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Class 540/509 - Acyclic nitrogen bonded directly to the hetero ring


Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which acyclic nitrogen is bonded directly to
No. of patents: 101
Last issue date: 03/24/2009


1      
NumberTitleIssue Date
7507815Succinoylamino lactams as inhibitors of a-β protein production
This invention relates to novel lactams having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-pe...
03/24/2009
7456278Lactams substituted by cyclic succinates as inhibitors of Aβ protein production
This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifica...
11/25/2008
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
7375101Benzodiazepine derivatives, preparation thereof and use thereof
Compounds of Formula (I) wherein R1, R3, R4, R5 and X are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in ther...
05/20/2008
7365196Sulphonamido-substituted bridged bicycloalkyl derivatives
A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease. ...
04/29/2008
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
7304055Succinoylamino lactams as inhibitors of Aβ protein production
This invention relates to novel lactams having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-pe...
12/04/2007
7276496Cyclic malonamides as inhibitors of Aβ protein protection
This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor prote...
10/02/2007
7276348Compositions and methods relating to F1F0-ATPase inhibitors and targets thereof
The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat...
10/02/2007
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
7226991Phenylalanine derivatives
Disclosed herein are phenylalanine derivative compounds of the following formula W—Y—(AA)n—Z wherein Y is a phenylalanyl radical, AA is an amino acid, n is an integer of 1 to 15, and substituent variables W and Z are as described...
06/05/2007
7205293Benodiazepine spirohydantoin CGRP receptor antagonists
The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pha...
04/17/2007
7196079Benzodiazepine CGRP receptor antagonists
The present invention is directed to compounds of Formula I: (where variables R1, R2, R3, R6, R7, G, J, W, X and Y are as defined herein) useful as antagonis...
03/27/2007
7186712Compositions and methods relating to novel compounds and targets thereof
The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat...
03/06/2007
7160880Short-acting benzodiazepines
The present invention provides a compound of formula (I): wherein all variables are as defined herein, pharmaceutical formulations containing the same, processes for preparing the same and their use therapy. ...
01/09/2007
7144880Compositions relating to novel compounds and targets thereof
The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat...
12/05/2006
7115598Substituted 1,4-diazepines and uses thereof
The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharm...
10/03/2006
7105509Benzodiazepine derivatives as APP modulators
A novel class of 1,4- and 1,5-benzodiazepines of formula (I) is disclosed. The compounds modulate the processing of amyloid precursor protein by γ-secretase, and hence find use in the treatment or prevention of conditions associated with the deposition of β-amyloi...
09/12/2006
7053084Succinoylamino benzodiazepines as inhibitors of Aβ protein production
This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, mor...
05/30/2006
6995155Benzodiazepine derivatives as inhibitors of gamma secretase
Compounds of formula (I) are disclosed. The compounds inhibit the action of gamma secretase, and hence find use in the treatment and prevention of Alzheimer's disease. ...
02/07/2006
6960576Hydroxyalkanoylaminolactams and related structures as inhibitors of Aβ protein production
This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more spec...
11/01/2005
6900222Pyrrolidinyl, piperdinyl 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 thereon wherein —Z1—Z2
05/31/2005
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
6759404Cyclic malonamides as inhibitors of aβ protein production
Novel cyclic malonamides having the formula (I): and their pharmaceutical compositions. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-pept...
07/06/2004
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
6713476Substituted cycloalkyls as inhibitors of a beta protein production
This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specif...
03/30/2004
6632812Substituted lactams as inhibitors of Aଲ protein production
This invention relates to novel lactams of Formula (I): ##STR1## having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifical...
10/14/2003
6569851Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ଲ-amyloid peptide release and/or its synthesis by use of such compounds
Disclosed are compounds which inhibit ଲ-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits ଲ-amylo...
05/27/2003
6552041Cyclized amide derivatives
The present invention relates to cyclized amide derivatives of formula (I) ##STR1## These cyclized amide derivatives are useful for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comp...
04/22/2003
6509333Lactams substituted by cyclic succinates as inhibitors of Aଲ protein production
This invention relates to novel lactams having the Formula (I): ##STR1## to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the produc...
01/21/2003
6503901Amino lactam sulfonamides as inhibitors of Aଲ protein production
This invention relates to novel lactams having the Formula (I): ##STR1## to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the produc...
01/07/2003
6503902Hydroxyalkanoylaminolactams and related structures as inhibitors of a ଲ protein production
This invention relates to novel lactams having the formula (I): ##STR1## to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the produc...
01/07/2003
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
6333321Selective factor Xa inhibitors
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders....
12/25/2001
6329365Inhibitors of interleukin-1ଲ converting enzyme
The present invention relates to novel classes of compounds which are inhibitors of interleukin-1ଲ converting enzyme ("ICE"). This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical com...
12/11/2001
62914521,4-benzodiazepinones and their uses as CCK antagonists
Benzodiazepine derivatives of the formula: ##STR1## wherein R2 is alkyl or cycloalkyl-alkyl when R4 is hydrogen, or R2 is a variety of specified groups when R4 is alkyl, halogen or dialkylamino, are useful as ch...
09/18/2001
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
6214823Benzodiazepine derivatives as antiarrhythmic agents
This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia....
04/10/2001
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
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