公开(公告)号：US11820758B2

公开(公告)日：2023-11-21

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 ,  A61K33/243 ,  A61K31/337 ,  A61K45/06

CPC classification number: C07D405/06 ,  C07D471/04 ,  A61K31/337 ,  A61K33/243 ,  A61K45/06

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：US09994524B2

公开(公告)日：2018-06-12

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: A61K31/403 ,  A61K31/165 ,  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：US09630954B2

公开(公告)日：2017-04-25

申请号：US14389759

申请日：2013-04-02

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: C07D207/08 ,  C07D401/04 ,  A61K31/4025 ,  A61K31/4439 ,  C07D407/12 ,  A61K31/343 ,  A61K31/40 ,  A61K31/403 ,  C07D409/12 ,  C07D207/06 ,  C07D209/86 ,  C07D209/88 ,  C07D307/91 ,  C07C251/86 ,  A61K31/165 ,  A61K31/381

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 ll-MHCII interaction. The compounds identified here open up new possibilities in the treatment of rheumatoid arthritis.

公开(公告)号：US20150073030A1

公开(公告)日：2015-03-12

申请号：US14389759

申请日：2013-04-02

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: C07D407/12 ,  C07D209/86 ,  C07D207/08

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 ll-MHCII interaction. The compounds identified here open up new possibilities in the treatment of rheumatoid arthritis.

Abstract translation: 特异于人类胶原II型的T细胞是可能的自身抗原之一，在HLA-DR4的背景下对类风湿性关节炎的发展起着至关重要的作用。 与HLA-DR4类HLA-DR4等位基因MHC相连的T细胞受体（TCR）和II型胶原之间的蛋白质 - 蛋白质相互作用因此可能代表了抗风湿性关节炎新药的发展的目标。 使用计算虚拟筛选技术，已经鉴定出干扰TCR /胶原II-MHCII相互作用的药理活性分子家族。 这里鉴定的化合物在治疗类风湿性关节炎方面开辟了新的可能性。