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WO/2001/021599A1 |
The present invention relates to an isoxazoline derivative of formula (I), the pharmaceutically acceptable salts, esters and stereochemically isomeric forms thereof, and the use of the derivative in inhibiting the activity of caspases. T...
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WO/2001/019791A2 |
The invention relates to 3-vinylpryrrole derivatives of general formula (I), wherein M represents a substituted peptide, a substituted hydantoin or thiohydantoin, tetrazole, lactam or lactone group, Y and Z independently represent a hydr...
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WO/2001/019788A2 |
Compounds of the formula A - Q - D - E - G - J - X in which D is a direct link, a substituted or unsubstituted phenyl or naphthyl group or a heterocyclic ring system; X is a substituted or unsubstituted phenyl or naphthyl group or a hete...
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WO/2001/019798A2 |
Compounds of formula A Q D E G J X in which D is a direct link, a substituted or unsubsituted phenyl or naphtyl gourp or a heterocyclic ring system; G is substituted or unsubstituted phenyl or a heterocyclic ring system; X is a substitut...
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WO/2001/018171A2 |
The present invention provides the compound having formula (I), wherein each of R¿1? and R¿2? is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or p...
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WO/2001/014338A1 |
The invention relates to novel compounds of formula (I) which are biologically active when present as ligands of the integrin $g(a)¿v?$g(b)¿3?: X-Y-Z-R?1¿-CH¿2?-R?2¿(R?4¿)-CH¿2?-CO-R?5¿ wherein the meaning of X, Y, Z, R?1¿, R?2Â...
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WO/2001/014345A1 |
Disclosed are 5-propynylpyrimidine derivatives of formula (I) wherein X is a leaving group, R¿1? is selected from the group consisting of -OH,-NH¿2?, and -SH; R¿2? is selected from the group consisting of -H, 2-deoxyribose and ester d...
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WO/2001/014372A2 |
A neurotrophin production/secretion promoting agent which comprises an azole derivative of formula (I), wherein R?1¿ represents a halogen atom, a heterocyclic group which may optionally be substituted, a hydroxy group which may optional...
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WO/2001/014371A1 |
N-Heterocyclic derivatives of formula (Ya) are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibit...
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WO/2001/011965A1 |
The invention relates to compounds of general formula I, where A?1¿, R?1¿, R?2¿ and Y are as defined in the description; and to their use as phytopathogenic fungicides.
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WO/2001/012187A2 |
The present invention relates to the use of certain benzoic acid derivatives of formula (I), where the substituents are as defined in the specification, which act as peroxisome proliferator activated receptor (PPAR) agonists, in particul...
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WO2000050418A9 |
The invention concerns compounds selected among the group consisting of (i) compounds of formula (I) wherein: Het1 represents a nitrogenous heterocycle with 5 apices, in particular imidazole, pyrazole, or triazole; Het2 represents a nitr...
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WO/2001/010380A2 |
Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided.
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WO/2001/010827A1 |
$g(a)-Amino hydroxamic acid derivative of formula (I), in which R is C¿2?-C¿7?-alkyl, which is mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C¿3?-C¿5?-cycloalkyl or unsubstituted or substitut...
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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/2001/010863A2 |
The invention relates to thienyl(amino)sulfonylureas of formula (I), wherein A, Q, R?1¿, R?2¿, R?3¿, R?4¿ and R?5¿ have the meaning given in the description, and to a method for the preparation of said compounds and their use as her...
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WO/2001/007431A2 |
Compounds of formula (I) in which R?1¿, R?2¿, Y, L and Z have the meanings given in the specification are GluR6 antagonists useful for the treatment of disorders of the central nervous system.
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WO/2001/007643A1 |
A novel method for evaluating the drug effect of an antimicrobial agent which comprises eliminating the antimicrobial agent remaining in a biological sample, etc. to thereby accurately evaluate the drug effect of the antimicrobial agent ...
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WO/2001/007409A1 |
The use of a compound of formula (I) in the manufacture of a medicament for the treatment, in a warm-blooded animal, of disorders mediated by the neuropeptide Y5 receptor wherein R¿1?, R¿2?, A, B, R¿3? and R¿4? are as defined within ...
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WO/2001/005783A1 |
Bradykinin B¿1? receptor antagonists of formula (I) are disclosed. The compounds are useful for treating diseases associated with inappropriate bradykinin receptor activity, such as diabetic vasculopathy, inflammation, pain, hyperalgesi...
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WO/2001/004087A1 |
A pharmaceutical compound of formula (I) in which the aminosulfonyl group is attached at the 3- or 4-position, and in which R?1¿ is hydrogen, C¿1-6? alkyl, C¿3-10? cycloalkyl, C¿3-10? cycloalkyl-C¿1-4? alkyl or optionally substitute...
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WO/2001/004102A1 |
The invention concerns quinazoline derivatives of Formula (I) wherein Q?1¿ includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q?3¿-X?1¿- wherein X?1Â...
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WO/2001/002349A1 |
Phenyl sulfamate derivatives of general formula (I) or salts thereof, exhibiting an excellent steroid sulfatase inhibitory activity and being therefore effective in the prevention or treatment of diseases related to steroids including es...
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WO/2001/003211A1 |
Improved nonaqueous electrolytes for application in electrical storage devices such as electrochemical capacitors or high energy density batteries are disclosed. The electrolytes of the invention contain salts comprising alkyl substitute...
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WO/2001/000578A1 |
Certain 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatmen...
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WO/2001/000581A1 |
The present invention includes array of new chiral ligands that are optically active or racemic. These ligands are bidentate, tridentate, tetradentate or pentadentate ligands which include P-P, P-N, N-N, mixed P-N, Schiff base or carbene...
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WO/2000/078730A1 |
The dihydropyrimidine derivative of structural formula (I) and analogues thereof exhibit a selective inhibitory activity against N-type calcium channel and are useful as remedies for various diseases related to the calcium channel.
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WO/2000/078723A1 |
The present invention relates to a novel process for the preparation of butoxycarbonylimino compounds, in particular (tert-butoxycarbonylimino-pyrazol-1-yl-methyl)-carbamic acid tert-butyl ester, otherwise known as bis-boc-1H-pyrazole-1-...
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WO/2000/078728A1 |
The present invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous s...
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WO/2000/076991A1 |
A process is provided for preparing chiral cyclopropane carboxylic acids, preferably of structure (I) which are intermediates used in preparing acyl guanidine sodium/proton exchange (NHE) inhibitors.
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WO/2000/075131A1 |
Substituted pyrazole compounds of general formula (I) or salts thereof, which exhibit an excellent p38 MAP kinase inhibiting effect and are useful in the prevention or treatment of tumor necrosis factor $g(a)-related diseases, interleuki...
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WO/2000/074679A1 |
Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, contr...
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WO/2000/072956A1 |
Ionic liquids were rapidly and efficiently prepared by microwave-assisted chemical transformations. A method for performing microwave-assisted reactions, including alkylation reactions, using ionic liquids as solvent resulted in high yie...
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WO/2000/073283A1 |
The present invention provides compounds, and pharmaceutical compositions containing those compounds, that are active at metabotropic glutamate receptors. The compounds are useful for treating neurological diseases and disorders. Methods...
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WO/2000/071509A1 |
The present application relates to compounds of the general formula A-Y-D-E-G-J-K-L, wherein A, Y, D, E, G, J, K and L have the meanings given in the description, having activity against mammalian factor Xa. The compounds are useful in v...
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WO/2000/071119A1 |
MAG expression promoters containing compounds represented by general formula (I), optically active isomers thereof or pharmaceutically acceptable salts of the same, wherein each symbol is as defined in the description. As an example of t...
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WO/2000/071512A1 |
The present application relates to compounds of the general formula A-Y-D-E-G-J-Z-L, wherein A, Y, D, E, G, J, Z and L have the meanings given in the description, having activity against mammalian factor Xa. The compounds are useful in v...
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WO/2000/071529A1 |
The invention provides substituted phenyl compounds of general formula (I) wherein R?1¿, T, U and Ar are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for prepar...
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WO/2000/069853A1 |
Azole compounds represented by general formula [1a] or [1b]; and herbicide compositions containing effective amounts of the compounds. In said formulas, Q, X, p, R?1¿ to R?6¿, R?12¿ to R?15¿, and Z?1¿ to Z?4¿ are each as defined in...
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WO/2000/069821A1 |
A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-...
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WO/2000/069826A1 |
The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds having Formula (I) or a pharmaceutically acceptable salt thereof, wherein: a.o., $g(C) is selected from the group consisting of NH and NOH; useful as ...
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WO/2000/069841A2 |
Benzofuranylaminoalcohols of general formula (I), process for their preparation and their use in medicaments, especially for the treatment of inflammatory processes.
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WO/2000/066112A1 |
Invented are substituted cyclam derivatives, pharmaceutical compositions containing these compounds, the use of these compounds as CXCR-4 receptor antagonists and to use of these compounds as thrombopoietin (TPO) mimetics.
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WO/2000/066120A1 |
Compounds, pharmaceutically acceptable salts, and compositions thereof of general formula (I): wherein Ar is aryl and heteroaryl; R?1¿, R?2¿, R?3¿, and R?4¿ are hydrido, alkyl, cyano, heteroaryl, hydroxy, amino, acylamino, halo, alko...
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WO/2000/066580A2 |
The present invention concerns compounds of formula (I) the N-oxide forms, the salts, the quaternary amines and stereochemically isomeric forms thereof, wherein D represents a tetrahydrofuran or dioxolane ring substituted with aryl and a...
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WO/2000/064445A1 |
Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure (I) wherein n is 0 to 4; X is a bond, O, S, SO, SO¿2?, CO, (a), or NR?7¿; Y is a bond, O, S, SO, SO¿2?, CO, (b) or NR?7'¿ wherein...
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WO/2000/064873A1 |
The present invention relates to compound of formula (I) wherein R?1¿, R?2¿ and R?3¿ are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment of diseases wh...
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WO/2000/063198A1 |
Compounds represented by general formula (I) or salts thereof; and use of both in hair tonics and so on: wherein R?1¿ and R?2¿ are each independently an optionally substituted C¿1?-C¿30? hydrocarbon group or an optionally substituted...
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WO/2000/063183A1 |
The invention relates to a process for the preparation of substituted pyrimidines of formula (I), wherein R?1¿, R?2¿, R?3¿, R?4¿ and X are as defined in Claim 1, which comprises reacting an amidine of formula (II), or a salt thereof,...
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WO/2000/063171A1 |
Compounds of general formula (I) or salts thereof, useful as the active ingredient for appetite regulating agents efficacious for neuropeptide Y-related diseases, hyperphagia or the like wherein A is a five- to seven-membered hydrocarbon...
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