50 results about "Receptor blockade" patented technology

Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective alpha 1A adrenergic activity. The compounds are useful for treatment of disease conditions, such as peripheral vascular disease, congestive heart failure, hypertension and especially benign prostatic hypertrophy.

Methods and compositions for the detection, diagnosis, and prevention of cardiac conditions are provided. Polymorphisms of β1-adrenergic receptor are provided. The Gly389 β1-adrenergic receptor variants are not as responsive to treatment β blockers such as carvedilol, metoprolol or bisoprol. Thus, genotyping β1-adrenergic receptor polymorphisms is useful for predicting relative responsiveness to treatment with beta blockers. The Gly389 polymorphism also may be used, alone or in conjunction with other adrenergic receptor polymorphisms, to predict relative risk of developing cardiovascular diseases such as heart failure or to predict relative survival rate in patients with heart failure or other cardiovascular diseases. Also provided are transgenic mice and transgenic cells expressing the β1-adrenergic receptor polymorphisms, and their use in identifying therapeutic agents.

The present invention provides a method for identifying a subject having a risk of developing obesity, coronary microvasular dysfunction, or hypertension, comprising detection of the presence of a single nucleotide polymorphism (SNP) in a nucleic acid encoding an element of at least one beta-adrenergic receptor from the subject. The presence of the SNP is correlated with obesity, coronary microvascular dysfunction, or hypertension, and thereby identifies the subject as having a risk of developing obesity, coronary microvascular dysfunction, of hypertension. The subject invention also provides methods of identifying patients likely to benefit from the prescription of beta blocker hypertension medications. In various embodiments, the nucleic acids detected include those genes encoding ADRB1 (beta1AR), ADRB2 (beta2AR), ADRB3 (beta3AR), GNB3 (G protein beta3 subunit), or GNAS1 (Gs protien alpha subunit). Methods of treating identified individuals are also provided.

The invention discloses a yeast which has the stereoselective lipase activity and the application of the yeast in the preparation of an S-type betaxolol hydrochloride by using a biological separation method. The method selects one yeast with the stereoselective lipase activity by screening from the soil, utilizes an immobilized cell which is obtained by immobilizing the wet bacteria or sodium alginate-activated carbon-polyethylenimine as an enzyme preparation, carries out an enantiomer separation to a substrate which contains acyl group and prepares the S-type betaxolol hydrochloride. The conversion method is simple, the cost is low and the stereoselectivity is better. The usage of the bacterial strain can carry out the chiral separation of Beta-receptor blocker of betaxolol etc., ephedrine hydrochloride, epinephrine, levodropropizine, salbutamol sulfate, captopril, zofenopril and other compounds which contain hydroxy group or acyl group at the chiral center, thereby having important application value for promoting the development process of the chiral drugs of China.

The invention relates to pharmaceutical compositions comprising: (a) at least one angiotensin receptor blocker or a pharmaceutically acceptable salt thereof, and (b) at least one chemokine receptor pathway inhibitor or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising: (a) at least one angiotensin receptor blocker or a pharmaceutically acceptable salt thereof; and (b) at least one chemokine receptor pathway inhibitor or a pharmaceutically acceptable salt thereof which inhibits a component of the chemokine receptor pathway other than the chemokine receptor. Oral sustained release pharmaceutical compositions comprising the pharmaceutical composition, as well as injectable sustained release pharmaceutical compositions comprising the pharmaceutical composition are described. The invention further relates to tablets, capsules, injectable suspensions, and compositions for pulmonary or nasal delivery comprising the pharmaceutical composition. Also described are: methods for assessing the efficacy of the pharmaceutical composition; methods for assessing the inhibition or partial inhibition activity of the pharmaceutical composition; methods for the treatment, amelioration or prevention of a condition or disease comprising administering to a subject a therapeutically effective amount of the pharmaceutical composition; and the use of the pharmaceutical composition for the manufacture of a dosage form for the treatment of a disease.

The present invention relates to pharmaceutical compositions comprising the selective beta 1 (B1)-receptor blocker nebivolol and / or a pharmaceutically acceptable salt thereof and a liquid vehicle comprising a semifluorinated alkane. The pharmaceutical composition of the present invention is useful for topical administration, for example ophthalmic topical administration and for use in the treatment of glaucoma, increased intraocular pressure, ocular hypertension and / or a symptom associated therewith.

Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). Despite their relative inability to access brain and spinal cord, the compounds attenuate behavioral responses indicative of persistent pain in rodent models of inflammation and peripheral nerve injury, and suppresses noxious stimulus-evoked neuronal activation in spinal cord regions implicated in nociceptive processing. CBi receptor blockade prevents these effects. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the inhibition of peripheral FAAH would be of benefit. The compounds of the invention are according to the formula (I): in which R1 is a polar group. In some embodiments, R1 is selected from the group consisting of hydroxy and the physiologically hydro lysable esters thereof. R2 and R3 are independently selected from the group consisting of hydrogen and substituted or unsubstituted hydrocarbyl; each R4 is independently selected from the group consisting of halogen and substituted or unsubstituted hydrocarbyl and n is an integer from 0 to 4; each R5 is independently selected from the group consisting of halo and substituted or unsubstituted hydrocarbyl and m is an integer from 0 to 3; and R6 is substituted or unsubstituted cyclohexyl; and the pharmaceutically acceptable salts thereof.

The present invention discloses an application of benzamine in preparation of drugs for preventing and treating myocardial ischemia-reperfusion injury or ischemic heart disease. Through transcriptomedata analysis of peripheral blood of patients with acute coronary syndrome and based on co-expression pathways and a drug gene set enrichment analysis method, a list of drug candidates for preventingand treating the acute coronary syndrome are obtained and comprise several marketed drugs for the acute coronary syndrome, the benzamine having functions of preventing and treating the acute coronarysyndrome is not found in the list, besides, an effect of the benzamine is verified to be comparable to that of metoprolol, a common beta-receptor antagonist cardiovascular disease drug on a hypoxia-reoxygenation cell model that simulates the myocardial ischemia-reperfusion injury and ischemic heart disease, thus the benzamine can be used to prepare the drugs for preventing and treating the myocardial ischemia-reperfusion injury or the ischemic heart disease.

The present invention relates to the use of an Angiotensin II type 1 (AT1) receptor blocker for promoting sleep and / or the treatment of insomnia. It is based, at least in part, on the results of experiments performed using a validated rat model of stress-induced insomnia in which candesartan was found to ameliorate sleep disturbances induced by stress. Further, it was observed that this effect seems to be caused by blockade of AT1 receptors located in several brain regions that are key components of the neural circuitry activated during insomnia. In contrast to currently marketed treatments for insomnia, the AT1 receptor blocker was found to restore normal sleep without inhibiting REM sleep and / or inducing atypical wave components in the EEG.

The invention provides compounds which are selective PDE2 inhibitors for use in the treatment of tachycardia or tachyarrhythmia Such compounds are particularly suitable for use in the treatment of any of the following conditions: atrial tachycardia, atrial fibrillation, atrial flutter, paroxysmal supraventricular tachycardia, premature ventricular contractions (PVCs), ventricular fibrillation and ventricular tachycardia, and may be used alone or in combination therapy with other conventional cardiovascular drugs, e.g. beta-blockers. In particular, the invention provides compounds which are selective PDE2 inhibitors for use in the treatment of ventricular tachycardia in patients who are suffering from, or who are at risk of suffering from heart failure, CPVT or long QT syndrome.