266 results about "Adrenergic receptor agonists" patented technology

The present invention relates to a method of treating, reducing, inhibiting, preventing and/or reversing cutaneous facial flushing caused by abnormal, endogenously-induced vasomotor instability associated with, but not limited to acne rosacea, menopause-associated hot flashes, hot flashes resulting from orchiectomy or ingestion of substances capable of inducing a cutaneous facial flushing reaction (e.g.: alcohol, chocolate, spices) by topical dermatological application of an effective dose of a composition comprising at least one α₂ adrenergic receptor agonist (such as a (2-imidazolin-2-ylamino) quinoxaline derivative such as brimonidine tartrate)and a suitable carrier.

The present invention pertains to the identification of moieties and methods of using the same for preventing tolerance to bronchodilators. More specifically, the present invention pertains to the identification of compositions and methods which are capable of preventing tolerance to beta2-adrenergic agonists. The methods and compositions according to the invention are also useful as analytical tools for functional studies and as combination therapeutic tools.

Compositions, formulations, methods, and systems for treating regional fat deposits comprise contacting a targeted fat deposit with a composition comprising long acting beta-2 adrenergic receptor agonist and a compound that reduces desensitization of the target tissue to the long acting beta-2 adrenergic receptor agonist, for example, glucocorticosteroids and/or ketotifen. Embodiments of the composition are administered, for example, by injection, and/or transdermally.

Pharmaceutical compositions comprising at least one alpha2-adrenergic agonist or baclofen and at least one alpha1-adrenergic agonist are disclosed. Pharmaceutical compositions comprising tizanidine and modafinil are disclosed. Methods for reducing somnolence, sleepiness, lethargy, dizziness, drowsiness, somnolence, tiredness, lightheadedness, increased weakness, confusion, unsteadiness, clumsiness, or a combination of the symptoms thereof in a human patient; treating pain; and attenuating muscle spasticity, using pharmaceutical compositions comprising at least one alpha2-adrenergic agonist or baclofen and at least one alpha1-adrenergic agonist are disclosed.

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 novel β₂ adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β₂ adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

A method is provided for using α₂δ subunit calcium channel modulators or other compounds that interact with the α₂δ calcium channel subunit in combination with one or more compounds with smooth muscle modulatory effects to treat pain. According to the present invention, α₂δ subunit calcium channel modulators include GABA analogs (e.g., gabapentin and pregabalin), fused bicyclic or tricyclic amino acid analogs of gabapentin, and amino acid compounds. Compounds with smooth muscle modulatory effects include antimuscarinics, β3 adrenergic agonists, spasmolytics, neurokinin receptor antagonists, bradykinin receptor antagonists, and nitric oxide donors.

The invention features a method of treating a B-cell proliferative disorder by administering to a patient a BAR agonist, e.g., formulated for administration by a route other than inhalation (such as for oral or intravenous administration), in an amount effective to treat the B-cell proliferative disorder. The BAR agonist may be administered as a monotherapy or in combination with one or more other agents, e.g., a PDE inhibitor, an A2A receptor agonist, or an antiproliferative compound, in amounts that together are effective to treat the B-cell proliferative disorder. The invention further features pharmaceutical compositions and kits including a BAR agonist, alone or in combination with additional agents, for the treatment of a B-cell proliferative disorder.

PCT No. PCT/US97/15230 Sec. 371 Date May 4, 1998 Sec. 102(e) Date May 4, 1998 PCT Filed Aug. 28, 1997 PCT Pub. No. WO98/09625 PCT Pub. Date Mar. 12, 1998Disclosed herein are selective beta 3 adrenergic agonists represented by the following structural formula: The variables in the structural formula shown above are defined in the specification. Also disclosed are methods of using these compounds for agonizing the beta 3 adrenergic receptor in patients in need of such treatment, for example, patients in need of treatment for obesity or Type II diabetes.

This invention relates to methods of treating pulmonary diseases in patients that beta adrenergic receptor agonist therapy is not effective. The method comprises the steps of: identifying a patient who suffers from a pulmonary disease and has reduced responsiveness to treatment with one or more beta adrenergic receptor agonists, and administering to the patient an effective amount of a Rho kinase inhibitor compound, wherein said pulmonary disease is selected from the group consisting of: asthma, chronic obstructive pulmonary disease, respiratory tract illness caused by respiratory syncytial virus infection such as RSV-induced wheezing, airway hyperreactivity, or bronchiolitis, bronchiectasis, alpha-1-antitrypsin deficiency, lymphangioleiomyomatosis, cystic fibrosis, bronchiolitis or wheezing caused by agents other than respiratory syncytial virus, chronic bronchitis, and occupational lung diseases.

Guanosine triphosphate pathway tetrahydrobiopterin synthesis antagonist and/or pterin salvage pathway tetrahydrobiopterin synthesis antagonists are administered to inhibit nitric oxide synthesis from arginine in vascular cells in a subject in need of such inhibition (e.g., for prophylactic or curative effect for endotoxin- or cytokine-induced hypotension or for restoration of vascular contractile sensitivity to pressor agents in the treatment of such hypotension). The tetrahydrobiopterin synthesis antagonist may be administered with alpha 1-adrenergic agonist or with nitric oxide synthase inhibitor. The tetrahydrobiopterin synthesis antagonists are also administered to attenuate inflammation caused by induced nitric oxide production in immune cells. Unwanted counterproductive or side effects can be eliminated or ameliorated by administration additionally of levodopa with or without carbidopa and L-5-hydroxytryptophane.

The invention provides a crystalline salt form of a novel β₂ adrenergic receptor agonist. The invention also provides pharmaceutical compositions comprising the crystalline form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt form to treat diseases associated with β₂ adrenergic receptor activity, and processes useful for preparing such a crystalline compound.

A method is provided for using α₂δ subunit calcium channel modulators or other compounds that interact with the α₂δ calcium channel subunit in combination with one or more compounds with smooth muscle modulatory effects to treat and/or alleviate the symptoms associated with painful and non-painful lower urinary tract disorders in normal and spinal cord injured patients. According to the present invention, α₂δ subunit calcium channel modulators include GABA analogs, e.g., gabapentin and pregabalin, fused bicyclic or tricyclic amino acid analogs of gabapentin, and amino acid compounds. Compounds with smooth muscle modulatory effects include antimuscarinics, β3 adrenergic agonists, spasmolytics, neurokinin receptor antagonists, bradykinin receptor antagonists, and nitric oxide donors.

Disclosed is an extended release pharmaceutical formulation containing at least an alpha-2 adrenergic agonist, such as tizanidine, for the treatment and prevention of spasticity in a subject, e.g., painful inflammatory conditions associated with skeletal muscle spasms.

Compositions and methods that employ various combinations of such factors as retinoic acid signaling inhibitors, antioxidants, BMP4, VEGF, prostaglandin E₂ pathway stimulants, TPO, SCF, FLT-3, EPO, TGFβ1, p38 MAPK inhibitors, beta adrenergic receptor agonists, cell cycle inhibitors, RXR agonists, Cripto, and chromatin remodelers to drive differentiation of pluripotent stem cells towards primitive blood cells. Uses of such primitive blood cells are provided.

The present invention provides compositions and stable liquid formulations comprising alpha adrenergic receptor antagonists and use thereof for increasing blood flow. In one embodiment, the stable liquid formulations of this invention are useful for reversing the effects of an anesthetic agent, preferably a long-lasting local anesthetic agent administered in conjunction with an alpha adrenergic receptor agonist. The invention further relates to drug delivery systems for administering alpha adrenergic receptor antagonists.

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.

This invention provides biphenyl derivatives of formula I: wherein R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both beta2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.