85 results about "Racemic mixture" patented technology

Compositions for inducing and maintaining a state of flow in a subject include optically pure S-beta-hydroxybutyrate or non-racemic mixtures enriched with the S-enantiomer. The S-beta-hydroxybutyrate enantiomer modulates the effect of ketone bodies in the subject and controls the rate at which ketosis is achieved. 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. Beta-hydroxybutyrate salts are more slowly absorbed and utilized by the body and can provide one or more electrolytes. Compositions for controlling ketone body level 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.

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.

Compositions for inducing and maintaining a state of flow in a subject include optically pure S-beta-hydroxybutyrate or non-racemic mixtures enriched with the S-enantiomer. The S-beta-hydroxybutyrate enantiomer modulates the effect of ketone bodies in the subject and controls the rate at which ketosis is achieved. 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. Beta-hydroxybutyrate salts are more slowly absorbed and utilized by the body and can provide one or more electrolytes. Compositions for controlling ketone body level 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 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 discloses a borneol derivative and application thereof in pharmacy. The borneol derivative is a compound shown as a general formula (I) and a general formula (II), and pharmaceutically acceptable salt and / or hydrate and deuterated compound thereof, and / or racemic mixture, hydrate, solvate, prodrug, enantiomer, diastereoisomer and tautomer thereof. Experimental results show that the borneol derivative can significantly reduce the epileptic seizure grade and improve the epileptic seizure latency, shows a good anti-epileptic effect, and has a good development prospect. # imgabs0 #

This disclosure relates to heterogeneous nuclear ribonucleic acid A2B1 (hnRNPA2B1) agonist compounds and their use in combination with chemotherapeutic agents for antitumor treatment. Specifically, this disclosure relates to fused ring compounds of formula (I), their cis-trans isomers, their enantiomers, their diastereomers, their racemic mixtures, their solvates, their hydrates, or their pharmaceutically acceptable salts or prodrugs thereof, compositions comprising any of the former, and products thereof, as well as the use of the aforementioned substances as hnRNPA2B1 agonists in the preparation of products for the prevention and / or treatment of tumors, said products may further comprise or be used in combination with chemotherapeutic agents. This disclosure has broad application prospects for the prevention and treatment of tumors.

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.

The present invention relates to a method for purifying a compound of formula (IV-F), or a stereoisomer, racemic mixture, pharmaceutically acceptable salt, hydrate or solvate thereof, comprising a C1-4 alkyl sulfonate as a leaving group. The compounds of formula (IV-F) can be used as precursors to 18F-labeled agents for imaging and determining the amount of alpha-synuclein aggregates. The 18F-labelled agents may be used to diagnose a disease, disorder, or abnormality associated with alpha-synuclein aggregates (e.g., multi-system atrophy (MSA)), determine the susceptibility of such a disease, disorder, or abnormality, predict the prognosis of such a disease, disorder, or abnormality, monitor disease evolution in a patient suffering from such a disease, disorder, or abnormality, and, for example, to diagnose a disease, disorder, or abnormality associated with alpha-synuclein aggregates. The progression of such diseases, disorders or abnormalities is monitored, as well as the response of patients suffering from such diseases, disorders or abnormalities to their treatment is predicted. # imgabs0 #

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.

The present invention discloses a class of 4-(1H)-imidazole derivatives represented by the following formula (I), their pharmaceutically acceptable salts, racemic mixtures, enantiomers, optical isomers and tautomers, as well as pharmaceutical compositions containing them, and their use as α2-adrenergic receptor agonists, especially as α 2A -agonists and their methods of use. Compared with the prior art, the compounds of the present invention show more potent agonist activity and higher selectivity for α 2A -AR, superior to the positive drug dexmedetomidine; and at the same time have a potent in vivo sedative effect. #imgabs0#

This application encompasses an enantiomerically pure compound of formula (R)-I or a salt and / or solvate thereof. Also included are compositions of an enantiomerically pure compound of formula (R)-I, and methods of using a compound of formula (R)-I or a composition thereof for treating, for example, diseases, disorders or medical conditions for which psychotherapy is beneficial. The application also encompasses a composition comprising a non-racemic mixture of a compound of formula (R)-I or a salt and / or solvate thereof, and a compound of (S)-I or a salt and / or solvate thereof, wherein the (R)-I or a salt and / or solvate thereof is present in the composition in a greater amount, expressed in enantiomeric equivalents, compared to the (S)-I or a salt and / or solvate thereof, and the use thereof. Further included is a process for preparing a compound of formula (R)-I or (S)-I. JPEG2025524763000070.jpg5277 JPEG2025524763000071.jpg72155

The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formulawhereinAr1 is phenyl or a five or six membered heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O−);R1 is lower alkyl, halogen, cyano or cycloalkyl;Ar2 is a five or six membered heteroaryl group, containing one, two, three or four heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O−), or is benzo[b]thiophenyl;R2 is hydrogen, lower alkyl, halogen, cyano, lower alkyl substituted by hydroxyl, lower alkyl substituted by halogen, lower alkyl substituted by amino, lower alkyl substituted by alkoxy, lower alkyl substituted by amide, or is cycloalkyl;X is CH or N;n is 1 or 2;m is 1 or 2;as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and / or optical isomer and / or stereoisomer thereofThe compounds may be used in the treatment of CNS diseases related to positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, neurodegenerative disease, sleep disturbances, chronic fatigue syndrome, stiffness, inflammatory disease, asthma, Huntington's disease, ADHD, amyotrophic lateral sclerosis, epilepsy, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems.

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 application discloses a kind of 5-amino-1-alkyl-1H-1, 2, 3-triazole-4-formamide compounds with the structure general formula shown in formula (1), its pharmaceutically acceptable salt, or its racemic mixture, hydrate, solvate, prodrug, enantiomer, diastereoisomer, tautomer.The application also discloses a pharmaceutical composition containing the compound of formula (1), and the application of the compound of formula (1), its pharmaceutically acceptable salt, or its racemic mixture, hydrate, solvate, prodrug, enantiomer, diastereoisomer, tautomer, or the pharmaceutical composition in preparing medicaments for treating diseases responsive to the regulation of ion channel function.

The present application includes an enantiomerically pure compound of Formula (R)-I or a salt and / or solvate thereofAlso included are compositions of the enantiomerically pure compound of Formula (R)-I as well as methods of using the compound of Formula (R)-I or composition thereof for treating, for example, disease, disorder or condition that benefits from psychotherapy.The present application also includes a composition comprising a non-racemic mixture a compound of Formula (R)-I, or a salt and / or solvate thereof, and (S)-I, or a salt and / or solvate thereof:wherein (R)-I, or a salt and / or solvate thereof, is present in the composition in a greater amount by enantiomeric equivalents, relative to (S)-I, or a salt and / or solvate thereof and uses thereof.Further included are process preparing a compound of Formula (R)-I or (S)-I.

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 invention discloses a 2,4-dianilinopyrimidine derivative represented by the general formula I or its optical isomer, enantiomer, diastereomer, racemate or racemic mixture, or its pharmaceutically acceptable salt or ester: Such compounds can release the signaling molecule NO while maintaining the FAK kinase inhibitory activity, ensuring the synergistic anti-tumor proliferation, invasion and metastasis effects of the FAK inhibitor and NO. In addition, the synergistic mechanism between the FAK inhibitor and NO is further explored.

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 present invention relates to methods and uses for controlling herbicide resistant or tolerant weed species by applying the herbicidal compound (±)-2-exo-(2-Methylbenzyloxy)-1-methyl-4-isopropyl-7-oxabicyclo[2.2.1]heptane, any of its individual enantiomers or any non-racemic mixture thereof. The methods and uses are particularly suitable for the protection of crops. The invention also relates to specific herbicidal compositions comprising said herbicidal compound.

This invention provides a method for separating optical isomers from racemic mixtures via electrodialysis. Specifically, this invention applies electrodialysis technology to enzyme resolution processes, primarily for the separation of products after enzyme resolution. Taking the preparation process of D-pantolactone as an example, the key point is to separate D-pantolactone and L-pantolactone from the enzyme resolution solution using electrodialysis, replacing existing organic solvent extraction methods. The process is simple and easy to implement, yields high-purity D-pantolactone, significantly reduces the amount of organic solvent used, lowers production costs, is environmentally friendly, and can greatly improve the working environment and operational safety. The method provided by this invention has great application potential in enzyme resolution processes.

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.