| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 544137000 | The five-membered hetero ring has at least oxygen and nitrogen as ring hetero atoms | 48 |
| 20080200674 | SUBSTITUTED OXAZOLIDINONES AND THEIR USE IN THE FIELD OF BLOOD COAGULATION - The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) | 08-21-2008 |
| 20080319191 | Crystalline form IV of linezolid - The present invention provides a novel crystalline form of linezolid referred to herein as Form IV as well as methods for the preparation and use of Form IV. The present invention provides pharmaceutical compositions that comprise therapeutically effective amounts of Form IV that can be used to treat patients suffering from gram-positive bacterial infections. Various processes for making crystalline linezolid Form IV are disclosed. | 12-25-2008 |
| 20090062534 | LINEZOLID CRYSTALLINE HYDRATE FORM AND LINEZOLID SALTS - Linezolid salts, useful as such and as intermediates in a process for the preparation of novel and known crystalline linezolid forms, in particular known as Form III. | 03-05-2009 |
| 20090076264 | DEUTERIUM-ENRICHED RIVAROXABAN - The present application describes deuterium-enriched rivaroxaban, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
| 20090093631 | Processes for the preparation of a linezolid intermediate, linezolid hydroxide - Provided are methods for the enantiomeric purification of Linezolid hydroxide, comprising providing a solution or a slurry of Linezolid hydroxide and a solvent selected from alcohols and ketones and crystallizing Linezolid hydroxide from the solution or slurry to obtain Linezolid hydroxide with a low content of S isomer. | 04-09-2009 |
| 20090118502 | BIARYL HETEROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING THE SAME - The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents. | 05-07-2009 |
| 20090156806 | Process for the Preparation of Oxazolidinone Derivatives - A process for the preparation of oxazolidinone derivatives, in particular [(S)—N-[[3-(3-fluoro-4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]-acetamide] (linezolid), and novel intermediates useful for the synthesis thereof. | 06-18-2009 |
| 20100081807 | METHOD FOR PRODUCING 5-CLORO-N-(METHYL)-2-THIOPHENECARBOXAMIDE - The invention relates to a method for producing 5-chloro-N-({5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide starting from 5-chlorothiophene-2-carbonyl chloride, (2S)-3-amino-propane-1,2-diol and 4-(4-aminophenyl)-3-morpholinone. | 04-01-2010 |
| 20100240891 | DRUG CONTAINING BENZOPHENONE DERIVATIVE OR ITS SALT - Pharmaceutical agents characterized by containing benzophenone derivatives represented by the general formula: | 09-23-2010 |
| 20110275805 | METHOD FOR PREPARING LINEZOLID AND INTERMEDIATES THEREOF - A method for preparing the linezolid (compound 1), which comprises the steps of: (1) carrying out the debenzyl reaction of compound 4 in solvent, to obtain the compound 5 or its acetate; (2) carrying out the acetylation reaction in the amino of the compound 5 or its acetate obtained in step (1) in solvent to obtain the compound 1. The intermediates to prepare the compound 1 and the acetate of compound 5. The present preparation method is easy to obtain the chiral materials and the chiral materials are cheap, the process and the post treatment are simple, the intermediate products and the end product are easy to be purified, the total yield is high, their purities are also high, this preparation method is easy to be used in the industry manufacture. | 11-10-2011 |
| 20110288294 | Preparation process for an inhibitor of a blood clotting factor - The invention relates to a process for the preparation of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide (I) from 5-chlorothiophene-2-carboxylic acid and 4-[4-((S)-5-aminomethyl-2-oxooxazolidin-3-yl)phenyl]morpholin-3-one (II) | 11-24-2011 |
| 20120172592 | ACID ADDITION SALTS, HYDRATES AND POLYMORPHS OF 5-(2,4-DIHYDROXY-5-ISO-PROPYL-PHENYL)-4-(4-MORPHOLIN-4-YLMETHYL-PHENYL)-I- SOXAZOLE-3-CARBOXYLIC ACID ETHYLAMIDE AND FORMULATIONS COMPROSING THESE FORMS - The present invention relates to new salt forms of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide, in particular the mesylate, hydrochloride, tartrate, phosphate and hemi fumarate salt thereof; to crystalline forms of such salts; to polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide; to hydrates and polymorphs of the new salt forms mentioned above; to the use of the new salt forms mentioned above for the manufacture of a medicament for the treatment of a disorder mediated by Hsp90; to a method for treating a disorder mediated by Hsp90 using the new salt forms; to formulations comprising such salt forms, in particular aqueous solutions suitable for intravenous administration; and to amber glass containers being filled with such formulations. | 07-05-2012 |
| 20120283434 | PROCESS FOR THE PREPARATION OF RIVAROXABAN AND INTERMEDIATES THEREOF - A process for the preparation of rivaroxaban, or a pharmaceutically acceptable salt thereof, or a solvate thereof, including a hydrate, comprising submitting an amine compound of formula (III) wherein R | 11-08-2012 |
| 20130053557 | PROCESSES FOR PREPARING LINEZOLID - Processes and intermediates for preparing linezolid, and pharmaceutically acceptable salts thereof, are described herein. | 02-28-2013 |
| 20130072680 | PROCESSES FOR THE PREPARATION OF RIVAROXABAN AND INTERMEDIATES THEREOF - Provided are process for the preparation of (R)- and/or (S)-Rivaroxaban, and compounds which are intermediate compounds used in the processes for the preparation of (R)- and/or (S)-Rivaroxaban. | 03-21-2013 |
| 20130137864 | PROCESS FOR THE PREPARATION OF LINEZOLID - The present invention provides an improved process for the preparation of Linezolid of formula (D. The present invention relates to preparation of intermediate (R)—N-[[3-[3-fluoro-4-morpholinyl]phenyl|-2-oxo-5-oxazolidinyl]methanol of formula (II), Linezolid amine of formula (Ia) and their use in the preparation of Linezolid. The present invention further provides process for the preparation of Form I of Linezolid of formula (I). | 05-30-2013 |
| 20130172553 | CHIRAL SYNTHESIS OF ISOXAZOLINES, ISOXAZOLINE COMPOUNDS, AND USES THEREOF - Processes for the chiral syntheses of isoxazolines and intermediates are described. Compounds prepared thereby, and methods of using the compounds are also described. | 07-04-2013 |
| 20130172554 | PROCESSES FOR THE PREPARATION OF 4-MORPHOLIN-3-ONE - The present invention provides processes for the preparation of 4-{4-[5(S)-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one which are simple, eco-friendly, cost-effective, reproducible, robust and are well amenable on industrial scale. | 07-04-2013 |
| 20130184457 | METHOD FOR THE PREPARATION OF RIVORAXABAN - The present invention relates to the use of a compound having the formula (II) for the preparation of a compound having the formula (V). Methods of preparing the compound having the formula (V) using the compound having the formula (II) are also described. Individual reaction steps as well as intermediates are additionally claimed. | 07-18-2013 |
| 20130296556 | Acid Addition Salts, Hydrates and Polymorphs of 5-(2,4-Dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-is- oxazole-3-carboxylic Acid Ethylamide and Formulations Comprising These Forms - The present invention relates to new salt forms of | 11-07-2013 |
| 20130324719 | NOVEL PROCESS FOR PREPARATION OF LINEZOLID AND ITS NOVEL INTERMEDIATES - A novel process for preparing oxazolidinone antibacterial agent Linezolid including key intermediates of oxazolidinones comprising: reacting 3-fluoro-4-morpholinyl aniline with R-epichlorohydrin; carbonylation to form oxazolidinone derivative; acetylation of (5R)-5-(chloromethyl)-3-(3-fluoro-4-morpholinophenyl-oxazolidin-2-one with sodium acetate to get novel intermediate; hydrolysis of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl acetate; mesylation of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methanol; reaction of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl methane sulphonate with potassium phthalimide; hydrolysis of (S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl phthalimide with hydrazine hydrate; acetylation of (S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl amine with acetic anhydride yields Linezolid in high yield. | 12-05-2013 |
| 20130345419 | AZOLE DERIVATIVE - Provided are novel compounds that bind to FKBP12 or pharmaceutically acceptable salts thereof, as well as new therapeutics useful in the prevention or treatment of alopecia which comprise those compounds or pharmaceutically acceptable salts thereof. Specifically, compounds represented by formula (1) | 12-26-2013 |
| 20140024827 | LINEZOLID INTERMEDIATE AND METHOD FOR SYNTHESIZING LINEZOLID - Provided are a linezolid intermediate and the preparation method thereof and a method for synthesizing linezolid. The structure of the intermediate is shown as formula F2, wherein the compound is prepared by a condensation reaction of (S)—N—(3-chloro-2-hydroxy-1-propyl) acetamide and the compound shown in formula F4. In the preparation methods of the compound shown in formula F2 and linezolid, the reaction system is mild, side reactions are few and the product yield is high. | 01-23-2014 |
| 20140114065 | ANHYDROUS LINEZOLID CRYSTALLINE FORM-II - The present invention relates to oxazolidinone antibacterial agent anhydrous Linezolid crystalline Form-II. | 04-24-2014 |
| 20140114066 | NOVEL METHOD FOR SYNTHESIZING RIVAROXABAN INTERMEDIATE, 4-MORPHOLIN-3-ONE - The present invention discloses novel methods for synthesizing Rivaroxaban intermediate, i.e., 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3 -oxazolidin-3 -yl]phenyl}morpholin-3-one. The novel methods provided in the present invention involve mild reaction conditions, convenient operations, easy purification, and low production costs, and thus the process is environmental-friendly and suitable for industrial production. | 04-24-2014 |
| 20140128601 | PROCESS FOR OBTAINING RIVAROXABAN AND INTERMEDIATE THEREOF - This invention relates to a procedure for obtaining a thiophene-2-carboxamide compound, specifically rivaroxaban, which comprises the (i) fragmentation of the N═C bond of a compound of formula 23 where R1 is selected among hydrogen, halogen, and (C1-C6)alkyl; and (ii) acylation of the resulting intermediate with 5-chloro-tiofen-2-carbonyl chloride in a solvent medium, in the presence of a base. The invention also relates to the compounds of formula 23 and their use in the obtention of rivaroxaban. | 05-08-2014 |
| 20140142303 | PROCESS FOR THE PREPARATION OF A RIVAROXABAN AND INTERMEDIATES FORMED IN SAID PROCESS - The invention relates to a process for the preparation of 5-chloro-N-({(5-S)-2-oxo3-[4-(3-oxo-morj)holine-4-yl)-phenyl]-1,3-oxazolidine-5-yl}-methyl) thiophen-2-carboxamide having the INN rivaroxaban. The process is characterized by the reactions according to claim | 05-22-2014 |
| 20140171640 | 1,3-OXAZOLIDINE-2-ONE-LIKE COMPOUND, PREPARATION METHOD AND USES THEREOF - This invention provides 1,3-oxazolidin-2-one compounds of formula I and their salts, their preparation methods, and use in the preparation of linezolid racemate and its optical isomer, which are used as oxazolidinone antibacterial agents. In the formula, R is H, hydroxyl, halogen, C | 06-19-2014 |
| 20140378682 | PROCESSES AND INTERMEDIATES FOR PREPARING RIVAROXABAN - The invention discloses processes for the preparation of rivaroxaban and its pharmaceutically acceptable salts, solvates, and hydrates thereof. The invention also relates to novel intermediates for the preparation of rivaroxaban. | 12-25-2014 |
| 20150011756 | PROCESS FOR PREPARATION OF RIVAROXABAN AND INTERMEDIATES THEREOF - An improved process for the preparation of Rivaroxaban wherein the process substantially eliminates the potential impurities. process for preparation of Rivaroxaban which uses a novel intermediate. A process for preparing the novel intermediate which is used for the preparation of Rivaroxaban. | 01-08-2015 |
| 20150011757 | METHOD FOR PREPARING LINEZOLID INTERMEDIATE - Disclosed is a new method for preparing a methyl substitute of a linezolid intermediate, (S)-2-(3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazoline) (I), wherein the intermediate (I) is obtained by the cyclization of 3-fluoro-4-morpholinophenyl isocyanate (II) and epoxy compound (III). This process has a short process route, low cost, easy operation, and high yield, so is suitable for a large-scale industrial production. | 01-08-2015 |
| 20150025236 | PROCESS FOR THE PREPARATION OF STABLE CRYSTALLINE FORM-I OF LINEZOLID, SUBSTANTIALLY FREE OF RESIDUAL SOLVENT - The invention relates to a substantially pure linezolid hydroxide having R-isomer content more than about 99.9% relative to its S-isomer. Further aspect of invention provides the ambient moisture condition, which is critical for enantiomeric pure linezolid hydroxide. The obtained substantially enantiomerically pure linezolid hydroxide compound of formula-II can be subsequently converted into the linezolid compound of formula-I, having S-isomer content more than 99.9% relative to R-isomer. Further the invention provides an improved process for preparation of enantiomeric pure linezolid Form-I, wherein linezolid Form-I having the purity more than 99.9% relative to any other known polymorphic form of linezolid. The obtained enantiomeric pure linezolid Form-I can be subsequently converted into the other known polymorphic forms linezolid. The invention also provides stable and substantially solvent-free crystal of Form-I of linezolid. | 01-22-2015 |
| 20150038704 | METHOD FOR PREPARING RIVAROXABAN INTERMEDIATE - A method for preparing a Rivaroxaban intermediate I is presented, including the following step: in a non-protonic solvent, under the effect of lewis acid, performing cyclization reaction on 4-(4-phenyl isocyanate)morpholine-3-ketone (II) and (S)-epoxy compound (III), the reaction temperature ranging from 20° C. to 60° C., where R is amino replaced by amino protecting group. The preparation method of the present invention has a mild condition, a simple process, a low cost, and high efficiency; the product is easy to purify and the method is applicable to industrial production. | 02-05-2015 |
| 20150119571 | NEPRILYSIN INHIBITORS - In one aspect, the invention relates to compounds having the formula X: | 04-30-2015 |
| 20150126733 | IMPROVED PROCESS FOR PREPARING RIVAROXABAN USING NOVEL INTERMEDIATES - The present inventors have surprisingly found that rivaroxaban of formula I can be prepared in a one-pot process, in high purity and with high yield, by reacting 5-chlorothiophene-2-carboxylic acid or a salt thereof with a sulfonylating agent to produce a sulfonyl ester intermediate, which is then condensed with 4-[4-[(SS)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]morjJholine-3-one or an acid addition salt thereof to produce rivaroxaban. | 05-07-2015 |
| 20150133657 | PROCESS FOR THE PREPARATION OF RIVAROXABAN - The present invention provides processes for the preparation of rivaroxaban. The present invention also provides an intermediate for the preparation of rivaroxaban. | 05-14-2015 |
| 20150299160 | PROCESS FOR THE PREPARATION OF RIVAROXABAN AND INTERMEDIATES THEREOF - The present invention provides processes for the preparation of rivaroxaban and its intermediates. | 10-22-2015 |
| 20150299175 | RIVAROXABAN INTERMEDIATE AND PREPARATION THEREOF - This invention relates to novel intermediate, formula (A) for rivaroxaban and process for the preparation thereof. Further it extends to the process for preparation of rivaroxaban by using the said novel intermediate, by treating with 5-chlorothiophene carbonyl chloride to form the rivaroxaban derivatives of formula (B). The obtained formula (B) further treated with acid to form rivaroxaban. | 10-22-2015 |
| 20160024032 | PROCESSES FOR PREPARING LINEZOLID - Processes and intermediates for preparing linezolid, and pharmaceutically acceptable salts thereof, are described herein. | 01-28-2016 |
| 20160039803 | PROCESS FOR THE PREPARATION OF OXAZOLIDINONE DERIVATIVES - The present invention relates to an improved process for the preparation of Oxazolidinone derivatives. More specifically, the present invention relates to an improved process for preparing (S)-N-[[3-[3-fluoro-4-[4-morpholinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl]phthalimide, an intermediate used in the preparation of Oxazolidinone derivatives. | 02-11-2016 |
| 20160052919 | PROCESS FOR THE PREPARATION OF RIVAROXABAN - Disclosed is a process for the preparation of rivaroxaban and purifying rivaroxaban. | 02-25-2016 |
| 20160090393 | NEPRILYSIN INHIBITORS - In one aspect, the invention relates to compounds having the formula X: | 03-31-2016 |
| 20160102064 | IMPROVED PROCESSES FOR THE PREPARATION OF LINEZOLID USING NOVEL INTERMEDIATES - Provided herein are improved, commercially viable and industrially advantageous processes for the preparation of Linezolid, in high yield and purity, using novel intermediates. In one aspect, provided herein are efficient, industrially advantageous and environmentally friendly processes for the preparation of linezolid, in high yield and with high purity, using novel intermediates. The processes disclosed herein avoid the tedious and cumbersome procedures of the prior processes, thereby resolving the problems associated with the processes described in the prior art, which is more convenient to operate at lab scale and in commercial scale operations. | 04-14-2016 |
| 20160194309 | A Process For The Preparation Of Rivaroxaban | 07-07-2016 |
| 20160251342 | ALDEHYDE DERIVATIVE OF SUBSTITUTED OXAZOLIDINONES | 09-01-2016 |
| 544138000 | Oxadiazole ring (including hydrogenated) | 3 |
| 20100204470 | METHOD FOR SALT PREPARATION - The present invention provides a new method for preparation and crystallization of hydrochlorides, hydrobromides or hydroiodides of pharmaceutical compounds or their intermediates in which the base or its acid addition salt is reacted in a solvent with a Trialkylsilylhalogenide. | 08-12-2010 |
| 20130137865 | HETEROARYL-PYRAZOLE DERIVATIVE - A compound represented by formula [I] and a pharmaceutically accepted salt of said compound are a novel compound and a pharmaceutically accepted salt thereof which exert antagonistic activity against group II metabotropic glutamate (mGlu) receptors, and are effective as a novel preventive or therapeutic agent for disorders such as mood disorders (depressive disorder, bipolar disorder, etc.), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, a specific phobic disorder, acute stress disorder, etc.), schizophrenia, Alzheimer's disease, cognitive impairment, dementia, drug dependence, convulsions, shivering, pain, sleep disorders, and the like. | 05-30-2013 |
| 20150299149 | SELECTIVE SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS AND METHODS OF CHIRAL SYNTHESIS - Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated. | 10-22-2015 |
