thereof. | 08-15-2013 |
20130324746 | NOVEL PACLITAXEL TRIHYDRATES AND METHODS OF MAKING THEREOF - Novel paclitaxel trihydrates. The paclitaxel trihydrates described herein are obtained by recrystallizing paclitaxel from a water/alcohol solution. Such recrystallization is known in the art to yield the one previously known paclitaxel crystalline trihydrate polymorph. Formation of the novel paclitaxel trihydrates described herein is induced by subjecting paclitaxel trihydrate crystals to an elevated pressure. As evidenced by NMR spectra, the novel paclitaxel trihydrates described herein have three-dimensional structures and/or water coordination geometry structures that are distinct from any previously known paclitaxel trihydrate. | 12-05-2013 |
20140005419 | Method for Preparing a Polymer Conjugate | 01-02-2014 |
20140024845 | Non-Ring Hydroxy Substituted Taxanes and Methods for Synthesizing the Same - The invention relates to (among other things) non-ring hydroxy substituted taxanes and methods for synthesizing the same. The invention further relates to conjugating the non-ring hydroxyl substituted taxanes to a water-soluble, non-peptidic polymer. | 01-23-2014 |
20140039209 | PROCESS FOR PREPARING DOCETAXEL AND ITS HYDRATE - The present invention provide process of preparation of (2R,3S)—N-carboxy-3-phenylisoserine, N-tert-butyl ester, 13-ester with 5(β)-20-epoxy-1,2(α),4,7(β),10(β),13(α)-hexa hydroxy tax-11-en-9-one 4-acetate 2-benzoate or docetaxel and its trihydrate (I) | 02-06-2014 |
20140350272 | CRYSTALLINE FORMS OF DIMETHOXY DOCETAXEL AND METHODS FOR PREPARING THE SAME - The invention relates to anhydrides, solvates and ethanol hetero-solvates and hydrates of dimethoxy docetaxel or (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate of 4-acetoxy-2α-benzoyloxy-5β,20-epoxy-1-hydroxy-7β, 10β-dimethoxy-9-oxo-tax-11-ene-13α-yle, and to the preparation thereof. | 11-27-2014 |
20140350273 | PEDIATRIC USES OF CABAZITAXEL - The present invention relates to the compound of formula (I): | 11-27-2014 |
20150057458 | PROCESS FOR THE PRODUCTION OF CHEMICAL COMPOUNDS FROM CARBON DIOXIDE - Process for the production of a chemical compound from a carbon dioxide starting material, comprising the steps of a) providing a feed stream consisting mainly of carbon dioxide; b) electrolysing in an electrolysis stage the carbon dioxide in the feed stream to a first gas stream containing carbon monoxide and a second gas stream containing oxygen, wherein the molar ratio between carbon monoxide and oxygen is about 1:0.5 in an electrolysis stage; c) adjusting the composition of the first gas stream or the second gas stream or both gas streams to include carbon dioxide, either by operating at less than full conversion of CO2 or by sweeping one or both gas streams with a gas containing CO | 02-26-2015 |
20150073159 | Solid State Forms Of Cabazitaxel And Processes For Preparation Thereof - The invention relates to solid state forms of Cabazitaxel, and processes for preparation, via novel synthetic intermediates, thereof, and formulations comprising one or more of the solid state forms of Cabazitaxel. The present invention further provides pharmaceutical compositions comprising one or more of the solid state forms of Cabazitaxel, and a method of treating hormone-refractory prostate cancer | 03-12-2015 |
20150119589 | METHODS FOR MAKING OXETAN-3-YLMETHANAMINES - This invention relates to methods for making oxetan-3-ylmethanamines having the formula (I) wherein R1? and R2? are as defined herein. The methods of the invention provide the compounds of formula (I) in high yields and under conditions amenable for large-scale commercial production. | 04-30-2015 |
20150141673 | NOVEL CRYSTALLINE FOR W OF CABAZITAXEL AND METHOD FOR PREPARING IT - The present invention relates to a novel crystalline polymorph form W of cabazitaxel and to method for the preparation thereof. | 05-21-2015 |
20150141674 | CRYSTAL FORM OF CABAZITAXEL AND PREPARATION METHOD THEREOF - The present invention relates to the field of medical chemistry, and discloses a preparing method for three crystal forms of cabazitaxel, that is, crystalline form J of cabazitaxel esterate, crystalline form G of cabazitaxel hydrate and crystalline form I of cabazitaxel, and a novel crystalline form of cabazitaxel. The novel crystalline form of cabazitaxel according to the invention has good stability and good solubility in commonly used solvents, and is easy to be preserved and is stable under treatment during preparation of dosage forms, thus could be used for the preparation of a medicament for treating prostate cancer. | 05-21-2015 |
20150307468 | PROCESS FOR THE PREPARATION OF CABAZITAXEL AND ITS INTERMEDIATES - The present invention relates to a novel process for preparation of cabazitaxel (I) starting from 10-Deacetyl baccatin or derivative that involves methylation of 7, 10 —OH groups. Also provided is a novel process using chiral bis-lactam linker for the synthesis of cabazitaxel. | 10-29-2015 |
20160024037 | Thermal Extraction Method and Product - The present invention is related to a thermal extract of a plant material and methods of extraction thereof. The method of producing a thermal extract from a plant starting material by means of a thermal extraction of the starting material wherein the improvement consists in requiring smaller amounts of costly and/or toxic organic solvents for the extraction and partitioning steps. | 01-28-2016 |
20160039751 | NOVEL HYDROXAMIC ACID DERIVATIVE OR SALT THEREOF - A compound represented by general formula (1) (wherein R | 02-11-2016 |
20160176837 | PURIFICATION OF TAXANES | 06-23-2016 |
20190144405 | Polyfunctional Oxetane-Based Compound and Production Method Thereof | 05-16-2019 |
20190144406 | CRYSTALLINE FORMS OF DIMETHOXY DOCETAXEL AND METHODS FOR PREPARING THE SAME | 05-16-2019 |
549511000 | Sulfur or halogen attached directly or indirectly to the hetero ring by nonionic bonding | 5 |
20080242878 | Semi-Synthetic Taxane Derivatives With Antitumor Activity - The invention discloses novel secotaxane derivatives of general formula 1, having cytotoxic activity, which can be administered through the injective or oral route, for the therapy of tumors. | 10-02-2008 |
20090149665 | FLUORINE-CONTAINING ADAMANTANE DERIVATIVE, FLUORINE-CONTAINING ADAMANTANE DERIVATIVE HAVING POLYMERIZABLE GROUP, AND RESIN COMPOSITION CONTAINING SAME - Provided are a polymerizable group-containing and fluorine-containing adamantane derivative capable of affording a cured product having good heat resistance, good mechanical properties such as surface hardness and a low refractive index, a resin composition containing such a polymerizable group-containing adamantane derivative, and a fluorine-containing adamantane derivative which is useful as a reaction intermediate used for the production of the polymerizable group-containing and fluorine-containing adamantane derivative. Specifically provided are a fluorine-containing adamantane derivative represented by the general formula (I) below, a polymerizable group-containing and fluorine-containing adamantane derivative represented by the general formula (II) below, and a resin composition containing such a polymerizable group-containing and fluorine-containing adamantane derivative. In the formulas, X | 06-11-2009 |
20110275841 | PREPARATION OF DOCETAXEL - The present invention relates to docetaxel and processes for preparing docetaxel, including process-related intermediates. The present invention also relates to processes for preparing substantially pure docetaxel and intermediates. | 11-10-2011 |
20130310580 | Method For Producing Optically Active Fluorine-Containing Oxeten - A method for producing an optically active fluorine-containing oxeten, the method being provided to include the steps of causing a fluorine-containing α-ketoester and an internal alkyne to react with each other in the presence of a transition metal complex that has an optically active ligand. | 11-21-2013 |
20140371474 | CABAZITAXEL, RELATED COMPOUNDS AND METHODS OF SYNTHESIS - The invention provides new cabazitaxel isoserine ester intermediates and new synthetic methods, and a preparation method for the anti-tumour drugs cabazitaxel, docetaxel and paclitaxel from the new cabazitaxel isoserine intermediates. | 12-18-2014 |