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222 条记录 (耗时 0.015 秒)

    N-(4-Pyrazolidinyl)benzamides and their amino precursors
    21.
    发明授权
    N-(4-Pyrazolidinyl)benzamides and their amino precursors 失效
    N-（4-吡唑烷基）苯甲酰胺及其氨基前体

    公开(公告)号：US4207327A

    公开(公告)日：1980-06-10

    申请号：US41461

    申请日：1979-05-22

    申请人： Carl D. Lunsford ,  Albert D. Cale, Jr.

    发明人： Carl D. Lunsford ,  Albert D. Cale, Jr.

    IPC分类号： C07D231/04 ,  A61K31/415

    CPC分类号： C07D231/04 ,  Y10S514/872

    摘要： N-(4-Pyrazolidinyl)benzamides having the formula ##STR1## and their amino precursors are disclosed wherein R is lower alkyl, lower cycloalkyl or phenyllower-alkyl; R.sup.1 is lower alkyl, lower cycloalkyl, or phenyllower-alkyl; R.sup.2 is hydrogen, lower alkyl or phenyl; R.sup.3 is hydroxy, cyano, nitro, amino, fluoro, chloro, bromo, trifluoromethyl, lower alkyl, lower alkoxy, sulfamoyl or actamido, R.sup.3 can be the same radical or different radicals; n is an integer from zero to three inclusive, and pharmaceutically acceptable acid addition salts thereof. The compounds have anti-emetic and gastric emptying properties.

    摘要翻译： 公开了具有式“IMAGE”的N-（4-吡唑烷基）苯甲酰胺及其氨基前体，其中R是低级烷基，低级环烷基或苯基低级烷基; R1是低级烷基，低级环烷基或苯基低级烷基; R2是氢，低级烷基或苯基; R3是羟基，氰基，硝基，氨基，氟，氯，溴，三氟甲基，低级烷基，低级烷氧基，氨磺酰基或酰胺基，R3可以是相同的基团或不同的基团; n为0〜3的整数，和其药学上可接受的酸加成盐。 该化合物具有抗呕吐和胃排空的特性。

    Antimotion sickness remedy
    23.
    发明授权
    Antimotion sickness remedy 失效
    抗疟药补救

    公开(公告)号：US4070463A

    公开(公告)日：1978-01-24

    申请号：US663407

    申请日：1976-03-03

    申请人： Ashton Graybiel

    发明人： Ashton Graybiel

    IPC分类号： A61K31/54 ,  A61K31/135

    CPC分类号： A61K31/54 ,  Y10S514/872

    摘要： A pharmaceutical composition for the prevention of motion sickness which prises two parts of promethazine hydrochloride and one part of 1-ephedrine sulfate.

    摘要翻译： 一种用于预防晕车的药物组合物，其包含两部分盐酸异丙嗪和一部分1-麻黄碱硫酸盐。

    Pyrazine derivatives
    24.
    发明授权
    Pyrazine derivatives 失效
    吡嗪衍生物

    公开(公告)号：US4041032A

    公开(公告)日：1977-08-09

    申请号：US534636

    申请日：1974-12-19

    申请人： Masuo Murakami ,  Kozo Takahashi ,  Yasuhumi Hirata ,  Mutsuo Takashima ,  Masaaki Takeda ,  Hiroyoshi Ino ,  Sumio Iwanami

    发明人： Masuo Murakami ,  Kozo Takahashi ,  Yasuhumi Hirata ,  Mutsuo Takashima ,  Masaaki Takeda ,  Hiroyoshi Ino ,  Sumio Iwanami

    IPC分类号： C07D241/24 ,  C07D241/28

    CPC分类号： C07D241/24 ,  Y10S514/872

    摘要： Pyrazine derivatives by the formula ##STR1## are disclosed. In the above formula, R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom, a halogen atom, a hydroxy group, a lower alkoxy group, a phenyl lower alkoxy group, a phenoxy group, a mercapto group, a lower alkylthio group, a phenyl lower alkylthio group, a phenylthio group, an amino group, a substituted amino group, a lower alkyl group, a carbamoyl group or a sulfamoyl group; R.sup.3 represents a lower alkoxy group; R.sup.4, R.sup.5, and R.sup.6, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, a phenyl lower alkyl group, or a phenyl group; and A represents a lower alkylene group; said R.sup.4 and A, said R.sup.5 and A, said R.sup.4 and R.sup.5, or said R.sup.5 and R.sup.6 may form a 5-membered or 6-membered nitrogen-containing heterocyclic ring which may further contain a hetero-atom together with nitrogen atom, and the pharmacologically acceptable non-toxic salts thereof. The compounds of this invention have a strong and selective antiematic activity and an effect of stimulating the gastric motility.

    摘要翻译： 披露了通过式“IMAGE”的吡嗪衍生物。 在上式中，R 1和R 2可以相同或不同，表示氢原子，卤素原子，羟基，低级烷氧基，苯基低级烷氧基，苯氧基，巯基， 低级烷硫基，苯基低级烷硫基，苯硫基，氨基，取代氨基，低级烷基，氨基甲酰基或氨磺酰基; R3表示低级烷氧基; R 4，R 5和R 6可以相同或不同，分别表示氢原子，低级烷基，环烷基，苯基低级烷基或苯基。 A表示低级亚烷基; 所述R4和A表示R5和A表示R4和R5，或所述R5和R6可以形成还可以与氮原子一起含有杂原子的5元或6元含氮杂环，并且 其药理学上可接受的无毒盐。 本发明的化合物具有强的选择性的抗活性和刺激胃动力的作用。

    Methods of protection against emesis in mammals by administration of a 3-alkoxy-thianaphthene-2-carboxamide
    25.
    发明授权
    Methods of protection against emesis in mammals by administration of a 3-alkoxy-thianaphthene-2-carboxamide 失效
    通过施用3-烷氧基 - 硫茚-2-甲酰胺来防止哺乳动物呕吐的方法

    公开(公告)号：US3976780A

    公开(公告)日：1976-08-24

    申请号：US538805

    申请日：1975-01-06

    申请人： Michel Leon Thominet

    发明人： Michel Leon Thominet

    IPC分类号： A61K31/40 ,  C07D333/70 ,  A61K31/38

    CPC分类号： A61K31/40 ,  C07D333/70 ,  Y10S514/872

    摘要： Emesis in mammals is prevented by administration of 3-alkoxy-thianaphthene-2-carboxamides in a daily dosage ranging from 50 to 500 .mu.g/kg as determined by a physician or veterinarian. When administered to dogs in a daily dosage of 250 .mu.g/kg, 100% protection is obtained against vomiting normally induced by subcutaneous administration of apomorphine.

    摘要翻译： 通过由医师或兽医确定的每日剂量为50-500μg/ kg的3-烷氧基 - 硫茚-2-甲酰胺，可以防止哺乳动物的呕吐。 当以250μg/ kg的日剂量给予狗时，通过皮下给予阿朴吗啡可以获得100％的针对呕吐的保护作用。

    2-Substituted-1,2,3,4,6,7,12,12A-octahydropyrazino(2{40 ,1{40 :6,1)pyrido(3,4-B)indoles
    26.
    发明授权
    2-Substituted-1,2,3,4,6,7,12,12A-octahydropyrazino(2{40 ,1{40 :6,1)pyrido(3,4-B)indoles 失效
    2-取代-1,2,3,4,6,7,12,12-八氢吡嗪（2 {40,1 {40：6,1）吡啶并（3,4-B）吲哚

    公开(公告)号：US3917599A

    公开(公告)日：1975-11-04

    申请号：US34640873

    申请日：1973-03-30

    申请人： COUNCIL SCIENT IND RES

    发明人： SAXENA ANIL KUMAR ,  JAIN PADAM CHAND ,  SINGH GURBUKSH ,  DUA PRITHVI RAJ ,  SRIMAL RIKHAB CHAND ,  DHAWAN BHOLA NATH ,  ANAND NITYA

    IPC分类号： C07D471/04 ,  C07D471/14 ,  C07D295/10

    CPC分类号： C07D471/04 ,  C07D471/14 ,  Y10S514/872

    摘要： Pharmacologically active 2-substituted-1,2,3,4,-6,7,12,12Aoctahydropyrazino(2'',1'':6,1)pyrido(3,4 -b)indoles corresponding to the formula

    WHEREIN X is a straight or branched chain alkylene group optionally interrupted by a CO or a CHOH group, R is hydrogen, lower alkyl, aryl, aryloxy, cyano, carboxy, carbalkoxy, dialkylamino, benzodioxanyl or 4-pyridyl, and X and R together may be hydrogen; Y and Z independently are H2 or an oxygen atom; and R'' is hydrogen or a lower alkyl group. The compounds of the invention have tranquilizing and hypotensive activity. The inventive compounds are prepared by reacting an alkyl 1,2,3,4tetrahydro-9H-pyrido(3,4-b)indole-3-carboxylate starting material with ethyleneimine to give a 1-oxo-1,2,3,4,6,7,12,12aoctahydropyrazino(2'',1'':6,1)-pyrido(3,4-b)indole in which substituents are then introduced at position 2 by a variety of methods, before or after having hydrogenated the oxo group at position 1. Alternatively, an alkyl 2-chloro-acetyl-1,2,3,4tetrahydro-9H-pyrido(3,4-b)indole-3-carboxylate and a primary amine H2NXR are reacted to give a 1,4-dioxo-1,2,3,4,6,7,12,12aoctahydropyrazino(2'',1'':6,1)pyrido(3,4-b)indole, in which substituents are then introduced before or after having hydrogenated the two oxo groups at positions 1 and 4.

    摘要翻译： 对应于式WHEREIN X的药理活性2-取代-1,2,3,4,6,7,12,12-八氢吡嗪并[2'，1'：6,1]吡啶并[3,4-b]吲哚 是任选被CO或CHOH基团中断的直链或支链亚烷基，R是氢，低级烷基，芳基，芳氧基，氰基，羧基，烷氧基，二烷基氨基，苯并二氧杂环戊烷基或4-吡啶基，X和R可以一起 氢; Y和Z独立地为H 2或氧原子; 和R'是氢或低级烷基。 本发明化合物具有镇静作用和降血压活性。 通过使1,2,3,4-四氢-9H-吡啶并[3,4-b]吲哚-3-羧酸烷基酯原料与乙烯亚胺反应制得本发明化合物，得到1-氧代-1,2,3 ，4,6,7,12,12a-八氢吡嗪并[2'，1'：6,1] - 吡啶并[3,4-b]吲哚，其中取代基然后通过多种方法引入到位置2， 在氢化位置1上的氧代基之后。或者，将2-氯 - 乙酰基-1,2,3,4-四氢-9H-吡啶并[3,4-b]吲哚-3-羧酸烷基酯和伯胺H 2 NXR 反应得到1,4-二氧代-1,2,3,4,6,7,12,12a-八氢吡嗪并[2'，1'：6,1]吡啶并[3,4-b]吲哚， 然后在氢化位置1和4之间的两个氧代基团之前或之后引入取代基。

    Diphenyl-methylene-n-benzyl-piperidines
    27.
    发明授权
    Diphenyl-methylene-n-benzyl-piperidines 失效
    二苯甲基-N-苄基哌啶

    公开(公告)号：US3759928A

    公开(公告)日：1973-09-18

    申请号：US3759928D

    申请日：1970-06-02

    申请人： UCB SA

    发明人： ZIVKOVIC D

    IPC分类号： C07D211/70 ,  C07D29/12

    CPC分类号： C07D211/70 ,  Y10S514/821 ,  Y10S514/872

    摘要： WHEREIN A1, A2, A3, A4, A5 and B, taken separately, each represents hydrogen, halogen, halomethyl, alkyl, alkoxy, nitro, cyano or amino, and A5 and B, taken together, represent a bivalent radical selected from the group consisting of alkylene, alkenylene and alkadienylene having 3 to 5 carbon atoms and alkylene dioxy having 1 to 3 carbon atoms, said bivalent radical being connected to two adjacent carbon atoms of the benzene nucleus, WITH THE PROVISO THAT WHEN A1, A2, A3, A4, A5 and B are all hydrogen atoms, the diphenyl-methylene radical is in the ortho or meta position with regard to the nitrogen atom in the piperidine nucleus, AND THE ADDITION SALTS THEREOF WITH PHARMACEUTICALLY ACCEPTABLE INORGANIC OR ORGANIC ACIDS.

    Blood circulation activating, anti-arrhythmic and antihistaminic diphenyl-methylene-N-benzyl-piperidines having the general formula

    摘要翻译： 具有通式为A1，A2，A3，A4，A5和B的血液循环活化，抗心律不齐和抗组胺二苯基 - 亚甲基-N-苄基 - 哌啶分别代表氢，卤素，卤代甲基，烷基，烷氧基， 硝基，氰基或氨基，并且A 5和B一起代表选自具有3至5个碳原子的亚烷基，亚烯基和亚烷基二烯基以及具有1至3个碳原子的亚烷基二氧基的二价基团，所述二价基团连接 对于苯核的两个相邻的碳原子，当A1，A2，A3，A4，A5和B都是氢原子时，二苯基 - 亚甲基相对于氮原子在邻位或间位 哌啶核，以及其与药物接受无机或有机酸的添加剂。