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WO/2001/055121A1 |
Azepine derivatives of the general formula (I) or salts thereof, and drugs containing the derivatives or the salts as the active ingredient. In said Formula, R?1¿ is hydrogen, alkyl, aryl, or the like; R?2¿ is hydrogen or a carboxyl-pr...
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WO/2001/055111A1 |
The invention relates to biaryl compounds, their preparation and their use in the treatment of bacterial and viral infection.
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WO/2001/053258A1 |
Novel compounds exhibiting excellent calcium antagonism, particularly neuroselective calcium antagonism, namely, compounds of the general formula (I), salts of the same, or hydrates of both wherein Ar is a group derived from an optionall...
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WO/2001/053255A1 |
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 diastereoisomers of known protease i...
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WO/2001/049681A1 |
A method for the preparation of selectively substituted benzene derivatives by application of solid phase synthesis is disclosed. In particular, the invention provides a novel method for the preparation of substituted benzene derivatives...
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WO/2001/047899A1 |
The invention relates to substituted piperazine derivatives of general formula (I), wherein R¿a? to R¿c?, Y¿a?, Y¿b?, X and n have the meanings given in claim no.1, and isomers and salts thereof, especially physiologically suitable s...
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WO/2001/047510A2 |
The present invention provides a method of treating a subject with arthritis or an arthritic disease or preventing arthritis or arthritic disease in a subject, comprising administering to the subject a therapeutically effective amount of...
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WO/2001/044190A1 |
Use of compound of Formula (I): at least one of R?1¿, R?2¿, R?5¿ and R?6¿ is a group -AB and the others are independently selected from hydrogen, hydroxy, alkoxy or acyloxy, a group -AB a group -amino-(R?7¿)¿n?X-Y wherein R?7¿ is ...
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WO/2001/042243A2 |
Disclosed are compounds which inhibit or modulate the activity of protein kinases and pharmaceutical compositions containing such compounds. The disclosed compound contain two or more ligand moieties covalently linked together by one or ...
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WO/2001/040197A1 |
Calcium salts of 1,5-benzodiazepine derivatives as represented by the general formula (I); a process for producing the salts; and drugs containing the same as the active ingredient: (wherein R?1¿ is lower alkyl; R?2¿ is phenyl or cyclo...
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WO/2001/030769A2 |
The subject invention involves processes for selective monoalkylation or dialkylation of benzodiazepin-2,5-dione compounds which are unsubstituted in the 1- and 4-positions, and monoalkylation of such compounds already substituted in the...
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WO/2001/029005A1 |
Compounds according to general formula (1), and pharmaceutically acceptable salts thereof, wherein V is a covalent bond or NH, X is selected from CH¿2?, O and N-alkyl, Z is either S or -CH=CH-, R?1¿ and R?2¿ are independently selected...
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WO/2001/029011A2 |
The present invention relates to compounds of general formula (I) wherein X is a single bond or an ethynediyl group, wherein, in case X is a single bond, R?1¿ is halogen or phenyl which is optionally substituted with halogen, lower alky...
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WO/2001/029012A2 |
The present invention relates to compounds of general formula (I) wherein R?3¿ is phenyl; pyridine; thiophenyl or thiazolyl, which are optionally substituted. The compounds according to the present invention can be used for treating or ...
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WO/2001/027102A1 |
The invention provides novel diazepanes having interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1, -ICAM-2 or -ICAM-3 interactions.
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WO/2001/027108A1 |
This invention relates to novel lactams having Formula (I), 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 p...
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WO/2001/027091A1 |
This invention relates to novel lactams having Formula (I) 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 pr...
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WO/2001/019797A2 |
This invention relates to novel lactams having formula (I) 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 pr...
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WO/2001/016110A1 |
Formulation components such as bleach boosting compounds selected from the group consisting of bleach boosters comprising quaternary imine cations, zwitterions, polyions having a net charge of from about +3 to about -3 and mixtures there...
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WO2000071516B1 |
Compounds, e.g. described in claim 5, formula (I) and formula (II), where A-B is (1), their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo fo...
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WO/2001/010847A2 |
The invention relates to novel compounds of formula (I) which bind to integrin receptors, wherein G and L have the following meaning: L is a structural element of formula I¿L?, wherein T represents a COOH group or a radical that can be ...
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WO/2001/010216A1 |
1H-Benzo[e][1,4]diazepin-2-one compounds of Formula (I) which are selective I¿Ks? antagonists useful for the treatment and prevention of cardiac arrhythmias are disclosed. Also claimed herein is the method of treatment or prevention of ...
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WO/2001/010797A1 |
Oxidation of organic compounds is catalyzed by addition of a catalytic amount of a metalloporphyrin in a non-reactive aprotic solvent.
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WO/2001/010799A1 |
A method for preparing an 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.
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WO/2001/010846A2 |
The present invention relates to therapeutically active novel 1,4-benzodiazepine compounds and derivatives thereof, of formula (I), wherein R31 or/and R32 contain at least a carboxy, or an amino group or both. Also provided is a method o...
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WO/2001/004103A1 |
Compounds of formula (I), as well as pharmaceutically usable salts and esters thereof, wherein R?1¿, R?2¿, X, Y, Z and p have the significance given in claim 1, inhibit the binding of adhesive proteins to the surface of different types...
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WO/2001/004122A2 |
The invention relates to new 2,3-benzodiazepine derivatives of general Formula (I), (wherein R?1¿ stands for methyl, formyl, carboxy, cyano, -CH=NOH, -CH=NNHCONH¿2? or -NR?5¿R?6¿, wherein R?5¿ and R?6¿ independently from each other...
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WO/2001/002381A1 |
The invention provides compounds of general formula (I), wherein R?1¿, R?2¿, R?3¿, R?4¿, R?5¿, X, Y, Z, m and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and th...
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WO/2001/002373A1 |
The invention concerns a benzodiazepin derivative of formula (I) and their use for treating dyslipidemia, atherosclerosis, diabetes and its complications.
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WO/2001/002358A2 |
The present invention relates to cyclized amide derivatives of formula (I) for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present...
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WO/2001/002403A1 |
The invention concerns a method for preparing enantiopure diazepino-indolone of formula (I) which consists in the intramolecular cyclisation of a product of formula (II) wherein A, B, X?1¿, X?2¿, Z, Z?1¿, Z?2¿ and R are as defined in...
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WO/2001/002372A1 |
The present invention relates to cyclized amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention...
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WO/2001/000625A1 |
The present invention relates to a process for the synthesis of a compound having formula (I), from a compound of formula (II), which allows the synthesis to be carried out in a single reaction vessel and without column chromatography pu...
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WO/2000/078725A1 |
The present invention provides a process for preparing amidines starting from carboxylic acid derivatives, in which the carboxylic acid containing moiety is attached to a sp?3¿-, or sp?2¿- or sp?1¿-hybridized carbon atom. The sp?2¿-h...
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WO/2000/078744A1 |
Methods for the use of compounds of formula (I) for treatment of neurological disorders, wherein n, r and s are as defined in the specification and R?1¿, R?2¿, R?3¿, R?4¿ and R?5¿ are various substituents, also as defined in the spe...
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WO/2000/078736A1 |
Methods for the use of compounds of formula (I) for treatment of neurological disorders, wherein p and q are as defined in the specification and R?1¿, R?2¿ and R?3¿ are various substituents, also as defined in the specification, such ...
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WO/2000/073284A2 |
The present invention relates to 1,4-benzodiazepin-2-ones of Formula (I) or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, an...
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WO/2000/071515A2 |
Compounds, e.g. described in Table (1), 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.
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WO/2000/071518A2 |
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate rece...
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WO/2000/069830A1 |
The synthesis of individual di- and tri-substituted-1,4-diazacyclic compounds having 6- to 8-atoms in the cyclic ring, their corresponding 1,6-diketo-2,5-diazacyclic compounds and similar 1,4-diazacyclic ring compounds having one ring ca...
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WO/2000/069835A2 |
The present invention relates to a process for manufacturing diazepine derivatives of general formula (I) wherein R?1¿ is lower alkyl and R?2¿ is hydrogen, or R?1¿ and R?2¿ are together -(CH¿2?)¿n?- and n is 2 or 3; R?3¿ is haloge...
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WO/2000/069836A1 |
It has now been found that compounds of the present invention as described in Benzodiazepine derivatives of Formula (I) containing a carboxylic ester moiety and thereby capable of being inactivated by nonspecific tissue esterases in an o...
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WO/2000/068209A2 |
An enantiomerically enriched compound of Formula (I) is disclosed, processes for its preparation, pharmaceutical compositions containing it and the use therefore, for the treatment of CCK-A mediated diseases or conditions, such as obesity.
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WO/2000/064900A1 |
Novel pyrazolobenzodiazepines having formula (I) and the pharmaceutically acceptable salts thereof, wherein R?1¿, R?2¿, R?3¿ and R?4¿ are as defined herein inhibit cyclin-dependent kinases (CDKs), in particular CDK2, are anti-prolife...
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WO/2000/063195A1 |
The current invention discloses novel heterocyclic amino carbonyl derivatives useful as nitric oxide synthase inhibitors
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WO/2000/063186A1 |
A new process and intermediates for preparing 1,4-benzodiazepines of formula (I) is disclosed: wherein, R?1¿ is H, OH, Br, I, NR?5¿R?6¿, CO¿2?R?7¿, CF¿3?SO¿3?, C¿1-4?alkoxy, or (4,4'-bipiperidinyl) carbonyl; R?2¿ is alkyl, optio...
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WO/2000/061587A1 |
The invention relates to novel pyrido-thieno-diazepines of general formula (I), wherein R¿1?, R¿2?, X, R¿3a?, R¿3b?, R¿4? represent various radicals, and to a method for the production thereof and to pharmaceutical compositions cont...
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WO/2000/061569A1 |
The invention provides compounds of general formula (I) in which m, A, R?1¿ and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the...
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WO/2000/059880A1 |
The present invention relates to cinnamide compounds of formula (I), in which at least one of R¿1? to R¿5? is a '$i(cis)-cinnamide' (a) or a '$i(trans)-cinnamide' (b) and the other variables are as defined in the claims, that are usefu...
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WO/2000/058294A1 |
Compounds of formula (I) are antibacterial agents wherein: R¿3? and R¿4?, taken together with the carbon atoms to which they are respectively attached, form an optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 1...
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