Polycyclic compounds
    2.
    发明授权
    Polycyclic compounds 失效
    多环化合物

    公开(公告)号:US4322370A

    公开(公告)日:1982-03-30

    申请号:US877303

    申请日:1978-02-13

    申请人: Derek V. Gardner

    发明人: Derek V. Gardner

    摘要: Compounds of the formula (II): ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is phenyl or naphthyl or substituted phenyl or naphthyl group; R.sub.2 is: ##STR2## wherein R.sub.5 is hydrogen or C.sub.1-6 alkyl, R.sub.6 is hydrogen or C.sub.1-6 alkyl, phenyl, tolyl or benzyl and R.sub.7 is hydrogen; R.sub.3 and R.sub.4 are each hydrogen atom or C.sub.1-4 alkyl, and X is CO, CHOH, CHCI or C.dbd.C R.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 are each hydrogen or C.sub.1-4 alkyl; or CR.sub.10 OH or CHR.sub.10, wherein R.sub.10 is C.sub.1-4 alkyl, have been found to be mood-modifying agents and anorexic agents.

    摘要翻译: 式(II)化合物:其中R 1为苯基或萘基或取代的苯基或萘基; R2是:其中R5是氢或C1-6烷基,R6是氢或C1-6烷基,苯基,甲苯基或苄基,R7是氢; R3和R4各自为氢原子或C1-4烷基,X为CO,CHOH,CHCl或C = C R8 R9,其中R8和R9各自为氢或C1-4烷基; 或其中R 10为C 1-4烷基的CR 10 OH或CHR 10已经被发现是情绪调节剂和厌食剂。

    Process of making nadolol
    3.
    发明授权
    Process of making nadolol 失效
    制作纳多洛尔的过程

    公开(公告)号:US5319141A

    公开(公告)日:1994-06-07

    申请号:US675907

    申请日:1991-05-20

    CPC分类号: C07C213/08 C07C217/38

    摘要: A process for making 5-(d-3-(tert-butylamino)-2-hydroxypropoxy)-1,2,3,4-tetrahydro-1-cis-2,3 naphthalenediol of the formula ##STR1## by reacting ##STR2## in an essentially water free environment with (a) M'IO.sub.3 wherein M' represents a suitable ion for forming the salt.(b) I.sub.2 (iodine)(c) CH.sub.3 COO.sup.- M".sup.+ wherein M" represents a suitable ion for forming the salt(d) glacial acetic acid and(e) ROH/M'"OH where R is alkyl and M'" is a suitable metal ion.

    摘要翻译: PCT No.PCT / CA90 / 00316 Sec。 371日期1991年5月20日 102(e)日期1991年5月20日PCT提交1990年9月25日PCT公布。 出版物WO91 / 04244 日期:1991年4月4日。一种制备式(I)的5-(d-3-(叔丁基氨基)-2-羟基丙氧基)-1,2,3,4-四氢-1-顺式-2,3-萘二醇的方法 (I)通过使基本上不含水的环境中的(II)与(a)M'IO3反应,其中M'表示用于形成盐的合适的离子。 (b)I2(碘)(c)CH3COO-M“+其中M”表示形成盐的合适离子(d)冰醋酸和(e)ROH / M“OH,其中R是烷基, M“'是合适的金属离子。

    Spiro substituted indanones and tetralones
    4.
    发明授权
    Spiro substituted indanones and tetralones 失效
    螺环取代的茚满酮和四氢萘酮

    公开(公告)号:US4322437A

    公开(公告)日:1982-03-30

    申请号:US795439

    申请日:1977-05-10

    摘要: The present invention relates to a compound of formula I, ##STR1## wherein A is straight chain alkylene of 2 to 4 carbon atoms, or straight chain alkenylene of 2 to 4 carbon atoms,n is 1, 2 or 3,R is hydrogen or halogen of atomic number from 9 to 35, andeither (i) R.sub.1 is a group of formula II, ##STR2## wherein R.sub.2 and R.sub.3, independently, are hydrogen or alkyl of 1 to 4 carbon atoms, andR.sub.4 is alkyl of 1 to 4 carbon atoms, alkoxyalkyl of 2 to 5 carbon atoms, alkylthioalkyl of 2 to 5 carbon atoms, phenylalkyl or phenoxyalkyl or phenylthioalkyl, wherein the alkyl moiety has from 1 to 3 carbon atoms, or phenyl, the phenyl ring of each of the last four radicals being unsubstituted or mono-substituted by, or disubstituted independently by, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, hydroxy or halogen of atomic number from 9 to 35, andR.sub.5 is hydrogen,or (ii) R.sub.1 and R.sub.5 together with the nitrogen atom to which they are bound are (a) 2,2,6,6-tetramethylpiperidinyl, (b) 2,2,5,5-tetramethylpyrrolidinyl,or (c) piperazinyl substituted in the 4 position by alkyl of 1 to 4 carbon atoms or phenyl which is unsubstituted, or mono-substituted by, or di-or tri-substituted independently by, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, or halogen of atomic number from 9 to 35,useful as anti-hypertensives.

    摘要翻译: 本发明涉及式Ⅰ化合物,其中A为2至4个碳原子的直链亚烷基或2至4个碳原子的直链亚烯基,n为1,2或3,R为氢 或原子序数为9至35的卤素,和(i)R 1是式II,其中R 2和R 3独立地是氢或1-4个碳原子的烷基,R 4是 1至4个碳原子,2至5个碳原子的烷氧基烷基,2至5个碳原子的烷硫基烷基,苯基烷基或苯氧基烷基或苯硫基烷基,其中烷基部分有1至3个碳原子,或苯基, 最后四个基团是未取代的或被1至4个碳原子的烷基,1至4个碳原子的烷氧基单独取代或原子数为9至35的羟基或卤素单取代,R5为氢或( ii)R 1和R 5与它们所连接的氮原子一起是(a)2,2,6,6-四甲基哌啶基,(b)2,2, 或(c)在4位上被1至4个碳原子的烷基取代的哌嗪基或未被取代的或被1或2的烷基独立地被二取代或二取代或三取代的苯基取代的哌嗪基 4个碳原子,1至4个碳原子的烷氧基或9至35个原子序数的卤素,可用作抗高血压药。