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2. 发明专利

JP3805905B2 Aromatic antifungal 有权
公开(公告)号：JP3805905B2
公开(公告)日：2006-08-09
申请号：JP24655498
申请日：1998-08-17
申请人：ポーラ化成工業株式会社
发明人：琢自中島 , 隆男伊藤 , 幸雄河津 , 雅之湯浅 , 暁野沢 , 利光鈴木 , 敏郎馬島
IPC分类号： A61K31/135 , C07C323/32 , A61P17/00 , A61P31/10 , C07C317/32

3. 发明专利

JP3589817B2 Antifungal 失效
公开(公告)号：JP3589817B2
公开(公告)日：2004-11-17
申请号：JP31011196
申请日：1996-11-06
申请人：ポーラ化成工業株式会社
发明人：琢自中島 , 隆男伊藤 , 幸雄河津 , 雅之湯浅 , 利光鈴木 , 敏郎馬島
IPC分类号： A61K31/135 , A01N33/10 , A61K31/137 , A61P31/04 , A61P31/10 , C07C211/27 , C07C217/56

4. 发明专利

JP3927117B2 Evaluation of an antifungal agent 有权
公开(公告)号：JP3927117B2
公开(公告)日：2007-06-06
申请号：JP2002516356
申请日：2001-07-31
申请人：ポーラ化成工業株式会社
发明人：琢自中島 , 隆男伊藤 , 暁野沢
IPC分类号： C12Q1/18 , C12Q1/06 , G01N33/15 , G01N33/50
CPC分类号： C12Q1/18 , C12Q1/06 , G01N33/5088

5. 发明专利

JP3839551B2 Amine derivative 失效
公开(公告)号：JP3839551B2
公开(公告)日：2006-11-01
申请号：JP13087897
申请日：1997-05-21
申请人：ポーラ化成工業株式会社
发明人：琢自中島 , 隆男伊藤 , 浩治横山 , 幸雄河津 , 雅之湯浅 , 浩之滝本 , 暁野沢 , 利光鈴木 , 敏郎馬島
IPC分类号： A61K31/135 , C07C211/27 , A01N33/04 , A01N33/08 , A01N35/04 , A01P3/00 , A61P31/04 , A61P31/10 , C07C209/60 , C07C211/35 , C07C213/02 , C07C215/28 , C07C221/00 , C07C223/02 , C07C225/16

6. 发明专利

JP3474939B2 Drug resistance overcoming agent 失效
公开(公告)号：JP3474939B2
公开(公告)日：2003-12-08
申请号：JP25002394
申请日：1994-09-19
申请人：ポーラ化成工業株式会社
发明人：隆男伊藤 , 正彦土屋 , 孝雄服部
IPC分类号： C07D215/22 , A61K31/495 , A61K31/496 , A61K45/00 , A61P31/04 , A61P33/02 , A61P35/00 , A61P43/00
CPC分类号： Y02A50/411
摘要： PURPOSE: To obtain a new compound useful as a medicinal resistance overcoming agent low in calcium antagonistic activity, provided with the resistance to chemotherapeutic agents, overcoming the medicinal resistance to cancers or pathogenic microbes and improving the therapeutic effect by chemotherapeutic agents. CONSTITUTION: This compound (a physiologically permissible salt thereof) is expressed by formula I [R1 is of formula II, formula III or formula IV ((n) is 1-3; (o) is 0-5; (p) is 0-4; R2 is H or a halogen)], e.g. 1-benzosuberyl-4-[2- hydroxy-3-(7-chloroquinolin-4-on-1-yl)propyl] piperazine. The compound of formula I is obtained by the following process: a compound of formula V is prepared by reaction of a halogen compound of formula R1 Cl with piperazine; separately, an epoxy compound of formula VII is formed by reaction between a compound of formula VI and an epihalohydrin in the presence of sodium hydride; and the compound of formula V and the epoxy compound of formula VII are subjected to ring opening condensation reaction. The microbial infectious diseases associated with this compound are involved in Staophylococcus aureus, Plasmodium, Trypanosoma, Escherichia coil, and Spirochete.

7. 发明专利

JP3839518B2 Antifungal 失效
公开(公告)号：JP3839518B2
公开(公告)日：2006-11-01
申请号：JP9760796
申请日：1996-03-27
申请人：ポーラ化成工業株式会社
发明人：琢自中島 , 隆男伊藤 , 優一横溝 , 幸雄河津 , 雅之湯浅 , 暁野沢 , 利光鈴木 , 敏郎馬島
IPC分类号： A61K31/135 , C07C211/27 , A01N33/04 , A01P3/00 , A61P17/00 , A61P31/04 , A61P31/10

8. 发明专利

JP3589818B2 Antifungal 失效
公开(公告)号：JP3589818B2
公开(公告)日：2004-11-17
申请号：JP31011996
申请日：1996-11-06
申请人：ポーラ化成工業株式会社
发明人：琢自中島 , 隆男伊藤 , 幸雄河津 , 雅之湯浅 , 利光鈴木 , 敏郎馬島
IPC分类号： A61K31/135 , A01N33/10 , A61K31/137 , A61P31/04 , A61P31/10 , C07C211/27 , C07C217/56

9. 发明专利

JP3474941B2 Drug resistance overcoming agent 失效
标题翻译：空值
公开(公告)号：JP3474941B2
公开(公告)日：2003-12-08
申请号：JP25006794
申请日：1994-09-19
申请人：ポーラ化成工業株式会社
发明人：隆男伊藤 , 正彦土屋 , 孝雄服部
IPC分类号： C07D295/08 , A61K31/495 , A61K31/496 , A61K45/00 , A61P31/04 , A61P33/02 , A61P35/00 , A61P43/00 , C07D215/20 , C07D215/22
CPC分类号： Y02A50/411
摘要： PURPOSE: To obtain a new compound useful as a medicinal resistance overcoming agent low in calcium antagonistic activity, provided with the resistance to chemotherapeutic agents, overcoming the medicinal resistance to cancers or pathogenic microbes and improving the therapeutic effect by chemotherapeutic agents. CONSTITUTION: This compound (a physiologically permissible salt thereof) is expressed by formula I [X and Y are each H or a halogen; R1 is a halogen, alkyl, alkyloxy, or monocyclic or bicyclic aromatic ring which may contain one nitrogen atom in the ring], e.g. 1-(3,3-diphenylpropyl)-4-[2- hydroxy-3-(quinolin-5-yloxy)propyl]piperazine. The compound of formula I is obtained by the following process: a compound of formula III is prepared by reaction of a halogen compound of formula II with piperazine; separately, an epoxy compound of formula V is formed by reaction between a compound of formula IV and an epihalohydrin in the presence of sodium hydride; and the compound of formula III and the epoxy compound of formula V are subjected to ring opening condensation reaction. The microbial infectious diseases associated with this compound are involved in Staphylococcus aureus, Plasmodium, Trypanosoma, etc.
摘要翻译：目的：获得一种新的化合物，可用作抗钙化拮抗作用的药物抵抗剂，具有抗化学治疗药物，克服对癌症或致病微生物的药用抗性，并改善化学治疗剂的治疗效果。构成：该化合物（其生理上允许的盐）由式I表示[X和Y各自为H或卤素; R1是可以在环中含有一个氮原子的卤素，烷基，烷氧基或单环或双环芳环]，例如。 1-（3,3-二苯基丙基）-4- [2-羟基-3-（喹啉-5-基氧基）丙基]哌嗪。式I化合物通过以下方法获得：式III化合物通过式II的卤素化合物与哌嗪的反应来制备; 另外，通过式IV化合物与表卤代醇在氢化钠存在下反应形成式V的环氧化合物; 并使式III化合物和式V的环氧化合物进行开环缩合反应。与该化合物相关的微生物感染性疾病涉及金黄色葡萄球菌，疟原虫，锥虫病等。

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