Containing six-membered aromatic rings (C07C59/64)

ethod for alcoxyphenol and alcoxyhydroxybenzaldehyde production // 2628525
FIELD: chemistry.SUBSTANCE: method for alkoxyphenol production comprises O-alkylation of at least one hydroxyphenol to form at least one alkoxyphenol, at that, the said reaction is carried out using an O-alkylating agent, an aqueous solvent containing a Bronsted base and an organic solvent with a base/O-alkylating agent ration in the range of 0.5 to 1.5 moles of base per mole of O-alkylating agent, with an O-alkylating agent/hydroxyphenol ratio in the range of 0.5 to 2 moles of O-alkylating agent per mole of hydroxyphenol and with an organic solvent/hydroxyphenol ratio of less than 280 ml, preferably in the range of 10 to 250 ml and more preferably in the range of 50 to 150 ml of an organic solvent per mole of hydroxyphenol. One of the versions of the alkoxyhydroxybenzaldehyde production method comprises preparation of alkoxyphenol from hydroxyphenol by the foregoing method and a reaction of the aldehyde group addition to the resulting alkoxyphenol to obtain the corresponding alkoxyhydroxybenzaldehyde, preferably by condensation reaction between alkoxyphenol and glyoxylic acid, followed by oxidation of the resulting compound.EFFECT: proposed method for alkoxyphenol production allows the desired product to be obtained in good yield and high purity with high conversion of initial hydroxyphenol.11 cl, 3 dwg, 7 ex

Co-crystalline forms of tramadol and nsaid // 2599717
FIELD: chemistry.SUBSTANCE: invention relates to novel co-crystalline form of tramadol in form of free base and naproxen, or co-crystalline form of solvate methanol containing tramadol and naproxen, wherein molecular ratio of tramadol to naproxen makes 1:2. Co-crystalline form can be applied to pain treatment, preferably, acute pain, chronic pain, neuropathic pain, heavy or moderate pain, allodynia, hyperalgesia, or cancer pain, including diabetic neuropathy or diabetic peripheral neuropathy and osteoarthritis, fibromyalgia; rheumatoid arthritis, ankylosing spondylitis, scapulohumeral periarthritis, or ischialgia. Co-crystalline form mainly contains enantiomeric forms of naproxen and tramadol, in particular (S)-naproxen or (R)-naproxen and (-)-tramadol or (+)-tramadol. Proposed co-crystalline forms are characterised by X-ray powder diffraction data, as well as by indices of monoclinic elementary cell and indices of endometric acute peak, corresponding to melting point, which has start at 82-84C.EFFECT: invention also relates to method for producing co-crystalline form and pharmaceutical composition based thereon.12 cl, 11 dwg, 5 tbl, 4 ex

Tetrasubstituted benzenes // 2527177
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to novel compounds of formula III or to its pharmaceutically acceptable salts, in which: R1 and R2 are independently selected from group, consisting of: (a) H, (b) (C2-C6)alkyl, (c) C1-C6 alkyl, interrupted by one or more groups -O-, (d) (C0-C3)alkyl-(C3-C7)cycloalkyl and (e) (CH2)nQ, where n=1-2 and where Q stands for aromatic ring system, which has from 5 to 6 ring atoms C, and Q can be independently substituted with groups up to 3 in number, selected from halogen, on condition that R1 and R2 simultaneously do not stand for H, and each alkyl of R1 and R2 can be independently substituted with one or more groups, selected from group, consisting of halogen, hydroxy, cyano, CF3 or C1-C4 alkyl, or R1 and R2 together with carbon, to which they are attached, form 3-7-member cycloalkyl or 6-member heterocycloalkyl ring, including one oxygen atom and which in case of necessity carries C1-C4 alkyl substituent, or R1 and R2 together with carbon, to which they are connected, form 3-7-member cycloalkyl ring, substituted with R20 and R21, and R20 and R21 together with carbon or carbons, to which they are connected, form 3-7-member cycloalkyl ring; R6 stands for C1-C6 alkyl; each R7 independently stands for C1-C6 alkyl; Y stands for -O-; R4 is selected from group, consisting of: (a) (C0-C3)alkyl-(C3-C7)cycloalkyl, (b) trifluoroethyl, and (c) trifluoropropyl; Z stands for phenyl or bicyclic ring system, which has 9 ring atoms, independently selected from C, N, O and S, on condition that not more than 3 ring atoms in any single ring differs from C, and said ring system can carry to 3 substituents, independently selected from group, consisting of R6, CF3 and SR6; and R5 is selected from group, consisting of NO2, NH2, F, Cl, Br, CN, SR6, S(O)2N(R7)2 and (C1-C4)alkyl, and each alkyl can be independently substituted with one or more halogens or CF3. Invention also relates to pharmaceutical composition for treatment of neurodegenerative disorder or improvement of cognitive function, containing therapeutically effective quantity of said compound; as well as to method of treatment of neurodegenerative disorder, for instance Alzheimer's disease, or improvement of cognitive function.EFFECT: compounds act as modulators of gamma-secretase.31 cl, 14 tbl, 3147 ex, 1 dwg

ethod for asymmetrical hydrogenation of acrylic acid derivatives, catalysed by transition metals, and novel catalyst system for asymmetrical catalysis with transition metals // 2415127
FIELD: chemistry.SUBSTANCE: invention relates to an improved method for asymmetrical hydrogenation, catalysed by transition metals, acrylic acid derivatives of formula (I), in which R1 denotes H or optionally substituted C1-C20-alkyl, C5-C20-aryl or C5-C20-heteroryl radical, R2 denotes optionally substituted C1-C20-alkyl, C5-C20-aryl or C5-C20-heteroaryl radical, and R3 denotes H or C1-C6-alkyl radical, which involves hydrogenation of compounds of formula (I), optionally in a solvent, in the presence of one or more hydrogen donors, using a catalyst system which contains a transition metal selected from ruthenium, rhodium and iridium and a combination of a chiral phosphoric ligand of formula (II), in which Cn, together with two oxygen atoms and a phosphorus atom, form an optionally substituted ring, having 2-6 carbon atoms, and R4 denotes an optionally substituted alkyl, aryl, alkoxy- or aryloxy-radical or a NR5R6 group in which R5 and R6 can be independently hydrogen or optionally substituted alkyl, aryl, aralkyl or alkaryl radical, or together with a nitrogen atom can form a ring, and an achiral phosphinic ligand of formula (III), in which R is optionally substituted alkyl or aryl radical, to obtain corresponding compounds of formula (IV) in which each R1, R2 and R3 are as described above. Formula (I), Formula (II), Formula P(R)3 (III), Formula (IV).EFFECT: improved method for asymmetrical hydrogenation.20 cl, 3 tbl, 29 ex

Derivatives of carboxylic acid, their pharmaceutically acceptable salts or esters, medicinal agent and pharmaceutical composition based on thereof, their using and methods for treatment and prophylaxis of diseases // 2316537
FIELD: organic chemistry, medicine, pharmacy.SUBSTANCE: invention relates to novel derivatives of carboxylic acid represented by the general formula (I): , their pharmaceutically acceptable salts or esters wherein values Y, L, X, T, Z, M, R1, W and are given in the invention claim. Proposed compounds possess insulin-sensitizing effect and they are double agonists with respect to PPARα and γ, and triple agonists with respect to PPARα, β(δ) and γ. Except for, the invention relates to a medicinal agent and pharmaceutical compositions based on the claimed derivatives of carboxylic acid, to methods for prophylaxis or treatment of diseases, and to using derivatives carboxylic acid for preparing a medicinal agent.EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.56 cl, 2 tbl, 609 ex

Synthesis of oxygen-substituted benzocycloheptenes as valuable intermediate compounds for preparing tissue-selective estrogens // 2310643
FIELD: organic chemistry, chemical technology.SUBSTANCE: invention relates to novel intermediate compounds and inmproved method for synthesis of compound of the formula (C): . Proposed method is based on using inexpensive parent substances and provides synthesis of intermediate compounds with the high yield and high purity degree being without carrying out procedures for chromatographic purification and can be realized in large-scale industry manufacture. Invention relates to improved methods for synthesis of compound of the formula (I): , compound of the formula (II): , compound of the formula (III): , compound of the formula (VIII): , compound of the formula (IX): , and to a reagent consisting of boron tribromide and 2,6-dimethylpyridine. Method is used for a sparing and selective splitting a methyl group in aromatic methyl ethers.EFFECT: improved method of synthesis.12 cl, 8 ex

A method of obtaining a possibly substituted p-hydroxymandelic connections // 2232746
The invention relates to an improved method for producing a p-hydroxymandelic compounds by condensation in the water, in the presence of an alkaline agent, an aromatic compound containing at least one hydroxyl group and having a free parapolitica, with Glyoxylic acid

Bicyclic aromatic compounds and compositions on their basis // 2188190
The invention relates to new bicyclic aromatic compounds of General formula (I) having the ability to bind RXRand pharmaceutical compositions based on them, which can be used in medicine, veterinary medicine and in cosmetics

The way to obtain 2,2-dimethyl-5-(2,5-dimethylphenoxy)- pentanol acid // 2056403
The invention relates to a new process for the preparation of 2,2-dimethyl-5-(2,5-dimethylphenoxy)-pentanol acid of the formula (I)OCOOH(I) This connection is used for regulating the level of blood lipids