| 摘要 |
Compounds of formula (I):;
wherein Ra, Rb, Rc, Rd, R1, R2, R3, R4, R5, X, Y and Het are as defined in the description.
;Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system. |
| 主权项 |
1. A compound of formula (I):wherein:
X and Y represent a carbon atom or a nitrogen atom, wherein X and Y may not simultaneously represent two carbon atoms or two nitrogen atoms; the Het moiety of the group represents an optionally substituted, aromatic or non-aromnatic ring composed of 5, 6 or 7 ring members, which ring may have, in addition to the nitrogen represented by X or by Y, from one to 3 heteroatoms selected independently from oxygen, sulphur and nitrogen, wherein the nitrogen atom may be substituted by a hydrogen atom, a linear or branched (C1-C6)alkyl group or a —C(O)—O-Alk group wherein Alk is a linear or branched (C1-C6)alkyl group; R1 and R2 independently of one another represent a hydrogen atom or a linear or branched (C1-C6)alkyl group, or R1 and R2 together with the nitrogen atom carrying them form a heterocycloalkyl composed of from 4 to 7 ring members, which ring may have, in addition to the nitrogen atom, another heteroatom selected from oxygen, sulphur, SO2 and NR wherein R represents a hydrogen atom, a linear or branched (C1-C6)alkyl group, a (C1-C6)alkylsulphonyl group, a linear or branched (C1-C6)polyhaloalkyl group or a —C(O)—O-Alk group wherein Alk is a linear or branched (C1-C6)alkyl group; R3 represents a linear or branched (C1-C6)alkyl group, a (C2-C6)alkenyl group, a (C2-C6)alkynyl group, a cycloalkyl group, a (C4-C10)cycloalkyl-(C1-C6)alkyl group wherein the alkyl group may be linear or branched, an aryl group or a heteroaryl group; R4 represents an aryl, heteroaryl, cycloalkyl or linear or branched (C1-C6)alkyl, group; R5 represents a hydrogen atom or a halogen atom; Ra, Rb, Rc, and Rd independently of one another represent a hydrogen atom, a halogen atom, a linear or branched (C1-C6)alkyl group, a linear or branched (C1-C6)alkoxy group, a hydroxy group, a linear or branched (C1-C6)polyhaloalkyl group, or a trifluoromethoxy group, or the substituents of one of the pairs (Ra,Rb), (Rb,Rc) or (Rc,Rd) together with the carbon atoms carrying them form a ring composed of from 5 to 7 ring members, which ring may have from one to 3 heteroatoms selected from oxygen, sulphur and nitrogen, wherein the nitrogen atom may be substituted by a hydrogen atom, a linear or branched (C1-C6)alkyl group or a —C(O)—O-Alk group wherein Alk is a linear or branched (C1-C6)alkyl group, wherein one or more carbon atoms of the ring defined hereinbefore may be deuterated,it being understood that:
“aryl” means a phenyl, naphthyl, biphenyl or indenyl group, “heteroaryl” means any mono- or bi-cyclic group composed of from 5 to 10 ring members, having at least one aromatic moiety and containing from 1 to 3 hetero atoms selected from oxygen, sulphur and nitrogen, “cycloalkyl” means any mono- or bi-cyclic non-aromatic carbocyclic group containing from 4 to 10 ring members,wherein the alkyl, aryl, heteroaryl, cycloalkyl and heterocycloalkyl groups so defined may be optionally substituted by from 1 to 3 groups selected from optionally substituted linear or branched (C1-C6)alkyl, (C3-C6)spiro, linear or branched (C1-C6)alkoxy, (C1-C6)alkyl-S—, hydroxy, oxo (or N-oxide where appropriate), nitro, cyano, —COOR′, NR′R″, linear or branched (C1-C6)polyhaloalkyl, trifluoromethoxy, (C1-C6)alkylsulphonyl or halogen, wherein R′ and R″ independently of one another represent a hydrogen atom or a linear or branched (C1-C6)alkyl group,and wherein the Het moiety of the groupdefined hereinbefore may be optionally substituted by a group selected from linear or branched (C1-C6)alkyl, hydroxy, NR1′R1″ and halogen, wherein R1′ and R1″ independently of one another represent a hydrogen atom or a linear or branched (C1-C6)alkyl group,or an enantiomer, a diastereoisomer, or an addition salt thereof with a pharmaceutically acceptable acid or base. |
