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1. 发明授权

US6046218A Pyridine derivative and medicament containing the same as an effective ingredient 失效
标题翻译：吡啶衍生物和含有与有效成分相同的药物
公开(公告)号：US6046218A
公开(公告)日：2000-04-04
申请号：US952072
申请日：1997-11-17
申请人： Hiroshi Hasegawa , Tadashi Mikami , Koichi Tachibana , Kazuo Yamazaki , Noriyuki Kawamoto , Noriaki Shioiri , Koji Kusano , Susumu Sato , Hideaki Matsuda , Toshio Yokoyama
发明人： Hiroshi Hasegawa , Tadashi Mikami , Koichi Tachibana , Kazuo Yamazaki , Noriyuki Kawamoto , Noriaki Shioiri , Koji Kusano , Susumu Sato , Hideaki Matsuda , Toshio Yokoyama
IPC分类号： C07D213/69 , C07D405/06 , C07D409/06 , A61K31/435 , A61K31/44 , C07D211/72
CPC分类号： C07D213/69 , C07D405/06 , C07D409/06 , Y10S514/885
摘要： Described is a pyridine derivative represented by the following formula (1): ##STR1## wherein R.sup.1 and R.sup.2 individually represent H, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, an alkoxyalkyl group which may have a substituent, a carboxyalkyl group, an alkoxycarbonylalkyl group, an aralkyl group which may have a substituent, a phenacyl group or an acyl group, R.sup.3 represents an alkyl group, a phenyl group which may have a substituent, a heteroaryl group or a cyclic amino group, X represents O or combination of OH and H, or a salt thereof; and a medicament, such as cytokine production suppressant, comprising the derivative or salt thereof as an effective ingredient. The invention compound has potential, highly specific and highly safe immunoregulating capacity so that it can suppress the excessive production of a specific cytokine in various diseases related to the immune system.
摘要翻译： PCT No.PCT / JP97 / 00712 Sec。 371日期：1997年11月17日 102（e）日期1997年11月17日PCT 1997年3月7日PCT公布。出版物WO97 / 33870 PCT 日期：1997年9月18日是由下式（1）表示的吡啶衍生物：其中R1和R2分别表示H，烷基，环烷基，羟烷基，可具有取代基的烷氧基烷基，羧基烷基烷氧基羰基烷基，可具有取代基的芳烷基，苯甲酰甲酰基或酰基，R3表示烷基，可具有取代基的苯基，杂芳基或环状氨基，X表示O 或OH和H的组合或其盐; 以及包含其衍生物或其盐作为有效成分的药物，例如细胞因子产生抑制剂。本发明化合物具有潜在的，高度特异性和高度安全的免疫调节能力，从而可以抑制与免疫系统相关的各种疾病中特定细胞因子的过量产生。

2. 发明授权

US5789419A 4-quinolinone derivative or salt thereof 失效
标题翻译： 4-喹啉酮衍生物或其盐
公开(公告)号：US5789419A
公开(公告)日：1998-08-04
申请号：US750146
申请日：1996-12-09
申请人： Kazuo Yamazaki , Shigeru Adegawa , Yoichiro Ogawa , Hideaki Matsuda , Tadayuki Kuraishi
发明人： Kazuo Yamazaki , Shigeru Adegawa , Yoichiro Ogawa , Hideaki Matsuda , Tadayuki Kuraishi
IPC分类号： C07D215/58 , C07D401/12 , C07D405/12 , A61K3/47
CPC分类号： C07D401/12 , C07D215/58 , C07D405/12
摘要： This invention relates to a 4-quinolinone derivative represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 mean individually H, halogen, cyano, or lower alkyl, lower alkylsulfonyl, lower alkylsulfinyl, lower alkylthio or lower alkoxy which may be substituted by halogen, or phenylsulfonyl, phenylsulfinyl or phenylthio which may have a substituent; and R.sup.3 and R.sup.4 denote individually H, lower alkyl or cycloalkyl which may be substituted by halogen, or pyridyl, furanyl or phenyl which may have a substituent, or R.sup.3 and R.sup.4 may form a 4-, 5- or 6-membered heterocyclic ring, or a salt thereof, and an intermediate useful for the preparation thereof, and besides a medicinal composition comprising this compound as an active ingredient. The compound (1) or the salt thereof has an excellent potassium channel-activating effect and is useful as, for example, a prophylactic and therapeutic agent for diseases of circulatory and bronchial systems.
摘要翻译： PCT No.PCT / JP95 / 01118 Sec。 371日期1996年12月9日第 102（e）日期1996年12月9日PCT提交1995年6月6日PCT公布。出版物WO95 / 33726 1995年12月14日发明内容本发明涉及由以下通式（1）表示的4-喹啉酮衍生物：其中R1和R2分别表示H，卤素，氰基或低级烷基，低级烷基磺酰基，低级烷基亚磺酰基，可被卤素取代的低级烷硫基或低级烷氧基，或可具有取代基的苯磺酰基，苯基亚磺酰基或苯硫基; 并且R 3和R 4各自表示可以被卤素取代的H，低级烷基或环烷基，或可以具有取代基的吡啶基，呋喃基或苯基，或者R3和R4可以形成4-，5-或6-元杂环，或其盐和可用于其制备的中间体，以及包含该化合物作为活性成分的药物组合物。化合物（1）或其盐具有优异的钾通道活化作用，可用作例如循环系统和支气管系统疾病的预防和治疗剂。

3. 发明授权

US5440036A 1,4-benzoxazine derivatives 失效
标题翻译： 1,4-苯并恶嗪衍生物
公开(公告)号：US5440036A
公开(公告)日：1995-08-08
申请号：US161264
申请日：1993-12-03
申请人： Kazuo Yamazaki , Shigeru Adegawa , Yoichiro Ogawa , Hideaki Matsuda , Tadayuki Kuraishi
发明人： Kazuo Yamazaki , Shigeru Adegawa , Yoichiro Ogawa , Hideaki Matsuda , Tadayuki Kuraishi
IPC分类号： A61K31/535 , A61K31/538 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/02 , A61P15/00 , C07D265/36 , C07D413/12
CPC分类号： C07D413/12 , C07D265/36
摘要： A 1,4-benzoxazine derivative represented by the following formula (1): ##STR1## wherein R.sup.1 represents an unsubstituted or halogen-substituted lower alkyl, unsubstituted or halogen-substituted lower alkylsulfonyl, nitro or cyano group, R.sup.2 and R.sup.3 may be the same or different and individually represent a hydrogen atom or a lower alkyl group or are fused together with the adjacent carbon atom into a 3- to 6-membered carbon ring, R.sup.4 represents a hydrogen atom or an unsubstituted or substituted lower alkyl or acyl group, R.sup.5 represents a hydrogen atom or a unsubstituted or substituted lower alkyl, lower alkenyl, lower alkoxyl, aryl, aryloxyl or heterocyclic ring group, and Y represents an oxygen or sulfur atom, with the proviso that R.sup.1 is other than a nitro or cyano group when R.sup.2 and R.sup.3 are individually a methyl group, R.sup.4 is a hydrogen atom, R.sup.5 is a 3-chloropropyl group and Y is an oxygen atom; or a salt thereof.
摘要翻译：由下式（1）表示的1,4-苯并恶嗪衍生物：其中R1表示未取代或卤素取代的低级烷基，未取代或卤素取代的低级烷基磺酰基，硝基或氰基，R2和R3 可以相同或不同，并且各自表示氢原子或低级烷基，或者与相邻碳原子一起稠合成3-至6-元碳环，R4表示氢原子或未取代或取代的低级烷基或酰基，R 5表示氢原子或未取代或取代的低级烷基，低级烯基，低级烷氧基，芳基，芳氧基或杂环基，Y表示氧或硫原子，条件是R1不是硝基或当R2和R3分别为甲基时，R4为氢原子，R5为3-氯丙基，Y为氧原子; 或其盐。

4. 发明授权

US5939448A Triazole derivative or salt thereof 失效
标题翻译：三唑衍生物或其盐
公开(公告)号：US5939448A
公开(公告)日：1999-08-17
申请号：US872159
申请日：1997-06-10
申请人： Minoru Tokizawa , Sunao Takeda , Yasushi Kaneko , Hiromichi Eto , Kazuya Ishida , Kazunori Maebashi , Masaru Matsumoto , Takemitsu Asaoka , Susumu Sato , Hideaki Matsuda
发明人： Minoru Tokizawa , Sunao Takeda , Yasushi Kaneko , Hiromichi Eto , Kazuya Ishida , Kazunori Maebashi , Masaru Matsumoto , Takemitsu Asaoka , Susumu Sato , Hideaki Matsuda
IPC分类号： C07D249/08 , C07D303/34 , C07D521/00 , A61K31/41
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D303/34
摘要： Described is a triazole derivative represented by the formula (1): wherein R represents a hydrogen atom, an alkyl group, an aralkyl group or an acyl group, n stands for 0 to 2 and m stands for 1 to 5 or salt thereof, and a pharmaceutical containing the derivative or salt as an effective ingredient.
摘要翻译：描述了由式（1）表示的三唑衍生物：其中R表示氢原子，烷基，芳烷基或酰基，n表示0至2，m表示1至5或其盐，含有衍生物或盐作为有效成分的药物。

5. 发明授权

US6124347A Chromene derivatives and salts thereof, and pharmaceuticals containing the same 失效
标题翻译：色烯衍生物及其盐，以及含有它们的药物
公开(公告)号：US6124347A
公开(公告)日：2000-09-26
申请号：US162451
申请日：1998-09-29
申请人： Fumio Ishii , Haruyoshi Honda , Fujiko Konno , Tomomi Okada , Terumitsu Kaihoh , Yoshihiro Nagao , Susumu Sato , Hideaki Matsuda
发明人： Fumio Ishii , Haruyoshi Honda , Fujiko Konno , Tomomi Okada , Terumitsu Kaihoh , Yoshihiro Nagao , Susumu Sato , Hideaki Matsuda
IPC分类号： A61K31/35 , A61K31/352 , A61P3/08 , A61P3/10 , A61P43/00 , C07D311/58 , C07D311/64 , A61K31/353 , C07D311/60
CPC分类号： C07D311/58
摘要： Disclosed are chromene derivatives represented by the following formula: ##STR1## wherein R.sup.1 s represent alkyl, alkoxy or like groups, R.sup.2 represents a hydrogen atom or an alkyl group, R.sup.3 represents a substituted or unsubstituted phenyl, naphthyl or heterocyclic group, and m stands for an integer of from 0 to 4, and their salts; and pharmaceuticals containing them as effective ingredients. The chromene derivatives and their salts show excellent AGE formation inhibitory action and are useful as preventives and therapeutics for diabetic complications.
摘要翻译：公开了由下式表示的色烯衍生物：其中R 1表示烷基，烷氧基或类似基团，R 2表示氢原子或烷基，R 3表示取代或未取代的苯基，萘基或杂环基，m表示 0至4，及其盐; 和含有它们作为有效成分的药物。色烯衍生物及其盐显示优异的AGE形成抑制作用，并且可用作糖尿病并发症的预防剂和治疗剂。

6. 发明授权

US5986144A Triazole derivative, preparation process thereof and pharmaceutical comprising the same as an effective ingredient 失效
标题翻译：三唑衍生物，其制备方法和包含其作为有效成分的药物
公开(公告)号：US5986144A
公开(公告)日：1999-11-16
申请号：US311057
申请日：1999-05-14
申请人： Minoru Tokizawa , Sunao Takeda , Yasushi Kaneko , Hiromichi Eto , Kazuya Ishida , Kazunori Maebashi , Masaru Matsumoto , Takemitsu Asaoka , Susumu Sato , Hideaki Matsuda
发明人： Minoru Tokizawa , Sunao Takeda , Yasushi Kaneko , Hiromichi Eto , Kazuya Ishida , Kazunori Maebashi , Masaru Matsumoto , Takemitsu Asaoka , Susumu Sato , Hideaki Matsuda
IPC分类号： C07D249/08 , C07D303/34 , C07D521/00 , C07C323/07
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D303/34
摘要： Described is a triazole derivative represented by the formula (1) or salt thereof, preparation process thereof, preparation intermediates represented by the formulas (2) and (3), and a pharmaceutical comprising the compound represented by the formula (1) or salt thereof. wherein n stands for 0, 1 or 2, X.sup.1 represents H or F and Y.sup.1 and Y.sup.2 each independently represents H, halogen or CF.sub.3.
摘要翻译：描述由式（1）表示的三唑衍生物或其盐，其制备方法，由式（2）和（3）表示的制备中间体，以及包含式（1）表示的化合物或其盐的药物。其中n表示0,1或2，X 1表示H或F，Y 1和Y 2各自独立地表示H，卤素或CF 3。

7. 发明授权

US6063945A Triazole derivative or salt thereof 失效
标题翻译：三唑衍生物或其盐
公开(公告)号：US6063945A
公开(公告)日：2000-05-16
申请号：US327516
申请日：1999-06-08
申请人： Minoru Tokizawa , Sunao Takeda , Yasushi Kaneko , Hiromichi Eto , Kazuya Ishida , Kazunori Maebashi , Masaru Matsumoto , Takemitsu Asaoka , Susumu Sato , Hideaki Matsuda
发明人： Minoru Tokizawa , Sunao Takeda , Yasushi Kaneko , Hiromichi Eto , Kazuya Ishida , Kazunori Maebashi , Masaru Matsumoto , Takemitsu Asaoka , Susumu Sato , Hideaki Matsuda
IPC分类号： C07D249/08 , C07D303/34 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D303/34
摘要： A compound having formula (2): ##STR1## wherein R represents hydrogen, a straight or branched C.sub.1-10 alkyl group, a C.sub.7-11 aralkyl group or a C.sub.2-10 carboacyl group and m stands for 1 to 5.
摘要翻译：具有式（2）的化合物：其中R表示氢，直链或支链C 1-10烷基，C 7-11芳烷基或C 2-10烷酰基，m代表1至5。

8. 发明授权

US5962509A Dithiolylidene acetamide derivatives 失效
标题翻译：二硫代亚乙酰胺衍生物
公开(公告)号：US5962509A
公开(公告)日：1999-10-05
申请号：US169989
申请日：1998-10-13
申请人： Fumio Ishii , Kinichi Mogi , Hiromichi Eto , Susumu Sato , Hideaki Matsuda
发明人： Fumio Ishii , Kinichi Mogi , Hiromichi Eto , Susumu Sato , Hideaki Matsuda
IPC分类号： A61K31/385 , A61P3/08 , A61P3/10 , A61P43/00 , C07D339/06 , C07D339/02
CPC分类号： C07D339/06
摘要： Disclosed are dithiolylidene acetamide derivatives represented by the following formula: ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and each independently represent a hydrogen atom or an alkyl group, or salts thereof; and pharmaceuticals containing them as effective ingredients. The dithiolylidene acetamide derivatives and their salts show AGE formation inhibitory action and are useful as preventives and therapeutics for diabetic complications.
摘要翻译：公开了由下式表示的二亚噻吩基乙酰胺衍生物：其中R1和R2可以相同或不同，各自独立地表示氢原子或烷基，或其盐; 和含有它们作为有效成分的药物。二硫代亚乙酰胺衍生物及其盐显示AGE形成抑制作用，可用作糖尿病并发症的预防药物和治疗剂。

9. 发明授权

US5945438A Triazole derivative and pharmaceutical comprising the same as an effective ingredient 失效
标题翻译：三唑衍生物和包含与有效成分相同的药物
公开(公告)号：US5945438A
公开(公告)日：1999-08-31
申请号：US767694
申请日：1996-12-17
申请人： Minoru Tokizawa , Sunao Takeda , Yasushi Kaneko , Hiromichi Eto , Kazuya Ishida , Kazunori Maebashi , Masaru Matsumoto , Takemitsu Asaoka , Susumu Sato , Hideaki Matsuda
发明人： Minoru Tokizawa , Sunao Takeda , Yasushi Kaneko , Hiromichi Eto , Kazuya Ishida , Kazunori Maebashi , Masaru Matsumoto , Takemitsu Asaoka , Susumu Sato , Hideaki Matsuda
IPC分类号： C07D249/08 , C07D303/34 , C07D521/00 , A61K31/41
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D303/34
摘要： Described is a triazole derivative represented by the formula (1) or salt thereof, preparation process thereof, preparation intermediates represented by the formulas (2) and (3), and a pharmaceutical comprising the compound represented by the formula (1) or salt thereof. ##STR1## wherein n stands for 0, 1 or 2, X.sup.1 represents H or F and Y.sup.1 and Y.sup.2 each independently represents H, halogen or CF.sub.3.
摘要翻译：描述由式（1）表示的三唑衍生物或其盐，其制备方法，由式（2）和（3）表示的制备中间体，以及包含式（1）表示的化合物或其盐的药物。其中n表示0,1或2，X 1表示H或F，Y 1和Y 2各自独立地表示H，卤素或CF 3。

10. 发明授权

US06174900B1 Substituted piperidine derivative for treating urinary disturbance 失效
标题翻译：用于治疗尿失禁的替代哌啶衍生物
公开(公告)号：US06174900B1
公开(公告)日：2001-01-16
申请号：US09332444
申请日：1999-06-14
申请人： Tomomi Okada , Fujiko Konno , Terumitsu Kaihoh , Masago Ishikawa , Yoshinori Takahashi , Hiroyuki Mizuno , Haruyoshi Honda , Susumu Sato , Hideaki Matsuda
发明人： Tomomi Okada , Fujiko Konno , Terumitsu Kaihoh , Masago Ishikawa , Yoshinori Takahashi , Hiroyuki Mizuno , Haruyoshi Honda , Susumu Sato , Hideaki Matsuda
IPC分类号： A61K31445
CPC分类号： C07D401/12 , C07D211/58 , C07D409/12
摘要： Disclosed herein is a substituted piperidine derivative represented by the following general formula (1): wherein R1 means an aryl or heteroaryl group which may have at least one substituent, R2 denotes an alkyl, alkenyl or aralkyl group, R3 stands for a hydrogen atom or an alkyl group, and R4 is a hydrogen atom, an alkyl group, or an aryl, heteroaryl, aralkyl, aralkenyl or heteroaralkyl group which may have at least one substituent, or a salt thereof. A medicine including this compound is also disclosed. The compound has excellent anticholinergic effect and calcium antagonism and inhibits reflex bladder contraction and is hence useful for prophylaxis of and treatment for a urinary disturbance such as pollakiuria.
摘要翻译：本文公开了由以下通式（1）表示的取代的哌啶衍生物：其中R 1表示可具有至少一个取代基的芳基或杂芳基，R 2表示烷基，烯基或芳烷基，R 3表示氢原子或烷基，可以具有至少一个取代基的芳基，杂芳基，芳烷基，芳烯基或杂芳烷基，或其盐。还公开了包含该化合物的药物。该化合物具有优异的抗胆碱能作用和钙拮抗作用并抑制反射膀胱收缩，因此可用于预防和治疗尿频紊乱如尿频。

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