Abstract

The present invention relates to the production of activated biological molecules for use in profiling biological molecule interactions. The activated biological molecule may be a ubiquitin (Ub) and ubiquitin-like conjugation enzyme as well as other proteins with internal reactive cysteine residues.

IPC Classes  ?

• C12Q 1/48 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving transferase
• G01N 33/532 - Production of labelled immunochemicals
• C12Q 1/44 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving esterase

Abstract

The present invention relates to the discovery that salt inducible kinases (SIKs) suppress the formation of anti-inflammatory molecules such as IL-10, which are important for the resolution of inflammation and identifies SIK inhibitors that may be used to treat disorders associated with undesirable inflammation, such as inflammatory bowel disease and/or autoimmune disorders.

IPC Classes  ?

• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• C07D 239/48 - Two nitrogen atoms
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 487/04 - Ortho-condensed systems

Abstract

The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.

IPC Classes  ?

• A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
• A61K 31/37 - Coumarins, e.g. psoralen
• A61K 31/52 - Purines, e.g. adenine
• A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61K 31/428 - Thiazoles condensed with carbocyclic rings
• A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61K 31/665 - Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
• C07D 487/04 - Ortho-condensed systems
• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 311/18 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring substituted otherwise than in position 3 or 7
• C07D 311/16 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring substituted in position 7
• C07D 307/80 - Radicals substituted by oxygen atoms
• A61K 31/664 - Amides of phosphorus acids
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline

Abstract

The present invention relates to the production of activated biological molecules for use in profiling biological molecule interactions. The activated biological molecule may be a ubiquitin (Ub) and ubiquitin-like conjugation enzyme as well as other proteins with internal reactive cysteine residues.

IPC Classes  ?

• C12Q 1/48 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving transferase
• G01N 33/532 - Production of labelled immunochemicals
• C12Q 1/44 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving esterase

Abstract

An ultrasonically actuated medical implement is used in improving medical interventions and in certain instances to the generation of image data, in particular data acquired during a medical intervention or procedure. The medical implement employs a piezoelectric element which causes reciprocation between first and second mass assemblies in order to ultrasonically actuate a probe member and improve the visibility of the probe member to imaging methods. The invention also concerns the visibility of structures in target regions to be imaged and how this may be enhanced using the medical implement of the invention.

IPC Classes  ?

• A61B 17/34 - TrocarsPuncturing needles
• A61B 17/32 - Surgical cutting instruments
• A61B 8/08 - Clinical applications
• A61B 8/00 - Diagnosis using ultrasonic, sonic or infrasonic waves
• A61B 10/02 - Instruments for taking cell samples or for biopsy
• A61B 90/00 - Instruments, implements or accessories specially adapted for surgery or diagnosis and not covered by any of the groups , e.g. for luxation treatment or for protecting wound edges
• A61B 17/00 - Surgical instruments, devices or methods

Abstract

The present invention relates to the discovery that salt inducible kinases (SIKs) suppress the formation of anti-inflammatory molecules such as IL-10, which are important for the resolution of inflammation and identifies SIK inhibitors that may be used to treat disorders associated with undesirable inflammation, such as inflammatory bowel disease and/or autoimmune disorders.

IPC Classes  ?

• C07D 239/48 - Two nitrogen atoms
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 487/04 - Ortho-condensed systems

Abstract

The invention relates to improving medical interventions and in certain instances to the generation of image data, in particular data acquired during a medical intervention or procedure. The invention also concerns the visibility of structures in target regions to be imaged and how this may be enhanced.

IPC Classes  ?

• A61B 8/08 - Clinical applications
• A61B 10/02 - Instruments for taking cell samples or for biopsy
• A61B 17/34 - TrocarsPuncturing needles
• A61B 19/00 - Instruments, implements or accessories for surgery or diagnosis not covered by any of the groups A61B 1/00-A61B 18/00, e.g. for stereotaxis, sterile operation, luxation treatment, wound edge protectors(protective face masks A41D 13/11; surgeons' or patients' gowns or dresses A41D 13/12; devices for carrying-off, for treatment of, or for carrying-over, body liquids A61M 1/00)

Abstract

A method of determining the vascular endothelial function of a subject using GAPDH as a biomarker is presented, whereby the level of GAPDH mRNA and/or GAPDH protein in a sample obtained from a subject is measured and compared to a reference. A difference in the level of GAPDH mRNA and/or GAPDH protein between that measured for the sample and a reference may be indicative of impaired vascular endothelial function and therefore may indicate the onset of a condition related to impaired vascular endothelial function such as atherosclerosis.

IPC Classes  ?

• G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing

Abstract

The present invention relates to the discovery that salt inducible kinases (SIKs) suppress the formation of anti-inflammatory molecules such as IL-10, which are important for the resolution of inflammation and identifies SIK inhibitors that may be used to treat disorders associated with undesirable inflammation, such as inflammatory bowel disease and/or autoimmune disorders.

IPC Classes  ?

• A61K 31/00 - Medicinal preparations containing organic active ingredients
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

The present invention relates to agents capable of binding sialic acid-binding immunoglobulin-like lectin-9 (Siglec-9) and their use in the treatment of cell proliferation and differentiation disorders. Furthermore, the present invention provides associated pharmaceutical formulations and methods.

IPC Classes  ?

• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

A process for the production of an aqueous dispersion of metal nano particles comprising palladium is provided. The process comprises the admixture of a water soluble organic polymer, a palladium salt and a first reducing agent to an aqueous liquid. The first reducing agent is a metal-containing polymer which has reducing properties or a saccharide which has reducing properties. The nano particles can include a second metal. The dispersions can be used as catalysts for electroless plating, to produce heterogeneous catalysts and in the production of anti-microbial devices and compositions.

IPC Classes  ?

• A61K 9/10 - DispersionsEmulsions
• A61K 9/14 - Particulate form, e.g. powders
• A61K 31/28 - Compounds containing heavy metals
• A61K 31/74 - Synthetic polymeric materials
• A61K 33/24 - Heavy metalsCompounds thereof

Abstract

The invention provides compounds according to formula (I): (wherein X, Y, Z1 R1, R2, R3, Ar and Ar' are as dedfined herein), and physiologically acceptable salts, solvates, esters or amides thereof, pharmaceutical compositions comprising these compounds and the compounds for use in medicine, for example for the treatment or prophylaxis of diseases involving cell proliferation, such as cancer, and for the treatment or prophylaxis of other diseases.

IPC Classes  ?

• C07C 335/26 - Y being a hydrogen or a carbon atom, e.g. benzoylthioureas
• C07C 327/54 - Y being a hetero atom
• A61K 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 25/16 - Anti-Parkinson drugs
• A61P 31/18 - Antivirals for RNA viruses for HIV
• A61P 33/06 - Antimalarials
• A61P 35/00 - Antineoplastic agents

Abstract

The invention relates to an intraoral approximal assessment device comprising an approximal optical portion adapted to fit within an intraoral approximal space, a means of applying a disclosing substance to the intraoral approximal space or at least one of the approximal surfaces of the contacting teeth and a detector, with the the approximal optical portion and the detector being operably connected via a light transmitting material. The invention also relates to a method of assessing one or both of the approximal surfaces of contacting teeth located in the same dental arch and a kit for assessing approximal dental surfaces.

IPC Classes  ?

• A61B 5/00 - Measuring for diagnostic purposes Identification of persons

Abstract

The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.

IPC Classes  ?

• A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61K 31/428 - Thiazoles condensed with carbocyclic rings
• A61K 31/664 - Amides of phosphorus acids
• C07D 307/80 - Radicals substituted by oxygen atoms
• C07D 311/16 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring substituted in position 7
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61P 35/00 - Antineoplastic agents
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

The present invention provides methods for diagnosing cell proliferation and/or differentiation disorders, compounds and methods for treating the same and methods for identifying agents potentially useful in the treatment of cell proliferation and/or differentiation disorders.

IPC Classes  ?

• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
• C07K 14/435 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
• C12N 15/85 - Vectors or expression systems specially adapted for eukaryotic hosts for animal cells
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The invention provides a compound according to formula (I): wherein: X is O or S; Y is O or S; each Ar and Ar' is independently a mono-, bi- or tricyclic aryl or heteroaryl group optionally substituted with one or more substituents selected from halo, alkyl, aryl, heteroaryl, hydroxyl, nitro, amino, alkoxy, alkylthio, cyano, thio, ester, acyl and amido; each R2 is independently hydrogen, halo, alkyl, aryl, heteroaryl, hydroxyl, nitro, amino, alkoxy, alkylthio, cyano and thio; and R1 is as defined herein, or a physiologically acceptable salt, solvate, ester, amide or other physiologically functional derivative thereof.

IPC Classes  ?

• C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
• C07D 239/56 - One oxygen atom and one sulfur atom
• A61P 35/00 - Antineoplastic agents

Abstract

The invention provides a compound of formula (I), wherein X, L1-4 and R1-4 are as defined herein, with the proviso that the compound is not (i) 4-benzoyl-3,5-dimethyl-1H-pyrrole-2-carboxylic acid ethyl ester; (ii) 4-(2,5-difluorobenzoyl)-3,5-dimethyl-1H-pyrrole-2-carboxylic acid ethyl ester); (iii) 4-acetyl-3,5-dimethyl-1H-pyrrole-2-carboxylic acid ethyl ester; or (iv) 4-(3-dimethylamino-acryloyl)-3,5-dimethyl-1H-pyrrole-2-carboxylic acid ethyl ester, or a pharmaceutically acceptable derivative thereof.

IPC Classes  ?

• C07D 207/06 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61P 35/00 - Antineoplastic agents

Abstract

Non-human animals which overexpress PPARd or which express transgenic PPARd are useful as models for inflammatory skin conditions such as psoriasis. Test substances can be screened to assess their suitability for the treatment of inflammatory skin conditions such as psoriasis. Methyl 3-({[2-(methoxy)-4-phenyl]amino}sulfonyl)-2-thiophenecarboxylate can be administered topically for the prevention or treatment of psoriasis.

IPC Classes  ?

• C12N 15/85 - Vectors or expression systems specially adapted for eukaryotic hosts for animal cells
• A01K 67/027 - New or modified breeds of vertebrates
• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals

Abstract

The present invention provides compounds which modulate the expression of keratin genes, particularly mutated or defective keratin genes, for treating epithelial fragility disorders such as Meesmann Epithelial Corneal Dystrophy (MECD).

IPC Classes  ?

• C12N 15/11 - DNA or RNA fragmentsModified forms thereof

Abstract

A process for the production of an aqueous dispersion of metal nano particles comprising palladium is provided. The process comprises the admixture of a water soluble organic polymer, a palladium salt and a first reducing agent to an aqueous liquid. The first reducing agent is a metal-containing polymer which has reducing properties or a saccharide which has reducing properties. The nano particles can include a second metal. The disperions can be used as catalysts for electroless plating, to produce heterogeneous catalysts and in the production of anti-microbial devices and compositions.

IPC Classes  ?

• C23C 18/30 - Activating
• C23C 18/44 - Coating with noble metals using reducing agents
• C25D 5/02 - Electroplating of selected surface areas
• C25D 5/34 - Pretreatment of metallic surfaces to be electroplated

Abstract

The present invention relates to specific compounds for use in controlling inflammatory cell function and their potential use in modulating an immune response or inflammation. The present invention also relates to the identification of an alternative RSK pathway in, for example, dendritic cells and the development of assays for the identification of compounds capable of modulating the alternative RSK associated pathway in dendritic cells/macrophage cells and their potential use in enhancing, or controlling an immune response or in treating inflammation.

IPC Classes  ?

• A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems

Abstract

The present invention relates to a method of modulating gene expression using snoRNA molecules or snoRNA like molecules or fragments, designed to target specific nucleic acid sequences.

IPC Classes  ?

• C12N 15/11 - DNA or RNA fragmentsModified forms thereof

Abstract

The present invention relates to the use of certain pyrimidine compounds to inhibit, for example, TBKl and/or IKK epsilon and which may therefore find application in treating cancer septic shock and/or Primary open Angle Glaucoma (POAG).

IPC Classes  ?

• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 27/06 - Antiglaucoma agents or miotics
• A61P 35/00 - Antineoplastic agents
• A61P 31/04 - Antibacterial agents

Abstract

The invention provides a method for determining a degree of phosphorylation of a substrate, for example a peptide substrate, using a fluorescence probe that acts alone or with another material and has a lifetime that varies when in proximity to a phosphate, the method comprising: causing the fluorescence probe to fluoresce; measuring a time response of the fluorescence, and analysing the fluorescence time response to identify a fluorescence component having a lifetime associated with phosphorylated substrate and a fluorescence component having a lifetime associated with un-phosphorylated substrate.

IPC Classes  ?

• G01N 33/58 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving labelled substances
• C12Q 1/42 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving phosphatase
• C12Q 1/48 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving transferase

Abstract

A medical imager, primarily for use in oral and dental applications. The imager has a source for providing a plurality of collimated beams of non-ionising radiation, in particular near-infrared light, and a plurality of correlated detectors. Each detector is arranged to receive unscattered light from one or part of one of said collimated beams and scattered light from one or more other beams. The imager further comprises means for using both the unscattered and scattered light to form an image.

IPC Classes  ?

• A61B 5/00 - Measuring for diagnostic purposes Identification of persons
• G01N 21/49 - Scattering, i.e. diffuse reflection within a body or fluid

Abstract

The invention relates to a composition for the detection of tooth demineralisation. More specifically, the invention concerns a composition comprising a complex capable of producing an optical signal characteristic of the presence of free ions, the pharmaceutical uses of such a composition, and methods and a kit for the detection of active demineralisation at tooth surfaces using such a composition.

IPC Classes  ?

• A61K 49/00 - Preparations for testing in vivo

Abstract

The present invention provides glucoimidazole derivatives and methods of making them. The compounds can be used to inhibit the activity of O-GlcNAcase enzymes, including both bacterial OGA (bOGA) and human OGA (hOGA) and can be selective, showing low inhibition of hexosaminidases. The compounds can be used to study the role of the O-GlcNAcase modification in human or animal cells. Furthermore the compounds can have therapeutic uses in the treatment of diseases mediated by the activity of O-GlcNAcase enzymes including type II diabetes, Alzheimers Disease, and cancer.

IPC Classes  ?

• A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• C07D 471/04 - Ortho-condensed systems
• A61P 5/50 - Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Abstract

The present invention relates to a new improved process for preparing Rimcazole and its salts.

IPC Classes  ?

• C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Abstract

The present invention relates to compounds which acivate the p53 response, and find use in, for example, hyperproliferative diseases such as cancer treatment and potentially other diseases/conditions (involving sirtuin function).

IPC Classes  ?

• A61K 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine

Abstract

The present invention relates to a method of identifying optimal or desirable conditions for maintaining a selected protein in solution for enabling proteins to be kept in solution at high enough concentrations for structural analysis and the like.

IPC Classes  ?

• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids

Abstract

The present invention relates to an improved assay for identifying compounds that may be of use in conjunction with cancer chemotherapeutic agents and anti-proliferative agents, to improve efficacy of such agents and/or render effective compounds with relatively little therapeutic activity. There is also provided a class of compounds of formula (I) and retinoids identified by said assay which may be used in a combination therapy, with current and novel agents, to treat cancers and other diseases associated with abnormal host cell proliferation, such as psoriasis.

IPC Classes  ?

• A61K 31/00 - Medicinal preparations containing organic active ingredients
• A61K 31/07 - Retinol compounds, e.g. vitamin A
• A61K 31/203 - Retinoic acids
• A61K 31/12 - Ketones
• A61P 35/00 - Antineoplastic agents
• A61P 17/06 - Antipsoriatics
• C12N 5/00 - Undifferentiated human, animal or plant cells, e.g. cell linesTissuesCultivation or maintenance thereofCulture media therefor
• C12Q 1/00 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions

Abstract

A resorbable insert, formed for attachment within the oral cavity of a subject comprises a polymer material slowly soluble in the mouth; and at least one therapeutic agent, for slow release in use. Methods of treatment or prevention of disease states using the resorbable inserts and methods of manufacture of the inserts are also provided.

IPC Classes  ?

• A61K 33/16 - Fluorine compounds
• A61K 33/24 - Heavy metalsCompounds thereof
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

The present invention relates to the prevention/treatment of ichthyosis vulgaris (IV), atopy and potentially other disorders associated with loss-of-function mutations in the filaggrin gene sequence. The prevention/therapy is based on the use of agents which enable the host's translational machinery to read through a nonsense mutation found in a mutant allele of the filaggrin gene.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
• A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids

Abstract

The present invention relates to the identification of loss-of-function mutations in the filaggrin gene and their use in diagnosing ichthyosis vulgaris and/or susceptibility to other diseases including atopic dermatitis (eczema), asthma, psoriasis and allergies (including food allergy).

IPC Classes  ?

• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids

Abstract

The present invention relates to agents capable of binding sialic acid-binding immunoglobulin-like lectin-9 (Siglec-9) and their use in the treatment of cell proliferation and differentiation disorders. Furthermore, the present invention provides associated pharmaceutical formulations and methods.

IPC Classes  ?

• A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates

Abstract

A surgical device (10) comprises an elongate member (12) defining at least one notch (16) in an outer surface thereof, wherein said elongate member (12) is adapted to be deformed in the region of said notch (16). The notch (16) is formed within the elongate member (12) at a location determined in accordance with specific patient requirements and geometries. A surgical instrument (14), such as a biopsy cutter, is mounted on an end of the elongate member (12).

IPC Classes  ?

• A61B 1/005 - Flexible endoscopes
• A61B 17/24 - Surgical instruments, devices or methods for use in the oral cavity, larynx, bronchial passages or noseTongue scrapers
• A61B 17/00 - Surgical instruments, devices or methods
• A61B 17/28 - Surgical forceps
• A61B 19/00 - Instruments, implements or accessories for surgery or diagnosis not covered by any of the groups A61B 1/00-A61B 18/00, e.g. for stereotaxis, sterile operation, luxation treatment, wound edge protectors(protective face masks A41D 13/11; surgeons' or patients' gowns or dresses A41D 13/12; devices for carrying-off, for treatment of, or for carrying-over, body liquids A61M 1/00)

Abstract

The described invention relates to compounds (I) which modulate cell migration, and find use in, for example, wound healing, cancer progression and angiogenesis. All definitions as in claim 1.

IPC Classes  ?

• A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 35/00 - Antineoplastic agents
• C07D 243/14 - 1,4-BenzodiazepinesHydrogenated 1,4-benzodiazepines

Abstract

A surgical apparatus (20) For trans-nasal use comprises an outer tubular member (22), an intermediate tubular member (24) slidably mounted within the outer member (22) and moveable between retracted and extended positions, and an inner member (26) slidably mounted within the intermediate tubular member (24) and adapted to be moved between retracted and extended positions. The intermediate member (24) defines a constrained shape when retracted within the outer member (22), and an unconstrained shape when extended from the outer tubular member (22), and the inner member (26) defines an unconstrained shape when in an extended position. The surgical apparatus (20) further comprises end effector means such as a cutter (30) mounted on a distal end (28) of the inner member (26) for cutting tissue from a patient (44) during a biopsy procedure, for example. In use, appropriate extension and retraction of the intermediate and inner members (24, 26) permits the end effector means (30) to be steered through a body cavity to a target site.

IPC Classes  ?

• A61B 10/04 - Endoscopic instruments, e.g. catheter-type instruments

Abstract

The present invention relates to compounds and uses of compounds which interact with chitinase enzymes, in particular inhibition of those enzymes.

IPC Classes  ?

• C07D 473/04 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
• A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• A61P 33/00 - Antiparasitic agents

Abstract

The present invention relates to drug screening assays. The present invention also relates to methods of identifying putative drug target genes/proteins, as well as methods of testing the efficacy of test drug candidates.

IPC Classes  ?

• C12Q 1/02 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving viable microorganisms