公开(公告)号：US4643849A

公开(公告)日：1987-02-17

申请号：US550933

申请日：1983-11-14

申请人： Shiro Hirai ,  Hiroshi Hirano ,  Hirotoshi Arai ,  Yasuo Kiba ,  Hisanari Shibata ,  Yoshikazu Kusayanagi ,  Minako Yotsuji ,  Kazuhiko Hashiba ,  Kikuko Tanada

发明人： Shiro Hirai ,  Hiroshi Hirano ,  Hirotoshi Arai ,  Yasuo Kiba ,  Hisanari Shibata ,  Yoshikazu Kusayanagi ,  Minako Yotsuji ,  Kazuhiko Hashiba ,  Kikuko Tanada

IPC分类号： C07C323/25 ,  C07D209/48 ,  C07D211/42 ,  C07D213/40 ,  C07D233/54 ,  C07D263/10 ,  C07D263/14 ,  C07D263/28 ,  C07D277/28 ,  C07D277/42 ,  C07D277/48 ,  C07D295/096 ,  C07D307/52 ,  C07D317/58 ,  C07D333/20 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07F7/18 ,  C07D203/20

CPC分类号： C07D209/48 ,  C07C323/25 ,  C07D211/42 ,  C07D213/40 ,  C07D233/64 ,  C07D263/10 ,  C07D263/14 ,  C07D263/28 ,  C07D277/28 ,  C07D277/48 ,  C07D295/096 ,  C07D307/52 ,  C07D317/58 ,  C07D333/20 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07F7/1804 ,  C07F7/1852

摘要： This invention relates to amine derivatives and salts thereof. These compounds have an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such compounds, a process for the preparation thereof and an anti-ulcer agent containing the same.

摘要翻译： 本发明涉及胺衍生物及其盐。 这些化合物具有对人类和动物有效的抗溃疡活性。 本公开涉及这些化合物，其制备方法和含有该化合物的抗溃疡剂。

公开(公告)号：US4923882A

公开(公告)日：1990-05-08

申请号：US919716

申请日：1986-10-16

申请人： Shiro Hirai ,  Hiroshi Hirano ,  Hirotoshi Arai ,  Yasuo Kiba ,  Hisanari Shibata ,  Yoshikazu Kusayanag ,  Minako Yotsuji ,  Kazuhiko Hashiba ,  Kikuko Tanada

发明人： Shiro Hirai ,  Hiroshi Hirano ,  Hirotoshi Arai ,  Yasuo Kiba ,  Hisanari Shibata ,  Yoshikazu Kusayanag ,  Minako Yotsuji ,  Kazuhiko Hashiba ,  Kikuko Tanada

IPC分类号： C07D233/64 ,  A61K31/155 ,  A61K31/34 ,  A61K31/341 ,  A61K31/357 ,  A61K31/415 ,  A61K31/425 ,  A61K31/426 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61P1/04 ,  A61P43/00 ,  C07C67/00 ,  C07C275/24 ,  C07C279/04 ,  C07C301/00 ,  C07C307/06 ,  C07C311/64 ,  C07C313/00 ,  C07C323/25 ,  C07C323/44 ,  C07C325/00 ,  C07C335/08 ,  C07D209/48 ,  C07D211/42 ,  C07D213/38 ,  C07D213/40 ,  C07D233/54 ,  C07D263/10 ,  C07D263/14 ,  C07D263/28 ,  C07D277/20 ,  C07D277/28 ,  C07D277/48 ,  C07D295/08 ,  C07D295/096 ,  C07D307/52 ,  C07D317/58 ,  C07D333/20 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12 ,  C07F7/18

CPC分类号： C07D209/48 ,  C07C323/25 ,  C07D211/42 ,  C07D213/40 ,  C07D233/64 ,  C07D263/10 ,  C07D263/14 ,  C07D263/28 ,  C07D277/28 ,  C07D277/48 ,  C07D295/096 ,  C07D307/52 ,  C07D317/58 ,  C07D333/20 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07F7/1852 ,  Y02P20/55

摘要： This invention relates to amine derivatives and salts thereof. These compounds have an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such compound, a process for the preparation thereof and an anti-ulcer agent containing the same.

摘要翻译： 本发明涉及胺衍生物及其盐。 这些化合物具有对人类和动物有效的抗溃疡活性。 本公开涉及这种化合物，其制备方法和含有该化合物的抗溃疡剂。

公开(公告)号：US5120746A

公开(公告)日：1992-06-09

申请号：US490056

申请日：1990-03-30

申请人： Shiro Hirai ,  Hiroshi Hirano ,  Hirotoshi Arai ,  Yasuo Kiba ,  Hisanari Shibata ,  Yoshikazu Kusayanag ,  Minako Yotsuji ,  Kazuhiko Hashiba ,  Kikuko Tanada

发明人： Shiro Hirai ,  Hiroshi Hirano ,  Hirotoshi Arai ,  Yasuo Kiba ,  Hisanari Shibata ,  Yoshikazu Kusayanag ,  Minako Yotsuji ,  Kazuhiko Hashiba ,  Kikuko Tanada

IPC分类号： C07C323/25 ,  C07D209/48 ,  C07D211/42 ,  C07D213/40 ,  C07D233/54 ,  C07D263/10 ,  C07D263/14 ,  C07D263/28 ,  C07D277/28 ,  C07D277/42 ,  C07D277/48 ,  C07D295/096 ,  C07D307/52 ,  C07D317/58 ,  C07D333/20 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07F7/18

CPC分类号： C07D209/48 ,  C07C323/25 ,  C07D211/42 ,  C07D213/40 ,  C07D233/64 ,  C07D263/10 ,  C07D263/14 ,  C07D263/28 ,  C07D277/28 ,  C07D277/48 ,  C07D295/096 ,  C07D307/52 ,  C07D317/58 ,  C07D333/20 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07F7/1804 ,  C07F7/1852

摘要： This invention relates to amine derivatives and salts thereof. These compounds have an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such compound, a process for the preparation thereof and an anti-ulcer agent containing the same.

公开(公告)号：US5605921A

公开(公告)日：1997-02-25

申请号：US261952

申请日：1994-06-17

申请人： Hiroyuki Imaizumi ,  Tetsuya Kajita ,  Kenichi Takashima ,  Minako Yotsuji ,  Keiko Takakura ,  Akira Yotsuji ,  Junichi Mitsuyama ,  Katsumi Shimizu ,  Hiroshi Sakai ,  Hirokazu Narita

发明人： Hiroyuki Imaizumi ,  Tetsuya Kajita ,  Kenichi Takashima ,  Minako Yotsuji ,  Keiko Takakura ,  Akira Yotsuji ,  Junichi Mitsuyama ,  Katsumi Shimizu ,  Hiroshi Sakai ,  Hirokazu Narita

IPC分类号： A61K31/41 ,  A61P31/04 ,  A61P31/10 ,  C07D249/08 ,  C07D401/12 ,  C07D417/06 ,  C07D521/00 ,  A01N43/653

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： The present invention relates to a compound represented by the general formula (1) or its salt, a process for producing the same, and an antifungal agent comprising the same as an effective component: ##STR1## wherein R.sup.1 represents a substituted or unsubstituted aryl group or a substituted or unsubstituted heterocyclic group bonded through a carbon atom in the ring to the main chain; R.sup.2 presents a hydrogen atom, a fluorine atom or a substituted or unsubstituted alkyl group; and R.sup.3 represents a cyano group, a thioamido group or a group represented by the formula ##STR2## in which R.sup.4 is a hydroxyl group or a group of the formula ##STR3## (R.sup.7 and R.sup.8, which may be the same or different, are hydrogen atoms or substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, amino, alkoxy, hydroxyl or heterocyclic groups, and may form a substituted or unsubstituted heterocyclic group together with the nitrogen atom to which R.sup.7 and R.sup.8 attach), R.sup.5 is a substituted or unsubstituted alkoxy group or a group of the formula ##STR4## (R.sup.7 and R.sup.8 are as defined above), and R.sup.6 is a hydrogen atom or a substituted or unsubstituted alkyl group.

摘要翻译： 本发明涉及由通式（1）表示的化合物或其盐，其制备方法和含有该化合物的有效成分的抗真菌剂：有或无取代的芳基或取代或未取代的杂环基 通过环中的碳原子键合到主链上; R2表示氢原子，氟原子或取代或未取代的烷基; 并且R 3表示氰基，硫代酰氨基或由下式表示的基团：其中R 4是羟基或式（R 3和R 8）可以相同或不同， 氢原子或取代或未取代的烷基，烯基，炔基，环烷基，芳基，氨基，烷氧基，羟基或杂环基，并且可以与R7和R8连接的氮原子一起形成取代或未取代的杂环基），R5是 取代或未取代的烷氧基或式的基团（R 7和R 8如上定义），R 6为氢原子或取代或未取代的烷基。

公开(公告)号：US06337399B1

公开(公告)日：2002-01-08

申请号：US09529407

申请日：2000-04-26

申请人： Minoru Yamada ,  Shoichi Hamamoto ,  Kazuya Hayashi ,  Kazuko Takaoka ,  Hiroko Matsukura ,  Minako Yotsuji ,  Kenji Yonezawa ,  Katsuji Ojima ,  Tamotsu Takamatsu ,  Kyoko Taya ,  Hirohiko Yamamoto ,  Taro Kiyoto ,  Hironori Kotsubo

发明人： Minoru Yamada ,  Shoichi Hamamoto ,  Kazuya Hayashi ,  Kazuko Takaoka ,  Hiroko Matsukura ,  Minako Yotsuji ,  Kenji Yonezawa ,  Katsuji Ojima ,  Tamotsu Takamatsu ,  Kyoko Taya ,  Hirohiko Yamamoto ,  Taro Kiyoto ,  Hironori Kotsubo

IPC分类号： C07D21516

CPC分类号： C07D401/04 ,  A61K31/4709 ,  C07C217/48 ,  C07D209/44 ,  C07D215/56 ,  C07F5/025 ,  Y02P20/55

摘要： This invention relates to processes for producing a 7-isoindoline-quinolonecarboxylic acid derivative represented by the general formula [1] which is useful as an antibacterial agent, and an intermediate thereof: wherein R1 represents a hydrogen atom or a carboxyl-protecting group; R2 represents a substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl or heterocyclic group; R3 represents at least one group selected from hydrogen atom, halogen atoms, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, alkoxy or alkylthio groups, nitro group, cyano group, acyl groups, protected or unprotected hydroxyl groups and protected or unprotected or substituted or unsubstituted amino groups; R4 represents at least one group selected from hydrogen atom, halogen atoms, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aralkyl, aryl, alkoxy or alkylthio groups, protected or unprotected hydroxyl or imino groups, protected or unprotected or substituted or unsubstituted amino groups, alkylidene groups, oxo group and groups each forming a cycloalkane group together with the carbon atom to which R4 bonds; R5 represents a hydrogen atom, an amino-protecting group, a substituted or unsubstituted alkyl, cycloalkyl, alkylsulfonyl, arylsulfonyl, acyl or aryl group; R6 represents a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl, alkoxy or alkylthio group, a protected or unprotected hydroxyl or amino group or a nitro group; and A represents CH or C—R7 in which R7 represents a halogen atom, a substituted or unsubstituted alkyl, alkoxy or alkylthio group or a protected or unprotected hydroxyl group, and to a salt of a 7-isoindoline-quinolonecarboxylic acid represented by the general formula [1], a hydrate thereof and a composition comprising them as an active ingredient.

公开(公告)号：US20070225506A1

公开(公告)日：2007-09-27

申请号：US11691740

申请日：2007-03-27

申请人： Minoru Yamada ,  Shoichi Hamamoto ,  Kazuya Hayashi ,  Kazuko Takaoka ,  Hiroko Matsukura ,  Minako Yotsuji ,  Kenji Yonezawa ,  Katsuji Ojima ,  Tamotsu Takamatsu ,  Kyoko Taya ,  Hirohiko Yamamoto ,  Taro Kiyoto ,  Hironori Kotsubo

发明人： Minoru Yamada ,  Shoichi Hamamoto ,  Kazuya Hayashi ,  Kazuko Takaoka ,  Hiroko Matsukura ,  Minako Yotsuji ,  Kenji Yonezawa ,  Katsuji Ojima ,  Tamotsu Takamatsu ,  Kyoko Taya ,  Hirohiko Yamamoto ,  Taro Kiyoto ,  Hironori Kotsubo

IPC分类号： C07D209/04

CPC分类号： C07D401/04 ,  A61K31/4709 ,  C07C217/48 ,  C07D209/44 ,  C07D215/56 ,  C07F5/025 ,  Y02P20/55

摘要： Process for producing a 7-bromoquinolone-carboxylic acid derivative of the following formula or its salt by reacting a 2,4-dibromo-3-hydroxybenzoic acid ester compound of the formula R7a-x to obtain a 3-alkoxy-2,4-dibromobenzoic acid ester, subjecting the 3-alkoxy-2,4-dibromobenzoic acid ester to elimination reaction of the carboxyl-protecting group to obtain a 3-alkoxy-2,4-dibromobenzoic acid, subjecting the 3-alkoxy-2,4-dibromobenzoic acid to ketoesterification reaction to obtain a 3-alkoxy-2,4-dibromobenyolacetic acid ester, reacting the 3-alkoxy-2,4-dibromobenzoylacetic acid ester with an orthoester or an acetal, then reacting the reaction product with a compound of the formula R2— NH or its salt to obtain a 2-(3-alkoxy-2,4-dibromobenzoyl)-3-substituted aminoacrylic acid ester and subjecting the 2-(3-alkoxy-2,4-dibromobenzoyl)-3-substituted aminoacrylic acid ester to ring-closing reaction, and products thereof.

摘要翻译： 制备下式的7-溴喹诺酮 - 羧酸衍生物或其盐的方法，其通过使式<β的在线式描述的2,4-二溴-3-羟基苯甲酸酯化合物=“在线式 “end =”lead“？> R 7a -x <？in-line-formula description =”In-line Formulas“end =”tail“？>以获得3-烷氧基-2， 4-二溴苯甲酸酯，使3-烷氧基-2,4-二溴苯甲酸酯与羧基保护基进行消去反应，得到3-烷氧基-2,4-二溴苯甲酸，将3-烷氧基-2,4-二溴苯甲酸 4-二溴苯甲酸进行酮酯化反应，得到3-烷氧基-2,4-二溴苯乙醇酸乙酯，使3-烷氧基-2,4-二溴苯甲酰基乙酸酯与原酸酯或缩醛反应，然后使反应产物与化合物 的式R 2 -O-NH或其盐，得到2-（3-烷氧基-2,4-二溴苯甲酰基）-3-取代的氨基丙烯酸酯，并使2-（3-烷氧基 - 3,4-二溴苯甲酰基）-3-取代基 叔氨基丙烯酸酯进行闭环反应，及其产物。

公开(公告)号：US06482835B2

公开(公告)日：2002-11-19

申请号：US09961364

申请日：2001-09-25

申请人： Minoru Yamada ,  Shoichi Hamamoto ,  Kazuya Hayashi ,  Kazuko Takaoka ,  Hiroko Matsukura ,  Minako Yotsuji ,  Kenji Yonezawa ,  Katsuji Ojima ,  Tamotsu Takamatsu ,  Kyoko Taya ,  Hirohiko Yamamoto ,  Taro Kiyoto ,  Hironori Kotsubo

发明人： Minoru Yamada ,  Shoichi Hamamoto ,  Kazuya Hayashi ,  Kazuko Takaoka ,  Hiroko Matsukura ,  Minako Yotsuji ,  Kenji Yonezawa ,  Katsuji Ojima ,  Tamotsu Takamatsu ,  Kyoko Taya ,  Hirohiko Yamamoto ,  Taro Kiyoto ,  Hironori Kotsubo

IPC分类号： A61K3147

CPC分类号： C07D401/04 ,  A61K31/4709 ,  C07C217/48 ,  C07D209/44 ,  C07D215/56 ,  C07F5/025 ,  Y02P20/55

摘要： Processes for producing a 7-isoindoline-quinolonecarboxylic acid derivative represented by the general formula [1] which is useful as an antibacterial agent, and an intermediate thereof: comprising reacting, in the presence of metallic palladium, an isoindoline-5-boronic acid, or of a 5-halogenoisoindoline, in the presence of a palladium catalyst, with a dialkoxyborane or an alkoxydiborane.

摘要翻译： 制备可用作抗菌剂的通式[1]表示的7-异二氢吲哚 - 喹诺酮羧酸衍生物的方法及其中间体：包括在金属钯存在下，异二氢吲哚-5-硼酸， 或5-卤代异吲哚啉，在钯催化剂存在下，与二烷氧基硼烷或烷氧基二硼烷。

公开(公告)号：US5366989A

公开(公告)日：1994-11-22

申请号：US986800

申请日：1992-12-08

申请人： Hiroyuki Imaizumi ,  Tetsuya Kajita ,  Kenichi Takashima ,  Minako Yotsuji ,  Keiko Takakura ,  Akira Yotsuji ,  Junichi Mitsuyama ,  Katsumi Shimizu ,  Hiroshi Sakai ,  Hirokazu Narita

发明人： Hiroyuki Imaizumi ,  Tetsuya Kajita ,  Kenichi Takashima ,  Minako Yotsuji ,  Keiko Takakura ,  Akira Yotsuji ,  Junichi Mitsuyama ,  Katsumi Shimizu ,  Hiroshi Sakai ,  Hirokazu Narita

IPC分类号： A61K31/41 ,  A61P31/04 ,  A61P31/10 ,  C07D249/08 ,  C07D401/12 ,  C07D417/06 ,  C07D521/00 ,  A01N43/653

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： The present invention relates to a compound represented by the general formula (1) or its salt, a process for producing the same, and an antifungal agent comprising the same as an effective component: ##STR1## wherein R.sup.1 represents a substituted or unsubstituted aryl group or a substituted or unsubstituted heterocyclic group bonded through a carbon atom in the ring to the main chain; R.sup.2 presents a hydrogen atom, a fluorine atom or a substituted or unsubstituted alkyl group; and R.sup.3 represents a cyano group, a thioamido group or a group represented by the formula ##STR2## in which R.sup.4 is a hydroxyl group or a group of the formula ##STR3## (R.sup.7 and R.sup.8, which may be the same or different, are hydrogen atoms or substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, amino, alkoxy, hydroxyl or heterocyclic groups, and may form a substituted or unsubstituted heterocyclic group together with the nitrogen atom to which R.sup.7 and R.sup.8 attach), R.sup.5 is a substituted or unsubstituted alkoxy group or a group of the formula ##STR4## (R.sup.7 and R.sup.8 are as defined above), and R.sup.6 is a hydrogen atom or a substituted or unsubstituted alkyl group.

摘要翻译： 本发明涉及由通式（1）表示的化合物或其盐，其制备方法和含有该化合物的有效成分的抗真菌剂：有或无取代的芳基或取代或未取代的杂环基 通过环中的碳原子键合到主链上; R2表示氢原子，氟原子或取代或未取代的烷基; 并且R 3表示氰基，硫代酰氨基或由下式表示的基团：其中R 4是羟基或式（R 3和R 8）可以相同或不同， 氢原子或取代或未取代的烷基，烯基，炔基，环烷基，芳基，氨基，烷氧基，羟基或杂环基，并且可以与R7和R8连接的氮原子一起形成取代或未取代的杂环基），R5是 取代或未取代的烷氧基或式6的基团是氢原子或取代或未取代的烷基。

公开(公告)号：US4472386A

公开(公告)日：1984-09-18

申请号：US46109

申请日：1979-06-06

申请人： Tsutomu Kodama ,  Masaakira Senoura ,  Hajime Aoyama ,  Tomonobu Yamaguchi ,  Isao Kitayama ,  Minako Yotsuji ,  Toru Hiraiwa ,  Masaharu Omori ,  Nobuo Terashima ,  Yutaka Kodama

发明人： Tsutomu Kodama ,  Masaakira Senoura ,  Hajime Aoyama ,  Tomonobu Yamaguchi ,  Isao Kitayama ,  Minako Yotsuji ,  Toru Hiraiwa ,  Masaharu Omori ,  Nobuo Terashima ,  Yutaka Kodama

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7072 ,  A61P35/00 ,  C07H19/06 ,  C07H19/073 ,  C07H19/08

CPC分类号： C07H19/06

摘要： 5-Fluoro-(.beta.-uridine or 2'-deoxy-.beta.-uridine) derivatives having an acyl group at the 3-position of the molecule. These compounds are useful as carcinostatic agent. This disclosure relates to such compounds, a process for producing the same and a carcinostatic agent comprising such a compound.

摘要翻译： 在分子的3位具有酰基的5-氟 - （β-尿苷或2'-脱氧-β-尿苷）衍生物。 这些化合物可用作制癌剂。 本公开涉及这样的化合物，其制备方法和包含这种化合物的制癌剂。