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|Title:||Intermediates for N-substituted carbamoyloxyalkyl-azolium derivatives|
|Abstract:||N-substituted carbamoyloxyalkyl-azolium derivatives which have antifungal activity and are useful for the treatment of fungal diseases.|
|Inventor(s):||Fukuda; Hiroshi (Tokyo, JP), Hayase; Tadakatsu (Chigasaki, JP), Mizuguchi; Eisaku (Kamakura, JP), Shimma; Nobuo (Chigasaki, JP), Ohwada; Jun (Kamakura, JP), Oikawa; Nobuhiro (Kawasaki, JP), Sakaitani; Masahiro (Chigasaki, JP), Tsukazaki; Masao (Fujisawa, JP), Umeda; Isao (Yokohama, JP)|
|Assignee:||Basilea Pharmaceutica AG (CH)|
|Filing Date:||Sep 03, 2004|
|Claims:||1. The compound having the formula: ##STR00037## wherein R.sup.1 is hydrogen or alkyl; R.sup.2 is hydrogen, alkyl, alkylcarbonyloxyalkyl, alkoxycarbonyl, alkylcarbonyl, mono- or dialkylaminoalkylcarbonyloxyalkyl; group ##STR00038## is pyridin-2-yl; L is a chloro, bromo, iodo, tosyloxy or mesyloxy; R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen, halogen, alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, carboxy, alkyloxycarbonyl, cyano, trifluoromethyl, trifluoromethoxy, nitro, aminosulfonyl, alkylaminocarbonyloxyalkyl, and sulfo, R.sup.4 and R.sup.5 are in addition alkylcarbonyloxyalkyl or aminoalkylcarbonyloxyalkyl and R.sup.6 is hydroxy, alkoxycarbonylalkylamino, alkoxycarbonylamino, amino, alkylamino, alkylcarbonyloxy, alkoxycarbonylalkylaminoalkylcarbonyloxy, alkoxycarbonylaminoalkylcarbonyloxy, alkylaminoalkylcarbonyloxy, aminoalkylcarbonyloxy, alkylcarbonylamino, alkylcarbonylalkylamino, acyloxy, acylamino, or acylalkylamino. |
2. The compound of claim 1 wherein the pyridin-2-yl group is substituted with alkylaminoalkylcarbonyloxyalkyl, alkylcarbonyloxyalkyl, or aminoalkylcarbonyloxyalkyl.
3. The compound of claim 1 wherein R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen, halogen, alkoxy, cyano, trifluoromethyl, trifluormethoxy and nitro.
4. The compound of claim 3 wherein R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen, halogen and alkoxy.
5. The compound of claim 4 wherein R.sup.4 and R.sup.5 are hydrogen.
6. The compound of claim 1 wherein R.sup.6 is alkylamino, alkylcarbonyloxy, alkylaminoalkylcarbonyloxy or aminoalkylcarbonyloxy.
7. The compound of claim 6 wherein R.sup.6 is alkylaminoalkylcarbonyloxy.
8. The compound of claim 4 wherein said compound is [N-methyl-N-3-((tert-butoxycarbonylmethylamino) acetoxymethl)pyridin-2-yl]carbamic acid 1-chloro-ethyl ester.
9. The compound of claim 4 wherein said compound is [N-methyl-N-3-(acetoxymethyl)pyridin-2-yl]carbamic acid 1-chloro ethyl ester.
10. The compound of claim 4 wherein said compound is [N-methyl-N-3-[(tert-butoxycarbonylamino)acetoxymethyl)pyridin-2-yl]carba- mic acid 1-chloro ethyl ester.
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