N-alkynyl-2-(substituted aryloxy)-alkyltioamide derivatives as fungicides
FIELD: chemistry.
SUBSTANCE: described are compounds of formula (I), in which Ar represents group of formula (A), (B1), (B2) or (C), or (D1), or (D2); R1, R2, R3, R4, R5, n, A1, A2, A3, A4, A5, Ka, Kb, L, M, V, W, X, Y, Z havevalues, determined in i.1 of invention formula, fungicide composition and method of combatting phytopathogenic fungi or their elimination, using compounds of formula (I).
EFFECT: high fungicide activity.
22 cl, 142 tbl, 34 ex
The text descriptions are given in facsimile form.
1. The compound of General formula (1):
in which Ar denotes a group of formula (A):,
in which And1And2and A3independently denote H, halogen, C1-C4alkyl, halogen(C1-C4)alkyl, C1-C4alkoxygroup, halogen(C1-C4)alkoxyl the PPU,
-S(O)m(C1-C4)alkyl, where m is 0; or
Ar denotes a group of formula (B1) or (B2):
in which L and M independently represent N, N-oxide or CQ, except that not more than one of L and M denotes N-oxide;
Toandandbdenote H;
V denotes H, halogen, C1-C6alkyl;
Q denotes H, halogen, C1-C8alkyl, C3-C6cycloalkyl, halogen(C1-C8)alkyl; or
Ar denotes a group of formula (C):
in which And4and5independently denote H, halogen; or
Ar denotes a group of the formula (D1) or (D2):
in which W denotes H, halogen, C1-C4alkyl,
X represents N or N-C1-C4alkyl,
Y represents CR, N, O,
Z represents CR, N, N-C1-C4alkyl, O or S,
R denotes H, halogen, C1-C4alkyl, mono-(C1-C4)alkylamino, the link connecting X, Y, Z and a condensed benzene ring are double or ordinary links corresponding to the valence of X, Y and Z, provided that only one of Y and Z may denote O, that only one of Y and Z may denote CH or CR, and that only one of X and Z may denote the N-C1-C4alkyl;
R1denotes methyl or ethyl;
R2denotes H;
R3and R4independently represent C1-C3alkyl, provided that the total amount of contained carbon atoms does not exceed 4, or R3and R4together with the carbon atom to which they are attached, form a 3 - or 4-membered carbocyclic ring;
R5denotes H, C1-C4alkyl in which the alkyl group optionally contains as substituents halogen, a hydroxy-group, C1-C6alkoxygroup, cyano, or
R5denotes optionally substituted phenyl, which is optionally substituted phenyl ring or fragments of the group R5optionally contain 1, 2 or 3 substituent selected from the group comprising halogen, a hydroxy-group, With1-C4alkyl, C1-C4alkoxygroup, a cyano, a nitro-group, or
R5denotes optionally substituted C1-C4the alkyl thienyl; and n is 0, 1 or 2.
2. The compound according to claim 1, in which Ar denotes a group of formula (A):,
in which And1And2and3independently denote H, halogen, C1-C4alkyl, halogen(C1-C4)alkyl, C1-C4alkoxygroup, halogen(C1-C4)alkoxygroup, -S(O)m(C1-C4)alkyl, where m is 0; or
Ar hereafter which denotes a group of formula (B):
,
in which one of L and M denotes N and the second one denotes CQ;
Q denotes H, halogen, C1-C8alkyl, C3-C6cycloalkyl, halogen(C1-C8)alkyl; or Ar represents a group of formula (C):
in which And4and5independently denote H, halogen; or
Ar denotes a group of the formula (D1):,
in which W denotes H, halogen, C1-C4alkyl,
X represents N or N-C1-C4alkyl,
Y represents CH, N, O,
Z represents CH, N, N-C1-C4alkyl, O or S, and
the link connecting X, Y, Z and a condensed benzene ring are double or ordinary links corresponding to the valence of X, Y and Z, provided that only one of Y and Z may denote O, that only one of Y and Z may denote SN and that only one of X and Z may denote the N-C1-C4alkyl;
R1denotes methyl or ethyl;
R2denotes H;
R3and R4independently denote With1-C3alkyl, and the total amount of contained carbon atoms does not exceed 4, or
R3and R4together with the carbon atom to which they are attached, form a 3 - or 4-membered carbocyclic ring;
R5denotes H, C1-C4alkyl, in which alkyl the second group optionally contains as substituents halogen,
the hydroxy-group, With1-C6alkoxygroup, cyano, or
R5denotes optionally substituted phenyl, which is optionally substituted phenyl ring or fragments of the group R5optionally contain 1, 2 or 3 substituent selected from the group comprising halogen, a hydroxy-group, With1-C4alkyl, C1-C4alkoxygroup, a cyano, a nitro-group, or R5denotes optionally substituted C1-C4the alkyl thienyl; and n is 0, 1 or 2.
3. The compound according to claim 1, in which Ar denotes a group of formula (A), where A1And2and3denote chlorine or methyl, or a1and3both represent chlorine, bromine or fluorine and2denotes H or methyl, or a1and3both represent methyl or methoxy group and a2denotes H, chlorine, bromine or allylthiourea, or And1denotes a methoxy group, And2denotes H and3denotes chlorine, or a1denotes methyl, And2denotes H and3denotes ethyl, or a1denotes chlorine, bromine, trifluoromethyl, cryptometer and2and3both represent H, or a1and3both represent H and2denotes chlorine or bromine, or a1denotes methyl, And2means (C1-C4)allylthiourea and3denotes N.
p> 4. The compound according to claim 1, in which Ar denotes a group of formula (B1) or (B2), in which M denotes N and L denotes CQ, or L and M both represent N, or L denotes N and M denotes CQ, or L and M both represent CQ and Q denotes H or halogen.5. The compound according to claim 1, in which Ar denotes a pyridine group of formula (C) and side chain amide alanovoy acid compound of General formula (1) is attached in position 3 of the pyridine ring.
6. The compound according to claim 5, in which the group of formula (C) And4denotes H and5denotes halogen.
7. The compound according to claim 1, in which Ar denotes a group of the formula (D1) or (D2), in which W denotes H, halogen, C1-C4alkyl, and
(1) X represents N, Y represents CR, Z represents O, S or N-C1-C4alkyl, and R denotes H, halogen, C1-C4alkyl or mono-(C1-C4)alkylamino, the link X-Y is a double bond and bond Y-Z and the link connecting X and Z to the benzene ring, are ordinary bonds; or
(2) X and Y denote the N and Z denotes O, S or N-C1-C4alkyl, link X-Y is a double bond and bond Y-Z and the link connecting X and Z to the benzene ring, are ordinary bonds; or
(3) X represents N, Y represents O, Z represents CR, and R denotes H, halogen, C1-C4alkyl or mono-(C1-C4)alkylamino, communication, X-Y and Y-Z are the hordes of the stationary relations and communications
connecting X and Z of the benzene ring are double bonds; or
(4) X is N-C1-C4-alkyl, Y represents N, Z represents CR, and R denotes H, halogen, C1-C4alkyl or mono-(C1-C4)alkylamino, link Y-Z is a double bond and bond Y-Z and the link connecting X and Z to the benzene ring, are ordinary links.
8. The connection according to claim 7, in which the group of formula (D1) or (D2) denotes a 5 -, and 6-benzothiazolyl, not necessarily containing 2-s-Deputy, 5 - and 6-(2,1-benzisothiazoles), optionally containing 3-With-Deputy, 5 - and 6-benzoxazolyl, not necessarily containing 2-s-Deputy, 5 - and 6-(2,1-benzisoxazoles), optionally containing 3-With-Deputy, 5 - and 6-(1H-benzimidazolyl), not necessarily containing 2--Deputy and optionally containing N-C1-C4alkyl substituent, 5-and 6-(1H-indazole), optionally containing 3-C substituent and optionally containing N-C1-C4alkyl substituent, 5 - and 6-(2H-indazole), optionally containing 3-C substituent and optionally containing N-C1-C4alkyl substituent, 5 - and 6-(1,2,3-benzothiadiazole), 5 - and 6-(1,2,3-benzoxadiazole), 5 - and 6-(1H-benzotriazolyl), optionally containing N-C1-C4alkyl substituent, 5-(2H-benzotriazolyl), optionally containing N-C1-C4alkyl replace the e l e C 5-(2,1,3-benzothiadiazole) and 5-(2,1,3-benzoxadiazole)where any of the above optional substituents selected from the group comprising halogen, C1-C4alkyl,
9. The connection according to claim 7, in which the group of formula (D1) or (D2) denotes a 5 - or 6-benzothiazolyl, not necessarily containing 2-s-Deputy, 5-(2,1-benzisothiazoles), optionally containing 3-With-Deputy, 6-benzoxazolyl, not necessarily containing 2-s-Deputy, 5-(2,1-benzisoxazoles), optionally containing 3-With-Deputy, 6-(1H-benzimidazolyl), not necessarily containing 2-C substituent and optionally containing N-C1-C4alkyl substituent, 5-(1H-indazole), optionally containing 3-C substituent and optionally containing N-C1-C4alkyl substituent, 6-(1,2,3-benzothiadiazole) or 6-(1,2,3-benzoxadiazole)where any of the above optional substituents selected from the group comprising halogen, C1-C4alkyl.
10. The compound according to claim 1, in which R2denotes N.
11. The compound according to claim 1, in which R3and R4both denote methyl,
12. The compound according to claim 1, in which R5denotes H, methyl, hydroxymethyl, methoxymethyl, 1-methoxyethyl, 3-cyano-n-propyl, 3-chloro-n-propyl, phenyl, 4-forfinal, Tien-2-yl, Tien-3-yl.
13. The compound according to claim 1, in which R2denotes H; R3and R4both hereafter is widely methyl; and R5denotes H, methyl, hydroxymethyl, methoxymethyl, 1-methoxyethyl, 3-cyano-n-propyl, 3-chloro-n-propyl, phenyl, 4-forfinal, Tien-2-yl, Tien-3-yl.
14. The compound according to claim 1, in which Ar denotes a group of formula (A), where A1And2and3denote chlorine or methyl, or a1and3both represent chlorine, bromine or fluorine and2denotes H or methyl, or a1and3both represent methyl or methoxy group and a2denotes H, chlorine, bromine or (C1-C4)allylthiourea, or And1denotes methyl, And2denotes H and3denotes ethyl, or a1denotes chlorine, bromine, trifluoromethyl, cryptometer and2and3both represent H, or a1and3both represent H and2denotes chlorine or bromine, or a1denotes methyl, And2means (C1-C4)allylthiourea and3denotes H; R2denotes H; R3and R4both represent methyl; and R5denotes H, methyl, hydroxymethyl, hydroxymethyl, methoxymethyl, 1-methoxyethyl, 3-cyano-n-propyl, 3-chloro-n-propyl, phenyl, 4-forfinal, Tien-2-yl, Tien-3-yl.
15. The compound according to claim 1, in which Ar denotes a group of formula (B1) or (B2), in which L and M independently represent N,N-oxide or CQ, except that not more than one of L and M denotes N-oxide; Q Ref is no H or halogen; R2denotes H; R3and R4both represent methyl; and R5denotes H, methyl, hydroxymethyl, methoxymethyl, 1-methoxyethyl, 3-cyano-n-propyl, 3-chloro-n-propyl, phenyl, Tien-2-yl, Tien-3-yl.
16. The compound according to claim 1, in which Ar denotes a group of formula (C), in which And4denotes H; and5denotes halogen; R2denotes H; R3and R both represent methyl; and R5denotes H, methyl, hydroxymethyl, methoxymethyl, 1-methoxyethyl, 3-cyano-n-propyl, 3-chloro-n-propyl, phenyl, Tien-2-yl, Tien-3-yl.
17. The compound according to claim 1, in which Ar denotes a group of formula (C), in which And4denotes H; And5denotes H, halogen; R2denotes H; R3and R4both represent methyl; R5denotes H, methyl, hydroxymethyl, methoxymethyl, 1-methoxyethyl, 3-cyano-n-propyl, 3-chloro-n-propyl, phenyl, Tien-2-yl, Tien-3-yl; and the side chain amide alanovoy acid attached in position 3 of the pyridine ring.
18. The compound according to claim 1, in which Ar denotes a group of formula (C), in which And4denotes H; And5denotes H, halogen; R2denotes H; R3and R4both represent methyl; R5denotes H, methyl, hydroxymethyl, methoxymethyl, 1-methoxyethyl, 3-cyano-n-propyl, 3-chloro-n-propyl, phenyl, Tien-2-yl, Tien-3-yl;
and the side chain amide alanovoy acid attached in position of the pyridine ring.
19. The compound according to claim 1, in which Ar denotes a 5 - or 6-benzothiazolyl, not necessarily containing 2-s-Deputy, 5-(2,1-benzisothiazoles), optionally containing 3-With-Deputy, 6-benzoxazolyl, not necessarily containing 2-s-Deputy, 5-(2,1-benzisoxazoles), optionally containing 3-With-Deputy, 6-(1H-benzimidazolyl), not necessarily containing 2-C substituent and optionally containing N-C1-C4alkyl substituent, 5-(1H-indazole), optionally containing 3-C substituent and optionally containing N-C1-C4alkyl substituent, 6-(1,2,3-benzothiadiazole) or 6-(1,2,3-benzoxadiazole)where any of the above optional substituents selected from the group comprising halogen, C1-C4alkyl; R2denotes H; R3and R4both represent methyl; and R5denotes H, methyl, hydroxymethyl, methoxymethyl, 1-methoxyethyl, 3-cyano-n-propyl, 3-chloro-n-propyl, phenyl, Tien-2-yl.
20. Fungicidal composition comprising fungicide effective amount of the compounds of formula (1) according to claim 1 and a suitable carrier or diluent.
21. A method of combating phytopathogenic fungi or their destruction, which comprises applying to the plant, to seed of the plant, the locus of the plant or seed or to soil or any other medium in which the plant grows fungicide the effective amount of the compound according to claim 1.
FIELD: chemistry.
SUBSTANCE: invention concerns new compounds of the formula (I) and their pharmaceutically acceptable salts. The compounds claimed by the invention have inhibition effect on VR1 receptor activation and can be applied in pain prevention or treatment. In the general formula (I) , or
, L is a low alkylene, E cycle is benzene or 5-membered heteroaromatic ring containing sulfur atom as a heteroatom, D cycle is a monocyclic or bicyclic hydrocarbon cycle optionally condensed with C5-7 cycloalkyl, 6-membered monocyclic heteroaromatic cycle containing nitrogen atom as heteroatom or 9-11-membered bicyclic heteroaromatic cycle containing 1 to 3 equal or different heteroatoms selected out of the group including N, S and O, G cycle is a 5-7-membered monocyclic saturated or partially saturated heterocycle or 10-membered bicyclic heterocycle containing 1 to 3 equal or different heteroatoms selected out of the group including N, S and O. The invention also concerns pharmaceutical composition based on the said compounds, and application thereof in obtaining pain prevention or treatment medication, and a method of pain prevention or treatment.
EFFECT: obtaining prevention or treatment medium against pain.
24 cl, 470 ex, 41 tbl
FIELD: medicine; pharmacology.
SUBSTANCE: invention is related to the compounds of general formula (I) and their pharmaceutically acceptable salts with properties β2-adrenoreceptor agonists, to the method of their production and based on them pharmaceutical composition. The compounds can be used for treatment of conditions when the symptomatic severity can be reduced by β2- adrenoreceptor activation, e.g., obstructive or inflammatory respiratory diseases. In the general formula (I) , X means -R1-Ar-R2 or -Ra-Y; Ar means phenylen, optionally substituted by group of the row: halogen, hydroxy, C1-C10alkyl, C1-C10alcoxy, phenyl, C1-C10 alcoxy, substituted by phenyl group or phenyl, substituted by C1-C10 alcoxy group; R1 and R2 are bound to the adjacent carbon atoms within Ar group, and either R1 means C1-C10alkylen, and R2 means hydrogen, C1-C10alkyl or halogen, Ra means the bond or C1-C10 alkylen optionally substituted by group of the row: hydroxy, C1-C10 alcoxy, C6-C10aryl or C7-C14aralkyl; Y means C1-C10alkyl, or C2-C10alkynil, optionally substituted by hydroxyl group, C3-C10cycloalkyl, optionally condensed with one or more benzene rings and optionally substituted by group of the row: C1-C10alkyl, C1-C10alcoxy, C3-C10cycloalkyl, C7-C14aralkyl, C7-C14aralkyloxy or C6-C10aryl, where groups C7-C14aralkyl, C7-C14aralkyloxy or C6-C10 aryl are optionally substituted by group of the row: halogen, C1-C10alkyl, C1-C10alcoxy; C6-C10aryl, optionally substituted by group of the row: halogen, hydroxy, C1-C10alkyl, C1-C10alcoxy, C1-C10halogenalkyl, phenoxy, C1-C10alkylthio, C6-C10aryl, 5-6-term saturated heterocyclic ring, containing one nitrogen atom in cycle; phenoxy, optionally substituted by C1-C10alcoxy group; 5-6-term heterocyclic ring, containing one or two nitrogen or oxygen atoms in cycle, and the described heterocyclic ring is optionally substituted by group of the row: C1-C10alkyl, C6-C10aryl, C7-C14aralkyl, C1-C10alcoxycarbonil or 5-7-term heterocyclil (C1-C10)alkyl, containing one nitrogen atom in cycle; -NRdRe, where Rd means hydrogen or C1-C10alkyl, and Re means C1-C10alkyl, or Re means C6-C10aryl, or Re means 5-6-term heterocyclic ring, containing one nitrogen or sulfur atom in cycle, and the ring is optionally substituted by halogen-substituted phenyl group or Re means C6-C10arylsypfonil, optionally substituted by groups C1-C10alkylamino or di(C1-C10alkyl)amino; -SRf, where Rf means C6-C10aryl or C7-C14aralkyl, optionally substituted by group of row: halogen or C1-C10halogenalkyl; or -CONHRg, where Rg means C6-C10aryl, provided, if Ra means the bond, then Y doesn't mean C1-C5alkyl.
EFFECT: compound can prevent or reduce symptom's intensity.
15 cl, 4 tbl, 157 ex
FIELD: organic chemistry, chemical technology.
SUBSTANCE: invention relates to the improved method for synthesis of 2-cyano-6-methoxybenthiazole that is a key intermediate compound used in synthesis of luminescent biological systems, in particular, lupiferin. Method involves cyaniding reaction of 2-chloro-6-methoxybenzthiazole wherein acetonecyanohydrine is used as a cyaniding agent that is treated with alkaline metal alcoholate alcoholic solution, benzene is added and azeotropic mixture alcohol-benzene is distilled off followed by addition of dimethylsulfoxide and 2-chloro-6-methoxybenzthiazole. Method allows avoiding contact of workers with highly toxic cyanides and to obtain 2-cyano-6-methoxybenzthiazole with higher yield 50-50.8% as compared with the prototype (40%).
EFFECT: improved method of synthesis.
3 ex
< / BR>in which R3stands WITH1-C6alkyl or halogen; Q1denotes heteroaryl, which is optionally substituted by 1, 2, 3 or 4 substituents selected from the group comprising hydroxy, halogen, trifluoromethyl, cyano, amino, C1-C6alkyl, C2-C6alkenyl,2-C6quinil,1-C6alkoxy, etc., R2denotes hydroxy, halogen, C1-C6alkyl, C2-C6alkenyl,2-C6quinil,1-C6alkoxy, p = 0, 1, or 2; q = 0, 1, 2, 3 or 4; and Q2denotes aryl, aryl-C1-C6alkoxy, aryloxy, arylamino, N-C1-C6alkylamino, aryl-C1-C6alkylamino, cycloalkyl, heteroaryl, heteroallyl, heteroaryl-C1-C6alkylamino or heterocyclyl and so on, or its pharmaceutically acceptable salt or cleaved in vivo ester
2-adrenoreceptor" target="_blank">
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to novel anthranilic acid amides with a by-side heteroarylsulfonyl chain. Invention describes compounds of the formula (I): wherein R1 means compounds of formulae:
or
wherein A means -CnH2n- wherein n = 0, 1, 2, 3, 4 or 5; D means a bond or -O-; E means -CmH2m- wherein m = 0, 1, 2, 3, 4 or 5; R8 means hydrogen atom, alkyl with 1, 2, 3 or 4 carbon atoms or -CpH2p-R14 wherein p = 1, 2, 3, 4 or 5; R14 means phenyl or heteroaryl wherein phenyl and heteroaryl are unsubstituted or substituted with 1, 2 or 3 substitutes chosen from group consisting fluorine (F), chlorine (Cl), bromine (Br) and iodine (J) atom, alkyl with 1, 2, 3 or 4 carbon atoms; R9 means hydrogen atom or alkyl with 1, 2, 3, 4, 5 or 6 carbon atoms; R10 means hydrogen atom, alkyl with 1, 2, 3 or 4 carbon toms, phenyl, naphthyl or heteroaryl wherein phenyl, naphthyl and heteroaryl are unsubstituted or substituted with 1, 2 or 3 substitutes chosen from group consisting of F, Cl, Br, J, alkyl with 1, 2, 3 or 4 carbon atoms; R11 means cycloalkyl with 3, 4, 5 or 6 carbon atoms, phenyl, furyl, pyridyl, pyrazinyl wherein phenyl, furyl, pyridyl, pyrazinyl are unsubstituted or substituted with 1, 2 or 3 substitutes chosen from group consisting of F, Cl, Br, J, alkyl with 1, 2, 3 or 4 carbon atoms, alkoxy-group with 1, 2, 3 or 4 carbon atoms; R12 means alkyl with 1, 2, 3 or 4 carbon atoms, alkynyl with 1, 2, 3 or 4 carbon atoms, cycloalkyl with 3, 4, 5 or 6 carbon atoms, phenyl or heteroaryl; R13 means -CpH2p-R14 wherein p = 0, 1, 2, 3, 4 or 5; R15 means cycloalkyl with 3, 4, 5, 6, 7 or 8 carbon atoms; R2 means hydrogen atom; R3 means heteroaryl wherein heteroaryl is unsubstituted or substituted with 1, 2 or 3 substitutes chosen from group consisting of F, Cl, Br, J, alkyl with 1, 2, 3 or 4 carbon atoms; R4, R5, R6 and R7 mean independently of one another hydrogen atom, F, Cl, Br, J, alkyl with 1, 2, 3 or 4 carbon atoms, alkoxy-group with 1, 2, 3 or 4 carbon atoms, and their pharmaceutically acceptable salts also. Also, invention describes pharmaceutical composition containing compounds of the formula (I) possessing the effect blocking Kv1.5-channel. Proposed compounds can be used in treatment and prophylaxis of diseases mediated by K+-channel.
EFFECT: valuable medicinal property of compounds and pharmaceutical composition.
20 cl, 4 tbl, 70 ex
FIELD: organic chemistry, chemical technology.
SUBSTANCE: invention relates to a method for synthesis of benzofurazans by reduction of benzofuroxanes in ethylene glycol medium. Sulfur is used as a reducing agent and taken in the amount 0.5-1.0 g-atom per 1 g-mole of furoxane, and the process is carried out at temperature 140-155°C. Proposed method for reduction of benzofuroxanes with sulfur in ethylene glycol is safety and economy.
EFFECT: improved method of synthesis.
4 ex
FIELD: organic chemistry.
SUBSTANCE: invention relates to 5,7-disubstituted 4,6-dinitrobenzofuroxanes of the general formula (I): wherein R1 represents: 2-chlorophenylamino-group of the formula
, 2,5-dichlorophenylamino-group of the formula
, 4,5-dichlorophenylamino-group of the formula
, 2-hydroxyphenylamino-group of the formula
, 4-hydroxyphenylamino-group of the formula
, 4-bromophenylamino-group of the formula
, 2-methyl-5-chlorophenylamino-group of the formula
and 4-aminodiphenyl of the formula
that elicit acaricidal and bactericidal activity in low concentrations. These compounds can be used in veterinary science, medicine and agriculture.
EFFECT: valuable properties of compounds.
2 tbl, 5 ex
< / BR>or their salts, where in the formula Ia W represents N or C-CO-R, where R denotes HE OC1-C6alkyl or NR3R4where R3and R4- N or C1-C6alkyl, or formula Ib Az denotes imidazopyridine and in both formulas Ia and Ib R1represents C1-C4alkyl, R2denotes phenyl fragment or 2,5-cyclohexadiene-3,4-ridin-1 silt fragment
, 20-Olean-12-EN-29-OIC acid of the formula III, R4=H, R5--D-glucuronidase, R6=R7=H and R8= C(O)OH, or, if n= 7, R3=N, R4and R7- simple connection, R5and R6= H or (CH2CH(CH3)O)mH, where m=1 to 14, and R8=CH2OH or CH2O(CH2CH(CH3)O)mH, where m=1-14, generating nitric oxide and activating the soluble form of guanylate cyclase (RGC), antispasmodic, vasodilator and hypotensive means quick action and platelet aggregation inhibitors, method for their production and pharmaceutical compositions based on
< / BR>where-A= B-C= D - represents-CH=CH-CH=CH-group, in which 1 or 2 CH may be replaced by nitrogen;
Ar denotes phenyl or naphthyl, unsubstituted or one-, two - or three-fold substituted with H, Gal, Q, alkenyl with the number of C-atoms up to 6, Ph, OPh, NO2, NR4R5, NHCOR4, CF3, OCF3CN, OR4, COOR4, (CH2)nCOOR4, (CH2)nNR4R5, -N=C=O or NHCONR4R5phenyl or naphthyl;
R1, R2, R3each independently from each other, are absent or represent H, Gal, Q, CF3, NO2, NR4R5, CN, COOR4or CHCOR4;
R4, R5each independently of one another denote H or Q, or together also denote-CH2-(CH2)N-CH2-;
Q denotes alkyl with 1-6 C-atoms;
Ph denotes phenyl;
X denotes O or S;
Gal denotes F, Cl, Br or I;
"n" represents 1, 2 or 3;
and their salts, except 4-methyl-N-(2,1,3-benzothiadiazole - 5-yl)benzosulfimide, 4-nitro-N-(2,1,3-benzothiadiazole-5-yl)- benzosulfimide and 4-amino-N-(2,1,3-benzothiadiazole-5-yl)- benzolsulfonat
FIELD: pharmacology.
SUBSTANCE: refers to application of compounds of common formula 1 for production of medicinal agent for inhibition of cdc25-phosphatases and/or CD45- phosphatase, medicinal agent for inhibition of cdc25-phosphatases or CD45- phosphatase, pharmaceutical formulations for inhibition of cdc25-phosphatases or CD45-phosphatase; invention also refers to compounds of formula 1 and provides high-degree inhibition of cdc25-phosphatases and/or CD45- phosphatase.
EFFECT: high degree of inhibition.
22 cl, 1 dwg, 3 tbl, 131 ex
FIELD: organic chemistry, heterocyclic compounds, medicine.
SUBSTANCE: invention relates to derivatives of piperazine and piperidine of the formula (I): wherein ---Z represents =C or -N; Q means benzyl or 2-, 3- or 4-pyridylmethyl that can be substituted with one or more substitutes taken among group comprising halogen atom, cyano-group, (C1-C3)-alkoxy-group, CF3, OCF3, SCF3, (C1-C4)-alkyl, (C1-C3)-alkylsulfonyl and their salts, and to a method for their preparing also. It has been found that these compounds elicit valuable pharmacological properties owing to combination of (partial) agonism with respect to members of dopamine receptors subtype and affinity with respect to corresponding serotonin and/or noradrenergic receptors and can be useful in preparing compositions used in treatment of fear and/or depression or Parkinson's disease.
EFFECT: valuable medicinal properties of compounds.
7 cl, 1 tbl, 3 ex
