Derivative of 2 - (phenyl) - 2H - pyrazole carboxylic acid - 3 - 4 - N - (tioxo - heterociclil) phenyl imino Amide - and heterociclil derivatives and related compounds, procedures, Medications, Kit

摘要

These compounds are inhibitors of XA coagulation factor and can be used in the prevention and / or treatment of thrombotic diseases and the treatment of tumors. Claim 1: compound of formula (1): D does not exist, or a saturated tar chain composed of 3 to 4 members, all or part of which is unsaturated, wherein 1 to 3 C atoms can be replaced by N and / or 1 to 2 C atoms, 1 to 2 O and / or 1 to 2 S atoms, But you can replace up to three C atoms and a monkey theredi or trisubstitution of the alkylene chain and / or of a nitrogen found there by Hal, A, - [C (R3) 2] n-Ar, - [C (R3) 2] n-Het, - [C (R3) 2] n-cycloalkyl, OR2, N (R2) 2, NO2, CN, COOR2, CON (R2) 2, NR2COA, NR2SO2A, COR2, SO2NR2, and / or S (O) mA, and where also a CH2 group of the alkylene chain may be replaced by a group C = O; M is a phenyl ring or an aromatic heterocycle that may contain 1-2 atoms of N, O and / or S; R1, R1 'are in each case, independently of each other,H. One or one or one or one or one or one or one or one or one or one or one or one or one or one or more are replaced by a conventional and formulaic amino protection group (2);R2 is H, A, - [C (R3) 2] n-Ar, - [C (R3) 2] n-Het, - [C (R3) 2] n-cycloalkyl, - [C (R3) 2] nN (R3) 2 or - [C (R3) 2] n-OR3; R2 'is H, A, - [C (R3) 2] n-Ar',- C (R3) 2 n-Het- [C (R3) 2] n-cycloalkyl, - [C (R3) 2] n-N (R3) 2 or - [C (R3) 2] n-OR3; R2 '' is H, A, - [C (R3) 2] n-Ar 'or - [C (R3) 2] n-cycloalkyl, - [C (R3) 2] nN (R3) 2 or - [C (R3) 2] n-OR3; R3 is H or A; W is a saturated, unsaturated or aromatic mono or bicyclic carbocycle or heterocycle with 1 to 4 atoms of N, O and / or S, which may be mono or disubstituted by R2; X is CONR2, CONR2C (R3) 2, -C (R3) 2NR2 or -C (R3) 2NR2C (R3) 2, -C (R3) 2O-,-C (R3) 2OC (R3) 2- or NR2CO; Y is alkylene, cycloalkylene, Het-diyl or Ar-diyl; T is a saturated, unsaturated or aromatic mono or bicyclic carbocycle or heterocycle with 1 to 4 atoms of N, O and / or S, which is mono or disubstituted by = S, = NR2, = N-CN, = N-NO2 , = NOR2, = NCOR2, = NCOOR2, = NOCOR2 and which may also be mono, disubstituted or trisubstituted by Hal, A, - [C (R3) 2] n-Ar, - [C (R3) 2] n-Het - [C (R3) 2] n-cycloalkyl, -OR3, N (R3) 2, NO2, CN, COOR2, CON (R2) 2, NR2COA, NR2CON (R2) 2, NR2SO2A, COR2, SO2NR2 and / or S (O) mA; A is C1-10 unbranched or branched alkyl,donde uno o dos grupos CH2 pueden estar reemplazados por tomos de O o S y 2Fo por grupos -CH 3DCH y 2Fo tambi n 1-7 tomos de H pueden estar reemplazados por F Ar es fenilo naftilo o bifenilo insustituido o mono di o trisustituido por u -O- C (R3) 2 o-COOR2Ar es fenilo o bencilo insustituido o mono o disustituido por Hal Het es un heterociclo mono o bic clico saturado no saturado o arom tico con 1 a 4 tomos de NO y 2Fo S que puede estar insustituido o mono di o trisustituido por el ox geno del - C (R3) 2 n-N (R2) 2 NO2 CN - C (R3) 2 n-COOR2- [C (R3) 2] n-CON (R2 ') 2, - [C (R3) 2] n-NR2'COA, NR2'CON (R2') 2, - [C (R3) 2] n- NR2'SO2A, COR2 ',So2nr2'y / O S (o) MA; hett1 is a single or double cycle heterocycle with one or two N, Y / or S atoms, which can be replaced, unsaturated, unsaturated or modified by carbide oxygen, = s (R3), 2, Hal, a, or2 ',N (R2) 2 NO2 CN COOR2CON (R2) 2 NR2 COA NR2 CON (R2) 2 NR2 SO2A COR2So2nr2 '' and / or s (o) MA; Hal is f, Cl, Br or I; n is 0, 1 or 2; m is 0, 1 or 2; or 1, 2 or 3; and stereoisomeric derivatives with the same drug use, including mixtures in various proportions.