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WO/2001/034566A2 |
This invention relates to the compound of Formula (I) or a pharmaceutically acceptable salt, hydrate or solvate thereof, which is an inhibitor of cysteine proteases, particularly cathepsin K, and is useful in the treatment of diseases in...
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WO/2001/027122A1 |
The invention relates to a method for the production of a pre-cursor of a radiodiagnostic agent, which comprises alkylation of an enolate of a chiral glycine auxiliary by means of a compound of formula (I); where OR is in either the meta...
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WO/2001/012575A1 |
The present invention relates to chemical synthesis of radiolabelled perfluorinated bioactive compounds. More particularly, the present invention relates to radiolabelled compounds to be used as indicators for tissue hypoxia. More partic...
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WO/2001/009146A1 |
A method of making a bisphosphonate RC(OH)(PO.]OH]¿2?)¿2? comprises reacting a tris(silyl)phosphite with an activated carbonyl compound and hydrolysing the resulting intermediate. Preferably the tris(silyl)phosphite is labelled with ?3...
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WO/2001/009095A1 |
A compound of formula (I) wherein R¿2? is arylene or heterocyclene; or R and R¿2? together with the nitrogen atom to which they are attached form non-aromatic heterocyclene; and the other residues have various meanings, useful as pharm...
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WO/2000/078362A2 |
The invention relates to a stable radioactive nanoparticle and to a method for the production thereof, whereby a nanoparticle is reacted with a radioactively marked molecule, especially in an aqueous medium, and covalent binding or the r...
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WO/2000/063216A1 |
Sulfur heteroatom substitution at the C4 position of ?18¿F-labeled fatty acids yields a tracer that is retained in proportion to the beta-oxidation rates in mammalian tissue, particularly hypoxic myocardium. Most preferably, the inventi...
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WO/2000/061525A1 |
Site-specific isotopically-labeled valine, leucine, and isoleucine and biosynthetic precursors for these amino acids are provided. The amino acids are labeled with ?13¿C or ?14¿C at the methyl group carbon atom(s) most remote from the ...
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WO/2000/059896A1 |
The present invention provides an $g(a)-particle-emitting radioisotope chelation complex comprising ?225¿Actinium (?225¿Ac) and 1,4,7,10,13,16-hexaazacyclohexadecane-N,N',N'',N''',N'''',N'
''''-hexaacetic acid (HEHA) (?225¿Ac-HEHA). A...
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WO/2000/058504A1 |
The present invention relates to a method for determining the enantioselectivity of kinetic racemate resolutions and of asymmetrical reactions of prochiral compounds carrying enantiotopic groups. According to the inventive method, isotop...
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WO/2000/057887A1 |
The present invention is directed to salt-free and essentially salt-free $i(p)-boronophenylalanine-carbohydrate or $i(p)-boronophenylalanine-polyol complexes, as well as methods for making such compounds. In addition, the present inventi...
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WO/2000/053235A2 |
A method for the preparation of radio labelled acrylic acid monomer including the steps of adding at least one radio labelled compound selected from the group consisting of malonic acid, malonic ester and malononitrile to paraformaldehyd...
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WO/2000/052031A2 |
Methods and kits for radiolabeling proteins and peptides with radiolytic isotopes, particularly yttrium-90, are disclosed, whereby sufficient purity, specific activity and binding affinity are achieved such that the radiolabeled protein ...
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WO/2000/044747A1 |
Biologically active derivatives of the tropane ring system are provided having formula (1) wherein R¿1? is selected from the group consisting of hydrogen and C¿1? to C¿8? alykl; R¿2? is selected from the group consisting of hydrogen,...
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WO/2000/043004A1 |
1,4,8,11-Tetraazacyclotetradecane which is chemically linked to from one to four nitroimidazol groups provides an effective radiodiagnostic agent for determining tissue hypoxia and radioresistance of tumor tissue.
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WO1999063547A9 |
Apparatus for the preparation of radioactive solutions includes a plastic housing that pivotally mounts a reagent support adapted to receive a plurality of radiation-shielded vials with the option of being pivotable to allow agitation or...
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WO/2000/018403A1 |
The present invention is directed to radiolabeled neurokinin-1 receptor antagonists which are useful for the labeling and diagnostic imaging of neurokinin-1 receptors in mammals.
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WO/1999/064389A1 |
This invention relates to anandamide transport inhibitors and their use as analgesic.
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WO/1999/060018A1 |
Synthetic analogues of lysine and glutamine are provided which function as substrates for the fibrin-stabilising enzyme Factor XIIIa even when labelled with a detectable moiety. The use of suitable protecting groups provides compounds wh...
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WO/1999/059642A1 |
Drugs containing as the active ingredient compounds having a radioactive element and an organic substituent carrying an unpaired electron in a single molecule, for example, labeled nitroxyl compounds represented by general formula (I) wh...
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WO/1999/056791A1 |
A radiolabeled tris(2-mercaptobenzyl)amine complex is provided. Complexes containing analogs of the tris(2-mercaptobenzyl)amine ligand are also described. The complex is useful for diagnostic or therapeutic applications which involve loc...
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WO/1999/051560A1 |
The present invention relates to a compound of the general formula (I) which is a non-hydrolysable analogue of endogenous cannabinoids, which are found to be more potent therapeutic agents as they are more stable, for example, to hydroly...
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WO/1999/044970A1 |
The invention relates to a method for producing [?15¿O] butanol. The invention also relates to a device for implementing said method. According to the inventive method for producing [?15¿O] butanol, a column containing an adsorbent is ...
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WO/1999/024080A1 |
The invention provides a method of magnetic resonance investigation of a sample, said method comprising: (i) reacting para-hydrogen enriched hydrogen with a hydrogenatable MR imaging agent precursor containing a non-hydrogen non-zero nuc...
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WO/1999/018053A1 |
According to a first aspect of the invention, a process is disclosed for the preparation of radiolabelled haloaromatic compounds. According to a second aspect of the invention, intermediate precursor insoluble polymer compounds used in t...
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WO/1999/018120A1 |
Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporins and cyclosporine derivatives. The cyclosporine derivatives of the present inventi...
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WO/1999/016757A1 |
Novel compounds suitable as contrasting agents, in particular for infarct and necrosis imaging, are disclosed, as well as processes for preparing the same and pharmaceuticals containing these compounds.
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WO1998055153A9 |
The present invention relates to non-steroidal radiolabeled androgen receptor ligands and their use in methods of imaging the prostate.
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WO/1999/013920A2 |
The invention relates to a method for treating proliferative diseases by therapy, characterised in that an application catheter is first placed at the site of the lesion and a radioactive substance is applied locally. The catheter is the...
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WO/1999/012893A1 |
Diamine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity for imaging the dopamine neurons are provided. The diamine compounds or serotonin are characterized by formula (I), wh...
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WO/1999/011589A1 |
This invention is concerned with determining the three-dimensional structure of biological macromolecules such as proteins. In particular, it is concerned with methods for rapidly determining protein structure by NMR, by providing method...
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WO/1999/011590A1 |
Thiol-containing peptides can be radiolabeled with fluorine-18 (F-18) by reacting a peptide comprising a free thiol group with an F-18-bound labelling reagent which also has a group that is reactive with thiols. The resulting F-18-labele...
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WO/1999/000386A1 |
Described herein are D4 receptor-selective compounds of formula (I) wherein Z is selected from N and C(R?5¿); R?1¿ is selected from H and an acid labile protecting group; R?2¿, R?3¿, R?4¿ and R?5¿ are independently selected from H,...
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WO/1998/057909A1 |
The present invention is related to a process for producing radioiodinated neuroreceptor agents with improved yields. In said process the trialkyltin group of the precursor of the neuroreceptor agent is replaced by radioiodine in the pre...
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WO/1998/056428A1 |
Radioactive arsenic (?72�As) labelled tissue specific ligands are prepared and used in the medical imaging of malignant breast or prostate tumors.
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WO/1998/048848A1 |
The invention relates to a method of preparing a compound of the general formula (I): $i(fac)-[M(CO)�3?(OH�2?)�3?]?+� wherein M is Mn, ?99m�Tc, ?186�Re or ?188�Re, by reacting a metal in the permetallate form with carbon mo...
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WO/1998/049196A1 |
This invention relates to calcitonin receptor binding reagents comprising compounds which are covalently linked to a radiometal chelator. The invention is embodied as calcitonin receptor binding peptide derivatives and analogues of calci...
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WO/1998/047969A1 |
Amyloid binding compounds which are non-azo derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain $i(in vivo) and to diagnose other pathological conditions cha...
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WO/1998/045263A1 |
The invention provides a compound of formula (I), wherein R?1�, R?2�, R?3�, and Y have any of the meanings defined in the specification; as well as a pharmaceutical composition comprising a compound of formula (I); intermediates an...
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WO/1998/034893A1 |
A novel process for producing alcohols, characterized by reacting an organic halide represented by the formula R-X (wherein R means an organic residue and X means a halogen atom) with oxygen molecules in the presence of an organotin comp...
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WO/1998/027036A1 |
Liquid-crystal compounds represented by general formula (1) and a liquid-crystal composition containing any of the compounds, wherein R?1� represents C�1-15? alkyl; rings A?1�, A?2�, and A?3� each independently represents trans...
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WO/1998/024480A1 |
Improved radioiodinated phospholipid ether analogs are described which demonstrate significant tumor avidity and longer plasma half-life than shorter-chain analogs, providing superior imaging and visualization of neoplastic lesions and t...
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WO/1998/018499A1 |
Process for the preparation of radiohalogenated radiopharmaceuticals by an electrophillic substitution, preferably halogenodestannylation reactions, by the reaction of an organometallic substituted precursors, preferably a trialkyl tin s...
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WO/1998/014436A1 |
The present invention relates to benzoxazinones of formula I, or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical comp...
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WO/1998/004906A1 |
The 13C-labeled compounds chloroacetic acid (CA), chloroacetamide (CAM), and chloroacetonitrile (CCN), have been synthesized, and provide the side reactivity probes (SRP) of the present disclosure. The reactivity of diverse environmental...
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WO/1997/046558A1 |
Herein described are radiolabelled compounds and their precursors useful to image D4 receptors in vivo, of formula (I) wherein R is selected from iodo, tri(loweralkyl)tin and a radioisotopically labelled iodide and R1 is selected from H ...
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WO/1997/043271A1 |
The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is O or S; n is 2, 3, 4 or 5; R1 is hydrogen, C1-6a...
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WO/1997/041856A1 |
Novel organometallic compounds for binding amyloid are described. Methods using such compounds for determining by imaging the localization or quantification of amyloid fibrils in a mammal, for diagnosing the degree of progression of Alzh...
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WO/1997/042203A1 |
A method for synthesising compounds labelled with any isotopic element is disclosed. The method comprises the steps of preparing the labelling agent, labelling a precursor in the form of a protected substrate, pre-purifying and deprotect...
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WO/1997/040010A1 |
Halogenated naphthyl methoxy piperidines having a strong affinity for the serotonin transporter are disclosed. Those compounds can be labeled with positron-emitting and/or gamma emitting halogen isotopes by a late step synthesis that max...
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