EP 1435958 A1 20040714 - USE OF PHOSPHORODIESTERASE IV INHIBITORS

Title (en)

USE OF PHOSPHORODIESTERASE IV INHIBITORS

Title (de)

VERWENDUNG VON PHOSPHODIESTERASE IV - INHIBITOREN

Title (fr)

UTILISATION D'INHIBITEURS DE LA PHOSPHODIESTERASE IV

Publication

EP 1435958 A1 20040714 (DE)

Application

EP 02777150 A 20020919

Priority

DE 10150517 A 20011012
EP 0210507 W 20020919

Abstract (en)

[origin: DE10150517A1] The use of phenyl-substituted 2,3,4,5-tetrahydro-pyridazin-3-one, 3,6-dihydro-thiadiazin-2-one or 3,6-dihydro-oxadiazin-2-one derivatives (I) for treatment of osteoporosis, tumors, tumor metastases, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, ulcerative colitis or AIDS. The use of phenyl-substituted 2,3,4,5-tetrahydro-pyridazin-3-one, 3,6-dihydro-thiadiazin-2-one or 3,6-dihydro-oxadiazin-2-one derivatives of formula (I) or their salts, for treatment of osteoporosis, tumors, tumor metastases, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, ulcerative colitis or AIDS. (i) X = CH2 or S, provided that R<3> is in the 3-position and R<4> in the 4-position if X = S; Q = -Q'-R<5>; R<1>, R<2> = H or A; R<3>, R<4> = OH, OR<10>, SR<10>, SOR<10>, SO2R<10>, halo, OCH2O, NO2, NH2, NHR<10> or NR<10>R<11>; R<5> = phenyl (optionally substituted (os) by R<6> and/or R<7>); Q' = direct bond or 1-6C alkylene; R<6>, R<7> = NH2, NR<8>R<9>, NHR<10>, NR<10>R<11>, NO2, halo, OA, COOH or COOA; R<8>, R<9> = H, 1-8C acyl (os by 1-5 F and/or Cl), COOA, SOA, SO2A, CONH2, CONHA, CONA2, COCOOH, COCOOA, COCONH2, COCONHA or COCONA2; A = 1-6C alkyl (os by 1-5 F and/or Cl); R<10>, R<11> = A, 3-7C cycloalkyl, 4-8C methylenecycloalkyl or 2-8C alkenyl; (ii) X = CH2, S or O; Q = -Q'-C6H4-NHCOB; Q' = direct bond or 1-6C alkylene; B = aromatic heterocycle with 1-4 N, O and/or S heteroatom(s), bonded via N or C, os by 1-3 of halo, A and/or OA and optionally fused with a benzene or pyridine ring; R<1>, R<2> = H or A; R<3>, R<4> = OH, OR<5>, SR<5>, SOR<5>, SO2R<5>, halo, OCH2O, NO2, NH2, NHR<5> or NR<5>R<6>, R<3> being in the 3-position and R<4> in the 4-position; R<5>, R<6> = A, 3-7C cycloalkyl, 4-8C methylenecycloalkyl or 2-8C alkenyl; A = 1-10C alkyl (os by 1-5 F and/or Cl); (iii) X = S; Q = H; R<1>, R<2> = H or A; R<3> = H, OA or OA'; R<4> = OA'; A = 1-6C alkyl; A' = 1-6C alkyl, substituted by 1-13 F or Cl; (iv) X = S; Q = -Q'-R<5>; Q' = 1-6C alkylene; R<5> = NR<6>R<7>; or tri-, tetra-, penta- or hexamethyleneimino (optionally having one CH2 replaced by O); R<1>, R<2>, R<6>, R<7> = H or A; R<3>, R<4> = OH, OA, SA, SOA, SO2A, halo, OCH2O, 3-7C cycloalkoxy or OA'; A = 1-6C alkyl; A' = 1-6C alkyl, substituted by 1-13 F; or (v) X = CH2 or S; Q = -Q'-C6H4-NHCOB; Q' = direct bond or 1-4C alkylene; B = -YR<5> or -O-YR<5>; Y = direct bond or 1-10C alkylene; R<3>, R<4> = OH, OA, SA, SOA, SO2A, halo, OCH2O, NO2, NH2, NHA or NAA', R<3> being in the 3-position and R<4> in the 4-position; A, A' = 1-10C alkyl (os by 1-5 F and/or Cl), 3-7C cycloalkyl or 4-8C methylenecycloalkyl; R<5> = NH2,. NHA, NA2 or 3-8 membered saturated heterocycle (containing at least one N, os by A or OH and optionally having further CH2 groups replaced by NA, S or O).

IPC 1-7

A61K 31/50; A61K 31/54; A61K 31/535; A61P 19/10; A61P 35/00; A61P 37/00; A61P 3/10

IPC 8 full level

A61K 31/50 (2006.01); A61K 31/501 (2006.01); A61K 31/535 (2006.01); A61K 31/5395 (2006.01); A61K 31/54 (2006.01); A61K 31/549 (2006.01); A61P 1/04 (2006.01); C07D 237/04 (2006.01); A61P 3/10 (2006.01); A61P 9/10 (2006.01); A61P 19/02 (2006.01); A61P 19/10 (2006.01); A61P 25/00 (2006.01); A61P 29/00 (2006.01); A61P 31/18 (2006.01); A61P 35/00 (2006.01); A61P 35/04 (2006.01); A61P 37/00 (2006.01); A61P 43/00 (2006.01); C07D 285/16 (2006.01); C07D 401/12 (2006.01); C07D 411/12 (2006.01); C07D 413/12 (2006.01)

CPC (source: EP KR US)

A61K 31/50 (2013.01 - EP US); A61K 31/501 (2013.01 - KR); A61K 31/535 (2013.01 - EP US); A61K 31/54 (2013.01 - EP US); A61P 1/04 (2018.01 - EP); A61P 3/08 (2018.01 - EP); A61P 3/10 (2018.01 - EP); A61P 9/10 (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 31/18 (2018.01 - EP); A61P 35/00 (2018.01 - EP); A61P 35/04 (2018.01 - EP); A61P 37/00 (2018.01 - EP); A61P 43/00 (2018.01 - EP)

Designated contracting state (EPC)

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

DOCDB simple family (publication)

US 2004235845 A1 20041125; AR 037741 A1 20041201; AU 2002338734 B2 20071108; CA 2460135 A1 20030424; CA 2460135 C 20100824; CN 1564687 A 20050112; CZ 2004457 A3 20050413; DE 10150517 A1 20030417; EP 1435958 A1 20040714; HU P0401641 A2 20041129; HU P0401641 A3 20070228; JP 2005505604 A 20050224; KR 20050028900 A 20050323; MX PA04002639 A 20040607; NO 20041938 L 20040511; SK 1652004 A3 20050505; WO 03032993 A1 20030424

DOCDB simple family (application)

US 49236704 A 20040412; AR P020103824 A 20021011; AU 2002338734 A 20020919; CA 2460135 A 20020919; CN 02819863 A 20020919; CZ 2004457 A 20020919; DE 10150517 A 20011012; EP 0210507 W 20020919; EP 02777150 A 20020919; HU P0401641 A 20020919; JP 2003535796 A 20020919; KR 20047005415 A 20040412; MX PA04002639 A 20020919; NO 20041938 A 20040511; SK 1652004 A 20020919