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11. 发明专利

JP2008044948A Process for manufacturing calcium salt of rosuvastatin(e)-7-[4-(4-fluorophenyl)-6-iosopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3r, 5s)-3,5-dihydroxyhept-6-enoic acid and crystalline intermediate thereof 审中-公开
标题翻译：制备ROSUVASTATIN（E）-7- [4-（4-氟代戊基）-6-多烯丙基-2- [甲基（甲基磺酰基）氨基]嘧啶-5-基]（3R，5S）-3,5的钙盐的方法 -DIHYDROXYHEPT-6-乙酸及其中间体
公开(公告)号：JP2008044948A
公开(公告)日：2008-02-28
申请号：JP2007228621
申请日：2007-09-04
申请人： Astrazeneca Uk Ltd , Shionogi & Co Ltd , アストラゼネカ・ユーケイ・リミテッドAstraZeneca UK Limited , 塩野義製薬株式会社
发明人： OKADA TETSUO , HORBURY JOHN , LAFFAN DAVID DERMOT PATRICK
IPC分类号： C07D239/42 , C07D405/06
CPC分类号： C07D239/42 , C07D405/06 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide a process for manufacturing a 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. SOLUTION: The process includes the acidic hydrolysis of an acetal protective group of a compound represented by formula (7) (wherein A is an acetal or ketal protective group; and R is alkyl), the isolation of a crystalline compound of the resultant compound, and the hydrolysis of the resultant compound, thus preparing a dihydroxycarboxylate derivative. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：要解决的问题：提供（E）-7- [4-（4-氟苯基）-6-异丙基-2- [甲基（甲基磺酰基）氨基]嘧啶-5-基的钙盐的制备方法，（3R，5S）-3,5-二羟基庚-6-烯酸。解决方案：该方法包括式（7）表示的化合物的缩醛保护基的酸性水解（其中A是缩醛或缩酮保护基; R是烷基），分离出所得化合物和所得化合物的水解，从而制备二羟基羧酸酯衍生物。版权所有（C）2008，JPO＆INPIT

12. 发明专利

JPH07118233A PRODUCTION OF PYRIMIDINE DERIVATIVE 失效
公开(公告)号：JPH07118233A
公开(公告)日：1995-05-09
申请号：JP26136593
申请日：1993-10-19
申请人： SHIONOGI & CO
发明人： OKADA TETSUO , KONOIKE TOSHIRO
IPC分类号： C07D239/26 , C07D213/55 , C07D215/14 , C07F7/18
摘要： PURPOSE:To facilitate the removal of by-products under mild conditions and obtain the pyrimidine derivative having inhibiting activities against 3-hydroxy-3- methylglutaryl coenzyme A (HMG-CoA) reductases by reacting a specific aldehyde compound with a specified ketophosphonate in the presence of a base in an organic solvent. CONSTITUTION:This process for producing a pyrimidine derivative expressed by formula III (R is an alkyl, a cycloalkyl, an aryl or amino; R and R are each H, an alkyl, a cycloalkyl or phenyl; R is H or carboxy-protecting group; R is H or a hydroxy-protecting group] is to react an aldehyde compound expressed by formula I [X is N or R C (R is an alkyl, or, together with the adjacent C may form a condensed benzene ring)] with a ketophosphonate derivative expressed by formula II (R and R are each an alkoxy) in the presence of a base in an organic solvent such as toluene at about ambient temperature. An HMG-CoA reductase inhibitor which is a central enzyme for biosynthesis of cholesterol can safely be produced in a high yield according to the method for production. This process is advantageous due to the use of the ketophosphonate derivative having high reactivity and by-products can readily be removed due to their water solubility.

13. 发明专利

JPH0532621A METHOD FOR OPTICALLY RESOLVING CYCLIC AMINE AND OPTICALLY ACTIVE ISOMER OBTAINED BY THE METHOD 失效
公开(公告)号：JPH0532621A
公开(公告)日：1993-02-09
申请号：JP32129091
申请日：1991-11-08
申请人： SHIONOGI & CO
发明人： OKADA TETSUO , TSUSHIMA TADAHIKO
IPC分类号： C07B57/00 , C07D207/22
摘要： PURPOSE:To readily and inexpensively produce in a high yield, a (-)-(S)-3- methylamino-4-methylenepyrrolidine derivative having a high optical purity and useful as a raw material for substituents to be introduced into various pyridone carboxylic acid series antibiotics. CONSTITUTION:A 3-methylamino-4-methylene pyrrolidine derivative of formula I (R is H, amino-protecting group) and L-(+)-tartaric acid in a molar ratio of 2:1 are subjected to a salt-forming reaction to form a tartaric acid salt of formula II. The salt of formula II is treated with a base and subsequently subjected to a protecting group-removing reaction to effectively and simply produce a (-)-(S)-3-methylamino-4-methylenepyrrolidine derivative. The L-(+)- tartaric acid is very inexpensive and can resolve the compound of formula I in a half amount in comparison with conventional methods. The L-(+)-tartaric acid does not require any complicated operation on the resolution and crystallization of the compound of formula I, and gives (-)-(S)-3-methylamino-4-methylene pyrrolidine derivative of formula III substantially quantitatively in a high yield of >=90% and in the optically pure form by a single crystallization and resolution process.

14. 发明专利

JPS5946933B2 JPS5946933B2 - 失效
公开(公告)号：JPS5946933B2
公开(公告)日：1984-11-15
申请号：JP7295374
申请日：1974-06-26
申请人： Shionogi & Co
发明人： HAMADA YOSHINORI , OKADA TETSUO
IPC分类号： C07D333/24 , C07C51/377 , C07D209/44 , C07D213/24 , C07D215/14 , C07D217/24 , C07D235/26 , C07D239/26 , C07D257/04 , C07D277/00 , C07D307/40 , C07D333/16

15. 发明专利

JP2008024712A Calcium salt of rosuvastatin : (e)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino] pyrimidin-5-yl](3r,5s)-3,5-dihydroxyhept-6-enoic acid, and, method for producing crystalline intermediates thereof 审中-公开
标题翻译：（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）-3,5-二羟基乙酸的盐酸盐 -6-酸，以及用于生产其结晶中间体的方法
公开(公告)号：JP2008024712A
公开(公告)日：2008-02-07
申请号：JP2007228620
申请日：2007-09-04
申请人： Astrazeneca Uk Ltd , Shionogi & Co Ltd , アストラゼネカ・ユーケイ・リミテッドAstraZeneca UK Limited , 塩野義製薬株式会社
发明人： OKADA TETSUO , HORBURY JOHN , LAFFAN DAVID DERMOT PATRICK
IPC分类号： C07D239/42 , A61K31/505 , A61P3/06 , A61P9/10 , A61P43/00 , C07D405/06
CPC分类号： C07D239/42 , C07D405/06 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide calcium salt of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhepta-6-enoate, and to provide a crystalline intermediate thereof. SOLUTION: The compound represented by formula (7) (A is an acetal or ketal-protecting group; R is an alkyl), and a crystalline intermediate such as a protecting group-free diol compound or lactone compound. These are used to produce a reductase inhibitor. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：提供（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）-3,5-二羟基庚-6-烯酸酯，并提供其结晶中间体。解决方案：由式（7）表示的化合物（A是缩醛或缩酮保护基; R是烷基）和结晶中间体如不含保护基的二醇化合物或内酯化合物。这些用于产生还原酶抑制剂。版权所有（C）2008，JPO＆INPIT

16. 发明专利

JPH0276875A QUINOLONECARBOXYLIC ACID DERIVATIVE 失效
公开(公告)号：JPH0276875A
公开(公告)日：1990-03-16
申请号：JP5880989
申请日：1989-03-10
申请人： SHIONOGI & CO
发明人： TSUJI SHOJI , SATO HISAO , OKADA TETSUO
IPC分类号： A61K31/47 , A61P31/04 , C07D401/04 , C07D409/14
摘要： NEW MATERIAL:Compounds represented by formula I [R is lower alkyl; R is H or lower alkyl; R is H or protecting group for amino; R is cyclopropyl, (substituted)phenyl or (substituted)thienyl; R is halogen] or salts thereof. EXAMPLE:1-Cyclopropyl-5-amino-6,8-difluoro-1,4-dihydro-7-(cis-3-methyl amino-4- methoxy-1-pyrolidinyl)-4-oxo-3-quinolinecarboxylic acid. USE:An antibacterial agent having a strong antibiotic action while central side effects such as convulsion are reduced. PREPARATION:For example, a compound of formula II is reacted with an amine of formula III to obtain a compound of formula I.

17. 发明专利

JPS6253992A PRODUCTION OF HYDROXYMETHYLCEPHEM 失效
公开(公告)号：JPS6253992A
公开(公告)日：1987-03-09
申请号：JP12532686
申请日：1986-05-29
申请人： SHIONOGI & CO
发明人： TSUJI SHOJI , OKADA TETSUO
IPC分类号： A61K31/545 , C07D501/00 , C07D501/04 , C07D501/26 , C07D501/28 , C07D501/34 , C07D501/57
摘要： PURPOSE:To obtain in high yield the titled compound useful as an antibacterial agent, by reacting a 7beta-acylaminocephalosporanic acid with an aqueous solution of an alkali metallic hydroxide in a lower alkanol. CONSTITUTION:A 7beta-acylaminocephalosporanic acid which may contain methoxy group at the 7alpha position is reacted with an aqueous solution of an alkali metallic hydroxide in a lower alkanol (preferably methanol, ethanol, propanol or butanol) preferably at -40-40 deg.C for 5min-3hr, to give a 7beta-acylamino-3- hydroxymethyl-3-cephem-4-carboxylic acid which may contain methoxy group at the 7alpha-position of its alkali metallic salt.

18. 发明专利

JPS5738783A Cephalosporin relating compound for oral administration 失效
标题翻译： CEPHOROSPORIN相关化合物用于口服管理
公开(公告)号：JPS5738783A
公开(公告)日：1982-03-03
申请号：JP10177980
申请日：1980-07-23
申请人： Shionogi & Co Ltd
发明人： NARISADA MASAYUKI , OKADA TETSUO , YOSHIDA TADASHI , MATSUURA SHINZOU
IPC分类号： A61K31/535 , A61P31/04 , C07D505/00
CPC分类号： C07D505/00
摘要： NEW MATERIAL:A cyanoalkaneamidooxacephalosporin derivative shown by the furmula I (A is lower alkyl, lower alkenyl, lower alkynyl; B
1 is H, salt-forming atom, salt-forming group, physiologically hydrolyzable ester group).
EXAMPLE: 7β-(2-Cyano-n-butyryl)amino-7α-methoxy-3-(1-methyl-5-tetrazolyl) thiomethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acid acetoxymethyl ester(formula II.
USE: An antimicrobial agent for oral administration or for injection. Effective for preventing and remedying infectious disease of urinary tract, infectious disease of inspiration, osteomyelitis, etc.
PROCESS: A corresponding compound is subjected to an operation, e.g., introduction of B
1 group, introduction of an acyl group in the side chain, introduction of cyano group, etc., to give a compound shown by the formula I.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新材料：由糠醛I（A为低级烷基，低级烯基，低级炔基，B 1为H，成盐原子，成盐基团，生理学上可水解的酯基）所示的氰基烷酰胺氧基乙酰孢子衍生物。实施例：7beta-（2-氰基正丁酰）氨基-7α-甲氧基-3-（1-甲基-5-叔唑基）硫甲基-1-脱硫-1-氧杂-3-头孢烯-4-羧酸乙酰氧基甲基酯（式II。用途：口服或注射用抗微生物剂，有效预防和治疗尿道感染性疾病，感染性感染性疾病，骨髓炎等。方法：对相应的化合物进行手术，引入B 1基团，在侧链中引入酰基，引入氰基等，得到式I所示的化合物。

20. 发明专利

AT466573T 未知
公开(公告)号：AT466573T
公开(公告)日：2010-05-15
申请号：AT08014713
申请日：2000-11-21
申请人： SHIONOGI & CO
发明人： KAWANISHI YASUYUKI , TAKENAKA HIDEYUKI , HANASAKI KOHJI , OKADA TETSUO
IPC分类号： A61K31/18 , A61K20060101 , A61K31/00 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/37 , A61K31/381 , A61K31/4015 , A61K31/402 , A61K31/4035 , A61K31/41 , A61K31/415 , 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 , A61K31/535 , A61K31/5375 , A61K31/63 , A61K31/635 , A61P20060101 , A61P3/04 , A61P43/00 , C07C20060101 , C07C311/06 , C07C311/07 , C07C311/08 , C07C311/14 , C07C311/20 , C07C311/21 , C07C311/46 , C07C323/40 , C07D20060101 , C07D207/09 , C07D207/12 , C07D207/16 , C07D209/08 , C07D209/48 , C07D209/88 , C07D211/08 , C07D211/58 , C07D211/62 , C07D213/75 , C07D213/82 , C07D215/36 , C07D215/38 , C07D217/04 , C07D219/10 , C07D231/12 , C07D231/16 , C07D231/56 , C07D233/68 , C07D239/42 , C07D241/02 , C07D261/08 , C07D265/30 , C07D277/46 , C07D277/56 , C07D277/70 , C07D285/06 , C07D295/135 , C07D307/02 , C07D307/68 , C07D307/91 , C07D311/16 , C07D317/66 , C07D333/38 , C07D333/72 , C07D521/00
摘要： Neuropeptide Y5 receptor antagonist comprises new or known aminosulfinyl or aminosulfonyl derivatives (I). Neuropeptide Y5 receptor antagonist comprises aminosulfinyl or aminosulfonyl derivatives of formula (I), their prodrugs, salts or solvates. [Image] R 1optionally substituted lower alkyl, cycloalkyl or aryl, or R 1 + R 2lower alkylene; n : 1 or 2; X : (CR 3R 4) pA(CR 5R 6) q, HetU, NR 2X or optionally substituted lower alkylene, lower alkenylene, CO-lower alkylene or CO-lower alkenylene; A : optionally substituted cycloalkylene, cycloalkenylene, bicycloalkylene, arylene or divalent heterocycle; p, q : 0 or 1; Het : piperidinediyl, piperazinediyl, pyridinediyl, pyrazinediyl, pyrrolidinediyl or pyrrolediyl all attached to NR 2 via N; U : a bond, lower alkylene or lower alkenylene; Y : OCONR 7, CONR 7, CSNR 7, NR 7CO or NR 7CS; R 2-R 7H or lower alkyl; Z : optionally substituted lower alkyl, lower alkenyl, amino, lower alkoxy, carbocyclyl or heterocyclyl. Independent claims are also included for compounds (I), their salts, prodrugs and solvates in which: (i) X = 2-6C alkylene or 3-6C alkenylene; and R 1 = optionally substituted 3-10C alkyl or 5 or 6C cycloalkyl; provided that when Y = NR 7, the Z is not lower alkylphenylamino, lower hydroxyalkylphenylamino or acylphenylamino; (ii) A = heteroarylene or optionally substituted cycloalkylene, cycloalkenylene, bicycloalkylene or piperidinylene; and R 1 = optionally substituted 3-10C alkyl or 5 or 6C cycloalkyl; and (iii) A = p-phenylene; R 1 = 3-10C alkyl or 5 or 6C cycloalkyl and Z = p-lower alkylphenylene; provided that when R 1 = isopropyl, the Z is not p-n-butylphenylene. ACTIVITY : Anorectic; antidiabetic; hypotensive; antilipemic; antiarteriosclerotic; cardiant. MECHANISM OF ACTION : Neuropeptide-Y5 antagonist. In assays, a compound of formula (Ia) exhibited IC 50 values for neuropeptide Y5 binding of 0.1 nM and for cAMP in Chinese hamster ovary cells of 1.9 nM. [Image].

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