2,4,6-phenyl-substituted cyclic ketoenols

FIELD: chemistry.

SUBSTANCE: described are 2,4,6-phenyl-substituted cyclic ketoenols of formula (I, in which W, X, Y and CKE are given in invention formula. Also described are esters of acylamino acids of formula (II), substituted derivatives of phenylacetic acid of formula (XXIX), (XXVII), (XXXI), which are intermediate compounds for obtaining formula (I) compound.

EFFECT: obtaining herbicidal preparation containing combinations of biologically active substances, including (a), formula (I) compound and (b') improving compatibility with cultural plants mefenpyr-diethyl, with weight ratio 5-1:1-7.7.

9 cl, 46 tbl, 36 ex

 

The text descriptions are given in facsimile form.

1. 2,4,6-phenylsilane circular ketoenol formula (I)

in which
W stands for C1-C6-alkoxy, C1-C6-alkoxy-C2-C4-alkyloxy or3-C6-cycloalkyl-C1-C3-alcadeias,
X means C1-C6-alkyl,
Y represents chlorine, bromine or iodine,
The NEC means one of the following groups:
, ,
or

in which
A represents hydrogen or C1-C12-alkyl,
In the mean hydrogen or C1-C12-alkyl, or
A and b together with the carbon atom to which they are attached represent a saturated, optionally containing one heteroatom, such as oxygen, unsubstituted or substituted C1-C8-alkyl or C1-C8-alkoxy With3-C10-cycloalkyl,
D is hydrogen, C1-C12-alkyl or saturated With a3-C8-cycloalkyl, or
A and D together with the atoms to which they are attached, denote With3-C6-landiolol group in which two adjacent substituent optionally form together with the carbon atoms to which they are attached, additional saturated cycle with five ring atoms,
G means hydrogen (a) or one of the following groups:
,,or,
where E means the ammonium ion (N+(C6H13)4),
L is oxygen,
M stands for oxygen,
R1means1-C20-alkyl, C2-C20alkenyl or C1-C8-alkoxy-C1-C8-alkyl,
R2means1-C20-alkyl or C2-C20alkenyl,
R3means C 1-C8-alkyl.

2. 2,4,6-phenylsilane circular ketoenol formula (I) according to claim 1, in which
W means1-C4-alkoxy, C1-C3-alkoxy-C2-C3-alkyloxy or3-C6-cycloalkyl-C1-C2-alcadeias,
X means C1-C3-alkyl,
Y represents chlorine or bromine,
The NEC means one of the following groups:
,,
or

A represents hydrogen or C1-C6-alkyl,
In the mean hydrogen or C1-C4-alkyl, or
A, b and the carbon atom to which they are attached represent saturated With5-C7-cycloalkyl, one ring member is optionally replaced by oxygen atom and which optionally 1-fold substituted C1-C6-alkyl or C1-C6-alkoxy, D is hydrogen, C1-C6-alkyl or C3-C6-cycloalkyl, or
A and D (in the case of compounds of formula (I-1)) together with the atoms to which they are attached represent the group AD-1:

G means hydrogen (a) or one of the following groups:
,,or,
where E means the ammonium ion (N+(C6H13)4),
L is for oxygen,
M stands for oxygen,
R1means C1-C8-alkyl, C2-C18alkenyl or C1-C4-alkoxy-C1-C2-alkyl,
R2means C1-C8-alkyl or C2-C8alkenyl,
R3means C1-C6-alkyl.

3. 2,4,6-phenylsilane circular ketoenol formula (I) according to claim 1, in which
W means methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, isobutoxy, sec-butoxy, methoxyethoxy or ethoxyethoxy,
X is methyl or ethyl,
Y represents chlorine or bromine, NEC means one of the following groups:
,,
or

A represents hydrogen or C1-C4-alkyl,
In the mean hydrogen, methyl or ethyl, or
A, b and the carbon atom to which they are attached represent saturated With5-C6-cycloalkyl, one ring member is optionally replaced by oxygen atom and which is optionally substituted once by the stands, ethyl, propylene, isopropyl, methoxy, ethoxy, propoxy or butoxy,
D is hydrogen, C1-C4-alkyl,
cyclopropyl, cyclopentyl or cyclohexyl, or
A and D together denote With3-C5-alcander,
or mean group AD-1,
G means hydrogen (a) or one of the following groups:
,,or,
in which L is oxygen,
M stands for oxygen, and
E. means ammonium ion (N+(C6H13)4),
R1means C1-C6-alkyl, C2-C17alkenyl or1-C2-alkoxy-C1-alkyl,
R2means C1-C6-alkyl or C2-C6alkenyl,
R3means C1-C6-alkyl.

4. 2,4,6-phenylsilane circular ketoenol formula (I) according to claim 1, in which
W means methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, isobutoxy, sec-butoxy, methoxyethoxy or ethoxyethoxy,
X is methyl or ethyl,
Y represents chlorine,
The NEC means one of the following groups:
,,
or

A represents hydrogen, methyl, ethyl, isopropyl, n-propyl, isobutyl, n-butyl, tert-butyl or sec-butyl,
In the mean hydrogen, methyl or ethyl,
A, b and the carbon atom to which they are attached represent saturated With5-C6-cycloalkyl, one ring member is optionally replaced by oxygen and which is optionally substituted once by the stands, methoxy, ethoxy, n-propoxy or n-butoxy,
D is hydrogen, methyl, ethyl, isopropyl, cyclopropyl or cyclohex is l, or
A and D together imply alcander with 3-5 carbon atoms or the group AD-1,
G means hydrogen (a) or one of the following groups:
,,or,
in which L is oxygen,
M stands for oxygen, and
E. means ammonium ion (N+(C6H13)4),
R1means C1-C8-alkyl, C1-C4-alkoxy-C1-alkyl or C2-C17alkenyl,
R2means C1-C8-alkyl or C2-C6alkenyl,
R3means1-C4-alkyl.

5. Esters of acylaminoacyl formula (II)

in which a, b, D, X and Y are specified in claims 1 to 4 values, a W means1-C8-alkoxy and R8means C1-C6-alkyl.

6. Substituted derivatives of phenylacetic acid of the formula

in which X and Y are specified in claims 1 to 4 values, W stands for C1-C6-alkoxy,
a Z means a group of the formula

where D denotes hydrogen, a and b together with the carbon atom to which they are attached represent saturated With5-C7-cycloalkyl, one ring member is replaced by oxygen.

7. Herbicide product with effective content combined the promotion of biologically active substances, includes the following components:
(a') at least one substituted cyclic ketoenol formula (I)according to claim 1, in which
W stands for C1-C6-alkoxy,
X means C1-C6-alkyl,
Y represents chlorine, bromine or iodine,
The NEC means one of the following groups:
,,
in which a represents hydrogen or C1-C12-alkyl,
In the mean hydrogen or C1-C12-alkyl, or
A and b together with the carbon atom to which they are attached represent a saturated unsubstituted or substituted C3-C10-cycloalkyl, D is hydrogen, C1-C12-alkyl or saturated With a3-C8-cycloalkyl,
G means hydrogen (a) or one of the following groups:
,,
in which L is oxygen,
M stands for oxygen,
R1means1-C20-alkyl,
R2means1-C20-alkyl, and
(b') one improves the compatibility with cultivated plants connection diethyl-1-(2,4-dichlorophenyl)-4,5-dihydro-5-methyl-1H-pyrazole-3,5-in primary forms (mefenpyr-diethyl) at a weight ratio of 5-1:1-7,7.

8. Substituted phenylacetic acids of the formula (XXVII)

in which X and Y are specified in claims 1 to 4 values, W stands for C1-C6-alkoxy.

9. the false esters of phenylacetic acid of the formula (XXXI)
,
in which X and Y are specified in claims 1 to 4 values, W means1-C6-alkoxy, and
R8means C1-C6-alkyl.



 

Same patents:

FIELD: chemistry; pharmacology.

SUBSTANCE: invention refers to new pyrimidine compounds of formula (I) with selective inhibition of "КДР" and "ФРФР" kinase. These compounds and their pharmaceutically acceptable salts are antiproliferative agents. In formula (I) , where R1 is chosen from series including -H, -(CH2)n -5-6-merous heterocycle containing 1-2 heteroatoms chosen from nitrogen, sulphur oxygen or dioxide, (C1-C6)alkyl, (C3-C6)cycloalkyl where n stands for 0, and each groups including heterocycle, alkyl, cycloalkyl is independently optionally substituted to three groups chosen from: -OR9, -COR10, -CO2R10, -CONR10R11 and -CN; R2 stands for -H or -OCH3; R3 stands for -H, -F or -OCH3; R4, R5 and R7 stand for -H, R6 means (C1-C6)alkyl or OR12; R8 stands for -H or -F; R9 stands for -H and (C1-C6)alkyl, (C1-C6)alkoxide R10 and R11 independently are chosen from -H and (C1-C6)alkyl, (C1-C6)alkoxy, and R12 stands for -H and (C1-C6)alkyl.

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FIELD: chemistry, pharmacology.

SUBSTANCE: invention refers to new compounds of formula I , where A stands for =C(R4)-, D stands for =C(R5)-, E stands for =C(R6)-, or one of A, D and E stands for =N-, L stands for =N- or =C(H)-, M stands for =C(R7)-, when L stands for =N-, or M stands for when L stands for -C(H)-, Q stands for CF3 or CHF2, R1 stands for -CN, unsubstituted pyridinyl, pyridinyl, substituted (C1-C4)-alkyl or (C1-C4alkanole, or stands for related pyridine N-oxide, R2 stands for hydrogen, R3 stands for hydrogen, R4 stands for hydrogen, halogen, unsubstituted (C1-C4)alkyl or fluorine substituted (C1-C4)alkyl, unsubstituted (C1-C4)alkoxy group or fluorine substituted (C1-C4)alkoxy group, unsubstituted (C3-C6)cycloalkyl or fluorine substituted (C3-C6)-cycloalkyl, R5 stands for hydrogen, halogen, unsubstituted (C1-C4)alkyl or fluorine substituted (C1-C4)alkyl, unsubstituted (C3-C6)cycloalkyl or fluorine substituted (C3-C6)cycloalkyl, R6 stands for hydrogen or halogen, and R7 stands for hydrogen, unsubstituted (C1-C4)alkyl or cyanogen group substituted (C1-C4)alkyl, unsubstituted (C3-C6)cycloalkyl or cyanogen group substituted (C3-C6)cycloalkyl provided when A stands for =C(R4)-, D stands for =C(H)-, E stands for =C(H)-, L stands for =N-, R1 stands for -CN, R2 stands for hydrogen, R3 stands for hydrogen, and (a) M stands for =C(H)-, R4 is not hydrogen, chlorine or methoxygroup; or (b) M stands for =C(CH3)-, R4 is not hydrogen, and to its pharmaceutically acceptable acid-additive salts. Besides, the invention concerns pharmaceutical compositions.

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FIELD: chemistry; pharmacology.

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25 cl, 3 tbl, 4 dwg, 29 ex

FIELD: chemistry; pharmacy.

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14 cl, 16 tbl, 333 ex

FIELD: chemistry.

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35 cl, 3 tbl, 147 ex

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25 cl, 28 tbl, 243 ex

FIELD: chemistry.

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16 cl, 5 tbl, 5 ex

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16 cl, 6 dwg, 10 ex

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17 cl, 6 dwg, 6 ex

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1 cl, 3 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: described is compound of general formula , in which W and Z represent N, and X and Y represent CH; R represents halogen; R1 represents phenyl, substituted with 1-3 substituents, selected from halogen; R2 represents NR3R4; R3 and R4 independently represent H, C1-C8alkyl, C2-C8alkenyl, halogen(C1-C8)alkyl, C1-C4alkoxy(C1-C8)alkyl, C3-C8cycloalkyl, optionally substituted with methyl, or R3 and R4 together form C3-C7alkylene chain, optionally containing as substituent C1-C4alkyl group, or together with nitrogen atom, to which they are bound, R3 and R4 form morpholine or pyperazine-N-(C1-C4)alkyl (more preferably N-methyl) ring. Described is method of obtaining compound of general formula (I), intermediate chemical products, as well as fungicidal composition for plants and method to combat phytopathogenic fungi or their elimination, using compound of formula (I).

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10 cl, 133 tbl, 6 ex

FIELD: chemistry.

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18 cl, 825 ex

FIELD: chemistry.

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41 cl, 2 tbl, 37 ex

FIELD: chemistry.

SUBSTANCE: present invention refers to tetrahydroquinoline derivatives, described by formula (I) where t is equal to 0, 1 or 2; each R independently represents H, alkyl, alkenyl, alkinyl, halogenalkyl, cycloalkyl; n is equal to 0; R2 is chosen from the group consisting of H, alkyl, halogenalkyl, cycloalkyl, -Racycloalkyl, alkenyl, alkinyl, -RaAy, -RaOR5; where R2 is not substituted with amine or alkylamine; R3 represents H; each R4 independently represents halogen, halogenalkyl, alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, -A'y, -NHAy, -Het, -NHHet, -OR10, -NR6R7, -RaNR6R7, -C(O)NR6R7, -C(O)Ay, -C(O)Het; m is equal to 0, 1 or 2; each R5 independently represents H; p is equal to 0 or 1; Y represents NR10-, -O-, -C(O)NR10-, -NR10C(O)-, -C(O)- , - -NR10C(O)N(R10)-; X represents -N(R10)2, -RaN(R10)2, -AyN(R10)2, -RaAyN(R10)2, -AyRaN(R10)2, -RaAyRaN(R10)2, -Het, -RaHet, -HetN(R10)2, -RaHetN(R10)2, -HetRaN(R10)2, - RaHetRaN(R10)2; each Ra independently represents alkylen, optionally substituted with with one or more alkyl; each R10 independently represents H, alkyl, cycloalkyl, alkenyl, alkinyl, cycloalkenyl, -Racycloalkyl; each R6 and R7 is independently chosen from H, alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, -Racycloalkyl, -RaNR8R9; each R8 and R9 is independently chosen from H or alkyl; each Ay independently represents optionally substituted aryl group; and each Het independently represents optionally substituted 4-, 5- or 6-merous heterocyclil or heteroaryl group where heteroatoms are chosen from N and O; or its pharmaceutically acceptable salt, or ester. Besides, there are disclosed pharmaceutical composition based on compound of formula (I), its application and methods of production.

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53 cl, 2 tbl, 105 ex

FIELD: chemistry; pharmacology.

SUBSTANCE: there are disclosed compounds composed as to formula , where n and m stand for integer 1 to 3; z stands for integer 0 to 1; R is chosen from hydrogen, hydroxy or alkoxy; R2 stands for hydrogen; R3 and R4 are independently chosen from the group consisting of hydrogen, halogen; R5 is chosen from the group consisting of halogen, alkyl; R6 represents alkyl; E is chosen from the group specified in item 1 of formula of invention, A is chosen from N and C(R11), X is chosen from C, a stands for double bond and b stands for single bond; and Y is chosen from N(R1) provided when Y stands for N(R1), X stands for C, where R1 is chosen from C3-C6-cyclolkyl, phenyl; provided if A stands for C(R11), X stands for C, and Y stands for N(R1), then R11 and R1 can be bonded thus forming morpholinyl.

EFFECT: compounds possess antibacterial activity and are suitable as antibacterial means for treating bacterial infections in humans and animals.

13 cl, 10 tbl

FIELD: chemistry; pharmacology.

SUBSTANCE: new compounds of formula (I) and its pharmaceutically acceptable salts. Offered compounds possess properties of bacterial gyrase and Topo-IV activity inhibitor. In general formula (I) , W is chosen from CH or CF; X represents CH; Z represents O or NH; R1 represents phenyl or 5-6-merous heteroaryl ring containing 1-3 nitrogen atoms where R1 is substituted with 0-3 groups independently chosen from -(T)y-Ar, R', oxo, C(O)R', OR', N(R')2, SR', CN or C(O)N(R')2; R2 is chosen from C1-3alkyl and C3-7-cycloalkyl; and ring A represents 5-6-merous heteroaryl ring containing 1-3 heteroatoms, independently chosen of nitrogen, oxygen or sulphur provided the specified ring has hydrogen bond acceptor in position adjacent to that of joining to B ring where ring A is substituted with 0-3 groups independently chosen from R', oxo, CO2R', OR', N(R')2, halogen, CN, C(O)N(R')2, NR'C(O)R', or NR'SO2R', and where two substitutes in adjacent positions of ring A, together can form 6-merous saturated heterocyclic or heteroaryl ring containing 1-2 nitrogen atoms.

EFFECT: pharmaceutical compositions with properties of bacterial gyrase and Topo-IV activity inhibitor containing disclosed compound as active component, method of gyrase and/or Toro IV-activity inhibition, method of bacteria number reduction.

25 cl, 3 tbl, 4 dwg, 29 ex

FIELD: chemistry.

SUBSTANCE: present invention pertains to new 7-azaindoles with general formula 1: where (a) A stands for an N-oxide group and B stands for CH, nitrogen, (b) A stands for nitrogen and B stands for an N-oxide group, or (c) A and B stand for an N-oxide group, R1 stands for (i) -C1-10-alkyl, unbranched or branched, which, if necessary, is monosubstituted with saturated mono- C3-C6carbocycle, or mono-, bi- multi-unsaturated C6-C10carbocycle. C6-10-aryl groups in turn, if necessary, can be mono- or multi-substituted with -C1-6-alkyl, -CN, -F, -CI, -Br, -I, -O-C1-6-alkyl groups. Alkyl groups in carboxylic substitutes, in turn, if necessary, can be mono- or multi-substituted with -F groups. R2 stands for hydrogen, C1-C3alkyl. R3 and R4 are identical or different, and stand for hydrogen, -F, -Cl, -Br, -I. The invention also relates to pharmaceutical salts of these 7-azaindoles.

EFFECT: compounds with general formula I exhibit phosphodiesterase 4 inhibiting activity, which allows for their use as therapeutic active substances for making medicinal agents, which suppress pulmonary neutrophilia and eosinophilia.

14 cl, 2 tbl, 7 ex

FIELD: chemistry.

SUBSTANCE: present invention pertains to hexahydropyrido[1,2-a]pyrazine derivatives. The invention also relates to methods of producing these compounds, to pharmaceutical compositions, containing a pharmacologically active amount of at least, one of these compounds as an active ingredient, as well as to use of these compositions for treating disorders, involving neurokinin receptors. The invention also relates to compounds with general formula (1) in which the denotations of symbols are given in the description.

EFFECT: exhibition of antagonistic activity towards neurokinin receptor NK1.

6 cl, 13 ex, 1 dwg

FIELD: chemistry.

SUBSTANCE: present invention pertains to new compounds with general formula (I), in which X1 is phenyl, 9-member bicyclic heteroaryl, containing S or O as heteroatoms, or 5-member heteroaryl, containing S or O as heteroatoms, each of which is optionally substituted with one or more substitutes, chosen from halogen or C1-6alkyl, which is optionally substituted with one or more halogens. X2 is phenyl, which is optionally substituted with one or more substitutes, chosen from halogen, or 5-member heteroaryl, containing S or O as heteroatoms. Ar is phenylene, which is optionally substituted with one or more substitutes, chosen from halogen, or C1-6alkyl, phenyl, C1-6alkoxy, each of which is optionally substituted with one or more halogens. Y1 is O or S, and Y2 represents O, Z represents -(CH2)n-, where n equals 1, 2 or 3. R1 is hydrogen or C1-6alkoxy and R2 is hydrogen, C1-6alkyl. The invention also relates to pharmaceutical salts of these compounds or any of their tautomeric forms, stereoisomers, stereoisomer mixtures, including racemic mixtures.

EFFECT: invention also pertains to use of these compounds as pharmaceutical compositions, with effect on receptors, activated by the peroxisome proliferator PPARδ subtype, and to pharmaceutical compositions, containing these compounds (I).

36 cl, 41 ex

Kinase inhibitors // 2348635

FIELD: chemistry; pharmacy.

SUBSTANCE: invention concerns new compounds of formula I: , where W is , X is N or C-R1; R is C1-C7alkyl, C3-C7cycloalkyl, (C1-C7alkylene)-(C3-C7cycloalkyl), -SO2-(C1-C7alkyl) or -SO2-NR5R6; R1 is hydrogen, amino, methyl or -N=CH(NMe)2; R is phenyl optionally substituted by one or more substitutes selected independently out of halogen; R3 is hydrogen, C1-C7alkyl, C3-C7cycloalkyl or phenyl optionally substituted by one or more substitutes selected independently out of halogen and trifluoromethyl; R4 is hydrogen or C1-C7alkyl; R5 and R6 are independently selected out of group including C1-C7alkyl; and its pharmaceutically acceptable salts. Also invention concerns pharmaceutical composition and application.

EFFECT: obtaining new bioactive compounds with inhibition effect on kinase p-38.

10 cl, 114 ex

FIELD: organic chemistry, insecticides.

SUBSTANCE: invention relates to compounds of formula I , wherein W is halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C4-haloalkyl or C1-C4-haloalkoxy; X is hydrogen, halogen, C1-C6-alkyl; Y is hydrogen, halogen, C1-C6-alkyl, C1-C4-haloalkyl, C1-C4-haloalcoxy or cyano; Z is hydrogen, halogen, etc.; G is halogen or nitro; meanings of the other substituents are as defined in specification. Also disclosed are methods for production of said compounds by interaction compounds of formula II with halogenation agents in presence of solvent and optionally of radical initiator of with fumed nitric acid in presence of solvent.

EFFECT: new compounds with insecticide activity.

17 cl, 20 tbl, 114 ex

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