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Last Updated: July 11, 2020

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Patent: 9,821,074

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Summary for Patent: 9,821,074
Title:Pyrrolobenzodiazepines and conjugates thereof
Abstract: Conjugate compounds of formula (A): ##STR00001## wherein: R.sup.2 is ##STR00002## where R.sup.36a and R.sup.36b are independently selected from H, F, C.sub.1-4 saturated alkyl, C.sub.2-3 alkenyl, which alkyl and alkenyl groups are optionally substituted by a group selected from C.sub.1-4 alkyl amido and C.sub.1-4 alkyl ester or, when one of R.sup.36a and R.sup.36b is H, the other is selected from nitrile and a C.sub.1-4 alkyl ester; R.sup.6 and R.sup.9 are independently selected from H, R, OH, OR, SH, SR, NH.sub.2, NHR, NRR\', NO.sub.2, Me.sub.3Sn and halo; R.sup.7 is independently selected from H, R, OH, OR, SH, SR, NH.sub.2, NHR, NRR\', NO.sub.2, Me.sub.3Sn and halo; Y is selected from formulae A1, A2, A3, A4, A5 and A6: ##STR00003## ##STR00004## 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; R.sup.A4 is a C.sub.1-6 alkylene group; either (a) R.sup.10 is H, and R.sup.11 is OH, OR.sup.A, where R.sup.A is C.sub.1-4 alkyl; or (b) R.sup.10 and R.sup.11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (c) R.sup.10 is H and R.sup.11 is OSO.sub.zM, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; R and R\' are each independently selected from optionally substituted C.sub.1-12 alkyl, C.sub.3-20 heterocyclyl and C.sub.5-20 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 R.sup.16, R.sup.17, R.sup.19, R.sup.20, R.sup.21 and R.sup.22 are as defined for R.sup.6, R.sup.7, R.sup.9, R.sup.10, R.sup.11 and R.sup.2 respectively; wherein Z is CH or N; wherein T and T\' are independently selected from a single bond or a C.sub.1-9 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).
Inventor(s): Howard; Philip Wilson (London, GB), Flygare; John A. (South San Francisco, CA), Pillow; Thomas (South San Francisco, CA), Wei; Binqing (South San Francisco, CA)
Assignee: Genentech, Inc. (San Francisco, CA) MedImmue Limited (GB)
Application Number:14/208,374
Patent Claims:see list of patent claims

Details for Patent 9,821,074

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Genentech Inc HERCEPTIN HYLECTA trastuzumab; hyaluronidase-oysk INJECTABLE;SUBCUTANEOUS 761106 001 2019-02-28   Start Trial Genentech, Inc. (San Francisco, CA) MedImmue Limited (GB) 2039-02-26 RX search
Genentech HERCEPTIN trastuzumab VIAL; INTRAVENOUS 103792 001 1998-09-25   Start Trial Genentech, Inc. (San Francisco, CA) MedImmue Limited (GB) 2039-02-26 RX Orphan search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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