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    COMPUESTOS HETEROCICLICOS CON AFINIDAD POR LOS RECEPTORES MUSCARINICOS.
    41.
    发明专利
    COMPUESTOS HETEROCICLICOS CON AFINIDAD POR LOS RECEPTORES MUSCARINICOS. 未知

    公开(公告)号：MX2009011499A

    公开(公告)日：2009-11-09

    申请号：MX2009011499

    申请日：2008-04-23

    Applicant: SOLVAY PHARM BV

    Inventor： KRUSE CORNELIS G ,  STOIT AXEL ,  COOLEN HEIN K A C ,  REINDERS JAN H

    IPC: C07D401/04 ,  A61K31/439 ,  A61K31/4427 ,  A61K31/4439 ,  A61P25/28 ,  C07D401/14 ,  C07D413/04 ,  C07D453/02 ,  C07D471/08

    Abstract: La presente invención se refiere compuestos heterociclicos de la fórmula (I) (ver fórmula (I)) en donde: el heterociclo comprende dos enlaces dobles que pueden estar presentes en varias posiciones, representados por las líneas de trazos (---); el heterociclo contiene dos heteroátomos, W es N o NH; Y es CH, O, o NH, en donde si Y es O, X1 es CH y X2 es el residuo C-Z-R2 o C-R3, en donde Z es NH, O, o S; y si Y es CH o NH, uno de X1 y X2 es CH o N, y el otro es el residuo C-Z-R2 o C-R3, en donde Z es NH, o S; R1 se selecciona de las estructuras (a), (b) y (c): (ver fórmulas (a), (b) y (c)) R2 se selecciona de alquilo de C1-C10, alquenilo de C2-C10 y alquinilo de C2-C10, opcionalmente sustituido independientemente con uno o más sustituyentes seleccionados de halógeno, hidroxi, ciano, oxo, alcoxi de C1-C6, alquiltio de C1-C6, alqueniloxi de C1-C6, alqueniltio de C1-C6, alcoxi(C1-C4,)-alcoxi de C1-C4, cicloalquilo de C5-C7, un heterociclo insaturado de 5 miembros (sustituido opcionalmente con halógeno), fenilo, feniloxi y feniltio, en donde el grupo fenilo está sustituido opcionalmente con halógeno; o R2 es un alquilo de C2-C8, no ramificado, sustituido en el simbolo Za de un grupo con la fórmula (la) (ver fórmula (Ia)) en donde si X1 es CH o N, X1a es CH o N y X2a es C-Za-, o si X1 es C-Z-R2, X1a es C-Za- y X2a es CH o N; y los símbolos Wa, Ya y Za y el sustituyente R1a tienen los mismos significados definidos anteriormente para los símbolos W, Y, y Z y el sustituyente R1, y no se seleccionan independientemente; cada uno de los símbolos Wa, Ya y Za y el sustituyente R1a, representan los mismos símbolos y sustituyentes, respectivamente, que los símbolos W, Y, y Z y el sustituyente R1 en la otra parte de la estructura de la fórmula (I); R3 se selecciona de alquilo C4-C10, alquenilo de C2-C10 y alquinilo de C2-C10, opcionalmente sustituidos independientemente con uno o más sustituyentes seleccionados de halógeno, hidroxi, ciano, alcoxi de C1-C6, alquiltio de C1-C6, alqueniloxi de C1-C6, alqueniltio de C1,-C6, alcoxi(C1-C4)-alcoxi de C1-C4, cicloalquilo de C5-C7, un heterociclo insaturado de 5 miembros sustituido opcionalmente con halógeno, fenilo, feniloxi y feniltio, en donde el grupo fenilo está sustituido opcionalmente con halógeno; o una sal, solvato o hidrato farmacéuticamente aceptable de los mismos; los compuestos de la invención tienen afinidad por los receptores muscarinicos y se pueden usar para el tratamiento, alivio o prevención de enfermedades y condiciones mediadas por el receptor muscarínico.

    43.
    发明专利
    未知

    公开(公告)号：NO20090539L

    公开(公告)日：2009-02-06

    申请号：NO20090539

    申请日：2009-02-03

    Applicant: SOLVAY PHARM BV

    Inventor： KRUSE CORNELIS GERRIT ,  COOLEN HEIN K A C ,  STOIT AXEL ,  NEUT MARTINA A W VAN DER

    IPC: C07D471/04 ,  C07D487/04

    Abstract: The invention concerns azaindole derivatives having the general formula (I) wherein the symbols have the meanings given in the specification. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.

    SILDENAFIL N-OXIDE AS PRODRUG
    45.
    发明专利
    SILDENAFIL N-OXIDE AS PRODRUG 未知

    公开(公告)号：CA2690294A1

    公开(公告)日：2008-12-31

    申请号：CA2690294

    申请日：2008-06-23

    Applicant: SOLVAY PHARM BV

    Inventor： TURSKI LECHOSLAW A ,  STOIT AXEL ,  KRUSE CORNELIS G ,  VADER SANDER ,  TULP MARTINUS TH M

    IPC: C07D487/04 ,  A61K31/519 ,  A61P11/00 ,  A61P15/10

    Abstract: The invention concerns sildenafil N-oxide as prodrug, to pharmaceutical compositions containing this compound, to methods for preparing it, and methods for preparing compositions. The invention relates to 1-[[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methyl-4-oxido-piperazine having formula (1A) and pharmacologically acceptable salts, hydrates and solvates thereof. The invention also relates to uses of the compound, and compositions containing it, particularly for the manufacture of medicaments useful in the treatment of affections or diseases effectively treatable - albeit with side effects - with sildenafil.

    Heterocyclic compounds with affinity to muscarinic receptors
    46.
    发明专利
    Heterocyclic compounds with affinity to muscarinic receptors 未知

    公开(公告)号：AU2008240704A1

    公开(公告)日：2008-10-30

    申请号：AU2008240704

    申请日：2008-04-23

    Applicant: SOLVAY PHARM BV

    Inventor： STOIT AXEL ,  TERWEL LOUISE HEIR OF REINDERS ,  KRUSE CORNELIS G ,  COOLEN HEIN K A C

    IPC: A61K31/439 ,  A61K31/4427 ,  A61K31/4439 ,  A61P25/28 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D453/02 ,  C07D471/08

    Abstract: The present invention relates to heterocyclic compounds of the formula (I) wherein - the heterocycle comprises two double bonds which may be present at several positions, represented by the dashed lines ( -- ); - the heterocycle contains two heteroatoms, - W being N or NH; - Y being CH, O or NH, wherein if Y is O, X1 is CH and X2 is the residue C-Z-R2 or C-R3, wherein Z is NH, O, or S; and if Y is CH or NH, one of X1 and X2 is CH or N, the other being the residue C-Z-R2 or C-R3, wherein Z is NH or S; - R1 is selected from the structures (a), (b) and (c): - R2 is selected from (C1-C10)alkyl, (C2-C10)alkenyl and (C2-C10)alkynyl, optionally independently substituted with one or more substituents selected from halogen, hydroxy, cyano, oxo, (C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkenyloxy, (C1-C6)alkenylthio, (C1-C4)alkoxy(C1-C4)alkoxy, (C5-C7)cycloalkyl, a 5-membered unsaturated heterocycle (optionally substituted with halogen), phenyl, phenyloxy and phenylthio, wherein the phenyl group is optionally substituted with halogen; or - R2 is an unbranched (C2-C8)alkyl substituted at the Za-symbol of a group with the formula (Ia) wherein if X1 is CH or N1 X1 is CH or N and X2a is C-Za-, or if X1 is C-Z-R2, X1a is C-Za- and X2a is CH or N; and the symbols Wa, Ya and Za and the substituent R1a have the same meanings as defined previously for the symbols W, Y and Z and the substituent R1, and are not independently selected, each of the symbols Wa, Ya and Za and the substituent R1 a representing identical symbols and substituents, respectively, as the symbols W, Y and Z and the substituent R1 in the other part of the structure of formula (I); - R3 is selected from (C4-C10) alkyl, (C2-C10) alkenyl and (C2-C10) alkynyl, optionally independently substituted with one or more substituents selected from halogen, hydroxy, cyano, (C1C6) alkoxy, (C1C6) alkylthio, (C1C6)alkenyloxy, (C1C6) alkenylthio, (C1-C4) alkoxy (C1-C4) alkoxy, (C5-C7) cycloalkyl, a 5-membered unsaturated heterocycle optionally substituted with halogen, phenyl, phenyloxy and phenylthio, wherein the phenyl group is optionally substituted with halogen; or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the invention have affinity to muscarinic receptors and may be used in the treatment, alleviation or prevention of muscarinic receptor mediated diseases and conditions.

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