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1. 发明专利

JPH069631A NEW PRODUCTION OF PYRAZOLOPYRIDINE 失效
公开(公告)号：JPH069631A
公开(公告)日：1994-01-18
申请号：JP12092893
申请日：1993-04-23
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： NAKAMURA HITOSHI , KAWAKAMI RYOICHI , YAMAZAKI HIROSHI , HASHIMOTO NORIO , TAKI ISAO
IPC分类号： C07D471/04
摘要： PURPOSE:To obtain a new method for producing a pyrazolopyridine compound useful as an intermediate for producing pyrazolopyridine derivatives useful as medicines. CONSTITUTION:A compound of formula III (R is lower alkyl; R is H or proper substituent group), e.g. 1-phenyl-1-butyn-3-one is made to react with a compound of formula II (R is H or proper substituent group; X is anion), e.g. N- aminopyridine iodide in a polar solvent such as N,N-dimethylformamide or dimethyl sulfoxide at ambient temperature to 50 deg.C to provide the objective compound of formula I, e.g. 3-acetyl-2-phenylpyrazolo[1,5-a]pyridine.

2. 发明专利

JPH08176154A PRODUCTION OF IMIDAZOLE DERIVATIVE 失效
公开(公告)号：JPH08176154A
公开(公告)日：1996-07-09
申请号：JP33780994
申请日：1994-12-26
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： KAWAKAMI RYOICHI , ICHIHARA MASAHARU , KODERA TETSUO , MORINAGA YASUHIRO , NISHIWAKI MASANORI
IPC分类号： C07D471/04 , A61K31/435 , A61P43/00
摘要： PURPOSE: To safely produce an imidazole derivative having a pharmacological action such as angiotensin II antagonistic action on an industrial scale at a low cost by subjecting a specific compound to a reaction to introduce a lower alkyl group. CONSTITUTION: A compound of formula I (R to R are each a lower alkyl; R is H or an imino-protecting group) is subjected to a lower-alkyl introduction reaction to obtain the objective compound of formula II (R is a lower alkyl), e.g. 5,7-dimethyl-2-hydroxy-3-[4-[1-ethyl-5-methyl-3-(1H-tetrazol-5-yl)-2- pyrrolyl]benzyl]-3H-imidazo[4,5-b]pyridine. The reaction is carried out e.g. in the presence of a lower alkyl iodide (e.g. methyl iodide) and a base such as alkali metal hydroxide (e.g. NaOH) in a solvent such as dioxane.

3. 发明专利

JPH08333339A PRODUCTION OF OPTICALLY ACTIVE PIPERIDINEACETIC ACID DERIVATIVE 失效
公开(公告)号：JPH08333339A
公开(公告)日：1996-12-17
申请号：JP14144495
申请日：1995-06-08
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： ICHIHARA MASAHARU , YAMAZAKI HIROSHI , FUKAGAWA MASAYASU , KAWAKAMI RYOICHI
IPC分类号： C07D211/34 , C07B57/00
摘要： PURPOSE: To obtain a compound useful as an intermediate for producing a compound which is an excellent adenosine antagonist, useful in the field of medicine industry and having extremely high optical purity in good yield. CONSTITUTION: This optically active piperidineacetic acid derivative, e. g. (R)-2-(2-piperidyl)acetic acid benzyl ester.L-tartaric acid salt can be produced by leading a racemic modification of a piperidineacetic acid derivative such as 2-(2-piperidyl)acetic acid expressed by the formula (R is a protected carboxy group such as benzyloxycarbonyl group) to a diastereomer using an optically active acid such as L-tartaric acid, D-mandelic acid or D-10-camphorsulfonic acid, carrying out fractional crystallization of the diastereomer and as necessary further, decomposing the separated crystal to the resolving reagent and the original compound.

4. 发明专利

JPH08169890A NEW CRYSTAL OF CEPHALOSPORIN COMPOUND 失效
公开(公告)号：JPH08169890A
公开(公告)日：1996-07-02
申请号：JP20620195
申请日：1995-08-11
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： KAWABATA KOJI , TERASAWA TAKESHI , OKI AYAKO , SHIRAI FUMIYUKI , YAMAMOTO HIROBUMI , KAWAKAMI RYOICHI , HAMAGUCHI CHIAKI
IPC分类号： C07D501/04 , A61K31/545 , A61K31/546 , A61P31/04 , C07B63/00 , C07D501/00 , C07D501/59
摘要： PURPOSE: To obtain a crystal of a cephalosporin compound, capable of manifesting extremely strong antimicrobial activities, stable to heat or light and manifesting physically, chemically and pharmaceutically excellent properties and its salt. CONSTITUTION: This crystal of 7β-[2-(2-aminothiazol-4-yl)-2-(Z)(hydroxyimino) acetamido]-3-[(pyrazo1-4-yl)-methylthio]-3-cephem-4-carboxylic acid which is an antibiotic substance represented by the formula or its salt is stabler than an amorphous form and includes all the crystal forms such as a solvate with water and an organic solvent (preferably lower alcohols) or a clathrate type. The crystal is obtained by cooling a solution containing the compound represented by the formula or its salt and depositing the crystal under acidic conditions at ambient temperature or under heating. The compound is useful for a peroral cephalosporin due to strong antimicrobial activities arid a high urination ratio in an animal.

5. 发明专利

JP2000080072A PRODUCTION OF L-ARGININE 失效
公开(公告)号：JP2000080072A
公开(公告)日：2000-03-21
申请号：JP18860599
申请日：1999-07-02
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： MUKAI KOJI , MUKUDA TAKASHI , KAWAKAMI RYOICHI
IPC分类号： C07C277/08 , C07C279/14
摘要： PROBLEM TO BE SOLVED: To obtain L-arginine having a small crystal particle size distribution width in good particle size distribution repeatability and suitable for powder filling treatments by adding a specific amount of L-arginine crystals as seed crystals to a supersaturated solution of the L-arginine, when the L-arginine is crystallized. SOLUTION: This method for producing arginine crystals comprises crystallizing L-arginine. Therein, L-arginine crystals are added as seed crystals to the supersaturated solution of the L-arginine. The L-arginine crystals use for the seed crystals are preferably particulate L-arginine which has an average particle diameter of 100-300 μm and to which many fine L-arginine crystals (preferably fine L-arginine crystals having a particle diameter of 0.5-2 μm in an amount of 1×109 to 1×1011 crystals/g of the seed crystals) are preferably adhered as secondary nuclei used as the crystallization of the L-arginine. The L-arginine crystals used as the seed crystals may be fine L-arginine crystals obtained by grinding L-arginine crystals by the use of a grinder, etc., and having a particle diameter of 0.5-2 μm.

6. 发明专利

JPH054987A PRODUCTION OF PYRAZOLOPYRIDINE DERIVATIVE 失效
公开(公告)号：JPH054987A
公开(公告)日：1993-01-14
申请号：JP22083391
申请日：1991-09-02
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： NAKAMURA HITOSHI , KAWAKAMI RYOICHI , YAMAZAKI HIROSHI
IPC分类号： A61K31/435 , A61K31/437 , A61P7/10 , A61P9/12 , C07D471/04
摘要： PURPOSE:To obtain the subject compound useful as a synthetic intermediate for diuretic and hypotensive agent in high purity and efficiency in one step without necessitating particular refining process by reacting a specific compound containing triple bond with a specific aminopyridine compound in the presence of a base. CONSTITUTION:The objective compound of formula III [R is (protected) carboxyl] is produced by reacting a compound of formula I [R is (substituted) aryl; R is protected carboxyl; A is lower alkenylene] with an N-aminopyridine compound of formula II (R is H, halogen, lower alkyl or lower alkoxy; X is anion) in an organic solvent (e.g. DMF) in the presence of a base (e.g. potassium hydroxide) and, as necessary, deprotecting the protected carboxyl group.

7. 发明专利

JP2001033410A DIFFERENTIAL THERMAL ANYLYZER 失效
公开(公告)号：JP2001033410A
公开(公告)日：2001-02-09
申请号：JP20249799
申请日：1999-07-16
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： KAWAKAMI RYOICHI , KAWAI NOBUTAKA , TAKEUCHI HIROKI , KINOSHITA NOBORU
IPC分类号： G01N25/20
摘要： PROBLEM TO BE SOLVED: To observe the generation of gas, foaming, decomposition or the like a sample by forming both side walls of a sample cylinder and an outer cylinder from a light transmittable material permitting the internal observation of the sample cylinder from the outside of the outer cylinder. SOLUTION: A reference substance cell 2 and a sample cell 3 are housed in a sample cylinder 4 made of quartz glass and the sample cylinder 4 is surrounded by an outer cylinder 5 made of borosilicate glass. An apparatus main body 6 holds the sample cylinder 4 in the outer cylinder 5 coaxially at a predetermined position and a heater 7 is provided to the sample cylinder 4. An analyzing part 8 measures the temp. difference between a reference substance and a sample by a thermocouple 9 and a cold contact point is compensated by a DTA unit 10 to be amplified and the thermal characteristics of the sample are analyzed by a data processor 11 and the temp. (difference) of the sample is displayed on a temp. display device 12. Since the sample cylinder 4 and the outer cylinder 5 are composed of a light transmittable material as mentioned above, the state change of the sample can be observed or measured directly by an eye or through an optical mechanism.

8. 发明专利

JPH08183789A PRODUCTION OF NEW CEPHEM COMPOUND 失效
公开(公告)号：JPH08183789A
公开(公告)日：1996-07-16
申请号：JP22807895
申请日：1995-09-05
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： KAWABATA KOJI , TERASAWA TAKESHI , OKI AYAKO , SHIRAI FUMIYUKI , YAMAMOTO HIROBUMI , KAWAKAMI RYOICHI , KOGA KEIICHI
IPC分类号： C07D501/04 , A61K31/545 , A61K31/546 , A61P31/04 , C07B63/00 , C07D501/00 , C07D501/59
摘要： PURPOSE: To obtain the subject compound, a cephalosporin-based antibiotic showing strong antimicrobial activity in a short process by a method for reacting a specific pyrazole ring-containing cephem compound with a thiazole ring-containing iminoacetic acid. CONSTITUTION: This cephem compound, a cephalosporin-based antibiotic of formula IV showing strongly antimicrobial action, is obtained by a short process in a high yield by a method for reacting a 7β-amino-3-[(pyrazol-4-yl) methylthio]-3-cephem-4-carboxylic acid of formula I [R is H or an imino- protecting group; R is a (protected) carboxy] with a 2-(2-aminothiazol-4- yl)-2-(Z)-(alkoxyimino)acetic acid or reacting a cephem compound of formula III (Y is a halogen) with an N-substituted thiourea compound to form a thiazol ring.

9. 发明专利

JPS6456683A PRODUCTION OF 7-AMINO-3-(2-METHYL-1-PYRAZOLIO)METHYL-3-CEPHEM-4-CARBOXYLIC ACID OR SALTS THEREOF 失效
公开(公告)号：JPS6456683A
公开(公告)日：1989-03-03
申请号：JP12260788
申请日：1988-05-19
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： NAKAMURA HITOSHI , KAWAKAMI RYOICHI , YONISHI SATOSHI , MORIKI SHIGERU , MUKODA YASUSHI
IPC分类号： C07D501/18 , C07D501/38
摘要： NEW MATERIAL:The compound of formula I. USE:Intermediate for cephalosporin compound. PREPARATION:A compound of formula II (R is protected amino; R is protected carboxy; X is anion) [e.g. 7-(2-hydroxybenzylidene-amino)-3-(2-methyl-1-pyrazolio) methyl-3-cephem-4-carboxylic acid benzhydryl ester iodide] is subjected to the reaction to eliminate the amino- and carboxyl-protecting groups.

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