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    1-azabicycloalkane derivatives, their preparation process and their use as medicaments
    2.
    发明授权
    1-azabicycloalkane derivatives, their preparation process and their use as medicaments 失效
    1-氮杂双环链烷烃衍生物，其制备方法及其作为药物的用途

    公开(公告)号：US5015655A

    公开(公告)日：1991-05-14

    申请号：US426778

    申请日：1989-10-26

    申请人： Giulio Galliani ,  Fernando Barzaghi ,  Carla Bonetti ,  Emilio Toja

    发明人： Giulio Galliani ,  Fernando Barzaghi ,  Carla Bonetti ,  Emilio Toja

    IPC分类号： A61K31/40 ,  A61K31/435 ,  A61K31/55 ,  A61P25/02 ,  A61P25/28 ,  C07D453/02 ,  C07D471/08 ,  C07D487/08

    CPC分类号： C07D487/08 ,  C07D453/02

    摘要： Compounds useful in the treatment of Alzheimers's disease, senile dementia or memory disorders of the aged of the formula ##STR1## in which n represents the number 1, 2 or 3,R.sub.1 and R.sub.2, identical or different, represent hydrogen, a linear, branched or cyclic alkyl, alkenyl, or alkynyl which contain up to 6 carbon atoms, R.sub.1 and R.sub.2 optionally substituted by hydroxy, alkoxy containing up to 6 carbon atoms, aralkyl containing up to 14 carbon atoms, a COOalk.sub.1 radical in which alk.sub.1 represents alkyl containing up to 6 carbon atoms, a --CON(alk.sub.2).sub.2 radical in which alk.sub.2 represents alkyl containing up to 6 carbon the radical --C(R.sub.1).dbd.NOR.sub.2 being in position 2, 3 or 4, in all their isomer forms and their mixture, as well as their addition salts with pharmaceutically acceptable organic or mineral acids. Also therapeutic compositions containing the compounds, method of treatment and method of preparation.

    摘要翻译： 用于治疗阿尔茨海默病，老年痴呆或老年化记忆障碍的化合物，其中n表示数字1,2或3，R 1和R 2相同或不同，表示氢，a 含有至多6个碳原子的直链，支链或环状烷基，烯基或炔基，任选被羟基取代的R 1和R 2，含有至多6个碳原子的烷氧基，含有至多14个碳原子的芳烷基，其中alk1代表 含有至多6个碳原子的烷基，-CON（alk2）2基团，其中alk2表示含有至多6个碳的烷基，基团-C（R 1）= NOR 2位于2,3或4位，全部为其异构体形式， 它们的混合物，以及它们与药学上可接受的有机或无机酸的加成盐。 还含有该化合物的治疗组合物，治疗方法和制备方法。

    Derivatives of 1,2,5,6-tetrahydropyridin-3-carboxaldehyde oxime
    3.
    发明授权
    Derivatives of 1,2,5,6-tetrahydropyridin-3-carboxaldehyde oxime 失效
    1,2,5,6-四氢吡啶-3-羧甲醛氧化物的衍生物

    公开(公告)号：US5204479A

    公开(公告)日：1993-04-20

    申请号：US699631

    申请日：1991-05-15

    申请人： Emilio Toja ,  Carla Bonetti ,  Fernando Barzaghi ,  Giulio Galliani

    发明人： Emilio Toja ,  Carla Bonetti ,  Fernando Barzaghi ,  Giulio Galliani

    IPC分类号： A61K31/445 ,  A61K31/00 ,  A61K31/4465 ,  A61P25/28 ,  C07D211/70

    CPC分类号： C07D211/70

    摘要： The subject of the invention is the compounds of formula (I): ##STR1## in which: R represents a hydrogen atom, a saturated or unsaturated, linear, branched or cyclic alkyl radical containing up to 8 carbon atoms,R' represents an amine-containing moiety of an .alpha.-amino acid or a peptide, containing as an end group an amine-containing moiety of an .alpha.-amino acid as well as their addition salts with organic or mineral acids.The compounds of formula (I) have useful pharmacological properties which justify their use in therapeutics.

    摘要翻译： 本发明的主题是式（I）的化合物：其中：R表示氢原子，含有至多8个碳原子的饱和或不饱和的直链，支链或环状烷基，R' 代表α-氨基酸或肽的含胺部分，其含有作为端基的α-氨基酸的含胺部分以及它们与有机或无机酸的加成盐。 式（I）化合物具有有用的药理学性质，其证明其在治疗中的用途。

    Compounds of 1,2,5,6-tetrahydropyridin-3-carboxaldehyde oxime which are useful as cholinergic agents
    5.
    发明授权
    Compounds of 1,2,5,6-tetrahydropyridin-3-carboxaldehyde oxime which are useful as cholinergic agents 失效
    可作为纯化剂使用的1,2,5,6-四氢吡啶-3-羰氧基二甲氧基化合物的化合物

    公开(公告)号：US5219872A

    公开(公告)日：1993-06-15

    申请号：US19256

    申请日：1987-02-26

    申请人： Giulio Galliani ,  Fernando Barzaghi ,  Alina Butti ,  Carla Bonetti ,  Emilio Toja

    发明人： Giulio Galliani ,  Fernando Barzaghi ,  Alina Butti ,  Carla Bonetti ,  Emilio Toja

    IPC分类号： A61K31/44 ,  A61P25/28 ,  A61P43/00 ,  C07D211/28 ,  C07D211/70

    CPC分类号： C07D211/70

    摘要： Compounds useful in the treatment of Alzheimer's disease, senile dementia, or memory disorders which have the formula ##STR1## in which R represents a hydrogen atom, a linear, branched or cyclic alkyl radical, saturated or unsaturated, containing up to 8 carbon atoms, possibly substituted by a free or esterified carboxy radical or R represents an aralkyl radical containing up to 10 carbon atoms and R' represents a linear or branched, saturated or unsaturated, alkyl radical, containing up to 8 carbon atoms, a radical --COalk.sub.1 or a radical --(CH.sub.2).sub.2 N(alk.sub.2).sub.2, alk.sub.1 and alk.sub.2 representing an alkyl radical containing up to 8 carbon atoms, as well as their addition salts with acids. Also compositions containing the same, method of preparation and method of treatment using the same.

    摘要翻译： 用于治疗阿尔茨海默病，老年性痴呆或记忆障碍的化合物，其具有式（IMAGE），其中R表示氢原子，含有至多8个碳原子的饱和或不饱和的直链，支链或环状烷基， 可能被游离或酯化的羧基取代，或R表示含有至多10个碳原子的芳烷基，R'表示含有至多8个碳原子的直链或支链，饱和或不饱和的烷基，基团-COalk1或 自由基 - （CH2）2N（alk2）2，alk1和alk2代表含有至多8个碳原子的烷基，以及它们与酸的加成盐。 还含有相同的组合物，制备方法和使用其的处理方法。

    Oxime of 1, 2, 5, 6-tetrahydropyridine compounds their use as medicaments and the compositions containing them
    6.
    发明授权
    Oxime of 1, 2, 5, 6-tetrahydropyridine compounds their use as medicaments and the compositions containing them 失效
    1,2,5,6-四氢吡啶的肟化合物用作药物和含有它们的组合物

    公开(公告)号：US4902699A

    公开(公告)日：1990-02-20

    申请号：US234627

    申请日：1988-08-22

    申请人： Emilio Toja ,  Carla Bonetti ,  Fernando Barzaghi ,  Giulio Galliani

    发明人： Emilio Toja ,  Carla Bonetti ,  Fernando Barzaghi ,  Giulio Galliani

    IPC分类号： A61K31/445 ,  A61P25/28 ,  C07D211/94

    CPC分类号： C07D211/94

    摘要： Compounds useful in the treatment of patients suffering from senile dementia, Alzheimer's disease or memory defects, of the formula ##STR1## in which R represents hydrogen or a linear, branched or cyclic alkyl, alkenyl, or alkynyl, containing up to 8 carbon atoms, or the radical ##STR2## in which R.sub.1 represents a linear or branched, alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, a linear or branched, saturated or unsaturated, alkoxy containing up to 8 carbon atoms, or aryl containing up to 14 carbon atoms, or the radical ##STR3## in which R.sub.2 represents a linear or branched alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, aryl containing up to 14 carbon atoms, possibly substituted, or aralkyl containing up to 18 carbon atoms, possibly substituted, and R' represents a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, as well as their addition salts with organic or mineral acids.

    摘要翻译： 用于治疗患有老年性痴呆，阿尔茨海默氏病或​​记忆缺陷的患者，其中R表示氢或含有至多8个碳原子的直链，支链或环状的烷基，烯基或炔基， 或其中R 1表示含有至多8个碳原子的直链或支链的烷基，烯基或炔基，含有至多8个碳原子的直链或支链，饱和或不饱和的烷氧基，或含有至多 14个碳原子，或者其中R 2表示含有至多8个碳原子的直链或支链烷基，烯基或炔基，含有至多14个碳原子的芳基，可能被取代的基团，或含有至多18个碳原子的芳烷基 ，可能被取代，R'代表含有至多8个碳原子的直链，支链或环状的烷基，烯基或炔基，以及它们与有机或无机酸的加成盐。

    Derivatives of 1,2,5,6-tetrahydropyridine substituted by a thiazolyl or oxazolyl radical, their use as medicaments and compositions containing them
    7.
    发明授权
    Derivatives of 1,2,5,6-tetrahydropyridine substituted by a thiazolyl or oxazolyl radical, their use as medicaments and compositions containing them 失效
    作为药物和组合物使用的由噻唑啉或氧杂唑基衍生物取代的1,2,5,6-四氢吡啶的衍生物

    公开(公告)号：US5053416A

    公开(公告)日：1991-10-01

    申请号：US457566

    申请日：1989-12-27

    申请人： Emilio Toja ,  Carla Bonetti ,  Fernando Barzaghi ,  Giulio Galliani

    发明人： Emilio Toja ,  Carla Bonetti ,  Fernando Barzaghi ,  Giulio Galliani

    IPC分类号： A61K31/425 ,  A61K31/435 ,  A61P25/00 ,  C07D413/04 ,  C07D417/04

    CPC分类号： C07D413/04 ,  C07D417/04

    摘要： Compounds of formula (I) ##STR1## in which X represents oxygen or sulphur, R.sub.1 represents hydrogen, a linear, branched or cyclic alkyl containing up to 8 carbon atoms, an alkenyl or alkynyl containing up to 6 carbon atoms, hydroxyl, an OCOalk.sub.1 radical in which alk.sub.1 represents alkyl containing up to 6 carbon atoms, an OCONHalk.sub.2 radical in which alk.sub.2 represents alkyl containing up to 6 carbon atoms, a CO.sub.2 alk.sub.3 radical in which alk.sub.3 represents alkyl or alkenyl containing up to 6 carbon atoms, an Oalk.sub.4 radical in which alk.sub.4 represents alkyl containing up to 6 carbon atoms, an OCOAr.sub.1, OCONHAr.sub.2 or CO.sub.2 Ar.sub.3 radical in which Ar.sub.1, Ar.sub.2 or Ar.sub.3 represents aryl containing up to 14 carbon atoms, R.sub.2 represents hydrogen, a linear, branched or cyclic alkyl containing up to 6 carbon atoms, alkenyl or alkynyl containing up to 6 carbon atoms, an alkoxyalkyl alk'.sub.1 Oalk'.sub.2 radical in which alk'.sub.1 and alk'.sub.2 represent alkyl containing up to 6 carabon atoms, hydroxyalkyl in which the alkyl contains up to 6 carbon atoms or aryl containing up to 14 carbon atoms, as well as their addition salts with organic or mineral acids, which compounds are useful in the treatment of patients suffering from Alzheimer's disease, senile dementia or memory disorders of the aged; also, compositions containing the same, method of use, method of preparation, and intermediates therefor.

    摘要翻译： 式（I）化合物其中X表示氧或硫，R1表示氢，含有至多8个碳原子的直链，支链或环状烷基，含有至多6个碳原子的烯基或炔基，羟基 ，其中alk1表示含有至多6个碳原子的烷基的OCOalk1基团，其中alk2表示含有至多6个碳原子的烷基的OCONHalk2基团，其中alk3表示含有至多6个碳原子的烷基或烯基的CO 2alk 3基团，Oalk4 其中alk4表示含有至多6个碳原子的烷基，OCOAr1，OCONHAr2或CO2Ar3基团，其中Ar1，Ar2或Ar3表示含有至多14个碳原子的芳基，R2表示氢，直链，支链或环状烷基， 6个碳原子，含有至多6个碳原子的烯基或炔基，烷基alk'1Oalk'2基团，其中alk'1和alk'2代表含有多达6个carabon原子的烷基，其中烷基含有多达6个碳原子的羟烷基 含有至多14个碳原子的原子或芳基，以及它们与有机或无机酸的加成盐，该化合物可用于治疗患有阿尔茨海默病，老年痴呆或老年记忆障碍的患者; 也可以使用含有该组合物的组合物，使用方法，制备方法及其中间体。

    Compounds of 1,2,5,6-tetrahydropyridine which are useful as cholinergic agents
    8.
    发明授权
    Compounds of 1,2,5,6-tetrahydropyridine which are useful as cholinergic agents 失效
    可用作胆碱能剂的1,2,5,6-四氢吡啶的化合物

    公开(公告)号：US5219873A

    公开(公告)日：1993-06-15

    申请号：US408441

    申请日：1989-09-15

    申请人： Giulio Galliani ,  Fernando Barzaghi ,  Carla Bonetti ,  Emilio Toja

    发明人： Giulio Galliani ,  Fernando Barzaghi ,  Carla Bonetti ,  Emilio Toja

    IPC分类号： C07D211/70 ,  C07D211/94

    CPC分类号： C07D211/94 ,  C07D211/70

    摘要： Compounds useful in the treatment of Alzheimer's disease, senile dimentia and memory disorders of the formula ##STR1## in which R represents hydrogen, hydroxyl, a linear, branched or cyclic, saturated or unsaturated, alkyl, containing up to 8 carbon atoms, possibly substituted by free or esterified carboxy or R represents aralkyl containing up to 10 carbon atoms or --COOZ in which Z represents a linear, branched or cyclic saturated or unsaturated, alkyl containing up to 8 carbon atoms and R.sub.2 represents hydrogen or a linear or branched, saturated or unsaturated alkyl containing up to 8 carbon atoms, COalk.sub.1 radical or (CH.sub.2).sub.2 N(alk.sub.2).sub.2, alk.sub.1 and alk.sub.2 representing an alkyl containing up to 8 carbon atoms, as well as their addition salts with acids provided that if R represents an alkyl R.sub.2 does not represent hydrogen; also therapeutic compositions containing at least one said compound and method of treating patients with said compounds.

    摘要翻译： 用于治疗阿尔茨海默氏病，老年病和记忆障碍的化合物，其中R代表氢，羟基，含有至多8个碳原子的直链，支链或环状饱和或不饱和的烷基，可能被取代 通过游离或酯化的羧基或R表示含有至多10个碳原子的芳烷基或-COOZ，其中Z表示含有至多8个碳原子的直链，支链或环状饱和或不饱和的烷基，R2表示氢或直链或支链饱和 或含有至多8个碳原子的不饱和烷基，COalk1基或（CH2）2N（alk2）2，alk1和alk2代表含有至多8个碳原子的烷基，以及它们与酸的加成盐，条件是如果R表示烷基 R2不代表氢; 还含有至少一种所述化合物的治疗组合物和用所述化合物治疗患者的方法。

    1-azabicycloalkane derivatives, their preparation process and their use as medicaments
    10.
    发明授权
    1-azabicycloalkane derivatives, their preparation process and their use as medicaments 失效
    1-氮杂双环链烷烃衍生物，其制备方法及其作为药物的用途

    公开(公告)号：US5183893A

    公开(公告)日：1993-02-02

    申请号：US664120

    申请日：1991-03-26

    申请人： Giulio Galliani ,  Fernando Barzaghi ,  Carla Bonetti ,  Emilio Toja

    发明人： Giulio Galliani ,  Fernando Barzaghi ,  Carla Bonetti ,  Emilio Toja

    IPC分类号： C07D453/02 ,  C07D487/08

    CPC分类号： C07D487/08 ,  C07D453/02

    摘要： Compounds useful in the treatment of Alzheimer's disease, senile dementia or memory disorders of the aged of the formula ##STR1## in which n represents the number 1, 2 or 3,R.sub.1 and R.sub.2, identical or different, represent hydrogen, a linear, branched or cyclic alkyl, alkenyl, or alkynyl which contain up to 6 carbon atoms, R.sub.1 and R.sub.2 optionally substituted by hydroxy, alkoxy containing up to 6 carbon atoms, aralkyl containing up to 14 carbon atoms, a COOalk.sub.1 radical in which alk.sub.1 represents alkyl containing up to 6 carbon atoms, a --CON(alk.sub.2).sub.2 radical in which alk.sub.2 represents alkyl containing up to 6 carbon atoms, the radical --C(R.sub.1).dbd.NOR.sub.2 being in position 2, 3 or 4, in all their isomer forms and their mixture, as well as their addition salts with pharmaceutically acceptable organic or mineral acids. Also therapeutic compositions containing the compound, method of treatment and method of preparation.

    摘要翻译： 用于治疗阿尔茨海默氏病，老年痴呆或老年化记忆障碍的化合物，其中n表示1,2或3，R1和R2相同或不同，表示氢，a 含有至多6个碳原子的直链，支链或环状烷基，烯基或炔基，任选被羟基取代的R 1和R 2，含有至多6个碳原子的烷氧基，含有至多14个碳原子的芳烷基，其中alk1代表 含有至多6个碳原子的烷基，-CON（alk2）2基团，其中alk2表示含有至多6个碳原子的烷基，基团-C（R 1）= NOR 2位于其所有异构体的2,3或4位 形式及其混合物，以及它们与药学上可接受的有机或无机酸的加成盐。 还含有该化合物，治疗方法和制备方法的治疗组合物。