| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 546133000 | Quinuclidines (including unsaturated) | 52 |
| 20080200681 | Processes for preparing palonosetron salts - The present invention provides processes for preparing Palonosetron salts, especially, the hydrochloride salt and intermediates used to prepare Palonosetron salts. | 08-21-2008 |
| 20080221330 | Mutilin-Derivative Substituted at Position 12 - A position 12-substituted mutilin derivative, a novel mutilin analogue, is provided that exhibits strong antimicrobial activity against abroad spectrum of Gram-positive or Gram-negative bacteria, including various drug-resistant bacteria, as well as intermediates for the production of such mutilin derivatives. | 09-11-2008 |
| 20090099364 | Process for preparation of 1-(2s,3s)-2-benzhydryl-n-(5- tert-butyl-2-methoxybenzyl)quinuclidin-3-amine - This invention relates to an improved process for the preparation of (2S,3S)-2-benzhydryl-N-(5-tent-butyl-2-methoxybenzyl)quinuclidin-3-amine, (hereinafter “compound of Formula I”) and its pharmaceutically acceptable salts. In particular, the invention is directed to an improved synthesis of the monohydrate citrate salt of the compound of Formula (Ia). | 04-16-2009 |
| 20090137810 | Synthetic Methods and Intermediates for Stereoisomeric Compounds Useful for the Treatment of Gastrointestinal and Central Nervous System Disorders - The subject invention provides methods and/or processes for making stereoisomeric compounds of formula (X): | 05-28-2009 |
| 20090198064 | Process for preparing quinuclidinium carbamate derivatives - A new process for preparing carbamate derivatives having the structure of formula (I) | 08-06-2009 |
| 20100174080 | NOVEL PALONOSETRON SALTS AND PROCESSES FOR PREPARATION AND PURIFICATION THEREOF - Provided are novel salts of 2-(1-azabicyclo-[2.2.2]oct-3-yl)-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one, methods of using such salts, and processes for producing such salts | 07-08-2010 |
| 20100249420 | Process for preparing quinuclidinium carbamate derivatives - A new process for preparing carbamate derivatives having the structure of formula (I) | 09-30-2010 |
| 20110172428 | METHODS FOR THE PREPARATION OF INDAZOLE-3-CARBOXYLIC ACID AND N-(S)-1-AZABICYCLO[2.2.2]OCT-3-YL-1H-INDAZOLE-3-CARBOXAMIDE HYDROCHLORIDE SALT - The present invention provides novel methods for preparing indazole-3-carboxylic acid 2, a key starting material for the manufacture of agonists or partial agonists of the nicotinic α-7 receptor, such as N—(S)-1-azabicyclo[2.2.2]oct-3-yl-1H-indazole-3-carboxamide HCl salt 13. Nicotinic α-7 receptor agonists and partial agonists are being useful in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing indazole-3-carboxylic acid on scaled-up levels. | 07-14-2011 |
| 20110263859 | (2S, 3R)-N-(2-((3-PYRIDINYL)METHYL)-1-AZABICYCLO[2.2.2]OCT-3-YL)BENZOFURAN- -2-CARBOXAMIDE, NOVEL SALT FORMS, AND METHODS OF USE THEREOF - The present invention relates to (2S,3R)-N-(2((3-pyridiny)triethyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2-carboxamide, novel salt forms thereof, methods for its preparation, novel intermediates, and methods for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central and autonomic nervous systems. | 10-27-2011 |
| 20120088917 | NEW QUINUCLIDINE DERIVATIVE USEFUL IN THE PREPARATION OF MEQUITAZINE - The invention relates to a 1-aza-bicyclo [2.2.2] oct-2-en-3-ylmethyl acetate of the formula (I), wherein said compound is useful as a synthesis intermediate for the production of mequitazine. | 04-12-2012 |
| 20120259120 | DIAZONIUM-FREE METHOD TO MAKE AN INDAZOLE INTERMEDIATE IN THE SYNTHESIS OF BICYCLIC 5-(TRIFLUORMETHOXY)-1H-3-INDAZOLECARBOXYLIC ACID AMIDES - The present invention provides novel methods for preparing 5-(trifluoromethoxy)-1H-3-indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5-trifluoromethoxy-1H-indazole-3-carboxylic acid amides of Formula (1). Compounds of Formula (1) are active as agonists and partial agonists of the nicotinic α-7 receptor and are being studied for their use in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing compound (3) on scale up levels. | 10-11-2012 |
| 20130060039 | AZABICYCLIC CARBAMATES AND THEIR USE AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR AGONISTS - The invention relates to novel benzothiophene-, benzofuran-, and indole ureas and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning, and/or memory. | 03-07-2013 |
| 20150031891 | BIS-QUARTERNARY CINCHONA ALKALOID SALTS AS ASYMMETRIC PHASE TRANSFER CATALYSTS - The invention is directed to novel bis-quarternary cinchona alkaloid salts and the use of bis-quarternary cinchona alkaloid salts in asymmetric phase transfer catalysis. The present invention is directed to novel bis-quarternary cinchona alkaloid salts and the use of bis-quarternary cinchona alkaloid salts in asymmetric phase transfer catalysis. On certain substrates and under specific reaction conditions, the inventors have discovered that the use of bis-quarternary cinchona alkaloid salts in asymmetric phase transfer catalysis surprisingly provides for a more active and efficient process as compared to mono-quarternary catalysts. | 01-29-2015 |
| 20160159786 | CHEMICAL PROCESS - The present invention relates to a process for the preparation of umeclidinium bromide, and to processes for preparing intermediates used in the preparation of umeclidinium bromide. | 06-09-2016 |
| 546134000 | Quinoline containing (including hydrogenated) | 19 |
| 20080287680 | Solifenacin Succinate-Containing Composition - A solifenacin succinate-containing composition with less impurities which can be used as a bulk for pharmaceutical is provided. | 11-20-2008 |
| 20090099365 | Processes for solifenacin preparation - Processes for preparing solifenacin comprising distilling ethanol and organic solvent from a reaction mixture and recycling the organic solvent are described. Also described are processes for reducing solifenacin diastereomeric and enantiomeric impurities. | 04-16-2009 |
| 20090203913 | Asymmetric Friedel-Crafts Alkylations Catalyzed By Bifunctional Cinchona Alkaloids - In certain embodiments, the present invention relates to methods for asymmetric Friedel-Crafts alkylation catalyzed by bifunctional cinchona alkaloids. In certain embodiments, the catalyst is a 6′-OH cinchona alkaloid. In certain embodiments, the electrophile is an α-ketoester or aldehyde. In certain embodiments, the nucleophile is an aromatic heterocycle. In certain embodiments, the nucleophile is an aromatic N-containing heterocycle. In certain embodiments, the nucleophile is an indole. In certain embodiments, the methods of the invention are relatively insensitive to concentration, temperature, air and moisture. | 08-13-2009 |
| 20090203914 | PROCESS FOR THE PREPARATION OF SOLIFENACIN - A process for the preparation of (1S)-QR)-I -azabicyclo[2.2.2.]oct-3-yl 3,4-dihydro-1-phenyl- 2(1H)-isoquino-line carboxylate by reacting (1S)-alkyl 1-phenyl-1,2,3,4-tetrahydro-2-isoquinoline carboxylate with 3-(R)-quinuclidol in an inert solvent, where a primary alkyl ester of the carboxylate whose alkyl length is C | 08-13-2009 |
| 20090203915 | Process for the preparation of solifenacin - A process for the preparation of (1S,3′R)-quiniclidin-3′-yl-1-phenyl-3,4-dihydro-1H-isoquinolin-2-carboxylate, namely solifenacin, comprising the reaction of a compound of formula (IV) with a compound of formula (V), as herein defined, | 08-13-2009 |
| 20110257403 | Processes and Intermediates for Preparing a Macrocyclic Protease Inhibitor of HCV - The present invention relates to the cinchonidine salt | 10-20-2011 |
| 20110295011 | Conjugate Addition Reactions Using Bifunctional Cinchona-Alkaloid-Based Catalysts - One aspect of the present invention relates to quinine-based and quinidine-based catalysts. Another aspect of the present invention relates to a method of preparing a chiral, non-racemic compound from a prochiral electron-deficient alkene, comprising the step of: reacting a prochiral electron-deficient alkene with a nucleophile in the presence of a catalyst; thereby producing a chiral, non-racemic compound; wherein said catalyst is a derivatized quinine or quinidine. | 12-01-2011 |
| 20110319621 | METHOD FOR THE PREPARATION OF SOLIFENACIN AND INTERMEDIATE THEREOF - A method for the preparation of solifenacin by reacting quinuclidin-3-ol and bis(aryl) carbonate to form (3R)-1-azabicyclo[2.2.2]oct-3-yl 4-aryl carbonate of formula (IVa); and treating (3R)-1-azabicyclo[2.2.2]oct-3-yl 4-aryl carbonate of formula (IVa) with (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline of formula (V) in an inert atmosphere to form a Solifenacin base, which is converted into its pharmaceutically acceptable salts. The invention also provides a compound, (3R)-1-azabicyclo[2.2.2]oct-3-yl 4-aryl carbonate of formula (IVa), which is used as an intermediate for the preparation of Solifenacin base and a process for the preparation thereof. | 12-29-2011 |
| 20120029197 | Method for Preparing Sulfur-Containing Compounds - The invention provides a method for preparing sulfur-containing compounds, the method comprising reacting a donor compound comprising at least one sulfur having at least one lone pair of electrons, with an acceptor compound; wherein the reaction occurs in the presence of an amine, optionally an amine catalyst, capable of activating the sulfur having at least one lone pair of electrons; and wherein the reaction occurs via the formation of an transient intermediate species, optionally a transient intermediate species, between the amine, optionally the amine catalyst and the donor compound; and wherein the donor compound is selected from the group consisting of a sulfurous acid, a sulfenic acid and a sulfinic acid or a salt, ester or amide of a sulfurous acid, a sulfenic acid and a sulfinic acid. The invention also provides sulfur-containing compounds of the formula: wherein R is selected from: (a) 1-(4-Nitro-phenyl)-3-oxo-3-phenyl-propane; (b) 2-(3-Methyl-4-nitro-isoxazol-5-yl)-1-phenyl-ethane; (c) 1-(4-Methoxy-phenyl)-2-(3-methyl-4-nitro-isoxazol-5-yl)-ethane; (d) 2-(3-Methyl-4-nitro-isoxazol-5-yl)-1-(4-nitro-phenyl)-ethane; (e) 1-(4-Fluoro-phenyl)-2-(3-methyl-4-nitro-isoxazol-5-yl)-ethane; (f) 1-(4-Chloro-phenyl)-2-(3-methyl-4-nitro-isoxazol-5-yl)-ethane; and (g) 3-Oxo-cyclohexane. Finally, the invention provides use of chiral sulfur-containing compounds obtainable by the above-mentioned method or chiral sulfur-containing compounds as mentioned above for the resolution of racemic mixtures of amines. | 02-02-2012 |
| 20120046468 | INTERMEDIATES IN THE ENANTIOSELECTIVE SYNTHESIS OF 3-(AMINOMETHYL)-5-METHYL-HEXANOIC ACID - (S)-(+)-3-(aminomethyl)-5-methyl-hexanoic acid or (S)-pregabalin is an anticonvulsive drug. In addition to its use as an anticonvulsive agent, pregabalin has also been indicated as a medicament in the treatment of anxiety, neuropathic pain and pain in patients with fibromyalgia. Provided herein are thioester intermediates in the synthesis of and processes for the synthesis of 3-(aminomethyl)-5-methyl-hexanoic acid in the (R) or (S) configuration. | 02-23-2012 |
| 20120277437 | KINETIC RESOLUTION - Whilst methodologies for the Kinetic Resolution of alcohols are well established, no analogous direct methods exist for the highly selective, direct catalytic Kinetic Resolution of thiols (i.e., R—SH). The present invention relates to a method for resolving stereoisomeric mixtures of thiols. In particular, the present invention relates to purely organocatalytic mediated resolution of enantiomeric mixtures of thiols without the need for enzymes. Also disclosed are some novel catalysts. Such catalysts may comprise a cinchona alkaloid-derived moiety. | 11-01-2012 |
| 20130144062 | HETEROARYL CARBOXAMIDES - The invention relates to novel heteroaryl carboxamides, a process for their preparation, and pharmaceutical compositions containing them. These materials are useful for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory. | 06-06-2013 |
| 20140249313 | Conjugate Addition Reactions Using Bifunctional Cinchona-Alkaloid-Based Catalysts - One aspect of the present invention relates to quinine-based and quinidine-based catalysts. Another aspect of the present invention relates to a method of preparing a chiral, non-racemic compound from a prochiral electron-deficient alkene, comprising the step of: reacting a prochiral electron-deficient alkene with a nucleophile in the presence of a catalyst; thereby producing a chiral, non-racemic compound; wherein said catalyst is a derivatized quinine or quinidine. | 09-04-2014 |
| 20140296527 | PROCESSES FOR THE PREPARATION OF PYRROLIDINE INTERMEDIATES - The present invention relates to processes for the enantio-selective preparation of spyrrolidine derivatives useful in the manufacture of pesticidally active compounds, as well as to intermediates in the processes. The processes include those comprising | 10-02-2014 |
| 20140350261 | METHOD FOR CATALYTIC ASYMMETRIC SYNTHESIS OF OPTICALLY ACTIVE ISOXAZOLINE COMPOUND, AND OPTICALLY ACTIVE ISOXAZOLINE COMPOUND - There is provided a method for catalytic asymmetric synthesis of optically active isoxazoline compound and an optically active isoxazoline compound. A method for catalytic asymmetric synthesis of optically active isoxazoline compound of a formula (6) including reacting an α,β-unsaturated carbonyl compound of a formula (1) and a hydroxylamine in a solvent in the presence of a base by adding a chiral phase transfer catalyst. An optically active isoxazoline compound of a formula (13) that can be synthesized by the method. | 11-27-2014 |
| 20150080577 | Processes and Intermediates for Preparing a Macrocyclic Protease Inhibitor of HCV - The present invention relates to the cinchonidine salt | 03-19-2015 |
| 546135000 | Additional hetero ring containing | 1 |
| 20120004412 | METHODS FOR THE PREPARATION OF N-(S)-1-AZABICYCLO[2.2.2]OCT-3-YL-1H-INDAZOLE-3-CARBOXAMIDE HYDROCHLORIDE SALT - The present invention provides novel methods for preparing N—(S)-1-azabicyclo[2.2.2]oct-3-yl-1H-indazole-3-carboxamide HCl salt 1, a nicotinic α-7 receptor ligand, that are useful for the scaled-up preparation of compound 1. Compound 1 is useful in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. | 01-05-2012 |
| 546136000 | Three or more chalcogens attached indirectly to the quinuclidine ring system by nonionic bonding | 2 |
| 20110213151 | CINCHONA-BASED BIFUNCTIONAL ORGANOCATALYSTS AND METHOD FOR PREPARING CHIRAL HEMIESTERS USING THE SAME - The present invention relates to cinchona-based bifunctional organocatalysts and methods for preparing chiral hemiesters using the same. More specifically, the present invention relates to methods for preparing chiral hemiesters from prochiral or meso cyclic acid anhydrides via desymmetrization, using bifunctional cinchona alkaloid catalysts comprising sulfonamide functional groups. | 09-01-2011 |
| 20130245268 | ENANTIOSELECTIVE ORGANIC ANHYDRIDE REACTIONS - Disclosed herein is enantioselective synthetic method comprising reacting an enolisable C | 09-19-2013 |
| 546137000 | Chalcogen bonded directly to ring carbon of the quinuclidine ring system | 19 |
| 20080221331 | ALCOHOL OXIDATION CATALYST AND ITS PREPARATION PROCESS - An alcohol oxidation catalyst which is an organic oxidation catalyst to oxidize an alcohol, which contains azabicyclo [3.3.1]nonane N-oxyl represented by the following formula (1) having an N-oxyl group incorporated in a bicycle[3.3.1]nonane skeleton: | 09-11-2008 |
| 20080249312 | Process for the preparation of 2-methylspiro(1,3-oxathiolane-5,3')quiniclidine - An industrially acceptable process for the preparation of 2-methylspiro(1,3-oxathiolane-5,3′)quiniclidine. The cis-isomer of 2-methylspiro(1,3-oxathiolane-5,3′)quiniclidine is known generally as Cevimeline. | 10-09-2008 |
| 20090326230 | PROCESS FOR PREPARING SOLIFENACIN AND ITS SALTS - The present invention relates to solifenacin in solid form and a process for its preparation and to a process for the preparation of (1S)-1-Phenyl-1,2,3,4-tetrahydro-isoquinoline, a key intermediate in the synthesis of solifenacin and its salts. | 12-31-2009 |
| 20100029944 | Process for the Synthesis of Solifenacin - This invention provides improved methods for making solifenacin and pharmaceutically acceptable salts thereof. The instant methods are unexpectedly advantageous in their simplicity and efficiency. | 02-04-2010 |
| 20100145055 | METHOD FOR THE PREPARATION OF SOLIFENACIN - A method of preparing (1S)-(3R)-1-azabicyclo[2.2.2]oct-3-yl 3,4-dihydro-1-phenyl-2(1H)-isoquinoline carboxylate (solifenacin) or its pharmaceutically acceptable salts with high optic purity, wherein the crude solifenacin base is transformed to the hydrogen tartrate, which is then optionally transformed to another pharmaceutically acceptable salt or the base of solifenacin. A crystalline salt of solifenacin hydrogen tartrate. | 06-10-2010 |
| 20100174081 | PRODUCTION PROCESS OF OPTICALLY ACTIVE 3-QUINUCLIDINOL DERIVATIVE - A process is provided for efficiently producing an optically active 3-quinuclidinol derivative of high optical purity using a readily available ruthenium compound as an asymmetric reduction catalyst. This process is a process for producing an optically active 3-quinuclidinol derivative represented by the following formula (III) comprising asymmetrically hydrogenating a 3-quinuclidinone derivative represented by the following formula (I) in the presence of a ruthenium compound (II) represented by formula (II): Ru(X)(Y)(Px) | 07-08-2010 |
| 20110028725 | Preparation and Use of Alkylating Agents - The present disclosure provides methods of synthesizing alkylating agents and methods of use. | 02-03-2011 |
| 20110065922 | Process for Preparation Of Solifenacin and/or the Pharmaceutically Acceptable Salts Thereof of High Pharmaceutical Purity - A process for the preparation of solifenacin and/or the pharmaceutically acceptable salts thereof of high pharmaceutical purity is characterized in that 3-(R)-quinuclidinoloxy anion generated in situ from 3-(R)-quinuclidinol in a presence of strong base in polar organic solvent is subject to acylation with (S)-1-phenyl-1,2,3,4-tetrahydroisoquinolinecarbonyl chloride of chemical purity at least 98%, while maintaining constant anion excess in a reaction mixture, and after reaction completion solifenacin base is optionally transformed into solifenacin salt according to standard procedures. (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinolinecarbonyl chloride of chemical purity at least 98% is obtained in a reaction of (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline and molar excess of phosgene in a presence of tertiary aromatic amine in aromatic hydrocarbon, and isolated in a crystalline form. | 03-17-2011 |
| 20110077405 | PROCESS FOR PREPARATION OF ENANTIOMERICALLY PURE (S)-1-PHENYI-1,2,3,4- TETRAHYDROISOQUINOLINE - Process for preparation of (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline wherein 1-phenyl-1,2,3,4-tetrahydroisoquinoline is reacted with D-(−)-tartaric acid in a solvent system comprising of methanol and water, preferably at 3.3:1 to 1:1 volume ratio, the crystallization mixture is left for crystallization and (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline is released from obtained crystalline diastereoisomeric salt according to standard procedures. (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline is the intermediate in enantiomeric synthesis of solifenacin. | 03-31-2011 |
| 20120004413 | ISOTOPICALLY LABELED CHEMICALLY STABLE REAGENTS AND PROCESS FOR THE SYNTHESIS THEREOF - A radioisotope labeled reagent includes a compound having the general formula (I), | 01-05-2012 |
| 20130030184 | ISOTOPICALLY LABELED CHEMICALLY STABLE REAGENTS AND PROCESS FOR THE SYNTHESIS THEREOF - A radioisotope labeled reagent includes a compound having the general formula (I), | 01-31-2013 |
| 20130123502 | NOVEL PROCESS FOR THE PREPARATION OF SOLIFENACIN SUCCINATE - The present invention relates to a process for the preparation of Solifenacin succinate by condensing a compound of formula (IVb) with (RS)-3-quinuclidinol, wherein, R represents methyl, ethyl, isopropyl; to produce a diastereomeric mixture of (1S)-3,4-dihydro-1-phenyl-2(1H)-isoquinolinecarboxylic acid (3RS)-1-azabicyclo[2.2.2]oct-3-yl ester, which is treated with succinic acid in a solvent or mixture of solvents to produce optically pure Solifenacin succinate, Formula (X). | 05-16-2013 |
| 20130225824 | PRODUCTION PROCESS OF OPTICALLY ACTIVE 3-QUINUCLIDINOL DERIVATIVE - A process is provided for efficiently producing an optically active 3-quinuclidinol derivative of high optical purity using a readily available ruthenium compound as an asymmetric reduction catalyst. This process is a process for producing an optically active 3-quinuclidinol derivative represented by the following formula (III) comprising asymmetrically hydrogenating a 3-quinuclidinone derivative represented by the following formula (I) in the presence of a ruthenium compound (II) represented by formula (II): Ru(X)(Y)(P | 08-29-2013 |
| 20140303374 | METHOD FOR PRODUCING COMPOUND WITH CARBONYL GROUP BY USING RUTHENIUM CARBONYL COMPLEX HAVING TRIDENTATE LIGAND AS DEHYDROGENATION OXIDATION CATALYST - Provided by the present invention is a method for efficient oxidation of alcohols by using, as a catalyst for dehydrogenation oxidation, a ruthenium complex which can be easily produced and easily handled and is obtainable at a relatively low cost. The invention relates to a method of producing a compound having a carbonyl group by dehydrogenation oxidation of alcohols by using as a catalyst the ruthenium carbonyl complex represented by the following general formula (1) RuXY(CO)(L) (1) (in the general formula (1), X and Y may be the same or different from each other and represent an anionic ligand, and L represents a tridentate aminodiphosphine ligand). | 10-09-2014 |
| 20140371460 | GLUCOSYLCERAMIDE SYNTHASE INHIBITORS - The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer. | 12-18-2014 |
| 20150087841 | SYNTHESIS OF MSE-FRAMEWORK TYPE MOLECULAR SIEVES - A method of synthesizing a crystalline molecular sieve having an MSE framework type comprises crystallizing a reaction mixture comprising a source of water, a source of an oxide of a tetravalent element, Y, selected from at least one of silicon, tin, titanium, vanadium, and germanium, optionally a source of a trivalent element, X, a source of an alkali or alkaline earth metal, M, and a source of organic dications, Q, such as 3-hydroxy-1-(4-(1-methylpiperidin-1-ium-1-yl)butyl)quinuclidin-1-ium, 3-hydroxy-1-(5-(1-methylpiperidin-1-ium-1-yl)pentyl)quinuclidin-1-ium, 1,1′-(butane-1,4-diyl)bis(1-methylpiperidin-1-ium), 1,1′-(pentane-1,5-diyl)bis(1-methylpiperidin-1-ium), 1,1′-(hexane-1,6-diyl)bis(1-methylpiperidin-1-ium), and 1,1′-((3as,6as)-octahydropentalene-2,5-diyl)bis(1-methylpiperidin-1-ium). | 03-26-2015 |
| 20150112072 | PROCESS OF PREPARING SOLIFENACIN OR SALT THEREOF, AND NOVEL INTERMEDIATE USED IN THE PROCESS - Disclosed herein is a method of preparing solifenacin or a salt thereof, including the steps of: (a) reacting (R)-quinuclidinol with bis(pentafluorophenyl)carbonate in an organic solvent to prepare a solifenacin intermediate, (3R)-1-azabicyclo[2,2,2]oct-3-yl pentafluorophenylcarbonate, and (b) reacting the solifenacin intermediate with (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline in an organic solvent to prepare solifenacin. The method is advantageous in that high-purity solifenacin or a salt thereof can be simply and efficiently prepared with high yield using a novel intermediate. | 04-23-2015 |
| 20160039805 | SALT FORMS OF (S)-QUINUCLIDIN-3-YL (2-(2-(4-FLUOROPHENYL)THIAZOL-4-YL)PROPAN-2-YL)CARBAMATE - The present invention relates to novel salt forms of (S)-Quinuclidin-3-yl(2-(2-(4-fluorophenyl)thiazol-4-yl)propan-2-yl)carbamate useful as an inhibitor of glucosylceramide synthase (GCS) and for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer. | 02-11-2016 |
| 20160039806 | METHOD OF PREPARING GLUCOSYLCERAMIDE SYNTHASE INHIBITORS - The invention relates to a method of preparing inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer. | 02-11-2016 |
