28 results about "Adrenoceptor agonist" patented technology

There is herein provided a pharmaceutical formulation comprising one or more compounds that are β2-adrenergic receptor agonist, or a pharmaceutically acceptable salt thereof, and β3-adrenergic receptor agonist, or a pharmaceutically acceptable salt thereof, and optionally one or more pharmaceutically acceptable excipient, for use in the treatment or prophylaxis of obesity and other medical uses.

The invention relates to an ophthalmic spray combined preparation for relieving blepharoptosis or relieving red eyes from blepharoptosis. The ophthalmic spray combined preparation is characterized by comprising the following components in percentage by mass: 0.01-1.15% of an alpha-adrenergic receptor agonist, 0.01-1.15% of an emulsifier, 0.01-1.15% of an emulsifier and the balance of water. 0.1% to 0.3% of sodium hyaluronate; 0.01%-2% of an osmotic pressure regulator; the liquid medicine further comprises a pH buffering agent, wherein the concentration of the pH buffering agent is 0.002 M to 0.16 M; the thickening agent is one or a combination of more of hydroxyethyl cellulose, polyvinyl alcohol and povidone, and the mass percent of the vitamin A derivative and the vitamin E derivative is 0.01%-0.2%. The spray preparation comprises a spraying device, and the spray particle size ranges from 5 mu m to 500 mu m, preferably ranges from 5 mu m to 100 mu m, and more preferably ranges from 10 mu m to 30 mu m.

Disclosed are methods and compositions for treatment of androgenetic alopecia, telogen effluvium, hair shedding, and / or other forms of alopecia. The method involves: a) topically applying a composition including an androgenic agonist, an ADRB2- agonist, and / or a trace amine-associated receptor (TAAR) agonist; or b) orally administering a composition including an androgenic agonist, an adrenoceptor beta 2 (ADRB2) agonist, and / or a TAAR agonist; or c) administering a composition including an androgenic agonist, an adrenoceptor beta 2 (ADRB2) agonist, and / or a TAAR agonist via a transdermal, subdermal, or subcutaneous vehicle.

The present invention discloses a class of 4-(1H)-imidazole derivatives represented by the following formula (I), their pharmaceutically acceptable salts, racemic mixtures, enantiomers, optical isomers and tautomers, as well as pharmaceutical compositions containing them, and their use as α2-adrenergic receptor agonists, especially as α 2A -agonists and their methods of use. Compared with the prior art, the compounds of the present invention show more potent agonist activity and higher selectivity for α 2A -AR, superior to the positive drug dexmedetomidine; and at the same time have a potent in vivo sedative effect. #imgabs0#

Combinations of a muscarinic acetylcholine receptor antagonist and a beta 2 agonist for inhaled administration via the nose or mouth, compositions thereof, and methods of using them are provided.

There is provided herein a method of treatment comprising: (i) a first treatment cycle comprising administration of a therapeutically effective amount of a therapeutic agent, or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the therapeutic agent directly or indirectly induces muscle wasting; and (ii) a second treatment cycle following the discontinuation of the first treatment cycle, wherein the second treatment cycle comprises administration of a therapeutically effective amount of a β2-adrenergic receptor agonist, or a pharmaceutically acceptable salt thereof, to the subject, wherein the first and second treatment cycles are within the same therapeutic intervention.

This specification provides a β2-adrenergic receptor agonist or a pharmaceutically acceptable salt thereof for use in the treatment and / or prophylactic care of hyperglycemia or a disorder characterized by hyperglycemia, wherein the treatment and / or prophylactic care further comprises the administration of (a) insulin or a therapeutic insulin derivative, or (b) a therapeutic agent that stimulates the release of insulin.

The present disclosure relates to novel alpha-2 adrenergic receptor (α2AR) agonists and uses thereof. In particular, the present disclosure relates to imidazole containing compounds, in particular, of formula (I-A), formula (I-B), formula (I-C), formula (I-D), or formula (II). These compounds can be useful as peripherally selective α2AR agonists for the treatment or prevention of disease thereof, either used alone or in combination with a second therapeutical agent.

The present disclosure relates to novel sulfate salt forms of 2-(5-methoxyisochroman-1-yl)-4,5-dihydro-1H-imidazole (I). Compound (I) is a selective alpha2A adrenoceptor agonist and is useful in the treatment of anxiety, and for use as a sedative or analgesic agent, and other diseases were alpha2A agonism is desired.

There is provided herein a β2-adrenergic receptor agonist, or a pharmaceutically acceptable salt thereof, for use in the treatment and / or prophylaxis of hyperglycaemia or a disorder characterized by hyperglycaemia, wherein the treatment and / or prophylaxis further comprises administration of an SGLT2 inhibitor.

Described herein are compositions, devices, and methods useful for treating (reversing) and / or preventing fentanyl overdose resulting in respiratory failure or airway obstruction (FIVCC). Compositions are provided that include optimized amounts and / or ratios of two active ingredients, including: an alpha 2 adrenergic receptor agonist (e.g., lofexidine, dexmedetomidine, clonidine) and a short acting mu opioid receptor antagonist (e.g., naloxone); an alpha 2 adrenergic receptor agonist and a long acting mu opioid receptor antagonist (nalmefene); and an alpha 2 adrenergic receptor agonist and a fentanyl opioid analgesic. Methods and devices for concurrent delivery of combined active ingredients are also provided.

The present disclosure relates to novel alpha2 adrenergic receptor (alpha2AR) agonists and uses thereof. Specifically, the present disclosure relates to imidazole-containing compounds, in particular to compounds represented by formula (I-A), formula (I-B), formula (I-C), formula (I-D) or formula (II). The compounds are useful as peripheral selective alpha2AR agonists for the treatment or prevention of related diseases.

To provide methods for inhibiting postoperative inflammatory conditions following ophthalmologic surgical procedures by administering intraocularly during an ophthalmologic surgical procedure a solution including a nonsteroidal anti-inflammatory drug and an α-1 adrenergic mydriatic agent, such as a liquid irrigation solution of ketorolac and phenylephrine.SOLUTION: In one aspect, there is provided a method for inhibiting a postoperative inflammatory condition following an ophthalmologic surgical procedure, including: identifying a subject with an elevated risk of suffering from a postoperative inflammatory condition; and administering intraocularly to the subject during the ophthalmologic surgical procedure a solution including a nonsteroidal anti-inflammatory drug (NSAID) and an α-1 adrenergic receptor agonist mydriatic agent in an intraocular irrigation carrier.SELECTED DRAWING: None

A method for preparing an intermediate of an adrenergic receptor agonist. The method comprises the following steps: cyclizing the compound of formula E1 or the compound of formula E2 and the compound of formula F0 to obtain the compound of formula C, where R1 is methyl, ethyl, isopropyl, propyl, tert-butyl, or butyl; R3 is H, Cl, F or Br; and L1 and L2 are each individually a leaving group. The method uses easily available raw materials, avoids the use of toxic and harmful reagents, is mild in terms of reaction conditions, is simple to operate, achieves a substantial improvement in yield and reduction in cost, and is more favorable for commercial production.

The present disclosure relates to novel salts, particularly crystalline salts of 2-(5-methoxyisochroman-1-yl)-4,5-dihydro-1H-imidazole (I) which are suitable for use in the manufacture of pharmaceutical compositions. Compound (I) is selective alpha2A adrenoceptor agonist and is useful in the treatment of anxiety, and for use as a sedative or analgesic agent, and other diseases were alpha2A agonism is desired.

The invention provides a dry powder inhalation composition for inhalation, a dry powder inhalation for inhalation, a preparation method of the dry powder inhalation and an inhalation dry powder inhalation, and belongs to the technical field of pharmaceutical preparations. The dry powder inhalation composition comprises a first component and a second component, the first component is corticoid or pharmaceutically acceptable salt or isomer thereof; the second component is a beta2 adrenergic receptor agonist or a pharmaceutically acceptable salt or an isomer of the beta2 adrenergic receptor agonist; the molar ratio of the first component to the second component is (0.1-25): 1. According to the dry powder inhalation composition provided by the invention, the delivery efficiency of the first component and the second component in the dry powder inhalation composition can be higher than the delivery efficiency of a single component of the first component and the delivery efficiency of a single component of the second component, so that the drug effects of corticoid and a beta2 adrenergic receptor stimulant in the dry powder inhalation composition can be fully exerted; the traditional Chinese medicine composition can help patients with lung diseases such as mild and moderate asthma, chronic obstructive pneumonia and the like to relieve respiratory obstruction and has the effect of treating inflammation at the same time.

The invention relates to an alpha-adrenergic receptor agonist ophthalmic composition and application thereof. The composition comprises an alpha-adrenergic receptor agonist and an M choline receptor agonist. The ophthalmic composition provided by the invention can meet the requirements of different patients for improving short-distance vision and long-distance vision, and has a relatively long retention time up to 10 hours. In addition, the composition provided by the invention can quickly eliminate conjunctival congestion and asthenopia, and has a good curative effect on preventing and treating eye diseases such as presbyopia, ocular hypertension, xerophthalmia, myopia, hyperopia, strabismus, astigmatism, photophobia or glaucoma.

The present invention relates generally to methods of assessing platelet function, e.g., for assessing platelet function from a sample of a subject. These methods may be used to identify a subject based on the responsiveness or sensitivity of platelets of the subject to a platelet activating substance, such as collagen-related peptide (CRP), or thrombin, ADP, thromboxane A2, or adrenergic receptor agonist. The invention also provides a method for evaluating the level of CD36, the level of GPVI and / or the age of a subject in platelets of the subject as a functional indicator of the platelets of the subject. These methods can be used to predict the responsiveness of a subject to anti-platelet therapy, and thus can be part of a therapeutic method.

Provided herein is a pharmaceutical composition comprising two or more compounds, wherein each compound is independently a phosphodiesterase inhibitor, an adenosine receptor antagonist, a calcium channel blocker, a histamine H1-receptor agonist, a histamine H2-receptor agonist, a histamine H3-receptor antagonist, or a β2-adrenoreceptor agonist. Also provided herein is a method of treating, preventing, or ameliorating a cardiovascular disease in a subject, comprising administering to the subject in need thereof two or more compounds, wherein each compound is independently a phosphodiesterase inhibitor, an adenosine receptor antagonist, a calcium channel blocker, a histamine H1-receptor agonist, a histamine H2-receptor agonist, a histamine H3-receptor antagonist, or a β2-adrenoreceptor agonist.

The present application belongs to the field of medical technology, and in particular, relates to the use of β3-adrenergic receptor agonists in the preparation of drugs for preventing or / and treating abdominal aortic aneurysms. The present application discloses the use of β3-adrenergic receptor agonists in the preparation of drugs for preventing or / and treating abdominal aortic aneurysms. The present application aims at the problem that there is no effective drug in the prior art that can delay the progression of abdominal aortic aneurysms, and discloses a new application of β3-adrenergic receptor agonists.

The present invention relates to a transdermal composition comprising a compound selected from the group comprising formoterol, salbutamol, salmeterol, fenoterol, mixtures thereof or salts thereof, and dimethylsulfoxide. The present invention further relates to a composition comprising a compound selected from the group comprising salbutamol, clenbuterol or salts thereof, and comprising at least one of water or a monohydric alcohol.

Pharmaceutical formulations in powder form for intranasal administration of a pharmaceutically active agent, providing for sustained release and improved bioavailability of the active agent in the nasal cavity. In addition to the active agent and various carriers, the formulation comprise sustained release agent / s. Exemplary active agents are opioid receptor antagonists, such as naloxone, or adrenergic receptor agonists, such as epinephrine. Methods for the preparation of the disclosed pharmaceutical formulations and to methods of treatment of a subject in need thereof by intranasal administration of a pharmaceutically active agent are disclosed.

The invention discloses a sedative pharmaceutical composition special for proton therapy, the sedative pharmaceutical composition has a double-layer skeleton structure, the outer layer comprises a benzodiazepine derivative subjected to cyclodextrin inclusion treatment, and the inner layer comprises an alpha2-adrenergic receptor agonist wrapped by PLGA microspheres. The sedative pharmaceutical composition special for proton therapy can realize quick release-slow release biphasic regulation, the outer quick release layer takes effect within 5 minutes, the inner slow release layer keeps sedative for 2-4 hours, and the requirements of all treatment stages are met; meanwhile, the analgesic effect of the alpha2-adrenergic receptor stimulant is combined, so that the addiction of traditional opioids is avoided; and a pH-responsive nano-carrier (the disintegration threshold pH is 5.5 + / -0.2) is adopted, is only triggered and released in an acidic microenvironment of a proton treatment target region, and acts synchronously with an irradiation region.

The invention relates to the technical field of medicines, in particular to an ophthalmic pharmaceutical composition and application thereof. The ophthalmic pharmaceutical composition comprises one or two of a choline receptor stimulant, an anti-cholinesterase drug, an alpha-adrenergic receptor stimulant or a choline receptor antagonist. The ophthalmic pharmaceutical composition disclosed by the invention has a very good curative effect on myopia, takes effect quickly, is high in patient compliance, has no specific use time and occasion, and changes the conventional mode of using myopia drugs at night.

Combinations of a muscarinic acetylcholine receptor antagonist and a beta 2 agonist for inhaled administration via the nose or mouth, compositions thereof, and methods of using them are provided.

The present disclosure relates to imidazole containing compounds, in particular, of formula (La) or formula (I-b). These compounds can be useful as alpha2 adrenergic receptor (a2AR) agonists for the treatment of disease thereof.

The invention provides a liquid pharmaceutical composition comprising: a) at least one long-acting muscarinic receptor antagonist (LAMA) selected from the group consisting of glycopyrronium bromide, ipratropium bromide, umiclidium bromide, and revefenacin; b) at least one long-acting adrenoceptor agonist (LABA) selected from the group consisting of formoterol fumarate, salmeterol xinofoate; alformoterol tartarate, and vilanterol trifenate; and c) at least one inhaled corticosteroid (ICS) selected from the group consisting of beclomethasone dipropionate, budesonide, ciclesonide, fluticasone furoate, and fluticasone propionate; and wherein the composition is in the form of a solution for aerosolization, as well as methods and devices for use of the composition.

Described herein is a crystalline form of a hemihydrate of the β-3 adrenergic receptor agonist vibegron. The disclosure also relates to preparations of the crystalline form, pharmaceutical compositions thereof, methods of making the crystalline form, and methods of using the crystalline form in the treatment of overactive bladder.