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| Number | Title | Issue Date |
| 8039623 | Inhibitors 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 |
| 7910735 | Substituted 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 |
| 7388008 | Lysine 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 |
| 7378421 | Chromenone 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 |
| 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... | 03/11/2008 |
| 7326706 | Pyrazine 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 |
| 7319100 | 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... | 01/15/2008 |
| 7282502 | CCR9 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 |
| 7273946 | Prostaglandin 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 |
| 7273868 | Pyrazine 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 |
| 7265115 | Diazabicyclic CNS active agents Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals. ... | 09/04/2007 |
| 7259157 | N-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 |
| 7238717 | CCR9 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 |
| 7223774 | Benzamide 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 |
| 7208600 | Inhibitors 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 |
| 7199123 | Pyrazine 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 |
| 7153965 | Pharmaceutically 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 |
| 7151178 | Method 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 |
| 7144886 | Dipeptidyl 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 |
| 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,... | 11/07/2006 |
| 7132418 | Peptidyl 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 |
| 7109172 | Inhibitors 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 |
| 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... | 09/12/2006 |
| 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... | 11/15/2005 |
| 6949556 | Acylated 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 |
| 6914160 | Oxytocin inhibitors This invention relates to compounds of formula (I) ... | 07/05/2005 |
| 6909000 | Bridged 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 |
| 6878706 | Cyanamides 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 |
| 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... | 12/21/2004 |
| 6800629 | Pyrazine 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 |
| 6797706 | Heterocyclecarboxamide 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 |
| 6787546 | Heterocycle 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 |
| 6759412 | Acylated 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 |
| 6677354 | Piperdines 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 |
| 6673784 | Electrophilic 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 |
| 6635766 | Process 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 |
| 6632816 | Aromatic 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 |
| 6608067 | Inhibitors 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 |
| 6548504 | Compounds 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 |