Details for Patent: 4,316,839

Summary for Patent: 4,316,839

Patent landscape, scope, and claims:

Title:	Imidazodiazepine derivatives
Abstract:	Imidazodiazepine derivatives of the formula ##STR1## wherein A together with the two carbon atoms denoted as .alpha. and .beta. is selected from the group consisting of ##STR2## the dotted line represents the double bond present in groups (a) and (b), D is >C.dbd.O or >C.dbd.S, R.sup.1 is selected from the group consisting of cyano, lower alkanoyl and a group of the formula --COOR.sup.4, R.sup.4 is selected from the group consisting of methyl, ethyl, isopropyl and 2-hydroxyethyl, R.sup.5 is selected from the group consisting of hydrogen, trifluoromethyl and halogen and R.sup.6 is selected from the group consisting of hydrogen, trifluoromethyl, halogen and lower alkyl and either R.sup.2 is hydrogen and R.sup.3 is hydrogen or lower alkyl or R.sup.2 and R.sup.3 together are trimethylene or propenylene and the carbon atom denoted as .gamma. has the S- or R,S-configuration, and pharmaceutically acceptable salts thereof are presented and have utility for antagonizing the central-depressant, muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillizing activity. They can be used, for example, as antidotes in the case of intoxications in which excessive intake of 1,4-benzodiazepines which have tranquillizing participates, or for shortening an anaesthesia induced by such 1,4-benzodiazepines. They can also be used for suppressing the activities on the central nervous system of 1,4-benzodiazepines used in other fields of indication, for example of schistosomicidally-active 1,4-benzodiazepines such as (+)-5-(o-chlorophenyl)-1,3-dihydro-3-methyl-7-nitro-2H-1,4-benzodiazepin-2 -one. Also presented are processes to produce the imidazodiazepine derivatives and intermediates therefor.
Inventor(s):	Gerecke; Max (Reinach, CH), Haefely; Willy (Reinach, CH), Hunkeler; Walter (Magden, CH), Kyburz; Emilio (Reinach, CH), Mohler; Hanns (Inzlingen, DE), Pieri; Lorenzo (Riehen, CH), Polc; Petar (Binningen, CH)
Assignee:	Hoffman-La Roche Inc. (Nutley, NJ)
Application Number:	06/193,775
Patent Claim Types: see list of patent claims	Compound;

Drugs Protected by US Patent 4,316,839

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

Foreign Priority and PCT Information for Patent: 4,316,839

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Switzerland	8971/79	Oct 04, 1979
Switzerland	8972/79	Oct 04, 1979
Switzerland	10664/79	Nov 30, 1979
Switzerland	10665/79	Nov 30, 1979
Switzerland	5716/80	Jul 25, 1980

International Family Members for US Patent 4,316,839

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	227293
Austria	7497
Australia	533641
Australia	6278280
Brazil	8006404