149 results about "Drug compound" patented technology

The present invention relates to antibodies or antibody fragments that bind to human and non-human primate transferrin receptors. The antibodies described herein can be used as agents to deliver pharmaceutical compounds into or through cells during receptor-mediated endocytosis and / or transendocytosis processes. As transferrin receptors are also present in the blood brain barrier endothelial cells, one aspect of the invention provides means and methods to increase delivery of pharmaceutical compounds to the central nervous system.

An implantable device for delivery of a macromolecular drug compound is provided. The device comprises a core having an outer surface and a membrane layer positioned adjacent to the outer surface of the core. The core comprises a core polymer matrix within which is dispersed a drug compound having a molecular weight of about 5 kDa or more, the polymer matrix containing a hydrophobic polymer. The membrane polymer matrix includes from about 70 wt. % to about 99 wt. % of an ethylene vinyl acetate copolymer.

The invention belongs to the technical field of computer biology, and relates to a lightweight drug-target interaction prediction method based on double pre-training language models. Downloading a protein information data set of required drug compounds and drug action targets from a public database; sending the protein sequence into an encoder to obtain a generated vector; the method comprises the following steps: labeling a compound sequence of a drug by using a tokenizer, pre-defining a corresponding relation between a compound sequence label and an integer, then converting into an integer value, and inputting the integer value into an encoder to generate a vector; splicing the class tokens to obtain a drug target pair, and feeding the drug target pair into an interaction head; and calculating an interaction probability between the two. According to the method, the drug pre-training language model and the protein pre-training language model are introduced at the same time, deep semantic coding is performed on the SMILES sequence and the amino acid sequence, molecular structure characteristics and protein sequence characteristics can be comprehensively captured, and the expression ability is remarkably enhanced.

The invention relates to the technical field of biological medicines, and discloses hyaluronic acid modified metal coordination albumin nanoparticles as well as a preparation method and application thereof. The hyaluronic acid modified metal coordination albumin nanoparticle comprises a core and a hyaluronic acid shell layer, wherein the core is formed by self-assembly of an albumin-drug compound, poly-L-aspartic acid and ferric ions through coordination, and the hyaluronic acid shell layer is connected to the surface of the core through coordination or adsorption. According to the hyaluronic acid modified metal coordination albumin nanoparticles as well as the preparation method and the application thereof, the preparation method is simple, convenient and rapid, does not need complex covalent modification, is mild in condition and is easy for large-scale production, and the prepared nanoparticles are uniform in particle size, good in stability and high in stability. In addition, due to the fact that the hyaluronic acid is modified on the surface, the active targeting capacity on CD44 receptor high-expression tumor cells is achieved, the enrichment and treatment effects of the medicine on the tumor site are remarkably improved, and the application prospect in preparation of the anti-tumor medicine is wide.

The present invention relates to pharmaceutical compounds of Formula (I):as further described herein, and pharmaceutical compositions containing such compounds, as well as methods of using these compounds to modulate the activity of aryl hydrocarbon receptor (AhR) and to treat conditions comprising inflammation inside the intestinal tract and certain disorders of the central nervous system affected by the gut-brain axis, including IBD, ulcerative colitis, Crohn's disease, Huntington's disease, and multiple sclerosis.

The present invention relates to pharmaceutical compounds, compositions, and methods, particularly as they relate to compositions and methods for treating and / or preventing proliferative disorders associated with TGFβR1 activity, such as cancer or fibrosis. The present invention provides compounds of Formula (I) and Formula (II) as further described herein, which have an acidic moiety that enhances tissue specificity to target tissues and organs. The present invention includes pharmaceutical compositions, pharmaceutical combinations, and methods of using these compounds to treat disorders including cancer or fibrosis.

The invention discloses a benzofuran glycoside compound as well as a separation and extraction method, a pharmaceutical composition and application thereof. The compound 1 is separated from an eupatorium chinense extract. And separating and purifying chemical components of the n-butyl alcohol part of the eupatorium chinense root to obtain the benzofuran compound. The inhibition activity of target cyclooxygenase-2 of inflammatory related diseases of all the separated compounds 1 is tested, and the compounds 1 have good inhibition activity on COX-2 enzyme and have good binding energy with target protein. In addition, the compound also has a good NLRP3-related inhibition effect, can be independently used or combined with other medicines to regulate NLRP3-related proteins, and is used for treating NLRP3-related mediated diseases and / or diseases and preparing medicines for preventing or treating the diseases or diseases. The compound 1 also has a good inhibition effect on acetylcholin esterase, and can be used for treating Alzheimer's disease, myasthenia gravis, Parkinson's disease and other diseases.

The present invention relates to pharmaceutical compounds and formulations comprising said compounds, wherein said compounds have the structure according to Formula I or II. The compounds and formulations are suitable for use as medicaments for the prevention or treatment of diseases or conditions characterized by percutaneous cell dysfunction, detachment and / or loss, for medical treatment for vascular stabilization, for treatment for promoting, restoring or maintaining attachment of percutaneous cells to blood vessels, and / or for the treatment of vascular-related diseases in patients. (I) (II)

The present invention relates to pharmaceutical compounds and pharmaceutical compositions comprising said compounds, methods for preparing said compounds and uses of said compounds as SMARCA2 protein inhibitors and their use in the treatment of SMARCA4 deletion cancers, such as SMARCA4 deletion non-small cell lung cancer (NSCLC). (I)

The disclosure describes selective and potent CDK 4 / 6 inhibitors that show advantageous inhibition of cancer growth, even at low concentrations. A class of the CDK 4 / 6 inhibitors relates to substituted pyridopyrimidines compounds having a fatty acid moiety, and are namely derivatives of Palbociclib of general formula [2A], wherein R1 is hydrogen, aryl, alkyl, alkoxy, cycloalkyl, or heterocyclyl; R2 is hydrogen, halogen, alkyl, acyl, cycloalkyl, alkoxy, alkoxy alkyl, haloalkyl, hydroxy alkyl, alkenyl, alkynyl, nitrile, or nitro; R3 is hydrogen, halogen, alkyl, haloalkyl, hydroxy alkyl, or cycloalkyl; and n is an integer from 9 to 20. These compounds may be used as pharmaceutical compounds for anti-cancer therapies, and are useful for the treatment, prevention and / or amelioration of cancer.

The present invention relates to pharmaceutical compounds of Formula (I) and pharmaceutical compositions comprising said compounds, methods for preparing said compounds and the use of said compounds as Cyclin-Dependent Kinase 7 (CDK7) inhibitors and their use in the treatment of diseases, such as cancer.

The invention relates to pharmaceutical compounds and pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds as inhibitors of the SMARCA2 protein and to its use in the treatment of SMARCA4 deficient cancers, e.g., SMARCA4 deficient non-small cell lung cancer (NSCLC).

The invention provides a rehmannia pigment compound as shown in a formula (I), a stereoisomer thereof or pharmaceutically acceptable salt thereof, and particularly relates to the technical field of natural pharmaceutical chemistry and pharmaceutical compounds. The invention aims to solve the problems that the radix rehmanniae pigment is not clear in material basis and lacks a compound with a clear structure and excellent anti-inflammatory activity. The rehmannia pigment compound disclosed by the invention comprises a structure as shown in a formula (I). The invention also discloses a preparation method of the compound and application of the compound in medicines. The compound has a novel chemical structure and remarkable anti-inflammatory activity, release of nitric oxide can be effectively inhibited in a lipopolysaccharide induced macrophage model, the cytotoxicity is far lower than that of a positive control drug quercetin, and the compound shows huge potential as an anti-inflammatory drug lead compound.

The invention relates to the technical field of biological medicines, in particular to a bupivacaine sustained-release injection as well as a preparation method and application thereof. The invention provides a bupivacaine drug compound. The bupivacaine drug compound contains an amide local anesthetic bupivacaine as an active component and a plurality of pharmaceutically acceptable slow-release carrier materials. The drug compound disclosed by the invention adopts a supramolecular synthesis strategy and is prepared into nano-particles through a self-assembly method of a molecular recognition mechanism between Ad and Cd. The novel bupivacaine nano-particles provided by the invention solve the problem of too fast release of the bupivacaine hydrochloride, the preparation method is simple, flexible and modularized, the nano-preparation with controllable carrier size, stable surface chemical property and high drug loading capacity is prepared, the slow release time in vivo can be prolonged, and the analgesic effect can be continuously exerted.

The present invention relates to a compound of formula (I) [Formula 1] JPEG2026502845000045.jpg42170 (wherein L represents a linker, W 1 , W 2 , X 1-5 , x, m, n and R 1-4 The present invention relates to novel linker-drug compounds based on specific phosphoantigens (pAgs) having the general structure reflected in (wherein R is as defined herein). Also provided are conjugates comprising a targeting moiety, preferably a tumor-targeting antibody or antigen-binding fragment thereof, covalently attached to the linker-drug compounds of the invention. The conjugates can be used, for example, to treat diseases such as cancer, infectious diseases, and autoimmune diseases.

The application discloses a FAPI derivative containing 4-cyano thiazolidine modification and application thereof, relates to the field of drug compounds for diagnosing tumors, and provides a FAPI derivative containing 4-cyano thiazolidine modification, a chemical structural formula of which is shown as formula I. The FAPI derivative has good stability, is simple to prepare, has high radiochemical purity and good biological performance, and can be further used for clinical PET / CT tumor imaging, effectively solving the problems of low tumor uptake rate, short retention time and inability to further delay imaging of F-labeled FAPI probes. 18 The FAPI derivative containing 4-cyano thiazolidine modification can solve the problems of low tumor uptake rate, short retention time and inability to further delay imaging of F-labeled FAPI probes, and make up for the defects of the prior art.

The Cardio-Tox Tissue Engineered Model (TEEM) invention provides a robust in vitro model for cardiotoxicity evaluation using three-dimensional (3D) human heart microtissues to quantify dose-dependent changes in electromechanical activity, resulting in a comprehensive cardiotoxicity and arrhythmia risk assessment of test compounds. The invention also provides a predictive in vitro screening platform for pro-arrhythmic toxicity testing using human three-dimensional cardiac microtissues. The invention enables the screening of environmental and pharmaceutical compounds, chemicals, and toxicants to establish safe human exposure levels.

In one embodiment, a method includes receiving a querying image associated with a tissue sample after a treatment by a drug compound, identifying a target layer of the tissue sample based on a machine-learning model trained to identify layers of tissue samples, calculating a normalized thickness of the identified target layer, and determining a toxicity indication of the treatment by the drug compound based on the normalized thickness of the identified target layer.

The invention discloses a phototherapy nano-drug with mitochondrial / STAT3 protein double-site targeting. The phototherapy nano-drug is ATO / CR nano-particles formed by self-assembling a compound CR and atorvaquone under the action of distearoyl phosphatidyl ethanolamine-polyethylene glycol; the structure of the compound CR is shown as a formula I in the specification. The invention discloses an application of the phototherapy nano-drug with mitochondrial / STAT3 protein double-site targeting in preparation of drugs for treating tumors. The phototherapy nano-drug can target mitochondria and STAT3 protein in tumor cells through ATO, and can also passively target tumor sites through the high-permeability long-retention effect of nano-particles, so that more nano-therapeutic agents are enriched around tumors, and the curative effect is improved. The phototherapy nano-drug provided by the invention has good photothermal performance, can effectively enhance the PTT effect of gastric cancer, and exerts the tumor synergistic treatment ability by promoting cell apoptosis, inhibiting angiogenesis and hindering the cell cycle.

The present invention relates to pharmaceutical compounds and pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds, and the use of said compounds as SMARCA2 protein inhibitors, and their use in the treatment of SMARCA4 deficient cancers, such as SMARCA4 deficient non-small cell lung cancer (NSCLC).

The present invention relates to pharmaceutical compounds and pharmaceutical compositions comprising said compounds, methods for preparing said compounds and uses of said compounds as SMARCA2 protein inhibitors and their use in the treatment of SMARCA4 deletion cancers, such as SMARCA4 deletion non-small cell lung cancer (NSCLC).

The invention belongs to the field of pharmaceutical compounds, and discloses a 3-(2-thiazole-5-yl methyl) benzoxazolone derivative and application thereof, and the 3-(2-thiazole-5-yl methyl) benzoxazolone derivative has a chemical structure as shown in a general formula A; ; wherein R1 is selected from alkyl with the C atom number of 1-10, naphthenic base with the C atom number of 3-8, substituted or unsubstituted aryl containing 5-10 main chain atoms, aryl heterobase or alkyl with the C atom number of 1-10, cycloalkyl with the C atom number of 3-8, substituted or unsubstituted aryl containing 5-10 main chain atoms and aryl heterobase; in the formula, n is 0-4, and Z is selected from three-to-eight-membered cycloalkyl, three-to-eight-membered heteroalkyl or substituted or unsubstituted aryl and heteroaryl containing 5-10 main chain atoms. The derivative has the effect of inhibiting quorum sensing of pseudomonas aeruginosa, can be used as a novel biological membrane inhibitor, and can also be used as an antibacterial sensitizer.

The present application relates to a preparation method for a linker-drug compound. In particular, a preparation method for a target compound is provided. The method comprises reacting a compound represented by Formula a with a Lewis acid to obtain a crude product, and purifying the crude product to obtain a compound represented by Formula A.

JPEG2026525352000192.jpg3981 The present invention relates to compounds of formula (I) that are useful as inhibitors of ubiquitin-specific protease USP19 activity. The present invention also relates to pharmaceutical compositions comprising these compounds and methods of using these compounds in therapeutics.

The present invention relates to pharmaceutical compounds of Formula (I) and pharmaceutical compositions comprising said compounds, to methods for preparing said compounds and to the use of said compounds as inhibitors of cyclin-dependent kinase 7 (CDK7) and their use in the treatment of diseases, such as cancer.

The present invention relates to compounds or a pharmaceutically acceptable salt thereof of formula (Ia) or (Ib), wherein each -D- is independently a drug moiety; each -AB1 and -AB2 is independently an albumin-binding moiety; each -L1- is independently a linker moiety covalently and reversibly connected to -D-; each -L2- is independently a single chemical bond or is absent; and x and y are an integer; to pharmaceutical compositions comprising at least one such compound and to their uses.

Hemicyanine-based compounds having optoacoustic properties and methods of their use as imaging and diagnostic agents and as conjugates with targeting and / or drug compounds.

The present invention relates to pharmaceutical compounds and pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds as SMARCA2 protein inhibitors and their use in the treatment of SMARCA4 deletion cancers, such as SMARCA4 deletion non-small cell lung cancer (NSCLC). (I)