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Class 548/537 - Acyclic nitrogen bonded directly to the -C(=X)- (e.g., 4,5-dihalopyrrole -2 carboxamides, etc.)


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the group is bonded directly to acyclic
No. of patents: 437
Last issue date: 05/29/2012


1                      
NumberTitleIssue Date
8188300Atorvastatin 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. ...
05/29/2012
8143427Method for producing aminoacetylpyrrolidinecarbonitrile derivative
It is to provide a method for efficiently producing an aminoacetylpyrrolidinecarbonitrile derivative which is useful as a DPP-IV inhibitor. It is a method for producing an aminoacetylpyrrolidinecarbonitrile derivative represented by the formula (2):
03/27/2012
8115015Process 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. ...
02/14/2012
8097734Crystalline sodium atorvastatin
Crystalline sodium atorvastatin, compositions containing the same and methods for the production thereof. ...
01/17/2012
8080672Crystal form of atorvastatin hemi-calcium and processes for preparation thereof
Provided is a crystal form of atorvastatin hemi-calcium and processes for its preparation. ...
12/20/2011
8026377Process 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. ...
09/27/2011
8026376Forms of [R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-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 XX...
09/27/2011
7994343Process 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. ...
08/09/2011
7968734Organocatalysts and methods of use in chemical synthesis
The present invention pertains generally to compositions comprising organocatalysts that facilitate stereo-selective reactions and the method of their synthesis and use. Particularly, the invention relates to metal-free organocatalysts for facilitation of stereo-sel...
06/28/2011
7956198Pharmaceutical compositions
This invention relates to a combination product or medicament comprising at least one novel substituted pyrrole derivative and one or more dyslipidemic agents, antiobesity agents, antihyperglycaemic agents, anti-inflammatory agents or mixture thereof. Also provided ...
06/07/2011
7939675Process 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 a...
05/10/2011
7935832Pyrrole and isoindole carboxamide derivatives as P2X7 modulators
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: R2 represents hydrogen, halogen, C1-6 alkyl, C6-10 arylmethyl-, C2-6
05/03/2011
7875731Salt forms of [R-(R*,R*)]-2-(4-fluorophenyl)-β, δ-dihydroxy-5-(1-methylethyl)-3-phenyl-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 method...
01/25/2011
7834195Atorvastatin 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. ...
11/16/2010
7812179Process 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: (a) reacting the aldehyde 1 with...
10/12/2010
7732623Polymorphic 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...
06/08/2010
7645888Process for the production of amorphous atorvastatin calcium
A novel process of the preparation of amorphous atorvastatin calcium starting from a compound of Formula (II). ...
01/12/2010
7598400AMPO spin traps
Provided are spin traps for the study of radical formation in vivo or in vitro. 5-carbamoyl-5-methyl-1-pyrroline N-oxide (AMPO) and 2-amino-5-carbamoyl-5-methyl-1-pyrroline N-oxide (NH2-AMPO), have the following structures, respectively:
10/06/2009
7589216Process for preparing N-hydroxyformamido-propyl pyrrolidin compounds and intermediates
The present invention is directed to a process for preparing intermediates that are useful to prepare certain antibacterial N-formyl hydroxylamine compounds which are peptide deformylase inhibitors. The process makes use α β-lactarn intermediate. Certain optically...
09/15/2009
7563911Process for the preparation of amorphous atorvastin calcium salt (2:1)
Improved process for the preparation of amorphous atorvastatin calcium salt (2:1) comprises hydrolyzing the lactone form of atorvastatin of formula of FIG. 1 with aqueous alkali or alkaline earth metal base, extracting with organic solvent the reaction mixtur...
07/21/2009
7511157Hepatitis C inhibitor dipeptide analogs
Compounds of formula (I): wherein R1, R2, R3, R4, n and m are as defined herein. The compounds are useful as inhibitors of HCV NS3 protease. ...
03/31/2009
7468444Crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms
The present invention provides novel forms of atorvastatin designated Forms VI, VIII, IX, X, XI and XII and novel processes for their preparation as well as processes for preparing atorvastatin Forms I, II, IV, V and amorphous atorvastatin. ...
12/23/2008
7456297Crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms
The present invention provides novel forms of atorvastatin designated Forms VI, VIII, IX, X, XI and XII and novel processes for their preparation as well as processes for preparing atorvastatin Forms I, II, IV, V and amorphous atorvastatin. ...
11/25/2008
7429613Process 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: (a) reacting the aldehyde 1 with...
09/30/2008
7425576Compounds as inhibitors of hepatitis C virus NS3 serine protease
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of us...
09/16/2008
7423058Inhibitors of hepatitis C virus NS3 protease
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of us...
09/09/2008
7411075Polymorphic 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...
08/12/2008
7402683Cinnamic acid amides
The present invention relates to compounds, to processes for preparing them, to pharmaceutical compositions comprising them, and to their use in the therapy and/or prophylaxis in illnesses in people or animals, especially diseases of bacterial infection. ...
07/22/2008
7396851Heterocyclic and benzoheterocyclic polyamides structurally related to the natural antibiotic distamycin A for the treatment of β-thalassaemia
The invention relates to the use of structural analogues of distamycin having the general formula (I), (II), (III), (IV) or (V) or their pharmaceutically acceptable salts, for the preparation of a medicament for the therapeutic treatment of β-thalassaemia. ...
07/08/2008
7388008Lysine based compounds
The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for exampl...
06/17/2008
7388017Inhibitors of serine proteases, particularly hepatitis C virus NS3 protease
The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, eith...
06/17/2008
7381727Pyrrole derivatives, their preparation and their therapeutic use
The invention concerns compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The in...
06/03/2008
7378409Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
05/27/2008
7371865Process for the manufacture of HMG-CoA reductase inhibitors
The invention relates to a process for the manufacture of a compound of formula or a salt, especially a pharmaceutically acceptable salt with a base, thereof or a lactone thereof wherein the element represents —CH2
05/13/2008
7371855Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1-pyrrole-3-carboxylic acid phenylamide
An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide by a novel synthesis is described where methyl cyanoacetate is converted in eight ...
05/13/2008
7361772Process for the production of atorvastatin calcium
In one aspect, the invention provides a process for the production of 5-(4-Fluoro-phenyl)-2-isopropyl-4-phenyl-1-(3,5,7-trihydroxy-heptyl)-1H-pyrrole-3-carboxylic acid phenylamide hemicalcium salt, stereoisomers thereof or polymorphs thereof from a (6-{2-[2-(4-Fluor...
04/22/2008
7361771Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1-pyrrole-3-carboxylic acid phenylamide
An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide by a novel synthesis is described where methyl cyanoacetate is converted in eight ...
04/22/2008
73420413,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis C virus NS3 serine protease
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of us...
03/11/2008
7342120Crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms
The present invention provides novel forms of atorvastatin designated Forms VI, VIII, IX, X, XI and XII and novel processes for their preparation as well as processes for preparing atorvastatin Forms I, II, IV, V and amorphous atorvastatin. ...
03/11/2008
7329762Prodrugs of mitotic kinesin inhibitors
The present invention relates to phosphate ester prodrugs of dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relate...
02/12/2008
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