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1. 发明授权

US5478844A Method of using aminocoumaran derivatives for treating cerebrovascular diseases 失效
标题翻译：氨基青霉烷衍生物治疗脑血管疾病的方法
公开(公告)号：US5478844A
公开(公告)日：1995-12-26
申请号：US305717
申请日：1994-09-14
申请人： Tetsuya Aono , Shigenori Ohkawa , Takayuki Doi
发明人： Tetsuya Aono , Shigenori Ohkawa , Takayuki Doi
IPC分类号： A61K31/34 , A61K31/343 , A61K31/415 , A61K31/44 , A61K31/443 , A61K31/445 , A61P3/06 , A61P9/00 , A61P29/00 , A61P37/08 , C07C233/25 , C07D307/79 , C07D307/80 , C07D307/81 , C07D307/82 , C07D405/04 , C07D405/06 , C07D405/12 , C07D417/12 , C07D521/00
CPC分类号： C07D307/79 , C07C233/25 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/80 , C07D307/81 , C07D405/04 , C07D405/12 , C07D417/12 , Y10S514/87
摘要： A novel aminocoumaran derivatives of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are a hydrogen atom, an acyl group, an alkoxycarbonyl group, an aliphatic group or aromatic group; R.sup.3, R.sup.4 and R.sup.5 are an optionally acylated hydroxyl optionally substituted amino group, alkoxy group or aliphatic group, or two of R.sup.3, R.sup.4 and R.sup.5 may be linked together to form a carbocyclic group; R.sup.6 and R.sup.7 are an aliphatic group and at least: one of them has a methylene group at the .alpha.-position; R.sup.8 and R.sup.9 are a hydrogen atom or an aliphatic group or aromatic group, or a salt thereof is useful for medicines for treating various diseases such as arterial sclerosis, hepatopathy, cerebrovascular diseases and the like.
摘要翻译：通式（I）的新型氨基香草醛衍生物：其中R 1和R 2为氢原子，酰基，烷氧基羰基，脂族基团或芳族基团; R3，R4和R5是任选被酰化的羟基任选取代的氨基，烷氧基或脂族基团，或者R 3，R 4和R 5中的两个可以连接在一起形成碳环基团; R6和R7是脂族基团，并且至少：其中一个在α位具有亚甲基; R8和R9是氢原子或脂族基团或芳族基团，或其盐可用于治疗各种疾病如动脉硬化，肝病，脑血管疾病等的药物。

2. 发明授权

US5594154A Intermediates for pharmaceutically useful aminocoumaran derivatives 失效
标题翻译：用于药学上有用的氨基香豆素衍生物的中间体
公开(公告)号：US5594154A
公开(公告)日：1997-01-14
申请号：US447450
申请日：1995-05-23
申请人： Tetsuya Aono , Shigenori Ohkawa , Takayuki Doi
发明人： Tetsuya Aono , Shigenori Ohkawa , Takayuki Doi
IPC分类号： A61K31/34 , A61K31/343 , A61K31/415 , A61K31/44 , A61K31/443 , A61K31/445 , A61P3/06 , A61P9/00 , A61P29/00 , A61P37/08 , C07C233/25 , C07D307/79 , C07D307/80 , C07D307/81 , C07D307/82 , C07D405/04 , C07D405/06 , C07D405/12 , C07D417/12 , C07D521/00
CPC分类号： C07D307/79 , C07C233/25 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/80 , C07D307/81 , C07D405/04 , C07D405/12 , C07D417/12 , Y10S514/87
摘要： A novel aminocoumaran derivative of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are a hydrogen atom, an acyl group, an alkoxycarbonyl group, an aliphatic group or aromatic group; R.sup.3, R.sup.4 and R.sup.5 are an optionally acylated hydroxyl optionally substituted amino group, alkoxy group or aliphatic group, or two of R.sup.3, R.sup.4 and R.sup.5 may be linked together to form a carbocyclic group; R.sup.6 and R.sup.7 are an aliphatic group and at least one of them has a methylene group at the .alpha.-position; R.sup.8 and R.sup.9 are a hydrogen atom or an aliphatic group or aromatic group, or a salt thereof is useful for medicines for preventing and treating various diseases such as arterial sclerosis, hepatopathy, cerebrovascular diseases and the like.
摘要翻译：通式（I）的新型氨基香草衍生物：其中R 1和R 2为氢原子，酰基，烷氧基羰基，脂族基团或芳族基团; R3，R4和R5是任选被酰化的羟基任选取代的氨基，烷氧基或脂族基团，或者R 3，R 4和R 5中的两个可以连接在一起形成碳环基; R6和R7是脂族基团，并且它们中的至少一个在α位具有亚甲基基团; R8和R9是氢原子或脂族基团或芳族基团，或其盐可用于预防和治疗诸如动脉硬化症，肝病，脑血管病等各种疾病的药物。

3. 发明授权

US5376681A Aminocoumaran derivatives, their production and use 失效
标题翻译：氨基花青衍生物，其生产和使用
公开(公告)号：US5376681A
公开(公告)日：1994-12-27
申请号：US784988
申请日：1991-10-30
申请人： Tetsuya Aono , Shigenori Ohkawa , Takayuki Doi
发明人： Tetsuya Aono , Shigenori Ohkawa , Takayuki Doi
IPC分类号： A61K31/34 , A61K31/343 , A61K31/415 , A61K31/44 , A61K31/443 , A61K31/445 , A61P3/06 , A61P9/00 , A61P29/00 , A61P37/08 , C07C233/25 , C07D307/79 , C07D307/80 , C07D307/81 , C07D307/82 , C07D405/04 , C07D405/06 , C07D405/12 , C07D417/12 , C07D521/00
CPC分类号： C07D307/79 , C07C233/25 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/80 , C07D307/81 , C07D405/04 , C07D405/12 , C07D417/12 , Y10S514/87
摘要： A novel aminocoumaran derivatives of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are a hydrogen atom, an acyl group, an alkoxycarbonyl group, an aliphatic group or aromatic group; R.sup.3 R.sup.4 and R.sup.5 are an optionally acylated hydroxyl optionally substituted amino group, alkoxy group or aliphatic group, or two of R.sup.3, R.sup.4 and R.sup.5 may be linked together to form a carbocyclic group; R.sup.6 and R.sup.7 are an aliphatic group and at least one of them has a methylene group at the .alpha.-position; R.sup.8 and R.sup.9 are a hydrogen atom or an aliphatic group or aromatic group, or a salt thereof is useful for medicines for preventing and treating various diseases such as arterial schleosis, hepatopathy, cerebrovascular diseases and the like.
摘要翻译：通式（I）的新型氨基香草醛衍生物：其中R 1和R 2为氢原子，酰基，烷氧基羰基，脂族基团或芳族基团; R3 R4和R5是任选被酰化的羟基任选取代的氨基，烷氧基或脂族基团，或者R 3，R 4和R 5中的两个可以连接在一起形成碳环基; R6和R7是脂族基团，并且它们中的至少一个在α位具有亚甲基基团; R8和R9是氢原子或脂族基团或芳族基团，或其盐可用于预防和治疗动脉淤塞，肝病，脑血管病等各种疾病的药物。

4. 发明授权

US5770772A Intermediates for the preparation of aminocoumaran derivatives 失效
标题翻译：用于制备氨基香豆素衍生物的中间体
公开(公告)号：US5770772A
公开(公告)日：1998-06-23
申请号：US715216
申请日：1996-09-17
申请人： Tetsuya Aono , Shigenori Ohkawa , Takayuki Doi
发明人： Tetsuya Aono , Shigenori Ohkawa , Takayuki Doi
IPC分类号： A61K31/34 , A61K31/343 , A61K31/415 , A61K31/44 , A61K31/443 , A61K31/445 , A61P3/06 , A61P9/00 , A61P29/00 , A61P37/08 , C07C233/25 , C07D307/79 , C07D307/80 , C07D307/81 , C07D307/82 , C07D405/04 , C07D405/06 , C07D405/12 , C07D417/12 , C07D521/00 , C07C233/03
CPC分类号： C07D307/79 , C07C233/25 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/80 , C07D307/81 , C07D405/04 , C07D405/12 , C07D417/12 , Y10S514/87
摘要： Disclosed are intermediates for the preparation of novel aminocoumaran derivatives of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are a hydrogen atom, an acyl group, an alkoxycarbonyl group, an aliphatic group or aromatic group; R.sup.3, R.sup.4 and R.sup.5 are an optionally acylated hydroxyl, optionally substituted amino group, alkoxy group or aliphatic group, or two of R.sup.3, R.sup.4 and R.sup.5 may be linked together to form a carbocyclic group; R.sup.6 and R.sup.7 are an aliphatic group and at least one of them has a methylene group at the .alpha.-position; R.sup.8 and R.sup.9 are a hydrogen atom or an aliphatic group or aromatic group, or a salt thereof is useful for medicines for preventing and treating various diseases such as arterial sclerosis, hepatopathy, cerebrovascular diseases and the like.
摘要翻译：公开了用于制备通式（I）的新型氨基香草醛衍生物的中间体：其中R 1和R 2是氢原子，酰基，烷氧基羰基，脂族基团或芳族基团; R 3，R 4和R 5是任选被酰化的羟基，任选取代的氨基，烷氧基或脂族基团，或者R 3，R 4和R 5中的两个可以连接在一起形成碳环基团; R6和R7是脂族基团，并且它们中的至少一个在α位具有亚甲基基团; R8和R9是氢原子或脂族基团或芳族基团，或其盐可用于预防和治疗诸如动脉硬化症，肝病，脑血管病等各种疾病的药物。

5. 发明授权

US07750037B2 Antidepressant 失效
标题翻译：抗抑郁药
公开(公告)号：US07750037B2
公开(公告)日：2010-07-06
申请号：US11475539
申请日：2006-06-27
申请人： Shigenori Ohkawa , Masaomi Miyamoto
发明人： Shigenori Ohkawa , Masaomi Miyamoto
IPC分类号： A61K31/4035 , C07D405/02
CPC分类号： C07D405/04 , C07D307/79 , C07D405/12 , C07D409/12 , C07D491/04 , C07D491/10
摘要： A PKB (Akt) activating agent comprising a compound represented by the formula (I): wherein R1 and R2: H, a hydrocarbon group or a heterocyclic group or R1 and R2 form a ring in cooperation with the adjacent carbon atom; R3: H, a hydrocarbon group or a heterocyclic group; W: represents a group represented by the formulas: wherein ring A: an optionally substituted benzene ring; ring B: an optionally substituted 5- to 7-membered nitrogen-containing heterocycle; R4: an aliphatic hydrocarbon group substituted with an aromatic group and further optionally substituted, or an acyl group containing an aromatic group; R5: H, C1-6 alkyl or acyl; R4c: an aromatic group, an aliphatic hydrocarbon group or acyl; and X: O or S; Y: O, S or NH; and ring C: an optionally substituted benzene ring, or a salt or a prodrug thereof, and use of the activating agent in prevention or treatment of depression, anxiety, manic-depressive psychosis or PTSD are provided.
摘要翻译：一种PKB（Akt）活化剂，其包含由式（I）表示的化合物：其中R1和R2：H，烃基或杂环基或R1和R2与相邻碳原子一起形成环; R3：H，烃基或杂环基; W：表示由下式表示的基团：其中环A：任选取代的苯环; 环B：任选取代的5-至7-元含氮杂环; R4：被芳基取代并进一步任选取代的脂族烃基或含芳基的酰基; R5：H，C1-6烷基或酰基; R4c：芳基，脂族烃基或酰基; 和X：O或S; Y：O，S或NH; 和环C：任选取代的苯环，或其盐或前药，并且提供了用于预防或治疗抑郁，焦虑，躁狂抑郁性精神病或PTSD的活化剂。

6. 发明申请

US20050148650A1 Antidepressant 审中-公开
标题翻译：抗抑郁药
公开(公告)号：US20050148650A1
公开(公告)日：2005-07-07
申请号：US10506269
申请日：2003-02-28
申请人： Shigenori Ohkawa , Masaomi Miyamoto
发明人： Shigenori Ohkawa , Masaomi Miyamoto
IPC分类号： A61P25/00 , A61P25/14 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D307/79 , C07D405/04 , C07D405/12 , C07D409/12 , C07D491/04 , C07D491/056 , C07D491/10 , C07D491/107 , A61K31/4035 , A61K31/407
CPC分类号： C07D405/04 , C07D307/79 , C07D405/12 , C07D409/12 , C07D491/04 , C07D491/10
摘要： A PKB (Akt) activating agent comprising a compound represented by the formula (I): wherein R1 and R2: H, a hydrocarbon group or a heterocyclic group or R1 and R2 form a ring in cooperation with the adjacent carbon atom; R3: H, a hydrocarbon group or a heterocyclic group; W: represents a group represented by the formulas: wherein ring A: an optionally substituted benzene ring; ring B: an optionally substituted 5- to 7-membered nitrogen-containing heterocycle; R4: an aliphatic hydrocarbon group substituted with an aromatic group and further optionally substituted, or an acyl group containing an aromatic group; R5: H, C1-6 alkyl or acyl; R4c: an aromatic group, an aliphatic hydrocarbon group or acyl; and X:O or S; Y:O, S or NH; and ring C: an optionally substituted benzene ring, or a salt or a prodrug thereof, and use of the activating agent in prevention or treatment of depression, anxiety, manic-depressive psychosis or PTSD are provided.
摘要翻译：一种PKB（Akt）活化剂，其包含由式（I）表示的化合物：其中R 1和R 2：H，烃基或杂环基或R 与相邻的碳原子一起形成环;和<！ - SIPO

7. 发明授权

US06872718B1 Tricyclic dihydrobenzofuran derivatives, process for the preparation thereof and agents 失效
标题翻译：三环二氢苯并呋喃衍生物，其制备方法和试剂
公开(公告)号：US06872718B1
公开(公告)日：2005-03-29
申请号：US10069180
申请日：2000-08-18
申请人： Shigenori Ohkawa , Tadatoshi Hashimoto , Tetsuya Tsukamoto
发明人： Shigenori Ohkawa , Tadatoshi Hashimoto , Tetsuya Tsukamoto
IPC分类号： A61P9/08 , A61P9/10 , A61P13/02 , A61P25/00 , A61P25/16 , A61P25/28 , C07D491/04 , C07D491/048 , D07D491/048 , A61K31/407 , A61K31/4741 , A61K31/55
CPC分类号： C07D491/04
摘要： A compound represented by the formula: wherein Ring A is a non-aromatic 5- to 7-membered nitrogen-containing heterocyclic ring which may be further substituted, Ring B is benzene ring which is further substituted, Ring C is a dihydrofuran-ring which may be further substituted and R is hydrogen atom or an acyl group or a salt thereof has an excellent lipid peroxidation inhibitory activity and is useful as a lipid peroxidation inhibitor.
摘要翻译：一种由下式表示的化合物：其中环A是可进一步被取代的非芳族5-至7-元含氮杂环，环B为进一步取代的苯环，环C为二氢呋喃环，其中可以进一步被取代，R是氢原子或酰基或其盐具有优异的脂质过氧化抑制活性，可用作脂质过氧化抑制剂。

8. 发明授权

US06583146B1 Thiazolopyrimidine compounds, its production and use 失效
标题翻译：噻唑并嘧啶化合物，其生产和使用
公开(公告)号：US06583146B1
公开(公告)日：2003-06-24
申请号：US09889139
申请日：2001-07-12
申请人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
发明人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
IPC分类号： A61K31519
CPC分类号： C07D513/04 , A61K31/519
摘要： Compounds represented by general formula (I): and salts thereof, exhibiting excellent adenosine A3 receptor antagonism: wherein A is an optionally substituted benzene ring; B may be further substituted; and R1 is an optionally substituted cyclic group.
摘要翻译：由通式（I）表示的化合物及其盐，显示出优异的腺苷A3受体拮抗作用：其中A为任选取代的苯环; B可以进一步被取代; 并且R 1是任选取代的环状基团。

9. 发明授权

US06248766B1 Tricyclic compounds, their production and use 失效
标题翻译：三环化合物，其生产和使用
公开(公告)号：US06248766B1
公开(公告)日：2001-06-19
申请号：US09254446
申请日：1999-03-09
申请人： Shigenori Ohkawa , Masaki Setoh , Zen-ichi Terashita
发明人： Shigenori Ohkawa , Masaki Setoh , Zen-ichi Terashita
IPC分类号： A61K31428
CPC分类号： C07D277/60 , C07D277/84 , C07D513/04
摘要： A compound of the formula: wherein R1 is H or a substituent; m is 1-3; Ar is an aromatic group which may be substituted; X is a bond or a divalent straight-chain group having 1-6 atoms which may be substituted; Y is —S—, —O—, or —N(R2— (R2 is H or a substituent group), Z is —N═ or —C(R3)═ (R3 is H or a hydrocarbon group), ring A is a benzene ring; ring B is a 5- to 7-membered ring which may be substituted, or a salt thereof is useful for eliciting a prostaglandin I2 receptor agonistic effect.
摘要翻译：下式的化合物：其中R 1是H或取代基; m为1-3; Ar是可以被取代的芳基; X是可以被取代的具有1-6个原子的键或二价直链基团; Y是-S-，-O-或-N（R2-（R2是H或取代基），Z是-N =或-C（R3）=（R3是H或烃基），环A 是苯环;环B是可被取代的5-至7-元环，或其盐可用于引发前列腺素I2受体激动作用。

10. 发明授权

US5116861A Nitrosothiol derivatives and their use 失效
标题翻译：硝基苯酚衍生物及其用途
公开(公告)号：US5116861A
公开(公告)日：1992-05-26
申请号：US562626
申请日：1990-08-03
申请人： Giichi Goto , Shigenori Ohkawa , Shoji Fukumoto
发明人： Giichi Goto , Shigenori Ohkawa , Shoji Fukumoto
IPC分类号： A61K38/00 , C07C381/00 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/093
CPC分类号： C07K5/0819 , C07C381/00 , C07K5/0215 , C07K5/0606 , A61K38/00
摘要： Novel nitrosothiol derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.3 is a hydrogen atom, an acyl group or a hydrocarbon residue which may be substituted; X.sup.1 is a hydrogen atom, an acyl group, a lower alkoxy group or a hydrocarbon residue which may be substituted; X.sup.2 is an acyl group or a carboxyl group which may be esterified or which may form an amide; with proviso that when X.sup.2 is a carboxyl group X.sup.1 is not a hydrogen atom or acetyl group and that when both R.sup.1 and R.sup.2 are hydrogen atoms X.sup.1 is not acetyl group or .gamma.-glutamyl group, and salts thereof, show excellent hypotensive action, antiarrhythmic action, anti-anginal action, cardiotonic action or coronary vasodilation, thus being useful as therapeutic or prophylactic agents for the cardiovascular diseases such as hypertension and angina pectoris.

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