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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/2003/041649A2 |
The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K. Pharmaceutical composition comprising these compounds, method of...
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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/2003/040080A2 |
This invention is directed to lipoxin A¿4? analogs of the following formulas (I) and (II), wherein R?1¿, R?2¿, R?3¿, R?4¿ and R?5¿ are described herein. These analogs are useful in treating inflammatory and autoimmune disorders in ...
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WO/2003/040088A1 |
A process for preparation of fluorinated sulfides, characterized by reacting a sulfide of the general formula (1) having at least one hydrogen atom with IF5 to thereby replace at least one hydrogen atom of the sulfide by a fluorine atom:...
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WO/2003/037853A1 |
The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.
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WO/2003/037854A1 |
Disclosed is a method of preparing intermediates required for synthesis of natural carotenoid products using sulfone compounds, which is advantageous in terms of high preparation efficiency due to a relatively simple process. Specificall...
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WO/2003/034989A2 |
Acylated $g(a)-hydroxyarylbutanamines and related sulfonamides, ureas and carbamates that inhibit aspartyl protease are disclosed, as are methods of treating diseases, particularly HIV, using these compounds. The compounds have the formu...
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WO/2003/035603A1 |
The invention relates to novel substituted acetic acid derivatives, to methods for their production and to their use in medicaments, in particular as potent compounds for PPAR-delta activation, for the prophylaxis and/or treatment of car...
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WO/2003/033453A1 |
A novel class of dicarboxylic acid derivatives, the use of these compounds as phar-maceutical compositions, pharmaceutical compositions comprising the compounds and meth-ods of treatment employing these compounds and compositions. The pr...
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WO/2003/033470A1 |
According to the invention there is provided a compound the formula I&semi wherein : A is an optionally substituted: phenyl, naphthyl, pyridyl, pyrazinyl, pyridazinyl, paramidal, thienyl, thiazolyl, oxazolyl or thiadiazolyl&semi B is an ...
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WO/2003/033447A1 |
Compounds represented by the following general formula (I): R−Y−(−X−Phe−COCH2COCnF2n&plus 1)m (I) wherein R represents hydrogen, alkyl, phenyl or a group capable of binding to a protein, a peptide, an amino acid, a nucleic acid...
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WO/2003/030812A2 |
This invention relates to 1-[(4-methyl thio)phenyl]-2-(phenyl acetoxy)-1-ethanone. This compound is convertible into 4-(4-methyl thio phenyl)-3-phenyl-2 (5H)-furanone by an economically viable process. This substituted furanone is an int...
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WO/2003/031399A1 |
A process for preparing an intermediate compound of formula (II) where n is an integer of from 3 to 14; R?1¿ is haloC¿1-10?alkyl, C¿1-10?alkyl, C¿2-10?alkenyl, C¿2-10?cycloalkyl, carboxyC¿1-10?alkyl, C¿1-10?alkoxycarbonylC¿1-10?a...
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WO/2003/029206A1 |
The present invention is concerned with novel HIV protease Inhibitors of formula (I), as individual isomers, racemates, non-racemic mixtures or mixtures of diastereoisomers; wherein A is a group formulas (II, III), n, R?1¿, R?2¿, R?3¿...
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WO/2003/029185A1 |
There are provided novel compounds of formula (I) wherein A, R?1¿, R?3¿, R?4¿, R?5¿, T, U, V, W, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparatio...
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WO/2003/029205A1 |
A diaryl sulfide derivative having excellent immunosuppressive activity and reduced in side effects. The diaryl sulfide derivative is represented by the general formula (1): (1) &lcub e.g., 2−amino−2−[4−(3−benzyloxyphenylthio)â...
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WO/2003/029477A1 |
The compounds of formula (I) are useful for the preparation of 1,5-benzothiazepines which are useful as enzyme inhibitors, such as protease, interleukin-1$g(b)-converting enzyme, elastase or angiotensin enzyme, GPCR antagonists (cholecys...
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WO/2003/029198A1 |
The invention relates to the use of compounds having general formula X-(A)¿n?-Y, wherein: n varies between 6 and 20; X denotes a hydrogen atom, an R¿a?CO, R¿a?OCO, R¿a?NHCO or R¿a?SO¿2? group, R¿a? being an alkyl, alkenyl, alkynyl...
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WO/2003/029200A2 |
Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R¿1?, R¿2?, R¿3?, R¿4?, R¿5?, R¿6?, R¿8?, R¿9? and X aredefined herein. The compoundsare useful for treating autoi...
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WO/2003/029188A2 |
The present invention describes pesticidal β-substituted nitrostyrene and cyanostyrene compounds having the formula I: wherein A,Ar,R,R1,Y,X,k,l, and m are as defined herein. The present invention is directed to compositions that includ...
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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/2003/024395A2 |
Compounds, compositions and methods that are useful for the treatment of metabolic disorders, inflammatory diseases and cancer are provided herein. In particular, the invention provides compounds which modulate the expression and/or func...
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WO/2003/024390A2 |
A hydroxyeicosenoic acid analog represented by the following Formula (I), the bond $m(Z) represents a cis-vinylene group or an ethynylene group; Y represents CH?2¿, O or S(O)?p¿ wherein p is 0, 1 or 2; m represents an integer of 1 to 4...
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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/2003/024591A1 |
The invention relates to a process for the preparation of an active alumina catalyst impregnated with a base, which is chosen from alkali or alkaline earth metals and its synthetic applications. The catalyst has been used for the protect...
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WO/2003/024922A1 |
A hydroxyfattysulfonic acid analog represented by Formula (I): wherein X is an ethylene group, a vinylene group or an ethynylene group; Y is an ethylene group, a vinylene group, an ethynylene group, OCH¿2? or S(O)pCH¿2? wherein p is 0,...
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WO/2003/022277A1 |
The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic ac...
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WO/2003/022802A1 |
A compound having a thioacetal skeleton, precursor therefor, cured article, and composition for producing these are provided as thermally dissociable materials, based on the inventor's finding that a thioacetal group thermally dissociate...
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WO2002087556A9 |
It has been discovered that certain selected probucol monoesters, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) i...
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WO/2003/020694A1 |
The invention relates to derivatives of C2-substituted indan-1-ol systems and to their physiologically compatible salts and physiologically functional derivatives. The invention concerns compounds of formula (I), wherein the radicals hav...
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WO/2003/020696A1 |
The invention relates to C2-substituted indane-1-ols and to their physiologically compatible salts and physiologically functional derivatives. The invention also relates to compounds of formula (I), wherein the groups are defined as per ...
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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/2003/020697A1 |
The invention relates to C2-disubstituted indane-1-ones and to their physiologically compatible salts and physiologically functional derivatives. The invention also relates to compounds of formula (I), wherein the groups are defined as p...
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WO/2003/020677A2 |
The invention relates to C2-substituted indane-1-ones and to their physiologically compatible salts and physiologically functional derivatives. The invention also relates to compounds of formula (I), wherein the groups are defined as per...
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WO/2003/020199A1 |
The invention relates to the use of C2-substituted indan-1-ol systems, and to the physiologically tolerable salts and the physiologically functional derivatives of the same, for producing medicaments used to reduce the weight of mammals,...
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WO/2003/020695A1 |
The invention relates to C2-disubstituted indane-1-ol systems and to their physiologically compatible salts and physiologically functional derivatives. The invention also relates to compounds of formula (I), wherein the groups are define...
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WO/2003/020693A1 |
The invention relates to polysubstituted indan-1-ol systems, the physiologically acceptable salts and physiologically functional derivatives thereof. The invention relates to the compounds of formula (I), wherein the groups are defined a...
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WO/2003/018530A1 |
An iodine compound represented by the following general formula (I): (I) (wherein Ar1 and Ar2 each independently represents (un)substituted aryl having at least one iodine atom as a substituent&semi L1 and L2 each independently represent...
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WO/2003/018535A2 |
The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compo...
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WO/2003/018070A1 |
This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compound...
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WO/2003/018544A1 |
The present invention relates to an efficient and industrially advantageous process for the preparation of pure cilastatin.
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WO/2003/018665A1 |
The present invention relates to a process for the preparation of activated polyethylene glycols, or PEG(NPC)?2¿s, comprising reacting polyethylene glycol with an activator while in the presence of an aromatic nitrogen containing hetero...
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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/2003/014062A1 |
Certain thiol and acylthiol compounds inhibit retrovirus growth by attacking the highly conserved zinc finger regions of essential viral proteins. These compounds, compositions containing them, and methods of using them to treat retrovir...
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WO/2003/014073A1 |
The invention concerns novel molecules, their preparation and their uses, in particular in the field of human and veterinary medicine and in cosmetics. The inventive compounds are partly fatty acid derivatives and exhibit advantageous ph...
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WO2002030882A9 |
The present invention relates to novel sulfoxide and bis-sulfoxide compounds, compositions comprising sulfoxide and bis-sulfoxide compounds, and methods useful for treating and preventing caridovascular diseases, dyslipidemias, dysprotei...
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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/2003/014064A1 |
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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