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| Number | Title | Issue Date |
| 8039616 | Benzodiazepine derivatives for treating hepatitis C infection Use of a benzodiazepine of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing a hepatitis C infection, wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R | 10/18/2011 |
| 7994313 | Unsolvated benzodiazepine compositions and methods The present invention relates to systems and methods for generating new forms of benzodiazepine and benzodiazepine related compounds as well as new compounds and formulations generated by such methods. In particular, the present invention provides high throughput sy... | 08/09/2011 |
| 7528249 | Cyclic malonamides as inhibitors of aβ protein production 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 protein and, mor... | 05/05/2009 |
| 7410963 | Benzo-1,4-diazepin-2-one derivatives as phosphodiesterase PDE2 inhibitors, preparation and therapeutic use thereof The invention relates to compounds having PDE2 inhibitory activities, as well as therapeutic methods by administering said compounds, in particular for treating various diseases of the central or peripheral nervous system. It further deals with pharmaceutical compos... | 08/12/2008 |
| 7390801 | 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/... | 06/24/2008 |
| 7378411 | Substituted thienopyrimidinones as a mitotic kinesin inhibitor The present invention relates to thienopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which ... | 05/27/2008 |
| 7358239 | Pyrrolidinyl, 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 |
| 7262187 | Substituted oxazolo- and thizaolopyrimidinones as a mitotic kinesin inhibitor The present invention relates to azolopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which c... | 08/28/2007 |
| 7262186 | Substituted pyrazolo[3,4-d] pyrimidinones as a mitotic kinesin inhibitor The present invention relates to azolopyriniidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which ... | 08/28/2007 |
| 7250410 | Cyclic 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 |
| 7244723 | Substituted furopyrimidinones as a mitotic kinesin inhibitors The present invention relates to furanopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which ... | 07/17/2007 |
| 7238685 | Benzo-fused heterocycles as endothelin antagonists The invention relates to novel benzo-fused heterocycles and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compos... | 07/03/2007 |
| 7192949 | Substituted bicyclic pyrimidinones as a mitotic kinesin KSP inhibitors The present invention relates to cycloalkylpyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions wh... | 03/20/2007 |
| 7074921 | Process for the preparation of 3,7-disubstituted-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine compounds Methods for the synthesis of benzodiazepine compounds having farnesyl protein transferase inhibitory activity. ... | 07/11/2006 |
| 7067512 | Substituted 1,4-benzodiazepines and uses thereof The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or ... | 06/27/2006 |
| 7053084 | Succinoylamino 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 |
| 6916805 | Quinoxalinones 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 |
| 6838455 | Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-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/... | 01/04/2005 |
| 6825191 | Benzodiazepine 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 |
| 6815543 | Process for catalyzing the oxidation of organic compounds Oxidation of organic compounds is catalyzed by addition of a catalytic amount of a metalloporphyrin in a non-reactive aprotic solvent. ... | 11/09/2004 |
| 6774125 | Deoxyamino acid 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/... | 08/10/2004 |
| 6696438 | 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... | 02/24/2004 |
| 6686350 | Cell 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 |
| 6683075 | Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ଲ-amyloid peptide release and/or its synthesis by use 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... | 01/27/2004 |
| 6653303 | 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... | 11/25/2003 |
| 6558649 | Vitronectin receptor antagonist pharmaceuticals The present invention describes novel compounds of the formula: (Q)d --Ln --Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present ... | 05/06/2003 |
| 6495545 | 1,4-benzodiazepinone derivatives and their use as integrin antagonists The present invention relates to compounds of general formula (I) and their preparation and use for the production of pharmaceuticals, and pharmaceuticals comprising these compounds.... | 12/17/2002 |
| 6492553 | Methods 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 |
| 6462037 | 1,4-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 |
| 6458784 | Vitronectin 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 |
| 6403578 | Bicyclic 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 |
| 6369221 | Thiazolobenzoheterocycles, preparation and medicines containing same Disclosed are thiazolobenzoheterocycles of the general formula ##STR1## Including their isomers, racemates, enantioners and salts thereof, as well as processes for preparing these compounds and medicaments containing them. Also disclosed are novel interme... | 04/09/2002 |
| 6339083 | Multiheterocyclic pharmAceuticals The present invention relates to compounds of the general formula (I): ##STR1## and their preparation and use for the production of pharmaceuticals, and pharmaceuticals comprising these compounds.... | 01/15/2002 |
| 6252067 | Method of preparing oxoquazepam A method of preparing oxoquazepam which comprises reacting 2,2,2-trifluoroethyl trifluoromethanesulfonate with 7-chloro-1,3-dihydro-5-(2-fluorophenyl)-2H-1,4-benzodiazepin-2-one in tetrahydrofuran or ethyl acetate in the presence of potassium carbonate ... | 06/26/2001 |
| 6232308 | Bezazepine 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 |
| 6225465 | Process for the aminocarbonylation of benzazepines and benzodiazepines A new process for preparing substituted 7-aminocarbonyl-3-oxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepines is disclosed.... | 05/01/2001 |
| 6222032 | Use of ylides of phosphorus as slightly nuceophilic strong bases In a process for C-alkylation or N-alkylation, the improvement comprising conducting the C-alkylation or N-alkylation reaction in the presence of a slightly nucleophilic strong base of the following formula ##STR1## wherein R'1, R'2 ... | 04/24/2001 |
| 6171578 | Benzodiazepine derivatives for imaging thrombi The invention provides compounds comprising glycoprotein IIb/IIIa receptor-binding benzodiazepine derivatives covalently linked to metal ion chelators. The compounds of the invention may be labeled with a radionuclide such as 99m Tc and used to... | 01/09/2001 |
| 6121258 | 1,5-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 |
| 6117866 | Bicyclic 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 |
