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1. 发明授权

US5607949A [(Benzodioxan, benzofuran or benzopyran) alkylamino] alkyl substituted guanidines 失效
标题翻译： [（苯并二恶烷，苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍
公开(公告)号：US5607949A
公开(公告)日：1997-03-04
申请号：US632227
申请日：1996-04-15
申请人： Guy R. E. Van Lommen , Marcel F. L. De Bruyn , Walter J. J. Janssens
发明人： Guy R. E. Van Lommen , Marcel F. L. De Bruyn , Walter J. J. Janssens
IPC分类号： C07C279/00 , C07D307/78 , A61K31/34 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/415 , A61K31/443 , A61K31/445 , A61K31/505 , A61K31/53 , A61P9/00 , A61P9/02 , A61P25/04 , C07C277/00 , C07D307/81 , C07D311/58 , C07D319/08 , C07D319/20 , C07D405/06 , C07D405/12 , C07D405/14
CPC分类号： C07D405/12 , C07D307/81 , C07D311/58 , C07D319/20 , C07D405/14
摘要： The present invention is concerned with vasoconstricive [(benzodioxan, benzofuran or benzopyran)alkylamino]alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.1-3 alkanediyl radical; A is a bivalent radical of formula: ##STR2## wherein each R.sup.5 is hydrogen or C.sub.1-4 alkyl; wherein each R.sup.6 is hydrogen or C.sub.1-4 alkyl; Alk.sup.2 is C.sub.2-15 alkanediyl or C.sub.5-7 cycloalkanediyl; and each p is 0, 1 or 2; provided that [2-[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amino]ethyl guanidine is excluded. Pharmaceuticals which are useful as vasoconstrictors. Compositions comprising said guanidine derivatives as active ingredients, processes for preparing said guanidine derivatives and novel N-cyano guanidine, intermediates; and a use as a medicine are described.
摘要翻译：本发明涉及具有下式的[（苯并二恶烷，苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍，（I）其药学上可接受的酸加成盐及其立体化学异构形式，其中X是O，CH 2 或直接债券; R1是氢或C1-6烷基; R2是氢，C1-6烷基，C3-6烯基或C3-6炔基; R3是氢或C1-6烷基; 或者R 2和R 3可以一起形成式 - （CH 2）m - 的二价基团，其中m为4或5; 或R 1和R 2一起形成式-CH = CH-或式 - （CH 2）n - 的二价基团，其中n为2,3或4; 或者当R 1和R 2一起形成式-CH = CH-CH =，-CH = CH-N =或-CH = N-CH =的二价基团时，R 3可以表示键。 R4是氢或C1-6烷基; Alk1是二价C 1-3烷二基; （a）其中每个R 5为氢或C 1-4烷基;（e）其中每个R 5为氢或C 1-4烷基;（c）其中每个R 6是氢或C 1-4烷基; Alk2是C2-15烷二基或C5-7环烷二基; 每个p为0,1或2; 条件是排除[2 - [（2,3-二氢-1,4-苯并二恶英-2-基）甲基]氨基]乙基胍。可用作血管收缩药物的药物。包含所述胍衍生物作为活性成分的组合物，制备所述胍衍生物的方法和新的N-氰基胍，中间体; 并描述了作为药物的用途。

2. 发明授权

US5624952A [(Benzodioxan, benzofuran or benzopyran) alkylamino] alkyl substituted guanidines 失效
标题翻译： [（苯并二恶烷，苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍
公开(公告)号：US5624952A
公开(公告)日：1997-04-29
申请号：US632226
申请日：1996-04-15
申请人： Guy R. E. Van Lommen , Marcel F. L. De Bruyn , Walter J. J. Janssens
发明人： Guy R. E. Van Lommen , Marcel F. L. De Bruyn , Walter J. J. Janssens
IPC分类号： C07C279/00 , C07D307/78 , A61K31/34 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/415 , A61K31/443 , A61K31/445 , A61K31/505 , A61K31/53 , A61P9/00 , A61P9/02 , A61P25/04 , C07C277/00 , C07D307/81 , C07D311/58 , C07D319/08 , C07D319/20 , C07D405/06 , C07D405/12 , C07D405/14 , A61K31/40
CPC分类号： C07D405/12 , C07D307/81 , C07D311/58 , C07D319/20 , C07D405/14
摘要： The present invention is concerned with vasoconstricive [(benzodioxan, benzofuran or benzopyran)alkylamino]alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sub.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.1-3 alkanediyl radical; A is a bivalent radical of formula: ##STR2## wherein each R.sup.5 is hydrogen or C.sub.1-4 alkyl; wherein each R.sup.6 is hydrogen or C.sub.1-4 alkyl; Alk.sup.2 is C.sub.2-15 alkanediyl or C.sub.5-7 cycloalkanediyl; and each p is 0, 1 or 2; provided that [2-[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amino]ethyl guanidine is excluded. Pharmaceuticals which are useful as vaseconstrictors. Compositions comprising said guanidine derivatives as active ingredients, processes for preparing said guanidine derivatives and novel N-cyano guanidine, intermediates; and a use as a medicine are described.
摘要翻译：本发明涉及具有下式的[（苯并二恶烷，苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍，（I）其药学上可接受的酸加成盐及其立体化学异构形式，其中X是O，CH 2 或直接债券; R1是氢或C1-6烷基; R2是氢，C1-6烷基，C3-6烯基或C3-6炔基; R3是氢或C1-6烷基; 或者R 2和R 3可以一起形成式 - （CH 2）m - 的二价基团，其中m为4或5; 或R 1和R 2一起形成式-CH = CH-或式 - （CH 2）n - 的二价基团，其中n为2,3或4; 或者当R 1和R 2一起形成式-CH = CH-CH =，-CH = CH-N =或-CH = N-CH =的二价基团时，R 3可以表示键。 R4是氢或C1-6烷基; Alk1是二价C 1-3烷二基; （a）其中每个R 5为氢或C 1-4烷基;（e）其中每个R 5为氢或C 1-4烷基;（c）其中每个R 6是氢或C 1-4烷基; Alk2是C2-15烷二基或C5-7环烷二基; 每个p为0,1或2; 条件是排除[2 - [（2,3-二氢-1,4-苯并二恶英-2-基）甲基]氨基]乙基胍。用作血管收缩药物的药物。包含所述胍衍生物作为活性成分的组合物，制备所述胍衍生物的方法和新的N-氰基胍，中间体; 并描述了作为药物的用途。

3. 发明授权

US5541180A [(benzodioxan, benzofuran or benzopyran) alkylamino] alkyl substituted guanidines 失效
标题翻译： [（苯并二恶烷，苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍
公开(公告)号：US5541180A
公开(公告)日：1996-07-30
申请号：US256995
申请日：1994-07-29
申请人： Guy R. E. Van Lommen , Marcel F. L. De Bruyn , Walter J. J. Janssens
发明人： Guy R. E. Van Lommen , Marcel F. L. De Bruyn , Walter J. J. Janssens
IPC分类号： C07C279/00 , C07D307/78 , A61K31/34 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/415 , A61K31/443 , A61K31/445 , A61K31/505 , A61K31/53 , A61P9/00 , A61P9/02 , A61P25/04 , C07C277/00 , C07D307/81 , C07D311/58 , C07D319/08 , C07D319/20 , C07D405/06 , C07D405/12 , C07D405/14 , A61K31/33 , C07D239/42 , C07D243/04
CPC分类号： C07D405/12 , C07D307/81 , C07D311/58 , C07D319/20 , C07D405/14
摘要： The present invention is concerned with vasoconstricive [(benzodioxan, benzofuran or benzopyran)alkylamino]alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl;Alk.sup.1 is a bivalent C.sub.1-3 alkanediyl radical; A is a bivalent radical of formula: ##STR2## wherein each R.sup.5 is hydrogen or C.sub.1-4 alkyl; wherein each R.sup.6 is hydrogen or C.sub.1-4 alkyl; Alk.sup.2 is C.sub.2-15 alkanediyl or C.sub.5-7 cycloalkanediyl; and each p is 0, 1 or 2; provided that [2-[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amino]ethyl guanidine is excluded. Pharmaceuticals which are useful as vasoconstrictors. Compositions comprising said guanidine derivatives as active ingredients, processes for preparing said guanidine derivatives and novel N-cyano guanidine, intermediates; and a use as a medicine are described.
摘要翻译： PCT No.PCT / EP93 / 00435 Sec。 371日期1994年7月29日第 102（e）日期1994年7月29日PCT提交1993年2月19日PCT公布。出版物WO93 / 17017 日本1993年9月2日本发明涉及具有式（I）表示的药物上可接受的酸加成盐的血管收缩素[（苯并二恶烷，苯并呋喃或苯并吡喃）烷基氨基]烷基取代的胍及其立体化学异构形式，其中 X是O，CH 2或直接键; R1是氢或C1-6烷基; R2是氢，C1-6烷基，C3-6烯基或C3-6炔基; R3是氢或C1-6烷基; 或者R 2和R 3可以一起形成式 - （CH 2）m - 的二价基团，其中m为4或5; 或R 1和R 2一起形成式-CH = CH-或式 - （CH 2）n - 的二价基团，其中n为2,3或4; 或者当R 1和R 2一起形成式-CH = CH-CH =，-CH = CH-N =或-CH = N-CH =的二价基团时，R 3可以表示键。 R4是氢或C1-6烷基; Alk1是二价C1-3烷二基; （a）其中每个R 5为氢或C 1-4烷基;（e）其中每个R 5为氢或C 1-4烷基;（c）其中每个R 6是氢或C 1-4烷基; Alk2是C2-15烷二基或C5-7环烷二基; 每个p为0,1或2; 条件是排除[2 - [（2,3-二氢-1,4-苯并二恶英-2-基）甲基]氨基]乙基胍。可用作血管收缩药物的药物。包含所述胍衍生物作为活性成分的组合物，制备所述胍衍生物的方法和新的N-氰基胍，中间体; 并描述了作为药物的用途。

4. 发明授权

US4994103A 1,5-substituted 1H-imidazoles 失效
标题翻译： 1,5-取代的1H-咪唑
公开(公告)号：US4994103A
公开(公告)日：1991-02-19
申请号：US420248
申请日：1989-10-12
申请人： Marcel F. L. De Bruyn , Guy R. E. Van Lommen , William R. Lutz
发明人： Marcel F. L. De Bruyn , Guy R. E. Van Lommen , William R. Lutz
IPC分类号： A01N43/50 , C07D233/54 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D401/04 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04
CPC分类号： C07D233/64 , A01N43/50 , C07D233/84 , C07D401/04 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04
摘要： Novel herbicidal 1,5-substituted 1H-imidazole derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Further the invention also relates to a process for making these novel compounds.

5. 发明授权

US4654362A Derivatives of 2,2'-iminobisethanol 失效
标题翻译： 2,2'-亚氨基双酚的衍生物
公开(公告)号：US4654362A
公开(公告)日：1987-03-31
申请号：US660355
申请日：1984-10-12
申请人： Guy R. E. Van Lommen , Marcel F. L. De Bruyn , Marc F. J. Schroven
发明人： Guy R. E. Van Lommen , Marcel F. L. De Bruyn , Marc F. J. Schroven
IPC分类号： C07D307/81 , C07D311/22 , C07D311/58 , C07D311/66 , C07D311/92 , C07D407/04 , A61K31/35 , A61K31/34 , C07D307/87
CPC分类号： C07D407/04 , C07D307/81 , C07D311/22 , C07D311/58 , C07D311/66 , C07D311/92
摘要： Derivatives of 2,2'-iminobisethanol having useful properties in the treatment and/or the prevention of disorders of the coronary-vascular system.
摘要翻译：具有治疗和/或预防冠状动脉血管系统障碍的有用性质的2,2'-亚氨基双酚的衍生物。

6. 发明授权

US4878940A Herbicidal 1,5-substituted 1H-imidazoles 失效
标题翻译：除草剂1,5-取代的1H-咪唑
公开(公告)号：US4878940A
公开(公告)日：1989-11-07
申请号：US173511
申请日：1988-03-25
申请人： Marcel F. L. De Bruyn , Guy R. E. Van Lommen , William R. Lutz
发明人： Marcel F. L. De Bruyn , Guy R. E. Van Lommen , William R. Lutz
IPC分类号： A01N43/50 , C07D233/54 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D401/04 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04
CPC分类号： C07D233/64 , A01N43/50 , C07D233/84 , C07D401/04 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04
摘要： Novel herbicidal 1,5-substituted 1H-imidazole derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Further the invention also relates to a process for making these novel compounds.

7. 发明授权

US4927449A Tricyclic 1H-imidazole-5-carboxylic acid derivatives as herbicides 失效
标题翻译：三环咪唑-5-羧酸衍生物作为除草剂
公开(公告)号：US4927449A
公开(公告)日：1990-05-22
申请号：US289947
申请日：1988-12-27
申请人： William R. Lutz , Wim G. Verschueren , Hanspeter Fischer , Guy R. E. Van Lommen
发明人： William R. Lutz , Wim G. Verschueren , Hanspeter Fischer , Guy R. E. Van Lommen
IPC分类号： A01N43/50 , A01N43/56 , A01N45/02 , C07D233/90 , C07D401/04 , C07D405/04 , C07D409/04
CPC分类号： C07D405/04 , A01N43/50 , A01N45/02 , C07D233/90 , C07D409/04
摘要： Novel herbicidal tricyclic 1H-imidazole-5-carboxylic acid derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants.

8. 发明授权

US4824472A Herbicidal polycyclyl substituted 1H-imidazole-5-carboxylic acids 失效
标题翻译：除草多环基取代的1 H-咪唑-5-羧酸
公开(公告)号：US4824472A
公开(公告)日：1989-04-25
申请号：US137384
申请日：1987-12-23
申请人： Guy R. E. Van Lommen , Victor Sipido , Wim G. Verschueren , William R. Lutz
发明人： Guy R. E. Van Lommen , Victor Sipido , Wim G. Verschueren , William R. Lutz
IPC分类号： C07D233/54 , A01N43/50 , A01N43/836 , A01N45/02 , C07D233/60 , C07D233/84 , C07D233/90 , C07D401/04 , C07D405/04 , C07D409/04
CPC分类号： C07D401/04 , A01N43/50 , A01N45/02 , C07D233/90 , C07D405/04 , C07D409/04
摘要： Novel herbicidal 1-cyclyl or polycyclyl substituted 1H-imidazole-5-carboxylic acid derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Processes for making these novel compounds.

9. 发明授权

US5369084A Isonicotinic acid derivatives and related spiro compounds with herbicidal action 失效
标题翻译：异烟酸衍生物和具有除草作用的相关螺环化合物
公开(公告)号：US5369084A
公开(公告)日：1994-11-29
申请号：US50269
申请日：1993-05-06
申请人： Hans-Rudolf Waespe , Guy R. E. Van Lommen , Victor K. Sipido
发明人： Hans-Rudolf Waespe , Guy R. E. Van Lommen , Victor K. Sipido
IPC分类号： A01N43/40 , A01N43/42 , A01N43/50 , A01N43/76 , A01N43/78 , A01N43/90 , C07D213/79 , C07D213/81 , C07D213/82 , C07D213/83 , C07D405/04 , C07D409/04 , C07D471/04 , C07D471/10 , C07D491/048 , C07D491/10 , C07D491/107 , C07D491/20 , C07D213/78
CPC分类号： C07D213/79 , A01N43/40 , A01N43/90 , C07D213/81 , C07D213/82 , C07D213/83 , C07D405/04 , C07D409/04 , C07D471/10 , C07D491/10
摘要： Isonicotinic acid derivatives and related furo-, thieno- and pyrrolo[3,4-c]pyridin-1(3H)-one, -thione and -imine compounds having the formula ##STR1## wherein R is ##STR2## Q is O, S or NR.sup.7 ; Y is O, S or NR.sup.8 ; L is COOR.sup.9, CONR.sup.10 R.sup.11, C(.dbd.S)NR.sup.10 R.sup.11, CN, or a radical of formula ##STR3## the acceptable addition salts, the stereochemically isomeric forms and the N-oxides thereof, having herbicidal properties, compositions containing the same and methods for controlling weeds.
摘要翻译：异烟酸衍生物和相关的具有式（I）的呋喃并噻吩并吡咯并[3,4-c]吡啶-1（3H） - 酮 - 硫酮和亚胺化合物，其中R为< 图像> 或 Q是O，S或NR7; Y为O，S或NR8; L是COOR 9，CONR 10 R 11，C（= S）NR 10 R 11，CN或式（VII）的基团，其具有除草性质的可接受的加成盐，立体化学异构形式和N-氧化物，含有它们的组合物和控制杂草。

10. 发明授权

US5246915A Method for controlling weeds 失效
标题翻译：杂草防治方法
公开(公告)号：US5246915A
公开(公告)日：1993-09-21
申请号：US842301
申请日：1992-02-26
申请人： William R. Lutz , Guy R. E. Van Lommen , Jozef F. E. Van Gestel
发明人： William R. Lutz , Guy R. E. Van Lommen , Jozef F. E. Van Gestel
IPC分类号： A01N43/50 , A01N45/02 , C07D233/66 , C07D233/90
CPC分类号： C07D233/90 , A01N43/50 , A01N45/02
摘要： A method for controlling weeds preferably in the crops of useful plants by using a 5-imidazolecarboxylic acid derivative; herbicidal compositions containing the same; novel 5-imidazolecarboxylic acid derivatives.
摘要翻译：一种通过使用5-咪唑羧酸衍生物优选在有用植物作物中控制杂草的方法; 含有它们的除草组合物; 新的5-咪唑羧酸衍生物。

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