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公开(公告)号：US20050032786A1
公开(公告)日：2005-02-10
申请号：US10488384
申请日：2002-09-02
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。
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2.发明授权公开(公告)号：US07659267B2
公开(公告)日：2010-02-09
申请号：US10537520
申请日：2003-12-04
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。
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公开(公告)号：US20090082343A1
公开(公告)日：2009-03-26
申请号：US12099779
申请日：2008-04-08
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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公开(公告)号：US07767665B2
公开(公告)日：2010-08-03
申请号：US12099779
申请日：2008-04-08
IPC分类号： C07D417/04 , A61K31/538
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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公开(公告)号：US07399759B2
公开(公告)日：2008-07-15
申请号：US10488384
申请日：2002-09-02
IPC分类号： C07D417/04 , A61K31/538
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; 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，它们各自可以具有取代基; 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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6.发明申请1,3-Benzothiazinone derivatives, process for producing the same and use thereof 失效1,3-苯并噻嗪酮衍生物，其制备方法及其用途公开(公告)号：US20060052371A1
公开(公告)日：2006-03-09
申请号：US10537520
申请日：2003-12-04
IPC分类号： A61K31/5415 , C07D279/16
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 ：
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公开(公告)号：US20060252797A1
公开(公告)日：2006-11-09
申请号：US10533833
申请日：2003-11-05
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。
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8.发明授权1-heterocyclylsulfonyl, 3-aminomethyl, 5- (hetero-) aryl substituted 1-H-pyrrole derivatives as acid secretion inhibitors 有权1-杂环基磺酰基，3-氨基甲基，5-（杂）芳基取代的1 H-吡咯衍生物作为酸分泌抑制剂公开(公告)号：US08338462B2
公开(公告)日：2012-12-25
申请号：US13156226
申请日：2011-06-08
IPC分类号： C07D401/02 , A61K31/444
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D417/12 , C07D487/04
摘要： The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl pup, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.
摘要翻译： 本发明提供具有优异的酸分泌抑制作用并显示出抗溃疡活性等的化合物。 本发明提供由式（I）表示的化合物，其中R 1是任选与苯环或杂环稠合的含氮单环杂环基，任选地与苯环或杂环稠合的含氮单环杂环基 具有取代基，R 2为任选取代的C 6-14芳基，任选取代的噻吩基或任选取代的吡啶基，R 3和R 4各自为氢原子，或者R 3和R 4中的一个为氢原子， 另一个是任选取代的低级烷基小时，酰基，卤素原子，氰基或硝基，R 5是烷基或其盐。
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9.发明申请1-HETEROCYCLYLSULFONYL, 2-AMINOMETHYL, 5- (HETERO-) ARYL SUBSTITUTED 1-H-PYRROLE DERIVATIVES AS ACID SECRETION INHIBITORS 有权作为酸分泌抑制剂的1-杂环甲硅烷基，2-氨基乙基，5-（异丁基）芳基取代的1-H-吡咯烷酮衍生物公开(公告)号：US20110144161A1
公开(公告)日：2011-06-16
申请号：US13037690
申请日：2011-03-01
IPC分类号： A61K31/444 , A61K31/4439 , C07D401/14 , C07D401/02 , A61P35/00 , A61P1/04
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D417/12 , C07D487/04
摘要： The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.
摘要翻译： 本发明提供具有优异的酸分泌抑制作用并显示出抗溃疡活性等的化合物。 本发明提供由式（I）表示的化合物，其中R 1是任选与苯环或杂环稠合的含氮单环杂环基，任选地与苯环或杂环稠合的含氮单环杂环基 具有取代基，R 2为任选取代的C 6-14芳基，任选取代的噻吩基或任选取代的吡啶基，R 3和R 4各自为氢原子，或者R 3和R 4中的一个为氢原子， 另一个是任选取代的低级烷基，酰基，卤素原子，氰基或硝基，R 5是烷基或其盐。
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10.发明授权1-heterocyclylsulfonyl, 3-aminomethyl, 5- (hetero-) aryl substituted 1-H-pyrrole derivatives as acid secretion inhibitors 有权1-杂环基磺酰基，3-氨基甲基，5-（杂）芳基取代的1 H-吡咯衍生物作为酸分泌抑制剂公开(公告)号：US08436187B2
公开(公告)日：2013-05-07
申请号：US13156204
申请日：2011-06-08
IPC分类号： C07D401/02
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D417/12 , C07D487/04
摘要： The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.
摘要翻译： 本发明提供具有优异的酸分泌抑制作用并显示出抗溃疡活性等的化合物。 本发明提供由式（I）表示的化合物，其中R 1是任选与苯环或杂环稠合的含氮单环杂环基，任选地与苯环或杂环稠合的含氮单环杂环基 具有取代基，R 2为任选取代的C 6-14芳基，任选取代的噻吩基或任选取代的吡啶基，R 3和R 4各自为氢原子，或者R 3和R 4中的一个为氢原子， 另一个是任选取代的低级烷基，酰基，卤素原子，氰基或硝基，R 5是烷基或其盐。
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