|8466284||Some 2-pyrazinone derivatives and their use as inhibitors of neutrophile elastase|
The invention provides certain novel compounds as listed in the specification and pharmaceutically acceptable salts thereof and particular Forms thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in ther...
|RE43748||Nitrogen-containing heterocyclic carboxamide derivatives or salts thereof and antiviral agents comprising the same|
Nitrogen-containing heterocyclic carboxamide derivatives represented by the following general formula: wherein ring A is a substituted or unsubstituted pyrazine, pyrimidine, pyridazine or triazine ring; R1 is O o...
|8106197||Aminoheteroaryl compounds as protein kinase inhibitors|
Aminopyridine and aminopyrazine compounds of formula (1), compositions including these compounds, and methods of their use are provided. Preferred compounds of formula 1 have activity as protein kinase inhibitors, including as inhibitors of c-MET. ...
|8076481||Chemical process 632|
A process for preparing pharmaceutically active compounds of formula (I) or a salt thereof wherein R1, n, m, R3, R6, X1, X2, X3 and X4 are as defi...
|7964725||Heteroarylbenzamide derivatives for use in the treatment of diabetes|
The invention relates to a novel group of compounds of Formula (I) or a salt thereof: wherein R1, R2, R3, n, A and HET-1 are as described in the specification, which may be useful in the tre...
|7947835||Certain substituted amides, method of making, and method of use thereof|
At least one chemical entity chosen from compounds of Formula 2 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical c...
|7371743||Carboxylic acid amides, the preparation thereof and their use as medicaments|
The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers,...
|7358239||Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives|
The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is...
|7342019||5, 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...
Novel compounds of the formula I in which W, X, Y, T, R1 and R2 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders
|7265115||Diazabicyclic CNS active agents|
Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals. ...
|7265108||Nitrogen containing heterocyclic compounds and medicines containing the same|
Compounds represented by the following general formula: [wherein X1, X2, X3 and X4 each independently represent a single bond, C1-6 alkylene, etc.; A2
|7205306||Substituted 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...
|7205302||Heterocyclic compound derivatives and medicines|
The present invention provides a compound which is useful as a PGI2 receptor agonist, and a pharmaceutical composition. The present invention is directed to a pharmaceutical composition comprising a compound represented by the following formula ...
Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators or CRF receptors. Compounds of the invention are provided by the following formula: The 5-substituted-2-aryl...
|7176312||Kinase inhibitor scaffolds and methods for their preparation|
General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, bor...
|7132424||Monocyclic 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,...
|7132425||5-substituted-six-membered heteroaromatic glucokinase activators|
The present invention provides a compound according to formula I where the substituent designations are provided in the specification. Pharmaceutical compositions comprising a compound according to formula I are ...
|7125863||Inhibitors of dipeptidyl peptidase IV|
Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of t...
|7119094||Substituted polycyclic aryl and heteroarpyl pyrazinones useful for selective inhibition of the coagulation cascade|
The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a varie...
|7119203||Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors|
This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metallop...
|7105522||HIV 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...
|7064201||Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof|
Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an in...
|7056925||Urea kinase inhibitors|
Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
Compounds of Formula 1 [Region α]—[Region β]—[Region γ]—[Region δ] (1) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and m...
|RE39056||4-Azasteroids for treatment of hyperandrogenic conditions|
Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5α-reductase inhibitory activity. These compounds inhibit 5α-reductase type 1 and type 2. The compounds of structural Formula...
Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases as...
|6964965||Substituted 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...
|6949551||Dihalopropene compounds, processes for their preparation, compositions comprising them and their use as pesticides|
Dihalopropene compounds, process for their preparation, compositions comprising them and their use as pesticides What is described are dihalopropene compounds of the formula (I) in which R1 and R...
|6900210||Pyridinyl, pyrimidinyl and pyrazinyl amides as potassium channel openers|
The present invention provides novel heterocyclic amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A, B and Z...
|6867210||Aryl substituted pyrimidines|
This invention relates aryl substituted pyridines, pyrimidines, pyrazines and triazines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein A1, A2, A3
|6833370||Heterocycle 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...
|6806369||Peptide deformylase inhibitors|
PDF inhibitors and novel methods for their use are provided. ...
|6787544||Nitrogen-containing heterocyclic carboxamide derivatives or salts thereof and antiviral agents comprising the same|
Nitrogen-containing heterocyclic carboxamide derivatives represented by the following general formula: wherein ring A is a substituted or unsubstituted pyrazine, pyrimidine, pyridazine or triazine ring; R1 is ...
|6713472||Thiazine or pyrazine derivatives|
A compound which is a chymase inhibitor and which is represented by a formula [I] and salts thereof. In the formula [I], X is R6—(A2)n—N, R1 and R2 are H, alkyl, cycloalkyl or aryl, R3 and R4...
|6706021||Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors|
Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: wherein X is O or NR9 and Het, R1, R7, R8, R12-R15, R
|6699856||Pyrazinones, compositions containing such compounds and methods of use|
Compounds represented by formula I: ##STR1## as well as pharmaceutically acceptable salts, esters, N-oxides and hydrates thereof are disclosed. Pharmaceutical compositions and methods of use are also included. The compounds are active against the caspase-...
|6689781||Phenylalanine derivatives as alpha 4 integrin inhibitors|
Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine....
|6673795||Pyrimidine, pyrazine and triazane derivatives|
The present invention is a pyrimidine, triazine or pyrazine derivative of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, R4, X, Y and Z are as defined in the specification...
|6635641||Amide compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use|
Amide compounds represented by the formula: ##STR1## wherein: R1 is a moiety represented by the formula ##STR2## where X is selected from the group consisting of CH2, O, S, and NH; and Y is selected from the group consisting...