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1435 results about "Pharmacometrics" patented technology
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Pharmacometrics is mathematical models of biology, pharmacology, disease, and physiology used to describe and quantify interactions between xenobiotics and patients (human and non-human), including beneficial effects and adverse effects. It is normally applied to quantify drug, disease and trial information to aid efficient drug development, regulatory decisions and rational drug treatment in patients.
Apolipoprotein A-I agonists and their use to treat dyslipidemic disorders
The present invention provides peptides and peptide analogues that mimic the structural and pharmacological properties of human ApoA-I. The peptides and peptide analogues are useful to treat a variety of disorders associated with dyslipidemia.
Owner:DASSEUX JEAN LOUIS +5
Methods and systems for administering an appropriate pharmacological treatment to a patient for managing epilepsy and other neurological disorders
InactiveUS20070287931A1Reduced magnitudeShorten the durationElectroencephalographyBiocidePharmacometricsNeurological disorder
The present invention provides systems and methods for managing epilepsy. In one embodiment, a method of the present invention characterize a patient's propensity for a future epileptic seizure and facilitates administration of a pharmacological agent. The dosage of the pharmacological agent is typically a function of at least one of the patient's propensity for the future epileptic seizure and time period to seizure.
Owner:CYBERONICS INC
Cinnamide compound
The present invention relates to a compound represented by Formula (I):
(wherein Ar1 represents an imidazolyl group which may be substituted with 1 to 3 substituents; Ar2 represents a pyridinyl group, a pyrimidinyl group, or a phenyl group which may be substituted with 1 to 3 substituents; X1 represents (1) —C≡C— or (2) a double bond etc. which may be substituted; R1 and R2 represent, for example, a C1-6 alkyl group or C3-8 cycloalkyl group which may be substituted)
or a pharmacologically acceptable salt thereof and to the use thereof as pharmaceutical agents. The object of the present invention is to find a therapeutic or preventive agent for diseases caused by Aβ. According to the present invention, a therapeutic or preventive agents for diseases caused by Aβ can be provided.
Owner:EISIA R&D MANAGEMENT CO LTD
Systems and methods for characterizing a patient's propensity for a neurological event and for communicating with a pharmacological agent dispenser
InactiveUS20070149952A1Selectively limit accessSelectively limit to administrationDrug and medicationsTelemedicinePharmacometricsAntiepileptic drug
The present invention provides systems and methods for managing intake of a pharmacological agent. In one method of the present invention, the systems and methods are for controlling intake of an anti-epileptic drug. In such embodiments, one or more signals from a patient are processed to predict an onset of a seizure. Upon the prediction of the seizure, the patient is allowed to access the pharmacological agent in a pharmacological agent dispenser.
Owner:CYBERONICS INC
Mucoadhesive drug delivery devices and methods of making and using thereof
ActiveUS20050196440A1Improve drug absorptionPromote resultsPowder deliveryOrganic active ingredientsActive agentSolvent
The present invention relates to mucoadhesive drug delivery devices and their methods of preparation and use. More specifically the present invention relates to mucoadhesive drug delivery devices comprising one or more biocompatible purified proteins combined with one or more biocompatible solvents and one or more mucoadhesive agents. The mucoadhesive drug delivery devices may also include one or more pharmacologically active agents. The drug delivery devices of the present invention adhere to mucosal tissue, thereby providing a vehicle for delivery of the pharmacologically active agent(s) through such tissue.
Owner:PETVIVO HLDG INC
Engineering absorption of therapeutic compounds via colonic transporters
Methods of modifying therapeutic compounds such as drugs to be substrates for active transporters expressed in epithelial cells lining the lumen of the human colon are disclosed. The transporters expressed in the human colon include the sodium dependent multi-vitamin transporter (SMVT), and monocarboxylate transporters 1 and 4 (MCT 1 and MCT 4). The modified compounds can themselves be pharmacologically active, or upon cleavage of a chemical moiety after uptake from the colon, can be metabolized to form a compound that is pharmacologically active (e.g., a prodrug). The modified compounds disclosed herein are suitable for use in extended release oral dosage forms, particularly those that release drug over periods of greater than about 2-4 hours following administration.
Owner:XENOPORT
Method of treating contrast-induced nephropathy
InactiveUS20120122844A1Treating and preventing and ameliorating contrast-induced nephropathyImprove the level ofBiocideOrganic chemistryNephrosisActive agent
The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I:
wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.
Owner:NOVARTIS AG
Sulfonamide-containing heterocyclic compounds
The present invention provides a sulfonamide- or sulfonylurea-containing heterocyclic compounds. Specifically, it provides a heterocyclic compound represented by the formula (I), a pharmacologically acceptable salt thereof or a hydrate of them.In the formula, A is hydrogen atom, a halogen atom, a C1-C4 alkyl or alkoxy group which may be substituted with a halogen atom, or cyano group; B is an optionally substituted aryl group or monocyclic heteroaryl group, or:(wherein, the ring Q is an aromatic ring which may have nitrogen atom; and the ring M is a ring sharing a double bond with the ring Q, which ring may have a heteroatom; and the rings Q and M may share nitrogen atom); K is a single bond; T, W, X and Y are the same as or different from each other and each is =C(D)- (wherein, D is hydrogen or a halogen atom) or nitrogen atom; U and V are the same as or different from each other and each is =C(D)-, nitrogen atom, -CH2-, oxygen atom or -CO-; Z is a single bond or -CO-NH-; and R1 is hydrogen atom, etc.
Owner:EISIA R&D MANAGEMENT CO LTD
Pyrazole compounds and their use as antidiabetes agents
The present invention provides a pyrazole compound that has liver glycogen phosphorylase inhibitory activity and is useful as a therapeutic or prophylactic agent for diabetes, the pyrazole compound represented by the following general formula (I): wherein Ring Q represents an aryl or heteroaromatic group, R1 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group or a C1-6 alkoxy group, R2 represents a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or an azido group, R3 represents a halogen atom, a hydroxyl group, a C1-6 alkyl group, a halo C1-6 alkyl group, a C1-6 alkoxy group, an azido group, an amino group, an acylamino group or a C1-6 alkylsulfonylamino group, R4 and R5 are identical with or different from each other and represent a hydrogen atom, a substituted or unsubstituted C1-6 alkyl group, a C3-8 cycloalkyl group, a substituted or unsubstituted saturated heterocyclic group, a substituted or unsubstituted aryl group, a C7-14 aralkyl group, a heteroaromatic group, or the like, or a pharmacologically acceptable salt thereof.
Owner:JAPAN TOBACCO INC
Method and system for screening compounds for muscular and/or neurological activity in animals
Screening methods and instrumentation for candidate pharmacological agents are applied to discover compounds with muscular and / or neurological activity. The method comprises the use of teleost fish, such as the medaka (Oryzias latipes), which may be stimulated with chemical agents or an electric field to produce, for example, seizure activity and / or convulsive activity. The convulsive behavior may be recorded optically and electrically. Antagonism of the convulsive behavior is produced by application of candidate pharmacological agents to the well containing the fish. The method may include stimulation and antagonism in a plurality of sample wells with a repetitive or simultaneous application of threshold electric fields. The methods and instrumentation can be applied to the study of other serious neurological diseases such as neuropathic pain. In addition the process of assaying the protection of animals to convulsant agents the assay measures pharmacological safety parameters including sedation and cognitive impairment.
Owner:MURPHY RANDALL +1
Medicament for treatment of dermal pigmentation
InactiveUS20070042997A1Inhibit dermal pigmentationLow toxicityBiocideOrganic chemistryPharmacometricsBackbone chain
A medicament for preventive and/or therapeutic treatment of dermal pigmentation and/or development of skin cancer, which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof:
wherein X represents a connecting group whose number of atoms in a main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a heteroaryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above.
Owner:INST OF MEDICINAL MOLECULAR DESIGN
Gel compositions for topical administration
Pharmaceutical gel compositions containing pharmacologically active agent for topical administration, as well as a method of making the same, are disclosed.Owner:APTALIS PHARMA
Preventives or remidies for alzheimer's disease or amyloid protein fibrosis inhibitors containing nitrogen-containing heteroaryl compounds
InactiveUS20050054732A1Powerful activityImprove securityBiocideNervous disorderFibrosisBULK ACTIVE INGREDIENT
The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors:
(where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).
Owner:BTG INT LTD
Excipient removal from pharmacological samples
InactiveUS20140319077A1Easy to separateSolvent extractionWater/sewage treatment with mechanical oscillationsPharmaceutical drugPharmacometrics
Active pharmaceutical ingredients can be separated from their excipients by dissolving a pharmaceutical product (e.g. tablet, pill) into a solvent, then running the solution through an acoustophoretic device. Standing waves are used to separate the excipient from the active ingredient dissolved in the solvent.
Owner:FLODESIGN SONICS
Cyclic compounds
InactiveUS20040142930A1Strong inhibitory activityLess side effectsBiocideGroup 5/15 element organic compoundsArylAlkoxy group
1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is =CH- or =N-, Y is -NH-, -NR<4>-, -S-, -O-, -CH=N-, -N=CH-, -N=N-, -CH=CH-, etc., R<1 >is a lower alkoxy group, an amino group, a heterocyclic ring containing N atom(s), or a hydroxy group substituted by a heterocyclic ring containing N atom(s) (each of which is optionally substituted), R<2 >is a lower alkylamino group which is optionally substituted by an aryl group, a lower alkoxy group which is optionally substituted by an aryl group, a lower alkoxy group substituted by an aromatic heterocyclic ring containing N atom(s), R<3 >is an aryl group, a heterocyclic ring containing N atom(s), a lower alkyl group, a lower alkoxy group, a cyclo lower alkoxy group, a hydroxy group substituted by a heterocyclic ring containing N atom(s), or an amino group (each of which is optionally substituted), and R<3 >and a substituent in Y may be combined to form a lactone ring. The compound of the present invention has excellent selective PDE V inhibitory activity and therefore, is useful as a therapeutic or prophylactic drug for treating various diseases due to functional disorders on cGMP-signaling.
Owner:MITSUBISHI TANABE PHARMA CORP
Dosing regimens for the treatment of lysosomal storage diseases using pharmacological chaperones
The present invention provides dosing regimens for administering pharmacological chaperones to a subject in need thereof. The dosing regimens can be used to treat disorders caused by improper protein misfolding, such as lysosomal storage disorders.
Owner:AMICUS THERAPEUTICS INC
Highly concentrated stable meloxicam solutions for needleless injection
Aqueous cyclodextrin-free solution of meloxicam suitable for administration by needleless injection, containing a pharmacologically acceptable meloxicam salt of an organic or inorganic base and one or more suitable excipients, the content of dissolved meloxicam salt being from 35 to 100 mg / ml. The formulation according to the invention has a shelf-life of up to 24 months or more.Owner:FOLGER MARTIN ANDREAS +3
Triphenylalkene derivatives and their use as selective estrogen receptor modulators
InactiveUS6576645B1Efficient productionSufficient amountBiocideNervous disorderHalogenStereoisomerism
The invention provides novel selective estrogen receptor modulator compounds of the general formula:wherein R1 and R2, which are the same or different area) H, halogen, OCH3, OH; or where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, -CH2C=CH or -CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; orc) -Y-(CH2)nCH2-O-R6where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, -CH2CH2OH, or -CH2CH2Cl; ord) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; andR3 is H, halogen, OH or -OCH3;stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.
Owner:FORENDO PHARMA LTD
Multi-cyclic compounds
InactiveUS20090062529A1Proceed efficientlyValid conversionNervous disorderOrganic chemistryPolycyclic compoundPharmacometrics
A compound represented by the formula (I):or a pharmacologically acceptable salt thereof, wherein Ar1 represents an imidazolyl group or the like which may be substituted with a C1-6 alkyl group, Ar2 represents a phenyl group or the like which may be substituted with a C1-6 alkoxy group, X1 represents a double bond or the like and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, is effective as a therapeutic or prophylactic agent for a disease caused by Aβ.
Owner:EISIA R&D MANAGEMENT CO LTD
Method for the treatment of fabry disease using pharmacological chaperones
InactiveUS20100113517A1High activityHigh protein activityBiocidePeptide/protein ingredientsPharmacometricsCytoplasmic staining
The present invention provides a method treating a patient with Fabry disease by determining whether there is an improvement of a surrogate marker that is associated with Fabry disease following administration of a specific pharmacological chaperone of α-galactosidase A. The method includes administering an effective amount of 1-deoxygalactonojirimycn to the individual, wherein the 1-deoxygalactonojirimycin binds to alpha-galactosidase A in an amount effective to increase activity of the alpha-galactosidase A. The present invention also provides a method for monitoring and increasing a therapeutic response of a patient with Fabry disease following administration of a specific pharmacological chaperone of α-galactosidase A by evaluating the effect on the cytoplasmic staining pattern of a cell from the patient, wherein detection of a staining pattern in the cell that is similar to the staining pattern in a cell from a healthy individual indicates that the individual with Fabry disease is a responder.
Owner:AMICUS THERAPEUTICS INC
Indole derivative, and pharmacologically acceptable salt thereof
The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism:wherein A represents a pyridine ring, a furan ring, or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents —C(═O)—NH—SO2R6, an acidic 5-membered hetero ring group, or the like; R2 represents an optionally substituted phenyl group, an optionally substituted 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], and a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.
Owner:KISSEI PHARMA
Process to prepare clopidogrel
InactiveUS6635763B2Increased cost-effectivenessOrganic chemistryThienopyridine DerivativesPharmacometrics
The present invention relates to a process for the preparation of thieno[3,2-c]pyridine derivatives having pharmacologically significant anti-aggregating and anti-thrombotic properties.
Owner:CADILA HEALTHCARE LTD
Chimeric fibroblast growth factors with altered receptor specificity
The present invention is directed to novel chimeric fibroblast growth factor (FGF) polypeptides, novel DNA encoding chimeric FGF polypeptides, and to the recombinant production of chimeric FGF polypeptides, and to methods, compositions and assays utilizing chimeric FGF polypeptides for the therapeutic treatment of metabolic-related disorders and other conditions, and for producing pharmaceutically active compositions including chimeric FGF polypeptides, the compositions having therapeutic and pharmacologic properties including those associated with the treatment of metabolic-related disorders and other conditions.
Owner:F HOFFMANN LA ROCHE & CO AG
Methods of screening for pharmacologically active compounds for the treatment of tumour diseases
InactiveUS6383733B1Growth inhibitionInhibit transferPeptide/protein ingredientsGenetic material ingredientsDiseaseFibroblast
Pharmaceutical compositions containing as active compound a substance which inhibits the activity of TGFbeta on tumour cells of epithelial origin, for the treatment of epithelial, invasive tumour diseases which are characterized by a reversible transition of the cells from an epithelial, non-invasive state into a fibroblastoid, invasive state. The pharmaceutical composition contains a TGFbeta inhibitor, preferably combined with an Ras inhibitor. Process for screening substances for the treatment of epithelial, invasive tumour diseases.
Owner:BOEHRINGER INGELHEIM INT GMBH
Dosing regimens for the treatment of lysosomal storage diseases using pharmacological chaperones
The present invention provides dosing regimens for administering pharmacological chaperones to a subject in need thereof. The dosing regimens can be used to treat disorders caused by improper protein misfolding, such as lysosomal storage disorders.
Owner:AMICUS THERAPEUTICS INC
Methods of treating fabry disease in patients having the G9331A mutation in the GLA gene
ActiveUS10537564B2Metabolism disorderPharmaceutical delivery mechanismPharmacometricsPharmacological chaperone
Provided are methods of treating a patient diagnosed with Fabry disease and methods of enhancing α-galactosidase A in a patient diagnosed with or suspected of having Fabry disease. Certain methods comprise administering to a patient a therapeutically effective dose of a pharmacological chaperone for α-galactosidase A, wherein the patient has a splice site mutation in intron 4 of the nucleic acid sequence encoding α-galactosidase A. Also described are uses of pharmacological chaperones for the treatment of Fabry disease and compositions for use in the treatment of Fabry disease.
Owner:BPCR LLP
Combination of an oxidant, a photosensitizer and a wound healing agent for oral disinfection and treatment of oral disease
ActiveUS8685466B2Enhancing and accelerating dispersion of lightImprove responseAntibacterial agentsOrganic active ingredientsOral diseaseDisease
The present document describes methods of use of photo activated compositions for oral disinfection and / or treatments which comprise at least one oxidant, at least one photoactivator capable of activating the oxidant, and at least one healing factor chosen from hyaluronic acid, glucosamine and allantoin, in association with a pharmacologically acceptable carrier.
Owner:FLE INT SRL
Pharmacological profiling of drugs with cell-based assays
InactiveUS20060040338A1Enable optimizationBioreactor/fermenter combinationsCompound screeningPost translationalAssay
The instant invention provides a method for establishing safety profiles for chemical compounds, as well as pharmacological profiling said method comprising (A) testing the effects of said chemical compounds on the amount and/or post-translational modifications of two or more macromolecules in intact cells; (B) constructing a pharmacological profile based on the results of said tests; and (C) comparing said profile to the profile(s) of drugs with established safety characteristics. Additionally, the invention is also directed to a composition comprising an assay panel, said panel comprising at least one high-content assay for the amount and/or post-translational modification of a protein and at least one high-content assay for the amount and/or subcellular location of a protein-protein interaction.
Owner:ODYSSEY THERA INC
Co-Administration of an Agent Linked to an Internalization Peptide with an Anti-Inflammatory
ActiveUS20090176713A1Reduce capacityInhibit the inflammatory responseOrganic active ingredientsNervous disorderCo administrationBiotin
The invention provides methods of delivering pharmacologic agents linked to an internalization peptide, in which an inflammatory response inducible by the internalization peptide is inhibited by co-administration of an anti-inflammatory or by linking the internalization peptide to biotin or similar molecule. Such methods are premised in part on the results described in the examples whereby administration of a pharmacological agent linked to tat high dosages is closely followed by an inflammatory response, which includes mast cell degranulation, histamine release and the typical sequelae of histamine release, such as redness, heat, swelling, and hypotension.
Owner:NONO INC
Pyrazine derivatives
InactiveUS7273868B2Strong inhibitory activityLess side effectsBiocideGroup 5/15 element organic compoundsDiseasePyrazine
1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof,wherein X is ═CH— or ═N—,Y is —NH—, —NR4—, —S—, —O—, —CH═N—, —N═CH—,—N═N—, —CH═CH—, etc., R1 is a lower alkoxy group, an amino group, a heterocyclic ring containing N atom(s), or a hydroxy group substituted by a heterocyclic ring containing N atom(s) (each of which is optionally substituted), R2 is a lower alkylamino group which is optionally substituted by an aryl group, a lower alkoxy group which is optionally substituted by an aryl group, a lower alkoxy group substituted by an aromatic heterocyclic ring containing N atom(s), R3 is an aryl group, a heterocyclic ring containing N atom(s), a lower alkyl group, a lower alkoxy group, a cyclo lower alkoxy group, a hydroxy group substituted by a heterocyclic ring containing N atom(s), or an amino group (each of which is optionally substituted), and R3 and a substituent in Y may be combined to form a lactone ring. The compound of the present invention has excellent selective PDE V inhibitory activity and therefore, is useful as a therapeutic or prophylactic drug for treating various diseases due to functional disorders on cGMP-signaling.
Owner:MITSUBISHI TANABE PHARMA CORP
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