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1. 发明授权

US5393769A Anti-fungal triazole derivatives 失效
标题翻译：抗真菌三唑衍生物
公开(公告)号：US5393769A
公开(公告)日：1995-02-28
申请号：US24827
申请日：1993-03-01
申请人： Sadao Oida , Takeo Miyaoka , Yawara Tajima , Toshiyuki Konosu , Noriko Takeda , Hiroshi Yasuda
发明人： Sadao Oida , Takeo Miyaoka , Yawara Tajima , Toshiyuki Konosu , Noriko Takeda , Hiroshi Yasuda
IPC分类号： C07D249/08 , C07D401/12 , C07D521/00 , A61K31/41
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： Compounds of formula (I): ##STR1## in which: Ar is optionally substituted phenyl; R.sup.1 is alkyl; R.sup.2 is substituted alkyl or substituted cycloalkyl; and n is 0, 1 or 2; and pharmaceutically acceptable salts and esters thereof have valuable anti-fungal properties and can be used for pharmaceutical and veterinary treatment. Methods of preparing these compounds are also provided.
摘要翻译：式（I）化合物：其中：Ar为任选取代的苯基; R1是烷基; R2是取代的烷基或取代的环烷基; 且n为0,1或2; 及其药学上可接受的盐和酯具有有价值的抗真菌性质，并可用于药物和兽医治疗。还提供了制备这些化合物的方法。

2. 发明授权

US5489606A Anti-fungal triazole derivatives, their uses 失效
标题翻译：抗真菌三唑衍生物，其用途
公开(公告)号：US5489606A
公开(公告)日：1996-02-06
申请号：US316082
申请日：1994-09-30
申请人： Sadao Oida , Takeo Miyaoka , Yawara Tajima , Toshiyuki Konosu , Noriko Takeda , Hiroshi Yasuda
发明人： Sadao Oida , Takeo Miyaoka , Yawara Tajima , Toshiyuki Konosu , Noriko Takeda , Hiroshi Yasuda
IPC分类号： C07D249/08 , C07D401/12 , C07D521/00 , A01N43/653
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： Compounds of formula (I): ##STR1## in which: Ar is optionally substituted phenyl; is R.sup.1 is alkyl; R.sup.2 is substituted alkyl, substituted cycloalkyl R.sup.2 or optionally substituted heterocyclic; and n is 0, 1 or 2; and pharmaceutically acceptable salts and esters thereof have valuable anti-fungal properties and can be used for pharmaceutical and veterinary treatment. Methods of preparing these compounds are also provided.
摘要翻译：式（I）化合物：其中：Ar为任选取代的苯基; R1是烷基; R2是取代的烷基，取代的环烷基R2或任选取代的杂环; 且n为0,1或2; 及其药学上可接受的盐和酯具有有价值的抗真菌性质，并可用于药物和兽医治疗。还提供了制备这些化合物的方法。

3. 发明授权

US06300357B1 Triazole antifungal agent 失效
标题翻译：三唑抗真菌剂
公开(公告)号：US06300357B1
公开(公告)日：2001-10-09
申请号：US09241369
申请日：1999-02-01
申请人： Sadao Oida , Teruo Tanaka , Yawara Tajima , Toshiyuki Konosu , Atsushi Somada , Takeo Miyaoka , Hiroshi Yasuda
发明人： Sadao Oida , Teruo Tanaka , Yawara Tajima , Toshiyuki Konosu , Atsushi Somada , Takeo Miyaoka , Hiroshi Yasuda
IPC分类号： C07D24908
CPC分类号： C07D231/12 , A01N43/653 , C07D233/56 , C07D249/08
摘要： A triazole compound having the formula: wherein Ar1 represents a phenyl group which may be substituted, Ar2 represents a heterocyclic group which may be substituted, R0 represents a hydrogen atom or a lower alkyl; R1 represents a lower alkyl; R2 to R5 each represent a hydrogen atom or an unsubstituted or halo substituted alkyl; n represents 0 to 2; p represents 0 or 1; q, r and s each represent 0 to 2; A represents a 4- to 7-membered carbon ring or a 4- to 7-membered heterocyclic group. The compound of the present invention exhibits an excellent antifungal activity.
摘要翻译：具有下式的三唑化合物：其中Ar1表示可被取代的苯基，Ar2表示可被取代的杂环基，R0表示氢原子或低级烷基; R1代表低级烷基; R 2至R 5各自表示氢原子或未取代或卤素取代的烷基; n表示0〜2; p表示0或1; q，r和s各自表示0〜2; A表示4-至7-元碳环或4-至7-元杂环基。本发明的化合物显示出优异的抗真菌活性。

4. 发明授权

US5977152A Triazole antifungal agent 失效
标题翻译：三唑抗真菌剂
公开(公告)号：US5977152A
公开(公告)日：1999-11-02
申请号：US944304
申请日：1997-10-06
申请人： Sadao Oida , Teruo Tanaka , Yawara Tajima , Toshiyuki Konosu , Atsushi Somada , Takeo Miyaoka , Hiroshi Yasuda
发明人： Sadao Oida , Teruo Tanaka , Yawara Tajima , Toshiyuki Konosu , Atsushi Somada , Takeo Miyaoka , Hiroshi Yasuda
IPC分类号： A01N43/653 , A61K31/4196 , C07D249/08 , C07D401/12 , C07D409/12 , C07D521/00 , A61K31/41
CPC分类号： C07D231/12 , A01N43/653 , C07D233/56 , C07D249/08
摘要： A triazole compound having the formula: ##STR1## wherein Ar.sup.1 represents an optionally substituted phenyl, Ar.sup.2 represents an optionally substituted phenyl, R.sup.0 represents a hydrogen atom or a lower alkyl; R.sup.1 represents a lower alkyl; R.sup.2 to R.sup.5 represent a hydrogen atom or an unsubstituted or halo substituted alkyl, n represents 0 to 2; p represents 0 or 1; q, r and s each represent 0 to 2; and A represents a 1,3-dioxan-5-yl. The triazole compound of the present invention exhibits an excellent antifungal activity.
摘要翻译：具有下式的三唑化合物：其中Ar 1表示任选取代的苯基，Ar 2表示任选取代的苯基，R 0表示氢原子或低级烷基; R1代表低级烷基; R 2至R 5表示氢原子或未取代或卤素取代的烷基，n表示0至2; p表示0或1; q，r和s各自表示0〜2; A代表1,3-二恶烷-5-基。本发明的三唑化合物表现出优异的抗真菌活性。

5. 发明授权

US06306880B1 Triazole antifungal agent 失效
标题翻译：三唑抗真菌剂
公开(公告)号：US06306880B1
公开(公告)日：2001-10-23
申请号：US09241370
申请日：1999-02-01
申请人： Sadao Oida , Teruo Tanaka , Yawara Tajima , Toshiyuki Konosu , Atsushi Somada , Takeo Miyaoka , Hiroshi Yasuda
发明人： Sadao Oida , Teruo Tanaka , Yawara Tajima , Toshiyuki Konosu , Atsushi Somada , Takeo Miyaoka , Hiroshi Yasuda
IPC分类号： C07D40112
CPC分类号： C07D231/12 , A01N43/653 , C07D233/56 , C07D249/08
摘要： A triazole compound having the formula: wherein Ar1 represents a phenyl group which may be substituted; Ar2 represents a phenyl group which may be substituted; R0 represents a hydrogen atom or a lower alkyl; R1 represents a lower alkyl; R2 to R5 each represnet a hydrogen atom or an unsubstituted or halo substituted alkyl; n represnets 0 to 2; p represents 0 or 1; q, r and s each represent 0 to 2; A represents a 4- to 7-membered carbon ring or a 4- to 7-membered heterocyclic, not including 1,3-dioxan-5-yl. The compound of the present invention exhibits an excellent antifungal activity.
摘要翻译：具有下式的三唑化合物：其中Ar 1表示可被取代的苯基; Ar2表示可以被取代的苯基; R 0表示氢原子或低级烷基; R1代表低级烷基; R2至R5各自代表氢原子或未取代或卤代取代的烷基; n表示0到2; p表示0或1; q，r和s各自表示0〜2; A代表4-至7-元碳环或4-至7-元杂环，不包括1,3-二恶烷-5-基。本发明的化合物显示出优异的抗真菌活性。

6. 发明授权

US4564676A Process for preparing cephalosporin derivatives 失效
标题翻译：制备头孢菌素衍生物的方法
公开(公告)号：US4564676A
公开(公告)日：1986-01-14
申请号：US477836
申请日：1983-03-23
申请人： Junichi Nakazawa , Teruo Hashimoto , Masanao Kaneko , Takeo Miyaoka
发明人： Junichi Nakazawa , Teruo Hashimoto , Masanao Kaneko , Takeo Miyaoka
IPC分类号： A61K20060101 , A61K31/545 , C07D501/04 , C07D501/18 , C07D501/36 , C07D501/38 , C07D501/48
CPC分类号： C07D501/04
摘要： A 7-acylamino (or 7-amino)-3-(substituted thiomethyl)cephalosporin derivative or a carboxyl derivative thereof is prepared by heating the corresponding 7-acylamino (or 7-amino)-3-carbamoyloxymethylcephalosporanic acid or a carboxyl derivative thereof with a thiol corresponding to the group which it is desired to introduce at the 3-position under conditions in which the water present is minimized, specifically, either no water is present or the amount of water is limited to less than 5 times the weight of the 7-acylamino (or 7-amino)-3-carbamoyloxymethylcephalosporanic acid or carboxyl derivative thereof. The compounds thus prepared are useful as pharmaceuticals or as intermediates in the production of pharmaceuticals. One of the compounds thus prepared, namely 7.alpha.-methoxy-3-(1-methyl-1H-tetrazol-5-yl)thiomethyl-7.beta.-(O-5-p-nitrobenzoylamino-5-carboxyvaleramido-3-cephem-4-carboxylic acid, is a new compound and it and its salts and esters also form part of the present invention.
摘要翻译：通过将相应的7-酰基氨基（或7-氨基）-3-氨基甲酰氧基甲基头孢烷酸或其羧基衍生物加热而制备7-酰基氨基（或7-氨基）-3-（取代的硫代甲基）头孢菌素衍生物或其羧基衍生物对应于在存在水存在的条件下期望在3-位引入的基团的硫醇，具体地说，不存在水或水的量被限制在小于5重量％ 7-酰基氨基（或7-氨基）-3-氨基甲酰氧基甲基头孢烷酸或其羧基衍生物。由此制备的化合物可用作药物或作为药物生产中的中间体。如此制备的一种化合物，即7α-甲氧基-3-（1-甲基-1H-四唑-5-基）硫甲基-7β-（O-5-对硝基苯甲酰氨基-5-羧基戊酰氨基-3-头孢烯-4-基） 4-羧酸，是一种新的化合物，它及其盐和酯也构成本发明的一部分。

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