82 results about "Adrenergic receptor sites" patented technology

Methods and compositions for the treatment of pain and other conditions in a mammal using a composition which directly or indirectly stimulates alpha 2 adrenoreceptor agonist activity with a minimum of sedation or other side effects.

The present invention is a new stable extended release drug composition particularly suitable for use as a beta-adrenoreceptor antagonist agent. The present invention is specifically a drug composition comprising a pharmaceutical, a methacrylic acid copolymer and a matrix forming agent, and a method for manufacturing same. When applied to highly soluble drugs like metoprolol succinate, the resulting drug composition is characterized by an extended-release profile.

The subject invention relates to methods of treating alpha-2 adenoreceptor modulated disorders, comprising administration, to a mammal in need of such treatment, of a safe and effective amount of a compound having the following structure: wherein: (a) R is unsubstituted C1-C3 alkanyl or alkenyl; and (b) R' is selected from hydrogen; unsubstituted C1-C3 alkanyl or alkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thiol; and halo. The subject invention also relates compounds and compositions for preventing or treating of disorders modulated by alpha-2 adrenoreceptors.

The present invention relates to new compounds of Formula (I): and pharmaceutically acceptable forms thereof, use of the compounds as α1a and / or α1d adrenoreceptor modulators, including use of a pharmaceutical composition, medicine or medicament comprising said compounds, a process to prepare said compounds and a method for treating an α1a and / or α1d adrenoreceptor mediated disorder.

In its many embodiments, the present invention provides a novel class of indolines as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.

The invention relates to an aryl [a] indole [2,3-g] quinolizine compound as well as a preparation method, a pharmaceutical composition and application thereof, and particularly relates to a aryl [a] indole [2,3-g] quinolizine compound with a novel structure as shown in a general formula (I) and a derivative, a preparation method and a pharmaceutical composition thereof and application of the aryl [a] indole [2,3-g] quinolizine compound in preparation of a drug for treating diseases related to alpha 1-adrenoreceptor and urinary system diseases, such as benign prostatic hyperplasia, uroschesis and bladder outlet obstruction, especially.

The invention relates to the combination of one or more beta-blockers and of one or more Kv1.5 blockers, in particular phenylcarboxamides of the formula la and / or lb and / or physiologically tolerable salts thereof, and the use of the combination for the treatment or prophylaxis of atrial arrhythmias.

The invention relates to an asymmetric hydrogen transfer synthesis method for (R,R)-formoterol, and relates to a novel method for synthesizing an optical pure beta 2-adrenoreceptor excitant, namely formoterol. The method comprises: firstly, taking 4-hydroxyl-3 nitroacetophenone as a raw material, using benzyl groups to protect phenolic hydroxyl groups, and obtaining alpha-bromo keto after bromination; secondly, taking (S,S)-Rh-PEG-BsDPEN as a catalyst and formic acid and derivatives of the formic acid as hydrogen sources, and synthesizing chiral alcohol intermediate by an asymmetric hydrogen transfer method; thirdly, using (R)-alpha-methyl phenylethylamine and methoxyl phenylacetone to generate imine compounds, and obtaining chiral amine intermediate through hydrogenation reduction under the catalysis of Pt / C; and fourthly, reacting and coupling the chiral alcohol intermediate and the chiral amine intermediate, removing protective groups, and obtaining the (R,R)-formoterol. The invention uses the asymmetric hydrogen transfer method and a chiral auxiliary reagent to synthesize the (R,R)-formoterol, and has high yield and good ee value. Compared with a method for synthesizing chiral formoterol through chemical splitting, the method has the advantages of high total yield, mild reaction conditions, low cost and so on, and is favorable for industrial production.

Method for the treatment of conditions including ocular and neurodegenerative conditions in a mammal using a composition which comprises an effective amount of an alpha 1 adrenoreceptor antagonist.

In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as α2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the α2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.

The present invention relates to compounds according to formula (I), a process for preparing them, the intermediate compounds of the process and the use of the compounds in the manufacture of a medicament for use in treating diseases such as ARDS, pulmonary emphysema, bronchitis, bronchiectasis, COPD, asthma and rhinitis. The compounds are beta2 adrenoreceptor agonists.

In its many embodiments, the present invention provides a novel class of indolines as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.

The invention provides compounds that bind with high affinities to the μ-, δ-and κ-opioid receptors and α2-adrenoreceptor. In addition to providing these compounds with novel pharmacological binding properties, the invention also describes detailed novel methods for the preparation of representative compounds and a scheme for the synthesis of related compounds that bind to the opioid receptors and / or α2-adrenoreceptor.

The present invention relates to piperidine substituted cyclohexane-1,4-diamine compounds of Formula (I) and pharmaceutically acceptable forms thereof, as α1a / α1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as method of treatments.

The present invention relates to the use of compositions comprising receptor ligands obtainable by a process comprising fermenting a food material, comprising animal milk or vegetable proteins, with lactic acid bacteria to obtain a fermented food or feed material that comprises ligands of specific adrenoreceptors and / or serotonin receptors. The fermented food or feed material is useful e.g. for reducing and / or stabilizing heart rate in a mammal. It may furthermore be used for treatment and / or relief of erectile dysfunctions and for treatment and / or relief of benign prostate hypertrophy (BPH), in a mammal.

A propanol amine type ether compound prepared from paeonol and its application in preparing the beta-adrenoreceptor paralyser kind of medicines for preventing and treating cardiovascular and cerebrovascular diseases are disclosed. Said ether compound is 1-isopropylamino-3-(2-acetyl-5-methoxy-phenoxy)-2-propanol. Its advantages are high pharmacological activity and low toxic by-effect.

The invention provides a pharmaceutical product comprising, in combination, (1) a named glucocorticosteroid receptor agonist and (2) a beta2 adrenoreceptor agonist, a dual beta 2 adrenoreceptor agonist / M3 receptor antagonist, a muscarinic antagonist, a p38 kinase inhibitor, a neutrophil elastase inhibitor, a phosphodiesterase PDE4 inhibitor, an IKK2 kinase inhibitor or a non-steroidal glucocorticoid receptor agonist, and the use of said product in treating respiratory diseases.

Disclosed herein is a method for screening for the allele associated with a desired SCS phenotype, which comprises: obtaining a DNA sample from a bull to be tested for the desired SCS phenotype; and detecting the presence of an adenine at position 11 in a gene encoding a bovine beta2-adrenoreceptor. Also disclosed is a milling attribute PCR-RFLP kit containing a pair of primers which flank the 11th nucleotide position of the bovine beta2-adrenoreceptor gene, and a restriction enzyme specific for the CCCGGG site, which can be SmaI.

In its many embodiments, the present invention provides a novel class of heterocyclic derivatives as a2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the a2C adrenergic receptors using such compounds or pharmaceutical compositions.

The invention provides a cyproheptadine hydrochloride immune colloidal gold detection card and a preparation method thereof, and relates to the technical field of beta-adrenoreceptor agonist detection. According to the present invention, the test paper strip in the detection card housing comprises a PVC glue plate, a sample pad, a colloidal gold conjugation pad, a coating membrane and a water absorbing pad, wherein the colloidal gold membrane is a glass cellulose membrane containing cyproheptadine hydrochloride monoclonal antibody, the coating membrane is a nitrocellulose membrane and is provided with a T line and a C line, a cyproheptadine hydrochloride protein conjugate is coated on the T line, and a goat anti-mouse IgG antibody is coated on the C line; and the detection card and the detection method are effectively used for cyproheptadine hydrochloride detection, and advantages of convenience, rapidness and accurate result are provided.

The invention provides compounds that bind with high affinities to the μ-, δ- and κ-opioid receptors and α2-adrenoreceptor. In addition to providing these compounds with novel pharmacological binding properties, the invention also describes detailed novel methods for the preparation of representative compounds and a scheme for the synthesis of related compounds that bind to the opioid receptors and / or α2-adrenoreceptor.

Provided herein is a pharmaceutical composition comprising (i) a phosphodiesterase inhibitor or an adenosine receptor antagonist, (ii) a calcium channel blocker, (iii) a histamine H1-receptor agonist, a histamine H2-receptor agonist, or a histamine H3-receptor antagonist, and (iv) a β2-adrenoreceptor agonist; wherein at least one of two or more active pharmaceutical compounds is deuterium enriched. Also provided herein is a pharmaceutical composition comprising at least one of two or more deuterated compounds which increase pharmacokinetic half-life (increasing the duration of action) and reduce side effects by allowing for reduction of the dose levels. A method of use thereof pharmaceutical composition for treating, preventing, or ameliorating a cardiovascular disease.

The present invention relates to the use of compositions comprising receptor ligands obtainable by a process comprising fermenting a food material, comprising animal milk or vegetable proteins, with lactic acid bacteria to obtain a fermented food or feed material that comprises ligands of specific adrenoreceptors and / or serotonin receptors. The fermented food or feed material is useful e.g. for reducing and / or stabilizing heart rate in a mammal. It may furthermore be used for treatment and / or relief of erectile dysfunctions and for treatment and / or relief of benign prostate hypertrophy (BPH), in a mammal.

The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereo- chemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having se- lective a2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are usefull for the prevention and / or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and / or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.

The invention provides beta3-adrenoreceptor agonists, pharmaceutical compositions comprising beta3-adrenoreceptor agonist compounds, and methods of using such compounds for stimulating, regulating or modulating metabolism of fats in adipose tissue in animals.

The invention provides beta3-adrenoreceptor agonists, pharmaceutical compositions comprising beta3-adrenoreceptor agonist compounds, and methods of using such compounds for stimulating, regulating or modulating metabolism of fats in adipose tissue in animals.

The present invention relates to compounds according to formula (I) , a process for preparing them, the intermediate compounds of the process and the use of the compounds in the manufacture of a medicament for use in treating diseases such as ARDS, pulmonary emphysema, bronchitis, bronchiectasis, COPD, asthma and rhinitis. The compounds are beta2 adrenoreceptor agonists.