3477results about "Amide active ingredients" patented technology

The present invention provides a compound having a structure of formula (I) and can be used as an SHP2 inhibitor, a pharmaceutical composition comprising the compound, a method for preparing the compound, and a use of the compound in the treatment of cancer.

The present disclosure relates generally to various salt forms and compositions thereof useful for the modulation of interleukin-1 receptor-associated kinase 4 ("IRAK4") via ubiquitination and / or degradation and uses of the same in the treatment various diseases.

The present disclosure features a combination therapy useful for the treatment of solid tumors.

Computer-implemented methods of predicting the QTc of a subject in response to administration of QTc prolonging drugs, especially those that are dose adjusted for renal function, such as antiarrhythmic drugs. Included is a method of administering an antiarrhythmic drug to a subject, comprising: providing as inputs into a treatment management application i) Baseline QTc and ii) at least a Creatinine Clearance, Weight, Age, Sex, or Heart Rate; the treatment management application providing as an output one or more predicted QTc or predicted QTc range for the subject expected from administration of a 1-5 hour IV dose, alone or followed by one or more oral doses, of an antiarrhythmic drug to the subject; and upon the one or more QTc or QTc range being within an acceptable range, administering the 1-5 hour IV dose to the subject optionally followed by administering one or more of the oral doses to the subject.

The present disclosure provides methods of treating opioid use disorder in a patient in need thereof by intravenously administering to the patient a therapeutically effective amount of ibogaine or pharmaceutically acceptable salt thereof.

Methods of administering sotalol hydrochloride in an amount effective for treating one or more cardiovascular disease or disorder in pediatric patients are described and include IV and / or oral doses based on age-specific creatinine clearance ranges.

The invention relates to the technical field of pharmaceutical preparations, and discloses a composition with liver protection and antioxidation effects and a preparation method thereof.The composition is prepared from galactosamine modified astragalus membranaceus exosome, schisandra chinensis nanocrystals, liquorice-chitosan nanoparticles, lactobacillus acidophilus freeze-dried powder, beta-(1, 3) / (1, 3, 4-tetramethyl-1, 3-pentanediol monoisobutyrate) sourced from saccharomyces cerevisiae, and beta-(1, 3, 4-tetramethyl-1, 3-pentanediol monoisobutyrate). And (6) a dextran, grape exosome-curcumin hybrid vesicle freeze-dried powder, a curcumin-mitochondrial targeting peptide compound, a resveratrol-hydroxypropyl-beta-cyclodextrin inclusion compound and reduced panthenol. According to the liver-protecting and anti-oxidation composition disclosed by the invention, multi-dimensional intervention on liver protection is realized through an elaborately designed ternary system. The system is composed of a traditional Chinese medicine extract, a microorganism-plant exosome combination and a high-bioavailability antioxidant, all the parts have a synergistic effect, and the liver protection effect is remarkably improved.

Disclosed are naphthyl compounds comprising either a ureido piperidine-1 -carboxamide or a ureido piperidine-1 -carboxylate moiety, compositions thereof, and methods of use thereof, for treating or preventing a disease or disorder associated with abnormal levels of amino acids by modulation of SLC6A19 transport, such as phenylketonuria, hyperphenylalaninemia, diabetes and chronic kidney disease.

The present invention provides novel methods of administering sotalol hydrochloride to patients in need thereof.

The present invention provides novel methods of initiating and escalating sotalol hydrochloride in patients in need thereof.

Disclosed are methods of treating a subject having clinically significant signs and symptoms associated with blood cell differentiation and treated with an agent that reduces the level and / or activity of BRG1 and / or BRM. The methods disclosed herein may include, e.g., administering to the subject an effective amount of a corticosteroid, hydroxyurea, or furosemide, or subjecting the subject to leukapheresis.

The invention provides a VEGFR2-HDAC6 dual inhibitor containing chalcone fragments as well as a preparation method and application of the VEGFR2-HDAC6 dual inhibitor, and relates to the technical field of medicinal chemistry. The invention discloses a VEGFR2-HDAC6 dual inhibitor containing chalcone fragments. The structural formula of the VEGFR2-HDAC6 dual inhibitor is shown as a formula A, according to the invention, the VEGFR2-HDAC6 dual inhibitor containing the chalcone fragment and having a novel structure is designed and synthesized by utilizing a splicing principle, the anti-proliferative activity test is carried out on cervical cancer cells Siha and chronic granulocytic leukemia cells K562, and the result shows that the VEGFR2-HDAC6 dual inhibitor containing the chalcone fragment provided by the invention has relatively good inhibitory activity on the Siha cells and the K562 cells.

The invention relates to mRNA comprising lipid nanoparticles and their medical uses. The lipid nanoparticles of the present invention comprise a cationic lipid according to formula (I), (II) or (III) and / or a PEG lipid according to formula (IV), as well as an mRNA compound comprising an mRNA sequence encoding an antigenic peptide or protein. The invention further relates to the use of said lipid nanoparticles as vaccines or medicaments, in particular with respect to influenza or rabies vaccination.

The invention discloses a double-layer gel patch for diabetic wounds and a preparation method of the double-layer gel patch. The double-layer gel patch is composed of an upper gel layer and a lower gel layer, and when the double-layer gel patch is used, the lower gel layer is attached to the surface of skin; the upper gel layer is prepared from methacrylated gelatin, oxidized hyaluronic acid, a photoinitiator and an anti-inflammatory drug, and the lower gel layer is prepared from 3-carboxyphenylboronic acid grafted gelatin, dihydrocaffeic acid grafted epsilon-polylysine and an antibacterial agent. The double-layer gel disclosed by the invention has high mechanical strength and absorbability, and meanwhile, a sequential treatment strategy of firstly resisting bacteria and then resisting inflammation can be realized.

The invention provides combination therapies comprising disease modifying anti-rheumatic drugs and mitochondrial complex I modulator (MCIM) compounds, which find utility in the medical field of inflammatory and progressive disorders, for example autoimmune diseases such as arthritis.

The present invention relates to N-palmitoyl ethanolamide for the treatment of inflammatory pain in combination with a non-steroidal anti-inflammatory drug, to the use of N-palmitoyl ethanolamide (referred to as palmitoyl ethanolamide or PEA) in combination with a non-steroidal anti-inflammatory drug for the treatment of inflammatory pain. Specifically, the present invention relates to palmitoyl ethanolamide for use in the treatment of inflammatory pain, in particular non-neurological inflammatory pain, in which palmitoyl ethanolamide is administered in combination or in combination with a non-steroidal anti-inflammatory drug as needed, in which the administration is separate, combined or simultaneous.

The invention discloses an antibacterial peptide simulant based on adamantane modification and application of the antibacterial peptide simulant. The preparation method comprises the following steps: performing amide condensation on Fmoc amino acid to obtain a compound of which the carboxyl terminal is modified by amantadine or Boc protected aliphatic amine, and then removing an Fmoc group by piperidine to obtain a series of amantadine modified crude products and Boc protected aliphatic amine modified intermediate compounds; the intermediate compound is subjected to amide condensation to obtain a compound of which the amino terminal is further modified by adamantanic acid, then other protecting groups are cracked by trifluoroacetic acid to obtain a series of adamantanic acid modified crude products, and the crude products are purified to obtain the adamantane modified peptidomimetic. The adamantane modified peptidomimetic is used for preparing drugs for treating infectious diseases caused by sensitive bacteria and drug-resistant bacteria, has efficient antibacterial activity and low toxicity, and is not influenced by a traditional drug-resistant mechanism.

Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.

The invention discloses an N-phenylbenzenesulfonamide compound as well as a preparation method and application thereof. The compound disclosed by the invention is shown as a formula (I). The compound is an LDHA enzyme inhibitor, is a sulfonamide compound with anti-tumor activity, shows good anti-tumor activity at the cellular level, has good safety and can be used for preparing anti-tumor drugs. # imgabs0 #

Disclosed herein are compounds used as inhibitors of KAT6, or a pharmaceutically acceptable salt, deuterated analog, N-oxide, or tautomer thereof. Also disclosed is a pharmaceutical composition comprising a compound disclosed herein, and a method for treating or preventing a disorder or a disease responsive to the inhibition of KAT6 activity in a subject using the same. In some embodiments, the compounds are of formula (I), wherein values for the variables are disclosed herein.

The present invention relates to the use of N-palmitoylethanolamide (known as palmitoylethanolamide or PEA) in combination with a non-steroidal anti-inflammatory drug in the treatment of inflammatory pain. In particular, the present invention is directed to palmitoylethanolamide for use in the treatment of inflammatory pain, in particular non-neuropathic inflammatory pain, where palmitoylethanolamide is administered as needed in association or combination with a non-steroidal anti-inflammatory drug, where said administration is separate, combined, or simultaneous.

The invention discloses application of carbaspillin calcium in preparation of a medicine for treating hydrocephalus, belongs to the technical field of medicines for treating hydrocephalus, and particularly relates to application of carbaspillin calcium in preparation of a medicine for treating hydrocephalus, and the medicine takes carbaspillin calcium as a unique or main effective component. The effect of carbaspillin calcium in treating hydrocephalus is found for the first time, the fourth ventricle area of the hydrocephalus model zebrafish can be remarkably reduced, and the swimming distance, swimming time, swimming speed and rotational motion frequency of the hydrocephalus model zebrafish can be remarkably increased; experimental data provided by the invention show that the carbaspillin calcium has a huge application prospect in treatment of hydrocephalus, and an effective candidate drug is provided for relieving the treatment pain of a patient with hydrocephalus and reducing the treatment risk and cost; and the action range of the carbaspirin calcium is widened.

The invention belongs to the technical field of OAB-14 medical chemistry and preparation thereof, and particularly relates to a crystal form D of OAB-14 and a preparation method thereof. The preparation method of the crystal form D of OAB-14 comprises the following steps: adding OAB-14 into a solvent, and carrying out suspension pulping, heat preservation stirring, suction filtration and drying to obtain the crystal form D. The solvent is one of THF (tetrahydrofuran), MeOH (methanol), EtOH (methanol), EA (ethyl acetate) and MTBE (methyl tert-butyl ether). The suspension pulping temperature is 15 to 25 DEG C. And the heat-preservation stirring time is 1-5 days. After the OAB-14 is added into the solvent, the concentration of the OAB-14 is 0.005 g / mL to 0.01 g / mL. According to the preparation method of the crystal form D of OAB-14 provided by the invention, the crystal form D is an anhydrous crystal form with high crystallinity, high dissolution rate and high stability.

The invention belongs to the technical field of stem cell biological preparations, and particularly relates to an anti-aging compound preparation based on stem cells and application of the anti-aging compound preparation in delaying skin aging. The composition is composed of an inner water phase, a middle oil phase and an outer water phase, wherein the inner water phase is prepared from the following components: stem cell exosomes, hyaluronic acid, nicotinamide ribose, trehalose, mannitol, glycine and a citric acid buffer solution; the medium oil phase is prepared from the following components: medium chain triglyceride, shea butter, vitamin E succinate, PEG (Polyethylene Glycol) modified ceramide NP and cholesterol succinic acid monoester; the external water phase is prepared from the following components: polydatin, cellulose nanocrystals and an emulsifying agent. On the basis of a W / O / W emulsion system, a multi-layer anti-aging mechanism is constructed by utilizing a three-dimensional delivery framework of an inner water phase, an oil phase and an outer water phase and space-time synergy of active ingredients, the exosome permeation efficiency is improved through microneedle introduction, and the anti-oxidation and barrier repair effects are achieved by using multiple ingredients.

The invention belongs to the technical field of biological medicines, and particularly relates to an iron-based nano material, a preparation method and application of the iron-based nano material in preparation of medicines for treating breast cancer. The iron-based nano material is formed by loading a ferroptosis inducer on a nano carrier; the nano carrier is an iron-based metal organic framework material Fe-MOF (Metal Organic Framework). A product FEH for treating breast cancer is obtained based on coupling of the iron-based nano-material provided by the invention with a targeted drug such as trastuzumab. The FEH provides a new method for developing a nano platform with an antibody function, and realizes a treatment strategy of trastuzumab and ferroptosis combined anti-tumor. As a safe and effective tumor treatment strategy, the EFH has huge clinical transformation potential.

The invention discloses application of an IL-8 inhibitor to treatment of diabetic retinopathy patients. The molecular mechanism of IL-8 in the diabetic retinopathy generation and development process is deeply explored, a theoretical basis is provided for SB225002 to influence the generation and development of diabetic retinopathy through inflammation, and a feasible direction is provided for diabetic retinopathy treatment and targeted retinal neovascularization treatment drugs.

Compositions and methods for cleansing the eyelid and treating an ocular condition with an ophthalmic composition consisting essentially of water, PEG-80 sorbitan laurate, methyl gluceth-20, PEG-120 methyl glucose dioleate, phytosphingosine HCl, decyl glucoside, 1,2-hexanediol, caprylyl glycol, disodium cocoamphodiacetate, panthenol, polyaminopropyl biguanide, sodium chloride, potassium chloride and calcium chloride.

The present disclosure is related to a conjugate of an active drug and a glycosaminoglycan, such as hyaluronic acid (HA). For example, the active drug can be lenalidomide, nimesulide, or gemcitabine. The conjugate of the present disclosure is useful in the treatment of certain cancers.

The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and / or angiogenesis in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.

The invention relates to a dihydroarteannuic acid compound as well as a preparation method and application thereof. The structure of the dihydroarteannuic acid compound is shown as a formula I in the specification. The dihydroarteannuic acid compound or the pharmaceutically or cosmetically acceptable salt of the dihydroarteannuic acid compound shows good melanogenesis inhibition activity and anti-inflammatory activity at the cellular level, has good safety, can be used as a melanogenesis inhibitor, and can be used for preparing anti-inflammatory drugs. The composition is used for preparing medicines for treating senile plaques, chloasma, freckles and hyperpigmentation after inflammation and cosmetics for whitening and removing freckles.