Title:
金属タンパク質(metalloprotein)インヒビターとしてのアズレンヒドロキサム酸誘導体
Document Type and Number:
Japanese Patent JP3545338
Kind Code:
B2
Abstract:
Substituted carbamoylmethyl-azulene derivatives (I) are new. 6-(Substituted carbamoylmethyl)-azulene derivatives of formula (I) and their tautomers, enantiomers, diastereomers, racemates, salts, esters and derivatives which are hydrolysed or metabolized in vivo to compounds (I) are new: R1-R3 = H; OH; NH2; SH; optionally substituted saturated or unsaturated 1-15C aliphatic group; alkoxy; mono- or di-alkylamino; alkylmercapto; alkylsulphinyl; alkylsulphonyl; alkenyl; alkynyl; alkenyloxy; alkenylmercapto; alkynyloxy; alkynylmercapto; mono- or di-alkylcarbonylamino; alkylaminocarbonyl; CHO; alkylcarbonyl; COOH; alkoxycarbonyl; alkenyloxycarbonyl; alkynyloxycarbonyl; carboxyalkyl; alkoxycarbonylalkyl; alkenyloxycarbonylalkyl; alkynyloxycarbonylalkyl; NO2; CN: halo; CF3; N3; optionally substituted phenyl or phenylcarbonyl; 7-15C mono- di- or tricarbocyclyl; or heterocyclyl; R5, R6 = as R1-R3 other than OH, NH2 or SH; R7 = H or alkyl; X = bond; alkylene; CO or alkylenecarbonyl; R8 = alkyl optionally substituted by OH, alkoxy, NH2 or mono- or dialkylamino; 1,3-dioxolan-4-yl optionally substituted in the 2-position; PO(R11)(R12); PO(OR13)(OR14); or, when X is other than a bond, then R8 may also be OH, alkoxy, hydroxyalkoxy, alkanoyloxy, alkylcarbonylamino, alkoxycarbonyloxy, alkanoyloxyalkyl, carboxyvinyl, optionally substituted aminoalkanoyloxy, aminoalkylphenyl or aminoalkylbenzoyloxy; alkanoyloxyalkoxy or NR9R10; R9, R10 = H or alkyl optionally substituted by OH, alkoxy, NH2 or mono- or dialkylamino; or R9 = H and R10 = OH; imidazolin-2-yl; or tetrazol-5-yl; or NR9R10 = heterocyclic ring optionally containing N or O, optionally substituted with alkyl, alkoxy, OH, hydroxyalkyl, oxo, COOH, CONH2 or alkoxycarbonyl and optionally benzo-fused; R11, R12 = alkyl; R13, R14 = H or alkyl.
Inventors:
Dick Hout, Joachim
Fribe, Walter-Gunner
Glams, frank
Hack, liner
Reinert, Herbert
Fribe, Walter-Gunner
Glams, frank
Hack, liner
Reinert, Herbert
Application Number:
JP2000539005A
Publication Date:
July 21, 2004
Filing Date:
December 09, 1998
Export Citation:
Assignee:
Roche Diagnostics Gaem Behr
International Classes:
A61K31/015; A61K31/16; A61K31/357; A61K31/40; A61K31/41; A61K31/4164; A61K31/445; A61K31/4453; A61K31/495; A61K31/5375; A61K31/662; A61P29/00; C07C239/20; C07C259/06; C07C271/60; C07D233/02; C07D257/06; C07D295/088; C07D295/12; C07D295/08; C07D295/185; C07D295/20; C07D317/22; C07D317/30; C07F9/38; C07F9/40; (IPC1-7): C07D295/08; A61K31/16; A61K31/357; A61K31/40; A61K31/41; A61K31/4164; A61K31/445; A61K31/4453; A61K31/495; A61K31/5375; A61K31/662; A61P29/00; C07C239/20; C07D233/02; C07D257/06; C07D295/20; C07D317/30; C07F9/38; C07F9/40
Domestic Patent References:
| JP58039640A |
Foreign References:
| US5081152 | ||||
| US5235076 |
Attorney, Agent or Firm:
Hajime Tsukuni
Fumio Shinoda
Fumio Shinoda