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| Number | Title | Issue Date |
| 7718795 | Succinoylamino benzodiazepines as inhibitors of aβ protein production This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifica... | 05/18/2010 |
| 7390801 | Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/... | 06/24/2008 |
| 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... | 04/15/2008 |
| 7115598 | Substituted 1,4-diazepines and uses thereof The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharm... | 10/03/2006 |
| 7109326 | Halo-alkoxycarbonyl prodrugs Halo-alkoxycarbonyl derivatives are provided as prodrug moieties for pharmaceutical agents containing a basic or polar nitrogen containing functionality. The prodrugs are provided as pharmaceutical compositions as well as in methods of treatment. ... | 09/19/2006 |
| 7105509 | Benzodiazepine derivatives as APP modulators A novel class of 1,4- and 1,5-benzodiazepines of formula (I) is disclosed. The compounds modulate the processing of amyloid precursor protein by γ-secretase, and hence find use in the treatment or prevention of conditions associated with the deposition of β-amyloi... | 09/12/2006 |
| 7067512 | Substituted 1,4-benzodiazepines and uses thereof The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or ... | 06/27/2006 |
| 7064121 | N-acylated lipophilic amino acid derivatives Compounds of structural Formula (I) where A is a lipophilic group including an aliphatic bridging group, B is a lipophilic group, D is a group having at least one amino or substituted amino group and R is hydrogen, alkyl or cycloalkyl, and pharmaceutically acceptabl... | 06/20/2006 |
| 7053084 | Succinoylamino benzodiazepines as inhibitors of Aβ protein production This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, mor... | 05/30/2006 |
| 6900222 | Pyrrolidinyl, piperdinyl 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 thereon wherein —Z1—Z2 | 05/31/2005 |
| 6686350 | Cell adhesion inhibitors The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of us... | 02/03/2004 |
| 6492553 | Methods for preparing N-[(aliphatic or aromatic)carbonyl)]-2-aminoaetamide compounds and for cyclizing such compounds A method for preparing a N-[(aliphatic or aromatic)carbonyl)]-2-aminoacetamide compound, and for preparing a cyclized compound therefrom, as well as novel resin bound intermediate compounds that are useful for preparing such compounds.... | 12/10/2002 |
| 6448270 | 4-substituted piperidine analogs and their use as subtype selective NMDA receptor antagonists Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using the 4-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions... | 09/10/2002 |
| 6403578 | Bicyclic fibrinogen antagonists This invention relates to compounds of the formulae: ##STR1## wherein A1 is O, S, N--R1 or CHR1 ; A4 is N--R4 or CHR4 ; R2 is a sidechain containing an acid or ester group; R1, ... | 06/11/2002 |
| 6288082 | Substituted 3-cyanoquinolines This invention provides compounds of formula I having the structure ##STR1## wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as... | 09/11/2001 |
| 6218387 | Vitronectin receptor anatagonists, their preparation and their use The present invention relates to compounds of the formula I, A--B--D--E--F--G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitro... | 04/17/2001 |
| 6207663 | Vitronectin receptor antagonists, their preparation and use Vitronectin receptor antagonists, their preparation and their use The present invention relates to compounds of the formula I A--B--D--E--F--G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as ... | 03/27/2001 |
| 6130234 | 4-substituted piperidine analogs and their use as subtype selective NMDA receptor antagonists Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions suc... | 10/10/2000 |
| 6121258 | 1,5-heterocyclic metalloprotease inhibitors The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibito... | 09/19/2000 |
| 6100254 | Inhibitors of protein tyrosine kinases Disclosed herein are small molecule, non-peptidyl inhibitors of protein tyrosine kinases, and methods for their use. The instant inhibitors are based on a 1,4-benzodiazepin-2-one nucleus. Methods are provided for inhibition of specific protein tyrosine ki... | 08/08/2000 |
| 6015791 | Serine protease inhibitors-cycloheptane derivatives The present invention relates to certain substituted oxadiazole, thiadiazole, and triazoles, in particular those including a cycloheptane structure, that are useful as serine protease inhibitors, including inhibitors for human neutrophil elastase. Compoun... | 01/18/2000 |
| 6011029 | Inhibitors of farnesyl protein transferase The present invention comprises benzodiazepine compounds having farnesyl transferase inhibitory activity.... | 01/04/2000 |
| 5962337 | Combinatorial 1,4-benzodiazepin-2,5-dione library A method has now been found of synthesizing a combinatorial library of 1,4-benzodiazepin-2,5-diones on solid supports via an aza-Wittig ring closure, said compounds optionally encoded with tags, and to the use of this library in assays to discover biologi... | 10/05/1999 |
| 5693637 | Bicycle derivatives, their preparation and use The description relates to bicyclene derivatives of formula (I) in which A, B, D, E, G, K, L, R1, R2, Z1 and Z2 have the meanings given in the description, and their production. These compounds are suitable for ... | 12/02/1997 |
| 5691331 | N-(2,4-Dioxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-3yl) -3- amides This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.... | 11/25/1997 |
| 5683998 | Tricyclic triazolo derivatives, processes for producing the same and the uses of the same Novel tricyclic triazolo derivatives and pharmaceutically acceptable salts thereof, which are useful as anti-inflammation agents, anti-allergy agents or anti-PAF agents as well as processes for producing the same are disclosed. The triazolo derivatives of... | 11/04/1997 |
| 5674865 | Nonpeptidyl integrin inhibitors having specificity for the GPIIb IIIa A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPIIb IIIa receptor and is provided in therapeutic compositions for t... | 10/07/1997 |
| 5674863 | Nonpeptidyl integrin inhibitors having specificity for the GPIIb IIIa receptor A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPIIb IIIa receptor and is provided in therapeutic compositions for t... | 10/07/1997 |
| 5438035 | Methods for controlling undesirable plant species with benzodiazepine compounds There are provided methods for controlling undesirable plant species with benzodiazepine compounds of formulas I and II ##STR1## Further provided are herbicidal compositions comprising those compounds.... | 08/01/1995 |
| 5416083 | Benzodiazepinyl-terminated non-peptidyl -succinamidoacyl aminodiols as anti-hypertensive agents Non-peptidyl compounds characterized generally as -succinamidoacyl aminodiols having a benzodiazepinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.... | 05/16/1995 |
| 5403836 | Benzazepine platelet aggregation inhibitors having specificity for the GPIIb IIIa receptor A benzazepine derivative that acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPIIb IIIa receptor and is provided in therapeutic compositions for the treatm... | 04/04/1995 |
| 5393760 | Guanidine derivatives Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The co... | 02/28/1995 |
| 5175159 | 3-substituted-1,4-benzodiazepines as oxytocin antagonists Compounds of Formula I are antagonists of oxytocin and are useful in the treatment of preterm labor and dysmenorrhea, and for stoppage of labor prepatory to Caesarean delivery. ##STR1##... | 12/29/1992 |
| 4820834 | Benzodiazepine analogs Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).... | 04/11/1989 |
| 4808605 | Tetrahydronaphthalene derivatives as calcium antagonists Compounds of the formula ##STR1## wherein R is lower-alkyl, R1 is halogen, R2 is C1 -C12 -alkyl, R3 is hydroxy, lower-alkoxy, lower-alkyl-carbonyloxy, lower-alkoxy-lower-alkylcarbonoyloxy, lower-... | 02/28/1989 |
| 4775671 | Imidazodiazepines There is presented compounds of the formula ##STR1## wherein A together with the two carbon atoms denoted by and ଲ signifies one of the groups ##STR2## and the dotted line signifies the double bond present in cases (1), (2) an... | 10/04/1988 |
| 4772696 | Oxadiazolyl imidazobenzodiazepine process New oxadiazolyl imidazobenzodiazepine derivatives having the formula ##STR1## wherein R3 has the formula ##STR2## wherein R" is hydrogen, C1-6 alkyl C1-6 alkoxymethyl or C3-6 -cycloalkyl; R4... | 09/20/1988 |
| 4594191 | Process for preparing a benzodiazepinedione derivative A non-fermentation process for preparing a benzodiazepinedione of the formula: ##STR1## and intermediates is disclosed.... | 06/10/1986 |
| 4576750 | Tryptophan derivative A non-fermentation process for preparing a benzodiazepinedione of the formula: ##STR1## and intermediates are disclosed.... | 03/18/1986 |
| 4554272 | Substituted quinazolino-1,4-benzodiazepin-6,9-diones and their preparation Tetracyclic compounds of the formula: ##STR1## and a process for their preparation are disclosed. The compounds have cholecystokinin inhibiting activity.... | 11/19/1985 |
