公开(公告)号：US06337334B1

公开(公告)日：2002-01-08

申请号：US09434474

申请日：1999-11-05

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： A61K31505

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: [wherein R1 represents a lower alkyl group; each of R2 and R3 represents H, alkyl, or alkoxy; each of R4 and R5 represents H or alkyl; R6 represents alkyl, —OR7, or —NR8R9; and n is a number between 0 and 3 inclusive (wherein each of R7, R8, and R9 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： 本发明涉及下式（1）的嘧啶衍生物或其衍生物的盐：其中R 1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。

公开(公告)号：US06297283B1

公开(公告)日：2001-10-02

申请号：US09269764

申请日：1999-04-09

申请人： Hiroyuki Ishiwata ,  Mototsugu Kabeya ,  Masami Shiratsuchi ,  Yukio Hattori ,  Hiroshi Nakao ,  Takao Nagoya ,  Seiichi Sato ,  Soichi Oda ,  Makoto Suda ,  Manabu Shibasaki

发明人： Hiroyuki Ishiwata ,  Mototsugu Kabeya ,  Masami Shiratsuchi ,  Yukio Hattori ,  Hiroshi Nakao ,  Takao Nagoya ,  Seiichi Sato ,  Soichi Oda ,  Makoto Suda ,  Manabu Shibasaki

IPC分类号： A61K31165

CPC分类号： C07D213/40 ,  C07C235/34 ,  C07C235/36 ,  C07C235/38 ,  C07C235/44 ,  C07C235/56 ,  C07C237/34 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07D207/09 ,  C07D207/14 ,  C07D213/75 ,  C07D213/82

摘要： The present invention relates to compounds represented by the following general formula (1): wherein A is a phenyl, naphthyl, dihydronaphthyl, indenyl, pyridyl, indolyl, isoindolyl, quinolyl or isoquinolyl group which may be substituted; X is a lower alkylene group which may be substituted, or the like; Y is a single bond or an alkylene group; Z is a group of —CH═CH—, —C≡C—, —(CH═CH)2—, —C≡C—CH═CH— or —CH═CH—C≡C—, or the like; and R is a hydrogen atom, a lower alkyl group or the like, and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.

摘要翻译： 本发明涉及由以下通式（1）表示的化合物：其中A为可被取代的苯基，萘基，二氢萘基，茚基，吡啶基，吲哚基，异吲哚基，喹啉基或异喹啉基; X是可以被取代的低级亚烷基等; Y是单键或亚烷基; Z是-CH = CH-，-C = C - ， - （CH = CH）2 - ， - C = C-CH = CH-或-CH = CH-C = C - 等的基团; R为氢原子，低级烷基等，以及含有该化合物的药物。 这些化合物对IgE抗体的产生具有优异的抑制作用，因此可用作抗变应性剂等。

公开(公告)号：US5264559A

公开(公告)日：1993-11-23

申请号：US656829

申请日：1991-02-19

申请人： Masahito Nakayama ,  Takeo Deushi ,  Yoshio Takahashi ,  Hiroyuki Ishiwata ,  Yukihiro Okuno ,  Hisakatsu Itoh ,  Masami Shiratsuchi

发明人： Masahito Nakayama ,  Takeo Deushi ,  Yoshio Takahashi ,  Hiroyuki Ishiwata ,  Yukihiro Okuno ,  Hisakatsu Itoh ,  Masami Shiratsuchi

IPC分类号： A01N51/00 ,  C07C291/08

CPC分类号： C07C291/08 ,  A01N51/00 ,  C07C2101/16

摘要： A compound expressed by the formula: ##STR1## in which R.sub.11, R.sub.21 and R.sub.31 are identical with or different from each other and each denotes a hydrogen atom, a halogen atom, an alkyl group, an alkenyl group, a haloalkyl group, an alkoxy group, an alkylthio group, an aryl or an aralkyl group which aromatic ring is optionally substituted appropriately by one to three substituents or a heterocyclic group optionally substituted appropriately by one to three substituents, or R.sub.11 and R.sub.21 may together form an alkylene group, Y denotes O or NOH, with a proviso that where R.sub.21 (or R.sub.11) and R.sub.31 denote a hydrogen atom at the same time, R.sub.11 (or R.sub.21) cannot represent an n-butyl group. This compound is useful as an antifungal agent.

公开(公告)号：US5093480A

公开(公告)日：1992-03-03

申请号：US499435

申请日：1990-06-21

申请人： Masahito Nakayama ,  Isamu Watanabe ,  Takeo Deushi ,  Kazuhiro Kamiya ,  Hisakatsu Ito ,  Masami Shiratsuchi

发明人： Masahito Nakayama ,  Isamu Watanabe ,  Takeo Deushi ,  Kazuhiro Kamiya ,  Hisakatsu Ito ,  Masami Shiratsuchi

IPC分类号： A01N51/00 ,  C07C291/08 ,  C07D213/88 ,  C07D307/68 ,  C07D333/38 ,  C07D521/00

CPC分类号： C07D231/12 ,  A01N51/00 ,  C07C291/08 ,  C07D213/88 ,  C07D233/56 ,  C07D249/08 ,  C07D307/68 ,  C07D333/38

摘要： A novel 2-imino derivative of an antifungal product KA-7367A represented by formula, ##STR1## which has high antifungal activity and excellent stability and is useful as an antifungal agent for warm-blooded animals including humans and for agricultural and horticultural usages.

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。

公开(公告)号：US4394382A

公开(公告)日：1983-07-19

申请号：US271927

申请日：1981-06-09

申请人： Masami Shiratsuchi ,  Noboru Shimizu ,  Hiromichi Shigyo ,  Yoshinori Kyotani ,  Hisashi Kunieda ,  Kiyoshi Kawamura ,  Seiichi Sato ,  Toshihiro Akashi ,  Masahiko Nagakura ,  Naotoshi Sawada ,  Yasumi Uchida

发明人： Masami Shiratsuchi ,  Noboru Shimizu ,  Hiromichi Shigyo ,  Yoshinori Kyotani ,  Hisashi Kunieda ,  Kiyoshi Kawamura ,  Seiichi Sato ,  Toshihiro Akashi ,  Masahiko Nagakura ,  Naotoshi Sawada ,  Yasumi Uchida

IPC分类号： C07D311/04 ,  A61K31/353 ,  A61P9/02 ,  A61P9/04 ,  A61P21/02 ,  C07D311/22 ,  C07D311/58 ,  C07D311/64 ,  C07D311/66 ,  A61K31/35

CPC分类号： C07D311/22 ,  C07D311/58 ,  C07D311/64 ,  C07D311/66 ,  Y10S514/821

摘要： A benzopyran compound represented by the following ##STR1## wherein A represents a direct bond or the bond --CH.sub.2 --O--,R.sub.1 represents a member selected from the group consisting of a C.sub.3 -C.sub.5 alkyl group, a hydroxy-(C.sub.3 -C.sub.5 alkyl) group, a lower alkylamino-lower alkyl group, a nitrato-(C.sub.3 -C.sub.5 alkyl) group and a phenyl-(C.sub.1 -C.sub.5) alkyl group, provided that the phenyl may be substituted by a lower alkoxy group, R.sub.2 represents a member selected from the group consisting of hydrogen, halogen, OH, NO.sub.2, a carbamoyl group, a lower alkyl group, a lower alkoxy group, a lower alkyleneoxy group and acetyl group,R.sub.3 represents hydrogen or NO.sub.2,B represents a direct bond, a C.sub.1 -C.sub.7 alkylene group, a --O-lower alkylene group or a --CONH-lower alkylene group, andn represents 1 or 2;and an acid addition salt thereof and a pharmaceutical composition comprising aforesaid compound.

摘要翻译： 由下式（I）表示的苯并吡喃化合物，其中A表示直接键或键-CH2-O-，R1表示选自C3-C5烷基，羟基 - （C3 -C 5烷基）基，低级烷基氨基 - 低级烷基，硝基 - （C 3 -C 5烷基）基和苯基 - （C 1 -C 5）烷基，条件是苯基可以被低级烷氧基取代，R 2 表示选自氢，卤素，OH，NO 2，氨基甲酰基，低级烷基，低级烷氧基，低级亚烷基氧基和乙酰基的成员，R 3表示氢或NO 2，B表示直接键 ，C 1 -C 7亚烷基，-O-低级亚烷基或-CONH-低级亚烷基，n表示1或2; 及其酸加成盐和包含上述化合物的药物组合物。