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1. 发明授权

US07208495B2 Benzo-fused 5-membered hetrocycle compounds, process for preparation of the same, and use thereof 失效
标题翻译：苯并稠合的5元杂环化合物，其制备方法及其用途
公开(公告)号：US07208495B2
公开(公告)日：2007-04-24
申请号：US10481367
申请日：2002-07-04
申请人： Shigenori Ohkawa , Masaomi Miyamoto , Masahiro Okura , Tetsuya Tsukamoto
发明人： Shigenori Ohkawa , Masaomi Miyamoto , Masahiro Okura , Tetsuya Tsukamoto
IPC分类号： A61K31/497 , A61K31/445 , C07D405/00 , C07D401/00
CPC分类号： A61K31/4525 , A61K31/496 , C07D307/79 , C07D307/80 , C07D307/81 , C07D307/82 , C07D307/83 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/14
摘要： A compound represented by the formula: (wherein, R1 and R2 are the same or different and each represents a hydrogen atom, hydrocarbon group or heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3–8 membered iso- or heterocyclic group, R3 represents a cyclic group, a hydroxy group, a mercapto group that may have oxo, or an amino group, R4 represents a hydrogen atom, a hydrocarbon group, a hydroxy group, a mercapto group which may have oxo, or an amino group, or R2 and R4 may link together to form a double bond, X represents a bond or a linear hydrocarbon group, W represents an oxygen atom or a sulfur atom, ring B represents a 5–8 membered nitrogen-containing heterocyclic group, ring C represents a benzene ring, and— represents a single bond or a double bond), or a salt or a prodrug thereof that has excellent neurodegenerative inhibitory activity and brain penetrability, and is useful as an agent for preventing/treating neurodegenerative diseases.
摘要翻译：由下式表示的化合物（其中，R 1和R 2相同或不同，各自表示氢原子，烃基或杂环基，可以与相邻的碳原子一起形成3-8元的异或杂环基，R 3表示环状基团，羟基，可具有氧代基的巯基或氨基，R 4表示氢原子，烃基，羟基，可具有氧代基的巯基，或氨基或R 2和R 4可以连接在一起形成双键，X表示键或直链烃基，W表示氧原子或硫原子，环B表示5-8元含氮杂环基，环C表示苯环，代表单键或双键）或其盐或前药具有优异的神经变性抑制活性，脑穿透性并且可用作预防/治疗神经变性疾病的药剂。

2. 发明申请

US20070149558A1 Benzo-fused 5-membered heterocyclic compounds, their production and use 审中-公开
标题翻译：苯并稠合的5元杂环化合物，其生产和使用
公开(公告)号：US20070149558A1
公开(公告)日：2007-06-28
申请号：US11679257
申请日：2007-02-27
申请人： Shigenori Ohkawa , Masaomi Miyamoto , Masahiro Okura , Tetsuya Tsukamoto
发明人： Shigenori Ohkawa , Masaomi Miyamoto , Masahiro Okura , Tetsuya Tsukamoto
IPC分类号： A61K31/4747 , A61K31/407
CPC分类号： A61K31/4525 , A61K31/496 , C07D307/79 , C07D307/80 , C07D307/81 , C07D307/82 , C07D307/83 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/14
摘要： A compound represented by the formula: (wherein, R1 and R2 are the same or different and each represents a hydrogen atom, hydrocarbon group or heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3-8 membered iso- or heterocyclic group, R3 represents a cyclic group, a hydroxy group, a mercapto group that may have oxo, or an amino group, R4 represents a hydrogen atom, a hydrocarbon group, a hydroxy group, a mercapto group which may have oxo, or an amino group, or R2 and R4 may link together to form a double bond, X represents a bond or a linear hydrocarbon group, W represents an oxygen atom or a sulfur atom, ring B represents a 5-8 membered nitrogen-containing heterocyclic group, ring C represents a benzene ring, and represents a single bond or a double bond), or a salt or a prodrug thereof that has excellent neurodegenerative inhibitory activity and brain penetrability, and is useful as an agent for preventing/treating neurodegenerative diseases.
摘要翻译：由下式表示的化合物（其中，R 1和R 2相同或不同，各自表示氢原子，烃基或杂环基，可以与相邻的碳原子一起形成3-8元的异或杂环基，R 3表示环状基团，羟基，可具有氧代基的巯基或氨基，R 4表示氢原子，烃基，羟基，可具有氧代基的巯基，或氨基或R 2和R 4可以连接在一起形成双键，X表示键或直链烃基，W表示氧原子或硫原子，环B表示5-8元含氮杂环基，环C表示苯环，并且表示单键或双键）或其具有优异的神经变性抑制活性和脑渗透性的盐或其前药，并且可用作预防/治疗神经变性疾病的药剂。

3. 发明授权

US06235789B1 Benzocycloalkene compounds, their production and use 失效
标题翻译：苯并环烯烃化合物，其生产和使用
公开(公告)号：US06235789B1
公开(公告)日：2001-05-22
申请号：US08530148
申请日：1997-05-28
申请人： Shigenori Ohkawa , Osamu Uchikawa , Masaomi Miyamoto
发明人： Shigenori Ohkawa , Osamu Uchikawa , Masaomi Miyamoto
IPC分类号： A61K3116
CPC分类号： C07C271/16 , C07C233/18 , C07C233/20 , C07C233/36 , C07C233/60 , C07C233/73 , C07C235/08 , C07C235/48 , C07C275/24 , C07C275/34 , C07C2601/02 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07C2603/94 , C07D211/62
摘要： A compound of the formula wherein R1 and R2 are H, a hydrocarbon group or a heterocyclic group, or R1 and R2 are combinedly a spiro ring; R3 is a hydrocarbon group, a substituted amino group, a substituted hydroxyl group or a heterocyclic group; R4 is H or alkyl; ring A is a substituted benzene ring; m and n denote 1 to 4; {overscore (.........)} means a single or double bond or a salt, a process of producing thereof and a composition having a binding affinity for melatonin receptor.
摘要翻译：式R 1和R 2的化合物是H，烃基或杂环基，或R 1和R 2组合成螺环; R3是烃基，取代氨基，取代羟基或杂环基; R4是H或烷基; 环A是取代的苯环; m和n表示1至4; {overscore（.........）}是指单键或双键或其盐，其制备方法和具有对褪黑激素受体的结合亲和力的组合物。

4. 发明授权

US5922771A Benzocycloalkene compounds, their production and use 失效
标题翻译：苯并环烯烃化合物，其生产和使用
公开(公告)号：US5922771A
公开(公告)日：1999-07-13
申请号：US693058
申请日：1996-08-19
申请人： Shigenori Ohkawa , Osamu Uchikawa , Kohji Fukatsu , Masaomi Miyamoto
发明人： Shigenori Ohkawa , Osamu Uchikawa , Kohji Fukatsu , Masaomi Miyamoto
IPC分类号： C07C233/18 , C07C271/06 , C07D317/70 , A61K31/16 , A61K31/165 , A61K31/27 , A61K31/335 , C07C233/64 , C07C235/00 , C07C237/00
CPC分类号： C07C233/18 , C07C271/06 , C07C2102/08
摘要： A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.
摘要翻译： PCT No.PCT / JP96 / 02091 Sec。 371日期：1996年8月19日 102（e）日期1996年8月19日PCT提交1996年7月25日PCT公布。公开号WO97 / 05098 日期：1997年2月13日下式化合物其中R 1和R 2独立地表示H或任选取代的烃基; R3表示任选取代的烃基; R4表示H或烃基; 环A表示取代的苯环; X表示C2-4亚烷基等; Y表示键或低级亚烷基，或其盐可用作与褪黑激素相关的疾病的预防或治疗剂。

5. 发明授权

US06218429B1 Tricyclic compounds, their production and use 有权
标题翻译：三环化合物，其生产和使用
公开(公告)号：US06218429B1
公开(公告)日：2001-04-17
申请号：US09309519
申请日：1999-05-10
申请人： Shigenori Ohkawa , Osamu Uchikawa , Kohji Fukatsu , Masaomi Miyamoto
发明人： Shigenori Ohkawa , Osamu Uchikawa , Kohji Fukatsu , Masaomi Miyamoto
IPC分类号： A01N34308
CPC分类号： C07D263/52 , C07D265/34 , C07D307/93 , C07D311/94 , C07D317/70 , C07D319/14 , C07D491/04 , Y10S514/923
摘要： A compound of the formula: wherein R1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R2 is H or an optionally substituted hydrocarbon group; R3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR4, NR4, O or S in which R4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.
摘要翻译：下式的化合物：其中R 1是任选取代的烃，氨基或杂环基; R2是H或任选取代的烃基; R3是H或任选取代的烃或杂环基; X是CHR 4，NR 4，O或S，其中R 4是H或任选取代的烃基; Y为C，CH或N; 环A为任选取代的5-至7-元环; 环B是任选取代的苯环; 和m为1至4，或其盐，其制备方法，制备中间体和包含其的药物组合物。

6. 发明授权

US6034239A 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：US6034239A
公开(公告)日：2000-03-07
申请号：US812168
申请日：1997-03-06
申请人： Shigenori Ohkawa , Osamu Uchikawa , Kohji Fukatsu , Masaomi Miyamoto
发明人： Shigenori Ohkawa , Osamu Uchikawa , Kohji Fukatsu , Masaomi Miyamoto
IPC分类号： C07C233/00 , C07D307/92 , C07D413/00 , C07D493/00
CPC分类号： C07D307/77 , C07D263/62 , C07D311/94 , C07D317/70 , C07D319/14 , C07D491/04
摘要： A compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R.sup.2 is H or an optionally substituted hydrocarbon group; R.sup.3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR.sup.4, NR.sup.4, O or S in which R.sup.4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.
摘要翻译：下式的化合物：其中R 1是任选取代的烃，氨基或杂环基; R2是H或任选取代的烃基; R3是H或任选取代的烃或杂环基; X是CHR 4，NR 4，O或S，其中R 4是H或任选取代的烃基; Y为C，CH或N; 环A为任选取代的5-至7-元环; 环B是任选取代的苯环; 和m为1至4，或其盐，其制备方法，制备中间体和包含其的药物组合物。

7. 发明申请

US20060241168A1 Antidepressant 失效
标题翻译：抗抑郁药
公开(公告)号：US20060241168A1
公开(公告)日：2006-10-26
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

8. 发明授权

US06348485B1 Method for treating or preventing sleep disorders 失效
标题翻译：治疗或预防睡眠障碍的方法
公开(公告)号：US06348485B1
公开(公告)日：2002-02-19
申请号：US09700405
申请日：2000-11-14
申请人： Shigenori Ohkawa , Masaomi Miyamoto
发明人： Shigenori Ohkawa , Masaomi Miyamoto
IPC分类号： A61K31415
CPC分类号： A61K31/435 , A61K31/495 , A61K31/55 , A61K2300/00
摘要： The present invention provides a pharmaceutical composition for treating or preventing sleep disorders which comprises (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide in combination with at least one active component selected from zolpidem, zopiclone, triazolam and brotizolam.
摘要翻译：本发明提供了用于治疗或预防睡眠障碍的药物组合物，其包含（S）-N- [2-（1,6,7,8-四氢-2H-茚并[5,4-b]呋喃-8-基）乙基]丙酰胺与至少一种选自唑吡旦，佐匹克隆，三唑仑和brotizolam的活性成分组合。

9. 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。

10. 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

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