EP 1119566 A1 20010801 - NOVEL HETEROCYCLYL-METHYL-SUBSTITUTED PYRAZOLES
Title (en)
NOVEL HETEROCYCLYL-METHYL-SUBSTITUTED PYRAZOLES
Title (de)
NEUE HETEROCYCLYL-METHYL-SUBSTITUIERTE PYRAZOLE
Title (fr)
NOUVEAUX PYRAZOLES HETEROCYCLIQUES METHYL-SUBSTITUES
Publication
Application
Priority
- DE 19846514 A 19981009
- EP 9907202 W 19990929
Abstract (en)
[origin: DE19846514A1] 1-(Aryl or heterocyclyl)methyl-3-heteroaryl-indazole derivatives are new. The 1-(aryl or heterocyclyl)methyl-3-heteroaryl-indazole derivatives are compounds of formula (I) and their isomers, salts and N-oxides are new: R1 = 6-membered N-containing heteroaryl substituted with:(A) alkyl, alkenyl, alkynyl, cycloalkoxy or aryl (each optionally substituted with 17 groups (when aryl = phenyl, this must be substituted); and/or (B) saturated or unsaturated heterocyclyl optionally substituted with 6 groups; and/or (C) alkyl substituted with 13 groups; and/or (D) alkoxy substituted with OH, amino (optionally mono- or disubstituted with alkyl, cycloalkyl or acyl) or a N-bonded saturated or partly unsaturated heterocycle; and/or (E) halo-acyl, acyloxy, or arylthio or heteroarylthio (each optionally substituted with halo, alkyl or alkoxy); and/or (F) SO2Rq or SORr; and/or (G) -SO3H; and/or (H) -C(O)N=C(NH2)2 or -C= NH(NH2); and/or (I) -CONRsRt; and/or (J) -NRvRw; and/or (K) -PO(OR)(OR'); and R<1> is also optionally mono- or disubstituted with 16 groups or a group of formula (i), (j) or -CH=N-OR11 (k); Rq and Rr = alkyl, cycloalkyl, or aryl or heteroaryl (each optionally substituted with halo, alkyl or alkoxy); Rs and Rt = H, alkyl or cycloalkyl (each optionally substituted with 8 groups) or aryl or partly or fully unsaturated heterocyclyl (each optionally substituted with halo, alkyl, cycloalkyl or alkoxy); or NRsRt = a saturated or partly unsaturated heterocycle; Rv, Rw = acyclic or cyclic acyl, -SO2-alkyl, hydroxymethyl, hydroxyethyl, alkoxycarbonyl, alkoxyalkyl, acyloxymethyl or a group of formula (a), COO-CHRy-O-CO-Rx (b), of formulae (c)-(f), COO-CHRy-O-Rx or of formula (h);: Rx, Ry = H or alkyl; Rz = alkyl or cycloalkyl; or one of Rv and Rw = H; m = 0-2; R' = alkyl, aryl or benzyl; and R4, R5 = H, acyl, or alkyl optionally substituted with 6 groups; or NR4R5 = a saturated or partly unsaturated heterocycle; Alk = alkyl optionally substituted with 9 groups; R11 = H or alkyl; a = 1-3; b, b' = 1-3; R2+R3 = a phenyl ring optionally substituted with 16 groups; and A = phenyl or an aromatic or saturated heterocycle (each optionally substituted with 16 groups). The full definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are also included for: a) the preparation of compounds (I); and b) a pharmaceutical preparation containing a compound (I) and optionally (i) an organic nitrate or a NO donor or (ii) a compound which inhibits cyclic guanosine monophosphate (cGMP) degradation.
IPC 1-7
C07D 401/14; C07D 403/04; C07F 9/6512; A61K 31/505; A61K 31/495
IPC 8 full level
A61K 31/506 (2006.01); A61K 31/662 (2006.01); A61P 7/06 (2006.01); A61P 9/10 (2006.01); C07D 401/14 (2006.01); C07D 403/04 (2006.01); C07F 9/6512 (2006.01); C07F 9/6558 (2006.01); C07H 13/12 (2006.01)
CPC (source: EP)
A61P 7/06 (2017.12); A61P 9/10 (2017.12); C07D 401/14 (2013.01); C07D 403/04 (2013.01); C07F 9/6512 (2013.01); C07F 9/65583 (2013.01); C07H 13/12 (2013.01)
Citation (search report)
See references of WO 0021954A1
Designated contracting state (EPC)
DE ES FR GB IT
DOCDB simple family (publication)
DE 19846514 A1 20000420; AU 6330099 A 20000501; CA 2346698 A1 20000420; EP 1119566 A1 20010801; JP 2002527435 A 20020827; WO 0021954 A1 20000420
DOCDB simple family (application)
DE 19846514 A 19981009; AU 6330099 A 19990929; CA 2346698 A 19990929; EP 9907202 W 19990929; EP 99950564 A 19990929; JP 2000575860 A 19990929