Claims for Patent: 4,808,612

Summary for Patent: 4,808,612

Title:	2-Arylbenzo(b)(1,6)naphthyridines as inhibitors of interleukin 1
Abstract:	There is disclosed a method for the treatment of inflammatory conditions and of collegenase-induced tissue destruction which comprises the administration of a therapeutically effective amount of a compound of the formula ##STR1## wherein R.sup.1 is phenyl or naphthyl, or phenyl or naphthyl substituted with halo, lower alkyl, lower alkyl carbonyl, benzoyl, carboxy, lower alkoxycarbonyl, OR.sup.2, N(R.sup.2).sub.2, CON(R.sup.2).sub.2, SO.sub.3 R.sup.2, SO.sub.2 N(R.sup.2).sub.2, phenylsulfonyl, lower alkylsulfonyl, cyano nitro or trifluoromethyl; R.sup.2 is hydrogen, lower alkyl or phenyl; R.sup.3 is halo, morpholino, 4-methylpiperazino R.sup.4 NNHR.sup.5, NR.sup.4 R.sup.5, OR.sup.5, SR.sup.5, ##STR2## R.sup.4 is hydrogen or lower alkyl; R.sup.5 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkyl or phenyl; and R.sup.6 and R.sup.7 are each independently, hydrogen, halo, nitro, lower alkoxy, lower alkyl, cyano, trifluoromethyl, phenyl, carboxy or lower alkoxycarbonyl; which compounds, by virtue of their ability to inhibit interleukin 1, are useful as antiinflammatory agents and in treatment of disease states involving enzymatic tissue destruction, and are also intermediates in the preparation of other compounds which possess identical activities.
Inventor(s):	Skotnicki; Jerauld S. (Chadds Ford, PA), Gilman; Steven C. (Newtown Square, PA)
Assignee:	American Home Products Corporation (New York, NY)
Application Number:	07/047,970
Patent Claims:	1. A method for the treatment of inflammatory conditions and of collagenase-induced tissue destruction in warm-blooded animals which comprises the administration thereto of an anti-inflammatory/collagenase inhibitory amount of a compound having the formula ##STR8## wherein R.sup.1 is phenyl or naphthyl, or phenyl or naphthyl substituted with halo, lower alkyl, lower alkyl carbonyl, benzoyl, carboxy, lower alkoxycarbonyl, OR.sup.2, N(R.sup.2).sub.2, CON(R.sup.2).sub.2, SO.sub.3 R.sup.2, SO.sub.2 N(R.sup.2).sub.2, phenylsulfonyl, lower alkylsulfonyl, cyano, nitro or trifluoromethyl; R.sup.2 is hydrogen, lower alkyl or phenyl; R.sup.3 is halo, R.sup.4 NNHR.sup.5, NR.sup.4 R.sup.5, OR.sup.5, SR.sup.5, R.sup.4 NCH.sub.2 CH.sub.2 OCH.sub.3 or SCH.sub.2 CH.sub.2 CH.sub.2 NCH.sub.2 ; R.sup.4 is hydrogen or lower alkyl; R.sup.5 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkyl or phenyl; and R.sup.6 and R.sup.7 are each independently, hydrogen, halo, nitro, lower alkoxy, lower alkyl, cyano, trifluoromethyl, phenyl, carboxy or lower alkoxycarbonyl. 2. The method of claim 1, wherein the compound administered is 4-(7,10-dichloro-3,4-dihydrobenzo[b][1,6]naphthyridin-2(1H)-yl)benzonitril e. 3. The method of claim 1, wherein the compound administered is 4-(7,10-dichloro-3,4-dihydrobenzo[b][1,6]naphthyridin-2(1H)-yl)benzoic acid ethyl ester. 4. The method of claim 1, wherein the compound administered is 7,10-dichloro-1,2,3,4-tetrahydro-2-(4-methylsulfonyl)phenylbenzo[b][1,6]na phthyridine. 5. The method of claim 1, wherein the compound administered is 7,10-dichloro-2-(4-fluorophenyl)-1,2,3,4-tetrahydrobenz[b][1,6]naphthyridi ne. 6. The method of claim 1, wherein the compound administered is 4-(10-chloro-3,4-dihydrobenz[b][1,6]naphthyridine-2(1H)-yl)benzonitrile. 7. The method of claim 1, wherein the compound administered is 7,10-dichloro-1,2,3,4-tetrahydro-2-[4-(trifluoromethyl)phenyl]benzo[b][1,6 ]naphthyridine. 8. The method of claim 1, wherein the compound administered is 4-(10-chloro-3,4-dihydrobenzo[b][1,6]naphthyridin-2(1H)-yl)benzoic acid ethyl ester. 9. The method of claim 1, wherein the compound administered is 4-(8,10-dichloro-3,4-dihydrobenzo[b][1,6]naphthyridin-2(1H)-yl)benzonitril e. 10. The method of claim 1, wherein the compound administered is 4-(10-chloro-3,4-dihydro-7-methylbenzo[b][1,6]naphthyridin-2(1H)-yl)benzon itrile. 11. The method of claim 1, wherein the compound administered is 4-(10-chloro-7-fluoro-3,4-dihydrobenzo[b][1,6]naphthyridin-2(1H)-benzonitr ile. 12. The method of claim 1, wherein the compound administered is 4-[7-chloro-3,4-dihydro-10-(2-phenylhydrazino)benzo[b][1,6]naphthyridin-2( 1H)-yl]benzonitrile.

Details for Patent 4,808,612

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Smith & Nephew, Inc.	SANTYL	collagenase	Ointment	101995	06/04/1965		2039-03-29