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Class 548/530 - Having -C(=X)-, wherein X is chalcogen, bonded directly to the five membered hetero ring (e.g., pyrrole carbonyl halides, pyrrole carboxaldehyde, etc.)


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein a group, in which X is chalcogen (i.e.,
No. of patents: 353
Last issue date: 12/06/2011


1                  
NumberTitleIssue Date
8071787Pyrrolidine compounds
A compound of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12
12/06/2011
7982053Peptide deformylase inhibitors
Novel PDF inhibitors and novel methods for their use are provided. ...
07/19/2011
7932403Process 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...
04/26/2011
7825264Substituted heterocycles, their use as medicament, and pharmaceutical preparations comprising them
The invention relates to compounds of formula I in which A, R1, R2, R3, R4, R5, R6, R7 and n have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particula...
11/02/2010
7687643Process for preparing 3,3-dimethylindolines
Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for p...
03/30/2010
7569706Glycerol derivative
(wherein R represents a residue comprising a reactive group or a group capable of being transformed into the reactive group; n represents an integer of 3 or more; and X represents a residue capable of having the following structur...
08/04/2009
7482474Creatine pyroglutamic acid salts and methods for their production and use in individuals
The present invention relates to a method of production and the use of a compositional ingredient. Specifically, the present invention relates to hydrosoluble stable organic salts of creatine and pyroglutamic acid. The compositional ingredient may be useful for the ...
01/27/2009
7465812Creatine pyroglutamic acid salts and methods for their production and use in individuals
The present invention relates to a method of production and the use of a compositional ingredient. Specifically, the present invention relates to hydrosoluble stable organic salts of creatine and pyroglutamic acid. The compositional ingredient may be useful for the ...
12/16/2008
7425631Compounds and methods of use
Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for...
09/16/2008
7425641Carboxylic acid amides, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to carboxylic acid amides of general formula wherein R1 to R5, Ar, m and n are defined as in claim 1, the tautomers, stereoisomer...
09/16/2008
7423057Compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
The present invention relates to a novel compounds that can be used as anti-inflammatory, immunomodulatory and antiproliferatory agents. In particular, the invention refers to new compounds which inhibit dihydroorotate dehydrogenase (DHODH), a process for their manu...
09/09/2008
7411091N-acyl-N′-benzyl-alkylendiamino derivatives
This invention is related to compounds and use of N-Acyl-N′-benzyl-alkylendiamino derivatives of the following general formula (I), wherein A is a straight or branched C2-C8 alkyl chain; X is a methylene, oxygen, sulphur or a NR7 g...
08/12/2008
7405297Process for preparing inhibitors of nucleoside metabolism
A process of preparing a compound of the formula (I) wherein B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H halogen or SCH3; R is an optionally substituted alk...
07/29/2008
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
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
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
7368568Protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for production and the use
The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroarnides for the synthesis of edothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives. ...
05/06/2008
7368576Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
The present invention provides new uses of DPIV-inhibitors of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, for treating conditions mediated by DPIV or DPIV-like enzymes, such as cancer and tumors. In a more pre...
05/06/2008
7365094Compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
The present invention relates to compounds of the general formula (II) and salts and physiologically functional derivatives thereof, for the use as a medicament. ...
04/29/2008
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
7348440Mitotic kinesin inhibitors
The present invention relates to 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 related to compositions which comp...
03/25/2008
7348356Phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
Disclosed are compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's dis...
03/25/2008
7335677Inhibitors of dipeptidyl peptidase IV
Novel compounds that are inhibitors of one or most post-proline cleaving proteases, e.g. dipeptidyl peptidase IV, according to general formula (1). R1 is H or CN, X1 is O, S, CH2, CHF, CF2, CH(CH3), C(CH3
02/26/2008
7329763Creatine pyroglutamic acid salts and methods for their production and use in individuals
The present invention relates to a method of production and the use of a compositional ingredient. Specifically, the present invention relates to hydrosoluble stable organic salts of creatine and pyroglutamic acid. The compositional ingredient may be useful for the ...
02/12/2008
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
7317070Process for the preparation of polyamino acids
Among the various aspects of the present invention is an improved process for the preparation of polyamino acids generally, and more specifically, polyglutamic acid and polyaspartic acid. Another aspect is a process for the large scale (i.e. >1 kg) preparation of po...
01/08/2008
7304165Oligomers and polymers of di-substituted cyclic imino carboxylic acids
Disclosed are cyclic imino oligomers and polymers comprised of subunits of the formula: Also disclosed are combinatorial libraries and arrays of the cyclic imino compounds. ...
12/04/2007
7300956Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analog...
11/27/2007
7276610Aryl piperidine amides
The invention provides novel GlyT2 inhibiting compounds useful in modulating, treating, or preventing: anxiolytic disorders; a condition requiring treatment of injured mammalian nerve tissue; a condition amenable to treatment through administration of a neurotrophic...
10/02/2007
72681586H-THIENO [2,3-b]pyrrole derivatives as antagonists of gonadotropin releasing hormone (GnRH)
The invention relates to a group of novel thieno-pyrrole compounds of Formula (I): wherein: R1, R2, R3, R4 and R5 are as defined in the specification, which ...
09/11/2007
7265146Integrin receptor inhibitors
Provided are compounds of formula (I) wherein A, Q, W, X, Y, Z, R1 to R4, m and n are as defined herein. Compounds of the invention bind to α4 integrin receptors and thereby inhi...
09/04/2007
7259250C-nitroso compounds and use thereof
A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less th...
08/21/2007
7244758N-type calcium channel blockers
Compounds that are derivatives of 3-aminomethyl-pyrrolidine generally containing at least one benzhydril moiety are useful in treating conditions which benefit from blocking calcium ion channels. ...
07/17/2007
72355443-sulfonylamino-pyrrolidine-2-one derivatives as inhibitors of factor Xa
The invention relates to compounds of formula (I): wherein substituents are as defined. ...
06/26/2007
7230002Dipeptidyl peptidase IV inhibitors; processes for their preparation and compositions thereof
The present invention relates to novel dipeptidyl peptidase IV (DPP-IV) inhibitors their analogs, isomers, pharmaceutical compositions, therapeutic uses and methods of making the same. ...
06/12/2007
7217706Propanolamine derivatives
This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympatho...
05/15/2007
7211677Process for preparing inhibitors of nucleoside metabolism
A process of preparing a compound of the formula (I) wherein B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H halogen or SCH3; R is an optionally subs...
05/01/2007
RE39575Substituted thioacetamides
The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases. ...
04/17/2007
7199150Amino alcohol compounds
Amino alcohol compounds and phosphonic acid compounds having excellent immunosuppressive activity, pharmacologically acceptable salts thereof and pharmacologically acceptable esters thereof, and pharmaceutical compositions comprising such compounds, the compounds ha...
04/03/2007
7189756Pyrrolidine derivatives
The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction. ...
03/13/2007
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