260 results about "Potency" patented technology

The invention discloses a quality control method of a traditional Chinese medicine preparation based on an IV-catfish orifice-freeing prescription, and relates to the technical field of analysis of traditional Chinese medicine preparations, and the quality control method comprises the following steps: carrying out microscopic identification on traditional Chinese medicine components in the IV-catfish orifice-freeing prescription, and determining a pharmacodynamic material basis. According to the quality control method for the traditional Chinese medicine preparation based on the IVV orifice-freeing prescription, various evaluation means such as a drug effect equivalent evaluation index, a stability test, a quality test and a clinical test are comprehensively applied, the consistency and reliability of the curative effect of the traditional Chinese medicine preparation can be remarkably improved, and the drug effect equivalent evaluation index is analyzed from the two factors of drug effect intensity and action time; the method ensures the equivalence of the medicinal component group and the original traditional Chinese medicine preparation, comprehensively detects the raw material medicines and the preparation, including characters, identification, inspection and content determination items, and ensures that the quality of each batch of samples meets the standard, so that the curative effect of the traditional Chinese medicine preparation is effectively guaranteed, and the efficacy of the traditional Chinese medicine preparation is improved.

The invention provides novel compounds which are peptide hormone analogues, and which are useful in treating disorders such as diabetes and obesity. The compounds of the general sequence recited in the specification possess a tailored profile with regards to potency properties at the GIP receptor. With regard to in vivo properties, administration of example peptides of the invention have been shown, in animal models, to result in increased weight loss. Preferred compounds achieve this without reducing food intake significantly.

The present disclosure provides a PD1 targeted novel IL-2 VitoKine composition, featuring a high-affinity PD1 antibody domain and a bio-activable IL- 2 domain with optimally reduced potency. The PD1 Ab-IL2 VitoKine platform mitigates IL-2 therapy-related toxicities and synergizes the anti-tumor effects of PD1 and IL- 2 by: 1) efficiently targeting an inert IL-2 directly to tumor-infiltrating lymphocytes (TILs); 2) ensuring highly tumorspecific activation of the IL- 2 domain by TME- enriched proteases that co-localized with TILs; 3) allowing PD1 Ab and activated IL- 2 to act on intratumoral CD8+T cells in cis. The VitoKine demonstrates greatly enhanced concealment efficiency and has a lower intrinsic basal activity than what would typically be expected from the VitoKine platform incorporating a non-attenuated IL-2. This improvement permits a substantially higher dose tolerance, enabling safe administration at efficacious dose levels of the PD1 antibody, reversing T- cell anergy or exhaustion and further synergizing with IL-2 mediated anticancer immune response.

The present disclosure pertains to novel Glucagon like Peptide-1 (GLP-1) (7-37) analogs having an amino acid sequence with Leu or Ile at the C-terminal. The new analogs are potent GLP-1 agonists with reduced adverse effect and improved duration of action. The present disclosure further relates to acylated derivatives of the new analogs which have further improved potency and duration of action and are suitable for oral administration. The analogs of present disclosure may be useful in treatment of diabetes and obesity.

The invention relates to the technical field of biological pharmacy, and discloses a QS-21 saponin adjuvant as well as a preparation method and application thereof, the adjuvant is a composite liposome and comprises a liposome skeleton composed of distearoyl phosphatidylcholine and cholesterol, and QS-21 saponin, monophosphoryl lipid A and a local anesthetic are jointly entrapped in the liposome skeleton. The problem that high reactogenicity and immunogenicity of potent adjuvants are difficult to consider at the same time is solved, the immunostimulation component and the pain inhibition component are jointly entrapped in the same nano-carrier, collaborative delivery in injection local is achieved, and therefore pain and swelling caused by the adjuvants are accurately inhibited. The co-entrapment structure avoids the potential inhibition effect of the free anesthetic on the immune system, the potent body fluid and cellular immune enhancement activity of the adjuvant is completely reserved, and a new technical scheme is provided for developing vaccines with high safety and strong immune efficacy.

The present invention relates to methods using trained classifier for assessing potency of a compound to revert the phenotype of a myotube exhibiting features of a neuromuscular disorder of interest into a healthy phenotype, for predicting the ability of a compound to treat a neuromuscular disorder of interest, for monitoring the response to a therapeutic compound of a patient affected with a neuromuscular disorder of interest, for selecting a patient affected with a neuromuscular disorder of interest for a treatment with a therapeutic compound or for determining whether a patient affected with a neuromuscular disorder of interest is susceptible to benefit from a treatment with a therapeutic compound, or for diagnosing a neuromuscular disorder of interest.

Provided are a sustained-release microsphere for polypeptide drugs, a pharmaceutical formulation thereof, a method for preparing same, and use thereof. The method comprises the following steps: forming an inner aqueous phase; forming an oil phase; forming an outer aqueous phase; and dispersing the inner aqueous phase into the oil phase to give a primary emulsion, then re-dispersing the primary emulsion into the outer aqueous phase to give a pre-secondary emulsion, emulsifying the pre- secondary emulsion to form a secondary emulsion, and finally curing the secondary emulsion to give the sustained-release microsphere. The method features ease to operate, and the obtained sustained-release microsphere possesses ideal drug release behaviors (low early burst release, and stable mid- and later-stage releases) and safety and potency in reducing blood glucose, and is thus suitable for stable, long-term use with good patient compliance.

Disclosed herein are monoclonal antibodies and antigen-binding fragments thereof capable of selectively inhibiting TGFβ1 with high potency. Related compositions, methods and therapeutic use are also disclosed.

The invention discloses a multi-target joint optimized antibiotic molecule design system and method applied to the field of biological medicine, and the method comprises the steps: obtaining FabI enzyme and AcrAB-TolC efflux pump structure data, extracting double-target space and physicochemical characteristics, and constructing a joint pharmacophore model containing a FabI inhibition domain and an efflux pump blocking domain; screening candidate molecules meeting a double-domain space matching threshold, screening high-affinity double-target molecules through conformation sampling and free energy calculation, and forming a lead compound library through multi-layer filtration of metabolic stability, membrane penetrability, quantum chemical properties and synthesis feasibility; carrying out electron effect, chain length or heteroatom fine tuning on dominant molecules through in-vitro bacteriostasis and efflux inhibition experiment feedback, and carrying out iterative optimization until MIClt is met; 2 [mu] g / mL and the efflux inhibition rate is gt; according to the present invention, the antibacterial effect and the drug resistance inhibition ability are significantly improved, the molecular synthesizability and the biological safety are ensured, and the engineering design new path is provided for the Gram-negative bacterium drug resistance crisis.

The invention provides a high-potency glucocorticoid compound as well as a preparation method and application thereof. Specifically, the invention provides a high-potency glucocorticoid compound as shown in a formula I as well as a preparation method and application of the high-potency glucocorticoid compound. The glucocorticoid compound of the present invention can achieve the same effect at a lower dose, thereby minimizing side effects. # imgabs0 #

Methods of determining the potency of a human neonatal Fc receptor (FcRn) antagonist composition in inhibiting the binding of human IgG to FcRn using a competition binding assay are provided. Kits for carrying out said methods, and methods of manufacturing a FcRn antagonist composition comprising said methods of determining potency are also provided.

The invention discloses a dexmedetomidine and propofol combined reagent and a combination method, and relates to the technical field of combined use of anesthetic drugs. According to the method, firstly, dexmedetomidine is subjected to intravenous pump injection within 5-15 minutes according to the dosage of 0.5-1.0 mu g / kg, propofol is given within 2 minutes after the dexmedetomidine is subjected to general anesthesia, and the dosage of the propofol can be reduced by 10%-50% compared with that of propofol which is independently used. Through pretreatment of dexmedetomidine, the anesthetic effect of propofol can be enhanced, adverse reactions such as blood pressure drop and respiratory depression can be effectively reduced, and anesthetic safety and controllability are improved. The combined reagent comprises independent containers for respectively loading the dexmedetomidine injection and the propofol emulsion, and can be packaged by adopting a double-cavity pre-filled injector, and sequential injection is realized through a controllable opening mechanism, so that unstable emulsification and titer change caused by physical mixing of medicines are avoided.

The invention discloses a small molecular twin drug compound with a synergistic analgesic effect and a pharmaceutical composition, a preparation method and application thereof. The twin drug molecule is formed by connecting a drug A and a drug B through a covalent bond, the drug A is nefopam, and the drug B is gamma-aminobutyric acid (GABA) and analogues thereof and comprises gabapentin, pregabalin, GABA, melogabalin and crigabalin. The analgesic effect of the composition is superior to that of combined administration and single administration, and the composition can obviously improve various acute and chronic inflammation pains and can relieve paclitaxel-induced peripheral neuralgia; the anti-inflammatory activity is higher than that of combined use and single drug, so that the compound has the potential of treating pain, inflammation and inflammatory pain related diseases; the interaction among the medicines can be effectively reduced, and the medication compliance of a patient is improved.

A system and method for predicting effects of ligands on receptors. The method includes identifying a plurality of conformations of a receptor, computing a probability of each of the plurality of conformations when the receptor is in an equilibrium complex with a ligand, to obtain a set of equilibrium probabilities, and using the set of equilibrium probabilities to predict an effect of the ligand on the receptor. The system and method can be used for designing drugs to modulate one or more biological signaling pathways, by predicting an efficacy of the ligand for one or more biological signaling pathways, and prioritizing and / or designing ligands based on predicted efficacies.

To provide arylcyclohexylamine compounds and their use in the treatment of psychiatric disorders.SOLUTION: There are provided arylcyclohexylamine compounds and compositions of a single enantiomer or enantiomerically enriched mixtures of arylcyclohexylamine having significantly higher oral bioavailability, higher antidepressant potency, and / or greater therapeutic index between antidepressant effects and side effects, compared to ketamine.SELECTED DRAWING: None

The invention discloses a compound with an aryl amide structure and medical application of the compound. The compound is a compound shown in a formula (I) or a pharmaceutically acceptable salt thereof, # imgabs0 #. In-vitro anti-tumor cell experiments are used as carriers to evaluate the efficacy of the compound shown in the formula I in treating various cancers, and it is found that the compound has good in-vitro activity and extremely high selectivity; the compound can be used as a precursor substance for further development of a cancer treatment effect by selectively inhibiting the aldoketoreductase 1C3.

Provided herein is an antibody-drug conjugate (ADC) especially a PEGylated mono- or bispecific antibody hydroxyl-bearing drug conjugate prepared with site-specific conjugation to provide homogeneous conjugate with high potency and low toxicity. The disclosure also relates to a method for the preparation of the antibody hydroxyl-bearing drug conjugate, a composition comprising the antibody hydroxyl-bearing drug conjugate, and the use thereof in treating diseases.

The new compound 3-(1-(2,3-dichloro-4-methoxyphenyl)ethyl)-1-methyl-1-(1,3,3-trimethylpiperidin-4-yl)urea monohydrochloride salt has a high capability to permeate through the blood-brain barrier and to display, at central nervous system level, a consistent ghrelin agonist activity; the compound is effective in the treatment and / or prevention of a medical condition mediated by the ghrelin receptor in the central nervous system. In particular, in experimental tests, the compound has shown high efficacy in the treatment of neurotoxic damage, with a useful combined pattern of neuroprotective effects both at central and peripheral level. The compound is further useful in the treatment of conditions which require a reduction of the heart rate. The compound is pharmacologically active at low to moderate doses, thus showing a favourable therapeutic index.

Embodiments provide for methods of predicting glycation percentage of an amino acid in a therapeutic biomolecule. In one example, a method of predicting a glycation percentage of an amino acid in a biomolecule includes determining a first set of rates for a de-glycation reaction for a first set of temperatures, inferring a second set of one or more rate(s) for the de-glycation reaction for a second set of temperatures, and using the second set of one or more rate(s) to predict the glycation percentage at any temperature corresponding to the second set of temperatures and over any time duration. Also provided are methods for maintaining a glycation percentage of an amino acid within a predetermined glycation percentage range over a shelf-life of a therapeutic biomolecule, and methods for either reducing or increasing a potency of a therapeutic biomolecule in a subject at a time of administration.

The invention discloses a living body screening method of a high-throughput addiction inhibitor, which comprises the following steps: acquiring addictive nematodes with a plurality of addiction behavioral phenotypes; applying different addiction inhibitors to the addictive nematodes; the screening of the addiction inhibitors is realized according to the inhibition efficacy of the addiction inhibitors on the addiction behavioral phenotypes of the addiction nematodes, and based on the steps, the drug screening of the addiction inhibitors can be realized through the inhibition efficacy of the addiction inhibitors on the addiction behavioral phenotypes of the addiction nematodes in a high-throughput manner. Compared with the prior art, the medicine screening method of a traditional cell function system is abandoned, and medicine screening is carried out on the living animal behavioristics level in a brand new mode. Meanwhile, the advantages of easiness in large-scale culture, abundant behavioral modes and the like of the nematodes are utilized, and compared with expensive mammal feeding and experimental operation for drug screening, the method has higher cost performance, practical operability and high throughput.

Respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD) are commonly treated with β2-adrenergic receptor agonists that activate intracellular signaling pathways to induce airway relaxation. However, current therapies are limited by progressive receptor desensitization, or tachyphylaxis, largely attributed to β-arrestin recruitment. This desensitization reduces therapeutic efficacy over time and complicates long-term disease management, resulting in suboptimal outcomes for patients who rely on bronchodilators for daily symptom control. Disclosed herein are pharmaceutical compositions comprising biased agonists and their methods of use, which minimally activate recruitment of beta-arrestin2.

The present application relates to azapeptide compounds of formula (I) derived from melanocyte-stimulating hormone release-inhibiting factor-1. A method to obtain compounds of formula (I) is also described herein. The compounds of formula (I) have been shown to be suitable for the treatment of dopamine-related disorders of the central nervous system. These compounds showed enhanced potency as positive allosteric modulators of the dopamine D2 receptors in comparison with the melanocyte-stimulating hormone release- inhibiting factor-1 and, in general, do not exhibit meaningful cytotoxicity.

The present invention provides high potency pharmaceutical compositions comprising high activity pancreatin enzymes. The invention is also directed to a process of producing HA-pancreatin enzymes and its compositions or dosage forms, and methods for their use.

Methods and materials for treating mammals having cardiovascular and / or metabolic disease are provided herein. For example, methods and materials for treating mammals having cardiovascular and / or metabolic disease by administering (a) an analog of a natriuretic peptide (NP), such as atrial natriuretic peptide (ANP) or dendroaspis natriuretic peptide (DNP), and (b) a glucagon-like peptide-1 (GLP-1) receptor / glucose-dependent insulinotropic polypeptide (GIP) receptor agonist are provided herein. The NP analogs used in the methods provided herein can be less than 20 amino acids in length and, in some cases, can have one or more variations in their ring portion (as compared to wild type ANP or DNP) that affect the potency of the analog in activating the particulate guanylyl cyclase (GC-A) receptor.

The invention provides novel compounds which are peptide hormone analogues, and which are useful in treating disorders such as diabetes and obesity. The compounds of the general sequence recited in the specification possess a tailored profile with regards5 to potency properties at the GIP receptor. With regard to in vivo properties, administration of example peptides of the invention have been shown, in animal models, to result in increased weight loss. Preferred compounds achieve this without reducing food intake significantly.

Described herein are compositions, kits, and methods for potent delivery to a cell of a subject. The cell can be of a particular cell type, such as a basal cell. In some cases, the cell can be a lung cell of a particular cell type. Also described herein are pharmaceutical compositions comprising a therapeutic or prophylactic agent assembled to a lipid composition. The lipid composition can comprise an ionizable cationic lipid, and a selective organ targeting lipid. The lipid composition can further comprise a phospholipid. Further described herein are high-potency intravenous dosage forms of a therapeutic or prophylactic agent formulated with a lipid composition.

The present invention relates to hAM15-52 analogues with improved amylin receptor (hAMY3R) potency (hAMY3R-EC50≤250 pM) and which are largely based on the sequence of the human adrenomedullin fragment hAM15-52. The invention further relates to hAM15-52 analogues that are selective amylin receptor (hAMY3R) agonists (hAMY3R-EC50≤250 pM and an hAM1R-EC50≥25 nM) and which are largely based on the sequence of the human adrenomedullin fragment hAM15-52. The hAM15-52 analogues according to the invention maintain the good physical stability of hAM15-52. The invention further relates to pharmaceutical compositions comprising such polypeptides and their use in the treatment of a medical condition such as obesity, NASH and / or diabetes.

The invention discloses an application of a serum meso-diaminopimelic acid detection method based on liquid chromatography-mass spectrometry or a detection product in sepsis, and relates to the technical field of biological detection. The detection method comprises the following steps: serum sample treatment, derivatization of 6-aminoquinoline-N-hydrogen succinimide carbamate, chromatographic separation and mass spectrometric detection. The detection kit comprises a meso-DAP standard substance, a Lys (Lys-d4) internal standard substance, a borate buffer solution and 6-aminoquinoline-N-succinimide methyl ester. The diagnosis efficacy AUC of meso-DAP is equal to 0.835, compared with a PCT detection method, the meso-DAP has better supplementary diagnosis efficacy, and compared with levo-DAP and dextro-DAP and total DAP, the sepsis diagnosis efficacy of meso-DAP is greatly improved. In addition, the method provided by the invention can also monitor the illness state to a certain extent, and also has a certain indication effect on prognosis.

The application provides an aniline skeleton compound with antitumor activity and a preparation method and application thereof, and belongs to the technical field of small molecule inhibitor preparation. The aniline skeleton compound with antitumor activity has a structural formula as shown in formula I. The aniline skeleton compound has good antitumor activity in vivo and in vitro, and effectively solves the problems of target drug resistance and insufficient efficacy in the prior art.

The invention discloses a halogen modified hapten for enhancing antibody titer and affinity as well as a preparation method and application of the halogen modified hapten, and belongs to the technical field of biochemical engineering. According to the method, an amantadine structure is innovatively and chemically modified, various halogens such as fluorine, chlorine and bromine are introduced, the AMA halogen modified hapten shown in the formula (I) is formed, and the traditional'most similar 'design principle is broken through. Compared with an unmodified hapten, the hapten modified by halogen in the invention has the advantages that the titer of the polyclonal antibody on amantadine can be obviously improved by 3.4-14 times; wherein the haptens A5 and A6 can obviously improve the titer of the monoclonal antibody to amantadine by 3-18 times, and the affinity is improved by 10.8-16.1 times. The invention provides a new thought and a new method for the rational design of the hapten of the small molecule compound and the preparation of the high-affinity antibody, and the related halogen modification type and quantity strategy can also provide valuable reference for the design of the hapten of other small molecule compounds.