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1. 发明公开

EP1069123A4 PROCESS FOR PRODUCING BENZOTHIOPHENECARBOXYLIC ACID AMIDE DERIVATIVES 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG VON BENZOTHIEPHBAARBONSAUREAMID-DERIVATEN
公开(公告)号：EP1069123A4
公开(公告)日：2003-03-05
申请号：EP99910765
申请日：1999-03-30
申请人： SHIONOGI & CO
发明人： HONMA TSUNETOSHI , HIRAMATSU YOSHIHARU , OKADA TETSUO , KAKINUMA MAKOTO
IPC分类号： C07D333/64 , C07B61/00 , C07C213/00 , C07C213/02 , C07C215/42 , C07D333/68
CPC分类号： C07D333/68 , C07C213/02 , C07C2602/42 , C07C215/42
摘要： A process for producing compounds having PGD2 antagonism represented by formula (I), pharmaceutically acceptable salts thereof or hydrates of the same characterized by reacting an amino alcohol of formula (II) or its salt with a compound of formula (III) or its reactive derivative, oxidizing the obtained product in the presence of 2,2,6,6,-tetramethylpiperidine-1-oxyls, and then reacting with an ylide under Wittig reaction conditions optionally followed by deblocking.
摘要翻译：一种制备由式（I）表示的具有PGD 2拮抗作用的化合物或其药学上可接受的盐或水合物的方法，该方法包括使式（II）的氨基醇或其盐与式（III）的化合物反应）或其反应性衍生物，在2,6,6,6'-四甲基哌啶-1-氧基存在下用卤代含氧酸氧化产物，在Wittig反应条件下使产物与内鎓盐反应，并任选地将产品。

2. 发明公开

EP1249233A4 NPYY5 ANTAGONISTS 有权
标题翻译： NPYY5拮抗剂
公开(公告)号：EP1249233A4
公开(公告)日：2005-04-13
申请号：EP00976387
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： A61K20060101 , A61K31/00 , A61K31/18 , 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 , A61P3/00 , C07D295/12
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： NPYY5 receptor antagonists which contain compounds represented bygeneral formula (I), prodrugs thereof, pharmaceutically acceptable salts thereof or solvates of the same wherein R1 represents lower alkyl, cycloalkyl, etc.; R2 represents hydrogen, lower alkyl, etc.; n is 1 or 2; X represents lower alkylene, lower alkenylene, arylene, cycloalkylene, etc.; Y represents CONR?7, CSNR7, NR7CO, NR7¿CS, etc. (wherein R7 represents hydrogen or lower alkyl); and Z represents lower alkyl, an optionally substituted hydrocarbon cycle, an optionally substituted heterocycle, etc.

3. 发明专利

JP2002241368A NEW BENZOLACTAM DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 失效
公开(公告)号：JP2002241368A
公开(公告)日：2002-08-28
申请号：JP3357397
申请日：1997-02-18
申请人： SHIONOGI & CO
发明人： HAGISHITA YAMAJI , OKADA TETSUO , FUJIMOTO MASABUMI
IPC分类号： A61K31/55 , A61K31/554 , A61P3/04 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P43/00 , C07D223/16 , C07D225/06 , C07D267/14 , C07D267/22 , C07D281/10 , C07D281/18 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D413/12 , C07D417/12
摘要： PROBLEM TO BE SOLVED: To provide an excellent neuropeptide Y(NPY) antagonist, i.e., an antifeeding agent, a therapeutic agent for myocardial infarction, a therapeutic agent for angina pectoris and an antihypertensive agent. SOLUTION: A compound represented by the formula (I) (R1 and R2 are each H, a halogen or the like; R3 is a lower alkyl which may have a substituent, an aryl lower alkyl which may have a substituent or the like; and R4 is NHCOR5, NHCONR9R10 or the like), a pharmaceutically acceptable salt thereof or a hydrate thereof and a pharmaceutical composition containing the compound are provided. A method for suppressing feeding and a method for treating the myocardial infarction, angina pectoris and hypertension that are characterized by administering the compound are provided. A use of the compound for producing the pharmaceutical preparation for suppressing the feeding and treating the myocardial infarction, angina pectoris and hypertension is provided.

4. 发明专利

JPH04178366A PRODUCTION OF 3-AMINO-4-METHYLENE PYRROLIDINE DERIVATIVE 失效
公开(公告)号：JPH04178366A
公开(公告)日：1992-06-25
申请号：JP30809390
申请日：1990-11-13
申请人： SHIONOGI & CO
发明人： TSUSHIMA TADAHIKO , OKADA TETSUO , NISHITANI YASUHIRO
IPC分类号： C07D207/22
摘要： PURPOSE:To industrially and advantageously produce the title compound by using an 3-amino-4-oxopyrrolidine derivative as a starting raw material and subjecting the above-mentioned derivative to methylene formation without using harmful and specific reagent and simply and safely introducing a methylene side chain at the 4-position thereof. CONSTITUTION:An 3-amino-4-oxopyrrolidine derivative [e.g. 1-tert. butoxycarbonyl-N-methyl) amino-4-oxopyrrolidine] expressed by formula I (R and R are amino-protecting groups; R is H or lower alkyl) is subjected to methylene formation to provide 3-amino-4-methylenepyrrolidine derivative [1-tert. butoxycarbonyl-3-(N-methoxycarbonyl-N-methyl) amino-4-methylenepyrrolidine]. A compound expressed by the formula (C6H5)P=CH2 is used as an exomethylene-forming reagent of the ketone body expressed by formula I. The compound expressed by formula I is useful as a pyrrolidine derivative capable of forming 7 position of pyridonecarboxylic acid which is an antimicrobial agent.

5. 发明专利

JPS62135479A ALKYLCARBAMOYLOXYCEPHEM COMPOUND 失效
公开(公告)号：JPS62135479A
公开(公告)日：1987-06-18
申请号：JP18439786
申请日：1986-08-05
申请人： SHIONOGI & CO
发明人： HAMASHIMA YOSHIO , TSUJI SHOJI , OKADA TETSUO , MINAMI KYOJI , ISHITOBI HIROYUKI , ISHIKURA KOJI
IPC分类号： A01N43/90 , A23K20/195 , A23L3/34 , A61K20060101 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/06 , C07D501/20 , C07D501/34 , C07D501/46
摘要： NEW MATERIAL:The 3-(alkylcarbamoyloxymethyl)-3-cephem-4-carboxylic acid of formula I (R is H or amino-protecting group; R and R are alkyl; R is H, salt-forming group or ester-forming group; X is S or sulfinyl) and its derivative. EXAMPLE:7beta-[2-(2-tert-Butoxycarbonylamino-4-thiazolyl)-2-pentenoyla mino]-3-me thylcarbamoyloxymethyl-3-cephem-4-carboxylic acid diphenylmethyl ester. USE:It exhibits strong antibacterial activity against aerobic Gram-positive bacteria and is useful as a bactericidal agent, bacteriostatic agent, disinfectant, antiseptic, etc. It is useful also as a preventive and remedy for infectious diseases of man and animal. PREPARATION:The compound of formula I can be produced e.g. by reacting the corresponding 7beta-amino compound of formula II with the carboxylic acid of formula III or its reactive derivative under acylation reaction condition.

6. 发明专利

JPS59118789A Oxacephem derivative, its preparation and use 失效
标题翻译： OXACEPHEM衍生物，其制备和使用
公开(公告)号：JPS59118789A
公开(公告)日：1984-07-09
申请号：JP22935882
申请日：1982-12-27
申请人： Shionogi & Co Ltd
发明人： NARISADA MASAYUKI , WATANABE FUMIHIKO , OKADA TETSUO , MATSUMURA HIROSHI
IPC分类号： A61K31/535 , A61P31/04 , C07D505/00
CPC分类号： C07D505/00 , Y02P20/55
摘要： NEW MATERIAL:A compound shown by the formula I (Ar is phenyl, hydroxyphenyl, or thienyl; R is H, light metal atom, or carboxyl-protecting group).
EXAMPLE: 7β[ 2-( 2-Thienyl )-2-ureidoacetamido ]- 7α- methyoxy-3-( 1-carbamoylmethyl-5-1H-tetrazolyl )thiomethyl-1-dethia-1-oxa-3 -cephem-4-carboxylic acid diphenylmethyl ester.
USE: An antibacterial agent against Gram-positive bacteria (hemolytic streptococcus), Gram-negative bacteria (Escherichia coil, etc.), and an antiseptic.
PROCESS: A compound shown by the formula III is reacted with a substituted tetrazol-5-mercaptide shown by the formula IV, light metal or its reactive drivative.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：由式I表示的化合物（Ar是苯基，羟基苯基或噻吩基; R是H，轻金属原子或羧基保护基）。实施例：7beta [2-（2-噻吩基）-2-脲基乙酰胺基]-7α-甲氧基-3-（1-氨基甲酰基甲基-5- [四唑基]硫甲基-1-脱硫-1-氧杂-3-头孢-4-基）羧酸二苯甲酯。用途：抗革兰氏阳性菌（溶血性链球菌），革兰阴性菌（大肠杆菌等）和防腐剂的抗菌剂。方法：将式III化合物与式IV所示的取代的四唑-5-硫醇盐，轻金属或其反应性活性剂反应。

7. 发明专利

JP2002193898A METHOD FOR PRODUCING INTERMEDIATE IN SYNTHESIS OF BENZOTHIOPHENECARBOXYLIC ACID AMIDE DERIVATIVE 审中-公开
公开(公告)号：JP2002193898A
公开(公告)日：2002-07-10
申请号：JP2001353060
申请日：2001-11-19
申请人： SHIONOGI & CO
发明人： HONMA TSUNETOSHI , HIRAMATSU YOSHIHARU , OKADA TETSUO , KAKINUMA MAKOTO
IPC分类号： C07D333/64 , C07B61/00 , C07C213/00 , C07C213/02 , C07C215/42 , C07D333/68
摘要： PROBLEM TO BE SOLVED: To provide a method for producing an intermediate in a synthesis for a benzothiophenecarboxylic acid amide useful as a prostaglandin D2 (herein after PGD2) antagonist. SOLUTION: This method for producing an amino alcohol represented by formula (II) or its salt is characterized in that a compound represented by the following formula (II-2) (R2 is an alkyl; R3 is hydrogen or an alkyl) is reduced in a reducing agent-Lewis acid system.

8. 发明专利

JPH0532680A OPTICAL RESOLUTION OF OPTICALLY ACTIVE GLUTARIC ACID ESTER DERIVATIVE 失效
公开(公告)号：JPH0532680A
公开(公告)日：1993-02-09
申请号：JP21453491
申请日：1991-07-30
申请人： SHIONOGI & CO
发明人： HIRAI KENTARO , OKADA TETSUO
IPC分类号： C07C69/675 , C07B57/00 , C07F7/18
摘要： PURPOSE:To perform optical resolution of a specific racemic mixed solution in high yield and optical purity by reacting the racemic mixed solution with (+)-dehydroabietylamine, thereby forming (+)-dehydroabietylamine salt of R(-)- glutaric acid ester. CONSTITUTION:A racemic mixed solution of a glutaric acid of formula [R is hydroxyl-protecting group; R is (substituted) lower alkyl; * represents asymmetric carbon atom] is treated with (+)-dehydroabietylamine to form (+)- dehydroabietylamine salt of R(+)-glutaric acid ester and effect the optical resolution of optically active glutaric acid ester derivative. The produced salt is subjected to salt-decomposition to recover R(-)-glutaric acid ester and S(+)- glutaric acid ester.

9. 发明专利

JPH0129796B2 失效
公开(公告)号：JPH0129796B2
公开(公告)日：1989-06-14
申请号：JP10177980
申请日：1980-07-23
申请人： SHIONOGI & CO
发明人： NARISADA MASAYUKI , OKADA TETSUO , YOSHIDA TADASHI , MATSURA SHINZO
IPC分类号： A61K31/535 , A61P31/04 , C07D505/00

10. 发明专利

JPS6442490A SUBSTITUTED OXYCARBONYLAMINOCEPHEM COMPOUND 失效
公开(公告)号：JPS6442490A
公开(公告)日：1989-02-14
申请号：JP20051387
申请日：1987-08-10
申请人： SHIONOGI & CO
发明人： TSUJI SHOJI , OKADA TETSUO
IPC分类号： C07D501/18 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/04
摘要： NEW MATERIAL:A compound expressed by the formula (R represents alkyl, aralkyl or aryl; R represents H or carbamoyl which may be protected; R represents H or ester). EXAMPLE:7-t-butoxycarbonylaminocepholosporanic acid. USE:An intermediate for synthesis of cephalosporin compounds useful as an antibacterial agent, etc. PREPARATION:(A) The corresponding 7-substituted-oxycarbonylaminocepha losporanic acid is hydrolyzed with alkanol-water-alkali metal hydroxide and (B) thus obtained corresponding 7-substituted-oxycarbonyl-amino-3- hydroxymethylcephem-4-carboxylic acid is carbamoylated. (C) The corresponding 7-substituted-oxycarbonylamino-3-carbamoyloxymethylcephem-4-carboxyic acid is then esterified to afford the aimed cephem compound.

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