Class / Patent application number | Description | Number of patent applications / Date published |
548537000 | Acyclic nitrogen bonded directly to the -C(=X)- (e.g., 4,5-dihalopyrrole -2 carboxamides, etc.) | 44 |
20080287690 | Process For (3R, 5R)-7-[2-(4-Fluorophenyl)-5-Isopropyl-3-Phenyl-4- [(4-Hydroxy Methyl Phenyl Amino) Carbonyl]-Pyrrol-1-Yl]-3,5-Dihydroxy-Heptanoic Acid Hemi Calcium Salt - The present invention relates to processes for the manufacture of (3R, 5R)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-[(4-hydroxy methyl phenyl amino)carbonyl]-pyrrol-1-yl]-3,5-dihydroxy-heptanoic acid hemi calcium salt. | 11-20-2008 |
20080287691 | Polymorphic form of atorvastatin calcium - The present invention relates to atorvastatin calcium, a useful agent for lowering serum cholesterol levels. New atorvastatin calcium Form V, processes for preparing the new form, and pharmaceutical compositions and dosage forms containing the new form are disclosed. | 11-20-2008 |
20080306282 | Novel Forms of [R-(R*,R*)]-2-(4-Fluorophenyl)-Beta,Delta-Dihydroxy-5-(1-Methylethyl)-3-Phenyl-4-[(Phenylamino)Carbonyl]-1H-Pyrrole-1-HeptanoicAcid Calcium Salt (2:1) - Novel forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt designated Form XX, Form XXI, Form XXII, Form XXIII, Form XXIV, Form XXV, Form XXVI, Form XXVII, Form XXVIII, Form XXIX, and Form XXX, characterized by their X-ray powder diffraction, solid-state NMR, and/or Raman spectroscopy are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease. | 12-11-2008 |
20080312457 | Process - The present invention relates to a new process for the resolution of mandelic acid derivatives from racemic mandelic acid derivative mixtures by salt formation with chiral base cyclic amides; to the resolved mandelic acid cyclic amide salts (see, for example, formula IIa), as well as certain other metal and amine salts of the mandelic acid derivatives, and to the use of the resolved mandelic acid derivatives as intermediates suitable for large-scale manufacturing of, for example, pharmaceutical compounds; Formula IIa, wherein R is selected from CHF2, H, C1-6 Alkyl, CH2F, CHCl2 and CClF2; and wherein n is 0, 1 or 2; R1 is H or C1-6 Alkyl and X is H, halo or C1-6 Alkyl. | 12-18-2008 |
20090012312 | Process for Preparing Pyrrole Derivatives and Intermediates -
The present invention relates to a process for preparing pyrrole derivatives of a class that is effective at inhibiting the biosynthesis of cholesterol in humans, and more particularly to improved synthetic methods for preparing 3,5-dihydroxy-7-pyrrol-1-yl heptanoic acids from 1,4-diketo starting materials. The invention further relates to intermediates in this process formula (I). | 01-08-2009 |
20090048453 | Salt forms of [R-(R*,R*)]-2-(4-fluorophenyl)-beta, delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-p- yrrole-1-heptanoic acid - Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease. | 02-19-2009 |
20090099371 | PROCESS FOR THE PREPARATION OF AMORPHOUS ATORVASTATIN CALCIUM SALT - Disclosed is a novel process for preparing pure amorphous form of Atorvastatin employing a suitable solvent system selected from water, water-miscible solvents or water-immiscible solvents or a mixture thereof. | 04-16-2009 |
20090118520 | PROCESS FOR PREPARATION OF (3R, 5R)-7-[2-(4-FLUOROPHENYL)-5-ISOPROPYL-3-PHENYL-4-[(4-HYDROXY METHYL PHENYL AMINO) CARBONYL]-PYRROL-1-YL]-3,5-DIHYDROXY-HEPTANOIC ACID HEMI CALCIUM SALT - The present invention relates to processes for the preparation of (3R, 5R)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-[(4-hydroxy methyl phenyl amino)carbonyl]-pyrrol-1-yl]-3,5-dihydroxy-heptanoic acid hemi calcium salt. | 05-07-2009 |
20090124817 | Process for Preparing Amorphous Atorvastatin Calcium Nanoparticles - The present invention relates to a method of preparing amorphous atorvastatin calcium nanoparticles using a supercritical fluid process. Specifically, the method comprising the steps of: a) dissolving atorvastatin calcium in an organic solvent with/without a hydrophilic additive to prepare a drug solution; b) introducing the drug solution and carbon dioxide into a reactor, which maintains carbon dioxide at supercritical conditions, to produce atorvastatin calcium particles; and c) introducing carbon dioxide into the reactor to wash the particles through removal of the remaining organic solvent. The amorphous atorvastatin calcium prepared according to the method of the present invention has a particle size of nanometer order, large surface area and high solubility shows improved bioavailability, and thus can be formulated as various preparations for oral administration. | 05-14-2009 |
20090131683 | Process for the preparation of atorvastatin and intermediates - A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 comprising:
| 05-21-2009 |
20090171099 | PROCESS FOR THE PRODUCTION OF AMORPHOUS ATORVASTATIN CALCIUM - A novel process of the preparation of amorphous atorvastatin calcium starting from a compound of Formula (II). | 07-02-2009 |
20090171100 | METHOD FOR PREPARING ENANTIOMERICALLY PURE 4-PYRROLIDINO PHENYLBENZYL ETHER DERIVATIVES - The invention relates to a method for preparing enantiomerically pure 4-pyrrolidinophenylbenzyl ether derivatives of formula I: | 07-02-2009 |
20090216029 | PROCESS FOR THE PRODUCTION OF ATORVASTATIN CALCIUM IN AMORPHOUS FORM - A process for the production of amorphous atorvastatin calcium and stabilized, amorphous atorvastatin calcium is provided. | 08-27-2009 |
20090240064 | CRYSTALLINE FORM OF ATORVASTATIN HEMI-CALCIUM - The present invention relates to a new crystalline form of Atorvastatin hemi-calcium and also relates to a process for preparation of the same by treating Atorvastatin hemi-calcium amorphous form or form-I or mixture of amorphous and crystalline forms with methanol. | 09-24-2009 |
20090292129 | PROCESS FOR RESOLVING RACEMIC MIXTURES AND A DIASTEREOISOMERIC COMPLEX OF A RESOLVING AGENT AND AN ENANTIOMER OF INTEREST - A process for resolving a compound in racemic form comprising the following steps is described: a) reacting a compound in racemic form with a resolving agent, b) forming a diastereoisomeric complex of the resolving agent and an enantiomer of interest, c) separating the enantiomer of interest from the obtained diastereoisomer, wherein such a process is characterized in that said resolving agent is a compound of Formula (I). A diastereoisomeric complex between the resolving agent of Formula (I) and the enantiomer of interest is also described. The process according to the invention allows acid and basic racemic mixtures to be separated. | 11-26-2009 |
20100113802 | PROCESS FOR PREPARING AMORPHOUS ATORVASTATIN HEMI CALCIUM SALT AND ITS ITERMEDIATE - The invention relates to the HMG-CoA reductase inhibitor in particular to Atorvastatin Hemi-calcium. The present invention is directed to novel processes for preparing amorphous form of Atorvastatin hemi calcium and their intermediate in high purity. | 05-06-2010 |
20100190999 | PROCESS FOR THE PREPARATION OF AMORPHOUS ATORVASTATIN CALCIUM - The present invention also provides the amorphous form of hemi-calcium salt of atorvastatin with high purity and processes for preparation thereof. | 07-29-2010 |
20100197941 | Process for the production of atorvastatin calcium in amorphous form - A process for the production of amorphous atorvastatin calcium and stabilized, amorphous atorvastatin calcium is provided. | 08-05-2010 |
20110065931 | ATORVASTATIN CALCIUM PROPYLENE GLYCOL SOLVATES - Atorvastatin calcium propylene glycol solvates and processes to prepare these novel solvates which are particularly useful and suitable for pharmaceutical applications. | 03-17-2011 |
20110172443 | Salt Forms of [R-(R*,R*)]-2-(4-Fluorophenyl)-beta, alpha-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-p- yrrole-1-Heptanoic Acid - Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease. | 07-14-2011 |
20110218343 | SMALL MOLECULE INHIBITORS OF ROTAMASE ENZYME ACTIVITY - This invention relates to neurotrophic compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity. | 09-08-2011 |
20110301358 | Novel Forms of [R-(R*,R*)]-2-(4-fluorophenyl)-beta,delta-Dihydroxy-5-(1-Methylethyl)-3-P- henyl-4-[(Phenylmino)Carbonyl]-1H-Pyrrole-1-Heptanoic Acid Calcium Salt (2:1) - Novel forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt designated Form XX, Form XXI, Form XXII, Form XXIII, Form XXIV, Form XXVV, Form XXVI, Form XXVII, Form XXVIII, Form XXIX, and Form XXX, characterized by their X-ray powder diffraction, solid-state NMR, and/or Raman spectroscopy are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPII) and Alzheimer's disease. | 12-08-2011 |
20110319636 | METHOD FOR PREPARATION OF AMIDES FROM ALCOHOLS AND AMINES BY EXTRUSION OF HYDROGEN - The present invention relates to a method for preparation of carboxamides using alcohols and amines as starting materials in a dehydrogenative coupling reaction catalyzed by a ruthenium N-heterocyciic carbene (NHC) complex, which may be prepared in situ. | 12-29-2011 |
20120016135 | FURANOSE DERIVATIVES - The invention relates to a process for preparing furanose derivatives, to furanose intermediates used in said process and to the use of said derivatives in the manufacture of atorvastatin. | 01-19-2012 |
20120029207 | Novel Crystalline Form of Atorvastatin Hemi-calcium Salt, Hydrate Thereof, And Method of Producing The Same - The present invention provides a novel crystalline form of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-mthylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-heptanoic acid hemi-calcium salt (atorvastatin hemi-calcium salt) of the following formula 1, which is known to be useful as a drug, a hydrate thereof and a preparation method thereof: | 02-02-2012 |
20120029208 | PROCESS FOR (3R, 5R)-7-[2-(4-FLUOROPHENYL)-5-ISOPROPYL-3-PHENYL-4- [(4-HYDROXY METHYL PHENYL AMINO) CARBONYL]-PYRROL-1-YL]-3, 5-DIHYDROXY-HEPTANOIC ACID HEMI CALCIUM SALT - The present invention relates to processes for the manufacture of (3R,5R)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-[(4-hydroxy methyl phenyl amino)carbonyl]-pyrrol- | 02-02-2012 |
20120123132 | NOVEL CRYSTALLINE FORM OF ATORVASTATIN HEMI-CALCIUM SALT, HYDRATE THEREOF, AND METHOD OF PRODUCING THE SAME - The present invention provides a novel crystalline form of [R-(R | 05-17-2012 |
20120226053 | PROCESS FOR PREPARING ALPHA-CARBOXAMIDE DERIVATIVES - The present application provides a process for the preparation of α-carboxamide pyrrolidine derivatives of formula (I), wherein R | 09-06-2012 |
20130041162 | PRODUCTION OF ATORVASTATIN LOW IN ETHER IMPURITIES - The present invention relates to a method for the production of atorvastatin having decreased levels of impurities of general formulae (3) and (4) by means of a concentrating step. | 02-14-2013 |
20130041163 | PRODUCTION OF ATORVASTATIN LOW IN LACTONE IMPURITIES - The present invention relates to a method for the production of atorvastatin having decreased levels of impurity (3) by means of a pH-controlling step. | 02-14-2013 |
20130053577 | ANTIVIRAL COMPOUNDS - The invention 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. | 02-28-2013 |
20130123512 | PROCESS FOR THE PREPARATION OF PROLINE DERIVATIVES - The present invention relates in part to a process for the preparation of a proline derivative of formula I | 05-16-2013 |
20130197243 | SALTS OF 7-AMINO-3,5-DIHYDROXYHEPTANOIC ACID ESTERS - The invention relates to salts of acids with 2-propyl esters of general formula (2) The invention also relates to a method for the preparation of salts of acids with compounds of general formula (2) and to the use thereof in the preparation of atorvastatin. | 08-01-2013 |
20130338375 | Thioamide Compound, Method for Producing Thioamide Compound, Method for Producing [(4R,6R)-6-Aminoethyl-1,3-Dioxan-4-YL]Acetate Derivative, and Method for Producing Atorvastatin - A thioamide compound represented by the following general formula (1); | 12-19-2013 |
20140018546 | Novel Forms of [R-(R*,R*)]-2-(4-Fluorophenyl)-Beta, Gamma-Dihydroxy-5-(1-Methylethyl)-3-Phenyl-4-[(Phenylamino)carbonyl]-1H-P- yrrole-1-Heptanoic Acid Calcium Salt (2:1) - Novel forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt designated Form XX, Form XXI, Form XXII, Form XXIII, Form XXIV, Form XXV, Form XXVI, Form XXVII, Form XXVIII, Form XXIX, and Form XXX, characterized by their X-ray powder diffraction, solid-state NMR, and/or Raman spectroscopy are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease. | 01-16-2014 |
20140073801 | PYRROLIDINE DERIVATIVES AS SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - Disclosed are compounds of formula (I): | 03-13-2014 |
20140081033 | Novel Crystalline Form of Atorvastatin Hemi-calcium Salt, Hydrate Thereof, And Method of Producing The Same - The present invention provides a novel crystalline form of [R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-mthylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-heptanoic acid hemi-calcium salt (atorvastatin hemi-calcium salt) of the following formula 1, which is known to be useful as a drug, a hydrate thereof and a preparation method thereof: | 03-20-2014 |
20140100375 | NOVEL CRYSTALLINE FORM OF ATORVASTATIN HEMI-CALCIUM SALT, HYDRATE THEREOF, AND METHOD OF PRODUCING THE SAME - The present invention provides a novel crystalline form of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-mthylethyl)-3 -phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-heptanoic acid hemi-calcium salt (atorvastatin hemi-calcium salt) of the following formula 1, which is known to be useful as a drug, a hydrate thereof and a preparation method thereof: | 04-10-2014 |
20140155627 | Process for Forming Amorphous Atorvastatin - A process for forming amorphous atorvastatin comprising the steps of dissolving atorvastatin in a non-hydroxylic solvent and removing the solvent by freeze-drying, as well as processes of dissolving atorvastatin in a hydroxylic solvent with a solubilizing agent or an alkalizing agent or an antioxidant and removing the solvent by freeze-drying to afford amorphous atorvastatin. | 06-05-2014 |
20140336395 | Salt forms of [R-(R*,R*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-p- henyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid - Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease. | 11-13-2014 |
20150045563 | Novel Forms of [R-(R*,R*)]-2-(4-Fluorophenyl)-Beta, Gamma-Dihydroxy-5-(1-Methylethyl)-3-Phenyl-4-[(Phenylamino)carbonyl]-1H-P- yrrole-1-Heptanoic Acid Calcium Salt (2:1) - Novel forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt designated Form XX, Form XXI, Form XXII, Form XXIII, Form XXIV, Form XXV, Form XXVI, Form XXVII, Form XXVIII, Form XXIX, and Form XXX, characterized by their X-ray powder diffraction, solid-state NMR, and/or Raman spectroscopy are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease. | 02-12-2015 |
20160046575 | Novel Forms of [R-(R*,R*)]-2-(4-Fluorophenyl)-Beta, Gamma-Dihydroxy-5-(1-Methylethyl)-3-Phenyl-4-[(Phenylamino)carbonyl]-1H-P- yrrole-1-Heptanoic Acid Calcium Salt (2:1) - Novel forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt designated Form XX, Form XXI, Form XXII, Form XXIII, Form XXIV, Form XXV, Form XXVI, Form XXVII, Form XXVIII, Form XXIX, and Form XXX, characterized by their X-ray powder diffraction, solid-state NMR, and/or Raman spectroscopy are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease. | 02-18-2016 |
20170233341 | CRYSTAL OF PYRROLE DERIVATIVE AND METHOD FOR PRODUCING THE SAME | 08-17-2017 |
548538000 | The -C(=X)- is bonded directly to the ring nitrogen of the five-membered hetero ring (e.g., 1-pyrrolidine carboxanilides, etc.) | 1 |
20100261914 | IAP BINDING COMPOUNDS - Compounds that bind cellular IAPs (inhibitor of apoptosis proteins) are disclosed. The compounds are mimetics of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABOLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these compounds for therapeutic, diagnostic and assay purposes. | 10-14-2010 |