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    • 2. 发明授权
    • Aromatic thioethers
    • 芳香硫醚
    • US4785004A
    • 1988-11-15
    • US941676
    • 1986-12-15
    • Andreas Von SprecherWerner BreitensteinAndreas BeckRobert W. LangKonrad Oertle
    • Andreas Von SprecherWerner BreitensteinAndreas BeckRobert W. LangKonrad Oertle
    • C07D215/54C07D311/24C07C149/40A61K31/235
    • C07D311/24C07D215/54
    • Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: R.sup.0 represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted by one or more halogen atoms having an atomic number of at most 17,R.sup.2 represents an aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene, a single bond or vinylene,B.sup.1 represents C.sub.1-7 -alkylene or phenylene,B.sup.2 represents a single bond, ethylene or phenylene, andM represents an aromatic radical of the partial formula ##STR2## in which the symbols have the following meanings: R.sup.3 represents hydrogen or C.sub.1-4 -alkyl,X represents NH, O, S or if R.sup.4 represents hydrogen, a single bond,one of the symbols R.sup.4 and R.sup.5 represents hydrogen and the other represents the group --CO--R.sup.6, orR.sup.4 and R.sup.5 together represent the radical --CO--C(R.sup.6).dbd.C(R.sup.7)--or--CO--C(R.sup.7).dbd.C(R.sup.6)--orR.sup.4 R.sup.5, together with X, represent the radical --N.dbd.C(R.sup.8)--C(R.sup.6).dbd.CH--,in whichR.sup.6 represents --(CH.sub.2).sub.b --COOR.sup.3 (in which b=0 to 2)R.sup.7 represents hydrogen or C.sub.1-4 -alkyl andR.sup.8 represents hydrogen, methyl, mythoxy or halogen,and their salts are active as leucotriene antagonists since they eliminate the contractions of smooth muscles brought about by leucotrienes, and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.
    • 式(I)的新颖的不对称硫醚,其中通式符号具有以下含义:R 0表示氢或C 1-7 - 烷酰基,R 1表示可以被一个或多个具有 原子数最多为17,R 2表示具有5至15个碳原子的脂族基团,A表示乙烯,单键或亚乙烯基,B1表示C1-7 - 亚烷基或亚苯基,B2表示单键,乙烯或亚苯基 ,M表示部分结构式(M)的芳族基团,其中符号具有以下含义:R 3表示氢或C 1-4 - 烷基,X表示NH,O,S或如果R 4表示氢,则 单键,R4和R5之一表示氢,另一个表示-CO-R6基团,或R4和R5一起代表基团-CO-C(R6)= C(R7)-OR-CO-C( R7)= C(R6) - 或R4R5与X一起代表基团-N = C(R8)-C(R6)= CH-,其中R6表示 - (CH2)b-COOR3(其中b = 0至2)R7表示氢或C1-4烷基,R8表示氢,甲基,乙氧基或卤素,并且它们的盐作为白三烯拮抗剂是有活性的,因为它们消除了由白三烯引起的平滑肌的收缩,因此适用于 治疗过敏,特别是哮喘,病情。
    • 6. 发明授权
    • Phosphorous-containing phenylsulfonamides
    • 含磷苯基磺酰胺
    • US4677217A
    • 1987-06-30
    • US784274
    • 1985-10-04
    • Ludwig MaierWilly MeyerKonrad OertleAchim RoloffWerner Topfl
    • Ludwig MaierWilly MeyerKonrad OertleAchim RoloffWerner Topfl
    • A01N57/16A01N57/08A01N57/24C07D521/00C07F9/30C07F9/32C07F9/38C07F9/40C07F9/53C07F9/6512C07F9/6521
    • C07D521/00A01N57/08C07F9/304C07F9/3229C07F9/3808C07F9/3834C07F9/4006C07F9/4015C07F9/4021C07F9/4056C07F9/5325C07F9/65127C07F9/65217
    • Phenylsulfonamides of the formula ##STR1## in which X is a group ##STR2## Y is hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, trifluoromethyl, C.sub.2 -C.sub.5 -alkenyl, C.sub.2 -C.sub.5 -alkynyl, nitro, --COOR.sup.6 or --Q--R.sup.6, A is oxygen, sulfur, a direct bond, C.sub.1 -C.sub.5 -alkylene, C.sub.2 -C.sub.5 -alkenylene, C.sub.1 -C.sub.5 -halogenoalkylene or --NR.sup.7 --(CH.sub.2).sub.m --; --CH.sub.2 --NH--(CH.sub.2).sub.m ; --(CH.sub.2).sub.m --NR.sup.7 -- or --O--(CH.sub.2).sub.p --, --S--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --O-- or --(CH.sub.2).sub.p --S--, n is zero or one, G is oxygen or sulfur, R.sup.4 is C.sub.1 -C.sub.5 -alkoxy, C.sub.1 -C.sub.5 -halogenoalkoxy, C.sub.1 -C.sub.5 -alkylthio, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -halogenoalkyl, phenyl or hydroxyl, R.sup.5 is hydrogen, C.sub.1 -C.sub.5 -alkoxy, C.sub.1 -C.sub.5 -halogenoalkoxy, C.sub.1 -C.sub.5 -alkylthio, C.sub.1 -C.sub. 5 -alkyl or hydroxyl, R.sup.6 is hydrogen, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -halogenoalkyl or C.sub.2 -C.sub.6 -alkoxyalkyl, Q is oxygen, sulfur, --SO-- or --SO.sub.2 --, R.sup.7 is hydrogen, C.sub.1 -C.sub.5 -alkyl, phenyl, benzyl or phenyl which is substituted by C.sub.1 -C.sub.5 -alkyl, halogen, or nitro, m is a number from zero to three, p is a number from zero to two and r is one or two are useful as intermediates for phosphorous-containing N-phenylsulfonyl-N'-pyrimdinylurea and N-phenylsulfonyl-N'-triazinylurea herbicides.
    • 其中X是基团Y的式“IMAGE”的苯磺酰胺是氢,卤素,C 1 -C 5 - 烷基,三氟甲基,C 2 -C 5 - 烯基,C 2 -C 5炔基,硝基,-COOR 6或-Q- R6,A是氧,硫,直接键,C1-C5-亚烷基,C2-C5-亚烯基,C1-C5-卤代亚烷基或-NR7-(CH2)m-; -CH 2 -NH-(CH 2)m; - (CH 2)m -NR 7 - 或-O-(CH 2)p - , - S-(CH 2)p - , - (CH 2)p O-或 - (CH 2)p -S-,n为0或1,G为氧 或硫,R4是C1-C5-烷氧基,C1-C5-卤代烷氧基,C1-C5-烷硫基,C1-C5-烷基,C1-C5-卤代烷基,苯基或羟基,R5是氢,C1-C5-烷氧基,C1 -C5-卤代烷氧基,C1-C5-烷硫基,C1-C5-烷基或羟基,R6是氢,C1-C5-烷基,C1-C5-卤代烷基或C2-C6-烷氧基烷基,Q是氧,硫,-SO - 或-SO 2 - ,R 7是氢,C 1 -C 5 - 烷基,苯基,苄基或被C 1 -C 5 - 烷基,卤素或硝基取代的苯基,m是0至3的数,p是 0至2,r是1或2个可用作含磷的N-苯基磺酰基-N'-嘧啶基脲和N-苯基磺酰基-N'-三嗪基脲除草剂的中间体。
    • 7. 发明授权
    • Phenylsulfonyl isocyanates and thioisocyanates
    • 苯磺酰基异氰酸酯和硫代异氰酸酯
    • US4952726A
    • 1990-08-28
    • US440004
    • 1989-11-21
    • Willy MeyerKonrad Oertle
    • Willy MeyerKonrad Oertle
    • C07D249/16A01N43/70A01N47/36C07C20060101C07C67/00C07C301/00C07C309/86C07C311/15C07C311/16C07C311/17C07C311/29C07C311/39C07C311/53C07C311/65C07C325/00C07C331/16C07C331/32C07D239/42C07D239/46C07D239/47C07D239/48C07D239/52C07D239/56C07D239/69C07D251/16C07D251/18C07D251/22C07D251/46C07D251/52C07D521/00
    • C07C309/86A01N47/36C07C311/65C07D521/00
    • N-Phenylsulfonyl-N'-pyrimidinyl- and -triazinylureas of the formula I ##STR1## wherein A is 3,3,3-trifluoropropyl or 3,3-difluorobutyl,R.sup.1 is hydrogen, halogen, nitro, cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -alkylsulfonyl, C.sub.1 -C.sub.4 -alkylsulfonyl, --CO--R.sup.6, --NR.sup.7 R.sup.8, --CO--NR.sup.9 R.sup.10 or --SO.sub.2 --NR.sup.11 R.sup.12,R.sup.2 is hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -alkysulfonyl or C.sub.1 -C.sub.4 -alkylsulfonyl,R.sup.3 and R.sup.4 independently of one another are each hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.2 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkylthio, C.sub.2 -C.sub.4 -alkoxyalkyl, C.sub.1 -C.sub.4 -alkoxy or --NR.sup.13 R.sup.13,R.sup.5 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy,R.sup.6 is C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.2 -C.sub.6 -alkoxyalkoxy, hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -haloalkyl,R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12 and R.sup.13 independently of one another are each hydrogen or C.sub.1 -C.sub.4 -alkyl,E is nitrogen or the methine bridge, andZ is oxygen or sulfur;and also the salts of these compounds.
    • 式I的N-苯基磺酰基-N'-嘧啶基 - 和 - 三嗪基脲其中A是3,3,3-三氟丙基或3,3-二氟丁基,R 1是氢,卤素,硝基,氰基,C 1 C 1-4烷基,C 1 -C 4 - 卤代烷基,C 1 -C 4 - 烷氧基,C 1 -C 4 - 烷硫基,C 1 -C 4 - 烷基亚磺酰基,C 1 -C 4烷基磺酰基,-CO-R 6,-NR 7 R 8,-CO-NR 9 R 10或-SO 2 -NR 11 R 12,R 2是氢,卤素,C 1 -C 4 - 烷基,C 1 -C 4 - 烷氧基,C 1 -C 4 - 烷硫基,C 1 -C 4烷基亚磺酰基或C 1 -C 4烷基磺酰基,R 3和R 4彼此独立地各自为氢, 卤素,C 1 -C 4烷基,C 1 -C 4卤代烷基,C 2 -C 4卤代烷氧基,C 1 -C 4烷硫基,C 1 -C 4卤代烷硫基,C 2 -C 4烷氧基烷基,C 1 -C 4烷氧基或-NR 12 R 13, ,C 1 -C 4烷基或C 1 -C 4 - 烷氧基,R 6是C 1 -C 4 - 烷氧基,C 1 -C 4卤代烷氧基,C 1 -C 4烷硫基,C 2 -C 6烷氧基烷氧基,氢,C 1 -C 4烷基或C 1 -C 4 卤代烷基,R 7,R 8,R 9,R 10,R 11,R 12和R 13各自独立地为氢或C 1 -C 4烷基,E为氮或次甲基桥,Z为氧或硫; 以及这些化合物的盐。
    • 8. 发明授权
    • Certain fluoroalkylphenylsulfonamides
    • 某些氟代烷基苯基磺酰胺
    • US4908467A
    • 1990-03-13
    • US179339
    • 1988-04-08
    • Willy MeyerKonrad Oertle
    • Willy MeyerKonrad Oertle
    • C07D249/16A01N43/70A01N47/36C07C20060101C07C67/00C07C301/00C07C309/86C07C311/15C07C311/16C07C311/17C07C311/29C07C311/39C07C311/53C07C311/65C07C325/00C07C331/16C07C331/32C07D239/42C07D239/46C07D239/47C07D239/48C07D239/52C07D239/56C07D239/69C07D251/16C07D251/18C07D251/22C07D251/46C07D251/52C07D521/00
    • C07C309/86A01N47/36C07C311/65C07D521/00
    • N-Phenylsulfonyl-B'-pyrimidinyl- and -triazinylureas of the formula I ##STR1## wherein A is 3,3,3-trifluoropropyl or 3,3-difluorobutyl,R.sup.1 is hydrogen, halogen, nitro, cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -alkylsulfinyl, C.sub.1 -C.sub.4 -alkylsulfonyl, --CO--R.sup.6, --NR.sup.7 R.sup.8, --CO--NR.sup.9 R.sup.10 or --SO.sub.2 --NR.sup.11 R.sup.12,R.sup.2 is hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -alkylsulfinyl or C.sub.1 -C.sub.4 -alkylsulfonyl,R.sup.3 and R.sup.4 independently of one another are each hydrogen, halogen C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.2 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkylthio, C.sub.2 -C.sub.4 -alkoxyalkyl, C.sub.1 -C.sub.4 -alkoxy or --NR.sup.12 R.sup.13,R.sup.5 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy,R.sup.6 is C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.2 -C.sub.6 -alkoxyalkoxy, hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -haloalkyl,R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12 and R.sup.13 independently of one another are each hydrogen or C.sub.1 -C.sub.4 -alkyl,E is nitrogen or the methine bridge, andZ is oxygen or sulfur;and also the salts of these compounds.
    • 式I的N-苯基磺酰基-N'-嘧啶基 - 和 - 三嗪基脲其中A是3,3,3-三氟丙基或3,3-二氟丁基,R 1是氢,卤素,硝基,氰基,C 1 C 1-4烷基,C 1 -C 4 - 卤代烷基,C 1 -C 4 - 烷氧基,C 1 -C 4 - 烷硫基,C 1 -C 4 - 烷基亚磺酰基,C 1 -C 4烷基磺酰基,-CO-R 6,-NR 7 R 8,-CO-NR 9 R 10或-SO 2 -NR 11 R 12,R 2是氢,卤素,C 1 -C 4 - 烷基,C 1 -C 4 - 烷氧基,C 1 -C 4 - 烷硫基,C 1 -C 4烷基亚磺酰基或C 1 -C 4烷基磺酰基,R 3和R 4彼此独立地各自为氢, 卤素,C 1 -C 4烷基,C 1 -C 4卤代烷基,C 2 -C 4卤代烷氧基,C 1 -C 4烷硫基,C 1 -C 4卤代烷硫基,C 2 -C 4烷氧基烷基,C 1 -C 4烷氧基或-NR 12 R 13, ,C 1 -C 4烷基或C 1 -C 4 - 烷氧基,R 6是C 1 -C 4 - 烷氧基,C 1 -C 4卤代烷氧基,C 1 -C 4 - 烷硫基,C 2 -C 6 - 烷氧基烷氧基,氢,C 1 -C 4烷基或C 1 -C 4 卤代烷基,R 7,R 8,R 9,R 10,R 11,R 12和R 13各自独立地为氢或C 1 -C 4烷基,E为氮或次甲基桥,Z为氧或硫; 以及这些化合物的盐。
    • 9. 发明授权
    • N-phenylsulfonyl-N'-triazinylureas
    • N-苯基磺酰基-N'-三嗪基脲
    • US4780125A
    • 1988-10-25
    • US525366
    • 1983-08-22
    • Willy MeyerDieter ReinehrKonrad OertleRolf Schurter
    • Willy MeyerDieter ReinehrKonrad OertleRolf Schurter
    • B01J31/24A01N47/36A01P13/00C07B61/00C07C303/22C07C309/29C07C309/30C07C309/44C07C309/86C07C309/87C07C311/15C07C311/16C07C311/29C07C311/53C07C311/54C07C311/58C07C311/65C07C317/10C07D239/42C07D239/46C07D239/47C07D239/52C07D239/69C07D251/16C07D251/42C07D251/46C07D251/52C07D521/00A01N43/66
    • C07C311/65A01N47/36C07C309/00C07D239/47C07D521/00
    • The invention relates to N-phenylsulfonyl-N'-pyrimidinylureas and N-phenylsulfonyl-N-triazinylureas of the general formula ##STR1## wherein R.sub.1 is hydrogen, halogen, nitro, amino, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.4 haloalkyl or a --Q--R.sub.7, --CO--OR.sub.8 or --(CO).sub.n --NR.sub.9 R.sub.10 radical,R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkoxy, halogen or alkoxyalkyl containing not more than 4 carbon atoms,R.sub.3 is C.sub.2 -C.sub.10 alkenyl which is substituted by one or more fluorine or bromine atoms or by one or more hydroxyl, cyano, nitro, --(Y).sub.m --CO--(Z).sub.n --R.sub.8, --SO.sub.2 --NR.sub.11 R.sub.12, --S(O).sub.p --C.sub.1 --C.sub.3 haloalkyl or --S(O).sub.n --C.sub.1 -C.sub.3 alkyl groups and which may additionally be substituted by one or more chlorine atoms,R.sub.4 is C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 haloalkoxy, R.sub.5 is hydrogen, halogen, --NR.sub.13 R.sub.14, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.2 haloalkoxy,R.sub.6 is hydrogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy,X is oxygen or sulfur, andE is nitrogen or the methine group, andR.sub.7 is C.sub.1 -C.sub.4 alkyl which is substituted by halogen or C.sub.1 -C.sub.3 alkoxy or is C.sub.3 -C.sub.5 alkenyl,R.sub.8 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl or C.sub.2 -C.sub.6 alkoxyalkyl,R.sub.9, R.sub.10, R.sub.11, R.sub.12, R.sub.13 and R.sub.14, each independently of the other, are hydrogen or C.sub.1 -C.sub.3 alkyl,Q is oxygen, sulfur, the sulfinyl or sulfonyl bridge,Y is oxygen, sulfur or --NR.sub.16 --, wherein R.sub.16 is hydrogen or C.sub.1 -C.sub.3 alkyl,Z is oxygen, sulfur or --NR.sub.17 --, wherein R.sub.17 is hydrogen or C.sub.1 -C.sub.3 alkyl,m and n are each 0 to 1, andp is 0, 1 or 2, and to the salts of these compounds with amines, alkali metal bases or alkaline earth metal bases.These compounds have good pre- and postemergence selective herbicidal and growth regulating properties.
    • 本发明涉及通式为(I)的N-苯基磺酰基-N'-嘧啶基脲和N-苯基磺酰基-N-三嗪基脲,其中R 1是氢,卤素,硝基,氨基,C 1 -C 5烷基,C 1 -C 4卤代烷基或 -Q-R7,-CO-OR8或 - (CO)n-NR9R10基,R2是氢,C1-C4烷基,C1-C4烷氧基,C1-C4烷硫基,C1-C4卤代烷基,C1-C4卤代烷氧基,卤素或不大于 4个碳原子,R 3是被一个或多个氟或溴原子或一个或多个羟基,氰基,硝基, - (Y)m -CO-(Z)n -R 8,-SO 2 -NR 11 R 12取代的C 2 -C 10链烯基 ,-S(O)p-C 1 -C 3卤代烷基或-S(O)n -C 1 -C 3烷基,并且其可以另外被一个或多个氯原子取代,R 4是C 1 -C 3烷基,C 1 -C 3卤代烷基,C 1 -C 3烷氧基或 C1-C3卤代烷氧基,R5是氢,卤素,-NR13R14,C1-C3烷基,C1-C3卤代烷基,C1-C3烷氧基或C1-C2卤代烷氧基,R6是氢,C1-C3烷基或C1-C3烷氧基,X是氧或硫,E是 氮或次甲基,并且R 7为被所取代的C 1 -C 4烷基 卤素或C 1 -C 3烷氧基或C 3 -C 5链烯基,R 8为C 1 -C 4烷基,C 1 -C 4卤代烷基或C 2 -C 6烷氧基烷基,R 9,R 10,R 11,R 12,R 13和R 14各自独立地为氢或C 1 -C 3烷基, Q是氧,硫,亚磺酰基或磺酰基桥,Y是氧,硫或-NR 16 - ,其中R 16是氢或C 1 -C 3烷基,Z是氧,硫或-NR 17 - ,其中R 17是氢或C 1 -C 3烷基, m和n各自为0至1,p为0,1或2,以及这些化合物与胺,碱金属碱或碱土金属碱的盐。 这些化合物具有良好的芽前和芽后选择性除草和生长调节性质。