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    • 7. 发明授权
    • Unsymmetrical pyrrolobenzodiazepine-dimers for treatment of proliferative diseases
    • 用于治疗增殖性疾病的不对称吡咯并苯并二氮杂二聚体
    • US08592576B2
    • 2013-11-26
    • US13123327
    • 2009-10-16
    • Philip Wilson HowardStephen John GregsonLuke Masterson
    • Philip Wilson HowardStephen John GregsonLuke Masterson
    • C07D487/04
    • C07D487/04
    • Claimed are unsymmetrical Pyrrolobenzodiazepine-dimers (PBD-dimers) of formula (I), that are unsymmetrical due at least to the values that the variables R12 and R2 represent. Formula (I), wherein: R2 is of formula (II), where A is a C5-7 aryl group, X is selected from the group comprising: OH, SH, CO2H, COH, N═C═O, NHRN, wherein RN is selected from the group comprising H and C1-4 alkyl, and (OC2H4)mOCH3, where m is 1 to 3, and either: (i) Q1 is a single bond, and Q2 is selected from a single bond and —Z—(CH2)n—, where Z is selected from a single bond, O, S and NH and n is from 1 to 3; or (ii) Q1 is —CH═CH—, and Q2 is a single bond; R12 is a C5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, C1-7 alkyl, C3-7 heterocyclyl and bis-oxy-C1-3 alkylene. The other variables are as defined in the claims. The compounds are useful for the treatment of proliferative diseases.
    • 声称是式(I)的不对称吡咯并苯并二氮杂二聚体(PBD-二聚体),其至少与变量R12和R2表示的值不对称。 式(I)其中:R2为式(Ⅱ),其中A为C5-7芳基,X选自OH,SH,CO2H,COH,N = C = O,NHRN,其中 RN选自H和C 1-4烷基,和(OC 2 H 4)m OCH 3,其中m为1至3,以及:(i)Q1为单键,Q2选自单键和-Z - (CH 2)n - ,其中Z选自单键,O,S和NH,n为1至3; 或(ii)Q1为-CH = CH-,Q2为单键; R 12是任选被一个或多个选自以下的取代基取代的C 5-10芳基:卤素,硝基,氰基,醚,C 1-7烷基,C 3-7杂环基和双 - 氧C 1-3亚烷基。 其他变量如权利要求中所定义。 该化合物可用于治疗增殖性疾病。
    • 8. 发明授权
    • Pyrrolobenzodiazepines
    • 吡咯并苯并二氮杂卓
    • US08487092B2
    • 2013-07-16
    • US13124232
    • 2009-10-16
    • Philip Wilson HowardStephen John GregsonZhiZhi ChenArnaud Charles TiberghienLuke Masterson
    • Philip Wilson HowardStephen John GregsonZhiZhi ChenArnaud Charles TiberghienLuke Masterson
    • C07D519/00
    • C07D519/00
    • The invention relates to certain pyrrolobenzodiazepines (PBDs), and in particular pyrrolobenzodiazepine dimers bearing C2 substitutions, including compounds of formula (T): wherein: R2 is CHR2A, and R2A is independently selected from H, R, CO2R, COR, CHO, CO2H, and halo; 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; R8 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, NO2, Me3Sn and halo; R is independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; or the compound is a dimer with each monomer being of formula (M), where the R7 groups or R8 groups of each monomer form together a dimer bridge having the formula —X—R″—X— linking the monomers; wherein R″ is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms, e.g. O, S, N(H), and/or aromatic rings, e.g. benzene or pyridine; and each X is independently selected from O, S, or N(H); or any pair of adjacent groups from R6 to R9 together form a group —O—(CH2)p—O—, where p is 1 or 2, and salts and solvates thereof, and their use as intermediates for the preparation of other PBD compounds.
    • 本发明涉及某些吡咯并苯并二氮杂(PBD),特别是含有C2取代的吡咯并苯并二氮杂二聚体,包括式(T)化合物:其中:R2为CHR2A,R2A独立地选自H,R,CO2R,COR,CHO,CO2H ,和卤素; R 6和R 9独立地选自H,R,OH,OR,SH,SR,NH 2,NHR,NRR',NO 2,Me 3 Sn和卤素; R 7独立地选自H,R,OH,OR,SH,SR,NH 2,NHR,NRR',NO 2,Me 3 Sn和卤素; R 8独立地选自H,R,OH,OR,SH,SR,NH 2,NHR,NRR',NO 2,Me 3 Sn和卤素; R独立地选自任选取代的C 1-12烷基,C 3-20杂环基和C 5-20芳基; 或者化合物是每个单体具有式(M)的二聚体,其中每个单体的R 7基团或R 8基团一起形成具有式-X-R“-X-连接单体的二聚体桥; 其中R“是C 3-12亚烷基,该链可被一个或多个杂原子间隔,例如, O,S,N(H)和/或芳环,例如。 苯或吡啶; 并且每个X独立地选自O,S或N(H); 或R6至R9的任何一对相邻基团一起形成-O-(CH 2)p -O-基团,其中p为1或2,以及其盐和溶剂化物,以及它们作为制备其它PBD化合物的中间体的用途。
    • 9. 发明申请
    • PYRROLOBENZODIAZEPINES
    • PYRROBOBENZODIAZEPINES
    • US20110201803A1
    • 2011-08-18
    • US13124232
    • 2009-10-16
    • Philip Wilson HowardStephen John GregsonZhizhi ChenArnaud Charles TiberghienLuke Masterson
    • Philip Wilson HowardStephen John GregsonZhizhi ChenArnaud Charles TiberghienLuke Masterson
    • C07D487/04
    • C07D519/00
    • The invention relates to certain pyrrolobenzodiazepines (PBDs), and in particular pyrrolobenzodiazepine dimers bearing C2 substitutions, including compounds of formula (T): wherein: R2 is CHR2A, and R2A is independently selected from H, R, CO2R, COR, CHO, CO2H, and halo; 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; R8 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, NO2, Me3Sn and halo; R is independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; or the compound is a dimer with each monomer being of formula (M), where the R7 groups or R8 groups of each monomer form together a dimer bridge having the formula —X—R″—X— linking the monomers; wherein R″ is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms, e.g. O, S, N(H), and/or aromatic rings, e.g. benzene or pyridine; and each X is independently selected from O, S, or N(H); or any pair of adjacent groups from R6 to R9 together form a group —O—(CH2)p—O—, where p is 1 or 2, and salts and solvates thereof, and their use as intermediates for the preparation of other PBD compounds.
    • 本发明涉及某些吡咯并苯并二氮杂(PBD),特别是含有C2取代的吡咯并苯并二氮杂二聚体,包括式(T)化合物:其中:R2为CHR2A,R2A独立地选自H,R,CO2R,COR,CHO,CO2H ,和卤素; R 6和R 9独立地选自H,R,OH,OR,SH,SR,NH 2,NHR,NRR',NO 2,Me 3 Sn和卤素; R 7独立地选自H,R,OH,OR,SH,SR,NH 2,NHR,NRR',NO 2,Me 3 Sn和卤素; R 8独立地选自H,R,OH,OR,SH,SR,NH 2,NHR,NRR',NO 2,Me 3 Sn和卤素; R独立地选自任选取代的C 1-12烷基,C 3-20杂环基和C 5-20芳基; 或者化合物是每个单体具有式(M)的二聚体,其中每个单体的R 7基团或R 8基团一起形成具有式-X-R“-X-连接单体的二聚体桥; 其中R“是C 3-12亚烷基,该链可被一个或多个杂原子间隔,例如。 O,S,N(H)和/或芳环,例如。 苯或吡啶; 并且每个X独立地选自O,S或N(H); 或从R6至R9的任何一对相邻基团一起形成-O-(CH 2)p -O-基团,其中p为1或2,以及其盐和溶剂化物,以及它们作为制备其它PBD化合物的中间体的用途 。
    • 10. 发明申请
    • UNSYMMETRICAL PYRROLOBENZODIAZEPINE-DIMERS FOR TREATMENT OF PROLIFERATIVE DISEASES
    • 用于治疗增殖性疾病的非对称吡嗪二酮
    • US20110196148A1
    • 2011-08-11
    • US13123327
    • 2009-10-16
    • Philip Wilson HowardStephen John GregsonLuke Masterson
    • Philip Wilson HowardStephen John GregsonLuke Masterson
    • C07D487/04
    • C07D487/04
    • Claimed are unsymmetrical Pyrrolobenzodiazepine-dimers (PBD-dimers) of formula (I), that are unsymmetrical due at least to the values that the variables R12 and R2 represent. Formula (I), wherein: R2 is of formula (II), where A is a C5-7 aryl group, X is selected from the group comprising: OH, SH, CO2H, COH, N═C═O, NHRN, wherein RN is selected from the group comprising H and C1-4 alkyl, and (OC2H4)mOCH3, where m is 1 to 3, and either: (i) Q1 is a single bond, and Q2 is selected from a single bond and —Z—(CH2)m—, where Z is selected from a single bond, O, S and NH and n is from 1 to 3; or (ii) Q1 is —CH═CH—, and Q2 is a single bond; R12 is a C5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, C1-7 alkyl, C3-7 heterocyclyl and bis-oxy-C1-3 alkylene. The other variables are as defined in the claims. The compounds are useful for the treatment of proliferative diseases.
    • 声称是式(I)的不对称吡咯并苯并二氮杂二聚体(PBD-二聚体),其至少与变量R12和R2表示的值不对称。 式(I)其中:R2为式(II),其中A为C5-7芳基,X选自OH,SH,CO2H,COH,N = C = O,NHRN,其中 RN选自H和C 1-4烷基,和(OC 2 H 4)m OCH 3,其中m为1至3,以及:(i)Q1为单键,Q2选自单键和-Z - (CH 2)m - ,其中Z选自单键,O,S和NH,n为1至3; 或(ii)Q1是-CH = CH-,Q2是单键; R 12是任选被一个或多个选自以下的取代基取代的C 5-10芳基:卤素,硝基,氰基,醚,C 1-7烷基,C 3-7杂环基和双 - 氧C 1-3亚烷基。 其他变量如权利要求中所定义。 该化合物可用于治疗增殖性疾病。