Title (en)

NOVEL 1,2,5-TRISUBSTITUTED 1,2-DIHYDRO-INDAZOL-3-ONES WITH ANTI-ASTHMATIC, ANTI-ALLERGIC, ANTI-INFLAMMATORY, IMMUNO-MODULATING AND NEURO-PROTECTIVE EFFECT, METHOD FOR THE PRODUCTION AND USE THEREOF AS A MEDICAMENT

Title (de)

NEUE 1,2,5-TRISUBSTITUIERTE 1,2-DIHYDRO-INDAZOL-3-ONE MIT ANTIASTHMATISCHER, ANTIALLERGISCHER, ENTZÜNDUNGSHEMMENDER, IMMUNMODULIERENDER UND NEUROPROTEKTIVER WIRKUNG, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL

Title (fr)

NOUVELLES 1,2-DIHYDRO-INDAZOL-3-ONES TRISUBSTITUEES AUX POSITIONS 1,2,5, A EFFET ANTI-ASTHMATIQUE, ANTI-ALLERGIQUE, ANTI-INFLAMMATOIRE, IMMUNOMODULATEUR ET NEUROPROTECTEUR, LEUR PROCEDE DE PRODUCTION ET LEUR UTILISATION COMME MEDICAMENT

Publication

EP 1077948 A1 20010228 (DE)

Application

EP 99950343 A 19990401

Priority

• DE 19821003 A 19980511
• EP 9902291 W 19990401

Abstract (en)

[origin: US6180637B1] The invention relates to 1,2,5-trisubstituted 1,2-dihydroindazol-3-ones of formula (I)whereinX is -SO2-, -SO-, -(CH2)p-, -(CH2)p-O-, -(CH2)p-(C=O)-, -(CH2)p-(C=O)-NH-, -(CH2)p-CHOH-, -CHOH-(CH2)p-, -(CH2)p-CH=CH-, -CH=CH-(CH2)p-,Y is -(C=O)-, -(C=O)-NH-, -(C=O)-NH-(CH2)p-, -C=O)-(CH2)p-, -(CH2)p-, -(CH2)p-O-, -(CH2)p-(C=O)-, -(CH2)p-(C=O)-NH-, -(CH2)p-(C=O)-NH-(CH2)p-, -(CH2)p-CHOH-, -CHOH-(CH2)p-, -(CH2)p-CH=CH-, -CH=CH-(CH2)p-,Z is -O-, -O-(CH2)p-, -NH-, -NH-(C=O)-, -NH-(C=O)-NH-, -NH-(C=O)-O-, -NH-CH2-(C=O)- and -NH-(C=O)-CH2-,P is a cardinal number from 1 to 4,R1, R2 and R3 can be the same or different and are:mono-, bi- or tricyclic saturated or mono- or polyunsaturated carbocycles having from 5 to 14 ring members; or mono-, bi- or tricyclic saturated or mono- or polyunsaturated heterocycles having from 5 to 15 ring members and from 1 to 6 heteroatoms,in which the carbocycles and the heterocycles can be mono- or polysubstituted by:C1-6-alkyl, -O-C1-6-alkyl, -O-C3-7-cycloalkyl, mono-, bi- or tricyclic saturated or mono- or polyunsaturated carbocycles having from 3 to 14 ring members, mono-, bi- or tricyclic saturated or mono- or polyunsaturated heterocycles having from 5 to 15 ring members and from 1 to 6 heteroatoms,R1 is also H, provided that when X is CH2, then R1 is not H,R3-Z is also NO2,and their pharmaceutically acceptable salts,but excluding compounds of formula (I) in whichif Z is -NH-(C=O)-, -NH-(C=O)-NH-, -NH-(C=O)-O-, -NH-(C=O)-CH2 and at the same time R1 is phenyl, monosubstituted or polysubstituted by -COOH, -COOC1-6-alkyl, -(CH2)p-COOH, -(CH2)p-COOC1-6-alkyl -CONHC1-6-alkyl, -CONHC6-14-aryl, -CONHSO2C1-6-alkyl, -CONHSO2C6-4-aryl, 1H-tetrazol-5-yl, then R2 is not phenyl, monosubstituted or polysubstituted by CN, halogen, C1-4-alkyl, C1-4-alkyloxy, CF3; andif R3-Z is NO2, then R1-X is not benzyl or 4-methoxybenzyl, and R2-Y is not benzyl or 2-picolyl at the same time; and to pharmaceutical treatment processes, and processes for making.

IPC 1-7

C07D 231/56; C07D 417/06; C07D 403/06; A61K 31/415; A61K 31/425; A61K 31/495

IPC 8 full level

A61K 9/02 (2006.01); A61K 9/08 (2006.01); A61K 9/12 (2006.01); A61K 9/14 (2006.01); A61K 9/20 (2006.01); A61K 9/28 (2006.01); A61K 9/48 (2006.01); A61K 9/70 (2006.01); A61K 31/416 (2006.01); A61K 31/417 (2006.01); A61K 31/427 (2006.01); A61K 31/496 (2006.01); A61K 31/506 (2006.01); A61K 31/517 (2006.01); A61P 11/06 (2006.01); A61P 25/00 (2006.01); A61P 25/16 (2006.01); A61P 25/28 (2006.01); A61P 29/00 (2006.01); A61P 37/02 (2006.01); A61P 37/08 (2006.01); A61P 43/00 (2006.01); C07D 231/56 (2006.01); C07D 403/06 (2006.01); C07D 417/06 (2006.01)

CPC (source: EP KR US)

A61P 11/06 (2018.01 - EP); A61P 25/00 (2018.01 - EP); A61P 25/16 (2018.01 - EP); A61P 25/28 (2018.01 - EP); A61P 29/00 (2018.01 - EP); A61P 37/02 (2018.01 - EP); A61P 37/08 (2018.01 - EP); A61P 43/00 (2018.01 - EP); C07D 231/56 (2013.01 - EP KR US); C07D 235/26 (2013.01 - KR); C07D 277/22 (2013.01 - KR); C07D 295/135 (2013.01 - KR); C07D 401/06 (2013.01 - KR); C07D 403/06 (2013.01 - EP US); C07D 417/06 (2013.01 - EP KR US)

Designated contracting state (EPC)

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

DOCDB simple family (publication)

US 6180637 B1 20010130; AR 018605 A1 20011128; AU 4257699 A 19991129; AU 745796 B2 20020328; BG 104910 A 20010629; BR 9911772 A 20010206; CA 2271837 A1 19991111; CN 1309642 A 20010822; CO 5021131 A1 20010327; DE 19821003 A1 19991118; EP 1077948 A1 20010228; HK 1038751 A1 20020328; HU P0101707 A2 20020328; HU P0101707 A3 20020628; IL 139358 A0 20011125; JP 2002514627 A 20020521; KR 20010025011 A 20010326; NO 20005698 D0 20001110; NO 20005698 L 20010108; NZ 508646 A 20021126; PL 344254 A1 20011022; SK 17082000 A3 20010911; TR 200003302 T2 20010221; TW 448163 B 20010801; WO 9958504 A1 19991118; WO 9958504 A9 20000203; ZA 200006151 B 20001206

DOCDB simple family (application)

US 30560299 A 19990505; AR P990102212 A 19990511; AU 4257699 A 19990401; BG 10491000 A 20001103; BR 9911772 A 19990401; CA 2271837 A 19990511; CN 99808515 A 19990401; CO 99028290 A 19990507; DE 19821003 A 19980511; EP 9902291 W 19990401; EP 99950343 A 19990401; HK 02100376 A 20020117; HU P0101707 A 19990401; IL 13935899 A 19990401; JP 2000548308 A 19990401; KR 20007012614 A 20001110; NO 20005698 A 20001110; NZ 50864699 A 19990401; PL 34425499 A 19990401; SK 17082000 A 19990401; TR 200003302 T 19990401; TW 88106565 A 19990423; ZA 200006151 A 20001031