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171. 发明专利

JPH02264748A PRODUCTION OF 2-AMINOBENZYL ALCOHOL DERIVATIVE 失效
公开(公告)号：JPH02264748A
公开(公告)日：1990-10-29
申请号：JP8609389
申请日：1989-04-05
申请人： NIPPON CHEMIPHAR CO
发明人： MAZAKI MITSUO , YAMAKAWA TOMIO , OKAZOE TAKASHI
IPC分类号： C07D233/84 , C07C213/02 , C07C215/68 , C07C217/84 , C07D265/16
摘要： PURPOSE:To industrially and advantageously obtain the subject compound useful as an intermediate for medicines, agricultural chemicals, etc., by subjecting a 2-aminobanzyl alcohol corresponding to the objective compound and an aliphatic aldehyde to dehydrating reaction, then reducing the resultant compound or further subjecting the reduction product to N-alkylation. CONSTITUTION:A compound expressed by formula I (R is H, halogen, alkyl, alkoxy, CF3, OCF3 or NO2; n is 1, 2 or 3) and a 2-8C aliphatic aldehyde are subjected to dehydrating reaction in a suitable solvent at a temperature of 0 deg.C to the boiling point of the solvent, preferably 0-40 deg.C and the resultant reaction product is then reduced by a well-known method, such as hydrogenation in the presence of a catalyst, e.g. palladium-carbon, or reduction with a metal hydride, such as boron hydride or metal boron hydride, to provide a compound expressed by formula II (R is 1-7C alkyl), which, as desired, is further subjected to N-alkylation by a well-known method to more safely afford the objective compound expressed by formula II or formula III (R is alkyl) in high yield according to the method suitable for industrial mass production.

172. 发明专利

JPS643157A 2-AMINOBENZYL ALCOHOL DERIVATIVE 失效
公开(公告)号：JPS643157A
公开(公告)日：1989-01-06
申请号：JP15851087
申请日：1987-06-25
申请人： NIPPON CHEMIPHAR CO
发明人： MAZAKI MITSUO , NOMURA YUTAKA , YAMAKAWA TOMIO , TAKEDA HIROMITSU
IPC分类号： C07D235/28 , C07C67/00 , C07C209/16 , C07C211/52 , C07C213/00 , C07C213/02 , C07C215/68 , C07C217/84 , C07C233/54
摘要： NEW MATERIAL:The compound of formula I [R is H, alkyl, alkoxy, halogen or trifluoromethyl; R is H or alkyl). EXAMPLE:2-Isobutylaminobenzyl alcohol. USE:A synthetic intermediate for pharmaceuticals and agricultural chemicals, etc. Especially useful as an important synthetic intermediate for 2-(2-substituted- aminobenzylsulfinyl)-benzimidazole derivative having antiulcer activity and gastric and intestinal cell protection activity. PREPARATION:The compound of formula I can be produced by reducing a compound of formula II (R is H, alkyl or aralkyl) with aluminum lithium hydride, etc., at -5 deg.C - refluxing temperature and subjecting the resultant compound of formula III to N-alkylation reaction with an alkyl halide, etc.

173. 发明专利

JPS63303959A PRODUCTION OF 5-HYDROXYANTHRANILIC ACID ESTER 失效
公开(公告)号：JPS63303959A
公开(公告)日：1988-12-12
申请号：JP14089387
申请日：1987-06-05
申请人： NIPPON CHEMIPHAR CO
发明人： MAZAKI MITSUO , NOMURA YUTAKA , YAMAKAWA TOMIO , TAKEDA HIROMITSU
IPC分类号： C07C229/64 , C07C227/18
摘要： PURPOSE:To obtain a compound useful as an intermediate for medicines and agricultural chemicals in good yield by simple operation, by reacting a 5- hydroxyanthranilic acid with thionyl chloride and an alcohol. CONSTITUTION:5-Hydroxyanthranilic acid is reacted with thionyl chloride and an alcohol expressed by the formula ROH (R is lower alkyl or benzyl) in a solvent, such as ether or chloroform, at ambient temperature or by refluxing and heating to afford the aimed substance. The compound expressed by the formula is an important synthetic intermediate for 2-(2-substituted amino-5- alkoxybenzylsulfinyl)benzimidazole derivatives having especially antiulcer and gastrointestinal cytophylactic action.

174. 发明专利

JPS6345266A PRODUCTION OF IMIDAZOLE DERIVATIVE 失效
公开(公告)号：JPS6345266A
公开(公告)日：1988-02-26
申请号：JP18979786
申请日：1986-08-13
申请人： NIPPON CHEMIPHAR CO
发明人： YAMAKAWA TOMIO , TAKEDA HIROMITSU , MAZAKI MITSUO
IPC分类号： C07D233/64
摘要： PURPOSE:To produce cimetidine useful as a preventive and remedy for ulcer with simple process, by reacting an aminomethylimidazole compound or its acid addition salt with a mercaptoethylguanidine compound. CONSTITUTION:An imidazole compound of formula III (e.g. cimetidine) can be produced by reacting an aminomethylimidazole compound of formula I (R1 and R2 are lower alkyl, lower alkenyl or aralkyl; R1 and R2 may together with adjacent N form a ring) (e.g. 4-piperidinomethyl-5-methylimidazole) or its acid addition salt with a mercaptoethylguanidine compound of formula II [e.g. N-cyano-N'-methyl-N''-(2-mercaptoethyl)guanidine] in an organic solvent preferably at refluxing temperature.

175. 发明专利

JPS62198669A STABLE MICROCRYSTAL AND PRODUCTION THEREOF 失效
公开(公告)号：JPS62198669A
公开(公告)日：1987-09-02
申请号：JP3828686
申请日：1986-02-25
申请人： NIPPON CHEMIPHAR CO
发明人： MAZAKI MITSUO , MORIGA TERUMASA , YAMAKAWA TOMIO , TAKEDA HIROMITSU , YOSHIOKA MITSUKO
IPC分类号： A61K31/415 , A61K31/4184 , C07D235/28
摘要： PURPOSE:Thermostable-form microcrystals, consisting of microcrystals of 2-(2- dimethylaminobenzylsulfinyl)benzimidazole having a specific average particle diameter and decomposition point, having good stability and preservable as a medicine for a long period. CONSTITUTION:Microcrystals which are microcrystals of 2-(2- dimethylaminobenzylsulfinyl)benzimiazole, expressed by the formula and having

176. 发明专利

JPS62192366A SUBSTITUTED AMINOBENZYLSULFONYLBENZIMIDAZOLE COMPOUND 失效
公开(公告)号：JPS62192366A
公开(公告)日：1987-08-22
申请号：JP3405886
申请日：1986-02-18
申请人： NIPPON CHEMIPHAR CO
发明人： OKABE SUSUMU , SATO MASARU , YAMAKAWA TOMIO , NOMURA YUTAKA , HAYASHI MASATOSHI
IPC分类号： C07D235/28 , A61K31/415 , A61K31/4184 , A61P1/04
摘要： NEW MATERIAL:A substituted aminobenzylsulfonylbenzimidazole compound of formula I (R is H, alkyl, cycloalkyl, phenyl or aralkyl; R is H, alkyl or R and R together with adjacent N form a ring; R and R are H, halogen, CF3, alkyl, alkoxy, alkoxycarbonyl or amino). EXAMPLE:2-(2-Dimethylaminobenzylsulfonyl)benzimidazole. USE:An antiulcer agent having excellent effect to suppress gastric acid secretion and exhibiting high stability in acidic solution. It has desirable characteristics as an agent for oral administration. PREPARATION:The objective compound of formula I can be produced e.g. by reacting the 2-mercaptobenzimidazole compound of formula IV with the 2-aminobenzyl compound of formula V to obtain the compound of formula III, oxidizing the compound to the compound of formula II and further oxidizing the product.

177. 发明专利

JPS62167726A PHARMACEUTICAL COMPOSITION CONTAINING BENZIMIDAZOLE DERIVATIVE 失效
公开(公告)号：JPS62167726A
公开(公告)日：1987-07-24
申请号：JP758786
申请日：1986-01-17
申请人： NIPPON CHEMIPHAR CO
发明人： OKABE SUSUMU , YAMAKAWA TOMIO , NOMURA YUTAKA , HAYASHI MASATOSHI , MATSUKURA HITOSHI
IPC分类号： C07D235/28 , A61K31/415 , A61K31/4184 , A61P1/04
摘要： PURPOSE:To obtain an antiulcer agent containing a specific benzimidazole derivative as an active component and having excellent activity to suppress gastric acid secretion and extremely high safety. CONSTITUTION:The benzimidazole derivative of formula I (R1 is H, lower alkyl, phenyl, etc.; R2 is H or lower alkyl; R1 and R2 may together with adjacent N from a ring; R3 and R4 are H, halogen, lower alkyl, etc.) is used as an antiulcer agent. The compound of formula I is a synthetic intermediate for the compound of formula I' which is known as an antiulcer agent, however, it has been found that the compound has excellent action to suppress secretion of gastric acid and is excellent as an antiulcer agent. Dose: preferably about 10-500mg daily by oral administration. The compound of formula I can be produced by reacting a 2-mercaptobenzimidazole compound of formula II with a 2-aminobenzyl compound of formula III.

178. 发明专利

JPS62161769A NOVEL SULFOXIDE COMPOUND AND PRODUCTION THEREOF 失效
公开(公告)号：JPS62161769A
公开(公告)日：1987-07-17
申请号：JP301786
申请日：1986-01-10
申请人： NIPPON CHEMIPHAR CO
发明人： OKABE SUSUMU , SATO MASARU , YAMAKAWA TOMIO , NOMURA YUTAKA , HAYASHI MASATOSHI
IPC分类号： C07D401/12 , A61K31/495 , A61P1/04 , C07D213/00 , C07D241/00 , C07D241/44 , C07D471/04
摘要： NEW MATERIAL:A sulfoxide compound of formula I [R1-R3 are H or lower alkyl; X is CH or N; Z is (substituted) 2-pyridyl or (substituted) 2-aminophenyl of formula II (R4 and R5 are H or lower alkyl)]. EXAMPLE:2-(2-Pyridylmethylsulfinyl) quinoxaline. USE:An anticulcer agent exhibiting excellent activity to suppress the secretion of gastric juice by its specific H +K ATPase-inhibiting activity. PREPARATION:The compound of formula I can be produced by reacting a mercapto-derivative of formula III with the compound of formula IV (Q is reactive group) or its salt and oxidizing the resultant compound of formula V.

179. 发明专利

JP2013067652A Activating agent for peroxisome proliferator activated receptor delta 有权
标题翻译：过氧化物促进剂激活受体三角体激活剂
公开(公告)号：JP2013067652A
公开(公告)日：2013-04-18
申请号：JP2012279230
申请日：2012-12-21
申请人： Nippon Chemiphar Co Ltd , 日本ケミファ株式会社
发明人： SAKUMA SHOGO , MOCHIZUKI NOBUTAKA , USHIODA KATSUTOSHI , TAKAHASHI RIE , YAMAKAWA TOMIO , MASUI SEIICHIRO
IPC分类号： C07D263/32 , A61K31/381 , A61K31/421 , A61K31/426 , A61P3/06 , A61P3/10 , A61P43/00 , C07D277/24 , C07D333/22
CPC分类号： C07D277/22 , C07D263/32 , C07D277/20 , C07D277/30 , C07D333/22
摘要： PROBLEM TO BE SOLVED: To provide an activating agent for PPARδ (peroxisome proliferator activated receptor δ).SOLUTION: The activating agent comprises a compound expressed by formula (II) or its salt. In the formula, Grepresents O, CH2 or the like; Arepresents thiazole, oxazole, or thiophene, which can have a substituent selected from alkyl, alkoxy, halogen, alkyl substituted with halogen, or the like; Brepresents a 1-8C alkylene chain, and when the alkylene chain includes two or more carbon atoms, the chain may have a double bond; and Rand Rindependently represent hydrogen, alkyl, alkoxy, halogen, or alkyl substituted with halogen.
摘要翻译：要解决的问题：提供PPARδ（过氧化物酶体增殖物激活受体δ）的活化剂。活化剂包含由式（II）表示的化合物或其盐。在该公式中，G a 表示O，CH2等; A a 表示可以具有选自烷基，烷氧基，卤素，被卤素取代的烷基等的取代基的噻唑，恶唑或噻吩等。 B a 表示1-8C亚烷基链，当亚烷基链包含两个或更多个碳原子时，链可以具有双键; 并且R 1a 和R 2a独立地表示氢，烷基，烷氧基，卤素或被卤素取代的烷基。版权所有（C）2013，JPO＆INPIT

180. 发明专利

JP2008088057A N-substituted-n-(4-piperidinyl)amide derivative 审中-公开
标题翻译： N-取代-N-（4-哌啶子基）酰胺衍生物
公开(公告)号：JP2008088057A
公开(公告)日：2008-04-17
申请号：JP2005083653
申请日：2005-03-23
申请人： Nippon Chemiphar Co Ltd , 日本ケミファ株式会社
发明人： TAKAHASHI TOSHIHIRO , ENDO TAKESHI , SHIODA KATSUTOSHI , SAKUMA SHOGO , YAMAKAWA TOMIO , YOTSUYA KIICHI , KAWASAKI TORU , IMAI TOSHIYASU , HIRATE KENJI
IPC分类号： C07D211/58 , A61K31/445 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61P29/02 , A61P43/00 , C07D401/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/14
CPC分类号： C07D211/66 , C07D211/58
摘要： PROBLEM TO BE SOLVED: To provide an N-substituted-N-(4-piperidinyl)amide derivative or a salt thereof that exhibits analgesic actions. SOLUTION: A compound represented by general formula (I) or a salt thereof is used as an analgesic agent. In the formula, R 1 is a 1-6C alkyl group or an optionally substituted 5- or 6-membered heterocyclic group or the like; R 2 is a 1-6C acylamino group, a 2-6C alkyl(thiocarbonyl)amino group, a ureido group, a thioureido group or the like and the substitution position of R 2 is the ortho- or meta-position; R 3 is a hydrogen atom, a 2-8C alkoxycarbonyl group or the like; R 4 is an optionally substituted phenyl or 5- or 6-membered heterocyclic group; R 5 is a hydrogen atom or the like; R 6 is a hydrogen atom or the like; R 7 is a hydrogen atom or a methyl group; and m is 1 or 2. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：提供显示镇痛作用的N-取代-N-（4-哌啶基）酰胺衍生物或其盐。解决方案：将通式（I）表示的化合物或其盐用作止痛剂。在该式中，R 1 SP 1是1-6C烷基或任选取代的5或6元杂环基等; R 2 SP 2是1-6C的酰基氨基，2-6C的烷基（硫代羰基）氨基，脲基，硫脲基等，R 2的取代位置< SP>是邻位或间位; R 3是氢原子，2-8C烷氧基羰基等; R 4是任选取代的苯基或5或6元杂环基; R 5是氢原子等; R 6是氢原子等; R 7是氢原子或甲基; m为1或2.版权所有（C）2008，JPO＆INPIT

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