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Medicaments containing pyridazinone, thiadiazinone or oxadiazinone derivatives, used e.g. for treatment of osteoporosis, tumors, atherosclerosis, rheumatoid arthritis or multiple sclerosis
Medicaments containing pyridazinone, thiadiazinone or oxadiazinone derivatives, used e.g. for treatment of osteoporosis, tumors, atherosclerosis, rheumatoid arthritis or multiple sclerosis
The use of phenyl-substituted 2,3,4,5-tetrahydro-pyridazin-3-one, 3,6-dihydro-thiadiazin-2-one or 3,6-dihydro-oxadiazin-2-one derivatives (I) for treatment of osteoporosis, tumors, tumor metastases, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, ulcerative colitis or AIDS. The use of phenyl-substituted 2,3,4,5-tetrahydro-pyridazin-3-one, 3,6-dihydro-thiadiazin-2-one or 3,6-dihydro-oxadiazin-2-one derivatives of formula (I) or their salts, for treatment of osteoporosis, tumors, tumor metastases, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, ulcerative colitis or AIDS. (i) X = CH2 or S, provided that R3 is in the 3-position and R4 in the 4-position if X = S; Q = -Q'-R5; R1, R2 = H or A; R3, R4 = OH, OR10, SR10, SOR10, SO2R10, halo, OCH2O, NO2, NH2, NHR10 or NR10R11; R5 = phenyl (optionally substituted (os) by R6 and/or R7); Q' = direct bond or 1-6C alkylene; R6, R7 = NH2, NR8R9, NHR10, NR10R11, NO2, halo, OA, COOH or COOA; R8, R9 = H, 1-8C acyl (os by 1-5 F and/or Cl), COOA, SOA, SO2A, CONH2, CONHA, CONA2, COCOOH, COCOOA, COCONH2, COCONHA or COCONA2; A = 1-6C alkyl (os by 1-5 F and/or Cl); R10, R11 = A, 3-7C cycloalkyl, 4-8C methylenecycloalkyl or 2-8C alkenyl; (ii) X = CH2, S or O; Q = -Q'-C6H4-NHCOB; Q' = direct bond or 1-6C alkylene; B = aromatic heterocycle with 1-4 N, O and/or S heteroatom(s), bonded via N or C, os by 1-3 of halo, A and/or OA and optionally fused with a benzene or pyridine ring; R1, R2 = H or A; R3, R4 = OH, OR5, SR5, SOR5, SO2R5, halo, OCH2O, NO2, NH2, NHR5 or NR5R6, R3 being in the 3-position and R4 in the 4-position; R5, R6 = A, 3-7C cycloalkyl, 4-8C methylenecycloalkyl or 2-8C alkenyl; A = 1-10C alkyl (os by 1-5 F and/or Cl); (iii) X = S; Q = H; R1, R2 = H or A; R3 = H, OA or OA'; R4 = OA'; A = 1-6C alkyl; A' = 1-6C alkyl, substituted by 1-13 F or Cl; (iv) X = S; Q = -Q'-R5; Q' = 1-6C alkylene; R5 = NR6R7; or tri-, tetra-, penta- or hexamethyleneimino (optionally having one CH2 replaced by O); R1, R2, R6, R7 = H or A; R3, R4 = OH, OA, SA, SOA, SO2A, halo, OCH2O, 3-7C cycloalkoxy or OA'; A = 1-6C alkyl; A' = 1-6C alkyl, substituted by 1-13 F; or (v) X = CH2 or S; Q = -Q'-C6H4-NHCOB; Q' = direct bond or 1-4C alkylene; B = -YR5 or -O-YR5; Y = direct bond or 1-10C alkylene; R3, R4 = OH, OA, SA, SOA, SO2A, halo, OCH2O, NO2, NH2, NHA or NAA', R3 being in the 3-position and R4 in the 4-position; A, A' = 1-10C alkyl (os by 1-5 F and/or Cl), 3-7C cycloalkyl or 4-8C methylenecycloalkyl; R5 = NH2,. NHA, NA2 or 3-8 membered saturated heterocycle (containing at least one N, os by A or OH and optionally having further CH2 groups replaced by NA, S or O).
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机译：苯基取代的2,3,4,5-四氢哒嗪-3-酮，3,6-二氢噻二嗪-2-酮或3,6-二氢-恶二嗪-2-酮衍生物（I）的用途治疗骨质疏松症，肿瘤，肿瘤转移，动脉粥样硬化，类风湿性关节炎，多发性硬化症，糖尿病，溃疡性结肠炎或艾滋病。式（I）的苯基取代的2,3,4,5-四氢哒嗪-3-酮，3,6-二氢噻二嗪-2-酮或3,6-二氢-恶二嗪-2-酮衍生物的用途）或其盐，用于治疗骨质疏松症，肿瘤，肿瘤转移，动脉粥样硬化，类风湿性关节炎，多发性硬化症，糖尿病，溃疡性结肠炎或艾滋病。 （i）X ＝ CH 2或S，条件是如果X ＝ S，则R 3位于3位且R 4位于4位; Q = -Q'-R <5>; R 1，R 2 ＝ H或A; R 3，R 4 ＝ OH，OR 10，SR 10，SOR 10，SO 2 R 10，卤素，OCH 2 O，NO 2，NH 2，NHR 10或NR 10 R <11>; R 5 ＝苯基（被R 6和/或R 7任选取代（os））; Q'＝直接键或1-6C亚烷基; R 6，R 7 ＝ NH 2，NR 8 R 9，NHR 10，NR 10 R 11，NO 2，卤素，OA，COOH或COOA; R 8，R 9 ＝ H，1-8C酰基（通过1-5 F和/或Cl的os），COOA，SOA，SO2A，CONH2，CONHA，CONA2，COCOOH，COCOOA，COCONH2，COCONHA或COCONA2 ; A = 1-6C烷基（os 1-5 F和/或Cl R 10，R 11 ＝ A，3-7C环烷基，4-8C亚甲基环烷基或2-8C烯基; （ii）X = CH2，S或O; Q = -Q'-C6H4-NHCOB; Q'＝直接键或1-6C亚烷基; B =具有1-4个N，O和/或S杂原子的芳族杂环，通过N或C，os与卤素，A和/或OA的1-3个键合，并且任选地与苯或吡啶环稠合; R 1，R 2 ＝ H或A; R 3，R 4 ＝ OH，OR 5，SR 5，SOR 5，SO 2 R 5，卤素，OCH 2 O，NO 2，NH 2，NHR 5或NR 5 R <6>，R <3>在3位，R <4>在4位; R 5，R 6 ＝ A，3-7C环烷基，4-8C亚甲基环烷基或2-8C烯基; A = 1-10C烷基（os 1-5 F和/或Cl）; （iii）X = S; Q = H; R 1，R 2 ＝ H或A; R 3 ＝ H，OA或OA'; R 4 ＝ OA'; A = 1-6C烷基; A'＝ 1-6C烷基，被1-13F或Cl取代; （iv）X = S; Q = -Q'-R <5>; Q'＝ 1-6C亚烷基; R 5 ＝ NR 6 R 7;或三，四，五或六亚甲基亚氨基（可选地，一个CH2被O取代）; R 1，R 2，R 6，R 7 ＝ H或A; R 3，R 4 ＝ OH，OA，SA，SOA，SO 2 A，卤素，OCH 2 O，3-7C环烷氧基或OA'; A = 1-6C烷基; A'＝ 1-6C烷基，被1-13F取代;或（v）X = CH2或S; Q = -Q'-C6H4-NHCOB; Q'＝直接键或1-4C亚烷基; B ＝ -YR <5>或-O-YR <5>; Y ＝直接键或1-10C亚烷基; R 3，R 4 ＝ OH，OA，SA，SOA，SO 2 A，卤素，OCH 2 O，NO 2，NH 2，NHA或NAA'，R 3在3位，R 4在3位。 4位; A，A′＝ 1-10C烷基（由1-5 F和/或C 1表示的Os），3-7C环烷基或4-8C亚甲基环烷基; R 5 ＝ NH 2。 NHA，NA2或3-8元饱和杂环（通过A或OH包含至少一个N，os，并可选地用NA，S或O取代其他CH2基团）。
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