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11. 发明申请

US20140024650A1 SULFONAMIDE DERIVATIVE AND USE THEREOF 有权
标题翻译：磺酰胺衍生物及其用途
公开(公告)号：US20140024650A1
公开(公告)日：2014-01-23
申请号：US14009456
申请日：2012-04-05
申请人： Shoji Fukumoto , Osamu Ujikawa , Shinji Morimoto , Yasutomi Asano , Satoshi Mikami , Norihito Tokunaga , Masakuni Kori , Toshihiro Imaeda , Koichiro Fukuda , Shinji Nakamura , Kouichi Iwanaga
发明人： Shoji Fukumoto , Osamu Ujikawa , Shinji Morimoto , Yasutomi Asano , Satoshi Mikami , Norihito Tokunaga , Masakuni Kori , Toshihiro Imaeda , Koichiro Fukuda , Shinji Nakamura , Kouichi Iwanaga
IPC分类号： C07C311/07 , C07D401/12 , C07D309/14 , C07D295/092 , C07D333/16 , C07D231/12 , C07D233/56 , C07D211/58 , C07D307/22
CPC分类号： C07C311/07 , C07C311/09 , C07C311/14 , C07C317/28 , C07C323/26 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D207/27 , C07D207/273 , C07D209/04 , C07D211/56 , C07D211/58 , C07D211/76 , C07D213/61 , C07D213/64 , C07D213/85 , C07D231/12 , C07D231/14 , C07D233/56 , C07D233/68 , C07D237/04 , C07D239/28 , C07D261/08 , C07D263/32 , C07D277/24 , C07D277/32 , C07D277/62 , C07D295/092 , C07D295/192 , C07D305/06 , C07D307/22 , C07D309/06 , C07D309/14 , C07D333/16 , C07D401/04 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D493/08
摘要： Provided is a compound having an AMPA receptor function enhancing action, and useful as a prophylactic or therapeutic drug for depression, Alzheimer's disease, schizophrenia, attention deficit hyperactivity disorder (ADHD) and the like. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
摘要翻译：提供具有AMPA受体功能增强作用的化合物，可用作抑郁症，阿尔茨海默氏病，精神分裂症，注意力缺陷多动障碍（ADHD）等的预防或治疗药物。由式（I）表示的化合物或其盐，其中每个符号如本说明书中所定义。

12. 发明授权

US07851473B2 Amide compound 失效
标题翻译：酰胺化合物
公开(公告)号：US07851473B2
公开(公告)日：2010-12-14
申请号：US11667821
申请日：2005-11-17
申请人： Takahiro Matsumoto , Masakuni Kori , Junichi Miyazaki , Yoshihiro Kiyota
发明人： Takahiro Matsumoto , Masakuni Kori , Junichi Miyazaki , Yoshihiro Kiyota
IPC分类号： A61K31/501 , A61K31/497 , C07D401/12 , C07D403/12 , C07D413/12
CPC分类号： C12Q1/34 , A61K31/495 , C07D261/20 , C07D285/08 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , G01N33/6896 , G01N2333/978 , G01N2500/00 , G01N2800/28
摘要： There is provided a FAAH inhibitor and a prophylactic or therapeutic agent for cerebrovascular disorders or sleep disorders comprising it. The prophylactic or therapeutic agent comprises a compound of the formula (I0): wherein Z is oxygen or sulfur; R1 is aryl which may be substituted, or a heterocyclic group which may be substituted; R1a is a hydrogen atom, a hydrocarbon group which may be substituted, hydroxyl, etc.; R2 is piperidin-1,4-diyl which may be substituted, or piperazin-1,4-diyl which may be substituted; R3 is a group formed by eliminating two hydrogen atoms from a 5-membered aromatic heterocyclic group having 1 to 3 heteroatoms selected from nitrogen, oxygen and sulfur, which may be further substituted, —CO—, etc.; and R4 is a hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted; or a salt thereof.
摘要翻译：提供了FAAH抑制剂和包含其的脑血管障碍或睡眠障碍的预防或治疗剂。预防或治疗剂包括式（I0）化合物：其中Z是氧或硫; R1可以被取代的芳基，或可被取代的杂环基; R1a为氢原子，可被取代的烃基，羟基等; R2是可被取代的哌啶-1,4-二基，或可被取代的哌嗪-1,4-二基; R3是通过从具有1至3个选自氮，氧和硫的杂原子的5元芳族杂环基中除去两个氢原子而形成的基团，其可进一步被-CO-等取代; R 4为可被取代的烃基，或可被取代的杂环基; 或其盐。

13. 发明申请

US20090048263A1 Brain/neuronal cell-protecting agent and therapeutic agent for sleep disorder 失效
标题翻译：脑/神经元细胞保护剂和睡眠障碍治疗剂
公开(公告)号：US20090048263A1
公开(公告)日：2009-02-19
申请号：US11990385
申请日：2006-08-11
申请人： Takahiro Matsumoto , Masakuni Kori , Mitsunori Kouno
发明人： Takahiro Matsumoto , Masakuni Kori , Mitsunori Kouno
IPC分类号： A61K31/496 , C07D401/02 , C07D413/02 , C07D401/14 , A61K31/501 , A61P25/00 , C07D413/14 , C07D403/02 , C07D409/14
CPC分类号： C07D213/75 , C07D237/20 , C07D261/14 , C07D333/20 , C07D405/14 , C07D409/14 , C07D413/14
摘要： A compound represented by the formula (I) or a salt thereof; and an agent for protecting a brain/neuronal cell or a therapeutic agent for sleep disorder comprising the compound or salt: wherein Z represents an oxygen or sulfur; R1 represents an aryl or heterocyclic group which may be substituted, provided that R1 is not a 3-ethyl-6-methoxy-2-methyl-5-naphthalen-1-yl group; R1a represents a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxyl group or the like; R2 represents a piperidin-1,4-diyl or piperazin-1,4-diyl which may be substituted; R3 represents a bivalent group which is formed by removing two hydrogen atoms from a benzene ring or 6-membered aromatic heterocyclic ring which may have a substituent, provided that R3 is not a pyridazin-3,6-diyl; and R4 represents a group which is formed by removing one hydrogen atom from a benzene ring or 5- to 6-membered heterocyclic ring which may be substituted, provided that the substituent on the heterocyclic ring is not a phenylethyl group which may be substituted when Z is sulfur.
摘要翻译：由式（I）表示的化合物或其盐; 以及用于保护脑/神经元细胞或用于睡眠障碍的治疗剂的药剂，其包含所述化合物或盐：其中Z表示氧或硫; R1表示可被取代的芳基或杂环基，条件是R 1不是3-乙基-6-甲氧基-2-甲基-5-萘-1-基; R 1a表示氢原子，可被取代的烃基，羟基等; R2代表可被取代的哌啶-1,4-二基或哌嗪-1,4-二基; R3表示通过从可以具有取代基的苯环或6元芳族杂环除去2个氢原子而形成的二价基团，条件是R 3不是哒嗪-3,6-二基; 并且R 4表示通过从可以被取代的苯环或5-至6-元杂环除去一个氢原子而形成的基团，条件是杂环上的取代基不是Z时可以被取代的苯基乙基是硫。

14. 发明授权

US5770438A Process for enantioselective hydrolysis of .alpha.-(2-amino)-phenyl-benzenemethanol ester type compounds using bacillus, pseudomonas or streptomyces 失效
标题翻译：使用芽孢杆菌，假单胞菌或链霉菌的α-（2-氨基）苯基 - 苯甲醇酯型化合物的对映选择性水解方法
公开(公告)号：US5770438A
公开(公告)日：1998-06-23
申请号：US550643
申请日：1995-10-31
申请人： Kazuo Nakahama , Motowo Izawa , Yoichi Nagano , Naoki Tarui , Kiyoharu Matsumoto , Masakuni Kori , Tsuneo Kanamaru , Toshiaki Nagata
发明人： Kazuo Nakahama , Motowo Izawa , Yoichi Nagano , Naoki Tarui , Kiyoharu Matsumoto , Masakuni Kori , Tsuneo Kanamaru , Toshiaki Nagata
IPC分类号： C12P7/22 , C12P17/10 , C12P41/00
CPC分类号： C12P17/10 , C12P41/004 , C12P41/005 , C12P7/22
摘要： A process for producing an optically active form of a compound of formula (I) ##STR1## wherein R.sub.1 represents hydrogen or a hydrocarbon group that may be substituted; R.sub.2 and R.sub.3 independently represent hydrogen, a hydrocarbon group that may be substituted, or a heteroaromatic group that may be substituted; X' represents a substituent comprising an esterified carboxyl group or an acylated hydroxyl group; ring A represents a benzene ring that may be substituted or a heteroaromatic ring that may be substituted; ring J' represents a 7- or 8-membered heterocyclic ring containing at most 3 hetero-atoms as ring-constituent members, which may have a further substituent or substituents in addition to R.sub.1, R.sub.2, R.sub.3 and X', and C* denotes a chiral carbon atom or a salt thereof, which comprises subjecting the racemic compound of the formula (I) or a salt thereof, or alternatively a racemic starting compound for synthesizing the compound of the formula (I) to enzymatically enantioselective hydrolysis to provide an optically active form thereof.
摘要翻译：一种制备光学活性形式的式（I）化合物的方法其中R 1表示氢或可被取代的烃基; R2和R3独立地表示氢，可以被取代的烃基或可以被取代的杂芳基; X'表示包含酯化羧基或酰化羟基的取代基; 环A表示可被取代的苯环或可被取代的杂芳环; 环J'表示含有至多3个杂原子作为环构成成员的7或8元杂环，除R1，R2，R3和X'之外，还可以具有另外的取代基或取代基，C *表示手性碳原子或其盐，其包括使式（I）的外消旋化合物或其盐或外消旋起始化合物合成式（I）化合物进行酶对映选择性水解以提供光学其活性形式。

15. 发明授权

US5726306A 4,1-benzoxazepin derivatives and their use 失效
标题翻译： 4,1-苯并氧氮杂衍生物及其用途
公开(公告)号：US5726306A
公开(公告)日：1998-03-10
申请号：US338163
申请日：1994-11-09
申请人： Hidefumi Yukimasa , Ryuichi Tozawa , Masakuni Kori , Kazuaki Kitano , Yasuo Sugiyama
发明人： Hidefumi Yukimasa , Ryuichi Tozawa , Masakuni Kori , Kazuaki Kitano , Yasuo Sugiyama
IPC分类号： A61K31/395 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/553 , A61K31/554 , C07D267/14 , C07D413/06 , C07D413/12
CPC分类号： C07D413/06 , A61K31/395 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/553 , A61K31/554 , C07D267/14 , C07D413/12
摘要： N-containing, condensed heterocyclic compounds and salts thereof are disclosed which are useful for inhibiting squalene synthetase and fungal growth, and which are useful for treating or preventing hyperlipidemia. Also disclosed is a method for producing these compounds.
摘要翻译：公开了含氮，稠合的杂环化合物及其盐，其可用于抑制角鲨烯合成酶和真菌生长，并且其可用于治疗或预防高脂血症。还公开了这些化合物的制造方法。

16. 发明授权

US5498728A Derivatives of L-tryptophanal and their use as medicinals 失效
标题翻译： L-色氨酸的衍生物及其作为药物的用途
公开(公告)号：US5498728A
公开(公告)日：1996-03-12
申请号：US192038
申请日：1994-02-04
申请人： Takashi Sohda , Yukio Fujisawa , Tsuneo Yasuma , Junji Mizoguchi , Masakuni Kori , Masayuki Takizawa
发明人： Takashi Sohda , Yukio Fujisawa , Tsuneo Yasuma , Junji Mizoguchi , Masakuni Kori , Masayuki Takizawa
IPC分类号： A61K38/55 , A61K31/16 , A61K31/165 , A61K31/18 , A61K31/27 , A61K38/00 , A61P3/00 , A61P3/02 , A61P43/00 , C07C231/12 , C07C233/18 , C07C233/22 , C07C233/31 , C07C237/10 , C07C237/22 , C07C271/16 , C07C271/18 , C07C271/22 , C07C303/40 , C07C311/19 , C07C337/02 , C07D209/14 , C07D209/16 , C07K1/113 , C07K5/06 , C07K5/062 , C07K14/81 , A61K31/40
CPC分类号： C07D209/16 , C07C233/18 , C07C233/22 , C07C233/31 , C07C271/16 , C07C271/18 , C07C271/22 , C07C311/19 , C07K5/06034 , A61K38/00 , Y02P20/55
摘要： The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.Compound (I) is useful as a prophylactic/therapeutic agent for osteoporosis.
摘要翻译：本发明提供了含有下式化合物的组蛋白酶L抑制剂：其中R1是氢原子或可被取代的芳基烷基，杂环烷基或低级烷基; R2和R3独立地是氢原子或可以被取代的烃残基; R4是可以被取代的烷酰基，磺酰基，羰基氧基，氨基甲酰基或硫代氨基甲酰基; X是式：-CHO或-CHOOB（其中B是氢原子或羟基保护基）; m和n独立地为0或1的整数; 条件是R4是被芳基取代的烷酰基，被具有多于9个碳原子的芳基取代的磺酰基或低级烷基，或当R 1是未取代的低级烷基时可被取代的氨基甲酰基或硫代氨基甲酰基，甲基硫代乙基上的芳基烷基，R2和R3独立地是低级烷基或芳烷基，X是-CHO，m是1，n是0或1，或其盐。化合物（I）可用作骨质疏松症的预防/治疗剂。

17. 发明申请

US20130190291A1 HETEROCYCLIC COMPOUND AND USE THEREOF 有权
标题翻译：杂环化合物及其用途
公开(公告)号：US20130190291A1
公开(公告)日：2013-07-25
申请号：US13816137
申请日：2011-08-09
申请人： Masakuni Kori , Toshihiro Imaeda , Shinji Nakamura , Masashi Toyofuku , Eiji Honda , Yasutomi Asano , Osamu Ujikawa , Michiyo Mochizuki
发明人： Masakuni Kori , Toshihiro Imaeda , Shinji Nakamura , Masashi Toyofuku , Eiji Honda , Yasutomi Asano , Osamu Ujikawa , Michiyo Mochizuki
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.
摘要翻译：提供式（I）表示的化合物：其中每个符号如说明书中所定义，或其盐，其具有AMPA（α-氨基-3-羟基-5-甲基-4-异恶唑丙酸）受体增效作用本发明的化合物可用作抑郁症，精神分裂症，阿尔茨海默病或注意缺陷多动障碍（ADHD）等的预防或治疗药物。

18. 发明授权

US07812025B2 Brain/neuronal cell-protecting agent and therapeutic agent for sleep disorder 失效
标题翻译：脑/神经元细胞保护剂和睡眠障碍治疗剂
公开(公告)号：US07812025B2
公开(公告)日：2010-10-12
申请号：US11990385
申请日：2006-08-11
申请人： Takahiro Matsumoto , Masakuni Kori , Mitsunori Kouno
发明人： Takahiro Matsumoto , Masakuni Kori , Mitsunori Kouno
IPC分类号： A61K31/501 , A61K31/497 , A61K31/44 , C07D237/02 , C07D401/06 , C07D403/06 , C07D413/06 , C07D241/06 , C07D401/02 , C07D213/02
CPC分类号： C07D213/75 , C07D237/20 , C07D261/14 , C07D333/20 , C07D405/14 , C07D409/14 , C07D413/14
摘要： A compound represented by the formula (I) or a salt thereof; and an agent for protecting a brain/neuronal cell or a therapeutic agent for sleep disorder comprising the compound or salt: wherein Z represents an oxygen or sulfur; R1 represents an aryl or heterocyclic group which may be substituted, provided that R1 is not a 3-ethyl-6-methoxy-2-methyl-5-naphthalen-1-yl group; R1a represents a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxyl group or the like; R2 represents a piperidin-1,4-diyl or piperazin-1,4-diyl which may be substituted; R3 represents a bivalent group which is formed by removing two hydrogen atoms from a benzene ring or 6-membered aromatic heterocyclic ring which may have a substituent, provided that R3 is not a pyridazin-3,6-diyl; and R4 represents a group which is formed by removing one hydrogen atom from a benzene ring or 5- to 6-membered heterocyclic ring which may be substituted, provided that the substituent on the heterocyclic ring is not a phenylethyl group which may be substituted when Z is sulfur.
摘要翻译：由式（I）表示的化合物或其盐; 以及用于保护脑/神经元细胞或用于睡眠障碍的治疗剂的药剂，其包含所述化合物或盐：其中Z表示氧或硫; R1表示可被取代的芳基或杂环基，条件是R 1不是3-乙基-6-甲氧基-2-甲基-5-萘-1-基; R 1a表示氢原子，可被取代的烃基，羟基等; R2代表可被取代的哌啶-1,4-二基或哌嗪-1,4-二基; R3表示通过从可以具有取代基的苯环或6元芳族杂环除去2个氢原子而形成的二价基团，条件是R 3不是哒嗪-3,6-二基; 并且R 4表示通过从可以被取代的苯环或5-至6-元杂环除去一个氢原子而形成的基团，条件是杂环上的取代基不是Z时可以被取代的苯基乙基是硫。

19. 发明申请

US20100234389A1 AMIDE COMPOUND 审中-公开
标题翻译：酰胺化合物
公开(公告)号：US20100234389A1
公开(公告)日：2010-09-16
申请号：US12681854
申请日：2008-10-09
申请人： Masakuni Kori , Mitsunori Kouno
发明人： Masakuni Kori , Mitsunori Kouno
IPC分类号： A61K31/506 , C07D403/14 , A61K31/497 , C07D241/04 , A61K31/4965 , C07D413/12 , C07D403/12 , A61P25/22 , A61P25/24 , A61P29/00
CPC分类号： C07D213/75 , C07D213/74 , C07D231/40 , C07D237/20 , C07D241/20 , C07D261/14 , C07D295/205 , C07D401/12 , C07D403/12 , C07D413/12
摘要： An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic.The present invention relates to a compound represented by formula (I): wherein symbols are as defined in the specification, or salt thereof.
摘要翻译：本发明的目的是提供一种具有FAAH抑制作用并可用作止痛剂的新型稠环化合物。本发明涉及由式（I）表示的化合物：其中符号如说明书中所定义，或其盐。

20. 发明申请

US20100041891A1 AMIDE COMPOUND 审中-公开
标题翻译：酰胺化合物
公开(公告)号：US20100041891A1
公开(公告)日：2010-02-18
申请号：US12539559
申请日：2009-08-11
申请人： Masaki Setoh , Mitsunori Kouno , Yuhei Miyanohana , Masakuni Kori
发明人： Masaki Setoh , Mitsunori Kouno , Yuhei Miyanohana , Masakuni Kori
IPC分类号： C07D409/06 , C07D235/24 , C07D277/62
CPC分类号： C07D217/04 , C07D209/10 , C07D209/46 , C07D231/56 , C07D235/10 , C07D235/26 , C07D235/28 , C07D235/30 , C07D263/56 , C07D277/64 , C07D277/68 , C07D307/79 , C07D333/54 , C07D401/04 , C07D405/04 , C07D405/12 , C07D407/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D411/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/048
摘要： A compound having GPR52 agonist activity or a salt thereof is provided.The compound can be provided as a preventive/therapeutic agent for schizophrenia or the like. The compound is represented by the following formula: whereinA represents —CONRa— or —NRaCO—, Ra represents a hydrogen atom or the like, B represents a hydrogen atom or the like, a ring Cy1 represents a six-membered aromatic ring which may have one or more substituents in addition to a group represented by -A-B, a ring Cy2 represents a six-membered ring which may be substituted with a halogen atom or the like, a ring Cy3 represents a five- or six-membered ring which may have one or more substituents; X represents C1-2 alkylene or the like, m represents an integer of 0 to 2, and a ring Cy4 represents a six-membered aromatic ring which may have one or more substituents.
摘要翻译：提供具有GPR52激动剂活性的化合物或其盐。该化合物可以作为精神分裂症等的预防/治疗剂提供。该化合物由下式表示：其中A表示-CONRa-或-NRaCO-，Ra表示氢原子等，B表示氢原子等，环Cy1表示可以含有六元芳环的六元芳环除了由-AB表示的基团之外还具有一个或多个取代基，环Cy2表示可被卤素原子等取代的六元环，环Cy3表示五元或六元环，其可以具有一个或多个取代基; X表示C1-2亚烷基等，m表示0〜2的整数，环Cy4表示可具有一个以上取代基的六元芳香环。

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