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1.发明授权
公开(公告)号：US5225406A
公开(公告)日：1993-07-06
申请号：US753943
申请日：1991-09-03
申请人： Susumu Nakagawa , Ryuji Mitomo , Koji Yamada , Norikazu Otake , Fumio Nakano , Akira Asai , Satoru Kuroyanagi , Yoshiharu Tanaka , Moriaki Ishikawa , Ryosuke Ushijima
发明人： Susumu Nakagawa , Ryuji Mitomo , Koji Yamada , Norikazu Otake , Fumio Nakano , Akira Asai , Satoru Kuroyanagi , Yoshiharu Tanaka , Moriaki Ishikawa , Ryosuke Ushijima
IPC分类号： C07D235/28 , C07D263/46 , C07D263/58 , C07D271/10 , C07D271/113 , C07D277/20 , C07D277/36 , C07D277/56 , C07D285/12 , C07D285/125 , C07D501/20 , C07D501/36 , C07D501/46 , C07D501/59
CPC分类号： C07D263/58 , C07D235/28 , C07D263/46 , C07D271/113 , C07D277/36 , C07D277/56 , C07D277/587 , C07D285/125 , Y02P20/55
摘要： The present invention relates to a compound having the formula: ##STR1## wherein R is a hydrogen atom, a carboxyl-protecting group or a negative charge and Q is a hydrogen atom, a halogen atom, a hydroxyl group, an acetoxy group, a carbamoyloxy group, an azide group, a substituted or unsubstituted quarternary ammonio group or a substituted or unsubstituted heterocyclic thio group having at least one hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom, and a sulfur atom, or a non-toxic salt or physiologically hydrolyzable non-toxic ester thereof; a process for producing it; and an antibacterial agent comprising it as an active ingredient.Further, the present invention also relates to a compound having the formula: ##STR2## wherein R.sup.3 is a hydrogen atom or an amino-protecting group, and each of R.sup.4 and R.sup.5 which may be the same or different is a hydrogen atom or a carboxyl-protecting group, or a salt thereof; and a process for producing it.
摘要翻译： 本发明涉及具有下式的化合物：其中R是氢原子，羧基保护基或负电荷，Q是氢原子，卤原子，羟基，乙酰氧基 基团，氨基甲酰氧基，叠氮基，取代或未取代的季铵基或具有至少一个选自氮原子，氧原子和硫原子的杂原子的取代或未取代的杂环硫基， 或其无毒盐或其生理上可水解的无毒酯; 一个生产过程; 和含有它作为活性成分的抗菌剂。 此外，本发明还涉及具有下式的化合物：其中R 3是氢原子或氨基保护基，并且R 4和R 5可以相同或不同的是氢原子 或羧基保护基，或其盐; 及其生产工艺。
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公开(公告)号：US5061794A
公开(公告)日：1991-10-29
申请号：US377086
申请日：1989-07-10
申请人： Susumu Nakagawa , Koji Yamada , Fumio Nakano , Norikazu Otake , Akira Asai , Satoru Kuroyanagi , Yoshiharu Tanaka , Moriaki Ishikawa , Ryosuke Ushijima , Ryuji Mitomo
发明人： Susumu Nakagawa , Koji Yamada , Fumio Nakano , Norikazu Otake , Akira Asai , Satoru Kuroyanagi , Yoshiharu Tanaka , Moriaki Ishikawa , Ryosuke Ushijima , Ryuji Mitomo
IPC分类号： C07D235/28 , C07D263/46 , C07D263/58 , C07D271/10 , C07D271/113 , C07D277/20 , C07D277/36 , C07D277/56 , C07D285/12 , C07D285/125 , C07D501/36
CPC分类号： C07D263/58 , C07D235/28 , C07D263/46 , C07D271/113 , C07D277/36 , C07D277/56 , C07D277/587 , C07D285/125
摘要： A compound having the formula: ##STR1## wherein R is a straight chain or branched chain lower alkyl, cyclic lower alkyl, lower alkenyl (except for 1-carboxy-1-vinyl), lower alkynyl, aralkyl, phenyl or 2-pyrrolidon-3-yl group which may be substituted, and Q is ##STR2## (wherein R.sup.1 is a hydrogen atom or an acetyl group, R.sup.2 is a hydrogen atom, a carboxyl group or a carboxymethyl group, Y is a sulfur atom or an oxygen atom, Z is a sulfur atom, an oxygen atom or an imino group which may be substituted by a lower alkyl group); or a pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.
摘要翻译： 具有下式的化合物：其中R是直链或支链的低级烷基，环状低级烷基，低级烯基（1-羧基-1-乙烯基），低级炔基，芳烷基，苯基或2 可以被取代的吡咯烷酮-3-基，Q是氢原子或乙酰基，R2是氢原子，羧基或羧甲基， Y是硫原子或氧原子，Z是硫原子，氧原子或可被低级烷基取代的亚氨基）; 或其药学上可接受的盐，生理上可水解的酯或其溶剂合物。
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公开(公告)号：US5407930A
公开(公告)日：1995-04-18
申请号：US217023
申请日：1994-03-24
IPC分类号： C07D501/00 , C07D501/36 , C07D501/46 , A61K31/545
CPC分类号： C07D501/00
摘要： The present invention relates to a compound represented by the structural formula I: ##STR1## its pharmaceutically acceptable salt or ester, or its crystalline, which is a novel optically active compound useful as a curing agent for bacterial infections, a process for production thereof and a use thereof.
摘要翻译： 本发明涉及由结构式I表示的化合物：其药学上可接受的盐或酯或其结晶，其是可用作细菌感染的固化剂的新型光学活性化合物， 其制备方法及其用途。
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公开(公告)号：US5403835A
公开(公告)日：1995-04-04
申请号：US476439
申请日：1990-06-07
IPC分类号： C07D501/00 , C07D501/36 , A61K31/545
CPC分类号： C07D501/00
摘要： The present invention relates to a compound represented by the structural formula: ##STR1## or its pharmaceutically acceptable salt or ester, which is a novel optically active compound useful as a curing agent for bacterial infections, a process for production thereof and a use thereof.
摘要翻译： PCT No.PCT / JP89 / 01155 Sec。 371日期1990年6月7日 102（e）日期1990年6月7日PCT提交1989年11月13日PCT公布。 出版物WO91 / 07410 1991年5月30日的日期。本发明涉及由结构式表示的化合物或其药学上可接受的盐或酯，其是可用作细菌固化剂的新型光学活性化合物 感染，其生产方法及其用途。
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5.发明授权
公开(公告)号：US5084453A
公开(公告)日：1992-01-28
申请号：US265458
申请日：1988-10-13
申请人： Susumu Nakagawa , Ryuji Mitomo , Koji Yamada , Norikazu Otake , Fumio Nakano , Akira Asai , Satoru Kuroyanagi , Yoshiharu Tanaka , Moriaki Ishikawa , Ryosuke Ushijima
发明人： Susumu Nakagawa , Ryuji Mitomo , Koji Yamada , Norikazu Otake , Fumio Nakano , Akira Asai , Satoru Kuroyanagi , Yoshiharu Tanaka , Moriaki Ishikawa , Ryosuke Ushijima
IPC分类号： A61K31/545 , C07D235/28 , C07D263/46 , C07D263/58 , C07D271/10 , C07D271/113 , C07D277/20 , C07D277/36 , C07D277/40 , C07D277/56 , C07D285/12 , C07D285/125 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/46
CPC分类号： C07D263/58 , C07D235/28 , C07D263/46 , C07D271/113 , C07D277/36 , C07D277/56 , C07D277/587 , C07D285/125 , Y02P20/55
摘要： The present invention relates to a compound having the formula: ##STR1## wherein R is a hydrogen atom, a carboxyl-protecting group or a negative charge and Q is a hydrogen atom, a halogen atom, a hydroxyl group, an acetoxy group, a carbamoyl group, an azide group, a substituted or unsubstituted quarternary ammonio group or a substituted or unsubstituted heterocyclic thio group having at least one hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, or a non-toxic salt or physiologically hydrolyzable non-toxic ester thereof; a process for producing it; and an antibacterial agent comprising it as an active ingredient.Further, the present invention also relates to a compound having the formula: ##STR2## wherein R.sup.3 is a hydrogen atom or an amino-protecting group, and each of R.sup.4 and R.sup.5 which may be the same or different is a hydrogen atom or a carboxyl-protecting group, or a salt thereof; and a process for producing it.
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公开(公告)号：US5436354A
公开(公告)日：1995-07-25
申请号：US357257
申请日：1994-12-13
IPC分类号： C07D333/16 , B01J31/24 , C07B37/04 , C07B61/00 , C07C209/08 , C07C209/16 , C07C209/22 , C07C209/68 , C07C211/23 , C07C211/24 , C07C211/27 , C07C211/29 , C07C211/30 , C07C211/35 , C07C213/08 , C07C215/24 , C07C215/42 , C07C215/48 , C07C215/50 , C07C217/46 , C07C217/52 , C07C217/56 , C07C217/58 , C07D333/04 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58 , C07D333/62
CPC分类号： C07D333/62 , C07C209/08 , C07C209/68 , C07C211/24 , C07C211/29 , C07C211/30 , C07C213/08 , C07C215/50 , C07D333/16 , C07D333/20 , Y02P20/55
摘要： (E)-N-(3-Chloro-2-propenyl)-N-methyl-1naphthylenemethanamine and (E)-3-chloro-N-(3-chloro-2-propenyl)-N-methylbenzo[b]thiophene-7-methanamine which are useful as intermediates in the production of enyne compounds which exhibit squalene epoxidase inhibiting activity and anti-Eumycetes activity.
摘要翻译： （E）-N-（3-氯-2-丙烯基）-N-甲基-1-萘基甲胺和（E）-3-氯-N-（3-氯-2-丙烯基）-N-甲基苯并[b]噻吩 - 可用作生产具有角鲨烯环氧酶抑制活性和抗真菌活性的烯炔化合物的中间体的7-甲胺。
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公开(公告)号：US5296612A
公开(公告)日：1994-03-22
申请号：US974488
申请日：1992-11-12
IPC分类号： C07D333/16 , B01J31/24 , C07B37/04 , C07B61/00 , C07C209/08 , C07C209/16 , C07C209/22 , C07C209/68 , C07C211/23 , C07C211/24 , C07C211/27 , C07C211/29 , C07C211/30 , C07C211/35 , C07C213/08 , C07C215/24 , C07C215/42 , C07C215/48 , C07C215/50 , C07C217/46 , C07C217/52 , C07C217/56 , C07C217/58 , C07D333/04 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58 , C07D333/62 , C07C211/02
CPC分类号： C07D333/62 , C07C209/08 , C07C209/68 , C07C211/24 , C07C211/29 , C07C211/30 , C07C213/08 , C07C215/50 , C07D333/16 , C07D333/20 , Y02P20/55
摘要： A process for producing an enyne derivative, and intermediate, which is useful for preparing compounds showing strong inhibiting activities against squalane epoxidase of Eumycetes and strong anti-cholesterol activities. The process comprises reacting a compound of the formula: ##STR1## wherein W is a halogen atom, with an acetylene derivative, in the presence of a palladium catalyst, to obtain a compound of the formula: ##STR2## and, if necessary, N-alkylating this compound.
摘要翻译： 一种生产烯炔衍生物和中间体的方法，其可用于制备显示对Eumycetes的角鲨烷环氧酶的强抑制活性的化合物和强的抗胆固醇活性。 该方法包括在钯催化剂存在下使下式的化合物（*化学结构*）（Ⅳ）（其中W是卤素原子）与乙炔衍生物反应，得到下式化合物：（* CHEMICAL 结构*）（VII），如果需要，N-烷基化该化合物。
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公开(公告)号：US5359091A
公开(公告)日：1994-10-25
申请号：US153956
申请日：1993-11-18
IPC分类号： C07D333/16 , B01J31/24 , C07B37/04 , C07B61/00 , C07C209/08 , C07C209/16 , C07C209/22 , C07C209/68 , C07C211/23 , C07C211/24 , C07C211/27 , C07C211/29 , C07C211/30 , C07C211/35 , C07C213/08 , C07C215/24 , C07C215/42 , C07C215/48 , C07C215/50 , C07C217/46 , C07C217/52 , C07C217/56 , C07C217/58 , C07D333/04 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58 , C07D333/62 , C07D211/02
CPC分类号： C07D333/62 , C07C209/08 , C07C209/68 , C07C211/24 , C07C211/29 , C07C211/30 , C07C213/08 , C07C215/50 , C07D333/16 , C07D333/20 , Y02P20/55
摘要： A compound of the formula: ##STR1## wherein R.sup.11 is hydrogen, lower alkyl, haloloweralkyl, lower alkenyl, lower alkynyl or cycloalkyl; R.sup.21 is a group of the formula: ##STR2## wherein each of R.sup.3, R.sup.31, and R.sup.32 which may be the same or different, is hydrogen or lower alkyl, each of R.sup.4, R.sup.5, R.sup.41 and R.sup.51, which may be the same or different, is hydrogen, halogen, hydroxyl, lower alkyl or lower alkoxy, R.sup.42 is hydroxyl, halogen, R.sup.8 --O--, or R.sup.6 --X--Y-- wherein R.sup.6 is phenyl or thienyl which may have one or two substituents each of X and Y, which may be the same or different, is oxygen, sulfur, carbonyl, --CHR.sup.8 -- or --NR.sup.b, or X and Y together form a vinylene group or an ethynylene group, provided that when either one of X and Y is oxygen, sulfur or --NR.sup.b, the other is carbonyl or --CHR.sup.a, and R.sup.7 is lower alkyl or cycloalkyl which may be substituted by hydroxy or lower alkoxy, phenyl or tri-lower alkylsilyl; and W is chlorine or bromine.
摘要翻译： 下式的化合物：其中R11是氢，低级烷基，卤代低级烷基，低级烯基，低级炔基或环烷基; R21是下式的基团：其中可以相同或不同的R 3，R 31和R 32各自为氢或低级烷基，各自为R 4，R 5，R 41和R 51， 氢，卤素，羟基，低级烷基或低级烷氧基，R42是羟基，卤素，R8-O-或R6-XY-，其中R6是可以具有一个或两个取代基的苯基或噻吩基，其可以相同或不同 X和Y各自可以相同或不同，是氧，硫，羰基，-CHR8-或-NRb，或X和Y一起形成亚乙烯基或亚乙炔基，条件是当X和 Y是氧，硫或-NRb，另一个是羰基或-CHRa，并且R 7是可被羟基或低级烷氧基取代的低级烷基或环烷基，苯基或三低级烷基甲硅烷基; W是氯或溴。
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公开(公告)号：US5440049A
公开(公告)日：1995-08-08
申请号：US258772
申请日：1994-06-13
IPC分类号： C07D333/16 , B01J31/24 , C07B37/04 , C07B61/00 , C07C209/08 , C07C209/16 , C07C209/22 , C07C209/68 , C07C211/23 , C07C211/24 , C07C211/27 , C07C211/29 , C07C211/30 , C07C211/35 , C07C213/08 , C07C215/24 , C07C215/42 , C07C215/48 , C07C215/50 , C07C217/46 , C07C217/52 , C07C217/56 , C07C217/58 , C07D333/04 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58 , C07D333/62
CPC分类号： C07D333/62 , C07C209/08 , C07C209/68 , C07C211/24 , C07C211/29 , C07C211/30 , C07C213/08 , C07C215/50 , C07D333/16 , C07D333/20 , Y02P20/55
摘要： A compound of the formula: ##STR1## wherein R.sup.11 is hydrogen, lower alkyl, haloloweralkyl, lower alkenyl, lower alkynyl or cycloalkyl and R.sup.21 is a group selected from the group consisting of: ##STR2## wherein R.sup.3 -R.sup.5, R.sup.31, R.sup.32, R.sup.41, R.sup.42 and R.sup.51 are as defined herein, and W is chlorine or bromine, is prepared by reacting a compound of the formula:Z--CH.sub.2 --CH.dbd.CH--W (I)wherein W is as defined above and Z is a leaving group, with an amine of the formula: ##STR3## wherein R.sup.11 and R.sup.21 are as defined above.
摘要翻译： 下式的化合物：其中R 11是氢，低级烷基，卤代低级烷基，低级烯基，低级炔基或环烷基，R 21是选自以下的基团：其中R 11是氢，低级烷基，卤代低级烷基，低级烯基，低级炔基或环烷基， [IIIb]或其中R3-R5，R31，R32，R41，R42和R51如本文所定义，W为氯或溴的化合物通过使下式化合物：Z-CH 2 - CH = CH-W（I）其中W如上所定义，Z是离去基团，与下式的胺反应：其中R 11和R 21如上所定义。
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公开(公告)号：US5231183A
公开(公告)日：1993-07-27
申请号：US861160
申请日：1992-03-27
IPC分类号： C07D333/16 , B01J31/24 , C07B37/04 , C07B61/00 , C07C209/08 , C07C209/16 , C07C209/22 , C07C209/68 , C07C211/23 , C07C211/24 , C07C211/27 , C07C211/29 , C07C211/30 , C07C211/35 , C07C213/08 , C07C215/24 , C07C215/42 , C07C215/48 , C07C215/50 , C07C217/46 , C07C217/52 , C07C217/56 , C07C217/58 , C07D333/04 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58 , C07D333/62
CPC分类号： C07D333/62 , C07C209/08 , C07C209/68 , C07C211/24 , C07C211/29 , C07C211/30 , C07C213/08 , C07C215/50 , C07D333/16 , C07D333/20 , Y02P20/55
摘要： A process for producing an enyne derivative, and intermediate, which is useful for preparing compounds showing strong inhibiting activities against squalane.epoxidase of Eumycetes and strong anti-cholesterol activities. The process comprises reacting a compound of the formula:Z--CH.sub.2 --CH.dbd.CH--W [I]wherein W is a halogen atom, and Z is a leaving group, with an amine in the presence of a base, if necessary, to obtain a compound of the formula: ##STR1## then reacting an acetylene derivative to this compound in the presence of a palladium catalyst, to obtain a compound of the formula: ##STR2## and, if necessary, N-alkylating this compound.
摘要翻译： 一种制备烯炔衍生物和中间体的方法，其可用于制备显示出对Eumycetes的角鲨烷环氧酶和强抗胆固醇活性的强抑制活性的化合物。 该方法包括在碱存在的情况下使下式化合物：其中W是卤素原子的Z-CH 2 -CH = CH-W [I]和Z是离去基团与胺反应，如果需要， 得到下式的化合物：[IV]然后在钯催化剂存在下使乙炔衍生物与该化合物反应，得到下式化合物：必要时，N- 烷基化该化合物。
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