公开(公告)号：US20240059690A1

公开(公告)日：2024-02-22

申请号：US17999421

申请日：2021-05-20

Applicant: ESTEVE PHARMACEUTICALS, S.A.

Inventor： Ariadna FERNANDEZ-DONIS ,  José-Luis DÍAZ-FERNÁNDEZ ,  Carmen ALMANSA-ROSALES ,  Mónica GARCIA-LOPEZ ,  Joan-Carles FERNANDEZ-COLLADO ,  Jordi GONZALEZ-GARCIA ,  Maria GARRIDO-MARTINEZ

IPC: C07D487/04 ,  A61P29/02

CPC classification number: C07D487/04 ,  A61P29/02

Abstract: The present invention relates to pyrazolopyrimidine derivatives having dual pharmacological activity towards both the α2δ subunit of the voltage-gated calcium channel and the sigma-1 (σ1) receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

公开(公告)号：US20210395249A1

公开(公告)日：2021-12-23

申请号：US17288934

申请日：2019-11-04

Applicant: ESTEVE PHARMACEUTICALS, S.A.

Inventor： Carmen ALMANSA-ROSALES ,  Félix CUEVAG-CORDOBÉS

IPC: C07D471/04

Abstract: The present invention relates to new compounds of formula (I) that show dual activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels, and the noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.

公开(公告)号：US20190284195A1

公开(公告)日：2019-09-19

申请号：US16464736

申请日：2017-11-30

Applicant: ESTEVE PHARMACEUTICALS, S.A.

Inventor： Marina VIRGILI-BERNADO ,  Monica ALONSO-XALMA ,  Carmen ALMANSA-ROSALES

IPC: C07D487/04

Abstract: The present invention relates to ortho substituted phenylpyrazolo- and pyrrolo-pyridazine derivatives having dual pharmacological activity towards both the α2δ subunit, in particular the α2δ-1 subunit, of the voltage-gated calcium channel and the μ-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

公开(公告)号：US20190127357A1

公开(公告)日：2019-05-02

申请号：US16090403

申请日：2017-04-12

Applicant: ESTEVE PHARMACEUTICALS , S.A.

Inventor： Pilar GOYA ,  Antoni TORRENS-JOVER ,  Carmen ALMANSA-ROSALES ,  Joser-Luis DIAZ-FERNÁNDEZ ,  Ana-Maria CAAMAÑO-MOURE

IPC: C07D413/10 ,  C07D413/14 ,  C07D401/14 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14 ,  C07D405/14 ,  C07D417/14

CPC classification number: C07D413/10 ,  A61P25/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to arylamide derivatives having dual pharmacological activity towards both the α2δ subunit, in particular the α2δ-1 subunit, of the voltage-gated calcium channel and the μ-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

公开(公告)号：US20210395254A1

公开(公告)日：2021-12-23

申请号：US17289761

申请日：2019-11-04

Applicant: ESTEVE PHARMACEUTICALS, S.A.

Inventor： Félix CUEVAS-CORDOBÉS ,  Carmen ALMANSA-ROSALES

IPC: C07D487/04 ,  C07D471/04

Abstract: The present invention relates to new compounds of general formula (I) that show dual activity towards subunit α2δ of voltage-gated calcium channels (VGCC), especially α2δ-1 subunit of voltage-gated calcium channels, and noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions composing them, and to their use as medicaments.

公开(公告)号：US20200087291A1

公开(公告)日：2020-03-19

申请号：US16470568

申请日：2017-12-20

Applicant: ESTEVE PHARMACEUTICALS, S.A.

Inventor： Carmen ALMANSA-ROSALES ,  Susana YENES-MÍNGUEZ ,  Marina VIRGILI-BERNADO ,  Monica ALONSO-XALMA

IPC: C07D409/12 ,  C07D407/12 ,  C07D401/12 ,  C07D417/12

Abstract: The present invention relates to new compounds of formula (I): showing great affinity and activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels or dual activity towards subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels, and the noradrenaline transporter (NET).

公开(公告)号：US20190276415A1

公开(公告)日：2019-09-12

申请号：US16426024

申请日：2019-05-30

Applicant: ESTEVE PHARMACEUTICALS, S.A.

Inventor： Félix CUEVAS-CORDOBÉS ,  Carmen ALMANSA-ROSALES ,  Monica GARCIA-LOPEZ

IPC: C07D249/06 ,  C07D401/12 ,  C07D401/06 ,  C07D487/08 ,  C07D487/04 ,  C07D401/14 ,  C07D403/06 ,  C07D401/04 ,  C07D233/64 ,  C07D231/12 ,  C07D249/04

Abstract: The present invention relates to compounds having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opiod receptor and more particularly to piperazine compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

公开(公告)号：US20200002283A1

公开(公告)日：2020-01-02

申请号：US16307549

申请日：2017-06-26

Applicant: ESTEVE PHARMACEUTICALS, S.A.

Inventor： Carmen ALMANSA-ROSALES ,  Susana YENES-MÍNGUEZ ,  José-Luis DÍAZ-FERNÁNDEZ ,  Antonio David RODRIGUEZ-GARRIDO

IPC: C07D231/12 ,  C07D401/04 ,  C07D403/04 ,  C07D401/06 ,  C07D413/06 ,  C07D417/12

Abstract: The present invention relates to pyrazole derivatives having pharmacological activity towards the α2δ subunit, in particular the α2δ-1 subunit, of the voltage-gated calcium channel, in particular having dual pharmacological activity towards both the α2δ subunit, in particular the α2δ-1 subunit, of the voltage-gated calcium channel and the μ-opioid receptor. The present invention also relates to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

公开(公告)号：US20190241544A1

公开(公告)日：2019-08-08

申请号：US16301508

申请日：2017-05-19

Applicant: ESTEVE PHARMACEUTICALS, S.A.

Inventor： Monica GARCIA-LOPEZ ,  Carmen ALMANSA-ROSALES ,  Ana Virginia LLORENTE-FERNANDEZ ,  Ute CHRISTMANN ,  Sergio RODRIGUEZ ESCRICH

IPC: C07D405/04 ,  A61P29/00 ,  C07D405/14 ,  C07D487/04

Abstract: The present invention relates to tetrahydropyran and thiopyran derivatives having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

公开(公告)号：US20200377464A1

公开(公告)日：2020-12-03

申请号：US16649179

申请日：2018-10-16

Applicant: ESTEVE PHARMACEUTICALS, S.A.

Inventor： Carmen ALMANSA-ROSALES ,  Félix CUEVAS-CORDOBÉS

IPC: C07D239/48 ,  C07D333/20 ,  C07D409/12 ,  C07D413/12 ,  C07C235/56 ,  C07D213/82 ,  C07D211/58 ,  C07D239/34 ,  C07D213/75

Abstract: The present invention relates to new compounds of formula (I) that show great affinity and activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels or dual activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels, and the noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.