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WO/2009/074789A1 |
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11Î...
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WO/2009/068253A2 |
The present invention refers to a stable crystalline salt of (R)-3-fluorophenyl-3,4,5-trifluorobenzylcarbamic acid 1-azabicyclo[2.2.2]oct-3-yl ester of formula (I) and its use as medicament, in particular for the treatment of urinary inc...
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WO/2009/046624A1 |
The solution pertains to the technical field of organic chemistry, in particular to preparation methods of (4S,5R)-semiesters comprising the enantioselective ring-opening of cyclic acid anhydrides with alcohols under the catalysis of cin...
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WO/2009/046025A1 |
The present invention relates to compounds and formulations capable of affecting nicotinic acetylcholine receptors (nAChRs), for example, as modulators of specific nicotinic receptor subtypes (specifically, the alpha7 nAChR subtype). The...
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WO/2009/031526A1 |
Disclosed is a process for producing an optically active 3-quinuclidinol derivative having a high optical purity in high yield by using a readily available ruthenium compound as an asymmetrical reduction catalyst. Specifically disclosed ...
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WO/2009/013535A1 |
The invention relates to 2-aza-bicyclo[2.2.2]octane compounds and uses thereof. Particularly the invention relates to such compounds and their uses as pharmaceuticals in treating pyshoses such as schizophrenia and other diseases, disorde...
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WO/2009/010299A1 |
The present invention relates to substituted heteroarylpiperidine derivative (I) as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or se...
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WO/2009/010987A1 |
The present invention relates to an improved and industrially viable process for the preparation of high purity >99.8% chemical and >99.8% chiral of palonosetron hydrochloride of formula-I ((3as)-2[(3s)-1-azabicyclo [2.2.2] oct-3-yl]-2,3...
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WO/2009/011844A1 |
Processes for preparing solifenacin comprising distilling ethanol and organic solvent from a reaction mixture and recycling the organic solvent are described. Preferably the ethanol is removed using a Dean-Stark apparatus. Also described...
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WO/2008/146774A1 |
[PROBLEMS] To provide a compound which can be used as a medicinal agent, particularly a therapeutic agent for irritable bowel syndrome (IBS). [MEANS FOR SOLVING PROBLEMS] It is found that a tetrahydroisoquinolin-1-one derivative having a...
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WO/2008/145243A1 |
Compounds of formula (I), where R1, R2 and R3 have the meanings given in claim 1 are tyrosine kinase inhibitors, in particular of Met kinase and can amongst other things be used for treating tumours.
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WO/2008/132679A1 |
The invention relates to compounds of formula (I), wherein R1, R2, R1a, R2a, R3, R4, A, B, X, W and n are as defined in the description, and pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium chann...
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WO/2008/129054A2 |
The present invention relates to heterocyclic compounds of the formula (I) wherein - the heterocycle comprises two double bonds which may be present at several positions, represented by the dashed lines ( -- ); - the heterocycle contains...
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WO/2008/120080A2 |
The present invention provides an improved synthetic strategy for the preparation of solifenacin and pharmaceutically acceptable salts thereof.
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WO/2008/112900A1 |
The present invention relates to 11-(piperazin-l-yl)dibenzo[b,f][l,4]oxazapine compounds of the formula I (I) where the variables are as defined herein, their salts and pharmaceutically acceptable compositions thereof. Methods of prepari...
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WO/2008/107545A1 |
The invention relates to a 1-aza-bicyclo [2.2.2] oct-2-en- 3-ylmethyl acetate of the formula (I), wherein said compound is useful as a synthesis intermediate for the production of mequitazine.
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WO/2008/096870A1 |
[PROBLEMS] To provide a compound which has an antagonistic activity on a muscarinic M3 receptor and is therefore useful as an active ingredient of a prophylactic and/or therapeutic agent for an inflammatory disease such as chronic obstru...
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WO/2008/077357A2 |
A method of preparing (lS)-(3R)-l-azabicyclo[2.2.2]oct-3-yl 3,4-dihydro-l-phenyl-2(lH)- isoquinoline carboxylate (solifenacin) or its pharmaceutically acceptable salts with high optic purity, wherein the crude solifenacin base is transfo...
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WO/2008/077089A1 |
The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof where R1, R2, X, and y are defined herein. Compounds of the present invention are useful as progesterone receptor modulators.
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WO/2008/075005A1 |
The invention provides compounds of formula (I) wherein R5 is a group of formula (II) or (III) and R1, R2, R3, R4, R6, a, b, Z, Y and X are as defined in the specification, a process for their preparation, pharmaceutical compositions con...
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WO/2008/062282A2 |
This invention provides improved methods for making solifenacin and pharmaceutically acceptable salts thereof. The instant methods are unexpectedly advantageous in their simplicity and efficiency.
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WO/2008/059245A1 |
The invention provides compounds of formula (I) wherein R4 is a group of formula (II) or (IIIa) or (IIIb) and R1, R2, R3, R5, a, b and X are as defined in the specification, a process for their preparation, pharmaceutical compositions co...
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WO/2008/056263A2 |
Measurements of the squalene content in oil-in-water emulsions can be used as a way of checking for problems during production. In particular, it has been found that a drop in squalene content can indicate that filtration problems occurr...
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WO/2008/051564A2 |
The present invention provides crystalline forms of Palonosetron hydrochloride, processes for their preparation and pharmaceutical compositions containing such crystalline forms of Palonosetron HCl.
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WO/2008/051539A2 |
The present invention provides processes for preparing Palonosetron salts, especially, the hydrochloride salt and intermediates used to prepare Palonosetron salts.
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WO/2008/025541A1 |
A novel polymorphic crystal form of (R)-3-(2-hydroxy-2,2-diphenyl-acetoxy)-1-(isoxazol-3- ylcarbamoyl-methyl)-1-azonia-bicyclo-[2.2.2]octane bromide, designated crystal form Talpha. Methods for preparing same and the use of the crystal f...
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WO/2008/021339A2 |
Compounds of the structure (I) are described, wherein R1-R6, R11, R12, m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a va...
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WO/2008/019057A2 |
Polymorphic forms of 1(S)- phenyl -1,2,3,4-tetrahydroisoquinoline have been prepared and characterized. These polymorphic forms are particularly useful for preparing solifenacin salts.
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WO/2008/019103A2 |
Polymorphic forms of solifenacin base have been prepared and characterized. These polymorphic forms are particularly useful for preparing solifenacin salts.
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WO/2008/019055A2 |
Optically pure 1(S)-phenyl-1,2,3,4-tetrahydroisoquinoline tartrate is prepared. The 1(S)-phenyl-1,2,3,4-tetrahydroisoquinoline tartrate is particularly useful for preparing solifenacin succinate.
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WO/2008/019372A2 |
Compounds of Formulae (I), (II) and (III): are disclosed as 5-HT3 inhibitors. The compounds are useful in treating CINV, IBS-D and other diseases and conditions.
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WO/2008/019363A2 |
A genus of 2-alkylbenzoxazole carboxamides are disclosed as 5-HT3 inhibitors. Those compounds are useful in treating CINV, IBS-D and other diseases and conditions.
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WO/2008/012290A2 |
Quinuclidine derivative of the general formula (I) in the form of single enantiomers or mixtures thereof are useful in the manufacture of a medicament for the prevention and therapy of respiratory diseases such as asthma, chronic obstruc...
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WO/2008/013851A2 |
Polymorphic forms of solifenacin have been prepared and characterized. These polymorphic forms are particularly useful in pharmaceutical compositions.
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WO/2008/013269A1 |
Disclosed is an isoquinuclidine derivative which enables to easily synthesize oseltamivir or an analogue thereof. Specifically disclosed is an isoquinuclidine derivative represented by the formula (1) below or a mirror image structure of...
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WO/2008/009397A1 |
This invention is directed to a process for manufacturing 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)
-1-azoniabicyclo[2.2.2]octane bromide by reacting 2-hydroxy-2,2-dithien-2-ylacetic acid 1-azabicyclo[2.2.2]oct-3(R)yl ...
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WO/2008/005910A2 |
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11...
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WO/2007/147374A2 |
A process for the preparation of (1 S)-QR)-I -azabicyclo[2.2.2.]oct-3-yl 3,4-dihydro-1-phenyl- 2(1H)-isoquinoline carboxylate by reacting (1S)-alkyl 1-phenyl-1, 2,3, 4-tetrahydro-2- isoquinoline carboxylate with 3-(R)-quinuclidol in an i...
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WO/2007/149929A1 |
The subject invention provides stereoisomeric compounds of formula (X): wherein the variables are as defined herein, and compositions for the safe and effective treatment of various gastrointestinal disorders including, but not limited t...
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WO/2007/141504A1 |
A series of 5,6-dihydro-1-benzothiophen-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accor...
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WO/2007/119463A1 |
A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof (I) wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen...
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WO/2007/110637A1 |
Method for extracting a target alkaloid from a mixture of species, typically from plant matter, using an ionic liquid as an extracting solvent. The ionic liquid may in particular be an alkanolyl-, alkoxyalkyl- or aminoalkyl-substituted a...
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WO/2007/105049A1 |
Dibenzyl amine compounds and derivatives, of Formula (I), pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to l...
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WO/2007/100851A1 |
The invention provides a compound of formula (I) wherein R1-R6, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the ad...
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WO/2007/097276A1 |
[PROBLEMS] To provide a compound which can be used for the prevention and/or treatment of a disease associated with a 5-HT2B receptor or a 5-HT7 receptor, particularly for the treatment of irritable bowel syndrome (IBS). [MEANS FOR SOLVI...
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WO/2007/097197A1 |
[PROBLEMS] To provide a compound which can be used for the prevention and/or treatment of a disease associated with a 5-HT2B receptor or a 5-HT7 receptor, particularly for the treatment of irritable bowel syndrome (IBS). [MEANS FOR SOLVI...
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WO/2007/093366A1 |
The invention relates to aminoalcohol-substituted aryldihydroisoquinolinones and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least ...
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WO/2007/093602A1 |
This invention relates to novel enantiopure azabicyclo pyridazinyloxy derivatives of formula (I), which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporte...
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WO/2007/076116A2 |
Provided are new intermediates of solifenacin and methods for their preparation, as well as methods of preparing solifenacin and solifenacin succinate.
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WO/2007/066088A2 |
The present invention relates to a process for preparing a coupling product using α-lithio-quinuclidine N-oxide or a functionalised derivative or equivalent thereof.
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