1602 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 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 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.

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.

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.

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).

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.

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 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 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 is a method of treating a disease or condition, for example, obesity, weight gain, or diabetes, comprising administering to a subject in need thereof a glucose-dependent insulinotropic polypeptide receptor (GIPR) antagonist and a glucagon-like peptide 1 receptor (GLP-1R) agonist. Further described herein are pharmaceutical compositions comprising a GIPR antagonist and a GLP-1R agonist, which may be useful in the treatment of a disease or condition, for example, obesity, weight gain, or diabetes.

Methods for treating or preventing chronic rhinosinusitis without nasal polyps (CRSsNP) 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.

To provide a pharmaceutical composition comprising a novel compound which has a thyroid-stimulating hormone receptor antagonist activity and is useful for the treatment of thyroid-related diseases.SOLUTION: There is provided a pharmaceutical composition comprising a 3,4-dihydroquinolin-2(1H)-one compound represented by a formula (I) or a pharmacologically acceptable salt thereof. A pharmaceutical composition comprising the compound or the pharmacologically acceptable salt thereof has an antagonist activity against thyroid-stimulating hormone receptors and is useful as a therapeutic agent or the like for thyroid-related diseases (for example, hyperthyroidism, Graves' disease, thyroid eye disease and thyroid cancer).SELECTED DRAWING: None

The invention relates to an application of a CTHRC1 inhibitor in preparation of a medicine for preventing and / or treating arthritis. Specifically, the invention provides application of an inhibitor or an antagonist of a CTHRC1 gene or a protein thereof, the inhibitor or the antagonist is used for preparing a composition or a preparation, and the composition or the preparation is used for (a) preventing and / or treating arthritis-related diseases; and / or (b) inhibiting cartilage cell senescence.

The invention relates to the technical field of biological medicine, in particular to a nano-vesicle for targeted brain glioma metabolic immune remodeling and a preparation method and application thereof. According to the nano-vesicle for targeted brain glioma metabolism immune remodeling, double-target metabolism and cascade responsive cleavage site modified biological vesicles are integrated, and effective penetration of a drug blood brain barrier and precise targeting of brain glioma can be achieved. The ROS responsive nanoparticles II are prepared by selecting BSA as a drug carrier, applying a nanoprecipitation method and utilizing SLC1A5, LDHA antagonists and responsive linkers, so that the metabolic double-target inhibitor only responds to specific ROS of tumor cells, and specific release in the tumor cells is realized. The cascade response polypeptide provides a simple and convenient delivery scheme with low invasiveness and application prospects for treatment of brain glioma, and is expected to realize precise and individualized treatment in the field of treatment of malignant glioma.

Described herein, in part, are methods useful for preventing and / or treating a disease or condition relating to aberrant function or activity of a T-type calcium channel, such as psychiatric disorders (e.g., mood disorder (e.g., major depressive disorder)), pain, tremor (e.g., essential tremor), seizures (e.g., absence seizures), epilepsy, or an epilepsy syndrome (e.g., juvenile myoclonic epilepsy). The present invention further comprises methods for modulating the function of a T-type calcium channel and methods of administering a titrated dosage of a T-type calcium channel antagonist.

Described herein is a method of treating a disease or condition, for example, obesity, weight gain, or diabetes, comprising administering to a subject in need thereof a glucose-dependent insulinotropic polypeptide receptor (GIPR) antagonist and a glucagon-like peptide 1 receptor (GLP-1R) agonist. Further described herein are pharmaceutical compositions comprising a GIPR antagonist and a GLP-1R agonist, which may be useful in the treatment of a disease or condition, for example, obesity, weight gain, or diabetes.

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 an N-substituted cyclic amide compound represented by the formula or a pharmacologically acceptable salt thereof. The compound or the pharmacologically acceptable salt thereof according to the present invention has a thyroid-stimulating hormone receptor antagonistic activity and is useful as a therapeutic agent for thyroid-related diseases (e.g., hyperthyroidism, Graves' disease, thyroid eye disease, and thyroid cancer) and others.

Novel compounds that act as antagonists to human GPR39 protein are disclosed. Pharmaceutical compositions and methods of use for antagonists to human GPR39 protein are disclosed. In particular, methods of using the antagonists in the treatment of diseases or conditions including cardiovascular conditions, endocrine system and hormone disorders, cancer disorders, metabolic diseases, gastrointestinal and liver diseases, hematological disorders, neurological disorders and respiratory diseases are disclosed herein.

A topical ophthalmological composition includes a muscarinic receptor antagonist as an active pharmaceutical ingredient; and medium chain triglycerides (MCTs) or light liquid paraffin oil as liquid vehicle. The topical ophthalmological composition treats an ocular disease.

Described herein is a method of treating a disease or condition, for example, obesity, weight gain, or diabetes, comprising administering to a subject in need thereof a glucose-dependent insulinotropic polypeptide receptor (GIPR) antagonist and a glucagon-like peptide 1 receptor (GLP-1R) agonist. Further described herein are pharmaceutical compositions comprising a GIPR antagonist and a GLP-1R agonist, which may be useful in the treatment of a disease or condition, for example, obesity, weight gain, or diabetes.

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.

The invention belongs to the technical field of pharmaceutical composition pellet preparations, and particularly relates to a double-drug co-loaded oral pellet preparation with a multilayer core-shell structure as well as a preparation method and application of the double-drug co-loaded oral pellet preparation. According to the double-drug co-loaded oral pellet preparation provided by the invention, through the design of a multi-layer core-shell structure, the oral pellet preparation has microenvironment regulation and time difference release synergy, namely the peripheral antagonist trospium chloride on the outermost layer is preferentially released and acts on a peripheral muscarinic receptor (M1 / M4); the xanomeline of the pellet core is subjected to post-release or pulse release and acts on a peripheral receptor (M2 / M3), so that the curative effect and side effect inhibition of the two drugs form time difference synergy, peripheral adverse reactions caused by xanomeline can be reduced, and the problem of synergy in combined administration of xanomeline and an antagonist trospium chloride is solved.

The invention discloses application of a growth hormone receptor antagonist and a nucleic acid molecule in preparation of a medicine for preventing or treating retinal neovascularization diseases, and relates to the technical field of retinal neovascularization. The invention finds that the growth hormone receptor antagonist or the blocking reagent can effectively intervene the occurrence and development of the neovascular retina disease and improve the symptom of the disease. In addition, the transcription level of the encoding gene of the growth hormone receptor is reduced in a gene editing mode, and the pathological vascular change of the retinal neovascular disease can be effectively improved by knocking out the retina GHR, so that the pathological neovascular growth of the retina is reduced, and vascular exudation and inflammatory response are reduced. The invention provides a new direction for the treatment of retinal neovascular diseases, and provides a new choice for patients intolerant or unresponsive to anti-VEGF (Vascular Endothelial Growth Factor) treatment.

The present disclosure is directed to the combination of a Fas axis antagonist, such as an anti-FasL antibody, and a Treg cell depletion therapy, for example an anti-CD25 antibody, optionally with a cancer vaccine, for use in the treatment of cancer.

A method is described for the prophylaxis of hypertension in a cat in need thereof. The method includes administration of an effective amount of angiotensin II receptor 1 (AT-1) antagonist (sartan) to the cat, wherein the prophylaxis of hypertension is a delay of onset of hypertension.

The present disclosure relates to fusion molecules and chimeric molecules which comprise two components: an Ang-2 antagonist peptide linked to a VEGF-binding moiety. Further disclosed are methods of using said chimeric molecules to treat a patient cancer, proliferative retinopathy, neovascular glaucoma, macular edema, wet age-related macular degeneration (wAMD), macular edema following retinal vein occlusion (RVO), diabetic macular edema (DME), or diabetic retinopathy (DR).

The present invention relates to methods for treating or reducing the severity of thyroid eye disease. In particular, the present invention provides methods for treating or reducing the severity of thyroid eye disease in patients in need thereof comprising administering an IGF-1R antagonist antibody according to specific dosage regimens. Pharmaceutical compositions comprising the IGF-1R antagonist antibody for use in the methods are also described.

The invention belongs to the technical field of chemical drugs, and relates to a compound as shown in a general formula (I), or a racemate thereof, or an isomer thereof, or a pharmaceutically acceptable salt thereof, as a small molecule antagonist of alpha4beta7 integrin, and a method for treating various specific diseases or symptoms by using the compound. # imgabs0 #