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    12.
    发明专利
    未知

    公开(公告)号：AT405550T

    公开(公告)日：2008-09-15

    申请号：AT06291219

    申请日：2006-07-27

    Applicant: SERVIER LAB

    Inventor： GOLDSTEIN SOLO ,  GUILLONNEAU CLAUDE ,  CHARTON YVES ,  LOCKHART BRIAN ,  LESTAGE PIERRE

    IPC: C07D213/65 ,  A61K31/44 ,  A61P25/16 ,  A61P25/26 ,  A61P25/28 ,  A61P25/30

    Abstract: 1-Pyridinyloxyalkyl-1-aminocyclopropane derivatives (I), their enantiomers, diastereoisomers and acid or base addition salts are new. 1-Pyridinyloxyalkyl-1-aminocyclopropane derivatives of formula (I), their enantiomers, diastereoisomers and acid or base addition salts are new. n : 1-6; R 1 and R 2hydrogen, 1-6C alkyl or aryl(1-6C)alkyl; R 3 and R 4hydrogen or 1-6C alkyl but not both hydrogen; R 5 and R 6hydrogen, 1-6C alkyl, halo, hydroxy, 1-6C alkoxy, cyano, nitro, 2-6C acyl, 1-6C alkoxycarbonyl, 1-6C trihaloalkyl, 1-6C trihaloalkoxy or amino, optionally substituted by 1 or 2 1-6C alkyl; and aryl : (bi)phenyl, naphthyl, di- or tetra-hydronaphthyl, indanyl or indenyl, each optionally substituted by one or more halo, 1-6C alkyl, hydroxy, cyano, nitro, 1-6C alkoxy, 2-7C acyl, 1-6C alkoxycarbonyl, 1-6C trihalo-alkyl or -alkoxy, or amino, optionally substituted by 1 or 2 1-6C alkyl. An independent claim is included for several preparations of (I). [Image] ACTIVITY : Nootropic; Neuroprotective; Antiparkinsonian; Neuroleptic; Tranquilizer; Analgesic. The compound racemic N-2-dimethyl-1-[(3-pyridinyloxy)methyl]cyclopropanamine hydrochloride (Ia) was tested by the method of Psychopharmacology, 91 (1987) 363 in which the time taken for an adult rat to recognize a young rat when encountering 2 hours after an initial meeting was measured. The difference in recognition times was 38 s for a rat treated with 10 mg/kg (intraperitoneal) of (Ia), indicating a significant improvement in memory. MECHANISM OF ACTION : Central nicotinergic alpha 4beta 2 receptors Ligand.

    13.
    发明专利
    未知

    公开(公告)号：FR2896800B1

    公开(公告)日：2008-04-11

    申请号：FR0600784

    申请日：2006-01-30

    Applicant: SERVIER LAB

    Inventor： GOLDSTEIN SOLO ,  GUILLONNEAU CLAUDE ,  CHARTON YVES ,  LOCKHART BRIAN ,  LESTAGE PIERRE

    IPC: C07D401/10 ,  A61K31/4418 ,  A61K31/4439 ,  A61P25/28 ,  A61P25/34 ,  A61P29/00 ,  C07D213/22 ,  C07D213/65 ,  C07D213/73 ,  C07D257/04 ,  C07D401/04

    Abstract: Compounds of formula (I): wherein: n represents an integer of from 1 to 6 inclusive, X represents an oxygen atom or an NR6 group, Y represents a carbon atom or a nitrogen atom, Z represents a carbon atom or a nitrogen atom, R1 and R2 represent a hydrogen atom or an alkyl or arylalkyl group, R3 and R4 represent a hydrogen atom or an alkyl group, R5 represents a hydrogen atom or an alkyl, halogen, hydroxy, alkoxy, cyano, nitro, acyl, alkoxycarbonyl, trihaloalkyl, trihaloalkoxy or optionally substituted amino group, R6 represents a hydrogen atom or an alkyl or arylalkyl group, Ra, Rb, Rc, Rd and Re are as defined in the description. Medicinal products containing the same which are useful as specific nicotinic ligands of α4&bgr;2 receptors.

    NEW POLYSUBSTITUTED 1,1-PYRIDYLAMINOCYCLOPROPANAMINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    14.
    发明专利
    NEW POLYSUBSTITUTED 1,1-PYRIDYLAMINOCYCLOPROPANAMINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知

    公开(公告)号：HK1098146A1

    公开(公告)日：2007-07-13

    申请号：HK07104587

    申请日：2007-04-30

    Applicant: SERVIER LAB

    Inventor： GOLDSTEIN SOLO ,  GUILLONNEAU CLAUDE ,  CHARTON YVES ,  LOCKHART BRIAN ,  LESTAGE PIERRE

    IPC: A61K20090101 ,  A61K31/44 ,  A61P20090101 ,  A61P25/00 ,  C07D20090101 ,  C07D213/74

    Abstract: 1-amino-1-pyridylaminoalkyl-cyclopropane derivatives (I) are new. 1-amino-1-pyridylaminoalkyl-cyclopropane derivatives of formula (I) are new n : 1-6; R 1, R 2 and R 7hydrogen, 1-6C linear or branched alkyl or arylalkyl; R 3 and R 4hydrogen or 1-6C linear or branched alkyl; R 5 and R 6hydrogen, 1-6C alkyl or alkoxy, halo, hydroxy, cyano, nitro, 2-6C linear or branched acyl, 1-6C alkoxycarbonyl, trihaloalkyl or trihaloalkoxy (all linear or branched), or amino, optionally substituted by 1 or 2 1-6C linear or branched alkyl; aryl : (bi)phenyl, naphthyl (optionally di- or tetra-hydro), indanyl or indenyl, each optionally substituted by one or more of halo, 1-6C alkyl or alkoxy, hydroxy, cyano, nitro, 2-7C acyl, 1-6C alkoxycarbonyl, trihaloalkyl or trihaloalkoxy, or amino, optionally substituted by 1 or 2 1-6C alkyl An independent claim is included for several methods for preparing (I). [Image] ACTIVITY : Nootropic; Neuroprotective; Neuroleptic; Antismoking; Analgesic; Antiparkinsonian. In the social recognition test in rats ( Psychopharmacology, 91 (1987) 363), unspecified (I) were active at 1-3 mg/kg, intraperitoneally, indicating a strong memory-improving effect. MECHANISM OF ACTION : (I) are specific ligands for the central alpha 4beta 2 nicotinic receptors. When tested by the method of Mol. Pharmacol., 39 (1990) 9 for displacement of tritiated cytisine from such receptors in rat brain, unspecified (I) had Ki about 1 nM.

    New polysubstituted 1,1-pyridylamino-cyclopropanamine compounds, a process for their preparation and pharmaceutical compositions containing them
    15.
    发明专利
    New polysubstituted 1,1-pyridylamino-cyclopropanamine compounds, a process for their preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：SG129412A1

    公开(公告)日：2007-02-26

    申请号：SG200604917

    申请日：2006-07-21

    Applicant: SERVIER LAB

    Inventor： GOLDSTEIN SOLO ,  GUILLONNEAU CLAUDE ,  CHARTON YVES ,  LOCKHART BRIAN ,  LESTAGE PIERRE

    IPC: A61K31/44 ,  A61P25/00 ,  C07D213/74

    Abstract: 1-amino-1-pyridylaminoalkyl-cyclopropane derivatives (I) are new. 1-amino-1-pyridylaminoalkyl-cyclopropane derivatives of formula (I) are new n : 1-6; R 1, R 2 and R 7hydrogen, 1-6C linear or branched alkyl or arylalkyl; R 3 and R 4hydrogen or 1-6C linear or branched alkyl; R 5 and R 6hydrogen, 1-6C alkyl or alkoxy, halo, hydroxy, cyano, nitro, 2-6C linear or branched acyl, 1-6C alkoxycarbonyl, trihaloalkyl or trihaloalkoxy (all linear or branched), or amino, optionally substituted by 1 or 2 1-6C linear or branched alkyl; aryl : (bi)phenyl, naphthyl (optionally di- or tetra-hydro), indanyl or indenyl, each optionally substituted by one or more of halo, 1-6C alkyl or alkoxy, hydroxy, cyano, nitro, 2-7C acyl, 1-6C alkoxycarbonyl, trihaloalkyl or trihaloalkoxy, or amino, optionally substituted by 1 or 2 1-6C alkyl An independent claim is included for several methods for preparing (I). [Image] ACTIVITY : Nootropic; Neuroprotective; Neuroleptic; Antismoking; Analgesic; Antiparkinsonian. In the social recognition test in rats ( Psychopharmacology, 91 (1987) 363), unspecified (I) were active at 1-3 mg/kg, intraperitoneally, indicating a strong memory-improving effect. MECHANISM OF ACTION : (I) are specific ligands for the central alpha 4beta 2 nicotinic receptors. When tested by the method of Mol. Pharmacol., 39 (1990) 9 for displacement of tritiated cytisine from such receptors in rat brain, unspecified (I) had Ki about 1 nM.

    New polysubstituted 1,1-pyridyloxycyclopropanamine compounds, a process for their preparation and pharmaceutical compositions containing them
    16.
    发明专利
    New polysubstituted 1,1-pyridyloxycyclopropanamine compounds, a process for their preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：AU2006203241A1

    公开(公告)日：2007-02-15

    申请号：AU2006203241

    申请日：2006-07-28

    Applicant: SERVIER LAB

    Inventor： CHARTON YVES ,  GUILLONNEAU CLAUDE ,  GOLDSTEIN SOLO ,  LESTAGE PIERRE ,  LOCKHART BRIAN

    IPC: C07D213/65 ,  A61K31/44 ,  A61P25/00 ,  A61P25/24 ,  A61P25/28

    Abstract: 1-Pyridinyloxyalkyl-1-aminocyclopropane derivatives (I), their enantiomers, diastereoisomers and acid or base addition salts are new. 1-Pyridinyloxyalkyl-1-aminocyclopropane derivatives of formula (I), their enantiomers, diastereoisomers and acid or base addition salts are new. n : 1-6; R 1 and R 2hydrogen, 1-6C alkyl or aryl(1-6C)alkyl; R 3 and R 4hydrogen or 1-6C alkyl but not both hydrogen; R 5 and R 6hydrogen, 1-6C alkyl, halo, hydroxy, 1-6C alkoxy, cyano, nitro, 2-6C acyl, 1-6C alkoxycarbonyl, 1-6C trihaloalkyl, 1-6C trihaloalkoxy or amino, optionally substituted by 1 or 2 1-6C alkyl; and aryl : (bi)phenyl, naphthyl, di- or tetra-hydronaphthyl, indanyl or indenyl, each optionally substituted by one or more halo, 1-6C alkyl, hydroxy, cyano, nitro, 1-6C alkoxy, 2-7C acyl, 1-6C alkoxycarbonyl, 1-6C trihalo-alkyl or -alkoxy, or amino, optionally substituted by 1 or 2 1-6C alkyl. An independent claim is included for several preparations of (I). [Image] ACTIVITY : Nootropic; Neuroprotective; Antiparkinsonian; Neuroleptic; Tranquilizer; Analgesic. The compound racemic N-2-dimethyl-1-[(3-pyridinyloxy)methyl]cyclopropanamine hydrochloride (Ia) was tested by the method of Psychopharmacology, 91 (1987) 363 in which the time taken for an adult rat to recognize a young rat when encountering 2 hours after an initial meeting was measured. The difference in recognition times was 38 s for a rat treated with 10 mg/kg (intraperitoneal) of (Ia), indicating a significant improvement in memory. MECHANISM OF ACTION : Central nicotinergic alpha 4beta 2 receptors Ligand.

    17.
    发明专利
    未知

    公开(公告)号：NO20063462L

    公开(公告)日：2007-01-29

    申请号：NO20063462

    申请日：2006-07-27

    Applicant: SERVIER LAB

    Inventor： LOCKHART BRIAN ,  LESTAGE PIERRE ,  GOLDSTEIN SOLO ,  GUILLONNEAU CLAUDE ,  CHARTON YVES

    IPC: C07D213/63 ,  A61K31/44 ,  A61P25/00 ,  C07D213/74

    Abstract: 1-amino-1-pyridylaminoalkyl-cyclopropane derivatives (I) are new. 1-amino-1-pyridylaminoalkyl-cyclopropane derivatives of formula (I) are new n : 1-6; R 1, R 2 and R 7hydrogen, 1-6C linear or branched alkyl or arylalkyl; R 3 and R 4hydrogen or 1-6C linear or branched alkyl; R 5 and R 6hydrogen, 1-6C alkyl or alkoxy, halo, hydroxy, cyano, nitro, 2-6C linear or branched acyl, 1-6C alkoxycarbonyl, trihaloalkyl or trihaloalkoxy (all linear or branched), or amino, optionally substituted by 1 or 2 1-6C linear or branched alkyl; aryl : (bi)phenyl, naphthyl (optionally di- or tetra-hydro), indanyl or indenyl, each optionally substituted by one or more of halo, 1-6C alkyl or alkoxy, hydroxy, cyano, nitro, 2-7C acyl, 1-6C alkoxycarbonyl, trihaloalkyl or trihaloalkoxy, or amino, optionally substituted by 1 or 2 1-6C alkyl An independent claim is included for several methods for preparing (I). [Image] ACTIVITY : Nootropic; Neuroprotective; Neuroleptic; Antismoking; Analgesic; Antiparkinsonian. In the social recognition test in rats ( Psychopharmacology, 91 (1987) 363), unspecified (I) were active at 1-3 mg/kg, intraperitoneally, indicating a strong memory-improving effect. MECHANISM OF ACTION : (I) are specific ligands for the central alpha 4beta 2 nicotinic receptors. When tested by the method of Mol. Pharmacol., 39 (1990) 9 for displacement of tritiated cytisine from such receptors in rat brain, unspecified (I) had Ki about 1 nM.

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