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Class 544/141 - Five-membered hetero ring consisting of one nitrogen and four carbons


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the five-membered hetero ring consists
No. of patents: 377
Last issue date: 04/27/2010


1                    
NumberTitleIssue Date
7705146Hepatitis C inhibitor peptide analogs
The invention relates to compounds of formula (I) wherein R′, R2, R3, R4, R5, R6, Y, n and m are as defined herein. The compounds are useful for the treatment and prevention of hepatitis C viral infections in ...
04/27/2010
7504500Method for the production of pyrrolidine-1,2-dicarboxylic acid-1-(phenyl(-amide))-2(phenyl(-amide)) derivatives and 1-(phenylcarbamoyl)-pyrrolidine-2-carboxylic acid derivatives as intermediate products
Process for the preparation of compounds of the formula I in which R, R1, R2 and R3 are as defined in Patent claim 1, and compounds of the formula IV in which R and R1 are as defined in Patent claim 1, are intermediates fo...
03/17/2009
7442807N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands
The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n w...
10/28/2008
7429587Pyrrolidine derivatives as factor Xa inhibitors
The invention relates to compounds of formula (I) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for w...
09/30/2008
7419999Gamma lactams as prostaglandin agonists and use thereof
1,2-substituted 5-pyrrolidinone compounds are provided, and methods of treatment and pharmaceutical composition that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing pr...
09/02/2008
7402606Derivatives of 1-(oxoaminoacetyl) pentylcarbamate as cathepsin K inhibitors for the treatment of bone loss
Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle ...
07/22/2008
7388007Gamma-lactams as beta-secretase inhibitors
There is provided a series of novel substituted gamma-lactams of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R4, R5 and R6
06/17/2008
7348427Antipathogenic benzamide compounds
Antipathogenic benzamide compounds having the formula wherein at least one of the R1 groups is F, Cl, CN or CF3 and R2, R3, Y, Z, m, and n are as defined herein. ...
03/25/2008
7338947Cyclic 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 rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma, pro...
03/04/2008
7335645Effectors of dipeptidyl peptidase IV for topical use
The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula wherein A is an amino acid having at least one f...
02/26/2008
7332487Nitrogen-containing 5-membered ring compound
The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein symbols in the formula have the following meanings; ...
02/19/2008
7326785Pyrrolidine derivatives as factor XA inhibitors
The invention relates to compounds of formula (I) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical cond...
02/05/2008
7301037Charged compounds comprising a nucleic acid binding moiety and uses therefor
Charged compounds are provided that comprise one or more regions of localized positive charge, compositions comprising such compounds, methods of synthesizing such compounds, methods of screening such compounds to identify those having anti-infective activity, and m...
11/27/2007
72976921,3-dihydro-2-indol-2-one derivatives, process for preparing them and pharmaceutical compositions containing them
The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b
11/20/2007
7288540Phenylalkynes
Substituted phenylalkynes of formula (I) compositions containing them and their methods of use to treat histamine related disorders are described, wherein R1, R2, R3, R4
10/30/2007
7282497Pyrrolidin-2-one derivatives as inhibitors of factor xa
The invention relates to compounds of formula (Ic) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical con...
10/16/2007
7279472Compounds useful as reversible inhibitors of cysteine proteases
Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds
10/09/2007
72591634-(6-membered)-heteroaryl acyl pyrrolidine derivatives as HCV inhibitors
Novel anti-viral agents of Formula wherein: A represents OR1, NR1R2, or R1 wherein R1 and R2 are hydrogen, C1-6alkyl, aryl...
08/21/2007
72561883-aminoalkyl-2-aryl-indole derivatives and their use as GnRH antagonists
The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use of a compound of the present invention in the manufacture of a medicam...
08/14/2007
7253205Gem-disubstituted cyclohexane derivatives and their use as therapeutic agents
The present invention relates compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 represent a variety of substituents, ring A i...
08/07/2007
7250414Diphenylmethyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, e, m, n, Ar1, R1, R2, R3, R4a, R4b, R5 and R6 are as defined ...
07/31/2007
7247627Salts and polymorphs of a pyrrole-substituted indolinone compound
The invention relates to non-hygroscopic salts of 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, such as maleate salts, and to crystalline polymorphs of these salts. The ...
07/24/2007
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
7229991Substituted 5-aminomethyl-1H-pyrrole-2-carboxamides
5-aminomethyl-1H-pyrrole-2-carboxylic acid amide compounds corresponding to formula I and processes for the production thereof. Pharmaceutical preparations containing these compounds and the use of these compound...
06/12/2007
7205312N-[4-(heteroarylmethyl)phenyl]-heteroarylamines
The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydrox...
04/17/2007
7202242Substituted 1 and 2-naphthol Mannich bases
The invention relates to substituted 1 and 2 naphthol Mannich bases, a method for the production thereof, medicaments containing said compounds and the use of said compounds in the production of medicaments. ...
04/10/2007
7195751Compositions and kits pertaining to analyte determination
This invention pertains to methods, mixtures, kits and/or compositions for the determination of analytes by mass analysis using unique labeling reagents or sets of unique labeling reagents. The labeling reagents can be isomeric or isobaric and can be used to produce...
03/27/2007
7186718Piperidinyl-morpholinyl derivatives as modulators of chemokine receptor activity
The invention provides compounds of general formula (I), in which m, n, Z1, Z2, R1, R2, R3, R4 and R5 are as defined in the specification; processes for their preparation; pharmaceutical co...
03/06/2007
7186717Pyrrolidine derivatives as Factor Xa inhibitors
The invention relates to compounds of formula (I) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical cond...
03/06/2007
7186827Dipeptide synthesis
Disclosed are processes of making dipeptide compounds of formula(I) as further described in the detailed description section: ...
03/06/2007
7183270Cyclic 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 rheumatoid arthritis, multiple sclerosis, atherosclerosis and ...
02/27/2007
7183408Process 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 ...
02/27/2007
71798352-(3-sulfonylamino-2-oxopyrrolidin-1-yl)propanamides as factor xa inhibitors
The invention relates to compounds of formula (I) pharmaceutical compositions containing the same as well as methods of treating patients suffering from a condition susceptible to amelioration by a Factor Xa inhibitor using the same.
02/20/2007
7169805Captopril derivatives
Captopril nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment or prophylaxis of cardiovascular, inflammatory and renal diseases. ...
01/30/2007
7163937Cyclic 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 treatment of rheumatoid arthritis, multiple sclerosis, atherosclerosis and a...
01/16/2007
7157454Derivatives of n-(arylsulfonyl)beta-aminoacids comprising a substituted aminomethyl group, the preparation method thereof and the pharmaceutical compositions containing same
The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal pr...
01/02/2007
7132534Para-phenylenediamine derivatives containing a pyrrolidyl group, and use of these derivatives for coloring keratin fibers
The invention relates to novel pyrrolidyl-substituted para-phenylenediamine derivatives, to dye compositions containing them and to the process for dyeing keratin fibers using these compositions. The present invention makes it possible in particular to obtain...
11/07/2006
71292401,3-dihydro-2H-indol-2one derivatives, process for preparing them and pharmaceutical compositions containing them
The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V
10/31/2006
7122666Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses
Compounds having activity against production of an inflammatory cytokine of formula (I)′: A′ is pyrrole; R1′ is phenyl or naphthyl; R2′ is pyridyl or pyrimidinyl; R3′ is...
10/17/2006
7109186HIV integrase inhibitors
The present invention describes novel compounds of Formula I which inhibit HIV integrase. The invention also describes compositions and treatments of AIDS or ARC by using these compounds ...
09/19/2006
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