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1. 发明专利

JPS62273975A PHENYLPYRIDAZINONE DERIVATIVE AND CARDIOTONIC AGENT 失效
公开(公告)号：JPS62273975A
公开(公告)日：1987-11-28
申请号：JP11895486
申请日：1986-05-22
申请人： SHIONOGI & CO
发明人： OGATA HIDE , MATSUMOTO HIROSHI , KIMOTO SADATOSHI , UEDA MOTOHIKO
IPC分类号： A61K31/50 , A61P9/04 , C07D231/00 , C07D233/00 , C07D233/60 , C07D235/00 , C07D237/00 , C07D249/00 , C07D403/10 , C07D403/14
摘要： NEW MATERIAL:A compound expressed by formula I [formula II is single bond or double bond; R and R are H, alkyl or phenyl; R is H, alkyl or (substituted) aralkyl; X is H, alkyl or halogen; Az is 1H-benzimidazol-1-yl, 1H-imidazol-1-yl, 1H-pyrazol-1-yl or 1H-1,2,4-triazol-1-yl]. EXAMPLE:1-{[5(3-Hydroxy-pyrimidin-6-yl)-2-methoxyphenyl]vinyl}-1H-imid azole. USE:A medicine and cardiotonic agent capable of being orally or parenterally administered. PREPARATION:An ester expressed by formula III and hydrazine hydrate are subjected to cyclization reaction in a solvent, e.g. acid-alcohol, etc., to afford the compound expressed by formula I (formula II is single bind), which is then reacted and dehydrogenated with an oxidizing agent, e.g. SeO2, etc., in a solvent to provide the compound expressed by formula I (formula II is double bond).

2. 发明专利

JPS62201872A AZOLYLPROPANOL DERIVATIVE AND ANTIFUNGAL AGENT 失效
公开(公告)号：JPS62201872A
公开(公告)日：1987-09-05
申请号：JP4501186
申请日：1986-02-28
申请人： SHIONOGI & CO
发明人： OGATA HIDE , MATSUMOTO HIROSHI , KIDA SHIRO , TAWARA KATSUYA , SHIMIZU SUMIO
IPC分类号： A61K31/41 , A61K31/415 , A61P31/04 , A61P31/10 , C07D231/12 , C07D249/08 , C07D521/00
摘要： NEW MATERIAL:An azolylpropanol derivative of formula I (AZ , AZ are imidazolyl, triazolyl, pyrazolyl; R is alkyl, haloalkyl; R is halogen, trifluoromethyl; R is H halogen) or its salt. EXAMPLE:2-Methoxy-2-(1H-1,2,4-triazol-1-yl)-2',4'-difluoroacetop-h-enone. USE:It has excellent antifungal activity and can be used orally or by injection. Further, it is used as a fungicide for agricultural and horizontal purposes and as a remedy for fungal infection in mammarians other than human. PREPARATION:As shown in the reaction equations, for example, the reaction of a compound of formula II with N,N'-sulfinyl-bis-azole is followed by the oxirane formation of the produce to give a compound of formula IV. Then, the oxirane is allowed to react with 1H-imidazole to give the compound of formula I.

3. 发明专利

JPS59167573A Azole propylene glycol derivative 失效
标题翻译：丙烯酸衍生物衍生物
公开(公告)号：JPS59167573A
公开(公告)日：1984-09-21
申请号：JP4272883
申请日：1983-03-14
申请人： Shionogi & Co Ltd
发明人： OGATA HIDE , MATSUMOTO HIROSHI , TAWARA KATSUYA
IPC分类号： C07D249/08 , A61K31/41 , A61K31/415 , A61P31/04 , A61P31/10 , C07D233/60
摘要： NEW MATERIAL:An azole propylene glycol derivative shown by the formula I (Q is imidazolyl, or triazolyl; X
1 , X
2 , Y
1 , and Y
2 are H, halogen, alkyl, trifluoromethyl, alkoxy, or nitro, respectively) or its acid addition salt.
EXAMPLE: 1,2-Bis(2,4-dichlorophenyl)-3-(1H-imidazol-1-yl)propylene glycol.
USE: Showing improved antifungal action, useful as a drug or a drug for animals. Effective as an antifungal agent especially for internal use and injection.
PREPARATION: A raw material compound shown by the formula II is subjected to oxirane formation reaction, to give an ethylene oxide shown by the formula III. This compound shown by the formula III is then reacted with 1H-imidazole, etc. to give a ketol shown by the formula IV, the compound shown by the formula IV is reduced, to give a compound shown by the formula I .
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：式I所示的唑类丙二醇衍生物（Q为咪唑基或三唑基; X 1，X 2，Y 1和Y 2为H，卤素，烷基，三氟甲基，烷氧基或硝基）或其酸加成盐。实施例：1,2-双（2,4-二氯苯基）-3-（1H-咪唑-1-基）丙二醇。使用：显示出改善的抗真菌作用，可用作动物的药物或药物。作为抗真菌剂，特别适用于内部使用和注射。制备：将式II表示的原料化合物进行环氧乙烷生成反应，得到式III所示的环氧乙烷。然后将式III所示的化合物与1H-咪唑等反应，得到式IV所示的酮醇，将式IV所示的化合物还原，得到式I所示的化合物。

4. 发明专利

JPS5965038A Synthesis of 3,6-dichloro-2-hydroxyacetophenone 失效
标题翻译： 3,6-二氯-2-羟基乙酸乙酯的合成
公开(公告)号：JPS5965038A
公开(公告)日：1984-04-13
申请号：JP17489582
申请日：1982-10-04
申请人： Shionogi & Co Ltd
发明人： OGATA HIDE , MATSUMOTO HIROSHI
IPC分类号： C07C45/53 , B01J27/00 , B01J27/10 , C07B61/00 , C07C45/00 , C07C49/825 , C07C67/00
CPC分类号： Y02P20/52
摘要： PURPOSE: To prepare the titled compound useful as an intermediate of pharmaceuticals, agricultural chemicals, etc., in which selectivity, suppressing the production of para-isomer, by heating 2,5-dichlorophenol acetate in the presence of aluminum chloride in a solvent.
CONSTITUTION: The objective 3,6-dichloro-2-hydroxyacetophenone is prepared by heating 2,5-dichlorophenol acetate at 100W180°C, preferably 120W150°C in the presence of aluminum chloride, in a solvent such as nitrobenzene, carbon disulfide, ethane tetrachloride, dichlorobenzene, etc. (especially preferably nitrobenzen). The mixture of the produced isomers, etc. is separated preferably by steam distillation.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：目的：通过在溶剂中氯化铝存在下加热2,5-二氯苯酚乙酸酯，制备可用作药物，农药等中间体的标题化合物，其中选择性抑制对位异构体的产生。构成：目标3,6-二氯-2-羟基苯乙酮通过在氯化铝存在下，在100-180℃，优选120-150℃加热2,5-二氯苯酚乙酸酯，在溶剂如硝基苯，二硫化碳，四氯化乙烷，二氯苯等（特别优选硝基苯）。所产生的异构体等的混合物优选通过蒸汽蒸馏分离。

5. 发明专利

JPH05339250A 失效
公开(公告)号：JPH05339250A
公开(公告)日：1993-12-21
申请号：JP15392692
申请日：1992-06-12
申请人： SHIONOGI & CO
发明人： TAKASE AKIRA , KAI HIROYUKI , SUGIMOTO HIROHIKO , HATTORI NAOHIKO , FUJIWARA TAMIO , OGATA HIDE , MATSUMOTO HIROSHI
IPC分类号： A61K31/42 , A61P31/12 , C07D261/04 , C07D413/00
摘要： PURPOSE:To obtain a new compound, excellent in antiviral activity, especially antiinfluenzal activity and useful as a low toxic antiviral agent. CONSTITUTION:The objective compound of formula I (R1 to R3 are H, alkyl, alkoxy, alkenyl, etc.; R4 is H, alkyl, akoxyalkyl, etc.; R5 is cyano, alkyl or phenyl), e.g. 3-aminomethyl-5-t-butyl-2-isoxazoline. This compound of formula I is obtained by reacting a compound of formula II with an oxime derivative of formula III (Y is halogen or alkoxy) in the presence of a base (e.g. triethylamine) in a solvent (e.g. methanol) at -10 to +100 deg.C) for 0.5 to 100hr. The reaction is carried out by using the compound of formula II in an amount of 1-10 equiv. and the base in an amount of 1-5 equiv. based on 1 equiv. compound of formula II.

6. 发明专利

JPS59186906A Agricultural fungicide containing isocyanic acid phenyl ester 失效
标题翻译：含农药的异柠檬酸苯酯
公开(公告)号：JPS59186906A
公开(公告)日：1984-10-23
申请号：JP24814283
申请日：1983-12-26
申请人： Shionogi & Co Ltd
发明人： OGATA HIDE , WATANABE YOSHIYA , MATSUMOTO HIROSHI , TAWARA KATSUYA
IPC分类号： A01N47/46
摘要： PURPOSE: An agricultural fungicide capable of controlling blights of growing crops at part above the ground, and soil blights occurring on the ground part and in the underground part, containing an isocyanic acid phenyl ester as an active ingredient.
CONSTITUTION: A fungicide containing a compound shown by the formula (R
1 is 1W3C alkoxy, 2W6C dialkylamino; R
2 is 1W3C alkyl; R
3 is H, 1W3C alkyl, or 1W3C alkoxy), such as isothiocyanic acid 3-methoxycarbonyl-4-methoxyphenyl ester as an active ingredient. The compound has improved controlling effect on microorganisms such as Pythium, Rhizoctonia, Fusarium, etc. causing powdery mildew, downy mildew, anthrancose of cucurbitaceous plants, blast of rice plants, bacterial wilt of various kinds of crops. For example, 100W200l of 100W 1,000ppm spray based on 10 Are is applied, and in case of dust 3W4kg for each 10 Are.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：目的：一种能够控制地上部分生长作物枯萎的农药杀菌剂，以及含有异氰酸苯酯作为活性成分的地下部分和地下部分发生的土壤病害。构成：含有式（R 1）所示化合物的杀真菌剂为1-3C烷氧基，2-6C二烷基氨基; R 2为1-3C烷基; R 3为H，1-3C烷基或 1-3C烷氧基），例如异硫氰酸3-甲氧基羰基-4-甲氧基苯基酯作为活性成分。该化合物对腐霉，丝核菌，镰刀菌等微生物具有改善的防治效果，引起白粉病，霜霉病，葫芦科植物的唾液酸，水稻瘟病，各种作物的枯萎病。例如，100-200l 100ppm喷雾基于10被施加，并且在灰尘的情况下，每10个粉尘3-4kg。

7. 发明专利

JPS6041070B2 失效
公开(公告)号：JPS6041070B2
公开(公告)日：1985-09-13
申请号：JP13091082
申请日：1982-07-26
申请人： SHIONOGI & CO
发明人： OGATA HIDE , MATSUMOTO HIROSHI
IPC分类号： C07D207/09 , C07D307/14

8. 发明专利

JPS6019898B2 失效
公开(公告)号：JPS6019898B2
公开(公告)日：1985-05-18
申请号：JP13091182
申请日：1982-07-26
申请人： SHIONOGI & CO
发明人： OGATA HIDE , MATSUMOTO HIROSHI
IPC分类号： C07C235/46 , C07C67/00 , C07C235/44 , C07C235/48 , C07C235/60 , C07C301/00 , C07C307/10 , C07C311/08

9. 发明专利

JPS6017769B2 失效
公开(公告)号：JPS6017769B2
公开(公告)日：1985-05-07
申请号：JP22173483
申请日：1983-11-24
申请人： SHIONOGI & CO
发明人： OGATA HIDE , MATSUMOTO HIROSHI
IPC分类号： C07D207/09 , A61K31/40 , A61P25/00 , A61P25/18

10. 发明专利

JPS6016932B2 失效
公开(公告)号：JPS6016932B2
公开(公告)日：1985-04-30
申请号：JP13790880
申请日：1980-10-02
申请人： SHIONOGI & CO
发明人： OGATA HIDE , MATSUMOTO HIROSHI
IPC分类号： C07D207/09

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