公开(公告)号：US3742050A

公开(公告)日：1973-06-26

申请号：US3742050D

申请日：1970-02-16

Applicant: BURROUGHS WELLCOME CO

Inventor： HODSON H

IPC: A61K31/155 ,  A61K31/38 ,  C07C67/00 ,  C07C239/00 ,  C07C257/14 ,  C07D333/16 ,  C07D333/20 ,  C07D333/24 ,  C07D333/28 ,  C07D333/36 ,  C07C123/00

CPC classification number: C07C255/00 ,  C07D333/16 ,  C07D333/28

Abstract: An amidine of general formula I, as shown in the accompanying drawings, or an acid addition salt thereof wherein: R1 and R2 are the same of different and each is a phenyl or thien-2-yl group, optionally substituted in one or more positions by a substituent selected from the class consisting of halogen, lower alkyl, lower alkoxy, hydroxy, lower alkylthio, trifluoromethyl, phenyl, phenoxy, phenyl-(lower alkyl) and phenyl-(lower alkoxy), each of said phenyl, phenoxy, phenyl-(lower alkyl) and phenyl-(lower alkoxy) substituent groups being optionally substituted in one or more positions by a member selected from the class consisting of halogen, lower alkyl, lower alkoxy, hydroxy and lower alkylthio; A1 is a divalent straight or branched alkylene group containing from two to six carbon atoms and one or two divalent atoms which are each an oxygen or sulphur atom, provided that there are at least two carbon atoms between the divalent atom and the -NHgroup and between the two divalent atoms; A2 is a straight or branched alkylene chain containing from one to four carbon atoms; and Z is a member selected from the class consisting of hydrogen and lower alkyl. The compounds are specific antagonists of serotonin, useful specifically as antipressor agents, anticontracting agents and anti-inflammatory agents. Their high activity is maintained for at least 24 hours.

Abstract translation: 如附图所示的通式I的脒或其酸加成盐，其中：R 1和R 2相同，各自为苯基或噻吩-2-基，任选在一个或多个位置上被取代 选自卤素，低级烷基，低级烷氧基，羟基，低级烷硫基，三氟甲基，苯基，苯氧基，苯基 - （低级烷基）和苯基 - （低级烷氧基）的取代基，各自为苯基，苯氧基，苯基 - （低级烷基）和苯基 - （低级烷氧基）取代基任选在一个或多个位置被选自卤素，低级烷基，低级烷氧基，羟基和低级烷硫基的成员取代; A 1是含有2至6个碳原子和一个或两个二价原子的二价直链或支链亚烷基，它们各自为氧或硫原子，条件是在二价原子和-NH- 两个二价原子之间; A2是含有1-4个碳原子的直链或支链亚烷基链; Z为选自氢和低级烷基的成员。

公开(公告)号：US3792050A

公开(公告)日：1974-02-12

申请号：US3792050D

申请日：1971-08-26

Applicant: BURROUGHS WELLCOME CO

Inventor： HODSON H ,  RANDALL A

IPC: A61K31/505 ,  C07D217/22 ,  C07D471/04 ,  C07D51/46

CPC classification number: A61K31/505 ,  C07D217/22 ,  C07D471/04 ,  Y10S514/825

Abstract: THE COMPOUNDS 3,4-DIHYDRO-2-OXO-2H-PYRIMIDO (2,1-A) ISOQUINOLINE AND 3,4,6,7-TETRAHYDRO-2-OXO-2H-PYRIMIDO (2,1-A-)ISOQUINOLINE AND ACID ADDITION SALS THEREOF; PHARMACEUTICAL COMPOSITIONS CONTAINING THEM; AND METHODS OF PREPARAING THE COMPOUNDS, SALTS AND PHARMACEUTICAL COMPOSITIONS. THE COMPOUNDS, SALTS AND COMPOSITIONS ARE USE FUL IN THE TREATMENT OF ARTHRITIS.

公开(公告)号：US3728389A

公开(公告)日：1973-04-17

申请号：US3728389D

申请日：1969-12-15

Applicant: BURROUGHS WELLCOME CO

Inventor： HODSON H ,  RANDALL A

IPC: C07C123/00

CPC classification number: C07C257/18

Abstract: Amidine compounds of the formula

IN WHICH ONE OF Z3 and Z4 is halogen, hydrogen, trifluoromethyl or lower alkoxy when the other is hydrogen; salts of these compounds; their synthesis; and pharmaceutical preparations thereof. Said compounds are useful in the treatment of cardiac arrhythmias.

Abstract translation: 当另一个是氢时，Z 3和Z 4之一的式Ⅺ的脒化合物是卤素，氢，三氟甲基或低级烷氧基; 这些化合物的盐; 他们的合成; 及其药物制剂。 所述化合物可用于治疗心律失常。