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Class 540/510 - Having -C(=X)-, wherein X is chalcogen, bonded directly to the hetero ring


Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which- C - wherein X is chalcogen (i.e., oxygen,
No. of patents: 31
Last issue date: 07/31/2007


NumberTitleIssue Date
7250410Cyclic 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
7029918Water-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)n—Y;ā€ƒā€ƒ(I) where G is a lipophilic drug; L is a linker which is an alkyl group or heter...
04/18/2006
6825191Benzodiazepine 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
6765005Fab 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
6756511Gamma-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
6503903Fab 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
6232308Bezazepine 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
61212581,5-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
6100254Inhibitors 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
6015791Serine 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
6011029Inhibitors of farnesyl protein transferase
The present invention comprises benzodiazepine compounds having farnesyl transferase inhibitory activity....
01/04/2000
6008214Bicyclic 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
5985869Benzoheterocyclic 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
5891852Serine 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
5580979Phosphotyrosine 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
5416083Benzodiazepinyl-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
5324726Benzodiazepine 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
51751593-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
4997771Method 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
4820834Benzodiazepine analogs
Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK)....
04/11/1989
4587245Method 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
4406835Tranquillo-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
4342755Tranquillo-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
43293415-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
4327026Benzodiazepine 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
42462703-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
4235897Benzodiazepine 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
42320163-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
4051127Preparation 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
40454331,3,4,5-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
3966793Intermediates 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
 
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