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1. 发明授权

US06998412B2 Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US06998412B2
公开(公告)日：2006-02-14
申请号：US10781475
申请日：2004-02-17
申请人： Kenji Kuwabara , Tomiyoshi Aoki
发明人： Kenji Kuwabara , Tomiyoshi Aoki
IPC分类号： C07D413/10 , C07D417/06 , A61K31/421 , A61K31/426
CPC分类号： A61K31/4439 , A61K31/4178 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , C07D263/32 , C07D277/24 , C07D405/06 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14
摘要： The present invention provides a preventive or therapeutic agent for hyperlipidemia, comprising as an active ingredient a heterocyclic compound of the formula [1], or a pharmaceutically acceptable salt thereof: R1-Het-D-E [1] wherein: R1 is optionally substituted aryl or aromatic heterocyclic group, Het is a divalent aromatic heterocyclic group, D is alkylene, alkenylene, alkynylene, or the like, and E is carboxy, or the like, and novel compounds among the heterocyclic compounds of the formula [1] above, which has blood triglyceride lowering effect, LDL-C lowering effect, and blood glucose lowering effect and blood insulin lowering effect, or HDL-C increasing effect or atherogenic index lowering effect all together, and hence is useful in the prevention or treatment of hyperlipidemia, arteriosclerosis, diabetes mellitus, hypertension, obesity, and the like.
摘要翻译：本发明提供高脂血症的预防或治疗剂，其包含作为活性成分的式[1]的杂环化合物或其药学上可接受的盐

2. 发明申请

US20050009892A1 Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US20050009892A1
公开(公告)日：2005-01-13
申请号：US10781433
申请日：2004-02-17
申请人： Kenji Kuwabara , Tomiyoshi Aoki
发明人： Kenji Kuwabara , Tomiyoshi Aoki
IPC分类号： A61K31/4178 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , A61K31/4439 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P9/12 , C07D263/32 , C07D277/24 , C07D277/30 , C07D405/06 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D263/30
CPC分类号： A61K31/4439 , A61K31/4178 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , C07D263/32 , C07D277/24 , C07D405/06 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14
摘要： The present invention provides a preventive or therapeutic agent for hyperlipidemia, comprising as an active ingredient a heterocyclic compound of the formula [1], or a pharmaceutically acceptable salt thereof: R1—Het-D-E [1]wherein: R1 is optionally substituted aryl or aromatic heterocyclic group, Het is a divalent aromatic heterocyclic group, D is alkylene, alkenylene, alkynylene, or the like, and E is carboxy, or the like, and novel compounds among the heterocyclic compounds of the formula [1] above, which has blood triglyceride lowering effect, LDL-C lowering effect, and blood glucose lowering effect and blood insulin lowering effect, or HDL-C increasing effect or atherogenic index lowering effect all together, and hence is useful in the prevention or treatment of hyperlipidemia, arteriosclerosis, diabetes mellitus, hypertension, obesity, and the like.
摘要翻译：本发明提供高脂血症的预防或治疗剂，其包含作为活性成分的式[1]的杂环化合物或其药学上可接受的盐：R 1 -Het-DE [1]其中：R 1 >是任选取代的芳基或芳族杂环基，Het是二价芳族杂环基，D是亚烷基，亚烯基，亚炔基等，E是羧基等，并且式[ 1]，其具有血液甘油三酯降低效果，LDL-C降低作用，降血糖作用和血液胰岛素降低作用，或HDL-C增加作用或致动脉粥样化指数降低作用，因此可用于预防或治疗高脂血症，动脉硬化，糖尿病，高血压，肥胖等。

3. 发明授权

US07030143B2 Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US07030143B2
公开(公告)日：2006-04-18
申请号：US10781293
申请日：2004-02-17
申请人： Kenji Kuwabara , Tomiyoshi Aoki
发明人： Kenji Kuwabara , Tomiyoshi Aoki
IPC分类号： A61K31/421 , A61K31/4439 , C07D413/04
CPC分类号： A61K31/4439 , A61K31/4178 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , C07D263/32 , C07D277/24 , C07D405/06 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14
摘要： The present invention provides a preventive or therapeutic agent for hyperlipidemia, comprising as an active ingredient a heterocyclic compound of the formula [1], or a pharmaceutically acceptable salt thereof: wherein: R1 is optionally substituted aryl or aromatic heterocyclic group, Het is a divalent aromatic heterocyclic group, D is alkylene, alkenylene, alkynylene, or the like, and E is carboxy, or the like, and novel compounds among the heterocyclic compounds of the formula [1] above, which has blood triglyceride lowering effect, LDL-C lowering effect, and blood glucose lowering effect and blood insulin lowering effect, or HDL-C increasing effect or atherogenic index lowering effect all together, and hence is useful in the prevention or treatment of hyperlipidemia, arteriosclerosis, diabetes mellitus, hypertension, obesity, and the like.
摘要翻译：本发明提供高脂血症的预防或治疗剂，其包含作为活性成分的式[1]的杂环化合物或其药学上可接受的盐：其中：R 1是任选取代的芳基或芳族杂环基，Het为二价芳族杂环基，D为亚烷基，亚烯基，亚炔基等，E为羧基等，上述式[1]的杂环化合物中具有新化合物，其具有血液甘油三酯降低效果，降低LDL-C降低作用，血糖降低作用和血胰岛素降低作用，或HDL-C增加效果或致动脉粥样化指数降低作用，因此可用于预防或治疗高脂血症，动脉硬化，糖尿病，高血压，肥胖等。

4. 发明授权

US07022723B2 Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US07022723B2
公开(公告)日：2006-04-04
申请号：US10781433
申请日：2004-02-17
申请人： Kenji Kuwabara , Tomiyoshi Aoki
发明人： Kenji Kuwabara , Tomiyoshi Aoki
IPC分类号： A61K31/421 , C07D263/32
CPC分类号： A61K31/4439 , A61K31/4178 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , C07D263/32 , C07D277/24 , C07D405/06 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14
摘要： The present invention provides a preventive or therapeutic agent for hyperlipidemia, comprising as an active ingredient a heterocyclic compound of the formula [1], or a pharmaceutically acceptable salt thereof: R1-Het-D-E [1] wherein: R1 is optionally substituted aryl or aromatic heterocyclic group, Het is a divalent aromatic heterocyclic group, D is alkylene, alkenylene, alkynylene, or the like, and E is carboxy, or the like, and novel compounds among the heterocyclic compounds of the formula [1] above, which has blood triglyceride lowering effect, LDL-C lowering effect, and blood glucose lowering effect and blood insulin lowering effect, or HDL-C increasing effect or atherogenic index lowering effect all together, and hence is useful in the prevention or treatment of hyperlipidemia, arteriosclerosis, diabetes mellitus, hypertension, obesity, and the like.
摘要翻译：本发明提供高脂血症的预防或治疗剂，其包含作为活性成分的式[1]的杂环化合物或其药学上可接受的盐：<？在线配方描述=“在线配方”末端 =“引线”→R Het-DE [1] <？在线公式描述=“在线公式”end =“tail”？>其中： 1是任选取代的芳基或芳族杂环基，Het是二价芳族杂环基，D是亚烷基，亚烯基，亚炔基等，E是羧基等，杂环化合物中的新化合物具有血甘油三酯降低作用，低密度脂蛋白降低作用，血糖降低作用和血胰岛素降低作用，或HDL-C增加作用或致动脉粥样硬化指数降低作用的上述式[1]，因此是有用的在预防或治疗高脂血症，动脉硬化，糖尿病，高血压，obesi ty等。

5. 发明授权

US07144906B2 Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US07144906B2
公开(公告)日：2006-12-05
申请号：US10276670
申请日：2001-05-25
申请人： Kenji Kuwabara , Tomiyoshi Aoki
发明人： Kenji Kuwabara , Tomiyoshi Aoki
IPC分类号： A61K31/421 , C07D263/32
CPC分类号： A61K31/4439 , A61K31/4178 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , C07D263/32 , C07D277/24 , C07D405/06 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14
摘要： The present invention provides a preventive or therapeutic agent for hyperlipidemia, comprising as an active ingredient a heterocyclic compound of the formula [1], or a pharmaceutically acceptable salt thereof: R1-Het-D-E [1] wherein: R1 is optionally substituted aryl or aromatic heterocyclic group, Het is a divalent aromatic heterocyclic group, D is alkylene, alkenylene, alkynylene, or the like, and E is carboxy, or the like, and novel compounds among the heterocyclic compounds of the formula [1] above, which has blood triglyceride lowering effect, LDL-C lowering effect, and blood glucose lowering effect and blood insulin lowering effect, or HDL-C increasing effect or atherogenic index lowering effect all together, and hence is useful in the prevention or treatment of hyperlipidemia, arteriosclerosis, diabetes mellitus, hypertension, obesity, and the like.
摘要翻译：本发明提供高脂血症的预防或治疗剂，其包含作为活性成分的式[1]的杂环化合物或其药学上可接受的盐：<？在线配方描述=“在线配方”末端 =“引线”→R Het-DE [1] <？在线公式描述=“在线公式”end =“tail”？>其中： 1是任选取代的芳基或芳族杂环基，Het是二价芳族杂环基，D是亚烷基，亚烯基，亚炔基等，E是羧基等，杂环化合物中的新化合物具有血甘油三酯降低作用，低密度脂蛋白降低作用，血糖降低作用和血胰岛素降低作用或HDL-C增加作用或致动脉粥样硬化指数降低作用的上述式[1]，因此是有用的预防或治疗高脂血症，动脉硬化，糖尿病，高血压，肥胖等，等等。

6. 发明申请

US20050009785A1 Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US20050009785A1
公开(公告)日：2005-01-13
申请号：US10781293
申请日：2004-02-17
申请人： Kenji Kuwabara , Tomiyoshi Aoki
发明人： Kenji Kuwabara , Tomiyoshi Aoki
IPC分类号： A61K31/4178 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , A61K31/4439 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P9/12 , C07D263/32 , C07D277/24 , C07D277/30 , C07D405/06 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , A61K31/675
CPC分类号： A61K31/4439 , A61K31/4178 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , C07D263/32 , C07D277/24 , C07D405/06 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14
摘要： The present invention provides a preventive or therapeutic agent for hyperlipidemia, comprising as an active ingredient a heterocyclic compound of the formula [1], or a pharmaceutically acceptable salt thereof: wherein: R1 is optionally substituted aryl or aromatic heterocyclic group, Het is a divalent aromatic heterocyclic group, D is alkylene, alkenylene, alkynylene, or the like, and E is carboxy, or the like, and novel compounds among the heterocyclic compounds of the formula [1] above, which has blood triglyceride lowering effect, LDL-C lowering effect, and blood glucose lowering effect and blood insulin lowering effect, or HDL-C increasing effect or atherogenic index lowering effect all together, and hence is useful in the prevention or treatment of hyperlipidemia, arteriosclerosis, diabetes mellitus, hypertension, obesity, and the like.
摘要翻译：本发明提供高脂血症的预防或治疗剂，其包含作为活性成分的式[1]的杂环化合物或其药学上可接受的盐：其中：R 1是任选取代的芳基或芳族杂环基团，Het 是二价芳香族杂环基，D是亚烷基，亚烯基，亚炔基等，E是羧基等，上述式[1]的杂环化合物中具有降低血液甘油三酯的效果的新化合物， LDL-C降低作用，血糖降低作用及血胰岛素降低作用，或HDL-C增加作用或致动脉粥样硬化指标降低作用，因此可用于预防或治疗高脂血症，动脉硬化，糖尿病，高血压，肥胖等。

7. 发明授权

US5945426A Derivatives of pyrimidine for treating acute cerebrovascular disorders 失效
标题翻译：嘧啶衍生物用于治疗急性脑血管障碍
公开(公告)号：US5945426A
公开(公告)日：1999-08-31
申请号：US809004
申请日：1997-03-07
申请人： Shoichi Chokai , Yojiro Ukai , Tomiyoshi Aoki , Kyoichi Ideguchi
发明人： Shoichi Chokai , Yojiro Ukai , Tomiyoshi Aoki , Kyoichi Ideguchi
IPC分类号： A61K31/506 , A61K9/08 , A61K9/20 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/444 , A61K31/4453 , A61K31/495 , A61K31/505 , A61K31/53 , A61P9/10 , A61P25/28 , A61P43/00 , C07D213/63 , C07D213/64 , C07D239/32 , C07D239/34 , C07D239/38 , C07D239/52 , C07D239/56 , C07D251/16 , C07D251/22 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/04 , C07D409/12 , A01N43/54 , C07D239/02
CPC分类号： C07D213/64 , C07D239/34 , C07D239/38 , C07D239/52 , C07D239/56 , C07D251/22 , C07D401/04 , C07D401/12 , C07D409/04
摘要： A pharmaceutical composition comprising a compound of the following general formula �I! or its salt. ##STR1## wherein R.sup.1 represents aryl or a heteroaromatic group. R.sup.2 represents hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, haloalkyl, alkoxy, alkylthio, amino, monoalkylamino, dialkylamino, or phenyl. R.sup.3 and R.sup.4 independently represent hydrogen or alkyl or R.sup.3 and R.sup.4 taken together with the adjacent N atom represent a 5- through 7-membered cyclic amino group. A represents C.sub.2-10 alkylene. W represents O, S, or (CH).sub.n (where CH may be substituted by alkyl; n is an integer of 1 or 2). X, Y, and Z may be the same or different and each represents CH (which may be substituted by alkyl), or N. Provided, however, that the case in which X, Y, and Z concurrently represent CH is excluded. The compound of the invention has excellent neuronal death inhibitory activity and is useful as a therapeutic drug for cerebrovascular diseases.
摘要翻译： PCT No.PCT / JP95 / 01792 Sec。 371日期1997年3月7日 102（e）1997年3月7日PCT PCT 1995年9月8日PCT公布。公开号WO96 / 07641 日期：1996年3月14日包含下列通式[I]化合物或其盐的药物组合物。其中R1表示芳基或杂芳基。 R 2表示氢，烷基，烯基，环烷基，环烷基烷基，羟基烷基，卤代烷基，烷氧基，烷硫基，氨基，单烷基氨基，二烷基氨基或苯基。 R3和R4独立地表示氢或烷基，R3和R4与相邻的N原子一起表示5-至7-元环氨基。 A表示C2-10亚烷基。 W表示O，S或（CH）n（其中CH可以被烷基取代; n是1或2的整数）。 X，Y和Z可以相同或不同，各自表示CH（可以被烷基取代）或N.可以排除X，Y和Z同时表示CH的情况。本发明化合物具有优异的神经元死亡抑制活性，可用作脑血管疾病的治疗药物。

8. 发明授权

US5589477A Pyrimidine derivatives and drugs 失效
标题翻译：嘧啶衍生物和药物
公开(公告)号：US5589477A
公开(公告)日：1996-12-31
申请号：US983515
申请日：1993-02-26
申请人： Shoichi Chokai , Tomiyoshi Aoki , Kiyoshi Kimura
发明人： Shoichi Chokai , Tomiyoshi Aoki , Kiyoshi Kimura
IPC分类号： C07D239/34 , C07D239/42 , C07D401/12 , C07D453/02 , A61K31/505 , C07D403/04 , C07D403/12
CPC分类号： C07D453/02 , C07D239/34 , C07D239/42 , C07D401/12
摘要： The object of the present invention is to obtain new class of compounds which have improving effect on learning and memory disorders with good selectivity in central nervous system and little side effects and then to provide a good medicine for treatment of dementia.The present invention relates to the compounds represented by the following general formula or their pharmacologically acceptable salts and the drugs of improving learning or memory disorders comprising them as active ingredients. ##STR1## (wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen, hydroxy, alkoxy, trifluoromethyl or halogen. A represents methyl, trifluoromethyl, or tert-butyl. Y represents O or NH.)
摘要翻译： PCT No.PCT / JP91 / 01152 Sec。 371日期：1993年2月26日 102（e）日期1993年2月26日PCT 1991年8月29日PCT PCT。出版物WO92 / 04333 1992年3月19日本发明的目的是获得对中枢神经系统具有良好选择性和副作用小的学习和记忆障碍有改善作用的新一类化合物，并提供治疗痴呆症的良好药物。本发明涉及由以下通式表示的化合物或其药理学上可接受的盐以及改善学习或记忆障碍的药物，其包含它们作为活性成分。（其中R1和R2相同或不同，为氢，羟基，烷氧基，三氟甲基或卤素），A代表甲基，三氟甲基或叔丁基，Y代表O或NH。

9. 发明授权

US5342845A Indole derivatives and drugs 失效
标题翻译：吲哚衍生物和药物
公开(公告)号：US5342845A
公开(公告)日：1994-08-30
申请号：US983513
申请日：1993-02-26
申请人： Shoichi Chokai , Tomiyoshi Aoki , Yojiro Ukai
发明人： Shoichi Chokai , Tomiyoshi Aoki , Yojiro Ukai
IPC分类号： C07D453/02 , A61K31/435
CPC分类号： C07D453/02
摘要： The object of the invention is to provide a novel compound having serotonin antagonist activity.The invention is directed to an indolecarboxamide derivative of the following general formula [I] and a serotonin antagonist composition comprising the same derivative as an active ingredient. ##STR1## (wherein R.sup.1 is a lower alkyl and R.sup.2 is hydrogen, a halogen, a lower alkyl or a lower alkoxy.)The compound of the invention is effective as a gastrointestinal motor activity regulator, antimigraine, antipsychotic or antianxiety drug. The compound is also effective as a therapeutic drug for dementia or orthostatic hypotension.
摘要翻译： PCT No.PCT / JP91 / 01148 Sec。 371日期：1993年2月26日 102（e）日期1993年2月26日PCT 1991年8月29日PCT PCT。出版物WO92 / 04347 1992年3月19日，本发明的目的是提供一种具有5-羟色胺拮抗剂活性的新化合物。本发明涉及以下通式[I]的吲哚甲酰胺衍生物和包含与活性成分相同的衍生物的5-羟色胺拮抗剂组合物。是氢，卤素，低级烷基或低级烷氧基）。本发明化合物作为胃肠运动活性调节剂，抗偏头痛，抗精神病药或抗焦虑药有效。该化合物作为痴呆或直立性低血压的治疗药物也是有效的。

10. 发明授权

US06787546B2 Heterocycle derivatives and drugs 失效
标题翻译：杂环衍生物和药物
公开(公告)号：US06787546B2
公开(公告)日：2004-09-07
申请号：US10149622
申请日：2002-06-12
申请人： Toshiyuki Suzuki , Tomiyoshi Aoki
发明人： Toshiyuki Suzuki , Tomiyoshi Aoki
IPC分类号： A61K3144
CPC分类号： C07D213/42 , C07D213/89
摘要： The object of the invention is to provide an excellent compound as a drug. The invention relates to a heterocyclic compound shown by the following formula: A—B—D—E [1] wherein A is heteroaryl or its oxide; B is ethenylene; D is optionally substituted phenylene; and E is a group of the formula: wherein G is optionally substituted phenyl; and R is heteroaryl or heteroarylmethyl, or a group of the formula: wherein n is an integer of 1 to 5; R5 and R6 are same or different and are independently selected from the group consisting of hydrogen, C1—C6 alkyl, hydroxyalkyl, aminoalkyl; or R5 and R6 taken together with the adjacent nitrogen atom may form 5- to 7-membered cyclic amino group for —NR5R6 or a salt thereof.
摘要翻译：本发明的目的是提供作为药物的优异的化合物。本发明涉及下式所示的杂环化合物：其中A是杂芳基或其氧化物; B是亚乙烯基; D是任选取代的亚苯基; 和E是下式的基团：其中G是任选取代的苯基; R是杂芳基或杂芳基甲基，或下式的基团：其中n是1至5的整数; R 5和R 6相同或不同，并且独立地选自氢，C 1 -C 6烷基，羟基烷基，氨基烷基; 或R 5和R 6与相邻氮原子一起可以形成-NR 5 R 6的5-至7-元环氨基或其盐。

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