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    22.
    发明专利
    未知

    公开(公告)号：BRPI0500889A

    公开(公告)日：2005-11-01

    申请号：BRPI0500889

    申请日：2005-03-21

    Applicant: SERVIER LAB

    Inventor： NANTEUIL GUILLAUME DE ,  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 ,  A61K31/407

    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.

    4-Oxo-4,6,7,8-tetrahydrop-pyrrolofÄ1,2-aÜpyrazine-6-carbox-amide compounds, a process for their preparation and pharmaceutical compositions containingthem.
    23.
    发明专利
    4-Oxo-4,6,7,8-tetrahydrop-pyrrolofÄ1,2-aÜpyrazine-6-carbox-amide compounds, a process for their preparation and pharmaceutical compositions containingthem. 未知

    公开(公告)号：ZA200502316B

    公开(公告)日：2005-10-03

    申请号：ZA200502316

    申请日：2005-03-18

    Applicant: SERVIER LAB

    Inventor： NANTEUIL GUILLAUME DE ,  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 ,  A61K ,  C07C ,  C07D ,  A61P

    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.

    24.
    发明专利
    未知

    公开(公告)号：NO20051367D0

    公开(公告)日：2005-03-16

    申请号：NO20051367

    申请日：2005-03-16

    Applicant: SERVIER LAB

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

    IPC: A61K31/519 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D487/04 ,  C07D

    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.

    28.
    发明专利
    未知

    公开(公告)号：NO315468B1

    公开(公告)日：2003-09-08

    申请号：NO971861

    申请日：1997-04-23

    Applicant: SERVIER LAB

    Inventor： WIERZBICKI MICHEL ,  BOUSSARD MARIE-FRANCOISE ,  VERBEUREN TONY ,  VALLEZ MARIE-ODILE

    IPC: A61K31/35 ,  A61K31/352 ,  A61K31/36 ,  A61P9/00 ,  A61P43/00 ,  C07D311/30 ,  C07D407/12

    Abstract: Diosmetin acids and esters of formula (I), their enantiomers and salts are new. R2, R4, R6 = H, 1-5C alkyl, CH2CH=CH2, CH2C(CH3)=CH2, CH2CH=C(CH3)2, CH2CH2CH(CH3)2, 2,2-dimethyl-1,3-dioxolan-4-ylmethyl, CH2CH(OH)CH2OH or ACOOR8; A = 1-3C hydrocarbon chain (optionally substituted by methyl or OH); R8 = H or 1-5C alkyl; R3, R5 = H, CH2CH2CH3, CH2CH=CH2, CH2CH(CH3)2, C(CH3)2CH=CH2, C(CH3)2CH2CH3, CH2C(CH3)=CH2 or COCH3 R1, R7 = H, CH2CH2CH3, CH2CH=CH2, CH2CH=C(CH3)2, tert.-butyl, CH2CH2CH(CH3)CH3, CH2C(CH3)=CH2 or CH2CH(CH3)2 provided that if one or two of R2, R4, and R6 = ACOOR8, then at least one of the remaining R1-R7 is not H.

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