FIELD: chemistry.
SUBSTANCE: invention relates to the new derivatives of imide indolylmaleic acid with the formula I 
, where Ra denotes H; C1-4alkyl or C1-4alkyl, with substituted OH, NH2, NH(C1-4 alkyl) or H(C1-4alkyl)2; Rb denotes H or C1-4alkyl; R denotes a radical of the formula (d) 
or (e) 
, where each one from R8 and R11 independently denotes OH; heterocyclic residue; NR16R17, where each from R16 and R17 independently denotes H or C1-4alkyl, or R16 and R17 together with a nitrogen atom; to which they are joined, form a heterocyclic residue; or a radical of the formula 
-X-RC-Y (α) where X denotes a covalent bond, O, S or NR18, where R18 denotes H or C1-4alkyl; Rc denotes C1-4alkylen or C1-4alkylen, in which one CH2 has been changed with the group CRxRy, whereby one of Rx and Ry denotes H, and the other denotes CH3, each of the Rx and Ry denote CH3 or Rx and Ry together form the group -CH2-CH2-, and Y is joined with the terminal carbon atom and is selected from OH, -NR19R20, where each one of R19 and R20 independently denotes C1-4alkyl; each one of R9, R10, R12, R13 independently denotes H, halogen, C1-4alkyl, OH, NH2, C1-4alkoxy, NH(C1-4alkyl) or N(C1-4alkyl)2 or each E denotes -N= and G denotes -CH= or E denotes -CH= and G denotes -N=, and cycle A is unsubstituted, monosubstituted, where the substitute is selected from a group containing halogen, OH, C1-4alkoxy, C1-4alkyl, NO2, NH2, NH(C1-4alkyl) or N(C1-4alkyl)2 or CN; where the heterocyclic residue is 3-8 member saturated, heterocyclic rings, containing 1-2-heteroatoms, of which one is N, and the other N or O, possibly substituted with one or more carbon atoms in the cycle and/or with a nitrogen atom in the cycle, if it is in the ring; where the substitutes of the carbon atom ring, if they exist, are selected from the group which contains C1-4alkyl, C3-C6cycloalkyl, it is optional to further substitute C1-4alkyl; 
, where p denotes 1, 2 or 3; and where the substitutes on the nitrogen atom ring if they exist, are selected from a group which contains C1-4alkyl, C3-C6cycloalkyl, C3-C6cycloalkyl C1-4alkyl, phenyl, phenylC1-4alkyl, heterocyclic residue and the residue from the formula β: -R21-Y' (β) R21 - denotes C1-C4alkylen, a Y' denotes OH, NH2, NH(C1-4alkyl) or N(C1-4alkyl)2, where the heterocyclic residue is of importance, as stated above, or its pharmaceutically acceptable salts.
EFFECT: bonds possess an action, which has an inhibitory activity on proteinkinase C and can be used in a pharmaceutical composition for treatment or prophylaxis of acute or chronic rejection of allo or xenotransilants of organs or tissues.
10 cl, 7 tbl, 182 ex
| Title | Year | Author | Number |
|---|---|---|---|
| USING PKC INHIBITORS IN TRANSPLANTATION | 2007 |
|
RU2494738C2 |
| INDOLYLMALEIMIDE DERIVATIVES | 2005 |
|
RU2373201C2 |
| PIPERIDINE DERIVATIVES AS MODULATORS OF ACTIVITY OF CCR5 RECEPTOR, METHOD AND INTERMEDIATE COMPOUNDS FOR OBTAINING THEM, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM | 2002 |
|
RU2345990C2 |
| 3,7-DIAZABICYCLO[3.3.0]OCTANES AND THEIR USING IN TREATMENT OF CARDIAC ARRHYTHMIA | 2002 |
|
RU2293085C2 |
| PIPERIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR CCR5 | 2005 |
|
RU2368608C2 |
| PHARMACEUTICAL COMPOUNDS | 2019 |
|
RU2821941C2 |
| OPTIONALLY CONDENSED HETEROCYCLYL-SUBSTITUTED PYRIMIDINE DERIVATIVES SUITABLE FOR TREATING INFLAMMATORY, METABOLIC, ONCOLOGICAL AND AUTOIMMUNE DISEASES | 2015 |
|
RU2719422C2 |
| 6,7,8,9-SUBSTITUTED 1-PHENYL-1,5-DIHYDROPYRIDO (3,2-b) INDOLE-2-ONES EFFECTIVE AS ANTIINFECTIOUS PHARMACEUTICAL AGENTS | 2005 |
|
RU2377243C2 |
| PHENYLAMINOPYRIMIDINE COMPOUNDS AND USES THEREOF | 2008 |
|
RU2498983C2 |
| ISOINDOLINONE INHIBITORS OF MDM2-P53 INTERACTION WITH ANTI-CANCER ACTIVITY | 2016 |
|
RU2794333C1 |
