Saccharin derivatives as orally active elastase inhibitors
OwnerPeter Aranyi, Sandor Batori +11inventors
InventorsPeter Aranyi, Sandor Batori, Stephane Dessilla, Istvan Hermecz, Zoltan Kapui, Ferenc Levai, Endre Mikus, Marc Pascal, Lajos T. Nagy, Bruno Simonot, Katalin Urban Szabo, Marton Varga, Lelle Vasvarine Debreczy
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Abstract
Orally active compounds of general formula (I) wherein R1 is methyl, ethyl or 2-morpholino-ethyl group, R2 is piperidino, morpholino or 4-methyl-piperazinyl group, n is 2 or 3 and their salts, solvates and hydrates.
Claims31
Compounds of the general formula (I)
- wherein
- R1 is methyl, ethyl or 2-morpholino-ethyl-group;
- R2 is piperidino, morpholino or 4-methyl-piperazinyl group;
- n is 2 or 3—
- and their salts, solvates and hydrates:
2-[9-(2-piperidino-ethoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yl-oxymethyl]-4-isopropyl-6-methoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide and its salts, solvates and hydrates.
2-[9-(3-morpholino-propoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yl-oxymethyl]-4-isopropyl-6-methoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide and its salts, solvates and hydrates.
2-[9-(2-(4-methyl-piperazino)-ethoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yl-oxymethyl]-4-isopropyl-6-methoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide and its salts, solvates and hydrates.
2-[9-(3-morpholino-propoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yl-oxymethyl]-4-isopropyl-6-(2-morpholino-ethoxy)-1,2-benzisothiazol-3(2H)-one-1,2-dioxide and its salts, solvates and hydrates.
2-[9-(2-piperidino-ethoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yl-oxymethyl]-4-isopropyl-6-methoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide hydrochloride.
2-[9-(2-piperidino-ethoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yl-oxymethyl]-4-isopropyl-6-methoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide tartarate salts.
2-[9-(2-piperidino-ethoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yl-oxymethyl]-4-isopropyl-6-methoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide fumarate salts.
2-[9-(2-piperidino-ethoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yl-oxymethyl]-4-isopropyl-6-methoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide benzoate salt.
2-[9-(2-piperidino-ethoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yl-oxymethyl]-4-isopropyl-6-methoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide citrate salts.
2-[9-(2-piperidino-ethoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yl-oxymethyl]-4-isopropyl-6-methoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide mandelate salts.
2-(9-(2-piperidino-ethoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yl-oxymethyl)-4-isopropyl-6-methoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide 4-isopropyl-6-methoxy-saccharinate salt.
Compounds of the general formula (III)—wherein R2 is piperidino, morpholino or 4-methyl-piperazinyl group, n is 2 or 3—and their salts.
2-hydroxy-9-(2-piperidino-ethoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidine.
2-hydroxy-9-(3-morpholino-propoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidine.
2-hydroxy-9-(2-(4-methyl-piperazino)-ethoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidine.
Dependencies are inferred from the claim text.