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    • 1. 发明专利
      NZ751432A Pyrrolobenzodiazepines and conjugates thereof 未知
    • Pyrrolobenzodiazepines and conjugates thereof
    • NZ751432A
    • 2021-01-29
    • NZ75143214
    • 2014-03-13
    • GENENTECH INC , MEDIMMUNE LTD
    • FLYGARE JOHN , PILLOW THOMAS , HOWARD PHILIP , WEI BINQING
    • A61K31/5517 , A61K47/68 , C07D487/04
    • The present invention relates to pyrrolobenzodiazepines (PBDs), in particular pyrrolobenzodiazepines having a linker group connected to a cell binding agent. In one aspect, the present invention provides a conjugate comprising a PBD dimer connected through the dimer bridging portion via a specified linker to a cell binding agent. The present invention is suitable for use in providing a PBD conjugate to a preferred site in a subject. In particular, the present invention provides a conjugate of formula (A), use of a conjugate of formula (A) the manufacture of a medicament, a pharmaceutical composition comprising a conjugate of formula (A), a compound of formula (B), a compound of formula (C), a compound of formula (D), a compound of formula (E) and/or a method of synthesis of a compound. In preferred embodiments, use of a conjugate of formula (A) the manufacture of a medicament for treating cancer and/or a proliferative disease. Conjugate compounds of formula (A): wherein: R2 is, where R36a and R36b are independently selected from H, F, C1-4 saturated alkyl, C2-3 alkenyl, which alkyl and alkenyl groups are optionally substituted by a group selected from C1-4 alkyl amido and C1-4 alkyl ester; or, when one of R36a and R36b is H, the other is selected from nitrile and a C1-4 alkyl ester; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR’, NO2, Me3Sn and halo; R7 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR’, NO2, Me3Sn and halo; Y is selected from formulae A1, A2, A3, A4, A5 and A6: L is a linker connected to a cell binding agent; CBA is the cell binding agent; n is an integer selected in the range of 0 to 48; RA4 is a C1-6 alkylene group; either (a) R10 is H, and R11 is OH, ORA, where RA is C1-4 alkyl; or (b) R10 and R11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (c) R10 is H and R11 is OSOzM, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; R and R’ are each independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups, and optionally in relation to the group NRR’, R and R’ together with the nitrogen atom to which they are attached form an optionally substituted 4-, 5-, 6- or 7-membered heterocyclic ring; wherein R16, R17, R19, R20, R21 and R22 are as defined for R6, R7, R9, R10, R11 and R2 respectively; wherein Z is CH or N; wherein T and T’ are independently selected from a single bond or a C1-9 alkylene, which chain may be interrupted by one or more heteroatoms e.g. O, S, N(H), NMe, provided that the number of atoms in the shortest chain of atoms between X and X’ is 3 to 12 atoms; and X and X’ are independently selected from O, S and N(H).
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 2. 发明专利
      NZ710745A Pyrrolobenzodiazepines and conjugates thereof 未知
    • Pyrrolobenzodiazepines and conjugates thereof
    • NZ710745A
    • 2019-03-29
    • NZ71074514
    • 2014-03-13
    • GENENTECH INC , MEDIMMUNE LTD
    • FLYGARE JOHN , PILLOW THOMAS , HOWARD PHILIP , WEI BINQING
    • A61K31/5517 , A61K47/68 , C07D487/04
    • The present invention relates to pyrrolobenzodiazepines (PBDs), in particular pyrrolobenzodiazepines having a linker group connected to a cell binding agent. In one aspect, the present invention provides a conjugate comprising a PBD dimer connected through the dimer bridging portion via a specified linker to a cell binding agent. The present invention is suitable for use in providing a PBD conjugate to a preferred site in a subject. In particular, the present invention provides a conjugate of formula (A), use of a conjugate of formula (A) the manufacture of a medicament, a pharmaceutical composition comprising a conjugate of formula (A), a compound of formula (B), a compound of formula (C), a compound of formula (D), a compound of formula (E) and/or a method of synthesis of a compound. In preferred embodiments, use of a conjugate of formula (A) the manufacture of a medicament for treating cancer and/or a proliferative disease. Conjugate compounds of formula (A): wherein: R2 is, where R36a and R36b are independently selected from H, F, C1-4 saturated alkyl, C2-3 alkenyl, which alkyl and alkenyl groups are optionally substituted by a group selected from C1-4 alkyl amido and C1-4 alkyl ester; or, when one of R36a and R36b is H, the other is selected from nitrile and a C1-4 alkyl ester; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR’, NO2, Me3Sn and halo; R7 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR’, NO2, Me3Sn and halo; Y is selected from formulae A1, A2, A3, A4, A5 and A6: L is a linker connected to a cell binding agent; CBA is the cell binding agent; n is an integer selected in the range of 0 to 48; RA4 is a C1-6 alkylene group; either (a) R10 is H, and R11 is OH, ORA, where RA is C1-4 alkyl; or (b) R10 and R11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (c) R10 is H and R11 is OSOzM, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; R and R’ are each independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups, and optionally in relation to the group NRR’, R and R’ together with the nitrogen atom to which they are attached form an optionally substituted 4-, 5-, 6- or 7-membered heterocyclic ring; wherein R16, R17, R19, R20, R21 and R22 are as defined for R6, R7, R9, R10, R11 and R2 respectively; wherein Z is CH or N; wherein T and T’ are independently selected from a single bond or a C1-9 alkylene, which chain may be interrupted by one or more heteroatoms e.g. O, S, N(H), NMe, provided that the number of atoms in the shortest chain of atoms between X and X’ is 3 to 12 atoms; and X and X’ are independently selected from O, S and N(H).
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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