公开(公告)号：US20210147395A1

公开(公告)日：2021-05-20

申请号：US17045028

申请日：2019-04-02

Applicant: CONSIGLIO NAZIONALE DELLE RICERCHE ,  MOLIPHARMA S.R.L.

Inventor： Maria Cristina DE ROSA ,  Davide PIROLLI ,  Giovanni SCAMBIA ,  Daniela GALLO ,  Marco PETRILLO ,  Marta DE DONATO ,  Benedetta RIGHINO

IPC: C07D405/06 ,  C07D471/04

Abstract: The mitotic kinases regulating the dynamics of centrosomes and the functions of the mitotic spindle are potential targets for the antitumour therapy. In the present invention some molecules with inhibitory activity on NEK6 have been identified. The present invention relates to such molecules and to the compositions including them for use as inhibitors of NEK6 in a method of treatment of tumours both in monotherapy and in combinations with other drugs.

公开(公告)号：US20170204059A1

公开(公告)日：2017-07-20

申请号：US15469411

申请日：2017-03-24

Applicant: CONSIGLIO NAZIONALE DELLE RICERCHE ,  UNIVERSITÀ CATTOLICA DEL SACRO CUORE

Inventor： Maria Cristina DE ROSA ,  Francesco RIA ,  Bruno GIARDINA ,  Gianfranco FERRACCIOLI ,  Davide PIROLLI ,  Chiara NICOLO'

IPC: C07D209/86

CPC classification number: C07D209/86 ,  A61K31/165 ,  A61K31/343 ,  A61K31/381 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4439 ,  C07C251/86 ,  C07C2603/18 ,  C07D207/06 ,  C07D207/08 ,  C07D209/88 ,  C07D307/91 ,  C07D401/04 ,  C07D407/12 ,  C07D409/12

Abstract: The T cells specific to human collagen type II, one of the possible autoantigens, have a crucial role in the development of rheumatoid arthritis in the context of HLA-DR4. The protein-protein interactions between the T cell receptor (TCR) and the type II collagen linked to the allele MHC of class II HLA-DR4 may thus represent the target for the development of new drugs against rheumatoid arthritis. Using computational virtual screening techniques, families of pharmacologically active molecules have been identified that interfere with the TCR/collagen II-MHCII interaction. The compounds identified here open up new possibilities in the treatment of rheumatoid arthritis.

公开(公告)号：US20240425508A1

公开(公告)日：2024-12-26

申请号：US18728048

申请日：2023-01-11

Applicant: ISTITUTI CLINICI SCIENTIFICI MAUGERI SPA SB ,  CONSIGLIO NAZIONALE DELLE RICERCHE ,  INRCA

Inventor： Carlo GAETANO ,  Sandra ATLANTE ,  Maria Cristina DE ROSA ,  Davide PIROLLI ,  Antonella FARSETTI ,  Marco MALAVOLTA

IPC: C07D473/06 ,  A61K8/49 ,  A61K31/522 ,  A61P43/00 ,  A61Q19/08 ,  C07C273/18 ,  C07D239/545

Abstract: A compound of formula (I) or pharmaceutically acceptable salts or hydrates thereof: wherein R is chosen from phenyl, a 6-membered heteroaryl group, cyclohexyl, a 5-membered heteroaryl group; a bicyclo [3.1.0] hexanyl group; a C2-C5 alkynyl group; and a cubanyl group; wherein R1 and R2, independently, are chosen from H; C1-C6 alkyl (optionally substituted with one or more halogens); C1-C6 alkyl-S(O)n—; CO2H (or C1-C6 alkyl esters thereof or C1-C6 alkyl amides thereof); halogen; C1-C6 alkoxy; CN; NO2; and NR7R8; wherein R7 and R8, independently, each represent H, C1-C6 alkyl, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, arylsulphonyl, heteroarylsulphonyl, heterocyclosulphonyl, arylcarbonyl, heteroarylcarbonyl, heterocyclocarbonyl, or C1-C6 alkylsulphonyl, or R7, R8 and the nitrogen to which they are attached form a 5 or 6 membered heterocyclic ring (such as morpholine or piperidine); and wherein n represents 0-2.