Biologically active 3-substituted oxindole derivatives useful as anti-angiogenic agents
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United States of America Patent
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Nov 19, 1996
Grant Date -
N/A
app pub date -
Dec 12, 1994
filing date -
Dec 22, 1993
priority date (Note) -
Expired
status (Latency Note)
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Abstract
The new use of a compound of formula (I) ##STR1## wherein Y is a bicyclic ring selected from naphthalene, tetralin, quinoline, isoquinoline and indole; n is zero or an integer of 1 to 3; R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, cyano, carboxy, nitro, or NHR, wherein R is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkanoyloxy, carboxy, nitro or NHR, wherein R is as defined above; R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or halogen; or a pharmaceutically acceptable salt thereof; and wherein when Y is naphthalene then n is zero or an integer of 1 to 3, whereas when Y is tetralin, quinoline, isoquinoline or indole then n is zero, 1 or 2; and wherein when the bicyclic ring Y is naphthalene, quinoline, isoquinoline or indole, then each of the substituents OR.sub.1, R.sub.2 and oxindolylidene may be independently on either of the aryl or heteroaryl moieties of said bicyclic ring, whereas only the benzene moiety is substituted when Y is tetralin; and wherein when Y is naphthalene, tetralin, quinoline or isoquinoline, then R.sub.2 is hydrogen, halogen, cyano or C.sub.1 -C.sub.6 alkyl and R.sub.3, R.sub.4 and R.sub.5 are hydrogen; whereas when Y is indole, then R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, cyano, carboxy, nitro or --NHR, in which R is as defined above, R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyloxy, carboxy, nitro or --NHR, wherein R is as defined above, and R.sub.5 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl; as anti-angiogenic agent is disclosed.

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- 15 United States
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- 2 Other
Patent Owner(s)
Patent Owner | Address | |
---|---|---|
FARMITALIA CARLO ERBA S R L | VIA CARLO IMBONATI 24 20159 MILAN |
International Classification(s)
Inventor(s)
Inventor Name | Address | # of filed Patents | Total Citations |
---|---|---|---|
Ballinari, Dario | S. Donato Mil., IT | 24 | 388 |
Brasca, Maria G | Cusago, IT | 5 | 77 |
Buzzetti, Franco | Monza, IT | 31 | 565 |
Crugnola, Angelo | Varese, IT | 10 | 264 |
Longo, Antonio | Milan, IT | 69 | 11279 |
Mariani, Mariangela | Desio, IT | 3 | 33 |
Orzi, Fabrizio | Milan, IT | 12 | 69 |
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Maintenance Fees
Fee | Large entity fee | small entity fee | micro entity fee | due date |
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Fee | Large entity fee | small entity fee | micro entity fee |
---|---|---|---|
Surcharge after expiration - Late payment is unavoidable | $700.00 | $350.00 | $175.00 |
Surcharge after expiration - Late payment is unintentional | $1,640.00 | $820.00 | $410.00 |
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