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公开(公告)号:US10533058B2
公开(公告)日:2020-01-14
申请号:US15104388
申请日:2014-12-16
申请人: GENENTECH INC. , MEDIMMUNE LIMITED
发明人: John Flygare , Janet Gunzner-Toste , Thomas Pillow , Brian Safina , Vishal Verma , Binqing Wei , Guiling Zhao , Leanna Staben , Philip Wilson Howard , Luke Masterson
IPC分类号: A61K47/68 , A61K31/5517 , C07K16/30 , C07K16/28
摘要: This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof, pharmaceutical compositions containing them, and to their use in therapy for the prevention treatment of cancer.
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公开(公告)号:US10576164B2
公开(公告)日:2020-03-03
申请号:US15786055
申请日:2017-10-17
申请人: MedImmune Limited , Genentech, Inc.
IPC分类号: A61K47/68 , A61P35/00 , C07D498/14 , C07D519/00 , A61K31/5517 , C07D487/04 , C07D487/16
摘要: 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).
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公开(公告)号:US20160144052A1
公开(公告)日:2016-05-26
申请号:US14774535
申请日:2014-03-13
申请人: MEDIMMUNE LIMITED
IPC分类号: A61K47/48 , C07K16/28 , C07K16/40 , C07D519/00 , A61K31/5517
CPC分类号: A61K47/48646 , A61K31/5517 , A61K47/6803 , A61K47/6855 , A61K47/6871 , C07D519/00 , C07K16/2863 , C07K16/40 , C07K2317/92
摘要: A conjugate of formula (A):
摘要翻译: 式(A)的缀合物:
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公开(公告)号:US09649390B2
公开(公告)日:2017-05-16
申请号:US14774535
申请日:2014-03-13
申请人: MEDIMMUNE LIMITED
IPC分类号: C07D487/04 , A61K47/48 , C07D519/00 , A61K31/5517 , C07K16/28 , C07K16/40
CPC分类号: A61K47/48646 , A61K31/5517 , A61K47/6803 , A61K47/6855 , A61K47/6871 , C07D519/00 , C07K16/2863 , C07K16/40 , C07K2317/92
摘要: A conjugate of formula (A):
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公开(公告)号:US20210309660A1
公开(公告)日:2021-10-07
申请号:US16858004
申请日:2020-04-24
申请人: Genentech, Inc.
发明人: Nicole Blaquiere , Peter Dragovich , Lewis J. Gazzard , Thomas Pillow , Steven T. Staben , Binqing Wei , Jianfeng Xin
IPC分类号: C07D471/16 , C07D493/10 , C07D403/04 , C07D417/14 , C07D413/14 , A61P35/00
摘要: The present disclosure relates to bifunctional compounds, which can be used as modulators of targeted ubiquitination. In particular, the present disclosure is directed to compounds which contain on one end a VHL ligand moiety, which binds to the VHL E3 ubiquitin ligase, and on the other end a moiety that binds a target protein such that degradation of the target protein/polypeptide is effectuated. Also disclosed are VHL ligands.
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公开(公告)号:US20190175612A1
公开(公告)日:2019-06-13
申请号:US16194897
申请日:2018-11-19
申请人: Genentech, Inc.
发明人: Thomas Pillow , Jack Sadowsky , Leanna Staben , Steven Staben , Binqing Wei , Ingrid Wertz , Pragya Adhikari , Nicole Blaquiere , Peter Dragovich , Wayne Fairbrother
摘要: The subject matter described herein is directed to antibody-PROTAC conjugates (PACs), to pharmaceutical compositions containing them, and to their use in treating diseases and conditions where targeted protein degradation is beneficial.
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公开(公告)号:US20180125995A1
公开(公告)日:2018-05-10
申请号:US15612193
申请日:2017-06-02
申请人: Genentech, Inc.
发明人: Eric Brown , Wouter Hazenbos , Isidro Hotzel , Kimberly Kajihara , Sophie M. Lehar , Sanjeev Mariathasan , Thomas Pillow , Leanna Staben , Vishal Verma , Binqing Wei , Yi Xia , Min Xu
IPC分类号: A61K47/68 , C07K16/12 , A61K31/5383 , A61K45/06 , A61P31/04
CPC分类号: A61K47/6803 , A61K31/5383 , A61K45/06 , A61K47/6835 , A61K47/6889 , A61P31/04 , C07K16/1271 , C07K2317/21
摘要: The invention provides rF1 antibody antibiotic conjugates and methods of using same.
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公开(公告)号:US20180021450A1
公开(公告)日:2018-01-25
申请号:US15611985
申请日:2017-06-02
申请人: Genentech, Inc.
发明人: Eric Brown , Wouter Hazenbos , Isidro Hotzel , Kimberly Kajihara , Sophie M. Lehar , Sanjeev Mariathasan , Thomas Pillow , Leanna Staben , Vishal Verma , Binqing Wei , Min Xu
IPC分类号: A61K47/68 , A61K31/4468 , A61K39/40 , A61K31/496
CPC分类号: A61K47/6809 , A61K31/4468 , A61K31/496 , A61K39/40 , A61K47/6803 , A61K47/6835 , A61K47/6889
摘要: The invention provides anti-Staphylococcus aureus antibody rifamycin antibiotic conjugates and methods of using same.
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公开(公告)号:US09999681B2
公开(公告)日:2018-06-19
申请号:US15181825
申请日:2016-06-14
申请人: Genentech, Inc.
发明人: John Flygare , Janet Gunzner-Toste , Thomas Pillow , Brian Safina , Vishal Verma , Binqing Wei , Guiling Zhao , Leanna Staben
CPC分类号: A61K47/6803 , A61K47/6809 , A61K47/6849 , A61K47/6851 , A61K47/6889 , C07K16/28 , C07K16/2851 , C07K16/30 , C07K2317/24 , C07K2317/56 , C07K2317/76
摘要: This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer.
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公开(公告)号:US09821074B2
公开(公告)日:2017-11-21
申请号:US14208374
申请日:2014-03-13
申请人: Spirogen Sàrl , Genentech, Inc.
IPC分类号: A61K47/48 , A61K31/5517 , C07D519/00 , C07D487/04
CPC分类号: A61K47/6869 , A61K31/5517 , A61K47/6803 , A61K47/6851 , A61K47/6855 , A61K47/6889 , A61P35/00 , C07D487/04 , C07D487/16 , C07D519/00
摘要: 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).
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