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    ASOCIACION ENTRE UN ANTIATEROTROMBOTICO Y UN INHIBIDOR DE LA ENZIMA DE CONVERSION DE LA ANGIOTENSINA
    3.
    发明专利
    ASOCIACION ENTRE UN ANTIATEROTROMBOTICO Y UN INHIBIDOR DE LA ENZIMA DE CONVERSION DE LA ANGIOTENSINA 未知

    公开(公告)号：CO6020018A1

    公开(公告)日：2009-03-31

    申请号：CO08095778

    申请日：2008-09-11

    Applicant: SERVIER LAB

    Inventor： VERBEUREN TONY ,  SANSILVESTRI-MOREL PATRICIA ,  RUPIN ALAIN ,  VALLEZ MARIE ODILE ,  FRATACCI MARIE-DOMINIQUE ,  LEROND LAURENCE ,  LAVIELLE GILBERT

    IPC: A61K31/14 ,  A61K31/145 ,  A61P7/02 ,  A61P9/12

    Abstract: Asociación del compuesto (A) de la fórmula (I) opcionalmente bajo la forma de isómero óptico o de una de sus sales farmacéuticamente aceptable y de un inhibidor de la encima de conversión de la angiotensina o de una de sus sales farmacéuticamente aceptable: Asociación según la reivindicación 1, caracterizada porque el conpuesto (A) es terutroban. Asociación según una cualquiera de las reivindicaciones 1 ó 2, caracterizada porque el compuesto (A) está bajo la forma de una sal sódica. Asociación según una cualquiera de las reivindicaciones 1, 2 ó 3, caracterizada porque el inhibidor de la enzima de conversión de la angiotensina es perindopril opcionalrnente bajo la forma de su metabolito activo el perindoprilato, ramipril opcionalmente bajo la forma de su metabolito activo el ramiprilato, enalapril opcioualmente bajo la forma de su metabolito activo el enalaprilato, captopril, lisinopril, delapril, fosinopril, quinapril, espirapril, imidapril, trandolapril opcionalmente bajo la forma de su metabolito activo el trandolaprilato, benazepril, cilazapril, temocapril, alacepril, ceronapril, moveltipril o moexipril, así como sus sales de adición de un ácido o una base farmacéuticamente aceptable. Asociación según una cualquiera de las reivindicaciones 1 a 4, caracterizada porque el inhibidor de la enzima de conversión de la angiotensina es perindopril de la fórmula (B) así como sus sales de adición de un ácido o de una base farmacéuticamente aceptable. Asociación según la reivindicación 5, caracterizada porque el perindopril de la fórmula (B) está bajo la forma de una sal de terc-butilamina o de arginina. Composición farmacéutica que contiene como principio activo una asociación según una cualquiera de las reivindicaciones 1 a 6, en combinación con uno o múltiples excipientes o vehículos inertes farmacéuticamente aceptables.

    9.
    发明专利
    未知

    公开(公告)号：FR2867780B1

    公开(公告)日：2006-05-19

    申请号：FR0402841

    申请日：2004-03-19

    Applicant: SERVIER LAB

    Inventor： DE NANTEUIL GUILLAUME ,  GLOANEC PHILIPPE ,  PARMENTIER JEAN GILLES ,  BENOIST ALAIN ,  RUPIN ALAIN ,  VALLEZ MARIE ODILE ,  VERBEUREN TONY

    IPC: C07D487/04 ,  A61K31/4985 ,  A61K31/519 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D207/12 ,  C07D241/08

    Abstract: 4-Oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrazine-6-carboxamide compounds (I) are new. 4-Oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrazine-6-carboxamide compounds of formula (I) are new. A : 1-oxidopyridyl substituted by the remainder of the molecule in any one of the positions 2, 3 and 4; m, n : 1 - 3; R 1H or linear or branched (1-6C)alkyl; R 2, R 3hydrogen, halogen, linear or branched (1-6C)alkyl, hydroxy, linear or branched (1-6C)acyloxy or linear or branched (1-6C)alkoxy; R 2+R 33-6C cycloalkane; R 4, R 5H; R 4+R 5benzo ring; Ar : phenyl, biphenylyl or naphthyl (optionally substituted by at least one of T 1) or 5 - 12-membered mono- or bi-cyclic aromatic group (containing 1 - 3 heteroatoms selected from O, N or S; and optionally substituted by at least one of T 1); and T 1halo, linear or branched (1-6C)alkyl (optionally substituted by hydroxy, carboxy or carbamoyl (optionally mono- or di-substituted by linear or branched (1-6C)alkyl, linear or branched (1-6C)alkoxy, hydroxy, trihalo-(1-6C)alkyl (in which the alkyl moiety is linear or branched), amino (optionally mono- or di-substituted by linear or branched (1-6C)alkyl, carboxymethoxy or carbamoylmethoxy (optionally mono- or di-N-substituted by linear or branched (1-6C)alkyl, hydroxy-(1-6C)alkyl (in which the alkyl moiety is linear or branched), alkoxyalkyl (in which the alkoxy and alkyl moieties are each linear or branched 1-6C) or pyridylalkyl (in which the alkyl moiety is linear or branched 1-6C)))). The configuration of the asymmetric centre at the alpha position with respect to the amide is (S). [Image] ACTIVITY : Antianginal; Thrombolytic; Cardiant; Vasotropic; Cardiovascular-Gen.; Antiarteriosclerotic. MECHANISM OF ACTION : Thrombin inhibitors. The inhibitory activity of 3-{[2,2-difluoro-2-(1-oxido-2-pyridyl)ethyl]amino}-4-oxo-N-[2-(2-oxo-2-{[2-(2-pyridyl)ethyl]amino}ethoxy)benzyl]-4,6,7,8-tetrahydropyrrolo[1,2-a]pyrazine-6-carboxamide hydrochloride (A) was evaluated on human thrombin. The purified human fibrinogen (4 mM) was added to thrombin (0.7 nM) that had previously been incubated optionally with the inhibitor to be tested (20[deg]C, 10 minutes). Inhibitors, enzymes and substrates were diluted in the same buffer (0.01 mM phosphate buffer, pH 7.4, containing sodium chloride (0.12 M) and bovine serum albumin (0.05%)) and then distributed on a polystyrene microtitre plate in a volume of 50 mu l. The fibrin formed by the thrombin was measured using a spectrophotometer at 405 nm after 10 - 15 minutes reaction at 20[deg]C. The IC 50 value of (A) was found to be 1.4 nM.

    10.
    发明专利
    未知

    公开(公告)号：FR2867780A1

    公开(公告)日：2005-09-23

    申请号：FR0402841

    申请日：2004-03-19

    Applicant: SERVIER LAB

    Inventor： DE NANTEUIL GUILLAUME ,  GLOANEC PHILIPPE ,  PARMENTIER JEAN GILLES ,  BENOIST ALAIN ,  RUPIN ALAIN ,  VALLEZ MARIE ODILE ,  VERBEUREN TONY

    IPC: A61K31/519 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D487/04 ,  A61K31/4985

    Abstract: 4-Oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrazine-6-carboxamide compounds (I) are new. 4-Oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrazine-6-carboxamide compounds of formula (I) are new. A : 1-oxidopyridyl substituted by the remainder of the molecule in any one of the positions 2, 3 and 4; m, n : 1 - 3; R 1H or linear or branched (1-6C)alkyl; R 2, R 3hydrogen, halogen, linear or branched (1-6C)alkyl, hydroxy, linear or branched (1-6C)acyloxy or linear or branched (1-6C)alkoxy; R 2+R 33-6C cycloalkane; R 4, R 5H; R 4+R 5benzo ring; Ar : phenyl, biphenylyl or naphthyl (optionally substituted by at least one of T 1) or 5 - 12-membered mono- or bi-cyclic aromatic group (containing 1 - 3 heteroatoms selected from O, N or S; and optionally substituted by at least one of T 1); and T 1halo, linear or branched (1-6C)alkyl (optionally substituted by hydroxy, carboxy or carbamoyl (optionally mono- or di-substituted by linear or branched (1-6C)alkyl, linear or branched (1-6C)alkoxy, hydroxy, trihalo-(1-6C)alkyl (in which the alkyl moiety is linear or branched), amino (optionally mono- or di-substituted by linear or branched (1-6C)alkyl, carboxymethoxy or carbamoylmethoxy (optionally mono- or di-N-substituted by linear or branched (1-6C)alkyl, hydroxy-(1-6C)alkyl (in which the alkyl moiety is linear or branched), alkoxyalkyl (in which the alkoxy and alkyl moieties are each linear or branched 1-6C) or pyridylalkyl (in which the alkyl moiety is linear or branched 1-6C)))). The configuration of the asymmetric centre at the alpha position with respect to the amide is (S). [Image] ACTIVITY : Antianginal; Thrombolytic; Cardiant; Vasotropic; Cardiovascular-Gen.; Antiarteriosclerotic. MECHANISM OF ACTION : Thrombin inhibitors. The inhibitory activity of 3-{[2,2-difluoro-2-(1-oxido-2-pyridyl)ethyl]amino}-4-oxo-N-[2-(2-oxo-2-{[2-(2-pyridyl)ethyl]amino}ethoxy)benzyl]-4,6,7,8-tetrahydropyrrolo[1,2-a]pyrazine-6-carboxamide hydrochloride (A) was evaluated on human thrombin. The purified human fibrinogen (4 mM) was added to thrombin (0.7 nM) that had previously been incubated optionally with the inhibitor to be tested (20[deg]C, 10 minutes). Inhibitors, enzymes and substrates were diluted in the same buffer (0.01 mM phosphate buffer, pH 7.4, containing sodium chloride (0.12 M) and bovine serum albumin (0.05%)) and then distributed on a polystyrene microtitre plate in a volume of 50 mu l. The fibrin formed by the thrombin was measured using a spectrophotometer at 405 nm after 10 - 15 minutes reaction at 20[deg]C. The IC 50 value of (A) was found to be 1.4 nM.

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