公开(公告)号：CA3079865A1

公开(公告)日：2019-05-02

申请号：CA3079865

申请日：2018-10-26

Applicant: INST NAT SANTE RECH MED ,  UNIV GRENOBLE ALPES ,  COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIE ALTERNATIVES ,  SERVIER LAB

Inventor： ANDRIEUX ANNIE ,  MOUTIN MARIE-JOSE ,  BOSC CHRISTOPHE ,  AILLAUD CHRYSTELLE ,  PERIS LETICIA ,  DELAGRANGE PHILIPPE

IPC: C12N15/113 ,  A61K31/713 ,  C12Q1/37

Abstract: Using chemical proteomics with a potent unique irreversible inhibitor, inventors found that major brain tubulin carboxypeptidase (TCP)is a complex of vasohibin-1 (VASH1) with the Small Vasohibin-Binding Protein (SVBP). VASH1 and its homologue vasohibin-2 (VASH2), when complexed with SVBP, exhibit robust and specific Tyr/Phe carboxypeptidase activity on microtubules. Accordingly inventors are the first to identify the enzymatic activity of vasohibin and vasohibin/SVBP complex. Knock down of vasohibins or SVBP in cultured neurons results in a marked reduction of tyrosinated a-tubulin levels and onset of severe differentiation defects. Furthermore, knock down of vasohibins disrupts neuronal migration in developing mouse neocortex. These results establish vasohibin/SVBP complexes as TCP enzymes. Accordingly, the present invention relates methods and pharmaceutical compositions for treating tubulin carboxypeptidases (TCP) associated diseases such as neurological disorders and cardiovascular diseases with an inhibitor of activity or expression of Vasohibinor Vasohibin/SVBP complex.

公开(公告)号：UA94827C2

公开(公告)日：2011-06-10

申请号：UAA201000634

申请日：2008-07-01

Applicant: SERVIER LAB

Inventor： YOUS SAID ,  ETTAOUSSI MOHAMED ,  CABAOUNI AHMED ,  BERTHELOT PASCAL ,  SPEDDING MICHAEL ,  DELAGRANGE PHILIPPE ,  CAIGNARD DANIEL-HENRI ,  MILLAN MARK

IPC: A61K31/165 ,  C07C233/18 ,  A61P25/00 ,  C07C233/60

公开(公告)号：CA2593618C

公开(公告)日：2010-08-24

申请号：CA2593618

申请日：2007-06-29

Applicant: SERVIER LAB

Inventor： YOUS SAID ,  PERES BASILE ,  SABAOUNI AHMED ,  BERTHELOT PASCAL ,  SPEDDING MICHAEL ,  DELAGRANGE PHILIPPE ,  CAIGNARD DANIEL-HENRI ,  MILLAN MARK

IPC: C07C233/18 ,  A61K31/165 ,  A61P25/00 ,  C07C231/06 ,  C07C231/20

Abstract: Composés de formule (I) : (voir formule I) Médicaments.

公开(公告)号：FR2903102B1

公开(公告)日：2010-08-13

申请号：FR0605917

申请日：2006-06-30

Applicant: SERVIER LAB

Inventor： YOUS SAID ,  PERES BASILE ,  SABAOUNI AHMED ,  BERTHELOT PASCAL ,  SPEDDING MICHAEL ,  DELAGRANGE PHILIPPE ,  CAIGNARD DANIEL HENRI ,  MILLAN MARK

IPC: C07C235/34 ,  A61K31/165 ,  A61P9/00 ,  A61P15/00 ,  A61P25/00 ,  A61P35/00 ,  A61P37/02

公开(公告)号：UA91645C2

公开(公告)日：2010-08-10

申请号：UAA200904632

申请日：2007-10-17

Applicant: SERVIER LAB

Inventor： MARCHAND PASCAL ,  BABONNEAU VINCENT ,  PIESSARD SYLVIE ,  DUFLOS MURIEL ,  BOUTIN JEAN ALBERT ,  AUDINOT VALERIE ,  DELAGRANGE PHILIPPE ,  GAIGNARD DANIEL-HENRI

IPC: C07D209/32 ,  A61K31/454 ,  A61P3/04 ,  A61P15/00 ,  A61P25/00 ,  A61P35/00

公开(公告)号：CA2744178A1

公开(公告)日：2010-06-03

申请号：CA2744178

申请日：2009-11-24

Applicant: SERVIER LAB

Inventor： SUZENET FRANCK ,  GUILLAUMET GERALD ,  JEANTY MATTHIEU ,  DELAGRANGE PHILIPPE ,  CAIGNARD DANIEL-HENRI ,  SPEDDING MICHAEL

IPC: C07D209/20 ,  A61K31/4045 ,  A61P3/00 ,  A61P9/00 ,  A61P15/00 ,  A61P25/00 ,  A61P35/00

Abstract: Composés de formule (I) : dans laquelle : R représente un groupement alkyle, cycloalkyle, ou cycloalkylalkyle,

公开(公告)号：DK1873140T3

公开(公告)日：2010-01-11

申请号：DK07290819

申请日：2007-06-29

Applicant: SERVIER LAB

Inventor： YOUS SAID ,  PERES BASILE ,  SABAOUNI AHMED ,  BERTHELOT PASCAL ,  SPEDDING MICHAEL ,  DELAGRANGE PHILIPPE ,  CAIGNARD DANIEL-HENRI ,  MILLAN MARK

IPC: C07C233/18 ,  A61K31/165 ,  A61P9/00 ,  A61P15/00 ,  A61P25/00 ,  A61P35/00 ,  A61P37/02

Abstract: N-[3-Hydroxy-2-(7-methoxy-1-naphthyl)propyl] propanamide (I), its enantiomers and base addition salts, are new. N-[3-Hydroxy-2-(7-methoxy-1-naphthyl)propyl] propanamide of formula (I), its enantiomers and base addition salts, are new. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Hypnotic; Tranquilizer; Antidepressant; Cardiovascular-Gen; Gastrointestinal-Gen; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Nootropic; Antimigraine; Neuroprotective; Cerebroprotective; Contraceptive; Endocrine-Gen; Immunomodulator; Cytostatic. MECHANISM OF ACTION : Melatonin receptor binder. The ability of (I) to bind with melatonin was tested. The results showed that N-[3-hydroxy-2-(7-methoxy-1-naphthyl)propyl] propanamide exhibited an inhibition constant value of 1.4 nM and 3.2 nM to bind with melatonin receptors MT 1 and MT 2, respectively.

公开(公告)号：FR2918369B1

公开(公告)日：2009-08-28

申请号：FR0704746

申请日：2007-07-02

Applicant: SERVIER LAB

Inventor： YOUS SAID ,  ETTAOUSSI MOHAMED ,  SABAOUNI AHMED ,  BERTHELOT PASCAL ,  SPEDDING MICHAEL ,  DELAGRANGE PHILIPPE ,  CAIGNARD DANIEL HENRI ,  MILLAN MARK

IPC: C07C233/22 ,  A61K31/165 ,  A61P1/00 ,  A61P9/00 ,  A61P15/00 ,  A61P25/00 ,  A61P35/00 ,  C07C231/14

公开(公告)号：NO20091779A

公开(公告)日：2009-05-06

申请号：NO20091779

申请日：2009-05-06

Applicant: SERVIER LAB

Inventor： AUDINOT VALERIE ,  BOUTIN JEAN ALBERT ,  MARCHAND PASCAL ,  BADONNEAU VINCENT ,  PIESSARD SYLVIE ,  DUFLOS MURIEL ,  DELAGRANGE PHILIPPE ,  GAIGNARD DANIEL-HENRI

IPC: C07D209/32

CPC classification number: C07D209/14

公开(公告)号：MX2009004006A

公开(公告)日：2009-04-28

申请号：MX2009004006

申请日：2007-10-17

Applicant: SERVIER LAB

Inventor： DELAGRANGE PHILIPPE ,  AUDINOT VALERIE ,  MARCHAND PASCAL ,  BABONNEAU VINCENT ,  PIESSARD SYLVIE ,  DUFLOS MURIEL ,  BOUTIN JEAN ALBERT ,  CAIGNARD DANIEL-HENERI

IPC: C07D209/32 ,  A61K31/454 ,  A61P3/04 ,  A61P15/00 ,  A61P25/00 ,  A61P35/00

Abstract: Los compuestos de fórmula (I) en la cual: R1 es un grupo alquilo, cicloalquilo o cicloalquilalquilo, R2 y R3 forman junto con el átomo de nitrógeno el cual están unidos, un heterociclo que comprende 5 a 8 miembros en el anillo, y n es de 2 a 6; medicamentos. (ver fórmula I).