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Class 544/406 - Having -C(=X)-, wherein X is chalcogen, bonded directly to the diazine ring


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein a group, in which X is chalcogen (i.e.,
No. of patents: 228
Last issue date: 10/18/2011


1            
NumberTitleIssue Date
8039623Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As ...
10/18/2011
7910735Substituted pyrazinecarboxylic acid anilide derivatives or salts thereof, intermediates of the same, pesticides for agricultural and horticultural use, and usage thereof
Substituted pyrazinecarboxylic acid anilide derivatives represented by the general formula (I) or salts thereof; intermediates of them; pesticides (such as insecticides and acaricides) for agricultural and horticultural use, containing the compounds as the active in...
03/22/2011
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
7378421Chromenone derivatives
Novel compounds of the formula I in which R1, R2, R3 and Het are as defined herein, which are inhibitors of tyrosine kinases and/or Raf kinases and can be employed for...
05/27/2008
73420195, 6-diaryl-pyrazine-2-amide derivatives as CBantagonists
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, prodrugs, solvates and crystalline forms thereof, in which R1 and R2 independently represent: a C1-6alkyl group; an optionally substitu...
03/11/2008
7326706Pyrazine modulators of cannabinoid receptors
The present application describes compounds according to Formula I, wherein A, G1, G2 and R1 are described herein. Additionally, the present application describes pharmaceutical compositions comprising at least one compound according...
02/05/2008
7319100Substituted pyrazinones, pyridines and pyrimidines as corticotropin releasing factor ligands
Compounds provided herein are novel substituted pyrazinones, pyridines and pyrimidines of Formula (I) and (II): Such compounds are particularly useful as CRF receptor ligands, and hence, in the treatment of vario...
01/15/2008
7282502CCR9 inhibitors and methods of use thereof
The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compound...
10/16/2007
7273946Prostaglandin derivatives
Prostaglandin nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension. ...
09/25/2007
7273868Pyrazine derivatives
1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ═CH— or ═N—, Y is —NH—, —NR4—, —S—, ...
09/25/2007
7265115Diazabicyclic CNS active agents
Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals. ...
09/04/2007
7259157N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists
Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain. ...
08/21/2007
7238717CCR9 inhibitors and methods of use thereof
The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compound...
07/03/2007
7232821(2-((2-alkoxy)-phenyl) -cyclopent-1enyl) aromatic carbo and heterocyclic acid and derivatives
Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, R1, R2, Rx, R8, R9 and n are as defined in the specification, a proc...
06/19/2007
7223774Benzamide 2-hydroxy-3-diaminoalkanes
The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the...
05/29/2007
7208600Inhibitors of serine proteases, particularly HCV NS3-NS4A proteases
The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3–NS4A ...
04/24/2007
7199123Pyrazine compounds as transforming growth factor (TGF) compounds
Novel pyrazine compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming gro...
04/03/2007
7153965Pharmaceutically acceptable inorganic and organic salts of 5-methylpyrazine-2-carboxylic acid-4-oxide
Methods for the preparation of pharmaceutically acceptable organic or inorganic salts of 5-methylpyrazinecarboxylic acid-4-oxide esters including tris(hydroxymethyl)aminomethanol, N,N-dimethylethanolamine, N-methyl-D-glucamine, L-Lysine, L-arginine, Na, K, Ca and Mg...
12/26/2006
7151178Method for the preparation of 5-methylpyrazine-2-carboxylic acid-4-oxide and its salts
Methods for the preparation of pharmaceutically acceptable salts of 5-methylpyrazine-carboxylic acid-4-oxide by using the oxidizing agent OXONE® for the N-oxidation of C1-4 methylpyrazinecarboxylic acid esters. The pharmaceutically acceptable salts are t...
12/19/2006
7144886Dipeptidyl peptidase IV (DP-IV) inhibitors as anti-diabetic agents
The present invention relates to a series of prodrugs of inhibitors of DP-IV with improved properties. The compounds can be used for the treatment of a number of human diseases, including impaired glucose tolerance and type II diabetes. The compounds of the inventio...
12/05/2006
7132424Monocyclic derivatives as matrix metalloproteinase inhibitors
This invention provides compounds defined by Formula I R1-Q-D-(V1)m—R2I or a pharmaceutically acceptable salt thereof, wherein R1, Q, D, V1, m,...
11/07/2006
7132418Peptidyl heterocyclic ketones useful as tryptase inhibitors
The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particul...
11/07/2006
7109172Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
The present invention relates to compounds of formula I or formula Ia or pharmaceutically acceptable salts thereof, that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3–NS4A protease. As such, they act by interfering with the l...
09/19/2006
7105522HIV inhibiting pyrazinone derivatives
This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 is hydrogen, hydroxy, c...
09/12/2006
6964965Substituted pyrazine derivatives
The present invention provides substituted pyrazine derivatives of Formula I, that are CRF1 receptor antagonists, including human CRF1 receptors. This invention also relates to use of compounds of...
11/15/2005
6949556Acylated 1,2,3,4-tetrahydronaphthyl amines and their use as pharmaceutical agents
The present invention relates to compounds of general formula (I), wherein R1-R4 have the meanings given in the specification, A is CH2, CHOH or CH—(C1-C3-alkyl), B and C a...
09/27/2005
6914160Oxytocin inhibitors
This invention relates to compounds of formula (I) ...
07/05/2005
6909000Bridged bicyclic serine protease inhibitors
The present invention relates to peptidomimetic compounds which inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as a...
06/21/2005
6878706Cyanamides useful as reversible inhibitors of cysteine proteases
Compounds according to the following formula (I): wherein the variables Q and R1 to R6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F, L and B...
04/12/2005
6833370Heterocycle substituted aminoazacycles useful as central nervous system agents
Heterocyclic substituted aminoazacyclic compounds of formula I Z—R3  I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said comp...
12/21/2004
6800629Pyrazine derivatives or salts thereof, pharmaceutical composition containing the same, and production intermediates thereof
Pyrazine derivatives represented by general formula [1]: wherein the variables are as defined in the specification, or salts thereof have an excellent antiviral activity and are useful as a therapeutic agent for treating...
10/05/2004
6797706Heterocyclecarboxamide derivative
A nitrogen-containing six-membered heterocyclic compound having substituents —X—A—R3, —N(R1)-(Ph substituted by R2), and —CONH2, a salt thereof, a prodrug thereof, and a Syk inhibitor containing the same as an ac...
09/28/2004
6787546Heterocycle derivatives and drugs
The object of the invention is to provide an excellent compound as a drug. The invention relates to a heterocyclic compound shown by the following formula: A—B—D—E  [1] wherein A is heteroaryl or its oxi...
09/07/2004
6759412Acylated 6,7,8,9-tetrahydro-5H-benzocycloheptenyl amines and their use as pharmaceutical agents
The present invention relates to compounds according to the general formula (I), wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3
07/06/2004
6677354Piperdines for use as orexin receptor antagonists
Disclosed are compounds of formula (I): ##STR1## wherein: Y represents a group (CH2)n, wherein n represents 0, 1 or 2; R1 is phenyl, naphthyl, a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected ...
01/13/2004
6673784Electrophilic ketones for the treatment of herpesvirus infections
A class of compounds is described which can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula II ##STR1## wherein each of R1, R2, and R3 is independently selected f...
01/06/2004
6635766Process for the preparation of arylamides of heteroaromatic carboxylic acids
A process for the preparation of arylamides of heteroaromatic carboxylic acids of the formula: ##STR1## in which each An is nitrogen or CRn (n=1 to 5), with the proviso that at least one of the ring members is nitrogen and that two n...
10/21/2003
6632816Aromatic derivatives as HIV aspartyl protease inhibitors
The present invention provides HIV aspartyl protease inhibitors of the formula; ##STR1## and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein n is 3 or 4, wherein R1 may b...
10/14/2003
6608067Inhibitors of serine proteases, particularly HCV 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...
08/19/2003
6548504Compounds
The present invention therefore provides, in a first aspect, a compound of formula (I) or a salt thereof: ##STR1## in which the group D is selected from a group of formula (A), (B) or (C) below: ##STR2## in which P is a monocyclic, bicyclic or tricyc...
04/15/2003
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