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    Imidazole compounds, their preparation and use
    2.
    发明授权
    Imidazole compounds, their preparation and use 失效
    咪唑化合物，其制备和用途

    公开(公告)号：US5441969A

    公开(公告)日：1995-08-15

    申请号：US172427

    申请日：1993-12-22

    申请人： Oskar Axelsson ,  Dan Peters ,  Elsebet O Nielsen

    发明人： Oskar Axelsson ,  Dan Peters ,  Elsebet O Nielsen

    IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61K31/425 ,  A61P9/00 ,  A61P9/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  C07D235/30 ,  C07D401/10 ,  C07D403/10 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  C07D417/04 ,  C07D417/10 ,  A61K31/445

    CPC分类号： C07D401/10 ,  C07D235/30 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D417/10

    摘要： The present invention discloses compounds of the formula ##STR1## or a pharmaceutically-acceptable addition salt thereof whereinR' and R" independently of each other are hydrogen or alkyl, or R' and R" together form a 3 to 6 membered alkylene chain;one of R.sup.1 and R.sup.2 is aryl which may be substituted one or more times with halogen, CF.sub.3, CN, OH, alkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, amino, nitro, sulphamoyl, tetrazolyl, CO.sub.2 H, CO.sub.2 -alkyl and the other of R.sup.1 and R.sup.2 is hydrogen, halogen, alkoxy, amino or alkyl; andR.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently of each other are hydrogen, halogen, amino, nitro, CN, OH, CF.sub.3, alkyl or alkoxy; and n is 0 or 1; provided that neither of R.sup.1 and R.sup.2 is phenyl or substituted phenyl when n is 0.The compounds are useful as pharmaceuticals, for example, in the treatment of ischemia, anoxia, migraine and psychosis.

    摘要翻译： 本发明公开了式IMA的化合物或其药学上可接受的加成盐，其中R'和R“彼此独立地是氢或烷基，或者R'和R”一起形成3至6元亚烷基 链; R 1和R 2之一是可以被卤素，CF 3，CN，OH，烷基，环烷基烷基，烯基，炔基，烷氧基，氨基，硝基，氨磺酰基，四唑基，CO 2 H，CO 2 - 烷基和其它的取代一次或多次的芳基 的R 1和R 2是氢，卤素，烷氧基，氨基或烷基; R 4，R 5，R 6和R 7彼此独立地是氢，卤素，氨基，硝基，CN，OH，CF 3，烷基或烷氧基; 并且n为0或1; 条件是当n为0时，R 1和R 2都不是苯基或取代的苯基。该化合物可用作药物，例如用于治疗缺血，缺氧，偏头痛和精神病。

    Azacyclooctane and heptane derivatives, their preparation and use in therapy
    3.
    发明授权
    Azacyclooctane and heptane derivatives, their preparation and use in therapy 失效
    氮杂环辛烷和庚烷衍生物，其制备和用于治疗

    公开(公告)号：US06680314B2

    公开(公告)日：2004-01-20

    申请号：US10134498

    申请日：2002-04-30

    申请人： Dan Peters ,  Gunnar M. Olsen ,  Simon F. Nielsen ,  Elsebet O. Nielsen

    发明人： Dan Peters ,  Gunnar M. Olsen ,  Simon F. Nielsen ,  Elsebet O. Nielsen

    IPC分类号： A61K3155

    CPC分类号： C07D401/04 ,  C07D223/06 ,  C07D225/02

    摘要： Compounds of formula (1) or (2), enantiomers thereof, mixtures thereof, and pharmaceutically acceptable salts thereof: wherein: n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is aryl optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteroaryl group, or R is a monocyclic 5 to 6-membered heteroaryl group optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteraryl group, or R is a bicyclic heteroaryl group composed of a monocyclic 5 to 6-membered heteroaryl group fused to a benzene ring, optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteroaryl group. The compounds, enantiomers, and salts are useful as ligands for nicotinic ACh receptors.

    摘要翻译： 式（1）或（2）的化合物，其对映异构体，其混合物及其药学上可接受的盐：其中：n为0或1; R是氢，烷基，烯基，炔基，环烷基，环烷基烷基，芳基或芳烷基; 并且R 1为任选被烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3，OCF 3，CN，氨基，硝基，芳基或单环5至 或者R是任选被烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3，OCF 3，CN取代的单环5至6元杂芳基， 氨基，硝基，芳基或单环5至6元杂芳基，或R为由与苯环稠合的单环5至6元杂芳基组成的双环杂芳基，任选被烷基，环烷基，环烷基烷基烯基 炔基，烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3，OCF 3，CN，氨基，硝基，芳基或单环5至6元杂芳基。 化合物，对映体和盐可用作烟碱型ACh受体的配体。

    Azacyclooctane and heptane derivatives, their preparation and use in therapy
    4.
    发明授权
    Azacyclooctane and heptane derivatives, their preparation and use in therapy 失效
    氮杂环辛烷和庚烷衍生物，其制备和用于治疗

    公开(公告)号：US06420395B1

    公开(公告)日：2002-07-16

    申请号：US09450636

    申请日：1999-11-29

    申请人： Dan Peters ,  Gunnar M. Olsen ,  Simon F. Nielsen ,  Elsebet O. Nielsen

    发明人： Dan Peters ,  Gunnar M. Olsen ,  Simon F. Nielsen ,  Elsebet O. Nielsen

    IPC分类号： A61K3144

    CPC分类号： C07D401/04 ,  C07D223/06 ,  C07D225/02

    摘要： The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalky-alkyl, aryl or aralkyl; and R1 is aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cyloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3. CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group, or a bicyclic heteroaryl group composed of a monocyclic 5 to 6-membered heteroaryl group fused to a benzene ring and which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group. The compounds of the invention are useful as nicotinic ACh receptor ligands.

    摘要翻译： 本发明公开了式（1）或（2）的化合物，其任何对映体或其任何混合物或其药学上可接受的盐; 其中n为0或1; R是氢，烷基，烯基，炔基，环烷基，环烷基，芳基或芳烷基; 并且R 1是可以被选自烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3，OCF 3，CN，氨基的取代基取代一次或多次的芳基 ，硝基，芳基和单环5至6元杂芳基，可以被选自烷基，环烷基，环烷基烷基烯基，炔基，烷氧基， 环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3，OCF 3。 CN，氨基，硝基，芳基和单环5至6元杂芳基，或由与苯环稠合的单环5至6元杂芳基组成的双环杂芳基，其可以被取代基取代一次或多次 选自烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3，OCF 3，CN，氨基，硝基，芳基和单环5至6元杂芳基 。 本发明的化合物可用作烟碱ACh受体配体。

    1-substituted-2-(N-pheny l-N-(phenylmethyl)methanamine)-4,5-dihydro-imidazoles and related compounds and their use in treating calcium overload in brain cells
    5.
    发明授权
    1-substituted-2-(N-pheny l-N-(phenylmethyl)methanamine)-4,5-dihydro-imidazoles and related compounds and their use in treating calcium overload in brain cells 失效
    1-取代-2-（N-苯基-N-（苯甲基）甲胺）-4,5-二氢咪唑及其相关化合物及其在脑细胞中治疗钙超载中的应用

    公开(公告)号：US5296493A

    公开(公告)日：1994-03-22

    申请号：US704469

    申请日：1991-05-23

    申请人： Peter Moldt ,  Elsebet O. Nielsen

    发明人： Peter Moldt ,  Elsebet O. Nielsen

    IPC分类号： C07D233/24 ,  C07D233/54 ,  C07D233/60 ,  C07D235/14 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  A61K31/415 ,  A61K31/44 ,  C07D233/61 ,  C07D401/06

    CPC分类号： C07D233/64 ,  C07D233/24 ,  C07D235/14 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12

    摘要： The present patent application discloses compounds of the formula ##STR1## wherein R.sup.1 is C.sub.1-10 saturated or unsaturated alkyl; or ##STR2## wherein R'" is H or ##STR3## R.sup.2 is phenyl which is unsubstituted or substituted one or more times with halogen, CF.sub.3, C.sub.1-6 -alkoxy, NO.sub.2, CO.sub.2 --C.sub.1-6 -alkyl, methyl; benzyl which may be substituted one or more times with halogen, CF.sub.3, C.sub.1-6 -alkoxy, NO.sub.2, CO.sub.2 --C.sub.1-6 -alkyl, methyl; pyridyl; or cyclohexyl;R.sup.3 phenyl which is unsubstituted or substituted one or more times with halogen, CF.sub.3, C.sub.1-6 -alkoxy, NO.sub.2, CO.sub.2 --C.sub.1-6 -alkyl, methyl; naphthyl which may be substituted one or more times with halogen, CF.sub.3, C.sub.1-6 -alkoxy, NO.sub.2, CO.sub.2 --C.sub.1-6 -alkyl, methyl; pyridyl; C.sub.1-6 unsaturated alkyl; furanyl;R.sup.4 is H, C.sub.1-6 -alkyl, or benzyl; or ##STR4## together form ##STR5## R' and R" are each hydrogen or together form an extra benzo ring; and wherein the dotted line represents an optional extra bond between the two carbon atoms designated .alpha. and .beta.,or a pharmaceutically-acceptable addition salt thereof.The compounds are useful as pharmaceuticals, for example in the treatment of Ca overload in brain cells.

    摘要翻译： 本专利申请公开了式IMA的化合物，其中R 1是C 1-10饱和或不饱和的烷基; 或者其中R“'为H或R 2是未被取代或被卤素，CF 3，C 1-6 - 烷氧基，NO 2，CO 2 -C 1-6 - 烷基，甲基取代或被取代的苯基。 可以被卤素，CF 3，C 1-6 - 烷氧基，NO 2，CO 2 -C 1-6 - 烷基，甲基取代一次或多次的苄基; 吡啶基 或环己基; R 3苯基，其未被取代或被卤素，CF 3，C 1-6 - 烷氧基，NO 2，CO 2 -C 1-6烷基，甲基取代一次或多次; 可以被卤素，CF 3，C 1-6 - 烷氧基，NO 2，CO 2 -C 1-6 - 烷基，甲基取代一次或多次的萘基; 吡啶基 C 1-6不饱和烷基; 呋喃基 R4是H，C1-6烷基或苄基; 或一起形成 R'和R“各自为氢或一起形成额外的苯并环; 并且其中虚线表示指定为α和β的两个碳原子之间的任选的额外键或其药学上可接受的加成盐。 这些化合物可用作药物，例如用于治疗脑细胞中的Ca超载。