1003 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 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.

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.

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.

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.

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.

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.

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.

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 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.

Disclosed are methods of treating cancer comprising administering to a subject a treatment regimen comprising a compound of Formula (I): Formula (I), or a pharmaceutically acceptable salt thereof, and a PD-1 or PD-L1 antagonist.

The present invention provides methods for treating atopic dermatitis (AD). Also provided are methods for improving one or more AD-associated parameter(s), and methods for decreasing the level of at least one AD-associated biomarker in a subject in need thereof. The methods of the present invention comprise administering to a subject in need thereof a pharmaceutical composition comprising an interleukin-4 receptor (IL-4R) antagonist such as an anti-IL-4R antibody.

The subject invention provides a method for treating a non-alcoholic fatty liver disease (NAFLD) disease in a subject afflicted therewith comprising administering to the subject a pharmaceutical composition comprising an amount of a compound which is a non-retinoid retinol-binding protein 4 (RBP4) antagonist effective to treat the subject, thereby treating the subject.The subject invention provides a method for treating gout in a subject afflicted therewith comprising administering to the subject a pharmaceutical composition comprising an amount of a compound which is a retinol-binding protein 4 (RBP4) antagonist effective to treat the subject, thereby treating the subject.

The invention belongs to the technical field of biological medicines, and particularly relates to application of an adenosine A2a / A2b receptor dual antagonist in preparation of an anti-depression medicine and a medicine for preventing or treating depression. The invention provides a new application of the adenosine A2aR / A2bR double antagonist, animal experiments prove that the adenosine A2aR / A2bR double antagonist AB928 can effectively treat depression of mice, does not have obvious toxic or side effects, increases indications of the AB928, and has a prospect of being applied as an anti-depression drug in practice, so that the medical application of the adenosine A2aR / A2bR double antagonist AB928 is further expanded.

Disclosed are compounds that are thyroid stimulating hormone receptor antagonists, and methods useful for preventing or treating a thyroid disease.

The present invention provides antagonizing antibodies that bind to complement factor D (CFD), conjugates thereof, and methods of using same. The anti-CFD antibodies can be used therapeutically alone or in combination with other therapeutics to treat age related macular degeneration and other diseases.

The invention relates to a method for semi-solid-phase synthesis of a polycyclic compound and an intermediate, a long chain is synthesized through solid phase, then two-step ring closing is performed to form a key intermediate, and simple derivation is performed on the basis of the key intermediate to obtain a PCSK9 antagonist compound. According to the invention, starting materials for solid-phase synthesis are selected, steric hindrance is effectively avoided, and solid-phase reaction and subsequent liquid-phase correlation cyclization can be smoothly carried out, so that the yield is improved, and the cost is reduced.

The invention relates to a synthesis method of a polycyclic compound and an intermediate, a long chain is synthesized firstly, then two-step ring closing is performed to form a key intermediate, and simple derivation is performed on the basis of the key intermediate to obtain a PCSK9 antagonist compound. According to the invention, a ring closing route and an intermediate are optimized, and the ring closing yield is improved.

The invention provides a compound as shown in a formula I, and a tautomer, a stereoisomer, a solvate, a pharmaceutically acceptable salt or a prodrug thereof. The compound can be used as an antagonist of TRPM3.

The present application relates to a substituted heterocyclic derivative, a preparation method therefor, and medicinal use of a pharmaceutical composition comprising the derivative or a deuterated derivative. Specifically, the present application relates to a substituted heterocyclic derivative represented by general formula (I), (I-A), or (I-B), a preparation method therefor, a pharmaceutically acceptable salt thereof, and use thereof as a voltage-gated channel Nav 1.8 antagonist in the prevention and / or treatment of a Nav 1.8-related disease, particularly in the field of pain. The definition of each substituent in general formula (I), (I-A), or (I-B) is the same as that in the specification.

The present disclosure relates to methods of treating breast cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a radiopharmaceutical compound having a GRPR antagonist moiety, such as [177Lu] Lu-NeoB, in combination with a CDK4 / 6 inhibitor, such as ribociclib, and a therapeutically effective amount of an endocrine therapy, such as fulvestrant.

The invention provides methods for classifying lung cancer (e.g., small cell lung cancer (SCLC), e.g., extensive stage SCLC (ES-SCLC)); methods for treating lung cancer in a patient, for example, by administering a treatment regimen that comprises a PD-1 axis binding antagonist (e.g., atezolizumab) to the patient. Also provided are compositions for use, kits, and articles of manufacture for use in classifying and treating lung cancer in a patient.

The invention pertains to an inhalable dry powder formulation comprising a therapeutically effective amount of Glucagon-like peptide-1 (GLP-1) receptor agonist. Further, use of the inhalable dry powder formulation treatment of chronic weight management for people who are overweight or obese, with or without a weight-related comorbid condition. Further, a process for forming particles comprising a Glucagon- like peptide-1 (GLP-1) receptor agonist suitable for airborne inhalation.

Methods are provided for treating moderate to severe atopic dermatitis of the hands and / or feet in a subject. In one aspect, the methods include administering to the subject one or more doses of an interleukin-4 receptor (anti-IL-4R) antagonist, such as an anti-IL-4R antibody or antigen-binding fragment thereof.

Novel and known substituted purine compounds and salts thereof act as adenosine A2a receptor (A2aR) antagonists for cancer immunotherapy, depression, anxiety, multiple sclerosis, NASH, scleroderma, ADHD, Alzheimer's and Parkinsons. Pharmaceutical compositions comprising such compounds, and methods of their use in treating depression are also taught.

The invention relates to a substituted heterocyclic derivative, a preparation method thereof and application of a pharmaceutical composition containing the derivative or a deuterated derivative in medicine. Specifically, the invention relates to substituted heterocyclic derivatives as shown in general formulas (I), (I-A) and (I-B), a preparation method and medicinal salts thereof, and application of the substituted heterocyclic derivatives as voltage-gated channel Nav 1.8 antagonists in prevention and / or treatment of Nav 1.8 related diseases, especially in the field of pain. Wherein the definitions of substituent groups in the general formulas (I), (I-A) and (I-B) are the same as the definitions in the specification.

Provided herein are biomarkers for the treatment of pathological conditions, such as cancer, and method of using PD-1 / PD-L1 pathway antagonists. In particular, provided are biomarkers for patient selection and prognosis in cancer, as well as methods of therapeutic treatment, articles of manufacture and methods for making them, diagnostic kits, methods of detection and methods of advertising related thereto.

The present invention provides a solid dispersion of compound 1 or a pharmaceutical salt thereof, comprising the compound 1 or the pharmaceutical salt thereof as an active ingredient and a carrier material, wherein the carrier material is selected from one, two, or more of polyvinylpyrrolidone (PVP), copovidone, polyvinylpyrrolidone-vinyl acetate copolymer, hydroxypropyl methylcellulose acetate succinate, polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, hydroxypropyl methylcellulose, polyethylene glycol, and ethyl cellulose, enabling the drug to have good stability, dissolution, and therapeutic effects. The formulation of the present invention provides rapid drug release and can reduce the oral burden of large-dose tablets on menopausal patients, thereby improving treatment compliance and treatment efficiency.

The present invention is related to a C—X—C motif chemokine 12 (CXCL12) antagonist for use in a method for treating a tumor in a subject, wherein the method comprises administering to the subject—the C—X—C motif chemokine 12 (CXCL12) antagonist, —a radiotherapy, and—an anti-angiogenic compound, wherein the tumor is a brain tumor.

Provided are methods and compositions for enhancing radiotherapy in various cancers by administering dopamine receptor (DRD2)‐binding phenylpiperazine derivatives such as brexpiprazole, cariprazine, pipamperone, and perospirone. In vitro studies show that combining these agents with ionizing radiation (e.g., 5 Gy) significantly reduces cancer cell survival, suppresses metastatic and stemness markers (e.g., CD44, MMP‑2, Snail, Nanog), and promotes apoptosis. Fractionated or single‐fraction radiation regimens can be paired with DRD2 antagonists to lower treatment‐resistant phenotypes, decrease the likelihood of recurrence, and potentially reduce necessary radiation dosages. The approach applies to breast, prostate, lung, pancreatic, and brain cancers, among others. Depending on tumor characteristics, additional chemotherapeutic or immunotherapeutic agents may further improve outcomes.