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1. (WO2017004025) CONJUGATES OF CYSTEINE ENGINEERED ANTIBODIES
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/004025 International Application No.: PCT/US2016/039796
Publication Date: 05.01.2017 International Filing Date: 28.06.2016
IPC:
A61P 35/00 (2006.01) ,C07D 487/04 (2006.01) ,C07D 519/00 (2006.01) ,C07K 16/28 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
519
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/ or C07D455/257
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
16
Immunoglobulins, e.g. monoclonal or polyclonal antibodies
18
against material from animals or humans
28
against receptors, cell surface antigens or cell surface determinants
Applicants:
IMMUNOGEN, INC. [US/US]; 830 Winter Street Waltham, MA 02451, US
Inventors:
YODER, Nicholas, C.; US
BAI, Chen; US
MILLER, Michael, Louis; US
Agent:
LU, Yu; US
Priority Data:
62/186,25429.06.2015US
62/338,24518.05.2016US
Title (EN) CONJUGATES OF CYSTEINE ENGINEERED ANTIBODIES
(FR) CONJUGUÉS D'ANTICORPS À CYSTÉINE MODIFIÉE
Abstract:
(EN) The invention relates to novel cell-binding agent-cytotoxic agent conjugates, wherein the cell-binding agent (CBA) is covalently linked to the cytotoxic agent through an engineered Cys, such as an engineered Cys in the heavy chain CH3 domain, at a position corresponds to the EU/OU numbering position 442 (or C442) on an antibody CBA. The invention also provides methods of preparing the conjugates of the present invention. The invention further provides composition and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the conjugates of the invention.
(FR) L'invention concerne de nouveaux conjugués constitués d'un agent de liaison cellulaire et d'un agent cytotoxique, où l'agent de liaison cellulaire (CBA) est lié de manière covalente à l'agent cytotoxique par l'intermédiaire d'une Cys modifiée, telle qu'une Cys modifiée au niveau du domaine CH3 de la chaîne lourde, à une position correspondant à la position 442 en numérotation EU/OU (ou C442) sur un CBA de type anticorps. L'invention porte également sur des méthodes de préparation des conjugués de la présente invention. L'invention concerne, en outre, une composition et des méthodes utilisables pour inhiber une croissance cellulaire anormale ou traiter un trouble prolifératif chez le mammifère à l'aide des conjugués de l'invention.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
AU2016285929CN107708810KR1020180021176CA2988806EP3313845