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    Mycrocycles useful in the teatment of Alzheimer's disease
    1.
    发明申请
    Mycrocycles useful in the teatment of Alzheimer's disease 失效
    可用于阿尔茨海默病的咪唑类

    公开(公告)号：US20030236199A1

    公开(公告)日：2003-12-25

    申请号：US10171182

    申请日：2002-06-12

    发明人： Shon R. Pulley ,  James P. Beck ,  Ruth E. TenBrink

    IPC分类号： A61K038/12 ,  C07D267/22 ,  C07D281/18

    CPC分类号： C07D413/12 ,  C07D273/02

    摘要： The present invention are macrocycles of the formula (IX): 1 for treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

    摘要翻译： 本发明是式（Ⅸ）的大环化合物：用于治疗阿尔茨海默病和其它类似疾病。 这些化合物包括β-分泌酶的抑制剂，其可用于治疗阿尔茨海默病和以哺乳动物中Aβ肽沉积为特征的其它疾病。 本发明的化合物可用于降低Aβ肽形成的药物组合物和治疗方法。

    Antihypertensive lactams
    6.
    发明授权
    Antihypertensive lactams 失效
    抗高血压内酰胺

    公开(公告)号：US4347246A

    公开(公告)日：1982-08-31

    申请号：US263824

    申请日：1980-05-15

    申请人： John T. Suh ,  Bruce E. Williams ,  Jerry W. Skiles ,  Bernard Loev

    发明人： John T. Suh ,  Bruce E. Williams ,  Jerry W. Skiles ,  Bernard Loev

    IPC分类号： C07D277/06 ,  C07D279/12 ,  C07D281/06 ,  C07D513/04 ,  A61K31/55 ,  C07D281/04 ,  C07D281/18

    CPC分类号： C07D513/04 ,  C07D277/06 ,  C07D279/12 ,  C07D281/06

    摘要： A compound of the formula ##STR1## wherein: R.sub.1 is independently lower alkyl having from 1 to 6 carbon atoms, lower alkenyl having from 2 to 6 carbon atoms, lower alkynyl having from 2 to 6 carbon atoms, hydroxy, hydroxyalkyl, alkoxy, thio, thioalkyl, alkylmercapto, amino, aminoalkyl, alkylamino, nitro, cyano, alkanoyl, carboxy, carboxyalkyl, carbalkoxy, carbalkoxyalkyl, halogen, alkylsulfoxy, alkylsulfonyl, sulfonyl, sulfonamido, trifluoromethyl, or methylenedioxy, wherein the alkyl group in hydroxyalkyl, thioalkyl, aminoalkyl, carboxyalkyl, alkoxy, alkylmercapto, alkylsulfoxy, alkanoyl, carbalkoxy, and carbalkoxyalkyl has from 1 to 6 carbon atoms,n is an integer from 1 to 4 inclusive,R.sub.2 is selected from the group consisting of hydrogen and cycloalkyl, wherein the cycloalkyl group contains from 3 to 16 carbon atoms,R.sub.3 and R.sub.4 are hydrogen, andY is oxygen, sulphur, .dbd.NR.sub.1, .dbd.NOR.sub.1 or .dbd.N--NH.sub.2, R.sub.1 being the same as defined above.The compounds are useful as antihypertensives, and have angiotensin converting enzyme inhibitory activity.

    摘要翻译： 下式化合物其中：R 1独立地为具有1至6个碳原子的低级烷基，具有2至6个碳原子的低级烯基，具有2至6个碳原子的低级炔基，羟基，羟基烷基，烷氧基，硫代 ，烷基巯基，氨基，氨基烷基，烷基氨基，硝基，氰基，烷酰基，羧基，羧基烷基，烷氧基，烷氧基烷基，卤素，烷基磺酰氧基，烷基磺酰基，磺酰基，亚磺酰氨基，三氟甲基或亚甲二氧基，其中羟基烷基， ，羧基烷基，烷氧基，烷基巯基，烷基亚磺酰基，烷酰基，烷氧基和烷氧基烷基具有1至6个碳原子，n是1至4的整数，其中R 2选自氢和环烷基，其中环烷基包含 3至16个碳原子，R3和R4是氢，Y是氧，硫，= NR1，= NOR1或= N-NH2，R1与上述定义相同。 该化合物可用作抗高血压药，并具有血管紧张素转换酶抑制活性。

    Pyridopyrrolobenzheterocycles for combatting depression
    7.
    发明授权
    Pyridopyrrolobenzheterocycles for combatting depression 失效
    吡啶并吡唑并杂环用于对抗抑郁症

    公开(公告)号：US3914421A

    公开(公告)日：1975-10-21

    申请号：US35752873

    申请日：1973-05-07

    申请人： ENDO LAB

    发明人： RAJAGOPALAN PARTHASARATHI

    IPC分类号： C07D265/36 ,  C07D267/14 ,  C07D267/22 ,  C07D281/10 ,  C07D281/18 ,  C07D498/16 ,  C07D513/16 ,  A61K31/535

    CPC分类号： C07D267/14 ,  C07D265/36 ,  C07D267/22 ,  C07D281/10 ,  C07D281/18

    摘要： where X is O, S. S -> O, or SO2; n is 0 or 1; m is 0 or 1; the R''s are the same or different and are H or CH3, and one of them can be C2-C9 alkyl, phenyl, C7-C10 phenylalkyl, furyl, thienyl, pyridyl or substituted phenyl or phenylalkyl; when X is S, and m is 0, one R in the group -RCR- can be OCH3; when X is S and m is 1, the R in the group (CHR)mcan be OCH3; and R1is H, C1-C4 alkyl, C3-C5 alkenyl, C3-C5 alkynyl, C3-C6 cycloalkyl, C2-C4 alkoxycarbonyl, trifluoroacetyl, or substituted C1-C4 alkyl where the substituent is C3-C6 cycloalkyl, phenyl or substituted phenyl; and their pharmaceutically suitable salts. The compounds are useful as sedatives; some of them also exhibit antidepressant, antihypertensive and antibacterial activity. The compounds are prepared by cyclizing compounds of formula II

    wherein R2 is R1 or acyl. The latter compounds are prepared by reacting 4-piperidones with compounds of formula III in the presence of a reducing agent

    OR WITH COMPOUNDS OF FORMULA VI

    摘要翻译： 其中X是O，S.S-> O或SO2; n为0或1; m为0或1; 苯基，C7-C10苯基烷基，呋喃基，噻吩基，吡啶基或取代的苯基或苯基烷基;其中一个可以是C 2 -C 9烷基，苯基， 当X为S且m为0时，基团-RCR-中的一个R可为OCH 3; 当X为S且m为1时，基团（CHR）中的R可以是OCH 3; 和R 1为H，C 1 -C 4烷基，C 3 -C 5烯基，C 3 -C 5炔基，C 3 -C 6环烷基，C 2 -C 4烷氧基羰基，三氟乙酰基或取代的C 1 -C 4烷基，其中取代基为C 3 -C 6环烷基，苯基或取代苯基 ; 及其药学上合适的盐。 这些化合物可用作镇静剂; 其中一些还表现出抗抑郁，抗高血压和抗菌活性。