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WO/2006/014706A2 |
The present invention provides novel derivatives of MTX. The novel derivatives have increased selectivity, inhibit the activity of Her2, EGFR, or B-Raf to a greater degree than MTX, and display greater antiproliferative activity than MTX...
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WO/2006/008028A1 |
The invention relates to novel 6-formyltetrahydropteridines of general formula (I), where the groups R1 to R6 have the meanings given in the claims and the description and the isomers thereof, method for production of said 6-formyltetrah...
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WO/2006/005510A1 |
The invention relates to novel pyridodihydropyrazinones, a method for production and use thereof as medicaments. Said compounds correspond to general formula (I), where the groups L, R1, R2, R3, R4 and R5 have the meanings given in the c...
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WO/2006/002367A1 |
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activit...
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WO/2005/123736A1 |
The invention relates to the novel 2-benzylaminodihydropteridinones of general formula (I), wherein the groups R1 to R7, R10 and R11 are defined as in the claims and in the description, and to the isomers thereof. The invention also rela...
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WO/2005/095464A1 |
A hyaluronic acid/methotrexate compound useful as a therapeutic agent for joint diseases. The hyaluronic acid/methotrexate compound useful for the treatment of joint diseases comprises hyaluronic acid and methotrexate bonded to a hydroxy...
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WO/2005/092902A1 |
An efficient process for producing a folic acid derivative being suitable for formation of a conjugate of anticancer drug and folic acid. There is disclosed a process comprising the step of conducting a reaction between a 2-amino protect...
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WO/2005/085294A1 |
A hyaluronic acid/methotrexate compound useful as a therapeutic agent for joint diseases. The hyaluronic acid/methotrexate compound useful as a therapeutic agent for joint diseases comprises hyaluronic acid and methotrexate bonded to a c...
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WO/2005/080395A2 |
The inventive method for the production of crystalline (6RS)-N(5)-formyl-5,6,7,8-tetrahydrofolic acid or amorphic (6S)-N(5)-formyl-5,6,7,8-tetrahydrofolic acid is characterized in that an aqueous solution of (6RS)- or (6S)-calcium folina...
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WO/2005/068465A1 |
Disclosed are pteridine derivatives of formula (I): (I), wherein, for example, R1 and R2 are hydrogen, C1-C6 alkyl, carboxyl, formyl, C1-C6 hydroxyalkyl, C1-C6 carboxyalkyl, C1-C6 formyl alkyl, C1-C6 alkoxy, acyloxy, acyloxyalkyl wherein...
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WO/2005/065018A2 |
Crystal forms of (6R)-L-erythro-tetrahydrobiopterin dihydrochloride, hydrates and solvates and processes for their preparation are provided. These crystal forms are either intermediates for the preparation of stable polymorphic form B ...
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WO/2005/063752A1 |
The present invention relates to the area of NO synthase inhibition and, more particularly, relates to novel 4-amino-7,8-dihydropteridines, pharmaceutical compositions containing said compounds, and the use of said compounds in the treat...
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WO/2005/049614A2 |
Process for the preparation of tetrahydrobiopterin from neopterin and/or 6-substituted pterins with an improved yield and a high stereoselectivity. Also disclosed herein are novel individual intermediates prepared in the preparation of t...
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WO/2005/046588A2 |
Compounds, compositions and methods useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
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WO/2005/046698A1 |
This invention provides fused heterocyclic compounds, pharmaceutical compositions of the compounds, and methods of using the compounds for the treatment of, inter alia, IL-12 related disease and disorders.
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WO/2005/042498A2 |
Capsaicin receptor agonists are provided. Such compounds are ligands that may be used to modulate VRl activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to capsaicin receptor activation in...
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WO/2005/040163A1 |
The present invention relates to novel compounds of Formula (Ia) or (Ib), their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. Formula (Ia), or Formula (Ib) in the above formulae L represe...
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WO/2005/039587A1 |
This invention relates to a group of substituted pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydro-derivatives and enantiomers, possessing unexpectedly desirable pharmaceutical pr...
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WO/2005/032481A2 |
Quinazoline derivatives have the formula (I) or the pharmaceutically acceptable salts thereof; wherein each of Z5, Z6, Z7 and Z8 is N or CH and wherein one or two Z5, Z6, Z7 and Z8 are N and wherein two adjacent Z positions cannot be N; ...
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WO/2005/033115A1 |
There are disclosed novel compounds of formula (I) wherein A, R1, R2, R3 and X are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions...
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WO/2005/025574A2 |
This invention relates to the use of a group of pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydroderivatives and enantiomers, for the manufacture of a medicament for the preventio...
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WO/2005/021003A2 |
This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydro- derivatives and enantiomers, possessing unexpectedly de...
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WO2004112793B1 |
A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the structure IA...
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WO/2005/018531A2 |
The inventive pharmaceutical composition exhibits an inhibiting activity with respect to serine proteinase (Kaspaz) and comprises an active substance embodied in the form of a pharmaceutically acceptable quantity of an azo-heterocyclic c...
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WO/2005/014594A1 |
The invention relates to a process for the purification of riboflavin comprising the steps of (a) precipitating a first crystalline form of riboflavin, (b) isolating the first crystalline form of riboflavin, (c) transforming the first cr...
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WO/2004/104005A2 |
Novel poly-substituted pteridinediones (lumazines), and mono- or polysubstituted 2-thiolumazines, 4-thiolumazines or 2,4-dithiolumazines, having disclosed substituents in positions 1, 3, 6 and 7 of the pteridine ring, and pharmaceuticall...
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WO/2004/100960A2 |
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WO/2004/101554A1 |
The present invention relates to compounds of the formula (I) in which R0 ; R1 ; R2 ; R3 ; R4 ; R5 ; R6 ; R7 ; Q; V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active ...
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WO/2004/096287A2 |
The invention is related to phosphorus substituted IMPDH inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates u...
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WO/2004/096235A2 |
The invention is related to phosphorus substituted anti-cancer compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful...
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WO/2004/096236A2 |
The invention is related to phosphonate substituted compounds having immuno-modulatory activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes a...
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WO/2004/096286A2 |
The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermed...
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WO/2004/094427A1 |
The present invention relates to pharmaceutically active ornithine compounds, particularly to pharmaceutically acceptable ammonium salts of N&dgr -acyl derivatives of N&agr (4-amino-4-deoxypteroyl)-L-ornithine compounds; and methods of t...
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WO/2004/089925A1 |
The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.
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WO/2004/089889A2 |
The invention relates to an improved method for producing pure riboflavin (vitamin B2) of modification B/C in granular form. Also disclosed is pure riboflavin in granular form, said pure riboflavin being provided with a bulk density of 0...
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WO/2004/076454A1 |
The invention relates to novel dihydropteridinones of general formula (I), wherein rests L, R1-R5 have the significance indicated in claims and a specification, in the isomers thereof, in a method for producing and using said dihydropter...
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WO/2004/071463A2 |
Provided herein is are novel fluorine-substituted methotrexates and methods of using magnetic resonance spectroscopy of these novel compounds to determine the sensitivity of or resistance of a tumor to methotrexate. Such methods may be u...
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WO/2004/065378A1 |
The present invention provides substituted 2-aminopyridines of formula (I), wherein R1, A1, W, X, and Y are as defined in the specification, useful in treating cell proliferative disorders. The novel compounds of the present invention ar...
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WO/2004/045536A2 |
A method for modifying at least one non-ester-containing parent compound, and the compounds produced using such method, which compounds are deployed to temporarily incapacitate at least one subject are disclosed. The modified compounds a...
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WO/2004/045533A2 |
A method and compositions for treating persistent pulmonary hypertension in human newborns that deploys an intravenous infusion of a modified drug formed by adding one or more of a predetermined chemical arrangement to an efficacious par...
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WO/2004/043338A2 |
Compounds comprising flavin N-oxides for treatments of solid tumors, non-solid tumor masses, leukemias, and non-small cell lung cancers and for eradicating contaminants in blood products. Methods of treating patients having solid type ca...
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WO/2004/042002A2 |
The present invention pertains to compounds effective at modulating (inhibiting or enhancing) RNA interference in a cell or organism. Featured compounds are set forth and exemplified herein. Therapeutic methods and pharmaceutical composi...
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WO/2004/034972A2 |
Compounds, compositions and methods useful for treating cellular proliferative diseases and disorders, for example, by modulating the activity of KSP, are disclosed.
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WO/2004/031189A1 |
The present invention provides compounds of Formula (I): wherein the variables A, B, Ar, R1, R2, and R3 are as defined herein. The compounds of Formula (I) can function as corticotropin releasing factor (CRF) receptor antagonists and can...
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WO/2004/013142A1 |
Disclosed is a riboflavin derivative and its manufacture and uses. Oil suspended preparations constituted of the derivative have good stabilities and the effect will maintain for 3 months after intramuscular 150mg once. The invention com...
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WO/2004/011005A2 |
The present invention relates to pharmaceutical antimicrobial compositions and in particular to such compositions comprising 2,4-diamino-6-(hydroxymethyl) pteridine (DAP), 2,4-diaminopteroic acid (DAPA) and 2,4-diamino-N10-methylpteroic ...
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WO/2004/009036A2 |
Compounds, compositions and methods useful for treating cellular proliferative diseases and disorders, for example, by modulating the activity of KSP, are disclosed.
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WO/2004/005406A2 |
The present invention relates to charge transport compositions. The invention further relates to electronic devices in which there is at least one active layer comprising such charge transport compositions.
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WO/2004/006355A2 |
The present invention relates to charge transport compositions containing a quinazoline derivative of formula I, II or III . The invention further relates to electronic devices in which there is at least one active layer comprising such ...
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WO/2004/005288A2 |
The present invention relates to charge transport compositions comprising a compound of Formula (I). The invention further relates to electronic devices in which there is at least one active layer comprising such charge transport composi...
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