52 results about "Chromane" patented technology

A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.

To provide a protective agent for a retinal nerve or an optic nerve, which exhibits its efficacy through a mechanism that is different from that for a conventional therapeutic agent and can be ingested over a long period. [MEANS FOR SOLVING PROBLEMS] Disclosed is protective agent for a retinal nerve or an optic nerve, which comprises a compound having an inhibitory activity on an aldose reductase, such as a compound represented by the general formula below, as an active ingredient. Preferably, the compound is (2S,4S)-6- fluoro-2',5'-dioxospiro[chromane-4,4'-imidazolidine]-2- carboxamide. wherein X represents a halogen atom ora hydrogen atom; R and R independently represent a hydrogen atom or a C1-6 alkyl group which may be substituted, or R and R together with a nitrogen atom located at the base of R and R or additionally together with other nitrogen atom or an oxygen atom may form a 5- to 6-membered heterocyclic ring.

Compounds of formula I or pharmaceutically acceptable salts thereof are provided:wherein each of R1, R2, R3, R4, y, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.

The invention relates to a preparation process of ethyl chromane-4-formate. The preparation process is characterized by comprising the following steps of: carrying out Friedel-Crafts acylation reaction and cyclization, addition reaction, hydrolysis reaction and esterification reaction, wherein, in the Friedel-Crafts acylation reaction and cyclization, the Friedel-Crafts acylation reaction is carried out in the presence of anhydrous aluminium trichloride by using a compound of formula 1 and 3-chloropropionylchloride as initial raw materials, then carrying out cyclization on an obtained product and 10% NaOH to obtain a compound of formula 2; in the addition reaction, the addition reaction is carried out on the compound of formula 2 and trimethylsilyl cyanide in the presence of zinc iodide to obtain a compound of formula 3; in the hydrolysis reaction, the compound of formula 3 is hydrolyzed under the conditions of stannous chloride dihydrate, concentrated hydrochloric acid and acetic acid to obtain a compound of formula 4; and in the esterification reaction, the compound of formula 4 is esterified in the presence of concentrated sulfuric acid to obtain a compound of formula 5. According to the preparation process, expensive trifluoromethanesulfonic acid is replaced with cheap anhydrous aluminium trichloride in the Friedel-Crafts acylation step, and the yield is improved, so that the cost of preparing the compound is greatly reduced, and the high-quality product is obtained; and compared with the traditional method, the preparation process has obvious advantages.

The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases or conditions associated with and / or mediated by β-secretase activity, hydrolysis of a β-secretase site of a β-amyloid precursor protein, and / or β-amyloid protein accumulation, including a pharmaceutical composition for preventing or treating diseases including, but not limited to, Glaucoma, MCI (Mild cognitive impairment) or Alzheimer's disease, especially, Alzheimer's disease.

The present invention relates to a synthesis of chromanones or chromanes in a stereospecific matter in view of the 2-position in the chromanone or chromane ring. It has been found that this synthesis is particularly possible in the presence of a chiral compound of a specific type and of at least one Bransted acid or in the presence a specific chiral compound having a Bransted acid functional group in the molecule.

The invention relates to the technical field of medicine, mainly relating to the applications of chromane compound HEF-05 in preparing intestinal canal smooth muscle spasmolytic and in serving as potassium ion channel opener; the invention further comprises a preparation method of the inspected object HEF-05 in the invention. In animal in vitro experiment, HEF-05 can not only relax the amplitude and the tension of spontaneous activities of rabbit in vitro intestinal canal smooth muscle, but also relax the shrinkage of small intestine smooth muscle caused by acetylcholine chloride, barium chloride and potassium chloride. In addition, preliminary study on the relaxation mechanism of chromane compound HEF-05 proves that the relaxation effect of chromane compound HEF-05 is inhibited after the small intestine smooth muscle is incubated by ATP-sensitive potassium channel blocking agent Glibenclamide, therefore, HEF-05 can be used for preparing spasmolytic which is used for treating intestinal canal smooth muscle spasm, and can also be served as potassium ion channel opener.

The present invention relates to monobactam compounds of Formula I:and pharmaceutically acceptable salts thereof. The present invention also relates to compositions which comprise a monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.

Methods of preparing compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R2, R3, R4, x, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.

Disclosed are processes for producing chromane compounds, preferably chroman-2-yl acetic acid compounds and 6-amino-chroman-2-yl acetic acid esters which are intermediates for producing platelet aggregation inhibitors and / or are themselves potent platelet aggregation inhibitors.

The present invention relates to a synthesis of chromanone or chromane in a stereo-specific matter in view of the 2-position in the chromanone or chromane ring. It has been found that this synthesis is particularly possible in the presence of a chiral compound of formula of a specific type and of at least one phenol or thiophenol.

The invention discloses a chromanone compound, and a preparation method and application thereof. The chromanone compound is Tobchromanone A and is separated from aromatic tobacco; the molecular formula is C14H16O4; and the structure is shown in the specification. The preparation method of the chromanone compound comprises the following steps: crushing an aromatic tobacco sample, performing ultrasonic extraction with 95% ethanol for 3-5 times, merging the extracting solutions, and concentrating under reduced pressure to obtain an extract; and performing primary separation on the extract through silica gel column chromatography, and then performing further separation through high pressure liquid chromatography to obtain the required compound, namely the Tobchromanone A. The compound has a better cytotoxic effect on human neuroblastoma cells (SHSY5Y) with the IC50 value up to 2.8 mu M, and indicates a medium cytotoxic effect on other measured cell strains.