46 results about "Racemic mixture" patented technology

S-Beta-hydroxybutyric acid compositions for oral delivery are effective in rapidly raising blood ketone levels without causing acute acidosis or gastrointestinal (GI) distress when consumed in sufficiently dilute form and / or as a gel or suspension. By limiting added beta-hydroxybutyrate salts containing alkali or alkaline earth metal ions, beta-hydroxybutyric acid solutions, gels, or suspensions can deliver exogenous ketone bodies without significantly altering electrolyte balance. Although aqueous beta-hydroxybutyric acid solutions are moderately acidic with a pH of about 3.5 to 4, when diluted with sufficient water, the water acts as a pseudo buffering agent that offsets otherwise harsh acidic effects when consumed orally. Gels and suspensions can also ameliorate acidic effects by partially encapsulating the beta-hydroxybutyric acid. Beta-hydroxybutyric acid can be pure S-beta-hydroxybutyric acid or a non-racemic mixture enriched with S-beta-hydroxybutyric acid relative to R-beta-hydroxybutyric acid.

The invention discloses a compound as shown in a formula (I), and / or pharmaceutically acceptable salts thereof, and / or a raceme mixture, a hydrate, a solvate, a prodrug, an enantiomer, a diastereoisomer and a tautomer thereof, and belongs to the technical field of medicines. The invention also discloses a pharmaceutical composition containing the compound as shown in the formula (I), and the compound as shown in the formula (I) and / or a pharmaceutically acceptable salt thereof, and / or a racemic mixture, a hydrate, a solvate, a prodrug, an enantiomer, a diastereoisomer and a tautomer thereof, and / or the pharmaceutical composition, a pharmaceutically acceptable salt thereof, and / or a racemic mixture, a hydrate, a solvate, a prodrug, an enantiomer, a diastereoisomer and a tautomer thereof. The invention further discloses application of the cGAS agonist in preparation of the cGAS agonist and a medicament for treating diseases responding to activation of the cGAS-STING signal channel.

The present invention relates to the early treatment, including pre-diagnosis treatment, of sepsis and acute inflammatory syndromes such as systemic inflammatory response syndrome (SIRS) by PLA2 and metalloprotease inhibitors to improve the performance of antibiotics and outcomes prior to and after confirmation of the diagnosis of sepsis and / or SIRS in a patient or subject. Additional embodiments include methods of treating sepsis, anthrax and severe acute respiratory syndrome coronavirus (SARS and SARS-CoV2) and related inflammatory syndromes and compositions, including pharmaceutical compositions and blood sample compositions. In further embodiments, the present invention is directed to embodiments which evidence that LY315920, LY333013 and related sPLA2 inhibitors are particularly effective COVID-19 / cytokine release syndrome therapeutics-prophylactics. In embodiments, the PLA2 inhibitor is varespladib (LY315920), methyl varespladib (LY333013), AZD2716-(R)-3-(5′-benzyl-2′-carbamoyl-[1,1′-biphenyl]-3-yl)-2-methylpropanoic acid—as a racemic mixture or separately, as the “R” enantiomer), compound 4 (3-(5′-benzyl-2′-carbamoyl-[1,1′-biphenyl]-3-yl)-propanoic acid) and LY433771 ((9-[(phenyl)methyl]-5-carbamoylcarbazol-4-yl) oxyacetic acid), a pharmaceutically acceptable salt thereof or a mixture thereof. In embodiments, the metalloprotease inhibitor is Prinomastat, Batimastat, marimastat or vorinostat dosed alone or in combination with preferred sPLA2 inhibitors for the treatment of infection, inflammatory and wound conditions arising from various causes. Methods and compositions for achieving accelerated treatment of wounds and burns, anthrax metalloprotease toxin (lethal factor) driven complications, ARDS, neo-natal and pediatric acute respiratory distress syndrome (neo-natal / pediatric ARDS), including meconium aspiration syndrome and other disease states and conditions are also disclosed.

The present invention refers to a method for the preparation of a compound according to formula (45), its enantiomers, diastereomers, a racemic mixture, and the pharmaceutically acceptable salts thereof. Furthermore the invention refers to a compound of formula (45) prepared by said method for use in treatment of neurodegenerative disorders and to pharmaceutical compositions.

The present invention relates to a process for the preparation of (±)‑2‑exo‑(2‑methylbenzyloxy)‑1‑methyl‑4‑isopropyl‑7‑oxabicyclo[2.2.1]heptane of formula (I), any of its individual enantiomers or any non-racemic mixture thereof, comprising the steps of: (a) reacting (±)‑2‑exo‑hydroxy‑1‑methyl‑4‑isopropyl‑7‑oxabicyclo[2.2.1]heptane of formula (II), any of its individual enantiomers or any non-racemic mixture thereof, with a 2-methylbenzyl compound of formula (III), wherein X is a leaving group, in the presence of at least one base capable of forming water or a C1-C4 alkyl alcohol under the reaction conditions and at least one inert organic solvent, and (b) simultaneously removing water, C1-C4 alkyl alcohol or any mixture thereof from the reaction mixture.

The invention relates to the technical field of medical compounds, in particular to a deubiquitinating enzyme targeted chimera compound as well as a pharmaceutical composition and application of the deubiquitinating enzyme targeted chimera compound. The deubiquitinating enzyme targeting chimera compound is a compound with a structure as shown in a formula (I), and / or a pharmaceutically acceptable salt thereof, and / or a racemic mixture, a hydrate, a solvate, a prodrug, an enantiomer, a diastereoisomer and a tautomer thereof, the structural formula of the formula (I) is as shown in the specification, and the definitions of X, Linker and cGAS Ligand are as shown in the specification. The compound provided by the invention increases the abundance of the cGAS protein, has an obvious effect of improving the stability of the intracellular cGAS protein, and is used for preparing medicines for treating inflammatory diseases, tumors, cardiovascular and cerebrovascular diseases and infectious diseases.

The present invention relates to a compound of the chemical formula (1a): (1a) The invention relates to or its enantiomers, racemic mixtures, or pharmaceutically acceptable salts. The invention also relates to a pharmaceutical composition comprising a compound of formula (1a), its enantiomers, racemic mixtures, or pharmaceutically acceptable salts, and one or more pharmaceutically acceptable excipients, and a method for treating autoimmune diseases, central nervous system diseases, and leukocyte disorders, comprising the step of administering the pharmaceutical composition of the invention to an individual in need.

Beta-hydroxybutyrate compositions formulated for ingestion by oral delivery as a beverage, or as a dietary supplement for addition to water or beverage, include a liquid carrier, such as water, milk, drinkable liquid, coconut water, watermelon water, or electrolyte water, and beta-hydroxybutyrate. The beta-hydroxybutyrate composition can include enantiomerically pure R-beta-hydroxybutyrate or a non-racemic mixture enriched in R-beta-hydroxybutyrate relative to S-beta-hydroxybutyrate. Alternatively, the beta-hydroxybutyrate composition can include enantiomerically pure S-beta-hydroxybutyrate or a non-racemic mixture enriched in S-beta-hydroxybutyrate relative to R-beta-hydroxybutyrate. Alternatively, the beta-hydroxybutyrate composition can include a racemic mixture of R-beta-hydroxybutyrate and R-beta-hydroxybutyrate. The beta-hydroxybutyrate compositions comprise beta-hydroxybutyric acid and optionally one or more beta-hydroxybutyrate salts or esters.

Methods and compositions for the prevention and treatment of acute radiation syndromes and radiation illnesses from exposure to toxic radiation including radiation therapy treatments, the methods and compositions comprise Indole derivatives and their administration to a living being, where Indole derivative compositions include a racemic mixture of R-Indole derivative and S-Indole derivative enantiomers, or isolated R-Indole derivative enantiomers, or S-Indole derivative enantiomers. The compositions of the invention are suitable for treating and / or preventing radiation injury, and embodiments may comprise functional analogs, derivatives, racemic mixtures and / or chiral forms, S and / or R thereof. Indole derivative compositions include compositions having the formulae: (S)-1-(3-Indolyl)-2-(methylamino) ethanol; (S)-α-[(Methylamino)methyl]-1H- Indole-3-methanol, indolo[a]pyrrolo[3,4-c] carbazole integrin composition. The method involves administering an effective amount of an indole composition in a pharmaceutically acceptable form, to provide a fast-acting medical countermeasure with radioprotective and radiomitigative functionalities for treatment or prevention of radiation illnesses.

The present application relates to a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and stereoisomers thereof, including enantiomers, racemic mixtures, mixtures of enantiomers, or a combination thereof, for use in the treatment of cancer diseases. The present application also relates to a pharmaceutical composition comprising the above-mentioned compound.

Compositions for improving metabolic function in a subject include optically pure S-beta-hydroxybutyrate or non-racemic mixtures enriched with the S-enantiomer. S-beta-hydroxybutyrate in pure or enriched form provides energy to the heart, dilates the arteries, decreases blood pressure and systemic vascular resistance, and increases cardiac output. S-Beta-hydroxybutyric acid is more rapidly absorbed and utilized by the body than salts or esters, enhances taste, and reduces the need to include citric acid or other edible acids. S-Beta-hydroxybutyrate salts are more slowly absorbed and utilized by the body and provide one or more electrolytes. S-Beta-hydroxybutyrate esters provide more controlled release without adding electrolytes. Compositions for improving heart function in a subject may contain a dietetically or pharmaceutically acceptable carrier and optically pure S-beta-hydroxybutyrate or non-racemic mixture enriched with S-beta-hydroxybutyrate, wherein the compositions contain from about 50.5% to 100% by enantiomeric equivalents of S-beta-hydroxybutyrate and from about 49.5% to 0% by enantiomeric equivalents of R-beta-hydroxybutyrate.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a resolution method of an azacyclo derivative, which comprises the following steps: carrying out salt forming reaction on 5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1, 2, 4-triazole-5-yl)-2, 7, 8, 9-tetrahydro-3H-pyrido [4, 3, 2-de] phthalazin-3-one racemate and chiral acid, and carrying out crystallization resolution to obtain (8S, 8S)-1, 2, 4-triazole-5-yl)-2, 7, 8, 9-tetrahydro-3H-pyrido [4, 3, 2-de] phthalazin-3-one. According to the present invention, the (1R, 9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1, 2, 4-triazole-5-yl)-2, 7, 8, 9-tetrahydro-3H-pyridino [4, 3, 2-de] phthalazin-3-one is synthesized by using the method, the resolution method is simple, the production cost can be effectively reduced, the production efficiency can be improved, and the method is suitable for industrial production.

The invention belongs to the technical field of medicines, and particularly relates to application of tropine acid and a derivative thereof in preparation of a medicine for treating immune and inflammation related diseases and the medicine for treating the immune and inflammation related diseases. The tropine acid and the derivative thereof are compounds shown in the formulas I-IV or pharmaceutically acceptable salts thereof, and solvent compounds, enantiomers, diastereoisomers and tautomers of the compounds shown in the formulas I-IV or the pharmaceutically acceptable salts thereof or a mixture of the solvent compounds, the enantiomers, the diastereoisomers and the tautomers in any proportion, including a racemic mixture. Animal tests show that the tropine acid and the derivative thereof have broad-spectrum immunoregulation, anti-inflammatory and analgesic effects, have an obvious improvement effect on pathological indexes of numerous immune and inflammation-related disease animal models, can regulate abnormal immunoreactions to tend to be normal, and exert good anti-inflammatory and analgesic effects; the method can adapt to patients with different disease degrees and different types of immune and inflammation related diseases, and can be industrially applied.

Compositions for improving heart function in a subject include optically pure S-beta-hydroxybutyrate or non-racemic mixtures enriched with the S-enantiomer. S-beta-hydroxybutyrate in pure or enriched form provides energy to the heart, provides antiglycation and signaling, which lessens or reduces cardiovascular disease by lessening or preventing atherosclerosis, plaque formation, diastolic dysfunction, systolic dysfunction, fibrosis, and hypertension, and / or by facilitating normal nitric oxide (NO) production, which dilates the arteries, reduces blood pressure and systemic vascular resistance, and increases cardiac output in humans. S-Beta-hydroxybutyric acid is more rapidly absorbed and utilized by the body than salts or esters. S-Beta-hydroxybutyrate salts are more slowly absorbed and utilized by the body and provide one or more electrolytes. S-Beta-hydroxybutyrate esters provide more controlled release without adding electrolytes. Compositions for improving heart function may contain a dietetically or pharmaceutically acceptable carrier and S-beta-hydroxybutyrate or non-racemic mixture enriched with S-beta-hydroxybutyrate.

The invention belongs to the technical field of medicines, and particularly relates to application of tropine acid and a derivative thereof in preparation of a medicine for treating immune and inflammation related diseases and the medicine for treating the immune and inflammation related diseases. The tropine acid and the derivative thereof are compounds shown in the formulas I-IV or pharmaceutically acceptable salts thereof, and solvent compounds, enantiomers, diastereoisomers and tautomers of the compounds shown in the formulas I-IV or the pharmaceutically acceptable salts thereof or a mixture of the solvent compounds, the enantiomers, the diastereoisomers and the tautomers in any proportion, including a racemic mixture. Animal tests show that the tropine acid and the derivative thereof have broad-spectrum immunoregulation, anti-inflammatory and analgesic effects, have an obvious improvement effect on pathological indexes of numerous immune and inflammation-related disease animal models, can regulate abnormal immunoreactions to tend to be normal, and exert good anti-inflammatory and analgesic effects; the method can adapt to patients with different disease degrees and different types of immune and inflammation related diseases, and can be industrially applied.

The present application relates to novel compounds of formula (I) or detectably labeled compounds thereof, stereoisomers, racemic mixtures, pharmaceutically acceptable salts, hydrates or solvates, which are useful for imaging and determining the amount of alpha-synuclein aggregates. Furthermore, the compounds may be used to diagnose a disease, disorder, or disorder associated with alpha-synuclein aggregates (e.g., Parkinson's disease or e.g., multi-system atrophy (MSA)), to determine susceptibility to the disease, disorder, or disorder, to predict prognosis of the disease, disorder, or disorder, to monitor disease progression in a patient suffering from the disease, disorder, or disorder, and to diagnose a disease, disorder, or disorder associated with alpha-synuclein aggregates. The progression of such diseases, disorders or abnormalities is monitored and the responsiveness of patients suffering from such diseases, disorders or abnormalities to their treatment is predicted.

This invention discloses a method for resolving racemic mixtures based on dynamic kinetics, belonging to the field of catalysis technology. The method includes the following steps: taking a proton-selective permeable membrane and pretreating it; using the pretreated proton-selective permeable membrane to separate the aqueous phase and organic phase for reaction, thereby resolving the racemic mixture; wherein the aqueous phase is an acid solution, and the organic phase contains at least the racemic mixture, an acyl donor, an enzyme, and an organic solvent, and the racemic mixture is a racemic mixture of a chiral secondary alcohol or its derivative. This invention utilizes a proton-selective permeable membrane as a racemic catalyst applied to the dynamic kinetic resolution process, solving the problem of incompatibility between racemic catalysts and enzyme catalysts in conventional dynamic kinetic resolution techniques. This method has advantages such as a simple reaction system, easy process control, environmental friendliness, simple post-processing, and low cost.

A method of treating and / or preventing disease involving retinal pigment epithelium, including administering compound of formula (I)or a pharmaceutically acceptable salt, a racemic mixture, a corresponding enantiomer or a corresponding diastereomer thereof, wherein: R1, R11 and R12 are independently selected from the group consisting of hydrogen, fluoro, chloro, methoxy, trifluoromethyl, methyl and difluoromethoxy, whereby at least one of R1, R11 and R12 is not hydrogen, B is selected from the group consisting of a residue of formula (II), (III), (IV), (V), (VI) and (VII)wherein, “*” denotes point of attachment to remainder of the molecule, and R2, R3, R4, R5, R2I, R3I, R4I, R5I, R2II, R3II, R4II, R5II, R2III, R3III, R4III, R5III, R2IV, R3IV, R4IV, R5IV, R2V, R3V, R4V, R5V are independently selected from the group consisting of hydrogen, a linear or branched alkyl having 1 to 3 carbon atoms, fluoro, chloro, bromo, methoxy, ethoxy, propoxy, trifluoromethyl and difluoromethoxy.

The application discloses a kind of non-natural nucleoside analogues as shown in the following formula 1 and its pharmaceutically acceptable salt, racemic mixture, enantiomer, optical isomer, tautomer and solvate, and pharmaceutical composition comprising them, and its purposes in preparing antiviral infection and antitumor drug and its use method.The non-natural nucleoside analogues have good broad-spectrum antiviral activity or antitumor cytotoxicity.

Compositions for improving metabolic function in a subject include optically pure S-beta-hydroxybutyrate or non-racemic mixtures enriched with the S-enantiomer. S-beta-hydroxybutyrate in pure or enriched form provides energy to the heart, dilates the arteries, decreases blood pressure and systemic vascular resistance, and increases cardiac output. S-Beta-hydroxybutyric acid is more rapidly absorbed and utilized by the body than salts or esters, enhances taste, and reduces the need to include citric acid or other edible acids. S-Beta-hydroxybutyrate salts are more slowly absorbed and utilized by the body and provide one or more electrolytes. S-Beta-hydroxybutyrate esters provide more controlled release without adding electrolytes. Compositions for improving heart function in a subject may contain a dietetically or pharmaceutically acceptable carrier and optically pure S-beta-hydroxybutyrate or non-racemic mixture enriched with S-beta-hydroxybutyrate, wherein the compositions contain from about 50.5% to 100% by enantiomeric equivalents of S-beta-hydroxybutyrate and from about 49.5% to 0% by enantiomeric equivalents of R-beta-hydroxybutyrate.

This invention relates to a compound for treating thrombotic diseases. Specifically, this invention provides a compound of Formula I, or a pharmaceutically acceptable salt thereof, or its enantiomer, diastereomer, transtransferase, racemic mixture, polymorph thereof, solvate thereof, or isotopically labeled derivative thereof. The compound of this invention specifically binds to the SH3 domain protein of Src kinase, interfering with the binding of integrin αIIbβ3 to Src kinase, thereby selectively inhibiting outward-to-inward signal transduction without affecting inward-to-outward signal transduction. This allows the compound of this invention to exert antithrombotic effects without affecting normal physiological hemostasis, avoiding bleeding side effects, and thus becoming a new generation of effective drugs for the prevention and treatment of thrombosis-related cardiovascular and cerebrovascular diseases.

The invention discloses a hydroxamic acid compound containing gamma-tetrahydrocarboline as shown in a general formula (I), and / or pharmaceutically acceptable salts, racemic mixtures, hydrates, deuterated compounds, solvates, prodrugs, enantiomers, diastereoisomers and tautomers of the hydroxamic acid compound. The invention also relates to the use thereof in the preparation of a preparation responsive to histone deacetylase in medicine, and the use thereof in the preparation of medicine for treating and preventing parasitic infections.

The present application provides compositions, excipient systems, methods, and dispensers for delivery of active pharmaceutical ingredients (APIs) selected from aceclidine and lifitegrast, or a derivative, analogue, pharmaceutically acceptable salt, free base form, racemic mixture, or diastereomer or enantiomer thereof. In one example, a composition is provided comprising an active pharmaceutical ingredient; an alcohol selected from phenethyl alcohol, ethanol, isopropanol, glycerol, propylene glycol, polyethylene glycol, n-butanol, and combinations thereof; and a semifluorinated alkane compound. In another example, an excipient system is provided comprising an alcohol and a semi-fluorinated alkane compound. Dispensers containing the compositions are also provided and include glass and polyethylene terephthalate dispensers or containers. Methods of using the compositions are also provided and include a method for treating a condition in a subject comprising administering the compositions to the subject.

The present invention relates to novel compounds of formula (I), or detectably labeled compounds, stereoisomers, racemic mixtures, pharmaceutically acceptable salts, hydrates, or solvates thereof, which can be used to image and quantify alpha-synuclein aggregates. Furthermore, the compounds can be used to diagnose diseases, disorders, or conditions associated with alpha-synuclein aggregates (e.g., Parkinson's disease or multiple system atrophy (MSA)), determine a predisposition to such diseases, disorders, or conditions, prognose such diseases, disorders, or conditions, monitor the progression of such diseases, disorders, or conditions in patients suffering from such diseases, disorders, or conditions, monitor the progression of such diseases, disorders, or conditions, and predict the responsiveness of patients suffering from such diseases, disorders, or conditions to treatment.

This invention relates to novel compounds of formula (I) or detectable labeled compounds thereof, stereoisomers, racemic mixtures, pharmaceutically acceptable salts, hydrates, or solvates, which can be used for imaging and determining the amount of α-synuclein aggregates. Furthermore, the compounds can be used to diagnose diseases, conditions, or abnormalities associated with α-synuclein aggregates (including, but not limited to, Lewy bodies and / or Lewy neurites) (e.g., Parkinson's disease), determine susceptibility to said diseases, conditions, or abnormalities, predict the prognosis of said diseases, conditions, or abnormalities, monitor disease progression in patients with said diseases, conditions, or abnormalities, monitor the progression of said diseases, conditions, or abnormalities, and predict the responsiveness of patients with said diseases, conditions, or abnormalities to their treatment.

The present invention relates to a pillararene, a solid support, a composition, a process for removing perfluorinated acids from an aqueous stream and the use of the pillararene. The pillararene comprises n monomers independently selected from the group consisting of monomers of formula (I), or a stereoisomer, tautomer, raceme, hydrate, N-oxide or solvate thereof.

This invention belongs to the field of pharmaceutical technology, specifically relating to the use of tropic acid and its derivatives in the preparation of drugs for treating immune and inflammation-related diseases, and to drugs for treating immune and inflammation-related diseases. The tropic acid and its derivatives are compounds of formulas I-IV or pharmaceutically acceptable salts thereof, as well as solvent compounds, enantiomers, diastereomers, tautomers, or mixtures thereof in any proportion, including racemic mixtures, of the compounds of formulas I-IV or pharmaceutically acceptable salts thereof. Animal studies show that tropic acid and its derivatives have broad-spectrum immunomodulatory, anti-inflammatory, and analgesic effects, significantly improving pathological indicators in numerous animal models of immune and inflammation-related diseases. They can regulate abnormal immune responses towards normalcy and exert good anti-inflammatory and analgesic effects, making them suitable for patients with different disease degrees and types of immune and inflammation-related diseases, and thus have industrial applications.

The invention relates to the field of medicine, in particular to a PRMT5 inhibitor as well as a preparation method and application thereof, and the PRMT5 inhibitor is a compound shown as a formula (I), an enantiomer, a diastereoisomer, a raceme, a solvate, a hydrate, a polymorph, a prodrug, an isotope variant or a pharmaceutically acceptable salt thereof. The compound provided by the invention has better activity, selectivity, pharmacokinetic characteristics and safety or a wider therapeutic window.

The present invention relates to novel compounds of formula (I), or detectably labeled compounds, stereoisomers, racemic mixtures, pharmaceutically acceptable salts, hydrates, or solvates thereof, which can be used to image and quantify alpha-synuclein aggregates. Furthermore, the compounds can be used to diagnose diseases, disorders, or conditions associated with alpha-synuclein aggregates (e.g., Parkinson's disease or multiple system atrophy (MSA)), determine a predisposition to such diseases, disorders, or conditions, prognose such diseases, disorders, or conditions, monitor the progression of such diseases, disorders, or conditions in patients suffering from such diseases, disorders, or conditions, monitor the progression of such diseases, disorders, or conditions, and predict the responsiveness of patients suffering from such diseases, disorders, or conditions to treatment.