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1. 发明授权

US06673781B1 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：US06673781B1
公开(公告)日：2004-01-06
申请号：US10048348
申请日：2002-02-01
申请人： Mitsuaki Ohtani , Masahiro Fuji , Tetsuo Okada , Makoto Adachi , Tomoyuki Ogawa
发明人： Mitsuaki Ohtani , Masahiro Fuji , Tetsuo Okada , Makoto Adachi , Tomoyuki Ogawa
IPC分类号： C07D47104
CPC分类号： C07D471/04 , C07D471/14 , C07D491/14
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 CONH2 or CONHNH2; 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; 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。由式（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，杂环基等; R 2是CONH 2或CONHNH 2; 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; 其前体药物，其药学上可接受的盐或溶剂化物。

2. 发明授权

US06407104B1 Pyrrolo[1,2-a]pyrazine spla2 inhibitor 失效
标题翻译：吡咯并[1,2-a]吡嗪spl2抑制剂
公开(公告)号：US06407104B1
公开(公告)日：2002-06-18
申请号：US09623591
申请日：2000-09-05
申请人： Mitsuaki Ohtani , Masahiro Fuji , Tetsuo Okada
发明人： Mitsuaki Ohtani , Masahiro Fuji , Tetsuo Okada
IPC分类号： A61K31519
CPC分类号： A61K31/495 , C07D487/04
摘要： 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, C3 to C4 cycloalkyl or the like group; R3 is —(L2)-(acidic group); R4 and R5 are hydrogen atoms, non-interfering substituents, carbocyclic groups or the like; RA is —C(═X)—C(═X)—NH2 or the like; and X is independently oxygen atom or sulfur atom; 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：其中R1为 - （L1）-R6，其中L1为1至18个原子等的二价连接基团，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，C3-C4环烷基等基团; 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; RA是-C（= X）-C（= X）-NH 2等; X独立地为氧原子或硫原子; 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。

3. 发明授权

US06756376B1 Tricyclic azaindolizine derivatives having an sPLA2-inhibitory activities 失效
标题翻译：具有sPLA2抑制活性的三环唑烷衍生物
公开(公告)号：US06756376B1
公开(公告)日：2004-06-29
申请号：US10129658
申请日：2002-05-09
申请人： Masahiro Fuji , Tetsuo Okada , Makoto Adachi
发明人： Masahiro Fuji , Tetsuo Okada , Makoto Adachi
IPC分类号： C07D48704
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 E is N or C—R4; G is N or C—R25; R1 is a carbocyclic group, heterocyclic group or the like; one of R3 and R4 is —(L2)-(acidic group), the other is a hydrogen atom, wherein L2 is a group connecting with an acid group; A ring is optionally substituted 5-8 membered cyclohexane ring or cyclohexene ring; R24 and R25 are a hydrogen atom or the like, its prodrug, their pharmaceutically acceptable salt, or hydrate 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E为N或C-R 4; G是N或C-R 25; R 1是碳环基，杂环基等; R 3和R 4中的一个是 - （L 2） - （酸性基团），另一个是氢原子，其中L 2是与酸基连接的基团; 环是任选取代的5-8元环己烷环或环己烯环; R 24和R 25是氢原子等，其前药，其药学上可接受的盐或水合物。

4. 发明申请

US20060014766A1 Crystalline salts of 7- '4-(4-fluorophenyl) -6-isopropyl-2-'methyl (methylsulfonyl) amino! pyrimidin-5-yl!- (3R, 5S) - 3, 5-dihydroxyhept-6-enoic acid 有权
标题翻译： 7-（4-氟苯基）-6-异丙基-2-甲基（甲基磺酰基）氨基的结晶盐嘧啶-5-基 - （3R，5S）-3,5-二羟基庚-6-烯酸
公开(公告)号：US20060014766A1
公开(公告)日：2006-01-19
申请号：US10985019
申请日：2004-11-10
申请人： Nigel Taylor , Tetsuo Okada
发明人： Nigel Taylor , Tetsuo Okada
IPC分类号： A61K31/513 , C07D239/02
CPC分类号： C07D239/42
摘要： The invention relates to crystalline salts of the compound (E)-7-[4-(4-fluorophenyl)isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid of formula (I), as well as processes for their manufacture, pharmaceutical compositions containing them, and their uses.
摘要翻译：本发明涉及化合物（E）-7- [4-（4-氟苯基）异丙基-2- [甲基（甲基磺酰基）氨基]嘧啶-5-基] - （3R，5S）-3,5 （I）的二羟基庚-6-烯酸，以及其制备方法，含有它们的药物组合物及其用途。

5. 发明授权

US06699891B1 Npyy5 antagonists 失效
标题翻译： Npyy5拮抗剂
公开(公告)号：US06699891B1
公开(公告)日：2004-03-02
申请号：US10111981
申请日：2002-05-01
申请人： Yasuyuki Kawanishi , Hideyuki Takenaka , Kohji Hanasaki , Tetsuo Okada
发明人： Yasuyuki Kawanishi , Hideyuki Takenaka , Kohji Hanasaki , Tetsuo Okada
IPC分类号： A61K3144
CPC分类号： C07D249/08 , A61K31/00 , A61K31/18 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/37 , A61K31/381 , A61K31/4015 , A61K31/402 , A61K31/4035 , A61K31/41 , A61K31/4196 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/433 , A61K31/44 , A61K31/4409 , A61K31/4453 , A61K31/451 , A61K31/495 , A61K31/4965 , A61K31/505 , A61K31/5375 , A61K31/63 , A61K31/635 , C07C311/06 , C07C311/07 , C07C311/08 , C07C311/14 , C07C311/20 , C07C311/21 , C07C311/46 , C07C323/40 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/44 , C07C2603/18 , C07D207/09 , C07D207/12 , C07D207/16 , C07D209/08 , C07D209/48 , C07D209/88 , C07D211/58 , C07D211/62 , C07D213/75 , C07D213/82 , C07D215/36 , C07D215/38 , C07D217/04 , C07D219/10 , C07D231/12 , C07D231/16 , C07D231/56 , C07D233/56 , C07D233/68 , C07D239/42 , C07D277/56 , C07D277/70 , C07D285/06 , C07D295/135 , C07D307/68 , C07D307/91 , C07D311/16 , C07D317/66 , C07D333/38 , C07D333/72
摘要： The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof.
摘要翻译：本发明提供用作NPY Y5受体拮抗剂的药物组合物，其包含式（I）化合物：其中R 1为低级烷基，环烷基等，R 2为氢，低级烷基或 n为1或2，X为低级亚烷基，低级亚烯基，亚芳基，亚环烷基等，Y为CONR 7，CSNR 7，NR 7 CO，NR 7 CS等， Z是低级烷基，任选取代的碳环基，任选取代的杂环基等，R 7是氢或低级烷基，前药，药学上可接受的盐或溶剂化物。

6. 发明授权

US4525355A 7-.beta.-Ureidoacetamido-oxacephalosporins 失效
标题翻译： 7-β-脲基乙酰氨基 - 氧杂七环素
公开(公告)号：US4525355A
公开(公告)日：1985-06-25
申请号：US566023
申请日：1983-12-27
申请人： Masayuki Narisada , Fumihiko Watanabe , Tetsuo Okada , Hiromu Matsumura
发明人： Masayuki Narisada , Fumihiko Watanabe , Tetsuo Okada , Hiromu Matsumura
IPC分类号： A61K31/535 , A61P31/04 , C07D505/00 , C07D498/04
CPC分类号： C07D505/00 , Y02P20/55
摘要： A 7.beta.-ureidoacetamido-7.alpha.-methoxy-3-(1-carbamoylmethyl-1H-tetrazol-5-yl)thiomethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acid derivative represented by the following formula: ##STR1## wherein Ar is phenyl, hydroxyphenyl, or thienyl and R is hydrogen, a light metal, or a carboxy-protecting group.
摘要翻译：由以下所示的7β-脲基乙酰胺基-7α-甲氧基-3-（1-氨基甲酰基甲基-1H-四唑-5-基）硫代甲基-1-脱硫-1-氧代-3-头孢烯-4-羧酸衍生物式：其中Ar是苯基，羟基苯基或噻吩基，R是氢，轻金属或羧基保护基。

7. 发明授权

US4903938A Micro flow control valve 失效
标题翻译：微流量控制阀
公开(公告)号：US4903938A
公开(公告)日：1990-02-27
申请号：US179942
申请日：1988-04-11
申请人： Jun-ichi Nishizawa , Shinzo Kasai , Tetsuo Okada , Mitsuhiko Dohzono
发明人： Jun-ichi Nishizawa , Shinzo Kasai , Tetsuo Okada , Mitsuhiko Dohzono
IPC分类号： F16K1/34 , F16K51/02
CPC分类号： F16K1/34 , F16K51/02
摘要： Disclosed is a micro gas flow rate control valve which is used in semi-conductor producing system operated under a high vacuum or various apparatus for analysis. The valve uses combination of a flat surface valve tip and a flat surface valve seat of cylindrical shape, and is capable of controlling minute flow and durable even used under severe conditions of high pressure differences and large temperature changes to have stable performance. Also enclosed is a metal-ceramics sealing mechanism suitable for the above valve. The sealing mechanism uses, in addition to a sealing member made of a soft metal, a seal assisting member, and durable under the conditions of repeated temperature changes.
摘要翻译：公开了一种微气体流量控制阀，其用于在高真空下操作的半导体生产系统或用于分析的各种装置。该阀采用平面阀头和圆柱形平面阀座的组合，能够在高压差和大温度变化的严酷条件下使用，并且能够控制微流量，耐用性能稳定。还包括适用于上述阀门的金属 - 陶瓷密封机构。密封机构除了由软金属制成的密封构件以外还使用密封辅助构件，并且在重复的温度变化的条件下使用。

8. 发明授权

US4371532A Malonamidooxadethiacephem compounds 失效
标题翻译：马洛替胺恶唑硫醚化合物
公开(公告)号：US4371532A
公开(公告)日：1983-02-01
申请号：US227202
申请日：1981-01-22
申请人： Masayuki Narisada , Tetsuo Okada
发明人： Masayuki Narisada , Tetsuo Okada
IPC分类号： A61K31/535 , A61P31/04 , C07D505/00 , C07D413/14 , A61K31/425 , C07D498/04
CPC分类号： C07D505/00
摘要： An antibacterial compound represented by the following formula: ##STR1## (wherein R is a hydrogen atom or a lower alkyl, lower alkenyl, lower alkynyl or lower alkylthio-lower alkyl group;B.sup.1 and B.sup.2 each is a hydrogen atom or an ester or salt forming group or atom same or different for each; andHet is a monocyclic hetero-cyclic group)showing strong antipseudomonal activity, process for preparing the same, pharmaceutical preparation containing the same and method for combating bacterial infection by applying the same.
摘要翻译：由下式表示的抗菌化合物：其中R是氢原子或低级烷基，低级烯基，低级炔基或低级烷硫基 - 低级烷基; B1和B2各自是氢原子或酯或成盐基团或每个相同或不同的原子; Het是单环杂环基团），其显示出强的抗假单胞菌活性，其制备方法，含有该药物的药物制剂和通过应用它们来防治细菌感染的方法。

9. 发明申请

US20070255060A1 Process for the Manufacture of the Calcium Salt of Rosuvastatin (E)-7-'4-(4-Fluorophenyl)-6-Isopropyl-2-'Methyl (Methylsulfonyl) Amino ! Pyrmidin -5-Yl! (3R, 5S)-3,5-Dihydroxyhept-6-Enoic Acid and Crystalline Intermediates Thereof 审中-公开
标题翻译：罗苏伐他汀（E）-7-（4-（4-氟苯基）-6-异丙基-2-甲基（甲基磺酰基）氨基铵盐的制造方法嘧啶-5-Y1 （3R，5S）-3,5-二羟基庚-6-烯酸及其结晶中间体
公开(公告)号：US20070255060A1
公开(公告)日：2007-11-01
申请号：US10576774
申请日：2004-10-22
申请人： Tetsuo Okada , John Horbury , David Laffan
发明人： Tetsuo Okada , John Horbury , David Laffan
IPC分类号： C07D405/06 , C07D239/42
CPC分类号： C07D239/42 , C07D405/06 , Y02P20/55
摘要： A process for the manufacture of the calcium salt of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)3,5-dihydroxyhept-6-enoic acid, useful as an HMGCoA reductase inhibitor, from a compound of the formula (7) wherein A is an acetal or ketal protecting group and R is alkyl, via isolated crystalline compounds of the formula (8) or of formula (10) is described. Crystalline intermediates of formulae 7, 8 and 10 are also described.
摘要翻译：（E）-7- [4-（4-氟苯基）-6-异丙基-2- [甲基（甲基磺酰基）氨基]嘧啶-5-基]（3R，5S）3的钙盐的制备方法通过分离的式（8）的结晶化合物，其中A为缩醛或缩酮保护基且R为烷基的式（7）化合物可用作HMGCoA还原酶抑制剂的5-二羟基庚-6-烯酸，或式（10）的化合物。还描述了式7,8和10的结晶中间体。

10. 发明授权

US06462241B2 Process for preparing benzothiophenecarboxamide derivatives 失效
公开(公告)号：US06462241B2
公开(公告)日：2002-10-08
申请号：US10133353
申请日：2002-04-29
申请人： Tetsuo Okada , Makoto Kakinuma
发明人： Tetsuo Okada , Makoto Kakinuma
IPC分类号： C07C20936
CPC分类号： C07D333/68 , C07C213/02 , C07C2602/42 , C07C215/42
摘要： A process for preparing a compound having PGD2 antagonism represented by the formula (I), or a pharmaceutically acceptable salt or hydrate thereof, which process comprises reacting an amino alcohol of the formula (II) or its salt with a compound of the formula (III) or its reactive derivative, oxidizing the product with halo oxoacid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyls, reacting the product with an ylide under the conditions for Wittig reaction, and optionally deprotecting the product.

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