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WO/2003/042168A1 |
The invention relates to &agr -oxygenated or &agr -thiolated carboxylic acid phenethylamide derivatives of general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein A stands for optionally substitute...
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WO/2003/042160A1 |
The invention provides novel β2 adrenergic receptor agonist compounds of Formula (I). WhereinR1 is methoxy or ethoxy, and R2 is hydrogen or phenyl; or R1 is hydrogen, and R2 is phenyl; and R3 is -CH2OH or -NHCHO, and R4 is hydrogen; or ...
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WO/2003/042167A1 |
The invention relates to $g(a)-oxygenated or $g(a)-thiolated carboxylic acid phenethylamide derivatives of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein A stands for optionally substitu...
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WO/2003/040096A2 |
Disclosed are compounds of the formula (I), wherein the variables RN, RC, R1, R25, R2, and R3 are as defined herein. These compounds have activity as inhibitors of betasecretase and are therefore useful in treating a variety of discorder...
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WO/2003/040074A1 |
A compound of formula (I) or a dimer thereof; where R?1¿ and R?2¿ are independently selected from optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, a functional group or a group of sub-formul...
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WO/2003/030937A1 |
Preventives and&sol or remedies for diseases, which are induced, worsened or made to recrudesce by stressors, comprising mitochondrial benzodiazepine receptor (MBR) antagonists such as compounds represented by the following general formu...
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WO/2003/029184A1 |
A diaryl ether derivative having excellent immunosuppressive activity and reduced in side effects. The diaryl ether derivative is represented by the general formula (1): (1) &lcub e.g., 2−amino−2−[4−(3−benzyloxyphenoxy)−2−c...
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WO/2003/029195A1 |
Acetonides of a ß−keto ester compound, ß−hydroxyacid compound, and 1,3−diol derivative respectively represented by the following formulae (I), (V), and (VIII): (I) (V) (VIII) (wherein the symbols are the same as defined in the de...
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WO/2003/027092A1 |
The separation of diastereomeric 1,3−diols, or the corresponding 1,3−diol acetals, or syn− and anti 1,3−diols of general formula (I) or (II), is conventionally only achieved with high technical complexity and loss of desired prod...
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WO/2003/027059A1 |
Acid amide derivatives represented by the formula (I) (I) [wherein A is phenyl optionally substituted by X, benzyl optionally substituted by X, naphthyl optionally substituted by X, a heterocyclic group optionally substituted by X, a fus...
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WO/2003/024448A2 |
The invention relates to the inhibition of histone deacetylase. The invention provides compounds e.g. (1) and methods for inhibiting deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell p...
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WO/2003/024955A2 |
The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein A, B, D, E, G, J, n, and R1 are as described generally and in classes and subclasses herein, and additionally provi...
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WO/2003/024953A1 |
A medicine containing as the active ingredient either a novel propanolamine derivative having a 1,4−benzodioxane ring or a pharmacologically acceptable salt thereof. (I) The compound is represented by the above formula (wherein R1 to R...
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WO/2003/024441A1 |
A medicinal composition which exasperates apo AI expression as a remedy for circulatory diseases based on the HDL function enhancement. It is an apo AI expression accelerator which contains a compound represented by the formula (I), a pr...
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WO/2003/022801A1 |
Reverse hydroxamic acid derivatives having specific structures represented by the general formula (Ia): (Ia) (wherein A represents hydrogen, etc.&semi Ar1 represents arylene, etc.&semi Ar2 represents optionally substituted aryl, heteroar...
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WO/2003/020688A1 |
Compounds of formula (I) or therapeutically acceptable salts thereof, are selective protein tyrosine kinase-B (PTP1B) inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of disorders using the c...
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WO/2003/018523A1 |
A process for easily producing from an inexpensive material an optically active halopropanediol derivative which is useful as an intermediate for medicines. An inexpensively available propargyl alcohol derivative is reacted with a hypoha...
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WO/2003/018555A1 |
A process for the preparation of compounds of formula (I) wherein R¿1? is unsubstituted or substituted C¿1?-C¿8?alkyl, R¿2?, R¿3?, R¿4? and R¿5? are each independently of the others hydrogen, unsubstituted or substituted C¿1?-C¿...
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WO/2003/014063A2 |
The invention relates to novel protected 3.5-dihydroxy-2.2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and to a method for the production and e use of said novel compounds in the production of epothilones or ep...
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WO/2003/013502A1 |
Compounds which mimic the chemical and/or biological activity of discodermolide are provided.
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WO/2003/014068A1 |
The invention relates to 3.5-dihydroxy-2.2-dimethyl-valeronitriles for the synthesis of epothilone and epothilone derivatives and a method for producing said novel intermediate products in the synthesis and the use thereof in the product...
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WO/2003/014064A1 |
Naphthylurea and naphthylacetamide derivatives of formula (I) which have vanilloid receptor 1 (VR1) antagonistic activity are disclosed, formula (I) wherein Y represents formula (II) and formula (III) and the variables Q, X, R6, R7, R8, ...
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WO/2003/009850A1 |
Selected substituted piperazine compounds are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, ...
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WO/2003/010157A1 |
The present invention relates to novel antidiabetic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs and pharmaceutically acceptable compositions containing them. More particularl...
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WO/2003/007956A1 |
A method for treating Attention Deficit/Hyperactivity Disorder (ADHD) in humans and the symptoms associated therewith, inattentiveness, and hyperactivity with impulsivity, using eltoprazine and related compounds is provided.
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WO/2003/008399A1 |
Disclosed is a novel enantiomeric synthesis cermamide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
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WO/2003/006423A1 |
Disclosed are compounds of the formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the betasecretase enzyme that are useful in the treatment of Alzeheimer's disease and ot...
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WO/2003/004459A2 |
A process is provided for the preparation of a compound of Formula (1) wherein: R?1¿ is H, optionally substituted acyl, optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl: R² and R³ each ind...
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WO/2003/004480A2 |
A novel class of substituted piperazines and diazepanes, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are us...
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WO2002062777A9 |
Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present inve...
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WO/2003/002524A2 |
The present invention relates to compounds of the formula I, in which R?1¿, R?2¿, R?4¿, R?5¿, D¿1?, D¿2?, X¿1?, X¿2?, X¿3?, A and B have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacol...
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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/2003/000181A2 |
Compounds having Formula (I), including pharmaceutically acceptable salts and prodrugs thereof are inhibitors of the dipeptidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of DP-IV mediated diseases and conditions, such ...
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WO/2003/000646A1 |
This invention relates to a series of substituted aromatic ethers of the formula (I), wherein ring A and X and Y are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptabl...
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WO/2002/100822A1 |
The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medic...
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WO/2002/098558A1 |
A carboxylic ester production catalyst which has higher catalytic activity. The catalyst, which is used for producing a carboxylic ester by reacting oxygen, an aldehyde, and an alcohol or (b) by reacting oxygen with one or more alcohols,...
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WO/2002/098832A1 |
The invention relates to CF¿2?O-bridged cyclohexane derivatives, in particular compounds of formula (I), R1-(-A1-Z1-)k1-Q-CF2O-A2-(-Z3-A3-)K3-R2, wherein Q represents group (a); W?1¿, W?2¿ represent -CH¿2?- and/or -0- independently f...
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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/2002/098851A1 |
The inventive derivatives of N,S-substitutions N'-1 [(hetero)aryl] alkyl-N'-[hetero) aryl] methyl isothioureas including bases and salts thereof with pharmacologically acceptable acids and individual optical isomers of said compositions ...
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WO/2002/099077A2 |
The invention relates to methods and reagents for selectively labeling membrane surface proteins using a labeling agent. The label may be used to isolate preparations of membrane surface proteins. Preparations of membrane surface protein...
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WO/2002/098854A2 |
A process is provided for preparing chiral diol sulfones of the structure (I) where R¿3? is preferably (II) or (III) where R¿4a? is preferably aryl such as phenyl, and R¿1a? is preferably alkyl such as t-butyl, which are intermediates...
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WO/2002/096864A1 |
The invention relates to carboxamide-substituted phenylurea derivatives and method for production thereof as medicaments, physiologically-acceptable salts and physiologically-functional derivatives thereof. Compounds of formula (I), in w...
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WO/2002/096424A1 |
A method for preventing or treating epileptogenesis-associated diseases comprising the administration of a $g(b)-heterocyclic-$g(b)-aminoacid to a subject is disclosed. The disease can be for example head trauma, pain, stroke, anxiety, s...
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WO/2002/096858A1 |
There is provided novel cinnamide derivatives of Formula I wherein R is C¿1-4? alkyl or trifluoromethyl, R?1¿ is selected from the group consisting of pyridinyl, quinolinyl, thienyl, furanyl, 1,4-benzodioxanyl, 1,3-benzodioxolyl, chrom...
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WO/2002/089782A2 |
In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I): and pharmaceutically acceptable derivatives thereof, w...
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WO/2002/087723A1 |
The invention relates to a reactor (1) for gas/liquid or gas/liquid/solid reactions comprising a vertical longitudinal axis, a feed inlet (2) for a liquid or liquid/solid educt stream in the upper area of the reactor and for a gaseous st...
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WO/2002/083661A1 |
The invention relates to a glycolide production process wherein a depolymerization reaction system comprising a glycolic acid oligomer or a glycolic acid oligomer and a polar organic solvent is heated to depolymerize the glycolic acid ol...
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WO/2002/079124A2 |
This invention relates to a process for preparing alditol acetals, such as dibenzylidene sorbitols, monobenzylidene sorbitols, and the like, through the reaction of unsubstituted or substituted benzaldehydes with alditols (such as sorbit...
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WO/2002/080161A2 |
The invention relates to an optical data carrier that contains a preferably transparent substrate that is optionally already coated with one or more reflective layers, onto whose surface an information layer which can be written on with ...
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WO/2002/079143A1 |
The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R?1¿ is optionally substituted C¿1-6?alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C¿1-...
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