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47759 results about "Combinatorial chemistry" patented technology
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Combinatorial chemistry comprises chemical synthetic methods that make it possible to prepare a large number (tens to thousands or even millions) of compounds in a single process. These compound libraries can be made as mixtures, sets of individual compounds or chemical structures generated by computer software. Combinatorial chemistry can be used for the synthesis of small molecules and for peptides.
6-modified bicyclic nucleic acid analogs
The present invention provides 6-modified bicyclic nucleoside analogs and oligomeric compounds comprising these nucleoside analogs. In preferred embodiments the nucleoside analogs have either (R) or (S)-chirality at the 6-position. These bicyclicnucleoside analogs are useful for enhancing properties of oligomeric compounds including nuclease resistance.
Owner:IONIS PHARMA INC
Target analyte sensors utilizing microspheres
A microsphere-based analytic chemistry system and method for making the same is disclosed in which microspheres or particles carrying bioactive agents may be combined randomly or in ordered fashion and dispersed on a substrate to form an array while maintaining the ability to identify the location of bioactive agents and particles within the array using an optically interrogatable, optical signature encoding scheme. A wide variety of modified substrates may be employed which provide either discrete or non-discrete sites for accommodating the microspheres in either random or patterned distributions. The substrates may be constructed from a variety of materials to form either two-dimensional or three-dimensional configurations. In a preferred embodiment, a modified fiber optic bundle or array is employed as a substrate to produce a high density array. The disclosed system and method have utility for detecting target analytes and screening large libraries of bioactive agents.
Owner:TRUSTEES OF TUFTS COLLEGETHE
Pentapeptide compounds and uses related thereto
Pentapeptide compounds are disclosed. The compounds have biological activity, e.g., cytotoxicity. Prodrugs having targeting groups and pentapeptide moieities, as well as precursors thereof are also disclosed. For example, precursors having a reactive linker that can serve as a reaction site for joining to a targeting agent, e.g., an antibody, as disclosed.
Owner:SEAGEN INC
Means to achieve sustained release of synergistic drugs by conjugation
A codrug composition of at least two drug compounds covalently linked to one another via a labile bond to form a single codrug composition, or ionically linked to one another to form a single workings composition, and methods of use of the codrug for the treatment of various medical conditions. The codrug may be administered by itself or in the form of a bioerodible or nonbioerodible substance.
Owner:UNIVERSITY OF KENTUCKY +1
Method for producing fluorinated organic compounds
ActiveUS20070197842A1Preparation by hydrogen halide split-offPreparation by halogen replacementPtru catalystDistillation
Disclosed are processes for the production of fluorinated olefins, preferably adapted to commercialization of CF3CF═CH2 (1234yf). Three steps may be used in preferred embodiments in which a feedstock such as CCl2═CClCH2Cl (which may be purchased or synthesized from 1,2,3-trichloropropane) is fluorinated (preferably with HF in gas-phase in the presence of a catalyst) to synthesize a compound such as CF3CCl═CH2, preferably in a 80-96% selectivity. The CF3CCl═CH2 is preferably converted to CF3CFClCH3 (244-isomer) using a SbCl5 as the catalyst which is then transformed selectively to 1234yf, preferably in a gas-phase catalytic reaction using activated carbon as the catalyst. For the first step, a mixture of Cr2O3 and FeCl3 / C is preferably used as the catalyst to achieve high selectivity to CF3CCl═CH2 (96%). In the second step, SbCl5 / C is preferably used as the selective catalyst for transforming 1233xf to 244-isomer, CF3CFClCH3. The intermediates are preferably isolated and purified by distillation and used in the next step without further purification, preferably to a purity level of greater than about 95%.
Owner:HONEYWELL INT INC
N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
The invention discloses certain N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing said compounds as an active ingredient thereof, and the use of said compounds in inhibiting dipeptidyl peptidase-IV.
Owner:NOVARTIS AG
N-benz-3-substituted amino pyrazoles compounds with insecticidal activity
The invention discloses an N-phenyl-3-substitution amino-pyrazole compound which is shown in a formular (1) and has the insecticidal activity, and a preparation method thereof.
Owner:HUNAN CHEM RES INST
Methods for synthesis of oligonucleotides
Improved methods for synthesis of oligonucleotides and other phosphorus-linked oligomers are disclosed. The methods include the use of aromatic solvents, alkyl aromatic solvents, halogenated aromatic solvents, halogenated alkyl aromatic solvents, or aromatic ether solvents to achieve deprotection of protected hydroxyl groups.
Owner:IONIS PHARMA INC
Processes for production and purification of hydrofluoroolefins
ActiveUS20060106263A1High selectivityPreparation by hydrogen halide split-offHydrogen fluorideHydrogen fluoridePurification methods
Owner:THE CHEMOURS CO FC LLC
Binding agent for solid block functional material
InactiveUS6258765B1Fit tightlyEasy to cleanInorganic/elemental detergent compounding agentsOrganic detergent compounding agentsBULK ACTIVE INGREDIENTActive ingredient
A solid functional material comprises a functional agent such as a cleaning composition, a sanitizing agent, where a rinse agent, etc. in a solid block format. The solid block is formed by a binding agent that forms the active ingredients into a solid block. The binding agent comprises a phosphonate or amino acetate sequestrant, a carbonate salt and water in an E-Form hydrate. These materials at a specific mole ratio form a novel binding agent that can form functional materials into a solid matrix form.
Owner:ECOLAB USA INC
Methods for detecting target analytes and enzymatic reactions
A microsphere-based analytic chemistry system and method for making the same is disclosed in which microspheres or particles carrying bioactive agents may be combined randomly or in ordered fashion and dispersed on a substrate to form an array while maintaining the ability to identify the location of bioactive agents and particles within the array using an optically interrogatable, optical signature encoding scheme. A wide variety of modified substrates may be employed which provide either discrete or non-discrete sites for accommodating the microspheres in either random or patterned distributions. The substrates may be constructed from a variety of materials to form either two-dimensional or three-dimensional configurations. In a preferred embodiment, a modified fiber optic bundle or array is employed as a substrate to produce a high density array. The disclosed system and method have utility for detecting target analytes and screening large libraries of bioactive agents.
Owner:TRUSTEES OF TUFTS COLLEGE TUFTS UNIV
N-(substituted glycyl)-thiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
The invention discloses certain N-(substituted glycyl)-thiazolidines, pharmaceutical compositions containing said compounds as an active ingredient thereof, and the use of said compounds in inhibiting dipeptidyl peptidase-IV.
Owner:NOVARTIS AG
Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components
InactiveUS6887470B1Easy to testPeptide/protein ingredientsImmunoglobulins against cell receptors/antigens/surface-determinantsBlood componentCombinatorial chemistry
A method for protecting a peptide from peptidase activity in vivo, the peptide being composed of between 2 and 50 amino acids and having a C-terminus and an N-terminus and a C-terminus amino acid and an N-terminus amino acid is described. In the first step of the method, the peptide is modified by attaching a reactive group to the C-terminus amino acid, to the N-terminus amino acid, or to an amino acid located between the N-terminus and the C-terminus, such that the modified peptide is capable of forming a covalent bond in vivo with a reactive functionality on a blood component. In the next step, a covalent bond is formed between the reactive group and a reactive functionality on a blood component to form a peptide-blood component conjugate, thereby protecting said peptide from peptidase activity. The final step of the method involves the analyzing of the stability of the peptide-blood component conjugate to assess the protection of the peptide from peptidase activity.
Owner:CONJUCHEM
Pentapeptide compounds and uses related thereto
Pentapeptide compounds are disclosed. The compounds have biological activity, e.g., cytotoxicity. Prodrugs having targeting groups and pentapeptide moieities, as well as precursors thereof are also disclosed. For example, precursors having a reactive linker that can serve as a reaction site for joining to a targeting agent, e.g., an antibody, as disclosed.
Owner:SEAGEN INC
Indole and azaindole inhibitors of fructose-1,6-bisphosphatase
Novel indole and azaindole compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described: and pharmaceutically acceptable prodrugs and salts thereof.
Owner:METABASIS THERAPEUTICS INC
Non-cross-linking pyrrolo[2,1-c][1,4]benzodiazepines and process thereof
The present invention relates to novel pyrrolo[2,1-c][1,4]benzodiazepines compounds of general formula V as shown below, which are useful as potential antitumour agents and a process of preparing these compounds; particularly the present invention provides a process for the preparation of 7-methoxy-8-{n-[7-methoxy-(11aS)-1,2,3,10,11,11a-hexahydro-5H-pyrrolo[2,1-c][1,4]ben-zodiazepine-5-one-8-yloxy]alkyloxy}-(11aS)-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one, with varying aliphatic chain length and its 2-hydroxy derivatives.
![Non-cross-linking pyrrolo[2,1-c][1,4]benzodiazepines and process thereof](https://images-eureka.patsnap.com/patent_img/a1449a37-a515-47d2-a66e-d0d6055aa076/US06884799-20050426-D00001.png "Non-cross-linking pyrrolo[2,1-c][1,4]benzodiazepines and process thereof")
![Non-cross-linking pyrrolo[2,1-c][1,4]benzodiazepines and process thereof](https://images-eureka.patsnap.com/patent_img/a1449a37-a515-47d2-a66e-d0d6055aa076/US06884799-20050426-C00001.png "Non-cross-linking pyrrolo[2,1-c][1,4]benzodiazepines and process thereof")
![Non-cross-linking pyrrolo[2,1-c][1,4]benzodiazepines and process thereof](https://images-eureka.patsnap.com/patent_img/a1449a37-a515-47d2-a66e-d0d6055aa076/US06884799-20050426-C00002.png "Non-cross-linking pyrrolo[2,1-c][1,4]benzodiazepines and process thereof")
Owner:COUNCIL OF SCI & IND RES
Prodrugs built as multiple self-elimination-release spacers
This invention concerns multiple release spacers and spacer systems, which release multiple leaving groups following a single activation. It concerns compounds comprising a specifier linked to two or more of the same or different leaving groups (L in the figure) via a self-eliminating multiple release spacer or spacer system, which compounds upon a single activation step, in particular removal or transformation of the specifier, release at least two leaving groups.
Owner:SYNTARGA BV
Lanthanide-based catalyst composition for producing cis-1,4-polydienes
InactiveUS7008899B2Easy to processHigh viscosityOrganic-compounds/hydrides/coordination-complexes catalystsCatalyst activation/preparationPtru catalystLanthanide
Owner:BRIDGESTONE CORP
11-hydroxy-5h-pyrrolo[2,1-c][1,4] benzodiazepin-5-one derivatives as key intermediates for the preparation of c2 substituted pyrrolobenzodiazepines
![11-hydroxy-5h-pyrrolo[2,1-c][1,4] benzodiazepin-5-one derivatives as key intermediates for the preparation of c2 substituted pyrrolobenzodiazepines](https://images-eureka.patsnap.com/patent_img/dfe0bdc2-9bfe-4984-a8af-93415b268a91/US07741319-20100622-C00001.png "11-hydroxy-5h-pyrrolo[2,1-c][1,4] benzodiazepin-5-one derivatives as key intermediates for the preparation of c2 substituted pyrrolobenzodiazepines")
![11-hydroxy-5h-pyrrolo[2,1-c][1,4] benzodiazepin-5-one derivatives as key intermediates for the preparation of c2 substituted pyrrolobenzodiazepines](https://images-eureka.patsnap.com/patent_img/dfe0bdc2-9bfe-4984-a8af-93415b268a91/US07741319-20100622-C00002.png "11-hydroxy-5h-pyrrolo[2,1-c][1,4] benzodiazepin-5-one derivatives as key intermediates for the preparation of c2 substituted pyrrolobenzodiazepines")
![11-hydroxy-5h-pyrrolo[2,1-c][1,4] benzodiazepin-5-one derivatives as key intermediates for the preparation of c2 substituted pyrrolobenzodiazepines](https://images-eureka.patsnap.com/patent_img/dfe0bdc2-9bfe-4984-a8af-93415b268a91/US07741319-20100622-C00003.png "11-hydroxy-5h-pyrrolo[2,1-c][1,4] benzodiazepin-5-one derivatives as key intermediates for the preparation of c2 substituted pyrrolobenzodiazepines")
Owner:MEDIMMUNE LTD
System and process for preparing aromatic hydrocarbon by converting methanol or dimethyl ether
ActiveCN101823929AHigh yieldHigh selectivityHydrogen separation using liquid contactHydrocarbon from oxygen organic compoundsAromatizationAromatic hydrocarbon
The invention relates to a system and a process for preparing aromatic hydrocarbon by converting methanol or dimethyl ether and belongs to the technical field of aromatic hydrocarbon production. The methanol or the dimethyl ether serving as a raw material firstly reacts in an aromatization reactor; a reaction product is separated; H2, methane, mixed C8 aromatic hydrocarbon and partial C9s + hydrocarbons serving as products are output from the system; and C2+ non-aromatic hydrocarbon and aromatic hydrocarbons except the mixed C8 aromatic hydrocarbon and the partial C9s + hydrocarbons are take as a circular material flow and return to corresponding reactors for further aromatization reaction. By separating and recycling the product obtained in the process of aromizing the methanol or the dimethyl ether, the system and the process improve the yield and selectivity of the aromatic hydrocarbon; and moreover, the process is flexible, and target products can be changed according to market demands.
Owner:TSINGHUA UNIV
Triple Combination Release Multi-Layered Tablet
This invention pertains to a multi-layered tablet for a triple combination release of active agents to an environment of use. More particularly, the invention pertains to a multi-layered tablet (1) comprising two external drug-containing layers (2 and 3) in stacked arrangement with respect to and on opposite sides of an oral dosage form (4) that provides a triple combination release of at least one active agent. In one embodiment of the invention the dosage form is an osmotic device. In another embodiment of the invention the dosage form is a gastro-resistant coated core. In yet another embodiment of the invention the dosage form is a matrix tablet. In a different embodiment the dosage form is a hard capsule.
Owner:ACELLA HLDG LLC +1
Biomolecular coupling methods using 1,3-dipolar cycloaddition chemistry
InactiveUS20050032081A1Bioreactor/fermenter combinationsBiological substance pretreatmentsBio moleculesCycloaddition
This invention provides methods for covalently affixing a biomolecule to either a second molecule or a solid surface using 1,3-dipolar cycloaddition chemistry. This invention also provides related methods and compositions.
Owner:THE TRUSTEES OF COLUMBIA UNIV IN THE CITY OF NEW YORK
Compositions of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
![Compositions of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide](https://images-eureka.patsnap.com/patent_img/7fc68549-2d37-4f83-89dd-f36e605466b3/US07553855-20090630-D00001.png "Compositions of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide")
![Compositions of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide](https://images-eureka.patsnap.com/patent_img/7fc68549-2d37-4f83-89dd-f36e605466b3/US07553855-20090630-D00002.png "Compositions of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide")
![Compositions of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide](https://images-eureka.patsnap.com/patent_img/7fc68549-2d37-4f83-89dd-f36e605466b3/US07553855-20090630-D00003.png "Compositions of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide")
Owner:VERTEX PHARMA INC
Liquid dosage compositions of stable nanoparticulate active agents
The present invention relates to liquid dosage compositions of stable nanoparticulate active agents. The liquid dosage compositions of the invention include osmotically active crystal growth inhibitors that stabilize the nanoparticulate active agents against crystal and particle size growth of the active agent.
Owner:ELAN PHRMA INT LTD
Topologically segregated, encoded solid phase libraries comprising linkers having an enzymatically susceptible bond
The invention relates to libraries of synthetic test compound attached to separate phase synthesis supports. In particular, the invention relates to libraries of synthetic test compound attached to separate phase synthesis supports that also contain coding molecules that encode the structure of the synthetic test compound. The molecules may be polymers or multiple nonpolymeric molecules. Each of the solid phase synthesis support beads contains a single type of synthetic test compound. The synthetic test compound can have backbone structures with linkages such as amide, urea, carbamate (i.e., urethane), ester, amino, sulfide, disulfide, or carbon-carbon, such as alkane and alkene, or any combination thereof. Examples of subunits suited for the different linkage chemistries are provided. The synthetic test compound can also be molecular scaffolds, such as derivatives of monocyclic of bicyclic carbohydrates, steroids, sugars, heterocyclic structures, polyaromatic structures, or other structures capable of acting as a scaffolding. Examples of suitable molecular scaffolds are provided. The invention also relates to methods of synthesizing such libraries and the use of such libraries to identify and characterize molecules of interest from among the library of synthetic test compound.
Owner:AVENTIS PHARMA INC
Conveniently implantable sustained release drug compositions
InactiveUS20080038316A1Economical and practical and efficientEasy to produceBiocideOrganic active ingredientsDiseaseSustained release drug
This invention provides for biocompatible and biodegradable syringeable liquid, implantable solid, and injectable gel pharmaceutical formulations useful for the treatment of systemic and local disease states.
Owner:RAMSCOR
High-throughput formation, identification, and analysis of diverse solid-forms
InactiveUS20020048610A1Cost-effectiveImprove bioavailabilitySequential/parallel process reactionsFrom normal temperature solutionsSolubilitySolid mass
The invention concerns arrays of solid-forms of substances, such as compounds and rapid-screening methods therefor to identify solid-forms, particularly of pharmaceuticals, with enhanced properties. Such properties include improved bioavailability, solubility, stability, delivery, and processing and manufacturing characteristics. The invention relates to a practical and cost-effective method to rapidly screen hundreds to thousands of samples in parallel. The invention further provides methods for determining the conditions and / or ranges of conditions required to produce crystals with desired compositions, particle sizes, habits, or polymorphic forms. In a further aspect, the invention provides high-throughput methods to identify sets of conditions and / or combinations of components compatible with particular solid-forms, for example, conditions and / or components that are compatible with advantageous polymorphs of a particular pharmaceutical.
Owner:MILLENNIUM PHARMA INC +1
Prodrugs containing novel bio-cleavable linkers
Owner:PIRAMAL ENTERPRISES LTD
Methods and apparatus for drug delivery involving phase changing formulations
InactiveUS20020004063A1Cleanly peeled from the skinMaintenance of such surfaceSalicyclic acid active ingredientsAnaestheticsPharmaceutical formulationSoft solids
This invention relates to an apparatus and method of drug delivery on a human body surface. The formulation comprises a drug, a conversion agent capable of converting the formulation from a less solid phase to a coherent, soft, solid phase, and a vehicle medium or carrier for the drug and conversion agent. The drug formulation is applied to this human body surface in its less than solid phase and is subsequently converted to a soft solid phase while the drug is being delivered through the human body surface. After delivery of the drug is complete, the soft solid formulation can be removed or peeled from the body surface as a coherent solid formulation. The drug formulation provides control over drug delivery rates and allows the formulation to be removed without leaving a messy, residual formulation on the body surface.
Owner:CRESCITA THERAPEUTICS INC
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