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| Number | Title | Issue Date |
| 7544679 | 6-oxo-6,7-dihydro-5h-dibenzo[b,d]azepin-7-yl derivatives The invention relates to 6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl derivatives of formula I wherein R1, R2 and R3 are as defined herein. The compounds are γ-secretase inhibitors useful i... | 06/09/2009 |
| 7429578 | Tricyclic inhibitors of poly(ADP-ribose) polymerases Compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. ... | 09/30/2008 |
| 7425551 | Malonamide derivatives The invention relates to malonamide derivatives of formula wherein A1, A2, R1, R2, R3, and R4 are as defined herein and to pharmaceutically acce... | 09/16/2008 |
| 7375099 | Malonamide derivatives The invention relates to malonamide derivatives of formula wherein each of the variables are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds are γ-secretase inh... | 05/20/2008 |
| 7351701 | Therapeutic compounds The invention relates to trycyclic lactam indole derivatives and triacyclic lactam benzimodole derivatives and their use in inhibiting the activity of PARP enzyme. The invention also relates to the use of these compounds in the preparation of medicaments. ... | 04/01/2008 |
| 7304049 | Succinoylaminobenzodiazepines 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... | 12/04/2007 |
| 7268126 | Polymorphic and amorphous forms of the phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-ce]indol-6-one The present invention relates to novel polymorphic and amorphous forms of a phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a compo... | 09/11/2007 |
| 7166587 | Carbamic acid alkyl ester derivatives The present invention provides compounds of the general formula wherein R4 is one of the following groups | 01/23/2007 |
| 7160875 | Malonamide derivatives The invention relates to malonamide derivatives of formula wherein each of the variables are as defined herein and to pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates and dia... | 01/09/2007 |
| 7153847 | Cycloalkyl, 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/... | 12/26/2006 |
| 7105508 | Integrin receptors antagonists The invention relates to novel compounds which bind to integrin receptors, and to the preparation thereof and the use thereof as drugs. ... | 09/12/2006 |
| 6960576 | Hydroxyalkanoylaminolactams 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 |
| 6958329 | Lactams substituted by cyclic succinates as inhibitors of A-β 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... | 10/25/2005 |
| 6958330 | Polycyclic α-amino-ε-caprolactams and related compounds Disclosed are polycyclic α-amino-ε-caprolactams and related compounds which are useful as synthetic intermediates in the preparation of inhibitors of β-amyloid peptide release and/or its synthesis. ... | 10/25/2005 |
| 6906056 | Cycloalkyl, 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 that include a compound which inhibits β-amyloid peptide release an... | 06/14/2005 |
| 6900199 | Substituted lactams as inhibitors of Aβ protein production This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor ... | 05/31/2005 |
| 6696436 | B-homoestra-1,3,5(10)-trienes as modulators of tubulin polymerization The invention provides B-ring expanded estra-1,3,5(10)-triene compounds of general formula (1) which modulate the polymerization of tubulin and/or the depolymerization of microtubules. The compounds have anti-angiogenic and anti-tumor activity. The invent... | 02/24/2004 |
| 6638925 | Benzazepine derivatives, medicaments containing the same and their use to prepare medicaments New derivatives of benzazepine, particularly of benzofuro[3a,3,2,ef][2]benzazepin of the general formula (I) ##STR1## and new compounds of the general formula (III) ##STR2## Drugs, containing compounds of formulas (I) and/or (III), which can be used ... | 10/28/2003 |
| 6635632 | Cycloalkyl, 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 comprising a compound which inhibits ଲ-amyloid... | 10/21/2003 |
| 6602866 | Mercaptoacetylamide derivatives, a process for their preparation and their use This invention discloses and claims a series of mercaptoacetylamide derivatives of formula I. Also disclosed and claimed are pharmaceutical compositions incorporating these compounds and processes for preparing said compounds. The use of said compounds fo... | 08/05/2003 |
| 6579867 | Cycloalkyl, 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 comprising a compound which inhibits ଲ-amyloid... | 06/17/2003 |
| 6559141 | Cycloalkyl, 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 comprising a compound which inhibits ଲ-amyloid... | 05/06/2003 |
| 6552013 | Deoxyamino acid 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 comprising a compound which inhibits ଲ-amyloid... | 04/22/2003 |
| 6544978 | Cycloalkyl, 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 comprising a compound which inhibits ଲ-amyloid... | 04/08/2003 |
| 6541466 | Cycloalkyl, 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 comprising a compound which inhibits ଲ-amyloid... | 04/01/2003 |
| 6528505 | Cyclic amino acid 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 comprising a compound which inhibits ଲ-amyloid... | 03/04/2003 |
| 6509331 | Deoxyamino acid 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 comprising a compound which inhibits ଲ-amyloid... | 01/21/2003 |
| 6468996 | Substituted hetero-polycyclic compounds as PPAR and PPARγ activators The present invention relates to compounds of the general formula (I) ##STR1## The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).... | 10/22/2002 |
| 6395728 | Method of treatment and pharmaceutical composition The invention relates to a method for the treatment or prevention of a condition or disease selected from the group consisting of hypertension, (acute and chronic) congestive heart failure, left ventricular dysfunction and hypertrophic cardiomyopathy, myo... | 05/28/2002 |
| 6387893 | Spirotricyclic substituted azacycloalkane derivatives and uses thereof Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, is in the treat... | 05/14/2002 |
| 6054448 | 2-amino-2-(3-substituted cyclobutyl) acetic acid derivatives Compounds of the formula ##STR1## in which R1 is Y or Y--C1-6 alkyl, where Y is carboxy, tetrazolyl, --SO2 H, --SO3 H, --OSO3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' ... | 04/25/2000 |
| 6054458 | Heterocyclic compounds The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R1, R2 and m are as defined in the detailed part of the present description, or salts thereof, to me... | 04/25/2000 |
| 6004933 | Cysteine protease inhibitors The present invention relates to cysteine protease inhibitors of the general formula (I): ##STR1## wherein Z is a cysteine protease binding moiety; X and Y are S, O or optionally substituted N; and R1 is optionally substituted alkyl or ... | 12/21/1999 |
| 5854273 | Bisimide compounds A compound of formula (I) ##STR1## in which: X and Y, which may be identical or different, represent hydrogen or halogen or alkyl, trihaloalkyl, alkoxy, hydroxyl, cyano, nitro, amino, alkylamino, or dialkylamino, Z represent a linear or branched C | 12/29/1998 |
| 5498609 | Benzoazepinyl compounds as oxytocin and vasopressin antagonists Novel benzoheterocyclic compound of the formula (1): ##STR1## and pharmaceutically acceptable salts thereof, which show excellent anti-vasopressin activity and oxytocin antagonistic activity, and are useful as a vasopressin antagonist or oxytocin ant... | 03/12/1996 |
| 5340807 | Tricyclic compounds and intermediates thereof Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R1, R2, R3 and R4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamin... | 08/23/1994 |
| 5238936 | Trisubstituted triazines The compounds are trisubstituted triazines and pyrimidines useful for the suppressing the resistance of tumour cells to anti-cancer agents and for suppressing the resistance of parasites to anti-parasitic agents. A compound disclosed is 2,4-diallylamino-6... | 08/24/1993 |
| 5134141 | Antidepressant polycyclic imides to treat depression A method for relieving depression with decahydro-3-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-1,5-methano-6,7,9-m etheno-2H-pentaleno[1,2-d]azepine-2,4(3H)-dione, or a pharmaceutically acceptable salt thereof.... | 07/28/1992 |
| 5080905 | Therapy of 10-amino-5,6-dihydro-11H-dibenzo(b,e)azepine-6,11-dione and derivatives as drugs for use in the treatment of urinary incontinence Use of a 10-amino-5,6-dihydro-11H-dibenzo(b,e)azepine-6,11-dione of formula I ##STR1## where R represents an atom of hydrogen or a lower alkyl group, especially containing from 1 to 5 carbon atoms, as well as of a therapeutically acceptable salt... | 01/14/1992 |
| 4959361 | Triazolo(4,3-A)(1,4)benzodiazepines and thieno (3,2-F)(1,2,4)triazolo(4,3-A)(1,4)diazepine compounds which have useful activity as platelet activating factor (PAF) antagonists The invention relates to compounds of the formula ##STR1## wherein X is --CH.dbd.CH-- or S; R1 is lower alkyl, lower alkoxy or trifluoromethyl; R2 is hydrogen, lower alkyl, lower alkoxy, hydroxy or alkanoyloxy; R3 and R | 09/25/1990 |
