05-07-2018 дата публикации
Номер: US20180185510A1
Автор:
BERNDT Sandra,
Cancho Grande Yolanda,
FISCHER Melanie,
FRANZ Juergen,
GLÜCK Julian Marius,
Greven Simone,
Gritzan Uwe,
LERCHEN Hans-Georg,
Mahlert Christoph,
MÄRSCH Stephan,
Paz Pedro,
Rebstock Anne-Sophie,
STELTE-LUDWIG Beatrix,
Weber Ernst,
WITTROCK Sven
Принадлежит:
The present application relates to novel binder drug conjugates (ADCs), to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for the treatment and/or prophylaxis of diseases and to the use of these ADCs for preparing medicaments for treatment and/or prophylaxis of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures. 2. Conjugate according to claim 1 , where A represents —C(═O)—.3. Conjugate according to claim 1 , where Rrepresents —H claim 1 , -L-#1 claim 1 , —COOH claim 1 , —C(═O)—NHNH claim 1 , —(CH)NH claim 1 , —C(═O)—NZ″(CH)NHor —C(═O)—NZ″CHCOOH claim 1 , where Z″ represents —H or —NH.4. Conjugate according to claim 1 ,{'sup': 2', '4, 'where Rand Rrepresent —H or'}{'sup': 2', '4', '11', '11, 'sub': 2', '2, 'claim-text': {'sup': '11', 'sub': 2', '2', '1-4, 'where Rrepresents —H, —COOH, F, methyl, —CHF, —Omethyl, —CHOH, —C(═O)—O—(C-alkyl) or OH.'}, 'where Rand Rtogether (with formation of a pyrrolidine ring) represent —CHR—CH— or —CH—CHR—;'}5. Conjugate according to claim 1 ,{'sup': 3', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4, 'sub': 1-3', '1-3', '1-10', '1-10', 'n', '2', '2, 'claim-text': where', 'n represents 0, 1 or 2,', {'sup': '4', 'sub': 1-3', '1-3', '1-3, 'Yrepresents —H, phenyl which is optionally mono- or polysubstituted by halogen, C-alkyl or fluoro-C-alkyl, or represents alkyl which may be substituted by —OH, —COOH, and/or —NH—C(═O)—C-alkyl.'}], 'where Rrepresents -L-#1 or represents a phenyl group which may be mono- or polysubstituted by halogen, C-alkyl or fluoro-C-alkyl, or represents a C-alkyl group or fluoro-C-alkyl group which may optionally be substituted by —OY, —SY, —O—C(═O)—Y, —O—C(═O)—NH—Y, —NH—C(═O)—Y, —NH—C(═O)—NH—Y, —S(O)—Y, —S(═O)—NH—Y, —NH—Yor —N(Y),'}7. Conjugate according to where the substituent ...
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