The present invention is a formulation for oxygen delivery for organ preservation comprising a scalable stabilized nanoemulsion, and a method for using it. The nanoemulsion embraces a hydrocarbon lipid; a fluorocarbon or perfluorocarbon; water; a nonionic surfactant; and optionally a quaternary ammonium compound, so that droplets of the nanoemulsion have a droplet size of from about 90 nm to about 120 nm and wherein the diameter of the droplets does not change by more than 20% upon storage for at least 12 months.
A01N 1/126 - Agents physiologiquement actifs, p. ex. antioxydants ou nutriments
G01N 21/359 - CouleurPropriétés spectrales, c.-à-d. comparaison de l'effet du matériau sur la lumière pour plusieurs longueurs d'ondes ou plusieurs bandes de longueurs d'ondes différentes en recherchant l'effet relatif du matériau pour les longueurs d'ondes caractéristiques d'éléments ou de molécules spécifiques, p. ex. spectrométrie d'absorption atomique en utilisant la lumière infrarouge en utilisant la lumière de l'infrarouge proche
G01N 33/483 - Analyse physique de matériau biologique
The present invention is a specialized application of a system of GAN (“Generative Adversarial Network”) and image classifier technology in combination with automated or semi-automated submersible drones that can access coral reefs to photograph or image them, to capture the necessary data to prognose reef health. The present technology realizes for the first time that coral health analysis requires at least four-time element image collection—“past healthy coral;” “past compromised coral;” current status quo images from a first point in time of a reef to be monitored; and at least a second status quo image at a second point in time of the same reef. Critical to the method and device(s) of the invention is the use of a data augmentation tool to reach a “reasonably realistic” GAN-generated images of past healthy, past bleaching and past dead coral, together with prescribed standardized lighting protocols for reef photography.
H04N 23/56 - Caméras ou modules de caméras comprenant des capteurs d'images électroniquesLeur commande munis de moyens d'éclairage
H04N 23/695 - Commande de la direction de la caméra pour modifier le champ de vision, p. ex. par un panoramique, une inclinaison ou en fonction du suivi des objets
The present invention is an improvement in Lipid Nanoparticles (LNPs) for re-routing their distribution from the liver and spleen (the non-target organs) to hard-to-deliver targets such as the brain and other tissues for drug delivery. Specifically, the invention derivatizes or otherwise modifies LNPs to provide the surface or constituency thereof with “Ionic Liquid” (IL) so that the IL-LNP incorporates an ionizable lipid such as a cationic ionizable lipid, an optional helper lipid, cholesterol and a (true) ionic liquid component. Among other benefits of the inclusion of “Ionic Liquid” is to decrease the delivery of LNPs to the body's filtering organ—the liver—and thereby re-route delivery to other target organs.
A61K 9/1272 - Liposomes non conventionnels, p. ex. liposomes modifiés par un PEG ou liposomes enduits de ou greffés avec des polymères comprenant des agents tensioactifs non phosphatidyliques comme substances formant des bicouches, p. ex. lipides cationiques ou liposomes non phosphatidyliques enduits de ou greffés avec des polymères
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
The present invention is a personal security method and a writer's tool, in two or three modules, that assures generation of text by a user which cannot be identified has having been written by said user. The present invention uses Large Language Modules (LLMs such as but not limited to ChatGPT) principally to generated the document. Using an LLM together with the two or three modules of the present invention side-steps the author's (user's) features entirely by having the LLM generate the text, creating an authorship opaque document, and thus concealing and securing the identity of the writer.
The instant document converter transforms any text or text-predominant document, virtually immediately and automatically, to a list containing solely its culled, formatted references, together with one or more coordinated executables that launch the culled formatted references as a search query, when triggered, to a search engine for verification analysis.
A method of inhibiting M2-like macrophages in a patient is provided comprising administering to a patient having ovarian cancer a therapeutically effective amount of a FRB-transported C1 inhibitor compound having selective efficacy to FRβ expressing tumor cells. The method includes wherein the FRB-transported C1 inhibitor compound is a substituted pyrrolo[2,3-d]pyrimidine antifolate inhibitor compound having selective efficacy to FRβ expressing tumor cells. The present invention provides a method for targeting both the tumor and the tumor microenvironment with the FRB-transported C1 inhibitor compounds.
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
The present invention is a ready-delivery oral dosage form for laboratory animals, for the testing of candidate active agents, that meets a number of design parameters. First, the oral dosage form is chewable but neither fragile nor sticky, so it does not fall apart or scatter in the living space in which it is administered—but also cannot become lodged in the animal's teeth or mouth. Second, the palatability profile is greater than the ordinary animal feed (such as rodent chow and so forth) and therefore will be consumed immediately and preferentially, when administered, prior to any other available food. Finally, the oral dosage form must be readily compounded such as with an automated tablet press without the need to add heat or volatile solvents, with inclusion of active agent added followed by optional refrigeration prior to administration.
A compound having the structure of AGN5 or AGN11
A compound having the structure of AGN5 or AGN11
A compound having the structure of AGN5 or AGN11
is provided. A composition comprising either AGN5 or AGN11 and a pharmaceutically acceptable carrier is provided. A method of treating a patient having dementia with Lewy Bodies, Parkinson's Disease, and Alzheimer Disease with Lewy Bodies comprising administering to said patient a therapeutically effective amount of the compound AGN5, AGN11, or the composition comprising AGN5 or AGN11 and a pharmaceutically acceptable carrier.
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p. ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
11.
Design, Synthesis, and Structure-Activity Relationships of Substituted Pyrido[3,2-d]Pyrimidines as Microtubule Targeting Agents and Anti-Cancer Agents
A compound is provided having a structure of the formula:
A compound is provided having a structure of the formula:
A compound is provided having a structure of the formula:
wherein Ar is a structure of the formula including at least one of 2, 3, 4, 6, 7, 8, or 9:
A compound is provided having a structure of the formula:
wherein Ar is a structure of the formula including at least one of 2, 3, 4, 6, 7, 8, or 9:
A compound is provided having a structure of the formula:
wherein Ar is a structure of the formula including at least one of 2, 3, 4, 6, 7, 8, or 9:
A compound having the formula
A compound is provided having a structure of the formula:
wherein Ar is a structure of the formula including at least one of 2, 3, 4, 6, 7, 8, or 9:
A compound having the formula
A compound is provided having a structure of the formula:
wherein Ar is a structure of the formula including at least one of 2, 3, 4, 6, 7, 8, or 9:
A compound having the formula
is also provided.
A compound is provided having a structure of the formula:
wherein Ar is a structure of the formula including at least one of 2, 3, 4, 6, 7, 8, or 9:
A compound having the formula
is also provided.
Compositions are provided that include one or more of these compounds and a pharmaceutically acceptable vehicle. A method of treating a patient having cancer is provided that includes administering to said patient a therapeutically effective amount of one or more of these compounds or these compositions for treating said patient.
The present invention is a modular electromechanical system for proctoring an online examination, as to a test-taker at a remote computer location, incorporating modules which collect and compare only motion-detected biometrics. The modules of the system include a computer keyboard or equivalent input device, a User Registration Database, a module for motion sensing (during testing) and data transmission that populates a Motion Capture Database, and a compiler for comparing or contrasting the User Registration Database and the Motion Capture Database, with the compiler's rendering its analytical data to a Secure Compilation Database Storage with User Output. The User Registration Database is populated in advance of the test to be proctored, in a secure setting.
G09B 7/02 - Dispositifs ou appareils d'enseignement à commande électrique procédant par questions et réponses du type où l'élève doit donner une réponse à la question posée, ou bien où la machine donne une réponse à la question posée par l'élève
In aspects, the present disclosure provides methods for quantifying microorganisms. In aspects, the present disclosure provides methods for identifying microorganisms. In aspects, the present disclosure provides methods of analyzing food. In aspects, the present disclosure provides methods of treating a human subject having an infection. In aspects, the present disclosure provides methods of analyzing environmental samples.
C12Q 1/04 - Détermination de la présence ou du type de micro-organismeEmploi de milieux sélectifs pour tester des antibiotiques ou des bactéricidesCompositions à cet effet contenant un indicateur chimique
G06T 7/62 - Analyse des attributs géométriques de la superficie, du périmètre, du diamètre ou du volume
G06V 10/82 - Dispositions pour la reconnaissance ou la compréhension d’images ou de vidéos utilisant la reconnaissance de formes ou l’apprentissage automatique utilisant les réseaux neuronaux
G06V 20/69 - Objets microscopiques, p. ex. cellules biologiques ou pièces cellulaires
The present invention is a composition, and a method for making and administering, a pharmaceutical in unit dosage form in which mitochondria-enriched extracellular vesicles are delivered, “as is” or with an optional suitable carrier, after increasing the mitochondria content of the vesicles by generating the vesicles from a human brain endothelial cell line in the presence of one or more suitable promoting agents. Such mitochondria-enriched vesicles are effective to treat tissues needing amelioration of mitochondrial dysfunction or boosting of mitochondrial function. The EVs intrinsically are able to cross the blood-brain barrier and thus are particularly well suited for treating compromised tissues of the brain in situ. as well as other tissues under stress and in need of treatment not limited to neurologic tissues, and are typically administered parenterally.
A61K 9/127 - Vecteurs à bicouches synthétiques, p. ex. liposomes ou liposomes comportant du cholestérol en tant qu’unique agent tensioactif non phosphatidylique
A61P 9/10 - Médicaments pour le traitement des troubles du système cardiovasculaire des maladies ischémiques ou athéroscléreuses, p. ex. médicaments antiangineux, vasodilatateurs coronariens, médicaments pour le traitement de l'infarctus du myocarde, de la rétinopathie, de l'insuffisance cérébro-vasculaire, de l'artériosclérose rénale
A method of inhibiting M2-like macrophages in a patient is provided comprising administering to a patient having ovarian cancer a therapeutically effective amount of a FRβ-transported C1 inhibitor compound having selective efficacy to FRβ expressing tumor cells. The method includes wherein the FRβ-transported C1 inhibitor compound is a substituted pyrrolo[2,3-d]pyrimidine antifolate inhibitor compound having selective efficacy to FRβ expressing tumor cells. The present invention provides a method for targeting both the tumor and the tumor microenvironment with the FRβ-transported C1 inhibitor compounds.
A compound of the Formula I and optionally a pharmaceutically acceptable salt thereof is provided:
A compound of the Formula I and optionally a pharmaceutically acceptable salt thereof is provided:
A compound of the Formula I and optionally a pharmaceutically acceptable salt thereof is provided:
Formula I, wherein, R is one selected from the group consisting of H and CH3; n is an integer 4 when X is -CH2- and Ar is 1,4-phenyl, or n is an integer ranging from 1 to 4 when X is -CH2-and Ar is either 2'-fluoro-1,4-phenyl or 2,5-thienyl, or n is an integer ranging from 1 to 4 when X is one selected from the group consisting of O, S, -NH-, -NHCHO-, -NHCOCH3-, and -NHCOCF3- and Ar is one selected from the group consisting of (a) 1,4-phenyl, (b) 2'-fluoro-1,4-phenyl, and (c) 2,5-thienyl, or n is an integer 3 when X is -CH2-, R is CH3 and Ar is 1,4-phenyl.
UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION (USA)
DUQUESNE UNIVERSITY OF THE HOLY SPIRIT (USA)
Inventeur(s)
Kellum, Jr., John Alston
Edgar, Robert Hugh
White, Cierra Lynn
Viator, John, Andrew
Hempel, John D.
Abrégé
A method of determining antibiotic resistance of bacteria includes dividing a sample including the bacteria into a plurality of sub-samples, mixing labeling: agents with each of the plurality of sub-samples. Each of the labeling agents is detectible via a detection system including a sensor to detect photoacoustic waves. The labeling: agents are further active to selectively bind with the bacteria. The method further includes applying an antibiotic to one or more of the plurality of sub-samples and not to one or more others of the plurality of sub- samples, characterizing at least one of the sub- samples to which the antibiotic has been applied and at least one of the sub-samples to which no antibiotic has been applied after a determined period of time via the detection system, and determining antibiotic resistance of the bacteria on the basis of the characterization via the detection system.
In aspects, the present disclosure provides methods for quantifying microorganisms. In aspects, the present disclosure provides methods for identifying microorganisms. In aspects, the present disclosure provides methods of analyzing food. In aspects, the present disclosure provides methods of treating a human subject having an infection. In aspects, the present disclosure provides methods of analyzing environmental samples.
C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques
G01N 33/569 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour micro-organismes, p. ex. protozoaires, bactéries, virus
19.
Implantable Device Coated by a Self-Assembled Monolayer and Therapeutic Agent
A61K 31/7076 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées contenant des purines, p. ex. adénosine, acide adénylique
20.
MICRO RNA INTERACTIONS AS THERAPEUTIC TARGETS FOR COVID-19 AND OTHER VIRAL INFECTIONS
Provided is an agent that binds to a SARS-CoV-2 s2m motif, a SARS-CoV-2 3'-UTR Terminus, or a SARS-CoV-2 DIS-s2m extended sequence. Provided is a method of treating an infection in a subject, comprising: administering a therapeutically effective amount of the agent to the subject. In some embodiments, the infection is SARS-CoV-2 infection.
Provided is an agent that binds to a SARS-CoV-2 s2m motif, a SARS-CoV-2 3′-UTR Terminus, or a SARS-CoV-2 DIS-s2m extended sequence. Provided is a method of treating an infection in a subject, comprising: administering a therapeutically effective amount of the agent to the subject. In some embodiments, the infection is SARS-CoV-2 infection.
41 - Éducation, divertissements, activités sportives et culturelles
Produits et services
Educational services, namely, providing courses of instruction at the undergraduate, graduate, and professional levels in the fields of medicine, pharmacology, biomedical sciences, and health and wellness, and distributing course materials in connection therewith; medical training and teaching; clinical education services, namely, providing mentoring, tutoring, classes, seminars and workshops in the fields of medicine, pharmacology, biomedical sciences, and health and wellness; conducting educational seminars, lectures, and educational conferences relating to medicine, health, and wellness for professionals and the public
23.
DUQUESNE UNIVERSITY COLLEGE OF OSTEOPATHIC MEDICINE
41 - Éducation, divertissements, activités sportives et culturelles
Produits et services
Educational services, namely, providing courses of instruction at the undergraduate, graduate, and professional levels in the fields of medicine, pharmacology, biomedical sciences, and health and wellness, and distributing course materials in connection therewith; medical training and teaching; clinical education services, namely, providing mentoring, tutoring, classes, seminars and workshops in the fields of medicine, pharmacology, biomedical sciences, and health and wellness; conducting educational seminars, lectures, and educational conferences relating to medicine, health, and wellness for professionals and the public
41 - Éducation, divertissements, activités sportives et culturelles
Produits et services
Educational services, namely, providing courses of instruction at the undergraduate, graduate, and professional levels in the fields of medicine, pharmacology, biomedical sciences, and health and wellness, and distributing course materials in connection therewith; medical training and teaching; clinical education services, namely, providing mentoring, tutoring, classes, seminars and workshops in the fields of medicine, pharmacology, biomedical sciences, and health and wellness; conducting educational seminars, lectures, and educational conferences relating to medicine, health, and wellness for professionals and the public
25.
AN RNA G-QUADRUPLEX STRUCTURE IN PRE-miRNA-1229 AS A THERAPEUTIC TARGET FOR ALZHEIMER'S DISEASE AND VARIOUS CANCERS
Provided is an agent that binds to a wild type or variant pre-miRNA-1229 comprising a G-quadruplex (GQ) structure, wherein binding of the agent to the wild type or variant pre-miRNA-1229 stabilizes the GQ structure of the wild type or variant pre-miRNA-1229. In some embodiments, the variant is rs2291418. Provided is a method of treating a disease in a subject, comprising: administering a therapeutically effective amount of the agent to the subject. In some embodiments, the disease is Alzheimer's disease, cancer or coronary artery calcification.
University of Pittsburgh—Of the Commonwealth System of Higher Education (USA)
Duquesne University of the Holy Spirit (USA)
Inventeur(s)
Kellum, John Alston
Hempel, John D.
Edgar, Robert Hugh
Viator, John Andrew
Abrégé
A method of detecting a species, strain or type of bacteria includes mixing a labeled bacteriophage including a label that is detectible via a detection system with a bacterial culture including the species, strain or type of bacteria to which the labeled bacteriophage selectively binds and using the detection system to detect the labeled bacteriophage bound to the species, strain or type of bacteria.
C12Q 1/04 - Détermination de la présence ou du type de micro-organismeEmploi de milieux sélectifs pour tester des antibiotiques ou des bactéricidesCompositions à cet effet contenant un indicateur chimique
A compound of Formula II, or optionally a salt or a hydrate of the compound of Formula II is provided:
b is either a hydrogen or an alkyl group having from one to six carbon atoms, an aryl group, a heteroaryl group, and a halogen; R is an alkyl group having from one to six carbon atoms; and Ar is selected from the group consisting of an alkyl group having from one to six carbon atoms, a substituted aryl, and a substituted heteroaryl.
This invention provides substituted bicyclic pyrimidine compounds of the following formula:
or a pharmaceutically acceptable salt thereof, wherein R is selected from the group consisting of a straight or a branched chain alkyl group having from 1 to 10 carbon atoms, wherein the alkyl group is partially or completely saturated. Methods of treating a patient diagnosed with cancer are disclosed comprising administering to the patient a therapeutically effective amount of the substituted bicyclic pyrimidine compounds, or a pharmaceutically acceptable salt thereof.
The present invention provides substituted pyrrolo-, furano-, and cyclopentylpyrimidine bicyclic pharmaceutical compositions comprising compounds of Formula IV,
and pharmaceutically acceptable salts, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds and pharmaceutical compositions for treating tumor cells and inhibiting mitosis of cancerous cells.
C07D 491/048 - Systèmes condensés en ortho avec un seul atome d'oxygène comme hétéro-atome du cycle contenant de l'oxygène le cycle contenant de l'oxygène étant à cinq chaînons
C07D 239/70 - Composés hétérocycliques contenant des cycles diazine-1, 3 ou diazine-1, 3 hydrogéné condensés avec des carbocycles ou avec des systèmes carbocycliques
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
A61P 35/04 - Agents anticancéreux spécifiques pour le traitement des métastases
C12Q 1/6886 - Produits d’acides nucléiques utilisés dans l’analyse d’acides nucléiques, p. ex. amorces ou sondes pour les maladies provoquées par des altérations du matériel génétique pour le cancer
30.
First-in-class of SHMT2 and MTHFD2 inhibitors as antitumor agents
Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.
C07D 491/048 - Systèmes condensés en ortho avec un seul atome d'oxygène comme hétéro-atome du cycle contenant de l'oxygène le cycle contenant de l'oxygène étant à cinq chaînons
2/n) is smaller than a second predetermined threshold then author i cannot be the correct author; or if no author garners significantly more votes than all other contenders then none of the named authors is the author of a document in question—in a number of novel applications. Personality profiling and authorship attribution may also be used to verify user identity to a computer.
The present invention discloses a compound of the formula:
2 or O, and optionally comprising a pharmaceutically acceptable salt or hydrate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt or hydrate thereof.
A61K 31/343 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à cinq chaînons avec un oxygène comme seul hétéro-atome d'un cycle, p. ex. isosorbide condensés avec un carbocycle, p. ex. coumarane, bufaralol, béfunolol, clobenfurol, amiodarone
C07D 403/02 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles
A61K 31/505 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime
C07D 405/02 - Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle contenant deux hétérocycles
A61K 31/4709 - Quinoléines non condensées contenant d'autres hétérocycles
The present invention discloses a compound of the formula:
and optionally comprising a pharmaceutically acceptable salt or hydrate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt or hydrate thereof.
A61K 31/343 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à cinq chaînons avec un oxygène comme seul hétéro-atome d'un cycle, p. ex. isosorbide condensés avec un carbocycle, p. ex. coumarane, bufaralol, béfunolol, clobenfurol, amiodarone
C07D 403/02 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles
A61K 31/505 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime
C07D 405/02 - Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle contenant deux hétérocycles
A61K 31/4709 - Quinoléines non condensées contenant d'autres hétérocycles
UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION (USA)
DUQUESNE UNIVERSITY OF THE HOLY SPIRIT (USA)
Inventeur(s)
Pacella, John, J.
Gawalt, Ellen, S.
Romeo, Jared
Abrégé
An implantable device includes a body configured to be implanted within a body of a patient and a self-assembled monolayer. The self-assembled monolayer includes molecules having a first portion (moiety) bonded to a surface of the body, a second portion (moiety) opposite the first portion, and a linkage portion (moiety) extending between the first portion and the second portion. The implantable device also includes a therapeutic agent having at least one therapeutic molecule covalently bonded to the second portion of the molecules of the self-assembled monolayer. A method of preparing the implantable device and a method for deploying the implantable device within a vascular system of a patient are also provided.
A61K 47/00 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif
A61P 9/00 - Médicaments pour le traitement des troubles du système cardiovasculaire
A compound of Formula II, or optionally a salt or a hydrate of the compound of Formula II is provided:
b is either a hydrogen or an alkyl group having from one to six carbon atoms, an aryl group, a heteroaryl group, and a halogen; R is an alkyl group having from one to six carbon atoms; and Ar is selected from the group consisting of an alkyl group having from one to six carbon atoms, a substituted aryl, and a substituted heteroaryl.
Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula I:
These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.
C07D 239/70 - Composés hétérocycliques contenant des cycles diazine-1, 3 ou diazine-1, 3 hydrogéné condensés avec des carbocycles ou avec des systèmes carbocycliques
A61P 35/04 - Agents anticancéreux spécifiques pour le traitement des métastases
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
38.
Cyclopenta[d]pyrimidines and substituted cyclopenta[d]pyrimidines as antitubulin and microtubule targeting agents, monocyclic pyrimidines as tubulin inhibitors, and pyrrolopyrimidines as targeted antifolates and tubulin and multiple receptor tyrosine kinase inhibitor and antitumor agents
The present invention provides a compound of Formula III, and salts thereof, and a pharmaceutical composition comprising a compound of Formula III:
1 is selected from the group consisting of:
4 is H or an alkyl group having from one to ten carbon atoms. Methods of treating a patient with cancer with these compounds are also provided.
C07D 239/70 - Composés hétérocycliques contenant des cycles diazine-1, 3 ou diazine-1, 3 hydrogéné condensés avec des carbocycles ou avec des systèmes carbocycliques
C07D 405/12 - Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
University of Pittsburgh Of the Commonwealth System of Higher Education (USA)
Duquesne University of the Holy Spirit (USA)
Inventeur(s)
Kellum, John Alston
Hempel, John D.
Edgar, Robert Hugh
Viator, John Andrew
Abrégé
A system for identifying at least one species, strain or type of bacteria in a sample including at least one a labeled bacteriophage which binds selectively to the species, strain or type of bacteria, the at least one labeled bacteriophage comprising a label attached thereto, the system further comprising a detection system adapted to detect the labeled bacteriophage bound to the species of bacteria.
C12Q 1/04 - Détermination de la présence ou du type de micro-organismeEmploi de milieux sélectifs pour tester des antibiotiques ou des bactéricidesCompositions à cet effet contenant un indicateur chimique
The present invention provides a compound of Formula XXVII:
3; or a salt or a hydrate of the compound, and further provides a pharmaceutical composition comprising the compound of Formula XXVII and one or more acceptable pharmaceutical carriers. A method of treating a patient having cancer comprising administering a therapeutically effective amount of a compound of Formula XXVII, or a pharmaceutical composition comprising a compound of Formula XXVII and one or more acceptable pharmaceutical carriers to the patient is disclosed.
Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.
C07D 491/048 - Systèmes condensés en ortho avec un seul atome d'oxygène comme hétéro-atome du cycle contenant de l'oxygène le cycle contenant de l'oxygène étant à cinq chaînons
43.
Tricyclic compounds having antimitotic and/or antitumor activity and methods of use thereof
The present invention provides tricyclic compounds, and pharmaceutically acceptable salts thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
C07D 491/048 - Systèmes condensés en ortho avec un seul atome d'oxygène comme hétéro-atome du cycle contenant de l'oxygène le cycle contenant de l'oxygène étant à cinq chaînons
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
44.
Substituted bicyclic pyrimidine compounds with tubulin and multiple receptor inhibition
This invention provides substituted bicyclic pyrimidine compounds of the following formula:
or a pharmaceutically acceptable salt thereof, wherein R is selected from the group consisting of H and a straight or branched chain alkyl group having from 1 to 10 carbon atoms, wherein the alkyl group is partially or completely saturated, each having tubulin and multiple receptor inhibition properties. Methods of treating a patient diagnosed with cancer are disclosed comprising administering to the patient a therapeutically effective amount of the substituted bicyclic pyrimidine compounds, or a pharmaceutically acceptable salt thereof.
A compound that is a pyrazolo[4,3-d]pyrimidine, and optionally a salt or a hydrate thereof, is disclosed. A pharmaceutical composition comprising a compound that is a pyrazolo[4,3-d]pyrimidine, and optionally a salt or a hydrate of the compound, and includes an optional pharmaceutically acceptable carrier, is provided. A method of treating a patient with cancer including administering a therapeutically acceptable amount of one or more of these compounds and pharmaceutical compositions is set forth.
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
A61K 31/505 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
C07D 231/00 - Composés hétérocycliques contenant des cycles diazole-1, 2 ou diazole-1, 2 hydrogéné
C07D 487/02 - Composés hétérocycliques contenant des atomes d'azote comme uniques hétéro-atomes dans le système condensé, non prévus par les groupes dans lesquels le système condensé contient deux hétérocycles
The present invention discloses a compound comprising the formula:
2 or O, and optionally comprising a pharmaceutically acceptable salt or hydrate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt or hydrate thereof.
A61K 31/343 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à cinq chaînons avec un oxygène comme seul hétéro-atome d'un cycle, p. ex. isosorbide condensés avec un carbocycle, p. ex. coumarane, bufaralol, béfunolol, clobenfurol, amiodarone
C07D 403/02 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles
A61K 31/505 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime
C07D 405/02 - Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle contenant deux hétérocycles
A61K 31/4709 - Quinoléines non condensées contenant d'autres hétérocycles
41 - Éducation, divertissements, activités sportives et culturelles
Produits et services
Clothing, namely, headwear, neckwear, scarves, t-shirts, gloves, golf shirts, jerseys, hoodies, sweatshirts, sweatpants, shorts, tank-tops, jackets, windbreakers, sweaters, and vests Entertainment services, namely, athletic exhibitions and contests presented live and through broadcast and telecast media
41 - Éducation, divertissements, activités sportives et culturelles
Produits et services
Clothing, namely, headwear, neckwear, scarves, t-shirts, gloves, golf shirts, jerseys, hoodies, sweatshirts, sweatpants, shorts, tank-tops, jackets, windbreakers, sweaters, and vests Entertainment services, namely, athletic exhibitions and contests presented live and through broadcast and telecast media
41 - Éducation, divertissements, activités sportives et culturelles
Produits et services
Headwear, t-shirts, golf shirts, jerseys, hoodies, sweatshirts, sweatpants, shorts Entertainment services, namely, athletic exhibitions and contests presented live and through broadcast and telecast media
41 - Éducation, divertissements, activités sportives et culturelles
Produits et services
Headwear, t-shirts, golf shirts, jerseys, hoodies, sweatshirts, sweatpants, shorts Entertainment services, namely, athletic exhibitions and contests presented live and through broadcast and telecast media
A compound of the Formula I and optionally a pharmaceutically acceptable salt thereof is provided:
3—; and Ar is one selected from the group consisting of (a) 1,4-phenyl, (b) 2′-fluoro-1,4-phenyl, and (c) 2,5-thienyl. Methods of treating a patient having cancer, targeting mitochondrial metabolism, and targeting SHMT2 and MTHFD2 using the compounds of this invention are disclosed.
Pyrrolopyrimidine compounds and pharmaceutically acceptable salt thereof are provided. Pharmaceutical compositions having these compounds and acceptable pharmaceutical carriers are disclosed. Pyrrolopyrimidine compounds and pharmaceutically acceptable salts are set forth that are useful to treat a patient having pancreatic, colon, and lung cancers, to target mitochondrial metabolism, and to target serine hydroxymethyltransferase 2 (SHMT2) and 5,10-methylene tetrahydrofolate dehydrogenase 2 (MTHFD2).
The present invention provides substituted pyrrolo-, furano-, and cyclopentylpyrimidine bicyclic compounds of Formula III,
and Formula IV,
and pharmaceutically acceptable salts, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds and pharmaceutical compositions for treating tumor cells and inhibiting mitosis of cancerous cells.
C07D 491/048 - Systèmes condensés en ortho avec un seul atome d'oxygène comme hétéro-atome du cycle contenant de l'oxygène le cycle contenant de l'oxygène étant à cinq chaînons
C07D 239/70 - Composés hétérocycliques contenant des cycles diazine-1, 3 ou diazine-1, 3 hydrogéné condensés avec des carbocycles ou avec des systèmes carbocycliques
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
University of Pittsburgh—Of the Commonwealth System of Higher Education (USA)
Duquesne University of the Holy Spirit (USA)
Inventeur(s)
Kellum, John Alston
Hempel, John D.
Edgar, Robert Hugh
Viator, John Andrew
Abrégé
A method of detecting a species, strain or type of bacteria includes mixing a labeled bacteriophage including a label that is detectible via a detection system with a bacterial culture including the species, strain or type of bacteria to which the labeled bacteriophage selectively binds and using the detection system to detect the labeled bacteriophage bound to the species, strain or type of bacteria.
C12Q 1/04 - Détermination de la présence ou du type de micro-organismeEmploi de milieux sélectifs pour tester des antibiotiques ou des bactéricidesCompositions à cet effet contenant un indicateur chimique
The present invention implements, in a trend or pattern trigger device or system, the generation of hypotheses automatically while considering any collection of data by automatically assessing with templates or charts the presence of patterns in the data without a priori postulation of what the pattern might be. The trend or pattern examination templates or charts contain quantifiable thresholds for data or change in data so that trends or patterns in data can be discerned inductively and automatically without preconceived notions of what or where the patterns or trends might be.
G06N 5/04 - Modèles d’inférence ou de raisonnement
G06Q 10/04 - Prévision ou optimisation spécialement adaptées à des fins administratives ou de gestion, p. ex. programmation linéaire ou "problème d’optimisation des stocks"
G06Q 40/04 - TransactionsOpérations boursières, p. ex. actions, marchandises, produits dérivés ou change de devises
62.
Conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as anti-tumor agents
The present invention provides conformationally restricted 4-substituted 2,6-dimethylfuro[2,3-d]pyrimidine compounds and pharmaceutical compositions comprising these compounds. Preferably, the compounds exhibit dual inhibition of microtubule assembly and receptor tyrosine kinases. Methods of treating cancer comprising administering a therapeutically effective amount of at least one conformationally restricted 4-substituted 2,6-dimethylfuro[2,3-d]pyrimidine compound to a patient is disclosed.
C07D 491/048 - Systèmes condensés en ortho avec un seul atome d'oxygène comme hétéro-atome du cycle contenant de l'oxygène le cycle contenant de l'oxygène étant à cinq chaînons
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
63.
Substituted pyrimidine compounds and methods of use and manufacture
This invention provides substituted pyrimidine compounds having the formula:
2, S, or O, and R is an alkyl group having from one to ten carbon atoms, and optionally salts, hydrates, or solvates thereof, that are useful in treating a patient having a disease or cancer. The compounds of this invention are useful as multi-enzyme antifolates selectively targeting the folate receptor (FR). Further, a method of making 5- and 6-substituted cyclopenta[d]pyrimidine for nonclassical and classical antifolates as TS and DHFR inhibitors is provided.
C07D 239/70 - Composés hétérocycliques contenant des cycles diazine-1, 3 ou diazine-1, 3 hydrogéné condensés avec des carbocycles ou avec des systèmes carbocycliques
64.
Pyrimidine compounds and pyrimido indole compounds and methods of use
The present invention discloses a compound comprising the formula:
2, and optionally comprising a pharmaceutically acceptable salt, hydrate, or solvate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt, hydrate, or solvate thereof.
A61K 31/343 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à cinq chaînons avec un oxygène comme seul hétéro-atome d'un cycle, p. ex. isosorbide condensés avec un carbocycle, p. ex. coumarane, bufaralol, béfunolol, clobenfurol, amiodarone
C07D 403/02 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles
A61K 31/505 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime
C07D 405/02 - Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle contenant deux hétérocycles
A61K 31/4709 - Quinoléines non condensées contenant d'autres hétérocycles
The present invention provides tricyclic compounds, pharmaceutically acceptable salts, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula I:
These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.
C07D 457/04 - Composés hétérocycliques contenant des systèmes cycliques indolo [4, 3-f, g] quinoléine, p. ex. dérivés d'ergoline, de formule p. ex. acide lysergique avec des atomes de carbone comportant trois liaisons à des hétéro-atomes avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement en position 8
The invention generally relates to compounds having structure I:
wherein x represents alkyl, aryl or het-aryl, each of y independently represents hydrogen or halogen and z represents hydrogen or alkyl. Further, said compounds are inhibitors of MEK 1, 2 and 5. Furthermore, the invention includes methods of making said compounds, compositions including said compounds and uses for inhibiting MEK 1, 2 and 5.
C07C 227/10 - Formation de groupes amino dans des composés contenant des groupes carboxyle avec augmentation simultanée du nombre d'atomes de carbone dans le squelette carboné
C07C 229/58 - Composés contenant des groupes amino et carboxyle liés au même squelette carboné ayant des groupes amino et carboxyle liés à des atomes de carbone de cycles aromatiques à six chaînons du même squelette carboné avec des groupes amino et carboxyle liés à des atomes de carbone du même cycle aromatique à six chaînons non condensé avec des groupes amino et carboxyle liés en position ortho ayant l'atome d'azote d'au moins un des groupes amino lié de plus à un atome de carbone d'un cycle aromatique à six chaînons, p. ex. acides N-phénylanthraniliques
68.
MONOCYCLIC, THIENO, PYRIDO, AND PYRROLO PYRIMIDINE COMPOUNDS AND METHODS OF USE AND MANUFACTURE OF THE SAME
The present invention provides monocyclic, thieno, pyrido and pyrrolo pyrimidine compounds. Pharmaceutical compositions comprising one or more of these compounds and optionally comprising a pharmaceutically acceptable salt or hydrate of one or more of the compounds are provided. Preferably, these pharmaceutical compositions further comprise at least one pharmaceutically acceptable carrier. Methods of treating a patient having cancer are provided wherein a therapeutically effective amount of one or more of these compounds or pharmaceutical compositions are administered to the patient.
C07D 401/14 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant au moins trois hétérocycles
69.
Monocyclic, thieno, pyrido, and pyrrolo pyrimidine compounds and methods of use and manufacture of the same
UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION (USA)
DUQUESNE UNIVERSITY OF THE HOLY SPIRIT (USA)
Inventeur(s)
Kellum, John, Alston
Hempel, John, D.
Edgar, Robert, Hugh
Viator, John, Andrew
Abrégé
A method of detecting a species, strain or type of bacteria includes mixing a labeled bacteriophage including a label that is detectible via a detection system with a bacterial culture including the species, strain or type of bacteria to which the labeled bacteriophage selectively binds and using the detection system to detect the labeled bacteriophage bound to the species, strain or type of bacteria.
The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
C07D 491/048 - Systèmes condensés en ortho avec un seul atome d'oxygène comme hétéro-atome du cycle contenant de l'oxygène le cycle contenant de l'oxygène étant à cinq chaînons
72.
Tricyclic compounds having cytostatic and/or cytotoxic activity and methods of use thereof
The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.
C07D 239/70 - Composés hétérocycliques contenant des cycles diazine-1, 3 ou diazine-1, 3 hydrogéné condensés avec des carbocycles ou avec des systèmes carbocycliques
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
73.
Cyclopenta[d]pyrimidines and substituted cyclopenta[d]pyrimidines as antitubulin and microtubule targeting agents, monocyclic pyrimidines as tubulin inhibitors, and pyrrolopyrimidines as targeted antifolates and tubulin and multiple receptor tyrosine kinase inhibition and antitumor agents
The present invention provides a compound of Formula I, and salts thereof, and a pharmaceutical composition comprising a compound of Formula I:
1 is selected from the group consisting of
2 is selected from the group consisting of
3 is a halogen, and most preferably wherein the halogen is chlorine. Methods of treating a patient with cancer with these compounds are also provided.
CYCLOPENTA[D]PYRIMIDINES AND SUBSTITUTED CYCLOPENTA[D]PYRIMIDINES AS ANTITUBULIN AND MICROTUBULE TARGETING AGENTS, MONOCYCLIC PYRIMIDINES AS TUBULIN INHIBITORS, AND PYRROLOPYRIMIDINES AS TARGETED ANTIFOLATES AND TUBULIN AND MULTIPLE RECEPTOR TYROSINE KINASE INHIBITION AND ANTITUMOR AGENTS
The present invention provides a pyrimidine compound and salts thereof, and substituted pyrimidine compounds and salts thereof, and a pharmaceutical composition comprising these compounds. Methods of treating a patient with cancer with these compounds are also provided.
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
The invention is a method for scanning an image data file to determine the presence of a payload, including the steps of identifying the values of one or more lower-order bits in the bytes of an uncompressed image data file to determine the distribution of values at one or more bit positions, and comparing bit position images to reveal hidden payloads from significant variations in contiguous color blocks in the bit position images not otherwise explainable from the original image.
G06K 9/00 - Méthodes ou dispositions pour la lecture ou la reconnaissance de caractères imprimés ou écrits ou pour la reconnaissance de formes, p.ex. d'empreintes digitales
H04N 1/32 - Circuits ou dispositions pour la commande ou le contrôle entre l'émetteur et le récepteur
76.
Substituted furo[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents
Compounds of Formula I:
and compounds of Formula II:
are provided. Pharmaceutical compositions comprising either the compound of Formula I or Formula II are disclosed. Methods of treating patients having cancer are provided by administering to the patient a therapeutically effective amount of one or more compounds having Formula I or Formula II to treat the patient. The compounds of Formula I or II are preferably conformationally restricted furo[2,3-d]pyrimidines having dual inhibition of microtubule assembly and receptor tyrosine kinases.
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
C07D 491/048 - Systèmes condensés en ortho avec un seul atome d'oxygène comme hétéro-atome du cycle contenant de l'oxygène le cycle contenant de l'oxygène étant à cinq chaînons
77.
CONFORMATIONALLY RESTRICTED 4-SUBSTITUTED-2,6-DIMETHYLFURO[2,3-d]PYRIMIDINES AS ANTITUMOR AGENTS
The present invention provides conformationally restricted 4-substituted 2,6-dimethylfuro[2,3-d]pyrimidine compounds and pharmaceutical compositions comprising these compounds. Preferably, the compounds exhibit dual inhibition of microtubule assembly and receptor tyrosine kinases. Methods of treating cancer comprising administering a therapeutically effective amount of at least one conformationally restricted 4-substituted 2,6-dimethylfuro[2,3-d]pyrimidine compound to a patient is disclosed.
C07D 491/048 - Systèmes condensés en ortho avec un seul atome d'oxygène comme hétéro-atome du cycle contenant de l'oxygène le cycle contenant de l'oxygène étant à cinq chaînons
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
78.
PYRIMIDINE COMPOUNDS AND PYRIMIDO INDOLE COMPOUNDS AND METHODS OF USE
The present invention discloses substituted pyrimidine and pyrimido indole compounds and optionally pharmaceutically acceptable salts, hydrates or solvates thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt, hydrate, or solvate thereof.
C07D 403/12 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07D 239/28 - Composés hétérocycliques contenant des cycles diazine-1, 3 ou diazine-1, 3 hydrogéné non condensés avec d'autres cycles comportant au moins trois liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, liés directement aux atomes de carbone du cycle
This invention provides substituted pyrimidine compounds that are useful in treating a patient having a disease or cancer. The compounds of this invention are useful as multi-enzyme antifolates selectively targeting the folate receptor (FR). Further, a method of making 5-and 6-substituted cyclopenta[d]pyrimidine for nonclassical and classical antifolates as TS and DHFR inhibitors is provided.
C07D 239/70 - Composés hétérocycliques contenant des cycles diazine-1, 3 ou diazine-1, 3 hydrogéné condensés avec des carbocycles ou avec des systèmes carbocycliques
80.
SUBSTITUTED CYCLOPENTA PYRIMIDINE BICYCLIC COMPOUNDS HAVING ANTIMITOTIC AND/OR ANTITUMOR ACTIVITY AND METHODS OF USE THEREOF
The present invention provides substituted cyclopenta and cyclopentyl pyrimidine bicyclic compounds of Formula III, and 5,6 - saturated and unsaturated and pharmaceutically acceptable salts, prodrugs, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
C07D 239/70 - Composés hétérocycliques contenant des cycles diazine-1, 3 ou diazine-1, 3 hydrogéné condensés avec des carbocycles ou avec des systèmes carbocycliques
81.
SUBSTITUTED BICYCLIC PYRIMIDINE COMPOUNDS WITH TUBULIN AND MULTIPLE RECEPTOR INHIBITION
This invention provides substituted bicyclic pyrimidine compounds and pharmaceutically acceptable salts, hydrates, and solvates of the compounds, each having tubulin and multiple receptor inhibition properties. Methods of treating a patient diagnosed with cancer is disclosed comprising administering to the patient a therapeutically effective amount of the substituted bicyclic pyrimidine compounds and pharmaceutically acceptable salts, hydrates, and solvates of the compounds, for treating cancer.
The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
C07D 491/048 - Systèmes condensés en ortho avec un seul atome d'oxygène comme hétéro-atome du cycle contenant de l'oxygène le cycle contenant de l'oxygène étant à cinq chaînons
The present invention provides tricyclic compounds, pharmaceutically acceptable salts, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
C07D 239/70 - Composés hétérocycliques contenant des cycles diazine-1, 3 ou diazine-1, 3 hydrogéné condensés avec des carbocycles ou avec des systèmes carbocycliques
C07D 491/048 - Systèmes condensés en ortho avec un seul atome d'oxygène comme hétéro-atome du cycle contenant de l'oxygène le cycle contenant de l'oxygène étant à cinq chaînons
84.
Kinetic-based tool for biometric identification, verification, validation and profiling
A method for identifying an animal or human, including the steps of collecting and retaining an archive data set of measurements of two or more kinetic stylometrics of a first individual animal or human; collecting and retaining a test data set of measurements of the same two or more kinetic stylometrics of a test individual; and comparing archive and test data sets to determine similarity therefore, wherein similarity within any appropriate confidence interval confirms that the test individual and the first individual are the same. Using similar methods, social or other groups maybe kinetically stylometrically profiled for subsequent individual testing.
G06K 9/00 - Méthodes ou dispositions pour la lecture ou la reconnaissance de caractères imprimés ou écrits ou pour la reconnaissance de formes, p.ex. d'empreintes digitales
The present invention provides substituted pyrrolo-, furano-, and cyclopentylpyrimidine bicyclic compounds of Formula III,
and Formula IV,
and pharmaceutically acceptable salts, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds and pharmaceutical compositions for treating tumor cells and inhibiting mitosis of cancerous cells.
C07D 491/048 - Systèmes condensés en ortho avec un seul atome d'oxygène comme hétéro-atome du cycle contenant de l'oxygène le cycle contenant de l'oxygène étant à cinq chaînons
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
C07D 239/70 - Composés hétérocycliques contenant des cycles diazine-1, 3 ou diazine-1, 3 hydrogéné condensés avec des carbocycles ou avec des systèmes carbocycliques
2/n) is smaller than a second predetermined threshold then author i cannot be the correct author; or if no author garners significantly more votes than all other contenders then none of the named authors is the author of a document in question—in a number of novel applications. Personality profiling and authorship attribution may also be used to verify user identity to a computer.
The present invention provides substituted cyclopenta and cyclopentyl pyrimidine bicyclic compounds of Formula III,
and pharmaceutically acceptable salts, prodrugs, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
C07D 491/048 - Systèmes condensés en ortho avec un seul atome d'oxygène comme hétéro-atome du cycle contenant de l'oxygène le cycle contenant de l'oxygène étant à cinq chaînons
C07D 239/70 - Composés hétérocycliques contenant des cycles diazine-1, 3 ou diazine-1, 3 hydrogéné condensés avec des carbocycles ou avec des systèmes carbocycliques
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A combination hormone and melatonin therapy is provided to reduce the risk of developing, or to reduce the severity of, breast cancer by administering at least one estrogen hormone and optionally at least one progesterone-receptor-binding compound or composition and melatonin together, preferably at normal bed time.
A61K 31/57 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes substitués en position 17 bêta par une chaîne à deux atomes de carbone, p. ex. prégnane ou progestérone
A61K 31/56 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes
A61K 31/566 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes non substitués en position 17 bêta par un atome de carbone, p. ex. œstrane, œstradiol ayant un groupe oxo en position 17, p. ex. œstrone
A61K 31/567 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes non substitués en position 17 bêta par un atome de carbone, p. ex. œstrane, œstradiol substitués en position 17 alpha, p. ex. mestranol, noréthandrolone
A61K 31/573 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes substitués en position 17 bêta par une chaîne à deux atomes de carbone, p. ex. prégnane ou progestérone substitués en position 21, p. ex. cortisone, dexaméthasone, prednisone ou aldostérone
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
A61K 31/4045 - Indole-alkylaminesLeurs amides, p. ex. sérotonine, mélatonine
89.
A METHOD OF DETECTING STEGANOGRAPHICALLY HIDDEN IMAGES VIA LOW-ORDER BIT COMPARISONS
The invention is a method for scanning an image data file to determine the presence of a payload, including the steps of identifying the values of one or more lower-order bits in the bytes of an uncompressed image data file to determine the distribution of values at one or more bit positions, and comparing bit position images to reveal hidden payloads from significant variations in contiguous color blocks in the bit position images not otherwise explainable from the original image.
A method for identifying an animal or human, including the steps of collecting and retaining an archive data set of measurements of two or more kinetic stylometrics of a first individual animal or human; collecting and retaining a test data set of measurements of the same two or more kinetic stylometrics of a test individual; and comparing archive and test data sets to determine similarity therefore, wherein similarity within any appropriate confidence interval confirms that the test individual and the first individual are the same. Using similar methods, social or other groups maybe kinetically stylometrically profiled for subsequent individual testing.
A61K 31/135 - Amines, p. ex. amantadine ayant des cycles aromatiques, p. ex. méthadone
A01N 43/38 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un atome d'azote comme unique hétéro-atome du cycle des cycles à cinq chaînons condensés avec des carbocycles
A61K 31/405 - Acides indole-alkanecarboxyliquesLeurs dérivés, p. ex. tryptophane, indométhacine
A bone implant, and bone implant material, includes a calcium- and oxide-containing artificial graft material in a scaffold, to which melatonin and an optional cell adhesion peptide are absorbed or covalently linked.
A functionalized composition and resulting functionalized body or prosthesis for in vitro and in vivo use comprising at least one calcium phosphate containing phase that is functionalized with a linker group comprising at least one of an organic acid molecule, a phosphoric acid, an amine, N,N-dicyclohexylcarbodiimide, and 3-maleimidopropionic acid N-hydroxysuccinimide ester, wherein the linker group provides for a reactive location for the attachment of one or more of a chemical and/or a biologically active moiety to the calcium phosphate containing phase. The functionalized compositions have a pliable physical property when mixed with water and adhere to natural bone and subsequently harden at ambient temperatures. Methods of manufacturing a functionalized artificial prosthesis that may be used as artificial bones, joints, in-vitro support structures, and in-vivo support structures for cells, tissues, organs, and nerve growth and regeneration are disclosed. Methods of repairing a bone, vertebrae, or tissue structures using the functionalized compositions are provided.
Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula 1:
These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.
Novel distractorless authorship verification technology optionally combines with novel algorithms to solve authorship attribution as to an open set of candidates—such as without limitation by analyzing the voting of "mixture of experts" and outputting the result to a user using the following: if z (z = pi - pj √ pi + pj- (pi - pj)2 /n) is larger than a first predetermined threshold then author j cannot be the correct author; or if z (z = pi - pj √ pi + pj- (pi - pj)2 /n) is smaller than a second predetermined threshold then author i cannot be the correct author; or if no author garners significantly more votes than all other contenders then none of the named authors is the author of a document in question— in a number of novel applications. Personality profiling and authorship attribution may also be used to verify user identity to a computer.
G06F 21/00 - Dispositions de sécurité pour protéger les calculateurs, leurs composants, les programmes ou les données contre une activité non autorisée
G06F 17/00 - Équipement ou méthodes de traitement de données ou de calcul numérique, spécialement adaptés à des fonctions spécifiques
96.
BICYCLIC AND TRICYCLIC PYRIMIDINE TYROSINE KINASE INHIBITORS WITH ANTITUBULIN ACTIVITY AND METHODS OF TREATING A PATIENT
Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.
A01N 43/90 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant plusieurs hétérocycles déterminants condensés entre eux ou avec un système carbocyclique commun
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
97.
SELECTIVE PROTON COUPLED FOLATE TRANSPORTER AND FOLATE RECEPTOR, AND GARFTASE AND/OR OTHER FOLATE METABOLIZING ENZYMES INHIBITOR COMPOUNDS AND METHODS OF USING THE SAME
The present invention provides selective proton coupled folate transporter and folate receptor, and glycinamide ribonucleotide formyltransferase enzyme and/or other folate metabolizing enzyme inhibitors having a fused cyclic pyrimidine compound, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof. These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase and/or other folate metabolizing enzymes in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.
A01N 43/90 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant plusieurs hétérocycles déterminants condensés entre eux ou avec un système carbocyclique commun
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
98.
Functionalized calcium phosphate artificial bone and joint compositions and methods of use and manufacture
The present invention provides a functionalized composition and resulting functionalized body or prosthesis for in vitro and in vivo use comprising at least one calcium phosphate containing phase that is functionalized with a linker group comprising at least one of an organic acid molecule, a phosphonic acid, an amine, N,N-dicyclohexylcarbodiimide, and 3-maleimidopropionic acid N-hydroxysuccinimide ester, and combinations thereof, and one or more of a chemical and/or a biologically active moieties, wherein the linker group provides for a reactive location for the attachment of the chemical or biologically active moiety, or both, to the calcium phosphate containing phase, and optionally including an unmodified and/or modified calcium aluminate containing phase. Methods of manufacturing a functionalized artificial prosthesis and methods of repairing a bone, vertebrae, or tissue structures are provided.
A61K 33/06 - Aluminium, calcium ou magnésiumLeurs composés
C12N 5/00 - Cellules non différenciées humaines, animales ou végétales, p. ex. lignées cellulairesTissusLeur culture ou conservationMilieux de culture à cet effet
A61K 38/02 - Peptides à nombre indéterminé d'amino-acidesLeurs dérivés
B29C 33/38 - Moules ou noyauxLeurs détails ou accessoires caractérisés par la matière ou le procédé de fabrication
A61K 31/43 - Composés contenant des systèmes cycliques thia-4 aza-1 bicyclo [3.2.0] heptane, c.-à-d. composés contenant un système cyclique de formule , p. ex. pénicillines, pénèmes
A61K 31/7036 - Composés ayant des radicaux saccharide liés à des composés non-saccharide par des liaisons glycosidiques liés à un composé carbocyclique, p. ex. phloridzine ayant au moins un groupe amino lié directement au carbocycle, p. ex. streptomycine, gentamycine, amikacine, validamycine, fortimicines
The present invention implements, in a trend or pattern trigger device or system, the generation of hypotheses automatically while considering any collection of data by automatically assessing with templates or charts the presence of patterns in the data without a priori postulation of what the pattern might be. The trend or pattern examination templates or charts contain quantifiable thresholds for data or change in data so that trends or patterns in data can be discerned inductively and automatically without preconceived notions of what or where the patterns or trends might be.
The combined use — whether by adsorption or covalent linkage — of Melatonin adjacent any bone implant or graft, preferably any calcium- and oxide-containing artificial bone graft material, and more preferably a calcium aluminate composition. Alternatively, the bone graft or implant material may be used as a scaffold for tissue engineering.
