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41. 发明专利

CA2901114C NOVEL ANTIBODY CONJUGATES AND USES THEREOF 未知
公开(公告)号：CA2901114C
公开(公告)日：2020-01-07
申请号：CA2901114
申请日：2014-02-21
申请人： STEMCENTRX INC , SPIROGEN SARL
发明人： TORGOV MICHAEL , HOWARD PHILIP WILSON
IPC分类号： C07K16/28 , A61P35/00 , C07K5/062 , C07K16/00 , C07K16/18
摘要： Provided are novel antibody drug conjugates (ADCs), and methods of using such ADCs to treat proliferative disorders.

42. 发明专利

CA2850373C PYRROLOBENZODIAZEPINES AND TARGETED CONJUGATES 未知
公开(公告)号：CA2850373C
公开(公告)日：2019-07-16
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 , 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.

43. 发明专利

CA2849039C PYRROLOBENZODIAZEPINES AS UNSYMMETRICAL DIMERIC PBD COMPOUNDS FOR INCLUSION IN TARGETED CONJUGATES 未知
公开(公告)号：CA2849039C
公开(公告)日：2018-09-18
申请号：CA2849039
申请日：2012-09-20
申请人： SPIROGEN SARL
发明人： HOWARD PHILIP WILSON
IPC分类号： C07D519/00 , A61K31/5517 , 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.

44. 发明专利

CA2850096C SYNTHESIS METHOD AND INTERMEDIATES USEFUL IN THE PREPARATION OF PYRROLOBENZODIAZEPINES 未知
公开(公告)号：CA2850096C
公开(公告)日：2018-07-03
申请号：CA2850096
申请日：2012-10-12
申请人： SPIROGEN SARL
发明人： HOWARD PHILIP WILSON , TIBERGHIEN ARNAUD
IPC分类号： C07D207/20 , A61K31/5517 , A61P35/00 , C07D207/24 , C07D207/27 , C07D401/12 , C07D409/12 , C07D413/12 , C07D487/04 , C07D519/00
摘要： A compound of formula I wherein: R7 is selected from: ORA, where RA is selected from C1-4 saturated alkyl, optionally substituted by phenyl, which may bear a chloro substituent, pyridyl and furanyl; chloro; NH2; -CH2-O-C(=O)Me; R8 is OProt°, where Prot° is a silicon-based oxygen protecting group orthogonal to Rc; R9 is selected from H, methyl and methoxy; Rs is selected from CF3, (CF2)3CF3, CH3 and (formula 2) and Rc is selected from: (i) -C(=O)-ORC1, where RC1 is a saturated C1-4 alkyl group; (ii) -CH2-O-C(=0)RC2, where RC2 is methyl or phenyl; (iii) -CH2-O-Si-(RSi1)(RSi2)(RSi3), where RSi1, RSi2, RSi3 are independently selected from C1-6 a saturated alkyl group and a phenyl group; and (iv) -C(-YRC3)(-YRC4) where each Y is independently O or S, and where RC3 and RC4 are independently a saturated C1-4 alkyl group, or together form a C2-3 alkylene.

45. 发明专利

AU2013366493A1 Pyrrolobenzodiazepines and conjugates thereof 未知
公开(公告)号：AU2013366493A1
公开(公告)日：2015-07-09
申请号：AU2013366493
申请日：2013-12-20
申请人： SPIROGEN SARL
发明人： HOWARD PHILIP WILSON
IPC分类号： C07D487/04 , A61K47/48 , A61P35/00
摘要： A compound with the formula (I) and salts and solvates thereof, wherein: when there is a double bond present between C2 and C3, R

46. 发明专利

RS53818B1 PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 未知
公开(公告)号：RS53818B1
公开(公告)日：2015-06-30
申请号：RSP20150105
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.

47. 发明专利

AU2013328580A1 Pyrrolobenzodiazepines and conjugates thereof 未知
公开(公告)号：AU2013328580A1
公开(公告)日：2015-04-02
申请号：AU2013328580
申请日：2013-10-11
申请人： SPIROGEN SARL
发明人： HOWARD PHILIP WILSON
IPC分类号： C07D487/04 , A61K47/48 , A61P35/00 , 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.

48. 发明专利

ES2530968T3 Pirrolobenzodiazepinas y conjugados de las mismas 未知
公开(公告)号：ES2530968T3
公开(公告)日：2015-03-09
申请号：ES13780100
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： Un compuesto B:**Fórmula** y sales y solvatos del mismo.

49. 发明专利

NZ602933A Pyrrolobenzodiazepines used to treat proliferative diseases 未知
公开(公告)号：NZ602933A
公开(公告)日：2014-09-26
申请号：NZ60293311
申请日：2011-04-15
申请人： SEATTLE GENETICS INC , SPIROGEN SARL
发明人： SENTER PETER , TIBERGHIEN ARNAUD , MASTERSON LUKE , BURKE PATRICK , JEFFREY SCOTT , HOWARD PHILIP WILSON
IPC分类号： C07D519/00 , A61K31/5517 , A61P35/00
摘要： Disclosed herein is a compound of the formula I, wherein the variables are defined herein; a conjugate of the formula III, L – (LU-D)p, wherein L is a Ligand unit, LU is a Linker unit, p is 1 to 20, and D is a Drug unit of formula I; and the use of said conjugate for treating a proliferative disease or an autoimmune disease. Specific embodiments of the compound include (S)-2-(4-aminopheny/)-7-methoxy-8-(3-((S)-7-methoxy-2-(trifluoromethylsulfonyl)-5,11-dioxo-10-((2-(trimethylsilyl)ethoxy)methyl)-5,10,11,11a-tetrahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-8-yloxy)propoxy)-10-((2-(trimethylsilyl)ethoxy)methyl)-1H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11(10H, 11aH)-dione.

50. 发明专利

CA2894961A1 PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 未知
公开(公告)号：CA2894961A1
公开(公告)日：2014-06-26
申请号：CA2894961
申请日：2013-12-20
申请人： SPIROGEN SARL
发明人： HOWARD PHILIP WILSON
IPC分类号： C07D487/04 , A61K47/48 , A61P35/00
摘要： A compound with the formula (I) and salts and solvates thereof, wherein: when there is a double bond present between C2 and C3, R2 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, C1-7 alkyl, C3-7 heterocyclyl and bis-oxy-C1-3 alkylene; (ib) C1-5 saturated aliphatic alkyl; (ic) C3-6 saturated cycloalkyl; (id) (Formula (S)), wherein each of R11, R12 and R13 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 R2 group is no more than 5; (ie) (Formula (T)), wherein one of R15a and R15b 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) (Formula (U)), where R14 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, R2 is (Formula (V)), where R16a and R16b 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 R16a and R16b is H, the other is selected from nitrile and a C1-4 alkyl ester; 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) (Formula (W)), 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) (Formula (X)), 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) (Formula (Y)), 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; R20 is H or Me and R21a and R21b are both H or together form =O; RL is a linker for connection to a cell binding agent; R11b is selected from OH, ORA, where RA is C1-4 alkyl, and SOzM, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation.

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