"That the automobile has practically reached the limit of its development is suggested by the fact that during the past year no improvements of a radical nature have been introduced."
Scientific American ; Jan. 2 edition, 1909
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| Number | Title | Issue Date |
| 7250410 | Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses thereof The invention concerns novel benzodiazepine derivatives and their uses in the field of therapeutics particularly for treating pathologies involving the activity of a cyclic nucleotide phosphodiesterase. It also concerns methods for preparing them and novel synthesis... | 07/31/2007 |
| 7029918 | Water-soluble derivatives of lipophilic drugs A water-soluble reference standard is useful for immunoassays of a lipophilic drugs. The reference standard is a compound of formula (I): G-(L)nāY;āā(I) where G is a lipophilic drug; L is a linker which is an alkyl group or heter... | 04/18/2006 |
| 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 |
| 6765005 | Fab I inhibitors Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections: ... | 07/20/2004 |
| 6756511 | Gamma-secretase inhibitors Gamma-secretase inhibitors, useful in the treatment or prevention of Alzheimer's disease, are disclosed. The preferred compounds have, as the central portion of the molecule, the structure (a) and are di-astereoisomers of known protease inhibitors. | 06/29/2004 |
| 6503903 | Fab I inhibitors Compounds of the formula (I) are disclosed which are FabI inhibitors and are useful in the treatment bacterial infections: ##STR1## wherein: R1 is H, C1-6 alkyl or Ar--C0-6 alkyl; R2 is H, C1-6 alkyl, Ar--... | 01/07/2003 |
| 6232308 | Bezazepine derivatives as v integrin receptor antagonists The present invention relates to benzazepine derivatives and their use as v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors v댣, v댥, and/o... | 05/15/2001 |
| 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 |
| 6008214 | Bicyclic compounds This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, which are effective for inhibiting platelet aggregation and bone resorption, pharmaceutical compositions for effecting such activity, and a me... | 12/28/1999 |
| 5985869 | Benzoheterocyclic compounds Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R2 is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy,... | 11/16/1999 |
| 5891852 | Serine protease inhibitors-cycloheptane derivatives The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respira... | 04/06/1999 |
| 5580979 | Phosphotyrosine peptidomimetics for inhibiting SH2 domain interactions The present invention makes available novel compounds represented by the general formula ##STR1## wherein Y represents a phosphate analog. Which compounds are useful for inhibiting an interaction between a protein containing an SH2 domain and a ... | 12/03/1996 |
| 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 |
| 5324726 | Benzodiazepine analogs Benzodiazepine analogs of the formula: ##STR1## wherein: R3 is ##STR2## --NH(CH2)2 --3 NHCOR7, ##STR3## or --X11 NR18 SO2 (CH2)q... | 06/28/1994 |
| 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 |
| 4997771 | Method for measuring the BZ-1 receptor binding activity in a test sample or test compound The invention describes a method for determining the BZ-1 receptor activity of a test sample or a potential anxiolytic drug.... | 03/05/1991 |
| 4820834 | Benzodiazepine analogs Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).... | 04/11/1989 |
| 4587245 | Method of treating neuropsychic disturbances by benzodiazepine derivatives and composition therefor Benzodiazepines of formula ##STR1## wherein R3 is methyl or ethyl and R4 is chlorine or fluorine are useful therapeutic agents for the treatment of neuropsychic disturbances.... | 05/06/1986 |
| 4406835 | Tranquillo-sedative benzodiazepine derivatives A tranquillo-sedative substituted 1,3,4,5-tetrahydro-2H-1,4-benzodiazepine-2-one of the formula (I), ##STR1## wherein R1 is halogen or nitro, R2 is hydrogen or methyl, R3 is --CONH2 or --CONHCH3, and ... | 09/27/1983 |
| 4342755 | Tranquillo-sedative benzodiazepine derivatives A tranquillo-sedative substituted 1,3,4,5-tetrahydro-2H-1,4-benzodiazepine-2-one of the formula (I), ##STR1## wherein R1 is halogen or nitro, R2 is hydrogen or C1 to C6 alkyl, R3 is --CONH2... | 08/03/1982 |
| 4329341 | 5-Phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-ones, and pharmaceutical compositions containing them The invention relates to new optically active or racemic 5-phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-one derivatives of the general formula (I) ##STR1## wherein R1 stands for hydrogen, halogen, trifluoromethyl or a nitro group;... | 05/11/1982 |
| 4327026 | Benzodiazepine derivatives There is presented benzodiazepine derivatives of the formula ##STR1## wherein A is the group ##STR2## R1 is lower alkyl, R2 and R3 each are hydrogen or lower alkyl, R4 is the group ##STR3## R... | 04/27/1982 |
| 4246270 | 3-Fluorobenzodiazepines and compositions and uses thereof 3-Fluorobenzodiazepines, such as 3-fluoro-1,3-dihydro-1-methyl-7-chloro-5-phenyl-2H-1,4-benzodiazepin-2-one , useful as tranquilizers, muscle relaxants, and sedatives.... | 01/20/1981 |
| 4235897 | Benzodiazepine derivatives and pharmaceutical compositions thereof The invention relates to benzodiazepine compounds of the formula: ##STR1## wherein R5 is C1 -C4 alkyl, R3 is C1 -C4 alkyl, and R4 is selected from Cl and F, and medicaments conta... | 11/25/1980 |
| 4232016 | 3-Fluorobenzodiazepines 3-Fluoro-2,3-dihydro-1H-1,4-benzodiazepin-2-ones of the formula ##STR1## wherein R1 is H, alkyl or fluorinated alkyl of 1-4 carbon atoms and up to 9 fluorine atoms or cycloalkylalkyl of 4-8 carbon atoms; R2 is phenyl; monohaloph... | 11/04/1980 |
| 4051127 | Preparation of benzodiazepine derivatives A process for the manufacture of benzodiazepine derivatives which comprises reacting 2-amino-5-chloro-benzophenone with a primary amine H2 N--R1 to give an imine which is reacted with an amino-ester ##STR1## to give a ketimine s... | 09/27/1977 |
| 4045433 | 1,3,4,5-Tetrahydro-2H-1,4-benzodiazepin-2-ones An N-substituted carbonyl tetrahydrobenzodiazepines having ethoxycarbonyl, formyl, carbamoyl or methyl carbamoyl as the N4 substituent.... | 08/30/1977 |
| 3966793 | Intermediates for preparing 1,4-benzodiazepine-2-ones having a carboxylic acid ester or amide group in the 3-position Intermediates for preparing novel benzodiazepines having the formula ##SPC1## In which R1 is a hydrogen or halogen atom or a trifluoromethyl, loweralkyl, loweralkoxy, nitro or amino group; R2 is a furyl, a thienyl, cyclohexyl, a lowe... | 06/29/1976 |