Aromatic compound

FIELD: chemistry.

SUBSTANCE: invention describes a novel compound of general formula (1), where radicals R1, R2, X1, Y and A are as described in claim 1 of the invention. The invention also describes a method of obtaining compounds of formula (1), as well as a pharmaceutical composition based on said compounds, for treating fibrosis.

EFFECT: novel compounds with excellent collagen formation suppression, cause fewer side-effects and which are safer are obtained.

62 cl, 2717 ex, 432 tbl

 

The text descriptions are given in facsimile form.

1. The aromatic compound represented by General formula (1), or its salt

[where X1represents a nitrogen atom or a group-CH=,
R1represents a group-Z-R6,
Z represents a group-N(R8)-B-, group-B-N(R8)-, group-In0-O -,

group-CO-, a group-CH(OH)-, group

group-N=CH-group

lower alkynylamino group, a group-NHCO-B1-, a group-NHCO-B2-(W)u-group-In0O19a-group

group

group

the group-S-, lower alkynylamino group, lower alkylenes group, group

or group
-CO-NH-B18a-
where R8represents a hydrogen atom, a lower alkyl group which may contain a lower alkoxygroup as a substituent, a lower alkanoyloxy group, phenyl-lower alkyl group or lower alkylsulfonyl group,
Represents a group-CO - or lower alkylenes group,
In0represents the lowest alkylenes group,
each of R9aand R9bthat are the same or different from each other, represents a hydrogen atom or a lower alkyl group,
R10ais the Wallpaper a hydrogen atom or a lower alkyl group,
In22Arepresents the lowest alkylenes group or lower alkynylamino group,
e is 0 or 1,
B1represents the lowest alkenylamine group which may contain a phenyl group as a substituent,
In2represents the lowest alkylenes group which may be substituted by a group selected from the group consisting of lower alkoxygroup and phenyl groups,
W represents an oxygen atom, a group-NH - or a sulfur atom,
u is 0 or 1,
B18arepresents the lowest alkylenes group,
B19arepresents the lowest alkylenes group,
In20Arepresents the lowest alkylenes group,
B21arepresents the lowest alkylenes group,
R8drepresents a hydrogen atom or a lower alkyl group,
k has a value of 2 or 3,
C has a value of 0 or 1,
d' is 0 or 1,
R10brepresents a hydrogen atom or a lower alkyl group,
R6represents a 5 to 15-membered monocyclic, bicyclic or tricyclic saturated or unsaturated heterocyclic group containing 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (where the heterocyclic ring may be substituted by 1-3 groups selected from the group comprising oxoprop; not necessarily galogenirovannami lower alkoxygroup; optionally halogenated lower alkyl group; a halogen atom; a lower alkylsulfonyl group; phenyl group which may be substituted in the phenyl ring optionally halogenated lower alkyl group; a lower allylthiourea; pyrrolidino group; benzoyloxy group; lower alkanoyloxy group; lower alkoxycarbonyl group; and amino group, which may contain as a substituent group selected from the group comprising lower alkyl group and lower alkanoyloxy group), adamantly group, naftalina group (where the naphthalene ring may be substituted by 1-3 groups selected from the group comprising lower alkyl group, halogen atom and an amino group, which may contain as a substituent group selected from the group comprising lower alkyl group and lower alkanoyloxy group), alkyl group which may contain a lower alkoxygroup as Deputy, cycloalkyl group which may be substituted in cycloalkene ring group selected from the group comprising amino-replaced lower alkyl group which may contain a lower alkyl group, amino group, lower alkyl group which may contain a halogen atom as a substituent, a lower alkenylphenol group which may contain a halo atom is s as Deputy, lower alkanoyloxy group, benzoyloxy group which may be substituted in the phenyl ring, 1-3 groups selected from the group comprising lower alkyl group which may contain a halogen atom as a substituent, and a halogen atom,

substituted by a halogen atom lower alkyl group or cycloalkyl-lower alkyl group,
R7represents a hydrogen atom, phenyl group, carboxypropyl, hydroxyl group, halogen atom, lower alkyl group which may contain a halogen atom as a substituent, fenoxaprop, lower alkoxygroup, which may contain a halogen atom as a substituent, a lower alkylenedioxy, the amino group, which may contain as a substituent group selected from the group comprising lower alkyl group, lower alkanoyloxy group, benzoyloxy group and cycloalkyl group, cyano, lower alkanoyloxy group which may contain a halogen atom as a substituent, a lower alkylsulfonyl group, aminosulfonyl group, lower alkoxycarbonyl group, lower alkanoyloxy, 5 - or 6-membered saturated or unsaturated heterocyclic group containing 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (where the heterocyclic collomore to be replaced by oxopropoxy) or group lowest alkoxycarbonyl-lower alkyl,
m is an integer having a value of from 1 to 5, where when m has a value of 2-5, from two to five groups of R7may be the same or different from each other,
R2represents a hydrogen atom, halogen atom or lower alkyl group,
Y represents a group-O-, a group-N(R5)-, group-CO-, a group-CH(OH)-, lower alkylenes group, a group-S(O)n - or a group-C(=N-OH)-,
R5represents a hydrogen atom, a lower alkyl group, lower alkanoyloxy group, benzoyloxy group, phenyl-lower alkyl group or cycloalkyl group,
n is 0, 1 or 2,
A represents a group

or group

p has a value of 1 or 2,
R3represents a hydrogen atom, a lower alkoxygroup, halogen atom, lower alkyl group which may contain a halogen atom as a substituent, a lower alkoxycarbonyl group, carboxypropyl, group
-CONR11R12or cyano,
where each of R11and R12that are the same or different from each other, represents a hydrogen atom, a lower alkyl group,
cycloalkyl group or phenyl group, or R11and R12together with the nitrogen atom to which they are attached, can communicate with each other is m directly or through a nitrogen atom, an oxygen atom or a sulfur atom with the formation of a 5-7-membered saturated heterocyclic ring, R4represents a group -(T)1-N(R14R15,
T represents a lower alkylenes group, a group-N(R17)-B3-CO-, a group-B19-N(R18)-CO-, a group-In4-CO-, a group-Q-B5-CO-, a group-B6-N(R19)7-CO-, a group-CO-B8-, a group-CH(OH)-IN9-, a group-CO10-CO-, a group-CH(OH)-IN11-CO-, a group-CO-, a group-SO2- or group-In23a-CO-CO-,
where R17represents a hydrogen atom, a lower alkyl group, cycloalkyl group, cycloalkylcarbonyl group, lower alkanoyloxy group which may contain a halogen atom as a substituent, a lower alkenylphenol group, aminosilane lower alkanoyloxy group which may contain a lower alkyl group as a substituent, or a lower alkylsulfonyl group,
In3represents the lowest alkylenes group,
In19represents the lowest alkylenes group,
R18represents a hydrogen atom or a lower alkyl group,
In4represents the lowest alkenylamine group or lower alkylenes group which may contain a hydroxyl group as a substituent,
Q represents an oxygen atom, Il is a group-S(O) n- (where n has the values defined above),
In5represents the lowest alkylenes group,
B6represents the lowest alkylenes group,
R19represents a hydrogen atom or a lower alkanoyloxy group,
B7represents the lowest alkylenes group,
B8represents the lowest alkylenes group,
In9represents the lowest alkylenes group,
In10represents the lowest alkylenes group,
In11represents the lowest alkylenes group,
In23arepresents the lowest alkylenes group,
l is 0 or 1,
R14and R15together with the nitrogen atom to which they are attached, can communicate with each other directly or via a nitrogen atom, an oxygen atom or a sulfur atom with the formation of 5-to 10-membered saturated or unsaturated heterocyclic ring; or a group

where the heterocyclic ring may be substituted by 1-3 groups selected from the group comprising (28) phenylseleno lower alkyl group which contains 1-2 phenyl groups and which can contain pyridyloxy group lower alkyl group, where the phenyl ring may be substituted by 1-3 groups selected from the group comprising lower alkanoyloxy group, amino group, which the traveler may contain lower alkanoyloxy group as substituent, lower alkoxycarbonyl group, a cyano, a nitro-group, phenyl group, halogen atom, lower alkyl group which may contain a halogen atom as a substituent, a lower alkoxygroup, which may contain a halogen atom as a substituent, a phenyl-lower alkoxygroup, a hydroxyl group and a lower alkylenedioxy, (29) karbamoilnuyu group, (30) pyridyl-lower alkyl group, which may contain as Deputy(deputies) in the pyridine ring, 1-3 groups selected from the group comprising a hydroxyl group and a lower alkyl group which may contain a hydroxyl group as Deputy, (31) pyrrolyl-lower alkyl group which may contain 1-3 lower alkyl groups as a Deputy(deputies) in pyrrole ring, (32) benzoxazolyl-lower alkyl group, (33) benzothiazolyl-lower alkyl group, (34) furyl-lower alkyl group, (35) benzoyloxy group which may be substituted in the phenyl ring, 1-3 groups selected from the group of cyano, amino group, which may contain lower alkylsulfonyl group as a substituent, a halogen atom, a lower alkoxygroup, a lower alkyl group, which may contain a halogen atom as a substituent, diazolidinyl-lower alkyl group, the which may contain oxoprop as Deputy in thiazolidinone ring, thiazolidinone-lower alkyl group which may contain oxoprop as Deputy in thiazolidinones the ring, and the lower alkylenedioxy, (36) pyrimidinyl group, (37) personilnya group, (38) pyridyloxy group, (39) lower alkoxycarbonyl group, (40) diazolidinyl lowest alkanoyloxy group which may be substituted in thiazolidinone ring group selected from the group consisting of a carbonyl group and groups

(where each of Raand Rbrepresents a lower alkyl group), (41) a lower alkyl group which may contain a group selected from the group comprising a hydroxyl group and halogen atom as a substituent, (42) lower alkanoyloxy group which may contain a halogen atom as a substituent, (43) phenyl group which may be substituted in the phenyl ring, 1-3 groups selected from the group comprising carbamoyl group which may contain a group selected from the group consisting of lower alkoxy-lower alkyl groups and lower alkyl groups, lower alkoxycarbonyl group, carboxypropyl, cyano, phenyl group, halogen atom, lower alkyl group which may contain a halogen atom as a substituent, a lower alkoxygroup, which may contain a halogen atom in the when asked Deputy, benzoyloxy group which may contain a halogen atom as a substituent in the phenyl ring, phenyl-lower alkyl group which may contain a halogen atom as a substituent in the phenyl ring, and a hydroxyl group, (44) phenyl group, which may contain lower alkylenedioxy as a substituent in the phenyl ring, (45) naphthyl-lower alkyl group, (46) fenoxaprop, which can be substituted in the phenyl ring, 1-3 groups selected from the group of cyano, lower alkyl group which may contain a halogen atom as a substituent, and the lower alkoxygroup, which may contain a halogen atom as a substituent, (47) phenoxy-lower alkyl group, (48) phenyl-lower alkoxygroup, which can be substituted in the phenyl ring, 1-3 groups selected from the group comprising halogen atom, a lower alkyl group which may contain a halogen atom as a substituent, and a lower alkoxygroup, which may contain a halogen atom as a substituent, (49) group(B12CO)t-N(R20R21, (50) a group -(CO)about-B13-N(R22R23, (51) 1,2,3,4-tetrahydronaphthyl-substituted lower alkyl group which may be substituted in 1,2,3,4-tetrahydronaphthalene ring 1-5 lower alkyl groups as the of " (Deputy), (52) cycloalkyl group which may contain a hydroxyl group as a substituent, (53) piperidinyloxy group which may be substituted in piperidinium ring 1-3 lower alkyl groups as a Deputy(deputies), (54) chinolin-lower alkyl group, (55) 1,2,3,4-tetrazolyl-lower alkyl group which may contain a group selected from the group comprising lower alkyl group and a phenyl-lower alkyl group as a substituent tetrazolium the ring (56) thiazolyl-lower alkyl group which may contain a phenyl group in as Deputy to the thiazole ring (57) benzoyl-lower alkyl group which may contain 1-3 groups selected from the group consisting of lower alkoxygroup and halogen atom as a Deputy(deputies) in the phenyl ring, (58) piperidinyl-lower alkyl group which may contain a lower alkyl group as a substituent piperidinium ring, (59) imidazolidinyl group, which may contain 1-3 phenyl groups as a Deputy(deputies) in the imidazole ring (60) benzimidazolyl group, which may contain 1-3 lower alkyl groups as Deputy(deputies) benzimidazole ring, (61) pyridyl-lower alkoxygroup, (62) 1,2,3,4-tetrahydroquinolin-lower alkyl gr the PPU, which may contain oxoprop as Deputy in tetrahydroquinolines ring (63) 1,3,4-oxadiazolyl-lower alkyl group which may contain oxoprop as Deputy in 1,3,4-oxadiazole ring (64) cycloalkyl-lower alkyl group, (65) tetrahydropyranyloxy group, (66) thienyl-lower alkyl group, (67) pyrimidinecarbonitrile group which may contain oxoprop as Deputy in the pyrimidine ring (68) hydroxyl group, (69) carboxypropyl, (70) a lower alkoxy-lower alkyl group, (71) lower alkoxy-lower alkoxygroup, (72) benzoyloxy, (73) the lowest alkoxycarbonyl-lower alkoxygroup, (74) carboxy-lower alkoxygroup, (75) phenoxy lowest alkanoyloxy group, (76) 1,2,3,4-tetrahydroisoquinoline group which may contain oxoprop as Deputy in tetrahydroquinolines the ring (77) phenylsulfonyl group, (78) imidazolyl lowest alkanoyloxy group, (79) imidazolyl-lower alkyl group, (80) pyridylcarbonyl group, (81) imidazoledicarbonitrile group, (82) group low alkoxycarbonyl-lower alkyl, (83) carboxy-lower alkyl group, (84) a group -(O-B15)s-CO-N(R26R27, (85) the group-N(R28)-CO-B16-N(R29R30, (86) the group-N(R31)-B17-CO-N(R32R33, (87) benzoxazolyl group is, (A) benzothiazoline group, (89a) oxoprop and (90A) 1,2,3,4-tetrahydroquinoline group which may contain oxoprop as Deputy in tetrahydroquinolines ring,
In12represents the lowest alkylenes group,
t is 0 or 1,
each of R20and R21that are the same or different from each other, represents a hydrogen atom; cycloalkyl group;
the amino group, which may contain lower alkoxycarbonyl group as a substituent; benzoyloxy group, which may contain 1-3 low alkoxygroup as Deputy(deputies) in the phenyl ring; a lower alkyl group; a lower alkyl group containing 1-2 phenyl group which may be substituted in the phenyl ring, 1-3 groups selected from the group comprising lower alkoxycarbonyl group, a cyano, a nitro-group, phenyl group, halogen atom, lower alkyl group which may contain a halogen atom as a substituent, a lower alkoxygroup, which may contain a halogen atom as a substituent, and a lower allylthiourea; phenyl group which may be substituted in the phenyl ring, 1-3 groups selected from the group comprising lower alkoxygroup, which may contain a halogen atom as a substituent, and the lower lilou group, which may contain a halogen atom as a substituent; a lower alkoxycarbonyl group; cycloalkyl-lower alkyl group; pyrrolidinyl-lower alkyl group which may contain 1-3 lower alkyl groups, which may contain a hydroxyl group as a substituent in the pyrolidine ring; aminosilane lower alkyl group which may contain a group selected from the group including a phenyl group and lower alkyl group as a substituent; 1,2,3,4-tetrahydronaphthyl-substituted lower alkyl group, which may contain 1-5 lower alkyl groups as a Deputy(deputies) of 1,2,3,4-tetrahydronaphthalene ring; naphthyl-lower alkyl group; a pyridyl-lower alkyl group; chinolin-lower alkyl group; 1,2,3,4-tetrazolyl-lower alkyl group which may contain 1-3 groups selected from the group comprising lower alkyl group and a phenyl-lower alkyl group as a Deputy(deputies) in tetrazole ring; 1,2,4-triazolyl-lower alkyl group; tetrahydrofuryl-lower alkyl group which may contain a hydroxyl group as a substituent a lower alkyl group; phenoxy-lower alkyl group which may contain 1-3 groups selected from the group comprising lower alkyl group and neither is regroupe as Deputy(deputies) in the phenyl ring; phenyl-lower alkanoyloxy group; lower alkanoyloxy group which may contain a halogen atom as a substituent; imidazolyl lowest alkanoyloxy group; a group of the lowest alkoxycarbonyl-lower alkyl; pyridyloxy group; or a carboxy-lower alkyl group, or R20and R21together with the nitrogen atom to which they are attached, can communicate with each other directly or via a nitrogen atom, an oxygen atom or a sulfur atom with the formation of a 5-7-membered saturated heterocyclic ring, where the heterocyclic ring may be substituted by 1-3 groups selected from the group comprising lower alkyl group, phenyl group, which may contain 1-3 groups selected from the group consisting of a halogen atom and a lower alkyl group which may contain a halogen atom as a Deputy(deputies) in the phenyl ring, phenyl-lower alkyl group which may contain the lower alkylenedioxy as a substituent in the phenyl ring, o is 0 or 1,
In13represents the lowest alkylenes group,
each of R22and R23that are the same or different from each other, represents a hydrogen atom, a lower alkyl group, benzoyloxy group, which may contain 1-3 low alkoxygroup as the Deputy is(Deputy) in the phenyl ring, phenoxy-lower alkyl group which may contain a lower alkyl group as a substituent in the phenyl ring, phenyl-lower alkyl group or phenyl group, or R22and R23together with the nitrogen atom to which they are attached, can communicate with each other directly or via a nitrogen atom, an oxygen atom or a sulfur atom with the formation of a 5-7-membered saturated heterocyclic ring, where the heterocyclic ring may be substituted by 1-3 groups selected from the group consisting of lower alkyl groups and phenyl-lower alkyl group which may contain a lower alkylenedioxy as a substituent in the phenyl ring,
In15represents the lowest alkylenes group,
s is 0 or 1,
each of R26and R27that are the same or different from each other, represents a hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group or imidazolyl-lower alkyl group, or R26and R27together with the nitrogen atom to which they are attached, can communicate with each other directly or via a nitrogen atom, an oxygen atom or a sulfur atom with the formation of a 5-7-membered saturated heterocyclic ring, where the heterocyclic ring may be substituted by 1-3 phenyl-lower alkyl groups in which the number of Deputy(deputies), which may contain lower alkylenedioxy as a substituent in the phenyl ring,
R28represents a hydrogen atom or a lower alkyl group,
In16represents the lowest alkylenes group,
R29and R30together with the nitrogen atom to which they are attached, can communicate with each other directly or via a nitrogen atom, an oxygen atom or a sulfur atom with the formation of a 5-7-membered saturated heterocyclic group, where the heterocyclic ring may be substituted by 1-3 groups selected from the group comprising lower alkyl group, phenyl group and phenyl-lower alkyl group which may contain a lower alkylenedioxy as a substituent in the phenyl ring,
R31represents a hydrogen atom or a lower alkyl group,
In17represents the lowest alkylenes group,
R32and R33together with the nitrogen atom to which they are attached, can communicate with each other directly or via a nitrogen atom, an oxygen atom or a sulfur atom with the formation of a 5-7-membered saturated heterocyclic group, where the heterocyclic ring may be substituted by 1-3 groups selected from the group comprising lower alkyl group, phenyl group and phenyl-lower alkyl group which may contain lower and is calendarscope as a substituent in the phenyl ring,
provided that the above described aromatic compound or its salt satisfy the following requirements (i)-(ii):
(i) when X1represents a group-CH=, then R3represents a hydrogen atom;
(ii) when X1represents a group-CH=, l has a value of 1, and T
represents-N(R17)3-CO-, then R14and R15together with the nitrogen atom to which they are attached, can communicate with each other directly or via a nitrogen atom, an oxygen atom or a sulfur atom with the formation of 5-to 10-membered saturated or unsaturated heterocyclic ring, where the heterocyclic ring is substituted with 1-3 groups (28)described above].

2. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formulas (1-1)to(1-7):



[where in the above General formulas (1-1)to(1-7) R6,, R8, R2, R5n, X1and a have the meanings indicated in claim 1 and Y3represents the lowest alkylenes group].

3. Aromatic compound or with the ü according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-8)-(1-14):



[where in the above General formulas (1-8)-(1-14) R6,, R8, R2, R5n, X1and a have the meanings indicated in claim 1, and Y3matter specified in paragraph 2].

4. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-15)-(1-21):



[where in the above General formulas (1-15)-(1-21) R6In0, R2, R5n, X1and a have the meanings indicated in claim 1, and Y3matter specified in paragraph 2].

5. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-22)-(1-28):



[where in the above General formulas (1-22)-(1-28) R6, R2, R5n, X1and a have the meanings indicated in claim 1, and Y3matter specified in paragraph 2].

6. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-29)-(1-35):



[where in the above General formulas (1-29)-(1-35) R6, R2, R5n, X1and a have the meanings indicated in claim 1, and Y3matter specified in paragraph 2].

7. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-36)-(1-42):



[where indicated in the data of the General formulas (1-36)-(1-42) R 6, R2, R5n, X1and a have the meanings indicated in claim 1, and Y3matter specified in paragraph 2].

8. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-43)-(1-49):



[where in the above General formulas (1-43)-(1-49) R6, R2, R5n, X1, A, R9aand R9bhave the meanings indicated in claim 1, and Y3matter specified in paragraph 2].

9. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-50)-(1-56):



[where in the above General formulas (1-50)-(1-56) R6, R2, R5n, X1and a have the meanings indicated in claim 1, and Y3matter specified in paragraph 2].

10. Aromatic compound or its salt according to claim 1, where the connection represented by the General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-57)-(1-63):




[where in the above General formulas (1-57)-(1-63) R6, R2, R5n, X1, A, R10aB22aand e have the meanings indicated in claim 1, and Y3matter specified in paragraph 2].

11. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-64)-(1-70):



[where in the above General formulas (1-64)-(1-70) R6, R2, R5n, X1and a have the meanings indicated in claim 1, and Y3matter specified in paragraph 2, and Z1represents the lowest alkenylamine group].

12. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group VK is ycause the following General formula (1-71)-(1-77):



[where in the above General formulas (1-71)-(1-77) R6, R2B1, R5n, X1and A have the meanings indicated in claim 1, and Y3matter specified in paragraph 2].

13. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-78)-(1-84):



[where in the above General formulas (1-78)-(1-84) R6, W, u, V2, R2, R5n, X1and a have the meanings indicated in claim 1, and Y3matter specified in paragraph 2].

14. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-85)-(1-91):




[where in the above General formulas (1-85)-(1-91) R5, R6B19aIn0, R2X1, n and a have the meanings indicated in claim 1, and Y3matter specified in paragraph 2].

15. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-92)-(1-98):




[where in the above General formulas (1-92)-(1-98) R5, R6In20A, R2X1, A, n, d' and k have the meanings specified in claim 1, and Y3matter specified in paragraph 2].

16. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-99)-(1-105):




[where in the above General formulas (1-99)-(1-105) R6, R5B21a, R2X1, A, n and C have meant what I specified in claim 1, and Y3matter specified in paragraph 2].

17. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-106)-(1-112):




[where in the above General formulas (1-106)-(1-112) R5, n, R6, R10bX1, R2and a have the meanings indicated in claim 1, and Y3matter specified in paragraph 2].

18. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-113)-(1-119):



[where in the above General formulas (1-113)-(1-119) R6, R2X1, R5, n and a have the meanings indicated in claim 1, and Y3matter specified in paragraph 2].

19. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1), the Chairman shall place any of the compounds, selected from the group comprising the following General formula (1-120)-(1-126):



[where in the above General formulas (1-120)-(1-126) R6, R2X1And R5and n have the meanings indicated in claim 1, Y3matter specified in paragraph 2, and Z2represents the lowest alkynylamino group].

20. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-127)-(1-133):




[where in the above General formulas (1-127)-(1-133) R6B18a, R2X1, A, R5and n have the meanings indicated in claim 1, and Y3matter specified in paragraph 2].

21. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-134)-(1-140):



[where in the above General formulas (1-134)-(1-140) R6, R2X1, A, R5and n have the meanings indicated in claim 1, Y3matter specified in paragraph 2, and Z3represents the lowest alkylenes group or the group(R8dmatter specified in claim 1)].

22. Aromatic compound or its salt according to any one of claims 1 to 21, where Y represents a group-O-.

23. Aromatic compound or its salt according to any one of claims 1 to 21, where Y represents a group-N(R5)- (R5matter specified in item 1).

24. Aromatic compound or its salt according to any one of claims 1 to 21, where Y represents a group-CO-, a group-CH(OH)-, lower alkylenes group, a group-S(O)n- (n has the values specified in claim 1) or a group-C(=N-OH)-.

25. Aromatic compound or its salt according to any one of claims 1 to 21, where a represents a group

(R3, R4and p have the meanings stated in claim 1).

26. Aromatic compound or its salt according to any one of claims 1 to 21, where a represents a group

(R4matter specified in item 1).

27. Aromatic compound or its salt according to any one of claims 1 to 21, the de R 4represents a group -(T)1-N(R14R15(T, R14and R15have the meanings indicated in claim 1), and 1 is set to 0.

28. Aromatic compound or its salt according to any one of claims 1 to 21, where R4represents a group -(T)1-N(R14R15(T, R14and R15have the meanings indicated in claim 1), and 1 is set to 1.

29. Aromatic compound or its salt according to any one of claims 1 to 21, where R4represents a group -(T)1-N(R14R15,1 is set to 1, and T represents a group-N(R17)3-CO- (R14, R15, R17and In3have the meanings indicated in claim 1).

30. Aromatic compound or its salt according to any one of claims 1 to 21, where R4represents a group -(T)1-N(R14R15,1 is set to 1, and T represents a group-B19-N(R18)-CO- (R14, R15B19and R18have the meanings indicated in claim 1).

31. Aromatic compound or its salt according to any one of claims 1 to 21, where R4represents a group -(T)1-N(R14R15, 1 is set to 1, and T is a group-In4-CO- (R14, R15and In4have the meanings indicated in claim 1).

32. Aromatic compound or its salt according to any one of claims 1 to 21, where R4represents a group -(T)1-N(R14R15, 1 is set to 1, and T p is ecstasy a group-Q-B 5-CO- (R14, R15, Q5have the meanings indicated in claim 1).

33. Aromatic compound or its salt according to any one of claims 1 to 21, where R4represents a group -(T)1-N(R14R15, 1 is set to 1, and T is a group-In6-N(R19)-B7- (R14, R15In6, R19and In7have the meanings indicated in claim 1).

34. Aromatic compound or its salt according to any one of claims 1 to 21, where R4represents a group -(T)1-N(R14R15, 1 is set to 1, and T represents a group-CO-B8- (R14, R15and B8have the meanings indicated in claim 1).

35. Aromatic compound or its salt according to any one of claims 1 to 21, where R4represents a group -(T)1-N(R14R15, 1 is set to 1, and T represents a group-CH(OH)-IN9- (R14, R15and In9have the meanings indicated in claim 1).

36. Aromatic compound or its salt according to any one of claims 1 to 21, where R4represents a group -(T)1-N(R14R15, 1 is set to 1, and T represents a group-CO10-CO- (R14, R15and In10have the meanings indicated in claim 1).

37. Aromatic compound or its salt according to any one of claims 1 to 21, where R4represents a group -(T)1-N(R14R15, 1 is set to 1, and T is the Wallpaper group-CH(OH)-IN 11-CO- (R14, R15and In11have the meanings indicated in claim 1).

38. Aromatic compound or its salt according to any one of claims 1 to 21, where R4represents a group -(T)1-N(R14R15, 1 is set to 1, and T represents a group-CO- (R14and R15have the meanings indicated in claim 1).

39. Aromatic compound or its salt according to any one of claims 1 to 21, where R4represents a group -(T)1-N(R14R15, 1 is set to 1, and T is a group-SO2- (R14and R15have the meanings indicated in claim 1).

40. Aromatic compound or its salt according to any one of claims 1 to 21, where R4represents a group -(T)1-N(R14R15, 1 is set to 1, and T is a group-In23a-CO-CO- (R14, R15and In23ahave the meanings indicated in claim 1).

41. Aromatic compound or its salt according to any one of claims 1 to 21, where R4represents a group -(T)1-N(R14R15, 1 is set to 1, and T represents the lowest alkylenes group (R14and R15have the meanings indicated in claim 1).

42. Aromatic compound or its salt according to claim 1, where the compound represented by General formula (1)represents any one of the compounds selected from the group comprising the following General formula (1-1), (1-2), (1-8), (1-9), (1-15), (1-16), (1-29), (1-30), (1-43), (1-44),(1-57), (1-58), (1-64) and (1-65)as defined in claim 2, 3, 4, 6, 8, 10 and 11, And represents a group

(R3, R4and p have the meanings indicated in claim 1 and R4represents a group
-(T)1-N(R14R15(T, l, R14and R15have the meanings indicated in claim 1).

43. Aromatic compound or its salt according to § 42, where 1 is set to l, and T represents a group-N(R17)3-CO- (R17and In3have the meanings indicated in claim 1).

44. Aromatic compound or its salt according to § 42, where 1 is 1, and T is a group-In4-CO - (4matter specified in item 1).

45. Aromatic compound or its salt according to § 42, where 1 is 1, and T represents a group-CO-.

46. Aromatic compound or its salt according to § 42, where 1 is set to 0.

47. Aromatic compound or its salt according to § 42, where 5-10-membered saturated or unsaturated heterocyclic group formed by linking R14and R15together with the nitrogen atom to which they are attached, directly or via a nitrogen atom, an oxygen atom or a sulfur atom, a represents any group selected from 1,2,3,4,5,6-hexahydropyridine, pyrrolidinyloxy, piperidinyloxy, piperazinilnom, morpholino, thiomorpholine, homopiperazine, homopiperazine, thiazole enilno, 1,2,5,6-tetrahydropyridine, pyrrolidino, pyrazolidine, imidazolidine, 2-pyrrolidine, 2-imidazolidone, imidazolidinyl, 2-pyrazolinone, pyrazolidinone, 1,2-dihydropyridine, 1,2-dihydroquinoline, 1,2,3,4-tetrahydroquinoline, 1,2,3,4-tetrahydroisoquinoline, 1,2-dihydroisoquinolines, indolines, isoindolines, indolenines, isoindolines, 3,4-dihydro-2H-1,4-benzoxazinones, 3,4-dihydro-2H-1,4-benzothiazolinone, 1,4-benzothiazepines, 1,2,3,4-tetrahydroisoquinoline, 1,2,3,4-tetrahydrocannabinol, 1,2,3,4-tetrahydroquinoline, 1,2,3,4-tetrahydroquinazoline, 1,2-dihydroisoquinolines, 3,4-dihydroisoquinolines, 1,4-dihydroquinoxaline, 1,2-dihydrosanguinarine, 1,2-dihydropteridine, 3,4-dihydropteridine, 1,2-dihydroquinazolines, 3,4-dihydroquinazolines, indazolinone, indazolinone, 6-azabicyclo[3,2,1]octiles, 3-Aza-Spiro[5,5]undecylenoyl and thiazolidinones group.

48. Aromatic compound or its salt p, where 5-10-membered saturated or unsaturated heterocyclic group formed by linking R14and R15together with the nitrogen atom to which they are attached, directly or via a nitrogen atom, an oxygen atom or a sulfur atom, a represents any group selected from piperidinyl group or piperazinilnom group is s.

49. Aromatic compound or its salt p where piperidinyl group or piperazinilnom group may be substituted by (28) phenyl-substituted lower alkyl group that contains 1-2 phenyl groups and which can contain pyridyloxy group lower alkyl group, where the phenyl ring may be substituted by 1-3 groups selected from the group comprising lower alkanoyloxy group, amino group, which may contain lower alkanoyloxy group as a substituent, a lower alkoxycarbonyl group, a cyano, a nitro-group, phenyl group, halogen atom, lower alkyl group which may contain a halogen atom as a substituent, the lower alkoxygroup, which may contain a halogen atom as a substituent, a phenyl-lower alkoxygroup, a hydroxyl group and a lower alkylenedioxy.

50. Aromatic compound selected from the group including:
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]ethylamino}-2-methoxyphenoxy)pyridine-3-yl]-3,4-dichlorobenzamide,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]ethylamino}phenoxy)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]ethylamino}-2-pertenece)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]methylamino}-2-pertenece)pyridine-3-yl]-4-triptime ylbenzene,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]methylamino}-2-methoxyphenoxy)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]ethylamino}-2-methoxyphenoxy)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]ethylamino}-2-methylphenoxy)pyridine-3-yl]-3,4-dichlorobenzamide,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]methylamino}-2-methylphenoxy)pyridine-3-yl]-4-cryptomelane,
N-(6-{4-[3-(4-piperonylpiperazine-1-yl)-3-oxopropyl]phenoxy}pyridine-3-yl)-3,4-dichlorobenzenesulfonate,
N-[6-(4-{4-[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]piperazine-1-yl}phenoxy)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{4-[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}phenoxy)pyridine-3-yl]-4-cryptomelane,
N-{6-[(4-{4-[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}phenyl)methylamino]pyridine-3-yl}-4-cryptomelane,
N-[6-(4-{4-[2-(4-benzylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}-2-methylphenoxy)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{4-[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}-2-methylphenoxy)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{4-[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}-2-methylphenoxy)pyridine-3-yl]-3,4-dichlorobenzamide,
N-{6-[4-(4-benzylpiperazine-1-carbonyl)phenoxy]pyridine-3-yl}-4-cryptomelane,
N-{6-[4-(4-benzylpiperazine-1-carbonyl)phenoxypyridine-3-yl}-3,4-dichlorobenzamide,
N-[6-({4-[3-(4-piperonylpiperazine-1-yl)-3-oxopropyl]phenyl}methylamino)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]ethylamino}-2-pertenece)pyridine-3-yl]-3,4-dichlorobenzamide,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]methylamino}-2-pertenece)pyridine-3-yl]-3,4-dichlorobenzamide,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]methylamino}-2-methoxyphenoxy)pyridine-3-yl]-3,4-dichlorobenzamide,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]methylamino}phenoxy)pyridine-3-yl]-3,4-dichlorobenzamide,
1-(6-{4-[3-(4-piperonylpiperazine-1-yl)-3-oxopropyl]phenoxy}pyridine-3-yl)-3-(3,4-dichlorophenyl)-1-atilmotin,
N-(6-{4-[3-(4-piperonylpiperazine-1-yl)-3-oxopropyl]phenoxy}pyridine-3-yl)-4-cryptomelane,
N-[6-(4-{[2-(4-benzylpiperazine-1-yl)-2-oxoethyl]methylamino}-2-methylphenoxy)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{4-[2-(4-benzylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}phenoxy)pyridine-3-yl]-3,4-dichlorobenzamide,
N-(6-{4-[3-(4-piperonylpiperazine-1-carbonyl)piperidine-1-yl]phenoxy}pyridine-3-yl)-3,4-dichlorobenzamide,
N-[6-(4-{4-[2-(4-benzylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}phenoxy)pyridine-3-yl]-4-cryptomelane,
N-{6-[(4-{4-[2-(4-benzylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}phenyl)methylamino]pyridine-3-yl}-4-cryptomelane,
N-(6-{4-[(2-{4-[4-(4-perbenzoic)phenyl]piperazine-1-yl}-2-oxoethyl)methylamino]-2-methoxyphenoxy}pyridine-3-yl-4-cryptomelane,
2-(4-piperonylpiperazine-1-yl)-N-{3-methyl-4-[5-(4-triftormetilfullerenov)pyridine-2-yloxy]phenyl}-2-oxoacetate,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]methylamino}-2-methylphenoxy)pyridine-3-yl]-2-fluoro-4-cryptomelane,
N-[6-(4-{4-[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}-2-methoxyphenoxy)pyridine-3-yl]-4-cryptomelane and
ethyl ester of 4-(3-{3-methyl-4-[5-(4-triphtalocyaninine)pyridine-2-yloxy]phenyl}-2-oxohexanoate-1-yl)benzoic acid
or their salts.

51. The method of obtaining aromatic compounds according to claim 1, comprising a step for compound (1A) by the following formula reaction 1:
[formula reactions 1]

where X1, R1, R2and a have the meanings defined in claim 1,
Y1represents-O - group, -S - group or a-NH group, and X2represents a halogen atom.

52. The method of obtaining aromatic compounds according to claim 1, comprising a step for connection (lqq) according to the following formula reactions 14:
[formula reactions 14]

where R2X1, Y, R14and R15have the meanings defined in claim 1,
And10represents a group of the formula
or
where R3and p have the meanings defined in claim 1, provided that in compounds (37) is (lqq), a and b within the A10associated with Y and T2respectively, and R95is an R1or halogen atom,
T2represents a group-N(R17)-B3-, group-B19-N(R18)-, group-In4-, a group-Q-B5-, group-B6-N(R19)-B7-, a group-CO10-, a group-CH(OH)-IN11-group
In23a-CO - or a direct link, where R17In3B19, R18B4In5In6, R19B7In10and In11In23ahave the meanings given in claim 1.

53. The method of obtaining aromatic compounds according to claim 1, comprising a step for connection 1x according to the following formula reactions 37-1:
[formula reactions 37-1]

where R2X1, R6, R8and Y have the meanings defined in claim 1,
X2has the meaning given in § 51,
B21represents the lowest alkylenes group,
And16represents a group-a or group-A10-T2-COOP59awhere A10and T2have the meanings given in paragraph 52, and R59arepresents a hydrogen atom or a lower alkyl group.

54. The method of obtaining aromatic compounds according to claim 1, comprising a step for connection 1y by the following formula reaction 37-2:
[Formula reactions 37-2]

DG is R 2X1, R6, R8and Y have the meanings defined in claim 1, B21represents the lowest alkylenes group,
A16represents a group-a or group-A10-T2-COOR59awhere a10and T2have the meanings given in paragraph 52, and R59arepresents a hydrogen atom or a lower alkyl group,
RArepresents a hydrogen atom or a lower alkyl group, provided that the fragment B21CHRAin the group (R6-B21CHRA-) in the compound (1y) contains not more than 6 carbon atoms.

55. The method of obtaining aromatic compounds according to claim 1, comprising a step for connection 1z according to the following formula reactions 37-3:
[formula reactions 37-3]

where R2X1, R6, R8and Y have the meanings defined in claim 1,
A16represents a group-a or group-A10-T2-COOR59awhere A10and T2have the meanings given in paragraph 52, and R59arepresents a hydrogen atom or a lower alkyl group.

56. The method of obtaining aromatic compounds according to claim 1, comprising a step for connection (72b) according to the following formula reactions 48-1:
[formula reactions 48-1]

where R2X1, Y3, R14and R15have the meanings defined the military in claim 1;
A10has the meaning given in paragraph 52;
X2has the meaning given in § 51;
R74arepresents a nitro group or a group-R1and R1has the meaning given in claim 1,
Rcrepresents a group-CONR14R15or a group-COOR59b, R59brepresents a lower alkyl group or phenyl-lower alkyl group; and
R17arepresents a lower alkyl group, cycloalkyl group, lower alkyl-sulfonyloxy group or lower alkenylphenol group;
moreover, in the composition (a) is associated with a group Y, and b is associated with a group-NHB3-Rcor a group-N(R17a)B3-Rc.

57. The method of obtaining aromatic compounds according to claim 1, comprising a step for connection (72s) according to the following formula reactions 48-2:
[formula reactions 48-2]

where R2X1, Y3, R14and R15have the meanings given in claim 1;
A10has the meaning given in paragraph 52;
RAhas the meaning given in item 54;
R74arepresents a nitro group or a group-R1and R1has the meaning given in claim 1,
Rcrepresents a group-CONR14R15or a group-COOR59b, R59brepresents a lower alkyl group or phenyl-lower alkyl group; and
R 17brepresents a hydrogen atom or a lower alkyl group;
moreover, in the composition And10linked to the group Y and b associated with the group-NHB3-Rcor a group-N(CH(RA)(R17b))B3-Rc.

58. The method of obtaining aromatic compounds according to claim 1, comprising a step for connection (72d) according to the following formula reactions 48-3:
[formula reactions 48-3]

where R2X1, Y3, R14and R15have the meanings given in claim 1;
And10has the meaning given in paragraph 52;
R74arepresents a nitro group or a group-R1and R1has the meaning given in claim 1,
Rcrepresents a group-CONR14R15or a group-COOR59b, R59brepresents a lower alkyl group or phenyl-lower alkyl group; and
R17crepresents cycloalkylcarbonyl group, lower alkanoyloxy group which may have a halogen atom as a substituent, or aminosilane lower alkanoyloxy group which may have lower alkyl group as a substituent; and in the composition of A10linked to the group Y and b associated with the group-NHB3-Rcor a group-N(R17c)B3-Rc.

59. Pharmaceutical composition for the treatment of fibrosis, including aromatic connected to the e, selected from the group including:
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]ethylamino}-2-methoxyphenoxy)pyridine-3-yl]-3,4-dichlorobenzamide,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]ethylamino}phenoxy)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]ethylamino}-2-pertenece)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]methylamino}-2-pertenece)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]methylamino}-2-methoxyphenoxy)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]ethylamino}-2-methoxyphenoxy)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]ethylamino}-2-methylphenoxy)pyridine-3-yl]-3,4-dichlorobenzamide,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]methylamino}-2-methylphenoxy)pyridine-3-yl]-4-cryptomelane,
N-(6-{4-[3-(4-piperonylpiperazine-1-yl)-3-oxopropyl]phenoxy}pyridine-3-yl)-3,4-dichlorobenzenesulfonate,
N-[6-(4-{4-[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]piperazine-1-yl}phenoxy)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{4-[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}phenoxy)pyridine-3-yl]-4-cryptomelane,
N-{6-[(4-{4-[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}phenyl)methylamino]pyridine-3-yl}-4-cryptomelane
N-[6-(4-{4-[2-(4-benzylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}-2-methylphenoxy)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{4-[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}-2-methylphenoxy)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{4-[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}-2-methylphenoxy)pyridine-3-yl]-3,4-dichlorobenzamide,
N-{6-[4-(4-benzylpiperazine-1-carbonyl)phenoxy]pyridine-3-yl}-4-cryptomelane,
N-{6-[4-(4-benzylpiperazine-1-carbonyl)phenoxy]pyridine-3-yl}-3,4-dichlorobenzamide,
N-[6-({4-[3-(4-piperonylpiperazine-1-yl)-3-oxopropyl]phenyl}methylamino)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]ethylamino}-2-pertenece)pyridine-3-yl]-3,4-dichlorobenzamide,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]methylamino}-2-pertenece)pyridine-3-yl]-3,4-dichlorobenzamide,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]methylamino}-2-methoxyphenoxy)pyridine-3-yl]-3,4-dichlorobenzamide,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]methylamino}phenoxy)pyridine-3-yl]-3,4-dichlorobenzamide,
1-(6-{4-[3-(4-piperonylpiperazine-1-yl)-3-oxopropyl]phenoxy}pyridine-3-yl)-3-(3,4-dichlorophenyl)-1-atilmotin,
N-(6-{4-[3-(4-piperonylpiperazine-1-yl)-3-oxopropyl]phenoxy}pyridine-3-yl)-4-cryptomelane,
N-[6-(4-{[2-(4-benzylpiperazine-1-yl)-2-oxoethyl]methylamino}-2-methylphenoxy)pyridine-3-yl]-4-cryptomelane,
N-[6-(4-{4-[2-(4-benzyl who piperazin-1-yl)-2-oxoethyl]piperidine-1-yl}phenoxy)pyridine-3-yl]-3,4-dichlorobenzamide,
N-(6-{4-[3-(4-piperonylpiperazine-1-carbonyl)piperidine-1-yl]phenoxy}pyridine-3-yl)-3,4-dichlorobenzamide,
N-[6-(4-{4-[2-(4-benzylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}phenoxy)pyridine-3-yl]-4-cryptomelane,
N-{6-[(4-{4-[2-(4-benzylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}phenyl)methylamino]pyridine-3-yl}-4-cryptomelane,
N-(6-{4-[(2-{4-[4-(4-perbenzoic)phenyl]piperazine-1-yl}-2-oxoethyl)methylamino]-2-methoxyphenoxy}pyridine-3-yl)-4-cryptomelane,
2-(4-piperonylpiperazine-1-yl)-N-{3-methyl-4-[5-(4-triftormetilfullerenov)pyridine-2-yloxy]phenyl}-2-oxoacetate,
N-[6-(4-{[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]methylamino}-2-methylphenoxy)pyridine-3-yl]-2-fluoro-4-cryptomelane,
N-[6-(4-{4-[2-(4-piperonylpiperazine-1-yl)-2-oxoethyl]piperidine-1-yl}-2-methoxyphenoxy)pyridine-3-yl]-4-cryptomelane, and
ethyl ester of 4-(3-{3-methyl-4-[5-(4-triphtalocyaninine)pyridine-2-yloxy]phenyl}-2-oxohexanoate-1-yl)benzoic acid
or their salts.

60. Pharmaceutical composition for the treatment of fibrosis in p, where fibrosis is a lung fibrosis.

61. Pharmaceutical composition for the treatment of fibrosis in p, where fibrosis is a fibrosis of the liver.

62. Pharmaceutical composition for the treatment of fibrosis in p, where fibrosis is a glomerulosclerosis.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: compound of formula pharmaceutically acceptable salt or solvate of a compound or salt (I), ring Q represents optionally substituted monocyclic or condensed (C6-C12)aryl or optionally substituted monocyclic or condensed heteroaryl where said substitutes are chosen from: halogen; (C1-C6)alkyl optionally substituted by 1-3 halogen atoms; (C1-C6)alkylsulphonyl; phenyl optionally substituted by 1 or 2 substitutes chosen from halogen, (C1-C6)alkyl which can be substituted by 1-3 halogen atoms, groups (C1-C6)alkylamino, di(C1-C6)alkylamino, (C1-C6)alkoxy, (C1-C6)alkoxy(C1-C6)alkyl and (C1-C6)alkylthio; monocyclic or condensed heteroaryl optionally substituted by halogen; or oxo; Y1 represents a bond or -NR6-CO-, where R6 represents hydrogen, ring A represents optionally substituted a nonaromatic heterocyclyldiyl where said substitutes are chosen from (C1-C6)alkyl optionally substituted by groups hydroxy, (C1-C6)alkylamino, di(C1-C6)alkylamino, morpholino, (C1-C6)alkylaminocarbonyl, di(C1-C6)alkylaminocarbonyl; cyano; (C3-C6)cycloalkyl; (C1-C6)alkoxy; (C1-C6)alkoxy(C1-C6)alkyl; phenyl; benzyl; benzyloxymethyl; thienyl; 4-8-members monocyclic nonaromatic heterocycle having 1 or 2 heteroatoms chosen from N or O, and optionally substituted by 1 or 2 substitutes chosen from (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkoxy(C1-C6)alkyl and oxo; (C1-C6)alkylamino; di(C1-C6)alkylamino; a group of formula: -Y2Z'- represents a group of formula: [Formula 2] each R7 independently represents hydrogen, (C1-C6)alkyl or (C3-C6)cycloalkyl, each of R8 and R9 independently represents hydrogen or (C1-C6)alkyl, n is equal to an integer 0 to 3, Z1 represents a bond, -O-, -S- or-NR9 - where R9 represents hydrogen, (C1-C6)alkyl, acyl or (C1-C6)alkylsulphonyl, ring B represents optionally substituted aromatic carbocyclediyl or optionally substituted aromatic heterocyclediyl where said substitutes are chosen from (C1-C6)alkyl, halogen, (C1-C6)alkoxy and oxo; Y3 represents a bond optionally substituted (C1-C6)alkylene or (C3-C6)cycloalylene, optionally interrupted -O- or optionally substituted (C2-C6)alkenylene where said substitutes are chosen from (C1-C6)alkyl, (C3-C6)cycloalkyl, halogen and (C1-C6)alkoxycarbonyl; Z2 represents COOR3; R3 represents hydrogen or (C1-C6)alkyl.

EFFECT: preparation of new compounds.

30 cl, 9 tbl, 944 ex

FIELD: medicine.

SUBSTANCE: invention refers to the compound 3-{[5-(azetidine-1-ylcarbonyl)pyrazine-2-yl] oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazine-5-yl)benzamide or to its pharmaceutically acceptable salt. Also, it refers to a pharmaceutical composition for treating insulin-independent diabetes or obesity containing said compound.

EFFECT: there is produced and described a new compound which can be effective in treating insulin-independent diabetes and obesity.

5 cl, 64 ex

FIELD: chemistry.

SUBSTANCE: invention relates to oxazolidinone derivatives of formula (I) or pharmaceutically acceptable salts thereof, synthesis method thereof and pharmaceutical compositions containing said derivatives which are used as an antibiotic. Oxazolidinone derivatives, where R1 and R1' independently denote hydrogen or fluorine; R2 denotes -OR7, fluorine, monophosphate or metal phosphate; and R7 denotes hydrogen, C1-3alkyl or an acylated amino acid group, where the amino acid is alanine, glycine, proline, proline, isoleucine, leucine, phenylalanine, β-alanine or valine; R3 denotes hydrogen, a C1-4alkyl group which is unsubstituted or substituted cyano, , -(CH2)m-OR7 (m equals 0, 1, 2, 3, 4) or a ketone group. Oxazolidinone derivatives of formula (I) have antibacterial activity against different human and animal pathogens.

EFFECT: oxazolidinone derivatives, having inhibiting activity towards a wide range of bacteria and having low toxicity.

27 cl, 4 tbl, 73 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new pyrrolidine derivatives of general formula (1) or its pharmaceutically acceptable salts where R101 and R102 values are described by the patent claim. The compounds inhibit serotonin and/or norepinephrine and/or dopamine reabsorption thereby allowing to be used for treating depression and anxiety disorder. A method for preparing thereof is described.

EFFECT: preparation of new pyrrolidine derivatives.

10 cl, 162 tbl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to compounds of formula I and to their pharmaceutically acceptable salts. In formula I p is integer, equal to 0-1; L2 is selected from group including -XOX-, -XSX- and -XSXO-; where X is independently selected from group, including bond and C1-C4alkylene; R13 is selected from group, including halogen, C1-C6alkyl, C1-C6alkoxygroup, -C(O) C1-C6alkyl; R14 is selected from group, including -XOXC(O)OR17 and -C1-C4alkylene-C(O)OR17; where X represents bond or C1-C4alkylene; and R17 is selected from group, including hydrogen and C1-C6alkyl; R15 and R16 are independently selected from group, including -R18 and -YR18; where Y represents C2-C6alkenylene, and R18 is selected from group, including C6-C10aryl, benzo[1,3]dioxolyl, pyridinyl, pyrimidinyl, quinolyl, phenoxatiinyl, benzofuranyl, dibenzofuranyl, benzoxasolyl, 2,3-dihydrobenzofuranyl, 2-oxo-2,3-dihydrobenzooxasolyl, indolyl, 3-oxo-3,4-dihydro-2H-benzo[1,4]oxazinyl, 2,3-dihydrobenzo[1,4]dioxinyl, 3,4-dihydro-2H-benzo[b][1,4]dioxepinyl, where any C6-C10aryl, pyridinyl, benzoxasolyl, indolyl in R18 is optionally substituted by 1-2 radicals, independently selected from group, including halogen, nitrogroup, cyanogroup, C1-C6alkyl, C1-C6alkoxygroup, C1-C6alkylthiogroup, hydroxy-C1-C6alkyl, halogen-substituted C1-C6alkyl, halogen-substituted C1-C6alkoxygroup, piperidinyl, morpholinyl, pyrrolidinyl, phenyl, XS(O)0-2R17, -XNR17R17, -XNR17S(O)2R17, -XNR17C(O)R17, -XC(O)NR17R17, -XC(O)NR17R19, -XC(O)R17, -XC(O)R19 and -XOXR19, where X represents bond; R17 is selected from group, including hydrogen, C1-C6alkyl, halogen-substituted C1-C6alkyl, and R19 is selected from group, including C3-C12cycloalkyl, phenyl, piperidinyl, morpholinyl.

EFFECT: ensuring application of invention compounds for production of medication, modulating activity of activated receptors of peroxisome proliferators δ (ARPPδ), to pharmaceutical composition, possessing properties of ARPPδ activity modulator, including therapeutically efficient quantity of invention compound and to application of pharmaceutical composition for medication manufacturing.

8 cl, 1 tbl, 301 ex

FIELD: chemistry.

SUBSTANCE: invention describes compounds of formula I

, where R1 is selected from a group comprising hydrogen, lower alkyl, lower hydroxyl, lower alkoxyalkyl, lower halogenalkyl, lower cyanoalkyl; unsubstituted or substituted phenyl; lower phenylalkyl, where the phenyl ring can be unsubstituted or substituted; and heteroaryl, selected from pyridyl and pyrimidinyl; R2 denotes hydrogen or halogen; G denotes a group selected from

, where m equals, 0, 1; R3 is selected from lower alkyl, cycloalkyl and lower cycloalkylalkyl; n equals 0, 1; R4 denotes lower alkyl, as well as pharmaceutical compositions.

EFFECT: said compounds are used to treat or prevent diseases associated with histaminase receptor modulation.

19 cl, 1 tbl, 24 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula 1, its pharmaceutically acceptable salts and stereoisomers: $ (1), where: R1 means H, amidino, C1-C4-alkyl amidino, C1-C4alkanoylamidino, C1-C10-alkyl, C3-C7-cycloalkyl, C6-C10-aryl, 6-members heterocycle with O atom, 5-members heterocycle with two N atoms, 6-members heteroaryl with one or two N atoms, 5-members heteroaryl with two heteroatoms, one of which is N, and the other is S, C1-C6-alkylcarbonyl, C3-C7-cycloalkylcarbonyl, C1-C4-alkoxycarbonyl, C6-C10-aryl-C1-C4-alkoxycarbonyl, -SO2-C1-C4-alkyl, -C(O)-N(R6)(R7) or -C(S)-N(R6)(R7); and, R6, R7 means H, C1-C6-alkyl, C3-C7-cycloalkyl; alkyl, cycloalkyl, heterocycle, aryl or heteroaryl are unsubstituted or substituted; R2 means C6-C10-aryl which is unsubstituted or mono- or disubstituted; R3 means H, CN, C1-C6-alkyl, C3-C7-cycloalkyl, C2-C6-alkenyl, monocyclic 5-members heterocycle with N and O, monocyclic 5-members heteroaryl with two heteroatoms, one of which is N, and the other is O or S, C(O)-R8 or -C(S)-R8; and R8 means OH, C1-C4-alkyl, C1-C4-alkyloxy or N(R9)(R10); R9, R10 mean N, C1-C6-alkyl, C3-C7-cycloalkyl, C1-C4-alkyloxy, phenyl or 5-members heteroaryl with two heteroatoms, one of which is N, and the other is S, 6-members heteroaryl with N; R9, R10 together with N whereto attached can form a single 4-6-members ring which can include in addition O or S; and alkyl, cycloalkyl, heterocycle, phenyl or heteroaryl are unsubstituted or substituted. R4 means C3-C8-cycloalkyl, C6-C10-aryl, 5-members heteroaryl with two heteroatoms, one of which is N, and the other is S, 6-members heteroaryl with N, 6-members heterocycle with O, and C6-C10-aryl or heteroaryl are unsubstituted or mono- or polysubstituted. R5 means N, C1-C6-alkyl, -C(O)-R11, C1-C6-alkylsulphonyl, C6-C10-arylsulphonyl, -(CH2)p-C6-C10-aryl, -(CH2)p-heteroaryl or -(CH2)p-C3-C8-cycloalkyl where heteroaryl means 5-members heteroaryl with O or with N or with S which can contain in addition N. p is equal to 1 or 2; R11 means C1-C10-alkyl, C1-C6-alkenyl, C3-C8-cycloalkyl, C3-C8-cycloalkenyl, NH2, C1-C4alkylamino, (C1-C4-alkyl)(C1-C4-alkyl)amino, C6-C10-aryl, 5-members heteroaryl with N or with O or with 8 which can contain in addition N, 6-members heterocycle with N and O, 5- or 6-members heterocycle with O, and alkyl is unsubstituted or substituted with one substitute. Aryl, heteroaryl, cycloalkyl, cycloalkenyl or heterocycle are unsubstituted or mono- or disubstituted.

EFFECT: compounds are melanocortin receptor agonists so presented to be used in a pharmaceutical composition for treatment and prevention of obesity, diabetes, inflammation, erectile dysfunction.

19 cl, 18 tbl

FIELD: chemistry.

SUBSTANCE: present invention relates to novel derivatives of cis-2,4,5-triarylimidazoline of general formula I and pharmaceutically acceptable salts thereof, where X1 is selected from a group comprising lower alkoxy; X2 and X3 are independently selected from a group comprising hydrogen, halogen, cyano, lower alkyl, lower alkoxy, piperidinyl, -NX4X5, -SO2NX4X5, -C(O)NX4X5, -C(O)X6, -SOX6, -SO2X6, -NC(O)-lower alkoxy, -C≡C-X7, provided that both X2 and X3 do not denote hydrogen, lower alkyl or lower alkoxy, provided that when X2 or X3 denote hydrogen, the other does not denote lower alkyl, lower alkoxy or halogen, provided that when X2 denotes -HX4X5, X3 does not denote hydrogen, X2 and X3 together can form a ring selected from 5-7-member unsaturated rings which can contain three heteroatoms selected from S, N and O, X4 and X5 are independently selected from a group comprising hydrogen, lower alkyl, lower alkoxy, lower alkyl, substituted by a lower alkoxy, -SO2-lower alkyl, -C(O)piperazinyl-3-one; X6 is selected from a group comprising lower alkyl, morpholine, piperidine, pyrrolidine; X7 is selected from a group comprising hydrogen, lower alkyl, trifluoromethyl; Y1 and Y2 are independently selected from a group comprising halogen; R is selected from a group comprising lower alkoxy, piperidinyl substituted with a five-member heterocyclic ring which contains one nitrogen heteroatom, piperidinyl substituted with a hydroxy, -CH2OH or -C(O)NH2, piperazinyl substituted with one or two R1 [1,4]diazepanyl, substituted R1, R1 can denote one or two substitutes selected from a group comprising oxo, lower alkyl substituted with one R2, -C(O)R3, -SO2-lower alkyl, -SO2-five-memer heterocyclyl, which is selected from isoxazolyl, dimethylisoxazolyl, pyrrolidinyl, pyrrolyl, thiophenyl, imidazolyl, thiazolyl, thiazolidinyl, imidazolidinyl; R2 is selected from a group comprising -SO2-lower alkyl, hydroxy, lower alkoxy, -NH-SO2-lower alkyl, -cyano, -C(O)R4; R3 is selected from a group comprising a five-member heterocyclyl which is selected from isoxazolyl, dimethylisoxazolyl, pyrrolidinyl, pyrrolyl, thiophenyl, imidazolyl, thiazolyl, thiazolidinyl, imidazolidinyl, lower alkyl, lower alkenyl, lower alkyl substituted with a six-member heterocyclyl selected from piperidinyl, piperazinyl, 3-oxopiperazinyl, morpholinyl, C3-cycloalkyl; R4 is selected from a group comprising hydroxy, morpholine, piperidine, 4-acetylpiperazinyl, -NR5R6; R5 and R6 are independently selected from a group comprising hydrogen, lower alkyl, lower alkyl substituted with lower alkoxy or cyano, lower alkoxy and C3-cycloalkyl. The invention also relates to a pharmaceutical composition based on the formula I compound, use of the formula I compound in preparing a medicinal agent and a method for synthesis of the formula I compound.

EFFECT: novel derivatives of cis-2,4,5-triarylimidazoline of general formula I are obtained, which can be used to treat diseases, based on reaction of the MDM2 protein with p53-like protein, particularly as anticancer agent.

54 cl, 412 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to compounds of formula (I), where R1 denotes a 5- or 6-member ring of formulae

(II) or (III), respectively: R2 denotes H, C1-C7-alkyl, C3-C6-cycloalkyl or -(CH2)m,-Ra; R3 denotes aryl or heteroaryl, which can be substituted with CN, Cl, F, Br, CF3, CHF2, C3-C6-cycloalkyl or denotes heteroaryl which can be possibly substituted with C1-C7-alkyl; R4 denotes H, -OH, Cl, F, Br, CN, -CHF2, CF3, C1-C7-alkyl, C3-C6-cycloalkyl or -(CH2)m-Re; R5 denotes C1-C7-alkyl, -(CH2)n-O-Rf, or -(CH2)n-Re; Ra denotes -OH; Re denotes -OH; Rf denotes C1-C7-alkyl; m equals 1-4; n equals 2-6; and pharmaceutically acceptable salts thereof. The invention also relates to a medicinal agent containing said derivatives, use thereof in preparing medicinal agents suitable for treating diseases of the central nervous system.

EFFECT: novel compounds suitable for treating diseases of the central nervous system are obtained and described.

29 cl, 111 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel antibacterial compounds of formula (I). Compounds of formula (I) Q-NH-CO-R3, where Q stands for group of the following structure , R1 represents hydrogen, halogen, hydroxy, amino, mercapto, alkyl, heteroalkyl, alkeloxy, heteroalkyloxy, cycloalkyl, heterocycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, cycloalkyloxy, alkylcycloalkyloxy, heterocycloalkyloxy or heteroalkylcycloalkyloxy, X1, X2, X3, X4, X5 and X6 each independently on each other represent nitrogen atom or group of formula CR2, R2 represents hydrogen, halogen or hydroxy, amino, alkyl, alkenyl, alkinyl or heteroalkyl group, R3 is selected from the following groups R5 represents group of formula -B-Y, where B represents alkylene, alkenylene, alkinylene, -NH- or heteroalkylene, and Y represents aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl, heterocycloalkyl, alkylcycloalkyl or heteroalkylcycloalkyl, or their pharmaceutically acceptable salt, solvate, hydrate or pharmaceutically acceptable composition, as well as to pharmaceutical composition, which possesses antibacterial activity, based on said compounds and to their application for preparation of medication, intended for treatment of bacterial infections.

EFFECT: obtained and described are compounds, which can be useful in medicine.

9 cl, 147 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I) or pharmaceutically acceptable salts thereof, where Q is CH or N; R2 is C1-C4 alkyl or C3-C4-cycloalkyl; Y is R5-O; where R5 is propynyl; X is selected from a group consisting of aryl, heteroaryl, C1-C5-alkyloxy, heterocycloalkyl, arylamino, heteroarylamino, heteroaryl-C1-C4-alkylamino, aryloxy, aryl-C1-C2-alkyloxy or C3-C6-cycloalkyl-C1-C4-alkyloxy, each of which is optionally substituted with 1-3 times; the optional substitute(s) for X is(are) independently selected from a group comprising halogen, cyano, trifluoromethyl, nitro, hydroxy, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkyloxy-C1-C4-alkoxy, -SMe, SO2-C1-C2-alkyl, -NMe2, - C(O)O-C1-C5-alkyl, -SCF3, -SO2-NH2, -SO2-C2-alkyl-OH, -CONH2, -COMe, - CONH-C1-C4-alkyl, -CONMe2, -NHCOMe, -CH2COOEt, -OCH2COOEt, -CH2- cyclopropyl, and each R3 and R4 is H; where aryl denotes phenyl or naphthyl; heteroaryl denotes monocyclic or bicyclic hydrocarbon containing 5-10 ring atoms, one or more of which are heteroatoms selected from O, N or S; heterocyclyl denotes piperidinyl or benzodioxolyl; or a compound or pharmaceutically acceptable salt thereof, selected from a group comprising (4-dimethylaminophenyl)-[4-(4-cyclopropylphenyl)-6-propargyloxyquinazolin-2-yl]methanone, (3-sulphamoylphenyl)amide 4-(4-isopropylphenyl)-6-prop-2-ynyloxy-3,4-dihydroquinazoline-2-carboxylic acid, [3-(2-hydroxyethanesulphonyl)phenyl]amide 4-(4-isopropylphenyl)-6-prop-2-ynyloxy-3,4-dihydroquinazoline-2-carboxylic acid, (3-methylsulphanylphenyl)amide 4-(4-isopropylphenyl)-6-prop-2-ynyloxy-3,4-dihydroquinazoline-2-carboxylic acid, (3-methanesulphonylphenyl)amide 4-(4-isopropylphenyl)-6-prop-2-ynyloxy-3,4-dihydroquinazoline-2-carboxylic acid, and (5-ethanesulphonyl-2-hydroxyphenyl)amide 4-(4-isopropylphenyl)-6-prop-2-ynyloxy-3,4- dihydroquinazoline -2-carboxylic acid. The invention also relates to a pharmaceutical composition based on the compound of formula (I) and use of the compound of formula (I).

EFFECT: novel benzoquinazoline derivatives, which are useful in treating bone disorders, are obtained.

6 cl, 128 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new cyclopenta[b]benzofuranyl derivatives of formula wherein substitutes R1, R2, R3, R4, R5, R6 and R7 and n are specified in the patent clam. These compounds exhibit properties of NF-kB-activity and/or AP-1 inhibitor/modulator. Also, the inventive subject matter are methods for preparing intermediate compounds thereof, a pharmaceutical composition containing them, administration thereof for prevention and/or treatment of inflammatory and autoimmune diseases, neurodegenerative diseases and hyperproliferative diseases caused by NF-kB- and/or AP-1-activity, and a method for prevention and/or treatment of said diseases.

EFFECT: preparation of new cyclopenta[b]benzofuranyl derivatives.

21 cl, 3 tbl, 151 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: compound of formula pharmaceutically acceptable salt or solvate of a compound or salt (I), ring Q represents optionally substituted monocyclic or condensed (C6-C12)aryl or optionally substituted monocyclic or condensed heteroaryl where said substitutes are chosen from: halogen; (C1-C6)alkyl optionally substituted by 1-3 halogen atoms; (C1-C6)alkylsulphonyl; phenyl optionally substituted by 1 or 2 substitutes chosen from halogen, (C1-C6)alkyl which can be substituted by 1-3 halogen atoms, groups (C1-C6)alkylamino, di(C1-C6)alkylamino, (C1-C6)alkoxy, (C1-C6)alkoxy(C1-C6)alkyl and (C1-C6)alkylthio; monocyclic or condensed heteroaryl optionally substituted by halogen; or oxo; Y1 represents a bond or -NR6-CO-, where R6 represents hydrogen, ring A represents optionally substituted a nonaromatic heterocyclyldiyl where said substitutes are chosen from (C1-C6)alkyl optionally substituted by groups hydroxy, (C1-C6)alkylamino, di(C1-C6)alkylamino, morpholino, (C1-C6)alkylaminocarbonyl, di(C1-C6)alkylaminocarbonyl; cyano; (C3-C6)cycloalkyl; (C1-C6)alkoxy; (C1-C6)alkoxy(C1-C6)alkyl; phenyl; benzyl; benzyloxymethyl; thienyl; 4-8-members monocyclic nonaromatic heterocycle having 1 or 2 heteroatoms chosen from N or O, and optionally substituted by 1 or 2 substitutes chosen from (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkoxy(C1-C6)alkyl and oxo; (C1-C6)alkylamino; di(C1-C6)alkylamino; a group of formula: -Y2Z'- represents a group of formula: [Formula 2] each R7 independently represents hydrogen, (C1-C6)alkyl or (C3-C6)cycloalkyl, each of R8 and R9 independently represents hydrogen or (C1-C6)alkyl, n is equal to an integer 0 to 3, Z1 represents a bond, -O-, -S- or-NR9 - where R9 represents hydrogen, (C1-C6)alkyl, acyl or (C1-C6)alkylsulphonyl, ring B represents optionally substituted aromatic carbocyclediyl or optionally substituted aromatic heterocyclediyl where said substitutes are chosen from (C1-C6)alkyl, halogen, (C1-C6)alkoxy and oxo; Y3 represents a bond optionally substituted (C1-C6)alkylene or (C3-C6)cycloalylene, optionally interrupted -O- or optionally substituted (C2-C6)alkenylene where said substitutes are chosen from (C1-C6)alkyl, (C3-C6)cycloalkyl, halogen and (C1-C6)alkoxycarbonyl; Z2 represents COOR3; R3 represents hydrogen or (C1-C6)alkyl.

EFFECT: preparation of new compounds.

30 cl, 9 tbl, 944 ex

FIELD: medicine.

SUBSTANCE: compounds of the invention exhibit properties of β2- adrenoreceptor agonists. In formula (I) , R1 represents hydrogen; each R2, R3, R4, R5, R4' and R5' independently represents hydrogen or C1-C6alkyd; e is equal to 0 or 1; A represents C(O); D represents oxygen or sulphur; m is equal to an integer 0 to 3; n is equal to an integer 0 to 3; R6 represents the group -(X)p-Y-(Z)q-R10; each X and Z independently represents C1-C6akylene group; each p and q is independently equal to 0 or 1; Y represents a bond, oxygen, CH2 or NR9; R7a and R7b independently represent hydrogen or C1-C6alkyl; R9 represents C1-C6alkyl; R10 represents hydrogen or saturated or unsaturated 6-members ring system optionally containing at least one ring heteroatom, chosen of nitrogen. And this ring system is optionally substituted by C1-C6alkoxycarbonyl; R7 represents 6-12-members aromatic ring system which is optionally substituted by halogen, trifluoromethyl, hydroxyl, C1-C6alkyl, C1-C6alkoxy or NH2; provided R6 does not represent hydrogen or unsubsituted C1-C6alkyl group. Also, the invention refers to methods for producing compounds of formula (I), to a pharmaceutical composition exhibiting properties of β2- adrenoreceptor agonists containing the compound of formula (I) as an active ingredient, to application of the compound of formula (I) in preparing a drug, to a combination containing the compound of formula (I) and one or more agents.

EFFECT: improved properties of the composition.

27 cl, 2 tbl, 32 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel derivatives of isothiazole-3(2H)-OH-1,1-dioxides of formula (I) or pharmaceutically acceptable salts thereof, which can increase expression of LXR α and/or β, a pharmaceutical composition based on said derivatives, use thereof in preparing a medicinal agent, as well as novel intermediate compounds of formula (V) or salts thereof. In formulae (I), (V) R2 denotes phenyl, and R1 and R3 are as described in the claim.

EFFECT: improved properties of the derivatives.

7 cl, 9 dwg, 172 ex

FIELD: chemistry.

SUBSTANCE: invention relates to crystalline forms of a hydrate of 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H-benzimidazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione dihydrochloride of formula (I). The invention also relates to methods for synthesis of said compounds and to pharmaceutical compositions based on said compounds, having PPARy activating property.

EFFECT: said forms of the compounds are more stable and can be used in medicine to prepare medicinal agents for treating diabetes, cancer accompanied by diabetes.

16 cl, 7 tbl, 5 dwg, 6 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new pyrrolidine derivatives of general formula (1) or its pharmaceutically acceptable salts where R101 and R102 values are described by the patent claim. The compounds inhibit serotonin and/or norepinephrine and/or dopamine reabsorption thereby allowing to be used for treating depression and anxiety disorder. A method for preparing thereof is described.

EFFECT: preparation of new pyrrolidine derivatives.

10 cl, 162 tbl, 7 ex

FIELD: chemistry.

SUBSTANCE: invention describes compounds of formula I

, where R1 is selected from a group comprising hydrogen, lower alkyl, lower hydroxyl, lower alkoxyalkyl, lower halogenalkyl, lower cyanoalkyl; unsubstituted or substituted phenyl; lower phenylalkyl, where the phenyl ring can be unsubstituted or substituted; and heteroaryl, selected from pyridyl and pyrimidinyl; R2 denotes hydrogen or halogen; G denotes a group selected from

, where m equals, 0, 1; R3 is selected from lower alkyl, cycloalkyl and lower cycloalkylalkyl; n equals 0, 1; R4 denotes lower alkyl, as well as pharmaceutical compositions.

EFFECT: said compounds are used to treat or prevent diseases associated with histaminase receptor modulation.

19 cl, 1 tbl, 24 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula [I-D1] or pharmaceutically acceptable salt thereof,

,

where each symbol is defined in the claim. The invention also relates to pharmaceutical compositions containing said compound and having HCV polymerase inhibiting activity.

EFFECT: disclosed compound exhibits anti-HCV activity, based on HCV polymerase inhibiting activity and is useful as an agent for preventing and treating hepatitis C.

32 cl, 497 tbl, 1129 ex

FIELD: chemistry.

SUBSTANCE: invention relates to 4-phenyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivatives of formula I

or pharmaceutically acceptable salts thereof, where R1 denotes (1-6C)alkyl; R2, R3 independently denote halogen, (1-4C)alkoxy; R4 denotes phenyl or a 5-6-member heteroaryl, having one or two heteroatoms selected from nitrogen, oxygen or sulphur, phenyl or said heteroaryl, substituted with R7 and optionally substituted on the (hetero)aromatic ring with one or two substitutes selected from halogen, nitro, trifluoromethyl and (1-4C)alkyl; R7 denotes H, (1-4C)alkylthio, (1-4C)alkylsulphonyl, R8R9-amino, R10R11-aminocarbonyl, R12R13-amino(1-4C)alkylcarbonyl-amino, R14R15-amino(1-4C)alkyl, R16-oxy, R17R18-aminocarbonyl (1-4C)alkoxy, R19-oxy(1-4C)alkyl, R19-oxycarbonyl(1-4C)alkyl, R20R21-aminosulphonyl, R20-oxysulphonyl, aminoiminomethyl, (di)(1-4C)alkylaminoiminomethyl, morpholinyliminomethyl, trifluoromethylsulphonyl; R23-oxycarbonyl, or R23R24-aminocarbonyl; R8 denotes H or (1-4C)alkyl; R9 denotes (1-4C)alkylsulphonyl, (1-6C)alkylcarbonyl, (2-6C)alkenylcarbonyl, (3-6C)cycloalkylcarbonyl, (1-4C)alkoxycarbonyl, (3-4C)alkenyloxycarbonyl, (di)(1-4C)alkylaminocarbonyl, piperazinylcarbonyl, (5-8C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl or phenylcarbonyl, furylcarbonyl, thiophenylsulphonyl, 5-member heteraryl(1-4C)alkyl, having one or two nitrogen atoms, optionally substituted on the heteroaromatic ring with one, two or three substitutes selected from hydroxy, amino, halogen, nitro, trifluoromethyl, (1-4C)alkoxy; R10 denotes H or (1-4C)alkyl; R11 denotes hydroxy(2-4C)alkyl, (1-4C)alkoxy(2-4C)alkyl; R12, R13 independently denote H, (1-6C)alkyl, (3-6C)-cycloalkyl, (1-4C)alkoxy(2-4C)alkyl, (3-6C)cycloalkyl-(1-4C)alkyl, pyrrolidinyl(1-4C)alkyl, amino(2-4C)alkyl, (di)(1-4C)-alkylamino(2-4C)alkyl or phenyl(1-4C)alkyl, pyridinyl (1-4C)alkyl; or R12R13 in R12R13-amino(1-4C)alkylcarbonylamino can be bonded together with the nitrogen atom to which they are bonded into a (5-6C)heterocycloalkyl ring, having one or two nitrogen atoms, optionally substituted with hydroxy(1-4C)alkyl; R14, R15 independently denote H, (1-6C)alkyl, (1-6C)alkylcarbonyl, (1-4C)alkoxycarbonyl or pyridinyl(1-4C)alkyl, optionally substituted on the aromatic ring with one substitute selected from halogen; or R16 denotes (di)(1-4C)alkylamino(2-4C)alkyl, hydroxycarbonyl(1-4C)alkyl, (1-4C)alkoxycarbonyl(1-4C)alkyl, phenyl(1-4C)alkyl or pyridinyl(1-4C)alkyl; R17, R18 independently denote H, (1-6C)alkyl, thiophenyl(1-4C)alkyl; or R17R18 in R17R18-aminocarbonyl(1-4C)alkoxy can be bonded into a morpholine or piperazine ring, R19 denotes H or (1-6C)alkyl; R20R21 independently denote H, (1-6C)alkyl or (1-4C)alkoxy(1-4C)alkyl; or R20R21 in R20R21-aminosulphonyl can be bonded into a morpholine ring; X denotes O or N-R22; Y denotes CH2 or C(O); Z denotes CN or NO2; R22 denotes H; R23, R24 independently denotes H; (1-4C)alkyl; or R23R24 in R23R24-aminocarbonyl can be bonded into a dihydropyridine ring; provided that compounds of formula I, in which X denotes O, R4 denotes phenyl and R7 is selected from H, (1-4C)alkylthio, (1-4C)alkylsulphonyl, R23-oxycarbonyl, and R23R24-aminocarbonyl, and compounds of formula I, in which X denotes O, R4 denotes (2-5C)heteroaryl and R7 denotes H are excluded. The invention also relates to use of 4-phenyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivatives to prepare a medicinal agent for treating sterility.

EFFECT: improved useful biological properties.

12 cl, 73 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula 1, compounds of formula 5 and pharmaceutically acceptable salts thereof. In formulae 1 5 Y denotes -C(O)-, X denotes -N(R11)-, R1 denotes a residue of formula 1a or 1b - for formula 1 or residue of formulae 5a or 5b - for formula 5 1a 1b 5a 5b, R2 and R7 independently denote H, hydroxyl or (C1-C6)alkyl; R3 and R6 each independently denotes H, hydroxyl or (C1-C6)alkyl; R4 and R5 each independently denotes H or (C1-C6)alkyl; the rest of the radicals are described in the formula of invention. The invention also relates to separate compounds given in the formula of invention, a pharmaceutical composition having Bcl bound protein inhibiting properties, which contains a therapeutically effective amount of the disclosed compound, a method of treating a bc1 mediated disorder, involving introduction of a therapeutically effective amount of the disclosed compound and a method of treating a bc1 mediated disorder involving administration to a patient in need of treatment of an effective amount of camptothecin and therapeutically effective amount of the disclosed compound.

EFFECT: high efficiency of the composition.

84 cl, 12 tbl, 1 dwg, 217 ex

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