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1. 发明授权

US07393866B2 Amide compounds and medications containing the same 失效
标题翻译：酰胺化合物和含有相同的药物
公开(公告)号：US07393866B2
公开(公告)日：2008-07-01
申请号：US10985938
申请日：2004-11-09
申请人： Kimiyuki Shibuya , Toru Miura , Katsumi Kawamine , Yukihiro Sato , Tadaaki Ohgiya , Takahiro Kitamura , Chiyoka Ozaki , Toshiyuki Edano , Mitsuteru Hirata
发明人： Kimiyuki Shibuya , Toru Miura , Katsumi Kawamine , Yukihiro Sato , Tadaaki Ohgiya , Takahiro Kitamura , Chiyoka Ozaki , Toshiyuki Edano , Mitsuteru Hirata
IPC分类号： A61K31/4436 , C07D417/12
CPC分类号： C07D403/12 , A61K31/4439 , C07D401/12 , C07D413/12 , C07D417/12 , C07D513/04
摘要： The present invention provides to a novel compound having an ACAT inhibiting activity.The present invention relates to compounds represented by formula (I) wherein represents an optionally substituted divalent residue such as benzene, pyridine, cyclohexane or naphthalene, or a group, Het represents a 5- to 8-membered, substituted or unsubstituted heterocyclic group containing at least one heteroatom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, such as a monocyclic group, a polycyclic group or a group of a fused ring, X represents —NH—, an oxygen atom or a sulfur atom, Y represents —NR4—, an oxygen atom, a sulfur atom, a sulfoxide or a sulfone, Z represents a single bond or —NR5—, R4 represents a hydrogen atom, a lower alkyl group, an aryl group or an optionally substituted silyl lower alkyl group, R5 represents a hydrogen atom, a lower alkyl group, an aryl group or an optionally substituted silyl lower alkyl group, and n is an integer of from 1 to 15, or salts or solvates thereof, and a pharmaceutical composition containing at least one of these compounds.
摘要翻译：本发明提供具有ACAT抑制活性的新型化合物。本发明涉及由式（I）表示的化合物，其中表示任选取代的二价残基例如苯，吡啶，环己烷或萘，或者基团，Het表示5至8元，取代或未取代的杂环基，至少一个选自氮原子，氧原子和硫原子的杂原子，如单环基团，多环基团或稠环基团，X表示-NH-，氧原子或硫原子原子，Y表示-NR 4 - ，氧原子，硫原子，亚砜或砜，Z表示单键或-NR 5 - ， - R 4表示氢原子，低级烷基，芳基或任选取代的甲硅烷基低级烷基，R 5表示氢原子，低级烷基，芳基基团或任选取代的甲硅烷基低级烷基，n为1至15的整数，或其盐或溶剂化物， d含有这些化合物中的至少一种的药物组合物。

2. 发明授权

US06969711B2 Cyclic diamine compounds and medicine containing the same 失效
标题翻译：环状二胺化合物和含有相同的药物
公开(公告)号：US06969711B2
公开(公告)日：2005-11-29
申请号：US10371234
申请日：2003-02-20
申请人： Kimiyuki Shibuya , Katsumi Kawamine , Yukihiro Sato , Toru Miura , Chiyoka Ozaki , Toshiyuki Edano , Mitsuteru Hirata , Tadaaki Ohgiya
发明人： Kimiyuki Shibuya , Katsumi Kawamine , Yukihiro Sato , Toru Miura , Chiyoka Ozaki , Toshiyuki Edano , Mitsuteru Hirata , Tadaaki Ohgiya
IPC分类号： C07D235/28 , C07D263/58 , C07D277/74 , C07D401/12 , C07D413/12 , C07D417/12 , C07D498/04 , C07F9/6509 , C07F9/6558 , C07D403/12 , A61K31/454 , A61P9/10
CPC分类号： C07D263/58 , C07D235/28 , C07D277/74 , C07D401/12 , C07D413/12 , C07D417/12 , C07F9/650952 , C07F9/65583
摘要： The present invention offers novel cyclic diamine compounds and a pharmaceutical composition containing the same.The present invention relates to a compound represented by the formula (I) or salt(s) or solvate(s) thereof. (In the formula, is an optionally substituted divalent residue of benzene, pyridine, cyclohexane or naphthalene or is a vinylene group where Ar is an optionally substituted aryl group; X is —NH—, oxygen atom or sulfur atom; Y is —NR1—, oxygen atom, sulfur atom, sulfoxide or sulfone; Z is a single bond or —NR2—; R1 is hydrogen atom, optionally substituted lower alkyl group, optionally substituted aryl group or optionally substituted silyl lower alkyl group; R2 is hydrogen atom, optionally substituted lower alkyl group, optionally substituted aryl group or optionally substituted silyl lower alkyl group; l is an integer of from 0 to 15; m is an integer of 2 or 3; and n is an integer of from 0 to 3). The compound of the present invention is useful as a pharmaceutical composition, particuarly as an inhibitor of acyl coenzyme A cholesterol acyltransferase (ACAT).
摘要翻译：本发明提供新的环状二胺化合物和含有它们的药物组合物。本发明涉及由式（I）表示的化合物或其盐或溶剂化物。（式中，是苯，吡啶，环己烷或萘的任选取代的二价残基，或者是亚乙烯基，其中Ar是任意取代的芳基; X是-NH-，氧原子或硫原子; Y是-NR' SO 2， - 氧原子，硫原子，亚砜或砜; Z是单键或-NR 2 - ; R 1是氢原子，任选取代的低级烷基，任选取代的芳基或任选取代的甲硅烷基低级烷基; R 2是氢原子，任选取代的低级烷基，任选取代的芳基或任选取代的甲硅烷基低级烷基; l 为0〜15的整数，m为2或3的整数，n为0〜3的整数。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）的抑制剂。

3. 发明授权

US4746737A Phenyl guanidinobenzoate derivatives which have protease inhibitory activity 失效
标题翻译：具有蛋白酶抑制活性的苯胍基苯甲酸酯衍生物
公开(公告)号：US4746737A
公开(公告)日：1988-05-24
申请号：US886046
申请日：1986-07-16
申请人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Koichiro Watanabe , Tomio Ohta , Nobuo Yokoo , Masahiko Nagakura
发明人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Koichiro Watanabe , Tomio Ohta , Nobuo Yokoo , Masahiko Nagakura
IPC分类号： C07C279/18 , C07D207/16 , C07D207/26 , C07D207/27 , C07D243/08 , C07D295/185 , C07D265/30
CPC分类号： C07D207/27 , C07C279/18 , C07D207/16 , C07D243/08 , C07D295/185
摘要： Novel benzoyl esters of the following formula (I), and acid addition salts thereof, ##STR1## in which R.sub.1 and R.sub.2 are the same or different and represent a hydrogen atom or a lower alkoxy group, A represents a single bond, a linear or branched lower alkylene group, a lower alkenylene group, R.sub.3 and R.sub.4 are the same or different and represent a hydrogen atom or a lower alkyl group, or R.sub.3 and R.sub.4 join together to form a lower alkylene group, R.sub.5 represents a group of the formula, --X--(CO).sub.n --Y in which X represents a single bond, a linear or branched lower alkylene group or an alkenylene group, n is 0 or 1, Y represents a hydrogen atom, a cycloalkyl group, an aryl group, a hydroxyl group, a lower alkoxy group and the like are prepared by reacting para-nitrobenzoic acid or its derivative with a compound of the general formula (III) or its derivative ##STR2## to obtain a compound of the general formula (IV) ##STR3## followed by reducing the compound of the formula (IX) ##STR4## and subjecting the compound (IX) to guanidylation reaction, or by reaction para-guanidinobenzoic derivative with compound (III) or its derivative.The benzoyl esters have strong anti-trypsin activity, anti-thrombin activity and anticoagulant activity with low toxicity and are useful as a medicine for treatment of pancreatitis and disseminated intravascular coagulation (DIC).
摘要翻译：下式（I）的新型苯甲酰基酯及其酸加成盐，其中R 1和R 2相同或不同，表示氢原子或低级烷氧基，A表示单键，直链或支链低级亚烷基，低级亚烯基，R3和R4相同或不同，表示氢原子或低级烷基，或R3和R4连接在一起形成低级亚烷基，R5表示其中X表示单键的-X-（CO）nY，直链或支链低级亚烷基或亚烯基，n为0或1，Y表示氢原子，环烷基，芳基，通过使对硝基苯甲酸或其衍生物与通式（III）的化合物或其衍生物（IMAGE）（III）反应来制备羟基，低级烷氧基等，以获得通式（III）的化合物（Ⅳ），然后还原式（Ⅸ）化合物（IX）和使化合物（IX）进行胍基化反应，或通过反应对 - 胍基苯甲酸衍生物与化合物（III）或其衍生物反应。苯甲酰酯具有很强的抗胰蛋白酶活性，抗凝血酶活性和抗凝血活性，毒性低，可用作治疗胰腺炎和弥散性血管内凝血（DIC）的药物。

4. 发明授权

US06849647B1 Amide compounds and medications containing the same technical field 失效
标题翻译：酰胺化合物和含有相同技术领域的药物
公开(公告)号：US06849647B1
公开(公告)日：2005-02-01
申请号：US09666152
申请日：2000-09-20
申请人： Kimiyuki Shibuya , Toru Miura , Katsumi Kawamine , Yukihiro Sato , Tadaaki Ohgiya , Takahiro Kitamura , Chiyoka Ozaki , Toshiyuki Edano , Mitsuteru Hirata
发明人： Kimiyuki Shibuya , Toru Miura , Katsumi Kawamine , Yukihiro Sato , Tadaaki Ohgiya , Takahiro Kitamura , Chiyoka Ozaki , Toshiyuki Edano , Mitsuteru Hirata
IPC分类号： A61K31/4439 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D498/04 , C07D513/04
CPC分类号： C07D403/12 , A61K31/4439 , C07D401/12 , C07D413/12 , C07D417/12 , C07D513/04
摘要： The present invention provides to a novel compound having an ACAT inhibiting activity.The present invention relates to compounds represented by formula (I) wherein represents an optionally substituted divalent residue such as benzene, pyridine, cyclohexane or naphthalene, or a group, Het represents a 5- to 8-membered, substituted or unsubstituted heterocyclic group containing at least one heteroatom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, such as a monocyclic group, a polycyclic group or a group of a fused ring, X represents —NH—, an oxygen atom or a sulfur atom, Y represents —NR4—, an oxygen atom, a sulfur atom, a sulfoxide or a sulfone, Z represents a single bond or —NR5—, R4 represents a hydrogen atom, a lower alkyl group, an aryl group or an optionally substituted silyl lower alkyl group, R5 represents a hydrogen atom, a lower alkyl group, an aryl group or an optionally substituted silyl lower alkyl group, and n is integer of from 1 to 15, or salts or solvates thereof, and a pharmaceutical composition containing at one of these compounds.
摘要翻译：本发明涉及一种具有ACAT抑制活性的新型化合物。本发明涉及式（I）表示的化合物，其中表示任选取代的二价残基如苯，吡啶，环己烷或萘，或基团，Het表示含有至少一个选自氮原子，氧原子和硫原子的杂原子的5-至8-元，取代或未取代的杂环基，例如单环基团，多环基团或稠合基团环，X表示-NH-，氧原子或硫原子，Y表示-NR4-，氧原子，硫原子，亚砜或砜，Z表示单键或-NR5-，R4表示氢原子，低级烷基，芳基或任选取代的甲硅烷基低级烷基，R 5表示氢原子，低级烷基，芳基或任选取代的甲硅烷基低级烷基，n为1至15的整数，要么盐或溶剂合物，以及含有这些化合物之一的药物组合物。

5. 发明授权

US06337334B1 Pyrimidine derivatives 失效
标题翻译：嘧啶衍生物
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。

6. 发明授权

US07414066B2 Amide compounds and medications containing the same technical field 失效
标题翻译：酰胺化合物和含有相同技术领域的药物
公开(公告)号：US07414066B2
公开(公告)日：2008-08-19
申请号：US10985915
申请日：2004-11-09
申请人： Kimiyuki Shibuya , Toru Miura , Katsumi Kawamine , Yukihiro Sato , Tadaaki Ohgiya , Takahiro Kitamura , Chiyoka Ozaki , Toshiyuki Edano , Mitsuteru Hirata
发明人： Kimiyuki Shibuya , Toru Miura , Katsumi Kawamine , Yukihiro Sato , Tadaaki Ohgiya , Takahiro Kitamura , Chiyoka Ozaki , Toshiyuki Edano , Mitsuteru Hirata
IPC分类号： A61K31/4439 , C07D401/12
CPC分类号： C07D403/12 , A61K31/4439 , C07D401/12 , C07D413/12 , C07D417/12 , C07D513/04
摘要： The present invention provides to a novel compound having an ACAT inhibiting activity.The present invention relates to compounds represented by formula (I) wherein represents an optionally substituted divalent residue such as benzene, pyridine, cyclohexane or naphthalene, or a group, Het represents a 5- to 8-membered, substituted or unsubstituted heterocyclic group containing at least one heteroatom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, such as a monocyclic group, a polycyclic group or a group of a fused ring, X represents —NH—, an oxygen atom or a sulfur atom, Y represents —NR4—, an oxygen atom, a sulfur atom, a sulfoxide or a sulfone, Z represents a single bond or —NR5—, R4 represents a hydrogen atom, a lower alkyl group, an aryl group or an optionally substituted silyl lower alkyl group, R5 represents a hydrogen atom, a lower alkyl group, an aryl group or an optionally substituted silyl lower alkyl group, and n is an integer of from 1 to 15, or salts or solvates thereof, and a pharmaceutical composition containing at least one of these compounds.
摘要翻译：本发明提供具有ACAT抑制活性的新型化合物。本发明涉及由式（I）表示的化合物，其中表示任选取代的二价残基例如苯，吡啶，环己烷或萘，或者基团，Het表示5至8元，取代或未取代的杂环基，至少一个选自氮原子，氧原子和硫原子的杂原子，如单环基团，多环基团或稠环基团，X表示-NH-，氧原子或硫原子原子，Y表示-NR 4 - ，氧原子，硫原子，亚砜或砜，Z表示单键或-NR 5 - ， - R 4表示氢原子，低级烷基，芳基或任选取代的甲硅烷基低级烷基，R 5表示氢原子，低级烷基，芳基基团或任选取代的甲硅烷基低级烷基，n为1至15的整数，或其盐或溶剂化物， d含有这些化合物中的至少一种的药物组合物。

7. 发明申请

US20050131002A1 Novel amide compounds and medications containing the same 失效
标题翻译：新颖的酰胺化合物和含有相同的药物
公开(公告)号：US20050131002A1
公开(公告)日：2005-06-16
申请号：US10985938
申请日：2004-11-09
申请人： Kimiyuki Shibuya , Toru Miura , Katsumi Kawamine , Yukihiro Sato , Tadaaki Ohgiya , Takahiro Kitamura , Chiyoka Ozaki , Toshiyuki Edano , Mitsuteru Hirata
发明人： Kimiyuki Shibuya , Toru Miura , Katsumi Kawamine , Yukihiro Sato , Tadaaki Ohgiya , Takahiro Kitamura , Chiyoka Ozaki , Toshiyuki Edano , Mitsuteru Hirata
IPC分类号： A61K31/4439 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D498/04 , C07D513/04 , A61K31/506 , C07D413/02 , C07D417/02 , C07D43/02
CPC分类号： C07D403/12 , A61K31/4439 , C07D401/12 , C07D413/12 , C07D417/12 , C07D513/04
摘要： The present invention provides to a novel compound having an ACAT inhibiting activity. The present invention relates to compounds represented by formula (I) wherein represents an optionally substituted divalent residue such as benzene, pyridine, cyclohexane or naphthalene, or a group, Het represents a 5- to 8-membered, substituted or unsubstituted heterocyclic group containing at least one heteroatom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, such as a monocyclic group, a polycyclic group or a group of a fused ring, X represents —NH—, an oxygen atom or a sulfur atom, Y represents —NR4—, an oxygen atom, a sulfur atom, a sulfoxide or a sulfone, Z represents a single bond or —NR5—, R4 represents a hydrogen atom, a lower alkyl group, an aryl group or an optionally substituted silyl lower alkyl group, R5 represents a hydrogen atom, a lower alkyl group, an aryl group or an optionally substituted silyl lower alkyl group, and n is an integer of from 1 to 15, or salts or solvates thereof, and a pharmaceutical composition containing at least one of these compounds.
摘要翻译：本发明提供具有ACAT抑制活性的新型化合物。本发明涉及由式（I）表示的化合物，其中表示任选取代的二价残基例如苯，吡啶，环己烷或萘，或者基团，Het表示5至8元，取代或未取代的杂环基，至少一个选自氮原子，氧原子和硫原子的杂原子，如单环基团，多环基团或稠环基团，X表示-NH-，氧原子或硫原子原子，Y表示-NR 4 - ，氧原子，硫原子，亚砜或砜，Z表示单键或-NR 5 - ， - R 4表示氢原子，低级烷基，芳基或任选取代的甲硅烷基低级烷基，R 5表示氢原子，低级烷基，芳基基团或任选取代的甲硅烷基低级烷基，n为1至15的整数，或其盐或溶剂化物， d含有这些化合物中的至少一种的药物组合物。

8. 发明授权

US06797717B2 Anilide compounds and drugs containing the same 失效
标题翻译：苯胺类化合物和含有相同的药物
公开(公告)号：US06797717B2
公开(公告)日：2004-09-28
申请号：US10034669
申请日：2001-12-19
申请人： Kimiyuki Shibuya , Katsumi Kawamine , Yukihiro Sato , Toshiyuki Edano , Mitsuteru Hirata , Chiyoka Ozaki
发明人： Kimiyuki Shibuya , Katsumi Kawamine , Yukihiro Sato , Toshiyuki Edano , Mitsuteru Hirata , Chiyoka Ozaki
IPC分类号： A61K31435
CPC分类号： C07D263/58 , C07D233/84 , C07D235/28 , C07D263/60 , C07D277/74 , C07D413/04 , C07D413/12 , C07D471/04
摘要： The invention relates to a novel anilide compound and a pharmaceutical composition comprising the same. The invention relates to a compound represented by the following general formula: represents a divalent residue of benzene with a substituent(s), heterocycle-condensed benzene which may or may not have a substituent, pyridine which may or may not have a substituent, cyclohexane or naphthalene Ar represents an aryl group which may or may not have a substituent, X represents —NH—, oxygen atom or sulfur atom; Y represents —NR4—, oxygen atom, sulfur atom, sulfoxide or sulfone; Z represents single bond or —NR5—; R4 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; R5 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; and n represents an integer of 0 to 15. The inventive compounds are useful in the form of pharmaceutical composition, specifically as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitor.
摘要翻译：本发明涉及一种新的酰苯胺化合物和包含其的药物组合物。本发明涉及由以下通式表示的化合物：表示具有取代基的苯的二价残基，可以具有也可以不具有取代基的杂环稠合苯，可以具有也可以不具有取代基的吡啶，可以不具有取代基的吡啶，环己烷或萘Ar表示可以具有或不具有取代基的芳基，X表示-NH-，氧原子或硫原子; Y表示-NR4-，氧原子，硫原子，亚砜或砜; Z表示单键或-NR5 - ; R4表示氢原子，可以具有或不具有取代基的低级烷基，芳基或甲硅烷基化低级烷基; R5表示氢原子，低级烷基，芳基或甲硅烷基化的低级烷基，可以或可以不具有取代基; andn表示0至15的整数。本发明化合物可以药物组合物的形式使用，特别是作为酰基辅酶A胆固醇酰基转移酶（ACAT）抑制剂。

9. 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。

10. 发明授权

US4898876A Benzoylpiperazine esters and a process for their production 失效
标题翻译：苯甲酰哌嗪酯及其制备方法
公开(公告)号：US4898876A
公开(公告)日：1990-02-06
申请号：US796525
申请日：1985-11-12
申请人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Koichiro Watanabe , Kazuhiro Onogi , Masahiko Nagakura
发明人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Koichiro Watanabe , Kazuhiro Onogi , Masahiko Nagakura
IPC分类号： C07D209/48 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D237/28 , C07D241/44 , C07D261/18 , C07D295/192 , C07D307/79 , C07D307/84 , C07D307/86 , C07D311/12 , C07D311/58 , C07D311/84 , C07D317/68 , C07D319/18 , C07D333/54 , C07D333/60
CPC分类号： C07D209/48 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D237/28 , C07D241/44 , C07D261/18 , C07D295/192 , C07D307/79 , C07D307/84 , C07D307/86 , C07D311/12 , C07D311/58 , C07D311/84 , C07D317/68 , C07D319/18 , C07D333/54 , C07D333/60
摘要： A benzopylpiperazine ester of the following formula: ##STR1## wherein A represents a single bond or an alkylene group, vinylene group, --O--alkylene group or methine group, R.sub.1 represents a bicyclic carbon ring residue which may be substituted with a lower alkyl group, lower alkoxy group, oxo group or nitro group or a halogen atom, or may be partially saturated; a fluorene residue which may contain an oxo group; a fluorenylidene group; an anthracene residue; a phenanthrene residue which may be substituted with a lower alkyl group, or may be partially saturated; a benzofuran residue or thianaphthene residue which may be substituted with a lower alkyl group or lower alkoxy group; a benzopyran residue or benzoazine residue which may be substituted with an oxo group or phenyl group and partially saturated; a phthalimide residue; a benzodiazine residue; an isozazole residue which may be substituted with a lower alkyl group or phenyl group; or an alkylene dioxybenzene residue or xanthene residue; and R.sub.2 represents an alkyl group, cycloalkyl group, cycloalkylalkyl group or aralkyl group, excepting the case where A is a single bond, R.sub.1 is ##STR2## and R.sub.2 is a methyl group, exhibits excellent chymotrypsin inhibitive activity.
摘要翻译：下式的苯甲酰基哌嗪酯：其中A表示单键或亚烷基，亚乙烯基，-O-亚烷基或次甲基，R 1表示可被低级烷基取代的双环碳环残基，低级烷氧基，氧代基或硝基或卤素原子，或可部分饱和; 可含有氧代基的芴残基; 亚芴基; 蒽残基; 可以被低级烷基取代的菲残基，或可以部分饱和; 可以被低级烷基或低级烷氧基取代的苯并呋喃残基或硫杂残基; 可被氧代基或苯基取代并部分饱和的苯并吡喃残基或苯并嗪残基; 邻苯二甲酰亚胺残基; 苯并二氮残基; 可以被低级烷基或苯基取代的异唑残基; 或亚烷基二氧基苯残基或呫吨残基; 除了A为单键，R 1为甲基，R 2为甲基的情况外，R 2表示烷基，环烷基，环烷基烷基或芳烷基，表现出优异的糜蛋白酶抑制活性。

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