82 results about "Α2 adrenergic receptor" patented technology

RNA interference is provided for inhibition of ocular hypertension target mRNA expression for lowering elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Ocular hypertension targets include carbonic anhydrase II, IV, and XII; β1- and β2 adrenergic receptors; acetylcholinesterase; Na+ / K+-ATPase; and Na—K-2Cl cotransporter. Ocular hypertension is treated by administering interfering RNAs of the present invention.

RNA interference is provided for inhibition of ocular hypertension target mRNA expression for lowering elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Ocular hypertension targets include carbonic anhydrase II, IV, and XII; β1- and β2 adrenergic receptors; acetylcholinesterase; Na+ / K+-ATPase; and Na—K-2Cl cotransporter. Ocular hypertension is treated by administering interfering RNAs of the present invention.

Methods and kits for treating or preventing psoriasis or a symptom associated with psoriasis in a subject are described. The methods involve topical applications to the subject a therapeutically effective amount of an α2 adrenergic receptor agonist, such as brimonidine.

The present invention generally relates to compositions and kits comprising a β2-AR agonist and a modulator of a β2-AR regulator gene, where the modulator of the β2-AR regulator gene inhibits the internalization and / or degradation of the β2-ad-renergic receptor (β2-AR). More specifically, the present invention relates to the use of an agonist of β2-adrenergic receptor (β2-AR) and an agent which inhibits agonist induced β2-adrenergic receptor (β2-AR) internalization and / or degradation in method for the treatment of a respiratory disorder in a subject.

RNA interference is provided for inhibition of ocular hypertension target mRNA expression for lowering elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Ocular hypertension targets include carbonic anhydrase II, IV, and XII; β1- and β2 adrenergic receptors; acetylcholinesterase; Na+ / K+-ATPase; and Na—K-2Cl cotransporter. Ocular hypertension is treated by administering interfering RNAs of the present invention.

Methods, compounds, and topical formulations for reduction of skin sagging, creasing and / or wrinkling are disclosed. The methods comprise topically applying a composition comprising an α2 adrenergic receptor agonist. Amelioration of skin sagging, creasing and / or wrinkling begins within minutes after topical application of a disclosed composition. A single application can significantly reduce skin sagging, creasing and / or wrinkling for at least about 8 hours.

The invention provides the structure of a human β2-adrenergic receptor, a cholesterol consensus motif, and methods of identifying modulators of G-protein coupled receptors (GPCRs). Methods of using the modulators of the receptor, GPCRs, and the cholesterol consensus motif are also provided.

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 compound of formula (I) or a pharmaceutically-acceptable salt, solvate or stereoisomer thereof wherein R1 is a group chosen from —CH2OH and —NHC(O)H; R2 is a hydrogen atom or R1 together with R2 form the group —NH—C(O)—CH═CH—, wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R1 and the carbon atom is bound to the carbon atom in the phenyl ring holding R2; R3 is chosen from a hydrogen atom, a halogen atom and groups chosen from —SO—R5, —SO2—R5, —NH—CO—NH2, —CO—NH2, hydantoino, C1-4alkyl, C1-4alkoxy and —SO2NR5R6; R4 is chosen from a hydrogen atom, a halogen atom and a C1-4 alkyl group; R5 is chosen from a C1-4 alkyl group and a C3-8 cycloalkyl group; R6 is independently chosen from a hydrogen atom and a C1-4 alkyl group; n, p and q are independently 0, 1, 2, 3 or 4; m and s are independently 0, 1, 2 or 3; and r is 0, 1 or 2 with the provisos that at least one of m and r is not 0, the sum n+m+p+q+r+s is 7, 8, 9, 10, 11, 12 or 13, and the sum q+r+s is 2, 3, 4, 5 or 6.

Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and / or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and / or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and / or sedatory activity are useful for treating pain and other conditions with minimal side effects.

Disclosed are multibinding compounds which are β2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

The present invention is directed to crystalline addition salts of (i) 8-hydroxyquinolin-2(1H)-one derivatives and (ii) a hydroxycarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvates thereof.

The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the β2 adrenergic receptor.

Compounds of Formula 1where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and / or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and / or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and / or sedatory activity are useful for treating pain and other conditions with minimal side effects.

Described is the use in the treatment of either male or female sexual dysfunction of selective antagonists of the α1B-adrenergic receptor and the pharmaceutical compositions containing them as compounds capable of helping the sexual act avoiding at the same time excessive side effects due to acute hypotension.

Methods, compounds, and topical formulations for reduction of skin sagging, creasing and / or wrinkling are disclosed. The methods comprise topically applying a composition comprising an α2 adrenergic receptor agonist. Amelioration of skin sagging, creasing and / or wrinkling begins within minutes after topical application of a disclosed composition. A single application can significantly reduce skin sagging, creasing and / or wrinkling for at least about 8 hours.

Compounds of Formula 1where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and / or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and / or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and / or sedatory activity are useful for treating pain and other conditions with minimal side effects.

The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the β2 adrenergic receptor.

The present invention provides a compound, which is a hydroxyquinolinone derivative of formula (I),in the form of a racemate, a stereoisomer or a mixture of stereoisomers, or a pharmaceutically acceptable salt or solvate thereof, for use in a method of treating, for example, a pulmonary disease or condition associated with β2 adrenergic receptor activity in a mammal, in which the compound is administered by the inhalatory route at a metered nominal dose of less than 5 μg.

The invention discloses a medicament for treating amphetamine type stimulant dependency and mixed dependency of amphetamine type stimulants and opiates substances. The medicament is prepared from the following components by weight percent: 2-95% of antipsychotics, 0.001-5% of alpha2 adrenergic agonists, 0-5% of anticholinergic agent, 0-80% of nonopioid analgesic, and 0-10% of benzodiazepine. The pharmaceutical composition disclosed by the invention achieves an ideal effect when the symptoms of a sufferer abusing stimulants such as benzedrine, or abusing the opiates substances in a merging manner are treated; the withdrawal symptom can be rapidly and obviously controlled; the detoxification recovery rate can be up to over 90%.

The invention provides well-defined aryl fluoroethyl ureas that are useful as selective alpha2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of alpha2 adrenergic receptors.

Compounds of Formula 1where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and / or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and / or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and / or sedatory activity are useful for treating pain and other conditions with minimal side effects.

The present invention provides stereoscopically-pure diastereomers of Formula I:In a preferred embodiment, the stereoisomers of the present invention are of Formula II, depicted below:R2, R3 and R4 are independently H, OH, OCH3, CH2OH, NHCONH2, NH2, halogen or CF3, and R1 is pyridine, or an amine which may be substituted with hydrogen, lower alkyl, lower alkylenearyl, lower alkylenephenyl, lower alkylenehydroxyphenyl, lower alkyleneamine, lower alkyleneaminoaryl, lower alkylaminohydroxyphenyl, or a similar functional group. R5 is hydrogen, hydroxyl or methyl; R6 is hydrogen, lower alkyl, lower alkylenaryl, lower alkylenephenyl, lower alkylenehydroxyphenyl, lower alkyleneamine, lower alkyleneaminoaryl, lower alkylaminohydroxyphenyl, and the like. For both Formula I and Formual II, the first carbon on the side chain progressing from the ring is preferably in the R-configuration. The second carbon atom on the side chain of Formula II, which is attached to R5, may or may not be a chiral center. However, when the second carbon atom is a chiral center, it is preferably in the S-configuration. The present invention contemplates each stereoisomer of Formula I and II in substantially-pure form.The present invention also provides methods of relieving nasal, sinus and bronchial congestion and of treating attention deficit hyperactivity disorder and obesity. The present stereoisomers may also be used to induce pupil dilation. These methods include administering to a mammal a composition containing a therapeutically effective amount of a stereoscopically-pure stereoisomer of Formula I or II with a pharmaceutically acceptable excipient.