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    • 5. 发明授权
    • Aryloxy propyldiamines
    • 丙烯酰氧基丙基二胺
    • US4140779A
    • 1979-02-20
    • US687850
    • 1976-05-19
    • Jean-Marie FerlandReal R. LaliberteWilbur LippmannThomas A. Pugsley
    • Jean-Marie FerlandReal R. LaliberteWilbur LippmannThomas A. Pugsley
    • C07D295/092C07D295/13C07D295/12A61K31/455
    • C07D295/088C07D295/13
    • Disclosed herein are compounds of the formula ##STR1## in which Ar is l-naphthyl; R.sup.1 and R.sup.2 are either the same or different selected from the group consisting of hydrogen or lower alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are joined form a heterocyclic amine radical selected from the group consisting of 1-pyrrolidinyl, piperidine, morpholine and 4-(lower alkyl)-1-piperazinyl; and R.sup.3 and R.sup.4 are either the same or different selected from the group consisting of hydrogen or lower alkyl, or R.sup.3 and R.sup.4 together with the nitrogen to which they are joined represent a heterocyclic amine radical selected from the group consisting of 1-pyrrolidinyl, piperidino, morpholino and 4-(lower alkyl)-1-piperazinyl; or a therapeutically acceptable acid addition salt thereof. The compounds are antidepressant agents and methods for their preparation and use also are disclosed.
    • 本文公开的是其中Ar是1-萘基的式“IMAGE”1的化合物; R 1和R 2可以相同或不同,选自氢或低级烷基,或者R 1和R 2与它们所连接的氮原子一起形成杂环胺基,其选自1-吡咯烷基,哌啶 ,吗啉和4-(低级烷基)-1-哌嗪基; 并且R 3和R 4可以相同或不同,选自氢或低级烷基,或者R 3和R 4与它们所连接的氮一起代表杂环胺基,其选自1-吡咯烷基,哌啶子基 ,吗啉代和4-(低级烷基)-1-哌嗪基; 或其治疗上可接受的酸加成盐。 这些化合物是抗抑郁剂,并且也公开了它们的制备和使用方法。
    • 8. 发明授权
    • Reducing the incidence of gastrointestinal side effects during the
treatment of inflammatory conditions with antiinflammatory drugs
    • 在治疗炎性反应性药物的治疗条件期间减少胃肠道副作用的发生率
    • US3937801A
    • 1976-02-10
    • US378112
    • 1973-07-10
    • Wilbur Lippmann
    • Wilbur Lippmann
    • A61K31/405A61K31/415C07C405/00C07D309/12C07F9/40A61K31/19A61K31/40A61K31/61
    • C07C405/00A61K31/405A61K31/415C07D309/12C07F9/4018Y10S514/922
    • A method is disclosed for inhibiting and alleviating gastrointestinal side effects often encountered during therapy with antiinflammatory agents such as indomethacin, phenylbutazone, oxyphenylbutazone and the like. The method comprises the administration to a mammal receiving such therapy of a prostaglandin derivative of formula 1, ##SPC1##In whichA. W is C = O, X and Y each are single bonds, Z is either C = O, CHOH or C(CH.sub.3)OH, R.sup.1 and R.sup.2 each are hydrogen, R.sup.3 is (CH.sub.2).sub.3 CH.sub.3 and R.sup.4 is hydrogen or lower alkyl;B. W is CHOH, X and Y each are single bonds, Z is either CHOH or C(CH.sub.3)OH, R.sup.1 and R.sup.2 each are hydrogen, R.sup.3 is (CH.sub.2).sub.3 CH.sub.3 and R.sup.4 is hydrogen or lower alkyl;C. W is C = O, X is a single bond, Y is a trans double bond, Z is CH.sub.2, CHOH or C(CH.sub.3)OH, R.sup.1 and R.sup.2 each are hydrogen and R.sup.3 is (CH.sub.2).sub.3 CH.sub.3 and R.sup.4 is hydrogen or lower alkyl;D. W is C = O, X is a single bond, Y is a trans double bond, Z is CHOH, R.sup.1 and R.sup.2 each are hydrogen, R.sup.3 is cyclohexyl and R.sup.4 is hydrogen or lower alkyl;E. W is C = O, X is a cis double bond, Y is a trans double bond, Z is CHOH, or C(CH.sub.3)OH, R.sup.1 is hydrogen and R.sup.2 is hydrogen or methyl, R.sup.3 is (CH.sub.2).sub.3 CH.sub.3 and R.sup.4 is hydrogen or lower alkyl; orF. W is C = O, X is a cis double bond, Y is a trans double bond, Z is CHOH, R.sup.1 and R.sup.2 each are methyl, R.sup.3 is (CH.sub.2).sub.3 CH.sub.3 and R.sup.4 is hydrogen or lower alkyl.Also disclosed are useful pharmaceutical compositions for treating inflammatory conditions comprising a combination of a gastrointestinal side effect-inhibiting dose of the above prostaglandin derivative of formula 1 and a therapeutic dose of an antiinflammatory agent.