公开(公告)号：US4310533A

公开(公告)日：1982-01-12

申请号：US182513

申请日：1980-08-29

申请人： Yoshiaki Uegai ,  Tsuyoshi Watanabe ,  Masashi Shiota ,  Itsuo Okumoto ,  Naohiro Kayama

发明人： Yoshiaki Uegai ,  Tsuyoshi Watanabe ,  Masashi Shiota ,  Itsuo Okumoto ,  Naohiro Kayama

IPC分类号： A61K31/215 ,  A61K31/245 ,  A61K31/395 ,  A61K31/445 ,  A61P7/04 ,  A61P43/00 ,  C07C279/18 ,  C07D295/185 ,  C12N9/99 ,  C07C101/68

CPC分类号： C07D295/185 ,  C07C279/18

摘要： The guanidinobenzoic acid derivatives of the general formula: ##STR1## wherein Z represents a carbon-carbon covalent bond, or a methylene, ethylene or vinylene group, R.sup.1 represents a hydrogen atom, or a straight- or branched-chain alkyl group containing from 1 to 4 carbon atoms, R.sup.2 represents a straight- or branched-chain alkyl group containing from 4 to 10 carbon atoms, or a cycloalkyl or cycloalkenyl or straight- or branched-chain alkenyl group containing from 3 to 8 carbon atoms, or a phenyl or benzyl group, or NR.sup.1 R.sup.2 represents a 4- to 8-membered heterocyclic ring, and acid addition salts thereof, have anti-plasmin and anti-trypsin activities.

摘要翻译： 通式为：其中Z表示碳 - 碳共价键，或亚甲基，亚乙基或亚乙烯基的通式为（I）的胍基苯甲酸衍生物，R1表示氢原子或直链或支链烷基 含有1至4个碳原子，R 2表示含有4至10个碳原子的直链或支链烷基，或含有3至8个碳原子的环烷基或环烯基或直链或支链烯基，或 苯基或苄基，或NR1R2表示4至8元杂环，并且其酸加成盐具有抗纤溶酶和抗胰蛋白酶活性。

公开(公告)号：US4283418A

公开(公告)日：1981-08-11

申请号：US123609

申请日：1980-02-22

申请人： Setsuro Fujii ,  Tsuyoshi Watanabe ,  Masashi Shiota ,  Itsuo Okumoto ,  Naohiro Kayama

发明人： Setsuro Fujii ,  Tsuyoshi Watanabe ,  Masashi Shiota ,  Itsuo Okumoto ,  Naohiro Kayama

IPC分类号： A61K31/155 ,  A61K31/165 ,  A61K31/18 ,  A61K31/24 ,  A61K31/245 ,  C07C101/56

CPC分类号： A61K31/155 ,  A61K31/165 ,  A61K31/18 ,  A61K31/24 ,  A61K31/245

摘要： Guanidinobenzoic acid derivatives represented by the general formula [I] ##STR1## wherein R.sup.1, R.sup.2 and Z are as defined hereinafter, having antiplasmin and anti-trypsin activities and process for their preparation as well as a pharmaceutical composition and a method of inhibiting the activity of plasmin and trypsin is disclosed.

摘要翻译： 由通式[I]表示的胍基苯甲酸衍生物其中R1，R2和Z如下文所定义，具有抗血浆素和抗胰蛋白酶活性及其制备方法以及药物组合物和方法 公开了抑制纤溶酶和胰蛋白酶的活性。

公开(公告)号：US20060217565A1

公开(公告)日：2006-09-28

申请号：US11443300

申请日：2006-05-31

申请人： Hiroaki Hibino ,  Susumu Ohtsuka ,  Yasunobu Miyamoto ,  Tomoyasu Yoshida ,  Itsuo Okumoto

发明人： Hiroaki Hibino ,  Susumu Ohtsuka ,  Yasunobu Miyamoto ,  Tomoyasu Yoshida ,  Itsuo Okumoto

IPC分类号： C07D311/02

CPC分类号： C07C205/37 ,  C07C201/12 ,  C07D311/24

摘要： A process for producing a dicarboxylic acid compound represented by the formula (4): wherein R1 and R2 are the same or different and each represents lower alkyl and the wavy line indicates that this compound is the E- or Z-isomer or a mixture of them, characterized by reacting a compound represented by the formula (2): wherein R1, R2 and the wavy line have the same meanings as the above, and one of X2 and X3 represents hydrogen and the other represents halogen, with nitrophenol represented by the formula (3): in the presence of a base; a process for producing a nitrochromone compound represented by the formula (5): wherein R1 has the same meaning as the above, characterized by reacting the dicarboxylic acid compound or carboxylic acid thereof with an acid; a process for producing an aminochromone compound which comprises reducing the nitrochromone compound; and a process for producing an amidochromone compound which comprises acylating the aminochromone compound are provided.

公开(公告)号：US20050085664A1

公开(公告)日：2005-04-21

申请号：US10506119

申请日：2003-02-27

申请人： Hiroaki Hibino ,  Susumu Ohtsuka ,  Yasunobu Miyamoto ,  Tomoyasu Yoshida ,  Itsuo Okumoto

发明人： Hiroaki Hibino ,  Susumu Ohtsuka ,  Yasunobu Miyamoto ,  Tomoyasu Yoshida ,  Itsuo Okumoto

IPC分类号： C07C205/37 ,  C07D311/24 ,  C07C25/53

CPC分类号： C07C205/37 ,  C07C201/12 ,  C07D311/24

摘要： A process for producing a dicarboxylic acid compound represented by the formula (4): wherein R1 and R2 are the same or different and each represents lower alkyl and the wavy line indicates that this compound is the E- or Z-isomer or a mixture of them, characterized by reacting a compound represented by the formula (2): wherein R1, R2 and the wavy line have the same meanings as the above, and one of X2 and X3 represents hydrogen and the other represents halogen, with nitrophenol represented by the formula (3): in the presence of a base; a process for producing a nitrochromone compound represented by the formula (5): wherein R1 has the same meaning as the above, characterized by reacting the dicarboxylic acid compound or carboxylic acid thereof with an acid; a process for producing an aminochromone compound which comprises reducing the nitrochromone compound; and a process for producing an amidochromone compound which comprises acylating the aminochromone compound are provided.

摘要翻译： 一种由式（4）表示的二羧酸化合物的制备方法：其中R 1和R 2相同或不同，各自代表低级烷基和波浪线 表示该化合物是E-或Z-异构体或它们的混合物，其特征在于使由式（2）表示的化合物：其中R 1，R 2， >和波浪线具有与上述相同的含义，X 2和X 3之一表示氢，而另一个表示卤素，由式（ 3）：在一个基地的存在下; 一种制备由式（5）表示的硝基色酮化合物的方法：其中R 1具有与上述相同的含义，其特征在于使二羧酸化合物或其羧酸与酸反应; 一种制备氨基色酮化合物的方法，其包括还原硝基色酮化合物; 并提供了包括酰化氨基色酮化合物的酰胺色酮化合物的制备方法。

公开(公告)号：US06861566B2

公开(公告)日：2005-03-01

申请号：US10468226

申请日：2002-03-11

申请人： Hiroaki Hibino ,  Susumu Ohtsuka ,  Yasunobu Miyamoto ,  Itsuo Okumoto

发明人： Hiroaki Hibino ,  Susumu Ohtsuka ,  Yasunobu Miyamoto ,  Itsuo Okumoto

IPC分类号： C07C17/32 ,  C07C17/26 ,  C07C22/04 ,  C07C41/30 ,  C07C17/00 ,  C07C22/00 ,  C07C25/00

CPC分类号： C07C41/30 ,  C07C17/2632 ,  C07C22/04 ,  C07C43/225

摘要： There is provided an industrially advantageous process for producing a 1-chloro-4-arylbutane represented by the general formula (2): wherein R represents hydrogen, lower alkyl, or lower alkoxy, characterized by reacting 1-bromo-3-chloropropane with a compound represented by the general formula (1): wherein R is as defined above; and X represents chlorine, bromine, or iodine, in a solvent.

摘要翻译： 提供了用于制备由通式（2）表示的1-氯-4-芳基丁烷的工业上有利的方法：其中R表示氢，低级烷基或低级烷氧基，其特征在于使1-溴-3-氯丙烷与 由通式（1）表示的化合物：其中R如上定义; X表示氯，溴或碘。

公开(公告)号：US07094914B2

公开(公告)日：2006-08-22

申请号：US10506119

申请日：2003-02-27

申请人： Hiroaki Hibino ,  Susumu Ohtsuka ,  Yasunobu Miyamoto ,  Tomoyasu Yoshida ,  Itsuo Okumoto

发明人： Hiroaki Hibino ,  Susumu Ohtsuka ,  Yasunobu Miyamoto ,  Tomoyasu Yoshida ,  Itsuo Okumoto

IPC分类号： C07D311/24 ,  C07C205/37

CPC分类号： C07C205/37 ,  C07C201/12 ,  C07D311/24

摘要： A process for producing a dicarboxylic acid compound represented by the formula (4): wherein R1 and R2 are the same or different and each represents lower alkyl and the wavy line indicates that this compound is the E- or Z-isomer or a mixture of them, characterized by reacting a compound represented by the formula (2): wherein R1, R2 and the wavy line have the same meanings as the above, and one of X2 and X3 represents hydrogen and the other represents halogen, with nitrophenol represented by the formula (3): in the presence of a base; a process for producing a nitrochromone compound represented by the formula (5): wherein R1 has the same meaning as the above, characterized by reacting the dicarboxylic acid compound or carboxylic acid thereof with an acid; a process for producing an aminochromone compound which comprises reducing the nitrochromone compound; and a process for producing an amidochromone compound which comprises acylating the aminochromone compound are provided.

摘要翻译： 一种由式（4）表示的二羧酸化合物的制备方法：其中R 1和R 2相同或不同，各自代表低级烷基和波浪线 表示该化合物是E-或Z-异构体或它们的混合物，其特征在于使由式（2）表示的化合物：其中R 1，R 2， >和波浪线具有与上述相同的含义，X 2和X 3之一表示氢，而另一个表示卤素，由式（ 3）：在一个基地的存在下; 一种制备由式（5）表示的硝基色酮化合物的方法：其中R 1具有与上述相同的含义，其特征在于使二羧酸化合物或其羧酸与酸反应; 一种制备氨基色酮化合物的方法，其包括还原硝基色酮化合物; 并提供了包括酰化氨基色酮化合物的酰胺色酮化合物的制备方法。