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1. 发明授权

US5420348A Urea derivatives and salts thereof 失效
标题翻译：尿素衍生物及其盐
公开(公告)号：US5420348A
公开(公告)日：1995-05-30
申请号：US086689
申请日：1993-07-02
申请人： Noriki Ito , Koyo Matsuda , Kiyoshi Iwaoka , Yuichi Iizumi
发明人： Noriki Ito , Koyo Matsuda , Kiyoshi Iwaoka , Yuichi Iizumi
IPC分类号： C07C275/28 , C07C275/26
CPC分类号： C07C275/28 , C07C2101/18 , C07C2103/18 , C07C2103/26
摘要： Urea derivatives of the general formula (I) ##STR1## and salts thereof, pharmaceutical compositions containing the same, and methods for producing the same are-disclosed.The urea derivatives of the general formula (I) and salts thereof are novel compounds having the acyl-CoA cholesterol acyltransferase (ACAT) inhibiting activity.
摘要翻译：通式（I）的脲衍生物（Ⅰ）及其盐，含有它们的药物组合物及其制备方法公开。通式（I）的脲衍生物及其盐是具有酰基-CoA胆固醇酰基转移酶（ACAT）抑制活性的新化合物。

2. 发明授权

US5258405A Urea derivatives and salts thereof in method for inhibiting the ACAT enzyme 失效
标题翻译：尿素衍生物及其盐在抑制ACAT酶的方法中
公开(公告)号：US5258405A
公开(公告)日：1993-11-02
申请号：US953755
申请日：1992-09-29
申请人： Noriki Ito , Koyo Matsuda , Kiyoshi Iwaoka
发明人： Noriki Ito , Koyo Matsuda , Kiyoshi Iwaoka
IPC分类号： C07C275/28 , A61K31/17
CPC分类号： C07C275/28 , C07C2101/18 , C07C2103/18 , C07C2103/26
摘要： Urea derivatives of the general formula (I) ##STR1## and salts thereof, pharmaceutical compositions containing the same, and methods for producing the same are disclosed.The urea derivatives of the general formula (I) and salts thereof are novel compounds having the acyl-CoA cholesterol acyltransferase (ACAT) inhibiting activity.
摘要翻译：公开了通式（I）的脲衍生物及其盐，含有它们的药物组合物及其制备方法。通式（I）的脲衍生物及其盐是具有酰基-CoA胆固醇酰基转移酶（ACAT）抑制活性的新化合物。

3. 发明授权

US4960908A Isoflavone derivatives, salts thereof, and oncostatic and immunosuppressive agents 失效
标题翻译：异黄酮衍生物，其盐，保健和免疫抑制剂
公开(公告)号：US4960908A
公开(公告)日：1990-10-02
申请号：US261388
申请日：1988-10-21
申请人： Noriki Ito , Hiroshi Ogawara , Shunichi Watanabe
发明人： Noriki Ito , Hiroshi Ogawara , Shunichi Watanabe
IPC分类号： C07D311/24 , A61K31/35 , A61K31/352 , A61K31/40 , A61K31/425 , A61K31/435 , A61K31/535 , A61P35/00 , A61P37/06 , A61P43/00 , C07D311/36
CPC分类号： C07D311/36
摘要： Novel isoflavone derivatives are provided which have the formula ##STR1## and which exhibit cancerocidal and immunosuppressive activity. The invention also provides pharmaceutical compositions containing the derivatives, methods of use and processes for their preparation.

4. 发明授权

US4727082A Dihydropyridine compounds and pharmaceutical compositions containing them 失效
标题翻译：二氢吡啶化合物和含有它们的药物组合物
公开(公告)号：US4727082A
公开(公告)日：1988-02-23
申请号：US908350
申请日：1986-09-17
申请人： Takashi Fujikura , Noriki Ito , Yuzo Matsumoto , Yasuo Isomura , Masaharu Asano , Toichi Takenaka
发明人： Takashi Fujikura , Noriki Ito , Yuzo Matsumoto , Yasuo Isomura , Masaharu Asano , Toichi Takenaka
IPC分类号： C07D211/82 , A61K31/44 , A61K31/455 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , A61P25/28 , C07D211/90 , C07D401/12
CPC分类号： C07D401/12 , C07C317/00 , C07C323/00 , C07D211/90
摘要： A dihydropyridine compound of the following general formula (I) or a salt thereof: ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, each represents a C.sub.1 to C.sub.10 alkyl group, a lower alkyl group which is interrupted by oxygen atom(s), or a lower alkyl group substituted by C.sub.3 to C.sub.6 alicyclic group(s); R.sup.3 and R.sup.4, which are the same or different, each represents a lower alkyl group; R.sup.5 and R.sup.6, which are the same or different, each represents a hydrogen atom, a nitro group, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkylsulfonyl group, or a lower alkylsulfinyl group; R.sup.7 and R.sup.8, which are the same or different, each represents a hydrogen atom, a halogen atom, a cyano group, a lower alkoxy group, or a lower alkanoylamino group, or R.sup.7 may combine with R.sup.8 to form a naphthyl group together with the adjacent phenyl group; A represents a single bond, a vinylene group (--CH.dbd.CH--), or a ethynylene group (--C.dbd.C--); B represents a single bond or --CH.sub. 2 O--; and m and n, which are the same or different, each represents 0 or an integer of 1 to 5.The compounds are useful for the treatment of various cardiovascular disorders, since they possess both Ca.sup.2+ -antagonistic and adrenergic beta-receptor blocking activities.
摘要翻译：下列通式（I）的二氢吡啶化合物或其盐：其中R 1和R 2相同或不同，各自表示C1至C10烷基，低级烷基其被氧原子或被C3-C6脂环族基团取代的低级烷基取代; R 3和R 4相同或不同，各自表示低级烷基; R 5和R 6相同或不同，分别表示氢原子，硝基，卤素原子，低级烷基，低级烷氧基，低级烷硫基，低级烷基磺酰基或低级烷基亚磺酰基 ; R 7和R 8相同或不同，各自表示氢原子，卤素原子，氰基，低级烷氧基或低级烷酰氨基，或者可以与R 8结合形成萘基，相邻苯基; A表示单键，亚乙烯基（-CH = CH-）或亚乙炔基（-C = C-）; B表示单键或-CH 2 O-; 和m和n相同或不同，各自表示0或1至5的整数。该化合物可用于治疗各种心血管疾病，因为它们具有Ca 2+拮抗剂和肾上腺素能β受体阻断活性。

5. 发明授权

US4186200A Novel fused derivatives of 2-pyridones 失效
标题翻译： 2-吡啶酮的新型融合衍生物
公开(公告)号：US4186200A
公开(公告)日：1980-01-29
申请号：US876517
申请日：1978-02-09
申请人： Kazuo Kubo , Noriki Ito , Isao Souzu , Yasuo Isomura , Hiroshige Homma , Masuo Murakami
发明人： Kazuo Kubo , Noriki Ito , Isao Souzu , Yasuo Isomura , Hiroshige Homma , Masuo Murakami
IPC分类号： A61K31/44 , C07D213/64 , C07D213/74 , C07D213/89 , C07D455/02 , C07D471/04 , C07D498/04 , C07D513/04 , A61K31/415
CPC分类号： C07C255/00 , C07D213/64 , C07D213/89 , C07D471/04 , C07D513/04
摘要： Novel nitrogen-containing heterocyclic compounds shown by the formula ##STR1## wherein one of R.sub.1 and R.sub.2 represents a lower alkyl group, a phenyl group, a halophenyl group, or a lower alkoxyphenyl group and the other of them represents a hydrogen atom, a lower alkyl group, or a phenyl lower alkyl group; said R.sub.1 and R.sub.2 may combine with each other to form a trimethylene group or a tetramethylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, a phenyl group, or a phenyl lower alkyl group; X represents an oxygen atom, a sulfur atom, an imino group, or a group shown by ##STR2## wherein m represents 1 or 2 and R.sub.4 represents a lower alkyl group, a hydroxy lower alkyl group, a cycloalkyl group or a phenyl lower alkyl group; and Y represents an ethylene group which may be substituted by lower alkyl group, a trimethylene group, a tetramethylene group, a vinylene group which may be substituted by a lower alkyl group, or ##STR3## wherein R.sub.5 represents a hydrogen atom, a lower alkyl group, a trifluoromethyl group, or a phenyl group; said X is the group shown by ##STR4##when one of said R.sub.1 and R.sub.2 is a lower alkyl group and the other is a hydrogen atom, and said Y is an ethylene group, and the pharmacologically acceptable non-toxic salts thereof. The compounds described above are strong analgesic anti-inflammatory agents.
摘要翻译：式中，R 1和R 2中的一个表示低级烷基，苯基，卤代苯基或低级烷氧基苯基，另一方表示氢原子，低级烷基或苯基低级烷基; 所述R1和R2可以相互结合形成三亚甲基或四亚甲基; R3表示氢原子，低级烷基，苯基或苯基低级烷基; X表示氧原子，硫原子，亚氨基或由下式表示的基团，其中m表示1或2，R4表示低级烷基，羟基低级烷基，环烷基或苯基低级烷基组; Y表示可以被低级烷基，三亚甲基，四亚甲基，可被低级烷基取代的亚乙烯基取代的亚乙基，或者R5表示氢原子的低级烷基基，三氟甲基或苯基; 说X是所示的组

6. 发明授权

US5227492A Diurea derivatives useful as medicaments and processes for the preparation thereof 失效
标题翻译：用作药物的二脲衍生物及其制备方法
公开(公告)号：US5227492A
公开(公告)日：1993-07-13
申请号：US906735
申请日：1992-06-30
申请人： Noriki Ito , Tomoyuki Yasunaga , Yuichi Iizumi , Tomio Araki
发明人： Noriki Ito , Tomoyuki Yasunaga , Yuichi Iizumi , Tomio Araki
IPC分类号： C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C335/14 , C07D213/75
CPC分类号： C07D213/75 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C335/14 , C07C2101/14 , C07C2101/18
摘要： Diurea derivatives are provided which can be represented by the following general formula and salts thereof: ##STR1## Illustrative derivatives include 1,3-bis[[1-cycloheptyl-3-(3-pyridyl)ureido]-methyl]benzene, 1,3-bis[[1-cycloheptyl-3-(2-pyridyl)ureido]-methyl]benzene, and 1,3-bis[[1-cycloheptyl-3-(4-pyridyl)ureido]-methyl]benzene.The above compounds inhibit acyl-coenzyme A cholesterol acyltransferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester to the smooth muscle of arterial wall in the blood vessel.
摘要翻译：提供二脲衍生物，其可以由以下通式及其盐表示：示例性衍生物包括1,3-双[[1-环庚基-3-（3-吡啶基）脲基] - 甲基]苯，苯，1,3-双[[1-环庚基-3-（4-吡啶基）脲基] - 甲基]苯。上述化合物抑制酰基辅酶A胆固醇酰基转移酶（ACAT酶），从而控制胆固醇酯对血管中动脉壁平滑肌的积累。

7. 发明授权

US5110820A Dihydropyridine compounds which process both calcium (2+)-antagonistic and beta receptor blocking activities 失效
标题翻译：二钙二氢化合物（2 +） - 拮抗剂和受体阻断活性
公开(公告)号：US5110820A
公开(公告)日：1992-05-05
申请号：US611340
申请日：1990-11-13
申请人： Takashi Fujikura , Noriki Ito , Yuzo Matsumoto , Masaharu Asano , Toichi Takenaka
发明人： Takashi Fujikura , Noriki Ito , Yuzo Matsumoto , Masaharu Asano , Toichi Takenaka
IPC分类号： A61K31/4427 , A61K31/455 , A61P3/00 , A61P3/14 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , C07D211/90 , C07D401/12
CPC分类号： C07D401/12 , C07D211/90
摘要： Dihydropyridine compounds and salts thereof are provided which exhibit both Ca.sup.2+ -antagonistic and adrenergic beta-receptor blocking activities and therefore are useful for the treatment of ischemic heart diseases and hypertension. The compounds have the formula ##STR1## wherein A represents a straight or branched carbon chain alkylene group having 1 to 10 carbon atoms which may be interrupted by an oxygen atom(s); R.sup.1 and R.sup.4, which may be the same or different, each represents a lower alkyl group; R.sup.2 represents an amino group, ##STR2## R.sup.3 represents a straight or branched carbon chain alkyl group having 1 to 10 carbon atoms which may be interrupted by an oxygen atom(s), or ##STR3## R.sup.5 and R.sup.6, which may be the same or different, each represents a hydrogen atom, a nitro group, a halogen atom, a trifluoromethyl group, a cyano group, a lower alkyl group, a lower alkoxy group or a lower alkenyloxy group; R.sup.7 represents a hydrogen atom, a cyano group, a halogen atom, a lower alkoxy group or a lower alkanoyl group; R.sup.8 and R.sup.9, which may be the same or different, each represents a lower alkyl group or an aralkyl group; and n represents an integer of 1 to 2: these symbols, hereafter, have the same significances.
摘要翻译：提供二氢吡啶化合物及其盐，其表现出Ca 2+ +拮抗性和肾上腺素能β受体阻断活性，因此可用于治疗缺血性心脏病和高血压。化合物具有式（I）的化合物，其中A表示可被氧原子间隔的具有1-10个碳原子的直链或支链碳链亚烷基; R 1和R 4可以相同或不同，各自表示低级烷基; R 2表示氨基，R 3表示可被氧原子间隔的具有1〜10个碳原子的直链或支链碳链烷基，或者R 5和R 6 可以相同或不同，分别表示氢原子，硝基，卤素原子，三氟甲基，氰基，低级烷基，低级烷氧基或低级链烯氧基。 R7表示氢原子，氰基，卤素原子，低级烷氧基或低级烷酰基; R 8和R 9可以相同或不同，各自表示低级烷基或芳烷基; n表示1〜2的整数，以下，符号相同。

8. 发明授权

US4251533A Nitrogen-containing heterocyclic compounds 失效
标题翻译：含氮杂环化合物
公开(公告)号：US4251533A
公开(公告)日：1981-02-17
申请号：US67918
申请日：1979-08-20
申请人： Kazuo Kubo , Noriki Ito , Isao Souzu , Yasuo Isomura , Hiroshige Homma , Masuo Murakami
发明人： Kazuo Kubo , Noriki Ito , Isao Souzu , Yasuo Isomura , Hiroshige Homma , Masuo Murakami
IPC分类号： A61K31/44 , C07D213/64 , C07D213/74 , C07D213/89 , C07D455/02 , C07D471/04 , C07D498/04 , C07D513/04 , A61K31/435 , C07D471/02
CPC分类号： C07C255/00 , C07D213/64 , C07D213/89 , C07D471/04 , C07D513/04
摘要： Novel nitrogen-containing heterocyclic compounds shown by the formula ##STR1## wherein one of R.sub.1 and R.sub.2 represents a lower alkyl group, a phenyl group, a halophenyl group, or a lower alkoxyphenyl group and the other of them represents a hydrogen atom, a lower alkyl group, or a phenyl lower alkyl group; said R.sub.1 and R.sub.2 may combine with each other to form a trimethylene group or a tetramethylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, a phenyl group, or a phenyl lower alkyl group; X represents an oxygen atom, a sulfur atom, an imino group, or a group shown by ##STR2## wherein m represents 1 or 2 and R.sub.4 represents a lower alkyl group, a hydroxy lower alkyl group, a cycloalkyl group or a phenyl lower alkyl group; and Y represents an ethylene group which may be substituted by lower alkyl group, a trimethylene group, a tetramethylene group, a vinylene group which may be substituted by a lower alkyl group, or ##STR3## wherein R.sub.5 represents a hydrogen atom, a lower alkyl group, a trifluoromethyl group, or a phenyl group; said X is the group shown by ##STR4## when one of said R.sub.1 and R.sub.2 is a lower alkyl group and the other is a hydrogen atom, and said Y is an ethylene group, 1/7and the pharmacologically acceptable non-toxic salts thereof.The compounds described above are strong analgesic anti-inflammatory agents.
摘要翻译：式中，R 1和R 2中的一个表示低级烷基，苯基，卤代苯基或低级烷氧基苯基，另一方表示氢原子，低级烷基或苯基低级烷基; 所述R1和R2可以相互结合形成三亚甲基或四亚甲基; R3表示氢原子，低级烷基，苯基或苯基低级烷基; X表示氧原子，硫原子，亚氨基或由下式表示的基团，其中m表示1或2，R4表示低级烷基，羟基低级烷基，环烷基或苯基低级烷基组; Y表示可以被低级烷基，三亚甲基，四亚甲基，可被低级烷基取代的亚乙烯基取代的亚乙基，或者R5表示氢原子的低级烷基基，三氟甲基或苯基; 当所述R 1和R 2中的一个为低级烷基且另一个为氢原子，所述Y为亚乙基时，X为所示的基团，其药理学上可接受的无毒性盐。上述化合物是强镇痛抗炎剂。

9. 发明授权

US4198512A 1-Oxo-1,2-dihydroisoquinoline derivatives 失效
标题翻译： 1-氧代-1,2-二氢异喹啉衍生物
公开(公告)号：US4198512A
公开(公告)日：1980-04-15
申请号：US925217
申请日：1978-07-17
申请人： Kazuo Kubo , Noriki Ito , Isao Souzu , Yasuo Isomura , Hiroshige Homma
发明人： Kazuo Kubo , Noriki Ito , Isao Souzu , Yasuo Isomura , Hiroshige Homma
IPC分类号： A61K31/47 , A61K31/472 , A61P25/04 , A61P29/00 , C07D217/24
CPC分类号： C07D217/24
摘要： Novel 1-oxo-1,2-dihydroisoquinoline compounds of the formula ##STR1## wherein R.sub.1 represents a lower alkyl group or a phenyl lower alkyl group; R.sub.2 represents a lower alkyl group; R.sub.3 represents a hydrogen atom, a lower alkanoyl group, a lower alkyl group or a hydroxy lower alkyl group; and n is 0, 1 or 2 and the pharmacologically acceptable non-toxic salts thereof.The compounds of this invention are strong analgesic anti-inflammatory agents.
摘要翻译：新颖的式Ⅰ-1-氧代-1,2-二氢异喹啉化合物，其中R1代表低级烷基或苯基低级烷基; R2表示低级烷基; R3表示氢原子，低级烷酰基，低级烷基或羟基低级烷基; 和n为0,1或2及其药理学上可接受的无毒盐。本发明的化合物是强镇痛抗炎剂。

10. 发明授权

US5384425A Diurea derivatives useful as medicaments and processes for the preparation thereof 失效
标题翻译：用作药物的二脲衍生物及其制备方法
公开(公告)号：US5384425A
公开(公告)日：1995-01-24
申请号：US64850
申请日：1993-10-07
申请人： Noriki Ito , Tomoyuki Yasunaga , Yuichi Iizumi , Tomio Araki
发明人： Noriki Ito , Tomoyuki Yasunaga , Yuichi Iizumi , Tomio Araki
IPC分类号： C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C335/14 , C07D213/75 , C07C69/017
CPC分类号： C07D213/75 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C335/14 , C07C2101/14 , C07C2101/18
摘要： Diurea derivatives are provided which can be represented by the following general formula and salts thereof: ##STR1## wherein, R.sup.1 and R.sup.2 are the same or different, and each represents C.sup.1 -10 alkyl group, a C.sup.3 -18 cycloalkyl group, or a lower alkyl group substituted by cycloalkyl radical(s);R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different, and each represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, hydrocarbyl aralkyl group, a pyridyl group, or an unsubstituted or substituted phenyl group, the substituents of the phenyl group being selected from a group consisting of lower alkyl radical, halogen atom-substituted lower alkyl radical, halogen atom, nitro radical, amino radical, mono- or di-lower alkylamino radical, lower acylamino radical, hydroxyl radical, lower alkoxy radical and lower acyloxy radical;X represents an oxygen atom or a sulfur atom, and n.sup.1 and n.sup.2 represent an integer of 1 to 6; and wherein at least one of R.sup.3 -R.sup.6 is a phenyl substituted by acyloxy.
摘要翻译：提供了可由以下通式表示的二脲衍生物及其盐：其中，R 1和R 2相同或不同，各自表示C 1-10烷基，C 3-18环烷基或低级被环烷基取代的烷基; R 3，R 4，R 5和R 6相同或不同，各自表示氢原子，低级烷基，环烷基，烃基芳烷基，吡啶基或未取代或取代的苯基，苯基基团选自低级烷基，卤素原子取代的低级烷基，卤原子，硝基，氨基，一或二低级烷基氨基，低级酰基氨基，羟基，低级烷氧基和低级烷基酰氧基; X表示氧原子或硫原子，n1和n2表示1〜6的整数，并且其中R 3 -R 6中的至少一个是被酰氧基取代的苯基。

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