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1. 发明申请

US20070276011A1 Plasminogen Activator Inhibitor-1 Inhibitor 审中-公开
标题翻译：纤溶酶原激活物抑制剂-1抑制剂
公开(公告)号：US20070276011A1
公开(公告)日：2007-11-29
申请号：US10571324
申请日：2004-09-03
申请人： Susumu Muto , Asako Kubo , Akiko Itai , Tomomi Sotome , Yoichi Yamaguchi
发明人： Susumu Muto , Asako Kubo , Akiko Itai , Tomomi Sotome , Yoichi Yamaguchi
IPC分类号： A61K31/426 , A61K31/4152 , A61K31/44 , A61P7/02 , C07D231/18 , C07D277/34 , C07D417/06 , C07D233/70 , A61P7/04 , A61P7/00 , A61K31/4166
CPC分类号： C07D405/06 , C07D231/20 , C07D277/20 , C07D279/06 , C07D409/06 , C07D417/06 , C07D417/12
摘要： A medicament having inhibitory activity against plasminogen activator inhibitor-1, which comprises as an active ingredient a compound represented by the following general formula (I) or a salt thereof: wherein R1 and R2 represents an aromatic group which may be substituted, W represents a group selected from the following connecting group W-1: (wherein a bond at the left end binds to the carbon atom and a bond at the right end binds to the nitrogen atom, X represents sulfur atom or NH, Y represents oxygen atom or sulfur atom, R3 represents a hydrocarbon group, hydroxy group, or carboxy group), Z represents a single bond or a connecting group wherein a number of atoms in a main chain is 1 to 3.
摘要翻译：一种对纤溶酶原激活物抑制剂-1具有抑制活性的药物，其包含作为活性成分的由以下通式（I）表示的化合物或其盐：其中R 1和R 2 表示可以被取代的芳基，W表示选自以下连接基团W-1中的基团：（其中左端的键与碳原子结合，右端的键与氮原子，X表示硫原子或NH，Y表示氧原子或硫原子，R 3表示烃基，羟基或羧基），Z表示单键或连接基团，其中主链中的原子数为1〜3。

2. 发明申请

US20100274051A1 INFLAMMATORY CYTOKINE RELEASE INHIBITOR 有权
标题翻译：炎性细胞因子释放抑制剂
公开(公告)号：US20100274051A1
公开(公告)日：2010-10-28
申请号：US12830018
申请日：2010-07-02
申请人： Susumu MUTO , Tatsuo Nagano , Tomomi Sotome , Akiko Itai
发明人： Susumu MUTO , Tatsuo Nagano , Tomomi Sotome , Akiko Itai
IPC分类号： C07C233/88
CPC分类号： C07D207/327 , A61K31/055 , A61K31/12 , A61K31/136 , A61K31/166 , A61K31/167 , A61K31/17 , A61K31/18 , A61K31/357 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/421 , A61K31/422 , A61K31/428 , A61K31/433 , A61K31/44 , A61K31/47 , A61K31/498 , A61K31/505 , A61K31/5375 , A61K31/695 , C07D209/08 , C07D209/34 , C07D209/42 , C07D209/80 , C07D209/88 , C07D213/64 , C07D213/65 , C07D213/75 , C07D215/12 , C07D215/38 , C07D231/40 , C07D239/22 , C07D241/44 , C07D263/48 , C07D277/24 , C07D285/08 , C07D321/10 , C07D333/16 , C07D333/38 , C07D413/14 , C07D471/04
摘要： A medicament having inhibitory activity against NF-κB activation, which comprises a compound represented by the following general formula (I) or α pharmacologically acceptable salt as an active ingredient: wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.
摘要翻译：一种具有对NF-κB活化的抑制活性的药物，其包含由以下通式（I）表示的化合物或α药理学上可接受的盐作为活性成分：其中X表示连接基团，A表示氢原子或乙酰基 E表示芳基或杂芳基，X表示芳烃或杂芳烃。

3. 发明授权

US08097759B2 Inflammatory cytokine release inhibitor 有权
标题翻译：炎性细胞因子释放抑制剂
公开(公告)号：US08097759B2
公开(公告)日：2012-01-17
申请号：US12830018
申请日：2010-07-02
申请人： Susumu Muto , Tatsuo Nagano , Tomomi Sotome , Akiko Itai
发明人： Susumu Muto , Tatsuo Nagano , Tomomi Sotome , Akiko Itai
IPC分类号： C07C233/64 , A61K31/166
CPC分类号： C07D207/327 , A61K31/055 , A61K31/12 , A61K31/136 , A61K31/166 , A61K31/167 , A61K31/17 , A61K31/18 , A61K31/357 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/421 , A61K31/422 , A61K31/428 , A61K31/433 , A61K31/44 , A61K31/47 , A61K31/498 , A61K31/505 , A61K31/5375 , A61K31/695 , C07D209/08 , C07D209/34 , C07D209/42 , C07D209/80 , C07D209/88 , C07D213/64 , C07D213/65 , C07D213/75 , C07D215/12 , C07D215/38 , C07D231/40 , C07D239/22 , C07D241/44 , C07D263/48 , C07D277/24 , C07D285/08 , C07D321/10 , C07D333/16 , C07D333/38 , C07D413/14 , C07D471/04
摘要： A medicament having inhibitory activity against NF-κB activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient: wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.
摘要翻译：一种具有对NF-κB活化的抑制活性的药物，其包含由以下通式（I）表示的化合物或药理学上可接受的盐作为活性成分：其中X表示连接基团，A表示氢原子或乙酰基 E表示芳基或杂芳基，X表示芳烃或杂芳烃。

4. 发明授权

US08263657B2 Inhibitors against the production and release of inflammatory cytokines 有权
标题翻译：抑制炎症细胞因子的产生和释放
公开(公告)号：US08263657B2
公开(公告)日：2012-09-11
申请号：US10433619
申请日：2001-12-18
申请人： Susumu Muto , Tatsuo Nagano , Tomomi Sotome , Akiko Itai
发明人： Susumu Muto , Tatsuo Nagano , Tomomi Sotome , Akiko Itai
IPC分类号： A01N37/12
CPC分类号： C07D207/327 , A61K31/055 , A61K31/12 , A61K31/136 , A61K31/166 , A61K31/167 , A61K31/17 , A61K31/18 , A61K31/357 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/421 , A61K31/422 , A61K31/428 , A61K31/433 , A61K31/44 , A61K31/47 , A61K31/498 , A61K31/505 , A61K31/5375 , A61K31/695 , C07D209/08 , C07D209/34 , C07D209/42 , C07D209/80 , C07D209/88 , C07D213/64 , C07D213/65 , C07D213/75 , C07D215/12 , C07D215/38 , C07D231/40 , C07D239/22 , C07D241/44 , C07D263/48 , C07D277/24 , C07D285/08 , C07D321/10 , C07D333/16 , C07D333/38 , C07D413/14 , C07D471/04
摘要： A medicament having inhibitory activity against NF-κB activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient: wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.
摘要翻译：一种具有对NF-κB活化的抑制活性的药物，其包含由以下通式（I）表示的化合物或药理学上可接受的盐作为活性成分：其中X表示连接基团，A表示氢原子或乙酰基 E表示芳基或杂芳基，X表示芳烃或杂芳烃。

5. 发明授权

US08633245B2 PAI-1 inhibitor 有权
标题翻译： PAI-1抑制剂
公开(公告)号：US08633245B2
公开(公告)日：2014-01-21
申请号：US12422099
申请日：2009-04-10
申请人： Youichi Yamaguchi , Takeshi Yanase , Susumu Muto , Akiko Itai
发明人： Youichi Yamaguchi , Takeshi Yanase , Susumu Muto , Akiko Itai
IPC分类号： A61K31/19 , C07C51/00
CPC分类号： C07C59/90 , C07C39/27 , C07C47/277 , C07C47/55 , C07C47/565 , C07C47/575 , C07C49/84 , C07C69/712 , C07C205/06 , C07C205/35 , C07C205/37 , C07C205/38 , C07C205/44 , C07C205/56 , C07C211/52 , C07C217/80 , C07C217/86 , C07C217/90 , C07C229/18 , C07C233/15 , C07C233/56 , C07C233/60 , C07C237/40 , C07C251/24 , C07C255/13 , C07C255/37 , C07C255/54 , C07C311/08 , C07C311/29 , C07C317/22 , C07C323/20 , C07C323/41 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2603/74 , C07D211/76 , C07D295/096 , C07D295/135 , C07D295/155 , C07D295/205 , C07D317/18 , C07D317/28 , C07F7/1804
摘要： The compound represented by the following formula (I) and the like have PAI-1 inhibition activity;wherein: R1 represents a C6-10 aryl group which may be substituted or the like; T represents a single bond or the like; m represents 0 or 1; when m is 0, G represents —N—C(═O)—CO2H or the like; when m is 1, G represents an oxygen atom or the like; R2 represents a C6-10 aryl group which may be substituted or the like; E represents the following formula (II) wherein one of R31, R32, R33 and R34 represents the formula R1-T-, each of the other three independently represents a hydrogen atom or the like, and R35 represents the formula —X—Y′, a hydrogen atom or the like; X represents —CH2— or the like; Y′ represents a carboxy group or the like; M represents a single bond or the like.
摘要翻译：由下式（I）等表示的化合物具有PAI-1抑制活性; 其中：R1表示可以被取代的C6-10芳基等; T表示单键等; m表示0或1; 当m为0时，G表示-N-C（= O）-CO 2 H等; 当m为1时，G表示氧原子等; R2表示可以被取代的C6-10芳基等; E表示式（II）中，R 31，R 32，R 33和R 34之一表示式R 1〜T，其余3个独立地表示氢原子等，R 35表示式-X-Y' ，氢原子等; X表示-CH 2 - 等; Y'表示羧基等; M表示单键等。

6. 发明申请

US20100234363A1 HETEROCYCLIC DERIVATIVE HAVING INHIBITORY ACTIVITY ON TYPE-I 11 DATA-HYDROXYSTEROID DEHYDROGENASE 审中-公开
标题翻译：具有I型11数据羟基脱氢酶抑制活性的杂环衍生物
公开(公告)号：US20100234363A1
公开(公告)日：2010-09-16
申请号：US12679159
申请日：2008-09-17
申请人： Akiko Itai , Susumu Muto , Ryuko Tokuyama , Hiroshi Fukasawa , Takeshi Yanase
发明人： Akiko Itai , Susumu Muto , Ryuko Tokuyama , Hiroshi Fukasawa , Takeshi Yanase
IPC分类号： A61K31/5415 , C07D279/08 , A61P3/10 , C07D265/24 , A61K31/536
CPC分类号： C07D279/06 , C07D265/24 , C07D279/08 , C07D417/04 , C07D417/12
摘要： Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor.A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein X is O or S, a broken line and a wavy line represent the presence or the absence of a bond, (i) when a broken line represents the presence of a bond, a wavy line represents the absence of a bond, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, (ii) when a broken line represents the absence of a bond, a wavy line represents the presence of a bond, R1 and R4 are each independently hydrogen, halogen or the like, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, and R5 and R6 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like.
摘要翻译：公开了可用作11-羟基类固醇脱氢酶1型抑制剂的化合物。由下式表示的化合物：其药学上可接受的盐或其溶剂合物，其中X为O或S，虚线和波浪线表示存在或不存在键，（i）当虚线表示键的存在，波浪线表示不存在键，R2和R3各自独立地为氢，卤素，氰基，羟基，羧基，任选取代的烷基，任选取代的烯基，任选取代的炔基等，（ii）当虚线表示不存在键，波浪线表示键的存在，R 1和R 4各自独立地为氢，卤素等，R 2和R 3各自独立地为氢，卤素，氰基，羟基，羧基，任选地取代的烷基，任选取代的烯基，任选取代的炔基等，R 5和R 6各自独立地为氢，任选取代的烷基，任选取代的烯基，任选取代的炔基等。

7. 发明申请

US20100113448A1 OXAZOLIDINONE DERIVATIVE HAVING INHIBITORY ACTIVITY ON 11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 失效
标题翻译：在11BETA-羟基脱氢酶脱氢酶1型上具有抑制活性的奥沙利酮衍生物
公开(公告)号：US20100113448A1
公开(公告)日：2010-05-06
申请号：US12594093
申请日：2008-03-27
申请人： Akiko Itai , Susumu Muto , Ryuko Tokuyama , Hiroshi Fukasawa , Takeshi Yanase
发明人： Akiko Itai , Susumu Muto , Ryuko Tokuyama , Hiroshi Fukasawa , Takeshi Yanase
IPC分类号： A61K31/421 , C07D413/12 , C07D263/24 , A61P3/10 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K31/496
CPC分类号： C07D263/20 , A61K31/421 , A61K31/422 , A61K31/4412 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , C07D413/12
摘要： Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor.A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(═O)— or —NR3S(═O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.
摘要翻译：公开了可用作11-羟基类固醇脱氢酶1型抑制剂的化合物。由下式表示的化合物：其药学上可接受的盐或其溶剂合物，其中R 1是任选取代的环烷基，任选取代的环烷基烷基，任选取代的杂环或任选取代的杂环烷基，X是-O-，-NR 3 - ， - NR 3 C（= O） - 或-NR 3 S（= O）2 - ，R 2是任选取代的芳基，任选取代的芳基烷基，任选取代的杂芳基或任选取代的杂芳基烷基，R 3是氢或任选取代的烷基。

8. 发明授权

US07700655B2 Antiallergic agents 失效
标题翻译：抗过敏剂
公开(公告)号：US07700655B2
公开(公告)日：2010-04-20
申请号：US11783324
申请日：2007-04-09
申请人： Susumu Muto , Akiko Itai
发明人： Susumu Muto , Akiko Itai
IPC分类号： A61K31/165
CPC分类号： C07D295/192 , A61K31/055 , A61K31/137 , A61K31/15 , A61K31/165 , A61K31/167 , A61K31/18 , A61K31/357 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/445 , A61K31/4453 , A61K31/455 , A61K31/47 , A61K31/498 , A61K31/5375 , A61K31/606 , A61K31/609 , A61K31/616 , A61K31/63 , C07C235/64
摘要： A medicament for the preventive and/or therapeutic treatment of allergic diseases and/or endometriosis and/or hysteromyoma which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substitutents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substitutents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above.
摘要翻译：一种用于预防和/或治疗过敏性疾病和/或子宫内膜异位症和/或子宫肌瘤的药物，其包含作为活性成分的选自以下通式（I）表示的化合物和药理学上可接受的物质其盐及其水合物及其溶剂化物：其中X表示主链中的原子数为2〜5的连接基（所述连接基可以被取代），A表示氢原子或乙酰基，E表示可以被取代的芳基或可以被取代的杂芳基，环Z表示可以具有一个或多个取代基的芳族，除了由式-OA表示的基团之外，其中A具有与上述相同的含义，由式-XE表示的基团，其中X和E各自具有与上述定义相同的含义，或可以具有一个或多个取代基的杂芳烃与式-O-A表示的基团的离子，其中A具有与上述相同的含义和由式-X-E表示的基团，其中X和E各自具有与上述相同的含义。

9. 发明授权

US07411076B2 Coumarin derivative 失效
标题翻译：香豆素衍生物
公开(公告)号：US07411076B2
公开(公告)日：2008-08-12
申请号：US10488254
申请日：2002-09-12
申请人： Susumu Muto , Masayuki Komukai , Akiko Itai
发明人： Susumu Muto , Masayuki Komukai , Akiko Itai
IPC分类号： C07D311/16 , C07D409/12 , C07D405/12 , C07C407/12
CPC分类号： C07D405/12 , A61K31/282 , A61K31/37 , A61K31/381 , A61K31/382 , A61K31/385 , A61K31/407 , A61K31/4433 , A61K31/675 , A61K31/704 , A61K31/7064 , A61K33/24 , A61K45/06 , C07D311/16 , C07D407/12 , C07D409/12
摘要： A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the following general formula (I): wherein X represents a single bond or a C1 to C6 alkylene group which may be substituted; A represents a C1 to C6 alkyl group which may be substituted, a C6 to C10 aryl group which may be substituted, or a 4 to 10-membered monocyclic or bicyclic and unsaturated, partly saturated, or completely saturated heterocyclic group which may be substituted, wherein said heterocyclic group comprises as ring-constituting atoms 1 to 4 hetero atoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom.
摘要翻译：一种用于增强基于DNA损伤作用模式的癌症治疗效果的药物，其包含作为活性成分的由以下通式（I）表示的化合物：其中X表示单键或C < 1可以被取代的C 6亚烷基; A表示可被取代的C 6〜C 6烷基，C 6〜C 10芳基的C 1〜可以被取代的基团，或可以被取代的4元至10元单环或双环和不饱和的，部分饱和的或完全饱和的杂环基，其中所述杂环基包含1-4个选自以下的杂原子：由氮原子，氧原子和硫原子组成的组。

10. 发明申请

US20070185110A1 Antiallergic agents 失效
标题翻译：抗过敏剂
公开(公告)号：US20070185110A1
公开(公告)日：2007-08-09
申请号：US11783324
申请日：2007-04-09
申请人： Susumu Muto , Akiko Itai
发明人： Susumu Muto , Akiko Itai
IPC分类号： A61K31/5375 , A61K31/445 , A61K31/40 , A61K31/165
CPC分类号： C07D295/192 , A61K31/055 , A61K31/137 , A61K31/15 , A61K31/165 , A61K31/167 , A61K31/18 , A61K31/357 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/445 , A61K31/4453 , A61K31/455 , A61K31/47 , A61K31/498 , A61K31/5375 , A61K31/606 , A61K31/609 , A61K31/616 , A61K31/63 , C07C235/64
摘要： A medicament for the preventive and/or therapeutic treatment of allergic diseases and/or endometriosis and/or hysteromyoma which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substitutents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substitutents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above.
摘要翻译：一种用于预防和/或治疗过敏性疾病和/或子宫内膜异位症和/或子宫肌瘤的药物，其包含作为活性成分的选自以下通式（I）表示的化合物和药理学上可接受的物质其盐及其水合物及其溶剂化物：其中X表示主链中的原子数为2〜5的连接基（所述连接基可以被取代），A表示氢原子或乙酰基，E表示可以被取代的芳基或可以被取代的杂芳基，环Z表示可以具有一个或多个取代基的芳族，除了由式-OA表示的基团之外，其中A具有与上述相同的含义，由式-XE表示的基团，其中X和E各自具有与上述相同的含义，或另外可以具有一个或多个取代基的杂芳烃与由式-O-A表示的基团，其中A具有与上述相同的含义和由式-X-E表示的基团，其中X和E各自具有与上述相同的含义。

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