公开(公告)号：US5783555A

公开(公告)日：1998-07-21

申请号：US605202

申请日：1996-08-29

申请人： Shigeharu Suzuki ,  Katsumi Takaada

发明人： Shigeharu Suzuki ,  Katsumi Takaada

IPC分类号： A61K9/02 ,  A61K38/57 ,  A61K38/22

CPC分类号： A61K9/02 ,  A61K38/57

摘要： Ulinastatin-containing suppository is produced by emulsifying an aqueous solution of ulinastatin in an oily base uniformly in the presence of an emulsifier and then solidifying the emulsion. The ulinastatin-containing suppository exhibits high stability even if it is stored for a prolonged time. In addition, it can be manufactured on an industrial scale.

摘要翻译： PCT No.PCT / JP95 / 02762 Sec。 371日期：1996年8月29日 102（e）日期1996年8月29日PCT 1995年12月28日PCT PCT。 公开号WO96 / 20726 日期1996年7月11日含有兴奋剂的栓剂是通过在乳化剂的存在下将油状基质中的乌司他丁水溶液乳化，然后使乳液固化而制得的。 含有乌司他丁的栓剂即使长时间储存​​，也表现出高的稳定性。 此外，它可以在工业规模上制造。

公开(公告)号：US5695964A

公开(公告)日：1997-12-09

申请号：US587389

申请日：1996-01-17

申请人： Atsushi Nii ,  Hideaki Morishita ,  Akio Uemura ,  Ei Mochida

发明人： Atsushi Nii ,  Hideaki Morishita ,  Akio Uemura ,  Ei Mochida

IPC分类号： A61K38/00 ,  C07K14/745 ,  C12N15/12 ,  C12N15/63 ,  C12N15/85

CPC分类号： C07K14/7455 ,  A61K38/00

摘要： This invention relates to novel vectors and host cells containing nucleic acids coding for a polypeptide having thrombin binding ability, anticoagulant activity and thrombolytic activity. The polypeptide can be efficiently produced in large quantities by means of genetic recombination techniques using the vectors and host cells of the present invention. Since the polypeptide exhibits anticoagulant activity and thrombolytic activity without generating side effects such as bleeding tendencies, it can be applied effectively to the prevention and treatment of hypercoagulability-related diseases.

摘要翻译： 本发明涉及含有编码具有凝血酶结合能力，抗凝血活性和溶栓活性的多肽的核酸的新载体和宿主细胞。 通过使用本发明的载体和宿主细胞的遗传重组技术可以大量有效地产生多肽。 由于多肽具有抗凝血活性和血栓溶解活性而不产生诸如出血倾向的副作用，因此可有效地应用于预防和治疗高凝状态相关疾病。

公开(公告)号：US5589360A

公开(公告)日：1996-12-31

申请号：US431412

申请日：1995-04-28

申请人： Hideaki Morishita ,  Toshinori Kanamori ,  Masahiro Nobuhara

发明人： Hideaki Morishita ,  Toshinori Kanamori ,  Masahiro Nobuhara

IPC分类号： A61K38/00 ,  C07K14/81 ,  C12N15/15 ,  C12P21/06 ,  C07H19/00 ,  C07H21/00 ,  C12N1/20

CPC分类号： C07K14/811 ,  A61K38/00

摘要： This invention particularly provides a novel polypeptide having high protease-inhibiting activity, preferably FXa-inhibiting activity, which comprises, an lease as a part of the polypeptide, an amino acid sequence resulting from substitution of an amino acid for at least one amino acid in the following amino acid sequence (1), wherein the amino acid substitution is at least one substitution selected from the following substitution means (i) to (iii). It also provides a process for the production of the polypeptide, a novel DNA fragment encoding the polypeptide and a drug composition containing the same.______________________________________ Amino acid sequence (1) ______________________________________ Cys Asn Leu Pro Ile Val Arg Gly Pro Cys Arg Ala Phe Ile Gln Leu Trp Ala Phe Asp Ala Val Lys Gly Lys Cys Val Leu Phe Pro Tyr Gly Gly Cys Gln Gly Asn Gly Asn Lys Phe Tyr Ser Glu Lys Glu Cys Arg Glu Tyr Cys ______________________________________ (i) Substitution of 15 position Gln counting from the N-terminus by an amino acid other than Gln.(ii) Substitution of 42 position Tyr counting from the N-terminus by an amino acid other than Tyr.(iii) Substitution of 7 position Arg counting from the N-terminus by an amino acid other than Arg.

摘要翻译： 本发明特别提供了具有高蛋白酶抑制活性，优选FXa抑制活性的新型多肽，其包括作为多肽的一部分的租赁，由氨基酸取代至少一个氨基酸得到的氨基酸序列 以下氨基酸序列（1），其中所述氨基酸取代为选自以下取代方案（i）至（iii）中的至少一种取代基。 它还提供了制备多肽的方法，编码多肽的新型DNA片段和含有该多肽的药物组合物。 - 氨基酸序列（1） - Cys Asn Leu Pro Ile Val Arg Gly Pro Cys - Arg Ala Phe Ile Gln Leu Trp Ala Phe Asp - Ala Val Lys Gly Lys Cys Val Leu Phe Pro - Tyr Gly Gly Cys Gln Gly Asn Gly Asn Lys-Phe Tyr Ser Glu Lys Glu Cys Arg Glu Tyr - Cys - （i）通过除Gln之外的氨基酸从N末端取代15位Gln。 （ii）用除Tyr之外的氨基酸从N末端取代42位Tyr计数。 （iii）用除Arg以外的氨基酸从N末端取代7位Arg。

公开(公告)号：US5587392A

公开(公告)日：1996-12-24

申请号：US453054

申请日：1995-05-26

申请人： Kimihiro Murakami ,  Shuhei Ohnishi ,  Takashi Yano ,  Manabu Itoh

发明人： Kimihiro Murakami ,  Shuhei Ohnishi ,  Takashi Yano ,  Manabu Itoh

IPC分类号： C07D233/60 ,  C07D249/08 ,  C07D521/00 ,  A61K31/41 ,  C07D403/10 ,  C07D403/12 ,  C07D247/18

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

摘要： Compounds exerting excellent aromatase inhibitory activity in vivo and in vitro with higher specificity and greater safety are provided together with the salts thereof. Using the same, there are also provided, prophylactic agents and/or therapeutical agents of estrogen-dependent diseases, contraceptive agents for females, and aromatase inhibitory agents for use in the form of reagents for human or animals. The compounds are of the formula (I), wherein R.sup.2 is represented by the formula (II) or (III). ##STR1##

摘要翻译： 在其体内和体外具有优异芳香化酶抑制活性的化合物与其盐具有更高的特异性和更高的安全性。 使用同样的方法，还提供雌激素依赖性疾病的预防剂和/或治疗剂，雌性避孕剂和用于人或动物试剂形式的芳香酶抑制剂。 所述化合物具有式（I），其中R 2由式（II）或（III）表示。 （I） （II）或

公开(公告)号：US5521103A

公开(公告)日：1996-05-28

申请号：US719656

申请日：1991-06-24

申请人： Gijsbert Zomer ,  Johannus F. C. Stavenuiter

发明人： Gijsbert Zomer ,  Johannus F. C. Stavenuiter

IPC分类号： G01N33/532 ,  C07D219/02 ,  C07D219/04 ,  C09K11/07 ,  G01N21/76 ,  G01N33/58 ,  G01N33/536 ,  C07K16/18

CPC分类号： C09K11/07 ,  C07D219/04 ,  Y10S436/805

摘要： New acridinium compounds are provided which comply with formula 1, whereinA is a divalent organic moiety, such as an alkylene chain,X is a group which can be transformed together with C-9 of the acridine into a dioxetane by reaction with hydrogen peroxide, such as an aryloxy group,Y is a counter ion, andZ is a functional group, such as a carboxyl derivative.These acridinium compounds are useful as chemiluminogenic labels for both heterogeneous and homogeneous immunoassays.

公开(公告)号：US5438139A

公开(公告)日：1995-08-01

申请号：US188724

申请日：1994-01-31

申请人： Naofumi Sato ,  Hiroshi Mochizuki ,  Toshinori Kanamori

发明人： Naofumi Sato ,  Hiroshi Mochizuki ,  Toshinori Kanamori

IPC分类号： C07D219/04 ,  C07D401/06 ,  C07D401/10 ,  C07K14/00 ,  C07K14/575 ,  C07K16/00 ,  G01N21/76 ,  G01N33/532 ,  G01N33/58 ,  C07D219/08

CPC分类号： C07D219/04

摘要： Acridinium compounds represented by the general formula (I) where A is an intervening group which does not have activity for binding with a specific binding substance, Z is a labelling active group which has activity for binding with a specific binding substance, R.sup.1 is a halogen atom, an alkyl group or an aryl group; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each a hydrogen atom, an alkyl group, an aryl group, an alkoxy group, a nitro group, a halogen atom or a carbonyl group, and Y is a counter ion. The acridinium compounds may form conjugates with specific binding substances. The acridinium compounds have high emission efficiency and stability and, hence, are useful as chemiluminescence labelling agents.

摘要翻译： 由通式（I）表示的吖啶鎓化合物，其中A是不具有与特异性结合物质结合的活性的中间基团，Z是具有与特异性结合物质结合的活性的标记活性基团，R1是卤素 原子，烷基或芳基; R2，R3，R4和R5各自为氢原子，烷基，芳基，烷氧基，硝基，卤素原子或羰基，Y为抗衡离子。 吖啶鎓化合物可以形成具有特异性结合物质的缀合物。 吖啶鎓化合物具有高发射效率和稳定性，因此可用作化学发光标记试剂。

公开(公告)号：US5409895A

公开(公告)日：1995-04-25

申请号：US791213

申请日：1991-11-13

申请人： Hideaki Morishita ,  Toshinori Kanamori ,  Masahiro Nobuhara

发明人： Hideaki Morishita ,  Toshinori Kanamori ,  Masahiro Nobuhara

IPC分类号： A61K38/55 ,  A61K38/00 ,  A61P1/00 ,  A61P1/16 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P11/16 ,  A61P13/02 ,  A61P15/00 ,  A61P29/00 ,  A61P37/08 ,  C07K14/81 ,  C12N1/21 ,  C12N9/99 ,  C12N15/09 ,  C12N15/15 ,  C12P21/02 ,  C12Q1/37 ,  C12R1/19 ,  A61K37/64 ,  C07K7/10

CPC分类号： C07K14/8114 ,  A61K38/005 ,  C12Q1/37

摘要： This invention provides a novel polypeptide which comprises an amino acid sequence that constitutes a portion of urinary trypsin inhibitor (UTI) and which has no antigenicity against human and high activity to inhibit various proteases, as well as other novel polypeptides having excellent activities to inhibit various proteases obtained by mutation of the former novel polypeptide. This invention also provides novel enzyme inhibition processes, drug compositions and treating methods making use of the novel polypeptide, DNA fragments containing nucleotide sequences which encode the novel polypeptides, vectors containing the DNA fragments and transformants transformed with the DNA fragments or the vectors, as well as processes for the production of the novel polypeptides.

摘要翻译： 本发明提供了一种新型多肽，其包含构成尿胰蛋白酶抑制剂（UTI）的一部分的氨基酸序列，并且其对人体没有抗原性和抑制各种蛋白酶的高活性，以及​​具有优异的抑制各种蛋白酶活性的新型多肽 通过前一种新型多肽突变获得的蛋白酶。 本发明还提供新的酶抑制过程，药物组合物和利用新多肽的治疗方法，含有编码新多肽的核苷酸序列的DNA片段，含有DNA片段的载体和用DNA片段或载体转化的转化体 作为生产新型多肽的方法。

公开(公告)号：US5262526A

公开(公告)日：1993-11-16

申请号：US811533

申请日：1991-12-20

申请人： Kazumi Sasamoto ,  Daikichi Horiguchi ,  Masahiro Nobuhara ,  Hiroshi Mochizuki

发明人： Kazumi Sasamoto ,  Daikichi Horiguchi ,  Masahiro Nobuhara ,  Hiroshi Mochizuki

IPC分类号： C07D471/22 ,  C12Q1/68 ,  C12Q1/70 ,  G01N33/533 ,  G01N33/576 ,  G01N33/76 ,  G01N33/78 ,  C07D257/10 ,  C07H19/073 ,  C09D29/036

CPC分类号： C07D471/22 ,  G01N33/533 ,  G01N33/5764 ,  G01N33/76 ,  G01N33/78

摘要： A fluorescent compound, which is readily capable of forming a stable complex with a rare-earth metal ion having fluorescence with satisfactory intensity even in an aqueous system and long fluorescence lifetime when formed a complex with the rare-earth metal ion, a complex of the fluorescent compound and the rare-earth metal ion, and a labelled reagent made therefrom, together with a specific binding assay using said labelling agent.A fluorescent compound expressed by the following formula A, typically exemplified by 2,15-diaza[3,3](2,9)-1,10-phenanthrolinophane-N.sup.2,N.sup.15 -diacetic acid. ##STR1##

公开(公告)号：US5219762A

公开(公告)日：1993-06-15

申请号：US454018

申请日：1989-12-20

申请人： Tomoaki Katamine ,  Hiroshi Sato ,  Ei Mochida

发明人： Tomoaki Katamine ,  Hiroshi Sato ,  Ei Mochida

IPC分类号： C12M1/34 ,  A61B10/00 ,  C12Q1/56 ,  C12Q1/68 ,  G01N33/543 ,  G01N33/574

CPC分类号： G01N33/57473 ,  A61B10/0035 ,  A61B10/0041 ,  G01N33/54366 ,  Y10S435/805 ,  Y10S436/807 ,  Y10T436/112499 ,  Y10T436/25375 ,  Y10T436/2575

摘要： A method for measuring target substance contained in a liquid sample is disclosed. The measurement is carried out by using a device having at least one reaction area comprising a solid phase, and the liquid sample is applied onto the reaction area through a porous member to allow for a reaction of predetermined volume of the liquid sample on the reaction area. A device used for such measurement is also disclosed. A device comprises a body having at least one reaction area comprising a solid phase, and a porous member disposed on or above the reaction area. The porous member allows for the liquid sample to be permeated therethrough.

公开(公告)号：US5158748A

公开(公告)日：1992-10-27

申请号：US642643

申请日：1991-01-17

申请人： Hiroshi Obi ,  Kohei Ishida ,  Ei Mochida

发明人： Hiroshi Obi ,  Kohei Ishida ,  Ei Mochida

IPC分类号： G01F23/14 ,  G01N1/00 ,  G01N1/28 ,  G01N1/38 ,  G01N35/10

CPC分类号： G01N35/109 ,  G01N1/38 ,  G01N2001/382 ,  G01N2035/1025

摘要： A system for automatically dispensing and diluting an accurate volume of a sample includes a nozzle tip removably mounted on a nozzle for collecting a predetermined volume of the sample. The nozzle includes an inner tube and an outer tube. The system also includes a sample pump for sucking and discharging the sample and the reagent into and out of the nozzle tip, a first three-way valve that is adapted to communicate the reagent bottle with the sample pump or the sample pump with the nozzle, and a plunger pump for sucking and discharging a liquid surface-detecting gas supplied from a gas source. A second three way valve is adapted to communicate the gas source with the plunger pump or the plunger pump with the nozzle, and a pressure sensor is positioned between the second three-way valve and the gas passage in the nozzle. Also, a two-way valve is positioned between the pressure sensor and the gas passage of the nozzle.