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    NUEVOS COMPUESTOS 1,1-PIRIDINILAMINOCICLOPROPANAMINAS POLISUSTITUIDAS, SU PROCEDIMIENTO DE PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN.
    41.
    发明专利
    NUEVOS COMPUESTOS 1,1-PIRIDINILAMINOCICLOPROPANAMINAS POLISUSTITUIDAS, SU PROCEDIMIENTO DE PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN. 未知

    公开(公告)号：ES2318700T3

    公开(公告)日：2009-05-01

    申请号：ES06291218

    申请日：2006-07-27

    Applicant: SERVIER LAB

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

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

    Abstract: Compuesto de fórmula (I): ** ver fórmula** donde n representa un número entero comprendido entre 1 y 6, ambos inclusive, R1 y R2, idénticos o diferentes, independientemente uno de otro, representan un átomo de hidrógeno o un grupo alquilo (C1-C6) lineal o ramificado o arilalquilo(C1-C6) lineal o ramificado, R 3 y R 4, idénticos o diferentes, independientemente uno de otro, representan un átomo de hidrógeno o un grupo alquilo (C1-C6) lineal o ramificado, R5 y R6, idénticos o diferentes, independientemente uno de otro, representan un átomo de hidrógeno o un grupo alquilo (C 1-C 6) lineal o ramificado, un halógeno, hidroxilo, alcoxilo(C 1-C 6) lineal o ramificado, ciano, nitro, acilo(C 2- C 6) lineal o ramificado, alcoxicarbonilo(C 1-C 6) lineal o ramificado, trihaloalquilo(C 1-C 6) lineal o ramificado, trihaloalcoxilo(C1-C6) lineal o ramificado o amino eventualmente sustituido con uno o dos grupos alquilo(C1- C6) lineales o ramificados, R 7 representa un átomo de hidrógeno o un grupo alquilo(C 1-C 6) lineal o ramificado o arilalquilo(C 1-C 6) lineal o ramificado, entendiéndose por grupo arilo un grupo fenilo, bifenilo, naftilo, dihidronaftilo, tetrahidronaftilo, indanilo e indenilo, estando cada uno de esos grupos eventualmente sustituidos con uno o varios grupos, idénticos o diferentes, seleccionados de entre halógeno, alquilo(C1-C6) lineal o ramificado, hidroxilo, ciano, nitro, alcoxilo(C1-C6) lineal o ramificado, acilo(C2-C7) lineal o ramificado, alcoxicarbonilo(C1-C6) lineal o ramificado, trihaloalquilo(C1-C6) lineal o ramificado, trihaloalcoxilo(C1-C6) lineal o ramificado y amino eventualmente sustituido con uno o dos grupos alquilo (C 1-C 6) lineales o ramificados, sus enantiómeros, diastéreoisómeros, así como sus sales de adición de un ácido o de una base farmacéuticamente aceptables.

    43.
    发明专利
    未知

    公开(公告)号：DE602005005456T2

    公开(公告)日：2009-04-09

    申请号：DE602005005456

    申请日：2005-02-18

    Applicant: SERVIER LAB

    Inventor： CASARA PATRICK ,  CHOLLET ANNE-MARIE ,  DHAINAUT ALAIN ,  BERT LIONEL ,  LESTAGE PIERRE ,  LOCKHART BRIAN

    IPC: A61K31/403 ,  A61P25/00 ,  C07D209/52 ,  C07D403/12

    Abstract: Azabicyclic derivatives (I) are new. Azabicyclic derivatives of formula (I) and their enantiomers, diastereoisomers or acid or base addition salts are new. ALK : alkylene, 2-6C alkenylene (contains 1-3 double bonds) or 2-6C alkynylene (contains 1-3 triple bonds); Y, Y 1> : H, halo, alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, SH, OH, perhaloalkyl, nitro, amino (optionally substituted by one or two alkyl), acyl of formula C(O)R1a, aminocarbonyl (optionally N-substituted by one or two alkyl), acylamino (optionally N-substituted by alkyl), alkoxycarbonyl, COOH, sulfo or CN; R1a : H or alkyl; X : O, S or NR; R : H or alkyl; W 1> : CN (only when X = O or NR), N(R 1>)Z 1>R 2>or Z 1>NR 1>R 2>; Z 1> : C(O), C(S), C(NR 4>), C(O)N(R 3>), C(S)N(R 3>), C(NR 4>)N(R 3>), C(O)O, C(S)O or S(O) r; r : 1 or 2; Z 2> : C(O), C(S), C(NR 4>), S(O) ror bond; R 1>-R 4> : alkyl, 3-6C alkenyl (contains 1-3 double bonds), 3-6C alkynyl (contains 1-3 triple bonds), cycloalkyl, heterocycloalkyl, aryl or heteroaryl (all optionally substituted), alkoxy or H; or R 1>+R 2>or R 2>+R 3> : heterocyclyl or heteroaryl (both optionally substituted); m, n : 0-2, where the sum of m+n is 2 or 3; and p, q : 0-2. alkyl = 1-6C unless specified; perhaloalkyl = 1-3C with 1-7 halogen; aryl = phenyl, naphthyl, indanyl, indenyl, dihydronaphthyl or tetrahydronaphthyl; cycloalkyl = 3-11 membered mono- or bi-cyclic ring system, optionally with 1 or 2 unsaturations; heterocyclyl = 4-11 membered mono- or bicyclic ring system optionally with 1 or 2 unsaturations and/or 1-4 heteroatoms from N, O and/or S; heteroaryl = 5-11 membered mono- or bicyclic ring system with 1-4 heteroatoms from N, O and/or S; for cycloalkyl, aryl, heteroaryl or heterocyclyl, 'optionally substituted' comprises 1-3 substituents from alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, halogen, OH, SH, perhaloalkyl, nitro, amino or aminocarbonyl (optionally substituted by 1 or 2 alkyl), C(O)R1a, NHC(O)R1a (optionally N-substituted by alkyl), alkoxycarbonyl, COOH, sulfo or CN; or aryl, heteroaryl, cycloalkyl, heterocyclyl or benzyl with one or two optional oxo substituents where possible; for alkyl, alkenyl or alkynyl, 'optionally substituted ' comprises one or two of alkylthio, alkylsulfinyl, alkylsulfonyl, alkoxy, halogen, OH, SH, nitro, amino, C(O)R1a, aminocarbonyl, NHC(O)R1a, alkoxycarbonyl, COOH, sulfo, CN or aryl, heteroaryl, cycloalkyl, heterocylyl or aryloxy (all optionally substituted). An independent claim is included for the preparation of (I). [Image] ACTIVITY : Nootropic; Neuroprotective; Anticonvulsant; Tranquilizer; Anorectic; Analgesic. MECHANISM OF ACTION : Histamine (H3) activator. The ability of (I) to activate histamine was tested in mice. The results showed that 4-(3-hexahydrocyclopenta[c]-pyrrol-2(1H)-ylpropoxy)benzonitrile oxalate exhibited the percentage increase of N-methylhistamine in brain of 92%.

    POLYSUBSTITUTED 1,1-PYRIDINYLOXYCYCLOPROPANAMINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    44.
    发明专利
    POLYSUBSTITUTED 1,1-PYRIDINYLOXYCYCLOPROPANAMINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知

    公开(公告)号：HRP20080536T5

    公开(公告)日：2009-03-31

    申请号：HRP20080536

    申请日：2008-11-19

    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.

    47.
    发明专利
    未知

    公开(公告)号：AT416166T

    公开(公告)日：2008-12-15

    申请号：AT06291218

    申请日：2006-07-27

    Applicant: SERVIER LAB

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

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

    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.

    АЗАБИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ЭТИ СОЕДИНЕНИЯ
    48.
    发明专利
    АЗАБИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ЭТИ СОЕДИНЕНИЯ 未知

    公开(公告)号：UA84598C2

    公开(公告)日：2008-11-10

    申请号：UAA200610040

    申请日：2005-02-18

    Applicant: SERVIER LAB

    Inventor： CASARA PATRICK ,  CHOLLET ANNE-MARIE ,  DHAINAUT ALAIN ,  BERT LIONEL ,  LESTAGE PIERRE ,  LOCKHART BRIAN

    IPC: A61K31/403 ,  A61P25/00 ,  C07D209/52 ,  C07D403/12

    Abstract: Изобретениеотноситсяк соединениямформулы (І): EMBED ISISServer где: m и n могутбытьодинаковымиилиразличными, причемкаждоеизнихявляетсяцелымчисломот 0 до 2 включительноприсуммедвухцелыхчиселот 2 до 3 включительно; ри q могутбытьодинаковымиилиразличными, причемкаждоеизнихявляетсяцелымчисломот 0 до 2 включительно; Alk представляетсобойалкиленовую, алкениленовуюилиалкиниленовуюцепь; X представляетсобойатомкислорода, атомсерыили -N(R)-группу, вкоторой R представляетсобоюатомводородаилиалкильнуюгруппу, Y, Y' и W определеныв описании. Изобретениетакжеотноситсяк ихэнантиомерам, диастереоизомерам, атакжеихаддитивнымсолямс однойилинесколькимифармацевтическиприемлемымикислотойилиоднимилинесколькимиоснованиями.

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