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1. 发明专利

ES2930295T3 Compuestos y conjugados de los mismos 未知
公开(公告)号：ES2930295T3
公开(公告)日：2022-12-09
申请号：ES20713873
申请日：2020-03-23
申请人： MEDIMMUNE LTD
发明人： HOWARD PHILIP , DICKINSON NIALL , CAILLEAU THAIS , MASTERSON LUKE , GOUNDRY WILLIAM
IPC分类号： A61K47/68 , A61P35/00 , C07D491/22 , C07K5/06 , C07K5/08 , C07K5/10

2. 发明专利

NZ751432A Pyrrolobenzodiazepines and conjugates thereof 未知
公开(公告)号：NZ751432A
公开(公告)日：2021-01-29
申请号：NZ75143214
申请日：2014-03-13
申请人： GENENTECH INC , MEDIMMUNE LTD
发明人： FLYGARE JOHN , PILLOW THOMAS , HOWARD PHILIP , WEI BINQING
IPC分类号： A61K31/5517 , A61K47/68 , C07D487/04
摘要： The present invention relates to pyrrolobenzodiazepines (PBDs), in particular pyrrolobenzodiazepines having a linker group connected to a cell binding agent. In one aspect, the present invention provides a conjugate comprising a PBD dimer connected through the dimer bridging portion via a specified linker to a cell binding agent. The present invention is suitable for use in providing a PBD conjugate to a preferred site in a subject. In particular, the present invention provides a conjugate of formula (A), use of a conjugate of formula (A) the manufacture of a medicament, a pharmaceutical composition comprising a conjugate of formula (A), a compound of formula (B), a compound of formula (C), a compound of formula (D), a compound of formula (E) and/or a method of synthesis of a compound. In preferred embodiments, use of a conjugate of formula (A) the manufacture of a medicament for treating cancer and/or a proliferative disease. 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).

3. 发明专利

ES2731779T3 Pirrolobenzodiazepinas y conjugados de las mismas 未知
公开(公告)号：ES2731779T3
公开(公告)日：2019-11-19
申请号：ES14741363
申请日：2014-03-13
申请人： MEDIMMUNE LTD
发明人： HOWARD PHILIP , FLYGARE JOHN , PILLOW THOMAS , WEI BINQING
IPC分类号： A61K47/68 , A61P35/00 , C07D519/00
摘要： Un conjugado de fórmula (Ia):**Fórmula** en la que: R2a y R22a se seleccionan independientemente del grupo que consiste en: (ia)**Fórmula** (ib)**Fórmula** (ic)**Fórmula** (id)**Fórmula** (ie)**Fórmula** (if)**Fórmula** R7a y R17a se seleccionan independientemente de metilo y fenilo; Y se selecciona de las fórmulas A1, A2, A3, A4, A5 y A6:**Fórmula** L es un enlazador conectado a un agente de unión celular; CBA es el agente de unión celular; n es un número entero seleccionado en el intervalo de 0 a 48; RA4 es un grupo alquileno C1-6; bien (a) R10 es H y R11 es OH, ORA, donde RA es alquilo C1-4; o (b) R10 y R11 forman un doble enlace nitrógeno-carbono entre los átomos de nitrógeno y de carbono a los que están unidos; o (c) R10 es H y R11 es OSOzM, donde z es 2 o 3 y M es un catión monovalente farmacéuticamente aceptable; en donde R20 y R21 son como se definen para R10 y R11 respectivamente; en donde Z es CH o N; y t1 y t2 se seleccionan independientemente de 0, 1 y 2.

4. 发明专利

NZ710746A Pyrrolobenzodiazepines and conjugates thereof 未知
公开(公告)号：NZ710746A
公开(公告)日：2018-11-30
申请号：NZ71074614
申请日：2014-03-13
申请人： MEDIMMUNE LTD
发明人： FLYGARE JOHN , PILLOW THOMAS , HOWARD PHILIP , WEI BINQING
IPC分类号： A61K47/68 , A61K47/00 , A61P35/00 , C07D487/04 , C07D519/00
摘要： The present invention relates to a pyrrolobenzodiazepines (PBD), in particular pyrrolobenzodiazepines having a linker group connected to a cell binding agent. Further or alternatively, the invention relates to conjugates of formula Ia, pharmaceutical compositions thereof, use thereof in the preparation of a medicament for the treatment of a proliferative disease (in particular breast cancer), and/or PBD compounds IIa, IIIa, IVa and/or Va.

5. 发明专利

LT3946464T JUNGINIAI IR JŲ KONJUGATAI 未知
公开(公告)号：LT3946464T
公开(公告)日：2022-11-10
申请号：LT20057984
申请日：2020-03-23
申请人： MEDIMMUNE LTD
发明人： HOWARD PHILIP , DICKINSON NIALL , CAILLEAU THAIS , MASTERSON LUKE , GOUNDRY WILLIAM
IPC分类号： A61K47/68 , A61P35/00 , C07D491/22 , C07K5/06 , C07K5/08 , C07K5/10

6. 发明专利

ECSP22064855A COMPUESTOS Y CONJUGADOS DE ESTOS 未知
公开(公告)号：ECSP22064855A
公开(公告)日：2022-09-30
申请号：ECDI202264855
申请日：2022-08-18
申请人： MEDIMMUNE LTD
发明人： HOWARD PHILIP , YOU FEI , DICKINSON NIALL
IPC分类号： A61K47/68 , A61P35/00
摘要： Un conjugado que comprende el siguiente derivado de un inhibidor de la topoisomerasa (A*): con un conector para la unión a una Unidad de Ligando, donde el conector está enlazado de una forma escindible al residuo amínico. La Unidad de Ligando es preferentemente un anticuerpo. También se proporciona A* con la unidad conectora enlazada e intermedios para su síntesis, así como también la carga útil liberada.

7. 发明专利

SG11202110524VA COMPOUNDS AND CONJUGATES THEREOF 未知
公开(公告)号：SG11202110524VA
公开(公告)日：2021-10-28
申请号：SG11202110524V
申请日：2020-03-23
申请人： MEDIMMUNE LTD
发明人： HOWARD PHILIP , DICKINSON NIALL , CAILLEAU THAIS , MASTERSON LUKE , GOUNDRY WILLIAM
IPC分类号： A61K47/68 , A61P35/00 , C07D491/22 , C07K5/06 , C07K5/08 , C07K5/10
摘要： A conjugate comprising the following topoisomerase inhibitor derivative (A*):with a linker for connecting to a Ligand Unit, wherein the linker is attached in a cleavable manner to the amino residue. The Ligand Unit is preferably an antibody. Also provided is A* with the linking unit attached, and intermediates for their synthesis, as well as the released warhead.

8. 发明专利

ES2728869T3 Pirrolobenzodiazepinas y conjugados de las mismas 未知
公开(公告)号：ES2728869T3
公开(公告)日：2019-10-29
申请号：ES14793027
申请日：2014-10-10
申请人： MEDIMMUNE LTD
发明人： HOWARD PHILIP , EZEADI EBELE , D'HOOGE FRANCOIS , PATEL NEKI , KEMP GARY
IPC分类号： A61K47/68 , A61P35/00 , C07D487/04 , C07D519/00
摘要： Un compuesto que es C**Fórmula** y sales y solvatos del mismo.

9. 发明专利

ES2660233T3 Pirrolobenzodiazepinas y conjugados dirigidos 未知
公开(公告)号：ES2660233T3
公开(公告)日：2018-03-21
申请号：ES12840422
申请日：2012-10-12
申请人： SEATTLE GENETICS INC , MEDIMMUNE LTD
发明人： JEFFREY SCOTT , BURKE PATRICK , HOWARD PHILIP
IPC分类号： A01N43/62 , C07D487/04 , C07D519/00
摘要： Un compuesto con la fórmula I:**Fórmula** en la que: R2 es de fórmula III:**Fórmula** en la que A es fenilo y Q2 se selecciona entre un enlace sencillo y -CH2-; R12 es fenilo, sustituido con un grupo seleccionado entre OH, CO2H y CO2Me; R6, R6', R9 y R9' son H; R7 es un alquiloxi C1-4 y: (a) R10 es H, y R11 es OH, ORA, en donde RA es alquilo C1-4; o (b) R10 y R11 forman un doble enlace nitrógeno-carbono entre los átomos de nitrógeno y carbono a los que están unidos; R" es un grupo alquileno C3-7; Y e Y' son O; R7' se selecciona entre los mismos grupos que R7 y R10' y R11' son iguales que R10 y R11, en donde el término alquilo incluye las subclases alquenilo, alquinilo y cicloalquilo, y el término alquileno incluye las subclases alquenileno, alquinileno y cicloalquileno.

10. 发明专利

AU2021211892A1 Compounds and conjugates thereof 未知
公开(公告)号：AU2021211892A1
公开(公告)日：2022-09-08
申请号：AU2021211892
申请日：2021-01-21
申请人： MEDIMMUNE LTD
发明人： YOU FEI , DICKINSON NIALL , HOWARD PHILIP
IPC分类号： A61K47/68 , A61P35/00
摘要： A conjugate comprising the following topoisomerase inhibitor derivative (A*): with a linker for connecting to a Ligand Unit, wherein the linker is attached in a cleavable manner to the amino residue. The Ligand Unit is preferably an antibody. Also provided is A* with the linking unit attached, and intermediates for their synthesis, as well as the released warhead.

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