# US 2010/0168087 A1 · Benzo[1,2,3]thiadiazine derivates > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2010/0168087 A1 - Document ID: US20100168087A1 - Status: Published application - Kind: A1 - Application number: 12/377,771 - Filed: 2007-08-13 - Published: 2010-07-01 - Earliest claimed: 2006-08-16 - Inventors: Marta Porcs-Makkay; Gyula Lukacs; Gabor Kapus; Istvan Gacsalyi; Gyula Simig; Gyoergy Levay; Tibor Mezei; Miklos Vegh; Szabolcs Kertesz; Jozsef Barkoczy; Csilla Leveleki; Laszlo Gabor Harsing - Web page: https://patentgrep.com/patent/US20100168087A1 ## CPC - C07D 285/16: Thiadiazines; Hydrogenated thiadiazines - A61P 25/00: Drugs for disorders of the nervous system - C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract The present invention relates to new benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the general Formula (I), medicaments containing such compounds and the use thereof in the medicine. Benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the general Formula (I) are suitable for the prevention or treatment of the diseases of the central nervous system. ## Claims ### Claim 1 Benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the Formula (I), wherein R1 and R2 each represents hydrogen or a straight- or branched-chain alkyl group containing 1 to 4 carbon atoms R3, R4, R5 and R6 each represents hydrogen, halogen, a straight- or branched-chain alkyl group having 1 to 4 carbon atoms or an alkoxy group containing a straight- or branched-chain alkyl having 1 to 4 carbon atoms. ### Claim 2 (depends on 1) 7,8-Dichloro-4-methylbenzo[1,2,3]thiadiazine-1,1-dioxide as defined in claim 1. ### Claim 3 (depends on 1) 7,8-Dichloro-4,5-dimethylbenzo[1,2,3]thiadiazine-1,1-dioxide as defined in claim 1. ### Claim 4 (depends on 1) 2,4-Dimethyl-7-chlorobenzo[1,2,3]thiadiazine-1,1-dioxide as defined in claim 1. ### Claim 5 (depends on 1) 2,4-Diethyl-7,8-dichlorobenzo[1,2,3]thiadiazine-1,1-dioxide as defined in claim 1. ### Claim 6 (depends on 1) Process for the preparation of berizo[1,2,3]thiadiazine-1,1-dioxide derivatives, of the Formula (I) as defined in claim 1 wherein R1 and R2 each represents hydrogen or a straight- or branched-chain alkyl having 1 to 4 carbon atoms; R3, R4, R5 and R6 represent hydrogen, halogen, a straight- or branched-chain alkyl group having 1 to 4 carbon atoms or an alkoxy group containing a branched- or straight chain alkyl having 1 to 4 carbon atoms, which comprises a) for the preparation of the compounds of the Formula (I) wherein R1 is hydrogen, R2, R3, R4, R5 and R6 is defined hi claim 1, reacting a 2-acyl benzenesulfonylchloride derivative of the Formula (II) wherein the meaning of R2, R3, R4, R5 and R6 is the above, with a hydrazine derivative, preferably with acetyl-hydrazine and reacting the thus obtained product with a strong acid, preferably with hydrochloric acid; or b) for the preparation of the compounds of the Formula (I), wherein R1 is hydrogen, the meaning of R2, R3, R4, R5 and R6 is as defined in claim 1, reacting a 2-acyl-benzenesulfonylchloride derivative of the Formula (III) wherein the meaning of R2, R3, R4, R5 and R6 is as defined above, with a hydrazine derivative; or c) for the preparation of the compounds of the Formula (I), wherein R1 and R6 represent hydrogen and the meaning of R2, R3, R4, R5 is as defined in claim 1, reacting a benzo[1,2,3]thiadiazine-1,1-dioxide derivative wherein R1 represents hydrogen, R6 is halogen, preferably chloride and the meaning of R2, R3, R4, R5 is the above, with alkyl lithium and converting the thus obtained metal-organic compound by reacting said compound with water, or d) for the preparation of the benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the Formula (I), wherein R1 represents a straight- or branched-chain alkyl group having 1 to 4 carbon atoms, the meaning of R2, R3, R4, R5, R6 is as defined in claim 1, reacting a benzo[1,2,3]thiadiazine-1,1-dioxide derivative of the Formula (I) wherein R1 represents hydrogen, the meaning of R2, R3, R4, R5 and R6 is as defined above with an alkyl halogenide. ### Claim 7 (depends on 6) Process variant d) of claim 6, which comprises using an alkyl ? chloride, alkyl bromide or alkyl iodide as alkyl halogenide. ### Claim 8 (canceled) ### Claim 9 (depends on 1) A medicament suitable for the prevention or treatment of anxiety, which comprises a benzo[1,2,3) thiadiazine-1,1-dioxide derivative of the Formula (I) as defined in claim 1 wherein R1 and R2 each represents hydrogen, a straight- or branched-chain alkyl group having 1 to 4 carbon atoms; the meaning of R3, R4, R5 and R6 is hydrogen, halogen, a straight- or branched-chain alkyl group having 1 to 4 carbon atoms or an alkoxy group containing a straight- or branched-chain alkyl group having 1 to 4 carbon atoms and one or more pharmaceutically acceptable vehicle(s) or optionally auxiliary agents. ### Claim 10 (depends on 1) A medicament suitable for the treatment or prevention of generalized anxiety disorder, panic disorder, phobias, compulsive disorders including obsessive-compulsive disorder, posttraumatic stress disorder, stress-induced anxiety condition, comprising a benzo[1,2,3]thiadiazine-1,1-dioxide derivative of the Formula (I) according to claim 1 and one or more pharmaceutically acceptable vehicle(s) or auxiliary agent(s). ### Claim 11 (depends on 1) A medicament suitable for the prevention or treatment of attention-deficient hyperactivity disorder, stress-induced adaptation disorder, posttraumatic stress disorder, anorexia nervosa, bulimia nervosa, insomnia, parasomnia, compulsive disorders, disturbances of the sexual function and the symptoms related to the use or withdrawal of chemical agents including alcohol, caffeine, nicotine, drugs of abuse, sedatives, hypnotic and doping agents comprising a benzo[1,2,3]thiadiazine-1,1-dioxide derivative of the Formula (I) according to claim 1 and one or more pharmaceutically acceptable vehicle(s) or auxiliary agen(s)t. ### Claim 12 (canceled) ### Claim 13 (canceled) ### Claim 14 (canceled) ### Claim 15 (depends on 1) Method for the treatment of the diseases, disorders or conditions of the central nervous system, especially of anxiety, generalized anxiety disorder, panic disorder, phobias, compulsive disorders, posttraumatic stress disorder, stress-induced anxiety disorder, attention-deficit hyperactivity disorder, stress-related adaptation disorder, anorexia nervosa, bulimia nervosa, insomnia, parasomnia, disturbances of the sexual function and the symptoms of the use or withdrawal of chemical agents including alcohol, caffeine, nicotine, sedatives, narcotics, drugs of abuse or doping agents, which comprises administering to a patient in need of such treatment a therapeutically effective amount of benzo[1,2,3]thiadiazine-1,1-dioxide derivative of the Formula (I) according to claims 1.