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1. 发明授权

US06576642B2 Diamide compounds and compositions containing the same 失效
标题翻译：二酰胺化合物和含有它们的组合物
公开(公告)号：US06576642B2
公开(公告)日：2003-06-10
申请号：US09858592
申请日：2001-05-17
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： Compounds having the formula (1): wherein A is a phenyl, naphthyl, dihydronaphthyindeny, pyridyl, indolyl,isoindolyl, quinolyl or isoquinolyl group which are optionally substituted; X is optionally substituted alicyclic, aromatic, imino or heterocyclic groups or —S— or —O—; Y is a single bond or an alkylene group; Z is an unsubstituted aliphatic group or divalent residue of benzene or pyridine, which is optionally substituted; anis hydrogen, lower alkyl, cycloalkyl, aryl or aralkyl; with certain provisos. These compounds exhibit an inhibitory effect on the production of IgE antibodies and are, hence, useful as antiallergic agents.
摘要翻译：具有式（1）的化合物：其中A是任选取代的苯基，萘基，二氢萘并噻吩基，吡啶基，吲哚基，异吲哚基，喹啉基或异喹啉基; X是任选取代的脂环族，芳族，亚氨基或杂环基或-S-或-O-; Y是单键或亚烷基; Z是任选取代的未取代的脂族基团或苯或吡啶的二价残基; 芳烃氢，低级烷基，环烷基，芳基或芳烷基; 具有一定的条件。这些化合物对IgE抗体的产生具有抑制作用，因此可用作抗过敏剂。

2. 发明授权

US5541169A Azoxy compound 失效
标题翻译：偶氮化合物
公开(公告)号：US5541169A
公开(公告)日：1996-07-30
申请号：US232245
申请日：1994-05-10
申请人： Takeo Deushi , Yoshio Takahashi , Hiroyuki Ishiwata , Yukihiro Okuno , Toshiaki Oda , Masami Shiratsuchi , Katsuhiro Yamamoto
发明人： Takeo Deushi , Yoshio Takahashi , Hiroyuki Ishiwata , Yukihiro Okuno , Toshiaki Oda , Masami Shiratsuchi , Katsuhiro Yamamoto
IPC分类号： A01N51/00 , C07C291/08 , A61K31/655
CPC分类号： C07C291/08 , A01N51/00
摘要： An azoxy compound represented by the following general formula ##STR1## wherein R.sub.1 denotes a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkoxy group, a lower alkoxy-lower alkoxy group or a group of the formula X.sub.1 --C.tbd.C--CH.sub.2 O-- wherein X.sub.1 is a hydrogen atom or a halogen atom;R.sub.2 denotes a hydrogen atom or a lower alkyl group;R.sub.3 denotes a hydrogen atom or a lower alkyl group;R.sub.4 denotes a hydrogen atom or a group of the formula X.sub.2 --C.tbd.C--CH.sub.2 -- wherein X.sub.2 is a hydrogen atom or a halogen atom;R.sub.5 denotes a hydrogen atom or a lower alkyl group;andn is 0 or 1.This compound has an excellent antifungal activity against fungi infectious to warm-blooded animals and fungi infectious to agrohorticultural crops or fruit trees, and is useful as a medicine, a veterinary drug and an agrohorticultural antifungal agent.
摘要翻译： PCT No.PCT / JP93 / 01295 Sec。 371日期1994年5月10日 102（e）日期1994年5月10日PCT提交1993年9月10日PCT公布。出版物WO94 / 05629 日期：1994年3月17日由以下通式表示的氧化偶氮化合物（Ⅰ）其中R1表示氢原子，卤原子，羟基，低级烷氧基，低级烷氧基 - 低级烷氧基或基团式X1-C3Bic C-CH2O-，其中X1是氢原子或卤素原子; R2表示氢原子或低级烷基; R3表示氢原子或低级烷基; R4表示氢原子或式X2-C 3BOND C-CH2-的基团，其中X2是氢原子或卤素原子; R5表示氢原子或低级烷基; 并且n为0或1.该化合物对感染了农作物或果树的温血动物和真菌感染真菌具有优异的抗真菌活性，并且可用作药物，兽药和农业园艺抗真菌剂。

3. 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.

4. 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。

5. 发明授权

US4482562A Aromatic aminoethanol compounds, and utilization thereof as cardiovascular agents 失效
标题翻译：芳香族氨基乙醇化合物及其作为心血管药物的用途
公开(公告)号：US4482562A
公开(公告)日：1984-11-13
申请号：US414819
申请日：1982-09-03
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： A61K31/21 , A61K31/135 , A61K31/165 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61P9/00 , A61P9/12 , A61P25/02 , A61P25/28 , C07C67/00 , C07C203/04 , C07C213/00 , C07C217/32 , C07C217/70 , C07C219/16 , C07C219/34 , C07C225/16 , C07C231/00 , C07C231/12 , C07C235/42 , C07C235/46 , C07C237/30 , C07C301/00 , C07C303/40 , C07C311/17 , C07C311/29 , C07C313/00 , C07C315/04 , C07C317/22 , C07C317/24 , C07C317/32 , C07C319/20 , C07C323/25 , C07D213/30 , C07D213/60 , C07D213/64 , C07D213/69 , C07D303/24 , C07D303/26 , C07D309/12 , C07D213/74
CPC分类号： C07D213/64 , C07C203/04 , C07D213/69 , C07D303/24 , C07D303/26 , C07D309/12
摘要： A compound represented by the following formula ##STR1## wherein A represents a direct bond or the bond --O--CH.sub.2 --,B represents a C.sub.1 -C.sub.11 alkylene group bonded to a carbon atom of the aromatic ring D either directly or through --O--, --S--, --SO-- or --NH--,W represents a carbon or nitrogen atom,R.sub.1 represents a C.sub.3 -C.sub.7 alkyl group, a hydroxy-C.sub.1 -C.sub.6 alkyl group, or a phenyl- or diphenyl-alkyl group with the alkyl group having 1 to 4 carbon atoms,R.sub.2 represents a member selected from the group consisting of hydrogen, halogen, OH, C.sub.1 -C.sub.4 alkyl, NO.sub.2, C.sub.1 -C.sub.4 alkoxy, acetyl, allyloxy, carbamoyl and sulfamoyl, and when two or more R.sub.2 groups exist, they may be identical or different, andn represents 1, 2 or 3 and m represents 1 or 2, provided that n+m.gtoreq.4;and an acid addition salt thereof; a process for producing the same; and a pharmaceutical composition comprising aforesaid compound.

6. 发明授权

US4374840A Certain phenyl or pyridyl-propanol-amines containing alkyl-nitrate moieties 失效
标题翻译：含有烷基 - 硝酸盐部分的某些苯基或吡啶基 - 丙醇 - 胺
公开(公告)号：US4374840A
公开(公告)日：1983-02-22
申请号：US233643
申请日：1981-02-11
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： A61K31/21 , A61K31/135 , A61K31/165 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61P9/00 , A61P9/12 , A61P25/02 , A61P25/28 , C07C67/00 , C07C203/04 , C07C213/00 , C07C217/32 , C07C217/70 , C07C219/16 , C07C219/34 , C07C225/16 , C07C231/00 , C07C231/12 , C07C235/42 , C07C235/46 , C07C237/30 , C07C301/00 , C07C303/40 , C07C311/17 , C07C311/29 , C07C313/00 , C07C315/04 , C07C317/22 , C07C317/24 , C07C317/32 , C07C319/20 , C07C323/25 , C07D213/30 , C07D213/60 , C07D213/64 , C07D213/69 , C07D303/24 , C07D303/26 , C07D309/12 , C07D213/74
CPC分类号： C07D213/64 , C07C203/04 , C07D213/69 , C07D303/24 , C07D303/26 , C07D309/12
摘要： A compound represented by the following formula ##STR1## wherein A represents a direct bond or the bond --0--CH.sub.2--,B represents a C.sub.1 -C.sub.11 alkylene group bonded to a carbon atom of the aromatic ring D either directly or through --O--, --S--, --SO-- or --NH--,W represents a carbon or nitrogen atom,R.sub.1 represents a C.sub.3 -C.sub.7 alkyl group, a hydroxy-C.sub.1 -C.sub.6 alkyl group, or a phenyl- or diphenyl-alkyl group with the alkyl group having 1 to 4 carbon atoms,R.sub.2 represents a member selected from the group consisting of hydrogen, halogen, OH, C.sub.1 -C.sub.4 alkyl, NO.sub.2, C.sub.1 -C.sub.4 alkoxy, acetyl, allyloxy, carbamoyl and sulfamoyl, and when two or more R.sub.2 groups exist, they may be identical or different, andn represents 1, 2 or 3 and m represents 1 or 2, provided that n+m.gtoreq.4;and an acid addition salt thereof; a process for producing the same; and a pharmaceutical composition comprising aforesaid compound.
摘要翻译：由下式表示的化合物：其中A表示直接键或-O-CH 2 - 键，B表示与芳环D的碳原子键合的C1-C11亚烷基直接或-O- ，-S-，-SO-或-NH-，W表示碳原子或氮原子，R1表示C3-C7烷基，羟基-C1-C6烷基或苯基或二苯基 - 烷基，其中具有1至4个碳原子的烷基，R 2表示选自氢，卤素，OH，C 1 -C 4烷基，NO 2，C 1 -C 4烷氧基，乙酰基，烯丙氧基，氨基甲酰基和氨磺酰基的成员，当两个或更多个 R2基团存在，它们可以相同或不同，n表示1,2或3，m表示1或2，条件是n + m> = 4; 及其酸加成盐; 其制造方法; 和包含上述化合物的药物组合物。

7. 发明授权

US4290954A Tetrahydroxanthone derivatives 失效
标题翻译：四氢呫吨酮衍生物
公开(公告)号：US4290954A
公开(公告)日：1981-09-22
申请号：US89403
申请日：1979-10-30
申请人： Kazuhiro Onogi , Hisashi Kunieda , Kiyoshi Kawamura , Masami Shiratsuchi , Masahiko Nagakura , Naoki Machida, deceased , by Takayasu Miwa, heir
发明人： Kazuhiro Onogi , Hisashi Kunieda , Kiyoshi Kawamura , Masami Shiratsuchi , Masahiko Nagakura , Naoki Machida, deceased , by Takayasu Miwa, heir
IPC分类号： A61K31/35 , A61K31/352 , A61K31/41 , A61K31/495 , A61K31/535 , A61P25/04 , A61P29/00 , A61P37/08 , C07D311/86 , C07D405/04 , C07D405/12 , C07D405/10 , C07D413/10
CPC分类号： C07D311/86
摘要： A tetrahydroxanthone derivative represented by the general formula: ##STR1## wherein R is a hydrogen atom, a hydroxyl, cyano, lower alkyl, lower alkoxy, lower acyloxy, benzoyloxy or tetrazolyl group, or ##STR2## (R.sub.3 is a hydrogen atom, R.sub.4 is a hydrogen atom, a phenyl group which may be optionally substituted, or a tetrazolyl group; or R.sub.3 and R.sub.4 commonly form a ring together with the adjacent nitrogen atom and another nitrogen atom or an oxygen atom); R.sub.1 is a hydrogen or halogen atom, a lower alkyl, cyano, carboxyl or tetrazolyl group, or ##STR3## (R.sub.5 is a hydrogen atom, R.sub.6 is a phenyl group which may be optionally substituted, or a tetrazolyl group; or R.sub.5 and R.sub.6 commonly form a ring together with the adjacent nitrogen atom and an oxygen atom); and R.sub.2 is a hydrogen or halogen atom, or a lower alkyl group; with the proviso that neither R nor R.sub.1 is a hydrogen atom; when R is --CONH.sub.2, R.sub.1 and R.sub.2 are not respectively a hydrogen atom nor a hydrogen or halogen atom, or a lower alkyl group; and R.sub.2 and R.sub.1 are not respectively a hydrogen atom nor a halogen atom or a lower alkyl group. Exhibits anti-allergic, anti-inflammatory, analgesic, inhibitory and asthma-treating activities.
摘要翻译：其中R是氢原子，羟基，氰基，低级烷基，低级烷氧基，低级酰氧基，苯甲酰氧基或四唑基，或者是（R 3是氢原子，R 4 是氢原子，可以被任意取代的苯基或四唑基;或者R3和R4通常与相邻的氮原子和另一个氮原子或氧原子一起形成环）; R 1是氢或卤素原子，低级烷基，氰基，羧基或四唑基，或者R 5是氢原子，R 6是任选被取代的苯基或四唑基;或R 5和R 6 通常与相邻的氮原子和氧原子一起形成环）; 并且R 2是氢或卤原子或低级烷基; 条件是R和R1都不是氢原子; 当R为-CONH 2时，R 1和R 2不分别为氢原子或氢或卤素原子或低级烷基; R2和R1不分别为氢原子或卤素原子或低级烷基。展示抗过敏，抗炎，镇痛，抑制和哮喘治疗活动。

8. 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。

9. 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。

10. 发明授权

US5883092A Pyrimidine derivatives as endothelin antagonists 失效
标题翻译：嘧啶衍生物作为内皮素拮抗剂
公开(公告)号：US5883092A
公开(公告)日：1999-03-16
申请号：US29244
申请日：1998-03-04
申请人： Mitsuteru Hirata , Takeo Deushi , Yoshio Takahashi , Masahiro Tamura , Takeshi Ohshima , Toshiaki Oda , Tetsuya Ishikawa , Hiroyuki Sonoki , Masami Shiratsuchi
发明人： Mitsuteru Hirata , Takeo Deushi , Yoshio Takahashi , Masahiro Tamura , Takeshi Ohshima , Toshiaki Oda , Tetsuya Ishikawa , Hiroyuki Sonoki , Masami Shiratsuchi
IPC分类号： C07D403/04 , A61K31/506 , A61P9/00 , A61P9/12 , C07D213/00 , C07D239/52 , C07D239/545 , C07D295/00 , C07D401/14 , C07D413/04 , A61K31/505 , A61K31/535
CPC分类号： C07D239/52
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 hydroxyl group, a lower alkoxy group, a phenyloxy group which may have a substituent, an aralkyloxy group which may have a substituent, or --NR.sup.2 R.sup.3 ; X represents an oxygen atom or N--R.sup.4 ; m is 2 or 3; and n is 1 or 2 (wherein each of R.sup.2 and R.sup.3, which are identical to or different from each other, represents a hydrogen atom, a hydroxyl group, a lower alkyl group which may have a substituent, a phenyl group which may have a substituent, an aralkyl group which may have a substituent, or a heterocyclic group which may have a substituent; R.sup.4 represents a lower alkyl group, a phenyl group, a formyl group, or a lower alkoxycarbonyl group)!, as well as to a medicine containing the derivative or salt as the active ingredient. The compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.
摘要翻译： PCT No.PCT / JP96 / 02494 Sec。 371日期：1998年3月4日 102（e）1998年3月4日PCT PCT 1996年9月4日PCT公布。公开号WO97 / 09318 日期1997年3月13日本发明涉及下式（1）的嘧啶衍生物或衍生物的盐：其中R1表示羟基，低级烷氧基，苯氧基其可以具有取代基，可以具有取代基的芳烷氧基或-NR2R3; X表示氧原子或N-R4; m为2或3; n为1或2（式中，R2，R3各自相同或不同，表示氢原子，羟基，可具有取代基的低级烷基，可具有取代基的苯基，取代基，可以具有取代基的芳烷基或可以具有取代基的杂环基; R4表示低级烷基，苯基，甲酰基或低级烷氧基羰基）]以及药物含有衍生物或盐作为活性成分。该化合物对具有强烈血管收缩作用的内皮素表现出强烈的结合抑制活性。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。

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