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    NOVEL POLYSUBSTITUTED 1,1-PYRIDINYL AMINOCYCLOPROPANAMINE DERIVATIVES, METHOD FOR PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
    2.
    发明申请
    NOVEL POLYSUBSTITUTED 1,1-PYRIDINYL AMINOCYCLOPROPANAMINE DERIVATIVES, METHOD FOR PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
    新的多取代的1,1-吡啶基亚氨基环丙胺衍生物，其制备方法及含有该化合物的药物组合物

    公开(公告)号：WO2007012761A8

    公开(公告)日：2007-12-21

    申请号：PCT/FR2006001831

    申请日：2006-07-27

    Applicant: SERVIER LAB ,  GOLDSTEIN SOLO ,  GUILLONNEAU CLAUDE ,  CHARTON YVES ,  LOCKHART BRIAN ,  LESTAGE PIERRE

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

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

    CPC classification number: C07D213/74

    Abstract: The invention concerns compounds of formula (I), wherein: n represents an integer between 1 and 6 inclusively; R 1 and R 2 represent a hydrogen atom a (C 1 -C 6 ) alkyl or (C 1 -C 6 ) arylalkyl group; R 3 and R 4 represent a hydrogen atom, a (C 1 -C 6 ) alkyl group; R 5 and R 6 represent a hydrogen atom, a (C 1 -C 6 ) alkyl group, halogen, hydroxy, (C 1 -C 6 ) alkoxy, cyano, nitro, (C 2 -C 6 ) acyl, (C 1 -C 6 ) alkoxycarbonyl, (C 1 -C 6 ) trihalogenoalkyl, (C 1 -C 6 ) trihalogenoalkoxy or amino optionally substituted; R 7 represents a hydrogen atom, a (C 1 -C 6 ) alkyl group or arylalkyl. The invention is useful for preparing medicines.

    Abstract translation: 本发明涉及式（I）的化合物，其中：n表示1至6的整数; R 1和R 2代表氢原子a（C 1 -C 6）烷基或（C 1 -C 6烷基） 1〜6）芳基烷基; R 3和R 4代表氢原子，（C 1 -C 6）烷基;并且R 4代表氢原子，（C 1 -C 6） R 5和R 6代表氢原子，（C 1 -C 6）6烷基，卤素 ，羟基，（C 1 -C 6）烷氧基，氰基，硝基，（C≡C2 -C 6） ）酰基，（C 1 -C 6）烷氧基羰基，（C 1 -C 6）亚烷基，（（C 1 -C 6） C1-C6）任选取代的三卤代烷氧基或氨基; R 7代表氢原子，（C 1 -C 6）烷基或芳基烷基。 本发明对于制备药物是有用的。

    7.
    发明专利
    未知

    公开(公告)号：AT437857T

    公开(公告)日：2009-08-15

    申请号：AT07730888

    申请日：2007-01-30

    Applicant: SERVIER LAB

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

    IPC: C07D213/65 ,  A61K31/4418 ,  A61P25/00 ,  C07D401/10

    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.

    DERIVADOS 1,1-PIRIDINILOXICICLOPROPANOAMINAS POLISUSTITUIDOS, SU PROCEDIMIENTO DE PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN.
    8.
    发明专利
    DERIVADOS 1,1-PIRIDINILOXICICLOPROPANOAMINAS POLISUSTITUIDOS, SU PROCEDIMIENTO DE PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN. 未知

    公开(公告)号：ES2313589T3

    公开(公告)日：2009-03-01

    申请号：ES06291219

    申请日：2006-07-27

    Applicant: SERVIER LAB

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

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

    Abstract: Compuestos 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 del otro, representan un átomo de hidrógeno o un grupo alquilo(C1-C6) lineal o ramificado o arilalquilo (C1-C6) lineal o ramificado, R3 y R4, idénticos o diferentes, independientemente uno del otro, representan un átomo de hidrógeno o un grupo alquilo(C1-C6) lineal o ramificado, entendiéndose que al menos uno de los dos grupos R3 ó R4 representa un grupo alquilo(C1-C6) lineal o ramificado, R5 y R6, idénticos o diferentes, independientemente uno del otro, representan un átomo de hidrógeno o un grupo alquilo(C1-C6) lineal o ramificado, un halógeno, hidroxilo, alcoxi(C1-C6) lineal o ramificado, ciano, nitro, acilo(C2-C6) lineal o ramificado, alcoxicarbonilo(C1-C6) lineal o ramificado, trihaloalquilo(C1-C6) lineal o ramificado, trihaloalcoxi( C1-C6) lineal o ramificado o amino, eventualmente sustituido con uno o dos grupos alquilo(C1-C6) lineales o ramificados, por grupo arilo se entiende un grupo fenilo, bifenilo, naftilo, dihidronaftilo, tetrahidronaftilo, indanilo e indenilo, estando cada uno de estos grupos eventualmente sustituido con uno o varios grupos, idénticos o diferentes, seleccionados de entre halógeno, alquilo(C1-C6) lineal o ramificado, hidroxilo, ciano, nitro, alcoxi(C1-C6) lineal o ramificado, acilo(C2-C7) lineal o ramificado, alcoxicarbonilo(C1-C6) lineal o ramificado, trihaloalquilo(C1-C6) lineal o ramificado, trihaloalcoxi(C1-C6) lineal o ramificado y amino, eventualmente sustituido con uno o dos grupos alquilo(C1-C6) lineales o ramificados, sus enantiómeros, diastereoisómeros, así como sus sales de adición de un ácido o de una base farmacéuticamente aceptables.

    NOVEL AZABICYCLIC DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
    10.
    发明专利
    NOVEL AZABICYCLIC DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 未知

    公开(公告)号：HRP20080184T5

    公开(公告)日：2008-10-31

    申请号：HRP20080184

    申请日：2008-04-22

    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%.

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