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| Number | Title | Issue Date |
| 8168638 | Pyrazinecarboxamide derivatives and plant disease controlling agents containing the same The present invention provides the compounds represented by the general formula (I): [wherein X is a halogen atom or an (C1-C3)alkyl group which may be substituted with a halogen atom(s); Y is a hydrog... | 05/01/2012 |
| 8158631 | Heterocyclic antiviral compounds Compounds having the formula I wherein R1, R2, R3, R4, and R5 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and... | 04/17/2012 |
| 8158630 | Application of 2,5 -dihydroxymethyl-3,6-dimethyl pyrazine and its derivates in pharmacy An application of 2,5-dihydroxymethyl-3,6-dimethyl pyrazine and its derivatives in the preparation of drugs for the treatment of, prevention of, and/or protection from heart failure wherein the structural formula of the compound is as follows: | 04/17/2012 |
| 8138189 | Substituted benzene compounds as modulators of the glucocorticoid receptor The present invention relates to compounds of formula I wherein R.sup.1a to R.sup.1e and R.sup.2 to R.sup.5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are gluc... | 03/20/2012 |
| 8110577 | Histone deacetylase inhibitors The present invention provides histone deacetylase inhibitors of general formula (I), a process for the preparation of such compounds and uses of the compounds in medicine, especially in the treatment of cancers and the inhibition of histone deacetylase activity. | 02/07/2012 |
| 8067418 | Tricyclic angiotensin II agonists There is provided compounds of formula I, wherein the dotted line, X1, X2, X3, A, Y1, Y2, Y3, Y4, Z1, Z2, R2 and ... | 11/29/2011 |
| 7981894 | Polymorphic forms of 1-′4-(5-cyanoindol-3-yl) butyl-4-(2-carbamoylbenzofuran-5-yl)piperazine hydrochloride The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl) butyl]-4-(2-carbomyl-benzofuran-5-yl)-piperazine, crystaline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl) butyl]-4-(2-carbomyl-benzofuran-5-yl)... | 07/19/2011 |
| 7968547 | Heteroaryl, heterocyclic and aryl compounds which inhibit leukocyte adhesion mediated by VLA-4 Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, su... | 06/28/2011 |
| 7960384 | Dipeptidyl peptidase inhibitors Compounds, pharmaceutical compositions, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound of the formula: wherein the substituents are as defined herein. ... | 06/14/2011 |
| 7947685 | Pyrazine-2-carboxyamide derivatives The present invention is concerned with novel pyrazine 2-carboxyamide derivatives of formula (I) wherein R1, R2 and R3 are as defined in the specification. These compounds are useful for the... | 05/24/2011 |
| 7947684 | 1-aroyl-piperidinyl benzamidines This invention relates to compounds of formula which inhibit Factor Xa or tryptase, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from condi... | 05/24/2011 |
| 7820671 | Peptidomimetic protease inhibitors The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective ... | 10/26/2010 |
| 7807677 | HIV protease inhibitors Compounds of the formula I: wherein R1, R2, X and N are as defined in the specification; E is N, CH; A′ and A″ are terminal groups as defined in the specifica... | 10/05/2010 |
| 7803802 | Substituted amide beta secretase inhibitors Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defin... | 09/28/2010 |
| 7622471 | Pyrazole derivatives having a pyridazine and pyridine functionality The present invention is directed to a strong platelet aggregation-inhibiting agent which does not inhibit COX-1 or COX-2. Further, the present invention provides compounds represented by formula (I), salts of the compounds, and solvates or hydrates of the compounds... | 11/24/2009 |
| 7622472 | Combination of Src kinase inhibitors and chemotherapeutic agents for the treatment of proliferative diseases Compositions and methods are disclosed which are useful of the treatment and prevention of proliferative disorders. ... | 11/24/2009 |
| 7612074 | Diazabicyclic aryl derivatives as cholinergy ligands This invention relates to novel diazabicyclic aryl compounds of the formula wherein: R′ represents hydrogen or alkyl; A represents an aromatic monocyclic or bicyclic carbocyclic or heterocyclic; and is hydrogen or a subsi... | 11/03/2009 |
| 7598248 | Certain 1H-imidazo[4,5-b]pyrazin-2(3H)-ones and 1H-imidazo[4,5-b]pyrazin-2-ols, compositions thereof, and methods for their use Provided is at least one chemical entity chosen from compounds of Formula I and compounds of Formula II: and pharmaceutically acceptable salts thereof, compositions thereof, and methods for their use in modulating of one or... | 10/06/2009 |
| 7595318 | Polyethylene glycol conjugates of heterocycloalkyl carboxamido propanoic acids Disclosed are conjugates which bind VLA-4. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such conjugates are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human,... | 09/29/2009 |
| 7566716 | Imidazopyrazines as Raf inhibitor compounds Compounds of Formula I are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo... | 07/28/2009 |
| 7547701 | Haloalkyl containing compounds as cysteine protease inhibitors The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compo... | 06/16/2009 |
| 7531541 | Partial mGluR5 antagonists for treatment of anxiety and CNS disorders Provided is a method of treating conditions and disorders for which full mGluR5 antagonists are potentially effective, such as, e.g., anxiety, epilepsy, schizophrenia and other psychotic disorders, Parkinson's disease, addictive disorders, and the like in a subject ... | 05/12/2009 |
| 7514437 | Substituted diketopiperazines as oxytocin antagonists A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a mammal in need thereof of an effective amount of a compound of the formula (I) and/or a ph... | 04/07/2009 |
| 7511043 | FXR modulators The present invention provides compounds, pharmaceutical compositions and methods that are useful in modulating the farnesoid X receptor (FXR). As FXR is involved in negatively controlling the expression level of cholesterol 7α-hydroxylase (cyp7a), the rate-limitin... | 03/31/2009 |
| 7498331 | Arthropod repellent pharmacophore models, compounds identified as fitting the pharmacophore models, and methods of making and using thereof Disclosed herein is a pharmacophore model for arthropod repellent activity and methods of making and using thereof. The pharmacophore comprises two hydrophobic aliphatic functions, one aromatic function and one hydrogen bond acceptor function. The pharmacophore mode... | 03/03/2009 |
| 7456179 | Methods of treating ischemic related conditions The present invention relates to methods of treating ischemia-related conditions by administering to a patient in need of such methods certain thiosemicarbazone compounds. Preferred embodiments of the present invention relates to methods of treating specific ischemi... | 11/25/2008 |
| 7432271 | Pyrazolyl inhibitors of 15-lipoxygenase The present invention provides pyrazolyl inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions. ... | 10/07/2008 |
| 7407959 | Cathepsin cysteine protease inhibitors This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, s... | 08/05/2008 |
| 7407985 | Compounds that abrogate DNA damage induced cell cycle G2 checkpoint and/or augment anti-cancer activity of DNA-damaging treatments The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to... | 08/05/2008 |
| 7390908 | Compounds effecting glucokinase The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or preventio... | 06/24/2008 |
| 7381726 | Polymorphic forms of 1-′4-(5-cyanoindol-3-yl)butyl-4-(2-carbamoylbenzofuran-5-yl)piperazine hydrochloride The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl... | 06/03/2008 |
| 7371220 | System and method for real-time apnea/hypopnea detection using an implantable medical system Techniques are provided for detecting the onset of an episode of apnea/hypopnea substantially in real-time. A moving threshold is generated based on recent respiration cycles and differences are accumulated between amplitudes of new respiration cycles and the moving... | 05/13/2008 |
| 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,... | 05/13/2008 |
| 7365075 | Aryl sulfonamide compounds and uses related thereto The present invention provides Aryl Sulfonamide Compounds having the formula: and prodrugs or pharmaceutically acceptable salts or prodrugs thereof. The Aryl Sulfonamide Compounds are useful for treating diabetes, obesity, ... | 04/29/2008 |
| 7365073 | 3-(heteroaryl) alanine derivatives-inhibitors of leukocyte adhesion mediated by VLA-4 Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, a... | 04/29/2008 |
| 7361365 | Vermin repellent A method for repelling a pest using 2-isopropyl-3-methoxi-pyrazine as a pest repellent, particularly a mole repellent, and a pest repelling composition which comprises this compound. ... | 04/22/2008 |
| 7361146 | System and method for detecting abnormal respiration via respiratory parameters derived from intracardiac electrogram signals Techniques are provided for tracking patient respiration based upon intracardiac electrogram (IEGM) signals or other electrical cardiac signals. Briefly, respiration patterns are detected based upon cycle-to-cycle changes in morphological features associated with in... | 04/22/2008 |
| 7342018 | Urokinase inhibitors and uses thereof The invention relates to the use of derivatives of 3-amidinophenylalanine as urokinase inhibitors for treating malignant tumors and the formation of metastases. ... | 03/11/2008 |
| 7342011 | Rifamycin analogs and uses thereof The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated... | 03/11/2008 |
| 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 |
