EP 1244628 A1 20021002 - SUBSTITUTED 8-ARYLQUINOLINE PHOSPHODIESTERASE-4 INHIBITORS

Title (en)

SUBSTITUTED 8-ARYLQUINOLINE PHOSPHODIESTERASE-4 INHIBITORS

Title (de)

SUBSTITUTIERTE 8-ARYLCHINOLIN PHOSPHODIESTERASE-4 INHIBITOREN

Title (fr)

INHIBITEURS DE 8-ARYLQUINOLINE PHOSPHODIESTERASE-4 SUBSTITUEE

Publication

EP 1244628 A1 20021002 (EN)

Application

EP 00986937 A 20001220

Priority

CA 0001559 W 20001220
US 17152299 P 19991222

Abstract (en)

[origin: WO0146151A1] Novel substituted 8-arylquinolines represented by Formula (I), or a pharmaceutically acceptable salt thereof, wherein S1, S2 and S3 are independently H, -OH; halogen, -C1-C6alkyl, -NO2, -CN, or -C1-C6alkoxy, wherein the alkyl and alkoxy groups are optionally substituted with 1-5 substituents; wherein each substituent is independently a halogen or OH; R1 is a H, OH, halogen, carbonyl, or -C1-C6alkyl, -cycloC3-C6alkyl, -C1-C6alkenyl, -C1-C6alkoxy, aryl, heteroaryl, -CN, -heterocycloC3-C6alkyl, -amino, -C1-C6alkylamino, -(C1-C6alkyl)(C1-C6alkyl)amino, -C1-C6alkyl(oxy)C1-C6alkyl, -C(O)NH(aryl), -C(O)NH(heteroaryl), -SOnNH(aryl), -SOnNH(heteroaryl), -SOnNH(C1-C6alkyl), -C(O)N(C0-C6alkyl) (C0-C6alkyl), -NH-SOn-(C1-C6alkyl), -SOn-(C1-C6alkyl), -(C1-C6alkyl)-O-C(CN)-dialkylamino, or -(C1-C6alkyl)-SOn-(C1-C6alkal) group, wherein any of the groups is optionally substituted with 1-5 substituents; wherein each substituent is independently a halogen, -OH, -CN, -C1-C6alkyl, -cycloC3-C6alkyl, -C(O)(heterocycloC3-C6alkyl), -C(O)-O-(C0-C6alkyl), -C(O)-aryloxy, -C1-C6alkoxy, -(C0-C6alkyl)(C0-C6alkyl)amino, cycloalkyloxy, acyl, acyloxy, -cycloC3-C6alkyl, heterocycloC3-C6alkyl, aryl, heteroaryl, carbonyl, carbamoyl, or -SOn-(C1-C6alkyl); A is CH, C-ester, or C-R4; R2 and R3 independently is an aryl, heteroaryl, H, halogen, -CN, -C1-C6alkyl, heterocycloC3-6alkyl, -C1-C6alkoxy, carbonyl, carbamoyl, -C(O)OH, -C1-C6alkyl)-SOn-(C1-C6alkyl), -C(O)N(C0-C6alkyl)(C0-C6alkyl), or -C1-C6alkylacylamino group, wherein any of the groups is optionally substituted with 1-5 substituents, wherein each substituent is independently an aryl, heteroaryl, halogen, -NO2, -C(O)OH, carbonyl, -CN, -C1-C6alkyl, -SOn-(C1-C6alkyl), -SOn-(aryl), aryloxy, -heteroaryloxy, C1-C6alkoxy, N-oxide, -C(O)-heterocycloC3-C6alkyl, -NH-cycloC3-C6alkyl, amino, -OH, or -(C0-C6alkyl)(C0-C6alkyl)amino, -C(O)-N(C0-C6alkyl)(C0-C6alkyl) substituent group, wherein each substituent group independently is optionally substituted with -OH, C1-C6alkoxy, -C1-C6alkyl, -cycloC3-C6alkyl, aryloxy, -C(O)OH, -C(O)O(C1-C6alkyl), halogen, -NO2, -CN, -SOn-(C1-C6alkyl), or -C(O)-N(C0-C6alkyl)(C0-C6alkyl); one of R2 and R3 must be an aryl or heteroaryl, optionally substituted; when R2 and R3 are both an aryl or heteroaryl, then R2 and R3 may be optionally connected by a thio, oxy, or (C1-C4alkyl) bridge to form a fused three ring system; are PDE4 inhibitors.

IPC 1-7

C07D 215/12; A61K 31/47; A61K 31/4709; C07D 215/14; C07D 401/10; C07D 413/10; C07D 417/10

IPC 8 full level

A61K 31/47 (2006.01); A61K 31/4709 (2006.01); A61K 45/00 (2006.01); A61P 1/04 (2006.01); A61P 7/12 (2006.01); A61P 9/00 (2006.01); A61P 11/00 (2006.01); A61P 11/06 (2006.01); A61P 11/16 (2006.01); A61P 13/12 (2006.01); A61P 17/00 (2006.01); A61P 17/04 (2006.01); A61P 17/06 (2006.01); A61P 19/02 (2006.01); A61P 19/10 (2006.01); A61P 37/08 (2006.01); C07D 215/12 (2006.01); C07D 215/14 (2006.01); C07D 401/10 (2006.01); C07D 401/14 (2006.01); C07D 405/12 (2006.01); C07D 409/10 (2006.01); C07D 413/10 (2006.01); C07D 413/14 (2006.01); C07D 417/10 (2006.01); C07D 417/12 (2006.01); C07D 417/14 (2006.01)

CPC (source: EP KR)

A61P 1/04 (2018.01 - EP); A61P 7/12 (2018.01 - EP); A61P 9/00 (2018.01 - EP); A61P 11/00 (2018.01 - EP); A61P 11/06 (2018.01 - EP); A61P 11/16 (2018.01 - EP); A61P 13/12 (2018.01 - EP); A61P 17/00 (2018.01 - EP); A61P 17/04 (2018.01 - EP); A61P 17/06 (2018.01 - EP); A61P 19/02 (2018.01 - EP); A61P 19/10 (2018.01 - EP); A61P 25/00 (2018.01 - EP); A61P 29/00 (2018.01 - EP); A61P 31/00 (2018.01 - EP); A61P 35/00 (2018.01 - EP); A61P 37/00 (2018.01 - EP); A61P 37/08 (2018.01 - EP); C07D 215/12 (2013.01 - EP KR); C07D 215/14 (2013.01 - EP KR); C07D 401/10 (2013.01 - EP KR); C07D 401/14 (2013.01 - EP KR); C07D 405/12 (2013.01 - EP KR); C07D 409/10 (2013.01 - EP KR); C07D 413/10 (2013.01 - EP KR); C07D 413/14 (2013.01 - EP KR); C07D 417/10 (2013.01 - EP KR); C07D 417/12 (2013.01 - EP KR); C07D 417/14 (2013.01 - EP)

Designated contracting state (EPC)

AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE TR

DOCDB simple family (publication)

WO 0146151 A1 20010628; AR 029214 A1 20030618; AU 2336201 A 20010703; AU 778531 B2 20041209; BG 106840 A 20030131; BG 65403 B1 20080630; BR 0016651 A 20020910; CA 2393749 A1 20010628; CA 2393749 C 20080617; CN 1221534 C 20051005; CN 1434801 A 20030806; CO 5261613 A1 20030331; CZ 20022171 A3 20021113; DZ 3244 A1 20010628; EA 004747 B1 20040826; EA 200200702 A1 20030227; EE 200200342 A 20030616; EP 1244628 A1 20021002; GE P20053626 B 20051010; HK 1057560 A1 20040408; HR P20020545 A2 20051031; HU P0203896 A2 20030428; HU P0203896 A3 20030528; IL 150114 A0 20021201; IS 6413 A 20020611; JP 2003531112 A 20031021; JP 3782011 B2 20060607; KR 20020082839 A 20021031; MX PA02006329 A 20040514; MY 134008 A 20071130; NO 20023013 D0 20020621; NO 20023013 L 20020822; NZ 520258 A 20040528; PE 20010989 A1 20011001; PL 355752 A1 20040517; SK 8972002 A3 20021106; TW I280240 B 20070501; UA 74815 C2 20060215; YU 47102 A 20050610; ZA 200204862 B 20030317

DOCDB simple family (application)

CA 0001559 W 20001220; AR P000106867 A 20001221; AU 2336201 A 20001220; BG 10684002 A 20020619; BR 0016651 A 20001220; CA 2393749 A 20001220; CN 00818951 A 20001220; CO 00096650 A 20001220; CZ 20022171 A 20001220; DZ 003244 A 20001220; EA 200200702 A 20001220; EE P200200342 A 20001220; EP 00986937 A 20001220; GE AP2000004903 A 20001220; HK 04100511 A 20040126; HR P20020545 A 20020621; HU P0203896 A 20001220; IL 15011400 A 20001220; IS 6413 A 20020611; JP 2001547062 A 20001220; KR 20027008079 A 20020621; MX PA02006329 A 20001220; MY PI20005965 A 20001219; NO 20023013 A 20020621; NZ 52025800 A 20001220; PE 0013962000 A 20001222; PL 35575200 A 20001220; SK 8972002 A 20001220; TW 89127506 A 20001221; UA 2002076108 A 20001220; YU P47102 A 20001220; ZA 200204862 A 20020618