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    Substituted thienlycyclohexanone derivatives for enhancing cognition
    1.
    发明授权
    Substituted thienlycyclohexanone derivatives for enhancing cognition 失效

    公开(公告)号：US6156787A

    公开(公告)日：2000-12-05

    申请号：US296753

    申请日：1999-04-22

    Applicant: Howard Barff Broughton ,  Mark Stuart Chambers

    Inventor： Howard Barff Broughton ,  Mark Stuart Chambers

    IPC: C07D333/72 ,  C07D417/12 ,  A61K31/38 ,  A61K31/40 ,  C07D333/56 ,  C07D405/00

    CPC classification number: C07D417/12 ,  C07D333/72

    Abstract: The present invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof: ##STR1## where A is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, arylC.sub.1-6 alkyl, aryl, S(O),R.sup.1, OR.sup.1 or NR.sup.1 R.sup.6 ;R.sup.1 is hydrogen; C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkenyl each of which is optionally substituted by amino, C.sub.1-6 alkylamino, di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkoxy, C.sub.1-6 alkylaminocarbonyl, one, two or three hydroxy groups, one, two or three halogen atoms or a four, five or six-membered saturated heterocyclic ring containing a nitrogen atom and optionally either an oxygen atom or a further nitrogen atom which ring is optionally substituted by C.sub.1-4 alkyl on the further nitrogen atom; aryl, arylC.sub.1-6 alkyl, arylC.sub.2-6 alkenyl or arylC.sub.2-6 alkynyl optionally substituted on the aryl ring by halogen, nitro, cyano, C.sub.1-6 alkylcarbonylamino, hydroxy or C.sub.1-6 alkoxy; or a five-membered aromatic ring containing 1, 2, 3 or 4 heteroatoms chosen from O, N and S provided that not more than one heteroatom is other than N, or a six-membered aromatic ring containing 1, 2, 3 or 4 nitrogen atoms, each of which rings is optionally substituted by halogen, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, aryl, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl;R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1-6 alkyl or together with the carbon atom to which they are attached form a C.sub.3-8 cycloalkyl group;R.sup.4 and R.sup.5 are individually hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl or C.sub.3-8 cycloalkyl or R.sup.12 and R.sup.13, together with the nitrogen atom to which they are attached, form a saturated 4 to 8 membered ring optionally containing an oxygen atom or a further nitrogen atom as a ring member, the further nitrogen atom being unsubstituted or substituted by C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl;R.sup.6 is hydrogen or C.sub.1-6 alkyl;p is zero, 1 or 2; andq is 0, 1 or 2;the preparation of these compounds, their use in enhancing cognition in disease states, particularly Alzheimer's disease, and methods of treatment using them.

    Substituted thienobenzisoxazole derivatives for enhancing cognition
    2.
    发明授权
    Substituted thienobenzisoxazole derivatives for enhancing cognition 失效

    公开(公告)号：US6143773A

    公开(公告)日：2000-11-07

    申请号：US296848

    申请日：1999-04-22

    Applicant: Howard Barff Broughton ,  Mark Stuart Chambers

    Inventor： Howard Barff Broughton ,  Mark Stuart Chambers

    IPC: C07D498/04 ,  C07D495/04 ,  A61K31/42

    CPC classification number: C07D498/04

    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein A is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, arylC.sub.1-6 alkyl, aryl, S(O).sub.p R.sup.1, OR.sup.1 or NR.sup.1 R.sup.12 ;B is optionally substituted 5- or 6-membered heteroaromatic ring or C(O)NR.sup.10 R.sup.11 ;R.sup.1 is hydrogen, optionally substituted C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkenyl, optionally substituted aryl, arylC.sub.1-6 alkyl, arylC.sub.2-6 alkenyl or arylC.sub.2-6 alkynyl or an optionally substituted 5- or 6-membered heteroaromatic ring;R.sup.2 and R.sup.3 are hydrogen or C.sub.1-6 alkyl;R.sup.4 is hydrogen, C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, aryl or CH.sub.2 (CO).sub.m NR.sup.8 R.sup.9 ;R.sup.5 is NR.sup.6 R.sup.7, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;R.sup.6 is independently as defined for R.sup.4 ;R.sup.7 is aryl optionally substituted by halogen, nitro or cyano;R.sup.8 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkenyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl; arylC.sub.1-6 alkyl, arylC.sub.2-6 alkenyl or arylC.sub.2-6 alkynyl optionally substituted on the aryl ring by halogen, nitro or cyano; thiophene or pyridine;R.sup.9 is C.sub.1-6 alkyl; C.sub.2- alkenyl; C.sub.2-6 alkynyl; or phenyl optionally substituted by one, two or three substituents independently chosen from halogen, CF.sub.3, OCH.sub.3, nitro and cyano;R.sup.10 and R.sup.11 are individually hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl or C.sub.3-8 cycloalkyl or R.sup.10 and R.sup.11, together with the nitrogen atom to which they are attached, form a saturated 4 to 8 membered ring optionally containing an oxygen atom or a further nitrogen atom as a ring member, the further nitrogen atom being unsubstituted or substituted by C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl;R.sup.12 is hydrogen or C.sub.1-6 alkyl;m is zero or 1;p is zero, 1 or 2;q is 0, 1 or 2; andr is 0, 1 or 2;the preparation of these compounds, their use in enhancing cognition in disease states, particularly Alzheimer's disease, and methods of treatment using them.

    Tetrahydroindolone derivatives as gabaaalpha5 ligands for enhancing cognition
    3.
    发明授权
    Tetrahydroindolone derivatives as gabaaalpha5 ligands for enhancing cognition 失效
    四氢吲哚酮衍生物作为增加认知的gabaaalpha5配体

    公开(公告)号：US06395766B1

    公开(公告)日：2002-05-28

    申请号：US09674740

    申请日：2000-11-06

    Applicant: Howard Barff Broughton ,  Helen Jane Bryant ,  Mark Stuart Chambers ,  Neil Roy Curtis

    Inventor： Howard Barff Broughton ,  Helen Jane Bryant ,  Mark Stuart Chambers ,  Neil Roy Curtis

    IPC: A61K31404

    CPC classification number: C07D401/04 ,  A61K31/40 ,  C07D209/08 ,  C07D401/14 ,  C07D403/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

    Abstract: Compounds according to Formula (I) or a pharmaceutically acceptable salt thereof are GABA-A Alpha 5 ligands useful for enhancing cognition: where A is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, arylC1-6alkyl, or aryl wherein the aryl group is optionally substituted by halogen, C1-6alkyl, CF3, CN, NO2 or NH2, NR1R10, S(O)pR1, heteroarylC1-6alkyl or heteroaryl where heteroaryl is a 5- or 6-membered heteroaromatic ring as defined for B; and B is phenyl or a 5-membered ring having one or two unsaturations containing 1, 2, 3, or 4 heteroatoms chosen from O, N and S provided that not more than one heteroatom is other than N, a 6-membered heteroaromatic ring containing 1, 2, 3 or 4 nitrogen atoms, each of which rings is optionally substituted by one or more substituents.

    Abstract translation: 根据式（I）的化合物或其药学上可接受的盐是可用于增强认知的GABA-Aα5配体：其中A是C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基，芳基C 1-6烷基或芳基 其中芳基任选被卤素，C 1-6烷基，CF 3，CN，NO 2或NH 2，NR 1 R 10，S（O）p R 1，杂芳基C 1-6烷基或杂芳基取代，其中杂芳基是5-或6-元杂芳环， B; 并且B是苯基或具有1或2个不饱和基团的5元环，其含有1,2,3或4个选自O，N和S的杂原子，条件是不超过一个杂原子不是N，6元杂芳环 含有1,2,3或4个氮原子，其中每个环任选被一个或多个取代基取代。

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