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1. 发明申请

US20060252797A1 Receptor regulator 审中-公开
标题翻译：受体调节剂
公开(公告)号：US20060252797A1
公开(公告)日：2006-11-09
申请号：US10533833
申请日：2003-11-05
申请人： Masahiro Kajino , Shuji Hinuma , Naoki Tarui , Toshiro Yamashita , Yutaka Nakayama
发明人： Masahiro Kajino , Shuji Hinuma , Naoki Tarui , Toshiro Yamashita , Yutaka Nakayama
IPC分类号： A61K31/4545 , A61K31/454 , C07D401/02 , C07D417/02
CPC分类号： C07D401/04 , A61K31/4468 , A61K31/454 , A61K31/4545 , C07D211/58 , C07D211/66 , C07D401/06 , C07D409/14 , C07D417/04 , C07D417/14
摘要： A compound having a partial structure represented by the formula (A) (wherein ring Xa represents a nitrogen-containing ring and R represents optionally substituted amino) or a salt thereof. The compound or salt is highly effective in regulating neuromedin U receptors and is useful as a preventive/therapeutic agent for hypertension, etc.
摘要翻译：具有由式（A）表示的部分结构的化合物（其中环Xa表示含氮环，R表示任选取代的氨基）或其盐。该化合物或盐在调节神经介肽U受体方面非常有效，并且可用作高血压等的预防/治疗剂。

2. 发明申请

US20090270625A1 FUSED QUINOLINE DERIVATIVE AND USE THEREOF 失效
标题翻译：熔融喹啉衍生物及其用途
公开(公告)号：US20090270625A1
公开(公告)日：2009-10-29
申请号：US12476619
申请日：2009-06-02
申请人： Masahiro Kajino , Nicholas William Hird , Naoki Tarui , Hiroshi Banno , Yasuhiko Kawano , Nobuhiro Inatomi
发明人： Masahiro Kajino , Nicholas William Hird , Naoki Tarui , Hiroshi Banno , Yasuhiko Kawano , Nobuhiro Inatomi
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein R1 is a hydrogen atom and the like; R2 is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R3 is unsubstituted (i.e., absence), a hydrogen atom and the like; R4 and R5 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R6 is (cyclic group optionally having substituent(s))-carbonyl, and the like; R7, R8, R9 and R10 are the same or different and each is a hydrogen atom, halogen and the like; or R7 and R8, R8 and R9, and R9 and R10 may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5; — --- represents unsubstituted (i.e., absence) or a single bond; and represents a single bond or a double bond, or a salt thereof, and the like.
摘要翻译：本发明旨在提供具有神经激肽2（NK2）受体拮抗作用的喹啉衍生物，其涉及式（I）表示的化合物，其中R1为氢原子等; R2是氢原子，任选具有取代基的烃基等; R3是未取代的（即不存在），氢原子等; R 4和R 5相同或不同，各自为氢原子，任选具有取代基的烃基等; R6是（任选具有取代基的环状基团） - 羰基等; R 7，R 8，R 9和R 10相同或不同，各自为氢原子，卤素等; 或R 7和R 8，R 8和R 9，并且R 9和R 10可与相邻碳原子一起形成环; n为1〜5的整数， ---表示未取代（即不存在）或单键; ＆lt; img id =“CUSTOM-CHARACTER-00001”he =“2.79mm”wi =“7.03mm”file =“US20090270625A1-20091029-P00001.TIF”img-content =“character”img-format =“tif”/ >表示单键或双键，或其盐等。

3. 发明申请

US20090258893A1 FUSED QUINOLINE DERIVATIVE AND USE THEREOF 失效
标题翻译：熔融喹啉衍生物及其用途
公开(公告)号：US20090258893A1
公开(公告)日：2009-10-15
申请号：US12476626
申请日：2009-06-02
申请人： Masahiro Kajino , Nicholas William Hird , Naoki Tarui , Hiroshi Banno , Yasuhiko Kawano , Nobuhiro Inatomi
发明人： Masahiro Kajino , Nicholas William Hird , Naoki Tarui , Hiroshi Banno , Yasuhiko Kawano , Nobuhiro Inatomi
IPC分类号： A61K31/437 , C07D471/04 , A61P1/00
CPC分类号： C07D471/04
摘要： The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein R1 is a hydrogen atom and the like; R2 is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R3 is unsubstituted (i.e., absence), a hydrogen atom and the like; R4 and R5 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R6 is (cyclic group optionally having substituent(s))-carbonyl, and the like; R7, R8, R9 and R10 are the same or different and each is a hydrogen atom, halogen and the like; or R7 and R8, R8 and R9, and R9 and R10 may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5; represents unsubstituted (i.e., absence) or a single bond; and represents a single bond or a double bond, or a salt thereof, and the like.
摘要翻译：本发明旨在提供具有神经激肽2（NK2）受体拮抗作用的喹啉衍生物，其涉及式（I）表示的化合物，其中R1为氢原子等; R2是氢原子，任选具有取代基的烃基等; R3是未取代的（即不存在），氢原子等; R 4和R 5相同或不同，各自为氢原子，任选具有取代基的烃基等; R6是（任选具有取代基的环状基团） - 羰基等; R 7，R 8，R 9和R 10相同或不同，各自为氢原子，卤素等; 或R 7和R 8，R 8和R 9，并且R 9和R 10可与相邻碳原子一起形成环; n为1〜5的整数， “img id =”CUSTOM-CHARACTER-00001“he =”0.68mm“wi =”3.13mm“file =”US20090258893A1-20091015-P00001.TIF“img-content =”character“img-format =”tif“/> 表示未取代的（即不存在）或单键; ＆lt; img id =“CUSTOM-CHARACTER-00002”he =“1.02mm”wi =“3.13mm”file =“US20090258893A1-20091015-P00002.TIF”img-content =“character”img-format =“tif”/ >表示单键或双键，或其盐等。

4. 发明申请

US20080139639A1 Proton Pump Inhibitors 有权
标题翻译：质子泵抑制剂
公开(公告)号：US20080139639A1
公开(公告)日：2008-06-12
申请号：US11664346
申请日：2005-09-30
申请人： Masahiro Kajino , Atsushi Hasuoka , Naoki Tarui , Terufumi Takagi
发明人： Masahiro Kajino , Atsushi Hasuoka , Naoki Tarui , Terufumi Takagi
IPC分类号： A61K31/40 , C07D207/48 , A61P1/04
CPC分类号： C07D207/48 , A61K31/4025 , A61K31/41 , A61K31/4439 , A61K31/501 , A61K31/506 , C07D207/335 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/12 , C07D487/04
摘要： A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof. or a prodrug thereof is provided.
摘要翻译：一种质子泵抑制剂，其含有式（I）表示的化合物，其中X和Y相同或不同，并且各自是主链中具有1至20个碳原子的键或间隔基，R 1 >是任选取代的烃基或任选取代的杂环基，R 2，R 3和R 4相同或不同，并且各自任选取代的苯并[b]噻吩基，任选取代的呋喃基，任意取代的吡啶基，任意取代的吡唑基，任意取代的嘧啶基，酰基，卤素原子，氰基或硝基，R 5和R 6相同或不同，各自为氢原子或任选地取代烃基，其具有优异的质子泵作用，并显示出抗溃疡活性等转化为体内的质子泵抑制剂或其盐。或其前药。

5. 发明申请

US20080039452A1 Fused Quinoline Derivative and Use Thereof 失效
标题翻译：熔融喹啉衍生物及其用途
公开(公告)号：US20080039452A1
公开(公告)日：2008-02-14
申请号：US11587788
申请日：2005-04-28
申请人： Masahiro Kajino , Nicholas Hird , Naoki Tarui , Hiroshi Banno , Yasuhiko Kawano , Nobuhiro Inatomi
发明人： Masahiro Kajino , Nicholas Hird , Naoki Tarui , Hiroshi Banno , Yasuhiko Kawano , Nobuhiro Inatomi
IPC分类号： A61K31/535 , A61P1/00 , C07D471/00
CPC分类号： C07D471/04
摘要： The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein R1 is a hydrogen atom and the like; R2 is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R3 is unsubstituted (i.e., absence), a hydrogen atom and the like; R4 and R5 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R6 is (cyclic group optionally having substituent(s))-carbonyl, and the like; R7, R8, R9 and R10 are the same or different and each is a hydrogen atom, halogen and the like; or R7 and R8, R8 and R9, and R9 and R10 may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5; --- represents unsubstituted (i.e., absence) or a single bond; and represents a single bond or a double bond, or a salt thereof, and the like.
摘要翻译：本发明旨在提供具有神经激肽2（NK2）受体拮抗作用的喹啉衍生物，其涉及式（I）表示的化合物，其中R 1为氢原子等; R 2是氢原子，任选具有取代基的烃基等; R 3是未取代的（即不存在），氢原子等; R 4和R 5相同或不同，各自为氢原子，任选具有取代基的烃基等; R 6是（任选具有取代基的环状基团） - 羰基等; R 7，R 8，R 9和R 10相同或不同，各自为氢原子，卤素等; 或R 7和R 8，R 8和R 9和R 9和/或 >和R 10可以与相邻的碳原子一起形成环; n为1〜5的整数， ---表示未取代（即不存在）或单键; “img id =”custom-character-00001“he =”2.79mm“wi =”4.57mm“file =”US20080039452A1-20080214-P00900.TIF“img-content =”character“img-format =”tif“/ >表示单键或双键，或其盐等。

6. 发明申请

US20110028476A1 PROTON PUMP INHIBITORS 审中-公开
标题翻译： PROTON PUMP抑制剂
公开(公告)号：US20110028476A1
公开(公告)日：2011-02-03
申请号：US12873971
申请日：2010-09-01
申请人： Masahiro Kajino , Atsushi Hasuoka , Naoki Tarui , Terufumi Takagi
发明人： Masahiro Kajino , Atsushi Hasuoka , Naoki Tarui , Terufumi Takagi
IPC分类号： A61K31/5377 , C07D207/48 , A61K31/40 , C07D409/12 , A61K31/4025 , C07D403/12 , A61K31/506 , C07D401/12 , A61K31/4439 , C07D405/12 , C07D417/12 , A61K31/428 , A61K31/4178 , C07D403/04 , A61K31/4155 , C07D487/04 , A61K31/519 , A61K31/501 , C07D413/12 , A61P1/00
CPC分类号： C07D207/48 , A61K31/4025 , A61K31/41 , A61K31/4439 , A61K31/501 , A61K31/506 , C07D207/335 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/12 , C07D487/04
摘要： A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof. or a prodrug thereof is provided.
摘要翻译：一种含有式（I）表示的化合物的质子泵抑制剂，其中X和Y相同或不同，并且各自是主链中的键或具有1至20个碳原子的间隔基，R 1是任选取代的烃基或任选取代的杂环基，R 2，R 3和R 4相同或不同，各自为氢原子，任选取代的烃基，任选取代的噻吩基，任选取代的苯并[b]噻吩基，任选取代的呋喃基，任选取代的吡啶基，任选取代的吡唑基，任选取代的嘧啶基，酰基，卤素原子，氰基或硝基，R 5和R 6相同或不同，各自为氢原子或任选取代的烃基，其具有优异的质子泵作用，并且在体内转化为质子泵抑制剂之后显示出抗溃疡活性等，或其中的盐的。或其前药。

7. 发明申请

US20090275568A1 FUSED QUINOLINE DERIVATIVE AND USE THEREOF 审中-公开
标题翻译：熔融喹啉衍生物及其用途
公开(公告)号：US20090275568A1
公开(公告)日：2009-11-05
申请号：US12498629
申请日：2009-07-07
申请人： Masahiro Kajino , Nicholas William Hird , Naoki Tarui , Hiroshi Banno , Yasuhiko Kawano , Nobuhiro Inatomi
发明人： Masahiro Kajino , Nicholas William Hird , Naoki Tarui , Hiroshi Banno , Yasuhiko Kawano , Nobuhiro Inatomi
IPC分类号： A61K31/437 , C07D471/04 , C07D413/14 , C07D417/14 , A61K31/5377 , A61K31/538 , A61K31/541 , A61P1/00 , A61P25/24
CPC分类号： C07D471/04
摘要： The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein R1 is a hydrogen atom and the like; R2 is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R3 is unsubstituted (i.e., absence), a hydrogen atom and the like; R4 and R5 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R6 is (cyclic group optionally having substituent(s))-carbonyl, and the like; R7, R8, R9 and R10 are the same or different and each is a hydrogen atom, halogen and the like; or R7 and R8, R8 and R9, and R9 and R10 may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5; represents unsubstituted (i.e., absence) or a single bond; and represents a single bond or a double bond, or a salt thereof, and the like.
摘要翻译：本发明旨在提供具有神经激肽2（NK2）受体拮抗作用的喹啉衍生物，其涉及式（I）表示的化合物，其中R1为氢原子等; R2是氢原子，任选具有取代基的烃基等; R3是未取代的（即不存在），氢原子等; R 4和R 5相同或不同，各自为氢原子，任选具有取代基的烃基等; R6是（任选具有取代基的环状基团） - 羰基等; R 7，R 8，R 9和R 10相同或不同，各自为氢原子，卤素等; 或R 7和R 8，R 8和R 9，并且R 9和R 10可与相邻碳原子一起形成环; n为1〜5的整数，表示未取代的（即不存在）或单键; ＆lt; img id =“CUSTOM-CHARACTER-00002”he =“2.46mm”wi =“4.23mm”file =“US20090275568A1-20091105-P00002.TIF”img-content =“character”img-format =“tif”/ >表示单键或双键，或其盐等。

8. 发明申请

US20050032786A1 1, 3-benzothiazinone derivatives and use thereof 有权
标题翻译： 1,3-苯并噻嗪酮衍生物及其用途
公开(公告)号：US20050032786A1
公开(公告)日：2005-02-10
申请号：US10488384
申请日：2002-09-02
申请人： Masahiro Kajino , Akira Kawada , Yutaka Nakayama , Haruhide Kimura
发明人： Masahiro Kajino , Akira Kawada , Yutaka Nakayama , Haruhide Kimura
IPC分类号： A61K31/5415 , A61P1/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P13/12 , A61P17/00 , A61P19/00 , A61P19/02 , A61P25/00 , A61P31/00 , A61P43/00 , C07D417/04 , C07D417/14 , C07D279/16
CPC分类号： C07D417/04 , A61K31/5415 , C07D417/14
摘要： This invention provides a compound represented by the formula (I): wherein R1 is a hydrogen atom, a halogen atom, hydroxy, nitro, optionally halogenated alkyl, alkoxy optionally having substituents, acyl or amino optionally having substituents; R2 is pyridyl, furyl, thienyl, pyrrolyl, quinolyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolyl, tetrahydroquinolyl or thiazolyl, each of which may have substituents; n is 1 or 2; or a salt. And this invention provides a safe pharmaceutical comprising the compound of the formula (I), which has an excellent apoptosis inhibitory effect and MIF binding effect, for preventing and/or treating heart disease, nervous degenerative disease, cerebrovascular disease, central nervous infectious disease, traumatorathy, demyelinating disease, bone and articular disease, kidney disease, liver disease, osteomyelodysplasia, AIDS, cancer, and the like.
摘要翻译：本发明提供由式（I）表示的化合物：其中R 1为氢原子，卤素原子，羟基，硝基，任选卤代烷基，任选具有取代基的烷氧基，任选具有取代基的酰基或氨基; R 2是吡啶基，呋喃基，噻吩基，吡咯基，喹啉基，吡嗪基，嘧啶基，哒嗪基，吲哚基，四氢喹啉基或噻唑基，其各自可以具有取代基; n为1或2; 或盐。本发明提供一种安全药物，其包含具有优异的细胞凋亡抑制作用和MIF结合作用的式（I）化合物，用于预防和/或治疗心脏病，神经退行性疾病，脑血管病，中枢神经感染性疾病，外伤，脱髓鞘疾病，骨和关节疾病，肾脏疾病，肝病，骨发育不良，艾滋病，癌症等。

9. 发明授权

US07659267B2 1,3-Benzothiazinone derivatives, process for producing the same use thereof 失效
标题翻译： 1,3-苯并噻嗪酮衍生物，其制备方法相同
公开(公告)号：US07659267B2
公开(公告)日：2010-02-09
申请号：US10537520
申请日：2003-12-04
申请人： Masahiro Kajino , Yutaka Nakayama , Haruhide Kimura
发明人： Masahiro Kajino , Yutaka Nakayama , Haruhide Kimura
IPC分类号： C07D279/16 , A61K31/5415
CPC分类号： C07D263/58 , A61K31/5415 , C07D279/08
摘要： As prophylactic and/or therapeutic agents for cardiovascular diseases, bone or joint diseases, infectious diseases, inflammatory diseases, kidney diseases, etc. having safe and excellent effects of cell death inhibition, MIF binding, etc., there are provided compounds represented by formula: [wherein, R1 represents a halogen atom, etc., R2 represents a group represented by formula: (wherein, R3 represents hydrogen atom, an optionally substituted alkoxy, etc., R4 represents hydrogen atom, bromine atom, cyano, etc., R5 represents hydrogen atom, hydroxy, etc., R6 represents hydrogen atom, etc., R7 represents hydrogen atom, etc.) etc., and n represents an integer of 0 to 4] or salts thereof.
摘要翻译：作为具有安全且优异的细胞死亡抑制作用，MIF结合等的心血管疾病，骨或关节疾病，感染性疾病，炎性疾病，肾脏疾病等的预防和/或治疗剂，提供了式 [其中，R1表示卤素原子等，R2表示由式（其中R3表示氢原子，任选取代的烷氧基等，R4表示氢原子，溴原子，氰基等）表示的基团， R5表示氢原子，羟基等，R6表示氢原子等，R7表示氢原子等）等，n表示0〜4的整数]或其盐。

10. 发明申请

US20090082343A1 1,3-BENZOTHIAZINONE DERIVATIVES AND USE THEREOF 有权
标题翻译： 1,3-苯并噻嗪酮衍生物及其用途
公开(公告)号：US20090082343A1
公开(公告)日：2009-03-26
申请号：US12099779
申请日：2008-04-08
申请人： Masahiro Kajino , Yutaka Nakayama , Akira Kawada , Haruhide Kimura , Taisuke Tawaraishi
发明人： Masahiro Kajino , Yutaka Nakayama , Akira Kawada , Haruhide Kimura , Taisuke Tawaraishi
IPC分类号： A61K31/5415 , C07D401/04 , A61P9/00 , A61P1/00
CPC分类号： C07D417/04 , A61K31/5415 , C07D417/14
摘要： This invention provides a compound represented by the formula (I): wherein R1 is a hydrogen atom, a halogen atom, hydroxy, nitro, optionally halogenated alkyl, alkoxy optionally having substituents, acyl or amino optionally having substituents; R2 is pyridyl, furyl, thienyl, pyrrolyl, quinolyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolyl, tetrahydroquinolyl or thiazolyl, each of which may have substituents; n is 1 or 2; or a salt. And this invention provides a safe pharmaceutical comprising the compound of the formula (I), which has an excellent apoptosis inhibitory effect and MIF binding effect, for preventing and/or treating heart disease, nervous degenerative disease, cerebrovascular disease, central nervous infectious disease, traumatorathy, demyelinating disease, bone and articular disease, kidney disease, liver disease, osteomyelodysplasia, AIDS, cancer, and the like.
摘要翻译：本发明提供由式（I）表示的化合物：其中R1是氢原子，卤素原子，羟基，硝基，任选卤代烷基，任选具有取代基的烷氧基，任选具有取代基的酰基或氨基; R 2是可以具有取代基的吡啶基，呋喃基，噻吩基，吡咯基，喹啉基，吡嗪基，嘧啶基，哒嗪基，吲哚基，四氢喹啉基或噻唑基。 n为1或2; 或盐。本发明提供了一种安全药物，其包含具有优异的细胞凋亡抑制作用和MIF结合作用的式（I）化合物，用于预防和/或治疗心脏病，神经退行性疾病，脑血管病，中枢神经感染性疾病，外伤，脱髓鞘疾病，骨和关节疾病，肾脏疾病，肝病，骨发育不良，艾滋病，癌症等。

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