Benzothiazol-2-on derivatives as lipase and phospholipase inhibitorsThe invention relates to benzothiazol-2-on derivatives of general formula (I) with the meanings indicated in the description, the pharmaceutically usable salts thereof, and the use thereof as medicinal substances.The compound of formula i:wherein each group implication is as follows:r1 is (c 5-c 16)-alkyl, (c 1-c 4)-alkylidene group-(c 6-c 10)-aryl, (c 1-c 4)-alkylidene group -(c 5-c 12)-heteroaryl, (c 1-c 4)-alkylidene group-(c 4-c 12)-cycloalkyl, (c 8-c 14)-two ring, wherein aryl, heteroaryl, cycloalkyl or two rings can be by halogen, (c 1-c 6)- alkyl, (c 1-c 3)-alkoxyl group, hydroxyl, (c 1-c 6)-alkylthio, amino, (c 1-c 6)- alkylamino, two-(c 2-c 12)-alkylamino, list-(c 1-c 6)-alkyl amino-carbonyl, two-(c 2-c 8)-alkyl amino-carbonyl, (c 1-c 6)-alkoxy carbonyl, (c 1-c 6)-alkyl oxycarbonyl base, cyano group, trifluoromethyl, trifluoromethoxy, (c 1-c 6)-alkyl sulphonyl or amino alkylsulfonyl replaces one or many;r2 is hydrogen, (c 1-c 6)-alkyl; or r1 and r2 form the monocyclic saturated or undersaturated 4-of part extremely with the nitrogen-atoms that has them7-unit ring system or bicyclic is saturated or the undersaturated 8-to 14-of part unit ring system, wherein ringthe system each member can by 1 to 3 be selected from-chr8-,-cr8r8a-,-(c=r8)-,-nr9-,-c (=o)-,-o-,-s-,-so-,-so 2-atom or atomic group replaces, and condition is two and is selected from-o-,-s-,-so-,-so 2-the unit do not adjoin;r3 is a hydrogen;r4, r5 are hydrogen, halogen, (c identical or differently 1-c 6)-alkyl, (c 1-c 3)-alkoxyl group-(c 1-c 3)- alkylidene group, hydroxyl, (c 1-c 6)-alkylthio, amino, (c 1-c 6)-alkylamino, two -(c 2-c 12)-alkylamino, (c 1-c 6)-alkyl-carbonyl, co-or7, trifluoromethyl, (c 1-c 6)-alkyl sulphonyl, (c 1-c 6)-alkyl sulphinyl, amino-sulfonyl, five fluorine sulfenyl, (c 6-c 10)-aryl, (c 5-c 12)-heteroaryl, co-nr9r10, o-co-nr9r10, o-co-(c 1-c 6)-alkylidene group-co-o-(c 1-c 6)-alkyl, o-co-(c 1-c 6)-alkylidene group-co-oh, o-co-(c 1-c 6)-alkylidene group -co-nr9r10 is unsubstituted or single-or (c that replaces of many-f- 1-c 6)-alkoxyl group; r6 is hydrogen, (c 1-c 3)-alkoxyl group-(c 1-c 3)-alkylidene group, hydroxyl, (c 1-c 6)-alkylthio, amino, (c 1-c 6)-alkylamino, two-(c 2-c 12)-alkylamino, five fluorine sulfenyls, (c 6-c 10)-aryl, (c 5-c 12)-heteroaryl, co-nr9r10, o-co-nr9r10, o-co-(c 1-c 6)-alkylidene group-co-o-(c 1-c 6)-alkyl, o-co-(c 1-c 6)-alkylene base-co-oh, o-co-(c 1-c 6)-alkylidene group-co-nr9r10 or unsubstituted or single-or (c of many-f-replacement 1-c 6)-alkoxyl group; condition be among substituent r 3, r4, the r5 at the most one be halogen, trifluoromethyl or(c 1-c 6)-alkyl; r7 is hydrogen, (c 1-c 6)-alkyl, benzyl; r8, r8a are (c identical or differently 1-c 6)-alkyl, halogen, trifluoromethyl, co-or7, ring propyl group, cyclopropylidene;r9, r10 are hydrogen, (c identical or differently 1-c 6)-alkyl ,-(c 6-c 10)-aryl, (c 5-c 12)-assorted aryl, (c 3-c 12)-cycloalkyl, (c 1-c 4)-alkylidene group-(c 6-c 10)-aryl, (c 1-c 4)- alkylidene group-(c 5-c 12)-heteroaryl, (c 1-c 4)-alkylidene group-(c 3-c 12)-cycloalkyl, (c 8-c 14)-two ring; the tautomeric form of this compound and the salt of its physiological tolerance.
리파제 및 포스포리파제 억제제로서의 벤조티아졸-2-온유도체본 발명은 화학식 I의 벤조티아졸-2-온 유도체, 약제학적으로 유용한 이의 염 및 의약용 물질로서의 이의 용도에 관한 것이다. 화학식 I  상기 화학식 I에서, 치환체는 명세서에 기재된 것과 같다. 화학식 I의 화합물, 당해 화합물의 호변이성체 형태 및 생리학적으로 허용되는 이의 염. 화학식 I [이미지] 상기 화학식 I에서, R1은 (C5-C16)-알킬, (C1-C4)-알킬렌-(C6-C10)-아릴, (C1-C4)-알킬렌-(C5-C12)-헤테로아릴, (C1-C4)-알킬렌-(C4-C12)-사이클로알킬 또는 (C8-C14)-바이사이클이고, 여기서, 아릴, 헤테로아릴, 사이클로알킬 또는 바이사이클은 할로겐, (C1-C6)-알킬, (C1-C3)-알킬옥시, 하이드록시, (C1-C6)-알킬머캅토, 아미노, (C1-C6)-알킬아미노, 디-(C2-C12)-알킬아미노, 모노-(C1-C6)-알킬아미노카보닐, 디-(C2-C8)-알킬아미노카보닐, (C1-C6)-알콕시카보닐, (C1-C6)-알킬카보닐, 시아노, 트리플루오로메틸, 트리플루오로메틸옥시, (C1-C6)-알킬설포닐 또는 아미노설포닐에 의해 1회 이상 치환될 수 있고; R2는 수소 또는 (C1-C6)-알킬이거나; R1 및 R2는 이들이 보유하는 질소 원자와 함께, 모노사이클릭 포화 또는 부분 불포화 4원 내지 7원 환 시스템 또는 바이사이클릭 포화 또는 부분 불포화 8원 내지 14원 환 시스템을 형성하고, 여기서, 환 시스템의 개별적 구성원은 -CHR8-, -CR8R8a-, -(C=R8)-, -NR9-, -C(=O)-, -O-, -S-, -SO- 및 -SO2-로부터의 1 내지 3개의 원자 또는 원자 그룹으로 치환될 수 있으며, 단 -O-, -S-, -SO- 및 -SO2-로부터의 2개의 단위는 인접될 수 없고; R3은 수소이고; R4 및 R5는 동일하거나 상이하게 수소, 할로겐, (C1-C6)-알킬, (C1-C3)-알킬옥시-(C1-C3)-알킬렌, 하이드록시, (C1-C6)-알킬머캅토, 아미노, (C1-C6)-알킬아미노, 디-(C2-C12)-알킬아미노, (C1-C6)-알킬카보닐, CO-OR7, 트리플루오로메틸, (C1-C6)-알킬설포닐, (C1-C6)-알킬설피닐, 아미노설포닐, 펜타플루오로설파닐, (C6-C10)-아릴, (C5-C12)-헤테로아릴, CO-NR9R10, O-CO-NR9R10, O-CO-(C1-C6)-알킬렌-CO-O-(C1-C6)-알킬, O-CO-(C1-C6)-알킬렌-CO-OH, O-CO-(C1-C6)-알킬렌-CO-NR9R10 또는 비치환되거나 단일- 또는 다중-F-치환된 (C1-C6)-알킬옥시이고; R6은 수소, (C1-C3)-알킬옥시-(C1-C3)-알킬렌, 하이드록시, (C1-C6)-알킬머캅토, 아미노, (C1-C6)-알킬아미노, 디-(C2-C12)-알킬아미노, 펜타플루오로설파닐, (C6-C10)-아릴, (C5-C12)-헤테로아릴, CO-NR9R10, O-CO-NR9R10, O-CO-(C1-C6)-알킬렌-CO-O-(C1-C6)-알킬, O-CO-(C1-C6)-알킬렌-CO-OH, O-CO-(C1-C6)-알킬렌-CO-NR9R10 또는 비치환되거나 단일- 또는 다중-F-치환된 (C1-C6)-알킬옥시이고; 단, 치환체 R3, R4 및 R5 중 1개 이하는 할로겐, 트리플루오로메틸 또는 (C1-C6)-알킬이고; R7은 수소, (C1-C6)-알킬 또는 벤질이고; R8 및 R8a는 동일하거나 상이하게 (C1-C6)-알킬, 할로겐, 트리플루오로메틸, CO-OR7, 사이클로프로필 또는 사이클로프로필렌이고; R9 및 R10은 동일하거나 상이하게 수소, (C1-C6)-알킬, -(C6-C10)-아릴, (C5-C12)-헤테로아릴, (C3-C12)-사이클로알킬, (C1-C4)-알킬렌-(C6-C10)-아릴, (C1-C4)-알킬렌-(C5-C12)-헤테로아릴, (C1-C4)-알킬렌-(C3-C12)-사이클로알킬 또는 (C8-C14)-바이사이클이다. 