Oxime derivatives and preparation thereof

FIELD: medicine.

SUBSTANCE: in formula (I) , the ring A represents 6-members aryl or 5-6-members heteroaryl containing 1-2 heteroatoms selected from nitrogen and sulphur; Q means C3-8 cycloalkyl, 5-6-members heterocycle containing 1 heteroatom selected from oxygen, nitrogen or sulphur, C1-6 alkyl or C2-6 alkenyl; the ring T represents 5, 6, 9 or 10-members heteroaryl or 9-members heterocycle optionally additionally substituted by 1-3 heteroatoms independently selected from nitrogen or sulphur. The values of other substitutes are specified in the patent claim. Also, the invention refers to methods for preparing oxime derivatives of general formula (I), to pharmaceutical compositions containing the compound of the invention as an active ingredient and to applications of the compounds of the invention in preparing a drug.

EFFECT: compounds of the invention exhibit properties of a glucokinase activator.

33 cl, 1499 ex

 

The text descriptions are given in facsimile form.

1. Derived oxime of General formula [1]:

where ring a is a 6-membered aryl or 5-6-membered heteroaryl containing 1-2 heteroatoms selected from nitrogen and sulfur;
Q means3-8cycloalkyl, 5-6-chleny a heterocycle containing 1 heteroatom selected from oxygen, nitrogen or sulfur, C1-6alkyl or C2-6alkenyl;
ring T represents a 5, 6, 9, or 10-membered heteroaryl or 9-membered heterocycle
,
optionally additionally substituted by 1-3 heteroatoms independently selected from nitrogen or sulfur;
R1means a hydrogen atom or a halogen atom;
R2means (1) With the3-8cycloalkylcarbonyl is, (2) C1-6alkylsulfonyl which may be substituted by a group selected from (a) C1-6alkoxycarbonyl, (b) C1-6alkoxy, (C)3-8cycloalkyl, d) hydroxy, (e) amino, optionally substituted by same or different 1 to 2 groups selected from C1-6the alkyl and C2-7alkanoyl, (f) a 5-membered heteroaryl containing 2-4 heteroatoms selected from nitrogen, optionally substituted C1-6the alkyl, (g) C1-6alkylsulfonyl, (h) cyano, and (i) a 9-membered heterocycle, containing 1 heteroatom selected from nitrogen, optionally substituted 2 oxo, (3) aminosulfonyl, which can be substituted by the same or different 1 to 2 substituents selected from (a) C1-6the alkyl which may be substituted by same or different 1 to 2 substituents, selected amino, substituted CI-C1-6by alkyl; carbamoyl, optionally substituted mono - or di-C1-6by alkyl; hydroxy; C1-6alkoxy; 5-6-membered heteroaryl containing 1-2 heteroatoms selected from nitrogen, optionally substituted C1-6by alkyl; C3-8cycloalkyl; C1-6alkoxycarbonyl; hydroxy-C1-6alkoxy; 5 to 6 membered heterocycle containing 1-2 heteroatom selected from oxygen or nitrogen; a halogen, or C1-6alkylthio; (b) (C3-8cycloalkyl, (C) 6-membered heterocycle containing 1 heteroatom selected from sour the ode or nitrogen, optionally substituted C1-6by alkyl; and (d) With 1-6 alkoxy or (4) 4-7-membered heterocyclisation containing 1-2 heteroatoms selected from nitrogen, oxygen or sulfur which can be substituted by the same or different 1 to 3 substituents selected from hydroxy; (C1-6of alkyl; oxo, C1-6alkanoyl; hydroxy-C1-6of alkyl; carbamoyl, substituted CI-C1-6by alkyl; a 6-membered heteroaryl containing 1 heteroatom selected from nitrogen; aminosulfonyl, optionally substituted mono - or di-C1-6by alkyl; amino, substituted CI-C1-6the alkyl, C1-6alkylsulfonyl; C1-6alkoxy; C1-6alkoxy-C1-6of alkyl;
R3and R4independent means (1) a hydrogen atom, (2) C1-6alkoxy, (3) 5-membered heterocycle containing 1-2 heteroatom selected from oxygen or nitrogen, which may be substituted by same or different 1 to 2 substituents selected from C1-6alkoxycarbonyl, oxo, C1-6of alkyl, C2-7alkanoyl, (4) 5-6-membered heteroaryl containing 1-3 heteroatom selected from oxygen, nitrogen or sulfur, which may be substituted by same or different 1 to 2 substituents selected from C1-6of alkyl; amino, substituted CI-C1-6the alkyl, (5) C1-6alkoxy-C1-6alkoxy, (6) With3-8cycloalkyl, (7) cyano, (8) 6-membered aryl, which may be zames the n group, selected from cyano, halogen, C1-6alkoxy, (9) carbarnoyl, which can be substituted by the same or different 1-3 C1-6alkilani, (10) hydroxy, (11) C2-7alkanoyl, (12) C1-6alkylthio, (13) C1-6alkoxycarbonyl, (14) a 6-membered, aryloxy, (15) halogen atom, (16) oxo, or (17) 6-membered, arylcarboxylic;
R5means (1) a hydrogen atom, (2) formyl, (3) halogen atom, (4) oxo, (5) C1-6alkoxy which may be substituted by a group selected from (a) amino, optionally substituted by same or different 1 to 2 groups selected from C1-6the alkyl and C1-6alkoxycarbonyl; (b) C1-6alkoxycarbonyl; (C) carbamoyl, optionally substituted mono - or di - C1-6by alkyl; (d) carboxyl; (e) hydroxy; (f) a 5-membered heterocycle containing 1 heteroatom selected from nitrogen; or (g) three-C1-6alkylsilane; (6) aminosulfonyl, substituted 2 C1-6alkilani, (7) 1-6, alkylthio, which may be substituted amino, optionally substituted mono - or di-C1-6the alkyl or C1-6alkoxycarbonyl, (8) cyano, (9) 6-membered heterocyclisation containing 2 heteroatoms selected from nitrogen, substituted C1-6the alkyl, (10) nitro, (11)3-8cycloalkyl, (12) C1-6alkoxycarbonyl, (13) C2-6alkenyl, (14) C1-6alkylsulfonyl, (15) carbarnoyl, which can be substituted by the same or different 1-2 h is Mascitelli, selected from (a) C1-6the alkyl, optionally substituted by hydroxy; 5-membered heterocycle containing 1 heteroatom selected from oxygen; amino, substituted CI-C1-6by alkyl; or 6-membered heteroaryl containing 1 heteroatom selected from nitrogen, or (b) (C3-8cycloalkyl, (16) a 5-membered, heteroaromatic containing 3 heteroatoms selected from nitrogen, substituted C1-6the alkyl, (17) amino which may be substituted by same or different 1 to 2 substituents selected from (a) C1-6of alkyl, (C) C2-7alkanoyl and (e) C1-6alkoxycarbonyl, (18) carboxyl, (19) 5-membered heteroaryl containing 4 heteroatoms selected from nitrogen, (20) C2-7-quinil, which is substituted by hydroxy, or amino, substituted CI-C1-6the alkyl, (21) 5-6-membered heterocalixarenes containing 1-2 heteroatom selected from oxygen or nitrogen which is substituted by hydroxy, C1-6the alkyl, or hydroxy-C1-6the alkyl, (22) 4-6-membered, heterocyclic containing 1 heteroatom selected from nitrogen, which can be substituted C1-6the alkyl, (23) a 5-membered heterocycle, which is substituted by 1 heteroatom selected from nitrogen, substituted oxo, (24) a 6-membered, heterocyclic containing 1 heteroatom selected from nitrogen which may be substituted C1-6the alkyl or C2-7alkanoyl, (26) C2-7alkanoyl or (27) C1-6Ala is l, which may be substituted by same or different 1 to 3 substituents selected from (a) 4-7-membered heterocycle containing 1-2 heteroatoms selected from oxygen, nitrogen or sulfur, or 9-membered bicyclic heterocycle containing 2-4 heteroatoms selected from nitrogen, which can be substituted by the same or different 1 to 3 substituents selected from C1-6of alkyl; oxo; C1-6alkoxy-C2-7alkanoyl; C2-7alkanoyl; C2-7alkanolamine; C3-8cycloalkylcarbonyl; three(halogeno)-C2-7alkanolamine; formylamino; C1-6alkoxycarbonyl; hydroxy; C3-8cycloalkylcarbonyl; three(halogeno)-C1-6of alkyl, C1-6alkoxycarbonyl; formyl; amino, optionally substituted CI-C1-6by alkyl; aminosulfonyl, optionally substituted mono - or di-C1-6the alkyl, C1-6alkylsulfonyl; 6-membered heteroaryl containing 1-2 heteroatoms selected from nitrogen; C1-6alkoxycarbonyl-C1-6of alkyl, C2-7alkanoyloxy-C2-7alkanoyl; C1-6alkoxycarbonylmethyl; amino-C2-7alkanoyl, substituted CI-C1-6by alkyl; carbamoyl, substituted C1-6by alkyl; hydroxy-(C2-7alkanoyl; di(halogeno)-C2-7alkanoyl; 5-membered heterocyclyl-carbonyl containing 1 heteroatom selected from oxygen, substituted on the co; (b) amino which may be substituted by same or different 1 to 2 substituents selected from C1-6of alkyl; carbarnoyl-C1-6of alkyl, substituted CI-C1-6by alkyl; amino-C1-6of alkyl, substituted the same or different 1 to 2 groups selected from C1-6the alkyl and C2-7alkanoyl; C1-6alkoxy-C1-6of alkyl; hydroxy-(C1-6of alkyl; 6-membered heteroaryl containing 1 heteroatom selected from nitrogen; 6-membered heteroaryl-C1-6of alkyl containing 1 heteroatom selected from nitrogen, (C) C1-6alkoxy which may be substituted by hydroxy or C1-6alkoxy, (d) carbamoyl, which is replaced by the same or different 1 to 2 substituents selected from C1-6of alkyl, C1-6alkoxy, (e) hydroxy, (f) three-C1-6alkylsilane, (g) C1-6alkylthio, (h) C1-6alkylsulfonyl, (i) a 6-membered, heterocyclic containing 1 heteroatom selected from nitrogen, which can be substituted C2-7alkanoyl, C1-6the alkyl, formyl, C3-8cycloalkylcarbonyl, C1-6alkoxy-C2-7alkanoyl, C1-6alkylsulfonyl, (j) a 5-membered heteroaryl containing 2 heteroatoms selected from nitrogen, (k) hydroxyimino, which may be substituted C1-6alkoxycarbonyl, (1) halogen atom, (m) carboxyl, (n) C1-6alkoxycarbonyl or (o) C2-7alkanoyloxy;
Rsup> 6means a hydrogen atom, a C1-6alkyl, halogen atom or carboxyl;
or its pharmaceutically acceptable salt.

2. Derived oxime according to claim 1,
where ring a is a 6-membered aryl or 5-6-membered heteroaryl containing 1-2 heteroatoms selected from nitrogen or sulfur;
Q represents C3-8cycloalkyl, 5-6-membered heterocycle containing 1 heteroatom selected from oxygen, nitrogen or sulfur, C1-6alkyl or C2-6alkenyl;
ring T represents a 5, 6, 9, or 10-membered heteroaryl or 9-membered heterocycle
; optional optionally containing 1-3 heteroatoms independently selected from nitrogen or sulfur;
R1means a hydrogen atom or a halogen atom;
R2means (1) With the3-8cycloalkylcarbonyl, (2) C1-6alkylsulfonyl which may be substituted by a group selected from (a) C1-6alkoxycarbonyl, (b) C1-6alkoxy, (C)3-8cycloalkyl, (d) hydroxy, (e) amino, optionally substituted by same or different 1 to 2 groups selected from C1-6the alkyl and C2-7alkanoyl, (f) a 5-membered heteroaryl containing 2-4 heteroatoms selected from nitrogen, optionally substituted C1-6the alkyl, (g) C1-6alkylsulfonyl, (h) cyano or (i) a 9-membered heterocycle, containing 1 heteroatom selected from nitrogen, zameshannogo oxo, (3) aminosulfonyl, which can be substituted by the same or different 1 to 2 Deputy selected from (a) C1-6the alkyl which may be substituted by the same or different and 1-2 substituent(s)selected from amino, substituted CI-C1-6by alkyl; carbamoyl, optionally substituted mono - or di-C1-6by alkyl; hydroxy; C1-6alkoxy; 5-6-membered heteroaryl containing 1-2 heteroatoms selected from nitrogen, optionally substituted C1-6by alkyl; C3-8cycloalkyl; C1-6alkoxycarbonyl; hydroxy-C1-6alkoxy; 5 to 6 membered heterocycle containing 1-2 heteroatom selected from oxygen or nitrogen; a halogen; or C1-6alkylthio; (b) (C3-8cycloalkyl; (C) 6-membered heterocycle containing 1 heteroatom selected from oxygen or nitrogen, substituted C1-6by alkyl; or (d) C1-6alkoxy, (4) 4-7-membered heterocyclisation containing 1-2 heteroatom selected from oxygen, nitrogen or sulfur, which may be substituted by same or different 1 to 3 substituents selected from hydroxy; (C1-6of alkyl; oxo; C2-7alkanoyl; hydroxy-C1-6of alkyl; carbamoyl, substituted CI-C1-6by alkyl; a 6-membered heteroaryl containing 1 heteroatom selected from nitrogen; aminosulfonyl, optionally substituted mono - or di-C1-6by alkyl; amino, substituted CI-C 1-6the alkyl, C1-6alkylsulfonyl; C1-6alkoxy, C1-6alkoxy-C1-6of alkyl;
R3and R4means independently (1) hydrogen atom, (2) C1-6alkoxy, (3) 5-membered heterocycle containing 1-2 heteroatom selected from oxygen or nitrogen, which may be substituted by same or different 1 to 2 substituents selected from C1-6allyloxycarbonyl, oxo, C1-6of alkyl, C2-7alkanoyl, (4) 5-6-membered heteroaryl containing 1-3 heteroatom selected from oxygen, nitrogen or sulfur, which may be substituted by same or different 1 to 2 substituents selected from C1-6of alkyl; amino, substituted CI-C1-6the alkyl, (5) C1-6alkoxy-C1-6alkoxy, (6) With3-8cycloalkyl, (7) cyano, (8) 6-membered aryl which may be substituted by a group selected from cyano, halogen atom, a C1-6alkoxy, (9) carbarnoyl, which can be substituted by the same or different 1-3 C1-6alkilani, (10) hydroxy, (11) C2-7alkanoyl, (12) C1-6alkylthio, (13) C1-6alkoxycarbonyl, (14) a 6-membered, aryloxy, (15) halogen atom, (16) oxo, or (17) 6-membered, arylcarboxylic;
R5means (1) a hydrogen atom, (2) formyl, (3) halogen atom, (4) oxo, (5) C1-6alkoxy which may be substituted by a group selected from (a) amino, optionally substituted by same or different 1 to 2 groups selected the C C 1-6the alkyl and C1-6alkoxycarbonyl; (b) C1-6alkoxycarbonyl; (C) carbamoyl, rebaseline substituted mono - or di-C1-6by alkyl; (d) carboxyl; (e) hydroxy; (f) a 5-membered heterocycle containing 1 heteroatom selected from nitrogen, or (g) three-C1-6alkylsilane; (6) aminosulfonyl, which substituted 2 C1-6alkilani, (7) C1-6alkylthio, which may be substituted amino, optionally substituted mono - or di-C1-6by alkyl; or C1-6alkoxycarbonyl, (8) cyano, (9) 6-membered heterocyclisation containing 2 heteroatoms selected from nitrogen, substituted C1-6the alkyl, (10) nitro, (11)3-8cycloalkyl, (12) C1-6alkoxycarbonyl, (13) C2-6alkenyl, (14) C1-6alkylsulfonyl, (15) carbarnoyl, which can be substituted by the same or different 1 to 2 substituents selected from (a) C1-6the alkyl, optionally substituted by hydroxy; 5-membered heterocycle containing 1 heteroatom selected from oxygen; amino, substituted CI-C1-6by alkyl; or 6-membered heteroaryl containing 1 heteroatom selected from nitrogen or (b) (C3-8cycloalkyl, (16) a 5-membered, heteroaromatic containing 3 heteroatoms selected from nitrogen, substituted C1-6the alkyl, (17) amino which may be substituted by same or different 1 to 2 substituents selected from C1-6of alkyl, C2- alkanoyl, C1-6alkoxycarbonyl, (18) carboxyl, (19) 5-membered heteroaryl containing 4 heteroatoms selected from nitrogen, (20) C2-7-quinil, which is substituted by hydroxy or amino, substituted CI-C1-6the alkyl, (21) 5-6-membered heterocalixarenes containing 1-2 heteroatom selected from oxygen or nitrogen which is substituted by hydroxy, C1-6the alkyl, or hydroxy-C1-6the alkyl, (22) 4-6-membered, heterocyclic containing 1 heteroatom selected from nitrogen, which can be substituted C1-6the alkyl, (23) a 5-membered heterocycle containing 1 heteroatom selected from a nitrogen which is substituted by oxo, (24) a 6-membered, heterocyclic containing 1 heteroatom selected from nitrogen, which can be substituted C1-6the alkyl or C2-7alkanoyl, (26) C2-7alkanoyl, or (27) C1-6alkyl which may be substituted by same or different 1 to 3 substituents selected from (a) 4-7-membered heterocycle containing 1-2 heteroatoms selected from oxygen, nitrogen or sulfur, or 9-membered bicyclic heterocycle containing 2-4 heteroatoms selected from nitrogen, which can be substituted by the same or different 1 to 3 substituents selected from C1-6of alkyl; oxo; C1-6alkoxy-C2-7alkanoyl; C2-7alkanoyl; C2-7alkanolamine; C3-8cycloalkylcarbonyl; three(halogeno)-C2-7is alkanolamine; formylamino; C1-6alkoxycarbonyl; hydroxy; C3-8cycloalkylcarbonyl; three(halogeno)-C1-6of alkyl, C1-6alkoxycarbonyl; formyl; amino, optionally substituted CI-C1-6by alkyl; aminosulfonyl, optionally substituted mono - or di-C1-6the alkyl, C1-6alkylsulfonyl; 6-membered heteroaryl containing 1-2 heteroatoms selected from nitrogen; C1-6alkoxycarbonyl-C1-6of alkyl, C2-7alkanoyloxy-C2-7alkanoyl; C1-6alkoxycarbonylmethyl; amino-C2-7alkanoyl, substituted CI-C1-6by alkyl; carbamoyl, substituted C1-6by alkyl; hydroxy-(C2-7alkanoyl; di(halogeno)-C2-7alkanoyl; 5-membered geterotsiklicheskikh containing 1 heteroatom selected from oxygen, substituted oxo; (b) amino which may be substituted by same or different 1 to 2 substituents selected from C1-6of alkyl; carbarnoyl-C1-6of alkyl, substituted CI-C1-6by alkyl; amino-C1-6of alkyl, substituted the same or different 1 to 2 groups selected from C1-6the alkyl and C2-7alkanoyl; C1-6alkoxy-C1-6of alkyl; hydroxy-(C1-6of alkyl; 6-membered heteroaryl containing 1 heteroatom selected from nitrogen; 6-membered heteroaryl-C1-6of alkyl containing 1 heteroatom selected from nitrogen; (C) C1-6alcox is, which may be substituted by hydroxy or C1-6alkoxy, (d) carbamoyl, which is replaced by the same or different 1 to 2 substituents selected from C1-6of alkyl, C1-6alkoxy, (e) hydroxy, (f) three-C1-6alkylsilane, (g) C1-6alkylthio, (h) C1-6alkylsulfonyl, (i) a 6-membered, heterocyclic containing 1 heteroatom selected from nitrogen, which can be substituted C2-7alkanoyl, C1-6the alkyl, formyl, C3-8cycloalkylcarbonyl, C1-6alkoxy-C2-7alkanoyl or C1-6alkylsulfonyl, (j) a 5-membered heteroaryl containing 2 heteroatoms selected from nitrogen, (k) hydroxyimino, which may be substituted C1-6alkoxycarbonyl, (1) halogen atom, (m) carboxyl, (n) C1-6alkoxycarbonyl or (Oh)2-7alkanoyloxy;
R6means a hydrogen atom, a C1-6alkyl, halogen atom or carboxyl;
provided that if Q is a C3-8cycloalkyl, C1-6alkyl or C2-6alkenyl, R3and R4not mean any combination of two groups independently selected from hydrogen, C1-6alkoxy, cyano, 6-membered aryl which may be substituted by groups selected from cyano, halogen atom, a C1-6alkoxy; hydroxy, C1-6alkylthio, C1-6alkoxycarbonyl or halogen atom;
or its pharmaceutically acceptable the salt.

3. Derived oxime according to claim 2, where R1means a hydrogen atom, or its pharmaceutically acceptable salt.

4. Proizvodnoe of oxime according to any one of claims 1 to 3, where R2means (1) With the3-8cycloalkylcarbonyl, (2) C1-6alkylsulfonyl which may be substituted by a group selected from (a) C1-6alkoxycarbonyl, (b) C1-6alkoxy, (C)3-8cycloalkyl, (d) hydroxy, (e) amino, optionally substituted by same or different 1 to 2 groups selected from C1-8the alkyl and C2-7alkanoyl, (f) a 5-membered heteroaryl containing 2-4 heteroatoms selected from nitrogen, optionally substituted C1-6the alkyl, (g) C1-6alkylsulfonyl, (h) cyano, and (i) a 9-membered heterocycle, containing 1 heteroatom selected from nitrogen, substituted 2 oxo or (3) aminosulfonyl, which can be substituted by the same or different 1 to 2 substituents selected from (a) C1-6the alkyl which may be substituted by 1-2 are the same or different substituents selected from amino, substituted CI-C1-6by alkyl; carbamoyl, optionally substituted mono - or di-C1-6by alkyl; hydroxy; C1-6alkoxy; 5-6-membered heteroaryl containing 1-2 heteroatoms selected from nitrogen, optionally substituted C1-6by alkyl; C3-8cycloalkyl; C1-6alkoxycarbonyl; hydroxy-C1-6alkoxy; 5-6-clinohumite, containing 1-2 heteroatoms selected from nitrogen; a halogen; or C1-6alkylthio; (b) (C3-8cycloalkyl; (C) 6-membered heterocycle containing 1 heteroatom selected from oxygen or nitrogen, substituted C1-6by alkyl; and (d) C1-6alkoxy, or its pharmaceutically acceptable salt.

5. Derived oxime according to any one of claims 1 to 3, where R2means3-8cycloalkylcarbonyl, or its pharmaceutically acceptable salt.

6. Derived oxime according to any one of claims 1 to 4, where the Deputy "C1-6alkylsulfonyl" in R2represents a C1-6alkoxy, or its pharmaceutically acceptable salt.

7. Derived oxime according to any one of claims 1 to 6, where the ring a represents a 6-membered aryl, or its pharmaceutically acceptable salt.

8. Derived oxime according to any one of claims 1 to 6, where ring a is a phenyl or pyridyl, or its pharmaceutically acceptable salt.

9. Derived oxime according to any one of claims 1 to 8, where
Q represents C3-8cycloalkyl, 5-6-membered heterocycle containing 1 heteroatom selected from oxygen, nitrogen or sulfur, or C1-6alkyl,
R3and R4are independently (1) hydrogen atom, (2) C1-6alkoxy, (3) 5-membered heterocycle containing 1-2 heteroatom selected from oxygen or nitrogen, which may be substituted by the same or different 1-2 mandated what teli, selected from C1-6alkoxycarbonyl, oxo, C1-6of alkyl, C2-7alkanoyl, (4) 5-6-membered heteroaryl containing 1-3 heteroatom selected from oxygen, nitrogen or sulfur, which may be substituted by same or different 1 to 2 substituents selected from C1-6of alkyl; amino, substituted CI - C1-6the alkyl, (5)3-8cycloalkyl, (6) 6-membered aryl which may be substituted by a group selected from cyano, halogen atom, a C1-6alkoxy, (7) carbarnoyl, which can be substituted by the same or different 1-3 C1-6alkilani, (8) hydroxy, (9) C2-7alkanoyl, (10) C1-6alkylthio, (11) 6-membered, aryloxy, (12) halogen atom, (13) oxo, or (14) a 6-membered, arylcarboxylic,
provided that when Q means3-8cycloalkyl or C1-6alkyl, then R3and R4each independently are (1) hydrogen, (2) C1-6alkoxy, (3) a 6-membered aryl which may be substituted by a group selected from cyano, halogen atom, a C1-6alkoxy, (4) hydroxy, (5) C1-6alkylthio or (6) halogen atom,
or its pharmaceutically acceptable salt.

10. Proizvodnoe of oxime according to any one of claims 1 to 8, where
Q represents C3-8cycloalkyl or 5-6-membered heterocycle containing 1 heteroatom selected from oxygen, nitrogen or sulfur,
R3and R4are independently (1) hydrogen atom, (2) C-6 alkoxy, (3) 5-6-membered heteroaryl containing 1-3 heteroatom selected from oxygen, nitrogen or sulfur, which may be substituted by same or different 1 to 2 substituents selected from C1-6of alkyl; amino, substituted CI-C1-6the alkyl, (4)3-8cycloalkyl, (5) hydroxy,
provided that when Q means3-8cycloalkyl, then R3and R4each independently are (1) hydrogen, (2) C1-6alkoxy, (3) hydroxy,
or its pharmaceutically acceptable salt.

11. Derived oxime according to any one of claims 1 to 8, wherein the group - Q(R3)(R4) is a 5-6-membered heterocycle containing 1 heteroatom selected from oxygen, nitrogen or sulfur, or C1-6alkyl substituted by 1-2 groups of 5-6-membered heteroaryl containing 1-3 heteroatom selected from oxygen, nitrogen or sulfur, which may be substituted by same or different 1 to 2 substituents selected from C1-6of alkyl; amino, substituted CI-C1-6the alkyl, or its pharmaceutically acceptable salt.

12. Derived oxime according to any one of claims 1 to 8, where Q represents a 5-6 membered heterocycle containing 1 heteroatom selected from oxygen, nitrogen or sulfur, and both R3and R4are a hydrogen atom, or its pharmaceutically acceptable salt.

13. Derived oxime according to any one of claims 1 to 12, where the ring T represents the 5, 6, 9, or any heteroaryl
not necessarily optionally containing 1-3 heteroatoms independently selected from nitrogen or sulfur, or its pharmaceutically acceptable salt.

14. Derived oxime according to any one of claims 1 to 12, where the ring T represents thiazolyl, triazolopyridines, pyridyl, pyrazinyl, benzothiazolyl, hinely, thiadiazolyl, pyrazolyl, triazolopyridines, triazolopyrimidines, cyclohexanediethanol or dihydroisocodeine, or its pharmaceutically acceptable salt.

15. Derived oxime according to any one of claims 1 to 12, where the ring T is thiazolyl, triazolopyridines, pyridyl, pyrazinyl, benzothiazolyl, thiadiazolyl, triazolopyridines, triazolopyrimidines, cyclohexanediethanol or dihydroisocodeine, or its pharmaceutically acceptable salt.

16. Derived oxime according to any one of claims 1 to 12, where the ring T is thiazolyl, triazolopyridines, pyrazinyl, thiadiazolyl, triazolopyridines, triazolopyrimidines, or its pharmaceutically acceptable salt.

17. Derived oxime according to any one of claims 1 to 12, where the ring T is thiazolyl or triazolopyridine, or its pharmaceutically acceptable salt.

18. Derived oxime according to any one of claims 1 to 17, where R5represents (1) hydrogen atom, (2) formyl, (3) halogen atom, (4) oxo, (5) C1-6alkoxy which may be substituted by a group selected the nd from (a) amino, optionally substituted by the same or different 1 or 2 groups selected from C1-6the alkyl and C1-6alkoxycarbonyl; (b) C1-6alkoxycarbonyl; (C) carbamoyl, optionally substituted mono - or di-C1-6by alkyl; (d) carboxyl; (e) hydroxy; (f) a 5-membered heterocycle containing 1 heteroatom selected from nitrogen; (g) three-C1-6alkylsilane; (6) aminosulfonyl, substituted 2 C1-6alkilani, (7) C1-6alkylthio, which may be substituted by an optionally substituted mono - or di-C1-6the alkyl, C1-6alkoxycarbonyl, (8) cyano, (9) 6-membered heterocyclisation containing 2 heteroatoms selected from nitrogen, substituted C1-6the alkyl, (10) nitro, (11)3-8cycloalkyl, (12) C1-6alkoxycarbonyl, (13) C1-6alkenyl, (14)2-7alkanoyl, (15) carbarnoyl, which can be substituted by the same or different 1 to 2 substituents selected from (a) C1-6the alkyl, optionally substituted by hydroxy; 5-membered heterocycle containing 1 heteroatom selected from oxygen; amino, substituted CI-C1-6by alkyl; and 6-membered heteroaryl containing 1 heteroatom selected from nitrogen, (b) (C3-8cycloalkyl, (16) a 5-membered, heteroaromatic containing 3 heteroatoms selected from nitrogen, substituted C1-6by alkyl; (17) amino which may be substituted by the same or different and are 1 or 2 substituents, selected from C1-6of alkyl, C2-7alkanoyl, C1-6alkoxycarbonyl, (18) a 5-membered heteroaryl containing 4 heteroatoms selected from nitrogen, (19) quinil, substitutions hydroxy or amino, substituted CI-C1-6the alkyl, (20) 4-6-membered, heterocyclic containing 1 heteroatom selected from nitrogen, which can be substituted C1-6the alkyl, or (21) C1-6alkyl which may be substituted by same or different 1 to 3 substituents selected from (a) 4-7-membered heterocycle containing 1-2 heteroatoms selected from oxygen, nitrogen or sulfur, or 9-membered bicyclic heterocycle containing 2-4 heteroatoms selected from nitrogen, which can be substituted by the same or different 1 to 3 substituents selected from C1-6of alkyl; oxo; C1-6alkoxy-C2-7alkanoyl; C2-7alkanoyl; C2-7alkanolamine; C3-8cycloalkylcarbonyl; three(halogeno)-C2-7alkanolamine; formylamino; C1-6alkoxycarbonyl; hydroxy; C3-8cycloalkylcarbonyl; three(halogeno)-C1-6of alkyl, C1-6alkoxycarbonyl; formyl; amino, optionally substituted CI-C1-6by alkyl; aminosulfonyl, optionally substituted mono - or di-C1-6the alkyl, C1-6alkylsulfonyl; 6-membered heteroaryl containing 1-2 heteroatoms selected from nitrogen; C1-6alkoxide is of IMT-C 1-6of alkyl, C2-7alkanoyloxy-C2-7alkanoyl; C1-6alkoxycarbonylmethyl; amino-C2-7alkanoyl, substituted CI-C1-6by alkyl; carbamoyl, substituted C1-6by alkyl; hydroxy-C2-7alkanoyl; di(halogeno)-C2-7alkanoyl; 5-membered heterocyclyl-carbonyl containing 1 heteroatom selected from oxygen, substituted oxo; (b) amino which may be substituted by same or different 1 or 2 substituents selected from C1-6of alkyl; carbarnoyl-C1-6of alkyl, substituted CI-C1-6by alkyl; amino-C1-6of alkyl, substituted the same or different 1 or 2 groups selected from C1-6the alkyl and C2-7alkanoyl; C1-6alkoxy-C1-6of alkyl; hydroxy-(C1-6of alkyl; 6-membered heteroaryl containing 1 heteroatom selected from nitrogen; 6-membered heteroaryl-C1-6of alkyl containing 1 heteroatom selected from nitrogen; (C) C1-6alkoxy which may be substituted by hydroxy or C1-6alkoxy, (d) carbamoyl, which is replaced by the same or different 1 or 2 substituents selected from C1-6of alkyl, C1-6alkoxy, (e) hydroxy, (f) three-C1-6alkylsilane, (g) C1-6alkylthio, (h) C1-6alkylsulfonyl, (i) a 6-membered, heterocyclic containing 1 heteroatom selected from nitrogen, which can be substituted C2-7Alcano the scrap, C1-6the alkyl, formyl, C3-8cycloalkylcarbonyl, C1-6alkoxy-C2-7alkanoyl or C1-6alkylsulfonyl, (j) a 5-membered heteroaryl containing 2 heteroatoms selected from nitrogen, (k) hydroxyimino, which may be substituted C1-6alkoxycarbonyl, (l) halogen atom, (m) carboxyl, (n) C1-6alkoxycarbonyl or (o) C2-7alkanoyloxy, or its pharmaceutically acceptable salt.

19. Derived oxime according to any one of claims 1 to 17, where R5represents (1) hydrogen atom, (2) halogen atom, (3) C1-6alkoxy which may be substituted by a group selected from (a) amino, optionally substituted by same or different 1 or 2 groups selected from C1-6the alkyl and C1-6alkoxycarbonyl; (b) C1-6alkoxycarbonyl; (C) carbamoyl, optionally substituted mono - or di-C1-6by alkyl; (d) carboxyl; (e) hydroxy; (f) a 5-membered heterocycle containing 1 heteroatom selected from nitrogen; or (g) three-C1-6alkylsilane; (4) C1-6alkylthio, which may be substituted amino, optionally substituted mono - or di-C1-6by alkyl; or C1-6alkoxycarbonyl, (5) cyano, (6) C3-8cycloalkyl, (7) C2-7alkanoyl, (8) carbarnoyl, which can be substituted by the same or different 1 to 2 substituents selected from substituted or unsubstituted C1-6al the sludge (alternates: 1 or 2 groups, selected from hydroxy; 5-membered heterocycle containing 1 heteroatom selected from oxygen; amino, substituted CI-C1-6by alkyl; a 6-membered heteroaryl containing 1 heteroatom selected from nitrogen), or C3-8cycloalkyl, (9) amino which may be substituted by same or different 1 or 2 zamestitelyami selected from C1-6of alkyl, C2-7alkanoyl, C1-6alkoxycarbonyl, (10) 4-6-membered, heterocyclic containing 1 heteroatom selected from nitrogen, which can be substituted C1-6the alkyl or (11) C1-6alkyl which may be substituted by same or different 1 to 3 substituents selected from (a) 4-7-membered heterocycle containing 1 to 2 heteroatoms selected from oxygen, nitrogen or sulfur, or 9-membered bicyclic heterocycle containing 2-4 heteroatoms selected from nitrogen, which can be substituted by the same or different 1 to 3 substituents selected from C1-6of alkyl; oxo; C1-6alkoxy-C2-7alkanoyl; C2-7alkanoyl; C2-7alkanolamine; C3-8cycloalkylcarbonyl; three(halogeno)-C2-7alkanolamine; formylamino; C1-6alkoxycarbonyl; hydroxy; C3-8cycloalkylcarbonyl; three(halogeno)-C1-6of alkyl, C1-6alkoxycarbonyl; formyl; amino, optionally substituted CI-C1-6by alkyl; aminosulfonyl, long is Ino substituted mono - or di-C 1-6the alkyl, C1-6alkylsulfonyl; 6-membered heteroaryl containing 1-2 heteroatoms selected from nitrogen; C1-6alkoxycarbonyl-C1-6of alkyl, C2-7alkanoyloxy-C2-7alkanoyl; C1-6alkoxycarbonylmethyl; amino-C2-7alkanoyl, substituted CI-C1-6, alkyl; carbamoyl, substituted C1-6by alkyl; hydroxy-(C2-7alkanoyl; di(halogeno)-C2-7alkanoyl; 5-membered geterotsiklicheskikh containing 1 heteroatom selected from oxygen, substituted oxo; (b) amino which may be substituted by same or different 1 or 2 substituents selected from C1-6of alkyl; carbarnoyl-C1-6of alkyl, substituted CI-C1-6by alkyl; amino-C1-6of alkyl, substituted the same or different 1 to 2 groups selected from C1-6the alkyl and C2-7alkanoyl; C1-6alkoxy-C1-6of alkyl; hydroxy-(C1-6of alkyl; 6-membered heteroaryl containing 1 heteroatom selected from nitrogen; 6-membered heteroaryl-C1-6of alkyl containing 1 heteroatom selected from nitrogen, (C) C1-6alkoxy which may be substituted by hydroxy or C1-6alkoxy, (d) carbamoyl, which is replaced by the same or different 1 or 2 substituents selected from C1-6of alkyl, C1-6alkoxy, (e) hydroxy, (f) three-C1-6alkylsilane, (g) C1-6alkylthio, (h) C1-6 alkylsulfonyl, (i) a 6-membered, heterocyclic containing 1 heteroatom selected from nitrogen, which can be substituted C2-7alkanoyl, C1-6the alkyl, formyl, C3-8cycloalkylcarbonyl, C1-6alkoxy-C2-7alkanoyl or C1-6alkylsulfonyl, (j) a 5-membered heteroaryl containing 2 heteroatoms selected from nitrogen, (K), hydroxyimino, which may be substituted C1-6alkoxy-carbonyl, (l) halogen atom, (m) carboxyl, (n) C1-6alkoxycarbonyl or (o) C2-7alkanoyloxy, or farmaceutiske acceptable salt.

20. Derived oxime according to any one of claims 1 to 17, where R5represents (1) halogen atom, (2) C1-6alkoxy which may be substituted by a group selected from (a) amino, optionally substituted by same or different 1 or 2 groups selected from C1-6the alkyl and C1-6alkoxycarbonyl; (b) C1-6alkoxycarbonyl; (C) carbamoyl, which may be substituted mono - or di-C1-6by alkyl; (d) carboxyl; (e) hydroxy; (f) a 5-membered heterocycle containing 1 heteroatom selected from oxygen or nitrogen, or (g) three-C1-6alkylsilane; (3) C1-6alkylthio, which may be substituted amino, optionally substituted mono - or di-C1-6by alkyl; or C1-6alkoxycarbonyl, (4) amino which may be substituted by same or different 1 or 2 Zam is a Fort worth, selected from C1-6of alkyl, C2-7alkanoyl, C1-6alkoxycarbonyl, (5) 4-6-membered, heterocyclic containing 1 heteroatom selected from nitrogen, which can be substituted C1-6the alkyl or (6) C1-6alkyl which may be substituted by same or different 1 to 3 substituents selected from (a) 4-7-membered heterocycle containing 1-2 heteroatoms selected from oxygen, nitrogen or sulfur, or 9-membered bicyclic heterocycle containing 2-4 heteroatoms selected from nitrogen, which can be substituted by the same or different 1 to 3 substituents selected from C1-6of alkyl; oxo; C1-6alkoxy-C2-7alkanoyl; C2-7alkanoyl; C2-7alkanolamine; C3-8cycloalkylcarbonyl; three(halogeno)-C2-7alkanolamine; formylamino; C1-6alkoxycarbonyl; hydroxy; C3-8cycloalkylcarbonyl; three(halogeno)-C1-6of alkyl, C1-6alkoxycarbonyl; formyl; amino, optionally substituted CI-C1-6by alkyl; aminosulfonyl, optionally substituted mono - or di-C1-6the alkyl, C1-6alkylsulfonyl; 6-membered heteroaryl containing 1-2 heteroatoms selected from nitrogen; C1-6alkoxycarbonyl-C1-6of alkyl, C2-7alkanoyloxy-C2-7alkanoyl; C1-6alkoxycarbonylmethyl; amino-C2-7alkanoyl, substituted di- 1-6by alkyl; carbamoyl, substituted C1-6by alkyl; hydroxy-(C2-7alkanoyl; di(halogeno)-C2-7alkanoyl; 5-membered geterotsiklicheskikh containing 1 heteroatom selected from oxygen, substituted oxo; (b) amino which may be substituted by same or different 1 or 2 substituents selected from C1-6of alkyl; carbarnoyl-C1-6of alkyl, substituted CI-C1-6by alkyl; amino-C1-6of alkyl, substituted the same or different 1 or 2 groups selected from C1-6the alkyl and C2-7alkanoyl; C1-6alkoxy-C1-6of alkyl; hydroxy-(C1-6of alkyl; 6-membered heteroaryl containing 1 heteroatom selected from nitrogen; 6-membered heteroaryl-C1-6of alkyl containing 1 heteroatom selected from nitrogen, (C) C1-6alkoxy which may be substituted by hydroxy or C1-6alkoxy, (d) carbamoyl, which is replaced by the same or different 1 or 2 substituents selected from C1-6of alkyl, C1-6alkoxy, (e) hydroxy, (f) three-C1-6alkylsilane, (g) C1-6alkylthio, (h) C1-6alkylsulfonyl, (i) a 6-membered, heterocyclic containing 1 heteroatom selected from nitrogen, which can be substituted C2-7alkanoyl, C1-6the alkyl, formyl, C3-8cycloalkylcarbonyl, C1-6alkoxy-C2-7alkanoyl or C1-6alkylsulfonyl, (j) 5-h of the military heteroaryl, containing 2 heteroatoms selected from nitrogen, (k) hydroxyimino, which may be substituted C1-6alkoxycarbonyl, (l) halogen atom, (m) carboxyl, (n) C1-6alkoxycarbonyl or (o) C2-7alkanoyloxy, or its pharmaceutically acceptable salt.

21. Derived oxime according to any one of claims 1 to 17, where R5represents (1) C1-6alkoxy which may be substituted by a group selected from (a) amino, optionally substituted by same or different 1 or 2 groups selected from C1-6the alkyl and C1-6alkoxycarbonyl; (b) C1-6alkoxycarbonyl; (C) carbamoyl, optionally substituted mono - or di-C1-6by alkyl; (d) carboxyl; (e) hydroxy; (f) a 5-membered heterocycle containing 1 heteroatom selected from nitrogen, or (g) three-C1-6alkylsilane; (2) amino which may be substituted by same or different 1 or 2 substituents selected from C1-6of alkyl, C2-7alkanoyl, C1-6alkoxycarbonyl, (3) 4-6-membered, heterocyclic containing 1 heteroatom selected from nitrogen, which can be substituted C1-6the alkyl or (4) C1-6alkyl which may be substituted by same or different 1 to 3 substituents selected from (a) 4-7-membered heterocycle containing 1-2 heteroatoms selected from oxygen, sulfur or nitrogen, or a 9-membered bicyclic heterocycle, which contains Amigo 2-4 heteroatoms, selected from nitrogen, which can be substituted by the same or different 1 to 3 substituents selected from C1-6of alkyl; oxo; C1-6alkoxy-C2-7alkanoyl; C2-7alkanoyl; C2-7alkanolamine; C3-8cycloalkylcarbonyl; three(halogeno)-C2-7alkanolamine; formylamino; C1-6alkoxycarbonyl; hydroxy; C3-8cycloalkylcarbonyl; three(halogeno)-C1-6of alkyl, C1-6alkoxycarbonyl; formyl; amino, optionally substituted CI-C1-6by alkyl; aminosulfonyl, optionally substituted mono - or di-C1-6the alkyl, C1-6alkylsulfonyl; 6-membered heteroaryl containing 1-2 heteroatoms selected from nitrogen; C1-6alkoxycarbonyl-C1-6of alkyl, C2-7alkanoyloxy-C2-7alkanoyl; C1-6alkoxycarbonylmethyl; amino-C2-7alkanoyl, substituted CI-C1-6by alkyl; carbamoyl, substituted C1-6by alkyl; hydroxy-(C2-7alkanoyl; di(halogeno)-C2-7alkanoyl; 5-membered heterocyclyl-carbonyl containing 1 heteroatom selected from oxygen, substituted oxo; (b) amino which may be substituted by same or different 1 or 2 substituents selected from C1-6of alkyl; carbarnoyl-C1-6of alkyl, substituted CI-C1-6by alkyl; amino-C1-6of alkyl, substituted the same or different 1 or 2 Gy is pami, selected from C1-6the alkyl and C2-7alkanoyl; C1-6alkoxy-C1-6of alkyl; hydroxy-(C1-6of alkyl; 6-membered heteroaryl containing 1 heteroatom selected from nitrogen; 6-membered heteroaryl-C1-6of alkyl containing 1 heteroatom selected from nitrogen, (C) C1-6alkoxy which may be substituted by hydroxy or C1-6alkoxy, (d) carbamoyl, which may be substituted, odinakovimi or different 1 or 2 substituents selected from C1-6the alkyl or C1-6alkoxy, (e) hydroxy, (f) three-C1-6alcolici, (g) C1-6alkylthio, (h) C1-6alkylsulfonyl, (i) a 6-membered, heterocyclic containing 1 heteroatom selected from nitrogen, which can be substituted C2-7alkanoyl, C1-6the alkyl, formyl, C3-8cycloalkylcarbonyl, C1-6alkoxy-C2-7alkanoyl, C1-6alkylsulfonyl, (j) a 5-membered heteroaryl containing 2 heteroatoms selected from nitrogen, (k) hydroxyimino, which may be substituted C1-6alkoxycarbonyl, (l) halogen atom, (m) carboxyl, (n) C1-6alkoxycarbonyl or (o) C2-7alkanoyloxy, or its pharmaceutically acceptable salt.

22. Derived oxime according to any one of claims 1 to 21, where R6represents a hydrogen atom or a C1-6alkyl, or its pharmaceutically acceptable salt.

23. Derived oxime any ISP-21, where R6represents a hydrogen atom, or its pharmaceutically acceptable salt.

24. Derived oxime according to any one of claims 1 to 23, where ring a is a phenyl, Q means 3-tetrahydrofuryl, ring T is a 2-thiazolyl, one of R1and R2represents a hydrogen atom, and the other cyclopropanesulfonyl, both of R3and R4are a hydrogen atom, R5represents a C1-6alkyl, substituted piperazinil, optionally substituted by 1-3 substituents selected from C1-6of alkyl, oxo, C2-7alkanoyl and C1-6alkoxy-C2-7alkanoyl, or its pharmaceutically acceptable salt.

25. Derived oxime according to claim 1, chosen from:
(2E)-2-[4-(cyclopropanesulfonyl)phenyl]-N-{5-[(4-methylpiperazin-1-yl)methyl]-1,3-thiazol-2-yl}-2-{[(3R)-tetrahydrofuran-3-yloxy]imino}ndimethylacetamide;
(2E)-2-[4-(cyclopropanesulfonyl)phenyl]-N-(5-{[(3S)-4-(methoxyacetyl)-3-methylpiperazin-1-yl]methyl}-1,3-thiazol-2-yl)-2-{[(3R)-tetrahydrofuran-3-yloxy]imino}ndimethylacetamide;
(2E)-N-(5-{[(3S)-4-acetyl-3-methylpiperazin-1-yl]methyl}-1,3-thiazol-2-yl)-2-[4-(cyclopropanesulfonyl)phenyl]-2-{[(3R)-tetrahydrofuran-3-yloxy]imino}ndimethylacetamide;
(2E)-N-{5-[(4-acetylpiperidine-1-yl)methyl]-1,3-thiazol-2-yl}-2-[4-(cyclopropanesulfonyl)phenyl]-2-{[(3R)-tetrahydrofuran-3-yloxy]imino}ndimethylacetamide;
(2E)-2-[4-(cyclopropanesulfonyl)phenyl]-N-[5-(methoxymethyl)-1,3-thiazol-2-yl]-2-{[(3)-tetrahydrofuran-3-yloxy]imino}ndimethylacetamide;
(2E)-2-[4-(cyclopropanesulfonyl)phenyl]-N-(5-{[(3S)-3,4-dimethylpiperidin-1-yl]methyl}-1,3-thiazol-2-yl)-2-{[(3R)-tetrahydrofuran-3-yloxy]imino}ndimethylacetamide;
(2E)-2-[4-(cyclopropanesulfonyl)phenyl]-N-(5-{[(3S)-4-glycol-3-methylpiperazin-1-yl]methyl}-1,3-thiazol-2-yl)-2-{[(3R)-tetrahydrofuran-3-yloxy]imino}ndimethylacetamide;
(2E)-2-[4-(cyclopropanesulfonyl)phenyl]-N-(5-{[(3S)-4-formyl-3-methylpiperazin-1-yl]methyl}-1,3-thiazol-2-yl)-2-{[(3R)-tetrahydrofuran-3-yloxy]imino)ndimethylacetamide;
(2E)-N-(5-{[(1-acetylpiperidine-4-yl)oxy]methyl}-1,3-thiazol-2-yl)-2-[4-(cyclopropanesulfonyl)phenyl]-2-{[(3R)-tetrahydrofuran-3-yloxy]imino}ndimethylacetamide; or
(2E)-2-[4-(cyclopropanesulfonyl)phenyl]-N-{5-[(1-methylpiperidin-4-yl)thio]-1,3-thiazol-2-yl}-2-{[(3R)-tetrahydrofuran-3-yloxy]imino}ndimethylacetamide,
or their pharmaceutically acceptable salts.

26. The method of deriving the oxime of General formula [I]:

where all symbols have the same meanings as defined in claim 1, including the interaction of the compounds of General formula [II]:

where Z2represents a hydrogen atom or a C1-6alkyl, and other symbols have the same meanings as defined in claim 1, with a compound of General formula [III]:

where the symbols have the same meanings as defined in claim 1.

27. The method of deriving the oxime of General formula [I]:

where the symbols have the same meanings as defined in claim 1, including the interaction of the compounds of General formula [IX]:

where the symbols have the same meanings as defined in claim 1 with a compound of General formula [V]:

where Z3represents hydroxy, halogen atom, 6-14-membered, arylsulfonate or C1-6alkylsulfonate, and the other symbol has the same meaning as defined in claim 1.

28. The method of deriving the oxime of General formula [I]:

where the symbols have the same meanings as defined in claim 1, including the interaction of the compounds of General formula [X]:

where the symbols have the same meanings as defined in claim 1, with a compound of General formula [XI]:

where the symbols have the same meanings as defined in claim 1.

29. The compound according to any one of claims 1 to 25 or its pharmaceutically acceptable salt, which exhibits the properties of a glucokinase activator.

30. Pharmaceutical composition for treatment or prevention of diabetes or complications of diabetes, including retinopathy, nephropathy, neuropathy, ischemic heart disease, atherosclerosis or obesity, comprising as active ingredient a compound according to any one of claims 1 to 25 or FA is matemticas acceptable salt.

31. The use of compounds according to any one of claims 1 to 25 or its pharmaceutically acceptable salts in the manufacture of a medicinal product for the treatment or prevention of diabetes, or complications associated with diabetes, including retinopathy, nephropathy, neuropathy, ischemic heart disease, atherosclerosis or obesity.

32. Pharmaceutical composition having the properties of a glucokinase activator containing as active ingredient a compound according to any one of claims 1 to 25 or its pharmaceutically acceptable salt and a pharmaceutically acceptable carrier.

33. The use of compounds according to any one of claims 1 to 25 or its pharmaceutically acceptable salts in the manufacture of a medicinal product having the properties of a glucokinase activator.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula

wherein Q together with carbon and nitrogen atoms whereto attached forms a 5-6-members monocyclic heteroaromatic ring; or Q together with carbon and nitrogen atoms whereto attached forms a 9-10-members bicyclic heterocycle; R1 and R2 independently mean hydrogen, halogen, alkyl, alkyl substituted by one or more halogen, alkoxygroup, alkoxygroup substituted by alkoxygroup, alkylthiogroup, sulphonyl, free or etherified carboxygroup, carbamoyl, sulohamoyl, morpholinyl or pyridinyl; or R2 is absent; R3 means (C3-C6)cycloalkyl; R4 means hydrogen, halogen, lower alkyl or lowest alkyl substituted by one or more halogen; R5 means (C3-C6cycloalkyl, (C6-C10) aryl, (C3-C10)heterocyclyl or (C1-C6)alkyl optionally substituted by (C1-C6)alkoxygroup, (C3-C7)cycloalkyl, (C6-C10)aryl or (C3-C10)heterocyclyl; R6 means free or etherified carboxygroup; and n is an integer equal to 1-6; or to its enanthiomer, or a mixture of its enanthiomers, or its pharmaceutically acceptable salt. Besides, the invention refers to a method of glucokinase activation in mammals, to a method of treating pathological conditions associated with glucokinase activation in mammals and impaired glucose tolerance, as well as to a pharmaceutical composition based on these compounds and to application of said compositions for preparing a drug.

EFFECT: there are produced and described new compounds which are activators and can be used as therapeutic agents for treating the glucokinase mediated pathological conditions.

31 cl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a derivative of 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine of formula

and its optical isomers and pharmaceutically acceptable salts where R1 represents CH3 or CH3CH2; R2 represents H, 2-F, 2-Cl, 3-F, 3-OCN3, 3-CN, 3-CF3, 3-CONH2 or 3-SO2CH3; R3 represents H or CH3; R4 represents H or CH3; and R5 represents H; or when R4 represents CH3, R5 represents H or F. Also, the invention refers to methods for producing the compounds of formula (I) and to pharmaceutical compositions exhibiting CX3CR1 receptor antagonist properties containing the compounds of formula (I).

EFFECT: production of 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine as selective CX3CR1 receptor antagonists.

15 cl, 2 tbl, 18 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to compounds (la) of formula applied as tyrosine kinase c-Met inhibitors. , where: LA is selected from ,

or ; RA is selected from:

or each RA2 and RA6 represents hydrogen; RA3 represents RAr; or RA3, RA4 and carbon atoms whereto attached form 6-members aryl, optionally substituted, in the amount up to 4 by independent groups RAr, or a 5-6-members heterocyclyl or heteroaryl ring containing at least one O, N or S atom; R represents -OH; RA5 represents hydrogen or RAr; LB represents a covalent bond or -N(R*)-; RB represents halogen, NH2 or C1-8aliphatic group, optionally substituted by R; a 6-10-members aryl ring; a 3-7-members carbocyclyl ring, a 5-10-members heteroaryl ring containing 1-4 heteroatoms independently selected from nitrogen, oxygen and sulphur atoms, where each said aryl or heteroaryl ring is optionally substituted, in the amount up to five by independent groups RAr; R represents halogen, -R°, -SR°, Ph, optionally substituted R° or -C(O)OR°; each RAr is independently selected from halogen, -R°, -OR°, -SR°, Ph, optionally substituted in the amount up to five by independent groups -R°, -CN, -N(R°)2 or -C(O)OR°; or two adjacent groups RAr taken together, represent 1,2-methylenedixy or 1,2-ethylenedixy; each R* represents hydrogen; and each R° represents independently hydrogen, an optionally substituted C1-6aliphatic radical or an unsubstituted 5-6-members heteroaryl or heterocyclic ring containing 1-3 heteroatoms independently selected from nitrogen, oxygen and sulphur atoms.

EFFECT: invention refers to pharmaceutically acceptable compositions containing the compounds under the invention, and methods of application of the compositions in treatment of various proliferative disorders.

10 cl, 4 tbl, 548 ex, 9 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to azole derivatives of formula I , where: A denotes S, O; W denotes -(C=O)-; X are identical or different and denote =C(-R)- or =N-; Y denotes -O- or -NR1-; R denotes hydrogen, halogen, (C1-C6)-alkyl, nitro; R1 denotes hydrogen; R2 denotes (C5-C16)-alkyl, (C1-C4)alkyl-phenyl, where phenyl can be optionally mono- or poly-substituted with (C1-C6)-alkyl; R3 denotes hydrogen; or R2 and R3 together with the nitrogen atom bearing them can form a monocyclic saturated 6-member ring system, where separate members of this ring system can be substituted with 1 group selected from the following: -CHR5-, -NR5-; R5 denotes (C1-C6)-alkyl, trifluoromethyl; and physiologically acceptable salts thereof. The invention also pertains to methods of producing said compounds and a medicinal agent based on said compounds.

EFFECT: novel compounds and a medicinal agent based on said compounds are obtained, which can be used as hormone-sensitive lipase (HSL) or endothelial lipase (EL) inhibitors.

12 cl, 11 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel sulphonamidethiazole pyrimidine derivatives of formula (I)

, which are glucokinase activators or to their enantiomers, mixture of enantiomers or pharmaceutically acceptable salts. The invention also relates to a pharmaceutical composition based on the novel compounds, use of the compounds to prepare a medicinal agent and to a method of activating glucokinase. In formula (I) R1 denotes (C1-C10)alkoxy, R2 denotes (C3-C6)cycloalkyl, R3 denotes hydrogen, and values of substitutes R4 and R5 are given in the formula of invention.

EFFECT: more effective use of the compounds.

33 cl, 166 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: medicine, pharmaceutics.

SUBSTANCE: invention refers to derivatives of 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidine-2(3H)-one of formula (I) where R1 represents CH3 or CH3CH2; R2 represents H, 3-CN, 2-CF3, 2-F, 3-F, 3-CF3, 3-CONH2 or SO2CH3; R3 represents H; R4 represents H or CH3; and R5 represents H; or, when R4 represents CH3, R5 represents H or F; and to its pharmaceutically acceptable salts. Also, the invention refers to a pharmaceutical composition exhibiting properties of CX3CR1 receptor antagonist containing compound (I) of formula or its pharmaceutically acceptable salt mixed with a pharmaceutically acceptable diluent or carrier.

EFFECT: enabled administration of the derivatives of 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidine-2(3H)-one as selective CX3CR1 receptor antagonists.

13 cl, 1 tbl, 20 ex

FIELD: chemistry.

SUBSTANCE: invention relates to 3-cyclohexylaminomethylthiazole[3,2-a]benzimidazole dihydrochloride of formula I: , having immunotropic and anti-aggregation activity.

EFFECT: novel compounds have useful biological properties.

2 cl, 8 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds which possess inhibiting properties with respect to PI3-kinase of general formula (1), where R1 is selected from group, including -NHRC, -NHC(O)Rc, -NHC(O)ORc, -NHC(O)NRcRc and -NHC(O)SRc, R2 stands for residue, optionally substituted with one or two substituents R4, selected from group, including C1-C6alkyl, C3-C8cycloalkyl, 5-6-member heterocycloalkyl with one heteroatom, selected from nitrogen and sulphur, phenyl, benzyl and 5-6-member heteroaryl, including 1-2 nitrogen atoms, R3 stands for optionally substituted with one or several substituents Re and/or Rf residue, selected from group, including phenyl and 5-6-member heteroaryl with 1-3 heteroatoms, selected from nitrogen and oxygen, R4 represents residue, selected from group, including Ra, Rb, and substituted with one or several identical or different substituents Rc and/or Rb , Ra in each case is independently selected from group, including C1-C6alkyl, phenyl, 4-7-member heterocycloalkyl with 1-2 heteroatoms, selected from nitrogen and oxygen, and 9-member heteroaryl with one atom of nitrogen as heteroatom, Rb in each case is independently selected from group, including =O, -ORc, -NRCRC, halogen, -CF3, -CN, -S(O)Rc, -C(O)Rc, -C(O)ORc, -C(O)NRcRc, -C(O)N(Rg)NRcRc, -N(Rg)C(O)Rc, -N(Rg)S(O)2Rc, -N(Rg)S(O)2NRcRc, -N(Rg)C(O)ORc and -N(Rg)C(O)NRcRc, RC in each case independently represents hydrogen or optionally substituted with one or two identical or different substituents R and/or Re residue, selected from group, including C1-C6alkyl, C3-C8cycloalkyl, C6-C9aryl, 4-7-member heterocycloalkyl with 1-2 heteroatoms, selected from nitrogen and oxygen, and 5-6-member heteroaryl with 1-2 heteroatoms, selected from nitrogen, oxygen and sulphur, Rd in each case independently represents hydrogen or optionally substituted with one or two identical or different substituents Re and/or Rf residue, selected from group, including C1-C6alkyl, C3-C8cycloalkyl, phenyl, 4-7-member heterocycloalkyl with 1-2 heteroatoms, selected from nitrogen and oxygen, and 5-10-member heteroaryl with one atom of nitrogen, Re in each case is independently selected from group, including =O, -ORf, -SRf, -NRfRf, -CN, -S(O)2Rf, -C(O)Rf, -C(O)ORf, -C(O)NRfRf and -OC(O)Rf, Rf in each case independently represents hydrogen or optionally substituted with one or two identical or different substituents Rg residue, selected from group, including C1-C6alkyl, C3-C8cycloalkyl, phenyl, 4-7-member heterocycloalkyl with 1-2 heteroatoms, selected from nitrogen and oxygen and 5-6-member heteroaryl with one heteroatom, selected from nitrogen and sulphur, Rg in each case independently represents hydrogen, C1-C6alkyl, C3-C8cycloalkyl and 4-7-member heterocycloalkyl with one nitrogen as heteroatom, as well as to their pharmaceutically harmless acid-additive salts. Invention also relates to compounds, used as intermediate products of synthesis of formula (I) compounds, pharmaceutical composition and application of compounds for preparation of medication, possessing properties of PI3-kinase inhibitor.

EFFECT: elaborated are novel compounds, which possess properties of PI3-kinase inhibitor.

11 cl, 9 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to compounds of formula (I) and formula (II), their tautomers and pharmaceutically acceptable salts. In formula (I) and in formula (II), X - S; R1 - H; R2 - NR5R6; R3 - 5-6-member heteroaryl with 1 heteroatom, selected from N and S, or phenyl, optionally substituted with one or two substituents, selected from halogen, amino, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-halogenalkyl and C1-C6-halogenalkoxy; R4 - H, C1-C6 alkyl, C1-C6 alkoxy or XR3, where X and R3 are determined above; R5 - H; R6 - H; L - N or CR7, where R7 - H; M - S. Invention also relates to pharmaceutical composition, containing as active component invention compound, to method of inhibiting activity of caseinkinase lε and to method of obtaining compounds of formula (I) or formula (II).

EFFECT: compounds of claimed invention possess properties of casein kinase lε inhibitors.

13 cl, 5 tbl, 44 ex

FIELD: medicine.

SUBSTANCE: compounds can be used for treating neurological conditions, more specifically for treating neurodegenerative conditions, such as Alzheimer's disease. In a compound of formula I R2 represents H or CH2NR1R4 where R1 and R4 are independently selected from H, unsubstituted C1-6alkyl, substituted or unsubstituted C3-6 cycloalkyl, R3 represents H; substituted or unsubstituted C1-4alkyl; substituted or unsubstituted C2-4alkenyl; substituted or unsubstituted 6-members aryl condensed or uncondensed with substituted or unsubstituted 6-members aryl or 5-6-members heteroaryl, containing 1-2 nitrogen atoms in a cycle; substituted or unsubstituted saturated or unsaturated 5 or 6-members N-containing heterocycle which can additionally contain nitrogen, oxygen or the sulphur atom condensed or ucondensed with substituted or unsubstituted 6-members aryl or 5-6-members heteroaryl containing nitrogen in a cycle; (CH2)nR6 where n is an integer from 1 to 6, and the values of R6 and the values of other radicals are specified in the patent claim.

EFFECT: increased antiamyloidogenic action.

20 cl, 20 tbl, 6 dwg, 7 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I): where: A is a monocyclic or polycyclic aryl or heteroaryl group, where the heteroaryl radical denotes a 5-10-member cyclic system containing at least one heteroaromatic ring and containing at least one heteroatom selected from O, S and N; optionally substituted with one or more substitutes independently selected from a group comprising halogen atoms, C1-4alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-4alkyl, C1-4alkoxy and a hydroxyl group; B is a monocyclic nitrogen-containing heteroaryl group, where the heteroaryl radical denotes a 5-6-member heteroaromatic ring containing at least one heteroatom selected from S and N; optionally substituted with one or more substitutes selected from a group consisting of halogen atoms, C1-4alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-4alkyl, aryl and C1-8alkylthio; either a) R1 is a group of formula: -L-(CR'R")n-G, where L is a binding group selected from a group consisting of a direct bond, -(CO)-, -(CO)NR'- and -SO2-; R' and R" is independently selected from hydrogen atoms; n assumes values from 0 to 1; and G is selected from a group consisting of a hydrogen atom and C1-4alkyl, aryl, heteroaryl, where the heteroaryl radical denotes a 5-6-member heteroaromatic ring containing at least one heteroatom selected from O, S and N; C3-8cycloalkyl and saturated heterocyclic groups, where heterocyclic group denotes a non-aromatic saturated 6-member carbocyclic ring in which one or two carbon atoms are substituted with a N heteroatom; where alkyl, C3-8cycloalkyl, aryl or heteroaryl groups are unsubstituted or substituted with one or more substitutes selected from halogen atoms; and R2 is a group selected from hydrogen atoms, halogen atoms and C1-4alkyl, C2-5alkynyl, C1-4alkoxy, -NH2 and cyano groups, where alkyl and alkynyl groups may be unsubstituted or substituted with one aryl group; or b) R2, R1 and -NH- group to which R1 is bonded form a group selected from groups of formulae and , where: Ra is selected from a hydrogen atom or groups selected from C1-4alkyl, C3-8cycloalkyl, aryl, aryl-C1-4alkyl, heteroaryl, where the heteroaryl radical denotes a 5-6-member heteroaromatic ring containing at least one heteroatom selected from O and N; saturated heterocyclic rings, where the heterocyclic group denotes a non-aromatic saturated 6-member carbocyclic ring in which one carbon atom is substituted with a heteroatom selected from O and N; and C1-4alkylthio; where the aryl or heteroaryl groups are unsubstituted or substituted with one or more groups selected from halogen atoms, cyano group, trifluoromethoxy and carbamoyl; Rb denotes hydrogen; and pharmaceutically acceptable salts thereof and N-oxides; provided that the compound is not selected from N-[6-(1-methyl-1H-indol-3-yl)-5-pyridin-2-ylpyrazin-2-yl]benzamide, N-[3-ethoxycarbonyl-6-(1-methyl-1H-indol-3-yl)-5-pyridin-2-ylpyrazin-2-yl]benzamide, and N-[3-ethoxycarbonyl-6-(1-methyl-1H-indol-3-yl)-5-pyridin-2-ylpyrazin-2-yl]formamide. The invention also relates to a pharmaceutical composition, use of compounds in any of claims 1-20, a method of treating a subject, as well as a composite product.

EFFECT: obtaining novel biologically active compounds having adenosine A2B receptor antagonist activity.

27 cl, 160 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted 2-quinolyloxazoles of formula (I) or pharmaceutically acceptable salts thereof, having PDE4 inhibiting properties, a pharmaceutical composition based on said compounds and use thereof to prepare a medicinal agent which inhibits inflammatory cell recruitment in respiratory tracts. , where is , X is O, R1 is alkyl, R3 and R4 are independently selected from H, R5 and R6 are independently selected from a group comprising H, alkyl, hydroxyalkyl, t equals 1 or 2. Values of substitutes R7-R11, R13 are given in the formula of invention.

EFFECT: high efficiency of using the composition.

24 cl, 1 dwg, 64 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to oxazolidinone derivatives covered by general graphic formula (I) and to their pharmaceutically acceptable salts. In formula (I) R1, R2, R3 and R4 are independently chosen from a group including -H and halogen; A is chosen from a group including R5 and R6 are independently chosen from a group including -H, -F, -CI, -Br, -OH, alkyl(C1-C6), haloalkyl(C1-C6), alkoxygroup(C1-C6); R7 is chosen from a group including -H, alkyl(C1-C6); either R7 and R5 or R6 taken together form a cycle of 2 carbon atoms and include 1 group chosen from O which in turn can be substituted by one substitute chosen from alkyl(C1-C6); R12 is chosen from a group including -H, -COR14, -CSR14, -COOR14; R14 is chosen from a group including alkyl (C1-C6), cycloalkyl(C3-C6), alkenyl(C2-C6), R16, R17 and R18 represent -H; R21 is chosen from a group including -H, alkyl(C1-C6); X is chosen from a group including O, S, and Y is chosen from a group including O, S, SO, SO2, and NR12; and optional substitutes of alkyl(C1-C6) groups can represent one or two groups chosen from the following: -OR21, -CN.

EFFECT: invention refers to methods for preparing the compounds of the invention, to application of oxazolidinone derivatives for preparing a drug for treating bacterial infections and to a pharmaceutical composition for treating bacterial infections, including a therapeutically effective amount of the compound of the invention.

36 cl, 10 tbl, 44 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates or tautomers thereof, where substitute M is selected from groups D1 and D2, having structural formulae given below, and R1, E, A and X are as described in the formula of invention. Disclosed also are pharmaceutical compositions which contain these compounds, methods for synthesis of these compounds, intermediate compounds and synthesis methods thereof, as well as use of compounds of formula (I) in preventing or treating diseases mediated by CDK kinases, GSK-3 kinases or Aurora kinases.

EFFECT: high effectiveness of the compounds.

40 cl, 8 dwg, 18 tbl, 84 ex

Aromatic compound // 2416608

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

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.

SUBSTANCE: compounds can be used for treating neurological conditions, more specifically for treating neurodegenerative conditions, such as Alzheimer's disease. In a compound of formula I R2 represents H or CH2NR1R4 where R1 and R4 are independently selected from H, unsubstituted C1-6alkyl, substituted or unsubstituted C3-6 cycloalkyl, R3 represents H; substituted or unsubstituted C1-4alkyl; substituted or unsubstituted C2-4alkenyl; substituted or unsubstituted 6-members aryl condensed or uncondensed with substituted or unsubstituted 6-members aryl or 5-6-members heteroaryl, containing 1-2 nitrogen atoms in a cycle; substituted or unsubstituted saturated or unsaturated 5 or 6-members N-containing heterocycle which can additionally contain nitrogen, oxygen or the sulphur atom condensed or ucondensed with substituted or unsubstituted 6-members aryl or 5-6-members heteroaryl containing nitrogen in a cycle; (CH2)nR6 where n is an integer from 1 to 6, and the values of R6 and the values of other radicals are specified in the patent claim.

EFFECT: increased antiamyloidogenic action.

20 cl, 20 tbl, 6 dwg, 7 ex

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