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1. 发明授权

US5719152A Tricyclic quinoxalinedione derivatives 失效
标题翻译：三环喹喔啉二酮衍生物
公开(公告)号：US5719152A
公开(公告)日：1998-02-17
申请号：US611973
申请日：1996-03-06
申请人： Ryu Nagata , Norihiko Tanno , Toru Kodo , Hiroshi Yamaguchi , Nobuyuki Ae
发明人： Ryu Nagata , Norihiko Tanno , Toru Kodo , Hiroshi Yamaguchi , Nobuyuki Ae
IPC分类号： C07C271/16 , C07C271/20 , C07C271/22 , C07D471/06 , A61K31/495 , C07D215/48 , C07D487/06
CPC分类号： C07D471/06 , C07C271/16 , C07C271/20 , C07C271/22
摘要： A tricyclic quinoxalinedione derivative represented by the formula 1: ##STR1## wherein X represents hydrogen, alkyl, halogen, cyano, trifluoromethyl, or nitro; R.sup.1 represents hydrogen, alkyl, cycloalkyl, or cycloalkylalkyl; G represents --CONR.sup.2 -- or --NR.sup.2 CO--, wherein R.sup.2 represents hydrogen or alkyl; J represents an acidic group or a group which is convertible thereto in vivo; E represents an basic group or a group which is convertible thereto in vivo; Y represents a single bond, alkylene, alkenylene, substituted alkylene, or Y.sup.1 --Q--Y.sup.2, wherein Y.sup.1 represents a single bond or alkylene, Y.sup.2 represents alkylene, and Q represents a heteroatom selected from oxygen or sulfur; Z represents alkylene, or a pharmaceutically acceptable salt thereof, these compounds are selective antagonists of glycine binding site of the NMDA receptor.
摘要翻译：由式1表示的三环喹喔啉二酮衍生物：其中X表示氢，烷基，卤素，氰基，三氟甲基或硝基; R1代表氢，烷基，环烷基或环烷基烷基; G表示-CONR2-或-NR2CO-，其中R2表示氢或烷基; J表示酸性基团或可在体内转化的基团; E表示可在体内转化的碱性基团或基团; Y表示单键，亚烷基，亚烯基，取代的亚烷基或Y1-Q-Y2，其中Y1表示单键或亚烷基，Y2表示亚烷基，Q表示选自氧或硫的杂原子; Z表示亚烷基或其药学上可接受的盐，这些化合物是NMDA受体的甘氨酸结合位点的选择性拮抗剂。

2. 发明授权

US5616586A Tricyclic quinoxalinediones 失效
标题翻译：三环喹喔啉
公开(公告)号：US5616586A
公开(公告)日：1997-04-01
申请号：US211314
申请日：1994-04-01
申请人： Ryu Nagata , Norihiko Tanno , Toru Kodo
发明人： Ryu Nagata , Norihiko Tanno , Toru Kodo
IPC分类号： A61K31/495 , A61P9/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D471/06 , C07D487/06 , C07D215/48
CPC分类号： C07D471/06 , C07D487/06
摘要： Tricyclic quinoxalinediones of the formula: ##STR1## wherein X is alkyl, halogen, cyano, trifluoromethyl, nitro, hydroxy, amino, etc.; R.sup.1 is H, etc.; R.sup.2 is H, alkyl, cycloalkyl, alkenyl, alkynyl, cycloalkylalkyl, arylalkyl, substituted arylalkyl, aryl, or substituted aryl; W is H, CO.sub.2 R.sup.3, CO.sub.2 Y, CONR.sup.3 R.sup.4, CONR.sup.3 Y, CON(OR.sup.3)R.sup.4, COR.sup.3, CN, tetrazolyl, or substituted alkyl; R.sup.3 and R.sup.4 independently are H, alkyl, cycloalkyl, alkenyl, alkynyl, etc.; Y is mono-substituted alkyl or di-substituted alkyl; and n is an integer 0 or 1, or a pharmaceutically acceptable salt thereof, which are useful as a selective antagonist of glutamate receptor for the treatment or prevention of various diseases in animals including human being, for example, minimizing damage of central nervous system induced by ischaemic or hypoxylic conditions, treatment and/or prevention of neurodegenerative disorders, and further analgesics, antidepressants, anxiolitics, and anti-schizophrenics.
摘要翻译： PCT No.PCT / JP92 / 01375 Sec。 371日期1994年04月1日 102（e）日期1994年4月1日PCT提交1992年10月22日PCT公布。出版物WO93 / 08188 日期：1993年4月29日三氟甲基，硝基，羟基，氨基等的三环喹喔啉。 R1为H等; R2是H，烷基，环烷基，烯基，炔基，环烷基烷基，芳基烷基，取代的芳基烷基，芳基或取代的芳基; W是H，CO 2 R 3，CO 2 Y，CONR 3 R 4，CONR 3 Y，CON（OR 3）R 4，COR 3，CN，四唑基或取代的烷基; R3和R4独立地是H，烷基，环烷基，烯基，炔基等; Y是单取代的烷基或二取代的烷基; 并且n是整数0或1，或其药学上可接受的盐，其可用作谷氨酸受体的选择性拮抗剂，用于治疗或预防动物中的各种疾病，包括人类，例如使中枢神经系统诱导的损伤最小化通过缺血或缺氧条件，治疗和/或预防神经变性疾病，以及进一步的镇痛药，抗抑郁药，焦虑症和抗精神分裂症。

3. 发明授权

US5496843A Tricyclic indole-2-carboxylic acid derivatives 失效
标题翻译：三环吲哚-2-羧酸衍生物
公开(公告)号：US5496843A
公开(公告)日：1996-03-05
申请号：US339687
申请日：1994-11-14
申请人： Ryu Nagata , Norihiko Tanno , Nobuyuki Ae
发明人： Ryu Nagata , Norihiko Tanno , Nobuyuki Ae
IPC分类号： C07D209/90 , A61K31/40 , C07D209/62
CPC分类号： C07D209/90 , Y02P20/55
摘要： A tricyclic indole-2-carboxylic acid derivative represented by the formula 1: ##STR1## wherein X represents alkyl, halogen or cyano;R.sup.1 represents hydrogen, or a protecting group of carboxyl group;W represents hydrogen, --CO.sub.2 R.sup.3i, --CONR.sup.3i R.sup.4i, --A--CO.sub.2 R.sup.3i or --A--CONR.sup.3i R.sup.4i, wherein --A-- represents alkylene and R.sup.3i and R.sup.4i independently represent hydrogen, alkyl, aryl or substituted aryl,or a pharmaceutically acceptable salt thereof, these compounds are selective antagonists of glycine binding site of the NMDA receptor.
摘要翻译：由式1表示的三环吲哚-2-羧酸衍生物：其中X表示烷基，卤素或氰基; R1表示氢或羧基的保护基; W代表氢，-CO2R3i，-CONR3iR4i，-A-CO2R3i或-A-CONR3iR4i，其中-A-表示亚烷基，R3i和R4i独立地表示氢，烷基，芳基或取代的芳基或其药学上可接受的盐，这些化合物是NMDA受体的甘氨酸结合位点的选择性拮抗剂。

4. 发明申请

US20110183993A1 CYCLOALKANE DERIVATIVE 审中-公开
标题翻译：循环衍生物
公开(公告)号：US20110183993A1
公开(公告)日：2011-07-28
申请号：US13015745
申请日：2011-01-28
申请人： Ryu Nagata , Mayumi Oda , Norihiko Tanno , Masayuki Muto , Ikutaro Saji
发明人： Ryu Nagata , Mayumi Oda , Norihiko Tanno , Masayuki Muto , Ikutaro Saji
IPC分类号： A61K31/496 , C07D417/14 , A61P25/18
CPC分类号： C07D417/14
摘要： The present invention relates to a novel cycloalkane derivative which has an excellent psychotropic action.
摘要翻译：本发明涉及一种具有优良精神作用的新型环烷烃衍生物。

5. 发明授权

US06495587B1 Tricyclic indole-2-carboxylic acid compound used as NMDA receptor antagonist 失效
标题翻译：用作NMDA受体拮抗剂的三环吲哚-2-羧酸化合物
公开(公告)号：US06495587B1
公开(公告)日：2002-12-17
申请号：US09914461
申请日：2001-08-29
申请人： Nobuyuki Ae , Seiji Katayama , Hisakazu Kishimoto , Ryu Nagata
发明人： Nobuyuki Ae , Seiji Katayama , Hisakazu Kishimoto , Ryu Nagata
IPC分类号： A61K3140
CPC分类号： C07D209/90
摘要： The present invention provides novel tricyclic indole-2-carboxylic acids of the following chemical formula, which have potent NMDA receptor antagonistic activity.
摘要翻译：本发明提供具有下列化学式的新型三环吲哚-2-羧酸，其具有有效的NMDA受体拮抗活性。

6. 发明授权

US07781479B2 Heteroaryl derivatives 失效
标题翻译：杂芳基衍生物
公开(公告)号：US07781479B2
公开(公告)日：2010-08-24
申请号：US11795147
申请日：2006-01-12
申请人： Yoko Takahashi , Ryu Nagata , Kantaro Ushiroda
发明人： Yoko Takahashi , Ryu Nagata , Kantaro Ushiroda
IPC分类号： A61K31/405 , A61K31/404 , A61K31/192 , C07D209/04 , C07D209/12
CPC分类号： C07D233/64 , C07D209/12 , C07D231/56 , C07D235/12 , C07D471/04
摘要： A compound of the following formula (1), or its prodrug or pharmaceutically acceptable salt thereof, being useful as a diabetic medicine or preventive, or blood sugar regulator, or therapeutic agent for hyperlipemia, etc. wherein the ring Z is an optionally substituted heteroaryl, W4 is a single bond, lower alkylene, etc., Ar2 is an optionally substituted aryl, etc., W3 is a single bond, lower alkylene, etc., Ar1 is an optionally substituted arylene, etc., each of W1 and W2 is an optionally substituted lower alkylene, etc., and R1 is carboxyl, an alkoxycarbonyl.
摘要翻译：下式（1）的化合物或其前药或药学上可接受的盐可用作糖尿病药物或预防性或血糖调节剂或高脂血症治疗剂等，其中环Z为任选取代的杂芳基 W4为单键，低级亚烷基等，Ar2为任意取代的芳基等，W3为单键，低级亚烷基等，Ar1为任意取代的亚芳基等，W1，W2分别为是任选取代的低级亚烷基等，并且R 1是羧基，烷氧基羰基。

7. 发明申请

US20080306275A1 NOVEL HETEROARYL DERIVATIVE 审中-公开
标题翻译：新世代衍生
公开(公告)号：US20080306275A1
公开(公告)日：2008-12-11
申请号：US12173792
申请日：2008-07-15
申请人： Ken-ichi WATANABE , Katsunori Maruta , Kantaro Ushiroda , Ryu Nagata
发明人： Ken-ichi WATANABE , Katsunori Maruta , Kantaro Ushiroda , Ryu Nagata
IPC分类号： C07D233/58 , C07D401/14
CPC分类号： C07D207/333
摘要： A heteroaryl derivative of the formula (1): (wherein Ring Z is an optionally substituted heteroaryl, R1 is a carboxyl group or an alkoxycarbonyl group, etc., W1 and W2 are an optionally substituted lower alkylene, Ar1 is an optionally substituted arylene or an optionally substituted heteroarylene, W3 is a single bond, a lower alkylene, a lower alkenylene, etc., W4 is a single bond, —NR10—, etc., Ar2 is an optionally substituted aryl or an optionally substituted heteroaryl), or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
摘要翻译：式（1）的杂芳基衍生物：（其中环Z是任选取代的杂芳基，R 1是羧基或烷氧基羰基等，W 1和W 2是任选取代的低级亚烷基，Ar 1是任选取代的亚芳基或任选取代的杂亚芳基，W3是单键，低级亚烷基，低级亚烯基等，W4是单键，-NR10-等，Ar2是任选取代的芳基或任选取代的杂芳基）或前药，或其药学上可接受的盐。

8. 发明授权

US07425642B2 Heteroaryl derivative 失效
标题翻译：杂芳基衍生物
公开(公告)号：US07425642B2
公开(公告)日：2008-09-16
申请号：US10563361
申请日：2004-07-13
申请人： Ken-ichi Watanabe , Katsunori Maruta , Kantaro Ushiroda , Ryu Nagata
发明人： Ken-ichi Watanabe , Katsunori Maruta , Kantaro Ushiroda , Ryu Nagata
IPC分类号： C07D207/00 , C07D295/00
CPC分类号： C07D207/333
摘要： A heteroaryl derivative of the formula (1): (wherein Ring Z is an optionally substituted heteroaryl, R1 is a carboxyl group or an alkoxycarbonyl group, etc., W1 and W2 are an optionally substituted lower alkylene, Ar1 is an optionally substituted arylene or an optionally substituted heteroarylene, W3 is a single bond, a lower alkylene, a lower alkenylene, etc., W4 is a single bond, —NR10—, etc., Ar2 is an optionally substituted aryl or an optionally substituted heteroaryl), or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
摘要翻译：式（1）的杂芳基衍生物：（其中环Z是任选取代的杂芳基，R 1是羧基或烷氧基羰基等，W 1，和W 2是任选取代的低级亚烷基，Ar 1是任选取代的亚芳基或任选取代的亚杂芳基，W 3是单键，低级亚烷基，低级亚烯基等，W 4是单键，-NR 10 - 等，Ar 2，是任选取代的芳基或任选取代的杂芳基）或其前药，或其药学上可接受的盐。

9. 发明申请

US20080167306A1 Novel Heteroaryl Derivative 失效
标题翻译：新型杂芳衍生物
公开(公告)号：US20080167306A1
公开(公告)日：2008-07-10
申请号：US11795147
申请日：2006-01-12
申请人： Yoko Takahashi , Ryu Nagata , Kantaro Ushiroda
发明人： Yoko Takahashi , Ryu Nagata , Kantaro Ushiroda
IPC分类号： A61K31/5377 , C07D207/00 , A61K31/40 , C07D209/04 , A61K31/404 , C07D213/02 , A61K31/437 , C07D231/10 , A61P9/00 , A61P3/10 , A61K31/415 , C07D235/04 , A61K31/4184 , C07D231/54 , C07D221/02 , C07D295/00
CPC分类号： C07D233/64 , C07D209/12 , C07D231/56 , C07D235/12 , C07D471/04
摘要： A compound of the following formula (1), or its prodrug or pharmaceutically acceptable salt thereof, being useful as a diabetic medicine or preventive, or blood sugar regulator, or therapeutic agent for hyperlipemia, etc. wherein the ring Z is an optionally substituted heteroaryl, W4 is a single bond, lower alkylene, etc., Ar2 is an optionally substituted aryl, etc., W3 is a single bond, lower alkylene, etc., Ar1 is an optionally substituted arylene, etc., each of W1 and W2 is an optionally substituted lower alkylene, etc., and R1 is carboxyl, an alkoxycarbonyl.
摘要翻译：下式（1）的化合物或其前药或药学上可接受的盐可用作糖尿病药物或预防性或血糖调节剂或高脂血症治疗剂等，其中环Z为任选取代的杂芳基，W 4是单键，低级亚烷基等，Ar 2是任选取代的芳基等，W 3是单键，低级亚烷基等，Ar 1是任选取代的亚芳基等，W 1和W 2中的每一个是任选取代的低级亚烷基等，R 1是羧基，烷氧基羰基。

10. 发明申请

US20050227978A1 Fibrosis inhibitor 审中-公开
标题翻译：纤维化抑制剂
公开(公告)号：US20050227978A1
公开(公告)日：2005-10-13
申请号：US10502933
申请日：2003-01-28
申请人： Teruhisa Tokunaga , Willian Hume , Makoto Kitoh , Ryu Nagata , Michiko Kishino , Tsutomu Nakagawa , Jun Nagamine , Mutsuo Taiji
发明人： Teruhisa Tokunaga , Willian Hume , Makoto Kitoh , Ryu Nagata , Michiko Kishino , Tsutomu Nakagawa , Jun Nagamine , Mutsuo Taiji
IPC分类号： A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4174 , A61K31/425 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/498 , A61K31/4985 , A61K31/5377 , A61P11/00 , A61P13/12 , A61P17/00 , A61P43/00 , C07D207/32 , C07D207/333 , C07D233/64 , C07D401/06 , A61K31/401 , A61K31/4164
CPC分类号： C07D207/333 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4174 , A61K31/425 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/498 , A61K31/4985 , A61K31/5377 , C07D401/06
摘要： Medicament being useful as a fibrosis inhibitor for organs or tissues, which comprises a compound of the formula (I): wherein Ring Z is optionally substituted pyrrole ring, etc.; W2 is —CO—, —SO2—, optionally substituted C1-C4 alkylene, etc.; Ar2 is optionally substituted aryl, etc.; W1 and Ar1 mean the following (1) and (2): (1) W1 is optionally substituted C1-C4 alkylene, etc.; Ar1 is optionally substituted bicyclic heteroaryl having 1 to 4 nitrogen atoms as ring-forming atoms: (2) W1 is optionally substituted C2-C5 alkylene, optionally substituted C2-C5 alkenylene, etc.; and Ar1 is aryl or monocyclic heteroaryl, which is substituted by carboxyl, alkoxycarbonyl, etc. at the ortho- or meta-position thereof with respect to the binding position of W1, or a pharmaceutically acceptable salt thereof.
摘要翻译：药物用作器官或组织的纤维化抑制剂，其包含式（I）的化合物：其中环Z是任选取代的吡咯环等; W 2是-CO - ， - SO 2 - ，任选取代的C 1 -C 4亚烷基等。 Ar 2是任选取代的芳基等; （1）和（2）：（1）W 1是任选取代的C 1 亚烷基等; 任选取代的具有1至4个氮原子的双环杂芳基作为成环原子：（2）W 1是任选取代的C 2 - -C 5亚烷基，任选取代的C 2 -C 5亚烯基等; 和Ar 1是在相邻或相对于W 1的结合位置的邻位或间位被羧基，烷氧基羰基等取代的芳基或单环杂芳基 >，或其药学上可接受的盐。

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