Class / Patent application number | Description | Number of patent applications / Date published |
536170300 | Nitrogen containing hetero ring | 42 |
20100121041 | METHOD FOR PRODUCTION OF SUGAR OXAZOLINE DERIVATIVE - Disclosed is a process for producing an oxazoline derivative from a non-protected sugar in a simple manner. Also disclosed is a process for producing a glycoside by utilizing the product of the aforementioned process. A sugar oxazoline derivative is synthesized in one step in an aqueous solution from a sugar having a free hemiacetalic hydroxy group and an amido group by using a haloformamidinium derivative as a dehydrating agent. A glycoside compound is produced by using the oxazoline derivative as a sugar donor and also using a sugar dehydrogenase. The method can be applied to the production of a compound having a long sugar chain, and is therefore useful for the production of a physiologically active oligosaccharide, a carrier for a drug delivery system, a surfactant, a carbohydrate-based drug, a glycopeptide, a glycoprotein, a carbohydrate polymer or the like. | 05-13-2010 |
20120095197 | METHODS AND COMPOUNDS USEFUL FOR THE PREPARATION OF SODIUM GLUCOSE CO-TRANSPORTER 2 INHIBITORS - Methods of synthesizing sodium glucose co-transporter 2 inhibitors, as well as compounds useful therein, are disclosed. Particular inhibitors are compounds of formula I: | 04-19-2012 |
20130203975 | GLYCOSIDE DERIVATIVES AND USES THEREOF - The present invention provides a compound of formula I; | 08-08-2013 |
536170400 | Nitrogen in aglycone moiety | 39 |
20080262209 | Activated Sialic Acid Derivatives for Protein Derivatisation and Conjugation - Derivatives of PSAs are synthesised, in which a reducing and/or non-reducing end terminal sialic acid unit is transformed into a N-hydroxysuccinimide (NHS) group. The derivatives may be reacted with substrates, for instance substrates containing amine or hydrazine groups, to form non-cross-linked/crosslinked polysialylated compounds. The substrates may, for instance, be therapeutically useful drugs, peptides or proteins or drug delivery systems. | 10-23-2008 |
20080287663 | Process For Production Of 4-Biphenylyazetidin-2-Ones - The present invention relates to processes for the production of 4-biphenylylazetidin-2-one derivatives of formula | 11-20-2008 |
20090036657 | PYRROLO[2, 1-C][1, 4]BENZODIAZEPINE-GLYCOSIDE PRODRUG USEFUL AS A SELECTIVE ANTI TUMOR AGENT - The present invention provides novel pyrrolo[2,1-c][1,4]benzodiazepine-glycoside prodrug of general formula 1a-b, useful as selective anticancer agents. The present invention also provides a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine-glycoside prodrugs of general formula 1a-b. This invention also provides activation of these produgs by | 02-05-2009 |
20090062518 | PROCESS FOR PRODUCTION OF GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVE - The present invention relates to a method for preparing the glucopyranosyloxypyrazole derivatives which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like. | 03-05-2009 |
20090209745 | RADIOGRAPHIC CONTRASTING AGENTS AND RADIO-OPAQUE POLYMERIC MATERIALS FOR MEDICAL DEVICES - The present invention discloses a radiographic contrasting agent containing multiple aromatic groups, each of which is substituted with at least three halogen atoms. The radiographic contrasting agent can initiate a polymerization process. The present invention also discloses a radio-opaque polymeric material that comprises a biodegradable polymer having at least one radiographic contrasting moiety covalently attached thereto. The radio-opaque polymeric material provides enhanced contrasting intensity in radiographic imaging. The radio-opaque polymeric material can be applied on at least a portion of one surface of a medical device. The radio-opaque polymeric material can also be used to construct a medical device, a component thereof, or a portion of a component thereof. | 08-20-2009 |
20100029919 | PYRAZOLE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF AND INTERMEDIATE IN PRODUCING THE SAME - The present invention provides pyrazole derivatives represented by the general formula: | 02-04-2010 |
20100145036 | CHEMICAL LINKERS AND CLEAVABLE SUBSTRATES AND CONJUGATES THEREOF - The present disclosure provides drug-ligand conjugates and drug-cleavable substrate conjugates that are potent cytotoxins. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them. | 06-10-2010 |
20100240878 | Fluorescent saccharide conjugates - The present invention relates to improved fluorescently labeled monosaccharide and low molecular weight oligosaccharide conjugates for immunofluorescent staining, confocal microscopic imaging and flow cytometry/fluorescence activated cell sorting (FACS). These fluorophore conjugates target cells, components of cell surfaces and extracellular components; and are useful as probes for tumor targeting and cellular uptake. | 09-23-2010 |
20100324274 | NOVEL SYNTHETIC GANGLIOSIDE DERIVATIVES AND COMPOSITIONS THEREOF - Novel synthetic gangliosides and pharmaceutical compositions containing such synthetic gangliosides are described. Methods of making the novel synthetic ganglioside compounds and compositions as well as their use in the field of neuroprotection and cancer treatment is also described. | 12-23-2010 |
20110021765 | FLUORINATED LANTHANIDE PROBES FOR 19F MAGNETIC RESONANCE APPLICATIONS - The invention provides a paramagnetic lanthanide (III) complex comprising a lanthanide (III) ion and a polydentate ligand wherein the polydentate ligand comprises one or more fluorine atoms in which the distance of at least. one of the fluorine atoms to the lanthanide ion is less than 7, said polydentate ligand not being a DPTA bisamide of p-CF | 01-27-2011 |
20110034679 | HEMIFUMARATE OF A PYRAZOLE DERIVATIVE - The present invention provides a novel form of 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide with improved storage stability. Since 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}-propylamino)-2,2-dimethylpropionamide hemifumarate dihydrate has extremely excellent storage stability, it is useful as a drug substance. Furthermore, it shows an extremely good crystalline property and can be purified by a convenient method, and therefore is suitable for the industrial preparation. | 02-10-2011 |
20110201793 | PROCESS FOR PRODUCTION OF GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVE - The present invention relates to a method for preparing the glucopyranosyloxypyrazole derivatives which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like. | 08-18-2011 |
20110224413 | CHEMICAL PROCESS - Disclosed herein are processes for preparing glucopyranosyloxypyrazole derivatives and pyrazole intermediates of the same. In particular, the present invention relates to glucopyranosyloxypyrazole derivatives having SGLT2 inhibitory activity and processes and intermediates for preparing the same. | 09-15-2011 |
20120149887 | ALKYNYL SUGAR ANALOGS FOR LABELING AND VISUALIZATION OF GLYCOCONJUGATES IN CELLS - Methods for metabolic oligosaccharide engineering that incorporates derivatized alkyne-bearing sugar analogs as “tags” into cellular glycoconjugates are disclosed. Alkynyl derivatized Fuc and alkynyl derivatized ManNAc sugars are incorporated into cellular glycoconjugates. Chemical probes comprising an azide group and a visual or fluorogenic probe and used to label alkyne-derivatized sugar-tagged glycoconjugates are disclosed. Chemical probes bind covalently to the alkynyl group by Cu(I)-catalyzed [3+2] azide-alkyne cycloaddition and are visualized at the cell surface, intracellularly, or in a cellular extract. The labeled glycoconjugate is capable of detection by flow cytometry, SDS-PAGE, Western blot, ELISA, confocal microscopy, and mass spectrometry. | 06-14-2012 |
20120178915 | PYRIMIDINE DERIVATIVES AND ANALOGS, PREPARATION METHOD AND USE THEREOF - This invention relates with the arylheterocycle-fused pyrimidines, derivatives and analogs of formula I: | 07-12-2012 |
20120190832 | LOW-MOLECULAR SERINE PROTEASES INHIBITORS COMPRISING POLYHYDROXY-ALKYL AND POLYHYDROXY-CYCLOALKYL RADICALS - The invention relates to novel amidines and quanidines, the production and use thereof and the use thereof as trypsine-type serine protease competitive inhibitors, especially thrombine and compliment proteases CIs and C1r. The invention also relates to pharmaceutical compositions which contain said compounds as active ingredients, in addition to the use of the compounds as thrombine inhibitors, anticoagulants, compliment inhibitors and anti-inflammatory agents. The novel compositions are characterised by the linkage of a serine protease inhibitor having amidine or guanidine functions with an alkyl radical having two or more hydroxyl functions, whereby said alkyl radical is derived from sugar derivates. Several sugar structural components or components derived from sugar can therefore be linked to each other. Said principle of linking sugar derivates enables oral active compounds to be obtained. | 07-26-2012 |
20120202979 | POLYMER-CARBOHYDRATE-LIPID CONJUGATES - The invention comprises compounds, methods of making, and methods of using. The compounds may have a backbone and three appended functional groups: one lipid, one hydrophilic polymer, and one carbohydrate. Specific functional groups may be selected for specific applications in formulating pharmaceuticals, cosmetics, nutriceuticals, and the like. A variety of linkers between the backbone and functional groups may also be selected to optimize performance. | 08-09-2012 |
20120264925 | METHOD FOR PRODUCING PYRAZOLE GLYCOSIDE DERIVATIVES - A process for preparing pyrazole-glycoside derivatives of the general Formula (I) in which the meanings are R1 H and R2 F; or R1 F and R2 H; or R1 F and R2 F; R3 (C | 10-18-2012 |
20130012692 | SODIUM CHANNEL BLOCKERS - The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers. | 01-10-2013 |
20130018179 | PROCESSES FOR THE CONVERGENT SYNTHESIS OF CALICHEAMICIN DERIVATIVES - This invention describes processes for the convergent synthesis of calicheamicin derivatives, and similar analogs using bifunctional and trifunctional linker intermediates. | 01-17-2013 |
20130060014 | SURFACE MODIFIED INORGANIC MATERIAL AND PRODUCING METHOD THEREOF - A surface-modified inorganic material and a preparation method thereof. A surface-modified inorganic material is provided which is obtained by allowing an organosilane compound having allyl or an allyl derivative to react with an inorganic material, particularly solid silica or ITO glass, in the presence of an acid and an organic solvent, to introduce an organic group into the inorganic material even at room temperature, as well as a preparation method thereof. The invention can effectively introduce the organic group into the inorganic material even at room temperature, and thus is very effective in introducing compounds having a thermally sensitive functional group, for example, natural compounds or proteins. It is possible to introduce various organic groups into an inorganic material and to separate and purify organic molecule-bonded organosilane compounds using a silica gel column to effectively bond them to inorganic materials. | 03-07-2013 |
20130116417 | Methods for the Development of Vaccines Based on Oligosaccharide-Oligonucleotide Conjugates - Described herein are oligosaccharide-oligonucleotide conjugates useful as vaccines against one or more human or veterinary therapeutic indications, and methods of synthesizing and identifying them. The conjugates may be identified using non-human antibodies as binding targets, thereby expanding the power and scope of the invention. Efficacious conjugates may be identified through an iterative. | 05-09-2013 |
20130144045 | NOVEL SELF-REACTIVE ARMS AND PRODRUGS COMPRISING SAME - The present invention relates to a compound of general formula (I): | 06-06-2013 |
20140005371 | CAPRAZENE AS A NOVEL COMPOUND AND DERIVATIVES THEREOF, AND CAPRAZOL AS A NOVEL COMPOUND AND DERIVATIVES THEREOF | 01-02-2014 |
20140011988 | Dibenzo[B,F][1,4]Oxazepin-11-yl-N-Hydroxybenzamides as HDAC Inhibitors - This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) | 01-09-2014 |
20140031535 | BETA-GLUCURONIDE-LINKER DRUG CONJUGATES - Ligand Drug conjugate compounds comprising a β-glucuronide-based linker and methods of using such compounds are provided. | 01-30-2014 |
20140081010 | PROCESSES FOR THE CONVERGENT SYNTHESIS OF CALICHEAMICIN DERIVATIVES - This invention describes processes for the convergent synthesis of calicheamicin derivatives, and similar analogs using bifunctional and trifunctional linker intermediates. | 03-20-2014 |
20140107327 | METHODS FOR PREPARING DEUTERATED 1,2,3-TRIAZOLES - This disclosure relates to a method that involves reacting an azide with an alkyne in the presence of deuterated water and a copper-containing catalyst, thereby forming a deuterated 1,2,3-triazole. | 04-17-2014 |
20140235839 | PROCESS FOR PRODUCING NOVEL SIALO-SUGAR CHAIN - The present invention provides a novel sialo-sugar chain, a process for producing the sialo-sugar chain, and a device for producing the sialo-sugar chain. A sialo-sugar chain can be easily and efficiently mass-produced by reacting a sugar wherein a hydroxy groups is substituted with an alkynyl group (herein sometimes referred to as “alkynylated sugar”) with a specific sialic acid donor in the presence of a sialic acid-introducing enzyme. | 08-21-2014 |
20140256922 | TOLL-LIKE RECEPTOR-7 AND -8 MODULATORY 1H IMIDAZOQUINOLINE DERIVED COMPOUNDS - The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeic and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure. | 09-11-2014 |
20140275505 | PROCESS FOR THE PREPARATION OF CERTAIN TRIARYL RHAMNOSE CARBAMATES - Triaryl rhamnose carbamate insecticides are prepared from triaryl carbamates and the tetrahydropyran-2-ols in good yield without the use of a hydride base. | 09-18-2014 |
20140303360 | Small Molecule Compounds for the Control of Nematodes - The present invention relates to compounds involved in nematode signaling. | 10-09-2014 |
20140309409 | Sialic Acid Derivatives - An amine or hydrazide derivative of a sialic acid unit, e.g. in a polysaccharide, is reacted with a bifunctional reagent at least one of the functionalities of which is an ester of N-hydroxy succinimide, to form an amide or hydrazide product. The product has a useful functionality, which allows it to be conjugated, for instance to proteins, drugs, drug delivery systems or the like. The process is of particular utility for derivatising amine groups introduced in sialic acid terminal groups of polysialic acids. | 10-16-2014 |
20140364595 | CONJUGATE-BASED ANTIFUNGAL AND ANTIBACTERIAL PRODRUGS - The invention provides conjugate-based antifungal or antibacterial prodrugs formed by coupling at least one anti-fungal agent or antibacterial agent with at least one linker and/or carrier. The prodrugs are of formula: (i) (AFA) | 12-11-2014 |
20140378674 | PROCESS FOR THE PREPARATION OF CERTAIN TRIARYL RHAMNOSE CARBAMATES - Triaryl rhamnose carbamate insecticides are prepared from triaryl acyl azides and tetrahydropyran-2-ols in good yield without the use of a hydride base. | 12-25-2014 |
20150141631 | PYRAZOLE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES - The present invention provides pyrazole derivatives, uses thereof for medical purposes and so on. More particularly, the present invention relates to pharmaceuticals useful for the prevention or treatment of constipation, which comprise as an active ingredient 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide, or a pharmaceutically acceptable salt thereof. The pharmaceuticals of the present invention exert an effect of increasing the frequency of bowel movement or the like, and are useful for the prevention or treatment of constipation. | 05-21-2015 |
20150148527 | SUGAR CHAIN-CONTAINING POLYMER, AND SUGAR CHAIN-CONTAINING POLYMER COMPLEX - A sugar chain-containing polymer that enables targeting to the lesion area of liver fibrosis and is useful for imaging, diagnosis and therapy of liver fibrosis; and a sugar chain-containing polymer complex comprising the polymer as a carrier for an anionic substance useful fix therapy and the like; are provided. The polymer is a sugar chain-containing polymer which is a cationic polymer comprising an amine, which polymer comprises N-acetylglucosamine bound thereto. The polymer preferably has a disulfide bond. The polymer preferably has a structure in which polyethyleneimine is linked via a disulfide bond. | 05-28-2015 |
20150376146 | SODIUM CHANNEL BLOCKERS - The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers. | 12-31-2015 |
20160108076 | MODULAR SYNTHESIS OF AMPHIPHILIC JANUS GLYCODENDRIMERS AND THEIR SELF-ASSEMBLY INTO GLYCODENDRIMERSOMES - The invention concerns compounds of the formula (I) wherein: Y | 04-21-2016 |