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公开(公告)号：US07608716B2
公开(公告)日：2009-10-27
申请号：US10533806
申请日：2003-11-05
IPC分类号： A61K31/4375 , C07D471/14 , C07D471/16
CPC分类号： A61K31/4375 , A61K31/444 , C07D471/14
摘要： The target is to provide PDE IV inhibitors which have a highly potent anti-asthmatic and/or COPD-prophylactic/therapeutic profile with unexpectedly excellent safety. A compound of the formula (1): wherein A is phenyl, pyridyl, 1-oxypyridyl, or thienyl, which may be unsubstituted or optionally substituted with one or more members selected from the group consisting of hydroxyl, halogen, cyano, nitro, lower alkyl, lower alkoxy, lower alkylcarbonyloxy, amino, carboxyl, lower alkoxycarbonyl, carboxy-lower alkylene, lower alkoxycarbonyl-lower alkylene, lower alkylsulfonyl, lower alkylsulfonylamino, and ureido; R1 is a group selected from the group consisting of hydrogen, hydroxyl, halogen, cyano, nitro, lower alkoxy, amino, carboxyl, and lower alkoxycarbonyl; R2 is hydrogen or lower alkyl; and m is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof, possesses highly excellent PDE IV-specific inhibitory actions and is useful as an anti-asthmatic drug and/or a prophylactic/therapeutic drug for COPD with high safety.
摘要翻译： 目标是提供具有非常有效的抗哮喘和/或COPD预防/治疗特征的PDE IV抑制剂，具有出人意料的极好的安全性。 式（1）的化合物：其中A是苯基，吡啶基，1-氧代吡啶基或噻吩基，其可以是未取代的或任选地被一个或多个选自羟基，卤素，氰基，硝基，低级 烷基，低级烷氧基，低级烷基羰基氧基，氨基，羧基，低级烷氧基羰基，羧基 - 低级亚烷基，低级烷氧基羰基 - 低级亚烷基，低级烷基磺酰基，低级烷基磺酰基氨基和脲基。 R 1是选自氢，羟基，卤素，氰基，硝基，低级烷氧基，氨基，羧基和低级烷氧基羰基的基团。 R2是氢或低级烷基; m为1〜3的整数。 或其药学上可接受的盐具有非常优异的PDE IV特异性抑制作用，并且可用作具有高度安全性的抗哮喘药和/或用于COPD的预防/治疗药物。
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公开(公告)号：US20090131467A1
公开(公告)日：2009-05-21
申请号：US11991858
申请日：2006-09-15
IPC分类号： A61K31/437 , C07D471/04 , A61P11/06 , A61P11/00
CPC分类号： C07D471/14 , C07D471/04
摘要： The compound of the present invention is a novel compound which has a specific heterocycle skeleton, particularly a pyrazolonaphthyridine or pyrazoloquinoline skeleton having an organic group (e.g., a carbocycle and a heterocycle) bonding through an alkylene group at 3-position and a carbocycle bonding at 5-position and has a phosphodiesterase IV inhibitory activity. At least one of the ring (the carbocycle or the heterocycle) bonding at 3-position of the pyrazolonaphthyridine skeleton and the carbocycle bonding at 5-position may have a halogenated alkyl group and/or a halogenated alkoxy group as a substituent. Such a compound or a salt thereof is useful as a phosphodiesterase IV inhibitor and the like. According to the present invention, a novel compound having a high phosphodiesterase IV inhibitory effect can be provided.
摘要翻译： 本发明的化合物是具有特定杂环骨架的新型化合物，特别是具有通过3-位亚烷基键合的有机基团（例如，碳环和杂环）的吡唑并萘并吡啶骨架， 具有磷酸二酯酶IV抑制活性。 在吡唑并萘啶骨架的3位键合的环（碳环或杂环）中的至少一个和在5位键合的碳环可以具有卤代烷基和/或卤代烷氧基作为取代基。 这种化合物或其盐可用作磷酸二酯酶IV抑制剂等。 根据本发明，可以提供具有高磷酸二酯酶IV抑制作用的新型化合物。
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公开(公告)号：US08193356B2
公开(公告)日：2012-06-05
申请号：US11991858
申请日：2006-09-15
IPC分类号： C07D471/04 , A61K31/437 , A61P11/00 , A61P11/06
CPC分类号： C07D471/14 , C07D471/04
摘要： The compound of the present invention is a novel compound which has a specific heterocycle skeleton, particularly a pyrazolonaphthyridine or pyrazoloquinoline skeleton having an organic group (e.g., a carbocycle and a heterocycle) bonding through an alkylene group at 3-position and a carbocycle bonding at 5-position and has a phosphodiesterase IV inhibitory activity. At least one of the ring (the carbocycle or the heterocycle) bonding at 3-position of the pyrazolonaphthyridine skeleton and the carbocycle bonding at 5-position may have a halogenated alkyl group and/or a halogenated alkoxy group as a substituent. Such a compound or a salt thereof is useful as a phosphodiesterase IV inhibitor and the like. According to the present invention, a novel compound having a high phosphodiesterase IV inhibitory effect can be provided.
摘要翻译： 本发明的化合物是具有特定杂环骨架的新型化合物，特别是具有通过3-位亚烷基键合的有机基团（例如，碳环和杂环）的吡唑并萘并吡啶骨架， 具有磷酸二酯酶IV抑制活性。 在吡唑并萘啶骨架的3位键合的环（碳环或杂环）中的至少一个和在5位键合的碳环可以具有卤代烷基和/或卤代烷氧基作为取代基。 这种化合物或其盐可用作磷酸二酯酶IV抑制剂等。 根据本发明，可以提供具有高磷酸二酯酶IV抑制作用的新型化合物。
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公开(公告)号：US20100056613A1
公开(公告)日：2010-03-04
申请号：US12312640
申请日：2007-11-21
IPC分类号： A61K31/385 , C07D339/06 , A61P9/12 , A61P25/00 , A61P3/10 , A61P3/04 , A61P13/12 , A61P29/00
CPC分类号： C07D339/06
摘要： A novel spiroquinone derivative having a high ABCA1 stabilization effect and being useful for prophylactic and/or therapeutic agents for various diseases developing hypo-high density lipoproteinemia is obtained. The novel spiroquinone derivative is a compound represented by the following formula: wherein R1a, R1b, R1c and R1d each represents a hydrogen atom, a halogen atom, an alkyl group which may have a substituent, or an alkoxy group which may have a substituent, and R2a and R2b each represents a hydrogen atom, or an alkyl group which may have a substituent (e.g., a carboxyl group, an alkoxycarbonyl group, a carbamoyl group, and an N-substituted carbamoyl group), the groups R2a and R2b may bond together to form a hydrocarbon ring with an adjacent carbon atom, provided that compounds in which all of the groups R1a, R1b, R1c and R1d are t-butyl groups, and both of the groups R2a and R2b are hydrogen atoms or both of the groups R2a and R2b are methyl groups are excluded; or a pharmacologically acceptable salt thereof.
摘要翻译： 获得具有高ABCA1稳定作用并可用于发生低密度脂蛋白血症的各种疾病的预防和/或治疗剂的新型螺醌衍生物。 新型螺醌衍生物为下式表示的化合物：其中R1a，R1b，R1c和R1d各自表示氢原子，卤素原子，可具有取代基的烷基或可具有取代基的烷氧基， R2a和R2b各自表示氢原子或可具有取代基的烷基（例如羧基，烷氧基羰基，氨基甲酰基和N-取代氨基甲酰基），基团R 2a和R 2b可以键合 一起形成具有相邻碳原子的烃环，条件是其中所有基团R 1a，R 1b，R 1c和R 1d都是叔丁基，并且基团R 2a和R 2b各自为氢原子或两个基团 R2a和R2b是甲基; 或其药理学上可接受的盐。
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15.发明授权
公开(公告)号：US5198450A
公开(公告)日：1993-03-30
申请号：US601795
申请日：1991-01-07
申请人： Kuniyoshi Ogura , Tomoji Aotsuka , Motoki Torizuka , Mitsuo Soeda , Yoshiaki Tanaka , Hisayoshi Kato , Naoyoshi Miura , Noaki Nakata , Hikaru Morita , Akihiro Okubo
发明人： Kuniyoshi Ogura , Tomoji Aotsuka , Motoki Torizuka , Mitsuo Soeda , Yoshiaki Tanaka , Hisayoshi Kato , Naoyoshi Miura , Noaki Nakata , Hikaru Morita , Akihiro Okubo
IPC分类号： C07D295/18 , A61K31/40 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/535 , A61K31/5375 , A61K31/54 , A61P25/28 , C07D207/20 , C07D211/70 , C07D277/04 , C07D295/185
CPC分类号： C07D295/185 , C07D207/20 , C07D211/70 , C07D277/04
摘要： An agent for treating or preventing cerebral circulation disorder, cerebral metabolism disorder, or memory disturbance is disclosed. The agent comprises as an effective component a phenylalkanoylamine derivative represented by the following formula (I), ##STR1## wherein A represents a 1,3-thiazolidin-3-yl group, a 1,2,3,6-tetrahydropyridin-1-yl group, a morpholino group, a thiomorpholin-4-yl group, or a 3-pyrrolin-1-yl group, R.sup.1 and R.sup.2, which may be the same or different, represent a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, an amino group, a guanidino group, or a group ##STR2## (wherein R.sup.3 and R.sup.4 independently represent a lower alkyl group or form in combination 5- or 6-membered heterocyclic group), and n represents an integer of 2-6, or a salt thereof. This agent is effective for treating or preventing cerebral hemorrhage sequela, cerebral infarction sequela, cerebral arterioscleosis, subarachnoid hemorrhage sequela, cranial injury sequela, cerebral operation sequela, cerebrovascular dementia, Parkinson's disease, Alzheimer's disease, Pick's disease, various anoxia toxicosis including, but not limited to anthracemia sequela, cerebral alcoholism related diseases, and the like.
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公开(公告)号：US07666900B2
公开(公告)日：2010-02-23
申请号：US10586338
申请日：2004-12-22
申请人： Shinji Yokoyama , Maki Tsujita , Reijiro Arakawa , Tomoji Aotsuka
发明人： Shinji Yokoyama , Maki Tsujita , Reijiro Arakawa , Tomoji Aotsuka
CPC分类号： A61K31/385 , A61K31/05 , A61K31/122 , Y10S514/824
摘要： To provide a pharmaceutically effective prophylactic/preventive agent for low-HDL cholesterolemia, focusing on an HDL-generating mechanism. The ABCA1 stabilizer of the present invention contains a bisphenol-type compound selected form probucol spiroquinone, probucol diphenoquinone, and probucol bisphenol as an effective ingredient. The ABCA1 stabilizer can continuously and stably express ABCA1 by a mechanism quite different from that of conventional processes, and thus is useful as prophylactic/preventive agent for low-HDL cholesterolemia or arteriosclerosis.
摘要翻译： 提供用于低HDL胆固醇血症的药学上有效的预防/预防药物，重点是HDL生成机制。 本发明的ABCA1稳定剂含有选自普罗布考螺醌，普罗布考二苯醌和普罗布考双酚作为有效成分的双酚型化合物。 ABCA1稳定剂可以通过与常规方法完全不同的机制连续稳定地表达ABCA1，因此可用作低HDL胆固醇血症或动脉硬化的预防/预防剂。
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公开(公告)号：US6136831A
公开(公告)日：2000-10-24
申请号：US402433
申请日：1999-10-07
IPC分类号： C07D403/04 , C07D413/04 , C07D417/04 , A61K31/4184 , A61K31/423 , A61K31/428
CPC分类号： C07D403/04 , C07D413/04 , C07D417/04
摘要： The purpose is to provide anti-inflammatory agents which have potent pharmacological actions and exert a selective inhibitory activity on COX-2, thereby being expected to reduce adverse effects such as disorders in gastric mucosa. The present invention encompasses a compound of the formula (1): wherein R.sup.1 is hydrogen or halogen, R.sup.2 and R.sup.3 are each independently hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy or lower alkanoyloxy, R.sup.4 is lower haloalkyl or lower alkyl, X is sulfur, oxygen or NH, and Y is lower alkylthio, lower alkylsulfonyl or sulfamoyl, which exerts superior anti-inflammatory activity, and highly inhibits COX-2 induced in inflamed sites, with less inhibitory action on COX-1 present in stomach, kidney, etc. Pharmaceutical agents comprising the compound of the present invention are provided as selective COX-2 inhibitors, and anti-inflammatory agents rarely accompanying adverse actions including attacks on gastric mucosa.
摘要翻译： PCT No.PCT / JP98 / 01664 Sec。 371 1999年10月7日第 102（e）日期1999年10月7日PCT提交1998年4月10日PCT公布。 公开号WO98 / 46594 日期1998年10月22日目的是提供具有有效药理作用并对COX-2具有选择性抑制活性的抗炎剂，从而预期减少诸如胃粘膜疾病的不良反应。 本发明包括式（1）的化合物：其中R1是氢或卤素，R2和R3各自独立地是氢，卤素，低级烷基，低级烷氧基，羟基或低级烷酰氧基，R4是低级卤代烷基或低级烷基，X 是硫，氧或NH，Y是低级烷硫基，低级烷基磺酰基或氨磺酰基，其具有优异的抗炎活性，并且高度抑制炎症部位诱导的COX-2，对胃，肾中COX-1的抑制作用较小 提供包含本发明化合物的药物作为选择性COX-2抑制剂，和很少伴随不良反应（包括攻击胃粘膜）的抗炎剂。
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公开(公告)号：US5028604A
公开(公告)日：1991-07-02
申请号：US444702
申请日：1989-12-01
申请人： Motoki Torizuka , Tomoji Aotsuka , Mitsuo Soeda , Kuniyoshi Ogura , Yoshiaki Tanaka , Hisayoshi Kato , Naoki Nakata , Naoyoshi Miura , Hikari Morita
发明人： Motoki Torizuka , Tomoji Aotsuka , Mitsuo Soeda , Kuniyoshi Ogura , Yoshiaki Tanaka , Hisayoshi Kato , Naoki Nakata , Naoyoshi Miura , Hikari Morita
IPC分类号： C07D207/16 , C07D211/60 , C07D277/06 , C07D279/12 , C07D417/06 , C07K5/078
CPC分类号： C07D417/06 , C07D207/16 , C07D211/60 , C07D277/06 , C07D279/12 , C07K5/06165
摘要： Novel condensed benzene derivatives having prolyl endopeptidase inhibitory, anti-hypoxic, and anti-amnesic activities are disclosed. The compounds are represented by the following (I), ##STR1## wherein A represents a methylene, ethylene, or propylene group, B represents a methylene or ethylene group, m denotes an integer of 0-5, X and Y, which may be same or different, individually represent a methylene group or sulfur atom, R.sup.1 represents a hydrogen atom, a carboxyl, lower alkyloxycarbonyl, hydroxymethyl, or formyl group, R.sup.2 represents a hydrogen atom, a halogen atom, a lower alkyl, lower alkoxy, nitro, or amino group, R.sup.3 represents a hydrogen atom or a lower alkyl group, and the dotted line may optionally be present. They are useful as a medicine for treating or preventing cerebral circulation disorder, cerebral metabolism disorder, or memory disturbance.
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19.发明授权Amino acid imide derivatives, usage thereof, and medicinal composition containing the same 失效氨基酰亚胺衍生物，其用途和含有它们的药物组合物
公开(公告)号：US4916146A
公开(公告)日：1990-04-10
申请号：US288556
申请日：1988-12-22
申请人： Yoshiaki Tanaka , Tomoji Aotsuka , Naomi Kobayashi , Naoki Nakata , Kuniyoshi Ogura , Motoki Torizuka , Naoyoshi Miura , Heihachiro Arai
发明人： Yoshiaki Tanaka , Tomoji Aotsuka , Naomi Kobayashi , Naoki Nakata , Kuniyoshi Ogura , Motoki Torizuka , Naoyoshi Miura , Heihachiro Arai
IPC分类号： C12N9/99 , A61K31/425 , A61K31/426 , A61P25/28 , A61P43/00 , C07D207/00 , C07D277/06 , C07D413/06 , C07D417/06
CPC分类号： C07D417/06 , C07D277/06
摘要： Novel N-substituted amino acid imide derivatives are disclosed. The compounds are represented by formula (I): ##STR1## wherein n represents an integer of 0 to 5, and X and Y, which may be the same or different, represent a methylene group or a sulfur atom, provided that not both X and Y are methylene groups at the same time. The compounds are useful as a medicine for treating or preventing cerebral circulation disorder, cerebral metabolism disorder, or memory disturbance.
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公开(公告)号：US09365553B2
公开(公告)日：2016-06-14
申请号：US13699892
申请日：2011-05-23
申请人： Makoto Okada , Koichi Hasumi , Takahiro Nishimoto , Miwa Yoshida , Kouki Ishitani , Tomoji Aotsuka , Hashime Kanazawa
发明人： Makoto Okada , Koichi Hasumi , Takahiro Nishimoto , Miwa Yoshida , Kouki Ishitani , Tomoji Aotsuka , Hashime Kanazawa
IPC分类号： C07D401/06 , C07D211/46 , C07D405/06 , C07D213/79 , C07D333/40 , C07D407/08 , C07D409/06 , C07D413/06 , C07D417/06
CPC分类号： C07D405/06 , C07D211/46 , C07D213/79 , C07D333/40 , C07D401/06 , C07D407/08 , C07D409/06 , C07D413/06 , C07D417/06
摘要： A heterocyclic compound useful as an antiallergic agent is provided.A compound represented by the following formula (1) or a salt thereof: wherein the ring A is a homocyclic or heterocyclic ring; the ring B is a heterocyclic ring which contains G and nitrogen atom N as constituent atoms thereof, wherein G is CH or N; R1 is a carbonyl group or an alkylene group; R2a and R2b are an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; X is an oxygen atom or a sulfur atom; Z is a hydroxyl group, an alkoxy group, a cycloalkyloxy group, an aryloxy group, an aralkyloxy group, an amino group, or an N-substituted amino group; and n is 0 or 1; with the proviso that when the ring A is a benzene ring or when the ring B is a piperazine ring, R1 is an alkylene group which may have a substituent.
摘要翻译： 提供了可用作抗过敏剂的杂环化合物。 由下式（1）表示的化合物或其盐：其中环A是稠环或杂环; 环B是含有G和氮原子N作为其构成原子的杂环，其中G是CH或N; R1是羰基或亚烷基; R2a和R2b是烷基，环烷基，芳基或杂环基; X是氧原子或硫原子; Z是羟基，烷氧基，环烷氧基，芳氧基，芳烷氧基，氨基或N-取代氨基; 并且n为0或1; 条件是当环A为苯环时，或当环B为哌嗪环时，R 1为可具有取代基的亚烷基。
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