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1. 发明申请

US20110190351A1 Benzoimidazole Derivatives and Glycogen Synthase Kinase-3 Beta Inhibitors Containing the Same 审中-公开
标题翻译：苯并咪唑衍生物和含有其的糖原合酶激酶-3β抑制剂
公开(公告)号：US20110190351A1
公开(公告)日：2011-08-04
申请号：US13056591
申请日：2009-07-30
申请人： Mitsuaki Ohtani , Yo Matsuo , Yingfu Li , Joel R. Walker , David M. Jenkins , Feryan Ahmed , Ryuji Ohsawa , Shoji Hisada
发明人： Mitsuaki Ohtani , Yo Matsuo , Yingfu Li , Joel R. Walker , David M. Jenkins , Feryan Ahmed , Ryuji Ohsawa , Shoji Hisada
IPC分类号： A61K31/4439 , C07D409/04 , A61K31/4184 , C07D403/04 , C07D235/04 , C07D417/12 , A61K31/427 , C07D409/14 , A61K31/422 , C07D413/14 , A61P25/28 , A61P25/24 , A61P25/06 , A61P3/10
CPC分类号： C07D409/04 , C07D235/18 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： Benzoimidazole Derivatives are provided. The compounds of the present invention are useful for Glycogen Synthase Kinase-3 Beta Inhibitors.
摘要翻译：提供苯并咪唑衍生物。本发明的化合物可用于糖原合酶激酶-3β抑制剂。

2. 发明授权

US07074836B1 Para-terphenyl compounds 失效
标题翻译：对三联苯化合物
公开(公告)号：US07074836B1
公开(公告)日：2006-07-11
申请号：US10705505
申请日：2003-11-12
申请人： Kenji Kawada , Mitsuaki Ohtani , Ryuji Suzuki , Akinori Arimura
发明人： Kenji Kawada , Mitsuaki Ohtani , Ryuji Suzuki , Akinori Arimura
IPC分类号： A61K31/075 , A61K31/09 , C07C43/205 , C07C43/225 , C07C43/23
CPC分类号： C07D213/30 , C07C15/14 , C07C43/225 , C07C43/23 , C07C43/253 , C07C43/315 , C07C45/68 , C07C47/57 , C07C47/575 , C07C59/64 , C07C59/70 , C07C65/24 , C07C65/28 , C07C69/712 , C07C69/734 , C07C69/94 , C07C205/35 , C07C205/37 , C07C217/20 , C07C217/76 , C07C217/80 , C07C229/52 , C07C233/25 , C07C233/27 , C07C233/80 , C07C235/60 , C07C251/38 , C07C251/60 , C07C255/54 , C07C271/28 , C07C275/32 , C07C281/04 , C07C281/10 , C07C307/10 , C07C309/65 , C07C309/66 , C07C309/73 , C07C311/08 , C07C311/21 , C07C311/29 , C07C317/22 , C07C327/42 , C07D215/14 , C07D239/54 , C07D295/30 , C07D307/42 , C07D309/22 , C07D317/54 , C07D319/20 , C07D333/28 , C07D333/38 , C07D333/54 , C09K2019/123
摘要： The present invention provides a selective suppressor of the IgE production comprising a compound which suppresses the IgE production in a process from a differentiation of a mature B cell into an antibody-producing cell to the production of an antibody and which does not suppress or weakly suppresses the production of IgG, IgM and/or IgA which are produced at the same time, a compound of the formula (I): wherein R1–R13 are hydrogen, halogen, lower alkyl, lower alkoxy or the like, X is —O—, —CH2—, NR14— or —S(O)p— and Y is lower alkyl, lower alkenyl or the like, a process for producing the same and a pharmaceutical composition comprising the same.
摘要翻译：本发明提供了IgE生产的选择性抑制剂，其包含抑制从成熟B细胞分化成抗体产生细胞至产生抗体并且不抑制或弱抑制的过程中的IgE产生的化合物同时产生的IgG，IgM和/或IgA的制备，式（I）的化合物：其中R 1 -R 13是氢，卤素，低级烷基，低级烷氧基等，X是-O-，-CH 2 - ，NR 14 - 或-S（O）p-和Y是低级烷基，低级烯基等，其制备方法和含有该方法的药物组合物。

3. 发明授权

US06919375B1 Sulfonated amino acid derivatives and metalloproteinase inhibitors containing the same 失效
公开(公告)号：US06919375B1
公开(公告)日：2005-07-19
申请号：US09120383
申请日：1998-07-22
申请人： Fumihiko Wantanabe , Hiroshige Tsuzuki , Mitsuaki Ohtani
发明人： Fumihiko Wantanabe , Hiroshige Tsuzuki , Mitsuaki Ohtani
IPC分类号： C07C311/06 , C07C311/13 , C07C311/19 , C07C311/29 , C07C311/32 , C07C311/42 , C07C311/46 , C07C311/47 , C07C311/49 , C07C323/62 , C07C323/67 , C07D209/20 , C07D209/42 , C07D213/54 , C07D213/55 , C07D213/81 , C07D213/82 , C07D235/16 , C07D241/24 , C07D257/04 , C07D261/18 , C07D277/30 , C07D277/64 , C07D333/34 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/195
CPC分类号： C07D209/42 , C07C311/06 , C07C311/13 , C07C311/19 , C07C311/29 , C07C311/42 , C07C311/46 , C07C311/47 , C07C311/49 , C07C323/62 , C07C323/67 , C07C2601/14 , C07D209/20 , C07D213/54 , C07D213/55 , C07D213/81 , C07D213/82 , C07D235/16 , C07D241/24 , C07D257/04 , C07D261/18 , C07D277/30 , C07D277/64 , C07D333/34 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.

4. 发明授权

US06703385B1 Tricyclic compounds having sPLA2-inhibitory activities 失效
标题翻译：具有sPLA2抑制活性的三环化合物
公开(公告)号：US06703385B1
公开(公告)日：2004-03-09
申请号：US10031443
申请日：2002-01-22
申请人： Mitsuaki Ohtani , Masahiro Fuji , Makoto Adachi , Tomoyuki Ogawa
发明人： Mitsuaki Ohtani , Masahiro Fuji , Makoto Adachi , Tomoyuki Ogawa
IPC分类号： A61K3133
CPC分类号： C07D471/04
摘要： The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is COCONH2 or the like; Q1 is a nitrogen atom or C—R4; one of R3 and R4 is —(L2)-(acidic group) wherein L2 is a group connecting with an acid group and the length of the connecting groups 1 to 5 atoms, and the other is a hydrogen atom; R21 and R22 are hydrogen atoms or the like; X is —CR23R24— or the like wherein R23 and R24 are hydrogen atoms or the like; Y is —CR25R26— or the like wherein R25 and R26 are hydrogen atoms or the like; Z is CH2 or the like; a broken line ( - - - ) represents the presence or absence of a bond, its prodrug, their pharmaceutically acceptable salt, or solvate thereof.
摘要翻译：本发明提供具有sPLA2抑制活性的化合物。式（I）表示的化合物：其中R 1为（a）C 1至C 20烷基，C 2至C 20烯基，C 2至C 20炔基，碳环基，杂环基或类似物; R 2是COCONH 2等; Q 1是氮原子或C-R 4; R 3和R 4之一是 - （L 2） - （酸性基团）其中L 2是与酸基连接的基团和连接基团的长度为1至5个原子，以及另一个是氢原子; R 21和R 22是氢原子等; X是-CR 23 R 24 - 等，其中R 23和R 24是氢原子等; Y是-CR 25 R 26 - 等，其中R 25和R 26是氢原子等; Z是CH 2等; 虚线（ - - - ）表示键的存在或不存在，其前体药物，其药学上可接受的盐或溶剂合物。

5. 发明授权

US06645976B1 Indolizine SPLA2inhibitors 失效
标题翻译： Indolizine SPLA2抑制剂
公开(公告)号：US06645976B1
公开(公告)日：2003-11-11
申请号：US08765566
申请日：1997-04-28
申请人： Robert D. Dillard , Sanji Hagishita , Mitsuaki Ohtani
发明人： Robert D. Dillard , Sanji Hagishita , Mitsuaki Ohtani
IPC分类号： C07D22104
CPC分类号： C07D471/04 , C07F9/6561
摘要： A class of novel indolizine-1-functional compounds and indolizine-3-functional compounds is disclosed together with the use of such indolizine compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock. The compounds are indolizine-1-acetamides, indolizine-1-acetic acid hydrazides, indolizine-1-glyoxylamides, indolizine-3-acetamides, indolizine-3-acetic acid hydraxides, and indolizine-3-glyoxylasides.
摘要翻译：公开了一类新的中氮嗪-1-功能化合物和中氮嗪-3-功能化合物，以及使用这种中氮茚化合物来抑制sPLA2介导的脂肪酸释放以治疗诸如败血性休克的病症。所述化合物为中氮茚-1-乙酰胺，中氮茚-1-乙酸酰肼，中氮茚-1-乙醛酰胺，中氮茚-3-乙酰胺，中氮茚-3-乙酸氢氧化物和中氮茚-3-乙醛酸酯。

6. 发明授权

US06472389B1 Pyrrolo[1,2-b] pyridazine derivatives having sPLA2 inhibitory effect 失效
标题翻译：具有sPLA2抑制作用的吡咯并[1,2-b]哒嗪衍生物
公开(公告)号：US06472389B1
公开(公告)日：2002-10-29
申请号：US09673413
申请日：2000-10-18
申请人： Mitsuaki Ohtani , Masahiro Fuji , Yoshikazu Fukui , Makoto Adachi
发明人： Mitsuaki Ohtani , Masahiro Fuji , Yoshikazu Fukui , Makoto Adachi
IPC分类号： A61K315025
CPC分类号： C07D487/04
摘要： The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is —(L1)—R6 wherein L1 is a divalent linking group of 1 to 18 atoms or the like, and R6 is a carbocyclic ring substituted by at least one non-interfering substituent or the like; R2 is C1 to C3 alkyl or the like; R3 is —(L2)-(acidic group); R4 and R5 are hydrogen atoms, non-interfering substituents, carbocyclic groups or the like; X is independently oxygen atom of sulfur atom; and RA is —C(═X)—C(═X)—NH2 or the like; the prodrugs thereof, their pharmaceutically acceptable salts, or their solvates, and a composition for inhibiting sPLA2 containing them as effective ingredients.
摘要翻译：本发明提供具有sPLA2抑制活性的化合物。式（I）表示的化合物：其中R1为 - （L1）-R6，其中L1为1至18个原子的二价连接基团等，R6为被至少一个非干扰取代基等取代的碳环; R2是C1-C3烷基等; R3是 - （L2） - （酸性基团）; R4和R5是氢原子，非干扰取代基，碳环基团等; X独立地是硫原子的氧原子; RA为-C（= X）-C（= X）-NH 2等; 其前体药物，其药学上可接受的盐或其溶剂合物，以及用于抑制含有它们作为有效成分的sPLA2的组合物。

7. 发明授权

US6147100A Pyrrolidine derivatives having phospholipase A.sub.2 inhibitory activity 失效
标题翻译：具有磷脂酶A2抑制活性的吡咯烷衍生物
公开(公告)号：US6147100A
公开(公告)日：2000-11-14
申请号：US355008
申请日：1999-07-22
申请人： Kaoru Seno , Mitsuaki Ohtani , Fumihiko Watanabe
发明人： Kaoru Seno , Mitsuaki Ohtani , Fumihiko Watanabe
IPC分类号： A61K31/26 , A61P29/00 , C07D413/12 , C07D417/12 , C07D417/14 , A61K31/426
CPC分类号： C07D413/12 , C07D417/12 , C07D417/14
摘要： A compound represented by the formula (I): ##STR1## wherein, for example, R.sup.1 is optionally substituted aralkyl, Z is nitrogen atom which optionally substituted with alkyl, X.sup.1 is --CH.sub.2 NHCO--, X.sup.2 is phenylene, X.sup.3 is a bond, Y.sup.2 is optionally substituted aryl, B is oxygen atom, its pharmaceutically acceptable salt, or hydrate thereof and a pharmaceutical composition which contains them as an active ingredient.
摘要翻译： PCT No.PCT / JP98 / 00307 Sec。 371日期：1999年7月22日 102（e）日期1999年7月22日PCT提交1998年1月27日PCT公布。公开号WO98 / 33797 日期：1998年6月8日由式（I）表示的化合物：其中，例如，R 1为任选取代的芳烷基，Z为任选被烷基取代的氮原子，X 1为-CH 2 NHCO-，X 2为亚苯基，X 3为键，Y2为任选取代的芳基，B为氧原子，其药学上可接受的盐或水合物，以及含有它们作为活性成分的药物组合物。

8. 发明授权

US5117039A Monoesters of arylacetic acid and the process thereof 失效
标题翻译：芳香酸单酯及其制备方法
公开(公告)号：US5117039A
公开(公告)日：1992-05-26
申请号：US447518
申请日：1989-12-07
申请人： Mitsuaki Ohtani , Takaharu Matsuura , Toshiro Konoike , Yoshitaka Araki
发明人： Mitsuaki Ohtani , Takaharu Matsuura , Toshiro Konoike , Yoshitaka Araki
IPC分类号： C07C69/753
CPC分类号： C07C69/753 , Y02P20/55
摘要： An optically active ester of arylacetic acid of the fomula: ##STR1## wherein R.sup.1 is hydrogen or optionally substituted C.sub.1 -C.sub.2 alkyl or phenyl or taken together to from C.sub.2 -C.sub.6 alkylene, or C.sub.2 C.sub.4 -C.sub.6 alkenylene, or bicyclic-ring; R.sup.2 is hydrogen or methyl; X is single bond or Ch.sub.2, C.dbd.O, N--R.sup.4, O, S, CHNHR.sup.4, CHCH.sub.3, CH--Ar, or CHOR.sup.5 (provided that when X is single bond or CH.sub.2, C.dbd.O, N--R.sup.4, O, or S, R.sup.1 and R.sup.2 are not simultaneouly hydrogen or methyl); R.sup.3 is hydrogen, optionally substituted alkyl, or optionally substituted aralkyl; R.sup.4 is hydrogen or amino protecting group; R.sup.5 is hydrogen or hydroxy protecting group; and Ar is optionally substituted aryl; prepared by the reaction of a 94 symmetric acid anhydride with an (R)-or (S)-arylacetic acid derivative in high optical purity; useful as a intermediate for the various optically active natural products and medicines.

9. 发明授权

US5043451A Bicyclo (2.2.1.) hept-exo-2-yl and bicyclo (2.2.2.) oct-endo-2-yl compounds 失效
标题翻译：双环（2.2.1。）庚 - 外-2-基和双环（2.2.2。）辛 - 内-2-基化合物
公开(公告)号：US5043451A
公开(公告)日：1991-08-27
申请号：US516140
申请日：1990-04-27
申请人： Mitsuaki Ohtani , Fumihiko Watanabe , Tadadiko Tsushima , Kenji Kawada , Susumu Kamata
发明人： Mitsuaki Ohtani , Fumihiko Watanabe , Tadadiko Tsushima , Kenji Kawada , Susumu Kamata
IPC分类号： C07D493/08 , A61K31/00 , A61K31/335 , A61K31/336 , A61K31/34 , A61K31/557 , A61P7/02 , A61P9/08 , A61P11/08 , C07C20060101 , C07C67/00 , C07C301/00 , C07C311/00 , C07C311/02 , C07C311/07 , C07C311/10 , C07C311/13 , C07C311/15 , C07C311/20 , C07C311/37 , C07C313/00 , C07C323/52 , C07D209/52 , C07D209/56 , C07D213/34 , C07D213/71 , C07D221/22 , C07D303/40 , C07D303/46 , C07D331/02 , C07D491/044 , C07D493/04 , C07D495/04
CPC分类号： C07D493/08 , C07D213/34 , Y02P20/55
摘要： There are provided compounds of the formula: ##STR1## wherein R.sub.1 is a hydrogen or C.sub.1 -C.sub.5 alkyl; R.sub.2 is an C.sub.1 -C.sub.10 alkyl, aryl, aralkyl, or pyridyl, where the aryl, aralkyl, or pyridyl are unsubstituted or are substituted by C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, nitro, hydroxy, carboxy, amino, C.sub.1 -C.sub.5 alkylamino, C.sub.1 -C.sub.5 dialkylamino whose two alkyl groups may be different from each other, C.sub.2 -C.sub.3 alkanoylamino, or halogen and X is an C.sub.1 -C.sub.7 alkylene, C.sub.2 -C.sub.7 alkenylene, --CH(F)CH.dbd.CH(CH.sub.2).sub.3 --, --(CH.sub.2).sub.3 --S--(CH.sub.2).sub.2 --, --CH.sub.2).sub.2 --S--(CH.sub.2).sub.3 --, --C.sub.6 H.sub.4 --O--CH.sub.2 --or --CH.sub.2 CH.dbd.CH--m--C.sub.6 H.sub.4 --, or their pharmaceutically acceptable salts. The compounds are useful as antithrombotic, anti-vasoconstricting and anti-bronchoconstricting drugs.

10. 发明授权

US4960909A 7-oxabicyclo[2.2.1] heptane sulfonamide derivatives 失效
标题翻译： 7-氧杂二环[2.2.1]庚烷磺酰胺衍生物
公开(公告)号：US4960909A
公开(公告)日：1990-10-02
申请号：US327772
申请日：1989-03-23
申请人： Masayuki Narisada , Mitsuaki Ohtani , Fumihiko Watanabe , Sanji Hagishita , Kaoru Seno , Susumu Kamata , Nobuhiro Haga , Tatsuo Tsuri , Tadahiko Tsushima , Kenji Kawada
发明人： Masayuki Narisada , Mitsuaki Ohtani , Fumihiko Watanabe , Sanji Hagishita , Kaoru Seno , Susumu Kamata , Nobuhiro Haga , Tatsuo Tsuri , Tadahiko Tsushima , Kenji Kawada
IPC分类号： C07D493/08 , A61K31/00 , A61K31/335 , A61K31/336 , A61K31/34 , A61K31/557 , A61P7/02 , A61P9/08 , A61P11/08 , C07C20060101 , C07C67/00 , C07C301/00 , C07C311/00 , C07C311/02 , C07C311/07 , C07C311/10 , C07C311/13 , C07C311/15 , C07C311/20 , C07C311/37 , C07C313/00 , C07C323/52 , C07D209/52 , C07D209/56 , C07D213/34 , C07D213/71 , C07D221/22 , C07D303/40 , C07D303/46 , C07D331/02 , C07D491/044 , C07D493/04 , C07D495/04
CPC分类号： C07D493/08 , C07D213/34 , Y02P20/55
摘要： Bicyclic sulfonamido derivatives represented by the formula: ##STR1## wherein R.sub.1 is a hydrogen or lower alkyl; R.sub.2 is an alkyl, substituted or unsubstituted aryl, aralkyl or hetelocycle; R.sub.3 is a hydrogen or methyl; X is an alkylene or alkenylene which may be substituted by a fluorine atom or atoms and may contain an oxygen, sulfur and/or phenylene in the chain; Y is straight or branched alkylene or alkenylene oxygen, or sulfur; m is 0 or 1; and n is 0, 1 or 2, or their salt, said derivatives being useful as antithrombotic, anti-vasoconstricting, and anti-bronchoconstricting drugs.

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