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Class 540/507 - The additional chalcogen is bonded directly at the 3-position of the bicyclo ring system


Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the additional chalcogen is bonded directly
No. of patents: 27
Last issue date: 06/24/2008


NumberTitleIssue Date
7390801Cycloalkyl, 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
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;  (I) where G is a lipophilic drug; L is a linker which is an alkyl group or heter...
04/18/2006
6686350Cell 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
6492553Methods for preparing N-[(aliphatic or aromatic)carbonyl)]-2-aminoaetamide compounds and for cyclizing such compounds
A method for preparing a N-[(aliphatic or aromatic)carbonyl)]-2-aminoacetamide compound, and for preparing a cyclized compound therefrom, as well as novel resin bound intermediate compounds that are useful for preparing such compounds....
12/10/2002
64620371,4-benzodiazepin-2-ones useful as HIV reverse transcriptase inhibitors
The present invention relates to 1,4-benzodiazepin-2-ones of Formula (I): ##STR1## or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pha...
10/08/2002
6350870Process for preparing pure crystalline lorazepam
The present invention provides a process for preparing crystalline lorazepam substantially free of bound solvent from a lorazepam alcohol solvate or hydrate by suspending the lorazepam solvate in an organic medium selected from ethyl acetate, cyclohexane,...
02/26/2002
6255479Process for the preparation of ଱-oxolactams
A method for preparing an ଱-oxolactam comprising, reacting a corresponding ଱-diazolactam with an oxygen donor, in the presence of a transition metal catalyst, to yield the corresponding ଱-oxolactam....
07/03/2001
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
5662911Benzodiazepine protein conjugates
Benzodiazepine protein conjugates of the formula I ##STR1## wherein R1 is hydrogen, a methyl group or R, R2 is hydrogen, a hydroxyl or an OR group, with R1 or R2 containing an R group, R3 is a halogen, NO2 or NH2, X is hydrogen or a halogen, wherein R is ...
09/02/1997
5597922Glycine receptor antagonist pharmacophore
Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and D...
01/28/1997
5302715Benzodiazepine derivatives
The present invention is directed to novel benzodiazepine derivatives which are synthesized for the covalent attachment to antigens (proteins or polypeptides) for the preparation of antibodies or receptors to the benzodiazepine metabolites. The resulting ...
04/12/1994
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
4820834Benzodiazepine analogs
Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK)....
04/11/1989
4808605Tetrahydronaphthalene derivatives as calcium antagonists
Compounds of the formula ##STR1## wherein R is lower-alkyl, R1 is halogen, R2 is C1 -C12 -alkyl, R3 is hydroxy, lower-alkoxy, lower-alkyl-carbonyloxy, lower-alkoxy-lower-alkylcarbonoyloxy, lower-...
02/28/1989
4777169Benzodiazepine derivatives
Benzodiazepine derivatives useful in immunoassays for benzodiazepines....
10/11/1988
45606841,4-Benzodiazepine derivatives
1,4-Benzodiazepine derivatives of the formula: ##STR1## (in which R1 is pyrrolidinyl or piperidinyl each optionally substituted by C1-3 alkyl, phenyl-C1-3 alkyl, C1-5 alkanoyl, or C2-5 alkoxycarb...
12/24/1985
4412952Process for 3-hydroxy benzodiazepinones
Conversion of 3-acyloxy-benzodiazepin-2-ones into corresponding 3-hydroxy benzodiazepin-2-ones is carried out efficiently with potassium hydroxide or potassium alkoxide as catalyst in lower alkanol solvent at a pH of 11-11.5. The final products, which inc...
11/01/1983
4388313Novel 3-hydroxy-1,4-benzodiazepine-2-ones and process for the preparation thereof
The disclosure is directed to new 3-hydroxy-1,4-benzodiazepine-2-ones and to the process for the preparation thereof. The compounds of the invention have the structural formula ##STR1## in which R is methoxy or nitrile, R1 is hydrogen, hal...
06/14/1983
43139437-Chloro-2,3-dihydro-5-phenyl-1-propargyl-1H-1,4-benzodiazepine-2-one, and a pharmaceutical composition thereof
The invention relates to 1-propargyl-5-(halo) phenyl-1,4-benzodiazepines, and particularly to 7-chloro-2,3-dihydro-5-phenyl-1-propargyl-1H-1,4-benzodiazepine-2-one endowed with psycho-sedative, low myorelaxant, high anxiolytic, anticonvulsant and hyp...
02/02/1982
42619873-Di-n-propyl-acetoxy-benzodiazepine-2-ones and pharmaceutical compositions thereof
Novel 3-Di-n-Propyl-Acetoxy-Benzodiazepine-2-Ones and use thereof as anti-convulsant compounds....
04/14/1981
41338094H-S-Triazolo[4,3-2][1,5]benzodiazepin-5-ones
Compounds of the following formula ##STR1## are useful as central nervous system depressants, tranquilizers, sedatives, growth promotors, anti-convulsants and muscle relaxants in mammalian species....
01/09/1979
4083948Benzodiazepine radioimmunoassay using I125-label
An improved radioimmunoassay for benzodiazepines such as diazepam, chlordiazepoxide, oxazepam, demoxepam and metabolites thereof is disclosed. Such immunoassay employs novel 125 I-labelled 4'-hydroxy derivatives of these compounds as tracer....
04/11/1978
4043989Oxazepam derivatives for immunoassay reagents
Compounds are provided for use in the preparation of reagents which can be used in immunoassays for benzdiazepines, particularly as their urinary metabolites. The compounds are non-oxo-carbonyl derivatives conjugated to the 3-position of the benzdiazepine...
08/23/1977
4021469Process for preparing N-phenylcarbamates
Alkyl or Aralkyl N-[2-aroyl]phenylcarbamates are prepared by reacting a 3-aryl-2-indolinone with oxygen in the presence of an alkali metal alkoxide or aralkoxide....
05/03/1977
 
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