323results about "Silicon compound active ingredients" patented technology

The invention discloses a nitrogen-containing heterocyclic ring compound as well as a preparation method and application thereof, and particularly relates to a nitrogen-containing heterocyclic ring compound as shown in a general formula (I), or pharmaceutically acceptable salts thereof, or enantiomers, diastereoisomers, tautomers, torsion isomers, solvates, polymorphic substances or prodrugs thereof, and a preparation method and pharmaceutical application thereof. Wherein the definition of each group is described in the specification. # imgabs0 #

The invention relates to the technical field of medical chemistry, in particular to a bridge oxygen site regulatively modified rhodamine anti-cancer fluorescent compound as well as a preparation method and application thereof. The invention develops the rhodamine anti-cancer fluorescent compound of which the meso site is functionalized by tetraarylethene and the bridge oxygen site can be regulated and modified, the fluorescent compound has adjustable red light-near infrared fluorescence emission and excellent fluorescence quantum yield, and the quantum yield can be as high as 99%; the fluorescent compound specifically targets mitochondria, and mainly inhibits growth of tumor cells by inducing para-apoptosis; under irradiation of 655 nm near-infrared laser, ferroptosis is further triggered, efficient treatment of tumor cells is achieved through chemical-photodynamic synergistic effect, and a new treatment thought is provided for overcoming tumor drug resistance.

A method of selectively inhibiting pathogenic microbes includes: providing an antimicrobial compound that is functional having a structure of Formula 1, or derivative thereof, salt thereof, or stereoisomer thereof, or having any chirality at any chiral center, or tautomer, polymorph, solvate, or combination thereof; and contacting a microbe with the compound such that the microbe is selectively inhibited;

The invention relates to RIP1 inhibiting compounds and methods of making and using the same. In particular, disclosed herein are kinase inhibitory compounds, such as receptor interacting protein-1 (RIP1) kinase inhibitor compounds, and pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions and / or combinations may be used to treat or prevent kinase-related diseases or disorders, particularly RIP1-related diseases or disorders.

The present invention provides nitrogen-containing heterocyclic protein inhibitor compounds, their stereoisomers, tautomers or pharma- ceutically acceptable salts, and further provides the preparation of nitrogen-containing heterocyclic compounds and their uses, and medicaments prepared using such compounds have a wide range of uses in the treatment of diseases, including multiple types of autoimmune diseases such as multiple sclerosis, rheumatoid arthritis, inflammatory bowel disease, lupus erythematosus, neurodermatitis, dermatitis, psoriasis, psoriatic arthritis, Crohn's disease, sicca syndrome and scleroderma.

Compounds and compositions capable of modulating immune responses in patients, as well as implantable elements containing them, are provided. [Solution] For example, 4-((1-(2-(2-(2-(2-aminoethoxy)ethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)methyl)thiomorpholine 1,1-dioxide, as well as pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives and compositions thereof, and implantable elements (e.g., devices and materials) containing these are provided.

The present disclosure provides compounds, compositions, and methods for treating or preventing neurological disorders in a patient. The disclosed methods include administration to a subject suffering from a neurological disorder of a compound disclosed herein.

To provide a novel organosilicon quaternary ammonium compound that is effective in infectious disease.SOLUTION: A quaternary ammonium compound of the following formula is provided. In the formula, R2,R3, R4, R22, R23, and R24 are individually independent and selected from the group consisting of the following.SELECTED DRAWING: None

The present disclosure provides compounds of Formula I: (I), or an N- oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: A, Y, m, n, p, R1, R2, R3, R3a, R4, R5, R6, R7, and Z are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, Parkinson's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

The present invention relates to a composition comprising:-an organosilicon compound of formula (I) RxSi (OH) 4-x, in which each R is independently a group containing from 1 to 20 carbon atoms, x = 1 to 3, or a salt thereof; and-a cross-linked glycosaminoglycan or a salt thereof.

The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B. The compounds can be used alone or in combination with other drugs. TIFF2023509881001359.tif33128

The monoclonal antibody specifically binds to CD25, and the conjugate of anti-CD25 antibody are described.The CD25-specific monoclonal antibody and its conjugate do not block the binding of IL-2 to CD25, and induce little or no antibody-dependent cell-mediated cytotoxicity (ADCC).The anti-CD25 antibody and conjugate can be used, for example, to target photoimmunotherapy to T regulatory (Treg) cells in tumor beds to enhance local host immune response against tumors.

The present disclosure provides a compound of formula I:(1), or an N-oxide thereof, or a pharmaceutically acceptable salt of said compound or N-oxide, wherein A, Y, m, n, p, R 1 , R 2 , R 3 , R 3a , R 4 , R 5 , R 6 , R 7 and Z are as described herein; processes for their preparation; intermediates used in their preparation; and compositions containing such compounds, N-oxides or salts, and their uses for treating M4-mediated (or M4-associated) disorders, including, for example, Alzheimer's disease, Parkinson's disease, schizophrenia (e.g., the cognitive and negative symptoms thereof), pain, addiction, and sleep disorders.

The application belongs to the field of chemical drugs, and discloses a BTK protein degrading agent with a silicon-containing group as a hydrophobic tag, a preparation method, a pharmaceutical composition and application thereof.The structure of the BTK protein degrading agent with the silicon-containing group as the hydrophobic tag is shown in formula I, the linker is a saturated aliphatic chain, an unsaturated aliphatic chain, a connecting structure composed of an aromatic ring and a saturated aliphatic chain, or a connecting structure composed of an aromatic ring and an unsaturated aliphatic chain; and R is a specific silicon-containing group as the hydrophobic tag.A BTK protein degrading agent with a silicon-containing group as a hydrophobic tag is obtained, the preparation process is simple and easy to implement, the obtained BTK protein degrading agent has high liver microsomal metabolic stability, has considerable oral bioavailability, shows high treatment efficiency in in-vivo experiments, has a certain inhibitory effect on the proliferation of various tumor cells, and is suitable for the development of cancer drugs such as leukemia.

The invention relates to a high frequency magnetic induction device (100). The device (100) comprises magnetic nanosuspension (101) and an AMF generator (103). The AMF generator (103) further comprises copper induction coil (104), work head (105), flexible connector (106), power supply (107), chiller (108), display and control unit (109), fiberoptic thermometer sensors (110a &110b), auto-manual toggle switch (111), USB port (112a &112b) and bed support (113). Tumor site enclosed by the magnetic nanosuspension (101) comprising iron oxide magnetic nanoparticles (102) generates heat when exposed to AMF generated by the AMF generator (103). The heat generated does not cause any harm to the healthy tissues. The AMF generator (103) has precise control over thermal doses generated. The high frequency induction device (100) is safe, effective, non-invasive with mild side-effects.

The invention belongs to the technical field of preparation of anti-inflammatory drugs, and particularly discloses a tryptanthrin derivative and a preparation method and application thereof.The structural formula of the tryptanthrin derivative is # imgabs0, R is one of R1, R2 and R3, and when R is R1, # imgabs1 # reacts with H-R1, Pd (PPh3) 2Cl, copper iodide, triethylamine and an organic solvent to prepare the tryptanthrin derivative; when R is R2, the catalyst is prepared by reacting # imgabs2 # with H-R2, Pd2 (dppf) Cl2, potassium acetate and methylbenzene; when R is R3, the PdCl (PPh3) 4 is prepared by reacting with H-R3, silver carbonate, PdCl (PPh3) 4 and acetonitrile. The tryptanthrin derivative disclosed by the invention has high biological activity and solubility and low toxicity, and has the potential of being developed into a medicine for treating ulcerative colitis.

This disclosure provides methods of treating cystic fibrosis or a CFTR-mediated disease comprising administering Compound I, a deuterated derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing, e.g., administering about 1 mg to about 400 mg of Compound I. The disclosure also provides pharmaceutical compositions comprising Compound I, a deuterated derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing, and optionally comprising one or more additional CFTR-modulating agents.

To provide a compound having diacylglycerol kinase α (DGKα) inhibitory activity and useful for treating cancer including solid tumors and viral infections such as HIV or hepatitis B virus infection.SOLUTION: A compound of formula (I) or a pharmaceutically acceptable salt thereof is provided.SELECTED DRAWING: None

Provided herein are methods of treatment, including methods of treating subjects having or at risk of having or having a viral infection, and specifically a SARS-CoV-2 viral infection. The methods provided include the administration of 4-methylumbelliferone (4-MU), palmitoylethanolamide (PEA), reservatrol, fisetin, H2, nebulized hyaluronidase or combinations thereof. Also provided herein are a respiratory assistance device, methods of generating a customized respiratory assistance device, methods of treating a coronavirus infection, and methods of inhibiting a coronavirus infectivity, virulence and / or spread.

The purpose of the present invention is to provide a novel blood-brain barrier permeability regulator.　The present invention pertains to a blood-brain barrier permeability regulator containing a compound represented by formula (I) (Symbols in the formula (I) are as defined in the present specification.) or an isomer thereof, or a salt thereof. The present invention also pertains to a medicine for preventing and / or treating various brain diseases, severe infections, or sepsis by using the compound or an isomer thereof, or a salt thereof alone or in combination with a drug for preventing and / or treating a brain disease.

Provided herein are compositions comprising a silicate, inositol, and optionally an amino acid, which have improved solubility and / or are crystalline. Also provided are methods of making the disclosed compositions, as well as methods of making beverages comprising the disclosed compositions.

To provide compositions and methods for use in the treatment of Gram-positive bacterial infections.SOLUTION: The compound of formula I, or an optical isomer thereof, an isotopic isomer thereof, a prodrug thereof or a pharmaceutically acceptable salt thereof. (A, B:N, CH. n:0 to 3. R0:H, CH2PO (OH) 2, etc. R1: (CH2) m {(V) o (CH2) p} q W (V: CH2, CH=CH, CO, etc. W:H, halo, substituted / unsubstituted C1-6 alkyl, and the like. m:1-5. O, p, q:0-4). R2:H, halo, CN, etc. R3:Cl, F, Br, I, OH, etc. ) SELECTED DRAWING: None

The utility model provides a spherical tablet, and belongs to the field of pharmaceutical preparations. The spherical tablet comprises an upper hemisphere, a lower hemisphere and a middle belt, and the middle belt is located in the middle of the spherical tablet and is in a belt shape with the same thickness. The upper hemisphere and the lower hemisphere are located on the two end faces of the middle belt, and the two hemispheres are the same in size and shape. The diameter of the middle zone is larger than the diameter of the hemisphere, the diameter of the hemisphere of an upper stamping die and the diameter of the hemisphere of a lower stamping die of a tablet pressing die adopted when the spherical tablet is pressed ranges from 6.5 mm to 10 mm, and the ratio of the arc depth to the diameter of the hemisphere is (0.2-0.4): 1. The spherical tablet is small in size, easy to swallow, high in drug loading capacity and less in taking quantity; and the tablet has the advantages of good compressibility, good hardness, strong shock resistance and wear resistance, small tablet weight difference, facilitation of later coating and other operations, and good uniformity and reproducibility.

The application belongs to the field of medicinal chemistry, and provides a compound as an Akt kinase inhibitor, and particularly relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, a preparation method of the compound, a pharmaceutical composition containing the compound, and use of the compound in preparation of a medicament for treating an Akt kinase related disease.

PPAB derived near-infrared super-small fluorescent silica nanoparticles and synthesis method and application thereof, the fluorescent silica nanoparticles prepared by the present application exhibit strong near-infrared fluorescence and good water solubility, have a strong fluorescence emission peak near 650 nm-700 nm wavelength, exhibit good fluorescence spectrum performance, and therefore the silicon quantum dots have relatively good cell tissue penetration. Due to the unique optical properties and relatively good cell tissue penetration, the in vivo fluorescence imaging can be effectively carried out. The fluorescent silica nanoparticles prepared by the present application have excellent singlet oxygen generation performance and peroxidase performance in addition to excellent near-infrared optical performance and good biocompatibility, can be used as a photodynamic / chemodynamic synergistic treatment reagent, and are used for antibacterial and antitumor applications, and have no toxic side effects on the organism itself.

Disclosed are a compound as represented by formula I; a stereoisomer or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing same; and the use thereof as a PDE4B inhibitor in the preparation of a drug for the treatment of related diseases. Each group as shown in formula (I) is as defined in the description.