Heterocyclic tetracarbonyl

 

(57) Abstract:

The invention relates to new heterocyclic tetracarbonyl General formula I

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where X = -communication,

< / BR>
Connections can be used to obtain polyhexamethylene - fluorophores, bifluorophors besed, trifluoroprop. Such polyhexamethylene promising for use as active media of liquid and solid lasers, scintillators, especially for indication of hard radiation, for the transformation of shortwave radiation in the long wavelength in the transmission of information through fiber-optic communication lines, to increase the power of solar panels for protection of securities, for the manufacture of billboards. table 2.

The invention relates to the field of production of new tetranitride heterocyclic tetracosanoic acids, which can be used to obtain not previously described polyhexamethylene - fluorophores, bifluorophors besed, trifluoroprop. Such polyhexamethylene promising for use as active media of liquid and solid lasers, scintillators, especially for indication of hard radiation, for the transformation of short-wave radiation long-wave when pretendig securities, for the manufacture of billboards, etc.

You know the connection - pyromellitate, which together with nesnesinin the rhodamine is used to obtain fluorescent polyhexamethylene (Sealing C. A., Feofanov B. N., Lambs N.N. and other Polyhexamethylene based heterocyclic diamines. //Polymer sciense ser. Conn. B. 1988, T. 30, 4. C. 286-291).

The resulting polihexanide has the following characteristics: band radiation of 532 nm upon excitation in the band 312 nm.

The problem solved by the present invention is the obtaining of new heterocyclic tetracarbonyl.

Come heterocyclic tetracarbonyl General formula:

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where X = -communication,

< / BR>
The claimed compounds include 2-(3,4-dicyanovinyl)-3-phenyl-6,7-inoxidizability (I):

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2-[4-(3,4-dicyanobenzene)phenyl] -3-phenyl-6,7-inoxidizability (II):

< / BR>
These compounds obtained by condensation reaction of 4,5-diaminomaleonitrile with the corresponding diketone according to the scheme:

< / BR>
The reaction is carried out in acetic acid medium at boiling point for 1...1.5 hours.

The invention is illustrated by the following examples:

Example 1. In a flask equipped arr g (0.01 mol) of 4-(2-oxo-2-phenylacetyl)phthalonitrile. The reaction mixture was kept at boiling for 1.5 hours. Then the reaction was poured into 100 ml water, the precipitate is filtered off, washed with 50 ml of water and crystallized from DMF.

Get 3.25 g (85.1% of theory) of 2-(3,4-dicyanovinyl)-3-phenyl-6,7-inoxidizability (I) - white crystalline powder with so pl. >300oC.

Found, %: C 75,35; N TO 2.65; N 21,93

Calculated, %: C 75,38; N 2,64; N 21,98 C24H10N6< / BR>
1H-NMR ([N] DMSO): , M. D.: 9,00 (s, 2H), to 8.20 (s, 1H), 8,10 (d, 1H, J=7.9 Hz), 7,95 (d, 1H, J=8 Hz), 7,55 (m, 2H), 7,45 (m, 2H)

Example 2. The reaction is carried out analogously to example 1, except that the reagent (4-(2-oxo-2-phenylacetyl)phthalonitrile) respectively are used equimolar amount of 4-[4-(2-oxo-2-phenylacetyl)phenoxy] phthalonitrile. The conditions and results of the synthesis are given in table. 1.

Example 3. Condensation of 2-(3,4-dicyanovinyl)-3-phenyl-6,7-inoxidizability with rhodamine 123. In a flask equipped with stirrer, thermometer, reflux condenser and capillary to enter argon load of 3.2 g (0.01 mol) of 2-(3,4-dicyanovinyl)-3-phenyl-6,7-inoxidizability, 3.8 g (0.01 mol) of rhodamine 123 and 10 g of phenol. The resulting mixture was slowly heated with stirring Diya ammonia. After the reaction, the reaction mixture was poured into 20 ml of ethanol, and the precipitated precipitate is filtered off, washed with 3 ml of ethanol and dried at T=60oC for 2 hours, then vacuum over P2O5. Get to 9.9 g (95% of theory) of polyhexamethylene.

Found, %: C 75,96; N 4.09 TO; N 10,71

Calculated, %: C 75,99; N 4,07; N a 10.74 (C66H42N8O6)n< / BR>
The IR spectrum of polyhexamethylene no band 2220 cm-1-CN, there is a band at 680 cm-1-C=n

The structural formula of polyhexamethylene derived from 2-(3,4-dicyanovinyl)-3-phenyl-6,7-inoxidizability and rhodamine 123:

< / BR>
Polihexanide obtained 2-(3,4-dicyanovinyl)-3-phenyl-6,7-inoxidizability and rhodamine 123 has the following spectral characteristics: the maximum of a spectrum of radiation - 424 nm at the maxima of the absorption spectrum at 280 and 337 nm.

Example 4. The reaction is carried out analogously to example 3, except that instead of littleitaly I used an equimolar amount of littleitaly II.

The conditions and results of the syntheses and spectral characteristics obtained polyhexamethylene are given in table.2.

Heterocyclic tet is

 

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Imidazopyridine // 2092487
The invention relates to certain imidazoquinolines that selectively bind to the GABA-a receptors

The invention relates to a new series of tetracyclic compounds having two or three nitrogen atoms included in the ring, which have significant anti-allergic and anti-asthma activity, provides methods and compositions for their use, as well as technologies of their production

The invention relates to the field of organic chemistry, to the class of heterocyclic compounds - derivatives of 1,2,3,4-tetrahydroquinoxaline, namely to a new way to obtain previously unknown connections - 2,3-bis-koimeterion - 1,2,3,4-tetrahydroquinoxaline formula

< / BR>
(Ia, b) where R = Br(a), NO2(b) that may find application in medicine as drugs with antimicrobial action

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new biologically active ortho-substituted nitrogen-containing bis-aryl compounds. Invention describes compounds of the formula (I): wherein A1, A2, A3, A4, A5, A6, A7 and A8 mean independently of one another nitrogen atom or -CH and wherein at least one or two (not above) these groups mean nitrogen atom; R(1) means -C(O)OR(9) or -COR(11) wherein R(9) and R(11) mean independently of one another CxH2x-R(14) wherein x has a value 0, 1, 2, 3 or 4 and R(14) means alkyl c 1, 3, 4, 5 or 6 carbon atoms, phenyl or isoxazolyl wherein phenyl and isoxazolyl are not substituted or substituted with 1, 2 or 3 substitutes chosen from the group consisting of F, Cl, Br, J, CF3, OCF3, alkyl with 1, 2, 3 or 4 carbon atoms and alkoxy-group with 1, 2, 3 or 4 carbon atoms; R(2) means hydrogen atom; R(3) means CyH2y-R(16) wherein y has a value 0, 1, 2, 3 or 4but y can't mean 0 if R(16) means -OR(17), and R(16) means alkyl with 1, 2, 3, 4, 5 or 6 carbon atoms, cycloalkyl with 3 carbon atoms, -OR(17), phenyl or pyridyl wherein phenyl and pyridyl are not substituted or substituted with 1, 2 or 3 substitutes chosen from the group consisting of F, Cl, Br, J and alkoxy-group with 1, 2, 3 or 4 carbon atoms; R(17) means hydrogen atom; or R(3) means -CHR(18)R(19) wherein R(18) means alkyl with 1, 2, 3, 4, 5 or 6 carbon atoms and R(19) means -CONH2; R(4) means hydrogen atom; R(30) and R(31) mean hydrogen atom, and their pharmaceutically acceptable salts also. Also, invention describes a pharmaceutical composition showing effect that inhibits K+-channel and comprising the effective amount of at least compound of the formula (I) and using compounds of the formula (I). Invention provides preparing new compounds possessing useful biological properties.

EFFECT: valuable medicinal properties of compounds and composition.

10 cl, 8 tbl, 35 ex

FIELD: organic chemistry, biochemistry, enzymes.

SUBSTANCE: invention relates to compounds represented by the formula: wherein values of substitutes are given in the invention description. Also, invention relates to pharmaceutically acceptable salts of the compound that can be used in treatment and/or prophylaxis of cathepsin-dependent states or diseases of mammals. Proposed compound are useful in treatment of diseases wherein bone resorption inhibition is desired, such as osteoporosis, increased mineral density of bone and reducing risk of fractures. Proposed claimed compounds are designated for preparing a drug possessing the inhibitory activity with respect to cathepsin.

EFFECT: valuable medicinal and biochemical properties of compounds.

24 cl, 13 sch, 4 tbl, 15 ex

FIELD: chemistry.

SUBSTANCE: invention refers to 1,4-di-N-oxide-2,3-di(chloromethyl)quinoxaline process by halogenations of 1,4-di-N-oxide-2,3-dimethylquinoxaline in hydrochloric and acetic acid medium. Halogenating agent is gaseous chlorine or chlorine in statu nascendi. The process temperature is 70-95°C.

EFFECT: new compounds are characterised with useful biological activity.

3 cl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention relates organic chemistry and specifically to novel pyridine amide derivatives of general formula I where n equals 1; R1 and R2 together denote a residue selected from a group consisting of -CH=N-NH- and -CH=CH-N=CH-, which is bonded in any desirable direction to the parent structure or R2 and R3 together denote a residue selected from a group consisting of -CH=N-NH-; -CR28=N-NH-; -S-C(=S)-NH-; -S-CR29=N-; -N=CR30-O-; -N=CH-NH-; -N=N-NH-; -O-CH2-O-; -CH2-CH2-CH2-NH, -O-CH2-CH2-O-; -N=CH-CH=N-; -CH=CH-CH=N-, which is bonded in any desirable direction to the parent structure, or R3 and R4 together denote a -CH=N-NH- residue, which is bonded in any desirable direction to the parent structure, or R4 and R5 together denote a -CH=N-NH- residue, which is bonded in any desirable direction to the parent structure, and the rest of the residues R1, R2, R3, R4 and R5, mutually independently, in each case denote H; where R28 denotes F; Cl; Br or I; R29 and R30, mutually independently, in each case denote -NH-C(=O)-R31; -NH2; -NH-S(=O)2-R32; -NH-C(=O)-O-R33; -S-R34; where R31, R32, R33 and R34, mutually independently, in each case denote a straight or branched, saturated, unsubstituted aliphatic C1-10 residue; R6 denotes H or denotes a straight or branched, saturated, unsubstituted aliphatic C1-10 residue; R7 denotes hydrogen or -OH; R denotes -CF3; or denotes an unsubstituted tert-butyl residue; T denotes C-R35 and U denotes C-R36, V denotes N and W denotes C-R38; where R35 and R36 denote H; where R38 denotes -NR40R41; -OR42 or -SR43; where R40, R41, R42 and R43, mutually independently, in each case denote a straight or branched, saturated, unsubstituted aliphatic C1-10 residue; or denote a saturated, unsubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-member cycloaliphatic residue, or where R40 and R41 in each case together with a nitrogen atom as a ring member which binds them together, form a saturated 6-member heterocycloaliphatic residue, optionally substituted with one R57 residue, where R57 denotes a straight or branched, saturated, unsubstituted aliphatic C1-10 residue; in each case in form of corresponding physiologically acceptable salts. The invention also relates to a method of producing a compound of formula I, a medicinal agent based on the compound of formula I and use of the compound of formula I.

EFFECT: obtaining novel amide derivatives of pyridine, useful in treating vanilloid receptor 1 mediated diseases.

25 cl, 1 tbl, 18 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to application of formula

compound,

where stands for aromatic ring, where V represents C or N and, where V represents N, V is in meta- or para-position to Z, R independently represents hydrogen atom, halogen atom or group, selected from group -CN, hydroxyl group, group -COOR1, (C1-C3)fluoroalkyl group, (C1-C3)fluoroalkoxy group, group -NO2, group -NR1R2, (C1-C4)alkoxy group, phenoxy group and (C1-C3)alkyl group, where said alkyl is possibly monosubstituted with hydroxyl group, R1 and R2 independently represent hydrogen atom or (C1-C3)alkyl group, n equals 1, 2 or 3, n' equals 1 or 2, R' represents hydrogen atom, halogen atom or group, selected from (C1-C3)alkyl group, group -NO2, group -NR1R2, morpholinyl group, N-methylpiperazinyl group, (C1-C3)fluoroalkyl group and (C1-C4)alkoxy group, R" represents hydrogen atom, Z, Y, X, W, T, U independently represent N or C, and where maximum four of groups V, T, U, Z, Y, X and W represent N, and at least one of groups T, U, Y, X and W represents N, or any of its pharmaceutically acceptable salts for obtaining medication for prevention, inhibition or treatment of cancer. Invention also relates to application of particular compounds, to novel quinoline and isoquinoline derivatives, pharmaceutical composition based on novel quinoline and isoquinoline derivatives.

EFFECT: obtained are novel quinoline and isoquinoline derivatives, and novel biological activity of known compounds is discovered.

10 cl, 2 tbl, 6 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to using a compound of formula

or any of its pharmaceutically acceptable salts, wherein means an aromatic ring, wherein V represents C or N, and when V represents N, V is found in meta- or para-position to Z, R independently represents a hydrogen atom, halogen atom or group specified in -CN group, hydroxyl group, -COOR1 group, (C1-C3)fluoralkyl group, (C1-C3)fluoralkoxy group, -NO2 group, -NR1R2 group, (C1-C4)alkoxy group, phenoxy group and (C1-C3)alkyl group, wherein the above alkyl is optionally monosubstituted by a hydroxyl group, R1 and R2 independently represent a hydrogen atom or (C1-C3)alkyl group, n is equal to 1, 2 or 3, n′ is equal to 1 or 2, R′ represents a hydrogen atom, halogen atom or group specified in (C1-C3)alkyl group, -NO2 group, -NR1R2 group, morpholinyl group, N-methylpiperazinyl group, (C1-C3)fluoralkyl group and (C1-C4)alkoxy group, R″ represents a hydrogen atom, Z, Y, X, W, T and U represent N or C, and wherein at most four of V, T, U, Z, Y, X and W groups represent N, and at least one of T, U, Y, X and W groups represents N, for producing a medicinal preparation for preventing, inhibiting or treating AIDS. The invention also refers to using specific compounds, new quinoline derivatives, a pharmaceutical composition based on the new quinoline derivatives.

EFFECT: new quinoline derivatives are produced, and new biological activity of known compounds is stated.

15 cl, 2 tbl, 11 ex

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, specifically to a heterocyclic compound of formula (IA) or to a pharmaceutically acceptable salt thereof, where in each case R1 and R3 are independently selected from a group comprising hydrogen, halogen, -OH, -C1-2alkyl, -O-C1-2alkyl, -O-C1halogenalkoxy, -N(C1alkyl)2; R2 represents hydrogen; W represents a group selected from -CH= or -N=; X represents a group selected from -CH=CH- or -N=CH-, where nitrogen from -N=CH- is directly bonded with ring 'a'; Y represents a group selected from -CH=CH- or -C≡C-; Z denotes a bond or group selected from -(CH2)n- and -CH=CH-; A is a group selected from -OR, -O(CH2)nphenyl, -O(CH2)nthiophene; P is selected from a group comprising -O-; Q is a group selected from -COOH; where R is selected from a group comprising hydrogen, -C1-6alkyl, -C3-6cycloalkyl, -C1alkyl (C3-6cycloalkyl), -C3-6alkenyl and -C3-6alkynyl; 'n' in each case represents an integer, selected from 1, 2 or 3; 'm' in each case represents an integer, selected from 0-3, inclusive. Invention also relates to a compound of formula (Id), where radicals are described in patent claim.

EFFECT: obtaining novel heterocyclic compounds effective as antagonists of cysteinyl-leukotriene.

9 cl, 1 dwg, 2 tbl, 67 ex

FIELD: pharmacology.

SUBSTANCE: invention relates to benzopyrazine derivatives of the general formula (I)

,

including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof, wherein W is -N(R3)-; R2 is C1-4alkoxy; Y is -CR18=N-OR19 or -E-D; E is bond, C2-4alkynediyl, -CO-(CR22R23)s-, -NR22-(CR22R23)s-, -(CR22R23)s-CO-NR22-(CR22R23)s- or -(CR22R23)s-NR22-CO-(CR22R23)s-; D is phenyl, 3-6 membered cycloalkyl or 5-9 membered mono- or bicyclic saturated, partially saturated or aromatic heterocyclyl containing 1-4 heteroatoms selected from N, O or S, wherein the said phenyl, cycloalkyl and heterocyclyl can each optionally being substituted with 1-2 R1-groups; with the exception of the compounds indicated in the formula; R1 is halogen, cyano, C1-6alkyl, C1-6alkoxy, -C(=O)-O-C1-6alkyl, hydroxyC1-6alkyl, -NR4R5 , C1-6alkyl substituted by -O-C(=O)-C1-6alkyl, C1-6alkyl substituted by -NR4R5, -C(=O)-NR4R5, R6, C1-6alkyl substituted by R6, -C(=O)-R6; R3 is halogenC1-6alkyl, optionally substituted by -O-C(=O)-C1-6alkyl, hydroxyC1-6alkyl, hydroxyhalogenC1-6alkyl, C1-6alkoxyC1-6alkyl, where each C1-6alkyl may optionally be substituted by one hydroxyl group or -O-C(=O)-C1-6alkyl, C1-6alkyl substituted by R9, C2-6alkynyl substituted with R9, C1-6alkyl substituted by -NR10R11, C1-6alkyl substituted by -O-C(=O)-NR10R11; R4 and R5 are hydrogen, C1-6alkyl, C1-6alkyl substituted by -NR14R15, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, where each C1-6alkyl may optionally be substituted by one hydroxyl group, -C(=O)-NR14R15, -C(=O)-O-C1-6alkyl, -C(=O)-R13; R6 is a 6-membered saturated or aromatic monocyclic heterocyclyl having 1 to 2 heteroatoms selected from N or O; the said heterocyclyl is optionally substituted by 1 substituent selected from C1-6alkyl, halogen, C1-6alkyl-O-C(=O)-; R9 is C3cycloalkyl or 3-6 membered monocyclic saturated, partially saturated or aromatic heterocyclyl containing 1-2 heteroatoms selected from N or O, the said heterocyclyl is optionally substituted by 1 substituent selected from =O, hydroxyC1-4alkyl, C1-4alkyl-C(=O)-, C1-4alkyl substituted by -NR14R15, C1-4alkoxy; R10 and R11 are hydrogen, C1-6alkyl, halogen C1-6alkyl, hydroxyC1-6alkyl or C1-6alkyl substituted by carboxyl; R13 is a saturated 6-membered monocyclic heterocyclyl containing 1-2 heteroatoms selected from N and O; R14 and R15 are hydrogen or C1-4alkyl; R18 and R19 are C1-6alkyl; R22 and R23 are hydrogen; n=2; s=0, 1, 2, or 3. Invention also relates to a pharmaceutical composition and a product based thereon, the use of a compound of formula (I) and a method of prevention or treatment of conditions mediated by FGFR kinase.

EFFECT: new derivatives of benzopyrazine, useful for cancer treatment.

28 cl, 4 tbl, 54 ex

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