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WO/2005/037853A2 |
Protein structural determination using NMR techniques is improved through use of proteins in which one or more amino acids in the peptidic sequence are isotopically enriched in the sidechain with 2H and are isotopically enriched on the b...
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WO/2005/037737A1 |
Disclosed is a method for producing [18F] fluoride-marked aromatic L-amino acids, according to which the marking reaction takes place on an L-enantiomeric aromatic amino acid that is provided with protective groups. Also disclosed is a m...
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WO/2005/030676A1 |
This invention pertains to methods of [11C]-radiolabelling 'phenothiazine' and 'phenothiazine-like' compounds, which have a pendant group (which is a primary amino group; a cationic primary imino group; a secondary amino group; a cationi...
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WO/2005/030677A1 |
A process for producing a radioactive fluorine compound which comprises a step in which [18O] water containing [18F] fluoride ions is introduced into a column packed with an ion-exchange resin to collect the [18F] fluoride ions and a ste...
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WO/2005/014479A2 |
A novel process for preparing radiolabelled compounds by incorporation of radioactive carbonyl groups into precursors, which are then used to make the radiolabelled compounds. These radiolabelled compounds have a number of uses including...
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WO/2004/108636A2 |
A radioisotope labeled reagent includes a compound having the general formula (I) where a in each occurrence independently is a carbon mass number between 11 and 14 inclusive, b in each occurrence independently is a hydrogen mass number ...
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WO/2004/098650A2 |
The present invention relates to compositions and methods for preparing radiopharmaceutical compounds in high chemical-purity and isotopic-purity. The present invention provides polymer-bound precursors to radiopharmaceutical compounds t...
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WO/2004/100490A2 |
The invention relates to a device and a method for the fluorination of nucleophiles of a substance, especially for the synthesis of an 18F-marked substance for examination with the aid of a positron emission tomograph. The device compris...
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WO/2004/080492A1 |
The invention relates to conjugates of formula (V) or (VI): wherein X is -CO-NH-, -NH-, -O-, -NHCONH-, or -NHCSNH-; their use as radiopharmaceuticals, processes for their preparation, and synthetic intermediates used in such processes.
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WO/2004/069773A1 |
The present invention encompasses a compound of Formula (I) useful as caspase active site probes. These probes can be used to determine whether a caspase has been activated, in cells or in tissues of animal models of various pathologies....
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WO/2004/060831A1 |
A method of deuterizing a compound represented by the general formula [1]: R1-X-R2 [1] (wherein R1 represents alkyl, etc.; R2 represents alkyl, hydroxy, etc.; and X represents carbonyl or hydroxymethylene), which comprises reacting the c...
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WO/2004/056725A1 |
A process for the production of an 18F-labelled tracer which comprises treatment of a solid support-bound precursor of formula (I): SOLID SUPPORT-LINKER-SO2-O -TRACER (I) with 18F- to produce the labelled tracer of formula (II).
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WO/2004/056724A1 |
The invention relates to deuterated catecholamine derivatives and medicaments comprising said compounds. The invention further relates to the use of deuterated catecholamine derivatives, the pharmacologically-acceptable salts thereof and...
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WO/2004/046066A1 |
A method for deuteration or tritiation of a heterocyclic ring, characterized in that it comprises allowing a heterocyclic compound to be present under a sealing and refluxing condition in a deuterated or tritiated solvent in the presence...
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WO/2004/043496A1 |
The invention relates to fluorquinolines labelled with fluorine-18 of a general formula (I), wherein R1 is selected from a group consisting of substituted or non-substituted alkyl, cycloalkyl and aryl, and R2 selected from a group consis...
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WO/2004/029006A2 |
The invention provides a process for preparation of a fluorohaloalkane, preferably an [18F]fluorohaloalkane of formula (I) wherein X is halo and n is an integer of from 1 to 6; which comprises: reaction of the corresponding organosilicon...
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WO2002102743A9 |
The invention relates to deuterated N-substituted alpha , alpha -diphenyl- alpha -alkoxy acetic acid amino alkyl esters and to their physiologically compatible salts. The invention also relates to the use of deuterated N-substituted alph...
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WO/2004/010846A2 |
Aminophosphinic acid derivatives were synthesized as potential inhibitors of renal dipeptidase, an enzyme overexpressed in benign and malignant colon tumors. Several compounds showed potent enzyme-inhibitory activity. These compounds can...
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WO/2004/011400A1 |
A method of deuterating a compound having an aromatic ring in the presence of an activated catalyst. In particular, a method of deuterating a compound having an aromatic ring characterized in that a compound having an aromatic ring is re...
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WO/2003/104430A2 |
This invention provides an NMR method for obtaining both entropic and enthalpic data on proteins and protein/ligand complexes which can be used to obtain accurate structural and dynamic data of proteins and protein complexes having a wid...
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WO/2003/104166A1 |
The invention relates to a process for deuteration of inert alkanes with activated palladium−carbon, specifically, a process for deuterating a compound having either a methyl group or an alkylene group having two or more carbon atoms i...
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WO/2003/099746A1 |
The invention relates to a method for the production of 18F-fluorinated ?-amino acids and 18F-fluorinated &agr -amino acid derivatives, comprising the following steps: (a) reaction of a 18F-fluorinated compound of formula I, wherein R1 a...
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WO/2003/089438A1 |
The present invention provides isotopically labeled oxazinocarbazole derivatives having a ring connecting position 8 (C-8) and position 9 (N-9), and more specifically, provides compounds of formula (I) wherein R1, R2, R3 and R4 are descr...
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WO/2003/080544A1 |
The present invention relates to methods and reagents for [18F]-fluorination, particularly of peptides. The resultant 18F-labelled compounds are useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET). ...
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WO/2003/078358A2 |
This invention relates to the miniaturisation of radiosyntheses onto microfabricateddevices, and in particular to use of microfabricated devices for radiosynthesis, isolation, and analysis of radiotracers for use in Positron Emission Tom...
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WO2002070020A9 |
One aspect of the present invention relates to polymyer precusors Poly-L-R-Y where Poly=poly, L = -Sn(R3)2- or -SN(R3)2-Sn(R3)2-, R= aryl or heteroaryl, Y = hydrogen, alkyl, alkoxyl, carbonyl, formyl, amido, amino, alkylamino, dialkylami...
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WO/2003/065882A2 |
The invention provides a series of lipophilic phosphonium cations (PhCs) labeled with 18F for non-invasive assessment of &Dgr &PSgr m, lipophilic ammonium cation analogs of the PhCs, and methods of using same for imaging and detection of...
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WO/2003/064678A2 |
A system for radiolabeling compounds with a labeling module, which is fluidly connectable to a solvent delivery module, an HPLC pump and an HPLC column. The labeling module includes a loop and valves having different orientations to prov...
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WO/2003/053910A1 |
It is intended to provide a stable isotope-labeled amino acid which is at least one of amino acids constituting protein, characterized by having at least one of the following labeling patterns: (a) in one or more methylene groups, methyl...
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WO/2003/024940A1 |
The invention concerns a ligand comprising (I) wherein n is an integer from 1 to 5 Y is CO2H or PO3H2T represents −X or −phenyl−X, wherein X represents NO2, NH2, NCS, NHCOCH2−Z, NHCO−W−COCNHS, −NH−Q, −NHCS−Q, −NHCOC...
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WO/2003/008394A1 |
The present invention relates to novel bifunctional chelates that are based on asymmetrical cyclen derivatives. The chelates contain either three acetates and one methylphosphonic arm or three acetates and one methylphosphonic arm enabli...
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WO2001005805A9 |
The invention relates to novel C-19-halogen-substituted steroids of the androst-9(11)-ene series, i.e. 17 beta -hydroxy-19-halogen-androsta-4,9(11)-diene-3-one of general formula (I) and to methods for the production thereof. The inventi...
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WO/2003/002157A1 |
The present invention relates to novel solid-phase processes for the production of radiolabelled tracers, in particular for the production of ?18¿F-labelled compounds which may be suitable for use as Positron Emission Tomography (PET) r...
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WO/2003/002489A2 |
The invention relates to compounds of formula (I); wherein R?1¿ and R?2¿ independently selected from C¿1-6? alkyl; P?1¿, P?2¿, P?3¿, and P?4¿ are each independently hydrogen or a protecting group; and their use in the preparation ...
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WO/2003/000698A1 |
L-threo-$g(b)-benzyloxyaspartate derivatives having a substituent on the benzene ring, represented by the following formula (1): wherein R is hydrogen, a linear or branched lower aliphatic acyl group with the acyl portion optionally subs...
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WO/2002/102711A1 |
A new method for the production and use of a carbon-isotope monoxide enriched gas-mixture from an initial carbon-isotope dioxide gas mixture is presented. The method comprises the steps of providing carbon-isotope dioxide in a suitable c...
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WO/2002/102765A2 |
The compound O-(2-[?18¿F]fluoroethyl)-L-tyrosine has proven to be particularly suitable for positron emission tomography and has already been tested in clinical practice. Until now, the compound has been produced according to a relative...
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WO/2002/090298A2 |
The invention relates to a method for the synthesis of ?18¿F marked compounds which are low in carriers. Nucleophilic phase-transfer catalyzed ?18¿F- fluoridation was previously the only way to produce ?18¿F marked radiotracers having...
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WO/2002/088100A2 |
The invention relates to deuterated 3-piperidinopropiophenone and their physiologically acceptable salts. The invention also relates to the use of deuterated 3-piperidinopropiophenone in the treatment of muscular diseases and in the prod...
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WO/2002/085418A2 |
Improved sst-receptor binding peptidic ligands for diagnostic and therapeutic applications in nuclear medicine are provided. The improved ligands contain either natural or unnatural amino acids or peptidomimetic structures that are modif...
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WO/2002/044175A2 |
The present invention provides a compound for chelating a metal or a metal complex, characterized in that it consists of a bis-dithiocarbamate structure (F) having the formula below: (formule chimique ô insérer ici)in which n and m are...
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WO/2002/036581A1 |
This invention is directed to the use of radiopharmaceuticals of formula (I) in diagnosing Alzheimer's disease. In particular the radiopharmaceuticals of the invention are able to pass through the blood-brain barrier and bind to the CCR1...
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WO/2002/030937A2 |
This invention relates to resiniferatoxin derivatives useful in a vanilloid receptor binding assay and methods for production thereof.
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WO/2002/020434A1 |
Fluoroalkanes such as fluoromethane labeled with ?17¿F are produced by contracting ?17¿F labeled F¿2? with alkanes, preferably methane, substituted or unsubstituted alkenes, or substituted or unsubsituted alkynes in the presence of a ...
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WO/2002/000603A1 |
The use of pamoic acid or of one of its derivatives is described with general formula (I), in which groups R1 and R5 are as indicated in the description, or of one of their pharmaceutically acceptable salts, for the preparation of a medi...
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WO/2001/092188A1 |
A method for preparing a tritium-labeled compound, characterized in that it comprises reacting an organic compound with a hydride reagent in the presence of a solvent and a catalyst; and a tritium-labeled compound prepared by the method....
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WO/2001/077122A1 |
This invention relates to novel highly functionalized phosphine ligands as ancillary ligands in radiopharmaceuticals. Also, this invention provides radiopharmaceuticals comprised of highly functionalized phosphine ligated ?99m¿Tc labele...
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WO/2001/077102A1 |
This invention relates to new macrocyclic chelants and metal chelates thereof, methods of preparing the chelants and metal chelates, and pharmaceutical compositions comprising the macrocyclic chelants and metal chelates. This invention r...
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WO/2001/070755A1 |
There is provided a method of synthesis of a radiolabelled platinum chemotherapeutic agent comprising the steps of: converting a metal halide to a radiolabelled platinum halide wherein the radiolabel is a radioisotope of Pt; and synthesi...
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WO2000071506A9 |
Compounds of formula (I), wherein R<1> and R<2> are substituents on the A rings and are, independently, -SO2NR<7>2, -C(O)NR<7>2, -NR<7>SO2R<7>, -NR<7>C(O)R<7>, -SO2OR<7>, -C(O)OR<7>, -OSO2R<7>, or -OC(O)R<7>, R<3> and R<4> are, independe...
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