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1. 发明申请

US20070117840A1 Receptor antagonist 审中-公开
标题翻译：受体拮抗剂
公开(公告)号：US20070117840A1
公开(公告)日：2007-05-24
申请号：US10549889
申请日：2004-03-16
申请人： Fumio Itoh , Shuji Hinuma , Naoyuki Kanzaki , Yoshihiro Banno , Hiromi Yoshida , Hirokazu Matsumoto
发明人： Fumio Itoh , Shuji Hinuma , Naoyuki Kanzaki , Yoshihiro Banno , Hiromi Yoshida , Hirokazu Matsumoto
IPC分类号： A61K31/4704
CPC分类号： A61K31/4704
摘要： A compound represented by the formula (I): wherein ring A represents an aromatic ring; X represents a bond, oxygen, NR4 (R4 represents hydrogen, a hydrocarbon group, or a heterocyclic group), or alkylene; R1 represents a hydrocarbon group, or a heterocyclic group; R2 represents —COYR5 (Y represents a bond, alkylene, oxygen, sulfur, or NR6 (R6 represents hydrogen, a hydrocarbon group, or a heterocyclic group), and R5 represents a hydrocarbon group, or a heterocyclic group), a hydrocarbon group, or a heterocyclic group; and R3 represents a hydrocarbon group, a heterocyclic group, optionally substituted hydroxy, optionally substituted amino, or —S(O)nR7 (R7 represents a hydrocarbon group, or a heterocyclic group, and n is 0 to 2), a salt of the compound, or a prodrug or either is useful as an agent for modulating the function of an RFRP receptor.
摘要翻译：由式（I）表示的化合物：其中环A表示芳环; X表示键，氧，NR 4（R 4表示氢，烃基或杂环基）或亚烷基; R 1表示烃基或杂环基; R 2表示-COYR 5（Y表示键，亚烷基，氧，硫或NR 6（R 6） SUP>表示氢，烃基或杂环基），R 5表示烃基或杂环基），烃基或杂环基; 和R 3表示烃基，杂环基，任选取代的羟基，任选取代的氨基或-S（O）n R 7 （R 7表示烃基或杂环基，n为0〜2），化合物或前药的盐或其可用作调节其功能的试剂 RFRP受体。

2. 发明申请

US20090239839A1 RECEPTOR ANTAGONIST 审中-公开
标题翻译：受体拮抗剂
公开(公告)号：US20090239839A1
公开(公告)日：2009-09-24
申请号：US12391520
申请日：2009-02-24
申请人： Fumio ITOH , Shuji Hinuma , Naoyuki Kanzaki , Hiroshi Mabuchi , Hiromi Yoshida , Hirokazu Matsumoto , Takeshi Wakabayashi
发明人： Fumio ITOH , Shuji Hinuma , Naoyuki Kanzaki , Hiroshi Mabuchi , Hiromi Yoshida , Hirokazu Matsumoto , Takeshi Wakabayashi
IPC分类号： A61K31/553 , A61P25/04
CPC分类号： C07D267/08
摘要： An agent for modulating the function of an RFRP receptor, characterized by containing either a compound represented by the formula (I) [wherein ring A represents an optionally substituted aromatic ring; ring B represents an optionally substituted benzene ring; X represents oxygen, S(O)n (n is an integer of 0 to 2), or NR3 (R3 represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group); and R1 and R2 each represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group] or a salt of the compound.
摘要翻译：用于调节RFRP受体功能的试剂，其特征在于含有由式（I）表示的化合物[其中环A表示任选取代的芳环; 环B表示任选取代的苯环; X表示氧，S（O）n（n为0〜2的整数）或NR 3（R 3表示氢，任选取代的烃基或任意取代的杂环基）。并且R 1和R 2各自表示氢，任选取代的烃基或任选取代的杂环基]或该化合物的盐。

3. 发明申请

US20070129348A1 Receptor antagonist 审中-公开
标题翻译：受体拮抗剂
公开(公告)号：US20070129348A1
公开(公告)日：2007-06-07
申请号：US10553273
申请日：2004-04-15
申请人： Fumio Itoh , Shuji Hinuma , Naoyuki Kanzaki , Hiroshi Mabuchi , Hiromi Yoshida , Hirokazu Matsumoto , Takeshi Wakabayashi
发明人： Fumio Itoh , Shuji Hinuma , Naoyuki Kanzaki , Hiroshi Mabuchi , Hiromi Yoshida , Hirokazu Matsumoto , Takeshi Wakabayashi
IPC分类号： A61K31/554 , A61K31/553 , A61K31/5513
CPC分类号： C07D267/08
摘要： An agent for modulating the function of an RFRP receptor, characterized by containing either a compound represented by the formula (I) [wherein ring A represents an optionally substituted aromatic ring; ring B represents an optionally substituted benzene ring; X represents oxygen, S(O)n (n is an integer of 0 to 2), or NR3 (R3 represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group); and R1 and R2 each represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group] or a salt of the compound.
摘要翻译：用于调节RFRP受体功能的试剂，其特征在于含有由式（I）表示的化合物[其中环A表示任选取代的芳环; 环B表示任选取代的苯环; X表示氧，S（O）n N（n为0〜2的整数）或NR 3（R 3）表示氢，任选取代的烃基或任选取代的杂环基）; 和R 1和R 2各自表示氢，任选取代的烃基或任选取代的杂环基]或该化合物的盐。

4. 发明申请

US20060199795A1 Receptor agonists 失效
标题翻译：受体激动剂
公开(公告)号：US20060199795A1
公开(公告)日：2006-09-07
申请号：US10543997
申请日：2004-01-27
申请人： Fumio Itoh , Shuji Hinuma , Naoyuki Kanzaki , Takashi Miki , Yuji Kawamata , Satoru Oi , Taisuke Tawaraishi , Yuji Ishichi , Mariko Hirohashi
发明人： Fumio Itoh , Shuji Hinuma , Naoyuki Kanzaki , Takashi Miki , Yuji Kawamata , Satoru Oi , Taisuke Tawaraishi , Yuji Ishichi , Mariko Hirohashi
IPC分类号： A61K31/554 , A61K31/553 , A61K31/5513
CPC分类号： C07D267/14 , A61K31/4353 , A61K31/5513 , A61K31/553
摘要： The present invention provides a TGR5 receptor agonist comprising a fused ring compound represented by the formula wherein ring A is an optionally substituted aromatic ring; and ring B′ is a 5- to 8-membered ring having one or more substituents or a salt thereof or a prodrug thereof, which is useful for the treatment of various diseases.
摘要翻译：本发明提供一种TGR5受体激动剂，其包含由下式表示的稠环化合物：其中环A为任选取代的芳环; 环B'是具有一个或多个取代基的5-至8-元环或其盐或其前药，其可用于治疗各种疾病。

5. 发明授权

US07625887B2 Receptor agonists 失效
标题翻译：受体激动剂
公开(公告)号：US07625887B2
公开(公告)日：2009-12-01
申请号：US10543997
申请日：2004-01-27
申请人： Fumio Itoh , Shuji Hinuma , Naoyuki Kanzaki , Yuji Kawamata , Taisuke Tawaraishi , Yuji Ishichi , Mariko Hirohashi
发明人： Fumio Itoh , Shuji Hinuma , Naoyuki Kanzaki , Yuji Kawamata , Taisuke Tawaraishi , Yuji Ishichi , Mariko Hirohashi
IPC分类号： A61K31/553 , A61K45/00 , C07D267/22 , C07D281/02
CPC分类号： C07D267/14 , A61K31/4353 , A61K31/5513 , A61K31/553
摘要： It is intended to provide a TGR5 receptor agonist containing a fused ring compound represented by the following general formula, its salt or a prodrug thereof: (1) wherein ring A represents an optionally substituted aromatic ring; and the ring B′ represents a 5- to 8-membered ring having one or more substituents; which is useful in treating various diseases.
摘要翻译：本发明提供一种TGR5受体激动剂，其含有下述通式表示的稠环化合物，其盐或其前药：（1）其中环A表示任选取代的芳环; 环B'表示具有一个或多个取代基的5-至8-元环; 其用于治疗各种疾病。

6. 发明授权

US08741943B2 Bicyclic compound, production and use thereof 有权
标题翻译：双环化合物，其生产和使用
公开(公告)号：US08741943B2
公开(公告)日：2014-06-03
申请号：US13476454
申请日：2012-05-21
申请人： Mitsuru Shiraishi , Masanori Baba , Katsuji Aikawa , Naoyuki Kanzaki , Masaki Seto , Yuji Iizawa
发明人： Mitsuru Shiraishi , Masanori Baba , Katsuji Aikawa , Naoyuki Kanzaki , Masaki Seto , Yuji Iizawa
IPC分类号： C07D403/02 , A61K31/4178
CPC分类号： A61K31/4196 , A61K31/395 , A61K31/4178 , C07D225/06 , C07D313/20 , C07D403/12 , C07D405/12 , C07D407/12
摘要： The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
摘要翻译：本发明提供具有CCR拮抗剂活性，特别是CCR5拮抗剂活性的新的环状化合物及其用途。本发明化合物由下式表示：其中，R 1为可被取代的5-至6-元环基; X1是债券等; 环A是可以被取代的5至6元环基团; 环B是可以被取代的8至10元环基团; X 2是1至4个原子的二价基团; Z1是二价环状环基等; Z2是键或类似物; R 2为氨基，可以被取代的含氮杂环基等，或其盐。

7. 发明授权

US07132547B2 Preventives/remedies for urinary disturbance 有权
公开(公告)号：US07132547B2
公开(公告)日：2006-11-07
申请号：US10500217
申请日：2002-12-26
申请人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
发明人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
IPC分类号： C07D235/24
CPC分类号： A61K31/00 , A61K31/138 , A61K31/40 , A61K31/445 , A61K31/473 , A61K31/549 , A61K31/55 , A61K31/553 , C07C233/41 , C07C311/07 , C07C311/08 , C07C311/37 , C07C2602/08 , C07D209/08 , C07D209/14 , C07D209/48 , C07D211/32 , C07D215/227 , C07D217/04 , C07D217/06 , C07D217/08 , C07D223/16 , C07D235/26 , C07D239/80 , C07D265/36 , C07D285/14 , C07D285/22 , C07D307/78 , C07D307/79 , C07D311/58 , C07D319/18 , C07D333/22 , C07D471/06 , C07D513/06 , G01N2333/91215
摘要： Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an α1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.

8. 发明申请

US20060178359A1 Tricyclic compound, process for producing the same, and use 审中-公开
标题翻译：三环化合物，其制备方法和用途
公开(公告)号：US20060178359A1
公开(公告)日：2006-08-10
申请号：US10544470
申请日：2004-02-05
申请人： Mitsuru Shiraishi , Masaki Seto , Katsuji Aikawa , Naoyuki Kanzaki , Masanori Baba
发明人： Mitsuru Shiraishi , Masaki Seto , Katsuji Aikawa , Naoyuki Kanzaki , Masanori Baba
IPC分类号： A61K31/55 , A61K31/4745 , C07D487/14
CPC分类号： C07D471/04 , A61K31/4353 , A61K31/55
摘要： A compound of the formula: wherein R1 is a 5- or 6-membered ring; Z1 is a 5- or 6-membered aromatic ring; Z2 is a group -Z2a-W2-Z2b-, wherein Z2a and Z2b are each O, S(O)q (wherein q is 0, 1 or 2), an imino group, or a bond; and W2 is an alkylene chain; W is a group represented by wherein R3 and R3′ are each a hydrogen atom, a lower alkyl group, or a lower alkoxy group; X is CH or N; n and n′ are each an integer of 0 or 1 to 4; m and m′ are each 1 or 2; Y is O, S(O)p (wherein p is 0, 1 or 2), CH2 or NR4 (wherein R4 is a hydrogen atom, a lower alkyl group, or a lower acyl group); and R2 is (1) an amino group, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide, or (2) a nitrogen-containing heterocyclic group which may contain a sulfur atom or an oxygen atom as the ring-constituting atom, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide; or a salt thereof. The compound exhibits excellent CCR antagonist activity against CCR5, and is useful as a prophylactic and/or therapeutic agent for HIV infection in human peripheral blood mononuclear cells, especially for AIDS.
摘要翻译：下式的化合物：其中R 1是5或6元环; Z 1是5或6元芳环; Z 2是基团-Z 2 O 2 -W 2 -Z 2b 2，其中Z 2a 和/或O 2各自为O，S（O）q q（其中q为0,1或2），亚氨基或键; 和W 2是亚烷基链; W是由R 3和R 3'表示的基团各自为氢原子，低级烷基或低级烷氧基; X是CH或N; n和n'各自为0或1〜4的整数; m和m'分别为1或2; Y是O，S（O）p（其中p是0,1或2），CH 2或NR 4（其中R' SUP> 4 是氢原子，低级烷基或低级酰基）; R 2是（1）可以将氮原子转化为季铵或氧化物的氨基，或者（2）可含有硫原子的含氮杂环基或氧原子作为构成环的原子，其中氮原子可以转化为季铵或氧化物; 或其盐。该化合物对CCR5表现出优异的CCR拮抗剂活性，并且可用作人外周血单核细胞（特别是AIDS）中HIV感染的预防和/或治疗剂。

9. 发明申请

US20060135566A1 5-pyridyl-1,3-azole compounds, process for producing the same and use thereof 失效
标题翻译： 5-吡啶基-1,3-唑化合物，其制备方法及其用途
公开(公告)号：US20060135566A1
公开(公告)日：2006-06-22
申请号：US11354897
申请日：2006-02-16
申请人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
发明人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
IPC分类号： A61K31/4439 , C07D417/04 , C07D413/04
CPC分类号： C07D417/14 , C07D417/04
摘要： An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-α inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-α.
摘要翻译：由下式表示的任选的N-氧化化合物：其中R 1表示氢，烃，杂环，氨基，酰基，R 2表示芳族基团， 3表示氢，吡啶基，芳香烃，X表示氧，任选氧化的硫，Y表示键，氧，任选氧化的硫，由式NR 4表示的基团（R 4代表氢，烃或酰基），Z表示键或二价无环烃，或其盐具有优异的腺苷A 3受体拮抗活性，并用作用于预防或治疗与腺苷A 3受体相关的疾病的药剂。此外，化合物（I）或其盐具有p38 MAP激酶抑制活性和TNF-α抑制活性，并且用作预防或治疗与p38 MAP激酶相关的疾病和与TNF-α相关的疾病的药剂。

10. 发明申请

US20060063769A1 Preventives/remedies for urinary disturbance 有权
标题翻译：预防/治疗尿路障碍
公开(公告)号：US20060063769A1
公开(公告)日：2006-03-23
申请号：US10500217
申请日：2002-12-26
申请人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
发明人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
IPC分类号： A61K31/517 , A61K31/454
CPC分类号： A61K31/00 , A61K31/138 , A61K31/40 , A61K31/445 , A61K31/473 , A61K31/549 , A61K31/55 , A61K31/553 , C07C233/41 , C07C311/07 , C07C311/08 , C07C311/37 , C07C2602/08 , C07D209/08 , C07D209/14 , C07D209/48 , C07D211/32 , C07D215/227 , C07D217/04 , C07D217/06 , C07D217/08 , C07D223/16 , C07D235/26 , C07D239/80 , C07D265/36 , C07D285/14 , C07D285/22 , C07D307/78 , C07D307/79 , C07D311/58 , C07D319/18 , C07D333/22 , C07D471/06 , C07D513/06 , G01N2333/91215
摘要： Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an α1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.
摘要翻译：含有具有乙酰胆碱酯酶抑制作用的化合物和α1拮抗作用的化合物的预防/补救措施，其显示出改善膀胱尿功能的优异效果（即，改善尿流率和排尿效率的效果）而不影响尿压或血压。

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