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公开(公告)号:US08563732B2
公开(公告)日:2013-10-22
申请号:US12602441
申请日:2008-05-30
申请人: Moriyasu Masui , Hidenori Mikamiyama , Naoki Tsuno
发明人: Moriyasu Masui , Hidenori Mikamiyama , Naoki Tsuno
IPC分类号: A61K31/44 , C07D211/00
CPC分类号: C07D211/96
摘要: The invention relates to oxyimino compounds of (Formula I), and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is hydrogen, each optionally substituted lower alkyl, lower alkenyl, aryl, heterocyclyl etc. R1 and R2 are each independently hydrogen, each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl etc., each X is independently ═O, optionally substituted lower alkyl, cyano, nitro etc., m is 1 or 2, p is O, 1 or 2 and q is O or 1. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
摘要翻译: 本发明涉及(式I)的氧亚氨基化合物及其药学上可接受的盐,前药和溶剂化物,其中:Y是CO或SOm; Z是氢,每个任选取代的低级烷基,低级烯基,芳基,杂环基等.R 1和R 2各自独立地为氢,各自为任意取代的低级烷基,低级烯基,环烷基,芳基,杂环基等,各X独立地为= 任选取代的低级烷基,氰基,硝基等,m为1或2,p为O,1或2,q为O或1.本发明还涉及式I的用途化合物,以治疗,预防或改善 对钙通道阻断,特别是N型钙通道的阻滞作用。 本发明的化合物特别适用于治疗疼痛。
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公开(公告)号:US20130210839A1
公开(公告)日:2013-08-15
申请号:US13881112
申请日:2011-10-27
申请人: Moriyasu Masui , Genta Tadano
发明人: Moriyasu Masui , Genta Tadano
IPC分类号: C07D487/04
CPC分类号: C07D487/04 , A61K31/519
摘要: The present invention provides, for example, the following compound: wherein ring A is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, X1—X2═X3 is CR5—CR6═CR7, N—CR6═CR7, CR5—N═CR7 or CR5—CR6═N, R1 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2a and R2b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R4a, R4b, R5, R6 and R7 are each independently hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid β production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid β proteins.
摘要翻译: 本发明例如提供以下化合物:其中环A为取代或未取代的碳环或取代或未取代的杂环,X1-X2 = X3为CR5-CR6 = CR7,N-CR6 = CR7,CR5-N = CR7或CR5-CR6 = N,R1是取代或未取代的烷基,取代或未取代的烯基等,R2a和R2b各自独立地为氢,取代或未取代的烷基等,R4a,R4b,R5,R6和R7各自为 独立地是氢,卤素,羟基,取代或未取代的烷基等,其药学上可接受的盐或其溶剂合物具有抑制淀粉样蛋白β产生的作用,特别是BACE1抑制活性,并且可用作治疗由生产诱导的疾病, 淀粉样β蛋白的分泌或沉积。
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23.
公开(公告)号:US07935706B2
公开(公告)日:2011-05-03
申请号:US12278412
申请日:2007-02-21
IPC分类号: A61K31/497
CPC分类号: C07D209/08 , C07D209/34 , C07D215/38 , C07D235/08 , C07D235/26 , C07D249/18 , C07D263/58 , C07D277/68 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D498/04 , C07D513/04
摘要: It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist.A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is —(CR3R4)m-, —CO(CR3R4)n-, —CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.
摘要翻译: 发现由式(I)表示的含氮杂环衍生物特异性结合NR1 / NR2B的受体,并用作NR2B受体拮抗剂。 由下式表示的化合物:其中Z为N或CR1,A1为任选取代的含氮芳族单环基团,任选取代的含氮芳族稠合环基等,A2为芳族烃环基或 芳族杂环基,各自任选具有取代基,R 1,R 2,R a,R b,R c和R d各自独立地为氢,羟基等,w为2或3,t为1或2,X为 - (CR 3 R 4)m - ,-CO(CR 3 R 4)n - , - CONR 5(CR 3 R 4)n - 等,m为1〜4的整数,n为0〜4的整数,R 3和R 4各自独立地为氢,卤素,羟基等 R5为氢或低级烷基,或其药学上可接受的盐或溶剂合物。
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公开(公告)号:US5519139A
公开(公告)日:1996-05-21
申请号:US448193
申请日:1995-05-23
IPC分类号: A01N43/54 , C07D239/42 , C07D239/46 , C07D405/12 , C07D239/30 , C07D239/34 , C07D401/04
CPC分类号: C07D239/42 , A01N43/54 , C07D239/47 , C07D405/12
摘要: There is disclosed a novel 4-aminopyrimidine derivative containing an optionally esterified carboxyl group at the 5-position which has potent fungicidal activity as well as insecticidal and miticidal activity. The compound is useful as agricultural fungicides, insecticides and miticides. There are also disclosed a process for producing the above compound and agricultural fungicidal, insecticidal and miticidal compositions
摘要翻译: 公开了一种新的4-氨基嘧啶衍生物,其在5位含有任选酯化的羧基,其具有强的杀真菌活性以及杀虫和杀螨活性。 该化合物可用作农业杀真菌剂,杀虫剂和杀螨剂。 还公开了制备上述化合物和农业杀真菌剂,杀虫剂和杀螨剂组合物的方法
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公开(公告)号:US5506358A
公开(公告)日:1996-04-09
申请号:US207055
申请日:1994-03-08
申请人: Akira Takase , Hiroyuki Kai , Moriyasu Masui , Kazuo Ueda , Tsuneo Iwakawa
发明人: Akira Takase , Hiroyuki Kai , Moriyasu Masui , Kazuo Ueda , Tsuneo Iwakawa
IPC分类号: C07D215/22 , C07C249/12 , C07C251/48 , C07C255/62 , C07C317/48 , C07C323/60 , C07C323/63 , C07D213/65 , C07D277/68 , C07D303/46 , C07D307/42 , C07D309/12 , C07D239/02 , C07C249/04
CPC分类号: C07D213/65 , C07C249/12 , C07C251/48
摘要: There is disclosed a process for producing an alkoxyiminoacetamide compound which is useful as agricultural fungicides. Also dislclosed are novel intermediate compounds for the above process and their production.
摘要翻译: 公开了可用作农业杀真菌剂的烷氧基亚氨基乙酰胺化合物的制备方法。 也可以是上述方法的新型中间体化合物及其制备。
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公开(公告)号:US08999980B2
公开(公告)日:2015-04-07
申请号:US13513839
申请日:2010-12-10
申请人: Moriyasu Masui , Akihiro Hori
发明人: Moriyasu Masui , Akihiro Hori
IPC分类号: C07D413/12 , C07D413/14 , C07D498/04 , A61K31/535 , A61K31/5355 , C07D265/06 , C07D265/08
CPC分类号: C07D265/08 , C07D265/06 , C07D413/12 , C07D413/14 , C07D498/04
摘要: The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-β proteins.A compound of the formula (I): wherein R1, R2a, R2b, R3, R4a, R4b, ring A and the dashed lines are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
摘要翻译: 本发明例如提供下述化合物作为治疗或预防由淀粉样蛋白的生产,分泌或沉积引起的疾病的药物。 蛋白质。 式(I)的化合物:其中R1,R2a,R2b,R3,R4a,R4b,环A和虚线在本说明书中定义,其药学上可接受的盐或溶剂合物。
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公开(公告)号:US08865907B2
公开(公告)日:2014-10-21
申请号:US13260063
申请日:2010-03-26
IPC分类号: C07D213/79 , C07D213/80 , C07D471/04 , C07D309/32 , C07D405/06 , C07D498/14
CPC分类号: C07D498/14 , C07D213/80 , C07D309/32 , C07D309/40 , C07D405/06 , C07D471/04 , C07D471/14
摘要: The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.
摘要翻译: 本发明提供了作为合成抗流感药物的新中间体的吡喃酮衍生物和吡啶酮衍生物,其制造方法及其使用方法。
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公开(公告)号:US20120245157A1
公开(公告)日:2012-09-27
申请号:US13513839
申请日:2010-12-10
申请人: Moriyasu Masui , Akihiro Hori
发明人: Moriyasu Masui , Akihiro Hori
IPC分类号: C07D265/06 , A61K31/536 , C07D265/18 , C07D265/12 , C07D498/04 , C07D413/12 , A61K31/5355 , A61K31/5365
CPC分类号: C07D265/08 , C07D265/06 , C07D413/12 , C07D413/14 , C07D498/04
摘要: The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-β proteins.A compound of the formula (I): wherein R1, R2a, R2b, R3, R4a, R4b, ring A and the dashed lines are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
摘要翻译: 本发明例如提供下述化合物作为治疗或预防由淀粉样蛋白的生产,分泌或沉积引起的疾病的药物。 蛋白质。 式(I)的化合物:其中R1,R2a,R2b,R3,R4a,R4b,环A和虚线在本说明书中定义,其药学上可接受的盐或溶剂合物。
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公开(公告)号:US20120022069A1
公开(公告)日:2012-01-26
申请号:US13260185
申请日:2010-04-02
IPC分类号: A61K31/445 , C07D401/12 , A61K31/4545 , C07D405/12 , A61K31/4525 , C07D409/12 , C07D265/30 , A61K31/5375 , A61P25/00 , A61P25/08 , A61P25/06 , A61P25/18 , A61P25/28 , A61P25/24 , A61P25/22 , A61P9/12 , A61P9/06 , C07D211/96
CPC分类号: C07D211/70 , C07D211/96
摘要: The invention relates to acrylamide compounds of Formula I mentioned below.The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
摘要翻译: 本发明涉及下述式I的丙烯酰胺化合物。 本发明还涉及使用式I化合物来治疗或预防对阻塞钙通道,特别是N型钙通道有响应的病症。 本发明的化合物特别适用于治疗疼痛。
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公开(公告)号:US20110251212A1
公开(公告)日:2011-10-13
申请号:US12674275
申请日:2008-08-19
申请人: Moriyasu Masui , Minoru Tomida , Naotake Kobayashi , Kousuke Anan , Aya Tazawa , Kayoko Hata
发明人: Moriyasu Masui , Minoru Tomida , Naotake Kobayashi , Kousuke Anan , Aya Tazawa , Kayoko Hata
IPC分类号: A61K31/496 , C07D401/12 , C07D413/14 , C07D487/08 , A61P25/00 , C07D403/12 , A61P9/10 , A61P25/28 , A61P25/26 , A61P25/32 , C07D413/12 , A61K31/422
CPC分类号: C07D209/34 , C07D215/22 , C07D235/26 , C07D263/58 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D487/08 , C07D498/04
摘要: A compound which specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist is provided.It has been found out that a piperazine derivative represented by the formula (I) binds specifically to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist.A compound represented by: wherein R1 is each independently C1-C3 alkyl or the like, m is an integer of 0 to 4, X is —N(R4)—C(═O)—C(═O)—, —N(R4)—(CR5R6)p—C(═O)—, —N(R4)—C(═O)—(CR7R8)q— or —C(═O)—N(R4)—(CR7R8)q—, p and q are each independently an integer of 1 to 3, R4, R5, R6, R7 and R8 are each independently a hydrogen atom or lower alkyl, A1 is benzoxazolinone or the like, and A2 is optionally substituted phenyl or the like, or a pharmaceutically acceptable salt or a solvate thereof.
摘要翻译: 提供了特异性结合NR1 / NR2B的受体并用作NR2B受体拮抗剂的化合物。 已经发现,由式(I)表示的哌嗪衍生物与NR1 / NR2B的受体特异性结合,用作NR2B受体拮抗剂。 由下式表示的化合物:其中R 1各自独立地为C 1 -C 3烷基等,m为0〜4的整数,X为-N(R 4)-C(= O)-C(= O) - , - N (R4) - (CR5R6)p-C(= O) - , - N(R4)-C(= O) - (CR7R8)q-或-C(= O)-N(R4) - (CR7R8)q - ,p和q各自独立地为1〜3的整数,R4,R5,R6,R7和R8各自独立地为氢原子或低级烷基,A1为苯并恶唑啉酮等,A2为任选取代的苯基等 ,或其药学上可接受的盐或溶剂合物。
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