Entries |
Document | Title | Date |
20080261962 | METHOD OF INHIBITION OF RESPIRATORY DEPRESSION USING POSITIVE ALLOSTERIC AMPA RECEPTOR MODULATORS - The invention is directed to a method for alleviating respiratory depression in a subject as a result of disease of pharmacological agents such as opiates, opioids or barbiturates. The invention also discloses pharmaceutical compositions for use with the method, the composition containing in combination, an analgesic, anaesthetic, or a sedative and a positive allosteric AMPA receptor modulator in an amount sufficient to reduce or inhibit respiratory depression caused by the analgesic, anaesthetic, or sedative. | 10-23-2008 |
20080261963 | SUBSTITUTED QUINOBENZOXAZINE ANALOGS - The present invention relates to quinobenzoxazines analogs having the general formula: | 10-23-2008 |
20080318938 | METHODS FOR TREATING ABERRANT CELL PROLIFERATION DISORDERS - The invention relates in part to methods for inhibiting proliferation of cancer cells and treating one or more cell proliferative conditions using compounds described herein. | 12-25-2008 |
20080318939 | METHODS FOR TREATING OPHTHALMIC DISORDERS - The invention relates in part to methods for treating ophthalmic conditions using compounds described herein. The conditions to be treated include various ocular cancers. The compositions employed include a polycyclic quinolinone derivative or related heteroaromatic analog thereof. | 12-25-2008 |
20090005371 | Substituted Fused [1,2]Imidazo[4,5-C] Ring Compounds and Methods - Fused [1,2]imidazo[4,5-c] ring compounds, e.g., fused [1,2]imidazo[4,5-c]quinolines and [1,2]imidazo[4,5-c]naphthyridines, with a substituent, e.g., a substituted alkoxy substituent, at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed. | 01-01-2009 |
20090012071 | 4-SUBSTITUTED-1H-ISOTHIAZOLO[5,4-B][1,4]OXAZINO[2,3,4-IJ]QUINOLINE-7,8(2H,9H)-DIONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS - The present invention provides compounds of the formula that possess antimicrobial activity. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity. Particular compounds provided herein are also potent and/or selective inhibitors of microbial DNA synthesis and reproduction. The invention provides anti-microbial compositions, including pharmaceutical compositions, containing a compound of the invention and one or more or more carriers. The invention provides pharmaceutical compositions containing a 4-substituted- | 01-08-2009 |
20090088423 | METHODS AND COMPOSITIONS FOR TREATING BACTERIAL INFECTIONS AND DISEASES ASSOCIATED THEREWITH - The invention features methods and compositions for treating bacterial infections. | 04-02-2009 |
20090137575 | Fused Tetracyclic mGluR1 Antagonists as Therapeutic Agents - In its many embodiments, the present invention provides tetracyclic compounds of formula I or formula II (wherein the various moieties are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease. | 05-28-2009 |
20090143373 | QUINOLONE CARBOXYLIC ACID-SUBSTITUTED RIFAMYCIN DERIVATIVES - The compounds include substituted rifamycin derivatives in which a quinolone carboxylic acid pharmacophore is covalently bonded to a benzoxazinorifamycin or a spiropiperidinorifamycin. The rifamycin derivatives are useful as antimicrobial agents and are effective against a number of human and veterinary Gram positive and Gram negative pathogens. The advantage of the inventive compounds is that both the rifamycin and quinolone antibacterial pharmacophores are co-delivered with matched pharmacokinetics to the targeted pathogens of interests. Delivery of multiple antibacterial pharmacophores simultaneously to the targeted pathogens has the maximum chance of achieving synergy and minimizing the development of resistance to the antibiotics given. | 06-04-2009 |
20090149453 | METHODS AND COMPOSITIONS FOR TREATING BACTERIAL INFECTIONS AND DISEASES ASSOCIATED THEREWITH - The invention features methods and compositions for treating bacterial infections. | 06-11-2009 |
20090203682 | Rapamycin Analogues and the Uses Thereof in the Treatment of Neurological Disorders - Method of treatment of neurological disorders or complications due to stroke or head injury through the administration of a pharmaceutical composition including a pharmaceutically acceptable excipient or carrier and a compound of formula I are provided: | 08-13-2009 |
20090209527 | Methods for Using Rapamycin Analogues in the Treatment of Neurological Disorders - The present invention provides methods for treatment of neurological disorders or complications due to stroke or head injury; benign or malignant neoplastic disease, carcinomas and adenocarcinomas; proliferative disorders; and inflammatory disorders, comprising administering a compound as described herein to a subject in need thereof, and a pharmaceutically acceptable carrier, within a therapeutic window that is from about 4 hours to 24 hours, or longer, for example at least 4, 6, 9, 12, 15, 18, 21 or 24 hours, or longer, after the onset of the neurological, proliferative, or inflammatory disorder or a symptom thereof. In some embodiments, the compounds of the following structure, wherein R | 08-20-2009 |
20090215761 | QUINOBENZOXAZINE ANALOGS AND METHODS OF USING THEREOF - The present invention relates to quinobenzoxazines analogs having the general formula: | 08-27-2009 |
20090239855 | Rapamycin Analogues and the Uses Thereof in the Treatment of Neurological, Proliferative, and Inflammatory Disorders - The present invention provides for methods of treating neurological disorders or complications due to stroke or head injury; benign or malignant neoplastic disease, carcinomas and adenocarcinomas; proliferative disorders; and inflammatory disorders using compounds of the following structure: | 09-24-2009 |
20090258869 | METHODS AND COMPOUNDS FOR TREATMENT OR PREVENTION OF SUBSTANCE-RELATED DISORDERS - The present disclosure provides methods of treating or preventing a substance-related disorder using Hsp90 inhibitors, Hsp90 modulators, tyrosine hydroxylase modulators, and modulators that reduce the interaction between Hsp90 and tyrosine hydroxylase. | 10-15-2009 |
20090258870 | NOVEL ANSAMITOCIN DERIVATIVES - Provided are among other things ansamitocin derivatives, pharmaceutical compositions comprising these novel ansamitocin derivatives, methods for the production of the ansamitocin derivatives and their use for the treatment of cancer. | 10-15-2009 |
20090270377 | COMBINATION CANCER CHEMOTHERAPY - Provided is a method for improving treatment of a neoplastic condition by combining a therapeutically effective amount of a polyADP-ribose polymerase inhibitor with a therapeutically effective amount of a compound which triggers the release of nucleolin from the G-quadruplexes in rDNA. As specifically exemplified, the compound which increases nucleolin binding is a substituted quinobenzoxazine analog, for example CX-3543. | 10-29-2009 |
20100009981 | Tetracycline Derivatives with Reduced Antibiotic Activity and Neuroprotective Benefits - The present disclosure is directed to compositions and methods which utilize the tetracycline scaffold, preferably the scaffold of tetracycline or minocycline, and which significantly lack antibiotic activity. The compounds have neuroprotective attributes without interfering with the drugs capacity to pass through the blood brain barrier. These compounds have neuroprotective activity because of their inhibition of neuronal cell cycle progression. The compounds are characterized in part by a fifth ring joining positions 9 and 10. | 01-14-2010 |
20100069376 | 5-HYDROXYMETHYL-OXAZOLIDIN-2-ONE ANTIBACTERIALS - The invention relates to novel chimeric antibiotics of formula I | 03-18-2010 |
20100081654 | Oncogenic-RAS-signal dependent lethal compounds - Compounds with cancer cell specific lethality are provided. In particular, RAS-selective lethal compounds and compositions are provided. Also provided are methods of screening for such compounds and methods of treating a condition in a mammal, by administering to the mammal a therapeutically effective amount of such compounds or compositions. | 04-01-2010 |
20100093716 | THERAPEUTIC METHODS USING WRN BINDING MOLECULES - The present invention provides, inter alia, compositions and methods for treating various diseases and disorders in a mammal by administering to a mammal in need an effective amount of a composition comprising a non-DNA small molecule that binds WRN, such as members of the spirooxindole (SPOX) class. | 04-15-2010 |
20110207725 | CHIRAL FUSED [1,2]IMIDAZO[4,5-c] RING COMPOUNDS - Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X | 08-25-2011 |
20110218195 | METHODS AND COMPOSITIONS FOR TREATING BACTERIAL INFECTIONS AND DISEASES ASSOCIATED THEREWITH - The invention features methods and compostions for treating bacterial infections. | 09-08-2011 |
20110224201 | CGRP RECEPTOR ANTAGONISTS - Compounds of Formula (I), (wherein variables A | 09-15-2011 |
20110306607 | HETEROCYCLIC CHROMENE-SPIROCYCLIC PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS - The invention relates to heterocyclic chromene-spirocyclic piperidine amides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 12-15-2011 |
20120004219 | Method of Inhibition of Respiratory Depression Using Positive Allosteric AMPA Receptor Modulators - The invention is directed to a method for alleviating respiratory depression in a subject as a result of disease of pharmacological agents such as opiates, opioids or barbiturates. The invention also discloses pharmaceutical compositions for use with the method, the composition containing in combination, an analgesic, anaesthetic, or a sedative and a positive allosteric AMPA receptor modulator in an amount sufficient to reduce or inhibit respiratory depression caused by the analgesic, anaesthetic, or sedative. | 01-05-2012 |
20120046281 | RIFALAZIL COMPOSITIONS AND THERAPEUTIC REGIMENS - The invention features low-dosage rifalazil compositions and therapeutic regimens which are useful for the treatment of bacterial infections. | 02-23-2012 |
20120196852 | INHIBITORS OF METHIONINE AMINOPEPTIDASES AND METHODS OF TREATING DISORDERS - The invention is directed towards novel naphthoquinone and naphthothiazole compounds, and methods of treating disorders related to MetAP, including tuberculosis and bacterial infection, using various naphthoquinone, hydroxyquinonline, and naphthothiazole compounds. | 08-02-2012 |
20130005720 | PHARMACEUTICAL COMPOSITION FOR TREATING CANCER AND APPLICATIONS THEREOF - This invention relates to a pharmaceutical composition for treating cancer, comprising an effective amount of a compound represented by formula (I): | 01-03-2013 |
20130123248 | PHARMACOLOGICAL MODULATION OF POSITIVE AMPA RECEPTOR MODULATOR EFFECTS ON NEUROTROPHIN EXPRESSION - Antagonists of group 1 metabotropic glutamate receptors (mGluR) potentiate the effect of positive AMPA receptor modulators on neurotrophin expression, such as brain-derived neurotrophic factor (BDNF). The findings described herein suggest a combinatorial approach for drug therapies, using both positive AMPA receptor modulators and mGluR antagonists, to enhance brain neurotrophism. | 05-16-2013 |
20140051692 | Inhibitors of Human Immunodeficiency Virus Replication - The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. | 02-20-2014 |
20140080821 | PYRIMIDO-PYRROLO-OXAZINE-DIONE COMPOUND INHIBITORS OF THE CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR PROTEIN AND USES THEREFOR - Provided herein are benzopyrimido-pyrrolo-oxazine-dione (BPO) compounds and pyrimido-pyrrolo-quinoxalinedione (PPQ) compounds, and compositions comprising these compounds, that inhibit cystic fibrosis transmembrane conductance regulator (CFTR) mediated ion transport and that are useful for treating diseases and disorders associated with aberrantly increased CFTR chloride channel activity, such as polycystic kidney disease and secretory diarrheas. The compounds and compositions comprising the compounds described herein may be used for inhibiting expansion or preventing formation of cysts in persons who have polycystic kidney disease. | 03-20-2014 |
20140163021 | FKBP52-Tau Interaction as a Novel Therapeutical Target for Treating the Neurological Disorders Involving Tau Dysfunction - Candidate compounds for use in neuro-protection and repair in neurological disorders involving Tau dysfunction (including Alzheimer's disease) are identified from a direct interaction between proteins FKBP52 and Tau. The method for screening a drug for the prevention and treatment of neurological disorders involving Tau dysfunction includes determining the ability of a candidate compound, to modulate binding between a Tau polypeptide and a FKBP52 polypeptide, and selecting positively the candidate compound that modulates binding. | 06-12-2014 |
20140206677 | COMPOUNDS AND METHODS FOR TREATING BACTERIAL INFECTIONS - Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed. | 07-24-2014 |
20140256717 | MACROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS - There is provided compounds of formula I, wherein R1, R | 09-11-2014 |
20140303155 | PHARMACEUTICAL COMPOSITION AND KIT FOR TREATING BACTERIAL INFECTIONS - The invention relates to pharmacology and medicine, more particularly to novel pharmaceutical compositions and pharmaceutical kits for treating bacterial infections, and to novel method for treating diseases caused by bacterial infections including tuberculosis. | 10-09-2014 |
20140364429 | ANTIVIRAL COMPOUNDS HIGHLY EFFECTIVE AS HCV-NS5A INHIBITOR - Provided are compounds antiviral compounds represented by formula Ia and Ib: | 12-11-2014 |
20150025066 | CYCLIC DIAMINOPYRIMIDINE DERIVATIVES - Compounds of the formula I | 01-22-2015 |
20150057270 | CYCLIC PRODRUGS OF DUOCARMYCIN ANALOGS - The invention provides prodrugs of DNA-reactive analogs of duocarmycin and CC-1065 anticancer agents, wherein a cyclic prodrug form, such as carbamate, thionocarbamate, or carbamimidate, can be hydrolyzed by the patient in vivo to yield a respective bioactive agent comprising a DNA-alkylating moiety and a binding/targeting moiety. The DNA-reactive moiety is a γ-spiro-cyclohexenone fused to a heterocyclyl group which can be produced by endogenous hydrolysis of a cyclic carbamate prodrug of the invention. The cyclic carbamate prodrug produces no residual byproduct during activation in vivo. Methods of synthesis and biological methods and data are also provided. | 02-26-2015 |
20150359759 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF PERVASIVE DEVELOPMENT DISORDERS - A method of treating a pervasive development disorder in a subject includes administering to the subject an amount of an NMDAR antagonist effective to ameliorate biochemical and functional abnormalities in the subject associated with loss-of-function mutations of the gene encoding methyl-CpG binding protein 2 (MeCP2). | 12-17-2015 |
20150374707 | Methods and Compounds for the Inhibition of Cellular Proliferation - Methods for inhibiting translation, treating a cellular proliferative disorder, and inhibiting proliferation of cells using the compounds disclosed herein are provided. | 12-31-2015 |
20160016972 | Cyclic N-Acyl O-Amino Phenol CBI Derivative - A group of cyclic N-acyl O-amino phenol CBI derivatives were synthesized and shown to be pro-drugs, subject to reductive activation by cleavage of a N—O bond, effectively releasing the free drug in functional in vitro cellular assays for cytotoxic activity approaching the activity of the free drug, yet remain essentially stable to ex vivo DNA alkylation conditions. Assessment of the in vivo antitumor activity of a representative pro-drug indicates that a contemplated pro-drug approaches the potency and exceeds the efficacy of the free drug itself (CBI-indole | 01-21-2016 |
20160039844 | Inhibitors of Human Immunodeficiency Virus Replication - The disclosure generally relates to compounds of formula (I), including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. | 02-11-2016 |
20160120873 | Method of Inhibition of Respiratory Depression Using Positive Allosteric AMPA Receptor Modulators - The invention is directed to a method for alleviating respiratory depression in a subject as a result of disease of pharmacological agents such as opiates, opioids or barbiturates. The invention also discloses pharmaceutical compositions for use with the method, the composition containing in combination, an analgesic, anaesthetic, or a sedative and a positive allosteric AMPA receptor modulator in an amount sufficient to reduce or inhibit respiratory depression caused by the analgesic, anaesthetic, or sedative. | 05-05-2016 |
20160130281 | COMPOUNDS AND METHODS FOR TREATING BACTERIAL INFECTIONS - Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed. | 05-12-2016 |
20160152617 | COMPOUNDS FOR THE TREATMENT OF MALARIA | 06-02-2016 |
20160200737 | Maytansinoid Derivatives | 07-14-2016 |
20220133732 | BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR CAIX - The present invention relates to polypeptides which are covalently bound to aromatic molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of carbonic anhydrase IX (CAIX).The invention also includes dmg conjugates comprising said peptides,conjugated to one or more effector and/or functional groups, to pharmaceutical compositions comprising said peptide ligands and drug conjugates and to the use of said peptide ligands and drug conjugates in preventing, suppressing or treating a disease or disorder mediated by CAIX. | 05-05-2022 |