公开(公告)号：US5279835A

公开(公告)日：1994-01-18

申请号：US906465

申请日：1992-06-30

申请人： Kiichi Sawai ,  Masayasu Kurono ,  Takahiko Mitani ,  Yasuaki Kondo ,  Makoto Sato ,  Yoshiro Ishiwata ,  Syoji Yokochi ,  Toshiyuki Kouzaki

发明人： Kiichi Sawai ,  Masayasu Kurono ,  Takahiko Mitani ,  Yasuaki Kondo ,  Makoto Sato ,  Yoshiro Ishiwata ,  Syoji Yokochi ,  Toshiyuki Kouzaki

IPC分类号： A61K9/20 ,  A61K31/28 ,  A61K31/80 ,  A61K47/02 ,  A61K47/26 ,  A61P43/00

CPC分类号： A61K31/80 ,  A61K31/28 ,  A61K9/2009 ,  A61K9/2018

摘要： A 3-oxygermylpropionic acid preparation is provided, which activates the action of 3-oxygermylpropionic acid having the general formula:[(O.sub.1/2).sub.3 GeCH.sub.2 CH.sub.2 COOH]n wherein n=an integer of at least 1 and is readily solubilized and disintegrated in vivo. The present preparation is manufactured by compression-molding at high pressure a composition comprising 3-oxygermylpropionic acid and two or more low-molecular substance of high solubility in water. The low-molecular substances are selected from the group consisting of white sugar, sorbitol, fructose, sucrose, glucose, lactose, mannitol and sodium chloride.

摘要翻译： 提供了3-氧基甲基丙酸制剂，其活化具有以下通式的3-氧基甲基丙酸的作用：（（O1 / 2）3GeCH2CH2COOH）n，其中n =至少为1的整数，并且在体内容易溶解和分解。 本制剂通过高压压缩成型制备，该组合物包含3-氧基甲基丙酸和两种或更多种在水中的高溶解度的低分子量物质。 低分子物质选自白糖，山梨糖醇，果糖，蔗糖，葡萄糖，乳糖，甘露醇和氯化钠。

公开(公告)号：US5308836A

公开(公告)日：1994-05-03

申请号：US116682

申请日：1993-09-07

申请人： Kiichi Sawai ,  Masayasu Kurono ,  Yasuaki Kondo ,  Makoto Sato ,  Toshiyuki Kouzaki

发明人： Kiichi Sawai ,  Masayasu Kurono ,  Yasuaki Kondo ,  Makoto Sato ,  Toshiyuki Kouzaki

IPC分类号： A61K9/08 ,  A61K38/22 ,  A61K47/02 ,  A61K47/10 ,  A61K47/12 ,  A61K47/18 ,  A61K47/26 ,  A61K47/36 ,  A61K47/42 ,  A61P1/00 ,  C07K1/00 ,  C07K14/00 ,  C07K14/575 ,  A61K37/24 ,  A61K37/36

CPC分类号： A61K38/2214

摘要： There is disclosed a pharmaceutical composition of stabilized [Leu.sup.13 ]-motilin-Hse. The composition comprises at least one of organic acids and salts thereof, as a first stabilizer, and pH thereof is adjusted in a range of 5.5-8.0. The composition may contain at least one of substances selected from saccharides, amino acids, proteins and salts thereof, as a second stabilizer. Conversion of [Leu.sup.13 ]-motilin-Hse into [Leu.sup.13 ]-motilin-Hse-lactone is suppressed by increasing pH value and deamidization in asparagine residue at 19-position is suppressed by the presence of the organic acid or salt thereof.

摘要翻译： 公开了一种稳定的[Leu13] -Motilin-Hse的药物组合物。 该组合物包含至少一种有机酸及其盐作为第一稳定剂，其pH调节在5.5-8.0的范围内。 该组合物可以含有选自糖，氨基酸，蛋白质和盐的至少一种物质作为第二稳定剂。 通过增加pH值可以抑制[Leu13] -motilin-Hse转化为[Leu13] - 肌动蛋白-Hse-内酯，并且通过存在有机酸或其盐来抑制在19位的天冬酰胺残基中的脱酰胺化。

公开(公告)号：US4857521A

公开(公告)日：1989-08-15

申请号：US6199

申请日：1987-01-23

申请人： Masayasu Kurono ,  Yutaka Baba ,  Takahiko Mitani ,  Masao Onishi ,  Yasuaki Kondo ,  Kiichi Sawai

发明人： Masayasu Kurono ,  Yutaka Baba ,  Takahiko Mitani ,  Masao Onishi ,  Yasuaki Kondo ,  Kiichi Sawai

IPC分类号： A61K31/695 ,  A61P31/04 ,  C07F7/08 ,  C07F7/18

CPC分类号： C07F7/08 ,  Y02P20/55

摘要： A cephalosporin derivative represented by the formula ##STR1## wherein R is an organic residue known on .beta.-lactam antibiotics and Q is a radical of ##STR2## dotted-line means a possible double bond, R.sub.1 is hydrogen or monovalent substituent, R.sub.2, R.sub.3 and R.sub.4 are mono-valent substituent, respectively,a salt thereof, a process for the manufacture thereof and a pharmaceutical agent comprising same.

摘要翻译： 由式（I）表示的头孢菌素衍生物，其中R是β-内酰胺抗生素已知的有机残基，Q是虚线所示的基团是指可能的双键，R 1是氢或一价取代基， R2，R3和R4分别为一价取代基，其盐，其制备方法和包含其的药剂。

公开(公告)号：US5008416A

公开(公告)日：1991-04-16

申请号：US540535

申请日：1990-06-19

申请人： Masayasu Kurono ,  Yasuaki Kondo ,  Takahiko Mitani ,  Yutaka Baba ,  Kiichi Sawai

发明人： Masayasu Kurono ,  Yasuaki Kondo ,  Takahiko Mitani ,  Yutaka Baba ,  Kiichi Sawai

IPC分类号： C07F7/30

CPC分类号： C07F7/30

摘要： An organogermanium compound of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are hydrogen atom, alkyl, substituted alkyl, phenyl or substituted phenyl, and R.sub.5 is a radical of ##STR2## n is an integer of 2 or more, and R.sub.6 and R.sub.7 are hydrogen atom, alkyl, substituted alkyl, phenyl or substituted phenyl,a salt of the compound, a processs for the preparation of the compound as well as a use of the compound as an affective ingredient for pharmaceutical preparations.

公开(公告)号：US4870062A

公开(公告)日：1989-09-26

申请号：US183575

申请日：1988-04-19

申请人： Masayasu Kurono ,  Ryoichi Unno ,  Yukiharu Matsumoto ,  Yasuaki Kondo ,  Takahiko Mitani ,  Takahito Jomori ,  Hisashi Michishita ,  Kiichi Sawai

发明人： Masayasu Kurono ,  Ryoichi Unno ,  Yukiharu Matsumoto ,  Yasuaki Kondo ,  Takahiko Mitani ,  Takahito Jomori ,  Hisashi Michishita ,  Kiichi Sawai

IPC分类号： A61K31/28 ,  A61K31/282 ,  A61K31/55 ,  A61P35/00 ,  C07F15/00

CPC分类号： C07F15/0093

摘要： A removable rating plug for a circuit breaker provides an active variable impedance in series with a reference resistor between the sensing terminals of the circuit breaker trip circuit to adjust the sensing voltage produced in response to the input current received from current monitors in the protected circuit. The active variable impedance, which is energized by the input current, includes a high gain transistor amplifier, preferably a Darlington transistor, controlled by an operational amplifier. A control circuit includes a pair of reference diodes which match the forward drop across the Darlington transistor when full on, in series with a reference voltage selection circuit which applies a reference voltage to the non-inverting input of the operational amplifier. The voltage at the connection between the Darlington transistor and the reference resistor is fed back to the inverting input of the operational amplifier so that the gain of the amplifier, and therefore the variable impedance in series with the reference resistor, varies with the reference voltage.

公开(公告)号：US5110945A

公开(公告)日：1992-05-05

申请号：US776039

申请日：1991-10-15

申请人： Masayasu Kurono ,  Yasuaki Kondo ,  Yukiharu Matsumoto ,  Mitsuru Oka ,  Kiichi Sawai

发明人： Masayasu Kurono ,  Yasuaki Kondo ,  Yukiharu Matsumoto ,  Mitsuru Oka ,  Kiichi Sawai

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： There are described 1-azoniabicyclo[3.3.0]oct-1(5)-ene salt derivatives inclusive of 1-azonia-4,6-dimethylbicyclo[3.3.0]oct-1(5)-ene perchlorate, and a process for the preparation of the same. The derivatives can be prepared by heating dicyclopropylmethanimine salt derivative in a solvent, in the presence or absence of an ammonium salt. Each of the derivatives is employed as an intermediate for preparing various medicines and agricultural chemicals.

公开(公告)号：US4978758A

公开(公告)日：1990-12-18

申请号：US355624

申请日：1989-05-23

申请人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Kenji Miura ,  Toshinao Usui ,  Naofumi Terada ,  Kyoichi Asano ,  Kuniharu Mizuno ,  Akira Matsubara ,  Noriaki Kato ,  Kiichi Sawai ,  Ryoichi Unno ,  Hiroshi Ozawa ,  Masato Fukushima

发明人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Kenji Miura ,  Toshinao Usui ,  Naofumi Terada ,  Kyoichi Asano ,  Kuniharu Mizuno ,  Akira Matsubara ,  Noriaki Kato ,  Kiichi Sawai ,  Ryoichi Unno ,  Hiroshi Ozawa ,  Masato Fukushima

IPC分类号： C07D311/24 ,  C07D491/10 ,  C07D491/107 ,  C07D495/10

CPC分类号： C07D491/10 ,  C07D311/24 ,  C07D495/10

摘要： Hydantoin derivatives and salts thereof, intermediates therefor, process for the preparation thereof, and medicines containing the derivative, wherein said derivatives have the formula ##STR1## wherein one of V and W is hydrogen and the other is a halogenomethyl group, 1H-tetrazol-5-yl radical, --COOR group,in which R is hydrogen atom, an alkyl group, --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n is an integer of 1 to 113) or substituted phenyl, ##STR2## group, in which R.sub.1 and R.sub.2 are same or different independently, each is hydrogen atom, an alkyl group, substituted phenyl or --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n has the meaning as referred to) or R.sub.1 may form a heterocyclic ring together with R.sub.2 and nitrogen or oxygen atom, --CH.sub.2 OR.sub.3 group or ##STR3## group, in which R.sub.3 and R.sub.4 are same or different independently and each is hydrogen atom or an alkyl group,X is oxygen or sulfur atom, and Y and Z are same or different independently and each is hydrogen atom, a halogen atom, alkyl group, alkoxy group, alkylmercapto group, nitro radical or --NHR.sub.5 group, in which R.sub.5 is hydrogen atom or an acyl group.The derivatives and salts thereof are useful for the treatment of complications of diabetes.

公开(公告)号：US4897495A

公开(公告)日：1990-01-30

申请号：US351006

申请日：1989-05-12

申请人： Masayasu Kurono ,  Yasuaki Kondo ,  Ryoichi Unno ,  Yukiharu Matsumoto ,  Hiromoto Kimura ,  Mitsuru Oka ,  Kiichi Sawai

发明人： Masayasu Kurono ,  Yasuaki Kondo ,  Ryoichi Unno ,  Yukiharu Matsumoto ,  Hiromoto Kimura ,  Mitsuru Oka ,  Kiichi Sawai

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： A process for the preparation of pyrrolizine derivatives of the formula ##STR1## wherein R is --CN or --CH.sub.2 NH.sub.2, and salts thereof.

公开(公告)号：US5177102A

公开(公告)日：1993-01-05

申请号：US695121

申请日：1991-05-03

申请人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Ryoichi Unno ,  Hiromoto Kimura ,  Noboru Kuboyama ,  Takashi Ito ,  Mitsuru Oka ,  Akira Tashita ,  Kazumasa Nakano ,  Kiichi Sawai

发明人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Ryoichi Unno ,  Hiromoto Kimura ,  Noboru Kuboyama ,  Takashi Ito ,  Mitsuru Oka ,  Akira Tashita ,  Kazumasa Nakano ,  Kiichi Sawai

IPC分类号： A61K31/13 ,  A61K31/155 ,  A61P1/04 ,  C07C211/10 ,  C07C211/15 ,  C07C217/46 ,  C07C323/25 ,  C07C323/41 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07C323/25

摘要： There are given disclosures on a polyisoprene compound of the formula ##STR1## wherein Y is S, O, NH or ##STR2## .sub.l is an integer of 2-10, Z is a group of ##STR3## R.sup.1 and R.sup.2 are same or different and each means a hydrogen atom or an alkyl group having C.sub.1-4, m is an integer of 0 or 1, and .sub.n is an integer of 0, 1 or 2,a salt thereof, a process for the preparation of same, and use thereof.

公开(公告)号：US4985573A

公开(公告)日：1991-01-15

申请号：US355623

申请日：1989-05-23

申请人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Kenji Miura ,  Toshinao Usui ,  Naofumi Terada ,  Kyoichi Asano ,  Kuniharu Mizuno ,  Akira Matsubara ,  Noriaki Kato ,  Kiichi Sawai ,  Ryoichi Unno ,  Hiroshi Ozawa ,  Masato Fukushima

发明人： Masayasu Kurono ,  Yasuaki Kondo ,  Takuji Yamaguchi ,  Kenji Miura ,  Toshinao Usui ,  Naofumi Terada ,  Kyoichi Asano ,  Kuniharu Mizuno ,  Akira Matsubara ,  Noriaki Kato ,  Kiichi Sawai ,  Ryoichi Unno ,  Hiroshi Ozawa ,  Masato Fukushima

IPC分类号： C07D311/24 ,  C07D491/10 ,  C07D495/10

CPC分类号： C07D491/10 ,  C07D311/24 ,  C07D495/10

摘要： Hydantoin derivatives and salts thereof, intermediates therefor, process for the preparation thereof, and medicines containing the derivative, wherein said derivatives have the formula ##STR1## wherein one of V and W is hydrogen and the other is a halogenomethyl group, 1H-tetrazol-5-yl radical, --COOR group, in which R is hydrogen atom, an alkyl group, --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n is an integer of 1 to 113) or substituted phenyl, ##STR2## in which R.sub.1 and R.sub.2 are same or different independently, each is hydrogen atom, an alkyl group, substituted phenyl or --(CH.sub.2 CH.sub.2 O)nCH.sub.3 group (n has the meaning as referred to) or R.sub.1 may form a heterocyclic ring together with R.sub.2 and nitrogen or oxygen atom, ##STR3## in which R.sub.3 and R.sub.4 are same or different independently and each is hydrogen atom or an alkyl group,X is oxygen or sulfur atom, and Y and Z are same or different independently and each is hydrogen atom, a halogen atom, alkyl group, alkoxy group, alkylmercapto group, nitro radical or --NHR.sub.5 group, in which R.sub.5 is hydrogen atom or an acyl group.The derivatives and salts thereof are useful for the treatment of complications of diabetes.

摘要翻译： 乙内酰脲衍生物及其盐，其中间体，其制备方法和含有该衍生物的药物，其中所述衍生物具有式“IMAGE”，其中V和W之一是氢，另一个是卤代甲基，1H-四唑 - 其中R为氢原子，烷基， - （CH 2 CH 2 O）n CH 3基（n为1至113的整数）或取代的苯基，其中R 1和R 2相同的-COOR基团 或独立地不同，各自为氢原子，烷基，取代的苯基或 - （CH 2 CH 2 O）n CH 3基团（n具有所述的含义）或R 1可以与R 2和氮或氧原子一起形成杂环， 其中R3和R4独立地相同或不同，各自为氢原子或烷基，X为氧或硫原子，Y和Z独立地相同或不同，各自为氢原子，卤素原子，烷基，烷氧基 基团，烷基巯基，硝基或-NHR 5基团 ch R5是氢原子或酰基。 其衍生物和盐可​​用于治疗糖尿病并发症。