公开(公告)号：US3635983A

公开(公告)日：1972-01-18

申请号：US3635983D

申请日：1967-12-07

Applicant: ROUSSEL UCLAF

Inventor： BOISSIER JACQUES R ,  RATOUIS ROGER

IPC: A61K31/00 ,  C07D55/54

CPC classification number: A61K31/00 ,  Y10S514/91 ,  Y10S514/96

Abstract: THE COMPOUNDS ARE DERIVATIVES OF 11H-DIBENZO(1,2,5) TRIAZEPINE AND THEIR ACID ADDITION AND QUATERNARY AMMONIUM SALTS; THEY CORRESPOND TO THE FORMULA:

11-(R1-N(-R2)-A-)-11H-DIBENZO(1,2,5)TRIAZEPINE

A: AN ALKYLENE RADICAL CONTAINING FROM 2 TO 4 CARBON ATOMS. R1-R2: LOWER ALKYL OR HYDROXYALKYL RADICALS, OR FORM WITH THE NITROGEN ATOM N TO WHICH THEY ARE BOUND A HETEROCYCLIC EVENTUALLY SUBSTITUTED BY ONE OR SEVERAL LOWER ALKYL OR HYDROXYALKYL RADICALS. THEY ARE VERY USEFUL SUBSTANCES AS THERAPEUTICS, NAMELY, AS THYMOANALEPTICS, ANTIPARKINSONIANS, ANORECTICS, LOCAL ANESTHETICS AND ANTIHISTAMINICS. THE COMPOUNDS OF FORMULA 1 ARE PREPARED BY REACTING, IN THE PRESENCE OF AN ALKALINE AGENT, 11H-DIBENZO(1,2,5) TRIAZEPINE OF FORMULA:

11H-DIBENZO(1,2,5)TRIAZEPINE

WITH A COMPOUND OF FORMULA:

X-A-N(-R1)-R2

(X: HALOGEN ATOM).

公开(公告)号：US3697590A

公开(公告)日：1972-10-10

申请号：US3697590D

申请日：1969-07-28

Applicant: ROUSSEL UCLAF

Inventor： BOISSIER JACQUES R ,  RATOUIS ROGER

IPC: A61K31/19 ,  C07C101/44

CPC classification number: A61K31/19 ,  Y10S514/916

Abstract: WHERE R represents an hydrogen or a methyl radical. Compounds of formula (1) and their metallic and amine salts are very useful substances in human therapeutics, namely as analgesic, antipyretic and antiinflamatory medicines. Compounds of formula (1) are prepared by reacting a 2phenothiazinylacetic acid of formula:

Phenylacetic acid derivatives having the formula:
WITH A DESULFURIZING REDUCING AGENT.

D R A W I N G

公开(公告)号：US3651049A

公开(公告)日：1972-03-21

申请号：US3651049D

申请日：1970-03-12

Applicant: ROUSSEL UCLAF

Inventor： BOISSIER JACQUES R ,  RATOUIS ROGER

IPC: A61K31/573 ,  A61K31/58 ,  C07D319/08 ,  C07J21/00 ,  C07C173/00

CPC classification number: A61K31/573 ,  A61K31/58 ,  C07D319/08 ,  C07J21/00

Abstract: CYCLIC ACETAL DERIVATIVES OF PREGNANE OF GENERAL FORMULA:

3,5''-DI(O=),6-Z,9-Y,16-P,2''-(R1-CH=C(-R)-(CH2)N-)SPIRO

(ANDROSTA-1,4-DIENE-17,4''-(1,3)DIOXANE) WITH X IN

POSITION 11

WHEREIN X:CO OR CH2 OR CHOH-Y:H OR F-Z:H OR CH3-P:H OR ALKYL OR ALKYIDENE-N: O OR 1-R:H OR HALOGEN OR ALKYL-R1:H OR ALKYL OR CARBOXYL OR ALKOXYCARBONYL-BROKEN LINE IN THE RING A: OPTIONAL PRESENCE OF A DOUBLE BOND. THESE PRODUCTS ARE VERY USEFUL SUBSTANCES IN HUMAN AND ANIMAL THERAPY, ESPECIALLY OWING TO THEIR REMARKABLE ANTI-INFLAMMATORY ACTION. THE PRODUCTS ARE PREPARED BY ACTION OF A DIALKYL ACETAL ON A PREGNANE DERIVATIVE HAVING HYDROXYL RADICALS IN ITS 17 AND 21 POSITIONS, IN THE PRESENCE OF AN ACID CATALYST.