DK2906248T3 - Pyrrolobenzodiazepiner og konjugater deraf - Google Patents

Pyrrolobenzodiazepiner og konjugater deraf Download PDF

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Publication number
DK2906248T3
DK2906248T3 DK13780099.1T DK13780099T DK2906248T3 DK 2906248 T3 DK2906248 T3 DK 2906248T3 DK 13780099 T DK13780099 T DK 13780099T DK 2906248 T3 DK2906248 T3 DK 2906248T3
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antibody
vol
genbank
update date
cell
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DK13780099.1T
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English (en)
Inventor
Philip Wilson Howard
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Medimmune Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • A61K47/6855—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell the tumour determinant being from breast cancer cell
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Claims (15)

1. Forbindelse, som er B:
og salte og solvater deraf.
2. Konjugat med formel ConjB:
hvor CBA betegner et cellebindingsstof.
3. Konjugat ifølge krav 2, hvor cellebindingsstoffet er et antistof eller et aktivt fragment deraf.
4. Konjugat ifølge krav 3, hvor antistoffet eller antistoffragmentet er et antistof eller antistoffragment til et tumor-associeret antigen.
5. Konjugat ifølge krav 3, hvor antistoffet eller antistoffragmentet er et antistof, som binder til et eller flere tumor-associerede antigener eller celleoverfladereceptorer udvalgt fra (1)-(88): (1) BMPR1B; (2) E16; (3) STEAP1; (4) 0772P; (5) MPF; (6) Napi3b; (7) Sema 5b; (8) PSCA hig;
(9) ETBR; (10) MSG783; (11) STEAP2; (12) TrpM4; (13) CRIPTO; (14) CD21; (15) CD79b; (16) FcRH2; (17) HER2; (18) NCA; (19) MDP; (20) IL20R-alpha; (21) Brevican; (22) EphB2R; (23) ASLG659; (24) PSCA; (25) GEDA; (26) BAFF-R; (27) CD22; (28) CD79a; (29) CXCR5; (30) HLA-DOB; (31) P2X5; (32) CD72; (33) LY64; (34) FcRH1; (35) IRTA2; (36) TENB2; (37) PSMA- FOLH1; (38) SST; (38.1) SSTR2; (38.2) SSTR5; (38.3) SSTR1; (38.4) SSTR3; (38.5) SSTR4; (39) ITGAV; (40) ITGB6; (41) CEACAM5; (42) MET; (43) MUC1; (44) CA9; (45) EGFRvlll; (46) CD33; (47) CD19; (48) IL2RA; (49) AXL; (50) CD30 - TNFRSF8; (51) BCMA-TNFRSF17; (52) CT Ags - CTA; (53) CD174 (Lewis Y) - FUT3; (54) CLEC14A; (55) GRP78 - HSPA5; (56) CD70; (57) Stamcellespecifikke antigener; (58) ASG-5; (59) ENPP3; (60) PRR4; (61) GCC - GUCY2C; (62) Liv-1 - SLC39A6; (63) 5T4; (64) CD56 - NCMA1; (65) CanAg; (66) FOLR1; (67) GPNMB; (68) TIM-1 - HAVCR1; (69) RG-1/Prostatatumor target Mindin - Mindin/RG-1; (70) B7-H4 -VTCN1; (71) PTK7; (72) CD37; (73) CD138 -SDC1; (74) CD74; (75) Claudins - CLs; (76) EGFR; (77) Her3; (78) RON - MST1R; (79) EPHA2; (80) CD20-MS4A1; (81) Tenascin C - TNC; (82) FAP; (83) DKK-1; (84) CD52; (85) CS1 - SLAMF7; (86) Endoglin - ENG; (87) Annexin A1 - ANXA1; (88) V-CAM (CD106) - VCAM1.
6. Konjugat ifølge et af kravene 2 til 5, hvor antistoffet eller antistoffragmentet er et cystein-manipuleret antistof.
7. Konjugat ifølge et af kravene 2 til 6, hvor lægemiddelladningen (p) af lægemidler (D) i forhold til antistof (Ab) er et helt tal fra 1 til ca. 8.
8. Konjugat ifølge krav 7, hvor p er 1, 2, 3 eller 4.
9. Sammensætning omfattende en blanding af lægemiddelkonjugatforbindel-ser ifølge et af kravene 2 til 8, hvor den gennemsnitlige lægemiddelladning pr. antistof i blandingen af antistof-lægemiddelkonjugatforbindelser er ca. 1 til ca. 8.
10. Konjugat ifølge et af kravene 2 til 8 eller sammensætning ifølge krav 9 til anvendelse inden for behandling.
11. Konjugat ifølge et af kravene 2 til 8 eller sammensætning ifølge krav 9 til anvendelse ved behandling afen proliferativ sygdom i et individ.
12. Konjugat eller sammensætning til anvendelse ifølge krav 11, hvor sygdommen er cancer.
13. Farmaceutisk sammensætning omfattende kongugatet ifølge et af kravene 2 til 8 eller sammensætningen ifølge krav 9, og et farmaceutisk acceptabelt fortyndingsmiddel, bære- eller hjælpestof.
14. Farmaceutisk sammensætning ifølge krav 13, yderligere omfattende en terapeutisk virksom mængde af et kemoterapeutisk middel.
15. Fremgangsmåde til fremstilling af et konjugat ifølge et af kravene 2 til 8, hvor fremgangsmåden omfatter et trin, hvor et cellebindingsstof reageres med forbindelse B som defineret i krav 1.
DK13780099.1T 2012-10-12 2013-10-11 Pyrrolobenzodiazepiner og konjugater deraf DK2906248T3 (da)

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US201261712924P 2012-10-12 2012-10-12
PCT/EP2013/071235 WO2014057073A1 (en) 2012-10-12 2013-10-11 Pyrrolobenzodiazepines and conjugates thereof

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US (1) US9415117B2 (da)
EP (2) EP2906248B1 (da)
JP (2) JP6367811B2 (da)
KR (3) KR102138220B1 (da)
CN (2) CN110256469B (da)
AU (1) AU2013328674B2 (da)
BR (1) BR112015008251B1 (da)
CA (2) CA2885315C (da)
CY (2) CY1121390T1 (da)
DK (2) DK2906248T3 (da)
ES (2) ES2713164T3 (da)
HK (1) HK1213183A1 (da)
HR (2) HRP20190366T1 (da)
HU (2) HUE052835T2 (da)
LT (2) LT2906248T (da)
MX (2) MX366303B (da)
NZ (2) NZ705910A (da)
PL (2) PL3470086T3 (da)
PT (2) PT3470086T (da)
RS (2) RS58203B1 (da)
SI (2) SI3470086T1 (da)
TR (1) TR201902494T4 (da)
WO (1) WO2014057073A1 (da)
ZA (1) ZA201501781B (da)

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