5-[1-Hydroxy-2-(substituted-amino)]ethyl-8-hydroxycarbostyril derivatives
    7.
    发明授权
    5-[1-Hydroxy-2-(substituted-amino)]ethyl-8-hydroxycarbostyril derivatives 失效
    5- {8-羟基-2-(取代的 - 氨基){9乙基-8-羟基卡波特他尔衍生物

    公开(公告)号:US4022776A

    公开(公告)日:1977-05-10

    申请号:US536705

    申请日:1974-12-26

    摘要: 5-[Hydroxy-2-(substituted-amino)]ethyl-8-hydroxy-carbostyril derivatives represented by the formula (I) ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an aralkyl group containing a straight or branched chain alkyl moiety having 1 to 4 carbon atoms or a cycloalkyl group having 4 to 6 carbon atoms, or R.sup.1 and R.sup.2 may, when taken together with the nitrogen atom to which they are attached, form a 5 or 6-membered substituted or unsubstituted heterocyclic ring containing 1 or 2 nitrogen, oxygen or sulfur atoms as hetero atoms, the pharmaceutically acceptable acid addition salts thereof and a process for preparing the above compounds.

    摘要翻译: 由式(I)表示的5- [羟基-2-(取代 - 氨基)]乙基-8-羟基喹诺酮衍生物其中R1和R2可以相同或不同,各自表示 氢原子,具有1至4个碳原子的烷基,含有1至4个碳原子的直链或支链烷基部分或具有4至6个碳原子的环烷基的芳烷基,或者R 1和R 2可以一起 与它们所连接的氮原子形成5或6元取代或未取代的杂环,该杂环含有1或2个氮原子,氧原子或硫原子作为杂原子,其药学上可接受的酸加成盐及其制备方法 化合物。

    N,N'-bis-[(.beta.-hydroxy-.beta.-phenyl)-ethyl]-polymethylenediamines
and salts thereof
    8.
    发明授权
    N,N'-bis-[(.beta.-hydroxy-.beta.-phenyl)-ethyl]-polymethylenediamines and salts thereof 失效
    N,N {40-双 - {8({62-羟基 - {62-苯基) - 乙基{9-聚亚甲基二胺及其盐

    公开(公告)号:US4021485A

    公开(公告)日:1977-05-03

    申请号:US628819

    申请日:1975-11-04

    摘要: Compounds of the formula ##STR1## WHEREIN R.sub.1 is hydrogen or methyl, m is 0 or an integer from 1 to 8, inclusive, andAr is ##STR2## WHERE R is hydrogen or acyl, andR.sub.2 is hydrogen or --OR, as defined above, ##STR3## WHERE R has the meanings defined above, andR.sub.3 is hydroxy-lower alkyl, --NH--CO--R.sub.4, --NH--SO.sub.2 --R.sub.5, --CH.sub.2 --NH--CO--R.sub.4, --CH.sub.2 --NH--SO.sub.2 --R.sub.5 or --CH.sub.2 --NH--CO--NH--R.sub.4, whereR.sub.4 is hydrogen or lower alkyl, andR.sub.5 is lower alkyl or di-lower alkyl-amino, ##STR4## WHERE R.sub.6 is hydrogen, amino or hydroxyl,X is chlorine or bromine, andY is hydrogen, chlorine or bromine or ##STR5## WHERE R has the meanings defined above, andA is a saturated or unsaturated 5- to 6-membered ring,And their non-toxic, pharmacologically acceptable acid addition salts; the compounds as well as their salts are useful as bronchospasmolytics, uterine spasmolytics, antipruritics and antiallergics.

    摘要翻译: 式(Ⅰ)化合物其中R 1为氢或甲基,M为0或整数1至8,包含和Ar为(a)R为氢或酰基,R 2为氢 或-OR,如上所定义,(b)其中R具有上述定义,并且R 3是羟基 - 低级烷基,-NH-CO-R 4,-NH-SO 2 -R 5,-CH 2 -NH-CO -R4,-CH2-NH-SO2-R5或-CH2-NH-CO-NH-R4,其中R4是氢或低级烷基,R5是低级烷基或二 - 低级烷基 - 氨基,(c) 其中R6是氢,氨基或羟基,X是氯或溴,Y是氢,氯或溴。(d)其中R具有上述定义,A是饱和或不饱和的5-至6- 及其非毒性,药理学上可接受的酸添加剂; 化合物作为其作为BRONCHOSPASMOLYTICS,UTERINE SPASMOLYTICS,ANTIPRITICS和ANTIALLERGICS的有用的化合物。

    2-Amino-1,4-dihydropyridine derivatives

    公开(公告)号:US3971790A

    公开(公告)日:1976-07-27

    申请号:US574347

    申请日:1975-05-05

    摘要: 2-Amino-1,4-dihydropyridines bearing a carbonyl function in the 5-position and being optionally substituted by lower alkyl or phenyl in the 6-position, and the corresponding 2-amino-1,4,5,6,7,8-hexahydro-5-oxoquinolines, which derivatives are further substituted by a carbonyl group in the 3-position and optionally substituted in the 4-position by lower alkyl, phenyl, substituted phenyl or a heterocyclic group are antihypertensive agents and coronary vessel dilators. The compounds, of which 2-amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3,5-diethyl ester is a representative embodiment, are prepared through condensation of an ylideneacetoacetic acid ester and an amidine.CROSS REFERENCEThis is a division of Ser. No. 438,603 filed Feb. 1, 1974, now U.S. Pat. No. 3,929,798, which in turn is a division of Ser. No. 336,639 filed Feb. 28, 1973, now U.S. Pat. No. 3,867,393.