公开(公告)号：US20180186796A1

公开(公告)日：2018-07-05

申请号：US15520768

申请日：2015-10-29

Applicant: LEAD DISCOVERY SIENA S.R.L.

Inventor： Maurizio BOTTA ,  Adriano ANGELUCCI ,  Elena DREASSI ,  Silvia SCHENONE ,  Cristina TINTORI ,  Giulia VIGNAROLI

IPC: C07D487/04 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/519

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06

Abstract: The present invention refers to 4-amino-substituted pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine derivatives of formula I and IV able to target the Src family kinases (SFKs) such as Src, Fyn and Hck tyrosine kinases as well as Abl tyrosine kinase and uses and method of preparation thereof. In particular, the compounds of the invention are for use in the treatment and/or prevention of cancer, such as neuroblastoma (NB) or glioblastoma multiforme (GBM) or for use in the treatment and/or prevention of neurodegenerative diseases such as taupathies.

公开(公告)号：US20170304235A1

公开(公告)日：2017-10-26

申请号：US15517764

申请日：2015-10-09

Applicant: LEAD DISCOVERY SIENA S.R.L.

Inventor： Maurizio BOTTA ,  Giorgio MACCARI ,  Stefania SANFILIPPO ,  Filomena DE LUCA ,  Jean-Denis DOCQUIER ,  Davide DEODATO

IPC: A61K31/155 ,  C07C279/12 ,  C07C279/04 ,  C08K5/31 ,  C07C279/24 ,  C07C2601/02

CPC classification number: A61K31/155 ,  A61K31/17 ,  A61K45/06 ,  C07C279/04 ,  C07C279/12 ,  C07C279/24 ,  C07C2601/02 ,  C08K5/31 ,  Y02A50/473 ,  A61K2300/00

Abstract: The present invention relates to linear guanidine derivatives, methods of preparation, uses and pharmaceutical compositions thereof. The compounds of Formulas 1 or 2 exhibit high antimicrobial activity against Gram positive and Gram negative bacteria.