ME02055B - Pirolobenzodiazepini i njihovi konjugati - Google Patents

Pirolobenzodiazepini i njihovi konjugati

Info

Publication number
ME02055B
ME02055B MEP-2015-27A MEP201527A ME02055B ME 02055 B ME02055 B ME 02055B ME P201527 A MEP201527 A ME P201527A ME 02055 B ME02055 B ME 02055B
Authority
ME
Montenegro
Prior art keywords
antibody
conjugate
conjugate according
drug
binding agent
Prior art date
Application number
MEP-2015-27A
Other languages
English (en)
Inventor
Philip Wilson Howard
Original Assignee
Medimmune Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Medimmune Ltd filed Critical Medimmune Ltd
Publication of ME02055B publication Critical patent/ME02055B/me

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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
    • A61K47/6835—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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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
    • A61K47/68035—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a pyrrolobenzodiazepine
    • 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
    • A61K47/6891—Pre-targeting systems involving an antibody for targeting specific cells
    • 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
    • A61P39/00—General protective or antinoxious agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/582—Recycling of unreacted starting or intermediate materials

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

Claims (15)

1. Jedinjenje B: i njegove soli i solvati.
2. Konjugat formule ConjB: gde CBA predstavlja agens za vezivanje ćelija.
3. Konjugat prema patentnom zahtevu 2, gde je agens za vezivanje ćelija antitelo ili njegov aktivni fragment.
4. Konjugat prema patentnom zahtevu 3, gde su antitelo ili fragment antitela antitelo ili fragment antitela za tumorsk-pridruženi antigen.
5. Konjugat prema patentnom zahtevu 3, gde su antitelo ili fragment antitela antitelo koje se vezuje na jedan ili više tumor-pridruženih antigena ili površinskih ćelijskih receptora, izabranih od (1)-(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) 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) EGFRvIII;(46) CD33;(47) CD 19;(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) Antigeni specifični za matične ćelije;(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 – Mindin/RG-1 meta prostatnog tumora;(70) B7-H4 - VTCN1;(71) PTK7;(72) CD37;(73) CD138 - SDC1;(74) CD74;(75) Claudini - CLs;(76) EGFR;(77) Her3;(78) RON - MST1 R;(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.
6. Konjugat prema bilo kom od patentnih zahteva 2 do 5, gde su antitelo ili fragment antitela cisteinsko genetski modifikovano antitelo.
7. Konjugat prema bilo kom od patentnih zahteva 2 do 6, gde je unos leka (p) od lekova (D) na antitela (Ab) ceo broj od 1 do 8.
8. Konjugat prema patentom zahtevu 7, gde p iznosi 1, 2, 3 ili 4.
9. Kompozicija koji sadrži smesu konjugovanih jedinjenja leka prema bilo kom od patentnih zahteva 2 do 8, gde je prosečan unos leka po antitelu u smesi konjugata antitela i leka od otprilike 1 do otprilike 8.
10. Konjugat prema bilo kom od patentnih zahteva 2 do 8 ili kompozicija prema patentnom zahtevu 9, za upotrebu u terapiji.
11. Konjugat prema bilo kom od patentnih zahteva 2 do 8 ili kompozicija prema patentnom zahtevu 9, za upotrebu u lečenju proliferativnih bolesti kod pacijenta.
12. Konjugat namijenjen upotrebi prema patentnom zahtevu 11, gde bolest je karcinom.
13. Farmaceutska kompozicija koja sadrži konjugat prema bilo kom od patentnih zahteva 2 do 8 ili kompozicija prema patentnom zahtevu 9 i farmaceutski prihvatljiv razređivač, nosač ili eksipijent.
14. Farmaceutska kompozicija prema patentnom zahtevu 13 koja dalje sadrži terapeutski delotvornu količinu hemoterapeutsog agensa.
15. Postupak dobijanja konjugata prema bilo kom od patentnih zahteva 2 do 8, koji postupak uključuje korak reakcije agensa za vezivanje ćelija sa jedinjenjem B, kako je definisano u patentnom zahtevu 1. Strana 1
MEP-2015-27A 2012-10-12 2013-10-11 Pirolobenzodiazepini i njihovi konjugati ME02055B (me)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261712928P 2012-10-12 2012-10-12
EP13780100.7A EP2766048B1 (en) 2012-10-12 2013-10-11 Pyrrolobenzodiazepines and conjugates thereof
PCT/EP2013/071236 WO2014057074A1 (en) 2012-10-12 2013-10-11 Pyrrolobenzodiazepines and conjugates thereof

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ME02055B true ME02055B (me) 2015-05-20

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MEP-2019-172A ME03486B (me) 2012-10-12 2013-10-11 Pirolobenzodiazepini i njihovi konjugati

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US (6) US9889207B2 (me)
EP (2) EP2766048B1 (me)
JP (2) JP5993093B2 (me)
KR (2) KR101819404B1 (me)
CN (2) CN109134599A (me)
AU (2) AU2013328580B2 (me)
CA (2) CA2885340C (me)
CY (2) CY1116192T1 (me)
DK (2) DK2766048T3 (me)
EA (2) EA035405B1 (me)
ES (2) ES2530968T3 (me)
HR (2) HRP20150201T1 (me)
HU (1) HUE045435T2 (me)
IL (2) IL237940A (me)
LT (1) LT2839860T (me)
ME (2) ME02055B (me)
MX (2) MX338711B (me)
PL (2) PL2839860T3 (me)
PT (2) PT2766048E (me)
RS (2) RS53818B1 (me)
SI (2) SI2766048T1 (me)
SM (2) SMT201900431T1 (me)
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WO (1) WO2014057074A1 (me)

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