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1. 发明授权

US5043425A Thrombin-binding protein substance and process for preparing the same 失效
标题翻译：凝血酶结合蛋白质物质及其制备方法
公开(公告)号：US5043425A
公开(公告)日：1991-08-27
申请号：US394715
申请日：1989-08-16
申请人： Nobuo Aoki , Shigeru Kimura , Masami Shiratsuchi
发明人： Nobuo Aoki , Shigeru Kimura , Masami Shiratsuchi
IPC分类号： C12P21/00 , A61K38/00 , A61P7/02 , C07K1/00 , C07K1/16 , C07K1/22 , C07K14/00 , C07K14/47 , C07K14/745 , C12R1/91
CPC分类号： C07K14/7455 , A61K38/00 , Y10S530/834
摘要： Novel thrombin-binding substances (A) and (B) are disclosed. The thrombin-binding substances have the following characteristics:(a) molecular weight:Thrombin-binding substance (A):90,000-92,000 under reduced conditions55,000-58,000 under unreduced conditionsThrombin-binding substance (B):98,000-105,000 under reduced conditions60,000-65,000 under unreduced conditions(b) isoelectric point:Thrombin-binding substance (A): pH 6.0-6.8Thrombin-binding substance (B): pH 5.8-6.5(c) affinity: strong affinity to thrombin(d) activity:(1) capable of promoting the thrombin catalyzed activation of protein C(2) prolongs clotting time; and(e) stability: stable to denaturing agents (sodium dodecylsulfate and urea).The thrombin-binding substances are useful as a medicine for curing thrombosis.

2. 发明授权

US4748156A Thrombin-binding substance and process for preparing the same 失效
标题翻译：凝血酶结合物质及其制备方法
公开(公告)号：US4748156A
公开(公告)日：1988-05-31
申请号：US3465
申请日：1987-01-15
申请人： Nobuo Aoki , Masami Shiratsuchi , Shigeru Kimura
发明人： Nobuo Aoki , Masami Shiratsuchi , Shigeru Kimura
IPC分类号： A61K35/50 , A61K38/16 , C07G99/00 , C07K3/20 , C07K3/28
CPC分类号： A61K35/50
摘要： A novel thrombin-binding substance having the characteristics of (a) molecular weight: 47,000.+-.6,000 in reduced condition and 38,000.+-.6,000 in unreduced condition, (b) isoelectric point: pH 4.9-5.7, (c) affinity: strong affinity to thrombin, (d) activity: (1) capable of promoting the thrombin catalyzed activation of protein C, (2) prolongs clotting time; and (e) stability: stable to denaturing agents (urea sodium and dodecylsulfate), can be prepared from a human placenta by means of extraction, fractionation using ion exchange chromatography and affinity chromatography, and/or gel filtration, followed by electrophoresis. The substance is useful as a medicine for the treatment of thrombosis.
摘要翻译：一种具有以下特性的新型凝血酶结合物质：（a）分解质量为47,000 +/- 6,000，还原条件为38,000 +/- 6,000，（b）等电点：pH 4.9-5.7，（c）亲和力：（d）活性：（1）能促进凝血酶催化蛋白C的活化，（2）延长凝血时间; 和（e）稳定性：对变性剂（尿素钠和十二烷基硫酸盐）稳定，可以通过提取，使用离子交换层析和亲和层析分离，和/或凝胶过滤，然后电泳从人胎盘制备。该物质可用作治疗血栓形成的药物。

3. 发明授权

US5047503A Thrombin-binding substance and process for its preparation 失效
标题翻译：凝血酶结合物质及其制备方法
公开(公告)号：US5047503A
公开(公告)日：1991-09-10
申请号：US72051
申请日：1987-07-10
申请人： Nobuo Aoki , Shigeru Kimura , Masami Shiratsuchi
发明人： Nobuo Aoki , Shigeru Kimura , Masami Shiratsuchi
IPC分类号： A61K38/00 , C07K14/745 , C07K16/40
CPC分类号： C07K14/7455 , C07K16/40 , A61K38/00 , Y10S530/834
摘要： Thrombin-binding substances are obtained by fractionating human urine by ion-exchange chromatography, affinity chromatography using a thrombin-bound carrier, immune adsorption column chromatography, gel filtration, and/or molecular-weight fractionation. One of the substances has a molecular weight of 46,500.+-.6,000 in reduced condition and 39,000.+-.10,000 in unreduced condition by SDS PAGE and an isoelectric point at pH 5.0-5.3, while the other has a molecular weight of 40,000.+-.8,000 in reduced condition and 31,000.+-.10,000 in unreduced condition by SDS PAGE and an isoelectric point at pH 4.9-5.7. They have strong affinity to thrombin. They are capable of promoting the thrombin catalyzed activation of protein C and prolong clotting time. They are stable to denaturing agents (urea and sodium dodecylsulfate).
摘要翻译：凝血酶结合物质通过离子交换色谱法，使用凝血酶结合载体的亲和层析，免疫吸附柱色谱法，凝胶过滤和/或分子量分级法分级人尿获得。其中一种物质在还原条件下的分子量为46,500 +/- 6,000，通过SDS PAGE分析为39,000 +/- 10,000，在pH 5.0-5.3时为等电点，而另一种的分子量为40,000+ / -8,000的还原条件和31,000 +/- 10,000的未降解条件下通过SDS PAGE和等电点在pH 4.9-5.7。它们对凝血酶具有很强的亲和力。它们能够促进凝血酶催化蛋白C的活化并延长凝血时间。它们对变性剂（尿素和十二烷基硫酸钠）是稳定的。

4. 发明授权

US6008224A Pyrimidine derivatives 失效
标题翻译：嘧啶衍生物
公开(公告)号：US6008224A
公开(公告)日：1999-12-28
申请号：US849725
申请日：1997-06-27
申请人： Mitsuteru Hirata , Takeo Deushi , Yoshio Takahashi , Masahiro Tamura , Takeshi Ohshima , Toshiaki Oda , Hiroyuki Sonoki , Masami Shiratsuchi
发明人： Mitsuteru Hirata , Takeo Deushi , Yoshio Takahashi , Masahiro Tamura , Takeshi Ohshima , Toshiaki Oda , Hiroyuki Sonoki , Masami Shiratsuchi
IPC分类号： C07D239/69 , C07D401/04 , A61K31/505
CPC分类号： C07D239/69
摘要： The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: ##STR1## [wherein R.sup.1 represents a lower alkyl group; each of R.sup.2 and R.sup.3 represents H, alkyl, or alkoxy; each of R.sup.4 and R.sup.5 represents H or alkyl; R.sup.6 represents alkyl, --OR.sup.7, or --NR.sup.8 R.sup.9 ; and n is a number between 0 and 3 inclusive (wherein each of R.sup.7, R.sup.8, and R.sup.9 represents H, alkyl, aryl, aralkyl, amino, a heterocyclic ring, etc.)], as well as to a medicine containing the derivative or salt as the active ingredient. The present compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect and cell proliferation effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.
摘要翻译： PCT No.PCT / JP95 / 02605 Sec。 371日期：1997年6月27日 102（e）日期1997年6月27日PCT 1995年12月19日PCT公布。公开号WO96 / 20177 PCT 日期：1996年7月4日本发明涉及下述式（1）所示的嘧啶衍生物或其衍生物的盐：其中R1表示低级烷基; R 2和R 3各自表示H，烷基或烷氧基; R 4和R 5各自表示H或烷基; R 6表示烷基，-OR 7或-NR 8 R 9; 并且n是0和3之间的数字（其中R7，R8和R9各自表示H，烷基，芳基，芳烷基，氨基，杂环等）]，以及含有该衍生物或盐作为活性成分。本发明化合物对内皮素具有强烈的结合抑制活性，具有强烈的血管收缩作用和细胞增殖作用。因此，该化合物作为包括循环系统疾病在内的各种疾病的治疗方法是有效的。

5. 发明授权

US4678803A Optical isomers, processes for production thereof and pharmaceutical composition thereof 失效
标题翻译：光学异构体，其制备方法及其药物组合物
公开(公告)号：US4678803A
公开(公告)日：1987-07-07
申请号：US716462
申请日：1985-03-27
申请人： Masami Shiratsuchi , Kiyoshi Kawamura , Toshihiro Akashi , Hiroshi Ishihama , Yasumi Uchida
发明人： Masami Shiratsuchi , Kiyoshi Kawamura , Toshihiro Akashi , Hiroshi Ishihama , Yasumi Uchida
IPC分类号： A61K31/35 , A61K31/352 , A61P9/08 , A61P9/12 , A61P25/02 , C07D303/16 , C07D311/64 , C07D407/12
CPC分类号： C07D407/12 , C07D303/16 , C07D311/64
摘要： An optical isomer selected from the group consisting of (2'R),(3R)-3,4-dihydro-8-(2'-hydroxy-3'-isopropylamino)propoxy-3-nitroxy-2H-1-benzopyran, (2'S),(3R)-3,4-dihydro-8-(2'-hydroxy-3'-isopropylamino)propoxy-3-nitroxy-2H-1-benzopyran and acid addition salts of these isomers, process for producing these isomers and a pharmaceutical composition thereof useful for the treatment of cardiovascular diseases.
摘要翻译：选自（2'R），（3R）-3,4-二氢-8-（2'-羟基-3'-异丙基氨基）丙氧基-3-硝基苯基-2H-1-苯并吡喃的旋光异构体，（2'S），（3R）-3,4-二氢-8-（2'-羟基-3'-异丙氨基）丙氧基-3-硝基xy-2H-1-苯并吡喃和这些异构体的酸加成盐，方法制备这些异构体及其用于治疗心血管疾病的药物组合物。

6. 发明授权

US4981954A Novel azoxy compounds and process for production thereof 失效
标题翻译：新型azoxy化合物及其生产方法
公开(公告)号：US4981954A
公开(公告)日：1991-01-01
申请号：US167242
申请日：1988-03-11
申请人： Masahito Nakayama , Hisakatsu Ito , Isamu Watanabe , Masami Shiratsuchi
发明人： Masahito Nakayama , Hisakatsu Ito , Isamu Watanabe , Masami Shiratsuchi
IPC分类号： C12P13/00
CPC分类号： C12R1/465 , C12P13/00 , Y10S435/886
摘要： Novel azoxy compounds having antifungal activity and being useful for the treatment of mycoses, represented by the following formula ##STR1## are prepared by culturing a microorganism of Streptomyces sp. (KC-7367, FERM BP-1277) and separating the compounds from the culture broth.

7. 发明授权

US4727085A Racemates of 3,4-dihydro-8-(2'-hydroxy-3'-isopropylamino)propoxy-3-nitroxy-2H-1-benzo pyran, process for converting them and pharmaceutical compositions thereof 失效
标题翻译： 3,4-二氢-8-（2'-羟基-3'-异丙基氨基）丙氧基-3-硝基氧基-2H-1-苯并吡喃的外消旋体，其转化方法及其药物组合物
公开(公告)号：US4727085A
公开(公告)日：1988-02-23
申请号：US706748
申请日：1985-02-28
申请人： Masami Shiratsuchi , Kiyoshi Kawamura , Toshihiro Akashi , Hiroshi Ishihama , Yasumi Uchida
发明人： Masami Shiratsuchi , Kiyoshi Kawamura , Toshihiro Akashi , Hiroshi Ishihama , Yasumi Uchida
IPC分类号： A61K31/35 , C07D311/64
CPC分类号： A61K31/35 , C07D311/64
摘要： A novel racemate K-351A composed of an optical isomer (2'S),(3S)K-351 [3,4-dihydro-8-(2'-hydroxy-3'-isopropylamino)propoxy-3-nitroxy-2H-1-benzopyran] and (2'R),(3R)K-351, a novel racemate K-351B composed of an optical isomer (2'R),(3S)K-351 and (2'S),(3R)K351 and an acid addition salt of these two novel racemates; a process for converting the two racemates to each other; and also to a pharmaceutical composition comprising each of the two racemates useful for the treatment of cardiovascular diseases.
摘要翻译：由旋光异构体（2'S），（3S）K-351 [3,4-二氢-8-（2'-羟基-3'-异丙氨基）丙氧基-3-硝酰氧基-2H-1 （3S）K-351和（2'S），（3R）K351组成的新型外消旋体K-351B，（3R）K-351 和这两种新型外消旋体的酸加成盐; 将两种消旋体相互转化的过程; 并且还涉及包含用于治疗心血管疾病的两种外消旋体中的每一种的药物组合物。

8. 发明授权

US4448989A N-Nitroxyalkylene benzamide derivatives 失效
标题翻译： N-硝基亚烷基苯甲酰胺衍生物
公开(公告)号：US4448989A
公开(公告)日：1984-05-15
申请号：US451322
申请日：1982-12-20
申请人： Masami Shiratsuchi , Hiroshi Ishihama , Yasumi Uchida
发明人： Masami Shiratsuchi , Hiroshi Ishihama , Yasumi Uchida
IPC分类号： A61K31/165 , A61P9/00 , C07C67/00 , C07C231/00 , C07C235/48 , C07C235/60 , C07D303/22 , C07C103/76 , C07C103/78
CPC分类号： C07D303/22
摘要： A compound represented by the following formula ##STR1## wherein R represents a lower alkyl group having 2 to 6 carbon atoms, and n is an integer of from 1 to 5.
摘要翻译：由下式表示的化合物＆lt; IMAGE＆gt;其中，R表示碳原子数2〜6的低级烷基，n为1〜5的整数。

9. 发明申请

US20080021018A1 (S)-(-)-1-(4-Fluoroisoquinolin-5-Yl)Sulfonyl-2-Methyl-1,4-Homopiperazine Hydrochloride Dihydrate 有权
标题翻译：（S） - （ - ） - 1-（4-氟异喹啉-5-基）磺酰基-2-甲基-1,4-高哌嗪盐酸盐二水合物
公开(公告)号：US20080021018A1
公开(公告)日：2008-01-24
申请号：US11720288
申请日：2005-11-29
申请人： Takeshi Ohshima , Hiroyoshi Hidaka , Masami Shiratsuchi , Kazuhiro Onogi , Toshiaki Oda
发明人： Takeshi Ohshima , Hiroyoshi Hidaka , Masami Shiratsuchi , Kazuhiro Onogi , Toshiaki Oda
IPC分类号： A61K31/551 , A61P9/00 , C07D243/08
CPC分类号： C07D401/12
摘要： The present invention is directed to (S)-(−)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride dihydrate, to a method producing the dihydrate, and to a drug composition containing the dihydrate. The compound of the present invention has less hygroscopicity as compared with (S)-(−)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride anhydrous crystals and thus, exhibits excellent chemical stability.
摘要翻译：本发明涉及（S） - （ - ） - 1-（4-氟异喹啉-5-基）磺酰基-2-甲基-1,4-高哌嗪盐酸盐二水合物，生产二水合物的方法和药物含有二水合物的组合物。与（S） - （ - ） - 1-（4-氟异喹啉-5-基）磺酰基-2-甲基-1,4-高哌嗪盐酸盐无水晶体相比，本发明的化合物具有较少的吸湿性，化学稳定性。

10. 发明授权

US06825223B2 Anilide compounds and pharmaceutical compositions comprising them 失效
标题翻译：酰苯胺化合物和包含它们的药物组合物
公开(公告)号：US06825223B2
公开(公告)日：2004-11-30
申请号：US09789967
申请日：2001-02-21
申请人： Kimiyuki Shibuya , Katsumi Kawamine , Yukihiro Sato , Toshiyuki Edano , Souhei Tanabe , Masami Shiratsuchi
发明人： Kimiyuki Shibuya , Katsumi Kawamine , Yukihiro Sato , Toshiyuki Edano , Souhei Tanabe , Masami Shiratsuchi
IPC分类号： A61K31428
CPC分类号： C07D263/58 , C07D235/28 , C07D277/70
摘要： The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: wherein Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is —NH—, or an oxygen or sulfur atom; Y is —NH—, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or —NR6—; R4 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.
摘要翻译：本发明提供了新的酰苯胺化合物和包含它们的药物组合物。本发明涉及下式的化合物：其中Ar是任选取代的芳基; R 4和R 5相同或不同，并且各自是氢原子，低级烷基基团或低级烷氧基; 并且R 4和R 5可以一起形成低级亚烷基，其中一个或多个亚甲基部分可以任选地被氧和/或硫原子取代; X是-NH-或氧或硫原子; Y是-NH-，氧或硫原子，或亚砜或砜基; Z为单键或-NR 6 - ; R 4表示氢原子或低级亚烷基; 和n为0至15的整数;以及它们的盐和溶剂化物。本发明的化合物可用作药物组合物，特别是作为酰基辅酶A胆固醇酰基转移酶（ACAT）抑制剂。

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