487 results about "Benzodiazepine" patented technology

The present invention relates to novel 2-fluoro-pyrrolo[2,1-c][1,4]benzodiazepine dimers useful as antitumour agents and to a process for the preparation thereof.

The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like.

Nasal administration of benzodiazepines is described as providing improved therapeutic effects as compared to conventional delivery techniques. The compositions comprise a benzodiazepine hypnotic in a pharmaceutically acceptable nasal carrier.

This invention provides an antibody with high affinity for single-stranded DNA, low or no affinity for double-stranded DNA, and capable of specifically binding a DNA hairpin and the hybridoma cell lines which produces these monoclonal antibodies. A chimeric mouse comprising these hybridoma cell lines and a histocompatible mouse is further provided. A method for screening for an agent which will inhibit anti-DNA antibody.DNA binding. One such agent is a benzodiazepine derivative. This invention therefore provides a method of inhibiting the binding of an anti-DNA antibody to its DNA ligand in a sample by contacting the sample with an effective amount of a benzodiazepine derivative.

Described are nanoparticulate formulations of a benzodiazepine, such as lorazepam, that does not require the presence of polyethylene glycol and propylene glycol as stabilizers, and methods of making and using such formulations. The formulations are particularly useful in aerosol and injectable dosage forms, and comprise nanoparticulate benzodiazepine, such as lorazepam, and at least one surface stabilizer. The formulations are useful in the treatment of status epilepticus, treatment of irritable bowel syndrome, sleep induction, acute psychosis, and as a pre-anesthesia medication.

The present invention provides methods for treating a variety of urogenital disorders, such as, for example, vaginismus, dyspareunia, vulvodynia (including vulvar vestibulitis), interstitial cystitis, nonspecific urethriris (i.e., nonspecific pain and / or burning of the urinary tract) and sexual dysfunctions, such as, for example, female sexual arousal disorders and female sexual orgasmic disorders, using a variety of compounds, including, but not limited to, NO donors, calcium channel blockers, cholinergic modulators, α-adrenergic receptor antagonists, β-adrenergic receptor agonists, phosphodiesterase inhibitors, cAMP-dependent protein kinase activators (e.g., cAMP mimetics), superoxide scavengers, potassium channel activators, estrogen-like compounds, testosterone-like compounds, benzodiazepines, adrenergic nerve inhibitors, antidiarrheal agents, HMG-CoA reductase inhibitors, smooth muscle relaxants, adenosine receptor modulators, adenylyl cyclase activators, endothelin receptor antagonists, bisphosphonates and cGMP-dependent protein kinase activators (e.g., cGMP mimetics).

A method and system for determining the fall risk of a patient is provided. The method includes the evaluation of a patient to determine whether the patient exhibits one or more intrinsic fall risk factors selected from a group consisting of confusion, depression, altered elimination, dizziness, male gender, antiepileptic / anticonvulsant prescriptions and benzodiazepine prescriptions. A specific point value is assigned to each of the intrinsic risk factors found to be exhibited by the patient. A mobility test is also performed on the patient to evaluate the patient's ability to rise from a seated position, and a specific mobility test point value is assigned to the patient based upon the patient's performance of the mobility test. Each intrinsic risk factor's specific point value is then summed together with the specific mobility test point value to achieve a total risk score, and the patient's fall risk is determined based on the total risk score. An intervention process may be developed for the patient based on the patient's fall risk.

A method and system for determining the fall risk of a patient is provided. The method includes the evaluation of a patient to determine whether the patient exhibits one or more intrinsic fall risk factors selected from a group consisting of confusion, depression, altered elimination, dizziness, male gender, antiepileptic / anticonvulsant prescriptions and benzodiazepine prescriptions. A specific point value is assigned to each of the intrinsic risk factors found to be exhibited by the patient. A mobility test is also performed on the patient to evaluate the patient's ability to rise from a seated position, and a specific mobility test point value is assigned to the patient based upon the patient's performance of the mobility test. Each intrinsic risk factor's specific point value is then summed together with the specific mobility test point value to achieve a total risk score, and the patient's fall risk is determined based on the total risk score. An intervention process may be developed for the patient based on the patient's fall risk.

A compound of formula (I); or a salt or solvate thereof, wherein: the dotted line indicates the optional presence of a double bond between C2 and C3; R2 is selected from —H, —OH, =0, ═CH2, —CN, —R, OR, halo, ═CH—R, O—SO2—R, CO2R and COR; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, nitro, Me3Sn and halo, where R and R′ are independently selected from optionally substituted C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R10 and R11 either together form a double bond, or are selected from H and YRY, where Y is selected from O, S and NH and R is H or C1-7 alkyl or H and SOxM, where x is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; each X is independently a heteroarylene group; n is from 1 to 6; and RE is C1-4 alkyl. The compound is useful for the treatment of proliferative diseases.

The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like.

A compound of formula (I); or a salt or solvate thereof, wherein: the dotted line indicates the optional presence of a double bond between C2 and C3; R2 is selected from —H, —OH, =0, ═CH2, —CN, —R, OR, halo, ═CH—R, O—SO2—R, CO2R and COR; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, nitro, Me3Sn and halo, where R and R′ are independently selected from optionally substituted C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R10 and R11 either together form a double bond, or are selected from H and YRY, where Y is selected from O, S and NH and R is H or C1-7 alkyl or H and SOxM, where x is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; each X is independently a heteroarylene group; n is from 1 to 6; and RE is C1-4 alkyl. The compound is useful for the treatment of proliferative diseases.

The invention discloses a method which can carry out qualitative screening to 242 compounds (drugs or toxicants) simultaneously. A mode of liquid chromatogram-mass spectrometry (LC-MS / MS) multi-reaction monitoring (MRM) is adopted to carry out determinedness to objects by two pairs of parent ion-daughter ion pair and retention time. The 242 drugs or toxicants comprise toxic products such as opioids, amphetamine and cocaines and the like, bromazepam such as benzodiazepines and barbiturates, and common drugs, alkaloid, pesticide (including organophosphates, carbamates, pyrethroid pesticide residues and organochlorine pesticide), weed killer, raticide and the like.

A method for the treatment of Restless Leg Syndrome (RLS), which comprises administering an alpha2-agonist and a second agent selected from the group consisting of the dopamine agonists, opioids, benzodiazepines and the combination of L-DOPA plus a decarboxylase inhibitor.

The invention relates to the fields of analytical chemistry and food safety, in particular to a method for detecting the residual quantity of multiple alkaline drugs in animal derived food. Based on the vortex mixed extracting of acetonitrile, isopropanol and citric acid buffer solutions, the purification of a hydrophilic polystyrene-divinylbenzene solid phase extraction column and a cation exchange solid phase extraction column and the liquid phase chromatography-mass spectra determination, the method can detect the residual quantity of multiple alkaline drugs in pork, pork liver, eggs, shrimps and milk, such as beta-receptor agonists,sulfonamides, benzodiazepines, nitroimidazoles, benzimidazoles and triphenylmethanes. The method has the advantages of simple operation, fast and accurate detection and high efficiency.

Angiogenesis may be initiated or increased through the use of gamma-secretase inhibitors. The gamma-secretase inhibitor can be a dipeptide class, sulfonamide class, transition state mimic class, benzodiazepine class, or benzocaprolactam class gamma secretase inhibitor. Methods for initiating and increasing angiogenesis are used for disease prevention and treatment as well as for generating research models.

The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and related compounds and methods of using benzodiazepine derivatives and related compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like.

The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like.

The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like.

Novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids as well as processes for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids are dislcosed. More particularly, present invention relates to a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids as DNA sequence selective agents which are useful as potential antitumour agents. In particular, the present invention relates to a process for the preparation of new pyrrolo[2,1-c][1,4]benzodiazepine hybrids as potential antitumour agents. These compounds have the formula XIV shown below:

This invention relates to combinations of an atypical antipsychotic, and a GABA modulator, a benzodiazepine, and / or an anticonvulsant drug, kits containing such combinations, pharmaceutical compositions comprising such combinations, and methods of using such combinations to treat patients suffering from treatment-resistant anxiety disorders, psychotic disorders or conditions, or mood disorders or conditions.

The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like.

Methods for enhancing the complexation efficiency of a drug with cyclodextrin and for enhancing the availability of a drug following administration of a cyclodextrin-drug complex.

A drug having a high affinity for benzodiazepine ω3 receptors and showing curative and preventive effects for anxiety and depression, which comprises as the active ingredient, for example, a compound of the formula (1): wherein R1 and R2 are independently a hydrogen atom, an optionally substituted alkyl group, an optionally substituted aryl group, etc., R3 and R4 are independently a hydrogen atom, an optionally substituted alkyl group, etc., R5, R6, R7 and R8 are independently a hydrogen atom, an optionally substituted alkyl group, an optionally substituted aryl group, etc., X is an oxygen atom, a sulfur atom, NR10, etc. (in which R10 is a hydrogen atom, an optionally substituted alkyl group, etc.)

The present invention relates to a process for the preparation of novel pyrrolo [2,1-c][1,4]benzodiazepine hybrids useful as antitumour agents. This invention also relates to a process for the preparation of new pyrrolo[2,1-c][1,4]benzodiazepine hybrids as potential antitumour agents. More particularly, it provides a process for the preparation of 7-methoxy-8-[N-(1''-pyrenyl)-alkane-3'-carboxamide]-oxy-(11aS)-1,2,3,11a-tetraydro 5H-pyrrolo[2,1-c][1,4]benzodiazepine-5-one, with aliphatic chain length variation of these compounds and it also describes the DNA binding, anticancer (antitumour) activity. The structural formula of this novel pyrrolo[2,1-c][1,4]benzodiazepine is given below:

The present invention provides a compound of general formula 5, useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]benzodiazepine hybrids of general formula 5wherein, X1, X2, X3 is selected from H or Cl or CH3, Y is selected from O or NH, Z is selected from C═O or CH2 and n=1 to 4.

The present invention provides a compound of general formula 5, useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]benzodiazepine hybrids of general formula (5): wherein n=3, 4, 5, 6, 8 and wherein R1 and R2 is selected from the group consisting of R1═H, R2═H or R1═CH3O, R2=CH3O or R1═CH3O and R2═C2H5O.

The present invention includes benzodiazepine compositions formulated for intranasal administration, comprising a binary solvent system comprising a first solvent in which the benzodiazepine is soluble, the first solvent capable of penetrating nasal mucosal tissue, and a second solvent in which the benzodiazepine in less soluble. The compositions of the present invention may be used to treat a variety of disorders including, but not limited to, panic attacks, muscle spasms, anxiety, and seizures. In one aspect, the present invention relates to a fast-acting, clonazepam composition for transnasal administration that can be used for the treatment of seizure clusters.

The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like.

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.