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Class 540/514 - Nitrogen in the 1-position substituent of the bicyclo ring system


Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the 1-position substituent of the bicyclo
No. of patents: 22
Last issue date: 04/15/2008


NumberTitleIssue Date
7358239Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is...
04/15/2008
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
6916805Quinoxalinones as serine protease inhibitors
This invention discloses quinoxalinones which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically acceptable salts and prodrugs of the compounds, pharmaceutically acceptable co...
07/12/2005
6458784Vitronectin receptor antagonists
Pharmaceutically active benzodiazapine compounds of formula (I) are disclosed. These compounds inhibit the vitronectin receptor and are useful for treatment of osteoporosis. ##STR1##...
10/01/2002
6403578Bicyclic fibrinogen antagonists
This invention relates to compounds of the formulae: ##STR1## wherein A1 is O, S, N--R1 or CHR1 ; A4 is N--R4 or CHR4 ; R2 is a sidechain containing an acid or ester group; R1, ...
06/11/2002
6117866Bicyclic fibrinogen antagonists
Certain compounds within formula (I) are inhibitors of platelet aggregation: ##STR1## wherein A1 is NH or CH2 ; R is H, C1-6 alkyl, benzyl or a carboxy protecting group; R3 is C1-6 alkyl, Ar-C0-6...
09/12/2000
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
5843941Ras farnesyl transferase inhibitors
Benzodiazepine derivatives represented by the structure below are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases foe which in...
12/01/1998
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
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
5013836Process for methylating a hindered nitrogen atom in a polysubstituted diazacycloalkan-2-one
The difficulty of methylating a hindered piperidinyl, piperazinyl, or diazepinyl group with an Eschweiler-Clarke ("E-C") procedure without using a large molar excess (more than double) of formaldehyde is surprisingly found to be non-existent in the case o...
05/07/1991
4820834Benzodiazepine analogs
Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK)....
04/11/1989
4656026Magnetic resonance (MR) image enhancement compounds for specific areas of the brain
An improved imaging technique involving nuclear magnetic resonance. Known drug or neurotransmitter receptor ligands are covalently bound to magnetic resonance image enhancing spin label compounds, such as sterically hindered free radical nitroxide compoun...
04/07/1987
4579685Process for preparing 1-substituted-1,4-benzodiazepine derivatives
Improvement in the production of psychotropic 1-substituted-1,3-dihydro-1,4-benzodiazepin-2-ones starting from 2-(1-substituted)amino-benzophenonimines through novel intermediates of the formula: ##STR1## (wherein R is hydrogen, methyl or benzyl...
04/01/1986
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
42922402-Keto-1,4-diazacycloalkanes
Novel polysubstituted 2-keto-1,4-diazacycloalkanes are powerful stabilizers for materials subject to ultraviolet (UV) light degradation, particularly for polyolefins. The cyclic 2-keto compounds of this invention have (a) a fixed two-carbon bridge between...
09/29/1981
4160099Labile, non-heterocyclic quaternary ammonium salt/esters as transient derivatives
Labile quaternary ammonium salts of the following formula (I) and (II) are provided: ##STR1## wherein ##STR2## represents a tertiary aliphatic amine; wherein ##STR3## represents an unsaturated amine; wherein R represents a member selec...
07/03/1979
41512851,5-Disubstituted-1,2-dihydro-2H-1,4-benzodiazepin-2-ones
1,5-Disubstituted-1,2-dihydro-2H-1,4-benzodiazepin-2-ones of the formula ##STR1## wherein R is hydrogen or fluoro, R1 is hydrogen, fluoro chloro, bromo or trifluoromethyl, and n is 2 to 4, having anticonvulsant activity and useful as anti-...
04/24/1979
3991048Process for the preparation of 1,4-benzodiazepine derivatives
A 1,4-benzodiazepine derivative, or a pharmaceutically acceptable acid salt thereof, of the formula, ##SPC1## Wherein R1 is hydrogen, halogen, nitro or trifluoromethyl; R2 and R3 are independently hydrogen, halogen, lower ...
11/09/1976
39896817-Azoxy substituted-1,4-benzodiazepin-2-ones
Novel 1,4-benzodiazepin-2-ones of the formula ##SPC1## Wherein R1 is selected from the group consisting of hydrogen, lower alkyl, cycloalkyl-lower alkyl, hydroxylower alkyl, lower alkoxy-lower alkyl and di-lower alkylamino-lower alkyl; R2
11/02/1976
39706451,4-Benzodiazepine derivative
The invention relates to new 1,4-benzodiazepine derivatives of the formula ##SPC1## Wherein R1 is hydrogen, halogen, or the trifluoromethyl group, R2 and R3 are alkyl groups, and n is an integer from 1 to 4, and acid addit...
07/20/1976
 
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