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    • 5. 发明公开
    • 제초제로서 1,3-옥사진-4-온 유도체, 그 제조 방법및 중간물
    • 作为除草剂的1,3-氧化物-4-酮衍生物,其制备方法和中间体
    • KR1020000010565A
    • 2000-02-15
    • KR1019980708421
    • 1997-04-08
    • 롱-쁠랑 아그리컬쳐 리미티드
    • 하야시자끼게이찌우스이요시히로화이트까뜨린쟈끌린
    • C07D413/04A01N43/86
    • C07D413/04A01N43/86C07D265/06
    • PURPOSE: 1,3-oxazin-4-one derivatives, processes and intermediates are provided for their preparation, compositions containing them, and their use as herbicides is provided. CONSTITUTION: 1,3-oxazin-4-ones is formula (I) wherein: W represents -NR6; R1 represents thiophene optionally substituted by one to three groups which is the same or different selected from halogen, hydroxy, lower alkyl, lower haloalkyl, lower alkoxy, lower haloalkoxy, -S(O)nR7, -CO2R7, -COR7, cyano, nitro and phenoxy; R¬2 represents hydrogen, lower alkyl, lower haloalkyl, alkoxyalkyl, lower alkenyl, lower haloalkenyl, alkoxyalkenyl, -CHO, -COR7, -CO2R7, -CH2NO2, and lower alkyl which is substituted by a group selected from -S(O)mR7 and -OCOR7; R3 represents phenyl optionally substituted by one to five groups which is the same or different selected from halogen, lower alkyl, lower haloalkyl, lower alkoxy, lower haloalkoxy, -S(O)nR7, -CO2R7, -COR7, cyano, nitro, -OH, phenoxy, -NR8R9 and -SF5; or a cycloalkyl group containing from three to six carbon atoms, optionally substituted by lower alkyl, lower haloalkyl or one or more halogen atoms which is the same or different; R4 and R5 independently represent lower alkyl.
    • 目的:提供1,3-恶嗪-4-酮衍生物,制备方法和中间体,含有它们的组合物及其作为除草剂的用途。 构成:1,3-恶嗪-4-酮是式(I),其中:W表示-NR 6; R 1表示任选被一至三个选自卤素,羟基,低级烷基,低级卤代烷基,低级烷氧基,低级卤代烷氧基,-S(O)n R 7,-CO 2 R 7,-COR 7,氰基,硝基的相同或不同的基团取代的噻吩。 和苯氧基; R 2表示氢,低级烷基,低级卤代烷基,烷氧基烷基,低级烯基,低级卤代烯基,烷氧基烯基,-CHO,-COR 7,-CO 2 R 7,-CH 2 NO 2,和被选自-S(O) mR7和-OCOR7; R 3表示任选被一至五个选自卤素,低级烷基,低级卤代烷基,低级烷氧基,低级卤代烷氧基,-S(O)n R 7,-CO 2 R 7,-COR 7,氰基,硝基, OH,苯氧基,-NR8R9和-SF5; 或含有3至6个碳原子的环烷基,任选被相同或不同的低级烷基,低级卤代烷基或一个或多个卤素原子取代; R4和R5独立地表示低级烷基。
    • 9. 发明公开
    • 1,3-디헤테로시클릭 메탈로프로테아제 저해제
    • 1,3-二氢化物金属蛋白酶抑制剂
    • KR1020000035918A
    • 2000-06-26
    • KR1019997001654
    • 1997-08-22
    • 더 프록터 앤드 갬블 캄파니
    • 피쿨스태니슬로맥도우-던햄켈리린암스테드네일그레고리드비즈워나쓰네이쳐스마이클죠지타이워예툰데올라비지
    • C07D239/04
    • C07D239/10C07D233/02C07D233/38C07D239/04C07D243/04C07D265/06C07D265/14C07D277/06C07D279/06C07D409/14C07D413/14C07D487/04C07D495/10
    • PURPOSE: Compounds useful for the treatment of conditions and diseases which are characterized by unwanted MP activity, potent inhibitors of metalloproteases, pharmaceutical compositions comprising such inhibitors and a method of treatment for metalloprotease related maladies are provided. CONSTITUTION: The compounds are useful as inhibitors of metalloproteases and effective in treating conditions characterized by excess activity of these enzymes. In particular, the invention relates to a compound having a structure according to Formula (I) wherein R1 is H; R2 is hydrogen, alkyl, or acyl; Ar is COR3 or SO2R4; and R3 is alkoxy, aryloxy, heteroaryloxy, alkyl, aryl, heteroaryl, heteroalkyl, amino, alkylamino, dialkylamino, arylamino and alkylarylamino; R4 is alkyl, heteroalkyl, aryl, or heteroaryl, substituted or unsubstituted; X is O, S, SO, SO2, or NRg, wherein R5 is independently chosen from hydrogen, alkyl, heteroalkyl, heteroaryl, aryl, SO2R6, COR7, CSRg, PO(Rg)2 or may optionally form a ring with Y or W; and R6 is alkyl, aryl, heteroaryl, diarylamino and alkylarylamino; R7 is hydrogen, alkoxy, aryloxy, heteroaryloxy, alkyl, aryl,, dialkylamino, arylamino and alkylarylamino; R8 is alkyl, aryl, heteroaryl, arylamino, diarylamino and alkylarylamino; R9 is alkyl, aryl, heteroaryl, heteroalkyl.
    • 目的:提供可用于治疗以不需要的MP活性为特征的病症和疾病的化合物,金属蛋白酶的有效抑制剂,包含这些抑制剂的药物组合物和金属蛋白酶相关疾病的治疗方法。 构成:这些化合物可用作金属蛋白酶抑制剂,并有效治疗以这些酶的过度活性为特征的病症。 特别地,本发明涉及具有式(I)结构的化合物,其中R 1是H; R2是氢,烷基或酰基; Ar为COR3或SO2R4; 芳基,芳基,杂芳基,杂烷基,氨基,烷基氨基,二烷基氨基,芳基氨基和烷芳基氨基; R 4是烷基,杂烷基,芳基或杂芳基,取代或未取代的; X是O,S,SO,SO 2或NR g,其中R5独立地选自氢,烷基,杂烷基,杂芳基,芳基,SO2R6,COR7,CSRg,PO(Rg)2,或者可以任选地形成具有Y或W ; 并且R 6是烷基,芳基,杂芳基,二芳基氨基和烷基芳基氨基; R 7是氢,烷​​氧基,芳氧基,杂芳氧基,烷基,芳基,二烷基氨基,芳基氨基和烷芳基氨基; R8是烷基,芳基,杂芳基,芳基氨基,二芳基氨基和烷基芳基氨基; R9是烷基,芳基,杂芳基,杂烷基。