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WO/2000/061539A1 |
A pharmaceutical compound of formula (I) in which R?1¿ and R?2¿ are each hydrogen or C¿1-4? alkyl, or R?1¿ and R?2¿ together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperaziny...
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WO/2000/061540A1 |
The present invention provides processes for the preparation of 3-aryloxy-3-arylpropylamines and intermediates thereof using an nucleophilic aromatic displacement in 1,3-dimethyl-2-imidazolidinone or N-methylpyrrolidinone.
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WO/2000/061708A1 |
The invention relates to polyalkene alcohol polyetheramines of formula R?1¿-(CH¿2?)¿n?-(O-A)¿m?-NR?2¿R?3¿, wherein R?1¿ represents a polyalkene radical derived from C¿2?- to C¿30?-alkenes with a number average molecular weight o...
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WO/2000/059851A1 |
Methods of preparing, and compositions comprising, derivatives of venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depressi...
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WO/2000/059875A2 |
Derivatives of aryl and heterocyclic ureido and aryl and heterocyclic carboxamido phenoxy isobutyric acids have been found to inhibit the nonenzymatic glycation of proteins which often results in formation of advanced glycation endproduc...
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WO/2000/059883A2 |
The invention relates to a method for producing N-aryl-aza-heterocycles of general formula (I) in which: R1, R2, R3, R4 and R5 are the same or different and represent a hydrogen atom, a nitro group, a cyano group, an alkoxycarbonyl group...
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WO/2000/058262A1 |
The present invention provides stereospecific processes for the preparation of tomoxetine using a nucleophilic aromatic displacement, processes to intermediates thereof, and intermediates thereof.
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WO/2000/053572A1 |
The invention relates to compounds of general formula (I) wherein R is hydrogen, lower alkyl, lower alkoxy, halogen, amino, -N(R?6¿)¿2? or trifluoromethyl; R?1¿ is hydrogen, lower alkoxy or halogen; R and R?1¿ may be together -CH=CH-...
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WO/2000/051967A1 |
This invention relates to very specific oxyalkylene-substituted aminophenol compounds as intermediates for the production of poly(oxyalkylene)-substituted xanthene (or other type) colorants. Such an inventive intermediate compound is pro...
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WO/2000/050379A1 |
The invention relates to a process for the preparation of (1R,2S,4R) -(-) -2- (2-dimethylaminoethoxy) -2 -phenyl -1,7,7- trimethylbicyclo [2.2.1] heptane of Formula (I) and pharmaceutically acceptable acid addition salts thereof starting...
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WO/2000/050380A1 |
The present invention relates to compounds that are a useful exhibit activity as serotonin, norepinephrine and dopamine reuptake inhibitors, and their pharmaceutically acceptable salts, and their use in the treatment of central nervous s...
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WO1996012697A9 |
The present invention features compounds of general formulae a), b), c), able to modulate one or more activities of an inorganic ion receptor and methods for treating diseases or disorders by modulating inorganic ion receptor activity. P...
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WO2000002887B1 |
One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and car...
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WO/2000/048987A1 |
The invention relates to novel substituted 3-phenoxy or 3-phenylalkyloxy-2-phenyl-propylamines of general formula (1), to methods for producing them and to their use as medicaments.
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WO/2000/047546A1 |
The invention relates to a method for the racemization of optically active amines by reacting the optically active amine in the presence of hydrogen and of a hydrogenation or dehydrogenation catalyst at an elevated temperature. According...
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WO/2000/047545A1 |
The invention relates to a method for producing racemic amines of formula (I), in which R?1¿ and R?2¿ are not the same and R?1¿, R?2¿, R?3¿ are alkyl-, cycloalkyl-, arylalkyl-, aryl-, heteroaryl rests and heterocyclic rests and R?3Â...
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WO/2000/047548A1 |
Novel protein binding compounds of Formula (III): W-X-Y-(Z)¿n? in which Y is a branching moiety, Z represents a polydentate ligand chelating agent that coordinates a metal ion; X is a spacer moiety; n is an integer of at least 2 and W i...
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WO1999063936A9 |
Novel multi-binding compounds (agents) which bind endothelin receptors are used to treat disorders affecting the cardiovascular, renal, endocrine and nervous systems in mammals that are mediated by the endothelin receptors, such as conge...
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WO/2000/046187A2 |
The present invention is directed to agmatine and polyamine analogs and their use as drugs, as well as agricultural or environmentally useful agents. As drugs, the analogs decrease cellular polyamine levels, possibly by inducing antizyme...
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WO/2000/046179A1 |
A process for producing an aromatic primary amine, characterized by hydrogenating an aromatic nitrile at a low partial pressure of hydrogen in a heterogeneous system comprising a nonreducing polar solvent and a supported nickel catalyst ...
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WO/2000/044812A2 |
The invention relates to amino-functionalised polyoxyalkanes of general formula (I) wherein n = 1-5, m = 5-100, a = 0.1, b = 0.1, R = branched or linear hydrocarbon chains with 1-30 C-atoms, branched or linear single or multiple olefinic...
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WO/2000/044701A1 |
Norbornadienyl derivatives represented by general formula (1) (wherein R?1¿ and R?2¿ are the same or different and each is either an aromatic group containing a heteroatom or a phenyl group having one to three substituents selected fro...
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WO/2000/044371A1 |
The use of a compound of formula (1), wherein R¿1?, R¿2?, R¿3?, R¿4?, R¿5? and R¿6? are independently selected from hydrogen, alkyl and aryl, or pharmaceutically acceptable salts thereof, with the proviso that wherein R¿1? to R¿4...
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WO/2000/043350A1 |
Crystal polymorphism of 2-[4-[2-[[1s,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methyl ethyl]amino]ethyl]phenoxy]acetic acid which has potent $g(b)¿2? adrenergic receptor stimulating and $g(b)¿3?-adrenergic receptor stimulating effects, is us...
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WO1999066944A9 |
Disclosed are novel multi-binding compounds (agents) which bind cellular receptors. The compounds of this invention comprise a plurality of ligands each of which can bind to such cellular receptors thereby modulating the biological proce...
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WO/2000/042999A1 |
Disclosed are compounds of formula (I) wherein R represents hydrogen or is a C-3 to C-6 cycloalkyl or C-4 to C-10 straight or branched carbon chain alkyl-cycloalkyl or a group -B-D, where B is C-2 to C-10 straight or branched carbon chai...
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WO2000006533B1 |
A compound of formula (I) where R<1> is CH and R<6> is a bond, or R<1> and R<6> together form an electron withdrawing group; R<2> and R<3> are independently selected from (CR<7>R<8>)n, or a group CR<9>R<10>, -(CR<7>R<8>CR<9>R<10>)- or -(...
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WO/2000/040529A1 |
The invention relates to the use of compounds of formula (I): wherein X is -C(O)-, -C(S)-, -C=NOH, or -CH(R?7¿)- wherein R?7¿ is hydrogen, hydroxy, C¿1-7?alkoxy, -OR?8¿ or -NR?8¿R?9¿ (wherein R?8¿ is a group -Y?1¿R?10¿ (wherein ...
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WO/2000/040560A1 |
A compound of formula (I) wherein X¿1? is bond or -OCH¿2?-; X¿2? is -(CH¿2?)¿n?-, in which n is 1, 2 or 3; X¿3? is bond, -O-, -S-, -OCH¿2?-, or -NH-; R?1¿ is phenyl or pyridyl each of which may have one or two substituent(s) sele...
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WO/2000/040555A1 |
The invention relates to a method for producing (2S,4R,9S)-octahydro-1H-indole-2-carboxylic acid. The invention is characterised in that a. a compound of the formula (I) (R?1¿O)¿2?CH-CH¿2?-CH(OR?2¿)¿2?, wherein R?1¿ and R?2¿ are e...
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WO/2000/040950A1 |
This invention relates to a method for monitoring a chemical reaction of pharmaceutical relevance, comprising the steps of: consecutively obtaining Raman spectrum samples of a solution of chemical constituents contained within a reaction...
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WO1999064035A9 |
Disclosed are multibinding compounds which are beta 2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system...
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WO/2000/039072A1 |
A method for preparing a compound of formula (IXa) from a compound of formula (VIIa), and preparation of intermediates useful in the method.
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WO/2000/037425A1 |
Disclosed is a method for producing N-methyl-3-(p-trifluoromethylphenoxy)-3-phenyl-propylamine and its acid addition salts by (i) converting 3-chlorine-1-phenyl-propane-1-ol and/or 3-bromine-1-phenyl-propane-1-ol with methylamine to 3-me...
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WO/2000/037426A1 |
The present invention relates to novel oxo-aminotetralin compounds of formula (I), wherein X, R¿1?, R¿2?, R¿3?, R¿4?, R¿5?, and R¿6? are defined herein. The compounds of formula (I) are useful in pain management.
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WO1999064034A9 |
The present invention is directed to multibinding compounds which are beta 2 adrenergic receptor agonists and are therefore useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis, and the like. They are...
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WO/2000/035882A1 |
1,2,3,4-Tetrahydronapthalene derivatives of formula (I) wherein R?1¿ is selected from hydrogen, C¿1-6?alkyl, C¿2-6?alkenyl, C¿2-6?alkynyl and phenylC¿2-6?alkyl and R?2¿, R?3¿, R?4¿ and R?5¿ are as defined in the specification ar...
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WO2000012454A9 |
A cationic lipid for transfection of macromolecules in which the lipid has a polyether or glyceryl backbone which lipids can be contained in a liposome to effectively transfect a variety of cell types and improve the efficiency of transf...
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WO/2000/032557A1 |
The invention concerns novel 3-alkoxybenzylamine derivatives of general formula (1) used as medicines in particular as antipsychotic drug.
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WO/2000/032559A1 |
A class of cationic ester surfactants is described which has improved hydrolytic stability. In particular, the present invention relates to the use of quaternized alkanol amine ester compositions wherein the ester is based on a secondary...
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WO/2000/032556A1 |
Methods of preparing, and compositions comprising, derivatives of (-)-venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depr...
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WO/2000/032555A1 |
Methods of preparing and compositions comprising, derivatives of (+)-venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depre...
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WO/2000/032554A1 |
A process for preparing a substantially single enantiomer of tramadol, or a pharmaceutically-acceptable salt thereof, proceeds by means of a classical salt resolution using a substantially single enantiomer of $i(o,o)-di-$i(p)-toluoyltar...
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WO/2000/030444A1 |
The present invention relates to synthetic cationic lipids, liposome formulations and the use of such compounds to introduce functional bioactive agents into cultured cells.
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WO/2000/031022A1 |
Amphiphilic polyamidine compounds (I) and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds, wherein each of X¿1?, X¿2?, X¿3?, ...
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WO/2000/031019A1 |
Aniline derivatives represented by general formula (1) (wherein R and R' each independently represents C¿1-10? alkyl, C¿1-10? alkoxyalkyl, or hydrogen; X represents cyano, halogeno, haloalkyl, haloalkyloxy, or 2-cyanoethynyl; Y represe...
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WO/2000/031021A1 |
Compounds represented by general formula (I), salts thereof or prodrugs of the same which exhibit an excellent effect of inhibiting $g(b)-amyloid protein production/secretion, wherein Ar represents an aromatic group; X and Y represent ea...
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WO/2000/029357A1 |
The invention relates to a method for the racemization of optically active amines by reacting an optically active amine in the presence of hydrogen with a hydrogenation or dehydrogenation catalyst at an elevated temperature, wherein said...
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WO/2000/027790A1 |
A compound of formula (IA) or (IB): in which R?1¿ is R?A¿(CH¿2?)¿n?O(CH¿2?)¿m?, R?A¿(CH¿2?)¿p?, Formula (II) or in which R is a spiro-fused mono- or bi-cyclic ring containing one or two basic nitrogen atoms; and X?1¿ and X?2¿,...
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WO/2000/027795A1 |
Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having general structure (A).
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