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WO/2002/050090A1 |
Hypocholesterolemic sugar-substituted 2-azetidinone compounds of the formula: are disclosed, as well as a method of lowering cholesterol by administering said compounds, pharmaceutical compositions containing them, and the combination of...
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WO/2002/050046A1 |
Compound of formula (I), wherein X is C¿1-6? alkylene or C¿2-6? alkenylene, each of which is optionally substituted by one or more flluorine atoms; R is aryl or C¿3-8? cycloalkyl optionally substituted by one or more fluorine atoms; W...
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WO/2002/046199A1 |
This invention relates a process for preparing a compound of formula (I) wherein R?1¿ is para-nitrobenzyl or allyl; and X is halo, which is useful to prepare 3-cyclic-ether-substituted cephalosporins, from trimethylphosphinic compounds....
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WO/2002/044145A1 |
There is provided a compound of formula (I) wherein R?a¿, R?1¿, R?2¿, Y and R?3¿ have meanings given in the description and pharmaceutically-acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are use...
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WO/2002/036157A1 |
According to the invention there is provided the use of melagatran, or a pharmaceutically-acceptable derivative thereof, for the manufacture of a medicament for the treatment of ischemic disorders in patients having, or at risk of, non-v...
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WO/2002/032377A2 |
The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for t...
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WO/2002/030929A1 |
Pleuromutilin compounds of the formula (A) & (B) are of use in anti-bacterial therapy.
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WO/2002/028815A1 |
A compound of the formula in which R?1¿ and R?2¿ are each hydrogen or C¿1-4? alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl or morpholino group...
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WO/2002/028829A2 |
The invention is directed to a novel class of compounds, which inhibits peptide deformylase, pharmaceutical compositions containing compounds that inhibit peptide deformylase, and method of treating various infections.
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WO/2002/026705A2 |
The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one s...
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WO/2002/026750A2 |
Disclosed are substantially enantiomerically pure bis-phosphine compounds comprising a substantially enantiomerically pure chiral backbone linking two phosphine residues wherein one of the phosphine residues has three phosphorus-carbon b...
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WO/2002/026720A2 |
Novel compounds of the general formulae (I) or (II), including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containin...
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WO/2002/024629A1 |
The present invention is directed to certain novel compounds represented by structural formula (I), or a pharmaceutically acceptable salt thereof, wherein R?3¿, R?5¿, R?6¿, R?7¿, R?8¿, R?11¿, R?12¿, R?13¿, Q, W, X, Y and Z are de...
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WO/2002/024197A1 |
This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.
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WO/2002/024636A2 |
N-Benzoyl arylsulfonamides having the formula (I) are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.
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WO/2002/022572A2 |
One aspect of the present invention relates to heterocyclic compounds formula A; whereof the substituents are defined in the description. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligand...
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WO/2002/022592A2 |
Compounds represented by structural formula (I) including its N-oxides wherein Y is (a) or (b); R?1¿ is H or (C¿1?-C¿6?)alkyl; R?2¿ is H,(C¿1?-C¿6?)alkyl,(C¿3?-C¿9?)cycloalkyl or (C¿3?-C¿7?)cycloalkyl(C¿1?-C¿6?)alkyl; R?3¿ i...
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WO/2002/022549A1 |
A process which comprises reacting a 2- or 4-nitro- benzenesulfonamide with an alkali metal alkoxide to remove the nitrobenzenesulfonyl group and thereby obtain an amine corresponding to the amide, and, if necessary, reacting this amine ...
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WO/2002/020485A1 |
Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R¿2?, R¿3?, R¿4?, R¿5?, R¿6?, R¿7?, R¿8?, Het and X are defined herein. The compounds are useful for treating autoim...
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WO/2002/020476A2 |
Crystalline forms of [2R-[2$g(a)(R*),3$g(b)(R*)]]-3-(1-hydroxyethyl)-$g(g)-methyl
-$g(b),4-dioxo-2-azetidinebutanoic acid(4-nitrophenyl)methyl ester and crystalline form of ($g(g) R,2R,3S)-$g(a)-diazo-3-[(1R)-1-hydroxyethyl]-$g(g)-methyl...
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WO/2002/018432A2 |
The invention relates to a protein extracted from the intestines of vertebrates, which absorbs cholesterol. The protein could be identified using highly affine cross-linking compounds. The invention also relates to the use of this protei...
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WO/2002/014267A1 |
The present invention relates to compounds of formula (I) wherein U, V, W, A?1¿, A?2¿, A?3¿, A?4¿, A?5¿, A?6¿, m and n are as defined in the description and claims and pharmaceutically acceptable salts and/or pharmaceutically accep...
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WO/2002/014270A1 |
There is provided compounds of formula I, wherein Y and R?1¿ have meanings given in the description, and pharmaceutically acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are useful as, or are useful ...
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WO/2002/012187A1 |
There are provided novel compounds of formula (I) wherein R?1¿, R?2¿, R?3¿, R?4¿, R?5¿, R?6¿, R?7¿, R?8¿, R?9¿, W, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and r...
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WO/2002/012230A1 |
There is disclosed an azetidinones compound of the formula (I): Wherein R is hydrogen, or hydroxy protecting groups, R¿1? and R¿2? are each independently alkyl of 1-15 carbon atoms, benzyl, or cycloalkyl of 5-6 carbon atom which may ha...
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WO/2002/006221A2 |
This invention provides compounds of Formula (I), wherein R¿1?, R¿2?, R¿3?, W, X, and Z are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin res...
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WO/2002/006232A1 |
This invention provides compounds of Formula (I) wherein: R?1¿, R?2¿, R?3¿, R?4¿, R?5¿, T, T?1¿, T?2¿, and X are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting me...
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WO/2002/006269A1 |
Novel compounds of formula (I), wherein R?1¿, R?2¿, R?2'¿, R?2''¿, R?3¿, R?4¿, R?5¿, R?5'¿, R?5''¿, R?5'''¿, R?5''''¿, X, Y, U, V and W have the meanings given in claim no.1, are inhibitors of the coagulation factors Xa and VI...
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WO/2002/004402A1 |
Compounds of the general formula (|), which exhibit selective muscarinic M¿3? receptor antagonism, little have side effects, and are suitable for administration by inhalation and useful as therapeutic agents for respiratory system disea...
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WO/2002/002522A1 |
The present invention relates to novel cyclopropane-containing diaryl sulfide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibitin...
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WO/2001/092226A1 |
One aspect of the present invention relates to novel heterocyclic compounds, such as Formula (1). A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, ...
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WO/2001/081303A1 |
The invention relates to compounds of formula (I) wherein Ar?1¿ is pyridyl or phenyl, substituted by hydroxy, lower alkyl, halogen, amino, nitro, benzyloxy or lower alkoxy-lower alkoxy, or is the group (a) wherein Z?1¿ is a five member...
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WO/2001/077073A1 |
This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of Cathepsins K and L. These compounds are useful for treating diseases in which inhibition of bone res...
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WO/2001/072687A1 |
A compound of general formula (I), or pharmaceutically acceptable salts, solvates or polymorphs thereof; wherein R?3� is independ ently CF�3?, OCF�3?, C�1?-C�4?alkylthio or C�1?-C�4?alkoxy; n is 1, 2 or 3; and the other var...
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WO/2001/072704A1 |
The present invention relates to new azetidinone derivatives represented formula 2, synthetic process of that, and synthetic process of 1-$g(b)-alkyl azetidinone using that. According to the present invention, 1-$g(b)-alkyl azetidinone i...
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WO/2001/066534A2 |
Compounds of formula (I), compounds of formula (II), compounds of formula (III), and compounds of formula (IV), or pharmaceutically acceptable salts thereof are useful as H¿3? receptor antagonists. Processes to make the compounds and me...
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WO/2001/064632A1 |
The invention concerns a compound of formula (I) wherein R represents a CR¿1?R¿2? radical, C=C(R¿5?)SO¿2?R¿6? or C=C(R¿7?)SO¿2?alk, their preparation and pharmaceutical compositions containing them.
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WO/2001/064634A1 |
The invention concerns pharmaceutical compositions containing as active principle a compound of formula (I) wherein: R¿1? represents a -N(R¿4?)R¿5?, -N(R¿4?)-CO-R¿5?, -N(R¿4?)-SO¿2?R¿6? radical or one of its pharmaceutically acce...
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WO/2001/064633A1 |
The invention concerns pharmaceutical compositions containing as active ingredient a compound of formula (I) wherein: R¿1? represents a -NHCOR¿4? or -N(R¿5?)-Y-R¿6? radical; Y is CO or SO¿2?; R¿4? represents an -alk-SO¿2?R¿11?, -...
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WO/2001/060828A1 |
The present invention relates to novel processes for the preparation of 3-methylenecephams. More specifically, the present invention relates in part to the intramolecular cyclization of penicillin sulfoxide derived monocyclic azetidinone...
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WO/2001/058891A2 |
The present invention relates to piperazine and piperidine derivatives of Formula (1), with Q, X, Y, A, B and P as defined herein, which are especially useful for treating or preventing neuronal damage, particularly damage associated wit...
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WO/2001/056985A1 |
A process for preparing optically active azetidine -2-carboxylic acid efficiently, easily, simply, and industrially advantageously by cyclizing an optically active 4-amino- 2-halogenobutyric acid in an optical yield of as high as 90 % or...
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WO/2001/056986A1 |
There is provided a process for the production of a compound of formula (I), which process comprises reaction of a compound of formula (II), with a compound of formula (III), wherein R?1¿, R?2¿, n and R?3¿ have meanings given in the d...
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WO/2001/055104A1 |
A process for preparing optically active N-substituted azetidine-2-carboxylic acids of the general formula (2) efficiently, simply, easily and industrially advantageously by subjecting an optically active 4-(substituted amino)-2= halogen...
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WO/2001/051456A2 |
Hydroxyamidines and related compounds are provided which are suitable as antibacterial agents.
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WO/2001/047868A1 |
A phenylalanine derivative of formula (1-1) or analogues thereof exhibit an $g(a)¿4?$g(b)¿7? integrin inhibiting activity and selectivity for $g(a)¿4?$g(b)¿1? integrin, thus being useful as remedies for various diseases related to $g...
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WO/2001/046135A1 |
A process for preparing chiral isomers of N-protected 2-azetidinemethanol compounds of formula (5), particularly N-(phenylmethyl)-2-azetidinemethanol and N-BOC-2-azetidinemethanol, and especially the (R)-isomers thereof, as well as O-sub...
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WO/2001/041724A2 |
The invention relates to novel compositions for oxidation dyeing keratinic fibres, containing at least one paraphenylenediamine derivative with an azetidinyl group of formulae (I) and (II) as the oxidation base; to the dyeing method and ...
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WO/2001/042249A1 |
Fluorinated amine compounds, R'¿i?ArF-ER¿2?, where ArF is a fluoroaryl substituent, E is nitrogen or phosphorous, each R is independently a C¿1?-C¿20? hydrocarbyl substituent, or the two R's may be connected to form an unsubstituted ...
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WO/2001/029245A2 |
A process for the resolution of an enantiomeric mixture of $g(b)-lactams containing an ester, the process comprising selectively hydrolyzing the ester of one of the enantiomers by combining the mixture with homogenized liver.
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