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| Number | Title | Issue Date |
| 7696346 | Production method The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereo... | 04/13/2010 |
| 7638625 | Crystalline compounds The present invention relates to the new crystalline compounds A of general formula I wherein A1, A2, A3, X, Y1, Y2 and Y3 are defined as in claim 1, ... | 12/29/2009 |
| 7473778 | 3-(4-piperidinyl)-2,3,4,5-tetrahydro-1,3-benzodiazepin-2(1H)-one The present invention relates to a process for preparing the compound 3-(4-piperidinyl)-2,3,4,5-tetrahydro-1,3-benzodiazepin-2(1H)-one of formula which is to be found as a structural element in CGRP antagonists which are suitable above all for the oral therapy of mi... | 01/06/2009 |
| 7439237 | Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions The present invention relates to the CGRP antagonists of general formula wherein A, X and R1 to R3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the hydrates ther... | 10/21/2008 |
| 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 |
| 7259160 | Hexahydrodiazepinones as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes The present invention is directed to hexahydrodiazepinone compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is in... | 08/21/2007 |
| 7205292 | CGRP receptor antagonists The present invention is directed to compounds of Formula I and Formula II: (where variables R1, R2, R3, R4, R6, A, B, G, J, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the ... | 04/17/2007 |
| 7205294 | Selected CGRP-antagonists process for preparing them and their use as pharmaceutical compositions The present invention relates to substituted piperidines of general formula wherein A, B, D, E, X, R1 and R2 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the... | 04/17/2007 |
| 7183260 | C-terminal modified oxamyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inf... | 02/27/2007 |
| 7141667 | 3-(4-piperidinyl)-2,3,4,5-tetrahydro-1,3-benzodiazepin-2(1H)-one The present invention relates to a process for preparing the compound 3-(4-piperidinyl)-2,3,4,5-tetrahydro-1,3-benzodiazepin-2(1H)-one of formula which is to be found as a structural element in CGRP-antagonists, ... | 11/28/2006 |
| 7132535 | Process for preparing hexahydropyridazine-3-carboxylic acid derivatives According to the process of the invention, the hexahydropyridazine-3-carboxylic acid derivatives are prepared by reacting a compound of formula (II) with a compound of formula (III) | 11/07/2006 |
| 7053056 | C-terminal modified oxamyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inf... | 05/30/2006 |
| 7026312 | Substituted piperidines, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof The present invention relates to substituted piperidines of general formula wherein R, R2 to R5, A, X, Z and n are defined as in claim 1, the tautomers, diastereomers, enantiomers, mixtures and sa... | 04/11/2006 |
| 6949541 | Substituted piperidines, medicaments containing these compounds, and methods for the production thereof The present invention relates to substituted piperidines of general formula wherein A1, A2, R, R1 and R2 are defined as in claim 1, the tautomers, the diastereom... | 09/27/2005 |
| 6867298 | Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or a... | 03/15/2005 |
| 6825191 | Benzodiazepine derivatives The present invention provides benzodiazepine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of inhibiting activated blood-coagulation factor X. The... | 11/30/2004 |
| 6759404 | Cyclic malonamides as inhibitors of aβ protein production Novel cyclic malonamides having the formula (I): and their pharmaceutical compositions. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-pept... | 07/06/2004 |
| 6703500 | Method of preparing bicyclic intermediates from piperazic acid or an ester thereof useful in the manufacture of caspase inhibitors The invention relates to a process for synthesizing piperazic acid and similar, ring-containing acids. The invention also relates to a process for simultaneously N(2)-acylating piperazic acid or an ester thereof and forming a bicyclic ring structure. The ... | 03/09/2004 |
| 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 |
| 6632942 | Asymmetric synthesis of piperazic acid and derivatives thereof This invention provides a concise, asymmetric synthesis of piperazic acid and derivatives thereof, whereby either the (3S)- or (3R)-enantiomeric form may be obtained with high optical purity. (3S)-piperazic acid is derived from D-glutamic acid through an ... | 10/14/2003 |
| 6600036 | Condensed 2,3-benzodiazepine derivatives and their use as AMPA-receptor inhibitors Compounds of formula I are described, their production and use in pharmaceutical agents. ##STR1##... | 07/29/2003 |
| 6573259 | Inhibitors of interleukin-1ଲ converting enzyme The present invention relates to novel classes of compounds which are inhibitors of interleukin-1ଲ converting enzyme ("ICE"). This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical com... | 06/03/2003 |
| 6559304 | Method for synthesizing caspase inhibitors The invention relates to a process for simultaneously N(2)-acylating piperazic acid or an ester thereof and forming a bicyclic ring structure. The invention also relates to the use of that process step in a method of synthesizing a bicyclic compound usefu... | 05/06/2003 |
| 6551761 | Photoactivatable nitrogen-containing bases based on -ammonium ketones, iminium ketones or amidinium ketones and aryl borates This invention relates to -ammonium ketones, iminium ketones or amidinium ketones in the form of their tetraaryl- or triarylalkylborate salts which can be photochemically converted into amines, imines or amidines as well as to a process for their p... | 04/22/2003 |
| 6548664 | Octahydro-6, 10-dioxo-6h-pyridazino/1,2-a/ /1,2/diazepin-1-carboxylic acid, derivatives, preparation method and use for preparing therapeutically active compounds The invention concerns compounds of formula (I) in SR configuration or in the form of a SR+SS mixture, wherein R represents a hydrogen atom, an alkyl or aralkyl radical containing up to 18 carbon atoms, the amine function being free or protected. The comp... | 04/15/2003 |
| 6512111 | Process for the preparation of bicyclic compounds and the use of this process for the preparation of an ice inhibitor compound A method for preparing compounds of formula (I) ##STR1## wherein R is selected from the group consisting of H. alkyl, aryl, and aralkyl of up to 18 carbon atoms and the amine function may be free or protected from a compound of formula (IA) wherein cycliz... | 01/28/2003 |
| 6509328 | Glutamate receptor antagonists The present invention is a compound of formula ##STR1## wherein X is an ethynediyl group, R1, R2 and R3 are as defined in the specification.... | 01/21/2003 |
| 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 |
| 6432944 | Benzodiazepinone ଲ-amyloid inhibitors: arylacetamidoalanyl derivatives There is provided a series of arylacetamidoalanyl derivatives of benzodiazepinones of Formula I ##STR1## wherein R1 through R7 and n are defined herein, which are inhibitors of ଲ-amyloid peptide (ଲ-AP) production and are ... | 08/13/2002 |
| 6433164 | (3,4,7,8,9,10-hexahydro-6, 10 -6H-pyridazino [1,2-a] [1,2] diazepine-1-carboxylic-acid derivatives A compound of the formula ##STR1## wherein R is alkyl or aralkyl of up to 18 carbon atoms, the amine function being optionally protected are used to prepare compounds of the formula ##STR2## in which R retains its previous meaning and the amine is optiona... | 08/13/2002 |
| 6426413 | Inhibitors of caspases The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1ଲ converting enzyme ("ICE") inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The c... | 07/30/2002 |
| 6423840 | Inhibitors of interleukin-1ଲ converting enzyme The present invention relates to novel classes of compounds which are inhibitors of interleukin-1ଲ converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also rel... | 07/23/2002 |
| 6416922 | Azomethine dye precursor, image-forming material, and image-forming method The present invention related to an azomethine dye precursor represented by the following general formula (1) and the image-forming material and image-forming method using the azomethine dye precursor: wherein Ar represents an aryl group or a heterocyclic... | 07/09/2002 |
| 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 |
| 6344449 | Modified aminoacids, pharmaceuticals containing these compounds and method for their production The present invention relates to modified amino acids of general formula ##STR1## wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers,... | 02/05/2002 |
| 6331640 | Diaminopropionic acid derivatives A compound of formula 1a ##STR1## which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.... | 12/18/2001 |
| 6258948 | Inhibitors of Interleukin-1ଲ converting enzyme The present invention relates to novel classes of compounds which are inhibitors of interleukin-IB converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates t... | 07/10/2001 |
| 6258947 | (3,4,7,8,9,10-hexahydro-6,10-dioxo-6H pyridazino[1,2-A] [1,2] diazepine-1-carboxylic acid derivatives A compound of the formula ##STR1## wherein R is alkyl or aralkyl of up to 18 carbon atoms, the amine function being optionally protected are used to prepare compounds of the formula ##STR2## in which R retains its previous meaning and the amine is optiona... | 07/10/2001 |
| 6235899 | Method for preparing alkyloxy furanone derivatives, compounds obtained by said method and use of said compounds The invention relates to a novel process for preparing compounds of the formula (IV) or (I): ##STR1## from the racemic alkoxyfuranone of the formula (II): ##STR2## R1 and R2 being as defined in the description, to the novel comp... | 05/22/2001 |
| 6204261 | Inhibitors of interleukin-1ଲ Converting enzyme inhibitors The present invention relates to pyradazino[1,2-a][1,2]diazepine-1-carboxamide compounds of formula: ##STR1## which compounds are inhibitors of interleukin-1beta converting enzyme.... | 03/20/2001 |
