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WO/2003/033480A1 |
The invention thus provides compounds of formula (I), a salt, or solvate thereof.
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WO/2003/029252A1 |
The invention provides compounds of Formula (I), wherein Azabicyclo is formulas (II-VII), W is formulas (VIII-X). These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. ...
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WO/2003/024949A1 |
The invention relates to the use of compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of DNA-PK, wherein R?1¿ and R?2Â...
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WO/2003/024926A2 |
The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or bl...
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WO/2003/022790A2 |
There are described biphenylene compounds of formula (I) wherein R¿1? is a C¿1?-C¿18?alkyl, C¿2?-C¿18?alkenyl, C¿6?-C¿10?aryl or C¿6?-C¿10?aryl or C¿6?-C¿10?heteroaryl radical each unsubstituted or mono- or poly-substituted by...
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WO/2003/020029A1 |
Methods for treating CMV and CMV-related diseases are provided that use compounds having formula (II) wherein the subscripts m and n are each independently integers from 1 to 2; and the R groups are as defined in the specification.
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WO/2003/018549A2 |
Methods for treating CMV or a CMV-related disease are provided that use compounds having the formula (I) wherein Ar is a substituted or unsubstituted 5-14 membered heteroaryl group having from 1 to 5 heteroatoms as ring members; R?1¿ is...
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WO/2003/015517A1 |
The present invention provides compositions and methods for controlling an helminth or arthropod pest. In a preferred embodiment of the invention provided herein, the compositions comprise compounds which alter the 5-HT¿3? receptor of t...
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WO/2003/013528A1 |
GnRH receptor antagonists of formula (I) are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. Also disclosed are compositions containing a compound of this invention in c...
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WO/2003/013531A1 |
Novel compounds of formula (I), wherein D, W, X, Y, T and R?1¿ have the meaning as cited in Claim 1, are inhibitors of coagulation factor Xa and can be used in the prophylaxis and/or therapy of thromboembolic diseases and in the treatme...
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WO/2003/011799A1 |
One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing cataly...
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WO/2003/009848A1 |
The present invention relates to a method of treating abnormal anxiety behavior in companion animals comprising administering to a companion animal in need thereof a therapeutically effective amount of an NK-1 receptor antagonist.
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WO/2003/007949A1 |
Certain novel bridged piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control...
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WO/2003/006371A1 |
A method is provided for enhancing the solubility of an ionizable compound in a lipophilic medium by admixing the compound with an effective solubility-enhancing amount of an N,N-dinitramide salt. The ionizable compound, upon ionization,...
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WO/2003/006019A1 |
A capsaicin−sensitive sensory nerve depressant which contains quinuclidine−3'−yl 1−phenyl−1,2,3,4−tetrahydroisoquinoline−2−carboxyl
ate or a salt thereof as the active ingredient. It is a remedy for a urologic disease sel...
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WO/2003/004493A1 |
The present invention relates to novel compounds that are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compo...
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WO/2003/000682A1 |
Compounds of formula (I) and pharmaceutically acceptable salts thereof are useful in the treatment of cytokine mediated diseases such as arthritis and in the treatment and/or prevention of protozoal diseases such as coccidiosis.
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WO/2002/102766A2 |
A new and more efficient synthesis of combretastatin A-3 (2a) was completed (8.4% overall yield) starting from methyl gallate and isovanillin with aldehyde 5 and phosphonium salt 8 as key intermediates. Conversion of combretastatin A-3 (...
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WO/2002/100858A2 |
The invention provides compounds of Formula (I): wherein W?0¿ is a bicyclic moiety and is (I). These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are use...
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WO/2002/096855A2 |
In a preferred embodiment, the subject invention concerns novel analogs of oxybutynin. The present invention also concerns methods for synthesizing the oxybutynin analogs of the present invention. The invention also pertains to methods f...
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WO/2002/094790A1 |
A fused heterocyclic compound represented by the general formula (I): (I) (wherein the symbols are the same as defined in the description), optically active isomer thereof, pharmaceutically acceptable salt of any of these, hydrate of any...
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WO/2002/088114A2 |
The present invention relates to aryl olefinic azacyclic compounds and aryl acetylenic azacyclic compounds, including pyridyl olefinic cycloalkylamines and pyridyl acetylenic cycloalkylamines. The present invention also relates to prodru...
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WO/2002/085848A2 |
A new and efficient synthesis of the (+)-pancratistatin phosphate prodrug 2a has been accomplished. Selective protection (tetraacetate 4) of (+)-pancratistatin (1a) was followed by phosphorylation (to 5) with dibenzyl chlorophosphite (pr...
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WO/2002/085901A1 |
The invention provides compounds of Formula (I): (F) Formula (I) wherein m?1¿ is 0 or 1; m?2¿ is 1 or 2; R¿1? is-H, alkyl, halogenated alkyl, substituted alkyl, cycloakyl, or phenyl; R¿2? is -H, alkyl, halogenated alkyl, substituted ...
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WO/2002/083670A1 |
A novel asymmetric phase transfer catalyst and a method for producing alpha-amino acids using the same are disclosed. Using the catalyst in the production of alpha-amino acids, optically active alpha-amino acids can easily be produced wi...
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WO/2002/081420A1 |
A compound which has cytokine production inhibitory activity and is useful for the treatment of diseases in which cytokine participates. The compound is represented by the following general formula (I) [wherein A represents an optionally...
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WO/2002/076973A1 |
A compound having excellent squalene synthetase inhibitory activity. It is a compound (I) represented by the following general formula, a salt thereof, or a hydrate of either. (I) In the formula, R?1¿ means optionally substituted vinyl ...
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WO/2002/076981A1 |
An isoquinuclidine derivative represented by the following general formula (I): (I) [wherein A¿1? is methylene or carbonyl; R¿1? is hydrogen or methyl; R¿2? is -(CH¿2?)¿n?-A¿2?-Ph (n is an integer of 0 to 3 and A¿2? is a single bo...
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WO/2002/076975A1 |
The invention concerns cancer therapy and novel anti-cancer agents having a very particular mechanism of activity. The invention also concerns novel chemical compounds and their therapeutic use in humans.
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WO2001023385A9 |
The present invention provides compounds, specifically novel tropane analogs, capable of acting as inhibitors of reuptake of monoamines. In preferred embodiments, these compositions are selective inhibitors of serotonin and/or norepineph...
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WO2002018334B1 |
The invention provides sodium channel modulating compounds of formula (I) wherein X, Y, Q, R<1>, w, and R<2> have any of the values defined in the specification, and salts thereof, which are useful for treating diseases or conditions ass...
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WO/2002/070479A1 |
The invention provides a compound of formula (1): wherein R?1¿, R?2¿, R?3¿, R?3a¿, R?4¿, R?4a¿, R?5¿, and R?6¿ are as defined; or a pharmaceutically acceptable salt thereof or a solvate thereof; compositions containing these comp...
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WO/2002/070653A2 |
Novel PDF inhibitors and novel methods for their use are provided.
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WO/2002/070494A1 |
Aryl- and heteroaryl substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, f...
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WO/2002/064124A2 |
The invention relates to a novel medicament formulation containing the muscarinic agonist talsaclidine and to a method for the production thereof.
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WO/2002/057254A1 |
Compositions for prevention or treatment of hepatopathy, containing as the active ingredient compounds represented by the general formula (I), or pharmaceutically acceptable salts, ester, or other derivatives thereof: (I) wherein A is a ...
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WO/2002/055515A1 |
The invention relates to cancer therapy and concerns novel anti-cancer agents having a very particular action mechanism. The invention also concerns novel chemical compounds and their therapeutic use in humans.
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WO/2002/053564A2 |
A compound of formula (I), wherein B is a phenyl ring, a 5 to 10 membered heteroaromatic group containing one or more heteroatoms, or a naphthalenyl, 5, 6, 7, 8- tetrahydronaphthalenyl, benzo[1,3]dioxolyl, or biphenyl group; A represents...
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WO/2002/051841A1 |
A compound which is a carbamate of formula (I), wherein R1 represents (a), (b), (c), (d), (e), (f), (g), (h) or (i); R2 represents a benzyl, phenethyl, furan-2-ylmethyl, furan-3-ylmethyl, thiophen-2-ylmethyl or thiophen-3-ylmethyl group ...
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WO/2002/048150A2 |
The present invention provides compounds and methods of administering compounds to a subject taht can reduce βAPP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds a...
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WO1999059957A9 |
Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparatio...
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WO/2002/044144A2 |
Radiolabeled fluorinated compounds useful for imaging in the diagnosis of Parkinson's Disease are disclosed. Methods and kits for their synthesis are also disclosed.
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WO/2002/044176A1 |
This invention relates to novel 3-substituted quinuclidine derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacol...
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WO/2002/040058A2 |
Isolatable, hydroxyapatite-targeting polymeric structures, and biologically active conjugates thereof, are provided. The polymeric structure includes a linear or branched water-soluble and non-peptidic polymer backbone, such as a PEG bac...
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WO/2002/038528A1 |
Pleuromutilin compounds of the following formulae: (IA) and (IB) are of use in anti-bacterial therapy.
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WO/2002/032863A1 |
The invention provides 2, 3-, 4- or 5-substituted-N1-(benzensulfonyl)indoles compounds of the general formula (I) in which Ar, R?2¿, R?3¿, R?4¿ and R?5¿ are as defined in the specification. The said compounds have affinity for the 5-...
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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/2002/028837A1 |
The present invention concerns compounds of formula. In a preferable embodiment, X represents O; R?1¿ represents C¿1-6?alkyl; cycloC¿3-12?alkyl or (cycloC¿3-12?alkyl)C¿1-6?alkyl, wherein one or more hydrogen atoms in a C¿1-6?alkyl-...
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WO/2002/028847A1 |
The invention provides 1,3,4-thiadiazoles and 1,3,4-oxadiazoles having the following formula (I):in which, Y is S or O,R1 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl or a polycyclic group, opt...
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WO/2002/024692A1 |
The present invention provides novel compounds, corresponding to formulae I and II, respectively, which are able to reactivate the apoptosis-inducing function of mutant p53 proteins. This reactivation is provided by restoration of sequen...
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