EP 1718614 A1 20061108 - PYRIDINAMIDE DERIVATIVE AS KINASE INHIBITORS
Title (en)
PYRIDINAMIDE DERIVATIVE AS KINASE INHIBITORS
Title (de)
PYRIDINAMID-DERIVATE ALS KINASE-INHIBITOREN
Title (fr)
DERIVES PYRIDINAMIDE SERVANT D'INHIBITEURS DE KINASE
Publication
Application
Priority
- EP 2005000273 W 20050113
- DE 102004009238 A 20040226
Abstract (en)
[origin: DE102004009238A1] Aryl amide compounds (I) and their salts, derivatives, solvates and/or stereoisomers including their mixtures in all ratios are new. Aryl amide compounds (I) of formula (Ar 1>-N(R 2>)-CH(=Y)-Ar 2>-Z-Ar 3>) and their salts, derivatives, solvates and/or stereoisomers including their mixtures in all ratios are new. Ar 1>-Ar 3>aromatic (optionally substituted with R 1>) or Het; Het : 1-2 aromatic heterocyclic ring with 1-4 N-, O- and/or S-; R 1>H, A, aryl, OR 4>, SR 4>, Oaryl, Saryl, N(R 4>) 2, NHaryl, Hal, NO 2, CN, (CH 2) mCOOR 4>, (CH 2) mCOOaryl, (CH 2) mCON(R 4>) 2, (CH 2) mCONHaryl, COR 4>, COaryl, S(O) mA, S(O) maryl, NHCOA, NHCOaryl, NHSO 2A, NHSO 2aryl, SO 2N(R 4>) 2, O(CH 2) n, N(R 4>) 2, O(CH 2) nNHR 3>, O(CH 2) n-oxo-piperazine, O(CH 2) n-oxomorpholine, O(CH 2) n-oxopyrrolidine, O(CH 2) nC(CH 2) 2(CH 2) nN(R 4>) 2, N(CH 2) nC(CH 3) 2(CH 2) nN(R 4>) 2, O(CH 2) nN(R 4>)SO mA, O(CH 2) nN(R 4>)SO mN(R 4>)A, O(CH 2) nN(R 4>)SO maryl, (CH 2) nN(R 4>)SO mA, (CH 2) nN(R 4>)SO mN(R 4>)A, (CH 2) nN(R 4>)SO maryl, O(CH 2) nSO mA, O(CH 2) nSO mN(R 4>)A, O(CH 2) nSO maryl, (CH 2) nSO mA, (CH 2) nSO mN(R 4>)A and/or (CH 2) nSO maryl; Y : O, S, C-NO-2, C(CN) 2 or N-R 3>; Z : G 1> n, G 1> nEG 2> m, EG 1> nG 2> m or G 1> nG 2> mE; R 2>-R 4>H, A or -alkylene-aryl; A : 1-10C alkyl (where 1-2 CH 2- group is replaced with O-, S and/or with -CH=CH- and/or 1-7H atom is replaced with Hal), aryl (optionally substituted with A), phenyl, OA, SA, Ophenyl, NH 2, NA 2, hal, NO 2, CN, (CH 2) mCOOR 4>, (CH 2) mCON(R 4>) 2, COR 4>, COaryl, S(O) mA, NHCOA or NHSO 2A substituted phenyl; E : O, SO m, NR 1>, CO, C=N or alkene; G 1>, G 2>CR 1>R 1> or E; Hal : F, Cl, Br or I; n : 0-5; and m : 0-2. Independent claims are also included for: (1) the preparation of (I); (2) medicament comprising (I), carriers and/or adjuvants and optionally at least additional drug active agents; (3) a set (kit) comprising divided packings of (I) and additional drug active agents; and (4) use of (I) in combination with radiotherapy and a compound (estrogen receptor modulators, androgen receptor modulators, retinoid receptor modulators, cytotoxic drug, antiproliferative agents, prenyl-proteintransferase inhibitors, 3-hydroxy 3-methyl glutaryl coenzyme A reductase inhibitors, HIV-protease inhibitors, reverse transcriptase inhibitors, growth factor receptor inhibitors and angiogenesis inhibitors) for preparing medicaments for the treatment and/or prophylaxis of diseases. ACTIVITY : Antiangiogenic; Cytostatic; Antidiabetic; Ophthalmological; Osteopathic; Antiarthritic; Antipsoriatic; Antirheumatic; Antiinflammatory; Dermatological; Gynecological; Vulnerary; Immunostimulant; Immunosuppressive. MECHANISM OF ACTION : Kinase activator; Kinase inhibitor; Tyrosine kinase inhibitor; Raf-kinase inhibitor. The ability of (I) to inhibit tyrosine kinase activity using biological assays. The results showed that (I) inhibited vascular endothelial growth factor stimulated mitogenesis in a culture containing human endothelial cells at HK-50 value of 0.01-5 microM.
IPC 8 full level
A61K 31/435 (2006.01); A61P 35/00 (2006.01); C07D 213/81 (2006.01); C07D 401/12 (2006.01)
CPC (source: EP US)
A61P 9/00 (2017.12 - EP); A61P 9/10 (2017.12 - EP); A61P 13/08 (2017.12 - EP); A61P 15/08 (2017.12 - EP); A61P 17/00 (2017.12 - EP); A61P 17/02 (2017.12 - EP); A61P 17/06 (2017.12 - EP); A61P 19/02 (2017.12 - EP); A61P 27/02 (2017.12 - EP); A61P 29/00 (2017.12 - EP); A61P 35/00 (2017.12 - EP); A61P 35/02 (2017.12 - EP); A61P 37/06 (2017.12 - EP); A61P 37/08 (2017.12 - EP); A61P 43/00 (2017.12 - EP); C07D 213/81 (2013.01 - EP US); C07D 401/12 (2013.01 - EP US)
Citation (search report)
See references of WO 2005085202A1
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU MC NL PL PT RO SE SI SK TR
DOCDB simple family (publication)
DE 102004009238 A1 20050908; AU 2005219496 A1 20050915; CA 2557302 A1 20050915; EP 1718614 A1 20061108; JP 2007523921 A 20070823; US 2007142440 A1 20070621; WO 2005085202 A1 20050915
DOCDB simple family (application)
DE 102004009238 A 20040226; AU 2005219496 A 20050113; CA 2557302 A 20050113; EP 05700886 A 20050113; EP 2005000273 W 20050113; JP 2007500077 A 20050113; US 59072405 A 20050113