George F. Field - West Caldwell NJ William J. Zally - Cresskill NJ
Assignee:
Hoffmann-La Roche Inc. - Nutley NJ
International Classification:
C07D23904 C07D24506
US Classification:
544283
Abstract:
Novel intermediates of the formula ##STR1## wherein X and Y are hydrogen, halogen or trifluoromethyl and R. sub. 1 is hydrogen or lower alkyl are presented. Also disclosed is a process leading to the intermediates and their conversion to imidazobenzodiazepines, compounds of pharmacological activity.
4-(2-Benzoylphenyl-1-Pyazole And 4-(2-Benzoylphenyl)-1-Pyrazoline Derivatives
George F. Field - West Caldwell NJ Rodney I. Fryer - North Caldwell NJ Eugene J. Trybulski - Parsippany NJ Armin Walser - West Caldwell NJ
Assignee:
Hoffmann-La Roche Inc. - Nutley NJ
International Classification:
C07D23106 C07D23114
US Classification:
548356
Abstract:
There are presented compounds of the formula ##STR1## wherein R. sub. 1 is hydrogen or lower alkyl; R. sub. 6 is halo and R. sub. 5 is hydrogen or halo; and compounds of the formulas ##STR2## wherein R. sub. 2 and R. sub. 3 are selected from the group consisting of hydrogen, lower alkyl, C. sub. 2 to C. sub. 7 carboxylic acids, hydroxy C. sub. 2 to C. sub. 7 alkyl, C. sub. 2 to C. sub. 7 carboxylic acid esters and amides and the group COR. sub. 11 wherein R. sub. 11 and is selected from the group consisting of alkoxy, amino or mono-lower alkyl amino; R. sub. 35 is hydrogen or lower alkyl; R. sub. 5 is hydrogen or halo; and R. sub. 7 is methyl or chloromethyl, all of which are useful in the preparation of pyrazolobenzazepines.
George F. Field - West Caldwell NJ Rodney I. Fryer - North Caldwell NJ Eugene J. Trybulski - Parsippany NJ Armin Walser - West Caldwell NJ
Assignee:
Hoffmann-La Roche Inc. - Nutley NJ
International Classification:
A61K 3155 C07D48704
US Classification:
2602456
Abstract:
There are presented compounds of the formulas ##STR1## wherein R. sub. 1 is hydrogen or lower alkyl; R. sub. 2 and R. sub. 3 are selected from the group consisting of hydrogen, lower alkyl, C. sub. 2 to C. sub. 7 carboxylic acids, hydroxy C. sub. 2 to C. sub. 7 alkyl, C. sub. 2 to C. sub. 7 carboxylic acid esters and amides and the group COR. sub. 11 wherein R. sub. 11 is alkoxy, amino or mono- lower alkyl amino; R. sub. 6 is nitro or halo and R. sub. 5 is hydrogen or halo, and the pharmaceutically acceptable salts thereof. The pyrazolobenzazepines are useful as anxiolytic and sedative agents. Also provided are processes and intermediates in the production of the above pyrazolobenzazepines.
George F. Field - West Caldwell NJ William J. Zally - Cresskill NJ
Assignee:
Hoffmann-La Roche Inc. - Nutley NJ
International Classification:
C07D40306
US Classification:
548336
Abstract:
A multistep process is presented for the preparation of imidazobenzodiazepines of the formula ##STR1## wherein X and Y are selected from the group consisting of hydrogen, halogen and trifluoromethyl. Also presented are novel intermediates utilized in the process. The end products are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants. The end products are especially useful in intravenous compositions for use in preoperative anesthesia.
This invention relates to a synthesis of biotin by the reduction of dehydrobiotin. The dehydrobiotin is prepared from 6-hydroxy-7-nitro-heptanoic acid methyl ester. Novel intermediates are also obtained by this synthesis.
George F. Field - West Caldwell NJ William J. Zally - Cresskill NJ
Assignee:
Hoffmann-La Roche Inc. - Nutley NJ
International Classification:
C07D23364
US Classification:
548343
Abstract:
A multistep process is presented for the preparation of imidazobenzodiazepines of the formula ##STR1## wherein X and Y are selected from the group consisting of hydrogen, halogen and trifluoromethyl. Also presented are novel intermediates utilized in the process. The end products are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants. The end products are especially useful in intravenous compositions for use in preoperative anesthesia.
2-Aroyl-3-Amino Pyrazines And The 3(-2Haloacetamide Derivatives Thereof
George Francis Field - West Caldwell NJ Leo Henryk Sternbach - Upper Montclair NJ Armin Walser - West Caldwell NJ
Assignee:
Hoffmann-La Roche Inc. - Nutley NJ
International Classification:
C07D24114
US Classification:
260250BN
Abstract:
Novel pyrazino-1,4-diazepines are disclosed together with processes for their preparation and novel intermediates used in these processes. These novel diazepines are useful as sedatives, muscle-relaxants and anti-convulsants.
George F. Field - West Caldwell NJ William J. Zally - Cresskill NJ
Assignee:
Hoffmann-La Roche Inc. - Nutley NJ
International Classification:
A61K 3147 C07D21516
US Classification:
514313
Abstract:
Disclosed are compounds of the formula ##STR1## wherein: R. sup. 1 and R. sub. 2 may be either the same or different and each is hydrogen or lower alkyl; and wherein R. sup. 3 and R. sup. 4 may be either the same or different and each is hydrogen, halogen, or lower alkyl, with the proviso that R. sup. 3 and R. sup. 4 cannot both be hydrogen. These compounds are useful as anticonvulsant or anxiolytic agents.