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1. 发明授权

US5922767A Substituted benzylurea derivatives and medicine containing the same 失效
标题翻译：取代的苄基脲衍生物和含有它们的药物
公开(公告)号：US5922767A
公开(公告)日：1999-07-13
申请号：US946098
申请日：1997-10-07
申请人： Yoshihiko Kanamaru , Hiroyuki Hirota , Akihiro Shibata , Teruo Komoto , Hiroyuki Naito , Koichi Tachibana , Mari Ohtsuka , Fumio Ishii , Susumu Sato
发明人： Yoshihiko Kanamaru , Hiroyuki Hirota , Akihiro Shibata , Teruo Komoto , Hiroyuki Naito , Koichi Tachibana , Mari Ohtsuka , Fumio Ishii , Susumu Sato
IPC分类号： C07C275/28 , C07D213/30 , C07D307/42 , C07D333/16 , A61K31/17 , C07C275/06
CPC分类号： C07D213/30 , C07C275/28 , C07D307/42 , C07D333/16
摘要： Disclosed herein are substituted benzylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 are independently H, a halogen atom, or an alkyl or alkoxyl group, R.sup.3 is a phenyl or heterocyclic group which may be substituted, n is an integer of 1-6, and R.sup.4 is a phenyl group which may be substituted, or salts thereof, and medicines comprising such a derivative as an active ingredient. The derivatives or salts thereof strongly inhibit only ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.
摘要翻译：本文公开了由以下通式（1）表示的取代的苄基脲衍生物：其中R 1和R 2独立地为H，卤素原子或烷基或烷氧基，R 3为可被取代的苯基或杂环基，n为 1-6的整数，R4是可被取代的苯基或其盐，以及包含这种衍生物作为活性成分的药物。其衍生物或盐在巨噬细胞中仅强烈地抑制ACAT，因此可用作动脉硬化的预防和治疗剂。

2. 发明授权

US5532371A Piperazine substituted carboxylic acid derivatives for treating hyperlipimia 失效
标题翻译：哌嗪取代的羧酸衍生物用于治疗高脂血症
公开(公告)号：US5532371A
公开(公告)日：1996-07-02
申请号：US377965
申请日：1995-01-25
申请人： Teruo Komoto , Hiroyuki Hirota , Susumu Sato , Mari Ohtsuka , Hidehiko Koya , Hiroyuki Mizuno , Tadayuki Kuraishi
发明人： Teruo Komoto , Hiroyuki Hirota , Susumu Sato , Mari Ohtsuka , Hidehiko Koya , Hiroyuki Mizuno , Tadayuki Kuraishi
IPC分类号： C07D211/22 , C07D211/52 , C07D211/70 , C07D213/82 , C07D295/192 , C07D333/38 , C07D401/06 , C07D405/06 , C07D409/06 , C07D401/10
CPC分类号： C07D213/82 , C07D211/22 , C07D211/52 , C07D211/70 , C07D295/192 , C07D333/38 , C07D401/06 , C07D405/06 , C07D409/06
摘要： An arylamide derivative of formula (1), a salt thereof and a therapeutic agent for hyperlipemia which comprises the derivative or salt: ##STR1## wherein Ar represents a group ##STR2## a naphthyl group, a pyridinyl group, a furyl group, a thienyl group, a quinolyl group or an indolyl group; Y represents a group ##STR3## and Q represents --O-- or a single bond, Z represents an alkylene group, and R.sup.4 represents a hydroxyl group, an alkoxy group or a group --NH(CH.sub.2).sub.m COOH.
摘要翻译：式（1）的芳基酰胺衍生物，其盐和含有该衍生物或盐的高脂血症治疗剂：其中Ar表示基团，萘基，吡啶基，呋喃基噻吩基，喹啉基或吲哚基; Y表示基团，Q表示-O-或单键，Z表示亚烷基，R4表示羟基，烷氧基或基团-NH（CH2）mCOOH。

3. 发明授权

US5411972A Arylamide derivatives for treating hyperlipemia 失效
标题翻译：用于治疗高脂血症的芳酰胺衍生物
公开(公告)号：US5411972A
公开(公告)日：1995-05-02
申请号：US158398
申请日：1993-11-29
申请人： Teruo Komoto , Hiroyuki Hirota , Susumu Sato , Mari Ohtsuka , Hidehiko Koya , Hiroyuki Mizuno , Tadayuki Kuraishi
发明人： Teruo Komoto , Hiroyuki Hirota , Susumu Sato , Mari Ohtsuka , Hidehiko Koya , Hiroyuki Mizuno , Tadayuki Kuraishi
IPC分类号： C07D211/22 , C07D211/52 , C07D211/70 , C07D213/82 , C07D295/192 , C07D333/38 , C07D401/06 , C07D405/06 , C07D409/06 , A61K31/445 , C07D211/40 , C07D211/74 , C07D295/10
CPC分类号： C07D213/82 , C07D211/22 , C07D211/52 , C07D211/70 , C07D295/192 , C07D333/38 , C07D401/06 , C07D405/06 , C07D409/06
摘要： An arylamide derivative of formula (1), a salt thereof and a therapeutic agent for hyperlipemia which comprises the derivative or salt: ##STR1## wherein Ar represents a group ##STR2## a naphthyl group, a pyridinyl group, a furyl group, a thienyl group, a quinolyl group or an indolyl group; Y represents a group ##STR3## and Q represents --O-- or a single bond, Z represents an alkylene group, and R.sup.4 represents a hydroxyl group, an alkoxy group or a group --NH(CH.sub.2).sub.m COOH, useful for the treatment and prevention of hyperlipemia due to their excellent cholesterol reducing action, triglyceride reducing action and high safety.
摘要翻译：式（1）的芳基酰胺衍生物，其盐和含有该衍生物或盐的高脂血症治疗剂：其中Ar表示基团，萘基，吡啶基，呋喃基噻吩基，喹啉基或吲哚基; Y表示，Q表示-O-或单键，Z表示亚烷基，R4表示羟基，烷氧基或-NH（CH2）mCOOH基团，可用于治疗和预防高脂血症由于其优异的胆固醇降低作用，甘油三酯降低作用和高安全性。

4. 发明授权

US5063222A Antiinflammatory dexamethasone 17.alpha.-cyclopropanecarboxylates with reduced systemic activity 失效
标题翻译：具有降低的系统活性的抗炎消炎剂DEXAMETHASONE 17（ALPHA） - 环丙氧羰基氧化物
公开(公告)号：US5063222A
公开(公告)日：1991-11-05
申请号：US508686
申请日：1990-04-13
申请人： Teruo Komoto , Junji Okawa , Yoichiro Ogawa , Susumu Sato , Naokata Taido , Tadayuki Kuraishi
发明人： Teruo Komoto , Junji Okawa , Yoichiro Ogawa , Susumu Sato , Naokata Taido , Tadayuki Kuraishi
IPC分类号： A61K31/57 , A61P29/00 , C07J5/00 , C07J7/00
CPC分类号： C07J7/0055 , C07J5/0076 , C07J7/0085
摘要： Steroid derivatives represented by formula (I) are disclosed. ##STR1## wherein R is a hydrogen atom, a halogen atom, a hydroxy group, or a group --OCOR.sub.1, wherein R.sub.1 is a linear or branched alkyl group which may be substituted by a halogen atom or a cycloalkyl group, a cycloalkyl group, or an aryl group. The compounds are useful for curing or alleviating inflammation or rheumatism.

5. 发明授权

US06362203B1 4-hydroxy-4-phenylpiperidine derivatives and pharmaceuticals containing the same 失效
标题翻译： 4-羟基-4-苯基哌啶衍生物和含有它们的药物
公开(公告)号：US06362203B1
公开(公告)日：2002-03-26
申请号：US09698041
申请日：2000-10-30
申请人： Kinichi Mogi , Yoshihiko Kanamaru , Noriyuki Kawamoto , Teruo Komoto , Norimitsu Umehara , Susumu Sato , Tetsuo Oka
发明人： Kinichi Mogi , Yoshihiko Kanamaru , Noriyuki Kawamoto , Teruo Komoto , Norimitsu Umehara , Susumu Sato , Tetsuo Oka
IPC分类号： C07D21152
CPC分类号： C07D211/52
摘要： Described is a 4-hydroxy-4-phenylpiperidine derivative represented by the following formula (1): [wherein, R1 and R2 are the same or different and each independently represents a hydrogen atom, a lower alkyl, or the like, R3 represents a hydrogen atom or a group —(CR4R5)n—Y (in which, R4 and R5 each represents a hydrogen atom or a lower alkyl group, Y represents a group —COOR6, —CONR7R8, —OR9 or —OCOR10 (in which R6, R9 and R10 each independently represents a hydrogen atom, a lower alkyl group, or the like, R7 and R8 are the same or different and each independently represents a hydrogen atom, a lower alkyl group, or the like), and n stands for 1 to 6)], or salt thereof. The compound exhibits excellent peripheral analgesic action.
摘要翻译：描述了由下式（1）表示的4-羟基-4-苯基哌啶衍生物：[其中，R 1和R 2相同或不同，各自独立地表示氢原子，低级烷基等，R 3表示氢原子或基团 - （CR 4 R 5）n Y（其中，R 4和R 5各自表示氢原子或低级烷基，Y表示-COOR 6，-CONR 7 R 8，-OR 9或-OCOR 10（其中R 6，R 9和 R 10各自独立地表示氢原子，低级烷基等，R 7和R 8相同或不同，各自独立地表示氢原子，低级烷基等），n表示1〜6 ）]或其盐。该化合物表现出优异的外周镇痛作用。

6. 发明授权

US5866609A Substituted vinylurea derivatives and medicine containing the same 失效
标题翻译：取代的乙烯基脲衍生物和含有其的药物
公开(公告)号：US5866609A
公开(公告)日：1999-02-02
申请号：US899647
申请日：1997-07-24
申请人： Yoshihiko Kanamaru , Hiroyuki Hirota , Akihiro Shibata , Teruo Komoto , Hiroyuki Naito , Koichi Tachibana , Mari Ohtsuka , Fumio Ishii , Susumu Sato
发明人： Yoshihiko Kanamaru , Hiroyuki Hirota , Akihiro Shibata , Teruo Komoto , Hiroyuki Naito , Koichi Tachibana , Mari Ohtsuka , Fumio Ishii , Susumu Sato
IPC分类号： C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C275/42 , C07C317/42 , C07C323/44 , C07D211/58 , C07D317/58 , C07D317/66 , A61K31/17 , C07C275/04
CPC分类号： C07C317/42 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C275/42 , C07C323/44 , C07D211/58 , C07D317/58 , C07D317/66 , C07C2101/14
摘要： Disclosed herein are substituted vinylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.3 are independently a phenyl group which may be substituted, R.sup.2 is a phenyl group which may be substituted, or a cycloalkyl group, and wave lines mean that the bonding state may be either E or Z, with the proviso that the cases where R.sup.1, R.sup.2 and R.sup.3 are unsubstituted phenyl groups, and where R.sup.1 and R.sup.2 are unsubstituted phenyl groups and R.sup.3 is a 4-ethoxyphenyl group are excluded, or salt thereof, and medicines comprising such a derivative as an active ingredient as well as a method of preventing and treating arteriosclerosis with such a medicine. The derivatives or salts thereof selectively and strongly inhibit ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.
摘要翻译：本文公开了由以下通式（1）表示的取代的乙烯基脲衍生物：其中R 1和R 3独立地为可被取代的苯基，R 2为可被取代的苯基或环烷基并且波线意味着键合状态可以是E或Z，条件是其中R1，R2和R3是未取代的苯基，R1和R2是未取代的苯基，R3是4-乙氧基苯基的情况或其盐，以及包含这样的衍生物作为活性成分的药物，以及用这种药物预防和治疗动脉硬化的方法。其衍生物或其盐在巨噬细胞中选择性且强烈地抑制ACAT，因此可用作动脉硬化的预防和治疗剂。

7. 发明授权

US07214672B2 Preventives/remedies for inflammatory airway diseases 有权
标题翻译：炎症性气道疾病的预防/补救措施
公开(公告)号：US07214672B2
公开(公告)日：2007-05-08
申请号：US10451061
申请日：2001-12-21
申请人： Teruo Komoto , Hiroyuki Mizuno , Yoshinori Takahashi , Koichi Takahashi , Susumo Sato
发明人： Teruo Komoto , Hiroyuki Mizuno , Yoshinori Takahashi , Koichi Takahashi , Susumo Sato
IPC分类号： A61K31/56 , A61K31/58
CPC分类号： C07J5/00 , A61K31/57 , A61K31/573 , C07J7/00
摘要： A preventive and/or therapeutic agent for inflammatory respiratory tract diseases containing, as an active ingredient, a steroid derivative represented by the following formula (1): (wherein R represents a hydrogen atom, a halogen atom, a hydroxy group, or —OCOR1 (wherein R1 represents a linear or branched alkyl group which may be substituted by a halogen atom or a cycloalkyl group; a cycloalkyl group; or an aryl group)). These compounds can continuously suppress respiratory tract inflammation and respiratory tract hyperreaction and show a high site selectivity and little systemic effect when administered directly to the respiratory tract. By virtue of these characteristics, these compounds are remarkably useful in clinical medicine as highly safe preventive and/or therapeutic agents for inflammatory respiratory tract diseases which can be administered for a long period of time.
摘要翻译：一种炎性呼吸道疾病的预防和/或治疗剂，含有下式（1）表示的类固醇衍生物作为活性成分：（式中，R表示氢原子，卤素原子，羟基或-OCOR （其中R 1表示可被卤素原子或环烷基取代的直链或支链烷基;环烷基;或芳基））。这些化合物可以连续抑制呼吸道炎症和呼吸道高反应，并且当直接施用于呼吸道时显示出高的选择性和很小的全身效应。由于这些特征，这些化合物在临床医学中非常有用，作为可长期施用的炎症性呼吸道疾病的高度安全的预防和/或治疗剂。

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