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| Number | Title | Issue Date |
| 7402606 | Derivatives of 1-(oxoaminoacetyl) pentylcarbamate as cathepsin K inhibitors for the treatment of bone loss Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle ... | 07/22/2008 |
| 7385065 | Derivatives of asimadoline with covalently bonded acids The present invention relates to derivatives of N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamide with covalently bonded acids, and to the salts, solvates and prodrugs thereof, to the derivatives as medicaments, to the use of th... | 06/10/2008 |
| 7314932 | Methods for minimizing thioamide impurities Methods for minimizing the formation of thioamide compounds using decoy agents during reactions, such as thionations of carbonyl compounds containing nitrite groups, are provided. ... | 01/01/2008 |
| 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 |
| 7232817 | α- and β-amino acid hydroxyethlamino sulfonyl urea derivatives useful as retroviral protease inhibitors α- and β-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. ... | 06/19/2007 |
| 7230119 | Process for the preparation of substituted pyrrolidine derivatives and intermediates Two syntheses are provided; one for the preparation of (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol, and other for the preparation of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol. (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is prepared using the achiral ylide prepared from ben... | 06/12/2007 |
| 7217706 | Propanolamine derivatives This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympatho... | 05/15/2007 |
| 7160902 | Amide derivatives and methods of their use Amide derivatives of the general formulae Ia and Ib: are disclosed. Pharmaceutical compositions containing these compounds, and methods for their use, inter alia, for treating and/or preventing gastrointestinal d... | 01/09/2007 |
| 7135578 | Iminocyclitol inhibitors of hexoaminidase and glycosidase Designed imminocyclitols have potent inhibition activity with respect to hexoaminidases and glycosidases. ... | 11/14/2006 |
| 7132543 | Para-phenylenediamine derivatives containing a disubstituted pyrrolidinyl group bearing a cationic radical, and use of the same for dyeing keratin fibers The present disclosure relates to a novel a para-phenylenediamine derivative substituted with a pyrrolidinyl group of formula (I) and the addition salts thereof. The present disclosure also relates to a dyeing composition for keratin fibers comprising the paraphenyl... | 11/07/2006 |
| 7091204 | Sulfonamides The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II. ... | 08/15/2006 |
| 7084165 | Monoamine reuptake inhibitors for treatment of CNS disorders The present invention relates to compounds that are useful exhibit activity as serotonin, norepinephrine and dopamine reuptake inhibitors, and their pharmaceutically acceptable salts, and their use in the treatment of central nervous system and other disorders. ... | 08/01/2006 |
| 7026094 | Substituted oxime derivatives and the use thereof as latent acids New oxime sulfonate compounds of the formula (I) and (II), wherein R1 is C1-C12alkyl, C1C4haloalkyl, hydrogon, OR9, NR10R11, SR12 or is phenyl which is unsubstituted o... | 04/11/2006 |
| 6946468 | 3-mercaptopyrrolidines as farnesyl protein transferase inhibitors The present invention relates to inhibitors of ras farnesylation of the Formula I wherein: R1 is for example H and further values as defined in the specification; R2 | 09/20/2005 |
| 6936597 | Prodrugs of anticancer agents employing substituted aromatic acids Polymeric prodrugs of the formula: wherein B is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing m... | 08/30/2005 |
| 6933390 | Process for the arylation of aza-heterocycles with activated aromatics in presence of caesium carbonate The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of fur... | 08/23/2005 |
| 6923835 | Bis-para-phenylenediamine derivatives comprising a pyrrolidyl group and use of these derivatives for dyeing keratin fibres The invention relates to novel bis-para-phenylenediamine derivatives containing a pyrrolidyl group substituted with a cationic radical, to dye compositions containing them and to the process of dyeing keratin fibres using these compositions. The present inven... | 08/02/2005 |
| 6900322 | Method for stereochemically controlled production of isomerically pure highly substituted azacyclic compounds A method for stereochemically controlled production of azacyclic compounds of general formula (I) in which the substituents have the meanings given in the specification. The invention also relates to intermediate produ... | 05/31/2005 |
| 6794519 | Process for the production of sulfonic esters Sulfonic acid ester derivatives represented by the general formula (4) or (5) are produced by reacting an amino alcohol derivative represented by the general formula (1) or (2) with an organic sulfonyl halide represented by the general formula (3), in a mixed solven... | 09/21/2004 |
| 6774140 | Iminocyclitol inhibitors of hexoaminidase and glycosidase Designed iminocylitols that have potent inhibition activity with respect to hexominidases and glycosides are disclosed. ... | 08/10/2004 |
| 6770764 | Trypsin substrate and diagnostic device, and method of using same A compound of the formula (I) wherein R1 is a protecting group for Nα, R2 is a protecting group for NG, and R3 is aryl, and wherein the compound of formula (I) is a trypsin su... | 08/03/2004 |
| 6720335 | Sulfonamide inhibitors of aspartyl protease The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. T... | 04/13/2004 |
| 6660756 | N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6 alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C... | 12/09/2003 |
| 6624314 | Pyrrolothiazine and pyrrolothiazepine compounds having serotonin-2 receptor antagonistic and alpha-1-blocking action A pyrrolesulfonamide derivative having the following formula (I): ##STR1## wherein the ring P represented by ##STR2## is a pyrrole ring having the following structure: ##STR3## wherein R represents alkyl, cycloalkyl, cycloalkylalkyl or aralky... | 09/23/2003 |
| 6624142 | Trimethyl lock based tetrapartate prodrugs The invention is directed primarily to compounds of Formula I: ##STR1## wherein: R1 is a polymeric residue; L1 is a bifunctional linking group; Y1 and Y2 are independently O, S or NR7 ; R2-... | 09/23/2003 |
| 6590106 | Amino acid derivatives and methods of making the same Disclosed are novel compounds represented by Structural Formula II, IX or XXVIII: ##STR1## R1, R2, and R22 are independently an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic ... | 07/08/2003 |
| 6576780 | Hydroxyamidino derivatives useful as nitric oxide synthase inhibitors The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.... | 06/10/2003 |
| 6541491 | 4-mercaptopyrrolidine derivatives as farnesyl transferase inhibitors Pharmaceutical compositions comprising an inhibitor of ras farnesylation of formula (I) wherein, R1 is for example H and further values as defined in the specification; R2 is for example H and further values as defined in the specifi... | 04/01/2003 |
| 6534523 | Hepatitis C inhibitor tri-peptides Racemates, diastereoisomers and optical isomers of a compound of formula (I): ##STR1## wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alk... | 03/18/2003 |
| 6518437 | Process and intermediate compounds for the preparation of pyrrolidines Processes for the preparation of pyrrolidones (7 and 8) and pyrrolidines (9 and 10) from tri-O-acetyl-D-erythro-4-pentulosonic acid esters are described. The compounds are aza sugar analogs of D-ribofuranoside and are intermediates to drugs which regulate... | 02/11/2003 |
| 6518312 | Immune enhancement A method for stimulation of transcription factor AP (activator protein)-1 by administering a compound of the formula (I) ##STR1## wherein R is selected from methyl, ethyl, n-propyl, iso-propyl, c-propyl, n-butyl, sec.-butyl, iso-butyl, tert.-butyl, c-buty... | 02/11/2003 |
| 6503940 | Prodrugs for antimicrobial amidines A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I): ##STR1## wherein: X may be O, S, or NR' wherein R' is H or loweralkyl, R1 and R2 may be indepen... | 01/07/2003 |
| 6495546 | Propanolamine derivatives Propanolamine derivatives represented by the following formula (I): ##STR1## These derivatives may be 댣 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria ac... | 12/17/2002 |
| 6479669 | Amino acid derivatives and methods of making the same Disclosed are novel compounds, and methods of making the same, represented by Structural Formula II, IX or XXVII: ##STR1## The compounds can be used to prepare combinatorial libraries based on a multicomponent Ugi reaction.... | 11/12/2002 |
| 6455573 | Glycosidase inhibitors and methods of synthesizing same A method for synthesizing Salacinol, its stereoisomers, and non-naturally occurring selenium and nitrogen analogues thereof having the general formula (I): ##STR1## The compounds are potentially useful as glycosidase inhibitors. The synthetic schemes... | 09/24/2002 |
| 6451819 | Heterocyclic compounds useful as NMDA receptor selective subtype blockers The invention relates to treating neurodegeneration by selective blocking of NMDA receptor with compounds of formula ##STR1## wherein Ar1 is pyridyl or phenyl, substituted by hydroxy, lower alkyl, halogen, amino, nitro, benzyloxy or lower alkox... | 09/17/2002 |
| 6448286 | Imino pyrrolidine derivatives useful as nitric oxide synthase inhibitors The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.... | 09/10/2002 |
| 6436967 | Process for preparing prodrugs of benzenesulfonamide-containing cox-2 inhibitors This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to prodrugs of compounds which selectively inhibit cyclooxygenase-2. The use of non-steroidal antiinflammatory drugs (NSAIDs) in treating pain and the swelli... | 08/20/2002 |
| 6414163 | Process and intermediate compounds for the preparation of pyrrolidines Processes for the preparation of pyrrolidones (7 and 8) and pyrrolidines (9 and 10) from tri-O-acetyl-D-erythro-4-pentulosonic acid esters are described. The compounds are aza sugar analogs of D-ribofuranoside and are intermediates to drugs which regulate... | 07/02/2002 |
| 6392046 | Sulfonamide inhibitors of aspartyl protease The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical ... | 05/21/2002 |