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
| Title | Year | Author | Number |
|---|---|---|---|
| MELANOCORTIN-4 RECEPTOR AGONISTS | 2020 |
|
RU2786864C1 |
| DERIVATIVES OF BENZOPYRANE SUBSTITUTED WITH SECONDARY AMINES COMPRISING TETRAZOLE, METHOD FOR THEIR PREPARING AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEREOF | 2003 |
|
RU2283312C2 |
| AMIDE DERIVATIVES AS GRP119 AGONISTS | 2014 |
|
RU2642429C2 |
| COMPOUNDS WHICH ARE ANTAGONISTS OF THE A3-ADENOSINE RECEPTOR, A METHOD FOR PREPARING THEM AND MEDICAL USE THEREOF | 2017 |
|
RU2737157C2 |
| SUBSTITUTED CHROMANS | 2015 |
|
RU2718060C2 |
| PURINE INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA | 2013 |
|
RU2661896C2 |
| CYCLOALKENYLARYLIC DERIVATIVES FOR INHIBITING TRANSPORT PROTEIN CHOLESTERIN ESTERS | 2012 |
|
RU2597266C2 |
| PYRAZOLOPYRIMIDINE DERIVATIVES AS A KINASE INHIBITOR | 2017 |
|
RU2714206C1 |
| NOVEL AMIDE DERIVATIVE FOR INHIBITING GROWTH OF CANCER CELLS | 2008 |
|
RU2434010C2 |
| NOVEL COMPOUNDS, ISOMERS THEREOF OR PHARMACUTICALLY ACCEPTABLE SALTS THEREOF AS VANILLOID RECEPTOR ANTAGONISTS AND PHARMACEUTICAL COMPOSITION CONTAINING SAID COMPOUNDS | 2007 |
|
RU2448108C2 |
