Abstract: A novel process for preparing 4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides is disclosed. The process involves the base catalyzed rearrangement of a saccharinacetamide of structure I to give II, ##STR1## wherein R.sup.1 is hydrogen or lower alkyl and R.sup.2 is lower alkyl, aryl or a heterocyclic ring selected from the group consisting of pyridyl, substituted-pyridyl, and thiazolyl. Compounds of the formula II have useful anti-inflammatory properties. In addition, they can be used as intermediate in the preparation of known anti-inflammatory agents.

Abstract: Processes for the production of the compounds of the formula: ##STR1## are disclosed. In the above formula, R.sub.1 is aryl which may be substituted or unsubstituted; R.sub.2 is hydrogen, alkyl, aryl, aralkyl, alkoxy, halogen, cyano, nitro, trifluoromethyl and the like.These compounds are prepared by the following reaction schemes: ##STR2## These compounds are useful as anti-inflammatory agents.

Abstract: A novel process for preparing 4-hydroxy-3-(5-methyl-3-isoxazolylcarbamoyl)-2-methyl-2H-1,2-benzothiazine 1,1-dioxide (I), starting with 3-amino-5-methylisoxazole (II) is disclosed. Compound I exhibits anti-inflammatory properties and is useful for treating inflammation. In the process of the invention an intermediate obtained, 2,3-dihydro-N-(5-methyl-3-isoxazolyl)-3-oxo-1,2-benzisothiazole-2-acetamid e 1,1-dioxide (IV) undergoes rearrangement to provide 1-{[5-(4-hydroxy-2H-1,2-benzothiazin-3-yl)-1,2,4-oxadiazol-3-yl]methyl}eth anone S,S-dioxide (V), which is methylated, according to conventional procedures. The methylated intermediate VI, upon further treatment, undergoes a second rearrangement to obtain the desired anti-inflammatory compound I.

Abstract: A novel process for preparing 4-hydroxy-3-(5-methyl-3-isoxazolylcarbamoyl)-2-methyl-2H-1,2-benzothiazine 1,1-dioxide (I), starting with 3-amino-5-methylisoxazole (II) is disclosed. Compound I exhibits anti-inflammatory properties and is useful for treating inflammation. In the process of the invention an intermediate obtained, 2,3-dihydro-N-(5-methyl-3-isoxazolyl)-3-oxo-1,2-benzisothiazole-2-actamide 1,1-dioxide (IV) undergoes rearrangement to provide 1-{[5-(4-hydroxy-2H-1,2-benzothiazin-3-yl)-1,2,4-oxadiazol-3-yl]methyl}eth anone, S,S-dioxide (V), which is methylated, according to conventional procedures. The methylated intermediate VI, upon further treatment, undergoes a second rearrangement to obtain the desired anti-inflammatory compound I.

Abstract: A novel process for preparing 4-hydroxy-3-(5-methyl-3-isoxazolylcarbamoyl)-2-methyl-2H-1,2-benzothiazine 1,1-dioxide (I), starting with 3-amino-5-methylisoxazole (II) is disclosed. Compound I exhibits anti-inflammatory properties and is useful for treating inflammation. In the process of the invention an intermediate obtained, 2,3-dihydro-N-(5-methyl-3-isoxazolyl)-3-oxo-1,2-benzisothiazole-2-acetamid e 1,1-dioxide (IV) undergoes rearrangement to provide 1-{[5-(4-hydroxy-2H-1,2-benzothiazin-3-yl)-1,2,4-oxadiazol-3-yl]methyl}eth anone S,S-dioxide (V), which is methylated, according to conventional procedures. The methylated intermediate VI, upon further treatment, undergoes a second rearrangement to obtain the desired anti-inflammatory compound I.

Abstract: Processes for the production of the compounds of the formula: ##STR1## are disclosed. In the above formula, R.sub.1 is aryl which may be substituted or unsubstituted; R.sub.2 is hydrogen, alkyl, aryl, aralkyl, alkoxy, halogen, cyano, nitro, trifluoromethyl and the like.These compounds are prepared by the following reaction schemes: ##STR2## These compounds are useful as anti-inflammatory agents.

Abstract: Processes for the production of the compounds of the formula: ##STR1## are disclosed. In the above formula, R.sub.1 is aryl which may be substituted or unsubstituted; R.sub.2 is hydrogen, alkyl, aryl, aralkyl, alkoxy, halogen, cyano, nitro, trifluoromethyl and the like.These compounds are prepared by the following reaction schemes: ##STR2## These compounds are useful as anti-inflammatory agents.

Abstract: This invention relates to a process for the preparation of 1-{[5-(4-hydroxy-2H-1,2-benzothiazin-3-yl)-1,2,4-oxadiazol-3-yl]methyl}eth anone S,S-dioxide (III), a novel intermediate useful in the preparation of the known anti-inflammatory agent, 4-hydroxy-3-(5-methyl-3-isoxazolylcarbamoyl)-2-methyl-2H-1,2-benzothiazine 1,1-dioxide (IV). According to the process of this invention, the saccharin compound, 2,3-dihydro-N-(5-methyl-3-isoxazolyl)-3-oxo-1,2-benzisothiazole-2-acetamid e 1,1-dioxide (I) is reacted with an alkali metal alkoxide of a lower alcohol in an inert solvent at temperatures below 30.degree. C. to form the benzenesulfonylglycineamide, alkyl 2-{[({[(5-methyl-3-isoxazolyl)amino]carbonyl}methyl)amino]sulfonyl}benzoat e (II), which is ring closed and rearranged by reaction with an alkali metal alkoxide of a lower alcohol in an inert solvent at temperatures of from 60.degree. C. to 70.degree. C. to form the desired oxadiazole compound III.

Abstract: A novel process for preparing 4-hydroxy-3-(5-methyl-3-isoxazolylcarbamoyl)-2-methyl-2H-1,2-benzothiazine 1,1-dioxide (I), starting with 3-amino-5-methylisoxazole (II) is disclosed. Compound I exhibits anti-inflammatory properties and is useful for treating inflammation. In the process of the invention an intermediate obtained, 2,3-dihydro-N-(5-methyl-3-isoxazolyl)-3-oxo-1,2-benzisothiazole-2-acetamid e 1,1-dioxide (IV) undergoes rearrangement to provide 1-{[5-(4-hydroxy-2H-1,2-benzothiazin-3-yl)-1,2,4-oxadiazol-3-yl]methyl}eth anone S,S-dioxide (V), which is methylated, according to conventional procedures. The methylated intermediates VI, upon further treatment, undergoes a second rearrangement to obtain the desired anti-inflammatory compound I.

Abstract: .beta.-Ketoacyl derivatives of 6-aminopenicillanic acid of the formula: ##SPC1##Are disclosed. In the above structure R.sup.1 is hydrogen, alkyl, halogen, alkoxy, cyano, trifluoromethyl and the like; Z is CHR.sup.2 or NR.sup.2 ; R.sup.2 is hydrogen, alkyl, aralkyl; M is an alkali or alkaline earth metal such as sodium, potassium, or calcium. These compounds are useful as anti-bacterials.

Abstract: Compounds of the formula: ##SPC1##Are disclosed. In the above formula, R.sub.1 is aryl such as benzene or a heterocycle such as pyridine, isoxazole, or thiazole. The aryl or heterocyclic group R.sub.1 is substituted or unsubstituted. R.sub.2 is hydrogen, lower alkyl, halogen, lower alkoxy, trifluoromethyl and the like.These compounds are useful as anti-inflammatory agents indicated in conditions such as rheumatoid arthritis.

Abstract: A novel process for preparing 4-hydroxy-3-(5-methyl-3-isoxazolylcarbamoyl)-2-methyl-2H-1,2-benzothiazine 1,1-dioxide (I), starting with 3-amino-5-methylisoxazole (II) is disclosed. Compound I exhibits anti-inflammatory properties and is useful for treating inflammation. In the process of the invention an intermediate obtained, 2,3-dihydro-N-(5-methyl-3-isoxazolyl)-3-oxo-1,2-benzisothiazole-2-acetamid e 1,1-dioxide (IV) undergoes rearrangement to provide 1-{[5-(4-hydroxy-2H-1,2-benzothiazin-3-yl)-1,2,4-oxadiazol-3-yl]methyl}eth anone S,S-dioxide (V), which is methylated, according to conventional procedures. The methylated intermediate VI, upon further treatment, undergoes a second rearrangement to obtain the desired anti-inflammatory compound I.

Abstract: 3-Thiomethyl-2[2-(dialkylamino)ethyl]indoles having the following structural formula are disclosed ##SPC1##In the above formula, R.sub.1, R.sub.2, and R.sub.3 are hydrogen or alkyl, R.sub.4 is alkyl, aryl, aralkyl, or a heterocyclic, R.sub.5 is hydrogen, alkyl, halogen, alkoxy, hydroxyl and the like.These compounds exhibit central nervous system depressing properties and are useful as anti-aggression agents.

Abstract: The present invention concerns compounds of Formula I ##SPC1##wherein R.sub.1 is hydrogen, lower alkyl, aralkyl; R.sub.2 is hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl, cyano, nitro, and the like; R.sub.3 is lower alkyl; ##EQU1## (where R.sub.4 and R.sub.5 are lower alkyl), ##EQU2## (where R.sub.6 is hydrogen, lower alkyl, aryl, acetamido and R.sub.7 is lower alkyl), ##SPC2##(where R.sub.8 and R.sub.9 are hydrogen or lower alkyl), --CH(SO.sub.2 C.sub.6 H.sub.5).sub.2, ##SPC3## ##EQU3## (where R.sub.10 is hydrogen, CN, acyl), ##EQU4## (where R.sub.11 and R.sub.12 are lower alkyl), --SO.sub.2 C.sub.6 H.sub.5, --CONH.sub.2, --CO.sub.2 R.sub.13 (where R.sub.13 is lower alkyl), ##EQU5## (R.sub.14 and R.sub.15 are lower alkyl). These compounds are useful as sedatives and antiaggression agents.