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| Number | Title | Issue Date |
| 7709640 | Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such ki... | 05/04/2010 |
| 7381822 | Diagnostic and therapeutic alkyl piperidine/piperazine compounds and process Piperidine or piperazine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided. The compounds are characterized by the formulae: | 06/03/2008 |
| 7323563 | Hydroxamic acid derivatives as antibacterials A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily accepta... | 01/29/2008 |
| 7211670 | Method for producing 3-amidinophenylalanine derivatives The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture c... | 05/01/2007 |
| 7208496 | Substituted heterocyclic compounds Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, inte... | 04/24/2007 |
| 7208497 | Substituted piperazines and diazepanes A novel class of substituted piperazines and diazepanes, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment of dis... | 04/24/2007 |
| 7030115 | N-sulfonylurea apoptosis promoters Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds. ... | 04/18/2006 |
| 7019003 | Peptide deformylase inhibitors Novel PDF inhibitors and novel methods for their use are provided. ... | 03/28/2006 |
| 6992190 | Hydroxamic acid derivatives as antibacterials A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily accepta... | 01/31/2006 |
| 6951861 | Chemical compounds The invention relates to piperazine derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to their medical use. The novel compounds are antagonists of tachykinins, including substance P and other neurokinins. ... | 10/04/2005 |
| 6906074 | 2-phenylpiperazine derivatives A 2-phenylpiperazine derivative represented by the formula (I) or a pharmaceutically acceptable salt, hydrate, or complex thereof: wherein each of X1 and X3 is oxygen or two hydrogen atoms, X... | 06/14/2005 |
| 6903092 | Naphthamide neurokinin antagonists for use as medicaments Compounds having the general formula wherein R1, R2, R3, R4, R5, X1 and X2 are as defined in the specification, methods of using such compoun... | 06/07/2005 |
| 6897209 | Labelled factor XIIIa substrates A complex of a radiometal or paramagnetic metal ion with a metal chelating agent such as a diaminedioxime has attached thereto a substituent of formula (Y)m-A-NHR)k can function as a substrate for the fibrin-stabilizing Factor XIIIa. The comple... | 05/24/2005 |
| 6861435 | Urokinase inhibitors The invention relates to the compounds of general formula (I), that are present with respect to R1 as racemates as well as L- or D-configured compounds and as E/Z mixtures as well as E or Z isomers and in which the various symbols are defined as in the de... | 03/01/2005 |
| 6723730 | Capsaicin receptor ligands Disclosed are diaryl piperazines and related compounds of the following Formula: wherein the variables are as defined in the specification. These compounds are selective modulators of capsaicin receptors, including human... | 04/20/2004 |
| 6683184 | Piperazine derivatives and process for the preparation thereof The present invention relates to a novel compound of formula (I) and its pharmaceutically acceptable acid addition salt, and process for the preparation thereof, which have strong antitumor activities and very low toxicity: ##STR1## wherein R | 01/27/2004 |
| 6673799 | Cyanophenyl derivative This application relates to a piperazino-substituted novel cyanophenyl derivative in which a substituted carbamoyl or substituted sulfamoyl group having an aryl, heterocyclic or the like group that may have a substituent group is bonded to one nitrogen at... | 01/06/2004 |
| 6653299 | Labelled factor XIIIa substrates A complex of a radiometal or paramagnetic metal ion with a metal chelating agent such as a diaminedioxime has attached thereto a substituent of formula --(Y)m --A--NHR, can function as a substrate for the fibrin-stabilizing Factor XIIIa. The co... | 11/25/2003 |
| 6593327 | Compounds and compositions as protease inhibitors The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.... | 07/15/2003 |
| 6462046 | Heterocycle derivatives as PPAR-gamma agonists Compounds having the structure ##STR1## are peroxisome proliferator-activated receptor-gamma (PPAR-gamma) selective agonists and as such are useful in the modulation of blood glucose and the increase of insulin sensitivity in mammals. This activity of the... | 10/08/2002 |
| 6362174 | Reduced dipeptide analogues as calcium channel antagonitsts The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma. The nov... | 03/26/2002 |
| 6316440 | Reduced dipeptide analogues as calcium channel antagonists ##STR1## The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma... | 11/13/2001 |
| 6255120 | Combinatorial library of substituted statine esters and amides via a novel acid-catalyzed rearrangement A combinatorial chemical library comprising a plurality of members of the Formula [S]--C(O)--L'-Z containing hydroxyamides is disclosed, in which [S] represents a solid support and L'-Z is a linker/compound residue. In this library, Z is ##STR1## and... | 07/03/2001 |
| 6211242 | Benzamide derivatives as vasopressin antagonists This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc. and represented by the general formula (I): ##STR1## wherein R1 is aryl optionally substituted with lower alkyl, etc., R2 is lower alkyl,... | 04/03/2001 |
| 6114325 | 1,2-di-substituted benzene-carboxamide derivative, hair growth promoter and external composition for skin using the same A 1,2-di-substituted benzene-carboxamide derivative or a salt thereof expressed by the following Formula (I); ##STR1## wherein each of A and B is R1 or --(CH2)n-NR2 R3, wherein when A is R1, B is... | 09/05/2000 |
| 6080860 | Methods of making ureas and guanidines including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefor Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediate... | 06/27/2000 |
| 6028195 | Piperazine derivatives and process for the preparation thereof The present invention relates to novel compound having strong antimumor activities of the general formula(I) ##STR1## wherein R1 and R2 are independently hydrogen, substituted or unsubstituted C1 -C8 alkyl,... | 02/22/2000 |
| 5981531 | Acid derivatives The invention concerns acid derivatives of formula I R1 --CON(R2)--N(R3)CO--X1 --Q--X2 --G and pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts th... | 11/09/1999 |
| 5952503 | Method for producing optically-active 2-piperazinecarboxylic acid derivatives Optically-active 2-piperazinecarboxylic acid derivatives are produced through diastereomer salt resolution using optically-active acidic amino acid derivative as the resolving reagent. In this method, the recovery of the resolving reagent used is high, an... | 09/14/1999 |
| 5945534 | Process for the preparation of optically active piperazine-2-carboxylic acid derivatives Optically active piperazine-2-carboxylic acid derivatives of the general formula: ##STR1## in which X is alkoxy or a (substituted) amino group, are prepared by asymmetric hydrogenation of the corresponding pyrazinecarboxylic acid derivatives, ca... | 08/31/1999 |
| 5922873 | Process for preparing N-tert-butyl-2-pyrazinecarboxamide and N-tert-butyl-2-piperazinecarboxamide A process for preparing a N-tert-butyl-2-pyrazinecarboxamide having the formula (2): ##STR1## which comprises reacting a cyanopyrazine having the formula (1): ##STR2## with tert-butyl alcohol in the presence of sulfuric acid and a process for ... | 07/13/1999 |
| 5908843 | Piperazine compounds as fibrinogen inhibitors Novel piperazine derivatives of formula I: Y--(Cm H2m --CHR1)n --CO--(NH--CHR2 --CO)r -- Z wherein ##STR1## R1, R2 and R7 are each, independently, --Ct | 06/01/1999 |
| 5892038 | Hydroxy-amino acid amides Compounds of Formula I ##STR1## are disclosed as inhibitors of plasmepsin and cathepsin D. The compounds are therefore useful to treat diseases such as malaria. In preferred compounds of formula I, Y is the residue of an N-acylated amino acid, a ... | 04/06/1999 |
| 5886181 | Process for the preparation of optically active piperazine-2-carboxylic acid derivatives Optically active piperazine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein R1 and R2 are inter alia hydrogen, alkyl or acyl and X is alkoxy or a (substituted) amino group, are prepared by asymmetric ... | 03/23/1999 |
| 5872262 | Hydroxy-amino acid amides Compounds of Formula I ##STR1## are disclosed as inhibitors of plasmepsin and cathepsin D. The compounds are therefore useful to treat diseases such as malaria. In preferred compounds of formula I, Y is the residue of an N-acylated amino acid, a ... | 02/16/1999 |
| 5866609 | Substituted vinylurea derivatives and medicine containing the same Disclosed herein are substituted vinylurea derivatives represented by the following general formula (1): ##STR1## wherein R1 and R3 are independently a phenyl group which may be substituted, R2 is a phenyl group which... | 02/02/1999 |
| 5861512 | Process for making HIV protese inhibitors Intermediates of structural formula ##STR1## can be made by reacting a primary or secondary amine with glycosidol or an activated derivative thereof. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.... | 01/19/1999 |
| 5856485 | Process for preparing 2-piperazinecarboxylic acid derivatives A process for preparing 2-piperazinecarboxamides in the form of their enantiomers or their enantiomer mixtures of the general formula: ##STR1## wherein R1 is (a) unsubstituted or substituted alkyl or (b) --OR4, wherein R4 | 01/05/1999 |
| 5840896 | Method of preventing or limiting reperfusion damage There is disclosed a process for preparing (l)-(-)-2-aminocarbonyl)-N-(4-amino-2,6-dichlorophenyl)-4-5,5-bis(4-fluor ophenyl)pentyl!-1-piperazineacetamide which comprises the steps of (a) cyclizing (-)-(S,S)-N1,N2 -bis(1-phenylethyl... | 11/24/1998 |
| 5811462 | HIV Protease inhibitors useful for the treatment of AIDS Peptide analogs containing norbornene are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical compositi... | 09/22/1998 |
