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31. 发明专利

NZ602932A Targeted pyrrolobenzodiazapine conjugates 未知
公开(公告)号：NZ602932A
公开(公告)日：2014-08-29
申请号：NZ60293211
申请日：2011-04-15
申请人： SEATTLE GENETICS INC , SPIROGEN SARL
发明人： JEFFREY SCOTT , HOWARD PHILIP WILSON , BURKE PATRICK , SENTER PETER
IPC分类号： A61K47/48 , A01N29/06 , A61P37/00
摘要： Disclosed herein is a conjugate of formula I, L – (LU-D)p, wherein L is a cell binding agent that specifically binds to a target molecule on the surface of a target cell, LU is a Linker unit, p is 1 to 20; and D is a Drug unit comprising a PBD dimer of formula II, wherein the variable are defined herein. Additionally disclosed is the use of the conjugate in the treatment of a proliferative or autoimmune disease. Specific embodiments of the conjugate include (E)-6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-N’-(4-((S)-7-methoxy-8-((5-(((S)-7-methoxy-2-(4-methoxyphenyl)-5-oxo-5,11a-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-8-yl)oxy)pentyl)oxy)-5-oxo-5,11a-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-2-yl)benzylidene)hexanehydrazide.

32. 发明专利

CA2894959A1 UNSYMMETRICAL PYRROLOBENZODIAZEPINES-DIMERS FOR USE IN THE TREATMENT OF PROLIFERATIVE AND AUTOIMMUNE DISEASES 未知
公开(公告)号：CA2894959A1
公开(公告)日：2014-06-26
申请号：CA2894959
申请日：2013-12-20
申请人： SPIROGEN SARL
发明人： HOWARD PHILIP WILSON
IPC分类号： C07D487/04 , A61K31/5517 , A61P19/00 , A61P35/00
摘要： A compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein: R2 is of formula (IIa), formula (IIb) or formula (IIc): (a) where A is a C5-7 aryl group, 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; (b) where: RC1, RC2 and RC3 are independently selected from H and unsubstituted C1-2 alkyl; (c) where Q is selected from OH, SH and NRN, and RN is selected from H, methyl and ethyl X is selected from the group comprising: OH, SH, CO2H, COH, N=C=O, NHNH2, CONHNH2, (formula (x)), (formular (y), NHRN, wherein RN is selected from the group comprising H and C1-4 alkyl; and either: when there is a double bond present between C2' and C3', R12 is selected from the group consisting of: (ia) C5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, carboxy, ester, C1-7 alkyl, C3-7 heterocyclyl and bis-oxy-C1-3 alkylene; (ib) C1-5 saturated aliphatic alkyl; (ic) C3-6 saturated cycloalkyl; (id), wherein each of R21, R22 and R23 are independently selected from H, C1-3 saturated alkyl, C2-3 alkenyl, C2-3 alkynyl and cyclopropyl, where the total number of carbon atoms in the R12 group is no more than 5; (ie), wherein one of R25a and R25b is H and the other is selected from: phenyl, which phenyl is optionally substituted by a group selected from halo, methyl, methoxy; pyridyl; and thiophenyl; and (if), where R24 is selected from: H; C1-3 saturated alkyl; C2-3 alkenyl; C2-3 alkynyl; cyclopropyl; phenyl, which phenyl is optionally substituted by a group selected from halo, methyl, methoxy; pyridyl; and thiophenyl; when there is a single bond present between C2' and C3', R12 is (formula (z)), where R26a and R26b 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 R26a and R26b 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', 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, NHRR', 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; either: (A) R20 is H or Me and R21a and R21b are both H or together form =O and either: (i) R10 is H, R11a is H and R11b is OH or ORA, where RA is C1-4 alkyl; or (ii) R10 and R11b form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound and R11a is H; or (iii) R10 is H, R11a is H and R11b is SOzM, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; or (B) R10 is H or Me and R11a and R11b are both H or together form =O and either: (i) R20 is H, R21a is H and R21b is OH or ORA, where RA is C1-4 alkyl; or (ii) R20 and R21b form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound and R11a is H; or (iii) R20 is H, R21a is H and R21b is SOzM, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation.

33. 发明专利

AU2012322613A1 Pyrrolobenzodiazepines and targeted conjugates 未知
公开(公告)号：AU2012322613A1
公开(公告)日：2014-05-29
申请号：AU2012322613
申请日：2012-10-12
申请人： SPIROGEN SARL , SEATTLE GENETICS INC
发明人： JEFFREY SCOTT , BURKE PATRICK , HOWARD PHILIP WILSON
IPC分类号： A01N43/62
摘要： This invention relates to pyrrolobenzodiazepines (PBDs), in particular pyrrolobenzodiazepine dimers having a C2-C3 double bond and an aryl group at the C2 position in each monomer unit, and their inclusion in targeted conjugates. The differing substituent groups may offer advantages in the preparation and use of the compounds, particularly in their biological properties and the synthesis of conjugates, and the biological properties of these conjugates.

34. 发明专利

SG11201400770SA PYRROLOBENZODIAZEPINES AS UNSYMMETRICAL DIMERIC PBD COMPOUNDS FOR INCLUSION IN TARGETED CONJUGATES 未知
公开(公告)号：SG11201400770SA
公开(公告)日：2014-04-28
申请号：SG11201400770S
申请日：2012-09-20
申请人： SPIROGEN SARL
发明人： HOWARD PHILIP WILSON
IPC分类号： A61K31/5517 , C07D519/00 , A61K47/48 , A61P35/00
摘要： A compound with the formula I wherein: R2 is of formula II where Q is selected from OH, SH and NRN, and RN is selected from H, methyl and ethyl, as well as drug-linkers and drug-conjugates made from this compound.

35. 发明专利

CA2885340A1 PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 未知
公开(公告)号：CA2885340A1
公开(公告)日：2014-04-17
申请号：CA2885340
申请日：2013-10-11
申请人： SPIROGEN SARL
发明人： HOWARD PHILIP WILSON
IPC分类号： A61K47/48 , A61P35/00 , C07D487/04 , C07D519/00
摘要： A compound which is either A or B and salts and solvates thereof, as well as conjugates thereof with cell binding agent.

36. 发明专利

DK2528625T3 Pyrrolobenzodiazepiner og konjugater deraf 未知
公开(公告)号：DK2528625T3
公开(公告)日：2013-10-14
申请号：DK11716146
申请日：2011-04-15
申请人： SPIROGEN SARL
发明人： HOWARD PHILIP WILSON , MASTERSON LUKE , TIBERGHIEN ARNAUD , FLYGARE JOHN A , GUNZNER JANET L , POLAKIS PAUL , POLSON ANDREW , RAAB HELGA E , SPENCER SUSAN D
IPC分类号： A61K47/48 , A61P35/00 , C07D487/04

37. 发明专利

CA2850373A1 PYRROLOBENZODIAZEPINES AND TARGETED CONJUGATES 未知
公开(公告)号：CA2850373A1
公开(公告)日：2013-04-18
申请号：CA2850373
申请日：2012-10-12
申请人： SEATTLE GENETICS INC , SPIROGEN SARL
发明人： JEFFREY SCOTT , BURKE PATRICK , HOWARD PHILIP WILSON
IPC分类号： C07D519/00 , A61K31/5517 , A61K47/48 , A61P35/00
摘要： A compound, or a pharmaceutically acceptable salt or solvate thereof, or conjugates thereof, selected from the group consisting of formula wherein: (a) R10 is H, and R11 is OH, ORA, where RA is saturated C1-4 alkyl; (b) R10 and R11 form a nitrogen-carbon doub!e bond between the nitrogen and carbon atoms to which they are bound; or (c) R10 is H and R11 is S02M, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation, or both M together are a divalent pharmaceutically acceptable cation.

38. 发明专利

MX2012011901A PIRROLOBENZODIACEPINAS Y CONJUGADOS DE LAS MISMAS. 未知
公开(公告)号：MX2012011901A
公开(公告)日：2012-11-29
申请号：MX2012011901
申请日：2011-04-15
申请人： SPIROGEN SARL
发明人： POLAKIS PAUL , SPENCER SUSAN D , HOWARD PHILIP WILSON , POLSON ANDREW , MASTERSON LUKE , TIBERGHIEN ARNAUD , FLYGARE JOHN A , GUNZNER JANET L , RAAB HELGA E
IPC分类号： A61K47/48 , A61P35/00 , C07D487/04
摘要： Se desvelan conjugados y compuestos para fabricar conjugados que son moléculas de PBD engarzadas mediante la posición N10, junto con el uso de los conjugados para tratar enfermedades proliferativas, incluyendo cáncer.

39. 发明专利

ZA201505753B PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 未知
公开(公告)号：ZA201505753B
公开(公告)日：2022-03-30
申请号：ZA201505753
申请日：2015-08-11
申请人： SPIROGEN SARL
发明人： HOWARD PHILIP WILSON , FLYGARE JOHN A , PILLOW THOMAS , WEI BINQING
摘要： A conjugate of formula (A):

40. 发明专利

CA2872205C PYRROLOBENZODIAZEPINES 未知
公开(公告)号：CA2872205C
公开(公告)日：2020-07-21
申请号：CA2872205
申请日：2013-04-30
申请人： UCL BUSINESS PLC , SPIROGEN SARL
发明人： HOWARD PHILIP WILSON , THURSTON DAVID EDWIN , RAHMAN KHONDAKER MIRAZUR , TAYLOR PETER WILLIAM
IPC分类号： C07D487/04 , A61K31/5517 , A61P31/04
摘要： Disclosed are compounds of formula (l), salts and solvates thereof: (see formula I) and their use in treatment of bacterial infections.

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