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| Number | Title | Issue Date |
| 8173672 | Quinolizidinone M1 receptor positive allosteric modulators The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disord... | 05/08/2012 |
| 8143273 | Quinolizidine and indolizidine derivatives The present invention relates to a compound of formula I-A or I-B wherein X, R1, R2 and R3 are defined herein; or to a pharmaceutically acceptable acid add... | 03/27/2012 |
| 7915287 | Substituted heterocycles and methods of use Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophyl... | 03/29/2011 |
| 7879875 | P38 kinase inhibiting agents Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: (I) are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty ar... | 02/01/2011 |
| 7842702 | Treatment for irritable bowel syndrome N-(1H-tetrazol-5-yl)-1-phenoxy-4H-quinolizin-4-one-3-carboxamide is effective for treating IBS. In addition, IBS may be effectively treated with N-(1H-tetrazol-5-yl)-1-phenoxy-4H-quinolizin-4-one-3-carboxamide when used concomitantly with at least one of various ser... | 11/30/2010 |
| 7776880 | Derivatives of pyrrolizine, indolizine and quinolizine, preparation thereof and therapeutic use thereof The disclosure relates to a compound of formula (I): wherein m, n, Ar, and R are as defined in the disclosure, to compositions containing them and to their therapeutic use. The disclosure also relates to processes for prepa... | 08/17/2010 |
| 7745459 | Quinolizinone compound and use thereof as HIV integrase inhibitor A pharmaceutical agent having an anti-HIV action, particularly, a pharmaceutical agent having an integrase inhibitory action, is provided. The present invention relates to a quinolizinone compound represented by the following formula [I] | 06/29/2010 |
| 7595327 | Beta-sulfonamide hydroxamic acid inhibitors of tace/matrix metalloproteinase This invention provides compounds of Formula I, having the structure: that are useful in treating diseases or disorders mediated by TNF-α, such as arthritis (rheumatoid arthritis (RA), juvenile RA, psoriatic arthritis, ost... | 09/29/2009 |
| 7569583 | Aryl-substituted polycyclic amines, method for the production thereof, and use thereof as a medicament The invention relates to aryl-substituted polycyclic amines of the formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and ... | 08/04/2009 |
| 7417055 | Kinase inhibitory phosphonate analogs The invention is related to phosphorus substituted kinase inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such com... | 08/26/2008 |
| 7329657 | Indazolyl-substituted pyrroline compounds as kinase inhibitors The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or am... | 02/12/2008 |
| 7304060 | Indazolyl-substituted pyrroline compounds as kinase inhibitors The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or am... | 12/04/2007 |
| 7282221 | Antiviral product, use and formulation thereof An antiviral product is comprised of at least three dosages forms, each of which has a different release profile, with the Cmax for the antiviral product being reached in less than about twelve hours. In one embodiment, there is an immediate release dosag... | 10/16/2007 |
| 7253182 | Enantiomerically pure basic arylcycloalkylhydroxycarboxylic esters, processes for their preparation and their use in medicaments Disclosed are enantiomerically pure cyclic aminoalcohol esters of arylcycloalkylhydroxycarboxylic acids with at least 90% enantiomeric excess of the (3R,2′R), (3S,2′R), (3R,2′S), or (3S,2′S) configured enantiomer. ... | 08/07/2007 |
| 7229996 | Rifamycin derivatives Novel rifamycin derivatives of formula I (both hydroquinone and corresponding quinone (C1-C4) forms): or their salts, hydrates or prodrugs thereof, wherein: a preferred R comprises... | 06/12/2007 |
| 7226931 | (R/S) rifamycin derivatives, their preparations and pharmaceutical compositions Rifamycin derivatives having the following structure of general formula I (both hydroquinone and corresponding quinone (C1-C4) forms): or its salts, hydrates or prodrugs thereof; wherein a p... | 06/05/2007 |
| 7223773 | 4-oxoquinolizine antibacterial agent having 2-pyridone skeleton as partial structure The present invention provides a 4-oxoquinolizine antibacterial agent having a 2-pyridone skeleton as a partial structure and also having a strong antibacterial effect on gram-positive bacteria, gram-negative bacteria or anaerobic bacteria. The compound having the f... | 05/29/2007 |
| 7160898 | Pharmacological treatment for sleep apnea The present invention relates to pharmacological methods for the amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity. ... | 01/09/2007 |
| 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... | 10/24/2006 |
| RE39300 | Inhibiting the development of tolerance to and/or dependence on an addictive substance Nontoxic substances that block the N-methyl-D-aspartate (NMDA) receptor, e.g., a morphinan such as dextromethorphan or dextrorphan, or that block a major intracellular consequence of NMDA-receptor activation, e.g., a ganglioside such as GM1 or GT1b | 09/19/2006 |
| 7105701 | β2-adrenergic receptor agonists Disclosed are multibinding compounds which are β2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.... | 09/12/2006 |
| 7041677 | Use of monochloroflosequinan in the treatment of sexual dysfunction The present invention described the administration of halogenated flosequinan derivatives and the enantiomers of halogenated flosequinan derivatives for the treatment of sexual dysfunction (in males and females) and for the treatment of cardiovascular disease. ... | 05/09/2006 |
| 7041693 | Hydantoin derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE) The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein L, Z0, R1, R4, R5, a... | 05/09/2006 |
| 6962917 | Aminopiperidine quinolines and their azaisosteric analogues with antibacterical activity Aminopiperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man. ... | 11/08/2005 |
| 6900224 | Antimicrobial quinolones, their compositions and uses Compounds of the following formula: are effective antimicrobial agents. ... | 05/31/2005 |
| 6884806 | Bicyclic lactam derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE) The present application describes novel bicyclic lactam derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein A, B, C, D, R1, and R2 are defined in the present speci... | 04/26/2005 |
| 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 |
| 6878713 | Generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, their preparation, compositions and use as medicaments This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydr... | 04/12/2005 |
| 6870056 | Substitituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds useful inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of... | 03/22/2005 |
| 6841559 | Pyridinones to treat and prevent bacterial infections Novel pyridinones and their derivatives which are effective in treating or preventing Gram-negative bacterial infections are provided. The pyridinones are stable and easily derivatized; the methods by which these derivatizations occur is described. Two regioselectiv... | 01/11/2005 |
| 6762200 | Oxa(thia)zolidine derivative and anti-inflammatory drug The present invention provides medicinal compositions characterized by containing as the active ingredient either a compound represented by a general formula (1) or a pharmaceutically acceptable composite thereof, [where... | 07/13/2004 |
| 6762181 | Aminomethylpyrrolidine derivatives having aromatic substituents This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of th... | 07/13/2004 |
| 6743817 | Substituted fused pyrroleimines and pyrazoleimines Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists... | 06/01/2004 |
| 6740654 | Squaric acid derivatives Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —Sâ€... | 05/25/2004 |
| 6667315 | Cardioprotective phosphonates and malonates The present invention provides for pyridoxine phosphonate analogues such as, for example, ((2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)alkylphosphonates, and (2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)azaalkylphosphonates) and to pyridoxine malo... | 12/23/2003 |
| 6653309 | Inhibitors of IMPDH enzyme technical field of the invention The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for inhibit... | 11/25/2003 |
| 6632825 | Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis Compounds of the formula: ##STR1## where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containi... | 10/14/2003 |
| 6630488 | Quinolizinones as integrin inhibitors The present invention is directed towards novel compounds that are effective inhibitors of integrins, particularly IIbଲ.sub.3 or v integrins such as vଲ.sub.3 and vଲ.sub.5.... | 10/07/2003 |
| 6608079 | Indole derivatives and their use as 5-HT1F agonists The present invention relates to a compound of formula (I), or a pharmaceutical acid addition salt thereof, which are useful for activating 5-HT1F receptors and inhibiting neuronal protein extravasation in a mammal. ##STR1##... | 08/19/2003 |
| 6602882 | Quinoline derivatives and their use as antibacterial agents Piperidine derivatives and pharmaceutical derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.... | 08/05/2003 |