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1.发明授权[(Benzodioxan, benzofuran or benzopyran) alkylamino] alkyl substituted guanidines 失效[（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
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。
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2.发明授权[(Benzodioxan, benzofuran or benzopyran) alkylamino] alkyl substituted guanidines 失效[（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
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。
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3.发明授权[(benzodioxan, benzofuran or benzopyran) alkylamino] alkyl substituted guanidines 失效[（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
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。
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