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    • 3. 发明授权
    • Heteroarylethylamine as production promoters in livestock
    • 杂环三乙胺作为家畜生产促进剂
    • US4863939A
    • 1989-09-05
    • US80284
    • 1987-07-30
    • Hans LindelWerner HallenbachFriedrich BerschauerAnno de JongMartin Scheer
    • Hans LindelWerner HallenbachFriedrich BerschauerAnno de JongMartin Scheer
    • C07D213/84A23K20/132A61K31/44A61K31/4402A61K31/4412A61K31/4418A61P15/00C07D213/36C07D213/38C07D213/61C07D213/70C07D213/72C07D213/73C07D213/74C07D213/75C07D213/79C07D213/81
    • C07D213/73A23K20/132C07D213/38C07D213/61
    • The growth of livestock is promoted by the new compounds of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl, halogen, halogenoalkyl, hydroxyl, cyano, alkoxycarbonyl, aminocarbonyl, mono- and dialkylaminocarbonyl, alkoxy, halogenoalkoxy, halogenoalkylthio or NHSO.sub.2 -alkyl,R.sup.2 represents hydrogen, hydroxyl, alkoxy or the --NR.sup.11 R.sup.12 radical,R.sup.3 represents the radicals mentioned in the case of R.sup.1R.sup.4 represents hydroxyl, acyloxy or alkoxy,R.sup.5 represents hydrogen or alkyl,R.sup.6 represents hydrogen or alkyl,R.sup.7 represents hydrogen or alkyl,R.sup.8 represents hydrogen or alkyl,X represents C.sub.1 -C.sub.10 -alkylene or a direct bond,Y represents oxygen or a direct bond,R.sup.9 represents hydrogen, C.sub.1 -C.sub.10 -alkyl which is optionally substituted by hydroxyl, alkoxy, acyloxy or the --NR.sup.13 R.sup.14 radical, or represents the COR.sup.15 radical or the O--Z--R.sup.16 radical,Z represents C.sub.1 -C.sub.10 -alkylene, C.sub.1 -C.sub.10 -alkenylene or C.sub.1 -C.sub.10 -alkinylene,R.sup.10 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl or the COR.sup.15 radical,R.sup.11 represents hydrogen or alkyl,R.sup.12 represents hydrogen, alkyl, halogenoalkyl or acyl,R.sup.13 represents hydrogen, optionally substituted alkyl or optionally substituted aryl,R.sup.14 represents the radicals mentioned in the case of R.sup.13,R.sup.15 represents hydroxyl, alkoxy or the NR.sup.13 R.sup.14 radical, andR.sup.16 represents hydroxyl, alkoxy, acyloxy, the NR.sup.13 R.sup.14 radical or the COR.sup.15 radical,and the physiologically acceptable salts and N-oxides thereof. Several new intermediates are also disclosed.
    • 新型化合物“IMAGE”促进了家畜的生长,其中R1代表氢,烷基,卤素,卤代烷基,羟基,氰基,烷氧基羰基,氨基羰基,一烷基氨基羰基和二烷基氨基羰基,烷氧基,卤代烷氧基,卤代烷硫基或NHSO2-烷基 ,R 2表示氢,羟基,烷氧基或-NR 11 R 12基团,R 3表示在R 4表示羟基,酰氧基或烷氧基的情况下提及的基团,R 5表示氢或烷基,R 6表示氢或烷基,R 7表示氢或烷基, R8表示氢或烷基,X表示C1-C10-亚烷基或直接键,Y表示氧或直接键,R9表示氢,任选被羟基,烷氧基,酰氧基或-NR13R14基团取代的C1-C10-烷基 ,或表示COR15基团或OZ-R16基团,Z表示C1-C10-亚烷基,C1-C10亚烯基或C1-C10亚烯基,R10表示氢,卤素,烷基,烷氧基,羟基或COR15基,R11 代理人 R12表示氢,烷基,卤代烷基或酰基,R13表示氢,任选取代的烷基或任选取代的芳基,R 14表示在R 13的情况下提及的基团,R 15表示羟基,烷氧基或NR 13 R 14基,R 16 表示羟基,烷氧基,酰氧基,NR 13 R 14基或COR 15基,及其生理上可接受的盐和N-氧化物。 还披露了几个新的中间体。
    • 5. 发明授权
    • Heteroarylethanol-pyridylalkylamines for controlling animal growth
    • 用于控制动物生长的杂芳基乙醇 - 吡啶基烷基胺
    • US5028617A
    • 1991-07-02
    • US467593
    • 1990-01-19
    • Hans LindelWerner HallenbachFriedrich BerschauerHeinrich A. GreifeGernot Klotz
    • Hans LindelWerner HallenbachFriedrich BerschauerHeinrich A. GreifeGernot Klotz
    • A23K1/16A61K31/44A61K31/4402A61K31/4406A61K31/4409A61K31/4418A61P3/04C07D213/38C07D213/61C07D213/64C07D213/65C07D213/73C07D213/80
    • C07D213/64C07D213/38C07D213/61C07D213/65C07D213/73C07D213/80
    • A compound for promoting livestock production and for controlling obesity in humans and animals, of the formula ##STR1## in which A represents .dbd.CH-- or .dbd.N--,R.sup.0 represents hydrogen or methyl,R.sup.1 and R.sup.3 each independently represents hydrogen, hydroxyl, halogen, cyano, alkyl, halogenoalkyl, hydroxyalkyl, alkoxycarbonyl, aminocarbonyl, mono- and dialkylaminocarbonyl, alkoxy, halogenoalkoxy, halogenoalkylthio, NHSO.sub.2 -alkyl,R.sup.2 represents hydrogen, hydroxyl, alkoxy or the radical --NR.sup.5 R.sup.6,R.sup.4 represents hydrogen, C.sub.1 -C.sub.10 -alkyl which is optionally substituted by hydroxyl, halogen, alkoxy, acyloxy or the radical --NH.sup.7 R.sup.8, or represents the radical COR.sup.9 or the radical --O--Z--R.sup.10,Z represents C.sub.1 -C.sub.10 -alkylene, -alkenylene or alkynylene,R.sup.5 represents hydrogen or alkyl,R.sup.6 represents hydrogen, alkyl, halogenoalkyl or acyl, or R.sup.5 and R.sup.6 together with the adjoining N atom form a saturated or unsaturated heterocyclic 4-, 5- or 6-membered ring,R.sup.7 and R.sup.8 each independently represents hydrogen, optionally substituted alkyl, optionally substituted aryl,R.sup.9 represents hydroxyl, alkoxy or the radical --NR.sup.7 R.sup.8,R.sup.10 represents hydroxyl, alkoxy, acyloxy, optionally substituted aryloxy or aralkyloxy,with the substituent R.sup.4 and the alkylamino group in the pyridyl ring of the formula I being in the p position with respect to one another, or a physiologically tolerated salt thereof, or, if A represents nitrogen, optionally the N-oxide thereof.
    • 一种用于促进家畜生产和控制人和动物肥胖的化合物,其中A表示= CH-或= N-,R0表示氢或甲基,R1和R3各自独立地表示氢, 羟基,卤素,氰基,烷基,卤代烷基,羟基烷基,烷氧基羰基,氨基羰基,一烷基氨基羰基和二烷基氨基羰基,烷氧基,卤代烷氧基,卤代烷硫基,NHSO2-烷基,R2代表氢,羟基,烷氧基或基-NR5R6,R4代表氢,C1- 任选被羟基,卤素,烷氧基,酰氧基或基团-NH 7 R 8取代的C 10 - 烷基,或表示基团COR 9或基团-OZ-R 10,Z表示C 1 -C 10 - 亚烷基, - 亚烯基或亚炔基,R 5表示氢 或烷基,R 6表示氢,烷基,卤代烷基或酰基,或R 5和R 6与相邻的N原子一起形成饱和或不饱和的4-,5-或6-元环,R 7和R 8各自独立地表示氢, 取代的烷基,任选取代的芳基,R 9表示羟基,烷氧基或基团-NR 7 R 8,R 10表示羟基,烷氧基,酰氧基,任选取代的芳氧基或芳烷氧基,式I的吡啶环中的取代基R4和烷基氨基在 相对于彼此的p位置或其生理上耐受的盐,或者如果A表示氮,则任选地其N-氧化物。
    • 6. 发明授权
    • (2-aminopropyl) pyridines useful as intermediates
    • (2-氨基丙基)吡啶可用作中间体
    • US5216170A
    • 1993-06-01
    • US677020
    • 1991-03-28
    • Hans LindelWerner HallenbachFriedrich BerschauerHeinrich A. GreifeGernot Klotz
    • Hans LindelWerner HallenbachFriedrich BerschauerHeinrich A. GreifeGernot Klotz
    • C07D213/38C07D213/61C07D213/64C07D213/65C07D213/73C07D213/80
    • C07D213/64C07D213/38C07D213/61C07D213/65C07D213/73C07D213/80
    • A compound for promoting livestock production and for controlling obesity in humans and animals, of the formula ##STR1## in which A represents .dbd.CH-- or .dbd.N--,R.sup.0 represents hydrogen or methyl,R.sup.1 and R.sup.3 each independently represents hydrogen, hydroxyl, halogen, cyano, alkyl, halogenoalkyl, hydroxyalkyl, alkoxycarbonyl, aminocarbonyl, mono- and dialkylaminocarbonyl, alkoxy, halogenoalkoxy, halogenoalkylthio, NHSO.sub.2 -alkyl,R.sup.2 represents hydrogen, hydroxyl, alkoxy or the radical --NR.sup.5 R.sup.6,R.sup.4 represents hydrogen, C.sub.1 -C.sub.10 -alkyl which is optionally substituted by hydroxyl, halogen, alkoxy, acyloxy or the radical --NR.sup.7 R.sup.8, or represents the radical COR.sup.9 or the radical --O--Z--R.sup.10,Z represents C.sub.1 -C.sub.10 -alkylene, -alkenylene or alkynylene,R.sup.5 represents hydrogen or alkyl,R.sup.6 represents hydrogen, alkyl, halogenoalkyl or acyl, or R.sup.5 and R.sup.6 together with the adjoining N atom form a saturated or unsaturated heterocyclic 4-, 5- or 6-membered ring,R.sup.7 and R.sup.8 each independently represents hydrogen, optionally substituted alkyl, optionally substituted aryl,R.sup.9 represents hydroxyl, alkoxy or the radical --NR.sup.7 R.sup.8,R.sup.10 represents hydroxyl, alkoxy, acyloxy, optionally substituted aryloxy or aralkyloxy,with the substituent R.sup.4 and the alkylamino group in the pyridyl ring of the formula I being in the p position with respect to one another,or a physiologically tolerated salt thereof, or, if A represents nitrogen, optionally the N-oxide thereof.
    • 一种用于促进家畜生产和控制人和动物肥胖的化合物,其中A表示= CH-或= N-,R0表示氢或甲基,R1和R3各自独立地表示氢, 羟基,卤素,氰基,烷基,卤代烷基,羟基烷基,烷氧基羰基,氨基羰基,一烷基氨基羰基和二烷基氨基羰基,烷氧基,卤代烷氧基,卤代烷硫基,NHSO2-烷基,R2代表氢,羟基,烷氧基或基-NR5R6,R4代表氢,C1- 任选被羟基,卤素,烷氧基,酰氧基或基团-NR 7 R 8取代的C 10 - 烷基,或表示基团COR 9或基团-OZ-R 10,Z表示C 1 -C 10亚烷基, - 亚烯基或亚炔基,R 5表示氢 或烷基,R 6表示氢,烷基,卤代烷基或酰基,或R 5和R 6与相邻的N原子一起形成饱和或不饱和的4-,5-或6-元环,R 7和R 8各自独立地表示氢, 取代的烷基,任选取代的芳基,R 9表示羟基,烷氧基或基团-NR 7 R 8,R 10表示羟基,烷氧基,酰氧基,任选取代的芳氧基或芳烷氧基,式I的吡啶环中的取代基R4和烷基氨基在 相对于彼此的p位置或其生理上耐受的盐,或者如果A表示氮,则任选地其N-氧化物。
    • 8. 发明授权
    • Use of benzimidazole derivatives as yield promoters
    • 苯并咪唑衍生物作为产率促进剂的应用
    • US4960783A
    • 1990-10-02
    • US292581
    • 1988-12-30
    • Gerhard BonseWerner HallenbachHans LindelFriedrich Berschauer
    • Gerhard BonseWerner HallenbachHans LindelFriedrich Berschauer
    • A23K1/16C07D235/06C07D235/08C07D235/10C07D235/26
    • C07D235/06C07D235/08C07D235/10C07D235/26
    • Method of promoting the yield and growth of animals which comprises administering to such animals a yield and growth promoting effective amount of a benzimidazole derivative of the formula ##STR1## in which R.sup.1 stands for hydrogen, hydroxyl, alkyl or halogenoalkyl,R.sup.2 stands for hydrogen, alkyl, halogen, CN or halogenalkyl,R.sup.3 stands for hydrogen, alkyl or acyl,R.sup.4 stands for hydrogen, alkyl or halogenoalkyl,R.sup.5 stands for alkyl or halogenoalkyl,R.sup.6 stands for alkyl or cycloalkyl, which is optionally substituted by halogen, cycloalkyl, OH, alkoxy, halogenoalkoxy or aryl, which can in turn be substituted by alkyl, halogen, CN or the radicals --COR.sup.7, --O--alkylene--COR.sup.7, --alkylene--R.sup.8 or --O-- alkylene--R.sup.8,R.sup.7 stands for hydroxyl, alkoxy or --NR.sup.9 R.sup.10,R.sup.8 stands for hydroxyl, alkoxy or --NR.sup.9 R.sup.10,R.sup.9 stands for hydrogen or alkyl andR.sup.10 stands for hydrogen or alkyl,or physiologically tolerated salts thereof. The active materials are new except for those in whichR.sup.1 stands for hydrogen,R.sup.4 stands for hydrogen,R.sup.5 stands for methyl andR.sup.6 stands for methyl.
    • 促进动物产量和生长的方法,其包括向所述动物施用产量和生长促进有效量的式(I)的苯并咪唑衍生物,其中R1代表氢,羟基,烷基或卤代烷基,R2代表 对于氢,烷基,卤素,CN或卤代烷基,R3代表氢,烷基或酰基,R4代表氢,烷基或卤代烷基,R5代表烷基或卤代烷基,R6代表烷基或环烷基, 环烷基,OH,烷氧基,卤代烷氧基或芳基,其又可以被烷基,卤素,CN或基团-COR7,-O-亚烷基-COR7, - 亚烷基-R8或-O-亚烷基-R8取代,R7代表 羟基,烷氧基或-NR9R10,R8代表羟基,烷氧基或-NR9R10,R9代表氢或烷基,R10代表氢或烷基或其生理上耐受的盐。 活性物质是新的,除了其中R1代表氢,R4代表氢,R5代表甲基,R6代表甲基的那些。
    • 10. 发明授权
    • Substituted pyridylethanolamine livestock production promoters
    • 取代的吡啶乙醇胺家畜生产促进剂
    • US4920136A
    • 1990-04-24
    • US218740
    • 1988-07-13
    • Hans LindelWerner HallenbachFriedrich Berschauer
    • Hans LindelWerner HallenbachFriedrich Berschauer
    • C07D213/79A61K31/44A61K31/4418A61P15/00C07D213/80C07D213/81C07D213/84C07D213/85
    • C07D213/80C07D213/85
    • For promoting livestock production, the novel substituted pyridylethanolamines of the formula ##STR1## in which R.sup.1 represents CN, --COOR.sup.8 or --CONR.sup.9 R.sup.10,R.sup.2 represents optionally substituted alkyl,R.sup.3 represents hydrogen, alkyl or alkenyl,R.sup.4 represents hydrogen or optionally substituted alkyl or alkenyl, orR.sup.3 and R.sup.4 represent, together with the nitrogen atom to which they are bonded, an optionally substituted heterocyclic radical,R.sup.5 represents OH, acyloxy or alkoxy,R.sup.6 represents hydrogen or alkyl,R.sup.7 represents hydrogen, alkyl, cycloalkyl, substituted alkyl, optionally substituted aralkyl, aryl or heterocyclyl,R.sup.6 and R.sup.7 can, together with the nitrogen atom to which they are bonded, represent an optionally substituted heterocyclic radical,R.sup.8 represents alkyl, andR.sup.9 and R.sup.10, independently of one another, represent hydrogen, alkyl or alkenyl or, together with the nitrogen atom to which they are bonded, represent an optionally substituted heterocyclic radical,or a physiologically tolerated salt or N-oxide thereof. Some intermediates are also new.
    • 为了促进家畜生产,式(Ⅰ)所示的新型取代的吡啶基乙醇胺,其中R 1表示CN,-COOR 8或-CONR 9 R 10,R 2表示任意取代的烷基,R 3表示氢,烷基或烯基,R 4表示氢或任意取代的烷基或 烯基或R3和R4与它们所键合的氮原子一起表示任选取代的杂环基,R 5表示OH,酰氧基或烷氧基,R 6表示氢或烷基,R 7表示氢,烷基,环烷基,取代的烷基, 任选取代的芳烷基,芳基或杂环基,R6和R7可以与它们所键合的氮原子一起表示任选取代的杂环基,R 8表示烷基,R 9和R 10彼此独立地表示氢,烷基或 或者与它们所键合的氮原子一起代表任选取代的杂环基或生理层 其盐或N-氧化物。 一些中间体也是新的。