Phosphorus derivatives as SOS1 inhibitors

A compound of formula (I)

• in which
• X1 represents CH or N;
• X2 represents CRa or N
• X3 represents CRa or N
• X4 represents CH or N
• Y represents O or S;
• R1, R2 is independently of each other selected from C1-4 alkyl, ORb or NRcRd, or
• R1, R2 together with the phosphorus atom they are attached to form a 4-7 membered heterocycloalkyl in which one or more carbon atom can be replaced by —O—, —NRc—, —S—, —S(O)—, S(O)2— or —S(O)NRf—;
• and in which each remaining carbon atom can optionally be substituted by one or two —CH3 or by one —CH2—CH3,
• R3 is selected from —H, —OH, —CH3, —CN, —NRpRq, or C1-2-alkyl optionally substituted with —OH, —CH3, —CN or halogen
• R4 is selected from —H, —F, —Cl, —Br, —OH, —NH2, —N(CH3)H, —CH3 or —CF2H;
• R5 represents -A-B-E in which
• A represents —CRjRk— or is absent, and
• B represents —CRlRm— or is absent, and
• E represents —H, —F, —OH, —OCH3, —NH2, —NH—CH3, —N(CH3)2, —N(CH3)—OCH3, —CN, —SO2—CH3, —NH—SO2—CH3, —N(CH3)—SO2—CH3, —NH—C(O)—CH3, —N(CH3)—C(O)—CH3, —S(═NH)(═O)—CH3, —S(═N—CH3)(═O)—CH3, —C(O)—NH2, —C(O)—NH(CH3), —C(O)—N(CH3)2, or
• R5 represents —SO2—NRnRo,
• R6 is selected from —H, halogen or —CH3;
• Ra is selected from —H, halogen, —OH, —OCH3, —CN, cyclopropyl, —NH2, —NH(CH3), —N(CH3)2, or C1-2 alkyl optionally substituted one or more times by halogen, —OH or —OCH3, —CH3, —CF3, —NH2, —NH(CH3), —N(CH3)2, or —CN
• Rb is selected from —H (under the condition, that if R1 and R2 are both ORb only one Rb can be —H), —CH3, —CH2—CH3, —CH(CH3)2 or cyclopropyl,
• Rc is selected from —CH3, —CH2—CH3, —CH(CH3)2 or cyclopropyl,
• Rd is selected from —H, —CH3, —CH2—CH3, —CH(CH3)2 or cyclopropyl,
• Re is selected from —H, C1-3-alkyl optionally substituted by one or more —F, cyclopropyl, —C(O)—Rg, —SO2—CH3 or 5 membered heteroaryl optionally substituted by —CH3, halogen, —CF3 or —CF2H
• Rf is selected from —H, —CH3, or —CH2—CH3,
• Rg is selected from C1-4 alkyl optionally substituted by —OH, —OCH3, —CH3, halogen;
• or
• is selected from 5-membered heteroaryl optionally substituted by —CH3, —CH2CH3, CF2H, CF3 or halogen;
• or
• is selected from NRhRi,
• Rh is selected from —H or —CH3, and
• Ri is selected from C1-3 alkyl optionally substituted by halogen or from cyclopropyl,
• Rj and Rk are independently of each other selected from —H, —F or —CH3, or form together with the carbon atom they are attached to cyclopropyl;
• Rl and Rm are independently of each other selected from —H, Deuterium, or —CH3, —CH2—CH3, cyclopropyl;
• or form together with the carbon atom they are attached to cyclopropyl;
• or
• Rn and Ro are independently selected from —H or C1-4 alkyl optionally substituted by —OH, —OCH3, or
• Rn and Ro form together with the nitrogen atom they are attached to a 4 to 7 membered heterocycloalkyl optionally containing further heteroatoms selected from N or O, in which carbon atoms of this heterocycloalkyl can be optionally substituted by H or C1-4 alkyl and where this C1-4 alkyl can again be substituted by halogen, ═O, —OH, —OCH3, —NH2, —NH—CH3 or —N(CH3)2, and in which nitrogen atoms of this heterocycloalkyl can be optionally substituted by —C(O)-cyclopropyl or —C(O)—C1-4-alkyl, both optionally substituted one or more times with —F;
• Rp and Rq are independently selected from —H, —CH3 or —CH2—CH3;
• or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof.