33 results about "Receptor blockade" patented technology

A system for treating infantile hemangioma includes a first active substance delivery portion and a second active substance delivery portion. The first active substance delivery part delivers a first active substance to the superficial surface of the skin; the second active material delivery unit delivers a second active material to the deep part of the skin. The first active substance contains a beta receptor blocker, and the second active substance contains an antibiotic. Through verification, the beta receptor blocker and the antibiotic are delivered subcutaneously, and the effect of synergistically enhancing anti-angiogenesis and hardening promotion on infantile hemangioma is achieved.

Transdermal delivery of beta blockers to treat Infantile Hemangiomas (IH) with reduced systemic circulation of the active drug and reduced or eliminated drug exposure to internal organs. In some embodiments, the beta blocker is esmolol. Pharmaceutical compositions according to the invention may be formulated lotions, creams, ointments, gels, foams, liquid dispersions, solutions, or aerosols.

Provided herein are methods of treating patients by administering aficamten, or a pharmaceutically acceptable salt thereof, including in combination with beta blockers. The treatment methods include improving heart rate reserve, peak metabolic equivalents (METs), exercise duration, peak oxygen uptake (pVO2) as well as other parameters related to exercise capacity.

In various aspects and embodiments provided are compositions and methods for identifying patients in need of or desiring improvement of cognition and / or treating a neurodegenerative disease in a patient and treating such patient. More specifically, the disclosure in some embodiments includes administration of a β-AR agonist (such as a β-agent), a PDE inhibitor or adenosine antagonist, and optionally a peripherally acting β-blocker (PABRA) to a patient in need thereof.

In various aspects and embodiments provided are compositions and methods for identifying patients in need of improving cognition and / or treating a neurodegenerative disease in a patient and treating such patient. More specifically, the disclosure in some embodiments includes administration of a β-AR agonist and a peripherally acting β-blocker (PABRA) to a patient in need thereof.

In various aspects and embodiments provided are compositions and methods for identifying patients in need of or desiring improvement of cognition and / or treating a neurodegenerative disease in a patient and treating such patient. More specifically, the disclosure in some embodiments includes administration of a β-AR agonist (such as a β-agent), a PDE inhibitor or adenosine antagonist, and optionally a peripherally acting β-blocker (PABRA) to a patient in need thereof.

This invention discloses a novel use of carvedilol or its salts and compositions, as well as the composition and its preparation method. The β-blocker or pharmaceutical composition provided by this invention has good efficacy in preventing, treating, and / or alleviating drug-induced liver injury, effectively reducing mortality caused by this disease; simultaneously, it can significantly reduce serum transaminase levels, alleviate symptoms such as liver and spleen edema, and has a good inhibitory effect on pro-inflammatory cytokines. Furthermore, experimental results further indicate that the combination of the β-blocker and pharmaceutically acceptable excipients (steviosides and / or glycyrrhizate) has good safety and is easily dissolved, released, and / or absorbed, improving the bioavailability of carvedilol and exhibiting a synergistic effect, showing promising application prospects.

The present disclosure is directed to chemical compounds and to the use of such compounds in the treatment of diseases associated with an adrenergic receptor. In certain embodiments of the methods disclosed herein, the methods include administering to the subject a compound as disclosed herein and a peripherally acting P-blocker (PABRA).

Methods are provided to prevent and to treat diabetic retinopathy by using Calcium channel blockers, Angiotensin-Converting Enzyme (ACE) Inhibitors, or angiotensin receptor blockers (ARB), and more particularly, to a method to prevent and treat diabetic retinopathy by using calcium channel blockers, Angiotensin-Converting Enzyme Inhibitors, or angiotensin receptor blockers that may not need to be taken orally, but may also be administered by ophthalmic preparation directly onto or into the eye where diabetic retinopathy is formed, to increase the capillary network and augment the blood supply to the anatomy of the eye.

The invention relates to a non-aqueous oral solution comprising: losartan potassium in an amount of 0.01 mg / mL to 50 mg / mL, such as 10 mg / mL; a solubiliser, such as polyethylene glycol 400 in an amoun

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 that inhibits a component of the chemokine receptor pathway other than the chemokine receptor. Sustained-release oral pharmaceutical compositions comprising the pharmaceutical composition are described, as well as sustained-release injectable pharmaceutical compositions comprising the pharmaceutical composition.The invention further relates to tablets, capsules, injectable suspensions, and compositions for pulmonary or nasal administration comprising the pharmaceutical composition. Also described are: methods for evaluating the efficacy of the pharmaceutical composition; methods for evaluating the inhibitory or partial inhibitory activity of the pharmaceutical composition; methods for treating, alleviating, or preventing a condition or disease comprising administering a therapeutically effective amount of the pharmaceutical composition to a subject; and the use of the pharmaceutical composition for manufacturing a pharmaceutical dosage form for the treatment of a disease.

The present invention relates to pharmaceutical composition comprising the beta 1 (β1)-receptor blocker timolol and a liquid vehicle comprising a semifluorinated alkane. The pharmaceutical composition of the present invention may be 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.

The invention relates to the therapeutic application of multifunctional compounds that act as α2 adrenoreceptor antagonists and cholinesterase inhibitors for the treatment of Alzheimer's disease and other neurodegenerative diseases, or the concomitant use of a mixture of an α2 adrenoreceptor antagonist and a cholinesterase inhibitor to achieve the same effect.

In some aspects thereof, the present invention discloses compositions and methods for treating premature ejaculation utilizing tamsulosin at a 0.2 milligram dose administered orally or transdermally every 48 hours. Tamsulosin functions as a selective antagonist of alpha-1a and 1b adrenergic as well as 5HT1A serotonergic receptors implicated in seminal emission pathways. The quantity and frequency of dosing provides an optimal degree of reversible receptor blockade to mildly inhibit sympathetic and serotonergic mediated smooth muscle contraction kinetics governing seminal fluid secretion and transport. This marginally suppresses rate of emission to prolong intercourse without profoundly arresting physiological processes underlying ejaculation.

A use of a composition in the preparation of a drug. The composition comprises taurine and a β-blocker.

The present disclosure relates to treatment of Hypothalamic Obesity with Tesofensine alone or in combination with a beta-blocker. In particular the disclosure relates to treatments that lead to weight loss, loss of fat mass, in particular visceral fat, and to reduction of symptoms of pre-diabetes in patients suffering from Hypothalamic Obesity.

The invention provides a drug treatment prognosis risk score for ejection fraction reduction type and intermediate type heart failure and application thereof, and particularly relates to a multi-gene genetic risk score for influence of beta-receptor blockers on ejection fraction reduction type and intermediate type heart failure prognosis and application thereof. According to the method, ejection fraction reduction type and intermediate type heart failure drug treatment prognosis risk PRS scores are established on the basis of polygene single nucleotide polymorphic sites, and ejection fraction reduction type and intermediate type heart failure people sensitive to beta-receptor blockers can be well recognized.

In various aspects and embodiments provided are compositions and methods for identifying patients in need of improving cognition and / or treating a neurodegenerative disease in a patient and treating such patient. More specifically, the disclosure in some embodiments includes administration of a β-AR agonist and a peripherally acting β-blocker (PABRA) to a patient in need thereof.

In various aspects and embodiments provided are compositions and methods for identifying patients in need of improving cognition and / or treating a neurodegenerative disease in a patient and treating such patient. More specifically, the disclosure in some embodiments includes administration of a β-AR agonist (such as a β-agent) and a peripherally acting β-blocker (PABRA) to a patient in need thereof.

Methods of treatment comprising administering a therapeutically effective amount of a myosin modulator or a pharmaceutically acceptable salt thereof to a subject in need thereof and diagnostic methods useful in connection with those treatments are disclosed herein. Treatments performed in the absence of beta blocker therapy or with reduced beta blocker therapy are also disclosed.

Provided herein are methods of treating patients by administering aficamten, or a pharmaceutically acceptable salt thereof, including in combination with beta blockers. The treatment methods include improving heart rate reserve, peak metabolic equivalents (METs), exercise duration, peak oxygen uptake (pVCE) as well as other parameters related to exercise capacity.

The application provides a reduced ejection fraction and intermediate heart failure drug treatment prognosis risk score and application thereof, in particular, a multi-gene genetic risk score for affecting the prognosis of a reduced ejection fraction and intermediate heart failure by a beta-receptor blocker and application thereof. The application establishes a reduced ejection fraction and intermediate heart failure drug treatment prognosis risk PRS score based on multi-gene single nucleotide polymorphism sites, and the reduced ejection fraction and intermediate heart failure population sensitive to the beta-receptor blocker can be well identified.

The invention discloses an application of UFC1 as a biomarker in preparation of a reagent for diagnosing and / or treating benign prostatic hyperplasia. In the technical scheme provided by the invention, a cell experiment result shows that the multiplication capacity of WPMY-1 and BPH-1 cells can be remarkably inhibited by knocking down UFC1, and meanwhile, the apoptosis of the WPMY-1 and BPH-1 cells is powerfully promoted. The discovery reveals the core driving effect of UFC1 in BPH development, namely promoting tissue hyperplasia by maintaining unbalance of prostate cell proliferation and apoptosis. The mechanism indicates a precise intervention direction for targeted therapy: if the activity or expression of UFC1 can be specifically inhibited, abnormal proliferation of prostate cells can be blocked from the source, and meanwhile, a normal apoptosis procedure of the cells is recovered, so that bidirectional regulation is realized to reverse the proliferation process. Compared with an existing alpha receptor blocker only capable of relieving obstruction symptoms and a 5alpha-reductase inhibitor which needs to be used for a long time and possibly causes sexual dysfunction, a treatment strategy of targeting UFC1 directly strikes the cytobiology nature of hyperplasia, and the disease progress is expected to be more effectively controlled.

The invention discloses a preparation method of a beta receptor blocker crude product, which comprises the following steps: (1) adding [(S)-2, 2-dimethyl-1, 3-dioxolane-4-yl] methyl-3-[4-[(S)-2-hydroxy-3-(2-morpholine formylamino) ethylamino] propoxy] phenylpropionate into a solvent, and reacting with oxalic acid to generate [(S)-2, 2-dimethyl-1, 3-dioxolane-4-yl] methyl-3-[4-[(S)-2-hydroxy-3-(2-morpholine formylamino) ethylamino] propoxy] phenylpropionate; the preparation method comprises the following steps: preparing 1, 3-dioxolane-4-yl] methyl-3-[4-[(S)-2-hydroxy-3-(2-morpholine formylamino) ethylamino] propoxy] phenylpropionate oxalate; (2) dissolving the [(S)-2, 2-dimethyl-1, 3-dioxolane-4-yl] methyl-3-[4-[(S)-2-hydroxy-3-(2-morpholine formylamino) ethylamino] propoxy] phenylpropionate oxalate obtained in the step (1), and then forming a beta receptor blocker with a hydrogen chloride and ethyl acetate solution by using the dissolved [(S)-2, 2-dimethyl-1, 3-dioxolane-4-yl] methyl-3-[4-[(S)-2-hydroxy-3-(2-morpholine formylamino) ethylamino] propoxy] phenylpropionate oxalate and the hydrogen chloride and ethyl acetate solution; wherein the oxalic acid is oxalic acid dihydrate. The beta receptor blocker crude product obtained in the invention has relatively high purity and yield.

Compositions and methods for treating or preventing a condition related to myocardial infarction and infarct expansion, extension, and / or dilation following a cardiovascular disorder incident (e.g., post-myocardial infarction) using an effective amount of RRx-001, or a pharmaceutically acceptable salt thereof, are described. In some embodiments, an agent (such as a statin, an angiotension-converting-enzyme (ACE) inhibitor, aspirin, oxygen, a nitric oxide donor, a drug-eluting stent, an anticoagulant or antiplatelet therapy, a phosphodiesterase-5 inhibitor, a calcium channel blocker, an angiotensin II receptor blocker (ARB), a beta blocker, an aldosterone antagonist, a loop diuretic, an epigenetic inhibitor, and / or a nitrite) is administered prior to, concurrently with, or subsequent administering the effective amount of RRx-001, or a pharmaceutically acceptable salt thereof. In some embodiments, the effective amount of RRx-001, or a pharmaceutically acceptable salt thereof, is administered as a composition comprising a blood product and / or the agent.

The application discloses application of UFC1 as a biomarker in preparation of reagents for diagnosing and / or treating prostatic hyperplasia. In the technical scheme, the cell experiment result shows that UFC1 can significantly inhibit the proliferation ability of WPMY-1 and BPH-1 cells, and can effectively promote the apoptosis of the cells. The finding reveals the core driving role of UFC1 in BPH progress, that is, maintaining the imbalance between the proliferation and apoptosis of prostate cells, and promoting the tissue hyperplasia. The mechanism indicates the precise intervention direction of the targeted treatment: if the activity or expression of UFC1 can be specifically inhibited, the abnormal proliferation of prostate cells can be blocked from the source, the normal apoptosis program of the cells can be restored, and the proliferation progress can be reversed by realizing the "two-way regulation". Compared with the existing alpha receptor blockers which can only relieve the obstruction symptoms, and the 5 alpha-reductase inhibitors which need long-term medication and can cause sexual dysfunction, the treatment strategy of targeting UFC1 directly attacks the biological nature of the hyperplastic cells, and is expected to more effectively control the disease progress.

The present disclosure provides liposomal formulations comprising a lipid membrane comprising at least one liposome forming phospholipid and a sterol; and an intraliposomal aqueous compartment encapsulating at least one ATI receptor blocker (ARB) and a pH-dependent ionizable anion; with the liposomes having an effect upon administration to a subject in need of said effect, without causing a reduction in mean blood pressure of said subject of more than 50% as compared to the administration of the same amount of ARB in free form. The liposomes can be for systemic administration, e.g. by injection or for pulmonary administration, e.g. by inhalation.

This invention discloses the application of GLPG0187 in combination with propranolol in the preparation of drugs for the treatment or inhibition of hemangiomas. GLPG0187 is an integrin β1 inhibitor, and propranolol is a β-receptor blocker. This invention was validated through CCK8 assays, scratch assays, and tube formation assays. The results showed that, compared with propranolol monotherapy, GLPG0187 (4 nM) combined with propranolol (20-30 μM) could further inhibit the proliferation, migration, and tube formation ability of human hemangioma endothelial cells, demonstrating superior efficacy compared to propranolol monotherapy. This invention addresses the issue that approximately 2.1% of patients treated with propranolol monotherapy for infantile hemangiomas experience side effects such as sleep disturbances, bronchospasm, and hypoglycemia, providing a new combination therapy regimen and offering a new drug option for reducing the clinical dosage of propranolol and minimizing the risk of side effects. This invention identifies a new target for the treatment of hemangiomas, providing new possibilities for hemangioma treatment.