Derivative phenylsulfonylacetate (options)

 

The invention relates to new derivatives of phenylsulfonylacetate General formula (I), which are herbicide and regulating plant growth properties and can find application in agriculture. In the compounds of formula (I) R1means acyl residue of the formula SO2-R10or-Q-R11; R2, R3, R4, R5mean hydrogen; R6means hydrogen or alkyl with 1-6 carbon atoms; R7means acyl residue selected from the group including formyl, alkylsulphonyl with 1-4 carbon atoms in the alkyl part, possibly substituted with halogen, alkoxygroup with 1-4 carbon atoms, alkenylboronic with 2-4 carbon atoms in alkenylphenol part, alkenylboronic with 2-4 carbon atoms in alkenylphenol part, alkoxycarbonyl with 1-4 carbon atoms in the alkyl residue, alkoxycarbonylmethyl with 1-4 carbon atoms in the alkyl residue, alkylsulfonyl with 1 to 4 carbon atoms in the alkyl part, possibly substituted with halogen, cycloalkylcarbonyl with 3-6 carbon atoms, mono - or dialkylaminoalkyl with 1-4 carbon atoms in the alkyl part, phenylcarbinol, phenylsulfonyl, or group (1) or (2), or R6and R7together form a chain of formula-CH2)means a sulfur atom; Womeans an oxygen atom or a sulfur atom; W denotes an oxygen atom, R8means hydrogen; R9means hydrogen or methyl; R10and R11denote alkyl with 1-6 carbon atoms; R12means alkyl with 1-4 carbon atoms; R13and R14independently of one another denote hydrogen or alkyl with 1-4 carbon atoms; a represents a residue of formula 3, where X means halogen, alkyl with 1-3 carbon atoms or alkoxy with 1-3 carbon atoms, possibly substituted with halogen; or a group N(C1-C4-alkyl)2provided that Y does not mean the group NH(C1-C4-alkyl); Y represents alkyl with 1-3 carbon atoms or alkoxy with 1-3 carbon atoms, possibly substituted with halogen; or a group NH(C1-C4-alkyl), provided that X does not mean group N(C1-C4-alkyl)2; Z denotes CH or nitrogen, and their salts. The invention also relates to new intermediate product of the formula II, where R is an amino group. 2 S. and 2 C.p. f-crystals, 4 PL.

Description text in facsimile form (see graphic material)

where R1means acyl residue of the formula SO2-R10or CO-Q-R11;

R2, R3, R4, R5mean hydrogen;

R6means hydrogen or alkyl with 1-6 carbon atoms;

R7means acyl residue selected from the group including formyl, alkylsulphonyl with 1-4 carbon atoms in the alkyl part, possibly substituted with halogen, alkoxygroup with 1-4 carbon atoms, alkenylboronic with 2-4 carbon atoms in alkenylphenol part, alkenylboronic with 2-4 carbon atoms in alkenylphenol part, alkoxycarbonyl with 1-4 carbon atoms in the alkyl residue, alkoxycarbonylmethyl with 1-4 carbon atoms in the alkyl residue, alkylsulfonyl with 1 to 4 carbon atoms in the alkyl part, possibly substituted with halogen, cycloalkylcarbonyl with 3-6 carbon atoms, mono - or dialkylaminoalkyl with 1-4 carbon atoms in the alkyl part, phenylcarbinol, phenylsulfonyl or

or

or R6and R7together form a chain of formula-CH2)m1B1-, m1=3 or 4;

B1means SO2or CO;

Q denotes an oxygen atom or a sulfur atom;

Tmeans a sulfur atom/sup> means hydrogen;

R9means hydrogen or methyl;

R10and R11denote alkyl with 1-6 carbon atoms;

R12means alkyl with 1-4 carbon atoms;

R13and R14independently of one another denote hydrogen or alkyl with 1-4 carbon atoms;

A represents the residue of a formula

where X represents halogen, alkyl with 1-3 carbon atoms or alkoxy with 1-3 carbon atoms, possibly substituted with halogen, or the group N(C1-C4-alkyl)2provided that Y does not mean the group NH(C1-C4-alkyl);

Y represents alkyl with 1-3 carbon atoms or alkoxy with 1-3 carbon atoms, possibly substituted with halogen, or the group NH(C1-C4-alkyl), provided that X does not mean group N(C1-C4-alkyl)2;

Z denotes CH or nitrogen,

and their salts.

2. Derivative phenylsulfonylacetate General formula (I) under item 1, where R1means SO2-R10or CO-OR11, R6means hydrogen or alkyl with 1-4 carbon atoms, R7means formyl, alkylsulphonyl with 1-4 carbon atoms in the alkyl part, possibly substituted with halogen, alkoxygroup with 1-4 carbon atoms, alkenylboronic with 2-4 carbon atoms in alcanada in cycloalkyl, phenylcarbinol, phenylsulfonyl, mono - or dialkylaminoalkyl with 1-4 carbon atoms in the alkyl part, or a group of the formula-C(WT-R12or-C(W- NR13R14or R6, R7together represent a chain of formula-CH2)m1B1-, and m1=3 or 4, Wmeans an oxygen atom or sulfur, W denotes an oxygen atom, Tmeans an oxygen atom or sulfur, In1means SO2or, Q denotes an oxygen atom or sulfur, R8means a hydrogen atom, R9means hydrogen or methyl, R10and R11denote alkyl with 1-6 carbon atoms, R12means alkyl with 1-4 carbon atoms, R13, R14independently of one another denote hydrogen or alkyl with 1-4 carbon atoms and the remaining substituents are specified in paragraph 1.

3. Derivative phenylsulfonylacetate formula (I) under item 1 or 2, where R6means hydrogen or alkyl with 1-4 carbon atoms, R7means formyl, alkylsulphonyl with 1-6 carbon atoms in the alkyl, halogenoalkanes with 1-4 carbon atoms in the alkyl, alkoxycarbonyl with 1-4 carbon atoms in the CNS residue with 1-4 tamamono or dialkylaminoalkyl with 1-4 carbon atoms in the alkyl part, or a group of the formula-C(WT-R12or-C(W)NR13R14; Wmeans an oxygen atom or sulfur, W denotes an oxygen atom, Tmeans sulfur, Q denotes oxygen or sulfur, R10and R11denote alkyl with 1-4 carbon atoms, R12means alkyl with 1-4 carbon atoms, R13, R14independently of one another denote hydrogen or alkyl with 1-4 carbon atoms and the remaining substituents are specified in paragraph 1.

4. Derivative phenylsulfonylacetate General formula (II)

where R1-R8are specified in paragraph (1 value;

R is amino,

representing intermediate products to obtain derivatives phenylsulfonylacetate General formula (I) under item 1.

 

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The invention relates to compounds of formula (I)

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in which Ar1denotes a heterocyclic group, which represents a pyrazole which may be substituted by one or more radicals R1, R2or R3; Ar2denotes phenyl, naphthyl or tetrahydronaphthyl, each of which optionally is substituted by one to three groups R2; L denotes a saturated or unsaturated, branched or unbranched carbon C1-C10chain; in which one or more methylene groups are optionally independently replaced by O, NH or S, and in which the linking group is optionally substituted by 0-2 of doxography; Q has a value selected from a range of: a) phenyl, naphthyl, pyridine, imidazole, Piran, etc. b) tetrahydropyran, morpholine, thiomorpholine, thiomorpholine and t

The invention relates to new derivatives of benzothiadiazole, benzoxazoles and benzodiazines formula I in free base form or in the form of a pharmaceutically acceptable acid salt additive that can be used as an anxiolytic drug in the treatment of any condition, which is associated with increased endogenous levels of CRF or in which violated the regulation of the hPa system (hypothalamic - pituitary), or various diseases that are caused by CRF1or the manifestation of which contributes CRF1such as arthritis, asthma, allergies, anxiety, depression, etc

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The invention relates to amide derivative of the formula I

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where R3represents (1-6C)alkyl or halogen; m is 0, 1, 2 or 3; R1represents hydroxy, halogen, trifluoromethyl, nitro, amino, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)quinil, (1-6C)alkoxy, (1-6C)alkylamino, di-[(1-6C)alkyl] amino, amino-(2-6C)alkylamino, (1-6C)alkylamino-(2-6C)alkylamino etc

The invention relates to compounds of formula (1), where X and Y Is N or O; R1substituted alkyl, substituted arylalkyl or cycloalkyl; R2and R3Is h or alkyl; And a Is-C(O)-, -OC(O)-, -S(O)2-; R4- alkyl, cycloalkyl or (C5-C12)aryl; compounds of the formula (2), where X and Y are O, S or N; R1- alkyl, optionally substituted arylalkyl; R2and R3Is h or alkyl;- C(O)-; R6- Deputy, including the condensed heterocyclic rings; and compounds of the formula (3), where X and Y are O, S or N; R1- alkyl, alkylsilane, (C5-C12)arylalkyl, (C5-C12)aryl; R2and R3Is h or alkyl; R2' and R3' - N; R11, R12and E together form a mono - or bicyclic ring which may contain heteroatoms

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where

R - CH3C2H5

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where R1lower alkyl WITH1-C4

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-converting enzyme)" target="_blank">

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is a benzene ring, or is a heteroaryl ring of 5 to 6 atoms in the cycle, which may contain 0-2 heteroatoms selected from nitrogen, oxygen and sulfur, in addition to the heteroatom of nitrogen, denoted as W, where benzene or heteroaryl ring may optionally contain one or two substituent R1where permissible; Z is phenyl, which is optionally substituted by phenyl, alkyl with 1-8 carbon atoms, or a group OR2; R1represents halogen, alkyl with 1-8 carbon atoms, alkenyl with 2-6 carbon atoms, perfluoroalkyl from 1 to 4 carbon atoms, phenyl, optionally substituted by 1-2 groups OR2group-NO2group -(CH2)nZ, where Z is a phenyl which allows an alkyl with 1-8 carbon atoms, phenyl, optionally substituted with halogen, or heteroaryl radical containing 5 to 6 atoms in the cycle, including 1-2 heteroatoms selected from nitrogen, oxygen and sulfur; R5represents hydrogen, alkyl with 1-8 carbon atoms, phenyl, or heteroaryl containing 5 to 6 atoms in the cycle, including 1-2 heteroatoms selected from nitrogen, oxygen and sulfur; or their pharmaceutically acceptable salts

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in which the substituents have the following meanings: L, M denote hydrogen, alkyl, alkyloxy, alkylthio, chlorine, cyano, methylsulphonyl, nitro or trifluoromethyl, J denotes hydrogen, alkyl, cycloalkyl, alkenyl, quinil, acyl, phenyl, optionally substituted with halogen or alkyl, benzyl, means connected in position 2 optional substituted cyclohexane-1,3-diNovo ring of formula II

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in which R1- R6mean hydrogen or methyl, or, if R1, R2, R3, R5and R6mean hydrogen, R4mean 2-ethylthiophen, tetrahydrothiopyran-3 or metaltitlepane, or R1, R4, R5mean hydrogen, and R6means methyl, R2and R3form a three-membered ring, which is formed connected in position 2 bicyclo-(4.1.0)heptane ring of formula III

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and they are usually used in agriculture salt
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