Publication number: 20200115390
Abstract: A compound of formula I and salts and solvates thereof, wherein: R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo; where R and R? are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo; R? is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms, e.g. O, S, NRN2 (where RN2 is H or C1-4 alkyl), and/or aromatic rings, e.g. benzene or pyridine; Y and Y? are selected from O, S, or NH; R6, R7, R9 are selected from the same groups as R6, R7 and R9 respectively; R11b is selected from OH, ORA, where RA is C1-4 alkyl; and RL is a linker for connection to a cell binding agent.
Type:
Application
Filed:
April 18, 2018
Publication date:
April 16, 2020
Inventors:
Philip Wilson Howard, Stephen John Gregson
Publication number: 20200115402
Abstract: The present invention refers to a process for the preparation of a mono(acyl)phosphine of the general formula (I) and/or a bis(acyl)phosphine of the general formula (II), wherein R1, R2, R3, R4 and R5 are the same or different and are independently selected from H, halogen, linear or branched C1-C20-alkyl, linear or branched C2-C8-alkenyl, C1-C8-alkoxy, C2-C8-alkenyloxy, C3-C8-cycloalkyl, C6-C12-aryl, C3-C8-cycloalkoxy, C7-C12-arylalkoxy, C9-C15-alkenylarylalkoxy, nitro-, C6-C12-arylsulfonyl, 4-alkylaryl-sulfonyl, C1-C20-alkylcarboxy, C1-C8-alkoxycarbonyl, SR14, NIIR14 or NR14R15 with R14 and R15 being independently selected from H, linear or branched C1-C20-alkyl, linear or branched C2-C8-alkenyl and C3-C8-cycloalkyl, and an O-, S- or N-containing 5-or 6-membered heterocyclic ring; R6 is H or R6 is replaced by an alkaline earth metal cation or a mixed alkali metal/alkaline earth metal cation; Formula (II) wherein R1, R2, R3, R4, R5, R7, R8, R9, R10 and R11 are the same or different and are independently sele
Type:
Application
Filed:
May 30, 2018
Publication date:
April 16, 2020
Inventors:
Reinhard H. Sommerlade, Souad Boulmaaz
Publication number: 20200115403
Abstract: The present invention refers to a process for the preparation of a bis(acyl)phosphinic acid silyl ester of the general formula (I), wherein R1, R2, R3, R4, R5, R7, R8, R9, R10 and R11 are the same or different and are independently selected from H, halogen, linear or branched C1-C20-alkyl, linear or branched C2-C8-alkenyl, C1-C8-alkoxy, C2-C8-alkenyloxy, C3-C8-cycloalkyl, C6-C12-aryl, C3-C8-cycloalkoxy, C7-C12-arylalkoxy, C9-C15-alkenylarylalkoxy, nitro-, C6-C12-arylsulfonyl, 4-alkylarylsulfonyl, C1-C20-alkylcarboxy, C1-C8-alkoxycarbonyl, SR12, NHR12 or NR12R13 with R12 and R13 being independently selected from H, linear or branched C1-C20-alkyl, linear or branched C2-C8-alkenyl and C3-C8-cycloalkyl, and an O-, S- or N-containing 5- or 6-membered heterocyclic ring; R6 is OSiR14R15R16 with R14, R15 and R16 being independently selected from linear or branched C1-C20-alkyl or C6-C12-aryl; as well as the bis(acyl)phosphinic acid silyl ester and the bis(acyl)phosphinic acid obtained by the process.
Type:
Application
Filed:
June 27, 2018
Publication date:
April 16, 2020
Inventors:
Reinhard H. Sommerlade, Kai Uwe Luckner