| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 81 | JPH05397B2 - | JP24728886 | 1986-10-16 | JPH05397B2 | 1993-01-05 | UIRIAMU JON KOOTESU |
| 82 | Production of azole substituted compound | JP23969889 | 1989-09-14 | JPH03101664A | 1991-04-26 | OTA SHUNSAKU |
| PURPOSE: To readily and industrially advantageously obtain the title compound useful as an intermediate for medicinal production in high selectivity and high yield by reacting a specific ether compound with an azole compound having a specific azole ring under an acidic condition. CONSTITUTION: A noncyclic ether compound expressed by formula I (R 1 and R 2 are organic residues), preferably a compound expressed by formula II (R 3 and R 5 are R 1 and R 2; R 4 is H, R 1 or R 2) is reacted with an azole compound having an azole ring in which N number is 2-4, preferably in a solvent and atmosphere such as N 2 gas in the presence of an acid catalyst such as p- toluenesulfonic acid pyridinium salt under an acidic condition and at an ambient temperature to 150°C to provide the objective compound expressed by formula III (A is monovalent group having a free electronic charge on N atom of azole ring in the above-mentioned azole compound), preferably a compound expressed by formula IV, useful as an intermediate for producing an amide compound having an azole ring used for a medicine in drug design. COPYRIGHT: (C)1991,JPO&Japio | ||||||
| 83 | JPH0259806B2 - | JP410785 | 1985-01-16 | JPH0259806B2 | 1990-12-13 | KATO SHOZO; OKAMOTO HIDENORI |
| 84 | JPS63502511A - | JP50134387 | 1987-01-23 | JPS63502511A | 1988-09-22 | |
| 85 | Benzothiadiazine compound, its production and pharmaceutical composition containing said compound | JP29458887 | 1987-11-20 | JPS63183572A | 1988-07-28 | OKU TERUO; TODO EISHIRO; KASAHARA CHIYOSHI; NAKAMURA KATSUYA; KAYAKIRI HIROSHI; HASHIMOTO SHINJI |
| NEW MATERIAL:The compound of formula I (R 1 is halogen, alkyl, alkoxy, alkylamino, alkylthio, aryloxy, carboxyl, phenyl, etc.; A is alkylene; n is 0 or 1; R 2 is H or alkyl; R 3 is H, OH, halogen, alkyl, alkylamino, acylamino, etc.; R 4 and R 5 are H or halogen) and its salt. EXAMPLE: (1R)-(+)-2-(4-chlorophenyl)-6-(1-carboxyethoxy)-4-methyl-2H-1,2,4-benzo thiadiazin-3(4H)-one 1,1-dioxide. USE: The compound has bone-resorption suppressing action and is useful as a remedy for osteopathy characterized by bone dysbolism (e.g. osteoporosis, rheumatoid arthritis, etc.). PREPARATION: The compound of formula I can be produced e.g. by reacting a compound of formula II with a compound of formula III (R 6 and R 7 are halogen, alkoxy, etc.). COPYRIGHT: (C)1988,JPO&Japio | ||||||
| 86 | JPS63500037A - | JP50357186 | 1986-06-12 | JPS63500037A | 1988-01-07 | |
| 87 | Oxadiazol-2-one derivative and herbicide containing said derivative as active ingredient | JP879486 | 1986-01-18 | JPS62167778A | 1987-07-24 | OKIMURA NOBUO; SUZUKI SEIICHI; IKEDA OSAMU; WADA MAKIKO |
| NEW MATERIAL:An oxadiazol-2-one derivative expressed by formula I (R represents alkyl or benzyl; Q represents formula II or III; X represents halogen, alkylthio or cyano; n represents 0W3; substituent groups X may be the same or different when n represents 2 or 3). EXAMPLE: 3-Methyl-5-(4-chloro-2, 3-dihydro-2, 2-dimethylbenzofuran-7-yloxy)-1,3,4- oxadiazol-2-one. USE: Useful as a selective herbicide capable of exhibiting high herbicidal activity against many weeds, e.g. fat hen, posumbu knotweed, etc., in upland field and false pimpernel, spike-flowered rotala, etc., in paddy field without affecting crops, e.g. rice plant, soybean, etc. PREPARATION: For example, as shown in the reaction formula, a carbazic acid ester expressed by formula III is reacted with phosgene to give a phosgene derivative expressed by formula IV, which is then cyclized in the presence of a base to afford the aimed compound expressed by formula I. COPYRIGHT: (C)1987,JPO&Japio | ||||||
| 88 | Pyridyl-oxy-or-thio-or pyrimidyl-oxy-or-thio-benzoic acid derivative | JP28907686 | 1986-12-05 | JPS62132862A | 1987-06-16 | KURAUSU SATSUSE; RAINAA FUITSUSHIYAA; HERUMAN HAAGEMAN; HANSU YOAHIMU ZANTERU; ROBERUTO AARU SHIYUMITSUTO; KURAUSU RIYURUSEN |
| 89 | Pyrazolesulfonylurea derivative and herbicide | JP26073585 | 1985-11-20 | JPS62120385A | 1987-06-01 | YAMAMOTO SUSUMU; TSUNODA TAKUYA; SATOU TOSHIAKI; MORIMOTO KATSUYUKI; OYA EIICHI; IGAI TAKASHI; NAWAMAKI TSUTOMU |
| NEW MATERIAL:A compound expressed by formula I [R 1 and R 2 are H or lower alkyl; Q is formula IIWIV (R 3WR 6 are H or lower alkyl); X and Y are lower alkyl or lower alkoxy; Z is N or -CH=]. EXAMPLE: N-[(4,6-Dimethoxypyrimidin-2-yl)aminocarbonyl]-1-methyl-4-(5-methyl- 1,3,4-oxadiazol-2-yl)pyrazole-5-sulfonamide. USE: A herbicide. PREPARATION: A pyrazolesulfonyl isocyanate derivative expressed by formula V is dissolved in a sufficiently dried inert solvent, e.g. dioxane, acetonitrile, etc., and aminopyridine or aminotriazine derivative expressed by formula VI is added and reacted with the derivative expressed by formula V. COPYRIGHT: (C)1987,JPO&Japio | ||||||
| 90 | Production of amide compound | JP410785 | 1985-01-16 | JPS61165339A | 1986-07-26 | KATO SHOZO; OKAMOTO HIDENORI |
| PURPOSE: To obtain an amide compound useful as drugs, agricultural chemicals, their raw materials and intermediates by one stage in high yield, by reacting a Schiff base compound with a silane compound and a carboxylic acid derivative under a mild condition. CONSTITUTION: A schiff base compound shown by the formula I (R 1 and R 2 are alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, etc.) is reacted with a compound shown by the formula II (X, Y, and Z are H, or halogen) and a carboxylic acid derivative shown by the formula III (R 3 is as shown for R 1; M is halogen, or OCOR 3) in a molar ratio of 1:1W2:1W1.2 in a solvent such as benzene, chloroform, etc., at -20W150°C for 5minW10 days, to give a com pound shown by the formula IV. EFFECT: A reaction product is easily purified. COPYRIGHT: (C)1986,JPO&Japio | ||||||
| 91 | 1,4-dihydropyridine derivative | JP411584 | 1984-01-12 | JPS60149563A | 1985-08-07 | OONO SACHIO; MIZUKOSHI SEISHI; KOMATSU OSAMU; ICHIHARA KENJI; NAKAMURA YOSHIKI |
| NEW MATERIAL:A compound expressed by formula I [R is phenyl substituted by Br, Cl, CF 3, etc. at the 2- or 3-position, phenyl substituted by Cl at the 2-position or 2,1,3-benzoxadiazol-4-yl; R 1 is 1W3C alkyl; R 2 is acetylor cyclopropyl, provided that R 2 is acetyl when R is 2,3-dichlorophenyl or 2,1,3-benzoxadiazol-4- yl]. EXAMPLE: Methyl 2-oxopropyl 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylate. USE: A medicine for preventing or treating ischemic heart diseases, cerebral circulatory disorder, hypertension, etc. or complications thereof. PREPARATION: For example, a compound expressed by formula II is reacted with a compound expressed by formula III to give a compound expressed by formula IV, which is then reacted with an acid in an aqueous solvent containing the acid to afford the aimed compound expressed by formula I (R 2 is acetyl). COPYRIGHT: (C)1985,JPO&Japio | ||||||
| 92 | Novel 1,2,4-oxadiazole derivative | JP16016783 | 1983-08-30 | JPS6051188A | 1985-03-22 | YAMAMOTO MICHIHIRO |
| NEW MATERIAL:A compound shown by the formula I [R 1 is 2-fluoro-4-biphenylyl, 2-(2,6-dichloroanilino)phenyl, 3-benzoylphenyl, 1-(4-chlorobenzoyl)-5-methoxy-2- methylindol-3-yl; R 2 is 5-membered aromatic heterocyclic ring, or its condensed biheterocyclic ring; T 1 and T 2 are lower alkylene; T 3 is lower alkylene, or single bond; X is -O-, -S-, -S(O)-, SO 2-, or single bond]. EXAMPLE: 5-[1-(4-Chlorobenzoyl)-5-methoxy-2-methylindol-3-ylmethyl]-3-(imidazol- 1-ylmethyl)-1,2,4-oxadiazole. USE: An anti-inflammatory drug. Having weak damaging action on digestive organs, and low toxicity. PREPARATION: A carboxylic acid shown by the formula II is reacted with an amidoxime shown by the formula III to give an O-acylamidoxime shown by the formula IV, which is condensed through dehydration. COPYRIGHT: (C)1985,JPO&Japio | ||||||
| 93 | Chloroacetamide derivative | JP1953583 | 1983-02-08 | JPS58148868A | 1983-09-05 | SECKINGER KARL; KUHNEN FRED; MILZNER KARLHEINZ |
| 94 | JPS5812271B2 - | JP119873 | 1972-12-23 | JPS5812271B2 | 1983-03-07 | KAMYA TAKASHI; TERACHI TSUTOMU; HASHIMOTO SHINJI; NAKAGUCHI OSAMU; OKU TERUO |
| 95 | JPS57502259A - | JP50089282 | 1981-12-25 | JPS57502259A | 1982-12-23 | |
| 96 | Emitting device and device used therein | JP2009053571 | 2009-03-06 | JP4929302B2 | 2012-05-09 | ピロウ，ジョナサン，ニジェール，ジェラルド; フランプトン，マイケル，ジョン |
| 97 | 1,2,4-oxadiazoles as modulators of metabotropic glutamate receptor-5 | JP2010135508 | 2010-06-14 | JP2010248214A | 2010-11-04 | WENSBO DAVID; XIN TAO; STEFANAC TOMISLAV; ARORA JALAJ; EDWARDS LOUISE; ISAAC METHVIN; SLASSI ABDELMALIK; STORMANN THOMAS M; MCLEOD DONALD A; KERS ANNIKA; MALMBERG JOHAN; OSCARSSON KARIN; GYBACK HELENA; JOHANSSON MARTIN; MINIDIS ALEXANDER; WALDMAN MANGUS; YNGVE ULRIKA; OSTERWALL CHRISTOFFER |
| <P>PROBLEM TO BE SOLVED: To provide 1,2,4-oxadiazoles as modulators of metabotropic glutamate receptor-5, which play a role in diseases of neurological disorders, psychiatric disorders or the like. <P>SOLUTION: The present invention relates to new compounds of formula (I), a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing the compounds and to the use of the compounds in therapy. For example the compounds are 2-[5-(3-methoxy-phenyl)-[1,2,4]oxadiazole-3-ylmethylsulphanyl]-1H-benzimidazole; 5-(3-methoxy-phenyl)-3-(4-methyl-5-thiophene-2-yl-4H-[1,2,4]triazole-3-ylsulphanylmethyl)-[1,2,4]oxadiazole or the like. <P>COPYRIGHT: (C)2011,JPO&INPIT | ||||||
| 98 | The novel heterocyclic compounds, their use in the treatment of these manufacturing methods and pharmaceutical compositions containing them, as well as diabetes and related diseases | JP53930797 | 1997-06-30 | JP4339402B2 | 2009-10-07 | ガーラム、ランガ・マッドハバン; チャクラバルティ、ラニャン; パカラ、サルマ・ケー・エス; パラセリ、ラオ・ベーマ; ラマニャム、ラジャゴパラン; ローライ、ビッダヤ・ブースハン; ローライ、ブライ・ブースハン |
| 99 | Emitting device and device used therein | JP2003546416 | 2002-11-15 | JP4315808B2 | 2009-08-19 | ピロウ，ジョナサン，ニジェール，ジェラルド; フランプトン，マイケル，ジョン |
| 100 | 1,2,4-oxadiazoles as a regulator of the metabotropic glutamate receptor -5 | JP2004527872 | 2003-08-08 | JP2006503009A | 2006-01-26 | アニカ、カーズ; アブデルマリク、スラッシ; アレクサンデル、ミニディス; ウルリカ、インベ; カリン、オスカルソン; クリストファー、オステルウォール; ジャラジ、アローラ; タオ、シン; デイビッド、ウェンズボー; トーマス、エム．ストーマン; ドナルド、エイ．マクレオド; トミスラブ、ステファナック; ヘレナ、ギバック; マルティン、ヨハンソン; マングス、ワルトマン; メスビン、イサック; ヨハン、マルムベルク; ルイーズ、エドワーズ |
| 本発明は、下記式Ｉのの新規化合物、それらの製造方法、およびその製造方法において製造される中間体、この化合物を含有する医薬処方物、ならびにこの化合物の療法における使用に関する。
【化１】 |
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