IL41198A - 1-phenyl-3h-1,4-benzodiazepine-2,5(1h,4h)-diones,their preparation and pharmaceutical compositions containing them - Google Patents

Claims (1)

1. Claimsί 1. Compounds of the general formula :■ 0 wherein represents a phenyl group which may, if desired, be substituted in the o- , m- or £- position by a fluorine, chlorine or bromine atom or a trifluoromethyl or nitro group; and represents ar fluorine, chlorine or bromine atom or a trifluoromethyl , nitro, amino, cyano or hydroxyl group, 2. Compounds as claimed in claim 1 wherein represents a phenyl group which may, if desired, be substituted in the 0-, m- , or £- position by a fluorine, chlorine or bromine atom and represents a chlorine atom or a trifluoromethyl group. r 1 3. l-Phenyl-8-trifluoromethyl-3H-l,4-benzo|cLiazepin-2,5- (lH,4H)-dione. 4. 8-Chloro-l-phenyl-3H-l,4-benzodiazepin-2,5-(lH,4H)-dione. i- 5. 8-Chloro-/(o-chlorophenyl)-3H-l ,4-benzodiazepin-2 , 5- (lH,4H)-dione. :..-» 41198/2 ; 6. 8-Chloro- ( ο- fluoropheny1)-3H- 1 , 4-benzodiaze in- 2 , 5- (lH,4H)-dione. 7. Compounds as claimed in claim 1, other than as claimed in any of claims 3 to 6, as herein specifically disclosed. 8. A process for the preparation of compounds as claimed in claim 1 which comprises cyclizing a compound of the I1 formula:- wherein and R2 are as defined in claim 1 and R represents . a lower alkoxy group, a halogen atom or a hydroxy, O-tosyl or lower acyloxy group, whereby a compound of formula I is obtained* A process as claimed in olaim 8, wherein the cyclization is effected in the presence of a condensing w ere n an 2 are as e ine n c a m , R s as de ne in claim 8 and X represents a chlorine, bromine or iodine atom or an O-tosyl or lower alkoxy group, with ammonia, whereb a compound of formula II is obtained. 13· A process as claimed in claim 12, wherein the ammonia is produced in situ by the use of an ammonia from 20°C to the boiling temperature of the reaction mixture. 19.Ϊ A process as claimed in claim 8 or claim 16 substantially as herein described. 20. ' A process for the preparation of compounds as claimed in claim 1 substantially as herein described in any of Examples 1 to 15. ' i ' ' . ·"■ ■ 21. j Compounds as claimed in claim 1 when prepared... by a process as claimed in any of claims 8 to 20. 22. Pharmaceutical compositions comprising as active ingredient at least one compound of formula I as claimed in any of claims 1 to 7 in association with a pharmaceutical carrier or excipient. v 23.j Compositions as claimed in claim 22 in a form suitable for oral, parenteral, rectal or enteral administration. 24.1 Compositions as claimed in claim 22 or claim 23 · .'■ in the form of granules, tablets, coated tablets, capsules, pills, syrups, emulsions, suspensions, powders, drops t suppositories of injection solutions. ingredient. 27·| Compositions as claimed in claim 26 wherein each dosage unit contains from 5 to 25 mg o the said active ingredient. 23β| Compositions as claimed in any of claims 22 to 27 which contain a further physiologically active ingredient* \ 29 ·ί Compositions as claimed in claim 28 wherein the further physiologically active ingredient is a spasmolytic or psychopharmaceutical. 30· ' Compositions as claimed in claim 22 substantially as herein described. ^ ■ . ." 31. I Pharmaceutical compositions substantially as herein described in any of Examples 16 to 18. For the Applica ts DR. REINJiO¾p COHNl AND PARTNERS By: