MONOMETHYL AURISTATIN E CONJUGATE FOR PREPARING A COMPOSITION FOR TREATING PROSTATE CANCER Russian patent published in 2020 - IPC C07D207/09 A61K31/40 A61K47/55 A61P35/00 

Abstract RU 2729192 C1

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a conjugate of formula (I) for treating tumors expressing PSMA, including a PSMA ligand with a linker and an anti-tumor preparation MMAE, a composition for preparing a lyophilizate based thereon, dosage form for therapy and inhibition of growth of prostate tumor expressing PSMA, obtained by lyophilisation of said composition, solution for infusions or injections containing such a dosage form, reduced with a solvent containing ethyl alcohol 95 % and polysorbate 80 at weight ratio (30–60):(70–40), respectively.

EFFECT: technical result of claimed group of inventions is high affinity and selectivity of action of disclosed conjugates in relation to cells expressing PSMA.

12 cl, 15 dwg, 27 tbl, 7 ex

Similar patents RU2729192C1

Title Year Author Number
CONJUGATE OF A FLUORESCENT DYE WITH A PEPTIDE SUBSTANCE WHICH CONTAINS A PSMA-BINDING LIGAND BASED ON A UREA DERIVATIVE FOR VISUALIZING CELLS EXPRESSING PSMA, A METHOD FOR PRODUCTION THEREOF AND USE THEREOF 2019
  • Machulkin Aleksej Eduardovich
  • Uspenskaya Anastasiya Alekseevna
  • Ber Anton Petrovich
  • Petrov Stanislav Aleksandrovich
  • Yamansarov Emil Yulaevich
  • Finko Aleksandr Valerevich
  • Krasnovskaya Olga Olegovna
  • Nimenko Ekaterina Alekseevna
  • Zyk Nikolaj Yurevich
  • Ivanenkov Yan Andreevich
  • Skvortsov Dmitrij Aleksandrovich
  • Erofeev Aleksandr Sergeevich
  • Gorelkin Petr Vladimirovich
  • Beloglazkina Elena Kimovna
  • Khazanova Elena Sergeevna
  • Mazhuga Aleksandr Georgievich
RU2713151C1
COMPOUND FOR DIAGNOSING TUMOURS EXPRESSING PSMA AND COMPOSITION BASED THEREON 2019
  • Machulkin Aleksej Eduardovich
  • Mazhuga Aleksandr Georgievich
  • Ber Anton Petrovich
  • Petrov Stanislav Aleksandrovich
  • Ivanenkov Yan Andreevich
  • Skvortsov Dmitrij Aleksandrovich
  • Beloglazkina Elena Kimovna
  • Egorova Bajirta Vladimirovna
  • Kalmykova Taisiya Petrovna
RU2730507C1
PEPTIDE AGENT COMPRISING A PSMA-BINDING LIGAND BASED ON A UREA DERIVATIVE, A METHOD FOR PRODUCTION THEREOF AND USE THEREOF FOR PREPARING A CONJUGATE WITH A DRUG AND DIAGNOSTIC AGENT 2018
  • Machulkin Aleksej Eduardovich
  • Uspenskaya Anastasiya Alekseevna
  • Ber Anton Petrovich
  • Petrov Stanislav Aleksandrovich
  • Saltykova Irina Vladimirovna
  • Ivanenkov Yan Andreevich
  • Skvortsov Dmitrij Aleksandrovich
  • Erofeev Aleksandr Sergeevich
  • Gorelkin Petr Vladimirovich
  • Beloglazkina Elena Kimovna
  • Belov Evgenij Yurevich
  • Khazanova Elena Sergeevna
  • Mazhuga Aleksandr Georgievich
RU2697519C1
METHOD OF OBTAINING PSMA-TARGET COMPOUND COMPLEX BASED ON UREA Lu-PS-161 AND COMPLEX 2023
  • Tolmachev Vladimir Maksimilianovich
  • Orlova Anna Markovna
  • Zelchan Roman Vladimirovich
  • Bodenko Vitalina Vasilevna
  • Iusubov Mekhman Suleimanovich
  • Larkina Mariia Sergeevna
  • Plotnikov Evgenii Vladimirovich
  • Iuldasheva Feruza Sherzod Kizi
  • Stasiuk Elena Sergeevna
  • Ianovich Gleb Evgenevich
  • Seitova Kamila
  • Fominykh Anastasiia Sergeevna
  • Tretiakova Mariia Sergeevna
  • Prach Anastasiia Aleksandrovna
  • Bezverkhnyaya Ekaterina Aleksandrovna
  • Machulkin Aleksej Eduardovich
  • Petrov Stanislav Aleksandrovich
  • Beloglazkina Elena Kimovna
  • Mazhuga Aleksandr Georgievich
  • Chernov Vladimir Ivanovich
RU2808636C1
LYOPHILISATE BASED ON PROSTATE-SPECIFIC MEMBRANE ANTIGEN (PSMA) LIGANDS FOR PREPARING A RADIOPHARMACEUTICAL COMPOSITION IN FORM OF SOLUTION FOR INJECTIONS FOR TREATING PROSTATE CANCER, RADIOPHARMACEUTICAL COMPOSITION BASED ON IT FOR TREATING PROSTATE CANCER AND METHOD FOR PREPARING RADIOPHARMACEUTICAL COMPOSITION 2023
  • Tulskaia Tatiana Ivanovna
  • Kodina Galina Evgenevna
  • Silaeva Natalia Vladimirovna
  • Klementeva Olga Evgenevna
  • Larenkov Anton Alekseevich
  • Rakhimov Marat Galievich
  • Lunev Aleksandr Sergeevich
RU2817970C1
MONOMETHYLVALINE COMPOUNDS CAPABLE OF FORMING CONJUGATES WITH LIGANDS 2004
  • Doronina Svetlana O.
  • Senter Piter D.
  • Toki Brajan Eh.
  • Ehbens Allen Dzh.
  • Klajn Toni Bet
  • Polakis Pol
  • Slivkovski Mark Ks.
  • Spenser Sjuzan D.
RU2448117C2
PEPTIDE COMPOUND CAPABLE OF BINDING WITH PSMA, METHOD FOR PRODUCTION AND USE THEREOF 2021
  • Petrov Stanislav Aleksandrovich
  • Machulkin Aleksej Eduardovich
  • Larenkov Anton Alekseevich
  • Uspenskaya Anastasiya Alekseevna
  • Nimenko Ekaterina Alekseevna
  • Zyk Nikolaj Yurevich
  • Skvortsov Dmitrij Aleksandrovich
  • Shafikov Radik Radikovich
  • Beloglazkina Elena Kimovna
  • Mazhuga Aleksandr Georgievich
RU2823164C2
COMPLEX OF UREA DERIVATIVE WITH Tc RADIONUCLIDE LABEL FOR DIAGNOSIS OF TUMORS EXPRESSING PROSTATE-SPECIFIC MEMBRANE ANTIGEN, AND METHOD FOR PRODUCTION THEREOF 2023
  • Tolmachev Vladimir Maksimilianovich
  • Orlova Anna Markovna
  • Bezverkhnyaya Ekaterina Aleksandrovna
  • Panajotis Kanellopulos
  • Ajman Abuzajed
  • Ulrika Rozenstrem
  • Chernov Vladimir Ivanovich
  • Zelchan Roman Vladimirovich
  • Rybina Anastasiya Nikolaevna
  • Medvedeva Anna Aleksandrovna
  • Bragina Olga Dmitrievna
  • Larkina Mariya Sergeevna
  • Varvashenya Ruslan Nikolaevich
RU2825402C1
PSMA-TARGET COMPOUND AND ITS COMPLEX WITH RADIONUCLIDES FOR THERANOSTICS OF TUMOR EXPRESSING PSMA 2022
  • Tolmachev Vladimir Maksimilianovich
  • Orlova Anna Markovna
  • Seitova Kamila
  • Bodenko Vitalina Vasilevna
  • Fanny Lundmark
  • Ayman Abouzayed
  • Ulrika Rosenstrem
RU2803734C1
PHOTOSENSITIZER FOR PHOTODYNAMIC THERAPY OF PROSTATE CANCER AND METHOD FR MANUFACTURING THEREOF 2018
  • Grin Mikhail Aleksandrovich
  • Suvorov Nikita Vladimirovich
  • Machulkin Aleksej Eduardovich
  • Plotnikova Ekaterina Aleksandrovna
  • Yakubovskaya Raisa Ivanovna
  • Mazhuga Aleksandr Georgievich
  • Mironov Andrej Fedorovich
  • Filonenko Elena Vyacheslavovna
RU2670087C1

RU 2 729 192 C1

Authors

Machulkin Aleksej Eduardovich

Uspenskaya Anastasiya Alekseevna

Khazanova Elena Sergeevna

Rybalov Aleksej Alekseevich

Pchelintsev Svetozar Olegovich

Petrov Stanislav Aleksandrovich

Ber Anton Petrovich

Zyk Nikolaj Yurevich

Ivanenkov Yan Andreevich

Skvortsov Dmitrij Aleksandrovich

Erofeev Aleksandr Sergeevich

Gorelkin Petr Vladimirovich

Beloglazkina Elena Kimovna

Mazhuga Aleksandr Georgievich

Dates

2020-08-05Published

2019-11-22Filed