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Cinnamic acid compounds (versions), intermediate compounds for their obtaining, based on them pharmaceutical composition, method of inhibiting histone diacetase, method of treating diabetes, method of treating tumour or disease associated with cell proliferation, method of enhancing axon growth and method of treating neurodegenerative diseases and spinal muscular atrophy
Cinnamic acid compounds (versions), intermediate compounds for their obtaining, based on them pharmaceutical composition, method of inhibiting histone diacetase, method of treating diabetes, method of treating tumour or disease associated with cell proliferation, method of enhancing axon growth and method of treating neurodegenerative diseases and spinal muscular atrophy
IPC classes for russian patent Cinnamic acid compounds (versions), intermediate compounds for their obtaining, based on them pharmaceutical composition, method of inhibiting histone diacetase, method of treating diabetes, method of treating tumour or disease associated with cell proliferation, method of enhancing axon growth and method of treating neurodegenerative diseases and spinal muscular atrophy (RU 2492163):
Another patents in same IPC classes:
Intermediate compounds and methods of synthesis of analogues of halichondrin b Intermediate compounds and methods of synthesis of analogues of halichondrin b / 2489437
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Claimed invention relates to compounds of formula (I) or to their pharmaceutically acceptable salts, in which X is selected from group, consisting of-C(R1)2-, -O-, -S-, -S(O2)-, -NR1-; each R1 is independently selected from group consisting of H and alkyl; each of R2, R3 and R4 is independently selected from group consisting of (1) H, (2) alkyl, (3) -OR5, (4) alkylene-OR5, (5) -alkylene-R6, (6) -C(O)O-alkyl, (7) - alkylene-C(O)O-alkyl, (8) -alkylene-R8, (9) -NHR5, (10) -N(R5)2, (11) alkenyl, (12) -NH-R8, (13) -NH-CH(C(O)O(C1-C6)alkyl)-alkylene-O-alkyleneR6, (14)-NHCH(C(O)O(C1-C6)aalkyl)-alkylene-OH, (15) -NH-C(O)-alkenyl and (16) -N(C1-C6alkyl)C(O)-alkenyl; or R2 and R3 or R2 and R4 or R3 and R4 together with atoms with which they are bound, form condensed 3-7-member cycloalkyl or heterocycloalkyl ring, which represents non-aromatic monocyclic ring system, which contains in ring from about 5 to about 7 atoms, and one or several atoms in ring system represent atom of element, different from carbon, for instance, nitrogen or oxygen, and said condensed cycloalkyl or heterocycloalkyl ring is not substituted or is substituted with one or several groups L3 ; and on condition that if X represents -O-, and m equals 1, then, at least, one of R2, R3 or R4 is not H; each R5 is independently selected from group consisting of (1) H, (2) (C1-C6)alkyl, (3) hydroxy-substituted alkyl, (4) R6, (5) R7, (6) -C(O)-(C1-C6)alkyl, (7) -C(O)-(C1-C6)halogenalkyl, (8) -C(O)-R6, (9) -C(O)-R7, (10) -C(O)NH-(C1-C6)alkyl, (11) -C(O)N((C1-C6)alkyl)2, in which each alkyl group is selected independently, (12) -S(O)2-(C1-C6)alkyl, (13) -S(O)2-(C1-C6)halogenalkyl, (14) -S(O)2-R6, (15) -S(O)2-R7, (16) -S(O)2-R8, (17) -alkylene-C(O)-(C1-C6)alkyl, (18) -alkylene-C(O)-(C1-C6)halogen-alkyl, (19) -alkylene-C(O)-R6, (20) -alkylene-C(O)-R7, (21) -alkylene-S(O)2-(C1-C6)alkyl, (22) -alkylene-S(O)2-(C1-C6)halogenalkyl, (23) -alkylene-S(O)2-R6, (24) -alkylene-S(O)2-R7, (25) -alkylene-S(O)2-R8, (26) -alkylene-NHC(O)-(C1-C6)alkyl, (27) -alkylene-NHC(O)-(C1-C6)halogenalkyl, (28) alkylene-NHC(O)-R6, (29) -alkylene-NHC(O)-R7, (30) -alkylene-NHS(O)2-(C1-C6)alkyl, (31) -alkylene-NHS(O)2-(C1-C6)halogenalkyl, (32) -alkylene-NHS(O)2-R6, (33) -alkylene-NHS(O)2-R7, (34) -alkylene-N(alkyl)C(O)-(C1-C6)alkyl, (35) -alkylene-N(alkyl)C(O)-(C1-C6)halogenalkyl, (36) -alkylene-N(alkyl)C(O)-R6, (37) -alkylene-N(alkyl)C(O)-R7, (38) -alkylene-N(alkyl)S(O)2-(C1-Ce)alkyl, (39) -alkylene-N(alkyl)S(O)2-(C1-C6)halogen-alkyl, (40)-alkylene-N(alkyl)S(O)2-R6, (41) -alkylene-N(alkyl)S(O)2-R7, (42) -alkylene-C(O)-NH-(C1-C6)alkyl, (43) -alkylene-C(O)-NHR6, (44) -alkylene-C(O)-NHR7, (45) -alkylene-S(O)2NH-(C1-C6)alkyl, (46) -alkylene-S(O)2NH-R6, (47) -alkylene-S(O)2NH-R7 , (48) -alkylene-C(O)-N((C1-C6)alkyl)2, in which each alkyl group is selected independently, (49) -alkylene-C(O)-N(alkyl)-R6, (50) -alkylene-C(O)-N(alkylene)-R7, (51) -alkylene-S(O)2N((C1-C6)alkyl)2, in which each alkyl group is selected independently, (52) -alkylene-S(O)2N(alkyl)-R6, (53) -alkylene-S(O)2N(alkyl)-R7, (54) -alkylene-OH, (55) -alkylene-OC(O)-NH-alkyl, (56) -alkylene-OC(O)NH-R8, (57) -alkylene-CN, (58) -R8, (59) -alkylene-SH, (60) -alkylene-S(O)2-NH-R8, (61) -alkylene-S(O)2-alkylene-R6, (62) substituted with halogen alkylene, (63) -C(O)OR8, (64) -C(O)O(C1-C6)alkyl, (65) -C(O)R8, (66) -C(O)-alkylene-O-(C1-C6)alkyl, (67) -C(O)NH2, (68) -alkylene-O-(C1-C6)alkyl, (69) -alkylene-R8, (70) -S(O)2-halogen(C1-C6)alkyl, (71) hydroxy-substituted halogen(C1-C6)alkyl, (72) -alkylene-NH2, (73) -alkylene-NH-S(O)2-R8, (74) -alkylene-NH-C(O)-R8, (75) -alkylene-NH-C(O)O-(C1-C6)alkyl, (76) -alkylene-O-C(O)-(C1-C6)alkyl, (77) -alkylene-O-S(O)2-(C1-C6)alkyl, (78) -alkylene-R6 , (79) -alkylene-R7, (80) -alkylene-NH-C(O)NH-(C1-C6)alkyl, (81) -alkylene-N(S(O)2 halogen(C1-C6)alkyl)2, and each -S(O)2 halogen(C1-C6)alkyl fragment is selected independently, (82) -alkylene-N((C1-C6)alkyl)S(O)2-R8 , (83) -alkylene-OC(O)-N(alkyl)2, and each alkyl is selected independently, (84) -alkylene-NH-(C1-C6)alkyl, (85) -C(O)-alkylene-C(O)O-(C1-C6)alkyl, (86) -C(O)-C(O)-O-(C1-C6)alkyl, (87) -C(O)-alkylene-R6, (88) -C(O)-NH-R8, (89) -C(O)-NH-R6, (90) -C(O)-NH-alkylene-R6, (91) -C(O)-alkylene-NH-S(O)2-halogen(C1-C6)alkyl, (92) -C(O)-alkylene-NH-C(O)-O-(C1-C6)alkyl, (93) -C(O)-alkylene-NH2, (94) -C(O)-alkylene-NH-S(O)2-R8, (95) -C(O)-alkylene-NH-S(O)2-(C1-C6)alkyl, (96) -C(O)-alkylene-NH-C(O)-(C1-C6)alkyl, (97) -C(O)-alkylene-N(S(O)2(C1-C6)alkyl)2, and each -S(O)2(C1-C6)alkyl fragment is elected independently, (98) -C(O)-alkylene-NH-C(O)-NH-(C1-C6)alkyl, (99) -alkylene-O-R6, (100) -alkylene-R7, (101) -C(O)OH, (102) -alkylene-N(S(O)2(C1-C6)alkyl)2, (103) -alkylene-C(O)-O-(C1-C6)alkyl, (104) halogenalkyl, (105) halogen, (106) -alkylene-C(O)-NH2, (107) =N-O-(C1-C6)alkyl, (108) =N-O-alkylene-R6, (109) =N-O-alkenyl, (110) -N-O-R6, (111) =N-NH-S(O)2-R6, (112) alkenyl, (113) =R8, (114) -O-C(O)-R9, (115) -O-C(O)-(C1-C6)alkyl, (116)-CN, R6 is selected from group consisting of unsubstituted (C6-C14)aryl, (C6-C14)aryl, substituted with one or several groups L1, unsubstituted (C5-C14)heteroaryl and (C5-C14)heteroaryl, which represents aromatic monocyclic or bicyclic system, which contains in ring from about 5 to about 9 atoms, and one or several atoms in ring system represent atom of element, different from carbon, for instance, nitrogen, oxygen or sulphur, one or in combination, substituted with one or several groups L1; 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Invention also relates to pharmaceutical composition, as well as to application of one or several compounds by one of ii. 1-125.
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Method of producing optically active chromene oxide compound Method of producing optically active chromene oxide compound / 2448112
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The invention relates to compounds of General formula I

including their optical isomers and mixtures of such isomers, where r1denotes hydrogen, C1-C6alkyl, C3-C6cycloalkyl or aryl, optionally substituted by 1-3 halogen atoms, R2and R3each independently of one another denote hydrogen or C1-C6alkyl, R4stands WITH1-C6alkyl or C3-C6quinil, R5, R6, R7and r8each denotes hydrogen and

,

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< / BR>
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FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds, represented by the following formula (I) and their pharmaceutically acceptable salts, where values for groups R1, R4-R6, Ra, m, n, Y, X are determined in the invention formula. Said compounds are used as preparations for enhancing growth of axons and prevention of diseases associated with histone diacetases, in particular tumours or diseases associated with cell proliferation.

EFFECT: compounds in accordance with the claimed invention can be used as anti-cancer, antidiabetic agents and anti-neurodegenerative agents in case of diseases such as Alzheimer's disease, Huntington's disease, spinocerebral ataxia and spinal muscular atrophy in people.

18 cl, 44 dwg, 13 ex

 

The text descriptions are given in facsimile form.

1. Compounds cinnamic acid covered by the General structural formula (I)

where
R1represents hydrogen, C1-4alkyl or C2-6alkenyl,
X represents O or-CH2-,
Y represents O, NH or N-C1-4alkyl,
n represents the integer 0, 1, 2, 3, 4 and 5,
m is an integer 0, 1, 2, 3, 4 and 5,
Rarepresents H or C1-10alkyl which may be substituted by hydroxy, C2-10alkenyl or a heterocycle which may be optionally substituted by at least one1-4the alkyl
R4represents H, C1-4alkyl, C5-6cycloalkyl or 5 - or 6-membered unsaturated carbocycle or a heterocycle which may be substituted with halogen, CF3, CCl3, CBr3, OCF3C1-6the alkyl or or7where R7represents hydrogen or C1-6alkyl,
R5represents H, OH, OK, OLi, NH2C1-4alkyl or 6-membered unsaturated carbocycle or benzyl, where the alkyl, carbocycle optionally substituted NH2and benzyl optionally substituted with halogen, and
R6represents H or, together with R1represents a C2H2and their pharmaceutically acceptable salts,
provided that the excluded compounds cinnamic acid covered by the General structural formula (I), with the following set of substituents:
Y represents O, R5represents H, R1and R6form-C2H2-, X represents O, Rarepresents methyl, R4represents methyl, n and m are 0, Z-isomer,
Y represents O, R5represents H, R1and R6form-C2H2- , X represents O, Rarepresents H, R4represents methyl, n and m are 0, Z-isomer,
Y represents Oh, R5represents H, X represents-CH2-, R4represents methyl, n and m are 0, Rais a 1-isobutylene, R6represents H, R1represents methyl, Z-isomer,
Y represents Oh, R5represents H, X represents-CH2-, R4represents ethyl, n and m are 0, Rais a 1-isobutylene, R6represents H, R1represents methyl, Z-isomer,
Y represents O, R5represents H, X represents O, Rarepresents methyl, R4represents methyl, n and m are 0, R6represents H, R1represents methyl, Z-isomer,
Y represents O, R5represents H, X represents O, Rarepresents methyl, R represents methyl, n and m are 0, R6represents H, R1represents methyl, E-isomer,
Y represents O, R5represents H, X represents O, Ra, R4, R6and R1represent H, Z - and E-isomers,
Y represents O, R5represents methyl, X represents O, n and m are 0, Ra, R4and R1represent methyl, R6represents H, E-isomer,
Y represents O, R5represents methyl, X represents O, n and m are 0, Ra, R4and R1represent methyl, R6represents H, Z - and E-isomers,
Y represents O, R5represents methyl, X represents O, n and m are 0, Rarepresents H, R4and R1represent methyl, R6represents H, Z - and E-isomers,
Y represents O, R5represents methyl, X represents O, n and m are 0, R1and R6represent H, R4represents methyl, R6represents H, Z - and E-isomers,
Y represents O, R5represents H, X represents O, Rarepresents methyl, R4, R6and R1represent H, Z - and E-isomers,
Y represents O, R5represents H, X isone O, n and m are 0, Ra, R4and R1represent n-butyl, R6represents H, E-isomer,
Y represents O, R5represents H, X represents - CH2-, R4represents H, n and m are 0, Rais a 1-isobutylene, R6represents H, R1represents H, E-isomer,
Y represents O, R5represents H, n and m are 0, R4represents H, X represents O, R1and R6form-C2H2-, Rarepresents methyl, Z-isomer,
Y represents O, R5represents methyl, X represents-CH2-, n and m are 0, R6represents H, R4represents methyl, R1represents H, Rarepresents vinyl, E-isomer,
Y represents O, R5represents methyl, X represents-CH2-, n and m are 0, Rarepresents H, R4represents methyl, R1represents H, Rais a 1-isobutylene, E-isomer,
Y represents O, R5represents H, n and m are 0, R4represents H, X represents O, R1and R6form-C2H2-, R6represents methyl, E-isomer,
Y is NH, R5is the th H, n and m are 0, R6represents H, X represents O, R4represents methyl, R1and Rarepresent methyl, E-isomer,
Y is NH, R5represents H, n and m are 0, R6represents H, X represents O, R4represents methyl, R1and Rarepresent methyl, Z - and E-isomers,
Y represents O, R5represents ethyl, n and m are 0, R4represents H, X represents-CH2-, R6represents H, Rarepresents vinyl, R1represents methyl, E-isomer,
Y is NH, R5represents NH2n and m are 0, R1and R6form-C2H2-, R4represents H, Rarepresents methyl, X represents O, Z - and E-isomers,
Y is NH, R5represents H, n, and m is 0, X represents Oh, R4represents methyl, Rarepresents methyl, R1and R6form-C2H2-, Z - and E-isomers,
Y represents O, R5represents ethyl, n and m are 0, R4represents H, X represents-CH2-, R6represents H, R4represents H, Rarepresents vinyl, R1represents METI is, Z - and E-isomers,
Y represents O, R5represents H, n and m are 0, R4represents H, X represents O, R1and R6form-C2H2-, Rarepresents methyl, Z - and E-isomers,
Y represents O, R5represents ethyl, n and m is 0, X represents-CH2-, R1and R6form-C2H2-, Rarepresents H, R4represents methyl, E-isomer,
Y represents O, R5represents H, n and m are 0, R4represents H, X represents Oh, R1and R6form-C2H2-, Rarepresents H, Z - and E-isomers,
Y represents O, R5represents H, n and m are 0, R4represents methyl, R6represents H, X represents O, Rarepresents methyl, R1represents ethyl, Z - and E-isomers,
Y represents O, R5represents H, n and m are 0, R4represents methyl, R6represents H, X represents O, Rarepresents ethyl, R1represents methyl, Z+E isomers,
Y is O, X is O, R5represents ethyl, R1, R4, R6and Rarepresent H, E-isomer,
Y represents O, X depict the defaults a-CH 2-, R1and R4represent methyl, R5and R6represent H, Rais a 1-isobutylene, n and m are 0, E-isomer,
Y represents O, X represents-CH2-, R1, Raand R6represent H, R4represents a 1,3-dichlorophenyl, R5represents ethyl, n is 0, m is 1, E-isomer,
Y represents O, X represents-CH2-, R1and R4represent methyl, R5, R6and Rarepresent H, n and m are 0, E-isomer,
Y represents O, X represents-CH2-, R1, R4and R6represent methyl, Rais a 1-isobutylene, R6represents H, n and m are 0, Z-isomer,
Y represents O, X represents-CH2-, R1represents methyl, R4and R5are ethyl, R6represents H, Rais a 1-isobutylene, n and m are 0, Z-isomer,
Y represents O, X represents-CH2-, R1represents methyl, R4, R5and R6represent H, Rarepresents a 1,2-epoxy-2-methylpropyl, n and m are 0, Z+E isomers,
Y represents O, X represents-CH2-, R1represents methyl, R4, R5, R6R arepresent H, n and m are 0, E-isomer,
Y is O, X is O, R1and R6form-C2H2-, R4and R5represent H, Rarepresents a 3,4-dihydro-5-methyl-2,4-dioxo-1(2H)-pyrimidyl, n is 4, n is 0, E-isomer,
Y is O, X is O, R1and R6form-C2H2-, R4represents H, R5represents ethyl, Rarepresents a 3,4-dihydro-5-methyl-2,4-dioxo-1(2H)-pyrimidyl, n is 4, m is 0, E-isomer,
Y is O, X is O, R4, R5and R6represent methyl, R1and R6form-C2H2-, n and m are 0, E-isomer,
Y is O, X is O, R4, R5and Rarepresent methyl, R1and R6form-C2H2-, n and m are 0, Z-isomer,
Y represents O, R4and R5represent H, R1and R6form-C2H2-, Rarepresents n-butyl, n and m are 0, Z-isomer.

2. Compounds according to claim 1, in which X represents-CH2-.

3. Compounds according to claim 1, in which n and m is 1.

4. Compounds according to claim 1, which is selected from the group including













































.

5. Connection max is th acid, covered by the General structural formula (II)

where R1represents hydrogen, C1-4alkyl or C2-6alkenyl,
X represents-CH2-O,
Y represents O, NH, or N-C1-4alkyl,
n represents the integer 0, 1, 2, 3, 4 and 5,
m is an integer 0, 1, 2, 3, 4 and 5,
R2and R3independently represent a1-6alkyl,
R4represents H, C1-4alkyl, C5-6cycloalkyl or 5 - or 6-membered unsaturated carbocycle or a heterocycle which may be substituted with halogen, CF3, CCl3, CBr3, OCF3C1-6the alkyl, OR7where R7represents hydrogen or C1-6alkyl,
R5represents H, OH, OK, OLi, NH2C1-4alkyl or 6-membered unsaturated carbocycle or benzyl, where the alkyl or carbocycle optionally substituted NH2and benzyl optionally substituted with halogen, and
R6represents H or, together with R1represents a C2H2-,
and their pharmaceutically acceptable salts, provided that the excluded compounds cinnamic acid covered by the General structural formula (I), with the following set of substituents:
Y represents O, X represents-CH2-, R5and R6represent H, R1, R2, R3and 4represent methyl, n and m are 0, Z-isomer,
Y represents O, X represents-CH2-, R6and R6represent H, R1, R2and R3represent methyl, R4represents ethyl, n and m are 0, Z-isomer,
Y represents O, X represents-CH2, R1, R4, R5and R6represent H, R2and R3represent methyl, n and m are 0, E-isomer,
Y represents O, X represents-CH2-, R1and R6represent H, R2, R3, R4and R5represent methyl, n and m are 0, E-isomer,
Y represents O, X represents-CH2-, R1, R2, R3and R4represent methyl, R5and R6represent H, n and m are 0, E-isomer,
Y represents O, X represents-CH2-, R2and R3represent methyl, R1, R4, R6and R6represent H, n and m are 0, Z-isomer,
Y represents O, X represents-CH2-, R1, R2, R3, R4and R5represent methyl, R6represents H, n and m are 0, Z-isomer,
Y represents O, X represents-CH2-, R1, R2and R3represent methyl, R4and R5is own the th ethyl, R6represents H, n and m are 0, Z-isomer.

6. Compounds according to claim 5, in which R1, R2and R3independently represents a C1-4alkyl, R4represents phenyl or phenyl substituted with halogen, CF3, CCL3, CBr3OS1-4the alkyl, R5represents phenyl or phenyl substituted NH2and R6represents hydrogen.

7. Compounds according to claim 5, in which R1, R2and R3independently represent methyl, R4represents phenyl or phenyl, substituted by F, Cl, Br, CF3, CCl3, CBF3, OCH3, R5represents OH or phenyl, substituted NH2and R6represents hydrogen.

8. Compounds according to claim 5, in which X represents-CH2-.

9. Compounds according to claim 5, in which n and m is 1.

10. Compounds according to claim 5, which is selected from the group including













































11. Pharmaceutical composition for inhibiting ristanovi deacetylase, comprising a therapeutically effective amount of a compound according to claim 1 or its pharmaceutically acceptable salt as an active substance and a pharmaceutically acceptable carrier.

12. A method of inhibiting ristanovi deacetylase, comprising introducing a therapeutically effectiveagainst compounds according to claim 1 or their pharmaceutically acceptable salts.

13. A method of treating diabetes, comprising introducing a therapeutically effective amount of the compounds according to claim 1 or their pharmaceutically acceptable salts.

14. A method of treating tumors or diseases associated with cell proliferation, including the introduction of therapeutically effective amounts of compounds according to claim 1 or their pharmaceutically acceptable salts.

15. A way to enhance axon growth, including the introduction of therapeutically effective amounts of compounds according to claim 1 or their pharmaceutically acceptable salts.

16. A method of treating neurodegenerative diseases and spinal muscular atrophy person, including the introduction of therapeutically effective amounts of compounds according to claim 1 or their pharmaceutically acceptable salts.

17. The method according to clause 16, in which the neurodegenerative disease is selected from the group including Huntington's disease and polyglutamine disease.

18. Intermediate compounds, which were used to obtain the compounds or pharmaceutically acceptable salts according to claim 1 or 5, selected from the group including



in which R is a p-H, p-Cl, p-Br or OCF3.

 
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