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WO/2003/018135A1 |
This invention relates to novel 5-(arylsulfonyl)-thiazolidine-2,4-diones, and 5-(arylsulfanyl)-thiazolidine-2,4-diones of Formula (I), wherein Ar, Ar', R¿6?, m and n are as defined in the specification as inhibitors of Ras FPTase, and m...
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WO/2003/016254A1 |
Carboxylic acid derivatives represented by the following general formula (I) and nontoxic salts thereof: (I) wherein R1 represents COOH, COOR4 (wherein R4 represents alkyl, etc.), etc.&semi A represents alkylene, etc.&semi R2 represents ...
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WO/2003/015517A1 |
The present invention provides compositions and methods for controlling an helminth or arthropod pest. In a preferred embodiment of the invention provided herein, the compositions comprise compounds which alter the 5-HT¿3? receptor of t...
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WO/2003/016308A1 |
The invention relates to N-heterocyclyl substituted thienyloxy-pyrimidines of formula (I), agriculturally useful salts thereof, methods and intermediates for their production as well as the use of these compounds or agents containing the...
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WO/2003/016276A2 |
The present invention relates to a $g(b)3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type ...
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WO/2003/013518A1 |
Biaryl ketoamide derivatives (I), which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such biaryl ketoamide derivatives as well as methods of using the same in the trea...
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WO/2003/014075A2 |
This invention discloses novel gamma secretase inhibitors of the formula:(Chemical formula should be inserted here as it appears on abstract in paper form)wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 gro...
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WO/2003/014071A1 |
The invention relates to benzoylcyclohexenone derivatives of general formula (I) wherein the variables R?1¿ to R?10¿ and n have the designation cited in claim 1. The invention also relates to the salts of the same and the use of said d...
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WO/2003/011858A1 |
The invention relates to coagulation of the blood. Disclosed are novel compounds of formula (I), a method for the production and the use thereof as active medicamentous substances for the prevention and/or treatment of diseases.
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WO/2003/011872A1 |
Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and ac...
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WO/2003/010158A1 |
The invention relates to thiophene carboxamides of formula (I). wherein A, R?1¿, R?2¿, R?3¿, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing th...
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WO/2003/007958A1 |
The invention relates to novel tetrahydroquinoxalines of structure I/Ia, to a method for producing the same and to the use thereof for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of pa...
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WO/2003/007942A1 |
The invention relates to the field of blood clotting, to novel compounds of formula (I), to a method for their production and to the use of said compounds as active ingredients in medicaments for preventing and/or treating diseases. Said...
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WO/2003/007946A1 |
The invention relates to novel compounds, namely secondary thiazolylsulfonamides, according to formula (I), to method for producing them and to the use thereof as drugs, especially as antiviral drugs.
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WO/2003/008391A1 |
The present invention relates to the derivatives of specially substituted azole compounds which have improved antifungal activity as compared with presently available agents in this class and the processes for the preparation thereof. Th...
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WO/2003/008398A1 |
This invention relates aryl substituted thiazolidinones of Formula I: (I) or a pharmaceutically acceptable salt, or solvate thereof, wherein $i(n) is an integer from 1 to 2; R1 is selected from the group consisting of: (I) where Y is alk...
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WO/2003/006440A2 |
The present invention is directed to novel amide-containing compounds which have an improved solubility and a method of improving the solubility of amide-containing compounds. The amide-containing compounds include oxazolidinone compound...
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WO/2003/006436A1 |
The invention concerns novel azole or triazole derivatives of formula (Ia) or (Ib), wherein: X, Ar?1¿, Ar?2¿, Ar?3¿, A, B and R?1¿ are such as defined in the description, the method for preparing same and their use as fungicides.
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WO/2003/006456A1 |
Compound of general formula (I) in which Y is chosen from the following groups Y?1¿ to Y?3¿ (I*), the other substituents being as defined in the description, process for preparing this compound, fungicidal composition comprising this c...
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WO/2003/004493A1 |
The present invention relates to novel compounds that are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compo...
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WO/2003/004512A1 |
A process for the synthesis of oligonucleotides using phosphoramidite chemistry is provided. The process employs as activator a 1,1-dioxo-1,2-dihydro-1$g(l)?6¿-benzo[d]isothiazol-3-one, preferably in the presence of an organic base. The...
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WO/2003/004467A2 |
Aminothiazole compounds with mono-/di-substituted benzamide are represented by the Formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable prodrugs, pharmaceutically active metabolites, and pharmaceutically ...
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WO/2003/004023A1 |
The invention relates to novel benzimidazole derivatives of general formula (I), wherein the groups R?1¿, R?2¿, R?3¿, A, B and Y are defined as per the definition and the claims. The invention also relates to the use of these compound...
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WO/2003/004027A1 |
This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compou...
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WO/2003/002518A1 |
2,4-difluorobenzamide derivatives and their pharmaceutically acceptable salts, represented by following formula (1), are described in which the derivatives have excellent inhibitory effects on proliferation of hepatitis B virus (HBV) and...
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WO/2003/002542A1 |
N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I). Methods of production, pharmaceutical compositions ...
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WO2001072728B1 |
A compound of formula (I) or the pharmaceutically acceptable salt thereof; wherein a, b, c, d, e, j, R<1>, R<2>, R<3>, and R<4> ar e as defined above useful to treat inflammation and other immune disorders.
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WO/2003/002519A1 |
The invention relates to novel phenol derivatives, a method for the production of said derivatives and their use in medicaments.
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WO/2003/002498A1 |
Novel halophenyl derivatives of the general formula (I), wherein R?1¿ is halogen, a leaving group or 1H-1,2,4-triazol-l-yl and R?2¿ is ethynyl or carboxy, X?1¿ is halogen and X?2¿ and X?3¿ are each independently hydrogen or halogen,...
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WO/2003/000664A1 |
The invention relates to uracils, methods for the production thereof, pharmaceutical compositions containing said uracils, and the use of the same for treating diseases affecting humans or animals. The inventive compounds are of general ...
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WO/2003/000180A2 |
Compounds having Formula I, including pharmaceutically acceptable salts and prodrugs thereof: (Formula I) are inhibitors of the dipep tidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of DP-IV mediated diseases and condi...
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WO/2003/000653A1 |
The invention relates to novel substituted N-acyl aniline derivatives of general formula (I), where R?1¿ to R?5¿, A, X, Y and Z are as defined in claim 1, the tautomers, stereoisomers, mixtures, prodrugs, derivatives with a group, nega...
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WO/2002/100813A2 |
Disclosed is a compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aromatic group. Q is a covalent bond, -CH¿2?-or-CH¿2?CH¿2?-; W is a substituted or unsubstituted alkylene or a substituted or unsubsti...
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WO/2002/098849A2 |
Disclosed are compounds of formula X, where R¿n?, R¿20?, R¿1?, R¿2?, R¿3?, and R¿c? are defined herein. These compounds are useful in treating Alzheimer's disease and other similar diseases. Pharmaceutical compositions comprising c...
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WO/2002/098844A1 |
The invention relates to a method for producing perfluoroalkanesulfonic acid esters and for further transforming the same into the salts thereof. The invention also relates to the use of the produced compounds in electrolytes, batteries,...
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WO/2002/098848A1 |
The present invention provides antitumor compounds of the formula(I), and antitumor methods.
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WO/2002/098852A2 |
The invention concerns compounds of general formula (I), wherein, in particular: W represents H, SO¿2?R¿5?, CO(CH¿2?)¿n?R¿5?, (CH¿2?)¿n?R¿6?, CS(CH¿2?)¿n?R¿5?; X represents S or NH; Y represents (CH¿2?)¿p?, CO, (CH¿2?)¿p?C...
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WO/2002/098363A2 |
Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating mammalian re...
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WO/2002/096910A1 |
The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins o...
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WO/2002/096905A1 |
The present invention provides a compound of formula I: or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK3, Aurora2, and Syk mammalian protein kinases. ...
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WO/2002/096361A2 |
The present invention relates to certain 5-aralkylsulfonyl-3- (pyrrol-2-ylmethylidene)-2-indolinone derivatives that inhibit kinases, in particular met kinase. Pharmaceutical compositions comprising these compounds, methods of treating d...
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WO/2002/096902A1 |
The invention relates to novel carbazole derivatives, their use for the preparation of a pharmaceutical composition for the treatment of eating and metabolic disorders such as obesity, bulimia nervosa, anorexia nervosa, of sleep disturba...
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WO/2002/096883A1 |
There is provided compounds of formula (I), wherein X¿1?, X¿2?, X¿3?, X¿4?, Y¿1?, Y¿2?, Y¿3?, Y¿4?, Z¿1?, Z¿2?, R?4¿ and R?5¿ have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compou...
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WO/2002/096888A1 |
The invention relates to the pyrimidine derivatives of general formula (1), wherein R?1¿, R?2¿, X, A and B are defined as in the description, for use as inhibitors of the cyclin-dependent kinase. The invention further relates to the pr...
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WO/2002/094817A1 |
The invention relates to a method for the production of triazolylmethylepoxide isomers of formula (I), where A and B independently = C¿1?-C¿4? alkyl, phenyl-(C¿1?-C¿2? alkyl), C¿3?-C¿6? cycloalkyl, C¿3?-C¿6? cycloalkenyl, tetrahy...
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WO/2002/094883A2 |
This invention describes a one pot, single-step process for the preparation of halide-free hydrophobic salts comprising polyalkylated imidazolium cations and various anions in accordance with the following structure, where R?1¿ and R?3Â...
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WO/2002/094796A2 |
The present invention relates to benzo[g]quinoxaline derivatives of the general formula (I), processes for manufacturing said benzo[g]quinoxaline derivatives, the use of the benzo[g]quinoxaline derivatives as pharmaceutically active agen...
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WO/2002/094819A1 |
The invention relates to a method for producing triazolyl methyl oxiranes of formula I wherein A and B are the same or different and independently represent C¿1?-C¿4?-alkyl, phenyl-C¿1?-C¿2?-alkyl, C¿3?-C¿6?-cycloalkyl, C¿3?-C¿6?...
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WO/2002/092608A2 |
The invention relates to a novel method for producing nucleophilic substitutions, particularly of type SNAr and SN2. More specifically, the invention relates to the use as a fluorinating reaction medium of ionic liquid or fused salt comp...
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WO/2002/092575A1 |
The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion associated events such as viral transmi...
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