454 results about "Racemic mixture" patented technology

The invention provides compounds of Formula I: wherein Azabicyclo is W is a six-membered heterocyclic ring system having 1–2 nitrogen atoms or a 10-membered bicyclic-six-six-fused-ring system having up to two nitrogen atoms within either or both rings, provided that no nitrogen is at a bridge of the bicyclic-six-six-fused-ring system, and further having 1–2 substitutents independently selected from R3.These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat diseases or conditions in which α7 is known to be involved.

The present invention provides compounds and amyloid probes thereof that allow for an antemortem method of diagnosing AD and quantitating the extent or progression of amyloid deposits (plaques) by in vivo imaging of amyloid and / or amyloid deposits in the regions of the brain. Preferably, an amyloid probe of the invention can cross the blood-brain barrier and distinguish AD brain from normal brain. An amyloid probe can be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits. Amyloid probes of the invention can also be used to detect and quantitate amyloid deposits in diseases including, without limitation, Down's syndrome, familial AD and homozygotes for the apolipoprotein E4 allele. In one aspect, the compounds may be used in the treatment or prophylaxis of diseases that include, without limitation, AD and type 2 diabetes mellitus. The compounds and amyloid probes of the invention include analogs, salts, pharmaceutical compositions, derivatives, prodrugs, racemic mixtures or tautomeric forms thereof.

The present invention provides an α-2A / α-1A selective agonist that includes a compound represented by Structure 1 or a pharmaceutically acceptable salt, ester, amide, sterioisomer or racemic mixture thereof. The present invention further provides a pharmaceutical composition that contains a pharmaceutical carrier and a therapeutically effective amount of an α-2A / α-1A selective agonist that includes a compound represented by Structure 1 or a pharmaceutically acceptable salt, ester, amide, sterioisomer or racemic mixture thereof.

Methods are disclosed utilizing the optically pure (-) isomer of amlodipine. This compound is a potent drug for the treatment of hypertension while avoiding the concomitant liability of adverse effects associated with the racemic mixture of amlodipine. The (-) isomer of amlodipine is also useful for the treatment of angina and such other conditions as may be related to the activity of (-) amlodipine as a calcium channel antagonist such as cerebral ischemia, cerebral disorders, arrhythmias, cardiac hypertrophy, coronary vasospasm, myocardial infarction, renal impairment and acute renal failure, without the concomitant liability of adverse effects associated with the racemic mixture of amlodipine.

Certain benzopyran antiestrogens are disclosed for treating estrogen sensitive diseases such as breast cancer. Prodrug forms provide ease of manufacturing, good shelf life, and bioavailability, and preferred stereoisomers are shown to be more effective than racemic mixtures.

A toner including a colorant and a binder resin is provided. The binder resin includes a first resin comprising a block X comprising a resin comprising a racemic mixture of optically active monomers of a D-form compound and an L-form compound, and a block Y comprising another resin. The weight ratio of the D-form compound to the L-form compound is from 48 / 52 to 52 / 48, and the weight ratio of the block Y to the block X is from 1 / 3 to 3 / 1. The toner is obtained by dispersing or emulsifying a toner constituent liquid, in which the colorant and the binder resin are dissolved or dispersed in an organic solvent, in an aqueous medium.

A composition for use in making commercial food and skin products comprising S-equol or mixtures, including both a non-racemic mixture and a racemic mixture, of S-equol and R-equol. The composition can be used to make articles of commerce such as food supplements, pharmaceuticals, and medicaments. The compositions are useful in a method of delivering S-equol to a mammal to prevent or treat a disease or associated condition, including hormone-dependent diseases or conditions such as cardiovascular disease, lipid disorder, osteopenia, osteoporosis, liver disease, and acute ovarian estrogen deficiency. The S-equol enantiomer can be produced in a biological synthesis from the metabolism of an isoflavone by an organism.

The invention provides compounds of Formula I: wherein Azabicyclo is W0 is a bicyclic moiety and is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals in which α7 is known to be involved.

Methods and compositions are disclosed utilizing the optically pure (+) isomer of zopiclone. This compound is a potent drug for the treatment of sleep disorders, such as insomnia, and convulsive disorders, such as epilepsy. Similarly, these novel compositions and methods are useful for the treatment of sleep disorders and convulsive disorders while avoiding the concomitant liability of adverse effects associated with the racemic mixture of zopiclone. The optically pure (+) isomer of zopiclone is also useful for treating disorders that are affected by the binding of agonists to central nervous system or peripheral benzodiazepine receptors. Also described are methods and compositions for treating disorders that are affected by binding of agonists to central nervous system or peripheral benzodiazepine receptors while avoiding the adverse effects associated with the administration of the racemic mixture of zopiclone.

Provided herein are optically active compounds of the formulae (ii); and (III) and pharmaceutical compositions thereof. Also provided herein are processes of making these compounds and resolving the racemic mixture or the enrichment of same with in one of its enantiomers to provide (R)- and (S)-1-(3-(3-N,N-dimethylaminocarbonyl)phenoxyl-4-nitrophenyl)-1-ethyl-N,N'-bis(ethylene)phosphoramidate, andmethods of treating cancer comprising administering such compounds.

The present invention relates to 5-hydroxy-indole-3-carboxylate derivatives of formula I, or racemic mixture or optical isomers or pharmaceutically acceptable salts and / or hydrates thereof,wherein: substituents R1, R2, Z, X and Y are as defined in the description. The compounds of formula I can be useful for preparation of medicament for treatment and / or prophylaxis of virus infections, especially for preparation of medicament for anti-HBV (Hepatitis B virus) and anti-HIV (Human immunodeficiency virus).

The invention relates to peptides of general formula (I):R1-AA-R2   (I)which can regulate neuronal exocytosis, their stereoisomers and racemic or non-racemic mixtures thereof, and the cosmetically or pharmaceutically acceptable salts thereof, wherein AA is a sequence of 3 to 40 adjacent amino acids contained in the amino acid sequence of the SNAP-25 protein, R1 is selected from the group consisting of H or alkyl, aryl, aralkyl or acyl group; and R2 is selected from the group consisting of amino, hydroxyl or thiol, substituted or non-substituted with aliphatic or cyclic groups, with the condition that when R1 is H or acetyl, R2 is not non-substituted amino, hydroxyl or thiol. The invention also relates to a method of obtaining such peptides, cosmetic or pharmaceutical compositions containing them and their use to treat those conditions requiring neuronal exocytosis regulation, preferably for treating the skin.

The invention relates to a novel indoleamine-2,3-dioxygenase (IDO) inhibitor, as well as a preparation method and an application thereof. The inhibitor is compounds of a formula I or pharmaceutically-acceptable salt, solvate, polymorph, enantiomer or racemic mixture thereof, wherein R1 or R2 is independently selected from H, C1-C5 alkyl, halogen and a substituent of a formula II and either of R1 and R2 is the substituent of the formula II; R3 is an aryl group; and n is equal to 0, 1, 2 or 3. Compared with the know IDO inhibitors, the novel IDO inhibitor has significant inhibitory effect on IDO and can be used for treatment of diseases having IDO-mediated tryptophan metabolic pathway pathological features, such as tumors, cancers, Alzheimer's disease, autoimmune diseases, cataract, psychological disorders, depression and / or anxiety. The preparation method of the novel IDO inhibitor has the advantages of being convenient in operation, having mild reaction conditions and reducing solvent consumption and pollution, thereby facilitating industrial production.

One aspect of the present invention relates to a method of preparing a fibrous protein smectic hydrogel by way of a solvent templating process, comprising the steps of pouring an aqueous fibrous protein solution into a container comprising a solvent that is not miscible with water; sealing the container and allowing it to age at about room temperature; and collecting the resulting fibrous protein smectic hydrogel and allowing it to dry. Another aspect of the present invention relates to a method of obtaining predominantly one enantiomer from a racemic mixture, comprising the steps of pouring an aqueous fibrous protein solution into a container comprising a solvent that is not miscible with water; sealing the container and allowing it to age at about room temperature; allowing the enantiomers of racemic mixture to diffuse selectively into the smectic hydrogel in solution; removing the smectic hydrogel from the solution; rinsing predominantly one enantiomer from the surface of the smectic hydrogel; and extracting predominantly one enantiomer from the interior of the smectic hydrogel. The present invention also relates to a smectic hydrogel prepared according to an aforementioned method.

The instant disclosure is directed to a method of producing crystals of a racemic mixture of a 1-substituted-3-pyrrolate. A method of producing crystals of racemic glycopyrrolate in high purity is also disclosed.

The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.

A compound represented by formula I, or a pharmaceutically acceptable salt, solvate, polymorph, enantiomer or racemic mixture thereof, wherein, R1 and R2 are independently hydrogen, -OH, alkyl, -CF3, -OCHF2, -OCF3 or halogen,R3 is cycloalkyl, -OCH2CF3, -OCH2CHF2, -OCH2CH2F or -OCH2CH3,R4 is hydrogen, -OH, -O aryl, -OCH2 aryl, alkyl, cycloalkyl, -CF3, -OCHF2, -OCF3, -OCH2CF3, -OCH2CHF2, -OCH2CH2F or halogen,A is -CX1X2, wherein X1 and X2 are independently H, F and Cl, and when both X1 and X2 are H, R3 is other than -OCH2CH3. The compound has an activity of inhibitors of sodium-dependent glucose transport protein. A method for preparing the compound. A pharmaceutical composition comprising the compound. A use of the compound and pharmaceutical composition thereof in the preparation of medicaments of SGLT2 inhibitors for treating a disease of interest.

A bioengineered synthesis scheme for the production of L-1,2,4-butanetriol, D-1,2,4-butanetriol and racemic mixtures thereof from a carbon source is provided. Methods of producing L-1,2,4-butanetriol, D-1,2,4-butanetriol and racemic mixtures thereof are also provided. Methods are also provided for converting D-1,2,4-butanetriol and L-1,2,4,-butanetriol to D,L-1,2,4-butanetriol trinitrate.

One aspect of the present invention relates to a method of preparing a fibrous protein smectic hydrogel by way of a solvent templating process, comprising the steps of pouring an aqueous fibrous protein solution into a container comprising a solvent that is not miscible with water; sealing the container and allowing it to age at about room temperature; and collecting the resulting fibrous protein smectic hydrogel and allowing it to dry. Another aspect of the present invention relates to a method of obtaining predominantly one enantiomer from a racemic mixture, comprising the steps of pouring an aqueous fibrous protein solution into a container comprising a solvent that is not miscible with water; sealing the container and allowing it to age at about room temperature; allowing the enantiomers of racemic mixture to diffuse selectively into the smectic hydrogel in solution; removing the smectic hydrogel from the solution; rinsing predominantly one enantiomer from the surface of the smectic hydrogel; and extracting predominantly one enantiomer from the interior of the smectic hydrogel. The present invention also relates to a smectic hydrogel prepared according to an aforementioned method.

Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas 1 or 2, as described herein. The compounds of Formulas 1 and 2 are also useful for treating pain, and treating drug addiction, nicotine addiction, and / or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.

The invention is directed to a method of preventing or ameliorating a neuropsychiatric or neurodegenerative disease or disorder in a subject. The method includes administering a composition comprising equol in an amount sufficient to prevent or ameliorate the neuropsychiatric or neurodegenerative disease or disorder. The equol may be a racemic mixture of R-equol and S-equol. The equol may be enantiomerically enriched with R-equol or enantiomerically enriched with Sequol.

The invention relates to a novel method for the resolution of the racemic mixture of compound (R,S)-2-amino-6-propylamino-4,5,6,7-tetrahydrobenzothiazole, or the enrichment of same with in one of its enantiomers, and to intermediate compounds which can be used to perform said method.

A method of treating Parkinson's disease by administering the racemic mixture of D,L-DOPA in combination with both peripheral amino acid decarboxylase and catechol, O-methyltransferase (COMT) inhibitors in pharmaceutically acceptable salts forms and effective doses for the treatment of Parkinson's disease. Alternatively, D-DOPA is administered in combination with both peripheral amino acid decarboxylase and catechol, O-methyltransferase (COMT) inhibitors in pharmaceutically acceptable salts forms and effective doses for the treatment of Parkinson's disease.

The invention belongs to the technical field of medicaments and in particular relates to cardiac glycoside compounds with a general formula (I), as well as derivatives, stereoisomers, a racemic mixture or a non-racemic mixture of the stereoisomers and pharmaceutically acceptable acid addition salts or solvates, wherein R1 is CH3, CHO or CH2OH; R2 is H or a linear saccharide chain or a branched saccharide chain, the linear saccharide chain or the branched saccharide chain is formed by saccharides; and these acids comprise inorganic acids like hydrochloric acid, sulfuric acid, hydrobromic acid, phosphoric acid, nitric acid, carbonic acid and the like as well as organic acids like methanoic acid, acetic acid, succinic acid, citric acid, lactic acid, fumaric acid, tartaric acid, benzoic acid, p-methyl-benzenesulfonic acid, methylsulphonic acid, naphthalenesulfonic acid, gluconic acid and the like. The cardiac glycoside compounds can be obtained by separation from plants, in particular Streptocaulon plant juventas or Streptocaulon griffithii, by using multiple conventional separating means or obtained through synthesis, semisynthesis or bioconversion means. These compounds have excellent inhibiting and treatment effects on multiple tumor cells.

The invention provides compounds of Formula I: 1 wherein Azabicyclo is 2 W is a six-membered heterocyclic ring system having 1-2 nitrogen atoms or a 10-membered bicyclic-six-six-fused-ring system having up to two nitrogen atoms within either or both rings, provided that no nitrogen is at a bridge of the bicyclic-six-six-fused-ring system, and further having 1-2 substitutents independently selected from R.sub.3. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat diseases or conditions in which .alpha.7 is known to be involved.

This invention is directed to pharmaceutical compositions for topical administration to a mammal, wherein the pharmaceutical compositions comprise a spiro-oxindole compound, as an enantiomer, a racemate or a non-racemic mixture, or a pharmaceutically acceptable salt thereof. These pharmaceutical compositions are useful for the treatment and / or prevention of sodium channel-mediated diseases or conditions.

The invention relates to a novel non-catalytic enantioselective resolution process for the separation of enantiomer of arylpropionic acid drugs from the racemic mixture, which comprises dissolving the racemic mixture of the said drug an organic solvent, reacting this solution with an aqueous phase containing an ionic surfactant with or without a suitable co-surfactant, and an electrolyte in microemulsion / micellar / biphasic medium, reacting this mixture with an appropriate chiral amine at a temperature in the range of 0 to 70 degrees Celsius to obtain a diastereomeric salt, acid hydrolysing the diastereomeric salt to result in the pure enantiomer of the drug which is extracted by known methods.