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| Number | Title | Issue Date |
| 6562975 | Process for preparing zolpidem The invention relates to a process for preparing a compound of formula (I) ##STR1## wherein a compound of formula (II), ##STR2## wherein R1 denotes chlorine, bromine, iodine, --O--COCH3, tosylate or mesylate, is reacted with a compo... | 05/13/2003 |
| 6555558 | Oral dosage self-emulsifying formulations of pyranone protease inhibitors A microemulsion of pyranone protease inhibitor compounds that is substantially free of alcohol and propylene glycol comprising a pyranone protease inhibitor, one or more pharmaceutically acceptable surfactants, and a polyethylene glycol solvent having a m... | 04/29/2003 |
| 6545035 | Substituted indolinones with kinase inhibitory activity Substituted indolinones of general formula ##STR1## having effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells. Exemplary compounds are: 3-Z-[1-(4-(N-Benzyl-N-methyl-aminomethyl)-phenylamino)-1-methyl-methylene]... | 04/08/2003 |
| 6525045 | Positive allosteric AMPA receptor modulators The present invention relates to new positive allosteric AMPA receptor modulators of general formula (I) ##STR1## wherein R1, R2 R3, R4, R5 and R6 may have the meanings indicated in the spe... | 02/25/2003 |
| 6512000 | Aminocarbonyl-substituted benzimidazoles having tryptase-inhibitory activity A method for treating diseases in which tryptase inhibitors may be of thereapeutic value, which comprises the administration of a thereapeutic amount of a compound of the formula ##STR1## The invention also comprises novel compounds of the formula (I). Exempla... | 01/28/2003 |
| 6492408 | Small molecules useful in the treatment of inflammatory disease Compounds of the formula I ##STR1## which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary are: ##STR2##... | 12/10/2002 |
| 6479524 | Substituted aryl and heteroaryl derivatives, their production and their use as medicines Compounds that prolong thrombin time. Exemplary are: (a) rac-4-{3-[5-ethoxycarbonylmethyl-2-methyl-4-(2-methyl-pyrrolidinocarbonyl) -phenyl]-propargylamino}benzamidine, (b) rac-4-{3-[2,5-dimethyl-4-(2-methyl-pyrrolidinocarbonyl)-phenyl]-propargyla mino... | 11/12/2002 |
| 6451832 | Benzimidazoles with antithrombotic activity Novel benzimidazoles having antithrombotic activity. Exemplary are: (a) 2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(ethoxycarbonylmethylamino)-1 -(2,5-dihydropyrrolocarbonyl)-ethyl]-benzimidazole, (b) 2-[4-(N-phenylcarbonylamidino)-phenylaminomethyl]-1-m... | 09/17/2002 |
| 6420359 | Non-nucleoside reverse transcriptase inhibitors Provided are compounds of the general formula I: ##STR1## wherein R2 is selected from the group consisting of H, F, Cl, (C1-4) alkyl, (C3-4) cycloalkyl and CF3 ; R4 is H or Me; R5 is H, Me ... | 07/16/2002 |
| 6420380 | 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... | 07/16/2002 |
| 6417382 | Process for preparing aryl-iminomethyl-carbamino acid esters The invention relates to a process suitable for large-scale industrial use for preparing compounds of general formula (I) ##STR1## wherein: R1 denotes a group selected from among methyl, ethyl, propyl, cyclopentyl, cyclohexyl, phenyl, benzyl an... | 07/09/2002 |
| 6414153 | 1-phenylpydrrolidin-2-ones and -thiones and 1-(4-pyridyl)pydrrolidin-2-ones and -thiones which are useful in the treatment of inflammatory disease Novel compounds of the formula I: ##STR1## which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are: 3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-1,3-dihydroindol-2-one; 3-(4-bromobenzyl)-1-(3,5-dichloroph... | 07/02/2002 |
| 6414161 | Synthesis of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo[1 ,2-a]imidazol-2-one A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl- 1-H-imidazo[ 1 ,2-a]imidazol-2-one (1): ##STR1## This compound is useful as an intermediate in the preparation of certain small molecules that are us... | 07/02/2002 |
| 6413990 | Arylsulphonamide-substituted benzimidazoles having tryptase-inhibiting activity Bezimidazole derivatives of general formula (I) ##STR1## having tryptase-inhibitory activity. Exemplary are: N-{2-[2-(4-amidinophenyl)-ethyl]-1-methyl-benzimidazol-5-yl}-N-diethylamino ethyl-(4-ethoxycarbonyl-benzenesulphonamide)-hydrochloride, N-{2-[2-(4-amidi... | 07/02/2002 |
| 6410742 | Polymorphs of telmisartan The invention relates to polymorphs of 4'-[2-n-propyl-4-methyl-6-(l-methylbenzimid azol-2-yl)benzimidazol-1-ylmethyl]biphenyl-2-carboxylic acid (INN: telmisartan), particularly polymorphic form B, mixtures of the polymorphs, processes for preparing t... | 06/25/2002 |
| 6410531 | 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... | 06/25/2002 |
| 6407130 | Carboxamide-substituted benzimidazoles having tryptase-inhibiting activity The invention relates to carboxamide-substituted benzimidazole derivatives of general formula (I) ##STR1## wherein the groups R1, R2, R3 and R4 may have the meanings given in the claims and in the specification,... | 06/18/2002 |
| 6403580 | Quinazolines, pharmaceutical compositions containing these compounds, their use and processes for preparing them Quinazolines of the formula ##STR1## having an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract, and the preparation ... | 06/11/2002 |
| 6399781 | Process for making 3-amino-2-chloro-4-methylpyridine A method for making 3-amino-2-chloro-4-methylpyridine, as shown in Scheme 12, below. ##STR1##... | 06/04/2002 |
| 6390088 | Aerosol inhaler In an aerosol inhaler it is proposed that a thermal sensor 5 be arranged in the region of the atomization nozzle 4, which sensor, following the actuation of an actuating element and the triggering of an inhalation process, undergoes cooling as a result of... | 05/21/2002 |
| 6365615 | Small molecules useful in the treatment of inflammatory disease Novel compounds of the formula I ##STR1## which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are: 2-(3,5-Dichlorophenyl)-7-(R*)-phenyl-7a-(R*)-tetrahydropyrrolo[1,2-c]imidaz ole-1,3-dione; 2-(3,5... | 04/02/2002 |
| 6365584 | Arylysulphonamide-substituted benzimidazoles having tryptase-inhibiting activity Arylsulphonamide-substituted benzimidazole derivatives of formula (I) ##STR1## having tryptase-inhibiting activity. Exemplary are: 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethylaminoethyl)-benzenesu lphonylamino]-benzimidazole; 1-Methyl-2-[2-(4-amidinop... | 04/02/2002 |
| 6362210 | Carboxylic acid amides, pharmaceutical compositions containing these compounds and their use Carboxylic acid amides of general formula ##STR1## which inhibit telomerase and are useful for treating tumour diseases such as carcinomas, sarcomas and leukaemias. Exemplary compounds are: (1) trans-3-(naphth-2-yl)-but-2-enoic acid-N-(2-carboxy-phenyl)-amide,... | 03/26/2002 |
| 6358986 | Polymorphs of telmisartan The invention relates to polymorphs of 4'-[2-n-propyl-4-methyl-6-(1-methylbenzimid-azol-2-yl)benzimidazol-1-ylmet hyl]biphenyl-2-carboxylic acid (INN: telmisartan), particularly polymorphic form B, mixtures of the polymorphs, processes for preparing telmis... | 03/19/2002 |
| 6355664 | Phenylpyrrolidines, phenylimidazolidines, 3-phenyl-1,3-oxizolidines and 3-phenyl-1,3-thiazolidines and their use in the treatment of inflammatory disease A method treating or preventing inflammatory and immune cell-mediated diseases by the administration of certain novel and known small molecules. Exemplary of the novel compounds are those of the following structural formulas: ##STR1## ##STR2##... | 03/12/2002 |
| 6355652 | Substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines and their use as pharmaceutical compositions Substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines of general formula 1: ##STR1## wherein: R1 and R2, which may be identical or different, are each hydrogen, C1 -C6 -alkyl, C1 -C6... | 03/12/2002 |
| 6353013 | Small molecules useful in the treatment of inflammatory disease Novel compounds of the formula I ##STR1## which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are: 5-(R)-(4-bromobenzyl)-3-(3-chloro-5-nitrophenyl)-5-methylimidazoline-2,4-di one; and, 5-(R)-(4-br... | 03/05/2002 |
| 6350763 | Small molecules useful in the treatment of inflammation disease Novel compounds of the formula I ##STR1## which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are: 1-acetyl-5-(R)-(4-bromobenzyl)-3-(2,6-dichloropyridin-4-yl)-5-methylimidazo line-2,4-dione; 5-(R)... | 02/26/2002 |
| 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 |
| 6329379 | 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... | 12/11/2001 |
| 6329417 | Hepatitis C inhibitor tri-pepitides Racemates, diastereolsomers 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 ... | 12/11/2001 |
| 6323180 | Hepatitis C inhibitor tri-peptides A racemate, diastereoisomer and optical isomer 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 may be optionally substituted with C1-... | 11/27/2001 |
| 6319918 | Substituted indolinones with kinase inhibitory activity Substituted indolinones of general formula ##STR1## having effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells. Exemplary compounds are: 3-Z-[1-(4-(N-Benzyl-N-methyl-aminomethyl)-phenylamino)-1-methyl-methylene]... | 11/20/2001 |
| 6306580 | Preparation of human papillomavirus E1 having helicase activity and method therefor The present invention relates to a method for isolating cloned papillomavirus E1 protein from a eukaryotic expression system having demonstrable and reproducible viral helicase activity and preparation containing essentially pure E1 protein. The invention... | 10/23/2001 |
| 6299861 | Ipratropium bromide enantiomer with prolonged duration of effect On account of the surprisingly powerful and long-lasting effect thereof, the salts of the L-(-)-enantiomer of (endo, syn)-(-)-3-(3-hydroxy-1-oxo-2-phenylpropoxy)-8-methyl-8-(methylethyl)-8-az oniabicyclo [3,2,1]octane are suitable as active substances for ... | 10/09/2001 |
| 6294194 | Method for extraction and reaction using supercritical fluids Methods for removing soluble material from confined spaces within substrates such as containers, capsules and porous powders comprising extraction with supercritical fluids, the pressure of which is preferably modulated between an upper level and a lower ... | 09/25/2001 |
| 6291640 | Peptidomimetic inhibitors of the human cytomegalovirus protease A compound of formula (I) is disclosed: ##STR1## wherein X, z, W, Y, R1 through R5, m and n are as define herein. These compounds are peptidomimetic inhibitors of human cytomegalovirus (HCMV) protease and are useful for the treatment of h... | 09/18/2001 |
| 6277872 | Oxadiazoles, processes for their preparation and their use as medicaments The invention relates to oxadiazole derivatives of general formula (I) ##STR1## wherein X, Y, Z and R1 are defined as described in the specification and claims, processes for preparing them and their use as pharmaceutical compositions.... | 08/21/2001 |
| 6268207 | Enzymatic resolution of 1-amino-2-vinylcyclopropyl caboxylic acid methyl ester An enantiomeric-resolving process for obtaining (1R,2S)-1-amino-2-vinylcyclopropyl carboxylic acid methyl ester by use of an esterase, and especially Alcalase.RTM., is disclosed.... | 07/31/2001 |
| 6265612 | Benzamidine derivatives and the use thereof as medicaments with LTB4-antagonistic effect The present invention relates to new benzamidine derivatives, processes for preparing them and their use in pharmaceutical compositions. The new benzamidine derivatives correspond to general formula 1 ##STR1##... | 07/24/2001 |
