2882 results about "Antagonist" patented technology

This disclosure relates to administration of a combination of: 1) about 100-110 mg, about 104-106 mg, or about 105 mg of bupropion hydrochloride, or a molar equivalent amount of a free base form or another salt form of bupropion; and 2) about 40-50 mg, about 44-46 mg, or about 45 mg of dextromethorphan hydrobromide, or a molar equivalent amount of a free base form or another salt form of dextromethorphan in certain patient populations, such as patients having moderate renal impairment, patients having mild or moderate hepatic impairment, patients receiving a concomitant strong CYP2D6 inhibitor, patients who are known CYP2D6 poor metabolizers, those in need of an NMDA antagonist that does not cause dissociation, and those at risk of QT prolongation.

This disclosure relates to administration of a combination of: 1) about 100-110 mg, about 104-106 mg, or about 105 mg of bupropion hydrochloride, or a molar equivalent amount of a free base form or another salt form of bupropion; and 2) about 40-50 mg, about 44-46 mg, or about 45 mg of dextromethorphan hydrobromide, or a molar equivalent amount of a free base form or another salt form of dextromethorphan in certain patient populations, such as patients having moderate renal impairment, patients receiving a concomitant strong CYP2D6 inhibitor, patients who are known CYP2D6 poor metabolizers, those in need of an NMDA antagonist that does not cause dissociation, and those at risk of QT prolongation.

This disclosure relates to administration of a combination of: 1) about 100-110 mg, about 104-106 mg, or about 105 mg or less of bupropion hydrochloride, or a molar equivalent amount of the free base form or another salt form of bupropion; and 2) about 40-50 mg, about 44-46 mg, or about 45 mg or less of dextromethorphan hydrobromide, or a molar equivalent amount of the free base form or another salt form of dextromethorphan in certain patient populations, such as patients having moderate renal impairment, patients receiving a concomitant strong CYP2D6 inhibitor, patients who are known CYP2D6 poor metabolizers, those in need of an NMDA antagonist that does not cause dissociation, and those at risk of QT prolongation.

This disclosure relates to administration of a combination of: 1) about 100-110 mg, about 104-106 mg, or about 105 mg of bupropion hydrochloride, or a molar equivalent amount of a free base form or another salt form of bupropion; and 2) about 40-50 mg, about 44-46 mg, or about 45 mg of dextromethorphan hydrobromide, or a molar equivalent amount of a free base form or another salt form of dextromethorphan in certain patient populations, such as patients having moderate renal impairment, patients receiving a concomitant strong CYP2D6 inhibitor, patients who are known CYP2D6 poor metabolizers, those in need of an NMDA antagonist that does not cause dissociation, and those at risk of QT prolongation.

This disclosure relates to administration of a combination of: 1) about 100-110 mg, about 104-106 mg, or about 105 mg of bupropion hydrochloride, or a molar equivalent amount of the free base form or another salt form of bupropion; and 2) about 40-50 mg, about 44-46 mg, or about 45 mg of dextromethorphan hydrobromide, or a molar equivalent amount of the free base form or another salt form of dextromethorphan in certain patient populations, such as patients having moderate renal impairment, patients receiving a concomitant strong CYP2D6 inhibitor, patients who are known CYP2D6 poor metabolizers, those in need of an NMDA antagonist that does not cause dissociation, and those at risk of QT prolongation.

A surgical system includes a steerable instrument. The steerable instrument includes a first tube including a first serpentine beam formed in a tubular sidewall thereof, and a second tube including a second serpentine beam formed in a tubular sidewall thereof. The first and second tubes are concentrically nested and positioned so that the first and second serpentine beams are at least partially aligned with each other axially and face in radial directions that differ angularly from one another. The first and second tubes are connected to each other distally of the first and second serpentine beams. The first and second serpentine beams define a bending segment that is actuatable to form a bend in the nested tube structure in response to differential axial forces applied to the first and second tubes.

This disclosure relates to administration of a combination of: 1) about 100-110 mg, about 104-106 mg, or about 105 mg of bupropion hydrochloride, or a molar equivalent amount of a free base form or another salt form of bupropion; and 2) about 40-50 mg, about 44-46 mg, or about 45 mg of dextromethorphan hydrobromide, or a molar equivalent amount of a free base form or another salt form of dextromethorphan in certain patient populations, such as patients having moderate renal impairment, patients receiving a concomitant strong CYP2D6 inhibitor, patients who are known CYP2D6 poor metabolizers, those in need of an NMDA antagonist that does not cause dissociation, and those at risk of QT prolongation.

Aspects of the application provide hemojuvelin antagonists and methods of using the same in treating anemias of kidney disease and conditions associated with these anemias. Methods provided in the application relate to treatment of a subject having an anemia associated with chronic kidney disease and / or kidney disease in a subject that has a level of glomerular filtration rate lower than one or more thresholds.

The present invention relates to methods of treating Chronic Inflammatory Demyelinating Polyneuropathy (CIDP) using an antagonist of human neonatal Fc receptor (FcRn), which in certain embodiments is efgartigimod.

A compound as an LPAR1 antagonist, a pharmaceutical composition thereof and a use thereof. A compound represented by formula (I), as well as a racemate, stereoisomer, tautomer, nitrogen oxide, or pharmaceutically acceptable salt thereof. The compound of the LPAR1 antagonist has a good inhibitory effect on LPAR1, has excellent pharmacokinetic properties, and has good druggability.

Methods for treating or preventing asthma (e.g., allergic asthma, asthma associated with allergic bronchopulmonary aspergillosis (ABPA), moderate-to-severe asthma, persistent asthma or the like) and associated conditions (e.g., ABPA, ABPA comorbid with asthma, ABPA comorbid with cystic fibrosis (CF), ABPA comorbid with asthma and CF) in a subject are provided. Methods comprising administering to a subject in need thereof a therapeutic composition comprising an interleukin-4 receptor (IL-4R) antagonist, such as an anti-IL-4R antibody or antigen-binding fragment thereof, are provided.

The disclosure provides a method of treating a human subject afflicted with lung cancer (e.g., non-small cell lung cancer (NSCLC)) with a programmed death-1 (PD-1) pathway inhibitor (e.g., an anti-PD-1 antibody) and a concurrent chemoradiotherapy (CCRT, e.g., a platinum doublet chemotherapy (PDCT) and a radiation therapy) followed by a combination of a PD-1 pathway inhibitor (e.g., an anti-PD-1 antibody) and a lymphocyte activation gene-3 (LAG-3) antagonist (e.g., an anti-LAG-3 antibody). In some aspects, the method comprises a recovery period that begins upon completion of the treatment with the PD-1 pathway inhibitor and the CCRT and ends at the start of the treatment with the combination of the PD-1 pathway inhibitor and the LAG-3 antagonist.

Disclosed herein are (6-(4-(trifluoromethyl)pyridin-3-yl)pyridazin-3-yl)octahydrocyclopenta[c]pyrrol-5-amine, (6-(4-(difluoromethyl)pyridin-3-yl)pyridazin-3-yl)octahydrocyclopenta[c]pyrrol-5-amine, and (6-(2-(trifluoromethyl)pyridin-3-yl)pyridazin-3-yl)octahydrocyclopenta[c]pyrrol-5-amine compounds, useful as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.

This disclosure relates to administration of a combination of: 1) about 100-110 mg, about 104-106 mg, or about 105 mg of bupropion hydrochloride, or a molar equivalent amount of the free base form or another salt form of bupropion; and 2) about 40-50 mg, about 44-46 mg, or about 45 mg of dextromethorphan hydrobromide, or a molar equivalent amount of the free base form or another salt form of dextromethorphan in certain patient populations, such as patients having moderate renal impairment, patients receiving a concomitant strong CYP2D6 inhibitor, patients who are known CYP2D6 poor metabolizers, those in need of an NMDA antagonist that does not cause dissociation, and those at risk of QT prolongation.

This disclosure relates to administration of a combination of: 1) about 100-110 mg, about 104-106 mg, or about 105 mg of bupropion hydrochloride, or a molar equivalent amount of the free base form or another salt form of bupropion; and 2) about 40-50 mg, about 44-46 mg, or about 45 mg of dextromethorphan hydrobromide, or a molar equivalent amount of the free base form or another salt form of dextromethorphan in certain patient populations, such as patients having moderate renal impairment, patients receiving a concomitant strong CYP2D6 inhibitor, patients who are known CYP2D6 poor metabolizers, those in need of an NMDA antagonist that does not cause dissociation, and those at risk of QT prolongation.

Provided are novel methods of treating generalized myasthenia gravis in a subject. These methods generally comprise administering to the subject an effective amount of an isolated FcRn antagonist. In certain embodiments the FcRn antagonist binds to FcRn with increased affinity and reduced pH dependence relative to native Fc region.

Aspects of the disclosure provides composition and methods for treating a subject having a blood loss condition, the method comprising administering to the subject a hemojuvelin (HIV) antagonist (e.g., anti-HJV antibody).

Disclosed herein are substituted hexahydro-1H-cyclopenta[c]pyrrole compounds, which may be useful as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.

The present invention addresses the problem of providing a novel compound that has a thyroid-stimulating hormone receptor antagonistic activity and is useful for the treatment of thyroid-related diseases. The present invention relates to a nitrogen-containing condensed ring compound represented by formula (A-I) or a pharmacologically acceptable salt thereof. The present invention relates to a nitrogen-containing condensed ring compound represented by formula (A-I) or a pharmacologically acceptable salt thereof. The compound or the pharmacologically acceptable salt thereof according to the present invention has an antagonistic activity against thyroid-stimulating hormone receptors and is therefore useful as a therapeutic agent for thyroid-related diseases (e.g., hyperthyroidism, Graves' disease, thyroid eye disease, and thyroid cancer) and others.

The invention provides methods and compositions for classifying kidney cancer (e.g., RCC, e.g., an inoperable, locally advanced, or metastatic RCC); methods and compositions for treating kidney cancer in a patient, for example, by administering a treatment regimen that includes a PD-1 axis binding antagonist (e.g., atezolizumab) and a VEGF antagonist (e.g., bevacizumab) to the patient. Also provided are compositions, pharmaceutical compositions, kits, and articles of manufacture for use in classifying and treating kidney cancer in a patient.

Provided in the present invention are a TSHR antagonist compound, a pharmaceutical composition, and a preparation method therefor and the use thereof. The compound has good TSHR antagonism, and is used in the treatment of thyroid-associated conditions and / or diseases, such as hyperthyroidism, Graves' disease, Graves' ophthalmopathy, and thyroid eye disease, and in the preparation of a drug for treating such conditions or diseases.

The present disclosure relates to bicyclic heterocycles of Formula (I), and pharmaceutical compositions of the same, that are modulators, antagonists, or inhibitors of the G protein-coupled receptor MRGPRX2 and are useful in the treatment of MRGPRX2 dependent conditions such as inflammatory diseases.

The invention discloses a drug-combined anticancer composition and application of the composition in preparation of anticancer drugs. According to the present invention, the drug combination composition comprises the PARP inhibitor Olaparib and the calcium ion antagonist amlodipine maleate, the PARP inhibitor Olaparib and the calcium ion antagonist amlodipine maleate provide the synergistic effect, and compared with the single PARP inhibitor, the drug combination composition has characteristics of high stomach cancer sensitivity, significant gastric cancer efficiency improving, and wide application prospect. The Amlodipine in the drug combination composition provided by the invention enhances the curative effect of the PARP inhibitor Olaparib on the gastric cancer.

Provided herein are compounds that modulate the activity of melanoma inhibitor of apoptosis (ML-IAP) protein, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

The invention belongs to the field of medicinal chemistry, and particularly discloses a benzimidazole amine derivative, a preparation method thereof and application of the benzimidazole amine derivative as a beta2-adrenergic receptor allosteric antagonist. According to the benzimidazole amine derivative disclosed by the invention, R1 is a hydrogen atom or a bromine atom; r2 is substituted benzoyl, substituted benzyl and the like. Pharmacological results show that the benzimidazole amine derivative disclosed by the invention has relatively good antagonistic activity on beta2AR, and the functional activity of isoprenaline (ISO) can be subjected to negative allosteric regulation.

The invention discloses 7-aminobenzopyrone or 7-aminoquinolinone compounds and application thereof, the structural general formula of the compounds is as shown in formula (I), and the compounds are compounds with androgen receptor antagonistic activity. The compound provided by the invention has relatively high activity of antagonizing androgen receptor transcription, shows relatively good biological activity at molecular level, cellular level and animal level, and has relatively good safety. Therefore, the compound can be used as an androgen receptor antagonist in preparation of drugs for treating androgen receptor mediated diseases, including but not limited to prostate cancer, metastatic prostate cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer, androgen-derived alopecia and acne. The side effect of systemic androgen antagonism caused by systemic distribution can be avoided, and a safer and more targeted treatment choice is provided for patients.

Provided in the present invention are a TSHR antagonist compound, a pharmaceutical composition, a preparation method therefor and the use thereof. The compound (I) has a good TSHR antagonistic effect, and is used for treating thyroid-associated disorders and / or diseases, such as hyperthyroidism, Graves' disease, Graves' ophthalmopathy, and thyroid eye disease, and for preparing drugs for such disorders or diseases.

Described herein are Fc fusion molecules that bind FcRn (FcRn) with improved half-life and methods of use thereof.