利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

67 条记录 (耗时 0.033 秒)

    Bicyclic amides as inhibitors of acyl-coenzyme A: cholesterol acyl transferase
    5.
    发明授权
    Bicyclic amides as inhibitors of acyl-coenzyme A: cholesterol acyl transferase 失效
    作为酰基辅酶A：胆固醇酰基转移酶的抑制剂的双环酰胺

    公开(公告)号：US5416118A

    公开(公告)日：1995-05-16

    申请号：US122537

    申请日：1993-09-28

    申请人： John W. Clader ,  Thomas Fevig ,  Wayne Vaccaro ,  Joel G. Berger

    发明人： John W. Clader ,  Thomas Fevig ,  Wayne Vaccaro ,  Joel G. Berger

    IPC分类号： C07C233/11 ,  C07C233/23 ,  C07C275/24 ,  C07D213/40 ,  A61K31/165 ,  A61K31/35 ,  A61K31/44

    CPC分类号： C07D213/40 ,  C07C233/11 ,  C07C233/23 ,  C07C275/24 ,  C07C2102/08 ,  C07C2102/10 ,  C07C2102/12

    摘要： Novel bicyclic amides of the formula ##STR1## wherein Ar.sup.1 and Ar.sup.2 are phenyl, R.sup.2 -substituted phenyl, heteroaryl or R.sup.2 -substituted heteroaryl, wherein R.sup.2 is 1 to 3 substituents independently selected from the group consisting of halogeno, hydroxy, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino and lower dialkylamino;X, Y and Z are --CH.sub.2 --, --CH(alkyl)--, --C(alkyl).sub.2 --, --NH--, --N(alkyl)--, --O-- or --SO.sub.r, wherein r is 0, 1 or 2, and m, n and p are 0 or 1;R.sup.1 is an alkyl chain of 1 to 25 carbon atoms; an alkyl chain substituted by one or more optionally substituted phenyl or heteroaryl groups; an alkyl chain --O--, --SO.sub.r, phenylene, R.sup.2 -substituted phenylene, heteroarylene or R.sup.2 -substituted heteroarylene groups; an interrupted alkyl chain substituted by one or more optionally substituted phenyl or heteroaryl groups; an alkyl chain of 4 to 25 carbon atoms, interrupted by one or more --NH--, --C(O)-- or --N(lower alkyl)-- groups; an interrupted alkyl chain of 4 to 25 carbon atoms substituted by one or more phenyl, R.sup.2 -substituted phenyl, heteroaryl or R.sup.2 -substituted heteroaryl groups; a diphenylamino group; a di-(R.sup.2 -substituted phenyl)amino group; a diheteroarylamino group; or a di-(R.sup.2 -substituted heteroaryl)amino group;or a pharmaceutically acceptable salt thereof, useful in the treatment of artherosclerosis are disclosed.

    摘要翻译： PCT No.PCT / US92 / 02662 Sec。 371日期：1993年9月28日 102（e）日期1993年9月28日PCT提交1992年4月9日PCT公布。 第WO92 / 18462号公报 日期：1992年10月29日。式IMA IMA的新型双环酰胺其中Ar 1和Ar 2是苯基，R 2取代的苯基，杂芳基或R 2取代的杂芳基，其中R 2是1至3个独立地选自卤代 ，羟基，低级烷基，低级烷氧基，硝基，氨基，低级烷基氨基和低级二烷基氨基; X，Y和Z是-CH 2 - ， - CH（烷基） - ， - C（烷基）2 - ， - NH - ， - N（烷基） - ， - O-或-SOr，其中r是0,1或 2，m，n和p为0或1; R1是1〜25个碳原子的烷基链; 被一个或多个任选取代的苯基或杂芳基取代的烷基链; 烷基链-O-，-SOr，亚苯基，R 2取代的亚苯基，亚杂芳基或R 2取代的亚杂芳基; 被一个或多个任选取代的苯基或杂芳基取代的间断烷基链; 4个至25个碳原子的烷基链，被一个或多个-NH-，-C（O） - 或-N（低级烷基）基团间隔; 被一个或多个苯基，R 2取代的苯基，杂芳基或R 2取代的杂芳基取代的具有4至25个碳原子的中断的烷基链; 二苯基氨基; 二（R 2取代苯基）氨基; 二杂芳基氨基; 或二（R 2取代的杂芳基）氨基; 或其药学上可接受的盐，其可用于治疗动脉粥样硬化。

    4,5-bridged-2,3,4,5-tetrahydro-1H-3-benzazepine-7-ols and derivatives and compositions and methods employing such compounds
    7.
    发明授权
    4,5-bridged-2,3,4,5-tetrahydro-1H-3-benzazepine-7-ols and derivatives and compositions and methods employing such compounds 失效
    4,5桥连-2,3,4,5-四氢-1H-3-苯并氮杂-7-醇及其衍生物和组合物和方法

    公开(公告)号：US5362728A

    公开(公告)日：1994-11-08

    申请号：US915710

    申请日：1992-07-29

    申请人： Theodros Asberom ,  Edward O'Connor ,  Joel G. Berger ,  John W. Clader

    发明人： Theodros Asberom ,  Edward O'Connor ,  Joel G. Berger ,  John W. Clader

    IPC分类号： A61K31/55 ,  A61P25/04 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  A61P25/30 ,  C07D223/18 ,  C07D223/32

    CPC分类号： C07D223/18 ,  C07D223/32

    摘要： Novel benzazepines of the formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R represents H, alkyl, allyl or ##STR2## A represents --[CR.sup.1 R.sup.2].sub.n --; n represents 3 or 4; R.sup.1 and R.sup.2 may be the same or different and each independently represents H, OH, atkyl, alkoxy, phnenyl or substituted phenyl, with the proviso that R.sup.1 and R.sup.2 on the same carbon atom are not both OH, or R.sup.1 and R.sup.2 on the same carbon atom together represent=O;G represents H, R.sup.3 (CO)-- or ArNHCO--;R.sup.3 represents H, alkyl, alkoxy, phenyl or substituted phenyl;Ar represents phenyl or substituted phenyl; andY and Z may be the same or different and each is independently selected from H, halo, alkyl, alkoxy or halpalkyl;the pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, useful in the treatment of psychoses, drug dependence, D1 dependent neurological disorder or pain are disclosed.

    摘要翻译： PCT No.PCT / US91 / 00503 Sec。 371日期：1992年7月29日 102（e）日期1992年7月29日PCT PCT 1991年1月31日PCT。式I的新的苯并氮杂：其中R表示H，烷基，烯丙基或A表示 - [CR1R2] n- n表示3或4; R1和R2可以相同或不同，并且各自独立地表示H，OH，烷基，烷氧基，苯基或取代的苯基，条件是相同碳原子上的R 1和R 2不同时为OH，或者R 1和R 2在同一个上 碳原子一起代表= O; G表示H，R 3（CO） - 或ArNHCO-; R 3表示H，烷基，烷氧基，苯基或取代的苯基; Ar表示苯基或取代的苯基; 并且Y和Z可以相同或不同，并且各自独立地选自H，卤素，烷基，烷氧基或卤代烷基; 公开了可用于治疗精神病，药物依赖性，D1依赖性神经障碍或疼痛的药学上可接受的盐及其药物组合物。

    Process for the enantiospecific synthesis of intermediates for hexahydro-benzo[d]-naphtho[2,1-b]azepines
    8.
    发明授权
    Process for the enantiospecific synthesis of intermediates for hexahydro-benzo[d]-naphtho[2,1-b]azepines 失效

    公开(公告)号：US5091526A

    公开(公告)日：1992-02-25

    申请号：US635535

    申请日：1991-01-08

    申请人： Joel G. Berger ,  John W. Clader

    发明人： Joel G. Berger ,  John W. Clader

    IPC分类号： C07C209/28 ,  C07C209/70 ,  C07C211/42 ,  C07C213/08 ,  C07C217/74 ,  C07D223/14

    CPC分类号： C07C209/70 ,  C07C209/28 ,  C07C211/42 ,  C07C213/08 ,  C07C217/74 ,  C07D223/14 ,  C07C2102/10

    摘要： Biologically active, enantiomerically substantially pure intermediates of trans-hexahydro-benzo[d]naphtho[2,1-b]azepines are prepared.The present invention involves a process for preparing compounds of the general formula 3: ##STR1## wherein: R* is ##STR2## Each R.sup.1 is independently H or alkyl; Q is methylene, --O-- or --S--;m and n are independently variable and may each have a value of 0, 1 or 2, with the provisos that the sum of m and n is not greater than 3, that m may not equal zero when Q is --O-- or --S--, and that when Q is --CH.sub.2 --, m and n cannot both be zero;X is hydrogen, halo, alkyl, alkylthio, alkylsulfinyl, alkylsufonyl, hydroxy, alkoxy or trifluoromethyl;Y is hydrogen, hydroxy, alkoxy, --OC(O)NR.sup.2 R.sup.3, --OC(O)--R.sup.9, --N(R.sup.1).sub.2, --NHC(O)R.sup.1 or --OP(O)(OH)OR.sup.1,R.sup.2 and R.sup.3 are the same or different and each is hydrogen (provided that both are not hydrogen), alkyl, aralkyl, cycloalkyl, aryl, hydroxyalkyl, or alkoxyalkyl;in addition, when one of R.sup.2 and R.sup.3 is as defined above, the other may be --R.sup.4 NR.sup.5 R.sup.6 {wherein R.sup.4 is alkanediyl, R.sup.5 is hydrogen or alkyl and R.sup.6 is alkyl, or R.sup.5 and R.sup.6 together with the nitrogen atom form a 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl, 1-(4-alkylpiperazinyl), 4-morpholinyl or 1-(hexahydroazepinyl) group};in further addition, R.sup.2 and R.sup.3 together with the nitrogen atom may form a 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 1-(4-alkylpiperazinyl), 1-(4-alkoxyalkylpiperazinyl), 1-(4-hydroxyalkylpiperazinyl), 1-(3-hydroxyazetidinyl), 1-(3-alkoxyazetidinyl), 1-(-hydroxypyrrolidinyl), 1-(3-alkoxypyrrolidinyl), 1-(3- or 4-hydroxypiperidinyl), 1-(3- or 4-alkoxypiperidinyl), 1-(4-oxopiperidinyl) or 1-(3-oxopyrrolidinyl) ring;in still further addition, when R.sup.2 is hydrogen, R.sup.3 may be --CHR.sup.7 CO.sub.2 R.sup.8, wherein R.sup.7 and R.sup.8 are the same or different and each is hydrogen, alkyl or aralkyl;R.sup.9 is alkyl, aralkyl, aryl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, cycloalkylalkyl, alkoxycarbonylalkyl, cycloalkyl, 1-adamantyl, cycloalkoxyalkyl, alkoxy, aralkyloxy, cycloalkoxy, aryloxy or --CHR.sup.7 NHR.sup.8 ; andZ is X as defined above, amino, alkylamino or --NHC(O)R.sup.10 {wherein R.sup.10 is hydrogen, alkyl or aryl}.R.sup.11 is H or alkyl;R.sup.12 is alkylwith the proviso that R.sup.11 and R.sup.12 are different, and K is hydrogen, alkoxy, hydroxyl, aryloxy or alkyl.

    Substituted N-Arylsulfonylheterocyclic Amines As Gamma-Secretase Inhibitors
    10.
    发明申请
    Substituted N-Arylsulfonylheterocyclic Amines As Gamma-Secretase Inhibitors 失效
    取代的N-芳基磺酰基杂环胺作为γ-分泌酶抑制剂

    公开(公告)号：US20100093695A1

    公开(公告)日：2010-04-15

    申请号：US12633311

    申请日：2009-12-08

    申请人： Hubert B. Josien ,  John W. Clader ,  Thomas A. Bara ,  Ruo Xu ,  Hongmei Li ,  Dmitri A. Pissarnitski ,  Zhiqiang Zhao

    发明人： Hubert B. Josien ,  John W. Clader ,  Thomas A. Bara ,  Ruo Xu ,  Hongmei Li ,  Dmitri A. Pissarnitski ,  Zhiqiang Zhao

    IPC分类号： A61K31/438 ,  C07D413/14 ,  A61K31/5377 ,  C07D413/12 ,  C07D487/04 ,  A61K31/55 ,  A61K31/551

    CPC分类号： C07D265/30 ,  C07D413/12 ,  C07D451/02 ,  C07D487/08

    摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: L is —O—, —N(R6)—, —S—, —S(O)—, or —S(O2)—; R1 is selected from the group consisting of aryl and heteroaryl; R2 is selected from the group consisting of alkyl, —C(O)—Y, —X—C(O)—Y, -alkylene-X—C(O)—Y, -alkylene-C(O)—Y, -alkylene-cycloalkylene-X—C(O)—Y, -alkylene-cycloalkylene-C(O)—Y, -cycloalkylene-alkylene-X—C(O)—Y, -cycloalkylene-alkylene-C(O)—Y, -cycloalkylene-X—C(O)—Y, -cycloalkylene-C(O)—Y, -alkylene-cycloalkylene-alkylene-X—C(O)—Y, -alkylene-cycloalkylene-alkylene-C(O)—Y, aryl, and heteroaryl; R3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R4 and R5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of —NR8R9, —N(R6)—(CH2)b—NR8R9, aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, and arylheterocycloalkyl; or Y is selected from the group consisting of: One or more compounds of formula I, or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

    摘要翻译： 本发明公开了下式的新型γ-分泌酶抑制剂：其中：L是-O - ， - N（R6） - ， - S - ， - S（O） - 或-S（O 2） - ; R 1选自芳基和杂芳基; R 2选自烷基，-C（O）-Y，-X-C（O）-Y， - 亚烷基-X-C（O）-Y， - 亚烷基-C（O）-Y， - 亚烷基 - 亚环烷基-X-C（O）-Y-亚烷基 - 亚环烷基-C（O）-Y-亚烷基 - 亚烷基-X-C（O）-Y-亚烷基 - 亚烷基-C（O） （O）-Y-亚烷基-C（O）-Y-亚烷基 - 亚环烷基 - 亚烷基-X-C（O）-Y-亚烷基 - 亚环烷基 - 亚烷基-C（O ）-Y，芳基和杂芳基; R 3选自芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基，芳基杂环烷基和烷氧基烷基; 每个R 4和R 5独立地选自H和烷基; 并且Y选自-NR 8 R 9，-N（R 6） - （CH 2）b -NR 8 R 9，芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基和芳基杂环烷基。 或Y选自：一种或多种式I化合物或包含该化合物的制剂可用于，例如， 治疗阿尔茨海默病。