HRP20210126T1 - Pirolobenzodiazepini i njihovi konjugati - Google Patents

Pirolobenzodiazepini i njihovi konjugati Download PDF

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Publication number
HRP20210126T1
HRP20210126T1 HRP20210126TT HRP20210126T HRP20210126T1 HR P20210126 T1 HRP20210126 T1 HR P20210126T1 HR P20210126T T HRP20210126T T HR P20210126TT HR P20210126 T HRP20210126 T HR P20210126T HR P20210126 T1 HRP20210126 T1 HR P20210126T1
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Croatia
Prior art keywords
antibody
conjugate
conjugate according
preparation
drug
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HRP20210126TT
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English (en)
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Philip Wilson Howard
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Medimmune Limited
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Publication of HRP20210126T1 publication Critical patent/HRP20210126T1/hr

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    • 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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Cell Biology (AREA)
  • Oncology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Toxicology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Claims (14)

1. Spoj, naznačen time, da je A: [image] i njegove soli i njegovi solvati.
2. Konjugat, naznačen time, da ima formulu KonjA: [image] u kojoj CBA predstavlja sredstvo za vezanje stanice.
3. Konjugat prema patentnom zahtjevu 2, naznačen time, da se kod sredstva za vezanje stanice radi o protutijelu ili fragmentu protutijela za antigen koji je povezan s tumorom.
4. Konjugat prema patentnom zahtjevu 3, naznačen time, da protutijelo ili fragment protutijela je jedno protutijelo koje se veže na jedan ili više antigena povezanih s tumorom ili na receptore stanične površine koji su odabrani od (1) do (88): (1) BMPR1B; (2) E16; (3) STEAP1; (4) 0772P; (5) MPF; (6) Napi3b; (7) Sema 5b; (8) PSCA hlg; (9) ETBR; (10) MSG783; (11) STEAP2; (12) TrpM4; (13) CRIPTO; (14) CD21; (15) CD79b; (16) FcRH2; (17) HER2; (18) NCA; (19) MDP; (20) IL20R-alfa; (21) Brevikan; (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) EGFRvIII; (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) specifični antigeni matične stanice; (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/Mindin, meta za tumor prostate – Mindin/RG-1; (70) B7-H4 – VTCN1; (71) PTK7; (72) CD37; (73) CD138 – SDC1; (74) CD74; (75) Klaudini - 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) Aneksin A1 – ANXA1; (88) V-CAM (CD106) – VCAM1.
5. Konjugat prema bilo kojem od patentnih zahtjeva 2 do 4, naznačen time, da protutijelo ili fragment protutijela je protutijelo modificirano cisteinskim inženjeringom.
6. Konjugat prema bilo kojem od patentnih zahtjeva 2 do 5, naznačen time, da opterećenost lijekom (p) od lijekova (D) prema protutijelu (Ab), iznosi cijeli broj od 1 do oko 8.
7. Konjugat prema patentnom zahtjevu 6, naznačen time, da p je 1, 2, 3 ili 4.
8. Pripravak, naznačen time, da obuhvaća mješavinu spojeva lijeka i konjugata u skladu s bilo kojim od zahtjeva 2 do 7, pri čemu prosječna opterećenost lijekom po protutijelu u mješavini spojeva konjugata protutijelo-lijek, iznosi od oko 1 do oko 8.
9. Konjugat prema bilo kojem od patentnih zahtjeva 2 do 7, ili pripravak prema patentnom zahtjevu 8, naznačen time, da je za uporabu u liječenju.
10. Konjugat prema bilo kojem od patentnih zahtjeva 2 do 7, ili pripravak prema patentnom zahtjevu 8, naznačen time, da je za uporabu u liječenju proliferativne bolesti kod pojedinca.
11. Konjugat ili pripravak za uporabu prema patentnom zahtjevu 10, naznačen time, da bolest jest rak.
12. Farmaceutski pripravak, naznačen time, da sadrži konjugat u skladu s bilo kojim od patentnih zahtjeva 2 do 7, ili pripravak u skladu s patentnim zahtjevom 8, te farmaceutski prihvatljiv razrjeđivač, nosač ili pomoćnu tvar.
13. Farmaceutski pripravak prema patentnom zahtjevu 12, naznačen time, da dodatno sadrži terapijski učinkovitu količinu kemoterapijskog sredstva.
14. Postupak proizvodnje konjugata u skladu s bilo kojim od patentnih zahtjeva 2 do 7, naznačen time, da postupak obuhvaća korak reakcije sredstva za vezanje stanice sa spojem A koji je definiran u patentnom zahtjevu 1.
HRP20210126TT 2012-10-12 2021-01-22 Pirolobenzodiazepini i njihovi konjugati HRP20210126T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261712924P 2012-10-12 2012-10-12
EP18187765.5A EP3470086B1 (en) 2012-10-12 2013-10-11 Pyrrolobenzodiazepines and conjugates thereof

Publications (1)

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HRP20210126T1 true HRP20210126T1 (hr) 2021-03-19

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HRP20190366TT HRP20190366T1 (hr) 2012-10-12 2019-02-26 Pirolobenzodiazepini i njihovi konjugati
HRP20210126TT HRP20210126T1 (hr) 2012-10-12 2021-01-22 Pirolobenzodiazepini i njihovi konjugati

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US (1) US9415117B2 (hr)
EP (2) EP3470086B1 (hr)
JP (2) JP6367811B2 (hr)
KR (3) KR102138220B1 (hr)
CN (2) CN110256469B (hr)
AU (1) AU2013328674B2 (hr)
BR (1) BR112015008251B1 (hr)
CA (2) CA2885315C (hr)
CY (2) CY1121390T1 (hr)
DK (2) DK2906248T3 (hr)
ES (2) ES2713164T3 (hr)
HK (1) HK1213183A1 (hr)
HR (2) HRP20190366T1 (hr)
HU (2) HUE052835T2 (hr)
LT (2) LT2906248T (hr)
MX (2) MX362004B (hr)
NZ (2) NZ705910A (hr)
PL (2) PL3470086T3 (hr)
PT (2) PT3470086T (hr)
RS (2) RS58203B1 (hr)
SI (2) SI3470086T1 (hr)
TR (1) TR201902494T4 (hr)
WO (1) WO2014057073A1 (hr)
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