公开(公告)号：US20170190680A1

公开(公告)日：2017-07-06

申请号：US15314851

申请日：2015-05-29

Applicant: IEO - Istituto Europeo di Oncologia S.r.l.

Inventor： Paola VIANELLO ,  Mario VARASI ,  Ciro MERCURIO ,  Anna CAPPA ,  Giuseppe MERONI ,  Manuela VILLA ,  Antonello MAI ,  Sergio VALENTE

IPC: C07D295/155 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/445 ,  A61K31/421 ,  A61K45/06 ,  C07D211/34

CPC classification number: C07D295/155 ,  A61K31/421 ,  A61K31/445 ,  A61K31/495 ,  A61K31/5375 ,  A61K45/06 ,  C07D211/14 ,  C07D211/34 ,  C07D241/04 ,  C07D263/22 ,  C07D265/30

Abstract: The present disclosure relates to cyclopropyl compounds of general formula (I), wherein R1, and R2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy.

公开(公告)号：US20220339163A1

公开(公告)日：2022-10-27

申请号：US17616070

申请日：2020-06-03

Applicant: IFOM - FONDAZIONE ISTITUTO FIRC DI ONCOLOGIA MOLECOLARE ,  IEO - ISTITUTO EUROPEO DI ONCOLOGIA S.R.L.

Inventor： Sebastiano PASQUALATO ,  Maurizio PASI ,  Raffaella AMICI ,  Mario VARASI ,  Ciro MERCURIO ,  Luca SARTORI ,  Simona POLO ,  Elena MASPERO ,  Giovanni FAGA'

IPC: A61K31/5517 ,  C07D223/28 ,  C07D267/20 ,  C07D243/38 ,  C07D487/04 ,  C07D495/04 ,  A61P35/00 ,  A61K31/55 ,  A61K31/553 ,  A61K31/5513

Abstract: The present invention relates to tricyclic derivatives of formula (I), which are useful as inhibitors of HECT-domain-containing E3 ligases, in particular NEDD4. The present invention also refers to pharmaceutical compositions comprising compounds of formula (I), to their medical use and to their process of preparation.

公开(公告)号：US20200299303A1

公开(公告)日：2020-09-24

申请号：US16722554

申请日：2019-12-20

Applicant: Istituto Europeo di Oncologia S.r.l.

Inventor： Paola VIANELLO ,  Alessia ROMUSSI ,  Anna CAPPA ,  Paolo TRIFIRO' ,  Mario VARASI ,  Luca SARTORI ,  Ciro MERCURIO

IPC: C07D495/04 ,  A61P3/04 ,  A61P35/00

Abstract: The present invention relates to imidazole derivatives, wherein A, R, R1, and R2 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy.

公开(公告)号：US20200289463A1

公开(公告)日：2020-09-17

申请号：US16640030

申请日：2018-08-17

Applicant: Istituto Europeo di Oncologia S.r.l.

Inventor： Mario VARASI ,  Anna CAPPA ,  Paola VIANELLO ,  Loris MORETTI ,  Luca SARTORI ,  Ciro MERCURIO

IPC: A61K31/407 ,  A61K45/06 ,  C07D495/04

Abstract: The present application relates to compounds of formula (I), wherein A, R, R1, and R2 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy.

公开(公告)号：US20190152987A1

公开(公告)日：2019-05-23

申请号：US16301875

申请日：2017-05-18

Applicant: Istituto Europeo di Oncologia S.r.l.

Inventor： Paola VIANELLO ,  Alessia ROMUSSI ,  Anna CAPPA ,  Paolo TRIFIRO' ,  Mario VARASI ,  Luca SARTORI ,  Ciro MERCURIO

IPC: C07D495/04 ,  A61P3/04 ,  A61P35/00

CPC classification number: C07D495/04 ,  A61P3/04 ,  A61P35/00

Abstract: The present invention relates to imidazole derivatives of Formula (I), wherein A, R, R1, and R2 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy.

公开(公告)号：US20170260197A1

公开(公告)日：2017-09-14

申请号：US15508816

申请日：2015-09-04

Applicant: ISTITUTO EUROPEO DI ONCOLOGIA S.R.L.

Inventor： Paola VIANELLO ,  Luca SARTORI ,  Mario VARASI ,  Ciro MERCURIO ,  Elisa ZAGARRI ,  Anna CAPPA ,  Alessia ROMUSSI ,  Manuela VILLA ,  Giuseppe MERONI ,  Loris MORETTI

IPC: C07D495/04 ,  A61K31/407 ,  A61K31/55 ,  A61K31/5377 ,  A61K31/4439 ,  C07D519/00 ,  A61K31/438 ,  A61K31/454 ,  A61K31/496

CPC classification number: C07D495/04 ,  A61K31/407 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/55 ,  C07D519/00

Abstract: The present application relates to thienopyrrole derivatives, compounds of Formulas (I) and (Ia), wherein R, R1, R2 and R3 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy. The compounds of the application can be useful for inhibiting KDM1 and the prevention and/or treatment of cancer, infectious disease, or a disease characterized by aberration of cellular energy metabolism, e.g., obesity.