Abstract: The present invention relates to bendamustine derivatives and related compounds of formula (VII), (VIII) and (IX), and medical uses thereof in particular in cancer therapy.
Type:
Grant
Filed:
June 14, 2013
Date of Patent:
January 7, 2020
Assignee:
SYNBIAS PHARMA AG
Inventors:
Helmut Schickaneder, Christian Schickaneder, Armin Buschauer, Stefan Huber, Michael Limmert, Günther Bernhardt, Mathias Lubbe, Harald Hofmeier
Abstract: The present invention relates to a method for the production of a rapamycin derivative of formula (I), the method comprising the preparation of a 2-(tri-substituted silyl)oxyethyl triflate by reacting ethylene oxide and a tri-substituted silyl triflate, reaction of the resulting 2-(tri-substituted silyl)oxyethyl triflate with rapamycin in the presence of a molar excess of organic base, and deprotection to obtain the rapamycin derivative of compound (I).
Type:
Grant
Filed:
June 22, 2016
Date of Patent:
June 4, 2019
Assignee:
Synbias Pharma AG
Inventors:
Oleksandr Zabudkin, Christian Schickaneder, Iaroslav Matviienko, Volodymyr Sypchenko
Abstract: The present invention relates to bendamustine derivatives and related compounds of formula (VII), (VIII) and (IX), and medical uses thereof in particular in cancer therapy.
Abstract: The present invention is directed to crystalline vinorelbine monotartrate and its use for the prevention and treatment of cancer, particularly non-small cell lung cancer or breast cancer. The present invention also relates to a corresponding method for the manufacture of crystalline vinorelbine monotartrate.
Type:
Application
Filed:
March 9, 2016
Publication date:
March 28, 2019
Applicant:
SYNBIAS PHARMA AG
Inventors:
Oleksandr Zabudkin, Viktor Matviyenko, Vladimir Matha, Christian Schickaneder, Iaroslav Matviienko, Volodymyr Sypchenko
Abstract: The present invention relates to a method for the high yield production of the anticancer nucleoside clofarabine, the method comprising the preparation of 2-chloroadenosine by enzymatic transglycosylation between 2-chloroadenine and nucleosides, benzoylation, isomerization, sulfonate ester formation, fluorination, and deprotection.
Type:
Grant
Filed:
April 22, 2015
Date of Patent:
July 24, 2018
Assignee:
Synbias Pharma AG
Inventors:
Alexander Zabudkin, Victor Matvienko, Iaroslav Matviienko, Volodymyr Sypchenko
Abstract: The present invention relates to a method for the synthesis of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. iriniotecan), comprising: (a) preparing 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptotecin; and (b) selectively ethylating the compound of step (a) at the 7-position, thus resulting in the preparation of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin. The present invention is further directed to the use of 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. 7-des-ethyl-irinotecan) as intermediate in a method for the synthesis of irinotecan as described.
Abstract: The present invention relates to a method for the synthesis of 4-demethoxydaunorubicin (idarubicin) having the chemical structure of formula (I), which involves the demethylation of 3?-Prot-daunorubicin in the presence of a soft Lewis acid. The method of the present invention does not comprise cleavage of the glycosidic linkage at carbon C7, thus resulting in a faster synthesis cycle and an improved yield of the final product.
Type:
Grant
Filed:
April 29, 2011
Date of Patent:
September 30, 2014
Assignee:
Synbias Pharma AG
Inventors:
Alexander Zabudkin, Victor Matvienko, Alexey Matvyeyev