FIELD: chemistry; pharmacology.
SUBSTANCE: present invention relates to new condensed dicyclic nitrogen-containing heterocycles with the general formula (I), their pharmaceutically accepted salts and stereoisomers, possessing DGAT inhibiting action. In the compound of formula (I): , X is selected from a group, which consists of C(R1) and N; Y is selected from a group, which consists of C(R1), C(R2)(R2), N and N(R2); Z is selected from a group, which consists of O; W1 is selected from cyclo(C3-C6)alkyl, aryl and 5- or 6-member heteroaryl, containing 1-2 heteroatoms, selected from a group, which comprises of nitrogen and sulphur, W2 selected from cyclo(C3-C8)alkyl, (C5-C6)heterocycloalkyl, containing 1 or 2 heteroatoms, selected from groups, consisting of nitrogen or oxygen, benzol and 5-or 6-member heteroaryl, containing 1-2 nitrogen atoms as heteroatoms, L1 is the link; L2 is selected from a group consisting of links, 0, (C1-C4)alkylene and (C1-C4)oxyalkylene; m denotes 0 or 1; its not a must that when m denotes 1 and L2 denotes a link, the substitute for W2 can be integrated with the substitute for W1 forming a 5-or 6-member ring, condensed with c W1 forming a spiro-system or condensed with W2, where specified ring could be saturated or unsaturated and has 0 or 1 atom O, as a member of the ring R1 is H; R2 is H; R3 and R4 are independently selected from groups consisting of H and (C1-C8) alkyl; optionally, R3 and R4 can together form 3-, 4-, 5- or 6-member spirorings, R5 and R6 are independently H; optionally, when Y includes the group R1 or R2, R5 or R6 can be joined with R1 and R2 forming a 5- or 6-member condensate ring, containing a nitrogen atom, to which R5 or R6 are joined, and optionally containing an oxo-group; R7 is selected from a group, composed of H, (C1-C8) alkyl, halogen(C1-C4)alkyl, 0Ra and NRaRb ; Ra selected from groups composed of H and (C1-C8)alkyl; and Rb selected from groups consisting of H and (C1-C8)alkyl; a dotted line indicates a possible bond. The invention also relates to pharmaceutical compositions and applications of the compounds.
EFFECT: obtaining compounds which can be used for getting medicinal agents to treat or prevent diseases or a mediated action state of DGAT, such as obesity, diabetes, syndrome X, resistance of insulin, hyperglycemia, hyperinsulinemia, hypercholesterolemia, hyperlipidemia, hypertriglyceridemia, disease of non-alcoholic fatty infiltration of the liver, atherosclerosis, arteriosclerosis, coronary artery disease and myocardial infarction.
33 cl, 17 dwg, 11 tbl, 391 ex
Title | Year | Author | Number |
---|---|---|---|
INDOLE DERIVATIVE AND ITS USE IN THERAPEUTIC PURPOSES | 2008 |
|
RU2477274C2 |
CONDENSED HETEROCYCLIC DERIVATIVE, THERAPEUTIC COMPOSITION WHICH CONTAINS IT AND ITS APPLICATION IN MEDICINE | 2006 |
|
RU2418803C2 |
AZAINDOLES USEFUL AS JANUS KINASE INHIBITORS | 2007 |
|
RU2453548C2 |
5-MEMBERED HETEROCYCLIC COMPOUND AND ITS APPLICATION FOR MEDICINAL PURPOSES | 2008 |
|
RU2515968C2 |
AMINE DERIVATIVE POSSESSING NPY-Y5 RECEPTOR ANTAGONIST ACTIVITY, AND APPLICATION THEREOF | 2008 |
|
RU2460523C2 |
PYRROLOPYRIDINES EFFECTIVE AS PROTEINKINASE INHIBITORS | 2006 |
|
RU2435769C2 |
N,N-SUBSTITUTED 3-AMINOPYRROLIDINE COMPOUNDS EFFECTIVE AS MONOAMINE REUPTAKE INHIBITORS | 2006 |
|
RU2574406C2 |
NOVEL TRICYCLIC DERIVATIVE AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, METHOD FOR PRODUCTION THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING SAID DERIVATIVE | 2009 |
|
RU2470934C1 |
NOVEL COUMARIN DERIVATIVES WITH ANTI-TUMOUR ACTIVITY | 2007 |
|
RU2428420C2 |
COMPOSITIONS FOR ACTIVATION OF LIPOPROTEIN LIPASE CONTAINING BENZENE DERIVATIVES | 2008 |
|
RU2466725C2 |
Authors
Dates
2008-12-27—Published
2003-11-21—Filed