Tricyclic heterocyclic compound
    5.
    发明授权
    Tricyclic heterocyclic compound 失效
    三环杂环化合物

    公开(公告)号:US5563169A

    公开(公告)日:1996-10-08

    申请号:US204420

    申请日:1994-07-06

    摘要: ConstitutionTricyclic heterocyclyl compounds having a general formula (I): ##STR1## wherein: R.sup.1 and R.sup.2 each represents H, a lower alkyl or lower alkoxy group, a halogen atom or halogeno-lower alkyl; R.sup.3 represents H or a lower alkyl group; R.sup.4 represents a substituted phenyl or naphthyl group; R.sub.5 represents H or a lower alkyl group; A represents a lower alkylene group; B represents an --O-- or --S-- group; and n is 0-1.EffectThe compounds have an excellent activity in the inhibition of acyl-CoA: cholesterol acyltransferase (ACAT) and are useful for the treatment and prophylaxis of atherosclerosis.

    摘要翻译: PCT No.PCT / JP92 / 01164 Sec。 371日期:1994年7月6日 102(e)日期1994年7月6日PCT提交1992年9月11日PCT公布。 出版物WO93 / 03740 日期:1993年4月3日构造具有通式(I)的三环杂环基化合物:其中:R1和R2各自表示H,低级烷基或低级烷氧基,卤素原子或卤代低级烷基; R3代表H或低级烷基; R4表示取代的苯基或萘基; R5代表H或低级烷基; A表示低级亚烷基; B表示-O-或-S-基; n为0-1。 作用该化合物在酰基辅酶A:胆固醇酰基转移酶(ACAT)的抑制中具有优异的活性,可用于治疗和预防动脉粥样硬化。

    Silyl enol ether alkylation process
    7.
    发明授权
    Silyl enol ether alkylation process 失效
    甲硅烷基烯醇醚烷基化方法

    公开(公告)号:US5719275A

    公开(公告)日:1998-02-17

    申请号:US460546

    申请日:1995-06-02

    摘要: A method for preparing compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen or a hydroxy-protecting group; R.sup.2 is alkyl, alkoxy, halogen, optionally substituted phenyl or optionally substituted phenoxy; R.sup.3 is optionally substituted pyridyl, optionally substituted quinolyl or phenyl group which has a substituent of formula --CYNR.sup.5 R.sup.6, where Y is oxygen or sulfur, and R.sup.5 and R.sup.6 are each alkyl, aryl or aralkyl, or R.sup.5 and R.sup.6 and the nitrogen to which they are attached together form a heterocyclic group; R.sup.4 is hydrogen or an amino-protecting group; and Z is sulfur or oxygen. The process comprises reacting a compound of formula (II): ##STR2## in which R.sup.8, R.sup.9 and R.sup.10 are the same or different and each represents an alkyl group having from 1 to 4 carbon atoms or a phenyl group, with a compound of formula (III): ##STR3## in which R.sup.11 represents an acyloxy, alkylsulfonyl, arylsulfonyl, alkylsulfinyl or arylsulfinyl group.

    摘要翻译: 制备式(I)化合物的方法:其中:R1是氢或羟基保护基; R 2是烷基,烷氧基,卤素,任选取代的苯基或任选取代的苯氧基; R3是任选取代的吡啶基,任选取代的具有式-CYNR 5 R 6的取代基的喹啉基或苯基,其中Y是氧或硫,R 5和R 6各自是烷基,芳基或芳烷基,或者R 5和R 6以及它们 一起形成杂环基; R4是氢或氨基保护基; Z是硫或氧。 该方法包括使式(II)化合物:其中R 8,R 9和R 10相同或不同并且各自表示具有1至4个碳原子的烷基或苯基的式(II)化合物与 式(III)化合物:其中R 11表示酰氧基,烷基磺酰基,芳基磺酰基,烷基亚磺酰基或芳基亚磺酰基。

    Carbapenem
    8.
    发明授权
    Carbapenem 失效
    卡巴培南

    公开(公告)号:US5614624A

    公开(公告)日:1997-03-25

    申请号:US460209

    申请日:1995-06-02

    摘要: A compound of the formula ##STR1## in which: R.sup.1' is hydrogen or a carboxy-protecting group;R.sup.41' is hydrogen or a hydroxy-protecting group;R.sup.42' is a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy, a halogen, an aryl or an aryloxy; R.sup.43' is hydrogen, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy, a hydroxy, a halogen, a cyano, a nitro or a group of the formula --NR.sup.8' R.sup.9', where R.sup.8' and R.sup.9' are independently selected from the group consisting of hydrogen, amino-protecting groups, C.sub.1 -C.sub.6 alkyl groups and phenyl groups, or R.sup.8' and R.sup.9' together represent a group --(CH.sub.2).sub.q '--O.sub.r '--(CH.sub.2).sub.s '--, where q' and s' are independently 0 or an integer of from 1 to 5 and r' is 0 or 1, provided that (q'+s') is an integer of at least 2; R.sup.45' and R.sup.46' are independently selected from the group consisting of C.sub.1 -C.sub.6 alkyl groups and aryl groups, or R.sup.45' and R.sup.46' together represent a group --(CH.sub.2).sub.q '--O.sub.r '--(CH.sub.2).sub.s '--, where q' and s' are independently 0 or an integer of from 1 to 5 and r' is 0 or 1; Y' is oxygen or sulfur; and j' is 0, 1 or 2.

    摘要翻译: 式(IV')的化合物,其中:R1'是氢或羧基保护基; R 41'是氢或羟基保护基; R 42'是C 1 -C 6烷基,C 1 -C 6烷氧基,卤素,芳基或芳氧基; R 43'是氢,C 1 -C 6烷基,C 1 -C 6烷氧基,羟基,卤素,氰基,硝基或式-NR 8'R 9'基团,其中R 8'和R 9'独立地选自 由氢,氨基保护基,C 1 -C 6烷基和苯基组成的组,或者R 8'和R 9'一起表示基团 - (CH 2)q'-Or' - (CH 2)s',其中q' 和s'独立地为0或1至5的整数,r'为0或1,条件是(q'+ s')为至少2的整数; R 45'和R 46'独立地选自C 1 -C 6烷基和芳基,或者R 45'和R 46'一起表示基团 - (CH 2)q'-Or' - (CH 2)s - ,其中 q'和s'独立地为0或1至5的整数,r'为0或1; Y'是氧或硫; 并且j'为0,1或2。